A5101497681- Research on Leishmaniasis Studies
- Drug Transport and Resistance Mechanisms
- Synthesis and biological activity
- Malaria Research and Control
- Synthesis and Biological Evaluation
- Pharmacogenetics and Drug Metabolism
- Trypanosoma species research and implications
- Neonatal Health and Biochemistry
- Bioactive Compounds and Antitumor Agents
- Polyamine Metabolism and Applications
- Traditional and Medicinal Uses of Annonaceae
- Natural product bioactivities and synthesis
- Biochemical and Molecular Research
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Phytochemical compounds biological activities
- Amino Acid Enzymes and Metabolism
- HIV/AIDS drug development and treatment
- Erythrocyte Function and Pathophysiology
- Drug-Induced Hepatotoxicity and Protection
- Protein Degradation and Inhibitors
- Synthesis and Characterization of Heterocyclic Compounds
- Methemoglobinemia and Tumor Lysis Syndrome
- Phytochemistry and Biological Activities
- Mosquito-borne diseases and control
Southern Research Institute
2024
University of Mississippi
2012-2021
Tafila Technical University
2018
Pharmacology Research Institute
2012
National Center for Agricultural Utilization Research
2008
United States Department of Agriculture
2008
University of California, San Francisco
2006
San Francisco General Hospital
2006
McGill University
2004
Xavier University
2004
Hypocrellins A and B were evaluated for in vitro antimicrobial antileishmanial activities. Hypocrellin exhibited promising activity against Candida albicans moderate Staphylococcus aureus, methicillin-resistant S. Pseudomonas aeruginosa, Mycobacterium intracellulare. showed weak potent activity, while hypocrellin was only moderately active. These results of antifungal may be useful further structure-activity relationship vivo studies.
Primaquine (PQ) metabolism by the cytochrome P450 (CYP) 2D family of enzymes is required for antimalarial activity in both humans (2D6) and mice (2D). Human CYP 2D6 highly polymorphic, decreased enzyme has been linked to PQ activity. Despite importance efficacy, exact role that these play pharmacokinetics not extensively studied vivo. In this study, a series pharmacokinetic experiments were conducted with differential characteristics, including wild-type (WT), knockout (KO), humanized...
Artemisinin (1) and its analogues have been well studied for their antimalarial activity. Here we present the activity of some novel C-9-modified artemisinin synthesized using artemisitene as key intermediate. Further, antileishmanial more than 70 derivatives against Leishmania donovani promastigotes is described first time. A comprehensive structure−activity relationship study CoMFA discussed. These exhibited leishmanicidal in micromolar concentrations, overall profile appears to be similar...
Machaerium multiflorum yielded two additional new (+)-trans-hexahydrodibenzopyrans (HHDBP's), machaeriol C (1) and D (2), three 5,6-seco-HHDBP's, machaeridiol A (3), B (4), (5). Their structures stereochemistries were determined by 1D 2D NMR data, including HMBC, NOESY, circular dichroism experiments. Machaeriol demonstrated in vitro antibacterial activity against Staphylococcus aureus (IC50 0.65 μg/mL) methicillin-resistant S. (MRSA) 0.70 μg/mL), while its corresponding 5,6-seco-analogues...
The incidence of parasitic infections such as malaria, leishmaniasis, and trypanosomiasis has been steadily increasing. Since the existing chemotherapy these diseases suffers from lack safe effective drugs and/or presence widespread drug resistance, there is an urgent need for development potent, mechanism-based antiparasitic agents against diseases. Cysteine proteases have established valid targets this purpose. Available Chemical Directory consisting nearly 355 000 compounds was screened...
Abstract A bioassay‐guided fractionation of Juniperus procera berries yielded antiparasitic, nematicidal and antifouling constituents, including a wide range known abietane, pimarane labdane diterpenes. Among these, abieta‐7,13‐diene (1) demonstrated in vitro antimalarial activity against Plasmodium falciparum D6 W2 strains (IC 50 = 1.9 2.0 µg/mL, respectively), while totarol (6), ferruginol (7) 7 β ‐hydroxyabieta‐8,13‐diene‐11,12‐dione (8) inhibited Leishmania donovani promastigotes with IC...
Plasmodium falciparum lactate dehydrogenase (pfLDH) is a key enzyme for energy generation of malarial parasites and potential antimalarial chemotherapeutic target. It known that the oxamate moiety, pyruvate analog, alone shows higher inhibition against pfLDH than human LDHs, suggesting it can be used development selective inhibitors. Oxamic acid derivatives were designed synthesized. Derivatives 5 7 demonstrated activities with IC50 values 3.13 1.75 μM, respectively, have 59- 7-fold...
Inhibition of histone deacetylase (HDAC) function is a validated therapeutic strategy for cancer treatment. Of the several structurally distinct small molecule inhibitors (HDACi) reported, macrocyclic depsipeptides possess most complex cap groups and have demonstrated excellent HDAC inhibition potency isoform selectivity. Unfortunately, development has been hampered in part because problems characteristic large peptides reaction schemes required their synthesis. Herein we report that...
ABSTRACT Cytochrome P450 (CYP) 2D metabolism is required for the liver-stage antimalarial efficacy of 8-aminoquinoline molecule tafenoquine in mice. This could be problematic Plasmodium vivax radical cure, as human CYP ortholog (2D6) highly polymorphic. Diminished 2D6 enzyme activity, poor-metabolizer phenotype, compromise curative humans. Despite importance efficacy, exact role that plays and pharmacokinetics other molecules has not been extensively studied. In this study, a series...
Psychotria klugii yielded two new benzoquinolizidine alkaloids, klugine (1) and 7'-O-demethylisocephaeline (2), together with the previously known cephaeline (3), isocephaeline (4), 7-O-methylipecoside (5). The structures stereochemistry of 1 2 were determined by 1D 2D NMR data circular dichroism experiments. Cephaeline (3) demonstrated potent in vitro antileishmanial activity against Leishmania donavani (IC50 0.03 μg/mL) was >20- >5-fold more than pentamidine amphotericin B, respectively,...
S-Adenosylmethionine decarboxylase (AdoMetDC) is a pyruvoyl enzyme, and the pyruvate formed in an intramolecular reaction that cleaves proenzyme precursor converts serine residue into pyruvate. The wild type potato AdoMetDC processed much faster than human did not require putrescine for optimal rate of processing despite presence three acidic residues (equivalent to Glu11, Glu178, Glu256) were demonstrated previous studies be required activation (Stanley, B. A., Shantz, L. M., Pegg, A. E....
Significance This article describes the development and validation of a novel mouse model that can be used to predict hemolytic toxicity drugs occurs in individuals with an enzyme deficiency known as glucose-6-phosphate dehydrogenase (G6PD) deficiency. G6PD affects more than 400 million people worldwide. In this model, nonobese diabetic/SCID mice are transfused human RBCs from G6PD-deficient donors. Treatment cause anemia humans do not damage nor normal RBCs; but robust response is observed...