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.
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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 |
Journal | Nature communications
(Nat Commun)
Vol. 10
Issue 1
Pg. 1981
(04 30 2019)
ISSN: 2041-1723 [Electronic] England |
PMID | 31040273
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Hypoglycemic Agents
- Berberine
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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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