Sesquiterpenoids and flavonoids from Inula viscosa induce programmed cell death in kinetoplastids.

Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie
Ikrame ZeoukJosé E Piñero

Abstract

Neglected tropical diseases such as leishmaniasis and American trypanosomiasis represent an increasing health problem. Current treatments are not satisfactory which remains an urgent need for novel, cheap and safe chemotherapies. In the course of our ongoing search for new potential anti-protozoal agents, this study aimed to perform a bio-guided fractionation of Inula viscosa (Asteraceae) using in vitro assays against three strains of Leishmania and Trypanosma genus. Eight known compounds were identified from the ethanolic extract of leaves, sesquiterpenoids (3 and 4) and flavonoids (5 and 6) were characterized as the main bioactive constituents. Sesquiterpene lactones 3 and 4 (IC50 values between 4.99 and 14.26 μM) showed promising antiparasitic activity against promastigotes of L. donovani, L. amazonensis and epimastigotes of T. cruzi. Their structures were successfully characterized by spectroscopic techniques including 1D and 2D NMR experiments. Furthermore, the main bioactive compounds 4, 5 and 6 displayed higher potency (IC50 values between 0.64 and 2.13 μM) against amastigotes of L. amazonensis than miltefosine (IC50 3.11 μM), and a low toxicity on macrophages cell line (SI > 45). The analysis of structure-activity relat...Continue Reading

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Citations

Mar 24, 2021·Antimicrobial Agents and Chemotherapy·Marvin J NúñezIsabel L Bazzocchi
Jul 3, 2021·Pharmaceuticals·Carlos J Bethencourt-EstrellaJosé E Piñero

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