Studies On The Chemical Constituents And Bioactivities Of Ardisia Crenata Sims

Ardisia crenata Sims of Myrsinaceae family is widely distributed in thesouthern parts of China such as Jiangsu, Anhui, Zhejiang, Jiangxi, Fujian, Hunan,Guangxi, Guangdong, Sichuan and Yunnan provinces. Its roots have been used in thetreatment of respiratory tract infections and menstrual disorders and the significanteffects are well documented in Chinese traditional medicine.In our search for bioactive components via bioactivity trace from this plant, 13compounds were isolated by chromatograms of silica gel, ODS, sephadex LH-20 andDA101. Their structures were elucidated by analysis of several spectra such as UV, IR,MS, 1D-NMR and 2D-NMR and chemical methods. A new triterpene saponin amongthe 13 compounds was named as 3β-O{α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranosyl-(1→4)-[β-D-glucopyransyl-(1→2)]-α-L-arabinopyranosyl}-16α, 28-dihydrox-y-olean-12-en-30-oic acid 30-O-[3'-O-α-D-glucopyranumate] ester(1), the restknown compounds were listed below as ardisicrenoside D (2), 3β-O-{α-L-rhamn-opyranosyl-(1→2)-β-D-glucopyranosyl-(1→4)-α-L-arabinopyranosyl} cyclamiritinA(3), primulanin (4), cyclaminorin (5), ardisiacrispin B (6), ardisiacrenoside A (7),ardisimamilloside F (8), bergenin (9), norbergenin (10), astragalin (11),β-daucosterol(12),α-D-glucose (13).The anti-tumour bioactivities of all the extracts and compounds were evaluatedby MTT method. The extracts of n-butanol resulted in the IC₅₀ (μg/ml) 1.59, 1.67,1.78, 1.78, 2.05, 1.64 against KB, HCT-8, Be17402, BGC-823, A2780, respectively.Three triterpenoid trisaccharides 3, 4, 5 showed singnificant effects against A2780with IC₅₀ (μg/ml) 2.48, 1.51, 6.40, respectively. Ardisiacrispin B (6) showed strongercytotoxic activities against HCT-8, Be17402, BGC-823, A549, A2780, and KETR3.Their IC₅₀ (μg/ml) were 1.59, 1.67, 1.78, 1.78, 2.05, and 1.64, respectively. In orderto confirm its anti-tumor activity, ardisiacrispin B was subjected to H22 in mice withCTX as positive contrast and showed inhibit rate of 43.9% after 10 days at the doseof 10 mg/kg/day.