Xu Jing, Guo Yuan-Qiang, Li Xian, Wei Kun, Zhao Xiao-Jun
Department of Pharmaceutical Sciences, Nankai University, Tianjin 300071, PR China.
J Ethnopharmacol. 2008 Apr 17;117(1):175-7. doi: 10.1016/j.jep.2008.01.028. Epub 2008 Feb 6.
To investigate the cytotoxic compounds against human melanoma A375-S2 and human cervical carcinoma Hela cell lines from the fruits of Celastrus orbiculatus.
The ethanol extract of the fruits of C. orbiculatus was found to exhibit significant cytotoxic activity. After partition, the column chromatography and Semi-preparative HPLC were used for activity guided fractionation from the active petroleum ether-soluble part. NMR and ESI-MS spectra for structure analysis were recorded on spectrometers, respectively. The cytotoxic activities of the isolated compounds were determined using the MTT assay.
Four sesquiterpenoids (1-4) were isolated by activity guided fractionation from the ethanol extract of the fruits of C. orbiculatus. Compounds 1-3 exhibited promising cytotoxicities against the Hela cells and A375-S2 cells. The cytotoxic activities of compounds 1-3 seemed to be dose-dependent, which exhibited more potent inhibition for the proliferation of two cell lines when increased the concentrations of every compounds. Among these compounds, compound 2 showed most cytotoxicities against either Hela cells or the A375-S2 cells.
The cytotoxic activity of the ethanol extract of fruits of C. orbiculatus against human melanoma A375-S2 and human cervical carcinoma Hela cells due to its content of sesquiterpenoids, supports its potential therapeutic value for the treatment of tumor.
研究南蛇藤果实中对人黑色素瘤A375 - S2细胞系和人宫颈癌Hela细胞系具有细胞毒性的化合物。
发现南蛇藤果实的乙醇提取物具有显著的细胞毒性活性。分离后，采用柱色谱和半制备高效液相色谱法对活性石油醚可溶部分进行活性导向分离。分别在光谱仪上记录用于结构分析的核磁共振和电喷雾电离质谱光谱。使用MTT法测定分离化合物的细胞毒性活性。
通过活性导向分离从南蛇藤果实的乙醇提取物中分离出四种倍半萜（1 - 4）。化合物1 - 3对Hela细胞和A375 - S2细胞表现出有前景的细胞毒性。化合物1 - 3的细胞毒性活性似乎呈剂量依赖性，当增加每种化合物的浓度时，对两种细胞系的增殖表现出更强的抑制作用。在这些化合物中，化合物2对Hela细胞或A375 - S2细胞均表现出最强的细胞毒性。
南蛇藤果实乙醇提取物对人黑色素瘤A375 - S2细胞和人宫颈癌Hela细胞的细胞毒性活性归因于其倍半萜类成分，支持其在肿瘤治疗方面的潜在治疗价值。
