Synthesis of palmitoyl derivatives of insulin and their biological activities.
作者： Muneaki Hashimoto , Kanji Takada , Yoshiaki Kiso , Shozo Muranishi
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摘要: In order to improve the lipophilicity of peptides, bovine insulin was chosen for chemical modification using palmitic acid. The N-hydroxysuccinimide ester acid used attachment terminal amino groups, and p-methoxybenzoxycarbonyl azide protection glycine-Al terminus. We obtained two purified derivatives insulin, Bl-monopalmitoyl- Bl,B29-dipalmitoyl-insulin, which were confirmed be more lipophilic than parent on high-performance liquid chromatography (HPLC). hypoglycemic effects both products measured in rats after intravenous intramuscular injections. mono derivative active di produced a longer effect duration native injection. also shown less immunoreactive as judged by an enzyme immunoassay.
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