Flavones isolated from with tracheal smooth muscle relaxant properties.

The inflorescences of are used as folk medicine to treat various respiratory diseases. In this work, we report the isolation of seven known flavones: 5-hydroxy-3,7-dimethoxyflavone , 5,8-dihydroxy-3,7-dimethoxyflavone , 5,7-dihydroxy-3,8-dimethoxyflavone (gnaphaliin A), 3,5-dihydroxy-7,8-dimethoxyflavone (gnaphaliin B), 3,5-dihydroxy-6,7,8-trimethoxyflavone , 3,5,7-trimethoxyflavone and 3--methylquercetin . All these flavones except and showed a relaxant effect on guinea pig tracheal preparation with EC between 69.

Synergistic interaction between docosahexaenoic acid and diclofenac on inflammation, nociception, and gastric security models in rats.

Preclinical Research & Development The addition of polyunsaturated fatty acids to nonsteroidal anti-inflammatory drugs can increase their antinociceptive activity and produce a gastroprotective effect. The aim of the present study was to examine the effects of the interaction between docosahexaenoic acid (DHA) and diclofenac on inflammation (fixed ratios 1:1, 1:3, and 3:1), nociception (fixed ratio 1:3), and gastric injury in rats. DHA, diclofenac, or combinations of DHA and diclofenac produced anti-inflammatory and antinociceptive effects in rat.

Supra-Additive Interaction of Docosahexaenoic Acid and Naproxen and Gastric Safety on the Formalin Test in Rats.

Preclinical Research The aim of this work was to evaluate the effect of docosahexaenoic acid (DHA) on the pharmacokinetics and pharmacodynamics-nociception-of naproxen in rats, as well as to determine the gastric safety resulting from this combination versus naproxen alone. Female Wistar rats were orally administered DHA, naproxen or the DHA-naproxen mixture at fixed-ratio combination of 1:3. The antinociceptive effect was evaluated using the formalin test.

Gnaphaliin A and gnaphaliin B synergize the relaxant effect of salbutamol but not of ipratropium in guinea pig trachea.

Objective: This work was aimed to investigate the pharmacodynamic interactions between gnaphaliins A and B with ipratropium bromide (IBR) and salbutamol (SAL) using the guinea pig trachea model through application of the combination index (CI)-isobologram equation.

Methods: The guinea pig trachea rings in isolated chamber with Krebs-Henseleit solution (37°C) were contracted with carbachol (3 μm), and then, concentration-relaxant effect curves were constructed for individual drugs and in combination at fixed constant ratios (1 : 1, 3 : 1 and 1 : 3). Median effect and combination index (CI)-isobologram equations were used for determining interactions.

Synergistic antinociceptive effect and gastric safety of the combination of docosahexaenoic acid and indomethacin in rats.

The use of analgesics is limited by the presence of significant adverse side effects. Thus, combinations of non-steroidal anti-inflammatory drugs (NSAIDs) with other antinociceptive agents are frequently used to decrease these adverse reactions. The aims of this work were to evaluate the antinociceptive interaction of the systemic administration of the combination of DHA and indomethacin through an isobolographic analysis of the theoretical and experimental antinociceptive effect and to demonstrate the gastric safety of the mixture compared with indomethacin alone.

Synthesis, docking study and relaxant effect of 2-alkyl and 2-naphthylchromones on rat aorta and guinea-pig trachea through phosphodiesterase inhibition.

Chromone (4), which form the base structure of various flavonoids isolated as natural products, is capable of relaxing smooth muscle. This is relevant to the treatment of high blood pressure, asthma and chronic obstructive pulmonary disease. The former disorder involves the contraction of vascular smooth muscle (VSM), and the latter two bronchoconstriction of airway smooth muscle (ASM).

Development and validation of a column high-performance liquid chromatography method for quantification of ganaphaliin A and B in inflorescences of Gnaphalium liebmannii Sch. Bp ex Klatt.

An HPLC method was developed for the simultaneous determination of gnaphaliin A and B, active compounds of Gnaphalium liebmannii Sch. Bp ex Klatt. The HPLC separation was performed on an Inertsil ODS-3 (150 x 4.

Gnaphaliin A and B relax smooth muscle of guinea-pig trachea and rat aorta via phosphodiesterase inhibition.

Objectives: To explore the relaxant mechanism of action of gnaphaliin A and gnaphaliin B in guinea-pig trachea and rat aorta, and to investigate the theoretical and experimental phosphodiesterase (PDE) inhibitory activity of these flavones.

Methods: The relaxant effect and the inhibition of calcium chloride induced contractions of both flavones were evaluated on guinea-pig trachea and rat aorta rings. The PDE inhibitory activity was evaluated using a cyclic nucleotide PDE colorimetric assay kit with cAMP and cGMP as substrates.

Solving the confusion of gnaphaliin structure: gnaphaliin A and gnaphaliin B identified as active principles of Gnaphalium liebmannii with tracheal smooth muscle relaxant properties.

Inflorescences of Gnaphalium liebmannii, commonly known as "Gordolobo", is the most important remedy in Mexican traditional medicine to treat respiratory diseases, including asthma. By a bioguided fractionation of the n-hexane extract of this plant, following the relaxant effect on guinea pig tracheal smooth muscle, the flavones 5,7-dihydroxy-3,8-dimethoxyflavone (1) and 3,5-dihydroxy-7,8-dimethoxyflavone (2) were identified as the active relaxant compounds. Compounds 1 and 2 showed more potent relaxant properties than aminophylline in this model.