中药药性理论一直是中医药基础研究的难点和热点,但至今尚未取得重要突破。寒热辨证为中医首要辨证,寒热药性是中药的首要药性,"寒者热之、热者寒之"是中医首要治则,但是究竟寒热药性是否客观存在?能否/如何建立一套客观可行...中药药性理论一直是中医药基础研究的难点和热点,但至今尚未取得重要突破。寒热辨证为中医首要辨证,寒热药性是中药的首要药性,"寒者热之、热者寒之"是中医首要治则,但是究竟寒热药性是否客观存在?能否/如何建立一套客观可行的寒热药性评价方法体系?如何以寒热药性理论及其研究成果指导中医药实践?近年来课题组独辟蹊径,主要从热力学角度对中药寒热药性进行了一系列探索和研究,首次提出了"中医药(药性)热力学观"(thermodynam ic outlook of Ch inesem ed ic ine),建立了"源于临床,证于实验,回归临床"的中药药性研究模式,研制开发一套可用于中药寒热药性差异表征与评价的方法体系(包括冷热板差示法,微量量热法,药性循证医学分析),从体外到体内、从实验到临床,较系统地考察了机体新陈代谢过程中的能量转移和热变化及其不同寒热药性中药的干预效果,揭示中药寒热药性差异的客观性以及"寒者热之、热者寒之"的科学性,为审视和研究中药药性理论提供了新的视角和方法,为中医药现代化发展提供了新的科技支持。展开更多
The inhibitory effects of three berberine alkaloids (BAs) from rhizome of Coptis chinensis Franch, a traditional Chinese medicinal (TCM) herb, on Staphylococcus aureus growth were investigated by mi- crocalorimetry. T...The inhibitory effects of three berberine alkaloids (BAs) from rhizome of Coptis chinensis Franch, a traditional Chinese medicinal (TCM) herb, on Staphylococcus aureus growth were investigated by mi- crocalorimetry. The power–time curves of S. aureus with and without BAs were acquired; meanwhile the extent and duration of inhibitory effects on the metabolism were evaluated by studying the growth rate constant (k), half inhibitory ratio (IC50), maximum heat-output power (Pmax), peak time of maximum heat-output power (tp) and total heat production (Qt). The value of k of S. aureus in the presence of the three BAs decreased with the increasing concentrations of BAs. Moreover, Pmax was reduced and the value of tp increased with increasing concentrations of the three drugs. The inhibitory activity varied with different drugs. The values of IC50 of the three BAs are respectively, 101.4 μg/mL for berberine, 241.0 μg/mL for palmatine and 792.3 μg/mL for jateorrhizine. The sequence of antimicrobial activity of the three BAs is: berberine > palmatine > jateorrhizine. It is suggested that the functional group me- thylenedioxy or methoxyl at C2 on the phenyl ring could possibly improve antimicrobial activity more strongly than hydroxyl at C2 on the phenyl ring.展开更多
The inhibitory effects of five berberines alkaloids (BAs) from rhizoma ofCoptis chinensis Franch,a traditional Chinese medicinal (TCM) herb,on Bacillus shigae(B.shigae)growth were investigated by microcalorimetry.The ...The inhibitory effects of five berberines alkaloids (BAs) from rhizoma ofCoptis chinensis Franch,a traditional Chinese medicinal (TCM) herb,on Bacillus shigae(B.shigae)growth were investigated by microcalorimetry.The power-time curves of B.shigae with and without BAswere acquired;meanwhile,the extent and duration of inhibitory effects on the metabolism wereevaluated by growth rate constants (k1,k2),half inhibitory ratio (IC50),maximum heat output(P_(max)),and peak time (t_p).The values of k1 and k2 of a shigae in the presence of the five BAsdecreased with the increasing concentrations of BAs.Moreover,P_(max) was reduced,and the value oft_p increased with increasing concentrations of the five drugs.The inhibitory activity varied withdifferent drugs.IC50 of the five BAs was respectively 75 mu g/mL for berberine,90 ng/mL forcoptisine,115 mu g/mL for palmatine,220 mu g/mL for epiberberine,and 400 mu g/mL forjatrorrhizine.The sequence of antimicrobial activity of the five BAs:berberine 】 coptisine 】palmatine 】 epiberberine 】 jatrorrhizine.The functional groups methylenedioxy at C2 and C3 on phenylring improve antimicrobial activity more strongly than methoxyl at C2 and C3 on phenylring.However,the effect of bacteriostasis is not significant with methylenedioxy or methoxyl at C9and C10 on phenyl ring.展开更多
文摘中药药性理论一直是中医药基础研究的难点和热点,但至今尚未取得重要突破。寒热辨证为中医首要辨证,寒热药性是中药的首要药性,"寒者热之、热者寒之"是中医首要治则,但是究竟寒热药性是否客观存在?能否/如何建立一套客观可行的寒热药性评价方法体系?如何以寒热药性理论及其研究成果指导中医药实践?近年来课题组独辟蹊径,主要从热力学角度对中药寒热药性进行了一系列探索和研究,首次提出了"中医药(药性)热力学观"(thermodynam ic outlook of Ch inesem ed ic ine),建立了"源于临床,证于实验,回归临床"的中药药性研究模式,研制开发一套可用于中药寒热药性差异表征与评价的方法体系(包括冷热板差示法,微量量热法,药性循证医学分析),从体外到体内、从实验到临床,较系统地考察了机体新陈代谢过程中的能量转移和热变化及其不同寒热药性中药的干预效果,揭示中药寒热药性差异的客观性以及"寒者热之、热者寒之"的科学性,为审视和研究中药药性理论提供了新的视角和方法,为中医药现代化发展提供了新的科技支持。
基金Supported by the National Natural Science Foundation of China (Grant No. 30625042)
文摘The inhibitory effects of three berberine alkaloids (BAs) from rhizome of Coptis chinensis Franch, a traditional Chinese medicinal (TCM) herb, on Staphylococcus aureus growth were investigated by mi- crocalorimetry. The power–time curves of S. aureus with and without BAs were acquired; meanwhile the extent and duration of inhibitory effects on the metabolism were evaluated by studying the growth rate constant (k), half inhibitory ratio (IC50), maximum heat-output power (Pmax), peak time of maximum heat-output power (tp) and total heat production (Qt). The value of k of S. aureus in the presence of the three BAs decreased with the increasing concentrations of BAs. Moreover, Pmax was reduced and the value of tp increased with increasing concentrations of the three drugs. The inhibitory activity varied with different drugs. The values of IC50 of the three BAs are respectively, 101.4 μg/mL for berberine, 241.0 μg/mL for palmatine and 792.3 μg/mL for jateorrhizine. The sequence of antimicrobial activity of the three BAs is: berberine > palmatine > jateorrhizine. It is suggested that the functional group me- thylenedioxy or methoxyl at C2 on the phenyl ring could possibly improve antimicrobial activity more strongly than hydroxyl at C2 on the phenyl ring.
基金Supported by the National Natural Science Foundation of China (Grant No. 39970911)
文摘The inhibitory effects of five berberines alkaloids (BAs) from rhizoma ofCoptis chinensis Franch,a traditional Chinese medicinal (TCM) herb,on Bacillus shigae(B.shigae)growth were investigated by microcalorimetry.The power-time curves of B.shigae with and without BAswere acquired;meanwhile,the extent and duration of inhibitory effects on the metabolism wereevaluated by growth rate constants (k1,k2),half inhibitory ratio (IC50),maximum heat output(P_(max)),and peak time (t_p).The values of k1 and k2 of a shigae in the presence of the five BAsdecreased with the increasing concentrations of BAs.Moreover,P_(max) was reduced,and the value oft_p increased with increasing concentrations of the five drugs.The inhibitory activity varied withdifferent drugs.IC50 of the five BAs was respectively 75 mu g/mL for berberine,90 ng/mL forcoptisine,115 mu g/mL for palmatine,220 mu g/mL for epiberberine,and 400 mu g/mL forjatrorrhizine.The sequence of antimicrobial activity of the five BAs:berberine 】 coptisine 】palmatine 】 epiberberine 】 jatrorrhizine.The functional groups methylenedioxy at C2 and C3 on phenylring improve antimicrobial activity more strongly than methoxyl at C2 and C3 on phenylring.However,the effect of bacteriostasis is not significant with methylenedioxy or methoxyl at C9and C10 on phenyl ring.
