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Nat Prod Res. 2018 Nov 16:1-5. doi: 10.1080/14786419.2018.1508144. [Epub ahead of print]

Antiproliferative effect of 2-Hydroxy-6-tridecylbenzoic acid from ginkgo biloba sarcotestas through the aryl hydrocarbon receptor pathway in triple-negative breast cancer cells.

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a College of Food Science and Technology , Shenyang Agricultural University , Shenyang , China.
b College of Bioscience and Biotechnology , Shenyang Agricultural University , Shenyang , China.
c Department of Oncology , The First Affiliated Hospital of Jinzhou Medical University , Jinzhou , China.


This study aims to isolate the potential antiproliferative and cytotoxic compounds from ginkgo biloba sarcotestas (GBS) and investigates the underlying mechanism in human MDA-MB-231 and mouse 4T-1 triple-negative breast cancer cells. Our results showed that 2-Hydroxy-6-tridecylbenzoic acid was isolated by cytotoxicity-guided fractionation where different fractions were assessed using MTT assay against MDA-MB-231 and 4T-1 cells. Colony formation assay showed that 2-Hydroxy-6-tridecylbenzoic acid significantly inhibited cell proliferation. The inhibition was associated with the enhancement of cytochrome P450 (CYP) 1B1 expression in a dose- and time-dependent manner and no significant change of CYP1A1 expression by qPCR and Western blot assays in MDA-MB-231 and 4T-1 cells. The mechanism was further demonstrated by the activation of aryl hydrocarbon receptor (AhR) pathway with the upregulation of AhR, AhR nuclear translocator (ARNT) and AhR-dependent xenobiotic response elements (XRE) activity. These findings may have implications for development of anticancer agents containing 2-Hydroxy-6-tridecylbenzoic acid as functional additives.


2-Hydroxy-6-tridecylbenzoic acid; AhR; Breast cancer; CYP1B1; antiproliferation; ginkgo biloba sarcotestas

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