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Toward New Transmission-Blocking Combination Therapies: Pharmacokinetics of 10-Amino-Artemisinins and 11-Aza-Artemisinin and Comparison with Dihydroartemisinin and Artemether

August 4, 2021 - 16:26 -- Open Access
Daniel J Watson, Lizahn Laing, Liezl Gibhard, Ho Ning Wong, Richard K Haynes, Lubbe Wiesner
Antimicrob Agents Chemother. 2021 Jul 16;65(8):e0099021

As artemisinin combination therapies (ACTs) are compromised by resistance, we are evaluating triple combination therapies (TACTs) comprising an amino-artemisinin, a redox drug, and a third drug with a different mode of action. Thus, here we briefly review efficacy data on artemisone, artemiside, other amino-artemisinins, and 11-aza-artemisinin and conduct absorption, distribution, and metabolism and excretion (ADME) profiling in vitro and pharmacokinetic (PK) profiling in vivo via intravenous (i.v.) and oral (p.o.) administration to mice.

Parenteral artemisinins are associated with reduced mortality and neurologic deficits and improved long-term behavioral outcomes in children with severe malaria

August 4, 2021 - 15:44 -- Open Access
Conroy AL, Opoka RO, Bangirana P, Namazzi R, Okullo AE, Georgieff MK, Cusick S, Idro R, Ssenkusu JM, John CC
BMC Med. 2021 Jul 28;19(1):168

In 2011, the World Health Organization recommended injectable artesunate as the first-line therapy for severe malaria (SM) due to its superiority in reducing mortality compared to quinine. There are limited data on long-term clinical and neurobehavioral outcomes after artemisinin use for treatment of SM.

NOT Open Access | The End of the Artemisinin Era-We Should Aim at Malaria Eradication in Asia Using Free, Effective Treatment

August 4, 2021 - 12:17 -- NOT Open Access
Petersen E, Picot S
Clin Infect Dis. 2021 Aug 2;73(3):414-415

No abstract available

Artesunate relieves acute kidney injury through inhibiting macrophagic Mincle-mediated necroptosis and inflammation to tubular epithelial cell

August 3, 2021 - 17:28 -- Open Access
Lei XY, Tan RZ, Jia J, Wu SL, Wen CL, Lin X, Wang H, Shi ZJ, Li B, Kang Y, Wang L
J Cell Mol Med. 2021 Aug 1

Artesunate is a widely used derivative of artemisinin for malaria. Recent researches have shown that artesunate has a significant anti-inflammatory effect on many diseases. However, its effect on acute kidney injury with a significant inflammatory response is not clear. In this study, we established a cisplatin-induced AKI mouse model and a co-culture system of BMDM and tubular epithelial cells (mTEC) to verify the renoprotective and anti-inflammatory effects of artesunate on AKI, and explored the underlying mechanism.

Artemisinin and multidrug-resistant Plasmodium falciparum - a threat for malaria control and elimination

July 21, 2021 - 17:12 -- Open Access
Dhorda M, Amaratunga C, Dondorp AM
Curr Opin Infect Dis. 2021 Jul 15

Artemisinin-based combination therapies (ACTs) are globally the first-line treatment for uncomplicated falciparum malaria and new compounds will not be available within the next few years. Artemisinin-resistant Plasmodium falciparum emerged over a decade ago in the Greater Mekong Subregion (GMS) and, compounded by ACT partner drug resistance, has caused significant ACT treatment failure. This review provides an update on the epidemiology, and mechanisms of artemisinin resistance and approaches to counter multidrug-resistant falciparum malaria.

NOT Open Access | Mechanisms and Molecular Targets of Artemisinin in Cancer Treatment

July 13, 2021 - 15:01 -- NOT Open Access
Li D, Zhang J, Zhao X
Cancer Invest. 2021 Jul 9:1-23

The major problems with cancer therapy are drug-induced side effects. There is an urgent need for safe anti-tumor drugs. Artemisinin is a Chinese herbal remedy for malaria with efficacy and safety. However, several studies reported that artemisinin causes neurotoxicity and cardiotoxicity in animal models.

Not Open Access | Synthesis of [15,15,15-2H3]-Dihydroartemisinic Acid and Isotope Studies Support a Mixed Mechanism in the Endoperoxide Formation to Artemisinin

June 22, 2021 - 15:37 -- NOT Open Access
Varela K, Arman HD, Yoshimoto FK
J Nat Prod. 2021 Jun 17

Artemisinin is the plant natural product used to treat malaria. The endoperoxide bridge of artemisinin confers its antiparasitic properties. Dihydroartemisinic acid is the biosynthetic precursor of artemisinin that was previously shown to nonenzymatically undergo endoperoxide formation to yield artemisinin. This report discloses the synthesis of [15,15,15-2H3]-dihydroartemisinic acid and its use to determine the mechanism of endoperoxide formation.

Restructured Mitochondrial-Nuclear Interaction in Plasmodium falciparum Dormancy and Persister Survival after Artemisinin Exposure

June 1, 2021 - 15:38 -- Open Access
Connelly SV, Manzella-Lapeira J, Levine ZC, Brzostowski J, Krymskaya L, Rahman RS, Ellis AC, Amin SN, Sá JM, Wellems TE
mBio. 2021 May 28:e0075321

Artemisinin and its semisynthetic derivatives (ART) are fast acting, potent antimalarials; however, their use in malaria treatment is frequently confounded by recrudescences from bloodstream Plasmodium parasites that enter into and later reactivate from a dormant persister state. Here, we provide evidence that the mitochondria of dihydroartemisinin (DHA)-exposed persisters are dramatically altered and enlarged relative to the mitochondria of young, actively replicating ring forms. Restructured mitochondrial-nuclear associations and an altered metabolic state are consistent with stress from reactive oxygen species.

NOT Open Access | Bioactive half-sandwich Rh and Ir bipyridyl complexes containing artemisinin

June 1, 2021 - 12:24 -- NOT Open Access
Chellan P, Avery VM, Duffy S, Land KM, Tam CC, Kim JH, Cheng LW, Romero-Canelón I, Sadler PJ
J Inorg Biochem. 2021 Jun;219:111408

Reaction of dihydroartemisinin (DHA) with 4-methyl-4'-carboxy-2,2'-bipyridine yielded the new ester derivative L1. Six novel organometallic half-sandwich chlorido Rh(III) and Ir(III) complexes (1-6) containing pentamethylcyclopentadienyl, (Cp*), tetramethylphenylcyclopentadienyl (Cpxph), or tetramethylbiphenylcyclopentadienyl (Cpxbiph), and N,N-chelated bipyridyl group of L1, have been synthesized and characterized.

Artemisinin susceptibility in the malaria parasite Plasmodium falciparum: propellers, adaptor proteins and the need for cellular healing

May 12, 2021 - 12:39 -- Open Access
Sutherland CJ, Henrici RC, Artavanis-Tsakonas K
FEMS Microbiol Rev. 2021 May 5;45(3):fuaa056

Studies of the susceptibility of Plasmodium falciparum to the artemisinin family of antimalarial drugs provide a complex picture of partial resistance (tolerance) associated with increased parasite survival in vitro and in vivo.


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