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1

Chemical composition and in vitro schistosomicidal activity of the essential oil of Plectranthus neochilus grown in Southeast Brazil.  

PubMed

The chemical composition and the in vitro schistosomicidal effects of the essential oil of Plectranthus neochilus (PN-EO) grown in Southeast Brazil was studied. ?-Caryophyllene (1; 28.23%), ?-thujene (2; 12.22%), ?-pinene (3; 12.63%), ?-pinene (4; 6.19%), germacrene D (5; 5.36%), and caryophyllene oxide (6; 5.37%) were the major essential oil constituents. This chemical composition differed from that previously reported for specimens harvested in Africa. Concerning the in vitro schistosomicidal activity against adult Schistosoma mansoni worms, PN-EO was considered to be active, but less effective than the positive control praziquantel (PZQ) in terms of separation of coupled pairs, mortality, decrease in the motor activity, and tegumental alterations. However, PN-EO caused an interesting dose-dependent reduction in the number and the percentage of developed S. mansoni eggs. These results suggest that PN-EO might be very promising for the development of new schistosomicidal agents. PMID:22083928

Caixeta, Soraya C; Magalhăes, Lizandra G; de Melo, Nathalya I; Wakabayashi, Kamila A L; Aguiar, Gabriela de P; Aguiar, Daniela de P; Mantovani, André L L; Alves, Jacqueline M; Oliveira, Pollyanna F; Tavares, Denise C; Groppo, Milton; Rodrigues, Vanderlei; Cunha, Wilson R; Veneziani, Rodrigo C S; da Silva Filho, Ademar A; Crotti, Antônio E M

2011-11-01

2

Furofuran lignans display schistosomicidal and trypanocidal activities.  

PubMed

Parasitic diseases continue to be a major worldwide health problem, and there is an urgent need for development of therapeutic drugs. This paper describes synthesis of dehydrodiferulic acid dilactone 1 and dehydrodisinapic acid dilactone 2 furofuran lignans by oxidative coupling of ferulic and sinapic acids, respectively. Their schistosomicidal, trypanocidal, and leishmanicidal activities were evaluated in vitro against Schistosoma mansoni adult worms, trypomastigote and amastigotes forms of Trypanosoma cruzi, and promastigote forms of Leishmania amazonensis. Compound 1 did not display significant schistosomicidal activity, but it presented potent trypanocidal activity, since it induced death of trypomastigotes and amastigotes with IC50/24h of 9.3?M and 7.3?M, respectively. Compound 2 had slight trypanocidal and schistosomicidal activities. None of the compounds were active against L. amazonensis. These results demonstrated that furofuran lignans are potentially useful for anti-parasitic drugs development and should be further investigated. PMID:25200100

Andrade e Silva, Márcio Luis; Esperandim, Viviane Rodrigues; Ferreira, Daniele da Silva; Magalhăes, Lizandra Guidi; Lima, Thais Coelho; Cunha, Wilson Roberto; Nanayakkara, Dhammika N P; Pereira, Ana Carolina; Bastos, Jairo Kenupp

2014-11-01

3

In Vitro Schistosomicidal Activity of Some Brazilian Cerrado Species and Their Isolated Compounds  

PubMed Central

Miconia langsdorffii Cogn. (Melastomataceae), Roupala montana Aubl. (Proteaceae), Struthanthus syringifolius (Mart.) (Loranthaceae), and Schefflera vinosa (Cham. & Schltdl.) Frodin (Araliaceae) are plant species from the Brazilian Cerrado whose schistosomicidal potential has not yet been described. The crude extracts, fractions, the triterpenes betulin, oleanolic acid, ursolic acid and the flavonoids quercetin 3-O-?-D-rhamnoside, quercetin 3-O-?-D-glucoside, quercetin 3-O-?-D-glucopyranosyl-(1-2)-?-L-rhamnopyranoside and isorhamnetin 3-O-?-D-glucopyranosyl-(1-2)-?-L-rhamnopyranoside were evaluated in vitro against Schistosoma mansoni adult worms and the bioactive n-hexane fractions of the mentioned species were also analyzed by GC-MS. Betulin was able to cause worm death percentage values of 25% after 120?h (at 100??M), and 25% and 50% after 24 and 120?h (at 200??M), respectively; besides the flavonoid quercetin 3-O-?-D-rhamnoside promoted 25% of death of the parasites at 100??M. Farther the flavonoids quercetin 3-O-?-D-glucoside and quercetin 3-O-?-D-rhamnoside at 100??M exhibited significantly reduction in motor activity, 75% and 87.5%, respectively. Biological results indicated that crude extracts of R. montana, S. vinosa, and M. langsdorffii and some n-hexane and EtOAc fractions of this species were able to induce worm death to some extent. The results suggest that lupane-type triterpenes and flavonoid monoglycosides should be considered for further antiparasites studies. PMID:22924053

Cunha, Nayanne Larissa; Uchôa, Camila Jacintho de Mendonça; Cintra, Lucas Silva; de Souza, Herbert Cristian; Peixoto, Juliana Andrade; Silva, Claudia Peres; Magalhăes, Lizandra Guidi; Gimenez, Valéria Maria Meleiro; Groppo, Milton; Rodrigues, Vanderlei; da Silva Filho, Ademar Alves; Andrade e Silva, Márcio Luís; Cunha, Wilson Roberto; Pauletti, Patrícia Mendonça; Januário, Ana Helena

2012-01-01

4

In vitro schistosomicidal activity of some brazilian cerrado species and their isolated compounds.  

PubMed

Miconia langsdorffii Cogn. (Melastomataceae), Roupala montana Aubl. (Proteaceae), Struthanthus syringifolius (Mart.) (Loranthaceae), and Schefflera vinosa (Cham. & Schltdl.) Frodin (Araliaceae) are plant species from the Brazilian Cerrado whose schistosomicidal potential has not yet been described. The crude extracts, fractions, the triterpenes betulin, oleanolic acid, ursolic acid and the flavonoids quercetin 3-O-?-D-rhamnoside, quercetin 3-O-?-D-glucoside, quercetin 3-O-?-D-glucopyranosyl-(1-2)-?-L-rhamnopyranoside and isorhamnetin 3-O-?-D-glucopyranosyl-(1-2)-?-L-rhamnopyranoside were evaluated in vitro against Schistosoma mansoni adult worms and the bioactive n-hexane fractions of the mentioned species were also analyzed by GC-MS. Betulin was able to cause worm death percentage values of 25% after 120?h (at 100??M), and 25% and 50% after 24 and 120?h (at 200??M), respectively; besides the flavonoid quercetin 3-O-?-D-rhamnoside promoted 25% of death of the parasites at 100??M. Farther the flavonoids quercetin 3-O-?-D-glucoside and quercetin 3-O-?-D-rhamnoside at 100??M exhibited significantly reduction in motor activity, 75% and 87.5%, respectively. Biological results indicated that crude extracts of R. montana, S. vinosa, and M. langsdorffii and some n-hexane and EtOAc fractions of this species were able to induce worm death to some extent. The results suggest that lupane-type triterpenes and flavonoid monoglycosides should be considered for further antiparasites studies. PMID:22924053

Cunha, Nayanne Larissa; Uchôa, Camila Jacintho de Mendonça; Cintra, Lucas Silva; de Souza, Herbert Cristian; Peixoto, Juliana Andrade; Silva, Claudia Peres; Magalhăes, Lizandra Guidi; Gimenez, Valéria Maria Meleiro; Groppo, Milton; Rodrigues, Vanderlei; da Silva Filho, Ademar Alves; Andrade E Silva, Márcio Luís; Cunha, Wilson Roberto; Pauletti, Patrícia Mendonça; Januário, Ana Helena

2012-01-01

5

Schistosomicidal activity of the essential oil of Ageratum conyzoides L. (Asteraceae) against adult Schistosoma mansoni worms.  

PubMed

The in vitro schistosomicidal effects of the essential oil of Ageratum conyzoides L. (Ac-EO) against adult worms of Schistosoma mansoni is reported in this paper. Concerning this activity, Ac-EO was considered to be active, but less effective than the positive control (praziquantel, PZQ) in terms of separation of coupled pairs, mortality, decrease in motor activity, and tegumental alterations. However, Ac-EO caused an interesting dose-dependent reduction in the number of eggs of S. mansoni. Precocene I (74.30%) and (E)-caryophyllene (14.23%) were identified as the two major constituents of Ac-EO. These compounds were tested individually and were found to be much less effective than Ac-EO and PZQ. A mixture of the two major compounds in a ratio similar to that found in the Ac-EO was also less effective than Ac-EO, thus revealing that there are no synergistic effects between these components. These results suggest that the essential oil of A. conyzoides is very promising for the development of new schistosomicidal agents. PMID:21245809

de Melo, Nathalya I; Magalhaes, Lizandra G; de Carvalho, Carlos E; Wakabayashi, Kamila A L; de P Aguiar, Gabriela; Ramos, Rafael C; Mantovani, Andre L L; Turatti, Izabel C C; Rodrigues, Vanderlei; Groppo, Milton; Cunha, Wilson R; Veneziani, Rodrigo C S; Crotti, Antônio E M

2011-01-01

6

Fungal transformation and schistosomicidal effects of pimaradienoic acid.  

PubMed

The schistosomicidal effects of pimaradienoic acid (PA) and two derivatives, obtained by fungal transformation in the presence of Aspergillus ochraceus, were investigated. PA was the only compound with antischistosomal activity among the three diterpenes studied, with the ability to significantly reduce the viability of the parasites at concentrations ranging from 25 to 100 ?M. PA also promoted morphological alterations of the tegument of Schistosoma mansoni, separated all the worm couples, and affected the production and development of eggs. Moreover, this compound was devoid of toxicity toward human fibroblasts. In a preliminary in vivo experiment, PA at a dose of 100 mg/kg significantly diminished the number of parasites in infected Balb/c mice. Taken together, these results show that PA may be potentially employed in the discovery of novel schistosomicidal agents, and that diterpenes are an important class of natural compounds for the investigation of agents capable of fighting the parasite responsible for human schistosomiasis. PMID:22899607

Porto, Thiago S; da Silva Filho, Ademar A; Magalhăes, Lizandra G; dos Santos, Raquel A; Furtado, Niege A J C; Arakawa, Nilton S; Said, Suraia; de Oliveira, Dionéia C R; Gregório, Luiz E; Rodrigues, Vanderlei; Veneziani, Rodrigo C S; Ambrósio, Sérgio R

2012-08-01

7

In Vitro and In Vivo Anti-Schistosomal Activity of the Alkylphospholipid Analog Edelfosine  

PubMed Central

Background Schistosomiasis is a parasitic disease caused by trematodes of the genus Schistosoma. Five species of Schistosoma are known to infect humans, out of which S. haematobium is the most prevalent, causing the chronic parasitic disease schistosomiasis that still represents a major problem of public health in many regions of the world and especially in tropical areas, leading to serious manifestations and mortality in developing countries. Since the 1970s, praziquantel (PZQ) is the drug of choice for the treatment of schistosomiasis, but concerns about relying on a single drug to treat millions of people, and the potential appearance of drug resistance, make identification of alternative schistosomiasis chemotherapies a high priority. Alkylphospholipid analogs (APLs), together with their prototypic molecule edelfosine (EDLF), are a family of synthetic antineoplastic compounds that show additional pharmacological actions, including antiparasitic activities against several protozoan parasites. Methodology/Principal Findings We found APLs ranked edelfosine> perifosine> erucylphosphocholine> miltefosine for their in vitro schistosomicidal activity against adult S. mansoni worms. Edelfosine accumulated mainly in the worm tegument, and led to tegumental alterations, membrane permeabilization, motility impairment, blockade of male-female pairing as well as induction of apoptosis-like processes in cells in the close vicinity to the tegument. Edelfosine oral treatment also showed in vivo schistosomicidal activity and decreased significantly the egg burden in the liver, a key event in schistosomiasis. Conclusions/Significance Our data show that edelfosine is the most potent APL in killing S. mansoni adult worms in vitro. Edelfosine schistosomicidal activity seems to depend on its action on the tegumental structure, leading to tegumental damage, membrane permeabilization and apoptosis-like cell death. Oral administration of edelfosine diminished worm and egg burdens in S. mansoni-infected CD1 mice. Here we report that edelfosine showed promising antischistosomal properties in vitro and in vivo. PMID:25302497

Yepes, Edward; Varela-M, Rubén E.; López-Abán, Julio; Dakir, E. L. Habib; Mollinedo, Faustino; Muro, Antonio

2014-01-01

8

A study of the distribution of schistosomicidal drug H-3-7505 in mice  

SciTech Connect

The authors have studied the distribution of H-3 labelled schistosomicidal drug in mice by autoradiography. The H-3-labelled substances were found in liver and kidney and in successfully decreasing amounts in brain, lung, heart, fat, testis, pancreas and spleen. In various cells the silver granules were present mainly in the cytoplasms but a few in the nucleus. After administration of this labelled schistosomicidal drug, the mice were killed and studied in groups successively at 4, 8, 24 hrs. No difference in the distribution of silver granules were observed. This fact indicated that, this drug was rapidly absorbed and highly concentrated with a long duration of reservation in liver. All of these favours the schistosomicidal effect of the drug. As this drug was highly concentrated in the cytoplasm of liver cells, that might provide a pathophysiologic basis for the explanation of jaundice in the clinical practice. Moreover, the appearance of toxic reaction in nervous system may be related to the relatively high concentration of the drug distributed in the brain.

Hao, T.

1985-05-01

9

Spotlight on the in vitro effect of artemisinin-naphthoquine phosphate on Schistosoma mansoni and its snail host Biomphalaria alexandrina.  

PubMed

Malaria and schistosomiasis are the two most important parasitic diseases in the tropics and sub-tropics with geographic overlap. Efforts have been made for developing new schistosomicidal drugs, or testing existing drugs originally used for non-related diseases. The antimalarial artemisinin-naphthoquine phosphate combination (CO-ArNp) was recently reported to be a promising novel antischistosomal therapy with potent in vivo activity against Schistosoma mansoni. In this work, we report the in vitro dose- and time-response effect of CO-ArNp against the Egyptian strain of S. mansoni, and its snail host, Biomphalaria alexandrina. Incubation of adult S. mansoni with CO-ArNp at 40 or 20 ?g/ml for 48 or 72 h killed all worms. Exposure of S. mansoni miracidia and cercariae to the molluscicidal LC50 of CO-ArNp (16.8 ?g/ml) resulted in 100% mortality of the free larval stages within 90 and 15 min, respectively. Moreover, incubation of adult B. alexandrina snails with this drug combination killed all snails at 40 ?g/ml within 24h. Scanning electron microscope revealed marked morphological and tegumental alterations on the different stages of the parasite and its snail soft tissue. Our study highlights the schistosomicidal and molluscicidal effects of artemisinin-naphthoquine phosphate. No doubt more studies are needed to clarify its potential value to control schistosomiasis. PMID:25291045

El-Beshbishi, Samar N; El Bardicy, Samia; Tadros, Menerva; Ayoub, Magda; Taman, Amira

2015-01-01

10

In vitro antisickling activity of cromolyn sodium.  

PubMed

The improvement in sickle cell disease (SCD) children receiving cromolyn sodium therapy prompted us to investigate its antisickling activity in vitro. The number of sickle cells was determined in deoxygenated blood samples from 15 children with severe SCD. At the eight concentrations tested, cromolyn sodium exhibited a significantly higher activity than pentoxifylline, the standard compound. Therefore cromolyn sodium would appear to be an interesting candidate for SCD therapy and deserves further in vivo investigations. PMID:9886306

Fall, A B; Toppet, M; Ferster, A; Fondu, P; Vanhaelen-Fastré, R; Vanhaelen, M

1998-12-01

11

In vitro activity of aminosterols against dermatophytes.  

PubMed

We recently reported that aminosterols are fungicidal due to their disrupting the outer membranes of yeasts and that they have a significant in vitro activity against various mould species. Yet, their activity against dermatophytes had never been tested. This study's objective was to evaluate the in vitro activity of squalamine and a synthetic aminosterol derivative (ASD) against various dermatophytes. Susceptibility testing of squalamine, ASD, terbinafine, and griseofulvin was performed, in triplicate, in accord with the Clinical Laboratory and Standards Institute's M38-A2 procedure, using an 80% growth inhibition endpoint. The studies included the following dermatophytes: Trichophyton rubrum, T. mentagrophytes, T. soudanense, Microsporum canis, M. audouinii, M. persicolor; M. cookie and M. gypseum. Squalamine and ASD showed significant in vitro activity against these dermatophytes. The minimum inhibitory concentrations (MICs) ranged from 4-16 mg/l and from 2-8 mg/l for squalamine and ASD, respectively. These findings support further clinical studies of aminosterols activity against superficial dermatophyte infections. PMID:22998181

Coulibaly, Oumar; Alhanout, Kamel; L'Ollivier, Coralie; Brunel, Jean-Michel; Thera, Mahamadou A; Djimdé, Abdoulaye A; Doumbo, Ogobara K; Piarroux, Renaud; Ranque, Stéphane

2013-04-01

12

[The in vitro activity of veterinary antiseptics].  

PubMed

The in vitro activity of 28 veterinary antiseptic drugs was studied on 4 bacterial strains either with or without calf serum. Eight preparations (VT Dose, Dulcidrine, Collyre Clément, Cronic, Detecaďne, Lotion Maudor, Tano-Patt, Aurikan), half of which were eye-lotions, were found to be non antiseptic according to AFNOR standards. In the presence of calf serum, 4 other preparations (Albacetine, Nybocaďne, Pediplasme, Pedifort) did not meet the standard NF T 72.171 criteria. PMID:2111651

Maris, P

1990-01-01

13

Interference with Hemozoin Formation Represents an Important Mechanism of Schistosomicidal Action of Antimalarial Quinoline Methanols  

PubMed Central

Background The parasitic trematode Schistosoma mansoni is one of the major causative agents of human schistosomiasis, which afflicts 200 million people worldwide. Praziquantel remains the main drug used for schistosomiasis treatment, and reliance on the single therapy has been prompting the search for new therapeutic compounds against this disease. Our group has demonstrated that heme crystallization into hemozoin (Hz) within the S. mansoni gut is a major heme detoxification route with lipid droplets involved in this process and acting as a potential chemotherapeutical target. In the present work, we investigated the effects of three antimalarial compounds, quinine (QN), quinidine (QND) and quinacrine (QCR) in a murine schistosomiasis model by using a combination of biochemical, cell biology and molecular biology approaches. Methodology/Principal Findings Treatment of S. mansoni-infected female Swiss mice with daily intraperitoneal injections of QN, and QND (75 mg/kg/day) from the 11th to 17th day after infection caused significant decreases in worm burden (39%–61%) and egg production (42%–98%). Hz formation was significantly inhibited (40%–65%) in female worms recovered from QN- and QND-treated mice and correlated with reduction in the female worm burden. We also observed that QN treatment promoted remarkable ultrastructural changes in male and female worms, particularly in the gut epithelium and reduced the granulomatous reaction to parasite eggs trapped in the liver. Microarray gene expression analysis indicated that QN treatment increased the expression of transcripts related to musculature, protein synthesis and repair mechanisms. Conclusions The overall significant reduction in several disease burden parameters by the antimalarial quinoline methanols indicates that interference with Hz formation in S. mansoni represents an important mechanism of schistosomicidal action of these compounds and points out the heme crystallization process as a valid chemotherapeutic target to treat schistosomiasis. PMID:19597543

Corręa Soares, Juliana B. R.; Menezes, Diego; Vannier-Santos, Marcos A.; Ferreira-Pereira, Antonio; Almeida, Giulliana T.; Venancio, Thiago M.; Verjovski-Almeida, Sergio; Zishiri, Vincent K.; Kuter, David; Hunter, Roger; Egan, Timothy J.; Oliveira, Marcus F.

2009-01-01

14

Original article In vitro cholesterol-lowering activity  

E-print Network

Original article In vitro cholesterol-lowering activity of Lactobacillus plantarum of these microorganisms. One of the most studied properties is the cholesterol-lowering activity of bacteria and five Lactobacillus paracasei strains isolated from cheese were studied in vitro for their cholesterol

Paris-Sud XI, Université de

15

In Vitro Activities of Trioxaquines against Schistosoma mansoni?  

PubMed Central

We report the in vitro activities of trioxaquines against larval and adult-stage schistosomes at 5 and 50 ?g/ml, respectively. Such activities are equivalent to that of praziquantel, the major and rather unique drug currently used for the treatment of schistosomiasis. In this range of concentrations, artemisinin derivatives (artesunate and artemether) have no activity. PMID:19596887

Boissier, Jérôme; Coslédan, Frédéric; Robert, Anne; Meunier, Bernard

2009-01-01

16

In Vitro Activity of Voriconazole Against Candida Species  

Microsoft Academic Search

The in vitro activity of voriconazole was compared with that of itraconazole and fluconazole against 181 isolates of Candida albicans, 124 isolates of Candida glabrata, and 20 isolates of Candida krusei obtained from the early 1980s through the mid-1990s. Voriconazole had greater intrinsic activity than fluconazole or itraconazole against all three Candida species. For C. glabrata, C. krusei, and C.

Carol A Kauffman; Lidija T Zarins

1998-01-01

17

In vitro estrogenic activity of Achillea millefolium L  

Microsoft Academic Search

Isolation and biological characterization of pure compounds was used to identify and characterize estrogenic activity and estrogen receptors (ER) preference in chemical components of Achillea millefolium. This medicinal plant is used in folk medicine as an emmenagogue. In vitro assay, based on recombinant MCF-7 cells, showed estrogenic activity in a crude extract of the aerial parts of A. millefolium. After

G. Innocenti; E. Vegeto; S. Dall’Acqua; P. Ciana; M. Giorgetti; E. Agradi; A. Sozzi; G. Fico; F. Tomč

2007-01-01

18

ASSESSMENT OF IN VITRO ANDROGENIC ACTIVITY IN KRAFT MILL EFFLUENT  

EPA Science Inventory

Detection of In Vitro Androgenic Activity in Feedlot Effluent. Lambright, CS 1 , Guillette, LJ, Jr.2, Gray, LE, Jr.1 , 1USEPA, NHEERL, RTP, NC, 2 University of Florida, Dept. of Zoology, Gainesville FL Recent studies have shown the presence of androgenic activity in water...

19

Evaluation of the Anti-Schistosoma mansoni Activity of Thiosemicarbazones and Thiazoles  

PubMed Central

Schistosomiasis is a chronic and debilitating disease caused by a trematode of the genus Schistosoma and affects over 207 million people. Chemotherapy is the only immediate recourse for minimizing the prevalence of this disease and involves predominately the administration of a single drug, praziquantel (PZQ). Although PZQ has proven efficacy, there is a recognized need to develop new drugs as schistosomicides since studies have shown that repeated use of this drug in areas of endemicity may cause a temporary reduction in susceptibility in isolates of Schistosoma mansoni. Hydrazones, thiosemicarbazones, phthalimides, and thiazoles are thus regarded as privileged structures used for a broad spectrum of activities and are potential candidates for sources of new drug prototypes. The present study determined the in vitro schistosomicidal activity of 10 molecules containing these structures. During the assays, parameters such motility and mortality, oviposition, morphological changes in the tegument, cytotoxicity, and immunomodulatory activity caused by these compounds were evaluated. The results showed that compounds formed of thiazole and phthalimide led to higher mortality of worms, with a significant decline in motility, inhibition of pairing and oviposition, and a mortality rate of 100% starting from 144 h of exposure. These compounds also stimulated the production of nitric oxide and tumor necrosis factor alpha (TNF-?), thereby demonstrating the presence of immunomodulatory activity. The phthalyl thiazole LpQM-45 caused significant ultrastructural alterations, with destruction of the tegument in both male and female worms. According to the present study, phthalyl thiazole compounds possess antischistosomal activities and should form the basis for future experimental and clinical trials. PMID:24165185

de Oliveira, Sheilla Andrade; de Oliveira Filho, Gevânio Bezerra; Moreira, Diogo Rodrigo Magalhaes; Gomes, Paulo André Teixeira; da Silva, Anekécia Lauro; de Barros, Andréia Ferreira; da Silva, Aline Caroline; dos Santos, Thiago André Ramos; Pereira, Valéria Ręgo Alves; Gonçalves, Gabriel Gazzoni Araújo; Brayner, Fábio André; Alves, Luiz Carlos; Wanderley, Almir Gonçalves; Leite, Ana Cristina Lima

2014-01-01

20

In vitro activity of voriconazole against Mexican oral yeast isolates.  

PubMed

Oral candidiasis is the most prevalent complication in HIV-infected and AIDS patients. Topical antifungal treatment is useful for the initial episodes of oral candidiasis, but most patients suffer more than one episode and fluconazole or itraconazole can help in the management, and voriconazole may represent a useful alternative agent for the treatment of recalcitrant oral and oesophageal candidiasis. The aim of this research was to study the in vitro activity of voriconazole and fluconazole against Mexican oral isolates of clinically relevant yeast. The in vitro susceptibility of 187 oral yeast isolates from HIV-infected and healthy Mexicans was determined for fluconazole and voriconazole by the M44-A disc diffusion method. At 24 h, fluconazole was active against 179 of 187 isolates (95.7 %). Moreover, a 100% susceptibility to voriconazole was observed. Voriconazole and fluconazole are highly active in vitro against oral yeast isolates. This study provides baseline data on susceptibilities to both antifungal agents in Mexico. PMID:19389066

Sánchez Vargas, Luis Octavio; Eraso, Elena; Carrillo-Muńoz, Alfonso Javier; Aguirre, José Manuel; Gaitán-Cepeda, Luis Alberto; Quindós, Guillermo

2010-05-01

21

In vitro genotoxic activities of fibrous erionite.  

PubMed Central

A high incidence of mesothelioma has been reported from some villages in Cappadocia, Turkey. This type of cancer is usually associated with the inhalation of asbestos, but on the basis of the most prevalent fibre in the dust from these villages, the Turkish outbreak has been attributed to the inhalation of zeolite fibres. A counter hypothesis, based on the detection of very small quantities of chrysotile and tremolite in strata samples and human lung tissue, postulates a significant role of these minerals as one of several factors contributing to pleural disease. A respirable fraction of erionite, (from Oregon, USA, but with similar characteristics to the fibres found in Turkey), has some in vitro genotoxic properties associated with many conventional carcinogens. In this study these fibres caused an increase in morphological transformation and unscheduled DNA repair synthesis (UDS) in C3H10T1/2 cells and UDS in the human lung cell line--A549. It is therefore suggested that exposure to fibrous erionite alone may be sufficient to cause the high incidence of pleural tumours observed in Turkey. Images Figure 1 Figure 3 PMID:6303378

Poole, A.; Brown, R. C.; Turver, C. J.; Skidmore, J. W.; Griffiths, D. M.

1983-01-01

22

In Vitro Antibacterial Activity of Essential Oils against Streptococcus pyogenes.  

PubMed

Streptococcus pyogenes plays an important role in the pathogenesis of tonsillitis. The present study was conducted to evaluate the in vitro antibacterial activities of 18 essential oils chemotypes from aromatic medicinal plants against S. pyogenes. Antibacterial activity of essential oils was investigated using disc diffusion method. Minimum Inhibitory Concentration of essential oils showing an important antibacterial activity was measured using broth dilution method. Out of 18 essential oils tested, 14 showed antibacterial activity against S. pyogenes. Among them Cinnamomum verum, Cymbopogon citratus, Thymus vulgaris CT thymol, Origanum compactum, and Satureja montana essential oils exhibited significant antibacterial activity. The in vitro results reported here suggest that, for patients suffering from bacterial throat infections, if aromatherapy is used, these essential oils, considered as potential antimicrobial agents, should be preferred. PMID:23662123

Sfeir, Julien; Lefrançois, Corinne; Baudoux, Dominique; Derbré, Séverine; Licznar, Patricia

2013-01-01

23

In Vitro Antibacterial Activity of Essential Oils against Streptococcus pyogenes  

PubMed Central

Streptococcus pyogenes plays an important role in the pathogenesis of tonsillitis. The present study was conducted to evaluate the in vitro antibacterial activities of 18 essential oils chemotypes from aromatic medicinal plants against S. pyogenes. Antibacterial activity of essential oils was investigated using disc diffusion method. Minimum Inhibitory Concentration of essential oils showing an important antibacterial activity was measured using broth dilution method. Out of 18 essential oils tested, 14 showed antibacterial activity against S. pyogenes. Among them Cinnamomum verum, Cymbopogon citratus, Thymus vulgaris CT thymol, Origanum compactum, and Satureja montana essential oils exhibited significant antibacterial activity. The in vitro results reported here suggest that, for patients suffering from bacterial throat infections, if aromatherapy is used, these essential oils, considered as potential antimicrobial agents, should be preferred. PMID:23662123

Sfeir, Julien; Lefrançois, Corinne; Baudoux, Dominique; Derbré, Séverine; Licznar, Patricia

2013-01-01

24

Antibacterial activity of raspberry cordial in vitro.  

PubMed

Raspberry juice cordial has a long anecdotal use in Australia for the prophylaxis and treatment of gastroenteritis in livestock, cage birds and humans. The antimicrobial properties of raspberry juice cordial, raspberry juice, raspberry leaf extract and a commercial brand of raspberry leaf tea were investigated against five human pathogenic bacteria and two fungi. Raspberry cordial and juice were found to significantly reduce the growth of several species of bacteria, including Salmonella, Shigella and E. coli, but demonstrated no antifungal activity. No antimicrobial activity was detected in the leaf extract or tea. PMID:11798288

Ryan, T; Wilkinson, J M; Cavanagh, H M

2001-12-01

25

IN VITRO IRON BIOAVAILABILITY AND ANTIOXIDANT ACTIVITY OF RAISINS  

Technology Transfer Automated Retrieval System (TEKTRAN)

Iron bioavailabilities and antioxidant activities of three common generic raisin types, Golden Thompson, Dipped Thompson and Sun dried Thompson, were quantified and compared. Iron bioavailability was assessed with an in vitro digestion/Caco 2 cell culture model using cell ferritin formation as an i...

26

Evaluation of the antioxidant activity of melatonin in vitro  

Microsoft Academic Search

Melatonin is being increasingly promoted as a treatment for “jet lag” and insomnia and has been suggested to act as an antioxidant in vivo. The antioxidant and potential pro-oxidant activities of melatonin were investigated in vitro. Melatonin was able to scavenge hypochlorous acid (HOC1) at a rate sufficient to protect catalase against inactivation by this molecule. Melatonin could also prevent

Karyn-Ann Marshall; Rüssel J. Reiter; Burkhard Poeggeler; Okezie I. Aruoma; Barry Halliwell

1996-01-01

27

In vitro activity of HR 810, a new cephalosporin.  

PubMed Central

The in vitro susceptibility of 409 clinical isolates to HR 810, a new cephalosporin, was evaluated and compared with their susceptibility to aztreonam, cefazolin, ceftazidime, imipenem, moxalactam, piperacillin, and gentamicin. On a weight basis, the activity of HR 810 against gram-negative bacilli was equivalent or superior to that of the other beta-lactam agents except imipenem. PMID:6593000

Bertram, M A; Bruckner, D A; Young, L S

1984-01-01

28

In vitro antiprotozoal activity of the leaves of Artemisia ludoviciana  

Microsoft Academic Search

The inhabitants of Northeast of Mexico use an infusion of leaves from Artemisia ludoviciana as an antidiarrheal remedy. The aqueous, methanol, acetone and hexane leaf extracts from mature plants were found to be active in vitro against the parasitic protozoa Entamoeba histolytica and Giardia lamblia.

Salvador Said Fernández; Monica Celina Ramos Guerra; Benito David Mata Cárdenas; Javier Vargas Villarreal; Licet Villarreal Trevińo

2005-01-01

29

In vitro antiprotozoal activity of the leaves of Artemisia ludoviciana.  

PubMed

The inhabitants of Northeast of Mexico use an infusion of leaves from Artemisia ludoviciana as an antidiarrheal remedy. The aqueous, methanol, acetone and hexane leaf extracts from mature plants were found to be active in vitro against the parasitic protozoa Entamoeba histolytica and Giardia lamblia. PMID:15975735

Said Fernández, Salvador; Ramos Guerra, Monica Celina; Mata Cárdenas, Benito David; Vargas Villarreal, Javier; Villarreal Trevińo, Licet

2005-07-01

30

In Vitro Activity of OPT-80 against Clostridium difficile  

PubMed Central

Clostridium difficile remains the major cause of nosocomial diarrhea. Reports on impaired susceptibility of C. difficile to metronidazole and vancomycin and frequent relapses of patients after therapy necessitate the search for new substances. With this study, the activity of OPT-80, a new macrocycle, against 207 C. difficile strains and against other obligately anaerobic bacteria was tested. OPT-80 showed high in vitro activity against all C. difficile strains tested. PMID:15155234

Ackermann, Grit; Löffler, Birgit; Adler, Daniela; Rodloff, Arne C.

2004-01-01

31

Antimalarial activity of plumbagin in vitro and in animal models  

PubMed Central

Background Plumbagin is the major active constituent in several plants including Plumbago indica Linn. (root). This compound has been shown to exhibit a wide spectrum of biological and pharmacological activities. The present study aimed to evaluate the in vitro and in vivo antimalarial activity of plumbagin including its acute and subacute toxicity in mice. Methods In vitro antimalarial activity of plumbagin against K1 and 3D7 Plasmodium falciparum clones were assessed using SYBR Green I based assay. In vivo antimalarial activity was investigated in Plasmodium berghei-infected mouse model (a 4-day suppressive test). Results Plumbagin exhibited promising antimalarial activity with in vitro IC50 (concentration that inhibits parasite growth to 50%) against 3D7 chloroquine-sensitive P. falciparum and K1 chloroquine-resistant P. falciparum clones of 580 (270–640) and 370 (270–490) nM, respectively. Toxicity testing indicated relatively low toxicity at the dose levels up to 100 (single oral dose) and 25 (daily doses for 14 days) mg/kg body weight for acute and subacute toxicity, respectively. Chloroquine exhibited the most potent antimalarial activity in mice infected with P. berghei ANKA strain with respect to its activity on the reduction of parasitaemia on day 4 and the prolongation of survival time. Conclusions Plumbagin at the dose of 25 mg/kg body weight given for 4 days was safe and produced weak antimalarial activity. Chemical derivatization of the parent compound or preparation of modified formulation is required to improve its systemic bioavailability. PMID:24410949

2014-01-01

32

In vitro phytotoxicity and antioxidant activity of selected flavonoids.  

PubMed

The knowledge of flavonoids involved in plant-plant interactions and their mechanisms of action are poor and, moreover, the structural characteristics required for these biological activities are scarcely known. The objective of this work was to study the possible in vitro phytotoxic effects of 27 flavonoids on the germination and early radical growth of Raphanus sativus L. and Lepidium sativum L., with the aim to evaluate the possible structure/activity relationship. Moreover, the antioxidant activity of the same compounds was also evaluated. Generally, in response to various tested flavonoids, germination was only slightly affected, whereas significant differences were observed in the activity of the various tested flavonoids against radical elongation. DPPH test confirms the antioxidant activity of luteolin, quercetin, catechol, morin, and catechin. The biological activity recorded is discussed in relation to the structure of compounds and their capability to interact with cell structures and physiology. No correlation was found between phytotoxic and antioxidant activities. PMID:22754304

De Martino, Laura; Mencherini, Teresa; Mancini, Emilia; Aquino, Rita Patrizia; De Almeida, Luiz Fernando Rolim; De Feo, Vincenzo

2012-01-01

33

In Vitro Phytotoxicity and Antioxidant Activity of Selected Flavonoids  

PubMed Central

The knowledge of flavonoids involved in plant-plant interactions and their mechanisms of action are poor and, moreover, the structural characteristics required for these biological activities are scarcely known. The objective of this work was to study the possible in vitro phytotoxic effects of 27 flavonoids on the germination and early radical growth of Raphanus sativus L. and Lepidium sativum L., with the aim to evaluate the possible structure/activity relationship. Moreover, the antioxidant activity of the same compounds was also evaluated. Generally, in response to various tested flavonoids, germination was only slightly affected, whereas significant differences were observed in the activity of the various tested flavonoids against radical elongation. DPPH test confirms the antioxidant activity of luteolin, quercetin, catechol, morin, and catechin. The biological activity recorded is discussed in relation to the structure of compounds and their capability to interact with cell structures and physiology. No correlation was found between phytotoxic and antioxidant activities. PMID:22754304

De Martino, Laura; Mencherini, Teresa; Mancini, Emilia; Aquino, Rita Patrizia; De Almeida, Luiz Fernando Rolim; De Feo, Vincenzo

2012-01-01

34

Theta-like activity in the limbic cortex in vitro.  

PubMed

The generation of EEG theta rhythm in the mammalian limbic cortex is a prime example of rhythmic activity that involves central mechanisms of oscillations and synchrony. This EEG pattern has been extensively studied since 1938, when Jung and Kornmuller (28) (Eine methodik der ableitung lokalisierter potential schwankingen aus subcorticalen hirnyebieten, Arch. Psychiat. Neruenkr. 109 (1938) 1-30) demonstrated the first theta recordings in the hippocampal formation of rabbits. In 1986 we demonstrated for the first time that bath perfusion of hippocampal slices with the cholinergic agonist, carbachol, resulted in theta-like oscillations. Since this initial demonstration of in vitro theta-like activity, we have carried out a number of experiments in an attempt to answer the following question: what are the similarities between cholinergic-induced in vitro theta-like activity and theta rhythm which naturally occurs in the in vivo preparation. Thus far, our studies have provided strong evidence that theta-like activity recorded in vitro shares many of the physiological and pharmacological properties of theta rhythm observed in vivo. PMID:9579321

Konopacki, J

1998-03-01

35

In Vitro Activity of 39 Antimicrobial Agents Against Treponema hyodysenteriae  

PubMed Central

The in vitro activities of 39 antimicrobial agents against 23 isolates of Treponema hyodysenteriae, the majority of which were field isolates, were determined by the agar dilution technique. Quinoxalines, pleuromutilin, nitroimidazoles, and nitrofuran were the most active. Their activities ranged from ?0.10 to 1.56 ?g/ml. Lincomycin, penicillins, chloramphenicol, tetracyclines, cephalosporins, three peptides (virginiamycin, thiopeptin, and bacitracin), and one aminoglycoside (gentamicin) exhibited intermediate levels of activity ranging from 0.39 to 50 ?g/ml. Four peptides (enduracidin, viomycin, bicyclomycin, and colistin), three aminoglycosides (kanamycin, streptomycin, and neomycin), polyene, and other agents, including novobiocin, vancomycin, rifampin, nalidixic acid, and p-arsanilic acid, displayed limited activities ranging from 12.5 to ?100 ?g/ml. Macrolides showed varying degrees of activity depending upon isolates. PMID:464566

Kitai, Kazuhisa; Kashiwazaki, Mamoru; Adachi, Yoshikazu; Kume, Tsuneo; Arakawa, Akira

1979-01-01

36

In vitro antioxidant activity of Retama monosperma (L.) Boiss.  

PubMed

The relationship between the antioxidant activity and the phenolic contents (total polyphenol, flavonoid and condensed tannin) of Retama monosperma (Fabaceae), used commonly in the traditional medicine of Mediterranean regions, was investigated. The antioxidant activities of the various fractions (toluene, chloroform, ethyl acetate and butanol) of the hydromethanolic extract of the seeds, stems and flowers have been evaluated using in vitro 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) radical scavenging activities and Phosphomolybdic acid assays and were compared to ascorbic acid. A significant high Pearson's correlations between flavonoid content and antioxidant activities (r = 0.91) with Phosphomolybdic acid assays and (r = - 0.79) with IC50 DPPH radical scavenging activities. However, there was no correlation between condensed tannin and antioxidant activities. The results obtained in the present study indicate that the ethyl acetate fraction of seeds is a potential source of natural antioxidant for R. monosperma. PMID:25033217

Belmokhtar, Zoubir; Harche, Meriem Kaid

2014-01-01

37

Activities of Taurolidine In Vitro and in Experimental Enterococcal Endocarditis  

Microsoft Academic Search

In vitro, the antimicrobial agent taurolidine inhibited virtually all of the bacteria tested, including vanco- mycin-resistant enterococci, oxacillin-resistant staphylococci, and Stenotrophomonas maltophilia, at concentra- tions between 250 and 2,000 mg\\/ml. Taurolidine was not effective in experimental endocarditis. While it appears unlikely that this antimicrobial would be useful for systemic therapy, its bactericidal activity and the resistance rates found (<1029) are

C. Torres-Viera; C. Thauvin-Eliopoulos; M. Souli; P. DeGirolami; M. G. Farris; C. B. Wennersten; R. D. Sofia; G. M. Eliopoulos

2000-01-01

38

Pentamidine Is Active In Vitro against Fusarium Species  

PubMed Central

Fusariosis is an emerging opportunistic mycosis against which currently used antifungals have limited activity. Here, we investigated the in vitro activities of pentamidine (PNT) against 10 clinical isolates of Fusarium species (five Fusarium solani isolates and five non-F. solani isolates) by using the National Committee for Clinical Laboratory Standards microdilution method in three different media (RPMI, RPMI-2, and a yeast nitrogen base medium), disk diffusion testing, and viability dye staining. PNT had significant activities against all 10 Fusarium isolates. Non-F. solani isolates were more susceptible than F. solani isolates (P < 0.05). Additionally, PNT was fungicidal against all non-F. solani isolates, whereas it had fungistatic effects against four of the five F. solani isolates. PNT also exhibited greater activity against conidial than against hyphal development of the fungus. This fungicidal activity against non-F. solani Fusarium isolates was confirmed microscopically after staining of PNT-treated Fusarium oxysporum hyphae with the fluorescent viability dyes 5,(6)-carboxyfluorescein diacetate (CFDA) and bis-(1,3-dibutylbarbituric acid) trimethine oxonol (DiBAC). The MICs at which 50% of the isolates were inhibited (2 ?g/ml for non-F. solani isolates and 4 ?g/ml for F. solani isolates) and the minimum fungicidal concentration at which 50% of the isolates were killed (8 ?g/ml for non-F. solani isolates) were much lower than the PNT tissue concentrations previously reported in humans using conventional daily intravenous PNT dosing. Finally, PNT was more active against Fusarium isolates in a hypoxic environment of in vitro growth (P < 0.05). This finding may be clinically significant, because Fusarium, an angiotropic mold, causes tissue infarcts with resultant low tissue perfusion. Our findings suggest that PNT may have a role in the management of Fusarium infections. Future in vivo studies are needed to verify these in vitro findings. PMID:14506038

Lionakis, Michail S.; Lewis, Russell E.; Samonis, George; Kontoyiannis, Dimitrios P.

2003-01-01

39

In vitro activity of the nisin dehydratase NisB.  

PubMed

The biosynthesis of several classes of ribosomally synthesized and posttranslationally modified peptides involves dehydration of serine and threonine residues. For class I lantibiotics, thiopeptides, and goadsporin, this dehydration is catalyzed by lanthionine biosynthetic enzyme B (LanB) or LanB-like proteins. Although LanB proteins have been studied since 1992, in vitro reconstitution of their dehydration activity has been elusive. We show here the in vitro activity of the dehydratase involved in the biosynthesis of the food preservative nisin (NisB). In vitro, NisB dehydrated its substrate peptide NisA eight times in the presence of glutamate, ATP, Mg(2+), and the ribosomal/membrane fraction of bacterial cell extract. Mutation of 23 highly conserved residues of NisB identified a number of amino acids that are essential for dehydration activity. In addition, these mutagenesis studies identified three mutants, R786A, R826A, and H961A, that result in multiple glutamylations of the NisA substrate. Glutamylation was observed during both Escherichia coli coexpression of NisA with these mutants and in vitro assays. Treatment of the glutamylated substrate with WT NisB results in dehydrated NisA, suggesting that the glutamylated peptide is an intermediate in dehydration. Collectively, these studies suggest that dehydration involves glutamylation of the side chains of Ser and Thr followed by elimination. The latter step has precedent in the virginiamycin resistance protein virginiamycin B lyase. These studies will facilitate investigation of other LanB proteins involved in the biosynthesis of lantibiotics, thiopeptides, and goadsporin. PMID:23589847

Garg, Neha; Salazar-Ocampo, Luis M A; van der Donk, Wilfred A

2013-04-30

40

Hepatoprotective and antihyperliposis activities of in vitro cultured Anoectochilus formosanus.  

PubMed

The pharmacological effects of an aqueous extract of the whole plants of in vitro cultured Anoectochilus formosanus were investigated experimentally for hepatoprotective and antihyperliposis activities. The extract showed significant antihepatotoxic activity against carbon tetrachloride induced cytotoxicity in primary cultured rat hepatocytes. In an assay for antihyperliposis using aurothioglucose-induced obese mice, the extract suppressed significantly the increase in the weights of body and liver, ameliorated triglyceride levels in the liver and serum, and also significantly reduced the deposition of adipose tissue. PMID:12557243

Du, Xiao-Ming; Sun, Ning-Yi; Hayashi, Jun; Chen, Yang; Sugiura, Minoru; Shoyama, Yukihiro

2003-01-01

41

In Vitro Antifungal Activity of Isavuconazole against Madurella mycetomatis  

PubMed Central

Currently, therapy of black-grain mycetoma caused by Madurella mycetomatis consists of extensive debridement of the infected tissue combined with prolonged antifungal therapy with ketoconazole or itraconazole. In the present study, the in vitro activity of the new triazole isavuconazole toward M. mycetomatis was evaluated. Isavuconazole appeared to have high activity against M. mycetomatis, with MICs ranging from ?0.016 to 0.125 ?g/ml. Due to its favorable pharmacokinetics, isavuconazole could be a promising antifungal agent in the treatment of mycetoma. PMID:22964246

Meis, Jacques F.; Curfs-Breuker, Ilse; Fahal, Ahmed H.

2012-01-01

42

In vitro antifungal activity of isavuconazole against Madurella mycetomatis.  

PubMed

Currently, therapy of black-grain mycetoma caused by Madurella mycetomatis consists of extensive debridement of the infected tissue combined with prolonged antifungal therapy with ketoconazole or itraconazole. In the present study, the in vitro activity of the new triazole isavuconazole toward M. mycetomatis was evaluated. Isavuconazole appeared to have high activity against M. mycetomatis, with MICs ranging from ?0.016 to 0.125 ?g/ml. Due to its favorable pharmacokinetics, isavuconazole could be a promising antifungal agent in the treatment of mycetoma. PMID:22964246

Kloezen, Wendy; Meis, Jacques F; Curfs-Breuker, Ilse; Fahal, Ahmed H; van de Sande, Wendy W J

2012-11-01

43

In vitro activity of nicotinamide/antileishmanial drug combinations.  

PubMed

To improve the management of leishmaniasis, new drugs and/or alternative therapeutic strategies are required. Combination therapy of antileishmanial drugs is currently considered as one of the most rational approaches to lower treatment failure rate and limit drug resistance spreading. Nicotinamide (NAm), also known as vitamin B3 that is already is used in human therapy, exerts in vitro antileishmanial activity. Drug combination studies, performed on L. infantum axenic amastigotes, revealed that NAm significantly improves the antileishmanial activity of trivalent antimony in a synergistic manner while it shows additive activity with amphotericin B and slightly antagonizes pentamidine activity. NAm also significantly increases the toxicity of pentavalent antimony against the intracellular forms of L. infantum, L. amazonensis and L. braziliensis. The potential of NAm to be used as adjuvant during leishmaniasis chemotherapy is further discussed. PMID:20884376

Gazanion, Elodie; Vergnes, Baptiste; Seveno, Marie; Garcia, Deborah; Oury, Bruno; Ait-Oudhia, Khatima; Ouaissi, Ali; Sereno, Denis

2011-01-01

44

In Vitro Activities of Benzimidazoles against Echinococcus multilocularis Metacestodes  

PubMed Central

Alveolar echinococcosis, caused by the larval (metacestode) stage of the tapeworm Echinococcus multilocularis, is a lethal parasitosis of the liver prevalent in the Northern Hemisphere. For chemotherapy the benzimidazole derivatives mebendazole and albendazole were introduced, and their use has resulted in a significant improvement in the survival rates. However, data from experiments with animals and clinical observations indicate that these drugs elicit only parasitostatic activity and in most cases are not able to completely eliminate the parasitic metacestode tissue. In the present study, we applied a culture system for the in vitro growth and proliferation of E. multilocularis metacestodes to analyze the parasitostatic and parasitocidal potential of mebendazole. Here, we demonstrate for the first time that at concentrations of >0.1 ?M, i.e., at concentrations used for therapy of human alveolar echinococcosis, this antihelminth drug is parasitocidal in vitro. Viability assessment was performed by infection experiments with Meriones unguiculatus and mebendazole-treated metacestode tissue and by reverse transcription-PCR for the detection of E. multilocularis mRNA. The E. multilocularis in vitro model proved to be a valuable tool for the analysis of the potential of antihelminth drugs. PMID:9593125

Jura, Heike; Bader, Augustinus; Frosch, Matthias

1998-01-01

45

Antiprotozoal and cytotoxic activities in vitro of Colombian Annonaceae.  

PubMed

Ethnobotanical and chemotaxonomical studies for antiparasitic activity of Colombian Annonaceae were carried out. In vitro antiprotozoal activity of 36 extracts obtained from six different species was determined against promastigotes of three Leishmania species, epimastigotes of Trypanosoma cruzi and both chloroquine sensitive (F32) and resistant (W2) Plasmodium falciparum. Cytotoxic activity was evaluated in U-937 cells. Active extracts were selected according their selectivity index (SI). Extracts from Annona muricata, Rollinia exsucca, Rollinia pittieri and Xylopia aromatica were active against Leishmania spp. and Trypanosoma cruzi showing IC50 values lower than 25 microg/ml. Hexane extract from Rollinia pittieri leaves was the most selective against Trypanosoma cruzi and Leishmania spp. (IS=10 and 16, respectively). The extracts from Desmopsis panamensis, Pseudomalmea boyacana, Rollinia exsucca and Rollinia pittieri showed good antiplasmodial activity (IC50 < 10 microg/ml). No correlation between antiplasmodial activity and inhibition of beta-hematin production was found. The present study gives specific and useful information about antiprotozoal and cytotoxic activities of some Annonaceae extracts. Results presented here also demonstrate which plants and/or plant parts could be useful in the treatment of leishmaniasis, Chagas' disease and malaria. PMID:17296281

Osorio, Edison; Arango, Gabriel Jaime; Jiménez, Nora; Alzate, Fernando; Ruiz, Grace; Gutiérrez, David; Paco, Marco Antonio; Giménez, Alberto; Robledo, Sara

2007-05-22

46

[Antitumor activity of the root of Euphorbia helioscopic in vitro].  

PubMed

Antitumor activity of the aquatic extract the root of Euphorbia helioscopia L (EWE) in Vitro were studied. Viable cells count, MTT staining and colonal formation assays of three kinds of cancer cells were used to assess the antitumor activity. Determined by viable cells count, the IC50 values of EWE against 7721, Hela, MKN-45 cells were 1.26, 1.98, 1.72 mg/ml respectively (72 h). Determined MTT staining, the IC50 values EWE against 7721, Hela, MKN-45 cells were 1.43, 1.67, 0.97 mg/ml. Determined by colonal formation, the inhibition rate of EWE (4 mg/ml) against 7721, Hela, MKN-45 cells were 59.8%, 66.4%, 70.5%. The results indicated that EWE had obvious antitumor activity. PMID:12575050

Cai, Y; Wang, J; Liang, B

1999-02-01

47

In vitro antibacterial activity of a new quinolone, NM394.  

PubMed Central

NM394 is a new 6-fluoroquinolone antibacterial agent with a tricyclic structure which has a bridge that connects the N-1 and C-2 positions of the quinolone. The antibacterial activity of NM394 against clinical isolates of staphylococci, streptococci, enterococci, members of the family Enterobacteriaceae, and Pseudomonas aeruginosa was equal to or one-half that of ciprofloxacin. NM394 was as active as ofloxacin against gram-positive bacteria and was two to eight times more active against gram-negative bacteria, including P. aeruginosa. NM394 was two to eight times more active than enoxacin against gram-positive and gram-negative bacteria. The MICs of NM394 against Escherichia coli and P. aeruginosa at pH 5.5 were reduced 4 to 16 times compared with those at pH 7.0. Ciprofloxacin, ofloxacin, and enoxacin were 2 to 32 times less active against these two bacteria and Staphylococcus aureus at an acidic pH than they were at pH 7.0. In the presence of 5 mM Mg2+, the MICs of all of these drugs increased 2 to 32 times, but they were only slightly affected by 5 mM Ca2+, type of medium, serum, or size of inoculum. NM394 showed potent bactericidal activity and inhibited the supercoiling activity of E. coli DNA gyrase. The in vitro antibacterial profile of NM394 is similar to that of other 6-fluoroquinolones. PMID:1667251

Ozaki, M; Matsuda, M; Tomii, Y; Kimura, K; Kazuno, K; Kitano, M; Kise, M; Shibata, K; Otsuki, M; Nishino, T

1991-01-01

48

The estrogenic activity of phthalate esters in vitro.  

PubMed Central

A large number of phthalate esters were screened for estrogenic activity using a recombinant yeast screen. a selection of these was also tested for mitogenic effect on estrogen-responsive human breast cancer cells. A small number of the commercially available phthalates tested showed extremely weak estrogenic activity. The relative potencies of these descended in the order butyl benzyl phthalate (BBP) > dibutyl phthalate (DBP) > diisobutyl phthalate (DIBP) > diethyl phthalate (DEP) > diisiononyl phthalate (DINP). Potencies ranged from approximately 1 x 10(6) to 5 x 10(7) times less than 17beta-estradiol. The phthalates that were estrogenic in the yeast screen were also mitogenic on the human breast cancer cells. Di(2-ethylhexyl) phthalate (DEHP) showed no estrogenic activity in these in vitro assays. A number of metabolites were tested, including mono-butyl phthalate, mono-benzyl phthalate, mono-ethylhexyl phthalate, mon-n-octyl phthalate; all were wound to be inactive. One of the phthalates, ditridecyl phthalate (DTDP), produced inconsistent results; one sample was weakly estrogenic, whereas another, obtained from a different source, was inactive. analysis by gel chromatography-mass spectometry showed that the preparation exhibiting estrogenic activity contained 0.5% of the ortho-isomer of bisphenol A. It is likely that the presence of this antioxidant in the phthalate standard was responsible for the generation of a dose-response curve--which was not observed with an alternative sample that had not been supplemented with o,p'-bisphenol A--in the yeast screen; hence, DTDP is probably not weakly estrogenic. The activities of simple mixtures of BBP, DBP, and 17beta-estradiol were assessed in the yeast screen. No synergism was observed, although the activities of the mixtures were approximately additive. In summary, a small number of phthalates are weakly estrogenic in vitro. No data has yet been published on whether these are also estrogenic in vitro. No data has yet been published on whether these are also estrogenic in vivo; this will require tests using different classes of vertebrates and different routes of exposure. Images p802-a Figure 1. Figure 2. A Figure 2. B Figure 2. C Figure 3. Figure 4. Figure 5. A Figure 5. B Figure 5. C Figure 6. Figure 7. PMID:9347895

Harris, C A; Henttu, P; Parker, M G; Sumpter, J P

1997-01-01

49

Antiulcer and in vitro antioxidant activities of Jasminum grandiflorum L.  

PubMed

The study was aimed at evaluating the antiulcer and antioxidant activities of 70% ethanolic axtract of leaves of Jasminum grandiflorum L. (JGLE). The leaves of Jasminum grandiflorum L. (Family: Oleaceae) is used in folk medicine for treating ulcerative stomatitis, skin diseases, ulcers, wounds, corns - a hard or soft hyperkeratosis of the sole of the human foot secondary to friction and pressure (Stedman's Medical Dictionary, 28th ed. Lippincott Williams & Wilkins, Philadelphia. p. 443), etc., Antiulcerogenic activity of JGLE (100 and 200 mg/kg, b.w., orally) was evaluated employing aspirin + pylorus ligation (APL) and alcohol (AL) induced acute gastric ulcer models and ulcer-healing activity using acetic acid-induced (AC) chronic ulcer model in rats. Both the antisecretory and cytoprotection hypothesis were evaluated. The antioxidant activity of JGLE has been assayed by using in vitro methods like 2,2-diphenyl-1-picrylhydrazylhydrate (DPPH) assay, reductive ability, superoxide anion scavenging activity, nitric oxide scavenging activity and total phenolic content, in order to explain the role of antioxidant principles in the antiulcerogenic activity of the extract. There was a significant (P<0.01) dose-dependent decrease in the ulcerative lesion index produced by all the three models in rats as compared to the standard drug famotidine (20 mg/kg, b.w. orally). The reduction in gastric fluid volume, total acidity and an increase in the pH of the gastric fluid in APL rats proved the antisecretory activity of JGLE. Additionally, JGLE completely healed the ulcer within 20 days of treatment in AC model as evidenced by histopathological studies. Like antiulcer activity, the free radical scavenging activities of JGLE depends on concentration and increased with increasing amount of the extract. These results suggest that leaves of Jasminum grandiflorum possess potential antiulcer activity, which may be attributed to its antioxidant mechanism of action. PMID:17125945

Umamaheswari, M; Asokkumar, K; Rathidevi, R; Sivashanmugam, A T; Subhadradevi, V; Ravi, T K

2007-04-01

50

The in Vitro estrogenic activities of triclosan and triclocarban.  

PubMed

Triclosan (TCS) and triclocarban (TCC), as broad spectrum antibacterial agents, are distributed widely in the environment and humans. Most studies have focused on their distribution and biodegradation, but the endocrine-disrupting effects of these chemicals, especially their estrogenic effects, are still unclear. In the present study, we investigated the estrogenic effects of TCS and TCC using a series of in vitro assays, including the ER reporter gene assay in the CV-1 cells, E-screen assay and evaluation of estrogen-responsive genes in the MCF-7 cells. The tested concentrations of TCS and TCC were both from 1?×?10(-9) to 1?×?10(-6) ?M. Results showed that TCS and TCC exerted estrogenic activities by inducing luciferase activities in an ER reporter gene assay, promoting the proliferation of the MCF-7 cells, up-regulating the expression of pS2 and down-regulating ER? expression at both the mRNA and protein levels in the MCF-7 cells. We further found that TCS and TCC could alter the expression of multiple microRNAs (mir-22, mir-206 and mir-193b) in the MCF-7 cells, which would help understand the mechanisms of their estrogenic effects on regulating the expression of ER?. In brief, our results demonstrated the potential estrogenic effects and profiled in vitro data for further risk assessment of TCS and TCC. PMID:24740835

Huang, Hongyu; Du, Guizhen; Zhang, Wei; Hu, Jialei; Wu, Di; Song, Ling; Xia, Yankai; Wang, Xinru

2014-09-01

51

In vitro antibacterial activity of Q-35, a new fluoroquinolone.  

PubMed

The in vitro activity of Q-35, an 8-methoxy fluoroquinolone, was compared with those of ofloxacin, ciprofloxacin, tosufloxacin, lomefloxacin, and sparfloxacin. The MICs of Q-35 for 90% of strains tested (MIC90s) of Staphylococcus aureus, methicillin-resistant S. aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, and Streptococcus pyogenes were 0.2, 6.25, 0.2, 0.39, and 0.39 micrograms/ml, respectively. The activity of Q-35 was 4- to 16-fold greater than those of ofloxacin, ciprofloxacin and lomefloxacin but equal to those of tosufloxacin and sparfloxacin against these organisms. For 82 ciprofloxacin-resistant staphylococci (MIC90 = 100 micrograms/ml), Q-35 was the most active of the new quinolones tested (MIC90 = 6.25 micrograms/ml). The MIC90s of Q-35 against Escherichia coli, Enterobacter aerogenes, and Pseudomonas aeruginosa were 0.2, 0.78, and 12.5 micrograms/ml, respectively, and Q-35 was 2- to 16-fold less active than the other quinolones tested. Q-35 showed potent bactericidal activity and inhibited the supercoiling activity of DNA gyrase of S. aureus, E. coli, and P. aeruginosa. PMID:1329626

Ito, T; Otsuki, M; Nishino, T

1992-08-01

52

In vitro antibacterial activity of Q-35, a new fluoroquinolone.  

PubMed Central

The in vitro activity of Q-35, an 8-methoxy fluoroquinolone, was compared with those of ofloxacin, ciprofloxacin, tosufloxacin, lomefloxacin, and sparfloxacin. The MICs of Q-35 for 90% of strains tested (MIC90s) of Staphylococcus aureus, methicillin-resistant S. aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, and Streptococcus pyogenes were 0.2, 6.25, 0.2, 0.39, and 0.39 micrograms/ml, respectively. The activity of Q-35 was 4- to 16-fold greater than those of ofloxacin, ciprofloxacin and lomefloxacin but equal to those of tosufloxacin and sparfloxacin against these organisms. For 82 ciprofloxacin-resistant staphylococci (MIC90 = 100 micrograms/ml), Q-35 was the most active of the new quinolones tested (MIC90 = 6.25 micrograms/ml). The MIC90s of Q-35 against Escherichia coli, Enterobacter aerogenes, and Pseudomonas aeruginosa were 0.2, 0.78, and 12.5 micrograms/ml, respectively, and Q-35 was 2- to 16-fold less active than the other quinolones tested. Q-35 showed potent bactericidal activity and inhibited the supercoiling activity of DNA gyrase of S. aureus, E. coli, and P. aeruginosa. PMID:1329626

Ito, T; Otsuki, M; Nishino, T

1992-01-01

53

[In vitro antimycobacterial activities of a new quinolone, balofloxacin].  

PubMed

Balofloxacin (BLFX), a newly developed fluoroquinolone, was studied for its in vitro antimycobacterial activity by the agar dilution method with 7H11 agar medium. The MIC90s were as follows: 0.39 microgram/ml for M. tuberculosis, > 50 micrograms/ml for M. avium, > 50 micrograms/ml for M. intracellulare, 0.39 microgram/ml for M. kansasii, 0.39 microgram/ml for M. fortuitum, > 50 micrograms/ml for M. abscessus, and 50 micrograms/ml for M. chelonae. The antimycobacterial activity of BLFX was comparable or slightly inferior to that of levofloxacin (LVFX). Considering the present findings and pharmacokinetics of BFLX, it appears that BFLX may achieve favorable outcome in the treatment of patients with infection due to M. tuberculosis, M. kansasii, or M. fortuitum similar to that of ofloxacin or LVFX. PMID:11211780

Kawahara, S; Tada, A; Nagare, H

2001-01-01

54

In vitro Antioxidant Activities of Trianthema portulacastrum L. Hydrolysates  

PubMed Central

Hydrolysates of Trianthema portulacastrum in acidified methanol were evaluated for their total phenolic (TP) constituents and respective antioxidant activities using in vitro assays (i.e., 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, percent inhibition of linoleic acid peroxidation, and ferric reducing power). The observed results indicate that root, shoot, and leaf fractions of T. portulacastrum contain 50.75~98.09 mg gallic acid equivalents/g dry weight of TP. In addition, these fractions have substantial reducing potentials (0.10~0.59), abilities to inhibit peroxidation (43.26~89.98%), and DPPH radical scavenging capabilities (6.98~311.61 ?g/mL IC50). The experimental data not only reveal T. portulacastrum as potential source of valuable antioxidants, but also indicate that acidified methanol may be an ideal choice for the enhanced recovery of phenolic compounds with retained biological potential for the food and pharmaceutical industry. PMID:24772406

Yaqoob, Sadaf; Sultana, Bushra; Mushtaq, Muhammad

2014-01-01

55

In Vitro Anti-rotaviral Activity of Achillea kellalensis  

PubMed Central

Background Achillea kellalensis, which is frequently used by Chaharmahal va Bakhtiarians residing in, Southwest of Iran, as a traditional herbal medicine for the treatment of acute diarrhea, has been selected to examine its antiviral activities against bovine rotavirus and cell toxicity activity in MA-104 cells. Objectives The aim of this study was to evaluate the in vitro cytotoxic and anti-rotavirus properties of crude extracts of A. kellalensis. Materials and Methods The dried and powdered flowers of Achillea kellalensis were extracted with hot water and ethanol 50% (v/v). The cell viability and toxicity of the extracts were evaluated on MA-104 cells using four methods; trypan blue dye, NR, crystal violet and MTT assay. The in vitro anti-rotavirus properties were determined via four different assays, in order to evaluate the direct inhibition and/or the inhibition of viral replication. Results Cytotoxicity of two A. kellalensis extracts showed different concentrations. Hydro-alcoholic extract had low CC50 at 600 µg/mL by the NR assay while the aqueous extract had high CC50 at 1000µg/mL by the crystal violet method. In the simultaneous treatment assay and post treatment assay, the extracts were able to prevent viral replication and inhibit the viral CPE on MA-104 cells at 10 TCID50, but the extracts did not exhibit direct antiviral activity on rotavirus adsorption. The effective concentration (EC50) of both extracts was observed to be 100 µg/mL. Conclusions These results indicate that A. kellalensis extracts exert potent anti-rotaviral activity only after viral adsorption. The two extracts from A. kellalensis showed a good selectivity index. Also these results suggest that extracts prepared from the flowers of A. kellalensis may be potential anti-rotaviral agents in vivo and be useful in veterinary medicine. PMID:24624203

Taherkhani, Reza; Farshadpour, Fatemeh; Makvandi, Manoochehr

2013-01-01

56

Steroid dimers-in vitro cytotoxic and antimicrobial activities.  

PubMed

The in vitro cytotoxic activity of previously synthesized steroid dimers with different spacer group (sulfide, trithiolane ring or phosphorotrithioate) and the substituent at C-17 position was tested for their possible effects against following human tumor cell lines: cervical adenocarcinoma (HeLa), chronic myelogenous leukemia (K562) and two human breast cancer cell lines (MDA-MB-361 and MDA-MB-453). These compounds, applied at micromolar concentrations, exhibited cytotoxic activity of different intensity (compared with cisplatin as a control), modality and selectivity in these malignant cell lines. The best activity against all four cell cancer lines was exhibited by dimer-sulfides. All screened compounds exerted concentration-dependent cytotoxic activity against leukemia K562 cells. The compounds which exerted the most pronounced cytotoxic action exhibited notably higher cytotoxic activities against K562, HeLa and MDA-MB-453 cells in comparison to resting and PHA-stimulated PBMC, pointing to a significant selectivity in their antitumor actions. Examination of the mechanisms of cytotoxicity on leukemia K562 cells revealed pro-apoptotic action of each of the investigated compounds applied at concentrations 2IC50. The most prominent pro-apoptotic action was exhibited by dimer-sulfide of cholest-4-en-3-one. Furthermore, almost all of the tested compounds at IC50 concentrations induced G1 phase cell cycle arrest in K562 cells. Antimicrobial activity against Gram-positive, Gram-negative bacteria and fungal cells, and toxicity to brine shrimp Artemia salina, were evaluated. There was no antibacterial activity. The best antifungal activity was exhibited against Saccharomyces cerevisiae by dimers linked with trithiolane ring, indicating a selective activity of investigated compounds. PMID:24923733

Krsti?, Natalija M; Mati?, Ivana Z; Jurani?, Zorica D; Novakovi?, Irena T; Sladi?, Dušan M

2014-09-01

57

Synthesis of new 8-(5-substituted amino-1,3,4-oxadiazol-2-yl) and 8-(5-substituted amino-1,3,4-thiadiazol-2-yl) methoxyquinolines with antibilharzial activity.  

PubMed

Several 5-substituted amino-1,3,4-oxadiazol-2-yl and 5-substituted amino-1,3,4-thiadiazol-2-yl derivatives with different 8-hydroxyquinoline moieties in the 2-position were prepared and tested for their antiparasitic activity. Preliminary biological tests on mice experimentally infested with Schistosoma mansoni revealed that the new compounds show moderate schistosomicidal activity. PMID:6716252

Soliman, R; Mokhtar, H M; el Sadany, S K

1984-03-01

58

The in vitro biological activity of Lepidium meyenii extracts.  

PubMed

The biological activity of methanolic and aqueous extracts from dehydrated hypocotyls of Lepidium meyenii (Brassicaceae, vernacular name "maca"), was studied on rat hepatocytes and human breast cancer MCF-7 cells. The extracts did not exhibit cytotoxicity in hepatocyte primary cultures up to 10 mg/ml as measured by the MTT viability test, and lactate dehydrogenase (LDH) and aspartate aminotransferase (AST) leakage. Moreover, after 72 h, extracts inhibited LDH and AST leakage from the hepatocytes. When hepatocytes were intoxicated by t-butyl hydroperoxide, neither extract prevented oxidative damage. Both extracts showed weak antioxidant activity in the DPPH radical scavenging test with IC(50) values of 3.46 +/- 0.16 and 0.71 +/- 0.10 mg/ml, for aqueous and methanolic extracts, respectively. Thus, the observed effect on spontaneous enzyme leakage is probably mediated through mechanisms other than antioxidant activity. Both methanolic and aqueous extracts have shown estrogenic activity comparable with that of silymarin in MCF-7 cell line. Maca estrogenicity was exhibited in the range from 100 to 200 mug of extract per ml. The findings in the present study show that maca does not display in vitro hepatotoxicity. In contrast, a slight cytoprotective effect, probably not mediated by antioxidant capacity, was noted. Maca extracts exhibited estrogenic activity comparably to the effect of silymarin in MCF-7 cells. PMID:16528448

Valentová, K; Buckiová, D; Kren, V; Peknicová, J; Ulrichová, J; Simánek, V

2006-03-01

59

In-vitro Activity of Avermectins against Mycobacterium ulcerans.  

PubMed

Mycobacterium ulcerans causes Buruli ulcer (BU), a debilitating infection of subcutaneous tissue. There is a WHO-recommended antibiotic treatment requiring an 8-week course of streptomycin and rifampicin. This regime has revolutionized the treatment of BU but there are problems that include reliance on daily streptomycin injections and side effects such as ototoxicity. Trials of all-oral treatments for BU show promise but additional drug combinations that make BU treatment safer and shorter would be welcome. Following on from reports that avermectins have activity against Mycobacterium tuberculosis, we tested the in-vitro efficacy of ivermectin and moxidectin on M. ulcerans. We observed minimum inhibitory concentrations of 4-8 ?g/ml and time-kill assays using wild type and bioluminescent M. ulcerans showed a significant dose-dependent reduction in M. ulcerans viability over 8-weeks. A synergistic killing-effect with rifampicin was also observed. Avermectins are well tolerated, widely available and inexpensive. Based on our in vitro findings we suggest that avermectins should be further evaluated for the treatment of BU. PMID:25742173

Omansen, Till F; Porter, Jessica L; Johnson, Paul D R; van der Werf, Tjip S; Stienstra, Ymkje; Stinear, Timothy P

2015-03-01

60

In-vitro Activity of Avermectins against Mycobacterium ulcerans  

PubMed Central

Mycobacterium ulcerans causes Buruli ulcer (BU), a debilitating infection of subcutaneous tissue. There is a WHO-recommended antibiotic treatment requiring an 8-week course of streptomycin and rifampicin. This regime has revolutionized the treatment of BU but there are problems that include reliance on daily streptomycin injections and side effects such as ototoxicity. Trials of all-oral treatments for BU show promise but additional drug combinations that make BU treatment safer and shorter would be welcome. Following on from reports that avermectins have activity against Mycobacterium tuberculosis, we tested the in-vitro efficacy of ivermectin and moxidectin on M. ulcerans. We observed minimum inhibitory concentrations of 4–8 ?g/ml and time-kill assays using wild type and bioluminescent M. ulcerans showed a significant dose-dependent reduction in M. ulcerans viability over 8-weeks. A synergistic killing-effect with rifampicin was also observed. Avermectins are well tolerated, widely available and inexpensive. Based on our in vitro findings we suggest that avermectins should be further evaluated for the treatment of BU. PMID:25742173

Omansen, Till F.; Porter, Jessica L.; Johnson, Paul D. R.; van der Werf, Tjip S.; Stienstra, Ymkje; Stinear, Timothy P.

2015-01-01

61

In vitro radical scavenging activity of two Columbian Magnoliaceae  

NASA Astrophysics Data System (ADS)

The recent interest in the conservation of the tropical forest is due, at least in part, to the potential economic and health benefits that can be exploited from several plants. This report shows the in vitro antioxidant activity of some fractions isolated from leaves of two Columbian Magnoliaceae, Talauma hernandezii G. Lozano-C and Dugandiodendron yarumalense Lozano. The activity was determined using the radical monocation 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS·+) and the stable free radical 2-2-diphenyl-1-picrylhydrazyl (DPPH·), as part of general biological screening of these plants. The antioxidant capacity obtained from fractions was similar to those of ?-tocopherol, tert-butylated hydroxyanisole (BHA), and ascorbic acid. The most active scavenger extract was the fraction 7 (TAA = 48.6 mmol Trolox/kg extract and IC50 ? 0.01 kg extract/mmol DPPH); and the least active was the fraction 1 (TAA = 11.23 mmol Trolox/kg extract and IC50 = 0.21 kg extract/mmol DPPH) all of them isolated from D. yarumalense. These results suggest that these plants can be attractive as source of antioxidant compounds with the ability to reduce radicals like ATBS and DPPH.

Puertas M., Miguel A.; Mesa v., Ana M.; Sáez v., Jairo A.

2005-08-01

62

In vitro antimalarial activity and drug interactions of fenofibric acid.  

PubMed

Plasmodium falciparum has developed resistance to most available treatments, underscoring the need for novel antimalarial drugs. Fibrates are lipid-modifying agents used to reduce morbidity and mortality associated with cardiovascular disease. They may have antimalarial activity through modulation of P-glycoprotein and ATP-binding cassette subfamily A member (ABC-1)-mediated nutrient transport and/or via a putative peroxisome proliferator-activated receptor alpha-like protein. We therefore examined in vitro antimalarial activities of fibrates and their interactions with chloroquine and dihydroartemisinin in chloroquine-sensitive (3D7) and chloroquine-resistant (W2mef) strains of P. falciparum using the conventional isotopic assay microtechnique. A bioassay was used to assess inhibition activities of human plasma after therapeutic fenofibrate doses. Fenofibric acid, the main metabolite of fenofibrate, was the most potent of the fibrates tested, with mean 50% inhibitory concentrations of 152 nM and 1,120 nM for chloroquine-sensitive and -resistant strains, respectively. No synergistic interaction between fibrates and chloroquine or dihydroartemisinin was observed. Plasma fenofibric acid concentrations, quantified by high-performance liquid chromatography in seven healthy volunteers after treatment (mean, 15.3 mg/liter, or 48 ?M), inhibited P. falciparum. BLAST analysis revealed the likely presence of an ABC-1 transporter homolog in P. falciparum. Our findings demonstrate that fenofibric acid has activity similar to the activities of conventional antimalarial drugs at concentrations well below those achieved after therapeutic doses. It may inhibit P. falciparum growth by inhibiting intracellular lipid transport. PMID:22430967

Wong, Rina P M; Davis, Timothy M E

2012-06-01

63

Human filarial Wolbachia lipopeptide directly activates human neutrophils in vitro  

PubMed Central

The host inflammatory response to the Onchocerca volvulus endosymbiont, Wolbachia, is a major contributing factor in the development of chronic pathology in humans (onchocerciasis/river blindness). Recently, the toll-like pattern recognition receptor motif of the major inflammatory ligands of filarial Wolbachia, membrane-associated diacylated lipoproteins, was functionally defined in murine models of pathology, including mediation of neutrophil recruitment to the cornea. However, the extent to which human neutrophils can be activated in response to this Wolbachia pattern recognition motif is not known. Therefore, the responses of purified peripheral blood human neutrophils to a synthetic N-terminal diacylated lipopeptide (WoLP) of filarial Wolbachia peptidoglycan-associated lipoprotein (PAL) were characterized. WoLP exposure led to a dose-dependent activation of healthy, human neutrophils that included gross morphological alterations and modulation of surface expressed integrins involved in tethering, rolling and extravasation. WoLP exposure induced chemotaxis but not chemokinesis of neutrophils, and secretion of the major neutrophil chemokine, interleukin 8. WoLP also induced and primed the respiratory burst, and enhanced neutrophil survival by delay of apoptosis. These results indicate that the major inflammatory motif of filarial Wolbachia lipoproteins directly activates human neutrophils in vitro and promotes a molecular pathway by which human neutrophils are recruited to sites of Onchocerca parasitism. PMID:24909063

Tamarozzi, F; Wright, H L; Johnston, K L; Edwards, S W; Turner, J D; Taylor, M J

2014-01-01

64

Arrhenius temperature dependence of in vitro tissue plasminogen activator thrombolysis  

NASA Astrophysics Data System (ADS)

Stroke is a devastating disease and a leading cause of death and disability. Currently, the only FDA approved therapy for acute ischemic stroke is the intravenous administration of the thrombolytic medication, recombinant tissue plasminogen activator (tPA). However, this treatment has many contraindications and can have dangerous side effects such as intra-cerebral hemorrhage. These treatment limitations have led to much interest in potential adjunctive therapies, such as therapeutic hypothermia (T <= 35 °C) and ultrasound enhanced thrombolysis. Such interest may lead to combining these therapies with tPA to treat stroke, however little is known about the effects of temperature on the thrombolytic efficacy of tPA. In this work, we measure the temperature dependence of the fractional clot mass loss ?m(T) resulting from tPA exposure in an in vitro human clot model. We find that the temperature dependence is well described by an Arrhenius temperature dependence with an effective activation energy Eeff of 42.0 ± 0.9 kJ mole-1. Eeff approximates the activation energy of the plasminogen-to-plasmin reaction of 48.9 kJ mole-1. A model to explain this temperature dependence is proposed. These results will be useful in predicting the effects of temperature in future lytic therapies.

Shaw, George J.; Dhamija, Ashima; Bavani, Nazli; Wagner, Kenneth R.; Holland, Christy K.

2007-06-01

65

Influence of gold nanoparticles on platelets functional activity in vitro  

NASA Astrophysics Data System (ADS)

Now in the leading biomedical centers of the world approved new technology of laser photothermal destruction of cancer cells using plasmon gold nanoparticles. Investigations of influence of gold nanoparticles on white rat platelets aggregative activity in vitro have been made. Platelet aggregation was investigated in platelet rich plasma (PRP) with help of laser analyzer 230 LA <>, Russia). Aggregation inductor was ADP solution in terminal concentration 2.5 micromole (<>, Russia). Gold nanoshells soluted in salt solution were used for experiments. Samples of PRP were incubated with 50 or 100 ?l gold nanoshells solution in 5 minute, after that we made definition ADP induced platelet aggregation. We found out increase platelet function activity after incubation with nanoparticles solution which shown in maximum ADP-induced aggregation degree increase. Increase platelet function activity during intravenous nanoshells injection can be cause of thrombosis on patients. That's why before clinical application of cancer cell destruction based on laser photothermal used with plasmon gold nanoparticles careful investigations of thrombosis process and detail analyze of physiological blood parameters are very necessary.

Akchurin, Garif G.; Akchurin, George G.; Ivanov, Alexey N.; Kirichuk, Vyacheslav F.; Terentyuk, George S.; Khlebtsov, Boris N.; Khlebtsov, Nikolay G.

2008-02-01

66

Human filarial Wolbachia lipopeptide directly activates human neutrophils in vitro.  

PubMed

The host inflammatory response to the Onchocerca volvulus endosymbiont, Wolbachia, is a major contributing factor in the development of chronic pathology in humans (onchocerciasis/river blindness). Recently, the toll-like pattern recognition receptor motif of the major inflammatory ligands of filarial Wolbachia, membrane-associated diacylated lipoproteins, was functionally defined in murine models of pathology, including mediation of neutrophil recruitment to the cornea. However, the extent to which human neutrophils can be activated in response to this Wolbachia pattern recognition motif is not known. Therefore, the responses of purified peripheral blood human neutrophils to a synthetic N-terminal diacylated lipopeptide (WoLP) of filarial Wolbachia peptidoglycan-associated lipoprotein (PAL) were characterized. WoLP exposure led to a dose-dependent activation of healthy, human neutrophils that included gross morphological alterations and modulation of surface expressed integrins involved in tethering, rolling and extravasation. WoLP exposure induced chemotaxis but not chemokinesis of neutrophils, and secretion of the major neutrophil chemokine, interleukin 8. WoLP also induced and primed the respiratory burst, and enhanced neutrophil survival by delay of apoptosis. These results indicate that the major inflammatory motif of filarial Wolbachia lipoproteins directly activates human neutrophils in vitro and promotes a molecular pathway by which human neutrophils are recruited to sites of Onchocerca parasitism. PMID:24909063

Tamarozzi, F; Wright, H L; Johnston, K L; Edwards, S W; Turner, J D; Taylor, M J

2014-10-01

67

Amino ozonides exhibit in vitro activity against Echinococcus multilocularis metacestodes.  

PubMed

Artemisinin is an antimalarial sesquiterpene lactone that contains a 1,2,4-trioxane heterocycle. Dihydroartemisinin and artesunate demonstrated activity against Echinococcus multilocularis metacestodes in vitro but were not effective in a mouse model. In this study, the in vitro effects of a small library of synthetic ozonides (1,2,4-trioxolanes) were investigated. Initial compound screening against E. multilocularis metacestodes was performed at 20?M, and selected ozonides were further assessed in dose-response studies in metacestode cultures and mammalian cells. Transmission electron microscopy (TEM) was employed to characterise compound-induced structural alterations. At 20?M, the most potent ozonides (OZ401, OZ455, OZ491 and OZ494) led to death of ca. 60-100% of the parasites. Subsequent dose-response experiments demonstrated that OZ401, OZ455 and OZ491, which contain an aminopropylether substructure, were the most potent, with 50% inhibitory concentrations ranging from 11?M to 14?M. Cytotoxicity for these three ozonides, assessed in human foreskin fibroblasts, rat hepatoma cells and green monkey epithelial kidney (Vero) cells, was evident only at high concentrations. TEM demonstrated that OZ401 and OZ491 treatment induced considerable metabolic impairment in metacestodes at 1 day post exposure. At Day 3 post exposure, the germinal layer was severely distorted, although some intact cells were still visible, demonstrating that not all cell types in the parasite tissue were equally affected. Complete destruction of the germinal layer was noted at 5 days post exposure. Synthetic ozonides could represent interesting leads that will be further investigated in a suitable in vivo model of E. multilocularis infection. PMID:24239405

Küster, Tatiana; Kriegel, Nadja; Stadelmann, Britta; Wang, Xiaofang; Dong, Yuxiang; Vennerstrom, Jonathan L; Keiser, Jennifer; Hemphill, Andrew

2014-01-01

68

In vitro antimicrobial activity of ethanolic fractions of Cryptolepis sanguinolenta  

PubMed Central

Background Following claims that some plants have antimicrobial activities against infectious microbes, the in vitro antimicrobial activities of different solvent fractions of ethanolic extract of Cryptolepis sanguinolenta were evaluated against eight standard bacteria and clinical isolates. Methods The solvent partitioning protocol involving ethanol, petroleum ether, chloroform, ethyl acetate and water, was used to extract various fractions of dried pulverized Cryptolepis sanguinolenta roots. Qualitative phyto-constituents screening was performed on the ethanol extract, chloroform fraction and the water fraction. The Kirby Bauer disk diffusion method was employed to ascertain the antibiogram of the test organisms while the agar diffusion method was used to investigate the antimicrobial properties of the crude plant extracts. The microplate dilution method aided in finding the MICs while the MBCs were obtained by the method of Nester and friends. The SPSS 16.0 version was used to analyze the percentages of inhibitions and bactericidal activities. Results The phytochemical screening revealed the presence of alkaloids, reducing sugars, polyuronides, anthocyanosides and triterpenes. The ethanol extract inhibited 5 out of 8 (62.5%) of the standard organisms and 6 out of 8 (75%) clinical isolates. The petroleum ether fraction inhibited 4 out of 8 (50%) of the standard microbes and 1 out of 8 (12.5%) clinical isolates. It was also observed that the chloroform fraction inhibited the growth of all the organisms (100%). Average inhibition zones of 14.0?±?1.0?mm to 24.67?±?0.58?mm was seen in the ethyl acetate fraction which halted the growth of 3 (37.5%) of the standard organisms. Inhibition of 7 (87.5%) of standard strains and 6 (75%) of clinical isolates were observed in the water fraction. The chloroform fraction exhibited bactericidal activity against all the test organisms while the remaining fractions showed varying degrees of bacteriostatic activity. Conclusion The study confirmed that fractions of Cryptolepis sanguinolenta have antimicrobial activity. The chloroform fraction had the highest activity, followed by water, ethanol, petroleum ether and ethyl acetate respectively. Only the chloroform fraction exhibited bactericidal activity and further investigations are needed to ascertain its safety and prospects of drug development. PMID:22709723

2012-01-01

69

In Vitro Activities of Iodonium Salts against Oral and Dental Anaerobes  

PubMed Central

The comparative in vitro activities of 11 iodonium salt compounds, 0.12% chlorhexidine, and four antimicrobial agents against 322 anaerobic and fastidious potential dental and periodontal bacterial pathogens were studied. Iodonium salts 3, 4, 5, 9, and 10 had in vitro activities comparable to that of chlorhexidine against most isolates. These compounds may be suitable for incorporation into an oral mouthwash. PMID:15215147

Goldstein, Ellie J. C.; Citron, Diane M; Warren, Yumi; Merriam, C. Vreni; Tyrrell, Kerin; Fernandez, Helen; Radhakrishnan, Ukkiramapandian; Stang, Peter J.; Conrads, Georg

2004-01-01

70

In vitro activities of isavuconazole against opportunistic filamentous and dimorphic fungi.  

PubMed

The in vitro activity of isavuconazole was compared to those of amphotericin B, fluconazole, itraconazole, voriconazole, posaconazole, and ravuconazole against 300 clinical isolates of Pseudallescheria boydii, Paecilomyces lilacinus, Fusarium spp., Bipolaris spicifera, Curvularia lunata, Alternaria alternata, Exophiala spp., Rhizopus arrhizus, Mucor circillenoides, Absidia corymbifera, Blastomyces dermatitidis, Histoplasma capsulatum and Coccidioides posadasii. MICs were determined by a broth macrodilution method based on the CLSI M38-A procedure. The triazoles were relatively uniform in that they showed strong in vitro inhibitory activity against most of the tested fungi. In vitro activity was variable with strains of P. lilacinus while with Fusarium spp., the triazoles were found to have limited in vitro activity and amphotericin B was moderately active. The results suggest that isavuconazole is a broad-spectrum antifungal agent, effective against a wide range of moulds in vitro. PMID:19101837

González, Gloria M

2009-02-01

71

In vitro antimicrobial activity of Medilox® super-oxidized water  

PubMed Central

Aim Super-oxidized water is one of the broad spectrum disinfectants, which was introduced recently. There are many researches to find reliable chemicals which are effective, inexpensive, easy to obtain and use, and effective for disinfection of microorganisms leading hospital infections. Antimicrobial activity of super-oxidized water is promising. The aim of this study was to investigate the in-vitro antimicrobial activity of different concentrations of Medilox® super-oxidized water that is approved by the Food and Drug Administration (FDA) as high level disinfectant. Material and methods In this study, super-oxidized water obtained from Medilox® [Soosan E & C, Korea] device, which had been already installed in our hospital, was used. Antimicrobial activities of different concentrations of super-oxidized water (1/1, 1/2, 1/5, 1/10, 1/20, 1/50, 1/100) at different exposure times (1, 2, 5, 10, 30 min) against six ATCC strains, eight antibiotic resistant bacteria, yeasts and molds were evaluated using qualitative suspension test. Dey-Engley Neutralizing Broth [Sigma-Aldrich, USA] was used as neutralizing agent. Results Medilox® was found to be effective against all standard strains (Acinetobacter baumannii 19606, Escherichia coli 25922, Enterococcus faecalis 29212, Klebsiella pneumoniae 254988, Pseudomonas aeruginosa 27853, Staphylococcus aureus 29213), all clinical isolates (Acinetobacter baumannii, Escherichia coli, vancomycin-resistant Enterococcus faecium, Klebsiella pneumoniae, Pseudomonas aeruginosa, methicillin-resistant Staphylococcus aureus, Bacillus subtilis, Myroides spp.), and all yeastsat 1/1 dilution in ??1 minute. It was found to be effective on Aspergillus flavus at 1/1 dilution in ??2 minutes and on certain molds in ??5 minutes. Conclusion Medilox® super-oxidized water is a broad spectrum, on-site producible disinfectant, which is effective on bacteria and fungi and can be used for the control of nosocomial infection. PMID:25023905

2014-01-01

72

In vitro activity of olive oil polyphenols against Helicobacter pylori.  

PubMed

Helicobacter pylori is linked to a majority of peptic ulcers and to some types of gastric cancer, and resistance of the microorganism to antibiotic treatment is now found worldwide. Virgin olive oil is an unrefined vegetable oil that contains a significant amount of phenolic compounds. Under simulated conditions, we have demonstrated that these substances can diffuse from the oil into the gastric juice and be stable for hours in this acidic environment. In vitro, they exerted a strong bactericidal activity against eight strains of H. pylori, three of them resistant to some antibiotics. Among the phenolic compounds, the dialdehydic form of decarboxymethyl ligstroside aglycon showed the strongest bactericidal effect at a concentration as low as 1.3 microg/mL. Although the experimental conditions are different from other reported works, this bactericidal concentration is much lower than those found for phenolic compounds from tea, wine, and plant extracts. These results open the possibility of considering virgin olive oil a chemopreventive agent for peptic ulcer or gastric cancer, but this bioactivity should be confirmed in vivo in the future. PMID:17263460

Romero, Concepción; Medina, Eduardo; Vargas, Julio; Brenes, Manuel; De Castro, Antonio

2007-02-01

73

In vitro anti-leukaemia activity of sphingosine kinase inhibitor.  

PubMed

Compelling evidence indicates the role of sphingosine kinase 1 (SPHK1) deregulation in the processes of carcinogenesis and acquisition of drug resistance, providing the rationale for an effective anti-cancer therapy. However, no highly selective inhibitors of SPHK1 are available for in vitro and in vivo studies, except for the newly discovered 'SK inhibitor' (SKI). The present study showed that, in a panel of myeloid leukaemia cell lines, basal level of SPHK1 correlated with the degree of kinase inhibition by SKI. Exposure to SKI caused variable anti-proliferative, cytotoxic effects in all cell lines. In particular, SKI induced an early, significant inhibition of SPHK1 activity, impaired cell cycle progression and triggered apoptosis in K562 cells. Moreover, SKI acted synergistically with imatinib mesylate (IM) to inhibit cell growth and survival. Finally, the inhibitor affected the clonogenic potential and viability of primary cells from chronic myeloid leukaemia (CML) patients, including one harbouring the IM-insensitive Abl kinase domain mutation T315I. Due to the fact that the phenomenon of resistance to IM remains a major issue in the treatment of patients with CML, the identification of alternative targets and new drugs may be of clinical relevance. PMID:19036099

Ricci, Clara; Onida, Francesco; Servida, Federica; Radaelli, Franca; Saporiti, Giorgia; Todoerti, Katia; Deliliers, Giorgio Lambertenghi; Ghidoni, Riccardo

2009-02-01

74

Acaricide activity in vitro of Acmella oleracea against Rhipicephalus microplus.  

PubMed

Cattle tick control has been limited by the resistance of these parasites to synthetic acaricides. Natural products are a possible alternative as they have different mechanisms of action. Acmella oleracea is a native plant with a large cultivated area in the Amazon region and could be easily used for large-scale preparation of a commercial product. This study evaluated the in vitro action of the hexane extract of the aerial parts of A. oleracea on larvae and engorged females of the cattle tick Rhipicephalus microplus. Spilanthol was the major constituent with a content of 14.8% in the extract. The hexane extract of A. oleracea was highly effective against larvae of R. microplus with an LC50 of 0.8 mg mL(-1). Against engorged females, hexane extract of A. oleracea reduced oviposition and hatchability of eggs with an LC50 of 79.7 mg mL(-1). Larvae and engorged females were killed by the hexane extract with high efficiency (>95%) at concentrations of 3.1 and 150.0 mg mL(-1), respectively. These results demonstrate that the hexane extract of A. oleracea has significant activity against R. microplus and has potential to be developed into formulations for tick control. PMID:25033813

Castro, K N C; Lima, D F; Vasconcelos, L C; Leite, J R S A; Santos, R C; Paz Neto, A A; Costa-Júnior, L M

2014-10-01

75

In Vitro Antibacterial Activity of NB-003 against Propionibacterium acnes?  

PubMed Central

NB-003 and NB-003 gel formulations are oil-in-water nanoemulsions designed for use in bacterial infections. In vitro susceptibility of Propionibacterium acnes to NB-003 formulations and comparator drugs was evaluated. Both NB-003 formulations were bactericidal against all P. acnes isolates, including those that were erythromycin, clindamycin, and/or tetracycline resistant. In the absence of sebum, the MIC90s/minimum bactericidal concentrations (MBC90s) for NB-003, NB-003 gel, salicylic acid (SA), and benzoyl peroxide (BPO) were 0.5/2.0, 1.0/2.0, 1,000/2,000, and 50/200 ?g/ml, respectively. In the presence of 50% sebum, the MIC90s/MBC90s of NB003 and BPOs increased to 128/1,024 and 400/1,600 ?g/ml, respectively. The MIC90s/MBC90s of SA were not significantly impacted by the presence of sebum. A reduction in the MBC90s for NB-003 and BPO was observed when 2% SA or 0.5% BPO was integrated into the formulation, resulting in MIC90s/MBC90s of 128/256 ?g/ml for NB003 and 214/428 ?g/ml for BPO. The addition of EDTA enhanced the in vitro efficacy of 0.5% NB-003 in the presence or absence of 25% sebum. The addition of 5 mM EDTA to each well of the microtiter plate resulted in a >16- and >256-fold decrease in MIC90 and MBC90, yielding a more potent MIC90/MBC90 of ?1/<1 ?g/ml. The kinetics of bactericidal activity of NB-003 against P. acnes were compared to those of a commercially available product of BPO. Electron micrographs of P. acnes treated with NB-003 showed complete disruption of bacteria. Assessment of spontaneous resistance of P. acnes revealed no stably resistant mutant strains. PMID:21746943

Pannu, J.; McCarthy, A.; Martin, A.; Hamouda, T.; Ciotti, S.; Ma, L.; Sutcliffe, J.; Baker, J. R.

2011-01-01

76

In vitro antiplasmodial activity of Tithonia diversifolia and identification of its main active constituent: tagitinin C.  

PubMed

The antimalarial properties of Tithonia diversifolia, an Asteraceae traditionally used to treat malaria, were investigated in vitro against three strains of Plasmodium falciparum. The ether extract from aerial parts of the plant collected in Săo Tomé e Príncipe, demonstrated good antiplasmodial activity (IC 50 on FCA strain: 0.75 microg/ml). A bioassay guided fractionation of this extract led to the isolation of the known sesquiterpene lactone tagitinin C as an active component against Plasmodium (IC 50 on FCA strain: 0.33 microg/ml), but also possessing cytotoxic properties (IC 50 on HTC-116 cells: 0.706 microg/ml). PMID:12094301

Goffin, Eric; Ziemons, Eric; De Mol, Patrick; de Madureira, Maria do Céu; Martins, Ana Paula; da Cunha, Antonio Proença; Philippe, Genevičve; Tits, Monique; Angenot, Luc; Frederich, Michel

2002-06-01

77

Processed tart cherry products--comparative phytochemical content, in vitro antioxidant capacity and in vitro anti-inflammatory activity.  

PubMed

Processing of fruits and vegetables affects their phytochemical and nutrient content. Tart cherries are commercially promoted to possess antioxidant and anti-inflammatory activity. However, processing affects their phytochemical content and may affect their related health benefits. The current study compares the in vitro antioxidant capacity and anti-inflammatory cyclooxygenase activity of processed tart cherry (Prunus cerasus) products-cherry juice concentrate, individually quick-frozen cherries, canned cherries, and dried cherries. Cherry products were analyzed for total anthocyanin and proanthocyanidin content and profile. On a per serving basis, total anthocyanins were highest in frozen cherries and total proanthocyanidins were highest in juice concentrate. Total phenolics were highest in juice concentrate. Juice concentrate had the highest oxygen radical absorbance capacity (ORAC) and peroxynitrite radical averting capacity (NORAC). Dried cherries had the highest hydroxyl radical averting capacity (HORAC) and superoxide radical averting capacity (SORAC). Processed tart cherry products compared very favorably to the U.S. Dept. of Agriculture-reported ORAC of other fresh and processed fruits. Inhibition of in vitro inflammatory COX-1 activity was greatest in juice concentrate. In summary, all processed tart cherry products possessed antioxidant and anti-inflammatory activity, but processing differentially affected phytochemical content and in vitro bioactivity. On a per serving basis, juice concentrate was superior to other tart cherry products. PMID:23163942

Ou, Boxin; Bosak, Kristen N; Brickner, Paula R; Iezzoni, Dominic G; Seymour, E Mitchell

2012-05-01

78

In vitro antioxidant activity of acetylated and benzoylated derivatives of polysaccharide extracted from Ulva pertusa (Chlorophyta)  

Microsoft Academic Search

The antioxidant activity of natural ulvan and its derivatives (acetylated and benzoylated ulvans) in vitro was determined, including scavenging activity against superoxide and hydroxyl radicals, reducing power, and chelating ability. Obvious differences in antioxidant activity between natural ulvan and its derivatives were observed, moreover, the antioxidant activity of acetylated and benzoylated ulvans was stronger than that of natural ulvan.

Huimin Qi; Quanbin Zhang; Tingting Zhao; Rugui Hu; Kun Zhang; Zhien Li

2006-01-01

79

Activated ?? T cells inhibit osteoclast differentiation and resorptive activity in vitro  

PubMed Central

Extensive evidence suggests that the immune system exerts powerful effects on bone cells, particularly in chronic disease pathologies such as rheumatoid arthritis (RA). The chronic inflammatory state in RA, particularly the excessive production of T cell-derived proinflammatory cytokines such as tumour necrosis factor (TNF)-? and interleukin (IL)-17, triggers bone erosions through the increased stimulation of osteoclast formation and activity. While evidence supports a role for IL-17 and TNF-? secreted by conventional CD4+ T cells in RA, recent evidence in animal models of RA have implicated ?? T cells as a major producer of pathogenic IL-17. However, the capacity of ?? T cells to influence osteoclast formation and activity in humans has not yet been investigated widely. To address this issue we investigated the effects of ?? T cells on osteoclast differentiation and resorptive activity. We have demonstrated that anti-CD3/CD28-stimulated ?? T cells or CD4+ T cells inhibit human osteoclast formation and resorptive activity in vitro. Furthermore, we assessed cytokine production by CD3/CD28-stimulated ?? T cells and observed a lack of IL-17 production, with activated ?? T cells producing abundant interferon (IFN)-?. The neutralization of IFN-? markedly restored the formation of osteoclasts from precursor cells and the resorptive activity of mature osteoclasts, suggesting that IFN-? is the major factor responsible for the inhibitory role of activated ?? T cells on osteoclastogenesis and resorptive activity of mature osteoclasts. Our work therefore provides new insights on the interactions between ?? T cells and osteoclasts in humans. PMID:23815433

Pappalardo, A; Thompson, K

2013-01-01

80

[In vitro activity of sitafloxacin against clinical isolates in 2009].  

PubMed

In vitro activity of sitafloxacin (STFX) and various oral antimicrobial agents against bacterial isolates recovered from clinical specimens between January and December 2009, at different healthcare facilities in Japan was evaluated. A total of 1,620 isolates including aerobic and anaerobic organisms was available for the susceptibility testing using the microbroth dilution methods recommended by Clinical Laboratory Standard Institute. The minimum inhibitory concentration of STFX at which 90% of isolates (MIC90) was 0.06 microg/mL for methicillin-susceptible Staphylococcus aureus and was equal to that of garenoxacin (GRNX), 2 times lower than that of moxifloxacin (MFLX), and 8 times lower than that of levofloxacin (LVFX). STFX inhibited the growth of all the isolates of Streptococcus pneumoniae at 0.06 microg/mL or less. The MIC90s of STFX ranged from 0.03 to 0.06 microg/mL and were 1 to 2 times lower than those of GRNX, 2 to 4 times lower than those of MFLX, and 16 to 32 times lower than those of LVFX. Against Streptococcus pyogenes, the MIC90 of STFX was 0.06 microg/mL and was 2 times lower than that of GRNX, 4 times lower than that of MFLX, and 32 times lower than that of LVFX. The MIC90 of STFX was 0.25 microg/mL for Enterococcus faecalis, and was 2 times lower than those of GRNX and MFLX, and 8 times lower than that of LVFX. The MIC90 of STFX for E. coli was 2 microg/mL, and the MIC90s of other 10 species of Enterobacteriaceae which were the lowest values of the quinolones tested ranged from 0.03 to 1 microg/mL. The MIC90 of STFX for Pseudomonas aeruginosa isolates recovered from urinary infections was 8 microg/mL and was 16 times lower than those of GRNX, MFLX and LVFX. The MIC90 of STFX for P aeruginosa isolates recovered from respiratory infections was 2 microg/mL and was 32 times lower than those of GRNX and MFLX, and 16 times lower than that of LVFX. STFX inhibited the growth of all the isolates of Haemophilus influenzae at 0.004 microg/mL or less, and was 2 to 4 times lower than those of GRNX, 8 times lower than those of MFLX, and 4 times lower than those of LVFX. The MIC90 of STFX was 0.008 microg/mL for Moraxella catarrhalis, and was 2 times lower than that of GRNX, 8 times lower than those of MFLX and LVFX. The MIC90s of STFX ranged from 0.015 to 0.12 microg/mL for all the species of anaerobic bacteria and were the lowest values of all the antimicrobial agents tested. In conclusion, the activity of STFX against Gram-positive cocci was comparable or superior to those of GRNX, MFLX and LVFX. STFX showed the most potent activity against Gram-negative bacteria and anaerobic bacteria of all the antimicrobial agents tested in this study. PMID:21425595

Amano, Ayako; Matsuzaki, Kaoru; Kishi, Naoko; Saika, Takeshi; Hasegawa, Miyuki; Ikeda, Fumiaki; Matsumoto, Takuyuki; Yamaguchi, Hiroki; Kanda, Yuko; Shiozawa, Tomoo

2010-12-01

81

[In vitro activity of sitafloxacin against clinical isolates in 2012].  

PubMed

In vitro activity of sitafloxacin (STFX) and various oral antimicrobial agents against bacterial isolates recovered from clinical specimens between January and December 2012, at different healthcare facilities in Japan was evaluated. A total of 1,620 isolates including aerobic and anaerobic organisms were available for the susceptibility testing using the microbroth dilution methods recommended by Clinical and Laboratory Standards Institute. The minimum inhibitory concentration of STFX at which 90% of isolates (MIC90) was 0.5 microg/mL for methicillin-susceptible Staphylococcus aureus and was 2 times lower than that of garenoxacin (GRNX), 4 times lower than that of moxifloxacin (MFLX), and 16 times lower than that of levofloxacin (LVFX). STFX inhibited the growth of all the isolates of Streptococcus pneumoniae at 0.06 microg/mL or less. The MIC90 of STFX was 0.03 microg/mL and was 2 times lower than that of GRNX, 4 times lower than that of MFLX, and 32 times lower than that of LVFX. Against Streptococcus pyogenes, the MIC90 of STFX was 0.06 microg/mL and was 2 times lower than that of GRNX, 8 times lower than that of MFLX, and 32 times lower than that of LVFX. The MIC90 of STFX was 2 microg/mL for Enterococcus faecalis, and was 4 times lower than that of GRNX, 8 times lower than that of MFLX, and 32 times lower than that of LVFX. The MIC90 of STFX for Escherichia coli was 2 microg/mL, and the MIC90(s) of other 10 species of Enterobacteriaceae which were the lowest values of the quinolones tested ranged from 0.03 to 1 microg/mL. The MIC90 of STFX for Pseudomonas aeruginosa isolates recovered from urinary infections was 4 microg/mL and was 32 times lower than those of GRNX, MFLX and LVFX. The MIC90 of STFX for P. aeruginosa isolates recovered from respiratory infections was 4 microg/mL and was 8 to 16 times lower than those of GRNX, MFLX, and LVFX. STFX inhibited the growth of all the isolates of Haemophilus influenzae at 0.004 microg/mL or less, and was 4 times lower than that of GRNX, 16 times lower than that of MFLX, and 8 times lower than that of LVFX. The MIC90 of STFX was 0.015 microg/mL for Moraxella catarrhalis, and was equal to that of GRNX, 4 times lower than those of MFLX and LVFX. The MIC90(s) of STFX ranged from 0.03 to 0.25 microg/mL for all the species of anaerobic bacteria and were the lowest values of all the antimicrobial agents tested. In conclusion, the activity of STFX against Gram-positive cocci was comparable or superior to those of GRNX, MFLX and LVFX. STFX showed the most potent activity against Gram-negative bacteria and anaerobic bacteria of all the antimicrobial agents tested in this study. PMID:24649797

Amano, Ayako; Matsuzaki, Kaoru; Kishi, Naoko; Koyama, Hideaki; Hasegawa, Miyuki; Ikeda, Fumiaki; Matsumoto, Takuyuki; Yamaguchi, Hiroki; Okutani, Yukihiro

2013-12-01

82

In vitro and in vivo antitrypanosomal activity of Xanthium strumarium leaves  

Microsoft Academic Search

Antitrypanosomal activity of crude 50% ethanolic extract of Xanthium strumarium leaves was studied in vitro and in vivo. The extract exhibited trypanocidal activity at all the four concentrations tested i.e. 5, 50, 500 and 1000 ?g\\/ml, in vitro. In vivo trial revealed that the extract exerted antitrypanosomal effect at dosage of 100, 300 and 1000 mg\\/kg, intraperitoneally. At 100 and

T. S. Talakal; S. K. Dwivedi; S. R. Sharma

1995-01-01

83

In vitro antioxidant activity of polysaccharide from Gardenia jasminoides ellis  

USGS Publications Warehouse

A water-soluble polysaccharide, GP, was isolated from Gardenia jasminoides Ellis through hot water extraction followed by ethanol precipitation. The in vitro free radicals scavenging tests exhibited that GP has significant scavenging abilities especially for ABTS, DPPH, and hydroxyl radicals, which suggests that the polysaccharide GP is a novel antioxidant. ?? 2011 Academic Journals.

Fan, Y.; Ge, Z.; Luo, A.

2011-01-01

84

In vitro and in vivo antibacterial activities of Q-35, a novel fluoroquinolone.  

PubMed

Q-35, a new fluoroquinolone, was evaluated for its in vitro and in vivo antibacterial activities. In vitro antibacterial activity against gram-positive bacteria was almost equal to that of sparfloxacin or tosufloxacin, but its activity against gram-negative bacteria was 2 times or more lower than that of other quinolones tested. In experimental septicemia, the in vivo activity of Q-35 reflected its in vitro antibacterial activity. In respiratory tract infections with Streptococcus pneumoniae TMS-3 in mice, Q-35 showed a therapeutic effect similar to sparfloxacin and tosufloxacin. Q-35 showed almost the same activity as that of ofloxacin in mice with pyelonephritic infection due to Escherichia coli TMS-3. The peak levels of Q-35 in murine serum, lungs and kidneys after a single oral administration were intermediate compared to those of tested quinolones. PMID:7758353

Iwasaki, H; Miyazaki, S; Tsuji, A; Yamaguchi, K; Goto, S

1995-01-01

85

In Vitro Fungicidal Activities of Voriconazole, Itraconazole, and Amphotericin B against Opportunistic Moniliaceous and Dematiaceous Fungi  

Microsoft Academic Search

The NCCLS proposed standard M38-P describes standard parameters for testing the fungistatic antifungal activities (MICs) of established agents against filamentous fungi (molds); however, standard conditions are not available for testing their fungicidal activities (minimum fungicidal or lethal concentrations (MFCs)). This study evaluated the in vitro fungistatic and fungicidal activities of voriconazole, itraconazole, and amphotericin B against 260 common and emerging

ANA ESPINEL-INGROFF

2001-01-01

86

In vitro and in vivo antimalarial activities of T-2307, a novel arylamidine.  

PubMed

T-2307, a novel arylamidine, has been shown to exhibit broad-spectrum antifungal activities against clinically significant pathogens. Here, we evaluated the in vitro and in vivo antimalarial activity of T-2307. The 50% inhibitory concentrations (IC??s) of T-2307 against Plasmodium falciparum FCR-3 and K-1 strains were 0.47 and 0.17 ?M, respectively. T-2307 at 2.5 to 10 mg/kg of body weight/day exhibited activity against blood stage and liver stage parasites in rodent malaria models. In conclusion, T-2307 exhibited in vitro and in vivo antimalarial activity. PMID:22252809

Kimura, Akiko; Nishikawa, Hiroshi; Nomura, Nobuhiko; Mitsuyama, Junichi; Fukumoto, Shinya; Inoue, Noboru; Kawazu, Shin-Ichiro

2012-04-01

87

Studies on the activities of rumen microorganisms in vitro  

E-print Network

EXTRACTS AND SUCROSE SOLUTIONS TO INHIBIT CELLULOSE DIGESTION BI RUMEN MICROORGANISMS IN VITRO PART III l. SLVFRAL TYPES OF FISTULA PLUGS USED fN RUMEN STUDIES . ~ ~ 47 2. A NEW TYPE OF BJEUFATIC FISTULA PLUG 49 DETAILS OF CONSTRUCTION OF THE PNEUMATIC... FISTULA PLUG . . 50 PART I EFFECTS OF MESQUITE BEAN EXTRACTS ON THE DIGESTION OF CELLULOSE BY RUMEN MICROORGANISMS INTRODUCTION Mesquite beans have been used as feed for oattle sinoe the extensive invasion by the mesquite tree (PORN~, )~i...

Johnson, Carl Edward

1957-01-01

88

In Vitro Antioxidant Activities of Sulfated Derivatives of Polysaccharides Extracted from Auricularia auricular  

PubMed Central

In this research, two types of sulfated polysaccharide derivatives were successfully synthesized. Their antioxidant activities were investigated by employing various established in vitro systems. In addition, the degree of sulfation was evaluated using ion-chromatography and IR spectra. The results verify that, when employing scavenging superoxide radical tests, both the sulfation of acid Auricularia auricular polysaccharides (SAAAP) and the sulfation of neutral Auricularia auricular polysaccharides (SNAAP) derivatives possessed considerable antioxidant activity and had a more powerful antioxidant competence than that of the native non-sulfated polysaccharides (AAAP and NAAP). On the other hand, AAAP and NAAP exhibited stronger activity on scavenging both the hydroxyl radical and lipid peroxidation. Available data obtained with in vitro measurements indicates that the sulfated groups of AAAP and NAAP played an important role on antioxidant activity. In sum, the research demonstrates that the antioxidant activity of sulfated polysaccharide derivatives in vitro has a potential significance for seeking new natural antioxidant protective agents. PMID:21686185

Zhang, Hua; Wang, Zhen-Yu; Yang, Lin; Yang, Xin; Wang, Xue; Zhang, Zhi

2011-01-01

89

Chemical composition and biological activities of essential oil from Salvia sclarea plants regenerated in vitro.  

PubMed

The essential oils obtained by hydrodistillation of dried aerial parts of Salvia sclarea L. plants, regenerated in vitro and reproduced from seeds, were analyzed by GC and GC-MS. The oils from in vitro and in vivo plants were compared in respect to their chemical composition as well as antimicrobial and cytotoxic activities. The chemical profiles of both oils were very similar, although the yield of essential oil from in vitro plants was lower (0.1%, v/w) than the oil yield isolated from in vivo S. sclarea plants (0.2%, v/w). Both oils showed antimicrobial and cytotoxic activity. The oil from in vitro regenerated plants of S. sclarea exhibited stronger cytotoxic action against NALM-6 cell lines in comparison with the essential oil from in vivo plants. PMID:19384275

Ku?ma, Lukasz; Kalemba, Danuta; Rózalski, Marek; Rózalska, Barbara; Wieckowska-Szakiel, Marzena; Krajewska, Urszula; Wysoki?ska, Halina

2009-01-01

90

The potential of a niacinamide dominated cosmeceutical formulation on fibroblast activity and wound healing in vitro.  

PubMed

Knowledge on the intrinsic mechanisms involved in wound healing provides opportunity for various therapeutic strategies. The manipulation of dermal fibroblast proliferation and differentiation might prove to beneficially augment wound healing. This study evaluated the combined effects of niacinamide, L-carnosine, hesperidin and Biofactor HSP(®) on fibroblast activity. The effects on fibroblast collagen production, cellular proliferation, migration and terminal differentiation were assessed. In addition, the authors determined the effects on in vitro wound healing. The optimal concentrations of actives were determined in vitro. Testing parameters included microscopic morphological cell analysis, cell viability and proliferation determination, calorimetric collagen detection and in vitro wound healing dynamics. Results show that 0·31 mg/ml niacinamide, 0·10 mg/ml L-carnosine, 0·05 mg/ml hesperidin and 5·18 µg/ml Biofactor HSP® proved optimal in vitro. The results show that fibroblast collagen synthesis was increased alongside with cellular migration and proliferation. PMID:22892041

Wessels, Quenton; Pretorius, Etheresia; Smith, Celeste M; Nel, Hugo

2014-04-01

91

Antioxidant, Antibacterial and Antischistosomal Activities of Extracts from Grateloupia livida (Harv). Yamada  

PubMed Central

The present study was designated to evaluate the antioxidant, antibacterial and antischistosomal activities of Grateloupia livida (GL) extracts in vitro. A GL Ethanol extract (EE) was separated into petroleum ether (PE), ethyl acetate (EA), n-butyl alcohol (BuOH) and aqueous (AQ) fractions to fractionate the polar and non-polar compounds in the EE. Extracts antioxidant activities were evaluated in vitro by DPPH radical-scavenging, deoxyribose radical scavenging, and ?-carotene bleaching assays, all using butylated hydroxytoluene (BHT) as the reference antioxidant compound. The most effective antioxidant properties were observed in the PE fraction in all three assays. Antimicrobial testing showed that the PE fraction exhibited broad-spectrum antimicrobial activity, with the PE fraction also exhibiting strong activity against the human pathogenic trematode S. japonicum adult worm. In order to investigate the relationships between bioactivity and chemical composition, the chemical composition of the PE fraction was analyzed by gas chromatography-mass spectrometry (GC-MS). In total, 25 components were identified in the PE fraction, most of which have known antioxidant and antimicrobial activities. However, none of the compounds have reported activity against Schistosoma, suggesting that the schistosomicidal activity of the PE fraction may be related to minor constituents present in the extract, or governed by more intricate synergistic or additive relationships. Finally, fractions with the greatest biological activity displayed neither cellular cytotoxicity, at concentrations up to 100 ug/ml, or acute oral toxicity in mice, at doses up to 2000 mg/kg. Based on antioxidant, antimicrobial, antischistosomal activities, and low toxicity, the PE fraction possesses properties useful for food preservation and overall improvement of human health. PMID:24312216

Yao, Fen; Chen, Weizhou; Zhong, Shuping; Zheng, Fuchun; Shi, Ganggang

2013-01-01

92

Components of normal serum block the focal segmental glomerulosclerosis factor activity in vitro  

Microsoft Academic Search

Components of normal serum block the focal segmental glomerulosclerosis factor activity in vitro.BackgroundSera from some patients with focal segmental glomerulosclerosis (FSGS) increase glomerular albumin permeability (Palb) in vitro. The hypothesis that a component of normal serum can protect the glomerular permeability barrier was tested using sera from FSGS patients, normal individuals, and several mammalian and avian species.MethodsIn most experiments, isolated

Ram Sharma; Mukut Sharma; Ellen T. Mccarthy; Xiu-Li Ge; Virginia J. Savin

2000-01-01

93

Luliconazole Demonstrates Potent In Vitro Activity against Dermatophytes Recovered from Patients with Onychomycosis  

PubMed Central

The in vitro activities of luliconazole, amorolfine, ciclopirox, and terbinafine were determined against 320 dermatophyte isolates from large toenails of onychomycosis patients enrolled into an ongoing phase 2b/3 clinical study. The geometric mean MIC for luliconazole was 0.00022 ?g/ml against all isolates, compared to 0.0194 to 0.3107 ?g/ml for the three other agents. The in vitro potency of luliconazole was maintained regardless of the dermatophyte species. PMID:24709260

Wiederhold, Nathan P.; Fothergill, Annette W.; McCarthy, Dora I.

2014-01-01

94

Determination of In Vitro Antidiabetic Effects, Antioxidant Activities and Phenol Contents of Some Herbal Teas  

Microsoft Academic Search

In this research, some herbal teas and infusions traditionally used in the treatment of diabetes in Turkey, have been studied\\u000a for their antidiabetic effects on in vitro glucose diffusion and phenolic contents and antioxidant activities. Ten aqueous herbal tea extracts were examined using an\\u000a in vitro method to determine their effects on glucose movement across the gastrointestinal tract. Total phenol

Aynur Büyükbalci; Sedef Nehir El

2008-01-01

95

Appraisal of in vitro and in vivo antioxidant activity potential of cornelian cherry leaves.  

PubMed

The antioxidant activity of the 80% methanolic extract of Cornus mas L. leaves (CMM) was evaluated by various methods both in vitro and in vivo. In vitro screening tests indicated that CMM had high antioxidant activity in terms of free radical scavenging and metal reducing activity. In vivo antioxidant activity studies in normal healthy rats demonstrated that the total antioxidant capacity of liver homogenates were increased, although no changes were observed in the activities of antioxidant enzymes superoxide dismutase, catalase and glutathione peroxidase or in the level of lipid peroxidation. Studies on CCl4-treated rats also showed that CMM restored the activities of antioxidant enzymes, lowered the level of lipid peroxidation and elevated the total antioxidant capacities of both the total blood and liver homogenates of the animals. Further activity-guided fractionation studies led to the isolation of gallic acid, a well-known antioxidant, as one of the active components. PMID:24035707

Celep, Engin; Ayd?n, Ahmet; K?rm?z?bekmez, Hasan; Yesilada, Erdem

2013-12-01

96

In vitro antioxidant activity potential of lantadene A, a pentacyclic triterpenoid of Lantana plants.  

PubMed

Lantadenes are pentacyclic triterpenoids present in the leaves of the plant Lantana camara. In the present study, in vitro antioxidant activity and free radical scavenging capacity of lantadene A was evaluated using established in vitro models such as ferric reducing antioxidant power (FRAP), 2,2-diphenyl-1-picryl-hydrazyl (DPPH•), hydroxyl radical (OH•), nitric oxide radical (NO•), superoxide anion scavenging activities and ferrous ion chelating assay. Interestingly, lantadene A showed considerable in vitro antioxidant, free radical scavenging capacity activities in a dose dependant manner when compared with the standard antioxidant in nitric oxide scavenging, superoxide anion radical scavenging and ferrous ion chelating assay. These findings show that the lantadene A possesses antioxidant activity with different mechanism of actions towards the different free radicals tested. Since lantadene A is a very popular drug in modern medicine, it is a promising candidate for use as an antioxidant and hepatoprotective agent. PMID:22992785

Grace-Lynn, Chong; Darah, Ibrahim; Chen, Yeng; Latha, Lachimanan Yoga; Jothy, Subramanion L; Sasidharan, Sreenivasan

2012-01-01

97

In Vitro Activity of SCH-56592 and Comparison with Activities of Amphotericin B and Itraconazole against Aspergillus spp  

Microsoft Academic Search

In this study, we investigated the in vitro activity of SCH-56592 (SCH), a new triazole antifungal agent. We compared the activity of SCH with those of itraconazole (ITZ) and amphotericin B (AB) against 60 clinical isolates of Aspergillus spp. by using a microtiter format. Incubation was done at 37°C for 48 h, and MIC endpoints (no growth) were read visually.

KAREN L. OAKLEY; CAROLINE B. MOORE; DAVID W. DENNING

1997-01-01

98

In vitro antioxidant activity study of novel chromone derivatives.  

PubMed

Forty-eight chromone derivatives were evaluated for their antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl free radical scavenging assay, ferrous ions (Fe(2+) ) chelating activity test, total antioxidant activity test (Ferric thiocyanate and Thiobarbituric acid methods), and total reductive capability (potassium ferricyanide reduction). 7,8-Dihydroxy-2-(3'-trifluoromethylphenyl)-3-(3?-trifluoromethylbenzoyl) chromone 32 showed stronger radical scavenging and metal chelating activities than butylated hydroxytoluene, vitamin E, and trolox. Chromone derivatives that exhibited good radical scavenging and metal chelating also displayed strong total antioxidant and reductive power activities. The results obtained from this study indicated that the synthesized chromone derivatives have remarkable antioxidant activity. PMID:22381130

Phosrithong, Narumol; Samee, Weerasak; Nunthanavanit, Patcharawee; Ungwitayatorn, Jiraporn

2012-06-01

99

Evaluation of African medicinal plants for their in vitro trypanocidal activity  

Microsoft Academic Search

Petroleum ether, dichloromethane, methanol and water extracts from 24 plants, belonging to 19 families, which are reported in the literature as traditional remedies for sleeping sickness (human African trypanosomiasis) were screened for in vitro activity against Trypanosoma brucei rhodesiense, as well as for cytotoxicity for a human fibroblast cell-line (WI-38). The trypanocidal activity of the natural compounds berberine and harmane,

F. Freiburghaus; R. Kaminsky; M. H. H. Nkunya; R. Brun

1996-01-01

100

Development of an in vitro technique to measure the cellulolytic activity of donkey caecal contents  

E-print Network

Development of an in vitro technique to measure the cellulolytic activity of donkey caecal contents-111) to measure cellulolytic activity in the caecum of donkey. Three caecally-fistulated donkeys were fed samples were collected before the first meal from each donkey, mixed together and given 4 different

Paris-Sud XI, Université de

101

ANTICOAGULANT FUCOIDAN FRACTIONS FROM FUCUS VESICULOSUS INDUCE PLATELET ACTIVATION IN VITRO  

Microsoft Academic Search

Anticoagulant fucoidan fractions of different molecular weight and sulfate content were prepared and investigated for their effects on platelet function in vitro. The fucoidan fractions were incubated with human platelet rich plasma (PRP) at concentrations of 5, 10 and 50 ?g\\/ml. Platelet activation was subsequently studied by a standard aggregation assay and flow cytometric determination of the activation dependent platelet-surface

Jan Dürig; Thomas Bruhn; Karl-Heinz Zurborn; Kai Gutensohn; Hans D Bruhn; László Béress

1997-01-01

102

In vitro antioxidant activity of Holarrhena antidysenterica Wall. methanolic leaf extract  

PubMed Central

Antioxidative potential of methanolic leaf extract of Holarrhena antidysenterica was evaluated using hydroxyl radical, superoxide anion scavenging and reducing power assays. The antioxidant activity of the methanol extract increased in a concentration-dependent manner. The extract showed significant reactive oxygen species (ROS) scavenging activity in all in vitro antioxidant assays and contained high level of total phenolic content PMID:24826020

Ganapathy, P. S. Sujan; Ramachandra, Y. L.; Rai, S. Padmalatha

2011-01-01

103

Growth hormone, but not insulin, activates STAT5 proteins in adipocytes in vitro and in vivoq  

E-print Network

of the insulin receptor. In our studies, we have shown that physiological levels of insulin do not induce STAT 5 proteins are not activated by physi- ological levels of insulin in adipose tissue. Ó 2003 Elsevier ScienceGrowth hormone, but not insulin, activates STAT5 proteins in adipocytes in vitro and in vivoq

Stephens, Jacqueline

104

Activation of microglia by Borna disease virus infection: in vitro study  

Technology Transfer Automated Retrieval System (TEKTRAN)

Neonatal Borna disease virus (BDV) infection of the rat brain is associated with microglial activation and damage to the certain neuronal populations. Since persistent BDV infection of neurons in vitro is noncytolytic and noncytopathic, activated microglia have been suggested to be responsible for n...

105

In vitro activity of chloroquine, the two enantiomers of chloroquine, desethylchloroquine and pyronaridine against Plasmodium falciparum.  

PubMed Central

A 48 h in vitro test was conducted to compare the susceptibility of two strains of Plasmodium falciparum to chloroquine, the two enantiomers of chloroquine, desethylchloroquine and the new antimalarial drug pyronaridine. The five compounds similarly inhibited the chloroquine sensitive strain. However, desethylchloroquine was less active and pyronaridine was much more active than chloroquine and its enantiomers against the chloroquine resistant strain. PMID:3527245

Fu, S; Björkman, A; Wĺhlin, B; Ofori-Adjei, D; Ericsson, O; Sjöqvist, F

1986-01-01

106

In vitro antioxidant activity of Holarrhena antidysenterica Wall. methanolic leaf extract.  

PubMed

Antioxidative potential of methanolic leaf extract of Holarrhena antidysenterica was evaluated using hydroxyl radical, superoxide anion scavenging and reducing power assays. The antioxidant activity of the methanol extract increased in a concentration-dependent manner. The extract showed significant reactive oxygen species (ROS) scavenging activity in all in vitro antioxidant assays and contained high level of total phenolic content. PMID:24826020

Ganapathy, P S Sujan; Ramachandra, Y L; Rai, S Padmalatha

2011-09-01

107

In Vitro Activities of Isavuconazole and Other Antifungal Agents against Candida Bloodstream Isolates  

Microsoft Academic Search

Received 27 September 2006\\/Returned for modification 22 December 2006\\/Accepted 11 February 2007 Isavuconazole is the active component of the new azole antifungal agent BAL8557, which is entering phase III clinical development. This study was conducted to compare the in vitro activities of isavuconazole and five other antifungal agents against 296 Candida isolates that were recovered consecutively from blood cultures between

H. Seifert; U. Aurbach; D. Stefanik; O. Cornely

2007-01-01

108

Development of a novel in vitro onychomycosis model for the evaluation of topical antifungal activity.  

PubMed

A novel in vitro onychomycosis model was developed to easily predict the topical activity potential of novel antifungal drugs. The model encompasses drug activity and diffusion through bovine hoof slices in a single experimental set-up. Results correspond well with the antifungal susceptibility assay and Franz cell diffusion test. PMID:25772040

Sleven, Reindert; Lanckacker, Ellen; Boulet, Gaëlle; Delputte, Peter; Maes, Louis; Cos, Paul

2015-05-01

109

In vitro and in vivo evaluation of a new active heat moisture exchanger  

Microsoft Academic Search

INTRODUCTION: In order to improve the efficiency of heat moisture exchangers (HMEs), new hybrid humidifiers (active HMEs) that add water and heat to HMEs have been developed. In this study we evaluated the efficiency, both in vitro and in vivo, of a new active HME (the Performer; StarMed, Mirandola, Italy) as compared with that of existing HMEs (Hygroster and Hygrobac;

Davide Chiumello; Paolo Pelosi; Gilbert Park; Andrea Candiani; Nicola Bottino; Ezio Storelli; Paolo Severgnini; Dunia D'Onofrio; Luciano Gattinoni; Massimo Chiaranda

2004-01-01

110

IN VITRO AUGMENTATION OF NATURAL KILLER CELL ACTIVITY BY MANGANESE CHLORIDE  

EPA Science Inventory

The in vitro cultivation of murine spleen cells with MnCl2 resulted in the enhancement of natural killer (NK) cell activity as measured in a 4-h (51)Cr-release assay. Optimal enhancement of NK activity was observed at concentrations of 10-20 micrograms MnCl2 culture (72-144 micro...

111

INHIBITION OF HUMAN NATURAL KILLER CELL ACTIVITY FOLLOWING IN VITRO EXPOSURE TO OZONE  

EPA Science Inventory

In this study we have examined the effect of in vitro ozone exposure on human peripheral blood natural killer (NK) cell activity measured against K562 tumor cells. he data showed that NK activity was nhibited in a time dependent manner with marked suppression observed after 6 hou...

112

Stimulating activity of Chinese medicinal herbs on human lymphocytes in vitro  

Microsoft Academic Search

The effects of eight kinds of Chinese medicinal herbs (CMH) on human lymphocytes was studied in vitro. The extract of Cinnamomum cassia presl markedly stimulated human lymphocytes to proliferate. Codonopsis pilosula, Oldenlandia diffusa and Rhizoma typhonii weakly stimulated. These extracts enhanced cytotoxic T-lymphocyte (CTL) activity, but failed to enhance natural killer (NK)-cell activity. The extracts of these CMHs have stimulatory

B. E Shan; Y Yoshida; T Sugiura; U Yamashita

1999-01-01

113

Antioxidant activities of Satureja cilicica essential oil in butter and in vitro  

Microsoft Academic Search

Satureja (Labiatae) species are a well-known aromatic plant which is used to produce essential oil and aromatic water in the mountain regions of the Mediterranean part of Turkey. In our study, it was aimed to determine antioxidant activities of Satureja cilicica essential oil in butter and in vitro. Antioxidant activities of the oils at different concentrations were evaluated using the

Gulcan Ozkan; Bedia Simsek; Hakan Kuleasan

2007-01-01

114

Study of the in vitro antiplasmodial, antileishmanial and antitrypanosomal activities of medicinal plants from Saudi Arabia.  

PubMed

The present study investigated the in vitro antiprotozoal activity of sixteen selected medicinal plants. Plant materials were extracted with methanol and screened in vitro against erythrocytic schizonts of Plasmodium falciparum, intracellular amastigotes of Leishmania infantum and Trypanosoma cruzi and free trypomastigotes of T. brucei. Cytotoxic activity was determined against MRC-5 cells to assess selectivity. The criterion for activity was an IC?? < 10 ?g/mL (<5 ?g/mL for T. brucei) and a selectivity index of ?4. Antiplasmodial activity was found in the extracts of Prosopis juliflora and Punica granatum. Antileishmanial activity against L. infantum was demonstrated in Caralluma sinaica and Periploca aphylla. Amastigotes of T. cruzi were affected by the methanol extract of Albizia lebbeck pericarp, Caralluma sinaica, Periploca aphylla and Prosopius juliflora. Activity against T. brucei was obtained in Prosopis juliflora. Cytotoxicity (MRC-5 IC?? < 10 ?g/mL) and hence non-specific activities were observed for Conocarpus lancifolius. PMID:23011279

Al-Musayeib, Nawal M; Mothana, Ramzi A; Al-Massarani, Shaza; Matheeussen, An; Cos, Paul; Maes, Louis

2012-01-01

115

In vitro activity of Arbutus unedo against Leishmania tropica promastigotes.  

PubMed

Pentavalent antimonials are the first choice for the treatment of anthroponotic cutaneous leishmaniasis (ACL) in health centers in Turkey, however in rural areas, traditional plants may be preferred for the treatment of lesions. In recent years a number of papers are published related to the natural products especially plant derivates. Our aim is to investigate the antileishmanial effect of Arbutus unedo which is a wild plant mainly grown in maquis and rocky places of the seabord in South Europe. In the present study, the ethanolic, water and n-hexane extracts from the leaves of Arbutus unedo were originally tested in vitro against Leishmania tropica promastigotes. The ethanol extract of Arbutus unedo leaves at the concentrations of 100, 250, 500 microg/ml were found to be more effective than the other extracts (p:0.000). Our study showed that the ethanolic extract of Arbutus unedo leaves can be a promising antileishmanial agent and further experiments are needed. PMID:19598085

Kivçak, Bijen; Mert, Tuba; Ertabaklar, Hatice; Balcio?lu, I Cüneyt; Ozensoy Töz, Seray

2009-01-01

116

In vitro activities of tigecycline against clinical isolates from Shanghai, China.  

PubMed

To evaluate the in vitro activity of tigecycline, the minimum inhibitory concentrations (MICs) of tigecycline against 1,201 strains of recent clinical isolates from 10 hospitals in Shanghai, China were determined and compared with selected comparators. Results showed that tigecycline had broad-spectrum antimicrobial activity. It was highly active against Gram-positive cocci, including methicillin-resistant Staphylococcus spp., penicillin-intermediate Streptococcus pneumoniae, Enterococcus faecalis and E. faecium. Tigecycline also had good activity against most strains of Enterobacteriaceae, Haemophilus influenzae, Neisseria gonorrhoeae, and Moraxella catarrhalis. However, it was poorly active against Acinetobacter baumannii and Pseudomonas aeruginosa. Tigecycline was highly active against anaerobic Gram-positive cocci such as Peptococcus spp. The in vitro activity of tigecycline was significantly better than that of minocycline and tetracycline. It was as active as or slightly more active than vancomycin and teicoplanin in the activity against resistant aerobic Gram-positive cocci. Tigecycline was bactericidal against all Gram-positive cocci tested except Enterococcus spp. Inoculum size but not pH of medium or concentration of human serum in broth had significant effect on the in vitro activity of tigecycline. Aged media (48-72 hours after preparation) used in the test and specific resistance problem in China may have some effects on MIC values of tigecycline. PMID:15582300

Zhang, Ying-yuan; Zhou, Le; Zhu, De-mei; Wu, Pei-cheng; Hu, Fu-pin; Wu, Wei-hong; Wang, Fu

2004-12-01

117

Antioxidative Activity of Lichen Thamnolia vermicularis in vitro  

PubMed Central

This study was aimed at evaluating the antioxidant activities of methanol extract of Thamnolia vermicularis. The antioxidant activity, reducing power, superoxide anion radical scavenging and free radical scavenging activities were studied. The antioxidant activity of the extract correlated with its concentration (0.2~2 mg/ml) in the reaction mixtures containing linoleic acid. Upto 67% of lipid peroxidation was inhibited by 2 mg/ml of the lichen extract. The extract showed strong free radical scavenging activity similar to that of BHA (positive control) in a manner of concentration dependent. The lichen extract also showed moderate effects on superoxide anoin scavenging activity and reducing power, which was not so effective as that of Quercetin and BHA used as positive controls. This study suggests that T. vermicularis lichen can be used as a novel source of natural antioxidant. PMID:24039484

Luo, Heng; Ren, Meirong; Lim, Kwang-Mi; Koh, Young Jin; Wang, Li-Song

2006-01-01

118

In vitro screening of leishmanicidal activity in myanmar timber extracts.  

PubMed

Seventy-five Myanmar timber extracts belonging to 27 families were examined for their leishmanicidal activities. Some timber extracts had significant leishmanicidal activity, especially extracts of Millettia pendula, which exhibited the most potent activity (MLC 3.1 microg/ml, MIC 1.6 microg/ml). Other timber extracts showing potent activity included those from Cedrela serrata, Cedrela toona, Cordia fragrantissima, Calophyllum kunstleri, Dalbergia cultrate, Grevillea robusta, Haplophragma adenophyllum, Michelia champaca, and Tectona grandis. From a literature search for reports on the chemical constituents of these plants, most constituents were found to be quinone derivatives or other compounds with unsaturated carbonyl groups. PMID:15187448

Takahashi, Marii; Fuchino, Hiroyuki; Satake, Motoyoshi; Agatsuma, Yutaka; Sekita, Setsuko

2004-06-01

119

In-vitro anticoagulant activity of fucoidan derivatives from brown seaweed Laminaria japonica  

NASA Astrophysics Data System (ADS)

Fucoidan, a group of sulfated heteropolysaccharides, was extracted from Laminaria japonica, an important economic alga species in China. The anticoagulant activity of fucoidan and its derivatives (including sulfated, phosphorylated, and aminated fucoidan) was examined using in-vitro anticoagulant systems. The correlation between chemical variations within the fucoidan group and anticoagulant activity was determined. The in-vitro anticoagulant properties of fucoidan and its derivatives were determined by measuring activated partial thromboplastin time (APTT), prothrombin time (PT), and thrombin time (TT). The results indicate anticoagulant activity in all samples using APTT and TT assays; however, only the fucoidan derivatives affected the PT assay. Thus, the fucoidan derivatives were able to inhibit both intrinsic and extrinsic blood coagulants. Fucoidan (FPS) and its derivatives presented better anticoagulant activity than low molecular weight fucoidan (DFPS) and its derivatives, suggesting that molecular weight and proper conformation are contributing factors for anticoagulant activity of polysaccharides. Amino groups have a positive charge and can thus change the charge density of fucoidan. Accordingly, among the tested samples, aminated fucoidan (NF) was the most active reflecting the importance of charge density for anticoagulant activity. Available data obtained using in-vitro models suggest that the sulfate content, sulfate/total-sugar ratio, molecular weight, and the substituted group of fucoidan are important factors for anticoagulant activity but that the influence of sulfate, phosphate and amino groups on anticoagulant activity was different.

Wang, Jing; Zhang, Quanbin; Zhang, Zhongshan; Hou, Yun; Zhang, Hong

2011-05-01

120

In vitro evaluation of antioxidant activity of Cordia dichotoma (Forst f.) bark  

PubMed Central

Cordia dichotoma Forst. f. bark, identified as botanical source of Shleshmataka in Ayurvedic pharmacopoeia. Present investigation was undertaken to evaluate possible antioxidant potential of methanolic and butanol extract of C. dichotoma bark. In vitro antioxidant activity of methanolic and butanol extract was determined by 1,1, diphenyl–2, picrylhydrazyl (DPPH) free radical scavenging assay. The extracts were also evaluated for their phenolic contents and antioxidant activity. Phenolic content was measured using Folin–Ciocalteu reagent and was calculated as Gallic acid equivalents. Antiradical activity of methanolic extract was measured by DPPH assay and was compared to ascorbic acid and ferric reducing power of the extract was evaluated by Oyaizu method. In the present study three in vitro models were used to evaluate antioxidant activity. The first two methods were for direct measurement of radical scavenging activity and remaining one method evaluated the reducing power. The present study revealed that the C. dichotoma bark has significant radical scavenging activity. PMID:24049418

Nariya, Pankaj B.; Bhalodia, Nayan R.; Shukla, Vinay J.; Acharya, Rabinarayan; Nariya, Mukesh B.

2013-01-01

121

Lack of activity of cadmium in in vitro estrogenicity assays  

Microsoft Academic Search

Prompted by reports about strong estrogenic effects of cadmium, attempts were made to reproduce these observations using the yeast estrogen screen (YES) and the E-Screen assays. For the first time, possible activation of the Src\\/MAPK pathway was also investigated. In the YES, only a slight activation (10% of a maximal effect) of the estrogen receptor alpha (ER?) was observed at

Elisabete. Silva; Maria José Lopez-Espinosa; José-Manuel Molina-Molina; Marieta Fernández; Nicolas Olea; Andreas Kortenkamp

2006-01-01

122

In vitro peroxynitrite scavenging activity of diarylheptanoids from Curcuma longa.  

PubMed

Peroxynitrite is a cytotoxic intermediate produced by the reaction between the superoxide anion (O(2)) and nitric oxide (NO). The aim of this study was to investigate the scavenging effects of Curcuma longa L. on authentic peroxynitrite, and further studies are planned that will attempt to identify the active principles from the active fractions. The methanolic extract of C. longa showed 50% scavenging activity (IC(50)) at concentration of 1.7 +/- 0.08 micro g/ml, and was thus fractionated with several solvents. The peroxynitrite scavenging activity potential of the individual fraction was in the order of ethyl acetate > dichloromethane > water fraction. The ethyl acetate soluble fraction exhibiting strong scavenging activity was further purified by repeated silica gel column chromatography. Peroxynitrite scavenging diarylheptanoids, curcumin I (1), curcumin II (2), and curcumin III (3) were isolated as active principles. Compounds 1-3 showed the peroxynitrite scavenging activities with IC(50) values of 4.0 +/- 0.04, 6.4 +/- 0.30, and 29.7 +/- 1.29 micro M, respectively. Penicillamine as positive control exhibited IC(50) value of 2.38 +/- 0.34 micro M. The structure-activity relationship of diarylheptanoids on peroxynitrite was also discussed. PMID:12748983

Kim, Jung Eun; Kim, Ae Ra; Chung, Hae Young; Han, Shin Young; Kim, Byung Soo; Choi, Jae Sue

2003-05-01

123

In vitro and in vivo activities of Peganum harmala extract against Leishmania major  

PubMed Central

BACKGROUND: In vitro and in vivo antileishmanial activities of crude hydroalcoholic extract of peganum harmala seeds were investigated against Leishmania major. METHODS: The extract of aerial parts of P harmala was obtained by maceration. The in vitro experiments were performed on promastigotes to assess antileishmanial activity of the extract using amphotericin B as a reference. The in vivo studies were carried out on cutaneous leishmaniasis in outbred mice to evaluate the effects of topical application of the ointment-based extract. RESULTS: The in vitro experiments showed a concentration-dependent decrease of parasites number caused by the extract with an IC50 value of 59.4 ?g/ml. In vivo studies demonstrated a significant post-treatment decrease in the lesion size and parasite count in infected animals, compared to placebo and control groups. High performance liquid chromatography (HPLC) of the crude extract demonstrated the existence of harmaline and harmine as beta-carboline alkaloids. CONCLUSIONS: P harmala seeds extract showed significant in vitro and in vivo antileishmanial activities. Most biological activity of the extract could be attributed to its beta-carboline content. However, another alkaloid of P harmala seeds extract, peganine, has also been reported to have antileishmanial activity. These beneficial effects can be attributed to the cumulative effects of various biologically active components present in it. PMID:22279479

Rahimi-Moghaddam, Parvaneh; Ebrahimi, Soltan Ahmed; Ourmazdi, Hourmazd; Selseleh, Monawar; Karjalian, Maryam; Haj-Hassani, Giti; Alimohammadian, Mohammad Hossein; Mahmoudian, Massoud; Shafiei, Massoumeh

2011-01-01

124

In vitro and in vivo antitrypanosomal activity of Xanthium strumarium leaves.  

PubMed

Antitrypanosomal activity of crude 50% ethanolic extract of Xanthium strumarium leaves was studied in vitro and in vivo. The extract exhibited trypanocidal activity at all four concentrations tested i.e. 5, 50, 500 and 1000 micrograms/ml, in vitro. In vivo trial revealed that the extract exerted antitrypanosomal effect at dosage of 100, 300 and 1000 mg/kg, intraperitoneally. At 100 and 300 mg/kg doses the survival period of the Trypanosoma evansi infected mice was significantly prolonged. However, the extract was found to be toxic to the animals at 1000 mg/kg dose. PMID:8824739

Talakal, T S; Dwivedi, S K; Sharma, S R

1995-12-15

125

Activities of citrate synthase and other enzymes of Acetobacter xylinum in situ and in vitro.  

PubMed Central

The activities of a number of enzymes, extracted from Acetobacter xylinum, that are involved in carbohydrate metabolism may be accounted for in situ in permeabilized cells. The kinetic properties of citrate synthase and glycerokinase observed in vitro are also retained in situ. So is the regulatory sensitivity of these enzymes. Both in vitro and in situ, (a) citrate synthase, in contrast with the enzyme for other Gram-negative bacteria, is inhibited by ATP and is insensitive to NADH, and (b) glycerokinase is inhibited by fructose diphosphate and the ratio of its activities towards glycerol and dihydroxyacetone is the same. PMID:1275900

Swissa, M; Weinhouse, H; Benziman, M

1976-01-01

126

Anti-Herpetic Activity of Callissia fragrans and Simmondsia chinensis Leaf Extracts In Vitro  

PubMed Central

The antiviral activity of Callissia fragrans and Simnondsia chinensis aquatic and ethanol leaf extracts, as well as purified fractions from these extracts was studied against herpetic viruses in vitro. Ethanol extract of C. fragrans effectively inhibited the infection of Vero cells by HSV-1, HSV-2 in vitro, while its aquatic extract inhibited only VZV. Although S. chinensis leaf extract strongly inhibited all studied viruses, the selectivity index of this extract was very low, due to its high toxicity. However, the majority of its fractions showed low toxicity and higher antiviral activity and therefore very high SI. Strong interactions between virus and extracts were found. PMID:20700398

Yarmolinsky, Ludmila; Zaccai, Michele; Ben-Shabat, Shimon; Huleihel, Mahmoud

2010-01-01

127

In vitro angiogenic activity of Aloe vera gel on calf pulmonary artery endothelial (CPAE) cells  

Microsoft Academic Search

Angiogenic activity ofAloe vera gel was investigated byin vitro assay. We obtained the most active fraction from dichloromethane extract ofAloe vera gel by partitioning between hexane and 90% aqueous methanol. The most active fraction (F3) increased the proliferation of\\u000a calf pulmonary artery endothelial (CPAE) cells. In addition, F3 fraction induced CPAE cells to invade type I collagen gel\\u000a and form

Myoung-Jin Lee; Ok-Hee Lee; Soo-Hong Yoon; Seung-Ki Lee; Myung-Hee Chung; Young-In Park; Chung-Ki Sung; Jae-Sue Choi; Kyu-Won Kim

1998-01-01

128

In vitro activity of the enantiomers of mefloquine, halofantrine and enpiroline against Plasmodium falciparum.  

PubMed Central

The in vitro activity of the enantiomers of mefloquine, halofantrine and enpiroline was compared against chloroquine-resistant and -susceptible strains of Plasmodium falciparum using a semi-micro drug susceptibility test. For each strain, the corresponding enantiomers exhibited similar activities. The enantiomers of halofantrine were the most active against both susceptible and resistant strains, followed by the enantiomers of mefloquine and enpiroline. PMID:1524966

Basco, L K; Gillotin, C; Gimenez, F; Farinotti, R; Le Bras, J

1992-01-01

129

Antifungal activity of three mouth rinses--in vitro study.  

PubMed

Mouthrinses are nowadays routinely included in the home care oral hygiene maintenance besides dentifrice/tooth paste. Mouthrinses prevent bacterial attachment and prevent or slow down bacterial proliferation. Fungal organisms have now gained more importance due to increased incidence of AIDS/HIV. This has necessitated for mouthrinses to possess antifungal activity also. The mouthrinses used were Povidone iodine ( Wokadine), Thymol with Eucalyptol and Benzoic acid (Listerine) and fluoride with Triclosan (Colgate Plax), which were tested against oral isolates of different species of Candida. The agar diffusion test was used to evaluate the inhibitory activity of the mouthrinses and all of them exhibited antifungal activity especially against Candida albicans. PMID:16758789

Abirami, C P; Venugopal, Pankajalakshmi V

2005-01-01

130

In Vitro Neuroprotective Activities of Compounds from Angelica shikokiana Makino.  

PubMed

Angelica shikokiana is widely marketed in Japan as a dietary food supplement. With a focus on neurodegenerative conditions such as Alzheimer's disease, the aerial part was extracted and through bio-guided fractionation, fifteen compounds [?-glutinol, ?-amyrin, kaempferol, luteolin, quercetin, kaempferol-3-O-glucoside, kaempferol-3-O-rutinoside, methyl chlorogenate, chlorogenic acid, hyuganin E, 5-(hydroxymethyl)-2-furaldehyde, ?-sitosterol-3-O-glucoside, adenosine (isolated for the first time from A. shikokiana), isoepoxypteryxin and isopteryxin] were isolated. Isolated compounds were evaluated for in vitro neuroprotection using acetylcholine esterase inhibitory, protection against hydrogen peroxide and amyloid ? peptide (A?25-35)-induced neurotoxicity in neuro-2A cells, scavenging of hydroxyl radicals and intracellular reactive oxygen species and thioflavin T assays. Quercetin showed the strongest AChE inhibition (IC50 value = 35.5 µM) through binding to His-440 and Tyr-70 residues at the catalytic and anionic sites of acetylcholine esterase, respectively. Chlorogenic acid, its methyl ester, quercetin and luteolin could significantly protect neuro-2A cells against H2O2-induced neurotoxicity and scavenge hydroxyl radical and intracellular reactive oxygen species. Kaempferol-3-O-rutinoiside, hyuganin E and isoepoxypteryxin significantly decreased A?25-35-induced neurotoxicity and Th-T fluorescence. To the best of our knowledge, this is the first report about neuroprotection of hyuganin E and isoepoxypteryxin against A?25-35-induced neurotoxicity. PMID:25786165

Mira, Amira; Yamashita, Shuntaro; Katakura, Yoshinori; Shimizu, Kuniyoshi

2015-01-01

131

Inhibition of catalase activity in vitro by diesel exhaust particles  

Microsoft Academic Search

The effect of diesel exhaust particles (DEP) on the activity of catalase, an intracellular anti-oxidant, was investigated because HâOâ is a cytotoxic oxidant, and catalase released from alveolar cells is an important antioxidant in the epithelial lining fluid in the lung. DEP inhibited the activity of bovine liver catalase dose-dependently, to 25-30% of its original value. The inhibition of catalase

Yoki Mori; Sumika Murakami; Toshiyuki Sagae

1996-01-01

132

Activated T Lymphocytes Support Osteoclast Formation in Vitro  

Microsoft Academic Search

Osteoblastic stromal cells are capable of supporting osteoclast formation from hematopoietic precursors in the presence of osteotropic factors such as 1?,25(OH)2D3, PTH, and IL-11. Osteoblastic stromal cells produce receptor activator of NF-?B ligand (RANKL), a type II membrane protein of the TNF ligand family, in response to these agents. Activated T lymphocytes also produce RANKL; however, the ability of this

Nicole J. Horwood; Vicky Kartsogiannis; Julian M. W. Quinn; Evangelos Romas; T. John Martin; Matthew T. Gillespie

1999-01-01

133

In vitro antibacterial activity of some plant essential oils  

PubMed Central

Background: To evaluate the antibacterial activity of 21 plant essential oils against six bacterial species. Methods: The selected essential oils were screened against four gram-negative bacteria (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Proteus vulgaris) and two gram-positive bacteria Bacillus subtilis and Staphylococcus aureus at four different concentrations (1:1, 1:5, 1:10 and 1:20) using disc diffusion method. The MIC of the active essential oils were tested using two fold agar dilution method at concentrations ranging from 0.2 to 25.6 mg/ml. Results: Out of 21 essential oils tested, 19 oils showed antibacterial activity against one or more strains. Cinnamon, clove, geranium, lemon, lime, orange and rosemary oils exhibited significant inhibitory effect. Cinnamon oil showed promising inhibitory activity even at low concentration, whereas aniseed, eucalyptus and camphor oils were least active against the tested bacteria. In general, B. subtilis was the most susceptible. On the other hand, K. pneumoniae exhibited low degree of sensitivity. Conclusion: Majority of the oils showed antibacterial activity against the tested strains. However Cinnamon, clove and lime oils were found to be inhibiting both gram-positive and gram-negative bacteria. Cinnamon oil can be a good source of antibacterial agents. PMID:17134518

Prabuseenivasan, Seenivasan; Jayakumar, Manickkam; Ignacimuthu, Savarimuthu

2006-01-01

134

Botulinum Toxin Suppression of CNS Network Activity In Vitro  

PubMed Central

The botulinum toxins are potent agents which disrupt synaptic transmission. While the standard method for BoNT detection and quantification is based on the mouse lethality assay, we have examined whether alterations in cultured neuronal network activity can be used to detect the functional effects of BoNT. Murine spinal cord and frontal cortex networks cultured on substrate integrated microelectrode arrays allowed monitoring of spontaneous spike and burst activity with exposure to BoNT serotype A (BoNT-A). Exposure to BoNT-A inhibited spike activity in cultured neuronal networks where, after a delay due to toxin internalization, the rate of activity loss depended on toxin concentration. Over a 30?hr exposure to BoNT-A, the minimum concentration detected was 2?ng/mL, a level consistent with mouse lethality studies. A small proportion of spinal cord networks, but not frontal cortex networks, showed a transient increase in spike and burst activity with exposure to BoNT-A, an effect likely due to preferential inhibition of inhibitory synapses expressed in this tissue. Lastly, prior exposure to human-derived antisera containing neutralizing antibodies prevented BoNT-A induced inhibition of network spike activity. These observations suggest that the extracellular recording from cultured neuronal networks can be used to detect and quantify functional BoNT effects. PMID:24688538

Pancrazio, Joseph J.; Gopal, Kamakshi; Keefer, Edward W.; Gross, Guenter W.

2014-01-01

135

In vitro evaluation of the growth inhibitory activities of 15 drugs against Babesia gibsoni (Aomori strain).  

PubMed

The in vitro growth inhibitory activities of 15 drugs against Babesia gibsoni were evaluated following establishment of a continuous culture isolate (Aomori isolate). The culture was successfully continued in an RPMI-1640 medium supplemented with 20% normal canine serum or fetal bovine serum in a humidified atmosphere containing 5% CO2 and 5% O2 at 37 degrees C. We used this isolate to evaluate the growth inhibitory effect of naphthoquinone (atovaquone), aromatic diamidine (diminazene and pentamidine), artemisinin compounds (artesunate and dihydroartemisinin), an iron chelator (deferoxamine), quinoline-containing compounds (quinine and chloroquine), macrolide antibiotics (azithromycin), lyncomycin antibiotics (clindamycin), tetracycline antibiotics (doxycycline and minocycline), imidazole antifungals (clotrimazole and ketoconazole), and a nitroimidazole antiprotozoal (metronidazole). Atovaquone and aromatic diamidine showed the highest activity; they were followed by artesunate compounds with nanomole levels of IC50. Metronidazole did not exhibit activity against the parasite. Other drugs exhibited intermediate in vitro activities with micromole levels of IC50. This is the first report to screen drug activities against B. gibsoni in vitro. The results of our study may support further in vitro drug evaluation for the establishment of therapeutic strategies against canine B. gibsoni infections. PMID:18771856

Matsuu, Aya; Yamasaki, Masahiro; Xuan, Xuenan; Ikadai, Hiromi; Hikasa, Yoshiaki

2008-10-20

136

In vitro activities of four xyloglucan endotransglycosylases from Arabidopsis  

NASA Technical Reports Server (NTRS)

Xyloglucan endotransglycosylases (XETs) are encoded by a gene family in Arabidopsis thaliana. These enzymes modify a major structural component of the plant cell wall, xyloglucan, and therefore may influence plant growth and development. We have produced four Arabidopsis XETs (TCH4, Meri-5, EXGT and XTR9) using the baculovirus/insect cell system and compared their biochemical activities. TCH4, as previously demonstrated, and the other three proteins are capable of carrying out transglycosylation of xyloglucans. The K(m) for XLLGol acceptor oligosaccharide is in the range of 20-40 microM for all the XETs except XTR9, which has a Km of 5 microM and is significantly inhibited by high levels of XLLGol. All four enzymes are most active between pH 6.0 and 6.5. TCH4 and XTR9 have temperature optima of 18 degrees C, whereas Meri-5 and EXGT are most active at 28 and 37 degrees C, respectively. Although the activity levels of three of the XETs are not influenced by the presence of fucose on the xyloglucan polymer, XTR9 has a clear preference for non-fucosylated xyloglucan polymer. The four XETs show a marked preference for XLLGol over either XXFGol or XXXGol as acceptor oligosaccharide. All four XETs are glycosylated; however, only the activities of TCH4 and Meri-5 are affected by the removal of the N-glycan with PNGase F. These four enzymes most likely function solely as transglycosylases because xyloglucan endoglucanase activity was not apparent. Subtle differences in biochemical activities may influence the physiological functions of the distinct XETs in vivo.

Campbell, P.; Braam, J.; McIntire, L. V. (Principal Investigator)

1999-01-01

137

In vitro determination of the spermicidal activity of plant saponins.  

PubMed

The plant kingdom might yield an effective antifertility drug. A Mentha arvensis L. (Labiatae) fraction with uterotonic activity was isolated, and was found to be active on the nonpregnant as well as the pregnant rat uterus. According to folklore medicine, the Mexican plant Montanoa tomentosa Cerv. (zoapatle) possesses antifertility activity in women. The effect of various isolated preparations from this plant on early pregnancy were investigated in serveral rodent species including the mouse, rat hamster, and guinea pig. It was concluded that zoapatle plant extracts possess unique antifertility activity. Lin-Hsim and coworkers isolated fractions from Aristolochia molissima Hanceith contrceptive activity in female mice. Saponins of some plants were used in contraceptive formulations either as foaming agents or as spermicidal substances. Elbary and Nour investigated the spermicidal effects of saponins isolated from the following plants: Gypsophila paniculata L., Saponaria officinalis L., Enterolobium cyclocarpum, Griseb., Terminalia horrida Steud., Melilotus sicula Vitm., and Ruscus hypoglossum L. All of the saponins tested possessed spermicidal activity. Jain and coworkers isolated 2 new saponins in Pittosporum nilghrense with spermicidal effects. In this paper we have determined the spermicidal activity of saponins isolated from some Yugoslav plants, which in that aspect have not been investigated. The results are illustrated in the table. They show that all of the saponins tested were spermicidal in dependence on their nature. Saponins of Primula vulgaris Huds. and Cyclamen persicum Mill. immobilized human spermatozoa within a period of 20 s at a dilution 1:1000. Saponin of Gypsophila paniculata L. was spermicidal at dilution 1:20. These findings show that saponins isolated from some Yugoslav plants may be useful spermicides of natural origin. PMID:4080814

Primorac, M; Sekulovi?, D; Antoni?, S

1985-08-01

138

Secretory activity of Poecilia latipinna (Teleostei) pituitary in vitro: rostral pars distalis and proximal pars distalis.  

PubMed

The ultrastructure of each adenohypophysial secretory cell type was examined in pituitaries of adult female mollies (Poecilia latipinna) after various periods in vitro, and with varied medium osmotic pressure (OP), Na+, and Ca2+ concentrations. Prolactin (PRL) cells were markedly activated by 18 hr, and after 7 or 14 days were almost totally degranulated, with massive arrays of Golgi and RER. Reduction in OP, but not Na+ or Ca2+, caused an additional activation of PRL cells after periods of 18 hr or longer. Corticotroph (ACTH) cells became noticeably activated by 4 hr, and were possibly affected by OP, but not Na+ or Ca2+. Growth hormone (GH) cells were activated by 6 hr, and after 18 hr were quite degranulated with extensive arrays of RER. OP had no effect on GH cells before 3 days, when reduced OP appeared to cause an additional activation, with the appearance of large irregular secretory granule (SG)-like inclusions. Na+ and Ca2+ again had no effect. Gonadotrophic (GtH) cells appeared to be little affected by in vitro incubation; however, the very active cells from vitellogenic fish underwent a reduction in dilated RER after prolonged culture. Thyrotrophic (TSH) cells gradually became activated in vitro, but the response again varied with the sexual condition of the fish. Neither GtH nor TSH cells were affected by OP, Na+, or Ca2+. The findings are discussed in relation to hypothalamic control, via releasing/inhibiting factors, of adenohypophysial cell activity. PMID:6309607

Batten, T F; Young, G; Ball, J N

1983-07-01

139

PAC-1 Activates Procaspase-3 in vitro through Relief of Zinc-Mediated Inhibition  

PubMed Central

SUMMARY The direct induction of apoptosis has emerged as a powerful anti-cancer strategy, and small molecules that either inhibit or activate certain proteins in the apoptotic pathway have great potential as novel chemotherapeutic agents. Central to apoptosis is the activation of the zymogen procaspase-3 to caspase-3. Caspase-3 is the key “executioner” caspase, catalyzing the hydrolysis of a multitude of protein substrates within the cell. Interestingly, procaspase-3 levels are often elevated in cancer cells, suggesting a compound that directly stimulates the activation of procaspase-3 to caspase-3 could selectively induce apoptosis in cancer cells. We recently reported the discovery of a compound, PAC-1, which enhances procaspase-3 activity in vitro and induces apoptotic death in cancer cells in culture and in mouse xenograft models. Described herein is the mechanism by which PAC-1 activates procaspase-3 in vitro. We show that zinc inhibits the enzymatic activity of procaspase-3, and that PAC-1 strongly activates procaspase-3 in buffers that contain zinc. PAC-1 and zinc form a tight complex with one another, with a dissociation constant of approximately 42 nM. The combined data indicate that PAC-1 activates procaspase-3 in vitro by sequestering inhibitory zinc ions, thus allowing procaspase-3 to autoactivate itself to caspase-3. The small molecule mediated activation of procaspases has great therapeutic potential and thus this discovery of the in vitro mechanism of action of PAC-1 is critical to the development and optimization of other procaspase-activating compounds. PMID:19281821

Peterson, Quinn P.; Goode, David R.; West, Diana C.; Ramsey, Kara N.; Lee, Joy; Hergenrother, Paul J.

2009-01-01

140

In-vitro Antimicrobial Activities of Some Iranian Conifers.  

PubMed

Male and female leaves and fruits of eleven different taxons of Iranian conifers (Cupressus sempervirens var. horizontalis, C. sempervirens var. sempervirens, C. sempervirens cv. Cereifeormis, Juniperus communis subsp. hemisphaerica, J. excelsa subsp. excelsa, J. excelsa subsp. polycarpos, J. foetidissima, J. oblonga, J. sabina, Platycladus orientalis and Taxus baccata) were collected from different localities of Iran, dried and extracted with methanol. The extracts were tested for their antimicrobial activity against Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli and Candida albicans. The extracts were screened qualitatively using four different methods, the disc diffusion, hole plate, cylinder agar diffusion and agar dilution methods, whereas the minimum inhibitory concentrations (MIC) of each extract were determined by the agar dilution method. The best result was obtained by means of hole plate method in qualitative determination of antimicrobial activities of extracts and the greatest activity was found against S. aureus in all tested methods. PMID:24250573

Afsharzadeh, Maryam; Naderinasab, Mahboobe; Tayarani Najaran, Zahra; Barzin, Mohammad; Emami, Seyed Ahmad

2013-01-01

141

In-vitro Antimicrobial Activities of Some Iranian Conifers  

PubMed Central

Male and female leaves and fruits of eleven different taxons of Iranian conifers (Cupressus sempervirens var. horizontalis, C. sempervirens var. sempervirens, C. sempervirens cv. Cereifeormis, Juniperus communis subsp. hemisphaerica, J. excelsa subsp. excelsa, J. excelsa subsp. polycarpos, J. foetidissima, J. oblonga, J. sabina, Platycladus orientalis and Taxus baccata) were collected from different localities of Iran, dried and extracted with methanol. The extracts were tested for their antimicrobial activity against Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli and Candida albicans. The extracts were screened qualitatively using four different methods, the disc diffusion, hole plate, cylinder agar diffusion and agar dilution methods, whereas the minimum inhibitory concentrations (MIC) of each extract were determined by the agar dilution method. The best result was obtained by means of hole plate method in qualitative determination of antimicrobial activities of extracts and the greatest activity was found against S. aureus in all tested methods. PMID:24250573

Afsharzadeh, Maryam; Naderinasab, Mahboobe; Tayarani Najaran, Zahra; Barzin, Mohammad; Emami, Seyed Ahmad

2013-01-01

142

In vitro activity of ketoconazole against herpes simplex virus.  

PubMed Central

The effects of ketoconazole alone and in combination with acyclovir and adenine arabinoside upon the replication of herpes simplex virus types 1 and 2 (HSV-1 and -2) were investigated by using a yield reduction assay. Ketoconazole demonstrated antiviral activity against HSV-1 and -2 and synergistic antiviral activity when it was combined with acyclovir. Combinations of ketoconazole with adenine arabinoside resulted in either interference or indifference. The effects of ketoconazole upon the protein synthesis of HSV-2-infected cells were also determined in an effort to define the mechanism of action for the antiviral activity of ketoconazole. There was no reduction of HSV proteins when compared with acyclovir. These findings suggest that further investigations of the use of ketoconazole for the treatment of HSV infections are warranted. Images PMID:3021048

Pottage, J C; Kessler, H A; Goodrich, J M; Chase, R; Benson, C A; Kapell, K; Levin, S

1986-01-01

143

Impact of antibacterial drugs on human serum paraoxonase-1 (hPON1) activity: an in vitro study  

PubMed Central

Objective To investigate the in vitro effects of the antibacterial drugs, meropenem trihydrate, piperacillin sodium, and cefoperazone sodium, on the activity of human serum paraoxonase (hPON1). Methods hPON1 was purified from human serum using simple chromatographic methods, including DEAE-Sephadex anion exchange and Sephadex G-200 gel filtration chromatography. Results The three antibacterial drugs decreased in vitro hPON1 activity. Inhibition mechanisms meropenem trihydrate was noncompetitive while piperacillin sodium and cefoperazone sodium were competitive. Conclusions Our results showed that antibacterial drugs significantly inhibit hPON1 activity, both in vitro, with rank order meropenem trihydrate piperacillin sodium cefoperazone sodium in vitro. PMID:25183328

Söyüt, Hakan; Kaya, Elif Duygu; Beydemir, ?ükrü

2014-01-01

144

Antiulcer and in vitro antioxidant activities of Jasminum grandiflorum L  

Microsoft Academic Search

The study was aimed at evaluating the antiulcer and antioxidant activities of 70% ethanolic axtract of leaves of Jasminum grandiflorum L. (JGLE). The leaves of Jasminum grandiflorum L. (Family: Oleaceae) is used in folk medicine for treating ulcerative stomatitis, skin diseases, ulcers, wounds, corns—a hard or soft hyperkeratosis of the sole of the human foot secondary to friction and pressure

M. Umamaheswari; K. Asokkumar; R. Rathidevi; A. T. Sivashanmugam; V. Subhadradevi; T. K. Ravi

2007-01-01

145

In vitro anti-MRSA activity of carvone with gentamicin.  

PubMed

Carvone is one of the naturally occurring monoterpenes, the largest class of secondary metabolites in plants, and exists in two enantiomers, R-carvone (R-car) and S-car. The objective of this study was to investigate the antimicrobial activity of R-car and S-car with gentamicin (GET) against methicillin-resistant Staphylococcus aureus (MRSA). MRSA is a major human pathogen that causes serious problems, including hospital-acquired pneumonia, abscesses and surgical wound infections. Nosocomial MRSA infections often exhibit multidrug resistance. In the present study, antimicrobial susceptibility testing was performed with R-car, S-car and GET using the broth microdilution method. Minimal inhibitory concentration values for R- and S-car against six different strains of S. aureus ranged between 500 and 1,000 ?g/ml. Anti-MRSA activity was evaluated using the checkerboard and time-kill assays to investigate the potential synergistic effects of different combinations of the carvone enantiomers and GET. R-car plus S-car, R-car plus GET and S-car plus GET exhibited significant synergistic activity against MRSA. These findings suggest that the single-agent anti-MRSA activities of R-car, S-car and GET are effectively increased through combination therapy. This study showed that carvone may be a potential adjuvant antimicrobial agent. PMID:24669246

Mun, Su-Hyun; Kang, Ok-Hwa; Joung, Dae-Ki; Kim, Sung-Bae; Choi, Jang-Gi; Shin, Dong-Won; Kwon, Dong-Yeul

2014-04-01

146

In vitro anti-MRSA activity of carvone with gentamicin  

PubMed Central

Carvone is one of the naturally occurring monoterpenes, the largest class of secondary metabolites in plants, and exists in two enantiomers, R-carvone (R-car) and S-car. The objective of this study was to investigate the antimicrobial activity of R-car and S-car with gentamicin (GET) against methicillin-resistant Staphylococcus aureus (MRSA). MRSA is a major human pathogen that causes serious problems, including hospital-acquired pneumonia, abscesses and surgical wound infections. Nosocomial MRSA infections often exhibit multidrug resistance. In the present study, antimicrobial susceptibility testing was performed with R-car, S-car and GET using the broth microdilution method. Minimal inhibitory concentration values for R- and S-car against six different strains of S. aureus ranged between 500 and 1,000 ?g/ml. Anti-MRSA activity was evaluated using the checkerboard and time-kill assays to investigate the potential synergistic effects of different combinations of the carvone enantiomers and GET. R-car plus S-car, R-car plus GET and S-car plus GET exhibited significant synergistic activity against MRSA. These findings suggest that the single-agent anti-MRSA activities of R-car, S-car and GET are effectively increased through combination therapy. This study showed that carvone may be a potential adjuvant antimicrobial agent. PMID:24669246

MUN, SU-HYUN; KANG, OK-HWA; JOUNG, DAE-KI; KIM, SUNG-BAE; CHOI, JANG-GI; SHIN, DONG-WON; KWON, DONG-YEUL

2014-01-01

147

Assaying the kinase activity of LRRK2 in vitro.  

PubMed

Leucine Rich Repeat Kinase 2 (LRRK2) is a 2527 amino acid member of the ROCO family of proteins, possessing a complex, multidomain structure including a GTPase domain (termed ROC, for Ras of Complex proteins) and a kinase domain. The discovery in 2004 of mutations in LRRK2 that cause Parkinson's disease (PD) resulted in LRRK2 being the focus of a huge volume of research into its normal function and how the protein goes awry in the disease state. Initial investigations into the function of LRRK2 focused on its enzymatic activities. Although a clear picture has yet to emerge of a consistent alteration in these due to mutations, data from a number of groups has highlighted the importance of the kinase activity of LRRK2 in cell death linked to mutations. Recent publications have reported inhibitors targeting the kinase activity of LRRK2, providing a key experimental tool. In light of these data, it is likely that the enzymatic properties of LRRK2 afford us an important window into the biology of this protein, although whether they are potential drug targets for Parkinson's is open to debate. A number of different approaches have been used to assay the kinase activity of LRRK2. Initially, assays were carried out using epitope tagged protein overexpressed in mammalian cell lines and immunoprecipitated, with the assays carried out using this protein immobilised on agarose beads. Subsequently, purified recombinant fragments of LRRK2 in solution have also been used, for example a GST tagged fragment purified from insect cells containing residues 970 to 2527 of LRRK2. Recently, Daniëls et al. reported the isolation of full length LRRK2 in solution from human embryonic kidney cells, however this protein is not widely available. In contrast, the GST fusion truncated form of LRRK2 is commercially available (from Invitrogen, see table 1 for details), and provides a convenient tool for demonstrating an assay for LRRK2 kinase activity. Several different outputs for LRRK2 kinase activity have been reported. Autophosphorylation of LRRK2 itself, phosphorylation of Myelin Basic Protein (MBP) as a generic kinase substrate and phosphorylation of an artificial substrate--dubbed LRRKtide, based upon phosphorylation of threonine 558 in Moesin--have all been used, as have a series of putative physiological substrates including ?-synuclein, Moesin and 4-EBP. The status of these proteins as substrates for LRRK2 remains unclear, and as such the protocol described below will focus on using MBP as a generic substrate, noting the utility of this system to assay LRRK2 kinase activity directed against a range of potential substrates. PMID:22301813

Lewis, Patrick A

2012-01-01

148

In vivo and in vitro antileishmanial activity of Bungarus caeruleus snake venom through alteration of immunomodulatory activity.  

PubMed

Leishmaniasis threatens more than 350 million people worldwide specially in tropical and subtropical region. Antileishmanial drugs that are currently available have various limitations. The search of new drugs from natural products (plants, animals) possessing antileishmanial activity is ventured throughout the world. The present study deals with the antileishmanial activity of Bungarus caeruleus snake venom (BCV) on in vitro promastigotes and amastigotes of Leishmania donovani parasite and leishmania infected BALB/c mice. The effect of BCV on peritoneal macrophage, release of cytokines from the activated macrophages, production of nitric oxide, reactive oxygen species and cytokines were studied in vivo and in vitro. IC50 value of BCV on L. donovani promastigote was 14.5 ?g/ml and intracellular amastigote was 11.2 ?g/ml. It activated peritoneal macrophages, significantly increased cytokines and interleukin production. BCV (20 ?g/kg and 40 ?g/kg body weight of mice) decreased parasite count by 54.9% and 74.2% in spleen and 41.4% and 60.4% in liver of infected BALB/c mice. BCV treatment significantly increased production of TNF-?, IFN-?, ROS, NO in infected mice. Histological studies showed decreased granuloma formation in treated liver as compared with control. Liver and spleen structure was partially restored due to BCV treatment in infected mice. The present study revealed that BCV possessed antileishmanial activity against L. donovani parasite in vivo and in vitro and this activity was partly mediated through immunomodulatory activity involving macrophages. PMID:23830987

Bhattacharya, Shamik; Ghosh, Prasanta; De, Tripti; Gomes, Antony; Gomes, Aparna; Dungdung, Sandhya Rekha

2013-09-01

149

Lasting modulation of in-vitro oscillatory activity with weak direct current stimulation  

E-print Network

University of New York, New York, USA December 3, 2014 Abstract Transcranial Direct Current Stimulation (t hypothesis. Introduction The number of studies on transcranial direct current stimulation (tDCS) has rapidlyLasting modulation of in-vitro oscillatory activity with weak direct current stimulation Davide

Parra, Lucas C.

150

In Vitro Anthelmintic Activity of Allium sativum, Zingiber officinale, Curcurbita mexicana and Ficus religiosa  

Microsoft Academic Search

Methanol extracts of some commonly used plant materials of ethnoveterinary importance in Pakistan were screened for their in vitro anthelmintic activity. Results revealed that Zingiber officinale killed all the test worms (Haemonchus contortus) within two hours post exposure being 100% effective. Allium sativum and Cucurbita mexicana extracts were equally effective at 2 and 4 h post exposure; by 6 h

ZAFAR IQBAL; QAZI KHALID NADEEM; M. N. KHAN; M. S. AKHTAR; FAISAL NOUMAN WARAICH

151

Comparison of relative antioxidant activities of British medicinal plant species in vitro  

Microsoft Academic Search

We have determined the relative levels of endogenous antioxidant activity in a range of British medicinal plant species (representative of a variety of plant families, selected on the basis of their widespread use in traditional herbal medicine), via competitive scavenging of the ABTS+ or O2? radicals in vitro. A number of plant species with appreciable levels (i.e. greater than or

David Mantle; Fadel Eddeb; Anne T. Pickering

2000-01-01

152

In vitro antiplasmodial activity of medicinal plants native to or naturalised in South Africa  

Microsoft Academic Search

The increasing prevalence and distribution of malaria has been attributed to a number of factors, one of them being the emergence and spread of drug resistant parasites. Efforts are now being directed towards the discovery and development of new chemically diverse antimalarial agents. The present study reports on the in vitro antiplasmodial activity of 134 plant taxa native to or

Cailean Clarkson; Vinesh J. Maharaj; Neil R. Crouch; O GRACE; Pamisha Pillay; Motlalepula G. Matsabisa; Niresh Bhagwandin; Peter J. Smith; Peter I. Folb

2004-01-01

153

EFFECT OF WATER POLLUTANTS AND OTHER CHEMICALS UPON THE ACTIVITY OF LIPASE 'IN VITRO'  

EPA Science Inventory

Lipase preparations were treated in vitro with 100 chemicals of various classes, many of which are environmental pollutants, to determine their effect upon enzyme activity. The greatest inhibition was caused by mercuric ion and certain heavy metal cations; almost as inhibiting we...

154

In vitro activities of five new quinolones against 88 genital and neonatal Haemophilus isolates.  

PubMed Central

In vitro activities of five new quinolones against 88 strains of Haemophilus influenzae and H. parainfluenzae isolated from genitourinary or neonatal infections were studied. All strains were susceptible, and MICs were similar to those for respiratory tract isolates. However, H. influenzae biotype IV appeared to be more susceptible to norfloxacin, enoxacin, and ciprofloxacin than the other biotypes were. PMID:3258143

Quentin, R; Koubaa, N; Cattier, B; Gavignet, M; Goudeau, A

1988-01-01

155

Estrogenic Activity Assessment of Environmental Chemicals Using in Vitro Assays: Identification of Two New Estrogenic Compounds  

Microsoft Academic Search

Environmental chemicals with estrogenic activities have been suggested to be associated with deleterious effects in animals and humans. To characterize estrogenic chemicals and their mecha- nisms of action, we established in vitro and cell culture assays that detect human estrogen recep- tor ? (hER?)-mediated estrogenicity. First, we assayed chemicals to determine their ability to modulate direct interaction between the hER?

Isabelle Lascombe; Dominique Beffa; Urs Rüegg; Joseph Tarradellas; Walter Wahli

156

Polyphenols in Chocolate, Which Have Antioxidant Activity, Modulate Immune Functions in Humans in Vitro  

Microsoft Academic Search

We studied the effects of antioxidants from chocolate, cacao liquor polyphenol (CLP), on human immune functionsin vitro.CLP is an enriched polyphenol fraction purified from cacao liquor that is a major component of chocolate. It has been shown that polyphenols have antioxidant activity, and reactive oxygen species (ROS) are involved in immune responses. CLP inhibited both hydrogen peroxide and superoxide anion,

Chiaki Sanbongi; Noboru Suzuki; Tsuyoshi Sakane

1997-01-01

157

SPME determination of volatile aldehydes for evaluation of in-vitro antioxidant activity  

Microsoft Academic Search

The in-vitro antioxidant activity of natural (essential oils, vitamin E) or synthetic substances (tert-butyl hydroxy anisole (BHA), Trolox) has been evaluated by monitoring volatile carbonyl compounds released in model lipid systems subjected to peroxidation. The procedure employed methodology previously developed for the determination of carbonyl compounds as their pentafluorophenylhydrazine derivatives which were quantified, with high sensitivity, by means of capillary

Elena E. Stashenko; Miguel A. Puertas; Jairo R. Martínez

2002-01-01

158

In vivo anti-inflammatory and in vitro antioxidant activities of Mediterranean dietary plants  

Microsoft Academic Search

Five hydroalcoholic extracts of edible plants from Calabria region (Italy) used in local traditional medicine for the treatment of inflammatory diseases were evaluated for their in vivo topical anti-inflammatory activity (inhibition of croton oil-induced ear oedema in mice) and in vitro antioxidant and antiradical properties (inhibition of linoleic acid oxidation and bovine brain liposomes peroxidation, DPPH radical scavenging). All the

Filomena Conforti; Silvio Sosa; Mariangela Marrelli; Federica Menichini; Giancarlo A. Statti; Dimitar Uzunov; Aurelia Tubaro; Francesco Menichini; Roberto Della Loggia

2008-01-01

159

INFLUENCE OF CCL4 BIOTRANSFORMATION ON THE ACTIVATION OF RAT LIVER PHOSPHOLIPASE C IN VITRO  

EPA Science Inventory

The Influence of CCl4 Biotransforrnation on the Activation of Rat Liver Phospholipase C in Vitro. Coleman, J.F., Condie, L.W. AND LAMB, R.G. (1988). Toxicol. Appl Pharmacol. 95, 200-207. Carbon tetrachloride (CCL4) biotransformation and covalent binding was measured in l000g live...

160

Identification of a Vibrio furnissii Oligopeptide Permease and Characterization of Its In Vitro Hemolytic Activity? †  

PubMed Central

We describe purification and characterization of an oligopeptide permease protein (Hly-OppA) from Vibrio furnissii that has multifaceted functions in solute binding, in in vitro hemolysis, in antibiotic resistance, and as a virulence factor in bacterial pathogenesis. The solute-binding function was revealed by N-terminal and internal peptide sequences of the purified protein and was confirmed by discernible effects on oligopeptide binding, by accumulation of fluorescent substrates, and by fluorescent substrate-antibiotic competition assay experiments. The purified protein exhibited host-specific in vitro hemolytic activity against various mammalian erythrocytes and apparent cytotoxicity in CHO-K1 cells. Recombinant Hly-OppA protein and an anti-Hly-OppA monoclonal antibody exhibited and neutralized the in vitro hemolytic activity, respectively, which further confirmed the hemolytic activity of the gene product. In addition, a V. furnissii hly-oppA knockout mutant caused less mortality than the wild-type strain when it was inoculated into BALB/c mice, indicating the virulence function of this protein. Finally, the in vitro hemolytic activity was also confirmed with homologous ATP-binding cassette-type transporter proteins from other Vibrio species. PMID:17873048

Wu, Tung-Kung; Wang, Yu-Kuo; Chen, Yi-Chin; Feng, Jen-Min; Liu, Yen-Hsi; Wang, Ting-Yi

2007-01-01

161

Antiasthmatic Activity of a Macrolide Antibiotic, Roxithromycin: Analysis of Possible Mechanisms in vitro and in vivo  

Microsoft Academic Search

This study was designed to examine the possible mechanisms by which macrolide antibiotics favorably influence the clinical course of asthmatic patients. In the first set of experiments, we investigated the effect of roxithromycin (RXM), a newly synthesized macrolide antibiotic, on in vitro cytokine secretion by mitogen-activated human peripheral blood leukocytes. RXM suppressed the secretion of T cell cytokine interleukins (IL)

Shin-ichi Konno; Kazuhito Asano; Masatsugu Kurokawa; Kazuhito Ikeda; Ken-ichi Okamoto; Mitsuru Adachi

1994-01-01

162

“In vitro” antifungal activity of ozonized sunflower oil on yeasts from onychomycosis  

PubMed Central

The “in vitro” antifungal activity of ozonized sunflower oil (Bioperoxoil®) was tested on 101 samples of yeasts originating from onychomycosis using the disk diffusion method. The oil was efficacious against several clinical fungal strains: Candida parapsilosis, Candida albicans, Trichosporon asahii, Candida tropicalis and Candida guilliermondii. PMID:24031958

Guerrer, L.V.; Cunha, K. C.; Nogueira, M. C. L.; Cardoso, C. C.; Soares, M. M. C. N.; Almeida, M. T. G.

2012-01-01

163

In vitro antifungal activity of phenylheptatriyne from Bidens cernua L. against yeasts  

Microsoft Academic Search

In vitro antifungal activity of phenylheptatriyne from Bidens cernua L. (Asteraceae) was studied using broth macrodilution method against 125 strains of yeasts including 104 clinical and other isolates of Candida spp. (C. albicans, C. krusei, C. tropicalis, C. guilliermondii, C. parapsilosis, C. glabrata, C. inconspicua), 16 strains of basidiomycetous yeasts (Cryptococcus neoformans, C. albidus, Trichosporon cutaneum, Rhodotorula glutinis) and five

N. P. Rybalchenko; V. A. Prykhodko; S. S. Nagorna; N. N. Volynets; A. N. Ostapchuk; V. V. Klochko; T. V. Rybalchenko; L. V. Avdeeva

2010-01-01

164

IN VITRO ANDROGENIC ACTIVITY OF KRAFT MILL EFFLUENT IS ASSOCIATED WITH MASCULINIZATION OF FEMALE FISH  

EPA Science Inventory

In Vitro Androgenic Activity of Kraft Mill Effluent is Associated with Masculinization of Female Fish. Lambright, CS 1 , Parks, LG 1, Orlando, E 2, Guillette, LJ, Jr.2, Ankley, G 3, Gray, LE, Jr.1 , 1USEPA, NHEERL, RTP, NC, 2 University of Florida, Dept. of Zoology, Gainesville ...

165

In Vitro Activities of Eight Antifungal Drugs against 104 Environmental and Clinical Isolates of Aureobasidium pullulans  

PubMed Central

Aureobasidium pullulans is an unusual agent of phaeohyphomycosis. The in vitro activities of antifungals against 104 isolates of Aureobasidium pullulans var. pullulans and A. pullulans var. melanigenum revealed low MIC90s of amphotericin B, posaconazole, and itraconazole. However, they were resistant to fluconazole (?64 ?g/ml) and had high MICs of voriconazole, isavuconazole, caspofungin, and micafungin. PMID:25001309

Najafzadeh, M. Javad; Sutton, Deanna A.; Keisari, M. Saradeghi; Zarrinfar, H.; de Hoog, G. Sybren; Chowdhary, Anuradha

2014-01-01

166

In vitro activities of eight antifungal drugs against 104 environmental and clinical isolates of Aureobasidium pullulans.  

PubMed

Aureobasidium pullulans is an unusual agent of phaeohyphomycosis. The in vitro activities of antifungals against 104 isolates of Aureobasidium pullulans var. pullulans and A. pullulans var. melanigenum revealed low MIC90s of amphotericin B, posaconazole, and itraconazole. However, they were resistant to fluconazole (?64 ?g/ml) and had high MICs of voriconazole, isavuconazole, caspofungin, and micafungin. PMID:25001309

Najafzadeh, M Javad; Sutton, Deanna A; Keisari, M Saradeghi; Zarrinfar, H; de Hoog, G Sybren; Chowdhary, Anuradha; Meis, Jacques F

2014-09-01

167

In vitro Activity of Moxalactam against Pathogenic Bacteria and Its Comparison with Other Antibiotics  

Microsoft Academic Search

843 isolates from clinical specimens were tested against moxalactam by disc agar diffusion. The bacteria used in this study consisted of Escherichia coli, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Klebsiella pneumoniae, Proteus mirabilis, Providencia rettgeri, Pseudomonas aeruginosa, Serratia marcescens, Staphylococcus aureus, Staphylococcus epidermidis and group B and group D Streptococci. In vitro activity of moxalactam was compared with the following

Fred Perrymann; D. J. Flournoy; Hussain Qadri

1983-01-01

168

In vitro metabolism and bioavailability tests for the predictive toxicology of endocrine active substances  

EPA Science Inventory

Legislation and prospective legislative proposals internationally (may) require that chemicals are tested for their ability to disrupt the hormonal systems of animals. Chemicals found to test positive in vitro are considered to be endocrine active substances (EAS) and may be puta...

169

Effect of Proton Pump Inhibitors on In Vitro Activity of Tigecycline against Several Common Clinical Pathogens  

PubMed Central

In this study, we evaluated the effect of proton pump inhibitors (PPIs) on in vitro antimicrobial activity of tigecycline against several species of clinical pathogens. Clinical non-duplicate isolates of Acinetobacter baumannii, Staphylococcus aureus, Enterococcus faecalis and three species of Enterobacteriaceae (Escherichia coli, Klebsiella pneumonia and Enterobacter cloacae) were collected from a tertiary hospital and their MICs of tigecycline alone and in combination with PPIs (omeprazole, lansoprazole and pantoprazole) were determined. With one randomly selected isolate of each bacterial species, an in vitro time–kill study was performed for the confirmation of the effect of PPIs on tigecycline activity. The MIC changes after PPIs addition correlated with the PPIs concentrations in the test media. Compared with tigecycline alone, the addition of 5 mg/L PPIs could increase the MICs of tigecycline by 0 to 2-fold and the addition of 50 mg/L PPIs could increase the MICs of tigecycline by 4 to >128-fold. The time–kill study confirmed that the addition of PPIs could affect the in vitro activity of tigecycline. Even at low concentration (5 mg/L) of omeprazole and pantoprazole, antagonistic effect could be observed in E. cloacae and E. faecalis strains. We conclude that In vitro activity of tigecycline can be influenced by the presence of PPIs in a concentration-dependent manner. PMID:24466210

Ni, Wentao; Cai, Xuejiu; Liang, Beibei; Cai, Yun; Cui, Junchang; Wang, Rui

2014-01-01

170

In Vitro and In Vivo Cytotoxicities and Antileishmanial Activities of Thymol and Hemisynthetic Derivatives  

PubMed Central

The in vitro and in vivo antileishmanial and cytotoxic activities of thymol and structural derivatives in comparison to those of Glucantime were studied. The results showed here suggest that thymol and hemisynthetic derivatives have promising antileishmanial potential and could be considered as new lead structures in the search for novel antileishmanial drugs. PMID:15793164

Robledo, Sara; Osorio, Edison; Muńoz, Diana; Jaramillo, Luz Marina; Restrepo, Adriana; Arango, Gabriel; Vélez, Iván

2005-01-01

171

Glutathione S-Transferases Interact with AMP-Activated Protein Kinase: Evidence for S-Glutathionylation and Activation In Vitro  

PubMed Central

AMP-activated protein kinase (AMPK) is a cellular and whole body energy sensor with manifold functions in regulating energy homeostasis, cell morphology and proliferation in health and disease. Here we apply multiple, complementary in vitro and in vivo interaction assays to identify several isoforms of glutathione S-transferase (GST) as direct AMPK binding partners: Pi-family member rat GSTP1 and Mu-family members rat GSTM1, as well as Schistosoma japonicum GST. GST/AMPK interaction is direct and involves the N-terminal domain of the AMPK ?-subunit. Complex formation of the mammalian GSTP1 and -M1 with AMPK leads to their enzymatic activation and in turn facilitates glutathionylation and activation of AMPK in vitro. GST-facilitated S-glutathionylation of AMPK may be involved in rapid, full activation of the kinase under mildly oxidative physiological conditions. PMID:23741294

Polge, Cécile; Ramirez, Sacnicte; Michelland, Sylvie; Sčve, Michel; Vertommen, Didier; Rider, Mark; Lentze, Nicolas; Auerbach, Daniel; Schlattner, Uwe

2013-01-01

172

Relaxant activity of raspberry (Rubus idaeus) leaf extract in guinea-pig ileum in vitro.  

PubMed

Tea made from the leaves of Rubus idaeus L. (raspberry) has been used for centuries as a folk medicine to treat wounds, diarrhoea, colic pain and as a uterine relaxant. Extracts of dried raspberry leaves prepared with different solvents, (n-hexane, ethyl acetate, chloroform and methanol) were tested in vitro for relaxant activity on transmurally stimulated guinea-pig ileum. The methanol (MeOH) extract exhibited the largest response and also indicated that the active compounds are of a relatively polar nature. Hence the bulk of the leaves were extracted with methanol and the dried extract fractionated on a silica gel column, eluting with chloroform, mixtures of chloroform and methanol and finally methanol. Each fraction was examined by thin layer chromatography and tested for relaxant activity in an in vitro transmurally stimulated guinea-pig ileum preparation. The fractions eluted with chloroform (CHCl(3)) lacked relaxant activity. Samples eluted with CHCl(3)/MeOH (95:5) had moderate relaxant activity, while a second distinctive peak of activity eluted with a more polar solvent mixture (CHCl(3)/MeOH 50:50) provided strong dose dependent responses. Evidence was obtained that there are at least two components of raspberry leaf extract which exhibit relaxant activity in an in vitro gastrointestinal preparation. PMID:12410549

Rojas-Vera, Janne; Patel, Asmita V; Dacke, Christopher G

2002-11-01

173

In Vitro Larvicidal and Antioxidant Activity of Dihydrophenanthroline-3-carbonitriles  

PubMed Central

Many naturally occurring and synthetic compounds containing dihydrocyanopyridine and cyanopyran moiety show pharmacological properties. The aim of this study is to investigate the larvicidal and antioxidant potential of dihydrophenanthroline-3-carbonitrile derivatives 4a–f. A novel series of 2-amino-10-chloro-4,12-diphenyl-1,4,5,6-tetrahydrobenzo[j][1,7]phenanthroline-3-carbonitrile derivatives were synthesized by reacting different substituted acridine chalcones through Michel addition. The compounds were synthesized in excellent yields and the structures were corroborated on the basis of FT-IR, 1H NMR, 13C NMR, and ESI Mass analysis data. All the synthesized compounds were evaluated for larvicidal activity against Aedes aegypti and Culex quinquefasciatus larvae. Furthermore, the antioxidant activity was studied by the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay method. From the antioxidant assay, the compound 4c was reported with profound antioxidant potential. PMID:24868553

Bharathi, A.; Rahuman, Abdul Abdul; Rajakumar, Govindasamy

2014-01-01

174

The erlanger silver catheter: In vitro results for antimicrobial activity  

Microsoft Academic Search

Summary  The antimicrobial activity of a silver-impregnated polymer catheter (the Erlanger silver catheter) was demonstrated by determining\\u000a the microbial adhesion to the surface of the catheter and by measuring the rate of proliferation (viability) of microorganisms\\u000a at this site. On the surface of a catheter impregnated with silver, according to previously described methods, the bacterial\\u000a adhesion ofStaphylococcus epidermidis is reduced by

T. Bechert; M. Böswald; S. Lugauer; A. Regenfus; J. Greil; J.-P. Guggenbichler

1999-01-01

175

In vitro antioxidant and antiproliferative activities of nine Salvia species.  

PubMed

Supported by a growing increase of scientific research attesting the health properties of salvia species, we have decided to investigate nine Salvia namely Salvia sclarea, Salvia atropatana, Salvia sahendica, Salvia hydrangea, Salvia xanthocheila, Salvia macrosiphon, Salvia glutinosa, Salvia chloroleuca and Salvia ceratophylla species for their antioxidant and antiproliferative activities. In order to correlate the bioactivity with their phytochemical content, the total phenol and total flavonoid contents were also determined. S. ceratophylla exhibited the strongest activity against C32 cells with an IC50 value of 20.8 ?g mL(- 1), while S. glutinosa exhibited an IC50 value of 29.5 ?g mL(- 1) against ACHN cell line. Interestingly, S. glutinosa displayed also the highest DPPH radical-scavenging activity with an IC50 of 3.2 ?g mL(- 1). These species are characterised by the highest total phenol and flavonoid contents. The obtained results suggest that Salvia species are healthy plant foods. PMID:25039830

Loizzo, Monica Rosa; Abouali, Morteza; Salehi, Peyman; Sonboli, Ali; Kanani, Mohammad; Menichini, Francesco; Tundis, Rosa

2014-01-01

176

In vitro antimicrobial activity of Persian shallot (Allium hirtifolium).  

PubMed

Allium hirtifolium is a Persian native plant grown in cool mountain slopes of Iran. It has been used as a spice in Iran for many years. According to the literature review, there are no considerable reports on the antimicrobial properties of this plant. In this study, the antimicrobial activity of Persian shallot hydroalcoholic extract and F1 fraction of the plant (containing amino acid derivatives and/or other cationic compounds) was investigated on some Gram positive cocci and bacilli, Gram negative bacilli, two protozoa, a yeast and a fungus. Excellent activity against Candida albicans (MIC = 64 microg/ml, MBC = 128 microg/ml), Leishmania infantum (MIC = 0.2 mg/ml on the first day of study) and Trichomonas vaginalis (MIC = 5 microg/ml in PSDE form) and a moderate activity against Bacillus spp and Pseudomonas aeroginosa (MIC = 128 microg/ml) was observed. The results showed that this plant contains some anti-trichomonas and anti-leishmania components. PMID:23210319

Soroush, Setareh; Taherikalani, Morovat; Asadollahi, Parisa; Asadollahi, Khairollah; Taran, Mojtaba; Emaneini, Mohammad; Alizadeh, Sajjad

2012-01-01

177

Anthelmintic activity of cyclotides: In vitro studies with canine and human hookworms.  

PubMed

Hookworm infection is a leading cause of maternal and child morbidity in countries of the tropics and subtropics, as well as being an important parasite in companion-animal medicine. The cyclotides are a novel family of cyclic cystine knot containing peptides from plants that have been shown to possess anthelmintic activity against Haemonchus contortus and Trichostrongylus colubriformis, two important gastrointestinal nematodes of sheep. In the current study we demonstrated the in vitro effects of three representative cyclotides, kalata B1, kalata B6 and cycloviolacin O14, on the viability of larval and adult life stages of the dog hookworm Ancylostoma caninum, and larvae of the human hookworm Necator americanus. The cyclotides showed significant anthelmintic activity towards both hookworm species. The different cyclotides showed similar patterns of relative activity as that seen previously with the livestock nematode species. This study demonstrates that cyclotides have promising activity in vitro against important parasites of companion animals and humans. PMID:19059189

Colgrave, Michelle L; Kotze, Andrew C; Kopp, Steven; McCarthy, James S; Coleman, Glen T; Craik, David J

2009-02-01

178

Synthesis of novel substituted 1,3-diaryl propenone derivatives and their antimalarial activity in vitro.  

PubMed

The synthesis of novel 1,3-diaryl propenone derivatives and their antimalarial activity in vitro against asexual blood stages of human malaria parasite, Plasmodium falciparum, are described. Chalcone derivatives were prepared via Claisen-Schmidt condensation of substituted aldehydes with substituted methyl ketones. Antiplasmodial IC(50) (half maximal inhibitory concentration) activity of these compounds ranged between 1.5 and 12.3 microg/ml. The chloro-series, 1,2,4-triazole substituted chalcone was found to be the most effective in inhibiting the growth of P. falciparum in vitro while pyrrole and benzotriazole substituted chalcones showed relatively less inhibitory activity. This is the first report on antiplasmodial activity of chalcones with azoles on acetophenone ring. PMID:17977622

Mishra, Nidhi; Arora, Preeti; Kumar, Brajesh; Mishra, Lokesh C; Bhattacharya, Amit; Awasthi, Satish K; Bhasin, Virendra K

2008-07-01

179

In Vitro Activity of TR700, the Active Ingredient of the Antibacterial Prodrug TR701, against Linezolid-Resistant Strains  

Microsoft Academic Search

TR-701 is the orally active prodrug of TR-700, a novel oxazolidinone that demonstrates four- to eightfold- greater activity than linezolid (LZD) against Staphylococcus and Enterococcus spp. In this study evaluating the in vitro sensitivity of LZD-resistant isolates, TR-700 demonstrated 8- to 16-fold-greater potency than LZD against all strains tested, including methicillin-resistant Staphylococcus aureus (MRSA), strains of MRSA carrying the mobile

K. J. Shaw; S. Poppe; R. Schaadt; V. Brown-Driver; J. Finn; C. M. Pillar; D. Shinabarger; G. Zurenko

2008-01-01

180

In Vitro Activities of Tritrpticin Alone and in Combination with Other Antimicrobial Agents against Pseudomonas aeruginosa?  

PubMed Central

The in vitro activity of the cathelicidin tritrpticin was investigated against multidrug-resistant Pseudomonas aeruginosa. The isolates were susceptible to the peptide at concentrations of 0.50 to 8 mg/liter. Tritrpticin completely inhibits lipopolysaccharide procoagulant activity at a 10 ?M concentration. Fractionary inhibitory concentration indexes (0.385, 0.312, and 0.458) demonstrated synergy between the peptide and ?-lactams. PMID:16940073

Cirioni, Oscar?; Giacometti, Andrea; Silvestri, Carmela; Della Vittoria, Agnese; Licci, Alberto; Riva, Alessandra; Scalise, Giorgio

2006-01-01

181

Synthesis and in vitro biological activity of retinyl polyhydroxybenzoates, novel hybrid retinoid derivatives  

Microsoft Academic Search

A new hybrid derived from retinol was designed to improve the stability and anti-oxidant activity of retinol and also to add whitening properties besides its usual anti-aging properties. A variety of polyhydroxybenzoates of retinol were prepared either by base-catalysis or by direct esterification of retinol and screened for such desirable properties by analyzing the in vitro biological activity of the

Sungbum Kim; Youngmin Kim; Younggyu Kong; Hyojung Kim; Jahyo Kang

2009-01-01

182

Synthesis and in vitro antileukemic activity of new 4-triazenopyrazole derivatives  

Microsoft Academic Search

Several new 4-(3,3-dimethyltriazeno)-5-benzamidopyrazole derivatives were prepared by reacting 4-diazo-5-benzamidopyrazole derivatives with dimethylamine. The compounds were tested at 10 ?M for their vitro antileukemic activity against K562 (Human chronic myelogenous leukemia) and Raji (human Burkitt limphoma ) cell lines. Dacarbazine and methotrexate were used for comparative purpose. The 3-methyl-4-(3,3-dimethyltriazeno)-5-(substituted benzamido)pyrazoles, bearing the pyrazole nucleus free at 1 position, resulted more active than the 1-(substituted

Giuseppe Daidone; Benedetta Maggio; Demetrio Raffa; Salvatore Plescia; Domenico Schillaci; Maria Valeria Raimondi

2004-01-01

183

Synthesis of novel substituted 1,3-diaryl propenone derivatives and their antimalarial activity in vitro  

Microsoft Academic Search

The synthesis of novel 1,3-diaryl propenone derivatives and their antimalarial activity in vitro against asexual blood stages of human malaria parasite, Plasmodium falciparum, are described. Chalcone derivatives were prepared via Claisen–Schmidt condensation of substituted aldehydes with substituted methyl ketones. Antiplasmodial IC50 (half maximal inhibitory concentration) activity of these compounds ranged between 1.5 and 12.3?g\\/ml. The chloro-series, 1,2,4-triazole substituted chalcone was

Nidhi Mishra; Preeti Arora; Brajesh Kumar; Lokesh C. Mishra; Amit Bhattacharya; Satish K. Awasthi; Virendra K. Bhasin

2008-01-01

184

Antiangiogenic Activity of Sterically Stabilized Liposomes Containing Paclitaxel (SSL-PTX): In Vitro and In Vivo  

Microsoft Academic Search

The purpose of this present study was to evaluate the antiangiogenic activity of sterically stabilized liposomes containing\\u000a paclitaxel (SSL-PTX). The SSL-PTX was prepared by the thin-film method. The release of paclitaxel from SSL-PTX was analyzed\\u000a using a dialysis method. The effect of SSL-PTX on endothelial cell proliferation and migration was investigated in vitro. The antitumor and antiangiogenic activity of SSL-PTX

Yue Huang; Xiao-Mei Chen; Bing-Xiang Zhao; Xi-Yu Ke; Bo-Jun Zhao; Xin Zhao; Ying Wang; Xuan Zhang; Qiang Zhang

2010-01-01

185

In vitro screening of two Nigerian medicinal plants ( Vernonia amygdalina and Annona senegalensis) for anthelmintic activity  

Microsoft Academic Search

Vernonia amygdalina and Annona senegalensis, two plants used by local\\/smallholder livestock farmers in Nigeria as anthelmintic were screened for in vitro anthelmintic activity using Haemonchus contortus eggs. The extract of V. amygdalina did not show any significant activity at concentrations up to 11.2mg\\/ml. The extract of A. senegalensis showed significant (P<0.001) reduction in egg hatch at a concentration of 7.1mg\\/ml.

C. B. I Alawa; A. M Adamu; J. O Gefu; O. J Ajanusi; P. A Abdu; N. P Chiezey; J. N Alawa; D. D Bowman

2003-01-01

186

In vitro extracellular and intracellular activity of two newer and two earlier fluoroquinolones against Listeria monocytogenes  

Microsoft Academic Search

Two new fluoroquinolones (trovafloxacin and sparfloxacin) with enhanced activity against gram-positive pathogens and two earlier compounds (ciprofloxacin and ofloxacin) were tested for their in vitro inhibitory and bactericidal activity against 80 strains ofListeria monocytogenes. All strains were uniformly highly susceptible to trovafloxacin, the MIC90 being 0.25 mg\\/l. Resistance to sparfloxacin was not detected, however the MIC90 of sparfloxacin was eight

B. Facinelli; G. Magi; M. Prenna; S. Ripa; P. E. Varaldo

1997-01-01

187

Similar activity of mecamylamine stereoisomers in vitro and in vivo  

PubMed Central

A previous characterization of mecamylamine stereoisomers using nicotinic acetylcholine receptors expressed in Xenopus oocytes revealed only small differences between the activity of the R and S forms of mecamylamine. However, that work was limited in the breadth of receptor subtypes tested, especially in regard to the discrimination of high and low sensitivity receptors, which differ in the ratios of alpha and beta subunits. We report new data using subunit concatamers, which produce uniform populations of high-sensitivity or low-sensitivity receptors, as well as alpha2, alpha5, and alpha6-containing receptors, which were not studied previously. Consistent with previous studies, we found that beta4-containing receptors were most sensitive to mecamylamine and that the IC50 values for the inhibition of net charge were lower than for inhibition of peak currents. No large differences were seen between the activities of the mecamylamine isomers. Additionally, a previously reported potentiation of high-sensitivity ?4?2 receptors by S-mecamylamine could not be reproduced in the oocyte system, even with mutants that had greatly reduced sensitivity to mecamylamine inhibition or when the selective agonist TC-2559 was used. In vivo studies suggested that the R-isomer might be somewhat more potent than the S isomer at blocking CNS effects of nicotine. Although the potency difference was no more than a factor of two, it is consistent with lower LD50 estimates previously reported for the R isomer. Our results significantly extend knowledge of the nicotinic acetylcholine receptor activity profile of mecamylamine and support the hypothesis that these effects are not strongly stereoisomer selective. PMID:24161916

Papke, Roger L.; Stokes, Clare; Muldoon, Pretal; Damaj, M. Imad

2014-01-01

188

Antagonistic Activity of Lactobacillus Isolates against Salmonella typhi In Vitro  

PubMed Central

Background. Enteric fever is a global health problem, and rapidly developing resistance to various drugs makes the situation more alarming. The potential use of Lactobacillus to control typhoid fever represents a promising approach, as it may exert protective actions through various mechanisms. Methods. In this study, the probiotic potential and antagonistic activities of 32 Lactobacillus isolates against Salmonella typhi were evaluated. The antimicrobial activity of cell free supernatants of Lactobacillus isolates, interference of Lactobacillus isolates with the Salmonella adherence and invasion, cytoprotective effect of Lactobacillus isolates, and possibility of concurrent use of tested Lactobacillus isolates and antibiotics were evaluated by testing their susceptibilities to antimicrobial agents, and their oxygen tolerance was also examined. Results. The results revealed that twelve Lactobacillus isolates could protect against Salmonella typhi infection through interference with both its growth and its virulence properties, such as adherence, invasion, and cytotoxicity. These Lactobacillus isolates exhibited MIC values for ciprofloxacin higher than those of Salmonella typhi and oxygen tolerance and were identified as Lactobacillus plantarum. Conclusion. The tested Lactobacillus plantarum isolates can be introduced as potential novel candidates that have to be subjected for in vivo and application studies for treatment and control of typhoid fever. PMID:24191248

Abdel-Daim, Amira; Hassouna, Nadia; Hafez, Mohamed; Ashor, Mohamed Seif Aldeen; Aboulwafa, Mohammad M.

2013-01-01

189

Lack of activity of cadmium in in vitro estrogenicity assays  

SciTech Connect

Prompted by reports about strong estrogenic effects of cadmium, attempts were made to reproduce these observations using the yeast estrogen screen (YES) and the E-Screen assays. For the first time, possible activation of the Src/MAPK pathway was also investigated. In the YES, only a slight activation (10% of a maximal effect) of the estrogen receptor alpha (ER{alpha}) was observed at cadmium concentrations between 5 x 10{sup -7} M and 5 x 10{sup -6} M. In the E-Screen assay, carried out by two laboratories, the heavy metal was without observable cell proliferative effects when tested in the range between 6 x 10{sup -11} M and 1 x 10{sup -5} M. However, in both assays, cadmium led to a reduction of the effects of 17{beta}-estradiol (E2). Treatment of MCF-7 human breast cancer cells with 1 x 10{sup -7} M cadmium failed to induce phosphorylation of Src and the MAP kinases Erk1 and Erk2-effects shown to occur with E2 and epidermal growth factor (EGF). In summary, we were unable to confirm the strong estrogenicity of cadmium reported recently by a number of laboratories. This apparent absence of effects in our hands is not due to a lack of uptake of the metal or to effective protection against cadmium by high levels of glutathione or metallothionein, since toxicity and an antagonism of E2 responses were observed both in the YES and the E-Screen.

Silva, Elisabete [Centre for Toxicology, School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX (United Kingdom)]. E-mail: elisabete.silva@pharmacy.ac.uk; Lopez-Espinosa, Maria Jose [School of Medicine, Hospital Clinico, University of Granada, 18071-Granada (Spain); Molina-Molina, Jose-Manuel [School of Medicine, Hospital Clinico, University of Granada, 18071-Granada (Spain); Fernandez, Marieta [School of Medicine, Hospital Clinico, University of Granada, 18071-Granada (Spain); Olea, Nicolas [School of Medicine, Hospital Clinico, University of Granada, 18071-Granada (Spain); Kortenkamp, Andreas [Centre for Toxicology, School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX (United Kingdom)

2006-10-01

190

Spontaneous Electrical Activity in the Human Fetal Cortex in vitro  

PubMed Central

Our knowledge about the developing human cerebral cortex is based on the analysis of fixed postmortem material. Here we utilize electrical recordings from unfixed human postmortem tissue to characterize the synaptic physiology and spontaneous network activity of pioneer cortical neurons (“subplate neurons”). Our electrophysiological experiments show that functional glutamate or GABA ionotropic receptors are expressed on human subplate (SP) neurons as early as 20 gestational weeks. Extracellular (synaptic) stimulations evoked postsynaptic potentials in a very small fraction of SP neurons, suggesting that functional synaptic contacts are rare at mid-gestation. Although synaptic inputs were scarce, we regularly observed spontaneous (unprovoked) electrical activity among human SP neurons, comprised of sustained plateau depolarizations and bursts of action potential firing, which resembled cortical UP and DOWN states in the adult neocortex. Plateau depolarizations and bursts of AP firing are thought to depend on the mature morphology and physiology of adult cortical network. However, our current data reveal that similar cortical rhythm is generated by a very immature ensemble of human fetal neurons. In the relative absence of sensory inputs, as in development in utero, or in slow wave sleep (i.e. throughout the entire lifespan), the spontaneous slow oscillatory pattern (UP and DOWN states) is a fundamental aspect of human cortical physiology. PMID:21325506

Moore, Anna R.; Zhou, Wen-Liang; Jakovcevski, Igor; Zecevic, Nada; Antic, Srdjan D.

2011-01-01

191

In vitro antimicrobial activity and biocompatibility of propolis containing nanohydroxyapatite.  

PubMed

The high number of biomaterial associated infections demands new strategies to prevent this problem. In this study the suitability of nanohydroxyapatite (nanoHA)-based surfaces containing two Brazilian extracts of propolis (green and red ones) to prevent bacterial growth and biofilm formation, as well as its non-cytotoxic nature, was investigated. Optical density, colony forming units and MTT reduction assay were used to assess the materials' antibacterial activity against planktonic and sessile growth of Staphylococcus aureus. NanoHA matrix was able to absorb both types of propolis and the obtained results revealed the antibacterial effectiveness of the novel materials expressed as the reduction of bacterial growth and biofilm formation ability. Additionally, cell culture tests showed the growth of fibroblasts with high metabolic activity and without membrane damage. Therefore, these nanoHA-based surfaces containing natural products deriving from bees may be a promising bioactive biomaterial to be further studied with the aim of application to orthopaedic or dental devices. PMID:25784672

Grenho, L; Barros, J; Ferreira, C; Santos, V R; Monteiro, F J; Ferraz, M P; Cortes, M E

2015-01-01

192

In Vitro Activity of Ceftaroline against 623 Diverse Strains of Anaerobic Bacteria ?  

PubMed Central

The in vitro activities of ceftaroline, a novel, parenteral, broad-spectrum cephalosporin, and four comparator antimicrobials were determined against anaerobic bacteria. Against Gram-positive strains, the activity of ceftaroline was similar to that of amoxicillin-clavulanate and four to eight times greater than that of ceftriaxone. Against Gram-negative organisms, ceftaroline showed good activity against ?-lactamase-negative strains but not against the members of the Bacteroides fragilis group. Ceftaroline showed potent activity against a broad spectrum of anaerobes encountered in respiratory, skin, and soft tissue infections. PMID:20100877

Citron, D. M.; Tyrrell, K. L.; Merriam, C. V.; Goldstein, E. J. C.

2010-01-01

193

In vitro and in vivo immunomodulatory activity of sulfated polysaccharides from red seaweed Nemalion helminthoides.  

PubMed

Water-soluble sulfated polysaccharides from the red seaweed Nemalion helminthoides: two xylomannan fractions (N3 and N4) and a mannan fraction (N6) were investigated to determine their in vitro and in vivo immunomodulatory activities. N3 and N4 induced in vitro proliferation of macrophages of the murine cell line RAW 264.7 and significantly stimulated the production of nitric oxide (NO) and cytokines (IL-6 and TNF-?) in the same cells, whereas this response was not observed with the mannan N6. The cytokine production was also stimulated by sulfated xylomannans in vivo in BALB/c mice inoculated intravenously with these polysaccharides. Remarkably, when mice were treated with N3 and N4 for 1 h before being infected with Herpes simplex virus type 2, they remained asymptomatic with no signs of disease. The in vitro and in vivo results suggest that sulfated xylomannans could be strong immunomodulators. PMID:24444887

Pérez-Recalde, Mercedes; Matulewicz, María C; Pujol, Carlos A; Carlucci, María J

2014-02-01

194

Neuromuscular activity of Micrurus laticollaris (Squamata: Elapidae) venom in vitro.  

PubMed

In this work, we have examined the neuromuscular activity of Micrurus laticollaris (Mexican coral snake) venom (MLV) in vertebrate isolated nerve-muscle preparations. In chick biventer cervicis preparations, the MLV induced an irreversible concentration- and time-dependent (1-30 µg/mL) neuromuscular blockade, with 50% blockade occurring between 8 and 30 min. Muscle contractures evoked by exogenous acetylcholine were completely abolished by MLV, whereas those of KCl were also significantly altered (86% ± 11%, 53% ± 11%, 89% ± 5% and 89% ± 7% for one, three, 10 and 30 µg of venom/mL, respectively; n = 4; p < 0.05). In mouse phrenic nerve-diaphragm preparations, MLV (1-10 µg/mL) promoted a slight increase in the amplitude of twitch-tension (3 µg/mL), followed by neuromuscular blockade (n = 4); the highest concentration caused complete inhibition of the twitches (time for 50% blockade = 26 ± 3 min), without exhibiting a previous neuromuscular facilitation. The venom (3 µg/mL) induced a biphasic modulation in the frequency of miniature end-plate potentials (MEPPs)/min, causing a significant increase after 15 min, followed by a decrease after 60 min (from 17 ± 1.4 (basal) to 28 ± 2.5 (t15) and 12 ± 2 (t60)). The membrane resting potential of mouse diaphragm preparations pre-exposed or not to d-tubocurarine (5 µg/mL) was also significantly less negative with MLV (10 µg/mL). Together, these results indicate that M. laticollaris venom induces neuromuscular blockade by a combination of pre- and post-synaptic activities. PMID:24445448

Carbajal-Saucedo, Alejandro; Floriano, Rafael Stuani; Dal Belo, Cháriston André; Olvera-Rodríguez, Alejandro; Alagón, Alejandro; Rodrigues-Simioni, Léa

2014-01-01

195

Neuromuscular Activity of Micrurus laticollaris (Squamata: Elapidae) Venom in Vitro  

PubMed Central

In this work, we have examined the neuromuscular activity of Micrurus laticollaris (Mexican coral snake) venom (MLV) in vertebrate isolated nerve-muscle preparations. In chick biventer cervicis preparations, the MLV induced an irreversible concentration- and time-dependent (1–30 µg/mL) neuromuscular blockade, with 50% blockade occurring between 8 and 30 min. Muscle contractures evoked by exogenous acetylcholine were completely abolished by MLV, whereas those of KCl were also significantly altered (86% ± 11%, 53% ± 11%, 89% ± 5% and 89% ± 7% for one, three, 10 and 30 µg of venom/mL, respectively; n = 4; p < 0.05). In mouse phrenic nerve-diaphragm preparations, MLV (1–10 µg/mL) promoted a slight increase in the amplitude of twitch-tension (3 µg/mL), followed by neuromuscular blockade (n = 4); the highest concentration caused complete inhibition of the twitches (time for 50% blockade = 26 ± 3 min), without exhibiting a previous neuromuscular facilitation. The venom (3 µg/mL) induced a biphasic modulation in the frequency of miniature end-plate potentials (MEPPs)/min, causing a significant increase after 15 min, followed by a decrease after 60 min (from 17 ± 1.4 (basal) to 28 ± 2.5 (t15) and 12 ± 2 (t60)). The membrane resting potential of mouse diaphragm preparations pre-exposed or not to d-tubocurarine (5 µg/mL) was also significantly less negative with MLV (10 µg/mL). Together, these results indicate that M. laticollaris venom induces neuromuscular blockade by a combination of pre- and post-synaptic activities. PMID:24445448

Carbajal-Saucedo, Alejandro; Floriano, Rafael Stuani; Dal Belo, Cháriston André; Olvera-Rodríguez, Alejandro; Alagón, Alejandro; Rodrigues-Simioni, Léa

2014-01-01

196

Progress of in vitro factor VIII coagulant activity from 0 to 8 hours after reconstitution  

PubMed Central

Background Continuous infusion of factor VIII (FVIII) is a more cost-effective method for treating hemophilia A than intermittent bolus injection. However, there is currently no specific data in Korea about the progress of in vitro FVIII coagulant activity (FVIII:C) after reconstitution from its lyophilized form. Methods Three commercial FVIII concentrate products (two recombinant FVIII and one plasma-derived) were used. In vitro FVIII:C was measured at 0, 2, 4, 6, and 8 hours following reconstitution in both the indoor light-exposed and light-shielded groups. Results For the three drugs, in vitro FVIII:C decreased over the 8 hours following reconstitution (P<0.001). The decline of FVIII:C was linear (P<0.001). In vitro FVIII:C for the indoor light-exposed groups was 95.3±1.9% and 90.6±2.5% after 4 and 8 hours following reconstitution, respectively, compared to baseline activity. In the light-shielded group, FVIII:C was 95.4±1.1% and 90.9±1.7% of the baseline activity after 4 and 8 hours, respectively. There was no statistical difference between FVIII:C in the indoor light-exposed and light-shielded groups (P=0.849). Conclusion In vitro FVIII:C decreased after reconstitution, but activity was maintained at over 90% of the baseline value during 8 hours. Exposure to indoor light did not accelerate the loss of FVIII:C over the experimental time. This result indicates that CI with FVIII is available in 8-hour intervals, with no indoor light-exposure precautions needed. PMID:25548761

Shim, Ye Jee; Lee, Kun Soo; Kim, Uk Hyun; Suh, Jin Kyung; Baik, Sae Yun

2014-01-01

197

Relationship between in vivo activity and in vitro measures of function and stability of a protein  

SciTech Connect

The in vivo activities of mutant proteins are readily measured and can potentially be used to estimate changes in in vitro properties such as stability or function, but this connection has not been rigorously established. Gene V protein is a small protein produced by bacteriophage f1 that binds to single-stranded DNA and to RNA and for which fitness can be assayed both in vivo and in vitro. We have assembled a large number of temperature-sensitive mutants of the gene V protein of bacteriophage f1 and measured their ability to support phage growth and replication in vivo. We have also purified many of these mutant gene V proteins and measured their stabilities and ssDNA binding affinities in vitro. Mutations at surface residues frequently yielded temperature-sensitive mutants, but remarkably, no overall correlation between in vivo activity and in vitro measures of either stability or function was found for this group. Mutations at buried residues often lead to the temperature-sensitive phenotype. At buried sites temperature sensitivity was strongly correlated with in vitro stability changes, but not with in vitro ssDNA binding affinity. The implication of these observations for protein engineering efforts is that phenotypes conferred by amino acid substitutions at buried sites can be used to identify mutants whose stabilities fall into ranges of interest, while phenotypes of mutants with surface substitutions may be much less readily interpreted, even in the case of a single-stranded-DNA-binding protein. 54 refs., 3 figs., 2 tabs.

Sandberg, W.S.; Schlunk, P.M.; Zabin, H.G. [Univ. of Chicago, IL (United States)] [and others

1995-09-19

198

In vitro - in vivo correlations for endocrine activity of a mixture of currently used pesticides  

SciTech Connect

Two pesticide mixtures were investigated for potential endocrine activity. Mix 3 consisted of bitertanol, propiconazole, and cypermethrin, and Mix 5 included malathion and terbuthylazine in addition to the three pesticides in Mix 3. All five single pesticides and the two mixtures were investigated for their ability to affect steroidogenesis in vitro in H295R cells. The pesticides alone and both mixtures affected steroidogenesis with both mixtures causing increase in progesterone and decrease in testosterone. For Mix 5 an increase in estradiol was seen as well, indicating increased aromatase activity. The two mixtures were also investigated in pregnant rats dosed from gestational day 7 to 21, followed by examination of dams and fetuses. Decreased estradiol and reduced placental testosterone were seen in dams exposed to Mix 5. Also a significant increase in aromatase mRNA-levels in female adrenal glands was found for Mix5. However, either of the two mixtures showed any effects on fetal hormone levels in plasma or testis, or on anogenital distance. Overall, potential aromatase induction was found for Mix 5 both in vitro and in vivo, but not for Mix 3, an effect likely owed to terbuthylazine in Mix 5. However, the hormonal responses in vitro were only partly reflected in vivo, probably due to some toxicokinetic issues, as the pesticide levels in the amniotic fluid also were found to be negatively affected by the number of compounds present in the mixtures. Nonetheless, the H295R assay gives hints on conceivable interference with steroidogenesis, thus generating hypotheses on in vivo effects. - Highlights: • The study examines the endocrine disrupting potential of mixtures of pesticides. • All single pesticides and both mixtures affected steroidogenesis in vitro. • Potential aromatase induction was found for Mix 5 both in vitro and in vivo. • The hormonal responses in vitro were only partly reflected in vivo.

Taxvig, Camilla, E-mail: camta@food.dtu.dk [Division of Toxicology and Risk Assessment, National Food Institute, Technical University of Denmark, Mřrkhřj Bygade 19, DK-2860 Sřborg (Denmark); Hadrup, Niels; Boberg, Julie; Axelstad, Marta [Division of Toxicology and Risk Assessment, National Food Institute, Technical University of Denmark, Mřrkhřj Bygade 19, DK-2860 Sřborg (Denmark); Bossi, Rossana [Department of Environmental Science, Aarhus University, DK-4000 Roskilde (Denmark); Bonefeld-Jřrgensen, Eva Cecilie [Department of Public Health, University of Aarhus, DK-8000 Aarhus C (Denmark); Vinggaard, Anne Marie [Division of Toxicology and Risk Assessment, National Food Institute, Technical University of Denmark, Mřrkhřj Bygade 19, DK-2860 Sřborg (Denmark)

2013-11-01

199

An in vitro and in vivo study of the ?-amylase activity of phaseolamin.  

PubMed

We evaluated the polypeptide profiles, inhibition of human salivary ?-amylase activity, and hemagglutination properties of a commercial phaseolamin sample. We also performed an in vivo assay to investigate the effects of a commercial phaseolamin treatment (100, 500, or 1500?mg/kg) over 20 days on the glycemia, body weight, and serum biochemical parameters (total cholesterol, triglycerides, alanine aminotransferase, and aspartate aminotransferase) of nondiabetic and streptozotocin-induced diabetic rats. The in vitro evaluation showed defined protein profiles, low hemagglutination activity, and high ?-amylase inhibition. None of the experimental groups treated with phaseolamin or acarbose showed decreases in body weight. Our data demonstrate that phaseolamin inhibits amylase activity in vitro, reduces blood glucose levels, decreases or attenuates some of the renal and hepatic effects of diabetes in streptozotocin-induced rats, and could therefore have therapeutic potential in the treatment or prevention of the complications of diabetes. PMID:24650210

de Gouveia, Neire Moura; Alves, Fernanda Vieira; Furtado, Fabiana Barcelos; Scherer, Danielli Luana; Mundim, Antonio Vicente; Espindola, Foued Salmen

2014-08-01

200

Acaricidal activity of extracts from Adonis coerulea Maxim. against Psoroptes cuniculi in vitro and in vivo.  

PubMed

The acaricidal activity of Adonis coerulea extracts was investigated against Psoroptes cuniculi. The aqueous, methanol, acetic ether and petroleum ether extracts all showed marked acaricidal activity in vitro. Especially, the acetic ether extract possessed strong toxicity against mites in vitro with LT50 values 0.743 h, 2.730 h, 5.919 h and 22.536 h at concentrations of 500, 250, 125 and 62.5 mg/ml, respectively. At the same time, the acetic ether extract showed the best effectiveness topically to infested rabbits in vivo. After three times treatment, at the day 20, rabbits treated with A. coerulea extract were observed only small scabs or secretions in ear canal, but no mites. These findings suggested that as a potential insecticide, A. coerulea should be studied further to develop active components or a new acaricidal drug. PMID:23352106

Shang, Xiao-Fei; Miao, Xiao-Lou; Wang, Dong-Sheng; Li, Jian-Xi; Wang, Xue-Zhi; Yan, Zuo-Ting; Wang, Chun-Mei; Wang, Yu; He, Xi-Rui; Pan, Hu

2013-07-01

201

In vitro antisickling activity of a rearranged limonoid isolated from Khaya senegalensis.  

PubMed

We previously observed that aqueous extracts of the stem bark and leaves of Khaya senegalensis exhibited a strong antisickling activity. These results prompted us to find out the constituent(s) responsible for these properties using an in vitro bio-guided fractionation. The bioassay was based on sickle cells countings, before and after deoxygenation, in blood samples taken from patients with severe sickle cell anemia and pre-incubated with the drugs to be tested. The main active constituent was identified as a rearranged limonoid whose structure was recently elucidated. In comparison with pentoxifylline used as standard, the in vitro antisickling activity of this limonoid was much higher at any concentrations and incubation conditions. In addition, it did not alter significantly the corpuscular indices. PMID:10232063

Fall, A B; Vanhaelen-Fastré, R; Vanhaelen, M; Lo, I; Toppet, M; Ferster, A; Fondu, P

1999-04-01

202

Gamma radiation effects on phenolics, antioxidants activity and in vitro digestion of pistachio ( Pistachia vera) hull  

NASA Astrophysics Data System (ADS)

The effect of gamma radiation (10, 20, 30, 40, 50 and 60 kGy) on tannin, total phenolics, antioxidants activity and in vitro digestion of pistachio hulls has been investigated in this study. The possibility of using the radial diffusion method based on software measurement of the rings area has also been investigated in this study. The software based method in radial diffusion method showed a higher r2 (0.995) value when compared to the traditional method. Irradiation reduced the tannin content ( P<0.01) and activity of antioxidants ( P<0.05) of pistachio hull extracts but increased the total phenolic content ( P<0.05). There was no effect of gamma irradiation on the in vitro digestion of the pistachio hull. Irradiation decreased the digestion rate of the pistachio hull at the dose of 40 kGy when compared to the control. This study showed that gamma irradiation decreased tannin and antioxidants activity of pistachio hull.

Behgar, M.; Ghasemi, S.; Naserian, A.; Borzoie, A.; Fatollahi, H.

2011-09-01

203

G17-modified hammerhead ribozymes are active in vitro and in vivo  

PubMed Central

Natural hammerhead ribozymes (HHRz) feature tertiary interactions between hairpin loops or bulges in two of three helices that surround the catalytic core of conserved nucleotides. Their conservation was originally established on minimal versions lacking the tertiary interactions. While those sequence requirements in general also apply to natural versions, we show here differences for the HHRz cleavage site N17. A guanosine at this position strongly impairs cleavage activity in minimal versions, whereas we observe for the G17 variants of four tertiary stabilized HHRz significant cleavage and ligation activity in vitro. Kinetic analyses of these variants revealed a reduced rate and extent of cleavage, compared with wild-type sequences, while variants with distorted tertiary interactions cleaved at a reduced rate, but to the same extent. Contrary to this, G17 variants exhibit similar in vitro ligation activity as compared with the respective wild-type motif. To also address the catalytic performance of these motifs in vivo, we have inserted HHRz cassettes in the lacZ gene and tested this ?-galactosidase reporter in Dictyostelium discoideum. In colorimetric assays, we observe differences in the enzymatic activity of ?-galactosidase, which correlate well with the activity of the different HHRz variants in vitro and which can be unambiguously attributed to ribozyme cleavage by primer extension analysis. PMID:24145822

Kalweit, Anne; Hammann, Christian

2013-01-01

204

Differential in vitro activities of ionophore compounds against Plasmodium falciparum and mammalian cells.  

PubMed Central

Twenty-two ionophore compounds were screened for their antimalarial activities. They consisted of true ionophores (mobile carriers) and channel-forming quasi-ionophores with different ionic specificities. Eleven of the compounds were found to be extremely efficient inhibitors of Plasmodium falciparum growth in vitro, with 50% inhibitory concentrations of less than 10 ng/ml. Gramicidin D was the most active compound tested, with 50% inhibitory concentration of 0.035 ng/ml. Compounds with identical ionic specificities generally had similar levels of antimalarial activity, and ionophores specific to monovalent cations were the most active. Compounds were further tested to determine their in vitro toxicities against mammalian lymphoblast and macrophage cell lines. Nine of the 22 compounds, i.e., alborixin, lonomycin, nigericin, narasin, monensin and its methylated derivative, lasalocid and its bromo derivative, and gramicidin D, most specific to monovalent cations, were at least 35-fold more active in vitro against P. falciparum than against the two other mammalian cell lines. The enhanced ability to penetrate the erythrocyte membrane after infection could be a factor that determines ionophore selectivity for infected erythrocytes. PMID:8851578

Gumila, C; Ancelin, M L; Jeminet, G; Delort, A M; Miquel, G; Vial, H J

1996-01-01

205

Antioxidant activity of glycoprotein purified from Undaria pinnatifida measured by an in vitro digestion model.  

PubMed

The present study was performed to investigate the chemical composition and antioxidant activity of glycoprotein purified from Undaria pinnatifida Harvey (UPGP). On SDS-PAGE, UPGP migrated as a single band with a molecular weight of approximately 10 kDa and confirmed by staining with Schiff's reagent as glycoprotein. It consists of a carbohydrate component (42.53%) and protein component (57.47%). Amino acid profile, FT-IR spectrum and enzymatic glycosylation analysis suggested that protein is linked with carbohydrate by O-glycosylation. UPGP showed dose-dependent antioxidant activities as detected by different assays before and after in vitro digestion. The IC50 values of undigested UPGP were 0.25 ± 0.03, 0.08 ± 0.005, 0.69 ± 0.12, and 0.25 ± 0.08 mg/mL for DPPH, ABTS, FRAP, and NO, respectively. Following in vitro digestion, the antioxidant activities of UPGP were decreased during the gastric phase compared to those of undigested UPGP, with an increase occurring during the duodenal phase in all assays. However, the reducing power was unchanged after in vitro digestion. Furthermore, UPGP showed protective activity against oxidative DNA damage both undigested, after saliva and duodenal phase of digestion. These results indicate that the antioxidant and DNA protection activities of UPGP may be pH-dependent and assay specific. PMID:24060280

Rafiquzzaman, S M; Kim, Eun-Young; Kim, Yu-Ri; Nam, Taek-Jeong; Kong, In-Soo

2013-11-01

206

In vitro activities of natural products against oral Candida isolates from denture wearers  

PubMed Central

Background Candida-associated denture stomatitis is a frequent infectious disease. Treatment of this oral condition is difficult because failures and recurrences are common. The aim of this study was to test the in vitro antifungal activity of pure constituents of essentials oils. Methods Eight terpenic derivatives (carvacrol, farnesol, geraniol, linalool, menthol, menthone, terpinen-4-ol, and ?-terpineol), a phenylpropanoid (eugenol), a phenethyl alcohol (tyrosol) and fluconazole were evaluated against 38 Candida isolated from denture-wearers and 10 collection Candida strains by the CLSI M27-A3 broth microdilution method. Results Almost all the tested compounds showed antifungal activity with MIC ranges of 0.03-0.25% for eugenol and linalool, 0.03-0.12% for geraniol, 0.06-0.5% for menthol, ?-terpineol and terpinen-4-ol, 0.03-0.5% for carvacrol, and 0.06-4% for menthone. These compounds, with the exception of farnesol, menthone and tyrosol, showed important in vitro activities against the fluconazole-resistant and susceptible-dose dependent Candida isolates. Conclusions Carvacrol, eugenol, geraniol, linalool and terpinen-4-ol were very active in vitro against oral Candida isolates. Their fungistatic and fungicidal activities might convert them into promising alternatives for the topic treatment of oral candidiasis and denture stomatitis. PMID:22118215

2011-01-01

207

Titanium nanotubes activate genes related to bone formation in vitro  

PubMed Central

Background: Titanium is used worldwide to make osseointegrable devices, thanks to its favorable characteristics as mechanical proprieties and biocompatibility, demonstrated by in vivo studies with animal models and clinical trials over a forty-year period. However, the exact genetic effect of the titanium layer on cells is still not well characterized. Materials and Methods: To investigate how titanium nanotubes stimulate osteoblasts differentiation and proliferation, some osteoblast genes (SP7, RUNX2, COL3A1, COL1A1, ALPL, SPP1 and FOSL1) were analyzed by quantitative Real Time RT- PCR. Results: After 15 days, osteoblasts cultivated on titanium naotube showed the up-regulation of bone related genes SP7, ENG, FOSL1 and SPP1 and the down-regulation of RUNX2, COL3A1, COL1A1, and ALPL. After 30 days of treatment, the bone related genes SP7, ENG, FOSL1 and RUNX2 were up-regulated while COL3A1, COL1A1, ALPL and SPP1 were down-regulated. Conclusions: Our results, demonstrates that titanium nanotubes can lead to osteoblast differentiation and extracellular matrix deposition and mineralization in dental pulp stem cells by the activation of osteoblast related genes SPP1, FOSL1 and RUNX2. PMID:23814577

Pozio, Alfonso; Palmieri, Annalisa; Girardi, Ambra; Cura, Francesca; Carinci, Francesco

2012-01-01

208

The in Vitro Estrogenic Activities of Polyfluorinated Iodine Alkanes  

PubMed Central

Background: Polyfluorinated iodine alkanes (PFIs) are important intermediates in the synthesis of organic fluoride products. Recently, PFIs have been detected in fluoropolymers as residual raw materials, as well as in the ambient environment. Objectives: High production volumes and potential environmental releases of PFIs might become a concern, but the exposure risk and toxicity of these chemicals are still unclear. In this study, we investigated the potential estrogenic effects of PFIs. Methods: We studied the estrogenic effects of fluorinated iodine alkanes (FIAs), fluorinated telomer iodides (FTIs), and fluorinated diiodine alkanes (FDIAs) using the E-screen and MVLN assays and the evaluation of estrogen-responsive genes in MCF-7 cells. Results: FIAs have an iodine atom at one end of the perfluorinated carbon chain. 1-Iodoperfluorohexane (PFHxI) and 1-iodoperfluorooctane (PFOI) promoted the proliferation of MCF-7 cells, induced luciferase activity in MVLN cells, and up-regulated the expression of TFF1 and EGR3. In these assays, other FIAs gave negative responses. FDIAs have an iodine atom at each end of the perfluorinated carbon chain, and all the FDIAs showed estrogenic effects. The estrogenic potencies of FIAs and FDIAs correlate well with the carbon chain length of the chemicals. The optimum chain length for estrogenic effects is six carbons, and then eight and four carbons. All FTIs have a single iodine atom at the end of a partially fluorinated carbon chain. None of the FTIs showed estrogenic effects in the tests. Conclusions: The estrogenic effects of PFIs are dependent on the structural features of iodine substitution and chain length. This research will be helpful in further understanding the estrogenic effects of perfluorinated compounds. PMID:21990342

Wang, Chang; Wang, Thanh; Liu, Wei; Ruan, Ting; Zhou, Qunfang; Liu, Jiyan; Zhang, Aiqian; Zhao, Bin

2011-01-01

209

A superabsorbent polymer-containing wound dressing efficiently sequesters MMPs and inhibits collagenase activity in vitro.  

PubMed

Superabsorbent polymer (SAP)-containing wound dressings present a valuable and unique category of wound management products. An in vitro approach was used to assess the effects of a new SAP dressing in treatment of non-healing wounds. It was shown that the SAP dressing possesses a significant binding capacity for MMP-2 and MMP-9 in vitro (P\\0.001). The inclusion of the bound proteases was so strong that no MMP-2 and only marginal amounts of MMP-9 were released from the dressing samples in a subsequent elution step. In addition, the SAP dressing was able to take up collagenase and reduce its activity in vitro. However, collagenase was not completely inactivated upon binding and enzyme-mediated substrate turnover could be observed at the dressings. In conclusion, in vitro data confirm the positive effect of the SAP wound dressing observed in vivo. The findings suggest that it should be specifically useful for highly exuding wounds with an elevated proteolytic activity that needs to be reduced to support healing. PMID:23797827

Wiegand, Cornelia; Hipler, Uta-Christina

2013-10-01

210

Synthesis and Biological Evaluation of 1,4-Naphthoquinones and Quinoline-5,8-diones as Antimalarial and Schistosomicidal Agents  

PubMed Central

Improving the solubility of polysubstituted 1,4-naphthoquinone derivatives was achieved by introducing nitrogen in two different positions of the naphthoquinone core, at C-5 and at C-8 of menadione through a two-step, straightforward synthesis based on the regioselective hetero-Diels-Alder reaction. The antimalarial and the antischistosomal activities of these polysubstituted aza-1,4-naphthoquinone derivatives were evaluated and led to the selection of distinct compounds for antimalarial versus antischistosomal action. The AgII-assisted oxidative radical decarboxylation of the phenyl acetic acids using AgNO3 and ammonium peroxodisulfate was modified to generate the 3-picolinyl-menadione with improved pharmacokinetic parameters, high antimalarial effects and capacity to inhibit the formation of ?-hematin. PMID:22777178

Lanfranchi, Don Antoine; Cesar-Rodo, Elena; Bertrand, Benoît; Huang, Hsin-Hung; Day, Latasha; Johann, Laure; Elhabiri, Mourad; Becker, Katja; Williams, David L.

2012-01-01

211

In vitro antioxidant and cytotoxic activity of some synthetic riparin-derived compounds.  

PubMed

This study aimed to study the in vitro antioxidant activity and cytotoxicity on tumor cells lines of six synthetic substances derived from riparins. All the substances showed antioxidant activity and riparins C, D, E, F presented cell growth inhibition rates greater than 70%, suggesting that these molecules have antitumor properties. These substances also caused greater than 80% releases of cytoplasmic lactate dehydrogenase enzyme (LDH). Although the antioxidant and antitumor properties presented herein require further assessment, the outcomes indicate that these novel riparins are promising biologically active compounds. PMID:24731987

Nunes, Geandra B L; Policarpo, Paola R; Costa, Luciana M; da Silva, Teresinha G; Milităo, Gardenia Carmen G; Câmara, Celso A; Barbosa Filho, José Maria; Gutierrez, Stanley Juan C; Islam, Mohammed T; de Freitas, Rivelilson M

2014-01-01

212

Oxidative stress biomarkers and acetylcholinesterase activity in human erythrocytes exposed to clomazone (in vitro)  

PubMed Central

The aim of this study was to investigate the effect of clomazone herbicide on oxidative stress biomarkers and acetylcholinesterase activity in human erythrocytes in in vitro conditions. The activity of catalase (CAT), superoxide dismutase (SOD) and acetylcholinesterase (AChE), as well as the levels of thiobarbituric acid reactive substances (TBARS) and reduced glutathione (GSH) were measured in human erythrocytes exposed (in vitro) to clomazone at varying concentrations in the range of 0, 100, 250 and 500 µg/L for 1 h at 37 °C.TBARS levels were significantly higher in erythrocytes incubated with clomazone at 100, 250 and 500 µg/L. However, erythrocyte CAT and AChE activities were decreased at all concentrations tested. SOD activity was increased only at 100 µg/L of clomazone. GSH levels did not change with clomazone exposure. These results clearly showed clomazone to induce oxidative stress and AChE inhibition in human erythrocytes (in vitro). We, thus, suggest a possible role of ROS on toxicity mechanism induced by clomazone in humans. PMID:22058656

Santi, Adriana; Menezes, Charlene; Duarte, Marta Maria F.; Leitemperger, Jossiele; Lópes, Thais; Loro, Vania L.

2011-01-01

213

New triazoles and echinocandins: mode of action, in vitro activity and mechanisms of resistance.  

PubMed

Different types of mycoses, especially invasive mycoses caused by yeasts and molds, are a growing problem in healthcare. The most notable explanation for this increase is a rise in the number of immunocompromised patients owing to advances in transplantation, the emergence of AIDS and a rise in the number of invasive surgical procedures. Despite advances in medical practice, some therapeutic problems remain. In addition, intrinsic or acquired antifungal resistance may pose a serious problem to antifungal therapy. A new generation of triazole agents (voriconazole, posaconazole, isavuconazole, ravuconazole and albaconazole) and the recent class of the echinocandins (caspofungin, micafungin and anidulafungin) have become available, and represent an alternative to conventional antifungals for serious fungal infection management. Currently, only two of the recent triazole generation (voriconazole and posaconazole) and all three echinocandins are available for clinical use. More precisely, voriconazole and posaconazole are indicated for the treatment of invasive fungal infections and the echinocandins for the treatment of specific candidiasis. Voriconazole and posaconazole have a very broad spectrum of antifungal activity that includes Candida species, and filamentous and dimorphic fungi. Their activity extends to both fluconazole- and itraconazole-resistant strains of Candida. A major difference between posaconazole and voriconazole is that posaconazole has activity against Zygomycetes including Mucor spp., Rhizopus spp. and Cunninghamella spp., and voriconazole has no activity against this class of fungi. Ravuconazole, isavuconazole and albaconazole have shown very potent in vitro activity against species of Candida, Cryptococcus and Aspergillus, and they are currently in various stages of development. All three echinocandin agents, caspofungin, micafungin and anidulafungin, are similar in their spectrum of activity. Echinocandins do not possess in vitro activity against important basidiomycetes, including Cryptococcus, Rhodotorula and Trichosporon. This review attempts to deliver the most up-to-date knowledge on the mode of action and mechanisms of resistance to triazoles and echinocandins in fungal pathogens. In addition, the in vitro activity data available on triazoles and echinocandins are reported. PMID:19803707

Fera, Maria Teresa; La Camera, Erminia; De Sarro, Angelina

2009-10-01

214

In vitro activity of tigecycline against methicillin-resistant Staphylococcus aureus, including livestock-associated strains  

PubMed Central

The in vitro activity of tigecycline was determined using a well-defined collection of methicillin-resistant Staphylococcus aureus (MRSA) isolates (n?=?202), including 33 livestock-associated strains. Susceptibility testing was performed using the Etest system. Among the 202 MRSA strains, three (1.5%) had a minimum inhibitory concentration (MIC) value for tigecycline greater than 0.5 mg/l, which are considered to be resistant. When these strains were tested using Iso-Sensitest medium, the MICs were substantially lower and no resistance was found. This discrepancy warrants further investigations into the preferred test conditions for tigecycline. In conclusion, tigecycline showed good activity against MRSA strains in vitro. PMID:20186450

Verhulst, C. J. M. M.; Huijsdens, X. W.; Kluytmans, J. A. J. W.

2010-01-01

215

In vitro and in vivo antioxidant activities of polysaccharide purified from aloe vera (Aloe barbadensis) gel.  

PubMed

The in vitro and in vivo antioxidant potentials of a polysaccharide isolated from aloe vera gel were investigated. Enzymatic extracts were prepared from aloe vera gel by using ten digestive enzymes including five carbohydrases and five proteases. Among them, the highest yield was obtained with the Viscozyme extract and the same extract showed the best radical scavenging activity. An active polysaccharide was purified from the Viscozyme extract using ethanol-added separation and anion exchange chromatography. Purified aloe vera polysaccharide (APS) strongly scavenged radicals including DPPH, hydroxyl and alkyl radicals. In addition, APS showed a protective effect against AAPH-induced oxidative stress and cell death in Vero cells as well as in the in vivo zebrafish model. In this study, it is proved that both the in vitro and in vivo antioxidant potentials of APS could be further utilized in relevant industrial applications. PMID:24274519

Kang, Min-Cheol; Kim, Seo Young; Kim, Yoon Taek; Kim, Eun-A; Lee, Seung-Hong; Ko, Seok-Chun; Wijesinghe, W A J P; Samarakoon, Kalpa W; Kim, Young-Sun; Cho, Jin Hun; Jang, Hyeang-Su; Jeon, You-Jin

2014-01-01

216

Antifungal activity of hypothemycin against Peronophythora litchii in vitro and in vivo.  

PubMed

The antifungal activity of a natural resorcylic acid lactone, hypothemycin (HPM), against Peronophythora litchii in vitro and in vivo was investigated. HPM treatment substantially suppressed spore germination of P. litchi, with the inhibition rate of 100% when 0.78 ?g/mL HPM was applied. Similarly, mycelial growth of P. litchii was efficiently inhibited. Furthermore, HPM caused the ultrastructural modifications of P. litchii, including the disruption of the cell wall and the endomembrane system, especially the plasma membrane, mitochondria, and vacuoles, which led to the destruction of the cellular integrity. Moreover, application of HPM significantly reduced decay and suppressed peel browning of postharvest litchi fruit inoculated with P. litchii during storage at 28 °C. Overall, these findings suggested that HPM exhibited excellent antifungal activity against P. litchii both in vitro and in vivo, which could be helpful for the storage of harvest litchi fruit. PMID:24106914

Xu, Liangxiong; Xue, Jinghua; Wu, Ping; Wang, Duoduo; Lin, Lijing; Jiang, Yueming; Duan, Xuewu; Wei, Xiaoyi

2013-10-23

217

Sericins exhibit ROS-scavenging, anti-tyrosinase, anti-elastase, and in vitro immunomodulatory activities.  

PubMed

Some biological properties of Bombyx mori sericins from twenty strains were investigated, fourteen fed with artificial diet, two with fresh mulberry leaves and four with both diets. Sericin exhibited ROS-scavenging, anti-tyrosinase and anti-elastase properties, the strain significantly influenced these properties, while diet only influenced the anti-tyrosinase activity. Sericins were clustered into 5 groups and one sericin from each group was further studied: sericins showed anti-proliferative activity on in vitro stimulated peripheral blood mononuclear cells; some strains decreased in vitro secretion of IFN?, while no effects were observed on TNF? and IL10 release. Therefore, a mixture of sericins extracted from the most promising strains may be useful for dermatological and cosmetic use. PMID:23541552

Chlapanidas, Theodora; Faragň, Silvio; Lucconi, Giulia; Perteghella, Sara; Galuzzi, Marta; Mantelli, Melissa; Avanzini, Maria Antonietta; Tosca, Marta Cecilia; Marazzi, Mario; Vigo, Daniele; Torre, Maria Luisa; Faustini, Massimo

2013-07-01

218

Sulfated modification of longan polysaccharide and its immunomodulatory and antitumor activity in vitro.  

PubMed

A water-soluble polysaccharide fraction (LP1) was prepared from Dimocarpus longan Lour. by hot water extraction, DEAE-cellulose and Sephadex G-100 chromatography. Its sulfated derivative (LP1-S) was prepared by the sulfuric acid method. Preliminary tests in vitro showed LP1 and LP1-S could stimulate murine lymphocytes proliferation, increase pinocytic activity of murine macrophages and production of nitric oxide (NO), interleukin 6 (IL-6), IL-1? and tumor necrosis factor-alpha (TNF-?) in macrophages. Furthermore, LP1-S exhibited higher antiproliferative activity against human nasopharyngeal carcinoma HONE1 cells in vitro than LP1, which might be caused by the sulfate group in its structures. These results indicated that the LP1-S might be useful for developing safe antitumor drugs or health food. PMID:24680807

Jiang, Jie; Meng, Fa-Yan; He, Zhou; Ning, Yuan-Ling; Li, Xue-Hua; Song, Hui; Wang, Jing; Zhou, Rui

2014-06-01

219

In vitro and in vivo antimicrobial activities of sporaricin A, a new aminoglycoside.  

PubMed Central

The in vitro and in vivo antimicrobial activity of sporaricin A, a new aminoglycoside, was compared with that of amikacin, dibekacin, and gentamicin. Sporaricin A showed a broad spectrum of activity against various gram-positive and -negative bacteria, including amikacin-, dibekacin-, or gentamicin-resistant strains. Sporaricin A inhibited more than 90% of clinical isolates of staphylococci, Klebsiella, Enterobacter, Citrobacter, Serratia, and Proteus, except for P. morganii and P. inconstans, at the concentration of 3.13 microgram/ml. This activity, except for that against Serratia, was similar to that of amikacin. Against P. inconstans and S. marcescens, sporaricin A was more effective than amikacin, dibekacin, and gentamicin. However, its activity against Pseudomonas aeruginosa was relatively weak in comparison with three other aminoglycosides. Sporaricin A was highly effective against bacteria that had various aminoglycoside-inactivating enzymes and that were resistant to the other drugs tested, but it was not active against those with aminoglycoside 3-acetyltransferase-I. The activity of sporaricin A tended to be greater with a reduction in inoculum size of bacteria and an increase in medium pH and decreased slightly in the presence of 10 to 50% horse serum. The in vitro activity was confirmed by in vivo tests in experimental infections with various bacteria. Its protective effect seemed to be equal to or greater than that of amikacin or dibekacin. PMID:7425599

Kobayashi, F; Saino, Y; Koshi, T; Hattori, Y

1980-01-01

220

In vitro antioxidant activities of methanol and aqueous extract of Annona squamosa (L.) fruit pulp.  

PubMed

The present study evaluated the antioxidant activity of the fruit of Annona squamosa by means of in vitro studies involving two different solvent extracts: methanol and aqueous. The antioxidant properties of the extract were determined by scavenging 1, 1-diphenyl-2-picrylhydrazyl radical (DPPH), lipid peroxidation (LPO), nitric oxide (NO), superoxide anion (O2(-)), hydroxyl radical (OH(•)), reducing power and total antioxidant. The results showed that, compared to aqueous extract, a methanolic fruit extract of A squamosa has a higher percentage of inhibition of DPPH radical scavenging activity (97.99%), LPO (94.15%), NO scavenging activity (70.96%), O2(-) scavenging activity and OH(•) scavenging activity (78.68% and 85.25%, respectively), total antioxidant activity (206 ?g ?-tocopherol/g) and reducing power (56.0 ?g of ascorbic acid/g). The results obtained in the in vitro models clearly suggest that methanol extract has higher antioxidant activity than the aqueous extract due to a higher presence of phenolic and flavonodal constituents in the methanol extract. PMID:23787283

Nandhakumar, Elumalai; Indumathi, Parameswaran

2013-06-01

221

Carboxymethylation of a polysaccharide extracted from Ganoderma lucidum enhances its antioxidant activities in vitro  

Microsoft Academic Search

The chemical carboxylmethylated polysaccharide (C-GLP), which derived from water-insoluble crude Ganoderma lucidum polysaccharide (GLP), was prepared. Water solubility, chemical characterization, and antioxidant activities in vitro of C-GLP were determined. The solubility of C-GLP in distilled water reached 100mg\\/ml, which was much higher than the solubility of GLP. Chemical analysis indicated that C-GLP was composed of Glc:Man:Gal=33.0:1.0:3.4 with a molecular weight

Jing Xu; Wei Liu; Wenbing Yao; Xiubing Pang; Dengke Yin; Xiangdong Gao

2009-01-01

222

Activity of imipenem against Klebsiella pneumoniae biofilms in vitro and in vivo.  

PubMed

Encapsulated Klebsiella pneumoniae has emerged as one of the most clinically relevant and more frequently encountered opportunistic pathogens in combat wounds as the result of nosocomial infection. In this report, we show that imipenem displayed potent activity against established K. pneumoniae biofilms under both static and flow conditions in vitro. Using a rabbit ear model, we also demonstrated that imipenem was highly effective against preformed K. pneumoniae biofilms in wounds. PMID:24247132

Chen, Ping; Seth, Akhil K; Abercrombie, Johnathan J; Mustoe, Thomas A; Leung, Kai P

2014-01-01

223

In vitro Fungicidal Activity of Humic Acid Fraction from Oil Palm Compost  

Microsoft Academic Search

Fungicidal activity of humic acids isolated from empty fruit bunch of oil palm compost EFB-HA and commercial grade humic acid Co-HA were evaluated on the conidial germination and mycelial growth of Choanephora cucurbitarum. EFB-HA and Co-HA significantly (P ? 0.05) inhibited the mycelial growth and conidial germination of C. cucurbitarum in vitro compared to control. The inhibition in mycelial growth

YASMEEN SIDDIQUI; SARIAH MEON; RAZI ISMAIL; MAWARDI RAHMANI; ASGAR ALI

224

Effect of activated charcoal on endotoxin adsorption. Part I. An in vitro study.  

PubMed

An in vitro study by using cross-linked agarose coated activated charcoal (CAAC-II) as adsorbent was conducted. Endotoxin was quantitatively measured by chromogenic method of limulus lysate test. Results of the study demonstrated that endotoxin was fairly efficiently removed by CAAC-II. It may therefore be possible for effective adsorption of endotoxin in vivo studies and warrant further experimental study for CAAC-II hemoperfusion in clinical endotoxemia. PMID:3449139

Du, X N; Niu, Z; Zhou, G Z; Li, Z M

1987-01-01

225

Comparative in vitro activity of gemifloxacin, ciprofloxacin, levofloxacin and ofloxacin in a North American surveillance study  

Microsoft Academic Search

The in vitro activity of gemifloxacin, a new fluoroquinolone, was compared to three marketed fluoroquinolones; ciprofloxacin, levofloxacin and ofloxacin against over 4,000 recent clinical isolates covering 29 species isolated in the United States and Canada between 1997–1999. Based on MIC90s, gemifloxacin was the most potent fluoroquinolone tested against a majority of Gram-positive isolates: Streptococcus pneumoniae, penicillin resistant S. pneumoniae, macrolide

D. J Hoban; S. K Bouchillon; J. L Johnson; G. G Zhanel; D. L Butler; L. A Miller; J. A Poupard

2001-01-01

226

In vitro activity of clinafloxacin against fluoroquinolone resistant Spanish clinical isolates  

Microsoft Academic Search

The in vitro activity of clinafloxacin against 162 ciprofloxacin-resistant clinical isolates was determined. Isolates were selected when their MIC to ciprofloxacin was 2 mg\\/l (intermediate) or >2 mg\\/l (resistant). The following strains were tested: 61 Escherichiacoli, 12 Klebsiellapneumoniae, 7 Proteusmirabilis, 21 Serratiamarcescens, 4 Enterobactercloacae, 21 Pseudomonasaeruginosa, 21 Staphylococcus.aureus (resistant to methicillin) and 15 Enterococcus spp. Clinafloxacin, ciprofloxacin, ofloxacin and norfloxacin

Manuel López-Brea; Nuria Prieto; Diego Domingo; Carmen de las Cuevas; Isabel Sánchez; Teresa Alarcón

1999-01-01

227

In Vitro Activity of A-86719.1, a Novel 2Pyridone Antimicrobial Agent  

Microsoft Academic Search

This study evaluated the in vitro activity of A-86719.1, a novel 2-pyridone antimicrobial agent. The drug inhibited all tested members of the family Enterobacteriaceae at #0.5 mg\\/ml and all tested Pseudomonas aeruginosa,Burkholderia(Pseudomonas)cepacia, andXanthomonas maltophiliastrains at #2 mg\\/ml. All but two strains of gram-positive bacteria were inhibited by #1 mg of the new drug per ml, including isolates highly resistant to

G. M. ELIOPOULOS; C. B. WENNERSTEN; G. COLE; D. CHU; D. PIZZUTI; C. MOELLERING

1995-01-01

228

In Vitro and In Vivo Activities of Moxifloxacin and Clinafloxacin against Mycobacterium tuberculosis  

Microsoft Academic Search

On 10% oleic acid-albumin-dextrose-catalase-enriched 7H11 agar medium, the MIC at which 90% of the isolates are inhibited for 20 strains of Mycobacterium tuberculosis was 0.5 mg of sparfloxacin (SPFX) or moxifloxacin (MXFX) per ml and 1.0 mg of clinafloxacin (CNFX) per ml, indicating that the in vitro activities of SPFX and MXFX were virtually identical and were slightly greater than

BAOHONG JI; NACER LOUNIS; CAROLINE MASLO; CHANTAL TRUFFOT-PERNOT; PASCALE BONNAFOUS; JACQUES GROSSET

229

In vitro activity of sorghum non-tannin polyphenols against grain molding and weathering fungi  

E-print Network

Plant Phenolics and Disease Resistance . Location of Sorghum Polyphenols Extraction Methods Separation of Low Molecular Weight Phenols from Tannins Sorghum Molding and Weathering Fungi MATERIALS AND METHODS Sorghum Samples Grain Molding...IN VITRO ACTIVITY OF SORGHUM NON-TANNIN POLYPHENOLS AGAINST GRAIN MOLDING AND WEATHERING FUNGI A Thesis by PATCHARIN LEUNGCHAIKUL Submitted to the Graduate College of Texas A&M University in partial fulfillment of the requirement...

Leungchaikul, Patcharin

1982-01-01

230

In vitro activities of eight antifungal drugs against 55 clinical isolates of Fonsecaea spp  

Microsoft Academic Search

The in vitro activities of eight antifungal drugs against clinical isolates of Fonsecaea pedrosoi (n = 21), Fonsecaea monophora (n = 25), and Fonsecaea nubica (n = 9) were tested. The resulting MIC90s for all strains (n = 55) were as follows, in increasing order: posaconazole, 0.063 µg\\/ml; itraconazole, 0.125 µg\\/ml; isavuconazole, 0.25 µg\\/ml; voriconazole, 0.5 µg\\/ml; amphotericin B, 2

M. J. Najafzadeh; H. Badali; M. T. Illnait-Zaragozi; Hoog de G. S; J. F. Meis

2010-01-01

231

In vitro antibacterial activity of some Iranian medicinal plant extracts against Helicobacter pylori  

Microsoft Academic Search

Helicobacter pylori infection causes lifelong chronic gastritis, which can lead to peptic ulcer, mucosa-associated lymphoid tissue (MALT) lymphoma and gastric cancer. The growing problem of antibiotic resistance by the organism demands the search for novel candidates from plant-based sources. In the present study, we evaluated the in vitro anti-H. pylori activity of some selected medicinal plants on clinical isolates of H.

M. Hajimahmoodi; M. Shams-Ardakani; P. Saniee; F. Siavoshi; M. Mehrabani; H. Hosseinzadeh; P. Foroumadi; M. Safavi; M. Khanavi; T. Akbarzadeh; A. Shafiee; A. Foroumadi

2011-01-01

232

Antibacterial and antifungal activity of scabronine G and H in vitro  

Microsoft Academic Search

Two interesting cyathane-type diterpenoids, scabronines G and H, isolated from the fruiting bodies of the basidiomycete, Sarcodon scabrosus (L.: Fr.) Karst, were tested against the bacteria, Staphylococcus aureus, Bacillus thuringiensis, Escherichia coli, Bacillus megaterium and Bacillus subtilis. Both scabronine G and H showed promising activity in vitro against the five bacteria tested at 1 mg\\/ml and 100 ?g\\/ml. The degree

Bing-Ji Ma; Ting-Ting Wu; Yuan Ruan; Jin-Wen Shen; Han Zhou; Hai-You Yu; Xu Zhao

2010-01-01

233

In vitro propagation of the medicinal plant Ziziphora tenuior L. and evaluation of its antioxidant activity  

PubMed Central

Ziziphora tenuior L. (Lamiaceae) is an aromatic herb used for its medicinal values against fungi, bacteria. Micropropagation can be used for large-scale multiplication of essential oil producing plants thus avoiding an overexploitation of natural resources. This work aims to develop a reliable protocol for the in vitro propagation of Z. tenuior, and to compare the antioxidant activity between in vitro propagated and wild plants. The explants were sterilized and cultured on MS medium containing different concentrations of growth regulators naphthalene acetic acid (NAA) or indole-3-butyric acid (IBA) with 0.5 mg/L of kinetin (Kin) callus formation was 70.2% after 45 days of incubation in dark on medium supplemented with 1.5 mg/L of NAA. After one month of callus culture on medium supplemented with 2 mg/L BA the shoot number was 5.12 and for the multiplication stage. The shoot number was 4.21 and length was 6.17 cm on medium supplemented with 1 mg/L Kin + 0.1 mg/L NAA. DPPH• reagent was used to test the antioxidant activity. The aqueous and methanol extracts of in vitro plants which were treated with 1.5 and 1 mg/L of kin plus 0.1 mg/L of NAA showed a strong DPPH• scavenging activity where IC50 was 0.307 and 0.369 mg/ml, respectively, while the IC50 of aqueous and methanol extracts of wild plants was 0.516 and 9.229 mg/ml, respectively. Our results suggested that plant growth regulators and in vitro culture conditions increased the antioxidant activity. PMID:25183942

Dakah, Abdulkarim; Zaid, Salim; Suleiman, Mohamad; Abbas, Sami; Wink, Michael

2014-01-01

234

In vitro and in vivo Activities of a New Lead Compound I2906 against Mycobacterium tuberculosis  

Microsoft Academic Search

Background: Due to the long duration of treatment and the emergence of multidrug-resistant strains, new antitubercular agents are urgently needed. I2906, as a novel lead, was screened and tested for efficacy in vitro and in vivo. Methods:To determine the efficacy of I2906,the minimum inhibitory concentrations against Mycobacterium tuberculosis and cytotoxicity were tested, and its in vivo activities were assessed by

Jingning Lu; Jun Yue; Jing Wu; Rusong Luo; Zhidong Hu; Jianrong Li; Yun Bai; Zhijiao Tang; Qiaoyang Xian; Xuelian Zhang; Honghai Wang

2010-01-01

235

Antioxidant potential of water hyacinth (Eichornia crassipes): In vitro antioxidant activity and phenolic composition  

Microsoft Academic Search

The aims of the present study were (a) to extract and quantify the main phenolic acids and tocopherols from the petiole, leaves, and flowers of Eichornia crassipes, (b) to evaluate the antioxidant capacity of the extracts in four in vitro systems [1,1-diphenyl-2-pycryl-hydrazyl (DPPH) radical scavenging ability, iron chelating activity, reducing power, and prevention of oxidation in a liposome model system],

A. Surendraraj; K. H. Sabeena Farvin; R. Anandan

2012-01-01

236

Activity of Imipenem against Klebsiella pneumoniae Biofilms In Vitro and In Vivo  

PubMed Central

Encapsulated Klebsiella pneumoniae has emerged as one of the most clinically relevant and more frequently encountered opportunistic pathogens in combat wounds as the result of nosocomial infection. In this report, we show that imipenem displayed potent activity against established K. pneumoniae biofilms under both static and flow conditions in vitro. Using a rabbit ear model, we also demonstrated that imipenem was highly effective against preformed K. pneumoniae biofilms in wounds. PMID:24247132

Chen, Ping; Seth, Akhil K.; Abercrombie, Johnathan J.; Mustoe, Thomas A.

2014-01-01

237

Nanostructured Systems Containing Rutin: In Vitro Antioxidant Activity and Photostability Studies  

NASA Astrophysics Data System (ADS)

The improvement of the rutin photostability and its prolonged in vitro antioxidant activity were studied by means of its association with nanostructured aqueous dispersions. Rutin-loaded nanocapsules and rutin-loaded nanoemulsion showed mean particle size of 124.30 ± 2.06 and 124.17 ± 1.79, respectively, polydispersity index below 0.20, negative zeta potential, and encapsulation efficiency close to 100%. The in vitro antioxidant activity was evaluated by the formation of free radical ·OH after the exposure of hydrogen peroxide to a UV irradiation system. Rutin-loaded nanostructures showed lower rutin decay rates [(6.1 ± 0.6) 10-3 and (5.1 ± 0.4) 10-3 for nanocapsules and nanoemulsion, respectively] compared to the ethanolic solution [(35.0 ± 3.7) 10-3 min-1] and exposed solution [(40.1 ± 1.7) 10-3 min-1] as well as compared to exposed nanostructured dispersions [(19.5 ± 0.5) 10-3 and (26.6 ± 2.6) 10-3, for nanocapsules and nanoemulsion, respectively]. The presence of the polymeric layer in nanocapsules was fundamental to obtain a prolonged antioxidant activity, even if the mathematical modeling of the in vitro release profiles showed high adsorption of rutin to the particle/droplet surface for both formulations. Rutin-loaded nanostructures represent alternatives to the development of innovative nanomedicines.

Almeida, Juliana S.; Lima, Fernanda; Ros, Simoní Da; Bulhőes, Luis O. S.; de Carvalho, Leandro M.; Beck, Ruy C. R.

2010-10-01

238

Kaurenic acid: Evaluation of the in vivo and in vitro antitumor activity on murine melanoma  

PubMed Central

Objective: The in vivo and in vitro antitumor activity of kaurenic acid [kaur 16-en-19 oic acid] (KA) in melanoma was evaluated in a murine model in comparison with taxol (Tx). Materials and Methods: B16F1 melanoma was developed in C57BL/6 mice and cell cultures. Survival test, tumor growth, dissected-tumor measurements, histology, cytoxicity assay on cultured cells, and changes of apoptotic gene expression at mRNA level were analyzed. Results: KA showed antitumor effect in vivo and in vitro and compared with Tx, its antimelanoma activity was greater (P < 0.001). These results were confirmed by morphological analysis (P < 0.001). In melanoma cell cultures, KA IC50 was 0.79 ?M vs. 18.94 ?M for Tx (P < 0.001). RT-PCR analysis demonstrated that Bcl-xL mRNA expression was altered in B16F1 mouse melanoma cells obtained from mice treated with either KA or Tx. Conclusion: The data suggest that KA is active in animal melanoma models, both in vitro and in vivo, being its cytotoxic effects stronger than those exhibited by Tx. Further trials should be conducted to elucidate its mechanism of action in melanoma with respect to necrosis or apoptotic processes. Our results support other evidences indicating that KA is a potential chemotherapeutic agent against cancer that has to be widely explored. PMID:22144774

Sosa-Sequera, Miriam C.; Chiurillo, Miguel; Moscoso, Jaime; Dolinar, Josefina; Suarez, Omar; Neira, Natalia; Mendoza, Hernan; Rivero-Paris, María

2011-01-01

239

A putative sub-lo-kDa basement membrane activity required for lung alveolar formation in vitro  

E-print Network

A putative sub-lo-kDa basement membrane activity required for lung alveolar formation in vitro required for lung alveolar formation in vitro. Am. J. PhysioZ. 271 (Lung CeZZ. 2MoZ. PhysioZ. 15): L489-L494, 1996.-Basement membrane promotes the reassembly of isolated type II alveolar cells into alveoli

240

Causes of developmental failure of in-vitro matured rhesus monkey oocytes: impairments in embryonic genome activation  

Microsoft Academic Search

BACKGROUND: Understanding the causes of developmental failure of in-vitro matured primate oocytes may lead to viable strategies for improving their developmental competence. The aims of this study were to determine whether the timely onset of embryonic genome activation among individual blastomeres of preimplantation maca- que embryos is impaired by in-vitro maturation (IVM) of oocytes and whether these impairments are associated

R. Dee Schramm; Ann Marie Paprocki; Catherine A. VandeVoort

2003-01-01

241

In vitro antioxidant activity of hydro alcoholic extract from the fruit pulp of Cassia fistula Linn  

PubMed Central

The present study is aimed to investigate antioxidant activity of the extracts of Cassia fistula Linn. (Leguminosae) fruit pulp. Cassia fistula Linn., a Indian Laburnum, is widely cultivated in various countries and different continents including Asia, Mauritius, South Africa, Mexico, China, West Indies, East Africa and Brazil as an ornamental tree for its beautiful bunches of yellow flowers and also used in traditional medicine for several indications. The primary phytochemical study and in vitro antioxidant study was performed on hydro alcoholic extract of fruit pulp. Phytochemical screening of the plant has shown the presence of phenolic compounds, fatty acids, flavonoids, tannins and glycosides. Phenolic content was measured using Folin-Ciocalteu reagent and was calculated as gallic acid equivalents. Antiradical activity of hydro alcoholic extract was measured by DPPH (2,2-diphenyl-1- picrylhydrazyl) assay and was compared to ascorbic acid. Ferric reducing power of the extract was also evaluated by Oyaizu method. In the present study, three methods were used for evaluation of antioxidant activity. First two methods were for direct measurement of radical scavenging activity and third method to evaluate the reducing power. Results indicate that hydro alcoholic fruit pulp extracts have marked amount of total phenols which could be responsible for the antioxidant activity. These in vitro assays indicate that this plant extract is a significant source of natural antioxidant, Cassia fistula fruit pulp extract shows lower activity in DPPH and total phenol content as compared with standard which might be helpful in preventing the progress of various oxidative stresses. PMID:24250133

Bhalodia, Nayan R.; Nariya, Pankaj B.; Acharya, R. N.; Shukla, V. J.

2013-01-01

242

Urokinase-type plasminogen activator regulates cranial neural crest cell migration in vitro.  

PubMed

Proper migration and differentiation of neural crest (NC) cells are required for normal development of craniofacial structures, heart and great vessels, sensory and autonomic nervous systems, and other organs with vertebrate embryos. Serine-protease inhibitors reduce NC cell migration in vitro, suggesting the extracellular proteases are important mediators of NC cell migration. While plasminogen activator activity levels are high in NC cells relative to other embryonic tissue, its ability to regulate NC cell migration has not been specifically tested in vivo or in vitro through its ability to convert plasminogen to plasmin. Using a transfilter migration assay, NC cell migration was measured in the presence or absence of plasminogen. Our results showed that plasminogen significantly enhanced NC cell migration. This increase could not be attributed to differences in initial NC cell attachment or cytotoxicity and did not require a chemotactic gradient. The plasminogen-enhanced NC cell migration was blocked by aprotinin (a plasmin inhibitor) and was mimicked by the direct addition of plasmin to the NC cells, indicating that the plasminogen effect was mediated through plasmin generation. Furthermore, anticatalytic-uPA antibody blocked the plasminogen-enhanced NC cell migration showing that NC cell-associated uPA activity was required for this effect. Finally, decreasing NC-uPA activity by treating cells with transforming growth factor-Beta, also blocked the plasminogen-dependent increase in cell migration. These data show that in vitro, NC cell migration is regulated by NC-associated uPA activity suggesting that growth factor-regulation of this activity may play a major role in regulating NC cell migratory capacity in vivo. PMID:8922527

Agrawal, M; Brauer, P R

1996-11-01

243

Diphenyl diselenide in vitro and in vivo activity against the oomycete Pythium insidiosum.  

PubMed

This study evaluated the in vitro activity of diphenyl diselenide against 19 Pythium insidiosum isolates and the in vivo therapeutic response of rabbits with experimentally induced pythiosis. In vitro: susceptibility tests were performed using the broth macrodilution method in accordance with the CLSI document M38-A2. The criteria for interpretation were as follows: MIC-1 and MIC-2 (inhibition of 90% and 100% of mycelium growth, respectively) and the minimum fungicide concentration (MIC-3). In vivo: twenty rabbits were divided into four groups with five animals each and treated for 40 consecutive days: groups 1 and 2 (experimentally induced pythiosis) were treated with diphenyl diselenide (10mg/kg/day) and canola oil (1 mL/kg/day), respectively; groups 3 and 4 (controls) were treated with canola oil (1 mL/kg/day) and diphenyl diselenide (10mg/kg/day), respectively. Toxicity was evaluated using biochemical and haematological parameters. In vitro susceptibility tests showed that 89.4% of isolates had a MIC-1 ? 0.5 ?g/mL, 84.2% of isolates had a MIC-2 ? 1.0 ?g/mL and 94.7% of isolates had a MIC-3 ? 2.0 ?g/mL. The in vivo assay suggested that this compound has a fungistatic activity, and the biochemical and haematological parameters indicated that there was no renal, hepatic or haematological toxicity. The comparison of the unsaturated iron binding capacity levels between animals with and without pythiosis suggested the involvement of iron metabolism in the pathogenesis of pythiosis. This study demonstrated the absence of detectable toxicity caused by diphenyl diselenide and the in vitro fungicidal and in vivo fungistatic activities of this drug, which makes it an option for future therapeutic approaches in the treatment of pythiosis. PMID:22055205

Loreto, Erico Silva; Alves, Sydney Hartz; Santurio, Janio Morais; Nogueira, Cristina Wayne; Zeni, Gilson

2012-04-23

244

Anti-Helicobacter pylori activities of Chenopodium ambrosioides L. in vitro and in vivo  

PubMed Central

AIM: To investigate the bactericidal effects of Chenopodium ambrosioides L. (CAL) against Helicobacter pylori (H. pylori) both in vitro and in vivo. METHODS: For in vitro experiments, the inhibitory activity of CAL was tested using an agar dilution method; H. pylori strain NCTC11637 was incubated on Columbia blood agar plates containing serial concentrations of CAL. The minimal inhibitory concentration (MIC) was determined by the absence of H. pylori colonies on the agar plate. Time-kill curves were used to evaluate bactericidal activity; the average number of colonies was calculated at 0, 2, 8 and 24 h after liquid incubation with concentrations of CAL at 0.5, 1, and 2 × MIC. For in vivo experiments, H. pylori-infected mice were randomly divided into CAL, triple therapy (lansoprazole, metronidazole, and clarithromycin), blank control, or H. pylori control groups. The eradication ratios were determined by positive findings from rapid urease tests (RUTs) and by histopathology. RESULTS: In vitro, the MIC of CAL against H. pylori was 16 mg/L. The time-kill curves showed a stable and persistent decreasing tendency with increasing CAL concentration, and the intensity of the bactericidal effect was proportional to dose; the 1 and 2 × MIC completely inhibited the growth of H. pylori at 24 h. In vivo, the eradication ratios in the CAL group were 60% (6/10) by RUT and 50% (5/10) by histopathology. Ratios in the triple therapy group were both 70% (7/10), and there was no difference between the CAL and triple therapy groups. Histopathologic evaluation revealed massive bacterial colonization on the surface of gastric mucosa and slight infiltration of mononuclear cells after inoculation with H. pylori, but no obvious inflammation or other pathologic changes in gastric mucosa of mice from CAL and triple therapy groups. CONCLUSION: CAL demonstrates effective bactericidal activity against H. pylori both in vitro and in vivo.

Ye, Hui; Liu, Yu; Li, Ning; Yu, Jing; Cheng, Hong; Li, Jiang; Zhang, Xue-Zhi

2015-01-01

245

Phase of the electrical activity rhythm in the SCN in vitro not influenced by preparation time.  

PubMed

The mammalian circadian clock, located in the suprachiasmatic nucleus (SCN) of the hypothalamus, drives daily rhythms in behavioral, physiological, and endocrine functions. The SCN has a genetic basis for rhythm generation and remains rhythmic when it is isolated and kept in constant conditions. This allows for an in vitro analysis of circadian attributes, which is a powerful approach in the study of SCN cellular mechanisms. For studying the phase of the SCN rhythm in vitro, it is important to assess whether preparation of the tissue itself introduces phase shifts. In the present study, we investigated whether preparation of hypothalamic brain slices affects the phase and waveform of the rhythm in electrical impulse frequency of the mouse SCN. Mice were kept under a 12:12 h light-dark cycle, and slices were prepared at six timepoints distributed over the 24 h cycle. We used the peak time and the time of the half-maximum levels in electrical activity as markers for circadian phase. The peak time in electrical activity was observed during the mid-subjective day, irrespective of the time of preparation, at a mean ZT of 5.18+/-0.20 h (n = 39). After preparation in red light at the end of the subjective night, the circadian phase appeared slightly advanced. When slices were prepared in the dark, using infrared illumination, the ANOVA showed no significant differences in peak times and time of half-maximum values between preparation times. The results affirm the value of the slice preparation for studying the phase of the SCN in vitro. We conclude that the phase and waveform of the electrical activity in the SCN in vitro is unaffected by the time of slice preparation but may be influenced by short light presentation when preparation is performed during the subjective night. PMID:19731107

vanderLeest, Henk Tjebbe; Vansteensel, Mariska J; Duindam, Hans; Michel, Stephan; Meijer, Johanna H

2009-08-01

246

Sex differences and in vitro effects of steroids on serum aminopeptidase activities.  

PubMed

We studied the possible existence of physiological sex differences in serum aminopeptidase activities in mice, by evaluating the effect of gonadectomy and the in vitro response to the presence in the medium of cholesterol or steroid hormones. Alanyl- and glutamyl-aminopeptidase activities were measured in sera from male, female, orchiectomized and ovariectomized mice, incubated with substrate solutions, and compared with the same groups of serum incubated with substrate solutions including cholesterol, 17-beta-estradiol, testosterone, progesterone or hydrocortisone. Our results demonstrated highly significant sex differences, and an influence of cholesterol and steroid hormones on aminopeptidase activity. Depending on the nature of the aminopeptidase, these enzymes responded in different ways to the presence of these substances and also responded differently to gonadectomy. For alanyl-aminopeptidase activity, but not for glutamyl-aminopeptidase activity, there was a clear difference in response between males and females to incubation of the serum with steroid hormones. PMID:9864071

Martinez, J M; Ramirez, M J; Prieto, I; Alba, F; Ramirez, M

1998-01-01

247

[Anticoagulant activity of arabinogalactane sulfate and cedar bark extract studied in vitro].  

PubMed

We have studied in vitro the ability of the Siberian cedar crust (SCC) extract (Pinus sibirica Du Tour) and arabinogalactan sulphate (AGS) extracted from wood of Siberiam pine-tree (Larix sibirica Ledeb.) to increase the human blood plasma coagulation time and also to inhibit the amydolytic activity of thrombin (aIIa) and the coagulation factor Xa (aXa). A method has been developed by means of which SCC increases the aXa activity by a factor of 3.7 and the aIIŕ activity by a factor of 2.5. The AGS preparation increased the blood plasma coagulation time in the test for activated partial thromboplastin time. An effective concentration, at which the time of plasma coagulation was increased by a factor of 2 (in comparison to the control) was 2.94 +/- 0.33 mg/ml. AGS did not exhibit the ability to inhibit the Xa activity. PMID:18819438

Drozd, N N; Kuznetsova, S A; Lapikova, E S; Davydova, A I; Makarov, V A; Kuznetsov, B N; Butylkina, A I; Vasil'eva, N Iu; Skvortsova, G P

2008-01-01

248

Activation of c-Raf-1 by Ras and Src through different mechanisms: activation in vivo and in vitro.  

PubMed Central

The c-Raf-1 protein kinase plays a critical role in intracellular signaling downstream from many tyrosine kinase and G-protein-linked receptors. c-Raf-1 binds to the proto-oncogene Ras in a GTP-dependent manner, but the exact mechanism of activation of c-Raf-1 by Ras is still unclear. We have established a system to study the activation of c-Raf-1 in vitro. This involves mixing membranes from cells expressing oncogenic H-RasG12V, with cytosol from cells expressing epitope-tagged full-length wild-type c-Raf-1. This results in a fraction of the c-Raf-1 binding to the membranes and a concomitant 10- to 20-fold increase in specific activity. Ras was the only component in these membranes required for activation, as purified recombinant farnesylated K-Ras.GTP, but not non-farnesylated K-Ras.GTP or farnesylated K-Ras.GDP, was able to activate c-Raf-1 to the same degree as intact H-RasG12V membranes. The most potent activation occurred under conditions in which phosphorylation was prohibited. Under phosphorylation-permissive conditions, activation of c-Raf-1 by Ras was substantially inhibited. Consistent with the results from other groups, we find that the activation of c-Raf-1 by Src in vivo occurs concomitant with tyrosine phosphorylation on c-Raf-1, and in vitro, activation of c-Raf-1 by Src requires the presence of ATP. Therefore we propose that activation of c-Raf-1 by Ras or by Src occurs through different mechanisms. PMID:9171352

Stokoe, D; McCormick, F

1997-01-01

249

Arsenic trioxide and reduced glutathione act synergistically to augment inhibition of thyroid peroxidase activity in vitro.  

PubMed

Thyroid peroxidase (TPO) is the enzyme involved in thyroid hormone synthesis. Arsenic trioxide (As2O3) is known to inhibit TPO activity in vitro. This inhibition is believed to occur when As2O3 binds to TPO's free sulfhydryl groups. Reduced glutathione (GSH) is also known to inhibit TPO activity in vitro. This inhibition may occur because GSH acts as a competitive substrate for hydrogen peroxide, or possibly reduce the oxidized form of iodide, requirements for TPO action. On the other hand, one could speculate that GSH reduces arsenic-induced TPO inhibition by interacting directly with arsenic or TPO, consequently limiting arsenic's ability to inhibit TPO activity. Since GSH is known to inhibit thyroid hormone synthesis while at the same time it is also known to be an important antioxidant preventing cellular damage induced by oxidative stress and protecting the thyroid gland from oxidative damage induced by arsenic, we wanted to determine if a combination of As2O3 and reduced GSH would either attenuate or augment the As2O3-induced inhibition on TPO activity. Using an in vitro system, TPO was assayed spectrophotometrically in the presence of As2O3 (0.01, 0.1, 1, and 10 ppm), GSH (0.1, 1, 5, and 10 ppm), and As2O3 (0.1 ppm) and GSH (0.01, 0.1, 1, or 10 ppm) combinations. Our results show that 0.1, 1.0, and 10 ppm As2O3 inhibit TPO activity. Similarly, 5 and 10 ppm GSH also inhibit TPO activity. When 0.1 ppm As2O3 (i.e., the lowest dose of arsenic able to partially inhibit TPO activity) is combined with 0.01, 0.1, 1.0, or 10 ppm GSH inhibition of in vitro TPO activity is augmented as indicated by complete inhibition of TPO. The mechanism of this augmentation and whether it translates to living systems remains unclear. PMID:25595679

Palazzolo, Dominic L; Ely, Emily A

2015-05-01

250

A humanized anti-M2 scFv shows protective in vitro activity against influenza  

SciTech Connect

M2 is one of the most conserved influenza proteins, and has been widely prospected as a potential universal vaccine target, with protection predominantly mediated by antibodies. In this paper we describe the creation of a humanized single chain Fv from 14C2, a potent monoclonal antibody against M2. We show that the humanized scFv demonstrates similar activity to the parental mAb: it is able to recognize M2 in its native context on cell surfaces and is able to show protective in vitro activity against influenza, and so represents a potential lead antibody candidate for universal prophylactic or therapeutic intervention in influenza.

Bradbury, Andrew M [Los Alamos National Laboratory; Velappan, Nileena [Los Alamos National Laboratory; Schmidt, Jurgen G [Los Alamos National Laboratory

2008-01-01

251

Effect of Nano red elemental selenium on GPx activity of broiler chick kidney cells in vitro  

Microsoft Academic Search

A new selenium source, Nano red elemental selenium (Nano-Se) was used to study the effect on the GPx activity of broiler chick\\u000a kidney cells (BCKC)in vitro, Sodium selenite (Na2SeO3) and seleno-1-methionine (Se-Met) were used as the controls. The results showed that the effects of three kinds of Se forms\\u000a on the GPx activity of BCKC were accordant (p>0.05) compared with

Xu Bao-hua; Xu Zi-rong; Xia Mei-sheng; Hu Cai-hong; Deng Yue-song; Xiong Li

2003-01-01

252

Activation of human mononuclear cells by porcine biologic meshes in vitro  

Microsoft Academic Search

Introduction  While porcine-based biologic meshes are increasingly used for hernia repair, little data exist on tissue responses to such\\u000a products. Host foreign body reaction, local inflammation, and wound healing are principally controlled by monocytes\\/macrophages\\u000a (M\\/MŘs). Exaggerated activation of M\\/MŘs may deleteriously influence mesh integration and remodeling. We hypothesized that\\u000a common porcine meshes induce the differential activation of M\\/MŘs in vitro.\\u000a \\u000a \\u000a \\u000a \\u000a Materials

S. B. Orenstein; Y. Qiao; U. Klueh; D. L. Kreutzer; Y. W. Novitsky

2010-01-01

253

In vitro antifungal activity of phenylheptatriyne from Bidens cernua L. against yeasts.  

PubMed

In vitro antifungal activity of phenylheptatriyne from Bidens cernua L. (Asteraceae) was studied using broth macrodilution method against 125 strains of yeasts including 104 clinical and other isolates of Candida spp. (C. albicans, C. krusei, C. tropicalis, C. guilliermondii, C. parapsilosis, C. glabrata, C. inconspicua), 16 strains of basidiomycetous yeasts (Cryptococcus neoformans, C. albidus, Trichosporon cutaneum, Rhodotorula glutinis) and five standard reference strains of Candida species. Phenylheptatriyne has shown significant activity against investigated strains, and the Minimal Inhibitory Concentrations for Candida spp. were determined as 12.5-50 microg/ml and for basidiomycetous yeasts as 12.5-100 microg/ml. PMID:19837144

Rybalchenko, N P; Prykhodko, V A; Nagorna, S S; Volynets, N N; Ostapchuk, A N; Klochko, V V; Rybalchenko, T V; Avdeeva, L V

2010-07-01

254

In vitro screening of antifungal activity of marine sponge extracts against five phytopathogenic fungi.  

PubMed

The aim of our research is the screening of extracts of marine sponges for their antifungal activity against phytopathogenic fungi. The in vitro screening of hydroalcoholic and organic extracts of ten marine sponges from Atlantic coast of Morocco against five phytopathogenic fungi (Fusarium oxysporum f.sp. melonis, Fusarium oxysporum f.sp. radicis-lycopersici, Fusarium oxysporum f.sp. ciceris, Botrytis cinerea and Penicillium digitatum) showed that only two sponges (Haliclona viscosa and Cynachirella tarentina) are active against all phytopathogenic fungi studied. PMID:25392799

El Amraoui, Belkassem; El Wahidi, Majida; Fassouane, Aziz

2014-01-01

255

Qushi Huayu Decoction Inhibits Hepatic Lipid Accumulation by Activating AMP-Activated Protein Kinase In Vivo and In Vitro  

PubMed Central

Qushi Huayu Decoction (QHD), a Chinese herbal formula, has been proven effective on alleviating nonalcoholic fatty liver disease (NAFLD) in human and rats. The present study was conducted to investigate whether QHD could inhibit hepatic lipid accumulation by activating AMP-activated protein kinase (AMPK) in vivo and in vitro. Nonalcoholic fatty liver (NAFL) model was duplicated with high-fat diet in rats and with free fatty acid (FFA) in L02 cells. In in vivo experimental condition, QHD significantly decreased the accumulation of fatty droplets in livers, lowered low-density lipoprotein cholesterol (LDL-c), alanine aminotransferase (ALT), and aspartate aminotransferase (AST) levels in serum. Moreover, QHD supplementation reversed the HFD-induced decrease in the phosphorylation levels of AMPK and acetyl-CoA carboxylase (ACC) and decreased hepatic nuclear protein expression of sterol regulatory element-binding protein-1 (SREBP-1) and carbohydrate-responsive element-binding protein (ChREBP) in the liver. In in vitro, QHD-containing serum decreased the cellular TG content and alleviated the accumulation of fatty droplets in L02 cells. QHD supplementation reversed the FFA-induced decrease in the phosphorylation levels of AMPK and ACC and decreased the hepatic nuclear protein expression of SREBP-1 and ChREBP. Overall results suggest that QHD has significant effect on inhibiting hepatic lipid accumulation via AMPK pathway in vivo and in vitro. PMID:23573117

Feng, Qin; Gou, Xiao-jun; Meng, Sheng-xi; Huang, Cheng; Zhang, Yu-quan; Tang, Ya-jun; Wang, Wen-jing; Xu, Lin; Peng, Jing-hua; Hu, Yi-yang

2013-01-01

256

In vitro antiprotozoal activity of extracts of five Turkish Lamiaceae species.  

PubMed

The in vitro antiprotozoal activities of crude methanolic extracts from the aerial parts of five Lamiaceae plants (Salvia tomentosa, S. sclarea, S. dichroantha, Nepeta nuda subsp. nuda and Marrubium astracanicum subsp. macrodon) were evaluated against four parasitic protozoa, i.e. Trypanosoma brucei rhodesiense, T. cruzi, Leishmania donovani and Plasmodium falciparum. The cytotoxic potentials of the extracts on L6 cells were also evaluated. Melarsoprol, benznidazole, miltefosine, chloroquine and podophyllotoxin were used as reference drugs. All crude MeOH extracts showed antiprotozoal potential against at least three parasites, so they were dispersed in water and partitioned against n-hexane and chloroform to yield three subextracts that were screened in the same test systems. The n-hexane extract of N. nuda was the most active against T. brucei rhodesiense while the CHCl3 extracts of S. tomentosa and S. dichroantha showed significant activity against L. donovani. All organic extracts displayed in vitro antimalarial and moderate trypanocidal activities against T. cruzi with the n-hexane extract of S. sclarea being the most active against the latter. The extracts displayed low or no cytotoxicity towards mammalian L6 cells. PMID:22224291

Kirmizibekmez, Hasan; Atay, Irem; Kaiser, Marcel; Yesilada, Erdem; Tasdemir, Deniz

2011-11-01

257

In vitro ovicidal and larvicidal activity of Agave sisalana Perr. (sisal) on gastrointestinal nematodes of goats.  

PubMed

This study describes the in vitro anthelmintic activity of aqueous extracts (AE), ethyl acetate extracts (EE), flavonoid fractions (FF) and saponin fractions (SF) obtained from sisal waste (Agave sisalana) against gastrointestinal nematodes of goats. The activity of these extracts was evaluated by performing inhibition of egg hatch (EHA) and larval migration (LMI) assays. The EC(50) results of the EHA corresponded to 4.7, 0.1 and 0.05 mg/mL for EE, EA and FF, respectively. The SF fraction showed no ovicidal activity. The percent efficacies that were observed for the LMI were 50.3, 33.2 and 64.1% for the AE, EE and SF, respectively. The FF fraction did not show activity against the larvae. The analysis of the FF fraction indicates the presence of a homoisoflavonoid. This report suggests that the A. sisalana has activity in vitro against gastrointestinal nematodes of goats. This effect is likely related to the presence of homoisoflavonoid and saponin compounds, which have different actions for specific stages of nematode development. PMID:23146415

Botura, Mariana B; dos Santos, Jener David G; da Silva, Gisele D; de Lima, Hélimar G; de Oliveira, Joăo Victor A; de Almeida, Maria Angela O; Batatinha, Maria José M; Branco, Alexsandro

2013-02-18

258

Newly Designed and Synthesized Curcumin Analogs with in vitro Cytotoxicity and Tubulin Polymerization Activity.  

PubMed

Novel curcumin analogs with 4-piperidone ring were designed, synthesized, and evaluated for their cytotoxic activities against five different cancer cell lines. 3,5-bis(4-Hydroxy-3-methoxybenzylidene)-4-oxo-N-phenylpiperidine-1-carbothioamide (XIIe) exhibited considerable cytotoxic activity with IC50 values in 1-2.5 ?m range. In silico and in vitro, studies were also performed to predict the binding affinity of the target compounds to the ?-chain of tubulin receptor (PDB code 1SA1) and their abilities to affect microtubules polymerization cycle. 3,5-bis(3-Iodo-5-methoxy-4-propoxybenzylidene)-N-acetylpiperidin-4-one (VIIa) was found to exert 93.3% inhibition of tubulin and destabilization of microtubules in vitro compared to vincristine while, 3,5-bis(3,4,5-trimethoxybenzylidene)-N-benzoylpiperidin-4-one (XIIc) showed high potency in a different way where it exerted 94.8% stabilization of microtubules in vitro compared to positive control paclitaxel. PMID:25352318

Fawzy, Iten M; Youssef, Khairia M; Ismail, Nasser S M; Gullbo, Joachim; Abouzid, Khaled A M

2014-10-28

259

Specialization of the DNA-Cleaving Activity of a Group I Ribozyme Through In Vitro Evolution  

NASA Technical Reports Server (NTRS)

In an earlier study, an in vitro evolution procedure was applied to a large population of variants of the Tetrahymena group 1 ribozyme to obtain individuals with a 10(exp 5)-fold improved ability to cleave a target single-stranded DNA substrate under simulated physiological conditions. The evolved ribozymes also showed a twofold improvement, compared to the wild-type, in their ability to cleave a single-stranded RNA substrate. Here, we report continuation of the in vitro evolution process using a new selection strategy to achieve both enhanced DNA and diminished RNA-cleavage activity. Our strategy combines a positive selection for DNA cleavage with a negative selection against RNA binding. After 36 "generations" of in vitro evolution, the evolved population showed an approx. 100-fold increase in the ratio of DNA to RNA-cleavage activity. Site-directed mutagenesis experiment confirmed the selective advantage of two covarying mutations within the catalytic core of ribozyme that are largely responsible for this modified behavior. The population of ribozymes has now undergone a total of 63 successive generations of evolution, resulting in an average 28 mutations relative to the wild-type that are responsible for the altered phenotype.

Tsang, Joyce; Joyce, Gerald F.

1996-01-01

260

In Vitro Reconstitution of the Complete Clostridium thermocellum Cellulosome and Synergistic Activity on Crystalline Cellulose  

PubMed Central

Artificial cellulase complexes active on crystalline cellulose were reconstituted in vitro from a native mix of cellulosomal enzymes and CipA scaffoldin. Enzymes containing dockerin modules for binding to the corresponding cohesin modules were prepared from culture supernatants of a C. thermocellum cipA mutant. They were reassociated to cellulosomes via dockerin-cohesin interaction. Recombinantly produced mini-CipA proteins with one to three cohesins either with or without the carbohydrate-binding module (CBM) and the complete CipA protein were used as the cellulosomal backbone. The binding between cohesins and dockerins occurred spontaneously. The hydrolytic activity against soluble and crystalline cellulosic compounds showed that the composition of the complex does not seem to be dependent on which CipA-derived cohesin was used for reconstitution. Binding did not seem to have an obvious local preference (equal binding to Coh1 and Coh6). The synergism on crystalline cellulose increased with an increasing number of cohesins in the scaffoldin. The in vitro-formed complex showed a 12-fold synergism on the crystalline substrate (compared to the uncomplexed components). The activity of reconstituted cellulosomes with full-size CipA reached 80% of that of native cellulosomes. Complexation on the surface of nanoparticles retained the activity of protein complexes and enhanced their stability. Partial supplementation of the native cellulosome components with three selected recombinant cellulases enhanced the activity on crystalline cellulose and reached that of the native cellulosome. This opens possibilities for in vitro complex reconstitution, which is an important step toward the creation of highly efficient engineered cellulases. PMID:22522677

Krauss, Jan; Zverlov, Vladimir V.

2012-01-01

261

Modulation of Activity of Moloney Murine Leukemia Virus Preintegration Complexes by Host Factors In Vitro  

PubMed Central

We have explored the requirements for host proteins in the integration of Moloney murine leukemia virus (MoMuLV) cDNA in vitro. Following infection, it is possible to lyse cells and obtain preintegration complexes (PICs) capable of integrating the MoMuLV cDNA into an added target DNA in vitro (intermolecular integration). PICs can be stripped of required proteins by gel filtration in high-salt buffers (600 mM KCl), allowing the nature of the removed factors to be investigated by in vitro reconstitution. In a previous study of human immunodeficiency virus type 1 (HIV-1) PICs, the host protein HMG I(Y) was found to be able to restore activity to salt-stripped PICs. In contrast, salt stripping and reconstitution of MoMuLV PICs led to the proposal that a host factor is important for a different activity, blocking integration into the cDNA itself (autointegration). In this report, we investigated reconstitution of salt-stripped MoMuLV PICs and found that addition of cellular extract from uninfected NIH 3T3 cells could block autointegration and also restore intermolecular integration. Isolation of the intermolecular integration-complementing activity yielded HMG I(Y), as in the HIV-1 case. However, HMG I(Y) could not block autointegration, implicating a different host factor in this process. Additionally, when MoMuLV PICs were partially purified but not salt stripped, the intermolecular integration activity was reduced but could be stimulated by the addition of any of several purified DNA binding proteins. In summary, three activities were detected: (i) the intermolecular integration cofactor HMG I(Y), (ii) an autointegration barrier protein, and (iii) stimulatory DNA binding proteins. PMID:9499068

Li, Ling; Farnet, Chris M.; Anderson, W. French; Bushman, Frederic D.

1998-01-01

262

In vitro reconstitution of the complete Clostridium thermocellum cellulosome and synergistic activity on crystalline cellulose.  

PubMed

Artificial cellulase complexes active on crystalline cellulose were reconstituted in vitro from a native mix of cellulosomal enzymes and CipA scaffoldin. Enzymes containing dockerin modules for binding to the corresponding cohesin modules were prepared from culture supernatants of a C. thermocellum cipA mutant. They were reassociated to cellulosomes via dockerin-cohesin interaction. Recombinantly produced mini-CipA proteins with one to three cohesins either with or without the carbohydrate-binding module (CBM) and the complete CipA protein were used as the cellulosomal backbone. The binding between cohesins and dockerins occurred spontaneously. The hydrolytic activity against soluble and crystalline cellulosic compounds showed that the composition of the complex does not seem to be dependent on which CipA-derived cohesin was used for reconstitution. Binding did not seem to have an obvious local preference (equal binding to Coh1 and Coh6). The synergism on crystalline cellulose increased with an increasing number of cohesins in the scaffoldin. The in vitro-formed complex showed a 12-fold synergism on the crystalline substrate (compared to the uncomplexed components). The activity of reconstituted cellulosomes with full-size CipA reached 80% of that of native cellulosomes. Complexation on the surface of nanoparticles retained the activity of protein complexes and enhanced their stability. Partial supplementation of the native cellulosome components with three selected recombinant cellulases enhanced the activity on crystalline cellulose and reached that of the native cellulosome. This opens possibilities for in vitro complex reconstitution, which is an important step toward the creation of highly efficient engineered cellulases. PMID:22522677

Krauss, Jan; Zverlov, Vladimir V; Schwarz, Wolfgang H

2012-06-01

263

In vitro assays for assessment of androgenic and estrogenic activity of defined mixtures and complex environment samples  

EPA Science Inventory

Point sources of potentially endocrine active compounds to aquatic environments such as waste water treatment plants, pulp and paper mills, and animal feeding operations invariably contain complex mixtures of chemicals. The current study investigates the use of targeted in vitro ...

264

Rapeseed polysaccharides as prebiotics on growth and acidifying activity of probiotics in vitro.  

PubMed

In vitro digestibility, prebiotic activity and chemical composition of polysaccharides from rapeseed were deliberately studied in this paper. After preliminary treatments, two fractions of polysaccharides (RP1 and RP2) were obtained after purification by DEAE-cellulose and Sephadex G-100. Their primary structural feature and molecule weights were characterized. Furthermore, their digestibility was also evaluated by artificial gastric juice and ?-amylase. Finally, their proliferative effect on bifidobacteria and lactobacilli and acid production of the resulting probiotics in vitro were investigated. The results showed that RP1 and RP2 were homogeneously protein-bound polysaccharides with molecular weights of 28.51 and 6.55kDa, respectively. They were resistant to hydrolysis by artificial gastric juice and ?-amylase. Moreover, they could also significantly stimulate the tested probiotics to proliferate and produce organic acids. These findings clearly suggest the polysaccharides from rapeseed are potential to be exploited as novel prebiotics. PMID:25857979

Wang, Xiao; Huang, Meiying; Yang, Fan; Sun, Hanju; Zhou, Xianxuan; Guo, Ying; Wang, Xiaoli; Zhang, Manli

2015-07-10

265

Characterization of calcium responses and electrical activity in differentiating mouse neural progenitor cells in vitro.  

PubMed

In vitro methods for developmental neurotoxicity (DNT) testing have the potential to reduce animal use and increase insight into cellular and molecular mechanisms underlying chemical-induced alterations in the development of functional neuronal networks. Mouse neural progenitor cells (mNPCs) differentiate into nervous system-specific cell types and have proven valuable to detect DNT using biochemical and morphological techniques. We therefore investigated a number of functional neuronal parameters in primary mNPCs to explore their applicability for neurophysiological in vitro DNT testing. Immunocytochemistry confirmed that mNPCs express neuronal, glial, and progenitor markers at various differentiation durations (1, 7, 14, and 21 days). Because intracellular calcium ([Ca(2+)]i) plays an essential role in neuronal development and function, we measured stimulus-evoked changes in [Ca(2+)]i at these differentiation durations using the Ca(2+)-responsive dye Fura-2. Increases in [Ca(2+)]i (averages ranging from 65 to 226 nM) were evoked by depolarization, ATP, l-glutamic acid, acetylcholine, and dopamine (up to 87%, 57%, 93%, 28%, and 37% responding cells, respectively) and to a lesser extent by serotonin and gamma-aminobutyric acid (both up to 10% responding cells). Notably, the changes in percentage of responsive cells and their response amplitudes over time indicate changes in the expression and functionality of the respective neurotransmitter receptors and related calcium signaling pathways during in vitro differentiation. The development of functional intercellular signaling pathways was confirmed using multielectrode arrays, demonstrating that mNPCs develop electrical activity within 1-2 weeks of differentiation (55% active wells at 14 days of differentiation; mean spike rate of 1.16 spikes/s/electrode). The combined data demonstrate that mNPCs develop functional neuronal characteristics in vitro, making it a promising model to study chemical-induced effects on the development of neuronal function. PMID:24241723

de Groot, Martje W G D M; Dingemans, Milou M L; Rus, Katinka H; de Groot, Aart; Westerink, Remco H S

2014-02-01

266

In vitro antibacterial activity of faeriefungin, a new broad-spectrum polyene macrolide antibiotic.  

PubMed Central

The in vitro activity of faeriefungin, a new pentaene macrolide lactone antibiotic produced by Streptomyces griseus var. autotrophicus, against 263 clinical bacterial isolates was examined. In contrast to the related fungicidal antibiotics nystatin and amphotericin B, which show no activity against bacteria, faeriefungin showed bactericidal activity against all species of gram-positive bacteria examined. MICs for these species ranged from 8 to 64 micrograms/ml, and the MIC for 90% of the isolates tested was 32 micrograms/ml. Isolates of some fastidious gram-negative species, including Neisseria gonorrhoeae, N. meningitidis, and Haemophilus influenzae, were slightly susceptible to faeriefungin, with MICs ranging from 16 to 128 micrograms/ml, but all members of the families Enterobacteriaceae and Pseudomonadaceae, with the exception of Pseudomonas cepacia, were completely resistant to faeriefungin at the concentrations tested. Faeriefungin is also active against fungi, nematodes, and mosquito larvae. The mode of action of faeriefungin against both bacteria and fungi is under investigation. PMID:2126689

Mulks, M H; Nair, M G; Putnam, A R

1990-01-01

267

Medicinal activities of the leaves of Musa sapientum var. sylvesteris in vitro  

PubMed Central

Objective This study is to investigate the medicinal value of methanolic extract of the leaves of Musa sapientum var. sylvesteris in Bangladesh. Methods Several biochemical assays, thin layer chormatogarphy and ultra-violet spectroscopy were used to detect the presence of various types of compounds in this extract. Antioxidant effects were measured by DPPH scavenging assay, total reducing assay and hydrogen peroxide scavenging assay. Receptor binding activities and hydrogen peroxide induced hemolysis assay were performed by hemagglutination assay and hemolysis assay using erythrocytes. Disk diffusion assay was performed to show the antibacterial effect of the extract. Results Methanolic extract of the leaves showed antioxidant and antibacterial activity in vitro. The extract showed hemaglutination inhibition activities and hydrogen peroxide induced hemolysis inhibition activity of human red blood cells. Conclusion Musa sapientum var. sylvesteris can be an useful medicinal plant. PMID:23730561

Sahaa, Repon Kumer; Acharyaa, Srijan; Shovon, Syed Sohidul Haque; Royb, Priyanka

2013-01-01

268

Preparation of rotenone derivatives and in vitro analysis of their antimalarial, antileishmanial and selective cytotoxic activities.  

PubMed

Six derivatives of the known biopesticide rotenone were prepared by several chemical transformations. Rotenone and its derivatives showed differential in vitro antiparasitic activity and selective cytotoxicity. In general, compounds were more active against Plasmodium falciparum than Leishmania panamensis. Rotenone had an EC50 of 19.0 µM against P. falciparum, and 127.2 µM against L. panamensis. Although chemical transformation does not improve its biological profile against P. falciparum, three of its derivatives showed a significant level of action within an adequate range of activity with EC50 values < 50.0 µM. This antiplasmodial activity was not due to red blood cell hemolysis, since LC50 was >400 µM. On the other hand, all derivatives displayed a non-specific cytotoxicity on several cell lines and primary human cell cultures. PMID:25412039

Upegui, Yulieth; Gil, Juan F; Quińones, Wiston; Torres, Fernando; Escobar, Gustavo; Robledo, Sara M; Echeverri, Fernando

2014-01-01

269

The evaluation of nitric oxide scavenging activity of certain herbal formulations in vitro: a preliminary study.  

PubMed

The nitric oxide (NO) scavenging activities of traditional polyherbal drugs like abana, chyavanaprasha, geriforte, septilin, mentat and triphala were examined using sodium nitroprusside as a NO donor in vitro. All the drugs tested demonstrated direct scavenging of NO and were superior to Gingko biloba, which was used as a positive control. The extracts of various polyherbal drugs exhibited dose-dependent NO scavenging activities and the potency was in the following order: abana > chyavanaprasha > triphala > geriforte > septilin > mentat > Gingko biloba. The present results suggest that the traditional Indian polyherbal crude drugs may be potent and novel therapeutic agents for scavenging of NO, and thereby inhibit the pathological conditions caused by excessive generation of NO and its oxidation product, peroxynitrite. These findings may also help to explain, at least in part, the pharmacological activities like rejuvenating, adaptogenic, anti-infection, anti-inflammatory, cardioprotective and neuroprotective activities of these traditional, clinically used non toxic drugs. PMID:15305317

Jagetia, Ganesh Chandra; Rao, Shaival Kamalaksh; Baliga, Manjeshwar Shrinath; S Babu, Kiran

2004-07-01

270

Composition and in vitro anticancer activities of the leaf essential oil of Neolitsea variabillima from Taiwan.  

PubMed

This study investigated the chemical composition and in vitro anticancer activities of the essential oil isolated from the leaf of Neolitsea variabillima. The essential oil was isolated using hydrodistillation in a Clevenger-type apparatus, and characterized by GC-FID and GC-MS. Sixty-seven compounds were identified, representing 100% of the oil. The main components identified were trans-beta-ocimene (13.4%), alpha-cadinol (10.5%), terpinen-4-ol (9.3%), tau-cadinol (9.2%), beta-caryophyllene (8.8%), and sabinene (6.7%). The anticancer activities of oil were evaluated. The results showed that the oil exhibited cytotoxic activity against human oral, liver, lung, colon, melanoma, and leukemic cancer cells. The presence of beta-caryophyllene, tau-cadinol, and alpha-cadinol significantly contributed to the anticancer activities of N. variabillima leaf oil. PMID:23738472

Su, Yu-Chang; Hsu, Kuan-Ping; Wang, Eugene I-Chen; Ho, Chen-Lung

2013-04-01

271

In-vitro antiproliferative activity of benzopyranone derivatives in comparison with standard chemotherapeutic drugs.  

PubMed

The cytotoxic activities of five new benzopyranone derivatives containing basic amino side chain are described. Their cytotoxicities against ER(+) MCF-7 and ER(-) MDA-MB-231 human breast cancer cell lines, and Ishikawa human endometrial cell line were determined after 72 h drug exposure employing CellTiter-Glo assay at concentrations ranging from 0.01-1.0 × 10(5) nM. The antiproliferative activities of these compounds were compared to tamoxifen (TAM), 4-hydroxytamoxifen (4-OHT, active metabolite of tamoxifen), and raloxifene (RAL). In-vitro results indicated that compounds 9, 10, 12, and 13 were more potent than TAM against the human breast cancer cell lines with IC(50) ?activity relationships of these compounds and their binding mode within the estrogen receptor (ER) binding site using AutoDock vina are discussed. PMID:21290426

Musa, Musiliyu A; Cooperwood, John S; Khan, M Omar F; Rahman, Taufiq

2011-02-01

272

Molecular analysis of human papillomavirus virus-like particle activated langerhans cells in vitro.  

PubMed

Langerhans cells (LC) are the resident antigen-presenting cells in human epithelium, and are therefore responsible for initiating immune responses against human papillomaviruses (HPV) entering the epithelial and mucosal layers in vivo. Upon proper pathogenic stimulation, LC become activated causing an internal signaling cascade that results in the up-regulation of co-stimulatory molecules and the release of inflammatory cytokines. Activated LC then migrate to lymph nodes where they interact with antigen-specific T cells and initiate an adaptive T-cell response. However, HPV manipulates LC in a suppressive manner that alters these normal maturation responses. Here, in vitro LC activation assays for the detection of phosphorylated signaling intermediates, the up-regulation of activation-associated surface markers, and the release of inflammatory cytokines in response to HPV particles are described. PMID:25348303

Woodham, Andrew W; Raff, Adam B; Da Silva, Diane M; Kast, W Martin

2015-01-01

273

In vitro antioxidant and cytotoxic activities of essential oil of Feronia elephantum Correa  

PubMed Central

Objective To analyse the chemical composition and evaluation of antioxidant, cytotoxic and DNA fragmentation activities of essential oil of Feronia elephantum Correa. Methods Chemical composition analysis of hydrodistilled essential oil was determined by gas chromatography-mass spectrometry and in vitro antioxidant activity of oil was determined by DPPH free radical, hydroxyly radical scavenging, metal chelating and prevention of deoxyribose degradation. Cytotoxicity and DNA fragmentation activities against breast cancer cells (MCF-7) were also analyzed. Results Gas chromatography-mass spectrometry analysis revealed the presence of 24 compounds with caryophyllene oxide (62.29%) as major compound. A considerable antioxidant, cyotoxic and DNA fragmentation activities of oils was observed. Conclusions The result of this study clearly indicates oil could be useful for food preservation and preparation. PMID:25182553

Thirugnanasampandan, Ramaraj; David, Delma

2014-01-01

274

In vitro antiplasmodial activity of crude extracts of Tetrapleura tetraptera and Copaifera religiosa  

PubMed Central

Background Malaria remains a major public health problem, especially in tropical and subtropical regions because of the emergence and widespread of antimalarial drug resistance. Traditional medicine represents one potential source of new treatments. Here, we investigated the in vitro antiplasmodial activity of bark extracts from two Fabaceae species (Tetrapleura tertaptera and Copaifera religiosa) traditionally used to treat malaria symptoms in Haut-Ogooué province, Gabon. Findings The antiplasmodial activity of dichloromethane and methanolic extracts was tested on P. falciparum strains FCB (chloroquine-resistant) and 3D7 (chloroquine-sensitive) and on fresh clinical isolates, using the DELI method. Host cell toxicity was analyzed on MRC-5 human diploid embryonic lung cells using the MTT test. The dichloromethane extracts of the two plants had interesting activity (IC50 between 8.5 ± 4.7 and 13.4 ± 3.6 ?g/ml). The methanolic extract of Tetrapleura tetraptera was less active (IC50 around 30 ?g/ml) and the methanolic extract of Copaifera religiosa was inactive. The selectivity index (toxicity/antiplasmodial activity) of the dichloromethane extract of Tetrapleura tetraptera was high (around 7), while the dichloromethane extract of Copaifera religiosa had the lowest selectivity (0.6). The mean IC50 values for field isolates were less than 1.5 ?g/ml for dichloromethane extracts of both plants, while methanolic extracts of Tetrapleura tetraptera showed interesting activity (IC50 = 13.1 ?g/ml). The methanolic extract of Copaifera religiosa was also inactive on field isolates. Conclusions Dichloromethane extracts of Tetrapleura tetraptera and Copaifera religiosa, two plants used to treat malaria in Gabon, had interesting antiplasmodial activity in vitro. These data provide a scientific rationale for the traditional use of these plants against malaria symptoms. Bioactivity-guided phytochemical analyses are underway to identify the active compounds. PMID:22112366

2011-01-01

275

In vitro activities of amphotericin B deoxycholate and liposomal amphotericin B against 604 clinical yeast isolates  

PubMed Central

We determined the in vitro antifungal activity of liposomal amphotericin B (L-AmB) against 604 clinical yeast isolates. Amphotericin B deoxycholate (D-AmB) was tested in parallel against all the isolates. Susceptibility testing was performed according to the Clinical and Laboratory Standards Institute (CLSI) M27-A3 method. Overall, L-AmB was highly active against the isolates (mean MIC, 0.42 µg ml?1; MIC90, 1 µg ml?1; 97.2?% of MICs were ?1 µg ml?1) and comparable to D-AmB (mean MIC, 0.48 µg ml?1; MIC90, 1 µg ml?1; 97.3?% of MICs were ?1 µg ml?1). The in vitro activity of D-AmB and L-AmB was correlated (R2?=?0.61; exp(b), 2.3; 95?% CI, 2.19–2.44, P<0.001). Candida albicans (mean MICs of D-AmB and L-AmB, 0.39 µg ml?1 and 0.31 µg ml?1, respectively) and Candida parapsilosis (mean MICs of D-AmB and L-AmB, 0.38 µg ml?1 and 0.35 µg ml?1, respectively) were the species most susceptible to the agents tested, while Candida krusei (currently named Issatchenkia orientalis) (mean MICs of D-AmB and L-AmB, 1.27 µg ml?1 and 1.13 µg ml?1, respectively) was the least susceptible. The excellent in vitro activity of L-AmB may have important implications for empirical treatment approaches and support its role in treatment of a wide range of invasive infections due to yeasts. PMID:25210203

Lovero, Grazia; Coretti, Caterina; De Giglio, Osvalda; Martinelli, Domenico; Bedini, Andrea; Delia, Mario; Rosato, Antonio; Codeluppi, Mauro; Caggiano, Giuseppina

2014-01-01

276

In vitro studies on ?-glucosidase inhibition, antioxidant and free radical scavenging activities of Hedyotis biflora L.  

PubMed

Aim of this study was to evaluate the in vitro ?-glucosidase inhibition and antioxidant activity of hexane, ethyl acetate and methanol extracts of Hedyotis biflora L. (Rubiaceae). In in vitro ?-glucosidase inhibition and antioxidant activity, the methanol extract showed potent effect compared to hexane and ethyl acetate extracts. The methanol extract of H. biflora (HBMe) showed 50% ?-glucosidase inhibition at the concentration of 480.20 ± 2.37 ?g/ml. The total phenolic content of HBMe was 206.81 ± 1.11 mg of catechol equivalents/g extract. HBMe showed great scavenging activity on 2,2-diphenyl-picrylhydrazyl (DPPH) (IC(50) 520.21 ± 1.02 ?g/ml), hydroxyl (IC(50) 510.21 ± 1.51 ?g/ml), nitric oxide (IC(50) 690.20 ± 2.13 ?g/ml) and superoxide (IC(50) 510.31 ± 1.45 ?g/ml) radicals, as well as high reducing power. HBMe also showed a strong suppressive effect on lipid peroxidation. Using the ?-carotene method, the scavenging values of HBMe was significantly lower than BHT, and metal chelating ability of HBMe also showed a strong inhibition effect when compared to the reference standard. The active compound ursolic acid from HBMe was identified using various spectroscopical studies. The results obtained in this study clearly indicate that HBMe has a significant potential to use as a natural ?-glucosidase inhibition, antioxidant agent. PMID:23411299

Nimal Christhudas, I V S; Praveen Kumar, P; Sunil, Christudas; Vajravijayan, S; Lakshmi Sundaram, R; Jenifer Siril, S; Agastian, P

2013-06-01

277

Tyrosine, Cysteine, and S-Adenosyl Methionine Stimulate In Vitro [FeFe] Hydrogenase Activation  

PubMed Central

Background [FeFe] hydrogenases are metalloenzymes involved in the anaerobic metabolism of H2. These proteins are distinguished by an active site cofactor known as the H-cluster. This unique [6Fe–6S] complex contains multiple non-protein moieties and requires several maturation enzymes for its assembly. The pathways and biochemical precursors for H-cluster biosynthesis have yet to be elucidated. Principal Findings We report an in vitro maturation system in which, for the first time, chemical additives enhance [FeFe] hydrogenase activation, thus signifying in situ H-cluster biosynthesis. The maturation system is comprised of purified hydrogenase apoprotein; a dialyzed Escherichia coli cell lysate containing heterologous HydE, HydF, and HydG maturases; and exogenous small molecules. Following anaerobic incubation of the Chlamydomonas reinhardtii HydA1 apohydrogenase with S-adenosyl methionine (SAM), cysteine, tyrosine, iron, sulfide, and the non-purified maturases, hydrogenase activity increased 5-fold relative to incubations without the exogenous substrates. No conditions were identified in which addition of guanosine triphosphate (GTP) improved hydrogenase maturation. Significance The in vitro system allows for direct investigation of [FeFe] hydrogenase activation. This work also provides a foundation for studying the biosynthetic mechanisms of H-cluster biosynthesis using solely purified enzymes and chemical additives. PMID:19855833

Kuchenreuther, Jon M.; Stapleton, James A.; Swartz, James R.

2009-01-01

278

Synthesis and in vitro antimycobacterial activity of balofloxacin ethylene isatin derivatives.  

PubMed

A series of novel balofloxacin ethylene isatin derivatives with remarkable improvement in lipophilicity, as compared to the parent compound balofloxacin, were designed, synthesized and characterized by (1)H NMR, MS and HRMS. These derivatives were initially evaluated for their in vitro antimycobacterial activity against M. phlei CMCC 93201 and M. smegmatis CMCC 93202. Compounds 3b, 3d, 3g-j and 3l were chosen for further evaluation their in vitro activity against MTB 09710 clinical isolate, and then compounds 3h and 3g against MTB H37Rv ATCC 27294. All of the synthesized compounds were less active than balofloxacin against M. phlei CMCC 93201 and M. smegmatis CMCC 93202, but compounds 3g-j (MIC: <0.5-8 microg/mL) were more potent than balofloxacin (MIC: 16 microg/mL) against MTB 09710. In particular, compound 3h (MIC: 0.25- < 0.5 microg/mL) was found to be comparable to moxifloxacin, and >or=32 fold more potent than balofloxacin against MTB 09710 and MTB H37Rv ATCC 27294. The results demonstrated that the lipophilicity of the tested compounds was not the sole parameter affecting antimycobacterial activity, as well as the potential and importance of developing new fluoroquinolone derivatives against mycobacterial infections. PMID:20493593

Feng, Lian-Shun; Liu, Ming-Liang; Wang, Bo; Chai, Yun; Hao, Xue-Qin; Meng, Shuai; Guo, Hui-Yuan

2010-08-01

279

In vitro cytotoxicity of mouse macrophages activated by coculture with syngeneic sarcoma cells.  

PubMed

Normal resident peritoneal macrophages from C3D2 (C3H/Tif X DBA/2) F1 mice were activated in vitro by culturing with semisyngeneic tumour cells. The tumour cells originated from a methylcholanthrene-induced sarcoma (MC1M) growing in vivo in ascites form. Macrophage-mediated cytotoxicity was evaluated after 5 days of in vitro culture, using five different target cells. Semisyngeneic (L 929), allogeneic (B16 melanoma), and xenogeneic (HeLa) tumour cell lines and normal allogeneic fibroblast cell lines (3T3, 3T6) were tested. The morphology and kinetics of the cytotoxicity reaction were studied by scanning electron microscopy and compared with release of radioactivity from 14C-thymidine-labelled target cells. The activated macrophages were able to kill the semisyngeneic, allogeneic, and xenogeneic tumour cell lines tested under conditions that did not affect normal fibroblasts. The requirement for T cells during activation of the macrophages was also tested. The cytotoxicity decreased markedly when T cells were removed from the macrophage cultures before activation or when macrophages from nude mice were used in the experiments. PMID:6983715

Olstad, R; Kaplan, G; Seljelid, R

1982-11-01

280

In vitro activity of 23 tea extractions and epigallocatechin gallate against Candida species.  

PubMed

In this study, we investigate the susceptibility of Candida albicans, Candida glabrata, Candida krusei, Candida parapsilosis, Candida tropicalis, and Aspergillus fumigatus using the EUCAST microdilution minimum inhibitory concentration (MIC) method (final tea supernatant concentration range 5.0-0.005 mg/ml) to 23 different teas and tea catechins including epigallocatechin gallate (EGCG) isolated from green tea. All teas exhibited potent in vitro antifungal activity against C. glabrata. Six out of nine green teas and three of eight black teas had an MIC of 0.078 mg/ml, one white tea had an MIC of 0.156 mg/ml, and finally three of five oolong teas had an MIC of 0.156 mg/ml. Three teas exhibited activity against C. albicans (MIC 1.25 mg/ml), one green tea was active against C. parapsilosis (MIC 1.25 mg/ml), but none were effective against C. krusei, C. tropicalis or A. fumigatus at the concentrations tested. The MIC of EGCG was 0.3125 ?g/ml against C. glabrata and 5.0 ?g/ml against C. albicans and C. parapsilosis. The effect was fungicidal against C. glabrata at higher concentrations. In conclusion, EGCG and other yet undefined substances in tea have differential antifungal activity in vitro against C. glabrata, C. albicans and C. parapsilosis. These data indicate that components of tea and EGCG might be useful particularly for the treatment of C. glabrata infections and warrants further investigations. PMID:25605775

Chen, Ming; Zhai, Lin; Arendrup, Maiken Cavling

2015-02-01

281

Kinetic and sensitive analysis of tyrosinase activity using electron transfer complexes: in vitro and intracellular study.  

PubMed

Tyrosinase is an important marker of human diseases such as the neurodegeneration associated with Parkinson's disease and melanoma. Sensitive detection of tyrosinase activity in vitro and inside cells is of great significance to medical diagnostics and skin disorder treatments. With unique photophysical properties, semiconductor quantum dots (QDs) are employed as photoluminescent platforms for various biosensing, in particular for the detection of enzyme activities. In this work, QDs are functionalized with tyrosine and zwitterionic molecules to construct a nanometer-scale scaffold (QD-Tyr conjugate), and this is used to test tyrosinase activity in vitro and inside cells. Tyrosinase oxidizes tyrosine to dopachrome and switches on the electron-transfer access, which relates to fluorescence quenching. High quenching efficiency is achieved by shortening the distance between the electron donors and acceptors, which is attributed to the small size of the conjugated tyrosine. Enzymatic process curves reveal the enhanced enzymatic activity on the conjugated nanoparticle substrate, which leads to highly sensitive detection of tyrosinase (as low as 1 nM). It is also demonstrated that QD-Tyr conjugates can sensitively probe intracellular tyrosinase in melanoma cells, which promises great potential in disease monitoring and medical diagnostics. PMID:25285706

Zhu, Xianglong; Hu, Juan; Zhao, Zhenghuan; Sun, Mingjun; Chi, Xiaoqin; Wang, Xiaomin; Gao, Jinhao

2015-02-01

282

Molecular docking studies and in vitro cholinesterase enzyme inhibitory activities of chemical constituents of Garcinia hombroniana.  

PubMed

Garcinia species are reported to possess antimicrobial, anti-inflammatory, anticancer, anti-HIV and anti-Alzheimer's activities. This study aimed to investigate the in vitro cholinesterase enzyme inhibitory activities of garcihombronane C (1), garcihombronane F (2), garcihombronane I (3), garcihombronane N (4), friedelin (5), clerosterol (6), spinasterol glucoside (7) and 3?-hydroxy lup-12,20(29)-diene (8) isolated from Garcinia hombroniana, and to perform molecular docking simulation to get insight into the binding interactions of the ligands and enzymes. The cholinesterase inhibitory activities were evaluated using acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. In this study, compound 4 displayed the highest concentration-dependent inhibition of both AChE and BChE. Docking studies exhibited that compound 4 binds through hydrogen bonds to amino acid residues of AChE and BChE. The calculated docking and binding energies also supported the in vitro inhibitory profiles of IC50. In conclusion, garcihombronanes C, F, I and N (1-4) exhibited dual and moderate inhibitory activities against AChE and BChE. PMID:25219673

Jamila, Nargis; Yeong, Khaw Kooi; Murugaiyah, Vikneswaran; Atlas, Amir; Khan, Imran; Khan, Naeem; Khan, Sadiq Noor; Khairuddean, Melati; Osman, Hasnah

2015-01-01

283

Comparison of the antiviral activities of alkoxyalkyl and alkyl esters of cidofovir against human and murine cytomegalovirus replication in vitro.  

PubMed

Alkoxyalkyl esters of cidofovir (CDV) have substantially greater antiviral activity and selectivity than unmodified CDV against herpesviruses and orthopoxviruses in vitro. Enhancement of antiviral activity was also noted when cyclic CDV was esterified with alkoxyalkanols. In vitro antiviral activity of the most active analogs against human cytomegalovirus (HCMV) and orthopoxviruses was increased relative to CDV up to 1,000- or 200-fold, respectively. Alkyl chain length and linker structure are important potential modifiers of antiviral activity and selectivity. In this study, we synthesized a series of alkoxyalkyl esters of CDV or cyclic CDV with alkyl chains from 8 to 24 atoms and having linker moieties of glycerol, propanediol, and ethanediol. We also synthesized alkyl esters of CDV which lack the linker to determine if the alkoxyalkyl linker moiety is required for activity. The new compounds were evaluated in vitro against HCMV and murine CMV (MCMV). CDV or cyclic CDV analogs both with and without linker moieties were highly active against HCMV and MCMV, and their activities were strongly dependent on chain length. The most active compounds had 20 atoms esterified to the phosphonate of CDV. Both alkoxypropyl and alkyl esters of CDV provided enhanced antiviral activities against CMV in vitro. Thus, the oxypropyl linker moiety is not required for enhanced activity. CDV analogs having alkyl ethers linked to glycerol or ethanediol linker groups also demonstrated increased activity against CMV. PMID:15673748

Wan, William B; Beadle, James R; Hartline, Caroll; Kern, Earl R; Ciesla, Stephanie L; Valiaeva, Nadejda; Hostetler, Karl Y

2005-02-01

284

In vitro anti-inflammatory activity of Phlebodium decumanum. Modulation of tumor necrosis factor and soluble TNF receptors  

Microsoft Academic Search

The immunomodulatory activity of a standardized water soluble fraction of the fern Phlebodium decumanum (EXPLY-37®) previously shown to have “in vivo” anti-inflammatory activity was analyzed “in vitro”. This extract inhibited tumor necrosis factor (TNF) production by macrophages activated with lipopolysaccharide (LPS) or LPS plus interferon (IFN)-?. In contrast, nitric oxide (NO) and interleukin (IL)-1? production were not affected in the

Carmen Punzón; Antonio Alcaide; Manuel Fresno

2003-01-01

285

?-Crystallin Downregulates the Expression of TNF-? and iNOS by Activated Rat Retinal Microglia in vitro and in vivo  

Microsoft Academic Search

Purpose: Inhibition of microglial activation has become an important strategy to attenuate neurotoxic damage to the central nervous system. We evaluated the effects of ?-crystallin on the production of cytokines in lipopolysaccharides (LPS) and optic nerve injury-activated retinal microglia. Methods: Microglia were collected from retinas of newborn rats, cultured and treated with LPS in vitro. Microglia were also activated by

Nan Wu; Yan-Hua Wang; Hai-Sheng Zhao; Dong-Ning Liu; Xi Ying; Zheng-Qin Yin; Yi Wang

2009-01-01

286

In Vitro Activity of RX-P873 against Enterobacteriaceae, Pseudomonas aeruginosa, and Acinetobacter baumannii.  

PubMed

RX-P873 is a novel antibiotic from the pyrrolocytosine series which exhibits high binding affinity for the bacterial ribosome and broad-spectrum antibiotic properties. The pyrrolocytosines have shown in vitro activity against multidrug-resistant Gram-negative and Gram-positive strains of bacteria known to cause complicated urinary tract, skin, and lung infections, as well as sepsis. Enterobacteriaceae (657), Pseudomonas aeruginosa (200), and Acinetobacter baumannii (202) isolates from North America and Europe collected in 2012 as part of a worldwide surveillance program were tested in vitro by broth microdilution using Clinical and Laboratory Standards Institute (CLSI) methodology. RX-P873 (MIC90, 0.5 ?g/ml) was >32-fold more active than ceftazidime and inhibited 97.1% and 99.5% of Enterobacteriaceae isolates at MIC values of ?1 and ?4 ?g/ml, respectively. There were only three isolates with an MIC value of >4 ?g/ml (all were indole-positive Protea). RX-P873 (MIC50/90, 2/4 ?g/ml) was highly active against Pseudomonas aeruginosa isolates, including isolates which were nonsusceptible to ceftazidime or meropenem. RX-P873 was 2-fold less active against P. aeruginosa than tobramycin (MIC90, 2 ?g/ml; 91.0% susceptible) and colistin (MIC90, 2 ?g/ml; 99.5% susceptible) and 2-fold more potent than amikacin (MIC90, 8 ?g/ml; 93.5% susceptible) and meropenem (MIC90, 8 ?g/ml; 76.0% susceptible). RX-P873, the most active agent against Acinetobacter baumannii (MIC90, 1 ?g/ml), was 2-fold more active than colistin (MIC90, 2 ?g/ml; 97.0% susceptible) and 4-fold more active than tigecycline (MIC90, 4 ?g/ml). This novel agent merits further exploration of its potential against multidrug-resistant Gram-negative bacteria. PMID:25645834

Flamm, Robert K; Rhomberg, Paul R; Jones, Ronald N; Farrell, David J

2015-04-01

287

Evaluation of the in vitro activity of levornidazole, its metabolites and comparators against clinical anaerobic bacteria.  

PubMed

This study evaluated the in vitro anti-anaerobic activity and spectrum of levornidazole, its metabolites and comparators against 375 clinical isolates of anaerobic bacteria, including Gram-negative bacilli (181 strains), Gram-negative cocci (11 strains), Gram-positive bacilli (139 strains) and Gram-positive cocci (44 strains), covering 34 species. Minimum inhibitory concentrations (MICs) of levornidazole, its five metabolites and three comparators against these anaerobic isolates were determined by the agar dilution method. Minimum bactericidal concentrations (MBCs) of levornidazole and metronidazole were measured against 22 strains of Bacteroides fragilis. Levornidazole showed good activity against B. fragilis, other Bacteroides spp., Clostridium difficile, Clostridium perfringens and Peptostreptococcus magnus, evidenced by MIC90 values of 0.5, 1, 0.25, 2 and 1mg/L, respectively. The activity of levornidazole and the comparators was poor for Veillonella spp. Generally, levornidazole displayed activity similar to or slightly higher than that of metronidazole, ornidazole and dextrornidazole against anaerobic Gram-negative bacilli, Gram-positive bacilli and Gram-positive cocci, especially B. fragilis. Favourable anti-anaerobic activity was also seen with levornidazole metabolites M1 and M4 but not M2, M3 or M5. For the 22 clinical B. fragilis strains, MBC50 and MBC90 values of levornidazole were 2mg/L and 4mg/L, respectively. Both MBC50/MIC50 and MBC90/MIC90 ratios of levornidazole were 4, similar to those of metronidazole. Levornidazole is an important anti-anaerobic option in clinical settings in terms of its potent and broad-spectrum in vitro activity, bactericidal property, and the anti-anaerobic activity of its metabolites M1 and M4. PMID:25301712

Hu, Jiali; Zhang, Jing; Wu, Shi; Zhu, Demei; Huang, Haihui; Chen, Yuancheng; Yang, Yang; Zhang, Yingyuan

2014-12-01

288

Determination of in vitro antidiabetic effects, antioxidant activities and phenol contents of some herbal teas.  

PubMed

In this research, some herbal teas and infusions traditionally used in the treatment of diabetes in Turkey, have been studied for their antidiabetic effects on in vitro glucose diffusion and phenolic contents and antioxidant activities. Ten aqueous herbal tea extracts were examined using an in vitro method to determine their effects on glucose movement across the gastrointestinal tract. Total phenol content of herbal teas was analyzed by Folin-Ciocalteu's procedure. Antioxidant activities of herbal teas were evaluated by the effect of extracts on DPPH radical and hydrogen peroxide scavenging. Antioxidant activity was defined as the amount of the sample to decrease the initial DPPH concentration by 50% as efficient concentration, EC50. Antiradical activity [AE] was calculated as 1/EC50. Values were evaluated statistically. Results support the view that none of the herbal teas showed antidiabetic effect on glucose diffusion using in vitro model glucose absorption. Teas were arranged in the order of green tea > peppermint > thyme > black tea > relax tea > absinthium > shrubby blackberry > sage > roselle > olive leaves according to their total phenol contents. Among ten herbal teas, green tea had the highest hydrogen-donating capacity against to DPPH radical. Ranking of the herbal teas with respect to their DPPH radical scavenging activity were green tea > peppermint > black tea > thyme > relax tea > absinthium > roselle > olive leaves > sage > shrubby blackberry. It was determined that adding flavoring substances such as lemon, bergamot, clove and cinnamon, which are commonly used in preparation of black tea in Turkey resulted to have synergistic effect on total antioxidant activities of black and peppermint teas. The highest hydrogen peroxide inhibition value (65.50%) was obtained for green tea at a 250 microl/ml concentration. The H2O2 scavenging activity of herbal teas decreased in the order green tea > peppermint > relax tea > black tea > thyme > olive leaves > sage > absinthium > shrubby blackberry > roselle. In particular, their phenolic compounds and antioxidant activities may be useful for meal planning in type 2 diabetes. They could contribute to sustain plasma antioxidant level because antioxidants present in plants and herbs prevent the development of vascular diseases seen in type 2 diabetes. PMID:18183488

Büyükbalci, Aynur; El, Sedef Nehir

2008-03-01

289

Activities of Psilostachyin A and Cynaropicrin against Trypanosoma cruzi In Vitro and In Vivo  

PubMed Central

In vitro and in vivo activities against Trypanosoma cruzi were evaluated for two sesquiterpene lactones: psilostachyin A and cynaropicrin. Cynaropicrin had previously been shown to potently inhibit African trypanosomes in vivo, and psilostachyin A had been reported to show in vivo effects against T. cruzi, albeit in another test design. In vitro data showed that cynaropicrin was more effective than psilostachyin A. Ultrastructural alterations induced by cynaropicrin included shedding events, detachment of large portions of the plasma membrane, and vesicular bodies and large vacuoles containing membranous structures, suggestive of parasite autophagy. Acute toxicity studies showed that one of two mice died at a cynaropicrin dose of 400 mg/kg of body weight given intraperitoneally (i.p.). Although no major plasma biochemical alterations could be detected, histopathology demonstrated that the liver was the most affected organ in cynaropicrin-treated animals. Although cynaropicrin was as effective as benznidazole against trypomastigotes in vitro, the treatment (once or twice a day) of T. cruzi-infected mice (up to 50 mg/kg/day cynaropicrin) did not suppress parasitemia or protect against mortality induced by the Y and Colombiana strains. Psilostachyin A (0.5 to 50 mg/kg/day given once a day) was not effective in the acute model of T. cruzi infection (Y strain), reaching 100% animal mortality. Our data demonstrate that although it is very promising against African trypanosomes, cynaropicrin does not show efficacy compared to benznidazole in acute mouse models of T. cruzi infection. PMID:23939901

da Silva, Cristiane França; Batista, Denise da Gama Jaen; De Araújo, Julianna Siciliano; Batista, Marcos Meuser; Lionel, Jessica; de Souza, Elen Mello; Hammer, Erica Ripoll; da Silva, Patricia Bernardino; De Mieri, Maria; Adams, Michael; Zimmermann, Stefanie; Hamburger, Matthias; Brun, Reto; Schühly, Wolfgang

2013-01-01

290

Isolation of Polyribosomes and Messenger RNA Active in in Vitro Synthesis of Soybean Seed Proteins  

PubMed Central

Polyribosome preparations containing low proportions of monosomes to polyribosomes have been isolated from developing seeds of Glycine max L. Merrill using a high pH-high KCl buffer. The polyribosomes were functional in in vitro protein synthesis reactions using wheat germ 23,000g supernatant preparations. Results of experiments using aurintricarboxylic acid indicated that most or all of the amino acid incorporation in vitro resulted from the completion of nascent polypeptides associated with the isolated polyribosmes. RNA purified from polyribosome preparations by affinity chromatography on oligo(dT)-cellulose was also active in vitro, and had different Mg and K requirements for translation than did the polyribosomes. Translation of oligo(dT)-cellulose-purified mRNA was inhibited by the addition of 7-methylguanosine 5?-phosphate, suggesting that soybean mRNAs are “capped” at their 5? ends. Some, but not all, of the products of these reactions were identical in electrophoretic mobility to radioactive polypeptides of storage proteins produced in soybean cotyledons grown in culture. ImagesFig. 4Fig. 5 PMID:16660248

Beachy, Roger N.; Thompson, John F.; Madison, James T.

1978-01-01

291

Methyljasmonate displays in vitro and in vivo activity against multiple myeloma cells.  

PubMed

Jasmonates, plant stress hormones, have been demonstrated to be effective in killing various types of cancer cells. We therefore tested if methyljasmonate (MJ) has activity against multiple myeloma (MM) in vitro and in vivo. MM cell lines and primary MM tumour cells responded to MJ in vitro at concentrations that did not significantly affect normal haematopoietic cells, without stroma-mediated resistance. Brief MJ exposures of MM cells caused release of Hexokinase 2 (HK2) from mitochondria, rapid ATP depletion, perturbation of major intracellular signalling pathways, and ensuing mainly apoptotic cell death. Sensitivity to MJ correlated with lower cellular glucose consumption and lactate production, as well as lower intracellular protein levels of HK2, phosphorylated Voltage-dependent anion channel 2/3 (pVDAC2/3) and Aldo-keto reductase family 1 member C1 (AKR1C1), which represent potential biomarkers of responsiveness to MJ treatment, especially as AKR1C1 transcript levels also correlate with clinical outcome in bortezomib- or dexamethasone-treated MM patients. Interestingly, MJ synergized with bortezomib in vitro and prolonged survival of immunocompromised mice harbouring diffuse lesions of MM.1S cells compared to vehicle-treated mice (P = 0·0046). These studies indicate that jasmonates represent a new, promising strategy to treat MM. PMID:22970818

Klippel, Steffen; Jakubikova, Jana; Delmore, Jake; Ooi, Melissa; McMillin, Douglas; Kastritis, Efstathios; Laubach, Jacob; Richardson, Paul G; Anderson, Kenneth C; Mitsiades, Constantine S

2012-11-01

292

In Vitro Cestocidal Activity of Thymol on Mesocestoides corti Tetrathyridia and Adult Worms  

PubMed Central

Nothing is known about the possible effect of thymol or other compounds of essential oils against the adult worms of cestodes. The aim of the present work was to determine in vitro cestodicidal activity of thymol against Mesocestoides corti adult worms. Moreover, the in vitro effect on tetrathyridia was also demonstrated. Tetrathyridia exposed to different concentrations of thymol showed a concentration and time-dependent effect. At lower concentrations, the main change observed was mainly in morphology, with larvae exhibiting an elongation of the body. When tetrathyridia were exposed to higher concentrations, increased surface alterations and damage were detected. The body appeared elongated and flattened, and a complete loss of morphology and microtriches was observed. Thymol was able to kill M. corti tetrathyridia, since following inoculation of treated parasites in mice no parasites could be recovered. The effect on M. corti adult worms was dose and time-dependent. Changes in motility coincide with the tissue damage were observed at the structural and ultrastructural level. Thymol caused severe damages to both developmental stages analyzed. Damages were more significant in fully segmented worms. The data reported in this paper demonstrate a clear in vitro effect of thymol against M. corti tetrathyridia and adult worms. PMID:25258624

Maggiore, M.; Elissondo, M. C.

2014-01-01

293

In vitro and in vivo activity of a novel antifungal small molecule against Candida infections.  

PubMed

Candida is the most common fungal pathogen of humans worldwide and has become a major clinical problem because of the growing number of immunocompromised patients, who are susceptible to infection. Moreover, the number of available antifungals is limited, and antifungal-resistant Candida strains are emerging. New and effective antifungals are therefore urgently needed. Here, we discovered a small molecule with activity against Candida spp. both in vitro and in vivo. We screened a library of 50,240 small molecules for inhibitors of yeast-to-hypha transition, a major virulence attribute of Candida albicans. This screening identified 20 active compounds. Further examination of the in vitro antifungal and anti-biofilm properties of these compounds, using a range of Candida spp., led to the discovery of SM21, a highly potent antifungal molecule (minimum inhibitory concentration (MIC) 0.2-1.6 µg/ml). In vitro, SM21 was toxic to fungi but not to various human cell lines or bacterial species and was active against Candida isolates that are resistant to existing antifungal agents. Moreover, SM21 was relatively more effective against biofilms of Candida spp. than the current antifungal agents. In vivo, SM21 prevented the death of mice in a systemic candidiasis model and was also more effective than the common antifungal nystatin at reducing the extent of tongue lesions in a mouse model of oral candidiasis. Propidium iodide uptake assay showed that SM21 affected the integrity of the cell membrane. Taken together, our results indicate that SM21 has the potential to be developed as a novel antifungal agent for clinical use. PMID:24465737

Wong, Sarah Sze Wah; Kao, Richard Yi Tsun; Yuen, Kwok Yong; Wang, Yu; Yang, Dan; Samaranayake, Lakshman Perera; Seneviratne, Chaminda Jayampath

2014-01-01

294

Goldfish (Carassius auratus L.) possess natural antibodies with trypanocidal activity towards Trypanosoma carassii in vitro.  

PubMed

Natural infection of cyprinids, such as carp, with the extracellular protozoan parasite Trypanosoma carassii can attain up to 100% prevalence and cause significant host morbidity and mortality, particularly in aquaculture settings. Host recovery from T. carassii infection has been shown to be antibody (Immunoglobulin M; IgM)-mediated, conferring long-term immunity in recovered animals upon challenge. To assess the role of IgM in parasite clearance in the goldfish, IgM was purified by PEG-6000 precipitation from goldfish serum collected at 0 (naďve), 21 (peak parasitaemia) and 42 (recovery phase; immune) days post infection (dpi) and used for in vitro assays. Purified IgM from 0, 21, and 42 dpi serum showed dose- and time-dependent trypanocidal activity in vitro. Incubation of T. carassii with 0 dpi IgM showed the greatest reduction in trypanosome numbers after 24 h, followed by 42 dpi IgM, and finally by 21 dpi IgM. The trypanocidal activity of the PEG-purified IgM was abrogated by pre-absorption with parasites in vitro and was affected by temperature. Furthermore, studies using 0 dpi IgM purified using gel permeation chromatography showed increased trypanocidal activity, with complete elimination of parasites after 12 h when incubated with 200 ?g of 0 dpi IgM, or by 24 h when incubated with 80 ?g or 100 ?g of 0 dpi IgM. Lastly, in vivo passive transfer experiments demonstrated that while immune serum or purified IgM from 42 dpi serum conferred protection against a challenge, neither 0 dpi serum or 0 dpi purified IgM conferred protection against challenge with T. carassii. PMID:23333358

Katzenback, Barbara A; Plouffe, Debbie A; Belosevic, Miodrag

2013-05-01

295

In Vitro and In Vivo Activity of a Novel Antifungal Small Molecule against Candida Infections  

PubMed Central

Candida is the most common fungal pathogen of humans worldwide and has become a major clinical problem because of the growing number of immunocompromised patients, who are susceptible to infection. Moreover, the number of available antifungals is limited, and antifungal-resistant Candida strains are emerging. New and effective antifungals are therefore urgently needed. Here, we discovered a small molecule with activity against Candida spp. both in vitro and in vivo. We screened a library of 50,240 small molecules for inhibitors of yeast-to-hypha transition, a major virulence attribute of Candida albicans. This screening identified 20 active compounds. Further examination of the in vitro antifungal and anti-biofilm properties of these compounds, using a range of Candida spp., led to the discovery of SM21, a highly potent antifungal molecule (minimum inhibitory concentration (MIC) 0.2 – 1.6 µg/ml). In vitro, SM21 was toxic to fungi but not to various human cell lines or bacterial species and was active against Candida isolates that are resistant to existing antifungal agents. Moreover, SM21 was relatively more effective against biofilms of Candida spp. than the current antifungal agents. In vivo, SM21 prevented the death of mice in a systemic candidiasis model and was also more effective than the common antifungal nystatin at reducing the extent of tongue lesions in a mouse model of oral candidiasis. Propidium iodide uptake assay showed that SM21 affected the integrity of the cell membrane. Taken together, our results indicate that SM21 has the potential to be developed as a novel antifungal agent for clinical use. PMID:24465737

Yuen, Kwok Yong; Wang, Yu; Yang, Dan; Samaranayake, Lakshman Perera

2014-01-01

296

In vitro antioxidant and H+, K+-ATPase inhibition activities of Acalypha wilkesiana foliage extract  

PubMed Central

Aims: The aim of this study was to evaluate the antioxidant activty and anti-acid property of Acalypha wilkesiana foliage extract. Materials and Methods: Hot and cold aqueous extracts were prepared from healthy leaves of A. wilkesiana. Free radical scavenging activity and H+, K+-ATPase inhibition activities of aqueous foliage extracts was screened by in vitro models. Statistical Analysis Used: All experiments were performed in triplicate and results are expressed as mean ± SEM. Results: A. wilkesiana hot aqueous extract (AWHE) showed significant antioxidants and free radical scavenging activity. Further, AWHE has shown a potent H+, K+-ATPase inhibitory activity (IC50: 51.5 ± 0.28 ?g/ml) when compare to standard proton pump inhibitor omeprazole (56.2 ± 0.64 ?g/ml); however, latter activity is equal to A. wilkesiana cold aqueous extract (AWCE). Quantitative analysis of AWHE has revealed more content of phenols and flavonoids; this is found to be the reason for good antioxidant activity over AWCE. Molecular docking was carried out against H+, K+-ATPase enzyme crystal structure to validate the anti-acid activity of A. wilkesiana major phytochemicals. Conclusions: The present study indicates that the constituents of AWHE and AWCE have good antacid and free radical scavenging activity. PMID:24082698

Prakash Gupta, Rajesh Kashi; Pradeepa; Hanumanthappa, Manjunatha

2013-01-01

297

In vitro anticancer activity of fucoidan from Turbinaria conoides against A549 cell lines.  

PubMed

The present study was conducted to evaluate the anticancer activity of fucoidan isolated from brown seaweed Turbinaria conoides. Extracted fucoidan contained 53 ± 0.69% of fucose and 38 ± 0.42% of sulphate, respectively. Functional groups and structural characteristics of the fucoidan were analyzed by FT-IR and NMR. In vitro anticancer effect was studied on A549 cell line. Fucoidan inhibited the growth of cancer cells in a dose-dependent manner and potent anticancer activities were 24.9-73.5% in the concentrations of 31.25-500 ?g/ml. The CTC50 value against the cancer cell was found to be 45 ?g/ml and the CTC50 value of normal Vero cell line is 325 ?g/ml. This study suggests that the fucoidan from T. conoides could be significantly improved if the active component is further purified and tested for further investigation in various cancer cell lines. PMID:25451746

Marudhupandi, Thangapandi; Ajith Kumar, Thipramalai Thankappan; Lakshmanasenthil, Shanmugaasokan; Suja, Gunasekaran; Vinothkumar, Thirumalairaj

2015-01-01

298

Radiolabeling of intact dosage forms by neutron activation: effects on in vitro performance  

SciTech Connect

Compressed tablets containing various quantities of stable isotopes of Ba, Er, and Sm for use in neutron activation studies were evaluated for the effect of stable isotope incorporation on tablet hardness and disintegration times. At concentrations likely to be used in scintigraphic studies employing neutron activation as a radiolabeling method, no significant effect on in vitro parameters were observed. While the incorporation of stable isotopes influenced tablet hardness to a greater degree than disintegration time, irradiation of tablets in a neutron flux of 4.4 x 10(13) n/cm2 sec had a direct effect on tablet disintegration time. Thus, future neutron activation studies should focus on minimizing the amount of stable isotope to be incorporated with the formulation while using the shortest feasible irradiation time.

Parr, A.; Jay, M.

1987-12-01

299

In vitro inhibition activity of essential oils from some Lamiaceae species against phytopathogenic fungi.  

PubMed

Natural products have been in focus as alternative, effective and safe materials against the phytopathogens. Investigations show Nepeta oils as effective in controlling the food crops decay. The inhibitory effects of essential oils derived from Nepeta leucophylla, Nepeta ciliaris, Nepeta clarkei and Calamintha umbrosa against five phytopthogenic fungi have been determined. In vitro antifungal activity varied with their constituents and target species. More active being the oils containing oxygenated terpenoids. Helminthosporium maydis was sensitive to the all oils, IC50 values have 43.6-109.3 ?g mL(-1). The N. leucophylla oil possessing oxygenated iridoids was more effective against H. maydis (IC50 value of 43.6 ?g mL(-1)) while N. ciliaris was more active against Fusarium oxysporum (IC50 value of 219.2 ?g mL(-1)). The oils were effective against the spore germination of all the tested plant pathogens. PMID:25175652

Kumar, Vinod; Mathela, C S; Tewari, A K; Bisht, K S

2014-09-01

300

In vitro antimicrobial activity of plants used in Cambodian traditional medicine.  

PubMed

The purpose of the present study was to screen 27 plant species used in the traditional medicine of Cambodia for in vitro antibacterial and antifungal activities. Thirty-three methanolic extracts were tested against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Mycobacterium smegmatis and Candida albicans. Screened by disk diffusion assay, the extracts showed antimicrobial activity especially on Gram-positive bacteria. None of the crude methanolic extracts showed activity against P. aeruginosa. Twenty-five selected extracts were evaluated using a micro-dilution test. Harrisonia perforata (roots) and Hymenodictyon excelsum (bark) exhibited a bactericidal effect against S. aureus at a concentration of 500 microg/ml. Azadirachta indica (bark), Harrisonia perforata (roots and stem) and Shorea obtusa (roots) exhibited a bactericidal effect against M. smegmatis at 250 microg/ml. PMID:17963325

Chea, Aun; Jonville, Marie-Caroline; Bun, Sok-Siya; Laget, Michčle; Elias, Riad; Duménil, Gérard; Balansard, Guy

2007-01-01

301

Phytochemical constituents and in vitro radical scavenging activity of different Aloe species.  

PubMed

The phytochemical profile of Aloe barbadensis Mill. and Aloe arborescens Mill. was investigated using colorimetric assays, triple quadrupole and time-of-flight mass spectrometry, focusing on phenolic secondary metabolites in the different leaf portions. Hydroxycinnamic acids, several characteristic anthrones and chromones, the phenolic dimer feralolide and flavonoids such as flavones and isoflavones were identified. The stable radical DPPH test and the ORAC assay were then used to determine the in vitro radical scavenging. The outer green rind was the most active, while the inner parenchyma was much less effective. The 5-methylchromones aloesin, aloeresin A and aloesone were the most active among the pure secondary metabolites tested. The results suggest that several compounds are likely to contribute to the overall radical scavenging activity, and indicate that leaf portion must be taken into account when the plant is used for its antioxidant properties. PMID:25306376

Lucini, Luigi; Pellizzoni, Marco; Pellegrino, Roberto; Molinari, Gian Pietro; Colla, Giuseppe

2015-03-01

302

Chemical analysis and antioxidant activity in vitro of polysaccharides extracted from Boletus edulis.  

PubMed

Boletus edulis is a well-known delicious mushroom. In this study, three crude polysaccharides (BEPF30, BEPF60 and BEPF80) were isolated from the fruiting bodies of B. edulis with boiling water. Chemical and physical characteristics of the three crude polysaccharides were investigated by the combination of chemical and instrumental analysis methods. Their antioxidant activities were investigated in vitro systems including hydroxyl assay, superoxide radical assay, reducing power and chelating activity. Among these three polysaccharides, BEPF60 showed more significant reducing power and chelating activity; and highest inhibitory effects on superoxide radical and hydroxyl radical. These results indicated that polysaccharides extracted from B. edulis might be employed as ingredients in healthy and functional food to alleviate the oxidative stress. PMID:21930154

Zhang, Anqiang; Xiao, Nannan; He, Pengfei; Sun, Peilong

2011-12-01

303

In Vitro Activity of Moxifloxacin against 923 Anaerobes Isolated from Human Intra-Abdominal Infections  

PubMed Central

The in vitro activity of moxifloxacin against 923 recent anaerobic isolates obtained from pretreatment cultures in patients with complicated intra-abdominal infections was studied using the CLSI M11-A-6 agar dilution method. Moxifloxacin was active against 87% (96 of 110) Bacteroides fragilis strains at ?1 ?g/ml and 87% (79 of 90) B. thetaiotaomicron strains at ?2 ?g/ml. Species variation was seen, with B. uniformis, B. vulgatus, Clostridium clostridioforme, and C. symbiosum being least susceptible and accounting for most of the resistant isolates; excluding the aforementioned four resistant species, 86% (303 of 363) of Bacteroides species isolates and 94% (417 of 450) of all other genera and species were susceptible to ?2 ?g/ml of moxifloxacin. Overall, moxifloxacin was active against 763 of 923 (83%) of strains at ?2 ?g/ml, supporting its use as a monotherapy for some community-acquired intra-abdominal infections. PMID:16377680

Goldstein, Ellie J. C.; Citron, Diane M.; Warren, Yumi A.; Tyrrell, Kerin L.; Merriam, C. Vreni; Fernandez, Helen

2006-01-01

304

In vitro screening for antiplasmodial activity of isoquinoline alkaloids from Brazilian plant species.  

PubMed

In the search for new antimalarial agents, nine Brazilian plant species were selected, from the Annonaceae (6), Menispermaceae (2) and Siparunaceae (1) families naturally occurring at the cerrado and Atlantic rainforest regions, in order to investigate their in vitro antiplasmodial activity. The ethanol and the alkaloid extracts were tested against K1, chloroquine-resistant, and Palo Alto, chloroquine-sensitive, strains of Plasmodium falciparum. The majority of the alkaloid extracts were more active than the ethanol ones, with IC(50) ranging 0.3-8.2 microg/mL. The crude Guatteria australis alkaloids were the most active against K1 with an IC(50) = 0.3 microg/mL. The most promising total alkaloid fractions for further bioguided isolation are those with the IC(50) < or = 5 microg/mL: G. australis, Cissampelos ovalifolia and Duguetia lanceolata. PMID:15533296

Fischer, Dominique Corinne Hermine; de Amorim Gualda, Nilton Carlos; Bachiega, Danielle; Carvalho, Cyntia Salerno; Lupo, Fernanda Nogueira; Bonotto, Sonia Valéria; Alves, Mariana de Oliveira; Yogi, Alvaro; Santi, Silvia Maria Di; Avila, Priscilla Elisangela; Kirchgatter, Karin; Moreno, Paulo Roberto Hrihorowitsch

2004-01-01

305

Synthesis of isatin thiosemicarbazones derivatives: In vitro anti-cancer, DNA binding and cleavage activities  

NASA Astrophysics Data System (ADS)

New derivatives of thiosemicarbazone Schiff base with isatin moiety were synthesized L1-L6. The structures of these compounds were characterized based on the spectroscopic techniques. Compound L6 was further characterized by XRD single crystal. The interaction of these compounds with calf thymus (CT-DNA) exhibited high intrinsic binding constant (kb = 5.03-33.00 × 105 M-1) for L1-L3 and L5 and (6.14-9.47 × 104 M-1) for L4 and L6 which reflect intercalative activity of these compounds toward CT-DNA. This result was also confirmed by the viscosity data. The electrophoresis studies reveal the higher cleavage activity of L1-L3 than L4-L6. The in vitro anti-proliferative activity of these compounds against human colon cancer cell line (HCT 116) revealed that the synthesized compounds (L3, L6 and L2) exhibited good anticancer potency.

Ali, Amna Qasem; Teoh, Siang Guan; Salhin, Abdussalam; Eltayeb, Naser Eltaher; Khadeer Ahamed, Mohamed B.; Majid, A. M. S. Abdul

306

In vitro & in vivo estrogenic activity of glycoside fractions of Solanum nigrum fruit  

PubMed Central

Background & objectives: The mature fruits of Solanum nigrum contains steroidal glycosides. These are often used as vegetable and there are evidences on tribal use of these fruits as an oral contraceptive. The present study was carried out to evaluate the estrogenic potential of S. nigrum fruits by in vitro and in vivo assays. Methods: Defatted methanol extract of dried S. nigrum fruits was column fractionated and the glycoside positive fractions pooled. Definite concentrations of the fraction were used for in vitro and in vivo assays. The effect on cell viability was analyzed in MCF-7 cell lines by MTT assay followed by in vitro evaluation of estrogenicity by hydroxy apatite (HAP) binding assay. The results were further evaluated in vivo by performing uterotrophic assay in ovariectomized mouse models. Results: At low concentration (40 ?g/ml), SNGF induced a dose-dependent increase in MCF-7 cell proliferation, while higher extract concentrations (80-320 ?g/ml) caused progressive cell growth inhibition. The competitive binding assay using 3H-E2 suggests that this effect is mediated by estrogen receptor. Mouse uterotrophic assay revealed a classical uterotrophic response in ovariectomized mice in response to S. nigrum glycoside fraction (SNGF). SNGF at a dose of 100 mg/kg of body wt induced the maximum height of luminal epithelial cells which indicated an increase of 30.8 per cent over control (P<0.01) with a correlated increase in uterine wet wt (150% increase over control). Higher doses (250 and 500 mg/kg body wt) of SNGF did not induce any uterotrophic effect. Interpretation & conclusions: Our preliminary data demonstrate the hormone like activity of Solanum glycosides both in vitro and in vivo in mouse, which needs to be further explored to evaluate the possible mechanism and clinical implications. PMID:21985821

Jisha, S.; Sreeja, S.; Manjula, S.

2011-01-01

307

Alkali extraction and in vitro antioxidant activity of Monascus mycelium polysaccharides.  

PubMed

In the present work, alkali extraction technology was used to optimize the extraction of Monascus mycelium polysaccharides for the first time. The extracting parameters of alkali extracted Monascus mycelium polysaccharides were optimized by Box-Behnken design (BBD). The optimum conditions were extraction temperature 49 °C, alkali concentration 7%, solvent/material ratio 23:1 (ml/g) and extraction time 2.3 h with an enhanced yield of 10.1%, compared with the yield 4.76% of hot water extraction, indicating that alkali extraction is a more efficient way. In order to discuss the biological activity of alkali extracted polysaccharides, we compared the in vitro antioxidant activity of alkali extracted polysaccharides (AMP) with hot water extracted polysaccharides (HMP). The result showed that AMP have the similar capability of scavenging both superoxide radical and 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical of HMP in vitro. Therefore, alkali extraction technology is not only a high-efficiency way to extract AMP, but also can retain the natural antioxidant activities of AMP, which can be used in pharmaceutical and food industries. PMID:24966417

Wang, Pengrong; Chen, Danfeng; Jiang, Donghua; Dong, Xiameng; Chen, Panpan; Lin, Yaoxue

2014-07-01

308

A fluorescent assay to quantitatively measure in vitro acyl CoA:diacylglycerol acyltransferase activity.  

PubMed

Triacylglycerols (TG) are the major storage form of energy in eukaryotic organisms and are synthesized primarily by acyl CoA:1,2-diacylglycerol acyltransferase (DGAT) enzymes. In vitro DGAT activity has previously been quantified by measuring the incorporation of either radiolabeled fatty acyl CoA or diacylglycerol (DG) into TG. We developed a modified acyltransferase assay using a fluorescent fatty acyl CoA substrate to accurately quantify in vitro DGAT activity. In the modified assay, radioactive fatty acyl CoA is replaced with fluorescent NBD-palmitoyl CoA, which is used as a substrate by DGAT with DG to produce NBD-TG. After extraction with organic solvents and separation by thin layer chromatography, NBD-TG formation can be detected and accurately quantified using a fluorescent imaging system. We demonstrate that this method can be adapted to detect other acyltransferase activities. Because NBD-palmitoyl CoA is commercially available at a much lower cost compared with radioactive acyl CoA substrates, it is a more economical alternative to radioactive tracers. In addition, the exposure of laboratory personnel to radioactivity is greatly reduced. PMID:21653930

McFie, Pamela J; Stone, Scot J

2011-09-01

309

In vitro Cytotoxic and Antimicrobial Activity of Essential Oil From Satureja Intermedia  

PubMed Central

Background Many members of the genus Satureja have aromatic and medicinal characteristics. Objectives Objectives The purpose of the present work was to determine cytotoxic activity of the essential oil of S. intermedia CA Mey (Lamiaceae) on two human cancerous cell lines and its in vitro inhibitory effects against 11 pathogenic bacteria and fungi as well. Materials and Methods The essential oil was isolated by hydrodistillation and analyzed by combination of capillary GC-FID and GC-MS. The in vitro toxicological study was based on the MTT cytotoxicity assay and antimicrobial activity of the essential oil was studied according to the disc diffusion method and MIC value. Results Thymol (34.5%), ?-terpinene (18.2%) and ?-cymene (10.5%) were the main components of the essential oil. The toxicological study on 5637 and KYSE cell lines showed IC50 values of 156 ?g/ml. The essential oil exhibited considerable antimicrobial activity on tested bacteria and fungi. Conclusions From the results of the present study, it may be concluded that the essential oil of S. intermedia and its major constitutes are interesting in antibacterial and anticancer applications. PMID:23487431

Sadeghi, Iman; Yousefzadi, Morteza; Behmanesh, Mehrdad; Sharifi, Mozafar; Moradi, Aiuob

2013-01-01

310

In vitro antimicrobial activities of capuramycin analogues against non-tuberculous mycobacteria  

PubMed Central

Objectives To determine antibacterial activity of capuramycin analogues SQ997, SQ922, SQ641 and RKS2244 against several non-tuberculous mycobacteria (NTM). Methods In vitro antibiotic activities, i.e. MIC, MBC, rate of killing and synergistic interaction with other antibiotics, were evaluated. Results SQ641 was the most active compound against all the NTM species studied. The MIC of SQ641 was ?0.06–4 mg/L for Mycobacterium avium complex (MAC; n?=?20), 0.125–2 mg/L for M. avium paratuberculosis (MAP; n?=?9), 0.125–2 mg/L for Mycobacterium kansasii (MKN;n?=?2), 0.25–1 mg/L for Mycobacterium abscessus (MAB; n?=?11), 4 mg/L for Mycobacterium smegmatis (MSMG; n?=?1), and 1 and 8 mg/L for Mycobacterium ulcerans (MUL; n?=?1), by microdilution and agar dilution methods, respectively. SQ641 was bactericidal against NTM, with an MBC/MIC ratio of 1 to 32, and killed all mycobacteria faster than positive control drugs for each strain. In chequerboard titrations, SQ641 was synergistic with ethambutol against both MAC and MSMG, and was synergistic with streptomycin and rifabutin against MAB. Conclusions In vitro, SQ641 was the most potent of the capuramycin analogues against all NTM tested, both laboratory and clinical strains. PMID:20952419

Dubuisson, Tia; Bogatcheva, Elena; Krishnan, Manju Y.; Collins, Michael T.; Einck, Leo; Nacy, Carol A.; Reddy, Venkata M.

2010-01-01

311

In vitro and in vivo activities of the nitroimidazole CGI 17341 against Mycobacterium tuberculosis.  

PubMed Central

CGI 17341 (2-ethyl-5-nitro-2,3-dihydro[2-1b]imidazo-oxazole) is a novel orally active representative of the 5-nitroimidazole series of antimicrobial agents. At concentrations ranging from 0.1 to 0.3 micrograms/ml, CGI 17341 inhibited the drug-susceptible and multi-drug-resistant strains of Mycobacterium tuberculosis. CGI 17341 had no cross-resistance with isoniazid, rifampin, streptomycin, or ethambutol. While the in vitro activity of CGI 17341 against M. tuberculosis was comparable to those of isoniazid and rifampin, it was superior to those of streptomycin, ciprofloxacin or norfloxacin, and oxazolidinone DuP 721. The MIC of CGI 17341 was not affected when the pH of the medium was decreased from 6.8 to 5.6, while four- to sixfold increases in the MICs of ciprofloxacin and isoniazid were observed. In mice infected with M. tuberculosis, the 50% effective dose for CGI 17341 was 7.7 mg/kg of body weight (95% confidence limits, 3.5 and 10.27) when administered on days 11 and 12 postinfection. CGI 17341 gave a dose-dependent (r = 0.995) and significant increase in the survival time. Our data indicate that the 5-nitroimidazole CGI 17341 is a promising and novel antituberculosis compound with potent in vitro and in vivo activities. Further investigations on this compound are warranted. PMID:8452346

Ashtekar, D R; Costa-Perira, R; Nagrajan, K; Vishvanathan, N; Bhatt, A D; Rittel, W

1993-01-01

312

Synthesis and in vitro and in vivo antifungal activity of the hydroxy metabolites of saperconazole.  

PubMed

Herein we describe the scalable diastereoselective and enantioselective syntheses of eight enantiomers of hydroxy metabolites of saperconazole. The in vitro antifungal activity of the eight stereoisomers (compounds 1-8) was compared against a broad panel of Candida spp. (n=93), Aspergillus spp. (n=10), Cryptococcus spp. (n=19), and dermatophytes (n=27). The four 2S isomers 1-4 of the new agent were generally slightly more active than the four 2R isomers 5-8. All eight isomers were tested in a model of experimental A. fumigatus infection in guinea pigs by intravenous inoculation of the fungal conidia. Treatment doses were 1.25 mg kg(-1) and 2.5 mg kg(-1) per day. Infection severity was measured in terms of mean survival time (MST) after infection and mean tissue burdens in brain, liver, spleen, and kidney at postmortem examination. Among the eight isomers, the 2S diastereomers 1-4 showed a generally higher level of activity than the 2R diastereomers 5-8, revealing compounds 1 and 4 as the most potent overall in eradicating tissue burden and MST. Compared with reference compounds itraconazole and saperconazole, the hydroxy isomers 1-8 are less potent inhibitors of the growth of A. fumigatus in vitro and of ergosterol biosynthesis in both A. fumigatus and C. albicans. PMID:20379992

Meerpoel, Lieven; Heeres, Jan; Backx, Leo J J; Van der Veken, Louis J E; Hendrickx, Rob; Corens, David; De Groot, Alex; Leurs, Stef; Van der Eycken, Luc; Weerts, Johan; Luyts, Paul; Van Gerven, Frans; Woestenborghs, Filip A A; Van Breda, Andre; Oris, Michel; van Dorsselaer, Pascal; Willemsens, Gustaaf H M; Bellens, Danny; Marichal, Patrick J M G; Vanden Bossche, Hugo F; Odds, Frank C

2010-05-01

313

Comparative in vitro activities of fluconazole, voriconazole, and MXP-4509 against Romanian blood yeast isolates.  

PubMed

The aim of the study was to evaluate the antifungal activity of a new triazole formulation against 182 clinical isolates of yeasts recovered from blood cultures in three tertiary hospitals in Romania and to compare its activity with those of fluconazole and voriconazole. In vitro susceptibility was assessed by following the guidelines of AFST-EUCAST E. Def. 7.1. The distribution of minimum inhibitory concentrations (MICs) of MXP-4509 was very similar to that of voriconazole (MIC(50): 0.0312 mg/l vs. 0.0156 mg/l; MIC(90): 0.25 mg/l vs. 0.25 mg/l), but significantly different from that of fluconazole (MIC(50): 0.0312 mg/l vs. 0.5 mg/l; MIC(90): 0.25 mg/l vs. 32 mg/l). The new triazole MXP-4509 proved to have a good in vitro antifungal activity raising the interest for further pharmacological and microbiological investigations in order to assess its potential advantages for therapy. PMID:21805354

Mare?, Mihai; N?stas?, Valentin; Ramona, Florina Moraru; Doroftei, Bogdan; Stefanache, Alina

2011-12-01

314

In vitro antioxidant and antidiabetic activities of biomodified lignin from Acacia nilotica wood.  

PubMed

The antioxidant and antidiabetic activity of biomodified alkali lignin extracted from a deciduous plant Acacia nilotica, was evaluated in vitro. The extracted alkali lignin was subjected to microbial biotransformation by ligninolytic fungus Aspergillus flavus and Emericella nidulans. These modifications were done under varying concentration of carbon to nitrogen sources. The structural feature of the lignin samples were compared by FTIR, functional group analysis and (13)C solid state NMR. All lignin samples were tested for antioxidant efficiency, reducing power and H2O2 scavenging power. Modifications in all lignin samples showed correlation with their antioxidant scavenging activity and reducing power. Antidiabetic properties were evaluated in terms of in vitro glucose movement inhibition and ?-amylase inhibition assay. Modified samples exhibited increased glucose binding efficiency as demonstrated by the decreased glucose diffusion (55.5-76.3%) and 1.16-1.18-fold enhanced ?-amylase inhibition in comparison to their control samples. The results obtained demonstrate that the structure and functional modifications in lignin significantly affects its bioefficacy in term of antioxidant and antidiabetic activities. PMID:25600985

Barapatre, Anand; Aadil, Keshaw Ram; Tiwary, Bhupendra Nath; Jha, Harit

2015-04-01

315

?-noradrenergic receptor activation specifically modulates the generation of sighs in vivo and in vitro  

PubMed Central

The pre-Bötzinger complex (preBötC), an area that is critical for generating breathing (eupnea), gasps and sighs is continuously modulated by catecholamines. These amines and the generation of sighs have also been implicated in the regulation of arousal. Here we studied the catecholaminergic modulation of sighs not only in anesthetized freely breathing mice (in vivo), but also in medullary slice preparations that contain the preBötC and that generate fictive eupneic and sigh rhythms in vitro. We demonstrate that activating ?-noradrenergic receptors (?-NR) specifically increases the frequency of sighs, while eupnea remains unaffected both in vitro and in vivo. ?-NR activation specifically increased the frequency of intrinsically bursting pacemaker neurons that rely on persistent sodium current (INap). By contrast, all parameters of bursting pacemakers that rely on the non-specific cation current (ICAN) remained unaffected. Moreover, riluzole, which blocks bursting in INap pacemakers abolished sighs altogether, while flufenamic acid (FFA) which blocks the ICAN current did not alter the sigh-increasing effect caused by ?-NR. Our results suggest that the selective ?-NR action of sighs may result from the modulation of INap pacemaker activity and that disturbances in noradrenergic system may contribute to abnormal arousal response. The ?-NR action on the preBötC may be an important mechanism in modulating behaviors that are specifically associated with sighs, such as the regulation of the early events leading to the arousal response. PMID:24273495

Viemari, Jean-Charles; Garcia, Alfredo J.; Doi, Atsushi; Elsen, Gina; Ramirez, Jan-Marino

2013-01-01

316

Probiotic activities of Lactobacillus casei rhamnosus: in vitro adherence to intestinal cells and antimicrobial properties.  

PubMed

The interest of probiotics as remedies for a broad number of gastrointestinal and other infectious diseases has gained wide interest over the last few years, but little is known about their underlying mechanism of action. In this study, the probiotic activities of a human isolate of Lactobacillus casei subsp. rhamnosus strain (Lcr35) were investigated. Using intestinal Caco-2 cell line in an in vitro model, we demonstrated that this strain exhibited adhesive properties. The inhibitory effects of Lcr35 organisms on the adherence of three pathogens, enteropathogenic Escherichia coli (EPEC), enterotoxigenic E. coli (ETEC) and Klebsiella pneumoniae, were determined. A decrease in the number of adhering pathogens was observed, using either preincubation, postincubation or coincubation of the pathogens with Lcr35. Moreover, the antibacterial activities of cell-free Lcr35 supernatant was examined against nine human pathogenic bacteria, ETEC, EPEC, K. pneumoniae, Shigella flexneri, Salmonella typhimurium, Enterobacter cloacae, Pseudomonas aeruginosa, Enterococcus faecalis and Clostridium difficile. The growth of all strains was inhibited, as measured by determining the number of viable bacteria over time, but no bactericidal activity was detected in this in vitro assay. Together, these findings suggest that this probiotic strain could be used to prevent colonization of the gastrointestinal tract by a large variety of pathogens. PMID:11316370

Forestier, C; De Champs, C; Vatoux, C; Joly, B

2001-03-01

317

Functional analysis of HPV-like particle-activated Langerhans cells in vitro.  

PubMed

Langerhans cells (LCs) are antigen-presenting cells responsible for initiating an immune response against human papillomaviruses (HPVs) entering the epithelial layer in vivo as they are the first immune cell that HPV comes into contact with. LCs become activated in response to foreign antigens, which causes internal signaling resulting in the increased expression of co-stimulatory molecules and the secretion of inflammatory cytokines. Functionally activated LCs are then capable of migrating to the lymph nodes where they interact with antigen-specific T cells and initiate an adaptive T-cell response in vivo. However, HPV has evolved in a manner that suppresses LC function, and thus the induction of antigen-specific T cells is hindered. While many methods exist to monitor the activity of LCs in vitro, the migration and induction of cytotoxic T cells is ultimately indicative of a functional immune response. Here, methods in analyzing functional migration and induction of antigen-specific T cells after stimulation of LCs with HPV virus-like particles in vitro are described. PMID:25348318

Yan, Lisa; Woodham, Andrew W; Da Silva, Diane M; Kast, W Martin

2015-01-01

318

Determination of untreated whole-milk effects on in vitro antibacterial activity.  

PubMed

The effect of fresh whole milk without pasteurization or other pretreatment on in vitro antibacterial activity of selected compounds was determined in broth dilution. The milk was collected by hand directly from dairy goats, or by syringe or cannula from bovine quarters showing low bacterial counts. Antibacterial activity was determined in 50% (v/v) milk-broth medium against sensitive mastitis-etiologic strains of Streptococcus agalactiae and Staphylococcus aureus. The indicator salt 2,3,5-triphenyltetrazolium chloride was incorporated in the milk broth medium to determine inoculum growth. Contaminant interference was circumvented through early as well as late readings and comparisons with uninoculated control tubes, with and without the test compounds. Application of the method with more than 75 compounds, including nitrofurans, antibiotics, and other chemicals uncovered marked degrees of milk interference. The method warrants routine use among preliminary screens to relate in vitro with in vivo observations of antimicrobial activity. Similar procedures may be used with serum, skim milk, or mastitis-milk media for separating effects due to protein, lipid, or other elements in product evaluation. PMID:5461785

Van Natta, J P; Lo, P W; Chang, T S

1970-02-01

319

In vitro antitrypanosomal activity of some phenolic compounds from propolis and lactones from Fijian Kawa (Piper methysticum).  

PubMed

During our search to discover new antitrypanosomal compounds, eight known plant compounds (three phenolic compounds and five kawa lactones) were evaluated for in vitro activity against Trypanosoma brucei brucei. Among them, we found two phenolic compounds and three kawa lactones possessing an ?-pyrone influenced antitrypanosomal property. In particular, ?-phenethyl caffeate, farnesyl caffeate and dihydrokawain exhibited high or moderate selective and potent antitrypanosomal activity in vitro. We detail here the antitrypanosomal activity and cytotoxicities of the compounds, in comparison with two commonly used antitrypanosomal drugs (eflornithine and suramin). Our findings represent the first report of the promising trypanocidal activity of these compounds. PMID:22116743

Otoguro, Kazuhiko; Iwatsuki, Masato; Ishiyama, Aki; Namatame, Miyuki; Nishihara-Tsukashima, Aki; Kiyohara, Hiroaki; Hashimoto, Toshihiro; Asakawa, Yoshinori; Omura, Satoshi; Yamada, Haruki

2012-07-01

320

In vitro and in vivo antioxidant activity of a water-soluble polysaccharide from dendrobium denneanum  

USGS Publications Warehouse

The water-soluble crude polysaccharide (DDP) obtained from the aqueous extracts of the stem of Dendrobium denneanum through hot water extraction followed by ethanol precipitation, was found to have an average molecular weight (Mw) of about 484.7 kDa. Monosaccharide analysis revealed that DDP was composed of arabinose, xylose, mannose, glucose and galactose in a molar ratio of 1.00:2.66:8.92:34.20:10.16. The investigation of antioxidant activity both in vitro and in vivo showed that DDP is a potential antioxidant. ?? 2011.

Luo, A.; Ge, Z.; Fan, Y.; Chun, Z.; Jin, He X.

2011-01-01

321

In vitro and in vivo antioxidant activity of a water-soluble polysaccharide from Dendrobium denneanum.  

PubMed

The water-soluble crude polysaccharide (DDP) obtained from the aqueous extracts of the stem of Dendrobium denneanum through hot water extraction followed by ethanol precipitation, was found to have an average molecular weight (Mw) of about 484.7 kDa. Monosaccharide analysis revealed that DDP was composed of arabinose, xylose, mannose, glucose and galactose in a molar ratio of 1.00:2.66:8.92:34.20:10.16. The investigation of antioxidant activity both in vitro and in vivo showed that DDP is a potential antioxidant. PMID:21321529

Luo, Aoxue; Ge, Zhongfu; Fan, Yijun; Luo, Aoshuang; Chun, Ze; He, Xingjin

2011-01-01

322

In Vitro activity of terbinafine combined with caspofungin and azoles against Pythium insidiosum.  

PubMed

In this text we evaluated the in vitro antifungal activities of terbinafine combined with caspofungin, miconazole, ketoconazole, and fluconazole against 17 Pythium insidiosum strains by using the microdilution checkerboard method. Synergistic interactions were observed with terbinafine combined with caspofungin (41.2% of the strains), fluconazole (41.2%), ketoconazole (29.4%), and miconazole (11.8%). No antagonistic effects were observed. The combination of terbinafine plus caspofungin or terbinafine plus fluconazole may have significant therapeutic potential for treatment of pythiosis. PMID:19289531

Cavalheiro, Ayrton S; Maboni, Grazieli; de Azevedo, Maria I; Argenta, Juliana S; Pereira, Daniela I B; Spader, Tatiana B; Alves, Sydney H; Santurio, Janio M

2009-05-01

323

In Vitro Activity of Terbinafine Combined with Caspofungin and Azoles against Pythium insidiosum?  

PubMed Central

In this text we evaluated the in vitro antifungal activities of terbinafine combined with caspofungin, miconazole, ketoconazole, and fluconazole against 17 Pythium insidiosum strains by using the microdilution checkerboard method. Synergistic interactions were observed with terbinafine combined with caspofungin (41.2% of the strains), fluconazole (41.2%), ketoconazole (29.4%), and miconazole (11.8%). No antagonistic effects were observed. The combination of terbinafine plus caspofungin or terbinafine plus fluconazole may have significant therapeutic potential for treatment of pythiosis. PMID:19289531

Cavalheiro, Ayrton S.; Maboni, Grazieli; de Azevedo, Maria I.; Argenta, Juliana S.; Pereira, Daniela I. B.; Spader, Tatiana B.; Alves, Sydney H.; Santurio, Janio M.

2009-01-01

324

In Vitro Activities of Y-688, a New 7-Substituted Fluoroquinolone, against Anaerobic Bacteria  

PubMed Central

The in vitro activities of Y-688, a new 7-substituted fluoroquinolone derivative, against 317 nonduplicate anaerobic isolates were determined. Eighty-five percent of the Bacteroides fragilis group (n = 89) were inhibited by ?2 mg of Y-688 per liter, while 78, 100, 89, and 98% of gram-negative bacilli (n = 135), gram-positive cocci (n = 59), and non-spore-forming (n = 58) and spore-forming (n = 51) gram-positive bacilli, respectively, were inhibited by ?1 mg of Y-688 per liter. PMID:9527797

MacGowan, A. P.; Bowker, K. E.; Wootton, M.; Holt, H. A.; Reeves, D. S.

1998-01-01

325

In Vitro Activities of Eight Antifungal Drugs against 106 Waterborne and Cutaneous Exophiala Species  

PubMed Central

The in vitro activities of eight antifungal drugs against 106 clinical and environmental isolates of waterborne and cutaneous Exophiala species were tested. The MICs and minimum effective concentrations for 90% of the strains tested (n = 106) were, in increasing order, as follows: posaconazole, 0.063 ?g/ml; itraconazole, 0.25 ?g/ml; micafungin, 1 ?g/ml; voriconazole, 2 ?g/ml; isavuconazole, 4 ?g/ml; caspofungin, 8 ?g/ml; amphotericin B, 16 ?g/ml; fluconazole, 64 ?g/ml. PMID:24100491

Najafzadeh, M. J.; Saradeghi Keisari, M.; Vicente, V. A.; Feng, P.; Shamsian, S. A. A.; Rezaei-Matehkolaei, A.; de Hoog, G. S.; Curfs-Breuker, I.

2013-01-01

326

In vitro activities of eight antifungal drugs against 106 waterborne and cutaneous exophiala species.  

PubMed

The in vitro activities of eight antifungal drugs against 106 clinical and environmental isolates of waterborne and cutaneous Exophiala species were tested. The MICs and minimum effective concentrations for 90% of the strains tested (n = 106) were, in increasing order, as follows: posaconazole, 0.063 ?g/ml; itraconazole, 0.25 ?g/ml; micafungin, 1 ?g/ml; voriconazole, 2 ?g/ml; isavuconazole, 4 ?g/ml; caspofungin, 8 ?g/ml; amphotericin B, 16 ?g/ml; fluconazole, 64 ?g/ml. PMID:24100491

Najafzadeh, M J; Saradeghi Keisari, M; Vicente, V A; Feng, P; Shamsian, S A A; Rezaei-Matehkolaei, A; de Hoog, G S; Curfs-Breuker, I; Meis, J F

2013-12-01

327

In vitro activities of eight antifungal drugs against 55 clinical isolates of Fonsecaea spp.  

PubMed

The in vitro activities of eight antifungal drugs against clinical isolates of Fonsecaea pedrosoi (n = 21), Fonsecaea monophora (n = 25), and Fonsecaea nubica (n = 9) were tested. The resulting MIC(90)s for all strains (n = 55) were as follows, in increasing order: posaconazole, 0.063 microg/ml; itraconazole, 0.125 microg/ml; isavuconazole, 0.25 microg/ml; voriconazole, 0.5 microg/ml; amphotericin B, 2 microg/ml; caspofungin, 2 microg/ml; anidulafungin, 2 microg/ml; and fluconazole, 32 microg/ml. PMID:20086140

Najafzadeh, Mohammad J; Badali, Hamid; Illnait-Zaragozi, Maria Teresa; De Hoog, G Sybren; Meis, Jacques F

2010-04-01

328

Ceruminal diffusion activities and ceruminolytic characteristics of otic preparations – an in-vitro study  

PubMed Central

Background An in-vitro setup was established in order to determine a) the diffusion activities of eight otic preparations (Aurizon®, Eas Otic®, Epi Otic®, Otifree®, Otomax®, Panolog®, Posatex®, Surolan®) through synthetic cerumen, and b) the ceruminolytic capacity and impregnation effects of these products. The main lipid classes of canine cerumen produced with moderate, non-purulent otitis externa were determined by thin layer chromatography and were subsequently used to produce a standardised synthetic cerumen (SCC). SCC was filled into capillary tubes, all of which were loaded with six commercially available multipurpose otic medications and two ear cleaners, each mixed with two markers in two experimental setups. These two marker compounds (Oil red O and marbofloxacin) were chosen, since they exhibit different physicochemical drug characteristics by which it is possible to determine and verify the diffusion activity of different types of liquids (i.e. the otic preparations). A synthetic cerumen described in the literature (JSL) was also used for comparison as its lipid composition was different to SCC. The diffusion activities of the otic preparations through both types of synthetic cerumen were studied over 24 hours. A second in-vitro experiment determined both the ceruminolytic activity and impregnation effect of the otic preparations by comparing the weight loss or weight gain after repeated incubation of JSL. Results Canine cerumen is mainly composed of triglycerides, sterol esters, fatty acid esters and squalene. The diffusion experiments showed a high diffusion efficacy along with a high impregnation effect for one test product. All the other products exhibited a lower diffusion activity with a mild to moderate impregnation effect. A mild ceruminolytic activity was observed for the two ear cleaners but not for any of the otic medications. Conclusions The present study demonstrates that there are significant differences in the diffusion characteristics and ceruminolytic properties of the eight tested otic preparations. PMID:23574753

2013-01-01

329

Comparison of chemical, electrical, and combined activation methods for in vitro matured porcine oocytes.  

PubMed

Factors influencing porcine oocyte activation were systematically studied. This study included (1) the effect of ionomycin plus various chemical agents on activation, (2) comparison of different electrical activation parameters, (3) optimization of combined activation, and (4) evaluation of the optimized protocols. The results showed that (1) blastocyst rates of ionomycin (Ion) + 6-dimethylaminopurine (6-DMAP) (29.7?±?1.1%), Ion + cytochalasin B (CB) + cycloheximide (CHX) (29.8?±?1.2%), Ion + CB + 6-DMAP (30.4?±?1.6%), and Ion + CB + CHX + 6-DMAP (30.2?±?2.7%) were significantly higher than Ion + CHX (15.8?±?1.5%, p?activation was optimal when oocytes were activated by three direct current (DC) pulses of 1.00 kV cm(-1) for 80 ?s (39.5?±?1.1%); (3) blastocyst rates of DC + CB + CHX (55.4?±?1.2%) and DC + CB + 6-DMAP (50.4?±?2.9%) were significantly higher than DC + 6-DMAP, DC + CB + CHX + 6-DMAP, electrical activation, and chemical activation alone (p?activation blastocysts (40%). Using the optimized electrical and combined activation protocol, high blastocyst rates were generated by intracytoplasmic sperm injection (ICSI) (34.6?±?1.1%), cytoplasmic microinjection (CI) (52.3?±?2.2%), and handmade cloning (HMC) (31.2?±?1.0%), respectively. This study concludes that the optimal activation protocol of in vitro matured porcine oocytes was combined activation with parameter as three DC pulses of 1.00 kV cm(-1) for 80 ?s plus CB and CHX treatment. PMID:25424832

Liu, Shuai; Cui, Kuiqing; Li, Hong Li; Sun, Jun Ming; Lu, Xing Rong; Shen, Kai Yuan; Liu, Qing You; Shi, De Shun

2015-02-01

330

In vitro antimalarial activity and cytotoxicity of some selected cuban medicinal plants.  

PubMed

Terrestrial plants have been demonstrated to be sources of antimalarial compounds. In Cuba, little is known about antimalarial potentials of plant species used as medicinals. For that reason, we evaluated the antimalarial activity of 14 plant species used in Cuba as antimalarial, antipyretic and/or antiparasitic. Hydroalcoholic extracts were prepared and tested in vitro for the antimalarial activity against Plasmodium falciparum Ghana strain and over human cell line MRC-5 to determine cytotoxicity. Parasite multiplication was determined microscopically by the direct count of Giemsa stained parasites. A colorimetric assay was used to quantify cytotoxicity. Nine extracts showed IC50 values lower than 100 µg/mL against P. falciparum, four extracts were classified as marginally active (SI < 4), one as partially active (Parthenium hysterophorus) exhibiting SI equal to 6.2 and two extracts as active (Bambusa vulgaris and Punica granatum), showing SI > 10. B. vulgaris showed the most potent and specific antiplasmodial action (IC50 = 4.7 µg/mL, SI = 28.9). Phytochemical characterization of active extracts confirmed the presence of triterpenoids in B. vulgaris and polar compounds with phenol free groups and fluorescent metabolites in both extracts as major phytocompounds, by thin layer chromatography. In conclusion, antimalarial use of B. vulgaris and P. hysterophorus was validated. B. vulgaris and P. granatum extracts were selected for follow-up because of their strong antimalarial activity. PMID:21748227

Valdés, Aymé Fernández-Calienes; Martínez, Judith Mendiola; Lizama, Ramón Scull; Gaitén, Yamilet Gutiérrez; Rodríguez, Deyanira Acuńa; Payrol, Juan Abreu

2010-01-01

331

Effects of aluminium and lead on ATPase activity of knockout +/- mouse cerebral synaptosomes in vitro.  

PubMed

In this in vitro study, changes in the activity of the neural membrane integral protein, ATPase, were recorded after the exposure of isolated synaptosomes to different concentrations of aluminium and lead. Both total ATPase activity and Mg(2+)-ATPase activity were studied. A specific mouse strain, heterozygous for a glial cell line-derived neurotrophic factor (GDNF), and the corresponding wildtype mouse cerebral tissue, were used for the synaptosome isolations. The ATPase activities of the +/- mouse synaptosomes were compared with those of wild-type synaptosomes. The decrease in total ATPase activity was similar in both types of synaptosomes, but after exposure to aluminium, the decrease of Mg(2+)-ATPase activity in the GDNF+/- synaptosomes was smaller than that in the wild-type synaptosomes. After exposure to lead, the protective effect of GDNF was not so clear. The synaptosomal effects of lead were already found at concentrations lower than those where cell toxicity appeared in SH-SY5Y cell cultures. Thus, synaptosomal ATPase activity was considered to be a sensitive marker for the detection of lead-induced neurotoxicity. PMID:15651920

Kohila, Tarja; Tähti, Hanna

2004-10-01

332

In vitro and in vivo antibacterial activities of DC-159a, a new fluoroquinolone.  

PubMed

DC-159a is a new 8-methoxy fluoroquinolone that possesses a broad spectrum of antibacterial activity, with extended activity against gram-positive pathogens, especially streptococci and staphylococci from patients with community-acquired infections. DC-159a showed activity against Streptococcus spp. (MIC(90), 0.12 microg/ml) and inhibited the growth of 90% of levofloxacin-intermediate and -resistant strains at 1 microg/ml. The MIC 90s of DC-159a against Staphylococcus spp. were 0.5 microg/ml or less. Against quinolone- and methicillin-resistant Staphylococcus aureus strains, however, the MIC 90 of DC-159a was 8 microg/ml. DC-159a was the most active against Enterococcus spp. (MIC 90, 4 to 8 microg/ml) and was more active than the marketed fluoroquinolones, such as levofloxacin, ciprofloxacin, and moxifloxacin. The MIC 90s of DC-159a against Haemophilus influenzae, Moraxella catarrhalis, and Klebsiella pneumoniae were 0.015, 0.06, and 0.25 microg/ml, respectively. The activity of DC-159a against Mycoplasma pneumoniae was eightfold more potent than that of levofloxacin. The MICs of DC-159a against Chlamydophila pneumoniae were comparable to those of moxifloxacin, and DC-159a was more potent than levofloxacin. The MIC 90s of DC-159a against Peptostreptococcus spp., Clostridium difficile, and Bacteroides fragilis were 0.5, 4, and 2 microg/ml, respectively; and among the quinolones tested it showed the highest level of activity against anaerobic organisms. DC-159a demonstrated rapid bactericidal activity against quinolone-resistant Streptococcus pneumoniae strains both in vitro and in vivo. In vitro, DC-159a showed faster killing than moxifloxacin and garenoxacin. The bactericidal activity of DC-159a in a murine muscle infection model was revealed to be superior to that of moxifloxacin. These activities carried over to the in vivo efficacy in the murine pneumonia model, in which treatment with DC-159a led to bactericidal activity superior to those of the other agents tested. PMID:17938194

Hoshino, Kazuki; Inoue, Kazue; Murakami, Yoichi; Kurosaka, Yuichi; Namba, Kenji; Kashimoto, Yoshinori; Uoyama, Saori; Okumura, Ryo; Higuchi, Saito; Otani, Tsuyoshi

2008-01-01

333

Uridine 5?-Triphosphate Promotes In Vitro Schwannoma Cell Migration through Matrix Metalloproteinase-2 Activation  

PubMed Central

In response to peripheral nerve injury, Schwann cells adopt a migratory phenotype and modify the extracellular matrix to make it permissive for cell migration and axonal re-growth. Uridine 5?-triphosphate (UTP) and other nucleotides are released during nerve injury and activate purinergic receptors expressed on the Schwann cell surface, but little is known about the involvement of purine signalling in wound healing. We studied the effect of UTP on Schwannoma cell migration and wound closure and the intracellular signaling pathways involved. We found that UTP treatment induced Schwannoma cell migration through activation of P2Y2 receptors and through the increase of extracellular matrix metalloproteinase-2 (MMP-2) activation and expression. Knockdown P2Y2 receptor or MMP-2 expression greatly reduced wound closure and MMP-2 activation induced by UTP. MMP-2 activation evoked by injury or UTP was also mediated by phosphorylation of all 3 major mitogen-activated protein kinases (MAPKs): JNK, ERK1/2, and p38. Inhibition of these MAPK pathways decreased both MMP-2 activation and cell migration. Interestingly, MAPK phosphorylation evoked by UTP exhibited a biphasic pattern, with an early transient phosphorylation 5 min after treatment, and a late and sustained phosphorylation that appeared at 6 h and lasted up to 24 h. Inhibition of MMP-2 activity selectively blocked the late, but not the transient, phase of MAPK activation. These results suggest that MMP-2 activation and late MAPK phosphorylation are part of a positive feedback mechanism to maintain the migratory phenotype for wound healing. In conclusion, our findings show that treatment with UTP stimulates in vitro Schwannoma cell migration and wound repair through a MMP-2-dependent mechanism via P2Y2 receptors and MAPK pathway activation. PMID:24905332

Martiańez, Tania; Segura, Mňnica; Figueiro-Silva, Joana; Grijota-Martinez, Carmen; Trullas, Ramón; Casals, Núria

2014-01-01

334

GDKV-induced antiphospholipid antibodies enhance thrombosis and activate endothelial cells in vivo and in vitro.  

PubMed

Antiphospholipid (aPL) Abs are associated with thrombosis, pregnancy loss, and thrombocytopenia in patients with systemic lupus erythematosus or primary antiphospholipid syndrome (APS). beta2-Glycoprotein I (beta2GPI), a phospholipid-binding serum protein, is involved in aPL binding to phospholipids. aPL can be generated in mice by immunization with beta2GPI, and these Abs are thrombogenic and cause pregnancy loss in mice. The objective of this study is to determine whether aPL induced by immunization with the phospholipid-binding site of beta2GPI are thrombogenic and whether they activate endothelial cells (EC) in vivo and in vitro. Murine monoclonal aPL were generated from spleen cells of a mouse immunized with GDKV, a synthetic 15-aa peptide spanning Gly274-Cys288 in the fifth domain of human beta2GPI, which represents the phospholipid-binding site of beta2GPI. The Abs generated had aPL and anti-beta2GPI activities. The effect of these Abs on thrombus formation and on EC activation in vivo was determined using a mouse model of thrombosis and microcirculation that enables examination of the adhesion of leukocyte to EC as an indication of EC activation as well as adhesion molecule expression using in vitro ELISA analysis. Mice injected with this monoclonal aPL showed a significant increase in leukocyte sticking and also produced larger thrombi that persisted longer. Exposure to GDKV-induced aPL for 4 h significantly increased surface Ag expression of E-selectin, ICAM-1, and VCAM-1. These data indicate that aPL induced by immunization with the phospholipid binding site of beta2GPI are thrombogenic and activate endothelial cells. PMID:10453040

Gharavi, A E; Pierangeli, S S; Colden-Stanfield, M; Liu, X W; Espinola, R G; Harris, E N

1999-09-01

335

In vitro and in vivo anti-glioma activity of a chalcone-quinoxaline hybrid.  

PubMed

Chalcones are important compounds that exhibit multiple biological activities, including anti-inflammatory, antimitotic and antibacterial properties. In the present study, we have analyzed the potential anti-cancer activity of a chalcone named N9 (a hybrid chalcone-quinoxaline compound) using in vitro and in vivo experimental glioma models. Here, we report N9-induced inhibition of cell proliferation and also N9-induced cell death in a concentration-dependent manner in U87-MG glioma cells. These effects of N9 appear to be associated with its ability to inhibit the expression of cell cycle-associated proteins, and also the augmentation in the expression of the p21 (p21/Cip1) protein, a cyclin-dependent kinase inhibitor. Additionally, N9 also potentiates the production of the pro-apoptotic markers Bax and p53 via inhibition of MDM2. Moreover, our results show that N9 also significantly enhanced apoptosis of U87-MG cells with disruption of mitochondrial membrane potential, generation of ROS and caspase-9 activation. In vivo experiments carried out in a murine xenograft model of U87-MG revealed that N9 produced a significant reduction of tumors volume when compared to vehicle treated mice. Collectively, data demonstrate that N9 possess in vitro and in vivo anti-cancer activity, an effect that seems to involve the induction of p53 and p21 proteins, as well as, the activation of mitochondrial apoptosis pathway associated with the inhibition of protein MDM2. Overall, this study suggests N9 is affecting a variety of intracellular pathways related to tumor apoptosis. Perhaps N9 or derivate molecules could represent new potential drugs for cancer therapeutics. PMID:25461314

Loch-Neckel, Gecioni; Bicca, Maíra Assunçăo; Leal, Paulo César; Mascarello, Alessandra; Siqueira, Jarbas Mota; Calixto, Joăo B

2015-01-27

336

In vitro and in vivo activities of pterostilbene against Candida albicans biofilms.  

PubMed

Pterostilbene (PTE) is a stilbene-derived phytoalexin that originates from several natural plant sources. In this study, we evaluated the activity of PTE against Candida albicans biofilms and explored the underlying mechanisms. In 2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide (XTT) reduction assays, biofilm biomass measurement, confocal laser scanning microscopy, and scanning electron microscopy, we found that ?16 ?g/ml PTE had a significant effect against C. albicans biofilms in vitro, while it had no fungicidal effect on planktonic C. albicans cells, which suggested a unique antibiofilm effect of PTE. Then we found that PTE could inhibit biofilm formation and destroy the maintenance of mature biofilms. At 4 ?g/ml, PTE decreased cellular surface hydrophobicity (CSH) and suppressed hyphal formation. Gene expression microarrays and real-time reverse transcription-PCR showed that exposure of C. albicans to 16 ?g/ml PTE altered the expression of genes that function in morphological transition, ergosterol biosynthesis, oxidoreductase activity, and cell surface and protein unfolding processes (heat shock proteins). Filamentation-related genes, especially those regulated by the Ras/cyclic AMP (cAMP) pathway, including ECE1, ALS3, HWP1, HGC1, and RAS1 itself, were downregulated upon PTE treatment, indicating that the antibiofilm effect of PTE was related to the Ras/cAMP pathway. Then, we found that the addition of exogenous cAMP reverted the PTE-induced filamentous growth defect. Finally, with a rat central venous catheter infection model, we confirmed the in vivo activity of PTE against C. albicans biofilms. Collectively, PTE had strong activities against C. albicans biofilms both in vitro and in vivo, and these activities were associated with the Ras/cAMP pathway. PMID:24514088

Li, De-Dong; Zhao, Lan-Xue; Mylonakis, Eleftherios; Hu, Gan-Hai; Zou, Yong; Huang, Tong-Kun; Yan, Lan; Wang, Yan; Jiang, Yuan-Ying

2014-01-01

337

In Vitro and In Vivo Activities of Pterostilbene against Candida albicans Biofilms  

PubMed Central

Pterostilbene (PTE) is a stilbene-derived phytoalexin that originates from several natural plant sources. In this study, we evaluated the activity of PTE against Candida albicans biofilms and explored the underlying mechanisms. In 2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide (XTT) reduction assays, biofilm biomass measurement, confocal laser scanning microscopy, and scanning electron microscopy, we found that ?16 ?g/ml PTE had a significant effect against C. albicans biofilms in vitro, while it had no fungicidal effect on planktonic C. albicans cells, which suggested a unique antibiofilm effect of PTE. Then we found that PTE could inhibit biofilm formation and destroy the maintenance of mature biofilms. At 4 ?g/ml, PTE decreased cellular surface hydrophobicity (CSH) and suppressed hyphal formation. Gene expression microarrays and real-time reverse transcription-PCR showed that exposure of C. albicans to 16 ?g/ml PTE altered the expression of genes that function in morphological transition, ergosterol biosynthesis, oxidoreductase activity, and cell surface and protein unfolding processes (heat shock proteins). Filamentation-related genes, especially those regulated by the Ras/cyclic AMP (cAMP) pathway, including ECE1, ALS3, HWP1, HGC1, and RAS1 itself, were downregulated upon PTE treatment, indicating that the antibiofilm effect of PTE was related to the Ras/cAMP pathway. Then, we found that the addition of exogenous cAMP reverted the PTE-induced filamentous growth defect. Finally, with a rat central venous catheter infection model, we confirmed the in vivo activity of PTE against C. albicans biofilms. Collectively, PTE had strong activities against C. albicans biofilms both in vitro and in vivo, and these activities were associated with the Ras/cAMP pathway. PMID:24514088

Li, De-Dong; Zhao, Lan-Xue; Mylonakis, Eleftherios; Hu, Gan-Hai; Zou, Yong; Huang, Tong-Kun; Yan, Lan

2014-01-01

338

In vitro activity of origanum vulgare essential oil against candida species  

PubMed Central

The aim of this study was to evaluate the in vitro activity of the essential oil extracted from Origanum vulgare against sixteen Candida species isolates. Standard strains tested comprised C. albicans (ATCC strains 44858, 4053, 18804 and 3691), C. parapsilosis (ATCC 22019), C. krusei (ATCC 34135), C. lusitaniae (ATCC 34449) and C. dubliniensis (ATCC MY646). Six Candida albicans isolates from the vaginal mucous membrane of female dogs, one isolate from the cutaneous tegument of a dog and one isolate of a capuchin monkey were tested in parallel. A broth microdilution technique (CLSI) was used, and the inoculum concentration was adjusted to 5 x 106 CFU mL-1. The essential oil was obtained by hydrodistillation in a Clevenger apparatus and analyzed by gas chromatography. Susceptibility was expressed as Minimal Inhibitory Concentration (MIC) and Minimal Fungicidal Concentration (MFC). All isolates tested in vitro were sensitive to O. vulgare essential oil. The chromatographic analysis revealed that the main compounds present in the essential oil were 4-terpineol (47.95%), carvacrol (9.42%), thymol (8.42%) and ?-terpineol (7.57%). C. albicans isolates obtained from animal mucous membranes exhibited MIC and MFC values of 2.72 ?L mL-1 and 5 ?L mL-1, respectively. MIC and MFC values for C. albicans standard strains were 2.97 ?L mL-1 and 3.54 ?L mL-1, respectively. The MIC and MFC for non-albicans species were 2.10 ?L mL-1 and 2.97 ?L mL-1, respectively. The antifungal activity of O. vulgare essential oil against Candida spp. observed in vitro suggests its administration may represent an alternative treatment for candidiasis. PMID:24031471

Cleff, Marlete Brum; Meinerz, Ana Raquel; Xavier, Melissa; Schuch, Luiz Filipe; Schuch, Luiz Filipe; Araújo Meireles, Mário Carlos; Alves Rodrigues, Maria Regina; de Mello, Joăo Roberto Braga

2010-01-01

339

Antimicrobial Activity of Artemisinin and Precursor Derived from In Vitro Plantlets of Artemisia annua L.  

PubMed Central

Artemisia annua L., a medicinal herb, produces secondary metabolites with antimicrobial property. In Malaysia due to the tropical hot climate, A. annua could not be planted for production of artemisinin, the main bioactive compound. In this study, the leaves of three in vitro A. annua L. clones were, extracted and two bioactive compounds, artemisinin and a precursor, were isolated by thin layer chromatography. These compounds were found to be effective in inhibiting the growth of Gram-positive and Gram-negative bacteria but not Candida albicans. Their antimicrobial activity was similar to that of antibactericidal antibiotic streptomycin. They were found to inhibit the growth of the tested microbes at the minimum inhibition concentration of 0.09?mg/mL, and toxicity test using brine shrimp showed that even the low concentration of 0.09?mg/mL was very lethal towards the brine shrimps with 100% mortality rate. This study hence indicated that in vitro cultured plantlets of A. annua can be used as the alternative method for production of artemisinin and its precursor with antimicrobial activities. PMID:24575401

Appalasamy, Suganthi; Lo, Kiah Yann; Ch'ng, Song Jin; Nornadia, Ku; Othman, Ahmad Sofiman; Chan, Lai-Keng

2014-01-01

340

[Antiviral activity in vitro and pharmacokinetics of HCV entry inhibitor AVR560].  

PubMed

Several novel compounds were found to be potent inhibitors of the HCV (JFH-1 isolate) infection in vitro. Human serum did not significantly reduce antiviral activity of the lead compound, AVR560 (< 4-fold). The immunohistochemistry studies with the Huh7 cell line, infectable with the HCV (JFH-1 strain), demonstrated that AVR560 inhibited the early steps of viral infection and blocked the spread of the HCV infection in tissue culture. The cytotoxicity in Huh7 and Vero-76 cell lines was mild. AVR560 proved to be a specific HCV inhibitor and exhibited no activity against other flaviviruses such as yellow fever (strain 17D), West Nile (strain NY99), and dengue (New Guinea type 2) in in vitro infection experiments. AVR560 also did not inhibit any of the tested human CYP450 isozymes (3A4, 1A2, 2C19 and 2D6). In the pharmacokinetic studies in mice, rats and dogs, favorable pharmacokinetic profiles and good oral bioavailability were observed for AV560. Further pre-clinical studies with this novel HCV inhibitor are in progress. PMID:25518527

2014-01-01

341

Acaricidal activity of 9-oxo-10,11-dehydroageraphorone extracted from Eupatorium adenophorum in vitro.  

PubMed

The acaricidal activity of the 9-oxo-10,11-dehydroageraphorone (euptox A), a cadenine sesquiterpene from Eupatorium adenophorum (E. adenophorum) against Sarcoptes scabiei and Psoroptes cuniculi was tested in vitro. A complementary log-log (CLL) model was used to analyze the data of the toxicity tests in vitro. The results showed euptox A had strong toxicity against mites, killing all S. scabiei at 3 and 4 mg/ml (m/v) concentration, while 4 mg/ml euptox A was also found to kill all P. cuniculi within a 4 h period. Similarly, 2, 3 and 4 mg/ml concentration of euptox A had strong toxicity against S. scabiei, with median lethal time (LT50) values at 0.687, 0.526, 0.326 h, respectively. 3 mg/ml and 4 mg/ml showed strong acaricidal action against P. cuniculi; the LT50 values were 0.693 and 0.493 h, respectively. The median lethal concentration (LC50) values were 1.068 mg/ml for Scabies mite and 0.902 mg/ml for P. cuniculi in 2 h. The results indicate that euptox A has strong acaricidal activity and may exploit as novel drugs for the effective control of animal acariasis. PMID:24631419

Liao, Fei; Hu, Yanchun; Tan, Hui; Wu, Lei; Wang, Yunfei; Huang, Yue; Mo, Quan; Wei, Yahui

2014-05-01

342

Antiangiogenic activity of low-temperature lysozyme from a marine bacterium in vivo and in vitro  

NASA Astrophysics Data System (ADS)

We extracted marine low-temperature lysozyme (MLTL), a novel lysozyme, from a marine microorganism through fermentation. Our previous study suggested that a low molecular weight (16 kDa) may exert anti-tumor activity through antiangiogenesis. In this study, we extracted a high weight (39 kDa) and investigated its antiangiogenic activity in vivo and in vitro. Using zebrafish embryos as an in vivo study model, we found that treatment with MLTL significantly inhibited the growth of subintestinal vessels (SIVs) in a dose-dependent manner and that 400 µg/ml MLTL was sufficient to block the growth of SIVs. An in vitro study conducted using human umbilical vein endothelial cells (HUVECs) revealed that MLTL suppressed the proliferation, migration and tube formation of HUVECs in a dose-dependent manner. Interestingly, assays by flow cytometry and DNA electrophoresis indicated that MLTL was able to induce apoptosis of HUVECs. Moreover, further study demonstrated that the disruption of intracellular Ca2+ homeostasis may play an important role in MLTL induced apoptosis of HUVECs. Taken together, the results of this study demonstrate for the first time that MLTL inhibits angiogenesis through its pleiotropic effects on vascular endothelial cells and induces apoptosis through regulation of cellular Ca2+ levels. The results of this study also revealed a possible mechanism underlying the antiangiogenic effect of MLTL and suggested that MLTL may be a promising new antiangiogenic agent for use in cancer therapy.

Wang, Zhenhua; Liu, Jincheng; Su, Ai; Sun, Mi; Wang, Chunbo

2009-11-01

343

Partial characterization, in vitro antioxidant and antiproliferative activities of patatin purified from potato fruit juice.  

PubMed

Patatin from potato fruit juice was purified by a combination of ultrafiltration and chromatographic techniques. The in vitro antioxidant and antiproliferative activity against mouse melanoma B16 cells of patatin were investigated. The results showed that the monosaccharide composition of patatin included rhamnose, mannose, glucose, and galactose with a molar ratio of 41 : 30 : 21 : 8, and patatin consisted of (1 ? 3) linked ?-mannose, (1 ? 4) linked ?-galactose, (1 ? 4) linked ?-glucose, and (1 ? 2) linked ?-rhamnose. Furthermore, patatin possessed significant antioxidant activities measured by scavenging of the DPPH and superoxide free radicals, notable reducing power, protective effects against hydroxyl radical-induced oxidative DNA damage and lipid peroxidation inhibitory. Moreover, patatin was identified as a potent antiproliferative agent against mouse melanoma B16 cells, causing cell cycle arrest in the G1 phase. Assays of apoptotic cells also showed that patatin treatment at concentrations of 20 mg mL(-1) resulted in a marked reduction of viable cells. These results obtained in in vitro models suggested that patatin may have potential application as a cancer chemopreventive agent and food ingredient. PMID:24056776

Sun, Ying; Jiang, Lianzhou; Wei, Dongxu

2013-10-01

344

The Immunological Enhancement Activity of Propolis Flavonoids Liposome In Vitro and In Vivo  

PubMed Central

The aim of this study was to investigate and assess the effects of propolis flavonoids liposome imposed on the immune system by comparing it to propolis flavonoids and blank liposome. In vitro, the effects of the above drugs on macrophages were assessed by measuring the phagocytic function and cytokine production. In vivo, the immunological adjuvant activity of propolis flavonoids liposome was compared with those of propolis flavonoids and blank liposome. The results showed that in vitro propolis flavonoids liposome can significantly enhance the phagocytic function of macrophages and the release of IL-1?, IL-6, and IFN-?. In addition, subcutaneous administration of propolis flavonoids liposome with ovalbumin to mice could effectively activate the cellular and humoral immune response, including inducing higher level concentrations of IgG, IL-4, and IFN-? in serum and the proliferation rates of splenic lymphocytes. These findings provided valuable information regarding the immune modulatory function of propolis flavonoids liposome and indicated the possibility of use of propolis flavonoids liposome as a potential adjuvant. PMID:25383082

Tao, Yang; Wang, Deqing; Hu, Yuanliang; Huang, Yee; Yu, Yun; Wang, Deyun

2014-01-01

345

Activation of 2,4-diaminotoluene to proximate carcinogens in vitro, and assay of DNA adducts.  

PubMed

1. 2,4-Diaminotoluene, which yields adducts with DNA in vivo, has been studied for its ability to form adducts in vitro. Metabolic activation with rat liver post-mitochondrial supernatant gave 300 adducts/10(6) nucleotides in calf thymus single-stranded DNA, under defined experimental conditions. 2. 2,4-Diaminotoluene-modified DNA and deoxyhomopolymers showed characteristic u.v. absorption spectra, exhibiting hyperchromic effects at 235 and 220 nm, and hypochromic effect at 260 nm. The difference spectra between diamine-modified and untreated DNA, or deoxyhomopolymer, were very similar to the spectrum of 2,4-diaminotoluene alone. 3. 2,4-Diaminotoluene-modified DNA was assayed by ELISA with specific monoclonal antibodies directed against diamine-DNA adducts. Reactions with poly-d(A) or poly-d(A-T) gave no spectral modification, and immunochemical analysis showed that the diamine did not bind to these polynucleotides. On the other hand, in the case of poly-d(G) or poly-d(C-G), strong immunoreactions were observed, demonstrating that the guanine base is involved in the binding of the diamine to DNA. 4. Monoclonal antibodies directed against different diamine-DNA adducts have shown that 80% of the in vitro metabolic activation involves the para amino group of the aromatic diamine. PMID:8498094

Citro, G; Galati, R; Verdina, A; Marini, S; Zito, R; Giardina, B

1993-03-01

346

In vitro activity of Alkanna frigida extracts in comparison with glucantime against Leishmania major  

PubMed Central

Background and Objectives Current chemotherapies of cutaneous leihmaniasis have faced to some problems and limitations; Development of new leishmanicidal drugs from different sources like herbal plants, are crucially important. The objective of the present study was evaluation of in vitro activity of Alkanna frigida extracts in comparison with glucantime against Leishmania major. Materials and Methods L. major promastigotes were exposed to different concentrations of the A. frigida extracts, processed by ethyl acetate, ethanol, hexane and chloroform. The inhibitory effect, as the IC50, were calculated after 24, 48 and 72 hours by linear regression analysis values of the concentrations employed. Results The significant inhibition was observed after 24 and 48 hours with different concentrations of compounds (p < 0.05 in all tests). All extracts had potent activity against proliferation of the promastigotes, comparing to the untreated negative control. It could compete with the glucantime efficacy in some concentrations. Ethyl acetate and ethanol extractions showed potent IC50 value, 106 µg/ml and 86 µg/ml, respectively. Hexane and chloroform extractions had poor efficacy after 24 hours; however, the efficacy increased after 48 and 72 hours. Conclusion The results indicated that the A. frigida has appropriate inhibitory effects on the growth of L. major promastigotes in vitro and can be of herbal targets for further investigation in vivo. PMID:23825738

Jafari, Fariba; Nourian, Abbasali; Fazaeli, Asghar; Yazdinezhad, Alireza; Haniloo, Ali

2013-01-01

347

Antimicrobial activity of artemisinin and precursor derived from in vitro plantlets of Artemisia annua L.  

PubMed

Artemisia annua L., a medicinal herb, produces secondary metabolites with antimicrobial property. In Malaysia due to the tropical hot climate, A. annua could not be planted for production of artemisinin, the main bioactive compound. In this study, the leaves of three in vitro A. annua L. clones were, extracted and two bioactive compounds, artemisinin and a precursor, were isolated by thin layer chromatography. These compounds were found to be effective in inhibiting the growth of Gram-positive and Gram-negative bacteria but not Candida albicans. Their antimicrobial activity was similar to that of antibactericidal antibiotic streptomycin. They were found to inhibit the growth of the tested microbes at the minimum inhibition concentration of 0.09?mg/mL, and toxicity test using brine shrimp showed that even the low concentration of 0.09?mg/mL was very lethal towards the brine shrimps with 100% mortality rate. This study hence indicated that in vitro cultured plantlets of A. annua can be used as the alternative method for production of artemisinin and its precursor with antimicrobial activities. PMID:24575401

Appalasamy, Suganthi; Lo, Kiah Yann; Ch'ng, Song Jin; Nornadia, Ku; Othman, Ahmad Sofiman; Chan, Lai-Keng

2014-01-01

348

In vitro antimicrobial activity of nanoconjugated vancomycin against drug resistant Staphylococcus aureus.  

PubMed

The mounting problem of antibiotic resistance of Staphylococcus aureus has prompted renewed efforts toward the discovery of novel antimicrobial agents. The present study was aimed to evaluate the in vitro antimicrobial activity of nanoconjugated vancomycin against vancomycin sensitive and resistant S. aureus strains. Folic acid tagged chitosan nanoparticles are used as Trojan horse to deliver vancomycin into bacterial cells. In vitro antimicrobial activity of nanoconjugated vancomycin against VSSA and VRSA strains was determined by minimum inhibitory concentration, minimum bactericidal concentration, tolerance and disc agar diffusion test. Cell viability and biofilm formation was assessed as indicators of pathogenicity. To establish the possible antimicrobial mechanism of nanoconjugated vancomycin, the cell wall thickness was studied by TEM study. The result of the present study reveals that nano-sized vehicles enhance the transport of vancomycin across epithelial surfaces, and exhibits its efficient drug-action which has been understood from studies of MIC, MBC, DAD of chitosan derivative nanoparticle loaded with vancomycin. Tolerance values distinctly showed that vancomycin loaded into nano-conjugate is very effective and has strong bactericidal effect on VRSA. These findings strongly enhanced our understanding of the molecular mechanism of nanoconjugated vancomycin and provide additional rationale for application of antimicrobial therapeutic approaches for treatment of staphylococcal pathogenesis. PMID:22841851

Chakraborty, Subhankari Prasad; Sahu, Sumanta Kumar; Pramanik, Panchanan; Roy, Somenath

2012-10-15

349

Phytochemical analysis and in vitro antimicrobial activity of two Satureja species essential oils.  

PubMed

The phytochemical GC[sol ]MS analysis and in vitro antimicrobial activity of the essential oils of the aerial parts of Satureja montana L. and Satureja cuneifolia Ten., collected in Croatia were performed. The major compound of S. montana oil was the phenolic monoterpene carvacrol (45.7%). Other important compounds were the monoterpenic hydrocarbons p-cymene (12.6%), gamma-terpinene (8.1%) and the oxygen-containing compounds carvacrol methyl ether, borneol, thymol and thymol methyl ether. The volatile oil of S. cuneifolia was characterized as beta-cubebene (8.7%), limonene (8.3%), alpha-pinene (6.9%), spathulenol and beta-caryophyllene. The antimicrobial effects of S. montana and S. cuneifolia oils were found to have a broad spectrum activity against multidrug-resistant pathogens by the broth microdilution method. These oils were active against all the test strains, with the exception of Pseudomonas aeruginosa. Compared with S. cuneifolia, savory oil exhibited greater antimicrobial activity. The maximum activity of savory oil was observed against Escherichia coli, methicillin-resistant Staphylococcus aureus and against the yeast (Candida albicans). The essential oil of S. cuneifolia was also found to inhibit the growth of medically important pathogens such as S. aureus and E. coli. Fungicidal activity for both oils against C. albicans and S. cerevisiae was also observed. PMID:15742345

Skocibusi?, Mirjana; Bezi?, Nada

2004-12-01

350

In Vitro Analysis of Finasteride Activity against Candida albicans Urinary Biofilm Formation and Filamentation  

PubMed Central

Candida albicans is the 3rd most common cause of catheter-associated urinary tract infections, with a strong propensity to form drug-resistant catheter-related biofilms. Due to the limited efficacy of available antifungals against biofilms, drug repurposing has been investigated in order to identify novel agents with activities against fungal biofilms. Finasteride is a 5-?-reductase inhibitor commonly used for the treatment of benign prostatic hyperplasia, with activity against human type II and III isoenzymes. We analyzed the Candida Genome Database and identified a C. albicans homolog of type III 5-?-reductase, Dfg10p, which shares 27% sequence identity and 41% similarity to the human type III 5-?-reductase. Thus, we investigated finasteride for activity against C. albicans urinary biofilms, alone and in combination with amphotericin B or fluconazole. Finasteride alone was highly effective in the prevention of C. albicans biofilm formation at doses of ?16 mg/liter and the treatment of preformed biofilms at doses of ?128 mg/liter. In biofilm checkerboard analyses, finasteride exhibited synergistic activity in the prevention of biofilm formation in a combination of 4 mg/liter finasteride with 2 mg/liter fluconazole. Finasteride inhibited filamentation, thus suggesting a potential mechanism of action. These results indicate that finasteride alone is highly active in the prevention of C. albicans urinary biofilms in vitro and has synergistic activity in combination with fluconazole. Further investigation of the clinical utility of finasteride in the prevention of urinary candidiasis is warranted. PMID:25049253

Chavez-Dozal, Alba A.; Lown, Livia; Jahng, Maximillian; Walraven, Carla J.

2014-01-01

351

Alternative activation of human plasmacytoid DCs in vitro and in melanoma lesions: involvement of LAG-3.  

PubMed

Plasmacytoid dendritic cells (pDCs) at tumor sites are often tolerogenic. Although pDCs initiate innate and adaptive immunity upon Toll-like receptor (TLR) triggering by pathogens, TLR-independent signals may be responsible for pDC activation and immune suppression in the tumor inflammatory environment. To identify molecules that are potentially involved in alternative pDC activation, we explored the expression and function of lymphocyte activation gene 3 (LAG-3) in human pDCs. In this report, we showed the expression of LAG-3 on the cell surface of a subset of circulating human pDCs. LAG-3+ pDCs exhibited a partially mature phenotype and were enriched at tumor sites in samples from melanoma patients. We found that LAG-3 interacted with major histocompatibility complex class II (MHC-II) to induce TLR-independent activation of pDCs with limited IFN? and enhanced IL-6 production. This in vitro cytokine profile of LAG-3-activated pDCs paralleled that of tumor-associated pDCs analyzed ex vivo. By confocal microscopy, LAG-3+ pDCs detected in melanoma-invaded lymph nodes (LNs) stained positive for IL-6 and preferentially localized near melanoma cells. These results suggest that LAG-3-mediated activation of pDCs takes place in vivo at tumor sites, and it is in part responsible for directing an immune-suppressive environment. PMID:24441096

Camisaschi, Chiara; De Filippo, Annamaria; Beretta, Valeria; Vergani, Barbara; Villa, Antonello; Vergani, Elisabetta; Santinami, Mario; Cabras, Antonello Domenico; Arienti, Flavio; Triebel, Frédéric; Rodolfo, Monica; Rivoltini, Licia; Castelli, Chiara

2014-07-01

352

Synthesis and In Vitro Antioxidant Activity of New 3-Substituted-2-Oxindole Derivatives  

PubMed Central

A series of new 1,3-dihydro-3-hydroxy-3-(2-phenyl-2-oxoethyl)-2H-indol-2-ones (1a-g) and 1,3-dihydro-3-(2-phenyl-2-oxoethylidene)-2H-indol-2-ones (2a-g) were synthesised by Knoevenagel condensation of substituted indole-2,3-diones (isatins) with various acetophenones. The synthesised compounds were characterised by their physical data, elemental, IR, 1H NMR, 13C NMR and mass spectral analyses and their in vitro antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl free radical scavenging assay. These compounds showed moderate to good antioxidant activities as compared with the standard, ascorbic acid. The antioxidant potential of 3-hydroxy-3-substituted oxindoles (1a-g) increased in a concentration-dependent manner from 10 to 500 ?g/ml with 5-fluoro and 5-methyl analogues showing maximum activity. Of 3-aroyl methylene indol-2-ones (2a-g), majority of compounds with halogen substitution at position 5 of isatin ring exhibited good antioxidant activity within a concentration range of 5-100 ?g/ml and the maximum activity was observed at 20 and 25 ?g/ml concentrations. Thus, our study provides evidence that some newly synthesised isatin derivatives exhibit substantial antioxidant activity at low concentrations. PMID:23716882

Gupta, A. K.; Kalpana, S.; Malik, J. K.

2012-01-01

353

Low concentrations of citrate reduce complement and granulocyte activation in vitro in human blood  

PubMed Central

Background The use of acetate in haemodialysis fluids may induce negative effects in patients including nausea and increased inflammation. Therefore, haemodialysis fluids where acetate is substituted with citrate have recently been developed. In this study, we investigated the biocompatibility of citrate employing concentrations used in haemodialysis. Methods The effects of citrate and acetate were investigated in human whole blood in vitro under conditions promoting biomaterial-induced activation. Complement activation was measured as generation of C3a, C5a and the sC5b-9 complex, and granulocyte activation as up-regulation of CD11b expression. For the experimental set-up, a mathematical model was created to calculate the concentrations of acetate and citrate attained during haemodialysis. Results Citrate reduced granulocyte activation and did not induce higher complement activation compared with acetate at concentrations attained during haemodialysis. Investigating different citrate concentrations clearly showed that citrate is a potent complement inhibitor already at low concentrations, i.e. 0.25 mM, which is comparable with concentrations detected in the blood of patients during dialysis with citrate-containing fluids. Increased citrate concentration up to 6 mM further reduced the activation of C3a, C5a and sC5b-9, as well as the expression of CD11b. Conclusions Our results suggest that citrate is a promising substitute for acetate for a more biocompatible dialysis, most likely resulting in less adverse effects for the patients. PMID:25713707

Huang, Shan; Sandholm, Kerstin; Jonsson, Nina; Nilsson, Anders; Wieslander, Anders; Grundström, Gunilla; Hancock, Viktoria; Ekdahl, Kristina N.

2015-01-01

354

Juglans mandshurica Maxim extracts exhibit antitumor activity on HeLa cells in vitro.  

PubMed

The present study examined the potential application of Juglans mandshurica Maxim extracts (HT) for cancer therapy by assessing their anti?proliferative activity, reduction of telomerase activity, induction of apoptosis and cell cycle arrest in S phase in HeLa cells. From the perspective of using HT as a herbal medicine, photomicroscopy and florescent microscopy techniques were utilized to characterize the effect of the extracts on telomerase activity and cell morphology. Flow cytometry was employed to study apoptosis and cell cycle of HeLa cells, and DNA laddering was performed. The results showed that HT inhibited cell proliferation and telomerase activity, induced apoptosis and caused S phase arrest of HeLa cells in vitro. HT inhibited HeLa cell proliferation significantly, and the highest inhibition rate was 83.7%. A trap?silver staining assay showed that HT was capable of markedly decreasing telomerase activity of HeLa cells and this inhibition was enhanced in a time? and dose?dependent manner. Results of a Hoechst 33258 staining assay showed that HeLa cells treated by HT induced cell death. Through DNA agarose gel electrophoresis, DNA ladders of HeLa cells treated with HT were observed, indicating apoptosis. In conclusion, the present study demonstrated that HT exhibited anti?tumor effects comprising the inhibition of growth and telomerase activity as well as apoptosis and cell cycle arrest in HeLa cells. PMID:24566804

Xin, Nian; Hasan, Murtaza; Li, Wei; Li, Yan

2014-04-01

355

Anticancer activity of litchi fruit pericarp extract against human breast cancer in vitro and in vivo.  

PubMed

Litchi fruit pericarp (LFP) extract contains significant amounts of polyphenolic compounds and exhibits powerful antioxidative activity against fat oxidation in vitro. The purpose of this study is to confirm the anticancer activity of LFP extract on human breast cancer in vitro and in vivo, and to elucidate the mechanism of its activity. Human breast cancer cells were tested in vitro for cytotoxicity, colony formation inhibition, BrdU incorporation, and gene expression profiling after treatment with LFP extract. Seven nude mice bearing human breast infiltrating duct carcinoma orthotopically were tested for its anticancer activity and expression of caspase-3 in vivo by oral administration of 0.3% (0.3 mg/ml) of LFP water-soluble crude ethanolic extract (CEE) for 10 weeks. LFP extract demonstrated a dose- and time-dependent inhibitory effect on cell growth (IC(50) = 80 microg/ml), and it significantly inhibited colony formation and BrdU incorporation of human breast cancer cells. Oligonucleotide microarray analysis identified 41(1.22%) up-regulated and 129 (3.84%) down-regulated genes after LFP water-soluble CEE treatment; the predominantly up-regulated genes were involved in various biological functions including cell cycle regulation and cell proliferation, apoptosis, signal transduction and transcriptional regulation, and extracellular matrix/adhesion molecules; and down-regulated genes were mainly associated with adhesion, invasion, and malignancy of cancer cells. A 40.70% tumor mass volume reduction and significant increase of casepase-3 protein expression were observed in vivo experiment. The findings in this study suggested that LFP extract might have potential anticancer activity on both ER positive and negative breast cancers, which could be attributed, in part, to its DNA damage effect, proliferating inhibition and apoptosis induction of cancer cells through up-regulation and down-regulation of multiple genes involved in cell cycle regulation and cell proliferation, apoptosis, signal transduction and transcriptional regulation, motility and invasiveness of cancer cells; ADP-ribosyltransferase (NAD+; poly (ADP-ribose) polymerase)-like 1 (ADPRTL1), Cytochrome P450, subfamily I (CYP1A1) and Hyaluronan-mediated motility receptor (HMMR) might be the main molecular targets at which LFP water-soluble CEE acted. PMID:16563451

Wang, Xiujie; Yuan, Shulan; Wang, Jing; Lin, Ping; Liu, Guanjian; Lu, Yanrong; Zhang, Jie; Wang, Wendong; Wei, Yuquan

2006-09-01

356

Anticancer activity of litchi fruit pericarp extract against human breast cancer in vitro and in vivo  

SciTech Connect

Litchi fruit pericarp (LFP) extract contains significant amounts of polyphenolic compounds and exhibits powerful antioxidative activity against fat oxidation in vitro. The purpose of this study is to confirm the anticancer activity of LFP extract on human breast cancer in vitro and in vivo, and to elucidate the mechanism of its activity. Human breast cancer cells were tested in vitro for cytotoxicity, colony formation inhibition, BrdU incorporation, and gene expression profiling after treatment with LFP extract. Seven nude mice bearing human breast infiltrating duct carcinoma orthotopically were tested for its anticancer activity and expression of caspase-3 in vivo by oral administration of 0.3% (0.3 mg/ml) of LFP water-soluble crude ethanolic extract (CEE) for 10 weeks. LFP extract demonstrated a dose- and time-dependent inhibitory effect on cell growth (IC{sub 5} = 80 {mu}g/ml), and it significantly inhibited colony formation and BrdU incorporation of human breast cancer cells. Oligonucleotide microarray analysis identified 41(1.22%) up-regulated and 129 (3.84%) down-regulated genes after LFP water-soluble CEE treatment; the predominantly up-regulated genes were involved in various biological functions including cell cycle regulation and cell proliferation, apoptosis, signal transduction and transcriptional regulation, and extracellular matrix/adhesion molecules; and down-regulated genes were mainly associated with adhesion, invasion, and malignancy of cancer cells. A 40.70% tumor mass volume reduction and significant increase of casepase-3 protein expression were observed in vivo experiment. The findings in this study suggested that LFP extract might have potential anticancer activity on both ER positive and negative breast cancers, which could be attributed, in part, to its DNA damage effect, proliferating inhibition and apoptosis induction of cancer cells through up-regulation and down-regulation of multiple genes involved in cell cycle regulation and cell proliferation, apoptosis, signal transduction and transcriptional regulation, motility and invasiveness of cancer cells; ADP-ribosyltransferase (NAD+; poly (ADP-ribose) polymerase)-like 1 (ADPRTL1), Cytochrome P450, subfamily I (CYP1A1) and Hyaluronan-mediated motility receptor (HMMR) might be the main molecular targets at which LFP water-soluble CEE acted.

Wang Xiujie [Division of Experimental Oncology, National Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China)]. E-mail: xiujiewang@yahoo.com; Yuan Shulan [Division of Experimental Oncology, National Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China); Wang Jing [Division of Experimental Oncology, National Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China); Lin Ping [Division of Experimental Oncology, National Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China); Liu Guanjian [Department of Clinical Epidemiology, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China); Lu Yanrong [Division of Experimental Oncology, National Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China); Zhang Jie [Division of Experimental Oncology, National Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China); Wang, Wendong [Department of Pathology of Public Health School, Sichuan University, Chengdu 610041, Sichuan Province (China); Wei Yuquan [Division of Biotherapy, National Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China)]. E-mail: yuquanwei@mail.sc.cninfo.net

2006-09-01

357

In vitro Activation of heme oxygenase-2 by menadione and its analogs  

PubMed Central

Background Previously, we reported that menadione activated rat, native heme oxygenase-2 (HO-2) and human recombinant heme oxygenase-2 selectively; it did not activate spleen, microsomal heme oxygenase-1. The purpose of this study was to explore some structure–activity relationships of this activation and the idea that redox properties may be an important aspect of menadione efficacy. Methods Heme oxygenase activity was determined in vitro using rat spleen and brain microsomes as the sources of heme oxygenase-1 and ?2, respectively, as well as recombinant, human heme oxygenase-2. Results Menadione analogs with bulky aliphatic groups at position-3, namely vitamins K1 and K2, were not able to activate HO-2. In contrast, several compounds with similar bulky but less lipophilic moieties at position-2 (and ?3) were able to activate HO-2 many fold; these compounds included polar, rigid, furan-containing naphthoquinones, furan-benzoxazine naphthoquinones, 2-(aminophenylphenyl)-3-piperidin-1-yl naphthoquinones. To explore the idea that redox properties might be involved in menadione efficacy, we tested analogs such as 1,4-dimethoxy-2-methylnaphthalene, pentafluoromenadione, monohalogenated naphthoquinones, ?-tetralone and 1,4-naphthoquinone. All of these compounds were inactive except for 1,4-naphthoquinone. Menadione activated full-length recombinant human heme oxygenase-2 (FL-hHO-2) as effectively as rat brain enzyme, but it did not activate rat spleen heme oxygenase. Conclusions These observations are consistent with the idea that naphthoquinones such as menadione bind to a receptor in HO-2 and activate the enzyme through a mechanism that may involve redox properties. PMID:24533775

2014-01-01

358

Ethnopharmacological in vitro studies on Austria's folk medicine—An unexplored lore in vitro anti-inflammatory activities of 71 Austrian traditional herbal drugs?  

PubMed Central

Ethnopharmacological relevance In Austria, like in most Western countries, knowledge about traditional medicinal plants is becoming scarce. Searching the literature concerning Austria's ethnomedicine reveals its scant scientific exploration. Aiming to substantiate the potential of medicinal plants traditionally used in Austria, 63 plant species or genera with claimed anti-inflammatory properties listed in the VOLKSMED database were assessed for their in vitro anti-inflammatory activity. Material and methods 71 herbal drugs from 63 plant species or genera were extracted using solvents of varying polarities and subsequently depleted from the bulk constituents, chlorophylls and tannins to avoid possible interferences with the assays. The obtained 257 extracts were assessed for their in vitro anti-inflammatory activity. The expression of the inflammatory mediators E-selectin and interleukin-8 (IL-8), induced by the inflammatory stimuli tumor necrosis factor alpha (TNF-?) and the bacterial product lipopolysaccharide (LPS) was measured in endothelial cells. The potential of the extracts to activate the nuclear factors PPAR? and PPAR? and to inhibit TNF-?-induced activation of the nuclear factor-kappa B (NF-?B) in HEK293 cells was determined by luciferase reporter gene assays. Results In total, extracts from 67 of the 71 assessed herbal drugs revealed anti-inflammatory activity in the applied in vitro test systems. Thereby, 30 could downregulate E-selectin or IL-8 gene expression, 28 were strong activators of PPAR? or PPAR? (inducing activation of more than 2-fold at a concentration of 10 µg/mL) and 21 evoked a strong inhibition of NF-?B (inhibition of more than 80% at 10 µg/mL). Conclusion Our research supports the efficacy of herbal drugs reported in Austrian folk medicine used for ailments associated with inflammatory processes. Hence, an ethnopharmacological screening approach is a useful tool for the discovery of new drug leads. PMID:23770053

Vogl, Sylvia; Picker, Paolo; Mihaly-Bison, Judit; Fakhrudin, Nanang; Atanasov, Atanas G.; Heiss, Elke H.; Wawrosch, Christoph; Reznicek, Gottfried; Dirsch, Verena M.; Saukel, Johannes; Kopp, Brigitte

2013-01-01

359

In Vitro Antioxidant Activity of Selected 4-Hydroxy-chromene-2-one Derivatives—SAR, QSAR and DFT Studies  

PubMed Central

The series of fifteen synthesized 4-hydroxycoumarin derivatives was subjected to antioxidant activity evaluation in vitro, through total antioxidant capacity, 1,1-diphenyl-2-picryl-hydrazyl (DPPH), hydroxyl radical, lipid peroxide scavenging and chelating activity. The highest activity was detected during the radicals scavenging, with 2b, 6b, 2c, and 4c noticed as the most active. The antioxidant activity was further quantified by the quantitative structure-activity relationships (QSAR) studies. For this purpose, the structures were optimized using Paramethric Method 6 (PM6) semi-empirical and Density Functional Theory (DFT) B3LYP methods. Bond dissociation enthalpies of coumarin 4-OH, Natural Bond Orbital (NBO) gained hybridization of the oxygen, acidity of the hydrogen atom and various molecular descriptors obtained, were correlated with biological activity, after which we designed 20 new antioxidant structures, using the most favorable structural motifs, with much improved predicted activity in vitro. PMID:21686153

Mladenovi?, Milan; Mihailovi?, Mirjana; Bogojevi?, Desanka; Mati?, Sanja; Ni?iforovi?, Neda; Mihailovi?, Vladimir; Vukovi?, Nenad; Sukdolak, Slobodan; Soluji?, Slavica

2011-01-01

360

In vitro antioxidant activity of selected 4-hydroxy-chromene-2-one derivatives-SAR, QSAR and DFT studies.  

PubMed

The series of fifteen synthesized 4-hydroxycoumarin derivatives was subjected to antioxidant activity evaluation in vitro, through total antioxidant capacity, 1,1-diphenyl-2-picryl-hydrazyl (DPPH), hydroxyl radical, lipid peroxide scavenging and chelating activity. The highest activity was detected during the radicals scavenging, with 2b, 6b, 2c, and 4c noticed as the most active. The antioxidant activity was further quantified by the quantitative structure-activity relationships (QSAR) studies. For this purpose, the structures were optimized using Paramethric Method 6 (PM6) semi-empirical and Density Functional Theory (DFT) B3LYP methods. Bond dissociation enthalpies of coumarin 4-OH, Natural Bond Orbital (NBO) gained hybridization of the oxygen, acidity of the hydrogen atom and various molecular descriptors obtained, were correlated with biological activity, after which we designed 20 new antioxidant structures, using the most favorable structural motifs, with much improved predicted activity in vitro. PMID:21686153

Mladenovi?, Milan; Mihailovi?, Mirjana; Bogojevi?, Desanka; Mati?, Sanja; Ni?iforovi?, Neda; Mihailovi?, Vladimir; Vukovi?, Nenad; Sukdolak, Slobodan; Soluji?, Slavica

2011-01-01

361

In vitro activity of linezolid as assessed through the 2013 LEADER surveillance program.  

PubMed

The 2013 LEADER surveillance program monitored the in vitro activity of linezolid and comparator agents against Gram-positive bacteria at 60 medical centers in the United States. A total of 7183 pathogens were contributed from 6 predetermined pathogen groups. The groups were Staphylococcus aureus, coagulase-negative staphylococci, enterococci, Streptococcus pneumoniae, ?-hemolytic streptococci, and viridans group streptococci. The MIC90 value for each of the 6 pathogen groups was 1?g/mL. Susceptibility of "all organisms" to linezolid was 99.83%. Only 12 isolates (2 S. aureus, 3 Staphylococcus epidermidis, 1 Streptococcus sanguinis, 5 Enterococcus faecium, and 1 Enterococcus faecalis) were nonsusceptible to linezolid (0.17%). Three of these (2 S. aureus and 1 E. faecium) harbored the cfr resistance mechanism. The findings indicate that linezolid activity remains stable, although there are examples of clonal dissemination within several monitored institutions. PMID:25633420

Flamm, Robert K; Mendes, Rodrigo E; Hogan, Patricia A; Ross, James E; Farrell, David J; Jones, Ronald N

2015-04-01

362

In vivo anti-inflammatory and in vitro antioxidant activities of Mediterranean dietary plants.  

PubMed

Five hydroalcoholic extracts of edible plants from Calabria region (Italy) used in local traditional medicine for the treatment of inflammatory diseases were evaluated for their in vivo topical anti-inflammatory activity (inhibition of croton oil-induced ear oedema in mice) and in vitro antioxidant and antiradical properties (inhibition of linoleic acid oxidation and bovine brain liposomes peroxidation, DPPH radical scavenging). All the extracts showed an anti-inflammatory effect: 300 microg/cm(2) provoked oedema reductions ranging from 21 to 27%. All the extracts exerted also radical scavenging and/or antioxidant properties, the most active plant being Mentha aquatica L. (Lamiaceae) which contained the highest amount of phenolics (337 mg/g) and of flavonoids (15.75 mg/g). Moreover, the content and the composition of sterols were assessed by GC-MS in the examined plants Borago officinalis L. (Boraginaceae) contained the highest number of sterols. PMID:18164564

Conforti, Filomena; Sosa, Silvio; Marrelli, Mariangela; Menichini, Federica; Statti, Giancarlo A; Uzunov, Dimitar; Tubaro, Aurelia; Menichini, Francesco; Loggia, Roberto Della

2008-02-28

363

Augmentation of natural killer cell activity in vitro against tumor cells by wild plants from Jordan.  

PubMed

Thirteen aqueous extracts prepared from Jordanian plants, that are currently used in traditional medicine to treat various types of cancer, were tested in mice for their ability to augment natural killer (NK) cell function in vitro in generating cytotoxicity against YAC tumor targets. Lymphoid cells at a concentration of 5x10(6)/ml were incubated in medium alone or in medium containing different dilutions of either plant extract or purified interferon alpha for 20 h and tested for NK activity. Maximum NK activity (62. 3%) was obtained at 1:50 dilution of Nigella sativum fresh aqueous extract, 48.5% at 1:100 dilution for Allium sativum (and 38.3% at 1:50 dilution for Onopordum acanthium. Fresh aqueous plant extracts appeared to be more potent than old dried aqueous extract or ethanolic extracts. NK augmentation by plant extracts using nylon wool non-adherent spleen cells was slightly higher than the whole spleen cells. PMID:10904146

Abuharfeil, N M; Maraqa, A; Von Kleist, S

2000-07-01

364

Inhibition of iron induced lipid peroxidation and antioxidant activity of Indian spices and Acacia in vitro.  

PubMed

The spices used in the Indian foods such as Star anise (Illicium verum), Bay leaves (Cinnamomum zeylanicum) and Cobra's saffron (Mesua ferrea), and Acacia (Acacia catechu), which have medicinal value, were used as test samples, to find their effect on in vitro lipid peroxidation (LPO). Rat liver post mitochondrial supernatant (PMS) in Tris HCl buffer, pH 7.4 was incubated for 0 and 1 h, with various test extracts in three different oxidant systems. The results show that addition of test samples to FeCl(3) medium at 0 h significantly stop the initiation of the LPO. However, the propagation phase of LPO was inhibited by Cobra's saffron and Acacia and not by Star anise and Bay leaves. The test samples also showed strong reducing power and superoxide radical scavenging activity. Cobra's saffron and Acacia showed the highest antioxidant activity, probably due to the higher polyphenol content as compared to other test samples. PMID:20033297

Yadav, Amit Singh; Bhatnagar, Deepak

2010-03-01

365

Triazole derivatives with improved in vitro antifungal activity over azole drugs  

PubMed Central

A series of triazole antifungal agents with piperidine side chains was designed and synthesized. The results of antifungal tests against eight human pathogenic fungi in vitro showed that all the compounds exhibited moderate-to-excellent activities. Molecular docking between 8d and the active site of Candida albicans CYP51 was provided based on the computational docking results. The triazole interacts with the iron of the heme group. The difluorophenyl group is located in the S3 subsite and its fluorine atom (2-F) can form H-bonds with Gly307. The side chain is oriented into the S4 subsite and formed hydrophobic and van der Waals interactions with the amino residues. Moreover, the phenyl group in the side chain interacts with the phenol group of Phe380 through the formation of ?–? face-to-edge interactions. PMID:24748772

Yu, Shichong; Chai, Xiaoyun; Wang, Yanwei; Cao, Yongbing; Zhang, Jun; Wu, Qiuye; Zhang, Dazhi; Jiang, Yuanying; Yan, Tianhua; Sun, Qingyan

2014-01-01

366

Antibacterial activity of aqueous extracts of Indian chewing sticks on dental plaque: An in vitro study.  

PubMed

The anti-microbial efficacy of aqueous extracts of Indian chewing sticks against different kinds of plaque bacteria in vitro was investigated. Supra-gingival plaque is cultured and subjected to the antibacterial activity of the aqueous extracts of chewing sticks (Neem, Acacia, Pongamia glabra, Achyranthes aspera, Streblus asper) separately. The results of the study demonstrate that all the five chewing sticks under study possess inhibitory potential against bacteria present in dental plaque mainly on aerobes. The antibacterial efficacy of aqueous extracts has antibacterial effects and could be used as a therapeutic agent and therefore, it appears to be potent anti-microbial agents that could be considered as a medicinal plant. Results of this study showed chewing sticks contained antibacterial agents, but the concentration and composition of the active substances differed among the plants. PMID:25210357

Rao, Dola Srinivasa; Penmatsa, Tanuja; Kumar, Alapati Kranthi; Reddy, M Narendra; Gautam, Nalam Sai; Gautam, Nalam Radhika

2014-07-01

367

Evaluation of in Vitro and in Vivo Depigmenting Activity of Raspberry Ketone from Rheum officinale  

PubMed Central

Melanogenesis inhibition by raspberry ketone (RK) from Rheum officinale was investigated both in vitro in cultivated murine B16 melanoma cells and in vivo in zebrafish and mice. In B16 cells, RK inhibited melanogenesis through a post-transcriptional regulation of tyrosinase gene expression, which resulted in down regulation of both cellular tyrosinase activity and the amount of tyrosinase protein, while the level of tyrosinase mRNA transcription was not affected. In zebrafish, RK also inhibited melanogenesis by reduction of tyrosinase activity. In mice, application of a 0.2% or 2% gel preparation of RK applied to mouse skin significantly increased the degree of skin whitening within one week of treatment. In contrast to the widely used flavoring properties of RK in perfumery and cosmetics, the skin-whitening potency of RK has been demonstrated in the present study. Based on our findings reported here, RK would appear to have high potential for use in the cosmetics industry. PMID:21954327

Lin, Chia-Hsiang Victor; Ding, Hsiou-Yu; Kuo, Shiou-Yi; Chin, Ling-Wei; Wu, Jiumn-Yih; Chang, Te-Sheng

2011-01-01

368

In vitro antioxidant activities of leaf and root extracts of Albizia antunesiana harms.  

PubMed

The antioxidative activities of the ethanol and aqueous extracts of the leaf and root samples of Albizia antunesiana were determined across a series of four in vitro models. The results showed that all the extracts had reducing power (Fe(3+)- Fe2+), DPPH, hydroxyl and nitric oxide radical scavenging abilities. The ethanol root extract had more potent antioxidant power in all the experimental models and possesses a higher total phenol content of 216.6 +/- 6.7 mg/g. The GC-MS analysis of the aqueous and ethanol extracts of the roots and leaves indicated that several aromatic phenolic compounds, a coumarin and some common triterpenoids were present in these extracts. Data from this study suggest that the leaves and roots of Albizia antunesiana possessed antioxidative activities that varied depending on the solvents. PMID:24383327

Chipiti, Talent; Ibrahim, Mohammed Auwal; Koorbanally, Neil Anthony; Islam, Md Shahidul

2013-01-01

369

Coffee with cinnamon - impact of phytochemicals interactions on antioxidant and anti-inflammatory in vitro activity.  

PubMed

This paper evaluates the potential bioaccessibility and interactions between antiradical and anti-inflammatory compounds from coffee and cinnamon. Results obtained for whole plant material extracts were compared with those for chlorogenic and cinnamic acids (the main bioactive constituents of the study material). All samples, coffee, cinnamon and a mixture of the two showed abilities to scavenge free radicals and to inhibit lipoxygenase (LOX) activity. Both activities increased after simulated gastrointestinal digestion. In the mixture antiradical phytochemicals acted antagonistically - isoboles adopted the convex form. The same interactions were determined for chemical standards. The water-extractable LOX inhibitors acted synergistically - the isobole curve was "concave". The same type of interaction was determined for standard compounds. Interestingly, after digestion in vitro a slight antagonism in the action of LOX inhibitors was observed. The results show that the food matrix and/or its changes during digestion may play an important role in creating the biological properties. PMID:24874360

Durak, Agata; Gawlik-Dziki, Urszula; Pecio, Lukasz

2014-11-01

370

In vitro antimicrobial activity of methanolic leaf extract of Psidium guajava L.  

PubMed Central

Aim: This study was designed to examine the chemical composition and in vitro antimicrobial potential of methanolic extract of Psidium guajava Linn (Myrtaceae). Materials and Methods: The inhibitory effect of methanolic extract of P. guajava was tested against three bacterial and two fungal strains by using the paper disc diffusion method. Results: The methanolic extract exhibited antibacterial activity against E. coli with minimum inhibitory concentration, 0.78 ?g/ml, minimum bactericidal concentration of 50 ?g/ml, and appreciable antifungal activity with minimum inhibitory concentration of 12.5 ?g/ml. Preliminary phytochemical analysis of methanolic extract revealed the presence of antimicrobial compounds such as flavonoids, steroids, and tannins, which may contribute for the antimicrobial action of P. guajava. Conclusion: The extract was found to be bacteriostatic and fungistatic in action. PMID:21687350

Dhiman, Anju; Nanda, Arun; Ahmad, Sayeed; Narasimhan, B.

2011-01-01

371

Optimization of ultrasonic-assisted extraction and in vitro antioxidant activities of polysaccharides from Trametes orientalis.  

PubMed

A Box-Behnken design was employed to optimize ultrasonic-assisted extraction of Trametes orientalis polysaccharides (TOP). The crude polysaccharides were purified by DEAE cellulose-52 chromatography, giving a main fraction named as PTOP. The antioxidant properties of PTOP were evaluated by different in vitro antioxidant assays, such as 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activities, reducing power, superoxide radical scavenging activities, and chelating ability of ferrous ions. The results showed that optimal extraction parameters were as follows: ratio of water to raw material 30.6 mL/g, ultrasonic power 109.8 W, extraction temperature 40.2 °C, and extraction time 42.2 min. Under these conditions, the experimental yield of polysaccharides was 7.49 ± 0.14%, which agreed closely with the predicted value (7.47%). Furthermore, PTOP exhibited antioxidant capacity in a concentration-dependent manner in all assays. PMID:25037357

Zheng, Yi; Li, Yong; Wang, Wei-dong

2014-10-13

372

Antibacterial activity of aqueous extracts of Indian chewing sticks on dental plaque: An in vitro study  

PubMed Central

The anti-microbial efficacy of aqueous extracts of Indian chewing sticks against different kinds of plaque bacteria in vitro was investigated. Supra-gingival plaque is cultured and subjected to the antibacterial activity of the aqueous extracts of chewing sticks (Neem, Acacia, Pongamia glabra, Achyranthes aspera, Streblus asper) separately. The results of the study demonstrate that all the five chewing sticks under study possess inhibitory potential against bacteria present in dental plaque mainly on aerobes. The antibacterial efficacy of aqueous extracts has antibacterial effects and could be used as a therapeutic agent and therefore, it appears to be potent anti-microbial agents that could be considered as a medicinal plant. Results of this study showed chewing sticks contained antibacterial agents, but the concentration and composition of the active substances differed among the plants. PMID:25210357

Rao, Dola Srinivasa; Penmatsa, Tanuja; Kumar, Alapati Kranthi; Reddy, M. Narendra; Gautam, Nalam Sai; Gautam, Nalam Radhika

2014-01-01

373

Novel Diamidines with Activity against Babesia divergens In Vitro and Babesia microti In Vivo ?  

PubMed Central

Dicationic diamidines, such as diminazene and pentamidine, are well-studied chemotherapeutic agents with significant activity against parasitic diseases. The in vitro activities of novel diamidine compounds against the Babesia divergens strains 1903B and 4201 were investigated. The most potent compound, a diphenyl furan, had a 50% inhibitory concentration (IC50) of 1.5 ng/ml. In a murine model, several test compounds were effective enough to cure mice infected with Babesia microti at a dose of 12.5 and/or 25 mg/kg of body weight given by the subcutaneous route for 4 days. The best antibabesial properties were exhibited by terphenyls, benzimidazoles, diphenyl furans, pentamidine, and pentamidine analogues. PMID:21537025

Nehrbass-Stuedli, Angela; Boykin, David; Tidwell, Richard R.; Brun, Reto

2011-01-01

374

Inhibitory Activities of Cudrania tricuspidata Leaves on Pancreatic Lipase In Vitro and Lipolysis In Vivo  

PubMed Central

To identify effective herb to treat obesity, we screened 115 herbal extracts for inhibition of porcine pancreatic lipase (triacylg-ycerol acylhydrolase, EC 3.1.1.3) activity in vitro. Of the extracts tested, Cudrania tricuspidata leaves exhibited the most pronounced inhibitory effect on lipase activity with an IC50 value of 9.91??g/mL. Antilipid absorption effects of C. tricuspidata leaves were examined in rats after oral administration of lipid emulsions containing 50 or 250?mg??C. tricuspidata/kg body weight. Plasma triacylglycerol levels 2?h after the oral administration of emulsions containing C. tricuspidata were significantly reduced compared to the untreated group (P < 0.05). These results suggest that C. tricuspidata leaves may be useful for the treatment of obesity. PMID:23365603

Kim, Young Sook; Lee, Youngseop; Kim, Junghyun; Sohn, Eunjin; Kim, Chan Sik; Lee, Yun Mi; Jo, Kyuhyung; Shin, Sodam; Song, Yoojin; Kim, Joo Hwan; Kim, Jin Sook

2012-01-01

375

Evaluation of in vitro and in vivo depigmenting activity of raspberry ketone from Rheum officinale.  

PubMed

Melanogenesis inhibition by raspberry ketone (RK) from Rheum officinale was investigated both in vitro in cultivated murine B16 melanoma cells and in vivo in zebrafish and mice. In B16 cells, RK inhibited melanogenesis through a post-transcriptional regulation of tyrosinase gene expression, which resulted in down regulation of both cellular tyrosinase activity and the amount of tyrosinase protein, while the level of tyrosinase mRNA transcription was not affected. In zebrafish, RK also inhibited melanogenesis by reduction of tyrosinase activity. In mice, application of a 0.2% or 2% gel preparation of RK applied to mouse skin significantly increased the degree of skin whitening within one week of treatment. In contrast to the widely used flavoring properties of RK in perfumery and cosmetics, the skin-whitening potency of RK has been demonstrated in the present study. Based on our findings reported here, RK would appear to have high potential for use in the cosmetics industry. PMID:21954327

Lin, Chia-Hsiang Victor; Ding, Hsiou-Yu; Kuo, Shiou-Yi; Chin, Ling-Wei; Wu, Jiumn-Yih; Chang, Te-Sheng

2011-01-01

376

Endophytic fungi diversity of aquatic/riparian plants and their antifungal activity in vitro.  

PubMed

Two hundred and fourteen endophytic fungi were isolated from 500 segments of aquatic/riparian plants Ottelia acuminata, Myriophyllum verticillatum, Equisetum arvense, Cardamine multijuga, and Impatiens chinensis. They were identified to 31 taxa in which Cladosporium, Fusarium, and Geotrichum were the dominant genera. Among all isolates, 169 (79%) were anamorphic fungi, 1 (0.5%) was an teleomorphic ascomycete and 44 (21%) were sterile mycelia. There were significant differences in the colonization frequency of endophytes between the five plant species (X~2=51.128, P<0.001, Chi-square test). The riparian plants harboured more endophytes than the submerged plants. The antifungal activity of these isolates against Fusarium solani and Phytophthora nicotianae in vitro were tested and 28 (13.1%) isolates showed antifungal activities with more than 30% growth inhibition rate against the two pathogens. PMID:20221722

Li, Hai-Yan; Zhao, Chun-An; Liu, Chen-Jian; Xu, Xiao-Fei

2010-02-01

377

Triazole derivatives with improved in vitro antifungal activity over azole drugs.  

PubMed

A series of triazole antifungal agents with piperidine side chains was designed and synthesized. The results of antifungal tests against eight human pathogenic fungi in vitro showed that all the compounds exhibited moderate-to-excellent activities. Molecular docking between 8d and the active site of Candida albicans CYP51 was provided based on the computational docking results. The triazole interacts with the iron of the heme group. The difluorophenyl group is located in the S3 subsite and its fluorine atom (2-F) can form H-bonds with Gly307. The side chain is oriented into the S4 subsite and formed hydrophobic and van der Waals interactions with the amino residues. Moreover, the phenyl group in the side chain interacts with the phenol group of Phe380 through the formation of ?-? face-to-edge interactions. PMID:24748772

Yu, Shichong; Chai, Xiaoyun; Wang, Yanwei; Cao, Yongbing; Zhang, Jun; Wu, Qiuye; Zhang, Dazhi; Jiang, Yuanying; Yan, Tianhua; Sun, Qingyan

2014-01-01

378

Patterns of inspiratory phase-dependent activity in the in vitro respiratory network  

PubMed Central

Mechanistic descriptions of rhythmogenic neural networks have often relied on ball-and-stick diagrams, which define interactions between functional classes of cells assumed to be reasonably homogenous. Application of this formalism to networks underlying respiratory rhythm generation in mammals has produced increasingly intricate models that have generated significant insight, but the underlying assumption that individual cells within these network fall into distinct functional classes has not been rigorously tested. In the present study we used multiunit extracellular recording in the in vitro pre-Bötzinger complex to identify and characterize the rhythmic activity of 951 cells. Inspiratory phase-dependent activity was estimated for all cells, and the data set as a whole was analyzed with principal component analysis, nonlinear dimensionality reduction, and hierarchical clustering techniques. None of these techniques revealed categorically distinct functional cell classes, indicating instead that the behavior of these cells within the network falls along several continua of spiking behavior. PMID:23076109

Carroll, Michael S.; Viemari, Jean-Charles

2013-01-01

379

In vitro antifungal activities of isavuconazole and comparators against rare yeast pathogens.  

PubMed

We compared the in vitro activities of isavuconazole, posaconazole, voriconazole, and fluconazole against Dipodascus capitatus (n = 21), Saccharomyces cerevisiae (n = 20), Rhodotorula mucilaginosa (n = 18), and Trichosporon spp. (n = 15). The MIC(50)s, MIC(90)s, and MIC ranges (in microg/ml) obtained using the CLSI M27-A3 procedure were as follows: isavuconazole, 0.125, 0.5, and < or = 0.015 to 2; posaconazole, 0.5, 2, and < or = 0.015 to > 16; voriconazole, 0.125, 2, and < or = 0.015 to 8; and fluconazole, 4, > 128, and < or = 0.125 to > 128. Isavuconazole showed potent activity against the isolates studied. PMID:20566770

Guinea, Jesús; Recio, Sandra; Escribano, Pilar; Peláez, Teresa; Gama, Beatriz; Bouza, Emilio

2010-09-01

380

In vitro antioxidant activities of sulfated polysaccharide fractions extracted from Corallina officinalis.  

PubMed

Sulfated polysaccharides (F1, F2) from seaweed Corallina officinalis were isolated through anion-exchange column chromatography. Their chemical characteristics were determined by GC, HPLC, FT-IR and UV spectra. F1 and F2 contained only two monosaccharides, namely galactose and xylose. The antioxidant activities of F1, F2 and the de-sulfated polysaccharides (DF-1, DF-2) in vitro were investigated, including hydroxyl radicals scavenging effect, superoxide radical scavenging capacity, DPPH radical activity and reducing power. As expected, antioxidant assay showed that the two sulfated polysaccharide fractions (F1, F2) possessed considerable antioxidant properties and had more excellent abilities than de-sulfated polysaccharides (DF-1, DF-2). PMID:21896282

Yang, Yuling; Liu, Dan; Wu, Jun; Chen, Yan; Wang, Shusheng

2011-12-01

381

Selection of a T7 promoter mutant with enhanced in vitro activity by a novel multi-copy bead display approach for in vitro evolution.  

PubMed

In vitro evolution of nucleic acids and proteins is a powerful strategy to optimize their biological and physical properties. To select proteins with the desired phenotype from large gene libraries, the proteins need to be linked to the gene they are encoded by. To facilitate selection of the desired phenotype and isolation of the encoding DNA, a novel bead display approach was developed, in which each member of a library of beads is first linked to multiple copies of a clonal gene variant by emulsion polymerase chain reaction. Beads are transferred to a second emulsion for an in vitro transcription-translation reaction, in which the protein encoded by each bead's amplicon covalently binds to the bead present in the same picoliter reactor. The beads then contain multiple copies of a clonal gene variant and multiple molecules of the protein encoded by the bead's gene variant and serve as the unit of selection. As a proof of concept, we screened a randomized library of the T7 promoter for high expression levels by flow cytometry and identified a T7 promoter variant with an ~10-fold higher in vitro transcriptional activity, confirming that the multi-copy bead display approach can be efficiently applied to in vitro evolution. PMID:23074193

Paul, Siddhartha; Stang, Alexander; Lennartz, Klaus; Tenbusch, Matthias; Überla, Klaus

2013-01-01

382

Selection of a T7 promoter mutant with enhanced in vitro activity by a novel multi-copy bead display approach for in vitro evolution  

PubMed Central

In vitro evolution of nucleic acids and proteins is a powerful strategy to optimize their biological and physical properties. To select proteins with the desired phenotype from large gene libraries, the proteins need to be linked to the gene they are encoded by. To facilitate selection of the desired phenotype and isolation of the encoding DNA, a novel bead display approach was developed, in which each member of a library of beads is first linked to multiple copies of a clonal gene variant by emulsion polymerase chain reaction. Beads are transferred to a second emulsion for an in vitro transcription–translation reaction, in which the protein encoded by each bead’s amplicon covalently binds to the bead present in the same picoliter reactor. The beads then contain multiple copies of a clonal gene variant and multiple molecules of the protein encoded by the bead’s gene variant and serve as the unit of selection. As a proof of concept, we screened a randomized library of the T7 promoter for high expression levels by flow cytometry and identified a T7 promoter variant with an ?10-fold higher in vitro transcriptional activity, confirming that the multi-copy bead display approach can be efficiently applied to in vitro evolution. PMID:23074193

Paul, Siddhartha; Stang, Alexander; Lennartz, Klaus; Tenbusch, Matthias; Überla, Klaus

2013-01-01

383

Assessment of antioxidant activity of eugenol in vitro and in vivo.  

PubMed

Reactive oxygen species are implicated in many human diseases and aging process. Much of the evidence is based on experimental data indicating increasing rates of lipid peroxidation in disease states and the ameliorating effects of antioxidants. It is becoming increasingly evident that the natural antioxidants, which have phenolic structure, play an important role in protecting the tissues against free radical damage. Eugenol (4-allyl-2 methoxyphenol) is one such naturally occurring phenolic compound. The antioxidant activity of eugenol was evaluated by the extent of protection offered against free radical-mediated lipid peroxidation using both in vitro and in vivo studies. The in vitro lipid peroxidation was induced in mitochondria by (Fe(II)-ascorbate) or (Fe(II) + H(2)O(2)). The lipid peroxidation was assessed colorimetrically by measuring the formation of thiobarbituric acid reactive substances (TBARS) following the reaction of oxidized lipids with TBA. Eugenol completely inhibited both iron and Fenton reagent-mediated lipid peroxidation. The inhibitory activity of eugenol was about fivefold higher than that observed for alpha-tocopherol and about tenfold less than that observed for BHT. The in vivo lipid peroxidation-mediated liver damage was induced by administration of CCl(4) to rats. Eugenol significantly inhibited the rise in SGOT activity and cell necrosis without protecting the endoplasmic reticulum (ER) damage as assessed by its failure to prevent a decrease in cytochrome p450 and G-6-phosphatase activity. The protective action of eugenol has been found to be due to interception of secondary radicals derived from ER lipids rather than interfering with primary radicals of CCl(4) (CCl(3)/CCl(3)OO). PMID:20013178

Nagababu, Enika; Rifkind, Joseph M; Boindala, Sesikeran; Nakka, Lakshmaiah

2010-01-01

384

The Effect of Bioactive Compounds on In Vitro and In Vivo Antioxidant Activity of Different Berry Juices  

PubMed Central

Background Berry fruit is known for its high contents of various bioactive compounds. The latter constitute of anthocyanins, flavonols and flavanols and posses high antioxidative activity. The highly dynamic antioxidant system can be evaluated in vitro and in vivo in several model organisms. These measurements represent a good approximation of the real potential of bioactive compounds in the cells of higher eucarions. The aim of the study was thus to determine in vitro and in vivo antioxidant activity of different berry juices, which reportedly contain high amounts of phenolics. Methodology/Principal Findings Five different berry species were collected from several locations in central Slovenia and juice was extracted from each species separately. Juice was assessed for their in vitro and in vivo antioxidant activity. Phenolic profiles of berries were determined with the use of a HPLC/MS system, in vitro antioxidant activity with the DPPH radical scavenging method and in vivo antioxidative activity using Saccharomyces cerevisiae. The highest diversity of individual phenols was detected for bilberry juice. The highest in vitro antioxidant capacity was determined for blackcurrant juice. A decrease in intracellular oxidation compared to control was observed in the following order: blackcurrant < chokeberry?=?blueberry < bilberry. The results indicate important differences in antioxidant activity of berry juices between in vitro and in vivo studies. Conclusion/Significance In addition to the total content of phenolic compounds entering the cells, a key factor determining antioxidative activity of berry juices is also the ratio between the compounds. Where high content levels of anthocyanins and very low content levels of flavonols and hydroxycinnamic acids were measured a lower intracellular oxidation has been detected. Specifically, intracellular oxidation increased with higher consumption of hydroxycinnamic acids and lower consumption of anthocyanins in the cells. Antioxidative activity also increased when the consumption of analyzed phenols was rather low. PMID:23110118

Slatnar, Ana; Jakopic, Jerneja; Stampar, Franci; Veberic, Robert; Jamnik, Polona

2012-01-01

385

In Vitro Activities of Voriconazole, Itraconazole, and Terbinafine Alone or in Combination against Pythium insidiosum Isolates from Brazil?  

PubMed Central

We evaluated the in vitro activities of voriconazole, itraconazole, and terbinafine against 30 clinical isolates of Pythium insidiosum using a checkerboard macrodilution method. The combined activity of terbinafine plus itraconazole or plus voriconazole was synergic against 17% of the strains. Antagonism was not observed. PMID:18056274

Argenta, Juliana S.; Santurio, Janio M.; Alves, Sydney H.; Pereira, Daniela I. B.; Cavalheiro, Ayrton S.; Spanamberg, Andréia; Ferreiro, Laerte

2008-01-01

386

In vitro effect of a fish gonadotropin on aromatase and 17 ?-hydroxysteroid dehydrogenase activities in the ovary  

E-print Network

In vitro effect of a fish gonadotropin on aromatase and 17 ?-hydroxysteroid dehydrogenase activities in the ovary of the rainbow trout (Salmo gairdneri Rich.) O. SIRE, J. DÉPĘCHE Université Pierre. Summary. Aromatase activity has been studied in the rainbow trout ovary in a perifu- sion system. During

Paris-Sud XI, Université de

387

Comparative In Vitro Activities of Retapamulin (SB-275833) against 141 Clinical Isolates of Propionibacterium spp., Including 117 P. acnes Isolates  

PubMed Central

Using the NCCLS agar dilution method, we studied the in vitro activity of retapamulin (SB-275833) against 141 clinical isolates of Propionibacterium species, including seven multiresistant strains, and found retapamulin to be the most active agent among those tested with MICs of ?1 ?g/ml against all isolates. PMID:16377717

Goldstein, Ellie J. C.; Citron, Diane M.; Merriam, C. Vreni; Warren, Yumi A.; Tyrrell, Kerin L.; Fernandez, Helen T.

2006-01-01

388

Anabolic activity of ursolic acid in bone: Stimulating osteoblast differentiation in vitro and inducing new bone formation in vivo  

Microsoft Academic Search

In the field of osteoporosis, there has been growing interest in anabolic agents that enhance bone mass and improve bone architecture. In this study, we demonstrated that the ubiquitous plant triterpenoid, ursolic acid, enhances differentiation and mineralization of osteoblasts in vitro. We found that ursolic acid induced the expression of osteoblast-specific genes with the activation of mitogen-activated protein kinases, nuclear

Su-Ui Lee; Sang-Joon Park; Han Bok Kwak; Jaemin Oh; Yong Ki Min; Seong Hwan Kim

2008-01-01

389

Synthesized oversulphated, acetylated and benzoylated derivatives of fucoidan extracted from Laminaria japonica and their potential antioxidant activity in vitro  

Microsoft Academic Search

Three sulphated polysaccharide derivatives (oversulphated, acetylated and benzoylated fucoidan) were successfully synthesized, and their antioxidant activities were investigated employing various established in vitro systems. A novel catalyst N-bromosuccinimide (NBS) was used in acetylation and benzoylation reaction, and the degree of acetylation was evaluated using IR and NMR spectra. Both fucoidan derivatives possessed considerable antioxidant activity, and had stronger antioxidant ability

Jing Wang; Li Liu; Quanbin Zhang; Zhongshan Zhang; Huimin Qi; Pengcheng Li

2009-01-01

390

In vitro cytoprotective activity of squalene on a bone marrow versus neuroblastoma model of cisplatin-induced toxicity  

Microsoft Academic Search

The development of a non-toxic selective cytoprotective agent that preferentially protects normal tissues from chemotherapy toxicity, without protecting malignant tissues, is a major challenge in cancer chemotherapy research. The available cytoprotective agents are either toxic or lack selective cytoprotective activity. Here, we report the in vitro selective cytoprotective activity of squalene, an isoprenoid molecule with antioxidant properties. Normal human bone

B Das; H Yeger; H Baruchel; M. H Freedman; G Koren; S Baruchel

2003-01-01

391

Visualization of bisphosphonate-induced caspase-3 activity in apoptotic osteoclasts in vitro.  

PubMed

Bisphosphonates inhibit osteoclast-mediated bone resorption by mechanisms that have only recently become clear. Whereas nitrogen-containing bisphosphonates affect osteoclast function by preventing protein prenylation (especially geranylgeranylation), non-nitrogen-containing bisphosphonates have a different molecular mechanism of action. In this study, we demonstrate that nitrogen-containing bisphosphonates (risedronate, alendronate, pamidronate, and zoledronic acid) and non-nitrogen-containing bisphosphonates (clodronate and etidronate) cause apoptosis of rabbit osteoclasts, human osteoclastoma-derived osteoclasts, and human osteoclast-like cells generated in cultures of bone marrow in vitro. Osteoclast apoptosis was shown to involve characteristic morphological changes, loss of mitochondrial membrane potential, and the activation of caspase-3-like proteases capable of cleaving peptide substrates with the sequence DEVD. Caspase-3-like activity could be visualized in unfixed, dying osteoclasts and osteoclast-like cells using a cell-permeable, fluorogenic substrate. Bisphosphonate-induced osteoclast apoptosis was dependent on caspase activation, because apoptosis resulting from alendronate, clodronate, or zoledronic acid treatment was suppressed by zVAD-fmk, a broad-range caspase inhibitor, or by SB-281277, a specific isatin sulfonamide inhibitor of caspase-3/-7. Furthermore, caspase-3 (but not caspase-6 or caspase-7) activity could be detected and quantitated in lysates from purified rabbit osteoclasts, whereas the p17 fragment of active caspase-3 could be detected in human osteoclast-like cells by immunofluorescence staining. Caspase-3, therefore, appears to be the major effector caspase activated in osteoclasts by bisphosphonate treatment. Caspase activation and apoptosis induced by nitrogen-containing bisphosphonates are likely to be the consequence of the loss of geranylgeranylated rather than farnesylated proteins, because the ability to cause apoptosis and caspase activation was mimicked by GGTI-298, a specific inhibitor of protein geranylgeranylation, whereas FTI-277, a specific inhibitor of protein farnesylation, had no effect on apoptosis or caspase activity. PMID:11344045

Benford, H L; McGowan, N W; Helfrich, M H; Nuttall, M E; Rogers, M J

2001-05-01

392

Tumoricidal activity of human monocytes activated in vitro by free and liposome-encapsulated human lymphokines.  

PubMed Central

Human peripheral blood mononuclear cells from normal donors obtained by separation on a Percoll gradient were incubated with free or liposome-entrapped lymphokines produced from concanavalin A-stimulated lymphocytes and then were tested for cytotoxic activity against tumor cells. The treated monocytes lysed tumorigenic melanoma and glioblastoma target cells, but had no effect on three types of nontumorigenic target cells. The activation of monocytes to become tumoricidal was caused by macrophage-activating factor (MAF) and not by contamination with endotoxins, concanavalin A, or interferon. The endocytosis of liposomes containing MAF, but not of those containing control supernatants, led to the activation of cytotoxic properties in the monocytes. Activation by liposome-encapsulated MAF was very efficient and required less than 1/800th of the amount of free MAF necessary to achieve the same levels of cytotoxicity. Thus, the encapsulation of mitogen-induced MAF in liposomes could provide an effective approach for the activation of blood monocytes in situ. Images FIGURE 2 PMID:6348087

Kleinerman, E S; Schroit, A J; Fogler, W E; Fidler, I J

1983-01-01

393

Design, in vitro stability, and ocular hypotensive activity of t-butalone chemical delivery systems.  

PubMed

The objective of this work was to synthesize two bioreversible diacyl derivatives of t-butalone (chemical delivery systems), determine their chemical and in vitro stability, and investigate their potential use as topical antiglaucoma agents. The stability of these compounds was determined in isotonic phosphate buffers (pH range 5-8) and in selected biological media, including human whole blood, rabbit and rat blood, and the anterior segment tissues of rabbit. The ocular hypotensive activity of these compounds in unrestrained, normotensive albino rabbits was determined with a pneumatonometer. The two compounds were stable at lower pH. The stability decreased as the pH increased, suggesting their lability to base-catalyzed hydrolysis. These compounds exhibited significant differences in the hydrolytic rates in the whole blood among species examined (rat > rabbit > human). The observed rates of disappearance in different ocular tissues were indicative of relative enzyme activity in these media (iris-ciliary body > cornea > aqueous humor). The two compounds exhibited a significant ocular hypotensive activity (P < 0.01) at 2% dose level. The peak activity was found between 2 and 4 h, and the activity was maintained for 4.5 to 7 h. The dipivalyl derivative of t-butalone exhibited more pronounced decrease in intraocular pressure than that of diisovaleryl derivative. The present study suggests the possible use of diacyl derivatives of t-butalone as ocular hypotensive agents. PMID:11536206

Reddy, I K; Vaithiyalingam, S R; Khan, M A; Bodor, N S

2001-08-01

394

In vitro assessment of thyroidal and estrogenic activities in poultry and broiler manure.  

PubMed

Among the many chemicals found in avian manure, endocrine disruptors (EDs), of natural or anthropogenic origin, are of special environmental concern. Nowadays, an increasing amount of estrogens is being released into the environment via the use of manure to fertilize agricultural land. While most research in this field has focused on estrogenic phenomena, little is known about alterations related to other endocrine systems, such as the thyroidal one. Here we simultaneously assessed the potential estrogenic and thyroidal activity of poultry and broiler litter manure using in vitro approaches based on estrogen receptor (Er) and thyroid receptor (Tr) transactivation assays. In addition, leaching experiments were performed to assess whether the EDs present in the manure pass through a soil column and potentially reach the groundwater. Manure from four broiler and four poultry farms was collected in two sampling campaigns carried out in two seasons (fall and spring). Extracts from broiler and poultry manure exhibited strong thyroidal activity. Only poultry manure showed estrogenic activity, which is consistent with the low levels of estrogens expected in hatchlings. Leakage experiments were performed in columns with two kinds of arable soils: sandy and loamy. No estrogenicity or thyroidal activity was detectable in soils treated with the manure or in the corresponding leachates. These results indicate that substances with estrogenic or thyroidal activity were degraded in the soil under our experimental conditions. However, the long-term effects associated with the constant and intensive application of manure to agricultural land in some regions require further research. PMID:24317169

Valdehita, A; Quesada-García, A; Delgado, M M; Martín, J V; García-González, M C; Fernández-Cruz, M L; Navas, J M

2014-02-15

395

An alternative method to access in vitro the hemorrhagic activity of snake venoms.  

PubMed

Local and systemic hemorrhages are major problems concerning bites by viper snakes. Therefore, accessing venom hemorrhagic activity is an important feature in order to characterize viper venom major toxicities or to assay antivenom efficacy. The methods currently used to access hemorrhagic activity involve animal experiments and according to the general ethical committees, these procedures should be substituted to in vitro assays in order to minimize animal use in research. In this work, we have developed an immunoassay to detect the content of hemorrhagic metalloproteinases in snake venoms using a neutralizing monoclonal antibody anti-jararhagin (MAJar 3). The correlation between the reactivity of this monoclonal antibody and venom-induced hemorrhage was further revealed by a study comparing the hemorrhagic activity of venom samples collected individually from 88 specimens of Bothrops jararacussu with their reactivity with MAJar 3. As a result, a significant correlation (r=0.942) was achieved between samples hemorrhagic activity and their reactivity with MAJar 3, suggesting that this assay can be used as a substitute of the conventional tests performed in vivo to estimate the hemorrhagic activity. PMID:18262214

Rafael, A; Tanjoni, I; Fernandes, I; Moura-da-Silva, A M; Furtado, M F D

2008-03-15

396

In vitro radical scavenging and cytotoxic activities of novel hybrid selenocarbamates.  

PubMed

Novel selenocyanate and diselenide derivatives containing a carbamate moiety were synthesised and evaluated in vitro to determine their cytotoxic and radical scavenging properties. Cytotoxic activity was tested against a panel of human cell lines including CCRF-CEM (lymphoblastic leukaemia), HT-29 (colon carcinoma), HTB-54 (lung carcinoma), PC-3 (prostate carcinoma), MCF-7 (breast adenocarcinoma), 184B5 (non-malignant, mammary gland derived) and BEAS-2B (non-malignant, derived from bronchial epithelium). Most of the compounds displayed high antiproliferative activity with GI50 values below 10?M in MCF-7, CCRF-CEM and PC-3 cells. Radical scavenging properties of the new selenocompounds were confirmed testing their ability to scavenge DPPH and ABTS radicals. Based on the activity of selenium-based glutathione peroxidases (GPxs), compounds 1a, 2e and 2h were further screened for their capacity to reduce hydrogen peroxide under thiol presence. Results suggest that compound 1a mimics GPxs activity. Cytotoxic parameters, radical scavenging activity and ADME profile point to 1a as promising drug candidate. PMID:25792142

Romano, Beatriz; Plano, Daniel; Encío, Ignacio; Palop, Juan Antonio; Sanmartín, Carmen

2015-04-15

397

Colloidal aggregation and the in vitro activity of traditional chinese medicines.  

PubMed

Traditional Chinese Medicines (TCMs) have been the sole source of therapeutics in China for two millennia. In recent drug discovery efforts, purified components of TCM formulations have shown activity in many in vitro assays, raising concerns of promiscuity. Here, we investigated 14 bioactive small molecules isolated from TCMs for colloidal aggregation. At concentrations commonly used in cell-based or biochemical assay conditions, eight of these compounds formed particles detectable by dynamic light scattering and showed detergent-reversible inhibition against ?-lactamase and malate dehydrogenase, two counter-screening enzymes. When three of these compounds were tested against their literature-reported molecular targets, they showed similar reversal of their inhibitory activity in the presence of detergent. For three of the most potent aggregators, contributions to promiscuity via oxidative cycling were investigated; addition of 1 mM DTT had no effect on their activity, which is inconsistent with an oxidative mechanism. TCMs are often active at micromolar concentrations; this study suggests that care must be taken to control for artifactual activity when seeking their primary targets. Implications for the formulation of these molecules are considered. PMID:25606714

Duan, Da; Doak, Allison K; Nedyalkova, Lyudmila; Shoichet, Brian K

2015-04-17

398

The in-vitro antimicrobial activities of some medicinal plants from Cameroon.  

PubMed

The antimicrobial activities of 10 plant species (Voacanga africana, Crepis cameroonica, Plagiostyles africana, Crotalaria retusa, Mammea africana, Lophira lanceolata, Ochna afzelii, Ouratea elongata, Ou. flava and Ou. sulcata), each of which is currently used in the traditional medicine of Cameroon, were investigated in vitro. The activities of a methanol extract of each plant were tested, in disc-diffusion assays, against 37 reference or laboratory strains of seven species of microorganism (Staphylococcus aureus, S. epidermidis, Enterococcus hirae, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and Candida albicans). The minimal inhibitory concentrations of each extract were then estimated, against each of the more susceptible microorganisms (i.e. those giving an inhibition zone measuring at least 9 mm in diameter in the disc-diffusion assays), by agar dilution. Although, in the disc-diffusion assays, each of the 10 methanol extracts investigated displayed some degree of antimicrobial activity against at least one species of microorganism, no activity against the Gram-negative bacteria (Es. coli, K. pneumoniae and Ps. aeruginosa) was observed. The extract with the greatest antimicrobial activity was that of Pl. africana (Euphorbiaceae). PMID:16630381

Gangoué-Piéboji, J; Pegnyemb, D E; Niyitegeka, D; Nsangou, A; Eze, N; Minyem, C; Mbing, J Ngo; Ngassam, P; Tih, R Ghogomu; Sodengam, B L; Bodo, B

2006-04-01

399

In vitro and in vivo antifungal activities of D0870, a new triazole agent.  

PubMed Central

In vitro and in vivo antifungal activities of D0870 were evaluated in comparison with those of fluconazole. D0870, which is the R-enantiomer of ICI195,739, was found to be the mycologically active enantiomer by comparing the activities of D0870 with those of M16355 (S-enantiomer of ICI195,739). D0870 showed a broad spectrum of antifungal activity and MICs and minimum antibiotic concentrations 4- to 2,000-fold lower in synthetic amino acid medium (fungal) agar than those of fluconazole for various fungi. Although MICs of D0870 were affected by variation of the test conditions, such as type of medium, inoculum size of fungi, supplementation with fetal bovine serum, and pH of medium, they were consistently much lower than those of fluconazole under any condition. In vivo activities of D0870 in the systemic infection models with Candida albicans, Cryptococcus neoformans, and Aspergillus fumigatus in normal mice and in the mice immunosuppressed with cyclophosphamide or cortisone acetate were 2- to 7-fold and 3- to 89-fold greater than those of fluconazole, respectively. In these infection models in immunosuppressed mice, the therapeutic efficacy of D0870 was almost equivalent to that in normal mice, whereas the efficacy of fluconazole was 2- to 50-fold lower than that in normal mice. PMID:8285626

Yamada, H; Tsuda, T; Watanabe, T; Ohashi, M; Murakami, K; Mochizuki, H

1993-01-01

400

In vitro study on ?-amylase inhibitory activity of an Indian medicinal plant, Phyllanthus amarus  

PubMed Central

Objective: The objective of this study was to evaluate the ?-amylase inhibitory activity of different extracts of Phyllanthus amarus against porcine pancreatic amylase in vitro. Materials and Methods: The plant extracts were prepared sequentially with ethanol, chloroform, and hexane. Each extract was evaporated using rotary evaporator, under reduced pressure. Different concentrations (10, 20, 40, 60, 80, and 100 ?g/mL) of each extract were made by using dimethyl sulfoxide (DMSO) and subjected to ?-amylase inhibitory assay using starch azure as a substrate. The absorbance was read at 595 nm using spectrophotometer. Using this method, the percentage of ?-amylase inhibitory activity and IC50values of each extract was calculated. Results: The chloroform extract failed to inhibit ?-amylase activity. However, the ethanol and hexane extracts of P. amarus exhibited appreciable ?-amylase inhibitory activity with an IC50 values 36.05 ± 4.01 ?g/mL and 48.92 ± 3.43 ?g/mL, respectively, when compared with acarbose (IC50value 83.33 ± 0.34 ?g/mL). Conclusion: This study supports the ayurvedic concept that ethanol and hexane extracts of P. amarus exhibit considerable ?-amylase inhibitory activities. Further, this study supports its usage in ethnomedicines for management of diabetes. PMID:21206618

Tamil, Iniyan G.; Dineshkumar, B.; Nandhakumar, M.; Senthilkumar, M.; Mitra, A.

2010-01-01

401

A soluble form of the human transferrin receptor is released by activated lymphocytes in vitro.  

PubMed Central

Soluble transferrin receptors (sTfR) were detected in culture supernatants of activated human peripheral blood mononuclear cells (PBMC) using a sandwich ELISA technique with two non-cross-reacting TfR MoAbs. Mitogenic stimulation of lymphoid cells induced both up-regulation of TfR surface density and release of sTfR to the medium. Peak levels of sTfR in culture supernatants occurred at day 4 after activation, 1 day later than maximum expression of TfR in the plasma membrane. Production of sTfR was independent of proliferation, as demonstrated by measuring sTfR release by PBMC, which had been irradiated with a dose of 20 Gy before activation. In addition to these in vitro experiments, we tested the sera of 85 patients with systemic lupus erythematosus (SLE), an autoimmune disease accompanied by in vivo activation of lymphocytes, for their sTfR levels. No correlation of these data was detectable to serum concentrations of the soluble alpha-chain of the IL-2 receptor, an unequivocal marker of lymphocyte activation. However, they correlated negatively to the haemoglobin content of the patients' erythrocytes, indicating that erythroid progenitors are the predominant source of sTfR in SLE patients' sera. PMID:8513587

Woith, W; Nüsslein, I; Antoni, C; Dejica, D I; Winkler, T H; Herrmann, M; Pirner, K; Kalden, J R; Manger, B

1993-01-01

402

Anti-Salmonella activity of Terminalia belerica: in vitro and in vivo studies.  

PubMed

To search for an herbal remedy for protection against and treatment for typhoid fever, a number of plants were screened. Anti-Salmonella activity of Terminalia belerica, an ingredient of Ayurvedic preparation 'triphala' used for treatment of digestive and liver disorders, has been reported. Fruits of T. belerica were extracted with petroleum ether, chloroform, acetone, alcohol and water and efficacy of extracts against Salmonella typhi and Salmonella typhimurium was evaluated. Alcoholic and water extracts of T. belerica showed significant anti-Salmonella activity and MIC was 12.5 mg/ml against S. typhimurium. Aqueous extracts of Picrohiza kurroa and Vitits vinefera also showed low anti-Salmonella activity where as aqueous extracts of Asparagus racemosus and Zingiber officinale showed no anti-Salmonella activity. Extracts of T. belerica, Picrohiza kurroa and Vitits vinefera with other solvents such as chloroform and petroleum ether showed insignificant activity. Results showed that aqueous extract of T. belerica was bactericidal at high concentrations where as low concentrations showed bacteriostatic property. In vitro cellular toxicity studies showed no cyto-toxicity associated with T. belerica extracts. Pretreatment of mice with aqueous extract of T. belerica conferred protection against experimental Salmonellosis and 100% survival of animals has been reported when challenged with lethal doses of S. typhimurium. PMID:19245178

Madani, A; Jain, S K

2008-12-01

403

In Vitro Activation of [FeFe] Hydrogenase: New Insights into Hydrogenase Maturation  

SciTech Connect

The in vitro activation of the [FeFe] hydrogenase is accomplished by combining Escherichia coli cell extracts containing the heterologously expressed inactive HydA with extracts in which hydrogenase-specific maturation proteins HydE, HydF, and HydG are expressed in concert. Interestingly, the process of HydA activation occurs rapidly and in the absence of potential substrates, which suggests that the hydrogenase accessory proteins synthesize an H-cluster precursor that can be quickly transferred to the hydrogenase enzyme to affect activation. HydA activity is observed to be dependent on the protein fraction containing all three accessory proteins expressed in concert and cannot be accomplished with addition of heat-treated extract or extract filtrate, suggesting that the activation of the hydrogenase structural protein is mediated by interaction with the accessory assembly protein(s). These results represent the first important step in understanding the process of H-cluster assembly and provide significant insights into hydrogenase maturation.

McGlynn, S. E.; Ruebush, S. S.; Naumov, A.; Nagy, L. E.; Dubini, A.; King, P. W.; Broderick, J. B.; Posewitz, M. C.; Peters, J. W.

2007-01-01

404

Effect of ibudilast on ciliary activity of human paranasal sinus mucosa in vitro.  

PubMed

The effect of ibudilast (CAS 50847-11-5, 3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine, KC-404), an anti-asthmatic drug, on ciliary beat frequency (CBF) of human paranasal sinus mucosa was examined in vitro. Ciliary activation was observed after a 10-min exposure to 4.6 x 10(-6) mol/l ibudilast. Ibudilast dose-dependently increase CBF at the concentrations ranging from 4.6 x 10(-7) mol/l to 4.6 x 10(-5) mol/l. Propranolol inhibited ciliary activity induced by ibudilast; however, neither indometacin nor verapamil affected the activation of ibudilast on CBF. Platelet activating factor (PAF) and Leukotriene D4 (LTD4) are chemical mediators inducing mucosal dysfunction and damage. Ibudilast prevented ciliary inhibition induced by PAF and LTD4. These findings indicated that ibudilast activates CBF and inhibits the effect of PAF and LTD4 on ciliated cells, and consequently improves the pathogenesis of allergic disorders such as the inhibited mucociliary transport system and airway hyperresponsiveness. PMID:7575753

Ganbo, T; Hisamatsu, K; Mizukoshi, A; Inoue, H; Kikushima, K; Kou, J; Kozuka, Y; Murakami, Y

1995-08-01

405

Bromelain treatment reduces CD25 expression on activated CD4+ T cells in vitro.  

PubMed

Bromelain (Br), an extract from pineapple stem with cysteine protease activity, exerts anti-inflammatory effects in a number of inflammatory models. We have previously shown that Br treatment decreased activated CD4(+) T cells and has a therapeutic role in an ovalbumin-induced murine model of allergic airway disease. The current study was designed to determine the effect of Br on CD4(+) T cell activation, specifically the expression of CD25 in vitro. CD25 is up regulated upon T cell activation, found as a soluble fraction (sCD25) and is a therapeutic target in inflammation, autoimmunity and allergy. Br treatment of anti-CD3 stimulated CD4(+) T cells reduced CD25 expression in a dose and time dependent manner. This reduction of CD25 was dependent on the proteolytic action of Br as the addition of E64 (a cysteine protease inhibitor) abrogated this response. The concentration of sCD25 was increased in supernatants of Br treated activated CD4(+) T cells as compared to control cells, suggesting that Br proteolytically cleaved cell-surface CD25. This novel mechanism of action identifies how Br may exert its therapeutic benefits in inflammatory conditions. PMID:19162239

Secor, Eric R; Singh, Anurag; Guernsey, Linda A; McNamara, Jeff T; Zhan, Lijun; Maulik, Nilanjana; Thrall, Roger S

2009-03-01

406

Bromelain treatment reduces CD25 expression on activated CD4+ T cells in vitro?  

PubMed Central

Bromelain (Br), an extract from pineapple stem with cysteine protease activity, exerts anti-inflammatory effects in a number of inflammatory models. We have previously shown that Br treatment decreased activated CD4+ T cells and has a therapeutic role in an ovalbumin-induced murine model of allergic airway disease. The current study was designed to determine the effect of Br on CD4+ T cell activation, specifically the expression of CD25 in vitro. CD25 is up regulated upon T cell activation, found as a soluble fraction (sCD25) and is a therapeutic target in inflammation, autoimmunity and allergy. Br treatment of anti-CD3 stimulated CD4+ T cells reduced CD25 expression in a dose and time dependent manner. This reduction of CD25 was dependent on the proteolytic action of Br as the addition of E64 (a cysteine protease inhibitor) abrogated this response. The concentration of sCD25 was increased in supernatants of Br treated activated CD4+ T cells as compared to control cells, suggesting that Br proteolytically cleaved cell-surface CD25. This novel mechanism of action identifies how Br may exert its therapeutic benefits in inflammatory conditions. PMID:19162239

Secor, Eric R.; Singh, Anurag; Guernsey, Linda A.; McNamara, Jeff T.; Zhan, Lijun; Maulik, Nilanjana; Thrall, Roger S.

2009-01-01

407

Comparison of inhibitory activities of donepezil and other cholinesterase inhibitors on acetylcholinesterase and butyrylcholinesterase in vitro.  

PubMed

This study was designed to compare the in vitro inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) of donepezil and some other cholinesterase (ChE) inhibitors which have been developed for the treatment of Alzheimer's disease. The carbamate derivatives physostigmine and rivastigmine needed preincubation to exhibit appropriate anti-ChE activity. The maximum ChE inhibition by physostigmine developed within 30-60 min, while the inhibitory effect of rivastigmine on AChE and BuChE activities reached its peak after 48 and 6 h, respectively. The order of inhibitory potency (IC50) towards AChE activity under optimal assay conditions for each ChE inhibitor was: physostigmine (0.67 nM) > rivastigmine (4.3 nM) > donepezil (6.7 nM) > TAK-147 (12 nM) > tacrine (77 nM) > ipidacrine (270 nM). The benzylpiperidine derivatives donepezil and TAK-147 showed high selectivity for AChE over BuChE. The carbamate derivatives showed moderate selectivity, while the 4-aminopyridine derivatives tacrine and ipidacrine showed no selectivity. The inhibitory potency of these ChE inhibitors towards AChE activity may illustrate their potential in vivo activity. PMID:11256231

Ogura, H; Kosasa, T; Kuriya, Y; Yamanishi, Y

2000-10-01

408

In Vitro and In Vivo Activities of Three Oxazolidinones against Nonreplicating Mycobacterium tuberculosis  

PubMed Central

Oxazolidinones represent a new class of antituberculosis drugs that exert their function by inhibiting protein synthesis. Here, we compared the activities of three oxazolidinones, linezolid, PNU-100480, and AZD5847, against latent tuberculosis using a simple model employing the streptomycin-starved Mycobacterium tuberculosis strain 18b. The in vitro drug susceptibility results showed that the three oxazolidinones had a bacteriostatic effect against actively growing bacilli but potent bactericidal activity against nonreplicating cells. In the murine model of latent infection with M. tuberculosis 18b, the efficacy of the three compounds varied greatly. Indeed, AZD5847 or its prodrug exhibited no activity or only modest activity, respectively, after 2 months of treatment, whereas both linezolid and PNU-100480 were effective against latent bacilli in mice and showed promising outcomes in combination therapy with rifampin. Moreover, the potency of PNU-100480 was significantly greater than that of linezolid, making it an attractive drug candidate in the development of new combination therapies for latent tuberculosis. PMID:24663022

Zhang, Ming; Sala, Claudia; Dhar, Neeraj; Vocat, Anthony; Sambandamurthy, Vasan K; Sharma, Sreevalli; Marriner, Gwendolyn; Balasubramanian, V.

2014-01-01

409

In vitro antiplasmodial activity of benzophenones and xanthones from edible fruits of Garcinia species.  

PubMed

Species of Garcinia have been used to combat malaria in traditional African and Asian medicines, including Ayurveda. In the current study, we have identified antiplasmodial benzophenone and xanthone compounds from edible Garcinia species by testing for in vitro inhibitory activity against Plasmodium falciparum. Whole fruits of Garcinia xanthochymus, G. mangostana, G. spicata, and G. livingstonei were extracted and tested for antiplasmodial activity. Garcinia xanthochymus was subjected to bioactivity-guided fractionation to identify active partitions. Purified benzophenones (1-9) and xanthones (10-18) were then screened in the plasmodial lactate dehydrogenase assay and tested for cytotoxicity against mammalian (Vero) cells. The benzophenones guttiferone E (4), isoxanthochymol (5), and guttiferone H (6), isolated from G. xanthochymus, and the xanthones ?-mangostin (15), ?-mangostin (16), and 3-isomangostin (17), known from G. mangostana, showed antiplasmodial activity with IC50 values in the range of 4.71-11.40 µM. Artemisinin and chloroquine were used as positive controls and exhibited IC50 values in the range of 0.01-0.24 µM. The identification of antiplasmodial benzophenone and xanthone compounds from G. xanthochymus and G. mangostana provides evidence for the antiplasmodial activity of Garcinia species and warrants further investigation of these fruits as dietary sources of chemopreventive compounds. PMID:24963617

Lyles, James T; Negrin, Adam; Khan, Shabana I; He, Kan; Kennelly, Edward J

2014-06-01

410

Phosphorylated H2AX in parthenogenetically activated, in vitro fertilized and cloned bovine embryos.  

PubMed

Summary In vitro embryo production methods induce DNA damage in the embryos. In response to these injuries, histone H2AX is phosphorylated (?H2AX) and forms foci at the sites of DNA breaks to recruit repair proteins. In this work, we quantified the DNA damage in bovine embryos undergoing parthenogenetic activation (PA), in vitro fertilization (IVF) or somatic cell nuclear transfer (SCNT) by measuring ?H2AX accumulation at different developmental stages: 1-cell, 2-cell and blastocyst. At the 1-cell stage, IVF embryos exhibited a greater number of ?H2AX foci (606.1 ± 103.2) and greater area of ?H2AX staining (12923.6 ± 3214.1) than did PA and SCNT embryos. No differences at the 2-cell stage were observed among embryo types. Although PA, IVF and SCNT were associated with different blastocyst formation rates (31.1%, 19.7% and 8.3%, P < 0.05), no differences in the number of ?H2AX foci or area were detected among the treatments. ?H2AX is detected in bovine preimplantation embryos produced by PA, IVF and SCNT; the amount of DNA damage was comparable among those embryos developing to the blastocyst stage among different methods for in vitro embryo production. While IVF resulted in increased damage at the 1-cell embryo stage, no difference was observed between PA and SCNT embryos at any developmental stage. The decrease in the number of double-stranded breaks at the blastocyst stage seems to indicate that DNA repair mechanisms are functional during embryo development. PMID:24735637

Pereira, A F; Melo, L M; Freitas, V J F; Salamone, D F

2014-04-15

411

Inhibition of rabbit platelet activation in vitro by antagonists of platelet-activating factor (PAF)  

SciTech Connect

The authors used washed, (/sup 3/H)serotonin-labeled rabbit platelets to study the in vitro aggregation and secretion responses induced by graded doses of PAF in the presence or absence of specific antagonists of PAF. These antagonists included CV-3988, L-652,731, triazolam and alprazolam. Platelets were pretreated with either an antagonist or the appropriate diluent for 60 sec prior to the addition of PAF (2 x 10/sup -10/ to 2 x 10/sup -7/ M). Aggregation was monitored continuously and recorded as the height of the aggregation tracing at 60 sec post-PAF. Secretion of (/sup 3/H)-serotonin was measured in a sample of the platelets removed at 60 sec post-PAF. When 2 x 10/sup -10/ M PAF was used as the stimulus, the concentration of antagonist needed for 50% inhibition (IC/sub 50/) of secretion was obtained at 0.05 ..mu..M, 0.15 ..mu..M, 0.6 ..mu..M and 2.5 ..mu..M, respectively, for L-652,731, CV-3988, triazolam and alprazolam. The corresponding IC/sub 50/ for aggregation was obtained at 0.2 ..mu..M, 0.1 ..mu..M, 1.5 ..mu..M and 6.5 ..mu..M, respectively. The inhibitory effects of these antagonists could be overcome by increasing the dose of PAF used. Although all of the antagonists were capable of completely inhibiting platelet aggregation and secretion, L-652,731 was the most potent PAF antagonist on a molar basis.

Cox, C.P.; Wood, K.L.

1986-03-05

412

Microbial metabolites of omeprazole activate murine aryl hydrocarbon receptor in vitro and in vivo.  

PubMed

Omeprazole (OME), a proton pump inhibitor used to treat gastritis, is also an aryl hydrocarbon receptor (AhR) activator. OME activates AhR in human hepatocytes and hepatoma cells, but not in mice in vivo or in vitro. We recently discovered that this species-specific difference results from a difference in a few amino acids in the ligand-binding domain of AhR. However, OME activates both mouse and human AhRs in the yeast reporter assay system. Nevertheless, the cause of this discrepancy in OME responses remains unknown. Here, we report that CYP1A1 mRNA expression in mouse cecum was elevated after OME administration, although the mouse is regarded as an OME-unresponsive animal. Using the yeast reporter assay system with human and murine AhRs, we found AhR agonist-like activity in the cecal extracts of OME-treated mice. We speculated that OME metabolites produced by cecal bacteria might activate murine AhRs in vivo. In high-performance liquid chromatography (HPLC) analysis, AhR agonist-like activity of cecal bacterial culture and cecal extracts were detected at the same retention time. AhR agonist-like activity was also detected in the HPLC fractions of yeast culture media containing OME. This unknown substance could induce reporter gene expression via mouse and human AhRs. The agonist-like activity of the OME metabolite was reduced by concomitant ?-naphthoflavone exposure. These results indicate that a yeast-generated OME metabolite elicited the response of mouse AhR to OME in the yeast system, and that bacterial OME metabolites may act as AhR ligands in human and mouse intestines. PMID:25061160

Shiizaki, Kazuhiro; Kawanishi, Masanobu; Yagi, Takashi

2014-10-01

413

VP22 mediates intercellular trafficking and enhances the in vitro antitumor activity of PTEN.  

PubMed

PTEN acts as a phosphatidylinositol phosphatase with a possible role in the phosphatidylinositol 3?kinase (PI3K)/AKT pathway. Mutations in PTEN are frequent and their presence is associated with poor prognosis in breast cancer, which is the most common type of non?cutaneous malignancy in females. Delivery of the tumor suppressor PTEN gene represents a powerful strategy for breast cancer therapy, but a present limitation of gene therapy is the ability to deliver sufficient quantities of active proteins to target cells. The capacity of HSV?1VP22 fusion proteins to spread from the primary transduced cell to surrounding cells could improve gene therapeutics, particularly in cancer. To assess the potential efficacy of VP22 as a gene therapy for breast cancer, expression vectors for N? and C?terminal PTEN?VP22 fusion proteins were constructed. VP22?mediated intercellular transport and antitumor efficacy in BT549 (PTEN?null) breast tumor cells were investigated. The results showed that PTEN?VP22 has the same spreading abilities as VP22. In cell proliferation and apopt