Enhancing effect of cystamine in its amides with betulinic acid as antimicrobial and antitumor agent in vitro

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22330%2F19%3A43917966" target="_blank" >RIV/60461373:22330/19:43917966 - isvavai.cz</a>
Alternative codes found
RIV/61389030:_____/19:00507538 RIV/61388963:_____/19:00507538 RIV/61989592:15110/19:73597217 RIV/61989592:15310/19:73597217
Result on the web
<a href="https://www.sciencedirect.com/science/article/pii/S0039128X19300698" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0039128X19300698</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.steroids.2019.04.004" target="_blank" >10.1016/j.steroids.2019.04.004</a>

Result language
angličtina
Original language name
Enhancing effect of cystamine in its amides with betulinic acid as antimicrobial and antitumor agent in vitro
Original language description
Amides of betulinic acid with cystamine were synthesized to investigate their antimicrobial and antitumor activity, and their influence on the cell cycle and cell apoptosis. The former target amide (6) displayed cytotoxicity in CEM cell line after 72 h of treatment (IC50 = 3.0 +/- 0.7 mu M; TI = 20), and induced apoptosis by caspase-3/7 activation in CEM cells. The latter target amide (9) displayed antimicrobial activity against Streptococcus mutans (MIC 3.125 mu M; MBC 3.125 mu M) and Bacillus cereus (MIC 25 mu M; MBC 25 mu M). The achieved results demonstrate enhancing of their biological activity over that of the parent compounds. However, two intermediate compounds (2 and 7) displayed either considerable cytotoxicity (2; 7.5 +/- 0.8 mu M; TI = 10, against G361) or antimicrobial activity (7; both against Actinomyces odontolycus and Clostridium perfrigens with MIC 12.5 mu M and MBC 12.5 mu M). The experimental data were compared with the in silica calculated physico-chemical and ADME parameters of the target compounds, including successful intermediates.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10401 - Organic chemistry

Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2019
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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