RESUMO
OBJECTIVE: To study chemical constituents from rhizome of Daphne papyracea var. crassiuscula. METHOD: Ethyl acetate fraction of 75% ethanol extracts from rhizome of D. papyracea var. crassiuscula, and its strucutre was identified by spectral method. RESULT: Nine compounds were separated and identified as daphneticin (1), daphnetin (2), hydrangetin (3), daphnoretin (4), 1-4'-hydroxyphenyl-5-phenyl-2 (E)-en-1-pentanone (5), daphneolon (6), 3beta-O-acetyl-olean-12-en (7), and (+)-usnic acid (8). CONCLUSION: Compounds 1-8 were separated from D. papyracea var. crassiuscula for the first time. Compound 8 was separated from the genus for first time.
Assuntos
Daphne/química , Medicamentos de Ervas Chinesas/química , Rizoma/química , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas/isolamento & purificação , Espectroscopia de Ressonância Magnética , Estrutura MolecularRESUMO
PURPOSE: To evaluate oleanolic acid derivatives on liver disease related bioactivities, 29 oleanolic acid derivatives of several series were tested for their inhibitory activity on hepatitis C viral protease and for their cytotoxic effects on Hep G2 cells. RESULTS: The amino derivatives showed potent cytotoxicity, among which, the beta-amino isomer exhibited more distinct cytotoxicity than the alpha-isomer. The cytotoxicity of hemiesters and hemiamides varied as the chain lengths varied. The oxalic and malonic hemiesters showed weaker cytototoxicity than oleanolic acid, while those with longer chain lengths showed higher cytotoxicity. Contrary to the cytotoxic activity, the free amino derivatives showed little inhibitory activity on HCV protease. All the hemiesters and hemiamides showed high activity against HCV protease. CONCLUSION: The findings that addition of amino-group enhanced the cytotoxicity and that introduction of acidic group increased the inhibition on HCV protease may be useful for further design and synthesis of triterpene derivatives as drug candidates for liver diseases.
Assuntos
Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Inibidores Enzimáticos/farmacologia , Hepacivirus/enzimologia , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/farmacologia , Proteínas não Estruturais Virais/antagonistas & inibidores , Antivirais/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Células Hep G2 , Hepacivirus/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Neoplasias Hepáticas/tratamento farmacológico , Relação Estrutura-Atividade , Proteínas não Estruturais Virais/metabolismoRESUMO
OBJECTIVE: A HPLC method is established to determine the content of trigonelline in Trigonella foenum-graecum. METHOD: The medicinal material was extracted by petholeum ether-ethanol. Asahipak NH2P-50 column was used, mobilephase consisted of acetonitrile-water(75:25) and detection wavelength was set at UV 265 nm. RESULT: The standard curve was linear in the range of 3.68-73.60 micrograms.mL-1 with the correlation coefficient of 0.9999. The average recovery rate and RSD were 97.4% and 1.83% (n = 6) respectively. CONCLUSION: It provides scientific indexes for quality control of T. foenum-graecum.