Antiprotozoal Activity Against Entamoeba hystolitica and Giardia lamblia of Cyclopeptides Isolated from Annona diversifolia Saff

• Published in: Molecules (Basel, Switzerland) Switzerland), 2024-11, Vol.29 (23), p.5636
• Main Authors: Murrieta-Dionicio, Ulises, Calzada, Fernando, Barbosa, Elizabeth, Valdés, Miguel, Reyes-Trejo, Benito, Zuleta-Prada, Holber, Guerra-Ramírez, Diana, Del Río-Portilla, Federico
• Format: Article
• Language: English
• Subjects: Aldose reductase; Amino acids; Annona - chemistry; antiprotozoal activity; Antiprotozoal Agents - chemistry; Antiprotozoal Agents - isolation & purification; Antiprotozoal Agents - pharmacology; cherimolacyclopeptide D; cyclopeptides; Entamoeba histolytica - drug effects; Enzymes; Flavonoids; Giardia lamblia - drug effects; Health aspects; Herbal medicine; Humans; Metronidazole; molecular docking; Molecular Docking Simulation; Molecular weight; Monosaccharides; NMR; Nuclear magnetic resonance spectroscopy; Peptides, Cyclic - chemistry; Peptides, Cyclic - isolation & purification; Peptides, Cyclic - pharmacology; Plant Extracts - chemistry; Plant Extracts - pharmacology; Protozoa; Scientific imaging; Seeds; squamines C and D; Sugars; Tropical diseases
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules29235636

Diseases caused by intestinal parasites such as protozoa represent a worldwide problem mainly for developing countries. From morbidity in different groups of people to cases of mortality in children and/or immunocompromised patients. In addition to the above, there is growing resistance to the drugs used in the treatment of these diseases, as well as undesirable side effects in patients. Therefore, there is an interest in the search for new alternatives for the base and/or development of new drugs with antiparasitic activities without harmful effects. In this sense, natural products offer to be a diverse source of compounds with biological activities. In this work, we describe the isolation and elucidation by 1D and 2D NMR spectroscopy of three cyclopeptides obtained from seeds of Saff.: cherimolacyclopeptide D ( ), squamin D ( ), and squamin C ( ). The fractions enriched in cyclopeptides, as well as a pure compound ( ), showed antiprotozoal activity against Schaudinn and Kunstler in vitro assays, with values of IC = 3.49 and 5.39 μg mL , respectively. The molecular docking study revealed that has a strong interaction with targets used, including aldose reductase and PFOR enzymes. The antiprotozoal activity of cherimolacyclopeptide D is reported for the first time in this study.