2. Academic Validation
  3. Novel berberine-based derivatives with potent hypoglycemic activity

Novel berberine-based derivatives with potent hypoglycemic activity

  • Bioorg Med Chem Lett. 2019 Dec 1;29(23):126709. doi: 10.1016/j.bmcl.2019.126709.
Jian-Ta Wang 1,  Jin-Gang Peng 2,  Ji-Quan Zhang 3,  Zhong-Xiao Wang 2,  Yi Zhang 3,  Xun-Rong Zhou 4,  Jing Miao 2,  Lei Tang 5
Affiliations

Affiliations

  • 1 State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, Guizhou Medical University, Guiyang 550004, China; School of Basic Medical Sciences, Guizhou Medical University, Guiyang 550004, China; Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guiyang 550004, China.
  • 2 State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, Guizhou Medical University, Guiyang 550004, China.
  • 3 State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, Guizhou Medical University, Guiyang 550004, China; Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guiyang 550004, China.
  • 4 The Second Affiliated Hospital of Guizhou Chinese Traditional Medicine University, Guiyang 550001, China.
  • 5 State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, Guizhou Medical University, Guiyang 550004, China; Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guiyang 550004, China. Electronic address: tlei1974@163.com.
PMID: 31629632 DOI: 10.1016/j.bmcl.2019.126709
Abstract

Four series of berberine derivatives were designed and synthesized. All the synthetic compounds were screened for in vitro glucose consumption activity in HepG2 cell lines. The results showed that most of the tested compounds exhibited potent hypoglycemic activity, and the most potent compound 20b exhibited its potency by 3.23-fold of berberine, 1.39-fold of metformin and 1.20-fold of rosiglitazone, respectively. Western blot assay indicated these novel berberine-based derivatives executed their glucose-decreasing activity via the activation of AMPK pathway.

Keywords

AMP-activated protein kinase; Berberine; Hypoglycemic activity; Synthesis; Type 2 diabetes.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z