Yangambin, a lignan obtained from Ocotea duckei, differentiates putative PAF receptor subtypes in the gastrointestinal tract of rats.
We investigated the presence of PAF receptor subtypes in the tissues of the gastrointestinal tract, airways, blood vessels and in murine macrophages. For this purpose we have used a competitive PAF receptor antagonist, yangambin (YAN), extracted from the Brazilian plant "louro de cheiro" (Ocotea duckei Vattimo). Rat duodenum, jejunum, ileum, colon, stomach fundus, trachea and bronchia were removed and 1.5-2 cm muscle segments from those regions were mounted in a 10 ml organ bath with aerated physiological solution at 37 degrees C. PAF evoked a contraction of the rat jejunum, ileum, colon and stomach fundus. The contraction was slow and resistant to wash and was followed by desensitization to further doses of PAF. Contractions induced by PAF (10(-6) M) were inhibited by YAN (10(-7) to M-2 x 10(-5) M) and WEB 2086 (10(-6) m to M-5 M) in rat jejunum, ileum and colon but not in the stomach fundus. In the rat stomach fundus only WEB 2086 (5 x 10(-6) M) was able to block PAF-induced contraction. The contractions induced by acetylcholine, histamine, 5-hydroxytryptamine and vasopressin were not inhibited by prior administration of YAN. Yangambin also significantly inhibited PAF-induced vascular permeability in rat duodenum, jejunum, ileum, colon, and mesentery. Yangambin significantly inhibited PAF-induced lipid body formation in mice peritoneal macrophages. We suggest that YAN is a selective PAF antagonist which is able to discriminate putative PAF receptors subtypes present in the stomach fundus.
Jesus-Morais
C M
CM
INCQS, Instituto Nacional de Controle de Qualidade em Saúde, Fundação Oswaldo Cruz, Rio de Janeiro, Brazil.
Assis
E F
EF
Cordeiro
R S
RS
Barbosa-Filho
J M
JM
Lima
W T
WT
Silva
Z L
ZL
Bozza
P T
PT
Castro-Faria-Neto
H C
HC
D000818:Animals; D001381:Azepines / Q000494:pharmacology; D004064:Digestive System / Q000187:drug effects* / Q000378:metabolism; D005260:Female; D005663:Furans / Q000378:metabolism / Q000494:pharmacology*; D066298:In Vitro Techniques; D019770:Lauraceae / Q000737:chemistry*; D017705:Lignans / Q000378:metabolism / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008809:Mice, Inbred C3H; D010975:Platelet Aggregation Inhibitors / Q000378:metabolism / Q000494:pharmacology*; D010980:Platelet Membrane Glycoproteins / Q000145:classification / Q000187:drug effects*; D051381:Rats; D017208:Rats, Wistar; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; D014230:Triazoles / Q000494:pharmacology
D001381:Azepines; D005663:Furans; D017705:Lignans; D010975:Platelet Aggregation Inhibitors; D010980:Platelet Membrane Glycoproteins; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; D014230:Triazoles; C039351:platelet activating factor receptor; C052518:WEB 2086; C082827:epiyangambin