nakhjavani-stereoselective-2019.pdf (2.3 MB)
Stereoselective anti-cancer activities of ginsenoside rg3 on triple negative breast cancer cell models
journal contribution
posted on 2019-01-01, 00:00 authored by Maryam Nakhjavani, H M Palethorpe, Y Tomita, E Smith, T J Price, A J Yool, J V Pei, A R Townsend, J E HardinghamGinsenoside Rg3 (Rg3) has two epimers, 20(S)-ginsenoside Rg3 (SRg3) and 20(R)-ginsenoside Rg3 (RRg3), and while Rg3 itself has been reported to have anti-cancer properties, few studies have been reported on the anti-cancer effects of the different epimers. The aim was to investigate the stereoselective effects of the Rg3 epimers on triple negative breast cancer (TNBC) cell lines, tested using cell-based assays for proliferation, apoptosis, cell cycle arrest, migration and invasion. Molecular docking showed that Rg3 interacted with the aquaporin 1 (AQP1) water channel (binding score −9.4 kJ mol−1). The Xenopus laevis oocyte expression system was used to study the effect of Rg3 epimers on the AQP1 water permeability. The AQP1 expression in TNBC cell lines was compared with quantitative-polymerase chain reaction (PCR). The results showed that only SRg3 inhibited the AQP1 water flux and inhibited the proliferation of MDA-MB-231 (100 μM), due to cell cycle arrest at G0/G1. SRg3 inhibited the chemoattractant-induced migration of MDA-MB-231. The AQP1 expression in MDA-MB-231 was higher than in HCC1143 or DU4475 cell lines. These results suggest a role for AQP1 in the proliferation and chemoattractant-induced migration of this cell line. Compared to SRg3, RRg3 had more potency and efficacy, inhibiting the migration and invasion of MDA-MB-231. Rg3 has stereoselective anti-cancer effects in the AQP1 high-expressing cell line MDA-MB-231.
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Journal
PharmaceuticalsVolume
12Issue
3Article number
117Pagination
1 - 14Publisher
MDPI AGLocation
Basel, SwitzerlandPublisher DOI
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eISSN
1424-8247Language
engPublication classification
C1 Refereed article in a scholarly journalUsage metrics
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