Antiplasmodial potential of compounds isolated from Ziziphus mucronata and their binding to Plasmodium falciparum HGXPRT using biophysical and molecular docking studies.

The increasing resistance of Plasmodium parasites to currently available antiplasmodial therapies poses a significant challenge in treating malaria. Since ancient times, plants have served as a primary source of novel pharmacologically active compounds for drug development. Therefore, this study aimed to explore the antiplasmodial properties of pentacyclic triterpenes isolated from Ziziphus mucronata bark, with an emphasis on their mechanism of action.

A promising class of antiprotozoal agents, design and synthesis of novel Pyrimidine-Cinnamoyl hybrids.

Malaria, caused by parasitic protozoans of the Plasmodium genus, continues to be one of the greatest global health crises, especially in Africa. The emergence of antimalarial drug resistance continues to be a health problem necessitating an urgent need for alternative and cost-effective antimalarials. Using a molecular hybridization approach, we report the design and synthesis of an efficacious novel class of antiprotozoal agents; (E)-1-(4-(4,6-diphenylpyrimidin-2-yl)piperazin-1-yl)-3-phenyl prop-2-en-1-one derivatives (8a-r).

Investigation into the Interaction between Penicillin-Resistant and Penicillin-Susceptible Gonococcal Penicillin-Binding Protein 2 and Target Phenolic Ligands through Molecular Docking Studies and Structure-Activity Relationship Analysis.

Gonococcal infections present a notable public health issue, and the major approach for treatment involves using -lactam antibiotics that specifically target penicillin-binding protein 2 (PBP2) in . This study examines the influence of flavonoids, namely, rutin, on the structural changes of PBP2 in both penicillin-resistant (FA6140) and penicillin-susceptible (FA19) strains. The research starts by clarifying the structural effects of certain mutations, such as the insertion of an aspartate residue at position 345 (Asp-345a), in the PBP2.

Rational design and application of broad-spectrum antibodies for Bt Cry toxins determination.

Using the amino acid sequences and analysis of selected known structures of Bt Cry toxins, Cry1Ab, Cry1Ac, Cry1Ah, Cry1B, Cry1C and Cry1F we specifically designed immunogens. After antibodies selection, broad-spectrum polyclonal antibodies (pAbs) and monoclonal antibody (namely 1A0-mAb) were obtained from rabbit and mouse, respectively. The produced pAbs displayed broad spectrum activity by recognizing Cry1 toxin, Cry2Aa, Cry2Ab and Cry3Aa with half maximal inhibitory concentration (IC) values of 0.

A systematic review of Neisseria gonorrhoeae drug resistance development in South Africa.

In South Africa, basic healthcare centres treat sexually transmitted infections (STIs) using a syndromic approach. In line with Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) recommendations, a complete study of all randomised controlled trials and surveillance data relevant to N. gonorrhoeae antibiotic resistance was conducted.

An Exploratory Review of the Potential of Lytic Proteins and Bacteriophages for the Treatment of Tuberculosis.

Tuberculosis (TB) is a highly prevalent infectious disease that causes more than 1.5 million deaths a year. More than 25% of TB deaths occur in Africa, and TB is South Africa's leading cause of death, with about 89,000 people dying of it yearly.

Ursolic acid acetate and iso-mukaadial acetate bind to Plasmodium falciparum Hsp90, abrogating its chaperone function in vitro.

Plasmodium falciparum is the most lethal malaria parasite. Increasing incidences of drug resistance of P. falciparum have prompted the need for discovering new and effective antimalarial compounds with an alternative mode of action.

A Systematic Review of Endemic to South Africa: Phytochemistry, Pharmacology, and Toxicology.

The use of traditional medicine in treating a variety of both human and animal infections is ancient and still relevant. This is due to the resistance exhibited by most pathogenic microbial stains to currently-used antibiotics. The current work reports the phytochemistry, ethno-medicinal uses, toxicology, and most important pharmacological activities that validate the use of the plant species in African traditional medicine.

Establishment of novel receptor-antibody sandwich assays to broadly detect Bacillus thuringiensis Cry1 and Cry2 toxins.

Bacillus thuringiensis (Bt) Cry toxins have been widely used in the development of genetically modified organisms (GMOs) for pest control. This work aimed to establish more cost effective and broader detection methods for commonly used Cry toxins. Using ligand blot and bio-layer interferometry, we confirmed that a recombinant toxin-binding fragments derived from Helicoverpa armigera cadherin-like protein (HaCad-TBR) could broadly bind Cry1Ab, Cry1Ac, Cry2Aa, and Cry2Ab with the affinity of 0.

Evaluation of Antimicrobial Activity by Marine against Foodborne and Shiga Toxin-Producing .

The emergence of multidrug-resistant pathogens creates public health challenges, prompting a continuous search for effective novel antimicrobials. This study aimed to isolate marine actinomycetes from South Africa, evaluate their in vitro antimicrobial activity against and Shiga toxin-producing , and characterize their mechanisms of action. Marine actinomycetes were isolated and identified by 16S rRNA sequencing.

South Africa's indigenous microbial diversity for industrial applications: A review of the current status and opportunities.

The unique metagenomic, metaviromic libraries and indigenous micro diversity within Southern Africa have the potential for global beneficiation in academia and industry. Microorganisms that flourish at high temperatures, adverse pH conditions, and high salinity are likely to have enzyme systems that function efficiently under those conditions. These attributes afford researchers and industries alternative approaches that could replace existing chemical processes.

Screening of Antimicrobial Properties and Bioactive Compounds of Extracts against and .

In recent years, the potential of pathogenic bacteria to acquire resistance to a variety of antimicrobial drugs has developed significantly due to the indiscriminate exposure of a number of antibiotic compounds. The purpose of this study is to determine the antibacterial capabilities and activities of crude extracts against (ATCC 25923), (ATCC 25922), (ATCC 49926), and nine multidrug-resistant clinical isolates of . All of these isolates exhibited sensitivity to azithromycin and ceftriaxone, while the majority of antibiotic resistance was seen against penicillin G, sulphonamide, and ciprofloxacin.

Identification of Emerging Multidrug-Resistant Isolates against Five Major Antimicrobial Agent Options.

Antimicrobial drug resistance in has been documented all over the world. However, the situation in Sub-Saharan Africa has received little attention. It is critical to establish diagnostics and extend surveillance in order to prevent the emergence of illnesses that are resistant to several treatments.

Chemical Profile, Antioxidant and Antibacterial Activities, Mechanisms of Action of the Leaf Extract of Mill.

Mill's extracts have been explored for antibacterial and antioxidant efficacies. However, there is limited information on its chemical composition and mechanism of action. The purpose of this study was to assess the chemical composition, antibacterial and antioxidant activities and mechanism of the whole leaf extract of Mill.

Improved sensitivity of the anti-microcystin-LR ELISA using phage-displayed alpha-type anti-idiotypic nanobody.

Anti-idiotypic antibodies (Ab2) are valuable tools that can be used for a better understanding of molecular mimicry and the immunological network. In this work, we showed a new application of a phage-displayed alpha-type Ab2 (Ab2α) to improve the sensitivity of an enzyme-linked immunosorbent assay (ELISA) detecting cyanobacterial toxin microcystin-LR (MC-LR). A monoclonal antibody (mAb) against MC-LR was used as an antigen to isolate binders in a camelid nanobody library.

Bioprospecting of endophytic actinobacterium associated with Aloe ferox mill for antibacterial activity.

Background: The emergence of drug resistance among pathogens has resulted in renewed interest in bioprospecting for natural microbial products.

Methods: This study aimed to bioprospecting endophytic actinobacterium associated with Aloe ferox Mill for its antibacterial activity. Endophytic actinomycetes were isolated from the gel of A.

Generation of Human Domain Antibody Fragments as Potential Insecticidal Agents against by Cadherin-Based Screening.

New insecticidal genes and approaches for pest control are a hot research area. In the present study, we explored a novel strategy for the generation of insecticidal proteins. The midgut cadherin of () was used as a target to screen materials that have insecticidal activity.

Protein PEGylation: Navigating Recombinant Protein Stability, Aggregation, and Bioactivity.

Enzymes play a powerful role as catalysts with high specificity and activity under mild environmental conditions. Significant hurdles, such as reduced solubility, reduced shelf-life, aggregate formation, and toxicity, are still ongoing struggles that scientists come across when purifying recombinant proteins. Over the past three decades, PEGylation techniques have been utilized to significantly overcome low solubility; increased protein stability, shelf-life, and bioactivity; and prevented protein aggregate formation.

The Effect of Supplementing Mushroom Growing Substrates on the Bioactive Compounds, Antimicrobial Activity, and Antioxidant Activity of .

mushroom contains important bioactive compounds and has several biological activities; however, mushroom growing substrates have major influence on chemical and functional characteristics of the mushroom. Hence, the study aimed to evaluate the influence of supplementing mushroom growing substrates with wheat bran (WB) towards yield/productivity, bioactive compounds, and antimicrobial and antioxidant activity of . .

Recombinant Expression, Purification and PEGylation of DNA Ligases.

Background: Reagent proteins such as DNA ligases play a central role in the global reagents market. DNA ligases are commonly used and are vital in academic and science research environments. Their major functions include sealing nicks by linking the 5'-phosphorylated end to a 3'-hydroxyl end on the phosphodiester backbone of DNA, utilizing ATP or NADP molecules as an energy source.

Reverse vaccinology approach to design a multi-epitope vaccine construct based on the Mycobacterium tuberculosis biomarker PE_PGRS17.

Mycobacterium tuberculosis (Mtb) is responsible for high mortality rates in many low- and middle-income countries. This infectious disease remains accountable for around 1.4 million deaths yearly.

Identification of single domain antibodies with insect cytotoxicity using phage-display antibody library screening and Plutella xylostella ATP-binding cassette transporter subfamily C member 2 (ABCC2) -based insect cell expression system.

It is extremely imminent to study a new strategy to manage agricultural pest like Plutella xylostella (P. xylostella) which is currently resistant to most of pesticides, including three domain-Cry toxins from Bacillus thuringiensis (Bt). In this study, we reported a phage displayed single domain antibody screening from human domain antibody (DAb) library targeted on Spodoptera frugiperda 9 (Sf9) cells expressed Cry1Ac toxin receptor, ATP-dependent binding cassette transporter C2 in P.

Lactate dehydrogenase and malate dehydrogenase: Potential antiparasitic targets for drug development studies.

Parasitic diseases remain a major public health concern for humans, claiming millions of lives annually. Although different treatments are required for these diseases, drug usage is limited due to the development of resistance and toxicity, which necessitate alternative therapies. It has been shown in the literature that parasitic lactate dehydrogenases (LDH) and malate dehydrogenases (MDH) have unique pharmacological selective and specificity properties compared to other isoforms, thus highlighting them as viable therapeutic targets involved in aerobic and anaerobic glycolytic pathways.

Iso-mukaadial acetate and ursolic acid acetate inhibit the chaperone activity of Plasmodium falciparum heat shock protein 70-1.

Plasmodium falciparum is the most lethal malaria parasite. The present study investigates the interaction capabilities of select plant derivatives, iso-mukaadial acetate (IMA) and ursolic acid acetate (UAA), against P. falciparum Hsp70-1 (PfHsp70-1) using in vitro approaches.

Design and synthesis of quinoline-pyrimidine inspired hybrids as potential plasmodial inhibitors.

Presently, artemisinin-based combination therapy (ACT) is the first-line therapy of Plasmodium falciparum malaria. With the emergence of malaria parasites that are resistant to ACT, alternative antimalarial therapies are urgently needed. In line with this, we designed and synthesised a series of novel N-(7-chloroquinolin-4-yl)-N'-(4,6-diphenylpyrimidin-2-yl)alkanediamine hybrids (6a-7c) and evaluated their inhibitory activity against the NF54 chloroquine-susceptible strain as a promising class of antimalarial compounds.