Isolation and identification of two galangin metabolites from rat urine and determination of their <i>in vitro</i> hypolipidemic activity

Abstract

Purpose: To investigate the lipid-lowering activity of two metabolites of galangin, namely, galangin-3-O-β-D-glucuronic acid (GG-1) and galangin-7-O-β-D-glucuronic acid (GG-2). Methods

Flavonoids: A treasure house of prospective pharmacological potentials

“…Last but not least, the lipid-lowering activity of these compounds was observed through various mechanisms including the reduction of LOX-1 protein expression [ 84 , 213 ], SREBP-1a, SREBP-1c, SREBP-2 transcription factor, expression of FAS, ACC, HMGR [ 117 ], and levels of TC, TG, LDL, VLDL, FFA, phospholipids [ 33 , 119 ]; while increasing autophagic efflux [ 99 , 214 ], autophagic lipid breakdown [ 99 ], PPAR-α expression, acetyl Co-A oxidase and HDL levels [ 148 ] ( Fig. 11 ).…”

“…A study inspected the hypolipidemic action of galangin and its two metabolites including galanin-3-O-β- d -glucuronic acid and galanin-7-O-β- d -glucuronic acid against female Sprague Dawley rats and observed that the compound and both of its metabolites were found to have potential hypolipidemic potency by down-regulating lipogenic genes like SREBP-1a, SREBP-1c, and SREBP-2 transcription factors, as well as suppressed genes like FAS, ACC, and HMGR [ 117 ].…”

Simultaneous determination of two galangin metabolites from Alpinia Officinarum Hance in rat plasma by UF LC-MS/MS and its application in pharmacokinetics study

“…In this work, after oral administration of galangal extract in rats, we actually determined two galangin metabolites GG-1 and GG-2 which was in accordance with our previous conclusion that galangin was preferentially glucuronidated after oral administration. Besides, our previous study has indicated that both the glucuronidated and the sulfated were more efficient than free parent galangin which highlight the importance of conducting research on galangin metabolites ( Zhang et al, 2016 ).…”

“…GG-1 and GG-2 standards (the purity of both standards was over 97%) were separated from rat urine after oral administration of galangin according to previous reports and quantified by HPLC–PDA–MS ( Zhang et al, 2016 ). As IS, chrysin (the purity: 98.0%) was separated from A. oxyphylla fruits by our laboratory and confirmed through MS and NMR analysis.…”

“…Our previous pharmacokinetic studies have indicated that galangin can be rapidly converted into glucuronidated metabolites after oral or intravenous administration in rats ( Chen et al, 2015 ). Two galangin metabolites, galangin-3-O-β-D-glucuronic acid (GG-1) and galangin-7-O-β-D-glucuronic acid (GG-2), were isolated from rat urine that was collected after oral administration of galangin ( Zhang et al, 2016 ). The chemical structures and relationships of galangin, GG-1 and GG-2 are shown in Fig.…”