Disease relevance of QUIRAL TADEODAL

• The mechanism by which polygodial produces antinociception seems likely to involve an interaction with the opioid system, mainly kappa and delta subtypes, depend on the activation of G(i/o) protein sensitive to pertussis toxin, alpha(1)-adrenoceptors, and the serotoninergic system [1].
• Polygodial and (2E)-hexenal were found to possess antibacterial activity against Salmonella choleraesuis with the minimum bactericidal concentrations (MBC) of 50 microg/mL (0.17 mM) and 100 microg/mL (0.98 mM), respectively [2].
• Finally, polygodial (4.2-42.7 micromol/kg, i.p.) produced dose-related inhibition of paw oedema induced by ovalbumin, protecting in a time-dependent manner the anaphylactic shock induced by endovenous administration of ovalbumin in animals which had been actively sensitised by this antigen [3].
• Stereospecificity of allergic contact dermatitis (ACD) to enantiomers. Part III. experimentally induced ACD to a natural sesquiterpene dialdehyde, polygodial in guinea pigs [4].
• OBJECTIVE: The aim of the present study was to test the hypothesis that protein-calorie malnutrition aggravates the gut translocation of Candida albicans triggered by mesenteric ischemia-reperfusion (IR) injury in an experimental model while testing a natural product containing the antifungal anethole/polygodial mixture (Kolorex) [5].

High impact information on QUIRAL TADEODAL

• A pet9 mutant which lacks a functional ADP-ATP translocator and is therefore respiration dependent was rapidly inhibited by polygodial [6].
• Previous studies have reported that plasma membrane disruption is the mechanism of polygodial-induced cell death; however, these results support a more complex picture of its effect [6].
• Pharmacological characterisation of the plant sesquiterpenes polygodial and drimanial as vanilloid receptor agonists [7].
• In rat isolated urinary bladder, polygodial and drimanial produced a tachykinin-mediated contraction that was inhibited by combination of NK(1) and NK(2) tachykinin receptor antagonists, SR 140333 and SR 48968 [7].
• These results suggest that polygodial uncouples ATP synthesis from electron transport at low concentrations [8].

Chemical compound and disease context of QUIRAL TADEODAL

• In contrast, polygodial antinociception was significantly attenuated by i.p. treatment of animals with naloxone, naltrindole, 2-(3, 4-dichlorophenyl)-n-methyl-n-[(1S)-1-(3-isothiocynatophenyl)-2-(1- pry rolidinyl)ethyl]acetamide, p-chlorophenylalanine, prazosin, or by i. c.v. treatment with pertussis toxin [1].

Biological context of QUIRAL TADEODAL

• The effect of polygodial on the mitochondrial energy metabolism is described in this paper [8].
• We postulate that polygodial uncouples mitochondrial ATP synthesis by affecting the electrical properties of the membrane surface and consequently collapsing the membrane potential (Deltapsi) and/or the localized transmembrane pH difference (DeltapH(S)) without affecting the DeltapH between the two bulk aqueous phases (DeltapH(B)) [8].
• Based on killing kinetics against growing and nongrowing C. albicans, polygodial showed strong and rapid fungicidal activity [9].
• These results demonstrate that the vasorelaxation of polygodial is partly dependent on the release of nitric oxide (NO )or an NO-derived substance from the vascular endothelium through an activation of a guanylyl cyclase-dependent mechanism [10].
• At the median inhibitory concentration (IC50) level, polygodial was approximately 114- to 177-fold more active in inhibiting mediated contractions to senktide and phorbol ester [11].

Anatomical context of QUIRAL TADEODAL

• A transitory stimulation of the electron transport in intact rat liver mitochondria in state 4 was also obtained at low polygodial concentrations (EC(50)=20+/-4 microM) [8].
• Similar concentrations of polygodial partially abolished the ANS fluorescence enhancement (IC(50)=2.2+/-0.4 microM) induced by succinate oxidation in submitochondrial particles but did not collapse the DeltapH [8].
• When tested in the guinea-pig trachea from animals which had been actively sensitised to ovalbumin, polygodial (30 to 40 microM) caused time and concentration-dependent inhibition of ovalbumin-mediated contraction [12].
• Action of polygodial, a sesquiterpene isolated from Drymis winteri, in the guinea-pig ileum and trachea 'in vitro' [12].
• The sesquiterpene polygodial produces graded relaxation in rings of rabbit pulmonary artery or thoracic aorta and guinea-pig pulmonary artery with endothelium [10].

Associations of QUIRAL TADEODAL with other chemical compounds

• In addition, polygodial (85 to 342 microM) inhibited contraction induced by compound 48/80 (1 to 1000 microg/ml), in the guinea-pig trachea from non-sensitised animals [12].
• When assessed in the guinea-pig trachea, polygodial (5 to 342 microM) caused significant inhibition of bradykinin (10 pM to 1 microM), 9,11-dideoxy-9alpha,11alpha-methano-epoxy prostaglandin F2alpha (0.1 to 1000 nM) and KCl (1 to 100 mM)-induced contractions, although the action against bradykinin was not concentration-dependent [12].
• Effect of EDTA alone and in combination with polygodial on the growth of Saccharomyces cerevisiae [13].
• In the lipid fraction derived from cells treated with polygodial, no PE and PS were detected, indicating a disturbance in the balance of the plasma membrane [14].
• Synergism of polygodial and trans-cinnamic acid on inhibition of root elongation in lettuce seedling growth bioassays [15].

Gene context of QUIRAL TADEODAL

• The polygodial-induced formation of IP1 was reduced by 71% under extracellular calcium-free conditions, which suggests feedback interactions between the IP formation and the increase in [Ca2+]i to account for a periodic activation of phospholipase C(PLC) [16].
• In addition, these data confirm and extend our previous suggestion that polygodial preferentially antagonizes tachykinin-mediated contraction, especially the NK3-mediated responses [11].
• When assessed in the tonic contraction induced by endothelin-1 (0.5 nM) or by phorbol (3 microM), polygodial (0.1-100 microM) produced concentration-dependent relaxation, with maximal inhibition (E(max)) of 62 +/- 2% and 100%, respectively [11].
• The sesquiterpene, polygodial, also exhibited strong inhibitory activity against human platelet aggregation and 5-LOX [17].

Analytical, diagnostic and therapeutic context of QUIRAL TADEODAL

• In addition, polygodial antinociception was not cross-tolerant to morphine, nor was its effect affected by the adrenalectomy of animals [1].
• Guinea pigs were sensitized to polygodial 1, a natural sesquiterpene dialdehyde, using intradermal injections in Freund's complete adjuvant [4].
• Considering the anti-anaphylactic properties of polygodial, a major constituent of WPE, the mast cell accumulation was concluded to be an adaptive change in response to the subchronic oral administration of WPE [18].
• The bioassay-guided chemical fractionation of this extract afforded the sesquiterpene dialdehyde polygodial as the active constituent [19].

References