Action of polygodial, a sesquiterpene isolated from Drymis winteri, in the guinea-pig ileum and trachea `in vitro

• Published in: European journal of pharmacology 1998-03, Vol.344 (2), p.215-221
• Main Authors: El Sayah, Mariem, Cechinel Filho, Valdir, Yunes, Rosendo A, Pinheiro, Tânia R, Calixto, João B
• Format: Article
• Language: English
• Subjects: Allergy; Animals; Asthma; Biological and medical sciences; Bradykinin; Compound 48/80; Contraction; Female; General pharmacology; Guinea Pigs; Histamine - metabolism; Hypersensitivity - metabolism; Ileum - drug effects; Ileum - physiology; Ileum, guinea-pig; In Vitro Techniques; Male; Medical sciences; Muscle Relaxation; Muscle, Smooth - drug effects; Muscle, Smooth - physiology; Ovalbumin; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; Plants, Medicinal; Polygodial; Prostanoid; Sesquiterpenes - pharmacology; Trachea - drug effects; Trachea - physiology; Trachea, guinea-pig
• ISSN: 0014-2999; 1879-0712
• DOI: 10.1016/S0014-2999(97)01570-7

This study describes the action of the sesquiterpene polygodial, the major constituent isolated from the bark of Drymis winteri in the guinea pig ileum and trachea in vitro. Polygodial (5 to 128 μM), added for 20 min, did not affect the resting tone of the preparations, but caused graded inhibition, associated in some cases with rightward displacement of the acetylcholine, histamine (1 nM to 10 μM), bradykinin (0.1 nM to 1 μM) and KCl (1 to 100 mM)-contraction response curves. When assessed in the guinea-pig trachea, polygodial (5 to 342 μM) caused significant inhibition of bradykinin (10 pM to 1 μM), 9,11-dideoxy-9 α,11 α-methano-epoxy prostaglandin F 2 α (0.1 to 1000 nM) and KCl (1 to 100 mM)-induced contractions, although the action against bradykinin was not concentration-dependent. Polygodial (5 to 80 μM) caused a small but significant shift to the right of substance P and also the selective agonist of tachykinin NK 2 receptor [ β-Ala 8]neurokinin A-(4-10)-induced contractions in guinea pig trachea. This action of polygodial seems to be quite selective towards tachykinin NK 2 receptors since up to 432 μM, polygodial had no effect against contraction caused by tachykinin NK 1 receptor agonist, substance P methyl ester. When tested in the guinea-pig trachea from animals which had been actively sensitised to ovalbumin, polygodial (30 to 40 μM) caused time and concentration-dependent inhibition of ovalbumin-mediated contraction. In addition, polygodial (85 to 342 μM) inhibited contraction induced by compound 48/80 (1 to 1000 μg/ml), in the guinea-pig trachea from non-sensitised animals. These findings and those from our previous study are consistent with the notion that the main sesquiterpene polygodial isolated from the bark of D. winteri is responsible for most, if not all, of the relevant pharmacological action reported previously for the extract of this plant. Thus, polygodial could be of potential value in the development of a new drug for the treatment of asthma, allergy and other inflammatory processes.