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Effects of sulfur and salicylic acid in a shampoo base in the treatment of dandruff: a double-blind study using corneocyte counts and clinical grading.

The effectiveness of sulfur 2 percent and salicylic acid 2 percent either alone or in combination in a shampoo base was determined in a double-blind controlled study using two methods of evaluation: clinical assessment of scaling and corneocyte counts (the number of desquamating cells/cm2). Forty-eight subjects (twenty-nine men and nineteen women) with moderate to severe scaling shampooed their hair under supervision twice a week for five weeks, using one of four formulas: sulfur 2 percent plus salicylic acid 2 percent in a shampoo vehicle; sulfur 2 percent in a shampoo vehicle; salicylic acid 2 percent in a shampoo vehicle; or the shampoo vehicle alone. On days 0, 7, 14, 21, 28, and 35 the degree of scaling was assessed, and specimens were taken for corneocyte counts. Significantly greater and earlier reductions in both degree of scaling and corneocyte counts were seen in subjects treated with the formula containing both sulfur 2 percent and salicylic acid 2 percent in the shampoo base than in those who received either active ingredient alone or the shampoo vehicle.

Adult↗

Systemic absorption of topical salicylic acid.

The systemic absorption of salicylic acid in humans following topical application in either hydrophilic ointment or polyethylene glycol 400 vehicle was studied. Drug absorption was minimal following application to intact skin; however, measurable levels (8 mg/dl) were attained when the stratum corneum was removed prior to application of the drug in hydrophilic ointment. A one-compartment open model with first order absorption and elimination processes was fitted to the plasma salicylate concentrations as a function of time. Computer simulations predict that plasma salicylate levels associated with toxicity in some patients may be present after repetitive application of the drug in hydrophilic ointment.

Adult↗

High-performance liquid chromatographic method for the determination of salicylic acid and its metabolites in urine by direct injection.

A direct injection method has been developed for the determination of salicylic acid and its metabolites in urine. Urine samples are treated with hydroxylamine to convert salicyl acyl glucuronide to salicylhydroxamic acid, which can be accurately quantitated by direct injection into a high-performance liquid chromatographic system along with salicylic acid, gentisic acid and salicyluric acid. Salicyl phenolic glucuronide is quantitated by difference after hydrochloric acid hydrolysis at 65 degrees C with no loss of salicylic acid by sublimation or hydrolytic loss of salicyluric acid. This method has been applied to urine samples from human subjects and the results are discussed.

Chromatography, High Pressure Liquid↗

Effect of Daylength on the Ability of Salicylic Acid to Induce Flowering in the Long-day Plant Lemna gibba G3 and the Short-day Plant Lemna paucicostata 6746.

When the long-day plant Lemna gibba L., strain G3 is grown on control medium the critical daylength is just under 10 hours. With 3.2 micromolar salicylic acid added to the medium substantial flower promotion is obtained on 9-, 10-, and 11-hour daylengths. On an 8-hour daylength salicylic acid treatment results in only a very small flowering response, and with daylengths less than 8 hours flowering is never obtained. Thus, salicylic acid treatment causes a shift in the critical daylength of about 2 hours, from just under 10 hours to just under 8 hours.Salicylic acid treatment also results in flower promotion in the short-day plant Lemna paucicostata Hegelm., strain 6746, and the optimal concentration of 1.8 to 3.2 micromolar agrees well with the results for L. gibba G3. In control medium the critical daylength for L. paucicostata 6746 is about 14 hours. When the plants are given 3.2 micromolar salicylic acid substantial flower promotion is obtained on daylengths of 13 and 14 hours, and the critical daylength is close to 15 hours. With daylengths longer than 15 hours, flowering is never obtained. These results are similar to those for L. gibba G3 since for both plants salicylic acid stimulates flowering by causing a shift in the critical daylength curve, but for L. paucicostata 6746 the shift is only about 1 hour and the critical daylength is extended rather than shortened.

Journal Article↗

"Keratolytic" effect of salicylic acid.

The "keratolytic" effect of salicylic acid was examined in guinea-pig skin. Using a fluorescent staining method the str. corneum cells could be seen to rapidly become detached. The cellular walls remained unchanged. This drug therefore appears to primarily reduce the intercellular cohesiveness of the horny cells.

Animals↗

Simultaneous determination of aspirin and salicylic acid in bulk aspirin and in plain, buffered, and enteric-coated tablets by high-pressure liquid chromatography with UV and fluorescence detectors.

A quantitative high-pressure liquid chromatographic method that uses a reversed-phase column coupled to UV and fluorescence detectors was developed to determine aspirin and salicylic acid in bulk aspirin and in plain, buffered, and enteric-coated tablets. The aspirin was dissolved, filtered, and injected into the chromatograph. The UV absorbance of aspirin was determined at 254 nm, and the fluorescence of salicylic acid was measured at 425 nm. Excipients and impurities did not interfere. Recoveries of 100% were obtained for aspirin and salicylic acid from simulated tablet formulations. Results obtained by the USP XIX procedure and the proposed method were compared. The coefficient of variation for the aspirin analysis was 0.59%; for salicylic acid, it was 1.69%. The rate of hydrolysis of aspirin to salicylic acid in the solvents used was < 0.05%/hr.

Aspirin↗

Down regulation of virulence factors of Pseudomonas aeruginosa by salicylic acid attenuates its virulence on Arabidopsis thaliana and Caenorhabditis elegans.

Salicylic acid (SA) is a phenolic metabolite produced by plants and is known to play an important role in several physiological processes, such as the induction of plant defense responses against pathogen attack. Here, using the Arabidopsis thaliana-Pseudomonas aeruginosa pathosystem, we provide evidence that SA acts directly on the pathogen, down regulating fitness and virulence factor production of the bacteria. Pseudomonas aeruginosa PA14 showed reduced attachment and biofilm formation on the roots of the Arabidopsis mutants lox2 and cpr5-2, which produce elevated amounts of SA, as well as on wild-type Arabidopsis plants primed with exogenous SA, a treatment known to enhance endogenous SA concentration. Salicylic acid at a concentration that did not inhibit PA14 growth was sufficient to significantly affect the ability of the bacteria to attach and form biofilm communities on abiotic surfaces. Furthermore, SA down regulated three known virulence factors of PA14: pyocyanin, protease, and elastase. Interestingly, P. aeruginosa produced more pyocyanin when infiltrated into leaves of the Arabidopsis transgenic line NahG, which accumulates less SA than wild-type plants. This finding suggests that endogenous SA plays a role in down regulating the synthesis and secretion of pyocyanin in vivo. To further test if SA directly affects the virulence of P. aeruginosa, we used the Caenorhabditis elegans-P. aeruginosa infection model. The addition of SA to P. aeruginosa lawns significantly diminished the bacterium's ability to kill the worms, without affecting the accumulation of bacteria inside the nematodes' guts, suggesting that SA negatively affects factors that influence the virulence of P. aeruginosa. We employed microarray technology to identify SA target genes. These analyses showed that SA treatment affected expression of 331 genes. It selectively repressed transcription of exoproteins and other virulence factors, while it had no effect on expression of housekeeping genes. Our results indicate that in addition to its role as a signal molecule in plant defense responses, SA works as an anti-infective compound by affecting the physiology of P. aeruginosa and ultimately attenuating its virulence.

Animals↗

[Determination of resorcinol and salicylic acid in piyanning tincture by high performance liquid chromatography].

A method for the simultaneous determination of resorcinol and salicylic acid in Piyanning tincture by HPLC has been proposed. Operating conditions were Hyppersil ODS column, 4.6 mm x 200 mm, V (methanol): V(water): V(acetic acid) = 50:50:0.9 mobile phase and UV detection at 285 nm. The linear ranges of the method were 0.05-0.25 g/L(r = 1.000) for resorcinol and 0.025-0.127 g/L(r = 1.000) for salicylic acid. The limits of detection were both 0.2 mg/L at a signal-to-noise of 3. The assay method was capable to resolve resorcinol and salicylic acid from their impurities.

Chromatography, High Pressure Liquid↗

Percutaneous absorption of salicylic acid.

The potential hazards of repeated topical application of salicylic acid under occlusion to large areas of the body was evaluated by measuring the percutaneous absorption and serum salicylate concentrations in four patients with active psoriasis. Serum salicylate concentrations never exceeded 5 mg/100 ml in any of the patients, and although greater than 60 percent of the salicylic acid applied was absorbed, no evidence of accumulation or toxicity was observed. This form of treatment appears to present little potential hazard even in patients with extensive skin disease. Therapy could be hazardous for patients with impaired hepatic or renal function or for smaller children. The urinary excretory products of salicylate metabolism were compared following topical and intravenous salicylate administration to determine if the skin plays any part in the biotransformation of salicylate during percutaneous absorption. Our data are too limited and inconclusive to answer this question.

Administration, Topical↗

Comparison of a salicylic acid cleanser and a benzoyl peroxide wash in the treatment of acne vulgaris.

A four-week crossover study to compare the efficacy of an acne cleanser containing 2% salicylic acid with that of a 10% benzoyl peroxide wash was conducted in 30 patients with acne vulgaris. The results demonstrated that only patients treated with the salicylic acid cleanser had a significant reduction in comedones. Patients treated with the salicylic acid cleanser for the first two weeks showed a significant improvement in acne, but worsened during benzoyl peroxide therapy over the following two weeks. In contrast, patients initially treated with the benzoyl peroxide wash for the first two weeks continued to improve with salicylic acid cleanser over the next two weeks.

Acne Vulgaris↗

[Effect of salicylic acid and finely divided sulfur on the bioavailability of corticosteroids in the skin in external therapy].

Investigation on 60 volunteers are reported in whom the influence of salicylic acid and finely divided sulfur on the blanching effect of ointments with and without steroid was analysed. The higher the concentration of salicylic acid the greater is the decrease in the blanching effect of the steroid free ointment. At low concentrations finely divided sulfur also reduces the blanching effect of the steroid is reduced by salicylic acid as well as by sulfur. This effect is at least partly produced by the decrease of the blanching effect due to the base. An increase in the bioavailability of corticosteroids in the skin after local application cannot be achieved by addition of salicylic acid or sulfur under the conditions chosen.

Adult↗

Binding of diazepam, salicylic acid and digitoxin to albumin isolated from fetal and adult serum.

Albumin was isolated from pooled fetal serum obtained at normal delivery at term and from pooled adult plasma. Albumin isolation was carried out by means of PEG precipitation followed by ion exchange chromatography on DEAE-Sephadex A 50 and then on SP-Sephadex C 50. The binding of diazepam (1 microM), salicylic acid (2 mM) and digitoxin (6 nM) to albumin (40 g/l) was measured by equilibrium dialysis at 37 degrees C. The unbound fraction (mean +/- SD) for fetal and adult albumin of diazepam was 1.86 +/- 0.24 and 1.82 +/- 0.15% (NS), that of digitoxin was 3.18 +/- 0.27 and 3.36 +/- 0.04% (NS) and that of salicylic acid was 11.65 +/- 0.99 and 9.47 +/- 0.75% (p less than 0.05), respectively. With both fetal and adult albumin, a single class of binding sites was observed for diazepam and digitoxin, whereas two classes of binding sites were observed for salicylic acid. The number of binding sites (n, moles of drug per mole of albumin) for fetal and adult albumin was 0.83 and 1.02 for diazepam and 0.014 and 0.018 for digitoxin, respectively. For salicylic acid, n was 1.45 (fetal albumin) and 1.55 (adult albumin) for the higher affinity site, and 3.06 (fetal albumin) and 3.27 (adult albumin) for the lower affinity site. The association constant (Ka, M-1) for diazepam was 1.36 x 10(5) (fetal albumin) and 1.00 x 10(5) (adult albumin) and that for digitoxin was 4.12 x 10(6) (fetal albumin) and 2.7 x 10(6) (adult albumin). For salicylic acid, Ka was 38.4 x 10(3) (fetal albumin) and 35.8 x 10(3) (adult albumin) for the higher affinity site, and 2.7 x 10(3) (fetal albumin) and 4.3 x 10(3) (adult albumin) for the lower affinity site. This work shows that fetal and adult albumin have similar binding properties and corroborates our previous findings with furosemide.

Adult↗

The safety and efficacy of salicylic acid chemical peels in darker racial-ethnic groups.

BACKGROUND: There is a dearth of published data regarding chemical peels in darker racial-ethnic groups. OBJECTIVE: The purpose of the present investigation was to assess the clinical efficacy and safety of a new superficial salicylic acid peel in individuals of skin types V and VI. METHODS: Twenty-five patients were included in this pilot investigation. Nine had acne vulgaris, 5 had post-inflammatory hyperpigmentation, 6 had melasma, and 5 had rough, oily skin with enlarged pores. The patients were pre-treated for 2 weeks with hydroquinone 4% prior to undergoing a series of five salicylic acid chemical peels. The concentrations of salicylic acid were 20% and 30%. The peels were performed at 2 week intervals. RESULTS. Moderate to significant improvement was observed in 88% of the patients. Minimal to mild side effects occurred in 16%. CONCLUSION: The results of this study suggest that superficial salicylic acid peels are both safe and efficacious for treatment of acne vulgaris, oily skin, textural changes, melasma, and post-inflammatory hyperpigmentation in patients with skin types V and VI.

Acne Vulgaris↗

Inhibition of phenolsulphotransferase by salicylic acid: a possible mechanism by which aspirin may reduce carcinogenesis.

BACKGROUND: Recent epidemiological evidence has shown that chronic use of aspirin decreases susceptibility to bowel cancer. Animal studies have shown that sulphotransferase inhibitors coadministered with sulphation activated carcinogens dramatically reduce the incidence of cancer. AIMS: To investigate the effect of the main aspirin breakdown product, salicylic acid, on the P and M isoforms of phenolsulphotransferase from human platelets and colonic mucosa. METHODS: Platelets were obtained from healthy blood donors and isolated within 24 hours after donation. Samples of colonic mucosa were obtained at resection for non-malignant disease. Phenolsulphotransferase activity was measured in cellular homogenates using a standard radiolabelling assay. RESULTS: Salicylic acid consistently and selectively inhibited the P form of phenolsulphotransferase at subtherapeutic concentrations in both tissue samples. A 50% inhibition of sulphation by the P phenolsulphotransferase occurred at salicylic acid concentrations of about 40 and 130 microM in platelets and bowel mucosa respectively. M phenolsulphotransferase was virtually unaffected by salicylic acid up to a concentration of 1.5 mM (the therapeutic plasma concentration for salicylates when treating rheumatoid arthritis is about 1-2 mM). CONCLUSION: The action of salicylic acid on P phenolsulphotransferase, by preventing the excessive activation of carcinogens, is a possible additional pathway by which aspirin can reduce cancer risk.

Aged↗

Determination of free salicylic acid in chewing aspirin tablets by HPLC.

OBJECTIVE: To establish a HPLC method for determining the content of free salicylic acid in chewing aspirin tablets. METHOD: The determination was conducted on a HPLC column (C(18), 150 mm x 4.6 mm x 5 microm) with methanol-water-glacial acetic acid (8.0 5.5 1.0) as the mobile phase and the detection wavelength of 302 nm. RESULTS: The calibration curve was linear within the concentration range of 2.65 to 31.77 microg/ml (r=0.999 97) of salicylic acid. The average recovery rate was 100.21% with relative standard deviation of 0.53% (n=6). CONCLUSION: HPLC is quick and accurate of determining the content of free salicylic acid for chewing aspirin tablets.

Aspirin↗

Effect of salicylic acid on protein composition of Tatar buckwheat Fagopyrum tataricum calluses with different ability for morphogenesis.

The effect of salicylic acid on the content of soluble proteins and individual polypeptides in Tatar buckwheat Fagopyrum tataricum calluses differing in ability for morphogenesis was studied. Changes in the protein composition of the calluses cultivated in the dark and in the light indicated the higher sensitivity of the non-morphogenic callus. Different response of callus cultures to salicylic acid and conditions of cultivation (light, darkness) is suggested to be associated with the antioxidant defense system, which is, in particular, characterized by the hydrogen peroxide content in the calluses. Salicylic acid increased the H2O2 content in non-morphogenic calluses more strongly than in morphogenic calluses, and the difference was more significant for the calluses cultivated in the light.

Darkness↗

Hepatic structure-pharmacokinetic relationships: the hepatic disposition and metabolite kinetics of a homologous series of O-acyl derivatives of salicylic acid.

1. The hepatic disposition and metabolite kinetics of a homologous series of O-acyl (acetyl, propionyl, butanoyl, pentanoyl, hexanoyl and octanoyl) esters of salicylic acid (C2SA, C3SA, C4SA, C5SA, C6SA and C8SA, respectively) was determined using a single-pass, in-situ rat liver preparation. 2. The hepatic venous outflow profiles for the parent esters and the generated metabolite, salicylic acid (SA) were analysed by HPLC. Non-parametric moments analysis was used to determine the area under the curve (AUC'), mean transit time (MTT) and normalized variance (CV2) for the parent esters and generated SA. 3. Pregenerated SA ([14C]-salicylic acid) was injected into each liver with the parent ester to determine its distribution characteristics. 4. The overall recovery of ester plus metabolite was 89% of the ester dose injected and independent of the ester carbon number, suggesting that ester extraction was due to hepatic metabolism to salicylic acid. 5. The metabolite AUC' value increased directly with the lipophilicity of the parent ester (from 0.12 for C2SA to 0.95 for C8SA). By contrast, the parent AUC' decreased with the lipophilicity (from 0.85 for C2SA to zero for C8SA). The metabolite MTT value also showed a trend to increase with the lipophilicity of the parent ester (from 15.72 s for C3SA to 61.97 s for C8SA). However, the parent MTT value shows no significant change across the series. 6. The two-compartment dispersion model was used to derive the kinetic parameters for parent ester, pregenerated SA and generated SA. Consequently, these parameters were used to estimate the values of AUC', MTT and CV2 for the parent ester and metabolite. The moments values obtained using the two-compartment dispersion model show similar trends to the corresponding moments values obtained from the outflow profiles using a non-parametric approach. 7. The more lipophilic aspirin analogues are more confined to the portal circulation after oral administration than aspirin due to their more extensive hepatic elimination avoiding systemic prostacyclin inhibition. Given that aspirin's selectivity as an anti-thrombotic agent has been postulated to be due to selective anti-platelet effects in the portal circulation, the more lipophilic and highly extracted analogues are potentially more selective anti-thrombotic agents than aspirin.

Animals↗

Nonliner tissue disposition: salicylic acid in rat brain.

A model was developed to detect nonlinear disposition of a drug in a tissue. The model was experimentally tested relating to salicylic acid disposition in the brain. Experimental data obtained in rats are reported for doses of 25 and 40 mg/kg ip. The parameters measured for each dose were the ratio of the area under the brain concentration-time curve to the area under the plasma concentration-time curve and the ratio of the maximum brain concentration of salicylic acid to the plasma concentration at that point in time. The ratios increased with dose; furthermore, ratios calculated using plasma concentrations corrected for plasma protein binding were dose dependent. Calculations performed on literature data for salicylic acid disposition in mouse brain corroborated the results of this sutdy. The existence of a saturable transport system for the elimination of salicylic acid from the brain is supported by the data presented. The rationale necessary to apply the model to any tissue is discussed.

Animals↗