Albaconol的抗肿瘤活性及对DNA拓扑异构酶Ⅱ的影响
Study on the antitumor activity of Albaconol and its effect on DNA topoisomerase Ⅱ
查看参考文献10篇
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文摘
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目的研究地花菌提取物Albaconol的体内外抗肿瘤活性及对DNA拓扑异构酶Ⅱ(TOPO Ⅱ)活性的影响.方法以人白血病细胞株K562、人乳腺癌细胞株Bcap-37、人胃腺癌细胞株BGC-823和人非小细胞肺癌细胞株A549为模型,采用MTT法测试Albaconol对肿瘤细胞增殖的影响;以小鼠移植性肉瘤S180和小鼠移植性肝癌H22为模型,检测Albaconol静脉给药对肿瘤生长的影响;以pBR322 DNA为底物,采用琼脂糖凝胶电泳法测定Albaconol对肿瘤细胞DNA TOPO Ⅱ活性的影响.结果 Albaconol对K562、Bcap-37、BGC-823、A549的半数抑制浓度 (IC50) 分别为(2.42±1.77)、(1.88±1.41)、(1.04±0.64)、(1.18±1.10) mg·L-1;Albaconol 0.87、1.73、3.46 mg·kg-1剂量组对S180生长的抑制百分率(抑瘤率)分别为28.2%、43.2%、47.4% ;对H22的抑瘤率分别为15.6%、22.4%、37.8%;Albaconol能明显影响DNA TOPO Ⅱ的活性,表现为促进其介导的DNA解旋或断裂,并抑制其介导的DNA再连接反应.结论 Albaconol具有较强的体内、外抗肿瘤活性,DNA TOPO Ⅱ是其抗肿瘤作用的细胞内靶点之一. |
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其他语种文摘
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To study the antitumor activity of Al cell lines baconol from Albatrellus confluens and its effect on DNA topoisomerase I (TOPO H) activity. Methods The cytotoxicity of Albaconol on human leukemia K-562 , breast carcinoma Bcap-37, gastric adenocarcino-ma BGC-823 and lung adenocarcinoma A549 cell lines were determined by MTT assay and the results were ex-pressed as IC30 values. The inhibitory effect of Alba-conol on tumor growth was observed by the models of implanted sarcoma 180 (Slg0) and hepatoma 22 (H22) in mice and the results were expressed as inhibitory rate of tumor growth. The effect of Albaconol on TOPO II activity was measured by agarose gel electrophoresis using Plasmid on K562, Bcap-37, BGC-823 and A549 were (2.42 ±1. 77), (1. 88 ± 1.41) , ( 1. 04 ± 0. 64) and (1. 18 ± 1. 10) mg . L~', respectively. The in-hibitory rates of tumor growth at doses of 0. 87,1. 73 , 3.46 mg ? kg'1 Of Albaconol on Sm and H22 were 28.2%, 43.2%, 47.4% and 15.6%, 22.4%, 37. 8% .respectively. Albaconol influenced obviously DNA TOPO n activity , stimulated DNA cleavage and inhibited DNA reunion mediated by TOPO TJ. Con-clusion Albaconol exhibited significant antitumor ac-tivity in vitro and in vivo, and DNA TOPO H is one of the targets oriented by Albaconol. |
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来源
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中国药理学通报
,2004,20(11):1224-1228 【核心库】
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关键词
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Albaconol
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MTT法
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抗肿瘤
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DNA拓扑异构酶
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地址
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昆明医学院, 云南省天然药物药理重点实验室, 云南, 昆明, 650031
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中国科学院昆明植物研究所, 植物化学与西部植物资源可持续利用国家重点实验室, 云南, 昆明, 650204
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语种
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中文 |
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文献类型
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研究性论文 |
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ISSN
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1001-1978 |
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学科
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中国医学;基础医学;肿瘤学 |
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基金
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国家自然科学基金
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云南省自然科学基金重点项目
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文献收藏号
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CSCD:1795863
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