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Background  Studies have shown that the barks and roots of some Apocynaceae species have anticancer and antimalarial properties. In this study, leaf extracts of five selected species of Apocynaceae used in traditional medicine ( Alstonia angustiloba ,  Calotropis gigantea ,  Dyera costulata ,  Kopsia fruticosa  and  Vallaris glabra ) were assessed for antiproliferative (APF) and antiplasmodial (APM) activities, and analysed for total alkaloid content (TAC), total phenolic content (TPC) and radical-scavenging activity (RSA). As  V. glabra  leaf extracts showed wide spectrum APF and APM activities, they were further screened for saponins, tannins, cardenolides and terpenoids.    Methods  APF and APM activities were assessed using the sulphorhodamine B and lactate dehydrogenase assays, respectively. TAC, TPC and RSA were analysed using Dragendorff precipitation, Folin-Ciocalteu and DPPH assays, respectively. Screening for saponins, tannins, cardenolides and terpenoids were conducted using the frothing, ferric chloride, Kedde and vanillin-H 2 SO 4  tests, respectively.    Results  Leaf extracts of  A. angustiloba ,  C. gigantea  and  V. glabra  displayed positive APF activity. Dichloromethane (DCM) extract of  C. gigantea , and DCM and DCM:MeOH extracts of  V. glabra  showed strong APF activity against all six human cancer cell lines tested. DCM extract of  A. angustiloba  was effective against three cancer cell lines. Against MCF-7 and MDA-MB-231 cell lines, DCM extract of  C. gigantea  was stronger than standard drugs of xanthorrhizol, curcumin and tamoxifen. All five species were effective against K1 strain of  Plasmodium falciparum  and three species ( C. gigantea, D. costulata and K. fruticosa ) were effective against 3D7 strain. Against K1 strain, all four extracts of  V. glabra  displayed effective APM activity. Extracts of  D. costulata  were effective against 3D7 strain. Selectivity index values of extracts of  A. angustiloba ,  C. gigantea  and  V. glabra  suggested that they are potentially safe for use to treat malaria. Extracts of  K. fruticosa  had the highest TAC while  D. costulata  had the highest TPC and RSA. Phytochemical screening of extracts of  V. glabra  also showed the presence of terpenoids, tannins and saponins.    Conclusions  Leaf extracts of  C. gigantea  and  V. glabra  showed great promise as potential candidates for anticancer drugs as they inhibited the growth of all six cancer cell lines. Against K1 strain of  P. falciparum , all four extracts of  V. glabra  displayed effective APM activity. The wide spectrum APF and APM activities of  V. glabra  are reported for the first time and this warrants further investigation into its bioactive compounds.

Assessment of antiproliferative and antiplasmodial activities of five selected Apocynaceae species