Introduction ! Natural products and malaria Malaria remains one of the most prevalent infec- tious diseases worldwide and is, therefore, a glob- al health problem despite substantial efforts to control the disease over the past few decades. Ap- proximately 3.3 billion people are at risk, and 250 million cases each year were reported in the peri- od 2006–2008, primarily in Africa [1]. In the Americas, malaria transmission occurs in 21 countries. P. vivax caused 77 % of all cases reported in 2008, but P. falciparum was responsible for al- most 100 % of all cases in Haiti and the Dominican Republic [1]. Brazil reported the highest number of malaria cases (603 532) in the region in 2005, primarily in the Brazilian Legal Amazon Region, where 10–15% of the population is at risk. Brazil was among the 30 highest-burden countries for malaria [2]. However, a decrease of approximately 25 % in the number of reported cases has been re- corded since 2006 [3, 4]. Historically, plants have had a remarkable role in therapeutics and were the principal source of drugs until the 19th century. Quinine, isolated in 1820, from Cinchona species (Rubiaceae), was the first antimalarial drug introduced in chemother- apy and remained the only clinical weapon until the 1940s, when chloroquine, a synthetic 4-ami- noquinoline, became available. Efficient and inex- pensive, chloroquine was widely used until the 1960s, when resistance to the drug by P. falcipa- rum became widespread in the malaria-endemic countries, causing a strong increase in mortality rates. The antimalarial drugs in current use are ar- temisinin, the active compound from Artemisia annua L. (Asteraceae), a traditional plant used for millennia in China, and its semisynthetic deriva- tives artemether, artesunate, and arteether [5]. Artemisinins are currently the most effective drugs for antimalarial chemotherapy and have been globally adopted for the treatment of P. falci- parum malaria. The most recently introduced antimalarial drug is atovaquone, a synthetic naphthoquinone based on lapachol. Lapachol, a prenylnaphtoquinone, was first isolated from Ta- bebuia impetiginosa (Mart. ex DC.) Standl. (synon. T. avellanedeae Lor. ex Griseb.), a South American representative of the Bignoniaceae [6]. The emergence of P. falciparum strains resistant to artemisinin and its derivatives would cause a re- surgence of human malaria to high levels in many Abstract ! Several plant species belonging to the genus Aspi- dosperma are traditionally used in Brazil and oth- er Meso- and South American countries for the treatment of malaria and fevers. These traditional uses were motivation for this review. A literature survey completed for this review has identified scientific bibliographical references to the use of 24 Aspidosperma species to treat malaria/fevers and to 19 species that have had their extracts and/or alkaloids evaluated, with good results, for in vitro and/or in vivo antimalarial activity. Indole alkaloids are typical constituents of Aspidosperma species. However, only 20 out of more than 200 known indole alkaloids isolated from this genus have been assayed for antimalarial activity. These data support the potential of Aspidosperma spe- cies as sources of antimalarials and the impor- tance of research aimed at validating their use in the treatment of human malaria. * For Part I see [48], for Part II see [36]. Part of RCP Doctor- ate Thesis at PPGCF, UFMG, Belo Horizonte, MG, Brazil. ** All authors contributed equally to this article. Aspidosperma Species as Sources of Antimalarials. Part III. A Review of Traditional Use and Antimalarial Activity* Authors Renata Cristina de Paula 1 **, Maria Fâni Dolabela 2 **, Alaíde Braga de Oliveira 1 ** Affiliations 1 Departamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil 2 Departamento de Farmácia, ICS, Universidade Federal do Pará, Belém, PA, Brazil Key words l " Aspidosperma spp. l " Apocynaceae l " malaria l " Plasmodium falciparum l " antimalarial activity received August 18, 2013 revised January 10, 2014 accepted January 11, 2014 Bibliography DOI http://dx.doi.org/ 10.1055/s-0034-1368168 Published online March 3, 2014 Planta Med 2014; 80: 378–386 © Georg Thieme Verlag KG Stuttgart · New York · ISSN 0032‑0943 Correspondence Alaíde Braga de Oliveira Departamento de Produtos Farmacêuticos Faculdade de Farmácia Universidade Federal de Minas Gerais Av. Antônio Carlos, 6.627 31270–901 Belo Horizonte, MG Brazil Phone: + 55 31 34 09 69 50 Fax: + 55 31 34 41 55 75 alaide.braga@pq.cnpq.br 378 de Paula RC et al. Aspidosperma Species as … Planta Med 2014; 80: 378–386 Reviews This document was downloaded for personal use only. Unauthorized distribution is strictly prohibited.