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1

Schistosoma mansoni: in vitro schistosomicidal activity of essential oil of Baccharis trimera (less) DC.  

PubMed

Schistosomiasis is a chronic parasitic disease caused by the trematode species Schistosoma mansoni. Chemotherapy is the only immediate recourse to minimize the prevalence and incidence of this disease worldwide. At present, praziquantel (PZQ) is the drug of choice for the treatment of all forms of schistosomiasis. However, dependence on a single drug is concern because some strains can become resistant. In this context, medicinal plants become potential candidates as sources of new drug prototypes. This study provides findings on the schistosomicidal activity of the essential oil of Baccharis trimera in in vitro assays. During the assays parameters such as motility of adult worms, oviposition, morphological changes on the tegument and especially the mortality rate of adult worms of the BH strain were evaluated. The assays, which were carried out with four concentrations - 24, 48, 91 and 130 ?g/mL - of the essential oil, have shown a promising activity regarding the parameters under study. It was possible to notice a significant decline in the motility of the worms and a mortality rate of 100% 30 h after they had been exposed to the essential oil in the concentration of 130 ?g/mL. Male worms were more susceptible, producing a dose-response effect within a smaller exposition period than female worms. In what refers to morphological changes, the essential oil of B. trimera induced a peeling on the tegument surface, as well as the destruction of tubercles and spines, which resulted in smooth areas on the body surface. The essential oil also caused tegument destruction in female worms, in addition to destruction of the oral and acetabular suckers. It is the first time that the schistosomicidal activity has been reported for essential oil of B. trimera (less) DC. PMID:22771865

de Oliveira, Rosimeire Nunes; Rehder, Vera Lúcia Garcia; Santos Oliveira, Adriana S; Júnior, Ílio Montanari; de Carvalho, Joăo Ernesto; de Ruiz, Ana Lúcia Tasca Gois; Jeraldo, Veronica de Lourdes Sierpe; Linhares, Arício Xavier; Allegretti, Silmara Marques

2012-10-01

2

In vitro schistosomicidal effects of aqueous and dichloromethane fractions from leaves and stems of Piper species and the isolation of an active amide from P. amalago L. (Piperaceae).  

PubMed

Dichloromethane and aqueous fractions from leaves and stems of Piper arboreum Aubl., P. aduncum L., P. amalago L., P. crassinervium H.B. & K., P. diospyrifolium Kunth, P. hispidum Sw. and P. xylosteoides (Kunth) Steud. were tested against adult worms of Schistosoma mansoni. The in vitro activity was evaluated in terms of mortality, number of separated worms and number of worms with reduced motor activity. Most dichloromethane fractions from all Piper species showed moderate schistosomicidal activity, but aqueous fractions were not active. The dichloromethane fraction of P. amalago leaves (at 100 ?g/ml) showed the highest activity, resulting in worm mortality, the separation of worm pairs and reduced motor activity. Chromatographic fractionation of the dichloromethane fraction of P. amalago leaves led to the isolation of its major compound, which was also tested against adults of S. mansoni. The isolated piperamide N-[7-(3',4'-methylenedioxyphenyl)-2(Z),4(Z)-heptadienoyl] pyrrolidine, at 100 ? m, resulted in the mortality of all adult worms after 24 h of incubation. The findings suggest that species of Piper are potential sources of schistosomicidal compounds. PMID:23561585

Carrara, V S; Vieira, S C H; de Paula, R G; Rodrigues, V; Magalhăes, L G; Cortez, D A G; Da Silva Filho, A A

2013-04-01

3

In vitro evaluation of schistosomicidal activity of essential oil of Mentha x villosa and some of its chemical constituents in adult worms of Schistosoma mansoni.  

PubMed

This study aimed to determine the composition of the essential oil of Mentha x villosa and to evaluate its biological effects in vitro on adult worms of S. mansoni. Rotundifolone (70.96 %), limonene (8.75 %), trans-caryophyllene (1.46 %), and ?-pinene (0.81 %) were shown to be the major constituents of this oil. Adult worms of S. mansoni were incubated with different concentrations of the essential oil (1, 10, 100, 250, 500, and 1000 µg/mL) and of its constituents rotundifolone (0.7, 3.54, 7.09, 70.96, 177.4, 354.8, and 700.96 µg/mL), limonene (43.75 µg/mL), trans-caryophyllene (7.3 µg/mL), and ?-pinene (4.03 µg/mL). No schistosomicidal activity was identified at the trans-caryophyllene and ?-pinene concentrations studied. However, use of the essential oil (10 µg/mL), rotundifolone (7.09 µg/mL), and limonene (43.75 µg/mL) resulted in decreased worm motility continuing until 96 hours of observation. At higher concentrations (100 and 70.96 µg/mL, respectively), both the essential oil and rotundifolone caused mortality among adult worms of S. mansoni. The positive control praziquantel caused the death of all parasites after 24 h of evaluation. The results from this study suggest that the essential oil of Mentha x villosa presents schistosomicidal efficacy. PMID:23945759

Matos-Rocha, Thiago José; dos Santos Cavalcanti, Marília Gabriela; Barbosa-Filho, José Maria; Lúcio, Ana Silvia Suassuna Carneiro; Veras, Dyana Leal; Feitosa, Ana Paula Sampaio; de Siqueira Júnior, José Pinto; de Almeida, Reinaldo Nóbrega; Marques, Márcia Ortiz Mayo; Alves, Luiz Carlos; Brayner, Fábio André

2013-09-01

4

Antiprotozoal, schistosomicidal, and antimicrobial activities of the essential oil from the leaves of Baccharis dracunculifolia.  

PubMed

Baccharis dracunculifolia DC. (Asteraceae), popularly known as 'alecrim do campo', is a native plant from Brazil used in folk medicine as febrifuge, anti-inflammatory, antiseptic, and to treat skin sores. Also, B. dracunculifolia is the most important plant source of the Brazilian green propolis, which is recognized for its antiseptic and antiprotozoal activities. This study aimed at investigating the in vitro antiprotozoal, schistosomicidal, and antimicrobial activities of the essential oil from the leaves of B. dracunculifolia. The essential oil was obtained by hydrodistillation and analyzed by GC and GC/MS, which allowed the identification of 14 compounds, mainly oxygenated sesquiterpenes, such as (E)-nerolidol (33.51%) and spathulenol (16.24%). The essential oil showed activity against promastigote forms of Leishmania donovani, with IC(50) values of 42 microg/ml. The essential oil displayed high activity in the schistosomicidal assay, since all pairs of Schistosoma mansoni adult worms were dead after incubation with the essential oil (10, 50, and 100 microg/ml). B. dracunculifolia essential oil was neither cytotoxic against Vero cells, nor active in the antimicrobial and antiplasmodial assays. PMID:20397234

Parreira, Natállia A; Magalhăes, Lizandra G; Morais, Denis R; Caixeta, Soraya C; de Sousa, Joăo P B; Bastos, Jairo K; Cunha, Wilson R; Silva, Márcio L A; Nanayakkara, N P D; Rodrigues, Vanderlei; da Silva Filho, Ademar A

2010-04-01

5

Succinate cytochrome c reductase in schistosomiasis: in vitro inhibition by some schistosomicidal drugs.  

PubMed

Enzymes in mitochondria play an important role in biological oxidation and energy production. To understand the effect of schistosomiasis on these important processes, succinate cytochrome c reductase (SCR) from control and Schistosoma-infected mice was subjected for investigation. In this article, we report that SCR from Schistosoma-infected mouse showed a significant decrease in its Vmax and Km compared to control using both cytochrome c and 2,6-dichlorophenolindophenol as substrates. Furthermore, the kinetic studies of the purified SCR in the absence and presence of the schistosomicidal drugs praziquantel and Commiphora extract reveal that both drugs have an inhibitory action on the enzyme from the control and Schistosoma-infected mice and praziquantel changes the type of inhibition of SCR towards cytochrome c from mixed type in control to a competitive one in the case of the infection. PMID:20680542

Balbaa, Mahmoud; Abdel Moneam, Nihad M; El-Kersh, Mohamed; Omran, Heba; Kandeel, Kamal

2010-12-01

6

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

7

In vitro activity of doripenem.  

PubMed

Doripenem is a carbapenem antibiotic that covers a wide range of gram-positive and gram-negative pathogens. In vitro studies have provided insight into certain features of doripenem's activity profile that may have particular relevance in the clinical setting. For instance, in vitro data indicate that doripenem combines the intrinsic activity of meropenem against gram-negative pathogens with the intrinsic activity of imipenem against gram-positive pathogens. Also notable is the fact that the in vitro activity of doripenem against problematic gram-negative pathogens, in particular Pseudomonas aeruginosa, is potent-recent data show that the minimum concentration necessary for inhibition of 90% of all isolates (MIC(90)) of doripenem with respect to P. aeruginosa (4 microg/mL) is 2-4 times lower than the corresponding MIC(90) values of meropenem and imipenem. Furthermore, doripenem shows a limited ability to select for carbapenem-resistant mutants in vitro. Such experimental findings suggest that doripenem may represent a valuable option when carbapenem therapy is warranted for the treatment of serious infection. PMID:19619017

Sahm, Daniel

2009-08-15

8

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.

Katz, Naftale; Couto, Flavia Fernanda Bubulo; Araujo, Neusa

2013-01-01

9

In vitro electrical activity in canine colon  

Microsoft Academic Search

In vitro slow wave activity was studied in strips of right and left canine colon with silver\\/silver chloride electrodes. Using visual and computer analysis, slow wave frequency and coupling was assessed between different recording sites and the effect of a cholinergic agonist on coupling and frequency was determined. A regular slow wave was always found to be present. Frequency in

N L Shearin; K L Bowes; Y J Kingma

1979-01-01

10

In vitro antimycoplasmal activity of oleuropein  

Microsoft Academic Search

The activity of oleuropein, a phenolic glycoside contained in olive oil, was investigated in vitro against Mycoplasma hominis, Mycoplasma fermentans, Mycoplasma pneumoniae and Mycoplasma pirum. Oleuropein inhibited mycoplasmas at concentrations from 20 to 320 mg\\/l. The MICs of oleuropein to M. pneumoniae, M. pirum, M. hominis and M. fermentans were 160, 320, 20 and 20 mg\\/l, respectively.

Pio Maria Furneri; Andreana Marino; Antonina Saija; Nicola Uccella; Giuseppe Bisignano

2002-01-01

11

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

12

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.

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

13

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

PubMed Central

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

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

2009-01-01

14

Estrogenic activity of tissue conditioners in vitro  

Microsoft Academic Search

Objectives. In order to assess the estrogenic activities of plasticizers used in tissue conditioners and four commercial tissue conditioners, we carried out in vitro tests.Methods. Seven plasticizers and two metabolites were diluted to concentrations ranging from 10?9 to 10?4M. Four commercial tissue conditioners were also diluted to concentrations ranging from 2×10?8 to 2×10?3g\\/ml. Estrogenic activities were tested by the E-screen

Yoshiya Hashimoto; Minoru Kawaguchi; Koji Miyazaki; Masaaki Nakamura

2003-01-01

15

In Vitro Activity of Coumermycin A1  

PubMed Central

The in vitro activity of coumermycin A1 was compared with that of novobiocin, ampicillin, and minocycline. Coumermycin was found to be the most active antibiotic of the four against Staphylococcus aureus. It was about 50 times more active than novobiocin or minocycline against the strains tested. Coumermycin also showed good activity against group A streptococci and pneumococci, moderate activity against Escherichia coli, indole-positive Proteus species, and Pseudomonas aeruginosa, and poor activity against Klebsiella-Enterobacter and enterococci. Against P. mirabilis, however, coumermycin activity was almost equal to that of ampicillin. The new antibiotic was further found to be greatly reduced in activity in the presence of plasma, but its minimal inhibitory concentration was not greatly affected by inoculum size. Coumermycin was found to be bacteriostatic in its action, and resistance to it developed slowly. Also, cross-resistance was present with novobiocin but absent with ampicillin or minocycline.

Fedorko, Joseph; Katz, Sol; Allnoch, Hedi

1969-01-01

16

Antischistosomal activity of the terpene nerolidol.  

PubMed

Schistosomiasis is a neglected tropical disease that affects hundreds of millions of people worldwide. Since the treatment of this disease currently relies on a single drug, praziquantel, new and safe schistosomicidal agents are urgently required. Nerolidol, a sesquiterpene present in the essential oils of several plants, is found in many foods and was approved by the U.S. Food and Drug Administration. In this study we analysed the in vitro antiparasitic effect of nerolidol on Schistosoma mansoni adult worms. Nerolidol at concentrations of 31.2 and 62.5 ?M reduced the worm motor activity and caused the death of all male and female schistosomes, respectively. In addition, confocal laser scanning microscopy revealed morphological alterations on the tegument of worms such as disintegration, sloughing and erosion of the surface, and a correlation between viability and tegumental damage was observed. In conclusion, nerolidol may be a promising lead compound for the development of antischistosomal natural agents. PMID:24662089

Silva, Marcos P N; Oliveira, George L S; de Carvalho, Rusbene B F; de Sousa, Damiăo P; Freitas, Rivelilson M; Pinto, Pedro L S; de Moraes, Josué

2014-01-01

17

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

18

[The in vitro activity of veterinary antiseptics].  

PubMed

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

Maris, P

1990-01-01

19

Acidosis activates complement system in vitro.  

PubMed Central

We investigated the in vitro effect of different forms of acidosis (pH 7.0) on the formation of anaphylatoxins C3a and C5a. Metabolic acidosis due to addition of hydrochloric acid (10 micromol/ml blood) or lactic acid (5.5 micromol/ml) to heparin blood (N=12) caused significant activation of C3a and C5a compared to control (both p=0.002). Respiratory acidosis activated C3a (p=0.007) and C5a (p=0.003) compared to normocapnic controls. Making blood samples with lactic acidosis hypocapnic resulted in a median pH of 7.37. In this respiratory compensated metabolic acidosis, C3a and C5a were not increased. These experiments show that acidosis itself and not lactate trigger for activation of complement components C3 and C5.

Emeis, M; Sonntag, J; Willam, C; Strauss, E; Walka, M M; Obladen, M

1998-01-01

20

In vitro antioxidant activity of silymarin.  

PubMed

Silymarin, a known standardized extract obtained from seeds of Silybum marianum is widely used in treatment of several diseases of varying origin. In the present paper, we clarified the antioxidant activity of silymarin by employing various in vitro antioxidant assay such as 1,1-diphenyl-2-picryl-hydrazyl free radical (DPPH(.)) scavenging, 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical scavenging activity, total antioxidant activity determination by ferric thiocyanate, total reducing ability determination by Fe3+ - Fe2+ transformation method and Cuprac assay, superoxide anion radical scavenging by riboflavin/methionine/illuminate system, hydrogen peroxide scavenging and ferrous ions (Fe2+) chelating activities. Silymarin inhibited 82.7% lipid peroxidation of linoleic acid emulsion at 30 microg/mL concentration; butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), alpha-tocopherol and trolox indicated inhibition of 83.3, 82.1, 68.1 and 81.3% on peroxidation of linoleic acid emulsion at the same concentration, respectively. In addition, silymarin had an effective DPPH(.) scavenging, ABTS(.)+ scavenging, superoxide anion radical scavenging, hydrogen peroxide scavenging, ferric ions (Fe3+) reducing power by Fe3+-Fe2+ transformation, cupric ions (Cu2+) reducing ability by Cuprac method, and ferrous ions (Fe2+) chelating activities. Also, BHA, BHT, alpha-tocopherol and trolox, were used as the reference antioxidant and radical scavenger compounds. Moreover, this study, which clarifies antioxidant mechanism of silymarin, brings new information on the antioxidant properties of silymarin. According to the present study, silymarin had effective in vitro antioxidant and radical scavenging activity. It could be used in the pharmacological and food industry because of its antioxidant properties. PMID:18830883

Köksal, Ekrem; Gülçin, Ilhami; Beyza, Sevim; Sarikaya, Oztürk; Bursal, Ercan

2009-04-01

21

In vitro assays for studying helicase activities.  

PubMed

Unwinding of double-stranded DNA is required to create a single-stranded DNA template for essential DNA processes such as those involved in recombination, repair, and replication. A set of specialized enzymes called DNA helicases is dedicated to this purpose, catalyzing DNA strand separation by breaking hydrogen bonds and other noncovalent interactions that stably hold the two complementary DNA strands together. They use energy derived from the hydrolysis of nucleotide triphosphates for both bond breakage between complementary bases and translocation of a helicase enzyme along DNA. DNA unwinding activity catalyzed by a helicase usually exhibits a specific directionality (5' to 3' or 3' to 5') with respect to the DNA strand to which the enzyme is bound and moves. Unwinding activity ofa DNA helicase and its related properties can be easily measured in vitro using common lab equipment. We will describe the detailed methods and notes for preparation of various helicase substrates and in vitro helicase assays using the substrates prepared. PMID:19563117

Kim, Jeong-Hoon; Seo, Yeon-Soo

2009-01-01

22

In vitro leishmanicidal activity of aurones.  

PubMed

A series of aurones with drug-potential for Leishmania infections was identified in vitro using both a direct cytotoxicity assay against extracellular promastigotes of Leishmania donovani, L. infantum, L. enriettii, and L. major, and a test against intracellular amastigote forms of L. donovani residing within murine macrophages. The most active aurone (6-hydroxy-2-[phenylmethylene]-3(2H)-benzofuranone) had an EC50 of 0.45 microgram/ml in the extra-, and an EC50 of 1.40 micrograms/ml in the intracellular assay. Other aurones were active between 0.06-12.50 micrograms/ml and 0.04-7.81 micrograms/ml, respectively. When tested against murine bone marrow-derived macrophages as a mammalian host cell control, the compounds showed only moderate cytotoxicity (EC50 2.32 to > 25.0 micrograms/ml). This is the first report on aurones as a new class of natural products with leishmanicidal activity. PMID:10364835

Kayser, O; Kiderlen, A F; Folkens, U; Kolodziej, H

1999-05-01

23

Schistosomicidal evaluation of Zanthoxylum naranjillo and its isolated compounds against Schistosoma mansoni adult worms.  

PubMed

Chemical investigation of the EtOAc fraction (EF) obtained from the ethanolic extract of Zanthoxylum naranjillo (Rutaceae) leaves (EE) by preparative HPLC resulted in the isolation of protocatechuic acid (1), gallic acid (2), p-hydroxybenzoic acid (3), and 5-O-caffeoylshikimic acid (4). This is the first time that the presence of compounds 1-4 in Z. naranjillo has been reported. Compounds 1-4, the EE, and EF were tested in vitro against Schistosoma mansoni adult worms. The results showed that the S. mansoni daily egg production decreased by 29.8%, 13.5%, 28.4%, 17.7%, 16.3%, and 6.4%, respectively. Compounds 1 and 3 were also able to separate adult worm pairs into male and female. This activity may be correlated with the reduction in egg production, since 1 and 3 showed better inhibitory properties compared with 2 and 4. PMID:20158148

Braguine, Caio G; Costa, Eveline S; Magalhăes, Lizandra G; Rodrigues, Vanderlei; da Silva Filho, Ademar A; Bastos, Jairo K; Silva, Márcio L A; Cunha, Wilson R; Januário, Ana H; Pauletti, Patrícia M

2009-01-01

24

In vitro neuromuscular activity of snake venoms.  

PubMed

1. Snake venoms consist of a multitude of pharmacologically active components used for the capture of prey. Neurotoxins are particularly important in this regard, producing paralysis of skeletal muscles. These neurotoxins can be classified according to their site of action (i.e. pre- or post-synaptic). 2. Presynaptic neurotoxins, which display varying phospholipase A2 activities, have been identified in the venoms of the four major families of venomous snakes (i.e. Crotalidae, Elapidae, Hydrophiidae and Viperidae). The blockade of transmission produced by these toxins is usually characterized by a triphasic effect on acetylcholine release. Considerable work has been directed at identifying the binding site(s) on the presynaptic nerve terminal for these toxins, although their mechanism of action remains unclear. 3. Post-synaptic neurotoxins are antagonists of the nicotinic receptor on the skeletal muscle. Depending on their sequence, post-synaptic toxins are subdivided into short- and long-chain toxins. These toxins display different binding kinetics and different affinity for subtypes of nicotinic receptors. Post-synaptic neurotoxins have only been identified in venoms from the families Elapidae and Hydrophiidae. 4. Due to the high cost of developing new antivenoms and the reluctance of many companies to engage in this area of research, new methodologies are required to test the efficacy of existing antivenoms to ensure their optimal use. While chicken eggs have proven useful for the examination of haemorrhagic venoms, this procedure is not suited to venoms that primarily display neurotoxic activity. The chick biventer cervicis muscle has proven useful for this procedure, enabling the rapid screening of antivenoms against a range of venoms. 5. Historically, the lethality of snake venoms has been based on murine LD50 studies. Due to ethical reasons, these studies are being superseded by in vitro studies. Instead, the time taken to produce 90% inhibition of nerve-mediated twitches (i.e. t90) in skeletal muscle preparations can be determined. However, these two procedures result in different rank orders because they are measuring two different parameters. While murine LD50 determinations are based on "quantity", t90 values are based on how "quick" a venom acts. Therefore, knowledge of both parameters is still desirable. 6. In vitro neuromuscular preparations have proven to be invaluable tools in the examination of snake venoms and isolated neurotoxins. They will continue to play a role in further elucidating the mechanism of action of these highly potent toxins. Further study of these toxins may provide more highly specific research tools or lead compounds for pharmaceutical agents. PMID:12165047

Hodgson, Wayne C; Wickramaratna, Janith C

2002-09-01

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.

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

In vitro immunomodulatory activity of ruthenium complexes  

Microsoft Academic Search

Objective and Design: We have explored the in vitro immunomodulatory effects of pure ruthenium red and a series of pyridine and imidazole substituted ruthenium complexes (RCs). Material: Human peripheral blood lymphocytes and purified T cells were used in these studies along with various cell lines. Methods: Cells were treated with dilutions of RCs and assessed in various assays of immune

J. R. Newcomb; B. Rivnay; C. M. Bastos; T. D. Ocain; K. Gordon; P. Gregory; S. M. Turci; K. A. Sterne; M. Jesson; J. Krieger; J. C. Jenson; B. Jones

2003-01-01

27

Semisynthesis and in vitro anticancer activities of andrographolide analogues  

Microsoft Academic Search

The plant Andrographis paniculata found throughout Southeast Asia contains Andrographolide 1, a diterpenoid lactone, which has antitumour activities against in vitro and in vivo breast cancer models. In the present study, we report on the synthesis of andrographolide derivatives, 3,19-isopropylideneandrographolide (2), 14-acetyl-3,19-isopropylideneandrographolide (3) and 14-acetylandrographolide (4), and their in vitro antitumour activities against a 2-cell line panel consisting of MCF-7

Srinivasa Rao Jada; Genevieve Suseno Subur; Charlie Matthews; Ahmad Sazali Hamzah; Nordin Haji Lajis; Mohammad Said Saad; Malcolm F. G. Stevens; Johnson Stanslas

2007-01-01

28

In Vitro Antibacterial and Antifungal Activity of Salicylanilide Benzoates  

PubMed Central

The resistance to antimicrobial agents brings a need of novel antimicrobial agents. We have synthesized and found the in vitro antibacterial activity of salicylanilide esters with benzoic acid (2-(phenylcarbamoyl)phenyl benzoates) in micromolar range. They were evaluated in vitro for the activity against eight fungal and eight bacterial species. All derivatives showed a significant antibacterial activity against Gram-positive strains with minimum inhibitory concentrations ?0.98??mol/L including methicillin-resistant Staphylococcus aureus strain. The most active compounds were 5-chloro-2-(3,4-dichlorophenylcarbamoyl)phenyl benzoate and 4-chloro-2-(4-(trifluoromethyl)phenylcarbamoyl)phenyl benzoate. The antifungal activity is significantly lower.

Kratky, Martin; Vinsova, Jarmila; Buchta, Vladimir

2012-01-01

29

In vitro activity of ertapenem against selected respiratory pathogens  

Microsoft Academic Search

Objectives: The in vitro activity of ertapenem was evaluated in comparison to 21 selected agents against a large collection of recently isolated respiratory tract pathogens including: 180 Streptococcus pneumoniae, 100 Streptococcus pyogenes ,7 0Haemophilus influenzae ,7 0Moraxella catarrhalis, 100 methicillin-susceptible Staphylococcus aureus and 30 Klebsiella pneumoniae. Additional in vitro tests (time-kill curves with ertapenem alone and in combination with four

A. Marchese; L. Gualco; A. M. Schito; E. A. Debbia; G. C. Schito

2004-01-01

30

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.

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

1997-01-01

31

In Vitro Activity of Thimerosal against Ocular Pathogenic Fungi  

Microsoft Academic Search

The in vitro activity of thimerosal versus those of amphotericin B and natamycin was assessed against 244 ocular fungal isolates. The activity of thimerosal against Fusarium spp., Aspergillus spp., and Alternaria alternata was 256 times, 512 times, and 128 times, respectively, greater than that of natamycin and 64 times, 32 times, and 32 times, respectively, greater than that of amphotericin

Yan Xu; Guangren Pang; Dongqing Zhao; Chuanwen Gao; Lutan Zhou; Shengtao Sun; Bingliang Wang

2010-01-01

32

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...

33

Antiviral activities of coffee extracts in vitro.  

PubMed

Both hot water extracts of coffee grinds and instant coffee solutions inhibited the multiplication of herpes simplex virus type 1, a representative enveloped DNA virus, when they were added to the culture medium of the virus-infected cells at a dose of one fifth the concentration suitable for drinking. The antiherpetic activity was independent of the suppliers (companies) of the coffee grinds and of the locations where the coffee beans were produced. Further characterization revealed that there are two different mechanisms, by which the coffee extracts exert inhibitory activities on the virus infection; (1) a direct inactivation of the infectivity of virus particle (i.e., a virucidal activity) and (2) the inhibition of progeny infectious virus formation at the late stage of viral multiplication in the infected cells. Caffeine, but not quinic acid and chlorogenic acid, inhibited the virus multiplication to some extent, but none of them showed the virucidal activity, suggesting that other component(s) in the coffee extracts must play a role in the observed antiviral activity. In addition, the coffee extracts inhibited the multiplication of poliovirus, a non-enveloped RNA virus, but showed no virucidal effect on this virus. PMID:18314244

Utsunomiya, Hirotoshi; Ichinose, Masao; Uozaki, Misao; Tsujimoto, Kazuko; Yamasaki, Hisashi; Koyama, A Hajime

2008-06-01

34

In Vitro Activities of Six New Fluoroquinolones against Brucella melitensis  

PubMed Central

We have tested the in vitro activities of eight fluoroquinolones against 160 Brucella melitensis strains. The most active was sitafloxacin (MIC at which 90% of the isolates are inhibited [MIC90], 0.12 ?g/ml). In decreasing order, the activities (MIC90s) of the rest of the tested fluoroquinolones were as follows: levofloxacin, 0.5 ?g/ml; ciprofloxacin, trovafloxacin, and moxifloxacin, 1 ?g/ml; and ofloxacin, grepafloxacin, and gatifloxacin, 2 ?g/ml.

Trujillano-Martin, Ignacio; Garcia-Sanchez, Enrique; Martinez, Isaias Montes; Fresnadillo, Maria Jose; Garcia-Sanchez, Jose Elias; Garcia-Rodriguez, JoseAngel

1999-01-01

35

Purification and in vitro activities of rabbit platelet microbicidal proteins.  

PubMed Central

Recent in vitro studies have demonstrated that rabbit platelets release a small, cationic antimicrobial protein in response to thrombin stimulation under physiological conditions (M. R. Yeaman, S. M. Puentes, D. C. Norman, and A. S. Bayer, Infect. Immun. 60:1202-1209, 1992). This observation prompted our present investigation, focused on determining the array of antimicrobial proteins contained within rabbit platelets and their in vitro activity against common bloodstream pathogens. A group of small (6.0- to 9.0-kDa), cationic proteins with in vitro antimicrobial activity was purified from whole and thrombin-stimulated rabbit platelets by gel filtration and reversed-phase high-performance liquid chromatography. Purified proteins in micromolar concentrations (10 to 40 microg/ml) exerted in vitro microbiostatic and/or microbicidal activities against Staphylococcus aureus, Escherichia coli, and Candida albicans in a dose-dependent manner. The antimicrobial activities of proteins purified from rabbit platelet acid extracts were generally inversely related to pH, with maximal activity observed at pH 5.5. In contrast, the predominant protein isolated from thrombin-stimulated rabbit platelets, though biochemically and microbiologically similar to proteins extracted by acid, exhibited antimicrobial activities which were modestly enhanced at pH 7.2 compared with pH 5.5. Amino acid compositional analyses in combination with molecular mass determinations suggest that the majority of these proteins are distinct molecules not derived from a single common precursor. Collectively, these data indicate that rabbit platelets contain proteins which exert potent in vitro antimicrobial activity against bacterial and fungal pathogens which commonly invade the bloodstream. Moreover, several of these proteins were released from platelets stimulated with thrombin under physiological conditions and exerted potent antimicrobial activities in physiological pH ranges. These observations support the hypothesis that platelets serve an important role in host defense against infection, via localized release of antimicrobial proteins in response to stimuli associated with tissue injury or microbial colonization.

Yeaman, M R; Tang, Y Q; Shen, A J; Bayer, A S; Selsted, M E

1997-01-01

36

Antimalarial activity of plumbagin in vitro and in animal models  

PubMed Central

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

2014-01-01

37

Subicular activation preceding hippocampal ripples in vitro  

PubMed Central

Sharp wave-ripple complexes (SW-Rs), a transient form of high-frequency field oscillations observed in the hippocampus, are thought to mediate memory consolidation. They are initiated mainly in hippocampal CA3 area and propagate to the entorhinal cortex through the subiculum; however, little is known about how SW-Rs are initiated and propagate. Here, we used functional multineuronal calcium imaging to monitor SW-R-relevant neuronal activity from the subiculum at single-cell resolution. An unexpected finding was that a subset of subicular neurons was activated immediately before hippocampal SW-Rs. The SW-R-preceding activity was not abolished by surgical lesion of the CA1-to-subiculum projection, and thus, it probably arose from entorhinal inputs. Therefore, SW-Rs are likely to be triggered by entorhinal-to-CA3/CA1 inputs. Moreover, the subiculum is not merely a passive intermediate region that SW-Rs pass through, but rather, it seems to contribute to an active modification of neural information related to SW-Rs.

Norimoto, Hiroaki; Matsumoto, Nobuyoshi; Miyawaki, Takeyuki; Matsuki, Norio; Ikegaya, Yuji

2013-01-01

38

Subicular activation preceding hippocampal ripples in vitro.  

PubMed

Sharp wave-ripple complexes (SW-Rs), a transient form of high-frequency field oscillations observed in the hippocampus, are thought to mediate memory consolidation. They are initiated mainly in hippocampal CA3 area and propagate to the entorhinal cortex through the subiculum; however, little is known about how SW-Rs are initiated and propagate. Here, we used functional multineuronal calcium imaging to monitor SW-R-relevant neuronal activity from the subiculum at single-cell resolution. An unexpected finding was that a subset of subicular neurons was activated immediately before hippocampal SW-Rs. The SW-R-preceding activity was not abolished by surgical lesion of the CA1-to-subiculum projection, and thus, it probably arose from entorhinal inputs. Therefore, SW-Rs are likely to be triggered by entorhinal-to-CA3/CA1 inputs. Moreover, the subiculum is not merely a passive intermediate region that SW-Rs pass through, but rather, it seems to contribute to an active modification of neural information related to SW-Rs. PMID:24045268

Norimoto, Hiroaki; Matsumoto, Nobuyoshi; Miyawaki, Takeyuki; Matsuki, Norio; Ikegaya, Yuji

2013-01-01

39

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

40

Activity of the anthelmintic benzimidazoles against Giardia lamblia in vitro.  

PubMed

In vitro growth of the protozoan parasite Giardia lamblia was highly sensitive to certain anthelmintic benzimidazoles. Albendazole and mebendazole were 30- to 50-fold more active than metronidazole and 4- to 40-fold more active than quinacrine. Thiabendazole, a noncarbamate benzimidazole, was less active. Since lack of intestinal absorption makes mebendazole an attractive new antigiardial agent, its in vitro activity was further characterized. At low concentrations (0.05 micrograms/ml) mebendazole had a static effect on G. lamblia growth; however, lethal activity was observed at a concentration fivefold lower (0.3 micrograms/ml) than necessary for the cidal agent metronidazole. Two observations are consistent with a microtubule target for mebendazole. First, attachment of cells to the culture tube, mediated by the ventral disk and flagella, was rapidly disrupted by mebendazole treatment. Second, the characteristic cell structure was grossly distorted by treatment. No mebendazole-resistant G. lamblia were detected in a population of 10(8) cells. PMID:2230276

Edlind, T D; Hang, T L; Chakraborty, P R

1990-12-01

41

In Vitro Antibacterial Activity of Essential Oils against Streptococcus pyogenes  

PubMed Central

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

Sfeir, Julien; Lefrancois, Corinne; Baudoux, Dominique; Derbre, Severine; Licznar, Patricia

2013-01-01

42

In Vitro Antileishmanial Activity of Nicotinamide  

PubMed Central

Our study represents the first report demonstrating the antileishmanial activity of nicotinamide (NAm), a form of vitamin B3. A 5 mM concentration of NAm significantly inhibited the intracellular growth of Leishmania amastigotes and the NAD-dependent deacetylase activity carried by parasites overexpressing Leishmania major SIR2 (LmSIR2). However, the transgenic parasites were as susceptible as the wild-type parasites to NAm-induced cell growth arrest. Therefore, we conclude that NAm inhibits leishmanial growth and that overexpression of LmSIR2 does not overcome this inhibition. The mechanism of the inhibition is not defined but may include other in vivo targets. NAm may thus represent a new antileishmanial agent which could potentially be used in combination with other drugs during therapy.

Sereno, D.; Alegre, A. Monte; Silvestre, R.; Vergnes, B.; Ouaissi, A.

2005-01-01

43

[Cefamandole: in vitro and in vivo activity].  

PubMed

Among the cephalosporin antibiotics, a relatively new derivative of Cefamandole has been studied, the sodium salt of its formyl ester, Cefamandole nafate. It has shown a broad spectrum of antibiotic activity against a wide variety of Gram-positive and Gram-negative Bacteria (127 strains); the susceptibility was good even with beta-lactamase-producing bacteria. Good protective doses (PD50) were found after mice infections with Staphylococcus aureus and Salmonella wien. The pharmacokinetics of Cefamandole carried out comparatively in 5 human volunteers and in laboratory animals exhibited high levels, especially in the urines. PMID:553842

Martinetto, P; Valtz, A; Cavallo, G P; Angeretti, A

1979-01-01

44

In vitro antifungal activities of new imidazole salts towards dermatophytes.  

PubMed

The in vitro activities of two new miconazole and econazole salts with the sulphosalicylic acid against 71 clinical isolates of dermatophytes were evaluated in comparison with those of miconazole, miconazole nitrate, econazole and econazole nitrate. Miconazole sulphosalicylate and econazole sulphosalicylate were equally effective in inhibiting the fungal growth compared with miconazole, econazole, and their nitrates. PMID:2267004

Tullio, V; Cuffini, A M; Carlone, N A

1990-05-01

45

In vitro activity of ciprofloxacin, norfloxacin and nalidixic acid  

Microsoft Academic Search

The in vitro antibacterial activity of the new quinoline derivative ciprofloxacin (BAY 0 9867) was evaluated in comparison to norfloxacin and nalidixic acid using 495 clinical strains of gram-negative and gram-positive bacteria. The compound was highly active againstEnterobacteriaceae, with MICs ranging from 0.008 mg\\/l to 4 mg\\/l, whereas the MICs of norfloxacin ranged from 0.03 mg\\/l to 16 mg\\/l. All

A. Bauernfeind; C. Petermüller

1983-01-01

46

In vitro activity of LY146032 (Daptomycin), a new peptolide  

Microsoft Academic Search

The in vitro activity of LY146032, a new peptolide antibiotic, was compared with those of vancomycin, teicoplanin, imipenem, amoxicillin and erythromycin. LY146032 inhibited 90% ofStaphylococcus aureus andStaphylococcus epidermidis, including methicillin-resistant isolates at ? 1?g\\/ml. Its activity was comparableto those of vancomycin and teicoplanin. MIC90s for the beta-hemolytic streptococci varied from 0.25 ?g\\/ml for group B streptococci to 4?g\\/ml for some

F. Ehlert; H. C. Neu

1987-01-01

47

In vitro antiplasmodial activity of extracts of Argentinian plants.  

PubMed

Fifteen extracts from nine selected Argentine medicinal plants were tested for their antiplasmodial activity in vitro by assessing their ability to inhibit the uptake of [3H]-hypoxanthine into the Plasmodium falciparum K1 pyrimethamine/chloroquine resistant strain. The methanol extract of Satureja parvifolia showed good antiplasmodial activity (IC(50) 3 microg/ml). Inhibition of the growth of P. falciparum was also observed with aqueous extracts of Buddleja globosa and S. parvifolia. PMID:12007706

Debenedetti, S; Muschietti, L; van Baren, C; Clavin, M; Broussalis, A; Martino, V; Houghton, P J; Warhurst, D; Steele, J

2002-05-01

48

Icariin suppresses bone resorption activity of rabbit osteoclasts in vitro  

Microsoft Academic Search

The effect of icariin on the bone resorption activity of rabbit osteoclasts is assessed in vitro. Osteoclasts were isolated from Japanese white rabbits and cultured on plates with a sterilized bone slice in each well.\\u000a After treatment with icariin at various concentrations, the bone resorption activity of osteoclasts was evaluated by examining\\u000a pit areas, superoxide anion (·O\\u000a 2\\u000a ?\\u000a )

Jian Huang; JinChao Zhang; TianLan Zhang; Kui Wang

2007-01-01

49

Controversial Constitutive TSHR Activity: Patients, Physiology, and In Vitro Characterization.  

PubMed

G protein-coupled receptors constitute a large family of transmembrane receptors, which activate cellular responses by signal transmission and regulation of second messenger metabolism after ligand binding. For several of these receptors it is known that they also signal ligand-independently. The G protein-coupled thyroid stimulating hormone receptor (TSHR) is characterized by a high level of constitutive activity in the wild type state. However, little is known yet concerning the physiological relevance of the constitutive wild type TSHR activity. Certainly, knowledge of the physiological relevance of constitutive wild type receptor activity is necessary to better understand thyroid physiology and it is a prerequisite for the development of better therapies for nonautoimmune hyperthyroidism and thyroid cancer. Based on a literature search regarding all published TSHR mutations, this review covers several mutations which are clearly associated with a hyperthyroidism-phenotype, but interestingly show a lack of constitutive activity determined by in vitro characterization. Possible reasons for the observed discrepancies between clinical phenotypes and in vitro characterization results for constitutive TSHR activity are reviewed. All current in vitro characterization methods for constitutive TSHR mutations are "preliminary attempts" and may well be revised by more comprehensive and even better approaches. However, a standardized approach for the determination of constitutive activity can help to identify TSHR mutations for which the investigation of additional signaling mechanisms would be most interesting to find explanations for the current clinical phenotype/in vitro discrepancies and thereby also define suitable methods to explore the physiological relevance of constitutive wild type TSHR activity. PMID:24845969

Huth, S; Jaeschke, H; Schaarschmidt, J; Paschke, R

2014-06-01

50

In vitro study of oxytetracycline adsorption on activated charcoal.  

PubMed

In vitro adsorption experiments simulating pH in gastric environment and using Langmuir isotherm, showed that 408 mg of oxytetracycline was adsorbed per gram of activated charcoal. Langmuir isotherm fitted adsorption data better than a Freundlich isotherm. Freundlich isotherm showed a specific adsorption capacity of 518 mg/g for activated charcoal. Both isotherm parameters indicated a strong oxytetracycline adsorption on activated charcoal in terms of quantity and binding strength. The results demonstrate that the concomitant use of oxytetracyline and activated charcoal should be avoided. PMID:10968607

Alegakis, A K; Tzatzarakis, M N; Tsatsakis, A M; Vlachonikolis, I G; Liakou, V

2000-09-01

51

In vitro antiplasmodial activity of Central American medicinal plants.  

PubMed

The in vitro antiplasmodial activities of 14 plant species traditionally used in Central America for the treatment of malaria or fever were evaluated. Lipophilic extracts of Piper hispidum, Siparuna andina, S. pauciflora, S. tonduziana, and Xylopia cf. frutescens, proved to be active against both a chloroquine-sensitive and a resistant strain of Plasmodium falciparum. IC50 values ranged between 3.0 microg/ml and 21.9 microg/ml; however, moderate cytotoxicity of active extracts was observed. Bioactivity-guided fractionation of Piper hispidum yielded 2',4, 6'-trihydroxy-4'-methoxydihydrochalcone (asebogenin) as an active compound. PMID:10540301

Jenett-Siems, K; Mockenhaupt, F P; Bienzle, U; Gupta, M P; Eich, E

1999-09-01

52

Antifungal activity of the allylamine derivative terbinafine in vitro.  

PubMed Central

Terbinafine, an allylamine derivative, represents the most effective of this new chemical class of antimycotic compounds. Under in vitro conditions, terbinafine proved to be highly active against dermatophytes (MIC range, 0.001 to 0.01 microgram/ml), aspergilli (MIC range, 0.05 to 1.56 micrograms/ml), and Sporothrix schenckii (MIC range, 0.1 to 0.4 microgram/ml) and also exerted good activity against yeasts (MIC range, 0.1 to greater than 100 micrograms/ml). The growth of Malassezia furfur was inhibited also (MIC range, 0.2 to 0.8 microgram/ml). Terbinafine displays a primary fungicidal action against dermatophytes, other filamentous fungi, and S. schenckii. The type of action against yeasts is species dependent and can be primarily fungicidal (Candida parapsilosis) or fungistatic (Candida albicans). The in vitro activity of terbinafine is pH dependent and rises with increasing pH value.

Petranyi, G; Meingassner, J G; Mieth, H

1987-01-01

53

In Vitro Phytotoxicity and Antioxidant Activity of Selected Flavonoids  

PubMed Central

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

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

2012-01-01

54

In vitro antioxidant activity of Anthriscus cerefolium L. (Hoffm.) extracts.  

PubMed

Standardised aqueous extracts of chervil (Anthriscus cerefolium L. Hoffm.) (Apiacae) were investigated for antioxidant effect. Numerous in vitro test methods were used to determine whether the extracts, from different vegetative parts (root, herb) had H-donor, metal binding, reductive, free radical scavenging and membrane protective activity. Apiin was used as a reference material. The herb extract showed better activity in all experiments than the root extract. The present results underline that the wateric chervil extracts have antioxidant and anti-lipoperoxidant activity. PMID:10722209

Fejes, S; Blázovics, A; Lugasi, A; Lemberkovics, E; Petri, G; Kéry, A

2000-03-01

55

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

56

Activated neutrophils inhibit cerebrovascular endothelium-dependent relaxations in vitro.  

PubMed

The effect of formyl-Met-Leu-Phe- (fMLP-) activated feline neutrophil granulocytes on endothelium-dependent and independent relaxations was studied in the middle cerebral artery of the cat in vitro. Endothelium-dependent relaxations caused by acetylcholine and ATP were markedly inhibited after 30 minutes of incubation of the vessels with neutrophils (5000 cells/microliter) in the presence of 5 microM fMLP, followed by a replacement of the bath solution in order to remove the neutrophils from the medium. Direct vasorelaxations in response to the nitric oxide donor compound SIN-1, however, remained unchanged. Both neutrophils and fMLP caused transient contractions during the incubation period. The present study provides direct evidence for the ability of activated neutrophils to cause an inhibition of vascular endothelium-dependent responses in vitro. PMID:1895871

Csaki, C; Szabo, C; Benyo, Z; Reivich, M; Kovach, A G

1991-01-01

57

In vitro activity of terpenes against Candida biofilms  

Microsoft Academic Search

The antibiofilm activity of 10 terpenes was tested in vitro against three Candida species by 24-h treatment of biofilms aged 1–5 days. Treatment of 24-h-old Candida albicans biofilms with carvacrol, geraniol or thymol (0.06%) resulted in >80% inhibition. Carvacrol (0.03%) inhibition was ?75% independent of the age of the C. albicans biofilm. Carvacrol (0.125%) inhibition was >75% against Candida glabrata

Stéphanie Dalleau; Estelle Cateau; Thierry Bergčs; Jean-Marc Berjeaud; Christine Imbert

2008-01-01

58

Risperidone and Paliperidone Inhibit P-Glycoprotein Activity In Vitro  

Microsoft Academic Search

Risperidone (RSP) and its major active metabolite, 9-hydroxy-risperidone (paliperidone, PALI), are substrates of the drug transporter P-glycoprotein (P-gp). The goal of this study was to examine the in vitro effects of RSP and PALI on P-gp-mediated transport. The intracellular accumulation of rhodamine123 (Rh123) and doxorubicin (DOX) were examined in LLC-PK1\\/MDR1 cells to evaluate P-gp inhibition by RSP and PALI. Both

Hao-Jie Zhu; Jun-Sheng Wang; John S Markowitz; Jennifer L Donovan; Bryan B Gibson; C Lindsay DeVane

2007-01-01

59

Antioxidant activities of flavidin in different in vitro model systems  

Microsoft Academic Search

Flavidin was isolated from Orchidaceae species and purified by silica gel column chromatography. The structure was identified using physical and spectral (1H, 13C NMR, and mass) data. Antioxidant potency of flavidin was investigated employing various established in vitro model systems viz., ?-carotene-linoleate, 1,1-diphenyl-2-picryl hydrazyl (DPPH), phosphomolybdenum method, and scavenging of hydrogen peroxide methods. Flavidin showed very good antioxidant activity (90.2%)

Guddadarangavvanahally K. Jayaprakasha; Lingamallu Jaganmohan Rao; Kunnumpurath K. Sakariah

2004-01-01

60

In vitro adsorption of dichlorvos and parathion by activated charcoal.  

PubMed

Accidental and suicidal ingestions of organophosphate compounds continue to be a common occurrence in Turkey. Activated charcoal administration without gastric emptying has been advocated as primary therapy in most acute poisoning cases, although some references do not recommend activated charcoal use in organophosphate poisoning. This study was performed to determine the in vitro adsorption of dimethyl dichlorovinyl phosphate (dichlorvos) and parathion by activated charcoal over a wide range of charcoal:organophosphate ratios (1:1, 2.5:1, 5:1, 10:1 and 20:1, g:g). The charcoal binding ability of dichlorvos and parathion were studied in both pH 1.2 and pH 7 environments. The supernatant was extracted with n-hexane and then analyzed by gas chromatography. Each incremental increase in charcoal dose increased the percent adsorption of dichlorvos and parathion. At the 20:1 ratio, 82.8 +/- 2.0/87.3 +/- 2.9% (pH 1.2/7.0) of dichlorvos and 59.3 +/- 4.5/64.5 +/- 6.1% (pH 1.2/7.0) of parathion were bound by activated charcoal. There were no significant differences in amounts of compound bound in the acid and neutral solutions. Large doses of activated charcoal effectively bind dichlorvos and parathion in vitro. In vivo research should be performed to determine activated charcoal's role in organophosphate poisoning cases. PMID:8145355

Guven, H; Tuncok, Y; Gidener, S; Gelal, A; Demetci, M; Fowler, J; Apaydin, S; Keskin, M

1994-01-01

61

New imidazole derivates: in-vitro activity on dermatophytes.  

PubMed

The in-vitro activities of two new miconazole and econazole salts (sulfosalicylic acid formulation) against 98 clinical isolates of dermatophytes were evaluated, in comparison to those of miconazole, miconazole nitrate, econazole and econazole nitrate. Miconazole sulfosalicylate and econazole sulfosalicylate exhibited good activity towards all the dermatophytes tested, although econazole and its derivatives were more efficacious than miconazole and its salts. The new imidazoles were equally effective in inhibiting the fungal growth with respect to miconazole, miconazole nitrate, econazole and econazole nitrate. PMID:12041784

Tullio, V; Cuffini, A M; Carlone, N A; Spignoli, G

1991-01-01

62

Hepatoprotective and antihyperliposis activities of in vitro cultured Anoectochilus formosanus.  

PubMed

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

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

2003-01-01

63

Antioxidant activities of flavidin in different in vitro model systems.  

PubMed

Flavidin was isolated from Orchidaceae species and purified by silica gel column chromatography. The structure was identified using physical and spectral ((1)H, (13)C NMR, and mass) data. Antioxidant potency of flavidin was investigated employing various established in vitro model systems viz., beta-carotene-linoleate, 1,1-diphenyl-2-picryl hydrazyl (DPPH), phosphomolybdenum method, and scavenging of hydrogen peroxide methods. Flavidin showed very good antioxidant activity (90.2%) and almost equivalent to that of BHA at 50ppm level by beta-carotene-linoleate method. Radical scavenging activity of flavidin was compared with BHA at 5, 10, 20, and 40ppm concentration and flavidin showed more radical scavenging activity than BHA at all the tested concentrations. Furthermore, flavidin showed very good antioxidant capacity by the formation of phosphomolybdenum complex method. Besides this, flavidin showed effective hydrogen peroxide scavenging activity. The data obtained in the in vitro models clearly establish the antioxidant potency of flavidin. However, comprehensive studies need to be conducted to ascertain the in vivo safety of flavidin in experimental animal models. This is the first report on antioxidant activity of 9,10-dihydro-5H-phenanthro-(4,5 bcd)-pyrans/flavidin type of compounds. PMID:15351397

Jayaprakasha, Guddadarangavvanahally K; Jaganmohan Rao, Lingamallu; Sakariah, Kunnumpurath K

2004-10-01

64

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

65

Activin A inhibits activation of human primordial follicles in vitro  

PubMed Central

Purpose To determine whether Activin A affects the activation and survival of human primordial follicles in vitro. Methods Ovarian cortical biopsies from eight women undergoing elective caesarean sections or benign gynaecological procedures were taken and cut into small pieces (1–3 mm3), cultured in serum-free medium for 7 days with/without human recombinant Activin A at a concentration of either 50 or 100 ng/ml. Ovarian tissue were analysed by histology for follicle viability, development and density. Result(s) Significant activation of primordial follicles within cultured cortical tissue was observed after 7 days in control medium. However, medium supplemented with Activin A at 50 ng/ml resulted in significant inhibition of follicular activation. Increasing the concentration of Activin A to 100 ng/ml reversed the inhibitory effect. The effect of Activin A appeared to be specific to activation of non-growing (primordial) follicles into the growing population since no significant differences in follicle viability was observed between treatment groups. Conclusion(s) Activin A at a concentration of 50 ng/ml can inhibit the spontaneous activation of human primordial follicles in vitro indicating that this may be a component of the signalling mechanisms that maintain follicular quiescence.

Ding, Chi Christina; Thong, K. Joo; Krishna, Archie

2010-01-01

66

In vitro activity of doripenem against Acinetobacter baumannii clinical isolates.  

PubMed

Doripenem is a carbapenem with activity against Gram-positive and Gram-negative pathogens. This study evaluated the in vitro activity of doripenem against a collection of 87 Acinetobacter baumannii clinical isolates, showing that the activity of doripenem was superior to imipenem and meropenem for strains carrying the bla(OXA-58) gene. A. baumannii clinical isolates expressing the bla(OXA-24) gene were resistant to doripenem, imipenem and meropenem. However, in clinical isolates expressing the bla(OXA-58) gene, the percentage of isolates with a doripenem minimum inhibitory concentration >8microg/mL was much lower than that of imipenem and meropenem. This study shows that the activity of doripenem was superior to imipenem and meropenem for strains carrying the bla(OXA-58) gene. PMID:18977642

Marti, Sara; Sánchez-Céspedes, Javier; Alba, Verónica; Vila, Jordi

2009-02-01

67

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.

Jura, Heike; Bader, Augustinus; Frosch, Matthias

1998-01-01

68

Antiprotozoal and cytotoxic activities in vitro of Colombian Annonaceae.  

PubMed

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

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

2007-05-22

69

MEA-based recording of neuronal activity in vitro.  

PubMed

Based on the advantages of MEA-based recording, developmental changes of spontaneous activity and tetanus-induced modification of evoked activity were studied. Rat cortical neurons were cultured on MEAs and the spontaneous activity was continuously monitored for two months. The activity started a few days after plating. During the second week, the cultures generated periodic synchronized bursts, which were the characteristic properties of cortical neurons in vitro. In about one month, the cultured networks reached a steady state. Between these two, we found a critical period during which only weak activities were generated. This critical period might reflect the transition from immature networks to mature networks including precisely controlled excitatory and inhibitory synapses. We could elicit clear evoked responses with high reproducibility in mature cultures. A focal tetanic stimulation was applied to the mature cultures and how the tetanus affects 64 kinds of evoked activity was studied. The evoked responses showed bi-directional changes in their propagation patterns, potentiation and depression. These induced changes reflected the correlation properties with the tetanized activity pattern. The next step will be the combination of long-term recording and multi-site stimulation. How long does the induced change last, as well as how additional strong activity affects the previously induced changes, will be studied. PMID:18075122

Jimbo, Y

2007-11-01

70

In vitro activity of ceftobiprole against Acinetobacter baumannii clinical isolates.  

PubMed

Acinetobacter baumannii is a multiresistant opportunistic nosocomial pathogen responsible for outbreaks worldwide. The main infection caused by this microorganism is nosocomial pneumonia, in particular ventilator-associated pneumonia in patients in Intensive Care Units. Treatment of these nosocomial infections is becoming problematic because the level of resistance to antimicrobial agents is rising. Ceftobiprole is a new cephalosporin with activity against Gram-positive and Gram-negative pathogens. This study evaluated the in vitro activity of ceftobiprole against a collection of 58 A. baumannii clinical isolates and showed that the activity of ceftobiprole was superior to ceftazidime and cefepime when the bla(ADC)-like gene was not expressed or was expressed at a low level. PMID:19406625

Marti, Sara; Sánchez-Céspedes, Javier; Espinal, Paula; Vila, Jordi

2009-09-01

71

Spermicidal activity of Indian seaweeds: an in vitro study.  

PubMed

Contraceptive properties of seaweeds are still stands as lacuna; in this context, the screening of in vitro male contraceptive properties of crude ethanolic extract of Indian seaweeds against normal human sperm is carried out. In total, twelve seaweeds were screened for in vitro spermicidal activity. Among these twelve seaweeds, Halimeda gracilis showed 100% inhibition of human spermatozoa at 10 mg ml(-1) concentration in 20 s and its EC50 value was 2.05 mg ml(-1) in 20 s. Further, dose- and time-dependent spermicidal assay revealed that the sperm was completely immobilised for 20 s. Plasma membrane of sperm was damaged due to the exposure of H. gracilis extract. MTT assay with H. gracilis extract showed 88.5% of cytotoxic incidence. H. gracilis extract tested for cytotoxicity against Artemia salina recorded LC50 value of 34.8 ?g ml(-1) . Phytochemical analysis of H. gracilis extract evidenced the presence of alkaloids, flavonoids, proteins and sugars. Results of this study clearly inferred that the synergistic effect of active principles reside within the H. gracilis extract had shown better contraceptive activity. PMID:23557355

Prakash, S; Ravikumar, S; Reddy, K V R; Kannapiran, E

2014-05-01

72

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.

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

73

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

74

In vitro antioxidant activities of the polysaccharides from Tricholoma lobayense.  

PubMed

The antioxidant activities of three polysaccharide components (TLH-1, TLH-2, TLH-3) extracted from Tricholoma lobayense were evaluated by three different in vitro methods, namely superoxide radical (O(2)(-)) scavenging activity, inhibition of mice erythrocyte hemolysis (MEH) and malondialdehyde (MDA) mediated by hydrogen peroxide (H(2)O(2)) and investigation of oxidative modification of human serum albumin (HSA) induced by 2,2-azobis(2-amidinopropane)dihydrochloride (AAPH) through fluorescence spectroscopy. The antioxidant experiments showed that the polysaccharides had a notable activity in scavenging O(2)(-) in a concentration-dependent manner; H(2)O(2)-induced MEH and formation of MDA were effectively inhibited; by fluorescence spectroscopy, it was demonstrated that the polysaccharides could obviously inhibit AAPH-induced oxidative modification of HSA. The experimental data obtained from the in vitro models clearly revealed that TLH-3 had stronger antioxidant potency than TLH-1 and TLH-2, which indicated that TLH-3 might be exploited as effective natural antioxidant to alleviate oxidative stress. PMID:22305884

Wang, Cui; Chen, Yan; Hu, Meili; Ding, Jingna; Xu, Cunji; Wang, Ruijun

2012-04-01

75

In vitro activity of roxithromycin against Moraxella catarrhalis.  

PubMed

The in vitro activity of roxithromycin was compared with that of the other antimicrobial agents (erythromycin, tetracycline, ampicillin, and cotrimoxazole) against 188 distinct clinical isolates of Moraxella catarrhalis. Of these, 106 strains (66%) produced beta-lactamase. The MIC90 of roxithromycin was 0.25 micrograms/ml compared with values of 0.5, 1, greater than 8, greater than 8:0.4 micrograms/ml for erythromycin, tetracycline, ampicillin, and sulfamethoxazole-trimethoprim, respectively. These results, allied with its improved pharmacokinetic properties, suggest that roxithromycin should be an effective treatment in children and adults for upper and lower respiratory tract infections caused by M. catarrhalis. PMID:1617926

Spencer, R C; Wheat, P F

1992-01-01

76

In vitro screening of Indian medicinal plants for antiplasmodial activity.  

PubMed

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 following five species seems to be of special interest for further antimalarial studies, Casearia elliptica, Holarrhena pubescens, Pongamia pinnata, Soymida febrifuga, and Plumbago zeylanica. PMID:11167038

Simonsen, H T; Nordskjold, J B; Smitt, U W; Nyman, U; Palpu, P; Joshi, P; Varughese, G

2001-02-01

77

Spontaneous activity of rat pretectal nuclear complex neurons in vitro  

PubMed Central

Background Neurons in the mammalian pretectum are involved in the control of various visual and oculomotor tasks. Because functionally independent pretectal cell populations show a wide variation of response types to visual stimulation in vivo, they may also differ in their intrinsic properties when recorded in vitro. We therefore performed whole-cell patch clamp recordings from neurons in the caudal third of the pretectal nuclear complex in frontal brain slices obtained from 3 to 6 week old hooded rats and tried to classify pretectal neurons electrophysiologically. Results Pretectal neurons showed various response types to intracellular depolarizations, including bursting and regular firing behavior. One population of pretectal nuclear complex neurons could be particularly distinguished from others because they displayed spontaneous activity in vitro. These cells had more positive resting potentials and higher input resistances than cells that were not spontaneously active. The maintained firing of spontaneously active pretectal cells was characterized by only small variances in interspike intervals and thus showed a regular temporal patterning. The firing rate was directly correlated to the membrane potential. Removing excitatory inputs by blockade of AMPA and/or NMDA receptors did not change the spontaneous activity. Simultaneous blockade of excitatory and inhibitory synaptic input by a substitution of extracellular calcium with cobalt neither changed the firing rate nor its temporal patterning. Each action potential was preceeded by a depolarizing inward current which was insensitive to calcium removal but which disappeared in the presence of tetrodotoxin. Conclusions Our results indicate that a specific subpopulation of pretectal neurons is capable of generating maintained activity in the absence of any external synaptic input. This maintained activity depends on a sodium conductance and is independent from calcium currents.

Prochnow, Nora; Schmidt, Matthias

2004-01-01

78

In vitro neuronal network activity in NMDA receptor encephalitis  

PubMed Central

Background Anti-NMDA-encephalitis is caused by antibodies against the N-methyl-D-aspartate receptor (NMDAR) and characterized by a severe encephalopathy with psychosis, epileptic seizures and autonomic disturbances. It predominantly occurs in young women and is associated in 59% with an ovarian teratoma. Results We describe effects of cerebrospinal fluid (CSF) from an anti-N-methyl-D-aspartate receptor (NMDAR) encephalitis patient on in vitro neuronal network activity (ivNNA). In vitro NNA of dissociated primary rat cortical populations was recorded by the microelectrode array (MEA) system. The 23-year old patient was severely affected but showed an excellent recovery following multimodal immunomodulatory therapy and removal of an ovarian teratoma. Patient CSF (pCSF) taken during the initial weeks after disease onset suppressed global spike- and burst rates of ivNNA in contrast to pCSF sampled after clinical recovery and decrease of NMDAR antibody titers. The synchrony of pCSF-affected ivNNA remained unaltered during the course of the disease. Conclusion Patient CSF directly suppresses global activity of neuronal networks recorded by the MEA system. In contrast, pCSF did not regulate the synchrony of ivNNA suggesting that NMDAR antibodies selectively regulate distinct parameters of ivNNA while sparing their functional connectivity. Thus, assessing ivNNA could represent a new technique to evaluate functional consequences of autoimmune encephalitis-related CSF changes.

2013-01-01

79

Inhibitory Action of Quercetin on Eosinophil Activation In Vitro  

PubMed Central

The influence of quercetin on eosinophil functions was examined in vitro and in vivo. The first set of experiments was undertaken to examine whether quercetin could suppress eosinophilia and IgE hyperproduction induced by Mesocestoides corti infection in BALB/c mice. The number of peripheral blood eosinophils and IgE levels were examined 21 days after infection. Oral administration of quercetin for 21 days could not suppress both peripheral blood eosinophilia and IgE hyperproduction, even when 20.0?mg/kg quercetin was used for treatment. The second part of the experiment was designed to examine the influence of quercetin on eosinophil activation induced by SCF stimulation in vitro. Eosinophils were obtained from M. corti-infected mice and stimulated with SCF in the presence of various concentrations of quercetin for 24?h. The addition of quercetin into cell cultures could suppress eosinophil activation induced by SCF stimulation as assessed by measuring the contents of RANTES, MIP-1?, ECP, and MBP in culture supernatants. The minimum concentration of quercetin which caused significant suppression of factor secretion was 5.0??M. These results may suggest that quercetin will be a good candidate for the supplement on the management of eosinophil-mediated diseases, such as allergic rhinitis and asthma.

2013-01-01

80

In vitro trypanocidal activity of phenolic derivatives from Peperomia obtusifolia.  

PubMed

The trypanocidal activity of crude extracts and fractions from the leaves and stems of Peperomia obtusifolia (Piperaceae) was evaluated in vitro against the epimastigote forms of Trypanosoma cruzi. Bioactivity-guided fractionation of the most active extracts afforded seven known compounds, including three chromanes, two furofuran lignans and two flavone C-diglycosides. The most active compounds were the chromanes peperobtusin A and 3,4-dihydro-5-hydroxy-2,7-dimethyl-8-(2''-methyl-2''-butenyl)-2-(4'-methyl-1',3'-pentadienyl)-2 H-1-benzopyran-6-carboxylic acid, with IC (50) values of 3.1 microM (almost three times more active than the positive control benznidazole, IC (50) 10.4 microM) and 27.0 microM, respectively. Cytotoxicity assays using peritoneal murine macrophages indicated that the chromanes were not toxic at the level of the IC (50) for trypanocidal activity. This is the first report on the trypanocidal activity besides unspecific cytotoxicity of chromanes from Peperomia species. Additionally it represents the first time isolation of 3,4-dihydro-5-hydroxy-2,7-dimethyl-8-(2''-methyl-2''-butenyl)-2-(4'-methyl-1',3'-pentadienyl)-2 H-1-benzopyran-6-carboxylic acid from P. obtusifolia. PMID:19241331

da Silva Mota, Jonas; Leite, Ana Cristina; Batista Junior, Joăo Marcos; Noelí López, Silvia; Luz Ambrósio, Daniela; Duó Passerini, Gabriela; Kato, Massuo Jorge; da Silva Bolzani, Vanderlan; Barretto Cicarelli, Regina Maria; Furlan, Maysa

2009-05-01

81

Latanoprost exerts neuroprotective activity in vitro and in vivo.  

PubMed

Prostaglandins may influence cyclo-oxygenase (COX-2) and nitric oxide (NO) synthase activity, thus interfering with ischemia-induced neurotoxic processes. The prostaglandin synthetic derivative, latanoprost was tested in different in vivo and in vitro models of neuronal damage in order to study its influence on these processes. Ischemia was induced in rats by bilateral occlusion of the carotid arteries for 30 min. Latanoprost (0.01 mg x kg(-1)per die, i.p. for 3 days) or the ionotropic glutamate receptors antagonist, MK-801 (0.1 mg x kg(-1)per die, i.p. for 3 days) were equal in preventing lactate accumulation in retinal tissue of animals subjected to acute ischemia. Similar results were obtained in animals with retinal ischemia induced by increasing intraocular pressure to 120 mm Hg for 45 min. PGF2alpha, PGE2, latanoprost and acid of latanoprost (PhXA85) reduced the release of LDH from primary cultures of human retinal cells in vitro subjected to glutamate (10 microM) or hypoxia/re-oxygenation exposure. This effect was observed only at concentrations of 1-0.01 microM for PGF2alpha and PGE2, and of 0.1-0.001 microM for latanoprost (0.01 microM-0.1 nM for PhXA85). The COX-2 activity in cultured retinal cells exposed to glutamate was measured as PGE2 production when latanoprost was applied compared to arachidonic acid (AA) at different molar concentrations. The COX-2 activity was reduced by arachidonic acid (0.1-0.01 microM) as well as by latanoprost (0.1-0.001 microM) and PhXA85 (0.01-0.001 microM) in retinal cells exposed to glutamate. Inhibition of inducible NO synthase was also found with the same drug concentrations. These results suggest that latanoprost exerts a neuroprotective activity in vitro and in vivo. This effect seems to be present only at low concentrations of the drug. A negative feedback on neuronal COX-2 activity may be possibly involved. PMID:11273675

Drago, F; Valzelli, S; Emmi, I; Marino, A; Scalia, C C; Marino, V

2001-04-01

82

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.

Sharma, Uma Shankar; Kumar, Arun

2011-01-01

83

In vitro Antioxidant Activities of Trianthema portulacastrum L. Hydrolysates  

PubMed Central

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

Yaqoob, Sadaf; Sultana, Bushra; Mushtaq, Muhammad

2014-01-01

84

Quantification of the in vitro activity of some compounds with spermicidal activity.  

PubMed

The in vitro spermicidal activity of the commonly used surfactant spermicides and the antiseptic chlorhexidine, were quantified in a statistically reproducible manner, using donor semen and image capture analysis. The spermicidal activity was expressed as the ED50 under defined assay conditions. Using these parameters, the order of spermicidal activity was: Menfegol > nonoxynol-9 approximately benzalkonium chloride > sodium docusate > chlorhexidine. These differences were statistically significant. PMID:1283567

Chantler, E; Fisher, H; Solanki, S; Elstein, M

1992-12-01

85

In vitro activity of L-627, a new carbapenem.  

PubMed

The in vitro activity of L-627, a new parenterally administered carbapenem, was compared with those of imipenem, meropenem, FCE 22101 (a penem), ceftazidime, and ceftriaxone. L-627 was active against members of the family Enterobacteriaceae (MIC for 90% of strains tested [MIC90] ranging from 0.03 to 4 micrograms/ml). L-627 displayed activity equal to that of meropenem against Pseudomonas aeruginosa (MIC90, 2 micrograms/ml), although, as with other carbapenems, the antipseudomonal activity was reduced against D2-deficient strains. Staphylococci and streptococci were susceptible (MIC90 of 1.0 micrograms/ml for Staphylococcus aureus and 0.015 micrograms/ml for group A streptococci). L-627 also had activity against anaerobic bacteria (MIC90, 2.0 micrograms/ml for Bacteroides fragilis). Neisseria gonorrhoeae and Neisseria meningitidis were highly susceptible (MIC90, 0.06 micrograms/ml), and against the common respiratory pathogens (Haemophilus influenzae, Streptococcus pneumoniae, and Moraxella catarrhalis), the MIC90s were less than or equal to 2.0 micrograms/ml. The protein binding of L-627 ranged from 13.8 to 22%, depending on the concentration. The presence of human serum had little effect on the MIC or MBC of L-627. These results suggest that L-627 merits further study in the treatment of infections caused by a wide range of pathogens. PMID:1416883

Catchpole, C R; Wise, R; Thornber, D; Andrews, J M

1992-09-01

86

In vitro radical scavanging activities of Chrysaora quinquecirrha nematocyst venom.  

PubMed

The venom of Chrysaora quinquecirrha (sea nettle) contains several toxins that have bioactivity in mammals. In our study we aimed to extract proteins from Chrysaora quinquecirrha and to test the antioxidant potential of both crude protein and purified fractions. Proteins extracted from sea nettle nematocyst venom were purified through Sephadex G-100 column chromatography. The molecular weight of purified proteins was determined by gel filtration and SDS-PAGE and was found to be 105, 65, and 9 kDa for Frc-1, Frc-2, Frc-3, respectively. The in vitro antioxidant potential of Chrysaora quinquecirrha was evaluated in different systems viz. radical scavenging activity by DPPH reduction, superoxide radical scavenging activity in PMS/NADH-NBT system, hydroxyl radical by Fe(3+)-Ascorbate-EDTA-H2O2 system and nitric oxide (NO) radical scavenging activity in sodium nitroprusside/Greiss reagent system. Frc-3 displayed the maximal antioxidant activity and found to have different levels of antioxidant properties in the models tested. In scavenging hydroxyl radicals, its activity was intense (IC(50) = 50.8 ?g/mL) while in scavenging NO radical, it was moderate (IC(50) = 381.4 ?g/mL). PMID:22495478

Balamurugan, E; Menon, V P

2009-04-01

87

In vitro antibacterial activity of roselle calyx and protocatechuic acid.  

PubMed

The in vitro inhibitory effect of roselle calyx and protocatechuic acid, a compound derived from roselle calyx, on the growth of methicillin-resistant Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa and Acinetobacter baumannii was studied. The data from inhibition zone and minimum inhibitory concentration (MIC) values showed that both roselle calyx extract and protocatechuic acid inhibited effectively the growth of all test bacterial pathogens, the antibacterial activity of protocatechuic acid being significantly greater than roselle calyx (p < 0.05). Furthermore, heat treatment did not affect the antibacterial activity of roselle calyx and protocatechuic acid against all test pathogens. The time-kill data from protocatechuic acid showed this agent provided concentration dependent antibacterial activities in broth and human plasma (p < 0.05); however, protocatechuic acid showed less inhibitory activity in human plasma than in broth (p < 0.05). These agents based on their lower MIC values, heat tolerance and concentration dependent antibacterial activity may be useful in clinical infection prevention or therapy. PMID:16317650

Liu, Keh-sen; Tsao, Shyh-ming; Yin, Mei-chin

2005-11-01

88

In vitro radical scavenging activity of two Columbian Magnoliaceae  

NASA Astrophysics Data System (ADS)

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

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

2005-08-01

89

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

90

In vitro activity of A-16686, a potential antiplaque agent.  

PubMed Central

A-16686, a new glycoproteide antibiotic from Actinoplanes sp., was evaluated as a potential antiplaque agent in comparison with chlorhexidine, benzalkonium chloride, and cetylpyridinium chloride. A-16686 had good activity against gram-positive organisms associated with dental plaque (various streptococci, Streptococcus mutans in particular, lactobacilli, Actinomyces viscosus, and Actinomyces naeslundii); most of the strains tested were clinical isolates. It was bactericidal for streptococci (MBC/MIC ratio of less than or equal to 8 for 92% of the strains) and for growing cells of S. mutans briefly exposed to antibiotic (99.9% killing within 5 min of contact with 200 micrograms of A-16686 per ml). It also inhibited the in vitro plaque formation by S. mutans and had good activity against preformed plaques. For most cases, its activity was comparable to those of chlorhexidine, benzalkonium chloride, and cetylpyridinium chloride. A-16686 appears to be a promising antiplaque agent because of the following attributes: narrow spectrum of activity, rapid bactericidal action, lack of selection of resistant mutants, absence of cross-resistance with clinically used antibiotics, nonabsorption by oral route, good tolerability by the oral mucosa (rats and dogs), and physical characteristics (white powder, soluble in water).

Pallanza, R; Scotti, R; Beretta, G; Cavalleri, B; Arioli, V

1984-01-01

91

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

92

Antileishmanial Structure-Activity Relationships of Synthetic Phospholipids: In Vitro and In Vivo Activities of Selected Derivatives? †  

PubMed Central

Antileishmanial activities of 91 synthetic phospholipids against Leishmania donovani were evaluated in vitro and cytotoxicity assessed against two mammalian cell lines. Promising compounds were tested further in vivo. In vitro structure-activity relationships showed a positive contribution of head groups bearing ring systems (N-methylpiperidino and N-methylmorpholino) to antileishmanial activity.

Seifert, Karin; Lemke, Andreas; Croft, Simon L.; Kayser, Oliver

2007-01-01

93

Substrate elasticity affects bovine satellite cell activation kinetics in vitro.  

PubMed

Satellite cells support efficient postnatal skeletal muscle hypertrophy through fusion into the adjacent muscle fiber. Nuclear contribution allows for maintenance of the fiber myonuclear domain and proficient transcription of myogenic genes. Niche growth factors affect satellite cell biology; however, the interplay between fiber elasticity and microenvironment proteins remains largely unknown. The objective of the experiment was to examine the effects of hepatocyte growth factor (HGF) and surface elasticity on bovine satellite cell (BSC) activation kinetics in vitro. Young's elastic modulus was calculated for the semimembranosus (SM) and LM muscles of young bulls (5 d; n = 8) and adult cows (27 mo; n = 4) cattle. Results indicate that LM elasticity decreased (P < 0.05) with age; no difference in Young's modulus for the SM was noted. Bovine satellite cells were seeded atop polyacrylamide bioscaffolds with surface elasticities that mimic young bull and adult cow LM or traditional cultureware. Cells were maintained in low-serum media supplemented with 5 ng/mL HGF or vehicle only for 24 or 48 h. Activation was evaluated by proliferating cell nuclear antigen (PCNA) immunocytochemistry. Results indicate that BSC maintained on rigid surfaces were activated at 24 h and refractive to HGF supplementation. By contrast, fewer (P < 0.05) BSC had exited quiescence after 24 h of culture on surfaces reflective of either young bull (8.1 ± 1.7 kPa) or adult cow (14.6 ± 1.6 kPa) LM. Supplementation with HGF promoted activation of BSC cultured on bioscaffolds as measured by an increase (P < 0.05) in PCNA immunopositive cells. Culture on pliant surfaces affected neither activation kinetics nor numbers of Paired box 7 (Pax7) immunopositive muscle stem cells (P > 0.05). However, with increasing surface elasticity, an increase (P < 0.05) in the numbers of muscle progenitors was observed. These results confirm that biophysical and biochemical signals regulate BSC activation. PMID:23463548

Lapin, M R; Gonzalez, J M; Johnson, S E

2013-05-01

94

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

95

Influence of gold nanoparticles on platelets functional activity in vitro  

NASA Astrophysics Data System (ADS)

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

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

2008-03-01

96

In vitro photogenotoxic activity of clinafloxacin: a paradigm predicting photocarcinogenicity.  

PubMed

Fluoroquinolone antiinfective drugs exhibit phototoxic, photogenotoxic, and photocarcinogenic activities in experimental systems which may be interrelated. Clinafloxacin (CLX), a new fluoroquinolone, is a potent antiinfective agent being developed for use in life-threatening infections. While this drug has previously been demonstrated to be phototoxic, this report evaluated the photogenotoxic and photocarcinogenic potential of CLX. When Skh-1 mice were administered CLX in the presence of ultraviolet light (UVA) at the maximum tolerated dose expected for a photocarcinogenicity bioassay, induction of DNA strand breakage was noted in keratinocytes isolated from these animals. When compared with other well-studied fluoroquinolones in vitro, CLX and Lomefloxacin (LMX) were equally effective in producing chromosome damage and DNA strand breakage in Chinese hamster ovary (CHO) cells exposed to UVA. Treatment of CHO cells with CLX in the presence of UVA also resulted in hydroxyl radical formation. However, coincubation of CHO cells with CLX and various antioxidants markedly reduced hydroxyl radical formation, but inhibited photogenotoxicity only to a limited extent. Thus, while reactive oxygen species contribute to the photogenotoxic activity of CLX, other factors may be involved. Since CLX exhibits both phototoxic and photogenotoxic activity, we predict that CLX would be photocarcinogenic in vivo. The present study suggests that under conditions of human exposure, the potential risk for CLX-induced photocarcinogenicity is small. PMID:10222314

Bulera, S J; Theiss, J C; Festerling, T A; de la Iglesia, F A

1999-05-01

97

Glucosamine Activates Autophagy In Vitro and In Vivo  

PubMed Central

Objectives Aging-associated changes in articular cartilage represent a main Osteoarthritis (OA) risk factor. Autophagy is an essential cellular homeostasis mechanism. Aging-associated or experimental defects in autophagy contribute to organismal and tissue specific aging while enhancement of autophagy may protect against certain aging related pathologies such as OA. The objective of this study was to determine whether glucosamine (GlcN) could activate autophagy. Methods Chondrocytes from normal human articular cartilage were treated with GlcN (0.1-10 mM). Autophagy activation and phosphorylation levels of Akt, FoxO3 and ribosomal protein S6 (prbS6) were determined by Western blotting. Autophagosome formation was analyzed by microscopy. Transgenic reporter mice with green fluorescent protein fused to LC3 (GFP-LC3 mice) were used to test changes in autophagy in response to starvation and GlcN administration. Results GlcN treatment of chondrocytes activated autophagy as indicated by increased of LC3-II levels, formation of LC3 puncta and increased LC3 turnover. This was associated with GlcN-mediated inhibition of Akt, FoxO3 and mTOR pathway. Administration of GlcN to GFP-LC3 mice markedly activated autophagy in articular cartilage. Conclusions GlcN modulates molecular targets of the autophagy pathway in vitro and in vivo and the enhancement of autophagy was mainly dependent on the Akt/FoxO and mTOR pathway. These findings suggest that GlcN is an effective autophagy activator and motivate future studies on its efficacy in modifying aging-related cellular changes and supporting joint health.

Carames, Beatriz; Kiosses, William B.; Akasaki, Yukio; Brinson, Diana C.; Eap, William; Koziol, James; Lotz, Martin K.

2013-01-01

98

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

PubMed Central

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

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

2011-01-01

99

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.

2012-01-01

100

In vitro antifungal activity of naftifine hydrochloride against dermatophytes.  

PubMed

The incidence of superficial dermatophytoses is high in developed countries, and there remains a need for effective topical antifungals. In this study, we evaluated the in vitro antifungal activity of naftifine hydrochloride, the active ingredient in naftifine hydrochloride cream and gel 1% and 2%, against dermatophytes. The MICs and minimum fungicidal concentrations (MFCs) of naftifine hydrochloride against 350 clinical strains, including Trichophyton rubrum, T. mentagrophytes, T. tonsurans, Epidermophyton floccosum, and Microsporum canis, were determined using the CLSI methodology. Subsets from this test panel were subsequently tested in a time-kill assay at 0.125×, 0.25×, 0.5×, and 1× the MFC for each isolate. CFU counts were performed over a period of 48 h of incubation. Additionally, in order to determine the potential for resistance development, six strains were subjected to 15 serial passages in concentrations higher than the MIC for each strain. MICs were determined following each passage. The MIC range against the dermatophyte isolates tested was 0.015 to 1.0 ?g/ml, with naftifine hydrochloride being fungicidal against 85% of the Trichophyton species. The time-kill assay showed dose-dependent activity, with the greatest reduction in the numbers of CFU corresponding to the highest drug concentration. There was no increase in MIC for any strains following repeated exposure to naftifine hydrochloride. Naftifine hydrochloride demonstrated potent activity against all dermatophytes tested, and none of the isolates within this test panel demonstrated the potential for the development of resistance. Thus, future clinical studies of naftifine hydrochloride against dermatophytes may be warranted for the treatment of superficial dermatophytoses. PMID:23817365

Ghannoum, M; Isham, N; Verma, A; Plaum, S; Fleischer, A; Hardas, B

2013-09-01

101

In vitro activity and human pharmacokinetics of teicoplanin.  

PubMed Central

The in vitro activity of teicoplanin, a new antibiotic related to vancomycin, was determined against 456 gram-positive cocci. The activity of teicoplanin in comparison with that of vancomycin was similar against staphylococci but 4 to 40 times higher against enterococci and beta-hemolytic and viridans streptococci. The single-dose pharmacokinetics of teicoplanin were studied in six healthy volunteers after administration of 3 and 6 mg/kg intravenously and of 3 mg/kg intramuscularly. The kinetic parameters after both intravenous doses were very similar. The curves for concentration in plasma for the 3- and 6-mg/kg intravenous doses showed a triexponential decline with elimination half-lives of 47.3 and 44.1 h, respectively. The percentages of the doses recovered in urine (0 to 102 h) were 43.2 and 44.1%, respectively. The areas under the plasma curves were dose related: 256.5 and 520.9 micrograms/h per ml, respectively. The bioavailability of teicoplanin after injection of 3 mg/kg intramuscularly was 90%, and the peak level was 7.1 micrograms/ml. The mean levels in plasma 24 h after the 3-mg/kg doses were 2.1 and 2.3 micrograms/ml, respectively, and the mean level in plasma 24 h after the 6-mg/kg intravenous dose was 4.2 micrograms/ml.

Verbist, L; Tjandramaga, B; Hendrickx, B; Van Hecken, A; Van Melle, P; Verbesselt, R; Verhaegen, J; De Schepper, P J

1984-01-01

102

In vivo and in vitro antimalarial activity of bergenin  

PubMed Central

Malaria is a potentially life-threatening protozoal parasitic disease transmitted by female Anopheles mosquitoes. Drug therapy is currently the most widely used method for the control and treatment of this disease. Several plants were found to contain substances possessing antimalarial properties. In this study, we investigated the antimalarial activity of bergenin, a sesquiterpene lactone compound derived from Rodgersia aesculifolia Batal. The results indicated that bergenin effectively inhibited Plasmodium falciparum growth in vitro (IC50, 14.1 ?g/ml, with ~100% inhibition at 50 ?g/ml), without apparent cytotoxicity to erythrocytes or to mammalian HeLa and HepG2 cells. Bergenin exhibited less cytotoxic activity and the selectivity index (SI) was 887 and 1,355 for HeLa and HepG2 cells, respectively. The administration of bergenin to Plasmodium berghei-infected mice for 6 days significantly inhibited the growth of the parasites. Taken together, these findings provide evidence that bergenin may be a promising novel drug for antimalarial treatment.

LIANG, JIAO; LI, YINGHUI; LIU, XUEWU; HUANG, YUXIAO; SHEN, YAN; WANG, JUN; LIU, ZHONGXIANG; ZHAO, YA

2014-01-01

103

Evaluation of antioxidant activity of isoferulic acid in vitro.  

PubMed

Isoferulic acid (3-hydroxy-4-methoxycinnamic acid, IFA), the isomer of ferulic acid (4-hydroxy-3-methoxycinnamic acid), is a rare phenolic acid occurring in Rhizoma Cimicifugae. Unlike ferulic acid, which has been well investigated, the antioxidant activity of IFA has not been measured. In this study, IFA was systematically evaluated for its in vitro antioxidant activity for the first time. IC50 values were calculated of 7.30 +/- 0.57, 4.58 +/- 0.17, 1.08 +/- 0.01, 8.84 +/- 0.43, 7.69 +/- 0.39, 1.57 +/- 0.2, 13.33 +/- 0.49 microg/mL, respectively, for lipid peroxidation, DPPH (1,1-diphenyl-2-picrylhydrazyl radical) and ABTS (3-ethylbenzthiazoline-6-sulfonic acid diammonium salt) radical scavenging, reducing power on Fe3+ and CU2+ ions, and hydroxyl and superoxide anion radical scavenging. Comparison with the IC50 values with those of the positive controls, Trolox and butylated hydroxyanisole (BHA), it can be concluded that isoferulic acid is an effective natural antioxidant in both lipid and aqueous media. PMID:21941899

Wang, Xiaozhen; Li, Xican; Chen, Dongfeng

2011-09-01

104

In vitro anti-Helicobacter pylori activity of usnic acid.  

PubMed

Eradication of Helicobacter pylori is an important objective in overcoming gastric diseases. Many regimens are currently available but none of them could achieve 100% success in eradication. Medicinal lichen is used in the treatment of gastric ulcer in local folk medicine in Anatolia (Turkey). The present study was performed to assess the in vitro effects of usnic acid from Usnea dasypoga against clinical isolates and standard H. pylori strains and their minimum inhibitory concentrations (MICs). A total of 38 strains was assayed for anti-H. pylori activity. The agar dilution method was used for the determination of usnic acid and clarithromycin resistance.Six (16.2%) clinical isolates were resistant to usnic acid and five (13.5%) were resistant to clarithromycin. Dual susceptibility to usnic acid and clarithromycin rate was detected as very high (97.3%). Usnic acid has a strong and dose-dependent activity against H. pylori strains. The synergism between usnic acid and clarithromycin may be effective in the treatment of H. pylori infection. PMID:19367654

Safak, Birol; Ciftci, Ihsan Hakki; Ozdemir, Mehmet; Kiyildi, Nilay; Cetinkaya, Zafer; Aktepe, Orhan Cem; Altindis, Mustafa; Asik, Gulsah

2009-07-01

105

Cell-free NADPH oxidase activation assays: "in vitro veritas".  

PubMed

The superoxide (O2 (?-))-generating NADPH oxidase complex of phagocytes comprises a membrane-imbedded heterodimeric flavocytochrome, known as cytochrome b 558 (consisting of Nox2 and p22 (phox) ) and four cytosolic regulatory proteins, p47 (phox) , p67 (phox) , p40 (phox) , and the small GTPase Rac. Under physiological conditions, in the resting phagocyte, O2 (?-) generation is initiated by engagement of membrane receptors by a variety of stimuli, followed by specific signal transduction sequences leading to the translocation of the cytosolic components to the membrane and their association with the cytochrome. A consequent conformational change in Nox2 initiates the electron "flow" along a redox gradient, from NADPH to oxygen, leading to the one-electron reduction of molecular oxygen to O2 (?-). Methodological difficulties in the dissection of this complex mechanism led to the design "cell-free" systems (also known as "broken cells" or in vitro systems). In these, membrane receptor stimulation and all or part of the signal transduction sequence are missing, the accent being placed on the actual process of "NADPH oxidase assembly," thus on the formation of the complex between cytochrome b 558 and the cytosolic components and the resulting O2 (?-) generation. Cell-free assays consist of a mixture of the individual components of the NADPH oxidase complex, derived from resting phagocytes or in the form of purified recombinant proteins, exposed in vitro to an activating agent (distinct from and unrelated to whole cell stimulants), in the presence of NADPH and oxygen. Activation is commonly quantified by measuring the primary product of the reaction, O2 (?-), trapped immediately after its generation by an appropriate acceptor in a kinetic assay, permitting the calculation of the linear rate of O2 (?-) production, but numerous variations exist, based on the assessment of reaction products or the consumption of substrates. Cell-free assays played a paramount role in the identification and characterization of the components of the NADPH oxidase complex, the deciphering of the mechanisms of assembly, the search for inhibitory drugs, and the diagnosis of various forms of chronic granulomatous disease (CGD). PMID:24504963

Pick, Edgar

2014-01-01

106

Nickel effects on DNA polymerase activity in vitro  

SciTech Connect

The effect of nickel ions (Ni{sup +2}) on DNA polymerase activity was studied in vitro using several different purified DNA polymerases and either primed single stranded or gapped duplex M13mp2 DNA as the template. The concentration of nickel giving 50% relative activity varied by several orders of magnitude for the different polymerases and for different templates. Under the conditions used, only E. coli Polymerase I-Klenow fragment (Pol I-KF) was able to effectively use Ni{sup +2} as the activation cation in place of Mg{sup +2}. Besides inhibiting nucleotide incorporation, nickel also inhibited primer extension by T7 and T4 polymerases. Nickel was significantly more inhibitory to Sequenase-2.0, an exo minus derivative of T7 polymerase, than to T7 polymerase itself. It also preferentially inhibited the 3{prime}-5{prime} exonuclease activity of T7 polymerase. This may indicate that Ni{sup +2} binds preferentially to the exonuclease active site of T7 polymerase. A rapid, minus dNTP, primer-extension assay for polymerase fidelity was also performed in the presence of Ni{sup +2}. In the absence of one of the 4 required dNTPs an accurate polymerase will pause at or before the first base that pairs with the missing dNTP. An inaccurate polymerase will misincorporate an incorrect base and bypass this and subsequent pause sites. Using this assay nickel did not cause misincorporation by AMV polymerase. However, the presence of increasing Ni{sup +2} (from 10 to 200 {mu}M) first increased and then decreased the fidelity of Pol I KF and exo minus KF and decreased the fidelity of Sequenase. The fidelity of T7 polymerase was not altered by Ni{sup +2}, despite an almost complete inhibition of the 3{prime}-5{prime} exonuclease activity by high Ni{sup +2} concentrations. These results indicate that nickel mutagenesis may vary significantly depending on the polymerase.

Snow, E.T.; Xu, L.S.; Kinney, P.L. [NYU Medical Center, Tuxedo, NY (United States)

1994-12-31

107

Antitumor activity of triptolide against cholangiocarcinoma growth in vitro and in hamsters  

Microsoft Academic Search

One of the diverse biological activities of triptolide, a diterpene from Tripterygium wilfordii, is its antitumor effect. We recently reported its in vitro cytotoxicity against several cultured tumor cell lines. Limited availability of purified fraction has prevented detailed investigation on its antitumor activity. In the present study, we showed by in vitro cytotoxicity assay and in vivo inhibition of tumor

Tasanee Tengchaisri; Runglawan Chawengkirttikul; Nattawan Rachaphaew; Vichai Reutrakul; Ranee Sangsuwan; Stitaya Sirisinha

1998-01-01

108

In-vitro activity of four new fluoroquinolones.  

PubMed

The in-vitro activities of four new fluoroquinolones, E-4749, E-4874, E-4884 and E-4904, were compared with that of ciprofloxacin and sparfloxacin against 1106 clinical isolates. Against majority of Enterobacteriaceae, general antibacterial activities of E-4749 (MIC90s 0.06-1 mg/L), E-4874 (MIC90s, 0.03-0.25 mg/L) and E-4884 (MIC90s 0.01-0.5 mg/L) were comparable or slightly lower than those of ciproloxacin (MIC90s 0.01-0.25 mg/L) and sparfloxacin (MIC90s 0.01-1 mg/L). The activity of E-4904 (MIC90s 0.06-2 mg/L) was lower than those of its analogues. Most of the Escherichia coli which were resistant to ciprofloxacin (MIC > or = 2 mg/L) and Serratia spp., were resistant to the new fluoroquinolones. beta-Lactamase producing strains of Moraxella catarrhalis were very susceptible to these compounds (MICs < or = 0.008 mg/L). Most of Pseudomonas aeruginosa, non-aeruginosa Pseudomonas spp., Xanthomonas maltophilia, and Acinetobacter spp. were resistant to the new quinolones (MIC90s 8- > 16 mg/L). On the contrary, these new antimicrobials were active against the majority of the Aeromonas spp. (MIC90s < or = 0.5 mg/L). E-4749, E-4874, E-4884 and E-4904 remained active (MIC90s < or = 0.25 mg/L) against Staphylococcus aureus strains susceptible to methicillin. However, its activity was two- to eight-fold lower than that of ciprofloxacin (MIC90 0.03 mg/L) and sparfloxacin (MIC90 0.06 mg/L). Against S. aureus resistant to methicillin or ciprofloxacin, activity of these new compounds and comparators agents, was very low (MIC90s 2- > 16 mg/L). Most of the strains of Enterococcus faecalis were resistant (MIC90s > 16 mg/L). The activity of E-4874, E-4904 and sparfloxacin (MIC90 1 mg/L for each one) was higher than that of the rest of the agents tested. E-4874 (MIC90 0.25 mg/L) was four-fold more active than the other antibacterials tested (MIC90 2 mg/L) against Listeria monocytogenes. No new quinolone was active against Bacteroides fragilis (MIC90s 4-16 mg/L), Bacteroides thetaiotaomicron (MIC90s 8- > 16 mg/L), and other B. fragilis group (MIC90s 16- > 16 mg/L). Ciprofloxacin (MIC90s > 16 mg/L), and sparfloxacin (MIC90s 8-16 mg/L) also were inactive. E-4874 (MIC90 4 mg/L) was the most active quinolone tested against B.fragilis. PMID:7961215

García-Rodríguez, J A; García Sánchez, J E; García García, M I; Fresnadillo, M J; Trujillano, I; García Sánchez, E

1994-07-01

109

Effect of 1-Desoxynojirimycin Derivatives on Small Intestinal Disaccharidase Activities and on Active Transport in vitro  

Microsoft Academic Search

The influence of two new 1-desoxynojirimycin derivatives, BAY m 1099 and BAY·1248, on rat small intestinal disaccharidases (sucrase, maltase, isomaltase, glucoamylase, lactase, trehalase) and alkaline phosphatase activity has been investigated in vitro. Both compounds are very potent ?-glucosidase inhibitors. Tested in the range of 0.1–5.0 ?g\\/ml, inhibition is strongest on sucrase (up to 97.1 %) and glucoamylase (up to 96.7%).

B. Lembcke; U. R. Fölsch; W. Creutzfeldt

1985-01-01

110

Mersacidin, a new antibiotic from Bacillus. In vitro and in vivo antibacterial activity.  

PubMed

Mersacidin is a new peptide antibiotic of the proposed lantibiotic family. It is active in vitro and in vivo against Gram-positive bacteria including the methicillin-resistant Staphylococci. Its in vitro activity is less than those of vancomycin and erythromycin but it shows much higher activity in the in vivo system than can be expected from the in vitro testing results. A water soluble potassium salt has been prepared which has an activity profile similar to that of mersacidin, but has better in vivo activity against Streptococcus pyogenes than the parent compound. PMID:1500348

Chatterjee, S; Chatterjee, D K; Jani, R H; Blumbach, J; Ganguli, B N; Klesel, N; Limbert, M; Seibert, G

1992-06-01

111

What is the clinical relevance of in vitro epileptiform activity?  

PubMed

In vitro preparations provide an exceptionally rapid, flexible, and accessible approach to long-standing problems in epilepsy research including ictogenesis, epileptogenesis, and drug resistance. Acute slices suffer from a reduction in network connectivity that has traditionally been compensated through the application of acute convulsants. The utility and limitations of this approach have become clear over time and are discussed here. Other approaches such as organotypic slice preparations demonstrate the full spectrum of spontaneous epileptic activity and more closely mimic human responses to anticonvulsants, including the development of drug resistance. Newly developed transgenic and vector expression systems for fluorophores, optogenetics, and orphan receptors are being coupled with advances in imaging and image analysis. These developments have created the capacity to rapidly explore many new avenues of epilepsy research such as vascular, astrocytic and mitochondrial contributions to epileptogenesis. Rigorous study design as well as close collaboration with in vivo laboratories and clinical investigators will accelerate the translation of the exciting discoveries that will be revealed by these new techniques. PMID:25012364

Heinemann, Uwe; Staley, Kevin J

2014-01-01

112

In vitro and in vitro activity of eugenol oil ( Eugenia caryophylata) against four important postharvest apple pathogens  

Microsoft Academic Search

The activity of eugenol oil was evaluated in vitro and in vivo against four apple pathogens namely Phlyctema vagabunda, Penicillium expansum, Botrytis cinerea and Monilinia fructigena. The minimum inhibitory concentration (MIC) of eugenol incorporated in malt extract agar medium was found to be 2 mg ml?1. Mycelial growth of the four test pathogens was completely inhibited when treated with 150 µl l?1

Achour Amiri; Robert Dugas; Anne L. Pichot; Gilbert Bompeix

2008-01-01

113

Activity of (+)-cyclaradine (Sch 31172) against herpes simplex virus in vitro and in vivo.  

PubMed Central

(+)-Cyclaradine (Sch 31172) is the carbocyclic derivative of adenosine arabinoside (9-beta-D-arabinofuranosyladenine). Because it is not deaminated by deaminase in serum, as is adenosine arabinoside, (+)-cyclaradine is about 2 to 5 times more active in vitro against herpes simplex virus. (+)-Cyclaradine has in vitro activity nearly equivalent to that of phosphonoformate but is significantly less active than acycloguanosine (acyclovir; ACV), trifluorothymidine, or 9-(1,3-dihydroxy-2-propoxymethyl)guanine. The absolute ratios of in vitro activities are difficult to determine because of variability among virus strains, inoculum size, and dependence on the tissue culture cell line in which the comparative test is carried out. (+)-Cyclaradine is active against TK-, ACV-resistant mutants. In the guinea pig model of vaginal herpes simplex virus infection, (+)-cyclaradine is only slightly less active than ACV when both molecules are nearly equivalently bioavailable; thus, the large difference in activity seen in vitro is not reflected in this in vivo model system.

Schwartz, J; Ostrander, M; Butkiewicz, N J; Lieberman, M; Lin, C; Lim, J; Miller, G H

1987-01-01

114

Risperidone and paliperidone inhibit p-glycoprotein activity in vitro.  

PubMed

Risperidone (RSP) and its major active metabolite, 9-hydroxy-risperidone (paliperidone, PALI), are substrates of the drug transporter P-glycoprotein (P-gp). The goal of this study was to examine the in vitro effects of RSP and PALI on P-gp-mediated transport. The intracellular accumulation of rhodamine123 (Rh123) and doxorubicin (DOX) were examined in LLC-PK1/MDR1 cells to evaluate P-gp inhibition by RSP and PALI. Both compounds significantly increased the intracellular accumulation of Rh123 and DOX in a concentration-dependent manner. The IC(50) values of RSP for inhibiting P-gp-mediated transport of Rh123 and DOX were 63.26 and 15.78 microM, respectively, whereas the IC(50) values of PALI were >100 microM, indicating that PALI is a less potent P-gp inhibitor. Caco-2 and primary cultured rat brain microvessel endothelial cells (RBMECs) were utilized to investigate the possible influence of RSP on intestinal absorption and blood-brain barrier (BBB) transport of coadministered drugs that are P-gp substrates. RSP, 1-50 microM, significantly enhanced the intracellular accumulation of Rh123 in Caco-2 cells by inhibiting P-gp activity with an IC(50) value of 5.87 microM. Following exposure to 10 microM RSP, the apparent permeability coefficient of Rh123 across Caco-2 and RBMECs monolayers was increased to 2.02 and 2.63-fold in the apical to basolateral direction, but decreased to 0.37 and 0.21-fold in the basolateral to apical direction, respectively. These data suggest that RSP and PALI, to a lesser extent, have a potential to influence the pharmacokinetics and hence the pharmacodynamics of coadministered drugs via inhibition of P-gp-mediated transport. However, no human data exist that address this issue. In particular, RSP may interact with its own active metabolite PALI by promoting its brain concentration through inhibiting P-gp-mediated efflux of PALI across endothelial cells of the BBB. PMID:16936711

Zhu, Hao-Jie; Wang, Jun-Sheng; Markowitz, John S; Donovan, Jennifer L; Gibson, Bryan B; DeVane, C Lindsay

2007-04-01

115

Antioxidant, antibacterial and antischistosomal activities of extracts from Grateloupia livida (Harv). Yamada.  

PubMed

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

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

2013-01-01

116

In Vitro Antimicrobial, Cytotoxic and Antioxidant Activity of Flower Extract of Saccharum Spontaneum Linn  

Microsoft Academic Search

The research work was conducted to investigate the in vitro antimicrobial, cytotoxic and antioxidant activity of chloroform extract of flower Saccharum spontaneum Linn. (Family- Gramineae). Disc diffusion technique was used for in vitro antibacterial and antifungal screening. Zones of inhibition were observed in disc diffusion for antimicrobial investigation against 4 Gram-positive and 8 Gram negative pathogenic bacteria. The extract showed

Farhana Alam Ripa; Mahmuda Haque

117

In Vitro Activity of R126638 and Ketoconazole Against Malassezia Species  

Microsoft Academic Search

The in vitro activity of a new triazole R126638 against Malassezia yeasts was compared with that of ketocona­ zole. With the agar dilution technique, minimal inhibi­ tory concentrations were lower for R126638 compared with ketoconazole against Malassezia globosa, M. obtusa, M. slooffiae , M. restricta and two strains of M. sympodia- lis. On human stratum corneum in vitro, both R126638

J Faergemann; J Ausma; M Borgers

2006-01-01

118

fl-l,3 GLUCAN ACTIVATION OF CRUSTACEAN HEMOCYTES IN VITRO AND IN VIVO  

Microsoft Academic Search

The effects of 13-1 ,3 glucans on the hemocytes of the freshwater crayfish, Astacus astacus, and the shore crab, Carcinus maenas, were studied in vitro and in vivo to determine the role ofthe prophenoloxidase activating system, in the cellular defense reactions of crustaceans. In vitro, phagocytosis of the bacterium, Moraxella sp. was significantly raised by addition of laminarin, a $-l

VALERIE J. SMITH; KENNETH SODERHALL

119

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

PubMed

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

Pappalardo, A; Thompson, K

2013-11-01

120

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

PubMed

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

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

2013-12-01

121

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

PubMed

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

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

2010-12-01

122

In vitro antimicrobial activity of Cryptolepis sanguinolenta (periplocaceae)  

Microsoft Academic Search

The aim of the present study was to investigate in vitro, the effect of three different preparations of Cryptolepis sanguinolenta, obtained from 2 mg\\/ml each of 70% ethanol, hot and cold aqueous extract, as antimicrobial agents using agar diffusion method. The microbes used in this study consisted of one strain of Salmonella typhimurium, two strains each of Proteus mirabilis, Pseudomonas

Felix C. Mills-Robertson; Frederick A. Aboagye; George Duker-Eshun; Sylvester Kaminta; Samuel Agbeve

123

AMP-activated protein kinase (AMPK) activation regulates in vitro bone formation and bone mass  

PubMed Central

Adenosine 5?-monophosphate-activated protein kinase (AMPK), a regulator of energy homeostasis, has a central role in mediating the appetite-modulating and metabolic effects of many hormones and antidiabetic drugs metformin and glitazones. The objective of this study was to determine if AMPK can be activated in osteoblasts by known AMPK modulators and if AMPK activity is involved in osteoblast function in vitro and regulation of bone mass in vivo. ROS 17/2.8 rat osteoblast-like cells were cultured in the presence of AMPK activators (AICAR and metformin), AMPK inhibitor (compound C), the gastric peptide hormone ghrelin and the beta-adrenergic blocker propranolol. AMPK activity was measured in cell lysates by a functional kinase assay and AMPK protein phosphorylation was studied by Western Blotting using an antibody recognizing AMPK Thr-172 residue. We demonstrated that treatment of ROS 17/2.8 cells with AICAR and metformin stimulates Thr-172 phosphorylation of AMPK and dose-dependently increases its activity. In contrast, treatment of ROS 17/2.8 cells with compound C inhibited AMPK phosphorylation. Ghrelin and propranolol dose-dependently increased AMPK phosphorylation and activity. Cell proliferation and alkaline phosphatase activity were not affected by metformin treatment while AICAR significantly inhibited ROS 17/2.8 cell proliferation and alkaline phosphatase activity at high concentrations. To study the effect of AMPK activation on bone formation in vitro, primary osteoblasts obtained from rat calvaria were cultured for 14-17 days in the presence of AICAR, metformin and compound C. Formation of ‘trabecular-shaped’ bone nodules was evaluated following alizarin red staining. We demonstrated that both AICAR and metformin dose-dependently increase trabecular bone nodule formation, while compound C inhibits bone formation. When primary osteoblasts were co-treated with AICAR and compound C, compound C suppressed the stimulatory effect of AICAR on bone nodule formation. AMPK is a ??? heterotrimer, where ? is the catalytic subunit. RT-PCR analysis of AMPK subunits in ROS17/2.8 osteoblastic cells and in mouse tibia showed that the AMPK?1 subunit is the dominant isoform expressed in bone. We analysed the bone phenotype of 4 month-old male wild type (WT) and AMPK?1?/? KO mice using micro-CT. Both cortical and trabecular bone compartments were smaller in the AMPK ?1-deficient mice compared to the WT mice. Altogether, our data support a role for AMPK signalling in skeletal physiology.

Shah, M.; Kola, B.; Bataveljic, A.; Arnett, T.R.; Viollet, B.; Saxon, L.; Korbonits, M.; Chenu, C.

2013-01-01

124

Antifungal Activity of Tamoxifen: In Vitro and In Vivo Activities and Mechanistic Characterization? †  

PubMed Central

Tamoxifen (TAM), an estrogen receptor antagonist used primarily to treat breast cancer, has well-recognized antifungal properties, but the activity of TAM has not been fully characterized using standardized (i.e., CLSI) in vitro susceptibility testing, nor has it been demonstrated in an in vivo model of fungal infection. In addition, its mechanism of action remains to be clearly defined at the molecular level. Here, we report that TAM displays in vitro activity (MIC, 8 to 64 ?g/ml) against pathogenic yeasts (Candida albicans, other Candida spp., and Cryptococcus neoformans). In vivo, 200 mg/kg of body weight per day TAM reduced kidney fungal burden (?1.5 log10 CFU per g tissue; P = 0.008) in a murine model of disseminated candidiasis. TAM is a known inhibitor of mammalian calmodulin, and TAM-treated yeast show phenotypes consistent with decreased calmodulin function, including lysis, decreased new bud formation, disrupted actin polarization, and decreased germ tube formation. The overexpression of calmodulin suppresses TAM toxicity, hypofunctional calmodulin mutants are hypersensitive to TAM, and TAM interferes with the interaction between Myo2p and calmodulin, suggesting that TAM targets calmodulin as part of its mechanism of action. Taken together, these experiments indicate that the further study of compounds related to TAM as antifungal agents is warranted.

Dolan, Kristy; Montgomery, Sara; Buchheit, Bradley; DiDone, Louis; Wellington, Melanie; Krysan, Damian J.

2009-01-01

125

Meropenem: in-vitro activity and kinetics of activity against organisms of the Bacteroides fragilis group.  

PubMed

Meropenem was compared with imipenem and nine other antimicrobial agents, against 101 strains of the Bacteroides fragilis group. Meropenem was active against all strains tested, and its activity was similar to, and in many cases better than, that of imipenem. The activity of meropenem was similar to that of metronidazole, and greater than that of the other antimicrobial agents tested. The bactericidal activity of meropenem against B. fragilis was impressive, since the MBC to MIC ratios were no greater than two. The bactericidal activity was confirmed by time-killing curve assays with two strains which showed that meropenem was rapidly bactericidal and reduced the initial inoculum significantly during the first 4-6 h. The postantibiotic effect of meropenem (2-4 h) and a sub-inhibitory concentration of 1/4 x MIC suggested that meropenem interferes with the normal growth of B. fragilis, even when administered concentrations fall below the MIC. MICs of meropenem were affected minimally by the pH of the medium or by an increase in inoculum size. Meropenem continued to have good activity against a B. fragilis strain that had been induced for the production of cephalosporinase. The in-vitro data presented in this paper indicate that meropenem is a promising antimicrobial agent which may be useful in the treatment of problematic mixed infections. PMID:1885418

García-Rodriguez, J A; García Sánchez, J E; Trujillano, I; Sánchez de San Lorenzo, A

1991-05-01

126

In vitro accelerated mass propagation and ex vitro evaluation of Aloe vera L. with aloin content and superoxide dismutase activity.  

PubMed

An innovative protocol on accelerated in vitro propagation and acclimatisation was developed in Aloe vera L. Culture was initiated with rhizomatous stem where Murashige and Skoog (MS) medium fortified with 0.5?mg?L(-1) ?-naphthalene acetic acid and 1.5?mg?L(-1) N(6)-benzylaminopurine (BAP) promoted earliest shoot induction. Maximum shoot multiplication was achieved in MS medium supplemented with 2.5?mg?L(-1)BAP. The best in vitro rooting was observed in the MS medium with 0.5?mg?L(-1) indole-3-acetic acid plus 2?g?L(-1) activated charcoal. The simple acclimatisation process, primarily with a combination of sand and soil (1?:?1 v/v) and finally with a blend of sand, soil and farm yard manure (2?:?1?:?1 v/v), ensured a 98% survival rate. Overall, 192 true-to-type plantlets were achieved from a single explant within 85 days. Morphologically, in vitro generated plants performed better than conventionally propagated plants; nevertheless the similarity in aloin content, gel content and superoxide dismutase activity was corroborated. PMID:21859262

Gantait, Saikat; Mandal, Nirmal; Das, Prakash Kanti

2011-08-01

127

In vitro studies on antiradical and antioxidant activities of fenugreek ( Trigonella foenum graecum) seeds  

Microsoft Academic Search

An extract of fenugreek (Trigonella foenum graecum) seeds was isolated and evaluated for antioxidant activity using various in vitro assay systems. The seed extract exhibited scavenging of hydroxyl radicals (OH) and inhibition of hydrogen peroxide-induced lipid peroxidation in rat liver mitochondria. The OH scavenging activity of the extract was evaluated by pulse radiolysis and the deoxyribose system. The antimutagenic activity

S. Kaviarasan; G. H. Naik; R. Gangabhagirathi; C. V. Anuradha; K. I. Priyadarsini

2007-01-01

128

In vitro Activity of Sparfloxacin Compared with Ciprofloxacin and Ofloxacin against Respiratory Tract Pathogens  

Microsoft Academic Search

The in vitro activity of sparfloxacin, a new fluoroquinolone, was compared with ciprofloxacin and ofloxacin against 166 consecutive isolates from the upper respiratory tract of outpatients. The strains were fully susceptible to three quinolones. The antibacterial activity of sparfloxacin was comparable or better than that of ofloxacin and ciprofloxacin against all strains. Sparfloxacin was fourfold more active against Staphylococcus aureus

A.-S. Malmborg; S. Ahlén

1993-01-01

129

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.

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

2011-01-01

130

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

Microsoft Academic Search

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

ANA ESPINEL-INGROFF

2001-01-01

131

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.

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

2000-01-01

132

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.

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

1992-01-01

133

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

134

In vitro cultures of Bituminaria bituminosa: pterocarpan, furanocoumarin and isoflavone production and cytotoxic activity evaluation.  

PubMed

Bituminaria bituminosa L. is known for producing several compounds with considerable pharmaceutical interest, such as phenylpropanoids, furanocoumarins and pterocarpans. In vitro cultures of seedlings, shoots, and callus have been produced to obtain plant materials useful for the production of these metabolites. The secondary metabolite profile was evaluated by HPLC-DAD. The extracts of all the in vitro material contained the flavonoid daidzein, while plicatin B, erybraedin C and bitucarpin A were found only in the extracts of the in vitro shoots and in wild shoots. The furanocoumarins angelicin and psoralen were found in in vivo and in vitro plants, but in the callus were not detectable. The extracts were also tested for cytotoxic activity in HeLa cell culture; the highest level of cytotoxicity was found in in vitro shoot extracts. PMID:24868860

D'Angiolillo, Francesca; Pistellia, Laura; Noccioli, Cecilia; Ruffoni, Barbara; Piaggi, Simona; Scarpato, Roberto; Pistelli, Luisa

2014-04-01

135

Platelet Microparticles Bind, Activate and Aggregate Neutrophils In Vitro  

Microsoft Academic Search

The interaction of activated platelets with leukocytes are believed to play an important role in ischemic reperfusion injury and other thrombotic conditions. Upon activation, platelets shed platelet microparticles (PMP) and express activation markers. CD62P expressed on activated platelets mediates adhesion of platelets to leukocytes, chiefly neutrophils, but little is known of the interaction of PMP with neutrophils. We investigated this

Wenche Jy; Wei-Wei Mao; Lawrence L. Horstman; Jianguo Tao; Yeon S. Ahn

1995-01-01

136

Synthesis and biological evaluation of 1,4-naphthoquinones and quinoline-5,8-diones as antimalarial and schistosomicidal agents.  

PubMed

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

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

2012-08-21

137

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

PubMed Central

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

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

2012-01-01

138

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

139

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

140

miRNA studies in in vitro and in vivo activated hepatic stellate cells  

PubMed Central

AIM: To understand which and how different miRNAs are implicated in the process of hepatic stellate cell (HSC) activation. METHODS: We used microarrays to examine the differential expression of miRNAs during in vitro activation of primary HSCs (pHSCs). The transcriptome changes upon stable transfection of rno-miR-146a into an HSC cell line were studied using cDNA microarrays. Selected differentially regulated miRNAs were investigated by quantitative real-time polymerase chain reaction during in vivo HSC activation. The effect of miRNA mimics and inhibitor on the in vitro activation of pHSCs was also evaluated. RESULTS: We found that 16 miRNAs were upregulated and 26 were downregulated significantly in 10-d in vitro activated pHSCs in comparison to quiescent pHSCs. Overexpression of rno-miR-146a was characterized by marked upregulation of tissue inhibitor of metalloproteinase-3, which is implicated in the regulation of tumor necrosis factor-? activity. Differences in the regulation of selected miRNAs were observed comparing in vitro and in vivo HSC activation. Treatment with miR-26a and 29a mimics, and miR-214 inhibitor during in vitro activation of pHSCs induced significant downregulation of collagen type?I?transcription. CONCLUSION: Our results emphasize the different regulation of miRNAs in in vitro and in vivo activated pHSCs. We also showed that miR-26a, 29a and 214 are involved in the regulation of collagen type I mRNA.

Maubach, Gunter; Lim, Michelle Chin Chia; Chen, Jinmiao; Yang, Henry; Zhuo, Lang

2011-01-01

141

Antioxidant and antibacterial activities of lichen Usnea ghattensis in vitro.  

PubMed

Various solvent extracts of the lichen Usnea ghattensis showed good antioxidant activity. A methanol extract prevented lipid peroxidation by 87% followed by 65% in Trolox at 20 microg/ml. It also showed superoxide anion scavenging activity and free radical scavenging activity 56% and 73%, respectively. The known antioxidants butylated hydroxytoluene (BHT), butylated hydroxyanisol (BHA) and quercetin at similar concentrations showed superoxide anion scavenging activity of 68, 59 and 47% and free radical scavenging activity 83, 77 and 69%, respectively. In addition, these extracts were inhibitory against Bacillus licheniformis, Bacillus megaterium, Bacillus subtilis and Staphylococcus aureus with MIC values of 5-10 microg/ml. PMID:16132842

Behera, B C; Verma, Neeraj; Sonone, Anjali; Makhija, Urmila

2005-07-01

142

In vitro activity of RU 29246, the active compound of the cephalosporin prodrug ester HR 916.  

PubMed

The in vitro activity of RU 29246 was compared with those of other agents against 536 recent clinical isolates. The MICs of RU 29246 for 90% of members of the family Enterobacteriaceae tested (MIC90s) were less than 2 micrograms/ml except those for Morganella spp. (16 micrograms/ml) and Proteus spp. (8 micrograms/ml). RU 29246 was active against Staphylococcus aureus (MIC90, < or = 8 micrograms/ml) and against Staphylococcus saprophyticus and coagulase-negative staphylococci (MIC90s, < or = 2 micrograms/ml). Streptococci and Neisseria gonorrhoeae were highly susceptible to RU 29246, and the activity of the agent against isolates of Streptococcus pneumoniae (MIC90, < or = 0.5 micrograms/ml), Haemophilus influenzae (MIC90, < or = 2 micrograms/ml), and Moraxella catarrhalis (MIC90, < or = 2 micrograms/ml) was comparable to those of the other cephalosporins tested. RU 29246 was insusceptible to hydrolysis by the common plasmid-mediated beta-lactamases (TEM-1 and SHV-1). However, hydrolysis by the new extended-spectrum beta-lactamases (TEM-3, TEM-5, and TEM-9) was detected. Results of the study suggested that RU 29246 should be investigated clinically for use in the treatment of a wide range of infections. PMID:1489178

Riess, G; Andrews, J; Thornber, D; Wise, R

1992-11-01

143

Oleamide activates peroxisome proliferator-activated receptor gamma (PPAR?) in vitro  

PubMed Central

Background Oleamide (ODA) is a fatty acid primary amide first identified in the cerebrospinal fluid of sleep-deprived cats, which exerts effects on vascular and neuronal tissues, with a variety of molecular targets including cannabinoid receptors and gap junctions. It has recently been reported to exert a hypolipidemic effect in hamsters. Here, we have investigated the nuclear receptor family of peroxisome proliferator-activated receptors (PPARs) as potential targets for ODA action. Results Activation of PPAR?, PPAR? and PPAR? was assessed using recombinant expression in Chinese hamster ovary cells with a luciferase reporter gene assay. Direct binding of ODA to the ligand binding domain of each of the three PPARs was monitored in a cell-free fluorescent ligand competition assay. A well-established assay of PPAR? activity, the differentiation of 3T3-L1 murine fibroblasts into adipocytes, was assessed using an Oil Red O uptake-based assay. ODA, at 10 and 50??M, was able to transactivate PPAR?, PPAR? and PPAR? receptors. ODA bound to the ligand binding domain of all three PPARs, although complete displacement of fluorescent ligand was only evident for PPAR?, at which an IC50 value of 38??M was estimated. In 3T3-L1 cells, ODA, at 10 and 20??M, induced adipogenesis. Conclusions We have, therefore, identified a novel site of action of ODA through PPAR nuclear receptors and shown how ODA should be considered as a weak PPAR? ligand in vitro.

2012-01-01

144

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

PubMed

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

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

2012-01-01

145

Synthesis and in vitro antitumor activity of new butenolide-containing dithiocarbamates.  

PubMed

Three series of butenolide-containing dithiocarbamates were designed and synthesized. Their anti-tumor activity in vitro was evaluated. Among them compound I-14 exhibited broad spectrum anti-cancer activity against five human cancer cell lines with IC(50) <30 ?M. Structure-activity relationship analysis showed that the introduction of dithiocarbamate side chains on the C-3 position of butenolide was crucial for anti-tumor activity. PMID:21486694

Wang, Xiao-Juan; Xu, Hai-Wei; Guo, Lin-Lin; Zheng, Jia-Xin; Xu, Bo; Guo, Xiao; Zheng, Chen-Xin; Liu, Hong-Min

2011-05-15

146

Antithrombotic activities of oroxylin A in vitro and in vivo.  

PubMed

Here, the anticoagulant activities of oroxylin A (OroA), a major component of Scutellaria baicalensis Georgi, were examined by monitoring activated partial thromboplastin time (aPTT), prothrombin time (PT), and the activities of cell-based thrombin and activated factor X (FXa). Furthermore, the effects of OroA on the expressions of plasminogen activator inhibitor type 1 (PAI-1) and tissue-type plasminogen activator (t-PA) were tested in tumor necrosis factor (TNF)-? activated human umbilical vein endothelial cells (HUVECs). Treatment with OroA resulted in prolonged aPTT and PT and inhibition of the activities of thrombin and FXa, and OroA inhibited production of thrombin and FXa in HUVECs. And OroA inhibited thrombin-catalyzed fibrin polymerization and platelet aggregation. In accordance with these anticoagulant activities, OroA elicited anticoagulant effects in mouse. In addition, treatment of OroA resulted in the inhibition of TNF-?-induced production of PAI-1, and treatment with OroA resulted in the significant reduction of the PAI-1 to t-PA ratio. Collectively, OroA possess antithrombotic activities and offer bases for development of a novel anticoagulant. PMID:23963976

Ku, Sae-Kwang; Lee, In-Chul; Bae, Jong-Sup

2014-05-01

147

In vitro activities of furoquinoline and acridone alkaloids against Plasmodium falciparum.  

PubMed Central

The in vitro activities of furo[2,3b]quinoline and acridone alkaloids against Plasmodium falciparum were evaluated by an isotopic semimicrotest. A pyran ring in the furoquinoline nucleus and 2-O-pyranoglycoside and 2-nitro substituents in the acridone nucleus improved the antimalarial activities of the compounds. These findings provide a clue for further chemical modifications.

Basco, L K; Mitaku, S; Skaltsounis, A L; Ravelomanantsoa, N; Tillequin, F; Koch, M; Le Bras, J

1994-01-01

148

In vitro antiprotozoal activities and cytotoxicity of some selected Cameroonian medicinal plants  

Microsoft Academic Search

Eight extracts from seven selected Cameroonian medicinal plants, traditionally used to treat malaria and other protozoal diseases, were tested in vitro for their antiprotozoal activities against Plasmodium falciparum K1 chloroquine-resistant strain, Leishmania donovani, Trypanosoma cruzi and Trypanosoma brucei rhodesiense, protozoa responsible for malaria, visceral leishmaniasis, Chagas disease and African trypanosomiasis, respectively. The most active extract against Plasmodium falciparum K1 strain

B. Ndjakou Lenta; C. Vonthron-Sénécheau; R. Fongang Soh; F. Tantangmo; S. Ngouela; M. Kaiser; E. Tsamo; R. Anton; B. Weniger

2007-01-01

149

IN VITRO ANTIMICROBIAL ACTIVITY OF OCIMUM AMERICANUM L. ESSENTIAL OIL AGAINST ORAL MICROORGANISMS  

Microsoft Academic Search

The aim of the present study was to evaluate the efficacy of the essential oil of Ocimum americanum L. on in vitro activity against Streptococcus mutans, Lactobacillus casei and Candida albicans. An agar disk diffusion method was employed for screening antimicrobial activity. Minimum inhibitory concentration (MIC) and minimum cidal concentration (MCC) values of the oil against planktonic cells were determined

Sroisiri Thaweboon; Boonyanit Thaweboon

2009-01-01

150

[In vitro bacteriocidal activity of 5 oral antiseptics against the principal microorganisms implicated in oral disease].  

PubMed

Bactericidal activities of five mouthrinses containing cetylpyridinium chloride, hexetidine or chlorhexidine have been tested in vitro, against the main microorganisms involved in buccal affections. Mouthrinses containing hexetidine or chlorhexidine are effective, but chlorhexidine activity appears more extensive and homogeneous. PMID:1811047

Luc, J; Roques, C; Frayret, M N; Michel, G; Ducani, M; Vandermander, J

1991-11-01

151

Flavonoids and lignans from Virola surinamensis twigs and their in vitro activity against Trypanosoma cruzi.  

PubMed

Dichloromethane extracts from twigs of Virola surinamensis (Myristicaceae) showed in vitro trypanosomicidal activity against trypomastigote form of Trypanosoma cruzi. The extract, fractionated by preparative circular chromatography and preparative high-performance liquid chromatography yielded two steroids, two lignans, five flavonoids, and one polyketide. Among the isolated compounds, the lignans presented the highest trypanosomicidal activity. PMID:9810278

Lopes, N P; Chicaro, P; Kato, M J; Albuquerque, S; Yoshida, M

1998-10-01

152

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

153

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

154

In vitro Augmentation of Natural Killer Cell Activity by Manganese Chloride.  

National Technical Information Service (NTIS)

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 Mn...

R. J. Smialowicz R. R. Rogers M. M. Riddle D. G. Rowe R. W. Luebke

1986-01-01

155

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...

156

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

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

2011-01-01

157

Liposomal incorporation of Artemisia arborescens L. essential oil and in vitro antiviral activity  

Microsoft Academic Search

The effect of liposomal inclusion on the in vitro antiherpetic activity of Artemisia arborescens L. essential oil was investigated. In order to study the influence of vesicle structure and composition on the antiviral activity of the vesicle-incorporated oil, multilamellar (MLV) and unilamellar (SUV) positively charged liposomes were prepared by the film method and sonication. Liposomes were obtained from hydrogenated (P90H)

Chiara Sinico; Alessandro De Logu; Francesco Lai; Donatella Valenti; Maria Manconi; Giuseppe Loy; Leonardo Bonsignore; Anna Maria Fadda

2005-01-01

158

In vitro Antifungal Activity of Thai Herb and Spice Extracts against Food Spoilage Fungi  

Microsoft Academic Search

The screening of Thai herbs and spices was carried out to investigate their in vitro antifungal activity against Aspergillus niger, A. oryzaeand Penicilliumsp. by using agar well diffusion method. Of thirteen plants tested, crude ethanol extracts of three, namely Piper betel, Boesenbergia pandurata, Andrographis paniculata exhibited antifungal activity against all test microorganisms. Penicillium sp. was more resistant to the extracts

Penkhae Wanchaitanawong; Piyamat Chaungwanit; Ngamtip Poovarodom; Sunee Nitisinprasert

159

Effect of pulmonary surfactant on antimicrobial activity in vitro.  

PubMed

Time-kill curve experiments were performed with linezolid, doripenem, tigecycline, moxifloxacin, and daptomycin against Staphylococcus aureus and with colistin, moxifloxacin, and doripenem against Pseudomonas aeruginosa to evaluate the effect of porcine pulmonary surfactant on antimicrobial activity. Pulmonary surfactant significantly impaired the activities of moxifloxacin and colistin. When antibiotics are being developed for respiratory tract infections, the method described here might be used to preliminarily quantify the effect of pulmonary surfactant on antimicrobial activity. PMID:23877678

Schwameis, R; Erdogan-Yildirim, Z; Manafi, M; Zeitlinger, M A; Strommer, S; Sauermann, R

2013-10-01

160

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

161

In vitro and in vivo cutaneous penetration and antifungal activity of naftifine.  

PubMed

The topical antifungal agent naftifine has shown considerable potency against a broad spectrum of dermatophytes. In this study, an in vitro penetration test in human cadaver skin and an in vivo tape-stripping test were used to evaluate the penetration and antifungal activity of naftifine gel 1 percent and naftifine cream 1 percent compared with other antifungal agents. In both models, Trichophyton rubrum and T. mentagrophytes were the fungal species. Results show that naftifine gel 1 percent and naftifine cream 1 percent, in vitro and in vivo, penetrate the stratum corneum in concentrations that inhibit the growth of both fungal species. Following penetration in vitro, naftifine gel and cream were significantly more active against T. rubrum than econazole nitrate cream 1 percent. Following penetration in vivo, naftifine gel and cream were as active as econazole nitrate cream 1 percent and clotrimazole cream 1 percent against T. rubrum and T. mentagrophytes. PMID:2805810

Stoughton, R B; Sefton, J; Zeleznick, L

1989-10-01

162

Activity of flumequine against Escherichia coli: in vitro comparison with nalidixic and oxolinic acids.  

PubMed Central

The in vitro activity of the new antibacterial agent, flumequine, against Escherichia coli was compared with those of oxolinic acid and nalidixic acid. As judged by turbidimetric criteria, flumequine was considerably more active than nalidixic acid and slightly less active than oxolinic acid against both nalidixic acid-susceptible and -resistant strains. Resistance to all three drugs could be easily induced in vitro. The comparative efficacy of flumequine, oxolinic acid, and nalidixic acid was also tested in an in vitro model of the treatment of bacterial cystitis. In this system, suppression of bacterial growth was obtained with markedly lower concentrations of flumequine and oxolinic acid than of nalidixic acid, but prevention of the emergence of bacterial populations that exhibited increased resistance to these compounds depended on the maintenance of adequate drug levels.

Greenwood, D

1978-01-01

163

Antioxidant and antiinflammatory activity of pine pollen extract in vitro.  

PubMed

To determine the medicinal properties of pine pollen, the antioxidant and antiinflammatory activities of the ethanol extract of pine pollen extract (PPE) were investigated. PPE displayed a strong free radical scavenger activity on 1,1-diphenyl-2-picrylhydrazyl radical and hydrogen peroxide. It was observed also that the antioxidant activity, measured by the ferric thiocyanate method, increased with the addition of PPE to the linoleic acid emulsion system. PPE was also found to inhibit significantly the amount of malondialdehyde and protein carbonyls formed from liver homogenate. Like the antioxidant activity, the reducing power of PPE was excellent. Thereafter, the study investigated the effects of PPE in modulating the production of pro-inflammatory mediators in lipopolysaccharide (LPS)-activated RAW 264.7 macrophages, and the effect of PPE on interleukin (IL)-1beta-induced matrix metalloproteinases (MMPs) production and mitogen-activated protein kinases (MAPKs) activation in the human synovial sarcoma cell line, SW982. PPE was found to inhibit the production of nitric oxide, tumor necrosis factor-alpha, IL-1 and IL-6 in LPS-activated macrophages. Treatment with PPE at 10 microg/mL significantly (p < 0.05) inhibited IL-1beta-induced MMPs (MMP-1 and -3) production in SW982 cells. IL-1beta-induced JNK activation was inhibited by PPE (10 microg/mL), whereas p38 and ERK1/2 were not affected. These findings suggest that pine pollen is a potential antioxidant and beneficial for inflammatory conditions through down-regulation of JNK and MMPs. PMID:19107823

Lee, Kyung-Hee; Kim, Ae-Jung; Choi, Eun-Mi

2009-01-01

164

Photosensitizing activity of thiocolchicoside: photochemical and in vitro phototoxicity studies.  

PubMed

The phototoxic drug thiocolchicoside (2-dimethoxy-2-glucosidoxythiocolchicine, 1), is photolabile under irradiation with UV-A light from TL 100 W-P Philips bulbs (at lambda max 355 nm) light and also with a N2 laser (at 337 nm) in aerobic and anaerobic conditions. Irradiation of a methanol solution of 1 produces two photoproducts without a glucoside group. One of these lost the methylthio-group, while the other is oxidized (only under aerobic conditions) to sulfoxide. The formation of singlet oxygen by photolysis of 1 was evidenced by trapping with 2,5-dimethylfuran (GC-MS), furfuryl alcohol, 1,3-cyclohexadiene-1,4-diethanoate (HPLC) and by the histidine test as 1O2 scavengers. Thiocolchicoside has been shown to photosensitize the reduction of nitro blue tetrazolium by direct electron transfer mechanism, when irradiated under the same conditions as for photolysis. Oxygen may also be involved in this electron transfer reaction to form the superoxide anion radical. Thiocolchicoside was screened in vitro in different concentrations for UV-Vis-induced phototoxic effects in a photohemolysis test, in the presence and absence of different radical scavengers, singlet oxygen and superoxide radical quenchers. In addition, 1 photosensitized the peroxidation of linoleic acid, monitored by the UV-detection of dienic hydroperoxides. Studies on peripheral blood mononuclear cells (lymphocytes) demonstrated phototoxic effects on them. Protection by GSH, DABCO, sodium azide and SOD are indicative of both Type I and II photosensitization pathways mediated by free radicals and singlet molecular oxygen. PMID:11210677

Vargas, F; Méndez, H; Fuentes, A; Sequera, J; Fraile, G; Velásquez, M; Cáceres, G; Cuello, K

2001-01-01

165

Activated T Lymphocytes Support Osteoclast Formation in Vitro  

Microsoft Academic Search

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

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

1999-01-01

166

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.

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

2014-01-01

167

Botulinum toxin suppression of CNS network activity in vitro.  

PubMed

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

168

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

169

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

PubMed

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

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

2013-01-01

170

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.

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

171

In vitro antimicrobial activity against reference strains and field isolates of Treponema hyodysenteriae.  

PubMed

The in vitro susceptibilities of eight isolates of Treponema hyodysenteriae from pigs naturally infected with swine dysentery between 1976 and 1983 were determined by an agar dilution technique. Carbadox, olaquindox, tiamulin, metronidazole, furazolidone, and monensin were the most active against these field isolates regardless of the year of recovery. The influence of inoculum size on the MICs against four reference strains of T. hyodysenteriae was studied. Various degrees of activities of ampicillin and lincomycin were found, depending on the inoculum size. The effect of successive in vitro subcultures on the susceptibility of a reference strain of T. hyodysenteriae was examined. The strain resistant to tylosin became susceptible to the drug. PMID:3439804

Kitai, K; Kashiwazaki, M; Adachi, Y; Kunugita, K; Arakawa, A

1987-12-01

172

In vitro activity of cefoxitin and imipenem against Mycobacterium abscessus complex.  

PubMed

The in vitro activity of cefoxitin and imipenem was compared for 43 strains of the Mycobacterium abscessus complex, mostly isolated from cystic fibrosis patients. The MICs of imipenem were lower than those of cefoxitin, although the number of imipenem-resistant strains was higher according to the CLSI breakpoints. Strain comparisons indicated that the MICs of cefoxitin were significantly higher for Mycobacterium bolletii than for M. abscessus. The MICs of both ?-lactams were higher for the rough morphotype than for the smooth morphotype. The clinical impact of the in vitro difference between the activity of imipenem and that of cefoxitin remains to be determined. PMID:24112243

Lavollay, M; Dubée, V; Heym, B; Herrmann, J-L; Gaillard, J-L; Gutmann, L; Arthur, M; Mainardi, J-L

2014-05-01

173

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

PubMed Central

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

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

2010-01-01

174

In vitro anti-HMPV activity of meroditerpenoids from marine alga Stypopodium zonale (Dictyotales).  

PubMed

In this paper, we evaluated the antiviral activity against HMPV replication of crude extract of the marine algae Stypopodium zonale and of two meroditerpenoids obtained from it, atomaric acid and epitaondiol, and a methyl ester derivative of atomaric acid. Their selectivity indexes were 20.78, >56.81, 49.26 and 12.82, respectively. Compared to ribavirin, the substances showed a relatively low cytotoxicity on LLC-MK2 cells, with a significant antiviral activity, inhibiting at least 90% of viral replication in vitro, which demonstrates the potential of these marine natural products to combat infections caused by HMPV in vitro. PMID:21986522

Mendes, Gabriella; Soares, Angélica Ribeiro; Sigiliano, Lorena; Machado, Fernanda; Kaiser, Carlos; Romeiro, Nelilma; Gestinari, Lísia; Santos, Norma; Romanos, Maria Teresa Villela

2011-01-01

175

Promoters of bovine papillomavirus type 1: in vitro activity and utilization.  

PubMed Central

Five of six bovine papillomavirus type 1 (BPV-1) promoters which were previously mapped by determining the 5' termini of viral mRNAs from bovine fibropapillomas and BPV-1-transformed cells were found to be active under in vitro transcription conditions. Transcription initiation at each of these promoters was accurate at the nucleotide level as determined by primer extension analysis. The most active promoter in vitro was P89, a typical RNA polymerase II promoter with both TATA and CAAT boxes. The promoters P7185 and P2443 also have TATA-like boxes, but none of the other promoters contain these typical regulatory elements. Images

Linz, U; Baker, C C

1988-01-01

176

Antiphospholipid Antibodies From Antiphospholipid Syndrome Patients Activate Endothelial Cells In Vitro and In Vivo  

Microsoft Academic Search

Background—Antiphospholipid (aPL) antibodies are associated with thrombosis in patients diagnosed with antiphospho- lipid syndrome (APS) and enhance thrombus formation in vivo in mice, but the mechanism of thrombosis by aPL is not completely understood. Although aPL antibodies have been shown to inhibit protein C activation and activate endothelial cells (ECs) in vitro, no study has examined whether these antibodies activate

Silvia S. Pierangeli; Margaret Colden-Stanfield; Xiaowei Liu; John H. Barker; Gary L. Anderson; E. Nigel Harris

177

In vitro activity of premafloxacin, a new extended-spectrum fluoroquinolone, against pathogens of veterinary importance.  

PubMed Central

The in vitro activity of premafloxacin against 673 veterinary pathogens was evaluated. Premafloxacin was equivalent to ciprofloxacin, enrofloxacin, and danofloxacin in activity against the gram-negative bacilli but was much more active (MIC for 90% of the strains tested [MIC90], 0.015 to 0.25 microg/ml) than the comparison antimicrobial agents (MIC90, 0.13 to 16.0 microg/ml) against the staphylococci, streptococci, and anaerobes tested.

Watts, J L; Salmon, S A; Sanchez, M S; Yancey, R J

1997-01-01

178

In vitro activities of new macrolides and rifapentine against Brucella spp.  

PubMed

We have tested the in vitro activities of streptomycin, rifampin, tetracyclines, trimethoprim-sulfamethoxazole, erythromycin, four new macrolides (roxithromycin, azithromycin, clarithromycin, and dirithromycin), and rifapentine against 62 strains of Brucella spp. Azithromycin and clarithromycin were, respectively, eight- and twofold more active than erythromycins (MIC for 90% of strains = 2, 8, and 16 micrograms/ml, respectively). The activity of rifapentine was similar to that of rifampin (MIC for 90% of strains = 1 microgram/ml). PMID:8494391

García-Rodríguez, J A; Muńoz Bellido, J L; Fresnadillo, M J; Trujillano, I

1993-04-01

179

In vitro activities of new macrolides and rifapentine against Brucella spp.  

PubMed Central

We have tested the in vitro activities of streptomycin, rifampin, tetracyclines, trimethoprim-sulfamethoxazole, erythromycin, four new macrolides (roxithromycin, azithromycin, clarithromycin, and dirithromycin), and rifapentine against 62 strains of Brucella spp. Azithromycin and clarithromycin were, respectively, eight- and twofold more active than erythromycins (MIC for 90% of strains = 2, 8, and 16 micrograms/ml, respectively). The activity of rifapentine was similar to that of rifampin (MIC for 90% of strains = 1 microgram/ml).

Garcia-Rodriguez, J A; Munoz Bellido, J L; Fresnadillo, M J; Trujillano, I

1993-01-01

180

Comparative in vitro activity of levofloxacin and ofloxacin against Gram-positive bacteria  

Microsoft Academic Search

The in vitro activity of levofloxacin against 506 Gram-positive bacteria was compared with those of D(?)-ofloxacin, ofloxacin, ciprofloxacin, and sparfloxacin. Levofloxacin was generally twice as active as ofloxacin against these organisms (range, 0–3 twofold dilutions). Sparfloxacin appeared to have the greatest activity overall, but for several groups of organisms minimum inhibitory concentrations (MIC90s) of this com pound were within one

George M. Eliopoulos; Christine B. Wennersten; Robert C. Moellering

1996-01-01

181

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

182

Potential role for imidazole in the rhythmic respiratory activity of the in vitro neonatal rat brainstem  

Microsoft Academic Search

We used the imidazole-binding agent, diethylpyrocarbonate (DEPC), to test the hypothesis that rhythmic respiratory activity of the in vitro neonatal rat brainstem-spinal cord preparation was functionally dependent on imidazole. Neural activity was recorded from spinal nerves (C1-C4) during superfusion with 95%O2\\/5%CO2 buffer at pH 7.3 and T=26°C. Superfusate containing DEPC (40 mM) caused cessation of rhythmic activity within minutes. In

William L Krause; Homayoun Kazemi; Melvin D Burton

1998-01-01

183

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

Microsoft Academic Search

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

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

1998-01-01

184

New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi.  

PubMed

The antiparasitic activity of azole and new 4-aminopyridine derivatives has been investigated. The imidazoles 1 and 3-5 showed a potent in vitro antichagasic activity with IC50 values in the low nanomolar concentration range. The (S)-1, (S)-3, and (S)-5 enantiomers showed (up to) a thousand-fold higher activity than the reference drug benznidazole and furthermore low cytotoxicity on rat myogenic L6 cells. PMID:24900706

Friggeri, Laura; Scipione, Luigi; Costi, Roberta; Kaiser, Marcel; Moraca, Francesca; Zamperini, Claudio; Botta, Bruno; Di Santo, Roberto; De Vita, Daniela; Brun, Reto; Tortorella, Silvano

2013-06-13

185

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

186

In vivo expression of in vitro anticoccidial activity.  

PubMed Central

Large-scale screening has led to the identification of several experimental compounds that have very potent intrinsic activity against coccidia, but the lack of translation to in vivo efficacy has been a major hurdle in developing such leads into effective new drugs. We developed methods to explore the impact of oral availability and appropriate distribution in tissue, both of which are potentially important factors in the expression of activity in vivo. For the compounds that we examined, neither oral absorption nor distribution to the site of infection appeared to be the critical barrier to in vivo expression of intrinsic anticoccidial activity. Elucidation of the nature of additional factors that might be involved could assist greatly in the identification of useful new anticoccidial agents.

Ricketts, A P; Olson, J A; Rice, J R

1992-01-01

187

In vitro biological activities of South African Pelargonium (Geraniaceae) species  

Microsoft Academic Search

Despite commercial interest and ethnobotanical data, the pharmacological activities of a number of indigenous Pelargonium species hitherto remain poorly explored. The acetone extracts of twenty-one Pelargonium species (section Pelargonium) were included in this study. Using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, potent anti-oxidant activity was observed for the crude extracts of P. betulinum and P. crispum (IC50 values of 4.13±0.14 ?g\\/ml and 4.49±0.18 ?g\\/ml,

J. Y. Y. Lalli; R. L. Van Zyl; S. F. Van Vuuren; A. M. Viljoen

2008-01-01

188

In Vitro Anthelmintic Activity of Baliospermum montanum Muell. Arg roots  

PubMed Central

Alcohol and aqueous extracts from the roots of Baliospermum montanum Muell. Arg were investigated for their anthelmintic activity against Pheretima posthuma and Ascardia galli. Various concentrations (10-100 mg/ml) of each extract were tested in the bioassay, which involved determination of time of paralysis and time of death of the worms. Both the extracts exhibited significant anthelmintic activity at highest concentration of 100 mg/ml. Piperazine citrate (10 mg/ml) was included as standard reference and distilled water as control.

Mali, R. G.; Wadekar, R. R.

2008-01-01

189

[In vitro activity of ketoconazole, itraconazole and terbinafine against Malassezia strains isolated from neonates].  

PubMed

Malassezia, a yeast-like fungus found in normal skin flora is known to be associated with various skin diseases and systemic infections. There is yet no standardized in vitro susceptibility testing method and minimum inhibitory concentration (MIC) breakpoints for Malassezia species. In this study, we investigated the in vitro activity of ketoconazole, itraconazole and terbinafine against 30 Malassezia strains (22 Malassezia furfur/dermatis, 8 M. japonica) isolated from cheek and/or scalp swabs and/or cephalic pustules of 21 neonates. The isolates were identified to species level on the basis of growth on Sabouraud dextrose agar, assimilation of Tween compounds and catalase reaction. The antifungal susceptibility tests were performed by agar dilution method using modified Dixon agar (MDA) and the agar dilution plates were incubated at 32 degrees C. For the isolates which exhibited sufficient growth, MICs were read at 48 hours, for the remaining slow-growing isolates, MIC readings were done on 7th day. For all drugs tested, the lowest concentration that provided complete inhibition of growth visually was interpreted as the MIC (microg/ml) value. Itraconazole was the most active drug in vitro against Malassezia species, followed by ketoconazole and terbinafine in rank order. In vitro activity of terbinafine was poor for half of the Malassezia strains tested. Variations in activity against individual Malassezia strains were detected for ketoconazole and terbinafine, while in vitro activity of itraconazole was similar for all strains tested. In order to validate the clinical significance of these results, further in vitro and in vivo correlation studies are needed. PMID:16358489

Sancak, Banu; Ayhan, Meltem; Karaduman, Ay?en; Arikan, Sevtap

2005-07-01

190

In Vitro Antibacterial Activity of Thymus serpyllum Extracts  

Microsoft Academic Search

Antibacterial activity of the water, ethanol and ethyl acetate extracts of Thymus serpyllum L., that grows wild in Serbia, was studied in this paper. An aerial part of the herb was investigated. Eight saprophytic and phytopathogenic bacteria were tested. The effect on bacteria was determined by filter disc diffusion method. A commercial antibiotic dovicin (Galenika a.d., Belgrade) was used as

Aleksandra STANOJKOVI?

191

In vitro anthelmintic activity of Melia azedarach naturalized in Argentina.  

PubMed

The anthelmintic activity of the drupe extracts of Melia azedarach L. (Meliaceae) growing in Argentina was tested against tapeworms, hookworms, nodular worms and earthworms, and was shown to be better than the standards piperazine phosphate and hexylresorcinol against tapeworms and hookworms, respectively. PMID:16941610

Szewczuk, Víctor D; Mongelli, Elena R; Pomilio, Alicia B

2006-11-01

192

In vitro antioxidant activities of Stevia rebaudiana leaves and callus  

Microsoft Academic Search

Leaf extract of Stevia rebaudiana promotes effects on certain physiological systems such as the cardiovascular and renal and influences hypertension and hyperglycemia. Since these activities may be correlated with the presence of antioxidant compounds, leaf and callus extracts of Stevia rebaudiana were evaluated for their total phenols, flavonoids content and total antioxidant capacity. Total phenols and flavonoids were analyzed according

M. B. Tadhani; V. H. Patel; Rema Subhash

2007-01-01

193

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

194

In vitro antiviral activity of Heterophyllaea pustulata extracts.  

PubMed

The antiviral activity was tested of different polarity extracts, with differing chemical composition, obtained from aerial parts of Heterophyllaea pustulata Hook f. (Rubiaceae) against Herpes Simplex Virus Type I (HSV-1) and Saint Louis Encephalitis Virus (SLEV). The Vero cell line was employed as a host cell for the antiviral assessment of benzene (Ben), ethyl acetate (EtOAc) and ethanol (EtOH) extracts by means of the Neutral Red uptake assay and plaque reduction test. None of the extracts showed antiviral activity against SLEV. Only the extracts (Ben and EtOAc) with a high content of anthraquinones (AQs) inhibited HSV-1 replication, exhibiting Selectivity Index (SI) values of 2.7 and 2.4, respectively. Therefore, these extracts could be good candidates as natural sources for antiviral drug development against HSV-1. PMID:22978221

Konigheim, Brenda S; Beranek, Mauricio; Comini, Laura R; Aguilar, Javier J; Marioni, Juliana; Cabrera, José L; Contigiani, Marta S; Montoya, Susana C Núńez

2012-08-01

195

Comparative in vitro activity of quinolones against Stenotrophomonas maltophilia.  

PubMed

The susceptibility of 109 Stenotrophomonas maltophilia isolates, all characterized by pulsed-field gel electrophoresis, to nine quinolones was studied. Grepafloxacin, trovafloxacin, and moxifloxacin displayed similar intrinsic activities (MIC90, 0.5 microg/ml), which were lower than those of ofloxacin and ciprofloxacin (MIC90, 4 microg/ml), norfloxacin (MIC90, 64 microg/ml), and nalidixic acid (MIC90, 32 microg/ml). Nalidixic acid was generally one- to twofold dilutions more active than norfloxacin. According to the criteria of the National Committee for Clinical Laboratory Standards (NCCLS), the percentage of isolates susceptible to ciprofloxacin (breakpoint < or = 1 microg/ml) was 76.1%. Using the NCCLS breakpoint for comparative purposes, the percentage of isolates susceptible to grepafloxacin, moxifloxacin, and trovafloxacin was 95.4, 96.4, and 96.4%, respectively. These results indicate that new quinolones may potentially be used for the management of Stenotrophomonas maltophilia infections. PMID:10691206

Valdezate, S; Vindel, A; Baquero, F; Cantón, R

1999-12-01

196

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.

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

2014-01-01

197

In vitro antibacterial activity of Phx-3 against Helicobacter pylori.  

PubMed

Phx-3, one of the phenoxazine derivatives, is reported to have inhibitory effect on Mycobacterium species and Chlamydia pneumoniae but not Escherichia coli, Salmonella Typhimurium, Pseudomonas aeruginosa, Staphylococcus aureus, Listeria monocytogenes. The bactericidal activities of Phx-3 against Helicobacter pylori strains have not been assessed. Then, we measured minimum inhibitory concentration of Phx-3 for Helicobacter strains and assessed the morphological and biochemical effects of Phx-3 on H. pylori. In present study, it has shown that H. pylori strains including clarithromycin resistant strain and Helicobacter musterae were killed effectively by the treatment with Phx-3. Furthermore, severe morphological changes such as membrane blebbing and formation of hollows in H. pylori were detected. In addition, induction of heat shock protein 60 was observed. Taken together, Phx-3 has antibacterial activity against Helicobacter pylori. PMID:20118538

Hanawa, Tomoko; Osaki, Takako; Manzoku, Taki; Fukuda, Minoru; Kawakami, Hayato; Tomoda, Akio; Kamiya, Shigeru

2010-01-01

198

In vitro activity of ertapenem: review of recent studies  

Microsoft Academic Search

Ertapenem is a long-acting, 1?-methyl parenteral Group 1 carbapenem antibiotic that has a broad anti- bacterial spectrum and once-a-day dosing supported by clinical studies. Ertapenem is active against both Gram-positive and Gram-negative bacteria, including Enterobacteriaceae, Streptococcus pneumoniae and most species of anaerobic bacteria. Isolates from a variety of infections (intra-abdominal infections, skin\\/ soft-tissue infections, community-acquired pneumonia, pelvic infections and urinary

Hannah M. Wexler

199

In-vitro activity of oxazolidinones against Mycobacterium avium complex.  

PubMed

Options for treating disseminated Mycobacterium avium complex (MAC) disease have improved. However, efficacy is not always certain, resistance is common and rapidly bactericidal agents would improve efficacy and prevent resistance. Certain oxazolidinones were tested against MAC strains and inhibited growth at expected serum concentrations or lower. Activity correlated with hydrophobicity and one agent was bactericidal at concentrations two to five times greater than the MIC. PMID:7592181

Peters, J; Kondo, K L; Lee, R K; Lin, C K; Inderlied, C B

1995-05-01

200

In vitro Evaluation of Anthelmintic Activity of Nauclea orientalis Leaves  

PubMed Central

Antianthelmintic activity of successive extracts (chloroform, acetone, ethanol and aqueous) of Nauclea orientalis leaves were evaluated separately on adult Indian earthworm (Pheretima posthuma) and compared with that of albendazole. It was found that the extracts exhibited, respectively dose-dependent action and inhibition of spontaneous motility (paralysis) and death of earthworms. The results indicated that the chloroform, ethyl acetate and ethanol extracts were more potent.

Raghavamma, S. T. V.; Rao, N. Rama

2010-01-01

201

In vitro anti-proliferative activities of ellagic acid  

Microsoft Academic Search

The potential cytotoxic and anti-proliferative activities of ellagic acid (a naturally occurring bioactive compound in berries, grapes, and nuts) was evaluated using human umbilical vein endothelial cells (HUVEC), normal human lung fibroblast cells HEL 299, Caco-2 colon, MCF-7 breast, Hs 578T breast, and DU 145 human prostatic cancer cells. Ellagic acid at concentration in the range 10–100 ?mol\\/L did not

Jack N. Losso; Rishipal R. Bansode; Alfred Trappey; Hiba A. Bawadi; Robert Truax

2004-01-01

202

In vitro antioxidant activity of species collected in Paraná.  

PubMed

Hydroalcoholic extracts of 10 medicinally used species collected from the area covered by a reservoir due to a dam built for the Salto Caxias Hydro-electric power plant in the State of Paraná, Southern Brazil, and Casearia sylvestris, were investigated for their potential antioxidant activity against DPPH (1,1-diphenyl-2-picrylhydrazyl) free radicals and by the phosphomolybdenum method. The extract of Bauhinia microstachya was found to be the most potent in both models. PMID:15159006

Menezes, P R; Schwarz, E A; Santos, C A M

2004-06-01

203

Steady States and Dynamics of Urokinase-Mediated Plasmin Activation In Silico and In Vitro  

PubMed Central

Plasmin (PLS) and urokinase-type plasminogen activator (UPA) are ubiquitous proteases that regulate the extracellular environment. Although they are secreted in inactive forms, they can activate each other through proteolytic cleavage. This mutual interplay creates the potential for complex dynamics, which we investigated using mathematical modeling and in vitro experiments. We constructed ordinary differential equations to model the conversion of precursor plasminogen into active PLS, and precursor urokinase (scUPA) into active urokinase (tcUPA). Although neither PLS nor UPA exhibits allosteric cooperativity, modeling showed that cooperativity occurred at the system level because of substrate competition. Computational simulations and bifurcation analysis predicted that the system would be bistable over a range of parameters for cooperativity and positive feedback. Cell-free experiments with recombinant proteins tested key predictions of the model. PLS activation in response to scUPA stimulus was found to be cooperative in vitro. Finally, bistability was demonstrated in vitro by the presence of two significantly different steady-state levels of PLS activation for the same levels of stimulus. We conclude that ultrasensitive, bistable activation of UPA-PLS is possible in the presence of substrate competition. An ultrasensitive threshold for activation of PLS and UPA would have ramifications for normal and disease processes, including angiogenesis, metastasis, wound healing, and fibrosis.

Venkatraman, Lakshmi; Li, Huipeng; Dewey, C. Forbes; White, Jacob K.; Bhowmick, Sourav S.; Yu, Hanry; Tucker-Kellogg, Lisa

2011-01-01

204

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

PubMed

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

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

2013-09-01

205

Similar activity of mecamylamine stereoisomers in vitro and in vivo.  

PubMed

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

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

2013-11-15

206

In Vitro Analyses of Ethanol Activity against Candida albicans Biofilms  

PubMed Central

Candida albicans is a common cause of catheter-related bloodstream infections (CR-BSI). Ethanol (EtOH) lock therapy has been attempted despite limited data on optimal dose and duration. Concentrations of 35% EtOH or higher for a minimum of 4 h demonstrated a >99% reduction in mature C. albicans biofilm metabolic activity and prevented regrowth. Concentrations of 10% EtOH or higher reduced C. albicans biofilm formation by >99%. Further investigation of EtOH lock therapy for treatment and prevention of C. albicans CR-BSI is warranted.

Rane, Hallie S.; Bernardo, Stella M.; Walraven, Carla J.

2012-01-01

207

In Vitro Antiviral Activity of V-073 against Polioviruses ?  

PubMed Central

V-073, an enterovirus capsid inhibitor, was evaluated for its spectrum of antipoliovirus activity. V-073 inhibited all 45 polioviruses tested in a virus-induced cytopathic effect protection assay, with 50% effective concentration (EC50) values ranging from 0.003 to 0.126 ?M. Ninety percent of the polioviruses tested were inhibited at EC50s of ?0.076 ?M (MIC90 = 32 ng/ml). V-073 is a promising antiviral candidate for the posteradication management of poliovirus incidents.

Oberste, M. Steven; Moore, Deborah; Anderson, Barbara; Pallansch, Mark A.; Pevear, Daniel C.; Collett, Marc S.

2009-01-01

208

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

PubMed Central

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

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

2013-01-01

209

In vitro antiprotozoal activity of the lipophilic extracts of different parts of Turkish Pistacia vera L  

Microsoft Academic Search

Thirteen lipophilic extracts prepared with n-hexane from various parts of Pistacia vera L. tree (Anacardiaceae) growing in Turkey were screened for their in vitro activity against four parasitic protozoa, Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani and Plasmodium falciparum. Melarsoprol, benznidazole, miltefosine, artemisinin and chloroquine were used as reference drugs. The cytotoxic potentials of the extracts on rat skeletal myoblast

I. Orhan; M. Aslan; B. Sener; M. Kaiser; D. Tasdemir

2006-01-01

210

Preliminary phytochemical screening and In vitro antioxidant activities of the aqueous extract of Helichrysum longifolium DC  

Microsoft Academic Search

BACKGROUND: Many oxidative stress related diseases are as a result of accumulation of free radicals in the body. A lot of researches are going on worldwide directed towards finding natural antioxidants of plants origins. The aims of this study were to evaluate in vitro antioxidant activities and to screen for phytochemical constituents of Helichrysum longifolium DC. [Family Asteraceae] aqueous crude

Olayinka A Aiyegoro; Anthony I Okoh

2010-01-01

211

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

212

In vitro antioxidant activities of the methanol extracts of four Helichrysum species from Turkey  

Microsoft Academic Search

This study was designed to examine the in vitro antioxidant activities of the methanol extracts of four Helichrysum species (Helichrysum noeanum Boiss., H. chionophilum Boiss. & Bal., H. plicatum DC. subsp. plicatum, H. arenarium (L.) Moench. subsp. aucheri (Boiss.) Davis & Kuphicha). The extracts were screened for their possible antioxidant activitiy by two complementary test systems, namely DPPH free radical-scavenging

Bektas Tepe; Munevver Sokmen; H. Askin Akpulat; Atalay Sokmen

2005-01-01

213

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...

214

Posaconazole Enhances the Activity of Amphotericin B against Hyphae of Zygomycetes In Vitro?  

PubMed Central

The in vitro activity of posaconazole plus amphotericin B against conidia and hyphae of 30 clinical zygomycetes was investigated. The combination of posaconazole with amphotericin B was found to be significantly more synergistic (40%) against hyphae (P < 0.05) than against conidia (10%). Antagonism was not observed.

Perkhofer, Susanne; Locher, Maria; Cuenca-Estrella, Manuel; Ruchel, Reinhard; Wurzner, Reinhard; Dierich, Manfred P.; Lass-Florl, Cornelia

2008-01-01

215

Simulated active control produces repeatable motion pathways of the elbow in an in vitro testing system  

Microsoft Academic Search

The purpose of this study was to determine if the repeatability and pattern of elbow kinematics are affected by changing the relative magnitudes of loads applied to muscles around the elbow in vitro. In eight cadaveric upper extremities, passive and three methods of simulated active elbow flexion were tested with the forearm maintained in both pronation and supination. Passive flexion

Cynthia E. Dunning; Teresa R. Duck; Graham J. W. King; James A. Johnson

2001-01-01

216

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

PubMed Central

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

Robledo, Sara; Osorio, Edison; Munoz, Diana; Jaramillo, Luz Marina; Restrepo, Adriana; Arango, Gabriel; Velez, Ivan

2005-01-01

217

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

PubMed Central

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

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

2007-01-01

218

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

219

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

Microsoft Academic Search

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.

Levon Gasparyan; Grigory Brill; Anu Makela

2006-01-01

220

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

Microsoft Academic Search

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

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

2008-01-01

221

In Vitro Activities of Voriconazole in Combination with Three Other Antifungal Agents against Candida glabrata  

Microsoft Academic Search

Candida glabrata has recently emerged as a significant pathogen involved in both superficial and deep-seated infections. In the present study, a checkerboard broth microdilution method was performed to investigate the in vitro activities of voriconazole (VOR) in combination with terbinafine (TRB), amphotericin B (AMB), and flucytosine (5FC) against 20 clinical isolates of C. glabrata. Synergy, defined as a fractional inhibitory

Francesco Barchiesi; Elisabetta Spreghini; Monia Maracci; Annette W. Fothergill; Isabella Baldassarri; Michael G. Rinaldi; Giorgio Scalise

2004-01-01

222

In vitro anti-mycotic activity of some medicinal plants containing flavonoids.  

PubMed

Aqueous, ethanolic and petroleum ether extracts of Citrus sinensis L. (Osbeck), Euphrasia officinalis L., Glycyrrhiza glabra L., Matricaria recutita L., Rosa canina L. and Ruta graveolens L. have been studied. The antimycotic activity was evaluated "in vitro" on strains of Candida albicans isolated from clinical samples obtained in the course of acute vaginitis. PMID:11213443

Trovato, A; Monforte, M T; Forestieri, A M; Pizzimenti, F

2000-01-01

223

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

224

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

EPA Science Inventory

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

225

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

Microsoft Academic Search

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

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

2002-01-01

226

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

227

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

228

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...

229

In vitro and in vivo effect of organophosphate pesticides on monoamine oxidase activity in rat brain  

Microsoft Academic Search

The effects of some organophosphate pesticides, e.g. lebaycid, metacid and metasystox on the monoamine oxidase (MAO) activity in rat brain mitochondria have been studied. These pesticides cause significant inhibition of MAO activityin vitro but have negligible effects on its activityin vivo.

Maitreyi Nag; Namita Nandi

1987-01-01

230

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

231

Spontaneous Electrical Activity in the Human Fetal Cortex in vitro  

PubMed Central

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

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

2011-01-01

232

In vitro antimicrobial activity of sulfonamides against some porcine pathogens.  

PubMed

The minimal inhibitory concentrations (MIC) of sulfonamides were determined against Bordetella bronchiseptica (n = 10), Pasteurella multocida (n = 10), Haemophilus pleuropneumoniae (n = 20), and Streptococcus suis (n = 10) strains isolated from pigs with atrophic rhinitis, pneumonia, or meningitis. Sulfonamides tested in an agar dilution method were sulfachloropyridazine, sulfadiazine, sulfadimethoxine, sulfamethazine, sulfadoxine, sulfisoxazole, sulfamerazine, sulfamethoxazole, sulfamethoxypyridazine, sulfanilamide, sulfatroxazole, and sulfisomidine. Results indicated that monotherapy of S suis infections with sulfonamides should not be encouraged because the MIC50 of all sulfonamides investigated was greater than 32 micrograms/ml. The MIC50 of the sulfonamides against B bronchiseptica ranged from 0.5 to 8 micrograms/ml, against P multocida from 2 to 32 micrograms/ml, and against H pleuropneumoniae from 8 to 64 micrograms/ml. The MIC50 of sulfachloropyridazine, sulfadiazine, sulfadimethoxine, sulfamerazine, and sulfamethoxazole for the gram-negative bacteria did not exceed 16 micrograms/ml. Among these compounds, sulfamethoxazole had the highest activity. The frequently prescribed sulfamethazine had an overall low antimicrobial activity. PMID:2774319

Mengelers, M J; van Klingeren, B; van Miert, A S

1989-07-01

233

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

PubMed Central

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

Soyut, Hakan; Kaya, Elif Duygu; Beydemir, Sukru

2014-01-01

234

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

235

Estrogenic Activity and Metabolism of N-Butyl Benzyl Phthalate in Vitro: Identification of the Active Molecule(s)  

Microsoft Academic Search

Some phthalates are suspected to disrupt the endocrine system, especially by mimicking estrogens. N-butyl benzyl phthalate (BBP) has estrogenic effects in vitro but not in vivo. The aim of this study was to identify the active molecule(s) (parent compound and\\/or metabolite(s)) involved in the estrogenic activities of BBP. The estrogenic effects of BBP and its in vivo metabolites were assessed

Karine Picard; Jean-Claude Lhuguenot; Marie-Chantal Lavier-Canivenc; Marie-Christine Chagnon

2001-01-01

236

In vitro anti-proliferative activities of ellagic acid.  

PubMed

The potential cytotoxic and anti-proliferative activities of ellagic acid (a naturally occurring bioactive compound in berries, grapes, and nuts) was evaluated using human umbilical vein endothelial cells (HUVEC), normal human lung fibroblast cells HEL 299, Caco-2 colon, MCF-7 breast, Hs 578T breast, and DU 145 human prostatic cancer cells. Ellagic acid at concentration in the range 10-100 micromol/L did not affect the viability of normal fibroblast cells during a 24-hour incubation. An increase in adenosine triphosphate (ATP) bioluminescence of approximately 18-21% was observed in normal cells incubated with ellagic acid. In contrast, ellagic acid at 1-100 micromol/L dose-dependently inhibited HUVEC tube formation and proliferation on a reconstituted extracellular matrix and showed strong anti-proliferative activity against the colon, breast, and prostatic cancer cell lines investigated. The most sensitive cells were the Caco-2, and the most resistant were the breast cancer cells. Ellagic acid induced cancer cell death by apoptosis as shown by the microscopic examination of cell gross morphology. Ellagic acid induced reduced cancer cell viability as shown by decreased ATP levels of the cancer cells. After 24 hours incubation of 100 micromol/L of ellagic acid with Caco-2, MCF-7, Hs 578T, and DU 145 cancer cells, ellagic acid suppressed fetal bovine serum (FBS) stimulation of cell migration. The apoptosis induction was accompanied by a decreased in the levels of pro-matrix metalloproteinase-2 (pro-MMP-2 or gelatinase A), pro-matrix metalloproteinase-9 (pro-MMP-9 or gelatinase B), and vascular endothelial growth factor (VEGF(165)) in conditioned media. The results suggest that ellagic acid expressed a selective cytotoxicity and anti-proliferative activity, and induced apoptosis in Caco-2, MCF-7, Hs 578T, and DU 145 cancer cells without any toxic effect on the viability of normal human lung fibroblast cells. It was also observed that the mechanism of apoptosis induction in ellagic acid-treated cancer cells was associated with decreased ATP production, which is crucial for the viability of cancer cells. PMID:15590271

Losso, Jack N; Bansode, Rishipal R; Trappey, Alfred; Bawadi, Hiba A; Truax, Robert

2004-11-01

237

Studies on the In Vitro and In Vivo Antifungal Activity of Fosetyl-Al and Phosphorous Acid  

Microsoft Academic Search

Fenn, M. E., and Coffey, M. D. 1984. Studies on the in vitro and in vivo antifungal activity of fosetyl-A1 and phosphorous acid. Phytopathology 74:606-611 In a low-phosphate medium fosetyl-A1 showed a much higher activity in vitro against Phytophthora than previously reported in the literature. Both fosetyl-Al, and more particularly phosphorous acid (HjPO,), were highly inhibitory in vitro against several

M. E. Fenn; M. D. Coffey

1984-01-01

238

An in vitro model for assessment of the biological activity of hepatocyte growth factor.  

PubMed

Hepatocyte growth factor (HGF) is a multifunctional growth factor with potent wound-healing properties that functions in the healing of chronic injuries. However, there may be a loss of HGF activity in certain chronic cases; this might be indicated by the presence of high amounts of HGF in body fluids and by the elevated expression of the HGF receptor in tissue biopsies. In such cases, a reliable means of assessing the activity of endogenous HGF would be valuable in allowing clinicians to decide if treatment with HGF would be useful. In this study, we developed an in vitro wound assay that used a mouse skin epithelial cell line to evaluate the biological activity of HGF. We showed that HGF accelerated the motility of the epithelial cells in a dose-dependent fashion with high sensitivity and specificity. This in vitro assay might be used to determine the activity of both endogenous and recombinant HGF. PMID:17454148

Nayeri, Fariba; Holmgren-Pettersson, Kajsa; Perskvist, Nasrin; Forsberg, Pia; Peterson, Curt; Sundqvist, Tommy

2007-02-01

239

Antihypertensive activity of peptides identified in the in vitro gastrointestinal digest of pork meat.  

PubMed

This study investigated the in vivo antihypertensive activity of three novel peptides identified in the in vitro digest of pork meat. These peptides were RPR, KAPVA and PTPVP and all of them showed significant antihypertensive activity after oral administration to spontaneously hypertensive rats, RPR being the peptide with the greatest in vivo activity. To our knowledge, this is the first report showing the in vivo antihypertensive action of the three peptides from nebulin (RPR) and titin (KAPVA and PTPVP), thus confirming their reported in vitro angiotensin I-converting enzyme (ACE) inhibitory activity. These findings suggest that pork meat could constitute a source of bioactive constituents that could be utilized in functional foods or nutraceuticals. PMID:22405912

Escudero, Elizabeth; Toldrá, Fidel; Sentandreu, Miguel Angel; Nishimura, Hitoshi; Arihara, Keizo

2012-07-01

240

In vitro antitumor activity of broccolini seeds extracts.  

PubMed

Broccolini (Brassica oleracea Italica × Alboglabra) is a hybrid of broccoli and kai-lan, Chinese broccoli. To date, no report on antitumor activity of Broccolini (NOT Broccoli) is available. In this study, we evaluated the antiproliferative effects of broccolini seeds extract (BSE) on human lung and ovarian cancer cells. It was found that BSE induces A549 and OVCAR-3 cells apoptosis in a dose-dependent manner by using MTT assay. The IC(50) values of BSE in A549 and OVCAR-3 cells were estimated to be 81.94 and 78.6?µg/ml, respectively. Furthermore, the phase contrast microscope showed that in high-dose group (90?120?µg/ml), the morphology structure of OVCAR-3 cells become irregular and exhibited characteristics of apoptosis such as cell membrane shrinkage, condensation and fragmentation of nuclear chromatin as well as formation of apoptotic bodies. PMID:21695707

Yang, Yanjing; Zhang, Xuewu

2011-01-01

241

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

PubMed

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

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

2014-01-01

242

Two different interictal spike patterns anticipate ictal activity in vitro.  

PubMed

4-Aminopyridine (4AP, 50 ?M) induces interictal- and ictal-like discharges in brain slices including parahippocampal areas such as the entorhinal cortex (EC) but the relation between these two types of epileptiform activity remains undifined. Here, by employing field potential recordings in rat EC slices during 4AP application, we found that: (i) interictal events have a wide range of duration (0.4-3.3 s) and interval of occurrence (1.4-84 s); (ii) ictal discharges are either preceded by an isolated "slow" interictal discharge (ISID; duration=1.5 ± 0.1s, interval of occurrence=33.8 ± 1.8 s) or suddenly initiate from a pattern of frequent polispike interictal discharge (FPID; duration=0.8 ± 0.1 s; interval of occurrence=2.7 ± 0.2 s); and (iii) ISID-triggered ictal events have longer duration (116 ± 7.3s) and interval of occurrence (425.8 ± 42.3 s) than those initiating suddenly during FPID (58.3 ± 7.8 s and 202.1 ± 21.8 s, respectively). Glutamatergic receptor antagonists abolished ictal discharges in all experiments, markedly reduced FPIDs but did not influence ISIDs. We also discovered that high-frequency oscillations (HFOs, 80-500 Hz) occur more frequently during ISIDs as compared to FPIDs, and mainly coincide with the onset of ISID-triggered ictal discharges. These findings indicate that interictal events may define ictal onset features resembling those seen in vivo in low-voltage fast activity onset seizures. We propose a similar condition to occur in vivo in temporal lobe epileptic patients and animal models. PMID:23270790

Avoli, Massimo; Panuccio, Gabriella; Herrington, Rochelle; D'Antuono, Margherita; de Guzman, Philip; Lévesque, Maxime

2013-04-01

243

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

PubMed Central

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

Carbajal-Saucedo, Alejandro; Floriano, Rafael Stuani; Dal Belo, Chariston Andre; Olvera-Rodriguez, Alejandro; Alagon, Alejandro; Rodrigues-Simioni, Lea

2014-01-01

244

Potential anticancer activity of litchi fruit pericarp extract against hepatocellular carcinoma in vitro and in vivo.  

PubMed

Litchi fruit pericarp (LFP) extract contains significant amounts of polyphenolic compounds, and exhibits powerful antioxidative activity against fat oxidation in vitro. The purpose of this study is to confirm the anticancer activity of LFP extract against hepatocellular carcinoma in vitro and in vivo, and to elucidate the mechanism of its activity. Human hepatocellular carcinoma cell line was tested in vitro for cytotoxicity, colony formation inhibition, and cell cycle distribution through flow cytometry after treatment with water-soluble crude ethanolic extract (CEE) from LFP. Murine hepatoma bearing-mice were fed doses of 0.15, 0.3, and 0.6g/kg/day of water-soluble CEE in DH(2)O p.o. for 10 days, respectively, to test the anticancer activity and BrdU incorporation of cancer cells in vivo. LFP extract demonstrated a dose- and time-dependent inhibitory effect on cancer cell growth; IC(50) was 80microg/ml, and significantly inhibited colony formation in vitro, tumor growth and BrdU incorporation into cancer cells in vivo. The tumor inhibitory rates at doses of 0.15, 0.3, and 0.6g/kg/day were 17.31% (P>0.05), 30.77% (P<0.05), and 44.23% (P<0.01), respectively. BrdU labeled tumor cells of treated animals were 11.80+/-2.79%, and were significantly lower than that in untreated controls (23.00+/-5.42%, P<0.05). Our findings showed that LFP extract exhibited potential anticancer activity against hepatocellular carcinoma in vitro and in vivo through proliferating inhibition and apoptosis induction of cancer cells. PMID:16300877

Wang, Xiujie; Wei, Yuquan; Yuan, Shulan; Liu, Guanjian; Zhang, Yanrong Lu Jie; Wang, Wendong

2006-07-28

245

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

246

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

247

Factors influencing the activity of tiamulin against Histomonas meleagridis in vitro.  

PubMed

In this study, we investigated the activity of tiamulin fumerate against three strains of Histomonas meleagridis in vitro under different conditions. Tiamulin reduced histomonal growth of all three strains at concentrations of 20 ppm and higher. Cultures in phosphate-buffered saline-based medium were more susceptible than cultures in traditional Dwyers medium. When the cultures were inoculated with higher numbers of histomonads, the activity of tiamulin was reduced. Bacteria present in the cultures were resistant against tiamulin. PMID:20608543

Hauck, R; Lotfi, A; Hafez, H M

2010-06-01

248

In vitro assessment of anti - cutaneous leishmaniasis activity of some Sudanese plants.  

PubMed

Examination of crude methanol extracts of four Sudanese plants (Azadirachta indica, Acacia nilotica, Balanites aegyptiaca and Allium sativa) revealed that only three species had a considerable in-vitro anti-leishmanial activity on Leishmania major promastigotes. The plants Azadrachta indica, Allium sativa, and Acacia nilotica gave a LC50 of 10.2, 4.94, and 89.38 microg/ml, respectively. Extracts of Balanites aegyptiaca had a moderate biological activity on L major promastigotes. PMID:17167733

Fatima, Fatima; Khalid, A; Nazar, Nazar; Abdalla, M; Mohomed, Husam; Toum, Abdalla M; Magzoub, Mubark; Al?, M Siddig

2005-01-01

249

In vitro bactericidal activity of oxazolidinone, RBx 8700 against Mycobacterium tuberculosis and Mycobacterium avium complex.  

PubMed

RBx 8700, an investigational oxazolidinone, has excellent activity against respiratory pathogens. We evaluated the in vitro minimum inhibitory concentration (MIC) and bactericidal activity of RBx 8700 against Mycobacterium tuberculosis and Mycobacterium avium complex (MAC) isolates. RBx 8700 had an MIC of 1 gLg/ml against M. tuberculosis isolates resistant to both isoniazid (INH) and rifampicin (RIF), whereas its MIC against M. tuberculosis isolates resistant to either INH or RIF was 0.5 microg/ml. PMID:16736882

Rao, M; Sood, R; Malhotra, S; Fatma, T; Upadhyay, D J; Rattan, A

2006-04-01

250

In vitro and in vivo antibacterial activities of E1077, a novel parenteral cephalosporin.  

PubMed Central

E1077, a new injectable cephalosporin with a broad antibacterial spectrum and potent antibacterial activity, was evaluated for its in vitro and in vivo antibacterial activities in comparison with those of cefpirome, cefuzonam, ceftazidime, and cefotaxime. E1077 showed broad in vitro antibacterial activity against gram-positive and gram-negative bacteria. Against methicillin-susceptible Staphylococcus aureus, E1077 was as active as cefpirome; the MIC for 90% of strains tested (MIC90) was 1.0 microgram/ml. Against methicillin-resistant S. aureus, E1077 was less active (MIC90, 64 micrograms/ml). For Enterobacter cloacae and Pseudomonas aeruginosa, E1077 was fourfold more active than cefpirome, with MIC90s of 1.0 and 16 micrograms/ml, respectively. For Proteus vulgaris, the MIC90 of E1077 was 32 micrograms/ml, which was fourfold greater than that of cefpirome. Against other gram-negative strains tested, the in vitro activity of E1077 was comparable to that of cefpirome. The broad antibacterial spectrum of E1077 was reflected by its in vivo efficacy against experimental septicemia caused by gram-positive and gram-negative bacteria. Against S. aureus 90 and P. aeruginosa E7, E1077 had activity superior to those of the reference compounds; against most other bacterial strains, the efficacy of E1077 was similar to that of cefpirome. Levels of E1077 in plasma and tissue of mice were studied. At 15 min after a single subcutaneous administration, E1077 displayed high peak levels (mean, 31.8 +/- 3.1 micrograms/ml). These results indicate that the in vitro and in vivo efficacies of E1077 are similar to those of cefpirome except against P. aeruginosa and P. vulgaris.

Toyosawa, T; Miyazaki, S; Tsuji, A; Yamaguchi, K; Goto, S

1993-01-01

251

Antibacterial activity in vitro of cefpirome against clinical isolates causing sexually transmitted diseases.  

PubMed

The in-vitro activity of cefpirome was compared with other antibiotics against organisms causing sexually transmitted diseases (STD). The excellent activity of cefpirome against Neisseria gonorrhoeae (MIC90 1.0 mg/L), Haemophilus ducreyi (MIC90 0.5 mg/L), and Gardnerella vaginalis (MIC90 1.0 mg/L) suggests that this agent might be useful in the empirical treatment of a variety of venereal diseases. PMID:1318294

Limbert, M; Seibert, G; Winkler, I; Isert, D; Klesel, N; Markus, A; Schrinner, E

1992-04-01

252

In Vitro and In Vivo Antifungal Activities of T-2307, a Novel Arylamidine  

Microsoft Academic Search

The in vitro and in vivo antifungal activities of T-2307, a novel arylamidine, were evaluated and compared with those of fluconazole, voriconazole, micafungin, and amphotericin B. T-2307 exhibited broad-spectrum activity against clinically significant pathogens, including Candida species (MIC range, 0.00025 to 0.0078 g\\/ml), Cryptococcus neoformans (MIC range, 0.0039 to 0.0625 g\\/ml), and Aspergillus species (MIC range, 0.0156 to 4 g\\/ml).

Junichi Mitsuyama; Nobuhiko Nomura; Kyoko Hashimoto; Eio Yamada; Hiroshi Nishikawa; Makoto Kaeriyama; Akiko Kimura; Yozo Todo; Hirokazu Narita

2008-01-01

253

In Vitro Activities of 15 Antimicrobial Agents against Clinical Isolates of South African Enterococci  

PubMed Central

The activities of a panel of currently available antibiotics and the investigational agents LY 333328, linezolid, CL 331,002, CL 329,998, moxifloxacin (BAY 12-8039), trovafloxacin, and quinupristin-dalfopristin against 274 clinical isolates of enterococci were determined. No vancomycin resistance or ?-lactamase production was observed. Except for 12 isolates (all non-Enterococcus faecalis) showing reduced susceptibility to quinupristin-dalfopristin (MIC, ?4 ?g/ml), the new agents exhibited promising in vitro antienterococcal activity.

Struwig, M. C.; Botha, P. L.; Chalkley, L. J.

1998-01-01

254

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

Microsoft Academic Search

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

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

2006-01-01

255

A comparison of in vitro anticancerous activity and mechanism of ethanolic extracts from different Ganoderma genus  

Microsoft Academic Search

Five ethanolic extracts from the mycelia of Ganoderma lucidum, G. tsugae, G. oerstedii, G. subamboinense, and G. resinaceum were respectively studied on their anticancerous activities against leukemic HL-60 cell line in vitro. Results showed that\\u000a all five extracts potently inhibited HL-60 proliferation. The extract from G. lucidum mycelia exerted the highest activity. Annexin V\\/PI bivariate flow cytometric analysis further revealed

Yueqin Zhou; Xiaotong Yang; Xuquan Li; Huiqin Feng; Ke Mi; Qingyao Yang

2006-01-01

256

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

Microsoft Academic Search

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

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

2010-01-01

257

In vitro anti-influenza virus activity of a cardiotonic glycoside from Adenium obesum (Forssk.)  

Microsoft Academic Search

Methanolic extracts of six Saudi plants were screened for their in vitro antiviral activity using influenza virus A\\/PR\\/8\\/34 (H1N1) and MDCK cells in an MTT assay. The results indicated that the extracts of Adeniumobesum and Tephorosianubica possessed antiviral activity (99.3 and 93.3% inhibition at the concentration of 10?g\\/ml, respectively). Based on these results A. obesum was selected for further study

Hiroaki Kiyohara; Chikara Ichino; Yuka Kawamura; Takayuki Nagai; Noriko Sato; Haruki Yamada; Maha M. Salama; Essam Abdel-Sattar

258

Comparative in vitro activity of several antimicrobial agents against selected clinical isolates.  

PubMed

A comparison between the in vitro activities of ceftazidime, cefotaxime, ceftriaxone, ampicillin, piperacillin, gentamicin, tobramycin and netilmicin was performed on selected clinical isolates. The activity of the agents was assessed by means of minimum inhibitory concentration determinations, and time-kill studies. The third generation cephalosporins were active against all members of the Enterobacteriaceae excluding some Enterobacter species. Their activity against these bacteria was generally comparable and greater than that of piperacillin. Netilmicin was the most active of the aminoglycosides tested against members of the Enterobacteriaceae; however, aminoglycoside-resistant strains were encountered. Ceftazidime was the most active of the third generation cephalosporins against the non-fermenters (e.g. Pseudomonas and Acinetobacter spp), its inhibitory activity also being greater than that of piperacillin. Using a time-kill study, ceftazidime also demonstrated greater bactericidal activity than piperacillin against an isolate of Pseudomonas aeruginosa. The aminoglycoside demonstrating the greatest activity against the non-fermenters was tobramycin. PMID:2109875

Liebowitz, L D; Saunders, J; Chalkley, L J; Koornhof, H J

1990-04-21

259

Evaluation of anticancer activity of dehydrocostuslactone in vitro.  

PubMed

Dehydrocostuslactone is a sesquiterpene lactone derived from Saussurea lappa, a plant used in traditional herbal medicines. The anti-proliferative activity of dehydrocostuslactone was investigated in human breast cancer (MDA-MB-231, MDA-MB-453 and SK-BR-3) and ovarian cancer (SK-OV-3 and OVCAR3) cell lines using the methyl thiazolyl tetrazolium assay. In the cells, exposure to dehydrocostuslactone resulted in a dose-dependent decline in cell proliferation. The IC50 value was found to be 21.5, 43.2, 25.6, 15.9 and 10.8 µM in MDA-MB-231, MDA-MB-453, SK-BR-3, SK-OV-3 and OVCAR3 cells, respectively. Dehydrocostuslactone exerted its antiproliferative effects by inducing cell cycle arrest and apoptosis. Cell cycle distribution and apoptosis were analyzed using flow cytometry in cell lines exposed to 10 µM dehydrocostuslactone for 48 h. Compared to the controls, exposure to dehydrocostuslactone resulted in accumulation in the G2/M phase and a marked increase in the apoptotic cell population. These results suggest that dehydrocostuslactone has potential anticancer properties. PMID:21472220

Choi, Eun J; Kim, Gun-Hee

2010-01-01

260

Antimycobacterial activity in vitro of pigments isolated from Antarctic bacteria.  

PubMed

In this study, we describe the antimycobacterial activity of two pigments, violacein, a purple violet pigment from Janthinobacterium sp. Ant5-2 (J-PVP), and flexirubin, a yellow-orange pigment from Flavobacterium sp. Ant342 (F-YOP). These pigments were isolated from bacterial strains found in the land-locked freshwater lakes of Schirmacher Oasis, East Antarctica. The minimum inhibitory concentrations (MICs) of these pigments for avirulent and virulent mycobacteria were determined by the microplate Alamar Blue Assay (MABA) and Nitrate Reductase Assay (NRA). Results indicated that the MICs of J-PVP and F-YOP were 8.6 and 3.6 ?g/ml for avirulent Mycobacterium smegmatis mc˛155; 5 and 2.6 ?g/ml for avirulent Mycobacterium tuberculosis mc˛6230; and 34.4 and 10.8 ?g/ml for virulent M. tuberculosis H??Rv, respectively. J-PVP exhibited a ~15 times lower MIC for Mycobacterium sp. than previously reported for violacein pigment from Chromobacterium violaceum, while the antimycobacterial effect of F-YOP remains undocumented. Our results indicate these pigments isolated from Antarctic bacteria might be valuable lead compounds for new antimycobacterial drugs used for chemotherapy of tuberculosis. PMID:20556653

Mojib, Nazia; Philpott, Rachel; Huang, Jonathan P; Niederweis, Michael; Bej, Asim K

2010-11-01

261

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

262

In Vitro and In Vivo Antifungal Activity of Amphotericin B Lipid Complex: Are Phospholipases Important?  

PubMed Central

Amphotericin B lipid complex for injection (ABLC) is a suspension of amphotericin B complexed with the lipids l-?-dimyristoylphosphatidylcholine (DMPC) and l-?-dimyristoylphosphatidylglycerol. ABLC is less toxic than amphotericin B deoxycholate (AmB-d), while it maintains the antifungal activity of AmB-d. Active amphotericin B can be released from ABLC by exogenously added (snake venom, bacteria, or Candida-derived) phospholipases or by phospholipases derived from activated mammalian vascular tissue (rat arteries). Such extracellular phospholipases are capable of hydrolyzing the major lipid in ABLC. Mutants of C. albicans that were resistant to ABLC but not AmB-d in vitro were deficient in extracellular phospholipase activity, as measured on egg yolk agar or as measured by their ability to hydrolyze DMPC in ABLC. ABLC was nevertheless effective in the treatment of experimental murine infections produced by these mutants. Isolates of Aspergillus species, apparently resistant to ABLC in vitro (but susceptible to AmB-d), were also susceptible to ABLC in vivo. We suggest that routine in vitro susceptibility tests with ABLC itself as the test material may not accurately predict the in vivo activity of ABLC and that the enhanced therapeutic index of ABLC relative to that of AmB-d in vivo may be due, in part, to the selective release of active amphotericin B from the complex at sites of fungal infection through the action of fungal or host cell-derived phospholipases.

Swenson, Christine E.; Perkins, Walter R.; Roberts, Patricia; Ahmad, Imran; Stevens, Rachel; Stevens, David A.; Janoff, Andrew S.

1998-01-01

263

Synthesis of an enzymatically active FLP recombinase in vitro: search for a DNA-binding domain.  

PubMed Central

We have used an in vitro transcription and translation system to synthesize an enzymatically active FLP protein. The FLP mRNA synthesized in vitro by SP6 polymerase is translated efficiently in a rabbit reticulocyte lysate to produce enzymatically active FLP. Using this system, we assessed the effect of deletions and tetrapeptide insertions on the ability of the respective variant proteins synthesized in vitro to bind to the FLP recognition target site and to carry out excisive recombination. Deletions of as few as six amino acids from either the carboxy- or amino-terminal region of FLP resulted in loss of binding activity. Likewise, insertions at amino acid positions 79, 203, and 286 abolished DNA-binding activity. On the other hand, a protein with an insertion at amino acid 364 retained significant DNA-binding activity but had no detectable recombination activity. Also, an insertion at amino acid 115 had no measurable effect on DNA binding, but recombination was reduced by 95%. In addition, an insertion at amino acid 411 had no effect on DNA binding and recombination. On the basis of these results, we conclude that this approach fails to define a discrete DNA-binding domain. The possible reasons for this result are discussed. Images

Amin, A A; Sadowski, P D

1989-01-01

264

Review on in vivo and in vitro methods evaluation of antioxidant activity  

PubMed Central

A good number of abstracts and research articles (in total 74) published, so far, for evaluating antioxidant activity of various samples of research interest were gone through where 407 methods were come across, which were repeated from 29 different methods. These were classified as in vitro and in vivo methods. And those are described and discussed below in this review article. In the later part of this review article, frequency of in vitro as well as in vivo methods is analyzed with a bar diagram. Solvents are important for extracting antioxidants from natural sources. Frequency of solvents used for extraction is also portrayed and the results are discussed in this article. As per this review there are 19 in vitro methods and 10 in vivo methods that are being used for the evaluation of antioxidant activity of the sample of interest. DPPH method was found to be used mostly for the in vitro antioxidant activity evaluation purpose while LPO was found as mostly used in vivo antioxidant assay. Ethanol was with the highest frequency as solvent for extraction purpose.

Alam, Md. Nur; Bristi, Nusrat Jahan; Rafiquzzaman, Md.

2012-01-01

265

The in Vitro Estrogenic Activities of Polyfluorinated Iodine Alkanes  

PubMed Central

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

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

2011-01-01

266

Modulation of complement activity in vitro and in vivo by Yersinia wild and mutant strains.  

PubMed

The ability of released proteins (Yops) and surface lipopolysaccharides (LPS) from the wild-type strain Yersinia enterocolitica 8081-L2, serotype 0:8 to influence the complement activity was determined. Yops and LPS from wild-type and mutant strains showed different ability to affect the classical pathway (CP) functional complement activity in vitro. The serum CP activity was inhibited during the infection induced with six Y. enterocolitica and three Y. pseudotuberculosis strains in rabbits. The changed complement activity might be of importance for the course of Yersinia infections. PMID:16821708

Yordanov, M; Golkocheva, E; Najdenski, H

2006-01-01

267

Verbascoside isolated from Lepechinia speciosa has inhibitory activity against HSV-1 and HSV-2 in vitro.  

PubMed

Verbascoside has been isolated form L. speciosa after several different chromatographic methods. After its purification, the structure has been unequivocally established using modern spectroscopic techniques. As for the antiviral activity, the maximum non toxic concentration has been established and this concentration has been used in the anti herpes assay, in vitro. Mechanism of action for this molecule regarding the anti-herpes activity has been studied encompassing the following assays: virucidal activity, cellular receptor assay, penetration assay and intracellular assay, in order to understand the activity for this natural product. PMID:20120109

Martins, Fernanda O; Esteves, Patricia F; Mendes, Gabriella S; Barbi, Nanci S; Menezes, Fabio S; Romanos, Maria T V

2009-12-01

268

Optimized combined electrical-chemical parthenogenetic activation for in vitro matured bovine oocytes.  

PubMed

Sperm-mediated oocyte activation is a complex procedure, both in steps and duration, not yet been completely mimicked during in vitro studies, e.g., parthenogenesis or somatic cell nuclear transfer. Furthermore, parthenogenetic studies have been recognized as a suitable model for studying activation efficiency for nuclear transfer cloning. This study, therefore, was conducted to develop an optimized artificial activation method, based on bovine cloning. In vitro matured bovine oocytes were initially exposed to electrical pulse, used for cell fusion during cloning, and then treated with 15 temporal sequential combinations of 3 chemical activators [calcium ionophore (CI), strontium (SR) and ethanol (ET)], followed by exposure to a protein kinase inhibitor or used for in vitro fertilization as control group. Treated and naturally fertilized oocytes were further cultured for up to 8 days. Embryo development was scored daily and blastocyst cell counting was carried out using differential staining at day 8 of culture. Among 15 temporal sequential combinations of three chemical activators, the best cleavage rates were associated with double (SR-CI, 84.4%), triple (CI-SR-ET, 79.4%) and single (CI, 73.7%) compounds, respectively, which were not significantly different with each other and with in vitro fertilized (IVF) (85.5%). The highest blastocyst rates were gained with ET-SR (24.5%), SR-CI-ET (20.4%) and CI (24.5%) accordingly which were not significantly different with each other but significantly lower than IVF (47%). Embryo cell counting further confirmed reasonably better quality of blastocysts produced using double, triple and single compounds. Although most of the sequential artificial activation compounds induced high cleavage rate, close to IVF, but this did not assure comparable further embryo development to the blastocyst stage. Nevertheless, the results suggest exposure of in vitro matured bovine oocytes to electrical pulse, followed by exposure to CI-6-dimethylaminopurine (6-DMAP) or ET-SR-6-DMAP could be regarded as the optimal artificial activation protocol for in vitro development of parthenogenic bovine oocytes or as a step for activation protocol in cloning procedure. PMID:17826013

Hosseini, S M; Hajian, M; Moulavi, F; Shahverdi, A H; Nasr-Esfahani, M H

2008-10-01

269

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

270

Surface activity in vitro: role of surfactant proteins.  

PubMed

Pattle, who provided some of the initial direct evidence for the presence of pulmonary surfactant in the lung, was also the first to show surfactant was susceptible to proteases such as trypsin. Pattle concluded surfactant was a lipoprotein. Our group has investigated the roles of the surfactant proteins (SP-) SP-A, SP-B, and SP-C using a captive bubble tensiometer. These studies show that SP-C>SP-B>SP-A in enhancing surfactant lipid adsorption (film formation) to the equilibrium surface tension of approximately 22-25 mN/m from the 70 mN/m of saline at 37 degrees C. In addition to enhancing adsorption, surfactant proteins can stabilize surfactant films so that lateral compression induced through surface area reduction results in the lowering of surface tension (gamma) from approximately 25 mN/m (equilibrium) to values near 0 mN/m. These low tensions, which are required to stabilize alveoli during expiration, are thought to arise through exclusion of fluid phospholipids from the surface monolayer, resulting in an enrichment in the gel phase component dipalmitoylphosphatidylcholine (DPPC). The results are consistent with DPPC enrichment occurring through two mechanisms, selective DPPC adsorption and preferential squeeze-out of fluid components such as unsaturated phosphatidylcholine (PC) and phosphatidylglycerol (PG) from the monolayer. Evidence for selective DPPC adsorption arises from experiments showing that the surface area reductions required to achieve gamma near 0 mN/m with DPPC/PG samples containing SP-B or SP-A plus SP-B films were less than those predicted for a pure squeeze-out mechanism. Surface activity improves during quasi-static or dynamic compression-expansion cycles, indicating the squeeze-out mechanism also occurs. Although SP-C was not as effective as SP-B in promoting selective DPPC adsorption, this protein is more effective in promoting the reinsertion of lipids forced out of the surface monolayer following overcompression at low gamma values. Addition of SP-A to samples containing SP-B but not SP-C limits the increase in gamma(max) during expansion. It is concluded that the surfactant apoproteins possess distinct overlapping functions. SP-B is effective in selective DPPC insertion during monolayer formation and in PG squeeze-out during monolayer compression. SP-A can promote adsorption during film formation, particularly in the presence of SP-B. SP-C appears to have a superior role to SP-B in formation of the surfactant reservoir and in reinsertion of collapse phase lipids. PMID:11369545

Possmayer, F; Nag, K; Rodriguez, K; Qanbar, R; Schürch, S

2001-05-01

271

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

272

Microplitis croceipes teratocytes: in vitro culture and biological activity of teratocyte secreted protein.  

PubMed

Teratocytes originate from the dissociation of the extraembryonic serosal membrane in some Braconidae and Scelionidae. Methods used to culture teratocytes in vitro are described and the yield of teratocyte secreted proteins (TSP) was measured. Although 90% are viable after 6 days, in vitro teratocytes reached only half the diameter (32&mgr;m) of the same age teratocytes obtained in vivo. Teratocytes cultured in vitro secrete as much as 0.7&mgr;g of protein per day per larval equivalent ( approximately 900 cells). Presence of parasitoid larvae enhanced teratocyte viability while periodic exchange of medium did not. However, medium exchange significantly increased the total amount of protein secreted. Size and viability were improved with the addition of 10% FBS to the Ex-cell 400 culture medium. Non-denaturing PAGE showed at least 15 proteins with molecular sizes estimated to be between 24 to 347kDa in medium containing teratocytes. An in vitro fat body assay was developed to measure the effect of TSP on protein synthesis and juvenile hormone esterase (JHE) activity. Crude TSP inhibited in vitro incorporation of [(35)S]-methionine into protein synthesized by the fat body. The amount of JHE released from in vitro fat body treated with crude TSP was significantly less than controls, most likely caused by the inhibition of general protein synthesis. The active fraction of TSP passed through a 30kDa molecular weight cutoff filter but was retained by a 3kDa filter. SDS-PAGE revealed four proteins with molecular weights between 8 and 20kDa not present in control medium incubated without teratocytes. PMID:12769872

Zhang, D; Dahlman, D L.; Schepers, E J.

1998-09-01

273

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

PubMed

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

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

2013-07-01

274

In vitro and in vivo anti-plasmodial activity of essential oils, including hinokitiol.  

PubMed

Abstract. The anti-plasmodial activity of 47 essential oils and 10 of their constituents were screened for in vitro activity against Plasmodium falciparum. Five of these essential oils (sandalwood, caraway, monarda, nutmeg, and Thujopsis dolabrata var. hondai) and 2 constituents (thymoquinone and hinokitiol) were found to be active against P. falciparum in vitro, with 50% inhibitory concentration (IC50) values equal to or less than 1.0 microg/ml. Furthermore, in vivo analysis using a rodent model confirmed the anti-plasmodial potential of subcutaneously administered sandalwood oil, and percutaneously administered hinokitiol and caraway oil against rodent P. berghei. Notably, these oils showed no efficacy when administered orally, intraperitoneally or intravenously. Caraway oil and hinokitiol dissolved in carrier oil, applied to the skin of hairless mice caused high levels in the blood, with concentrations exceeding their IC50 values. PMID:23082579

Fujisaki, Ryuichi; Kamei, Kiyoko; Yamamura, Mariko; Nishiya, Hajime; Inouye, Shigeharu; Takahashi, Miki; Abe, Shigeru

2012-03-01

275

In vitro activity of the spermicide nonoxynol-9 against Chlamydia trachomatis.  

PubMed Central

The in vitro activity of nonoxynol-9 against four serotypes (C, D, H, and K) of Chlamydia trachomatis was investigated. A constant inoculum of each serotype was exposed to serial twofold dilutions (1:100 to 1:800) of Koromex, Conceptrol, or reference preparations (not containing nonoxynol-9) for 4 and 24 h at 37 degrees C. The mixtures of nonoxynal-9 or nonnonoxynol preparations and control inocula were dispensed into triplicate wells containing McCoy cell monolayers. After incubation at 37 degrees C, the monolayers were fixed and stained with iodine and examined for evidence of infection with C. trachomatis. All nonoxynol-9-containing preparations showed marked antichlamydial activity as judged by percent reduction of glycogen-containing intracytoplasmic inclusions. The reference preparations, which did not contain nonoxynol-9, were markedly less active when tested in this in vitro system.

Kelly, J P; Reynolds, R B; Stagno, S; Louv, W C; Alexander, W J

1985-01-01

276

In vitro antiplasmodial activity of ethanolic extracts of seaweed macroalgae against Plasmodium falciparum.  

PubMed

Malaria is a major health problem in many developing countries. The drugs resistant Plasmodium falciparum causes the most virulent form of malaria in humans and it is described as a public health disaster causing increased morbidity and mortality. Thirteen seaweeds species which belong to four different families (Rhodomelaceae, Cladophoraceae, Ulvaceae, and Caulerpaceae) were collected from Mandapam coastal area and the seaweeds extracts were tested for in vitro antiplasmodial activity against P. falciparum. Among them, Caulerpa toxifolia (IC(50) 5.06 ?g·ml(-1)) showed potential antiplasmodial activity than other seaweeds extracts and it can be comparable with the positive control artemether (IC(50) 4.09 ?g·ml(-1)). Caulerpa peltata (IC(50) 16.69 ?g·ml(-1)) also exhibited good antiplasmodial activity and the IC(50) value is lesser than the positive control chloroquine (IC(50) 19.59 ?g·ml(-1)). Statistical analysis reveals that significant in vitro antiplasmodial activity (P<0.05) was observed between the concentrations and time of exposure. The chemical injury to erythrocytes was also carried out and it shows that no morphological changes in erythrocytes by the ethanolic extract of seaweeds extracts after 48 h of incubation. The in vitro antiplasmodial activity might be due to the presence of sugars, proteins, and phenols in the ethanolic extracts of seaweeds. It is concluded from the present study that, the ethanolic extracts of seaweeds of C. toxifolia and C. peltata possesses lead compounds for development of antiplasmodial drugs. PMID:21120527

Ravikumar, Sundaram; Inbaneson, Samuel Jacob; Suganthi, Palavesam; Gokulakrishnan, Ramasamy; Venkatesan, Malaiyandi

2011-06-01

277

The estrogenic activity of isoflavones extracted from chickpea Cicer arietinum L sprouts in vitro.  

PubMed

Isoflavones have drawn attention due to their potential therapeutic use. Isoflavones are the important chemical components of the seeds and sprouts of chickpea and higher isoflavones in sprouts than in seeds. However, there have been no previous reports of the estrogenic activity of isoflavones extracted from chickpea Cicer arietinum L sprouts (ICS) in vitro. In this study, which incorporated several in vitro bioassays methods, we systematically evaluated the estrogenic properties of ICS. MTT assay showed that ICS at the low concentration ranges (10(-3)-1 mg/L) promoted MCF-7 cell growth, while at high concentrations, (>1 mg/L) inhibited cell proliferation, indicating ICS worked at a diphasic mechanism. Flow cytometric analysis further calculated the proliferation rate of ICS at low concentration (1 mg/L). ER?/Luc trans-activation assay and then semi-quantitative RT-PCR analysis indicated that ICS at low concentrations induced ER?-mediated luciferase activity in MCF-7 cells and promoted the ER downstream target gene pS2 and PR trans-activation. These effects were inhibited by ICI 182,780, a special antagonist of ER, indicating that an ER-mediating pathway was involved. Alkaline phosphatase (AP) expression in Ishikawa cells showed that ICS at low concentrations stimulated AP expression. Our current study is the first to demonstrate that ICS has significant estrogenic activity in vitro. ICS may be useful as a supplement to hormone replacement therapy and in dietary supplements. PMID:23065723

HaiRong, Ma; HuaBo, Wei; Zhen, Chen; Yi, Yang; ZhengHua, Wang; Madina, Habasi; Xu, Cao; Akber, Aisa Haji

2013-08-01

278

Activated charcoal: in vivo and in vitro studies of effect on gas formation.  

PubMed

It has been reported that activated charcoal reduces intestinal gas production after ingestion of beans as evidenced by decreased breath hydrogen excretion and decreased passage of flatus. In the present study we assessed the ability of activated charcoal to reduce intestinal gas production by in vitro and in vivo methods. In vitro studies were performed using human fecal homogenates incubated with or without additional carbohydrate. In all studies hydrogen and carbon dioxide production and consumption occurred at similar rates in the charcoal-treated homogenate as compared with the untreated control. The influence of activated charcoal on gas production, in vivo, was studied by double-blind assessment of breath hydrogen excretion and flatus excretion after ingestion of a baked bean meal. No significant difference was observed in breath hydrogen concentration or number of passages of flatus in subjects who ingested 16 capsules of activated charcoal (4 g) as opposed to the placebo. We conclude that activated charcoal does not influence gas formation in vitro or in vivo. PMID:3917957

Potter, T; Ellis, C; Levitt, M

1985-03-01

279

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

PubMed Central

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

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

1996-01-01

280

Antioxidative and in vitro antiproliferative activity of Arctium lappa root extracts  

PubMed Central

Background Arctium lappa, known as burdock, is widely used in popular medicine for hypertension, gout, hepatitis and other inflammatory disorders. Pharmacological studies indicated that burdock roots have hepatoprotective, anti-inflammatory, free radical scavenging and antiproliferative activities. The aim of this study was to evaluate total phenolic content, radical scavenging activity by DPPH and in vitro antiproliferative activity of different A. lappa root extracts. Methods Hot and room temperature dichloromethanic, ethanolic and aqueous extracts; hydroethanolic and total aqueous extract of A. lappa roots were investigated regarding radical scavenging activity by DPPH, total phenolic content by Folin-Ciocalteau method and antiproliferative in vitro activity was evaluated in human cancer cell lines. The hydroethanolic extract analyzed by high-resolution electrospray ionization mass spectroscopy. Results Higher radical scavenging activity was found for the hydroethanolic extract. The higher phenolic contents were found for the dichloromethane, obtained both by Soxhlet and maceration extraction and hydroethanolic extracts. The HRESI-MS demonstrated the presence of arctigenin, quercetin, chlorogenic acid and caffeic acid compounds, which were identified by comparison with previous data. The dichloromethane extracts were the only extracts that exhibited activity against cancer cell lines, especially for K562, MCF-7 and 786-0 cell lines. Conclusions The hydroethanolic extracts exhibited the strongest free radical scavenging activity, while the highest phenolic content was observed in Soxhlet extraction. Moreover, the dichloromethanic extracts showed selective antiproliferative activity against K562, MCF-7 and 786-0 human cancer cell lines.

2011-01-01

281

Immunolocalization of protease-activated receptor-2 in skin: receptor activation stimulates interleukin-8 secretion by keratinocytes in vitro.  

PubMed Central

The protease-activated receptor-2 (PAR-2) is a seven transmembrane domain receptor related to the thrombin receptor, which is activated in vitro by cleavage by trypsin. Affinity-purified rabbit IgG raised against a peptide corresponding to the trypsin cleavage site of PAR-2 was used for an immunohistochemical study of skin. The expression of PAR-2 in epidermis was striking, with keratinocytes showing abundant intercellular and cytoplasmic staining. Basal cells showed the strongest staining intensity and the stratum corneum was negative. Staining with control IgG used at the same concentration was consistently negative. The functional expression of PAR-2 by the simian virus transformed human skin keratinocyte cell line SVK14 was demonstrated by Northern blot analysis, flow cytometric analysis and the measurement of intracellular calcium. Treatment of SVK14 with trypsin or a receptor agonist peptide (SLIGKV-NH2) caused a dose-dependent increase in the secretion of the chemokine interleukin-8 (IL-8) in vitro. The effect of the peptide was specific, since control acetylated peptide was without activity. We conclude that PAR-2 is highly expressed by epidermal keratinocytes and receptor activation in vitro leads to increased IL-8 secretion by keratinocytes. These data raise the possibility that PAR-2 may play a role in epidermal homeostasis and inflammatory conditions. Images Figure 2 Figure 3 Figure 5

Hou, L; Kapas, S; Cruchley, A T; Macey, M G; Harriott, P; Chinni, C; Stone, S R; Howells, G L

1998-01-01

282

Immunolocalization of protease-activated receptor-2 in skin: receptor activation stimulates interleukin-8 secretion by keratinocytes in vitro.  

PubMed

The protease-activated receptor-2 (PAR-2) is a seven transmembrane domain receptor related to the thrombin receptor, which is activated in vitro by cleavage by trypsin. Affinity-purified rabbit IgG raised against a peptide corresponding to the trypsin cleavage site of PAR-2 was used for an immunohistochemical study of skin. The expression of PAR-2 in epidermis was striking, with keratinocytes showing abundant intercellular and cytoplasmic staining. Basal cells showed the strongest staining intensity and the stratum corneum was negative. Staining with control IgG used at the same concentration was consistently negative. The functional expression of PAR-2 by the simian virus transformed human skin keratinocyte cell line SVK14 was demonstrated by Northern blot analysis, flow cytometric analysis and the measurement of intracellular calcium. Treatment of SVK14 with trypsin or a receptor agonist peptide (SLIGKV-NH2) caused a dose-dependent increase in the secretion of the chemokine interleukin-8 (IL-8) in vitro. The effect of the peptide was specific, since control acetylated peptide was without activity. We conclude that PAR-2 is highly expressed by epidermal keratinocytes and receptor activation in vitro leads to increased IL-8 secretion by keratinocytes. These data raise the possibility that PAR-2 may play a role in epidermal homeostasis and inflammatory conditions. PMID:9767417

Hou, L; Kapas, S; Cruchley, A T; Macey, M G; Harriott, P; Chinni, C; Stone, S R; Howells, G L

1998-07-01

283

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

PubMed

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

Wiegand, Cornelia; Hipler, Uta-Christina

2013-10-01

284

Evaluation of potential endocrine activity of 2,4-dichlorophenoxyacetic acid using in vitro assays.  

PubMed

The herbicide 2,4-dichlorophenoxyacetic acid (2,4-D) was evaluated in five in vitro screening assays to assess the potential for interaction with the androgen, estrogen and steroidogenesis pathways in the endocrine system. The assays were conducted to meet the requirements of the in vitro component of Tier 1 of the United States Environmental Protection Agency's Endocrine Disruptor Screening Program (EDSP), and included assays for estrogen receptor (ER) binding (rat uterine cytosol ER binding assay), ER-mediated transcriptional activation (HeLa-9903-ER? transactivation assay), androgen receptor (AR) binding (rat prostate cytosol AR binding assay), aromatase enzymatic activity inhibition (recombinant human CYP19 aromatase inhibition assay), and interference with steroidogenesis (H295R steroidogenesis assay). Results from these five assays demonstrated that 2,4-D does not have the potential to interact in vitro with the estrogen, androgen, or steroidogenesis pathways. These in vitro data are consistent with a corresponding lack of endocrine effects observed in apical in vivo animal studies, and thus provide important supporting data valuable in a comprehensive weight of evidence evaluation indicating a low potential of 2,4-D to interact with the endocrine system. PMID:24815817

Coady, Katherine K; Lynn Kan, H; Schisler, Melissa R; Bhaskar Gollapudi, B; Neal, Barbara; Williams, Amy; LeBaron, Matthew J

2014-08-01

285

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

286

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

PubMed Central

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

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

2011-01-01

287

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

PubMed

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

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

2011-09-01

288

In vitro and in vivo Antiinflammatory Activity of Clerodendrum paniculatum Linn. Leaves.  

PubMed

Preliminary phytochemical screening showed the presence of terpenes, flavonoids, tannins, alkaloids, phenolic acid, sterols, and glycosides. This study was intended to evaluate the antiinflammatory activity of various extracts of fresh leaves of Clerodendrum paniculatum Linn experimentally by in vitro (human red blood cell membrane stabilization method) and in vivo methods (0.1 ml of 1% w/v carrageenan-induced rat paw oedema model). Petroleum ether, chloroform, ethyl acetate, alcohol, and aqueous extracts were screened for in vitro antiinflammatory activity. Petroleum ether and chloroform extracts which showed, best in vitro antiinflammatory activity was screened for in vivo antiinflammatory activity at the dose level of 200 and 400 mg/kg. Indomethacin at the dose level of 10 mg/kg was used as reference standard drug. Both the extracts showed a dose dependent significant (P<0.001) reduction in paw edema when compared to the control, at all the time intervals and comparable to indomethacin (reference standard) treated group. The results of the present study demonstrate that petroleum ether and chloroform extracts possess significant (P<0.001) antiinflammatory potential which provide scientific basis for the traditional claims of Clerodendrum paniculatum Linn leaves as an antiinflammatory drug. PMID:24082358

Joseph, Jeenu; Bindhu, A R; Aleykutty, N A

2013-05-01

289

Antimalarial acridines: synthesis, in vitro activity against P. falciparum and interaction with hematin.  

PubMed

A series of acridine derivatives were synthesised and their in vitro antimalarial activity was evaluated against one chloroquine-susceptible strain (3D7) and three chloroquine-resistant strains (W2, Bre1 and FCR3) of Plasmodium falciparum. Structure-activity relationship showed that two positives charges as well as 6-chloro and 2-methoxy substituents on the acridine ring were required to exert a good antimalarial activity. The best compounds possessing these features inhibited the growth of the chloroquine-susceptible strain with an IC(50)0.07 microM, close to that of chloroquine itself, and that of the three chloroquine-resistant strains better than chloroquine with IC(50)0.3 microM. These acridine derivatives inhibited the formation of beta-hematin, suggesting that, like CQ, they act on the haem crystallization process. Finally, in vitro cytotoxicity was also evaluated upon human KB cells, which showed that one of them 9-(6-ammonioethylamino)-6-chloro-2-methoxyacridinium dichloride 1 displayed a promising antimalarial activity in vitro with a quite good selectivity index versus mammalian cell on the CQ-susceptible strain and promising selectivity on other strains. PMID:19879150

Guetzoyan, Lucie; Yu, Xiao-Min; Ramiandrasoa, Florence; Pethe, Stéphanie; Rogier, Christophe; Pradines, Bruno; Cresteil, Thierry; Perrée-Fauvet, Martine; Mahy, Jean-Pierre

2009-12-01

290

In vitro anti-influenza viral activities of constituents from Caesalpinia sappan.  

PubMed

Six constituents with neuraminidase (NA) inhibitory activity, namely brazilein, brazilin, protosappanin A, 3-deoxysappanchalcone, sappanchalcone and rhamnetin, were isolated from the hearthwood of Caesalpinia sappan (Leguminosae). Their in vitro anti-influenza virus activities were evaluated with the cytopathic effect (CPE) reduction method. The results showed that 3-deoxysappanchalcone and sappanchalcone exhibited the highest activity against influenza virus (H3N2) with IC50 values of 1.06 and 2.06 microg/mL, respectively, in comparison to the positive control oseltamivir acid and ribavirin with IC50 values of 0.065 and 9.17 microg/mL, respectively. PMID:19148862

Liu, Ai-Lin; Shu, Shi-Hui; Qin, Hai-Lin; Lee, Simon Ming Yuen; Wang, Yi-Tao; Du, Guan-Hua

2009-03-01

291

Synthesis, spectral characterization and in vitro antimicrobial activity of some new azopyridine derivatives  

NASA Astrophysics Data System (ADS)

A series of arylpicolino and/or isonicotinohydrazonyl cyanide 2a-d and 4a-f were prepared by coupling the approprite aryl diazonium salt with 2-cyanomethyl and/or 4-cyanomethyl-pyridine, respectively. These compounds were characterized by analytical and spectral analyses and screened for their antibacterial activity against Gram-positive bacteria, Gram-negative bacteria and antifungal activity. Among the synthesized compounds, N'-(4-phenyldiazenyl)phenylisonicotinohydrazonyl cyanide 4f showed a significant activity toward both Gram-positive, Gram-negative bacteria and exhibit the most potent in vitro antifungal with MIC's (625 ?g/mL) against Aspergillus nieger.

Abuo-Melha, Hanaa; Fadda, A. A.

2012-04-01

292

Butirosin, a New Aminoglycosidic Antibiotic Complex: Antibacterial Activity In Vitro and in Mice  

PubMed Central

Butirosin is a new aminoglycosidic antibiotic complex which has broad gram-negative and gram-positive inhibitory antibacterial activity, as well as some bactericidal properties. Significantly susceptible bacteria include strains of Staphylococcus aureus and Streptococcus pyogenes, and pathogenic gram-negative species such as Enterobacter aerogenes, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and P. vulgaris, Salmonella enteritidis and S. typhimurium, Shigella flexneri and S. sonnei. Good activity by parenteral dosing was obtained in various acute mouse infections. Butirosin is especially interesting because of its activity against Pseudomonas aeruginosa in vitro, including gentamicin-resistant clinical isolates, and in experimental mouse infections at relatively low doses.

Heifetz, C. L.; Fisher, M. W.; Chodubski, J. A.; DeCarlo, M. O'.

1972-01-01

293

Telbivudine Exhibits No Inhibitory Activity against HIV-1 Clinical Isolates In Vitro?  

PubMed Central

Most approved drugs with activity against hepatitis B virus (HBV) have activity against human immunodeficiency virus type 1 (HIV-1), which precludes their use in patients who are coinfected with HBV and HIV-1 and who are not receiving antiretroviral therapy due to the risk of inducing resistance. The activity of telbivudine, a highly selective HBV inhibitor, against temporally and geographically distinct wild-type and multidrug-resistant HIV-1 clinical isolates was evaluated in vitro. No inhibition was observed with up to 600 ?M drug, which supports further exploration of telbivudine as a therapeutic option for the treatment of HBV infections in patients coinfected with HIV-1.

Lin, Kai; Karwowska, Sylwia; Lam, Eric; Limoli, Kay; Evans, Thomas G.; Avila, Claudio

2010-01-01

294

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

PubMed

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

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

2013-07-01

295

Evaluation of in vitro antifungal activity of N-benzylsalicylamide derivatives.  

PubMed

A series of 65 derivatives of N-benzylsalicylamide was tested against eight potentially human pathogenic fungi by microdilution broth method modified according to M27-A standard. The majority of these compounds showed only weak in vitro antifungal activity. The most significant effect was observed against filamentous fungi Trichophyton mentagrophytes, Absidia corymbifera, and Aspergillus fumigatus while yeasts, in general, were less susceptible. N-(4'-Chlorobenzyl) salicylamides, N-(3',4'-dichlorobenzyl)-salicylamides, and partially N-benzylsalicylamides exhibited relatively high in vitro antifungal activity. The most efficient derivatives had MIC < or = 7.8 mumol/L against T. mentagrophytes. Regression analysis suggested an indirect relationship between MIC values and lipophilicity (log P). PMID:12879744

Kubanová, P; Buchta, V; Perina, M; Waisser, K; Pour, M

2003-01-01

296

Enhanced in vitro activity of WR99210 in combination with dapsone against Mycobacterium avium complex.  

PubMed

WR99210, a dihydrofolate reductase inhibitor, has promising in vitro activity against Mycobacterium avium complex (MAC). The in vitro activities of WR99210 alone and in combination with a fixed concentration of dapsone (0.5 microgram/ml) were evaluated against 35 clinical MAC isolates by a broth dilution method. The MIC at which 50% of isolates were inhibited (MIC50) and MIC90 of WR99210 alone were 2 and 8 micrograms/ml, respectively. The MIC50 and MIC90 of WR99210 in combination with dapsone were 0.25 and 4 micrograms/ml, respectively. Overall, 75% of the MAC isolates displayed enhanced susceptibility to the combination. PMID:8913480

Shah, L M; DeStefano, M S; Cynamon, M H

1996-11-01

297

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

298

The mariner Mos1 transposase produced in tobacco is active in vitro.  

PubMed

The mariner-like transposon Mos1 is used for insertional mutagenesis and transgenesis in different animals (insects, nematodes), but has never been used in plants. In this paper, the transposition activity of Mos1 was tested in Nicotiana tabacum, but no transposition event was detected. In an attempt to understand the absence of in planta transposition, Mos1 transposase (MOS1) was produced and purified from transgenic tobacco (HMNtMOS1). HMNtMOS1 was able to perform all transposition reaction steps in vitro: binding to ITR, excision and integration of the same pseudo-transposon used in in planta transposition assays. The in vitro transposition reaction was not inhibited by tobacco nuclear proteins, and did not depend on the temperature used for plant growth. Several hypotheses are proposed that could explain the inhibition of HMNtMOS1 activity in planta. PMID:19847655

Thomas, Xavier; Hedhili, Sabah; Beuf, Laurent; Demattéi, Marie-Véronique; Laparra, Hélčne; Khong, Giang Ngan; Breitler, Jean-Christophe; Montandon, Frédéric; Carnus, Elodie; Norre, Frédéric; Burtin, Daniel; Gantet, Pascal; Bigot, Yves; Renault, Sylvaine

2010-05-01

299

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

300

In Vitro and In Vivo Antifungal Activities of T-2307, a Novel Arylamidine?  

PubMed Central

The in vitro and in vivo antifungal activities of T-2307, a novel arylamidine, were evaluated and compared with those of fluconazole, voriconazole, micafungin, and amphotericin B. T-2307 exhibited broad-spectrum activity against clinically significant pathogens, including Candida species (MIC range, 0.00025 to 0.0078 ?g/ml), Cryptococcus neoformans (MIC range, 0.0039 to 0.0625 ?g/ml), and Aspergillus species (MIC range, 0.0156 to 4 ?g/ml). Furthermore, T-2307 exhibited potent activity against fluconazole-resistant and fluconazole-susceptible-dose-dependent Candida albicans strains as well as against azole-susceptible strains. T-2307 exhibited fungicidal activity against some Candida and Aspergillus species and against Cryptococcus neoformans. In mouse models of disseminated candidiasis, cryptococcosis, and aspergillosis, the 50% effective doses of T-2307 were 0.00755, 0.117, and 0.391 mg·kg?1·dose?1, respectively. This agent was considerably more active than micafungin and amphotericin B against candidiasis and than amphotericin B against cryptococcosis, and its activity was comparable to the activities of micafungin and amphotericin B against aspergillosis. The results of preclinical in vitro and in vivo evaluations performed thus far indicate that T-2307 could represent a potent injectable agent for the treatment of candidiasis, cryptococcosis, and aspergillosis.

Mitsuyama, Junichi; Nomura, Nobuhiko; Hashimoto, Kyoko; Yamada, Eio; Nishikawa, Hiroshi; Kaeriyama, Makoto; Kimura, Akiko; Todo, Yozo; Narita, Hirokazu

2008-01-01

301

Cadmium restores in vitro splicing activity inhibited by zinc-depletion.  

PubMed

Zinc (Zn)-depletion inhibits the second step of RNA splicing, namely exon-ligation. To investigate the effects of cadmium (Cd) and other metal ions on RNA splicing inhibited by Zn-depletion, we measured in vitro splicing activities in the presence of these metals. Zn-depletion in the splicing reaction mixture was achieved by addition of a Zn-chelator, 1,10-phenanthroline. Cd(II) at 1, 5 and 10 microM restored the splicing activity to 2, 24 and 72% of that in the control reaction mixture, while higher concentrations of Cd(II) decreased the splicing activity, and more than 50 microM Cd(II) showed a complete absence of spliced products. Hg(II) also restored the splicing activity, albeit to a lesser extent, since 5 and 10 microM Hg(II) restored the splicing activity to 3 and 4% of the control value. The other metal ions examined in this study, Co(II), Cu(II), Mg(II) and Mn(II), did not show any restoration of the splicing activity. We concluded that Cd(II) could restore the in vitro splicing activity inhibited by Zn-depletion, although higher concentrations of Cd(II) prevented progress of the RNA splicing reaction. These results suggest that Cd(II) has a bifunctional property regarding RNA splicing, and is stimulatory at low concentrations and inhibitory at high concentrations. PMID:16645842

Lee, Myeong Jin; Ayaki, Hitoshi; Goji, Junko; Kitamura, Keiko; Nishio, Hisahide

2006-10-01

302

Characterization of VIP1 activity as a transcriptional regulator in vitro and in planta  

PubMed Central

VIP1 (VirE2 interacting protein 1), initially discovered as a host protein involved in Agrobacterium-plant cell DNA transfer, is a transcription factor of the basic leucine-zipper (bZIP) domain family that regulates several defence-related genes in Arabidopsis. We have developed assays to assess VIP1 binding to its DNA target in vitro and transcriptional activation efficiency in planta. Several point mutations in the VIP1 response element VRE affected the VIP1 activity, and a strong correlation between VIP1-VRE binding and transcriptional activation levels was observed. Promoter activation by VIP1 was influenced by bacterial and plant proteins known to interact with VIP1 during Agrobacterium infection, i.e., VirE2, VirF and VIP2. VirF, an F-box protein, strongly decreased VIP1 transcriptional activation ability, but not its binding to VRE in vitro, most likely by triggering proteasomal degradation of VIP1. Finally, activation of a VRE-containing promoter was observed in dividing cells, probably resulting from activation of endogenous VIP1.

Lacroix, Benoit; Citovsky, Vitaly

2013-01-01

303

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

304

Endogenous activation of nicotinic receptors underlies sympathetic tone generation in neonatal rat spinal cord in vitro.  

PubMed

Without the brainstem, thoracic spinal cords of neonatal rats in vitro spontaneously generate tonic sympathetic nerve discharge (SND) in the splanchnic nerves. Activation of nicotinic receptors in cords is known to alter a repertoire of neurotransmitter releases to sympathetic preganglionic neurons (SPNs). Using in vitro nerve-cord preparations, we investigated whether endogenous nicotinic receptor activity is essential for SND genesis. Application of mecamylamine, an open-channel nicotinic receptor blocker, reduced SND in a progressive manner. Exogenous activation of nicotinic receptors by application of various nicotinic agonists generally excited SND at low agonistic concentrations. At higher concentrations, however, agonists induced biphasic responses characterized by an initial excitation followed by prolonged SND suppression. Whether ionotropic glutamate, GABA(A), or glycine receptors are downstream signals of nicotinic receptor activation was explored by pretreatment of cords with selective antagonists. The initial excitation of SND persisted in the presence of ionotropic glutamate receptor antagonists. In contrast, the SND suppression was partially reversed by glycine or GABA(A) receptor antagonists. Incubation of the cord in a low Ca(2+)/high Mg(2+) bath solution to block Ca(2+)-dependent synaptic transmission did not affect SND excitation induced by nicotinic agonists, confirming direct activation of postsynaptic nicotinic receptors on SPNs. In conclusion, the endogenous activity of nicotinic receptors is essential for SND genesis in the thoracic spinal cord. Nicotinic activation of glycinergic and GABAergic interneurons may provide a recurrent inhibition of SPNs for homeostatic regulation of sympathetic outflow. PMID:16904709

Chen, Hsin-Kai; Su, Chun-Kuei

2006-12-01

305

Comparative in vitro activities of ertapenem against bacterial pathogens from patients with acute pelvic infection  

Microsoft Academic Search

This study compared the in vitro activities of ertapenem, ceftriaxone, co-amoxiclav, cipro- floxacin and piperacillin-tazobactam against 314 aerobic bacteria and of ertapenem, piperacillin-tazobactam, cefoxitin, ceftriaxone, chloramphenicol, ticarcillin-clavulanate, ampicillin-sulbactam, clindamycin and metronidazole against 500 anaerobic bacteria from 212 patients with acute pelvic infection. Antimicrobial susceptibilities were determined by broth microdilution (aerobes) or agar dilution (anaerobes), following NCCLS guidelines. The most common

Barbara A. Pelak; Diane M. Citron; Mary Motyl; Ellie J. C. Goldstein; Gail L. Woods; Hedy Teppler

306

Peroxide-supported in-vitro cytochrome P450 activities in Haemonchus contortus  

Microsoft Academic Search

The potential for cytochrome P450 from Haemonchus contortus to operate in the oxygen-poor intestinal environment was investigated by examining the ability of the cytochrome to act in vitro as a peroxygenase in utilising cumene hydroperoxide for substrate oxidations not requiring molecular oxygen. Peroxygenase and NADPH-supported monooxygenase activities were measured in microsomes prepared from L3 and adult nematodes. Both cumene hydroperoxide-

A. C Kotze

1999-01-01

307

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

308

Antioxidant activity of ethanolic extract of inflorescence of Ormenis Africana in vitro and in cell cultures  

Microsoft Academic Search

Background  The antioxidant potency of the hydroethanolic extract of Ormenis Africana (HEOA), Asteraceae was evaluated with regards to total polyphenol, flavonoid and anthocyanins content. Antioxidant activity\\u000a has been assessed chemically and biologically. First, the free radical scavenging ability of HEOA was evaluated using two\\u000a commonly in vitro tests: ABTS and DPPH radicals. Then, the protection effect of this extract against oxidative

Riadh Ben Mansour; Bochra Gargouri; Mohamed Bouaziz; Nésrine Elloumi; Imtinčne Belhadj Jilani; Zaineb Ghrabi; Saloua Lassoued

2011-01-01

309

Effects of halogenated benzenes on arylesterase activity in vivo and in vitro.  

PubMed

Hepatic arylesterase activity was induced by 1,2,4-trichlorobenzene, hexachlorobenzene, 1,2,4-tribromobenzene, and 1,3,5-tribromobenzene but not by 1,3,5-trichlorobenzene or hexabromobenzene. Serum arylesterase was not induced by any of the halogenated benzenes and was inhibited in vivo by 1,2,4-trichlorobenzene, hexachlorobenzene, and 1,3,5-tribromobenzene. It was also inhibited in vitro. PMID:7444163

Carlson, G P

1980-11-01

310

In Vitro and In Vivo Activities of a New Cephalosporin, FR264205, against Pseudomonas aeruginosa  

Microsoft Academic Search

FR264205 is a novel parenteral 3-aminopyrazolium cephalosporin. This study evaluated the in vitro and in vivo activities of FR264205 against Pseudomonas aeruginosa. The MIC of FR264205 at which 90% of 193 clinical isolates of P. aeruginosa were inhibited was 1 g\\/ml, 8- to 16-fold lower than those of ceftazidime (CAZ), imipenem (IPM), and ciprofloxacin (CIP). FR264205 also exhibited this level

Shinobu Takeda; Toru Nakai; Yoshimi Wakai; Fumiaki Ikeda; Kazuo Hatano

2007-01-01

311

14-3-3 Facilitates Ras-Dependent Raf1 Activation In Vitro and In Vivo  

Microsoft Academic Search

14-3-3 proteins complex with many signaling molecules, including the Raf-1 kinase. However, the role of 14-3-3 in regulating Raf-1 activity is unclear. We show here that 14-3-3 is bound to Raf-1 in the cytosol but is totally displaced when Raf-1 is recruited to the plasma membrane by oncogenic mutant Ras, in vitro and in vivo. 14-3-3 is also displaced when

SANDRINE ROY; ROBERT A. MCPHERSON; ANN APOLLONI; JUN YAN; JODI CLYDE-SMITH; JOHN F. HANCOCK

1998-01-01

312

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

313

In Vitro Activities of SCH27899 Alone and in Combination with 17 Other Antimicrobial Agents  

PubMed Central

SCH27899, an everninomicin antibiotic, was tested for its in vitro activity against 718 bacterial isolates representing 27 species. The Enterobacteriaceae and nonenteric gram-negative bacilli were resistant to ?8.0 ?g/ml, but all others were inhibited by ?1.0 ?g/ml. When tested in combination with 17 other antimicrobial agents against 110 strains, SCH27899 demonstrated no significant antagonism or synergy. Consequently, combination therapy is not contraindicated.

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

1999-01-01

314

In Vitro Activity of ABT 773, a New Ketolide Antibiotic, against Chlamydia pneumoniae  

Microsoft Academic Search

The in vitro activities of ABT 773, telithromycin (HMR 3647), azithromycin, clarithromycin, erythromycin, and levofloxacin were tested against 20 strains of Chlamydia pneumoniae. The MIC at which 90% of the isolates were inhibited and the minimal bactericidal concentration at which 90% of the isolates were killed by ABT 773 were 0.015 mg\\/ml (range, 0.008 to 0.015 mg\\/ml). ABT 773 was

SEBASTIAN STRIGL; PATRICIA M. ROBLIN; TAMARA REZNIK; M. R. Hammerschlag

2000-01-01

315

In vitro antimicrobial activity of extracts and compounds of some selected medicinal plants from Cameroon  

Microsoft Academic Search

Aim of the studySeven extracts and eight compounds from four selected Cameroonian medicinal plants, Solanecio mannii Hook f. (Asteraceae), Monodora myristica Dunal (Annonaceae), Albizia gummifera (J.F. Gmel) C.A. Smith (Fabaceae\\/Mimosoideae) and Glyphaea brevis (Spreng) Monachino (Tiliaceae), traditionally used for the treatment of hepatitis, parasites and other infectious diseases, were tested in vitro for their antimicrobial activity against Gram-positive (5 species)

Emmanuel Jean Teinkela Mbosso; Silvčre Ngouela; Jules Clément Assob Nguedia; Véronique Penlap Beng; Michel Rohmer; Etienne Tsamo

2010-01-01

316

Issues Arising When Interpreting Results from an in Vitro Assay for Estrogenic Activity  

Microsoft Academic Search

Concern about possible adverse effects caused by the inadvertent exposure of humans and wildlife to endocrine-active chemicals, has led some countries to develop an in vivo–in vitro screening program for endocrine effects. In this paper, a previously described estrogen-inducible recombinant yeast strain (Saccharomyces cerevisiae) is used to investigate a number of issues that could potentially lead to the mislabeling of

N. Beresford; E. J. Routledge; C. A. Harris; J. P. Sumpter

2000-01-01

317

Potent Biphalin Analogs with µ/? Mixed Opioid Activity: In Vivo and In Vitro Biological Evaluation.  

PubMed

Biphalin [(Tyr-D-Ala-Gly-Phe-NH-)2 ] is an octapeptide with mixed ?/? opioid activity. Its structure is based on two identical enkephalin-like portions linked "tail-to-tail" by a hydrazine bridge. This study presents the synthesis and in vitro and in vivo bioassays of two biphalin analogs that do not present the toxicity connected with the presence of the hydrazine moiety and are able to elicit a higher antinociceptive effect than biphalin. PMID:24798820

Costante, Roberto; Pinnen, Francesco; Stefanucci, Azzurra; Mollica, Adriano

2014-05-01

318

In Vitro Activities of Three Nonfluorinated Quinolones against Representative Bacterial Isolates  

Microsoft Academic Search

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 cipro- floxacin, 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-resis- tant, methicillin-resistant Staphylococcus aureus strains were inhibited

ARTHUR L. BARRY; PETER C. FUCHS; STEVEN D. BROWN

2001-01-01

319

In vitro antimicrobial activity of the leaf essential oil of Spiraea alpina Pall  

Microsoft Academic Search

The qualitative and quantitive determination of chemical components of leaf essential oil of Spiraea alpina Pall. with Microwave-assisted Hydrodistillation is carried out by gas chromatography-mass spectrometry. About 69 compounds\\u000a have been identified from the leaf oil, accounting for 79.39% of the total. The in vitro antifungal activity of S. alpina essential oil was studied against eight test phytopathogenic bacteria and

Yun Teng; Qian Yang; Zhiyi Yu; Guoping Zhou; Qiu Sun; Hong Jin; Taiping Hou

2010-01-01

320

In Vitro Homocysteine Inhibits Platelet Na + , K + ATPase and Serum Butyrylcholinesterase Activities of Young Rats  

Microsoft Academic Search

Homocystinuria is an inborn error of sulphur amino acid metabolism, resulting in accumulation of tissue homocysteine. This disease is characterized predominantly by vascular and nervous system dysfunction. In the present study we investigated the in vitro effects of homocysteine, the main metabolite accumulated in homocystinuria, on platelet Na+,K+-ATPase and serum butyrylcholinesterase (BuChE) activities of young rats. Platelet and serum of

Francieli M. Stefanello; Renata Franzon; Clovis M. D. Wannmacher; Moacir Wajner; Angela T. S. Wyse

2003-01-01

321

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

Microsoft Academic Search

The in vitro activity of the fluoroquinolone BAY 12-8039 against 66 strains of different mycoplasma species and 30 strains of Ureaplasma urealyticum was compared with those of three other antimicrobial agents. BAY 12-8039 at 0.5 mg\\/ml inhibited 100% of all the mycoplasmal and ureaplasmal strains tested. The minimal bactericidal concentrations of BAY 12-8039 increased only two- to eightfold compared to

C. M. BEBEAR; H. RENAUDIN; A. BOUDJADJA; Universitede Bordeaux; Bayer Pharma

1998-01-01

322

Some flame retardants and the antimicrobials triclosan and triclocarban enhance the androgenic activity in vitro  

Microsoft Academic Search

Contaminants including flame retardants, antimicrobial agents and phthalates, occurring as residues in human tissues were associated with altered endocrine function. In our study we analysed the flame retardants tetrabromobisphenol A (TBBPA), hexabromocyclodecane (HBCD), penta-bromodiphenylether (BDE-100) and hexa-BDE (BDE-155), the antimicrobial compounds triclosan (TCS) and triclocarban (TCC) and eight phthalates for their androgenic and antiandrogenic activity in vitro in the MDA-kb2

Verena Christen; Pierre Crettaz; Aurelia Oberli-Schrämmli; Karl Fent

323

Application of modified in vitro screening procedure for identifying herbals possessing sulfonylurea-like activity  

Microsoft Academic Search

We describe here the application of a modified in vitro procedure for identifying herbs potentially possessing sulfonylurea-like activity. The procedure consists of the combination of an SUR1 receptor binding assay and an insulin secretion assay in cultures of HIT-T15 cells. This procedure could be used as an initial step in identifying new safe and efficacious agents for the management of

Y Rotshteyn; S. W Zito

2004-01-01

324

In vitro Antimicrobial Activity of the Volatile Oil of Nigella Sativa Linn Seeds  

Microsoft Academic Search

The in-vitro antimicrobial activity of the Volatile oils of Nigella Sativa Linn Seeds was tested against fifteen pathogenic microbial strains includung three gram-positive, eleven gram- negative and a yeast Candida albicans. The volatile oil showed strong sensitivity to all the organisms. The zone of inhibition was found 13-32mm at a dose of 600µg\\/disc. Minimum inhibitory concentration (MIC) of the volatile

Nazma Ara; S A R Choudhury; Ruhul Amin

2005-01-01

325

In vitro antioxidant activity and total phenolic content of ethanolic leaf extract of Stevia rebaudiana Bert  

Microsoft Academic Search

The aim of this study was to assess the in vitro potential of ethanolic leaf extract of Stevia rebaudiana as a natural antioxidant. The DPPH activity of the extract (20, 40, 50, 100 and 200?g\\/ml) was increased in a dose dependent manner, which was found in the range of 36.93–68.76% as compared to ascorbic acid 64.26–82.58%. The IC50 values of

Shruti Shukla; Archana Mehta; Vivek K. Bajpai; Savita Shukla

2009-01-01

326

Purification and in vitro activities of the Bacillus subtilis TnrA transcription factor.  

PubMed

The Bacillus subtilis nitrogen regulatory protein TnrA was purified and its interaction with the nrgAB regulatory region examined. The TnrA protein activates transcription from the nrgAB promoter in vitro. DNase I footprinting and methylation protection experiments demonstrated that TnrA binds to an inverted repeat, upstream of the -35 region of the nrgAB promoter. Gel mobility retardation assays were used to determine the affinity of TnrA for its DNA-binding site. The equilibrium dissociation binding constant for the interaction of TnrA with the nrgAB promoter fragment was 7.7 nM under the conditions used here. Mutations in the TnrA consensus sequence that reduce nrgAB expression in vivo were found to reduce significantly the in vitro affinity for TnrA. An A+T rich region located upstream of the TnrA-binding site was found to be necessary for optimal transcriptional activation. A mutant protein, TnrA(HTH), was constructed in which the putative helix-turn-helix DNA-binding motif was altered by exchanging two arginine residues for alanine residues. The TnrA(HTH) protein was unable to activate the in vivo expression of nrgAB and had an in vitro affinity for the nrgAB promoter that was significantly lower than that of the wild-type protein. PMID:10864496

Wray, L V; Zalieckas, J M; Fisher, S H

2000-06-30

327

Direct Evaluation of L-DOPA Actions on Neuronal Activity of Parkinsonian Tissue In Vitro  

PubMed Central

Physiological and biochemical experiments in vivo and in vitro have explored striatal receptor signaling and neuronal excitability to posit pathophysiological models of Parkinson's disease. However, when therapeutic approaches, such as dopamine agonists, need to be evaluated, behavioral tests using animal models of Parkinson's disease are employed. To our knowledge, recordings of population neuronal activity in vitro to assess anti-Parkinsonian drugs and the correlation of circuit dynamics with disease state have only recently been attempted. We have shown that Parkinsonian pathological activity of neuronal striatal circuits can be characterized in in vitro cerebral tissue. Here, we show that calcium imaging techniques, capable of recording dozens of neurons simultaneously with single-cell resolution, can be extended to assess the action of therapeutic drugs. We used L-DOPA as a prototypical anti-Parkinsonian drug to show the efficiency of this proposed bioassay. In a rodent model of early Parkinson's disease, Parkinsonian neuronal activity can be returned to control levels by the bath addition of L-DOPA in a reversible way. This result raises the possibility to use calcium imaging techniques to measure, quantitatively, the actions of anti-Parkinsonian drugs over time and to obtain correlations with disease evolution and behavior.

Plata, Victor; Perez-Ortega, Jesus E.; Galarraga, Elvira; Bargas, Jose

2013-01-01

328

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

PubMed Central

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

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

2011-01-01

329

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

NASA Astrophysics Data System (ADS)

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

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

2010-10-01

330

In vitro and in vivo evaluation of ribavirin and pleconaril antiviral activity against enterovirus 71 infection.  

PubMed

Enterovirus 71(EV71) causes recurring outbreaks of hand, foot and mouth disease and encephalitis leading to complications or death in young children. More effective antiviral drugs are needed to prevent or reduce EV71-related disease and complications. However, there are no standard models currently in use to evaluate activity against EV71 infection both in vitro and in vivo. In this study, the activity of ribavirin and pleconaril against EV71 infection was evaluated in two models. An in vitro EV71 infection model was developed in RD cells, and an in vivo EV71 infection model was applied. Ribavirin and pleconaril effectively increased the viability of infected cells. Pleconaril reduced the morbidity and mortality of one-day-old infected mice, but ribavirin did not protect the infected mice. In all, the results demonstrated that infected cells and infected mice can be used to evaluate antiviral activity of ribavirin and pleconaril against EV71 infection in vitro and in vivo. PMID:22245989

Zhang, Guofeng; Zhou, Feng; Gu, Bin; Ding, Chuanling; Feng, Dongju; Xie, Fangyi; Wang, Jinfeng; Zhang, Chun; Cao, Qingxian; Deng, Yinlai; Hu, Weixing; Yao, Kun

2012-04-01

331

[In vitro activity of cefepime against ESBL-positive clinical strains of gram-negative rods].  

PubMed

The aim of this study was to determine an in vitro activity of cefepime against ESBL-positive clinical strains of Gram-negative rods isolated from hospitalized patients. Experiments were performed with 100 ESBL-positive strains of Gram-negative rods isolated from clinical samples in 2004. Strains were identified with the use of automatic ATB Expression system and biochemical ID 32 GN tests (bioMdrieux sa). Extended-spectrum beta-lactamases (ESBLs) were detected by means of disc diffusion methods: the double-disc synergy test (DDST) and the diagnostic disc test (DD, Oxoid Ltd, UK). Susceptibility in vitro of ESBL producers to 4th generation--cefepime was determined with gradient diffusion method Etest (AB Biodisk, Solna, Sweden). MIC value of cefepime was assessed for each strain. Among 100 ESBL-producing strains, 94--belonged to enteric rods and 6--to nonfermentative rods. The greatest number of strains belonged to the species Serratia marcescens (27% of all strains) and next--to the species Enterobacter cloacae (21%). Fourteen strains were susceptible (S) in vitro to cefepime, 12--intermediately susceptible (I) and 74--resistant (R). Application of cefepime in a therapy of infections caused by ESBL-positive strains of Gram-negative rods highly susceptible in vitro to this antibiotic, should be considered. PMID:16773834

Rokosz, Alicja; Sawicka-Grzelak, Anna; Luczak, Miros?aw

2005-01-01

332

Acaricidal activity of usnic acid and sodium usnic acid against Psoroptes cuniculi in vitro.  

PubMed

Usnic acid, a major active compound in lichens, was first isolated in 1884. Since then, usnic acid and its sodium salt (sodium usnic acid) have been used in medicine, perfumery, cosmetics, and other industries due to its extensive biological activities. However, its acaricidal activity has not been studied. In this paper, we investigated the acaricidal activity of usnic acid and sodium usnic acid against Psoroptes cuniculi in vitro. After evaluating the acaricidal activity and toxicity of usnic acid and sodium usnic acid in vitro, the results showed that at doses of 250, 125, and 62.5 mg/ml, usnic acid and sodium usnic acid can kill mites with 91.67, 85.00, and 55.00 % and 100, 100, and 60.00 % mortality after treatment 24 h. The LT50 values were 4.208, 8.249, and 16.950 h and 3.712, 7.339, and 15.773 h for usnic acid and sodium usnic acid, respectively. Sodium usnic acid has a higher acaricidal activity than usnic acid, which may be related to the difference in their structures. PMID:24770718

Shang, Xiaofei; Miao, Xiaolou; Lv, Huiping; Wang, Dongsheng; Zhang, Jiqin; He, Hua; Yang, Zhiqiang; Pan, Hu

2014-06-01

333

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

PubMed

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

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

2013-04-01

334

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

PubMed Central

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

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

2013-01-01

335

In vitro trypanocidal activities of new S-adenosylmethionine decarboxylase inhibitors.  

PubMed Central

A series of novel aromatic derivatives based on the structure of methylglyoxal bis(guanylhydrazone) (MGBG) was examined for in vitro antitrypanosomal activities and cytotoxicities for human cells. One-third of the compounds tested showed trypanocidal activity at concentrations below 0.5 microM after an incubation period of 72 h. Structure-activity analysis revealed that bicyclic compounds with homocyclic rings and unmodified termini were the most active compounds. Results obtained in three laboratories employing different methods and trypanosome populations consistently ranked compound CGP 40215A highest. This compound had a 50% inhibitory concentration of 0.0045 microM for Trypanosoma brucei rhodesiense, was also active against other trypanosome species, including a multidrug-resistant Trypanosoma brucei brucei, and was significantly less toxic than other compounds tested for a human adenocarcinoma cell line, with a 50% inhibitory concentration of 1.14 mM. The effect of CGP 40215A was time and dose dependent, and low concentrations of the compound required exposure times of > 2 days to exert trypanocidal activity. Compounds were inactive against Leishmania donovani and Trypanosoma cruzi amastigotes in murine macrophages in vitro.

Brun, R; Buhler, Y; Sandmeier, U; Kaminsky, R; Bacchi, C J; Rattendi, D; Lane, S; Croft, S L; Snowdon, D; Yardley, V; Caravatti, G; Frei, J; Stanek, J; Mett, H

1996-01-01

336

Hilar somatostatin interneurons contribute to synchronized GABA activity in an in vitro epilepsy model.  

PubMed

Epilepsy is a disorder characterized by excessive synchronized neural activity. The hippocampus and surrounding temporal lobe structures appear particularly sensitive to epileptiform activity. Somatostatin (SST)-positive interneurons within the hilar region have been suggested to gate hippocampal activity, and therefore may play a crucial role in the dysregulation of hippocampal activity. In this study, we examined SST interneuron activity in the in vitro 4-aminopyridine (4-AP) model of epilepsy. We employed a multi-disciplinary approach, combining extracellular multi-electrode array (MEA) recordings with patch-clamp recordings and optical imaging using a genetically encoded calcium sensor. We observed that hilar SST interneurons are strongly synchronized during 4-AP-induced local field potentials (LFPs), as assayed by Ca(2+) imaging as well as juxtacellular or intracellular recording. SST interneurons were particularly responsive to GABA-mediated LFPs that occurred in the absence of ionotropic glutamatergic transmission. Our results present evidence that the extensive synchronized activity of SST-expressing interneurons contribute to the generation of GABAergic LFPs in an in vitro model of temporal lobe seizures. PMID:24465989

Grosser, Sabine; Queenan, Bridget N; Lalchandani, Rupa R; Vicini, Stefano

2014-01-01

337

Developmental changes in carboxylase activities in in vitro cultured coconut zygotic embryos: comparison with corresponding activities in seedlings  

Microsoft Academic Search

Phosphoenolpyruvate Carboxylase (PEPC; EC: 4.1.1.31) and Ribulose 1,5-bisphosphate Carboxylase\\/Oxygenase (RubisCO; EC: 4.1.1.39)\\u000a enzyme specific activities were measured during the in vitro development of coconut (Cocos nucifera L.) zygotic mature embryos into plantlets and compared with those of palms produced by conventional seed germination. At\\u000a the time of initiation of germination, high PEPC and low RubisCO activities were measured in both

Karine Triques; Alain Rival; Thierry Beulé; Stéphane Dussert; Valérie Hocher; Jean-Luc Verdeil; Serge Hamon

1997-01-01

338

In Vitro Antibacterial Activity of three Indian Spices Against Methicillin-Resistant Staphylococcus aureus  

PubMed Central

Objective To explore the in vitro antibacterial activity of ethanolic extracts of cinnamon (Cinnamomum zeylanicum; CIN), clove (Syzygium aromaticum, CLV) and cumin (Cuminum cyminum, CMN) against clinical isolates of methicillin resistant Staphylococcus aureus (MRSA), from Kolkata, India. Methods The CIN, CLV and CMN were tested for their antibacterial activity against MRSA by in vitro methods. Minimum inhibitory concentration (MIC) values of the three extracts were determined, and time-kill studies were performed in order to investigate the bactericidal activity of the extracts (at the MIC level) for the isolates. The killing efficacy of the extracts was determined at various concentrations. Results The zone diameter of inhibition (ZDI) obtained due to CIN, CLV and CMN ranged between 22-27 mm, 19-23 mm and 9-15 mm, respectively; while the MICs, for the isolates, were in the range of 64-256, 64-512 and 128-512 µg/ml, respectively. When tested for their MIC levels; the CIN and CLV were found to be bactericidal after 6 hrs of incubation, while CMN showed bactericidal activity after 24 hrs. However, when tested at various concentrations; CIN, CLV and CMN displayed bactericidal activity against S. aureus, after 24 hrs of incubation, at 200, 200 and 300 µg/ml, respectively. Conclusion The C. zeylanicum and S. aromaticum showed the strongest in vitro antibacterial activity followed by C. cyminum against MRSA, and such findings could be considered a valuable support in the treatment of infection and may contribute to the development of potential antimicrobial agents for inclusion in anti- S. aureus regimens.

Mandal, Shayamapda; Saha, Krishnendu; Pal, Nishith Kumar

2011-01-01

339

In vitro and in vivo assessment of the anti-malarial activity of Caesalpinia pluviosa  

PubMed Central

Background To overcome the problem of increasing drug resistance, traditional medicines are an important source for potential new anti-malarials. Caesalpinia pluviosa, commonly named "sibipiruna", originates from Brazil and possess multiple therapeutic properties, including anti-malarial activity. Methods Crude extract (CE) was obtained from stem bark by purification using different solvents, resulting in seven fractions. An MTT assay was performed to evaluate cytotoxicity in MCF-7 cells. The CE and its fractions were tested in vitro against chloroquine-sensitive (3D7) and -resistant (S20) strains of Plasmodium falciparum and in vivo in Plasmodium chabaudi-infected mice. In vitro interaction with artesunate and the active C. pluviosa fractions was assessed, and mass spectrometry analyses were conducted. Results At non-toxic concentrations, the 100% ethanolic (F4) and 50% methanolic (F5) fractions possessed significant anti-malarial activity against both 3D7 and S20 strains. Drug interaction assays with artesunate showed a synergistic interaction with the F4. Four days of treatment with this fraction significantly inhibited parasitaemia in mice in a dose-dependent manner. Mass spectrometry analyses revealed the presence of an ion corresponding to m/z 303.0450, suggesting the presence of quercetin. However, a second set of analyses, with a quercetin standard, showed distinct ions of m/z 137 and 153. Conclusions The findings show that the F4 fraction of C. pluviosa exhibits anti-malarial activity in vitro at non-toxic concentrations, which was potentiated in the presence of artesunate. Moreover, this anti-malarial activity was also sustained in vivo after treatment of infected mice. Finally, mass spectrometry analyses suggest that a new compound, most likely an isomer of quercetin, is responsible for the anti-malarial activity of the F4.

2011-01-01

340

Synthesis of novel psoralen analogues and their in vitro antitumor activity.  

PubMed

New tetracyclic benzofurocoumarin (benzopsoralen) analogues were synthesized and their inhibitory effect on the growth of tumor cell lines was evaluated. The human tumor cell lines used were MDA MB231 (breast adenocarcinoma), HeLa (cervix adenocarcinoma) and TCC-SUP (bladder transitional cell carcinoma). The in vitro antitumor activity of the new benzopsoralens was discussed in terms of structure-activity relationship. Molecular docking studies with human-CYP2A6 enzymes were also carried out with the synthesized compounds in order to evaluate the potential of these compounds to interact with the heme group of the enzymes. The results have demonstrated that the linear compounds have the most pronounced activity against tumor cell lines and this might be related to the better accessibility that these compounds have to the active site in relation to the angular ones that have shown in the majority of the cases multiple binding poses in the active site of CYP2A6. PMID:23886808

Francisco, Carla S; Rodrigues, Lígia R; Cerqueira, Nuno M F S A; Oliveira-Campos, Ana M F; Rodrigues, Lígia M; Esteves, Ana P

2013-09-01

341

Comparative in vitro antibacterial activity of sparfloxacin (AT-4140; RP 64206), a new quinolone.  

PubMed Central

The in vitro activity of sparfloxacin (AT-4140; RP 64206), a new fluoroquinolone, was compared with those of 10 other agents against 1,222 clinical isolates. Sparfloxacin and ciprofloxacin were the most active quinolones against members of the family Enterobacteriaceae and nonfermenting gram-negative bacilli; sparfloxacin had superior activity against gram-positive cocci in comparison with the activities of ciprofloxacin and the other quinolones tested (norfloxacin, lomefloxacin, and pefloxacin). Among the inhibited strains, several were resistant to the tested beta-lactam antibiotics or to aminoglycosides. The activity of sparfloxacin was not influenced by the medium that was used; lowering of the pH to 5 had a marked effect on the MICs for two strains each of Enterobacter cloacae and Pseudomonas aeruginosa and one strain each of Escherichia coli and Staphylococcus aureus; the MBC of sparfloxacin was within 1 to 2 dilution steps of the MIC for the strains that were tested.

Visser, M R; Rozenberg-Arska, M; Beumer, H; Hoepelman, I M; Verhoef, J

1991-01-01

342

In vitro antioxidant activity of extracts from the leaves of Abies pindrow Royle.  

PubMed

Traditionally, the leaves of Abies pindrow Royle are employed as an ayurvedic remedy for fever, hypoglycaemic, respiratory and inflammatory conditions. In this study, dichloromethane, methanol and acetone extracts of A. pindrow leaves were analysed for their phytochemical content and in vitro antioxidant activities. The methanol extract exhibited highest antioxidant activity while acetone extract showed presence of relatively high total phenol and flavonoids contents. The present study provides evidence that extracts of Abies pindrow leaves are a potential source of natural antioxidants and could serve as a base for future drugs. PMID:22654216

Gupta, D; Bhardwaj, R; Gupta, R K

2011-01-01

343

Reduction of the proteolytic activity of neutrophils by exposure to cigarette smoke in vitro.  

PubMed

Human peripheral blood neutrophils were exposed in vitro, in a tonometer, to two different fractions of cigarette smoke-designated particulate phase and vapor phase. The proteolytic activity of the cells following exposure was assessed by measuring their elastase release and ability to degrade fibronectin. At levels of smoke exposure that were physiologically attainable, neither smoke fraction caused an increase in elastase release or fibronectin degradation. In most experiments, fibronectin proteolysis was suppressed by smoke exposure--an effect that was reversible on treatment with phorbol myristate acetate. These data provide evidence that the proteolytic activity of neutrophils is not enhanced by a direct effect of cigarette smoke on these cells. PMID:1959503

Brown, G M; Drost, E; Donaldson, K; MacGregor, I; MacNee, W

1991-01-01

344

Role of paramagnetic polyconjugated clusters in lignin antioxidant activity (in vitro)  

NASA Astrophysics Data System (ADS)

Using physico-chemical methods (EPR, SEC, Py-GC/MS and UV/VIS spectroscopy) and wet chemical analysis, the characteristics of 6 hardwood lignins in terms of functionality, molecular weight and composition of lignin substructures were determined and considered together with the results of DPPH•, ABTS•+ and O2•- antioxidant assays with the aim to understand the relationships governing antioxidant properties of lignin. The strong positive linear correlation between lignin antioxidant capacity in the three assays used and the extent of conjugation of paramagnetic polyconjugated clusters in lignin macromolecules was found. The biological activity of the most active alkaline lignins was assessed by in vitro experiment with human blood.

Dizhbite, T.; Ponomarenko, J.; Andersone, A.; Dobele, G.; Lauberts, M.; Krasilnikova, J.; Mironova-Ulmane, N.; Telysheva, G.

2012-08-01

345

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

Microsoft Academic Search

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

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

2009-01-01

346

Evaluation of in vitro activity of aurones and related compounds against Cryptosporidium parvum.  

PubMed

The efficacy of a series of aurones, auronols and 4-methoxy-alpha-pyrones has been screened for the ability to inhibit the intracellular growth of the parasitic protist Cryptosporidium parvum using an in vitro enzyme linked immunosorbent assay (ELISA). All aurones of this series were active at 25 to 100 microM. 10 of 19 aurones inhibited the intracellular growth of C. parvum by > 90 % with moderate to no toxicity. The most active of these was 3',4',6-trihydroxy-2-[phenylmethylene]-3(2H)-benzofuranone. PMID:11731913

Kayser, O; Waters, W R; Woods, K M; Upton, S J; Keithly, J S; Kiderlen, A F

2001-11-01

347

[Comparison of in vitro activity of six disinfectants on bacteria from contamination in hemodialysis water].  

PubMed

The bactericidal and sporicidal activities of six disinfectants were compared in vitro by determination minimal bactericidal concentrations from AFNOR standards for antiseptics and disinfectants. These disinfectants were tested against seventeen bacterial strains and two suspensions of spores including reference strains and wild strains from water of hospital environment. The compound with peracetic acid, ACETOPER 200, is the only disinfectant with the two activities against all strains at 21 degrees C +/- 1 degree C in short length of time. Furthermore except for Serratia liquefaciens that is remarkably resistant to STERLANE, no significant differences of susceptibility to disinfectants appear between wild bacterial strains and reference strains. PMID:8120786

Ossia-Ongagna, Y; Sabatier, R

1993-01-01

348

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

349

In vitro evaluation of trypanocidal activity in plants used in Argentine traditional medicine.  

PubMed

Thirty-two organic and aqueous extracts, belonging to 12 Argentine medicinal plants were tested for their in vitro trypanocidal activity on epimastigote forms of Trypanosoma cruzi. Among the selected species, the organic extracts of Ambrosia scabra, Ambrosia tenuifolia, Baccharis spicata, Eupatorium buniifolium, Lippia integrifolia, Mulinum spinosum and Satureja parvifolia, and the aqueous extracts of E. buniifolium, L. integrifolia, M. spinosum and S. parvifolia showed trypanocidal activity with a percentage of growth inhibition higher than 70% at a concentration of 100 microg/ml. PMID:16341880

Sülsen, V; Güida, C; Coussio, J; Paveto, C; Muschietti, L; Martino, V

2006-03-01

350

Synthesis and in vitro antibacterial activity of oxazolidine LBM-415 analogs as peptide deformylase inhibitors.  

PubMed

The drug resistant bacteria pose a severe threat to human health. The increasing resistance of those pathogens to traditional antibacterial therapy renders the identification of new antibacterial agents with novel antibacterial mechanisms an urgent need. In this study, a series of (2S)-N-substituted-1-[(formyhydroxyamino)methyl]-1-oxohexyl]-2-oxazolidinecarboxamides were designed, synthesized and evaluated for in vitro antibacterial activity. Most of these compounds displayed good activities against Gram-positive organisms comparable to reference agent LBM-415. PMID:21288715

Yu, Linliang; Zhou, Weicheng; Wang, Zhenyu

2011-03-01

351

Tetracyclines as antiparasitic agents: lipophilic derivatives are highly active against Giardia lamblia in vitro.  

PubMed

Comparisons of the inhibitory activities of different tetracyclines have been reported for Plasmodium falciparum but no other parasites. The in vitro response of the intestinal parasite Giardia lamblia to six tetracyclines in current use was determined. In addition, the experimental drug thiacycline (EMD 33,330) was evaluated. Three groups were discerned, with representative 50 and 90% inhibitory concentrations of, respectively, 36 and 130 (tetracycline), 6.4 and 22 (doxycycline), and 1.8 and 3.4 (thiacycline) micrograms/ml. These dramatic differences in activity correlate with increased lipophilicity. PMID:2619281

Edlind, T D

1989-12-01

352

[Vitro antitumor activity and synthesis of the key intermediate of bakuchiol].  

PubMed

The in vitro antitumor activity of bakuchiol was exploited, compared with tamoxifen. The result of biological activities showed that bakuchiol could inhibit human breast cancer and the IC50 values were 2.89 x 10(-5) mol L(-1) and 8.29 x 10(-3) mol L(-1) against the cells line T-47D and MDA-MB-231 respectively. On the other hand, the key intermediate to synthesize bakuchiol was obtained by the method of Ireland-Claisen rearrangement. Comparing with traditional Claisen rearrangement, the reaction conditions are milder and the reaction reagents are safer. PMID:21355211

Chen, Hong-li; Feng, Hui-jin; Li, Yuan-chao

2010-04-01

353

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

PubMed Central

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

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

2013-01-01

354

Sulfated glycosaminoglycans enhance tumor cell invasion in vitro by stimulating plasminogen activation.  

PubMed

Metastasizing tumor cells invade host tissues by degrading extracellular matrix constituents. We report here that the highly sulfated glycosaminoglycans, heparin and heparan sulfate, as well as the sulfated polysaccharide, fucoidan, significantly enhanced tumor cell invasion in vitro into fibrin, the basement membrane extract, Matrigel, or through a basement membrane-like extracellular matrix. The enhancement of tumor cell invasion was due to a stimulation of the proteolytic cascade of plasminogen activation since the effect required plasminogen activation and was abolished by inhibitors of urokinase-type plasminogen activator (uPA) or plasmin. Sulfated polysaccharides enhanced five reactions of tumor-cell initiated plasminogen activation in a dose-dependent manner. They amplified plasminogen activation in culture supernatants up to 70-fold by stimulating (i) pro-uPA activation by plasmin and (ii) plasminogen activation by uPA. (iii) In addition, sulfated polysaccharides partially protected plasmin from inactivation by alpha 2-antiplasmin. Sulfated polysaccharides also stimulated tumor-cell associated plasminogen activation, e.g., (iv) cell surface pro-uPA activation by plasmin and (v) plasminogen activation by cell surface uPA. These results suggest that sulfated glycosaminoglycans liberated by tumor-cell mediated extracellular matrix degradation in vivo might amplify pericellular plasminogen activation and locally enhance tumor cell invasion in a positive feedback manner. PMID:9521847

Brunner, G; Reimbold, K; Meissauer, A; Schirrmacher, V; Erkell, L J

1998-03-15

355

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

356

In vitro and in vivo antioxidant activity of ethanolic extract of white button mushroom (Agaricus bisporus).  

PubMed

The antioxidant activities of ethanolic extract from edible mushroom Agaricus bisporus (A. bisporus) were evaluated by various methods in vitro and in vivo. In antioxidant assays in vitro, ethanolic extract of A. bisporus was found to have strong reducing power, superoxide radical, hydroxyl radical and 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity, and moderate hydrogen peroxide scavenging activity. In antioxidant assays in vivo, mice were administered with ethanolic extract of A. bisporus via gavage for 30 consecutive days. As a result, administration of ethanolic extract significantly enhanced the activities of antioxidant enzymes in serums, livers and hearts of mice. In addition, the total phenolic content in the extract determined by Folin-Ciocalteu method was 6.18mg of gallic acid equivalents per gram of dry weight. The main phenolic compounds in ethanolic extract analyzed by ultra-high performance liquid chromatography tandem mass spectrometry were determined as gallic acid, protocatechuic acid, catechin, caffeic acid, ferulic acid and myricetin. These results suggested that ethanolic extract of A. bisporus had potent antioxidant activity and could be explored as a novel natural antioxidant. PMID:23099505

Liu, Jun; Jia, Liang; Kan, Juan; Jin, Chang-Hai

2013-01-01

357

Basophil activation test for the in vitro diagnosis of nonsteroidal anti-inflammatory drug hypersensitivity.  

PubMed

There is need for an in vitro diagnostic test for hypersensitivity to nonsteroidal anti-inflammatory drugs (NSAIDs). The purpose of this study was to assess the reliability of one such diagnostic, the basophil activation test. Forty-three drug hypersensitive patients referring several immediate reactions (anaphylaxis, urticaria, angioedema, asthma, and rhinoconjunctivitis) to one or more NSAIDs and 29 controls participated. Using the Basotest commercial kit, 63 determinations were performed with the drugs implicated in the adverse reactions (ASA, ibuprofen, metamizol, diclofenac, paracetamol, and ketorolac). In 16 patients additional determinations were made with other chemically unrelated NSAIDs. Forty-two determinations were made for controls. The analysis was performed by flow colorimetric cytometry and double staining with the monoclonal antibodies anti-IgE and anti-CD63. A Basophil Activation Index (percentage of activated basophils after allergen stimulation/percentage of basally activated basophils) of two or more was considered a positive result. Specificity of 100% and sensitivity of 42.85% were achieved. The positive predictive value was 100%, and the negative predictive value was 53.84%. In 35.29% of intolerant patients there was a positive reaction to at least two drugs implicated in adverse reactions, and in 27.27% of these patients there was a positive reaction to other chemically unrelated NSAIDs. The basophil activation test is useful for the in vitro diagnosis of NSAID hypersensitivity, providing good specificity and positive predictive value and diagnostic reliability in the assessment of NSAID intolerance. PMID:18534081

Rodríguez-Trabado, Ana; Cámara-Hijón, Carmen; Ramos-Cantarińo, Alfonso; Porcel-Carreńo, Sergio Luis; Jiménez-Timón, Soledad; Pereira-Navarro, Gema; Hernández-Arbeiza, Francisco Javier; Fernández-Pereira, Luis

2008-01-01

358

Liposomal incorporation of Artemisia arborescens L. essential oil and in vitro antiviral activity.  

PubMed

The effect of liposomal inclusion on the in vitro antiherpetic activity of Artemisia arborescens L. essential oil was investigated. In order to study the influence of vesicle structure and composition on the antiviral activity of the vesicle-incorporated oil, multilamellar (MLV) and unilamellar (SUV) positively charged liposomes were prepared by the film method and sonication. Liposomes were obtained from hydrogenated (P90H) and non-hydrogenated (P90) soy phosphatidylcholine. Formulations were examined for their stability for over one year, monitoring the oil leakage from vesicles and the average size distribution. The antiviral activity was studied against Herpes simplex virus type 1 (HSV-1) by a quantitative tetrazolium-based colorimetric method. Results showed that Artemisia essential oil can be incorporated in good amounts in the prepared vesicular dispersions. Stability studies pointed out that vesicle dispersions were very stable for at least six months and neither oil leakage nor vesicle size alteration occurred during this period. After one year of storage oil retention was still good, but vesicle fusion was present. Antiviral assays demonstrated that the liposomal incorporation of A. arborescens essential oil enhanced its in vitro antiherpetic activity especially when vesicles were made with P90H. On the contrary, no significant difference in antiviral activity was observed between the free and SUV-incorporated oil. PMID:15567314

Sinico, Chiara; De Logu, Alessandro; Lai, Francesco; Valenti, Donatella; Manconi, Maria; Loy, Giuseppe; Bonsignore, Leonardo; Fadda, Anna Maria

2005-01-01

359

Hepatoprotective activity of Sapindus mukorossi and Rheum emodi extracts: In vitro and in vivo studies  

PubMed Central

AIM: To study the hepatoprotective capacity of Sapindus mukorossi (S. mukorossi) and Rheum emodi (R. emodi) extracts in CCl4 treated male rats. METHODS: The dried powder of S. mukorossi and R. emodi was extracted successively with petroleum ether, benzene, chloroform, and ethanol and concentrated in vacuum. Primary rat hepatocyte monolayer cultures were used for in vitro studies. In vivo, the hepatoprotective capacity of the extract of the fruit pericarp of S. mukorossi and the rhizomes of R. emodi was analyzed in liver injured CCl4-treated male rats. RESULTS: In vitro: primary hepatocytes monolayer cultures were treated with CCl4 and extracts of S. mukorossi & R. emodi. A protective activity could be demonstrated in the CCl4 damaged primary monolayer culture. In vivo: extracts of the fruit pericarp of S. mukorossi (2.5 mg/mL) and rhizomes of R. emodi (3.0 mg/mL) were found to have protective properties in rats with CCl4 induced liver damage as judged from serum marker enzyme activities. CONCLUSION: The extracts of S. mukorossi and R. emodi do have a protective capacity both in vitro on primary hepatocytes cultures and in in vivo in a rat model of CCl4 mediated liver injury.

Ibrahim, Mohammed; Khaja, Mohammed Nane; Aara, Anjum; Khan, Aleem Ahmed; Habeeb, Mohammed Aejaz; Devi, Yalavarthy Prameela; Narasu, Mangamoori Lakshmi; Habibullah, Chitoor Mohammed

2008-01-01

360

In Vitro Epsilon RNA-Dependent Protein Priming Activity of Human Hepatitis B Virus Polymerase  

PubMed Central

Hepatitis B virus (HBV) replicates its DNA genome through reverse transcription of a pregenomic RNA (pgRNA) by using a multifunctional polymerase (HP). A critical function of HP is its specific recognition of a viral RNA signal termed ? (H?) located on pgRNA, which is required for specific packaging of pgRNA into viral nucleocapsids and initiation of viral reverse transcription. HP initiates reverse transcription by using itself as a protein primer (protein priming) and H? as the obligatory template. We have purified HP from human cells that retained H? binding activity in vitro. Furthermore, HP purified as a complex with H?, but not HP alone, displayed in vitro protein priming activity. While the HP-H? interaction in vitro and in vivo required the H? internal bulge, but not its apical loop, and was not significantly affected by the cap-H? distance, protein priming required both the H? apical loop and internal bulge, as well as a short distance between the cap and H?, mirroring the requirements for RNA packaging. These studies have thus established new HBV protein priming and RNA binding assays that should greatly facilitate the dissection of the requirements and molecular mechanisms of HP-H? interactions, RNA packaging, and protein priming.

Jones, Scott A.; Boregowda, Rajeev; Spratt, Thomas E.

2012-01-01

361

In vitro xanthine oxidase inhibitory and in vivo hypouricemic activity of herbal coded formulation (Gouticin).  

PubMed

Currently, natural products have been used in treating gouty arthritis and are recognized as xanthine oxidase inhibitors. Current study was designed to evaluate in vitro xanthine oxidase inhibitory potential of Gouticin and its ingredients extracts and in vivo hypouricemic activity of gouticin tablet 500 mg twice daily. Ethanol extracts of Gouticin and its ingredients were evaluated in vitro, at 200, 100, 50, 25 ? g/ml concentrations for xanthine oxidase inhibitory activity. IC(50) values of Gouticin and its ingredients were estimated. Further, in vivo therapeutic effect of Gouticin was investigated in comparison with allopathic medicine (Allopurinol) to treat gout. Total patients were 200 that were divided into test and control group. Herbal coded medicine (Gouticin) was given to test group and allopathic medicine allopurinol was administered to control group. In vitro, Gouticin has the highest percent inhibition at 96% followed by Allopurinol with 93% inhibition. In vivo study, mean serum uric acid level of patients was 4.62 mg/dl and 5.21mg/dl by use of Gouticin and Allopurinol at end of therapy. The study showed that herbal coded formulation gouticin and its ingredients are potential sources of natural xanthine oxidase inhibitors. Gouticin 500 mg twice daily is more effective than the allopurinol 300mg once daily in the management of gout. PMID:24811815

Akram, Muhammad; Usmanghani, Khan; Ahmed, Iqbal; Azhar, Iqbal; Hamid, Abdul

2014-05-01

362

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.

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

2013-01-01

363

In vitro antioxidant and anticancer activity studies on drosera indica L. (Droseraceae).  

PubMed

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 Fe(2+)chelating assay. EEDI on the reducing power assay and ABTS showed higher IC50 than standard AA. IC50 values of AEDI on Fe(2+) 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

364

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

PubMed Central

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

Krauss, Jan; Zverlov, Vladimir V.

2012-01-01

365

Pharmacological activity of retinoic acid receptor alpha-selective antagonists in vitro and in vivo  

PubMed Central

Oral administration of a retinoic acid receptor (RAR) pan-antagonist reversibly inhibits spermatogenesis. Given the importance of RAR? in regulating spermatogenesis, we identified two RAR?-selective antagonists by transactivation and transactivation competition assays and asked whether they effectively inhibit spermatogenesis. Although these two antagonists were potent in vitro, they displayed poor in vivo activity in mice when administered orally. Testicular weights were normal and morphological analysis revealed normal spermatid alignment and sperm release. In vitro drug property analyses were performed with one of these antagonists and compared with the pan-antagonist. We showed that the discrepancies may be explained by several factors, including high plasma protein binding, faster hepatic metabolism relative to the pan-antagonist, and only moderate permeability. The conclusion of poor oral bioavailability was supported by more pronounced defects in mice when the antagonist was administered intravenously versus intraperitoneally. These results are crucial for designing new RAR?-selective antagonists for pharmaceutical application.

Chung, Sanny S. W.; Cuellar, Rebecca A. D.; Wang, Xiangyuan; Reczek, Peter R.; Georg, Gunda I.; Wolgemuth, Debra J.

2013-01-01

366

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

PubMed

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

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

2014-02-01

367

Molecular characterization of Mutator systems in maize embryogenic callus cultures indicates Mu element activity in vitro.  

PubMed

Active Mutator lines of maize (Zea mays L.) are characterized by their ability to generate new mutants at a high rate and by somatic instability at Mutator-induced mutant alleles. Mutagenically active lines with fewer than ten Mu elements per diploid genome have not been observed. Alteration of Mutator activity has been shown to correlate with the state of modification of Hinfl restiction sites that lie within inverted terminal repeats of Mu elements. To determine whether active Mutator systems can be established and maintained in culture, copy number and modification state of Mu elements were investigated in embryogenic callus lines derived from F1S of crosses of active Mutator stock with the inbred lines A188 and H99. All callus lines studied maintain high Mu-element copy numbers, and more than half show a continued lack of modification at the Mu element Hinfl sites; thus, parameters associated with mutagenic activity in planta are present in some, but not all, callus lines. Mutator activity was then tested directly by restriction fragment analysis of subclonal populations from A188/Mu (2) and H99/Mu (2) embryonic cultures. Novel Mu-homologous restriction fragments occurred in 38% of the subpopulations which contained unmodified Mu elements, but not in control cultures containing modified, genetically inactive Mu elements. We conclude that Mu elements from active Mutator parents can remain transpositionally active in embryogenic cell culture. Active Mutator cell lines may be useful for the production of mutations in vitro. PMID:24232617

James, M G; Stadler, J

1989-03-01

368

Carbenicillin: Activity In Vitro and Absorption and Excretion in Normal Young Men  

PubMed Central

Carbenicillin is a new semisynthetic penicillin which differs from other penicillins in showing moderate antibacterial activity against Pseudomonas. Its activity in vitro is enhanced at low pH. Serum binding is of low order and does not appreciably alter activity. Strains of Pseudomonas exposed to subinhibitory concentrations of carbenicillin rapidly develop resistance by a mechanism that does not depend upon destruction of the drug. In normal subjects, high levels of anti-Pseudomonas activity are readily obtained in the urine after intramuscular injection. Levels of carbenicillin adequate to inhibit many strains of Pseudomonas can be achieved in serum only with an intravenous administration of a large dose. Carbenicillin appears to exhibit the same low degree of toxicity as do other penicillins.

Smith, Charles B.; Finland, Maxwell

1968-01-01

369

Synthesis and in vitro antitumor activities of lupeol dicarboxylic acid monoester derivatives.  

PubMed

Ten lupeol dicarboxylic acid monoester derivatives as new potent antitumor agents were synthesized and evaluated for in vitro antitumor activities against A549, LAC, HepG2 and HeLa cell lines. Among them, compounds 1-5 showed excellent antitumor activities against all tested tumor cell lines and compounds 6-10 exhibited high activities against A549, HepG2 and HeLa cells, exceeded lupeol, lupanol and doxorubicin. Compound 2 displayed the highest potent antitumor activities with IC50 values of 5.78 ?M against A549 cell, 2.38 ?M against LAC cell, 6.14 ?M against HepG2 cell and 0.00842 ?M against HeLa cell. PMID:23700293

Li, Weijie; Hao, Jing; Xiao, Yeyu

2013-12-01

370

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

PubMed Central

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

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

2013-01-01

371

The effect of ethanol and its metabolites upon methionine synthase activity in vitro.  

PubMed

The association of alcoholism with macrocytic anaemia has lead to investigation of the role of cobalamin-dependent methionine synthase in mediating alcohol toxicity. Several studies have found that long-term ingestion of large quantities of ethanol causes inhibition of liver methionine synthase activity in vivo: however, ethanol has not been found to inhibit the enzyme directly. The effect of ethanol and its breakdown products, acetate and acetaldehyde, on highly purified rat liver methionine synthase was tested in vitro. Enzyme activity was not inhibited by ethanol or acetate. Acetaldehyde was found to inhibit methionine synthase activity, with an apparent IC50 of 2 mM. The reported inhibition by acetaldehyde was found to become irreversible over time. Acetaldehyde-induced inhibition of liver methionine synthase activity is thus proposed as the most likely explanation of the reported in vivo effect of ethanol upon methionine synthase. PMID:9590515

Kenyon, S H; Nicolaou, A; Gibbons, W A

1998-05-01

372

Activity of Five Aminoglycoside Antibiotics In Vitro Against Gram-Negative Bacilli and Staphylococcus aureus  

PubMed Central

The in vitro susceptibility to BB-K8, butirosin, gentamicin, sisomicin, and tobramycin of seven groups of clinically significant gram-negative bacilli and Staphylococcus aureus was assessed by using the International Collaborative Study-World Health Organization criteria. The activity of gentamicin, sisomicin, and tobramycin generally paralleled each other. Sisomicin was the most potent compound by weight and usually demonstrated the most rapid rate of killing. BB-K8 and butirosin were less potent, but higher serum levels may be achieved with these agents. BB-K8 generally showed the greatest ratio between achieveable mean peak serum levels and concentrations needed to inhibit [Formula: see text] of each group of organisms tested. Additionally, BB-K8 was active against six of seven highly gentamicin-resistant strains. All of these antibiotics showed diminished activity at pH 6.4 but only gentamicin and sisomicin showed occasionally enhanced activity at pH 8.4.

Young, Lowell S.; Hewitt, William L.

1973-01-01

373

The in vitro antibacterial activity of dietary spice and medicinal herb extracts.  

PubMed

The in vitro antibacterial activities of a total of 46 extracts from dietary spices and medicinal herbs were investigated by agar-well diffusion method against five foodborne bacteria (Bacillus cereus, Listeria monocytogenes, Staphylococcus aureus, Escherichia coli, and Salmonella anatum). Their total phenolic contents were also evaluated. Many herb and spice extracts contained high levels of phenolics and exhibited antibacterial activity against foodborne pathogens. Gram-positive bacteria were generally more sensitive to the tested extracts than Gram-negative ones. S. aureus was the most sensitive, while E. coli was the most resistant. There were highly positive relationships (R(2)=0.73-0.93) between antibacterial activities and phenolic content of the tested extracts against each bacterium. This suggested that the antibacterial activity of the tested extracts was closely associated with their phenolic constituents. PMID:17449125

Shan, Bin; Cai, Yi-Zhong; Brooks, John D; Corke, Harold

2007-06-10

374

In vitro activity of the tricyclic beta-lactam GV104326.  

PubMed

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

1996-05-01

375

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.

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

1996-01-01

376

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

PubMed Central

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

2011-01-01

377

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.

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

2013-01-01

378

In vitro Antioxidant and Antibacterial Activities of Methanol Extract of Kyllinga nemoralis  

PubMed Central

The present study was designed to evaluate the antioxidant and antibacterial activity of methanol extract of Kyllinga nemoralis. Six different in vitro antioxidant assays including 2,2-diphenyl-1-picrylhydrazyl, hydroxyl radical, superoxide anion radical, hydrogen peroxide radical, ferric reducing antioxidant power assay and reducing power were carried out to ensure the scavenging effect of the plant on free radicals. In addition, total antioxidant capacity assay, total phenolic contents, tannins, flavonoids and flavonol contents of the plant were also analysed by the standard protocols. Kyllinga nemoralis exhibited high antioxidant activity on 2,2-diphenyl-1-picrylhydrazyl assay (IC50= 90 ?g/ml), superoxide radical scavenging assay (IC50= 180 ?g/ml) and hydrogen peroxide radical scavenging assay (IC50= 200 ?g/ml), compared with standards. These observations provide comprehensible supporting evidence for the antioxidant potential of the plant extract. Reducing power (IC50= 213.16 ?g/ml) and hydroxyl radical scavenging activity (IC50= 223 ?g/ml) of the plant extract was remarkable. The methanol extract of K. nemoralis exhibited significant antimicrobial activity against Gram-positive human pathogenic bacteria. Standard in vitro antioxidant assays assessed the electron donating ability of the plant extract in scavenging free radicals. The inhibitory effect of the plant extract against bacterial pathogens may be due to the presence of phytochemicals. Thus, the results suggest that Kyllinga nemoralis is a potential source of antioxidants and could serve as the base for drug development.

Sindhu, T.; Rajamanikandan, S.; Srinivasan, P.

2014-01-01

379

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

380

Alternatively activated dendritic cells regulate CD4+ T-cell polarization in vitro and in vivo  

PubMed Central

Interleukin-4 is a cytokine widely known for its role in CD4+ T cell polarization and its ability to alternatively activate macrophage populations. In contrast, the impact of IL-4 on the activation and function of dendritic cells (DCs) is poorly understood. We report here that DCs respond to IL-4 both in vitro and in vivo by expression of multiple alternative activation markers with a different expression pattern to that of macrophages. We further demonstrate a central role for DC IL-4R? expression in the optimal induction of IFN? responses in vivo in both Th1 and Th2 settings, through a feedback loop in which IL-4 promotes DC secretion of IL-12. Finally, we reveal a central role for RELM? during T-cell priming, establishing that its expression by DCs is critical for optimal IL-10 and IL-13 promotion in vitro and in vivo. Together, these data highlight the significant impact that IL-4 and RELM? can have on DC activation and function in the context of either bacterial or helminth pathogens.

Cook, Peter C.; Jones, Lucy H.; Jenkins, Stephen J.; Wynn, Thomas A.; Allen, Judith E.; MacDonald, Andrew S.

2012-01-01

381

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.

Shaheen, Magda

2010-01-01

382

Computerized immunoblot analyses (CIBA) of the distribution of prekallikrein and its activation products in vivo and in vitro.  

PubMed

The distribution of prekallikrein and the complexes of kallikrein with C1 inhibitor (C1INH), alpha 2-macroglobulin and approximately 58-kDa protein(s) (e.g. antithrombin III), differs in normal and C1INH-deficient human plasma, activated in vitro, due to different C1INH levels. Different distribution in the deficient plasma activated in vivo or in vitro, suggests different rates of complex clearance. PMID:1281607

Veloso, D; Campbell, G

1992-01-01

383

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.

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

2012-01-01

384

Cytotoxic, cytoprotective and antioxidant activities of resveratrol and analogues in C6 astroglioma cells in vitro.  

PubMed

Resveratrol (3,4',5-trans-trihydroxystilbene) and other hydroxystilbenes exhibit in vitro antioxidant as well as prooxidant effects. The antioxidant properties are assumed to enable these compounds to protect cells from oxidative damage. The prooxidant effects are held likely to be responsible for their cytotoxic, anti-proliferative or pro-apoptotic effects observed in vitro. Regarding antioxidant/prooxidant activities in the past various studies were performed aiming at defining structure-activity relationships for hydroxystilbenes using cell-free systems. In the present study cultured C6 glioma cells were used in order to investigate the relationship between the antioxidant, cytoprotective and cytotoxic activities of resveratrol and selected analogues, e.g., 3,3',4',5-trans-tetrahydroxystilbene (piceatannol), 3,3',5,5'-trans-tetrahydroxystilbene (3,3',5,5'-THS) and 3,3',4',5,5'-trans-pentahydroxystilbene (3,3',4',5,5'-PHS). All these compounds were cytotoxic to growth-arrested C6 cells, with EC50-values between 20 and 85 microM. A higher cytotoxic potency in proliferating cells indicated a specific cytostatic activity of resveratrol and 3,3',4',5,5'-PHS. All hydroxystilbenes studied inhibited cellular radical generation induced by cumene hydroperoxide (CHP). The rank order of antioxidant potency was resveratrol>piceatannol>3,3',5,5'-THS>3,3',4',5,5'-PHS. However, only resveratrol and piceatannol inhibited cellular radical generation at lower than cytotoxic concentrations. At subcytotoxic concentrations only piceatannol was able to protect the cells from damage caused by CHP. Taken together, these results show that neither the cytotoxic or cytostatic activities of hydroxystilbenes nor their cytoprotective and antioxidant activities in living cells can be predicted from their antioxidant and prooxidant activity, respectively, in cell-free systems. PMID:19744470

Rüweler, Milena; Gülden, Michael; Maser, Edmund; Murias, Marek; Seibert, Hasso

2009-12-10

385

Synthesis and in vitro antitumor activity of novel ring D analogues of the marine pyridoacridine ascididemin: structure-activity relationship.  

PubMed

Marine compounds with pyridoacridine skeletons are known to exhibit interesting antitumor activities. Ascididemin has already been reported as displaying significant antitumor activities in vitro and has also been found to have a relatively high global toxicity in vivo. We synthesized a series of 16 analogues (among which 11 compounds were different from previously described ones) with the aim of developing new anticancer agents with significantly improved efficacy/tolerability ratios. These compounds were obtained either by total synthesis from 5,8-quinolinedione and substituted 2-aminoacetophenones or by the direct substitution of ascididemin. The different compounds and ascididemin used as the control compound were tested at six different concentrations on 12 different human cancer cell lines of various histopathological types (glioblastomas and breast, colon, lung, prostate, and bladder cancers). The IC(50) value (i.e., the drug concentration inhibiting the mean growth value of the 12 cell lines by 50%) of these compounds ranged over five log concentrations, i.e., between 10 000 and 0.1 nM. For several new chemical entities, the antitumor activity (determined in vitro) and tolerability (determined in vivo) were superior to those of the parent alkaloids, i.e., ascididemin and 2-bromoleptoclinidone. PMID:12166949

Delfourne, Evelyne; Darro, Francis; Portefaix, Philippe; Galaup, Chantal; Bayssade, Sylvie; Bouteillé, Anne; Le Corre, Laurent; Bastide, Jean; Collignon, Françoise; Lesur, Brigitte; Frydman, Armand; Kiss, Robert

2002-08-15

386

[ 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

387

In vitro activity of therapeutic drugs against Histomonas meleagridis (Smith, 1895).  

PubMed

Histomoniasis or blackhead is a life-threatening disease of turkeys that is caused by a flagellated protozoan, Histomonas meleagridis. The development of an assay to measure the sensitivity of drugs traditionally used against this parasite, as reputed to be effective against other protozoan parasites, is described. The in vitro minimum lethal concentrations (MLC), time for drug efficacy, and parasite viability after removal of residual drugs were determined. Three of the 10 tested drugs, fenbendazole, albendazole, and sulfadiazine, were found to be ineffective against H. meleagridis. Nifursol, the only compound still authorized as a feed additive in Europe, is an inhibiting agent but is not lethal in vitro. Roxarsone, an arsenical derivate similar to nitarsone (the only authorized drug in United States), is effective at high concentration (200 microg/mL) after a long exposure (48 h). The lethal activity of dimetridazole, metronidazole, ronidazole, tinidazole, and furazolidone in vitro was demonstrated. Dimetridazole (MLC = 25 microg/mL after 6 h of exposure), metronidazole (MLC = 50 microg/mL after 24 h), and furazolidone (MLC = 50 microg/mL after 24 h) are rapidly effective at low concentrations. These results confirm the effectiveness of dimetridazole, a drug that has been used in the treatment and prevention of blackhead. In May 2002 this compound was removed as feed additive in Europe. PMID:12211302

Callait, M P; Granier, C; Chauve, C; Zenner, L

2002-08-01

388

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

PubMed Central

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

da Silva, Cristiane Franca; Batista, Denise da Gama Jaen; De Araujo, 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; Schuhly, Wolfgang

2013-01-01

389

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

PubMed

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

390

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.

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

2014-01-01

391

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

PubMed

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

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

2014-01-01

392

In vitro and in silico antidiabetic activity of pyran ester derivative isolated from Tragia cannabina  

PubMed Central

Objective To investigate the in vitro antidiabetic effects of isolated 4-Oxo-4H-pyran-2,6-dicarboxylic acid bis-[6-methyl-heptyl] ester from the chloroform extract of root of Tragia cannabina (T. cannabina) and AMP kinase activation property of the isolated compound. Methods The roots of T. cannabina were collected and extracted with ethanol [95% v/v] then chromatographed over silica gel 60-120 mesh of column length 100 cm and diameter 3 cm. Elution was carried out with solvents and solvent mixtures of increasing polarities. Then the chloroform extract was used for isolation. In vitro antidiabetic activity was performed with fertile eggs of White Leghorn chicks by induction of diabetes by streptozotocin. Results The isolated pyran ester binds very efficiently within the active pocket of AMPK with the formation of hydrogen bond and consuming less binding energy, which is good when compared to orientation of standard drug metformin. In in vitro antidiabetic evaluation by streptozotocin treated chick embryo the administration of isolated compound at a doses of 0.5 mg/egg and 1 mg/egg produced a significant reduction in the blood glucose levels in a dose dependant manner (P<0.01). The blood glucose level of diabetic control was (244.20±12.64) mg/dL, whereas it was (207.40±2.43) mg/dL (P<0.001) for isolated compound 0.5 mg/egg and 174.800±2.410 mg/dL (P<0.001) for 1 mg/ egg of the isolated compound. Conclusions The significant glucose levels were reduced (P<0.01) after administration of the pyran ester isolated from T. cannabina to streptozotocin treated chick embryo.

Sivajothi, Vaiyapuri; Dakappa, Shruthi Shirur

2014-01-01

393

Comparison of In Vitro Activities of Camptothecin and Nitidine Derivatives against Fungal and Cancer Cells  

PubMed Central

The activities of a series of camptothecin and nitidine derivatives that might interact with topoisomerase I were compared against yeast and cancer cell lines. Our findings reveal that structural modifications to camptothecin derivatives have profound effects on the topoisomerase I-drug poison complex in cells. Although the water-soluble anticancer agents topotecan and irinotecan are less active than the original structure, camptothecin, other derivatives or analogs with substitutions that increase compound solubility have also increased antifungal activities. In fact, a water-soluble prodrug appears to penetrate into the cell and release its active form; the resulting effect in complex with Cryptococcus neoformans topoisomerase I is a fungicidal response and also potent antitumor activity. Some of the compounds that are not toxic to wild-type yeast cells are extremely toxic to the yeast cells when the C. neoformans topoisomerase I target is overexpressed. With the known antifungal mechanism of a camptothecin-topoisomerase I complex as a cellular poison, these findings indicate that drug entry may be extremely important for antifungal activity. Nitidine chloride exhibits antifungal activity against yeast cells through a mechanism(s) other than topoisomerase I and appears to be less active than camptothecin analogs against tumor cells. Finally, some camptothecin analogs exhibit synergistic antifungal activity against yeast cells in combination with amphotericin B in vitro. Our results suggest that camptothecin and/or nitidine derivatives can exhibit potent antifungal activity and that the activities of camptothecin derivatives with existing antifungal drugs may be synergistic against pathogenic fungi. These new compounds, which exhibit potent antitumor activities, will likely require further structural changes to find more selective activity against fungal versus mammalian cells to hold promise as a new class of antifungal agents.

Del Poeta, Maurizio; Chen, Shih-Fong; Von Hoff, Daniel; Dykstra, Christine C.; Wani, Mansukh C.; Manikumar, Govindarajan; Heitman, Joseph; Wall, Monroe E.; Perfect, John R.

1999-01-01

394

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.

Kumar, Ashok; Khan, Saleemulla

2011-01-01

395

Effect of neurotransmitters on NADPH-cytochrome P450 reductase in vitro activity.  

PubMed

Three neurotransmitters, namely adrenaline, serotonin and tryptamine inhibit the in vitro activity of several cytochrome P450 (CYP) isozymes (CYP1A2, CYP2C9, CYP2D6 and CYP3A). In order to test whether this effect is related to inhibition of the CYP-coupled NADPH reductase activity, we assayed the potential inhibitory effect of these neurotransmitters and their main metabolites on the NADPH reductase activity. Of the five compounds analyzed: tryptamine, tryptophol, serotonin, 5-hydroxytryptamine and adrenaline, only adrenaline significantly decreased NADPH reductase activity at the fixed concentration of 500 microM. However, the effect became negligible when adrenaline concentration was decreased to 100 microM: whereas a high inhibitory effect was observed in CYP2D6, CYP2C9 and CYP3A4 enzyme activities, the NADPH reductase activity remains unchanged. This study indicates that the effect of these endogenous neurotransmitters on CYP enzymes is not related to changes in the reductase activity. In the light of these findings further studies on the inhibitory effect of these neurotransmitters on CYP enzymes can be designed ruling out the modulation of the coupled NADPH reductase activity as a confounding factor. PMID:19356039

Gervasini, Guillermo; Martinez, Carmen; Benitez, Julio; Agúndez, Jose A G

2007-08-01

396

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

PubMed Central

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

Prakash Gupta, Rajesh Kashi; Pradeepa; Hanumanthappa, Manjunatha

2013-01-01

397

Relationships between drug activity in NCI preclinical in vitro and in vivo models and early clinical trials  

Microsoft Academic Search

An analysis of the activity of compounds tested in pre-clinical in vivo and in vitro assays by the National Cancer Institute's Developmental Therapeutics Program was performed. For 39 agents with both xenograft data and Phase II clinical trials results available, in vivo activity in a particular histology in a tumour model did not closely correlate with activity in the same

J I Johnson; S Decker; D Zaharevitz; L V Rubinstein; J M Venditti; S Schepartz; S Kalyandrug; M Christian; S Arbuck; M Hollingshead; E A Sausville

2001-01-01

398

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

NASA Astrophysics Data System (ADS)

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

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

399

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

PubMed

New derivatives of thiosemicarbazone Schiff base with isatin moiety were synthesized L1-L6. The structures of these compounds were characterized based on the spectroscopic techniques. Compound L6 was further characterized by XRD single crystal. The interaction of these compounds with calf thymus (CT-DNA) exhibited high intrinsic binding constant (k(b)=5.03-33.00×10(5) M(-1)) for L1-L3 and L5 and (6.14-9.47×10(4) M(-1)) for L4 and L6 which reflect intercalative activity of these compounds toward CT-DNA. This result was also confirmed by the viscosity data. The electrophoresis studies reveal the higher cleavage activity of L1-L3 than L4-L6. The in vitro anti-proliferative activity of these compounds against human colon cancer cell line (HCT 116) revealed that the synthesized compounds (L3, L6 and L2) exhibited good anticancer potency. PMID:24607427

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

2014-05-01

400

[Antibacterial activity in vitro of 10 quinolones against 20 strains of Legionella pneumophila].  

PubMed

Minimal inhibitory concentrations (MICs) of 10 quinolones were determined by dilution method on BCYE, for 20 strains of Legionella pneumophila. Since the BCYE Agar medium reduces the antibacterial activity of some antimicrobials, a correction factor was calculated. It was found to be 1 to 16 according to the antibiotic tested. The following mode adjusted MIC show the good in vitro antibacterial activity of quinolones on L. pneumophila: ofloxacin, pefloxacin, ciprofloxacin, norfloxacin, A 56620 cMIC: 0.06 microgram/ml), A 56619, enoxacin (cMIC: 0.12 microgram/ml), rosoxacin (cMIC: 0.25 microgram/ml). Pipemidic acid (cMIC: 2 micrograms/ml) and nalidixic acid (cMIC: 1 microgram/ml) were the least active. PMID:3534757

Deforges, L; Fournet, M P; Soussy, C J; Duval, J

1986-06-01

401

In vitro anti-influenza viral activities of stilbenoids from the lianas of Gnetum pendulum.  

PubMed

The anti-influenza viral activities of six stilbenoids from the lianas of Gnetum pendulum C. Y. Cheng were evaluated with two different assays, neuraminidase (NA) activity assay and cytopathic effect (CPE) reduction assay. The NA assay results showed that all six stilbenoids exerted an NA inhibitory effect, while the CPE assay indicated that among them, isorhapontigenin (2), gnetupendin B (3), shegansu B (4), and gnetin D 6) exhibit significant in vitro anti-influenza viral activity in MDCK cells, with IC(50) values from 0.67 to 11.99?µg/mL in comparison to the positive controls oseltamivir acid and ribavirin whose IC(50) values were 0.040 and 5.54 µg/mL, respectively. PMID:20539973

Liu, Ai-Lin; Yang, Fan; Zhu, Mian; Zhou, Dan; Lin, Mao; Lee, Simon Ming-Yuen; Wang, Yi-Tao; Du, Guan-Hua

2010-11-01

402

[In vitro activity of a liposomal nystatin formulation (Nyotran) against Cryptococcus neoformans].  

PubMed

The in vitro antifungal activity of a new liposomal nystatin formulation (NISTL, Nyotran, Aronex Ltd., EE.UU.) was evaluated by a microdilution method with RPMI based on the M27A document of the National Committee for Clinical Laboratory Standards (NCCLS) against 22 isolates of Cryptococcus neoformans. This antifungal activity was compared with those of other seven antifungal agents, such as nystatin (NIST), amphotericin B deoxycholate, liposomal amphotericin B, amphotericin B lipid complex, amphotericin B colloidal dispersion, fluconazole, and itraconazole. NISTL was more active in vitrothan NIST, showing MIC values 2-3 fold smaller in 90% of the isolates. The results obtained suggest that this new formulation would be very helpful for the treatment of cryptococcosis. PMID:15762799

Alonso-Vargas, R; González-Alvarez, L; Ruesga, M T; Carrillo-Muńoz, A J; Martín-Mazuelos, E; Wallace, T L; Cossum, P A; Pontón, J; Quindós, G

2000-09-01

403

In vitro and in vivo anticandidal activity of Swietenia mahogani methanolic seed extract.  

PubMed

Swietenia mahogani crude methanolic (SMCM) seed extract was investigated for the antifungal activity against Candida albicans which has not been evaluated previously. The antifungal activity was evaluated against C. albicans via disk diffusion, minimum inhibition concentration (MIC), scanning electron microscope (SEM), transmission electron microscope (TEM) and time killing profile. The MIC value of SMCM seed extract is 12.5 mg/ml. The SEM and TEM findings showed there is morphological changes and cytological destruction of C. albicans at the MIC value. Animal model was used to evaluate the in vivo antifungal activity of SMCM seed extract. The colony forming unit (CFU) were calculated per gram of kidney sample and per ml of blood sample respectively for control, curative and ketaconazole treated groups. There was significant reduction for the CFU/ml of blood and CFU/g of kidney. This indicated that the extract was observed to be effective against C. albicans in vitro and in vivo conditions. PMID:21602779

Sahgal, G; Ramanathan, S; Sasidharan, S; Mordi, M N; Ismail, S; Mansor, S M

2011-04-01

404

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

PubMed

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

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

2007-01-01

405

Diterpene formamides from the tropical marine sponge Cymbastela hooperi and their antimalarial activity in vitro.  

PubMed

Further investigations of the VLC (vacuum-liquid chromatography) fractions obtained from the dichloromethane solubles of the tropical marine sponge Cymbastela hooperi led to the isolation and characterization of five new diterpene formamides, 1-5. Compound 1 is one of the very few examples of a natural product that contains both formamide and isonitrile functionalities within the same molecule. In in vitro antiplasmodial bioassays, 1 was found to have moderate activity (IC(50) 0.5 microg/mL), 2 had weak activity (IC(50) 14.8 microg/mL), and 3-5 were inactive. The pattern of activity found for the metabolites investigated in the current study is consistent with previous findings for these classes of molecules. PMID:19199790

Wright, Anthony D; Lang-Unnasch, Naomi

2009-03-27

406

In vitro inhibitory activity of essential oil vapors against Ascosphaera apis.  

PubMed

This work evaluates the in vitro inhibitory activity of 70 essential oils (EOs) in the vapor phase for the control of Chalkbrood disease caused by Ascosphaera apis Maassen ex Claussen (Olive et Spiltoir). Two wild strains isolated from infected honey bee colonies together with one standard collection strain were tested by the microatmosphere method. From 70 EOs, 39 exhibited an antifungal effect against A. apis standard and wild strains. The greatest antifungal action was observed for EO vapors from Armoracia rusticana, followed by Thymus vulgaris, Cymbopogon flexosus, Origanum vulgare and Allium sativum. An investigation of chemical composition by GC-MS revealed, that the most active EOs contained allyl isothiocyanate, citral, carvacrol and diallyl sulfides as the main constituents. The chemical composition plays a key role, as activities of different EOs from the same botanical species were different according to their composition. PMID:22474973

Kloucek, Pavel; Smid, Jakub; Flesar, Jaroslav; Havlik, Jaroslav; Titera, Dalibor; Rada, Vojtech; Drabek, Ondrej; Kokoska, Ladislav

2012-02-01

407

[Pantogam and pantogam active: qualitative and quantitative features of the interaction with neurotransmitter receptors in vitro].  

PubMed

We conducted a comparative study on the effect of active compounds of pantogam and pantogam active (calcium D(R)-homopantothenate and calcium DL(RS)-homopantothenate) and its L(S)-isomer on the receptors of main brain neuromediators in rats using in vitro radioligand binding analysis. All three compounds interact with binding sites of specific GABA-A and, in particular, GABA-B receptor ligands. Racemate and S-enantiomer, but not its R-form, competed to a moderate degree for D2-receptor binding sites. In all cases, degrees of interaction with receptors were ranged as follows: S-isomer>racemate>R-isomer. These qualitative and quantitative differences are assumed to contribute to pharmacological activity of both drugs. PMID:22677754

Kovalev, G I; Firstova, Iu Iu; Abaimov, D A; Starikova, N A

2012-01-01

408

In vitro activities of 47 antimicrobial agents against three Campylobacter spp. from pigs.  

PubMed

The in vitro activities of 47 antimicrobial agents against 30 isolates of Campylobacter species from pigs were determined by the agar dilution technique. The isolates were obtained from pigs with proliferative enteritis and included 10 strains each of Campylobacter coli, Campylobacter sputorum subsp. mucosalis, and "Campylobacter hyointestinalis Gebhart et al." (this name is not on the Approved Lists). Carbadox, furazolidone, nitrofurantoin, gentamicin, and dimetridazole were the most active drugs, inhibiting all three Campylobacter species with a MIC for 50% of the isolates of 2 micrograms/ml or less. Trimethoprim-sulfamethoxazole, cefazolin, sulfachloropyridazine, novobiocin, vancomycin, sulfathiazole, cyclohexamide, bacitracin, p-arsanilic acid, and colistin were the least active, with MICs for 50% of the isolates ranging from 16 to greater than or equal to 128 micrograms/ml. PMID:3985597

Gebhart, C J; Ward, G E; Kurtz, H J

1985-01-01

409

An insight into synthetic Schiff bases revealing antiproliferative activities in vitro.  

PubMed

Schiff bases or azomethines are among the most important groups of biomolecules. These compounds have been found to reveal both remarkable biological activities and a variety of valuable practical applications. An interest in the exploration of novel series of synthetic Schiff bases has undoubtedly been growing due to their proven utility as attractive lead structures for the design of novel cytotoxic and cytostatic agents with a mechanism of action that sometimes differs from that of clinically authorized anticancer agents. Therefore, in the present paper we have focussed our attention on the collected synthetic simple Schiff bases of aldimine- and ketimine-types revealing anticancer activities in vitro, that have been described in the scientific literature during the last decade, and on structural variations whose affect the antiproliferative activity in sets of the designed molecules. PMID:23673213

Sztanke, Krzysztof; Maziarka, Agata; Osinka, Anna; Sztanke, Ma?gorzata

2013-07-01

410

Identification of triterpene hydroxycinnamates with in vitro antitumor activity from whole cranberry fruit (Vaccinium macrocarpon).  

PubMed

Bioactivity-guided fractionation of cranberry fruit was used to determine the identity of triterpenoid esters from Vaccinium macrocarpon, which inhibit tumor cell growth and may play a role in cancer prevention. In our previous study, a fraction from whole fruit exhibited tumor cell growth inhibition in vitro. The major components of this fraction were isolated by chromatographic separation of ethyl acetate extracts, purified by semipreparative HPLC, and identified by NMR as cis- (1) and trans- (2) isomers of 3-O-p-hydroxycinnamoyl ursolic acid. These triterpenoid esters have not been previously reported in Vaccinium fruit. Bioassay of the purified triterpene cinnamates in tumor cell lines in vitro showed slightly greater activity of compound 1 in most cell lines, with GI(50) values of approximately 20 microM in MCF-7 breast, ME180 cervical and PC3 prostate tumor cell lines. Quercetin was slightly less active than 1, while cyanidin-3-galactoside exhibited much lower cytotoxicity, with GI(50) greater than 250 microM in all cell lines. Phenylboronic acid (3) was also isolated from the fruit but showed insignificant antitumor activity. PMID:12769521

Murphy, Brian T; MacKinnon, Shawna L; Yan, Xiaojun; Hammond, Gerald B; Vaisberg, Abraham J; Neto, Catherine C

2003-06-01

411

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

PubMed

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

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

2014-07-01

412

Gold nanoparticles synthesis and biological activity estimation in vitro and in vivo.  

PubMed

The aim of the work was the synthesis of gold nanoparticles (GNP) of different sizes and the estimation of their biological activity in vitro and in vivo. Materials and Methods: Water dispersions of gold nanoparticles of different sizes have been synthesized by Davis method and characterized by laser-correlation spectroscopy and transmission electron microscopy methods. The GNP interaction with tumor cells has been visualized by confocal microscopy method. The enzyme activity was determined by standard biochemical methods. GNP distribution and content in organs and tissues have been determined via atomic-absorption spectrometry method; genotoxic influence has been estimated by "Comet-assay" method. Results: The GNP size-dependent accumulation in cultured U937 tumor cells and their ability to modulate U937 cell membrane Na(+),K(+)-???-ase activity value has been revealed in vitro. Using in vivo model of Guerin carcinoma it has been shown that GNP possess high affinity to tumor cells. Conclusions: Our results indicate the perspectives of use of the synthesized GNP water dispersions for cancer diagnostics and treatment. It's necessary to take into account a size-dependent biosafety level of nanoparticles. PMID:22453144

Rieznichenko, L S; Dybkova, S M; Gruzina, T G; Ulberg, Z R; Todor, I N; Lukyanova, N Yu; Shpyleva, S I; Chekhun, V F

2012-01-01