Characterization and Cytotoxicity Studies of the Rare 21:4 n-7 Acid and Other Polyunsaturated Fatty Acids from the Marine Opisthobranch Scaphander lignarius, Isolated Using Bioassay Guided Fractionation
The marine opisthobranch Scaphander lignarius has been analyzed in the systematic search for novel bioactive compounds in Arctic marine organisms using bioassay guided fractionation. A number of highly cytotoxic fractions were shown to contain mainly polyunsaturated fatty acids (PUFAs). Selected PUFAs were isolated and identified using both liquid chromatography-mass spectrometry (LC-MS) and nuclear magnetic resonance (NMR). It was shown that the opisthobranch contained unusual PUFAs such as several ω3 fatty acids and the ω7 heneicosa-5,8,11,14-tetraenoic acid (21:4 n-7) not isolated before. The organism was shown to be a very rich source of PUFAs and the activity of the isolated compounds against a range of human cancer cell lines (melanoma, colon carcinoma and breast carcinoma) is further reported. The ω7 PUFA was significantly more cytotoxic in comparison with reference ω6 arachidonic and ω3 eicosapentaenoic acid. A noteworthy non-selective cytotoxicity against normal lung fibroblasts was also established. The paper contains isolation protocols in addition to cytotoxicity data of the isolated compounds. The potential of marine mollusks as a source for rare PUFAs is also discussed.
CitationMarine Drugs 10(2012) nr. 12 s. 2676-2690
The following license file are associated with this item:
Showing items related by title, author, creator and subject.
A Biofocussed Chemoprospecting Approach to Drug Discovery: Design, Synthesis and Bioactivity Screening of Diverse Biofocussed Chemical Libraries Thakkar, Balmukund (Doctoral thesis; Doktorgradsavhandling, 2017-04-28)With pharma R & D witnessing rising cost, high attrition rates and an overall decline in productivity in recent times, newer approaches are needed for more efficient early phase drug discovery. This thesis describes a new approach, “biofocussed chemoprospecting”. The essence of the approach is to use diverse, yet “bio-like” compounds for efficient hit-finding, along with property filtering and ...
Novel [18F]fluorinated prosthetic groups for the labelling of peptides for positron emission tyomography (PET) Olberg, Dag Erlend (Doctoral thesis; Doktorgradsavhandling, 2009-11-20)Positron emission tomography is a non-invasive imaging modality allowing visualization and quantification of a wide variety of physiological and biochemical processes or of a specific lowdensity protein target. Some examples are blood flow, glucose consumption, fatty acid metabolism or detection and quantification of cell surface receptors in particular tissues. Within the spectrum of available ...
Toward Tripeptidomimetic CXCR4 Antagonists: Design, Synthesis, Biological Evaluation, and Binding Mode Studies Zachariassen, Zack George (Doctoral thesis; Doktorgradsavhandling, 2014-04-11)In order for the HIV virus to take over and destroy human immune cells, which results in AIDS, the virus first has to enter the cells. This takes place by interactions between viral proteins and specific receptors on the surface of our cells. One of these receptors is CXCR4, and it has been shown that chemical compounds that bind to and block the CXCR4 receptor, so-called CXCR4 antagonists, are able ...