8-氯腺苷抗肿瘤作用研究

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8-氯腺苷抗肿瘤作用研究

张礼和^*, 方家椿

1. 北京医科大学天然药物及仿生药物国家重点实验室, 北京 100083;
2. 北京市肿瘤研究所, 北京 100043

收稿日期:1996-12-03 修回日期:1997-01-16 出版日期:1997-03-15 发布日期:1997-03-15
通讯作者: 张礼和*

Studies on the Antitumour Activities of 8-Chloroadenosine

Li-He Zhang^*, Jia-Chun Fang

1. National Key Laboratory of Natural and Biomimetic Drugs, Beijing Medical University, Beijing 100083;
2. Beijing Institute for Cancer Research, Beijing 100043

Received:1996-12-03 Revised:1997-01-16 Online:1997-03-15 Published:1997-03-15
Contact: Li-He Zhang*

摘要/Abstract

摘要： (Sp)-8-氯腺苷3',5'环磷酸辛酯(OCC)是8-氯腺苷3',5'环磷酸的新衍生物, 对人白血病细胞HL-60有很强的抑制作用和诱导分化作用。用细胞流式光度术发现OCC阻断HL-60细胞周期于G1期。OCC对HL-60细胞DNA合成有显著抑制作用, 但不影响RNA和蛋白质合成。OCC能激活HL-60细胞浆中蛋白激酶A。8-氯腺苷是OCC的活性代谢产物, 能在体外和体内实验中明显抑制肿瘤的生长。8-氯腺苷也能诱导人胃癌MGc80-3细胞分化和人T淋巴母细胞MOTL-4的凋亡。本文讨论了8-氯腺苷抗肿瘤作用的机理。

关键词: (Sp)-8-氯腺苷3',5'-环磷酸辛酯(OCC), 8-氯腺苷, 抗肿瘤作用

Abstract: (Sp)-Octyl-8-chloroadenosine-3',5'-cyclophosphate (OCC), a newly synthesized 8-Cl-c-AMP derivative, strongly induced inhibition and differentiation in human leukemia HL 60 cells. In flow cytometry, OCC brought about a block at the G1 phase of HL-60 cell cycle. OCC inhibited strongly the synthesis of DNA without affecting the synthesis of RNA and protein in HL-60 cells and also activated the c-AMP dependent protein kinase in the cytosol of HL-60 cells. 8-Chloroadenosine is the active metabolite of OCC and inhibited significantly the growth of tumour in vitro and in vivo tests. 8-Chloroadenosine can induce differentiation of gastric mucoid adenocarcinoma cell line MGc80-3 and induce apoptosis in the MOLT-4 cells. The mechanism of the antitumour effects of 8 chloroadenosine was discussed.

Key words: (Sp)-Octyl-8-chloroadenosine-3',5'-cyclophosphate (OCC), 8-Chloroadeno- sine, Antitumour activities

Supporting:

张礼和^*, 方家椿. 8-氯腺苷抗肿瘤作用研究[J]. .

Li-He Zhang^*, Jia-Chun Fang . Studies on the Antitumour Activities of 8-Chloroadenosine[J]. .

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