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artesunate

Enhancing the antimalarial activity of artesunate

July 8, 2020 - 15:55 -- Open Access
Author(s): 
Adebayo JO, Tijjani H, Adegunloye AP, Ishola AA, Balogun EA, Malomo SO
Reference: 
Parasitol Res. 2020 Jul 7

The global challenge to the treatment of malaria is mainly the occurrence of resistance of malaria parasites to conventionally used antimalarials. Artesunate, a semisynthetic artemisinin compound, and other artemisinin derivatives are currently used in combination with selected active antimalarial drugs in order to prevent or delay the emergence of resistance to artemisinin derivatives.

NOT Open Access | Design, Synthesis, Structure-Activity Relationship and Docking Studies of Novel Functionalized Arylvinyl-1,2,4-Trioxanes as Potent Antiplasmodial as well as Anticancer Agents

July 6, 2020 - 16:38 -- NOT Open Access
Author(s): 
Tiwari MK, Coghi P, Chaudhary S, et al.
Reference: 
ChemMedChem. 2020 Jul 3;15(13):1216-1228

A novel series of synthetic functionalized arylvinyl‐1,2,4‐trioxanes (8 a –p ) has been prepared and assessed for their in vitro antiplasmodial activity against the chloroquine‐resistant Pf INDO strain of Plasmodium falciparum by using a SYBR green‐I fluorescence assay. Compounds 8 g (IC50=0.051 μM; SI=589.41) and 8 m (IC50=0.059 μM; SI=55.93) showed 11‐fold and >9‐fold more potent antiplasmodial activity, respectively, as compared to chloroquine (IC50=0.546 μM; SI=36.63).

Post-malarial anaemia in Mozambican children treated with quinine or artesunate: a retrospective observational study

June 8, 2020 - 15:02 -- Open Access
Author(s): 
Varo R, Quintó L, Bassat Q, et al.
Reference: 
Int J Infect Dis. 2020 Jun 1:S1201-9712(20)30396-9

This retrospective analysis performed in Manhiça, Southern Mozambique aimed to describe the occurrence of post-malarial anaemia (measured as a decrease of haematocrit ≥10%) and the need for blood transfusions in children with severe malaria treated with intravenous quinine or parenteral artesunate.

Is availability of artesunate associated with the prognosis of imported malaria in Spain

April 29, 2020 - 05:37 -- Open Access
Author(s): 
Camprubí D, Martí-Soler H, Subirà C, Ferrer E, Muñoz J
Reference: 
Travel Med Infect Dis. 2020 Apr 24:101695

Although there is a lot of aspects we stil need to understand about treatment with artemisinins, there is no doubt about their efficacy in treating malaria. Artesunate (AS) has demonstrated its superiority against quinine for treatment of severe malaria in terms of reduction of mortality in different randomized clinical trials performed in endemic countries and subsequent meta-analysis. Despite having been established as the first line treatment by WHO and several national guidelines, its full implementation in non-endemic countries has not been completed.

NOT Open Access | Synergistic antitumor activity of sorafenib and artesunate in hepatocellular carcinoma cells

April 20, 2020 - 09:33 -- NOT Open Access
Author(s): 
Yao X, Zhao CR, Yin H, Wang K, Gao JJ
Reference: 
Acta Pharmacol Sin. 2020 Apr 16

Sorafenib is currently the standard chemotherapy drug for treatment of advanced hepatocellular carcinoma (HCC). But its efficacy requires improvement, it is imperative to seek therapeutic strategies that combine sorafenib with other anticancer agents. In this study we investigated the synergistic anticancer effect of combining sorafenib and artesunate, an anti-malaria drug derivative, against HCC in vitro and in vivo. We first showed that artesunate (1–100 μM) alone dose-dependently inhibited the proliferation of five HCC cell lines tested with IC50 values of around 100 μM.

Artesunate Affects T Antigen Expression and Survival of Virus-Positive Merkel Cell Carcinoma

April 15, 2020 - 14:12 -- Open Access
Author(s): 
Sarma B, Willmes C, Angerer L, Adam C, Becker JC, Kervarrec T, Schrama D, Houben R
Reference: 
Cancers (Basel). 2020 Apr 9;12(4). pii: E919

Merkel cell carcinoma (MCC) is a rare and highly aggressive skin cancer with frequent viral etiology. Indeed, in about 80% of cases, there is an association with Merkel cell polyomavirus (MCPyV); the expression of viral T antigens is crucial for growth of virus-positive tumor cells. Since artesunate—a drug used to treat malaria—has been reported to possess additional anti-tumor as well as anti-viral activity, we sought to evaluate pre-clinically the effect of artesunate on MCC.

Preparations of Rectal Suppositories Containing Artesunate

March 10, 2020 - 16:05 -- Open Access
Author(s): 
Persaud S, Eid S, Swiderski N, Serris I, Cho H
Reference: 
Pharmaceutics. 2020 Mar 2;12(3)

Rectal artesunate suppositories are a useful option for pre-referral treatment of severe malaria, specifically in children under 6 years of age in remote malaria-endemic areas. The main challenges are to improve the solubility of drugs in the rectal fluids and prevent the product from turning rancid or melting in a tropical climate.

NOT Open Access | Propensity Score Analysis of Artesunate Versus Quinine for Severe Imported Plasmodium falciparum Malaria in France

January 7, 2020 - 14:04 -- NOT Open Access
Author(s): 
El Ket N, Kendjo E, Jauréguiberry S, et al.
Reference: 
Clinical Infectious Diseases, Volume 70, Issue 2, 15 January 2020, Pages 280–287

Little is known on the use of artesunate compared with quinine for the treatment of imported malaria cases in nonendemic countries with a high level of care. Therefore, we compared the 2 treatments in terms of mortality and hospital and intensive care unit (ICU) discharge rates.

Adherence to the referral advice after introduction of rectal artesunate for pre-referral treatment of severe malaria at the community level: a noninferiority trial in the Democratic Republic of the Congo

December 30, 2019 - 14:37 -- Open Access
Author(s): 
Patrick M. Mvumbi, Jeanine Musau, Ousmane Faye, Hyppolite Situakibanza and Emile Okitolonda
Reference: 
Malaria Journal 2019 18:438, 21 December 2019

The Democratic Republic of the Congo adopted the strategy of using, at the community level, a dose of rectal artesunate as a pre-referral treatment for severe malaria amongst children under 5 years who could not quickly reach a health care facility and take oral medication. However, the adherence to referral advice after the integration of this strategy and the acceptability of the strategy were unknown.

A novel approach to identifying patterns of human invasion-inhibitory antibodies guides the design of malaria vaccines incorporating polymorphic antigens

August 15, 2017 - 16:30 -- Open Access
Author(s): 
Drew D, Wilson D, Elliott S, Cross N, Terheggen U, Hodder A, Siba P, Chelimo K, Dent A, Kazura J, Mueller I, Beeson J
Reference: 
BMC Medicine 2016, 14 :144 (23 September 2016)

We found that AMA1 was a major target of naturally acquired invasion-inhibitory antibodies that were highly prevalent in malaria-endemic populations and showed a high degree of allele specificity. Significantly, the prevalence of inhibitory antibodies to different alleles varied substantially within populations and between geographic locations.

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