ABSTRACT
Ten halogenated monoterpenes (2-6 and 8-12) related to the novel antitumor compound halomon (1) or to the carbocyclic analog 7 have been isolated from different geographic collections of the red alga, Portieria hornemannii. Structures were assigned to the basis of spectral analyses (primarily NMR and MS). The absolute configuration of isohalomon (2) was further established by X-ray crystallography. The compounds were comparatively evaluated alongside 1 and 7 in the U.S. National Cancer Institute's in vitro human tumor cell line screening panel. The results provide some interesting initial insights into the structure/activity relationships in this series.
Subject(s)
Antineoplastic Agents/isolation & purification , Hydrocarbons, Halogenated/chemistry , Rhodophyta , Terpenes/isolation & purification , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Cell Survival/drug effects , Computer Simulation , Crystallography, X-Ray , Humans , Hydrocarbons, Halogenated/pharmacology , Magnetic Resonance Spectroscopy , Mass Spectrometry , Models, Molecular , Molecular Conformation , Molecular Structure , Terpenes/chemistry , Terpenes/pharmacology , Tumor Cells, CulturedABSTRACT
Lokysterolamine A and B are two steroidal alkaloids isolated from an undescribed species of the sponge genus Corticium, collected in Sulawesi, Indonesia. Compound A is N,N-dimethyl- and B is N-acetyl-4 beta-hydroxy-3-epi-plakinamine A.
Subject(s)
Alkaloids/isolation & purification , Anti-Infective Agents/isolation & purification , Antineoplastic Agents/isolation & purification , Porifera/chemistry , Steroids/isolation & purification , Alkaloids/pharmacology , Animals , Anti-Infective Agents/pharmacology , Antineoplastic Agents/pharmacology , Drug Screening Assays, Antitumor , Humans , Indonesia , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Molecular Structure , Spectrophotometry, Ultraviolet , Steroids/pharmacology , Tumor Cells, CulturedABSTRACT
The objective of this study was to investigate the effects of intraperitoneal administration of thioglycollate or LPS and subcutaneous injection of turpentine on chemotaxis, phagocytosis and respiratory burst of rat alveolar (AM) and peritoneal (PM) macrophages. All the stimulants caused an increase in chemotaxis of PM and its decrease in AM. Phagocytosis of AM and PM was increased after thioglycollate injection, LPS caused an increase in phagocytotic activity of AM and its decrease in PM; turpentine had no effect. Turpentine and thioglycollate caused a decrease and LPS an increase in respiratory burst activity of AM; all types of treatment caused an increase in this activity in PM.
Subject(s)
Macrophages/physiology , Animals , Chemotaxis, Leukocyte/drug effects , In Vitro Techniques , Indicators and Reagents , Lipopolysaccharides/pharmacology , Luminescent Measurements , Macrophages/drug effects , Macrophages, Alveolar/drug effects , Macrophages, Alveolar/physiology , Macrophages, Peritoneal/drug effects , Macrophages, Peritoneal/physiology , Male , Phagocytosis/drug effects , Rats , Rats, Wistar , Respiratory Burst/drug effects , Stimulation, Chemical , Thioglycolates/pharmacology , Turpentine/pharmacologyABSTRACT
Sixteen sesquiterpenoids and norsesquiterpenoids, six of them new, were isolated from the octocoral Lemnalia africana. Antileukemia activity (P-388) was found only in the known eremophilane derivative 15.
