Antileishmanial activity of neo-clerodane diterpenes from Croton echioides

Nowadays, new leishmanicidal drugs are needed and natural products arise as a promising alternative source. Therefore, bioguided fractionation of a hydroethanolic extract from the stem bark of Croton echioides Baill. were conducted based on its antileishmanial activity. Two novel neo-clerodane diter...

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Bibliographic Details
Published in:Natural product research 2022-02, Vol.36 (4), p.925-931
Main Authors: Novello, Cláudio Roberto, Düsman, Elisangela, Balbinot, Rodolfo Bento, de Paula, Jéssica Carreira, Nakamura, Celso Vataru, de Mello, João Carlos Palazzo, Sarragiotto, Maria Helena
Format: Article
Language:English
Subjects:
Antiprotozoal Agents - pharmacology
Bark
Clerodane diterpenes
Croton - chemistry
Croton echioides
Cytotoxicity
Diterpenes
Diterpenes - chemistry
Diterpenes - pharmacology
Diterpenes, Clerodane - chemistry
Diterpenes, Clerodane - pharmacology
Euphorbiaceae
Fractionation
Hexanes
Leishmania amazonensis
Leishmaniasis
Macrophages
Magnetic Resonance Spectroscopy
Molecular Structure
Natural products
NMR
Nuclear magnetic resonance
Selectivity
Stems
Toxicity
Vector-borne diseases
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Summary:Nowadays, new leishmanicidal drugs are needed and natural products arise as a promising alternative source. Therefore, bioguided fractionation of a hydroethanolic extract from the stem bark of Croton echioides Baill. were conducted based on its antileishmanial activity. Two novel neo-clerodane diterpenoids methyl-15,16-epoxy-3,13(16),14-neo-clerodatrien-17,18-dicarboxylate (1) and dimethyl-3-oxo-15,16-epoxy-13(16),14-neo-clerodadien-17,18-dicarboxylate (2) were isolated, as well as four known compounds (3-6) and lupeol, from the hexane fraction. Their structures were established by NMR analysis. The crude extract, fractions and the compounds (1 and 3-6) were evaluated for their in vitro antileishmanial activity and cytotoxicity against macrophages J774A.1. The selectivity index (SI) were calculated. The most active compound against promastigote forms of L. amazonensis was the clerodane diterpene 4, with IC 50 values of 8.3 µM and SI value of 80.9. Our results highlighted stem bark of Croton echioides Baill. as a promising source for the development of a new chemotherapeutic agent to combat leishmaniasis.
ISSN:1478-6419
1478-6427
DOI:10.1080/14786419.2020.1851221