A sesquiterpene lactone
Cynaropicrin is a sesquiterpene lactone originally isolated from artichoke (C. scolymus) that has diverse biological activities.1,2,3,4,5 It inhibits the growth of SKOV3, LOX-IMVI, A549, MCF-7, HCT15, and PC-3 cancer cells (IC50s = 1.1-8.7 μg/ml).1 Cynaropicrin inhibits hepatitis C virus (HCV) replication in Huh7.5 cells with EC50 values ranging from 0.4 to 1.4 μM for genotypes 1a, 1b, 2b, 3a, 4a, 5a, 6a, and 7a.2 It inhibits release of TNF-α and nitric oxide (NO) from LPS-stimulated RAW264.7 cells (IC50s = 8.24 and 1.1 μM, respectively) as well as LPS-induced lymphocyte proliferation (IC50 = 0.9 μM).3 Cynaropicrin inhibits the growth of T. cruzi bloodstream trypomastigotes isolated from infected mice (EC50 = 1 μg/ml).4 It also exhibits antifeedant activity against S. granarius beetles, T. confusum larvae, and T. granarium larvae.5
1.Elsebai, M.F., Mocan, A., and Atanasov, A.G.Cynaropicrin: A comprehensive research review and therapeutic potential as an anti-hepatitis C virus agentFront. Pharmacol.7:472(2016) 2.Elsebai, M.F., Koutsoudakis, G., Saludes, V., et al.Pan-genotypic hepatitis C virus inhibition by natural products derived from the wild egyptian artichokeJ. Virol.90(4)1918-1930(2015) 3.Cho, J.Y., Baik, K.U., Jung, J.H., et al.In vitro anti-inflammatory effects of cynaropicrin, a sesquiterpene lactone, from Saussurea lappaEur. J. Pharmacol.398(3)399-407(2000) 4.da Silva, C.F., Batista Dda, G., De Araújo, J.S., et al.Activities of psilostachyin A and cynaropicrin against Trypanosoma cruzi in vitro and in vivoAntimicrob. Agents Chemother.57(11)5307-5314(2013) 5.Cis, J., Nowark, G., and Kisiel, W.Antifeedant properties and chemotaxonomic implications of sesquiterpene lactones and syringin from Rhaponticum pulchrumBiochem. System. Ecol.34(12)862-867(2006)
Cell experiment: | Human U937 cells are cultured in RPMI1640 supplemented with 10% fetal bovine serum. To differentiate U937 cells, 2×106 cells/mL are treated with phorbol 12-myristate 13-acetate (PMA) of 20 ng/mL for 24 h. The PMA is removed by washing and adherent cells are then allowed to recuperate for 40 h. The recuperated cells are subsequently incubated with lipopolysaccharide of 1 μg/mL for 6 h with Cynaropicrin and positive control drugs. Supernatants are harvested and assayed by ELISA kit for human TNF-α[1]. |
Animal experiment: | Male Swiss mice are used in this study. Mice are housed at a maximum of 8 per cage and kept in a conventional room at 20 to 24°C under a 12 h to 12 h light-dark cycle. The animals are provided with sterilized water and chow ad libitum. Infection is performed by i.p. injection of 104 or 5×103 bloodstream trypomastigotes. The animals (18 to 21 g) are divided into the following groups (at least five mice per group): uninfected (noninfected and untreated), untreated (infected with T. cruzi but treated only with vehicle), and treated (infected and treated i.p. with 0.5 to 50 mg/kg/day compound (including Cynaropicrin) or 100 mg/kg/day benznidazole). Mice receive 0.1 mL (i.p.) at 5 and 8 days postinfection (dpi), or at 11, 12, and 13 dpi for the dose of 25 mg/kg, twice a day (b.i.d.)[3]. |
参考文献: [1]. Cho JY, et al. In vitro anti-inflammatory effects of cynaropicrin, a sesquiterpene lactone, from Saussurea lappa. Eur J Pharmacol. 2000 Jun 23;398(3):399-407. | |
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