Transcrocetin is a natural apocarotenoid isolated from C. sativus and G. jasminoides that has antioxidant, antiproliferative, anti-inflammatory, cardioprotective, and antinociceptive properties.1,2,3,4,5,6 It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals (IC50 = 17.8 μg/ml) and inhibits growth of MKN28 stomach, MCF-7 breast, and Caco-2 colon cancer cell lines (IC50s = 53, 63, and 103 μM, respectively).2,3 Transcrocetin (20 μM) protects primary rat microglial cells from LPS-induced death and decreases LPS-induced production of intracellular reactive oxygen species (ROS), TNF-α, IL-1β, and NF-κB.4 Transcrocetin (100 mg/kg) increases the level of glutathione (GSH), catalase (CAT), creatine kinase (CK), and lactate dehydrogenase (LDH) in cardiac tissue in a rat model of myocardial infarction induced by isoproterenol .5 It also increases the pressure threshold and latency to withdrawal in response to mechanical and thermal stimuli, respectively, indicating a decrease in allodynia in a mouse model of spared nerve injury when administered intrathecally at a dose of 30 mg/kg.6
1.Pfister, S.L., Meyer, P., Steck, A., et al.Isolation and structure elucidation of carotenoid?glycosyl esters in gardenia fruits (Gardenia jasminoides Ellis) and saffron (Crocus sativus Linne)J. Agric. Food Chem.44(9)2612-2615(1996) 2.Kanakis, C.D., Tarantilis, P.A., Tajmir-Riahi, H.A., et al.Crocetin, dimethylcrocetin, and safranal bind human serum albumin: Stability and antioxidative propertiesJ. Agric. Food Chem.55(3)970-977(2007) 3.Oliveira, H., Cai, X., Zhang, Q., et al.Gastrointestinal absorption, antiproliferative and anti-inflammatory effect of the major carotenoids of Gardenia jasminoides Ellis on cancer cellsFood Funct.8(4)1672-1679(2017) 4.Nam, K.N., Park, Y.-M., Jung, H.-J., et al.Anti-inflammatory effects of crocin and crocetin in rat brain microglial cellsEur. J. Pharmacol.648(1-3)110-116(2010) 5.Zhang, W., Li, Y., and Ge, Z.Cardiaprotective effect of crocetin by attenuating apoptosis in isoproterenol induced myocardial infarction rat modelBiomed. Pharmacother.93376-382(2017) 6.Wang, X., Zhang, G., Qiao, Y., et al.Crocetin attenuates spared nerve injury-induced neuropathic pain in miceJ. Pharmacol. Sci.135(4)141-147(2017)