Abstract：
:Estrogen-receptor-mediated signaling has been suggested to decrease the inflammatory response in monocyte macrophages. Previously, we showed that a novel selective estrogen receptor modulator (SERM2) promotes anti-inflammatory phenotype of monocytes in vitro. In this study, we demonstrate the potential of SERM2 in amelioration of colitis. We utilized a dextran sodium sulfate (DSS)-induced colitis model in FVB/n mice to demonstrate the effects of orally administered SERM2 on the clinical status of the mice and the histopathological changes in the colon, as well as proportion of Mrc-1 positive macrophages. SERM2 nuclear receptor affinities were measured by radioligand binding assays. Orally administered, this compound significantly alleviated DSS-induced colitis in male mice and induced local estrogen receptor activation in the inflamed colon, as well as promoting anti-inflammatory cytokine expression and infiltration of anti-inflammatory monocytes. We show that this novel drug candidate has an affinity to estrogen receptors α and β and progesterone receptors, but not to glucocorticoid receptor, thus expressing unique binding properties compared to other sex steroid receptor ligands. These results indicate that novel drug candidates to alleviate inflammatory conditions of the colon could be found among sex steroid receptor activating compounds.
journal_name
Int J Mol Scijournal_title
International journal of molecular sciencesauthors
Polari L,Anttila S,Helenius T,Wiklund A,Linnanen T,Toivola DM,Määttä Jdoi
10.3390/ijms20123007subject
Has Abstractpub_date
2019-06-20 00:00:00issue
12issn
1422-0067pii
ijms20123007journal_volume
20pub_type
杂志文章abstract：:Alzheimer's disease (AD) is the leading cause of dementia worldwide. It involves progressive impairment of cognitive function. A growing number of neuroprotective compounds have been identified with potential anti-AD properties through in vitro and in vivo models of AD. Quercetin, a natural flavonoid contained in a wi...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21020493
更新日期：2020-01-13 00:00:00
abstract：:This study was aimed to clarify the effect of honokiol (Hon) on the activity of Cytochrome P450 (CYP450) enzymes, and the level of mRNA expression of liver and kidney transporters in type 2 diabetic rats induced by high-fat diet and strepotozotocin. Rats were randomly divided into normal control (NC) group, diabetic c...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms19030815
更新日期：2018-03-12 00:00:00
abstract：:Therapeutic drug monitoring is routinely performed to maintain optimal tacrolimus concentrations in kidney transplant recipients. Nonetheless, toxicity and rejection still occur within an acceptable concentration-range. To have a better understanding of the relationship between tacrolimus dose, tacrolimus concentratio...
journal_title：International journal of molecular sciences
pub_type： 临床试验,杂志文章
doi：10.3390/ijms20194710
更新日期：2019-09-23 00:00:00
abstract：:Brassica campestris L., a hyperaccumulator of cadmium (Cd), is considered a candidate plant for efficient phytoremediation. The hairy roots of Brassica campestris L are chosen here as a model plant system to investigate the response mechanism of Brassica campestris L. to Cd stress. High-throughput sequencing technolog...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21010180
更新日期：2019-12-26 00:00:00
abstract：:Emodin, an active constituent of oriental herbs, is widely used to treat allergy, inflammation, and other symptoms. This study provides the scientific basis for the anti-inflammasome effects of emodin on both in vitro and in vivo experimental models. Bone marrow-derived macrophages were used to study the effects of em...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms16048102
更新日期：2015-04-10 00:00:00
abstract：:The abnormal deposition of calcium within renal parenchyma, termed nephrocalcinosis, frequently occurs as a result of impaired renal calcium handling. It is closely associated with renal stone formation (nephrolithiasis) as elevated urinary calcium levels (hypercalciuria) are a key common pathological feature underlyi...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms21010369
更新日期：2020-01-06 00:00:00
abstract：:An imbalance of excitatory and inhibitory neurotransmission leading to over excitation plays a crucial role in generating seizures, while enhancing GABAergic mechanisms are critical in terminating seizures. In recent years, it has been reported in many studies that astrocytes are deeply involved in synaptic transmissi...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms20122964
更新日期：2019-06-18 00:00:00
abstract：:The first algorithm for Emulsion Stability Simulations (ESS) was presented at the V Conferencia Iberoamericana sobre Equilibrio de Fases y Diseño de Procesos [Luis, J.; García-Sucre, M.; Urbina-Villalba, G. Brownian Dynamics Simulation of Emulsion Stability In: Equifase 99. Libro de Actas, 1(st) Ed., Tojo J., Arce, A....
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms10030761
更新日期：2009-03-01 00:00:00
abstract：:The growth and vascularization of prostate cancer is dependent on interactions between cancer cells and supporting stromal cells. The primary stromal cell type found in prostate tumors is the carcinoma-associated fibroblast, which produces placental growth factor (PlGF). PlGF is a member of the vascular endothelial gr...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms140917958
更新日期：2013-09-03 00:00:00
abstract：:T cells are essential mediators of the adaptive immune system, which constantly patrol the body in search for invading pathogens. During an infection, T cells that recognise the pathogen are recruited, expand and differentiate into subtypes tailored to the infection. In addition, they differentiate into subsets requir...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms21082674
更新日期：2020-04-11 00:00:00
abstract：:Meniscal injuries, particularly in the avascular zone, have a low propensity for healing and are associated with the development of osteoarthritis. Current meniscal repair techniques are limited to specific tear types and have significant risk for failure. In previous work, we demonstrated the ability of meniscus-deri...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21010044
更新日期：2019-12-19 00:00:00
abstract：:Adsorption of precious metals in acidic aqueous solutions using thiourea modified magnetic magnetite nanoparticle (MNP-Tu) was examined. The MNP-Tu was synthesized, characterized and examined as a reusable adsorbent for the recovery of precious metals. The adsorption kinetics were well fitted with pseudo second-order e...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms14059834
更新日期：2013-05-08 00:00:00
abstract：:Many systems, including polymers and molecular liquids, when adequately cooled and/or compressed, solidify into a disordered solid, i.e., a glass. The transition is not abrupt, featuring progressive decrease of the microscopic mobility and huge slowing down of the relaxation. A distinctive aspect of glass-forming mate...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms20225708
更新日期：2019-11-14 00:00:00
abstract：:Cardiovascular diseases (CVDs) are the leading causes of death worldwide. CVD pathophysiology is often characterized by increased stiffening of the heart muscle due to fibrosis, thus resulting in diminished cardiac function. Fibrosis can be caused by increased oxidative stress and inflammation, which is strongly linke...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms21165913
更新日期：2020-08-18 00:00:00
abstract：:Inositol hexaphosphate (IP6), or phytic acid is a natural dietary ingredient and has been described as a "natural cancer fighter", being an essential component of nutritional diets. The marked anti-cancer effect of IP6 has resulted in our quest for an understanding of its mechanism of action. In particular, our data p...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms141223545
更新日期：2013-12-02 00:00:00
abstract：:Evaluation of relationships between molecular modeling structural parameters and high-performance liquid chromatography (HPLC) retention data of 11 cardiovascular system drugs by principal component analysis (PCA) in relation to their pharmacological activity was performed. The six retention data parameters were deter...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms11072681
更新日期：2010-07-09 00:00:00
abstract：:One of the hallmarks of the acute toxicity of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) is a drastically reduced feed intake by an unknown mechanism. To further elucidate this wasting syndrome, we followed the effects of a single large dose (100 μg/kg) of TCDD on the serum levels of several energy balance-influencing...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms150813938
更新日期：2014-08-12 00:00:00
abstract：:The regeneration of dental tissues is a still an unmet clinical need; in fact, no therapies have been completely successful in regenerating dental tissue complexes such as periodontium, which is also due to the lack of scaffolds that are able to guide and direct cell fate towards the reconstruction of different minera...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms19113604
更新日期：2018-11-15 00:00:00
abstract：:Schizophrenia and autism spectrum disorder (ASD) are multi-factorial and multi-symptomatic psychiatric disorders, each affecting 0.5%-1% of the population worldwide. Both are characterized by impairments in cognitive functions, emotions and behaviour, and they undermine basic human processes of perception and judgment...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms17060856
更新日期：2016-06-01 00:00:00
abstract：:Non-melanomatous skin cancers (NMSCs), which include basal and squamous cell carcinoma (BCC and SCC respectively), represent a significant burden on the population, as well as an economic load to the health care system; yet treatments of these preventable cancers remain ineffective. Studies estimate that there has bee...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms18071369
更新日期：2017-06-27 00:00:00
abstract：:The consumption of carotenoid-rich vegetables such as tomatoes and tomato sauces is associated with reduced risk of several chronic diseases. The predominant carotenoids in tomato products are in the (all-E) configuration, but (Z) isomers can be formed during thermal processing. The effect of cooking time (15, 30, 45 ...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms16059588
更新日期：2015-04-28 00:00:00
abstract：:Neurodegenerative disorders can induce modifications of several proteins; one of which is ceruloplasmin (Cp), a ferroxidase enzyme found modified in the cerebrospinal fluid (CSF) of neurodegenerative diseases patients. Cp modifications are caused by the oxidation induced by the pathological environment and are usually...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms22020663
更新日期：2021-01-11 00:00:00
abstract：:The present study was designed to probe the effects of Huperzine A (HupA) on diabetes-associated cognitive decline (DACD) using a streptozotocin (STZ)-injected rat model. Diabetic rats were treated with HupA (0.05 and 0.1 mg/kg) for seven weeks. Memory functions were evaluated by the water maze test. Nissl staining wa...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms15057667
更新日期：2014-05-05 00:00:00
abstract：:A field experiment was conducted using a 3 × 3 orthogonal regression design to explore the growth promotion of one-year-old Yunnan pine seedlings (Pinus yunnanensis Franch.) in response to foliar application of IAA (indole-3-acetic acid) at rates of 0, 200 and 400 mg·L(-1) and IBA (indole-3-butyric acid) at rates of 0...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms13056507
更新日期：2012-01-01 00:00:00
abstract：:Asia-Pacific NMR (APNMR) has been an important scientific event in the region, engaging a large number of NMR scientists from academia and industries [...]. ...
journal_title：International journal of molecular sciences
pub_type： 社论
doi：10.3390/ijms21124419
更新日期：2020-06-22 00:00:00
abstract：:Prion diseases are rare transmissible neurodegenerative disorders caused by the accumulation of a misfolded isoform (PrPSc) of the cellular prion protein (PrPC) in the central nervous system (CNS). Neuropathological hallmarks of prion diseases are neuronal loss, astrogliosis, and enhanced microglial proliferation and ...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms21207765
更新日期：2020-10-20 00:00:00
abstract：:Several cellular insults can result in sperm DNA fragmentation either on one or both DNA strands. Oxidative damage, premature interruption of the apoptotic process and defects in DNA compaction during spermatogenesis are the main mechanisms that cause DNA breaks in sperm. The two-tailed Comet assay is the only techniq...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms21113882
更新日期：2020-05-29 00:00:00
abstract：:The 2010 McDonald criteria were developed to allow a more rapid diagnosis of relapsing-remitting multiple sclerosis (MS) by only one MRI of the brain. Although cerebrospinal fluid (CSF) is not a mandatory part of the latest criteria, the evidence of an intrathecal humoral immunoreaction in the form of oligoclonal band...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms17091592
更新日期：2016-09-21 00:00:00
abstract：:Matrix metalloproteinases (MMPs) play an important role in the degradation of extracellular matrix components crucial for tumor growth, invasion and metastasis. MMPs are controlled by natural inhibitors called tissue inhibitors of metalloproteinases (TIMPs). We and others have demonstrated that MMPs and TIMPs are espe...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms131013240
更新日期：2012-10-16 00:00:00
abstract：:Protein-protein interactions are important for biochemical processes in biological systems. The 3D structure of the macromolecular complex resulting from the protein-protein association is a very useful source to understand its specific functions. This work focuses on computational study for protein-protein docking, w...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms9010065
更新日期：2008-01-01 00:00:00
