Antinociceptive grayanane-derived diterpenoids from flowers of .
10.1016/j.apsb.2019.10.013
- Author:
Yong LI
1
;
Yuxun ZHU
1
;
Zhaoxin ZHANG
1
;
Li LI
1
;
Yunbao LIU
1
;
Jing QU
1
;
Shuanggang MA
1
;
Shishan YU
1
Author Information
1. State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
- Publication Type:Journal Article
- Keywords:
Analgesic;
Antinociceptive;
Dimeric;
Diterpenoid;
Grayanane;
Rhododendron molle
- From:
Acta Pharmaceutica Sinica B
2020;10(6):1073-1082
- CountryChina
- Language:English
-
Abstract:
Twelve new grayanoids (-) along with five known compounds were isolated from flowers of . Their structures were fully characterized using a combination of spectroscopic analyses, computational calculations, and single crystal X-ray diffraction. Rhomollone A () possesses an unprecedented 5/6/6/5 tetra-cyclic ring system (B- grayanane) incorporating a cyclopentene-1,3-dione scaffold. Rhodomollein XLIII () is a dimeric grayanoid, containing a novel 14-membered heterocyclic ring with a symmetry axis. The antinociceptive activities of compounds , , , , and - were evaluated by an acetic acid-induced writhing test. Among them, compounds , , , and displayed significant antinociceptive activities at a dose of 20 mg/kg with inhibition rates ranging from 41.9% to 91.6%. Compounds and inhibited 46.0% and 39.4% of the acetic acid-induced writhes at a dose of 2 mg/kg, while compound inhibited 34.3% of the writhes at a dose of 0.4 mg/kg.
