Effects of protease inhibitors on the absorption of phenol red and fluorescein isothiocyanate dextrans from the rat intestine
Effects of protease inhibitors on the absorption of phenol red and fluorescein isothiocyanate dextrans from the rat intestine
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DOI：
10.1021/js9505051
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发表时间：
1996-08-01
影响因子：
3.8
通讯作者：
Muranishi, S
中科院分区：
文献类型：
--
作者：
Gotoh, S;Nakamura, R;Muranishi, S
研究了抑肽酶、杆菌肽和大豆胰蛋白酶抑制剂对酚红（PR）和异硫氰酸荧光素葡聚糖（FD）在大鼠小肠和大肠吸收的促进作用。在这些蛋白酶抑制剂中，只有杆菌肽能增强PR和FD在大鼠小肠和大肠中的吸收。因此，我们认为杆菌肽不仅具有蛋白酶抑制作用，而且具有吸收增强作用。我们研究了各种蛋白酶抑制剂对肠粘膜毒性的影响，通过测量伊文思蓝（EB）从体循环中的泄漏。虽然在杆菌肽存在下EB的泄漏显著增加，但其显著低于用作阳性对照的聚氧乙烯9-月桂基醚（BL-9）的情况。因此，杆菌肽可能是一个很好的模型佐剂，用于改善肠道吸收不良的药物，因为没有引起严重的肠粘膜损伤，如在BL-9的情况下看到的。
The absorption enhancement effects of three types of protease inhibitors, aprotinin, bacitracin, and soybean trypsin inhibitor, on the small and large intestinal absorption of phenol red (PR) and fluorescein isothiocyanate dextrans (FDs) were examined in rats. Of these protease inhibitors, only bacitracin enhanced the absorption of PR and FDs from the rat small and large intestine. Thus, we suggest that bacitracin has not only a protease-inhibitory but also an absorption-enhancing capability. We examined the effects of various protease inhibitors on intestinal mucosal toxicity by measuring the leakage of Evans blue (EB) from the systemic circulation. Although there was a significant increase in the leakage of EB in the presence of bacitracin, it was considerably less than that in the case of polyoxyethylene 9-lauryl ether (BL-9), which was used as a positive control. Therefore, bacitracin may be a good model adjuvant for improving the intestinal absorption of poorly absorbable drugs because a did not cause serious intestinal mucosal damage, as seen in the case of BL-9.