Polyamine conjugates of stigmasterol |
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| Authors: | Norbert Vida Hana Svobodová Lucie Rárová Pavel Drašar David Saman Josef Cvačka Zdeněk Wimmer |
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| Affiliation: | Institute of Chemical Technology, Faculty of Food and Biochemical Technology, Department of Chemistry of Natural Compounds, Technická 5, 16628 Prague 6, Czech Republic. |
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| Abstract: | Three new polyamine conjugates with stigmasterol [(3β,22E)-stigmasta-5,22-dien-3-ol] were synthesized and subjected to basic antimicrobial and cytotoxic tests. The conjugate derived from spermine, (3β,22E)-stigmasta-5,22-dien-3-yl 4(12-amino-4,9-diaza-dodecylamino)-4-oxobutanoate (5c), displayed considerable antimicrobial activity on Staphylococcus aureus at low concentration (50μgmL(-1)). The cytotoxic activity was tested on cells of human T-lymfoblastic leukemia (IC(50)=35.8±10.3μM (5c) and IC(50)=35.9±5.7μM (5b)) and normal human fibroblasts (IC(50)=38.0±2.8μM (5c) and IC(50)=45.5±1.9μM (5b)). Conjugate 5a displayed no activity in both tests. |
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