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

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.
AuthorsHui-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
JournalNature communications (Nat Commun) Vol. 10 Issue 1 Pg. 1981 (04 30 2019) ISSN: 2041-1723 [Electronic] England
PMID31040273 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Hypoglycemic Agents
  • Berberine
Topics
  • Animals
  • Berberine (pharmacology)
  • Caco-2 Cells
  • Cardiovascular Diseases (blood, drug therapy)
  • Dyslipidemias (blood, drug therapy)
  • Hep G2 Cells
  • Humans
  • Hypoglycemic Agents (pharmacology, therapeutic use)
  • Lipid Metabolism (drug effects)
  • Liver (drug effects, metabolism)
  • Magnetic Resonance Spectroscopy
  • Male
  • Metabolic Diseases (blood, drug therapy)
  • Mice
  • Nanotechnology (methods)
  • Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization

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