Protein kinases play a critical role in cell regulation and their deregulation is a contributing factor in an increasing list of diseases including cancer. Marine sponges have yielded over 70 novel compounds to date that exhibit significant inhibitory activity towards a range of protein kinases. These compounds, which belong to diverse structural classes, are reviewed herein, and ordered based upon the kinase that they inhibit. Relevant synthetic studies on the marine natural product kinase inhibitors have also been included.
The MTT/MTS in vitro cell proliferation assay is one of the most widely used assays for evaluating preliminary anticancer activity of both synthetic derivatives and natural products and natural product extracts. The highly reliable, colorimetric based assay is readily performed on a wide range of cell lines. This assay gives an indication of whole cell cytotoxicity; however, to determine the exact molecular target further assays need to be performed. Of these, kinase inhibition assays are also one of the most widespread enzyme inhibition screening assays performed. Kinases are enzymes that play a key role in a number of physiological processes and their inhibitors have been found to exhibit anticancer activity against various human cancer cell lines. Herein, we describe the methods for performing both in vitro MTT/MTS cytotoxicity and kinase enzyme inhibition assays. These are two of the most useful anticancer screening techniques available that are relatively economical and can be easily and routinely performed in the laboratory to characterize anticancer activity. Both assays are highly versatile and can be modified to test against targeted disease processes by using specific kinase enzymes or cell lines.
The cAMP dependent protein kinase (PKA) inhibition, haemolytic activity, and cytoxicity of 21 extracts obtained from North Western Australian sponges collected from depths of 84-135 m were investigated. Hexane extracts from Ircinia/Sarcotragus sp. and Geodia sp. displayed PKA inhibitory activities of 100 and 97% respectively (at 100 μg/mL), while aq. methanol extracts from Haliclona sp. exhibited potent haemolytic activity (75%) and hexane extracts from Geodia sp. were highly toxic (88%) to the brine shrimp Artemia franciscana. As the non-polar extracts gave the greatest PKA inhibition, these were further analysed by GC-MS and 29 fatty acids were identified in the highest proportions in Ircinia/Sarcotragus sp. > Haliclona sp. > Geodia sp. In contrast to shallow-water sponges that are dominated by polyunsaturated fatty acids with a high percentage of long chain fatty acids, LCFAs (C 24-C 30), the deep-sea sponges investigated herein were all found to be rich in saturated fatty acids, in particular C 14-C 20 fatty acids, including odd and branched chain fatty acids, with only low levels (0-10%) of LCFAs. Screening of the PKA inhibitory activity of a series of commercially available fatty acids identified C 14-C 18 fatty acids as possessing significant PKA inhibitory activity that may contribute to the activity observed in the sponges studied.
A survey on macro-and micro-elements, phenolic compounds, biological activity and use of Morus spp. (Moraceae) Abstract-Introduction. Mulberry is the most medicinally important plant of the genus Morus. The mulberry fruit is used for many medical purposes. The species origin and adaptation, plant description, foliage, flowers and fruit, location, soil, and pests and diseases are summarized. Composition of mulberry. The studies from different countries show that the mulberry plant is rich in phenolic compounds, macro-elements (K, Ca, Mg, Na) and microelements (Fe, Zn, Ni). Phenolic compounds are found in all parts of the mulberry plant. Uses. Mulberry fruit can be used for making jam, jelly, pulp, fruit drinks, fruit sauce and cake. Mulberry fruits are rich in anthocyanins and should be exploited for the industrial production of natural color to be used in the food industry. Conclusion. The mulberry plant is of significant biological importance for its antioxidant and antimicrobial properties. Our study suggested the use of mulberry as a potential health food, or important antioxidant carrier in the food and pharmaceutical industries. Serbia / Morus / fruits / proximate composition / polyphenols / antioxidants / microbiological analysis Enquête sur les macro-et micro-éléments, la teneur en composés phénoliques, l'activité biologique et l'utilisation de Morus spp. (Moraceae). Résumé-Introduction. Le mûrier est la plante médicinale la plus importante du genre Morus. Le fruit mûr est utilisé à de nombreuses fins médicales. L'origine et l'adaptation des espèces, la description de la plante, de son feuillage, de ses fleurs et fruits, sa localisation, ses ravageurs et maladies ont été synthétisés. Composition du mûrier. Les études effectuées dans différents pays montrent que le mûrier est riche en composés phénoliques, en macroéléments (K, Ca, Mg, Na) et en micro-éléments (Fe, Zn, Ni). Les composés phénoliques sont présents dans toutes les parties de la plante adulte. Utilisation. Les fruits du mûrier peuvent être utilisés pour élaborer des confitures, gelées, pâtes de fruits, boissons aux fruits, sauces aux fruits et gâteaux. Les mûres sont riches en anthocyanes et aptes à être exploitées pour la production industrielle de colorants naturels à utiliser dans l'industrie alimentaire. Conclusion. Le mûrier est d'une importance biologique significative pour ses propriétés antioxydantes et antimicrobiennes. Notre étude suggère une utilisation de la mûre comme un aliment potentiel de santé ou une source importante d'antioxydants dans les industries alimentaires et pharmaceutiques.
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