Synergistic Effect of Lupenone and Caryophyllene Oxide against Trypanosoma cruzi.

The in vitro trypanocidal activity of a 1 : 4 mixture of lupenone and caryophyllene oxide confirmed a synergistic effect of the terpenoids against epimastigotes forms of T. cruzi (IC50 = 10.4 µ g/mL, FIC = 0.46). In addition, testing of the terpenoid mixture for its capacity to reduce the number of amastigote nests in cardiac tissue and skeletal muscle of infected mice showed a reduction of more than 80% at a dose level of 20.8 mg·kg(-1)·day(-1).

Metabolites from the leaf extract of Serjania yucatanensis with trypanocidal activity against Trypanosoma cruzi.

The bioassay-guided phytochemical investigation of the leaf extract of Serjania yucatanensis, a woody climbing plant endemic to the Yucatan peninsula, led to the identification of a mixture of a triterpene [lup-20(29)-en-3-one] and an oxygenated sesquiterpene (ß-caryophyllene oxide), as that responsible for the originally detected trypanocidal activity in the organic crude extract. Results showed that the mixture of lup-20(29)-en-3-one and ß-caryophyllene oxide is active against trypomastigotes of Trypanosoma cruzi (IC(50) =80.3 µg/mL) and inhibits the egress of trypomastigotes from infected Vero cells (when tested at 100 µg/mL) without being cytotoxic.

In vitro and in vivo trypanocidal activity of native plants from the Yucatan Peninsula.

Ethanol extracts of Senna villosa, Serjania yucatanensis, Byrsonima bucidaefolia, and Bourreria pulchra were evaluated for their in vitro activity against epimastigotes and trypomastigotes of Trypanosoma cruzi. Results showed that the leaf extracts of S. yucatanensis and B. pulchra were the most active against epimastigotes (IC(100) = 100 µg/mL) and trypomastigotes of T. cruzi (95% or more reduction in the number of parasites at 100 and 50 µg/mL). However, only the leaf extract of S. yucatanensis showed significant trypanocidal activity when tested in vivo, reducing 75% of the parasitemia in infected mice at 100 mg/kg. This same extract inhibited the egress of trypomastigotes from infected cells and proved not to be cytotoxic (IC(50) = 318.8 ± 2.3 µg/mL).

Antitrypanosomal activity of Senna villosa in infected BALB/c mice with Trypanosoma cruzi during the sub acute phase of infection.

Antitrypanosomal activity of chloroform extract of Senna villosa leaves was evaluated in the sub acute phase of mice infected with Trypanosoma cruzi. Oral doses of 3.3, 6.6 and 13.2 µg/g were tested during 15 days on infected mice BALB/c, beginning treatment 40 days after infection to evaluate specifically the antitrypanosomal activity over the amastigote form of the parasite. Two different amount of parasites (100 and 500) were inoculated to 25 mice for each doses tested. At the end of the assay the animals were sacrificed and cardiac and skeletal tissue sections were stained with hematoxylin-eosin (HE) for identification and quantification of amastigote nest. In mice infected with 100 parasites, a significant reduction in the number of amastigote nest was observed in cardiac tissue of treated animals at all doses evaluated (p<0.05). An important reduction of amastigote nest was also observed in treated animals and infected with 500 parasites in comparison with no treated mice or treated with allopurinol.