Introduction:

Substantial progress has been made in the control of malaria over the past decade. However, transmission of the disease persists in many countries of sub-Saharan Africa (SSA). Concerted efforts are needed to sustain malaria control towards elimination by 2030. Amongst them are strategies that disrupt the development of the malaria parasite within its mosquito vector. Recently, we isolated parthenin, a sesquiterpene lactone like artemisinin, from the invasive Star weed Parthenium hysterophorusand found it to arrest malaria parasite development in the mosquito. Parthenin however, was found to be cytotoxic to humans. This study was designed to investigate the potency and safety profiles of synthetic derivatives of parthenin.

Methods:

Parthenin was isolated from P. hysterophorus by soaking powdered leaves in MeOH at 25oC for 24 hrs; repeated thrice, followed by concentrating under reduced pressure at 40oC and purifying using various chromatographic methods. Thereafter, the structure of parthenin was modified to obtain different derivatives.

Results and conclusion:

We present data on the structures of the pure compounds determined by chemical analysis including Gas Chromatography (GC)-Mass spectrometry (MS), Liquid Chromatography (LC)- Mass spectrometry (MS), Liquid Chromatography Quadrupole Time-of-Flight Mass spectrometry (LC-QTOF-MS) and 1- and 2-D (13C and 1H) Nuclear magnetic resonance (NMR). Establishing the biological activity of the pure compounds is currently underway. Nevertheless, the implication of the structural differences of the compounds and their possible mechanism of action is discussed. We anticipate that these compounds can act as scaffold for developing drugs that can block transmission of malaria parasite via the mosquito host.