In vitro relaxant and spasmolytic effects of constituents from Viburnum prunifolium and HPLC quantification of the bioactive isolated iridoids.
BACKGROUND
Viburnum prunifolium is a North America shrub used in ethnomedicine because of its spasmolytic, sedative, and anti-asthmatic properties.


OBJECTIVE
Contrasting results were reported in past literature about the active principles of this plant. Our aim was to clarify this matter by evaluating the relaxant and spasmolytic activities of the main constituents obtained from the drug.


METHODS
The pharmacological assays were carried out on rabbit jejunum spontaneous contractions and on guinea-pig carbachol-precontracted trachea.


RESULTS
Cumulative concentration (1-100 microg/ml) of Viburnum prunifolium methanolic extract (MeOH extract), its purified fractions soluble in ethylacetate (EtOAc fraction) and in n-butanol (BuOH fraction), and the iridoid glucosides (2 x 10(-5) to 4 x 10(-4)M): 2'-O-acetyldihydropenstemide (1), 2'-O-trans-p-coumaroyldihydropenstemide (2), 2'-O-acetylpatrinoside (3), and patrinoside (4), isolated from EtOAc fraction (1 and 2) and BuOH fraction (3 and 4), induced both relaxant effect of rabbit jejunum spontaneous contractions and spasmolytic effect on guinea-pig carbachol (5.5 x 10(-7)M)-precontracted trachea. Propranolol (10(-6)M) antagonised all Viburnum prunifolium tested components relaxant and spasmolytic effects. At non-relaxing concentrations (0.5 microg/ml), MeOH extract and its fractions induced a potentiating effect of isoprenaline cumulative concentrations also in both isolated tissues.


CONCLUSIONS
In both tissues, the order of potency was EtOAc fraction>BuOH fraction>MeOH extract and 1>2>3>4 suggesting that the major iridoids of EtOAc fraction may be considered among the most active compounds. HPLC analysis of the bioactive iridoids indicates that 1 and 2 are present for 7.38% and 14.90% in EtOAc fraction, and 3 and 4 for 18.47% and 8.86% in BuOH fraction. By comparing the values of EC(50) of the fractions and compounds isolated from them, we may assume that the iridoids play a significant role in the biological activity of the corresponding fractions.
Department of Therapeutic Research and Medicines Evaluation, Istituto Superiore di Sanità, V.le Regina Elena 299, 00161 Rome, Italy. cometa@iss.it
Maria Francesca
MF
Cometa
Laura
L
Parisi
Maura
M
Palmery
Annarita
A
Meneguz
Lamberto
L
Tomassini
D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D005960:Glucosides / Q000302:isolation & purification / Q000494:pharmacology*; D006168:Guinea Pigs; D039823:Iridoids / Q000302:isolation & purification / Q000494:pharmacology*; D007583:Jejunum / Q000187:drug effects / Q000378:metabolism; D008297:Male; D008519:Medicine, Traditional; D009119:Muscle Contraction / Q000187:drug effects; D009126:Muscle Relaxation / Q000187:drug effects; D010276:Parasympatholytics / Q000302:isolation & purification / Q000494:pharmacology; D010936:Plant Extracts / Q000494:pharmacology*; D011817:Rabbits; D012997:Solvents / Q000737:chemistry; D014132:Trachea / Q000187:drug effects / Q000378:metabolism; D027925:Viburnum / Q000737:chemistry*
D005960:Glucosides; D039823:Iridoids; D010276:Parasympatholytics; D010936:Plant Extracts; D012997:Solvents