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印度尼西亚传统上用于治疗疟疾的叶下珠草药提取物的体外和体内抗疟活性及细胞毒性。

In vitro and in vivo antiplasmodial activity and cytotoxicity of extracts of Phyllanthus niruri L. herbs traditionally used to treat malaria in Indonesia.

作者信息

Sholikhah Eti Nurwening, Wahyuono Subagus

机构信息

Department of Pharmacology and Toxicology, Faculty of Medicine, Gadjah Mada University, Yogyakarta, Indonesia.

出版信息

Southeast Asian J Trop Med Public Health. 2007 Jul;38(4):609-15.

Abstract

In endemic areas where malaria is prevalent, medicinal plants are often used to treat malaria. This study was conducted to evaluate the in vitro and in vivo antiplasmodial activity and cytotoxicity of extracts of meniran (Phyllanthus niruri L.) herb traditionally used to treat malaria in Indonesia. Three extracts viz aqueous, methanolic and chloroformic extracts were obtained by maceration of the herbs. A radioactive method was used to evaluate the in vitro antiplasmodial activity of the extracts on chloroquine-resistant (FCR-3) and chloroquine-sensitive (D-10) strains of Plasmodium falciparum. In vitro antiplasmodial activity was expressed by the concentration inhibiting 50% of parasite growth (IC50). Cytotoxicity was estimated on Hela cells and the Cytotoxicity Index (CI = IC50 on HeLa cells/IC50 on FCR-3 strain) was calculated to evaluate the safety of tested extracts. A standard 4-day test on P berghei infected mice was used to evaluate the in vivo antiplasmodial activity of the extracts showing strong in vitro antiplasmodial activity, for both the methanolic and aqueous extracts. The in vivo antiplasmodial activity was expressed by the dose inhibiting 50% of parasite growth (ED50). The IC50 values obtained for these extracts against P. falciparum ranged from 2.3 to 202.4 microg/ml. The methanolic extract was the most active in vitro extract with an IC50 that ranged from 2.3 to 3.9 microg/ml and a CI that ranged from 41.3 to 57.5. This was also the most in vivo active extract with an ED50 of 9.1 mg/kg/d. Further study will be conducted to isolate and purify active compounds presented in the methanolic extract.

摘要

在疟疾流行的 endemic 地区,药用植物常被用于治疗疟疾。本研究旨在评估印尼传统上用于治疗疟疾的叶下珠(Phyllanthus niruri L.)草药提取物的体外和体内抗疟活性及细胞毒性。通过对草药进行浸渍获得了三种提取物,即水提取物、甲醇提取物和氯仿提取物。采用放射性方法评估提取物对氯喹抗性(FCR - 3)和氯喹敏感(D - 10)恶性疟原虫菌株的体外抗疟活性。体外抗疟活性用抑制 50%寄生虫生长的浓度(IC50)表示。在 Hela 细胞上评估细胞毒性,并计算细胞毒性指数(CI = Hela 细胞上的 IC50/FCR - 3 菌株上的 IC50)以评估受试提取物的安全性。对感染伯氏疟原虫的小鼠进行标准的 4 天试验,以评估甲醇提取物和水提取物中显示出强体外抗疟活性的提取物的体内抗疟活性。体内抗疟活性用抑制 50%寄生虫生长的剂量(ED50)表示。这些提取物对恶性疟原虫的 IC50 值范围为 2.3 至 202.4 μg/ml。甲醇提取物是体外活性最强的提取物,IC50 范围为 2.3 至 3.9 μg/ml,CI 范围为 41.3 至 57.5。它也是体内活性最强的提取物,ED50 为 9.1 mg/kg/d。将进一步开展研究以分离和纯化甲醇提取物中的活性化合物。

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