Abstract：
:A series of anti-inflammatory derivatives containing an N-acyl hydrazone subunit (4a-e) were synthesized and characterized. Docking studies were performed that suggest that compounds 4a-e bind to cyclooxygenase (COX)-1 and COX-2 isoforms, but with higher affinity for COX-2. The compounds display similar anti-inflammatory activities in vivo, although compound 4c is the most effective compound for inhibiting rat paw edema, with a reduction in the extent of inflammation of 35.9% and 52.8% at 2 and 4 h, respectively. The anti-inflammatory activity of N-acyl hydrazone derivatives was inferior to their respective parent drugs, except for compound 4c after 5 h. Ulcerogenic studies revealed that compounds 4a-e are less gastrotoxic than the respective parent drug. Compounds 4b-e demonstrated mucosal damage comparable to celecoxib. The in vivo analgesic activities of the compounds are higher than the respective parent drug for compounds 4a-b and 4d-e. Compound 4a was more active than dipyrone in reducing acetic-acid-induced abdominal constrictions. Our results indicate that compounds 4a-e are anti-inflammatory and analgesic compounds with reduced gastrotoxicity compared to their respective parent non-steroidal anti-inflammatory drugs.
journal_name
Int J Mol Scijournal_title
International journal of molecular sciencesauthors
de Melo TR,Chelucci RC,Pires ME,Dutra LA,Barbieri KP,Bosquesi PL,Trossini GH,Chung MC,dos Santos JLdoi
10.3390/ijms15045821subject
Has Abstractpub_date
2014-04-04 00:00:00pages
5821-37issue
4issn
1422-0067pii
ijms15045821journal_volume
15pub_type
杂志文章abstract：:Pinellia ternata is an important traditional Chinese medicinal plant. The growth of P. ternata is sensitive to high temperatures. To gain a better understanding of heat stress responses in P. ternata, we performed a comparative proteomic analysis. P. ternata seedlings were subjected to a temperature of 38 °C and sampl...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms141020614
更新日期：2013-10-15 00:00:00
abstract：:The rapid rise of obesity during the past decades has coincided with a profound shift of our living environment, including unhealthy dietary patterns, a sedentary lifestyle, and physical inactivity. Genetic predisposition to obesity may have interacted with such an obesogenic environment in determining the obesity epi...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms18040787
更新日期：2017-04-07 00:00:00
abstract：:Neuroblastoma is the most common extracranial solid tumor in childhood. The different treatments available for neuroblastoma are challenged by high rates of resistance, recurrence, and progression, most notably in advanced cases and highly malignant tumors. Therefore, the development of more targeted therapies, which ...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21186792
更新日期：2020-09-16 00:00:00
abstract：:Hepatocellular carcinoma (HCC) is a deadly form of liver malignancy with limited treatment options. Amplification and/or overexpression of c-MYC is one of the most frequent genetic events in human HCC. The mammalian target of Rapamycin Complex 1 (mTORC1) is a major functional axis regulating various aspects of cellula...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21228467
更新日期：2020-11-11 00:00:00
abstract：:An increase in intracellular Ca2+ concentration ([Ca2+]i) plays a key role in controlling endothelial functions; however, it is still unclear whether endothelial Ca2+ handling is altered by type 2 diabetes mellitus, which results in severe endothelial dysfunction. Herein, we analyzed for the first time the Ca2+ respon...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21010250
更新日期：2019-12-30 00:00:00
abstract：:Mitochondrial transplantation therapy is an innovative strategy for the treatment of mitochondrial dysfunction. The approach has been reported to be useful in the treatment of cardiac ischemic reperfusion injuries in human clinical trials and has also been shown to be useful in animal studies as a method for treating ...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms21176365
更新日期：2020-09-02 00:00:00
abstract：:The concept of "Sweet Immunity" postulates that sugar metabolism and signaling influence plant immune networks. In this study, we tested the potential of commercially available inulin-type fructans to limit disease symptoms caused by Botrytis cinerea in lettuce. Spraying mature lettuce leaves, with inulin-type fructan...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20051052
更新日期：2019-02-28 00:00:00
abstract：:Epithelia act as a barrier to the external environment. The extracellular environment constantly changes, and the epithelia are required to regulate their function in accordance with the changes in the environment. It has been reported that a difference of the environment between the apical and basal sides of epitheli...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms20143513
更新日期：2019-07-17 00:00:00
abstract：:We have generated the transgenic Tabaco plants expressing multiple monoclonal antibody (mAb) CO7-1A × BR55 by cross-pollinating with mAb CO17-1A and mAb BR55. We have demonstrated the anti-cancer effect of plant-derived multiple mAb CO17-1A × BR55. We find that co-treatment of colorectal mAbs (anti-epithelial cellular...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms151121105
更新日期：2014-11-14 00:00:00
abstract：:We previously reported that AR phosphorylation at serine 213 was associated with poor outcome and may contribute to prostate cancer development and progression. This study investigates if specific AR phosphorylation sites have differing roles in the progression of hormone naïve prostate cancer (HNPC) to castrate resis...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms140816656
更新日期：2013-08-13 00:00:00
abstract：:Chlorogenic acid (CGA) decreases colon cancer-cell proliferation but the combined anti-cancer effects of CGA with its major colonic microbial metabolites, caffeic acid (CA), 3-phenylpropionic acid (3-PPA) and benzoic acid (BA), needs elucidation as they occur together in colonic digesta. Caco-2 cancer cells were treat...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms19030723
更新日期：2018-03-03 00:00:00
abstract：:People with Alzheimer's disease (AD) have significantly higher rates of subclinical and overt epileptiform activity. In animal models, oligomeric Aβ amyloid is able to induce neuronal hyperexcitability even in the early phases of the disease. Such aberrant activity subsequently leads to downstream accumulation of toxi...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms21239318
更新日期：2020-12-07 00:00:00
abstract：:Ordered mesoporous silica (OMS) is a very interesting nanostructured material for the design and engineering of new target and controlled drug-delivery systems. Particularly relevant is the interaction between OMS and proteins. Large pores (6–9 nm) micrometric particles can be used for the realization of a drug depot ...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms19071991
更新日期：2018-07-08 00:00:00
abstract：:This study investigated the interaction between eupatorin and bovine serum albumin (BSA) using ultraviolet-visible (UV-vis) absorption, fluorescence, synchronous fluorescence, circular dichroism (CD) spectroscopies, and molecular modeling at pH 7.4. Results of UV-vis and fluorescence spectroscopies illustrated that BS...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms140714185
更新日期：2013-07-09 00:00:00
abstract：:Before utilization in biomedical diagnosis, therapeutic treatment, and biotechnology, the diverse variety of peptides and proteins must be preliminarily purified and thoroughly characterized. The recombinant DNA technology and heterologous protein expression have helped simplify the isolation of targeted polypeptides ...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms21030928
更新日期：2020-01-31 00:00:00
abstract：:NLRP3 (NOD-like receptor family, pyrin domain-containing protein 3) activation has been linked to several chronic pathologies, including atherosclerosis, type-II diabetes, fibrosis, rheumatoid arthritis, and Alzheimer's disease. Therefore, NLRP3 represents an appealing target for the development of innovative therapeu...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20204974
更新日期：2019-10-09 00:00:00
abstract：:Resistance to conventional chemotherapeutic agents, a typical feature of cholangiocarcinoma, prevents the efficacy of the therapeutic arsenal usually used to combat malignancy in humans. Mechanisms of chemoresistance by neoplastic cholangiocytes include evasion of drug-induced apoptosis mediated by autocrine and parac...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms18010149
更新日期：2017-01-13 00:00:00
abstract：:The aim of this study is to elucidate the detailed mechanism of endoplasmic reticulum (ER) stress-induced auditory cell death based on the function of the initiator caspases and molecular complex of necroptosis. Here, we demonstrated that ER stress initiates not only caspase-9-dependent intrinsic apoptosis along with ...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20235896
更新日期：2019-11-24 00:00:00
abstract：:Recessively-inherited NR2E3 gene mutations cause an unusual retinopathy with abnormally-increased short-wavelength sensitive cone (S-cone) function, in addition to reduced rod and long/middle-wavelength sensitive cone (L/M-cone) function. Progress toward clinical trials to treat patients with this otherwise incurable ...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20102497
更新日期：2019-05-21 00:00:00
abstract：:Lattice degeneration involves thinning of the retina that occurs over time. Here we performed an immunohistological study of tissue sections of human peripheral retinal lattice degeneration to investigate if retinal pigment epithelium (RPE) cells are involved in the pathogenesis of this condition. In two cases of reti...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21197347
更新日期：2020-10-05 00:00:00
abstract：:Due to the addressability and programmability, DNA has been applied not merely in constructing static elegant nanostructures such as two dimensional and three dimensional DNA nanostructures but also in designing dynamic nanodevices. Moreover, DNA could combine with hydrophobic organic molecules to be a new amphiphilic...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms19082283
更新日期：2018-08-03 00:00:00
abstract：:The common mutation BRAFV600 in primary melanomas activates the mitogen-activated protein kinase/extracellular-signal-regulated kinase (MAPK/ERK) pathway and the introduction of proto-oncogene B-Raf (BRAF) and mitogen-activated protein kinase kinase (MEK) inhibitors (BRAFi and MEKi) was a breakthrough in the treatment...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms21134576
更新日期：2020-06-27 00:00:00
abstract：:Spinal sarcopenia is a complex and multifactorial disorder associated with a loss of strength, increased frailty, and increased risks of fractures and falls. In addition, spinal sarcopenia has been associated with lumbar spine disorders and osteoporosis, which renders making decisions on treatment modalities difficult...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms21083010
更新日期：2020-04-24 00:00:00
abstract：:MicroRNAs (miRNAs) play important roles in the progression of human cancer. Although previous reports have shown that miR-145-5p is down-regulated in esophageal squamous cell carcinoma (ESCC), the roles and mechanisms of down-regulation of miR-145-5p in ESCC are still largely unknown. Using microRNA microarray and Gen...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms18091833
更新日期：2017-08-23 00:00:00
abstract：:Plants infected with DNA viruses produce massive quantities of virus-derived, 24-nucleotide short interfering RNAs (siRNAs), which can potentially direct viral DNA methylation and transcriptional silencing. However, growing evidence indicates that the circular double-stranded DNA accumulating in the nucleus for Pol II...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms140815233
更新日期：2013-07-24 00:00:00
abstract：:Understanding the role of substituents is of great importance for the preparation of novel phenolic compounds with enhanced antioxidative properties. In this work, the antioxidative activity of isoflavonoid derivatives with different substituents placed at the C2 position was determined by density functional theory (D...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20020397
更新日期：2019-01-18 00:00:00
abstract：:We have previously shown that ritonavir (RTV), a highly active anti-retroviral therapy (HAART) drug, can cause endothelial dysfunction through oxidative stress. Several antioxidants including ginsenoside Rb1, a compound with antioxidant effect, can effectively block this side effect of RTV in endothelial cells. In the...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20020294
更新日期：2019-01-12 00:00:00
abstract：:Perillafrutescen is used as traditional food and medicine in East Asia. Its seeds contain high levels of α-linolenic acid (ALA), which is important for health, but is scarce in our daily meals. Previous reports on RNA-seq of perilla seed had identified fatty acid (FA) and triacylglycerol (TAG) synthesis genes, but the...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms18112433
更新日期：2017-11-16 00:00:00
abstract：:Ischemic stroke is a leading cause of human death in present times. Two phases of pathological impact occur during an ischemic stroke, namely, ischemia and reperfusion. Both periods include individual characteristic effects on cell injury and apoptosis. Moreover, these conditions can cause severe cell defects and harm...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20246168
更新日期：2019-12-06 00:00:00
abstract：:The high abundance of mitochondria and the expression of mitochondrial uncoupling protein 1 (UCP1) confer upon brown adipose tissue (BAT) the unique capacity to convert chemical energy into heat at the expense of ATP synthesis. It was long believed that BAT is present only in infants, and so, it was not considered as ...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20143520
更新日期：2019-07-18 00:00:00
