Liver-target nanotechnology facilitates berberine to ameliorate cardio-metabolic diseases

Hui-Hui Guo, Chen-Lin Feng, Wen-Xuan Zhang, Zhi-Gang Luo, Hong-Juan Zhang, Ting-Ting Zhang, Chen Ma, Yun Zhan, Rui Li, Song Wu, Zeper Abliz, Cong Li, Xiao-Lin Li, Xiao-Lei Ma, Lu-Lu Wang (), Wen-Sheng Zheng (), Yan-Xing Han () and Jian-Dong Jiang ()
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Hui-Hui Guo: Chinese Academy of Medical Sciences and Peking Union Medical College
Chen-Lin Feng: Chinese Academy of Medical Sciences and Peking Union Medical College
Wen-Xuan Zhang: Chinese Academy of Medical Sciences and Peking Union Medical College
Zhi-Gang Luo: Chinese Academy of Medical Sciences and Peking Union Medical College
Hong-Juan Zhang: Chinese Academy of Medical Sciences and Peking Union Medical College
Ting-Ting Zhang: Chinese Academy of Medical Sciences and Peking Union Medical College
Chen Ma: Chinese Academy of Medical Sciences and Peking Union Medical College
Yun Zhan: Chinese Academy of Medical Sciences and Peking Union Medical College
Rui Li: Chinese Academy of Medical Sciences and Peking Union Medical College
Song Wu: Chinese Academy of Medical Sciences and Peking Union Medical College
Zeper Abliz: Chinese Academy of Medical Sciences and Peking Union Medical College
Cong Li: Chinese Academy of Medical Sciences and Peking Union Medical College
Xiao-Lin Li: Chinese Academy of Medical Sciences and Peking Union Medical College
Xiao-Lei Ma: Chinese Academy of Medical Sciences and Peking Union Medical College
Lu-Lu Wang: Chinese Academy of Medical Sciences and Peking Union Medical College
Wen-Sheng Zheng: Chinese Academy of Medical Sciences and Peking Union Medical College
Yan-Xing Han: Chinese Academy of Medical Sciences and Peking Union Medical College
Jian-Dong Jiang: Chinese Academy of Medical Sciences and Peking Union Medical College

Nature Communications, 2019, vol. 10, issue 1, 1-16

Abstract: Abstract Cardiovascular and metabolic disease (CMD) remains a main cause of premature death worldwide. Berberine (BBR), a lipid-lowering botanic compound with diversified potency against metabolic disorders, is a promising candidate for ameliorating CMD. The liver is the target of BBR so that liver-site accumulation could be important for fulfilling its therapeutic effect. In this study a rational designed micelle (CTA-Mic) consisting of α-tocopheryl hydrophobic core and on-site detachable polyethylene glycol-thiol shell is developed for effective liver deposition of BBR. The bio-distribution analysis proves that the accumulation of BBR in liver is increased by 248.8% assisted by micelles. Up-regulation of a range of energy-related genes is detectable in the HepG2 cells and in vivo. In the high fat diet-fed mice, BBR-CTA-Mic intervention remarkably improves metabolic profiles and reduces the formation of aortic arch plaque. Our results provide proof-of-concept for a liver-targeting strategy to ameliorate CMD using natural medicines facilitated by Nano-technology.

Date: 2019
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DOI: 10.1038/s41467-019-09852-0

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