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绵毛岩白菜乙醇提取物(根茎)抑制疟原虫的繁殖。

Ethanol extract of Bergenia ciliata (Haw.) Sternb. (rhizome) impedes the propagation of the malaria parasite.

机构信息

Parasitology Laboratory, Department of Zoology, Panjab University, Chandigarh, 160014, India.

University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India.

出版信息

J Ethnopharmacol. 2021 Nov 15;280:114417. doi: 10.1016/j.jep.2021.114417. Epub 2021 Jul 12.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

The increasing resistant cases even against artemisinin-based combination therapy have necessitated the need to develop new antimalarials. Phytomedicinal therapy is a benchmark for malaria in the Himalayan region. As the dialect and traditional variations have been seen along with this, usage of medicinal plant, its portion (shoot and root system) and mode of preparation also varies. There is no scientific evidence available for illustrating the antiplasmodial activity of the rhizomes of Bergenia ciliata (Saxifragaceae), which is known to be an antipyretic (fever akin to malaria), hepato-protective, and also for spleen enlargement.

AIM OF THE STUDY

The present study evaluates the antimalarial activity of ethanol extract of B. ciliata rhizomes (EREBC).

MATERIALS AND METHODS

HPTLC was performed to identify and quantify three marker compounds in EREBC. The in vitro antimalarial activity was evaluated by schizont maturation inhibition assay. MTT assay was employed to test the cytotoxicity of EREBC. Peter's 4-day test and Peters method was employed to discern the suppressive and preventive activity of the extract respectively.

RESULTS

HPTLC analysis revealed the presence of bergenin, epicatechin and gallic acid in the extract. EREBC exhibited considerable inhibition (IC < 5 μg/mL) of schizont maturation of both RKL-9 and MRC-2 strains of P. falciparum. EREBC was non-toxic to both HeLa cells and normal dermal fibroblasts (CC > 1000 μg/mL). The selectivity index was > 200 for both strains. Acute toxicity of EREBC was > 4 g/kg. EREBC exhibited considerable in vivo suppressive activity with 96.48% inhibition at 500 mg/kg in comparison to chloroquine (96.08%). The ED of the extract was < 50 mg/kg. No mortality was evident in mice administered with different doses of EREBC (50-500 mg/kg) throughout the follow up period of 28 days. EREBC exhibited safety to liver and kidney function of mice as observed from biochemical analysis.

CONCLUSION

Overall, the study illustrates the marked efficacy and potential of EREBC as an antimalarial agent with bergenin, epicatechin and gallic acid its major constituents, which played a pivotal role in the generation of the immune response.

摘要

民族药理学相关性

即使是基于青蒿素的联合疗法,耐药病例也在不断增加,这使得有必要开发新的抗疟药物。植物疗法是喜马拉雅地区疟疾的基准。由于存在方言和传统差异,药用植物的使用、其部分(茎和根系)和制备方式也有所不同。目前还没有科学证据表明,贝加尼亚·西里亚特(虎耳草科)的根茎具有抗疟原虫活性,而众所周知,这种根茎具有退热(类似于疟疾的发热)、保肝和脾肿大的作用。

研究目的

本研究评估了贝加尼亚·西里亚特根茎乙醇提取物(EREBC)的抗疟活性。

材料和方法

采用 HPTLC 鉴定和定量 EREBC 中的三种标记化合物。通过裂殖体成熟抑制试验评估体外抗疟活性。采用 MTT 试验检测 EREBC 的细胞毒性。采用彼得氏 4 天试验和彼得氏法分别检测提取物的抑制和预防活性。

结果

HPTLC 分析表明,提取物中存在 Bergenin、表儿茶素和没食子酸。EREBC 对 RKL-9 和 MRC-2 株疟原虫裂殖体成熟表现出显著的抑制作用(IC < 5 μg/mL)。EREBC 对 HeLa 细胞和正常皮肤成纤维细胞均无毒性(CC > 1000 μg/mL)。两种菌株的选择性指数均> 200。急性毒性试验中,EREBC 剂量> 4 g/kg 时无死亡。与氯喹(96.08%)相比,EREBC 在 500 mg/kg 时表现出显著的体内抑制活性,抑制率为 96.48%。该提取物的 ED 低于 50 mg/kg。在 28 天的随访期间,给予不同剂量 EREBC(50-500 mg/kg)的小鼠均未出现死亡。生化分析表明,EREBC 对小鼠的肝肾功能无影响。

结论

综上所述,该研究表明,EREBC 作为一种抗疟药物具有显著的疗效和潜力,其主要成分 Bergenin、表儿茶素和没食子酸在免疫反应的产生中发挥了关键作用。

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