SUMMARYShade-dried flowers of Sarcostemma brevistigma Wight Syn (SBF) belonging to Asclepiadaceae yielded a rare flavonol glycoside viz., Quercetin 5a prenyl, 3-O-glucosyl, 7-O-(4c-p-coumaroyl) neohesperidoside which were characterized based on chemical and spectral (including 2D NMR) studies. The ethyl acetate fraction of alcoholic concentrate (test sample) of flowers of this plant (SBF) was evaluated for its hepatoprotective and inhibition of lipid peroxidation activities to investigate the scientific basis of the traditional uses. The oral administration in varying doses viz., 125 and 250 mg/kg of aqueous suspension of SBF to rats for 7 days produced significant (P < 0.01) hepatoprotective effect comparable to that of standard drug silymarin. The SBF afforded good hepatoprotection against CCl 4 induced elevation levels of serum marker enzymes, serum bilirubin and liver weight. The free radical scavenging effects of SBF and flavonol glycoside (SA) were assigned by Fe 2 + /ascorbate induction method (in vitro), which revealed the inhibition of lipid peroxidation. The SBF and SA showed prominent anti-lipid peroxidation activity (IC 5 0 about 180 mg/ml and 11.0 mg/ml respectively), which was comparable to standard drug curcumin (IC 5 0 about ~ 8.25 mg/ml). Thus the hepatoprotective activity of SB could be correlated to the free radical scavenging property of the flavonol glycoside.