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Tolerance of Gambian Plasmodium falciparum to Dihydroartemisinin and Lumefantrine detected by Ex vivo Parasite Survival Rate Assay (PSRA)

October 7, 2020 - 15:39 -- Open Access
Mbye H, Bojang F, Jawara AS, Njie B, Mohammed NI, Okebe J, D'Alessandro U, Amambua-Ngwa A
Antimicrob Agents Chemother. 2020 Oct 5:AAC.00720-20

Monitoring of Plasmodium falciparum sensitivity to antimalarial drugs in Africa is vital for malaria elimination. However, the commonly used ex-vivo/in-vitro IC50 test is inconsistent for several antimalarials, while the alternative ring-stage survival assay (RSA) for artemisinin derivatives has not been widely adopted. Here we applied an alternative two-colour flow-cytometry based parasite survival rate assay (PSRA) to detect ex-vivo antimalarial tolerance in P. falciparum isolates from The Gambia.

Antimalarial drugs inhibit the replication of SARS-CoV-2: an in vitro evaluation

September 15, 2020 - 14:26 -- Open Access
Gendrot M, Andreani J, Pradines B, et al.
Travel Med Infect Dis. 2020 Sep 8:101873

In December 2019, a new severe acute respiratory syndrome coronavirus (SARS-CoV-2) causing coronavirus diseases 2019 (COVID-19) emerged in Wuhan, China. African countries see slower dynamic of COVID-19 cases and deaths. One of the assumptions that may explain this later emergence in Africa, and more particularly in malaria endemic areas, would be the use of antimalarial drugs.

NOT Open Access | A combined Raman optical activity and vibrational circular dichroism study on artemisinin-type products

August 10, 2020 - 14:34 -- NOT Open Access
Bogaerts J, Desmet F, Aerts R, Bultinck P, Herrebout W, Johannessen C
Phys Chem Chem Phys. 2020 Aug 5

Artemisinin and two of its derivatives, dihydroartemisinin and artesunate, which are front line drugs against malaria, were investigated using Raman optical activity (ROA) and vibrational circular dichroism (VCD) experiments, both supported by density functional theory (DFT) level calculations. The experimental techniques combined with DFT calculations could show that dihydroartemisinin was present as an epimeric mixture in solution.

NOT Open Access | Dihydroartemisinin exposure impairs porcine ovarian granulosa cells by activating PERK-eIF2α-ATF4 through endoplasmic reticulum stress

July 30, 2020 - 07:14 -- NOT Open Access
Luo Y, Guo Q, Zhang L, Zhuan Q, Meng L, Fu X, Hou Y
Toxicol Appl Pharmacol. 2020 Jul 25:115159

Dihydroartemisinin (DHA) is an artemisinin derivative commonly used in malaria therapy, and a growing number of studies have focused on the potent anticancer activity of DHA. However, the reproductive toxicity of anticancer drugs is a major concern for young female cancer patients. Previous studies have suggested that DHA can cause embryonic damage and affect oocyte maturation.

NOT Open Access | A Chemically Stable Fluorescent Mimic of Dihydroartemisinin, Artemether, and Arteether with Conserved Bioactivity and Specificity Shows High Pharmacological Relevance to the Antimalarial Drugs

July 20, 2020 - 14:52 -- NOT Open Access
Sissoko A, Vásquez-Ocmín P, Duval R, et al.
ACS Infect Dis. 2020 Jul 10; 6(7):1532-1547

Three novel tracers designed as fluorescent surrogates of artemisinin-derived antimalarial drugs (i.e., dihydroartemisinin, artemether, arteether, and artemisone) were synthesized from dihydroartemisinin.

NOT Open Access | Heterologous Expression, Purification, and Functional Analysis of the Plasmodium falciparum Phosphatidylinositol 4-Kinase IIIß

June 17, 2020 - 12:59 -- NOT Open Access
Sternberg AR, Roepe PD
Biochemistry. 2020 Jun 16

Recently we heterologously expressed, purified, and analyzed the function of the sole Plasmodium falciparum phosphatidylinositol 3-kinase (PI3K), found that the enzyme is a "class III" or "Vps34" PI3K, and that it is irreversibly inhibited by Fe2+-mediated covalent, nonspecific interactions with the leading antimalarial drug dihydroartemisinin (Hassett M. R., et al. (2017) Biochemistry 56, 4335-4345).

NOT Open Access | Dihydroartemisinin regulates the immune system by promotion of CD8+ T lymphocytes and suppression of B cell responses

May 7, 2020 - 13:32 -- NOT Open Access
Zhang T, Zhang Y, Jiang N, Zhao X, Sang X, Yang N, Feng Y, Chen R, Chen Q
Sci China Life Sci. 2020 May;63(5):737-749

Artemisia annua is an anti-fever herbal medicine first described in traditional Chinese medicine 1,000 years ago. Artemisinin, the extract of A. annua, and its derivatives (dihydroartemisinin (DHA), artemether, and artesunate) have been used for the treatment of malaria with substantial efficacy. Recently, DHA has also been tested for the treatment of lupus erythematosus, indicating that it may function to balance the immune response in immunocompromised individuals.

NOT Open Access | A chemically stable fluorescent mimic of dihydroartemisinin, artemether and arteether with conserved bioactivity and specificity shows high pharmacological relevance to the antimalarial drugs

April 13, 2020 - 14:01 -- NOT Open Access
Sissoko A, Vasquez-Ocmin P, Duval RA, et al.
ACS Infect Dis. 2020 Apr 8

Three novel tracers designed as fluorescent surrogates of artemisinin-derived antimalarial drugs (i. e., dihydroartemisinin, artemether, arteether and artemisone) were synthesized from dihydroartemisinin.

NOT Open Access | Combination of zingerone and dihydroartemisinin presented synergistic antimalarial activity against Plasmodium berghei infection in BALB/c mice as in vivo model

March 2, 2020 - 14:07 -- NOT Open Access
Ounjaijean S, Somsak V
Parasitology International, 20 February 2020, 102088

Malaria is a global health problem leading to the death of 435,000 cases in tropical and sub-tropical zones. Spread and emergence of increasing resistance to the antimalarial drugs are the major challenges in the control of malaria. Therefore, searching for alternative antimalarial drugs is urgently needed, and combination treatment preferred as an approach to address this. This study aimed to evaluate in vivo antimalarial activity of zingerone (ZN), and its combination with dihydroartemisinin (DHA) against Plasmodium berghei infected mice.

NOT Open Access | Dihydroartemisinin inhibits endothelial cell tube formation by suppression of the STAT3 signaling pathway

January 15, 2020 - 08:01 -- NOT Open Access
Gao P, Wang LL, Liu J, Dong F, Song W, Liao L, Wang B, Zhang W, Zhou X, Xie Q, Sun R, Liu J
Life Sciences, Volume 242, 1 February 2020, 117221

Endothelial cell (EC) tube formation is crucial for tumor angiogenesis, which becomes a target for chemotherapy. The anti-malaria agent dihydroartemisinin (DHA) inhibited tumor growth and angiogenesis. The aim of this study was to investigate the effects of DHA on EC tube formation and the underlying mechanisms.


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