Bioassay-guided fractionation of the EtOH extract of the stem bark of Funtumia elastica resulted in the isolation of four steroidal alkaloids, holarrhetine (1), conessine (2), holarrhesine (3) and isoconessimine (4). Their structures were determined on the basis of 1D- and 2D-NMR techniques and mass spectrometry. Compounds 1-4 exhibited in vitro antiplasmodial activity against the chloroquine-resistant strain FcB1 of Plasmodium falciparum with IC50 values ranging from 0.97 to 3.39 microM. They showed weak cytotoxicity against a rat cell line L-6 with IC50 values ranging from 5.13 to 36.55 microM.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2005.03.021DOI Listing

Publication Analysis

Top Keywords

antiplasmodial activity
8
steroidal alkaloids
8
funtumia elastica
8
ic50 values
8
values ranging
8
isolation characterization
4
characterization antiplasmodial
4
activity steroidal
4
alkaloids funtumia
4
elastica preuss
4

Similar Publications

, 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 PDF

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 PDF

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 PDF

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 PDF

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.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!