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出 处:《中国天然药物》2007年第2期115-119,共5页
摘 要:目的:合成新型小肽偶联物,寻找具有抗肿瘤活性及肝靶向性的新化合物。方法:以齐墩果酸和胆酸为母核,分别与活性小肽偶联,考察此类偶联物对T淋巴细胞增殖的影响。结果与结论:合成了8个新型小肽偶联物(Z1~Z8),其结构经IR,1HNMR和MS确证。初步药理结果表明,目标物Z1、Z2、Z4、Z8可不同程度地促进T淋巴细胞增殖,与对照药酪丝亮肽相比有显著性差异,其中化合物Z4最优,具有进一步研究的价值。AIM: To synthesize novel small poptide coupling derivatives with high anti-cancer activity and liver-targeting pmporty. METHODS: Oleanolic acid and cholic acid were coupled with active small poptides; the activity of the coupling compounds to induce T lymph cell proliferation was studied. RESULTS AND CONCLUSION: Eight small poptide coupling compounds(Z1-Z8) were obtained and their structures were confirmed by IR, ^1H NMR and MS. Compounds 1, 2,4 and 8 showed higher activity than the control YSL in inducing lymph cell proliferation. Compound Z4 was the most active one deserving further investigation.
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