1. Liver-target nanotechnology facilitates berberine to ameliorate cardio-metabolic diseases.
- Author
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Guo HH, Feng CL, Zhang WX, Luo ZG, Zhang HJ, Zhang TT, Ma C, Zhan Y, Li R, Wu S, Abliz Z, Li C, Li XL, Ma XL, Wang LL, Zheng WS, Han YX, and Jiang JD
- Subjects
- Animals, Caco-2 Cells, Cardiovascular Diseases blood, Cardiovascular Diseases drug therapy, Dyslipidemias blood, Dyslipidemias drug therapy, Hep G2 Cells, Humans, Hypoglycemic Agents pharmacology, Lipid Metabolism drug effects, Liver drug effects, Liver metabolism, Magnetic Resonance Spectroscopy, Male, Metabolic Diseases blood, Metabolic Diseases drug therapy, Mice, Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization, Berberine pharmacology, Hypoglycemic Agents therapeutic use, Nanotechnology methods
- 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.
- Published
- 2019
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