Studies On The Structures And Biological Activities Of Chemical Constituents From The Marine Sponge Hyrtios Erectus Acanthella Cavernosa And Dysidea Sp. In South China Sea

In our ongoing program to search for natural products with unique structural features and pronounced biological activities, the marine sponge Hyrtios erectus, Acanthella cavemosa and Dysidea sp.were collected from Sanya city, Hainan island, South china sea. Repeatedly column chromatography was performed for the isolation and purification of their MeOH extracts. 54 pure compounds were obtained from these three marine organisms. Their structures were determined by extensive spectroscopic analysis in association with physical and chemical properties, as well as comparison of their spectral data with these reported in literatures. Most of these compounds were screened for their antitumor(HL-60 human leukemic cell, A-549 human lung cancer cell, PC-3MIE8 human prostate cancer cell, BGC-823 human gastric cancer cell, MDA-MB-435 human breast cancer cell, Bel-7402 human hepatoma cancer cell, Hela human cerrical cancer cell), COX-2 inhibition, ACE inhibition, PTPIB inhibition activities and anti-HIV activities.31 Compounds, namely 20-formylhyrtiosal(1), 16-O-acetyl-20-formylhyrtiosal(2), 12-α-O-acetylhyrtiolide(3), 5,10-dihydroxyfurospinulosine-1 (4), 19-methoxy-scalarin (5), 21-hydroxy-16-deacetyl-12-epi-scalara furan acetate (6), 12,19-α-16-β-O-triacetyl hyrtiolide(7), 16-deacetyl-12-epi-scalara furan acetate (8), 21-hydroxydeoxoscalarin(9), 12-O-deacetyl-19-deoxyscalarin (10), scalarin (11), isoscalara furan-A(12), 16-acetyl-isoscalara furan-A(13), 12-O-deacetyl furoscalarol(14), furoscalarol(15), 12-epi-deoxoscalarin (16), 12-acetyl-16,20-α-dihydroxy-scalarolide (17), hyrtioacid(18), 5-hydroxy-tryptophan(19), 5-hydroxy-indol-3-aldehyde (20), 5-hydroxy-indol -3-(2-hydroxy)-ethyl (21), 5-ethoxy-indol-3-aldehyde (22), deoxyuridine(23), deoxy thymidine (24), deoxyadenosine(25), uracil (26), Batylalcohol (27), Ceotylalcohol (28), 16-ene-Batylalcohol (29) , ( - )-(1S,3S)-1-Methyl-1,2,3,4-tetrahydro-6-hydroxy-β-carbo-line-3-carboxylic acid (30), scalarin A (31) were isolated and identified from the marine sponge Hyrtios erectus. Among them, compounds1-6, 18, 31 were novel compounds. Sesterterpenoid 10 showed cytotoxic activities against P388 human leukemic cell with ED₅₀ 2.9 ug/ml. Compound 1 showed moderate cytotoxic activities against HL-60 human leukemic ce!i, A-549 human lung cancer cell. Sesterterpenoids 1 and 12 showed moderate inhibition ACE. Compounds 1 and 11 showed weak anti-bacteria activity.