Isoprenylated flavonoids from Morus nigra and their PPAR γ agonistic activities

  • Fitoterapia. 2018 Jun:127:109-114. doi: 10.1016/j.fitote.2018.02.004.
Liang-Jin Xu  1 ,  Mei-Hua Yu  2 ,  Chun-Yue Huang  1 ,  Li-Xin Niu  1 ,  Yi-Fan Wang  3 ,  Chun-Zhen Wu  1 ,  Pei-Ming Yang  1 ,  Xiao Hu  4
Affiliations
  • 1. Innovation Center of Chinese Medicine, China State Institute of Pharmaceutical Industry, Shanghai 201203, China.
  • 2. Department of Pharmacognosy, School of Pharmacy, Fudan University, Shanghai 201203, China.
  • 3. Innovation Center of Chinese Medicine, China State Institute of Pharmaceutical Industry, Shanghai 201203, China; Department of Pharmacognosy, School of Pharmacy, Fudan University, Shanghai 201203, China.
  • 4. Innovation Center of Chinese Medicine, China State Institute of Pharmaceutical Industry, Shanghai 201203, China. Electronic address: [email protected].
PMID: 29427594 DOI: 10.1016/j.fitote.2018.02.004
Abstract

A novel dihydroflavonol unprecedentedly with a prenyl group at C-2, nigragenon A (1), four new sanggenon-type Flavonones, nigragenons B-E (2-5), along with six known isoprenylated Flavonoids (6-11) were isolated from the twigs of Morus nigra. Their structures were elucidated through extensive analysis of spectroscopic data. Interestingly, compound 1 was the first reported biogenetic precursor of sanggenon-type flavanones and the biogenetic pathway from 1 to sanggenol F was proposed. The PPAR γ agonistic activity was investigated in HEK293 cells using dual luciferase reporter assay. Compounds 2, 4, 7, and 9 showed obvious agonistic activities on PPAR γ, and compound 2 was a potential PPAR γ partial agonist. Moreover, the preliminary structure-activity relationships for the tested compounds were discussed.

Keywords
Agonistic activity; Moraceae; Morus nigra; PPAR γ; Sanggenon-type flavonones.
Products