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目的:采用体内外抗肿瘤实验模型,筛选昆明山海棠的抗肿瘤活性部位。方法:采用离子吸附树脂柱层析法、大孔吸附树脂柱层析法,对昆明山海棠醇提物进行分离、纯化;采用MTT法测定昆明山海棠醇提物各分离部位的体外抗肿瘤活性,通过荷瘤小鼠模型考察各部位对S180实体瘤生长的影响。结果:昆明山海棠醇提物、离子树脂部位(IRP)、大孔树脂部位(MRP)均显示出较强的体内外抗肿瘤活性。IRP部位主要为生物碱类成分,其IC50低至29.90mg·L-1,IRP25,50,100mg.kg-1剂量组对S180实体瘤的抑瘤率分别为38.10%,50.60%,60.71%。MRP部位的IC50最低为98.56mg·L-1,MRP100,200,400mg·kg-1剂量组对S180实体瘤的抑瘤率分别为42.96%,53.57%,63.69%。大孔树脂不吸附的水溶性部位(WSP)未表现出明显的作用。结论:昆明山海棠具有较强的体内外抗肿瘤活性,总生物碱是其抗肿瘤作用的主要活性部位之一。
Objective: To screen the anti-tumor active site of Kunming Mountain Begonia by using in vitro and in vivo anti-tumor experimental models. METHODS: Ion adsorption resin column chromatography and macroporous adsorption resin column chromatography were used to separate and purify the ethanol extracts of Kunming Mountain Begonia. The MTT method was used to determine the in vitro anti-tumor activities of the ethanol extracts of Begonia halodendron. The tumor-bearing mouse model was used to examine the effects of various sites on the growth of S180 solid tumors. RESULTS: Ethanol extracts, IRPs and MRPs of Kunming Mountain Blast showed strong antitumor activity both in vitro and in vivo. The IRP site was mainly composed of alkaloids. The IC50 was as low as 29.90 mg·L-1. The tumor inhibition rates of the IRP25, 50, and 100 mg.kg-1 dose groups against S180 solid tumors were 38.10%, 50.60%, and 60.71%, respectively. The IC50 of the MRP site was 98.56 mg·L-1, and the inhibition rates of the MRP 100, 200, 400 mg·kg-1 dose group were 42.96%, 53.57% and 63.69%, respectively. The non-adsorbed water-soluble site (WSP) of the macroporous resin did not show a significant effect. Conclusion: Kunming Mountain Begonia has a strong anti-tumor activity in vitro and in vivo. Total alkaloids are one of the main active sites for its anti-tumor effect.