RESUMEN
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.
Asunto(s)
Antineoplásicos/aislamiento & purificación , Hidrocarburos Halogenados/química , Rhodophyta , Terpenos/aislamiento & purificación , Antineoplásicos/química , Antineoplásicos/farmacología , Supervivencia Celular/efectos de los fármacos , Simulación por Computador , Cristalografía por Rayos X , Humanos , Hidrocarburos Halogenados/farmacología , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Modelos Moleculares , Conformación Molecular , Estructura Molecular , Terpenos/química , Terpenos/farmacología , Células Tumorales CultivadasRESUMEN
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.
Asunto(s)
Macrófagos/fisiología , Animales , Quimiotaxis de Leucocito/efectos de los fármacos , Técnicas In Vitro , Indicadores y Reactivos , Lipopolisacáridos/farmacología , Mediciones Luminiscentes , Macrófagos/efectos de los fármacos , Macrófagos Alveolares/efectos de los fármacos , Macrófagos Alveolares/fisiología , Macrófagos Peritoneales/efectos de los fármacos , Macrófagos Peritoneales/fisiología , Masculino , Fagocitosis/efectos de los fármacos , Ratas , Ratas Wistar , Estallido Respiratorio/efectos de los fármacos , Estimulación Química , Tioglicolatos/farmacología , Trementina/farmacologíaRESUMEN
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.
Asunto(s)
Alcaloides/aislamiento & purificación , Antiinfecciosos/aislamiento & purificación , Antineoplásicos/aislamiento & purificación , Poríferos/química , Esteroides/aislamiento & purificación , Alcaloides/farmacología , Animales , Antiinfecciosos/farmacología , Antineoplásicos/farmacología , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Indonesia , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Espectrofotometría Ultravioleta , Esteroides/farmacología , Células Tumorales CultivadasRESUMEN
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.