斑蝥素类似物对黄嘌呤氧化酶的作用。

The effects of cantharidin analogues on xanthine oxidase.

作者信息

Tsauer W, Lin J G, Lin P Y, Hsu F L, Chiang H C

机构信息

Research Institute of Chinese Medicine, China Medical College, Taichung, Taiwan, R.O.C.

出版信息

Anticancer Res. 1997 May-Jun;17(3C):2095-8.

PMID:9216670

Abstract

Norcantharidin[3], the demethylated product of cantharidin[1] has been used for the treatment of hepatoma, carcinomas of esophagus and gastric cardia, leukopenia and hepatitis. Since the enzyme xanthine oxidase is involved in the diseases mentioned above, and the reactive oxygen species produced by the enzyme induces DNA damage and oxidative damage of tissues, fourteen cantharidin analogues and cantharidimide derivatives were tested for their effects on xanthine oxidase. The results showed that these compounds, listed in Figure 1, displayed very weak inhibitory effects on xanthine oxidase. Contrary to expectation, disodium cantharidate [2], Norcantharidin [3], dehydronorcantharidin [4], disodium dehydronorcantharidate [5], N-(2-pyridyl) cantharidimide [12], N-(3pyridyl) cantharidimide [13] and N-(4-pyridyl) cantharidimide [14] showed a slight stimulating effect on xanthine oxidase at several concentrations.

摘要

去甲斑蝥素[3]是斑蝥素[1]的去甲基化产物，已被用于治疗肝癌、食管癌和贲门癌、白细胞减少症及肝炎。由于黄嘌呤氧化酶与上述疾病相关，且该酶产生的活性氧会诱导DNA损伤和组织氧化损伤，因此对14种斑蝥素类似物和斑蝥酰亚胺衍生物进行了黄嘌呤氧化酶作用测试。结果表明，图1中列出的这些化合物对黄嘌呤氧化酶的抑制作用非常微弱。与预期相反，斑蝥酸钠[2]、去甲斑蝥素[3]、去氢去甲斑蝥素[4]、去氢斑蝥酸钠[5]、N-(2-吡啶基)斑蝥酰亚胺[12]、N-(3-吡啶基)斑蝥酰亚胺[13]和N-(4-吡啶基)斑蝥酰亚胺[14]在几种浓度下对黄嘌呤氧化酶表现出轻微的刺激作用。