Significant pharmacokinetic differences of berberine are attributable to variations in gut microbiota between Africans and Chinese.
We investigated the influence of gut microbiotal metabolism on the pharmacokinetics of berberine in healthy male Africans and Chinese. The Cmax and AUC in the Africans were 2.67-fold and 2.0-fold higher than the Chinese, respectively. Microbiotal compositions by 16S rRNA pyrosequencing showed higher abundance of the genera Prevotella, Bacteroides, and Megamonas (34.22, 13.88, and 10.68%, respectively) in the Chinese than the Africans (30.08, 9.43, and 0.48%, respectively). Scatter plot showed a strong negative correlation between the microbiotal abundance and the berberine AUC, especially for the genus Prevotella (r = -0.813) and its species. A more extensive metabolism was observed in Chinese with 1.83-fold higher metabolites, possibly contributing to the lower AUC than the Africans. In conclusion, significant PK differences of berberine were observed between Africans and Chinese, which is partly attributable to variations in gut microbiota and its corresponding metabolic capacity.
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu, China.
Raphael N
RN
Alolga
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu, China.
Yong
Y
Fan
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu, China.
Zhuo
Z
Chen
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu, China.
Li-Wei
LW
Liu
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu, China.
Yi-Jing
YJ
Zhao
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu, China.
Jin
J
Li
Department of Emergency Center, the First Affiliated Hospital of Nanjing Medical University, Nanjing, Jiangsu, China.
Yan
Y
Chen
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu, China.
Mao-De
MD
Lai
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu, China.
Ping
P
Li
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu, China.
Lian-Wen
LW
Qi
D000328:Adult; D044466:Asian People; D001599:Berberine / Q000097:blood*; D044383:Black People; D000069196:Gastrointestinal Microbiome; D006801:Humans; D008297:Male
D001599:Berberine