目的研究刺五加(Acanthopanax senticosus Harms)的化学成分及其抑制蛋白酪氨酸磷酸酶1B(PTP1B)活性。方法利用生物活性导向分离方法分离得到具有蛋白酪氨酸磷酸酶1B抑制活性的贝壳杉烷型二萜类化合物。结果9个化合物分别鉴定为17-isobutyryloxy-16αH-kauran-19-oic acid(1),17-hydroxy-16αH-kauran-19-oic acid(2),17-acetoxy-18-isobutyryloxy-16αH-kauran-19-oic acid(3),ent-kaur-16-en-19-oic acid(4),ent-kaur-16-en-19-oic acid(kaurenoic acid(5),4-epirulopezol(6),16α-hydroxy-ent-kauran-19-oic acid(7),16αH,17-isovaleryloxy-ent-kauran-19-oic acid(8)和16α-hydroxy-17-isovaleryloxyent-kauran-19-oic acid(9)。结论化合物1~3、5和6为首次从该植物中分离得到。化合物1、3~6和8,对PTP1B活性具有抑制作用,其IC50值在(5.6±0.8)到(22.8±1.2)μmol·L-1之间。
Abstract
OBJECTIVE To study the constituents isolated from Acanthopanax senticosus Harms and their inhibitory activity on protein tyrosine phosphatase 1B(PTP1B). METHODS Kaurane-type diterpenes with PTP1B inhibitory activity were obtained by bioassay-guided fractionation. RESULTS Nine compounds were identified as 17-isobutyryloxy-16αH-kauran-19-oic acid(1),17-hydroxy-16αH-kauran-19-oic acid(2),17-acetoxy-18-isobutyryloxy-16αH-kauran-19-oic acid(3),ent-kaur-16-en-19-oic acid(4),ent-kaur-16-en-19-oic acid(kaurenoic acid 5),4-epirulopezol(6),16α-hydroxy-ent-kauran-19-oic acid(7),16αH,17-isovaleryloxy-ent-kauran-19-oic acid(8) and 16α-hydroxy-17-isovaleryloxyent-kauran-19-oic acid(9). CONCLUSION Compounds 1-3,5 and 6 are obtained from the plant for the first time. Compounds 1,3-6 and 8 exhibite inhibitory effects on PTP1B with IC50 values ranging from (5.6±0.8) to (22.8±1.2) μmol·L-1.
关键词
刺五加 /
蛋白酪氨酸磷酸酯酶1B /
贝壳杉烷型二萜类化合物 /
2型糖尿病
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Key words
Acanthopanax senticosus Harms /
PTP1B /
kaurane-type diterpenes /
type 2 diabetes
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中图分类号：
R284
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参考文献
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脚注
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基金
吉林省科技发展计划资助项目(YYZX201240)
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