|溶解性||Soluble in water (1.8 g/L),|
|产品介绍||Salicylic acid is a natural product extract from Willow bark, well known as an antiinflammatory and antinociceptive agent and a close structural relative to acetylsalicylic acid (aspirin). Salicylic acid is a ubiquitous plant hormone with many regulatory functions involved in local disease resistance mechanisms and systemic acquired resistance. The antiinflammatory and antinociceptive effects produced by Salicylic acid and its derivatives in animals are due to inhibition of COX-1 and COX-2 (cyclooxygenase) enzyme activity and suppression of prostaglandin biosynthesis. Salicylic acid is also of interest as a starting material for the organic synthesis of more elaborate COX suppressors and other chemical structures.|
|别名||柳酸; 沙利西酸; 撒酸; 邻羟基苯甲酸; 2-羟基苯甲酸;2-Hydroxybenzoic acid; Bis(2-hydroxyethyl)iminotris(hydroxymethyl)methane|
A neural model based on a numerical molecular representation using CODES program to predict oral absorption of any structure is described. This model predicts both high and low-absorbed compounds with...Read More
Fragment-based lead design (FBLD) has been used to identify new metal-binding groups for metalloenzyme inhibitors. When screened at 1 mM, a chelator fragment library (CFL-1.1) of 96 compounds produced...Read More
Transdermal penetration was studied as a function of selected descriptors in QSPR using CART, boosted CART and MLR models....Read More
Carbonic anhydrase inhibitors: Inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid
Inhibition of 12 mammalian isoforms of the metalloenzyme carbonic anhydrase (CA, EC 184.108.40.206), CA I-XIV, with a series of phenols was investigated. The inhibition profile by phenols of these CAs was di...Read More
Carbonic anhydrase inhibitors (CAIs) are a class of pharmaceuticals used as antiglaucoma agents, diuretics, antiepileptics, in the management of mountain sickness, gastric and duodenal ulcers, neurolo...Read More
Benzenepolycarboxylic acids with potential anti-hemorrhagic properties and structure-activity relationships.
Previously, we reported the structural requirements of the cinnamic acid relatives for inhibition of snake venom hemorrhagic action. In the present study, we examined the effect of benzenepolycarboxyl...Read More
Tolerance and efficacy of a product containing ellagic and salicylic acids in reducing hyperpigmentation and dark spots in comparison with 4% hydroquinone.
Hydroquinone (HQ) is the benchmark prescription agent for skin lightening. However, HQ use is recently banned in Europe and in parts of Asia because of potential long-term consequences, including carc...Read More
Synthesis and anti-inflammatory activity of 3-(4'-geranyloxy-3'-methoxyphenyl)-2-trans propenoic acid and its ester derivatives
The synthesis of ester derivatives of the title acid and their anti-inflammatory activity are reported....Read More
Solubility plays a very important role in the selection of compounds for drug screening. In this context, a QSAR model was developed for predicting water solubility of drug-like compounds. First, a se...Read More
Involvement of lectin in the salicylic acid-induced wheat tolerance to cadmium and the role of endogenous ABA in the regulation of its level.
To investigate PAMPA permeability of hydrophobic compounds, we experimentally measured the P"a"p"p"-"p"a"m"p"a of compounds with high hydrophobicity, inclu...Read More
An early response to environmental stress involves regulation of OmpX and OmpF, two enterobacterial outer membrane pore-forming proteins.
Bacterial adaptation to external stresses and toxic compounds is a key step in the emergence of multidrug-resistant strains that are a serious threat to human health. Although some of the proteins and...Read More
Structure-activity relationship of salicylic acid derivatives on inhibition of TNF-α dependent NFκB activity: Implication on anti-inflammatory effect of N-(5-chlorosalicyloyl)phenethylamine against experimental colitis.
To develop a more potent NFκB inhibitor from salicylic acid which is known to inhibit activity of NFκB, a transcription factor regulating genes involved in immunity, inflammation and tumorigenesis, ...Read More
Inhibition of 15-lipoxygenase-catalysed oxygenation of arachidonic acid by substituted benzoic acids
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data
We developed an improved Lombardeo's method (J. Med. Chem., 2004) for prediction of VD"s"s in human. With ElogD substituted by logk"I"A"M, together with f"i" ...Read More
GH3 expression and IAA-amide synthetase activity in pea (Pisum sativum L.) seedlings are regulated by light, plant hormones and auxinic herbicides.
The formation of auxin conjugates is one of the important regulatory mechanisms for modulating IAA action. Several auxin-responsive GH3 genes encode IAA-amide synthetases that are involved in the main...Read More
Solubility and solid-state characteristics were determined and multivariate data analysis was used to deduce structural features important for solid-state limited solubility of marketed drugs. Molecul...Read More
Computational modeling continues to play an important role in novel therapeutics discovery and development. In this study, we have investigated the use of in silico approaches to develop inhibitors of...Read More
GC-MS determination of flavonoids and phenolic and benzoic acids in human plasma after consumption of cranberry juice.
A GC-MS method was developed for the determination of various flavonoids and phenolic and benzoic acids in human plasma. The procedure involved the extraction of flavonoids and phenolic and benzoic ac...Read More
Air to lung partition coefficients for volatile organic compounds and blood to lung partition coefficients for volatile organic compounds and drugs
Values of in vitro gas to lung partition coefficients, K"l"u"n"g, of VOCs have been collected from the literature. For 44 VOCs, application of the Abraham solvation equation to log...Read More
Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies
In the light of known HDAC inhibitors, 33 carboxylic acid derivatives were tested to understand the structural requirements for HDAC inhibition activity. Several modifications were applied to develop ...Read More
Parallel artificial membrane permeability assay: a new membrane for the fast prediction of passive human skin permeability.
This work was devoted to the search for new artificial membranes allowing a rapid evaluation of passive human skin permeation of compounds with a parallel artificial membrane permeability assay (PAMPA...Read More
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental...Read More
Surfactants, aromatic and isoprenoid compounds, and fatty acid biosynthesis inhibitors suppress Staphylococcus aureus production of toxic shock syndrome toxin 1.
Menstrual toxic shock syndrome is a rare but potentially life-threatening illness manifest through the actions of Staphylococcus aureus toxic shock syndrome toxin 1 (TSST-1). Previous studies have sho...Read More
Detection of autosomal dominant polycystic kidney disease by NMR spectroscopic fingerprinting of urine.
Autosomal dominant polycystic kidney disease (ADPKD) is a frequent cause of kidney failure; however, urinary biomarkers for the disease are lacking. In a step towards identifying such markers, we used...Read More
Structural variation governs substrate specificity for organic anion transporter (OAT) homologs. Potential remote sensing by OAT family members.
Organic anion transporters (OATs, SLC22) interact with a remarkably diverse array of endogenous and exogenous organic anions. However, little is known about the structural features that determine thei...Read More
GbWRKY1, a novel cotton (Gossypium barbadense) WRKY gene isolated from a bacteriophage full-length cDNA library, is induced by infection with Verticillium dahliae.
WRKY transcription factor proteins play important roles in diverse stress responses. In this study, we first cloned a novel WRKY from our constructed bacteriophage full-length cDNA library for cotton ...Read More
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
New experimental methodologies were applied to measure the unbound brain-to-plasma concentration ratio (K(p,uu,brain)) and the unbound CSF-to-plasma concentration ratio (K(p,uu,CSF)) in rats for 43 st...Read More
A chemical screening approach reveals that indole fluorescence is quenched by pre-fibrillar but not fibrillar amyloid-beta.
Aggregated amyloid-beta (Abeta) peptide is implicated in the pathology of Alzheimer's disease. In vitro and in vivo, these aggregates are found in a variety of morphologies, including globular ol...Read More
3D-QSAR and molecular docking studies of benzaldehyde thiosemicarbazone, benzaldehyde, benzoic acid, and their derivatives as phenoloxidase inhibitors
Inhibitions of three classes compounds against phenoloxidase were investigated, and 3D-QSAR was performed. The interactions between compounds N18 and phenoloxidase active site were also studied using ...Read More
Response to metal stress of Nicotiana langsdorffii plants wild-type and transgenic for the rat glucocorticoid receptor gene.
Recently our findings have shown that the integration of the gene coding for the rat gluco-corticoid receptor (GR receptor) in Nicotiana langsdorffii plants induced morphophysiological effects in tran...Read More
Programmed cell death (PCD) is a crucial process for plant innate immunity and development. In plant innate immunity, PCD is believed to prevent the spread of pathogens from the infection site. Althou...Read More
A novel class of 2-(R)-phenylpropionamides has been recently reported to inhibit in vitro and in vivo interleukin-8 (CXCL8)-induced biological activities. These CXCL8 inhibitors are derivatives of phe...Read More
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions
The displacement of probes that bind selectively to subdomains IIA or IIIA on human serum albumin (HSA) by competing compounds has been followed using fluorescence spectroscopy, and has therefore been...Read More
Yeast cells can extrude intracellular drugs through membrane-associated efflux pumps, such as ATP-binding cassette (ABC) transporters and members of the major facilitator superfamily. Gene expression ...Read More
To determine the chemical constituents of Gentiana rhodantha.To isolate the constituents, column chromatography over silica gel, MCI, Sephadex LH-20 and C18 reverse-phased silica gel were used. Spectr...Read More
Searching for new NO-donor aspirin-like molecules: a new class of nitrooxy-acyl derivatives of salicylic acid.
A new class of products in which the phenol group of salicylic acid is linked to alkanoyl moieties bearing nitrooxy functions has been synthesized and studied for their polyvalent actions. The product...Read More
Derivatives of 1,4-bis(3-hydroxycarbonyl-4-hydroxyl)styrylbenzene as PTP1B inhibitors with hypoglycemic activity
PTP1B inhibitor with hypoglycemic activity....Read More
Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrugs of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease
Colon-specific mutual azo prodrugs of 5-aminosalicylic acid with essential amino acids were synthesized for the management of inflammatory bowel disease. The structures were confirmed by elemental and...Read More
In vitro inhibition of salicylic acid derivatives on human cytosolic carbonic anhydrase isozymes I and II
[Therapy of rheumatic disease with a hydroxyethylsalicylate gel. Results of 2 clinical studies of effectiveness and bioavailability].
Two clinical studies were carried out to investigate the efficacy and safety as well as the local and systemic availability of a hydroxyethylsalicyclate gel. A double blind, multicenter trial, involvi...Read More
Reactive oxygen species promote chloroplast dysfunction and salicylic acid accumulation in fumonisin B1-induced cell death.
We report a novel regulatory mechanism by which reactive oxygen species (ROS) regulate fumonisin B1 (FB1)-induced cell death. We found that FB1 induction of light-dependent ROS production promoted the...Read More
Synthesis and biological evaluation of nitrogen-containing chalcones as possible anti-inflammatory and antioxidant agents.
A novel series of nitrogen-containing chalcones were synthesized by Mannich reaction and were screened for anti-inflammatory related activities such as inhibition of cyclooxygenase-2 (COX-2), trypsin ...Read More
Searching for new NO-donor aspirin-like molecules: Furoxanylacyl derivatives of salicylic acid and related furazans.
A new group of derivatives of salicylic acid containing NO-donor furoxans, and the related des-NO-furazans, were synthesized and evaluated as new aspirin-like molecules. Their stability was assessed i...Read More
A series of potent novel 8-hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors was identified. These compounds inhibited the strand transfer process of HIV-1 integrase and v...Read More
Viral warts are common skin lesions caused by human papilloma virus. This article describes the pathogenesis, symptoms and treatment methods of cutaneous warts. The majority resolves spontaneously and...Read More
Dehydroxymethylepoxyquinomicin (DHMEQ, 1) is a novel nuclear factor-@kB (NF-@kB) inhibitor that inhibits DNA binding of NF-@kB components including p65. To inspect its biological activity of 1, we syn...Read More
Inhibition of IKK-beta: a new development in the mechanism of the anti-obesity effects of PTP1B inhibitors SA18 and SA32.
In a previous study, protein tyrosine phosphatase 1B (PTP1B) inhibitors, SA18 and SA32, exhibited anti-obesity effects in a mouse model by suppressing weight gain and improving blood parameters, inclu...Read More
Genetic Requirements for Signaling from an Autoactive Plant NB-LRR Intracellular Innate Immune Receptor.
Plants react to pathogen attack via recognition of, and response to, pathogen-specific molecules at the cell surface and inside the cell. Pathogen effectors (virulence factors) are monitored by intrac...Read More
Synovial distribution of "systemically" administered acetylsalicylic acid in the isolated perfused equine distal limb.
This study investigated synovial concentrations of acetylsalicylic acid (ASA) and its metabolite salicylic acid (SA) in the equine fetlock joint following systemic administration of ASA. Salicylates w...Read More
Identification of promoter motifs regulating ZmeIF4E expression level involved in maize rough dwarf disease resistance in maize (Zea Mays L.).
Maize rough dwarf disease (MRDD, a viral disease) results in significant grain yield losses, while genetic basis of which is largely unknown. Based on comparative genomics, eukaryotic translation init...Read More
Co-synergism of endophyte Penicillium resedanum LK6 with salicylic acid helped Capsicum annuum in biomass recovery and osmotic stress mitigation.
Water-deficiency adversely affects crop growth by generating reactive oxygen species (ROS) at cellular level. To mitigate such stressful events, it was aimed to investigate the co-synergism of exogeno...Read More
Commentary: Salicylic Acid Peels Versus Jessner's Solution Peels for Acne Vulgaris: A Comparative Study.
Single-center, open-label study of a proprietary topical 0.5% salicylic acid-based treatment regimen containing sandalwood oil in adolescents and adults with mild to moderate acne.
A proprietary topical blend of salicylic acid and highly purified sandalwood oil from Australia was used in this open-label study in adolescents and adults with mild to moderate facial acne.The invest...Read More
Randomized, controlled, evaluator-blinded studies conducted to compare the efficacy and tolerability of 3 over-the-counter acne regimens in subjects with mild or moderate acne.
Acne vulgaris is a common dermatologic disease that most frequently affects adolescents and young adults. Over-the-counter (OTC) acne treatment regimens are increasingly being used by individuals with...Read More
Short chain fatty acids (SCFA) are absorbed by carrier mediated uptake in the small intestine by pH-dependent SCFA/HCO3 (-) exchangers on the apical membrane of epithelial cells. Conventional assumpti...Read More
Reduction in the Fitness of Bemisia tabaci Fed on Three Previously Infested Tomato Genotypes Differing in the Jasmonic Acid Pathway.
The effect of previous infestation (preconditioning) by the whitefly Bemisia tabaci (Gennadius) biotype B on the population fitness of subsequent infestations that fed on three isogenic tomato genotyp...Read More
Concentrations of carbon dioxide (CO(2)) are increasing in the atmosphere, affecting soybean (Glycine max L.) phytohormone signaling and herbivore resistance. Whether the impact of elevated CO(2) on p...Read More
The Arabidopsis Rho of plants GTPase AtROP6 functions in developmental and pathogen response pathways.
How plants coordinate developmental processes and environmental stress responses is a pressing question. Here, we show that Arabidopsis (Arabidopsis thaliana) Rho of Plants6 (AtROP6) integrates develo...Read More
Removal of cargos from the cell surface via endocytosis is an efficient mechanism to regulate activities of plasma membrane (PM)-resident proteins, such as receptors or transporters. Salicylic acid (S...Read More
The effects of host defence elicitors on betacyanin accumulation in Amaranthus mangostanus seedlings.
The effect of elicitors associated with host defence on betacyanin accumulation in Amaranthus mangostanus seedlings was investigated. Under the conditions of the experiments, betacyanin accumulation w...Read More
Anacardic acid derivatives exhibit a broad range of biological activities. In this report, an efficient method for the synthesis of anacardic acid derivatives was explored, and a small set of salicyli...Read More
Systemic acquired resistance (SAR) is an induced immune mechanism in plants. Unlike vertebrate adaptive immunity, SAR is broad spectrum, with no specificity to the initial infection. An avirulent path...Read More
Elevated early callose deposition results in complete penetration resistance to powdery mildew in Arabidopsis.
A common response by plants to fungal attack is deposition of callose, a (1,3)-β-glucan polymer, in the form of cell wall thickenings called papillae, at site of wall penetration. While it has been g...Read More
Evaluation of the efficacy, tolerability, and safety of an over-the-counter acne regimen containing benzoyl peroxide and salicylic acid in subjects with acne.
Benzoyl peroxide (BPO) is a widely used over-the-counter (OTC) topical acne treatment often used in combination with salicylic acid (SA) to achieve better comedone control than that achieved with BPO ...Read More
Photoluminescent spherical nanostructures were prepared through the self-assembly of a tyrosine-containing bolaamphiphilic molecule, and their antenna effect was examined. The photoluminescent spheric...Read More
Real-time monitoring on the adsorption process of salicylic acid onto chitosan membrane using dielectric spectroscopy: macroscale concentration polarization and dynamics.
The adsorption process of salicylic acid (SA) onto chitosan membrane is monitored in real time by the dielectric relaxation spectroscopy (DRS) method. A unique dielectric relaxation, which is related ...Read More
Determination of salicylate in blood serum by flow injection with immobilized salicylate hydroxylase.
A flow injection (FI) enzymatic system, based on the use of immobilized salicylate hydroxylase in glass beads, was developed for the determination of salicylate. Salicylate hydroxylase and nicotinamid...Read More
[Salicylism and glaucoma: reciprocal augmentation of the toxicity of acetazolamide and acetylsalicylic acid].
We report a case of salicylism caused by association of acetylsalicylic acid (ASA) and acetazolamide. A 50-year-old woman without chronic renal insufficiency, was admitted for confusion, cerebellar at...Read More
The potential of transdermal iontophoresis to facilitate drug delivery was evaluated by studying the transport kinetics of model compounds salicylate (anion), phenylethylamine (cation), mannitol (pola...Read More
1. Five rheumatoid patients with a knee joint effusion participated in the study. An aqueous solution (0.1 to 0.2 ml) containing paracetamol, salicylate, diclofenac and [125I]-albumin was injected int...Read More
Pharmacokinetic investigations with direct injection of plasma samples: possible savings using capillary electrophoresis (CE).
Capillary electrophoresis (CE) is often regarded as a separation technique of choice because of its high selectivity and its cost advantages compared to LC.RSD% of 0.5% have become standard for qualit...Read More
The aim of this study was to evaluate, in young volunteer subjects, the effects of salicylates on evoked otoacoustic emissions (EOAEs), which presumably reflect an active mechanical process in the coc...Read More
Microdialysis vs. suction blister technique for in vivo sampling of pharmacokinetics in the human dermis.
Our aim was to simultaneously investigate 2 techniques for in vivo sampling of peripheral compartment pharmacokinetics after systemic administration of acetylsalicylic acid. Ten volunteers were given ...Read More
[Identification and quantification of exogenous metabolites in biological liquids with new development in NMR spectroscopy in one and two dimensions].
By comparison of urine 1H NMR spectrum from a healthy person with those from poisoned patient, we have displayed one or several signals related to intoxication. In complement, various 1H and 13C NMR s...Read More
Determination of salicylate, gentisic acid and salicyluric acid in human urine by capillary electrophoresis with laser-induced fluorescence detection.
Acetylsalicylic acid (Aspirin) is rapidly metabolized to salicylic acid (salicylate) and other compounds, including gentisic acid and salicyluric acid. Monitoring of salicylate and its metabolites is ...Read More
The histamine concentration was measured from suction blister fluid obtained from normal and lesional skin of 8 patients with fixed drug eruption (FDE) caused by phenazone salicylate and from that of ...Read More
A sequential approach is presented to the problem of determining the minimum number of blood samples needed to calculate the plasma to saliva concentration ratio to a required precision. The method wa...Read More
Earlier studies have shown that drugs such as dilantin inhibit T4 binding by thyroid hormone binding globulin (TBG) and cause a displacement of T4 from TBG to prealbumin with no change in the albumin-...Read More
Previous studies by us suggested that luminally administered sodium salicylate blocks dihydroxy-bile acid-induced colonic secretion in the rat. In the present study, an in vivo rat cecal loop techniqu...Read More
Quantitative assessment of seminal vesicle and prostate drug concentrations by use of a noninvasive method
Background: The male genital tract is a complex collection of anatomically and biochemically distinct compartments that contribute to the ejaculate. Understanding the pharmacokinetics in these compart...Read More
Many non-steroidal anti-inflammatory drugs (NSAIDs) (including sulphasalazine, sulindac, indomethacin, naproxen, salicylic acid, ibuprofen, piroxicam and mefenamic acid) were found to be competitive i...Read More
Comparison of human skin or epidermis models with human and animal skin in in-vitro percutaneous absorption.
For the study of in-vitro skin penetration of candidate drugs, excised animal skin is frequently used as a replacement for human skin. Reconstructed human skin or epidermis equivalents have been propo...Read More
Cyclotides are small cysteine-rich plant peptides similar in size and processing to the defensins. Long-term growth of the Rubiaceae family plant Oldenlandia affinis under different conditions reveals...Read More