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https://dspace.ctu.edu.vn/jspui/handle/123456789/4217
Title: | Protein Tyrosine Phosphatase 1B Inhibitors from the Stems of Akebia quinata |
Authors: | An, Jin-Pyo Hà, Thị Kim Quy Oh, Won Keun Cho, Tae Oh Kim, Jinwoong |
Keywords: | Akebiaquinata Terpenes Proteintyrosinephosphatase1B(PTP1B) Breastcancer |
Issue Date: | 2016 |
Series/Report no.: | Molecules;21 .- p.1091 |
Abstract: | PTP1B deficiency in mouse mammary tumor virus (MMTV)-NeuNT transgenic mice inhibited the onset of MMTV-NeuNT-evoked breast cancer, while its overexpression was observed in breast cancer. Thus, PTP1B inhibitors are considered chemopreventative agents for breast cancer. As part of our program to find PTP1B inhibitors, one new diterpene glycoside (1) and 13 known compounds (2–14) were isolated from the methanol extract of the stems of Akebia quinata. All isolates were identified based on extensive spectroscopic data analysis, including UV, IR, NMR and MS. Compounds 2, 3, 6, 8 and 11 showed significant inhibitory effects on the PTP1B enzyme, with IC50 values ranging from 4.08 - 1.09 to 21.80 - 4.74 TM. PTP1B inhibitors also had concentration-dependent cytotoxic effects on breast cancer cell lines, such as MCF7, MDA-MB-231 and tamoxifen-resistant MCF7 (MCF7/TAMR) (IC50 values ranging from 0.84 - 0.04 to 7.91 - 0.39 TM). These results indicate that compounds 6 and 8 from Akebia quinata may be lead compounds acting as anti-breast cancer agents. |
URI: | http://dspace.ctu.edu.vn/jspui/handle/123456789/4217 |
Appears in Collections: | Tạp chí quốc tế |
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