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T. A. Bailey R. S. Sheen C. Silvanose J. H. Samour A. Garner D. W. G. Harron 《Journal of veterinary pharmacology and therapeutics》1998,21(4):288-297
The in-vitro activity of enrofloxacin against 117 strains of bacteria isolated from bustards was determined. Minimum inhibitory concentrations for 72% of the Proteus spp., E. coli, Salmonella spp. and Klebsiella spp. (n = 61) and for 48% of the Streptococci spp. and Staphylococci spp. (n = 31) were 0.5 μ g/mL. The minimum inhibitory concentration (MIC) of 76% of Pseudomonas spp. (n = 25) was 2 μg/mL. Fourteen strains were resistant to concentrations 128 μg/mL. The elimination half-lives (t½ elim β) (mean± SEM) of 10 mg/kg enrofloxacin in eight houbara bustards (Chlamydotis undulata) were 6.80± 0.79, 6.39± 1.49 and 5.63± 0.54 h after oral (p.o.), intramuscular (i.m.) and intravenous (i.v.) administration, respectively. Enrofloxacin was rapidly absorbed from the bustard gastro-intestinal tract and maximum plasma concentrations of 1.84± 0.16 μg/mL were achieved after 0.66± 0.05 h. Maximum plasma concentration after i.m. administration of 10 mg/kg was 2.75± 0.11 μg/mL at 1.72± 0.19 h. Maximum plasma concentration after i.m. administration of 15 mg/kg in two birds was 4.86 μg/mL. Bioavailability was 97.3± 13.7% and 62.7± 11.1% after i.m. and oral administration, respectively. Plasma concentrations of enrofloxacin 0.5 μg/mL were maintained for at least 12 h for all routes at 10 mg/kg and for 24 h after i.m. administration at 15 mg/kg. Plasma enrofloxacin concentrations were monitored during the first 3 days of treatment in five houbara bustards and kori bustards (Ardeotis kori) with bacterial infections receiving a single daily i.m. injection of 10 mg/kg for 3 days. The mean plasma enrofloxacin concentrations in the clinical cases at 27 and 51 h (3.69 and 3.86 μg/mL) and at 48 h (0.70 μg/mL) were significantly higher compared with the 3 h and 24 h time intervals from clinically normal birds. The maximum plasma concentration (Cmax)/MIC ratio was ranked i.v. (10/mg/kg) > i.m. (15 mg/kg) > i.m. (10 mg/kg) > oral (10 mg/kg), but it was only higher than 8:1 for i.v and i.m. administrations of enrofloxacin at 10 mg/kg and 15 mg/kg, respectively, against a low MIC (0.5 μg/mL). A dosage regimen of 10 mg/kg repeated every 12 h, or 15 mg/kg repeated every 24 h, would be expected to give blood concentrations above 0.5 μg/mL and hence provide therapeutic response in the bustard against a wide range of bacterial infections. 相似文献
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Tsai CW Chen HW Yang JJ Sheen LY Lii CK 《Journal of agricultural and food chemistry》2007,55(3):1019-1026
Garlic organosulfur compounds are recognized as potential chemopreventive compounds. This protection is related to the induction of phase II detoxification enzymes. We previously reported that diallyl disulfide (DADS) and diallyl trisulfide (DATS) up-regulate the gene expression of the pi class of glutathione S-transferase (GSTP) and that an enhancer element named GPE I is required for this induction. In the present study, we further investigated the signal pathway involved in DADS and DATS up-regulation of this detoxification enzyme in Clone 9 cells. Cells were cultured with 25-200 micromol/L of DADS or DATS for 24 h. Western and Northern blots showed that both garlic allyl sulfides concentration dependently induced GSTP protein and mRNA expression, respectively. Changes in GST activity toward ethacrynic acid were consistent with the increase in GSTP expression (P < 0.05). Electromobility gel shift assay showed that the DNA binding activity of nuclear activator protein-1 (AP-1) is concentration-dependently increased in the presence of DADS and DATS as compared with that of the control cells. The phosphorylation of c-Jun NH2-terminal kinase (JNK) and extracellular signal-regulated kinase (ERK), but not of p38, was stimulated in the presence of both garlic allyl sulfides. Pretreatment with SP600125 and PD98059, which are JNK and ERK inhibitors, respectively, abolished the increase in AP-1-DNA binding activity and also the induction of GSTP protein by either allyl sulfide. Our results indicate that the effectiveness of DADS and DATS on GSTP expression is likely related to the JNK-AP-1 and ERK-AP-1 signaling pathways and, thus, that DADS and DATS enhance the binding of AP-1 to GPE I. 相似文献
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Liu KL Chen HW Wang RY Lei YP Sheen LY Lii CK 《Journal of agricultural and food chemistry》2006,54(9):3472-3478
Diallyl trisulfide (DATS), diallyl sulfide (DAS), and diallyl disulfide (DADS) are the three major organosulfur compounds (OSCs) in garlic oil. In contrast to DADS and DATS, evidence of an anti-inflammatory effect of DATS is limited. In this study compares the efficacy of DATS with those of DAS and DADS on lipopolysaccharide (LPS)-induced inducible nitric oxide synthase (iNOS) expression and nitric oxide (NO) production in RAW 264.7 macrophages. The NO production in LPS-activated RAW 264.7 macrophages was suppressed by both DADS and DATS in a dose-dependent manner. At 100 muM, the nitrite levels of DADS- and DATS-treated cells were 57 and 34%, respectively, of cells treated with LPS alone. DAS, however, had no influence on NO production even at a concentration of 1 mM. Western blot and Northern blot assays showed that DADS and DATS but not DAS dose-dependently suppressed LPS-induced iNOS protein and mRNA expression in a pattern similar to that noted for NO production. LPS-induced cellular peroxide production was significantly inhibited by DADS and DATS (P < 0.05) but not by DAS. Electrophoresis mobility shift assays further indicated that DADS and DATS effectively inhibited the activation of NF-kappaB induced by LPS. Taken together, these results indicate that the differential efficacy of three major OSCs of garlic oil on suppression of iNOS expression and NO production is related to the number of sulfur atoms and is in the order DATS > DADS > DAS. The inhibitory effect of DATS on LPS-induced iNOS expression is likely attributed to its antioxidant potential to inhibit NF-kappaB activation. 相似文献
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Su ZY Hwang LS Kuo YH Shu CH Sheen LY 《Journal of agricultural and food chemistry》2008,56(20):9447-9454
The antihepatoma activity and related active components in the fermentation products of Agaricus blazei (AB) cultured in the medium containing soybean (S) or black soybean (BS) were investigated. AB(BS)-pE and AB(S)-pE were the ethanolic extracts from the fermentation products of AB(BS) and AB(S), respectively. According to the IC 50 values, AB(BS)-pE (161.1 and 24.0 microg/mL for Hep 3B and Hep G2 cells, respectively) exhibited stronger cytotoxicities against hepatoma cells than AB(S)-pE (>200 and 99.9 microg/mL for Hep 3B and Hep G2 cells, respectively). AB(BS)-pE was separated by silica gel column chromatography and eluted with n-hexane/ethyl acetate/methanol gradient solvent system into 21 fractions. Fraction 3 [AB(BS)-pE-F3], eluted with n-hexane/ethyl acetate (97:3 and 19:1, v/v), was the most active fraction having inhibitory activity on the proliferation of Hep 3B and Hep G2 cells (IC 50 of 3.6 and 1.9 microg/mL, respectively). Three major compounds, compounds 1- 3, were further isolated from the AB(BS)-pE-F3 fraction by reversed-phase semipreparative high-performance liquid chromatography. Compounds 2 and 3 gave better antihepatoma activity than that of compound 1. The IC 50 values of compounds 2 and 3 were 2.8 and 4.5 microg/mL for Hep 3B cells and 1.4 and 2.0 microg/mL for Hep G2 cells, respectively. The structures of compounds 2 and 3 were identified by UV, IR, electron impact mass spectrometry, and (1)H and (13)C NMR to be blazeispirols A and C, respectively. Blazeispirols A and C existed in the mycelia but not in the broth and were more in AB(BS)-pE (49.9 +/- 8.9 and 14.2 +/- 2.4 mg/g, respectively) than AB(S)-pE (15.9 +/- 1.7 and 3.9 +/- 0.6 mg/g, respectively). Additionally, the result shows that the production of blazeispirols A and C was increased after cultivation in the medium containing black soybean on day 6 and reached the maximum on day 12, and the contents of blazeispirols A and C were negatively correlated with Hep 3B and Hep G2 cell viabilities ( r = -0.84 to -0.93, P < 0.01). It suggests that blazeispirols A and C could be used as biomarkers to produce the fermentation product of A. blazei with antihepatoma activity. 相似文献
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5,7,3',4'-Tetramethoxyflavone (TMF), one of the major polymethoxyflavones (PMFs) isolated from Kaempferia parviflor , has been reported possessing various bioactivities, including antifungal, antimalarial, antimycobacterial, and anti-inflammatory activities. Although several studies on the TMF have been reported, the information about the metabolism of TMF and the structures of TMF metabolites is still not yet clear. In this study, an isotope-labeling method was developed for the identification of TMF metabolites. Three isotope-labeled TMFs (5,7,3',4'-tetramethoxy[3'-D(3)]flavone, 5,7,3',4'-tetramethoxy[4'-D(3)]flavone, and 5,7,3',4'-tetramethoxy[5,4'-D(6)]flavone) were synthesized and administered to rats. The urine samples were collected, and the main metabolites were monitored by ultrahigh-performance liquid chromatography-electrospray ionization-mass spectrometry. Five TMF metabolites were unambiguously identified as 3'-hydroxy-5,7,4'-trimethoxyflavone, 7-hydroxy-5,3',4'-trimethoxyflavone sulfate, 7-hydroxy-5,3',4'-trimethoxyflavone, 4'-hydroxy-5,7,3'-trimethoxyflavone, and 5-hydroxy-7,3',4'-trimethoxyflavone. 相似文献
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K. Joseph John Sheen Scariah V. A. Muhammed Nissar M. Latha S. Gopalakrishnan S. R. Yadav K. V. Bhat 《Genetic Resources and Crop Evolution》2013,60(3):1037-1046
Recent research point to the Indian wild taxa of Cucumis callosus (Rottler) Cogn. as the wild progenitor of melon (C. melo L.). Overlapping distribution with cultivated and weedy and feral forms of melo and normal fertility of F1 and BC1 generations of its cross with cultivated melon indicate its progenitor status. A perusal of herbarium data indicate its natural distribution pattern in the region comprising Vindhya Hills and Aravalli mountain ranges extending northwards to Indo-Gangetic plains and southwards to the Deccan plateau touching rain shadow areas of Western Ghats. Characterised by drought tolerance and field resistance to a host of pests and diseases, it is conspicuously absent in the high rainfall areas of Western Ghats and upper Himalayan region. Based on its morphological distinction and F1 and BC1 fertility with C. melo, a subspecific rank within C. melo is postulated. First-hand information on its occurrence, distribution and crossability relationship with other Indian taxa of Cucumis are given. 相似文献
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K. Joseph John R. Khedasana V. A. Muhammed Nissar Sheen Scariah Shrikant Sutar S. R. Rao M. Abdul Nizar M. Latha S. R. Yadav K. V. Bhat 《Genetic Resources and Crop Evolution》2014,61(2):345-355
Cucumis setosus Cogn. is a rare, endemic, wild gathered or semi-domesticated vegetable restricted to Maharashtra state and border districts of adjoining states in India. Herbarium and literature survey shows that it is poorly collected and inadequately studied. Morphological characters, basic chromosome number and crossability barriers indicate that Cucumis setosus is a valid species, distinct from C. sativus and endemic to western India. Its morphology, basic cytology, crossability relationship with other Cucumis species, taxonomy, distribution, ecology, conservation, economic importance and viability under cultivation are discussed. Besides, a key to distinguish it from C. sativus var. hardwickii (wild and feral form of C. sativus) and other species having sympatric distribution in the area is also presented. Absence of bitter principle in the fruits makes it a potential germplasm for melon and cucumber improvement as well as direct domestication as a future crop. 相似文献
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