Inhibitory Effects of Compounds and Extracts fromAmpelopsis brevipedunculataon IL-6-Induced STAT3 Activation

Author:

Jang Hyun-Jae1ORCID,Lee Seung-Jae1,Lim Hyung-Jin1,Jung Kyungsook1,Lee Soyoung1,Park Chan Sun1,Lee Seung Woong1ORCID,Rho Mun-Chual1ORCID

Affiliation:

1. Immunoregulatory Material Research Center, Korea Research Institute of Bioscience and Biotechnology, 181 Ipsin-gil, Jeongeup-si, Jeonbuk 56212, Republic of Korea

Abstract

Ampelopsis brevipedunculata(Maxim.) Trautv. (AB), a traditional East Asian medicine, exhibits protective effects against several inflammatory diseases. Our search for an inhibitor of IL-6-induced JAK2/STAT3 activation revealed that AB ethanolic extract (ABE) had a significant inhibitory effect on IL-6-induced STAT3 expression in Hep3B cells. The isolation and purification of an EtOAc-soluble fraction of ABE (ABEA) using reversed-phase high-performance liquid chromatography (RP-HPLC) afforded 17 compounds. The structures of these compounds (1-17) were elucidated based on1H and13C nuclear magnetic resonance (NMR) spectroscopy as well as electrospray-ionization mass spectrometry (ESI-MS) data. ABE and ABEA were screened by a luciferase assay using Hep3B cells transfected with the STAT3 reporter gene. ABEA exhibited potent inhibitory effects on IL-6-induced STAT3 expression; moreover, these effects arose from the inhibition of the phosphorylation of the STAT3, JAK2, and ERK proteins in U266 cells. In addition, the compounds isolated from ABEA were measured for their inhibitory effects on IL-6-stimulated STAT3 expression. Of the compounds isolated, betulin showed the greatest inhibitory effects on IL-6-induced STAT3 activation in the luciferase assay (IC50value: 3.12μM). Because of its potential for inhibiting STAT3 activation,A. brevipedunculatacould be considered a source of compounds of pharmaceutical interest.

Funder

Korea Research Institute of Bioscience and Biotechnology

Publisher

Hindawi Limited

Subject

General Immunology and Microbiology,General Biochemistry, Genetics and Molecular Biology,General Medicine

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