A benzoic acid with diverse biological activities
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Gentisic acid is a benzoic acid that has been found in Gentiana and an active metabolite of aspirin with diverse biological activities.1,2,3,4,5 It decreases radiation-induced production of thiobarbituric acid reactive substances (TBARS), hydrogen peroxide, and protein carbonyls, increases superoxide dismutase activity, and prevents hemolysis in isolated human erythrocytes when used at concentrations ranging from 5 to 100 μM.1 Gentisic acid (1-10 μM) inhibits LDL oxidation and formation of cholesterol ester hydroperoxides in isolated human plasma.2 It induces relaxation of isolated guinea pig trachea (EC50 = 20 μM), an effect that is reduced by the large-conductance calcium-activated potassium channel blocker charybdotoxin .3 Gentisic acid (10 and 100 mg/kg) reduces cardiac hypertrophy and fibrosis and pulmonary remodeling, suppresses the renin-angiotensin-aldosterone system, and inhibits cardiac dysfunction in a mouse model of transverse aortic constriction-induced cardiac hypertrophy.4 It also prevents cardiovascular collapse and lactic acidemia in a canine model of P. aeruginosa-induced septic shock.5
1.Joshi, R.P., Gangabhagirathi, R., Venu, S., et al.Antioxidant activity and free radical scavenging reactions of gentisic acid: In-vitro and pulse radiolysis studiesFree Radic. Res.46(1)11-20(2012) 2.Ashidate, K., Kawamura, M., Mimura, D., et al.Gentisic acid, an aspirin metabolite, inhibits oxidation of low-density lipoprotein and the formation of cholesterol ester hydroperoxides in human plasmaEur. J. Pharmacol.513(3)173-179(2005) 3.Cunha, J.F., Campestrini, F.D., Calixto, J.B., et al.The mechanism of gentisic acid-induced relaxation of the guinea pig isolated trachea: The role of potassium channels and vasoactive intestinal peptide receptorsBraz. J. Med. Biol. Res.34(4)381-388(2001) 4.Sun, S., Kee, H.J., Ryu, Y.L., et al.Gentisic acid prevents the transition from pressure overload-induced cardiac hypertrophy to heart failureSci. Rep.9(1)3018(2019) 5.Mink, S., Roy Chowdhury, S.K., Gotes, J., et al.Gentisic acid sodium salt, a phenolic compound, is superior to norepinephrine in reversing cardiovascular collapse, hepatic mitochondrial dysfunction and lactic acidemia in Pseudomonas aeruginosa septic shock in dogsIntensive Care Med. Exp.4(1)24(2016)
LX1606 Hippurate (Telotristat etiprate)
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