评价玛哈念汤藤配方及其植物成分的抗疟活性和毒性。
Evaluation of the antimalarial activity and toxicity of Mahanil-Tang-Thong formulation and its plant ingredients.
机构信息
Department of Medical Sciences, School of Medicine, Walailak University, Nakhon Si Thammarat, 80160, Thailand.
Faculty of Medical Technology, Huachiew Chalermprakiet University, Samutprakan, 10540, Thailand.
出版信息
BMC Complement Med Ther. 2022 Feb 27;22(1):51. doi: 10.1186/s12906-022-03531-2.
BACKGROUND
Novel potent antimalarial agents are urgently needed to overcome the problem of drug-resistant malaria. Herbal treatments are of interest because plants are the source of many pharmaceutical compounds. The Mahanil-Tang-Thong formulation is a Thai herbal formulation in the national list of essential medicines and is used for the treatment of fever. Therefore, this study aimed to evaluate the antimalarial activity of medicinal plants in the Mahanil-Tang-Thong formulation.
METHODS
Nine medicinal plant ingredients of the Mahanil-Tang-Thong formulation were used in this study. Aqueous and ethanolic extracts of all the plants were analyzed for their phytochemical constituents. All the extracts were used to investigate the in vitro antimalarial activity against Plasmodium falciparum K1 (chloroquine-resistant strain) by using the lactate dehydrogenase (pLDH) method and cytotoxicity in Vero cells by using the 3-(4,5-dimethylthiazol2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Additionally, an extract with potent in vitro antimalarial activity and no toxicity was selected to determine the in vivo antimalarial activity with Peters' 4-day suppressive test against the Plasmodium berghei ANKA strain. Acute toxicity was evaluated in mice for 14 days after the administration of a single oral dose of 2000 mg/kg.
RESULTS
This study revealed that ethanolic extracts of Sapindus rarak DC., Tectona grandis L.f., Myristica fragrans Houtt. and Dracaena loureiri Gagnep. exhibited potent antimalarial activity, with half-maximal inhibitory concentration (IC) values of 2.46, 3.21, 8.87 and 10.47 μg/ml, respectively, while the ethanolic of the formulation exhibited moderate activity with an IC value of 37.63 μg/ml and its aqueous extract had no activity (IC = 100.49 μg/ml). According to the in vitro study, the ethanolic wood extract of M. fragrans was selected for further investigation in an in vivo mouse model. M. fragrans extract at doses of 200, 400, and 600 mg/kg body weight produced a dose-dependent reduction in parasitemia by 8.59, 31.00, and 52.58%, respectively. No toxic effects were observed at a single oral dose of 2000 mg/kg body weight.
CONCLUSION
This study demonstrates that M. fragrans is a potential candidate for the development of antimalarial agents.
背景
为了克服抗药性疟疾的问题，急需开发新型高效抗疟药物。草药疗法引起了人们的兴趣，因为植物是许多药物化合物的来源。Mahanil-Tang-Thong 配方是泰国国家基本药物清单中的一种草药配方，用于治疗发热。因此，本研究旨在评估 Mahanil-Tang-Thong 配方中药用植物的抗疟活性。
方法
本研究使用了 Mahanil-Tang-Thong 配方中的九种药用植物成分。分析了所有植物的水提物和醇提物的植物化学成分。通过乳酸脱氢酶（pLDH）法，用 Vero 细胞检测 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐（MTT）法检测所有提取物的细胞毒性，评估所有提取物对恶性疟原虫 K1（氯喹耐药株）的体外抗疟活性。选择具有较强体外抗疟活性且无毒性的提取物，用 Peters 4 天抑制试验检测其对伯氏疟原虫 ANKA 株的体内抗疟活性。单次口服 2000mg/kg 后，在小鼠中评估 14 天的急性毒性。
结果
本研究表明，乙醇提取物 Sapindus rarak DC.、Tectona grandis L.f.、Myristica fragrans Houtt.和 Dracaena loureiri Gagnep. 表现出较强的抗疟活性，半数最大抑制浓度（IC）值分别为 2.46、3.21、8.87 和 10.47μg/ml，而配方的乙醇提取物表现出中等活性，IC 值为 37.63μg/ml，其水提取物无活性（IC=100.49μg/ml）。根据体外研究，选择 M. fragrans 的乙醇木提取物进行进一步的体内小鼠模型研究。M. fragrans 提取物在 200、400 和 600mg/kg 体重剂量下可分别使寄生虫血症减少 8.59%、31.00%和 52.58%，呈剂量依赖性。在 2000mg/kg 体重的单次口服剂量下，未观察到毒性作用。
结论
本研究表明，M. fragrans 是开发抗疟药物的潜在候选药物。
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