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      In vitro inhibition of Plasmodium falciparum by substances isolated from Amazonian antimalarial plants

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          Abstract

          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.

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          Human malaria parasites in continuous culture

          Plasmodium falciparum can now be maintained in continuous culture in human erythrocytes incubated at 38 degrees C in RPMI 1640 medium with human serum under an atmosphere with 7 percent carbon dioxide and low oxygen (1 or 5 percent). The original parasite material, derived from an infected Aotus trivirgatus monkey, was diluted more than 100 million times by the addition of human erythrocytes at 3- or 4-day intervals. The parasites continued to reproduce in their normal asexual cycle of approximately 48 hours but were no longer highly synchronous. The have remained infective to Aotus.
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            Synchronization of Plasmodium falciparum erythrocytic stages in culture.

            Synchronous development of the erythrocytic stages of a human malaria parasite, Plasmodium falciparum, in culture was accomplished by suspending cultured parasites in 5% D-sorbitol and subsequent reintroduction into culture. Immediately after sorbitol treatment, cultures consisted mainly of single and multiple ring-form infections. At the same time, varying degrees of lysis of erythrocytes infected with the more mature stages of the parasite was evident. Approximately 95% of the parasites were in the ring stage of development at 48 and 96 hr after sorbitol treatment-likewise, a high percentage of trophozoite and schizont stages was observed at 24, 72, and 120 hr. D-Mannitol produced similar, selective, lytic effects.
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              Simple and Inexpensive Fluorescence-Based Technique for High-Throughput Antimalarial Drug Screening

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                Author and article information

                Journal
                mioc
                Memórias do Instituto Oswaldo Cruz
                Mem. Inst. Oswaldo Cruz
                Instituto Oswaldo Cruz, Ministério da Saúde (Rio de Janeiro, RJ, Brazil )
                0074-0276
                1678-8060
                June 2007
                : 102
                : 3
                : 359-366
                Affiliations
                [01] Natal RN orgnameUniversidade Federal do Rio Grande do Norte orgdiv1Laboratório de Biologia da Malária e Toxoplasmose Brasil
                [02] Manaus AM orgnameInstituto Nacional de Pesquisas da Amazônia orgdiv1Coordenação de Pesquisas em Produtos Naturais orgdiv2Laboratório de Princípios Ativos da Amazônia Brasil
                [07] Manaus AM orgnameEmbrapa Amazonia Ocidental Brasil
                [08] Manaus AM orgnameUniversidade Estadual do Amazonas Brasil
                [03] Manaus AM orgnameFundação de Medicina Tropical do Amazonas orgdiv1Laboratório da Gerência de Malária Brasil
                [04] Manaus AM orgnameUniversidade Federal do Amazonas Brasil
                [05] Manaus AM orgnameCentro Federal de Educação Tecnológica do Amazonas Brasil
                [06] Manaus AM orgnameCentro Universitário Nilton Lins Brasil
                Article
                S0074-02762007000300016 S0074-0276(07)10200300016
                47415258-35ca-4ae6-8006-04642cc0c534

                This work is licensed under a Creative Commons Attribution 4.0 International License.

                History
                : 15 May 2007
                : 20 February 2007
                Page count
                Figures: 0, Tables: 0, Equations: 0, References: 65, Pages: 8
                Product

                SciELO Brazil

                Categories
                Articles

                aspidocarpine,ellipticine,neosergeolide,Aspidosperma spp,Picrolemma sprucei,Pothomorphe peltata,4-nerolidylcatechol

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