通过羧基修饰提高壳寡糖（COS）的ACE抑制活性。
Improvement of ACE inhibitory activity of chitooligosaccharides (COS) by carboxyl modification.
作者信息
Huang Ronghua, Mendis Eresha, Kim Se-Kwon
机构信息
Department of Chemistry, Pukyong National University, Busan 608-737, South Korea.
出版信息
Bioorg Med Chem. 2005 Jun 1;13(11):3649-55. doi: 10.1016/j.bmc.2005.03.034.
In the present research, chitooligosaccharides (COS) were carboxylated with -COCH(2)CH(2)COO(-) groups to obtain specific structural features similar to Captopril. Angiotensin I converting enzyme (ACE) inhibitory activity of carboxylated COS was studied and observed to enhance its activity with increased substitution degree. Further, Lineweaver-Burk plot analysis revealed that inhibition was competitive via obligatory binding site of the enzyme. This was accompanied with substitution of positively charged quarternized amino groups to COS with different substitution degrees, in which negative impact on ACE inhibition was observed.
在本研究中，壳寡糖（COS）用-COCH(2)CH(2)COO(-)基团进行羧化，以获得与卡托普利相似的特定结构特征。对羧化壳寡糖的血管紧张素I转换酶（ACE）抑制活性进行了研究，发现随着取代度的增加其活性增强。此外，Lineweaver-Burk图分析表明，抑制作用是通过酶的必需结合位点竞争性的。这伴随着不同取代度的带正电荷的季铵化氨基被取代到壳寡糖上，其中观察到对ACE抑制有负面影响。
Zotero 插件