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Studies on the Antitumour Activities of 8-Chloroadenosine

Li-He Zhang*, Jia-Chun Fang   

  1. 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*

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

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