Tag: M.W=100-150

do Sacramento, Priscila Mendonca published the artcileMajor depression favors the expansion of Th17-like cells and decrease the proportion of CD39+Treg cell subsets in response to myelin antigen in multiple sclerosis patients, Formula: C6H8O4, the publication is Cellular and Molecular Life Sciences (2022), 79(6), 298, database is CAplus and MEDLINE.

Mood disorders have been associated with risk of clin. relapses in multiple sclerosis (MS), a demyelinating disease mediated by myelin-specific T cells. Author aimed to investigate the impact of major depressive disorder (MDD) and cytokine profile of T-cells in relapsing remitting MS patients. For author study, plasma and PBMC were obtained from 60 MS patients (30 with lifetime MDD) in remission phase. The PBMC cultures were stimulated with anti-CD3/anti-CD28 beads or myelin basic protein (MBP), and effector and regulatory T cell phenotypes were determined by flow cytometry. The cytokine levels, both in the plasma or in the supernatants collected from PBMC cultures, were quantified by Luminex. In some experiments, the effect of serotonin (5-HT) was investigated. Here, higher Th17-related cytokine levels in response to anti-CD3/anti-CD28 and MBP were quantified in the plasma and PBMC cultures of the MS/MDD group in comparison with MS patients. Further, elevated frequency of CD4⁺ and CD8⁺ T cells capable of producing IL-17, IL-22 and GM-CSF was observed in depressed patients. Interestingly, the percentage of myelin-specific IFN-γ⁺IL-17⁺ and IFN-γ⁺GM-CSF⁺ CD4⁺ T cells directly correlated with neurol. disabilities. In contrast, the occurrence of MDD reduced the proportion of MBP-specific CD39⁺Tregs subsets. Notably, the severity of both neurol. disorder and depressive symptoms inversely correlated with these Tregs. Finally, the addition of 5-HT downregulated the release of Th17-related cytokines in response to anti-CD3/anti-CD28 and myelin antigen. In summary, author findings suggested that recurrent major depression, by favoring imbalances of effector Th17 and Treg cell subsets, contributes to MS severity.

Cellular and Molecular Life Sciences published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C6H8O4, Formula: C6H8O4.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Begum, Zubeda published the artcileSimple primary β-amino alcohols as organocatalysts for the asymmetric Michael addition of β-keto esters to nitroalkenes, Product Details of C6H8O3, the publication is RSC Advances (2021), 11(1), 203-209, database is CAplus and MEDLINE.

Simple primary β-amino alcs. acted as an efficient organocatalysts in the asym. Michael addition of β-keto esters with nitroalkenes which afforded highly pure chiral Michael adducts. Also, both enantiomers of the adducts were obtained, depending on the specific catalyst used and reaction temperature

RSC Advances published new progress about 517-23-7. 517-23-7 belongs to esters-buliding-blocks, auxiliary class Tetrahydrofuran,Ketone,Ester, name is 3-Acetyldihydrofuran-2(3H)-one, and the molecular formula is C6H8O3, Product Details of C6H8O3.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Pike, Ryan A. S. published the artcileK₂CO₃-Catalyzed Synthesis of 2,5-Dialkyl-4,6,7-tricyano-Decorated Indoles via Carbon-Carbon Bond Cleavage, SDS of cas: 5340-78-3, the publication is Organic Letters (2020), 22(8), 3268-3272, database is CAplus and MEDLINE.

A novel method to synthesize 2,5-dialkyl-4,6,7-tricyanoindole derivatives from a base-catalyzed reaction of 1,3-diketones with fumaronitrile was described. The reaction proceeded by the condensation of two mols. of fumaronitrile and one mol. of 1,3-diketone in a remarkable process that involved the cleavage of one C(sp³)-C(sp²) bond in 1,3-diketones and the formation of one carbon-nitrogen bond and four carbon-carbon bonds to construct both the aryl and pyrrole rings of the indole in one step.

Organic Letters published new progress about 5340-78-3. 5340-78-3 belongs to esters-buliding-blocks, auxiliary class Aliphatic Chain, name is Ethyltert-butylacetate, and the molecular formula is C8H16O2, SDS of cas: 5340-78-3.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Watanabe, Michiko published the artcileApplication of cytochrome P450 reactivity on the characterization of chemical compounds and its association with repeated-dose toxicity, Related Products of esters-buliding-blocks, the publication is Toxicology and Applied Pharmacology (2020), 114854, database is CAplus and MEDLINE.

Repeated-dose toxicity (RDT) studies are one of the critical studies to assess chem. safety. There have been some studies attempting to predict RDT endpoints based on chem. substructures, but it remains very difficult to establish such a method, and a more detailed characterization of chem. compounds seems necessary. Cytochrome P450s (P450s) comprise multiple forms with different substrate specificities and play important roles in both the detoxification and metabolic activation of xenobiotics. In this study, we investigated possible use of P 450 reactivity of chem. compounds to classify the compounds A total of 148 compounds with available rat RDT test data were used as test compounds and subjected to inhibition assays against 18 human and rat P450s. Among the tested compounds, 82 compounds inhibited at least one P 450 form. Hierarchical clustering analyses using the P 450 inhibitory profiles divided the 82 compounds into nine groups, some of which showed characteristic chem. and biol. properties. Principal component analyses of the P 450 inhibition data in combination with the calculated chem. descriptors demonstrated that P 450 inhibition data were plotted differently than most chem. descriptors in the loading plots. Finally, association analyses between P 450 inhibition and RDT endpoints showed that some endpoints related to the liver, kidney and hematol. were significantly associated with the inhibition of some P450s. Our present results suggest that the P 450 reactivity profiles can be used as novel descriptors for characterizing chem. compounds for the investigation of the toxicity mechanism and/or the establishment of a toxicity prediction model.

Toxicology and Applied Pharmacology published new progress about 517-23-7. 517-23-7 belongs to esters-buliding-blocks, auxiliary class Tetrahydrofuran,Ketone,Ester, name is 3-Acetyldihydrofuran-2(3H)-one, and the molecular formula is C18H24N6O6S4, Related Products of esters-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Mashima, Kiyomi published the artcileDimethyl fumarate ameliorates graft-versus-host disease by inhibiting T-cell metabolism and immune responses through a reactive oxygen species-dependent mechanism, Quality Control of 624-49-7, the publication is British Journal of Haematology (2022), 197(6), e78-e82, database is CAplus and MEDLINE.

Acute graft-vs.-host disease (GVHD) is among the leading causes of non-relapse mortality and morbidity after allogeneic haematopoietic stem cell transplantation. Di-Me fumarate (DMF), a fumaric acid derivative, is a novel therapeutic agent for relapsing multiple sclerosis and psoriasis. For instance, DMF succinates a key glycolytic enzyme, glyceraldehyde 3-phosphate dehydrogenase (GAPDH), and irreversibly inactivates its enzymic activity, thereby downregulating aerobic glycolysis in CD4+ T cells. This study investigated whether, and if so, how DMF impairs the metabolism and immune responses of antigen-activated Tcells both in vitro and in vivo using a xenogeneic GVHD mouse model. While the number of CD4+ T cells decreased, the proportion of CD25+ FoxP3+ regulatory T cells (Treg) was higher in DMF-treated mice, and thus the total number of Tregs was equivalent in both groups. Given that DMF depletes intracellular GSH levels by forming succinated glutathione, causing dysregulated ROS accumulation in diverse immune cells and cancer cells, we investigated the redox status of T-cell receptor (TCR)- stimulated T cells after DMF treatment and evaluated the association between their metabolic profiles and effector T-cell function. Furthermore, NAC almost completely restored viability (Figure 2F), proliferation (Figure 2G), and interferon gamma (IFN-γ) production (Figure 2H) of TCR-stimulated T cells following DMF treatment. Clin. relevant GVHD model, which show better disease control and prolonged survival by DMF treatment, can be readily translated to clin. settings. Our findings will provide a mol. basis for potential future clin. applications of DMF for the prevention and treatment of GVHD.

British Journal of Haematology published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C6H8O4, Quality Control of 624-49-7.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Maeta, Takahiro published the artcileDimethyl fumarate induces apoptosis via inhibiting NF-κB and STAT3 signaling in adult T-cell leukemia/lymphoma cells, Product Details of C6H8O4, the publication is Anticancer Research (2022), 42(5), 2301-2309, database is CAplus and MEDLINE.

Adult T-cell leukemia (ATL) is a peripheral T lymphocytic malignancy caused by human T-cell leukemia virus type 1 (HTLV-1) infection. Despite treatment that includes novel agents that have been developed, most of ATL patients relapse and acquire multidrug resistance. As a result, the creation of newer agents is critical Di-Me fumarate (DMF) has several effects in cancer cells, including cell signaling, proliferation and cell death. However, its antitumor effects on ATL cells remain unknown. In this study, we looked at DMF′s antitumor effects on ATL cells.Materials and methods: We examined the effects of DMF on proliferation and apoptosis using the trypan blue exclusion assay and annexin V/propidium iodide staining in HTLV-1-infected and transformed T-cell lines, MT-1 and MT-2 cells. We also evaluated the effects of DMF on the nuclear factor-kappa B (NF-κB) and signal transducers and activators of transcription 3 (STAT3) signaling pathways and anti-apoptotic proteins by immunoblotting.Results: DMF inhibited proliferation and induced apoptosis in MT-1 and MT-2 cells by activating poly ADP-ribose polymerase (PARP). Furthermore, DMF inhibited the constitutive activation of both canonical and non-canonical NF-κB pathways in MT-2 cells and the non-canonical NF-κB pathway in MT-1 cells. DMF also inhibited the constitutive tyrosine phosphorylation of STAT3 and the expression of anti-apoptotic proteins, c-IAP2 and survivin in both cells.Conclusion: These results indicate that DMF inhibits proliferation and induces apoptosis in HTLV-1-infected and transformed T-cells by suppressing NF-κB and STAT3 signaling pathways. DMF should be investigated further as a novel agent for ATL.

Anticancer Research published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C6H8O4, Product Details of C6H8O4.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Morozzi, Chiara published the artcileSynthesis and cellular evaluation of click-chemistry probes to study the biological effects of alpha, beta-unsaturated carbonyls, Product Details of C6H8O4, the publication is Redox Biology (2022), 102299, database is CAplus and MEDLINE.

Humans are commonly exposed to α,β-unsaturated carbonyls as both environmental toxins (e.g. acrolein) and therapeutic drugs (e.g. dimethylfumarate, DMFU, a front-line drug for the treatment of multiple sclerosis and psoriasis). These compounds undergo rapid Michael addition reactions with amine, imidazole and thiol groups on biol. targets, with reaction at protein Cys residues being a major reaction pathway. However, the cellular targets of these species (the ‘adductome’) are poorly understood due to the absence of readily identifiable tags or reporter groups (chromophores/fluorophores or antigens) on many α,β-unsaturated carbonyls. Here we report a ‘proof of concept’ study in which we synthesize novel α,β-unsaturated carbonyls containing an alkyne function introduced at remote sites on the α,β-unsaturated carbonyl compounds (e.g. one of the Me groups of dimethylfumarate). The presence of this tag allows ‘click-chem.’ to be used to visualize, isolate, enrich and characterize the cellular targets of such compounds The probes show similar selectivity and reactivity to the parent compounds and compete for cellular targets, yielding long-lived (stable) adducts that can be visualized in intact cells (such as primary human coronary artery smooth muscle cells), and extracted and enriched for subsequent target anal. It is shown using this approach that dimethylfumarate forms adducts with multiple intracellular targets including cytoskeletal, organelle and nuclear species, with these including the rate-limiting glycolytic enzyme, glyceraldehyde-3-phosphate dehydrogenase (GAPDH). This approach should be amenable to use with multiple α,β-unsaturated carbonyls and a wide variety of targets containing nucleophilic sites.

Redox Biology published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C6H8O4, Product Details of C6H8O4.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

La-ongthong, Kannika published the artcileCyclization of o-Alkynylisocyanobenzenes with 1,3-Dicarbonyl Compounds, Recommanded Product: 3-Acetyldihydrofuran-2(3H)-one, the publication is Synlett (2022), 33(14), 1411-1418, database is CAplus.

A facile and convenient reaction of o-alkynylisocyanobenzenes with various active-methylene compounds, including 1,3-diesters, 1,3-diketones,β-keto esters, and β-keto amides, under Bronsted basic conditions, had been developed. Di-Et malonate reacted smoothly with a collection of o-alkynylisocyanobenzenes to provide the corresponding 2-quinolin-2-yl malonates in excellent yields. Acetylacetone gave a mixture of quinolin-4-yl and quinolin-2-yl derivatives Acetoacetate esters and acetoacetyl amide derivative initially gave 2-quinolin-2-yl adducts that underwent partial deacetylation under the reaction conditions.

Synlett published new progress about 517-23-7. 517-23-7 belongs to esters-buliding-blocks, auxiliary class Tetrahydrofuran,Ketone,Ester, name is 3-Acetyldihydrofuran-2(3H)-one, and the molecular formula is C6H8O3, Recommanded Product: 3-Acetyldihydrofuran-2(3H)-one.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Ram, Ram N. published the artcileβ,β,β-Trichloroethyl-NH-Enamine as Viable System for 5-Endo-trig Radical Cyclization via Multifaceted Cu^I-Cu^II Redox Catalysis: Single Step Synthesis of Multi-Functionalized NH-Pyrroles, Category: esters-buliding-blocks, the publication is Advanced Synthesis & Catalysis (2019), 361(24), 5661-5676, database is CAplus.

A mild and regioselective copper-catalyzed direct synthesis of multi-substituted and functionalized NH-pyrroles was reported in high yields from diverse β,β,β-trichloroethyl-NH-enamines via a novel 5-endo-trig radical cyclization mode, previously known to be unviable in the enamine system. An approach to transform a geometrically ‘disfavored to favored’ 5-endo-trig radical cyclization mode in NH-enamine systems via multifaceted Cu^I-Cu^II redox catalysis generating radicals, preventing dehalogenative reduction of radical precursors and dehydrohalogenating the 5-endo-trig cyclized products was demonstrated exptl. With wider substrate scope, this method incorporated halo-, NH- and carbonyl functionalities besides alkyl, aryl and heteroaryl substituents in the pyrrole unit easily. These difficult 3-halo-NH-pyrroles are potential sources for natural products, agrochems., pharmaceuticals and organometallic chem.

Advanced Synthesis & Catalysis published new progress about 517-23-7. 517-23-7 belongs to esters-buliding-blocks, auxiliary class Tetrahydrofuran,Ketone,Ester, name is 3-Acetyldihydrofuran-2(3H)-one, and the molecular formula is C6H8O3, Category: esters-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Bagheri, Farshid published the artcileEffect of dimethyl fumarate on the changes in the medial prefrontal cortex structure and behavior in the poly(I:C)-induced maternal immune activation model of schizophrenia in the male mice, Formula: C6H8O4, the publication is Behavioural Brain Research (2022), 113581, database is CAplus and MEDLINE.

The link between maternal immune activation (MIA) and the risk of developing schizophrenia (SCZ) later in life has been of major focus in recent years. This link could be bridged by activated inflammatory pathways and excessive cytokine release resulting in adverse effects on behavior, histol., and cytoarchitecture. The down-regulatory effects of immunomodulatory agents on the activated glial cells and their therapeutic effects on schizophrenic patients are consistent with this hypothesis. We investigated whether treatment with the anti-inflammatory drug di-Me fumarate (DMF) could rescue impacts of prenatal exposure to polyinosinic:polycytidylic acid [poly (I:C)]. Pregnant dams were administered poly(I:C) at gestational day 9.5. Offspring born from these mothers were treated with DMF for fourteen consecutive days from postnatal day 80 and were assessed behaviorally before and after treatment. The brains were then stained with Cresyl Violet or Golgi-Cox. In addition to the estimation of stereol. parameters, cytoarchitectural changes were also evaluated in the medial prefrontal cortex. MIA caused some abnormalities in behavior, as well as changes in the number of neurons and non-neurons. These alterations were also extended to pyramidal layer III neurons with a significant decrease in dendritic complexity and spine d. which DMF treatment could prevent these changes. Furthermore, DMF treatment was also effective against abnormal exploratory and depression-related behavior, but not the changes in the number of cells. These findings support the idea of using anti-inflammatory agents as adjunctive therapy in patients with SCZ.

Behavioural Brain Research published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C6H8O4, Formula: C6H8O4.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics