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antimalarial activity

NOT Open Access | In vivo antimalarial activity of a probiotic bacterium Lactobacillus sakei isolated from traditionally fermented milk in BALB/c mice infected with Plasmodium berghei ANKA

July 28, 2021 - 13:55 -- NOT Open Access
Toukam LL, Tatsinkou Fossi B, Taiwe GS, Bila RB, Feugaing Sofeu DD, Ivo EP, Achidi EA
J Ethnopharmacol. 2021 Jul 22:114448

Milk production, processing and consumption are integral part of traditional practices in Fulani tribe of Cameroon. It has been observed that Fulani are resistant to malaria. Dairy products traditionally processed by Fulani are intensively used in the ritual treatment of malarial, inflammations and behavioural disorders. Many studies have demonstrated that fermented milk is a rich source of probiotic bacteria. However, the antimalarial activity of probiotics isolated from this natural source has not been experimentally tested.

Evaluation of the Antimalarial Activity of Ethanol Extracts of the Leaves of Three Plant Species Collected from Yayu Coffee Forest Biosphere Reserve, Southwest Ethiopia

July 21, 2021 - 18:18 -- Open Access
Yeshanew S, Gete W, Chilo D
J Exp Pharmacol. 2021 Jul 14;13:661-668

In the attempt of searching for potential plant derived antimalarial medicines, the aim of the present study was to examine In vivo antimalarial efficacy of crude ethanol extracts of the leaves of Croton macrostachyus, Ruta chalepensis and Vernonia amygdalina using chloroquine (CQ) sensitive strains of Plasmodium berghei in Swiss albino mice.

NOT Open Access | Evaluation of ethnopharmacologically selected Vitex negundo L. for In vitro antimalarial activity and secondary metabolite profiling

July 20, 2021 - 13:31 -- NOT Open Access
Dwivedi MK, Shukla R, Sharma NK, Manhas A, Srivastava K, Kumar N, Singh PK
J Ethnopharmacol. 2021 Jul 15;275:114076

Limited drugs, rise in drug resistance against frontline anti-malarial drugs, non-availability of efficacious vaccines and high cost of drug development hinders malaria intervention programs. Search for safe, effective and affordable plant based anti-malarial agents, thus becomes crucial and vital in the current scenario. The Vitex negundo L. is medicinal plant possessing a variety of pharmaceutically important compounds. The plant is used traditionally worldwide for the treatment of malaria including India and Malaysia by the indigenous tribes. In vitro studies have reported the anti-malarial use of the plant in traditional medicinal systems.

Pharmacokinetic evaluation of Chalcone derivatives with antimalarial activity in New Zealand White Rabbits

July 13, 2021 - 14:48 -- Open Access
Sinha S, Prakash A, Medhi B, Sehgal A, Batovska DI, Sehgal R
BMC Res Notes. 2021 Jul 8;14(1):264

Malaria is a major global health concern with the urgent need for new treatment alternatives due to the alarming increase of drug-resistant Plasmodium strains. Chalcones and its derivatives are important pharmacophores showing antimalarial activity. Determination of the pharmacokinetic variables at the preliminary step of drug development for any drug candidates is an essential component of in vivo antimalarial efficacy tests. Substandard pharmacokinetic variables are often responsible for insufficient therapeutic effect. Therefore, three chalcone derivatives, 1, 2, and 3, having antimalarial potency were studied further for potential therapeutic efficacy.

Not Open Access | Nucleotide analogues containing a pyrrolidine, piperidine or piperazine ring: Synthesis and evaluation of inhibition of plasmodial and human 6-oxopurine phosphoribosyltransferases and in vitro antimalarial activity

July 6, 2021 - 14:29 -- NOT Open Access
Frydrych J, Keough DT, Chavchich M, Travis J, Dračínský M, Edstein MD, Guddat LW, Hocková D, Janeba Z
Eur J Med Chem. 2021 Jul 5;219:113416

Parasites of the Plasmodium genus are unable to produce purine nucleotides de novo and depend completely on the salvage pathway. This fact makes plasmodial hypoxanthine-guanine-(xanthine) phosphoribosyltransferase [HG(X)PRT] a valuable target for development of antimalarial agents. A series of nucleotide analogues was designed, synthesized and evaluated as potential inhibitors of Plasmodium falciparum HGXPRT, P. vivax HGPRT and human HGPRT. These novel nucleoside phosphonates have a pyrrolidine, piperidine or piperazine ring incorporated into the linker connecting the purine base to a phosphonate group(s) and exhibited a broad range of Ki values between 0.15 and 72 μM.

NOT Open Access | Developmental stages influence in vivo antimalarial activity of aerial part extracts of Schkuhria pinnata

June 23, 2021 - 13:40 -- NOT Open Access
Nuwagira C, Peter EL, Ajayi CO, Adriko J, Grace KR, Olet EA, Ogwang PE, Tolo CU
J Ethnopharmacol. 2021 Jun 15:114341

Malaria remains a dire health challenge, particularly in sub-Saharan Africa. In Uganda, it is a most ordinary condition in hospital admission and outpatient care. The country's meager health services compel malaria patients to use herbal remedies such as Schkuhria pinnata (Lam.) Kuntze ex Thell (Asteraceae). Although in vivo studies tested the antimalarial activity of S. pinnata extracts, plant developmental stages and their effect at different doses remain unknown.

Search for the Active Ingredients from a 2-Aminothiazole DMSO Stock Solution with Antimalarial Activity

April 13, 2021 - 12:57 -- Open Access
Ropponen HK, Bader CD, Diamanti E, Illarionov B, Rottmann M, Fischer M, Witschel M, Müller R, Hirsch AKH
ChemMedChem. 2021 Apr 12

Chemical decomposition of DMSO stock solutions is a common incident that can mislead biological screening campaigns. Here, we share our case study of 2-aminothiazole 1, originating from an antimalarial class that undergoes chemical decomposition in DMSO at room temperature. As previously measured biological activities observed against Plasmodium falciparum NF54 and for the target enzyme Pf IspE were not reproducible for a fresh batch, we tackled the challenge to understand where the activity originated from.

Chemoprotective Antimalarial Activity of P218 against Plasmodium falciparum: A Randomized, Placebo-Controlled Volunteer Infection Study

February 10, 2021 - 09:44 -- Open Access
Chughlay MF, El Gaaloul M, Chalon S, et al.
Am J Trop Med Hyg. 2021 Feb 8:tpmd201165

P218 is a highly selective dihydrofolate reductase inhibitor with potent in vitro activity against pyrimethamine-resistant Plasmodium falciparum. This single-center, randomized, double-blind, placebo-controlled phase Ib study evaluated P218 safety and chemoprotective efficacy in a P. falciparum sporozoite (PfSPZ) volunteer infection study (VIS). Consecutive dose safety and tolerability were evaluated (cohort 1), with participants receiving two oral doses of P218 1,000 mg 48 hours apart (n = 6), or placebo (n = 2). P218 chemoprotective efficacy was assessed (cohorts 2 and 3) with direct venous inoculation of 3,200 aseptic, cryopreserved PfSPZ (NF54 strain) followed 2 hours later with two P218 doses of 1,000 mg (cohort 2, n = 9) or 100 mg (cohort 3, n = 9) administered 48 hours apart, or placebo (n = 6).

NOT Open Access | A Concise Total Synthesis of Dehydroantofine and the Antimalarial Activity against Chloroquine-Resistant P. falciparum

January 26, 2021 - 15:09 -- NOT Open Access
Yamasaki N, Iwasaki I, Sakumi K, Hokari R, Ishiyama A, Iwatsuki M, Nakahara M, Higashibayashi S, Sugai T, Imagawa H, Kubo M, Fukuyama Y, Ōmura S, Yamamoto H
Chemistry. 2021 Jan 2

A total synthesis of dehydroantofine was achieved by employing a novel, regioselective azahetero Diels-Alder reaction of the easily accessible 3,5-dichloro-2 H -1,4-oxazin-2-one with 4-ethynyl-1,2-dimethoxybenzene as a key step.

NOT Open Access | In vitro evaluation and molecular dynamics, DFT guided investigation of antimalarial activity of ethnomedicinally used Coptis teeta Wall

January 20, 2021 - 06:16 -- NOT Open Access
Goswami AK, Sharma HK, Gogoi N, Kashyap A, Gogoi BJ
Comb Chem High Throughput Screen. 2021 Jan 17

Malaria is caused by different species of Plasmodium; among which P. falciparum is the most severe. Coptis teeta is an ethnomedicinal plant of enormous importance for tribes of north east India.


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