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1,2,3,4,6-Penta-O-galloylglucose within Galla Chinensis Inhibits Human LDH-A and Attenuates Cell Proliferation in MDA-MB-231 Breast Cancer Cells
Joint Authors
Soliman, Karam F. A.
Deiab, Shihab
Mazzio, Elizabeth
Eyunni, Suresh
McTier, Oshlii
Mateeva, Nelly
Elshami, Faisel
Source
Evidence-Based Complementary and Alternative Medicine
Issue
Vol. 2015, Issue 2015 (31 Dec. 2015), pp.1-11, 11 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2015-03-30
Country of Publication
Egypt
No. of Pages
11
Main Subjects
Abstract EN
A characteristic feature of aggressive malignancy is the overexpression of lactic acid dehydrogenase- (LDH-) A, concomitant to pericellular accumulation of lactate.
In a recent high-throughput screening, we identified Rhus chinensis (Mill.) gallnut (RCG) (also known as Galla Chinensis) extract as a potent (IC50 < 1 µg/mL) inhibitor of human LDH-A (hLDH-A).
In this study, through bioactivity guided fractionation of the crude extract, the data demonstrate that penta-1,2,3,4,6-O-galloyl-β-D-glucose (PGG) was a primary constituent responsible for hLDH-A inhibition, present at ~9.95 ± 0.34% dry weight.
Theoretical molecular docking studies of hLDH-A indicate that PGG acts through competitive binding at the NADH cofactor site, effects confirmed by functional enzyme studies where the IC50 = 27.32 nM was reversed with increasing concentration of NADH.
Moreover, we confirm protein expression of hLDH-A in MDA-231 human breast carcinoma cells and show that PGG was toxic (LC50 = 94.18 µM), parallel to attenuated lactic acid production (IC50 = 97.81 µM).
In a 72-hour cell proliferation assay, PGG was found to be a potent cytostatic agent with ability to halt cell division (IC50 = 1.2 µM) relative to paclitaxel (IC50 < 100 nM).
In summary, these findings demonstrate that PGG is a potent hLDH-A inhibitor with significant capacity to halt proliferation of human breast cancer cells.
American Psychological Association (APA)
Deiab, Shihab& Mazzio, Elizabeth& Eyunni, Suresh& McTier, Oshlii& Mateeva, Nelly& Elshami, Faisel…[et al.]. 2015. 1,2,3,4,6-Penta-O-galloylglucose within Galla Chinensis Inhibits Human LDH-A and Attenuates Cell Proliferation in MDA-MB-231 Breast Cancer Cells. Evidence-Based Complementary and Alternative Medicine،Vol. 2015, no. 2015, pp.1-11.
https://search.emarefa.net/detail/BIM-1061308
Modern Language Association (MLA)
Deiab, Shihab…[et al.]. 1,2,3,4,6-Penta-O-galloylglucose within Galla Chinensis Inhibits Human LDH-A and Attenuates Cell Proliferation in MDA-MB-231 Breast Cancer Cells. Evidence-Based Complementary and Alternative Medicine No. 2015 (2015), pp.1-11.
https://search.emarefa.net/detail/BIM-1061308
American Medical Association (AMA)
Deiab, Shihab& Mazzio, Elizabeth& Eyunni, Suresh& McTier, Oshlii& Mateeva, Nelly& Elshami, Faisel…[et al.]. 1,2,3,4,6-Penta-O-galloylglucose within Galla Chinensis Inhibits Human LDH-A and Attenuates Cell Proliferation in MDA-MB-231 Breast Cancer Cells. Evidence-Based Complementary and Alternative Medicine. 2015. Vol. 2015, no. 2015, pp.1-11.
https://search.emarefa.net/detail/BIM-1061308
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1061308