About: 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

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About: 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 Goto Sponge NotDistinct Permalink

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Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	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
Creator	Deiab, Shihab Elshami, Faisel Eyunni, Suresh Mateeva, Nelly Mazzio, Elizabeth Mctier, Oshlii Soliman, Karam
Source	Medline; PMC
abstract	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 (IC(50) < 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 IC(50) = 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 (LC(50) = 94.18 µM), parallel to attenuated lactic acid production (IC(50) = 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 (IC(50) = 1.2 µM) relative to paclitaxel (IC(50) < 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.
has issue date	2015-03-30(xsd:dateTime)
bibo:doi	10.1155/2015/276946
bibo:pmid	25918543
has license	cc-by
sha1sum (hex)	424d6c622643d36a7f8d9a1d2714f4cef49387ed
schema:url	https://doi.org/10.1155/2015/276946
resource representing a document's title	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
has PubMed Central identifier	PMC4396556
has PubMed identifier	25918543
schema:publication	Evid Based Complement Alternat Med
resource representing a document's body	covid:424d6c622643d36a7f8d9a1d2714f4cef49387ed#body_text
is schema:about of	named entity 'CELL PROLIFERATION' named entity 'acid' named entity 'ability' named entity 'concentration' named entity 'inhibition' named entity 'inhibitor' named entity 'MDA-MB-231' named entity 'GALLOYLGLUCOSE' named entity 'PRIMARY' named entity 'CYTOSTATIC' named entity 'WAS A' named entity 'PENTA' named entity 'BREAST CANCER CELLS' named entity 'CARCINOMA CELLS' named entity 'PROLIFERATION' named entity 'LACTIC ACID' named entity 'OVEREXPRESSION' covid:arg/424d6c622643d36a7f8d9a1d2714f4cef49387ed named entity 'INCREASING CONCENTRATION' named entity 'CONFIRM' named entity 'THEORETICAL' named entity 'EFFECTS' named entity '1.2' named entity 'FINDINGS' named entity 'MOLECULAR DOCKING' named entity 'BREAST CARCINOMA' named entity 'D-GLUCOSE' named entity 'PENTA' named entity 'IS A' named entity 'COMPETITIVE BINDING' named entity 'HUMAN BREAST CANCER CELLS' named entity 'HOUR' named entity 'MALIGNANCY' named entity 'GALLA' named entity '2C6' named entity 'LDH-A' named entity 'HUMAN' named entity 'GALLA' named entity 'PACLITAXEL' named entity 'RHUS CHINENSIS' named entity 'BIOACTIVITY' named entity 'CELL DIVISION' named entity 'RECENT' named entity 'FEATURE' named entity 'STUDY' named entity 'RESPONSIBLE' named entity '231' named entity 'CHARACTERISTIC' named entity '2C6' named entity 'CONCENTRATION OF' named entity 'HALT' named entity 'AGGRESSIVE' named entity 'INHIBITOR' named entity 'REVERSED' named entity 'TOXIC' named entity 'DRY WEIGHT' named entity 'KNOWN' named entity 'IDENTIFIED' named entity 'SITE' named entity 'CELL PROLIFERATION ASSAY' named entity 'STUDIES' named entity 'HIGH-THROUGHPUT SCREENING' named entity 'ACTS' named entity 'CONSTITUENT' named entity 'SUMMARY' named entity 'NADH' named entity 'LDH-A' named entity 'AGENT' named entity 'COFACTOR' named entity 'A 72' named entity 'PRODUCTION' named entity 'LACTATE' named entity 'WHERE' named entity 'CAPACITY' named entity 'PRESENT'

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