The effect of thyme extract on beta2-receptors and mucociliary clearance.
Thyme is a broncholytic und secretomotoric agent. Thus, our aim was to investigate the influence of a thyme extract on beta (2)-receptors in competition binding experiments and relaxation experiments on rat uteri and trachea. Furthermore, the influence of the extract on respiratory clearance was of interest. Binding experiments were performed using purified rat lung membranes with the beta(2)-receptor ligand [(125)I]-CYP {[(125)I]-(+/-)-Iodocyanopindolol}. The transport of the fluorescence dye rhodamin 123 concerning ciliary action in the tracheal area of a mouse was investigated using a microdialysis technique. The thyme extract reduces only slightly [(125)I]-CYP binding and amplifies the displacement of [(125)I]-CYP by propranolol (non-specific beta-receptor antagonist): the displacement curve in the concentration range representing beta (2)-receptors (nM) is shifted to the left. Thyme extract had relaxing effects on organs possessing beta (2)-receptors (uterus and trachea). The propranolol-induced antagonism to isoprenaline is reverted concentration-dependently by the extract. A duplication of the rate of ciliary clearance by the extract was observed.


CONCLUSIONS
1) There is evidence for an influence of a thyme extract on beta (2)-receptors by both binding studies and biological effects: As can be derived from the shift of the propranolol displacement curve (nM), ingredients of the thyme extract slightly interact with beta (2)-receptors in rat lung tissue. This effect is indirect since no full range competition curve was reached. 2) An at least indirect interaction with beta (2)-receptors in rat uteri and trachea is revealed by a decreased antagonism of propranolol on the relaxing effect of isoprenaline by the plant extract. 3) An additional mechanism is presumed because at high extract concentrations isoprenaline-induced relaxation is complete, whereas the displacement of propranolol at beta (2)-receptors is only weak. 4) Thyme extract has an indirect (modulatory) effect on the beta (2)-receptor system. 5) Mucociliary clearance is improved in vivo. Its mechanism has still to be elucidated.
Wienkötter
N
N
Department of Pharmacology, Institute of Medicinal Chemistry, Münster, Germany.
Begrow
F
F
Kinzinger
U
U
Schierstedt
D
D
Verspohl
E J
EJ
D000318:Adrenergic beta-Agonists / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D000319:Adrenergic beta-Antagonists; D000818:Animals; D004305:Dose-Response Relationship, Drug; D005260:Female; D051379:Mice; D008810:Mice, Inbred C57BL; D009079:Mucociliary Clearance / Q000187:drug effects; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D011433:Propranolol; D051381:Rats; D017208:Rats, Wistar; D018343:Receptors, Adrenergic, beta-2 / Q000187:drug effects; D046930:Thymus Plant; D014132:Trachea / Q000187:drug effects*; D014590:Uterine Contraction / Q000187:drug effects*
D000318:Adrenergic beta-Agonists; D000319:Adrenergic beta-Antagonists; D010936:Plant Extracts; D018343:Receptors, Adrenergic, beta-2; D011433:Propranolol