Plant compounds play an important role in human medicine. They are a source of new drugs or serve as an inspiration for drugs' development. This thesis presents a study about syntheses of derivatives and biological activities of two groups of natural products, quinones and terpenoids. Terpenoids are plant secondary metabolites which are known for their antimicrobial, anti-inflammatory and anti-tumoral activities. We have focused on two representatives, paclitaxel and carvacrol. GnRH-paclitaxel anti-tumor conjugates potentially suitable for targeted delivery to cancer cells were prepared. Their antiproliferative activities in vitro were evaluated on MCF-7 cancer cell line and cytotoxicity in rat hepatocytes. Carvacrol and its derivative were tested for its possible anti- inflammatory effect, which was assessed in vitro as their potential to inhibit prostaglandin E2 biosynthesis via cyclooxygenase pathway. Quinones, other targets of the thesis, are well-known for biological activities similar to terpenoids. Thymoquinone, juglone and their derivatives were tested in vitro as inhibitors of cyclooxygenases and 5-lipoxygenase. Derivatives of juglone were prepared to help us to suggest structure-activity relationship of this compound. Thymoquinone and its derivatives were evaluated for their antioxidant capacity...
| Identifer | oai:union.ndltd.org:nusl.cz/oai:invenio.nusl.cz:322586 |
| Date | January 2013 |
| Creators | Přibylová, Marie |
| Contributors | Vaněk, Tomáš, Smrček, Stanislav, Hájek, Miroslav |
| Source Sets | Czech ETDs |
| Language | English |
| Detected Language | English |
| Type | info:eu-repo/semantics/doctoralThesis |
| Rights | info:eu-repo/semantics/restrictedAccess |
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