In Vitro and in Vivo Anti-Leishmanial Activity of Triterpenoid Saponins Isolated from Maesa balansae and Some Chemical Derivatives

Abstract

The methanolic extract from the leaves of the Vietnamese medicinal plant Maesa balansae showed potent in vitro and in vivo activity against the tropical protozoal parasite Leishmania infantum. Bioassay-guided purification of the extract led to the identification of six triterpenoid saponins, maesabalides I-VI (1-6), each having a strong and specific anti-leishmanial activity. Maesabalide III (3) and IV (4) were the most potent with IC(50) values against intracellular amastigotes of about 7 and 14 ng/mL. In comparison, the IC(50) value of sodium stibogluconate, the reference drug for treatment of leishmaniasis, is only 5.6 microg/mL. No cytotoxicity was present on a human fibroblast (MRC-5) cell line (CC(50) > 32 microg/mL). In vivo evaluation in the BALB/C mouse model demonstrated that >90% reduction of liver amastigote burdens was obtained 1 week after a single subcutaneous dose at 0.2-0.4 mg/kg was administered. Several chemical derivatives of maesabalides I-VI were prepared in order to study the structure-activity relationship.

Efficacy and tolerability of oleylphosphocholine (OlPC) in a laboratory model of visceral leishmaniasis

“…18 For the in vivo experiments, the drug-sensitive laboratory strain of L. infantum (MHOM/MA(BE)/67) was used. 19 In vitro drug susceptibility assay Amastigotes derived from the spleen of donor RAG1.B6 or BALB/c mice were used to infect primary peritoneal mouse macrophages collected 2 days after intraperitoneal induction with 2 mL 2% soluble starch. 20 The cells were grown in 16-well tissue culture slides (Lab Tecw) in RPMI 1640 medium supplemented with 200 mM L-glutamine, 16.5 mM NaHCO 3 and 10% FCS at 378C and 5% CO 2 .…”

In Vitro Antileishmanial Activity of Falcaria vulgaris Fractions on Leishmania major

“…In this regard, one previous study showed that F. vulgaris is rich in these compounds (10). In addition, saponin is another compound in this plant with antileishmanial effects (22,23). According to some research, a few plants show mild to strong activities against Leishmania species (24-27).…”

Herbal Drugs with Promising Anti-Leishmanial Activity: New Hope for Leishmaniasis Treatment

“…In another study in vivo potential effectiveness of Artemisia annua against Leishmania was reported (23). The methanolic extract from the leaves of the Vietnamese medicinal plant Maesa balansae displayed effective in vivo activity against Leishmania infantum with 90% reduction of liver amastigote burden (24). The experiments done by Maes et al showed that Triterpenoid Saponin Extract (PX-6518) from the Plant Maesa balansae had promising in vivo anti-leishmanial potential against Species of visceral Leishmania in BALB/c mouse model, and 80% reduction of liver amastigote burden was reported (25).…”