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巴西植物物种中异喹啉生物碱抗疟活性的体外筛选。

In vitro screening for antiplasmodial activity of isoquinoline alkaloids from Brazilian plant species.

作者信息

Fischer Dominique Corinne Hermine, de Amorim Gualda Nilton Carlos, Bachiega Danielle, Carvalho Cyntia Salerno, Lupo Fernanda Nogueira, Bonotto Sonia Valéria, Alves Mariana de Oliveira, Yogi Alvaro, Santi Silvia Maria Di, Avila Priscilla Elisangela, Kirchgatter Karin, Moreno Paulo Roberto Hrihorowitsch

机构信息

Faculdade de Ciências Farmacêuticas, Universidade de São Paulo, Av. Prof. Lineu Prestes 580, Bloco15, 05580-900, São Paulo, SP, Brazil.

出版信息

Acta Trop. 2004 Nov-Dec;92(3):261-6. doi: 10.1016/j.actatropica.2004.08.009.

Abstract

In the search for new antimalarial agents, nine Brazilian plant species were selected, from the Annonaceae (6), Menispermaceae (2) and Siparunaceae (1) families naturally occurring at the cerrado and Atlantic rainforest regions, in order to investigate their in vitro antiplasmodial activity. The ethanol and the alkaloid extracts were tested against K1, chloroquine-resistant, and Palo Alto, chloroquine-sensitive, strains of Plasmodium falciparum. The majority of the alkaloid extracts were more active than the ethanol ones, with IC(50) ranging 0.3-8.2 microg/mL. The crude Guatteria australis alkaloids were the most active against K1 with an IC(50) = 0.3 microg/mL. The most promising total alkaloid fractions for further bioguided isolation are those with the IC(50) < or = 5 microg/mL: G. australis, Cissampelos ovalifolia and Duguetia lanceolata.

摘要

在寻找新型抗疟药物的过程中,从自然生长于塞拉多和大西洋雨林地区的番荔枝科(6种)、防己科(2种)和单心木兰科(1种)中挑选了9种巴西植物物种,以研究它们的体外抗疟原虫活性。用乙醇提取物和生物碱提取物对恶性疟原虫的氯喹抗性K1株和氯喹敏感帕洛阿尔托株进行了测试。大多数生物碱提取物比乙醇提取物活性更强,半数抑制浓度(IC50)范围为0.3 - 8.2微克/毫升。粗制的南方瓜馥木生物碱对K1株活性最强,IC50 = 0.3微克/毫升。对于进一步的生物导向分离而言,最有前景的总生物碱部分是那些IC50≤5微克/毫升的部分:南方瓜馥木、椭圆叶锡生藤和披针叶杜桂。

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