脱氯嘌呤，一种含氯的新型腺苷脱氨酶抑制剂：制备、分离及性质

Adechlorin, a new adenosine deaminase inhibitor containing chlorine production, isolation and properties.

作者信息

Omura S, Imamura N, Kuga H, Ishikawa H, Yamazaki Y, Okano K, Kimura K, Takahashi Y, Tanaka H

出版信息

J Antibiot (Tokyo). 1985 Aug;38(8):1008-15. doi: 10.7164/antibiotics.38.1008.

DOI:10.7164/antibiotics.38.1008

Abstract

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 adechlorin 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 X 10(-10) M, 2.1 X 10(-10) M and 7.6 X 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.

摘要

从马杜拉放线菌OMR - 37的培养液中分离出了对小牛肠腺苷脱氨酶具有强效抑制活性的脱氯菌素。其分子式为C11H15N4O4Cl。脱氯菌素的苷元与已知的腺苷脱氨酶抑制剂助间型霉素和2'-脱氧助间型霉素的苷元相同。脱氯菌素在1.0 mg/ml时对多种细菌和真菌没有抑制活性。脱氯菌素、助间型霉素和2'-脱氧助间型霉素对腺苷脱氨酶的Ki值分别测定为5.3×10(-10) M、2.1×10(-10) M和7.6×10(-11) M。脱氯菌素以及助间型霉素和2'-脱氧助间型霉素增强了阿糖腺苷的抗病毒活性。脱氯菌素对小鼠的急性毒性小于助间型霉素和2'-脱氧助间型霉素。