Category: 112-63-0

Xu, Li; Wang, Han; Yu, Qian-qian; Ge, Jin-ru; Zhang, Xian-zheng; Mei, Dan; Liang, Fa-qin; Cai, Xiao-yu; Zhu, Yue; Shu, Jin-ling; Tai, Yu; Wei, Wei; Zhang, Ling-ling published the artcile< The monomer derivative of paeoniflorin inhibits macrophage pyroptosis via regulating TLR4/ NLRP3/ GSDMD signaling pathway in adjuvant arthritis rats>, Synthetic Route of 112-63-0, the main research area is paeoniflorin macrophage pyroptosis TLR NLRP GSDMD signaling pathway arthritis; Adjuvant arthritis; Macrophage pyroptosis; Monomer derivative of paeoniflorin; Rheumatoid arthritis; TLR4/NLRP3/GSDMD signaling pathway.

This study was aimed to investigate the effect of monomer derivative of paeoniflorin (MDP) on macrophage pyroptosis mediated by TLR4/NLRP3/GSDMD signaling pathway in adjuvant arthritis (AA) rats. Wistar rats were divided into normal group, AA model group, MDP (50 mg/kg) group and MTX (0.5 mg/kg) group. The expression of TLR4, NLRP3 and GSDMD in macrophage were detected by immunofluorescence assay. The expression of TLR4 and the ratio of macrophage pyroptosis were analyzed by flow cytometry. Cell morphol. was observed by SEM. The cytokine levels of IL-18 and IL-1β were detected by ELISA. The expressions of proteins related to macrophage pyroptosis were detected by western blot. MDP has a therapeutic effect on rats AA by reducing the secondary inflammation and improving pathol. changes. The results of X-ray imaging and ultrasound images showed that MDP could inhibit bone erosion, soft tissue swelling, and joint space narrowing. Macrophage pyroptosis was found in secondary inflammation of AA rats. The expressions of TLR4, MyD88, NLRP3, Caspase-1, ASC, and GSDMD-N in macrophage were increased, the levels of IL-18 and IL-1β were enhanced, and the morphol. of pyroptosis could be observed MDP could inhibit macrophage polarization and macrophage pyroptosis, and down-regulated the cytokine levels of IL-18 and IL-1β in AA rats. MDP could regulate the M1/m2 ratio, decreased the ratio of macrophage pyroptosis and down-regulated the expressions of TLR4, MyD88, NLRP3, Caspase-1, ASC, and GSDMD-N in vivo and in vitro. Abnormal activation of TLR4/NLRP3/GSDMD signaling pathway may be involved in macrophage pyroptosis in AA rats. The therapeutic effect of MDP on AA rats is related to the inhibition of macrophage pyroptosis by regulating the TLR4/NLRP3/GSDMD signaling pathway.

International Immunopharmacology published new progress about Arthritis. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Synthetic Route of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Zhao, Wenbo; Yun, Keming published the artcile< Propofol enhances the sensitivity of glioblastoma cells to temozolomide by inhibiting macrophage activation in tumor microenvironment to down-regulate HIF-1α expression>, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is Glioblastoma; Propofol; Temozolomide; Tumor-associated macrophages.

Temozolomide (TMZ) is the first-line drug for the clin. treatment of glioblastoma (GBM), but drug resistance limits its treatment benefits. This study was intended to investigate whether propofol could restrict the resistance of GBM cells to TMZ and uncover the underlying mechanisms. Human GBM cell line U251 and TMZ-resistant U251/TMZ cell line were transplanted into mice to construct GBM and TMZ-resistant GBM xenograft tumors. Tumor growth in mice was monitored, and the tumor tissues were collected for biochem. anal. THP-1 cell differentiated into M0 subtype macrophage using phorbol 12-myristate 13-acetate (PMA). The culture medium of M0 macrophage was collected for treating U251 cells with the presence or absence of propofol or propofol + DMOG (HIF-1α activator). Results showed that propofol significantly enhanced the inhibitory effect of TMZ on tumor growth, macrophage infiltration and inflammation in TMZ-resistant GBM xenograft tumors in vivo. Compared with GBM xenograft tumors, higher expression of HIF-1α, O6-methylguanine-DNA methyltransferase (MGMT), p-p65 and cyclooxygenase 2 (Cox2) was observed in TMZ-resistant GBM xenograft tumors, but propofol co-treatment markedly reduced the expression of these proteins. In in vitro experiments, culture medium from M0 macrophage promoted U251 cell survival, inflammation and expression of HIF-1α, MGMT, p65 and Cox2, whereas inhibited cell apoptosis. However, propofol suppressed the PMA-induced THP-1 M0 macrophage activation, and propofol-treated culture medium from M0 macrophage blocked all the effects of M0 medium on U251 cells. Addnl., DMOG reversed the effect of propofol-treated M0 medium on U251 cells. In conclusion, Propofol restricted TMZ resistance via inhibiting macrophage activation and down-regulating HIF-1α expression in GBM.

Experimental Cell Research published new progress about 112-63-0. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Wu, Xiaowei; Iwata, Takayuki; Scharf, Adam; Qin, Tian; Reichl, Kyle D.; Porco, John A. published the artcile< Asymmetric Synthesis of Gonytolide A: Strategic Use of an Aryl Halide Blocking Group for Oxidative Coupling>, Category: esters-buliding-blocks, the main research area is asym gonytolide A synthesis aryl halide oxidative coupling.

The first synthesis of the chromanone lactone dimer gonytolide A was achieved employing vanadium(V)-mediated oxidative coupling of the monomer gonytolide C. An o-bromine blocking group strategy was employed to favor para-para coupling and to enable kinetic resolution of (±)-gonytolide C. Asym. conjugate reduction enabled practical kinetic resolution of a chiral, racemic precursor and the asym. synthesis of (+)-gonytolide A and its atropisomer.

Journal of the American Chemical Society published new progress about Atropisomers. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Category: esters-buliding-blocks.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Jatyan, Reena; Singh, Prabhjeet; Sahel, Deepak Kumar; Karthik, Y. G.; Mittal, Anupama; Chitkara, Deepak published the artcile< Polymeric and small molecule-conjugates of temozolomide as improved therapeutic agents for glioblastoma multiforme>, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is review glioblastoma multiforme temozolomide therapeutic agent bioavailability nanocarrier liposome; Glioblastoma Multiforme; Polymer drug conjugates; Prodrugs; Small molecules; Temozolomide.

A review. Temozolomide (TMZ), an imidazotetrazine, is a second-generation DNA alkylating agent used as a first-line treatment of glioblastoma multiforme (GBM). It was approved by FDA in 2005 and declared a blockbuster drug in 2008. Although TMZ has shown 100% oral bioavailability and crosses the blood-brain barrier effectively, however it suffers from limitations such as a short half-life (∼1.8 h), rapid metabolism, and lesser accumulation in the brain (∼10-20%). Addnl., development of chemoresistance has been associated with its use. Since it is a potential chemotherapeutic agent with an unmet medical need, advanced delivery strategies have been explored to overcome the associated limitations of TMZ. Nanocarriers including liposomes, solid lipid nanoparticles (SLNs), nanostructure lipid carriers (NLCs), and polymeric nanoparticles have demonstrated their ability to improve its circulation time, stability, tissue-specific accumulation, sustained release, and cellular uptake. Because of the appreciable water solubility of TMZ (∼5 mg/mL), the phys. loading of TMZ in these nanocarriers is always challenging. Alternatively, the conjugation approach, wherein TMZ has been conjugated to polymers or small mols., has been explored with improved outcomes in vitro and in vivo. This review emphasized the practical evidence of the conjugation strategy to improve the therapeutic potential of TMZ in the treatment of glioblastoma multiforme.

Journal of Controlled Release published new progress about Bioavailability. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Gaynanova, Gulnara A.; Bekmukhametova, Alina M.; Mukhitova, Rezeda K.; Kharlamov, Sergey V.; Ziganshina, Albina Y.; Zakharova, Lucia Ya.; Konovalov, Alexander I. published the artcile< Pyrene fluorescence quenching in supramolecular systems based on dimethylaminomethylated resorcinarene>, Application In Synthesis of 112-63-0, the main research area is pyrene dimethylaminomethylated resorcinarene fluorescence quenching.

The aim of this work is the development of stable fluorophore-quencher pairs with a controlled response for bioassay in the laboratory The widely used in bioanal. pyrene and its water-soluble derivative were selected as organic fluorophores. Water-soluble aminomethylated calixarene with sulfonatoethyl groups at the “”lower rim”” was chosen as a stabilizer. We have established a strong fluorescence quenching in the solution of resorcinarene even at low premicellar concentrations which indicates the pyrene transition into a non-polar microenvironment. The data on the influence of pH, buffer composition, and the macrocyclic platform on the fluorescence quenching of pyrene in the presence of resorcinarene were obtained. The temperature dependence of the fluorescence quenching of pyrene was obtained with the aim of establishing the mechanism of the formation of complex fluorophore-resorcinarene (static vs. dynamic quenching).

Journal of Molecular Liquids published new progress about Fluorescence imaging. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application In Synthesis of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Thomson, Jennifer E.; Kyle, Andrew F.; Ling, Kenneth B.; Smith, Siobhan R.; Slawin, Alexandra M. Z.; Smith, Andrew D. published the artcile< Applications of NHC-mediated O- to C-carboxyl transfer: synthesis of (±)-N-benzyl-coerulescine and (±)-horsfiline>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is coerulescine horsfiline oxindole alkaloid synthesis carboxyl transfer rearrangement.

N-Heterocyclic carbene (NHC) promoted O- to C-carboxyl transfer of 3-allylindolyl Ph carbonates generated 3-allyl-3-phenoxycarbonyloxindoles with good catalytic efficiency, which were readily converted into (±)-N-benzylcoerulescine (I) and (±)-horsfiline (II).

Tetrahedron published new progress about Oxindole alkaloids Role: SPN (Synthetic Preparation), PREP (Preparation). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Kang, Hyunkoo; Lee, Haksoo; Kim, Dahye; Kim, Byeongsoo; Kang, JiHoon; Kim, Hae Yu; Youn, HyeSook; Youn, BuHyun published the artcile< Targeting Glioblastoma Stem Cells to Overcome Chemoresistance: An Overview of Current Therapeutic Strategies>, Reference of 112-63-0, the main research area is review brain tumor glioblastoma stem cell temozolomide drug repositioning; cancer stem cells; chemoresistance; glioblastoma; temozolomide.

A review. Glioblastoma (GBM) is the most malignant primary brain tumor. The current standard approach in GBM is surgery, followed by treatment with radiation and temozolomide (TMZ); however, GBM is highly resistant to current therapies, and the standard of care has not been revised over the last two decades, indicating an unmet need for new therapies. GBM stem cells (GSCs) are a major cause of chemoresistance due to their ability to confer heterogeneity and tumorigenic capacity. To improve patient outcomes and survival, it is necessary to understand the properties and mechanisms underlying GSC chemoresistance. In this review, we describe the current knowledge on various resistance mechanisms of GBM to therapeutic agents, with a special focus on TMZ, and summarize the recent findings on the intrinsic and extrinsic mechanisms of chemoresistance in GSCs. We also discuss novel therapeutic strategies, including mol. targeting, autophagy inhibition, oncolytic viral therapy, drug repositioning, and targeting of GSC niches, to eliminate GSCs, from basic research findings to ongoing clin. trials. Although the development of effective therapies for GBM is still challenging, this review provides a better understanding of GSCs and offers future directions for successful GBM therapy.

Biomedicines published new progress about Antitumor agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Reference of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Luo, Long; Li, Xiang; Crooks, Richard M. published the artcile< Low-Voltage Origami-Paper-Based Electrophoretic Device for Rapid Protein Separation>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is origami paper electrophoresis device protein fluorophore.

We present an origami paper-based electrophoretic device (oPAD-Ep) that achieves rapid (∼5 min) separation of fluorescent mols. and proteins. Due to the innovative design, the required driving voltage is just ∼10 V, which is more than 10 times lower than that used for conventional electrophoresis. The oPAD-Ep uses multiple, thin (180 μm/layer) folded paper layers as the supporting medium for electrophoresis. This approach significantly shortens the distance between the anode and cathode, and this, in turn, accounts for the high elec. field (>1 kV/m) that can be achieved even with a low applied voltage. The multilayer design of the oPAD-Ep enables convenient sample introduction by use of a slip layer as well as easy product anal. and reclamation after electrophoresis by unfolding the origami paper and cutting out desired layers. We demonstrate the use of oPAD-Ep for simple separation of proteins in bovine serum, which illustrates its potential applications for point-of-care diagnostic testing.

Analytical Chemistry (Washington, DC, United States) published new progress about Albumins Role: ANT (Analyte), PUR (Purification or Recovery), ANST (Analytical Study), PREP (Preparation). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Pero, Joseph E.; Rossi, Michael A.; Lehman, Hannah D. G. F.; Kelly, Michael J. III; Mulhearn, James J.; Wolkenberg, Scott E.; Cato, Matthew J.; Clements, Michelle K.; Daley, Christopher J.; Filzen, Tracey; Finger, Eleftheria N.; Gregan, Yun; Henze, Darrell A.; Jovanovska, Aneta; Klein, Rebecca; Kraus, Richard L.; Li, Yuxing; Liang, Annie; Majercak, John M.; Panigel, Jacqueline; Urban, Mark O.; Wang, Jixin; Wang, Ying-Hong; Houghton, Andrea K.; Layton, Mark E. published the artcile< Benzoxazolinone aryl sulfonamides as potent, selective Nav1.7 inhibitors with in vivo efficacy in a preclinical pain model>, Application In Synthesis of 112-63-0, the main research area is benzoxazolinone aryl sulfonamide preparation sodium channel inhibitor oral analgesic; Chronic pain; Na(v)1.7 inhibition; Oral bioavailability; Pharmacological selectivity; Voltage-gated sodium channel.

Studies on human genetics have suggested that inhibitors of the Nav1.7 voltage-gated sodium channel hold considerable promise as therapies for the treatment of chronic pain syndromes. Herein, we report novel, peripherally-restricted benzoxazolinone aryl sulfonamides as potent Nav1.7 inhibitors with excellent selectivity against the Nav1.5 isoform, which is expressed in the heart muscle. Elaboration of initial lead compound 3d afforded exemplar 13, which featured attractive physicochem. properties, outstanding lipophilic ligand efficiency and pharmacol. selectivity against Nav1.5 exceeding 1000-fold. Key structure-activity relationships associated with oral bioavailability were leveraged to discover compound 17, which exhibited a comparable potency/selectivity profile as well as full efficacy following oral administration in a preclin. model indicative of antinociceptive behavior.

Bioorganic & Medicinal Chemistry Letters published new progress about Analgesics. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application In Synthesis of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Wang, Yuxuan; Liu, Xintian; Su, Chen; Ding, Yanjun; Pan, Luqing published the artcile< Process optimization for fermented siwu decoction by multi-index-response surface method and exploration of the effects of fermented siwu decoction on the growth, immune response and resistance to Vibrio harveyi of Pacific white shrimp (Litopenaeus vannamei)>, SDS of cas: 112-63-0, the main research area is Vibrio Litopenaeus growth immune response fermented siwu decoction; Bacillus; Fermentation siwu decoction; Gut microbiota; Litopenaeus vannamei; Physiological functions.

The purpose of this study was to explore the optimal fermentation technol. of Chinese herbal medicine formula-Siwu Decoction and the effects of fermented Siwu Decoction (FSW) on the growth performance, immune response, intestinal microflora and anti microbial ability of Litopenaeus vannamei. Response to surface methodol. (RSM) was used to optimize the fermentation process of Siwu Decoction. The optimal fermentation conditions were obtained as follows: inoculation amount of mixed strains was 4.5%, fermentation time was 36 h, and the ratio of material to liquid was 20%. A total of 1260 shrimps were selected and divided into seven groups, three in parallel in each group. The dietary level of each group was as follows: Control (No additions), USW1 (0.2% unfermented herbal medicine), USW2 (0.5% unfermented herbal medicine), USW3 (0.8% unfermented herbal medicine), FSW1 (0.2% fermented herbal medicine), FSW2 (0.5% fermented herbal medicine), FSW3 (0.8% fermented herbal medicine). The immune response and antioxidant defense ability of hemocytes and intestine were measured at 21 and 42 days of feeding and the intestinal flora and growth performance were measured at 42 days of feeding, after that, a 7-day challenge test against Vibrio harveyi was conducted. The results showed that fermented Siwu Decoction significantly improved the growth performance and body composition of Litopenaeus vannamei; significantly increased the total number of hemocytes, phagocytic activity, antibacterial activity and bacteriolytic activity of Litopenaeus vannamei, and improved the antioxidant activity of Litopenaeus vannamei; the addition of fermented Siwu Decoction significantly increased the gene expression level of hemocytes and intestinal tract of Litopenaeus vannamei, and improved the antioxidant activity of Litopenaeus vannamei. The abundance of Bacillus increased, while the abundance of Vibrio decreased. After Vibrio harveyi challenge, the cumulative mortality of FSW group was significantly lower than that of control group. Fermented Siwu Decoction may be a potential physiol. enhancer in aquaculture, and can be widely used in aquaculture.

Fish & Shellfish Immunology published new progress about Actinobacteria. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, SDS of cas: 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics