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Protein Tyrosine Phosphatase 1B Inhibitors from the Stems of Akebia quinata
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...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2016
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273847/ https://www.ncbi.nlm.nih.gov/pubmed/27548130 http://dx.doi.org/10.3390/molecules21081091 |
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author | An, Jin-Pyo Ha, Thi Kim Quy Kim, Jinwoong Cho, Tae Oh Oh, Won Keun |
author_facet | An, Jin-Pyo Ha, Thi Kim Quy Kim, Jinwoong Cho, Tae Oh Oh, Won Keun |
author_sort | An, Jin-Pyo |
collection | PubMed |
description | 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 IC(50) 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) (IC(50) 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. |
format | Online Article Text |
id | pubmed-6273847 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62738472018-12-28 Protein Tyrosine Phosphatase 1B Inhibitors from the Stems of Akebia quinata An, Jin-Pyo Ha, Thi Kim Quy Kim, Jinwoong Cho, Tae Oh Oh, Won Keun Molecules Article 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 IC(50) 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) (IC(50) 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. MDPI 2016-08-19 /pmc/articles/PMC6273847/ /pubmed/27548130 http://dx.doi.org/10.3390/molecules21081091 Text en © 2016 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article An, Jin-Pyo Ha, Thi Kim Quy Kim, Jinwoong Cho, Tae Oh Oh, Won Keun Protein Tyrosine Phosphatase 1B Inhibitors from the Stems of Akebia quinata |
title | Protein Tyrosine Phosphatase 1B Inhibitors from the Stems of Akebia quinata |
title_full | Protein Tyrosine Phosphatase 1B Inhibitors from the Stems of Akebia quinata |
title_fullStr | Protein Tyrosine Phosphatase 1B Inhibitors from the Stems of Akebia quinata |
title_full_unstemmed | Protein Tyrosine Phosphatase 1B Inhibitors from the Stems of Akebia quinata |
title_short | Protein Tyrosine Phosphatase 1B Inhibitors from the Stems of Akebia quinata |
title_sort | protein tyrosine phosphatase 1b inhibitors from the stems of akebia quinata |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273847/ https://www.ncbi.nlm.nih.gov/pubmed/27548130 http://dx.doi.org/10.3390/molecules21081091 |
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