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. 2024 Jul 11:15:1390715.
doi: 10.3389/fphar.2024.1390715. eCollection 2024.

Bioassay-guided isolation of leishmanicidal cucurbitacins from Momordica charantia

Maria Carolina Silva Marques #  1 , Nídia Cristiane Yoshida #  2 , Eduardo Caio Torres-Santos  3 , Fernanda Rodrigues Garcez #  2 , Walmir Silva Garcez #  2
Affiliations

Bioassay-guided isolation of leishmanicidal cucurbitacins from Momordica charantia

Maria Carolina Silva Marques et al. Front Pharmacol. .

Abstract

Introduction: Leishmaniasis, a neglected tropical parasitic disease, is regarded as a major public health problem worldwide. The first-line drugs for leishmaniasis suffer from limitations related to toxicity and the development of resistance in certain parasitic strains. Therefore, the discovery of alternative treatments for leishmaniasis is imperative, and natural products represent a valuable source of potential therapeutic agents.

Methods: The present study aimed at finding new potential antileishmanial agents from the aerial parts of the medicinal plant Momordica charantia. This study was based on bioassay-guided fractionation of the M. charantia extract against promastigotes and amastigotes of Leishmania (Leishmania) amazonensis. The cytotoxicity of the extract, fractions, and isolated compounds were evaluated against peritoneal murine macrophages by employing the MTT assay for assessing cell metabolic activity.

Results: Antileishmanial assay-guided fractionation of the M. charantia extract led to the bioactive cucurbitacin-enriched fraction and the isolation of four bioactive cucurbitacin-type triterpenoids, which exhibited significant antileishmanial activity, with IC50 values between 2.11 and 3.25 μg.mL-1 against promastigote and amastigote forms, low toxicity and selectivity indexes ranging from 8.5 to 17.2.

Conclusion: Our findings demonstrate that the fractions and cucurbitacin-type triterpenoids obtained from the aerial parts of M. charantia are promising natural leishmanicidal candidates.

Keywords: Cucurbitaceae; Leishmania amazonensis; Momordica charantia; cucurbitacin; leishmanicidal activity; neglected tropical disease.

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Conflict of interest statement

The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest.

Figures

FIGURE 1
FIGURE 1
Structures of the isolated compounds obtained from the ethanol extract of aerial parts of Momordica charantia.
FIGURE 2
FIGURE 2
HPLC profile of (A) the ethanol extract of the aerial parts and (B) cucurbitacin-enriched fraction F7 of Momordica charantia. 1: 25-methoxy-3, 7-dihydroxycucurbita-5,23(E)-dien-19-al (7.12 min); 2: 3,7,25-trihydroxycucurbita-5,23(E)-dien-19-al (9.42 min); 3 + 4: 19(R),25-dimethoxy-5-19-epoxycucurbita-6,23(E)-dien-3-ol and 19(R)-methoxy-5-19-epoxycucurbita-6,23(E)-dien-3,25-diol (19.29 min).
See this image and copyright information in PMC

References

    1. Anversa L., Tiburcio M. G. S., Richini-Pereira V. B., Ramirez L. E. (2018). Human leishmaniasis in Brazil: a general review. Rev. Assoc. Méd. Bras. 64 (3), 281–289. 10.1590/1806-9282.64.03.281 - DOI - PubMed
    1. Barrett M. P., Croft S. L. (2012). Management of trypanosomiasis and leishmaniasis. Br. Med. Bull. 104 (1), 175–196. 10.1093/bmb/lds031 - DOI - PMC - PubMed
    1. Basselin M., Robert-Gero M. (1998). Alterations in membrane fluidity, lipid metabolism, mitochondrial activity, and lipophosphoglycan expression in pentamidine-resistant Leishmania. Parasitol. Res. 84, 78–83. 10.1007/s004360050361 - DOI - PubMed
    1. Bhattacharya S., Biswas M., Haldar P. K. (2013). The triterpenoid fraction from Trichosanthes dioica root exhibits in vitro antileishmanial effect against Leishmania donovani promastigotes. Pharmacogn. Res. 5 (2), 109–112. 10.4103/0974-8490.110540 - DOI - PMC - PubMed
    1. Cargnin S. T., Vieira P. deB., Cibulski S., Cassel E., Vargas R. M. F., Montanha J., et al. (2013). Anti-Trichomonas vaginalis activity of Hypericum polyanthemum extract obtained by supercritical fluid extraction and isolated compounds. Parasitol. Int. 62 (2), 112–117. 10.1016/j.parint.2012.10.006 - DOI - PubMed

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