Formylated phloroglucinols from Eucalyptus loxophleba foliage

Two new naturally occurring formylated phloroglucinol compounds (FPCs), a dimer, loxophlebal B (10) and a cyclized FPC, loxophlebene (8) together with eight other formylated phloroglucinols (1–7 and 9) were isolated from the chloroform-methanol (8:2) extract of the leaves of Eucalyptus loxophleba ssp. lissophloia. The structures of new compounds were established by comprehensive spectral analysis and by comparison of their NMR data with those of related compounds in the literature. All the isolated compounds were evaluated for anti-leishmanial activity against promastigotes of Leishmania donovani.     

Antiparasitic antioxidant phenylpropanoids and iridoid glycosides from Tecoma mollis

A radical scavenging guided phytochemical study on the stem bark of Tecoma mollis afforded seven active phenylpropanoid glycosides (1–7), including a new one (4), and one iridoid (8). The structures of the isolated compounds were elucidated on the basis of spectroscopic evidences and correlated with known compounds. Compounds (1–7) displayed promising antioxidant activity (DPPH assay) in relation to ascorbic acid (positive control). The antimicrobial activity for compounds (1–8) was evaluated against five bacterial and five fungal strains. The isolated compounds exhibited nonselective weak to moderate antimicrobial activity. The highest antileishmanial activity against Leishmania donovani was observed for compound (7) with an IC₅₀ value of 6.71 μg/ml, using pentamidine and amphotericin B as drug controls. Compound (5) exhibited moderate antimalarial activity (45% inhibition) against chloroquine sensitive (D6) clones of Plasmodium falciparum.     

Antileishmanial polyphenols from Garcinia vieillardii

Seven xanthones, the new vieillardiixanthones B and C (1) and (7), pancixanthones A (2), B (3), 1,6-dihydroxyxanthone (6), pyranojacareubin and 5,6-O-dimethyl-2-deprenylrheediaxanthone together with two benzophenones, clusiachromene (4) and 3-geranyl-2,4,6-trihydroxybenzophenone (5) were isolated from the stem bark of the neocaledonian Garcinia vieillardii. 2, 5 and 6 showed a significant antileishmanial activity against the promastigote forms of Leishmania mexicana and L. infantum and against the amastigote forms of L. infantum.     

Comprehensive investigations on anti-leishmanial potentials of Euphorbia wallichii root extract and its effects on membrane permeability and apoptosis

Clinically available synthetic chemotherapeutics to treat the vector-borne protozoan infection, leishmaniasis, are associated with serious complications such as toxicity and emergence of resistance. Natural products from plants consist of interesting biomolecules that may interfere with DNA or membrane integrity of the parasite and can possibly minimise the associated side effects. In the present study, various fractions of Euphorbia wallichii (EW) root extracts including n-hexane (EWNX), ethyl acetate (EWEA), chloroform (EWCH) and aqueous (EWAQ), were evaluated for their antileishmanial potential against Leishmania tropica followed by investigation of the possible mechanism of action via reactive oxygen species (ROS) quantification, membrane permeability (via sytox green dye) and apoptotic assay (via AO/EB method) using fluorescent microscopy. Two of the fractions i.e. EWEA and EWAQ inhibited the growth of promastigotes (IC₅₀ 7.8 and 10.2 μg/mL, respectively) and amastigotes (IC₅₀ 9.9 and 13.3 μg/mL, respectively) forms almost at similar concentrations as found for the standard antileishmanial drugs, tartar emetic (TA) and Glucantime (IC₅₀ 9.4 and 21.5 μg/mL, respectively). Both the active fractions remained non-toxic towards human blood erythrocytes and were able to cause membrane permeability and apoptotic induction (using Triton X-100 as a positive control) leading to death of Leishmania parasites. However, both the fractions could not triger significant and persistent ROS generation, compared to hydrogen peroxide used as a positive control. Antilesihmanial activity of the two active fractions might be attributed to the presence of high quantity of tannins and saponins.