Related Experiment Videos
Monoterpenoid bisindole alkaloids with intestinal anti-inflammatory activity from Kopsia hainanensis
Jiamin Wang1, Niping Li1, Zhuoying Lin1
1State Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, Jinan University, Guangzhou, 510632, PR China; Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, and Guangdong-Hong Kong-Macau Joint Laboratory for Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, 510632, PR China.
Abstract:
Five previously undescribed monoterpenoid bisindole alkaloids, kopsileuconines E-I (1-5), along with one known analogue (6), were isolated from Kopsia hainanensis Tsiang. Compound 1 represents the first example of an aspidofractinine-type dimer conjugated with a phenylpropanoid unit via an N-1'-C-9″ bond. Compounds 2-5 are dimeric aspidofractinine alkaloids connected by a methylene bridge (2) or a C-14-C-5' bond (3-5). Among them, compounds 2, 4, and 5 dose-dependently suppressed IL-6, IL-1β, and TNF-α mRNA in an LPS-induced Caco-2/THP-1 co-culture model of intestinal inflammation. Further investigation showed that the most potent compound 5 exhibited in vitro intestinal anti-inflammatory and barrier-protective effects by inhibiting the TLR4/NF-κB signaling pathway.
