Biological Activities of a Macrocyclic Diterpenoid Isolated from the Roots of <i>Jatropha gossypiifolia</i>

Abstract

Background: Extracts of Jatropha gossypiifolia L. (Euphorbiaceae) have been used ethnomedicinally for the treatment of various ailments. The present study was to investigate the biological activity of Jatrophone, a macrocyclic diterpenoid isolated from the roots of J. gossypiifolia. Methods: Phytochemical studies followed by chromatographic separation of the methanol root bark extract led to the isolation of a macrocyclic diterpenoid, identified as jatrophone on the basis of NMR and mass spectra data and by comparison with literature. The isolated compound, jatrophone was evaluated for its antiprotozoal activity against Plasmodium falciparum strains [D6 (chloroquine sensitive) and W2 (chloroquine-resistant)], Leishmania donovani and Trypanosoma brucei. The antimicrobial activity was evaluated against type culture of selected fungi and bacteria. Analgesic activity was investigated using the acetic acidinduced writhing and hot plate model in mice. The cytotoxicity was assessed against VERO cell line (monkey kidney fibroblast) using neural red uptake method. Results: Jatrophone showed significant antiplasmodial and antileishmanial activities with IC₅₀ of 0.55, 0.52 and < 0.4 µg/mL for P. falciparum (D6 strain), P. falciparum (W2 strain) and L. donovani respectively. Compound 1 was highly cytotoxic to VERO cell line with IC₅₀ of 0.43 µg/mL. Jatrophone demonstrated significant analgesic effect with a percentage reduction in acetic acid-induced writhes of 54.03% and 66.35% at 5 and 10 mg/kg respectively. No significant antimicrobial activity was observed against the test organisms. Conclusion: The present study has shown that jatrophone possess antimalarial, antileishmanial, and analgesic activities