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, yangam bin (YAN), extracted from the Brazilian plant "louro de cheiro" (Ocotea duc kei Vattimo). Rat duodenum, jejunum, ileum, colon, stomach fundus, trachea and bronchia were removed and 1.5-2 cm muscle segments from those regions w ere 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 s tomach fundus. The contraction was slow and resistant to wash and was follo wed 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 v ascular 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 th e stomach fundus.