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评价几种印度尼西亚药用植物提取物的抗疟原虫和抗弓形虫活性。

Evaluation of the antiplasmodial and anti-Toxoplasma activities of several Indonesian medicinal plant extracts.

机构信息

National Research Center for Protozoan Diseases, Obihiro University of Agriculture and Veterinary Medicine, Inada-cho, Obihiro, Hokkaido, 080-8555, Japan.

Department of Life, Food, and Environmental Sciences, Faculty of Agriculture, Yamagata University, Wakaba-machi 1-23, Tsuruoka, Yamagata, 997-8555, Japan; Department of Pharmaceutical Biology, Faculty of Pharmacy, Universitas Padjadjaran, Jatinangor, Sumedang, West Java, 45363, Indonesia.

出版信息

J Ethnopharmacol. 2024 Sep 15;331:118269. doi: 10.1016/j.jep.2024.118269. Epub 2024 Apr 30.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Malaria, caused by Plasmodium parasites, remains a significant global health challenge, particularly in tropical and subtropical regions. At the same time, the prevalence of toxoplasmosis has been reported to be 30% worldwide. Traditional medicines have long played a vital role in discovering and developing novel drugs, and this approach is essential in the face of increasing resistance to current antimalarial and anti-Toxoplasma drugs. In Indonesian traditional medicine, various plants are used for their therapeutic properties. This study focuses on eleven medicinal plants from which nineteen extracts were obtained and screened for their potential medicinal benefits against malaria and toxoplasmosis.

AIMS OF THE STUDY

The aim of this study was to evaluate the efficacy of extracts from Indonesian medicinal plants to inhibit Plasmodium falciparum, a parasite responsible for malaria, and Toxoplasma gondii, an opportunistic parasite responsible for toxoplasmosis.

METHODS

Nineteen extracts from eleven plants were subjected to in vitro screening against P. falciparum 3D7 (a chloroquine-sensitive strain) and the T. gondii RH strain. In vitro treatments were conducted on P. falciparum 3D7 and K1 (multidrug-resistant strains) using the potent extracts, and in vivo assessments were carried out with mice infected with P. yoelii 17XNL. LCMS analysis was also conducted to identify the main components of the most effective extract.

RESULTS

Seven extracts showed significant antiplasmodial activity (>80% inhibition) at a concentration of 100 μg/ml. These extracts were obtained from Dysoxylum parasiticum (Osbeck) Kosterm., Elaeocarpus glaber (Bl.) Bijdr., Eleutherine americana Merr., Kleinhovia hospita L., Peronema canescens Jack, and Plectranthus scutellarioides (L.) R.Br. Notably, the D. parasiticum ethyl acetate extract exhibited high selectivity and efficacy both in vitro and in vivo. Herein, the key active compounds oleamide and erucamide were identified, which had IC values (P. falciparum 3D7/K1) of 17.49/23.63 μM and 32.49/51.59 μM, respectively.

CONCLUSIONS

The results of this study highlight the antimalarial potential of plant extracts collected from Indonesia. Particularly, extracts from D. parasiticum EtOH and EtOAc stood out for their low toxicity and strong antiplasmodial properties, with the EtOAc extract emerging as a notably promising antimalarial candidate. Key compounds identified within this extract demonstrate the complexity of extracts' action against malaria, potentially targeting both the parasite and the host. This suggests a promising approach for developing new antimalarial strategies that tackle the multifaceted challenges of drug resistance and disease management. Future investigations are necessary to unlock the full therapeutic potential of these extracts.

摘要

民族药理学相关性

疟疾是由疟原虫引起的,仍然是一个重大的全球健康挑战,特别是在热带和亚热带地区。与此同时,全世界报道的弓形体病的患病率为 30%。传统药物在发现和开发新药方面一直发挥着重要作用,在面对当前抗疟药和抗弓形体病药物耐药性日益增加的情况下,这种方法至关重要。在印度尼西亚传统医学中,各种植物因其治疗特性而被使用。本研究重点研究了 11 种药用植物,从中获得了 19 种提取物,并对其抑制疟疾和弓形体病的潜在药用价值进行了筛选。

研究目的

本研究的目的是评估印度尼西亚药用植物提取物对引起疟疾的疟原虫和引起弓形体病的机会性病原体弓形虫的疗效。

方法

对 11 种植物的 19 种提取物进行了体外筛选,以检测其对恶性疟原虫 3D7(一种对氯喹敏感的株系)和弓形虫 RH 株的抑制作用。对恶性疟原虫 3D7 和 K1(多药耐药株)进行了有效的提取物的体外处理,并用感染疟原虫 17XNL 的小鼠进行了体内评估。还进行了 LCMS 分析,以鉴定最有效提取物的主要成分。

结果

七种提取物在浓度为 100μg/ml 时表现出显著的抗疟原虫活性(>80%抑制)。这些提取物来自 Dysoxylum parasiticum(Osbeck)Kosterm.、Elaeocarpus glaber(Bl.)Bijdr.、Eleutherine americana Merr.、Kleinhovia hospita L.、Peronema canescens Jack 和 Plectranthus scutellarioides(L.)R.Br.。值得注意的是,D. parasiticum 乙酸乙酯提取物在体内和体外均表现出高选择性和高效性。在此,鉴定出关键的活性化合物油酰胺和芥酸酰胺,其 IC 值(恶性疟原虫 3D7/K1)分别为 17.49/23.63μM 和 32.49/51.59μM。

结论

本研究结果突出了印度尼西亚植物提取物的抗疟潜力。特别是 D. parasiticum EtOH 和 EtOAc 提取物因其低毒性和强大的抗疟原虫特性而引人注目,其中 EtOAc 提取物是一种很有前途的抗疟候选药物。在该提取物中鉴定出的关键化合物表明了提取物对疟疾作用的复杂性,可能同时针对寄生虫和宿主。这表明开发新的抗疟策略具有很大的潜力,可以解决耐药性和疾病管理方面的多方面挑战。未来的研究有必要挖掘这些提取物的全部治疗潜力。

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