Abstract

Ethnobotanical surveys indicate that the Masai and Kikuyu in Kenya, the Venda in South Africa, and the Gumuz people of Ethiopia use Pappea capensis for the treatment of malaria. The present study aimed to investigate the phytochemical and antiplasmodial properties of the plant leaves. The bioactive compounds were isolated using chromatographic techniques. The structures were established using NMR, HRMS, and UV spectroscopy. Antiplasmodial activity of P. capensis leaf extract and isolated compounds against chloroquine-sensitive 3D7 P. falciparum was evaluated using the parasite lactate dehydrogenase assay. Cytotoxicity against HeLa (human cervix adenocarcinoma) cells was determined using the resazurin assay. The extract inhibited the viability of Plasmodium falciparum by more than 80% at 50 µg/mL, but it was also cytotoxic against HeLa cells at the same concentration. Chromatographic purification of the extract led to the isolation of four flavonoid glycosides and epicatechin. The compounds displayed a similar activity pattern with the extract against P. falciparum and HeLa cells. The results from this study suggest that the widespread use of P. capensis in traditional medicine for the treatment of malaria might have some merits. However, more selectivity studies are needed to determine whether the leaf extract is cytotoxic against noncancerous cells.

Highlights

  • Malaria continues to cause serious morbidity and mortality, especially in Africa, which accounted for over 90% of the approximately 409,000 global malaria deaths in 2019

  • P. capensis is the only species in the genus Pappea, and epicatechin and quercitrin were previously isolated from the plant leaves [15]

  • Four of the isolated flavonoids from the leaves of P. capensis are flavonol O-glucosides, whereas epicatechin is a monomer of some proanthocyanidin

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Summary

Introduction

Malaria continues to cause serious morbidity and mortality, especially in Africa, which accounted for over 90% of the approximately 409,000 global malaria deaths in 2019. Whether as mixtures or purified compounds, continue to play a leading role in drug discovery, as drug candidates and as inspiration for the design of novel drugs. This influence of natural products is pronounced in the area of anti-infective agents [3]. Plant natural products have historically produced successful antimalarial drugs. The quinoline antimalarials such as chloroquine and primaquine were inspired by quinine, which is obtained from the barks of South American Chinchona plants. Emerging cases of delayed drug response and resistance to artemisinin indicate that the search for new antimalarial agents is an urgent priority

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