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Antiprotozoal Compounds from Urolepis hecatantha (Asteraceae).

ABSTRACT: The dewaxed dichloromethane extract of Urolepis hecatantha and the compounds isolated from it were tested for their in vitro activity on Trypanosoma cruzi epimastigotes and Leishmania infantum promastigotes. The extract of U. hecatantha showed activity against both parasites with IC₅₀ values of 7?µg/mL and 31?µg/mL, respectively. Fractionation of the dichloromethane extract led to the isolation of euparin, jaceidin, santhemoidin C, and eucannabinolide. The sesquiterpene lactones eucannabinolide and santhemoidin C were active on T. cruzi with IC₅₀ values of 10?±?2?µM (4.2?µg/mL) and 18?±?3?µM (7.6?µg/mL), respectively. Euparin and santhemoidin C were the most active on L. infantum with IC₅₀ values of 18?±?4?µM (3.9?µg/mL) and 19?±?4?µM (8.0?µg/mL), respectively. Eucannabinolide has also shown drug-like pharmacokinetic and toxicity properties.

SUBMITTER: Elso OG

PROVIDER: S-EPMC7895558 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature

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Antiprotozoal Compounds from Urolepis hecatantha (Asteraceae).

Elso Orlando G OG Clavin Maria M Hernandez Natalia N Sgarlata Tomás T Bach Hernán H Catalan César A N CAN Aguilera Elena E Alvarez Guzman G Sülsen Valeria P VP

Evidence-based complementary and alternative medicine : eCAM 20210211

The dewaxed dichloromethane extract of Urolepis hecatantha and the compounds isolated from it were tested for their in vitro activity on Trypanosoma cruzi epimastigotes and Leishmania infantum promastigotes. The extract of U. hecatantha showed activity against both parasites with IC50 values of 7 µg/mL and 31 µg/mL, respectively. Fractionation of the dichloromethane extract led to the isolation of euparin, jaceidin, santhemoidin C, and ...[more]

PMID: 33628303

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Project description:BACKGROUND:Sphaeralcea angustifolia (Malvaceae) is extensively used in Mexican traditional medicine for the treatment of gastrointestinal disorders such as diarrhea and dysentery. OBJECTIVE:The current study was to validate the traditional use of S. angustifolia for the treatment of diarrhea and dysentery on biological grounds using in vitro antiprotozoal activity and computational experiments. MATERIALS AND METHODS:The ethanol extract, subsequent fractions, flavonoids, phenolic acids, and a sterol were evaluated on Entamoeba histolytica and Giardia lamblia trophozoites. Moreover, molecular docking studies on tiliroside were performed; it was tested for its affinity against pyruvate:ferredoxin oxidoreductase (PFOR) and fructose-1,6-bisphosphate aldolase (G/FBPA), two glycolytic enzymes of anaerobic protozoa. RESULTS:Bioassay-guided fractionation of extract of the aerial parts of S. angustifolia gives tiliroside and apigenin, caffeic acid, protocatechuic acid, and β-sitosterol. The in vitro antiprotozoal assay showed that tiliroside was the most potent antiprotozoal compound on both protozoa with 50% inhibitory concentration values of 17.5 μg/mL for E. histolytica and 17.4 μg/mL for G. lamblia. Molecular docking studies using tiliroside showed its probable antiprotozoal mechanism with PFOR and G/FBPA. In both cases, tiliroside showed high affinity and inhibition constant theoretic for PFOR (lowest free binding energy from -9.92 kcal/mol and 53.57 μM, respectively) and G/FBPA (free binding energy from -7.17 kcal/mol and 55.5 μM, respectively), like to metronidazole, revealing its potential binding mode at molecular level. CONCLUSION:The results suggest that tiliroside seems to be a potential antiprotozoal compound responsible for antiamoebic and antigiardial activities of S. angustifolia. Its in vitro antiprotozoal activities are in good agreement with the traditional medicinal use of S. angustifolia in gastrointestinal disorders such as diarrhea and dysentery. SUMMARY:Bioassay-guided fractionation of extract of the aerial parts of S. angustifolia gives: tiliroside and apigenin, caffeic acid, protocatechuic acid) and β-sitosterol. The in vitro antiprotozoal assay showed that tiliroside was the most potent antiprotozoal compound on both protozoa with IC50 values of 17.5 mg/mL for E. histolytica and 17.4 μg/mL for G. lamblia. Molecular docking studies using tiliroside showed its probable antiprotozoal mechanism with PFOR and G/FBPA. In both cases tiliroside showed high affinity and inhibition constant theoretic for PFOR (lowest free binding energy from -9.92 kcal/mol and 53.57 mM, respectively) and G/FBPA (free binding energy from -7.17 kcal/mol, respectively and 55.5 μM), like to metronidazole, revealing its potential binding mode at molecular level. The results suggest that tiliroside seems to be a potential antiprotozoal compound responsible for antiamoebic and antigiardial activities of Sphaeralcea angustifolia. Abbreviations Used: PFOR: Pyruvate:ferredoxin oxidoreductase; G/FBPA: Fructose 1,6 bisphosphate aldolase.

Dataset Information

Antiprotozoal Compounds from Urolepis hecatantha (Asteraceae).

Publications

Antiprotozoal Compounds from <i>Urolepis hecatantha</i> (Asteraceae).

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