Subject(s)
Colonialism , Ethnicity , Social Change , Sports , Anthropology, Cultural/education , Anthropology, Cultural/history , Colonialism/history , Ethnicity/education , Ethnicity/ethnology , Ethnicity/history , Ethnicity/legislation & jurisprudence , Ethnicity/psychology , History, 19th Century , History, 20th Century , Humans , Prejudice , Singapore/ethnology , Social Change/history , Sports/economics , Sports/education , Sports/history , Sports/legislation & jurisprudence , Sports/physiology , Sports/psychology , United Kingdom/ethnologyABSTRACT
Extracts and pure compounds isolated from four samples of Dysidea sp. sponges collected from two geographically distinct regions of the Indo-Pacific (Chuuk Atoll and Fiji) were assayed against five different enzyme assays, four of which are relevant to anticancer drug discovery and one of which (15-lipoxygenase) may detect compounds significant in modulating the development of atherosclerotic plaque. The pure compounds that inhibited various enzymes were polybrominated phenols and polybrominated phenoxyphenols. Fourteen of these phenols were isolated, six of which were new compounds. A variety of the phenols inhibited inosine monophosphate dehydrogenase (IMPDH), guanosine monophosphate synthetase, and 15-lipoxygenase. No activity was observed with protein tyrosine kinase pp60v-src or matrix metalloprotease.
Subject(s)
Carbon-Nitrogen Ligases , Enzyme Inhibitors/isolation & purification , Phenols/isolation & purification , Phenyl Ethers/isolation & purification , Porifera/chemistry , Animals , Biological Products/chemistry , Biological Products/isolation & purification , Biological Products/pharmacology , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , IMP Dehydrogenase/antagonists & inhibitors , Ligases/antagonists & inhibitors , Lipoxygenase Inhibitors , Molecular Structure , Phenols/chemistry , Phenols/pharmacology , Phenyl Ethers/chemistry , Phenyl Ethers/pharmacology , Protein-Tyrosine Kinases/antagonists & inhibitorsABSTRACT
Two sesquiterpene quinols, cyclorenierins A [1] and B [2], which are closely related to panicein A2 [3] and renierin A [4], were isolated as an inseparable mixture from the marine sponge Haliclona sp. collected in Vanuatu. Structures were proposed using nmr shift analogies to 3 and 4 and confirmed with 2D nmr data.
Subject(s)
Porifera/chemistry , Sesquiterpenes/isolation & purification , Animals , Magnetic Resonance Spectroscopy , Sesquiterpenes/chemistryABSTRACT
Two new cyclic sesquiterpenes, arenarans A [1] and B [2], were isolated from a Thai collection of Dysidea arenaria. Their chemical and cytotoxic properties are described.
Subject(s)
Antineoplastic Agents/isolation & purification , Porifera/chemistry , Sesquiterpenes/isolation & purification , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Drug Screening Assays, Antitumor , Humans , Magnetic Resonance Spectroscopy , Molecular Structure , Sesquiterpenes/chemistry , Sesquiterpenes/pharmacology , Stereoisomerism , Tumor Cells, CulturedABSTRACT
Three new peroxylactones, plakortolides B [6], C [7], and D [8], and a new peroxy ester, epiplakinic acid E methyl ester [9], were isolated and characterized from a previously unstudied marine sponge, Plakinastrella onkodes. A mixture of steroidal peroxides was also found in this organism. Plakortolides B [6] and D [8], and epiplakinic acid E methyl ester [9], were evaluated for biological activity and found to show cytotoxicity against the A549 human lung carcinoma and P388 murine leukemia cell lines, and to effect adhesion in an assay employing the EL-4.IL-2 cell line, which correlates with signal transduction activity.
Subject(s)
Antineoplastic Agents/pharmacology , Lactones/pharmacology , Porifera/chemistry , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/isolation & purification , Cell Adhesion/drug effects , Cell Line , Cell Survival/drug effects , Humans , Lactones/chemistry , Lactones/isolation & purification , Leukemia P388/drug therapy , Magnetic Resonance Spectroscopy , Mice , Tumor Cells, CulturedABSTRACT
Staurosporine aglycone (K252-c) (compound 1) and arcyriaflavin A (2) were isolated from a specimen of the marine ascidian, Eudistoma sp., collected off the coast of West Africa. In addition to expressing micromolar and submicromolar inhibition of enzyme activity against seven protein kinase C isoenzymes and inhibition of proliferation of the human lung cancer A549 and P388 murine leukemia cell lines, 1 also inhibited cell adhesion of the EL-4.IL-2 cell line and expressed activity in the K562 bleb and neutrophil assays.