Institute of Pharmaceutical and Medicinal Chemistry, Heinrich Heine University Düsseldorf, Universitätsstr. 1, 40225, Düsseldorf, Germany. Electronic address:
Published: November 2019
AI Article Synopsis
Article Abstract
Thia analogs of fosmidomycin are potent inhibitors of the non-mevalonate isoprenoid biosynthesis enzyme 1-deoxy-d-xylulose 5-phosphate reductoisomerase (IspC, Dxr) of Plasmodium falciparum. Several new thioethers displayed antiplasmodial in vitro activity in the low nanomolar range, without apparent cytotoxic effects in HeLa cells. The (S)-(+)-enantiomer of a typical representative selectively inhibited IspC and the growth of P. falciparum in continuous culture. The inhibitor was stable at pH 7.6 and room temperature, and no racemization was observed under these conditions during a period of up to two days. Oxidation of selected thioethers to sulfones reduced antiplasmodial activity and the inhibitory activity against Escherichia coli, Mycobacterium tuberculosis and P. falciparum IspC orthologs.
This study focused on the synthesis, structural validation, and evaluation of the antiplasmodial efficacy of brachangobinan A (BA) and its enantiomers, (+)-BA and (-)-BA, as potential antimalarial agents. BA, (+)-BA, and (-)-BA were synthesized through chemical processes and validated via advanced spectroscopic techniques. In vitro studies were conducted to assess their efficacy against Plasmodium falciparum strains 3D7 and K1 by determining their half maximal inhibitory concentration (IC) values, cytotoxicity profiles, and selectivity indices.
National Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, MS 38655, USA; Department of Biomolecular Sciences, Division of Pharmacognosy, School of Pharmacy, University of Mississippi, Oxford, MS 38677, USA. Electronic address:
Brazilian Red Propolis (BRP) is a natural product known for its rich chemical composition and therapeutic potential. This study investigates the phytochemical profile and evaluates the cytotoxic, antiplasmodial, and antimicrobial properties of red propolis extract and its isolated compounds vestitol (1), neovestitol (2), medicarpin (3), 7-O-methylvestitol (4), and oblongifolin B (5). The extract showed selective cytotoxicity against cancer cell lines (IC: 16-39 μg/mL).
Marine sponge diterpenoid isonitriles are exceptional nitrogenous natural products that exhibit antiplasmodial activity. Their biosynthesis presents a biosynthetic puzzle: how do the elements of NC engage terpenyl carbocations in isoprenoid secondary metabolism, and what is the biosynthetic precursor of the NC group? Cyanoformic acid (NC-COOH, ) is proposed as a plausible delivery vehicle of NC that resolves a paradox in the commonly held proposition that an inorganic cyanide anion, CN, terminates terpenoid isonitrile (TI) biosynthesis. DFT calculations of NC-COOH and its conjugate base, cyanoformate, NC-COO (), support high nucleophilicity at N and explain bond-forming constitutionality: attack at N and formation of an isonitrile over its nitrile isomer.
Malaria remains a significant global health challenge, with the deadliest infections caused by . In light of the escalating drug resistance and the limited effectiveness of available vaccines, innovative treatment approaches are urgently needed. This study explores the potential of the probiotic YZ01, isolated from traditionally fermented kindirmo milk, to modify host responses to ANKA infection.
Central Laboratory of The Lishui Hospital of Wenzhou Medical University, The First Affiliated Hospital of Lishui University, Lishui People's Hospital, Lishui, Zhejiang, 323000, China.
Natural products have perennially served as a cornerstone for the genesis of novel medicinal compounds. Most clinical therapeutics originate from ancestral herbal remedies and their formulations. Scholars and practitioners have always aimed to extract better remedies to treat various ailments.
