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drug resistance

Synthesis and Antiplasmodial Activity of Novel Fosmidomycin Derivatives and Conjugates with Artemisinin and Aminochloroquinoline

October 31, 2020 - 10:00 -- Open Access
Author(s): 
Palla D, Antoniou AI, Baltas M, Menendez C, Grellier P, Mouray E, Athanassopoulos CM.
Reference: 
Molecules. 2020 Oct 21;25(20):E4858

Malaria, despite many efforts, remains among the most problematic infectious diseases worldwide, mainly due to the development of drug resistance by Plasmodium falciparum. The antibiotic fosmidomycin (FSM) is also known for its antimalarial activity by targeting the non-mevalonate isoprenoid synthesis pathway, which is essential for the malaria parasites but is absent in mammalians.

Not Open Access | Describing the current status of Plasmodium falciparum population structure and drug resistance within mainland Tanzania using molecular inversion probes

October 28, 2020 - 10:19 -- NOT Open Access
Author(s): 
Moser KA, Madebe RA, Bailey JA, et al.
Reference: 
Mol Ecol. 2020 Oct 26

High-throughput Plasmodium genomic data is increasingly useful in assessing prevalence of clinically important mutations and malaria transmission patterns. Understanding parasite diversity is important for identification of specific human or parasite populations that can be targeted by control programs, and to monitor the spread of mutations associated with drug resistance. An up-to-date understanding of regional parasite population dynamics is also critical to monitor the impact of control efforts.

Not Open Access | Nanotized curcumin-benzothiophene conjugate: A potential combination for treatment of cerebral malaria

October 13, 2020 - 12:50 -- NOT Open Access
Author(s): 
Ghosh A, Banerjee T
Reference: 
IUBMB Life. 2020 Oct 9.

The declining effectiveness of the available antimalarial drugs due to drug resistance requires a continued effort to develop new therapeutic approaches. In this context, combination therapies hold a great promise for developing effective first-line antimalarial treatments for reducing malaria mortality. The present study explores the antimalarial efficacy of nanotized formulation of curcumin in combination with benzothiophene compound 6 (3-bromo-N-(4-fluorobenzyl)-benzo[b]thiophene-2-carboxamide) with a view to achieve better efficacy at a very low dose in comparison to that accomplished with monotherapy alone.

NOT Open Access | Associations between malaria preventive regimens and Plasmodium falciparum drug resistance mediating polymorphisms in Ugandan pregnant women

October 7, 2020 - 15:35 -- NOT Open Access
Author(s): 
Nayebare P, Asua V, Conrad MD, Kajubi R, Kakuru A, Nankabirwa JI, Muhanguzi D, Dorsey G, Kamya MR, Nsobya S, Rosenthal PJ
Reference: 
Antimicrob Agents Chemother. 2020 Oct 5:AAC.01047-20

Intermittent preventive treatment in pregnancy (IPTp) with monthly sulfadoxine-pyrimethamine (SP) is recommended for malaria-endemic parts of Africa, but efficacy is compromised by resistance and, in recent trials, dihydroartemisinin-piperaquine (DP) has shown better antimalarial protective efficacy. We utilized blood samples from a recent trial to evaluate selection by IPTp with DP or SP of Plasmodium falciparum genetic polymorphisms that alter susceptibility to these drugs.

NOT Open Access | Combination between antibacterial and antifungal antibiotics with phytocompounds of Artemisia annua L: A strategy to control drug resistance pathogens

October 1, 2020 - 15:50 -- NOT Open Access
Author(s): 
Rolta R, Sharma A, Sourirajan A, Mallikarjunan PK, Dev K
Reference: 
J Ethnopharmacol. 2020 Sep 27:113420

Artemisia annua L. is a traditional Chinese medicine used for the treatment of malaria, jaundice and intense fever.

NOT Open Access | The use of proteomics for the identification of promising vaccine and diagnostic biomarkers in Plasmodium falciparum

October 1, 2020 - 07:52 -- NOT Open Access
Author(s): 
Mansouri R, Ali-Hassanzadeh M, Shafiei R, Savardashtaki A, Karimazar M, Anvari E, Nguewa P, Rashidi S
Reference: 
Parasitology. 2020 Oct;147(12):1255-1262

Plasmodium falciparum is the main cause of severe malaria in humans that can lead to death. There is growing evidence of drug-resistance in P. falciparum treatment, and the design of effective vaccines remains an ongoing strategy to control the disease. On the other hand, the recognition of specific diagnostic markers for P. falciparum can accelerate the diagnosis of this parasite in the early stages of infection.

NOT Open Access | Synthesis, structure-activity relationship and antimalarial efficacy of 6-chloro-2-arylvinylquinolines

September 23, 2020 - 09:30 -- NOT Open Access
Author(s): 
Huang G, Murillo Solano C, Yuan Y, et al.
Reference: 
J Med Chem. 2020 Sep 22

There is an urgent need to develop new efficacious antimalarials to address the emerging drug-resistant clinical cases. Our previous phenotypic screening identified styrylquinoline UCF501 as a promising antimalarial compound.

Promising nanomaterials in the fight against malaria

September 23, 2020 - 08:50 -- Open Access
Author(s): 
Neves Borgheti-Cardoso L, San Anselmo M, Lantero E, Lancelot A, Serrano JL, Hernández-Ainsa S, Fernàndez-Busquets X, Sierra T
Reference: 
J Mater Chem B. 2020 Sep 21

For more than one hundred years, several treatments against malaria have been proposed but they have systematically failed, mainly due to the occurrence of drug resistance in part resulting from the exposure of the parasite to low drug doses. Several factors are behind this problem, including (i) the formidable barrier imposed by the Plasmodium life cycle with intracellular localization of parasites in hepatocytes and red blood cells, (ii) the adverse fluidic conditions encountered in the blood circulation that affect the interaction of molecular components with target cells, and (iii) the unfavorable physicochemical characteristics of most antimalarial drugs, which have an amphiphilic character and can be widely distributed into body tissues after administration and rapidly metabolized in the liver.

Distribution pattern of amino acid mutations in chloroquine and antifolate drug resistance associated genes in complicated and uncomplicated Plasmodium vivax isolates from Chandigarh, North India

September 16, 2020 - 13:09 -- Open Access
Author(s): 
Kaur H, Sehgal R, Kumar A, Bharti PK, Bansal D, Mohapatra PK, Mahanta J, Sultan AA
Reference: 
BMC Infect Dis. 2020 Sep 15;20(1):671

The increasing antimalarial drug resistance is a significant hindrance to malaria control and elimination programs. For the last six decades, chloroquine (CQ) plus pyrimethamine remains the first-line treatment for P. vivax malaria. Regions where both P. falciparum and P. vivax co-exist, P. vivax is exposed to antifolate drugs due to either misdiagnosis or improper treatment that causes selective drug pressure to evolve. Therefore, the present study aims to estimate antimalarial drug resistance among the complicated and uncomplicated P. vivax patients.

NOT Open Access | Humanized Mice and the Rebirth of Malaria Genetic Crosses

September 15, 2020 - 15:07 -- NOT Open Access
Author(s): 
Vendrely KM, Kumar S, Li X, Vaughan AM
Reference: 
Trends Parasitol. 2020 Sep 2:S1471-4922(20)30192-6

The first experimental crosses carried out with the human malaria parasite Plasmodium falciparum played a key role in determining the genetic loci responsible for drug resistance, virulence, invasion, growth rate, and transmission.

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