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Molecules 2016, 21(8), 1091; doi:10.3390/molecules21081091

Protein Tyrosine Phosphatase 1B Inhibitors from the Stems of Akebia quinata

1
Korea Bioactive Natural Material Bank, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Korea
2
Marine Bio Research Center, Department of Life Science, Chosun University, Gwangju 501-759, Korea
*
Author to whom correspondence should be addressed.
Academic Editor: Isabel C. F. Ferreira
Received: 17 July 2016 / Revised: 6 August 2016 / Accepted: 10 August 2016 / Published: 19 August 2016
(This article belongs to the Collection Bioactive Compounds)
View Full-Text   |   Download PDF [1055 KB, uploaded 19 August 2016]   |  

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 (214) 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 μM. 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 μM). These results indicate that compounds 6 and 8 from Akebia quinata may be lead compounds acting as anti-breast cancer agents. View Full-Text
Keywords: Akebia quinata; terpenes; protein tyrosine phosphatase 1B (PTP1B); breast cancer Akebia quinata; terpenes; protein tyrosine phosphatase 1B (PTP1B); breast cancer
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

An, J.-P.; Ha, T.K.Q.; Kim, J.; Cho, T.O.; Oh, W.K. Protein Tyrosine Phosphatase 1B Inhibitors from the Stems of Akebia quinata. Molecules 2016, 21, 1091.

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