Monomeric and dimeric guaianolide sesquiterpenoids with hypoglycemic activity from Achillea alpina.

Autor: Xue GM; College of Pharmacy, Henan University of Chinese Medicine, Zhengzhou 450046, China. Electronic address: xueguimin123@126.com., Zhao CG; College of Pharmacy, Henan University of Chinese Medicine, Zhengzhou 450046, China., Xue JF; College of Pharmacy, Henan University of Chinese Medicine, Zhengzhou 450046, China., Duan JJ; College of Pharmacy, Henan University of Chinese Medicine, Zhengzhou 450046, China., Pan H; College of Pharmacy, Henan University of Chinese Medicine, Zhengzhou 450046, China., Jia YY; College of Pharmacy, Henan University of Chinese Medicine, Zhengzhou 450046, China., Du K; College of Pharmacy, Henan University of Chinese Medicine, Zhengzhou 450046, China., Zhi YL; College of Pharmacy, Henan University of Chinese Medicine, Zhengzhou 450046, China., Feng WS; College of Pharmacy, Henan University of Chinese Medicine, Zhengzhou 450046, China. Electronic address: fwsh@hactcm.edu.cn.
Jazyk: angličtina
Zdroj: Fitoterapia [Fitoterapia] 2023 Apr; Vol. 166, pp. 105472. Date of Electronic Publication: 2023 Mar 11.
DOI: 10.1016/j.fitote.2023.105472
Abstrakt: Three new monomeric (1-3) and two newdimeric guaianolides (4 and 5), along with three known analogues (6-8) were isolated from the aerial part of Achillea alpina L. Compounds 1-3 were three novel 1,10-seco-guaianolides, while 4 and 5 were two novel 1,10-seco-guaianolides involved heterodimeric [4 + 2] adducts. The new structures were elucidated by analysis of spectroscopic data and quantum chemical calculations. All isolates were evaluated for their hypoglycemic activity with a glucose consumption model in palmitic acid (PA)-induced HepG2-insulin resistance (IR) cells, and compound 1 showed the most promising activity. A mechanistic study revealed that compound 1 appeared to mediate hypoglycemic activity via inhibition of the ROS/TXNIP/NLRP3/caspase-1 pathway.
Competing Interests: Declaration of Competing Interest The authors declare no conflicts of interest for this study.
(Copyright © 2023. Published by Elsevier B.V.)
Databáze: MEDLINE