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1

In vitro schistosomicidal activity of balsaminol F and karavilagenin C.  

PubMed

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

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

2012-10-24

2

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

2012-07-04

3

Schistosoma mansoni: in vitro schistosomicidal activity and tegumental alterations induced by piplartine on schistosomula.  

PubMed

Schistosomiasis is one of the most important parasitic infections in humans that occur in many tropical and subtropical countries. Currently, the control of schistosomiasis rests with a single drug, praziquantel, which is effective against adult worms but not the larval stages. Recent studies have shown that piplartine, an amide isolated from plants of the genus Piper (Piperaceae), reveals interesting antischistosomal properties against Schistosoma mansoni adult worms. Here, we report the in vitro antischistosomal activity of piplartine on S. mansoni schistosomula of different ages (3 h old and 1, 3, 5, and 7 days old), and examine alterations on the tegumental surface of worms by means of confocal laser scanning microscopy. Piplartine at a concentration of 7.5 ?M caused the death of all schistosomula within 120 h. The lethal effect occurred in a dose-dependent manner and was also dependent on the age of the parasite. Microscopy observation revealed extensive tegumental destruction, including blebbing, granularity, and a shorter body length. This report provides the first evidence that piplartine is able to kill schistosomula of different ages and reinforce that piplartine is a promising compound that could be used for the development of new schistosomicidal agent. PMID:22796749

de Moraes, Josué; Nascimento, Carlos; Yamaguchi, Lydia F; Kato, Massuo J; Nakano, Eliana

2012-07-14

4

Chemical composition and in vitro schistosomicidal activity of the essential oil from the flowers of Bidens sulphurea (Asteraceae)  

Microsoft Academic Search

In this study, the chemical composition and the in vitro schistosomicidal properties of the essential oil obtained from Bidens sulphurea flowers (Bs-EO) were investigated. Its major constituents were identified as being 2,6-di-tert-butyl-4-methylphenol (44.98%), germacrene D (33.70%) and ?-caryophyllene (10.23%). Bs-EO at 100?µg?mL caused death of all the adult worms and promoted separation of the couple pairs into individual male and female

G. P. Aguiar; N. I. Melo; K. A. L. Wakabayashi; M. H. S. Lopes; A. L. L. Mantovani; H. J. Dias; M. J. Fukui; L. C. Keles; V. Rodrigues; M. Groppo; A. A. Silva-Filho; W. R. Cunha; L. G. Magalhăes; A. E. M. Crotti

2012-01-01

5

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

6

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

2013-08-14

7

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

Microsoft Academic Search

The rhizomes of Dryopteris species have popularly been used as vermifuge in flatworm infections. The aim of this work was to evaluate the in vitro schistosomicidal\\u000a activity of some phloroglucinol compounds, obtained from the rhizomes of Dryopteris species, against Schistosoma mansoni adult worms. All worm pairs were dead after 24 h of incubation with aspidin 25 to 100 ?M (1), flavaspidic acid

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

2010-01-01

8

In vitro evaluation of schistosomicidal potential of curcumin against Schistosoma japonicum.  

PubMed

Curcumin is a polyphenol derived from the dietary spice turmeric. The aim of this study was to investigate the in vitro effect of curcumin against eggs, cercariae, pre-adults, and adults of Schistosoma japonicum compared to praziquantel. After incubated by different concentration of curcumin or praziquantel in different time, the percent hatching rates of eggs, the percent dead rates of cercariae, and the number of dead worms were observed. Curcumin showed time- and dose-dependent schistosomicidal effects on every life stages of S. japonicum. In addition, curcumin exhibited an optimal activity against the adult stage with no differential sensitivity between male and female worms and decreased motor activity of these worms without tegumental alterations. The promising in vitro effects on all stages of S. japonicum warrants further evaluation for the prophylactic and therapeutic values in the early and late schistosomiasis in field trials. PMID:23088385

Chen, Yan-Qin; Xu, Qiong-Ming; Li, Xiao-Ran; Yang, Shi-Lin; Zhu-Ge, Hong-Xiang

2012-10-23

9

In vitro evaluation of the schistosomicidal potential of Eremanthus erythropappus (DC) McLeisch (Asteraceae) extracts  

Microsoft Academic Search

Eremanthus erythropappus (DC) McLeisch, a plant popularly known as Candeia (Asteraceae), has high therapeutic potential. In this study, the in vitro schistosomicidal potentials of the ethanolic, dichloromethane and hexane extract of branches were evaluated. Couples of worms obtained from the infected mice were cultured in RPMI supplemented with foetal bovine serum and antibiotics. Four pairs of adult worms were exposed to

L. M. S. Almeida; P. G. S. Farani; L. A. Tosta; M. S. Silvério; O. V. Sousa; A. C. A. Mattos; P. M. Z. Coelho; E. G. Vasconcelos; P. Faria-Pinto

2011-01-01

10

In vivo schistosomicidal activity of three novels 8-hydroxyquinoline derivatives against adult and immature worms of Schistosoma mansoni.  

PubMed

Schistosomiasis control is widely dependent on a single drug, praziquantel (PZQ). The potential for development of resistance to PZQ has justified the search for new alternative chemotherapies. In a previous study, we have been reported that three of 8-hydroxyquinoline derivatives namely: 3-((8-hydroxyquinolin-5-yl) sulfonyl) pentane-2,4-dione (HQSP), 5-((2,4-diphenyl-3H-benzo[b][1,4]diazepin-3-yl) sulfonyl) quinolin-8-ol (HQBD), and 5-((2,4-diphenyl-3H-pyrido[3,4-b][1,4] diazepin-3-yl) sulfonyl) quinolin-8-ol (HQPD) possess a potent anti-schistosomal activity in vitro. The aim of the present study was to evaluate the in vivo schistosomicidal effect of these three compounds on adult and immature worms of Schistosoma mansoni and their induced pathology. Treatment of S. mansoni-infected mice with 1000, 250, 150, and 200 mg/kg body weight of PZQ, HQSP, HQBD, and HQPD, respectively, reduced adult and immature worm burden by 94.63 and 31.32 %, 73.63 and 5.45 %, 76.5 and 28.11 %, and 81.25 and 56.84 %, respectively, compared to infected untreated mice. Moreover, numbers of egg per gram liver and intestine were decreased by 84 and 95.51 %, 47.84 and 46.28 %, 53.18 and 59.37 %, and 54.22 and 67.26 as a result of PZQ, HQSP, HQBD, and HQPD treatment, respectively. Hepatic granuloma volume was also reduced by 40.10, 42.96, 35.72, and 72.09 % due to PZQ, HQSP, HQBD, and HQPD treatment, respectively. In addition, hepatic histopathological alterations and collagen fiber deposition that accompanied with S. mansoni infection were largely retrieved with different treatments, especially HQPD treatment. Furthermore, humoral immune response, especially IgG response against S. mansoni antigens, was augmented with different treatments. This study concluded that among the three tested 8-hydroxyquinoline derivatives, HQPD is the most effective compound against adult and pre-mature worms of S. mansoni and can be used for the development of a new schistosomicidal drug. PMID:23793335

Allam, Gamal; Eweas, Ahmad F; Abuelsaad, Abdelaziz S A

2013-06-22

11

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

12

Synthesis of benzo-benzothiopyranoquinolines (pyridobenzothioxanthones) as possible schistosomicidal and antitumor agents.  

PubMed

The synthesis of a new class of compounds structurally related to cyclohexenothiaxanthones and benzothiaxanthones including a pyridine ring is described in an attempt to find compounds that may have schistosomicidal and carcinostatic activity. Synthesis was achieved through the condensation of amino-cyclohexenothiaxanthones and amino-benzothiaxanthones with ethyl acetoacetate by the Knorr and Conrad-Limpach methods. PMID:724755

Nasr, M; Zayed, A; Nabih, I

1978-07-01

13

In vitro antimycobacterial activities of pyrazinamide analogs.  

PubMed Central

We synthesized various pyrazine derivatives and pyrazinamide analogs and assayed their antimycobacterial activities in vitro in order to find new drugs which are more active against Mycobacterium tuberculosis than pyrazinamide and also active against Mycobacterium avium and Mycobacterium intracellulare. Of the drugs synthesized, four drugs, namely, pyrazine thiocarboxamide, N-hydroxymethyl pyrazine thiocarboxamide, pyrazinoic acid n-octyl ester, and pyrazinoic acid pivaloyloxymethyl ester, were not only bacteriostatic but also bacteriocidal against these three species of mycobacteria in vitro under conditions in which pyrazinamide showed no or little activity. In conclusion, these four drugs are possible candidates for new antimycobacterial agents, and animal experiments are now under way.

Yamamoto, S; Toida, I; Watanabe, N; Ura, T

1995-01-01

14

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

PubMed

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

Allam, G; Abuelsaad, A S A

2013-05-01

15

In vitro activity of ciprofloxacin against mycobacteria  

Microsoft Academic Search

Sir, Ciprofloxacin, a new quinoline carboxylic acid derivative, has high in vitro activity against a wide range of pathogens including members of the family Enterobacteriaeeae and Pseudomonas aeruginosa (1). The pharmacokinetics after oral administration of the drug are characterized by rapid absorption, good diffusion into the extracellular space, and elimination by biliary excretion, hepatic metabolism, glomerular filtration and tubular secretion

H. Gaya; M. V. Chadwick

1985-01-01

16

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

17

In vitro activity of cefodizime (HR-221).  

PubMed Central

The in vitro activity of cefodizime (HR-221), a new cephalosporin antibiotic, was compared with the activities of selected antimicrobial agents against a broad spectrum of aerobic bacteria. Cefodizime concentrations of 2 micrograms/ml inhibited about 90% of Enterobacteriaceae studied. Serratia marcescens required 8 micrograms/ml to inhibit 90% of strains. Among gram-positive cocci, 50% of strains were inhibited by 2 micrograms/ml of cefodizime (including methicillin-resistant Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus faecalis, and penicillin-resistant Streptococcus pneumoniae). Pseudomonas aeruginosa was less susceptible to cefodizime. Cefotaxime, an antibiotic closely related to cefodizime structurally, was about fourfold more active.

Ahonkhai, V I; Cherubin, C E; Shulman, M A

1982-01-01

18

Comparative in vitro activity of five nitrofurans.  

PubMed

Five nitrofurans- nitrofurantoin, nifuratel, nitrofurazone, furazolidone and and SQ 18,506--have been tested against 201 microbial strains. Escherichia coli, Streptococcus faecalis, micrococci and Staphylococcus epidermidis were sensitive to all five compounds; furazolidone and SQ 18,506 were the most active against these species. Klebsiella aerogenes was less sensitive, and Proteus spp., Providencia stuartii and Pseudomonas aeruginosa strains were resistant. Nifuratel was inhibitory for some Candida albicans strains, and SQ 18,506 was highly active against this species. Nifuratel was judged overall to have superior in vitro antimicrobial properties to nitrofurantoin. PMID:657876

Hamilton-Miller, J M; Brumfitt, W

1978-01-01

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

Schistosomicidal and antifecundity effects of oral treatment of synthetic endoperoxide N-89  

Microsoft Academic Search

1,2,6,7-Tetraoxaspiro[7.11]nonadecane (N-89) is a chemically synthesized compound with good efficacy against malaria parasites. We observed strong anti-schistosomal activities of N-89 both in vitro and in vivo. In a murine model with experimental infection of Schistosoma mansoni, orally administered N-89 at the dose of 300mg\\/kg resulted in a significant reduction in worm burden (63%) when mice were treated at 2-weeks postinfection.

Toshie Taniguchi; Takashi Kumagai; Rieko Shimogawara; Shizuko Ichinose; Akiko Hiramoto; Akira Sato; Masayuki Morita; Masatomo Nojima; Hye-Sook Kim; Yusuke Wataya; Nobuo Ohta

2011-01-01

21

In Vitro Activities of Fluoroquinolones against the Spirochete Borrelia burgdorferi  

Microsoft Academic Search

Little is known to date about the in vitro activity of fluoroquinolones against Borrelia species. Our study aimed at determining the in vitro activities of 15 quinolones against nine isolates of the Borrelia burgdorferi sensu lato complex in addition to one Borrelia valaisiana and one Borrelia bissettii tick isolate. For the determination of MICs, a standardized colorimetric microdilution method was

PETER KRAICZY; JUDITH WEIGAND; THOMAS A. WICHELHAUS; PETER HEISIG; HERBERT BACKES; VOLKER SCHAFER; GEORG ACKER; VOLKER BRADE; KLAUS-PETER HUNFELD

2001-01-01

22

In vitro antimicrobial activity of potash alum.  

PubMed

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

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

1996-07-01

23

In Vitro Activity of Thimerosal against Ocular Pathogenic Fungi?  

PubMed Central

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 B. Thimerosal's antifungal activity was significantly superior to those of amphotericin B and natamycin against ocular pathogenic fungi in vitro.

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

2010-01-01

24

In vitro activity of thimerosal against ocular pathogenic fungi.  

PubMed

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 B. Thimerosal's antifungal activity was significantly superior to those of amphotericin B and natamycin against ocular pathogenic fungi in vitro. PMID:19841144

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

2009-10-19

25

Antiprotozoal and cytotoxic activities in vitro of Colombian Annonaceae  

Microsoft Academic Search

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

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

2007-01-01

26

Challenges in capturing oxygenase activity in vitro  

Microsoft Academic Search

Biocatalysis using oxygenase or desaturase enzymes has the potential to add value to native fats and oils by adding oxygen,\\u000a hydroxyl groups, or double bonds to create regio- and\\/or stereospecific products. These enzymes are a subset of the large\\u000a class of oxidoreductase enzymes (from EC subgroups 1.13 and 1.14) involved with biological oxidation and reduction. In vitro biocatalytic processing using

Vincent L. Vilker; Vytas Reipa; Martin Mayhew; Marcia J. Holden

1999-01-01

27

Cell proliferation in vitro modulates fibroblast collagenase activity  

Microsoft Academic Search

Collagenase enzyme activity is regulated by numerous control mechanisms which prevent excessive release and activation of this protease. A primary mechanism for regulating enzyme extracellular activity may be linked to cell division, therefore they have examined the release of collagenase by fibroblasts in vitro in response to cellular proliferation. Studies were performed using fibroblasts derived from adult rat dermis maintained

W. J. Lindblad; L. Flood

1986-01-01

28

In vivo and in vitro macrophage activation by systemic adjuvants.  

PubMed

Six systemic adjuvants of immunity were tested for their ability to induce macrophage activation. Four of them: living BCG, hydrosoluble extracts from BCG (HIU II) and from M.smegmatis (IPM), and lipopolysaccharide from E.coli (LPS), when administered to normal mice render macrophages non-specifically cytotoxic for tumor cells in vitro. The intensity of this phenomenon varied according to the route and time of adjuvant administration. In contrast, lentinan extracted from Lentinus edodes, and levamisole which is a synthetic chemical compound, depressed macrophage cytotoxic potential. BCG, IPM and LPS were shown to have a direct action on macrophages. After in vitro exposure to these agents, the cytotoxic potential of normal macrophages was greatly increased. Levamisole was unable to stimulate this macrophage function directly in vitro. On the other hand, such a macrophage activation has been induced in vitro when normal macrophages were cultivated in the presence of MIF coming from the supernatant of human lymphoblastoid cell lines. PMID:782207

Bruley-Rosset, M; Florentin, I; Mathé, G

1976-02-01

29

Antioxidant activity of Piper betle L. leaf extract in vitro  

Microsoft Academic Search

Piper betle leaves are used as masticatory in Asian countries. In the present study, antioxidant activities of aqueous extracts of three local varieties of P. betle leaves were evaluated by several in vitro systems, e.g. DPPH radical scavenging activity, superoxide radical scavenging activity in a riboflavin\\/light\\/NBT system, hydroxyl radical scavenging activity and inhibition of lipid peroxidation induced by FeSO4 in

Nabasree Dasgupta; Bratati De

2004-01-01

30

In vitro estrogenic activity of Achillea millefolium L  

Microsoft Academic Search

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

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

2007-01-01

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

Possible Mechanism for in Vitro Complement Activation in Blood and Plasma Samples: Futhan\\/ EDTA Controls in Vitro Complement Activation  

Microsoft Academic Search

Background: Ongoing in vitro complement (C) activa- tion in citrate or EDTA plasma has prevented an accu- rate analysis of C-activation products generated in vivo. The aim of this study was to characterize handling and storage conditions required to prevent in vitro C activa- tion in blood and plasma samples collected with Fu- than\\/EDTA. Methods: BiotrakTM RIAs were used to

Philippe H. Pfeifer; Marleen S. Kawahara; Tony E. Hugli

33

Antiviral activities of coffee extracts in vitro  

Microsoft Academic Search

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

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

2008-01-01

34

Ammonium chloride influences in vitro-neuronal network activity.  

PubMed

The objective of the present work is to image functional alterations in hepatic encephalopathy (HE) by ammonia-induced changes of in vitro-neuronal network activity and to identify counteracting strategies. Synchronous bursting behavior of rat cortical cells which is the result of synaptic interaction of excitatory and inhibitory neurons was recorded in vitro on microelectrode arrays (MEAs) after ammonium chloride exposure. In order to test the involvement of astrocytic glutamine metabolism and N-methyl-d-aspartic acid- (NMDA-) receptor function in the observed ammonia-induced network dysregulation and to identify potentially protective strategies, we investigated effects of the glutamine synthetase (GS) inhibitor methionine-sulfoximine (MSO) and the NMDA-receptor antagonist DL-2-Amino-5-phosphono-pentanoic acid (AP-5), respectively. We observed a characteristic ammonia-induced increase of global network activity while network synchrony was suppressed. The increase of global activity, but not the suppression of network synchrony was prevented by inhibiting GS. However, blocking NMDA-receptors prevented both, network excitation and desynchronization. Conclusions: 1. The observed desynchronization of in vitro-neuronal network activity after ammonium chloride treatment might reflect global neuronal network changes in HE in vivo and suggests the MEA technology as a valuable tool for measuring changes of neuronal connectivity in vitro. 2. Astrocytic glutamine metabolism might be involved in increased global network activity, but not in the suppression of network synchrony. 3. Overactivation of NMDA-receptors might underlie both, the ammonia-induced increase of activity and suppression of network synchrony, suggesting that NMDA-receptor function is involved in HE and that their blockage might be protective. 4. Measuring neuronal network activity in vitro by the MEA technology might help to describe functionally protective measures in HE. PMID:22421534

Schwarz, Clara-Sophie; Ferrea, Stefano; Quasthoff, Kim; Walter, Janine; Görg, Boris; Häussinger, Dieter; Schnitzler, Alfons; Hartung, Hans-Peter; Dihné, Marcel

2012-03-07

35

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

36

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

2013-04-11

37

In Vitro Studies of Nitrate Reductase Activity in Cotton Cotyledons  

PubMed Central

Germinating cotton (Gossypium hirsutum L. cv. Deltapine 16) cotyledons developed two peaks of in vitro nitrate reductase activity; the first was stable in vitro and appeared 24 hours after imbibition; and the second, which was extremely labile in vitro, began to develop after the seedlings had emerged and developed chlorophyll. Nitrite reductase activity peaked only after the seedlings had emerged. Dowex 1-Cl (10%, w/v) and bovine serum albumin (3%, w/v) significantly improved the activity of extracted enzyme; greater improvement occurred as expansion of the cotyledons progressed. The major effect of bovine serum albumin on nitrate reductase activity in cotyledon extracts appeared to be that of making the extracted enzyme more active rather than increasing the amount of nitrate reductase extracted or improving the stability of the extracted enzyme. Attempts to correlate protease activity with the increasingly labile nitrate reductase activity in expanding cotyledons were unsuccessful. Instead, when extracts containing stable nitrate reductase were mixed with extracts containing labile nitrate reductase, the latter was stabilized. The nature of the “protector” in the stable extracts is not known. It is heat-stable, but apparently does not function in vivo since nitrate reductase in germinating cotton seedlings rapidly declines following a peak of activity at 24 hours. We suggest that the protector may function by preventing nitrate reductase from dissociating into inactive subunits.

Purvis, Albert C.; Tischler, Charles R.; Fites, Roger C.

1976-01-01

38

In vitro Activity of Lithium Succinate against Malassezia furfur  

Microsoft Academic Search

Objective: The in vitro antifungal activity of lithium succinate has been evaluated against 46 different Malassezia furfur strains, isolated from patients suffering from dandruff, seborrheic dermatitis, and pityriasis versicolor. Methods: Minimum inhibitory concentrations of lithium succinate were measured by the agar dilution technique. Results: Lithium succinate was found to be able to inhibit growth of all investigated M. furfur isolates

P. Nenoff; U. F. Haustein; C. Münzberger

1995-01-01

39

Evaluation of the antioxidant activity of melatonin in vitro  

Microsoft Academic Search

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

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

1996-01-01

40

In Vitro Antimicrobial Activity of Pyridonecarboxylic Acids against Fish Pathogens  

Microsoft Academic Search

New pyridonecarboxylic acids (PCAs) were evaluated for in vitro antibacterial activity against Pasteurella piscicida, Vibrio anguillarum, Edwardsiella tarda, and Streptococcus sp., which were pathogens isolated from diseased fish in Japan. The minimal inhibitory concentrations of 11 PCAs, nalidixic acid, oxolinic acid, piromidic acid, pipemidic acid, miloxacin, flumequine, enoxacin, ofloxacin, norfloxacin, ciprofloxacin, and FR77040, were determined with the serial twofold agar

S. Nakano; T. Aoki; T. Kitao

1989-01-01

41

[In vitro activity of nitroxoline on urogenital mycoplasmas].  

PubMed

The product nitroxoline was studied in vitro for its activity towards Ureaplasma urealyticum and Mycoplasma hominis. In view of the low MIC values obtained, it seems nitroxoline could be used in the treatment of urinary infections. It is bactericidal, and should not produce resistant strains. PMID:3543811

Bonissol, C; Pua, K; Stoďljkovic, B

1986-11-01

42

PPAR agonists modulate human osteoclast formation and activity in vitro  

Microsoft Academic Search

Peroxisome proliferator-activated receptors (PPARs) are members of the nuclear steroid hormone superfamily and exist in three isoforms: PPAR?, ? and ?, each with specific functions. In this study, we have investigated the expression of PPARs by human osteoclast precursors and osteoclasts generated in vitro. In addition, the effects of fibrates and isoform-specific PPAR agonists on osteoclast formation and resorption in

B. Y. Chan; A. Gartland; P. J. M. Wilson; K. A. Buckley; J. P. Dillon; W. D. Fraser; J. A. Gallagher

2007-01-01

43

Comparative in vitro activity of biapenem, a new carbapenem antibiotic  

Microsoft Academic Search

Biapenem is a new carbapenem antibiotic with high stability to human renal dehydropeptidase I. Its in vitro activity was compared with that of imipenem, meropenem, ceftazidime, ceftriaxone, piperacillin and gentamicin against a total of 650 recent clinical isolates. MICs were determined by a standard agar dilution procedure and all isolates were tested at two inocula (104 and 106 cfu). Biapenem

A. M. Clarke; S. J. V. Zemcov

1993-01-01

44

Influence of gold nanoparticles on platelets functional activity in vitro  

Microsoft Academic Search

Now in the leading biomedical centers of the world approved new technology of laser photothermal destruction of cancer cells using plasmon gold nanoparticles. Investigations of influence of gold nanoparticles on white rat platelets aggregative activity in vitro have been made. Platelet aggregation was investigated in platelet rich plasma (PRP) with help of laser analyzer 230 LA <> (Russia). Aggregation inductor

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

2008-01-01

45

In vitro activity of potential anti-poxvirus agents  

Microsoft Academic Search

The potential use of variola or another orthopoxvirus such as monkeypox as a weapon of bioterrorism has stimulated efforts to develop new drugs for treatment of smallpox or other poxvirus infections. At the present time only cidofovir is approved for use in the emergency treatment of smallpox outbreaks. Although cidofovir is very active against the orthopoxviruses in vitro and in

Earl R Kern

2003-01-01

46

In vitro screening of medicinal plant extracts for macrofilaricidal activity  

Microsoft Academic Search

Methanolic extracts of 20 medicinal plants were screened at 1–10 mg\\/ml for in vitro macrofilaricidal activity by worm motility\\u000a assay against adult Setaria digitata, the cattle filarial worm. Four plant extracts showed macrofilaricidal activity by worm motility at concentrations below\\u000a 4 mg\\/ml and an incubation period of 100 min. Complete inhibition of worm motility and subsequent mortality was observed at\\u000a 3, 2, 1

Mathew Nisha; M. Kalyanasundaram; K. P. Paily; Abidha; P. Vanamail; K. Balaraman

2007-01-01

47

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

48

In vitro activity of chlorhydroxyquinoline against mycoplasma species.  

PubMed Central

The in vitro activities of 5-chloro-8-hydroxyquinoline (CHQ) against single strains of 12 different species of mycoplasma and the impacts of repeated exposure of these strains to CHQ on their susceptibility to this agent have been studied. On initial exposure, the minimal inhibitory concentrations for these strains ranged from 0.24 to 1.92 micrograms of CHQ per ml of test medium; activities remained unchanged during 10 serial transfers in CHQ-containing medium.

Cosgrove, R F; Baines, S

1978-01-01

49

In vitro activity of chlorhydroxyquinoline against mycoplasma species.  

PubMed

The in vitro activities of 5-chloro-8-hydroxyquinoline (CHQ) against single strains of 12 different species of mycoplasma and the impacts of repeated exposure of these strains to CHQ on their susceptibility to this agent have been studied. On initial exposure, the minimal inhibitory concentrations for these strains ranged from 0.24 to 1.92 micrograms of CHQ per ml of test medium; activities remained unchanged during 10 serial transfers in CHQ-containing medium. PMID:263891

Cosgrove, R F; Baines, S

1978-03-01

50

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

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

In Vitro Activity of Caspofungin against Candida albicans Biofilms  

PubMed Central

Most manifestations of candidiasis are associated with biofilm formation on biological or inanimate surfaces. Candida albicans biofilms are recalcitrant to treatment with conventional antifungal therapies. Here we report on the activity of caspofungin, a new semisynthetic echinocandin, against C. albicans biofilms. Caspofungin displayed potent in vitro activity against sessile C. albicans cells within biofilms, with MICs at which 50% of the sessile cells were inhibited well within the drug's therapeutic range. Scanning electron microscopy and confocal scanning laser microscopy were used to visualize the effects of caspofungin on preformed C. albicans biofilms, and the results indicated that caspofungin affected the cellular morphology and the metabolic status of cells within the biofilms. The coating of biomaterials with caspofungin had an inhibitory effect on subsequent biofilm development by C. albicans. Together these findings indicate that caspofungin displays potent activity against C. albicans biofilms in vitro and merits further investigation for the treatment of biofilm-associated infections.

Bachmann, Stefano P.; VandeWalle, Kacy; Ramage, Gordon; Patterson, Thomas F.; Wickes, Brian L.; Graybill, John R.; Lopez-Ribot, Jose L.

2002-01-01

53

In vitro phytotoxicity and antioxidant activity of selected flavonoids.  

PubMed

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

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

2012-05-04

54

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

55

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

56

In Vitro Antibacterial Activity and Pharmacodynamics of New Quinolones  

Microsoft Academic Search

  \\u000a This synopsis of published literature summarises data on the in vitro antibacterial activity and pharmacodynamics of fluoroquinolones.\\u000a Data were compiled for ciprofloxacin, levofloxcin, moxifloxacin, gatifloxacin, grepafloxacin, gemifloxacin, trovafloxacin,\\u000a sitafloxacin and garenoxacin. All of these quinolones are almost equipotent against gram-negative bacteria but demonstrate\\u000a improved activity against gram-positive species. The new quinolones are uniformly active against gram-positive species except\\u000a Streptococcus

A. Dalhoff; F.-J. Schmitz

2003-01-01

57

Comparative in vitro antimicrobial activity of Chinese medicinal herbs.  

PubMed

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

Franzblau, S G; Cross, C

1986-03-01

58

In vitro antileishmanial activity of acetogenins from Annonaceae  

Microsoft Academic Search

Twelve acetogenins from Annonaceae were evaluated in vitro for their antileishmanial activities in order to search for new lead-compounds having antileishmanial properties. The compounds were comparatively evaluated by the 50% inhibitory concentrations (IC50) determination on promastigote forms of wild-type and four drug-resistant lines of Leishmania donovani. In addition, after testing the toxicity on mouse peritoneal macrophages, the compounds were evaluated

S. Raynaud-Le Grandic; C. Fourneau; A. Laurens; C. Bories; R. Hocquemiller; P. M. Loiseau

2004-01-01

59

In vitro activity of pentamidine against Tropheryma whipplei.  

PubMed

Pentamidine is a group I intron splice inhibitor used as a chemotherapeutic agent to treat parasitic infections. It was recently found to be efficient intracellularly against Coxiella burnetii, the bacterial agent of Q fever. This in vitro activity was linked to the presence of self-splicing group I introns that disrupt the 23S rRNA of C. burnetii. However, there are several indications that pentamidine may have a wider range of antibacterial activity. The aim of this study was to determine the in vitro activity of pentamidine against Tropheryma whipplei, the agent of Whipple's disease, a chronic disease for which antibiotic treatment remains challenging. In vitro susceptibility testing of pentamidine and doxycycline was assessed both in axenic medium and in cell culture against three clinical isolates of T. whipplei using a quantitative real-time polymerase chain reaction (PCR) assay as previously described. Both doxycycline and pentamidine were found to be active against T. whipplei strains both in axenic medium and in cell culture, with minimum inhibitory concentration ranges of 0.5-1mg/L and 0.125-0.25mg/L for doxycycline and pentamidine, respectively. Pentamidine was effective in vitro against T. whipplei both intracellularly and in axenic medium. This is the first evidence of the direct efficacy of pentamidine against T. whipplei grown in axenic medium and in cells. Since pentamidine has been widely used in humans, we believe that it could be an alternative drug for the treatment of this chronic disease that should be further studied in clinical trials. PMID:22005072

Rolain, Jean-Marc; Fenollar, Florence; Raoult, Didier

2011-10-17

60

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

61

Activities of Taurolidine In Vitro and in Experimental Enterococcal Endocarditis  

PubMed Central

In vitro, the antimicrobial agent taurolidine inhibited virtually all of the bacteria tested, including vancomycin-resistant enterococci, oxacillin-resistant staphylococci, and Stenotrophomonas maltophilia, at concentrations between 250 and 2,000 ?g/ml. Taurolidine was not effective in experimental endocarditis. While it appears unlikely that this antimicrobial would be useful for systemic therapy, its bactericidal activity and the resistance rates found (<10?9) are favorable indicators for its possible development for topical use.

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

2000-01-01

62

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

63

In vitro activity of the nisin dehydratase NisB.  

PubMed

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

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

2013-04-15

64

Testosterone induces activation of porcine primordial follicles in vitro  

Microsoft Academic Search

Purpose  The mechanism underlying primordial follicle activation is poorly understood. In this study, in-vitro culture and subsequent\\u000a xenotransplantation were conducted to determine whether testosterone promotes the activation of porcine primordial follicles.\\u000a \\u000a \\u000a \\u000a \\u000a Methods  Prepubertal porcine ovarian cortical strips containing primordial follicles were cultured in the presence of testosterone\\u000a for 7 days, and subsequently transplanted to immunodeficient mice for 2 months. After culture and transplantation, development

Manjula P. S. MagamageMai; Mai Zengyo; Mohammad Moniruzzaman; Takashi Miyano

2011-01-01

65

In Vitro Antifungal Activity of Isavuconazole against Madurella mycetomatis  

PubMed Central

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

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

2012-01-01

66

In vitro antifungal activity of isavuconazole against Madurella mycetomatis.  

PubMed

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

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

2012-09-10

67

In Vitro Antibody-Enzyme Conjugates with Specific Bactericidal Activity  

PubMed Central

IgG with antibacterial antibody opsonic activity was isolated from rabbit antisera produced by intravenous hyperimmunization with several test strains of pneumococci, Group A ?-hemolytic streptococci, Staphylococcus aureus, Proteus mirabilis, Pseudomonas aeruginosa, and Escherichia coli. Antibody-enzyme conjugates were prepared, using diethylmalonimidate to couple glucose oxidase to IgG antibacterial antibody preparations. Opsonic human IgG obtained from serum of patients with subacute bacterial endocarditis was also conjugated to glucose oxidase. Antibody-enzyme conjugates retained combining specificity for test bacteria as demonstrated by indirect immunofluorescence. In vitro test for bactericidal activity of antibody-enzyme conjugates utilized potassium iodide, lactoperoxidase, and glucose as cofactors. Under these conditions glucose oxidase conjugated to antibody generates hydrogen peroxide, and lactoperoxidase enzyme catalyzes the reduction of hydrogen peroxide with simultaneous oxidation of I- and halogenation and killing of test bacteria. Potent in vitro bactericidal activity of this system was repeatedly demonstrated for antibody-enzyme conjugates against pneumococci, streptococci, S. aureus, P. mirabilis, and E. coli. However, no bactericidal effect was demonstrable with antibody-enzyme conjugates and two test strains of P. aeruginosa. Bactericidal activity of antibody-enzyme conjugates appeared to parallel original opsonic potency of unconjugated IgG preparations. Antibody-enzyme conjugates at concentrations as low as 0.01 mg/ml were capable of intense bactericidal activity producing substantial drops in surviving bacterial counts within 30-60 min after initiation of assay. These in vitro bactericidal systems indicate that the concept of antibacterial antibody-enzyme conjugates may possibly be adaptable as a mechanism for treatment of patients with leukocyte dysfunction or fulminant bacteremia.

Knowles, Daniel M.; Sullivan, Timothy J.; Parker, Charles W.; Williams, Ralph C.

1973-01-01

68

In vitro activities of purified visna virus integrase.  

PubMed Central

Although integration generally is considered a critical step in the retrovirus life cycle, it has been reported that visna virus, which causes degenerative neurologic disease in sheep, can productively infect sheep choroid plexus cells without detectable integration. To ascertain whether the integrase (IN) of visna virus is an inherently defective enzyme and to create tools for further study of integration of the phylogenetically related human immunodeficiency virus type 1 (HIV-1), we purified visna virus IN by using a bacterial expression system and applied various in vitro oligonucleotide-based assays to studying this protein. We found that visna virus IN demonstrates the full repertoire of in vitro functions characteristic of retroviral integrases. In particular, visna virus IN exhibits site-specific endonuclease activity following the invariant CA found two nucleotides from the 3' ends of viral DNA (processing activity), joins processed oligonucleotides to various sites on other oligonucleotides (strand transfer or integration activity), and reverses the integration reaction by resolving a complex that mimics one end of viral DNA integrated into host DNA (disintegration activity). In addition, although it has been reported that purified HIV-1 IN cannot specifically nick visna virus DNA ends, purified visna virus IN does specifically process and integrate HIV-1 DNA ends. Images

Katzman, M; Sudol, M

1994-01-01

69

Complement activation by Coccidioides immitis: in vitro and clinical studies.  

PubMed Central

Mycelial- or spherule-phase derivatives of Coccidioides immitis caused a decrease in vitro of total hemolytic complement in serum from a nonsensitized person. Activation involved both classic and alternative pathways as shown by deprssion of hemolytic C4 and by generation of products of activation of components C3, C4, and factor B. In addition, functional complement activity or immunoreactive levels of complement components or both were measured in 23 patients with self-limited or disseminated coccidioidomycosis. Low total hemolytic complement was found in nine, usually during the early phase of primary illness, and was transient. Hemolytic C4 was low, and the effect of inulin to decrease complement levels was blunted, suggested both classic and alternative pathways may be deficient. However, associated depression of immunoreactive levels of components assayed (C3, C4, C5, factor B, and properdin) was not consistently found. This disparity raises the possibility of enhanced in vitro inactivation analogous to activation by immune complexes. Images Fig. 2

Galgiani, J N; Yam, P; Petz, L D; Williams, P L; Stevens, D A

1980-01-01

70

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

PubMed

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

Alsterholm, Mikael; Karami, Nahid; Faergemann, Jan

2010-05-01

71

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

PubMed

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

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

2007-02-16

72

In vitro antioxidant activities of Solanum surattense leaf extract  

PubMed Central

Objective To evaluate the antioxidant activity of alcoholic leaf-extract of Solanum surattense (Solanaceae) (S. surattense). Methods Leaf extract were tested for in vitro free radical scavenging assays, such as hydroxyl radical and hydrogen peroxide, inhibition of superoxide anion radical and 2, 2-diphenyl-1-picryl hydrazyl radical (DPPH), total antioxidant activity and reducing ability. Further, total phenolic content of S. surattense was analyzed. Results S. surattense extract effectively scavenged free radicals at all different concentrations and showed its potent antioxidant activity. Further, these effects were in a dose dependent manner. Results were compared to standard antioxidants such as butylated hydroxytoluene, ascorbic acid and ?-tocopherol. Conclusions S. surattense have strong antioxidant potential. Further the study validates the therapeutic benefits of the Indian system of medicine.

Muruhan, Sridevi; Selvaraj, Senthil; Viswanathan, Pugalendi Kodukkur

2013-01-01

73

HIV-1 integrase crosslinked oligomers are active in vitro  

PubMed Central

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

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

2005-01-01

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

2012-01-25

75

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

2013-08-12

76

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

2013-04-01

77

Evaluation of antioxidant activity of Melothria maderaspatana in vitro  

Microsoft Academic Search

In this study, an aqueous extract of leaves from Melothria maderaspatana was tested for in vitro antioxidant activity. Free radical scavenging assays, such as hydroxyl radical, hydrogen peroxide, superoxide anion radical\\u000a and 2,2-diphenyl-1-picryl hydrazyl (DPPH), 2,2’-azinobis-(3-ethyl-enzothiazoline-6-sulfonic acid) (ABTS) radical scavenging,\\u000a and reducing power assay, were studied. The extract effectively scavenged hydroxyl radical, hydrogen peroxide and superoxide\\u000a anion radicals. It also

Boobalan Raja; Kodukkur Viswanathan Pugalendi

2010-01-01

78

The estrogenic activity of phthalate esters in vitro.  

PubMed

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

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

1997-08-01

79

In vitro Reconstitution of the Active T. castaneum Telomerase  

PubMed Central

Efforts to isolate the catalytic subunit of telomerase, TERT, in sufficient quantities for structural studies, have been met with limited success for more than a decade. Here, we present methods for the isolation of the recombinant Tribolium castaneum TERT (TcTERT) and the reconstitution of the active T. castaneum telomerase ribonucleoprotein (RNP) complex in vitro. Telomerase is a specialized reverse transcriptase1 that adds short DNA repeats, called telomeres, to the 3' end of linear chromosomes2 that serve to protect them from end-to-end fusion and degradation. Following DNA replication, a short segment is lost at the end of the chromosome3 and without telomerase, cells continue dividing until eventually reaching their Hayflick Limit4. Additionally, telomerase is dormant in most somatic cells5 in adults, but is active in cancer cells6 where it promotes cell immortality7. The minimal telomerase enzyme consists of two core components: the protein subunit (TERT), which comprises the catalytic subunit of the enzyme and an integral RNA component (TER), which contains the template TERT uses to synthesize telomeres8,9. Prior to 2008, only structures for individual telomerase domains had been solved10,11. A major breakthrough in this field came from the determination of the crystal structure of the active12, catalytic subunit of T. castaneum telomerase, TcTERT1. Here, we present methods for producing large quantities of the active, soluble TcTERT for structural and biochemical studies, and the reconstitution of the telomerase RNP complex in vitro for telomerase activity assays. An overview of the experimental methods used is shown in Figure 1.

Schuller, Anthony P.; Harkisheimer, Michael J.; Skordalakes, Emmanuel

2011-01-01

80

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

81

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

82

In vitro antiplasmodial activity of 4-phenylcoumarins from Exostema mexicanum.  

PubMed

The stem bark of Exostema mexicanum (Rubiaceae) is used in Latin American folk medicine as a quinine substitute for malaria treatment. Bioassay-guided fractionation of lipophilic and hydrophilic extracts from the stem bark and branches yielded two previously undescribed 4-phenylcoumarins: 4',8-dihydroxy-5,7-dimethoxy-4-phenylcoumarin (exomexin A) and 3',4'-dihydroxy-5,7,8-trimethoxy-4-phenylcoumarin (exomexin B). Together with five known derivatives the in vitro activities against a chloroquine-sensitive strain (poW) and a chloroquine-resistant strain (Dd2) of Plasmodium falciparum have been evaluated. The most lipophilic compound, 4',5,7,8-tetramethoxy-4-phenylcoumarin (O-methylexostemin) revealed the strongest antiplasmodial activity (IC50 values: 3.6 microg/ml [poW], 1.6 microg/ml [Dd2]). PMID:11270733

Köhler, I; Jenett-Siems, K; Mockenhaupt, F P; Siems, K; Jakupovic, J; González, J C; Hernández, M A; Ibarra, R A; Berendsohn, W G; Bienzle, U; Eich, E

2001-02-01

83

Australian plants show anthelmintic activity toward equine cyathostomins in vitro.  

PubMed

Anthelmintic resistance in gastrointestinal parasites of horses is an increasing problem, particularly in cyathostomins, and there is a need to find alternative means for the control of these parasites. We screened crude extracts from 37 species of Australian native plants for their anthelmintic activity in vitro against cyathostomin larvae (development from egg to third larval stage), with the aim of identifying those species that may be suitable for incorporation into sustainable parasite management programs. Water extracts from seven species, namely Acacia baileyana, Acacia melanoxylon, Acacia podalyriifolia, Alectryon oleifolius, Duboisia hopwoodii, Eucalyptus gomphocephala and Santalum spicatum completely inhibited larval development (100% inhibition compared to the control), while another 10 species caused 90% inhibition at the initial screening concentration of 1400 ?g of extractable solids/mL. The seven most potent extracts produced IC50 values (concentration of extract which resulted in a 50% inhibition of development) in the range 30.9-196 ?g/mL. Fourteen extracts were incubated with polyvinylpolypyrrolidone (PVPP) before the assays, which removed the anthelmintic activity from 12 of these extracts, indicating that tannins were likely to be the bioactive compound responsible for the effect, while in two species, i.e. A. melanoxylon and D. hopwoodii, compounds other than tannins were likely to be responsible for their anthelmintic action. Our results suggest that a number of Australian native plants have significant anthelmintic activity against cyathostomin larval development in vitro. There is potential for these plants to be used as part of sustainable parasite control programs in horses, although more research is needed to identify the compounds responsible for the anthelmintic effects and confirm their activity in vivo. PMID:23394801

Payne, S E; Kotze, A C; Durmic, Z; Vercoe, P E

2013-01-23

84

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

85

Cell proliferation in vitro modulates fibroblast collagenase activity  

SciTech Connect

Collagenase enzyme activity is regulated by numerous control mechanisms which prevent excessive release and activation of this protease. A primary mechanism for regulating enzyme extracellular activity may be linked to cell division, therefore they have examined the release of collagenase by fibroblasts in vitro in response to cellular proliferation. Studies were performed using fibroblasts derived from adult rat dermis maintained in DMEM containing 10% newborn calf serum, 25 mM tricine buffer, and antibiotics. Cells between subculture 10 and 19 were used with enzyme activity determined with a /sup 14/C-labelled soluble Type I collagen substrate with and without trypsin activation. Fibroblasts, trypsinized and plated at low density secreted 8.5 fold more enzyme than those cells at confluence (975 vs. 115 dpm/..mu..g DNA). This diminution occurred gradually as the cells went from logrithmic growth towards confluence. Confluent fibroblast monolayers were scraped in a grid arrangement, stimulating the remaining cells to divide, without exposure to trypsin. Within 24-48 hr postscraping enzyme levels had increased 260-400%, accompanied by enhanced incorporation of /sup 3/H-thymidine and /sup 3/H-uridine into cell macromolecules. The burst of enzyme release began to subside 12 hr later. These results support a close relationship between fibroblast proliferation and collagenase secretion.

Lindblad, W.J.; Flood, L.

1986-05-01

86

In Vitro Activities of Ketolide HMR 3647, Macrolides, and Clindamycin against Coryneform Bacteria  

PubMed Central

The in vitro activity of ketolide HMR 3647 against coryneform bacteria isolated from clinical samples was evaluated. Except against Corynebacterium jeikeium and C. urealyticum, HMR 3647 showed high activity against Corynebacterium spp., being more active than 14- and 16-membered macrolides, azithromycin, or clindamycin. HMR 3647 also had high in vitro activity against Brevibacterium spp. and Listeria monocytogenes.

Martinez-Martinez, Luis; Pascual, Alvaro; Suarez, Ana Isabel; Perea, Evelio J.

1998-01-01

87

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

88

In vitro estrogenic activity of Achillea millefolium L.  

PubMed

Isolation and biological characterization of pure compounds was used to identify and characterize estrogenic activity and estrogen receptors (ER) preference in chemical components of Achillea millefolium. This medicinal plant is used in folk medicine as an emmenagogue. In vitro assay, based on recombinant MCF-7 cells, showed estrogenic activity in a crude extract of the aerial parts of A. millefolium. After fractionation of the crude extract with increasing polar solvents, estrogenic activity was found in the methanol/water fraction. Nine compounds were isolated and characterized by HR-MS spectra and 1D- and 2D-NMR techniques. In particular, dihydrodehydrodiconiferyl alcohol 9-O-beta-D-glucopyranoside - a glycosyl-neolignan - was isolated for the first time from the genus Achillea in addition to six flavone derivatives, apigenin, apigenin-7-O-beta-D-glucopyranoside, luteolin, luteolin-7-O-beta-D-glucopyranoside, luteolin-4'-O-beta-D-glucopyranoside, rutin, and two caffeic acid derivatives, 3,5-dicaffeoylquinic acid and chlorogenic acid. Apigenin and luteolin, the most important estrogenic compounds among those tested, were studied for their ability to activate alpha or beta estrogen receptors (ERalpha, ERbeta) using transiently transfected cells. Our results suggest that isolation and biological characterization of estrogenic compounds in traditionally used medicinal plants could be a first step in better assessing further (e.g. in vivo) tests of nutraceutical and pharmacological strategies based on phytoestrogens. PMID:16860978

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

2006-07-24

89

Immunomodulating activity of seaweed extract on human lymphocytes in vitro.  

PubMed

Effect of eight kinds of seaweed extract (SWE) on human lymphocytes was studied in vitro. The extracts of Hizikiafusiformis and Meristotheca papulosa (green) markedly stimulated human lymphocytes to proliferate, whereas Eucheuma muricatum and Meristotheca papulosa (red) weakly stimulated proliferation. The responder cells are T cells, because T cells purified by sheep red blood cell (SRBC) rosette-formation were significantly stimulated with SWE, but B cells were not. These extracts enhanced the induction of cytotoxic T lymphocyte (CTL) activity, but failed to enhance natural killer (NK) cell activity. These extracts had a stimulatory effect on immunoglobulin (Ig) production by B cells and tumor necrosis factor (TNF) production by monocytes. The activity of Hizikia fusiformis associated with polysaccharides which were extracted with ethanol and purified by ion-exchange and gel filtration chromatography, whose molecular weight was about 100 kDa. These results suggest that SWE has an immunomodulating activity on human lymphocytes and this ability might be useful for clinical application to treat several diseases such as tumors. PMID:10411282

Shan, B E; Yoshida, Y; Kuroda, E; Yamashita, U

1999-01-01

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

In vitro activity of vinorelbine on human leukemia cells.  

PubMed

Vinorelbine (VNR) is a semi-synthetic Vinca rosea alkaloid that has been employed both as a single agent and in combination, and has shown significant antitumor activity. As little is known about VNR activity on human leukemia, we studied its in vitro cytotoxic effect on human leukemia cell lines (FLG 29.1, HL60, K562, Balm 4, CEM and Daudi) and on fresh leukemia cells from 28 patients: 2 acute myeloid leukemia (AML); 3 chronic myeloid leukemia in blastic phase (CML-BP); 5 acute lymphoblastic leukemia (ALL); 18 B-chronic lymphatic leukemia (B-CLL), employing the colorimetric INT assay and determining the IC50. We observed that VNR exerts its cytotoxic activity on leukemic cell lines in a dose-dependent fashion. The lymphoid cell lines appear more sensitive than the myeloid ones to the VNR-dependent growth inhibition. A similar pattern was noticed for leukemia cells in primary cultures. VNR is not effective on CML-BP cells, shows variable activity on the AML and ALL cells and is very effective against B-CLL cells. VNR inhibited the growth of fresh B-CLL cells from 15 of 18 patients, the IC50 doses ranging from 4 ng/ml to 83 microg/ml (doses coinciding with the plasma levels obtained in clinics). These observations strongly suggest that VNR could be useful in clinics for the treatment of B-CLL. PMID:11450890

Landini, I; Bartolozzi, B; Banchelli, I; Degli Innocenti, A; Nocentini, O; Bernabei, P A

2001-06-01

92

Synthesis and in vitro anticancer activities of some selenadiazole derivatives.  

PubMed

A novel series of fourteen substituted selenadiazoles has been synthesized and the compounds tested for their in vitro antiproliferative and cytotoxic activities. The tests were carried out against leukemia (CCRF-CEM), colon (HT-29), lung (HTB-54), and breast (MCF-7) cancer cells. In order to assess the selectivity of the compounds under investigation the assays were also carried out on two non-tumoral lines - one mammary (184B5) and one bronchial epithelium (BEAS-2B) cell line. Assay-based antiproliferative activity studies revealed that seven derivatives (2a, 2c, 2e, 2f, 2g, 3a, and 3b) exhibited good activity against MCF-7 cells: for instance, 2c and 2f inhibited cell growth with nanomolar GI?? values. Compound 2f had a better antitumoral profile than vinorelbine and paclitaxel, two drugs that are used as first-line treatments in advanced, recurrent, and/or metastatic cancer. In the other cell lines the compounds showed moderate activity or were inactive - with the exception of 2a, which was also found to have antiproliferative activity. Modulation of the cell cycle and apoptotic effects of active compounds were further evaluated in MCF-7 cells. Of these, 6-bromo[1,2,5]selenadiazolo[3,4-b]pyridine (2a) was the most active, with an apoptogenic effect 3.9 times higher than that of camptothecin, which was used as a positive control. Compound 2a also provoked cell cycle arrest with a significant decrease in the G?/G? phase cell population and an increase in S and G?/M cells, thus suggesting mitotic arrest prior to metaphase. PMID:21110339

Plano, Daniel; Moreno, Esther; Font, María; Encío, Ignacio; Palop, Juan Antonio; Sanmartín, Carmen

2010-11-01

93

In vitro activity of HSR-903, a new quinolone.  

PubMed Central

The in vitro activity of the new fluoroquinolone HSR-903 was compared with those of ciprofloxacin, lomefloxacin, sparfloxacin, and levofloxacin. HSR-903 inhibited 90% of methicillin-susceptible and -resistant Staphylococcus aureus (MRSA) clinical isolates at 0.78 and 1.56 microg/ml, respectively, and its activity against MRSA was 16-fold higher than those of sparfloxacin and levofloxacin and 64-fold higher than that of ciprofloxacin. The MICs at which 90% of the isolates are inhibited (MIC90s) of HSR-903 for Streptococcus pyogenes and penicillin G-susceptible and -resistant Streptococcus pneumoniae (PRSP) were 0.10, 0.05, and 0.05 microg/ml, respectively. Against PRSP, the activity of HSR-903 was 4-fold higher than that of sparfloxacin and 32- to 256-fold higher than those of the other quinolones. The MIC90 of HSR-903 for Enterococcus faecalis was 0.20 microg/ml, and HSR-903 was more active than the other quinolones against enterococci. The activity of HSR-903 against members of the family Enterobacteriaceae and Pseudomonas aeruginosa was roughly similar to that of ciprofloxacin and greater than those of the other quinolones. Against Haemophilus influenzae, Moraxella catarrhalis, and Helicobacter pylori, HSR-903 was the most potent of the quinolones tested. The activity of HSR-903 was not affected by the medium, the inoculum size, or the addition of serum, but decreased under acidic conditions, as did those of the other quinolones tested. HSR-903 exhibited rapid bactericidal action and had a good postantibiotic effect on S. aureus and P. aeruginosa. HSR-903 inhibited supercoiling by DNA gyrase from Escherichia coli, but it was much less active against human topoisomerase II.

Takahashi, Y; Masuda, N; Otsuki, M; Miki, M; Nishino, T

1997-01-01

94

In vitro antimycobacterial activities of Physalis angulata L.  

PubMed

The HIV-tuberculosis co-infection has caused an impact on tuberculosis epidemiology all over the world and the efficacies of the therapeutic schemes traditionally prescribed in the treatment of tuberculosis, such as isoniazid, rifampicin and pyrazinamide, have decreased due to the appearance of multidrug-resistant M. tuberculosis strains (MDR). This work is part of research on natural antimicrobial agents from plant extracts through bioassay-guided fractionation, by in vitro determination of the minimum inhibitory concentration (MIC) using the microdilution method with Alamar blue oxidation-reduction dye. Crude CHCl3 Physalis angulata extracts and physalin-containing fractions displayed antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium avium, Mycobacterium kansasii, Mycobacterium malmoense and Mycobacterium intracellulare. PMID:10969728

Pietro, R C; Kashima, S; Sato, D N; Januário, A H; França, S C

2000-07-01

95

Comparative in vitro activities of new quinolones against coryneform bacteria.  

PubMed

The in vitro activities of eight quinolones against 115 coryneform bacteria (20 Corynebacterium jeikeium, 15 Corynebacterium minutissimum, 15 Corynebacterium striatum, 25 Corynebacterium urealyticum, 10 Corynebacterium xerosis, 10 Corynebacterium group ANF-1, 10 Corynebacterium group 12, and 10 Listeria monocytogenes) were determined. The MICs of ciprofloxacin, ofloxacin, and sparfloxacin for 90% of C. jeikeium, C. urealyticum, and C. xerosis isolates tested were > 16 micrograms/ml. Those of BAY Y 3118 and clinafloxacin against these species were 0.5 and 1 to 2 micrograms/ml, respectively. The MICs for 90% of all 115 strains tested were 0.5 microgram/ml for BAY Y 3118, 1 microgram/ml for clinafloxacin, 2 micrograms/ml for E-5068, 4 micrograms/ml for E-5065, and > 16 micrograms/ml for ciprofloxacin, ofloxacin, sparfloxacin, and E-4868. PMID:8092851

Martínez-Martínez, L; Suárez, A I; Ortega, M C; Perea, E J

1994-06-01

96

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

2013-03-05

97

In Vitro Activity of BMS-181139, a New Carbapenem with Potent Antipseudomonal Activity  

Microsoft Academic Search

The in vitro activities of the carbapenem BMS-181139 were determined in comparison with those of imipenem, meropenem, ciprofloxacin, ceftriaxone, and vancomycin. BMS-181139 was the most active against species ofPseudomonasand related generaAlteromonasandBurkholderia, with MICs for 147 of 149 isolates of <4 mg\\/ml. Of 22 imipenem-resistant (MIC > 8 mg\\/ml) P. aeruginosa strains, only 1 required an MIC of BMS-181139 of >4

R. E. KESSLER; J. FUNG-TOMC; B. KOLEK; B. MINASSIAN; E. HUCZKO

98

In vitro antiplatelet activity of flavonoids from Leuzea carthamoides.  

PubMed

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

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

2008-01-01

99

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

100

Arrhenius temperature dependence of in vitro tissue plasminogen activator thrombolysis  

NASA Astrophysics Data System (ADS)

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

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

2007-06-01

101

Chemical constituents and in vitro antioxidant activity of Phyllanthus wightianus.  

PubMed

The whole plant of Phyllanthus wightianus (PW) was investigated for the antioxidant effects of three successive extracts: hexane (PWHE), chloroform (PWCE) and methanol (PWME), using standard in vitro models. The PWME exhibited a strong scavenging effect on 2,2-diphenyl-2-picryl hydrazyl (DPPH) free radicals and nitric oxide radical inhibition activity, due to possessing the highest content of tannins. The free radical scavenging effect of PWME was comparable with that of reference antioxidants. The extracts were subjected to isolation of their compounds: isomeric sterol mixture (1) [stigmasterol (1a), compesterol (1b) and ?-sitosterol (1c)], fredilin (2), lupeol (3), gallic acid (4), bergenin (5), geraniin (6), corilagin (7) and ellagic acid (8) were established through the use of column chromatographic methods and spectral data. The percentage of tannins was also determined and estimated using the HPLC method. The data suggest that tannins are the active antioxidant compounds of P. wightianus. This study provides proof for the ethnomedical claims and reported biological activities of this plant. The plant therefore has very good therapeutic potential. PMID:21644175

Priya, Olaganathan Siva; Viswanathan, Madepalli Byrappa Gowdu; Balakrishna, Kediki; Venkatesan, Muthappan

2011-06-01

102

In vitro antioxidant activity of coffee compounds and their metabolites.  

PubMed

In this paper we report the antioxidant activity of different compounds which are present in coffee or are produced as a result of the metabolism of this beverage. In vitro methods such as the ABTS*+ [ABTS = 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid)] decolorization assay and the oxygen radical absorbance capacity assay (ORAC) were used to assess the capacity of coffee compounds to scavenge free radicals. The importance of caffeine metabolites and colonic metabolites in the overall antioxidant activity associated with coffee consumption is shown. Colonic metabolites such as m-coumaric acid and dihydroferulic acid showed high antioxidant activity. The ability of these compounds to protect human low-density lipoprotein (LDL) oxidation by copper and 2,2'-azobis(2-amidinopropane) dihydrochloride was also explored. 1-Methyluric acid was particularly effective at inhibiting LDL oxidative modification. Different experiments showed that this caffeine metabolite is not incorporated into LDL particles. However, at physiologically relevant concentrations, it was able to delay for more than 13 h LDL oxidation by copper. PMID:17655324

Gómez-Ruiz, José Angel; Leake, David S; Ames, Jennifer M

2007-07-27

103

The in vitro activity of Vernonia amygdalina on Leishmania aethiopica.  

PubMed

Anti-leishmanial activity of chloroform and methanol extracts of Vernonia amygdalina, a plant widely used in Ethiopia for the treatment of parasitic infections, has been assessed in vitro on Leishmania aethiopica. Amastigotes were more sensitive to V. amygdalina than promastigotes. The chloroform extract had a stronger parasiticidal activity, with median effective doses (ED50) of 18.5 micrograms/ml and 13.3 micrograms/ml for promastigotes and amastigotes, than the methanol extract with ED50 of 74.4 micrograms/ml and 45.8 micrograms/ml respectively. Cytotoxicity caused by V. amygdalina to host cells, the human leukaemia monocyte THP-1 cell line, as determined by the methyl tetrazolium assay, resulted in a median lethal dose (LD50) of 19.6 micrograms/ml for the chloroform extract and 243.4 micrograms/ml for the methanol extract. In comparison, the ED50 and LD50 of pentamidine, a standard anti-leishmanial drug, were 0.5 micrograms/ml and 1.4 micrograms/ml respectively. These results indicate that V. amygdalina displays potent anti-leishmanial activities and warrants further investigation. PMID:8404883

Tadesse, A; Gebre-Hiwot, A; Asres, K; Djote, M; Frommel, D

1993-07-01

104

In Vitro Antimicrobial Activity of Cinoxacin Against 2,968 Clinical Bacterial Isolates  

PubMed Central

Cinoxacin demonstrated effective in vitro antimicrobial activity against the Enterobacteriaceae, but negligible activity against Pseudomonas aeruginosa and gram-positive cocci. The activity of cinoxacin was slightly greater than that of nalidixic acid.

Jones, R. N.; Fuchs, P. C.

1976-01-01

105

Azithromycin distinctively modulates classical activation of human monocytes in vitro  

PubMed Central

BACKGROUND AND PURPOSE Azithromycin has been reported to modify activation of macrophages towards the M2 phenotype. Here, we have sought to identify the mechanisms underlying this modulatory effect of azithromycin on human monocytes, classically activated in vitro. EXPERIMENTAL APPROACH Human blood monocytes were primed with IFN-? for 24 h and activated with LPS for 24 h. Azithromycin, anti-inflammatory and lysosome-affecting agents were added 2 h before IFN-?. Cytokine and chemokine expression was determined by quantitative PCR and protein release by ELISA. Signalling molecules were determined by Western blotting and transcription factor activation quantified with a DNA-binding ELISA kit. KEY RESULTS Azithromycin (1.5–50 µM) dose-dependently inhibited gene expression and/or release of M1 macrophage markers (CCR7, CXCL 11 and IL-12p70), but enhanced CCL2, without altering TNF-? or IL-6. Azithromycin also enhanced the gene expression and/or release of M2 macrophage markers (IL-10 and CCL18), and the pan-monocyte marker CD163, but inhibited that of CCL22. The Toll-like receptor (TLR) 4 signalling pathway was modulated, down-regulating NF-?B and STAT1 transcription factors. The inhibitory profile of azithromycin differed from that of dexamethasone, the phosphodiesterase-4 inhibitor roflumilast and the p38 kinase inhibitor SB203580 but was similar to that of the lysosomotropic drug chloroquine. Effects of concanamycin and NH4Cl, which also act on lysosomes, differed significantly. CONCLUSIONS AND IMPLICATIONS Azithromycin modulated classical activation of human monocytes by inhibition of TLR4-mediated signalling and possible effects on lysosomal function, and generated a mediator expression profile that differs from that of monocyte/macrophage phenotypes so far described.

Vrancic, M; Banjanac, M; Nujic, K; Bosnar, M; Murati, T; Munic, V; Stupin Polancec, D; Belamaric, D; Parnham, MJ; Erakovic Haber, V

2012-01-01

106

Adenovirus activates complement by distinctly different mechanisms in vitro and in vivo: indirect complement activation by virions in vivo.  

PubMed

Understanding innate immunity is key to improving the safety of adenovirus (Ad) vectors for systemic gene therapy. Ad has been shown to activate complement in vitro, but activation of complement after Ad injection in vivo has not been directly measured. Using complement protein C3a as a marker of complement activation, we show that types 2 and 5 human Ads cause rapid complement activation after intravenous injection in mice. Unexpectedly, the mechanisms in vivo were different than those in vitro. Antibodies were critical for the activation of complement by Ad in vitro, but antibodies were not required in vivo. The classical pathway was required in vitro, whereas complement activation in vivo involved both classical and nonclassical pathways as well as the reticuloendothelial system. Remarkably, the entry-deficient Ad mutant ts1 was completely unable to activate complement in vivo even though it was fully able to activate complement in vitro. This result demonstrates that the complement system senses intravenously injected Ad primarily by detecting the effects of Ad on cells rather than through direct interaction of complement with virions. Encouragingly, shielding Ad with polyethylene glycol was effective at reducing complement activation both in vitro and in vivo. In summary, intravenously injected Ad rapidly activates complement through multiple pathways, but these pathways are different than those identified by in vitro studies. In vitro studies are poorly predictive of in vivo mechanisms because Ad virions activate complement through indirect mechanisms in vivo. PMID:19321608

Tian, Jie; Xu, Zhili; Smith, Jeffrey S; Hofherr, Sean E; Barry, Michael A; Byrnes, Andrew P

2009-03-25

107

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

108

Isolation and In vitro Activation of Caenorhabditis elegans Sperm  

PubMed Central

Males and hermaphrodites are the two naturally found sexual forms in the nematode C. elegans. The amoeboid sperm are produced by both males and hermaphrodites. In the earlier phase of gametogenesis, the germ cells of hermaphrodites differentiate into limited number of sperm - around 300 - and are stored in a small 'bag' called the spermatheca. Later on, hermaphrodites continually produce oocytes1. In contrast, males produce exclusively sperm throughout their adulthood. The males produce so much sperm that it accounts for >50% of the total cells in a typical adult worm2. Therefore, isolating sperm from males is easier than from that of hermaphrodites. Only a small proportion of males are naturally generated due to spontaneous non-disjunction of X chromosome3. Crossing hermaphrodites with males or more conveniently, the introduction of mutations to give rise to Him (High Incidence of Males) phenotype are some of strategies through which one can enrich the male population3. Males can be easily distinguished from hermaphrodites by observing the tail morphology4. Hermaphrodite's tail is pointed, whereas male tail is rounded with mating structures. Cutting the tail releases vast number of spermatids stored inside the male reproductive tract. Dissection is performed under a stereo microscope using 27 gauge needles. Since spermatids are not physically connected with any other cells, hydraulic pressure expels internal contents of male body, including spermatids2. Males are directly dissected on a small drop of 'Sperm Medium'. Spermatids are sensitive to alteration in the pH. Hence, HEPES, a compound with good buffering capacity is used in sperm media. Glucose and other salts present in sperm media help maintain osmotic pressure to maintain the integrity of sperm. Post-meiotic differentiation of spermatids into spermatozoa is termed spermiogenesis or sperm activation. Shakes5, and Nelson6 previously showed that round spermatids can be induced to differentiate into spermatozoa by adding various activating compounds including Pronase E. Here we demonstrate in vitro spermiogenesis of C. elegans spermatids using Pronase E. Successful spermiogenesis is pre-requisite for fertility and hence the mutants defective in spermiogenesis are sterile. Hitherto several mutants have been shown to be defective specifically in spermiogenesis process7. Abnormality found during in vitro activation of novel Spe (Spermatogenesis defective) mutants would help us discover additional players participating in this event.

Singaravelu, Gunasekaran; Chatterjee, Indrani; Marcello, Matthew R.; Singson, Andrew

2011-01-01

109

Isolation and in vitro activation of Caenorhabditis elegans sperm.  

PubMed

Males and hermaphrodites are the two naturally found sexual forms in the nematode C. elegans. The amoeboid sperm are produced by both males and hermaphrodites. In the earlier phase of gametogenesis, the germ cells of hermaphrodites differentiate into limited number of sperm--around 300--and are stored in a small 'bag' called the spermatheca. Later on, hermaphrodites continually produce oocytes. In contrast, males produce exclusively sperm throughout their adulthood. The males produce so much sperm that it accounts for > 50% of the total cells in a typical adult worm. Therefore, isolating sperm from males is easier than from that of hermaphrodites. Only a small proportion of males are naturally generated due to spontaneous non-disjunction of X chromosome. Crossing hermaphrodites with males or more conveniently, the introduction of mutations to give rise to Him (High Incidence of Males) phenotype are some of strategies through which one can enrich the male population. Males can be easily distinguished from hermaphrodites by observing the tail morphology. Hermaphrodite's tail is pointed, whereas male tail is rounded with mating structures. Cutting the tail releases vast number of spermatids stored inside the male reproductive tract. Dissection is performed under a stereo microscope using 27 gauge needles. Since spermatids are not physically connected with any other cells, hydraulic pressure expels internal contents of male body, including spermatids. Males are directly dissected on a small drop of 'Sperm Medium'. Spermatids are sensitive to alteration in the pH. Hence, HEPES, a compound with good buffering capacity is used in sperm media. Glucose and other salts present in sperm media help maintain osmotic pressure to maintain the integrity of sperm. Post-meiotic differentiation of spermatids into spermatozoa is termed spermiogenesis or sperm activation. Shakes, and Nelson previously showed that round spermatids can be induced to differentiate into spermatozoa by adding various activating compounds including Pronase E. Here we demonstrate in vitro spermiogenesis of C. elegans spermatids using Pronase E. Successful spermiogenesis is pre-requisite for fertility and hence the mutants defective in spermiogenesis are sterile. Hitherto several mutants have been shown to be defective specifically in spermiogenesis process. Abnormality found during in vitro activation of novel Spe (Spermatogenesis defective) mutants would help us discover additional players participating in this event. PMID:21307834

Singaravelu, Gunasekaran; Chatterjee, Indrani; Marcello, Matthew R; Singson, Andrew

2011-01-31

110

In vitro and in vivo Antibacterial Activities of FK037, a New Parenteral Cephalosporin  

Microsoft Academic Search

In vitro and in vivo antibacterial activities of FK037, a new parenteral cephalosporin, were compared with those of cefpirome, ceftazidime and flo-moxef. The advantages of in vitro activity of FK037 were as follows: (1) a broad-spectrum antibacterial activity, (2) the most potent activity (MIC90: 25 ?g\\/ml) of the cephalosporins tested against highly methicillin-resistant Staphylococcus aureus (H-MRSA), (3) a strong activity

Takeshi Nishino; Masako Otsuki; Kazuo Hatano; Yutaka Nishihara

1994-01-01

111

In Vitro and In Vivo Antioxidant Activity of Bifidobacterium animalis 01 Isolated from Centenarians  

Microsoft Academic Search

Several studies reported the antioxidant activity of bifidobacteria using assays in vitro. In present study, the in vitro\\u000a and in vivo antioxidant activity of Bifidobacterium animalis 01 was investigated. Culture supernatant, intact cells, and intracellular cell-free extracts of B. animalis 01 were involved in this study. The antioxidant assays in vitro included lipid peroxidation assay, 1,1-diphenyl-2-picrylhydrazyl\\u000a (DPPH) assay, hydroxyl radical

Qian ShenNan; Nan Shang; Pinglan Li

2011-01-01

112

In vitro activity of dipteran ring glands and activation by the prothoracicotropic hormone.  

PubMed

The relationship between hemolymph ecdysteroid titer, ring gland (RG) activity, and prothoracicotropic hormone (PTTH) activation of RG in vitro has been examined during the postfeeding larval, prepupal, and pupal stages of Sarcophaga bullata. Using the ecdysteroid radioimmunoassay (RIA), two significant peaks were recorded during the red spiracular stage and during the first few hours after the formation of the white prepupa and a third large peak 9 hr later. It is postulated that these increases in ecdysteroid titer are involved in the processes of pupariation, puparial tanning, and pupation, respectively. Ring glands isolated from Sarcophaga of known ages were incubated in vitro and the secreted ecdysone was quantified by RIA. Ring glands from early red spiracular stage larvae proved to be the most active and subsequent secretory activity of the RG oscillated every 4 hr with the oscillations gradually decreasing in amplitude. RG activity returned to a basal level 24 hr after formation of the white prepupa, about the time that the hemolymph ecdysteroid titer fell to its basal level. To demonstrate PTTH activity in vitro, brains from 3- to 4-hr prepupae were chosen to activate ring glands from postfeeding larvae. Using a graded series of dilutions of PTTH extract it was shown that a dose-response relationship could be obtained for Sarcophaga similar to that demonstrated or the Manduca sexta PTTH-prothoracic gland system. In Sarcophaga maximal activation resulted in a 10-fold increase in ecdysone synthesis and secretion by ring glands stimulated with 0.5 brain eq. Half-maximal stimulation was attained with 0.2 brain eq of PTTH extract. PMID:6735164

Roberts, B; Gilbert, L I; Bollenbacher, W E

1984-06-01

113

Antioxidant Activity In Vitro of Three Constituents from Caesalpinia sappan L  

Microsoft Academic Search

Antioxidant activities of the 95% ethanol extract from Caesalpinia sappan heartwood (ECS), protosappanin A, protosappanin B, and brazilein were studied in vitro. The inhibition of the formation of malondialdehyde (MDA) and the scavenging of superoxide anions, hydrogen peroxide, and hydroxyl radicals were assayed. The experimental results show that all four substances had antioxidant activity in vitro but their capabilities differed

Jun Hu; Xiaoling Yan; Wei Wang; Hao Wu; Lei Hua; Lijun Du

2008-01-01

114

In vitro anticancer activity of stachydrine isolated from Capparis decidua on prostate cancer cell lines  

Microsoft Academic Search

In this article we report our work on the isolation, characterisation and evaluation of in vitro anticancer activity of stachydrine on solid tumour cells. The in vitro activity was assessed by MTT assay and propidium iodide (PI) staining. Further, an attempt was also made to check the effect of stachydrine on the invasion and metastasis of cancer cells by inhibiting the

Permender Rathee; Dharmender Rathee; Deepti Rathee; Sushila Rathee

2011-01-01

115

In vitro anticancer activity of stachydrine isolated from Capparis decidua on prostate cancer cell lines  

Microsoft Academic Search

In this article we report our work on the isolation, characterisation and evaluation of in vitro anticancer activity of stachydrine on solid tumour cells. The in vitro activity was assessed by MTT assay and propidium iodide (PI) staining. Further, an attempt was also made to check the effect of stachydrine on the invasion and metastasis of cancer cells by inhibiting the

Permender Rathee; Dharmender Rathee; Deepti Rathee; Sushila Rathee

2012-01-01

116

Ether lipid derivatives: Antineoplastic activity in vitro and the structure-activity relationship  

Microsoft Academic Search

The antineoplastic activity of two ether lipid derivatives, the alkyl-lysophospholipid derivative (ALP) ET-18-OCH3 and the ether-linked lipoidal amine CP-46,665 was tested in a human tumor clonogenic assay (HTCA) in vitro. CP-46,665 suppresed\\u000a the colony formation of various human tumors with a slight dose response relation after 1 hr incubation and with a clear optimum\\u000a (85% response rate) after continuous exposure

Wolfgang E. Berdela; Daniel D. Yon Hoffb; Clemens Ungerc; Hans D. Schicka; Ulrich Finka; Anneliese Reicherta; Hansjorg Eibld; Johann Rastettera

1986-01-01

117

In vitro rheological assessment of mucolytic activity induced by seaprose.  

PubMed

Proteolytic enzymes can act on the polymeric structure of the bronchial mucus, shortening the long chain of mucoproteins, DNA and other macromolecules, and thus reducing the viscosity of the mucus facilitating its expectoration. Seaprose (Flaminase, Puropharma) belongs to this class and is a proteinase from Aspergillus melleus and it is mainly used in traumatology, orthopaedics, gynaecology and pneumology. In the present study the in vitro activity of increasing concentrations (0.25, 0.5, 1%) of seaprose incubated with bronchial mucus samples (1 ml) was investigated by a rheological technique (transient test) that assesses changes in viscosity and elasticity. A dose-effect relationship between increasing concentrations of seaprose and the corresponding reductions in bronchial mucus viscosity was found. There was also a parallel reduction in elasticity after incubation with 0.5%, but an unfortunate distribution of values for 0.25 and 1% concentrations does not allow us to state whether there is a dose-effect relationship for elasticity. PMID:2277801

Braga, P C; Rampoldi, C; Ornaghi, A; Caminiti, G; Beghi, G; Allegra, L

118

Assaying different types of plant phospholipase D activities in vitro.  

PubMed

Over the past decade, tremendous progress has been made toward understanding the physiological functions of individual members of the diverse phospholipase D (PLD) family of enzymes in plants. For instance, the involvement of plant PLD members has been shown or suggested in a wide variety of the cellular and physiological processes such as regulating stomatal opening and closure; signaling plant responses to drought, salt, and other abiotic and biotic stresses; organizing microtubule and actin cytoskeletal structures; promoting pollen tube growth; cycling phosphorus; signaling nitrogen availability; regulating N-acylethanolamine stress signaling; and remodeling membrane phospholipids in plant responses to phosphate deprivation and during and after freezing. There are at least a dozen PLDs in Arabidopsis that can be separated into six classes, phospholipases D?, D?, D?, D?, D?, and D?, based on their molecular and enzymatic characteristics. Several of the classes have distinguishing enzymatic properties that can be used to discriminate among the various classes. Here we provide four variations of in vitro PLD activity assays using choline-labeled phosphatidylcholine to distinguish, to the extent possible, among the different PLD classes. PMID:23681536

Pappan, Kirk L; Wang, Xuemin

2013-01-01

119

Activation of human macrophages by mechanical ventilation in vitro.  

PubMed

Positive-pressure mechanical ventilation supports gas exchange in patients with respiratory failure but is also responsible for significant lung injury. In this study, we have developed an in vitro model in which isolated lung cells can be submitted to a prolonged cyclic pressure-stretching strain resembling that of conventional mechanical ventilation. In this model, cells cultured on a Silastic membrane were elongated up to 7% of their initial diameter, corresponding to a 12% increase in cell surface. The lung macrophage was identified as the main cellular source for critical inflammatory mediators such as tumor necrosis factor-alpha, the chemokines interleukin (IL)-8 and -6, and matrix metalloproteinase-9 in this model system of mechanical ventilation. These mediators were measured in supernatants from ventilated alveolar macrophages, monocyte-derived macrophages, and promonocytic THP-1 cells. Nuclear factor-kappaB was found to be activated in ventilated macrophages. Synergistic proinflammatory effects of mechanical stress and molecules such as bacterial endotoxin were observed, suggesting that mechanical ventilation might be particularly deleterious in preinjured or infected lungs. Dexamethasone prevented IL-8 and tumor necrosis factor-alpha secretion in ventilated macrophages. Mechanical ventilation induced low levels of IL-8 secretion by alveolar type II-like cells. Other lung cell types such as endothelial cells, bronchial cells, and fibroblasts failed to produce IL-8 in response to a prolonged cyclic pressure-stretching load. This model is of particular value for exploring physical stress-induced signaling pathways, as well as for testing the effects of novel ventilatory strategies or adjunctive substances aimed at modulating cell activation induced by mechanical ventilation. PMID:9843840

Pugin, J; Dunn, I; Jolliet, P; Tassaux, D; Magnenat, J L; Nicod, L P; Chevrolet, J C

1998-12-01

120

The effect of cisplatin on renal ATPase activity in vivo and in vitro  

Microsoft Academic Search

The effect of cisplatin on ATPase activity was determined in vitro and in vivo to investigate the correlation between nephrotoxicity and the inhibition of ATPase activity by cisplatin. Purified Na,K-ATPase was preincubated for 0–240 min with cisplatin at concentrations of 50–800 µM in vitro before the determination of enzyme activity. Although ATPase activity was reduced by cisplatin, either a high

Jiro Uozumi; Charles L. Litterst

1985-01-01

121

Amphipathic DNA Polymers Exhibit Antiherpetic Activity In Vitro and In Vivo  

Microsoft Academic Search

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

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

2008-01-01

122

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

Microsoft Academic Search

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

Alain Rival; Florence Bernard; Yvan Mathieu

1997-01-01

123

In vitro induced pinocytotic activity by a juvenile hormone analogue in oocytes of Drosophila melanogaster  

Microsoft Academic Search

Pinocytotic activity has been analyzed in Drosophila oocytes following either in vivo or in vitro exposure to horseradish peroxidase. The enzyme tracer gains access to the yolk spheres only when supplied to the oocyte in vivo. In oocytes cultured in vitro, peroxidase remains restricted to the residual coated vesicles and to the tubular profiles formed in excess in the cortical

Franco Giorgi

1979-01-01

124

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

PubMed

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

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

2012-05-01

125

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

126

[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

127

In vitro Antibacterial Activity of Lucilia sericata Maggot Secretions  

Microsoft Academic Search

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

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

2007-01-01

128

Quantitative Comparisons of in Vitro Assays for Estrogenic Activities  

Microsoft Academic Search

Substances that may act as estrogens show a broad chemical structural diversity. To thoroughly address the question of possible adverse estrogenic effects, reliable methods are needed to detect and identify the chemicals of these diverse structural classes. We compared three assays-- in vitro estrogen receptor competitive binding assays (ER binding assays), yeast-based reporter gene assays (yeast assays), and the MCF-7

Hong Fang; Weida Tong; Roger Perkins; Ana M. Soto; Nancy V. Prechtl; Daniel M. Sheehan

2000-01-01

129

Assessment of invasive activities of ovarian cancer cells in vitro  

Microsoft Academic Search

The interactions between neighboring cells and between cells and their attached substrate have long been studied in tissue culture. These in vitro studies may provide information regarding cell behavior in vivo including cell movement, cell proliferation, tissue development and wound healing. Transcellular resistance (or impedance) measurements, using various dc or ac techniques have been used to study the barrier function

Hetal Shah

2005-01-01

130

In vitro and in vivo developmental competence of dromedary (Camelus dromedarius) oocytes following in vitro fertilization or parthenogenetic activation.  

PubMed

Parthenogenetic activation of the oocyte represents an important step in the somatic cloning. The aim of the present study was to evaluate the effectiveness (in term of in vitro development) of different methods of parthenogenetic activation of dromedary oocytes. Selected cumulus-oocytes-complexes (n=1264) collected by follicular aspiration from ovaries obtained postmortem were matured in vitro (IVM) for 30 h then divided randomly into seven groups and submitted to artificial activation. Two groups were preactivated with 25 microM of calcium ionophore (CaI) for 20 min then incubated for 4h with either 2mM 6-dimethylaminopurine (6-DMAP) (group 1, n=202) or with 10 microg/mL cycloheximide (CHX) (group 2, n=194). Group 3 (n=172) and group 4 (n=184), oocytes were pretreated with 5 microM ionomycin (Iono) for 5 min then incubated with either 2mM 6-DMAP or 10 microg/mL cycloheximide for 4h, respectively. Group 5 (n=161) and group 6 (n=155) oocytes were preactivated with electrical stimulation (ES) then activated with either 2mM 6-DMAP or 10 microg/mL cycloheximide for 4h, respectively. Group 7 (n=196) oocytes were submitted to in vitro fertilization (IVF) and served as a control. All groups containing oocytes were cultured in vitro following activation or IVF, at 38.5 degrees C under 5% CO(2) in air with >95% humidity. The in vitro development rates of dromedary oocytes exposed to 6-DMAP after CaI (61%), ES (74%) and the IVF group (71%) were similar and significantly greater (P<0.05) than other treatments (10% for group 2, 47% for group 3, 27% for group 4 and 41% for group 6). The blastocyst developmental rate was better (P<0.05) in parthenotes following activation with Iono/6-DMAP (21%) compared to activation with Iono/CHX (12%). However, all were less than that achieved in the IVF group (35%). We conclude that parthenogenetic activation of camel oocytes with 6-DMAP is more effective than activation with CHX for all pre-treatments tested (CaI, Iono or ES). The viability of activated (n=15) or IVF (n=10) hatched-dromedary embryos was examined by transfer to synchronized recipients. An embryonic vesicle was seen by ultrasonography at 15 days post transfer in four females (CaI/6-DMAP: 1/5; 20%, IVF: 3/10; 30%). The only pseudopregnancy obtained with an activated embryo resorbed at 25 days. One of the females receiving the IVF produced embryos aborted at 2 months and the other two females carried to term and gave birth to healthy calves (one female and one male). This study shows that artificial activation of dromedary oocytes with CaI/6-DMAP or ES/6-DMAP is more effective than other treatments in terms of in vitro embryo development. This provides efficient activation conditions which may lead to the development of the somatic cell nuclear transfer procedure in dromedary. PMID:18789618

Khatir, H; Anouassi, A; Tibary, A

2008-07-29

131

[In vitro development of the reconstructed embryos of cattle activated after various electrofusion times].  

PubMed

The dynamics of in vitro development of reconstructed embryos of cattle after various electrofusion times was studied. The in vitro mature oocytes without zona pellucida enucleated using the touch method were taken as cytoplasts. Fetal fibroblasts were used as the nuclei source. Approximately 40% of embryos activated between 3 and 3.2 hours after electrofusion developed to blastocysts. The effectiveness of in vitro cloned embryo development did not decrease when the time between electrofusion and activation was extended up to 4-5 hours. The pattern of more successful development of in vitro reconstructed embryos was found using enucleated oocytes, excreting the first polar body after 18 hours in comparison with oocytes matured in vitro afterwards, as cytoplasts. PMID:21077361

Malenko, G P; Komissarov, A V; Stepanov, O I

132

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

133

In vitro Micro-Volume Procedure for Rapid Measurement of Erythrocytic Hexose Monophosphate Shunt Activity.  

National Technical Information Service (NTIS)

A radiometric micro-volume procedure for measurement of erythrocytic hexose monophosphate shunt (HMS) activity in intact cells in in vitro is described. The procedure is rapid, allowing 200 individual HMS determinations in a single experiment of 5 hr dura...

J. K. Baird J. E. Decker-Jackson D. E. Davidson

1984-01-01

134

In vitro activity of piperacillin, a new semisynthetic penicillin with an unusually broad spectrum of activity.  

PubMed Central

The in vitro activity of piperacillin (T-1220), a new semisynthetic derivative of aminobenzylpenicillin, was investigated. The majority of streptococci and pneumococci were inhibited by 0.12 micrograms/ml; the staphylococci and enterococci were inhibited by 2 micrograms/ml. Piperacillin was slightly more active against Neisseria and Haemophilus influenzae than was ampicillin. Piperacillin was active against all members of the Enterobacteriaceae including the Klebsiella, 58% of which were inhibited by 8 micrograms/ml. The activity of piperacillin was at least equivalent, but generally superior, to that of ampicillin or carbenicillin on species susceptible to these drugs. Most striking was its activity on Pseudomonas aeruginosa: 50% were inhibited by 2 micrograms/ml, and 83% were inhibited by 4 micrograms/ml. The minimum bactericidal concentrations were very close to the minimum inhibitory concentrations, and in most species only a slight inoculum effect was observed on the minimum bacterial values except for certain P. aeruginosa strains. A complete parallel resistance exists between piperacillin and ampicillin or carbenicillin. However, the clinical importance of this is largely mitigated by the intrinsically higher activity of piperacillin.

Verbist, L

1978-01-01

135

COMPARATIVE EVALUATION OF ALKYLPHENOLIC COMPOUNDS ON ESTROGENIC ACTIVITY IN VITRO AND IN VIVO  

Microsoft Academic Search

This study was undertaken to compare the sensitivity of screening test methods and to investigate the structure-activity relationships of the estrogenic activity of alkylphenolic compounds (APs) using in vitro and in vivo assays. Two in vitro systems, MCF-7 cell proliferation (E-screen assay) and competitive binding assay to estrogen receptor (ER), were selected to evaluate the estrogenic effects. Uterotrophic assay and

Seung Jun Kwack; Oran Kwon; Hyung Sik Kim; Soon Sun Kim; So Hee Kim; Kyung Hee Sohn; Rhee Da Lee; Chul Hoon Park; Eui Bae Jeung; Beum-Soo An; Kui Lea Park

2002-01-01

136

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

Microsoft Academic Search

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

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

2010-01-01

137

Genistein and daidzein modulate in vitro rat uterine contractile activity  

Microsoft Academic Search

The present study investigated the effect of genistein, daidzein and estradiol on in vitro rat uterine responsiveness to oxytocin (OT) and PGF2? or luprostiol (L). In a first experiment, animals were either sham-operated (SH; n=5), or ovariectomized (OVX; n=20) and orally treated for three months with either genistein (G; n=5; 10 ?g\\/g BW\\/d) or daidzein (D; n=5; 10 ?g\\/g BW\\/d)

C Picherit; M Dalle; G Néliat; P Lebecque; M. J Davicco; J. P Barlet; V Coxam

2000-01-01

138

Transport across rat trachea in vitro after exposure to cytoskeleton-active drugs in vitro or to ozone in vivo  

SciTech Connect

Full-length tracheas from Sprague-Dawley rats were exposed to cytoskeleton-active drugs in short-term organ culture, and the permeability of the tracheal epithelium was measured by instilling radiotracers into the lumen and assay of the radioactivity appearing in the external bathing medium. In vitro treatment with cytochalasin D (cyto D, 2-10 x 10(-6) M) increased the rate of movement of (14C)mannitol across the epithelium. Exposure to vinblastine (VB, 10(-4) M) alone had no significant effect. However, VB in combination with cyto D increased the permeability in a dose-dependent manner. In vivo exposure to ozone (O3, 0.8 or 2.0 ppm, 2 h) had only a slight effect on the rate of movement of the tracer as measured in vitro immediately after exposure. At 24 h postexposure there was no significant difference in permeability between ozone- and air-exposed tracheas. Prior in vivo O3 exposure sensitized the tracheas to the in vitro effects of cyto D; treatment of O3-exposed tracheas with cyto D immediately after O3 exposure produced a greater than additive effect on permeability measured in vitro. VB at concentrations up to 10(-4) M had no enhancing effect on permeability in O3-exposed tracheas. Sham exposure to clean air did not affect permeability compared to untreated (shelf) controls. Electron microscopic studies demonstrated penetration of horseradish peroxidase into intercellular spaces in the tracheas treated in vitro with cyto D or cyto D plus VB. Cyto D is known to affect intracellular microfilaments that have attachments at or near the cell surface, while VB affects microtubules associated with internal cellular structures. Therefore, the synergistic effect on tracheal permeability observed with O3 and cyto D, but not with O3 and VB, suggests that O3 may change cell surface structures associated with the microfilamentous cytoskeleton.

Rasmussen, R.E.; Bhalla, D.K.

1989-03-01

139

Comparative In Vitro Activity of ABT-773, a Novel Antibacterial Ketolide  

PubMed Central

The in vitro activities of ABT-773, erythromycin, clarithromycin, and azithromycin were compared. ABT-773 was the most active compound against macrolide-susceptible Streptococcus pneumoniae, Streptococcus pyogenes, Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Enterococcus spp. and multidrug-resistant Streptococcus pneumoniae. It also had good activity against gram-negative and atypical respiratory tract pathogens and Helicobacter pylori.

Nilius, A. M.; Bui, M. H.; Almer, L.; Hensey-Rudloff, D.; Beyer, J.; Ma, Z.; Or, Y. S.; Flamm, R. K.

2001-01-01

140

Purification and Identification of Bovine Cheese Whey Fatty Acids Exhibiting In Vitro Antifungal Activity  

Microsoft Academic Search

Milk lipids contain several bioactive factors exhib- iting antimicrobial activity against bacteria, viruses, and fungi. In the present study, we demonstrate that free fatty acids (FFA) derived from the saponification of bovine whey cream lipids are active in vitro at inhib- iting the germination of Candida albicans, a morpho- logical transition associated with pathogenicity. This activity was found to be

M. Clément; J. Tremblay; M. Lange; J. Thibodeau; P. Belhumeur

2008-01-01

141

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

142

In Vitro Activities of Newer Quinolones against Bacteroides Group Organisms  

Microsoft Academic Search

The activities of BMS-284576, clinafloxacin, moxifloxacin, sitafloxacin, trovafloxacin, imipenem, cefoxitin, and clindamycin against 589 Bacteroides fragilis group isolates were determined. The activity of BMS-284576 was comparable to that of trovafloxacin. Sitafloxacin and clinafloxacin were the most active quinolones, and moxifloxacin was the least active. B. fragilis was the most susceptible of the species, and Bacteroides vulgatus was the most resistant.

D. R. Snydman; N. V. Jacobus; L. A. McDermott; R. Ruthazer; E. Goldstein; S. Finegold; L. Harrell; D. W. Hecht; S. Jenkins; C. Pierson; R. Venezia; J. Rihs; S. L. Gorbach

2002-01-01

143

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

PubMed Central

T-2307, a novel arylamidine, has been shown to exhibit broad-spectrum antifungal activities against clinically significant pathogens. Here, we evaluated the in vitro and in vivo antimalarial activity of T-2307. The 50% inhibitory concentrations (IC50s) of T-2307 against Plasmodium falciparum FCR-3 and K-1 strains were 0.47 and 0.17 ?M, respectively. T-2307 at 2.5 to 10 mg/kg of body weight/day exhibited activity against blood stage and liver stage parasites in rodent malaria models. In conclusion, T-2307 exhibited in vitro and in vivo antimalarial activity.

Nishikawa, Hiroshi; Nomura, Nobuhiko; Mitsuyama, Junichi; Fukumoto, Shinya; Inoue, Noboru; Kawazu, Shin-ichiro

2012-01-01

144

Effect of plasmin, plasminogen activators and a plasmin inhibitor on bovine in vitro embryo production  

Microsoft Academic Search

In the present study, four experiments were conducted to investigate the possible effects of plasminogen activators (urokinase-type plasminogen activator (u-PA) and tissue-type plasminogen activator (t-PA)), plasmin, and a plasmin inhibitor (epsilon-aminocaproic acid (?-ACA)) on different stages of bovine in vitro embryo production (IVP). The concentrations of these modifiers in IVP media were conditioned according to the plasminogen activator activity of

Thomas PapanikolaouA; Georgios S. AmiridisA; Ioannis Dimitriadis; Emmanuel Vainas; Constantinos A. Rekkas

2008-01-01

145

In Vitro Activities of Doripenem and Comparator Agents against 364 Anaerobic Clinical Isolates  

PubMed Central

The in vitro activities of doripenem against 364 anaerobic isolates were measured and compared to those of ertapenem, imipenem, meropenem, ceftriaxone, and levofloxacin. All of the carbapenems were active against nearly all Bacteroides fragilis group isolates. Doripenem was either comparable to or slightly less active than imipenem and meropenem against most isolates but more active than the other penems against Clostridium difficile. Doripenem appears to have excellent activity against a broad range of anaerobes.

Wexler, Hannah M.; Engel, Adrian E.; Glass, Daniel; Li, Calida

2005-01-01

146

In vitro pharmacokinetic/pharmacodynamic modeling of voriconazole activity against Aspergillus species in a new in vitro dynamic model.  

PubMed

The pharmacodynamics (PD) of voriconazole activity against Aspergillus spp. were studied using a new in vitro dynamic model simulating voriconazole human pharmacokinetics (PK), and the PK-PD data were bridged with human drug exposure to assess the percent target (near-maximum activity) attainment of different voriconazole dosages. Three Aspergillus clinical isolates (1 A. fumigatus, 1 A. flavus, and 1 A. terreus isolate) with CLSI MICs of 0.5 mg/liter were tested in an in vitro model simulating voriconazole PK in human plasma with C(max) values of 7, 3.5, and 1.75 mg/liter and a t(1/2) of 6 h. The area under the galactomannan index-time curve (AUC(GI)) was used as the PD parameter. In vitro PK-PD data were bridged with population human PK of voriconazole exposure, and the percent target attainment was calculated. The in vitro PK-PD relationship of fAUC(0-24)-AUC(GI) followed a sigmoid pattern (global R(2) = 0.97), with near-maximum activities (10% fungal growth) observed at an fAUC(0-24) (95% confidence interval [CI]) of 18.9 (14.4 to 23.1) mg · h/liter against A. fumigatus, 26.6 (21.1 to 32.9) mg · h/liter against A. flavus, and 36.2 (27.8 to 45.7) mg · h/liter against A. terreus (F test; P < 0.0001). Target attainment for 3, 4, and 5 mg/kg-of-body-weight voriconazole dosages was 24% (11 to 45%), 80% (32 to 97%), and 93% (86 to 97%) for A. fumigatus, 12% (5 to 26%), 63% (17 to 93%), and 86% (73 to 94%) for A. flavus, and 4% (2 to 11%), 36% (6 to 83%), and 68% (47 to 83%) for A. terreus. Based on the in vitro exposure-effect relationships, a standard dosage of voriconazole may be adequate for most patients with A. fumigatus but not A. flavus and A. terreus infections, for which a higher drug exposure may be required. This could be achieved using a higher voriconazole dosage, thus highlighting the usefulness of therapeutic drug monitoring in patients receiving a standard dosage. PMID:22869563

Al-Saigh, R; Elefanti, A; Velegraki, A; Zerva, L; Meletiadis, J

2012-08-06

147

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

PubMed Central

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

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

2009-01-01

148

In Vitro Activities of Newer Quinolones against Bacteroides Group Organisms  

PubMed Central

The activities of BMS-284576, clinafloxacin, moxifloxacin, sitafloxacin, trovafloxacin, imipenem, cefoxitin, and clindamycin against 589 Bacteroides fragilis group isolates were determined. The activity of BMS-284576 was comparable to that of trovafloxacin. Sitafloxacin and clinafloxacin were the most active quinolones, and moxifloxacin was the least active. B. fragilis was the most susceptible of the species, and Bacteroides vulgatus was the most resistant. Association of specific antibiotic resistance with Bacteroides species was noted for all quinolones.

Snydman, D. R.; Jacobus, N. V.; McDermott, L. A.; Ruthazer, R.; Goldstein, E.; Finegold, S.; Harrell, L.; Hecht, D. W.; Jenkins, S.; Pierson, C.; Venezia, R.; Rihs, J.; Gorbach, S. L.

2002-01-01

149

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

2012-08-14

150

Activity of topoisomerase inhibitors against Pneumocystis carinii in vitro and in an inoculated mouse model.  

PubMed Central

Five topoisomerase II inhibitors (amsacrine [m-AMSA], two epipodophyllotoxins, and two quinolones) and the alkaloid camptothecin (a topoisomerase I inhibitor) were evaluated to assess their activities against Pneumocystis carinii. In vitro, both etoposide (VP-16) and teniposide (VM-26) at 1 microgram/ml suppressed P. carinii growth. Amsacrine was toxic to P. carinii and to the feeder cells in vitro. Camptothecin suppressed the growth of P. carinii in vitro only at 100 micrograms/ml. Studies in immunosuppressed mice demonstrated the efficacy of teniposide against P. carinii pneumonia, but successful administration of teniposide was schedule dependent with significant toxicity at therapeutic dosages.

Fishman, J A; Queener, S F; Roth, R S; Bartlett, M S

1993-01-01

151

Antithrombotic activities of pellitorine in vitro and in vivo.  

PubMed

Pellitorine (PLT), an active amide compound, is well known to possess insecticidal, antibacterial and anticancer properties. However, the anti-coagulant functions of PLT are not studied yet. Here, the anticoagulant activities of PLT 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 PLT 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 PLT resulted in prolonged aPTT and PT and inhibition of the activities of thrombin and FXa, and PLT inhibited production of thrombin and FXa in HUVECs. And PLT inhibited thrombin-catalyzed fibrin polymerization and platelet aggregation. In accordance with these anticoagulant activities, PLT elicited anticoagulant effects in mouse. In addition, treatment with PLT resulted in the inhibition of TNF-?-induced production of PAI-1 and in the significant reduction of the PAI-1 to t-PA ratio. Collectively, PLT possesses antithrombotic activities and offers bases for development of a novel anticoagulant. PMID:23973654

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

2013-08-22

152

Activation of polyunsaturated fatty acids by rat tissues in vitro  

SciTech Connect

The conversion of labeled palmitic, linoleic, arachidonic and docosahexaenoic acids to their respective acyl CoA's was studied in homogenates and microsomes of rat tissues. The highest activity, both in homogenates and microsomes, was seen in liver and heart. There was moderate activity in retina, brain, lung, kidney and testes and the lowest activity was found in spleen. Docosahexaenoic acid was activated much less actively in heart tissue than the other fatty acids. In all tissues examined, the highest activation was observed with arachidonic acid and the lowest with docosahexaenoic acid. Except for liver, those tissues that contained high levels of docosahexaenoic acid also had the highest activation capacity for this fatty acid.

Reddy, T.S.; Bazan, N.G.

1984-12-01

153

Comparative in vitro and in vivo antimicrobial activities of sitafloxacin, gatifloxacin and moxifloxacin against Mycobacterium avium.  

PubMed

Moxifloxacin exhibits therapeutic activity against Mycobacterium avium infection in mice. Since not only moxifloxacin but also another 8-methoxy quinolone, gatifloxacin, and a C-8-chloro quinolone, sitafloxacin, show favourable antimycobacterial activity in vitro, their anti-M. avium activities were compared in vivo. Minimum inhibitory concentrations (MICs), minimum bactericidal concentrations (MBCs) and mutant prevention concentrations (MPCs) of the test quinolones for M. avium were determined by microdilution in 7HSF broth. Antimicrobial activity against intracellular bacteria was measured using Mono Mac 6 human macrophages. Therapeutic efficacy of the quinolones when administered subcutaneously with or without clarithromycin plus ethambutol was assessed using mice intravenously infected with M. avium in terms of changes in bacterial loads in the lungs and spleen following infection. Based on the MICs, MBCs and MPCs, the in vitro activities of sitafloxacin and moxifloxacin were greater than that of gatifloxacin. Moxifloxacin exhibited the strongest activity against intramacrophage M. avium. When each test quinolone was administered alone to infected mice, sitafloxacin and gatifloxacin exhibited greater therapeutic efficacy than moxifloxacin based on intrapulmonary bacterial elimination. However, moxifloxacin exerted greater activity in killing bacteria in the spleen. Moxifloxacin and sitafloxacin exhibited combined effects on intrapulmonary bacterial elimination when administered to mice in combination with clarithromycin plus ethambutol. Sitafloxacin exerted the most marked combined effects in bacterial killing in the spleen. Levofloxacin displayed the lowest in vitro and in vivo activities amongst the tested quinolones. Taken together, these findings indicate that sitafloxacin and moxifloxacin exhibit favourable activities against M. avium in vitro and in vivo. PMID:21353489

Sano, Chiaki; Tatano, Yutaka; Shimizu, Toshiaki; Yamabe, Seiko; Sato, Katsumasa; Tomioka, Haruaki

2011-02-25

154

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

Microsoft Academic Search

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

Aynur Büyükbalci; Sedef Nehir El

2008-01-01

155

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

Microsoft Academic Search

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

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

2000-01-01

156

In vitro activity of Arbutus unedo against Leishmania tropica promastigotes.  

PubMed

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

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

2009-01-01

157

In Vitro Activities of Antibiotics against Plasmodium falciparum Are Inhibited by Iron  

PubMed Central

The in vitro activities of cyclines (tetracycline, doxycycline, minocycline, oxytetracycline, and rolitetracycline), macrolides (erythromycin, spiramycin, roxithromycin, and lincomycin), quinolones (norfloxacin and ofloxacin), rifampin, thiamphenicol, tobramycin, metronidazole, vancomycin, phosphomycin, and cephalosporins (cephalexin, cefaclor, cefamandole, cefuroxime, ceftriazone, cefotaxime, and cefoxitin) were evaluated on Plasmodium falciparum clones, using an isotopic, micro-drug susceptibility test. Only tetracyclines, macrolides, quinolones, and rifampin demonstrated in vitro activity against P. falciparum, which increased after a prolonged exposure (96 or 144 h). In the presence of iron (FeCl3), only the activities of tetracyclines and norfloxacin were decreased. Their in vitro activity against intraerythrocytic stages of multidrug-resistant P. falciparum and their efficacy in vivo favor the use of antibiotics as antimalarial drugs. However, due to their slow antimalarial action and to the fact that they act better after prolonged contact, they probably need to be administered in conjunction with a rapidly acting antimalarial drug, such as a short course of chloroquine or quinine.

Pradines, Bruno; Rogier, Christophe; Fusai, Thierry; Mosnier, Joel; Daries, William; Barret, Eric; Parzy, Daniel

2001-01-01

158

In vitro hypoglycemic and antimicrobial activities of Senecio leucanthemifolius Poiret  

Microsoft Academic Search

This study reports on the ?-amylase inhibitory and antimicrobial activities of Senecio leucanthemifolius Poiret. Extracts of S. leucanthemifolius were tested for their antimicrobial and antifungal activities against seven different pathogenic microorganisms using the microdilution technique. The ethyl acetate extract exhibited a strong antibiotic activity against Staphylococcus aureus with a MIC value of 31.25?µg?mL, while the n-hexane extract showed a significant

R. Tundis; M. R. Loizzo; G. A. Statti; P. J. Houghton; A. Miljkovic-Brake; F. Menichini

2007-01-01

159

In vitro antifungal activity of posaconazole against various pathogenic fungi  

Microsoft Academic Search

The antifungal activity of posaconazole (SCH56592), a new triazole antifungal, against stock cultures and fresh clinical isolates of a wide range of pathogenic fungi was compared with that of itraconazole, fluconazole and amphotericin B. Posaconazole inhibited growth of all the fungal species tested except Fusarium spp. at 1 mg\\/l or lower concentrations, showing a broad-spectrum antifungal activity. The activities of

Katsuhisa Uchida; Nobuko Yokota; Hideyo Yamaguchi

2001-01-01

160

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

2013-07-22

161

In vitro screening of leishmanicidal activity in myanmar timber extracts.  

PubMed

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

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

2004-06-01

162

T cell unresponsiveness in vitro can be due to activation in vivo.  

PubMed

During investigations into the behaviour and fate of ovalbumin (OVA)-specific CD8+ T cells in a TCR transgenic system, cytotoxic T lymphocyte (CTL) activity (as measured by classical in vitro stimulation followed by 51Cr-release assay) was found to be reduced after OVA peptide administration. This paradoxically occurred even during the peak of activation and expansion of these T cells. The reduced responsiveness occurred for both classical CTL assays and in vitro proliferation assays, and would apparently be consistent with induction of anergic or suppressor T cells. Instead, we provide evidence that in vivo peptide treatment generated activated killers which consequently killed the stimulator cells during in vitro culture, thus resulting in the unresponsive phenotype. In co-culture experiments, the proliferation and classical CTL activity were severely reduced when naive OVA-specific CD8+ T cells (OT-I) cells were co-cultured with cells from OVA peptide-treated mice. Moreover, cells obtained after peptide injection did not require in vitro stimulation to be able to kill target cells. Therefore, activation of killers in vivo should be considered as one pathway whereby unresponsiveness is found in assays requiring in vitro stimulation. PMID:9576625

Koniaras, C; Heath, W R; Lew, A M

1998-03-01

163

Evaluation of medicinal plants from Mali for their in vitro and in vivo trypanocidal activity  

Microsoft Academic Search

Water, methanol and dichloromethane extracts prepared from various parts of 40 medicinal plant species from Mali were investigated for their trypanocidal activity against Trypanosoma brucei brucei. Of a total of 165 extracts tested in vitro in the Low Inoculation Long Incubation Test (LILIT), 24 extracts showed a high trypanocidal activity. Using the Long-Term Viability Assay (LtVA) for corroboration of the

Nsekuye Bizimana; Uwe Tietjen; Karl-Hans Zessin; Drissa Diallo; Coulibaly Djibril; Matthias F. Melzig; Peter-Henning Clausen

2006-01-01

164

In Vitro Activity of Ravuconazole against 923 Clinical Isolates of Nondermatophyte Filamentous Fungi  

PubMed Central

The in vitro activities of ravuconazole against 575 clinical strains of Aspergillus spp. and 348 nondermatophyte non-Aspergillus spp. were analyzed. Ravuconazole was active against Aspergillus spp., other hyaline filamentous fungi, black molds, and some Mucorales. Species such as Scedosporium prolificans, Fusarium spp., and Scopulariopsis spp. were resistant to the triazole.

Cuenca-Estrella, Manuel; Gomez-Lopez, Alicia; Mellado, Emilia; Garcia-Effron, Guillermo; Monzon, Araceli; Rodriguez-Tudela, Juan Luis

2005-01-01

165

Engineering Active Pharmaceutical Ingredients by Spray Drying: Effects on Physical Properties and In Vitro Dissolution  

Microsoft Academic Search

Active pharmaceutical ingredients have very strict quality requirements; minor changes in the physical and chemical properties of pharmaceuticals can adversely affect the dissolution rate and therefore the bioavailability of a given drug. Accordingly, the aim of the present study was to investigate the effect of spray drying on the physical and in vitro dissolution properties of four different active pharmaceutical

R. M. Martins; M. O. Machado; S. V. Pereira; A. B. F. L. Nosari; L. A. Tacon; L. A. P. Freitas

2012-01-01

166

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

Microsoft Academic Search

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

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

2007-01-01

167

In vitro fertilization and artificial activation of eggs of the direct-developing anuran Eleutherodactylus coqui  

Microsoft Academic Search

Although much is known about the reproductive biology of pond-breeding frogs, there is comparatively little information about terrestrial-breeding anurans, a highly successful and diverse group. This study investigates the activation and in vitro fertilization of eggs of the Puerto Rican coqui frog obtained by hormonally induced ovulation. We report that spontaneous activation occurs in 34% of eggs, probably in response

Esteban Toro; Scott F Michael

2004-01-01

168

In Vitro Antimicrobial Activity of Extracts of Passiflora edulis (Passifloraceae) and Sphaeranthus indicus (Asteraceae)  

Microsoft Academic Search

The organic extracts of Passiflora edulis and Sphaeranthus indicus were evaluated for antimicrobial activity against clinically important bacteria, viz., Escherichia coli MTCC 443, Salmonella typhi MTCC 734, Staphylococus aureus MTCC 737, Bacillus subtilis, Streptococcus pyogens, Pseudomonas aeruginosa, Klebsiella pneumoniae, Proteus vulgaris, Aspergillus flavus, Pencillium restrictum, and Trichoderma viride. The in vitro antimicrobial activity was performed by agar disc diffusion method.

Asirvatham Doss; Pichai Anthoni Doss; Rangasamy Dhanabalan

2008-01-01

169

In vivo platelet activation with in vitro hyperaggregability to arachidonic acid in renal allograft recipients  

Microsoft Academic Search

In vivo platelet activation with in vitro hyperaggregability to arachidonic acid in renal allograft recipients. Renal allograft recipients were investigated to determine the extent and possible nature of in vivo platelet activation. In 92 allografted patients stable for more than 4 months' duration, intraplatelet serotonin in circulating platelets was depleted significantly. In a further 16 patients studied serially for 12

Geoffrey Frampton; Anwar Parbtani; Donatella Marchesi; Peter Duffus; Manuela Livio; Giuseppe Remuzzi; John Stewart Cameron

1983-01-01

170

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

171

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

Microsoft Academic Search

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

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

2006-01-01

172

In vitro Activity of Novel Fluoroquinolones against Streptococcus pneumoniae Isolated from Children with Acute Otitis media  

Microsoft Academic Search

Background: In recent years, novel fluoroquinolones with improved activity against gram-positive organisms have been introduced into clinical practice. These drugs may be of potential benefit for the treatment of pneumococcal otitis media, including infections caused by organisms resistant to conventional drugs. Methods: In vitro activity of 6 fluoroquinolones against 77 pneumococcal isolates from middle-ear fluid was determined by the E

P. Yagupsky; O. Katz; N. Peled; R. Dagan

2001-01-01

173

In vitro effect of some anthelmintics on lactate dehydrogenase activity of Cotylophoron cotylophorum (Digenea: Paramphistomidae)  

Microsoft Academic Search

Effects of praziquantel (PZQ), levamisole (LEV), mebendazole (MBZ), fenbendazole (FBZ) and albendazole (ABZ) on the lactate dehydrogenase (LDH) activity of Cotylophoron cotylophorum were studied in vitro. Maximum levels of inhibition of LDH catalysing both oxidation and reduction reactions were observed in PZQ- and LEV-treated worms. Similarly, benzimidazoles — MBZ, FBZ and ABZ — have also significantly inhibited the activity of

L Veerakumari; N Munuswamy

2000-01-01

174

In vitro activity of sitafloxacin compared with several fluoroquinolones against Streptococcus anginosus and Streptococcus constellatus  

Microsoft Academic Search

The in vitro activities of sitafloxacin and seven other fluoroquinolones a (ciprofloxacin, tosufloxacin, sparfloxacin, levofloxacin, T-3811ME, moxifloxacin and trovafloxacin) were examined by the microdilution method against 79 clinically isolated ‘Streptococcus milleri’ group (SMG) microorganisms. No statistically significant differences were found between the minimum inhibitory concentrations (MIC50 and MIC90) against Streptococcus anginosus and Streptococcus constellatus. Sitafloxacin was the most active agent

Natsuo Yamamoto; Jiro Fujita; Takashi Shinzato; Futoshi Higa; Masao Tateyama; Masato Tohyama; Isamu Nakasone; Nobuhisa Yamane

2006-01-01

175

In Vitro Antibacterial Activity of DX-619, a Novel Des-Fluoro(6) Quinolone  

PubMed Central

The in vitro activities of DX-619, des-fluoro(6) quinolone, against 1,208 clinical isolates were examined. DX-619 was particularly potent against staphylococci, including ciprofloxacin- and methicillin-resistant strains; the MIC at which 90% of the strains tested were inhibited was 0.5 ?g/ml. In addition, DX-619 was also active against gram-negative bacteria.

Fujikawa, Katsuko; Chiba, Megumi; Tanaka, Mayumi; Sato, Kenichi

2005-01-01

176

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

177

Phytochemical investigation and evaluation of in vitro free radical scavenging activity of Tabernaemontana divaricata Linn  

Microsoft Academic Search

We evaluate the in vitro free radical scavenging activity of the leaves of Tabernaemontana divaricata Linn. Petroleum ether, ethanol and aqueous extracts of T. divaricata were prepared with successive extraction in a soxhlet apparatus. Each extract was selected to study the free radical scavenging activity by superoxide scavenging assay method. It was found that the aqueous extract contained carbohydrates, glycosides,

Sachin Jain; Avijeet Jain; Neetesh Jain; D. K. Jain; Neelam Balekar

2010-01-01

178

[In vitro antifungal activity of nitroxoline. Preliminary clinical results].  

PubMed

Nitroxoline is an oxyquinoline derivative with a large antifungical activity. The fungistatic activity of nitroxoline is greater against Candida albicans than against Torulopsis glabrata, Candida tropicalis and Candida krusei. The MIC are compatible with urinary concentrations of nitroxoline. These preliminary clinical results favor the use of nitroxoline in the management of fungal urinary tract infections. PMID:3309833

Cancet, B; Amgar, A

1987-06-01

179

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

180

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

PubMed Central

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

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

2013-01-01

181

Developmental changes in the in vitro activated regenerative activity of primitive mammary epithelial cells.  

PubMed

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

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

2013-08-13

182

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

183

In vitro differentiation of human macrophages with enhanced antimycobacterial activity  

PubMed Central

Mycobacterium tuberculosis causes widespread, persistent infection, often residing in macrophages that neither sterilize the bacilli nor allow them to cause disease. How macrophages restrict growth of pathogens is one of many aspects of human phagocyte biology whose study relies largely on macrophages differentiated from monocytes in vitro. However, such cells fail to recapitulate the phenotype of tissue macrophages in key respects, including that they support early, extensive replication of M. tuberculosis and die in several days. Here we found that human macrophages could survive infection, kill Mycobacterium bovis BCG, and severely limit the replication of M. tuberculosis for several weeks if differentiated in 40% human plasma under 5%–10% (physiologic) oxygen in the presence of GM-CSF and/or TNF-? followed by IFN-?. Control was lost with fetal bovine serum, 20% oxygen, M-CSF, higher concentrations of cytokines, or premature exposure to IFN-?. We believe that the new culture method will enable inquiries into the antimicrobial mechanisms of human macrophages.

Vogt, Guillaume; Nathan, Carl

2011-01-01

184

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

185

Activity of armillarisin B in vitro against plant pathogenic fungi.  

PubMed

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

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

186

In vitro antibacterial activity of some plant essential oils  

PubMed Central

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

Prabuseenivasan, Seenivasan; Jayakumar, Manickkam; Ignacimuthu, Savarimuthu

2006-01-01

187

Quantitative correspondence between the in vivo and in vitro activity of teratogenic agents.  

PubMed Central

We have tested 74 teratogenic and 28 nonteratogenic agents in a recently developed in vitro teratogen assay system. The assay identifies teratogens by their ability to inhibit attachment of ascites tumor cells to plastic surfaces coated with concanavalin A. There is a qualitative agreement between in vivo animal data and in vitro activity for 81 of the 102 agents (79%). Quantitative analysis shows a highly significant correlation coefficient of 0.69 between the inhibitory in vitro dose and the lowest reported teratogenic dose for 54 of the 60 inhibitory teratogens. The doses analyzed ranged over 5 orders of magnitude. We interpret these results to mean that attachment inhibition in concert with other, complementary, in vitro assay systems can become a useful method for the assessment of the teratogenic potential of environmental agents.

Braun, A G; Buckner, C A; Emerson, D J; Nichinson, B B

1982-01-01

188

Rice dehydrin K-segments have in vitro antibacterial activity.  

PubMed

Dehydrins are groups of plant proteins that have been shown to response to various environmental stimuli such as dehydration, elevated salinity, and low temperature. However, their roles in plant defense against microbes have not been demonstrated. In an attempt to discover plant antimicrobial proteins, we have screened a rice cDNA library and isolated several cDNAs coding for dehydrins. Protein extracts from Escherichia coli expressing these cDNAs were tested for their activity against Gram-positive bacteria (Bacillus pumilus, B. subtilis, Staphylococcus aureus, and Sarcina lutea) and Gram-negative bacteria (Escherichia coli and Xanthomonas oryzae pv. oryzae). The results indicate that the crude protein extracts exhibited antibacterial activities against the Gram-positive bacteria. However, dehydrins purified by immunoaffinity chromatography were not active against the bacteria. To pinpoint the dehydrin peptides that were responsible for the bactericidal activity, we expressed DNA sequences coding for truncated dehydrins containing either K- or S-segment and found that K-segment peptides, and not S-segment, were responsible for the antibacterial activities against Gram-positive bacteria. Antibacterial assay with synthetic K-segments indicated that the peptides inhibited growth of B. pumilus with minimum inhibition concentration and minimum bactericidal concentration of 130 and 400 ?g/ml, respectively. PMID:21639844

Zhai, C; Lan, J; Wang, H; Li, L; Cheng, X; Liu, G

2011-06-01

189

[The antagonistic activity of bifidobacteria in vitro and in vivo studied by using gnotobiological technology].  

PubMed

The antagonistic activity of 4 strains of bifidobacteria (B. adolescentis 2 F1, B. longum Z4, B. breve R2 and B. bifidum G1), isolated from the vagina of healthy females of the reproductive age, with respect to Escherichia coli, Klebsiella ozaenae, Staphylococcus aureus, Enterococcus faecalis, Pseudomonas aeruginosa and Gardnerella vaginalis were studied in vitro and in vivo. The in vitro experiments revealed that all above-mentioned bifidobacteria were capable of inhibiting the growth of all indicator bacterial strains. Still of all the bifidobacteria under study had different levels of activity. B. adolescentis strain 2 F1 exhibited the highest inhibiting activity in vitro. In contrast to in vitro experiments, in vivo experiments with B. breve R2 demonstrated its high antagonistic activity with respect to E. coli. The data thus obtained indicate that in the study of antagonistic activity the use of the in vivo model as also expedient, for it is mainly in vivo that probiotic preparations show their activity. PMID:10852027

Korshunov, V M; Urtaeva, Z A; Smeianov, V V; Efimov, B A; Sarkisov, S E; Krymshokalova, Z A; Ba?nov, N A; Pikina, A P; Korshunova, O V

190

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

191

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

192

In vitro antimicrobial activity of pistachio (Pistacia vera L.) polyphenols.  

PubMed

We investigated the antimicrobial properties of polyphenol-rich fractions derived from raw shelled and roasted salted pistachios. American Type Culture Collection (ATCC), food and clinical isolates, of Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Pseudomonas mirabilis), Gram-positive bacteria (Listeria monocytogenes, Enterococcus hirae, Enterococcus faecium, Bacillus subtilis, Staphylococcus epidermidis, Staphylococcus aureus), the yeasts Candida albicans and Candida parapsilosis and the fungus Aspergillus niger were used. Pistachio extracts were active against Gram-positive bacteria with a bactericidal effect observed against L. monocytogenes (ATCC strains and food isolates), S. aureus and MRSA clinical isolates. Extracts from raw shelled pistachios were more active than those from roasted salted pistachios. The bactericidal activity of pistachio extracts could be used to help control the growth of some microorganisms in foods to improve safety and may find application as a topical treatment for S. aureus. PMID:23350629

Bisignano, Carlo; Filocamo, Angela; Faulks, Richard M; Mandalari, Giuseppina

2013-02-11

193

Preparation and in vitro anticancer activity of oxymatrine mixed micellar nanoparticles.  

PubMed

The aim of this study was to prepare oxymatrine (OMT) mixed micellar nanoparticles to delay release of the drug and enhance its cytotoxicity against cancer cells. A co-solvent evaporation method using lipoid E80, lipoid S75, MPEG-PLA and Poloxamer 188 was chosen to prepare the OMT formulation, and its release characteristics, cytotoxic activity in vitro and physical characteristics were evaluated. The results showed that OMT mixed micellar nanoparticles have sustained release and cytotoxic activity in vitro to the SMMC-7721 cell line. PMID:21812325

Jin, Nan; Zhao, Yong-Xing; Deng, Shu-Hua; Sun, Qian

2011-07-01

194

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

PubMed

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

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

1995-12-15

195

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

Microsoft Academic Search

The improvement of the rutin photostability and its prolonged in vitro antioxidant activity were studied by means of its association\\u000a with nanostructured aqueous dispersions. Rutin-loaded nanocapsules and rutin-loaded nanoemulsion showed mean particle size\\u000a of 124.30 ± 2.06 and 124.17 ± 1.79, respectively, polydispersity index below 0.20, negative zeta potential, and encapsulation\\u000a efficiency close to 100%. The in vitro antioxidant activity was evaluated by the

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

2010-01-01

196

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

2011-10-10

197

In Vitro and In Vivo Anticancer Activity of (+)-Spongistatin 1  

PubMed Central

The marine natural product (+)-spongistatin 1 is an extremely potent growth inhibitory agent having activity against a wide variety of cancer cell lines, while exhibiting low cytotoxicity against quiescent human fibroblasts. Consistent with a microtubule-targeting mechanism of action, (+)-spongistatin 1 causes mitotic arrest in DU145 human prostate cancer cells. More importantly, (+)-spongistatin 1 exhibits significant in vivo antitumor activity in the LOX-IMVI human melanoma xenograft model. (+)-Spongistatin 1 is thus an important class of microtubule targeting anticancer agent that warrants further investigation.

Xu, Qunli; Huang, Kuan-Chun; TenDyke, Karen; Marsh, Joanne; Liu, Junke; Qiu, Dayong; Littlefield, Bruce A.; Nomoto, Kenichi; Atasoylu, Onur; Risatti, Christina A.; Sperry, Jeffrey B.; Smith III, Amos B.

2011-01-01

198

In vitro and in vivo anticancer activity of (+)-spongistatin 1.  

PubMed

The marine natural product (+)-spongistatin 1 is an extremely potent growth inhibitory agent having activity against a wide variety of cancer cell lines, while exhibiting low cytotoxicity against quiescent human fibroblasts. Consistent with a microtubule-targeting mechanism of action, (+)-spongistatin 1 causes mitotic arrest in DU145 human prostate cancer cells. More importantly, (+)-spongistatin 1 exhibits significant in vivo antitumor activity in the LOX-IMVI human melanoma xenograft model. (+)-Spongistatin 1 is, thus, an important class of microtubule targeting anticancer agent that warrants further investigation. PMID:21868519

Xu, Qunli; Huang, Kuan-Chun; Tendyke, Karen; Marsh, Joanne; Liu, Junke; Qiu, Dayong; Littlefield, Bruce A; Nomoto, Kenichi; Atasoylu, Onur; Risatti, Christina A; Sperry, Jeffrey B; Smith, Amos B

2011-09-01

199

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

200

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

201

Activation of arylamines to mutagenic product(s) by two in vitro plant systems  

Microsoft Academic Search

Plant activation of three isomers of phenylenediamine, o-, m- and p-phenylenediamine, has been studied. Two in vitro plant systems have been used: Persea americana S117 with mixed-function oxidase (MFO) and peroxidase activities, and Zea mays S9 which contains only peroxidase activity. As genetic endpoint, the classical Salmonella tester strains, TA98 and TA100, their derivatives with high O-acetyltransferase levels (YG1024 and

Carles Chiapella; José Antonio Moreno; Rodrigo D Radovan; Nathalie Gaubert; Montserrat Llagostera

1997-01-01

202

Comparative in vitro and in vivo antimicrobial activities of sitafloxacin, gatifloxacin and moxifloxacin against Mycobacterium avium  

Microsoft Academic Search

Moxifloxacin exhibits therapeutic activity against Mycobacterium avium infection in mice. Since not only moxifloxacin but also another 8-methoxy quinolone, gatifloxacin, and a C-8-chloro quinolone, sitafloxacin, show favourable antimycobacterial activity in vitro, their anti-M. avium activities were compared in vivo. Minimum inhibitory concentrations (MICs), minimum bactericidal concentrations (MBCs) and mutant prevention concentrations (MPCs) of the test quinolones for M. avium were

Chiaki Sano; Yutaka Tatano; Toshiaki Shimizu; Seiko Yamabe; Katsumasa Sato; Haruaki Tomioka

2011-01-01

203

In vitro Activity of Biapenem against Recent Gram-Negative and Gram-Positive Clinical Isolates  

Microsoft Academic Search

The in vitro activity of biapenem, a new carbapenem, against 535 clinical recent isolates was compared with those of other antibiotics. Biapenem showed broad-spectrum activity against gram-negative and gram-positive clinical isolates. The new carbapenem was more active than imipenem against members of the family Enterobacteriaceae with MIC90S ranging from 0.12 to 2 mg\\/l and from 0.25 to 4 mg\\/l, respectively.

Giovanni Bonfiglio; Giuseppa Maccarone; Maria Lina Mezzatesta; Angela Privitera; Vincenzo Carciotto; Maria Santagati; Stefania Stefani; Giuseppe Nicoletti

1997-01-01

204

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

205

In vitro Remineralization of Caries Lesions Treated with Surface-Active Phosphates  

Microsoft Academic Search

Intact human enamel was demineralized in vitro to obtain artificial caries lesions. Part of the lesions was then treated with different surface-active compounds and remineralized with a remineralizing solution. The other part of the lesions was de- and remineralized in the same way, but was not treated with a surface-active compound. The results indicate that none of the surface-active compounds

J. M. P. M. Borggreven; P. C. Lammers; T. Hoeks; B. Zwanenburg; F. C. M. Driessens

1991-01-01

206

In Vitro Activities of Linezolid against Multiple Nocardia Species  

PubMed Central

Linezolid was tested by broth microdilution against 140 clinical Nocardia isolates belonging to seven species. The MIC at which 50% of the strains are inhibited (MIC50) and MIC90 for all species other than Nocardia farcinica were 2 and 4 ?g/ml. Linezolid is the first antimicrobial agent demonstrated to be active against all Nocardia species.

Brown-Elliott, Barbara A.; Ward, Shelby C.; Crist, Christopher J.; Mann, Linda B.; Wilson, Rebecca W.; Wallace, Richard J.

2001-01-01

207

Metabolic activation of drugs in mutagenicity tests in vitro  

Microsoft Academic Search

The metabolic pathways of chemical compounds of pharmaceutical interest are reviewed in relation to the role of activation and detoxification in the process of mutagenicity. The properties and subcellular localization of the enzymes involved are given together with the main reactions they catalyze.

M. B. Roberfroid

1980-01-01

208

Bromelain Activates Murine Macrophages and Natural Killer Cells in Vitro  

Microsoft Academic Search

The innate immune response is critical for effective immunity against most pathogens. In this study, we show that bromelain, a mixture of cysteine proteases, can enhance IFN-?-mediated nitric oxide and TNF? production by macrophages. Bromelain's effect was independent of endotoxin receptor activation and was not caused by direct modulation of IFN-? receptors. Instead, bromelain either enhanced or acted synergistically with

Christian R. Engwerda; Deborah Andrew; Michaela Murphy; Tracey L. Mynott

2001-01-01

209

In vitro study of antioxidant activity of Syzygium cumini fruit  

Microsoft Academic Search

Food rich in antioxidants plays an essential role in the prevention of diseases. The fruits of wild Indian Syzygium cumini (L.) Skeels (Myrtaceae), also known as black plum, are edible. Traditionally they are also used to cure a number of ailments. In this paper, the antioxidant activity of the fruit skin has been analysed using different assays, such as hydroxyl

Archana Banerjee; Nabasree Dasgupta; Bratati De

2005-01-01

210

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

211

Inhibition of catalase activity in vitro by diesel exhaust particles  

SciTech Connect

The effect of diesel exhaust particles (DEP) on the activity of catalase, an intracellular anti-oxidant, was investigated because H{sub 2}O{sub 2} is a cytotoxic oxidant, and catalase released from alveolar cells is an important antioxidant in the epithelial lining fluid in the lung. DEP inhibited the activity of bovine liver catalase dose-dependently, to 25-30% of its original value. The inhibition of catalase by DEP was observed only in the presence of anions such as Cl{sup {minus}}, Br{sup {minus}}, or thiocyanate. Other anions, such as CH{sub 3}COO{sup {minus}} or SO{sub 4}{sup {minus}}, and cations such as K{sup +}, Na{sup +}, Mg{sup 2+}, or Fe{sup 2+}, did not affect the activity of catalase, even in the presence of DEP extract. Catalase from guinea pig alveolar cells and catalase from red blood cells were also inhibited by DEP extracts, as was catalase from bovine liver. These results suggest that DEP taken up in the lung and located on alveolar spaces might cause cell injury by inhibiting the activity of catalase in epithelial lining fluid, enhancing the toxicity of H{sub 2}O{sub 2} generated from cells in addition to that of O{sub 2}{sup {minus}} generated by the chemical reaction of DEP with oxygen. 10 refs., 6 figs.

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

1996-02-09

212

Synthesis, cytotoxicity and in vitro antileishmanial activity of naphthothiazoles.  

PubMed

The leishmaniasis is a spectral disease caused by the protozoan Leishmania spp., which threatens millions of people worldwide. Current treatments exhibit high toxicity, and there is no vaccine available. The need for new lead compounds with leishmanicidal activity is urgent. Considering that many lead leishmanicidal compounds contain a quinoidal scaffold and the thiazole heterocyclic ring is found in a number of antimicrobial drugs, we proposed a hybridization approach to generate a diverse set of semi-synthetic heterocycles with antileishmanial activity. We found that almost all synthesized compounds demonstrated potent activity against promastigotes of Leishmania (Viannia) braziliensis and reduced the survival index of Leishmania amastigotes in mammalian macrophages. Furthermore, the compounds were not cytotoxic to macrophages at fivefold higher concentrations than the EC50 for promastigotes. All molecules fulfilled Lipinski's Rule of Five, which predicts efficient orally absorption and permeation through biological membranes, the in silico pharmacokinetic profile confirmed these characteristics. The potent and selective activity of semi-synthetic naphthothiazoles against promastigotes and amastigotes reveals that the 2-amino-naphthothiazole ring may represent a scaffold for the design of compounds with leishmanicidal properties and encourage the development of drug formulation and new compounds for further studies in vivo. PMID:23421616

de Toledo, Juliano S; Junior, Paulo E S; Manfrim, Viviane; Pinzan, Camila F; de Araujo, Alexandre S; Cruz, Angela K; Emery, Flavio S

2013-06-01

213

Mechanism of flavoxate antispasmodic activity comparative in vitro studies.  

PubMed

In order to clarify the pharmacological activity of flavoxate, its effect on the tone and spontaneous activity of the guinea-pig isolated ureter and of the muscle strip from rat urinary bladder were studied. Flavoxate, as well as papaverine, reduced all three parameters considered on the guinea-pig isolated ureter, namely: peristaltic motility, endoluminal pressure and longitudinal muscle contractility. In the same test, verapamil (a calcium antagonist), emepronium and atropine (both anticholinergic drugs) were used for comparison. Using strips of rat urinary bladder depolarized by KCl, flavoxate, papaverine and verapamil displayed a relaxant activity, while anticholinergic compounds such as atropine, hyoscine and emepronium failed to relax this tissue. In another series of experiments the effects of flavoxate and anticholinergic drugs on the contraction elicited by vagal electrical stimulation of the guinea-pig isolated stomach in toto were assayed. The results obtained suggest that the action of flavoxate is due to direct smooth muscle relaxation and does not involve anticholinergic activity. PMID:4026456

Cazzulani, P; Panzarasa, R; De Stefani, C; Graziani, G

1985-04-01

214

Phasic Vagal Sensory Feedback Transforms Respiratory Neuron Activity In Vitro  

Microsoft Academic Search

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

Nicholas M. Mellen; Jack L. Feldman

2001-01-01

215

Assaying the kinase activity of LRRK2 in vitro.  

PubMed

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

Lewis, Patrick A

2012-01-18

216

In vitro augmentation of natural killer cell activity by manganese chloride  

SciTech Connect

The in vitro cultivation of murine spleen cells with MnCl/sub 2/ resulted in the enhancement of natural killer (NK) cell activity as measured in a 4-h /sup 51/Cr-release assay. Optimal enhancement of NK activity was observed at concentrations of 10-20 ..mu..g MnCl/sub 2//culture (72-144 ..mu..M Mn/sup 2 +/). Enhancement of NK activity by MnCl/sub 2/ was not associated with any changes in the number or viability of cells following culture. The addition of antiasialo GM/sub 1/ antibody and complement to spleen cell cultures completely abrogated the enhancement of NK activity by MnCl/sub 2/. The enhancement of NK activity by MnCl/sub 2/ in vitro was accompanied by interferon induction. The addition of rabbit antimouse interferon to spleen cells cultured with MnCl/sub 2/ reduced NK activity. NK activity in cultures treated with MnCl/sub 2/ was also reduced upon removal of plastic adherent cells. However, restoration of enhanced NK activity by addition of adherent cells to nonadherent cells in the presence of MnCl/sub 2/ was not observed. Similar effects of NK activity were observed with polyinosinic-polycytidylic acid (Poly I x C), a known interferon inducer and NK enhancer. The results demonstrate that murine splenic NK activity is enhanced in vitro by MnCl/sub 2/ and that this enhancement may be mediated by interferon induction. The results also suggest that in vitro enhancement of NK activity by MnCl/sub 2/, as with Poly I x C, may require participation of an adherent cell population for NK augmentation.

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

1986-01-01

217

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

218

In vitro antimicrobial activity of peroxide-based bleaching agents.  

PubMed

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

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

2007-06-01

219

In vitro phosphatidylcholine peroxidation mediated by activated human neutrophils.  

PubMed

Activated human polymorphonuclear leukocytes (PMNs) mediated peroxidation of dilinoleoyl phosphatidylcholine (DPLC) liposomes. Concentration-response effects were demonstrated for both PMNs and DLPC in the system studied. Chelated iron facilitated peroxidation threefold. Superoxide dismutase variably inhibited peroxidation, but never completely. Although O2-. synthesis ceased 30-40 min after PMN stimulation, lipid peroxidation continued for an additional 30-60 min, suggesting that PMNs may initiate peroxidation which subsequently becomes autocatalytic. Enhanced PMN-mediated DLPC peroxidation was noted in acidic media. Separation of DLPC reaction products by high pressure liquid chromatography demonstrated the de novo appearance of conjugated diene species. Preliminary specific ion monitoring mass spectroscopy analysis of gas chromatography fractions of reaction products (derivatized to fatty acid methyl esters/trimethylsilane hydroxyl ethers) indicated that PMN-generated oxyradicals resulted in production of conjugated 9- and 13-hydroperoxy DLPC derivatives. These results illustrate directly how activated PMNs may participate in host autoinjury by mediating phospholipid peroxidation. PMID:1934323

Zimmerman, J J; Lewandoski, J R

1991-06-01

220

Human monocyte activation by biologic and biodegradable meshes in vitro  

Microsoft Academic Search

Background  Inflammation and wound healing play critical roles in the integration of biologic and biodegradable meshes (BMs) at hernia\\u000a repair sites. Monocytes\\/macrophages (M\\/MŘs) are key cells controlling inflammation and wound healing. These cells release\\u000a inflammatory cytokines and growth factors such as interleukin (IL)-1?, IL-6, IL-8, and vascular endothelial growth factor\\u000a (VEGF) upon activation. Although BMs have been increasingly used in hernia

Sean B. Orenstein; Yi Qiao; Manjot Kaur; Ulrike Klueh; Don L. Kreutzer; Yuri W. Novitsky

2010-01-01

221

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

222

In vitro Antibacterial and Antifungal Activity of Borreria articularis  

Microsoft Academic Search

Petroleum ether extract, chloroform extract, ethyl acetate extract, ethyl alcohol extract and a pure compound 6-methyl-5-cyclodecen-1-ol obtained from aerial parts of Borreria articularis were studied for their antimicrobial activities against eleven human pathogenic bacteria and four human pathogenic fungi using disc diffusion and poisoned food method respectively. Ethyl acetate extract, ethanol extracts and the pure compound 6-methyl-5-cyclodecen-1-ol exhibited good antibacterial

Razia Sultana; M Shafiqur Rahman; M Nazrul; Islam Bhuiyan; Jaripa Begum; M Nural Anwar

2008-01-01

223

In Vitro Antioxidant Activity of Brazilian Wines and Grape Juices  

Microsoft Academic Search

The antioxidant activity of eight commercial Brazilian wines and two grape juices was evaluated using the inhibition of lipid oxidation (average 25.75 to 59.66%) and the reducing power methods. The total phenolic content was determined (average 1647, 803 and 305 mg\\/L\\/GAE for red, pink and white wines, respectively, and 1150 mg\\/L\\/GAE for grape juices), and the resulting values were well correlated with

Emília Y. Ishimoto; Carlos K. B. Ferrari; Deborah H. M. Bastos; Elizabeth A. F. S. Torres

2006-01-01

224

In vitro antibacterial activity of some plant essential oils  

Microsoft Academic Search

BACKGROUND:: To evaluate the antibacterial activity of 21 plant essential oils against six bacterial species. METHODS:: The selected essential oils were screened against four gram-negative bacteria (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Proteus vulgaris) and two gram-positive bacteria Bacillus subtilis and Staphylococcus aureus at four different concentrations (1:1, 1:5, 1:10 and 1:20) using disc diffusion method. The MIC of the

Seenivasan Prabuseenivasan; Manickkam Jayakumar; Savarimuthu Ignacimuthu

2006-01-01

225

In vitro effects of acetylcholinesterase reactivators on monoamine oxidase activity.  

PubMed

Administration of acetylcholinesterase (AChE) reactivators (oximes) is usually used in order to counteract the poisoning effects of nerve agents. The possibility was suggested that oximes may show some therapeutic and/or adverse effects through their action in central nervous system. There are no sufficient data about interaction of oximes with monoaminergic neurotransmitter's systems in the brain. Oxime-type AChE reactivators pralidoxime, obidoxime, trimedoxime, methoxime and HI-6 were tested for their potential to affect the activity of monoamine oxidase of type A (MAO-A) and type B (MAO-B) in crude mitochondrial fraction of pig brains. The compounds were found to inhibit fully MAO-A with half maximal inhibitory concentration (IC(50)) of 0.375 mmol/l (pralidoxime), 1.53 mmol/l (HI-6), 2.31 mmol/l (methoxime), 2.42 mmol/l (obidoxime) and 4.98 mmol/l (trimedoxime). Activity of MAO-B was fully inhibited by HI-6 and pralidoxime only with IC(50) 4.81 mmol/l and 11.01 mmol/l, respectively. Methoxime, obidoxime and trimedoxime displayed non-monotonic concentration dependent effect on MAO-B activity. Because oximes concentrations effective for MAO inhibition could not be achieved in vivo at the cerebral level, we suppose that oximes investigated do not interfere with brain MAO at therapeutically relevant concentrations. PMID:21195145

Fišar, Zden?k; Hroudová, Jana; Korábe?ný, Jan; Musílek, Kamil; Ku?a, Kamil

2010-12-30

226

Steady states and dynamics of urokinase-mediated plasmin activation in silico and in vitro.  

PubMed

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. PMID:22004735

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

2011-10-19

227

In vivo and in vitro effects of aluminum on the activity of mouse brain acetylcholinesterase.  

PubMed

Cholinesterases are a large family of enzymatic proteins widely distributed throughout both neuronal and non-neuronal tissues. In Alzheimer's disease (AD), analytical as well as epidemiological studies suggest an implication of an abnormal focal accumulation of aluminum in the brain. In this devastating disease, aluminum may interfere with various biochemical processes including acetylcholine metabolism, and can thus act as a possible etiopathogenic cofactor. Acetylcholinesterase (AChE) exists in several molecular forms that differ in solubility and mode of membrane attachment rather than in catalytic activity. Mice were treated orally with aluminum chloride or aluminum lactate (Al(lac)(3)), and AChE activity in their brain homogenates was then assayed. Results showed that this in vivo treatment augmented the activity of the enzyme. An activating effect was also observed in vitro, when the aluminum compounds were added directly to mouse brain homogenates. However, the activating effect observed in vivo was much more marked than that observed in vitro. In addition, the activation produced by Al(lac)(3) was higher than that obtained after aluminum chloride treatment. Kinetics measurements of AChE activity in the absence and presence of treatment with aluminum both in vivo and in vitro are reported. The influence of the metal speciation on enzymatic activity is discussed in relation to a possible implication of aluminum in some neurodegenerative diseases. PMID:12372547

Zatta, P; Ibn-Lkhayat-Idrissi, M; Zambenedetti, P; Kilyen, M; Kiss, T

2002-10-15

228

Cefamandole: Antimicrobial Activity In Vitro of a New Cephalosporin  

PubMed Central

Cefamandole, a new cephalosporin derivative, was found to have a broad spectrum of activity against a cross-section of both gram-positive and gram-negative bacteria isolated from clinical material. Gram-positive cocci, except for Streptococcus faecalis, were very susceptible. Penicillin G-resistant Staphylococcus aureus also was susceptible to cefamandole. Minimal bactericidal concentrations for gram-positive cocci approximated the minimal inhibitory concentrations. Strains of Haemophilus influenzae were very susceptible to the drug. Most strains of Escherichia coli, Klebsiella sp., and Proteus sp. were inhibited by low concentrations. Increasing resistance occurred with larger inocula. Strains of Pseudomonas sp. were resistant to cefamandole.

Meyers, Burt R.; Leng, Bernard; Hirschman, Shalom Z.

1975-01-01

229

[In vitro study of the antimutagenic activity of alphahederin].  

PubMed

Authors have studied the antimutagenic power of alphahederin (a saponin extracted from Hedera helix) versus a clastogenic agent, doxorubicin and an aneugenic agent, carbendazim. We have applied a protocol of incorporation of alphahederin (pretreatment, simultaneous treatment and post treatment) to determine a mechanism of action. According to this protocol, alphahederin induces a significant diminution of the rate of micronuclei wathever the phases of the protocol. These results demonstrate the antimutagenic activity of alphahederin with a mechanism of action, both desmutagenic and bioantimutagenic. PMID:11397676

Villani, P; Orsičre, T; Sari-Minodier, I; Bouvenot, G; Botta, A

230

In vitro analyses of ethanol activity against Candida albicans biofilms.  

PubMed

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. PMID:22615286

Rane, Hallie S; Bernardo, Stella M; Walraven, Carla J; Lee, Samuel A

2012-05-21

231

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

2013-07-03

232

Lack of activity of cadmium in in vitro estrogenicity assays  

SciTech Connect

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

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

2006-10-01

233

Spontaneous electrical activity in the human fetal cortex in vitro.  

PubMed

Our knowledge about the developing human cerebral cortex is based on the analysis of fixed postmortem material. Here we use 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 midgestation. 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 action potential firing are thought to depend on the mature morphology and physiology of adult cortical network. However, our current data reveal that similar cortical rhythm is generated by a very immature ensemble of human fetal neurons. In the relative absence of sensory inputs, as in development in utero, or in slow-wave sleep (i.e., throughout the entire lifespan), the spontaneous slow oscillatory pattern (UP and DOWN states) is a fundamental aspect of human cortical physiology. PMID:21325506

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

2011-02-16

234

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

235

Synergistic in vitro antimalarial activity of plant extracts used as traditional herbal remedies in Mali.  

PubMed

In Mali, where malaria is endemic, plants are extensively used for treating periodic fevers and malaria. According to the advice of traditional medicine, plants are often mixed during the preparation of febrifugal decoctions. In previous studies, we demonstrated the potent in vitro antimalarial activity of extracts isolated from four plants commonly used in traditional remedies: Mitragyna inermis (Willd.) O. Kuntze, Rubiaceae, Nauclea latifolia (Sm.), Rubiaceae, Guiera senegalensis (Gmel.), Combretaceae, and Feretia apodanthera (Del.), Rubiaceae. In the present work, we evaluate the potent in vitro synergistic antimalarial interaction between these extracts, using standard isobologram analysis. Then, we evaluate their cytotoxicity on human monocytes and their mutagenic activity on an in vitro system of two beta-carboline alkaloids isolated from Guiera senegalensis (harman and tetrahydroharman). Three combinations demonstrate a strong, synergistic, inhibitory effect on in vitro plasmodial development and are devoid of cytotoxicity towards human cells. These results justify their use in association in traditional medicine. Moreover, tetrahydroharman, isolated from G. senegalensis, presents interesting antimalarial activity, no cytotoxicity and is not genotoxic in the Salmonella Ames test with and without metabolic activation. PMID:11936507

Azas, N; Laurencin, N; Delmas, F; Di, Giorgio C; Gasquet, M; Laget, M; Timon-David, P

2002-02-01

236

In vitro and in vivo Antiplasmodial Activity of Momordica balsamina Alone or in a Traditional Mixture  

Microsoft Academic Search

Background: Because of the dramatic situation of malaria in Africa, there is an urgent need to find new and cheap drugs, such as herbal medicines. Here we report the study of the in vitro and in vivo antimalarial activity of Momordica balsamina alone or in a traditional mixture used in Niger. Methods: Extracts were obtained with different solvents and tested

F. Benoit-Vical; P. Grellier; A. Abdoulaye; I. Moussa; A. Ousmane; A. Berry; K. Ikhiri; C. Poupat

2006-01-01

237

Comparison of spontaneous and evoked epileptiform activity in three in vitro epilepsy models  

Microsoft Academic Search

Rat neocortical slices express spontaneous epileptiform activity after incubation with GABAA receptor blocker bicuculline (BIC, 20 ?M), with potassium channel blocker 4-aminopyridine (4-AP, 50 ?M) or in Mg2+-free medium (LMG). Various parameters of spontaneous and evoked epileptiform discharges and their pharmacological sensitivity were analysed using extracellular field potential recordings in this comparative in vitro study. All types of convulsant solution

A Gulyás-Kovács; J Dóczi; I Tarnawa; L Détári; I Banczerowski-Pelyhe; I Világi

2002-01-01

238

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

Microsoft Academic Search

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

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

2000-01-01

239

In vitro antifungal activity of extracts of Mexican Chihuahuan Desert plants against postharvest fruit fungi  

Microsoft Academic Search

Chemical fungicides have been intensively used in the control of diseases in fruits in postharvest conditions; nevertheless these actions have developed resistance in the phytopathogens, have contaminated the atmosphere, and have affected people's health through residual toxic compounds present in the food for human consumption. The objective of this study was to evaluate the in vitro inhibiting activity of extracts

D. Jasso de Rodríguez; R. Rodríguez García; F. D. Hernández Castillo; C. N. Aguilar González; A. Sáenz Galindo; J. A. Villarreal Quintanilla; L. E. Moreno Zuccolotto

2011-01-01

240

Rifapentine Is Active In Vitro and In Vivo againstToxoplasma gondii  

Microsoft Academic Search

Rifapentine, a derivative of rifamycin, was examined for its in vitro and in vivo activities against the proto- zoanparasiteToxoplasmagondii.Thedruginhibitedtheintracellularreplicationofparasitesandwasnotcyto- toxic for the host cells at inhibitory concentrations. Mice infected either intraperitoneally with tachyzoites of the RH strain or orally with tissue cysts of the C56 strain were protected against death by treatment with rifa- pentine. The degree of protection was

FAUSTO G. ARAUJO; ANIS A. KHAN; ANDJACK S. REMINGTON

1996-01-01

241

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

242

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

243

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

244

A new in vitro assay of benzimidazole activity against adult Oesophagostomum dentatum  

Microsoft Academic Search

A new in vitro assay of benzimidazole activity against adult Oesophagostomum dentatum is described. The method is based on the ability of O. dentatum to migrate through polyamide nets after exposure to various concentrations of benzimidazole. To determine an appropriate mesh size, control worms and worms exposed to 10 ?M oxfendazole for 24 h were allowed to migrate through nets

Mads Bjelke Petersen; Christian Friis; Henrik Bjřrn

1997-01-01

245

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...

246

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

PubMed

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

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

247

In vitro antimycotic activity of a Williopsis saturnus killer protein against food spoilage yeasts  

Microsoft Academic Search

The in vitro antimycotic activity of a purified killer protein (KT4561) secreted by a strain of Williopsis saturnus was tested against 310 yeast strains belonging to 21 food spoilage species of 14 genera (Candida, Debaryomyces, Dekkera, Hanseniaspora, Issatchenkia, Kazachstania, Kluyveromyces, Pichia, Rhodotorula, Saccharomyces, Schizosaccharomyces, Torulaspora, Yarrowia and Zygosaccharomyces). Minimum inhibitory concentration (MIC) determinations showed that over 65% of the target

Marta Goretti; Benedetta Turchetti; Morena Buratta; Eva Branda; Lanfranco Corazzi; Ann Vaughan-Martini; Pietro Buzzini

2009-01-01

248

Activity of Posaconazole against Pseudallescheria boydii: In Vitro and In Vivo Assays  

PubMed Central

Thirty isolates of Pseudallescheria boydii were tested to compare the in vitro activity of posaconazole with those of fluconazole and itraconazole, using NCCLS methods. Posaconazole was evaluated in an immunosuppressed mouse model of disseminated pseudallescheriasis. Posaconazole was more effective than itraconazole and as effective as fluconazole in preventing death and significantly reducing the CFU of P. boydii from tissues.

Gonzalez, Gloria M.; Tijerina, Rolando; Najvar, Laura K.; Bocanegra, Rosie; Rinaldi, Michael G.; Loebenberg, David; Graybill, John R.

2003-01-01

249

In Vitro Activity of RU 64004, a New Ketolide Antibiotic, against Gram-Positive Bacteria  

Microsoft Academic Search

The comparative in vitro activity of RU 64004 (also known as HMR 3004), a new ketolide antibiotic, was tested by agar dilution against approximately 500 gram-positive organisms, including multiply resistant enterococci, streptococci, and staphylococci. All streptococci were inhibited by <1 mg of RU 64004 per ml. The ketolide was more potent than other macrolides against erythromycin A-susceptible staphylococci and was

T. SCHULIN; C. B. WENNERSTEN; R. C. MOELLERING; G. M. ELIOPOULOS

1997-01-01

250

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

Microsoft Academic Search

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

Chiaki Sanbongi; Noboru Suzuki; Tsuyoshi Sakane

1997-01-01

251

Comparative in vitro activities of twelve antimicrobial agents against Campylobacter species.  

PubMed Central

The in vitro susceptibility of 27 Campylobacter jejuni, 31 Campylobacter coli, and 30 Campylobacter fetus subsp. fetus strains to 12 antimicrobial agents was determined. Ciprofloxacin, a new quinoline derivative, was the most active agent tested. Antimicrobial susceptibility differed among the three species tested.

Fliegelman, R M; Petrak, R M; Goodman, L J; Segreti, J; Trenholme, G M; Kaplan, R L

1985-01-01

252

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

253

Natural killer cell activity and lymphocyte activation: Investigating the effects of a selection of essential oils and components in vitro  

Microsoft Academic Search

A selection of essential oils and components were tested in vitro for potential immunomodulating effects on natural killer cell activity (NKCA) and lymphocyte activation through CD69 expression.\\u000aMatricaria recutita, Boswellia carteri, Pelargonium graveolens, Lavandula angustifolia, Citrus limon, Melaleuca alternifolia, Melaleuca viridiflora, Santalum spicatum, Cedrus atlantica, and Thymus vulgaris ct. linalool essential oils were solubilised with ethanol and methylated â-cyclodextrin 1:5:25

M. D. Standen; Paul A Connellan; David N Leach

2006-01-01

254

In vitro fertilization and artificial activation of eggs of the direct-developing anuran Eleutherodactylus coqui  

PubMed Central

Although much is known about the reproductive biology of pond-breeding frogs, there is comparatively little information about terrestrial-breeding anurans, a highly successful and diverse group. This study investigates the activation and in vitro fertilization of eggs of the Puerto Rican coqui frog obtained by hormonally induced ovulation. We report that spontaneous activation occurs in 34% of eggs, probably in response to mechanical stress during oviposition. Artificial activation, as evidenced by the slow block to polyspermy and the onset of zygote division, was elicited both by mechanical stimulation and calcium ionophore exposure in 64% and 83% of the cases, respectively. Finally, one in vitro fertilization protocol showed a 27% success rate, despite the fact that about one third of all unfertilized eggs obtained by hormone injection auto-activate. We expect these findings to aid in the conservation effort of Eleutherodactylus frogs, the largest vertebrate genus.

Toro, Esteban; Michael, Scott F

2004-01-01

255

In vitro fertilization and artificial activation of eggs of the direct-developing anuran Eleutherodactylus coqui.  

PubMed

Although much is known about the reproductive biology of pond-breeding frogs, there is comparatively little information about terrestrial-breeding anurans, a highly successful and diverse group. This study investigates the activation and in vitro fertilization of eggs of the Puerto Rican coqui frog obtained by hormonally induced ovulation. We report that spontaneous activation occurs in 34% of eggs, probably in response to mechanical stress during oviposition. Artificial activation, as evidenced by the slow block to polyspermy and the onset of zygote division, was elicited both by mechanical stimulation and calcium ionophore exposure in 64% and 83% of the cases, respectively. Finally, one in vitro fertilization protocol showed a 27% success rate, despite the fact that about one third of all unfertilized eggs obtained by hormone injection auto-activate. We expect these findings to aid in the conservation effort of Eleutherodactylus frogs, the largest vertebrate genus. PMID:15296510

Toro, Esteban; Michael, Scott F

2004-08-05

256

[Effect of genistein on rat femoral bone metabolic activity in vitro].  

PubMed

This study is to investigate effects of genistein on rat femoral bone metabolic in vitro. Rat femoral tissues was isolated and randomly divided into two groups including control group and genistein (1 x 10(-5) mol x(-1)) group. Determinations of alkaline phosphatase (ALP) activity, calcium content and osteoprotegerin (OPG), type I-collagen (Collagen-I), RANKL, Runx-2 and bone morphogenetic protein (BMP-2) mRNA expression were done by real-time PCR. The results showed that 1 x 10(-5) mol x L(-1) genistein could increase the activity of ALP and contents of Ca, regulate bone metabolism activity of OPG, RANKL, BMP-2, Collagen-I and Runx-2 mRNA expression level. Genistein can significantly modulate bone metabolism related gene expression level of rat femoral tissue in vitro, and can increase calcium content and the activity of ALP. PMID:23984535

Zhou, Jian; Ge, Bao-Feng; Chen, Ke-Ming; Ma, Xiao-Ni; Cheng, Kui; Guo, Xiao-Yu; Lü, Xiang

2013-06-01

257

Sodium Tripolyphosphate: an excipient with intrinsic in vitro anti-Candida activity.  

PubMed

Sodium Tripolyphosphate (STPP) is a food additive that is being used in the development of micro and nanoparticles as it induces ionic interactions with chitosan molecules. Although the ability of STPP to inhibit the growth of several food contaminants has been reported, studies on its activity against clinical isolates are scarce. Candida spp. are common causative agents of mucocutaneous infections including the vulvovaginal tegument and new therapeutic approaches are needed in order to treat resistant and recurrent cases. The aim of this study was to evaluate in vitro both antifungal (anti-Candida spp.) activity, and cytotoxicity, on human dermal fibroblasts, of STPP solutions. STPP showed an inhibitory species-dependent activity against several Candida spp. strains being particularly active on C. glabrata, followed by C. guilliermondii. In vitro, STPP showed a concentration dependent cytotoxicity. Therefore STPP use, in low concentrations, seems to be interesting in the development of drug delivery systems for the treatment of vulvovaginal candidosis. PMID:21979249

Palmeira-de-Oliveira, R; Palmeira-de-Oliveira, A; Gaspar, C; Silvestre, S; Martinez-de-Oliveira, J; Amaral, M H; Breitenfeld, L

2011-09-29

258

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

259

Pharmacological activities of Vitex agnus-castus extracts in vitro.  

PubMed

The pharmacological effects of ethanolic Vitex agnus-castus fruit-extracts (especially Ze 440) and various extract fractions of different polarities were evaluated both by radioligand binding studies and by superfusion experiments. A relative potent binding inhibition was observed for dopamine D2 and opioid (micro and kappa subtype) receptors with IC50 values of the native extract between 20 and 70 mg/mL. Binding, neither to the histamine H1, benzodiazepine and OFQ receptor, nor to the binding-site of the serotonin (5-HT) transporter, was significantly inhibited. The lipophilic fractions contained the diterpenes rotun-difuran and 6beta,7beta-diacetoxy-13-hydroxy-labda-8,14-dien . They exhibited inhibitory actions on dopamine D2 receptor binding. While binding inhibition to mu and kappa opioid receptors was most pronounced in lipophilic fractions, binding to delta opioid receptors was inhibited mainly by a aqueous fraction. Standardised Ze 440 extracts of different batches were of constant pharmacological quality according to their potential to inhibit the binding to D2 receptors. In superfusion experiments, the aqueous fraction of a methanolic extract inhibited the release of acetylcholine in a concentration-dependent manner. In addition, the potent D2 receptor antagonist spiperone antagonised the effect of the extract suggesting a dopaminergic action mediated by D2 receptor activation. Our results indicate a dopaminergic effect of Vitex agnus-castus extracts and suggest additional pharmacological actions via opioid receptors. PMID:11081988

Meier, B; Berger, D; Hoberg, E; Sticher, O; Schaffner, W

2000-10-01

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

2010-06-17

261

In vitro release of biologically active materials from the bovine filarial parasite Setaria digitata.  

PubMed

Release of macromolecules by S. digitata, in 9 different media under in vitro condition have been studied. A direct relationship between microfilariae (mf) release and associated folin positive materials was seen in majority of the cases. High activities of hydrolytic enzymes such as protease, collagenase, alkaline phosphatase and lipase were detected in the excretary-secretary products and worm preparations. Activity of collagenase could not be detected in the male worm under experimental conditions. PMID:1816083

Murugan, A; Kaleysaraj, R

1991-11-01

262

Topical Activity of Ascorbic Acid: From in vitro Optimization to in vivo Efficacy  

Microsoft Academic Search

We present here a new cosmetic formula system containing 3% ascorbic acid based on an optimized oil-in-water (O\\/W) emulsion. This formulation demonstrated a good long-term stability of the active ingredient and also of the emulsion itself. It could be deduced from in vitro release studies that this O\\/W emulsion enabled a better release of the hydrophilic active agent than an

T. Raschke; U. Koop; H.-J. Düsing; A. Filbry; K. Sauermann; S. Jaspers; H. Wenck; K.-P. Wittern

2004-01-01

263

In vitro hemolytic activity of Plasmodium berghei on red blood cells  

Microsoft Academic Search

A suspension ofPlasmodium berghei obtained by lysis with saponin of red blood cells from an infected rat showed high hemolytic activity, when incubatedin vitro with normal rat red blood cells. The hemolysis was a temperature-dependent process and was dependent on the concentration\\u000a of the parasite. Plasma ofPlasmodium berghei infected albino rats also possessed lytic activity.

Sudhir Gupta; K. C. Saxena

1980-01-01

264

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

Microsoft Academic Search

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

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

2012-01-01

265

In vitro modulation of natural killer cell activity in non-Hodgkin's lymphoma patients after therapy  

Microsoft Academic Search

The depressed natural killer (NK) activity, antibody-dependent cellular cytotoxicity (ADCC) and NK cytotoxic factor cytotoxicity in untreated non-Hodgkin's lymphoma patients were found to be elevated after chemotherapy. In vitro treatment of the effector NK cells with interferon a could augment the NK activity in normal subjects and treated patients to a comparable degree. Chemotherapy mainly affected the post-binding events in

Bela A. Mehta; Mangesh N. Satam; Suresh H. Advani; Jayshree J. Nadkarni

1989-01-01

266

Oriented synthesis and in vitro anticancer activity of biquinazoline-2,2'-diones.  

PubMed

The synthesis of a series of biquinazoline-2,2'-diones starting from o-nitrobenzaldehydes, anilines, and triphosgene is presented. This general approach features a novel and easy way for access to the target products. The mechanistic course of the reaction suggests the involvement of reduction, coupling, and cyclization by one-pot. These compounds were also investigated in vitro for anticancer activity, and some were found to have good anticancer activity. PMID:20028094

Dou, Guolan; Shi, Daqing; Li, Yonghai

267

In Vitro Activity of PNU-100766 (Linezolid), a New Oxazolidinone Antimicrobial, against Nocardia brasiliensis  

PubMed Central

The in vitro activity of a novel oxazolidinone, linezolid, was studied by comparing the activity of linezolid with those of amikacin, trimethoprim-sulfamethoxazole, and amoxicillin-clavulanic acid against 25 strains of Nocardia brasiliensis isolated from patients with mycetoma. All N. brasiliensis strains tested were sensitive to linezolid (MIC at which 90% of strains are inhibited [MIC90], 2 ?g/ml; MIC50, 1 ?g/ml). This antimicrobial might constitute a good alternative for treatment of actinomycetoma.

Vera-Cabrera, Lucio; Gomez-Flores, Alejandra; Escalante-Fuentes, Wendy G.; Welsh, Oliverio

2001-01-01

268

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

269

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

270

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

271

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

272

In Vitro Effects of Alloxan–Vanadium Combination on Lipid Peroxidation and on Antioxidant Enzyme Activity  

Microsoft Academic Search

1.The in vitro effects of alloxan, dialuric acid and vanadium ions, alone or in combination, on lipid peroxidation and on antioxidant enzyme activity in rat liver and kidney were studied.2.Unlike alloxan, alloxan–glutathione (GSH) and dialuric acid increased lipid peroxidation, which could be explained by the decreased activity of catalase and GSH peroxidase during incubation.3.Vanadium(IV) ions increased the amount of thiobarbituric

A. Alexandrova; M. Kirkova; E. Russanov

1998-01-01

273

Inhibitory activity of limonene against Leishmania parasites in vitro and in vivo  

Microsoft Academic Search

Limonene is a monoterpene that has antitumoral, antibiotic and antiprotozoal activity. In this study we demonstrate the activity of limonene against Leishmania species in vitro and in vivo. Limonene killed Leishmania amazonensis promastigotes and amastigotes with 50% inhibitory concentrations of 252.0±49.0 and 147.0±46.0?M, respectively. Limonene was also effective against Leishmania major, Leishmania braziliensis and Leishmania chagasi promastigotes. The treatment of

Denise C. Arruda; Danilo C. Miguel; Jenicer K. U. Yokoyama-Yasunaka; Alejandro M. Katzin; Silvia R. B. Uliana

2009-01-01

274

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

Microsoft Academic Search

CL 188,624, CL 190,294, and CL 191,121 are novel aminomethyl tetrahydrofuranyl (THF)-1b-methylcarba- penems. The in vitro antibacterial activities of these THF carbapenems were evaluated and compared with those of biapenem, imipenem, and meropenem against 554 recent clinical isolates obtained from geographi- cally distinct medical centers across North America. The antibacterial activities of the THF carbapenems were equivalent to that of

WILLIAM J. WEISS; PETER J. PETERSEN; NILDA V. JACOBUS; YANG-I LIN; PANAYOTA BITHA; RAYMOND T. TESTA

275

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

Microsoft Academic Search

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

YOSHINARI ASAHI; SHUICHI MIYAZAKI; ANDKEIZO YAMAGUCHI

1995-01-01

276

In Vitro Antibacterial Activity and bLactamase Stability of a New Carbapenem, BO2727  

Microsoft Academic Search

The in vitro activity of BO-2727, a new carbapenem, was compared with those of meropenem, biapenem, imipenem, and ceftazidime. BO-2727 was four- or eightfold more active than the other carbapenems against methicillin-resistant staphylococci andPseudomonas aeruginosastrains, including imipenem- and ceftazidime- resistant bacteria. BO-2727 was quite stable to penicillinases, cephalosporinases, and oxyiminocephalospori- nases, but not to metallo-b-lactamase. Time-kill studies againstStaphylococcus aureusSmith,Escherichia coli

KUNIO INOUE; YOUKO HAMANA; ANDSUSUMU MITSUHASHI

1995-01-01

277

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

PubMed

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 cell line. No or only weak androgenic activity was observed for all the tested compounds. TBBPA showed weak antiandrogenic activity, which was demonstrated for the first time. The flame retardants HBCD, BDE-100 and BDE-155 enhanced the dihydrotestosterone-dependent activation of androgen receptor-responsive gene expression but exhibited little or no agonistic activity. The enhancement reached 150%, which was similar to the antimicrobials (TCS up to 180%, and TCC up to 130%). This enhancement of androgenic activity represents a novel mode of action of the endocrine activity of flame retardants. In contrast, most phthalates showed antiandrogenic activity. Butylbenzyl phthalate (BBP), dibutyl phthalate (DBP) and diethyl phthalate (DEP) showed strong antiandrogenicity, whereas the action of diethylhexyl phthalate (DEHP), dipentyl phthalate (DPP), dimethyl phthalate (DMP), and the DEHP metabolite monoethylhexyl phthalate (MEHP) was lower. Our in vitro study demonstrates for the first time a weak antiandrogenic activity of TBBPA, and a significant enhancement of the androgenic activity of HBCD, BDE-100 and BDE-155, which represents a novel mechanism of hormonal activity of flame retardants. PMID:20943248

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

2010-10-12

278

Activities against Streptococcus pneumoniae of amoxicillin and cefotaxime at physiological concentrations: in vitro pharmacodynamic simulation.  

PubMed Central

An in vitro model simulating amoxicillin and cefotaxime concentrations in human serum (after standard doses) was used to explore the activities of these drugs over time against penicillin-susceptible and penicillin-resistant Streptococcus pneumoniae strains. An initial inoculum reduction percentage of > or = 90% was obtained with amoxicillin and maintained for 2 to 8 h, regardless of the strain tested. In contrast, experiments showed that cefotaxime had significantly (P < 0.001) less capability to reduce initial inocula of the penicillin-resistant pneumococci from 0.5 h on than amoxicillin, despite the same in vitro susceptibility to amoxicillin and cefotaxime in both strains.

Balcabao, I P; Aguilar, L; Martin, M; Garcia, Y; Dal-Re, R; Prieto, J

1996-01-01

279

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

280

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

281

In vitro and in vivo antioxidant activity of Bifidobacterium animalis 01 isolated from centenarians.  

PubMed

Several studies reported the antioxidant activity of bifidobacteria using assays in vitro. In present study, the in vitro and in vivo antioxidant activity of Bifidobacterium animalis 01 was investigated. Culture supernatant, intact cells, and intracellular cell-free extracts of B. animalis 01 were involved in this study. The antioxidant assays in vitro included lipid peroxidation assay, 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay, hydroxyl radical ((•)OH) assay and superoxide anion (O??) assay. The antioxidant assays in vivo were conducted using mice model. Activities of antioxidative enzymes, malondialdehyde (MDA) content in serums and livers of aging mice were evaluated. Monoamine oxidase (MAO) activity and lipofuscin level in brains of aging mice were also characterized. Results showed that culture supernatant, intact cells and intracellular cell-free extracts of B. animalis 01 could effectively scavenge free radicals, significantly enhance mice's activities of antioxidative enzymes and reduce mice's MDA content, lipofuscin level and MAO activity. Our results indicated that B. animalis 01 has the potential to be developed into a dietary antioxidant supplements. PMID:21132298

Shen, Qian; Shang, Nan; Li, Pinglan

2010-12-04

282

In vitro antimalarial activity of limonoids from Khaya grandifoliola C.D.C. (Meliaceae).  

PubMed

The crude extract from the bark and seeds of Khaya grandifoliola was active in vitro against Plasmodium falciparum with an IC50 value of 13.23 microg/ml. The extract was purified to obtain seven limonoids--methylangolensate (1), 6-methylhydroxyangolensate (2), gedunin (3), 7-deacetylkhivorin (5), 1-deacetylkhivorin (6), swietenolide (7), 6-acetylswietenolide (8)--and one flavonoid, catechin (4). Five limonoids (1, 3, 5, 6, 8) were active with IC50 values between 1.25 and 9.63 microg/ml. Catechin was practically devoid of activity. The most active limonoid, gedunin, exhibited an additive effect when combined with chloroquine. PMID:10661881

Bickii, J; Njifutie, N; Foyere, J A; Basco, L K; Ringwald, P

2000-01-01

283

In Vitro and In Vivo Activities of Gatifloxacin against Mycobacterium tuberculosis  

PubMed Central

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

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

2002-01-01

284

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

285

In Vitro Activities of Daptomycin, Vancomycin, and Penicillin against Clostridium difficile, C. perfringens, Finegoldia magna, and Propionibacterium acnes  

Microsoft Academic Search

Daptomycin has in vitro activity against gram-positive anaerobic bacteria, although limited numbers of species have been tested. We studied the in vitro activities of daptomycin, vancomycin, and penicillin against more than 100 strains each of Clostridium difficile, C. perfringens, Finegoldia magna, and Propionibacterium acnes. Daptomycin Etest MICs and results from time-kill studies were determined for selected strains. For 392 of

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

2006-01-01

286

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

SciTech Connect

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

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

1995-09-19

287

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

PubMed

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

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

1999-04-01

288

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

289

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

NASA Astrophysics Data System (ADS)

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

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

2011-09-01

290

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

291

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

2010-12-01

292

In Vitro Activities of Quinine and Other Antimalarials and pfnhe Polymorphisms in Plasmodium Isolates from Kenya?  

PubMed Central

Resistance to the amino alcohol quinine has been associated with polymorphisms in pfnhe, a sodium hydrogen exchanger. We investigated the role of this gene in quinine resistance in vitro in isolates from Kenya. We analyzed pfnhe whole-gene polymorphisms, using capillary sequencing, and pfcrt at codon 76 (pfcrt-76) and pfmdr1 at codon 86 (pfmdr1-86), using PCR-enzyme restriction methodology, in 29 isolates from Kilifi, Kenya, for association with the in vitro activities of quinine and 2 amino alcohols, mefloquine and halofantrine. In vitro activity was assessed as the drug concentration that inhibits 50% of parasite growth (IC50). The median IC50s of quinine, halofantrine, and mefloquine were 92, 22, and 18 nM, respectively. The presence of 2 DNNND repeats in microsatellite ms4760 of pfnhe was associated with reduced susceptibility to quinine (60 versus 227 nM for 1 and 2 repeats, respectively; P < 0.05), while 3 repeats were associated with restoration of susceptibility. The decrease in susceptibility conferred by the 2 DNNND repeats was more pronounced in parasites harboring the pfmdr1-86 mutation. No association was found between susceptibility to quinine and the pfcrt-76 mutation or between susceptibility to mefloquine or halofantrine and the pfnhe gene and the pfcrt-76 and pfmdr1-86 mutations. Using previously published data on the in vitro activities of chloroquine, lumefantrine, piperaquine, and dihydroartemisinin, we investigated the association of their activities with pfnhe polymorphism. With the exception of a modulation of the activity of lumefantrine by a mutation at position 1437, pfnhe did not modulate their activities. Two DNNND repeats combined with the pfmdr1-86 mutation could be used as an indicator of reduced susceptibility to quinine.

Okombo, John; Kiara, Steven M.; Rono, Josea; Mwai, Leah; Pole, Lewa; Ohuma, Eric; Borrmann, Steffen; Ochola, Lynette Isabella; Nzila, Alexis

2010-01-01

293

In vitro activities of quinine and other antimalarials and pfnhe polymorphisms in Plasmodium isolates from Kenya.  

PubMed

Resistance to the amino alcohol quinine has been associated with polymorphisms in pfnhe, a sodium hydrogen exchanger. We investigated the role of this gene in quinine resistance in vitro in isolates from Kenya. We analyzed pfnhe whole-gene polymorphisms, using capillary sequencing, and pfcrt at codon 76 (pfcrt-76) and pfmdr1 at codon 86 (pfmdr1-86), using PCR-enzyme restriction methodology, in 29 isolates from Kilifi, Kenya, for association with the in vitro activities of quinine and 2 amino alcohols, mefloquine and halofantrine. In vitro activity was assessed as the drug concentration that inhibits 50% of parasite growth (IC50). The median IC50s of quinine, halofantrine, and mefloquine were 92, 22, and 18 nM, respectively. The presence of 2 DNNND repeats in microsatellite ms4760 of pfnhe was associated with reduced susceptibility to quinine (60 versus 227 nM for 1 and 2 repeats, respectively; P<0.05), while 3 repeats were associated with restoration of susceptibility. The decrease in susceptibility conferred by the 2 DNNND repeats was more pronounced in parasites harboring the pfmdr1-86 mutation. No association was found between susceptibility to quinine and the pfcrt-76 mutation or between susceptibility to mefloquine or halofantrine and the pfnhe gene and the pfcrt-76 and pfmdr1-86 mutations. Using previously published data on the in vitro activities of chloroquine, lumefantrine, piperaquine, and dihydroartemisinin, we investigated the association of their activities with pfnhe polymorphism. With the exception of a modulation of the activity of lumefantrine by a mutation at position 1437, pfnhe did not modulate their activities. Two DNNND repeats combined with the pfmdr1-86 mutation could be used as an indicator of reduced susceptibility to quinine. PMID:20516285

Okombo, John; Kiara, Steven M; Rono, Josea; Mwai, Leah; Pole, Lewa; Ohuma, Eric; Borrmann, Steffen; Ochola, Lynette Isabella; Nzila, Alexis

2010-06-01

294

In vitro and in vivo anticancer activity of 2-deacetoxytaxinine J and synthesis of novel taxoids and their in vitro anticancer activity.  

PubMed

The taxane diterpneoid 2-deacetoxytaxinine J (2-DAT-J) 1 has been isolated from the bark of Himalayan yew, Taxus baccata L. spp. wallichiana in a reasonably good yield (0.1%) and its anticancer activity against breast cancer cell lines (MCF-7 and MDA-MB-231) and normal human kidney epithelial cell line (HEK-293) has been studied. 2-DAT-J (1) showed significant in vitro activity against breast cancer cell line at a concentration of 20 microM and 10 microM in MCF-7 and MDA-MB-231 respectively. Few novel taxoids were derived (7, 8 and 10-13) from the naturally occurring 2-DAT-J (1) and screened for their anticancer activity. The structure-activity relationship studies indicated that the cinnamoyl group on C-5 and acetyl group on C-10 are essential for the anticancer activity. 2-DAT-J (1) was also tested for its in vivo activity on DMBA-induced mammary tumors in virgin female Sprague Dawley rats at a dose of 10mg/kg body weight orally for 30 days and showed significant regression in mammary tumors as compared to vehicle treated group (p<0.05). PMID:19446930

Reddy, K Papi; Bid, Hemant K; Nayak, V Lakshma; Chaudhary, Preeti; Chaturvedi, J P; Arya, K R; Konwar, Rituraj; Narender, T

2009-04-22

295

In Vitro Spectrum of Activity of Finafloxacin, a Novel, pH-Activated Fluoroquinolone, under Standard and Acidic Conditions?  

PubMed Central

Finafloxacin is a novel fluoroquinolone that exhibits enhanced antibacterial activity under acidic conditions. The aim of this study was to define the in vitro pH-activity relationship. Finafloxacin exhibited optimal antibacterial activity between pH 5.0 and 6.0 at which MICs were 4- to 8-fold lower than those determined at neutral pH. These observations were then confirmed against a larger collection of bacteria. These data suggest that finafloxacin could potentially offer a therapeutic advantage within acidic foci of infection.

Stubbings, Will; Leow, Pamela; Yong, Goh Chee; Goh, Falicia; Korber-Irrgang, Barbara; Kresken, Michael; Endermann, Rainer; Labischinski, Harald

2011-01-01

296

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

PubMed

The objective of this study was to determine the in vitro minimum inhibitory concentration (MIC) of antimicrobials against 10 isolates of Lawsonia intracellularis, the etiological agent of proliferative enteropathy (PE). Antimicrobials tested included carbadox, chlortetracycline, lincomycin, tiamulin, tylosin and valnemulin. The MIC of each antimicrobial against L. intracellularis was determined using a tissue culture system and was identified as the lowest concentration that inhibited 99% of L. intracellularis growth, as compared to the antimicrobial-free control. Each antimicrobial concentration was evaluated for both intracellular and extracellular activity against L. intracellularis, an obligately intracellular bacterium. When tested for intracellular activity, carbadox, tiamulin, and valnemulin were the most active antimicrobials with MICs of < or =0.5microg/ml. Tylosin (MICs ranging from 0.25 to 32microg/ml) and chlortetracycline (MICs ranging from 0.125 to 64microg/ml) showed intermediate activities and lincomycin (MICs ranging from 8 to >128mIcog/ml) showed the least activity. When tested for extracellular activity, valnemulin (MICs ranging from 0.125 to 4microg/ml) was the most active against most L. intracellularis isolates. Chlortetracycline (MICs ranging from 16 to 64microg/ml), tylosin (MICs ranging from 1 to >128microg/ml), and tiamulin (MICs ranging from 1 to 32microg/ml) showed intermediate activities. Lincomycin (MICs ranging from 32 to >128microg/ml) showed the least activity. Our in vitro results showed that each L. intracellularis isolate had a different antimicrobial sensitivity pattern and these data can be utilized as an in vitro guideline for the further antimicrobial evaluation of field L. intracellularis isolates. PMID:18823723

Wattanaphansak, Suphot; Singer, Randall S; Gebhart, Connie J

2008-08-22

297

Evaluation of RNA chaperone activity in vivo and in vitro using misfolded group I ribozymes.  

PubMed

Here two methods to measure RNA chaperone activity in vivo and in vitro are described. In both assays folding of a misfolded group I intron RNA into the splicing-competent form in the presence of proteins with RNA chaperone activity is measured. Folding is evaluated indirectly by assessing the difference in splicing activity with or without proteins with RNA chaperone activity. In vitro, we use the thymidylate synthase (td) group I intron of phage T4 that is split into two halves. As a consequence this split ribozyme is only capable to fold and in turn to splice in trans at elevated temperatures. Proteins with RNA chaperone activity enable splicing of the split intron at lower temperatures. This difference in splicing activity is measured to assess the efficacy of the RNA chaperone. In vivo, a mutant variant of the td group I intron is trapped in a misfolded conformation, resulting in a reduced splicing activity. Over-expression of proteins with RNA chaperone activity results in an increase in splicing in vivo, as these proteins resolve the misfolded conformation. PMID:24136608

Semrad, Katharina

2014-01-01

298

In Vitro Antianaerobic Activity of DX-619, a New Des-Fluoro(6) Quinolone  

PubMed Central

The in vitro activity of DX-619, a new des-F(6) quinolone, against anaerobic bacteria was evaluated. DX-619 showed potent activity against Bacteroides, Prevotella, Fusobacterium, Micromonas, Actinomyces, and Clostridium spp., with MIC50s/MIC90s of ?0.03 to 0.25/?0.03 to 1 ?g/ml, respectively. DX-619 was also active against imipenem-resistant Bacteroides spp., with MIC50s/MIC90s of 0.25/1 ?g/ml, respectively.

Tanaka, Kaori; Mikamo, Hiroshige; Nakao, Ken'ichi; Watanabe, Kunitomo

2006-01-01

299

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

2009-01-15

300

Efficacy of Carraguard-based microbicides in vivo despite variable in vitro activity.  

PubMed

Anti-HIV microbicides are being investigated in clinical trials and understanding how promising strategies work, coincident with demonstrating efficacy in vivo, is central to advancing new generation microbicides. We evaluated Carraguard and a new generation Carraguard-based formulation containing the non-nucleoside reverse transcriptase inhibitor (NNRTI) MIV-150 (PC-817). Since dendritic cells (DCs) are believed to be important in HIV transmission, the formulations were tested for the ability to limit DC-driven infection in vitro versus vaginal infection of macaques with RT-SHIV (SIVmac239 bearing HIV reverse transcriptase). Carraguard showed limited activity against cell-free and mature DC-driven RT-SHIV infections and, surprisingly, low doses of Carraguard enhanced infection. However, nanomolar amounts of MIV-150 overcame enhancement and blocked DC-transmitted infection. In contrast, Carraguard impeded infection of immature DCs coincident with DC maturation. Despite this variable activity in vitro, Carraguard and PC-817 prevented vaginal transmission of RT-SHIV when applied 30 min prior to challenge. PC-817 appeared no more effective than Carraguard in vivo, due to the limited activity of a single dose of MIV-150 and the dominant barrier effect of Carraguard. However, 3 doses of MIV-150 in placebo gel at and around challenge limited vaginal infection, demonstrating the potential activity of a topically applied NNRTI. These data demonstrate discordant observations when comparing in vitro and in vivo efficacy of Carraguard-based microbicides, highlighting the difficulties in testing putative anti-viral strategies in vitro to predict in vivo activity. This work also underscores the potential of Carraguard-based formulations for the delivery of anti-viral drugs to prevent vaginal HIV infection. PMID:18776937

Turville, Stuart G; Aravantinou, Meropi; Miller, Todd; Kenney, Jessica; Teitelbaum, Aaron; Hu, Lieyu; Chudolij, Anne; Zydowsky, Tom M; Piatak, Michael; Bess, Julian W; Lifson, Jeffrey D; Blanchard, James; Gettie, Agegnehu; Robbiani, Melissa

2008-09-08

301

Theileria annulata induces abberrant T cell activation in vitro and in vivo.  

PubMed Central

The protozoan parasite of cattle, Theileria annulata, causes a severe lymphoproliferative disease, developing initially in the draining lymph node, which is often fatal in naive animals. Infection of macrophages with T. annulata leads to an augmentation of their antigen-presenting capability in vitro and infected cells can induce proliferation of autologous resting T cells from naive animals. This inappropriate activation of T cells may play an important role in the failure of the host to mount an effective immune response in vivo. To investigate this hypothesis we characterized further the response of T cells from naive cattle to infected cells in vitro, and also examined the development of the immune response in lymph nodes draining the sites of T. annulata infection. Both CD4+ and CD8+ T cells from naive peripheral blood mononuclear cells (PBMC) were induced to proliferate and express the activation markers IL-2R and MHC class II when cultured with infected cells. This effect was seen in both 'naive' and 'memory' T cells, and was dependent upon contact with infected cells. In vitro, infected cells are therefore capable of activating T cells irrespective of their antigen specificity or memory status. In draining lymph nodes, although large numbers of IL-2R+ cells developed following infection, these activated cells were only associated with areas of parasite-induced proliferating cells, and subsequently disappeared from the node. Cells expressing IL-2R were not present in recognized sites for T cell development. Germinal centres were severely affected, losing T cell-dependent zones followed by a total destruction of morphology. T cell function is therefore severely disrupted within draining nodes. This study has shown that parasitized cells supply sufficient signals in vitro to activate T cells irrespective of specificity. T cells also are not stimulated in a conventional manner in vivo, and this may play an important role in preventing an effective immune response from being generated. Images Fig. 4 Fig. 5 Fig. 5

Campbell, J D; Howie, S E; Odling, K A; Glass, E J

1995-01-01

302

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

303

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

304

In Vitro and In Vivo Antidermatophyte Activities of NND-502, a Novel Optically Active Imidazole Antimycotic Agent  

PubMed Central

In vitro and in vivo antidermatophyte activities of NND-502, a new imidazole antimycotic agent, were compared with those of two existing antifungal agents, lanoconazole and terbinafine. NND-502 exhibited strong in vitro antifungal activity against Trichophyton spp.; its MIC was 1 to 4 times lower than that of lanoconazole or terbinafine. In an in vivo study with a guinea pig model of tinea pedis, 7-day topical treatment with a 0.5% solution of NND-502 (dissolved in polyethylene glycol 400) was more effective than that with a 0.5% solution of either lanoconazole or terbinafine for eradicating fungi from the infected feet. When the duration of treatment was shortened to 3 days, a topical 1% solution of NND-502 achieved a complete mycological cure, while topical 1% solutions of lanoconazole and terbinafine did not.

Niwano, Yoshimi; Kuzuhara, Naoki; Kodama, Hiroki; Yoshida, Masanori; Miyazaki, Tsuneo; Yamaguchi, Hideyo

1998-01-01

305

The role of lysozyme in the prophenoloxidase activation system of Manduca sexta: an in vitro approach.  

PubMed

Activation of the prophenoloxidase (proPO) system and synthesis of antimicrobial peptides (including lysozyme) are two key defense mechanisms in arthropods. Activation of proPO involves a cascade of serine proteinases that eventually converts proPO to active phenoloxidase (PO). However, a trade-off between lysozyme/antibacterial activity and PO activity has been observed in some insects, and a mosquito lysozyme can inhibit melanization. It is not clear whether lysozyme can inhibit PO activity and/or proPO activation. In this study, we used in vitro assays to investigate the role of lysozyme in proPO activation in the tobacco hornworm Manduca sexta. We showed that lysozymes from M. sexta, human milk and hen egg white did not inhibit PO activity in the pre-activated naďve plasma of M. sexta larvae, but significantly inhibited proPO activation in the naďve plasma. Western blot analysis showed that direct incubation of M. sexta lysozyme with the naďve plasma prevented conversion of proPO to PO, but stimulated degradation of precursor proteins for serine proteinase homolog-2 (SPH2) and proPO-activating proteinase-1 (PAP1), two key components required for proPO activation. Far-western blot analysis showed that M. sexta lysozyme and proPO interacted with each other. Altogether, our results suggest that lysozymes may inhibit the proPO activation system by preventing conversion of proPO to PO via direct protein interaction with proPO. PMID:19835909

Rao, Xiang-Jun; Ling, Erjun; Yu, Xiao-Qiang

2009-10-24

306

The Role of Lysozyme in the Prophenoloxidase Activation System of Manduca sexta: An in vitro approach  

PubMed Central

Activation of the prophenoloxidase (proPO) system and synthesis of antimicrobial peptides (including lysozyme) are two key defense mechanisms in arthropods. Activation of proPO involves a cascade of serine proteinases that eventually converts proPO to active phenoloxidase (PO). However, a trade-off between lysozyme/antibacterial activity and PO activity has been observed in some insects, and a mosquito lysozyme can inhibit melanization. It is not clear whether lysozyme can inhibit PO activity and/or proPO activation. In this study, we used in vitro assays to investigate the role of lysozyme in proPO activation in the tobacco hornworm Manduca sexta. We showed that lysozymes from M. sexta, human milk and hen egg white did not inhibit PO activity in the pre-activated naďve plasma of M. sexta larvae, but significantly inhibited proPO activation in the naďve plasma. Western blot analysis showed that direct incubation of M. sexta lysozyme with the naďve plasma prevented conversion of proPO to PO, but stimulated degradation of precursor proteins for serine proteinase homolog-2 (SPH2) and proPO-activating proteinase-1 (PAP1), two key components required for proPO activation. Far-western blot analysis showed that M. sexta lysozyme and proPO interacted with each other. Altogether, our results suggest that lysozymes may inhibit the proPO activation system by preventing conversion of proPO to PO via direct protein interaction with proPO.

Rao, Xiang-Jun; Ling, Erjun; Yu, Xiao-Qiang

2009-01-01

307

The glucocorticoid receptor hormone binding domain mediates transcriptional activation in vitro in the absence of ligand.  

PubMed Central

We show that recombinant rat glucocorticoid receptor (vvGR) expressed using vaccinia virus is indistinguishable from authentic GR with respect to DNA and hormone binding. In the absence of hormone, vvGR is mainly found in the cytoplasm in a complex with heat shock protein 90. Upon incubation with ligand, vvGR is released from this complex and translocated to the nucleus. Thus, the ligand binding domain displays the known biochemical properties. However, in vitro, transcription from a synthetic promoter and from the mouse mammary tumor virus (MMTV) promoter is enhanced by recombinant GR in a ligand independent manner. Both transactivation domains contribute to the transcriptional activity, additively on a synthetic promoter and cooperatively on the MMTV promoter. We thus provide the first evidence that in vitro the hormone binding domain has a transcriptional activity even in the absence of ligand. Images

Schmitt, J; Stunnenberg, H G

1993-01-01

308

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

PubMed

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

Verkade, E J M; Verhulst, C J M M; Huijsdens, X W; Kluytmans, J A J W

2010-02-26

309

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

2013-10-09

310

In vitro antioxidant activity of aged extracts of some Italian Allium species.  

PubMed

Antioxidant activity of fresh Allium sativum L. (garlic) is well known and is mainly due to unstable and irritating organosulphur compounds. Fresh garlic extracted over a prolonged period (up to 20 months) produces odourless aged garlic extract (AGE) containing stable and water soluble organosulphur compounds that prevent oxidative damage by scavenging free radicals. The aim of this study was to investigate the in vitro antioxidant activity of aged (up to 20 months) 15% hydroethanolic extracts of different parts (bulbs, bulblets, flower bulblets, flowers, and leaves) of three Allium spontaneous species which are endemic for Italian flora: Allium neapolitanum Cyr., Allium subhirsutum L., Allium roseum L. and to compare it with the in vitro antioxidant activity of aged 15% hydroethanolic extracts of bulbs and leaves of garlic. The antioxidant potential of aged extracts of all species has been evaluated using two different spectrophotometric assays: 2,2-diphenylpicrylhydrazyl (DPPH) test and the ferric reducing/antioxidant power (FRAP) assay. Furthermore the polyphenol content was determined. The aged extracts obtained from the leaves showed the best antioxidant activity, followed by flowers and then by bulbs in both used tests, while flower bulblets and bulblets exhibited lower results or no activity. The polyphenol content was generally directly correlated with antioxidant/antiradical activity. This study confirms the data obtained in previous researches, the wild-type species of Allium and in particular organs other than bulbs are more active and efficacious than garlic bulb. Surely leaves of these Allium spp. deserve special attention. PMID:21290188

Nencini, Cristina; Menchiari, Andrea; Franchi, Gian Gabriele; Micheli, Lucia

2011-03-01

311

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

PubMed

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. PMID:23942522

Lacroix, Benoît; Citovsky, Vitaly

2013-08-14

312

In Vitro Selection of Cathepsin E-Activity-Enhancing Peptide Aptamers at Neutral pH  

PubMed Central

The aspartic protease cathepsin E has been shown to induce apoptosis in cancer cells under physiological conditions. Therefore, cathepsin E-activity-enhancing peptides functioning in the physiological pH range are valuable potential cancer therapeutic candidates. Here, we have used a general in vitro selection method (evolutionary rapid panning analysis system (eRAPANSY)), based on inverse substrate-function link (SF-link) selection to successfully identify cathepsin E-activity-enhancing peptide aptamers at neutral pH. A successive enrichment of peptide activators was attained in the course of selection. One such peptide activated cathepsin E up to 260%, had a high affinity (KD; ?300?nM), and had physiological activity as demonstrated by its apoptosis-inducing reaction in cancerous cells. This method is expected to be widely applicable for the identification of protease-activity-enhancing peptide aptamers.

Biyani, Madhu; Futakami, Masae; Kitamura, Koichiro; Kawakubo, Tomoyo; Suzuki, Miho; Yamamoto, Kenji; Nishigaki, Koichi

2011-01-01

313

New in vitro reporter gene bioassays for screening of hormonal active compounds in the environment.  

PubMed

Identification of chemicals with endocrine-disrupting activities in the past two decades has led to the need for sensitive assays for detection and monitoring of these activities in the environment. In vitro reporter gene assays represent a relatively fast and easy-to-perform method for detection of compounds that are able to bind to hormonal receptors and stimulate or silence their transactivation activity, thus interfering with the hormone signaling pathways. This paper reviews upgrades on reporter gene assays performed during the last decade. The utilization of new reporter genes (luciferase and green fluorescent protein coding genes) significantly improved the sensitivity of the tests and made them faster. Reporter gene assays now represent a high-throughput system for screening chemicals for hormonal activity. Finally, modification of test set-ups for testing anti-hormonal activities also enabled measurements of endocrine-disrupting activities in complex environmental samples such as sediments and wastewater treatment plant effluents. PMID:20737269

Svobodová, Katerina; Cajthaml, Tomás

2010-08-25

314

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

Microsoft Academic Search

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

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

2011-01-01

315

Evaluation of several potential bioactive agents for reducing protozoal activity in vitro  

Microsoft Academic Search

The effects of 14 bioactive agents on ruminal fermentation and protozoal activity were investigated in vitro as potential feed additives to improve feed efficiency. Agents studied were: lecithin, herring meal, canola oil, coconut oil, linseed oil, palm oil, and soybean oil, with each oil at final concentrations of 0.5, 1.0 and 2.0%; the saponin-containing plants Yucca schidigera (yucca) and Quillaja

A. N Hristov; M Ivan; L Neill; T. A McAllister

2003-01-01

316

[(?(6)-Praziquantel)Cr(CO)3] derivatives with remarkable in vitro anti-schistosomal activity.  

PubMed

The antischistosomal effect of two [(?(6)-praziquantel)Cr(CO)(3)] derivatives was investigated. The compounds (see figure: Cr?purple, N?blue, O?red) were prepared in a one-step procedure from commercially available praziquantel. Both derivatives show a high in vitro activity against Schistosoma mansoni, a parasitic trematode, and only a minor cytotoxic effect on selected mammalian cell lines. PMID:23296750

Patra, Malay; Ingram, Katrin; Pierroz, Vanessa; Ferrari, Stefano; Spingler, Bernhard; Gasser, Robin B; Keiser, Jennifer; Gasser, Gilles

2013-01-07

317

In vitro antiplasmodial and cytotoxicity activities of 14 medicinal plants from Kenya  

Microsoft Academic Search

Organic and aqueous extracts obtained from 14 Kenyan medicinal plants were screened for their antimalarial properties on two strains of Plasmodium falciparum (K1 chloroquine resistant and NF54 chloroquine sensitive). Dichloromethane extracts had the highest activities with IC50 ranging from 1.4 to 35.2 ?g\\/ml. These extracts together with methanol extract of Turraea robusta were tested for their cytotoxicity properties in vitro on

Beatrice N. Irungu; Geoffrey M. Rukunga; Geoffrey M. Mungai; Charles N. Muthaura

2007-01-01

318

Detection of endotoxin-like interleukin-1-inducing activity during in vitro dialysis  

Microsoft Academic Search

Detection of endotoxin-like interleukin-1-inducing activity during in vitro dialysis. In order to study the integrity of dialysis membranes to pyrogens, the dialysate side of a closed loop hemodialysis (HD) circuit was challenged with E. coli microfiltrate containing 500 ng\\/ml endotoxin. Three solutions, a) tissue culture medium\\/saline, b) 5% human serum albumin, and c) 10% fresh human plasma, were circulated in

Gerhard Lonnemann; Marion Bingel; Juergen Floege; Karl M Koch; Charles A Dinarello

1988-01-01

319

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

320

Effect of Some Vajikaran Herbs on Pendiculation Activities and In vitro Sperm Count in Male  

Microsoft Academic Search

Ayurveda holds a special position amongst the various traditional systems of medicine. Vajikaran is a speciality in Ayurvedic\\u000a system of medicine in India dealing with herbs possessing rejuvenative and revitalizing properties for improving sexual dynamics.\\u000a In the present study, the effect of five vajikaran herbs on pendiculatory activity and in-vitro sperm count was assessed.\\u000a The lyophilized aqueous extracts of Asparagus

Mayank Thakur; V. K. Dixit

2007-01-01

321

Comparison of In Vitro Activities of Ketolides, Macrolides, and an Azalide against the Spirochete Borrelia burgdorferi  

Microsoft Academic Search

Two ketolides, three macrolides, and one azalide were tested in vitro against 17 isolates of the B. burgdorferi s.l. complex. As measured in micrograms per milliliter, activity was highest for cethromycin (MIC at which 90% of the tested isolates were inhibited (MIC90), 0.0019 g\\/ml) and telithromycin (MIC90, 0.0078 g\\/ml). Elec- tron-microscope analysis and time-kill studies also supported enhanced effectiveness of

Klaus-Peter Hunfeld; Thomas A. Wichelhaus; Rebecca Rodel; Georg Acker; Volker Brade; Peter Kraiczy

2004-01-01

322

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

323

Aplidin, a Marine Organism-Derived Compound with Potent Antimyeloma Activity In vitro and In vivo  

Microsoft Academic Search

Despite recent progress in its treatment, multiple myeloma (MM) remains incurable, thus necessitating identification of novel anti-MM agents. We report that the marine-derived cyclodepsipeptide Aplidin exhibits, at clinically achievable concentrations, potent in vitro activity against primary MM tumor cells and a broad spectrum of human MM cell lines, including cells resistant to conventional (e.g., dexamethasone, alkylating agents, and anthracyclines) or

Constantine S. Mitsiades; Enrique M. Ocio; Atanasio Pandiella; Patricia Maiso; Consuelo Gajate; Mercedes Garayoa; David Vilanova; Juan Carlos Montero; Nicholas Mitsiades; Ciaran J. McMullan; Nikhil C. Munshi; Teru Hideshima; Dharminder Chauhan; Pablo Aviles; Gabriel Otero; Glynn Faircloth; M. Victoria Mateos; Paul G. Richardson; Faustino Mollinedo; Jesus F. San-Miguel; Kenneth C. Anderson

324

In vitro and In vivo Antibacterial Activity of Punica granatum Peel Ethanol Extract Against Salmonella  

Microsoft Academic Search

Punica granatum is commonly used in Korea as a traditional medicine for the treatment of pathogenic bacteria. In this study, we investigated the in vitro and in vivo antimicrobial activity of P. granatum peel EtOH extract (PGPE) against 16 strains of Salmonella. The minimal inhibitory concentrations of PGPE were in the range of 62.5-1000m gm l1. In addition, the in

Jang-Gi Choi; Ok-Hwa Kang; Young-Seob Lee; Hee-Sung Chae; You-Chang Oh; Obiang-Obounou Brice; Min-San Kim; Dong-Hwan Sohn; Hun-Soo Kim; Hyun Park; Dong-Won Shin; Jung-Rae Rho; Dong-Yeul Kwon

2009-01-01

325

Effects of Adherence, Activation and Distinct Serum Proteins on the In Vitro Human Monocyte Maturation Process  

Microsoft Academic Search

Elutriator-punfied human monocytes were cultured in a serum-free (SF) medium, and various serum proteins and functional activating agents were assessed for their effects on the in vitro maturation of human monocytes to macrophages. Following 3 days of suspension culture in Teflon Iabware, 60% of the monocytes were easily recovered. When varying concentrations of human AB serum (HuAB) were employed, human

Yukio Akiyama; Richard Griffith; Paul Miller; G. W. Stevenson; Stacy Lund; D. J. Kanapa; Henry C. Stevenson

326

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

327

Thrombin formation in vitro in response to shear-induced activation of platelets  

Microsoft Academic Search

IntroductionThromboembolic events caused by implanted vascular devices present serious medical challenges. In particular bileaflet mechanical heart valves (MHVs) are prone to thrombus formation in the hinge region due to a combination of high shear stress and stagnation regions. Most studies of shear-induced platelet activation and aggregation have been performed using viscometers, parallel plate flow, and other non-physiologic in vitro configurations.

Anna M. Fallon; Ulla M. Marzec; Stephen R. Hanson; Ajit P. Yoganathan

2007-01-01

328

In Vitro and In Vivo Activities of Sitafloxacin against Chlamydia spp  

Microsoft Academic Search

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

NAOYUKI MIYASHITA; YOSHIHITO NIKI; TOSHIHARU MATSUSHIMA

2001-01-01

329

Comparison of cytotoxic activities between in vitro and field grown plants of Typhonium flagelliforme (Lodd.) blume  

Microsoft Academic Search

Anin vitro cytotoxicity screening of theTyphonium flagelliforme extracts indicated high cytotoxicity effect on human lung carcinoma NCl-H23 cells and human mammary gland carcinoma T-47D\\u000a cells, but the extracts were not active on human liver carcinoma HepG2 cells. NCl-H23 cells were more susceptible toT. flagelliforme extracts than T-47D cells. EDP50 values of the hexane fractions of the mature plant and thein

Lai Keng Chan; Wan Yee Koh; Tengku S. Tengku-Muhammad

2005-01-01

330

Development of in vitro screening system for assessment of antifilarial activity of compounds  

Microsoft Academic Search

Evaluation of antifilarial activity of new potential agents in vivo is extremely time consuming and uneconomic. In the present study effort has been made to develop an in vitro screening method using Acanthocheilonema viteae, a subcutaneously dwelling rodent filariid with anaerobic metabolic characteristics like human filariids, W. Bancrofti\\/Brugia malayi as test parasite. Motility test and tetrazolium (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide, MTT)

Monisha Mukherjee; Shailja Misra; R. K Chatterjee

1998-01-01

331

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

Microsoft Academic Search

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

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

2012-01-01

332

A comparison of in vitro and in vivo EDSTAC test battery results for detecting antiandrogenic activity  

Microsoft Academic Search

The androgen receptor (AR) transactivation, binding, and Hershberger assays are being developed for large-scale screening of chemicals for endocrine activity. The goal of this study was to evaluate the correlation between in vitro and in vivo antiandrogenicity assays using a variety of compounds (p,p'-DDE, flutamide (FLUT), spironolactone, procymidone, RU486, methoxychlor (MXC), benzo(a)pyrene (BAP), and selected metabolites). For the AR transactivation

Grantley D. Charles; H. Lynn Kan; Melissa R. Schisler; B. Bhaskar Gollapudi; M. Sue Marty

2005-01-01

333

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

334

In Vitro Activities of the New Antitubercular Agents PA-824 and BTZ043 against Nocardia brasiliensis  

PubMed Central

The in vitro activity of PA-824 and BTZ043 against 30 Nocardia brasiliensis isolates was tested. The MIC50 and MIC90 values for PA-824 were both >64 ?g/ml. The same values for BTZ043 were 0.125 and 0.250 ?g/ml. Given the MIC values for benzothiazinone (BTZ) compounds, we consider them good candidates to be tested in vivo against N. brasiliensis.

Campos-Rivera, Mayra Paola; Gonzalez-Martinez, Norma Alejandra; Ocampo-Candiani, Jorge; Cole, Stewart T.

2012-01-01

335

In Vitro Activities of Two Ketolides, HMR 3647 and HMR 3004, against Gram-Positive Bacteria  

Microsoft Academic Search

The in vitro activities of two new ketolides, HMR 3647 and HMR 3004, were tested by the agar dilution method against 280 strains of gram-positive bacteria with different antibiotic susceptibility profiles, including Staphylococcus aureus, Enterococcus faecalis, Enterococcus faecium, Streptococcus spp. (group A streptococci, group B streptococci, Streptococcus pneumoniae, and alpha-hemolytic streptococci). Seventeen erythromycin- susceptible (Em s ), methicillin-susceptible S. aureus

KUMTHORN MALATHUM; TERESA M. COQUE; KAVINDRA V. SINGH; BARBARA E. MURRAY

1999-01-01

336

Comparative In Vitro Activities of Daptomycin and Vancomycin against Resistant Gram-Positive Pathogens  

Microsoft Academic Search

The in vitro activity of daptomycin against 224 current gram-positive clinical isolates including vancomycin- resistant Enterococcus faecium (VREF), methicillin-resistant Staphylococcus aureus (MRSA), methicillin-resis- tant Staphylococcus spp. (MRSS), and penicillin-resistant Streptococcus pneumoniae (PRSP) was evaluated. The MICs at which 90% of isolates are inhibited for daptomycin and vancomycin, respectively, were as follows: MRSA, 1 and 2 mg\\/ml; MRSS, 1 and 4

D. R. Snydman; N. V. Jacobus; L. A. McDermott; J. R. Lonks; J. M. Boyce

2000-01-01

337

In vitro DNA-protective activity of roasted wheat germ and fractions thereof  

Microsoft Academic Search

An ethanolic extract of roasted wheat germ was shown to scavenge free radicals, using the DPPH-test, and to protect DNA efficiently in vitro, using the 3D-assay. The DNA-protective activity of a coffee extract was comparatively lower and strongly dependent on the concentration applied. Fractionation of the wheat germ extract by preparative HPLC demonstrated that most of the DNA protecting properties

Ulrich Krings; Lena Johansson; Holger Zorn; Ralf G. Berger

2006-01-01

338

In vitro antileishmanial activity of Adana propolis samples on Leishmania tropica : a preliminary study  

Microsoft Academic Search

Propolis (bee glue) is a natural resinous hive product, collected from various plant sources. It has attracted much attention\\u000a as a useful substance applied in medicine due to its pharmacological activities. It was aimed to investigate the in vitro\\u000a effects of an ethanolic extract of Adana propolis samples on the growth of Leishmania tropica. Parasite cells were treated with five

G. Duran; N. Duran; G. Culha; B. Ozcan; H. Oztas; B. Ozer

2008-01-01

339

In vitro imaging of human monocytic cellular activity using superparamagnetic iron oxide  

Microsoft Academic Search

The aim is to evaluate if a difference in activity of monocytic cells can be described on superparamagnetic iron oxide (SPIO)-magnetic resonance imaging (MRI) in vitro when a low concentration of SPIO is administered.Human monocytic cells were stimulated with phorbol 12-myristate 13-acetate (PMA) or left non-stimulated for 24h and then treated with SPIO with a final concentration of 7.2?g Fe\\/ml

Akihiro Nishie; Kengo Yoshimitsu; Tomohiro Nakayama; Masamitsu Hatakenaka; Hiroyuki Irie; Yoshiyuki Shioyama; Shuji Matsuura; Yunosuke Nishihara; Koji Kobayashi; Hiroshi Honda

2007-01-01

340

In vitro generation of activated natural killer cells and cytotoxic macrophages with lentinan  

Microsoft Academic Search

The in vitro effect of lentinan in inducing activation of killer cells and cytotoxic macrophages has been examined. Human peripheral blood mononuclear cells were cultured with lentinan for 2, 4 and 8 days. After 4 days cytotoxicity was increased 4% by lentinan <1,000 ng\\/ml. After 8 days, it was increased 12% by 25 and 1,000 ng\\/ml lentinan. The phenotype of

M. Tani; H. Tanimura; H. Yamaue; M. Iwahashi; T. Tsunoda; M. Tamai; K. Noguchi; K. Arii

1992-01-01

341

In vitro Antibacterial Activity of Norfloxacin and Other Agents against Ocular Pathogens  

Microsoft Academic Search

302 clinical isolates representing 16 bacterial species most often implicated in ocular infections were tested in vitro against norfloxacin and a panel of antibacterial agents. On the basis of the 90% minimal inhibitory concentration (MIC90) data, norfloxacin was 4–32 times more active than the next best antimicrobial tested against Citrobac-ter freundii, Escherichia coli, Morganellamorganii, Proteus mirabilis, Proteus vulgaris, Haemophilus influenzae,

D. L. Shungu; V. K. Tutlane; E. Weinberg; H. H. Gadebusch

1985-01-01

342

A comparative study of parthenogenic activation and in vitro fertilization of bubaline oocytes.  

PubMed

The effect of chemical activation protocols on in vitro-matured oocytes were compared to results with IVF (natural activation). Buffalo ovaries were collected in normal saline and transported to the laboratory within 2 h of slaughter. Good quality oocytes, collected by aspiration from 3 to 10 mm follicles, were matured for 22-24 h. Matured oocytes were subjected to either IVF (control) or chemical activation (treatment). For IVF, in vitro-matured oocytes were co-incubated with in vitro-capacitated approximately 1x10(6) frozen/thawed sperm of a Murrah bull and fertilized in modified synthetic oviductal fluid (mSOF) medium. Chemicals for oocytes activation comprised (a) 7% ethanol (ET) for 7 min+2.5 mM 6-dimethyl amino purine (6-DMAP) for 4h, (b) 7% ET for 7 min+10 microg/ml cycloheximide (CHX) for 6h and (c) 7% ET for 7 min+2.5 mM 6-DMAP+10 microg/ml CHX for 6 h. To study embryo development, fertilized and chemically activated oocytes were cultured in mSOF medium for up to 8 days. In this study, a mean of 1.9+/-0.02 maturable oocytes/ovary were recovered and 90.4% matured. Cleavage rate was significantly higher following ET+DMAP, ET+CHX and ET+CHX+DMAP activation (52.5%, 52.5% and 44.4%, respectively) compared to IVF (36.5%, 23.4% and 26.8%, respectively). Blastocyst development (30.9% versus 15.2%) was also significantly higher following ET+CHX+DMAP activation than IVF. The results of parthenogenesis reveal that buffalo oocytes had better inherent developmental competence and that the poor cleavage and embryo development following IVF may be due partly to the poor quality of frozen/thawed sperm, improper sperm capacitation and/or fertilization. PMID:17321079

Mishra, V; Misra, A K; Sharma, R

2006-12-30

343

Activated Rac1 GTPase translocates protein phosphatase 5 to the cell membrane and stimulates phosphatase activity in vitro.  

PubMed

Physiological studies of ion channel regulation have implicated the Ser/Thr protein phosphatase 5 (PP5) as an effector of Rac1 GTPase signaling, but direct biochemical evidence for PP5 regulation by Rac1 is lacking. In this study we used immunoprecipitation, in vitro binding, cellular fractionation, and immunofluorescence techniques to show that the tetratricopeptide repeat domain of PP5 interacts specifically and directly with active Rac1. Consequently, activation of Rac1 promoted PP5 translocation to the plasma membrane in intact cells and stimulated PP5 phosphatase activity in vitro. In contrast, neither constitutively active RhoA-V14 nor dominant negative Rac1N17, which preferentially binds GDP and retains an inactive conformation, bound PP5 or stimulated its activity. In addition, Rac1N17 and Rac1(PBRM), a mutant lacking the C-terminal polybasic region required for Rac1 association with the membrane, both failed to cause membrane translocation of PP5. Mutation of predicted contact residues in the PP5 tetratricopeptide repeat domain or within Rac1 also disrupted co-immunoprecipitation of Rac1-PP5 complexes and membrane translocation of PP5. Specific binding of PP5 to activated Rac1 provides a direct mechanism by which PP5 can be stimulated and recruited to participate in Rac1-mediated signaling pathways. PMID:19948726

Chatterjee, Anindya; Wang, Ling; Armstrong, David L; Rossie, Sandra

2009-11-30

344

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

345

In vitro induced pinocytotic activity by a juvenile hormone analogue in oocytes of Drosophila melanogaster.  

PubMed

Pinocytotic activity has been analyzed in Drosophila oocytes following either in vivo or in vitro exposure to horseradish peroxidase. The enzyme tracer gains access to the yolk spheres only when supplied to the oocyte in vivo. In oocytes cultured in vitro, peroxidase remains restricted to the residual coated vesicles and to the tubular profiles formed in excess in the cortical ooplasm. In an attempt to induce peroxidase uptake by oocytes cultured in vitro, various incubations were tested. Among these, hemolymph from both sexes is capable of promoting peroxidase uptake up to a level comparable to that detectable in vivo. On the other hand, fat body extracts fail to promote such cellular activity. Finally, the juvenile hormone analogue ZR-515 is shown to be the only factor required to promote pinocytotic activity under the experimental conditions tested. The observations are interpreted to indicate that vitellogenin has no inductive role on pinocytosis but simply acts by adhering to the forming coated vesicles which in turn are produced by the oolemma in response to the action of juvenile hormone. PMID:117896

Giorgi, F

1979-01-01

346

Potent Inhibitors of Plasmodium Phospholipid Metabolism with a Broad Spectrum of In Vitro Antimalarial Activities  

PubMed Central

We characterized the potent in vitro antimalarial activity and biologic assessment of 13 phospholipid polar head analogs on a comparative basis. There was a positive relationship between the abilities of the drugs to inhibit parasite growth in culture and their abilities to specifically inhibit phosphatidylcholine biosynthesis of Plasmodium falciparum-infected erythrocytes. Maximal activity of G25 was observed for the trophozoite stage of the 48-h erythrocytic cycle (50% inhibitory concentration, 0.75 nM), whereas the schizont and ring stages were 12- and 213-fold less susceptible. The compounds exerted a rapid nonreversible cytotoxic effect, with complete clearance of parasitemia after 5 h of contact with the mature stages. The compounds were highly specific against P. falciparum, with much lower toxicity against three other mammalian cell lines, and the in vitro therapeutic indices ranged from 300 to 2,500,000. Finally, the monoquaternary ammonium E10 and two bis-ammonium salts, G5 and G25, were similarly active against multiresistant strains and fresh isolates of P. falciparum. This impressive selective in vitro toxicity against P. falciparum strongly highlights the clinical potential of these quaternary ammonium salts for malarial chemotherapy.

Ancelin, Marie L.; Calas, Michele; Vidal-Sailhan, Valerie; Herbute, Serge; Ringwald, Pascal; Vial, Henri J.

2003-01-01

347

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

348

Quantitative studies on the in vitro metabolic activation of dimethylnitrosamine by rat liver postmitochondrial supernatant  

SciTech Connect

The metabolic activation of dimethylnitrosamine (DMN) to mutagenic and/or cytotoxic intermediates in vitro has been characterized and the relationship between DMN demethylase and ethoxyresorufin-O-deethylase (EROD) or ethylmorphine-N-demethylase (EMND) has been evaluated. A mammalian assay system which uses the postmitochondrial supernatant (S-15 fraction) prepared from a rat liver homogenate as an enzyme source and V79 Chinese hamster cells as targets for chemically induced damage was used. The enzyme pattern of the S-15 fraction was altered by pretreatment of experimental animals in vivo and/or by the use of enzyme inhibitors in vitro. The results of these studies indicate that the concentration of S-15 fraction in the reaction mixture can markedly influence the degree of DMN-induced cytotoxicity when it is metabolized in vitro and that the degree of DMN-induced cytotoxicity and mutagenicity are linearly related. The degree of cytotoxicity and mutagenicity induced in V79 cells by DMN does not correlate with EROD activity (a measure of 3-methylcholanthrene-inducible mixed-function oxidases) nor with EMND activity (a measure of phenobarbital-inducible mixed function oxidases) in the S-15 fraction. 28 references, 4 figures.

Doolittle, D.J.; Goodman, J.I.

1984-08-01

349

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

PubMed Central

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

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

2013-01-01

350

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

PubMed Central

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

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

1998-01-01

351

In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity at CYP450  

Microsoft Academic Search

Synthesis and in vitro cytotoxicity assays of new anthranilamide MDR modulators have been performed to assess their inhibition potency of the P-glycoprotein (P-gp) transporter. The aromatic spacer group between nitrogen atoms (N1 and N2) in the known inhibitor XR9576 was replaced with a flexible alkyl chain of 2 to 6 carbon atoms in length. 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline and their open-chain N-methylhomoveratrylamine counterparts

Philippe Labrie; Shawn. P. Maddaford; Jacques Lacroix; Concettina Catalano; David K. H. Lee; Suman Rakhit; René C. Gaudreault

2006-01-01

352

Chronic intrauterine pulmonary hypertension increases endothelial cell Rho kinase activity and impairs angiogenesis in vitro  

PubMed Central

Persistent pulmonary hypertension of the newborn (PPHN) is characterized by endothelial dysfunction and decreased vascular growth. The role of Rho kinase activity in modulating endothelial function and regulating angiogenesis during normal lung development and in PPHN is unknown. We hypothesized that PPHN increases Rho kinase activity in fetal pulmonary artery endothelial cells (PAECs) and impairs angiogenesis in vitro. Proximal PAECs were harvested from fetal sheep with partial ligation of the ductus arteriosus in utero (PPHN) and age-matched controls. Rho kinase activity was measured by RhoA, Rho GTP, and phosphorylated MYPT-1 protein content. The effects of Rho kinase activity on angiogenesis, endothelial nitric oxide (NO) synthase (eNOS) protein expression, and NO production were determined in normal and PPHN PAECs. Angiogenesis was assessed by tube formation in vitro with/without Y-27632 (a Rho kinase inhibitor) and calpeptin (a Rho kinase activator) in the presence/absence of N-nitro-l-arginine (l-NA, an NOS inhibitor). RhoA, Rho GTP, and phosphorylated MYPT-1 protein were increased in PPHN PAECs. Tube formation was reduced 29% in PPHN PAECs (P < 0.001) and increased with Y-27632 treatment in normal and PPHN PAECs, with PPHN PAECs achieving levels similar to those of normal PAECs. l-NA inhibited the Y-27632-induced increase in tube formation in normal, but not PPHN, PAECs. Calpeptin reduced tube formation in normal and PPHN PAECs. eNOS expression was reduced 42% in PPHN PAECs (P < 0.01). Y-27632 increased eNOS protein and NO production in normal and PPHN PAECs. Calpeptin decreased eNOS protein only in normal PAECs but reduced NO production in normal and PPHN PAECs. We conclude that Rho kinase activity is increased in PPHN PAECs and impairs angiogenesis and downregulates eNOS protein and NO production in vitro.

Gien, Jason; Seedorf, Gregory J.; Balasubramaniam, Vivek; Tseng, Nancy; Markham, Neil; Abman, Steven H.

2008-01-01

353

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

354

Comparative In Vitro Activities of Nemonoxacin (TG-873870), a Novel Nonfluorinated Quinolone, and Other Quinolones against Clinical Isolates ?  

PubMed Central

The in vitro antibacterial activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, against 770 clinical isolates were investigated. Nemonoxacin (tested as its malate salt, TG-875649) showed better in vitro activity than ciprofloxacin and levofloxacin against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenzae. The in vitro activity of TG-875649 was also comparable to or better than that of moxifloxacin against these pathogens, which included ciprofloxacin-resistant, methicillin-resistant Staphylococcus aureus and levofloxacin-resistant Streptococcus pneumoniae.

Lauderdale, Tsai-Ling; Shiau, Yih-Ru; Lai, Jui-Fen; Chen, Hua-Chien; King, Chi-Hsin R.

2010-01-01

355

In vitro and in vivo immunosuppressive activity of Spica Prunellae ethanol extract on the immune responses in mice  

Microsoft Academic Search

The immunosuppressive activity of the ethanol extract of Spica Prunellae (Prunella vulgaris fruiting spikes) (EESP) consisting of a mixture of triterpenoids, flavonoids, tannins and polysaccharide was studied on the immune responses in mice. The effects of EESP on mice splenocyte proliferation in vitro were measured. EESP significantly suppressed concanavalin A (Con A)- and lipopolysaccharide (LPS)-stimulated splenocyte proliferation in vitro in

Hong-Xiang Sun; Feng Qin; Yuan-Jiang Pan

2005-01-01

356

In vitro activity of nitroxoline against clinical isolates of Candida species.  

PubMed

The in vitro antifungal activity of the quinoline nitroxoline has been compared with those of amphotericin B, flucytosine, and two azoles, miconazole and ketoconazole, against clinical isolates of Candida spp. A total of 186 isolates of 10 species of Candida and two culture collection strains were tested by an agar-dilution technique. Nitroxoline was highly active against Candida spp. MICs for nitroxoline ranged between 0.25-2 micrograms ml-1 for 186 representative strains. With MIC90 as the measure of antifungal activity, nitroxoline appeared to be superior to the imidazoles studied. Data for individual species of Candida revealed that the activities of nitroxoline and amphotericin B were generally just as effective against C. albicans, whereas flucytosine was the most active agent against Candida spp. PMID:1803236

Hernández Molina, J M; Llosá, J; Ventosa, A

357

Nitric oxide - an activating factor of adenosine deaminase 2 in vitro.  

PubMed

In this study we have investigated the effect of reactive oxygen species produced by some chemicals in aqueous solutions on activity of adenosine deaminase 2 (ADA2) purified from human blood plasma. An activating effect on ADA2 was observed in vitro with sodium nitroprusside (SNP), the source of NO (nitrosonium ions NO(-) in aqueous solutions). Not SH-groups of cysteine but other amino acid residues sensitive to NO were responsible for ADA2 activation. The SNP-derived activation was more pronounced when purified ADA2 was preincubated with heparin and different proteins as an experimental model of the protein environment in vivo. The most effective was heparin, which is known for its ability to regulate enzyme and protein functions in extracellular matrix. We conclude that ADA2 is a protein with flexible conformation that is affected by the protein environment, and it changes its activity under oxidative (nitrosative) stress. PMID:22339638

Sargisova, Ye G; Andreasyan, N A; Hayrapetyan, H L; Harutyunyan, H A

2012-01-01

358

In vitro hypoglycemic activity of methanolic extract of some indigenous plants.  

PubMed

Pakistan is rich in medicinally important plants and has ancient herbal treatment methods. Present work is based on the study of six indigenous plants Eugenia jambolana, Lawsonia inermis, Momordica charantia, Morus alba, Nigella sativa and Trigonella foenum graecum which show the inhibitory effect of glucose utilization, and are in use as hypoglycemic agents of varying degree in traditional system of medicine. The glucose uptake activity of (methanolic extracts) of these plants was tested in vitro and glucose was estimated by glucose oxidase method. The results in three different media revealed that, hypoglycemic activity is more prominent in neutral and basic media as compared to acidic medium. PMID:17604247

Arayne, M Saeed; Sultana, Najma; Mirza, Agha Zeeshan; Zuberi, M Hashim; Siddiqui, Farhan Ahmed

2007-10-01

359

Activation of human mononuclear cells by porcine biologic meshes in vitro  

Microsoft Academic Search

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

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

2010-01-01

360

In vitro activities of ICI 194008 and ICI 193428, two new cephem antimicrobial agents.  

PubMed Central

The in vitro activities of two new cephem antibiotics, ICI 193428 and ICI 194008, were compared with those of cefpirome, cefotaxime, ceftazidime, and piperacillin. Essentially all strains of the family Enterobacteriaceae were inhibited by both study drugs at concentrations of less than or equal to 4 micrograms/ml. Both new cephems were comparable to ceftazidime against Pseudomonas aeruginosa (MIC for 90% of strains, 8 micrograms/ml) and were the most active agents tested against Pseudomonas maltophilia (MIC for 90% of strains, 16 micrograms/ml).

Allan, J D; Eliopoulos, G M; Reiszner, E; Moellering, R C

1987-01-01

361

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

SciTech Connect

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

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

2008-01-01

362

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

PubMed

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

Feng, Qin; Gou, Xiao-Jun; Meng, Sheng-Xi; Huang, Cheng; Zhang, Yu-Quan; Tang, Ya-Jun; Wang, Wen-Jing; Xu, Lin; Peng, Jing-Hua; Hu, Yi-Yang

2013-03-19

363

Plasminogen activators in normal and malignant oral epithelium in vivo and in vitro.  

PubMed

Urokinase-type (uPA) and tissue-type (tPA) plasminogen activators were identified by fibrinolytic autography in the sulcus epithelium of human gingival mucosa but not in the orthokeratinized gingival epithelium. Fibrinolytic activity was present only over blood vessels in frozen sections of oral squamous cell carcinomas, the malignant epithelial cells showing no plasminogen activator activity. Plasminogen activators could not be demonstrated in either the sulcus or gingival epithelium by immunofluorescence, but both uPA and tPA were found in occasional squamous carcinoma cells. Fibrinolytic activity of culture fluids from epithelial explants grown in vitro from human gingival mucosa showed marked variation, but activity was much higher in the culture supernatants than in the cell lysates. Fibrinolytic activity of culture fluids from epithelial explants of squamous cell carcinomas was low both in supernatants and lysates. Zymogram overlays of sodium dodecyl sulphate-polyacrylamide electrophoretic gels from culture supernatants showed that the low fibrinolytic activity of culture supernatants of oral squamous cell carcinomas was due to the associated presence of plasminogen activator inhibitors. The fibrinolytic activity in the zymogram was due predominantly to uPA but some lysis was due also to tPA. PMID:1417524

Barlow, Y; Southam, J C

1992-09-01

364

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

PubMed Central

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

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

1999-01-01

365

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

PubMed

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

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

2012-10-23

366

[Effects of cornel iridoid glycoside on activity of cholinesterases in vitro].  

PubMed

The purpose of the present study was to investigate the effects of cornel iridoid glycoside (CIG) on the activity of cholinesterases in vitro, and to investigate the mechanism of CIG's treating Alzheimer's disease (AD). The sources of cholinesterases were prepared from human blood cells, rat brain homogenate and human blood plasma, respectively. The biochemical methods were used to detect the activity of acetylcholine esterase (AChE) and butyryl cholinesterase (BuChE) to investigate the influence of CIG on cholinesterases. The results showed that CIG inhibited the activity of AChE of human blood cells and rat brain homogenate, with the 50% inhibition rate (IC50) of 1.6 g . L-1 and 3.3 g . L-1, respectively; and the inhibition of AChE of CIG is reversible. CIG also inhibited the activity of BuChE of human blood plasma, with the IC50 of 2.9 g . L-1. In conclusion, CIG can inhibit the activity of AChE and BuChE in vitro, which may be one of the mechanisms of CIG to treat AD. PMID:23944063

Chu, Si-Juan; Zhang, Lan; Liu, Gang; Zhou, Wen-Xia; Li, Lin

2013-05-01

367

In vitro antioxidant and antiproliferative activities of flavonoids from Ailanthus excelsa (Roxb.) (Simaroubaceae) leaves.  

PubMed

The present study aimed to investigate the chemical composition, and the antioxidant and antiproliferative activities of Ailanthus excelsa, a plant used in Egyptian traditional medicine. Chromatographic separation of a methanol extract of A. excelsa leaves yielded four flavones, namely apigenin (1), apigenin 7-O-beta-glucoside (2), luteolin (3), and luteolin 7-O-beta-glucoside (4), and seven flavonols, namely kaempferol (5), kaempferol 3-O-alpha-arabinoside (6), kaempferol 3-O-beta-galactoside (7), quercetin (8), quercetin 3-O-alpha-arabinoside (9), quercetin 3-O-beta-galactoside (10), and quercetin 3-O-rutinoside (11). The A. excelsa extract tested in different in vitro systems (DPPH and FRAP assays) showed significant antioxidant activity. The potential antiproliferative activity of the A. excelsa extract and isolated flavonoids against five human cancer cell lines such as ACHN, COR-L23, A375, C32, and A549 was investigated in vitro by the SRB assay in comparison with one normal cell line, 142BR. The extract exhibited the highest inhibitory activity against C32 cells with an IC50 value of 36.5 microg ml(-1). Interesting activity against COR-L23 was found with 10 (IC50 value of 3.2 microg ml(-1)). Compounds 1 and 3 inhibited cell growth in both amelanotic melanoma and malignant melanoma cells. PMID:20469635

Said, Ataa; Tundis, Rosa; Hawas, Usama W; El-Kousy, Salah M; Rashed, Khaled; Menichini, Federica; Bonesi, Marco; Huefner, Antje; Loizzo, Monica Rosa; Menichinib, Francesco

368

Potential antioxidant activity of celecoxib and amtolmetin guacyl: in vitro studies.  

PubMed

1. In vitro studies of the potential antioxidant activity of the selective cyclo-oxygenase-2 inhibitor celecoxib and the non-steroid anti-inflammatory drug amtolmetin guacyl (AMG) were carried out. The study included experiments on the ability of these drugs to affect some indices of the oxidative stress [lipid peroxidation (LP), activity of antioxidant enzymes, glutathione (GSH) level] in rat stomach and colon mucosa and in liver. 2. Celecoxib and AMG did not change the activity of the enzymes GSH-peroxidase, oxidased glutathione (GSSG)-reductase and glucose-6-phosphate-dehydrogenase, as well as the GSH level in all tissue preparations. An increased superoxide dismutase (SOD) activity and a tendency to a decreased Fe/ascorbic acid-induced LP in stomach and colon mucosa were found, but only in the presence of AMG. 3. In the liver, both celecoxib and AMG decreased spontaneous and Fe/ascorbic acid-induced LP. SOD activity was enhanced only in the presence of AMG. 4. Experiments aimed at studying celecoxib and AMG in free oxygen radical-generating systems were also carried out. AMG and tolmetin (the main metabolite of AMG) inhibited OH*-provoked deoxyribose degradation in a Fenton system. Celecoxib had no effect on free radicals when tested in the same system. 5. In conclusion, the results of the present in vitro studies suggest that AMG and celecoxib possess antioxidant and metal-chelating abilities, which might contribute to their beneficial effects. PMID:17199871

Kirkova, M; Alexandova, A; Kesiova, M; Tsvetanova, E; Georgieva, A; Todorov, S

2007-01-01

369

[In vitro activity of doripenem against strains from pediatric diseases and strains causing purulent meningitis].  

PubMed

This study evaluated the in vitro activity of doripenem (DRPM) against 200 Streptococcus pneumoniae and 197 Haemophilus influenzae from children and adults in 2007, 50 H. influenzae type b in 2006, 20 Listeria monocytogenes in 1990-2005, 23 Neisseria meningitidis in 2007-2009 and 83 Bordetella pertussis in 1989-2003. All strains were isolated from Japanese clinical facilities. We also investigated in vitro activity of other carbapenems (meropenem, imipenem, panipenem, biapenem), cephems (ceftriaxone, cefotaxime), ampicillin and clarithromycin. The all MICs were determined by a broth micro dilution method or an agar dilution method according to CLSI. The MIC90(s) of DRPM against S. pneumoniae and H. influenzae from children were 0.25 microg/mL, 1 microg/mL, respectively, which were similar to strains from adults. These results suggested that antibacterial activity of DRPM is not variable by patient's age. DRPM also showed excellent activities against H. influenzae type b, L. monocytogenes and N. meningitidis, which cause purulent meningitis, and B. pertussis causing whooping cough more than the other carbapenems. DRPM showed superior activities against serious strains of pediatric infection diseases. PMID:23593734

Ohta, Merime; Toba, Shinsuke; Ito, Akinobu; Nakamura, Rio; Tsuji, Masakatsu

2012-12-01

370

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

PubMed Central

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

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

1998-01-01

371

In vitro epsilon RNA-dependent protein priming activity of human hepatitis B virus polymerase.  

PubMed

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. PMID:22379076

Jones, Scott A; Boregowda, Rajeev; Spratt, Thomas E; Hu, Jianming

2012-02-29

372

Differential effects of low glucose concentrations on seizures and epileptiform activity in vivo and in vitro.  

PubMed

In vivo, severe hypoglycemia is frequently associated with seizures. The hippocampus is a structure prone to develop seizures and seizure-induced damage. Patients with repeated hypoglycemic episodes have frequent memory problems, suggesting impaired hippocampal function. Here we studied the effects of moderate hypoglycemia on primarily generalized flurothyl-induced seizures in vivo and, using EEG recordings, we determined involvement of the hippocampus in hypoglycemic seizures. Moderate systemic hypoglycemia had proconvulsant effects on flurothyl-induced clonic (forebrain) seizures. During hypoglycemic seizures, seizure discharges were recorded in the hippocampus. Thus, we continued the studies in combined entorhinal cortex-hippocampus slices in vitro. However, in vitro, decreases in extracellular glucose from baseline 10 mM to 2 or 1 mM did not induce any epileptiform discharges. In fact, low glucose (2 and 1 mM) attenuated preexisting low-Mg2+-induced epileptiform activity in the entorhinal cortex and hippocampal CA1 region. Osmolarity compensation in low-glucose solution using mannitol impaired slice recovery. Additionally, using paired-pulse stimuli we determined that there was no impairment of GABAA inhibition in the dentate gyrus during glucopenia. The data strongly indicate that, although forebrain susceptibility to seizures is increased during moderate in vivo hypoglycemia and the hippocampus is involved during hypoglycemic seizures, glucose depletion in vitro contributes to an arrest of epileptiform activity in the system of the entorhinal cortex-hippocampus network and there is no impairment of net GABAA inhibition during glucopenia. PMID:16553614

Kirchner, Anne; Velísková, Jana; Velísek, Libor

2006-03-01

373

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

PubMed

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

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

2012-04-20

374

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

PubMed Central

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

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

1981-01-01

375

Inhibition of HIV-1 replication by ribozymes that show poor activity in vitro.  

PubMed

Self-cleaving RNAs (ribozymes) can be engineered to cleave target RNAs of choice in a sequence-specific manner (1). Consequently, they could be used to inhibit virus replication or to analyse host gene function in vivo. However, ribozymes that are catalytic in vitro are generally disappointing when analysed in cells unless expressed at high levels relative to their target RNAs (2, 3). Here we provide evidence that this can be overcome by optimizing ribozyme structure using cellular rather than cell-free assays. We show that ribozymes of relatively long flanking complementary regions (FCRs), while poor catalysts in vitro, can produce profound inhibition of HIV replication in cells. By examining a series of ribozymes in which the FCRs vary from 9 to 564 nucleotides, we establish that the optimum length for activity in the cell is > or = 33 nucleotides. PMID:8255782

Crisell, P; Thompson, S; James, W

1993-11-11

376

Flavone C-glycosides from the leaves of Lophatherum gracile and their in vitro antiviral activity.  

PubMed

Four new flavone C-glycosides, luteolin 6-C-?-L-arabinopyranosyl-7-O-?-D-glucopyranoside, apigenin 6-C-?-D-galactopyranosiduronic acid (1???2)-?-L-arabinopyranoside, luteolin 6-C-?-D-galactopyranosiduronic acid (1???2)-?-L-arabinopyranoside, and luteolin 6-C-?-D-glucopyranosiduronic acid (1???2)-?-L-arabinofuranoside, along with three known ones, were isolated from the leaves of Lophatherum gracile. The structures of the new compounds were elucidated by extensive spectroscopic methods as well as acid hydrolysis. All the flavone glycosides isolated from this plant were screened for their in vitro antiviral activity against respiratory syncytial virus (RSV) with cytopathic effect (CPE) reduction assay, and several flavone 6-C-monoglycosides showed potent in vitro anti-RSV effect. PMID:21870321

Wang, Ying; Chen, Mei; Zhang, Jing; Zhang, Xiao-Li; Huang, Xiao-Jun; Wu, Xin; Zhang, Qing-Wen; Li, Yao-Lan; Ye, Wen-Cai

2011-08-25

377

In vitro antifungal activity and toxicity of itraconazole in DMSA-PLGA nanoparticles.  

PubMed

Itraconazole (ITZ) is a drug used to treat various fungal infections and may cause side effects. The aim of this study was to develop and evaluate the in vitro activity of DMSA-PLGA nanoparticles loaded with ITZ against Paracoccidioides brasiliensis, as well as their cytotoxicity. Nanoparticles were prepared using the emulsification-evaporation technique and characterized by their encapsulation efficiency, morphology (TEM), size (Nanosight) and charge (zeta potential). Antifungal efficacy in P. brasiliensis was determined by minimal inhibition concentration (MIC), and cytotoxicity using MTT assay. ITZ was effectively incorporated in the PLGA-DMSA nanoparticles with a loading efficiency of 72.8 +/- 3.50%. The shape was round with a solid polymeric structure, and a size distribution of 174 +/- 86 nm (Average +/- SD). The particles were negatively charged. ITZ-NANO presented antifungal inhibition (MIC = 6.25 ug/mL) against P. brasiliensis and showed lower in vitro cytotoxicity than free drug (ITZ). PMID:21449386

Cunha-Azevedo, Elaine P; Silva, Jaqueline R; Martins, Olimpia P; Siqueira-Moura, Marigilson P; Bocca, Anamélia L; Felipe, Maria Sueli S; Tedesco, Antonio C; Azevedo, Ricardo B

2011-03-01

378

Conditions Required for the Rapid Activation In Vitro of the Chloroplast Fructose-1,6-bisphosphatase  

PubMed Central

Conditions required for the reductive activation of purified, spinach chloroplast fructose-1,6-bisphosphatase (EC 3.1.3.11) have been determined in vitro. Full reductive activation was observed only when fructose-1,6-bisphosphate and Mg2+ were present at the same time as the reducing agent (dithiothreitol). Reduction in the absence either of fructose-1,6-bisphosphate or of Mg2+ slowly and irreversibly inactivated the enzyme. The concentration of fructose-1,6-bisphosphate that must be present during reduction for maximum activation depends upon the divalent cation present: it is highest with Mg2+, lower with Ca2+, and lowest when both Mg2+ and Ca2+ are present. A scheme for the reductive activation and inactivation of the enzyme is presented.

Rosa, Luciana; Whatley, F. Robert

1984-01-01

379

Evaluation of African medicinal plants for their in vitro trypanocidal activity.  

PubMed

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 fro cytotoxicity for a human fibroblast cell-line (WI-38). The trypanocidal activity of the natural compounds berberine and harmane, both documented as being trypanocidal, was also evaluated. Promising trypanocidal activity with IC50 values below 10 micrograms/ml was found in 32 extracts of 13 plant species. The most active extracts with IC50 below 1 microgram/ml were derived from Annona senegalensis, Bussea occidentalis and Physalis angulata. The plant extracts showed a modest selectivity index, in contrast to commercially available trypanocides which have a more distinct selective toxicity against trypanosomes. PMID:9121161

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

1996-12-01

380

In vitro effects of alloxan-vanadium combination on lipid peroxidation and on antioxidant enzyme activity.  

PubMed

1. The in vitro effects of alloxan, dialuric acid and vanadium ions, alone or in combination, on lipid peroxidation and on antioxidant enzyme activity in rat liver and kidney were studied. 2. Unlike alloxan, alloxan-glutathione (GSH) and dialuric acid increased lipid peroxidation, which could be explained by the decreased activity of catalase and GSH peroxidase during incubation. 3. Vanadium(IV) ions increased the amount of thiobarbituric acid-reacting substances, but neither vanadium(IV) nor vanadium(V) changed the enzyme activity. 4. The combination of vanadium ions and alloxan-GSH or dialuric acid had no additive effect on lipid peroxidation. Vanadium ions decreased the dialuric acid-induced inhibition of catalase activity. 5. The present results suggest the therapeutic value of vanadium as an antidiabetic agent. PMID:9703225

Alexandrova, A; Kirkova, M; Russanov, E

1998-09-01

381

In vitro activity of sitafloxacin compared with several fluoroquinolones against Streptococcus anginosus and Streptococcus constellatus.  

PubMed

The in vitro activities of sitafloxacin and seven other fluoroquinolones a (ciprofloxacin, tosufloxacin, sparfloxacin, levofloxacin, T-3811ME, moxifloxacin and trovafloxacin) were examined by the microdilution method against 79 clinically isolated 'Streptococcus milleri' group (SMG) microorganisms. No statistically significant differences were found between the minimum inhibitory concentrations (MIC(50) and MIC(90)) against Streptococcus anginosus and Streptococcus constellatus. Sitafloxacin was the most active agent of the eight fluoroquinolones tested against SMG, with a MIC(90) of 0.06 microg/mL, which was 8 times more active than ciprofloxacin and 16 times more active than levofloxacin. Although none of the SMG strains showed high resistance to any of the fluoroquinolones tested, three agents (trovafloxacin, sitafloxacin and T-3811ME) had low MICs against 23 SMG strains against which levofloxacin had a MIC> 1 microg/mL. In conclusion, several fluoroquinolones have low MICs against SMG, but sitafloxacin has the lowest. PMID:16417990

Yamamoto, Natsuo; Fujita, Jiro; Shinzato, Takashi; Higa, Futoshi; Tateyama, Masao; Tohyama, Masato; Nakasone, Isamu; Yamane, Nobuhisa

2006-01-18

382

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

2007-03-15

383

[Antiviral activity of different drugs in vitro against viruses of bovine infectious rhinotracheitis and bovine diarrhea].  

PubMed

In vitro experiments studied the antiviral activity of 11 different drugs against viruses of bovine infective rhinotracheitis (BIRT) and bovine viral diarrhea (BVD). The 50% inhibiting concentrations of the test agents were determined in the monolayers of MDBK and KCT cell cultures. Only did phosprenyl show a virucidal activity against BIRT virus. All the tested drugs significantly inhibited the reproduction of BIRT virus in the sensitive MDBK cell cultures. Thus, bromuridin, acyclovir, ribavirin and methisazonum inhibited the virus by > or = 100,000 times; liposomal ribavirin, gossypolum, anandinum, polyprenolum, phosprenyl, by 1000-10,000 times; eracond and argovit, by 100 times. In experiments on BVD virus, the cultured KCT cells displayed the antiviral activity of bromuridin, phosprenil, polyprenolum, methisazonum, acyclovir, gossypolum, argovit, and ribavirin (in two variants), which caused a statistically significant (100-10,000-fold) decrease in the productive activity of this virus. Eracond and anandid proved to be ineffective. PMID:15529864

Glotov, A G; Glotova, T I; Sergeev, A A; Belkina, T V; Sergeev, A N

384

Synthesis of dimeric phenol derivatives and determination of in vitro antioxidant and radical scavenging activities.  

PubMed

In this study, di(2,6-dimethylphenol) (Di-DMP), di(2,6-diisopropylphenol) (Di-DIP, dipropofol) and di(2,6-di-t-butylphenol) (Di-DTP) were synthesized by the reaction of monomeric phenol derivatives with catalytic CuCl(OH). TMEDA and Na2S2O4. Their antioxidant capacity and radical scavenging activity were examined using different in vitro methodologies such as 1,1-diphenyl-2-picryl-hydrazyl (DPPH*) free radical scavenging, 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical scavenging activity, total antioxidant activity by ferric thiocyanate, total reducing power by potassium ferricyanide reduction method, superoxide anion radical scavenging, hydrogen peroxide scavenging and ferrous ions chelating activities. PMID:18237020

Güllçin, Ilhami; Da?tan, Arif

2007-12-01

385

In vitro methods for evaluating the in vivo effectiveness of dosage forms of microparticulate or nanoparticulate active agent compositions  

US Patent & Trademark Office Database

Disclosed are in vitro methods for evaluating the in vivo redispersibility of dosage forms of poorly water-soluble active agents. The methods utilize media representative of in vivo human physiological conditions.

Cooper; Eugene R. (Berwyn, PA); Bullock; John A. (King of Prussia, PA); Chippari; John R. (Phonenixville, PA); Schaefer; John L. (Gilbertsville, PA); Patel; Rakesh A. (Bensalem, PA); Jain; Rajeev (Farmingham, MA); Strasters; Joost (Exton, PA); Ryde; Niels P. (Malvern, PA); Ruddy; Stephen B. (Schwenksville, PA)

2012-11-13

386

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

EPA Science Inventory

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

387

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

PubMed

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

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

2013-06-18

388

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

PubMed Central

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

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

2013-01-01

389

In vitro activity of extracts and isolated polyphenols from West African medicinal plants against Plasmodium falciparum.  

PubMed

The aim of the study was to screen 11 selected traditional medicinal plants from West Africa for their in vitro antiplasmodial activity in order to determine the activity of single and of combination of plant extracts and to examine the activity of isolated pure compounds. Ethanolic and aqueous extracts of the 11 selected plants and pure compounds from Phyllanthus muellerianus and Anogeissus leiocarpus were tested in vitro against Plasmodium falciparum 3D7. Proliferation inhibitory effects were monitored after 48 h. Among the plants and pure compounds investigated in this study, geraniin from P. muellerianus, ellagic, gentisic, and gallic acids from A. leiocarpus, and extracts from A. leiocarpus, P. muellerianus and combination of A. leiocarpus with P. muellerianus affected the proliferation of P. falciparum most potently. Significant inhibitory activity was observed in combination of A. leiocarpus with P. muellerianus (IC(50)?=?10.8 ?g/ml), in combination of A. leiocarpus with Khaya senegalensis (IC(50)?=?12.5 ?g/ml), ellagic acid (IC(50)?=?2.88 ?M), and geraniin (IC(50)?=?11.74 ?M). In general growth inhibition was concentration-dependent revealing IC(50) values ranging between 10.8 and -40.1 ?g/ml and 2.88 and 11.74 ?M for plant extracts and pure substances respectively. Comparison with literature sources of in vivo and in vitro toxicity data revealed that thresholds are up to two times higher than the determined IC(50) values. Thus, the present study suggests that geraniin from P. muellerianus; ellagic acid, gallic acid, and gentisic acid from A. leiocarpus; and combination of extracts from A. leiocarpus with either P. muellerianus or K. senegalensis could be a potential option for malaria treatment. PMID:22476602

Ndjonka, Dieudonné; Bergmann, Bärbel; Agyare, Christian; Zimbres, Flávia M; Lüersen, Kai; Hensel, Andreas; Wrenger, Carsten; Liebau, Eva

2012-04-05

390

Reverse transcriptase activity of hepatitis B virus polymerase in eukaryotic cell extracts in vitro.  

PubMed

In hepadnaviruses, reverse transcription is primed by the viral reverse transcriptase (RT) and requires the specific interaction between the RT and the viral RNA encapsidation signal termed e. To study the activity of the RT in vitro, the current procedure uses in vitro translated duck hepatitis B virus polymerase, but not the hepatitis B virus polymerase itself, in the rabbit reticulocyte lysate expression system. Here, the hepatitis B virus (HBV) polymerase has been successfully expressed in a translational extract that was obtained from monolayer human hepatocyte cells HuH-7. The translated polypeptide retained the RNA-directed polymerase (reverse transcriptase) activity on the viral RNA template containing the e signal. We suggest that the reverse transcription event of the viral RNA coding for the polymerase and containing an e structure is concomitant to the translation of the viral polymerase to the messenger RNA. In contrast to the duck polymerase, only a fraction of the reverse transcribed complementary DNA (cDNA) was covalently bound to the HBV polymerase in this system. When the e signal was missing on the mRNA, the translated full-length HBV polymerase could not reverse transcribe the viral RNA template. A truncated HBV polymerase that was lacking the YMDD catalytic active site for the initiation of reverse transcription was unable to reverse transcribe the viral mRNA template containing the e signal. The reverse transcription activity could also be partially inhibited by employing nucleoside analogues, such as 2'-3'-dideoxy-3'-thiacytidine (3TC; lamivudine) in the expression system. The procedure described here provides a method for the in vitro screening of new anti-HBV compounds directed against wild- type and mutants of this crucial viral protein, the HBV polymerase, without the use of animals (ducks) or animal extracts (rabbit reticulocyte lysate). PMID:18841316

Favre, Daniel

2008-01-01

391

In vitro and in vivo antiproliferative activity of laherradurin and cherimolin-2 of Annona diversifolia Saff.  

PubMed

Acetogenins from Annonaceae (ACG) are potent inhibitors of the mitochondrial complex I, they present cytotoxic activity on neoplasic lines, including those with multiresistance to drugs. In vivo antitumor activities of some ACG have been reported; however, no information is available regarding the relationship between their cytotoxic activity in cell cultures and their antiproliferative action in vivo. Laherradurin and cherimolin-2 acetogenins were isolated from Annona diversifolia seeds, and their inhibitory potential was analysed in vitro on HeLa and SW-480 cells. Doses containing 1, 10, 100 and 500 times the IC50 obtained from the proliferation assays and multiplied by the weight of the animal, were injected once daily into athymic mice bearing these cancer cell lines; their effect upon tumor growth was measured over a period of 20 days. Laherradurin was more active than cherimolin-2, and it showed in in vitro proliferation assays a similar IC50 in both neoplasic lines. In athymic mice, laherradurin administered in 10x, 100x and 500x doses, reduced the size of HeLa tumors, and with 100x and 500x doses, affected the SW-480 tumor development. These doses were similar to results found with the control drug doxorubicin (p < or = 0.05). On the other hand, cherimolin-2 had an effect on HeLa tumors cells at 100x and 500x doses (p < or = 0.05). PMID:19170140

Schlie-Guzmán, María Adelina; García-Carrancá, Alejandro; González-Esquinca, Alma Rosa

2009-08-01

392

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

SciTech Connect

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 {mu} g/ml, in a dose dependant manner. On the other hand potassium humate, at 40 {mu} g/ml, significantly inhibited the release of TNF-alpha, IL-1 beta, 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.

van Rensburg, C.E.J.; Naude, P.J. [University of Pretoria, Pretoria (South Africa)

2009-08-15

393

Identification of the active metabolite of ticlopidine from rat in vitro metabolites  

PubMed Central

Ticlopidine is a well-known anti-platelet agent, but is not active by itself in vitro. We identified a metabolite with anti-platelet activity, which was generated after incubation of 2-oxo-ticlopidine with phenobarbital-induced rat liver homogenate in vitro. An active moiety (UR-4501) was isolated by high-performance liquid chromatography after large-scale preparation of metabolites. The chemical structure of UR-4501 was determined by a combination of liquid chromatography mass/mass spectrometry (LC/MS/MS) and nuclear magnetic resonance (NMR) analysis. UR-4501 produced a concentration-dependent inhibition (3–100 ?M) of ADP (10 ?M)-induced human platelet aggregation, whereas 2-oxo-ticlopidine (3–100 ?M) did not elicit inhibitory responses. UR-4501 (10–100 ?M) strongly inhibited ADP- and collagen-induced aggregation and slightly inhibited thrombin-induced aggregation. The inhibition of rat washed platelet aggregation by UR-4501 (100 ?M) persisted, even after the platelets had been washed twice. These results suggest that UR-4501 is the molecule responsible for the in vivo activities of ticlopidine.

Yoneda, Kenji; Iwamura, Ryou; Kishi, Hiroko; Mizukami, Yoichi; Mogami, Kimiko; Kobayashi, Sei

2004-01-01

394

Cocoa flavanols and procyanidins can modulate the lipopolysaccharide activation of polymorphonuclear cells in vitro.  

PubMed

Flavanols and procyanidins isolated from cocoa have been reported to possess multiple activities potentially relevant to oxidant defenses, vascular function, and immune function. In a combination of in vivo and in vitro studies, we and others have observed that cocoa can be an anti-inflammatory modulator and that compounds in cocoa are capable of modulating eicosanoid production, platelet aggregation, and the pool size of nitric oxide. The present study extends these findings by examining the in vitro effects of cocoa procyanidins on polymorphonuclear cells (PMNs). PMNs, part of the innate arm of the immune system, represent 50-60% of the total peripheral white blood cells and are the first cells to be recruited to the sites of inflammation or injury secondary to bacterial infections. Herein, we demonstrate that certain flavanols and procyanidins isolated from cocoa can moderate a subset of signaling pathways derived from lipopolysaccharide (LPS) stimulation of PMNs, mainly, PMN oxidative bursts and activation markers, and they can influence select apoptosis mechanisms. We hypothesize that flavanols and procyanidins can decrease the impact of LPS on the N-formyl-Met-Leu-Phe-primed PMN ability to generate reactive oxygen species by partially interfering in activation of the mitogen-activated protein kinase pathway. PMID:19298189

Kenny, Thomas P; Shu, Shang-an; Moritoki, Yuki; Keen, Carl L; Gershwin, M Eric

2009-02-01

395

Individual and combinatory effects of soy isoflavones on the in vitro potentiation of lymphocyte activation.  

PubMed

Daidzein and genistein are two prominent soy isoflavones that have been reported as promising protectors against cancers at many sites. In a study focusing on the chemopreventive mechanisms, we previously demonstrated that daidzein was an effective immune stimulator in an in vivo murine system. In this study we further evaluated the effects of daidzein and genistein, individually and in combination, on in vitro mitogen-stimulated activation of murine lymphocytes. At physiologically relevant concentrations (0.01-10.0 microM), daidzein significantly potentiated proliferation of mixed splenocyte cultures activated with concanavalin A or lipopolysaccharide in a dose-dependent manner in comparison with vehicle control, whereas genistein had no influence on the response. Although a significant cooperativity with genistein (1 microM) was observed at low concentrations of daidzein (0.01 microM) in comparison with daidzein alone, genistein failed to augment or counteract the effects of high concentrations of daidzein on lymphocyte proliferation. The secretion of cytokine interleukins-2 and -3 from concanavalin A-activated lymphocytes was significantly increased again by daidzein and was unaffected or mildly decreased by genistein. Taken together, these results demonstrate that daidzein, rather than genistein, is able to enhance in vitro activation of murine lymphocytes and suggest that more studies focusing on the immunoregulatory mechanism of soy daidzein and the potential clinical relevance are warranted. PMID:9383781

Wang, W; Higuchi, C M; Zhang, R

1997-01-01

396

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

397

In vitro and in vivo antioxidant properties and DNA damage protective activity of green fruit of Ficus glomerata  

Microsoft Academic Search

This study evaluated the antioxidant properties of Ficus glomerata fruits using in vitro and in vivo assay. In order to find in vitro antioxidant properties, extract\\/fractions from F. glomerata were studied for TPC, AOA, RP, DPPH, O2-, OH scavenging activities and LPO. Among all the extract\\/fractions, FEF has shown potent antioxidant activity and was also found effective in protecting oxidative

Arti R. Verma; M. Vijayakumar; Chandana V. Rao; Chandra S. Mathela

2010-01-01

398

In Vitro Antifungal Activity of Pneumocandin L-743,872 against a Variety of Clinically Important Molds  

Microsoft Academic Search

The in vitro activity of the new antifungal drug pneumocandin L-743,872 against 55 isolates of clinically important molds was examined by an adapted macrobroth dilution method for yeasts. Pneumocandin L- 743,872 exhibited in vitro antifungal activity against Alternaria sp., Aspergillus flavus, Aspergillus fumigatus, Curvularia lunata, Exophiala jeanselmei, Fonsecaea pedrosoi, Paecilomyces variotii, and Scedosporium apiosper- mum. The drug appeared to lack

MAURIZIO DEL POETA; WILEY A. SCHELL; JOHN R. PERFECT

1997-01-01

399

In vitro Short-Time Killing Activity of PovidoneIodine (Isodine® Gargle) in the Presence of Oral Organic Matter  

Microsoft Academic Search

In order to estimate the clinical efficacy of a povidone-iodine oral antiseptic (PVP-I) on oral bacterial infectious diseases, we studied the effect of oral organic matter on the in vitro killing activity of PVP-I. In addition, we compared the in vitro short-time killing activity of PVP-I with those of other oral antiseptics using mouth-washing and gargling samples collected from healthy

Akiko Yoneyama; Masaki Shimizu; Makiko Tabata; Junko Yashiro; Toshihiko Takata; Muneo Hikida

2006-01-01

400

Different oxygenators for cardiopulmonary bypass lead to varying degrees of human complement activation in vitro.  

PubMed

Complement activation was studied in vitro with six different membrane and bubble oxygenators for cardiopulmonary bypass. There was a similar increase in terminal (C5 to C9) activation with all oxygenators (p less than 0.001), ranging from 281% (117% to 444%) to 453% (225% to 680%) after 60 minutes (median and 95% confidence intervals). C3 activation was not observed with a hollow fiber membrane and a soft shell bubble oxygenator. On the other hand, a capillary membrane, a sheet membrane, a nonporous membrane, and a hard shell bubble oxygenator all induced a similar increase in C3 activation (p less than 0.01), ranging from 107% (23% to 346%) to 272% (88% to 395%) after 60 minutes. The differences in C3 activation could not be explained by the blood contact materials or any other single factor known to induce activation, which suggests that overall complement activation during cardiopulmonary bypass is a multifactorial effect. The tubing set per se induced only minor C3 activation but contributed to the overall formation of terminal complement complex. The study further indicates that an arterial line blood filter prevents activated neutrophils from being reinfused to the patient and should be used regardless of type of oxygenator. PMID:2709867

Videm, V; Fosse, E; Mollnes, T E; Ellingsen, O; Pedersen, T; Karlsen, H

1989-05-01

401

In vitro activity of telithromycin against Haemophilus influenzae at epithelial lining fluid concentrations  

PubMed Central

Background Haemophilus influenzae is one of the main aetiological agents of community-acquired respiratory tract infections. The primary aim of this study was to evaluate the antibacterial activity of telithromycin against H. influenzae clinical isolates showing different pattern of resistance in comparison with azithromycin and clarithromycin at 1/4 ×, 1/2 ×, 1 ×, 2 ×, 4 × minimum inhibitory concentration (MIC) and to peak concentrations in epithelial lining fluid (ELF). The secondary aim was to determine the influence of CO2 enriched atmosphere on bacterial susceptibility. Results Telithromycin showed high activity against H. influenzae, including strains susceptible to ?-lactams (n = 200), ?-lactamase producer (n = 50) and ?-lactamase negative ampicillin resistant (BLNAR) (n = 10), with MIC from ?0.03 to 4 mg/L, and MIC50/MIC90 of 1/2 mg/L with susceptibility rate of 100%, and minimum bactericidal concentrations (MBC) from 2 to 4-fold higher than the MIC. Azithromycin was the most active tested macrolide (range: 0.25 – 4 mg/L; MIC50/MIC90: 1/2 mg/L), comparable to telithromycin, while clarithromycin showed the highest MICs and MBCs (range: 0.25 – 8 mg/L; MIC50/MIC90: 2/8 mg/L). In time-kill studies, telithromycin showed a bactericidal activity at the higher concentrations (4 – 2 × MIC and ELF) against all the strains, being complete after 12 – 24 hours from drug exposition. At MIC concentrations, at ambient air, bactericidal activity of telithromycin and azithromycin was quite similar at 12 hours, and better than that of clarithromycin. Besides, telithromycin and clarithromycin at ELF concentrations were bactericidal after 12 hours of incubation for most strains, while 24 hours were needed to azithromycin to be bactericidal. Incubation in CO2 significantly influenced the MICs and MBCs, and only slightly the in vitro killing curves. Conclusion Telithromycin showed an in-vitro potency against H. influenzae comparable to azithromycin, with an in-vitro killing rate more rapid and superior to clarithromycin at 2X-MIC against ?-lactamase producers and BLNAR strains, and to azithromycin at ELF concentrations against ?-lactamase negative strains. Against all strains, MICs and MBCs were lower in the absence of CO2 for the tested antibiotics, showing an adverse effect of incubation in a CO2 environment. The in-vitro potency together with the tissue concentrations of the antimicrobial, should be considered in predicting efficacy.

De Vecchi, Elena; Nicola, Lucia; Larosa, Monica; Drago, Lorenzo

2008-01-01

402

Activation of hepatocyte growth factor (HGF) by endogenous HGF activator is required for metanephric kidney morphogenesis in vitro.  

PubMed

The interaction of hepatocyte growth factor (HGF) with c-Met has been implicated in morphogenesis of the kidney, lung, mammary gland, liver, placenta, and limb bud. HGF is secreted as an inactive zymogen and must be cleaved by a serine protease to initiate Met signaling. We show here that a serine protease specific for HGF, HGF activator (HGFA), is expressed and activated by the ureteric bud of the developing kidney in vivo and in vitro. Inhibition of HGFA activity with serine protease inhibitors reduced ureteric bud branching and inhibited glomerulogenesis and nephrogenesis. Activated HGF rescued developing kidneys from the effects of inhibitors. HGFA was localized around the tips of the ureteric bud in developing kidneys, while HGF was expressed diffusely throughout the mesenchyme. These data show that expression of HGF is not sufficient for development, but that its activation is also required. The localization of HGFA to the ureteric bud and the mesenchyme immediately adjacent to it suggests that HGFA creates a gradient of HGF activity in the developing kidney. The creation and shape of gradients of activated HGF by the localized secretion of HGF activators could play an important role in pattern formation by HGF responsive tissues. PMID:11032833

van Adelsberg, J; Sehgal, S; Kukes, A; Brady, C; Barasch, J; Yang, J; Huan, Y

2000-10-13

403

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

PubMed

Obesity has become a worldwide health problem. Orlistat, an inhibitor of pancreatic lipase, is currently approved as an anti-obesity drug. However, gastrointestinal side effects caused by Orlistat may limit its use. In this study the inhibitory activities of dandelion (Taraxacum officinale) against pancreatic lipase in vitro and in vivo were measured to determine its possible use as a natural anti-obesity agent. The inhibitory activities of the 95% ethanol extract of T. officinale and Orlistat were measured using 4-methylumbelliferyl oleate (4-MU oleate) as a substrate at concentrations of 250, 125, 100, 25, 12.5 and 4 microg/ml. To determine pancreatic lipase inhibitory activity in vivo, mice (n=16) were orally administered with corn oil emulsion (5 ml/kg) alone or with the 95% ethanol extract of T. officinale (400 mg/kg) following an overnight fast. Plasma triglyceride levels were measured at 0, 90, 180, and 240 min after treatment and incremental areas under the response curves (AUC) were calculated. The 95% ethanol extract of T. officinale and Orlistat, inhibited, porcine pancreatic lipase activity by 86.3% and 95.7% at a concentration of 250 microg/ml, respectively. T. officinale extract showed dose-dependent inhibition with the IC(50) of 78.2 microg/ml. A single oral dose of the extract significantly inhibited increases in plasma triglyceride levels at 90 and 180 min and reduced AUC of plasma triglyceride response curve (p<0.05). The results indicate that T. officinale exhibits inhibitory activities against pancreatic lipase in vitro and in vivo. Further studies to elucidate anti-obesity effects of chronic consumption of T. officinale and to identify the active components responsible for inhibitory activity against pancreatic lipase are necessary. PMID:20016719

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

2008-12-31

404

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

PubMed Central

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

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

2008-01-01

405

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

PubMed

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

Büyükbalci, Aynur; El, Sedef Nehir

2008-01-09

406

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

PubMed

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

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

2013-08-12

407

Anaphylactic release of a prekallikrein activator from human lung in vitro.  

PubMed Central

We have demonstrated the in vitro IgE-mediated release of a prekallikrein activator from human lung. The lung prekallikrein activator was partially purified by sequential chromatography on sulfopropyl-Sephadex, DEAE-Sephacel, and Sepharose 6B. Purified human prekallikrein was converted to its active form (kallikrein) by the lung protease. The generated kallikrein was shown to be biologically active; that is, it generates bradykinin from purified human high-molecular weight kininogen and also cleaves benzoyl-propyl-phenyl-arginyl-p-nitroanilide, a known synthetic substrate of kallikrein. The lung prekallikrein activator differs from the known physiologic activators of prekallikrein (the activated forms of Hageman factor) with respect to: (a) size (it has a mol wt of approximately 175,000); (b) synthetic substrate specificity (D-propyl/phenyl/arginyl-p-nitroanilide is a substrate for the activated forms of Hageman factor, but not the lung protease); (c) antigenic specificity (an anti-Hageman factor immunoadsorbent column did not remove significant amounts of the lung protease, while it removed most of the activity of activated Hageman factor fragments); and (d) inhibition profile (the lung proteases was not inhibited by corn trypsin inhibitor). This prekallikrein activator provides a physiologic mechanism by which prekallikrein can be directly activated during IgE-mediated reactions of the lung. While the role of this lung prekallikrein activator in immediate hypersensitivity reactions and in other inflammatory processes is not clear, it does represent a first and important interface between IgE-mediated reactions and the Hageman factor-dependent pathways of the inflammatory response. Images FIGURE 6

Meier, H L; Kaplan, A P; Lichtenstein, L M; Revak, S; Cochrane, C G; Newball, H H

1983-01-01

408

In vitro assay of thyroid disruptors affecting TSH-stimulated adenylate cyclase activity.  

PubMed

Several natural or synthetic chemicals have been indicated as potential thyroid disruptors. The development of in vitro assays has been recommended to comprehensively assess the potential thyroid disrupting activity of a substance or a complex mixture. In this study, 12 substances suspected for acting as thyroid disruptors were tested for their ability to inhibit TSH-stimulated cAMP production in vitro. Those substances producing an inhibition were further studied to establish the level at which they interfere with this step of thyroid cell function. Using Chinese hamster ovary cells (CHO) transfected with the recombinant human TSH receptor, a dose-dependent inhibition of TSH-stimulated adenylate cyclase activity was produced by 1,1-bis-(4-chlorphenyl)-2,2,2-trichloroethan (DDT), Aroclor 1254 and Melissa Officinalis. All three substances also inhibited the cAMP production stimulated by TSH receptor antibody. Melissa Officinalis produced a significant inhibition of TSH binding to its receptor and of antibody binding to TSH, while no significant changes were produced by Aroclor 1254 or DDT in these assays. These data suggest that principles contained in Melissa Officinalis may block the binding of TSH to its receptor by acting both on the hormone and the receptor itself, while DDT and Aroclor 1254 affect cAMP production mainly at post-receptor step. In conclusion, we have developed a set of in vitro assays that allow investigation into the effect of thyroid disruptors on the TSH-mediated activation of the cAMP cascade. These assays may be useful to identify the mechanism of action of thyroid disruptors, coming beside and supporting animal studies or epidemiological surveys. PMID:14759065

Santini, F; Vitti, P; Ceccarini, G; Mammoli, C; Rosellini, V; Pelosini, C; Marsili, A; Tonacchera, M; Agretti, P; Santoni, T; Chiovato, L; Pinchera, A

2003-10-01

409

In vitro antifungal and antibacterial activities of pentacycloundecane tetra-amines.  

PubMed

The antifungal and antimicrobial activities of three pentacycloundecane (PCU) tetra-amine derivatives are reported herein. The in vitro activity of these PCU derivatives against yeasts (Candida albicans and non-albicans species) and filamentous fungi was evaluated using the Clinical and Laboratory Standards Institute (CLSI) M27-A2 and M38-A2 guidelines and the 2H-tetrazolium salt, (MTS) colorimetric method. The minimum inhibitory concentration against most of the tested clinical fungal strains for GKM8 and GKM9 derivatives ranges from 15.6 to 62.5 ?g/mL while GKM11 ranged from 3.9 to 7.8 ?g/mL. The GKM11 derivative was also active against fluconazole-resistant strains of fungi. The GKM11 derivative also exhibited promising activity against filamentous fungi in that it was 2.5 times more active than amphotericin B against Sporothrix schenckii. Antibacterial activity was determined using the broth microdilution method (BMM) and the iodonitrotetrazolium chloride (INT) colorimetric method. The GKM11 derivative was mainly active against Gram-positive bacteria with MIC ranging from 3.9 to 7.8 ?g/mL. Activity against Gram-negative bacteria tested was limited to Escherichia coli and Elizabethkingia meningoseptica (MIC of 31 ?g/mL). PMID:21241455

Onajole, Oluseye K; Coovadia, Yacoob; Govender, Thavendran; Kruger, Hendrik G; Maguire, Glenn E M; Naidu, Dianithi; Singh, Nisha; Govender, Patrick

2011-02-22

410

DNA superhelicity enhances the assembly of transcriptionally active chromatin in vitro.  

PubMed

Using an in vitro chromatin assembly system, we analyzed the influence of DNA superhelicity on the development of transcriptionally active minichromosomes. Plasmid DNA molecules containing either a Xenopus borealis 5S RNA gene or an X. laevis methionine tRNA gene were utilized as templates for the assembly of chromatin. Both plasmids were processed into active minichromosomes if introduced as supercoiled molecules into the extract (S-150). The degree of superhelicity is a determining factor in the assembly of active chromatin. Molecules containing varying superhelical densities were processed into minichromosomes with different transcriptional activities. The absence of supercoils leads to the assembly of chromatin with substantially lower transcriptional activity. Assembled minichromosomes are stable enough to be isolated by sucrose gradient centrifugation while retaining their transcriptional phenotype. The formation of nucleosomes with a periodic spacing occurred with the same efficiency and to the same degree regardless of the initial DNA topology. Hence, a determining factor in the development of transcriptionally active chromatin may be the initial superhelicity of the DNA molecule to which activator (trans-acting factors) or repressor (histones) proteins bind. Once the chromatin assembly process has begun, the transcriptional activity of the resulting minichromosome may already have been determined. PMID:2558288

Sekiguchi, J M; Kmiec, E B

1989-12-01

411

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

412

The stimulatory activities of polysaccharide compounds derived from algae extracts on insulin secretion in vitro.  

PubMed

We prepared two series of polysaccharide compounds derived from algae extracts and investigated their stimulatory activity on insulin secretion in vitro using the rat pancreatic cell line, RIN-5F. Several of the compounds exhibited significant stimulatory activity in a dose-dependent manner without apparent cytotoxicity at concentrations above 10 microM. Glybenclamide, a commonly prescribed sulfonylurea (SU) against diabetes mellitus type II, was used as a positive control and showed moderate cytotoxicity in the cell culture assay system. Amylin (IAPP; islet amyloid polypeptide), an inhibitor for glybenclamide, did not inhibit the activity of the isolated compounds, suggesting that they act through a mechanism(s) different from glybenclamide. Algae-derived extracts could be candidates for a new class of anti-diabetic drugs. PMID:18451519

Zhang, Dandan; Fujii, Isao; Lin, Changzheng; Ito, Kaori; Guan, Huashi; Zhao, Ji'en; Shinohara, Makoto; Matsukura, Makoto

2008-05-01

413

Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique.  

PubMed Central

A rapid, semiautomated microdilution method was developed for measuring the activity of potential antimalarial drugs against cultured intraerythrocytic asexual forms of the human malaria parasite Plasmodium falciparum. Microtitration plates were used to prepare serial dilutions of the compounds to be tested. Parasites, obtained from continuous stock cultures, were subcultured in these plates for 42 h. Inhibition of uptake of a radiolabeled nucleic acid precursor by the parasites served as the indicator of antimalarial activity. Results of repeated measurements of activity with chloroquine, quinine, and the investigational new drug mefloquine demonstrated that the method is sensitive and precise. Several additional antimalarial drugs and compounds of interest were tested in vitro, and the results were consistent with available in vivo data. The use of P. falciparum isolates with known susceptibility to antimalarial drugs also permitted evaluation of the cross-resistance potential of each compound tested. The applications and expectations of this new test system within a drug development program are discussed.

Desjardins, R E; Canfield, C J; Haynes, J D; Chulay, J D

1979-01-01

414

The ribonucleolytic activity of the ribotoxin ?-sarcin is not essential for in vitro protein biosynthesis inhibition.  

PubMed

Fungal ribotoxins are toxic secreted ribonucleases that cleave a conserved single phosphodiester bond located at the sarcin/ricin loop of the larger rRNA. This cleavage inactivates ribosomes leading to protein biosynthesis inhibition and cell death. It has been proposed that interactions other than those found at the active site of ribotoxins are needed to explain their exquisite specific activity. The study presented shows the ability of a catalytically inactive ?-sarcin mutant (H137Q) to bind eukaryotic ribosomes and interfere with in vitro protein biosynthesis. The results obtained are compatible with previous observations that ?-sarcin can promote cell death by a mechanism that is independent of rRNA cleavage, expanding the potential set of activities performed by this family of toxins. PMID:21767671

Alvarez-García, Elisa; Diago-Navarro, Elizabeth; Herrero-Galán, Elías; García-Ortega, Lucía; López-Villarejo, Juan; Olmo, Nieves; Díaz-Orejas, Ramón; Gavilanes, José G; Martínez-del-Pozo, Alvaro

2011-07-13

415

In vitro antiplasmodial, antiamoebic, and cytotoxic activities of a series of bisbenzylisoquinoline alkaloids.  

PubMed Central

Twenty-four bisbenzylisoquinoline alkaloids were screened for antiplasmoidal, antiamoebic, and cytotoxic activities by use of in vitro microtests. Eight of the alkaloids had antiplasmodial activity, with a 50% inhibitory concentration (IC50) of less than 1 microM against a multidrug-resistant strain of Plasmodium falciparum (chloroquine had an IC50 of 0.2 microM). The three alkaloids most active against Entamoeba histolytica, aromoline, isotrilobine, and insularine, had IC50s of 5 to 11.1 microM (metronidazole had an IC50 of 1.87 microM). None of the 24 bisbenzylisoquinoline alkaloids exhibited significant cytotoxicity against the KB cell line, the most toxic being berbamine, with an IC50 of 17.8 microM (the IC50 of podophyllotoxin was 0.008 microM). Bisbenzylisoquinoline alkaloids merit further investigation as potential novel antimalarial agents.

Marshall, S J; Russell, P F; Wright, C W; Anderson, M M; Phillipson, J D; Kirby, G C; Warhurst, D C; Schiff, P L

1994-01-01

416

In vitro activities of 47 antimicrobial agents against three Campylobacter spp. from pigs.  

PubMed Central

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.

Gebhart, C J; Ward, G E; Kurtz, H J

1985-01-01

417

In vitro activity of tigecycline and 10 other antimicrobials against clinical isolates of the genus Corynebacterium.  

PubMed

We studied the in vitro activity of tigecycline and 10 other commonly used antibiotics against 135 clinical isolates of non-diphtheria Corynebacterium spp. using the Etest system. Tigecycline minimum inhibitory concentrations for 50% and 90% of the organisms (MIC(50) and MIC(90) values, respectively, in mg/L) were: Corynebacterium urealyticum, 0.094 and 0.125; Corynebacterium amycolatum, 0.125 and 2; Corynebacterium jeikeium, 0.094 and 0.75; Corynebacterium coyleae, 0.064 and 0.064; Corynebacterium striatum, 0.064 and 1; Corynebacterium aurimucosum, 0.094 and 0.125; and Corynebacterium afermentans, 0.064 and 0.094. The activities of all other antimicrobials were variable, with good activity of glycopeptides, linezolid, quinupristin/dalfopristin and daptomycin and with resistance to macrolides in a high number of isolates. Tigecycline is a good alternative for the therapy of infections caused by non-diphtheria corynebacteria. PMID:19153032

Fernandez-Roblas, R; Adames, H; Martín-de-Hijas, N Z; Almeida, D García; Gadea, I; Esteban, J

2009-01-18

418

In vitro antifungal activity of dihydroxyacetone against causative agents of dermatomycosis.  

PubMed

Dihydroxyacetone (DHA), a three-carbon sugar, is the browning ingredient in commercial sunless tanning formulations. DHA preparations have been used for more than 50 years and are currently highly popular for producing temporary pigmentation resembling an ultraviolet-induced tan. In this work, the in vitro antifungal activity of dihydroxyacetone was tested against causative agents of dermatomycosis, more specifically against dermatophytes and Candida spp. The antifungal activity was determined by the broth microdilution method according to the Clinical and Laboratory Standards Institute guidelines for yeasts and filamentous fungi. The data obtained show that the fungicidal activity varied from 1.6 to 50 mg ml(-1). DHA seems to be a promising substance for the treatment of dermatomycosis because it has antifungal properties at the same concentration used in artificial suntan lotions. Therefore, it is a potential low-toxicity antifungal agent that may be used topically because of its penetration into the corneal layers of the skin. PMID:20936361

Stopiglia, Cheila Denise Ottonelli; Vieira, Fabiane Jamono; Mondadori, Andressa Grazziotin; Oppe, Tércio Paschke; Scroferneker, Maria Lúcia

2010-10-09

419

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

420

Synthesis, in vitro evaluation, and antileishmanial activity of water-soluble prodrugs of buparvaquone.  

PubMed

Water-soluble phosphate prodrugs of buparvaquone (1), containing a hydroxynaphthoquinone structure, were synthesized and evaluated in vitro for improved topical and oral drug delivery against cutaneous and visceral leishmaniasis. The successful prodrug synthesis involved a strong base; e.g., sodium hydride. Buparvaquone-3-phosphate (4a) and 3-phosphonooxymethyl-buparvaquone (4b) prodrugs possessed significantly higher aqueous solubilities (>3.5 mg/mL) than the parent drug (vitro and thus are promising bioreversible prodrugs for the improved topical and oral bioavailability of 1. Buparvaquone and its prodrugs showed nanomolar or low-micromolar ED(50) activity values against species that cause cutaneous leishmaniasis, e.g., L. major, L. amazonensis, L. aethiopica, L. mexicana, and L. panamensis and also L. donovani, which is the causative agent of visceral leishmaniasis. From these results, the human skin permeation of the prodrugs 4a and 4b were studied in vitro. While no buparvaquone permeated across post mortem skin in vitro during 72 h of experiments, both prodrugs 4a and 4b permeated readily through the skin. In addition, 4b easily released the parent drug in human skin homogenate and, therefore, is a promising prodrug candidate to deliver buparvaquone through the skin for the treatment of cutaneous leishmaniasis. PMID:14695832

Mäntylä, Antti; Garnier, Tracy; Rautio, Jarkko; Nevalainen, Tapio; Vepsälainen, Jouko; Koskinen, Ari; Croft, Simon L; Järvinen, Tomi

2004-01-01

421

In vitro activities of the new antifungal triazole SCH 56592 against common and emerging yeast pathogens.  

PubMed

A broth microdilution method performed in accordance with the National Committee for Clinical Laboratory Standards guidelines was used to compare the in vitro activity of the new antifungal triazole SCH 56592 (SCH) to that of fluconazole (FLC), itraconazole (ITC), and ketoconazole (KETO) against 257 clinical yeast isolates. They included 220 isolates belonging to 12 different species of Candida, 15 isolates each of Cryptococcus neoformans and Saccharomyces cerevisiae, and seven isolates of Rhodotorula rubra. The MICs of SCH at which 50% (MIC(50)) and 90% (MIC(90)) of the isolates were inhibited were 0.06 and 2.0 microg/ml, respectively. In general, SCH was considerably more active than FLC (MIC(50) and MIC(90) of 1.0 and 64 microg/ml, respectively) and slightly more active than either ITC (MIC(50) and MIC(90) of 0.25 and 2.0 microg/ml, respectively) and KETO (MIC(50) and MIC(90) of 0.125 and 4.0 microg/ml, respectively). Our in vitro data suggest that SCH has significant potential for clinical development. PMID:10602757

Barchiesi, F; Arzeni, D; Fothergill, A W; Di Francesco, L F; Caselli, F; Rinaldi, M G; Scalise, G

2000-01-01

422

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

PubMed Central

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

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

2013-01-01

423

In Vitro Shear Stress-Induced Platelet Activation: Sensitivity of Human and Bovine Blood.  

PubMed

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

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

2013-06-01

424

[Detection of Cre recombinase activity in Mx-Cre transgenic mice induced by INF in vitro].  

PubMed

The Cre recombinase and its activity in C57-TgN(Mx-Cre) transgenic mice is studied by polymerase chain reaction (PCR), Western blot, immunohistochemistry, immunogold electron microscopy and Southern blot. C57-TgN(Mx-Cre) transgenic mice harbouring cre gene in genomic DNA is demonstrated by PCR, and these mice which are induced by INF-alpha 1b could express Cre recombinase, which is confirmed by Western blot. With immunohistochemistry, we find that the Cre recombinase expresses in hepatocyte cytoplasm and nuclear of C57-TgN(Mx-Cre) transgenic mice. Cre recombinase expressed in hepatocyte cytoplasm and nuclear is further confirmed by immunogold electon microscopy. And it is supported that the Cre recombinase which is created from C57-TgN(Mx-Cre) transgenic mice induced by INF-alpha 1b can direct DNA recombination reaction in vitro. All evidence leads us supporting the view that the Cre recombinase expressed in C57-TgN(Mx-Cre) transgenic mice has activity. Thus we find a method to detect the activity of Cre recombinase in vitro. PMID:11582740

Zi, X Y; Yao, Y C; Xiong, J; Li, J X; Yan, Y B; Yu, H Y; Hu, Y P

2001-01-01