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 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.
Highlights
Breast cancer is a threat to the health of women, ranking as the most common cancer in women globally, with more than 1,600,000 cases diagnosed in 2012 [1]
Research reported that the number of breast cancer cases in the United States will increase by 50 percent in 2030 compared to 2011
Four compounds 2, 3, 6 and 8, had strong cytotoxic olean-12-en-28-oic acid (8) [14], ciwujianoside A1 (9) [15], ciwujianoside C3 (10) [16], 2α,3α,23activities against breast cancer lines, with IC50 values ranging from 0.84 ± 0.17 to 13.42 ± 1.26 μM, trihydroxyoleane-12-en-28-oic acid (11) [17], (−)-syringaresinol (12) [18], medioresinol (13) [19], compared with positive controls tamoxifen and 4-hydroxy tamoxifen
Summary
Breast cancer is a threat to the health of women, ranking as the most common cancer in women globally, with more than 1,600,000 cases diagnosed in 2012 [1]. Research reported that the number of breast cancer cases in the United States will increase by 50 percent in 2030 compared to 2011. Several drugs, including adriamycin and taxotere, are used to treat breast cancer, many adverse effects, such as heart problems and reduction of white blood cell numbers, have been reported [1]. Protein tyrosine phosphatase 1B (PTP1B), a negative insulin regulator, has been implicated in the signaling of breast cancer. Inhibitory activity plant been reported.InInthis thispaper, paper, we we report one new diterpene glycoside (1). Report one new diterpene glycoside (1) and 13 known compounds, including four diterpenes (2–5). The inhibitory activities of the isolated compounds were examined against. MCF-7, MDB-MB-231 the inhibitory activities of the isolated compounds were examined against MCF-7, MDB-MB-231 and and tamoxifen-resistant.
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