Antiprotozoal Compounds from Urolepis hecatantha (Asteraceae)

Abstract

The dewaxed dichloromethane extract of Urolepis hecatantha and the compounds isolated from it were tested for their in vitro activity on Trypanosoma cruzi epimastigotes and Leishmania infantum promastigotes. The extract of U. hecatantha showed activity against both parasites with IC50 values of 7 µg/mL and 31 µg/mL, respectively. Fractionation of the dichloromethane extract led to the isolation of euparin, jaceidin, santhemoidin C, and eucannabinolide. The sesquiterpene lactones eucannabinolide and santhemoidin C were active on T. cruzi with IC50 values of 10 ± 2 µM (4.2 µg/mL) and 18 ± 3 µM (7.6 µg/mL), respectively. Euparin and santhemoidin C were the most active on L. infantum with IC50 values of 18 ± 4 µM (3.9 µg/mL) and 19 ± 4 µM (8.0 µg/mL), respectively. Eucannabinolide has also shown drug-like pharmacokinetic and toxicity properties.

Anti-Trypanosoma cruzi Properties of Sesquiterpene Lactones Isolated from Stevia spp.: In Vitro and In Silico Studies

“…After filtration, the extract was dried by vacuum evaporation under reduced pressure, resulting in 18 g of crude extract (3.6% yield). The extract was dewaxed following the protocol described by Elso et al [ 26 ] and fractionated by column chromatography on Silicagel (50 × 4.5 cm, 180 g, 230–400 mesh) using dichloromethane:ethyl acetate (CH 2 Cl 2 :EtOAc) mixtures (100:0–0:100) of increasing polarity. Seven fractions were collected (A–G).…”

Plant Terpenoids as Hit Compounds against Trypanosomiasis

“…R.King & H.Rob., were active on T. cruzi epimastigotes with IC 50 values of 10 µM and 18 µM, respectively. Both compounds showed low SI values (CC 50 > 15 µM for 70 and CC 50 = 15 µM for 71 ) [ 72 ].…”

Stevia Genus: Phytochemistry and Biological Activities Update

“…Eucannabinolide was active on T. cruzi with IC 50 = 18 ± 3 µM (7.6 μg/mL). On Leishmania infantum , this compound was less active (IC 50 > 25 µM) [ 62 ]. Eucannabinolide has also demonstrated activity against Trypanosoma brucei rhodesiense trypomastigotes (IC 50 = 1.1 ± 0.1 µM).…”

“…Allison et al [ 230 ] demonstrated the antibacterial activity of jaceidin against E. coli (MIC = 50 μM). The antiprotozoal activity of cimpound 93 was evaluated by Elso et al [ 62 ]. Jaceidin showed moderate activity against T. cruzi epimastigotes and L. infantum promastigotes (IC 50 > 25 µM).…”