| 摘要: | In Paper I, the literature investigation focusing on the chemical constituents and biological activities of the secondary derived from cultivated soft corals came to a conclusion that cultured soft corals could be a resevoir of numerous bioactive secondary metabolites. In addition to the increasing diversity of novel compounds, the cultivation of soft corals could contribute sustainable and consistent resources of promising therapeutic agents to further insight studies and clinical applications. This insprired further investigations on aquacultured soft corals with the expectation that novel therapeutics could be developed from the isolated lead compounds.
Biscembranoids refer to a distinctive set of tetraterpenoids that have exceptional structures consisting of tricyclic frameworks with 14/6/14 members. In particular, the soft corals of the genus Sarcophyton have been considered to be prolific sources of these distinctive metabolites via an immense number of related studies. The recent results of bioactivity tests have shown that biscembranoid analogues have significant potential to act as anti-inflammatory agents in human neutrophils. Being encouraged by those promising findings, the number of studies focusing on these distinctive metabolites have been increasing to discover more novel structures and evaluate their pharmacological effects in order to sastify the demand for new anti-inflammatory drugs.
The target of this thesis is to hunt the biscembranoids originated from the cultured soft coral Sarcophyton trocheliophorum and investigates their anti-inflammatory effects on fMLF/CB-induced human neutrophils.
In Paper II and the manuscript, based on molecular networking strategies, a total of 10 biscembranes were successfully isolated, including sarcotrochelide A (1), sarcotrochelide B (2), ximaolide A (3), methyl tortuoate D (4), glaucumolide A (5), glaucumolide B (6), bistrochelide A (7), bistrochelide B (8), sarcotrochelide C (9), and sarcotrochelide D (10). Among the isolated compounds, there were 4 new derivatives that include sarcotrochelides A – D (1, 2, 9, and 10). The biscembranes were identified on the basis of spectral analysis and were assessed for their anti-inflammatory activities in in vitro experiments. According to the results of in vitro tests, compounds 1 – 4 showed weak effects in both assays. Furthermore, compounds 7 – 10 displayed moderate anti-inflammatory effects, whereas compound 6 exhibited the greatest inhibition against superoxide anion generation and elastase release in activated neutrophils, which was followed by compound 5. |
