The resistance of malaria parasites to the current antimalarial drugs has led to the search for novel effective drugs. Betula alnoides has been traditionally used for the treatment of malaria, but the scientific evidence to substantiate this claim is still lacking. Therefore, the present study aimed at evaluating the antimalarial activity and toxicity of an aqueous stem extract of B. alnoides in a mouse model. The in vivo antimalarial activity of an aqueous stem extract of B. alnoides was determined by a 4-day suppressive test in mice infected with chloroquine-sensitive Plasmodium berghei ANKA. The B. alnoides extract was administered orally at different doses of 200, 400, and 600 mg/kg body weight. The levels of parasitaemia, survival time, body weight change, and food and water consumption of the mice were determined. The acute toxicity of the extract was assessed in the mice for 14 days after the administration of a single oral dose of 5000 mg/kg. An aqueous stem extract of B. alnoides exhibited a significant dose-dependent reduction of parasitaemia in P. berghei-infected mice at all dose levels compared to the reduction in the negative control. Extract doses of 200, 400, and 600 mg/kg body weight suppressed the levels of parasitaemia by 46.90, 58.39, and 71.26%, respectively. The extract also significantly prolonged the survival times of the P. berghei-infected mice compared to the survival times of the negative control mice. In addition, at all dose levels, the extract prevented body weight loss in P. berghei-infected mice. For the acute toxicity, there were no significant alterations in the biochemical parameters and in the histopathology. In conclusion, the aqueous stem extract of B. alnoides possesses antimalarial properties. A single oral dose of 5000 mg/kg body weight had no significant toxic effects on the function and structure of the kidneys and liver. These results support its use in traditional medicine for the treatment of malaria.
Objective. To investigate the antimalarial effects and toxicity of the extracts of the flowers of Tagetes erecta L. and the leaves of Synedrella nodiflora (L.) Gaertn. in a mouse model. Methods. To determine the in vivo antimalarial activity of the extracts, mice were intraperitoneally injected with the Plasmodium berghei ANKA strain and then administered T. erecta or S. nodiflora extract daily for 4 days. Parasitemia was observed by light microscopy. For the detection of acute toxicity, the mice received a single dose of T. erecta or S. nodiflora extract and were observed for 14 days. Biochemical parameters of liver and kidney function and the histopathology of liver and kidney tissues of the acute toxicity group were then examined. Results. T. erecta and S. nodiflora crude extracts at a dose of 600 mg/kg body weight significantly suppressed parasitemia in malaria-infected mice by 65.65% and 62.65%, respectively. Mice treated with 400 mg/kg T. erecta and S. nodiflora crude extracts showed 50.82% and 57.67% suppression, and mice treated with 200 mg/kg displayed 26.33% and 38.57% suppression, respectively. Additionally, no symptoms of acute toxicity were observed in the T. erecta- and S. nodiflora-treated groups. Moreover, no significant alterations in the biochemical parameters of liver and kidney function and no histological changes in the liver or kidney tissues were observed. Conclusions. This study revealed that both T. erecta and S. nodiflora extracts have antimalarial properties in vivo with less toxic effects. Further studies are needed to elucidate the mechanisms of the active compounds from both plants.
The aim of this study was to investigate the antimalarial activities and toxicity of Pogostemon cablin extracts. In vitro activities against the chloroquine-resistant Plasmodium falciparum K1 strain were assessed by using the Plasmodium lactate dehydrogenase enzyme (pLDH) assay, while in vivo activity against the Plasmodium berghei ANKA strain in mice was investigated using a 4-day suppressive test. The in vitro and in vivo toxicity were determined in Vero cells and mice, respectively. The ethanolic extract possessed antimalarial activity with an IC50 of 24.49 ± 0.01 µg/ml, whereas the aqueous extract showed an IC50 of 549.30 ± 0.07 µg/ml. Cytotoxic analyses of the ethanolic and aqueous extracts revealed a nontoxic effect on Vero cells at a concentration of 80 µg/ml. Based on a preliminary study of in vitro antimalarial activity, the ethanolic extract was chosen as a potential agent for further in vivo antimalarial activity analysis in mice. The ethanolic extract, which showed no toxic effect on mice at a dose of 2000 mg/kg body weight, significantly suppressed parasitemia in mice by 38.41%, 45.12% and 89.00% at doses of 200, 400 and 600 mg/kg body weight, respectively. In conclusion, this study shows that the ethanolic P. cablin extract possesses in vitro and in vivo antimalarial activity without toxic effects.
Malaria remains a life-threatening health problem and encounters with the increasing of antimalarial drug resistance. Medicinal plants play a critical role in synthesizing novel and potent antimalarial agents. This study aimed to investigate the phytochemical constituents, antiplasmodial activity, and evaluate the toxicity of crude ethanolic extracts of Myristica fragrans, Atractylodes lancea, and Prabchompoothaweep remedy in a mouse model. The phytochemical constituents were characterized by liquid chromatography-mass spectrometry (LC-MS). Antimalarial efficacy against Plasmodium berghei was assessed using 4-day suppressive tests at doses of 200, 400, and 600 mg/kg body weight. Acute toxicity was assessed at a dose of 2000 mg/kg body weight of crude extracts. The 4-day suppression test showed that all crude extracts significantly suppressed parasitemia (p < 0.05) compared to the control group. Higher parasitemia suppression was observed both in Prabchompoothaweep remedy at a dose of 600 mg/kg (60.1%), and A. lancea at a dose of 400 mg/kg (60.1%). The acute oral toxicity test indicated that the LD50 values of all extracts were greater than 2000 mg/kg and that these extracts were not toxic in the mouse model. LC-MS analysis revealed several compounds in M. fragrans, A. lancea, and Prabchompoothaweep remedy. For quantitative analysis, 1,2,6,8-tetrahydroxy-3-methylanthraquinone 2-O-b-D-glucoside, chlorogenic acid, and 3-O-(beta-D-glucopyranosyl-(1->6)-beta-D-glucopyranosyl) ethyl 3-hydroxyoctanoate were found in A. lancea, while (7′x,8′x)-4,7′-epoxy-3,8′-bilign-7-ene-3,5′-dimethoxy-4′,9,9′-triol, edulisin III, and tetra-hydrosappanone A trimethyl ether are found in M. fragrans. 6′-O-Formylmarmin was present in the Prabchompoothaweep remedy, followed by pterostilbene glycinate and amlaic acid. This study showed that the ethanolic extracts of A. lancea and Prabchompoothaweep remedy possess antimalarial activity against Plasmodium berghei. None of the extracts had toxic effects on liver and kidney function. Therefore, the ethanolic extract of A. lancea rhizome and Prabchompoothaweep remedy could be used as an alternative source of new antimalarial agents. Further studies are needed to determine the active compounds in both extracts.
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 (IC50) 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 IC50 value of 37.63 μg/ml and its aqueous extract had no activity (IC50 = 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.
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