Inhibitory activity of kaurane-type diterpenes isolated from Acanthopanax senticosus Harms on protein tyrosine phosphatase 1B / 中国药学杂志

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 PTP1 B inhibitory activity were obtained by bio-assay-guided fractionation. RESULTS Nine compounds were identified as 17-isobutyryloxy-16αH-kauran-19-oic acid(1), 17-hydrox-y-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 PTP1 B with IC50 values ranging from (5.6 ± 0.8) to (22.8 ± 1.2) μmol · L-1.