Antiplasmodial and Cytotoxic Flavonoids from Pappea capensis (Eckl. & Zeyh.) Leaves

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.

[1]  F. R. Heerden,et al.  Antiplasmodial and Cytotoxic Activities of Extract and Compounds from Ozoroa obovata (Oliv.) R. & A. Fern. var. obovata , 2021, Chemistry & biodiversity.

[2]  N. Tajuddeen,et al.  Antiplasmodial natural products: an update , 2019, Malaria Journal.

[3]  S. Tsang,et al.  Antimalarial Activity of Plant Metabolites , 2018, International journal of molecular sciences.

[4]  Robert W. Snow,et al.  The prevalence of Plasmodium falciparum in sub Saharan Africa since 1900 , 2017, Nature.

[5]  Albert J. Ndakala,et al.  Four Prenylflavone Derivatives with Antiplasmodial Activities from the Stem of Tephrosia purpurea subsp. leptostachya , 2017, Molecules.

[6]  L. Lião,et al.  Phytochemical Analysis and Antimicrobial Activity of Myrcia tomentosa (Aubl.) DC. Leaves , 2017, Molecules.

[7]  Tilahun Teklehaymanot,et al.  Antimalarial medicinal plants used by Gumuz people of Mandura Woreda, Benishangul-Gumuz Regional State, Ethiopia , 2016 .

[8]  E. Bourreau,et al.  Wayanin and guaijaverin, two active metabolites found in a Psidium acutangulum Mart. ex DC (syn. P. persoonii McVaugh) (Myrtaceae) antimalarial decoction from the Wayana Amerindians. , 2016, Journal of ethnopharmacology.

[9]  N. Tajuddeen,et al.  A novel antimicrobial flavonoid from the stem bark of Commiphora pedunculata (Kotschy & Peyr.) Engl. , 2016, Natural product research.

[10]  J. Barbosa-Filho,et al.  Chemical constituents of Cardiospermum corindum L. and their distribution in Sapindaceae , 2014 .

[11]  J. J. Meyer,et al.  In vitro antiplasmodial screening of ethnopharmacologically selected South African plant species used for the treatment of malaria. , 2014, Journal of ethnopharmacology.

[12]  M. Emeje,et al.  Antiplasmodial activity-aided isolation and identification of quercetin-4’-methyl ether in Chromolaena odorata leaf fraction with high activity against chloroquine-resistant Plasmodium falciparum , 2014, Parasitology Research.

[13]  F. Pavan,et al.  Phenolic compounds and antioxidant, antimicrobial and antimycobacterial activities of Serjania erecta Radlk. (Sapindaceae) , 2013 .

[14]  N. Koorbanally,et al.  Antiprotozoal Screening of 60 South African Plants, and the Identification of the Antitrypanosomal Germacranolides Schkuhrin I and II , 2013, Planta Medica.

[15]  A. Ndhlala,et al.  Anti-inflammatory and mutagenic evaluation of medicinal plants used by Venda people against venereal and related diseases , 2013 .

[16]  David J Newman,et al.  Natural products as sources of new drugs over the 30 years from 1981 to 2010. , 2012, Journal of natural products.

[17]  P. Chiba,et al.  Antiplasmodial activity of flavonol quercetin and its analogues in Plasmodium falciparum: evidence from clinical isolates in Bangladesh and standardized parasite clones , 2012, Parasitology Research.

[18]  T. Wells Natural products as starting points for future anti-malarial therapies: going back to our roots? , 2011, Malaria Journal.

[19]  T. Seyama,et al.  Effects of hyperin, isoquercitrin and quercetin on lipopolysaccharide‐induced nitrite production in rat peritoneal macrophages , 2008, Phytotherapy research : PTR.

[20]  K. Saliba,et al.  Common dietary flavonoids inhibit the growth of the intraerythrocytic malaria parasite , 2008, BMC Research Notes.

[21]  R. Bussmann,et al.  Diversity and utilization of antimalarial ethnophytotherapeutic remedies among the Kikuyus (Central Kenya) , 2006, Journal of ethnobiology and ethnomedicine.

[22]  J. Pezzuto,et al.  Evaluation of plants used for antimalarial treatment by the Maasai of Kenya. , 2005, Journal of ethnopharmacology.

[23]  R. Cowling,et al.  On the origin of southern African subtropical thicket vegetation , 2005 .

[24]  R. Perozzo,et al.  Inhibiting activities of the secondary metabolites of Phlomis brunneogaleata against parasitic protozoa and plasmodial enoyl-ACP Reductase, a crucial enzyme in fatty acid biosynthesis. , 2004, Planta medica.

[25]  C. Welch,et al.  The Flavonoid Constituents of Two Polypodium Species (Calaguala) and their Effect on the Elastase Release in Human Neutrophils , 1997, Planta medica.

[26]  R. Piper,et al.  Parasite lactate dehydrogenase as an assay for Plasmodium falciparum drug sensitivity. , 1993, The American journal of tropical medicine and hygiene.

[27]  W. Trager,et al.  Human malaria parasites in continuous culture. , 1976, Science.

[28]  M. Moyo,et al.  Antimicrobial, antioxidant and cytotoxicity of isolated compounds from leaves of Pappea capensis , 2017 .

[29]  A. Hutchings,et al.  Zulu Medicinal Plants: An Inventory , 1996 .

[30]  I. Umadevi,et al.  Chemosystematics of the Sapindaceae , 1991 .