| 引用本文: | 李彦魁,安荣,吕娟.熊果酸与白藜芦醇缀合物的合成及其抗肿瘤活性评价[J].中国现代应用药学,2021,38(7):790-798. |
| LI Yankui,AN Rong,LYU Juan.Synthesis and Preliminary Anti-tumor Activity Evaluation of Ursolic Acid-resveratrol Conjugates[J].Chin J Mod Appl Pharm(中国现代应用药学),2021,38(7):790-798. |
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| 摘要: |
| 目的 设计、合成熊果酸与白藜芦醇缀合物，并对其抗肿瘤活性进行研究。方法 以熊果酸为原料，通过酯化反应合成了熊果酸-白藜芦醇缀合物，并采用MTT法评价缀合物的体外抗肿瘤活性。结果 合成了12个熊果酸-白藜芦醇缀合物，其结构经1H-NMR和MS进行确证。初步的生物活性结果表明，目标缀合物对乳腺癌细胞MCF-7和MDA-MB-231均有抑制活性，其中缀合物13b-c和15b-c对MCF-7的抑制活性强于熊果酸、白藜芦醇及阳性药物他莫昔芬。此外，目标缀合物对正常的MCF-10A细胞没有毒性。结论 熊果酸结构中引入白藜芦醇结构单元可提高其抗肿瘤活性。 |
| 关键词: 熊果酸-白藜芦醇缀合物 合成 抗肿瘤活性 |
| DOI：10.13748/j.cnki.issn1007-7693.2021.07.004 |
| 分类号:R284.3 |
| 基金项目:陕西省教育厅专项科学研究项目（17JK0197） |
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| Synthesis and Preliminary Anti-tumor Activity Evaluation of Ursolic Acid-resveratrol Conjugates |
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LI Yankui, AN Rong, LYU Juan
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School of Medical Technology, Shaanxi University of Chinese Medicine, Xi'an 712046, China
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| Abstract: |
| OBJECTIVE To design and synthesize ursolic acid-resveratrol conjugates and investigate their anti-cancer activities. METHODS Ursolic acid-resveratrol conjugates were synthesized from ursolic acid by esterification reaction, and the in vitro antitumor activity of target conjugates was assessed by MTT assay. RESULTS Twelve ursolic acid-resveratrol conjugates were synthesized, and structures were characterized by 1H-NMR and MS analysis. The preliminary biological results showed that these conjugates displayed inhibitory activity on both MCF-7 and MDA-MB-231. Specifically, the inhibitory activity of conjugate 13b-c and 15b-c on MCF-7 was stronger than that of ursolic acid, resveratrol and the positive drug of tamoxifen. Additionally, all conjugates were nontoxic to normal MCF-10A cells. CONCLUSION The introduction of resveratrol unit into the structure of ursolic acid can enhance its anti-tumor activity. |
| Key words: ursolic acid-resveratrol conjugates synthesis anti-tumor activity |
