In vitro antileishmanial activity of three saponins isolated from ivy, α-hederin, β-hederin and hederacolchiside A1, in association with pentamidine and amphotericin B

The in vitro antileishmanial activity of three saponins isolated from ivy, α-hederin, β-hederin and hederacolchiside A1, was investigated on parasites of the species Leishmania mexicana, in their promastigote and amastigote forms compared with their toxicity versus human monocytes. The results showed that saponins exhibited a strong antiproliferative activity on all stages of development of the parasite but demonstrated a strong toxicity versus human cells. Association of subtoxic concentrations of saponins with antileishmanial drugs such as pentamidine and amphotericin B demonstrated that saponins could enhance the efficiency of conventional drugs on both the promastigote and the amastigote stages of development of the parasite. The results demonstrated moreover that the action of saponins on promastigote membrane was cumulative with those of amphotericin B

Antileishmanial activity of three saponins isolated from ivy, α- hederin, β-hederin and hederacolchiside A1, as compared to their action on mammalian cells cultured in vitro

The in vitro antileishmanial activity of three saponins isolated from ivy, α-hederin, β-hederin and hederacolchiside A1, was investigated on Leishmania infantum. The assessment of possible targets (membrane integrity, membrane potential, DNA synthesis and protein content) was performed in both Leishmania promastigotes and human monocytes (THP1 cells). Results observed in Leishmania showed that the saponins exhibited a strong antiproliferative activity on all stages of development of the parasite by altering membrane integrity and potential: hederacolchiside A1 appeared to be the most active compound against both promastigotes and amastigotes. Results observed in THP1 cells demonstrated that the saponins exerted also a potent antiproliferative activity against human monocytes, by producing a significant DNA synthesis inhibition. The ratio between antileishmanial activity on amastigotes and toxicity to human cells suggested that the saponins could be considered as possible antileishmanial drugs

Cytotoxic triterpenoid saponins from the roots of Cephalaria gigantea

Three new oleanane-type saponins, giganteosides L (1)(I), M (2) and N (3) along with eight known ones were isolated from the roots of Cephalaria gigantea. Their structures were established as 3-O-[-D-galactopyranosyl-(12)--D-glucuronopyranosyl]-28-O-[-D-glucopyranosyl-(16)--D-glucopyranosyl]-oleanolic acid, 3-O-[-D-galactopyranosyl-(12)--D-glucuronopyranosyl]-28-O-[-D-glucopyranosyl-(16)--D-glucopyranosyl]-hederagenin, 3-O-[-L-rhamnopyranosyl-(12)--D-glucuronopyranosyl]-28-O-[-D-glucopyranosyl-(16)--D-glucopyranosyl]-hederagenin, resp., by means of spectroscopic methods (1D and 2D NMR, HR-ESI-MS). Cytotoxic activity of monodesmosides was investigated in vitro using three cancer cell lines, namely, human non pigmented melanoma MEL-5 and human leukemia HL-60. Giganteosides D (4) and E (5) showed antiproliferative effect on human cell lines with IC50 values in the range 3.15-7.5 M