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Synthesis and anti-tumor activity of NO-donating derivatives of gambogic acid
  • ISSN号:2095-6975
  • 期刊名称:《中国天然药物:英文版》
  • 时间:0
  • 分类:R284.3[医药卫生—中药学;医药卫生—中医学] R965[医药卫生—药理学;医药卫生—药学]
  • 作者机构:[1]Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China, [2]Department of Oncology, General Hospital of People's Liberation Army, Lanzhou 730050, China, [3]Key Laboratory of Carcinogenesis and Intervention of Jiangsu Province, China Pharmaceutical University, Nanjing 210009, China
  • 相关基金:This project was supported by the National Natural Science Foundation of China (Nos. 30873157, 21072231).
中文摘要:

试图从 gambogic 酸和它的衍生物发现有势力 apoptosis inducer。gambogic 酸的八新不捐赠的衍生物作为潜在的反肿瘤被综合的方法在 HT-29, Bel-7402, BGC-823,和 A549 房间线上带混合物和他们的禁止的活动被 MTT 试金在 vitro 评估。在这些混合物之中的结果, 4 通过 MTT 房间试金,词法变化的观察,和 Annexin-V/PI 作为 SKOV3 房间 apoptosis inducer 与在 gambogic 酸一半的 C35 的一个氢氧根组一起被识别两倍染色的试金。在导致 apoptosis 和力量的结论化合物 4 显示出的重要效果为新 anticancer 药的发现用作潜在的铅混合物。

英文摘要:

AIM: To find a potent apoptosis inducer from gambogic acid and its derivatives. METHODS: Eight new NO-donating derivatives of gambogic acid were synthesized as potential anti-tumor lead compounds and their inhibitory activity on the HT-29, Bel-7402, BGC-823, and A549 cell lines were evaluated in vitro by the MTF assay. RESULTS: Among these compounds, 4 with a hydroxyl group at C35 of the gambogic acid moiety was identified as a SKOV3 cell apoptosis inducer through the MTF cell assay, observations of morphological changes, and Annexin-V/PI double staining assay. CONCLUSION: Compound 4 showed significant effects in inducing apoptosis and might serve as a potential lead compound for the discovery of new anticancer drugs.

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期刊信息
  • 《中国天然药物:英文版》
  • 北大核心期刊(2008版)
  • 主管单位:中华人民共和国教育部
  • 主办单位:中国药科大学 中国药学会
  • 主编:吴晓明
  • 地址:南京童家巷24号中国药科大学2号信箱
  • 邮编:210009
  • 邮箱:cpucjnm@163.com
  • 电话:025-83271565 83271568
  • 国际标准刊号:ISSN:2095-6975
  • 国内统一刊号:ISSN:32-1845/R
  • 邮发代号:28-306
  • 获奖情况:
  • 国内外数据库收录:
  • 美国国际药学文摘,美国化学文摘(网络版),波兰哥白尼索引,美国生物医学检索系统,美国科学引文索引(扩展库),美国生物科学数据库,中国中国科技核心期刊,中国北大核心期刊(2008版)
  • 被引量:6564