白桦脂酸衍生物：一类新型的α-葡萄糖苷酶抑制剂及对 LPS 刺激的 RAW264.7 巨噬细胞一氧化氮生成的抑制作用。
Betulinic acid derivatives: a new class of α-glucosidase inhibitors and LPS-stimulated nitric oxide production inhibition on mouse macrophage RAW 264.7 cells.
机构信息
a Natural Products Chemistry Division , Indian Institute of Chemical Technology , Hyderabad , India.
b Department of Animal Biology , University of Hyderabad , Hyderabad , India.
出版信息
Nat Prod Res. 2019 Sep;33(18):2618-2622. doi: 10.1080/14786419.2018.1462182. Epub 2018 Apr 23.
Chemical manipulation studies were conducted on betulinic acid (), twenty-one new rationally designed analogues of 1 with modifications at C-28 were synthesized for their evaluation of inhibitory effects on α-glucosidase and LPS-stimulated nitric oxide production in mouse macrophage RAW 264.7 cells. Compound (IC = 5.4 μM) exhibited an almost 1.4-fold increase in α-glucosidase inhibitory activity on yeast α-glucosidase while analogues (IC 16.4 μM) and (IC 16.6 μM) exhibited a 2-fold enhanced inhibitory activity on NO-production than betulinic acid.
进行了白桦脂酸（）的化学操作研究，合成了 21 种新型的 1 位 C-28 位结构修饰的理性设计类似物，以评估其对α-葡萄糖苷酶的抑制作用和 LPS 刺激的 RAW 264.7 细胞中一氧化氮生成的抑制作用。化合物（IC = 5.4 μM）对酵母α-葡萄糖苷酶的α-葡萄糖苷酶抑制活性增加了近 1.4 倍，而类似物（IC 16.4 μM）和（IC 16.6 μM）对 NO 生成的抑制活性比白桦脂酸增加了 2 倍。
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