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 effect of three berberine alkaloids (BAs) from Coptis chinensis Franch, a traditional Chinese medicinal (TCM) herb, on Bifidobacterium adolescentis growth was investigated by micro- calorimetry. The pow...The inhibitory effect of three berberine alkaloids (BAs) from Coptis chinensis Franch, a traditional Chinese medicinal (TCM) herb, on Bifidobacterium adolescentis growth was investigated by micro- calorimetry. The power-time curves of B. adolescentis with and without BAs were acquired, meanwhile the extent and duration of inhibitory effect on the metabolism were evaluated by the growth rate con- stant (k), half inhibitory ratio (IC50), maximum heat-output power (Pmax), peak time of maximum heat-output power (tp) and total heat production (Qt). k, Pmax and Qt decreased, and tp was prolonged with the increase of BAs concentration. The IC50 of BAs is 806 μg/mL for berberine, 341 μg/mL for cop- tisine and 236 μg/mL for palmatine. The sequence of antimicrobial activity of BAs is berberine < cop- tisine < palmatine. Combined with previous studies, it could be shown that the sequences of antim- icrobial activity of BAs on both Bacillus shigae and Escherichia coli are berberine > coptisine > pal- matine. The structure-function relationship of BAs indicates that the functional group methylenedioxy or methoxyl at C2 and C3 might be the major group inducing the activities of BAs on E. coli and B. adolescentis. Meanwhile, the substituent groups at C2, C3, C9 and C10 almost have equal effect on B. shigae.展开更多
8-Oxocoptisine 1,a natural protoberberine alkaloid,can be more easily achieved starting from readily available and inexpensive berberine hydrochlorate 2.The structure of the target compound 1 was confirmed by melting ...8-Oxocoptisine 1,a natural protoberberine alkaloid,can be more easily achieved starting from readily available and inexpensive berberine hydrochlorate 2.The structure of the target compound 1 was confirmed by melting point,1H NMR,IR,MS and elemental analysis.展开更多
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 Nos. 30625042 and 30873385)Key Projects of National Science & Technology Pillar Program of China in the 11th Five-Year Period (Grant No. 2007BAI40B05)
文摘The inhibitory effect of three berberine alkaloids (BAs) from Coptis chinensis Franch, a traditional Chinese medicinal (TCM) herb, on Bifidobacterium adolescentis growth was investigated by micro- calorimetry. The power-time curves of B. adolescentis with and without BAs were acquired, meanwhile the extent and duration of inhibitory effect on the metabolism were evaluated by the growth rate con- stant (k), half inhibitory ratio (IC50), maximum heat-output power (Pmax), peak time of maximum heat-output power (tp) and total heat production (Qt). k, Pmax and Qt decreased, and tp was prolonged with the increase of BAs concentration. The IC50 of BAs is 806 μg/mL for berberine, 341 μg/mL for cop- tisine and 236 μg/mL for palmatine. The sequence of antimicrobial activity of BAs is berberine < cop- tisine < palmatine. Combined with previous studies, it could be shown that the sequences of antim- icrobial activity of BAs on both Bacillus shigae and Escherichia coli are berberine > coptisine > pal- matine. The structure-function relationship of BAs indicates that the functional group methylenedioxy or methoxyl at C2 and C3 might be the major group inducing the activities of BAs on E. coli and B. adolescentis. Meanwhile, the substituent groups at C2, C3, C9 and C10 almost have equal effect on B. shigae.
文摘8-Oxocoptisine 1,a natural protoberberine alkaloid,can be more easily achieved starting from readily available and inexpensive berberine hydrochlorate 2.The structure of the target compound 1 was confirmed by melting point,1H NMR,IR,MS and elemental analysis.
