Studies On The Bioactive Substances From Some Marine Invertebrates In Shandong Seashore

In order to find natural bioactive lead compounds from marine invertebrates, the extracts of 21 common marine invertebrates in Shandong seashore were screened for their antitumor, antibacteria, immune regulation and ?-glucosidase inhibition activities for the first time. 17 pure compounds were isolated from three species of marine invertebrates: Tubuaria marina Torrey, Asterias rollestoni and Asterina pectinifera. The structures of the 17 compounds were identified by spectroscopic methods including 1D NMR, 2D NMR, IR and MS, and 2 of them were found to be new compounds, whose structures were identified for the first time in the world. Moreover, the bioactivities of the pure compounds were determined using various pharmacology models.1 Pharmacological activity determination of the extractsAntitumor activity was determined by MTT method. It was found that the n-butanol part of Asterina pectinifera, the acetic ether part of Tubuaria marina,95% ethanol extract of Acanthochiton rubrolineatus have high inhibition rate of 96.7%,63.9% and 50.5% respectively on tumor cell line HL-60 at concentration of 0.063 mg/ml. The inhibition rate of the acetic ether part of Tubuaria marina on the tumor cell line A-549 is 65.4 % at concentration of 0.063 mg/ml.Micro dilution method was used to determine the antibacterial and antifungal activity on Staphylococeus aureus, Escherichia coli and Candida albicans, but the minimal inhibition concentration (MIC) of all the samples are all below 20μg/ml, indicating that they have no obvious antibacterial and antifungal activity.Immune regulation activity was studied using T and B lymphocytes in mice spleen in vitro. It was found that the ethanol extracts of the marine invertebrates have immune regulation activity on the proliferation of T and B lymphocytes. Among them,10 showed well concentration-dependent immunomodulatory effects, and 6 have exhibited fine dual-immunomodulatory effects at the doses of 1-100μg/ml. Most of the samples were found to have ?-glucosidase inhibition activity. Among them, the extracts of Scapharca subcrenata and Apostichopus japonicus have higher inhibition rates, which were 66.3% and 62.2% respectively at concentration of 79.6?g/ml.2 Isolation and identification of the 2 new compoundsTwo new compounds were isolated from Asterina pectinifera using silica gel and Sephadex LH-20 chromatography, and identified as 3-{O-β-D-fucopyranosyl-(1→3)-β-D-fucopyranosyl-(1→4)-[β-D- quinovopyranosy-(1→2)]-β-D-quinovopyranosyl}-2-(1'-imino-1'-ethyl) -furan and 15β, 16β-isopropylidenedioxy-5α-cholestane-3β, 4β, 6α, 7α, 8, 26-hexaol. Furthermore, their bioactivities were determined using various pharmacology models.3 Isolation and identification of the known compoundsFive pure compounds were isolated from Tubuaria marina, which were henicosene, cholest-5-en-3β-ol, 1-nonyl- glycerylether, inosine and 2'-deoxyinosine, and four pure compounds were isolated from Asterias rollestoni, which were phenylalanine, 2'-deoxythymidine, 2'-deoxyinosine-5'-monophosphate and 5-methoxyl-1-tridecanol. The six known compounds from Asterina pectinifera were identified as leucine, 2'-deoxythymidine, tryptophane, 5'-O-sulfate-24-(α-3'-O-methyl- L-arabinofuranosyl)-3β, 6α, 8β, 15α, 24ζ-pentaoxy-5α-cholestane, 24-(α-3'-O-methyl-L-arabinofuranosyl)-3β, 6α, 8β, 15α, 24ζ-pentaoxy-5α-cholestane and 5α-cholestane-3β, 4β, 6α, 7α, 8, 15β, 16β, 26- octol.