Abstract

Traditional medicine caters for about 80% of the health care needs of many rural populations around the world, especially in developing countries. In addition, plant-derived compounds have played key roles in drug discovery. Malaria is currently a public health concern in many countries in the world due to factors such as chemotherapy faced by resistance, poor hygienic conditions, poorly managed vector control programmes and no approved vaccines. In this review, an attempt has been made to assess the value of African medicinal plants for drug discovery by discussing the anti-malarial virtue of the derived phytochemicals that have been tested by in vitro and in vivo assays. This survey was focused on pure compounds derived from African flora which have exhibited anti-malarial properties with activities ranging from “very active” to “weakly active”. However, only the compounds which showed anti-malarial activities from “very active” to “moderately active” are discussed in this review. The activity of 278 compounds, mainly alkaloids, terpenoids, flavonoids, coumarines, phenolics, polyacetylenes, xanthones, quinones, steroids, and lignans have been discussed. The first part of this review series covers the activity of 171 compounds belonging to the alkaloid and terpenoid classes. Data available in the literature indicated that African flora hold an enormous potential for the development of phytomedicines for malaria.

Highlights

  • Malaria is an infectious disease with ravaging effects in the world

  • Some of the compounds have been isolated from plants reputed to have a long history of usage in African traditional medicine (ATM), inferring that knowledge from ATM could be very useful in drug discovery efforts from African medicinal plants

  • This calls for the need to develop the necessary applications required to turn acquired knowledge on Natural product (NP) derived from African medicinal plants into concrete applications in phytomedicine, within an industrial setting

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Summary

Background

Malaria is an infectious disease with ravaging effects in the world. The World Health Organization (WHO) has published statistics which reveal that half the world’s population is at risk of malaria and that one to two million annual deaths can be attributed to malaria alone [1,2]. Even though nitidine is mostly known for its potential anticancer properties, the investigations of Gakunju et al showed the alkaloidal extract of the roots of this plant to have high activity against the chloroquine-resistant K39 strain of P. falciparum, with an IC50 value of 0.04 μg mL-1. Bioassay-guided fractionation of this extract yielded the active compound, 3-hydroxy-20(29)-lupen-28-ol (154), Figure 19, which exhibited good anti-plasmodial activity (IC50 of 3.2 μg mL-1), when tested against a chloroquine-susceptible malarial strain (D10). Bioassay-guided fractionation of stem bark of the plant extract, using the parasite lactate dehydrogenase assay and multi-resistant strain of P. falciparum (K1) for assessing the in vitro anti-malarial activity led to the isolation of emodin and lupeol (161). Compounds and both showed high cytotoxicity whereas showed a better selectivity index

Conclusions
Findings
73. Kiplimo JJ
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