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

• DOI: 10.1038/s41467-019-09852-0
• Publication Date: 2019-04-30T10:03:45Z
• Authors: 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; Jian-Dong Jiang
• Keywords: Male; 0303 health sciences; Magnetic Resonance Spectroscopy; Berberine; Science; Q; Hep G2 Cells; Lipid Metabolism; Article; 3. Good health; Mice; 03 medical and health sciences; Liver; Metabolic Diseases; Cardiovascular Diseases; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; Animals; Humans; Hypoglycemic Agents; Nanotechnology; Caco-2 Cells; Dyslipidemias

AbstractCardiovascular 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.