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in vitro

NOT Open Access | Design, synthesis, and characterization of novel aminoalcohol quinolines with strong in vitro antimalarial activity

January 18, 2022 - 20:46 -- NOT Open Access
Dassonville-Klimpt A, Schneider J, Sonnet P, et al.
Eur J Med Chem. 2022 Jan 15;228:113981

Malaria is the fifth most lethal parasitic infections in the world. Herein, five new series of aminoalcohol quinolines including fifty-two compounds were designed, synthesized and evaluated in vitro against Pf3D7 and PfW2 strains. Among them, fourteen displayed IC50 values below or near of 50.0 nM whatever the strain with selectivity index often superior to 100.17b was found as a promising antimalarial candidate with IC50 values of 14.9 nM and 11.0 nM against respectively Pf3D7 and PfW2 and a selectivity index higher than 770 whatever the cell line is.

NOT Open Access | Comparison of in vitro transformation efficiency methods for Plasmodium falciparum

December 1, 2021 - 20:38 -- NOT Open Access
Wang S, Zeng W, Zhao W, Xiang Z, Zhao H, Yang Q, Li X, Duan M, Li X, Wang X, Si Y, Rosenthal BM, Yang Z
Mol Biochem Parasitol. 2021 Nov 23:111432

Poor efficiency plagues conventional methods to transfect Plasmodium falciparum with genetic modifications, impeding research aimed at limiting the damage wrought by this agent of severe malaria. Here, we sought and documented improvements, using fluoresce imaging, cell sorting, and drug selection as means to measure efficiency. Through the transfection of EGFP plasmid, the transfection efficiency of the three methods used in this study was as high as 10-3.

Probing the distinct chemosensitivity of Plasmodium vivax liver stage parasites and demonstration of 8-aminoquinoline radical cure activity in vitro

October 13, 2021 - 12:50 -- Open Access
Maher SP, Vantaux A, Kyle DE, et al.
Sci Rep. 2021 Oct 7;11(1):19905

Improved control of Plasmodium vivax malaria can be achieved with the discovery of new antimalarials with radical cure efficacy, including prevention of relapse caused by hypnozoites residing in the liver of patients. We screened several compound libraries against P. vivax liver stages, including 1565 compounds against mature hypnozoites, resulting in one drug-like and several probe-like hits useful for investigating hypnozoite biology. Primaquine and tafenoquine, administered in combination with chloroquine, are currently the only FDA-approved antimalarials for radical cure, yet their activity against mature P. vivax hypnozoites has not yet been demonstrated in vitro.

NOT Open Access | Novel Antiplasmodial Compounds Leveraged with Multistage Potency against the Parasite Plasmodium falciparum: In Vitro and In Vivo Evaluations and Pharmacokinetic Studies

June 16, 2021 - 09:52 -- NOT Open Access
Sharma N, Kashif M, Singh V, Fontinha D, Mukherjee B, Kumar D, Singh S, Prudencio M, Singh AP, Rathi B
J Med Chem. 2021 Jun 14

Hydroxyethylamine (HEA)-based novel compounds were synthesized and their activity against Plasmodium falciparum 3D7 was assessed, identifying a few hits without any apparent toxicity. Hits 5c and 5d also exhibited activity against resistant field strains, PfRKL-9 and PfC580Y. A single dose, 50 mg/Kg, of hits administered to the rodent parasite Plasmodium berghei ANKA exhibited up to 70% reduction in the parasite load.

NOT Open Access | Artesunate inhibits melanoma progression in vitro via suppressing STAT3 signaling pathway

February 23, 2021 - 13:10 -- NOT Open Access
Berköz M, Özkan-Yılmaz F, Özlüer-Hunt A, Krośniak M, Türkmen Ö, Korkmaz D, Keskin S
Pharmacol Rep. 2021 Feb 20

Melanoma is a life-threatening cancer characterized with a potentially metastatic tumor of melanocytic origin. Improved methods or novel therapies are urgently needed to eliminate the development of metastases. Artesunate is a semi-synthetic derivative of artemisinin used for trarment of malaria and cancer. The purpose of this study was to investigate the anti-cancer effect of artesunate and the role on STAT3 signaling in A375 human melanoma cell line.

NOT Open Access | Affinity purification of Plasmodium ookinetes from in vitro cultures using extracellular matrix gel

February 3, 2021 - 14:43 -- NOT Open Access
Recio-Tótoro B, Condé R, Claudio-Piedras F, Lanz-Mendoza H
Parasitol Int. 2021 Feb;80:102242

Malaria transmission depends on the parasites' successful invasion of the mosquito. This is achieved by the ookinete, a motile zygote that forms in the blood bolus after the mosquito takes an infectious blood meal. The ookinete invades the midgut epithelium and strongly attaches to the basal lamina, differentiating into an oocyst that produces the vertebrate-invasive sporozoites.

NOT Open Access | Plasmodium falciparum purine nucleoside phosphorylase as a model in the search for new inhibitors by high throughput screening

December 16, 2020 - 10:06 -- NOT Open Access
Holanda RJ, Deves C, Pereira da Silva LH, et al.
Int J Biol Macromol. 2020 Dec 15;165(Pt B):1832-1841

Studies have shown that inhibition of Plasmodium falciparum Purine Nucleoside Phosphorylase (PfPNP) blocks the purine salvage pathway in vitro and in vivo. In this study, PfPNP was evaluated as a model in the search for new inhibitors using surface plasmon resonance (SPR). Its expression, purification, oligomeric state, kinetic constants, calorimetric parameters and kinetic mechanisms were obtained. PfPNP was immobilized on a CM5 sensor chip and sensorgrams were produced through binding the enzyme to the substrate MESG and interactions between molecules contained in 10 fractions of natural extracts.

NOT Open Access | Assessment of in vitro and in vivo antimalarial efficacy and GC-fingerprints of selected medicinal plant extracts

December 2, 2020 - 08:38 -- NOT Open Access
Sachdeva C, Mohanakrishnan D, Kumar S, Kaushik NK
Exp Parasitol. 2020 Dec;219:108011

A hallmark of mortality and morbidity, malaria is affecting nearly half of the world's population. Emergence of drug-resistant strains of malarial parasite prompts identification and evaluation of medicinal plants and their constituents that may hold the key to a new and effective anti-malarial drug. In this context, nineteen methanolic extracts from seventeen medicinal plants were evaluated for anti-plasmodial potential against Plasmodium falciparum strain 3D7 (Chloroquine (CQ) sensitive) and INDO (CQ resistant) using fluorescence based SYBR-Green assay and for cytotoxic effects against mammalian cell lines.

NOT Open Access | A chimeric Plasmodium vivax Merozoite Surface Protein Antibody Recognises and Blocks Erythrocytic P. cynomolgi Berok Merozoites In Vitro

November 18, 2020 - 12:13 -- NOT Open Access
Shen FH, Ong JJY, Sun YF, Lei Y, Chu RL, Kassegne K, Fu HT, Jin C, Han ET, Russell B, Han JH, Cheng Y
Infect Immun. 2020 Nov 16:IAI.00645-20

Research on erythrocytic Plasmodium vivax merozoite antigens is critical for identifying potential vaccine candidates in reducing vivax disease. However, many P. vivax studies are constrained by its inability to undergo long-term culture in vitro Conserved across all Plasmodium spp, merozoite surface proteins are essential for invasion into erythrocytes and highly expressed on erythrocytic merozoites, thus making it an ideal vaccine candidate.

Dimethyl fumarate reduces TNF and Plasmodium falciparum induced brain endothelium activation in vitro

October 22, 2020 - 15:42 -- Open Access
Neida K. Mita-Mendoza, Ariel Magallon-Tejada, Priyanka Parmar, Raquel Furtado, Margaret Aldrich, Alex Saidi, Terrie Taylor, Joe Smith, Karl Seydel and Johanna P. Daily
Malaria Journal 2020 19:376, 21 October 2020

Cerebral malaria (CM) is associated with morbidity and mortality despite the use of potent anti-malarial agents. Brain endothelial cell activation and dysfunction from oxidative and inflammatory host responses and products released by Plasmodium falciparum-infected erythrocytes (IE), are likely the major contributors to the encephalopathy, seizures, and brain swelling that are associated with CM. The development of adjunctive therapy to reduce the pathological consequences of host response pathways could improve outcomes. A potentially protective role of the nuclear factor E2-related factor 2 (NRF2) pathway, which serves as a therapeutic target in brain microvascular diseases and central nervous system (CNS) inflammatory diseases such as multiple sclerosis was tested to protect endothelial cells in an in vitro culture system subjected to tumour necrosis factor (TNF) or infected red blood cell exposure. NRF2 is a transcription factor that mediates anti-oxidant and anti-inflammatory responses.


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