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PubMed1999

Regulation of the human skeletal muscle chloride channel hClC-1 by protein kinase C.

1. The regulation of a recombinant human muscle chloride channel, hClC-1, by protein kinase C (PKC) was investigated in human embryonic kidney (HEK 293) cells. 2. External application of 4beta-phorbol esters (4beta-PMA) reduced the instantaneous whole-cell current amplitude over the entire voltage range tested. This effect was abolished when the cells were intracellularly perfused with a specific protein kinase C inhibitor, chelerythine. Inactive 4alpha-phorbolesters did not affect the chloride currents. We conclude that the effect of 4beta-phorbol esters is mediated by protein kinase C (PKC). 3. Activation of PKC resulted in changes in macroscopic current kinetics. The time course of current deactivation determined in the presence and absence of 4beta-phorbol esters could be fitted with the sum of two exponentials and a constant value. In the presence of phorbol esters, the fast time constants and the minimum value of the fraction of non-deactivating current were increased, whereas the voltage dependence of all fractional current amplitudes remained unchanged. PKC-induced phosphorylation had only small effects on the voltage dependence of the relative open probability and the maximum absolute open probability was unaffected by treatment with 4beta-PMA, as shown by non-stationary noise analysis. 4. The kinetic changes indicate that phosphorylation alters functional properties of active channels. Since the absolute open probability is not reduced, the observed macroscopic current reduction implies alterations of the ion permeation process. 5. Phosphorylation by PKC appears to affect ion transfer and gating processes. It is postulated that the phosphorylation site may be located at the cytoplasmic vestibule face of the pore.

Alkaloids↗
PubMed2000

Endothelin-1 and photoreleased diacylglycerol increase L-type Ca2+ current by activation of protein kinase C in rat ventricular myocytes.

The amphotericin B-perforated whole-cell patch clamp technique was used to determine the modulation of L-type Ca2+ channels by protein kinase C (PKC)-mediated pathways in adult rat ventricular myocytes. Application of 10 nM endothelin-1 (ET-1) increased peak Ca2+ current (ICa) by 28.2 +/- 2.5 % (n = 13) and slowed current decay. These effects were prevented by the endothelin receptor antagonist PD145065 (10 microM) and by the PKC inhibitor chelerythrine (8 microM). To establish if direct activation of PKC mimicked the ET-1 effect, the active and inactive phorbol esters (phorbol-12-myristate-13-acetate and 4alpha-phorbol-12, 13-didecanoate) were tested. Both phorbol esters (100 nM) resulted in a small (approximately 10%) increase in ICa, suggesting PKC-independent effects. Bath application of dioctanoylglycerol (diC8), a diacylglycerol (DAG) analogue which is capable of directly activating PKC, caused a gradual decline in peak ICa (50.4 +/- 6.2 %, n = 5) and increased the rate of current decay. These effects were unaffected by the PKC inhibitor chelerythrine (8 microM). Intracellular photorelease of caged diC8 with 3 or 10 s exposure to UV light produced a concentration-dependent increase in peak ICa (20. 7 +/- 8.5 % (n = 8) for 3 s UV and 60.8 +/- 11.4 % (n = 13) for 10 s UV), which could be inhibited by chelerythrine. Our results demonstrate that both ET-1 and intracellularly photoreleased diC8 increase ICa by a PKC-mediated pathway, which is in direct contrast to the PKC-independent inhibition of ICa produced by bath-applied diC8. We conclude that specific cellular pools of DAG are crucially important in the regulation of ICa by PKC.

Alkaloids↗
PubMed2001

Protein kinase C isoform-dependent modulation of ATP-sensitive K+ channels during reoxygenation in guinea-pig ventricular myocytes.

ATP-sensitive K+ (KATP) channels activated by glucose-free anoxia close immediately upon reoxygenation in single guinea-pig ventricular myocytes, while KATP channels open persistently during reperfusion in coronary-perfused guinea-pig ventricular myocardium. To investigate the reasons behind this discrepancy, we investigated whether protein kinase C (PKC) modulates the opening of KATP channels during anoxia-reoxygenation and ischaemia-reperfusion. Exposure of guinea-pig ventricular cells to glucose-free anoxia shortened the action potential duration at 90% repolarisation (APD90) and evoked the glibenclamide-sensitive robust outward current (IK,ATP). Subsequent reoxygenation caused an immediate prolongation of APD90 and a decrease in IK,ATP within approximately 20 s. When the novel (Ca2+-independent) PKC was activated by applying 1,2-dioctanoyl-sn-glycerol (1,2DOG, 20 M) with EGTA (20 mM) in the pipette, the APD90 restored gradually after reoxygenation and the extent of recovery was appoximately 80% of the pre-anoxic value. Moreover, IK,ATP decreased slowly and remained opened for up to approximately 4 min after reoxygenation. These results suggest persistent opening of KATP channels during reoxygenation. The persistent activation of KATP channels was augmented when both novel and conventional (Ca2+-dependent) isoforms of PKC were activated by applying 1,2DOG without EGTA in the pipette. In coronary-perfused right ventricular myocardium, APD90 remained shortened for up to approximately 30 min of reperfusion. The gradual restoration of APD90 after ischaemia-reperfusion was facilitated by the KATP channel blocker glibenclamide and by the potent PKC inhibitor chelerythrine. Our results provide the first evidence that PKC activation contributes to the persistent opening of KATP channels during reoxygenation and reperfusion. We also conclude that both novel and conventional PKC isoforms co-operatively modulate the opening of KATP channels during the early phase of reoxygenation.

Action Potentials↗
PubMed1993

kappa-Opioid agonist modulation of [3H]thymidine incorporation into DNA: evidence for the involvement of pertussis toxin-sensitive G protein-coupled phosphoinositide turnover.

A body of evidence has indicated that mu-opioid agonists can inhibit DNA synthesis in developing brain. We now report that kappa-selective opioid agonists (U69593 and U50488) modulate [3H]thymidine incorporation into DNA in fetal rat brain cell aggregates in a dose- and developmental stage-dependent manner, kappa agonists decreased thymidine incorporation by 35% in cultures grown for 7 days, and this process was reversed by the kappa-selective antagonist, norbinaltorphimine, whereas in 21-day brain cell aggregates a 3.5-fold increase was evident. Cell labeling by [3H]thymidine was also inhibited by the kappa-opioid agonist as shown by autoradiography. In addition, U69593 reduced basal rates of phosphoinositide formation in 7-day cultures and elevated it in 21-day cultures. Control levels were restored by norbinaltorphimine. Pertussis toxin blocked U69593-mediated inhibition of DNA synthesis. The action of kappa agonists on thymidine incorporation in the presence of chelerythrine, a protein kinase C (PKC) inhibitor, or in combination with LiCl, a noncompetitive inhibitor of inositol phosphatase, was attenuated in both 7- and 21-day cultures. These results suggest that kappa agonists may inhibit DNA synthesis via the phosphoinositide system with a pertussis toxin-sensitive G protein as transducer. In mixed glial cell aggregates, U50488 increased thymidine incorporation into DNA 3.1-fold, and this stimulation was reversed by the opioid antagonist naltrexone.

Alkaloids↗
PubMed2005

AMPA receptor stimulation increases alpha5beta1 integrin surface expression, adhesive function and signaling.

Integrin proteins are critical for stabilization of hippocampal long-term potentiation but the mechanisms by which integrin activities are involved in synaptic transmission are not known. The present study tested whether activation of alpha-amino-3-hydroxy-5-methylisoxazole-4-proprionate (AMPA) class glutamate receptors increases surface expression of alpha5beta1 integrin implicated in synaptic potentiation. Surface protein biotinylation assays demonstrated that AMPA treatment of COS7 cells expressing GluR1 homomeric AMPA receptors increased membrane insertion and steady-state surface levels of alpha5 and beta1 subunits. Treated cells exhibited increased adhesion to fibronectin- and anti-alpha5-coated substrates and tyrosine kinase signaling elicited by fibronectin-substrate adhesion, as expected if new surface receptors are functional. Increased surface expression did not occur in calcium-free medium and was blocked by the protein kinase C inhibitor chelerythrine chloride and the exocytosis inhibitor brefeldin A. AMPA treatment similarly increased alpha5 and beta1 surface expression in dissociated neurons and cultured hippocampal slices. In both neuronal preparations AMPA-induced integrin trafficking was blocked by combined antagonism of NMDA receptor and L-type voltage-sensitive calcium channel activities but was not induced by NMDA treatment alone. These results provide the first evidence that glutamate receptor activation increases integrin surface expression and function, and suggest a novel mechanism by which synaptic activity can engage a volley of new integrin signaling in coordination with, and probably involved in, stabilization of synaptic potentiation.

Alkaloids↗
PubMedDate not supplied

Differential regulation by Ca(2+) of calmodulin- and PKC-dependent contractile pathways in cat lower oesophageal sphincter.

1. In the present investigation we examined the regulation of calmodulin (CaM)- and protein kinase C (PKC)-dependent pathways by cytosolic Ca(2+) in the contraction of cat lower oesophageal sphincter (LES). 2. Force developed in response to increasing doses of acetylcholine (ACh) was directly related to the increase of the [Ca(2+)](i) measured by fura-2. Thapsigargin, which depletes Ca(2+) stores, reduced the contraction and the [Ca(2+)](i). In addition, contraction in response to maximal ACh was reduced by the CaM inhibitor CGS9343B but not by the PKC inhibitor chelerythrine. The contraction in response to submaximal ACh was reduced by chelerythrine but not by CGS9343B. 3. In permeabilized cells, the contraction in response to low Ca(2+) (0.54 microm) was also reduced by CGS9343B. 4. The response to high Ca(2+) (1.0 microm) was reduced by CGS9343B. ACh also inhibited PKC activation induced by diacylglycerol, which activation is inhibited by the N-myristoylated peptide inhibitor derived from pseudosubstrate sequences of PKCalphabetagamma (myr-PKC-alphabetagamma), but not of myr-PKC-alpha. 5. These data are consistent with the view that activated CaM-dependent pathways inhibit PKC-dependent pathways, this switch mechanism might be regulated by Ca(2+) in the LES.

1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine↗
PubMed1994

Effects of protein kinase C activators upon the late stages of the ACTH secretory pathway of AtT-20 cells.

1. The mouse AtT-20/D16-16 anterior pituitary tumour cell line was used as a model system for the study of phorbol 12-myristate 13-acetate (PMA)-mediated enhancement of calcium-evoked adrenocorticotrophin (ACTH) secretion. 2. PMA stimulated ACTH secretion from intact cells in a concentration-dependent manner. Other phorbol esters; phorbol 12,13-dibutyrate (PDBu) and phorbol 12,13-didecanoate (PDD) and diacylglycerol analogues; 1-oleoyl-2-acetyl-sn-glycerol (OAG) and 1,2-dioctanoyl-sn-glycerol (DOG) also stimulated ACTH release from intact AtT-20 cells. This would suggest that activation of protein kinase C (PKC) stimulates ACTH secretion from AtT-20 cells. 3. Calcium stimulated ACTH secretion from electrically-permeabilized cells over the concentration-range of 10(-7) M to 10(-5) M. PMA (10(-7) M) enhanced the amount of ACTH secreted at every concentration of calcium investigated. The PKC inhibitor, chelerythrine (10(-5) M) blocked the PMA (10(-7) M)-evoked enhancement of calcium (10(-5) M)-stimulated ACTH secretion but did not alter significantly the calcium (10(-5) M)-evoked secretion itself. This suggests that PKC modulates the secretory response to increases in intracellular calcium but does not mediate the effects of calcium. 4. Guanosine 5'-O-(3-thiotriphosphate) (GTP-gamma-S, 10(-5) M) stimulated ACTH secretion from permeabilized cells in the absence of calcium and was additive with calcium-evoked ACTH secretion up to a maximum value which could be achieved by calcium acting alone. This suggests that a GTP-binding protein mediates the secretory response to increases in the intracellular calcium. PMA (10-7 M) enhanced ACTH secretion stimulated by the combination of calcium and GTP-gamma-S (10-5 M).5. GTP-gamma-S stimulated ACTH secretion from permeabilized cells in a concentration-dependent manner with a threshold of 10-6 M. PMA (10-7 M) increased the amount of ACTH secretion evoked by every concentration of GTP-gamma-S investigated. Chelerythrine (10-s M) blocked the PMA (10-7 M)-evoked enhancement of GTP-gamma-S (10-4 M)-stimulated ACTH secretion but did not significantly alter GTP-gamma-S(10-4 M)-evoked secretion itself. This suggests that PKC modulates the secretory response to GTP-gamma-S but does not mediate the effects of GTP-gamma-S.6. GTP-gamma-S (10-8-10-4-M) stimulated ACTH secretion from permeabilized cells either in the presence or absence of ATP (5 mM) indicating that its effects on secretion are ATP-independent.7. The results of the present study support the hypothesis that, in AtT-20 cells, PMA is acting at some site distal to calcium entry which modulates the ability of an increase in cytosolic calcium concentration to stimulate ACTH secretion. This site of action is either at the level of or at some stage distal to a GTP-binding protein which mediates the effects of calcium upon secretion.8. PMA, unlike adenosine 3':5'-cyclic monophosphate (cyclic AMP) (Guild, 1991), can stimulate ACTH secretion from permeabilized cells in the absence of added calcium and guanine nucleotides which suggests that PMA and cyclic AMP are acting through distinct mechanisms at this post calcium site of action.

Adenosine Triphosphate↗
PubMed1995

Effects of mastoparan upon the late stages of the ACTH secretory pathway of AtT-20 cells.

1. The mouse AtT-20/D16-16 anterior pituitary tumour cell line was used as a model system for the study of the effects of mastoparan upon the late stages of the adrenocorticotrophin (ACTH) secretory pathway. 2. Mastoparan (10(-8)-10(-5) M), an activator of heterotrimeric guanosine 5'-triphosphate binding proteins (G-proteins), stimulated ACTH secretion from electrically-permeabilized AtT-20 cells in a concentration-dependent manner in the effective absence of calcium ions with a threshold of 10(-6) M. Guanosine 5'-O-(3-thiotriphosphate) (GTP-gamma-S) (10(-8)-10(-4) M) also stimulated ACTH secretion from electrically-permeabilized AtT-20 cells in a concentration-dependent manner in the effective absence of calcium ions with a threshold of 10(-6) M. This GTP-gamma-S-evoked secretion is consistent with previous studies which demonstrated that a G-protein, termed GE, mediates calcium evoked ACTH secretion from AtT-20 cells. GTP-gamma-S-evoked secretion however was not as great as that obtained in response to mastoparan. 3. Both mastoparan (10(-5) M) and GTP-gamma-S (10(-4) M) stimulated ACTH secretion from electrically-permeabilized AtT20 cells in a time-dependent manner. A time of 30 min was adopted as the standard incubation period for the study of both mastoparan and GTP-gamma-S-stimulated ACTH secretion from permeabilized AtT-20 cells. 4. Mastoparan (10(-8)-10(-5) M) stimulated ACTH secretion from permeabilized AtT-20 cells to the same extent in the presence and absence of the protein kinase C (PKC) inhibitor, chelerythrine chloride (10(-5) M). 5. Mastoparan (10-8 10-5 M)-stimulated ACTH secretion from permeabilized AtT-20 cells was significantly reduced in the presence of guanosine 5'-O-(2-thiodiphosphate) (GDP-beta-S, 10-4 M).6. The mastoparan analogue, Mas-7 (10-8-10-5 M) stimulated ACTH secretion from permeabilized AtT-20 cells to a greater extent than mastoparan (10-8 10-5 M) however, the mastoparan analogue Mas-17 (10-8- 10-5 M) had no effect upon ACTH secretion from permeabilized AtT-20 cells.7. Mastoparan (10-8-10-5 M) stimulated ACTH secretion from permeabilized AtT-20 cells in the presence and absence of ATP, normally present in the standard permeabilization medium at a concentration of 5 mM. Mastoparan (10-8- 10-5 M)-stimulated ACTH secretion as well as control secretion was reduced when ATP was omitted.8. The results of the present study demonstrate that mastoparan stimulated ACTH secretion from permeabilized AtT-20 cells and displayed characteristics consistent with calcium ion- and GTP-y-gamma-S-stimulated ACTH secretion from permeabilized AtT-20 cells. This suggests that in permeabilized AtT-20 cells, mastoparan directly activates GE and that this G-protein may be a heterotrimeric G-protein. This study also suggests mastoparan may be a useful alternative to GTP-gamma-S as a means of directly activating GE.

Adrenocorticotropic Hormone↗
PubMed1995

Involvement of protein kinase C in the delayed cytoprotection following sublethal ischaemia in rabbit myocardium.

Rabbit hearts were preconditioned with four 5 min coronary artery occlusions 24 h before 30 min coronary occlusion with 120 min reperfusion. Preconditioning significantly reduced the percentage of myocardium infarcting within the risk zone from 49.1 +/- 4.3% to 31.8 +/- 3.5% (P < 0.05). When the protein kinase C (PKC) inhibitor, chelerythrine, was administered just before preconditioning, the delayed protection against infarction 24 h later was abolished. We conclude that the delayed cytoprotective response associated with ischaemic preconditioning of myocardium is likely to involve the early activation of one or more PKC subtypes.

Alkaloids↗
PubMed1995

Involvement of multiple protein kinase C isozymes in the ACTH secretory pathway of AtT-20 cells.

1. The mouse AtT-20/D16-16 anterior pituitary tumour cell line was used as a model system for the study of protein kinase C (PKC)-mediated enhancement of calcium- and guanine nucleotide-evoked adrenocorticotrophin (ACTH) secretion. 2. A profile of the PKC isozymes present in AtT-20 cells was obtained by Western blotting analysis and it was found that AtT-20 cells express the alpha, beta, epsilon and zeta isoforms of PKC. 3. PKC isozymes were activated by the use of substances reported to activate particular isoforms of the enzyme. The effects of these substances were investigated in both intact and electrically-permeabilized cells. Phorbol 12-myristate 13-acetate (PMA, EC50 = 1 +/- 0.05 nM, which activates all isozymes of PKC, except the zeta isozyme), thymeleatoxin (TMX, EC50 = 10 +/- 0.5 nM, which activates the alpha, beta and gamma isozymes) and 12-deoxyphorbol 13-phenylacetate 20-acetate (dPPA, EC50 = 3 +/- 0.5 nM, a beta 1-selective isozyme activator) all stimulated ACTH secretion from intact cells in a concentration-dependent manner. Maximal TMX stimulated ACTH secretion was of a similar degree to that obtained in response to PMA but maximal dPPA-stimulated ACTH secretion was only 60-70% of that obtained in response to PMA or TMX. 4. Calcium stimulated ACTH secretion from electrically-permeabilized cells over the concentration-range of 100 nM to 10 microM. PMA (100 nM), TMX (100 nM) but not dPPA (100 nM) enhanced the amount of ACTH secreted at every concentration of calcium investigated. PMA (100 nM) and TMX (100 nM)significantly enhanced ACTH secretion in the effective absence of calcium (i.e. where the free calcium concentration is nM).5. GTP-gamma-S stimulated ACTH secretion from permeabilized cells in a concentration-dependent manner with a threshold of 1 micro M. PMA (100 nM), TMX (100 nM) but not dPPA (100 nM) increased the amount of ACTH secretion evoked by every concentration of GTP-gamma-S investigated.6. The PKC inhibitor, chelerythrine chloride (10 micro M), blocked the PMA (100 nM)-evoked enhancement of calcium- and GTP-micro-S-stimulated ACTH secretion but did not significantly alter calcium- or GTP-micro-S-evoked secretion itself.7. The present paper indicates that AtT-20 cells express multiple isoforms of PKC and that these act at different sites in the secretory pathway for ACTH secretion. The alpha and epsilon isozymes of PKC can act distal to calcium entry to modulate the ability of increased cytosolic calcium concentrations to stimulate ACTH secretion. This site of action is either at the level of, or at some stage distal to, a GTP-binding protein which mediates the effects of calcium upon ACTH secretion. The beta isozyme of PKC may act ata stage early in the secretory pathway to regulate the cytosolic calcium concentration.

Adrenocorticotropic Hormone↗
PubMed1996

Differential effects of protein kinase C inhibitors on chemokine production in human synovial fibroblasts.

1. Rheumatoid arthritis is associated with the accumulation and activation of selected populations of inflammatory cells within the arthritic joint. One putative signal for this process is the production, by resident cells, of a group of inflammatory mediators known as the chemokines. 2. The chemokines interleukin-8 (IL-8), monocyte chemotactic protein-1 (MCP-1) and RANTES (regulated on activation normal T-cell expressed and presumably secreted) are target-cell specific chemoattractants produced by synovial fibroblasts in response to stimulation with interleukin-1 alpha (IL-1 alpha) or tumour necrosis factor alpha (TNF alpha). The signalling pathways involved in their production are not well defined. We therefore used four different protein kinase C inhibitors to investigate the role of this kinase in the regulation of chemokine mRNA and protein expression in human cultured synovial fibroblasts. 3. The non-selective PKC inhibitor, staurosporine (1-300 nM) significantly increased the production of IL-1 alpha-induced IL-8 mRNA and protein. A specific PKC inhibitor, chelerythrine chloride (0.1-3 microM), also caused a small concentration-dependent increase in IL-8 mRNA and protein production. In contrast, 3-[1-[3-(amidinothio)propyl]-3-indoly]-4-(1-methyl-3-indolyl )- 1H-pyrrole-2,5-dione methanesulphonate (Ro 31-8220) and 2[1-(3-dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3- yl)-maleimide (GF 109203X), two selective PKC inhibitors of the substituted bisindolylmaleimide family had a concentration-dependent biphasic effect on IL-1 alpha or TNF alpha-induced chemokine expression. At low concentrations they caused a stimulation in chemokine production, which was especially evident at the mRNA level. At higher concentrations both inhibited IL-1 alpha or TNF alpha-induced chemokine mRNA and protein production. Ro 31-8220 was 10 fold more potent than GF 109203X, with an IC50 of 1.6 +/- 0.08 microM (mean +/- s.e.mean, n = 4) for IL-1 alpha induced IL-8 production. Ro 31-8220 also inhibited the expression of IL-1 alpha or TNF alpha-induced MCP-1 and RANTES mRNA with a similar potency. 4. The stimulatory effect of staurosporine is discussed in relation to the known poor selectivity of this inhibitor for PKC. It is proposed that activation of an isoform of PKC, possibly PKC epsilon or zeta, which is inhibited by higher concentrations of the bisinodolylmaleimides, plays a role in the regulation of chemokine expression induced by IL-1 alpha or TNF alpha in synovial cells. 5. The inhibition of chemokine production by bisindolylmaleimide compounds heralds a novel approach for future anti-inflammatory therapies.

Alkaloids↗
PubMed1985

Some effects of a Sanguinarine-containing mouthrinse on developing plaque and gingivitis.

The present clinical trial was performed to assess the effect of a Sanguinarine-containing mouthrinse on developing plaque and gingivitis in man. The trial was designed as a blind cross-over study. The active mouthrinse consisted of a 0.03% aqueous solution of Sanguinaria extract; an aqueous solution with similar color and taste as the active rinse was used as the placebo preparation. 14 dental students participated in the trial. At the start of each of 2 test phases, their gingival conditions were normal and their tooth surfaces free from dental plaque. Following a baseline examination, the participants refrained from mechanical tooth cleaning measures for 2 weeks. They rinsed twice daily with either the active or the placebo mouthrinse. Clinical examinations of plaque and gingivitis were repeated after 4, 7 and 14 days use of the mouthrinse preparation. During the second test phase of no mechanical tooth cleaning, the subjects who previously had rinsed with the placebo solution now used the active compound and vice versa. The results demonstrated that the Sanguinarine-containing mouthrinse was effective in reducing plaque formation and retarding the development of gingivitis.

Adult↗
PubMed1986

The effect of mouthrinses on parameters characterizing human periodontal disease.

The objective of the present clinical trial was to assess the efficacy of mouthwashes containing antiseptic agents on established and developing plaque and periodontal disease in adult subjects using a newly described clinical research model. The study was carried out in 21 patients with periodontal disease. At the baseline examination, all tooth surfaces-sites were studied with regard to dental plaque, gingivitis, bleeding on probing to the base of the pocket and probing pocket depths. The patients were subsequently randomly assigned to 1 of 3 groups, each consisting of 7 individuals. Group A rinsed with a 0.01% solution of Sanguinarine, group B rinsed with a 0.2% solution of chlorhexidine and group C rinsed with a placebo solution. No instructions regarding mechanical plaque control measures or information regarding the etiology and pathogenesis of periodontal disease were given to any of the patients during the course of the 6-weeks of trial. The clinical examination was repeated after 2 weeks use of the mouthwash preparations. Following the re-examination, all patients were subjected to scaling and root planing in 2 jaw quadrants chosen at random. After another 2 weeks, the 2nd re-examination was performed and the teeth in the 2 remaining jaw quadrants were thoroughly scaled. The final examination was performed 2 weeks later. During the 4 weeks of rinsing, without adjunctive professional mechanical debridement, the frequency distribution of plaque Index scores 2 + 3 did not change in the group of patients using the placebo solution, but was significantly reduced in both the chlorhexidine and the Sanguinarine groups.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1987

Lacking anti-plaque efficacy of 2 sanguinarine mouth rinses.

The aim of the study was to compare the anti-plaque effect of sanguinaria extract to that of a known effective agent, chlorhexidine gluconate, and to that of a known ineffective agent, tap water. The study was conducted as a 3 times crossed-over and blindly evaluated 3 week clinical trial. 12 dental students rinsed in an individually randomized sequence twice daily for 4 days (Monday to Friday) with Viadent containing 0.03% sanguinaria extract (0.01% sanguinarine chloride) and a 1000 ppm concentration of zinc ions (ZnCl2), 2 X 30 s X 10 ml; with Hibitane Dental containing 0.2% chlorhexidine gluconate, 1 min X 10 ml; and with tap water, 1 min X 10 ml. Mechanical oral hygiene was allowed only during the 3 days between test periods. When measured according to the plaque index or in terms of plaque wet weight, only the chlorhexidine rinse further reduced the low Monday scores. No significant difference was observed between Friday scores after rinses with Viadent and water. The variation in effect of the 3 rinses was less marked when assessed by means of area of plaque on the tooth surfaces. Subjectively, both the taste and effect of Viadent was reported to be poor. In a second controlled clinical trial using the same design, no significant difference in anti-plaque effect was found between the commercially available Viadent rinse and an experimental rinse with a tripled concentration of sanguinarine chloride but the same content of zinc.

Alkaloids↗
PubMed1987

The relationship of sanguinaria extract concentration and zinc ion to plaque and gingivitis.

The effects of sanguinaria extract and zinc chloride on plaque growth and gingivitis inhibition were assessed on subjects with initially plaque-free tooth surfaces using a series of oral rinses in a single-blind, crossover, no-oral-hygiene study lasting 2 weeks. A placebo oral rinse containing no sanguinaria or zinc chloride (A), and test rinses containing 150 micrograms/ml sanguinaria and 0.2% zinc chloride (B), 300 micrograms/ml sanguinaria and no zinc chloride (C), and 300 micrograms/ml sanguinaria and 0.2% zinc chloride (D) were evaluated. Subjects using the higher concentration rinses C and D had significantly lower plaque scores than rinse A at 7 and 14 days (p less than 0.05 for C, p less than 0.01 for D). However, groups C and D were not significantly different from each other. Group D had significantly lower plaque (p less than 0.05) and gingivitis (p less than 0.01) scores than group B. Subjects who used rinse B and placebo rinse A had the highest plaque and gingivitis scores and comparison of these two groups revealed no significant difference. At the end of 14 days, the % distribution of 0 plaque and gingivitis scores was greatest among subjects using rinses C and D. Subjects in these 2 groups also had the lowest incidence of plaque and gingivitis scores of 2+. It is concluded that the effects of sanguinaria rinses on developing plaque and gingivitis are influenced more by sanguinaria concentrations than the presence or absence of zinc ion, but that zinc ion may provide a mild enhancement of sanguinaria effectiveness against gingivitis.

Adult↗
PubMed1987

Effect of sanguinaria extract on development of plaque and gingivitis when supragingivally delivered as a manual rinse or under pressure in an oral irrigator.

The effects on developing plaque and gingivitis following rinsing with a placebo oral rinse or an oral rinse containing 300 micrograms/ml sanguinaria extract (sanguinaria) were compared to effects produced by supragingival irrigation with dilute solutions of the rinse corresponding to 22.5 micrograms/ml sanguinaria and 90 micrograms/ml sanguinaria. The study design was a repeated measures, single-blind crossover with no oral hygiene over 2 weeks duration. After 7 and 14 [corrected] days, significantly lower plaque and gingivitis scores were obtained with use of the sanguinaria-containing rinse and irrigating solutions compared with the placebo rinse. There were no significant differences in plaque and gingivitis scores between the groups using the sanguinaria rinse and the sanguinaria irrigating solutions. A comparison [corrected] of % distribution of 0, 1 and 2+ scores also indicated that rinsing and supragingival irrigation with sanguinaria was more effective in plaque and gingivitis control than rinsing with the placebo. The results suggest that sanguinaria oral rinse may be effective in controlling plaque and gingivitis when delivered by manual rinsing or supragingival irrigation.

Adult↗
PubMed1987

Effect of sanguinaria extract on established plaque and gingivitis when supragingivally delivered as a manual rinse or under pressure in an oral irrigator.

Sanguinaria extract (sanguinaria) solutions were evaluated in 44 subjects in a 2-week, no oral hygiene study as a 300 micrograms/ml manual rinse, and the results compared to supragingival irrigation with 22.5 micrograms/ml sanguinaria concentration and supragingival irrigation with water. Both the manual use of sanguinaria and supragingival irrigation of dilute sanguinaria produced significantly less plaque growth than supragingival irrigation with deionized water. In terms of % changes from baseline, manual rinsing and supragingival irrigation with sanguinaria limited plaque growth to 17.7% and 24.2%, respectively, while irrigation with water had a 51.5% growth. For gingivitis, control supragingival irrigation with sanguinarine and with water were statistically different from manual rinsing with sanguinaria. Compared to baseline, the groups irrigating with sanguinaria and with water had gingivitis reductions of 68.7% and 73.3%, respectively, while manual rinsing with sanguinaria had a 29.6% reduction. The results suggest that dilute solutions of sanguinaria delivered via rinsing or supragingival irrigation are effective in controlling plaque as an additional benefit to the use of supragingival irrigation to control gingivitis. Supragingival irrigation with sanguinaria as part of a home care routine for patients with plaque and gingivitis is suggested.

Adult↗
PubMed1988

Photographic assessment of the antiplaque properties of sanguinarine and chlorhexidine.

The purpose of this study was to assess the effect of rinsing and topical application of sanguinarine on labial surface plaque accumulation, compared with topically applied water, and compared with rinsing with chlorhexidine, while refraining from all oral hygiene measures for 5 days. Color photographs of the disclosed plaque were taken at the end of each phase of treatment and blindly traced using an Apple II micro-computer graphic tablet digitizer. The plaque score for each tooth was calculated by dividing the computer reading of the labial plaque surface area by the total labial surface area of the tooth. Topically applied sanguinarine showed better plaque reduction than mouthrinsing with sanguinarine. There was a significant reduction in plaque accumulation after rinsing with chlorhexidine compared with topically applied sanguinarine, water, and mouthrinsing with sanguinarine. The results of this study indicate that chlorhexidine is a more superior antiplaque agent than sanguinarine. The use of an Apple II micro-computer graphic tablet digitizer provided a valuable method for accurate plaque assessments.

Administration, Topical↗