Prabhakaran K, Harris E B, Kirchheimer W F
J Bacteriol. 1969 Nov;100(2):935-8. doi: 10.1128/jb.100.2.935-938.1969.
Previous results had shown that the human leprosy bacilli possess a phenoloxidase, which, when compared with the enzyme from mammalian and plant sources, seemed unique in the range of substrates utilized and in the nature of the products formed. The effect of several inhibitors on the enzyme in Mycobacterium leprae was tested. Compounds which bind copper were found to be more effective than substrate analogues. Diethyldithiocarbamate penetrated the bacillus and completely suppressed its phenolase activity. Diasone (a derivative of diaminodiphenylsulfone used in the treatment of leprosy) proved to be a potent inhibitor of phenoloxidase of mammalian and plant origin. However, it was less efficient in the case of M. leprae. A biochemical peculiarity of M. leprae was observed in its ability to metabolize mimosine and penicillamine. These compounds produced total inhibition of tyrosinase in melanoma extract and of mushroom tyrosinase. Nontoxic inhibitors of phenoloxidase in the leprosy bacilli may be of value in developing a rational approach to chemotherapy of the disease.
先前的研究结果表明，人类麻风杆菌含有一种酚氧化酶，与来自哺乳动物和植物的该酶相比，其在底物利用范围和产物性质方面似乎具有独特性。测试了几种抑制剂对麻风分枝杆菌中该酶的作用。发现与铜结合的化合物比底物类似物更有效。二乙基二硫代氨基甲酸盐可穿透杆菌并完全抑制其酚酶活性。二氨二苯砜（一种用于治疗麻风病的二氨二苯砜衍生物）被证明是哺乳动物和植物来源酚氧化酶的有效抑制剂。然而，在麻风分枝杆菌的情况下，其效果较差。观察到麻风分枝杆菌在代谢含羞草碱和青霉胺方面的生化特性。这些化合物能完全抑制黑色素瘤提取物中的酪氨酸酶和蘑菇酪氨酸酶。麻风杆菌中酚氧化酶的无毒抑制剂可能对开发合理的麻风病化疗方法具有价值。
