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Coumarins from as inhibitors of the tumour-associated carbonic anhydrases IX and XII: isolation, biological studies and in silico evaluation

J Enzyme Inhib Med Chem. 2020-12-01; 
Benedetta Fois, Simona Distinto, Rita Meleddu, Serenella Deplano, Elias Maccioni, Costantino Floris, Antonella Rosa, Mariella Nieddu, Pierluigi Caboni, Claudia Sissi, Andrea Angeli, Claudiu T Supuran, Filippo Cottiglia
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Codon Optimization … Dueholm et al., 2015). Cloning of PsPT1 and PsPT2. The PsPT1 coding sequence was submitted to Genscript (http://www.genscript.com). This gene was synthesized using an N. benthamiana codon bias. The codon‐optimized … Get A Quote

摘要

In an screening for human carbonic anhydrase (hCA) inhibiting agents from higher plants, the petroleum ether and ethyl acetate extracts of seeds selectively inhibited hCA IX and hCA XII isoforms. The phytochemical investigation of the extracts led to the isolation of ten linear furocoumarins (-), four simple coumarins (-) and a new angular dihydrofurocoumarin (). The structures of the isolated compounds were elucidated based on 1?D and 2?D NMR, MS, and ECD data analysis. All isolated compounds were inactive towards the ubiquitous cytosolic isoform hCA I and II (?>?10,000?nM) while they were significantly active against the tumour-associated isoforms hCA IX and XII. Umbelliprenin was the most potent ... More

關鍵詞

Carbonic anhydrase, Magydaris pastinacea, coumarin, inhibitor, natural product
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