In this study the in vitro antiplasmodial activities of extracts from Cussonia spicata (Araliaceae), Artemisia afra, Vernonia colorata, V. natalensis (Asteraceae), Parinari curatellifolia (Chrysobalanaceae), Clutia hirsuta, Flueggea virosa, (Euphorbiaceae), Adenia gummifera (Passifloraceae) and Hymenodictyon floribundum, (Rubiaceae) were evaluated. The lipophilic extracts from the aerial parts of Artemisia afra and Vernonia colorata proved to be the most active against the chloroquine-sensitive strain PoW and against the chloroquine-resistant clone Dd2 of Plasmodium falciparum. Bioassay-guided fractionation of the extract of A. afra yielded seven flavonoids, from which acacetin, genkwanin and 7-methoxyacacetin showed in vitro activity; the IC(50) values ranged from 4.3 microgram/mL to 12.6 microgram/mL. In addition, several sesquiterpene lactones could be obtained from the most active fractions. Whereas eudesmaafraglaucolide proved to be inactive, the guaianolides 1-desoxy-1alpha-peroxy-rupicolin A-8-O-acetate, 1alpha,4alpha-dihydroxybishopsolicepolide and rupicolin A-8-O-acetate revealed in vitro antiplasmodial activity. Evaluation of V. colorata gained four sesquiterpenes 11beta,13-dihydrovernodalin, vernodalol, 11beta,13-dihydrovernolide and 11beta,13,17,18-tetrahydrovernolide, from which the first two constituents exhibited the strongest antiplasmodial activity (IC(50) values: 1.1-4.8 microgram/mL).
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http://dx.doi.org/10.1002/ptr.1066 | DOI Listing |
Appl Sci (Basel)
January 2024
Department of Microbiology and Medical Zoology, University of Puerto Rico School of Medicine, San Juan 00921, Puerto Rico.
Gracilioether M () and 11,12-dihydrogracilioether M (), two polyketides with a [2(5H)-furanylidene]ethanoate moiety, along with known plakortone G () and its new naturally occurring derivative 9,10-dihydroplakortone G (), were isolated from the Caribbean marine sponge . The structures and absolute configuration of , , and were characterized by analysis of HRESIMS and NMR spectroscopic data, chemical derivatization, and side-by-side comparisons with published NMR data of related analogs. Compounds and and a mixture of and were evaluated for cytotoxicity against MCF-7 human breast cancer cells.
View Article and Find Full Text PDFJ Med Chem
December 2024
Heinrich Heine University Düsseldorf, Faculty of Mathematics and Natural Sciences, Institute of Pharmaceutical and Medicinal Chemistry, Universitätsstr. 1, 40225 Düsseldorf, Germany.
Malaria continues to pose a significant burden on populations in endemic areas and requires innovative treatment options. Here, we report the synthesis and preclinical evaluation of the novel 3-hydroxypropanamidine (HPA) , which shows excellent antiplasmodial activity against drug-sensitive and -resistant strains. Moreover, in various human cell lines, the compound shows no cytotoxicity and excellent parasite selectivity.
View Article and Find Full Text PDFChem Biol Interact
December 2024
National Research Center for Protozoan Diseases, Obihiro University of Agriculture and Veterinary Medicine, Inada-cho, Obihiro, 080-8555, Japan. Electronic address:
This study focused on the synthesis, structural validation, and evaluation of the antiplasmodial efficacy of brachangobinan A (BA) and its enantiomers, (+)-BA and (-)-BA, as potential antimalarial agents. BA, (+)-BA, and (-)-BA were synthesized through chemical processes and validated via advanced spectroscopic techniques. In vitro studies were conducted to assess their efficacy against Plasmodium falciparum strains 3D7 and K1 by determining their half maximal inhibitory concentration (IC) values, cytotoxicity profiles, and selectivity indices.
View Article and Find Full Text PDFFitoterapia
December 2024
National Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, MS 38655, USA; Department of Biomolecular Sciences, Division of Pharmacognosy, School of Pharmacy, University of Mississippi, Oxford, MS 38677, USA. Electronic address:
Brazilian Red Propolis (BRP) is a natural product known for its rich chemical composition and therapeutic potential. This study investigates the phytochemical profile and evaluates the cytotoxic, antiplasmodial, and antimicrobial properties of red propolis extract and its isolated compounds vestitol (1), neovestitol (2), medicarpin (3), 7-O-methylvestitol (4), and oblongifolin B (5). The extract showed selective cytotoxicity against cancer cell lines (IC: 16-39 μg/mL).
View Article and Find Full Text PDFMolecules
November 2024
School of Chemistry and Biochemistry, Georgia Institute of Technology, Atlanta, GA 30332, USA.
Agunmu (ground herbal medicine) is a form of West African traditional medicine consisting of a cocktail of herbs. The goal of this study is to evaluate a formulation of Agunmu made from , , , , and , sold in the open market and commonly used for the treatment of malaria by the locals, for its antimalarial effects and to determine the active principles that may contribute to the antimalarial effect. The ethanolic extract obtained from this formulation (Ag-Iba) was analyzed, using TLC, LC-MS, and Tandem-MS techniques, to determine its phytochemical properties.
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