L-Chicoric Acid (Synonyms: L-Chicoric Acid, Dicaffeoyltartaric Acid, NSC 99173)

L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture[1][2][3].

L-Chicoric Acid inhibits integration at concentrations from 500 nM to 10 μM but also inhibits entry at concentrations above 1 μM. L-Chicoric Acid clearly affects viral entry at concentrations of 5 μM and higher. L-Chicoric Acid also inhibits integration as indicated both by an increased ratio of two LTR circle DNA to cDNA and an accompanying decrease in integrated provirus. The EC50 of L-Chicoric Acid against HIV is approximately 500 nM, a concentration that does not inhibit HIV entry in H9 cells[1].The ED50 of L-Chicoric Acid against HIVNL4-3 control virus is 400 nM, while HIVNL4-3 passaged in the presence of 8 μM L-Chicoric Acid is completely resistant to the compound[2].

[1]. Reinke RA, et al. L-chicoric acid inhibits human immunodeficiency virus type 1 integration in vivo and is a noncompetitive but reversible inhibitor of HIV-1 integrase in vitro. Virology. 2004 Sep 1;326(2):203-19. [2]. King PJ, et al. Resistance to the anti-human immunodeficiency virus type 1 compound L-chicoric acid results from a single mutation at amino acid 140 of integrase. J Virol. 1998 Oct;72(10):8420-4. [3]. Robinson WE Jr. L-chicoric acid, an inhibitor of human immunodeficiency virus type 1 (HIV-1) integrase, improves on the in vitro anti-HIV-1 effect of a protease inhibitor (AG1350). Antiviral Res. 1998 Aug;39(2):101-11.