ABSTRACT
In the present study, four new sesquiterpenoids, chimonols A-D (compounds 1-4), together with four known compounds (5-8) were isolated from the EtOAc extract of Chimonanthus praecox Link. The structures of these new compounds were elucidated on the basis of spectroscopic techniques (UV, IR, MS, and 1D and 2D NMR), and their absolute configurations were established by comparing experimental and calculated electronic circular dichroism (ECD) spectra. Compounds 1-8 were evaluated for antimicrobial activities and the minimum inhibitory concentrations (MICs) were determined by the broth microdilution method in 96-well culture plates. Compounds 1, 2, and 7 exhibited weak antibacterial effects for S. aureus (ATCC 6538), E. coli (ATCC 11775), and P. aeruginosa (ATCC 10145) with MIC values being 158-249 µg·mL. Compounds 3-7 showed activities against C. glabrata (ATCC 2001) and S. aureus (ATCC 43300) with MIC values being 128-197 µg·mL. Compounds 1-4 showed activity against S. aureus (ATCC 25923) with MIC values being 162-254 µg·mL. The present study provided a basis for future evaluation of these compounds as antibacterial agents.
Subject(s)
Anti-Bacterial Agents , Chemistry , Pharmacology , Calycanthaceae , Chemistry , Escherichia coli , Microbial Sensitivity Tests , Molecular Structure , Plant Extracts , Chemistry , Pharmacology , Sesquiterpenes , Chemistry , Pharmacology , Staphylococcus aureusABSTRACT
In the present study, four new sesquiterpenoids, chimonols A-D (compounds 1-4), together with four known compounds (5-8) were isolated from the EtOAc extract of Chimonanthus praecox Link. The structures of these new compounds were elucidated on the basis of spectroscopic techniques (UV, IR, MS, and 1D and 2D NMR), and their absolute configurations were established by comparing experimental and calculated electronic circular dichroism (ECD) spectra. Compounds 1-8 were evaluated for antimicrobial activities and the minimum inhibitory concentrations (MICs) were determined by the broth microdilution method in 96-well culture plates. Compounds 1, 2, and 7 exhibited weak antibacterial effects for S. aureus (ATCC 6538), E. coli (ATCC 11775), and P. aeruginosa (ATCC 10145) with MIC values being 158-249 µg·mL. Compounds 3-7 showed activities against C. glabrata (ATCC 2001) and S. aureus (ATCC 43300) with MIC values being 128-197 µg·mL. Compounds 1-4 showed activity against S. aureus (ATCC 25923) with MIC values being 162-254 µg·mL. The present study provided a basis for future evaluation of these compounds as antibacterial agents.
Subject(s)
Anti-Bacterial Agents , Chemistry , Pharmacology , Calycanthaceae , Chemistry , Escherichia coli , Microbial Sensitivity Tests , Molecular Structure , Plant Extracts , Chemistry , Pharmacology , Sesquiterpenes , Chemistry , Pharmacology , Staphylococcus aureusABSTRACT
Derris eriocarpa, a traditional Chinese medicine belonging to the family of Leguminosae, is widely distributed mainly over Yunnan, Guangxi and Guizhou of China. Modern pharmacological researches on this herb showed that it had extensive bioactivities, such as promoting urination, removing dampness and cough and reducing inspissated mucus and other biological activities. The extensive studies on the chemical constituents of this plant have resulted in the isolation of triterpenoids, steroids, fatty acid and others, but the flavone compounds haven't reported before. In our further research on the ethyl acetate of this plant, nine flavone compounds were obtained by column chromatography on silica gel, Sephadex LH-20, semi-prep HPLC, polyamide column chromatography and recrystallization for separation and purification. The structures were determined on the basis of extensive spectroscopic analysis, including MS, NMR experiments and comparison with spectroscopic data in the literature, respectively, as diosmetin (1), 3, 3'-di-O-methylquercetin (2), afromosin (3), 6, 3'-dihydroxy-7, 4'-dimethoxyisoflavone (4), odoratin (5), 7, 3'-dihydroxy-8, 4'-dimethoxyisoflavone (6), 6, 4'-dihydroxy-7, 3'-dimethoxyisoflavone (7), 5, 7, 4'-trihydroxy-3, 3', 5'-trimethoxyflavone (8), and alpinumisoflavone (9). All these compounds were isolated from Derris eriocarpa How for the first time. And the in vitro assays showed that compound 2 possessed moderate inhibitory activity against human cancer cells K562 and HEL.
Subject(s)
Humans , Derris , Chemistry , Flavonoids , Chemistry , Pharmacology , K562 CellsABSTRACT
This study was aimed to investigate the estrogenic effects ofCoicis Semen in order to preliminarily discuss the mechanism. Mouse uterine weight test and MCF-7 cell proliferation assay were used to evaluate the estrogenic effects ofC. Semen. Reporter gene assays were adopted to explore the action mechanism ofC. Semen. In reporter gene assay, HEK293 cells were co-transfected with pERE-TAL-luc, pβgal-Control, pCXN2-hERα, or pCXN2-hERβ. And the expression of reporter gene luc was controlled by ERE. Mouse uterine weight test showed that compared with the control group, the aqueous extracts ofC. Semen can increase the uterus index of premature female mice (P<0.01). It can significantly promote the proliferation of MCF-7 cells in the medium without estrogen (P<0.01). The reporter gene controlled by ERE technology showed thatwhen mediated by ERα or ERβ respectively, the normalized luciferase activity of aqueous extracts ofC. Semen was significantly higher than activity of the control group (P< 0.05 orP< 0.01). It was concluded that the aqueous extracts ofC.Semen can increase the uterus index of premature female mice and promote the proliferation of MCF-7 cells in the medium without estrogen. We found the estrogenic effects ofC. Semen for the first time. And the estrogenic effects ofC. Semen were mainly mediated by ERβ.
ABSTRACT
Objective To evaluate the efficacy of transcatheter arterial chemoembolization through left inferior phrenic artery (LIPA) in hepatocellular carcinoma (HCC) feeded by LIPA. Methods Angiographic data of 187 HCC patients were retrospectively analyzed. Five patients with LIPA feeding HCC were diagnosed and successfully treated with TACE through LIPA. Results All 5 patients underwent CT and angiography after 3 months, 3 of them achieved complete remission. LIPA recanalized in the other 2 patients, then these 2 patients underwent TACE through LIPA again. Conclusion LIPA could formed lateral branch to feed HCC. TACE through LIPA is safe and effective.
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Objective To explore the influence of montelukast on plasma nitric oxide in preschool children with asthma.Methods Forty-four preschool children with asthma aged 2-5 years who firstly met a criterion of asthma and treated 4 weeks with montelukast were investigated;and nitric oxide levels of plasma were inspected respectively before treatment and after treatment 1 week,4 weeks.Results The level of nitric oxide in the plasma of asthmatic children was obviously higher than that in normal control group(P
ABSTRACT
A novel reaction-enzymatic ammonolysis discovered in the mid of 1990s has been demonstrated to be a very promising alternative in the preparation of optically pure compounds. The effects of organic solvent, initial water activity, temperature and additives on lipase Novozym435-catalyzed enantioselective ammonolysis of racemic phenylglycine methyl ester were investigated systematically in this paper. Enzymatic reaction of ammonolysis showed higher activity and enantioselectivity than the corresponding reaction of hydrolysis and alcoholysis.
Subject(s)
Alcohols , Ammonia , Catalysis , Dimethylformamide , Pharmacology , Esters , Glycine , Metabolism , Hexoses , Pharmacology , Hydrolysis , Lipase , Metabolism , Organic Chemicals , Solvents , Surface-Active Agents , Pharmacology , Temperature , WaterABSTRACT
Enzymatic hydrolysis of nitrile was performed under mild conditions and afford high efficiency and selectivity,thus being highly potential for the synthesis of optically active carboxylic acids and their derivatives.The type of nitrile-hydrolyzing enzymes and hydrolysis reactions,reaction characteristics,factors influencing the hydrolysis and the prospect for its application to industrial production were reviewed in this paper.