de Andrade-Neto Valter F, Pohlit Adrian M, Pinto Ana Cristina S, Silva Ellen Cristina C, Nogueira Karla L, Melo Márcia R S, Henrique Marycleuma C, Amorim Rodrigo C N, Silva Luis Francisco R, Costa Mônica R F, Nunomura Rita C S, Nunomura Sergio M, Alecrim Wilson D, Alecrim M das Graças C, Chaves F Célio M, Vieira Pedro Paulo R
Laboratório de Biologia da Malária e Toxoplasmose, Universidade Federal do Rio Grande do Norte, Natal, RN, Brasil.
Mem Inst Oswaldo Cruz. 2007 Jun;102(3):359-65. doi: 10.1590/s0074-02762007000300016.
In the present study, a quassinoid, neosergeolide, isolated from the roots and stems of Picrolemma sprucei (Simaroubaceae), the indole alkaloids ellipticine and aspidocarpine, isolated from the bark of Aspidosperma vargasii and A. desmanthum (Apocynaceae), respectively, and 4-nerolidylcatechol, isolated from the roots of Pothomorphe peltata (Piperaceae), all presented significant in vitro inhibition (more active than quinine and chloroquine) of the multi-drug resistant K1 strain of Plasmodium falciparum. Neosergeolide presented activity in the nanomolar range. This is the first report on the antimalarial activity of these known, natural compounds. This is also the first report on the isolation of aspidocarpine from A. desmanthum. These compounds are good candidates for pre-clinical tests as novel lead structures with the aim of finding new antimalarial prototypes and lend support to the traditional use of the plants from which these compounds are derived.
在本研究中,从苦木科植物秘鲁苦木的根和茎中分离得到的一种苦木素类化合物新蛇床内酯,分别从夹竹桃科植物瓦氏白坚木和毛叶白坚木的树皮中分离得到的吲哚生物碱椭圆玫瑰树碱和阿朴长春胺酸,以及从胡椒科植物盾叶胡椒的根中分离得到的4-橙花叔基儿茶酚,均对恶性疟原虫多药耐药K1株表现出显著的体外抑制作用(比奎宁和氯喹更具活性)。新蛇床内酯在纳摩尔范围内呈现活性。这是关于这些已知天然化合物抗疟活性的首次报道。这也是首次从毛叶白坚木中分离得到阿朴长春胺酸的报道。这些化合物作为新型先导结构,是临床前试验的良好候选物,旨在寻找新的抗疟原型,并为这些化合物来源植物的传统用途提供了支持。