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1

In vitro schistosomicidal activity of balsaminol F and karavilagenin C.  

PubMed

Five cucurbitane-type triterpenes (1-5), previously isolated from the African medicinal plant Momordica balsamina, along with five ester derivatives (6-10) of karavilagenin C (2), were evaluated for their potential schistosomicidal activity against Schistosoma mansoni adult worms. The natural compounds were isolated from the ethyl acetate-soluble fraction of the methanol extract of the aerial parts of M. balsamina. In a preliminary study, a significant schistosomicidal activity was observed for both the crude methanol extract and the ethyl acetate fraction. The compounds responsible for the activity were found to be balsaminol F (1) and karavilagenin C (2) with LC50 values of 14.7?±?1.5 and 28.9?±?1.8?µM, respectively, after 24?h of incubation (positive control praziquantel, LC???=?1.2?±?0.1?µM). Both compounds (1, 2), at 10-50?µM, induced significant reductions in the motor activity of the worms and significantly decreased the egg production. Furthermore, they were able (at 10-100?µM) to separate the adult worm pairs into male and female after 24?h. Compounds 3-5, bearing a sugar moiety as a substituent, and the acylated derivatives of karavilagenin C (6-10) were inactive, suggesting that the presence of free hydroxyl groups in the tetracyclic skeleton might be important for the activity. A correlation between activity and the molecular volume/weight of compounds was also found. PMID:23096257

Ramalhete, Cátia; Magalhăes, Lizandra G; Rodrigues, Vanderlei; Mulhovo, Silva; Da Silva Filho, Ademar A; Ferreira, Maria-José U

2012-12-01

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

E Silva, Márcio Luis Andrade; 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; Uchoa, Camila Jacintho de Mendonca; Cintra, Lucas Silva; de Souza, Herbert Cristian; Peixoto, Juliana Andrade; Silva, Claudia Peres; Magalhaes, Lizandra Guidi; Gimenez, Valeria Maria Meleiro; Groppo, Milton; Rodrigues, Vanderlei; da Silva Filho, Ademar Alves; Andrade e Silva, Marcio Luis; Cunha, Wilson Roberto; Pauletti, Patricia Mendonca; Januario, Ana Helena

2012-01-01

4

Nanopharmaceutical approach of epiisopiloturine alkaloid carried in liposome system: preparation and in vitro schistosomicidal activity.  

PubMed

Schistosomiasis is a neglected tropical disease caused by blood flukes of the genus Schistosoma. This disease control has been widely made by praziquantel-reference drug, but resistance to this drug has already been found. There has been the finding of an imidazole alkaloid in jaborandi leaves-epiisopiloturine, which has known activity against adult, young and egg forms of Schistosoma mansoni. This alkaloid is an apolar molecule with difficult solubility; therefore, the liposomal structure of epiisopiloturine was proposed. Liposomes are carrying structures of drugs that may enhance solubility of compounds such as epiisopiloturine. In this work, we report in vitro epiisopiloturine-loaded liposomes effect formed by different concentrations of lipids 9:1 (weight ratio) dipalmitoylphosphatidylcholine:cholesterol and 8:2 (weight ratio) dipalmitoylphosphatidylcholine:cholesterol. Results have showed that epiisopiloturine extraction and isolation have been successful through high-performance liquid chromatography-HPLC and its purity confirmed through mass spectrometry has showed 287 Da molecular mass. Formulations from 9:1 DPPC:cholesterol and 8:2 DPPC:cholesterol with loaded EPI (300 microg/ml) have killed parasites at 100% after incubation 96 h and 120 h, respectively. Confocal microscopy employed to observe morphological alterations in the tegument of adult form of Schistosoma mansoni. Details from interaction, between epiisopiloturine and liposome, have been achieved by semi-empirical AM1 calculations, which have showed that epiisopiloturine inside is more stable than the outside form, at least 10 kcal. This is first time that schistosomicidal activity has been reported for epiisopiloturine-loaded into liposome. PMID:24738423

Guimarăes, Maria A; Campelo, Yuri D M; Véras, Leiz M C; Colhone, Marcelle C; Lima, David Fernandes; Ciancaglini, Pietro; Kuckelhaus, Selma S; Lima, Francisco C A; de Moraes, Josué; de Leite, José Roberto S A

2014-06-01

5

In vitro schistosomicidal effects of some phloroglucinol derivatives from Dryopteris species against Schistosoma mansoni adult worms.  

PubMed

The rhizomes of Dryopteris species have popularly been used as vermifuge in flatworm infections. The aim of this work was to evaluate the in vitro schistosomicidal activity of some phloroglucinol compounds, obtained from the rhizomes of Dryopteris species, against Schistosoma mansoni adult worms. All worm pairs were dead after 24 h of incubation with aspidin 25 to 100 microM (1), flavaspidic acid 50 and 100 microM (2), methylene-bis-aspidinol 100 microM (3), and desaspidin 25 to 100 microM (4). Worms incubated with 1 (25 to 100 microM) and 2 (50 to 100 microM) showed decrease motor activity with tegumental alterations, while 3 (100 microM) and 4 (10 to 100 microM) showed decrease motor activity without tegumental alterations. Desaspidinol (5) and filicinic acid (6), at the tested concentrations (10 to 100 microM), did not show activity against adult worms of S. mansoni. Praziquantel (10 microM), used as positive control, caused death of the parasites and tegumental alterations without separation of worms. In the groups treated with 100 microM of compounds 1-4, the viability of the adult worms was similar to the positive control group, in which the worms were dead. Also, both the egg productions and the development of eggs produced by the adult worms were inhibited by the incubation with compounds 1-4 (10 and 100 microM) in comparison with the negative control (RPMI 1640 medium). It is suggested that the in vitro schistosomicidal effects of phloroglucinols derivatives 1, 2, 3, and 4 may be related to the inhibition of oxidative phosphorylation pathway in S. mansoni. The present results confirmed the traditional indications of rhizomes from Dryopteris species, which possess phloroglucinol compounds, in the treatment of tapeworm infections. PMID:19898869

Magalhăes, Lizandra G; Kapadia, Govind J; da Silva Tonuci, Lígia R; Caixeta, Soraya C; Parreira, Natállia A; Rodrigues, Vanderlei; Da Silva Filho, Ademar A

2010-01-01

6

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

7

Evaluation of schistosomicidal activity of myrrh extract: parasitological and histological study.  

PubMed

Ninety mice were divided into three main groups: G. I (non-infected control), G. II (infected non treated control) and G. III (infected treated), which was further subdivided into 4 subgroups: IIIA, IIIB, IIIC & IIID, where the drug was administered in a dose of 500 mg/kg body weight for five days before infection for subgroup IIIA, on the 1st day post infection (PI) for subgroup IIIB, 21 days PI for subgroup IIIC and 45 days post infection for subgroup IIID. All animals were sacrificed 80 days after the start of the experiment. Anti-schistosomal activity was assessed parasitologically by estimating the percentage reducetion of worm burden, egg count/gm tissues (liver & intestine), and the oogram pattern; histologically & histopathologically by examination of jejunum using different stains. The percentage reduction of worm burden was 30.35%, 64.54%, 76.92% and 98.46% respectively when compared to the infected non-treated control G. The maximum effect of the drug was observed in subgroups IIIC & IIID. Also, there was marked reduction in the egg count in tissues (liver & intestine). In addition the oogram pattern showed that myrrh had high antischistosomal activity. The histologically and histopathologically infected untreated (GII), when compared to non-infected non-treated control G. showed apparent shortening and flattening of the jejunal villi with focal loss of the epithelial covering. Loss of PAS positive brush border of many enterocytes with goblet cells hyperplasia was seen. Bilharzial granulomas were frequently encountered in the submucosa and the musculosa with numerous eosinophils content. In subgroups IIIA & IIIB, there was mild amelioration of the mucosal structural abnormalities. The granulomas were less frequently seen with decrease of their eosinophils. In subgroups IIIC & IIID there was restoration of the jejunal mucosal continuity, marked decrease in the granulomas and paucity of eosinophils. The present data proved that myrrh has a valuable schistosomicidal effect against different maturation stages of S. mansoni. The chemotherapeutic effect was more evident when the drug was given to the infected mice on the 21st as well as on the 45th day PI. The drug proved a promising chemoprophylactic agent when used five days before exposure to infection. PMID:15658062

Massoud, Ahmed M A; El Ebiary, Faika H; Abou-Gamra, Maha M M; Mohamed, Ghada F; Shaker, Safaa M

2004-12-01

8

Molluscicidal and schistosomicidal activities of a steroidal saponin containing fraction from Dracaena fragrans (L.).  

PubMed

The steroidal saponin-containing fraction from methanolic extract of Dracaena fragrans (Family: Agavaceae) was tested for molluscicidal and ovicidal activities against Biomphalaria alexandrina and Bulinus truncatus, the snail vectors of Schistosoma mansoni and S. haematobium in Egypt, respectively. It was also tested for schistosemicidal activity in vitro on adult S. mansoni and against the free-living miracidia and cercariae of the parasite. The homogenated soft body of B. alexandrina was used to determine the effect of the saponin fraction on total protein, albumen, aminotransferase enzymes and acetylcholin esterase. The results showed that the saponin fraction had considerable molluscicidal activity; LC50 & LC90 were 2.7 ppm & 3.7 ppm for B. alexandrina and 2 ppm & 2.5 ppm for B. truncatus, respectively. Snail eggs did not hatch in concentration as low as half molluscicidal LC50 (1.35 ppm). The LC50 killed all miracidia and cercariae in 30 seconds and after 22 & 40 minutes at a very low concentration (0.165 ppm) respectively, and had in vitro lethal effect on adults with LC50 18.4 microg/ml 4 days post-exposure. The snail tissue homogenate showed significant increase in total protein content & albumen, in aminotransferases and acetylcholinesterase activities. PMID:18853630

Tadros, M M; Ghaly, N S; Moharib, M N

2008-08-01

9

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, Ruben E.; Lopez-Aban, Julio; Dakir, E. L. Habib; Mollinedo, Faustino; Muro, Antonio

2014-01-01

10

In vitro activity of sertaconazole.  

PubMed

The activity of 7-chloro-3-[1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl) ethoxy-methyl]benzo[b]thiophene (sertaconazole, FI 7045, CAS 99592-32-2), a new topical antifungal, was studied in vitro against several infecting organisms. The results obtained show that sertaconazole is a broad-spectrum antifungal against yeasts (C. albicans, C. tropicalis, C. pseudotropicalis, C. krusei, Trichosporon and Cryptococcus), dermatophytes (Microsporum, Trichophyton and Epidermophyton), opportunistic filamentous fungi (Aspergillus) and Gram-positive bacteria. The MIC (minimum inhibitory concentration) values for the fungistatic activity were between 0.35 and 5.04 micrograms/ml for yeasts and between 0.24 and 2 micrograms/ml for dermatophytes; even partial activities (IC25) against these organisms were obtained at concentrations 10 times lower than those mentioned. At concentrations superior to MIC (MFC between 0.5 and 16 micrograms/ml), sertaconazole exhibited fungicidal activity. PMID:1627186

Palacín, C; Sacristán, A; Ortiz, J A

1992-05-01

11

Imatinib activity on Schistosoma mansoni  

PubMed Central

Imatinib, a drug used for treatment of human chronic myeloid leukaemia, due to its activity against protein kinases, has been also evaluated in vitro against Schistosoma mansoni showing high schistosomicidal activity. In the present experiments imatinib activity in vitro was confirmed at the doses of 25 µM, 50 µM and 100 µM. The first drug activity observed with the lower dose was interruption of egg-laying and with the higher dosages was the death of the worms. In mice infected with S. mansoni no activity was found even with 1,000 mg/kg/day, 500 mg/kg/day, single oral dose or when administered for three consecutive days. This is another example of the difference of results related to in vitro and in vivo trials using S. mansoni worms. PMID:24037106

Katz, Naftale; Couto, Flávia Fernanda Bubulo; Araújo, Neusa

2013-01-01

12

Salbutamol exhibits androgenic activity in vitro  

Microsoft Academic Search

Background:Salbutamol has been shown to mediate anabolic effects after intravenous administration. However, the mechanism responsible for the anabolic actions of salbutamol remains unknown.Aim:To investigate the potential mechanism by which salbutamol mediates anabolic effects in vitro.Methods:The potential androgenic activity of salbutamol was investigated in vitro by the A-Screen assay that measures androgen-dependent inhibition of proliferation of the androgen receptor (AR)-positive human

André O von Bueren; Risheng Ma; Margret Schlumpf; Walter Lichtensteiger

2007-01-01

13

Antimycobacterial activity of lichen metabolites in vitro  

Microsoft Academic Search

Several compounds, whose structures represent the most common chemical classes of lichen metabolites, were screened for in vitro activity against Mycobacterium aurum, a non-pathogenic organism with a similar sensitivity profile to M. tuberculosis. Of the compounds tested, usnic acid from Cladonia arbuscula exhibited the highest activity with an MIC value of 32 ?g\\/ml. Atranorin and lobaric acid, both isolated from

Krist??n Ingólfsdóttir; Gavin A. C. Chung; Vilhjálmur G. Skúlason; Stefán R. Gissurarson; Margrét Vilhelmsdóttir

1998-01-01

14

Hydroxytyrosol expresses antifungal activity in vitro.  

PubMed

Hydroxytyrosol (HT) is a potent antioxidant found in olive oil and leaves. Using several in vitro approaches, we tested antifungal activity of HT. HT showed broad spectrum of antifungal activity against medically important yeasts and dermatophyte strains with MIC values ranging between 97.6 µgml?ą and 6.25 mgml?ą. The antimicrobial activity of HT was also tested using the time-kill methodology. Below the MIC value, HT showed potent damage of cell wall of Candida albicans ATCC 10231 using fluorescent dye-exclusion method. At the subinhibitory concentration, HT also influenced dimorphic transition of Candida indicating that HT is inhibitor of germ-tube formation as one of the most important virulence factor of C. albicans. Furthermore, HT showed disturbances in cell surface hydrophobicity (CSH) of C. albicans. The in vitro results indicate that HT caused a significant cell wall damage and changes in CSH as well as inhibition of germ-tube formation as virulence factor of C. albicans. The study indicates that HT has a considerable in vitro antifungal activity against medically important yeasts. PMID:23721186

Zoric, Natasa; Horvat, Igor; Kopjar, Nevenka; Vucemilovic, Ante; Kremer, Dario; Tomic, Sinisa; Kosalec, Ivan

2013-08-01

15

Antimycobacterial activity of lichen metabolites in vitro.  

PubMed

Several compounds, whose structures represent the most common chemical classes of lichen metabolites, were screened for in vitro activity against Mycobacterium aurum, a non-pathogenic organism with a similar sensitivity profile to M. tuberculosis. Of the compounds tested, usnic acid from Cladonia arbuscula exhibited the highest activity with an MIC value of 32 microg/ml. Atranorin and lobaric acid, both isolated from Stereocaulon alpinum, salazinic acid from Parmelia saxatilis and protolichesterinic acid from Cetraria islandica all showed MIC values >/=125 microg/ml. PMID:9795033

Ingólfsdóttir, K; Chung, G A; Skúlason, V G; Gissurarson, S R; Vilhelmsdóttir, M

1998-04-01

16

In vitro and in vivo effects of hesperidin treatment on adult worms of Schistosoma mansoni.  

PubMed

Hesperidin has been reported to exert a wide range of pharmacological effects, including antifungal, antiviral, antioxidant, anti-inflammatory and anticarcinogenic activities. Herein, the schistosomicidal activity of this compound was evaluated in vitro and in vivo. Using an in vitro assay, a concentration of 200 ?g/ml of hesperidin resulted in the mortality of 100% adult worms of Schistosoma (S.) mansoni within 72 h and a partial tegumental alteration in 10% of worms. However, after 144 h incubation, 50 and 100 ?g/ml concentrations showed 0% and 10% mortality in adult worms, respectively, without any changes to the tegument. Sublethal doses did not influence egg output nor the development of eggs deposited by pairs of adult worms. In an in vivo study, mice infected with S. mansoni and treated with 600 mg hesperidin/kg body weight showed a respective reduction of 50, 45.2, 50 and 47.5% of males, females, worm pairs and total worm burden. In addition, a respective reduction, based on the number of eggs/g tissue, of 41.5, 63.7 and 58.6% was observed in the liver, intestine and liver/intestinal tissue combined. Furthermore, S. mansoni-specific IgG level significantly increased with hesperidin treatment, whereas IgA and IgE levels were not significantly changed. IgM levels decreased in response to cercarial antigen preparation but were not altered in response to soluble worm or soluble egg antigen. As in hesperidin-treated mice, praziquantel-treated mice showed a similar pattern of specific antibody response to S. mansoni antigens. The present study represents the first report on the effects of the schistosomicidal activity of hesperidin. PMID:23656891

Allam, G; Abuelsaad, A S A

2014-09-01

17

Anthelmintic activity of crude extract and essential oil of Tanacetum vulgare (Asteraceae) against adult worms of Schistosoma mansoni.  

PubMed

Schistosomiasis, a parasitic disease caused by trematode flatworms of the genus Schistosoma, affects more than 200 million people worldwide, and its control is dependent on a single drug, praziquantel. Tanacetum vulgare (Asteraceae) is used in folk medicine as a vermifuge. This study aimed to investigate the in vitro schistosomicidal activity of the crude extract (TV) and the essential oil (TV-EO) from the aerial parts of T. vulgare. TV-EO was obtained by hydrodistillation and analyzed by GC/MS, which allowed the identification of ?-thujone (84.13%) as the major constituent. TV and TV-EO, at 200 ?g/mL, decreased motor activity and caused 100% mortality of all adult worms. At 100 and 50 ?g/mL, only TV caused death of all adult worms, while TV-EO was inactive. TV (200 ?g/mL) was also able to reduce viability and decrease production of developed eggs. Confocal laser scanning microscopy showed morphological alterations in the tegument of the S. mansoni surface after incubation with TV (50 and 100 ?g/mL). Quantitative analysis on the schistosomes tegument showed that TV caused changes in the numbers of tubercles of S. mansoni male worms in a dose-dependent manner. The findings suggest that T. vulgare is a potential source of schistosomicidal compounds. PMID:24672320

Godinho, Loyana Silva; Aleixo de Carvalho, Lara Soares; Barbosa de Castro, Clarissa Campos; Dias, Mirna Meana; Pinto, Priscila de Faria; Crotti, Antônio Eduardo Miller; Pinto, Pedro Luiz Silva; de Moraes, Josué; Da Silva Filho, Ademar A

2014-01-01

18

Anthelmintic Activity of Crude Extract and Essential Oil of Tanacetum vulgare (Asteraceae) against Adult Worms of Schistosoma mansoni  

PubMed Central

Schistosomiasis, a parasitic disease caused by trematode flatworms of the genus Schistosoma, affects more than 200 million people worldwide, and its control is dependent on a single drug, praziquantel. Tanacetum vulgare (Asteraceae) is used in folk medicine as a vermifuge. This study aimed to investigate the in vitro schistosomicidal activity of the crude extract (TV) and the essential oil (TV-EO) from the aerial parts of T. vulgare. TV-EO was obtained by hydrodistillation and analyzed by GC/MS, which allowed the identification of ?-thujone (84.13%) as the major constituent. TV and TV-EO, at 200??g/mL, decreased motor activity and caused 100% mortality of all adult worms. At 100 and 50??g/mL, only TV caused death of all adult worms, while TV-EO was inactive. TV (200??g/mL) was also able to reduce viability and decrease production of developed eggs. Confocal laser scanning microscopy showed morphological alterations in the tegument of the S. mansoni surface after incubation with TV (50 and 100??g/mL). Quantitative analysis on the schistosomes tegument showed that TV caused changes in the numbers of tubercles of S. mansoni male worms in a dose-dependent manner. The findings suggest that T. vulgare is a potential source of schistosomicidal compounds. PMID:24672320

Godinho, Loyana Silva; Aleixo de Carvalho, Lara Soares; Barbosa de Castro, Clarissa Campos; Dias, Mirna Meana; Pinto, Priscila de Faria; Crotti, Antonio Eduardo Miller; Pinto, Pedro Luiz Silva; de Moraes, Josue; Da Silva Filho, Ademar A.

2014-01-01

19

In vitro activities of two glycylcyclines.  

PubMed Central

The in vitro activities of two glycylcyclines, CL 329,998 and CL 331,002 (two new semisynthetic tetracyclines), were evaluated in comparison with those of tetracycline and other available oral antimicrobial agents. A total of 523 recent clinical isolates were studied, including strains resistant to tetracycline. Members of the family Enterobacteriaceae were generally > or = 16-fold more susceptible to the glycylcyclines than to tetracycline (although less difference was seen with Proteus spp.). Pseudomonas aeruginosa was modestly susceptible to both new compounds (MIC for 90% of strains tested [MIC90], 16 micrograms/ml). Tetracycline- and methicillin-susceptible and -resistant strains of Staphylococcus aureus were all susceptible to the glycylcyclines (MIC90 < or = 1 microgram/ml). Streptococci (including Streptococcus pneumoniae) and Enterococcus faecalis and Enterococcus faecium displayed a bimodal distribution of susceptibility to tetracycline yet were uniformly susceptible to the glycylcyclines (MIC90 < or = 0.25 microgram/ml). The glycylcyclines were highly potent against Neisseria, Moraxella, Haemophilus, and Bacteroides spp. (MIC90 < or = 0.5 microgram/ml). Strains of Chlamydia spp. (three C. trachomatis strains and one C. pneumoniae strain) were inhibited by < or = 0.25 microgram of CL 329,998 or CL 331,002 per ml. Two strains of Mycoplasma pneumoniae were inhibited by < or = 0.12 microgram of CL 331,002 per ml and by 1 microgram of CL 329,998 per ml. Mycobacterium tuberculosis and Mycobacterium avium were resistant to the two glycylcyclines (MIC > or = 8 micrograms/ml). These results indicate that the two glycylcyclines have potent in vitro activities against a wide range of clinically important pathogenic bacteria. PMID:8067744

Wise, R; Andrews, J M

1994-01-01

20

In vitro antifungal activity of sertaconazole.  

PubMed

The antifungal activity of 7-chloro-3-[1-(2,4-dichlorophenyl)-2-(1H- imidazol-1-yl)ethoxy-methyl]benzo[b]thiophene (sertaconazole, FI-7045, CAS 99592-32-2) versus miconazole has been studied in vitro against yeast-like fungi, dermatophytes and other filamentous fungi. Candida albicans was very sensitive to sertaconazole both in serotype A and serotype B strains (MIC = 0.21 micrograms/ml). Sensitivity of Candida non albicans species (MIC = 0.17 microgram/ml), Torulopsis (MIC = 0.09 microgram/ml) and Trichosporon (MIC = 0.09 microgram/ml) was also remarkable. For dermatophytes, partial inhibitions were observed at concentrations of 0.04 and 0.09 microgram/ml, the 50% inhibition ranging between 0.36 and 12.56 micrograms/ml for most strains. Filamentous opportunistic fungi were less sensitive to azoles, although sertaconazole MICs were lower than those of miconazole. Sertaconazole also proved to possess a remarkable fungicidal activity on all strains of Candida albicans under study. PMID:1627187

Drouhet, E; Dupont, B

1992-05-01

21

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

22

In vitro antimicrobial activity of potash alum.  

PubMed

This study reports the bactericidal activity of potash alum when added to water, against various epidemic causing enteric pathogens like Vibrio cholerae 01, V. cholerae 0139 and Shigella dysenteriae 1 by lowering the pH of water (from 6.0 to 4.0). Growth of the enteric pathogens was monitored in vitro by inoculating broth cultures of the different organisms in distilled water containing increasing concentrations of potash alum and quantitatively determining the concentration of viable organisms over a 48 h period by the standard plate count method. Controls constituted cultures of each organism grown in the absence of potash alum. The pH of alum administered water was measured in each test tube before inoculation of organisms. Potash alum was found to inhibit growth (10(5) viable count per ml) of most of the organisms examined, particularly V. cholerae 01 and V. cholerae 0139 in a dose dependent fashion. Reduction of colony forming units was observed in presence of 0.25 g/dl of alum after 5 h and no growth was noticed after 24 h. PMID:8783521

Dutta, S; De, S P; Bhattacharya, S K

1996-07-01

23

In vitro activities of new quinolones against Helicobacter pylori.  

PubMed Central

Compounds belonging to a new class of quinolones in which the fundamental C-6 fluorine atom was replaced were evaluated for in vitro antibacterial activity against 32 Helicobacter pylori strains. Since these substitutions resulted in higher inhibitory activities, these new desfluoroquinolones may be useful in eradicating H. pylori infections. PMID:9420062

Carbone, M; Fera, M T; Cecchetti, V; Tabarrini, O; Losi, E; Cusumano, V; Teti, G

1997-01-01

24

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...

25

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, Gevanio Bezerra; Moreira, Diogo Rodrigo Magalhaes; Gomes, Paulo Andre Teixeira; da Silva, Anekecia Lauro; de Barros, Andreia Ferreira; da Silva, Aline Caroline; dos Santos, Thiago Andre Ramos; Pereira, Valeria Rego Alves; Goncalves, Gabriel Gazzoni Araujo; Brayner, Fabio Andre; Alves, Luiz Carlos; Wanderley, Almir Goncalves; Leite, Ana Cristina Lima

2014-01-01

26

Studies on the activities of rumen microorganisms in vitro  

E-print Network

STCDIES ON THE ACTIVITIES OF RUMEN MICROORGANISMS IN VITRO A Thesis Carl~Johnson Submitted to the, Gr;. dusts School of the Agricultural and Mec?anical Co13 cgs oi' Texas in partial fulfillment of the requirements for the degree of MAST'% OS... SCIENCE August 1)57 Major Subject: Animal Nutrition STUDIES CN THE ACTIVITIES OF RUNEN MICROORGANISMS IN VITRO A Thesis Carl Johnson Approved as to style and oontent b Cha of Committee Head of Department August 1957 ACIQIOWLEDGMENTS The author...

Johnson, Carl Edward

2012-06-07

27

In vitro Activity of Cefdinir (FK 482, PD 134393, CI983): A New Orally Active Cephalosporin  

Microsoft Academic Search

Cefdinir is a new orally active cephalosporin which is undergoing in vitro and in vivo evaluations. Using the standard agar dilution method we compared the in vitro activity of this drug with other (3-lactam antibiotics against clinical isolates or Ente-robacteriaceae (625 strains), Pseudomonas aeruginosa (68 strains), Xanthomonas maltophilia (36 strains), Acinetobacter (52 strains), Aeromonas hydrophilia (47 strains), staphylococci (364 strains)

Hussain Qadri; Yoshio Ueno; Hishama Saldin; Burke A. Cunha

1993-01-01

28

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

29

Spontaneous activity of neostriatal cholinergic interneurons in vitro.  

PubMed

Neostriatal cholinergic interneurons fire irregularly but tonically in vivo. The summation of relatively few depolarizing potentials and their temporal sequence are thought to underlie spike triggering and the irregularity of action potential timing, respectively. In these experiments we used whole-cell, cell-attached, and extracellular recording techniques to investigate the role of spontaneous synaptic inputs in the generation and patterning of action potentials in cholinergic interneurons in vitro. Cholinergic cells were spontaneously active in vitro at 25 +/- 1 degrees C during whole-cell recording from 2 to 3 week postnatal slices and at 35 +/- 2 degrees C during cell-attached and extracellular recording from 3 to 4 week postnatal slices. A range of firing frequencies and patterns was observed including regular, irregular, and burst firing. Blockade of AMPA and NMDA receptors altered neither the firing rate nor the pattern, and accordingly, voltage-clamp data revealed a very low incidence of spontaneous EPSCs. GABAA receptor antagonists were also ineffective in altering the spiking frequency or pattern owing to minimal inhibitory input in vitro. Functional excitatory and inhibitory inputs to cholinergic cells were disclosed after application of 4-aminopyridine (100 microM), indicating that these synapses are present but not active in vitro. Blockade of D1 or D2 dopamine receptors or muscarinic receptors also failed to influence tonic activity in cholinergic cells. Together these data indicate that cholinergic interneurons are endogenously active and generate action potentials in the absence of any synaptic input. Interspike interval histograms and autocorrelograms generated from unit recordings of cholinergic cells in vitro were indistinguishable from those of tonically active neurons recorded in vivo. Irregular spiking is therefore embedded in the mechanism responsible for endogenous activity. PMID:10377365

Bennett, B D; Wilson, C J

1999-07-01

30

In Vitro Activities of Four Novel Triazoles against Scedosporium spp  

Microsoft Academic Search

In order to develop new approaches to the treatment of the severe and usually fatal infections caused by Scedosporium spp., the in vitro antifungal activities of four novel triazoles (posaconazole, ravuconazole, vori- conazole, and UR-9825) and some current antifungals (amphotericin B, ketoconazole, itraconazole, and ny- statin) were determined. The latter group was clearly ineffective against the two species tested. The

A. J. Carrillo; J. Guarro

2001-01-01

31

Influence of gold nanoparticles on platelets functional activity in vitro  

Microsoft Academic Search

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

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

2008-01-01

32

In vitro screening of Indian medicinal plants for antiplasmodial activity  

Microsoft Academic Search

Plants traditionally used in India to treat fever or malaria were examined in vitro for antiplasmodial properties against Plasmodium falciparum. Of 80 analysed ethanol extracts, from 47 species, significant effects were found for 31 of the extracts. These represent 23 different species from 20 families. Of the active species 20 were tested against P. falciparum for the first time. The

Henrik Toft Simonsen; Jesper Brćndegaard Nordskjold; Ulla Wagner Smitt; Ulf Nyman; Pushpangadan Palpu; Prabhakar Joshi; George Varughese

2001-01-01

33

In vitro antimicrobial activity against 10 North American and European Lawsonia intracellularis isolates  

E-print Network

In vitro antimicrobial activity against 10 North American and European Lawsonia intracellularis to evaluate the antimicrobial activities of most intracellular organisms since these bacteria only propagate themselves inside the host cell. Therefore, most in vitro studies of antimicrobial activities against

Singer, Randall

34

In Vitro Anti-Candida Activity of Zataria multiflora Boiss  

PubMed Central

Zataria multiflora Boiss known as Avishan Shirazi (in Iran) is one of the valuable Iranian medicinal plants. The aim of study was to evaluate anti-Candida activity of Z. multiflora against different species of Candida in vitro. Anti-Candida activity of the aqueous, ethanolic and methanolic maceration extract of the aerial parts of Z. multiflora Boiss was studied in vitro. Anti-Candida activity against Candida species was done using serial dilutions of extracts in Sabouraud's dextrose agar. Minimal inhibitory concentration (MIC) of the methanolic and ethanolic extracts was 70.7 and 127 mg l?1, respectively. Aqueous extract showed no remarkable activity against Candida species. We conclude that methanolic extract of the aerial parts of Z. multiflora Boiss has more anti-Candida effect at 70.7 mg l?1 compared to ethanolic extract 127 mg l?1. In addition, the isolates of Candida parapsilosis were more susceptible to methanolic extract than other tested species. PMID:17965766

Dabbagh, Muhammad Ali; Fouladi, Zahra

2007-01-01

35

Human macrophage polarization in vitro: maturation and activation methods compared.  

PubMed

Macrophages form a heterogeneous cell population displaying multiple functions, and can be polarized into pro- (M1) or anti-inflammatory (M2) macrophages, by environmental factors. Their activation status reflects a beneficial or detrimental role in various diseases. Currently several in vitro maturation and activation protocols are used to induce an M1 or M2 phenotype. Here, the impact of different maturation factors (NHS, M-CSF, or GM-CSF) and activation methods (IFN-?/LPS, IL-4, dexamethason, IL-10) on the macrophage phenotype was determined. Regarding macrophage morphology, pro-inflammatory (M1) activation stimulated cell elongation, and anti-inflammatory (M2) activation induced a circular appearance. Activation with pro-inflammatory mediators led to increased CD40 and CD64 expression, whereas activation with anti-inflammatory factors resulted in increased levels of MR and CD163. Production of pro-inflammatory cytokines was induced by activation with IFN-?/LPS, and TGF-? production was enhanced by the maturation factors M-CSF and GM-CSF. Our data demonstrate that macrophage marker expression and cytokine production in vitro is highly dependent on both maturation and activation methods. In vivo macrophage activation is far more complex, since a plethora of stimuli are present. Hence, defining the macrophage activation status ex vivo on a limited number of markers could be indecisive. From this study we conclude that maturation with M-CSF or GM-CSF induces a moderate anti- or pro-inflammatory state respectively, compared to maturation with NHS. CD40 and CD64 are the most distinctive makers for human M1 and CD163 and MR for M2 macrophage activation and therefore can be helpful in determining the activation status of human macrophages ex vivo. PMID:24916404

Vogel, Daphne Y S; Glim, Judith E; Stavenuiter, Andrea W D; Breur, Marjolein; Heijnen, Priscilla; Amor, Sandra; Dijkstra, Christine D; Beelen, Robert H J

2014-09-01

36

Antitumor activity of the marine natural product dibromophakellstatin in vitro  

Microsoft Academic Search

The pyrrole-imidazole alkaloid rac-dibromophakellstatin displayed selective antitumor activity in vitro when tested in 36 cell lines in a cell survival and proliferation assay. The ovarian cancer cell line OVXF 899L proved to be most sensitive (0.60?M, IC50), followed by the glioblastoma cell line CNXF 498NL (0.93?M), the non-small lung cancer cell line LXF 529L (0.96?M), and the uterus cancer cell

Michael Zöllinger; Gerhard Kelter; Heinz-Herbert Fiebig; Thomas Lindel

2007-01-01

37

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

2014-12-01

38

In vitro antioxidant activity of extracts from common legumes.  

PubMed

The in vitro antioxidant activity of pinto bean, cowpea, baby lima bean, lentil, chickpea, small red bean, red kidney bean, black kidney bean, navy bean, and mung bean extracts were investigated. Significant differences were observed in the phenolic content and the antioxidant activity amongst the legume extracts. Lentils demonstrated the highest phenolic content (47.6 mg/g), total antioxidant activity (720.68 U/g), DPPH• scavenging activity (38.5%), and total reducing power, whereas baby lima beans and navy beans had the lowest. Amongst the extracts, hydroxyl radicals (•OH) scavenging was higher in black kidney bean (85.68%) and baby lima bean (74.97%) extracts. The total antioxidant activity (r=0.84), DPPH• scavenging activity (r=0.83), and total reducing power (r=0.84) were positively correlated with the total phenolic content. However, •OH scavenging and the phenolic content were not correlated. PMID:24444962

Zhao, Yan; Du, Shuang-kui; Wang, Hanxin; Cai, Meng

2014-01-01

39

Comparative in vitro antimicrobial activity of Chinese medicinal herbs.  

PubMed

Eighteen herbs used in the treatment of infectious diseases in traditional Chinese medicine were evaluated for in vitro activity against ten microbial pathogens. Lyophilized teas were tested by the agar dilution technique at 100-1600 micrograms/ml. Eleven of the preparations were active against at least one microorganism and six of these were active against at least three of the test isolates. Huangqin (Scutellaria sp.) and Huanglian (Coptis sp.) were each active against five of the isolates. Huangqin inhibited Klebsiella pneumoniae and Proteus vulgaris at 200 micrograms/ml. Huangqin alone showed strong activity against Mycobacterium smegmatis (less than or equal to 100 micrograms/ml) and Candida albicans (200 micrograms/ml). The antimicrobial activity of various teas, prepared with equal weights of herbs, could be compared against a particular pathogen by considering both the percentage of water-soluble material in the herbs and the minimum inhibitory concentrations of the filtered, lyophilized decoctions. PMID:3724208

Franzblau, S G; Cross, C

1986-03-01

40

In vitro activities of novel catecholate siderophores against Plasmodium falciparum.  

PubMed Central

The activities of novel iron chelators, alone and in combination with chloroquine, quinine, or artemether, were evaluated in vitro against susceptible and resistant clones of Plasmodium falciparum with a semimicroassay system. N4-nonyl,N1,N8-bis(2,3-dihydroxybenzoyl) spermidine hydrobromide (compound 7) demonstrated the highest level of activity: 170 nM against a chloroquine-susceptible clone and 1 microM against a chloroquine-resistant clone (50% inhibitory concentrations). Compounds 6, 8, and 10 showed antimalarial activity with 50% inhibitory concentrations of about 1 microM. Compound 7 had no effect on the activities of chloroquine, quinine, and artemether against either clone, and compound 8 did not enhance the schizontocidal action of either chloroquine or quinine against the chloroquine-resistant clone. The incubation of compound 7 with FeCI3 suppressed or decreased the in vitro antimalarial activity of compound 7, while no effect was observed with incubation of compound 7 with CuSO4 and ZnSO4. These results suggest that iron deprivation may be the main mechanism of action of compound 7 against the malarial parasites. Chelator compounds 7 and 8 primarily affected trophozoite stages, probably by influencing the activity of ribonucleotide reductase, and thus inhibiting DNA synthesis. PMID:8878587

Pradines, B; Ramiandrasoa, F; Basco, L K; Bricard, L; Kunesch, G; Le Bras, J

1996-01-01

41

Comparison of in vitro exemestane activity versus other antiaromatase agents.  

PubMed

Anastrozole, letrozole, and exemestane are the most selective and potent oral antiaromatase agents currently available. However, in vitro and in vivo studies comparing these agents are lacking. Anastrozole and letrozole are reversible, competitive nonsteroidal type II inhibitors, whereas exemestane is an irreversible steroidal type I inactivator. The study was conducted to determine the impact of this characteristic on in vitro residual aromatase activity and protein levels after incubation of JEG-3 cells with aminoglutethimide (a type II inhibitor), anastrozole, exemestane, or letrozole. Aromatase activity was measured after various incubation times with each antiaromatase agent at a concentration 10 times higher than IC50 (concentration giving 50% inhibition). Only exemestane induced a residual inhibition of aromatase activity after its removal, without any change in the aromatase protein level. Aromatase activity increased after preincubation of JEG-3 cells with either aminoglutethimide or anastrozole without any change in the aromatase protein level. The aromatase protein level increased rapidly when cells were incubated with letrozole and aromatase activity inhibition disappeared immediately after removal of the drug. The breakthrough effects in aromatase activity or protein levels observed after treatment with reversible inhibitors may be a factor in therapeutic failure with these agents. These results suggest a possible advantage for exemestane because it is the only clinically available oral irreversible aromatase inactivator. PMID:11970753

Soudon, J

2000-09-01

42

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

43

Activity of "reversed" diamidines against Trypanosoma cruzi "in vitro".  

PubMed

Chagas' disease is an important parasitic illness caused by the flagellated protozoan Trypanosoma cruzi. The disease affects nearly 17 million individuals in endemic areas of Latin America and the current chemotherapy is quite unsatisfactory based on nitroheterocyclic agents (nifurtimox and benznidazol). The need for new compounds with different modes of action is clear. Due to the broad-spectrum antimicrobial activity of the aromatic dicationic compounds, this study focused on the activity of four such diamidines (DB811, DB889, DB786, DB702) and a closely related diguanidine (DB711) against bloodstream trypomastigotes as well as intracellular amastigotes of T. cruzi in vitro. Additional studies were also conducted to access the toxicity of the compounds against mammalian cells in vitro. Our data show that the four diamidines compounds presented early and high anti-parasitic activity (IC50 in low-micromolecular range) exhibiting trypanocidal dose-dependent effects against both trypomastigote and amastigote forms of T. cruzi 2h after drug treatment. Most of the diamidines compounds (except the DB702) exerted high anti-parasitic activity and low toxicity to the mammalian cells. Our results show the activity of reversed diamidines against T. cruzi and suggested that the compounds merit in vivo studies. PMID:17462605

Silva, C F; Batista, Marcos Meuser; Mota, Renata Alves; de Souza, Elen Mello; Stephens, Chad E; Som, Phanneth; Boykin, David Wilson; Soeiro, Maria de Nazaré C

2007-06-15

44

In vitro activity of ME1401, a new antifungal agent.  

PubMed Central

The in vitro antifungal activity of ME1401, a potential topical antifungal agent, was compared with that of haloprogin, clotrimazole, miconazole, tolnaftate, and ciclopirox olamine by using an agar dilution procedure. ME1401 showed a broad antifungal spectrum and inhibited all of the 428 strains of 52 species of pathogenic yeasts and filamentous fungi tested at concentrations ranging from 0.01 to 12.5 micrograms/ml. In general, the activity of ME1401 was comparable or superior to that of clotrimazole and was greater than that of haloprogin and the other reference drugs under the conditions used. Only tolnaftate was superior to ME1401 in its activity against clinical isolates of Trichophyton rubrum. ME1401 showed no cross-resistance with any of the reference drugs and exhibited potent fungicidal activity. PMID:3800346

Yamaguchi, H; Uchida, K; Hiratani, T; Hara, T; Fukuyasu, H; Kazuno, Y; Inouye, S

1986-01-01

45

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

46

Anthelmintic activity in vitro and in vivo of Baccharis trimera (Less) DC against immature and adult worms of Schistosoma mansoni.  

PubMed

Although its efficiency against all Schistosoma species, praziquantel (PZQ) shows low efficacy against schistosomula and juvenile stages. The potential for development of resistance to PZQ has justified the search for new alternative chemotherapies. In this scenario, studies to new formulations, more comprehensive and without adverse effects, are being conducted. One viable and promising treatment is the study of medicinal plants as a new approach to the experimental treatment for Schistosomiasis. Amongst all the variety of the medicinal species studied, we can highlight Baccharis trimera (Less) DC, known as "Carqueja-amarga". This paper not only describes the effect of crude dichloromethane extract (DE) and aqueous fraction (AF) obtained from B. trimera, in vitro but also is the first one that investigates the in vivo efficacy of B. trimera against schistosomula, juvenile and adult worms of Schistosoma mansoni BH strain. In the experiment, mice were treated with DE, AF and PZQ (40 and 200mg/kg) over the period of larval development (3 and 30 post-infection; pi), and adult worms (60days post-infection; pi). The in vitro results show that the DE and AF effects are dose-dependents, being the 130?g/mL the most effective one in a shorter period of incubation. The exposure of the in vitro samples over adult parasites were able to inhibit 100% of the oviposition in females. Likewise caused the mortality of the parasites with morphological alterations on the tegument, on the suckers, oral and acetabulum, in both males and females after 6-72h of exposure. Additionally, the in vivo treatments against juvenile and adult infection were more effective compared to the control group untreated. Administrations of AF and DE in day 30pi (juvenile worms) show female worm total burden reductions of 75% and 68% respectively. At the same period of infection reductions of respectively 98% and 97% egg/g in the faeces were seen. In relation to the different egg developmental stages (oogram), the results showed significant reductions, due to the reduction in the number of worms, especially the females. In conclusion, B. trimera exhibits major schistosomicidal effects in vivo against immature and adult worms of S. mansoni, opening up perspectives for future researches on substance or compound isolation and the elucidation of its mechanisms of action. PMID:24602876

de Oliveira, Rosimeire Nunes; Rehder, Vera Lúcia Garcia; Oliveira, Adriana Silva Santos; Jeraldo, Veronica de Lourdes Sierpe; Linhares, Arício Xavier; Allegretti, Silmara Marques

2014-04-01

47

Characterization of photosynthetically active duckweed (Wolffia australiana) in vitro culture by Respiration Activity Monitoring System (RAMOS).  

PubMed

The feasibility of oxygen transfer rate (OTR) measurement to non-destructively monitor plant propagation and vitality of photosynthetically active plant in vitro culture of duckweed (Wolffia australiana, Lemnaceae) was tested using Respiration Activity Monitoring System (RAMOS). As a result, OTR proofed to be a sensitive indicator for plant vitality. The culture characterization under day/night light conditions, however, revealed a complex interaction between oxygen production and consumption, rendering OTR measurement an unsuitable tool to track plant propagation. However, RAMOS was found to be a useful tool in preliminary studies for process development of photosynthetically active plant in vitro cultures. PMID:17450327

Rechmann, Henrik; Friedrich, Andrea; Forouzan, Dara; Barth, Stefan; Schnabl, Heide; Biselli, Manfred; Boehm, Robert

2007-06-01

48

In vitro and in vivo activities of antibiotic PM181104.  

PubMed

Drug resistance has become a global threat that, if not addressed, may return us to the preantibiotic era. A way to overcome the problem of growing incidence of global antibiotic resistance is to introduce compounds belonging to classes that are new to the clinic. During a screening of the marine microbial extract library for new antibiotics, one of the extracts showed promising antibacterial activity against Gram-positive organisms. Bioactivity-guided isolation and characterization of active metabolites led to the discovery of a novel thiazolyl cyclic-peptide antibiotic, PM181104. It was isolated and characterized from a marine sponge-associated actinobacterium strain of the genus Kocuria (MTCC 5269). The compound exhibited a potent in vitro antibacterial activity against a broad range of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). The MIC values evaluated for the compound were found to be in the single-digit nanomolar range. In in vivo studies of PM181104 in a BALB/c murine septicemia model, the compound displayed 100% effective dose (ED100) values of 2.5 and 5.0 mg/kg of body weight against MRSA and 10.0 mg/kg against VRE. In this report, in vitro and in vivo studies of PM181104 are described. PMID:23939903

Mahajan, Girish; Thomas, Becky; Parab, Rajashri; Patel, Zarine E; Kuldharan, Sandip; Yemparala, Vijayaphanikumar; Mishra, Prabhu Dutt; Ranadive, Prafull; D'Souza, Lisette; Pari, Koteppa; Sivaramkrishnan, H

2013-11-01

49

In Vitro and In Vivo Activities of Antibiotic PM181104  

PubMed Central

Drug resistance has become a global threat that, if not addressed, may return us to the preantibiotic era. A way to overcome the problem of growing incidence of global antibiotic resistance is to introduce compounds belonging to classes that are new to the clinic. During a screening of the marine microbial extract library for new antibiotics, one of the extracts showed promising antibacterial activity against Gram-positive organisms. Bioactivity-guided isolation and characterization of active metabolites led to the discovery of a novel thiazolyl cyclic-peptide antibiotic, PM181104. It was isolated and characterized from a marine sponge-associated actinobacterium strain of the genus Kocuria (MTCC 5269). The compound exhibited a potent in vitro antibacterial activity against a broad range of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). The MIC values evaluated for the compound were found to be in the single-digit nanomolar range. In in vivo studies of PM181104 in a BALB/c murine septicemia model, the compound displayed 100% effective dose (ED100) values of 2.5 and 5.0 mg/kg of body weight against MRSA and 10.0 mg/kg against VRE. In this report, in vitro and in vivo studies of PM181104 are described. PMID:23939903

Thomas, Becky; Parab, Rajashri; Patel, Zarine E.; Kuldharan, Sandip; Yemparala, Vijayaphanikumar; Mishra, Prabhu Dutt; Ranadive, Prafull; D'Souza, Lisette; Pari, Koteppa; Sivaramkrishnan, H.

2013-01-01

50

Antioxidant activity of Botryococcus braunii extract elucidated in vitro models.  

PubMed

Botryococcus braunii is a green colonial microalga that is used mainly for the production of hydrocarbons, exopolysaccharides, and carotenoids. In the present study, the antioxidant properties of acetone extracts of B. braunii were evaluated using in vitro model systems such as 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydroxy radical scavenging, and lipid peroxidation in human low-density lipoprotein and rat tissues. Acetone extracts of B. braunii (equivalent to 10 ppm total carotenoid) exhibited 71 and 67% antioxidant activity in DPPH and hydroxyl radical scavenging model systems, respectively. Similarly, the extract also showed 72, 71, and 70% antioxidant activity in the liver, brain, and kidney of rats. Low-density lipoprotein oxidation induced by Cu2+ ions was also protected (22, 38, and 51%) by the algal extract in a dose-dependent manner (4, 6, and 8 ppm levels of total carotenoid). Thiobarbituric acid reactive substances concentration in the blood, liver, and kidney of rats was also significantly decreased in B. braunii treated samples compared with those of control. Carotenoids (violaxanthin, astaxanthin, lutein, zeaxanthin, chlorophylls a and b, and alpha, beta-carotene) identified in the B. braunii acetone extract may be exhibiting antioxidant activity. Among the carotenoids, lutein represents more than 75% of the total carotenoids. B. braunii extract was shown to be effective for protecting biological systems against various oxidative stresses in vitro. This is the first report on the antioxidant properties of B. braunii. PMID:16787003

Rao, Ambati Ranga; Sarada, Ravi; Baskaran, Vallikannan; Ravishankar, Gokare Aswathanarayana

2006-06-28

51

Rainbow trout macrophages in vitro: morphology and phagocytic activity.  

PubMed

The properties of macrophages from the pronephros of Rainbow trout (Salmo gairdneri Richardson) were studied in vitro. We found that phagocytes obtained from the pronephros constitute a non-homogeneous cell population. Three populations with different adherence properties were examined with special emphasis on morphology and phagocytic capacity. The differentiation of the three populations in culture was similar morphologically, and their phagocytic activity showed only small variations. The methods for cell separation and culture reported here are a useful tool for gaining better understanding of how Rainbow trout macrophages function in the immune response. PMID:7095232

Braun-Nesje, R; Kaplan, G; Seljelid, R

1982-01-01

52

In vitro inhibitory activities of Lauraceae aporphine alkaloids.  

PubMed

The in vitro anti-inflammatory effect of eight aporphine alkaloids isolated from the leaves of two Lauraceae plants (Pleurothyrium cinereum and Ocotea macrophylla) was evaluated through inhibition of two isozymes of cyclooxygenase (COX-1 and COX-2), 5-lipoxygenase (5-LOX), and platelet aggregation induced by PAF, AA and ADP. All alkaloids exhibited inhibitory activities against COX-2 (IC50 25.9-116 microM range) and PAF- and AA-induced platelet aggregation, while only four and three of them were good COX-1 and 5-LOX inhibitors, respectively. (+)-N-acetyl-nornantenine 6 was the most potent COX-2, 5-LOX, AA and PAF inhibitor. PMID:20420312

Coy Barrera, Ericsson David; Cuca Suárez, Luis Enrique

2010-03-01

53

[Biological activity of regulatory peptides in model experiments in vitro].  

PubMed

Biological effects of short regulatory peptides, pinealon, vesugen, vilon and epitalon were studied in model experiments in vitro. These peptides were found not to demonstrate direct antioxidant activity but be able to restrict lipid peroxidation of human lipoproteins by modification of their structure. The short peptides increase stability of red blood cell membranes toward osmotic hemolysis. They also elevate the stationary level of intracellular reactive oxygen species and at the same time decrease (all excepting epitalon) percent of dead cells in neuronal population. The suggestion was made that under in vivo conditions, short peptides may participate in apoptosis/necrosis regulation. PMID:18546826

Kozina, L S; Arutiunian, A V; Stvolinski?, S L; Khavinson, V Kh

2008-01-01

54

HIV-1 integrase crosslinked oligomers are active in vitro  

PubMed Central

The oligomeric state of active human immunodeficiency virus type 1 (HIV-1) integrase (IN) has not been clearly elucidated. We analyzed the activity of the different purified oligomeric forms of recombinant IN obtained after stabilization by platinum crosslinking. The crosslinked tetramer isolated by gel chromatography was able to catalyze the full-site integration of the two viral LTR ends into a target DNA in vitro, whereas the isolated dimeric form of the enzyme was involved in the processing and integration of only one viral end. Accurate concerted integration by IN tetramers was confirmed by cloning and sequencing. Kinetic studies of DNA-integrase complexes led us to propose a model explaining the formation of an active complex. Our data suggest that the tetrameric IN bound to the viral DNA ends is the minimal complex involved in the concerted integration of both LTRs and should be the oligomeric form targeted by future inhibitors. PMID:15718297

Faure, Aurelie; Calmels, Christina; Desjobert, Cecile; Castroviejo, Michel; Caumont-Sarcos, Anne; Tarrago-Litvak, Laura; Litvak, Simon; Parissi, Vincent

2005-01-01

55

[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

56

Antimicrobial activity of topical skin pharmaceuticals - an in vitro study.  

PubMed

The aim of this study was to investigate the antimicrobial activity of currently available topical skin pharmaceuticals against Candida albicans, Escherichia coli, Staphylococcus aureus, Staphylococcus epidermidis and Streptococcus pyogenes. The agar dilution assay was used to determine the minimal inhibitory concentration for cream formulations and their active substances. Corticosteroid formulations with the antiseptics clioquinol or halquinol were active against all microbes. The hydrogen peroxide formulation was primarily active against staphylococci. Clotrimazole, miconazole and econazole showed an effect against staphylococci in addition to their effect on C. albicans. In contrast, terbinafine had no antibacterial effect. Fusidic acid was active against staphylococci, with slightly weaker activity against S. pyogenes and no activity against C. albicans or E. coli. In summary, some topical skin pharmaceuticals have broad antimicrobial activity in vitro, clioquinol and halquinol being the most diverse. In limited superficial skin infection topical treatment can be an alternative to systemic antibiotics and should be considered. With the global threat of multi-resistant bacteria there is a need for new, topical, non-resistance-promoting, antimicrobial preparations for the treatment of skin infections. PMID:20526539

Alsterholm, Mikael; Karami, Nahid; Faergemann, Jan

2010-05-01

57

Revealing phosphoproteins playing role in tobacco pollen activated in vitro.  

PubMed

The transition between the quiescent mature and the metabolically active germinating pollen grain most probably involves changes in protein phosphorylation status, since phosphorylation has been implicated in the regulation of many cellular processes. Given that, only a minor proportion of cellular proteins are phosphorylated at any one time, and that phosphorylated and nonphosphorylated forms of many proteins can co-exist within a cell, the identification of phosphoproteins requires some prior enrichment from a crude protein extract. Here, we have used metal oxide/hydroxide affinity chromatography (MOAC) based on an aluminum hydroxide matrix for this purpose, and have generated a population of phosphoprotein candidates from both mature and in vitro activated tobacco pollen grains. Both electrophoretic and nonelectrophoretic methods, allied to MS, were applied to these extracts to identify a set of 139 phosphoprotein candidates. In vitro phosphorylation was also used to validate the spectrum of phosphoprotein candidates obtained by the MOAC phosphoprotein enrichment. Since only one phosphorylation site was detected by the above approach, titanium dioxide phosphopeptide enrichment of trypsinized mature pollen crude extract was performed as well. It resulted in a detection of additional 51 phosphorylation sites giving a total of 52 identified phosphosites in this set of 139 phosphoprotein candidates. PMID:22976843

Fíla, Jan; Matros, Andrea; Radau, Sonja; Zahedi, René Peiman; Capková, V?ra; Mock, Hans-Peter; Honys, David

2012-11-01

58

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

59

In vitro antioxidant activity of Rubus ellipticus fruits  

PubMed Central

Various studies have been done to identify antioxidants from plant sources and efforts have been taken to incorporate it in conventional therapy. In our present study, petroleum ether, ethanolic, and aqueous extracts of Rubus ellipticus fruits have been evaluated for in vitro antioxidant activity using DPPH radical scavenging and reducing power assay. BHA was used as a standard antioxidant for DPPH radical scavenging activity. The reducing power assay of extracts was carried out with ascorbic acid as a standard reducing agent. All the analysis was made with the use of UV-Visible spectrophotometer. The results of the both assay showed that all the extracts of R. ellipticus fruits possess significant free radical scavenging and reducing power properties at concentration-dependent manner. Hence, it can be concluded that the R. ellipticus fruits could be pharmaceutically exploited for antioxidant properties. PMID:22171292

Sharma, Uma Shankar; Kumar, Arun

2011-01-01

60

Nitroimidazoles: in vitro activity and efficacy in anaerobic infections.  

PubMed

Nitroimidazoles, including metronidazole, tinidazole and ornidazole, are low molecular weight antimicrobial compounds with excellent activity against anaerobic microorganisms. These compounds are usually bactericidal at low concentrations and their spectrum of activity encompasses almost all the anaerobic bacteria and some capnophylic organisms. The few anaerobic bacteria known to be resistant to the nitroimidazoles include occasional anaerobic cocci, some nonsporing gram positive bacilli and Propionibacterium. Nitroimidazoles are the most active antimicrobial agents known against Bacteroides fragilis, the most resistant of anaerobic bacteria. Kill-curve studies demonstrate that there is a 2 to 5 log decrease in the number of colony forming units with Bacteroides fragilis and clostridium perfringens within one hour. The killing is unaffected by inoculum, growth rate or components of the medium. However, a metronidazole resistant isolate of B. fragilis has been shown to have decreased ability to take up 14C-metronidazole as well as lessened ability to reduce metronidazole. This is associated with a decrease in the nitroreductase activity. The in vitro observations have also been demonstrated in vivo. Clinical studies have shown nitroimidazoles to be efficacious in the therapy of a variety of anaerobic infections including non-traumatic brain abscess, intraabdominal abscesses, pelvic suppuration and necrotizing soft tissue infections. However, there have been disappointing results in the therapy of anaerobic pleuropulmonary infections, with a number of superinfections caused by aerobic bacteria. PMID:6941456

Tally, F P; Goldin, B; Sullivan, N E

1981-01-01

61

Silver and Gold Nanoparticles Alter Cathepsin Activity In vitro  

NASA Astrophysics Data System (ADS)

Nanomaterials are being incorporated into many biological applications for use as therapeutics, sensors, or labels. Silver nanomaterials are being utilized for biological implants and wound dressings as an antiviral material, whereas gold nanomaterials are being used as biological labels or sensors due to their surface properties and biocompatibility. Cytotoxicity data of these materials are becoming more prevalent; however, little research has been performed to understand how the introduction of these materials into cells affects cellular processes. Here, we demonstrate the impact that silver and gold nanoparticles have on cathepsin activity in vitro. Cathepsins are important cellular proteases that are imperative for proper immune system function. We have selected to examine gold and silver nanoparticles due to the increased use of these materials in biological applications. This manuscript depicts how both of these types of nanomaterials affect cathepsin activity, which could impact the host's immune system and its ability to respond to pathogens. Cathepsin B activity decreases in a dose-dependent manner with all nanoparticles tested. Alternatively, the impact of nanoparticles on cathepsin L activity depends greatly on the type and size of the material.

Speshock, Janice L.; Braydich-Stolle, Laura K.; Szymanski, Eric R.; Hussain, Saber M.

2010-12-01

62

Silver and Gold Nanoparticles Alter Cathepsin Activity In vitro  

NASA Astrophysics Data System (ADS)

Nanomaterials are being incorporated into many biological applications for use as therapeutics, sensors, or labels. Silver nanomaterials are being utilized for biological implants and wound dressings as an antiviral material, whereas gold nanomaterials are being used as biological labels or sensors due to their surface properties and biocompatibility. Cytotoxicity data of these materials are becoming more prevalent; however, little research has been performed to understand how the introduction of these materials into cells affects cellular processes. Here, we demonstrate the impact that silver and gold nanoparticles have on cathepsin activity in vitro. Cathepsins are important cellular proteases that are imperative for proper immune system function. We have selected to examine gold and silver nanoparticles due to the increased use of these materials in biological applications. This manuscript depicts how both of these types of nanomaterials affect cathepsin activity, which could impact the host's immune system and its ability to respond to pathogens. Cathepsin B activity decreases in a dose-dependent manner with all nanoparticles tested. Alternatively, the impact of nanoparticles on cathepsin L activity depends greatly on the type and size of the material.

Speshock, Janice L.; Braydich-Stolle, Laura K.; Szymanski, Eric R.; Hussain, Saber M.

2011-12-01

63

Potent antimalarial activity of acriflavine in vitro and in vivo.  

PubMed

Malaria continues to be a major health problem globally. There is an urgent need to find new antimalarials. Acriflavine (ACF) is known as an antibacterial agent and more recently as an anticancer agent. Here, we report that ACF inhibits the growth of asexual stages of both chloroquine (CQ) sensitive and resistant strains of human malarial parasite, Plasmodium falciparum in vitro at nanomolar concentration. ACF clears the malaria infection in vivo from the bloodstreams of mice infected with Plasmodium berghei. Interestingly, ACF is accumulated only in the parasitized red blood cells (RBCs) and parasite specific transporters may have role in this specific drug accumulation. We further show that ACF impairs DNA replication foci formation in the parasites and affects the enzymatic activities of apicoplast specific Gyrase protein. We thus establish ACF as a potential antimalarial amidst the widespread incidences of drug resistant Plasmodium strains. PMID:25089658

Dana, Srikanta; Prusty, Dhaneswar; Dhayal, Devender; Gupta, Mohit Kumar; Dar, Ashraf; Sen, Sobhan; Mukhopadhyay, Pritam; Adak, Tridibesh; Dhar, Suman Kumar

2014-10-17

64

Hexahydrocolupulone and its antitumor cell proliferation activity in vitro.  

PubMed

The purpose of this study was to evaluate the ability of hexahydrocolupulone (HHC) to inhibit the growth of tumor cells in vitro and to investigate the potential mechanism(s) involved. HHC was demonstrated to have a wide spectrum of activity against a number of established human tumor cell lines, including some exhibiting drug resistance. Culturing human breast adenocarcinoma (MCF-7) cells in the presence of HHC for 18 hr resulted in a significant decrease in the incorporation of [3H]uridine and [3H]leucine into RNA and protein, respectively. MCF-7 cells cultured in the presence of 1.5 microM HHC for 48 hr demonstrated an increase in the amount of cells detected in G0/G1 and a decrease in the amount of cells detected in S phase. In contrast, treatment with 25 microM HHC decreased the amount of cells detected in G0/G1 and increased the amount of cells detected in S phase. HHC did not cause single-stranded or double-stranded DNA breaks, interfere with topoisomerase function, or generate free radicals. Mice injected intraperitoneally for 5 consecutive days with HHC to a final in vivo blood concentration of 200 microM survived and showed no obvious signs of toxicity. Mass spectroscopy analysis, crystal generation, and structure elucidation confirmed HHC purity. Consequently, all activity observed can be attributed to HHC, a metabolite, and/or a combination thereof. These data suggest that HHC inhibits tumor cell proliferation in vitro via a mechanism(s) that may involve effects on macromolecular synthesis, precursor metabolism/transport, and/or the cell cycle or cell cycle-dependent pathway(s). PMID:9514086

Stephan, T E; Ngo, E O; Nutter, L M

1998-02-15

65

Screening for In Vitro and In Vivo Antitumor Activities of the Mushroom Agaricus Blazei  

Microsoft Academic Search

We have investigated the in vitro antitumor activity of the mushroom Agaricus blazei Murill on human cancer cell lines as well as its potential anticancer activity in a model of rat colon carcinogenesis. The in vitro anticancer analysis was performed using 9 human cancer cell lines incubated with organic and aqueous extracts of A. blazei. Antitumor activity was observed with

Liane Ziliotto; Fabriciano Pinheiro; Luís Fernando Barbisan; Maria Aparecida Marchesan Rodrigues

2009-01-01

66

Periodic oscillatory activity in parahippocampal slices maintained in vitro.  

PubMed

Brain slices maintained in vitro have been extensively used for studying neuronal synchronization. However, the validity of this approach may be questioned since pharmacological procedures are usually required to elicit spontaneous events similar to the EEG activity recorded in vivo. Here, we report that when superfused with control medium, rat brain slices comprising the entorhinal and perirhinal cortices along with a portion of the basolateral/lateral nuclei of the amygdala can synchronously generate periodic oscillatory activity at 5-11 Hz every 5-30 s. The periodic events: (i) correspond intracellularly to synaptic depolarizations in regularly firing neurons analyzed in the three areas; (ii) have no fixed site of onset; (iii) spread with time lags of 8-20 ms; and (iv) continue to occur asynchronously after their surgical isolation. NMDA receptor antagonism reduced the duration of the oscillatory events, while glutamatergic non-NMDA receptor antagonism abolished them. Activation of mu-opioid receptors, a procedure that hyperpolarizes interneurons thus decreasing GABA release, reversibly decreased the rate of occurrence of periodic oscillatory activity (POA). However, periodic events continued to occur during application of GABA(A) or GABA(B) receptor antagonists as well as in the presence of the cholinergic agent carbachol. We also found that POA was abolished by baclofen and irreversibly reduced by the gap junction decoupler carbenoxolone. These findings demonstrate that parahippocampal networks in a brain slice preparation can generate periodic, synchronous activity under quasi-physiological conditions. These network oscillations (i) reflect the activation of ionotropic glutamatergic and GABAergic receptors, (ii) are contributed by gap-junction interactions, and (iii) are controlled by GABA(B) receptors that are presumably located presynaptically. PMID:15652999

Kano, T; Inaba, Y; Avoli, M

2005-01-01

67

In vitro antiplatelet activity of flavonoids from Leuzea carthamoides.  

PubMed

Plants and their secondary metabolites, including flavonoids, exhibit a wide range of biological effects. Consequently, natural substances are receiving an increased attention in medicinal research. Owing to these facts, in vitro antiplatelet activity of ethanol summary extract and four flavonoids from Leuzea carthamoides was determined in human platelet-rich plasma. Arachidonic acid (AA), adenosine diphosphate (ADP), collagen (COL), and thrombin were used as agonists of platelet aggregation. The summary extract showed a significant inhibition of the aggregation induced by COL and ADP. Of the tested flavonoids, eriodictyol (1) and patuletin (2) influenced COL- and AA-induced aggregation. Their IC(50) values are presented. Flavonoid glycosides eriodictyol-7-beta-glucopyranoside (3) and 6-hydroxykaempferol-7-O-(6''-O-acetyl-beta-D[small cap]-glucopyranoside) (4) were found to be weak antiplatelet agents. These results confirmed the fact that glucosylation decreases the antiplatelet activity. Quantitative composition of tested flavonoids in L. carthamoides extract was also determined. Though two of the tested flavonoids inhibited platelet aggregation, further evaluation of L. carthamoides, in order to discover other antiplatelet active compounds and possible adverse health effects, is needed. PMID:18161506

Koleckar, Vit; Brojerova, Eliska; Rehakova, Zuzana; Kubikova, Katerina; Cervenka, Frantisek; Kuca, Kamil; Jun, Daniel; Hronek, Miloslav; Opletalova, Veronika; Opletal, Lubomir

2008-01-01

68

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

69

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

70

Assessment of antioxidant activity by using different in vitro methods.  

PubMed

In this study, six common tests for measuring antioxidant activity were evaluated by comparing four antioxidants and applying them to beverages (tea and juices): Trolox equivalent antioxidant capacity assay (TEAC I-III assay), Total radical-trapping antioxidant parameter assay (TRAP assay), 2,2-diphenyl-l-picrylhydrazyl assay (DPPH assay), N,N-dimethyl-p-phenylendiamine assay (DMPD assay), Photochemiluminescence assay (PCL assay) and Ferric reducing ability of plasma assay (FRAP assay). The antioxidants included gallic acid representing the group of polyphenols, uric acid as the main antioxidant in human plasma, ascorbic acid as a vitamin widely spread in fruits and Trolox as water soluble vitamin E analogue. The six methods presented can be divided into two groups depending on the oxidising reagent. Five methods use organic radical producers (TEAC I-III, TRAP, DPPH, DMPD, PCL) and one method works with metal ions for oxidation (FRAP). Another difference between these tests is the reaction procedure. Three assays use the delay in oxidation and determine the lag phase as parameter for the antioxidant activity (TEAC I, TRAP, PCL). They determine the delay of radical generation as well as the ability to scavenge the radical. In contrast, the assays TEAC II and III, DPPH, DMPD and FRAP analyse the ability to reduce the radical cation (TEAC II and III, DPPH, DMPD) or the ferric ion (FRAP). The three tests acting by radical reduction use preformed radicals and determine the decrease in absorbance while the FRAP assay measures the formed ferrous ions by increased absorbance. Gallic acid was the strongest antioxidant in all tests with exception of the DMPD assay. In contrast, uric acid and ascorbic acid showed low activity in some assays. Most of the assays determine the antioxidant activity in the micromolar range needing minutes to hours. Only one assay (PCL) is able to analyse the antioxidant activity in the nanomolar range. Black currant juice showed highest antioxidant activity in all tests compared to tea, apple juice and tomato juice. Despite these differences, results of these in vitro assays give an idea of the protective efficacy of secondary plant products. It is strongly recommended to use at least two methods due to the differences between the test systems investigated. PMID:11999386

Schlesier, K; Harwat, M; Böhm, V; Bitsch, R

2002-02-01

71

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

72

In Vitro Antimicrobial Activities of Bakuchiol against Oral Microorganisms  

PubMed Central

Bakuchiol was isolated from the seeds of Psoralea corylifolia, a tree native to China with various uses in traditional medicine, followed by extraction with ether and column chromatography combined with silica gel and octyldecyl silane. In this study, the antimicrobial activities of bakuchiol against some oral microorganisms were evaluated in vitro. The cell growth of Streptococcus mutans was inhibited in a bakuchiol concentration-dependent manner, and growth of S. mutans was completely prevented by 20 ?g of bakuchiol per ml. The bactericidal effect of bakuchiol on S. mutans was dependent on temperature and stable under the following conditions: sucrose, 0 to 10% (wt/vol); pH, 3.0 to 7.0; organic acids (3% [wt/vol] citric and malic acids). Bakuchiol showed bactericidal effects against all bacteria tested, including S. mutans, Streptococcus sanguis, Streptococcus salivarius, Streptococcus sobrinus, Enterococcus faecalis, Enterococcus faecium, Lactobacillus acidophilus, Lactobacillus casei, Lactobacillus plantarum, Actinomyces viscosus, and Porphyromonas gingivalis, with MICs ranging from 1 to 4 ?g/ml and the sterilizing concentration for 15 min ranging from 5 to 20 ?g/ml. Furthermore, bakuchiol was also effective against adherent cells of S. mutans in water-insoluble glucan in the presence of sucrose and inhibited the reduction of pH in the broth. Thus, bakuchiol would be a useful compound for development of antibacterial agents against oral pathogens and has great potential for use in food additives and mouthwash for preventing and treating dental caries. PMID:11600349

Katsura, Harumi; Tsukiyama, Ryo-Ichi; Suzuki, Akiko; Kobayashi, Makio

2001-01-01

73

In vitro antimicrobial activities of bakuchiol against oral microorganisms.  

PubMed

Bakuchiol was isolated from the seeds of Psoralea corylifolia, a tree native to China with various uses in traditional medicine, followed by extraction with ether and column chromatography combined with silica gel and octyldecyl silane. In this study, the antimicrobial activities of bakuchiol against some oral microorganisms were evaluated in vitro. The cell growth of Streptococcus mutans was inhibited in a bakuchiol concentration-dependent manner, and growth of S. mutans was completely prevented by 20 microg of bakuchiol per ml. The bactericidal effect of bakuchiol on S. mutans was dependent on temperature and stable under the following conditions: sucrose, 0 to 10% (wt/vol); pH, 3.0 to 7.0; organic acids (3% [wt/vol] citric and malic acids). Bakuchiol showed bactericidal effects against all bacteria tested, including S. mutans, Streptococcus sanguis, Streptococcus salivarius, Streptococcus sobrinus, Enterococcus faecalis, Enterococcus faecium, Lactobacillus acidophilus, Lactobacillus casei, Lactobacillus plantarum, Actinomyces viscosus, and Porphyromonas gingivalis, with MICs ranging from 1 to 4 microg/ml and the sterilizing concentration for 15 min ranging from 5 to 20 microg/ml. Furthermore, bakuchiol was also effective against adherent cells of S. mutans in water-insoluble glucan in the presence of sucrose and inhibited the reduction of pH in the broth. Thus, bakuchiol would be a useful compound for development of antibacterial agents against oral pathogens and has great potential for use in food additives and mouthwash for preventing and treating dental caries. PMID:11600349

Katsura, H; Tsukiyama, R I; Suzuki, A; Kobayashi, M

2001-11-01

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

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 MIC(90)s/minimum bactericidal concentrations (MBC(90)s) 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 MIC(90)s/MBC(90)s of NB003 and BPOs increased to 128/1,024 and 400/1,600 ?g/ml, respectively. The MIC(90)s/MBC(90)s of SA were not significantly impacted by the presence of sebum. A reduction in the MBC(90)s for NB-003 and BPO was observed when 2% SA or 0.5% BPO was integrated into the formulation, resulting in MIC(90)s/MBC(90)s 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 MIC(90) and MBC(90), yielding a more potent MIC(90)/MBC(90) 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

2011-09-01

76

Amphipathic DNA Polymers Exhibit Antiherpetic Activity In Vitro and In Vivo  

Microsoft Academic Search

Phosphorothioated oligonucleotides have a sequence-independent antiviral activity as amphipathic polymers (APs). The activity of these agents against herpesvirus infections in vitro and in vivo was investigated. The previously established sequence-independent, phosphorothioation-dependent antiviral activity of APs was confirmed in vitro by showing that a variety of equivalently sized homo- and heteropolymeric AP sequences were similarly active against herpes simplex virus type

David I. Bernstein; Nathalie Goyette; Rhonda Cardin; Earl R. Kern; Guy Boivin; James Ireland; Jean-Marc Juteau; Andrew Vaillant

2008-01-01

77

Danthron activates AMP-activated protein kinase and regulates lipid and glucose metabolism in vitro  

PubMed Central

Aim: To discover the active compound on AMP-activated protein kinase (AMPK) activation and investigate the effects of the active compound 1,8-dihydroxyanthraquinone (danthron) from the traditional Chinese medicine rhubarb on AMPK-mediated lipid and glucose metabolism in vitro. Methods: HepG2 and C2C12 cells were used. Cell viability was determined using MTT assay. Real-time PCR was performed to measure the gene expression. Western blotting assay was applied to investigate the protein phosphorylation level. Enzymatic assay kits were used to detect the total cholesterol (TC), triglyceride (TG) and glucose contents. Results: Danthron (0.1, 1, and 10 ?mol/L) dose-dependently promoted the phosphorylation of AMPK and acetyl-CoA carboxylase (ACC) in both HepG2 and C2C12 cells. Meanwhile, danthron treatment significantly reduced the lipid synthesis related sterol regulatory element-binding protein 1c (SREBP1c) and fatty acid synthetase (FAS) gene expressions, and the TC and TG levels. In addition, danthron treatment efficiently increased glucose consumption. The actions of danthron on lipid and glucose metabolism were abolished or reversed by co-treatment with the AMPK inhibitor compound C. Conclusion: Danthron effectively reduces intracellular lipid contents and enhanced glucose consumption in vitro via activation of AMPK signaling pathway. PMID:23770982

Zhou, Rong; Wang, Ling; Xu, Xing; Chen, Jing; Hu, Li-hong; Chen, Li-li; Shen, Xu

2013-01-01

78

Changes in peroxidase activity during in vitro rooting of oil palm ( Elaeis guineensis Jacq.)  

Microsoft Academic Search

Following induction by auxin treatment, the rooting performance of Elaeis guineensis Jacq. shoots obtained through in vitro clonal propagation by somatic embryogenesis varies considerably. This study involved a preliminary evaluation of guaiacol-peroxidase activity as a marker of in vitro rooting. It was carried out on 17 different clones obtained through a large-scale micropropagation procedure. No rooting occurred in the absence

Alain Rival; Florence Bernard; Yvan Mathieu

1997-01-01

79

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

80

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

PubMed

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. PMID:16481163

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

2006-05-01

81

Pseudorabies Virus Infection Alters Neuronal Activity and Connectivity In Vitro  

Microsoft Academic Search

Alpha-herpesviruses, including human herpes simplex virus 1 & 2, varicella zoster virus and the swine pseudorabies virus (PRV), infect the peripheral nervous system of their hosts. Symptoms of infection often include itching, numbness, or pain indicative of altered neurological function. To determine if there is an in vitro electrophysiological correlate to these characteristic in vivo symptoms, we infected cultured rat

Kelly M. McCarthy; David W. Tank; Lynn W. Enquist

2009-01-01

82

In vitro Antibacterial Activity of Lucilia sericata Maggot Secretions  

Microsoft Academic Search

Maggots of the green blowfly, Lucilia sericata, are used as an alternative to surgical intervention and long-term antiseptic therapy for the treatment of chronic wounds. The secretions of maggots are known to have antibacterial properties. To quantify the bactericidal effect of secretions from larvae of L. sericata, an in vitro test model based on the modified European quantitative suspension test

G. Daeschlein; K. Y. Mumcuoglu; O. Assadian; B. Hoffmeister; A. Kramer

2007-01-01

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 antioxidant activity of exopolysaccharide fractions from Bifidobacterium animalis RH  

Microsoft Academic Search

The aim of the study was to purify the exopolysaccharides (EPS) produced from Bifidobacterium animalis RH, which was isolated from the feces of Bama centenarians in Guangxi of China, and evaluate their antioxidant activities in vitro and in vivo. 2 fractions, a neutral EPS fraction (EPSa) and an acidic EPS fraction (EPSb), were obtained and compared for antioxidative activity. In vitro, they both

Rihua Xu; Nan Shang; Pinglan Li

2011-01-01

85

Phagocytic activity of Limulus polyphemus amebocytes in vitro.  

PubMed

Phagocytosis of invading microorganisms is a fundamental component of innate immunity. The Atlantic horseshoe crab, Limulus polyphemus, possesses a single immune cell type, the granular amebocyte. Amebocytes release a repertoire of potent immune effectors in the presence of pathogens, and function in hemostasis. In contrast to other arthropod immunocytes, the properties of amebocyte phagocytosis remain poorly characterised, restricted by the technical challenges associated with handling these labile cells. We have addressed these challenges and observed the internalisation of microbial and synthetic targets by amebocytes in vitro. Confirmation of target internalisation was achieved using a combination of fluorescent quenching and lipophilic membrane probes: R18 and FM 1-43. Viability, morphological integrity and functionality of extracted amebocytes appeared to be retained in vitro. The phagocytic properties of L. polyphemus amebocytes described here, in the absence of endotoxin, are similar to those observed for arthropod immunocytes and mammalian neutrophils. PMID:22910042

Coates, Christopher J; Whalley, Tim; Nairn, Jacqueline

2012-11-01

86

In Vitro Activity of Ceftaroline against a Broad Spectrum of Recent Clinical Anaerobic Isolates ?  

PubMed Central

The in vitro activity of ceftaroline was compared with those of ceftriaxone, clindamycin, imipenem, metronidazole, moxifloxacin, tigecycline, and vancomycin against 514 clinical anaerobic isolates using Clinical and Laboratory Standards Institute (CLSI) standard methodology. Ceftaroline demonstrated good to excellent activity against Gram-positive anaerobic pathogens and limited activity against Gram-negative pathogens, particularly Bacteroides fragilis group isolates. PMID:21041506

Snydman, David R.; Jacobus, Nilda V.; McDermott, Laura A.

2011-01-01

87

In vitro activity of moxifloxacin, levofloxacin, gatifloxacin and linezolid against Mycobacterium tuberculosis  

Microsoft Academic Search

The in vitro activity of moxifloxacin, gatifloxacin, levofloxacin and linezolid was evaluated against 234 strains of Mycobacterium tuberculosis isolated in the Southeast of Spain. All drugs tested showed good activity, with an MIC90 of less than 1 mg\\/l, and were active against isociacide and rifampicin resistant strains. Three strains were resistant to isoniazid and to the fluoroquinolones, which suggested the

J. C Rodr??guez; M Ruiz; M López; G Royo

2002-01-01

88

In Vitro Activities of Ketoconazole, Econazole, Miconazole, and Melaleuca alternifolia (Tea Tree) Oil against Malassezia Species  

PubMed Central

The in vitro activities of ketoconazole, econazole, miconazole, and tea tree oil against 54 Malassezia isolates were determined by agar and broth dilution methods. Ketoconazole was more active than both econazole and miconazole, which showed very similar activities. M. furfur was the least susceptible species. M. sympodialis, M. slooffiae, M. globosa, and M. obtusa showed similar susceptibilities to the four agents. PMID:10639388

Hammer, K. A.; Carson, C. F.; Riley, T. V.

2000-01-01

89

Synthesis, in vitro antimicrobial and cytotoxic activities of novel pyrimidine-benzimidazol combinations.  

PubMed

A series of novel 4-substituted-2-{[(1H-benzo[d]imidazol-2-yl)methyl] thio}-6-methylpyrimidine derivatives were designed, synthesized and evaluated for their cytotoxic activities against four human cancer cell lines and inhibitory activities against five type culture strains in vitro. Some of synthetic pyrimidine-benzimidazol combinations showed good inhibitory activities against Stenotrophomonas maltophilia, especially compounds 7b and 7c. Compounds 7a and 7d exhibited enhanced activities against MGC-803 in vitro, when compared to 5-Fu. PMID:24798098

Chen, Peng-Ju; Yang, Ang; Gu, Yi-Fei; Zhang, Xiao-Song; Shao, Kun-Peng; Xue, Deng-Qi; He, Peng; Jiang, Teng-Fei; Zhang, Qiu-Rong; Liu, Hong-Min

2014-06-15

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

The effect of recombinant tissue plasminogen activator on MMP-2 and MMP-9 activities in vitro.  

PubMed

One of the most significant side effects during recombinant tissue plasminogen activator (rtPA) for acute stroke treatment is intracranial bleeding. Gelatinases [matrix metalloproteinase (MMP)-2 and MMP-9] are one of the agents involved in the blood-brain barrier destruction resulting in secondary bleeding into the ischemic area during stroke. Previous papers revealed that patients with high baseline MMP-9 serum level have higher risk of intracranial bleeding after thrombolytic therapy. Our objective was to evaluate rtPA influence on serum MMP-2 and MMP-9 activities in vitro. Nine sera obtained from healthy donors were applied for experiment. The commercially available rtPA (Actylise) were diluted with included solvent and additionally with phosphate-buffered saline (PBS) to get concentrations: 2, 4, 8, and 16 ?g/ml. Next, 100 ?l of serum was mixed with equal proportion with different concentrations of rtPA to obtain final rtPA concentrations: 1, 2, 4, and 8 ?g/ml. The sera together with rtPA were incubated for 1 or 2 hours at 37°C. The activity of gelatinases was estimated with zymography. The activities of MMP-9 (92 kDa) and MMP-2 (72 kDa) were increased by incubation with rtPA in a dose-dependent manner. Simultaneously, the activity of band at 200 kDa (MMP-9/MMP-9 homodimer) was decreased. The activity of gelatinases incubated for 2 hours was elevated in comparison with 1-hour incubation; however, the increase was observed even for sample without rtPA. In conclusion, this study showed that rtPA can increase the biological activity of MMP-2 and MMP-9 on posttranslational level. PMID:24963695

Golab, Piotr; Kielbus, Michal; Bielewicz, Joanna; Kurzepa, Jacek

2015-01-01

92

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

93

Potassium Humate Inhibits Complement Activation and the Production of Inflammatory Cytokines In Vitro  

Microsoft Academic Search

The effects of brown coal derived potassium humate on lymphocyte proliferation, cytokine production and complement activation\\u000a were investigated in vitro. Potassium humate increased lymphocyte proliferation of phytohaemaglutinin A (PHA) and pokeweed mitogen (PWM) stimulated\\u000a mononuclear lymphocytes (MNL) in vitro from concentrations of 20 to 80 ?g\\/ml, in a dose dependant manner. On the other hand potassium humate, at 40 ?g\\/ml, significantly\\u000a inhibited

Constance E. Jansen van Rensburg; Pieter J. Naude

2009-01-01

94

In vitro biological activity of decoction of Joshanda.  

PubMed

Joshanda is a polyherbal product, commonly practicing in inflammation of upper respiratory tract as tea. The present study was conducted to find out its antimicrobial, phytotoxic, leishmanicidal and cytotoxic activities. The decoction of the product showed profound activity against Gram positive tested pathogens especially S. aureus 36.5 mm zone of inhibition at 8.0 ?g/ml. However, it was inactive against C. albicans. Closed correlation was observed between two methods in terms of results. It had potent phytotoxic activity (75%). However, it was devoid of any activity leishmanicidal and cytotoxic activity. Phytochemical studies of Joshanda showed the presence of various pharmacologically active groups. PMID:24577908

Abdullah; Inayat, Humaira; Khan, Haroon; Khan, Lajber; Khan, Mohammad Iqbal; Hassan, Sohail; Khan, Murad Ali

2014-03-01

95

Macrophage activation and leishmanicidal activity by galactomannan and its oxovanadium (IV/V) complex in vitro.  

PubMed

Compounds that activate macrophage antimicrobial activity are potential targets for treatment of leishmaniasis. The present study investigated the in vitro immunomodulatory effects of a galactomannan (GALMAN-A) isolated from seeds of Mimosa scabrella and its oxovanadium (IV/V) complex (GALMAN-A:VO(2+)/VO(3+)) on macrophage activity. GALMAN-A increased nitric oxide levels by ~33% at a concentration of 250?g/ml, while GALMAN-A:VO(2+)/VO(3+) decreased nitric oxide levels by ~33% at a concentration of 50?g/ml. Furthermore, GALMAN-A increased interleukin-1 beta (IL-1?) and interleukin-6 (IL-6) levels by 5.5 and 2.3 times, respectively, at a concentration of 25?g/ml; at the same concentration, GALMAN-A:VO(2+)/VO(3+) promoted an increase in IL-1? and IL-6 production by 8 and 5.5 times, respectively. However, neither GALMAN-A nor GALMAN-A:VO(2+)/VO(3+) affected tumor necrosis factor alpha (TNF-?) or interleukin-10 (IL-10) levels. Importantly, both GALMAN-A and GALMAN-A:VO(2+)/VO(3+) exhibited leishmanicidal activity on amastigotes of Leishmania (L.) amazonensis, reaching ~60% activity at concentrations of 100 and 25?g/ml, respectively. These results indicate that GALMAN-A is three times more potent and its oxovanadium complex is twelve times more potent than Glucantime (300?g/ml), which is the drug of choice in leishmaniasis treatment. The IC50 value for GALMAN-A:VO(2+)/VO(3+) was 74.4?g/ml (0.58?g/ml of vanadium). Thus, the significant activation of macrophages and the noted leishmanicidal effect demonstrate the need for further studies to clarify the mechanisms of action of these compounds. PMID:24169303

Adriazola, Izabela Ono; Evangelista do Amaral, Alex; Amorim, Juliana Carolina; Correia, Beatriz Lourenço; Petkowicz, Carmen Lúcia Oliveira; Mercę, Ana Lucia Ramalho; Noleto, Guilhermina Rodrigues

2014-03-01

96

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

97

Characterisation of the in vitro activity of the depsipeptide histone deacetylase inhibitor spiruchostatin A  

Microsoft Academic Search

We recently completed the total synthesis of spiruchostatin A, a depsipeptide natural product with close structural similarities to FK228, a histone deacetylase (HDAC) inhibitor (HDI) currently being evaluated in clinical trials for cancer. Here we report a detailed characterisation of the in vitro activity of spiruchostatin A. Spiruchostatin A was a potent (sub-nM) inhibitor of class I HDAC activity in

Simon J. Crabb; Melanie Howell; Helen Rogers; Muhammad Ishfaq; Alexander Yurek-George; Krystle Carey; Becky M. Pickering; Phil East; Richard Mitter; Satoko Maeda; Peter W. M. Johnson; Paul Townsend; Kazuo Shin-ya; Minoru Yoshida; A. Ganesan; Graham Packham

2008-01-01

98

Apparent inhibition of superoxide dismutase activity in vitro by diesel exhaust particles  

Microsoft Academic Search

The inhibitory effects of diesel exhaust particles (DEP) on superoxide dismutase (SOD) activity were examined in vitro because intratracheal administration of DEP to mice resulted in a suppression of the pulmonary enzyme activity (Sagai et al., Free Radic. Biol. Med. 14:37–47; 1993). Superoxide production, based on the reduction of cytochrome c, was suppressed considerably by the soluble fraction of mouse

Yoshito Kumagai; Junsei Taira; Masaru Sagai

1995-01-01

99

In Vitro and In Vivo Activities of Fluoroquinolones against Aeromonas hydrophila  

Microsoft Academic Search

Aeromonas hydrophila, an uncommon human pathogen, can cause invasive infections in immunocompro- mised individuals. As the fluoroquinolones have been shown to be active in vitro against mesophilic aero- monads and clinical experience with the use of fluoroquinolones to treat aeromonads infections is limited, the antimicrobial activities of five selected drugs (ciprofloxacin, gatifloxacin, levofloxacin, lomefloxacin, and moxi- floxacin) against A. hydrophila

Wen-Chien Ko; Shyh-Ren Chiang; Hsin-Chun Lee; Hung-Jen Tang; Yin-Yi Wang; Yin-Ching Chuang

2003-01-01

100

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

101

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...

102

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...

103

A Study on the In Vitro Antioxidant Activity of Juniper (Juniperus communis L.) Fruit Extracts  

Microsoft Academic Search

This study aimed at evaluating the in vitro antioxidant activity of water and ethanol extracts of juniper (Juniperus communis L., Family Cupressaceae) fruit. The antioxidant properties of both Juniper extracts were studied using different antioxidant assays, including reducing power, free radical scavenging, superoxide anion radical scavenging, hydrogen peroxide scavenging, and metal chelating activities. Both the water and the ethanol extracts

Mahfuz Elmasta?; ?lhami Gülçin; ?ükrü Beydemir; Ö. ?rfan Küfrevio?lu

2006-01-01

104

Antioxidative activity of persimmon and grape seed extract: in vitro and in vivo  

Microsoft Academic Search

We determined in vitro radical scavenging activity of persimmon seed extract (PSE) and grape seed extract (GSE), and quantified total tannin concentrations of each extract. It has been found that both PSE and GSE have radical scavenging activities, and total tannin concentration of PSE was significantly higher than GSE (p < 0.05). In order to investigate the protective effect on

Hong Seok Ahn; Tae Il Jeon; Joo Yong Lee; Seong Gu Hwang; Yoongho Lim; Dong Ki Park

2002-01-01

105

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

106

In Vitro Activities of Strychnos Alkaloids and Extracts against Plasmodium falciparum  

PubMed Central

The in vitro antimalarial activities of 46 alkaloids and extracts from Strychnos species were evaluated. Two types of quasidimeric alkaloids exhibit high and selective activities against Plasmodium. Strychnopentamine and isostrychnopentamine were active against chloroquine-sensitive and -resistant strains (50% inhibitory concentration [IC50] ? 0.15 ?M), while dihydrousambarensine exhibited a 30-fold higher activity against the chloroquine-resistant strain (IC50 = 0.03 ?M) than it did against the chloroquine-sensitive strain. PMID:10471592

Frederich, Michel; Hayette, Marie-Pierre; Tits, Monique; De Mol, Patrick; Angenot, Luc

1999-01-01

107

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

108

In vitro antioxidant activity of feruloyl arabinose isolated from maize bran by acid hydrolysis.  

PubMed

In this study feruloylated oligosaccharides (FOs) was released from maize bran by hydrochloric acid hydrolysis, and feruloyl arabinose (F-Ara) was obtained by D301 macroporous resin chromatography followed by polyamide resin purification from FOs. After structural identification, the antioxidant activity of F-Ara was evaluated in vitro by DPPH and superoxide radical scavenging activity assay, reducing power assay and chelating activity assay. The results show that F-Ara exhibited antioxidant activity in vitro when compared to standard antioxidants such as butylated hydroxyanisole, ferulic acid and L-ascorbic acid. The antioxidant activity depends on the concentration and increases with increasing dose of sample. The present study suggests that F-Ara possesses promising future for its strong reducing power, chelating activity and free radical-scavenging activity. Therefore, it can be a natural and efficient antioxidant used in food, medicine and cosmetic. PMID:24966430

Lin, Qiling; Ou, Shiyi; Wen, Qibiao

2014-07-01

109

Antimicrobial activity of extracts from in vivo and in vitro propagated Lamium album L. plants.  

PubMed

The antimicrobial activity of 18 different extracts from in vivo and in vitro grown L. album L. plants was evaluated against clinical bacteria and yeasts using the well diffusion method. All the used extracts demonstrated antibacterial activity, whereas only the water extracts from leaves (in vivo) possessed antifungal activity against Candida albicans NBIMCC 72 and Candida glabrata NBIMCC 8673 (14 and 20 mm diameter of inhibition zones and MIC 10 mg/ml, respectively). The methanol and ethanol extracts obtained from the in vitro propagated plants had a broader spectrum of antibacterial activity than those from in vivo plants, while the opposite tendency was observed for the chloroform extracts. All tested flower extracts possessed antimicrobial activity. The chloroform extract from in vivo flowers demonstrated the highest activity against E. faecalis NBIMCC 3915, S. aureus NBIMCC 3703, P. hauseri NBIMCC 1339 and P. aeruginosa NBIMCC 3700 (22 mm, 13 mm, 11 mm, 23 mm zone diameter of inhibition and MIC 0.313 mg/ml, respectively). The water extracts from leaves (both in vivo and in vitro) possessed higher antibacterial activity than extract from flowers. The obtained results showed that both in vivo and in vitro propagated L. album L. could be used as a source of antibacterial substances. PMID:24311888

Chipeva, Valentina Aleksandrova; Petrova, Detelina Christova; Geneva, Milena Evgenieva; Dimitrova, Milena Angelova; Moncheva, Penka Angelova; Kapchina-Toteva, Veneta Michova

2013-01-01

110

Temporal changes in intestinal Na+ -ATPase activity and in vitro  

E-print Network

, may contribute signifi- cantly to seawater adaptation. In brown trout (Salmo trutta), the activity activity and fluid absorption across this region of the gut in euryhaline rainbow trout (Salmo gairdneri) and Atlantic salmon (Salmo salar; Madsen, 1990; Cornell et al., 1994; Specker et al., 1994). Furthermore

Young, Graham

111

Developmental Changes in the in Vitro Activated Regenerative Activity of Primitive Mammary Epithelial Cells  

PubMed Central

Many normal adult tissues contain rare stem cells with extensive self-maintaining regenerative potential. During development, the stem cells of the hematopoietic and neural systems undergo intrinsically specified changes in their self-renewal potential. In the mouse, mammary stem cells with transplantable regenerative activity are first detectable a few days before birth. They share some phenotypic properties with their adult counterparts but are enriched in a subpopulation that displays a distinct gene expression profile. Here we show that fetal mammary epithelial cells have a greater direct and inducible growth potential than their adult counterparts. The latter feature is revealed in a novel culture system that enables large numbers of in vitro clonogenic progenitors as well as mammary stem cells with serially transplantable activity to be produced within 7 days from single fetal or adult input cells. We further show that these responses are highly dependent on novel factors produced by fibroblasts. These findings provide new avenues for elucidating mechanisms that regulate normal mammary epithelial stem cell properties at the single-cell level, how these change during development, and how their perturbation may contribute to transformation. PMID:23966837

Makarem, Maisam; Kannan, Nagarajan; Nguyen, Long V.; Knapp, David J. H. F.; Balani, Sneha; Prater, Michael D.; Stingl, John; Raouf, Afshin; Nemirovsky, Oksana; Eirew, Peter; Eaves, Connie J.

2013-01-01

112

Bioprotective properties of Dragon's blood resin: In vitro evaluation of antioxidant activity and antimicrobial activity  

PubMed Central

Background Food preservation is basically done to preserve the natural characteristics and appearance of the food and to increase the shelf life of food. Food preservatives in use are natural, chemical and artificial. Keeping in mind the adverse effects of synthetic food preservatives, there is a need to identify natural food preservatives. The aims of this study were to evaluate in vitro antioxidant and antimicrobial activities of Dragon's blood resin obtained from Dracaena cinnabari Balf f., with a view to develop safer food preservatives. Methods In this study, three solvents of varying polarity were used to extract and separate the medium and high polarity compounds from the non-polar compounds of the Dragon's blood resin. The extracts were evaluated for their antimicrobial activity against the food borne pathogens. The antioxidant activities of the extracts were assessed using DPPH and ABTS radical scavenging, FRAP, metal chelating and reducing power assays. Total phenolics, flavonoids and flavonols of extracts were also estimated using the standard methods. Results Phytochemical analysis of extracts revealed high phenolic content in CH2Cl2 extract of resin. Free radical scavenging of CH2Cl2 extract was found to be highest which is in good correlation with its total phenolic content. All test microorganisms were also inhibited by CH2Cl2 extract. Conclusions Our result provide evidence that CH2Cl2 extract is a potential source of natural antioxidant compounds and exhibited good inhibitory activity against various food borne pathogens. Thus, CH2Cl2 extract of Dragon's blood resin could be considered as possible source of food preservative. PMID:21329518

2011-01-01

113

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

114

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

115

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

116

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

117

Activity of armillarisin B in vitro against plant pathogenic fungi.  

PubMed

The methanolic extract of the fruiting bodies of the mushroom Armillariella tabescens was found to show antifungal activity against Gibberella zeae. The active compound was isolated from the fruiting bodies of A. tabescens by bioassay-guided fractionation of the extract and identified as armillarisin B. Armillarisin B eventually corresponds to 2-hydroxy-2-phenylpropanediamide and its structure was confirmed on the basis of spectroscopic studies including 2D NMR experiments. PMID:20158147

Shen, Jin-Wen; Ma, Bing-Ji; Li, Wen; Yu, Hai-You; Wu, Ting-Ting; Ruan, Yuan

2009-01-01

118

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

119

How Much In Vitro Cholesterol Reducing Activity of Lactobacilli Predicts Their In Vivo Cholesterol Function?  

PubMed Central

Background: Based on literature, in vitro cholesterol removal of lactic acid bacteria has been accounted for their in vivo cholesterol reduction. But recently it has been proposed that such in vitro characteristic may not be directly relevant to their in vivo activity. The objective of this study was to find how much in vitro cholesterol reducing potential of Lactobacillus plantarum A7 (LA7), a native strain isolated from an infant fecal flora, reflects its in vivo efficiency. LA7 previously showed serum cholesterol reducing capability in mice subjected to fatty diet. Here, we investigate whether the given strain is capable of in vitro cholesterol assimilation or consumption. Method: LA7 was cultured in whole milk and de-Man–Rogosa–Sharpe (MRS) added with water-soluble cholesterol. Colorimetric method was adopted for cholesterol determination in both cultured media during incubation period. Results: No cholesterol assimilation was detected by growth and incubation of the active culture in either of the medium. Thus, in vivo cholesterol function of LA7 was not caused by cholesterol consumption. A comprehensive review of literature on the related studies also showed that there are other documented studies which evidenced the uncertainty of the direct relation between in vitro and in vivo studies. Conclusion: Cholesterol removal from the cultured media may not be considered as an appropriate integral index for selection of Lactobacillus strains with cholesterol-lowering activity. PMID:23671771

Madani, Golnoush; Mirlohi, Maryam; Yahay, Mahmoud; Hassanzadeh, Akbar

2013-01-01

120

In Vitro Activity of Telavancin against Resistant Gram-Positive Bacteria?  

PubMed Central

The in vitro activity of telavancin was tested against 743 predominantly antimicrobial-resistant, gram-positive isolates. Telavancin was highly active against methicillin-resistant staphylococci (MIC90, 0.5 to 1 ?g/ml), streptococci (all MICs, ?0.12 ?g/ml), and VanB-type enterococci (all MICs, ?2 ?g/ml). Time-kill studies demonstrated the potent bactericidal activity of telavancin. PMID:18443122

Krause, Kevin M.; Renelli, Marika; Difuntorum, Stacey; Wu, Terry X.; Debabov, Dmitri V.; Benton, Bret M.

2008-01-01

121

In Vitro Activity of BAY 12-8039, a New Fluoroquinolone  

Microsoft Academic Search

The in vitro activity of BAY 12-8039, a newfluoroquinolone, was studied in comparison with those of cipro- floxacin, trovafloxacin (CP 99,219), cefpodoxime, and amoxicillin-clavulanate against gram-negative, gram- positive, and anaerobic bacteria. Its activity against mycobacteria and chlamydia was also investigated. BAY 12-8039 was active against members of the familyEnterobacteriaceae(MIC at which 90% of strains tested were inhibited (MIC90s) <1 mg\\/ml,

J. M. WOODCOCK; J. M. ANDREWS; F. J. BOSWELL; N. P. BRENWALD; ANDR. WISE

1997-01-01

122

Antioxidative and in vitro antiproliferative activity of Arctium lappa root extracts  

Microsoft Academic Search

Background  \\u000a Arctium lappa, known as burdock, is widely used in popular medicine for hypertension, gout, hepatitis and other inflammatory disorders.\\u000a Pharmacological studies indicated that burdock roots have hepatoprotective, anti-inflammatory, free radical scavenging and\\u000a antiproliferative activities. The aim of this study was to evaluate total phenolic content, radical scavenging activity by\\u000a DPPH and in vitro antiproliferative activity of different A. lappa

Fabricia S Predes; Ana LTG Ruiz; Joăo E Carvalho; Mary A Foglio; Heidi Dolder

2011-01-01

123

A PRELIMINARY STUDY ON THE IN VITRO ANTIOXIDANT ACTIVITY OF THE STEMS OF OPUNTIA VULGARIS  

PubMed Central

The in vitro antioxidant activity of stems of Opuntia vulgaris Mill had been investigated by estimating degree of non-enzymatic haemoglobin glycosylation measured colorimetrically at 520 urn. It was found that benzene and chloroform extract of O. vulgaris had better antioxidant activity than petroleum ether, ethyl acetate, ethanol and aqueous extract. The antioxidant activity of the extracts was concentration dependent and comparable to that of D-?- tocopherol (vitamin E) and ascorbic acid (vitamin C), standard antioxidant compounds used. PMID:22247855

Pal, Dilipkumar; Mitra, Sanmoy

2010-01-01

124

In vitro activity of SK&F 104662, a new glycopeptide antibiotic.  

PubMed Central

The in vitro activity of SK&F 104662, a new glycopeptide antibiotic, against gram-positive bacteria was evaluated. Activity was comparable to those of teicoplanin and vancomycin against most organisms. SK&F 104662 inhibited diphtheroids at concentrations of less than or equal to 0.5 microgram/ml. Addition of human serum to the test medium lowered the inhibitory activity of this glycopeptide against some organisms by as much as eightfold. PMID:2548444

Yao, J D; Eliopoulos, G M; Moellering, R C

1989-01-01

125

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

PubMed

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

1992-05-01

126

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

127

Composition and in vitro antimicrobial activity of Populus buds and poplar-type propolis  

Microsoft Academic Search

The antibacterial activity of propolis has been widely investigated. Since reports dealing with antimicrobial activity of\\u000a the origin of propolis are not available, this study was carried out aiming to analyse the in vitro antimicrobial activity\\u000a of the methanol extracts of poplar type propolis and Populus (Populus nigra, P. alba, P. tremuloides) buds as its sources against standard strains of a panel of

Gülhan Vardar-Ünlü; Sibel Silici; Mehmet Ünlü

2008-01-01

128

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

129

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

130

In vitro study of the proteolytic activity of rumen anaerobic fungi.  

PubMed

Proteolytic, aminopeptidase, endopeptidase and carboxypeptidase activities of seven strains of rumen anaerobic fungi, selected to represent the fungal population commonly found in the rumen, were investigated in vitro. Whatever the nitrogen source included in the culture medium, a proteolytic activity against the 14C-labelled casein was detected in only one fungal strain. This strain belonged to the genus Piromyces. The activity was extracellular and was found both in the culture supernatant and bound to the mycelium. No carboxypeptidase activity was detected in the seven strains. In contrast, all the strains exhibited aminopeptidase activity. Two strains had an endopeptidase activity. PMID:8319894

Michel, V; Fonty, G; Millet, L; Bonnemoy, F; Gouet, P

1993-06-01

131

In vitro and in vivo antioxidant activity of exopolysaccharide fractions from Bifidobacterium animalis RH.  

PubMed

The aim of the study was to purify the exopolysaccharides (EPS) produced from Bifidobacterium animalis RH, which was isolated from the feces of Bama centenarians in Guangxi of China, and evaluate their antioxidant activities in vitro and in vivo. 2 fractions, a neutral EPS fraction (EPSa) and an acidic EPS fraction (EPSb), were obtained and compared for antioxidative activity. In vitro, they both showed remarkable inhibition effect on lipid peroxidation and strong DPPH radical scavenging activity, hydroxyl radical scavenging activity, superoxide radical scavenging activity, in which the last two were measured by the electron spin resonance (ESR). In vivo, EPSa and EPSb were orally administrated for 30 days in a d-galactose induced aged mice model. As results, they both could significantly increase the activities of SOD, CAT and total antioxidant capacity (TAOC) in serums and glutathione GST in livers. They also could inhibit significantly the formation of MDA in serums and livers, and reduce the activity of MAO and lipofuscin accumulation in mice brain. Moreover, EPSb exhibited much higher antioxidant activities than EPSa in vitro and in vivo. The results suggested that EPS fractions of Bifidobacterium animalis RH had direct and potent antioxidant activities. PMID:21875680

Xu, Rihua; Shang, Nan; Li, Pinglan

2011-10-01

132

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

133

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

134

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

135

Evaluation of the anticryptococcal activity of the antibiotic polymyxin B in vitro and in vivo.  

PubMed

Polymyxin B (PMB), a cationic lipid oligopeptide used to treat Gram-negative bacterial infections, was previously identified to possess broad-spectrum antifungal activity and to work synergistically with azole antifungals in vitro. Here we evaluated the efficacy of PMB against Cryptococcus neoformans in vitro and in vivo and explored the mechanism of the hypersensitivity of this fungus to this compound. Using comparative time-course assays, PMB was found to kill both proliferative and quiescent cryptococcal cells in vitro. Presence of the polysaccharide capsule, a characteristic feature of Cryptococcus, significantly enhances the susceptibility of this fungus to the fungicidal activity of PMB. Furthermore, PMB is able to reduce the tissue fungal burden both in intravenous and inhalation models of murine cryptococcosis at a level comparable with the commonly used antifungal fluconazole. These findings suggest that PMB could provide an additional option for treatment against systemic cryptococcosis. PMID:23313397

Zhai, Bing; Lin, Xiaorong

2013-03-01

136

Antifungal activity of sertaconazole in vitro against clinical isolates of Candida spp..  

PubMed

Sertaconazole is a new azolic derivative containing a benzo(b)-thiophene group, for topical use. It showed in vitro fungistatic and fungicidal activity against yeasts, dermatophytes, opportunistic filamentous fungi and Gram-positive bacteria. In this study, we have evaluated the activity of sertaconazole in vitro against 215 strains of Candida spp. Fluconazole and ketoconazole were used throughout as reference compounds. The minimum inhibitory concentration (MIC) was determined in Casitone medium and the breakpoint was obtained spectrophotometrically and visually. Visual reading of MICs correlated with the spectrophotometric determination, the values of MIC50 and MIC90 showed no difference (+/- 1 dilution) in any of the species tested (range 0.1-16 mg/l). These results show that sertaconazole is an excellent antifungal agent and fungicide in vitro against various species of Candida. PMID:8697886

Martin-Mazuelos, E; Aller, A I; Morilla, D; Montero, O

1996-01-01

137

Inhibition of catalase activity in vitro by diesel exhaust particles  

SciTech Connect

The effect of diesel exhaust particles (DEP) on the activity of catalase, an intracellular anti-oxidant, was investigated because H{sub 2}O{sub 2} 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 by DEP was observed only in the presence of anions such as Cl{sup {minus}}, Br{sup {minus}}, or thiocyanate. Other anions, such as CH{sub 3}COO{sup {minus}} or SO{sub 4}{sup {minus}}, and cations such as K{sup +}, Na{sup +}, Mg{sup 2+}, or Fe{sup 2+}, did not affect the activity of catalase, even in the presence of DEP extract. Catalase from guinea pig alveolar cells and catalase from red blood cells were also inhibited by DEP extracts, as was catalase from bovine liver. These results suggest that DEP taken up in the lung and located on alveolar spaces might cause cell injury by inhibiting the activity of catalase in epithelial lining fluid, enhancing the toxicity of H{sub 2}O{sub 2} generated from cells in addition to that of O{sub 2}{sup {minus}} generated by the chemical reaction of DEP with oxygen. 10 refs., 6 figs.

Mori, Yoki; Murakami, Sumika; Sagae, Toshiyuki [Health Sciences Univ. of Hokkaido (Japan)] [and others] [Health Sciences Univ. of Hokkaido (Japan); and others

1996-02-09

138

Phasic Vagal Sensory Feedback Transforms Respiratory Neuron Activity In Vitro  

Microsoft Academic Search

The isolated neonatal rat medulla generates respiratory-related rhythms recorded from cervical spinal cord ventral roots. When lungs and their vagal innervation are retained, respiratory ac- tivity is modulated by lung mechanoreceptor feedback: tran- sient lung inflation triggered off inspiratory onset (phasic infla- tion) shortens inspiration and increases respiratory frequency. In this study, the activity of six respiratory neuron classes before

Nicholas M. Mellen; Jack L. Feldman

2001-01-01

139

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

140

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

141

Pseudorabies Virus Infection Alters Neuronal Activity and Connectivity In Vitro  

E-print Network

-herpesviruses, including human herpes simplex virus 1 & 2, varicella zoster virus and the swine pseudorabies virus (PRV on motor and sensory neuron activity. For example, herpes simplex virus type 1 causes herpes labialis with the sensations of numbness and tingling [1]; herpes simplex virus type 2 causes genital herpes

Tank, David

142

Neuronal Activity Patterns During Hippocampal Network Oscillations In Vitro  

E-print Network

Kopell, and Tamar Dugladze Overview Neurons form transient, functionally specialized assemblies ripples in CA1 area during slow-wave sleep. Upper traces, wide band recording, lower traces, band bath (40 trace, wide band recording, lower trace, ripple band-pass (140­320 Hz) filtered activity. Panels

Kopell, Nancy

143

In vitro antimicrobial and cytotoxic activities of ferrocene derivative compounds.  

PubMed

The aim of the present study was to investigate the biocidal activity of four new ferrocene derivative based coordination complexes, [1,2,3-trithia-/3/-ferrocenophane, C1]; [disodium-1,1'-ferrocenedithiolate, C2]; [1,1'-(ferrocene-1,1'-diyl)-diethanol, C3]; [ferrocenyl(ethyl-phenyl)-methanol, C4]; against microbes (bacteria and fungi) and brine shrimp (Artemia salina Lech.) nauplii. C2 showed modest antibacterial activity at the concentration of 200 microg disc(-1) and gave its Minimum Inhibitory Concentration values at 32-64 microg mL(-1) against the tested bacteria. These complexes gave comparatively better antibacterial activity against the Gram-positives than the Gram-negatives. C3, C1 and C4 showed moderate antifungal activity at concentration of 200 microg disc(-1). Brine shrimp eggs were hatched in artificial sea water and exposed to the complexes. Median lethal concentration (LC50) values were calculated. Both complexes showed toxicity against brine shrimp but complex C3 explored its potent cytotoxicity having LC50 values at 6.031 microg mL(-1) (ppm). PMID:19070108

Al-Bari, M Abdul Alim; Hossen, M Faruk; Khan, Alam; Islam, M Robiul; Kudrat-E-Zahan, M; Mosaddik, M Ashik; Zakaria, Choudhury M; Islam, M Anwar Ul

2007-08-01

144

In vitro activity of sertaconazole against Malassezia furfur and pachydermatis in different culture media.  

PubMed

The activity of sertaconazole against Malassezia furfur and pachydermatis was tested in different culture media in order to elucidate the factors that can influence its activity. The addition to the culture media of lipids, which are necessary for M. furfur to grow, was found to decrease the activity of this antifungal to a great extent. Since the aim of in vitro drug testing is to provide representative data of its activity which must be indicative for its clinical efficacy, and in view of the good clinical response of M. furfur infection to sertaconazole, it is concluded that the activity of this antifungal against M. furfur cannot be determined by the in vitro data provided by conventional methods due to such influential factors. PMID:9789868

Palacin, C; Tarragó, C; Ortiz, J A

1998-01-01

145

In vitro antimicrobial activity of peroxide-based bleaching agents.  

PubMed

Antibacterial activity of 4 commercial bleaching agents (Day White, Colgate Platinum, Whiteness 10% and 16%) on 6 oral pathogens (Streptococcus mutans, Streptococcus sobrinus, Streptococcus sanguinis, Candida albicans, Lactobacillus casei, and Lactobacillus acidophilus) and Staphylococcus aureus were evaluated. A chlorhexidine solution was used as a positive control, while distilled water was the negative control. Bleaching agents and control materials were inserted in sterilized stainless-steel cylinders that were positioned under inoculated agar plate (n = 4). After incubation according to the appropriate period of time for each microorganism, the inhibition zones were measured. Data were analyzed by 2-way analysis of variance and Tukey test (a = 0.05). All bleaching agents and the chlorhexidine solution produced antibacterial inhibition zones. Antimicrobial activity was dependent on peroxide-based bleaching agents. For most microorganisms evaluated, bleaching agents produced inhibition zones similar to or larger than that observed for chlorhexidine. C albicans, L casei, and L acidophilus were the most resistant microorganisms. PMID:17625621

Napimoga, Marcelo Henrique; de Oliveira, Rogério; Reis, André Figueiredo; Gonçalves, Reginaldo Bruno; Giannini, Marcelo

2007-06-01

146

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

147

In vitro antimicrobial activity of Achyranthes coynei Sant.  

PubMed Central

Objective To validate the traditional use of Achyranthes coynei (A. coynei) Sant. as an antimicrobial in treatment of various infectious diseases. Methods Leaf extracts of A. coynei obtained through successive solvent extraction using petroleum ether, dichrloromethane, chloroform and methanol were used to screen the antimicrobial activity on five Gram positive, five Gram negative bacteria and two fungi. Minimum inhibitory concentration (MIC) was determined by two fold tube-dilution method. Results Methanolic leaf extract was more effective than other three extracts on the tested bacteria. Methanolic extract was efficient on Staphylococcus epidermis, Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa with MIC values (0.62±0.00) mg/mL. The fungal organisms were less susceptible against extracts tested. Conclusions These results support the traditional use of leaf extracts of A. coynei as they have antimicrobial potential. Further studies are needed for establishing safety, toxicity and pharmacological activity with phytochemical investigation.

Ankad, Gireesh; Upadhya, Vinayak; Pai, Sandeep R.; Hegde, Harsha V.; Roy, Subarna

2013-01-01

148

In vitro antibacterial activity of some plant essential oils  

Microsoft Academic Search

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

Seenivasan Prabuseenivasan; Manickkam Jayakumar; Savarimuthu Ignacimuthu

2006-01-01

149

Anti-invasive activity of alkaloids and polyphenolics in vitro  

Microsoft Academic Search

Invasiveness, the ability of certain tumour cells to migrate beyond their natural tissue boundaries, often leads to metastasis, and usually determines the fatal outcome of cancer. The need for anti-invasive agents has led us to search for possibly active compounds among alkaloids and polyphenolics. One hundred compounds were screened in an assay based on the confrontation of invasive human MCF-7\\/6

Virinder S. Parmar; Marc E. Bracke; Jan Philippe; Jesper Wengel; Subhash C. Jain; Carl E. Olsen; Kirpal S. Bisht; Nawal K. Sharma; Andy Courtens; Sunil K. Sharma; Krist'l Vennekens; Veerle Van Marck; Sanjay K. Singh; Naresh Kumar; Ajay Kumar; Sanjay Malhotra; Rajesh Kumar; Vivek K. Rajwanshi; Rajni Jain; Marc M. Mareel

1997-01-01

150

In vitro activity of eugenol against Candida albicans biofilms  

Microsoft Academic Search

Most manifestations of candidiasis are associated with biofilm formation occurring on the surfaces of host tissues and medical\\u000a devices. Candida albicans is the most frequently isolated causative pathogen of candidiasis, and the biofilms display significantly increased levels\\u000a of resistance to the conventional antifungal agents. Eugenol, the major phenolic component of clove essential oil, possesses\\u000a potent antifungal activity. The aim of

Miao He; Minquan Du; Mingwen Fan; Zhuan Bian

2007-01-01

151

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

2014-12-01

152

Hepatitis C Virus NS3 Helicase Forms Oligomeric Structures That Exhibit Optimal DNA Unwinding Activity in Vitro*S?  

PubMed Central

HCV NS3 helicase exhibits activity toward DNA and RNA substrates. The DNA helicase activity of NS3 has been proposed to be optimal when multiple NS3 molecules are bound to the same substrate molecule. NS3 catalyzes little or no measurable DNA unwinding under single cycle conditions in which the concentration of substrate exceeds the concentration of enzyme by 5-fold. However, when NS3 (100 nm) is equimolar with the substrate, a small burst amplitude of ?8 nm is observed. The burst amplitude increases as the enzyme concentration increases, consistent with the idea that multiple molecules are needed for optimal unwinding. Protein-protein interactions may facilitate optimal activity, so the oligomeric properties of the enzyme were investigated. Chemical cross-linking indicates that full-length NS3 forms higher order oligomers much more readily than the NS3 helicase domain. Dynamic light scattering indicates that full-length NS3 exists as an oligomer, whereas NS3 helicase domain exists in a monomeric form in solution. Size exclusion chromatography also indicates that full-length NS3 behaves as an oligomer in solution, whereas the NS3 helicase domain behaves as a monomer. When NS3 was passed through a small pore filter capable of removing protein aggregates, greater than 95% of the protein and the DNA unwinding activity was removed from solution. In contrast, only ?10% of NS3 helicase domain and ?20% of the associated DNA unwinding activity was removed from solution after passage through the small pore filter. The results indicate that the optimally active form of full-length NS3 is part of an oligomeric species in vitro. PMID:18283103

Sikora, Bartek; Chen, Yingfeng; Lichti, Cheryl F.; Harrison, Melody K.; Jennings, Thomas A.; Tang, Yong; Tackett, Alan J.; Jordan, John B.; Sakon, Joshua; Cameron, Craig E.; Raney, Kevin D.

2008-01-01

153

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...

154

“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

155

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

156

Effects of sucrose on photosynthesis and phosphoenolpyruvate carboxylase activity of in vitro cultured strawberry plantlets  

Microsoft Academic Search

Photosynthesis and phosphoenolpyruvate carboxylase activity were investigated in 5, 10 and 28 day-old micropropagated strawberry plantlets (Fragaria x ananassa Duch. cv Kent) rooted in vitro with different levels of sucrose (0, 1, 3 and 5%) on cellulose plugs (Sorbarods). The photosynthetic capability was influenced by the level of sucrose in the culture medium with the largest rates of photosynthesis corresponding

Chafik Hdider; Yves Desjardins

1994-01-01

157

Transport of Biologically Active Interferon-gamma Across Human Skin in Vitro  

Microsoft Academic Search

Purpose. Several studies have suggested epidermal uptake of cytokines, such as interferons, can be facilitated using topical liposomal formulations. We have evaluated the in vitro transport of biologically active recombinant human interferon-? (rhIFN-?) into and through split-thickness human skin to assess this possibility.

Sarah M. Short; Werner Rubas; Brian D. Paasch; Randall J. Mrsny

1995-01-01

158

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

159

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 ...

160

Effect of proton pump inhibitors on in vitro activity of tigecycline against several common clinical pathogens.  

PubMed

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

161

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

162

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

163

Changes in phenol content and peroxidase activity during in vitro organogenesis in Xanthosoma sagittifolium L  

Microsoft Academic Search

Direct plant regeneration, multiple shoot formation and callogenesis were induced from cocoyam shoot tips cultured in vitro. At different stages of culture, phenol content, peroxidase activity and acidic soluble isoperoxidase patterns were analysed in plantlets. Results showed that phenol content of plantlets cultured on auxin-free media decreased with time, while it increased in those cultured on media supplemented with an

Gabriel Kanmegne; N. Denis Omokolo

2003-01-01

164

Novel Bacterial Metabolite Merochlorin A Demonstrates in vitro Activity against Multi-Drug Resistant Methicillin-  

E-print Network

of California San Diego, La Jolla, California, United States of America, 3 School of Pharmacy and Pharmaceutical of America Abstract Background: We evaluated the in vitro activity of a merochlorin A, a novel compound for this compound may include evaluation for topical use, coating biomedical devices, or the pursuit of chemically

Nizet, Victor

165

In vitro activities of streptomycin and 11 oral antimicrobial agents against clinical isolates of Klebsiella rhinoscleromatis.  

PubMed Central

We tested in vitro the activities of streptomycin and tetracycline--antibiotics that have long been used to treat rhinoscleroma--as well as several newer oral agents by using 23 isolates of the causative organism Klebsiella rhinoscleromatis. All isolates were inhibited by clinically achievable concentrations of trimethoprim-sulfamethoxazole, amoxicillin-clavulanate, chloramphenicol, ciprofloxacin, cephalexin, cefuroxime, and cefpodoxime. PMID:1416867

Perkins, B A; Hamill, R J; Musher, D M; O'Hara, C

1992-01-01

166

In Vitro Activities of the New Antifungal Triazole SCH 56592 against Common and Emerging Yeast Pathogens  

Microsoft Academic Search

A broth microdilution method performed in accordance with the National Committee for Clinical Labora- tory Standards guidelines was used to compare the in vitro activity of the new antifungal triazole SCH 56592 (SCH) to that of fluconazole (FLC), itraconazole (ITC), and ketoconazole (KETO) against 257 clinical yeast isolates. They included 220 isolates belonging to 12 different species of Candida, 15

FRANCESCO BARCHIESI; DANIELA ARZENI; ANNETTE W. FOTHERGILL; LUIGI FALCONI DI FRANCESCO; FRANCESCA CASELLI; MICHAEL G. RINALDI; GIORGIO SCALISE

2000-01-01

167

In Vitro activity of cepfodoxime in comparison with other oral ?-lactam antibiotics  

Microsoft Academic Search

Summary The aim of our study was to re-evaluate thein vitro activity of cefpodoxime in comparison with other oral ß-lactam antibiotics against bacteria causing respiratory tract infections. The study drugs were cefpodoxime, cefaclor, cefixime, cefuroxime, cefetamet, cefprozil, and the combination of amoxicillin and clavulanic acid (= augmentin). In addition, cefotaxime as the standard agent of parenteral third generation cephalosporins was

F. H. Kayser

1994-01-01

168

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...

169

In vitro antifungal activity of essential oils obtained from officinal plants against dermatophytes.  

PubMed

Thirteen essential oils were isolated from officinal plants and tested in vitro against dermatophyte strains isolated from patients with dermatophytosis. Of the tested oils, those obtained from Cinnamomum zeylanicum, Ocimum gratissimum, Cymbopogon citratus, Eugenia uniflora and Alpinia speciosa were found to be the most active, inhibiting 80% of the dermatophyte strains tested and producing inhibition zones more than 10 mm in diameter. PMID:8015567

Lima, E O; Gompertz, O F; Giesbrecht, A M; Paulo, M Q

1993-01-01

170

Synthesis and in vitro antitumor activity of phthalimide-based polymers containing camptothecin  

E-print Network

Synthesis and in vitro antitumor activity of phthalimide-based polymers containing camptothecin 2004 Abstract To improve the therapeutic efficacy of 20(s)-camptothecin (CPT) polymeric drugs,2,3,6-tetrahydrophthalimidoacetamidoglycine camptothecin ester (ETPA-gly-CPT), was synthesized by linking its hydroxyl group

Theodorakis, Emmanuel

171

In Vitro and In Vivo Activities of LB 10827, a New Oral Cephalosporin, against Respiratory Pathogens  

Microsoft Academic Search

The in vitro antibacterial activities of LB 10827, a new oral cephalosporin, against common respiratory tract pathogens were compared with those of six b-lactams (cefdinir, cefuroxime, cefprozil, penicillin G, amoxicillin- clavulanate, and ampicillin), two quinolones (trovafloxacin and ciprofloxacin), and one macrolide (clarithro- mycin). The MIC of LB 10827 at which 90% of the penicillin-resistant strains of Streptococcus pneumoniae tested were

KYONG-SOOK PAEK; MU-YONG KIM; CHANG-SEOK LEE; HASIK YOUN

2000-01-01

172

In Vitro and In Vivo Activities of Nitazoxanide against Clostridium difficile  

Microsoft Academic Search

We have used the hamster model of antibiotic-induced Clostridium difficile intestinal disease to evaluate nitazoxanide (NTZ), a nitrothiazole benzamide antimicrobial agent. The following in vitro and in vivo activities of NTZ in the adult hamster were examined and compared to those of metronidazole and vancomycin: (i) MICs and minimum bactericidal concentrations (MBCs) against C. difficile, (ii) toxicity, (iii) ability to

CATHERINE S. MCVAY; RIAL D. ROLFE

2000-01-01

173

Effects of cadmium on osteoclast formation and activity in vitro  

SciTech Connect

Chronic exposure to cadmium has been linked to bone loss, low bone mass, and increased incidence of fracture. To determine if Cd could directly increase the formation of cells responsible for bone resorption, we cultured normal canine bone marrow cells containing the progenitor cells for osteoclasts. Cultures were evaluated for the number of multinucleate osteoclast-like cells (MNOCs) formed. Exposure to Cd (10-100 nM) increased the number of MNOCs formed over control values when cultured in the presence but not in the absence of a bone wafer. The MNOCs formed were functional, evidenced by pits excavated on the bone wafers included in the cultures. By 12 days, MNOCs formed in the presence of 50 nM Cd excavated significantly more pits and a greater pit area than did untreated MNOCs. By 14 days, the control values were similar to those of the Cd-exposed MNOCs, but pit formation was enhanced by Cd in that the ratio of pit complexes to single pits was increased twofold over that for untreated cultures. Mature osteoclasts, isolated from the long bones of rat neonates and cultured for 1-3 days on bone slices, provided a direct method to assess the effect of Cd on osteoclast activity. Exposure of osteoclast cultures to 100 nm Cd increased the number of nM osteoclasts present over that for untreated osteoclasts by a factor of 1.7 {+-} 0.1, the number of pits excavated by 2.8 {+-} 0.6, the area excavated by 3.2 {+-} 0.8, and the area excavated per osteoclast by 1.8 {+-} 0.4 (mean SE; n = six experiments). These data suggest that Cd accelerates the differentiation of new osteoclasts from their progenitor cells and activates or increases the activity of mature osteoclasts. 48 refs., 4 figs., 3 tabs.

Wilson, A.K.; Cerny, E.A.; Smith, B.D.; Wagh, A. [Argonne National Lab., IL (United States)] [and others] [Argonne National Lab., IL (United States); and others

1996-12-31

174

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

175

In vitro activity of Bay Y3118 against anaerobic bacteria.  

PubMed Central

The antimicrobial activity of a new quinolone, Bay Y3118, was determined against 326 strains of anaerobic bacteria and compared with the activities of ampicillin-sulbactam, cefotetan, clindamycin, imipenem, metronidazole, and sparfloxacin. The National Committee for Clinical Laboratory Standards-approved Wadsworth agar dilution technique with Brucella-laked blood agar was used throughout the study. Breakpoints used to determine the percent susceptible were 2 micrograms/ml for Bay Y3118 and sparfloxacin, 4 micrograms/ml for clindamycin, 8 micrograms/ml for imipenem, 16 micrograms/ml for metronidazole and ampicillin-sulbactam, and 32 micrograms/ml for cefotetan. Species tested included Bacteroides fragilis (57 strains), other B. fragilis group species (79 strains), Bacteroides gracilis (10 strains), other Bacteroides spp. (9 strains), Prevotella spp. (30 strains), Porphyromonas spp. (9 strains), Fusobacterium spp. (36 strains), Bilophila wadsworthia (14 strains), Clostridium spp. (36 strains), Peptostreptococcus spp. (20 strains), and gram-positive non-spore-forming rods (26 strains). Bay Y3118 inhibited all but 1 of 326 anaerobic bacteria tested at the breakpoint level or lower. PMID:8285647

Wexler, H M; Molitoris, E; Finegold, S M

1993-01-01

176

In vitro antioxidant and antitumor activities of different sulfated polysaccharides isolated from three algae.  

PubMed

Three sulfated polysaccharides(Ulva fasciata (UFP), Gloiopeltis furcata (GFP), Sargassum henslouianum (SHP))were isolated from three algae including green alga Ulva fasciata, red alga Gloiopeltis furcata and brown alga Sargassum henslouianum by ultrasonic extraction and radial flow chromatography. Their in vitro antioxidant and antitumor activities were investigated and compared. Among these three polysaccharides, UFP, with relatively lower sulfate content, exhibited excellent antioxidant activities in superoxide radical assay, ABTS assay and DPPH assay; however, it demonstrated the minimal inhibitory effects on growth of MKN45 gastric cancer cells and DLD intestinal cancer cells. SHP with the lowest sulfate content gained relatively lower radical scavenging rates but showed significantly higher antitumor activities. These results indicated that the in vitro antitumor and antioxidant activities of the three polysaccharides may be related to combined effects of sulfate content and uronic acid content. PMID:23994786

Shao, Ping; Chen, Xiaoxiao; Sun, Peilong

2013-11-01

177

In vitro activity of gemifloxacin (SB 265805) against anaerobes.  

PubMed

Gemifloxacin mesylate (SB 265805), a new fluoronaphthyridone, was tested against 359 recent clinical anaerobic isolates by the National Committee for Clinical Laboratory Standards reference agar dilution method with supplemented brucella blood agar and an inoculum of 10(5) CFU/spot. Comparative antimicrobials tested included trovafloxacin, levofloxacin, grepafloxacin, sparfloxacin, sitafloxacin (DU-6859a), penicillin G, amoxicillin clavulanate, imipenem, cefoxitin, clindamycin, and metronidazole. The MIC(50) and MIC(90) (MICs at which 50 and 90% of the isolates were inhibited) of gemifloxacin against various organisms (with the number of strains tested in parentheses) were as follows (in micrograms per milliliter): for Bacteroides fragilis (28), 0.5 and 2; for Bacteroides thetaiotaomicron (24), 1 and 16; for Bacteroides caccae (12), 1 and 16; for Bacteroides distasonis (12), 8 and >16; for Bacteroides ovatus (12), 4 and >16; for Bacteroides stercoris (12), 0.5 and 0.5; for Bacteroides uniformis (12), 1 and 4; for Bacteroides vulgatus (11), 4 and 4; for Clostridium clostridioforme (15), 0.5 and 0.5; for Clostridium difficile (15), 1 and >16; for Clostridium innocuum (13), 0.125 and 2; for Clostridium perfringens (13), 0.06 and 0.06; for Clostridium ramosum (14), 0.25 and 8; for Fusobacterium nucleatum (12), 0.125 and 0.25; for Fusobacterium necrophorum (11), 0.25 and 0.5; for Fusobacterium varium (13), 0.5 and 1; for Fusobacterium spp. (12), 1 and 2; for Peptostreptococcus anaerobius (13), 0.06 and 0.06; for Peptostreptococcus asaccharolyticus (13), 0.125 and 0.125; for Peptostreptococcus magnus (14), 0.03 and 0.03; for Peptostreptococcus micros (12), 0.06 and 0.06; for Peptostreptococcus prevotii (14), 0.06 and 0.25; for Porphyromonas asaccharolytica (11), 0.125 and 0.125; for Prevotella bivia (10), 8 and 16; for Prevotella buccae (10), 2 and 2; for Prevotella intermedia (10), 0.5 and 0.5; and for Prevotella melaninogenica (11), 1 and 1. Gemifloxacin mesylate (SB 265805) was 1 to 4 dilutions more active than trovafloxacin against fusobacteria and peptostreptococci, and the two drugs were equivalent against clostridia and P. asaccharolytica. Gemifloxacin was equivalent to sitafloxacin (DU 6859a) against peptostreptococci, C. perfringens, and C. ramosum, and sitafloxacin was 2 to 3 dilutions more active against fusobacteria. Sparfloxacin, grepafloxacin, and levofloxacin were generally less active than gemifloxacin against all anaerobes. PMID:10471570

Goldstein, E J; Citron, D M; Warren, Y; Tyrrell, K; Merriam, C V

1999-09-01

178

In vitro activity of antimicrobial agents against Pseudomonas tolaasii, pathogen of cultivated button mushroom  

Microsoft Academic Search

In vitro antibacterial activity tests of seven biofungicides (Ekstrasol, Bisolbisan, Bisolbifit, Serenade, Sonata, Timorex, F-Stop) and two disinfectants (colloidal silver alone and in combination with hydrogen peroxide) against the Pseudomonas tolaasii strain (NS3B6) were carried out by the disc-diffusion, broth microdilution and broth macrodilution method. Biofungicides tested in this study did not exhibit any antimicrobial activity in neither one of

Biljana Todorovi?; Svetlana Milijasevi?-Mar?i?; Ivana Poto?nik; Miloš Stepanovi?; Emil Rekanovi?; Ljiljana Nikoli?-Bujanovi?; Milan ?ekerevac

2012-01-01

179

Effects of Aroclors and individual PCB congeners on activation of the human androgen receptor in vitro  

Microsoft Academic Search

To investigate possible interactions between the human androgen receptor and PCBs in vitro, we have used a previously characterized human androgen receptor reporter gene assay in which PC-3 LUCAR+ cells respond to 5?-dihydrotestosterone (DHT, 50pM) with enhanced luciferase activity. The effects of Aroclors, commercial mixtures of PCBs, or polychlorinated terphenyls (PCTs) (0, 0.1, 1.0, and 10.0?M) on luciferase activity in

Timothy J. Schrader; Gerard M. Cooke

2003-01-01

180

In vitro antimicrobial activity of a chitooligosaccharide mixture against Actinobacillus actinomycetemcomitans and Streptococcus mutans  

Microsoft Academic Search

The purpose of this study was to evaluate the in vitro antibacterial activity of a chitooligosaccharide mixture (MW 2000–30?000 Da) with a deacetylation degree of 91.5% against two representative oral pathogens, Actinobacillus actinomycetemcomitans and Streptococcus mutans. A 0.1% concentration of the chitooligosaccharides (derived from the exoskeletons of marine crustaceans) was used to estimate antibacterial activity. Approximately 2 logcolony forming units

Bong-Kyu Choi; Kwang-Yoon Kim; Yun-Jung Yoo; Suk-Jung Oh; Jong-Hoon Choi; Chong-Youl Kim

2001-01-01

181

In Vitro and In Vivo Antibacterial Activities of BO2727, a New Carbapenem  

Microsoft Academic Search

BO-2727, a new injectable carbapenem, was evaluated for its in vitro and in vivo antibacterial activities in comparison with those of biapenem, meropenem, imipenem, cefpirome, and ceftazidime. BO-2727 had activity comparable to that of imipenem against methicillin-susceptible staphylococci and streptococci, with MICs at which 90% of strains tested (MIC90s) are inhibited being equal to 0.5 mg\\/ml or less. Against methicillin-

YOSHINARI ASAHI; SHUICHI MIYAZAKI; ANDKEIZO YAMAGUCHI

1995-01-01

182

Nicking and joining activity of banana bunchy top virus replication protein in vitro  

Microsoft Academic Search

The major open reading frame of banana bunchy top virus (BBTV) DNA-1 encodes a putative repli- cation initiation protein (Rep). In vitro, a fusion protein of BBTV Rep linked to a maltose-binding protein exhibited both site-specific nicking and joining activities. These activities were dependent on the presence of Mg2M or Mn2M, but did not require ATP. The fusion protein specifically

Gregory J. Hafner; Mark R. Stafford; Lindsay C. Wolter; Robert M. Harding; James L. Dale

183

In vitro antiplasmodial and cytotoxic activities of asymmetrical pyridinium derivatives.  

PubMed

An in vitro investigation of the antiplasmodial and cytotoxic activities of a series of human choline kinase inhibitors against Plasmodium falciparum is reported. Structure-activity relationship analyses have allowed us to determine the essential parameters for the antimalarial effect of these asymmetrical pyridinium derivatives. One of the compounds meets the World Health Organization's criteria for hit identification against P. falciparum exhibiting an IC50 of 0.0016 ?g/ml and a selectivity index of >3000. PMID:25089811

Rubio-Ruiz, Belén; Castillo-Acosta, Víctor M; Pérez-Moreno, Guiomar; Espinosa, Antonio; González-Pacanowska, Dolores; Ruiz-Pérez, Luis M; Entrena, Antonio; Conejo-García, Ana

2014-10-01

184

In vitro activities of new oral beta-lactams and macrolides against Campylobacter pylori.  

PubMed Central

The in vitro activities of amoxicillin, cefuroxime, ceftetrame, cefetamet, cefixime, tigemonam, erythromycin, roxithromycin, and dirithromycin against 30 clinical isolates of Campylobacter pylori were determined by an agar dilution technique. Roxithromycin and amoxicillin (MICs for 90% of isolates tested, 0.01 and 0.06 micrograms/ml, respectively) were the most active antibiotics tested, but all strains were susceptible to all antimicrobial agents tested. PMID:2817868

García-Rodríguez, J A; García Sánchez, J E; García García, M I; García Sánchez, E; Muńoz Bellido, J L

1989-01-01

185

Comparative in vitro activities of ciprofloxacin and other 4-quinolones against Mycobacterium tuberculosis and Mycobacterium intracellulare.  

PubMed Central

The in vitro activity of ciprofloxacin, ofloxacin, amifloxacin, and norfloxacin against 22 clinical isolates of Mycobacterium tuberculosis was evaluated by agar dilution. The MICs for 90% of the isolates of ciprofloxacin and ofloxacin were 0.5 and 1 microgram/ml, respectively. Amifloxacin and norfloxacin were less active. The MICs for 90% of the isolates of ciprofloxacin and ofloxacin against 20 clinical isolates of Mycobacterium intracellulare were determined by agar dilution to be 2 and 8 micrograms/ml, respectively. PMID:2940969

Fenlon, C H; Cynamon, M H

1986-01-01

186

In Vitro Anti-Helicobacter pylori Activities of New Rifamycin Derivatives, KRM-1648 and KRM-1657  

Microsoft Academic Search

The new rifamycin derivatives KRM-1657 and KRM-1648 were evaluated for their in vitro antimicrobial activities against 44 strains of Helicobacter pylori. Although the drugs were not very active against other gram-negative bacteria, the MICs at which 90% of isolates are inhibited for these drugs were lower (0.002 and 0.008 mg\\/ml, respectively) than those of amoxicillin and rifampin for H. pylori.

JUNKO K. AKADA; MUTSUNORI SHIRAI; KENJI FUJII; KIWAMU OKITA; TERUKO NAKAZAWA

1999-01-01

187

In Vitro Activities of Ertapenem (MK-0826) against Recent Clinical Bacteria Collected in Europe and Australia  

Microsoft Academic Search

Ertapenem (MK-0826, L-749,345) is a 1-b-methyl carbapenem with a long serum half-life. Its in vitro activity was determined by broth microdilution against 3,478 bacteria from 12 centers in Europe and Australia, with imipenem, cefepime, ceftriaxone, and piperacillin-tazobactam used as comparators. Ertapenem was the most active agent tested against members of the family Enterobacteriaceae, with MICs at which 90% of isolates

DAVID M. LIVERMORE; MICHAEL W. CARTER; SIMONE BAGEL; BERND WIEDEMANN; FERNANDO BAQUERO; ELENA LOZA; HUBERT P. ENDTZ; NICOLE VAN DEN BRAAK; CLARENCE J. FERNANDES; LORNA FERNANDES; NIELS FRIMODT-MOLLER; LAURA S. RASMUSSEN; HELEN GIAMARELLOU; EVANGELOS GIAMARELLOS-BOURBOULIS; VINCENT JARLIER; JACQUELINE NGUYEN; CARL-ERIK NORD; MARC J. STRUELENS; CAIRE NONHOFF; JOHN TURNIDGE; JAN BELL; REINHARD ZBINDEN; STEFAN PFISTER; LORI MIXSON; DANIEL L. SHUNGU

2001-01-01

188

In Vitro and In Vivo Antibacterial Activities of CS834, a New Oral Carbapenem  

Microsoft Academic Search

CS-834 is a prodrug of the carbapenem R-95867, developed by Sankyo Co., Ltd., Tokyo, Japan. To investigate the possibility that CS-834 may be the first carbapenem usable in an oral dosage form, its in vitro antibacterial activity (as R-95867) and in vivo antibacterial activity were compared with those of cefpodoxime proxetil, cefdi- toren pivoxil, cefdinir, ofloxacin, imipenem, and amoxicillin. R-95867

KEIZO YAMAGUCHI; HARUKI DOMON; SHUICHI MIYAZAKI; KAZUHIRO TATEDA; AKIRA OHNO; KAZUHIRO ISHII; TETSUYA MATSUMOTO; NOBUHIKO FURUYA

189

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

190

In vitro free radical scavenging activity of platinum nanoparticles  

NASA Astrophysics Data System (ADS)

A polyacrylic acid (PAA)-protected platinum nanoparticle species (PAA-Pt) was prepared by alcohol reduction of hexachloroplatinate. The PAA-Pt nanoparticles were well dispersed and homogeneous in size with an average diameter of 2.0 ± 0.4 nm (n = 200). We used electron spin resonance to quantify the residual peroxyl radical (\\mathrm {AOO}^{\\bullet } ) generated from 2,2-azobis (2-aminopropane) dihydrochloride (AAPH) by thermal decomposition in the presence of O2 and a spectrophotometric method to quantify the residual 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical. PAA-Pt scavenged these two radicals in a dose-dependent manner. Platinum was the functional component. PAA-Pt reduced the rate of oxygen consumption required for linoleic acid peroxidation initiated by \\mathrm {AOO}^{\\bullet } generated from AAPH, indicating inhibition of the propagation of linolate peroxidation. A thiobarbituric acid test also revealed dose-dependent inhibition of the linolate peroxidation by PAA-Pt. Fifty micromolar platinum, as PAA-Pt, completely quenched 250 µM DPPH radical for 5 min. Even when twice diluted in half, the PAA-Pt still quenched 100% of the 250 µM DPPH radical. The scavenging activity of PAA-Pt is durable. These observations suggest that PAA-Pt is an efficient scavenger of free radicals.

Watanabe, Aki; Kajita, Masashi; Kim, Juewon; Kanayama, Atsuhiro; Takahashi, Kyoko; Mashino, Tadahiko; Miyamoto, Yusei

2009-11-01

191

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

192

Comparative in vitro activity of ceftibuten (Sch 39720) against bacterial enteropathogens.  

PubMed Central

Ceftibuten is a new orally active cephalosporin with significant bioavailability. Its in vitro activity was compared with those of other agents against 383 strains of enteric pathogens derived from clinical specimens. Ceftibuten was very active against the strains of the family Enterobacteriaceae tested (overall MIC for 90% of strains tested, 0.25 microgram/ml) but was less active against Campylobacter jejuni (MIC for 90% of strains, 16 micrograms/ml). The MBC was one to two dilutions higher than the corresponding MICs for most pathogens tested. PMID:2751289

Shawar, R; LaRocco, M; Cleary, T G

1989-01-01

193

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

194

In vitro and in vivo antibacterial activities of S-1090, a new oral cephalosporin.  

PubMed Central

S-1090, a new oral cephalosporin, was active against selected gram-negative bacteria and methicillin-susceptible clinical isolates of Staphylococcus aureus, Staphylococcus epidermidis, and Staphylococcus warneri, against which it had excellent activity. S-1090 was the most active compound against Streptococcus pyogenes and Streptococcus agalactiae among the agents compared. The in vivo efficacy of S-1090 against systemic and urinary and respiratory tract infections caused by gram-positive and -negative bacteria was superior to that expected from the in vitro and in vivo activities of the agents against which it was compared. PMID:8585742

Tsuji, M; Ishii, Y; Ohno, A; Miyazaki, S; Yamaguchi, K

1995-01-01

195

In Vitro and In Vivo Activities of Gatifloxacin against Mycobacterium tuberculosis  

PubMed Central

Gatifloxacin (GAT) and moxifloxacin (MXF) were evaluated in vitro to determine their activities against Mycobacterium tuberculosis. GAT was subsequently compared in a dose range study to isoniazid (INH) in a murine tuberculosis model. GAT was somewhat less active than INH. GAT and MXF were evaluated in mice infected with M. tuberculosis and were found to have similar activities. GAT was studied alone and in combination with ethambutol, ethionamide (ETA), and pyrazinamide (PZA) and compared to INH and rifampin (RIF). GAT appears to have sufficient activity alone and in combination with ETA with or without PZA to merit evaluation for treatment of tuberculosis. PMID:11897584

Alvirez-Freites, Enrique J.; Carter, Janna L.; Cynamon, Michael H.

2002-01-01

196

Embryo production by parthenogenetic activation and fertilization of in vitro matured oocytes from Cebus apella.  

PubMed

The efficiency of in vitro fertilization (IVF) depends on the viability of spermatozoa. For capuchin monkeys (Cebus apella), in vitro capacitation of spermatozoa is challenging because of their unique seminal coagulum. Motile spermatozoa can be obtained after liquefaction of the semen coagulum in coconut water-based solution. The objective of the present study was to establish an optimal in vitro maturation (IVM) protocol for capuchin monkeys and to observe the effect of follicle stimulating hormone (FSH) and luteinising hormone (LH) on IVF and parthenogenetic activation (PA) of oocytes collected from unstimulated females. We assessed spermatozoa quality after recovery from seminal coagulum using the solution ACP-118® as an extender. Oocytes were matured in vitro for 36 or 40 h and subjected to IVF or PA by applying ionomycin combined either with 6-dimethylaminopurine (6-DMAP) or roscovitine. In total, 87% of oocytes reached metaphase II (MII) after 40 IVM and 4-cell embryo production was obtained after IVF and parthenogenesis using ionomycin/6-DMAP. ACP-118® was used successfully to harvest viable spermatozoa from semen coagulum and in the preservation of spermatozoa, which were able to fertilize oocytes in vitro. PMID:22230224

Lima, Julianne S; Leăo, Danuza L; Sampaio, Rafael V; Brito, Adriel B; Santos, Regiane R; Miranda, Moysés S; Ohashi, Otávio M; Domingues, Sheyla F S

2013-05-01

197

In-vitro and in-vivo antibacterial activities of CS-834, a new oral carbapenem.  

PubMed

We evaluated the in-vitro and in-vivo antibacterial activities of R-95867 and CS-834, a new oral carbapenem which is an ester-type prodrug of R-95867. Against Gram-positive bacteria, R-95867 was as active or two to 256 times more active than cefpodoxime, cefdinir, cefditoren and ofloxacin, while its activity was similar to or two to eight times lower than that of imipenem. Against most Gram-negative bacteria it was as active or two to 1024 times more active than the other compounds tested. Against Helicobacter pylori it was two to 64 times more active than orally active anti-H. pylori agents, i.e. amoxycillin, clarithromycin and lansoprazole. It also showed potent bactericidal activity against Staphylococcus aureus and Escherichia coli. R-95867 induced a spherical form in E. coli and showed high affinity for PBP 2 in E. coli. Against systemic infections in mice caused by various bacteria, CS-834 showed an excellent protective effect and its in-vivo efficacy correlated well with the in-vitro activity of R-95867. These results suggest that CS-834 may be effective in the therapy of various bacterial infections. PMID:9818740

Sakagawa, E; Otsuki, M; Oh, T; Nishino, T; Ou, T

1998-10-01

198

Immunomodulatory Activity in Vitro and in Vivo of Verbascose from Mung Beans (Phaseolus aureus).  

PubMed

In the present study, the immunostimulatory activity of verbascose from mung beans (Phaseolus aureus) was evaluated by using in vitro cell models and in vivo animal models. The results of in vitro experiments showed that verbascose could enhance the ability of devouring neutral red of peritoneal macrophages and promote the release of nitric oxide and immune reactive molecules such as interleukin (IL)-6, IL-1?, interferon (IFN)-?, and IFN-?. Treatment with verbascose at a dose of 200 ?g/mL exhibited the best effects. For assay in vivo, administration of verbascose at a medium dose of 90 mg/kg body weight could significantly increase the index of spleen, activity of lysozyme in spleen and serum, hemolysin level in serum, and swelling rate of earlap in the delayed type of hypersensitivity (DTH) of immunosuppressed mice. All of the results suggested that verbascose had potent immunostimulatory activity and could be explored as a potential natural immunomodulatory agent in functional foods. PMID:25317918

Dai, Zhuqing; Su, Di; Zhang, Yun; Sun, Yi; Hu, Bing; Ye, Hong; Jabbar, Saqib; Zeng, Xiaoxiong

2014-11-01

199

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

200

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

201

Extraordinary Effects of Specific Monovalent Cations on Activation of Reovirus Transcriptase by Chymotrypsin In Vitro  

PubMed Central

Activation of reovirus transcriptase activity, latent in intact virions, by digestion of purified virions with chymotrypsin (CHT) in vitro shows a stringent requirement for specific monovalent cations. Cs+, Rb+, or K+ ions are capable of facilitating activation by chymotryptic digestion. Na+, Li+, or NH4+ ions are not capable of facilitating the CHT activation of polymerase activity and are antagonistic towards the effects of the facilitating ions. The data indicate that the effect of the cations is exerted on activation of the polymerase activity by CHT as opposed to an effect on polymerization per se. This effect may be important biologically in that it provides a mechanism whereby the virion can sense whether it is in an intracellular or an extracellular environment and thereby can avoid premature uncoating. PMID:4347424

Borsa, J.; Sargent, M. D.; Long, D. G.; Chapman, J. D.

1973-01-01

202

Eosinophils affect functions of in vitro-activated human CD3-CD4+ T cells  

PubMed Central

Background The recent development of eosinophil-targeting agents has raised enthusiasm for management of patients with hypereosinophilic syndromes. Roughly half of anti-IL-5-treated patients with corticosteroid-responsive lymphocytic (L-HES) and idiopathic disease variants can be tapered off corticosteroids. Potential consequences of corticosteroid-withdrawal on clonal expansion of pre-malignant CD3-CD4+ T-cells associated with L-HES are a subject of concern. Indeed, corticosteroid treatment inhibits T-cell activation and may lower blood CD3-CD4+ cell counts. On the other hand, previous studies have shown that eosinophils support CD4 T-cell activation, suggesting that targeted eosinophil depletion may negatively regulate these cells. Objectives Effects of eosinophils on CD4 T-cell activation in vitro were investigated as an indirect means of exploring whether treatment-induced eosinophil depletion may affect pathogenic T-cells driving L-HES. Methods Helper (CD4) T-cells and CD3-CD4+ cells from healthy controls and L-HES patients, respectively, were cultured in vitro in presence of anti-CD3/CD28 or dendritic cells. Effects of eosinophils on T-cell proliferation and cytokine production were investigated. Results Eosinophils enhanced CD3-driven proliferation of CD4 T-cells from healthy subjects in vitro, while inhibiting TCR-independent proliferation and IL-5 production by CD3-CD4+ T-cells. Conclusions While this study confirms previous work showing that eosinophils support activation of normal helper T-cells, our in vitro findings with CD3-CD4+ T-cells suggest that eosinophil-depletion may favor activation and expansion of this pathogenic lymphocyte subset. With the ongoing development of eosinophil-targeted therapy for various eosinophilic conditions, the indirect consequences of treatment on the underlying immune mechanisms of disease should be investigated in detail in the setting of translational research programs. PMID:23642304

2013-01-01

203

Silylation improves the photodynamic activity of tetraphenylporphyrin derivatives in vitro and in vivo.  

PubMed

The effects of silyl and hydrophilic groups on the photodynamic properties of tetraphenylporphyrin (TPP) derivatives have been studied in vitro and in vivo. Silylation led to an improvement in the quantum yield of singlet oxygen sensitization for both sulfo and carboxy derivatives, although the silylation did not affect other photophysical properties. Silylation also improved the cellular uptake efficiency for both sulfo and carboxy derivatives, enhancing the in vitro photodynamic activity of the photosensitizer in U251 human glioma cells. The carboxy derivative (SiTPPC4 ) was found to show higher cellular uptake efficiency and in vitro photodynamic activity than the corresponding sulfo derivative (SiTPPS4 ), which indicates that the carboxy group is a more promising hydrophilic group than the sulfo group in the silylated porphyrin. SiTPPC4 was found to show high selective accumulation efficiency in tumors, although almost no tumor selectivity was observed for the nonsilylated porphyrin. The concentration of SiTPPC4 in tumors was 13 times higher than that in muscle 12?h after drug administration. We also studied tumor response after treatment and found that silylation enhanced in vivo photodynamic activity significantly. SiTPPC4 shows higher photodynamic activity than NPe6 with white light irradiation. PMID:24710805

Horiuchi, Hiroaki; Hosaka, Masahiro; Mashio, Hiroyuki; Terata, Motoki; Ishida, Shintaro; Kyushin, Soichiro; Okutsu, Tetsuo; Takeuchi, Toshiyuki; Hiratsuka, Hiroshi

2014-05-12

204

In vitro activity of A-56619 and A56620, two new aryl-fluoroquinolone antimicrobial agents.  

PubMed Central

The in vitro antimicrobial activity of two new aryl-fluoroquinolone antibiotics, A-56619 and A-56620, was compared with those of norfloxacin and several other antibiotics against 448 bacterial isolates. A-56620 was the most active agent tested. The usual 90% MIC of A-56620 was less than or equal to 2 micrograms/ml, except for enterococci, gentamicin-resistant Serratia marcescens, and gentamicin-resistant Pseudomonas aeruginosa, for which the 90% MIC was 4 micrograms/ml. A-56619 and norfloxacin were generally severalfold less active than A-56620. Cross resistance was observed between the quinolone antibiotics and other unrelated antibiotic classes. PMID:3717937

Smith, B R; LeFrock, J L; Donato, J B; Joseph, W S; Weber, S J

1986-01-01

205

Overexpression of inactive arylsulphatase mutants and in vitro activation by light-dependent oxidation with vanadate  

PubMed Central

Arylsulphatases B (ASB) and A (ASA) are subject to a unique post-translational modification that is required for their function. The modification reaction, conversion of an active-site cysteine into a formylglycine, becomes saturated when these enzymes are overexpressed. We have removed the possibility of in vivo modification by expressing mutants of ASB and ASA in which the active-site cysteine is substituted with a serine. These mutants are expressed much more efficiently when compared with the native enzymes under identical conditions. The purified ASB mutant can then be converted into catalytically active ASB in vitro using vanadate and light. PMID:15175008

2004-01-01

206

In vitro activity of sertaconazole, fluconazole, ketoconazole, fenticonazole, clotrimazole and itraconazole against pathogenic vaginal yeast isolates.  

PubMed

The in vitro activity of sertaconazole was compared with those of the most commonly used vaginal antimycotic agents--fluconazole, ketoconazole, fenticonazole, clotrimazole and itraconazole--against 94 strains of clinical isolates of Candida spp. using a macrodilution method in Casitone agar medium. The sertaconazole concentration (microgram/ml), at which 90% of the strains were inhibited, was 0.06 for C. albicans, 0.25 for C. glabrata and C. parapsilosis, 1 for C. krusei and 2 for C. tropicalis. These values show that sertaconazole is one of the most active products against yeasts causing vulvovaginal candidiasis, its activity against C. glabrata being particularly relevant. PMID:11484411

Palacín, C; Tarragó, C; Agut, J; Guglietta, A

2001-03-01

207

In vitro antimycoplasmal activity of six Jordanian medicinal plants against three Mycoplasma species.  

PubMed

The in vitro effect of six Jordanian traditional medicine plant methanolic extracts were tested against 32 isolates of Mycoplasma species; Mycoplasma mycoides subsp. mycoides LC (6), Mycoplasma capricolum subsp. capricolum (8) and M. putrefaciens (18), all isolated from either nasal swabs or milk, from sheep and goats in different regions in Jordan. All Mycoplasma species showed susceptibility to Artemisia herba-alba and Artemisia arborescens with MIC ranges from 3.125-12.5 mg/ml. Allium sativum and Punica grantum showed limited activity against some Mycoplasma isolates. Olea europea and Citrullus colocynthis showed no in vitro activity against any of the Mycoplasma species tested. Artemisia herba-alba and Artemisia arborescens may therefore be useful for the treatment of mycoplasma infections. PMID:17969714

Al-Momani, W; Abu-Basha, E; Janakat, S; Nicholas, R A J; Ayling, R D

2007-10-01

208

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

209

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

210

Phosphatidyl derivative of hydroxytyrosol. In vitro intestinal digestion, bioaccessibility, and its effect on antioxidant activity.  

PubMed

Intestinal digestion of phosphatidyl derivatives of HT (PHT) and its bioaccessibility under in vitro conditions was performed. First, an in vitro intestinal digestion model for phospholipids was developed. The impact of digestion in the antioxidant ability of PHT was also assayed. PHT was progressively hydrolyzed to lyso-PHT. However, digestion was slower than the phospholipid control. Nevertheless, most hydrolysis products were found at the micellar phase fraction, meaning a high bioaccessibility. Either PHT or digested PHT showed lower antioxidant activity than HT. However, PHT improved its antioxidant ability after digestion, likely related to lyso-PHT. As a summary, the synthetic phosphatidyl derivative of HT as PHT is recognized by phospholipases during simulation of intestinal digestion, although less efficiently than analogous phospholipids. Nevertheless, taking into account the bioaccessibility and the antioxidant activity of digested PHT, the potential of carriers of HT under the form of phospholipids might be of interest. PMID:25255083

Martin, Diana; Moran-Valero, Maria I; Casado, Víctor; Reglero, Guillermo; Torres, Carlos F

2014-10-01

211

Receptor-mediated in vitro bioassay for characterization of Ah-R-active compounds and activities in sediment from Korea  

Microsoft Academic Search

Sediment extracts of stream sediments, collected from inland areas of Lake Shihwa (LSI) and Masan Bay (MBI), were screened for their abilities to induce aryl hydrocarbon receptor (Ah-R) mediated gene expression in vitro. Cell viability assay was also performed to examine cytotoxic effects on the Ah-R-mediated activities of sediment samples. Over 80% (30 out of 36) of sediment raw extracts

Hoon Yoo; Jong Seong Khim; John P. Giesy

2006-01-01

212

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

213

Activity of oritavancin and comparators in vitro against standard and high inocula of Staphylococcus aureus  

Microsoft Academic Search

In this study, the impact of inoculum density on the growth inhibitory and killing activities of oritavancin and comparators (vancomycin, daptomycin and linezolid) in vitro against four Staphylococcus aureus strains at clinically relevant drug concentrations was studied. Broth microdilution and time–kill assays were performed using a standard inoculum [ca. 105colony-forming units (CFU)\\/mL as per Clinical and Laboratory Standards Institute (CLSI)

Francis F. Arhin; Ingrid Sarmiento; Thomas R. Parr; Gregory Moeck

214

In Vitro Activity of OPT-80 Tested against Clinical Isolates of Toxin-Producing Clostridium difficile?  

PubMed Central

Agar dilution antimicrobial susceptibility testing (CLSI, M11-A7, 2007) performed for 208 toxin-producing clinical isolates of Clostridium difficile resulted in OPT-80 MICs ranging from 0.06 to 1 ?g/ml, with 90% of the isolates inhibited by a concentration of 0.5 ?g/ml. The in vitro activity of OPT-80 was independent of the susceptibilities of isolates to nine other antimicrobial agents. PMID:18725442

Karlowsky, James A.; Laing, Nancy M.; Zhanel, George G.

2008-01-01

215

In vitro evaluation of the antimicrobial activity of chlorhexidine and sodium hypochlorite  

Microsoft Academic Search

The aim of this study was to investigate in vitro the antimicrobial activity of 0.2%, 1%, and 2% chlorhexidine gluconate (CHX gel and CHX liquid), against endodontic pathogens and compare the results with the ones achieved by 0.5%, 1%, 2.5%, 4%, and 5.25% sodium hypochlorite (NaOCl). A broth dilution test was performed, and the timing for irrigants to kill microbial

Morgana Eli Vianna; Brenda P. F. A Gomes; Vanessa Bellocchio Berber; Alexandre Augusto Zaia; Caio Cezar Randi Ferraz; Francisco José de Souza-Filho

2004-01-01

216

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

217

In vitro activity of A-86719.1, a novel 2-pyridone antimicrobial agent.  

PubMed Central

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 < or = 0.5 microgram/ml and all tested Pseudomonas aeruginosa, Burkholderia (Pseudomonas) cepacia, and Xanthomonas maltophilia strains at < or = 2 micrograms/ml. All but two strains of gram-positive bacteria were inhibited by < or = 1 microgram of the new drug per ml, including isolates highly resistant to ciprofloxacin. PMID:7785983

Eliopoulos, G M; Wennersten, C B; Cole, G; Chu, D; Pizzuti, D; Moellering, R C

1995-01-01

218

CHS 828, a Novel Pyridyl Cyanoguanidine with Potent Antitumor Activity in Vitro and in Vivo  

Microsoft Academic Search

A new class of recently discovered antineoplastic agents, the pyridyl cyanoguanidines, exert a potent antitumor activity in rodents after oral administration. Optimization in vitro and in vivo has resulted in the selection of the lead candidate CHS 828 (N-(6-chlorophenoxyhexyl)-N*- cyano-N(-4-pyridylguanidine). CHS 828 was found to exert potent cyto- toxic effects in human breast and lung cancer cell lines, with lesser

Pernille-Julia Vig Hjarnaa; Elin Jonsson; Scilla Latini; Sumeer Dhar; Rolf Larsson; Erik Bramm; Torsten Skov; Lise Binderup

219

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

Microsoft Academic Search

190 isolates from clinical specimens were tested in vitro to determine their susceptibility pattern against augmentin. Of the 132 strains of Enterobacteriaceae tested, 109 (82.6%) were susceptible. 41 (93.2%) of the 44 gram-positive bacteria tested were also susceptible to augmentin. Strains of Pseudomonas aeruginosa and Serratia marcescens were resistant to augmentin. However, augmentin showed increased activity against Escherichia coli, and

Fred Perryman; Steve Johnson; Hussain Qadri

1983-01-01

220

In Vitro Activity of Tebipenem, a New Oral Carbapenem Antibiotic, against Penicillin-Nonsusceptible Streptococcus pneumoniae  

Microsoft Academic Search

The in vitro activity of tebipenem (TBM), a new oral carbapenem antibiotic, against Streptococcus pneumoniae clinical isolates (n 202) was compared with those of 15 reference agents. The isolates were classified into five genotypic classes after PCR identification of abnormal pbp1a, pbp2x, and pbp2b genes: (i) penicillin-susceptible S. pneumoniae (PSSP) isolates with no abnormal pbp genes (n 34; 16.8%), (ii)

Reiko Kobayashi; Mami Konomi; Keiko Hasegawa; Miyuki Morozumi; Keisuke Sunakawa; Kimiko Ubukata

2005-01-01

221

In Vitro and In Vivo Activities of Sitafloxacin against Chlamydia spp  

Microsoft Academic Search

The in vitro and in vivo antichlamydial activity of sitafloxacin was investigated. The MICs and minimal chlamydiacidal concentrations of sitafloxacin for various species of chlamydia ranged from 0.031 to 0.125 g\\/ml. Sitafloxacin had an excellent therapeutic effect on experimental Chlamydia psittaci pneumonia and was more potent than tosufloxacin, ofloxacin, and ciproflxacin, although slightly less potent than sparfloxacin. Sitafloxacin is a

NAOYUKI MIYASHITA; YOSHIHITO NIKI; TOSHIHARU MATSUSHIMA

2001-01-01

222

In vitro and in vivo anti-malarial activity of Boerhavia elegans and Solanum surattense  

PubMed Central

Background There is an urgent need to identify new anti-malarial drug targets for both prophylaxis and chemotherapy, due to the increasing problem of drug resistance to malaria parasites. In the present study, the aim was to discover novel, effective plant-based extracts for the activity against malaria. Methods Ten plants found in Iran were selected by ethnobotanical survey of medicinal plants. The crude ethanolic extracts were tested for in vitro anti-plasmodial activity against two strains of Plasmodium falciparum: K1 (chloroquine-resistant strain) and CY27 (chloroquine-sensitive strain), using the parasite lactate dehydrogenase (pLDH) assay. The anti-plasmodial activity of the extracts was also assessed in the 4-day suppressive anti-malarial assay in mice inoculated with Plasmodium berghei (ANKA strain). Crude ethanolic extracts showed good anti-plasmodial activity were further fractionated by partitioning in water and dichloromethane. Results Of 10 plant species assayed, three species: Boerhavia elegans (Choisy), Solanum surattense (Burm.f.) and Prosopis juliflora (Sw.) showed promising anti-plasmodial activity in vitro (IC50 ? 50 ?g/ml) and in vivo with no toxicity. The dichloromethane fraction of three extracts revealed stronger anti-plasmodial activity than the total extracts. Conclusion Anti-plasmodial activities of extracts of B. elegans and S. surattense are reported for the first time. PMID:20462416

2010-01-01

223

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

224

The protective role of AMP-activated protein kinase in alpha-synuclein neurotoxicity in vitro.  

PubMed

In the present study, we investigated the role of the main intracellular energy sensor, AMP-activated protein kinase (AMPK), in the in vitro neurotoxicity of ?-synuclein (ASYN), one of the key culprits in the pathogenesis of Parkinson's disease. The loss of viability in retinoic acid-differentiated SH-SY5Y human neuroblastoma cells inducibly overexpressing wild-type ASYN was associated with the reduced activation of AMPK and its activator LKB1, as well as AMPK target Raptor. ASYN-overexpressing rat primary neurons also displayed lower activity of LKB1/AMPK/Raptor pathway. Restoration of AMPK activity by metformin or AICAR reduced the in vitro neurotoxicity of ASYN overexpression, acting independently of the prosurvival kinase Akt or the induction of autophagic response. The conditioned medium from ASYN-overexpressing cells, containing secreted ASYN, as well as dopamine-modified or nitrated recombinant ASYN oligomers, all inhibited AMPK activation in differentiated SH-SY5Y cells and reduced their viability, but not in the presence of metformin or AICAR. The RNA interference-mediated knockdown of AMPK increased the sensitivity of SH-SY5Y cells to the harmful effects of secreted ASYN. AMPK-dependent protection from extracellular ASYN was also observed in rat neuron-like pheochromocytoma cell line PC12. These data demonstrate the protective role of AMPK against the toxicity of both intracellular and extracellular ASYN, suggesting that modulation of AMPK activity may be a promising therapeutic strategy in Parkinson's disease. PMID:24269733

Dulovic, Marija; Jovanovic, Maja; Xilouri, Maria; Stefanis, Leonidas; Harhaji-Trajkovic, Ljubica; Kravic-Stevovic, Tamara; Paunovic, Verica; Ardah, Mustafa T; El-Agnaf, Omar M A; Kostic, Vladimir; Markovic, Ivanka; Trajkovic, Vladimir

2014-03-01

225

Anti-glycated and antiradical activities in vitro of polysaccharides from Ganoderma capense  

PubMed Central

Background Ganoderma capense is a Ganoderma species and is widely used, especially in Asia, as a well-known medicinal mushroom for health-promoting effect and for treatment of chronic diseases, such as diabetes, aging, etc. G. capense is rich of polysaccharide. Objective: To isolate the polysaccharides from G. capense and evaluate their anti-glycated and antiradical activities in vitro. Materials and Methods The dried powder of submerged fermentation culturing mycelium of G. capense was defatted, extracted with water/alkaline water followed by ethanol precipitation and deproteinated. And four crude polysaccharides, named as GC50, GC70, GC90 and GCB, were obtained. For the first time, the in vitro anti-glycated activities of the four samples were studied by non-enzymatic glycation reaction. Then, the DPPH radical and hydroxyl radical assays were established to estimate the antiradical capacity of the four samples. Meanwhile the contents of polysaccharides were determined by phenol-sulphuric acid colorimetry. Results and Conclusion Preliminary antiradical in vitro studies indicated that the four crude polysaccharides showed concentration-dependent scavenging abilities on DPPH and hydroxyl radicals. The evaluation of anti-glycation activity suggested that GC70 had good potential for inhibiting the formation of advanced glycation end products. Time- and dose-dependent effects were also observed for all GC70 samples. PMID:23661989

Yan, Chunyan; Kong, Fansheng; Zhang, Dezhi; Cui, Jiangxia

2013-01-01

226

Regulation of Xenopus laevis DNA topoisomerase I activity by phosphorylation in vitro  

SciTech Connect

DNA topoisomerase I has been purified to electrophoretic homogeneity from ovaries of the frog Xenopus laevis. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis of the most purified fraction revealed a single major band at 110 kDa and less abundant minor bands centered at 62 kDa. Incubation of the most purified fraction with immobilized calf intestinal alkaline phosphatase abolished all DNA topoisomerase enzymatic activity in a time-dependent reaction. Treatment of the dephosphorylated X. laevis DNA topoisomerase I with a X. laevis casein kinase type II activity and ATP restored DNA topoisomerase activity to a level higher than that observed in the most purified fraction. In vitro labeling experiments which employed the most purified DNA topoisomerase I fraction, (..gamma..-/sup 32/P)ATP, and the casein kinase type II enzyme showed that both the 110- and 62-kDa bands became phosphorylated in approximately molar proportions. Phosphoamino acid analysis showed that only serine residues became phosphorylated. Phosphorylation was accompanied by an increase in DNA topoisomerase activity in vitro. Dephosphorylation of DNA topoisomerase I appears to block formation of the initial enzyme-substrate complex on the basis of the failure of the dephosphorylated enzyme to nick DNA in the presence of camptothecin. The authors conclude that X. laevis DNA topoisomerase I is partially phosphorylated as isolated and that this phosphorylation is essential for expression of enzymatic activity in vitro. On the basis of the ability of the casein kinase type II activity to reactivate dephosphorylated DNA topoisomerase I, they speculate that this kinase may contribute to the physiological regulation of DNA topoisomerase I activity.

Kaiserman, H.B.; Ingebritsen, T.S.; Benbow, R.M.

1988-05-03

227

In vitro and In vivo Antimalarial Activity of Amphiphilic Naphthothiazolium Salts with Amine-Bearing Side Chains.  

PubMed

Because of emerging resistance to existing drugs, new chemical classes of antimalarial drugs are urgently needed. We have rationally designed a library of compounds that were predicted to accumulate in the digestive vacuole and then decrystallize hemozoin by breaking the iron carboxylate bond in hemozoin. We report the synthesis of 16 naphthothiazolium salts with amine-bearing side chains and their activities against the erythrocytic stage of Plasmodium falciparum in vitro. KSWI-855, the compound with the highest efficacy against the asexual stages of P. falciparum in vitro, also had in vitro activity against P. falciparum gametocytes and in vivo activity against P. berghei in a murine malaria model. PMID:25184829

Ulrich, Peter; Gipson, Gregory R; Clark, Martha A; Tripathi, Abhai; Sullivan, David J; Cerami, Carla

2014-10-01

228

In Vitro and In Vivo Antibacterial Activities of S-4661, a New Carbapenem  

PubMed Central

The in vitro and in vivo antibacterial activities of S-4661, a new 1?-methylcarbapenem, were compared with those of imipenem, meropenem, biapenem, cefpirome, and ceftazidime. The activity of S-4661 against methicillin-susceptible staphylococci and streptococci was comparable to that of imipenem, with an MIC at which 90% of the strains tested were inhibited (MIC90) equal to 0.5 ?g/ml or less. S-4661 was highly active against members of the family Enterobacteriaceae, Haemophilus influenzae, and Moraxella catarrhalis, with MIC90s ranging from 0.032 to 0.5 ?g/ml. Against imipenem-resistant Pseudomonas aeruginosa, S-4661 was the most active among test agents (MIC90, 8 ?g/ml). Furthermore, S-4661 displayed a high degree of activity against many ceftazidime-, ciprofloxacin-, and gentamicin-resistant isolates of P. aeruginosa. The in vivo efficacy of S-4661 against experimentally induced infections in mice caused by gram-positive and gram-negative bacteria, including penicillin-resistant Streptococcus pneumoniae and drug-resistant P. aeruginosa, reflected its potent in vitro activity and high levels in plasma in mice. We conclude that S-4661 is a promising new carbapenem for the treatment of infections caused by gram-positive and -negative bacteria, including penicillin-resistant S. pneumoniae and drug-resistant P. aeruginosa. PMID:9449267

Tsuji, Masakatsu; Ishii, Yoshikazu; Ohno, Akira; Miyazaki, Shuichi; Yamaguchi, Keizo

1998-01-01

229

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

230

Synergy between RU 28965 (roxithromycin) and human neutrophils for bactericidal activity in vitro.  

PubMed Central

The in vitro effects of RU 28965 (roxithromycin), a new semisynthetic macrolide, on human neutrophil activity were compared with those of erythromycin. RU 28965, at a concentration as low as 0.1 microgram/ml, significantly enhanced the phagocytosis and killing of Staphylococcus aureus by neutrophils. Erythromycin displayed a less stimulating effect in a dose-dependent manner. Phagocytosis of Klebsiella pneumoniae was also increased after incubation of neutrophils with RU 28965, but killing was not altered. Neutrophil chemotaxis, myeloperoxidase activity, and O2 consumption were unchanged in the presence of RU 28965. PMID:3019233

Labro, M T; Amit, N; Babin-Chevaye, C; Hakim, J

1986-01-01

231

In vitro antibacterial activity of water-soluble extract of aghalokpe.  

PubMed

Water-soluble extracts of the bark of aghalokpe, a big tropical tree which grows in the rainforest of Bendel State of Nigeria, showed in vitro antibacterial activity against several of the Enterobacteriaceae. The activity was more pronounced with gram-positive than the gram-negative species. The minimum inhibitory concentration (MIC) which is in the range of 3.125-50 micrograms/ml, compares well with some broad-spectrum antibiotics on the market. The extract was remarkably effective against Neisseria gonorrhoea. PMID:6322551

Williams, B; Popoola, B

1983-06-01

232

Comparative study of the in vitro antifungal activity of bifonazole, naftifine and sertaconazole against yeasts.  

PubMed

The in vitro activity of three antifungal agents was tested and compared against 151 yeast strains, including ten Candida species, Cryptococcus neoformans, Rhodotorula rubra, and Trichosporon cutaneum. Minimum inhibitory concentrations (MICs) were determined by a microdilution technique in Shadomy modified liquid medium. The mean MICs of sertaconazole (0.34 mg/L) were lower than those of naftifine (16.3 mg/L) and bifonazole (13.2 mg/L). These results suggest that sertaconazole is more active against Candida spp than other topical agents such as bifonazole and naftifine. PMID:10435679

Carrillo-Muńoz, A J; Tur-Tur, C; Bornay-Llinares, F J; Arévalo, P

1999-06-01

233

In vitro activity of an evernimicin derivative, SCH27899, against anaerobic bacteria and Propionibacterium acnes.  

PubMed

The in vitro activity of SCH27899, a novel oligosaccharide antimicrobial agent, was compared with those of representatives of six classes of antimicrobial agents (piperacillin, clarithromycin, clindamycin, vancomycin, sitafloxacin and metronidazole) against clinical isolates of anaerobic bacteria and Propionibacterium acnes. Against Peptostreptococcus: spp. and Clostridium difficile, SCH27899 was the most potent (MIC(90) < 0.125 mg/L) of the agents examined. Besides these Gram-positive anaerobes, SCH27899 showed a moderate level of activity against Prevotella bivia, Prevotella intermedia and Porphyromonas: spp. (MIC(90)< or = 4 mg/L). PMID:10980176

Tanaka, K; Kato, N; Watanabe, K

2000-09-01

234

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

235

In vitro RNase and nucleic acid binding activities implicate coilin in U snRNA processing.  

PubMed

Coilin is known as the marker protein for Cajal bodies (CBs), subnuclear domains important for the biogenesis of small nuclear ribonucleoproteins (snRNPs) which function in pre-mRNA splicing. CBs associate non-randomly with U1 and U2 gene loci, which produce the small nuclear RNA (snRNA) component of the respective snRNP. Despite recognition as the CB marker protein, coilin is primarily nucleoplasmic, and the function of this fraction is not fully characterized. Here we show that coilin binds double stranded DNA and has RNase activity in vitro. U1 and U2 snRNAs undergo a processing event of the primary transcript prior to incorporation in the snRNP. We find that coilin displays RNase activity within the CU region of the U2 snRNA primary transcript in vitro, and that coilin knockdown results in accumulation of the 3' pre-processed U1 and U2 snRNA. These findings present new characteristics of coilin in vitro, and suggest additional functions of the protein in vivo. PMID:22558428

Broome, Hanna J; Hebert, Michael D

2012-01-01

236

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

237

Comparison of in vitro methods for assessing cytotoxic activity against two pancreatic adenocarcinoma cell lines.  

PubMed

Several models of pancreatic adenocarcinoma are now available for experimental evaluation of newer chemotherapeutic agents. The present study represents an attempt to develop a rapid in vitro screening technique that would allow prediction of cytotoxic activity (or lack thereof) as reliably as the clonogenic or colony formation assay. To this end, seven drugs (cisplatin, dactinomycin, doxorubicin, 5-fluorouracil, menogarol, mitoxantrone, and streptozocin) were tested against two pancreatic adenocarcinoma cell lines using a standard colony formation assay and a 24-hr microcytotoxicity assay. The cell lines tested were PANC-1, of human poorly differentiated pancreatic adenocarcinoma origin, and WD PaCa, of hamster well-differentiated pancreatic adenocarcinoma origin. The dose-survival curves and resulting determinations of drug dose (microgram/ml/1-hr exposure) at which there is a 50% inhibition of survival as compared to controls were compared for the two cell lines by each assay system. Lack of correlation of the two assays and considerable interdrug and inter-cell line variation were found. In addition, the microcytotoxicity assay was felt to underestimate the in vitro drug sensitivity of PANC-1 to three drugs (dactinomycin, doxorubicin, and mitoxantrone) and of WD PaCa to two drugs (5-fluorouracil and mitoxantrone). Despite the possible utility of the microcytotoxicity assay with other experimental models, the colony formation assay technique appears to provide the most reliable in vitro assessment of antineoplastic activity for pancreatic adenocarcinoma cell lines and should continue to be the standard to which other assay systems are compared. PMID:6850624

Chang, B K

1983-07-01

238

In Vitro RNase and Nucleic Acid Binding Activities Implicate Coilin in U snRNA Processing  

PubMed Central

Coilin is known as the marker protein for Cajal bodies (CBs), subnuclear domains important for the biogenesis of small nuclear ribonucleoproteins (snRNPs) which function in pre-mRNA splicing. CBs associate non-randomly with U1 and U2 gene loci, which produce the small nuclear RNA (snRNA) component of the respective snRNP. Despite recognition as the CB marker protein, coilin is primarily nucleoplasmic, and the function of this fraction is not fully characterized. Here we show that coilin binds double stranded DNA and has RNase activity in vitro. U1 and U2 snRNAs undergo a processing event of the primary transcript prior to incorporation in the snRNP. We find that coilin displays RNase activity within the CU region of the U2 snRNA primary transcript in vitro, and that coilin knockdown results in accumulation of the 3? pre-processed U1 and U2 snRNA. These findings present new characteristics of coilin in vitro, and suggest additional functions of the protein in vivo. PMID:22558428

Broome, Hanna J.; Hebert, Michael D.

2012-01-01

239

Sertaconazole: in-vitro antifungal activity against vaginal and other superficial yeast isolates.  

PubMed

The in vitro susceptibilities of 183 clinical yeast isolates to sertaconazole (STZ) were compared to their susceptibilities to clotrimazole (CTZ), econazole (ECZ), ketoconazole (KTZ), miconazole (MNZ), fluconazole (FLZ), itraconazole (ITZ), tioconazole (TCZ), amphotericin B (AMB) and flucytosine (5FC) by using a commercial agar diffusion method. Strains were isolated from vaginal and other superficial clinical samples (18 species of Candida and five strains belonging to other yeast genera). Only one strain (0.5%) was resistant to STZ out of 87.4% of susceptible strains (n=160). The percentage of susceptible strains was higher than those obtained with the other agents evaluated and the percentage of resistant strains was lower than for most of the other antifungals. The pattern of susceptibility of C. albicans to STZ, TCZ, ITZ and CLZ was similar and superior to the pattern of susceptibility of this species to MNZ, ECZ, FLZ, 5FC and KTZ. C. dubliniensis was more susceptible to STZ, MNZ, MNZ, FLZ, ITZ, CLZ than to TCZ, ECZ, 5FC, AMB or KTZ. Ten susceptible strains to STZ were resistant to FLZ and one strain was resistant to ITZ. The overall antifungal activity of STZ in vitro against a wide range of clinically important yeasts from vaginal and cutaneous samples indicates the therapeutic potential of this agent for the treatment of infections caused by these fungi. However, the activity of STZ and the clinical value of in vitro data need to be verified in human clinical trials. PMID:11760221

Carrillo-Muńoz, A J; Brió, S; Quindós, G; Palacín, C; Guglietta, A; Espinel-Ingroff, A

2001-10-01

240

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

241

In vitro antioxidant activity of non-cultivated vegetables of ethnic Albanians in southern Italy.  

PubMed

A total of 27 extracts from non-cultivated and weedy vegetables traditionally consumed by ethnic Albanians (Arbëreshë) in the Vulture area (southern Italy) were tested for their free radical scavenging activity (FRSA) in the DPPH (1,1-diphenyl-2-picrylhydrazil radical) screening assay, for their in vitro non-enzymatic inhibition of bovine brain lipid peroxidation and for their inhibition of xanthine oxidase (XO). In both antioxidant assays strong activity was shown for Leopoldia comosa (bulbs, syn.: Muscari comosum) and Centaurea calcitrapa (young whorls). In the lipid peroxidation assay, extracts from leaves of Origanum heracleoticum, Urtica dioica and Tordylium apulum showed a remarkable inhibitory activity (> 50%), too. In the case of Leopoldia comosa and Origanum heracleoticum this activity was comparable to quercetin (at a concentration of 50 microM) and Rhodiola rosea extract. Extracts from non-cultivated Cichorium intybus, Chondrilla juncea and Stellaria media showed strong in vitro inhibition of xanthine oxidase, with an activity higher than that of a reference extract from Ledum groenlandicum. These findings suggest that weedy vegetables may be useful antioxidants of interest in the prevention of ageing related diseases, CNS disorders and as potential sources of phytomedicines against hyperuricaemia and gout. PMID:12203269

Pieroni, A; Janiak, V; Dürr, C M; Lüdeke, S; Trachsel, E; Heinrich, M

2002-08-01

242

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

243

In vitro and in vivo antibacterial activities of CS-834, a new oral carbapenem.  

PubMed

CS-834 is a prodrug of the carbapenem R-95867, developed by Sankyo Co., Ltd., Tokyo, Japan. To investigate the possibility that CS-834 may be the first carbapenem usable in an oral dosage form, its in vitro antibacterial activity (as R-95867) and in vivo antibacterial activity were compared with those of cefpodoxime proxetil, cefditoren pivoxil, cefdinir, ofloxacin, imipenem, and amoxicillin. R-95867 had high levels of activity against methicillin-susceptible staphylococci and streptococci, including penicillin-resistant Streptococcus pneumoniae, as well as Neisseria gonorrhoeae, Moraxella catarrhalis, the members of the family Enterobacteriaceae (with the exception of Serratia marcescens), Haemophilus influenzae, and Bordetella pertussis; for all these strains, the MICs at which 90% of tested strains are inhibited (MIC90s) were 1.0 microg/ml or less. Against methicillin-resistant staphylococci, enterococci, Serratia marcescens, Burkholderia cepacia, Stenotrophomonas maltophilia, and Acinetobacter calcoaceticus, R-95867 showed activity comparable to or slightly less than that of imipenem, with MIC90s ranging from 2 to >128 microg/ml. The in vivo efficacy of oral CS-834 against experimental mouse septicemia caused by gram-positive and gram-negative bacteria was better than that of comparative drugs. In murine respiratory infection models, the efficacy of CS-834 reflected not only its potent in vitro activity but also the high levels present in the lungs. PMID:9517932

Yamaguchi, K; Domon, H; Miyazaki, S; Tateda, K; Ohno, A; Ishii, K; Matsumoto, T; Furuya, N

1998-03-01

244

In Vitro and In Vivo Antibacterial Activities of CS-834, a New Oral Carbapenem  

PubMed Central

CS-834 is a prodrug of the carbapenem R-95867, developed by Sankyo Co., Ltd., Tokyo, Japan. To investigate the possibility that CS-834 may be the first carbapenem usable in an oral dosage form, its in vitro antibacterial activity (as R-95867) and in vivo antibacterial activity were compared with those of cefpodoxime proxetil, cefditoren pivoxil, cefdinir, ofloxacin, imipenem, and amoxicillin. R-95867 had high levels of activity against methicillin-susceptible staphylococci and streptococci, including penicillin-resistant Streptococcus pneumoniae, as well as Neisseria gonorrhoeae, Moraxella catarrhalis, the members of the family Enterobacteriaceae (with the exception of Serratia marcescens), Haemophilus influenzae, and Bordetella pertussis; for all these strains, the MICs at which 90% of tested strains are inhibited (MIC90s) were 1.0 ?g/ml or less. Against methicillin-resistant staphylococci, enterococci, Serratia marcescens, Brukholderia cepacia, Stenotrophomonas maltophilia, and Acinetobacter calcoaceticus, R-95867 showed activity comparable to or slightly less than that of imipenem, with MIC90s ranging from 2 to >128 ?g/ml. The in vivo efficacy of oral CS-834 against experimental mouse septicemia caused by gram-positive and gram-negative bacteria was better than that of comparative drugs. In murine respiratory infection models, the efficacy of CS-834 reflected not only its potent in vitro activity but also the high levels present in the lungs. PMID:9517932

Yamaguchi, Keizo; Domon, Haruki; Miyazaki, Shuichi; Tateda, Kazuhiro; Ohno, Akira; Ishii, Kazuhiro; Matsumoto, Tetsuya; Furuya, Nobuhiko

1998-01-01

245

In Vitro Antioxidant and Anticancer Activity Studies on Drosera Indica L. (Droseraceae)  

PubMed Central

Purpose: The aim of present in vitro studies was performed to examine the antioxidant and anticancer activities of ethanol and aqueous extracts of Drosera indica L. Methods: Different concentrations (5 – 640mcg/ml) of the ethanol (EEDI) and aqueous (AEDI) extracts of D.indica L were used in various antioxidant assay methods such as hydroxyl radicals, DPPH, super oxide radical scavenging activity, chelating ability of ferrous ion, nitric oxide radical inhibition, ABTS and reducing power. Ascorbic acid (AA) was used as the standard antioxidant for the free radical scavenging assays. Dalton’s Ascitic Lymphoma (DAL) and Ehrlich Ascitic Carcinoma (EAC) cell lines were used as the in vitro cancer models for the tryphan blue dye and LDH leakage assays, where 5 to 250mcg /ml of both EEDI and AEDI were tested. Results: EEDI showed antioxidant activities with the minimum IC50 values of 34.8±0.43 mcg/ml in scavenging of hydroxyl radical and moreover AEDI showed minimum IC50 values of 94.51±0.84 mcg/ml in Fe2+chelating assay. EEDI on the reducing power assay and ABTS showed higher IC50 than standard AA. IC50 values of AEDI on Fe2+ chelating assay and super oxide radical assay was lesser than IC50 value of AA. Both extracts at 250mcg/ml dose showed remarkable increase in the percentage of dead cancer cells (90% by EEDI and 86% by AEDI in DAL model and 89% by EEDI and 80% by AEDI in EAC model). Conclusion: It is concluded from this study that D.indica L exhibited excellent antioxidant activity against the different in vitro antioxidant models and anticancer activity against the two different cell lines tested. PMID:24312822

Asirvatham, Raju; Christina, Arockiasamy Josphin Maria; Murali, Anita

2013-01-01

246

Highly compacted chromatin formed in vitro reflects the dynamics of transcription activation in vivo.  

PubMed

High-order chromatin was reconstituted in vitro. This species reflects the criteria associated with transcriptional regulation in vivo. Histone H1 was determinant to formation of condensed structures, with deacetylated histones giving rise to highly compacted chromatin that approximated 30 nm fibers as evidenced by electron microscopy. Using the PEPCK promoter, we validated the integrity of these templates that were refractory to transcription by attaining transcription through the progressive action of the pertinent factors. The retinoic acid receptor binds to highly compacted chromatin, but the NF1 transcription factor binds only after histone acetylation by p300 and SWI/SNF-mediated nucleosome mobilization, reflecting the in vivo case. Mapping studies revealed the same pattern of nucleosomal repositioning on the PEPCK promoter in vitro and in vivo, correlating with NF1 binding and transcription. The reconstitution of such highly compacted "30 nm" chromatin that mimics in vivo characteristics should advance studies of its conversion to a transcriptionally active form. PMID:20385088

Li, Guohong; Margueron, Raphael; Hu, Guobin; Stokes, David; Wang, Yuh-Hwa; Reinberg, Danny

2010-04-01

247

In Vitro Activities of Aminomethyl-Substituted Analogs of Novel Tetrahydrofuranyl Carbapenems  

PubMed Central

CL 188,624, CL 190,294, and CL 191,121 are novel aminomethyl tetrahydrofuranyl (THF)-1?-methylcarbapenems. The in vitro antibacterial activities of these THF carbapenems were evaluated and compared with those of biapenem, imipenem, and meropenem against 554 recent clinical isolates obtained from geographically distinct medical centers across North America. The antibacterial activities of the THF carbapenems were equivalent to that of biapenem, and the THF carbapenems were slightly more active than imipenem and less active than meropenem against most of the members of the family Enterobacteriaceae but lacked significant activity against Pseudomonas isolates. In general, CL 191,121 was two- to fourfold more active than CL 188,624 and CL 190,294 against the staphylococcal and enterococcal isolates tested. CL 191,121 was twofold less active than imipenem against methicillin-susceptible staphylococci and was as activity as imipenem against Enterococcus faecalis isolates. Biapenem and meropenem were two- and fourfold less active than CL 191,121, respectively, against the methicillin-susceptible staphylococci and E. faecalis. All the carbapenems displayed equivalent good activities against the streptococci. Biapenem was slightly more active than the other carbapenems against Bacteroides fragilis isolates. Time-kill curve studies demonstrated that the THF carbapenems were bactericidal in 6 h against Escherichia coli and Staphylococcus aureus isolates. The postantibiotic effect exerted by CL 191,121 was comparable to or slightly longer than that of imipenem against isolates of S. aureus, E. coli, and Klebsiella pneumoniae. PMID:10049250

Weiss, William J.; Petersen, Peter J.; Jacobus, Nilda V.; Lin, Yang-I; Bitha, Panayota; Testa, Raymond T.

1999-01-01

248

Plasma Lipoprotein Induction and Suppression of the Generation of Cellular Procoagulant Activity In Vitro  

PubMed Central

In the process of analyzing the effects of lipoproteins on functions of lymphoid cells, it was observed that physiological concentrations of isolated human plasma lipoproteins possess varying capacities to rapidly enhance the expression of procoagulant activity of human peripheral blood mononuclear cells in vitro. In a strict dose-dependent fashion, very low density lipoprotein, intermediate density lipoprotein, and high density lipoprotein enhanced both the surface expression by viable cells and the total cellular content of procoagulant activity during a 6-h incubation. Very low density lipoprotein induced a maximal 6.7-fold increase in the expression of a thromboplastin activity, which was consistent with tissue factor, in that it was dependent on Factors VII, X, and II. Both intermediate density lipoprotein and high density lipoprotein induced approximately a 12-fold increase of a different procoagulant activity which appears to be a direct prothrombin activator. This prothrombinase was calcium dependent and was inhibited by 2.5 mM diisopropylfluorophosphate, but was not neutralized by anti-Factor X antibodies or by inhibitors of Factor Xa. In contrast to the other lipoprotein density classes, low density lipoprotein did not stimulate procoagulant activity, but instead actively suppressed the generation of the two procoagulant activities induced by the stimulatory lipoproteins. Suppression by low density lipoprotein was clearly evident at molar ratios of low density lipoprotein to stimulatory lipoproteins of 1:3 or less. Reconstitution of all lipoproteins to physiological concentrations was not stimulatory as a consequence of the suppressive effects of low density lipoprotein. These data indicate that isolated plasma lipoproteins are capable of regulating the expression of two different procoagulant activities of peripheral blood mononuclear cells in vitro. The possibility that these interactions may be implicated in the association between certain types of hyperlipoproteinemias and thromboembolic disease merits study. Images PMID:7240413

Schwartz, Bradford S.; Levy, Gary A.; Curtiss, Linda K.; Fair, Daryl S.; Edgington, Thomas S.

1981-01-01

249

Augmentation of human natural killer cell activity by cyclophosphamide in vitro.  

PubMed

Cyclophosphamide (CY) has been shown to modulate a number of immune responses. In the present study, we have examined the effect of CY on human natural killer (NK) cells in vitro. Lymphocytes from six normal volunteers were cultured alone or with CY in the medium containing human AB plasma, and their cytotoxicity was assessed against cells of K562. The results demonstrated that lymphocytes when cultured with CY had 154 to 333% increase in NK cell activity as compared to lymphocytes that were cultured in the absence of CY. Similarly, CY markedly boosted the cytotoxic activity of lymphocytes from two healthy donors against cells from cultured B-leukemia 3163. Maximal augmentation occurred in cultured lymphocytes that expressed low levels of effector NK activity. Lymphocytes from 13 of 15 children with acute leukemia in remission when cultured alone had no reactivity to autologous leukemia cells. In the presence of CY, lymphocytes from eight of 15 of these patients developed cytotoxicity against autologous leukemia cells. CY was effective in augmenting NK cell activity at concentrations ranging from 7.5 to 60 micrograms/ml. Maximal potentiation of NK cell activity was induced after 8 hr of treatment with CY, although the increase in NK activity was started within 2 hr of incubation with CY. CY-activated NK cells were found in glass wool- and nylon wool-nonadherent cells. Treatment of lymphocytes with CY did not increase the extracellular levels of interferon. The results of this study demonstrate that CY can activate NK cells in vitro. The possible mechanisms of CY-induced augmentation of NK cell activity are discussed. PMID:6589041

Sharma, B; Vaziri, N D

1984-08-01

250

IN VITRO AND IN VIVO STUDY OF AN ANTIMICROBIAL ACTIVITY DISPLAYED BY THE REDMOUTH DISEASE AGENT, YERSINIA RUCKERI  

E-print Network

IN VITRO AND IN VIVO STUDY OF AN ANTIMICROBIAL ACTIVITY DISPLAYED BY THE REDMOUTH DISEASE AGENT of an antimicrobial factor secretion by Y ruckeri. As it was not possible to detail in a short note all our attempts

Paris-Sud XI, Université de

251

In vitro activity of R-95867, the active metabolite of a new oral carbapenem, CS-834, against anaerobic bacteria.  

PubMed

The in vitro activity of R-95867, the active metabolite of a new oral carbapenem, CS-834, was compared with those of DU-6859a, cefditoren, ampicillin/sulbactam and clindamycin against a variety of anaerobic bacteria. R-95867 inhibited 90% of anaerobic strains at active than DU-6859a but more active than other agents tested against strains of peptostreptococci, clostridia, the Bacteroides fragilis group, Porphyromonas spp. and fusobacteria. R-95867 was stable to hydrolysis by beta-lactamase type 2e derived from B. fragilis, Prevotella bivia and Prevotella intermedia, but unstable to hydrolysis by carbapenemase from B. fragilis. PMID:10702557

Kato, N; Tanaka, K; Kato, H; Watanabe, K

2000-03-01

252

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

253

[Trichomonacidal activity of newly synthesized derivatives of benzoizothiazolinon (BIT) in vitro].  

PubMed

Trichomonacidal activity in vitro of 2 newly synthesized derivatives of benzoizothiazolinon (BIT) in comparison with metronidazole was determined by calculating lethal concentration for 50% trichomonal population (C50). Experiments were carried out on 2 strains of T. vaginalis and 2 strains of T. anseris. Both preparations showed considerably higher trichomonacidal activity than metronidazole. Mean values of trichomonacidal activity of N-morpholinomethyl-1,2-benzoizothiazolinon-3 for T. vaginalis and T. anseris amounted to 885 and 1997 respectively, and were 6 and 8 times higher than those of hydrochloride of N-piperydynomethyloamide of (5-chloro-1,2-benzoizothiazolinon-3ylo-2)-acetic acid. The lowest trichomonacidal activity of hydrochloride of N-piperydynomethylamide of (5-chloro-1,2-benzoizotiazolinon-3ylo-2)-acetic acid was 10-fold higher than that of N-morpholinomethyl-1,2-benzoizothiazolinon-3 and several hundred times lower than metronidazole concentration. PMID:8023507

Ziomko, I; Kuczy?ska, E

1994-01-01

254

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

255

New antituberculotics originated from salicylanilides with promising in vitro activity against atypical mycobacterial strains.  

PubMed

A new series of 30 N-protected amino acid esters were prepared as a part of ongoing search for new anti-tuberculosis active salicylanilides. The esters possess high in vitro activity against Mycobacterium tuberculosis, Mycobacterium avium, and two strains of Mycobacterium kansasii, where one is an isolate from the patient, with MIC in the range 1-32 micromol/L for all tested strains. The prepared esters can be considered as prodrugs with better bio-availability and as more efficient transport forms through the mycobacterial cell membranes due to the higher lipophilicity. The experimental and calculated lipophilicity, stability, antituberculotic activity, cytotoxicity as well as the quantitative structure-activity relationships (QSARs) explored by the Intelligent Problem Solver (IPS) in Trajan Neural Network Simulator 6.0 are presented. PMID:19403314

Imramovský, Ales; Vinsová, Jarmila; Férriz, Juana Monreal; Dolezal, Rafael; Jampílek, Josef; Kaustová, Jarmila; Kunc, Filip

2009-05-15

256

In vitro antiprotozoal and cytotoxic activity of ethnopharmacologically selected guinean plants.  

PubMed

Based on an ethnobotanical survey, 41 Guinean plant species widely used in the traditional treatment of fever and/or malaria were collected. From these, 74 polar and apolar extracts were prepared and tested for their in vitro antiprotozoal activity along with their cytotoxicity on MRC-5 cells. A potent activity (IC50 activity (IC50 8.1?µg/mL) against Leishmania infantum. The selectivity index of the active samples varied from 0.08 to >?100. These results may validate at least in part the traditional use of some of the plant species. PMID:25180493

Traore, Mohammed Sahar; Diane, Sere; Diallo, Mamadou Saliou Telly; Balde, Elhadj Saďdou; Balde, Mamadou Aliou; Camara, Aďssata; Diallo, Abdoulaye; Keita, Abdoulaye; Cos, Paul; Maes, Louis; Pieters, Luc; Balde, Aliou Mamadou

2014-10-01

257

In vitro activity of thienyl-2-nitropropene compounds against Trypanosoma cruzi.  

PubMed

The in vitro activity of four 2-nitropropene derivatives, 1-(3-benzothienyl)-2-nitropropene (N1), 1-(3-thienyl)-2-nitropropene (N2), 1-(5-bromo-2-thienyl)-2-nitropropene (N3) and 1-(4-bromo-2-thienyl)-2-nitropropene (N4), were tested against cultures of the parasite Trypanosoma cruzi. Cytotoxicity studies were performed using Vero cells. The blood trypomastigotes, amastigotes and epimastigotes showed differential degrees of sensitivity towards the four tested compounds; the highest activity against the epimastigotes and blood tripomastigotes was exhibited by N1, followed by N3, N4 and finally N2. In contrast, whereas the compounds N1, N3 and N4 exerted similar magnitudes of activity against amastigotes, N2 was found to be a much less potent compound. According to our results, the compound N1 had the highest level of activity (IC50: 0.6 microM) against epimastigotes. PMID:20027464

Herrera, Cristina; Vallejos, Gabriel A; Loaiza, Randall; Zeledón, Rodrigo; Urbina, Andrea; Sepúlveda-Boza, Silvia

2009-11-01

258

SPECT/CT localization of oral radioiodine activity: a retrospective study and in-vitro assessment  

PubMed Central

Purpose We sought to further localize radioiodine activity in the mouth on post-thyroid cancer therapy imaging using single-photon emission computed tomography/computed tomography (SPECT/CT). Materials and methods We retrospectively reviewed all patients (58) who underwent thyroid cancer therapy with iodine-131 (131I) at our institution from August 2009 to March 2011 whose post-therapy radioiodine imaging included neck SPECT/CT. A small group (six) of diagnostic 123I scans including SPECT/CT was also reviewed. Separately, we performed in-vitro 131I (sodium iodide) binding assays with amalgam and Argenco HP 77 (77% dental gold alloy) as proof of principle for these interactions. Results Of the 58 post-therapy patients, 45 (78%) had undergone metallic dental restorations, and of them 41 (91%) demonstrated oral 131I activity localizing preferentially to those restorations. It was observed that radioiodine also localized to other dental restorations and to orthodontic hardware. Gum-line activity in edentulous patients suggests radioiodine interaction with denture adhesive. In vitro, dental amalgam and Argenco HP 77 bound 131I in a time-dependent manner over 1–16 days of exposure. Despite subsequent washings with normal saline, significant 131I activity (maximally 12% for amalgam and 68% for Argenco HP 77) was retained by these metals. Subsequent soaking in a saturated solution of potassium iodide partially displaced 131I from amalgam, with near-total displacement of 131I from Argenco HP 77. Conclusion SPECT/CT shows that radioiodine in the oral cavity localizes to metallic dental restorations. Furthermore, in-vitro studies demonstrate partially reversible binding of 131I to common dental metals. PMID:24128897

Burlison, Jared S.; Hartshorne, Michael F.; Voda, Alan M.; Cocks, Franklin H.

2013-01-01

259

MRN-100, an Iron-based Compound, Possesses Anti-HIV Activity In Vitro*  

PubMed Central

We examined the in vitro anti-human immunodeficiency virus (HIV) activity of MRN-100, an iron-based compound derived from bivalent and tervalent ferrates. MRN-100 action against HIV-1 (SF strain) was tested in primary cultures of peripheral blood mononuclear cells (MNC) by analyzing p24 antigen production and percent survival of MNC infected with HIV. MRN-100 at a concentration of 10% (v/v) inhibited HIV-1 replication in 11 out of 14 samples (79%). The percentage of suppression of p24 antigen was ?12.3 to 100% at 10 days post-treatment. MRN-100 also exhibited a significant protective effect in the survival of HIV-1-infected MNC. MNC survival post-treatment was dose dependent, 70.4% ± 8.4, 83.6% ± 10.7 and 90% ± 11.4, at concentrations 2.5, 5 and 10% (v/v), respectively, as compared with 53% ± 4 for HIV-1-infected MNC without treatment. The effect was detected as early as 4 days and continued up to 11 days. Treatment with MRN-100 caused no significant change in proliferative response of MNC alone or cocultured with different mitogens: PHA and Con-A (activators of T cell function) and PWM (activator of CD4+ T cell-dependent B cells). We concluded that MRN-100 possesses anti-HIV activity in vitro and without an increase in lymphocyte proliferation, MRN-100 may be a useful agent for treating patients with acquired immunodeficiency syndrome. PMID:18955328

Shaheen, Magda

2010-01-01

260

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

261

Potassium humate inhibits complement activation and the production of inflammatory cytokines in vitro.  

PubMed

The effects of brown coal derived potassium humate on lymphocyte proliferation, cytokine production and complement activation were investigated in vitro. Potassium humate increased lymphocyte proliferation of phytohaemaglutinin A (PHA) and pokeweed mitogen (PWM) stimulated mononuclear lymphocytes (MNL) in vitro from concentrations of 20 to 80 microg/ml, in a dose dependant manner. On the other hand potassium humate, at 40 microg/ml, significantly inhibited the release of TNF-alpha, IL-1beta, IL-6 and IL-10 by PHA stimulated MNL. Regarding complement activation it was found that potassium humate inhibits the activation of both the alternative and classical pathways without affecting the stability of the red blood cell membranes. These results indicate that the anti-inflammatory potential of potassium humate could be partially due to the inhibition of pro-inflammatory cytokines responsible for the initiation of these reactions as well as inhibition of complement activation. The increased lymphocyte proliferation observed, might be due to increased IL-2 production as previously been documented. PMID:19507015

van Rensburg, Constance E Jansen; Naude, Pieter J

2009-08-01

262

Synthesis, characterization and in vitro anti-diabetic activity of catechin grafted inulin.  

PubMed

In this study, a novel biological macromolecule with strong in vitro anti-diabetic activity was developed by grafting catechin onto inulin via a free radical mediated method. The characterization, ?-glucosidase and ?-amylase inhibitory activities of catechin grafted inulin (catechin-g-inulin) were investigated. Results showed that the grafting ratio of catechin-g-inulin was 124.8 mg CAE/g. UV-vis spectrum of catechin-g-inulin exhibited a new band at 280 nm, attributing to B ring of catechin moiety. FT-IR spectrum of catechin-g-inulin showed new absorption bands between 1540 and 1418 cm(-1), attributing to CC stretching vibration of catechin moiety. (1)H NMR spectrum of catechin-g-inulin preserved all the characteristic proton signals of inulin and partial signals of catechin. These all confirmed the successful grafting copolymerization. Conjugation probably occurred between OH of inulin (C-6) and H-6/H-8 of catechin (A ring). Catechin-g-inulin also exhibited increased thermal stability and crystallinity as compared to inulin. Moreover, in vitro anti-diabetic assays showed the ?-glucosidase inhibitory activity decreased in the order of catechin-g-inulin>catechin>acarbose>inulin, and ?-amylase inhibitory activity decreased in the order of catechin-g-inulin>acarbose>catechin>inulin. These indicated the potential of catechin-g-inulin in the development of a novel effective anti-diabetic agent. PMID:24315946

Liu, Jun; Lu, Jian-feng; Kan, Juan; Wen, Xiao-yuan; Jin, Chang-hai

2014-03-01

263

An in vitro study into the effect of zinc substituted hydroxyapatite on osteoclast number and activity.  

PubMed

Zinc ions have been shown to inhibit osteoclast development and proliferation both in vitro and in vivo. The same inhibiting effect has been observed in vitro when zinc was substituted into tri-calcium phosphate (TCP). Because of the solubility of TCP it is not an ideal candidate for a material to inhibit osteoclast activity in the long term. Hydroxyapatite (HA) is less soluble and so potentially offers a more long-term, sustainable effect. Previous work has shown that zinc can successfully be substituted into HA and still retain phase purity after heat treatment. The study reported here presents the effects of zinc substituted HA on the development and activity of osteoclast-like cells. It was found that increasing zinc substitution levels led to a decrease in the number of these cells present after 21 days. When resorption activity was investigated it was found that an increase in the amount of zinc present in the discs led to a significant decrease in the amount of resorption taking place on the discs. These results provide evidence for the potential of zinc substituted HA as a material to reduce resorptive activity to provide long-term bonding of implant to bone. © 2014 Wiley Periodicals, Inc. J Biomed Mater Res Part A: 102A: 4136-4141, 2014. PMID:24443251

Shepherd, David V; Kauppinen, Kyösti; Brooks, Roger A; Best, Serena M

2014-11-01

264

In vitro studies of the activity of dithiocarbamate organoruthenium complexes against clinically relevant fungal pathogens.  

PubMed

The in vitro antifungal activity of nine dirutheniumpentadithiocarbamate complexes C1-C9 was investigated and assessed for its activity against four different fungal species with clinical interest and related to invasive fungal infections (IFIs), such as Candida spp. [C. albicans (two clinical isolates), C. glabrata, C. krusei, C. parapsolisis, C. tropicalis, C.dubliniensis (six clinical isolates)], Paracoccidioides brasiliensis (seven clinical isolates), Cryptococcus neoformans and Sporothrix schenckii. All synthesized complexes C1-C9 and also the free ligands L1-L9 were submitted to in vitro tests against those fungi and the results are very promising, since some of the obtained MIC (minimal inhibitory concentration) values were very low (from 10-6 mol mL-1 to 10-8 mol mL-1) against all investigated clinically relevant fungal pathogens, except for C. glabrata, that the MIC values are close to the ones obtained for fluconazole, the standard antifungal agent tested. Preliminary structure-activity relations (SAR) might be suggested and a strong influence from steric and lipophilic parameters in the antifungal activity can be noticed. Cytotoxicity assays (IC50) showed that the complexes are not as toxic (IC50 values are much higher-30 to 200 fold-than MIC values). These ruthenium complexes are very promising lead compounds for novel antifungal drug development, especially in IFIs, one of most harmful emerging infection diseases (EIDs). PMID:24879585

Donnici, Claudio L; Nogueira, Luciano J; Araujo, Maria Helena; Oliveira, Sheila Rodrigues; Magalhăes, Thais F F; Lopes, Miriam T P; Araújo e Silva, Ana Cândida; Ferreira, Ana Maria da Costa; Martins, Cleide V B; de Resende Stoianoff, Maria A

2014-01-01

265

In vitro activity of the tricyclic beta-lactam GV104326.  

PubMed Central

GV104326 is a novel tricyclic beta-lactam (a trinem or, formerly, tribactam). The in vitro activity of GV104326 was compared with those of cefuroxime, cefixime, amoxicillin, amoxicillin-clavulanic acid, cefpirome, and ciprofloxacin. GV104326 had in vitro activity generally similar to that of cefixime against members of the family Enterobacteriaceae (MIC at which 90% of the isolates are inhibited [MIC90], < or = 2 micrograms/ml), with cefuroxime and amoxicillin-clavulanic acid being 8- to 32-fold less active and with cefpirome being 4- to 8-fold more active against members of this family. The trinem had no activity against Pseudomonas aeruginosa or Stenotrophomonas maltophilia (MIC90, > 128 micrograms/ml) but was the most active agent against Acinetobacter calcoaceticus. GV104326 was particularly active against gram-positive cocci. Ninety percent of methicillin-susceptible Staphylococcus aureus strains were susceptible to 0.03 microgram of GV104326 per ml, making it the most active agent studied. Enterococci and Lancefield group A and B streptococci were generally equally or somewhat more susceptible to GV104326 than they were to amoxicillin. Streptococcus pneumoniae strains were highly susceptible to GV104326, and those strains which showed decreased susceptibility to penicillin were generally twofold more susceptible to the trinem than to amoxicillin. Haemophilus influenzae and Moraxella catarrhalis were highly susceptible to GV104326 (MIC90s, 0.12 and 0.03 microgram/ml, respectively). The anaerobes Clostridium perfringens, Bacteroides fragilis, and Peptostreptococcus spp. were more susceptible to the trinems (formerly tribactams) than to the other agents studied. PMID:8723475

Wise, R; Andrews, J M; Brenwald, N

1996-01-01

266

The ruthenium compound KP1339 potentiates the anticancer activity of sorafenib in vitro and in vivo?  

PubMed Central

KP1339 is a promising ruthenium-based anticancer compound in early clinical development. This study aimed to test the effects of KP1339 on the in vitro and in vivo activity of the multi-kinase inhibitor sorafenib, the current standard first-line therapy for advanced hepatoma. Anticancer activity of the parental compounds as compared to the drug combination was tested against a panel of cancer cell lines with a focus on hepatoma. Combination of KP1339 with sorafenib induced in the majority of all cases distinctly synergistic effects, comprising both sorafenib-resistant as well as sorafenib-responsive cell models. Several mechanisms were found to underlie these multifaceted synergistic activities. Firstly, co-exposure induced significantly enhanced accumulation levels of both drugs resulting in enhanced apoptosis induction. Secondly, sorafenib blocked KP1339-mediated activation of P38 signalling representing a protective response against the ruthenium drug. In addition, sorafenib treatment also abrogated KP1339-induced G2/M arrest but resulted in check point-independent DNA-synthesis block and a complete loss of the mitotic cell populations. The activity of the KP1339/sorafenib combination was evaluated in the Hep3B hepatoma xenograft. KP1339 monotherapy led to a 2.4-fold increase in life span and, thus, was superior to sorafenib, which induced a 1.9-fold prolonged survival. The combined therapy further enhanced the mean survival by 3.9-fold. Synergistic activity was also observed in the VM-1 melanoma xenograft harbouring an activating braf mutation. Together, our data indicate that the combination of KP1339 with sorafenib displays promising activity in vitro and in vivo especially against human hepatoma models. PMID:23790465

Heffeter, Petra; Atil, Bihter; Kryeziu, Kushtrim; Groza, Diana; Koellensperger, Gunda; Korner, Wilfried; Jungwirth, Ute; Mohr, Thomas; Keppler, Bernhard K.; Berger, Walter

2013-01-01

267

The Arabidopsis thaliana SERK1 Kinase Domain Spontaneously Refolds to an Active State In Vitro  

PubMed Central

Auto-phosphorylating kinase activity of plant leucine-rich-repeat receptor-like kinases (LRR-RLK's) needs to be under tight negative control to avoid unscheduled activation. One way to achieve this would be to keep these kinase domains as intrinsically disordered protein (IDP) during synthesis and transport to its final location. Subsequent folding, which may depend on chaperone activity or presence of interaction partners, is then required for full activation of the kinase domain. Bacterially produced SERK1 kinase domain was previously shown to be an active Ser/Thr kinase. SERK1 is predicted to contain a disordered region in kinase domains X and XI. Here, we show that loss of structure of the SERK1 kinase domain during unfolding is intimately linked to loss of activity. Phosphorylation of the SERK1 kinase domain neither changes its structure nor its stability. Unfolded SERK1 kinase has no autophosphorylation activity and upon removal of denaturant about one half of the protein population spontaneously refolds to an active protein in vitro. Thus, neither chaperones nor interaction partners are required during folding of this protein to its catalytically active state. PMID:23236403

aan den Toorn, Marije; Huijbers, Mieke M. E.; de Vries, Sacco C.; van Mierlo, Carlo P. M.

2012-01-01

268

Activities of psilostachyin A and cynaropicrin against Trypanosoma cruzi in vitro and in vivo.  

PubMed

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; Soeiro, Maria de Nazaré Correia

2013-11-01

269

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.

Maggiore, M.; Elissondo, M. C.

2014-01-01

270

Pancreatic lipase inhibitory activity of taraxacum officinale in vitro and in vivo  

PubMed Central

Obesity has become a worldwide health problem. Orlistat, an inhibitor of pancreatic lipase, is currently approved as an anti-obesity drug. However, gastrointestinal side effects caused by Orlistat may limit its use. In this study the inhibitory activities of dandelion (Taraxacum officinale) against pancreatic lipase in vitro and in vivo were measured to determine its possible use as a natural anti-obesity agent. The inhibitory activities of the 95% ethanol extract of T. officinale and Orlistat were measured using 4-methylumbelliferyl oleate (4-MU oleate) as a substrate at concentrations of 250, 125, 100, 25, 12.5 and 4 µg/ml. To determine pancreatic lipase inhibitory activity in vivo, mice (n=16) were orally administered with corn oil emulsion (5 ml/kg) alone or with the 95% ethanol extract of T. officinale (400 mg/kg) following an overnight fast. Plasma triglyceride levels were measured at 0, 90, 180, and 240 min after treatment and incremental areas under the response curves (AUC) were calculated. The 95% ethanol extract of T. officinale and Orlistat, inhibited, porcine pancreatic lipase activity by 86.3% and 95.7% at a concentration of 250 µg/ml, respectively. T. officinale extract showed dose-dependent inhibition with the IC50 of 78.2 µg/ml. A single oral dose of the extract significantly inhibited increases in plasma triglyceride levels at 90 and 180 min and reduced AUC of plasma triglyceride response curve (p<0.05). The results indicate that T. officinale exhibits inhibitory activities against pancreatic lipase in vitro and in vivo. Further studies to elucidate anti-obesity effects of chronic consumption of T. officinale and to identify the active components responsible for inhibitory activity against pancreatic lipase are necessary. PMID:20016719

Zhang, Jian; Kang, Min-Jung; Kim, Myung-Jin; Kim, Mi-Eun; Song, Ji-Hyun; Lee, Young-Min

2008-01-01

271

The Ability to Associate with Activation Domains in vitro is not Required for the TATA Box-Binding Protein to Support Activated Transcription in vivo  

NASA Astrophysics Data System (ADS)

The TATA box-binding protein (TBP) interacts in vitro with the activation domains of many viral and cellular transcription factors and has been proposed to be a direct target for transcriptional activators. We have examined the functional relevance of activator-TBP association in vitro to transcriptional activation in vivo. We show that alanine substitution mutations in a single loop of TBP can disrupt its association in vitro with the activation domains of the herpes simplex virus activator VP16 and of the human tumor suppressor protein p53; these mutations do not, however, disrupt the transcriptional response of TBP to either activation domain in vivo. Moreover, we show that a region of VP16 distinct from its activation domain can also tightly associate with TBP in vitro, but fails to activate transcription in vivo. These data suggest that the ability of TBP to interact with activation domains in vitro is not directly relevant to its ability to support activated transcription in vivo.

Tansey, William P.; Herr, Winship

1995-11-01

272

Developmental potential of human oocytes matured in vitro followed by vitrification and activation  

PubMed Central

Background Oocyte in vitro maturation (IVM) and cryopreservation at the time of routine ovarian tissue freezing may be offered to cancer patients as an additional option for fertility preservation. This study aimed to investigate the developmental capacity of oocytes isolated from unstimulated ovaries. Methods Immature oocytes (n = 63) from seven consenting premenopausal patients were analysed. Oocytes were collected during routine laparoscopic examination with biopsy of an ovary (cystic adnexal mass, n = 3; cervical adenocarcinoma, n = 2) or oophorectomy (sex reassignment surgery, n = 2) without previous stimulation of the ovaries. The stage of the patient’s menstrual cycle was not considered. Oocytes in all visible antral follicles were aspirated from ovaries, cultured in IVM medium and vitrified at the MII stage before being kept in liquid nitrogen for at least one month. After warming, oocytes were subjected to parthenogenetic activation by chemical stimulus. Their further development was recorded at intervals of 24 hours for up to 6 days of culture. Results 61.9% of oocytes matured in vitro within 48 hours. The survival rate after vitrification and warming was 61.5%. A total of 75% of surviving oocytes were able to respond to artificial activation, 44.4% of the parthenotes developed to early embryonic stage. However, only 1 in 18 (5.6%) of the resulting embryos reached blastocyst stage. Conclusions Oocytes matured in vitro from unstimulated ovaries seem to have limited developmental potential after cryopreservation and artificial activation. Although the outcome of IVM for non-stimulated oocytes is poor, it is currently the only chance besides cryopreservation of ovarian tissue for women for whom ovarian stimulation is not possible due to life circumstances. Based on our preliminary results, we suggest that the use of cryopreserved ovaries for fertility preservation in women with cancer warrants further investigation. PMID:23597104

2013-01-01

273

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

274

In vitro cytotoxic activity of menispermaceae plants against HeLa cell line  

PubMed Central

Background: Menispermaceae, a family of flowering plants, is a medium-sized family of 70 genera totaling 420 extant species, mostly of climbing plants. It has various medicinal properties, which are used in the Ayurvedic system of medicine. Plants belonging to this family are rich in alkaloids, especially bisbenzylisoquinoline type. The hypothesis of this study is that the bisbenzylisoquinoline alkaloids present in the selected plants may exhibit in vitro cytotoxic property. Aim: The present study is aimed at estimating the total alkaloidal content of methanolic extract of Cocculus hirsutus and Cissampelos pareira and evaluating the in vitro cytotoxic activity of both the extracts on the HeLa cell line. Settings and Design: Methanolic extracts of both the plants in the concentrations of 500, 250, 125, 62.5, and 31.25 ?g/ml were assessed for its cytotoxic activity by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Materials and Methods: Total alkaloidal content was studied for both the plants using ultraviolet-visible spectroscopy method. Methanol extracts of both the plants were tested for its inhibitory effect on HeLa cell line. Cytotoxicity of the plant extracts was evaluated by MTT assay. Nonlinear regression graph was plotted between % cell inhibition and Log10 concentration, and IC50 was determined using GraphPad Prism software. Results: Preliminary phytochemical studies confirm the presence of alkaloids in both the plants. The total alkaloids present in C. hirsutus and C. pareira were found to be 0.252%w/w and 0.1656%w/w respectively. The IC50 values of C. hirsutus and C. pareria were found to be 111 ?g/ml and 129.3 ?g/ml respectively. Conclusion: From this study, it is observed that C. hirsutus and C. pareira have in vitro cytotoxic activity against HeLa cell line.

Thavamani, B. Samuel; Mathew, Molly; Dhanabal, S. P.

2013-01-01

275

[ Active trypanocidal alkaloids, bisbenzylisoquinoles ii. active in vitro against trypanosoma cruzi the agent responsible for trypanosomiasis, south america].  

PubMed

Chagas disease caused by the protozoan Trypanosoma cruzi is an endemic parasitic disease in Central and South America. The chemotherapeutic agents against Trypanosoma cruzi (imidazol compounds, lampit and benznidazol) are not very convenient products. Since it is known that protozoan Trypanosoma are close to Leishmania we studied the action of 14 bisbenzylisoquinoline alkaloids, in vitro, on three strains of T. cruzi (Tulahuen, C8C11, and 1979 CL1). As in the case of Leishmania, gyrocarpine, daphnandrine and obaberine showed an interesting activity and we judge them to be worthy of in vivo assays. PMID:3075676

Fournet, A; Manjon, A M; Muńoz, V; Angelo, A; Bruneton, J; Hocquemiller, R; Cortes, D; Cavé, A

1988-12-01

276

In vitro activity of BAY 12-8039, a new fluoroquinolone.  

PubMed Central

The in vitro activity of BAY 12-8039, a new fluoroquinolone, was studied in comparison with those of ciprofloxacin, trovafloxacin (CP 99,219), cefpodoxime, and amoxicillin-clavulanate against gram-negative, gram-positive, and anaerobic bacteria. Its activity against mycobacteria and chlamydia was also investigated. BAY 12-8039 was active against members of the family Enterobacteriaceae (MIC at which 90% of strains tested were inhibited [MIC90S] < or = 1 microgram/ml, except for Serratia spp. MIC90 2 microgram/ml), Neisseria spp. (MIC90S, 0.015 microgram/ml), Haemophilus influenzae (MIC90, 0.03 microgram/ml), and Moraxella catarrhalis (MIC90, 0.12 micrgram/ml), and these results were comparable to those obtained for ciprofloxacin and trovafloxacin. Against Pseudomonas aeruginosa, the quinolones were more active than the beta-lactam agents but BAY 12-8039 was less active than ciprofloxacin. Strains of Stenotrophomonas maltophilia were fourfold more susceptible to BAY 12-8039 and trovafloxacin (MIC90S, 2 micrograms/ml) than to ciprofloxacin. BAY 12-8039 was as active as trovafloxacin but more active than ciprofloxacin against Streptococcus pneumoniae (MIC90, 0.25 microgram/ml) and methicillin-susceptible Staphylococcus auerus (MIC90S, 0.12 micrograms/ml). The activity of BAY 12-8039 against methicillin-resistant S. aureus (MIC90, 2 micrograms/ml) was lower than that against methicillin-susceptible strains. BAY 12-8039 was active against anaerobes (MIC90S < or = 2 micrograms/ml), being three- to fourfold more active against Bacteroides fragilis, Prevotella spp., and Clostridium difficile than was ciprofloxacin. Against Mycobacterium tuberculosis, BAY 12-8039 exhibited activity comparable to that of rifampin (MICs < or = 0.5 micrograms/ml). Against Chlamydia trachomatis and Chlamydia pneumoniae BAY 12-8039 was more active (MICs < or = 0.12 microgram/ml) than either ciprofloxacin or erythromycin and exhibited a greater lethal effect than either to these two agents. The protein binding of BAY 12-8039 was determined at 1 and 5 micrograms/ml as 30 and 26.4%, respectively. The presence of human serum (at 20 or 70%) had no marked effect on the in vitro activity of BAY 12-8039. PMID:8980763

Woodcock, J M; Andrews, J M; Boswell, F J; Brenwald, N P; Wise, R

1997-01-01

277

Determination of Untreated Whole-Milk Effects on In Vitro Antibacterial Activity  

PubMed Central

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.

1970-01-01

278

Cationic nanoparticles for delivery of amphotericin B: preparation, characterization and activity in vitro  

PubMed Central

Background Particulate systems are well known to be able to deliver drugs with high efficiency and fewer adverse side effects, possibly by endocytosis of the drug carriers. On the other hand, cationic compounds and assemblies exhibit a general antimicrobial action. In this work, cationic nanoparticles built from drug, cationic lipid and polyelectrolytes are shown to be excellent and active carriers of amphotericin B against C. albicans. Results Assemblies of amphotericin B and cationic lipid at extreme drug to lipid molar ratios were wrapped by polyelectrolytes forming cationic nanoparticles of high colloid stability and fungicidal activity against Candida albicans. Experimental strategy involved dynamic light scattering for particle sizing, zeta-potential analysis, colloid stability, determination of AmB aggregation state by optical spectra and determination of activity against Candida albicans in vitro from cfu countings. Conclusion Novel and effective cationic particles delivered amphotericin B to C. albicans in vitro with optimal efficiency seldom achieved from drug, cationic lipid or cationic polyelectrolyte in separate. The multiple assembly of antibiotic, cationic lipid and cationic polyelctrolyte, consecutively nanostructured in each particle produced a strategical and effective attack against the fungus cells. PMID:18462496

Vieira, Débora B; Carmona-Ribeiro, Ana M

2008-01-01

279

In vitro shear stress-induced platelet activation: sensitivity of human and bovine blood.  

PubMed

As platelet activation plays a critical role in physiological hemostasis and pathological thrombosis, it is important in the overall hemocompatibility evaluation of new medical devices and biomaterials to assess their effects on platelet function. However, there are currently no widely accepted in vitro test methods to perform this assessment. In an effort to develop effective platelet tests for potential use in medical device evaluation, this study compared the sensitivity of platelet responses to shear stress stimulation of human and bovine blood using multiple platelet activation markers. Fresh whole blood samples anticoagulated with heparin or anticoagulant citrate dextrose, solution A (ACDA) were exposed to shear stresses up to 40?Pa for 2?min using a cone-and-plate rheometer model. Platelet activation was characterized by platelet counts, platelet surface P-selectin expression, and serotonin release into blood plasma. The results indicated that exposure to shear stresses above 20?Pa caused significant changes in all three of the platelet markers for human blood and that the changes were usually greater with ACDA anticoagulation than with heparin. In contrast, for bovine blood, the markers did not change with shear stress stimulation except for plasma serotonin in heparin anticoagulated blood. The differences observed between human and bovine platelet responses suggest that the value of using bovine blood for in vitro platelet testing to evaluate devices may be limited. PMID:23738621

Lu, Qijin; Hofferbert, Bryan V; Koo, Grace; Malinauskas, Richard A

2013-10-01

280

Chemical composition and possible in vitro phytotoxic activity of Helichrsyum italicum (Roth) Don ssp. italicum.  

PubMed

The chemical composition of the essential oil of Helichrysum italicum (Roth) Don ssp. italicum, collected in the National Park of Cilento and Diano Valley, Southern Italy, was studied by means of GC and GC/MS. Forty four compounds of 45 constituents were identified in the oil, mainly oxygenated sesquiterpenes. The essential oil was evaluated for its potential in vitro phytotoxic activity against germination and early radicle elongation of radish and garden cress. The radicle elongation of radish was significantly inhibited at the highest doses tested, while germination of both seeds was not affected. PMID:21904272

Mancini, Emilia; De Martino, Laura; Marandino, Aurelio; Scognamiglio, Maria Rosa; De Feo, Vincenzo

2011-01-01

281

Activity in vitro of hydrogen peroxide vapour against Clostridium difficile spores.  

PubMed

Clostridium difficile spores are shed in high numbers by infected patients and are resistant to desiccation and some disinfectants. We explored the in vitro activity of hydrogen peroxide vapour (HPV) against several strains of C. difficile spores using a spore-carrier test. Spores were dried on polyvinyl chloride or laminate carriers at mean concentrations of 4.7-6.9 log(10) spores/carrier, which were then decontaminated using HPV. C. difficile was completely eradicated from the exposed carriers regardless of the C. difficile strain or surface used. HPV can be considered for the eradication of C. difficile spores from the hospital environment. PMID:22099497

Barbut, F; Yezli, S; Otter, J A

2012-01-01

282

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

283

In vitro and in vivo activities of sparfloxacin and reference drugs against Chlamydia pneumoniae  

Microsoft Academic Search

The activities of sparfloxacin and reference drugs againstChlamydia pneumoniae were compared by using in vitro and in vivo methods. The minimum inhibitory concentration (MIC) (?g\\/ml) ranges of sparfloxacin,\\u000a levofloxacin, tosufloxacin, grepafloxacin, AM-1155, DU-6859a, clarithromycin, azithromycin, and minocycline for sixC. pneumoniae strains (two standard and four clinical strains) were 0.031 to 0.063, 0.25 to 0.5, 0.063 to 0.125, 0.063 to 0.125,

Rinzo Soejima; Yoshihito Niki; Toshio Kishimoto; Naoyuki Miyashita; Yoshifumi Kubota; Katsuhisa Nakata

1995-01-01

284

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

285

Growth of ovine granulocyte-macrophage precursors in vitro without exogenous colony-stimulating activity  

SciTech Connect

Ovine granulocyte-macrophage colony-forming units (CFU-GM) from peripheral blood and bone marrow were cultured in vitro. The colony-stimulating activity (CSA) was provided by various conditioned-media previously reported to contain CSA and by homologous sheep serum (SS). The maximum number of CFU-GM was observed in the cultures containing SS without the addition of exogenous CSA. The CFU-GM appeared earlier in the cultures containing bone marrow cells when compared to the peripheral blood CFU-GM. Replacement of SS by bovine fetal serum resulted in suboptimal growth of ovine CFU-GM.

Chandra, P.; Joel, D.D.; Chanana, A.D.

1983-11-01

286

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

287

In vitro antifungal activity and mechanism of action of chitinase against four plant pathogenic fungi.  

PubMed

To determine why chitinase has different antifungal activity on different pathogenic fungi in vitro, we purified recombinant rice chitinase from Pichia pastoris and investigated its antifungal activity against four fungi - Rhizopus stolonifer (Ehrenb. et Fr.) Vuill, Botrytis squamosa Walker, Pythium aphanidermatum (eds.) Fitzp, and Aspergillus niger van Tiegh. Scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR) were used to analyze the surface microstructure and proportion of chitin in the cell wall of the four fungi, respectively. The results showed that the chitinase exhibited different antifungal activities against the four fungi, which was directly correlated to the surface microstructure and the proportion of chitin in the fungal cell wall. It will help understanding the antifungal mechanism of the recombinant chitinase and further determining its application scope on crop protection and post-harvest storage of fruits and vegetables. PMID:18720488

Yan, Ruixiang; Hou, Jianhua; Ding, Dongfeng; Guan, Wenqqiang; Wang, Cuiyan; Wu, Zhiqiang; Li, Minggang

2008-08-01

288

In vitro bactericidal activities of antimicrobial agents and morphologic changes on Prevotella bivia.  

PubMed

Prevotella bivia is common in pelvic inflammatory diseases. Parenteral antimicrobial agents have been widely used against those infections. We investigated the bactericidal activities of three cephalosporins, i.e. cefluprenam (CFLP), ceftazidime (CAZ) and cefotaxime (CTX) and of two other antimicrobial agents, i.e. clindamycin (CLDM) and imipenem (IPM) against P. bivia. We also investigated the in vitro morphological changes induced by these agents in P. bivia. Cephalosporins exhibited bactericidal activities against P. bivia and induced time- and concentration-dependent morphological changes in P. bivia (filamentation). CLDM and IPM also had bactericidal activities, but induced different morphologic alterations: formation of spheroblasts and lysis. These results confirm the fact that each antimicrobial agent has characteristic aspects. PMID:10473922

Mikamo, H; Sato, Y; Hayasaki, Y; Kawazoe, K; Izumi, K; Satoh, M; Kai, J; Tamaya, T

1999-01-01

289

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

290

Phosphorylated modification and in vitro antioxidant activity of Radix Hedysari polysaccharide.  

PubMed

Phosphorylated modification of a polysaccharide obtained from Radix Hedysari (RHP) was studied. Three phosphorylated polysaccharides (RHPP) with variable degrees of substitution (DS(p)) were obtained with 4-dimethylaminopyridine (DMAP) and N, N' Dicyclocarbodiimide (DCC) as catalyst. The structures of RHPP were characterized by FT-IR spectra and (13)C NMR spectra. Depending on different reaction time, RHPP showed different DS(p) ranging from 0.30 to 0.66, and different Mw ranging from 86.6 to 89.7 KDa. Compared with RHP, RHPP exhibited superior antioxidant activities in vitro, which indicated that phosphorylated modification could enhance antioxidant activities of RHP. Furthermore, it was obvious that the DS(p) had a significant effect on the antioxidant activity. PMID:22535466

Wei, Dongfeng; Cheng, Weidong; Wei, Yanxia; Zhang, Lifeng

2012-05-01

291

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

292

In Vitro ?-Amylase Inhibition and Antioxidant Activities of Methanolic Extract of Amaranthus Caudatus Linn  

PubMed Central

Objectives The present study was aimed to investigate the ?-amylase inhibition and antioxidant activities of methanolic extract of Amaranthus caudatus Linn (MeAc). Methods Methanolic extract of Amaranthus caudatus was screened for ?-amylase inhibition activity by CNPG3 method (2-chloro-p-nitrophenyl-?-D-maltotrioside) and antioxidant activity was evaluated by 1,1-diphenyl-2-picryl-hydrazile (DPPH) free radical scavenging, superoxide dismutase (SOD) scavenging, hydroxyl free radical scavenging, nitric oxide (NO) radical scavenging, and 2.2’-azinobis-3-ethylbenzothiazole-6-sulfonic acid (ABTS) radical scavenging assays. MeAc was also screened for non enzymatic hemoglycosylation. Results The methanolic extract of Amaranthus caudatus showed potent ?-amylase inhibition activity (IC50 19.233 µg/ml). MeAc showed significant antioxidant activity in all the in vitro antioxidant models. Furthermore, the MeAc was found to be extremely effective in scavenging ABTS radical activity (IC50 48.75±1.1 µg/ml) when compared to DPPH (IC50 77.5±0.4 µg/ml), SOD (IC50 62.5±2.1 µg/ml), hydroxyl (IC50 88.50±1.8 µg/ml) and NO (IC50 67.5±2.2 µg/ml) scavenging activity. Conclusions The methanolic extract of A. caudatus showed potent ?-amylase inhibition and antioxidant activities. PMID:22043408

Kumar, Ashok; Khan, Saleemulla

2011-01-01

293

Comparative activity of macrolides against Toxoplasma gondii demonstrating utility of an in vitro microassay.  

PubMed Central

The utility of spiramycin for preventing transplacental transmission of toxoplasmosis and the efficacy of conventional macrolides against Toxoplasma gondii are subjects of active debate. An in vitro microassay was developed to determine the relative inhibitory activity against T. gondii of 24 conventional macrolides derived from erythromycin and tylosin (14- and 16-membered macrolides, respectively). Macrolides and T. gondii RH tachyzoites were added to monolayers of BT cells grown in 96-well plates. Plates were incubated for 20 h at 37 degrees C, and the growth of T. gondii was then measured by the selective incorporation of [3H]uracil in trichloroacetic acid-precipitable material during an additional incubation of 20 h. Dose-response curves and 50 and 90% inhibitory concentrations (IC50 and IC90, respectively) were determined for each drug. Microscopic examination was performed on stained replicates of the infected monolayers, and the relative toxicities of the drugs for host cells were determined. Spiramycin and tylosin showed only limited activity against T. gondii (IC50 of 20.16 and 20.00 micrograms/ml, respectively). Erythromycin and azithromycin had a better anti-Toxoplasma activity with IC50 of 14.38 and 8.61 micrograms/ml, respectively, whereas drugs like desmycosin, dirithromycin, and roxithromycin had no detectable activity. Although many macrolides inhibited intracellular proliferation of T. gondii, azithromycin was the only macrolide demonstrating prolonged inhibitory activity on the replication of intracellular tachyzoites. We conclude that conventional 14- and 16-membered macrolides often interfere with the growth of, but may not kill, T. gondii RH tachyzoites in vitro. Images PMID:1854172

Chamberland, S; Kirst, H A; Current, W L

1991-01-01

294

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

295

In Vitro and In Vivo Antibacterial Activities of DC-159a, a New Fluoroquinolone?  

PubMed Central

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. (MIC90, 0.12 ?g/ml) and inhibited the growth of 90% of levofloxacin-intermediate and -resistant strains at 1 ?g/ml. The MIC90s of DC-159a against Staphylococcus spp. were 0.5 ?g/ml or less. Against quinolone- and methicillin-resistant Staphylococcus aureus strains, however, the MIC90 of DC-159a was 8 ?g/ml. DC-159a was the most active against Enterococcus spp. (MIC90, 4 to 8 ?g/ml) and was more active than the marketed fluoroquinolones, such as levofloxacin, ciprofloxacin, and moxifloxacin. The MIC90s of DC-159a against Haemophilus influenzae, Moraxella catarrhalis, and Klebsiella pneumoniae were 0.015, 0.06, and 0.25 ?g/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 MIC90s of DC-159a against Peptostreptococcus spp., Clostridium difficile, and Bacteroides fragilis were 0.5, 4, and 2 ?g/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

296

Infliximab inhibits activation and effector functions of peripheral blood T cells in vitro from patients with clinically active ulcerative colitis.  

PubMed

Many patients with inflammatory bowel disease (IBD) are undergoing therapy with infliximab, an antibody specific for TNF. However, the exact mechanisms of action of infliximab are not completely understood. The aim of this study was to determine the in vitro effects of infliximab on blood T cells derived from anti-TNF therapy-naďve ulcerative colitis (UC) patients with clinically active disease. Peripheral blood mononuclear cells were stimulated polyclonally or by antigen in the presence or absence of infliximab. The T cell phenotype was investigated by flow cytometry, cytokine secretion was determined by ELISA, and cell proliferation was determined by thymidine assay or CFSE dye. Presence of infliximab resulted in reduced expression of CD25 in CD4(+) and CD8(+) T cell populations and inhibited secretion of IFN-?, IL-13, IL-17A, TNF as well as granzyme A. Infliximab also suppressed CD4(+) and CD8(+) T cell proliferation. These effects of infliximab were recorded both in T cells activated by polyclonal and antigen-specific stimulation. The effects of infliximab on T cell apoptosis and induction of FOXP3(+) CD4(+) T regulatory cells were ambiguous and depended on the originating cellular source and/or the stimulation mode and strength. In conclusion, infliximab is able to reduce T cell activation as measured by CD25, proliferation and cytokine secretion in vitro from UC patients with clinically active disease. These data suggest that suppression of T cell activity may be important for infliximab-mediated disease remission in patients with UC. PMID:23713660

Dahlén, R; Strid, H; Lundgren, A; Isaksson, S; Raghavan, S; Magnusson, M K; Simrén, M; Sjövall, H; Öhman, L

2013-09-01

297

Comparison of in vitro activities of meropenem productions on Klebsiella pneumoniae isolated from hospitalized patients  

PubMed Central

Purpose: Antimicrobial activities of meropenem products on Klebsiella pneumoniae isolates were determined. Methods: 212 non-duplicated Klebsiella pneumoniae isolates were examined for in vitro meropenem susceptibility test by using the following disks, which were made from Meronem (AstraZeneca, UK), Exipenem (Exir, Iran) and Meroxan (DAANA, Iran) powders. MIC50 and MIC90 for meropenem antibiotics were determined. Results: Meronem had good activities against most isolates of Klebsiella pneumoniae, and only a few strains had a rather high MIC. Exipenem and Meroxan showed a similar activity with Meronem. Conclusion: Regarding the comparison of two internal generic meropenem products with the external Meronem product have shown that they are equivalents in terms of microbiological activity, as measured using the disk diffusion and MIC. In developing countries, we suggested preparing disks with antibiotic powders that can be an equivalent function in microbiological activity with standard disks. In addition, since it demonstrated significant antimicrobial activity against the Klebsiella pneumoniae. For use of Exipenem and Meroxan in vivo, it would be better to perform additional testing (activity against different species, stability etc.). PMID:25152857

Akhi, Mohammad Taghi; Asghari, Babak; Nahaei, Mohammed Reza; Memar, Mohammad Yousef; Lari, Abdolaziz Rastegar; Naghili, Behrooz; Pirzadeh, Tahereh

2014-01-01

298

In vitro activity of N-formimidoyl thienamycin (MK0787), a crystalline derivative of thienamycin.  

PubMed Central

N-Formimidoyl thienamycin (MK0787) is a derivative of thienamycin, a unique, new beta-lactam antibiotic. Its activity against 285 aerobic and facultatively anaerobic clinical isolates was compared with the activities of cephalothin, ampicillin, penicillin G, ticarcillin, and tobramycin. All of the 285 isolates, with the exception of 1 Staphylococcus epidermidis isolate, were inhibited by a concentration of N-formimidoyl thienamycin of less than or equal to 8 micrograms/ml. More than 50% of all isolates were inhibited by the lowest concentration of N-formimidoyl thienamycin tested (0.125 micrograms/ml); 98% of Staphylococcus aureus and 80% of S. epidermidis isolates were inhibited by N-formimidoyl thienamycin at a concentration of 0.125 micrograms/ml. Only 2 of 45 enterococci were not inhibited by 1 microgram of N-formimidoyl thienamycin per ml, and this drug was the most active agent tested against 162 gram-negative bacilli. It inhibited more than 95% of the gram-negative isolates at a concentration of less than or equal to 2 micrograms/ml. N-Formimidoyl thienamycin was as active or more active than tobramycin against Escherichia coli, Pseudomonas aeruginosa, and Proteus mirabilis and substantially more active than ticarcillin. All 16 isolates of Klebsiella pneumoniae were inhibited by less than or equal to 0.5 micrograms of N-formimidoyl thienamycin per ml. The marked in vitro activity of this drug against a wide variety of clinical isolates makes it a promising new antibiotic. PMID:6934707

Horadam, V W; Smilack, J D; Montgomery, C L; Werringloer, J

1980-01-01

299

In vitro activity of E1210, a novel antifungal, against clinically important yeasts and molds.  

PubMed

E1210 is a new antifungal compound with a novel mechanism of action and broad spectrum of antifungal activity. We investigated the in vitro antifungal activities of E1210 compared to those of fluconazole, itraconazole, voriconazole, amphotericin B, and micafungin against clinical fungal isolates. E1210 showed potent activities against most Candida spp. (MIC(90) of ?0.008 to 0.06 ?g/ml), except for Candida krusei (MICs of 2 to >32 ?g/ml). E1210 showed equally potent activities against fluconazole-resistant and fluconazole-susceptible Candida strains. E1210 also had potent activities against various filamentous fungi, including Aspergillus fumigatus (MIC(90) of 0.13 ?g/ml). E1210 was also active against Fusarium solani and some black molds. Of note, E1210 showed the greatest activities against Pseudallescheria boydii (MICs of 0.03 to 0.13 ?g/ml), Scedosporium prolificans (MIC of 0.03 ?g/ml), and Paecilomyces lilacinus (MICs of 0.06 ?g/ml) among the compounds tested. The antifungal action of E1210 was fungistatic, but E1210 showed no trailing growth of Candida albicans, which has often been observed with fluconazole. In a cytotoxicity assay using human HK-2 cells, E1210 showed toxicity as low as that of fluconazole. Based on these results, E1210 is likely to be a promising antifungal agent for the treatment of invasive fungal infections. PMID:21825291

Miyazaki, Mamiko; Horii, Takaaki; Hata, Katsura; Watanabe, Nao-Aki; Nakamoto, Kazutaka; Tanaka, Keigo; Shirotori, Syuji; Murai, Norio; Inoue, Satoshi; Matsukura, Masayuki; Abe, Shinya; Yoshimatsu, Kentaro; Asada, Makoto

2011-10-01

300

In vitro anti-inflammatory and xanthine oxidase inhibitory activity of Tephrosia purpurea shoot extract.  

PubMed

The methanolic extract of Tephrosia purpurea (Leguminosae) shoots was evaluated in-vitro for its anti-inflammatory and xanthine oxidase inhibitory activity. Anti-inflammatory activity was measured by the Diene-conjugate, HET-CAM and beta-glucuronidase methods. The enzyme inhibitory activity was tested against isolated cow milk xanthine oxidase. The average anti-inflammatory activity of T. purpurea shoot extract in the concentration range of 1-2 microg/mL in the reacting system revealed significant anti-inflammatory activities, which, as recorded by the Diene-conjugate, HET-CAM and beta-glucuronidase assay methods, were 45.4, 10.5, and 70.5%, respectively. Screening of the xanthine oxidase inhibitory activity of the extract in terms of kinetic parameters revealed a mixed type of inhibition, wherein the Km and Vmax values in the presence of 25 to 100 microg/mL shoot extract was 0.20 mM/mL and 0.035, 0.026, 0.023 and 0.020 microg/min, while, for the positive control, the Km and Vmax values were 0.21 mM/mL and 0.043 microg/min, respectively. These findings suggest that T. purpurea shoot extract may possess constituents with good medicinal properties that could be exploited to treat the diseases associated with oxidative stress, xanthine oxidase enzyme activity and inflammation. PMID:22164776

Nile, Shivraj H; Khobragade, Chandrahasy N

2011-10-01

301

Effects of hydroxyethylrutosides on hypoxia-induced activation of human endothelial cells in vitro.  

PubMed Central

1. A clinically available mixture of hydroxyethylrutosides (HR) was examined as inhibitors of endothelial cell activation by hypoxia in vitro. Thus, the effects of HR on ATP depletion, phospholipase A2 activation and neutrophil adherence were investigated in hypoxia-activated human umbilical vein endothelial cells in primary cell culture. 2. Our results show that HR inhibited two important steps of the activation of endothelial cells by hypoxia: the decrease in ATP content, which is the starting point of the process, and the activation of phospholipase A2 one enzyme responsible for the release of inflammatory mediators. This inhibition was dose-dependent with 70 to 90% inhibition at 500 micrograms ml-1 of HR. 3. In addition, hypoxia-activated endothelial cells increased their adhesiveness for neutrophils. This process could also be prevented in a dose-dependent manner if endothelial cells were incubated in the presence of HR. This inhibition was confirmed by a morphological study. 4. In conclusion, the results of this study suggest that a possible explanation for the improvement in venous insufficiency by HR observed clinically could be their ability to inhibit the activation of endothelial cells during blood stasis. Images Figure 4 PMID:8762083

Janssens, D.; Michiels, C.; Arnould, T.; Remacle, J.

1996-01-01

302

In-vitro evaluation of anti-trichomonal activities of Eugenia uniflora leaf.  

PubMed

Eugenia uniflora, used ethnomedically in some tropical countries as an anti-infective, has shown anti-malarial and anti-trypanocidal activities. Therefore using bioactivity guided fractionation, anti-trichomonal activity of E. uniflora leaf was investigated. Anti-trichomonal activities of leaf methanol extract and its fractions against Trichomonas gallinae as well as their cytotoxicities using an in vitro haemaglutination assay were determined. Anti-trichomonacidal activities of the extract improved on purification up to a stage. Subfractions E(2-5) had LC(50) and LC(90) values of 4.77 - 5.28, 18.49 - 25.00 and 4.53 - 5.18, 18.32 - 19.07 µg/ml at 24 and 48 hrs, respectively that were better than those of metronidazole. Further purification of E(2-5) led to loss of activity suggesting that the active components were probably working synergistically and additively. Demonstration of low haemaglutination titre values of 0.00 - 5.33 by methanolic extract and its partition fractions suggested their low toxicity profile. The established safety of the leaf indicated that its anti-trichomonal activity was not due to non-specific cytotoxicity, hence could be used in ethnomedicine as an anti-trichomonal agent. PMID:22238499

Ibikunle, Gabriel Femi; Adebajo, Adeleke Clement; Famuyiwa, Funmilayo Gladys; Aladesanmi, Adetunji Joseph; Adewunmi, Clement Oladapo

2011-01-01

303

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; Araujo Meireles, Mario Carlos; Alves Rodrigues, Maria Regina; de Mello, Joao Roberto Braga

2010-01-01

304

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

305

In vitro activity of cefquinome, a new cephalosporin, compared with other cephalosporin antibiotics.  

PubMed

The in vitro activity of cefquinome, a new aminothiazolyl cephalosporin with a C-3 bicyclic pyridinium group, was compared with ceftazidime, cefpirome, and cefepime. Cefquinome inhibited members of the Enterobacteriaceae at less than or equal to 0.5 microgram/ml for Escherichia coli, Klebsiella pneumoniae, K. oxytoca, Citrobacter diversus, Salmonella Shigella, Proteus mirabilis, Morganella, and Providencia. Although most Citrobacter freundii and Enterobacter cloacae were inhibited by less than 2 micrograms/ml, some strains resistant to ceftazidime were resistant, [minimum inhibitory concentration (MIC) greater than 16 micrograms/ml]. Serratia marcescens were inhibited by less than 1 microgram/ml and Pseudomonas aeruginosa by 8 micrograms/ml similar to the activity of cefepime. The majority of Haemophilus influenzae and Neisseria gonorrhoeae were inhibited by less than 0.25 microgram/ml. Most enterococci had cefquinome MICs of 4-8 micrograms/ml. Cefquinome was extremely active against group-A streptococci and Streptococcus pneumoniae with MICs less than 0.12 microgram/ml. 90% of methicillin-susceptible Staphylococcus aureus 90% were inhibited by 2 micrograms/ml. Overall, the in vitro activity of cefquinome was comparable with aminothiazolyl cephalosporins. It inhibited some Enterobacter and Citrobacter freundii resistant to ceftazidime as did cefpirome and cefepime. Cefquinome was not destroyed by the common plasmid beta-lactamases TEM-1, TEM-2, SHV-1, or by the chromosomal beta-lactamases of Klebsiella, Branhamella, and Pseudomonas, but it was hydrolyzed by TEM-3, TEM-5, and TEM-9. Its activity was not adversely decreased in different medium or protein, and minimum bactericidal concentrations (MBCs) for most species except for Enterobacter were within a dilution of MICs. PMID:1611848

Chin, N X; Gu, J W; Fang, W; Neu, H C

1992-01-01

306

In vitro and in vivo antiproliferative and trypanocidal activities of ruthenium NO donors  

PubMed Central

Background and purpose: Many compounds liberating NO (NO donors) have been used as therapeutic agents. Here we test two ruthenium nitrosyls, which release NO when activated by biological reducing agents, for their effects in vitro and in vivo against Trypanasoma cruzi, the agent responsible for the American trypanosomiasis (Chagas' disease). Experimental approach: Ruthenium NO donors were incubated with a partially drug-resistant strain of T. cruzi and the anti-proliferative and trypanocidal activities evaluated. In a mouse model of acute Chagas' disease, trypanocidal activity was evaluated by measuring parasitemia, survival rate of infected mice and elimination of amastigotes in myocardial tissue. Key results: In vitro, the observed anti-proliferative and trypanocidal activities of trans-[Ru(NO)(NH3)4isn](BF4)3 and trans-[Ru(NO)(NH3)4imN](BF4)3 were due to NO liberated upon reduction of these nitrosyls. Ru(NO)isn had a lower IC50epi (67 ?M) than the NO donor, sodium nitroprusside (IC50epi=244 ?M) and Ru(NO)imN (IC50try=52 ?M) was more potent than gentian violet (IC50try=536 ?M), currently used in the treatment of blood. Both ruthenium nitrosyls eliminated, in vivo, extracellular as well as intracellular forms of T. cruzi in the bloodstream and myocardial tissue and allowed survival of up to 80% of infected mice at a dose (100 nmol kg?1 day?1) much lower than the optimal dose for benznidazole (385 ?mol kg?1 day?1). Conclusions and implications: Our data strongly suggest that NO liberated is responsible for the anti-proliferative and trypanocidal activities of the ruthenium NO donors and that these compounds are promising leads for novel and effective anti-parasitic drugs. PMID:17603548

Silva, J J N; Osakabe, A L; Pavanelli, W R; Silva, J S; Franco, D W

2007-01-01

307

Single Lysophosphatidylcholine Components Exhibit Adjuvant Activities In Vitro and In Vivo?  

PubMed Central

Improving vaccine immunogenicity by developing new adjuvant formulations has long been a goal of vaccinologists. It has previously been shown that a natural mix of lysophosphatidylcholine (LPC) from chicken eggs promotes mature dendritic cell (DC) generation in vitro and primes antigen-specific immune responses in mice. In the present study, we dissected the adjuvant potentials of five individual LPC components found in the chicken egg mixture. In vitro analyses of the impact of the individual components on the maturation of human DCs were performed by means of phenotypic analysis, chemokine secretion analysis, and analysis of the ability of mature DC to stimulate T lymphocytes. Two components, C16:0-LPC and C18:0-LPC, were identified to be capable of the upregulation of expression of CD86, HLA-DR, and CD40 on in vitro-cultured monocyte-derived DCs from healthy donors. Both induced the release of chemokines to high concentrations (macrophage inflammatory protein 1, monocyte chemoattractant protein 1) or moderate concentrations (interleukin-8 [IL-8], gamma interferon-inducible protein 10). In addition, C16:0-LPC engaged naďve T cells to produce gamma interferon. This suggests that C16:0-LPC and C18:0-LPC have the capacity to promote, at least in vitro, a Th1-oriented response. The intravenous injection of C16:0-LPC or C18:0-LPC into mice resulted in the detectable secretion of IL-6 and IL-5 in sera. Both LPC components were tested for their capacities to act as adjuvants for two selected immunogens: the hepatitis B virus surface antigen and the hepatitis C virus NS3 helicase. The secretion of specific IgG1 was observed with either or both C16:0-LPC and C18:0-LPC, depending on the immunogen tested, and was observed at an efficiency comparable to that of alum. These data identify C16:0-LPC and C18:0-LPC as the active components of the LPC natural mixture. Although discrepancies between the results of the in vitro and in vivo analyses existed, studies with animals suggest that these components can trigger significant and specific humoral-mediated immunity. PMID:20071492

Bach, Guillaume; Perrin-Cocon, Laure; Gerossier, Estelle; Guironnet-Paquet, Aurelie; Lotteau, Vincent; Inchauspe, Genevieve; Fournillier, Anne

2010-01-01

308

In vitro and ex vivo antihydroxyl radical activity of green and roasted coffee.  

PubMed

The specific antiradical activity against the hydroxyl radical of the water soluble components in green and dark roasted Coffea arabica and Coffea robusta coffee samples, both in vitro by the chemical deoxiribose assay and ex vivo in a biological cellular system (IMR32 cells), were determined. All the tested coffee solutions showed remarkable antiradical activity. In the deoxiribose assay, all the tested solutions showed similar inhibitory activity (IA%) against the sugar degradation (IA values ranged from 45.2 to 46.9%). In the cell cultures, the survival increase (SI%) ranged from 197.0 to 394.0% with C. robusta roasted coffee being significantly more active than the other samples. The coffee solutions underwent dialysis (3500 Da cutoff membrane) to fraction their components. In both systems, the dialysates (MW < 3500 Da) either from green or roasted coffee, showed antiradical activity, while the only retentates (MW > 3500 Da) from the roasted coffee samples were active. The preparative gel-filtration chromatography of roasted coffee C. robusta dialysate gave three fractions active in the biological system, all containing chlorogenic acid derivatives. The most active fraction was found to be that containing the 5-O-caffeoilquinic acid, which shows a linear relation dose-response ranging from 0.02 to 0.10 mM. The results show that both green and roasted coffee possess antiradical activity, that their more active component is 5-O-caffeoyl-quinic acid, and moreover that roasting process induces high MW components (later Maillard reaction products, i.e., melanoidins), also possessing antiradical activity in coffee. These results could explain the neuroprotective effects found for coffee consumption in recent epidemiological studies. PMID:15030233

Daglia, Maria; Racchi, Marco; Papetti, Adele; Lanni, Cristina; Govoni, Stefano; Gazzani, Gabriella

2004-03-24

309

In Vitro Intracellular Activity and In Vivo Efficacy of Modithromycin, a Novel Bicyclolide, against Legionella pneumophila?  

PubMed Central

The in vitro and in vivo activities of modithromycin, a novel bicyclolide, against Legionella pneumophila were compared with those of telithromycin, clarithromycin, azithromycin, and levofloxacin. All the test agents decreased the intracellular growth of viable L. pneumophila bacteria over 96 h of incubation in both types of cells used, A/J mouse-derived macrophages and A549 human alveolar epithelial cells, at extracellular concentrations of 4× and 16× MIC, respectively. However, when the agents were removed from the medium after exposure for 2 h, regrowth of intracellular bacteria occurred in both cell systems when they were exposed to telithromycin, clarithromycin, and levofloxacin but not when they were exposed to modithromycin and azithromycin. Once-daily administration of modithromycin at a dose of 10 mg/kg of body weight for 5 days led to a significant decrease of intrapulmonary viable L. pneumophila bacteria in immunosuppressed A/J mice. The efficacy of modithromycin was superior to the efficacies of telithromycin and clarithromycin and comparable to the efficacies of azithromycin and levofloxacin. In addition, modithromycin and azithromycin inhibited the intrapulmonary regrowth of bacteria even at 72 h after the last treatment, but telithromycin and levofloxacin did not. These results suggested that modithromycin has longer-lasting cellular pharmacokinetic features like azithromycin. In conclusion, modithromycin, as well as azithromycin, has excellent in vitro and in vivo bactericidal activities and persistent efficacy against intracellular L. pneumophila. Modithromycin should be a useful agent for treatment of pulmonary infections caused by this pathogen. PMID:21220530

Sato, Takafumi; Tateda, Kazuhiro; Kimura, Soichiro; Ishii, Yoshikazu; Yamaguchi, Keizo

2011-01-01

310

Microparticles containing propolis and metronidazole: in vitro characterization, release study and antimicrobial activity against periodontal pathogens.  

PubMed

Ethylcellulose microparticles containing metronidazole and propolis extractive solution were prepared and evaluated in vitro against periodontal pathogens. Scanning electron microscopy, particle size analysis, drug entrapment efficiency and drug release of microparticles were determined. The antimicrobial activity of microparticles was evaluated against microorganisms of periodontal importance (Enterococcus faecalis, Streptococcus pyogenes, Streptococcus mutans, Staphylococcus aureus, Klebsiella pneumoniae and Escherichia coli). It was obtained particles with regular morphology, mean diameter of 1.23?µm, and entrapment efficiency for propolis and metronidazole were 91.41% and 22.23%, respectively. In vitro release studies of propolis and metronidazole from microparticles showed prolonged drug release and controlled by Fickian diffusion. Both propolis and metronidazole displayed activity against the tested strains. Moreover, the results showed that the strains of E. faecalis, S. pyogenes and S. mutans were more susceptible to the propolis and E. faecalis to the metronidazole. It was also observed that the amount of metronidazole to inhibit the microorganism strains in the physical mixture with propolis was smaller than in the metronidazole alone, suggesting potentiation effect between propolis and metronidazole. These microparticles would be useful for developing intermediary or eventual dosage form to be administered into the periodontal pocket more easily and safely. PMID:23356908

de Souza Ferreira, Sabrina Barbosa; de Assis Dias, Bruno Rafael; Obregón, Clarissa Silva; Gomes, Carla Carolina; de Araújo Pereira, Raphaela Regina; Ribeiro Godoy, Janine Silva; Estivalet Svidzinski, Terezinha Inez; Bruschi, Marcos Luciano

2014-03-01

311

In vitro and in vivo antitumor activity of crude extracts obtained from Brazilian Chromobacterium sp isolates  

PubMed Central

Natural products produced by microorganisms have been an important source of new substances and lead compounds for the pharmaceutical industry. Chromobacterium violaceum is a Gram-negative ?-proteobacterium, abundant in water and soil in tropical and subtropical regions and it produces violacein, a pigment that has shown great pharmaceutical potential. Crude extracts of five Brazilian isolates of Chromobacterium sp (0.25, 2.5, 25, and 250?µg/mL) were evaluated in an in vitro antitumor activity assay with nine human tumor cells. Secondary metabolic profiles were analyzed by liquid chromatography and electrospray ionization mass spectrometry resulting in the identification of violacein in all extracts, whereas FK228 was detected only in EtCE 308 and EtCE 592 extracts. AcCE and EtCE 310 extracts showed selectivity for NCI/ADR-RES cells in the in vitro assay and were evaluated in vivo in the solid Ehrlich tumor model, resulting in 50.3 and 54.6% growth inhibition, respectively. The crude extracts of Chromobacterium sp isolates showed potential and selective antitumor activities for certain human tumor cells, making them a potential source of lead compounds. Furthermore, the results suggest that other compounds, in addition to violacein, deoxyviolacein and FK228, may be involved in the antitumor effect observed. PMID:23090123

Menezes, C.B.A.; Silva, B.P.; Sousa, I.M.O.; Ruiz, A.L.T.G.; Spindola, H.M.; Cabral, E.; Eberlin, M.N.; Tinti, S.V.; Carvalho, J.E.; Foglio, M.A.; Fantinatti-Garboggini, F.

2012-01-01

312

(-)-Epicatechin regenerates the chlorinating activity of myeloperoxidase in vitro and in neutrophil granulocytes.  

PubMed

The heme-containing enzyme myeloperoxidase (MPO) is mainly expressed in polymorphonuclear leukocytes (PMNs), the most abundant immune cell type in the blood. Accordingly, MPO is classically attributed to the innate immune response against pathogens. Yet, new results also show immune-regulatory functions of the halogenating MPO activity including the formation of anti-inflammatory mediators. In this work we tested the ability of the flavonoid (-)-epicatechin to regenerate this enzymatic activity both in vitro at the isolated MPO-H2O2-Cl(-) system and ex vivo in human PMNs. For all experiments the non-fluorescent dye aminophenyl fluorescein (APF) was used. Upon oxidation by the MPO, the halogenation product hypochlorous acid (HOCl) fluorescein is formed which can be detected e.g. by flow cytometry. The in vitro- and ex vivo-results concordantly show that (-)-epicatechin is a suitable substrate to overcome a compound II accumulation of MPO which was experimentally forced by applying excess hydrogen peroxide. Thereby concentration-dependent effects of the flavan-3-ol were found in both cases and confirmed the proposed mode of action of (-)-epicatechin. The results are in accordance with previous stopped-flow kinetic studies which showed a high reactivity of the polyphenol with MPO compound II. The obtained data may contribute to the explanation of the well-known health promoting effects of (-)-epicatechin. Moreover, the presented study provides new insights into the role of MPO during inflammation. PMID:24176923

Flemmig, Jörg; Remmler, Johannes; Röhring, Fiete; Arnhold, Jürgen

2014-01-01

313

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

314

Bufalin inhibits CYP3A4 activity in vitro and in vivo  

PubMed Central

Aim: To investigate the inhibitory interactions of bufalin and CYP3A4. Methods: Recombinant human CYP3A4 was incubated with bufalin in vitro. Bufalin was administered ig and iv to Wistar rats to further estimate its impact on CYP3A4, and midazolam was given to index the activity of CYP3A4. Results: The IC50 of bufalin was 14.52 ?mol/L. Bufalin affected CYP3A4 activity with increases in AUC0–t and t1/2, and decreases in CL and the formation of 1-hydroxy-midazolam after ig or iv administration of midazolam (P<0.05). An increase in Cmax after ig bufalin administration (P<0.05) was observed. Conclusion: Bufalin showed a modest but significant inhibition of CYP3A4 both in vitro and in vivo. The likelihood of an interaction between bufalin and the CYP3A4-metabolized drugs in human might not be negated. PMID:19417737

Li, Hai-yun; Xu, Wen; Zhang, Xi; Zhang, Wei-dong; Hu, Li-wei

2009-01-01

315

Neonatal Phosphate Nutrition Alters in Vivo and in Vitro Satellite Cell Activity in Pigs  

PubMed Central

Satellite cell activity is necessary for postnatal skeletal muscle growth. Severe phosphate (PO4) deficiency can alter satellite cell activity, however the role of neonatal PO4 nutrition on satellite cell biology remains obscure. Twenty-one piglets (1 day of age, 1.8 ± 0.2 kg BW) were pair-fed liquid diets that were either PO4 adequate (0.9% total P), supra-adequate (1.2% total P) in PO4 requirement or deficient (0.7% total P) in PO4 content for 12 days. Body weight was recorded daily and blood samples collected every 6 days. At day 12, pigs were orally dosed with BrdU and 12 h later, satellite cells were isolated. Satellite cells were also cultured in vitro for 7 days to determine if PO4 nutrition alters their ability to proceed through their myogenic lineage. Dietary PO4 deficiency resulted in reduced (P < 0.05) sera PO4 and parathyroid hormone (PTH) concentrations, while supra-adequate dietary PO4 improved (P < 0.05) feed conversion efficiency as compared to the PO4 adequate group. In vivo satellite cell proliferation was reduced (P < 0.05) among the PO4 deficient pigs, and these cells had altered in vitro expression of markers of myogenic progression. Further work to better understand early nutritional programming of satellite cells and the potential benefits of emphasizing early PO4 nutrition for future lean growth potential is warranted. PMID:22822445

Alexander, Lindsey S.; Seabolt, Brynn S.; Rhoads, Robert P.; Stahl, Chad H.

2012-01-01

316

Preliminary Phytochemical Screening and In Vitro Antioxidant Activities of Parkinsonia aculeata Linn.  

PubMed Central

Butanol and hexane leaves extracts of Parkinsonia aculeata L. (Fabaceae) were assessed for its antioxidant potential by in vitro methods. Phytochemical analysis and antioxidant activity of plant extracts were studied using different in vitro assays. UPLC analysis of extracts was carried out for the identification of chemical constituents. The total phenolic contents of the butanol and hexane leaf extract were 42?mgGAE/g and 34?mgGAE/g whereas flavonoid contents of these extracts were found to be 0.044?mgRE/g and 0.005?mgRE/g, respectively. Among both extracts, butanol extract shows maximum inhibition (%) of 93.88%, 80.02%, 52.06%, 94.68%, and 69.37% in DPPH, non-site-specific and site-specific, FTC, and TBA assays and absorbance of 0.852 and 0.522 in reducing power and CUPRAC assay at the highest concentration tested. The FRAP and TAC values of butanol extract were found to be 678??M Fe(II)/g and 36?mgAAE/100?mg. UPLC analysis of extracts revealed the presence of various polyphenols. The tested plant extracts were found to possess potent antioxidant and free radical scavenging activity which may be due to the presence of flavonoids and polyphenols. PMID:24822217

Sharma, Sonia; Vig, Adarsh Pal

2014-01-01

317

Evaluation of the immunomodulatory activities of royal jelly components in vitro.  

PubMed

In this work the effect of different components isolated from royal jelly (RJ) was studied using an in vitro rat T-cell proliferation assay. We found that lower concentrations of MEL 174 (final water extract of RJ) and MEL 147 (3-10-dihydroxydecanoic acid) stimulated T-cell proliferation, triggered by concanavalin A (Con-A) and the process was followed by an increase in the production of interleukin-2 (IL-2). Higher concentrations of MEL 174, MEL 247 (dry powder of RJ) and MEL 138 (trans-10-hydroxydec-2-enoic acid) inhibited T-cell proliferation. The inhibition of T-cell proliferation in the presence of MEL 174 was followed by a decrease in IL-2 production, which was partly abrogated by exogenous IL-2, a decrease in nitric oxide (NO) production and increased apoptosis. In conclusion, our results showed the complexity of biological activity of RJ and suggest that its water extract possesses the most potent immunomodulatory activity in vitro. PMID:18075862

Gasic, Sonja; Vucevic, Dragana; Vasilijic, Sasa; Antunovic, Mirjana; Chinou, Ioanna; Colic, Miodrag

2007-01-01

318

Activation of mononuclear bone marrow cells treated in vitro with a complex homeopathic medication.  

PubMed

Canova is a Brazilian homeopathic medication with immunomodulatory properties, recommended for patients where the immune system is depressed. Previous studies demonstrated that Canova induces up-regulation in numbers of leukocytes. The bone marrow microenvironment is composed of growth factors, stromal cells, extracellular matrix and progenitor cells that differentiate into mature blood cells. We now report the effect of in vitro administration of the medication on the mononuclear differentiation of the bone marrow cell. Swiss mice femurs were dissected cleaned and the cells of the marrow were flushed. The cells were plated, treated or not, incubated for different times and processed for light, transmission and scanning electron, and confocal microscopy analysis. Bone marrow cells showed an enhanced proliferation in vitro in response to Canova medication and Canova plus M-CSF and an increase was also observed in the numbers of the cell niches and ring-shaped nuclei cells. Confocal and transmission and scanning electron microscopy showed the stages of monocyte maturation, with resting and activated cells. With Canova treatment there was a marked increase in cell size, which is mainly attributable to the augmented cytoplasm, an increase in the number of mitochondria, expansion of the RER and an enlarged Golgi. The response to Canova treatment indicates that it influences mononuclear differentiation and activation of bone marrow progenitor and stromal cells. PMID:17379529

Cesar, Beatriz; Abud, Ana Paula R; de Oliveira, Carolina C; Cardoso, Francolino; Gremski, Waldemiro; Gabardo, Juarez; Buchi, Dorly de Freitas

2008-06-01

319

Antioxidant activities of saponins extracted from Radix Trichosanthis: an in vivo and in vitro evaluation  

PubMed Central

Background Radix Trichosanthis (RT), the dry root tuber of Trichosanthis kirilowii Maxim (Cucurbitaceae), is a traditional Chinese medicine. Although a wide range of saponin pharmacological properties has been identified, to our knowledge, this may be the first report to investigate the crude saponins from RT. The purpose of this study was to delineate the antioxidant activity both in vitro and in vivo by using ethyl acetate (EtOAc), n-butanol, and the mixture of n-butanol and EtOAc fractions. Methods In vitro antioxidant activity was detected by using DPPH free radical, hydrogen peroxide scavenging, and reducing power assays. After pretreatment with different fractions saponins at 2 mg/kg/d and 3 mg/kg/d of crude drug, respectively, an established CCl4 induced acute cytotoxicity model was used to evaluate the in vivo antioxidant potential by detection of superoxide dismutase (SOD), malonaldehyde (MDA), lactate dehydrogenase (LDH), and total antioxidant capacity (T-AOC) levels. Results The in vitro assay showed that the antioxidant activity of all the three fractions was promising. The reducing power of the EtOAc and the mixture of n-butanol and EtOAc extracts increased in a dose dependent manner. However, both the n-butanol and the mixture of n-butanol and EtOAc fractions in low dose exhibited in a time dependent manner with prolonged reaction time. As for hydrogen peroxide scavenging capability, the n-butanol fraction mainly demonstrated a time dependent manner, whereas EtOAc fraction showed a dose dependent manner. However, in case of in vivo assay, an increase of SOD and T-AOC and decrease of MDA and LDH levels were only observed in n-butanol (2 mg/kg/d of crude drug) extracts pretreatment group. Conclusions RT saponins in n-butanol fraction might be a potential antioxidant candidate, as CCl4-induced oxidative stress has been found to be alleviated, which may be associated with the time dependent manner of n-butanol saponins in a low dose. Further studies will be needed to investigate the active individual components in n-butanol extract, in vivo antioxidant activities and antioxidant mechanisms. PMID:24597831

2014-01-01

320

In vitro antifungal activity of sanguinarine and chelerythrine derivatives against phytopathogenic fungi.  

PubMed

In order to understand the antifungal activity of some derivatives of sanguinarine (S) and chelerythrine (C) and their structure-activity relationships, sixteen derivatives of S and C were prepared and evaluated for in vitro antifungal activity against seven phytopathogenic fungi by the mycelial growth rate method. The results showed that S, C and their 6-alkoxy dihydro derivatives S?-S?, C?-C? and 6-cyanodihydro derivatives S?, C? showed significant antifungal activity at 100 µg/mL against all the tested fungi. For most tested fungi, the median effective concentrations of S, S?, C and C? were in a range of 14-50 µg/mL. The structure-activity relationship showed that the C=N+ moiety was the determinant for the antifungal activity of S and C. S?-S? and C?-C? could be considered as the precursors of S and C, respectively. Thus, the present results strongly suggested that S and C or their derivatives S?-S? and C?-C? should be considered as good lead compounds or model molecules to develop new anti-phytopathogenic fungal agents. can't login to work station for 2hrs--took 2 hrs vacation PMID:23124471

Yang, Xin-Juan; Miao, Fang; Yao, Yao; Cao, Fang-Jun; Yang, Rui; Ma, Yan-Ni; Qin, Bao-Fu; Zhou, Le

2012-01-01

321

In Vitro Analysis of Finasteride Activity against Candida albicans Urinary Biofilm Formation and Filamentation.  

PubMed

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; Lee, Samuel A

2014-10-01

322

Comparison of in vitro activities of biotransformation enzymes in pig, cattle, goat and sheep.  

PubMed

In vitro activities of cytochromes P450 (7-alkyl/aryloxyresorufin dealkyl(aryl)ases, testosterone hydroxylase/oxidase, 6-chlorzoxazone hydroxylase, 7-methoxy-4-trifluoromethyl-coumarin demethylase, and lauric acid hydroxylases), reductases of carbonyl group (toward metyrapone, daunorubicin, glyceraldehyde, and 4-pyridine-carboxaldehyde) and conjugation enzymes (p-nitrophenol-UDP-glucuronosyl transferase, 1-chloro-2,4-dinitrobenzene glutathione-S-tranferase) in young adults, males, non-castrated (N=6) farm animals were studied and compared. Presence of proteins cross-reacting with anti-human CYP3A4, CYP2C9, and CYP2E1 IgG was detected in all farm species. Bovine microsomes differed from other microsomes of farm species in very high 7-ethoxyresorufin-O-deethylase activity (CYP1A1/2). Significantly higher 7-methoxy-4-trifluoromethyl-coumarin demethylase (2-3 times) and 12-lauric acid hydroxylases (4-10 times) activities (probably corresponding to CYP2C and CYP4A, respectively) were found in ovine microsomes. The highest 6beta-testosterone hydroxylase activity, which is usually considered to be a CYP3A activity marker, was found in pig. Reductases of all farm animals display considerable ability to reduce carbonyl group of xenobiotics. Significant differences in level and activity of many biotransformation enzymes tested suggest that extrapolation of pharmacokinetic data obtained in one species to another (even related) could be misleading. PMID:14659728

Szotáková, B; Baliharová, V; Lamka, J; Nozinová, E; Wsól, V; Velík, J; Machala, M; Neca, J; Soucek, P; Susová, S; Skálová, L

2004-02-01

323

Synthesis and in vitro antimicrobial activity of 1-methyl-3-sulfonylthio-4-aminoquinolinium chlorides.  

PubMed

Synthesis and in vitro antimicrobial activity (MIC) of novel 1-methyl-3-sulfonylthio-4-aminoquinolinium chlorides 2 are described. Compounds 2 were obtained in the reaction of 1-methyl-4-aminoquinolinium 3-thiolates 1 with sulfonyl chlorides. Antimicrobial activity of compounds 2 was investigated using Gram-positive Staphylococcus aureus, Staphylococcus saprophyticus, Staphylococcus epidermidis, Micrococcus luteus, Enterococcus faecalis, Bacillus subtilis, Corynebacterium pseudodiphtericum and Gram-negative Escherichia coil, Klebsiella pneumoniae, Proteus vulgaris, Serratia marcescens, Citrobacter freundii, Pseudomonas aeruginosa strains as well as Candida albicans. The investigated compounds exhibited growth-inhibitory activity towards Gram-positive bacteria in the 4-64 microg/mL range whereas that towards Gram-negative bacteria covered the 128-1024 microg/mL range. The highest activity was shown by compound 2c, featuring a phenylsulfonylthio substituent in the 3-quinoline position and a 4-chlorophenylamine group in the position 4. All of the investigated compounds 2 showed antifungal activity in the 32-128 microg/mL range. Correlations between antimicrobial activity and chemical structure of the tested compounds were observed. PMID:23610972

Zieba, Andrzej; Wojtyczka, Robert D; Idzik, Danuta; Kepa, Ma?gorzata

2013-01-01

324

In Vitro Activities of Three Nonfluorinated Quinolones against Representative Bacterial Isolates  

PubMed Central

In vitro susceptibility tests were performed to document the inhibitory activities of three nonfluorinated quinolone (NFQ) compounds (PGE 9262932, PGE 9509924, and PGE 4175997) compared to those of ciprofloxacin, levofloxacin, and trovafloxacin against 3,030 bacterial isolates. The spectra of the NFQ agents included most gram-positive species as well as quinolone-susceptible Enterobacteriaceae. Ciprofloxacin-resistant, methicillin-resistant Staphylococcus aureus strains were inhibited by the NFQ series at ?1.0 ?g/ml. The NFQ compounds were not very active against Pseudomonas aeruginosa and most other nonfermentative gram-negative bacilli. Against other species, the potency of the NFQ agents was similar to that of trovafloxacin. Continued investigation of the NFQ compounds seems to be warranted. PMID:11353655

Barry, Arthur L.; Fuchs, Peter C.; Brown, Steven D.

2001-01-01

325

Antiproliferative activities of interferons against human bladder carcinoma cell lines in vitro.  

PubMed

The antiproliferative effect of interferons against 5 human bladder carcinoma cell lines, RT112, T24, RT4, 647V and HT1197, was determined in vitro. Each of these human bladder carcinoma cell lines except 647V was sensitive to human interferons in liquid media. The antiproliferative effect of interferons was observed only upon continuous exposure, not after 1 hour. Partially purified, naturally produced interferon beta was more inhibitory of cell growth than naturally produced interferon alpha. Interferon alpha 54, 76, 61, 6L and 1 purified to homogeneity were as effective as naturally produced, partially pure interferon alpha. Although interferon beta, produced by recombinant DNA technology and purified to homogeneity, was not equivalent in effectiveness to naturally produced interferon beta, its antiproliferative activity was greater than interferon alpha 54 for 3 of 4 cell lines tested. Antimitotic effects may underlie, at least in part, the potential therapeutic activity of interferons for bladder carcinoma. PMID:6206246

Borden, E C; Groveman, D S; Nasu, T; Reznikoff, C; Bryan, G T

1984-10-01

326

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

327

Eco-friendly synthesis and in vitro antibacterial activities of some novel chalcones.  

PubMed

Chalcone derivatives have been synthesized by reaction of 1-(2,5-dimethyl-furan-3-yl)-ethanone with corresponding active aldehyde in ethanolic NaOH in microwave oven. The structure of these compounds was established by elemental analysis, IR, 1H-NMR, 13C-NMR, and EI-MS spectral analysis. The anti-bacterial activity of these compounds was first tested in vitro by the disc diffusion assay against two Gram-positive and two Gram-negative bacteria, and then the minimum inhibitory concentration (MIC) was determined with the reference of standard drug Chloramphenicol. The results showed that pyrazol containing chalcone (compound 8) inhibited both types of bacteria (Gram-positive and Gram-negative) better than chloramphenicol. PMID:24397034

Khan, Salman A; Asiri, Abdullah M; Alamry, Khalid A; El-Daly, Samy A; Zayed, Mohie A M

2013-01-01

328

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

329

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

330

Patterns of inspiratory phase-dependent activity in the in vitro respiratory network.  

PubMed

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; Ramirez, Jan-Marino

2013-01-01

331

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

332

In-vitro antifungal activity of sertaconazole, econazole, and bifonazole against Candida spp.  

PubMed

The in-vitro activity of sertaconazole (7-chloro-3-[1-(2,4-dichlorophenyl- 1-yl)ethoxy-methyl] benzo[b] thiophene) was compared with that of econazole and bifonazole against 150 strains of yeasts which includes six Candida species. Minimum inhibitory concentrations (MICs) were determined by a microdilution technique in Sabouraud's liquid medium, (pH 5.6). Sertaconazole (arithmetic mean MIC 0.77 mg/L) was more active than econazole (MIC 1.75 mg/L) and bifonazole (MIC 9.05 mg/L). MIC values for sertaconazole were generally and specifically lower for each tested species, Candida parapsilosis being the most susceptible (MIC 0.31 mg/L), in contrast to Candida tropicalis, which had the highest MIC (1.67 mg/L). PMID:8591947

Carrillo-Muńoz, A J; Torres-Rodriguez, J M

1995-10-01

333

In vitro and in vivo interactions of aluminum on NTPDase and AChE activities in lymphocytes of rats  

Microsoft Academic Search

Al adjuvants are used in vaccines to increase the immune response. NTPDase and AChE play a pivotal role and act in the regulation of the immune system. The effect of Al exposure in vitro and in vivo on NTPDase and AChE activities in the lymphocytes of rats was determined. In vitro, ATP hydrolysis was decreased by 20.4% and 17.3% and

Rosilene R. Kaizer; Jessié M. Gutierres; Roberta Schmatz; Rosélia M. Spanevello; Vera M. Morsch; Maria R. C. Schetinger; Joăo B. T. Rocha

2010-01-01

334

Antagonistic Activity against Helicobacter Infection In Vitro and In Vivo by the Human Lactobacillus acidophilus Strain LB  

Microsoft Academic Search

The purpose of the present study was to examine the activity of the human Lactobacillus acidophilus strain LB, which secretes an antibacterial substance(s) against Helicobacter pylori in vitro and in vivo. The spent culture supernatant (SCS) of the strain LB (LB-SCS) dramatically decreased the viability of H. pylori in vitro independent of pH and lactic acid levels. Adhesion of H.

MARIE-HELENE COCONNIER; VANESSA LIEVIN; ELISABETH HEMERY; ALAIN L. SERVIN

1998-01-01

335

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

336

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

337

Xenobiotic metabolizing enzyme activities in cells used for testing skin sensitization in vitro.  

PubMed

For ethical and regulatory reasons, in vitro tests for scoring potential toxicities of cosmetics are essential. A test strategy for investigating potential skin sensitization using two human keratinocytic and two human dendritic cell lines has been developed (Mehling et al. Arch Toxicol 86:1273–1295, 2012). Since prohaptens may be metabolically activated in the skin, information on xenobiotic metabolizing enzyme (XME) activities in these cell lines is of high interest. In this study, XME activity assays, monitoring metabolite or cofactor, showed the following: all three passages of keratinocytic (KeratinoSens® and LuSens) and dendritic (U937 und THP-1) cells displayed N-acetyltransferase 1 (NAT1) activities (about 6–60 nmol/min/mg S9-protein for acetylation of para-aminobenzoic acid). This is relevant since reactive species of many cosmetics are metabolically controlled by cutaneous NAT1. Esterase activities of about 1–4 nmol fluorescein diacetate/min/mg S9-protein were observed in all passages of investigated keratinocytic and about 1 nmol fluorescein diacetate/min/mg S9-protein in dendritic cell lines. This is also of practical relevance since many esters and amides are detoxified and others activated by cutaneous esterases. In both keratinocytic cell lines, activities of aldehyde dehydrogenase (ALDH) were observed (5–17 nmol product/min/mg cytosolic protein). ALDH is relevant for the detoxication of reactive aldehydes. Activities of several other XME were below detection, namely the investigated cytochrome P450-dependent alkylresorufin O-dealkylases 7-ethylresorufin O-deethylase, 7-benzylresorufin O-debenzylase and 7-pentylresorufin O-depentylase (while NADPH cytochrome c reductase activities were much above the limit of quantification), the flavin-containing monooxygenase, the alcohol dehydrogenase as well as the UDP glucuronosyl transferase activities. PMID:23958860

Fabian, E; Vogel, D; Blatz, V; Ramirez, T; Kolle, S; Eltze, T; van Ravenzwaay, B; Oesch, F; Landsiedel, R

2013-09-01

338

Suppression of aromatase activity in vitro by PCBs 28 and 105 and Aroclor 1221.  

PubMed

The effects of polychlorinated biphenyls (PCBs) on human cytochrome P450 aromatase activity in vitro were investigated using a commercially available microsomal fraction obtained from baculovirus infected insects that had been transfected with the human CYP19 gene and cytochrome P450 reductase. The assay measured the conversion of tritiated testosterone to estradiol in Tris buffer at pH 7.4. When aroclors, commercial preparations of PCBs, were added to aromatase assays at a 10 microM concentration, Aroclor 1221 caused a reduction in the aromatase activity, whereas other aroclors (1016, 1232, 1242, 1248, 1254, 1260, 5432, 5442 and 5460) were without effect. Further investigation of the effect of Aroclor 1221 on aromatase activity showed that the inhibition was dose dependent. When a reconstituted mixture (RM) of PCBs that represented the congeneric content of human milk was investigated, no inhibition of aromatase activity at the maximum treatment of 15.0 microM was observed. None of the congeners present in the reconstituted mixture, except PCB 28 and 105, affected P450 arom activity. PCB 28 showed a statistically significant inhibition of aromatase activity (P<0.05) at 1.5 and 15 microM and a significant inhibition of aromatase activity by PCB 105 was also observed, but only at 15 microM. In three separate kinetic analyses the Km(app) for aromatase was 64, 89 and 69 nM (mean 74 nM). In addition, PCB 28 resulted in an increase in the Km(app) without a significant effect on Vmax(app), suggesting competitive inhibition by this congener. This conclusion was supported by slope (Km(app)/Vmax(app) versus [inhibitor]) and intercept (1/Vmax(app) versus [inhibitor]) replots. The slope replots gave Ki(app) values for PCB 28 of 0.9, 1.3 and 2.0 microM (mean 1.4 microM), whereas intercept replots were almost horizontal. Thus, PCB 28 is a competitive inhibitor of aromatase with a Ki(app) value approximately 20-fold the Km(app) value. Based on these studies, we conclude that most PCBs are not inhibitors of aromatase activity in vitro. However, as being inhibitors of aromatase activity, Aroclor 1221, PCB 28 and PCB 105 would remain a priority for further study as possible endocrine disrupters. PMID:15294351

Woodhouse, Amanda J; Cooke, Gerard M

2004-08-30

339

Activation of VEGF and FGF induced angiogenesis under influence of low level laser radiation in vitro  

NASA Astrophysics Data System (ADS)

One of the feasible explanations for long-term treatment effects of laser therapy of diseases connected with tissue ischemia and altered blood circulation is activation of angiogenesis after low level laser irradiation. The aim of the current study was to investigate if laser irradiation can enhance vascular endothelial growth factor (VEGF) or basic fibroblast growth factor (FGF) induced angiogenesis in vitro. The study was conducted on rat thoracic aortal rings. Samples of group 1 served as control, samples of groups 2 and 3 were incubated with VEGF or FGF, group 4 samples were irradiated with laser (660 nm, 20 mW) during 10 min, samples of groups 5 and 6 were incubated with VEGF or FGF accordingly and received 10 min of laser irradiation. In the control group no noticeable angiogenesis occurred. The application of VEGF activated angiogenesis: the area covered by new vessels was 1,3+/-0,24 mm2 and the maximal length of vessels was 0,93+/-0,11 mm. Laser light irradiation (group 4) activated angiogenesis (1,9+/-0,29 mm2 and 0,75+/-0,10 mm). The combined influence of laser light and VEGF on angiogenesis (group 5) was significantly stronger (p <0,001), than each of the factors separately (6,98+/-0,88 mm2 and 1,7+/-0,23 mm). Application of FGF also activated angiogenesis: the area covered by new vessels was 2,76+/-0,22 mm2 and the maximal length of vessels was 1,19+/-0,12 mm. Combined influence of laser light and FGF on angiogenesis (group 6) was again significantly stronger (p <0,001), than each of the factors separately (5,43+/-0,28 mm2 and 1,99+/-0,10 mm). Studies show that laser irradiation can intensify effects of growth factors in vitro.

Gasparyan, Levon; Brill, Grigory; Makela, Anu

2006-02-01

340

What level of estrogenic activity determined by in vitro assays in municipal waste waters can be considered as safe?  

PubMed

In vitro assays are broadly used tools to evaluate the estrogenic activity in Waste Water Treatment Plant (WWTP) effluents and their receiving rivers. Since potencies of individual estrogens to induce in vitro and in vivo responses can differ it is not possible to directly evaluate risks based on in vitro measures of estrogenic activity. Estrone, 17beta-estradiol, 17alfa-ethinylestradiol and to some extent, estriol have been shown to be responsible for the majority of in vitro estrogenic activity of municipal WWTP effluents. Therefore, in the present study safe concentrations of Estrogenic Equivalents (EEQs-SSE) in municipal WWTP effluents were derived based on simplified assumption that the steroid estrogens are responsible for all estrogenicity determined with particular in vitro assays. EEQs-SSEs were derived using the bioassay and testing protocol-specific in vitro potencies of steroid estrogens, in vivo predicted no effect concentration (PNECs) of these compounds, and their relative contributions to the overall estrogenicity detected in municipal WWTP effluents. EEQs-SSEs for 15 individual bioassays varied from 0.1 to 0.4ng EEQ/L. The EEQs-SSEs are supposed to be increased by use of location-specific dilution factors of WWTP effluents entering receiving rivers. They are applicable to municipal wastewater and rivers close to their discharges, but not to industrial waste waters. PMID:24384232

Jarošová, Barbora; Bláha, Lud?k; Giesy, John P; Hilscherová, Klára

2014-03-01

341

Fast oscillatory activity induced by kainate receptor activation in the rat basolateral amygdala in vitro.  

PubMed

The basolateral amygdala (BLA) has a fundamental role in affective processing. In vivo studies have revealed rhythmic population activity of a similar type to that seen in the hippocampus and cortical areas during learning tasks. The amygdala contains densely interconnected networks of inhibitory interneurons similar to those responsible for fast network activity generation in the hippocampus and other cortical structures. Here we report that neuronal networks of the BLA in isolation generate persistent, gamma frequency (30-80 Hz) oscillations upon kainate receptor activation with kainic acid. We show that, like other cortical structures, BLA oscillations are completely dependent upon ?-aminobutyric acid (GABA)ergic inhibition. GABA(A) receptor blockade abolished all oscillations, and the activity was also sensitive to the barbiturate, pentobarbital. Blockade of ?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors or N-methyl-D-aspartate (NMDA) receptors had no significant effect on gamma activity. However, the GluR5-containing kainate receptor-specific antagonist (S)-1-(2-amino-2-carboxyethyl)-3-(2-carboxybenzyl) pyrimidine-2,4-dione (UBP302) abolished oscillations-evidence that glutamatergic receptor involvement is predominantly kainate receptor mediated. The mixed AMPA/kainate receptor antagonist 6-nitro-7-sulphamoylbenzo[f]quinoxalone-2,3-dione disodium (NBQX) abolished all oscillatory activity in 8/14 of slices tested. In the remaining slices, gamma frequency activity was abolished to reveal a low-amplitude, NMDA receptor-dependent, beta frequency (10-20 Hz) oscillation. Gamma oscillations are abolished by gap junction blockade. While these data show the BLA capable of generating gamma rhythms in common with other cortical areas studied to date, the network mechanisms appear to be different, suggesting a unique network structure underlies amygdala rhythmogenesis. Understanding how BLA networks produce synchronous activity is paramount to understanding how the BLA executes influence on important cognitive processes such as emotional learning. PMID:21255131

Randall, Fiona E; Whittington, Miles A; Cunningham, Mark O

2011-03-01

342

In Vitro Antituberculosis Activities of ACH-702, a Novel Isothiazoloquinolone, against Quinolone-Susceptible and Quinolone-Resistant Isolates?  

PubMed Central

ACH-702 is a new isothiazoloquinolone with potent in vitro and in vivo activities against important bacterial pathogens, including Staphylococcus aureus. In this study, ACH-702 was found to have promising in vitro antibacterial activity against Mycobacterium tuberculosis, with MICs of ?1 ?g/ml, comparable to that of the fluoroquinolone moxifloxacin for quinolone-susceptible isolates but superior to that for quinolone-resistant isolates. Biochemical assays involving M. tuberculosis gyrase enzymes indicated that ACH-702 had significantly improved inhibitory activity compared with fluoroquinolones. PMID:20516287

Pucci, Michael J.; Ackerman, Maria; Thanassi, Jane A.; Shoen, Carolyn M.; Cynamon, Michael H.

2010-01-01

343

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

Mladenovic, Milan; Mihailovic, Mirjana; Bogojevic, Desanka; Matic, Sanja; Niciforovic, Neda; Mihailovic, Vladimir; Vukovic, Nenad; Sukdolak, Slobodan; Solujic, Slavica

2011-01-01

344

In vitro activity of pyronaridine against field isolates and reference clones of Plasmodium falciparum.  

PubMed

Pyronaridine, a 9-substituted 1-aza-acridine, was assayed for in vitro activity against clinical and field isolates as well as characterized clones of Plasmodium falciparum. The in vitro antimalarial activity of pyronaridine was compared to activities of standard antimalarials against multidrug-resistant isolates of P. falciparum from eastern and northern Thailand using an assay based on the inhibition of schizont maturation. Isolates from eastern Thailand (n = 30) were susceptible to pyronaridine (IC50 8.40 nM), mefloquine (IC50 6.97 nM), and amodiaquine (IC50 12.7 nM) and resistant to chloroquine (IC50 361 nM), quinine (IC50 388 nM), and pyrimethamine (IC50 11,800 nM). The isolates from northern Thailand (n = 7) showed no statistical difference in susceptibility to pyronaridine (IC50 10.1 nM), amodiaquine (IC50 7.29 nM), and mefloquine (IC50 5.48 nM); however, isolates were significantly more susceptible to chloroquine (IC50 167 nM), quinine (IC50 248 nM), and pyrimethamine (IC50 1,980 nM). These data suggest a lack of cross-resistance between pyronaridine and either chloroquine, quinine, or pyrimethamine. Using the same assay system the in vitro activity of pyronaridine was evaluated against isolates from treatment failures of mefloquine or enpiroline from eastern Thailand. The IC50 values for mefloquine against five recrudescent isolates were significantly higher (IC50 16.4 nM) than the field isolates collected from the same region (IC50 6.97 nM); however, there was no significant difference in the pyronaridine susceptibility between the isolates from the field study (IC50 8.89 nM) and the isolates from the treatment failures (IC50 8.40 nM). These observations suggest a lack of cross-resistance to mefloquine following treatment failure with either mefloquine or enpiroline.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:3277460

Childs, G E; Häusler, B; Milhous, W; Chen, C; Wimonwattrawatee, T; Pooyindee, N; Boudreau, E F

1988-01-01

345

Effects of rumen fluid pre-incubation on in vitro proteolytic activity of enzymatic extracts from rumen microorganisms  

Microsoft Academic Search

Enzymatic extracts were prepared from rumen fluid (RF) either directly after collection or after incubation in enriched media and their proteolytic activities were measured and compared. The objective of RF in vitro cultivation was to augment enzymatic activity by using diverse incubation media containing different feed substrates to selectively induce microorganisms, with essentially unrestricted sources of energy and N. The

A. Velásquez; G. Pichard

2010-01-01

346

Antimutagenic activity of green tea and black tea extracts studied in a dynamic in vitro gastrointestinal model  

Microsoft Academic Search

An in vitro gastrointestinal model, which simulates the conditions in the human digestive tract, was used to determine potential antimutagenic activity of extracts of black tea and green tea. In this paper, results are presented on the availability for absorption of potential antimutagenic compounds present in tea and on the influence of the food matrix on this activity. Between 60

Cyrille Krul; Anja Luiten-Schuite; Aschwin Tenfelde; Ben van Ommen; Hans Verhagen; Robert Havenaar

2001-01-01

347

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

348

In vitro antifungal activity of three geophytic plant extracts against three post-harvest pathogenic fungi.  

PubMed

Plant extracts appear to be one of the most effective alternative methods of plant diseases control which are less harmful to human beings and environment. In vitro antifungal activity of methanolic extracts of three promising wild geophytic plants against three post-harvest pathogenic fungi using radial growth technique was conducted. These extracts included the shoot system (S) and underground parts (R) of Asparagus stipularis, Cyperus capitatus and Stipagrostis lanata. The tested fungi were Alternaria solani, Aspergillus niger and Rhizopus stolonifer. The results exhibited that, all plant extracts had antifungal activity against the tested fungi. The antifungal activity greatly varied depending on plant parts and/or plant species. R. stolonifer was the most susceptible fungus to the tested plant extracts followed by A. niger and then A. solani. On the other hand, the most effective plant extracts against tested fungi were S. lanata (S) and A. stipularis (R). The most effective plant extracts against R. stolonifer were S. lanata (R) and C. capitatus (S). While, the extracts of A. stipularis (R) and S. lanata (S) were the most effective against A. niger. The extracts of C. capitatus (S) and S. lanata (S) exhibited the highest antifungal activity against A. solani. The results demonstrated that, the methanolic extracts of A. stipularis, C. capitatus and S. lanata had potential antifungal activity against A. solani, A. niger and R. stolonifer. PMID:24506036

Maswada, Hanafey F; Abdallah, Sabry A

2013-12-01

349

In vitro and in vivo activities of anti-influenza virus compound T-705.  

PubMed

T-705 (6-fluoro-3-hydroxy-2-pyrazinecarboxamide) has been found to have potent and selective inhibitory activity against influenza virus. In an in vitro plaque reduction assay, T-705 showed potent inhibitory activity against influenza A, B, and C viruses, with 50% inhibitory concentrations (IC(50)s) of 0.013 to 0.48 microg/ml, while it showed no cytotoxicity at concentrations up to 1,000 microg/ml in Madin-Darby canine kidney cells. The selectivity index for influenza virus was more than 2,000. It was also active against a neuraminidase inhibitor-resistant virus and some amantadine-resistant viruses. T-705 showed weak activity against non-influenza virus RNA viruses, with the IC(50)s being higher for non-influenza virus RNA viruses than for influenza virus, and it had no activity against DNA viruses. Orally administered T-705 at 100 mg/kg of body weight/day (four times a day) for 5 days significantly reduced the mean pulmonary virus yields and the rate of mortality in mice infected with influenza virus A/PR/8/34 (3 x 10(2) PFU). These results suggest that T-705 may be a compound that is useful and highly selective against influenza virus infections and that has a mode of action different from those of commercially available drugs, such as amantadine, rimantadine, and neuraminidase inhibitors. PMID:11897578

Furuta, Y; Takahashi, K; Fukuda, Y; Kuno, M; Kamiyama, T; Kozaki, K; Nomura, N; Egawa, H; Minami, S; Watanabe, Y; Narita, H; Shiraki, K

2002-04-01

350

In Vitro Activities of the Multifunctional RNA Silencing Polymerase QDE-1 of Neurospora crassa*  

PubMed Central

QDE-1 is an RNA- and DNA-dependent RNA polymerase that has functions in the RNA silencing and DNA repair pathways of the filamentous fungus Neurospora crassa. The crystal structure of the dimeric enzyme has been solved, and the fold of its catalytic core is related closely to that of eukaryotic DNA-dependent RNA polymerases. However, the specific activities of this multifunctional enzyme are still largely unknown. In this study, we characterized the in vitro activities of the N-terminally truncated QDE-1?N utilizing structure-based mutagenesis. Our results indicate that QDE-1 displays five distinct catalytic activities, which can be dissected by mutating critical amino acids or by altering reaction conditions. Our data also suggest that the RNA- and DNA-dependent activities have different modes for the initiation of RNA synthesis, which may reflect the mechanism that enables the polymerase to discriminate between template nucleic acids. Moreover, we show that QDE-1 is a highly potent terminal nucleotidyltransferase. Our results suggest that QDE-1 is able to regulate its activity mode depending on the template nucleic acid. This work extends our understanding of the biochemical properties of the QDE-1 enzyme and related RNA polymerases. PMID:20647305

Aalto, Antti P.; Poranen, Minna M.; Grimes, Jonathan M.; Stuart, David I.; Bamford, Dennis H.

2010-01-01

351

In vitro screening of traditional medicines for anti-HIV activity: memorandum from a WHO meeting.  

PubMed Central

Many plant products are being used by patients with acquired immunodeficiency syndrome (AIDS) in some countries without any scientific proof that they possess anti-HIV (human immunodeficiency virus) activity. Traditional healers are now offering their remedies for scientific evaluation, and a few studies provide information on the inhibitory activity against HIV of plants such as Viola yedoensis, Arctium lappa, Epimedium grandiflorum, Glycyrrhiza uralensis and Castanospermum australe. Natural products can be selected for biological screening based on ethnomedical use, random collection or a chemotaxonomic approach (i.e., screening of species of the same botanical family for similar compounds), but the follow-up and selection of plants based on literature leads would seem to be the most cost-effective way of identifying plants with anti-HIV activity. No single in vitro screening methodology for anti-HIV activity is ideal and confirmatory assays in multiple systems are needed to examine completely the potential use of a compound. To promote further research in traditional medicine and AIDS, appropriate institutions will be identified where the different activities for the scientific evaluation of plants and their extracts for possible treatment of AIDS can be carried out. PMID:2633879

1989-01-01

352

Catalytic diesel particulate filters reduce the in vitro estrogenic activity of diesel exhaust.  

PubMed

An in vitro reporter gene assay based on human breast cancer T47D cells (ER-CALUX) was applied to examine the ability of diesel exhaust to induce or inhibit estrogen receptor (ER)-mediated gene expression. Exhaust from a heavy-duty diesel engine was either treated by iron- or copper/iron-catalyzed diesel particulate filters (DPFs) or studied as unfiltered exhaust. Collected samples included particle-bound and semivolatile constituents of diesel exhaust. Our findings show that all of the samples contained compounds that were able to induce ER-mediated gene expression as well as compounds that suppressed the activity of the endogenous hormone 17beta-estradiol (E2). Estrogenic activity prevailed over antiestrogenic activity. We found an overall ER-mediated activity of 1.63 +/- 0.31 ng E2 CALUX equivalents (E2-CEQs) per m(3) of unfiltered exhaust. In filtered exhaust, we measured 0.74 +/- 0.07 (iron-catalyzed DPF) and 0.55 +/- 0.09 ng E2-CEQ m(-3) (copper/iron-catalyzed DPF), corresponding to reductions in estrogenic activity of 55 and 66%, respectively. Our study demonstrates that both catalytic DPFs lowered the ER-mediated endocrine-disrupting potential of diesel exhaust. PMID:18264702

Wenger, Daniela; Gerecke, Andreas C; Heeb, Norbert V; Naegeli, Hanspeter; Zenobi, Renato

2008-04-01

353

In vitro activity of NifL, a signal transduction protein for biological nitrogen fixation.  

PubMed Central

In the free-living diazotroph Klebsiella pneumoniae, the NifA protein is required for transcription of all nif (nitrogen fixation) operons except the regulatory nifLA operon itself. NifA activates transcription of nif operons by the alternative holoenzyme form of RNA polymerase, sigma 54 holoenzyme. In vivo, NifL is known to antagonize the action of NifA in the presence of molecular oxygen or combined nitrogen. We now demonstrate inhibition by NifL in vitro in both a coupled transcription-translation system and a purified transcription system. Crude cell extracts containing NifL inhibit NifA activity in the coupled system, as does NifL that has been solubilized with urea and allowed to refold. Inhibition is specific to NifA in that it does not affect activation by NtrC, a transcriptional activator homologous to NifA, or transcription by sigma 70 holoenzyme. Renatured NifL also inhibits transcriptional activation by a maltose-binding protein fusion to NifA in a purified transcription system, indicating that no protein factor other than NifL is required. Since inhibition in the purified system persists anaerobically, our NifL preparation does not sense molecular oxygen directly. Images PMID:8244938

Lee, H S; Narberhaus, F; Kustu, S

1993-01-01

354

Insulin-like biological activity of culinary and medicinal plant aqueous extracts in vitro.  

PubMed

To evaluate the possible effects on insulin function, 49 herb, spice, and medicinal plant extracts were tested in the insulin-dependent utilization of glucose using a rat epididymal adipocyte assay. Cinnamon was the most bioactive product followed by witch hazel, green and black teas, allspice, bay leaves, nutmeg, cloves, mushrooms, and brewer's yeast. The glucose oxidation enhancing bioactivity was lost from cinnamon, tea, witch hazel, cloves, bay leaf and allspice by poly(vinylpyrrolidone) (PVP) treatment, indicating that the active phytochemicals are likely to be phenolic in nature. The activity of sage, mushrooms, and brewers's yeast was not removed by PVP. Some products such as Korean ginseng, flaxseed meal, and basil have been reported to be effective antidiabetic agents; however, they were only marginally active in our assay. Our technique measures direct stimulation of cellular glucose metabolism, so it may be that the active phytochemicals in these plants improve glucose metabolism via other mechanisms or that this in vitro screening is not a reliable predictor of hypoglycemic effects in vivo for some products. In summary, the positive effects of specific plant extracts on insulin activity suggest a possible role of these plants in improving glucose and insulin metabolism. PMID:10725162

Broadhurst, C L; Polansky, M M; Anderson, R A

2000-03-01

355

Evaluation of in vitro antioxidant, antimicrobial, genotoxic and anticancer activities of lichen Cetraria islandica.  

PubMed

In this study, the antioxidant, antimicrobial, genotoxic and anticancer activities of Cetraria islandica methanol extract were determined by using free radical and superoxide anion scavenging activity, reducing power, determination of total phenolic compounds and flavonoid contents, broth microdilution minimal inhibitory concentration against five bacterial and five fungal species, cytokinesis block micronucleus (MN) assay on peripheral blood lymphocytes (PBLs) and the microculture tetrazolium test on FemX (human melanoma) and LS174 (human colon carcinoma) cell lines. As a result of the study, we found that C. islandica methanol extract exhibited moderate free-radical-scavenging activity with IC50 values 678.38 ?g/ml. Moreover, the tested extract had effective reducing power and superoxide anion radical scavenging. The minimal inhibitory concentration values against the tested microorganisms ranged from 0.312 to 5 mg/ml. The extract increased MN frequency in a dose dependent manner, but it was significant in higher tested concentrations (50, 100 and 200 ?g/ml). No significant differences were observed between NDI values in all treatments and untreated PBLs. In addition, the tested extract had strong anticancer activity towards both cell lines with IC50 values of 22.68 and 33.74 ?g/ml. It can be concluded that the tested extract exhibited a certain level of in vitro antioxidant, antimicrobial, genotoxic and anticancer activities. PMID:24590925

Gruji?i?, Darko; Stoši?, Ivana; Kosani?, Marijana; Stanojkovi?, Tatjana; Rankovi?, Branislav; Miloševi?-Djordjevi?, Olivera

2014-10-01

356

In vitro and in vivo activities of three oxazolidinones against nonreplicating Mycobacterium tuberculosis.  

PubMed

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; Cole, Stewart T

2014-06-01

357

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

358

In Vitro Evaluation of the Antimicrobial Activity of Ceftaroline against Cephalosporin-Resistant Isolates of Streptococcus pneumoniae  

Microsoft Academic Search

Increasing pneumococcal resistance to extended-spectrum cephalosporins warrants the search for novel agents with activity against such resistant strains. Ceftaroline, a parenteral cephalosporin currently in phase 3 clinical development, has demonstrated potent in vitro activity against resistant gram-positive organisms, including penicillin-resistant Streptococcus pneumoniae. In this study, the activity of ceftaroline was evaluated against highly cefotaxime-resistant isolates of pneumococci from the Active

Lesley McGee; Donald Biek; Yigong Ge; Magderie Klugman; M. du Plessis; A. M. Smith; B. Beall; C. G. Whitney; K. P. Klugman

2009-01-01

359

Comparative in vitro activity of cefdinir (CI983; FK-482) against staphylococci, gram-negative bacilli and respiratory tract pathogens  

Microsoft Academic Search

The in vitro activity of cefdinir (CI-983; FK-482), a new oral cephalosporin, was compared with that of other antimicrobial agents against clinical isolates of staphylocci, gram-negative bacilli and common respiratory tract pathogens. Cefdinir (MIC90 ? 2.0 µg\\/ml) was more active than cefixime (MIC90 >64 µg\\/ml) and equally as active as cefuroxime (MIC90 2.0 µg\\/ml) against oxacillin-susceptible staphylococci. Cefdinir was active

S. R. Scriver; B. M. Willey; D. E. Low; A. E. Simor

1992-01-01

360

Feedback suppression of the immune response in vitro. I. Activity of antigen-stimulated B cells  

PubMed Central

Feedback regulation of the primary humoral immune response to sheep erythrocytes (SRBC) was studied in vitro. Whole spleen cells or spleen cell subpopulations were incubated with antigen for 4 d under Mishell- Dutton conditions (education) and the surviving cells tested for regulatory activity in fresh anti-SRBC spleen cell cultures assayed by measuring plaque-forming cells on day 4. The data indicate that (a) whole spleen cells educated with SRBC exert potent antigen-specific suppression in the assay culture, (b) surface Ig- (sIg-) cells (T cells) prepared by either nylon-wool separation or fractionation on rabbit anti-mouse-Ig-coated polystyrene Petri dishes failed to generate suppressive activity when educated alone, in 2-mercaptoethanol, or in the presence of additional macrophages, (c) surface Ig (sIg+) (B) cells educated alone also failed to generate suppressor cells, and (d) mixing sIg- (T) and sIg+, Lyt 123- (B) cells reconstituted the ability to induce suppressor cells under these conditions. The antigen-primed cell actually required to transfer suppression was also characterized by separating cells using anti-Ig coated dishes, by fluorescence-activated cell sorting and by anti-Lyt treatment. All these methods clearly identified sIg+ (B) and not sIg+ (T) cells as the important educated cells. It is concluded that under our conditions, T cell-dependent B cells triggered by antigen during primary in vitro cultures cause potent specific feedback suppression of humoral responses. Possible mechanisms for this suppression, including antigen blockade or anti- idiotypic responses, are discussed. PMID:6444663

1980-01-01

361

Comparision of Piceid and Resveratrol in Antioxidation and Antiproliferation Activities In Vitro  

PubMed Central

Background The clinic therapeutic effect of resveratrol is limited due to its low oral bioavailability. Piceid, a precursor of resveratrol, is the most abundant form of resveratrol in nature. A number of studies have hypothesized that piceid may have the same bioactivities like those of resveratrol. The aim of this work is to compare piceid with resveratrol in antioxidation and antiproliferation activities in vitro. Methods The antioxidative effects of resveratrol and piceid were evaluated by phenanthroline-Fe2+ method and H2O2-induced oxidative injury cell model. The antiproliferation effects were determined by MTT method in human liver tumor HepG2 cells, human breast cancer MDA-MB-231 cells and MCF-7 cells. The effects of resveratrol and piceid on the cell cycle and the apoptosis were evaluated by flow cytometry. Additionally, the uptake profiles of resveratrol and piceid in cancer cells were observed using fluorescence microscopy and clarified by LC-MS/MS. Conclusion Piceid exhibited higher scavenging activity against hydroxyl radicals than resveratrol in vitro. Resveratrol showed a significant protective effect against H2O2-induced cell damage. What is more, resveratrol had biphasic effects on tumor cells. Resveratrol and piceid only showed significant cytotoxicity on tumor cells at high concentration (?50 µmol/L), while low concentration of resveratrol (<30 µmol/L) increased the cell viability. The principal effect of resveratrol and piceid on the viability of tumor cells was caused by the cell cycle arrest, while the effect on apoptosis was relatively minor. The reason that piceid showed lower biological activity than resveratrol at the same concentration was probably because piceid was more difficult in being uptaken by cells. PMID:23342161

Liu, Daozhou; Cui, Han; Zhang, Bangle; Zhou, Siyuan; Yang, Tiehong; Mei, Qibing

2013-01-01

362

In Vitro and In Vivo Activities of the Novel Anticytomegalovirus Compound AIC246?  

PubMed Central

Human cytomegalovirus (HCMV) remains a serious threat for immunocompromised individuals, including transplant recipients and newborns. To date, all drugs licensed for the treatment of HCMV infection and disease target the viral DNA polymerase. Although these drugs are effective, several drawbacks are associated with their use, including toxicity and emergence of drug resistance. Hence, new and improved antivirals with novel molecular targets are urgently needed. Here we report on the antiviral properties of AIC246, a representative of a novel class of low-molecular-weight compounds that is currently undergoing clinical phase II studies. The anti-HCMV activity of AIC246 was evaluated in vitro and in vivo using various cell culture assays and an engineered mouse xenograft model. In addition, antiviral properties of the drug were characterized in comparison to the current gold standard ganciclovir. We demonstrate that AIC246 exhibits excellent in vitro inhibitory activity against HCMV laboratory strains and clinical isolates, retains activity against ganciclovir-resistant viruses, is well tolerated in different cell types (median selectivity index, 18,000), and exerts a potent in vivo efficacy in a mouse xenograft model. Moreover, we show that the antiviral block induced by AIC246 is reversible and the efficacy of the drug is not significantly affected by cell culture variations such as cell type or multiplicity of infection. Finally, initial mode-of-action analyses reveal that AIC246 targets a process in the viral replication cycle that occurs later than DNA synthesis. Thus, AIC246 acts via a mode of action that differs from that of polymerase inhibitors like ganciclovir. PMID:20047911

Lischka, Peter; Hewlett, Guy; Wunberg, Tobias; Baumeister, Judith; Paulsen, Daniela; Goldner, Thomas; Ruebsamen-Schaeff, Helga; Zimmermann, Holger

2010-01-01

363

Shc depletion stimulates brown fat activity in vivo and in vitro.  

PubMed

Adipose tissue is an important metabolic organ that integrates a wide array of homeostatic processes and is crucial for whole-body insulin sensitivity and energy metabolism. Brown adipose tissue (BAT) is a key thermogenic tissue with a well-established role in energy expenditure. BAT dissipates energy and protects against both hypothermia and obesity. Thus, BAT stimulation therapy is a rational strategy for the looming pandemic of obesity, whose consequences and comorbidities have a huge impact on the aged. Shc-deficient mice (ShcKO) were previously shown to be lean, insulin sensitive, and resistant to high-fat diet and obesity. We investigated the contribution of BAT to this phenotype. Insulin-dependent BAT glucose uptake was higher in ShcKO mice. Primary ShcKO BAT cells exhibited increased mitochondrial respiration; increased expression of several mitochondrial and lipid-oxidative enzymes was observed in ShcKO BAT. Levels of brown fat-specific markers of differentiation, UCP1, PRDM16, ELOVL3, and Cox8b, were higher in ShcKO BAT. In vitro, Shc knockdown in BAT cell line increased insulin sensitivity and metabolic activity. In vivo, pharmacological stimulation of ShcKO BAT resulted in higher energy expenditure. Conversely, pharmacological inhibition of BAT abolished the improved metabolic parameters, that is the increased insulin sensitivity and glucose tolerance of ShcKO mice. Similarly, in vitro Shc knockdown in BAT cell lines increased their expression of UCP1 and metabolic activity. These data suggest increased BAT activity significantly contributes to the improved metabolic phenotype of ShcKO mice. PMID:25257068

Tomilov, Alexey; Bettaieb, Ahmed; Kim, Kyoungmi; Sahdeo, Sunil; Tomilova, Natalia; Lam, Adam; Hagopian, Kevork; Connell, Michelle; Fong, Jennifer; Rowland, Douglas; Griffey, Stephen; Ramsey, Jon; Haj, Fawaz; Cortopassi, Gino

2014-12-01

364

Nicotine alters the ectonucleotidases activities in lymphocytes: In vitro and in vivo studies.  

PubMed

The aim of the present study was to investigate the effects in vivo and in vitro of nicotine, an important immunosuppressive agent, on NTPDase and ADA activities in lymphocytes of adult rats. The following nicotine doses in vivo study were evaluated: 0.0, 0.25 and 1.0mg/kg/day injected subcutaneously in rats for 10days. The activity of the enzymes were significantly decreased with nicotine 0.25 and 1mg/kg which inhibited ATP (22%, 54%), ADP (44%, 30%) hydrolysis and adenosine (43%, 34%) deamination, respectively. The expression of the protein NTPDase in rat lymphocytes was decreased to nicotine 1mg/kg and the lymphocytes count was decreased in both nicotine doses studied. The purine levels measured in serum of the rats treated with nicotine 0.25mg/kg significantly increased to ATP (39%), ADP (39%) and adenosine (303%). The nicotine exposure marker was determinate by level of cotinine level which significantly increased in rats treated with nicotine 0.25 (39%) and 1mg/kg (131%) when compared to rats that received only saline. The second set of study was in vitro assay which the ATP-ADP-adenosine hydrolysis were decreased by nicotine concentrations 1mM (0% - 0% - 16%, respectively), 5mM (42% - 32% - 74%, respectively), 10mM (80% - 27% - 80%, respectively) and 50mM (96% - 49% - 98%, respectively) when compared with the control group. We suggest that alterations in the activities of these enzymes may contribute to the understanding of the mechanisms involved in the suppression of immune response caused by nicotine. PMID:22475627

Thomé, Gustavo Roberto; Oliveira, Lizielle Souza de; Schetinger, Maria Rosa Chitolina; Morsch, Vera Maria; Spanevello, Rosélia Maria; Fiorenza, Amanda Maino; Seres, Jonas; Baldissarelli, Jucimara; Stefanello, Naiara; Pereira, Maria Ester; Calgaroto, Nicéia Spanholi; Pimentel, Victor Camera; Leal, Daniela Bitencourt Rosa; Souza, Viviane do Carmo Gonçalves; Jaques, Jeandre Augusto dos Santos; Leal, Claudio Alberto Martins; Cruz, Ritiel Corręa da; Thiesen, Flávia Valladăo; Melazzo Mazzanti, Cinthia

2012-04-01

365

Mitochondrial activity assessed by cytofluorescence after in-vitro-irradiation of primary rat brain cultures  

SciTech Connect

Mitochondria play a key role in cell homeostasis and are the first cell organells affected by ionizing irradiation, as it was proved by previous electron microscopic investigations. In order to observe functional parameters of mitochondria after low-dose irradiation, primary rat brain cultures (prepared from 15-day-old rat fetuses) were irradiated from a [sup 60]Co-source with 0.5 and 1 Gy at the age of 2 or 7 days in vitro (div). Cytofluorescence measurement was made by a Cytofluor[sup [trademark]2350] using Rhodamine 123. This fluorescent dye is positively charged and accumulates specifically in the mitochondria of living cells without cytotoxic effect. Since its retention depends on the negative membrane potential as well as the proton gradient that exists across the inner mitochondrial membrane, Rhodamine 123 accumulation reflects the status of mitochondrial activity as a whole. After irradiation with 0.5 and 1 Gy on day 2 in culture there was a decrease in Rhodamine uptake in the irradiated cultures during the first week after the irradiation insult which reached minimum values after 3 days. Rhodamine uptake increased during the following period and finally reached the values of the control cultures. In the second experiment with irradiated cultures on day 7 and the same doses of 0.5 and 1 Gy the accumulation of Rhodamine decreased only initially then increased tremendously. After both doses values of Rhodamine-accumulation were higher than the control level. The results demonstrated that irradiation caused a change in mitochondrial activity depending on the time of irradiation. The dramatic increase over the control levels after irradiation on day 7 in vitro is attributed to the fact that at this time synapses have already developed. Deficiency of mitochondrial activity as well as hyperactivity and the consequent change in energy production may lead to changes in neuronal metabolism including an increase in production of free radicals.

Cervos-Navarro, J.; Hamdorf, G. (Free Univ., Berlin (Germany))

1993-05-01

366

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

PubMed

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. pylori. Gastric biopsy samples were obtained from patients presenting with gastroduodenal complications. Helicobacter pylori was isolated from the specimens following standard microbiology procedures. The disc-diffusion method was used to determine the susceptibility of three H. pylori isolates to methanol extracts of 23 Iranian plants. All tests were performed in triplicate. Among them, the extracts of Punica granatum and Juglans regia had remarkable anti-H. pylori activity with mean of inhibition zone diameter of 39 and 16?mm at 100?µg?disc?ą, respectively. In view of the results obtained with P. granatum (pomegranate), the peel extracts of nine cultivars of pomegranate (Shirin-e-Pust Sefid, Agha Mohammad Ali-e-Shirin, Sefid-e-Shomal, Sefid-e-Torsh, Shirin-e-Malase, Tabestani-e-Torsh, Shirin-e-Saveh Malase, Alak-e-Shirin, Pust Siyah) were further assayed against the clinical isolates of H. pylori. The results revealed that all Iranian pomegranate cultivars, except for Alak-e-Shirin, showed significant in vitro anti-H. pylori activity against the clinical isolates of H. pylori (mean of inhibition zone diameter ranging from 16 to 40 mm at 50 µg disc?ą). PMID:21726128

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

2011-07-01

367

In vitro and in vivo activities of formycin B against Trypanosoma cruzi.  

PubMed Central

The inosine analog formycin B was examined for in vitro and in vivo activities against Trypanosoma cruzi. concentration of formycin B as low as 0.1 microgram/ml markedly inhibited intracellular multiplication of T. cruzi strains both in macrophages and in L929 cells. Mice infected with 10(5) blood form trypomastigotes of the highly virulent strain Y of T. cruzi were completely protected against death by treatment with 11.8 or 5.9 mg of formycin B per kg administered intraperitoneally each day for 19 days. Four different strains of T. cruzi were used, and each was susceptible to formycin B administered either intraperitoneally or orally. Parasitological cure, however, was not achieved with any of the treatments used, including prolonged treatment for up to 10 weeks. Formycin B has a remarkable capacity for inhibiting the in vitro intracellular replication of T. cruzi and protecting mice against death due to the acute infection with the organism. It does not appear, however, to be able to completely eliminate T. cruzi from infected mice. PMID:3923921

McCabe, R E; Remington, J S; Araujo, F G

1985-01-01

368

In vitro and in vivo anthelmintic activity of Euphorbia helioscopia L.  

PubMed

The anthelmintic potentials of the aqueous and methanol extracts of Euphorbia helioscopia were investigated. In folklore medicine, E. helioscopia (Euphorbiaceae) is used in the treatment of various gastrointestinal ailments and diseases. A worm motility inhibition (WMI) assay and egg hatch assay (EHA) were used for in vitro assessment, and a faecal egg count reduction (FECR) assay was used for an in vivo study. The in vitro study revealed anthelmintic effects of crude methanolic extracts of E. helioscopia on live Haemonchus contortus worms as evident from their paralysis and/or death at 8h after exposure, different concentrations (12.5 mg ml(-1), 25 mg ml(-1) and 50 mg ml(-1)) of aqueous and methanolic extracts were used against H. contortus which exhibited dose-dependent anthelmintic effects on H. contortus. Aqueous and methanolic extracts of aerial parts (stem, leaves and flowers) of E. helioscopia were found to have very low percent inhibitory egg hatching as compared to levamisole. It is concluded that the entire plant of E. helioscopia possesses significant anthelmintic activity and could be a potential alternative for treating cases of helminth infections in ruminants. PMID:22633018

Lone, Bashir A; Chishti, M Z; Bhat, Fayaz Ahmad; Tak, Hidayatullah; Bandh, Suhaib A

2012-10-26

369

In vitro antiviral activity of Ficus carica latex against caprine herpesvirus-1.  

PubMed

The latex of Ficus carica Linn. (Moraceae) has been shown to possess antiviral properties against some human viruses. To determine the ability of F. carica latex (F-latex) to interfere with the infection of caprine herpesvirus-1 (CpHV-1) in vitro, F-latex was resuspended in culture media containing 1% ethanol and was tested for potential antiviral effects against CpHV-1. Titration of CpHV-1 in the presence or in the absence of F-latex was performed on monolayers of Madin Darby Bovine Kidney (MDBK) cells. Simultaneous addition of F-latex and CpHV-1 to monolayers of MDBK cells resulted in a significant reduction of CpHV-1 titres 3 days post-infection and this effect was comparable to that induced by acyclovir. The study suggests that the F-latex is able to interfere with the replication of CpHV-1 in vitro on MDBK cells and future studies will determine the mechanisms responsible for the observed antiviral activity. PMID:24853920

Camero, Michele; Marinaro, Mariarosaria; Lovero, Angela; Elia, Gabriella; Losurdo, Michele; Buonavoglia, Canio; Tempesta, Maria

2014-11-01

370

Synthesis and Antifungal Activity In Vitro of Isoniazid Derivatives against Histoplasma capsulatum var. capsulatum  

PubMed Central

Histoplasmosis is a severe infection that affects millions of patients worldwide and is endemic in the Americas. Amphotericin B (AMB) and itraconazole are highly effective for the treatment of severe and milder forms of the disease, but AMB is toxic, and the bioavailability of itraconazole is erratic. Therefore, it is important to investigate new classes of drugs for histoplasmosis treatment. In this study, a series of nine isoniazid hydrazone derivatives were synthesized and evaluated for their antifungal activities in vitro against the dimorphic fungus Histoplasma capsulatum var. capsulatum. The drugs were tested by microdilution in accordance with CLSI guidelines. The compound N?-(1-phenylethylidene)isonicotinohydrazide had the lowest MIC range of all the compounds for the yeast and filamentous forms of H. capsulatum. The in vitro synergy of this compound with AMB against the planktonic and biofilm forms of H. capsulatum cells was assessed by the checkerboard method. The effects of this hydrazone on cellular ergosterol content and membrane integrity were also investigated. The study showed that the compound alone is able to reduce the ergosterol content of planktonic cells and can alter the membrane permeability of the fungus. Furthermore, the compound alone or in combination with AMB showed inhibitory effects against mature biofilms of H. capsulatum. N?-(1-Phenylethylidene)isonicotinohydrazide alone or combined with AMB might be of interest in the management of histoplasmosis. PMID:24514090

de Farias Marques, Francisca Jakelyne; de Aguiar Cordeiro, Rebecca; da Silva, Marcos Reinaldo; Donato Maia Malaquias, Angela; Silva de Melo, Charlline Vladia; Mafezoli, Jair; Ferreira de Oliveira, Maria da Conceicao; Nogueira Brilhante, Raimunda Samia; Gadelha Rocha, Marcos Fabio; Pinheiro Gomes Bandeira, Tereza de Jesus; Costa Sidrim, Jose Julio

2014-01-01

371

Mechanism of Action and Capsid-Stabilizing Properties of VHHs with an In Vitro Antipolioviral Activity  

PubMed Central

ABSTRACT Previously, we reported on the in vitro antiviral activity of single-domain antibody fragments (VHHs) directed against poliovirus type 1. Five VHHs were found to neutralize poliovirus type 1 in an in vitro setting and showed 50% effective concentrations (EC50s) in the nanomolar range. In the present study, we further investigated the mechanism of action of these VHHs. All five VHHs interfere at multiple levels of the viral replication cycle, as they interfere both with attachment of the virus to cells and with viral uncoating. The latter effect is consistent with their ability to stabilize the poliovirus capsid, as observed in a ThermoFluor thermal shift assay, in which the virus is gradually heated and the temperature causing 50% of the RNA to be released from the capsid is determined, either in the presence or in the absence of the VHHs. The VHH-capsid interactions were also seen to induce aggregation of the virus-VHH complexes. However, this observation cannot yet be linked to their mechanism of action. Cryo-electron microscopy (cryo-EM) reconstructions of two VHHs in complex with poliovirus type 1 show no conformational changes of the capsid to explain this aggregation. On the other hand, these reconstructions do show that the binding sites of VHHs PVSP6A and PVSP29F overlap the binding site for the poliovirus receptor (CD155/PVR) and span interfaces that are altered during receptor-induced conformational changes associated with cell entry. This may explain the interference at the level of cell attachment of the virus as well as their effect on uncoating. IMPORTANCE The study describes the mechanism of neutralization and the capsid-stabilizing activity of five single-domain antibody fragments (VHHs) that have an in vitro neutralizing activity against poliovirus type 1. The results show that the VHHs interfere at multiple levels of the viral replication cycle (cell attachment and viral uncoating). These mechanisms are possibly shared by some conventional antibodies and may therefore provide some insight into the natural immune responses. Since the binding sites of two VHHs studied by cryo-EM are very similar to that of the receptor, the VHHs can be used as probes to study the authentic virus-cell interaction. The structures and conclusions in this study are original and raise interesting findings regarding virus-receptor interactions and the order of key events early in infection. PMID:24501405

Schotte, Lise; Strauss, Mike; Thys, Bert; Halewyck, Hadewych; Filman, David J.; Bostina, Mihnea; Rombaut, Bart

2014-01-01

372

Bioaccessibility, in vitro antioxidant activities and in vivo anti-inflammatory activities of a purple tomato (Solanum lycopersicum L.).  

PubMed

The bioaccessibility, antioxidant activities and anti-inflammatory activities of phytochemicals in a purple tomato (Solanum lycopersicum L.) V118 was studied using a simulated gastrointestinal digestion model, chemical and cell based antioxidant assays. The total phenolic and carotenoid contents and the antioxidant activities were significantly lowered (37-72%) and degradation seemed to have occurred during the in vitro digestion. Results indicated that these phytochemicals were bioavailable to the cells as demonstrated by the cell based antioxidant assay. Extracts from the purple tomato showed significant and dose dependent anti-inflammatory effect in the in vivo carrageenan-induced paw oedema rat study (oedematous inhibition: 7.48% and 13.8%), suggesting that anthocyanins may play a role in the anti-inflammatory effect. Direct antioxidant actions as indicated by reduced MDA and NO production and indirect actions as shown in increased GPx and SOD activities in oedematous tissue support the conclusion that tomatoes containing anthocyanins can potentially provide better protection against oxidative stress related chronic diseases of humans. PMID:24767066

Li, Hongyan; Deng, Zeyuan; Liu, Ronghua; Loewen, Steven; Tsao, Rong

2014-09-15

373

SJ23B, a jatrophane diterpene activates classical PKCs and displays strong activity against HIV in vitro.  

PubMed

Existence of virus reservoirs makes the eradication of HIV infection extremely difficult. Current drug therapies neither eliminate these viral reservoirs nor prevent their formation. Consequently, new strategies are needed to target these reservoirs with the aim of decreasing their size. We analysed a series of jatrophane diterpenes isolated from Euphorbia hyberna and we found that one of them, SJ23B, induces the internalization of the HIV-1 receptors CD4, CXCR4 and CCR5 and prevents R5 and X4 viral infection in human primary T cells at the nanomolar range. Moreover, SJ23B is a potent antagonist of HIV-1 latency. Using Jurkat-LAT-GFP cells, a model for HIV-1 latency, we found that prostratin and SJ23B activate HIV-1 gene expression, with SJ23B being at least 10-fold more potent than prostratin. SJ23B did not elicit transforming foci activity in NIH 3T3 cells but is a potent activator of PKCalpha and delta as measured by in vitro kinase assays and by cellular translocation experiments. By using isoform-specific PKC inhibitors we found that cPKCs are critical for SJ23B-induced HIV-1 reactivation. We also showed that both SJ23B-induced IkappaBalpha degradation and NF-kappaB activation were inhibited by the classical PKC inhibitor, Gö6976. Accordingly, SJ23B synergizes with ionomycin to translocate PKCalpha to the plasma membrane and to activate the NF-kappaB pathway. Moreover, SJ23B activates both NF-kappaB and Sp1-dependent transcriptional activities in primary T cells. We have shown that diterpene jatrophanes represent a new member of anti-AIDS agents that could be developed for mitigating HIV reactivation. PMID:19100719

Bedoya, Luis M; Márquez, Nieves; Martínez, Natalia; Gutiérrez-Eisman, Silvia; Alvarez, Amparo; Calzado, Marco A; Rojas, José M; Appendino, Giovanni; Muńoz, Eduardo; Alcamí, José

2009-03-15

374

Structure-Activity-Dependent Regulation of Cell Communication by Perfluorinated Fatty Acids using in Vivo and in Vitro Model Systems  

PubMed Central

Background Perfluoroalkanoates, [e.g., perfluorooctanoate (PFOA)], are known peroxisome proliferators that induce hepatomegaly and hepatocarcinogenesis in rodents, and are classic non-genotoxic carcinogens that inhibit in vitro gap-junctional intercellular communication (GJIC). This inhibition of GJIC is known to be a function of perfluorinated carbon lengths ranging from 7 to 10. Objectives The aim of this study was to determine if the inhibition of GJIC by PFOA but not perfluoropentanoate (PFPeA) observed in F344 rat liver cells in vitro also occurs in F344 rats in vivo and to determine mechanisms of PFOA dysregulation of GJIC using in vitro assay systems. Methods We used an incision load/dye transfer technique to assess GJIC in livers of rats exposed to PFOA and PFPeA. We used in vitro assays with inhibitors of cell signaling enzymes and antioxidants known to regulate GJIC to identify which enzymes regulated PFOA-induced inhibition of GJIC. Results PFOA inhibited GJIC and induced hepatomegaly in rat livers, whereas PFPeA had no effect on either end point. Serum biochemistry of liver enzymes indicated no cytotoxic response to these compounds. In vitro analysis of mitogen-activated protein kinase (MAPK) indicated that PFOA, but not PFPeA, can activate the extracellular receptor kinase (ERK). Inhibition of GJIC, in vitro, by PFOA depended on the activation of both ERK and phosphatidylcholine-specific phospholipase C (PC-PLC) in the dysregulation of GJIC in an oxidative-dependent mechanism. Conclusions The in vitro analysis of GJIC, an epigenetic marker of tumor promoters, can also predict the in vivo activity of PFOA, which dysregulated GJIC via ERK and PC-PLC. PMID:19440492

Upham, Brad L.; Park, Joon-Suk; Babica, Pavel; Sovadinova, Iva; Rummel, Alisa M.; Trosko, James E.; Hirose, Akihiko; Hasegawa, Ryuichi; Kanno, Jun; Sai, Kimie

2009-01-01

375

Ligand Binding and Activation of PPAR? by Firemaster® 550: Effects on Adipogenesis and Osteogenesis in Vitro  

PubMed Central

Background: The use of alternative flame retardants has increased since the phase out of pentabromodiphenyl ethers (pentaBDEs). One alternative, Firemaster® 550 (FM550), induces obesity in rats. Triphenyl phosphate (TPP), a component of FM550, has a structure similar to that of organotins, which are obesogenic in rodents. Objectives: We tested the hypothesis that components of FM550 are biologically active peroxisome proliferator-activated receptor ? (PPAR?) ligands and estimated indoor exposure to TPP. Methods: FM550 and its components were assessed for ligand binding to and activation of human PPAR?. Solvent mapping was used to model TPP in the PPAR? binding site. Adipocyte and osteoblast differentiation were assessed in bone marrow multipotent mesenchymal stromal cell models. We estimated exposure of children to TPP using a screening-level indoor exposure model and house dust concentrations determined previously. Results: FM550 bound human PPAR?, and binding appeared to be driven primarily by TPP. Solvent mapping revealed that TPP interacted with binding hot spots within the PPAR? ligand binding domain. FM550 and its organophosphate components increased human PPAR?1 transcriptional activity in a Cos7 reporter assay and induced lipid accumulation and perilipin protein expression in BMS2 cells. FM550 and TPP diverted osteogenic differentiation toward adipogenesis in primary mouse bone marrow cultures. Our estimates suggest that dust ingestion is the major route of exposure of children to TPP. Conclusions: Our findings suggest that FM550 components bind and activate PPAR?. In addition, in vitro exposure initiated adipocyte differentiation and antagonized osteogenesis. TPP likely is a major contributor to these biological actions. Given that TPP is ubiquitous in house dust, further studies are warranted to investigate the health effects of FM550. Citation: Pillai HK, Fang M, Beglov D, Kozakov D, Vajda S, Stapleton HM, Webster TF, Schlezinger JJ. 2014. Ligand binding and activation of PPAR? by Firemaster® 550: effects on adipogenesis and osteogenesis in vitro. Environ Health Perspect 122:1225–1232;?http://dx.doi.org/10.1289/ehp.1408111 PMID:25062436

Pillai, Hari K.; Fang, Mingliang; Beglov, Dmitri; Kozakov, Dima; Vajda, Sandor; Stapleton, Heather M.; Webster, Thomas F.

2014-01-01

376

Effect of Aqueous Extract and Fractions of Fagonia arabica on In Vitro Anticoagulant Activity.  

PubMed

Fagonia arabica (FA) is a deobstruent and blood purifier, which possesses thrombolytic and antioxidant activities. In this study, the anticoagulant effects of FA and its derived fractions were evaluated. Plasma recalcification was performed with multisolvent extracts of FA and then with extracts prepared successively with increasing polarity of the solvents. Aqueous extract was the most potent anticoagulant extract, which was fractionated by thin-layer chromatography and column chromatography. Five fractions collected were checked for their anticoagulation effect. The most potent fraction was screened for phytoconstituents. Aqueous extract of FA is the most active anticoagulant (31 minutes). Results were statistically significant when compared to heparin (38 minutes) and saline (4.04 minutes; P > .001). The Fifth fraction (FA5), the most potent fraction (27 minutes), was found positive for flavonoids, saponin, tannin, triterpenoids, carbohydrates, reducing sugar, and monosaccharides. Aqueous FA and fraction FA5 were most active in in vitro anticoagulation, and any of the phytochemicals identified could be considered the active component. PMID:23814169

Chourasia, Sweta R; Kashyap, Rajpal Singh; Deopujari, Jayant Y; Purohit, Hemant J; Taori, Girdhar M; Daginawala, Hatim F

2014-11-01

377

In vitro methylation inhibits the promotor activity of a cloned intracisternal A-particle LTR.  

PubMed Central

We studied the relation between LTR methylation and expression of the family of endogenous retrovirus-like elements related to mouse intracisternal A-particles (IAP). Comparative HpaII/MspI and HhaI restriction analysis of genomic DNA's showed that in cells and tissues with a low level of IAP gene expression, HpaII and HhaI sites within the 5' LTR were heavily methylated, while in cells abundantly expressing IAP's 20 to 30% of the 5' LTRs were demethylated at these sites. The effects of methylation on the promoter activity of a cloned IAP 5' LTR was studied directly, using the plasmid pMIA5' L-cat in which this LTR was linked to the chloramphenicol acetyl transferase (CAT) gene. In vitro methylation of three HhaI sites located between -137 and -205 bp from the RNA start site of this LTR completely inactivated the promoter activity of pMIA5' L-cat transfected into COS7 cells. Methylation of a HpaII site located 94 bp downstream from the RNA start site reduced the promoter activity by 75%. The results show that methylation at sites both upstream and downstream from the RNA start site profoundly effects the promoter activity of this LTR and suggest that methylation within the 5' LTR can serve to regulate IAP gene expression in vivo. Images PMID:2423967

Feenstra, A; Fewell, J; Lueders, K; Kuff, E

1986-01-01

378

[Studies on the antitumor activity of human recombinant interferon alpha-2b in vitro].  

PubMed

Correlation between antiproliferative and binding activities of interferon (IFN) alpha-2b to various human cell lines was examined using human recombinant IFN alpha-2b. Burkitt's lymphoma Daudi cells and human renal cell carcinoma OS-RC-2 cells were sensitive to IFN alpha-2b, whereas two EB-virus-transformed B cell lines, FS and L-KT3, and human A375 melanoma cells showed low or no sensitivity. 125I-IFN alpha-2b binding assay revealed that the difference in IFN alpha-2b sensitivity was related to the number and the affinity of IFN alpha-2b receptors per cell. Experiments were then performed to investigate the influence of recombinant IFN alpha-2b on the cytostatic activity of monocytes against A375 cells in vitro. IFN alpha-2b enhanced the cytostatic activity of monocytes against A375 cells which showed low sensitivity to the direct growth inhibitory effect of IFN alpha-2b. Depletion of NK cells from the monocyte preparations by anti-Leu-11b monoclonal antibody and complement did not affect the monocyte activation by IFN alpha-2b, indicating that NK cells were not involved in this system. PMID:2946265

Haraguchi, S; Koide, Y; Matsuo, T; Yoshida, T O

1986-10-01

379

In vitro antioxidative activities and polyphenol content of Eugenia polyantha Wight grown in Indonesia.  

PubMed

Antioxidative activities of three bark extracts (methanol, methanol-water and water) from Eugenia polyantha Wight grown in Indonesia were evaluated using various in vitro assays; 2, 2-diphenyl-1-picrylhydrazyl radical-scavenging, hydrogen peroxide-scavenging and beta-carotene bleaching assays. From the assays, Eugenia polyantha bark extracts were found to be potential antioxidative activities. The methanol-water extract showed the highest level of free radical-scavenging activity (Effective dose (ED50) = 0.18 mg mL-1) and protection from beta-carotene bleaching (85.7% at 100 microg mL-1). The methanol-water extracts showed the highest total phenolic content (856 mg gallic acid equivalent (GAE)/g and 161 mg catechin equivalent (CE)/g) and total antioxidative capacity (449 mg ascorbic acid equivalent (AAE)/g). Furthermore, it exhibited dose-dependent antioxidative activities. A relationship between total antioxidative capacity and total phenolic content was recognized in the three extracts from Eugenia polyantha bark. PMID:20334117

Lelono, Raden Arthur Ario; Tachibana, Sanro; Itoh, Kazutaka

2009-12-15

380

In vitro vascular smooth muscle contractile activity of Aspilia africana extract on rat aortic preparations.  

PubMed

Aspilia africana is widely used in ethnomedical practice in Africa for its ability to stop bleeding, even from a severed artery, as well as promote rapid healing of wounds and sores, and for the management of problems related to cardiovascular diseases. In the present paper, the methylene chloride/methanol extract of A. africana leaves was tested for its contractile activity in vitro. Rings of rat aorta, with or without an intact endothelium, were mounted in tissue baths, contracted with norepinephrine, and then exposed to the plant extract. The effect of the extract was also assessed on the baseline tension of aortic rings in normal and calcium-free PSS. At the lower doses, A. africana slowly re-inforced contractions induced by norepinephrine and relaxed precontracted tension at the highest concentration. The relaxant activity of the extract was endothelium-independent and was not modified by pre-treatment with Nw-nitro-L-arginine methyl ester or indomethacin, suggesting that its effect was not mediated by either nitric oxide or prostacyclin. A. africana extract induced slow and progressive increase in the basal vascular tone which was partially endothelium-dependent. In calcium-free PSS, a high proportion of the contractile activity was inhibited (77%), suggesting that A. africana contractile activity in vascular tissue depends, in part, on extracellular calcium. PMID:12116882

Dimo, T; Tan, P V; Dongo, E; Kamtchouing, P; Rakotonirina, S V

2002-06-01

381

Further in vitro evaluation of antimicrobial activity of the marine sesquiterpene hydroquinone avarol.  

PubMed

This work extends in vitro screening of antimicrobial activity of the sesquiterpene hydroquinone avarol, a main secondary metabolite of the Mediterranean sponge species Dysidea avara. The antimicrobial activity was in part evaluated by microdilution method against selected bacterial and fungal strains. Additionally, the screening included evaluation of anti-quorum sensing (anti-QS) effects. At a different extent avarol was proven to be active against all the microorganisms tested (MIC 0.002-0.008 mg/mL and MBC 0.004-0.016 mg/mL; MIC 0.004-0.015 mg/mL and MFC 0.008-0.030 mg/mL; respectively). This marine natural product also showed moderate anti-QS effects, reducing Pseudomonas aeruginosa PAO1 biofilm formation (75%), its twitching and protrusions motilities as well as pyocianin production (39%). According to the best of our knowledge, this is the first report both on avarol anti Gram-negative bacterial activity and anti-QS effects. PMID:25213366

Pejin, Boris; Iodice, Carmine; Tommonaro, Giuseppina; Stanimirovic, Bojana; Ciric, Ana; Glamoclija, Jasmina; Nikolic, Milos; De Rosa, Salvatore; Sokovic, Marina

2014-01-01

382

Influence of laser irradiation on superoxide dismutase activity of human lymphocytes in vitro  

NASA Astrophysics Data System (ADS)

The treatment of blood with low intensity laser irradiation has become popular in a variety of clinical applications due to its anti-inflammatory, biostimulative and immune-stimulatory effects etc. Laser blood irradiation with infrared and red laser sources have the potential for stimulating antioxidant enzymes activities. At present study the influence of red and infra-red laser irradiation at different doses on superoxide dismutase (SOD) activity of peripheral blood lymphocytes was investigated in vitro. Suspensions of human lymphocytes (concentration of cells 1x10 6 cells/ml) were irradiated with red (670 nm) and infrared (980 nm) therapy lasers at different light doses (0-600 J/sample) and light power (4,5 and 15 mW for red; 50 and 500 mW for infrared) at 20°C. It is revealed doze-depended effect of red and infra-red laser irradiation on superoxide dismutaze activity of peripheral blood lymphocytes. The SOD activity, first of all, depends on irradiation time, but not on intensity or wavelength of irradiation. These data can explain the positive medical effects of a laser blood irradiation. The obtained results confirm a hypothesis that laser irradiation with the different wavelength characteristic (red and infra-red light ranges) reveals a stimulating effect on SOD - antioxidant defence system enzyme in peripheral blood lymphocytes.

Volotovskaya, Anna V.; Kozlova, Nataly M.; Antonovich, Anna N.; Slobozhanina, Ekaterina I.

2007-06-01

383

In vitro Cytotoxic Activity of Four Plants Used in Persian Traditional Medicine  

PubMed Central

Purpose: The aim of this study was to investigate in vitro cytotoxic activity of four methanolic crude plant extracts against panel cell lines. Methods: Methanolic extracts were tested for their possible antitumor activity and cytotoxicity using the 3-(4,5-dimetylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay on six cancer cell lines; non-Hodgkin’s B-cell lymphoma (Raji), human leukemic monocyte lymphoma (U937), human acute myelocytic leukemia (KG-1A), human breast carcinoma (MCF-7 cells), human Prostate Cancer (PC3) and mouse fibrosarcoma (WEHI-164) cell lines and one normal cell line; Human Umbilical Vein Endothelial Cells (HUVEC). Results: All species showed dose dependent inhibition of cell proliferation. IC50 values ranging from 25.66±1.2 to 205.11±1.3 ?g/ml. The highest cytotoxic activity Chelidonium majus L> Ferulago Angulata DC> Echinophora platyloba DC> Salvia officinalis L, respectively. Conclusion: all extracts demonstrate promising cytotoxicity activity as a natural resource for future bio-guided fractionation and isolation of potential antitumor agents. PMID:24312877

Zare Shahneh, Fateme; Baradaran, Behzad; Orangi, Mona; Zamani, Fatemeh

2013-01-01

384

Buffer nitrogen solubility, in vitro ruminal partitioning of nitrogen and in vitro ruminal biological activity of tannins in leaves of four fodder tree species.  

PubMed

This study explores the chemical composition, buffer N solubility, in vitro ruminal N degradability and in vitro ruminal biological activity of tannins in leaves from Gliricidia sepium, Leucaena leucocephala, Morus alba and Trichanthera gigantea trees. These tree leaves are a potential protein source for ruminants, but their site-influenced nutritive value is largely unknown. Leucaena leucocephala leaves had the highest N content (42.1 g/kg DM), while T. gigantea leaves had the least (26.1 g/kg DM). Leucaena leucocephala had the highest buffer solubility index (20%), while 10% of the total N in leaves of the other three species was soluble. The rapidly fermentable N fraction 'a' was highest in M. alba leaves (734.9 g/kg DM) and least in T. gigantea leaves (139.5 g/kg DM). The rate of fermentation (c) was highest for M. alba (7%/hours) leaves. No significant correlations were recorded between buffer solubility index of N and in vitro ruminal N degradability parameters: a, b, and c. The highest response to tannin inactivation using polyethylene glycol, in terms of percentage increase in 36-hours cumulative gas production, was recorded in M. alba (39%) and T. gigantea (38%) leaves. It was concluded that buffer solubility of N is not a good indicator of ruminal N degradation in the leaves of these tree species. Leaves of M. alba could be more valuable as a source of rapidly fermentable N when animals are offered low-protein, high-fibre diets compared with other tree species evaluated in the current study. However, when feeding M. alba leaves, the role of tannins must be considered because these secondary plant compounds showed significant in vitro ruminal biological activity. PMID:24750263

Cudjoe, N; Mlambo, V

2014-08-01

385

Anti-inflammatory activity of Devil’s claw in vitro systems and their active constituents  

Microsoft Academic Search

Cell suspension and Agrobacterium rhizogenes-transformed hairy root cultures of Devil’s claw (Harpagophytum procumbens), an African plant with high medicinal value, were cultivated in shake-flasks. A purification scheme to isolate their main active constituents (the phenylethanoid glycosides verbascoside, leucosceptoside A, ?-OH-verbascoside and martynoside; structurally identified by NMR and LC–MS) was then developed, and their concentrations in the cultures were determined by

Valeriya Gyurkovska; Kalina Alipieva; Alexandre Maciuk; Petya Dimitrova; Nina Ivanovska; Christiane Haas; Thomas Bley; Milen Georgiev

2011-01-01

386

Calcineurin (CN) Activation Promotes Apoptosis of Glomerular Podocytes Both in Vitro and in Vivo  

PubMed Central

To determine the role of Gq signaling and calcineurin (CN) activation in promoting apoptosis of glomerular podocytes, constitutively active Gq [Gq(+)] or CN [CN(+)] proteins were introduced into cultured podocytes using protein transduction by tagging the proteins with the transactivator of transcription peptide. To investigate the role of CN in promoting podocyte apoptosis in vivo, a genetic model of type 1 diabetes mellitus (Akita mice) was treated with the CN inhibitor FK506. In cultured podocytes, Gq(+) stimulated nuclear translocation of nuclear factor of activated T cells (NFAT) family members, activated an NFAT reporter construct, and enhanced podocyte apoptosis in a CN-dependent fashion. CN(+) similarly promoted podocyte apoptosis, and apoptosis induced by either angiotensin II or endothelin-1 was blocked by FK506. Induction of apoptosis required NFAT-induced gene transcription because apoptosis induced by either Gq(+) or CN(+) was blocked by an inhibitor that prevented CN-dependent NFAT activation without affecting CN phosphatase activity. Podocyte apoptosis was mediated, in part, by the NFAT-responsive gene cyclooxygenase 2 (COX2) and prostaglandin E2 generation because apoptosis induced by Gq(+) was attenuated by either COX2 inhibition or blockade of the Gq-coupled E-series prostaglandins receptor. The findings appeared relevant to podocyte apoptosis in diabetic nephropathy because apoptosis was significantly reduced in Akita mice by treatment with FK506. These data suggest that Gq stimulates CN and promotes podocyte apoptosis both in vitro and in vivo. Apoptosis requires NFAT-dependent gene transcription and is mediated, in part, by CN-dependent COX2 induction, prostaglandin E2 generation, and autocrine activation of the Gq-coupled E-series prostaglandins receptor. PMID:21622531

Wang, Liming; Chang, Jae-Hyung; Paik, Seung-Yeol; Tang, Yuping; Eisner, William

2011-01-01

387

Osteoclast Activated FoxP3+ CD8+ T-Cells Suppress Bone Resorption in vitro  

PubMed Central

Background Osteoclasts are the body’s sole bone resorbing cells. Cytokines produced by pro-inflammatory effector T-cells (TEFF) increase bone resorption by osteoclasts. Prolonged exposure to the TEFF produced cytokines leads to bone erosion diseases such as osteoporosis and rheumatoid arthritis. The crosstalk between T-cells and osteoclasts has been termed osteoimmunology. We have previously shown that under non-inflammatory conditions, murine osteoclasts can recruit naďve CD8 T-cells and activate these T-cells to induce CD25 and FoxP3 (TcREG). The activation of CD8 T-cells by osteoclasts also induced the cytokines IL-2, IL-6, IL-10 and IFN-?. Individually, these cytokines can activate or suppress osteoclast resorption. Principal Findings To determine the net effect of TcREG on osteoclast activity we used a number of in vitro assays. We found that TcREG can potently and directly suppress bone resorption by osteoclasts. TcREG could suppress osteoclast differentiation and resorption by mature osteoclasts, but did not affect their survival. Additionally, we showed that TcREG suppress cytoskeletal reorganization in mature osteoclasts. Whereas induction of TcREG by osteoclasts is antigen-dependent, suppression of osteoclasts by TcREG does not require antigen or re-stimulation. We demonstrated that antibody blockade of IL-6, IL-10 or IFN-? relieved suppression. The suppression did not require direct contact between the TcREG and osteoclasts. Significance We have determined that osteoclast-induced TcREG can suppress osteoclast activity, forming a negative feedback system. As the CD8 T-cells are activated in the absence of inflammatory signals, these observations suggest that this regulatory loop may play a role in regulating skeletal homeostasis. Our results provide the first documentation of suppression of osteoclast activity by CD8 regulatory T-cells and thus, extend the purview of osteoimmunology. PMID:22701612

Buchwald, Zachary S.; Kiesel, Jennifer R.; DiPaolo, Richard; Pagadala, Meghana S.; Aurora, Rajeev

2012-01-01

388

Equine cytochrome P450 aromatase exhibits an estrogen 2-hydroxylase activity in vitro.  

PubMed

Aromatase (estrogen synthetase) is a steroidogenic enzyme complex which catalyzes the conversion of androgens to estrogens (termed aromatization). This enzyme was purified from adult equine testis to homogeneity by five chromatographic steps. The ability of purified and reconstituted equine aromatase to exhibit an estrogen 2-hydroxylase activity was tested and compared to testosterone aromatization. Enzymatic activities were assessed by tritiated water release from labelled estradiol and testosterone. Kinetic analysis of estradiol 2-hydroxylation showed an apparent K(m) of 23 microM and a V(max) of 18 nmol/min/mg, whereas the values for testosterone aromatization were a K(m) of 15.7 nM and a V(max) of 34.6 pmol/min/mg. A specific antiserum raised against purified testicular equine P450arom and known to inhibit aromatase activity [1] was also found to inhibit the estrogen hydroxylase activity of equine placental microsomes in a dose-dependent manner with an IC50 value of 15 microl serum: 0.5 ml incubate. The estrogen hydroxylase activity was inhibited in a dose-dependent manner by two classes of aromatase inhibitors, i.e. steroidal-- (4-hydroxyandrostenedione and 7alpha-([4-aminophenyl]thio)-androst-4-ene-3, 17-dione)--and non-steroidal--(fadrozole and miconazole). The IC50 values were approximately 300 and 890 nM for 4-hydroxyandrostenedione and 7alpha-([4-aminophenyl]thio)-androst-4-ene-3, 17-dione, and 92 and 285 nM, for fadrozole and miconazole, respectively. Furthermore, 4-hydroxyandrostenedione caused a time-dependent inactivation of estrogen hydroxylase activity. We conclude that equine aromatase is able to use estradiol as a substrate, and converts it to catechol estradiol in vitro, possibly using the active site of aromatization. This is the first demonstration that equine aromatase functions as an estrogen 2-hydroxylase, in addition to transforming androgens into estrogen. PMID:9009238

Almadhidi, J; Moslemi, S; Drosdowsky, M A; Séralini, G E

1996-09-01

389

Designed, synthetically accessible bryostatin analogues potently induce activation of latent HIV reservoirs in vitro  

NASA Astrophysics Data System (ADS)

Bryostatin is a unique lead in the development of potentially transformative therapies for cancer, Alzheimer's disease and the eradication of HIV/AIDS. However, the clinical use of bryostatin has been hampered by its limited supply, difficulties in accessing clinically relevant derivatives, and side effects. Here, we address these problems through the step-economical syntheses of seven members of a new family of designed bryostatin analogues using a highly convergent Prins-macrocyclization strategy. We also demonstrate for the first time that such analogues effectively induce latent HIV activation in vitro with potencies similar to or better than bryostatin. Significantly, these analogues are up to 1,000-fold more potent in inducing latent HIV expression than prostratin, the current clinical candidate for latent virus induction. This study provides the first demonstration that designed, synthetically accessible bryostatin analogues could serve as superior candidates for the eradication of HIV/AIDS through induction of latent viral reservoirs in conjunction with current antiretroviral therapy.

Dechristopher, Brian A.; Loy, Brian A.; Marsden, Matthew D.; Schrier, Adam J.; Zack, Jerome A.; Wender, Paul A.

2012-09-01

390

The in vitro immunomodulatory activity of a polysaccharide isolated from Kadsura marmorata.  

PubMed

Kadsura marmorata has been used in traditional Chinese medicine as one of the major ingredients for the treatment of bronchial asthma, eczema, and acute and chronic infection due to either viruses or bacteria. The purpose of this study was to determine the immunomodulatory activities of the Kadsura polysaccharide (KPS) that was isolated and purified from the fruit of K. marmorata, designated as KPSIII and has a molecular weight of 130,406. The immunomodulatory effects of KPSIII were evaluated in vitro on chicken lymphocytes and macrophages. The results indicated that KPSIII could stimulate the cell proliferation of chicken T-lymphocytes, B-lymphocytes, and peritoneal macrophages and could significantly enhance cytokine secretion. Moreover, KPSIII regulated cytokine expression in T-lymphocytes and peritoneal macrophages. This study suggests that KPSIII has potential effects on regulating the immune system and might be an immunotherapeutic agent in treating various immunity-related diseases in chickens. PMID:23911505

Wang, Hongjun; Deng, Xuming; Zhou, Tiezhong; Wang, Chunhua; Hou, Yanjie; Jiang, Hong; Liu, Guangliang

2013-09-12

391

In vitro nematocidal activity of plant extracts of Mexican flora against Haemonchus contortus fourth larval stage.  

PubMed

Fourteen plant extracts were evaluated in vitro against the fourth larval stage of Haemonchus contortus. The plants species used were Tagetes erecta, Argemone mexicana, and Castela tortuosa. The assays were run in 24-well cell culture plates at room temperature with three replicates. After exposure, aliquots were taken from the corresponding wells and transferred to a microscope for observation. Evaluation criteria were based on the average of live and/or dead larvae. ANOVA test and Tukey test were used to determine significant differences among the treatments. After 96 h, the T. erecta acetonic extract produced 99.7% lethal activity, followed by C. tortuosa hexanic extract (85.8%) and T. erecta methanolic extract (58.3%) (P < 0.0001). PMID:19120198

Aguilar, Hector Hugo Galicia; de Gives, Pedro Mendoza; Sánchez, David Osvaldo Salinas; Arellano, María Eugenia López; Hernández, Enrique Liébano; Aroche, Ulises López; Valladares-Cisneros, Guadalupe

2008-12-01

392

Human androgen receptor expressed in HeLa cells activates transcription in vitro.  

PubMed Central

The androgen receptor (AR) is a ligand-responsive transcription factor, belonging to the class of steroid receptors. AR mutations have been associated with various X-linked diseases, characterized by complete or partial resistance to androgens. To further analyse the molecular mechanism of action of the AR, we have produced the human AR in HeLa cells with a Vaccinia virus expression system. Binding studies on infected HeLa cells demonstrate that the recombinant AR interacts specifically and with high affinity with natural and synthetic androgens. In a gel retardation assay the partially purified AR specifically recognizes an androgen response element of the rat prostatic binding protein gene. Moreover, the recombinant AR activates transcription in vitro from a synthetic promoter construct containing glucocorticoid response elements (GRE). Images PMID:8165128

De Vos, P; Schmitt, J; Verhoeven, G; Stunnenberg, H G

1994-01-01

393

Antimutagenic activities of naturally occurring polyamines in Chinese hamster ovary cell in vitro  

SciTech Connect

Spermine and spermidine, ubiquitous polyamines present in bacteria and animal cells, are also involved in cell growth. Since they interact with the double helix, they can stabilize the DNA molecule. Recent evidence of the antimutagenic and anticarcinogenic capacity of spermine has focused attention on the he mechanism(s) by which such agents can protect cells from induced damages. In the present paper the authors show the ability of spermine and spermidine to decrease the level of sister chromatid exchanges induced in Chinese hamster ovary cells cultivated in vitro, by treating them with Psoralen + UVA irradiation (able to induce mainly monoadducts and DNA cross-links). Two different mechanisms of polyamine action can be invoked to explain the preservative activity of this class of agents.

Cozzi, R.; Perticone, P.; Bona, R.; Polani, S. (Univ. La Sapienza, Rome (Italy))

1991-01-01

394

In vitro antimicrobial activity of Romanian medicinal plants hydroalcoholic extracts on planktonic and adhered cells.  

PubMed

The aim of this study was to assess the antibacterial and antifungal potential of some Romanian medicinal plants, arnica--Arnica montana, wormwood--Artemisia absinthium and nettle--Urtica dioica. In order to perform this antimicrobial screening, we obtained the vegetal extracts and we tested them on a series of Gram-positive and Gram-negative bacteria, and also against two fungal strains. The vegetal extracts showed antimicrobial activity preferentially directed against the planktonic fungal and bacterial growth, while the effect against biofilm formation and development was demonstrated only against S. aureus and C. albicans. Our in vitro assays indicate that the studied plant extracts are a significant source of natural alternatives to antimicrobial therapy, thus avoiding antibiotic therapy, the use of which has become excessive in recent years. PMID:21717806

Stanciuc, A M; Gaspar, A; Moldovan, L; Saviuc, C; Popa, M; M?ru?escu, L

2011-01-01

395

In vitro antagonistic activity of monoterpenes and their mixtures against 'toe nail fungus' pathogens.  

PubMed

The antibiotic effect of the active ingredients in Meijer medicated chest rub (eucalyptus oil, camphor and menthol) as well as the inactive ingredients (thymol, oil of turpentine, oil of nutmeg and oil of cedar leaf) were studied in vitro using the fungal pathogens responsible for onychomycosis, such as the dermatophytes Tricophyton rubrum, Trichophyton mentagrophytes, Microsporum canis, Epidermophyton fl occosum and Epidermophyton stockdale. The zones of inhibition data revealed that camphor (1). menthol (2). thymol (3). and oil of Eucalyptus citriodora were the most efficacious components against the test organisms. The MIC(100) for mixtures of these four components in various carrier solvents revealed that formulations consisting of 5 mg/mL concentrations of each have a potential to be efffective in controlling onychomycosis. PMID:12722144

Ramsewak, Russel S; Nair, Muraleedharan G; Stommel, Manfred; Selanders, Louise

2003-04-01

396

ACHN-490, a neoglycoside with potent in vitro activity against multidrug-resistant Klebsiella pneumoniae isolates.  

PubMed

The in vitro activity of ACHN-490, a novel aminoglycoside ("neoglycoside"), was evaluated against 102 multidrug-resistant (MDR) Klebsiella pneumoniae strains, including a subset of 25 strains producing the KPC carbapenemase. MIC50 values for gentamicin, tobramycin, and amikacin were 8 microg/ml, 32 microg/ml, and 2 microg/ml, respectively; MIC90 values for the same antimicrobials were > or = 64 microg/ml, > or = 64 microg/ml, and 32 microg/ml, respectively. ACHN-490 showed an MIC50 of 0.5 microg/ml and an MIC90 of 1 microg/ml, which are significantly lower than those of comparator aminoglycosides. ACHN-490 represents a promising aminoglycoside for the treatment of MDR K. pneumoniae isolates, including those producing KPC beta-lactamase. PMID:19770287

Endimiani, Andrea; Hujer, Kristine M; Hujer, Andrea M; Armstrong, Eliana S; Choudhary, Yuvraj; Aggen, James B; Bonomo, Robert A

2009-10-01

397

In Vitro Activity of Nemonoxacin, a Novel Nonfluorinated Quinolone Antibiotic, against Chlamydia trachomatis and Chlamydia pneumoniae  

PubMed Central

The in vitro activities of nemonoxacin, levofloxacin, azithromycin, and doxycycline were tested against 10 isolates each of Chlamydia trachomatis and Chlamydia pneumoniae. The MICs at which 90% of the isolates of both C. trachomatis and C. pneumoniae were inhibited (MIC90s) were 0.06 ?g/ml (range, 0.03 to 0.13 ?g/ml). The minimal bactericidal concentrations at which 90% of the isolates were killed by nemonoxacin (MBC90s) were 0.06 ?g/ml for C. trachomatis (range, 0.03 to 0.125 ?g/ml) and 0.25 for C. pneumoniae (range, 0.015 to 0.5 ?g/ml). PMID:24366753

Chotikanatis, Kobkul; Kohlhoff, Stephan A.

2014-01-01

398

Synthesis and antimalarial activity of urenyl Bis-chalcone in vitro and in vivo.  

PubMed

Some novel derivatives of Bis-chalcone were synthesized and characterized by their physical and spectral data. All the synthesized compounds were subsequently screened for in vitro globin hydrolysis, ?-hematin formation, and murine Plasmodium berghei, using chloroquine as the reference drug. Most of the synthesized compounds exhibited mild to moderate susceptibilities toward the parasite in comparison with the standard. The most active antimalarial compound was 1,1-Bis-[(3',4'-N-(urenylphenyl)-3-(3?,4?,5?-trimethoxyphenyl)]-2-propen-1-one 5, with a percentage of inhibition of heme