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巴西大西洋雨林茜草科Psychotria 属植物的抗分枝杆菌活性和生物碱研究。

Antimycobacterial activity and alkaloid prospection of Psychotria species (Rubiaceae) from the Brazilian Atlantic Rainforest.

机构信息

Laboratório de Biologia Celular e Tecidual, Centro de Biociências e Biotecnologia, Universidade Estadual do Norte Fluminense Darcy Ribeiro, Campos dos Goytacazes, RJ, Brazil.

出版信息

Planta Med. 2011 Jun;77(9):964-70. doi: 10.1055/s-0030-1250656. Epub 2011 Jan 17.

DOI:10.1055/s-0030-1250656
PMID:21243585
Abstract

Ten Psychotria species were collected in two fragments of Atlantic Forest in Rio de Janeiro: Psychotria pubigera (P1A and B), P. ruelliifolia (P2), P. suterela (P3), P. stachyoides (P4), P. capitata (P5), P. glaziovii (P6), P. leiocarpa (P7), P. nuda (P8), P. racemosa (P9) and P. vellosiana (P10). Ethanol extracts of these species were evaluated for their antimycobacterial activity, in an attempt to find new antituberculosis agents. Psychotria pubigera (P1A), P. ruelliifolia (P2) and P. stachyoides (P4) were the most active against Mycobacterium. The anti-inflammatory potential of these extracts was also evaluated in vitro to learn if they inhibit nitric oxide (NO) production in macrophages and if they have free-radical scavenging properties, because inflammation is a severe problem caused by tuberculosis, especially when the infection is from M. bovis or M. tuberculosis. Psychotria suterela (P3), P. stachyoides (P4) and P. capitata (P5) were the most active in inhibiting macrophage NO production but they were not the most antioxidant species. This suggests that NO inhibitory activity is not due to the scavenging of NO generated but due to a specific inhibition of iNOS activity or expression. In addition, cytotoxicity was tested in the macrophages (the host cells of the Mycobacterium) and it was verified that the extracts selectively killed the bacteria and not the host cells. When analyzing antimycobacterial, cytotoxicity and NO inhibitory activities in combination, P. stachyoides (P4) was the most promising anti-TB extract tested. Further, indol alkaloids were detected in P. suterela and P. nuda, and 5,6-dihydro-β-carboline alkaloids in all of the species studied, with the highest amounts found in P. capitata and P. racemosa.

摘要

10 种Psychotria 物种被收集于里约热内卢的两个大西洋森林片段中:Psychotria pubigera(P1A 和 B)、P. ruelliifolia(P2)、P. suterela(P3)、P. stachyoides(P4)、P. capitata(P5)、P. glaziovii(P6)、P. leiocarpa(P7)、P. nuda(P8)、P. racemosa(P9)和 P. vellosiana(P10)。评估这些物种的乙醇提取物对分枝杆菌的抗微生物活性,以寻找新的抗结核药物。Psychotria pubigera(P1A)、P. ruelliifolia(P2)和 P. stachyoides(P4)对分枝杆菌最为活跃。还评估了这些提取物的抗炎潜力,以了解它们是否抑制巨噬细胞中一氧化氮(NO)的产生,以及它们是否具有清除自由基的特性,因为炎症是由结核引起的严重问题,尤其是当感染来自牛分枝杆菌或结核分枝杆菌时。Psychotria suterela(P3)、P. stachyoides(P4)和 P. capitata(P5)在抑制巨噬细胞中 NO 的产生方面最为活跃,但它们并不是抗氧化能力最强的物种。这表明 NO 抑制活性不是由于清除生成的 NO,而是由于对 iNOS 活性或表达的特定抑制。此外,在巨噬细胞(分枝杆菌的宿主细胞)中测试了细胞毒性,并证实提取物选择性地杀死细菌而不是宿主细胞。在分析抗分枝杆菌、细胞毒性和 NO 抑制活性的综合作用时,P. stachyoides(P4)是测试的最有前途的抗结核提取物。此外,在 P. suterela 和 P. nuda 中检测到吲哚生物碱,在所有研究的物种中检测到 5,6-二氢-β-咔啉生物碱,在 P. capitata 和 P. racemosa 中含量最高。

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