Synthesis of water soluble pentacyclic dihydroxyterpene carboxylic acid derivatives coupled amino acids and their inhibition activities on α-glucosidase.,Bioorganic Chemistry

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Synthesis of water soluble pentacyclic dihydroxyterpene carboxylic acid derivatives coupled amino acids and their inhibition activities on α-glucosidase.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2019-02-02 , DOI: 10.1016/j.bioorg.2019.02.001
Zhen Zeng ₁ , Xiaoli Yin ₂ , Xueyuan Wang ₁ , Wuying Yang ₁ , Xiaoqin Liu ₁ , Yanping Hong ₁

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Twenty maslinic acid and corosolic acid derivatives were obtained by coupling with l-amino acids at C-28 position. The α-glucosidase inhibitory activities of the present compounds were evaluated in vitro. Results reveal that some of the derivatives exhibit a better α-glucosidase inhibitory activity than that of acarbose in the test conditions of ethanol-water solution and DMSO. It is worth noting that maslinic acid and corosolic acid derivatives coupled aspartic acid (9f: IC50 = 382 μm and 10f: IC50 = 364 μm, respectively) have the best water solubility and thus presented higher inhibitory activity than that of acarbose (IC50 = 484 μm). Unfortunately, all of the derivatives possess lower inhibitory properties of α-glucosidase than those of the parent compounds in the measurement system of DMSO solution, even if the derivatives exhibit better water solubility than that of the parent compounds.

中文翻译：

水溶性五环二羟基萜烯羧酸衍生物与氨基酸的合成及其对α-葡萄糖苷酶的抑制活性。

通过在C-28位与1-氨基酸偶联获得二十个山梨酸和熊果酸衍生物。在体外评价了本发明化合物的α-葡萄糖苷酶抑制活性。结果表明，在乙醇水溶液和DMSO的测试条件下，某些衍生物表现出比阿卡波糖更好的α-葡萄糖苷酶抑制活性。值得注意的是，山梨酸和熊果酸衍生物偶联天冬氨酸（分别为9f：IC50 = 382μm和10f：IC50 = 364μm）具有最佳的水溶性，因此具有比阿卡波糖更高的抑制活性（IC50 = 484）微米）。不幸的是，在DMSO溶液的测量系统中，所有衍生物都具有比母体化合物更低的α-葡萄糖苷酶抑制特性，

更新日期：2019-02-02

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