ADECHLORIN, A NEW ADENOSINE DEAMINASE INHIBITOR CONTAINING CHLORINE PRODUCTION, ISOLATION AND PROPERTIES

Adechlorin exhibiting a potent inhibitory activity against calf intestinal adenosine deaminase was isolated from the cultured broth of Actinomadura sp. OMR-37. The molecular formula was C11H15N4O4Cl. The aglycone of adechorin was identical with that of the known adenosine deaminase inhibitors coform...

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Bibliographic Details
Published in:Journal of antibiotics 1985, Vol.38(8), pp.1008-1015
Main Authors: OMURA, SATOSHI, IMAMURA, NOBUTAKA, KUGA, HIROSHI, ISHIKAWA, HIDEYO, YAMAZAKI, YUKIKO, OKANO, KEIKO, KIMURA, KEIKO, TAKAHASHI, YOKO, TANAKA, HARUO
Format: Article
Language:English
Subjects:
Actinomadura
Actinomycetales - classification
Actinomycetales - metabolism
Adenosine Deaminase Inhibitors
Animals
Chemical Phenomena
Chemistry
Chlorine - analysis
Kinetics
Magnetic Resonance Spectroscopy
Mice
Nucleoside Deaminases - antagonists & inhibitors
Nucleosides - isolation & purification
Nucleosides - pharmacology
Pentostatin - analogs & derivatives
Vidarabine - pharmacology
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Summary:Adechlorin exhibiting a potent inhibitory activity against calf intestinal adenosine deaminase was isolated from the cultured broth of Actinomadura sp. OMR-37. The molecular formula was C11H15N4O4Cl. The aglycone of adechorin was identical with that of the known adenosine deaminase inhibitors coformycin and 2'-deoxycoformycin. Adechlorin did not exhibit inhibitory activity against various bacteria and fungi at 1.0 mg/ml. The Ki values for adechlorin, coformycin and 2'-deoxycoformycin against adenosine deaminase were determined to be 5.3×10-10 M, 2.1×10-10 M and 7.6×10-11 M, respectively. Adechlorin as well as coformycin and 2'-deoxycoformycin enhanced the antiviral activity of Ara-A. The acute toxicity of adechlorin in mice was less than those of coformycin and 2'-deoxycoformycin.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.38.1008