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anti-malarial

Identification of Plasmodium falciparum heat shock 90 inhibitors via molecular docking

March 2, 2021 - 15:08 -- Open Access
Author(s): 
Everson N, Bach J, Hammill JT, Falade MO, Rice AL, Guy RK, Eagon S
Reference: 
Bioorg Med Chem Lett. 2021 Mar 1;35:127818

A virtual screen was performed to identify anti-malarial compounds targeting Plasmodium falciparum heat shock 90 protein by applying a series of drug-like and commercial availability filters to compounds in the ZINC database, resulting in a virtual library of more than 13 million candidates. The goal of the virtual screen was to identify novel compounds which could serve as a starting point for the development of antimalarials with a mode of action different from anything currently used in the clinic.

Selecting an anti-malarial clinical candidate from two potent dihydroisoquinolones

February 23, 2021 - 14:17 -- Open Access
Author(s): 
Yizhe Chen, Fangyi Zhu, R. Kiplin Guy, et al.
Reference: 
Malaria Journal 2021 20:107, 19 February 2021

The ongoing global malaria eradication campaign requires development of potent, safe, and cost-effective drugs lacking cross-resistance with existing chemotherapies. One critical step in drug development is selecting a suitable clinical candidate from late leads. The process used to select the clinical candidate SJ733 from two potent dihydroisoquinolone (DHIQ) late leads, SJ733 and SJ311, based on their physicochemical, pharmacokinetic (PK), and toxicity profiles is described.

Development and evaluation of a new Plasmodium falciparum 3D7 blood stage malaria cell bank for use in malaria volunteer infection studies

February 17, 2021 - 09:02 -- Open Access
Author(s): 
Stephen D. Woolley, Melissa Fernandez, Bridget E. Barber, et al.
Reference: 
Malaria Journal 2021 20:93, 16 February 2021

New anti-malarial therapeutics are required to counter the threat of increasing drug resistance. Malaria volunteer infection studies (VIS), particularly the induced blood stage malaria (IBSM) model, play a key role in accelerating anti-malarial drug development. Supply of the reference 3D7-V2 Plasmodium falciparum malaria cell bank (MCB) is limited. This study aimed to develop a new MCB, and compare the safety and infectivity of this MCB with the existing 3D7-V2 MCB, in a VIS. A second bank (3D7-V1) developed in 1995 was also evaluated.

Rapid ethnographic assessment for potential anti-malarial mass drug administration in an outbreak area of Santo Domingo, Dominican Republic

February 10, 2021 - 09:54 -- Open Access
Author(s): 
Hunter Keys, Keyla Ureña, Jhefres Reyes, Kevin Bardosh, Christopher Pell, Jose Puello, Stephen Blount and Gregory S. Noland
Reference: 
Malaria Journal 2021 20:76, 8 February 2021

In the Dominican Republic, a recent outbreak of malaria in the capital, Santo Domingo, threatens efforts to eliminate the disease. Mass drug administration (MDA) has been proposed as one strategy to reduce transmission. The success of MDA is contingent upon high levels of acceptance among the target population. To inform the design of future MDA campaigns, this rapid ethnographic assessment examined malaria-related knowledge and attitudes toward malaria MDA among residents of a transmission focus in Santo Domingo.

Multiplex-RT-PCR-ELISA panel for detecting mosquito-borne pathogens: Plasmodium sp. preserved and eluted from dried blood spots on sample cards

February 3, 2021 - 15:43 -- Open Access
Author(s): 
Philip Koliopoulos, Neema Mathias Kayange, Stephan Gehring, et al.
Reference: 
Malaria Journal 2021 20:66, 1 February 2021

Children are the most vulnerable group affected by malaria and other tropical, vector-borne diseases in low-resource countries. Infants presenting with acute onset fever represent a major sector of outpatient care in the Lake Victoria region. Misclassification and overuse of antibiotics and anti-malarial medications are consistent problems. Identifying the prevalent mosquito-borne pathogens in the region will reduce the prescription of non-indicated medicines.

In vivo anti-malarial activity of the hydroalcoholic extract of rhizomes of Kniphofia foliosa and its constituents

January 6, 2021 - 11:41 -- Open Access
Author(s): 
Yonatan Alebachew, Daniel Bisrat, Solomon Tadesse and Kaleab Asres
Reference: 
Malaria Journal 2021 20:3, January 2021

Kniphofia foliosa is a flamboyant robust perennial herb which has dense clumps and tick upright rhizomes with leaves at the base. In Ethiopia, it has several vernacular names including Abelbila, Ashenda, Amelmela, Yeznjero Ageda, Shemetmetie and Yezinjero Ageda. The plant is endemic to Ethiopian highlands, where its rhizomes are traditionally used for the treatment of malaria, abdominal cramps and wound healing. In the present study, the 80% methanol extract of K. foliosa rhizomes and its constituents are tested against Plasmodium berghei in mice.

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.

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