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anti-malarial

NOT Open Access | Identification and structure-activity relationship (SAR) studies of carvacrol derivatives as potential anti-malarial against Plasmodium falciparum falcipain-2 protease

October 1, 2020 - 07:50 -- NOT Open Access
Author(s): 
Uddin A, Singh V, Irfan I, Mohammad T, Singh Hada R, Imtaiyaz Hassan M, Abid M, Singh S
Reference: 
Bioorg Chem. 2020 Oct;103:104142

In an effort to develop a potent anti-malarial agent against Plasmodium falciparum, a structure-guided virtual screening using an in-house library comprising 652 compounds was performed. By docking studies, we identified two compounds (JMI-105 and JMI-346) which formed significant non-covalent interactions and fit well in the binding pocket of PfFP-2. We affirmed this observation by MD simulation studies.

NOT Open Access | Structure activity studies of truncated latrunculin analogues with anti-malarial activity

September 16, 2020 - 13:05 -- NOT Open Access
Author(s): 
Varghese S, Rahmani R, Drew DR, Beeson JG, Baum J, Smith BJ, Baell J
Reference: 
ChemMedChem. 2020 Sep 14

Malarial parasites employ actin dynamics for motility, and any disruption to these dynamics renders the parasites unable to effectively establish infection. Therefore, actin presents a potential target for malarial drug discovery, and naturally occurring actin inhibitors such as latrunculins are a promising starting point.

Screening for malaria antigen and anti-malarial IgG antibody in forcibly-displaced Myanmar nationals: Cox’s Bazar district, Bangladesh, 2018

March 31, 2020 - 15:35 -- Open Access
Author(s): 
Austin Lu, Olivia Cote, Eric Rogier, et al.
Reference: 
Malaria Journal 2020 19:130, 30 March 2020

Several refugee settlements in Bangladesh have provided housing and medical care for the forcibly-displaced Myanmar nationals (FDMN, also known as Rohingya) population. The identification of malaria infection status in the refugee settlements is useful in treating infected persons and in developing malaria prevention recommendations. Assays for Plasmodium antigens and human IgG against Plasmodium parasites can be used as indicators to determine malaria infection status and exposure.

NOT Open Access | The C-terminal region of the Plasmodium yoelii microgamete surface antigen PyMiGS induces potent anti-malarial transmission-blocking immunity in mice

March 17, 2020 - 12:55 -- NOT Open Access
Author(s): 
Tachibana M, Baba M, Takashima E, Tsuboi T, Torii M, Ishino T
Reference: 
Vaccine Volume 38, Issue 15, 30 March 2020, Pages 3129-3136

Malaria transmission-blocking vaccines (TBVs) aim to inhibit parasite fertilization or further development within the mosquito midgut. Because TBV-immunized individuals reduce the transmission of malaria parasites to mosquito vectors, TBVs could serve as a promising strategy to eliminate malaria.

NOT Open Access | Inhibition of Hemoglobin Degrading Protease Falcipain-2 as a Mechanism for Anti-Malarial Activity of Triazole-Amino Acid Hybrids

February 22, 2020 - 17:00 -- NOT Open Access
Author(s): 
Vigyasa Singh, Rahul Singh Hada, Amaduddin, Babita Aneja, Mohammad Abid, Kailash C. Pande, Shailja Singh
Reference: 
Current Topics in Medicinal Chemistry, 11/02/20

Novel drug development against malaria parasite over the old conventional anti-malarial drugs is essential due to rapid and indiscriminate use of drugs, which led to the emergence of resistant strains. In this study, previously reported triazole-amino acid hybrids (13-18) have been explored against Plasmodium falciparum as antimalarial agents. Among the six compounds, 15 and 18 exhibited antimalarial activity against P. falciparum with insignificant hemolytic activity and cytotoxicity towards HepG2 mammalian cells. Antimalarial half-maximal inhibitory concentration (IC50) of 15 and 18 compounds was found to be 9.26 μM and 20.62 μM, respectively.

An in vitro toolbox to accelerate anti-malarial drug discovery and development

January 6, 2020 - 16:26 -- Open Access
Author(s): 
Susan A. Charman, Alice Andreu, Nada Abla, et al.
Reference: 
Malaria Journal 2020 19:1, 2 January 2020

Modelling and simulation are being increasingly utilized to support the discovery and development of new anti-malarial drugs. These approaches require reliable in vitro data for physicochemical properties, permeability, binding, intrinsic clearance and cytochrome P450 inhibition. This work was conducted to generate an in vitro data toolbox using standardized methods for a set of 45 anti-malarial drugs and to assess changes in physicochemical properties in relation to changing target product and candidate profiles.

Anti-malarial ozonides OZ439 and OZ609 tested at clinically relevant compound exposure parameters in a novel ring-stage survival assay

December 23, 2019 - 15:09 -- Open Access
Author(s): 
Annabelle Walz, Didier Leroy, Nicole Andenmatten, Pascal Mäser and Sergio Wittlin
Reference: 
Malaria Journal 2019 18:427, 18 December 2019

Drug efficacy against kelch 13 mutant malaria parasites can be determined in vitro with the ring-stage survival assay (RSA). The conventional assay protocol reflects the exposure profile of dihydroartemisinin.

In vitro anti-malarial efficacy of chalcones: cytotoxicity profile, mechanism of action and their effect on erythrocytes

December 17, 2019 - 16:41 -- Open Access
Author(s): 
Shweta Sinha, Daniela I. Batovska, Bikash Medhi, B. D. Radotra, Ashish Bhalla, Nadezhda Markova and Rakesh Sehgal
Reference: 
Malaria Journal 2019 18:421, 16 December 2019

Malaria extensively leads to mortality and morbidity in endemic regions, and the emergence of drug resistant parasites is alarming. Plant derived synthetic pharmaceutical compounds are found to be a foremost research to obtain diverse range of potent leads. Amongst them, the chalcone scaffold is a functional template for drug discovery. The present study involves synthesis of ten chalcones with various substitution pattern in rings A and B and assessment of their anti-malarial efficacy against chloroquine sensitive and chloroquine resistant strains as well as of their cytotoxicity and effect on haemozoin production.

Not Open Access | Historical and experimental evidence for enhanced concentration of artemesinin, a global anti-malarial treatment, with recent and projected increases in atmospheric carbon dioxide

May 5, 2015 - 15:34 -- NOT Open Access
Author(s): 
C. Zhu, Q. Zeng, L.H. Ziska, et al.
Reference: 
Climatic Change, May 2015

In this study, artemesinin concentration was quantified for multiple A. annua populations in China using a free-air CO2 enrichment (FACE) system as a function of [CO2]-induced changes both in situ and as a function of the foliar ratio of carbon to nitrogen (C:N).

Multinormal in vitro distribution of Plasmodium falciparum susceptibility to piperaquine and pyronaridine

February 27, 2015 - 16:19 -- Open Access
Author(s): 
Aurélie Pascual, Marilyn Madamet, Sébastien Briolant, Tiphaine Gaillard, Rémy Amalvict, Nicolas Benoit, Dominique Travers, Bruno Pradines
Reference: 
Malaria Journal 2015, 14:49 (5 February 2015)

Dihydroartemisinin-piperaquine and artesunate-pyronaridine are two of these new combinations. The aim of the present work was to assess the distribution of the in vitro values of pyronaridine (PND) and piperaquine (PPQ) and to define a cut-off for reduced susceptibility for the two anti-malarial drugs.

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