维A酸衍生物抗癌药物的研究进展

史得发,,唐建斌,隋梅花,王新平*,申有青*

中国药学杂志 ›› 2013, Vol. 48 ›› Issue (5) : 321-325.

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中国药学杂志
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中国药学杂志 ›› 2013, Vol. 48 ›› Issue (5) : 321-325. DOI: 10.11669/cpj.2013.05.001
综 述

维A酸衍生物抗癌药物的研究进展

  • 史得发1,2,唐建斌2,隋梅花2,王新平1*,申有青2*
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摘要

目的 维A酸（tretinoin）有良好的肿瘤抑制能力,但是它本身毒性大、水溶性差,限制了其在临床上的进一步应用。通过对其羧基修饰,可进一步提高其抗肿瘤能力、增加水溶性等。方法 通过分析文献中具有抗肿瘤活性的维A酸及其衍生物的研究结果,总结维A酸衍生物改性的规律,为设计高活性、易临床应用的维A酸类抗肿瘤药物提供指导。结果与结论 维A酸与羟基苯胺形成的酰胺或酯,或与其他药物分子形成的键合物,具有更高的抗肿瘤药效,其IC50在微摩尔水平,而维A酸与组蛋白去乙酰基酶抑制剂的键合物的IC50达到了纳摩尔水平,但这些衍生物的水溶性问题仍没有解决。通过键合负载的方法可有效提高其水溶性,并可提高药效。因此,键合负载维A酸可能是提高其药效和水溶性的有效方法。

关键词

维A酸 / 衍生物 / 抗肿瘤

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史得发,,唐建斌,隋梅花,王新平*,申有青*. 维A酸衍生物抗癌药物的研究进展[J]. 中国药学杂志, 2013, 48(5): 321-325 https://doi.org/10.11669/cpj.2013.05.001
中图分类号： R979.1   

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基金

国家自然科学基金资助项目(20974096);国家“973 计划”(2009CB526403);长江学者和创新团队发展计划

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