Takano M, Tomita Y, Katsura T, Yasuhara M, Inui K, Hori R
Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Kyoto University, Japan.
Biochem Pharmacol. 1994 Mar 15;47(6):1089-90. doi: 10.1016/0006-2952(94)90421-9.
The effect of papain treatment on bestatin uptake by rabbit intestinal brush-border membrane vesicles (BBMVs) was studied. Papain treatment of BBMVs effectively diminished aminopeptidase activity but not bestatin uptake by a H+/dipeptide cotransporter. Bestatin uptake by BBMVs was composed of two saturable components, and after papain treatment the high-affinity component disappeared while the low-affinity component was retained. These findings suggest that high- and low-affinity components represent bestatin binding to aminopeptidase and the true uptake by the H+/dipeptide cotransporter, respectively.
研究了木瓜蛋白酶处理对兔小肠刷状缘膜囊泡(BBMVs)摄取贝司他汀的影响。用木瓜蛋白酶处理BBMVs可有效降低氨肽酶活性,但不会影响H⁺/二肽共转运体对贝司他汀的摄取。BBMVs对贝司他汀的摄取由两个可饱和成分组成,木瓜蛋白酶处理后,高亲和力成分消失,而低亲和力成分保留。这些发现表明,高亲和力和低亲和力成分分别代表贝司他汀与氨肽酶的结合以及H⁺/二肽共转运体的真正摄取。