Kikuchi Hinako, Nakamura Yuki, Inoue Chika, Nojiri Sayaka, Koita Miho, Kojima Minori, Koyama Hiroki, Miki Ryotaro, Seki Toshinobu, Egawa Yuya
Faculty of Pharmacy and Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado, Saitama 350-0295, Japan.
Mol Pharm. 2021 Nov 1;18(11):4224-4230. doi: 10.1021/acs.molpharmaceut.1c00760. Epub 2021 Oct 8.
-Boronophenylmethoxycarbonyl (BPmoc) is a protecting group for amines that is removable by treatment with hydrogen peroxide (HO). We prepared BPmoc-modified insulin (BPmoc-Ins) and subcutaneously injected the formulation into diabetic rats. The results demonstrated that BPmoc effectively sealed the blood glucose (Glc)-lowering effects of Ins. Conversely, coinjection of BPmoc-Ins and Glc oxidase (GOx) resulted in reduced blood Glc levels, indicating that Ins was generated from BPmoc-Ins through the following reactions: oxidation of endogenous Glc by GOx; production of HO accompanied by Glc oxidation; removal of BPmoc residues by HO. These results show the potential of BPmoc-Ins for a Glc-responsive Ins release system.
-硼苯基甲氧基羰基（BPmoc）是一种胺类保护基团，可通过用过氧化氢（HO）处理将其除去。我们制备了BPmoc修饰的胰岛素（BPmoc-Ins），并将该制剂皮下注射到糖尿病大鼠体内。结果表明，BPmoc有效地封闭了胰岛素降低血糖（Glc）的作用。相反，同时注射BPmoc-Ins和葡萄糖氧化酶（GOx）会导致血糖水平降低，这表明通过以下反应从BPmoc-Ins生成了胰岛素：GOx将内源性葡萄糖氧化；葡萄糖氧化伴随产生HO；HO去除BPmoc残基。这些结果表明BPmoc-Ins在葡萄糖响应性胰岛素释放系统方面具有潜力。
