Watkins J B, Wirthwein D P, Sanders R A
Medical Sciences Program, Indiana University School of Medicine, Bloomington 47405.
Drug Metab Dispos. 1991 May-Jun;19(3):708-13.
To assess the biotransformational capability of ocular tissues in the rabbit, representative phase II enzymes were assayed in five tissues from the eye, and in the liver, kidney, and intestine. Within the eye, the iris/ciliary body exhibited the highest glutathione S-transferase activity, whereas the cornea possessed the highest specific activities for N-acetyl-, sulfo-, and UDP-glucuronosyl-transferases. Cornea, iris/ciliary body, choroid, and retina exhibited significant activities of p-aminobenzoic acid N-acetyltransferase, 2-naphthol sulfotransferase, and 1-chloro-2,4-dinitrobenzene glutathione S-transferase. Despite its size and protein content, lens displayed little or no biotransformational activity. Only the iris/ciliary body conjugated sulfobromophthalein with glutathione. UDP-glucuronsyltransferase activity varied depending on tested substrates and tissues. When compared to liver, kidney, or intestine, N-acetyltransferase activity in the iris/ciliary body nearly matched the rate measured in kidney, glutathione S-transferase activity in cornea and iris/ciliary body was nearly 70 and 89%, respectively, of the rate in intestine, and corneal sulfotransferase activity was greater than that in kidney. These data suggest that biotransformation pathways are present in the eye, and particularly in ocular tissues having adequate blood supply or interfacing with the external environment.
为评估兔眼组织的生物转化能力,对兔眼的五种组织以及肝脏、肾脏和肠道中的代表性II相酶进行了测定。在眼内,虹膜/睫状体表现出最高的谷胱甘肽S-转移酶活性,而角膜对N-乙酰基转移酶、磺基转移酶和UDP-葡萄糖醛酸基转移酶具有最高的比活性。角膜、虹膜/睫状体、脉络膜和视网膜表现出对氨基苯甲酸N-乙酰基转移酶、2-萘酚磺基转移酶和1-氯-2,4-二硝基苯谷胱甘肽S-转移酶的显著活性。尽管晶状体体积大且蛋白质含量高,但几乎没有生物转化活性。只有虹膜/睫状体能使磺溴酞与谷胱甘肽结合。UDP-葡萄糖醛酸基转移酶的活性因测试底物和组织而异。与肝脏、肾脏或肠道相比,虹膜/睫状体中的N-乙酰基转移酶活性几乎与肾脏中的测定速率相当,角膜和虹膜/睫状体中的谷胱甘肽S-转移酶活性分别约为肠道中速率的70%和89%,且角膜磺基转移酶活性大于肾脏中的活性。这些数据表明,生物转化途径存在于眼中,尤其是在血液供应充足或与外部环境接触的眼组织中。