Anti-HIV-1 integrase diterpenoids from Dichrocephala benthamii. (December 2015)

• Record Type: Journal Article
• Authors: Song, Bo; Ding, Gang; Tian, Xin-hui; Li, Li; Zhou, Chao; Zhang, Qiu-bo; Wang, Meng-hua; Zhang, Tao; Zou, Zhong-mei
• Is Part Of: Phytochemistry letters. Volume 14(2015:Dec.)
• Page Start: 249
• Page End: 253
• Publication Date: 2015-12
• Subjects: Asteraceae -- Dichrocephala benthamii -- Clerodane diterpenoids -- HIV-1 integrase; Botanical chemistry -- Periodicals; Chimie végétale -- Périodiques; 572.205
• DOI: 10.1016/j.phytol.2015.10.027
• Languages: English
• ISSNs: 1874-3900

Abstract

Graphical abstract: Highlights: Five new clerodane diterpenoids were isolated from Dichrocephala benthamii . Compound1 possesses a rare pentacyclic ring with highly oxygenated functionalities. Compound6 exhibited the most potential inhibitory activity against HIV-1 integrase. Abstract: Five new clerodane diterpenoid dichrocephnoids A–E (1, 2, 6–8 ) together with three known analogues were isolated from the whole herb of Dichrocephala benthamii C.B. Clarke. Their structures were elucidated on the basis of spectroscopic analyses (UV, IR, MS, 1D and 2D NMR). The relative configurations of the new compounds were established by NOESY correlations, and the absolute configuration of1 was determined on the basis of CD methods. Dichrocephnoid A (1 ) possesses a very rare pentacyclic ring system with highly oxygenated functionalities. All of the isolated compounds exhibited inhibitory activity against HIV-1 integrase, however, dichrocephnoid C (6 ) showed the most promising inhibition of the enzyme with IC50 value of 12.35 ± 1.27 μM.