期刊
MOLECULES
卷 24, 期 6, 页码 -出版社
MDPI
DOI: 10.3390/molecules24061078
关键词
rosmarinic acid; quaternary phosphonium salts; anticancer; antibacterial; MRSA; antifungal; anti-Acanthamoeba activity
资金
- Grant Agency of Ministry of Education, Science, Research, and Sport of the Slovak Republic [VEGA-1/0290/16, VEGA-1/0298/16, VEGA 1/0365/16, VEGA 1/0389/19, VEGA-1/0653/19, KEGA 039UK-4/2019]
- Slovak Research and Development Agency [APVV-15-0123, APVV-16-0446]
- CEBV project [ITMS: 26240120034]
- Operational Programme Research & Innovation - ERDF [ITMS2014 + 313011D103]
On its own, rosmarinic acid possesses multiple biological activities such as anti-inflammatory, antimicrobial, cardioprotective and antitumor properties, and these are the consequence of its ROS scavenging and inhibitory effect on inflammation. In this study, two quaternary phosphonium salts of rosmarinic acid were prepared for the purpose of increasing its penetration into biological systems with the aim of improving its antimicrobial, antifungal, antiprotozoal and antitumor activity. The synthetized molecules, the triphenylphosphonium and tricyclohexylphosphonium salts of rosmarinic acid, exhibited significantly stronger inhibitory effects on the growth of HCT116 cells with IC50 values of 7.28 or 8.13 M in comparison to the initial substance, rosmarinic acid (>300 M). For the synthesized derivatives, we detected a greater than three-fold increase of activity against Acanthamoeba quina, and a greater than eight-fold increase of activity against A. lugdunensis in comparison to rosmarinic acid. Furthermore, we recorded significantly higher antimicrobial activity of the synthetized derivatives when compared to rosmarinic acid itself. Both synthetized quaternary phosphonium salts of rosmarinic acid appear to be promising antitumor and antimicrobial agents, as well as impressive molecules for further research.
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