Chemical Constituents And Its Bioactivities From Four Marine Organisms

In order to investigate the chemical diversity and the bioactivity from marine organisms, four species green alga Cladophora fascicularis (Mert.) Kütz, soft coral Cladiella krempfi, sponge Pseudoceratina sp. and Canavalia maritime (Aubl.) Thou were collected and examinated chemically. On the basis of extensive chromatography and spectroscopic analysis, totally, 74 compounds were isolated and elucidated, of which 10 are new compounds, 1 is a new natural product.From the green alga C. fascicularis, 21 compounds (see Fig.1) were isolated and characterized, including a new compound Porphyrinolactone 1^*(see talbe 1, marked *). 20-chlorinated- (132-S)-hydroxyphaeophytin a 2^** (see talbe 1, marked **) were isolateed from nature for the first time. The other known compounds were identified as pha- eophytins 3—6, Cycloart-triterpenoids 7—12, steroids 13—20, and 4-hydrox- ybenzaldehyde 21. Cycloart-triterpenoids were isolated from the genus for the first time. Phaeophytins 1*, 2**and 3—6 were assayed for in vitro inhibitory effect against NF-κB translocation activated by tumor necrosis factor alpha (TNF-α) without illum- ination. All compounds exhibited singificant inhibitory effect on the activation of NF-κB. We first examined their effect on proteasome ChT-L activity by using an enzyme- atic activity assay in vitro. Compounds 2** and 4 showed a significant inhibitory effe- ct on proteasome ChT-L activity inhibitory rates (C=50μM, 70% and 73.5%). Phar- macological screen indicated that compounds 1^*, 5, 7, 8, 11, and 14 showed no signi- fycant inhibitory on HL-60, MDA-ME-319, Bel-7402, PC-3M-18, BGC-823, and Hep-2, Hela; and compounds 5, 6, 8, 11, 13, and 14 showed no signifycant inhibitory on PTP1B. While under C=1μg/mL, compound 12 showed significant inhibitory on kinase EPHB₄, compounds 7—9 and 11—15 showed significant inhibitory on kinase on ERBB2, CDK2/CyA, CDK4/CycD1, FLT3, INSR, MET, PDGFRbeta, and COT, compound 7—15 showed significant inhibitory on kinase on ARK5, AuroraA, auroraB, B-RAFVE, CK2- alpha1, and PLK1, compound 8, 9, and 11—15 showed significant inhibitory on kinase on FAKand TIE2, compound 8, and 11—15 showed significant inhibitory on kinase on VE- GFR2 and VEGFR3, compound 15 showed significa- nt inhibitory on kinase on IGF1-R, compound 9—11 and 13—15 showed significant inhibitory on kinase on AKT1.