Enhancing the antimalarial activity of artesunate

Adebayo, Joseph O.; Tijjani, Habibu; Adegunloye, Adegbenro P.; Ishola, Ahmed Adebayo; Balogun, Elizabeth Abidemi; Malomo, Sylvia O.

doi:10.1007/s00436-020-06786-1

Cited by 39 publications

(45 citation statements)

References 122 publications

(131 reference statements)

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“…Artesunate undergoes metabolism to the active dihydroartemisinin which reacts with heme to generate free radicals that prevent synthesis of macromolecules required for plasmodium metabolism and proliferation. 26 Azadirachta indica extracts has also been reported to contain alkaloids, saponin, tannins, triterpenoids and other phenolics with a wide range of metabolic activities. 27 Physicians who see malaria patients at local hospitals may not be aware of, or be able to elicit history of previously used herbal preparations by their patients.…”

Section: Discussionmentioning

confidence: 99%

Toxicological implications of sequential administration of herbal and conventional medicines: Evidence from an in vivo study on Azadirachta indica and artesunate in male Wistar rats

Forcados

Adamu

Abdulsalam

et al. 2021

Toxicology Research and Application

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In most parts of West Africa and other developing countries, herbal medicines are sometimes used by patients concomitantly receiving conventional drugs, which can result in potentially serious adverse effects. This study examined in vivo cytotoxic effects of Azadirachta indica extracts followed by artesunate administration on some markers of liver and kidney toxicity. Serum ALT, GGT, urea, creatinine, interleukin 1β, tumor necrosis factor α, tissue malondialdehyde and glutathione levels and liver and kidney histology in healthy male Wistar rats administered 100 and 200 mg/kg A. indica for 5 days followed by 10 mg/kg Artesunate for 5 days was determined. Results showed significantly ( p < 0.05) higher serum ALT, GGT, urea, creatinine, interleukin 1β and tumor necrosis factor α levels with proportional increase of 16.5, 21.7, 9.2, 6.9, 9.1 and 9.1% respectively when compared to normal control was observed. Malondialdehyde levels were significantly ( p < 0.05) higher with a proportional increase of 57.8%, while glutathione levels were significantly ( p < 0.05) lower with a proportional decrease of 13.4% in liver homogenates of the treated rats relative to normal control. Histological examination of the liver and kidney of the co-treated rats showed vascular congestion and necrosis. Collectively, the results suggest that administration of A. indica followed by artesunate could predispose to liver and kidney associated cytotoxicity. These findings could have implications for people who habitually use herbal preparations and conventional drugs in sequential fashion.

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Section: Discussionmentioning

confidence: 99%

Toxicological implications of sequential administration of herbal and conventional medicines: Evidence from an in vivo study on Azadirachta indica and artesunate in male Wistar rats

Forcados

Adamu

Abdulsalam

et al. 2021

Toxicology Research and Application

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“…In the body, ART gets converted to dihydroartemisinin, which has a higher half-life of around 45 min. Mechanisms of action for ART (like any other artemisinin) include inhibiting heme polymerization, generating ROS, destabilizing parasite membrane, alkylating proteins and inhibiting PfATP6 [ 6 ].…”

Section: Malaria and Its Parasite Life Cyclementioning

confidence: 99%

“…Its administration can be intramuscular, oral, rectal, and intravenous [ 3 ]. When orally administered, ART has a short half-life ranging from 20 to 45 min, during which it is metabolized, through esterase-catalysed hydrolysis, to dihydroartemisinin, the active metabolite responsible for the antimalarial activity of artesunate [ 6 ].…”

Section: Introductionmentioning

confidence: 99%

Recent Advances in the Therapeutic Efficacy of Artesunate

2022

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Artesunate, a semisynthetic artemisinin derivative, is well-known and used as the first-line drug for treating malaria. Apart from treating malaria, artesunate has also been found to have biological activity against a variety of cancers and viruses. It also exhibits antidiabetic, anti-inflammatory, anti-atherosclerosis, immunosuppressive activities, etc. During its administration, artesunate can be loaded in liposomes, alone or in combination with other therapeutic agents. Administration routes include intragastrical, intravenous, oral, and parenteral. The biological activity of artesunate is based on its ability to regulate some biological pathways. This manuscript reports a critical review of the recent advances in the therapeutic efficacy of artesunate.

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“…The alteration of membrane transport proteins, including Kelch13, adjacent to the parasite's food vacuole, are expected to influence the parasite's susceptibility to artemisinin [81][82][83].…”

Section: Is the Incidence Of Artemisinin-induced Hypersensitivity Low Or Simply Under-reported?mentioning

confidence: 99%

Drug-induced hypersensitivity to artemisinin-based therapies for malaria

Nordmann

Borrmann

Ramharter

2022

Trends in Parasitology

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In the early 2000s, artemisinin-based combination therapy (ACT) was introduced as first-line treatment for uncomplicated Plasmodium falciparum malaria in virtually all endemic countries. However, despite the well-known excellent tolerability of ACTs, hypersensitivity to artemisinin derivatives remains a repeatedly documented adverse drug reaction of still unknown frequency. The clinical features of an artemisinin-induced hypersensitivity reaction range from mild to lifethreatening severity, and a significant number of cases may pass unnoticed. In this review, we discuss the medical importance of hypersensitivity to artemisinin derivatives and we review data on the presumed frequency and its potential underlying mechanisms. Furthermore, we advocate to make alternative non-artemisinin-based drugs available for patients who do not tolerate artemisinin derivatives and to continue investing in the development of novel non-artemisinin-based combination regimens.

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Enhancing the antimalarial activity of artesunate

Cited by 39 publications

References 122 publications

Toxicological implications of sequential administration of herbal and conventional medicines: Evidence from an in vivo study on Azadirachta indica and artesunate in male Wistar rats

Toxicological implications of sequential administration of herbal and conventional medicines: Evidence from an in vivo study on Azadirachta indica and artesunate in male Wistar rats

Recent Advances in the Therapeutic Efficacy of Artesunate

Drug-induced hypersensitivity to artemisinin-based therapies for malaria

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