L-Chicoric Acid

Chicoric acid is a dicaffeoyl ester that has been found in C. intybus with diverse biological activities.¹ Chicoric acid (50-200 μg/ml) dose-dependently reduces the viability of Caco-2 and HCT116 human colorectal cancer cells.² It inhibits HIV integrase activities, including 3'-processing of a DNA oligonucleotide and integration with template DNA (IC₅₀s = 1.1 and 0.8 μM, respectively).³ Chicoric acid (0.5-10 μM) noncompetitively inhibits integration of HIV DNA by HIV integrase and, at concentrations greater than or equal to 5 μM, inhibits HIV entry into H9 cells.⁴ Oral administration of chicoric acid (10 and 30 mg/kg) reduces hepatic lipid accumulation, lipid peroxidation, and fibrosis, inhibits production of pro-inflammatory cytokines and activation of NF-kB, and activates the AMPK signaling pathway in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a methionine and choline-deficient diet.⁵ Chicoric acid (2 mg/kg) also reduces blood glucose levels by 54% in mice with streptozotocin-induced diabetes.⁶

1.Xiao, H., Xie, G., Wang, J., et al.Chicoric acid prevents obesity by attenuating hepatic steatosis, inflammation and oxidative stress in high-fat diet-fed miceFood Res. Int.54(1)345-353(2013) 2.Tsai, Y.-L., Chiu, C.-C., Chen, J.Y.-F., et al.Cytotoxic effects of Echinacea purpurea flower extracts and cichoric acid on human colon cancer cells through induction of apoptosisJ. Ethnaopharmacol.143(3)914-919(2012) 3.Lin, Z., Neamati, N., Zhao, H., et al.Chicoric acid analogues as HIV-1 integrase inhibitorsJ. Med. Chem.42(8)1401-1414(1999) 4.Reinke, R.A., Lee, D.J., McDougall, B.R., 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 vitroVirology326(2)203-219(2004) 5.Kim, M., Yoo, G., Randy, A., et al.Chicoric acid attenuate a nonalcoholic steatohepatitis by inhibiting key regulators of lipid metabolism, fibrosis, oxidation, and inflammation in mice with methionine and choline deficiencyMol. Nutr. Food Res.61(5)(2017) 6.Casanova, L.M., da Silva, D., Sola-Penna, M., et al.Identification of chicoric acid as a hypoglycemic agent from Ocimum gratissimum leaf extract in a biomonitoring in vivo studyFiloterapia93132-141(2014)