Chemical constituents and their anti-inflammatory activities from the roots of Ardisia crenata var. bicolor

Abstract

Ardisia crenata var. bicolor is a common medicine used by Miao Minority in Guizhou, which has the effects of clearing throat and benefiting pharynx, reducing swelling and relieving pain, dispelling wind and dehumidifying. In order to study the chemical constituents and anti-inflammatory activities of A. crenata var. bicolor roots, the 70% ethanol extact was separated and purified by silica gel column chromatography, Sephadex LH-20 gel column chromatography, ODS reverse column chromatography and semi-preparative HPLC. The structures of the compounds were identified by spectral data of NMR, MS and published literatures. Using lipopolysaccharide (LPS)-activated RAW 264.7 cell line model in vitro, compounds 1-4 were evaluated for the inhibition against nitric oxide (NO) production. The results were as follows: (1) Ten compounds were isolated from the 70% ethanol extract and identified as 11-O-galloylbergenin (1), 11-O-(4-O-methylgalloyl) bergenin (2), 11-O-vanilloylbergenin (3), 6-O-(4-hydroxy benzoyl) bergenin (4), 11-syringylbergenin (5), 11-O-(3′,4′-dimethylgalloyl)-bergenin (6), demethoxybergenin (7), micractinin A (8), monomethyl olivetol (9), and dibutyl phthalate (10). Among them, compounds 4, 8, 9 were obtained from Ardisia for the first time. (2) The results of anti-inflammatory activities in vitro showed that compounds 1-4 could significantly inhibit NO release in RAW 264.7 cells (P<0.01), and the inhibition rates of compounds at the concentration of 20 μmol·mL-1 were 67.09%, 66.50%, 59.83%, 36.47%, respectively. This study enriches the chemical constituents of A. crenata var. bicolor roots, clarifies the material basis of its anti-inflammatory activities, verifies the scientificity of its traditional usage, and provides new insight and scientific evidence for its rational development and utilization of the medicinal resources.

Keywords

• ardisia crenata var. bicolor root
• chemical constituents
• isolation and purification
• structure identification
• bergenin
• anti-inflammatory activity