目的 研究沙苑子苷A潛在的抗腫瘤作用。方法 利用計(jì)算機(jī)模擬方法，采用Discovery Studio^TM 4.0（DS）軟件反向?qū)ぐ?，初步探討沙苑子苷A潛在的抗腫瘤靶點(diǎn)，并通過(guò)CDOCKER進(jìn)行分子對(duì)接初步驗(yàn)證結(jié)果；建立體外雞胚絨毛尿囊膜（CAM）模型實(shí)驗(yàn)，血管計(jì)數(shù)法觀察沙苑子苷A（0.2、0.4、0.8 mg/mL）對(duì)CAM新生血管生成的影響。結(jié)果 反向?qū)ぐ薪Y(jié)果表明，沙苑子苷A可調(diào)控原癌基因酪氨酸蛋白激酶（ABL1）、原癌基因酪氨酸蛋白激酶（SRC）、靶點(diǎn)蛋白纖維生長(zhǎng)因子受體1（FGFR1）、纖維生長(zhǎng)因子受體（FGFR2）和轉(zhuǎn)化生長(zhǎng)因子-β（TGF-β）；分子對(duì)接結(jié)果證明，沙苑子苷A能夠調(diào)控血管生長(zhǎng)相關(guān)靶點(diǎn)；體外CAM實(shí)驗(yàn)結(jié)果發(fā)現(xiàn)，與對(duì)照組比較，沙苑子苷A能顯著抑制新生中、小血管的生成（P<0.05、0.01）。結(jié)論沙苑子苷A可能是沙苑子發(fā)揮抗腫瘤作用的主要活性成分，可能通過(guò)調(diào)控腫瘤基因的表達(dá)和抑制新生血管的生成發(fā)揮作用。

Objective To study the potential anti-tumor effect of complanatoside A. Methods Target Searching of the anti-tumor protein correlated with complanatoside A based on reverse seeking target method, and further validated the target protein through the CDOCKER molecular docking approach. Finally, to validate neovascularization of complanatoside A (0.2, 0.4 and 0.8 mg/mL), the model of chick embryo chorioallantoic membrane was established. Results DS reverse seeking target found that the protooncogene of ABL1, SRC and 3 protein of FGFR1, FGFR2 and TGF-β, which were involved in tumor angiogenesis, were regulated by complanatoside A. Moreover, complanatoside A significantly inhibited small blood and medium vessels growth in Chick Embryo CAM model (P < 0.05 or 0.01). Conclusion The results suggested that CA might be an anti-tumor active ingredient of Astragalus complanatus. The anti-tumor mechanism of CA was involving in regulating the tumors gene expression and significantly suppressing angiogenesis in Chick Embryo CAM model.

R962

國(guó)家“重大新藥創(chuàng)制”科技重大專項(xiàng)（2019ZX09735-002）