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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-16αHkauran-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。
Objective To study the chemical constituents and inhibit the activity of protein tyrosine phosphatase 1B (PTP1B) in Acanthopanax senticosus Harms. Methods The kasugaminated diterpene with protein tyrosine phosphatase 1B inhibitory activity was isolated by bioactive guided separation method. 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-16αHkauran-19 enoic acid (4), ent-kaur-16-en-19-oic acid (kaurenoic acid (5), 4-epirulopezol 17-isovaleryloxy-ent-kauran-19-oic acid (8) and 16α-hydroxy- 17-isovaleryloxyent- kauran- 19-oic acid (9) .Conclusion Compounds 1 to 3, 5 and 6 are isolated from this plant for the first time.Compounds 1, 3, 6 and 8 have inhibitory effects on the activity of PTP1B with IC50 ranging from (5.6 ± 0.8) to (22.8 ± 1.2) μmol·L-1.