Ethnopharmacological Relevance: Resistance of the parasites to known antimalarial drugs has provided the necessity to find new drugs from natural products against malaria. The aim of the study was to evaluate the in vitro antiplasmodial activity of some plants used by Traditional Medical Practitioners (TMPs) of Prometra and Rukararwe in malaria treatment in Uganda to provide scientific proof of the efficacies claimed by these Herbalists.
Materials And Methods: The air dried samples of Clerodendrum rotundifolium (leaves), Microglossa pyrifolia (leaves), Momordica foetida (leaves) and Zanthoxylum chalybeum (stem bark) used for malaria treatment by TMPs were successively extracted with ethyl acetate, methanol and water to yield twelve extracts. The extracts were tested against the chloroquine-sensitive (NF54) and chloroquine-resistant (FCR3) Plasmodium falciparum strains in vitro using the micro Mark III test which is based on assessing the inhibition of schizont maturation. A compound A was extracted and purified from the stem bark of Z. chalybeum and its structure was identified and confirmed by spectroscopic methods.
Results: Most of the extracts tested (92%) showed an antiplasmodial activity with IC50<50µg/mL. In spite of successive extractions with different solvents, potent anti-plasmodial activity (IC50<5µg/mL) was observed in the ethyl acetate, methanol and aqueous extracts of M. pyrifolia and C. rotundifolium. Preferential enrichments of activity into water (IC50<15µg/mL) and Ethyl acetate (IC50<5µg/mL) were seen in the case of M. foetida and Z. chalybeum respectively. The most active extracts were from C. rotundifolium and M. pyrifolia with IC50 values less than 2µg/mL. Phytochemical analysis of the extracts revealed the presence of saponins, tannins, flavonoids, alkaloids and cardiac glycocides. Fagaramide isolated from Z. chalybeum had a higher activity (IC50 2.85µg/mL) against the chloroquine-resistant strain than against the chloroquine-senstive (IC50 16.6µg/mL) strain used in the study.
Conclusion: The plant extracts analysed in this study presented an average antiplasmodial activity (58%). This study revealed for the first time the antiplasmodial activity of the plant C. rotundofolium. It's the first time the compound fagaramide (N-isobutyl-3-(3,4-methylene dioxyphenyl)-2E-propenamide) has been isolated from Z. chalybeum as one of the compounds that contribute to the activity of this plant against P. falciparum.
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http://dx.doi.org/10.1016/j.jep.2016.03.047 | DOI Listing |
Int J Mol Sci
January 2025
Laboratory of Chemistry of Natural Molecules, Gembloux Agro Bio-Tech, University of Liège, 5030 Gembloux, Belgium.
, a tropical African plant, is traditionally used to treat several diseases, including fever, inflammation, and malaria. Essential oils (EOs) from the plant's leaves, roots, and trunk bark were obtained by hydrodistillation, and their chemical composition was analyzed by gas chromatography-mass spectrometry (GC-MS). The major constituents identified were virdiflorene (18.
View Article and Find Full Text PDFSci Rep
January 2025
Barcelona Institute for Global Health (ISGlobal, Hospital Clínic-University of Barcelona), Rosselló 149-153, Barcelona, 08036, Spain.
We recently characterized the potent antiplasmodial activity of the aggregated protein dye YAT2150, whose presumed mode of action is the inhibition of protein aggregation in the malaria parasite. Using single-dose and ramping methods, assays were done to select Plasmodium falciparum parasites resistant to YAT2150 concentrations ranging from 3× to 0.25× the in vitro IC of the compound (in the two-digit nM range) and performed a cross-resistance assessment in P.
View Article and Find Full Text PDFInt J Pharm
January 2025
Faculty of Pharmacy, Almarisah Madani University, Makassar, Indonesia; Department of Pharmacy and Pharmaceutical Technology, Almarisah Madani University, Makassar, Indonesia. Electronic address:
The combination of the active compounds curcumin and piperine (CP) is effective as an antimalarial; however, the solubility and bioavailability of CP are very low. This study aims to formulate CP in nanoparticles (NP), which are then fabricated into dissolving microneedles (DMN). The NPs were prepared with a concentration ratio of CP-Chitosan-So.
View Article and Find Full Text PDFCurr Top Med Chem
January 2025
Harbin University of Commerce, Harbin, China.
Halogenated natural products are an important class of secondary metabolites that are widely distributed in nature. The presence of halogen atoms usually enhances the pharmacological activity of the compounds. As a result, halogenated natural products have shown promising pharmacological activities in antibacterial, antitumour, anti-inflammatory and antiplasmodial properties, providing a rich resource for the development of new drugs.
View Article and Find Full Text PDFFront Pharmacol
January 2025
Department of Pathology, College of Korean Medicine, Kyung Hee University, Seoul, Republic of Korea.
The natural world is a vast reservoir of exceptionally varied and inventive chemical compositions. Natural products are used as initial compounds to create combinatorial libraries by targeted modifications and then by analyzing their structure-activity connections. This stage is regarded as a crucial milestone in drug discovery and development.
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