Some pharmacological activities of novel adenine-related compounds isolated from a marine sponge Agelas mauritiana.
Agelasimine A and agelasimine B, two novel compounds related to adenine, have been isolated from the orange sponge, Agelas mauritiana, and have been tested for a variety of biological activities. Both compounds inhibited proliferation of cultured L1210 leukemia cells at nanomolar concentrations with accumulation in the G1 stage of the cell cycle. However, no prolongation of life was observed in mice bearing P388 leukemia treated with these compounds. In the rat isolated aorta, micromolar concentrations of agelasimines were very effective in inhibiting contractions elicited by potassium chloride but had little or no effect on responses for prostaglandin F2 alpha and had modest effects on the responses to noradrenaline and significant effects on 5-hydroxytryptamine. Agelsamines A and B appeared to be equipotent in causing relaxation in rabbit jejunum and bovine coronary artery, and they also inhibited nucleoside transport into rabbit erythrocytes in micromolar concentrations.
Department of Pharmacology, University of Alberta, Edmonton, Canada.
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R
Fathi-Afshar
T M
TM
Allen
C A
CA
Krueger
D A
DA
Cook
A S
AS
Clanachan
R
R
Vriend
H P
HP
Baer
C E
CE
Cass
D000225:Adenine / Q000031:analogs & derivatives* / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use; D000241:Adenosine / Q000097:blood; D000818:Animals; D001011:Aorta / Q000187:drug effects / Q000502:physiology; D002453:Cell Cycle / Q000187:drug effects*; D004912:Erythrocytes / Q000187:drug effects / Q000378:metabolism*; D066298:In Vitro Techniques; D007700:Kinetics; D007939:Leukemia L1210 / Q000473:pathology; D007941:Leukemia P388 / Q000188:drug therapy*; D007942:Leukemia, Experimental / Q000188:drug therapy*; D051379:Mice; D009126:Muscle Relaxation / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000502:physiology*; D009284:Naphthols / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D011161:Porifera; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D011983:Receptors, Purinergic / Q000187:drug effects / Q000378:metabolism
D009284:Naphthols; D011983:Receptors, Purinergic; C060682:agelasimine A; C060683:agelasimine B; D000225:Adenine; D000241:Adenosine