Tag: M.W=300-400

Tierney, Elaine; Remaley, Alan T.; Thurm, Audrey; Jager, Leah R.; Wassif, Christopher A.; Kratz, Lisa E.; Bailey-Wilson, Joan E.; Bukelis, Irena; Sarphare, Geeta; Jung, Eun Sol; Brand, Boudewien; Noah, Kelly K.; Porter, Forbes D. published the artcile< Sterol and lipid analyses identifies hypolipidemia and apolipoprotein disorders in autism associated with adaptive functioning deficits>, Related Products of 434-16-2, the main research area is sterol lipid hypolipidemia apolipoprotein disorder autism adaptive functioning deficit.

An improved understanding of sterol and lipid abnormalities in individuals with autism spectrum disorder (ASD) could lead to personalized treatment approaches. Toward this end, in blood, we identified reduced synthesis of cholesterol in families with ≥2 children with ASD participating with the Autism Genetic Resource Exchange (AGRE), as well as reduced amounts of high-d. lipoprotein cholesterol (HDL), apolipoprotein A1 (ApoA1) and apolipoprotein B (ApoB), with 19.9% of the subjects presenting with apolipoprotein patterns similar to hypolipidemic clin. syndromes and 30% with either or both ApoA1 and ApoB less than the fifth centile. Subjects with levels less than the fifth centile of HDL or ApoA1 or ApoA1 + ApoB had lower adaptive functioning than other individuals with ASD, and hypocholesterolemic subjects had apolipoprotein deficits significantly divergent from either typically developing individuals participating in National Institutes of Health or the National Health and Nutrition Examination Survey III.

Translational Psychiatry published new progress about Apolipoprotein A-I Role: ANT (Analyte), ANST (Analytical Study). 434-16-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C27H44O, Related Products of 434-16-2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Hayek, Simon; Bekaddour, Nassima; Besson, Laurie; Alves de Sousa, Rodolphe; Pietrancosta, Nicolas; Viel, Sebastien; Smith, Nikaia; Jacob, Yves; Nisole, Sebastien; Mandal, Rupasri; Wishart, David S.; Walzer, Thierry; Herbeuval, Jean-Philippe; Vidalain, Pierre-Olivier published the artcile< Identification of Primary Natural Killer Cell Modulators by Chemical Library Screening with a Luciferase-Based Functional Assay>, Electric Literature of 434-16-2, the main research area is innate immunity NK CD8 T cell luciferase myeloid leukemia; dextromethorphan; diphenhydramine; luciferase; natural killer cells; screening.

Natural killer (NK) cells are essential players of the innate immune response that secrete cytolytic factors and cytokines such as IFN-γ when contacting virus-infected or tumor cells. They represent prime targets in immunotherapy as defects in NK cell functions are hallmarks of many pathol. conditions, such as cancer and chronic infections. The functional screening of chem. libraries or biologics would greatly help identify new modulators of NK cell activity, but commonly used methods such as flow cytometry are not easily scalable to high-throughput settings. Here we describe an efficient assay to measure the natural cytotoxicity of primary NK cells where the bioluminescent enzyme NanoLuc is constitutively expressed in the cytoplasm of target cells and is released in co-culture supernatants when lysis occurs. We fully characterized this assay using either purified NK cells or total peripheral blood mononuclear cells (PBMCs), including some patient samples, as effector cells. A pilot screen was also performed on a library of 782 metabolites, xenobiotics, and common drugs, which identified dextrometorphan and diphenhydramine as novel NK cell inhibitors. Finally, this assay was further improved by developing a dual-reporter cell line to simultaneously measure NK cell cytotoxicity and IFN-γ secretion in a single well, extending the potential of this system.

SLAS Discovery published new progress about CD8-positive T cell. 434-16-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C27H44O, Electric Literature of 434-16-2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Zhou, Wenxu; Fisher, Paxtyn M.; Vanderloop, Boden H.; Shen, Yun; Shi, Huazhong; Maldonado, Adrian J.; Leaver, David J.; Nes, W. David published the artcile< A nematode sterol C4α-methyltransferase catalyzes a new methylation reaction responsible for sterol diversity>, Application In Synthesis of 434-16-2, the main research area is C4alpha methyltransferase dinosterol Caenorhabditis review; 8(14)-lophenol; Caenorhabditis elegans • biosynthesis; evolution.

A review. Primitive sterol evolution plays an important role in fossil record interpretation and offers potential therapeutic avenues for human disease resulting from nematode infections. Recognizing that C4-Me stenol products [8(14)-lophenol] can be synthesized in bacteria while C4-Me stanol products (dinosterol) can be synthesized in dinoflagellates and preserved as sterane biomarkers in ancient sedimentary rock is key to eukaryotic sterol evolution. In this regard, nematodes have been proposed to convert dietary cholesterol to 8(14)-lophenol by a secondary metabolism pathway that could involve sterol C4 methylation analogous to the C2 methylation of hopanoids (radicle-type mechanism) or C24 methylation of sterols (carbocation-type mechanism). Here, we characterized dichotomous cholesterol metabolic pathways in Caenorhabditis elegans that generate 3-oxo sterol intermediates in sep. paths to lophanol (4-Me stanol) and 8(14)-lophenol (4-Me stenol). We uncovered alternate C3-sterol oxidation and Δ7 desaturation steps that regulate sterol flux from which branching metabolite networks arise, while lophanol/8(14)-lophenol formation is shown to be dependent on a sterol C4α-methyltransferse (4-SMT) that requires 3-oxo sterol substrates and catalyzes a newly discovered 3-keto-enol tautomerism mechanism linked to S-adenosyl-l-methionine-dependent methylation. Alignment-specific substrate-binding domains similarly conserved in 4-SMT and 24-SMT enzymes, despite minimal amino acid sequence identity, suggests divergence from a common, primordial ancestor in the evolution of Me sterols. The combination of these results provides evolutionary leads to sterol diversity and points to cryptic C4-Me steroidogenic pathways of targeted convergence that mediate lineage-specific adaptations.

Journal of Lipid Research published new progress about Caenorhabditis elegans. 434-16-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C27H44O, Application In Synthesis of 434-16-2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Tang, Yun-Zhi; Tan, Yu-Hui; Ge, Zong-Tang; Liu, Zhen-Xin; Liao, Chun-Fa; Xie, Xiao-Bin published the artcile< Synthesis and crystal structures of two rare-earth metal polymers of olsalazine>, Safety of Sodium 5,5′-(diazene-1,2-diyl)bis(2-hydroxybenzoate), the main research area is rare earth olsalazine phenanthroline polymer complex preparation structure; europium gadolinium olsalazine phenanthroline polymer complex preparation structure; crystal structure europium gadolinium olsalazine phenanthroline polymer complex.

Two 1-dimensional linear coordination polymers, {[Gd2(L)2·(Phen)2·2(H2O)·2(NO3)]·2(EtOH)}n (1, H2L = olsalazine) and {[Eu2(L)2·(Phen)2·2(H2O)·2(NO3)]·EtOH}n (2), were obtained from self-assembly of Gd(NO3)3·8H2O or Eu(NO3)3·8H2O with olsalazine. Both complexes are 1-dimensional polymers, for 1 with crystal data: space group P1̅, a 11.651(4), b 11.865(4), and c 12.296(4) Å, α 77.984(4), β 65.559(4), and γ 74.558(5)°, Z = 1, R1 = 0.0389, wR2 = 0.0793, and 2 with crystal data: space group P1̅, a 11.626(3), b 11.834(3), c 12.287(4) Å, α 77.743(3), β 65.576(3), γ 74.371(3)°, Z = 1, R1 = 0.0609, wR2 = 0.1185. Central atoms (Gd or Eu) in both complexes adopt nine-coordinate tricapped trigonal prismatic geometry.

Journal of Coordination Chemistry published new progress about Crystal structure. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Safety of Sodium 5,5′-(diazene-1,2-diyl)bis(2-hydroxybenzoate).

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Kishore, M.; VijayaKumar, B.; NarasimhaReddy, Y. published the artcile< Formulation and evaluation of olsalazine sodium enteric coated tablets in ulcerative colitis>, Computed Properties of 6054-98-4, the main research area is olsalazine sodium enteric tablet coating ulcerative colitis.

Aim: To formulate and evaluate the fabricated olsalazine sodium enteric coated tablets in ulcerative colitis and also compare the In-vitro dissolution profile of optimized Olsalazine sodium enteric coated tablets in the presence of β- glycosidase at targeted colonic region. Materials: Olsalazine sodium, obtained as a gift sample from Aurbindo Pharmaceuticals Hyderabad, Telangana, and India. Et cellulose, Chitosan, PVP K30, Magnesium stearate, Lactose, Eudragit S-100, Acetone, Tri-Et citrate was used as a plasticizer etc. All the above polymers and excipients are obtained from S.D Fine Chems., Mumbai. Conclusion: The present study was fabricated to observe the drug release of Olsalazine sodium enteric coated tablets at targeted site specific colon region. These tablets were formulated from F1-F8 by selecting time dependent and release retard biodegrable polymers such as Et cellulose-chitosan composite by combining with different concentrations by wet granulation. This composite was included in this study to control the solubility of premature drug release in gastrointestinal fluid and in this regard, the above formulation F6 was optimized and coated with Eudragit-S 100 as enteric polymer as to retard the drug release at specified site colon by changing suitable concentration as like 1, 3, 5, and7 %. From which F6 containing 5% Eudragit-S 100 was shown only 75.6 % drug release in 24 h and also it was compared with dissolution medium containing β-glycosidase. In which enzymic condition the above formulation enhanced the drug release i.e, 98.3% was found in 24 h. Finally the current study was contributed to evaluated all pre, post compressional parameters of optimized formulation with various release kinetic mechanism such as zero order, first order, higuchi plot and peppas mayer equations studies.

International Journal of Pharmacy and Technology published new progress about Compressibility. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Computed Properties of 6054-98-4.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Singer, M. V.; Schmausser, H.; Schoenfeld, G. published the artcile< Efficacy and tolerability of olsalazine (dipentum) in the treatment of patients with ulcerative colitis-results of a field study>, Formula: C14H8N2Na2O6, the main research area is Dipentum ulcerative colitis.

Background/Aims: In the treatment of ulcerative colitis, 5-aminosalicylic acid is the standard therapy for both acute exacerbations of the disease and the maintenance of remission. Clin. studies have shown that olsalazine (Dipentum) – a prodrug converted to two mols. of 5-ASA by colonic bacteria – induces and maintains remission. This study aimed to investigate the efficacy and tolerability of olsalazine in patients with ulcerative colitis who were being treated in daily practice by private physicians specializing in gastroenterol. Methodol.: A total of 260 patients with ulcerative colitis (aged 17-77 years, 116 men) were studied. The doses of olsalazine and the clin. data (including acute disease symptoms and the occurrence of adverse events) were recorded over a 6-mo period. Results: Twenty per cent of patients had pancolitis, 48% had left-sided disease and 32% had proctitis or proctosigmoiditis. At study entry, 86% of patients had active disease; the percentages of these patients in remission after 6 wk and 6 mo were 42% and 91%, resp. Patients with active disease received a mean dose of olsalazine – 2324mg per day initially and 1325mg per day at 6 mo. The corresponding figures for patients in remission at study entry were 1386mg and 1162mg per day, resp. Seventy-three per cent of patients took olsalazine with food, as recommended. The overall rate of adverse events was low; no serious adverse events occurred. Conclusions: Olsalazine therapy resulted in a rapid regression in the acute symptoms of ulcerative colitis. Olsalazine was also effective in maintaining remission. The drug was well tolerated.

Hepato-Gastroenterology published new progress about Gastrointestinal agents. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Formula: C14H8N2Na2O6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Khazan, Negar; Kim, Kyu Kwang; Hansen, Jeanne N.; Singh, Niloy A.; Moore, Taylor; Snyder, Cameron W. A.; Pandita, Ravina; Strawderman, Myla; Fujihara, Michiko; Takamura, Yuta; Jian, Ye; Battaglia, Nicholas; Yano, Naohiro; Teramoto, Yuki; Arnold, Leggy A.; Hopson, Russell; Kishor, Keshav; Nayak, Sneha; Ojha, Debasmita; Sharon, Ashoke; Ashton, John M.; Wang, Jian; Milano, Michael T.; Miyamoto, Hiroshi; Linehan, David C.; Gerber, Scott A.; Kawar, Nada; Singh, Ajay P.; Tabdanov, Erdem D.; Dokholyan, Nikolay V.; Kakuta, Hiroki; Jurutka, Peter W.; Schor, Nina F.; Rowswell-Turner, Rachael B.; Singh, Rakesh K.; Moore, Richard G. published the artcile< Identification of a Vitamin-D Receptor Antagonist, MeTC7, which Inhibits the Growth of Xenograft and Transgenic Tumors In Vivo>, Formula: C27H44O, the main research area is vitamin D receptor antagonist MeTC7 antitumor.

Vitamin-D receptor (VDR) mRNA is overexpressed in neuroblastoma and carcinomas of lung, pancreas, and ovaries and predicts poor prognoses. VDR antagonists may be able to inhibit tumors that overexpress VDR. However, the current antagonists are arduous to synthesize and are only partial antagonists, limiting their use. Here, we show that the VDR antagonist MeTC7 (5)(I), which can be synthesized from 7-dehydrocholesterol (6) in two steps, inhibits VDR selectively, suppresses the viability of cancer cell-lines, and reduces the growth of the spontaneous transgenic TH-MYCN neuroblastoma and xenografts in vivo. The VDR selectivity of 5 against RXRα and PPAR-γ was confirmed, and docking studies using VDR-LBD indicated that 5 induces major changes in the binding motifs, which potentially result in VDR antagonistic effects. These data highlight the therapeutic benefits of targeting VDR for the treatment of malignancies and demonstrate the creation of selective VDR antagonists that are easy to synthesize.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 434-16-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C27H44O, Formula: C27H44O.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Bryan, Arielle M.; You, Jeehyun Karen; Li, Guangtao; Kim, JiHyun; Singh, Ashutosh; Morstein, Johannes; Trauner, Dirk; Pereira de Sa, Nivea; Normile, Tyler G.; Farnoud, Amir M.; London, Erwin; Del Poeta, Maurizio published the artcile< Cholesterol and sphingomyelin are critical for Fcγ receptor-mediated phagocytosis of Cryptococcus neoformans by macrophages>, Name: (3S,9S,10R,13R,14R,17R)-10,13-Dimethyl-17-((R)-6-methylheptan-2-yl)-2,3,4,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol, the main research area is Cryptococcus macrophage phagocytosis cholesterol sphingomyelin Fcgamma receptor; Fc-gamma receptor; cholesterol; fungi; lipid raft; macrophage; phagocytosis; sphingomyelin.

Cryptococcus neoformans is a fungal pathogen that causes life-threatening meningoencephalitis in lymphopenic patients. Pulmonary macrophages comprise the first line of host defense upon inhalation of fungal spores by aiding in clearance but can also potentially serve as a niche for their dissemination. Given that macrophages play a key role in the outcome of a cryptococcal infection, it is crucial to understand factors that mediate phagocytosis of C. neoformans. Since lipid rafts (high-order plasma membrane domains enriched in cholesterol and sphingomyelin [SM]) have been implicated in facilitating phagocytosis, we evaluated whether these ordered domains govern macrophages ability to phagocytose C. neoformans. We found that cholesterol or SM depletion resulted in significantly deficient IgG (IgG)-mediated phagocytosis of fungus. Moreover, repletion of macrophage cells with a raft-promoting sterol (7-dehydrocholesterol) rescued this phagocytic deficiency, whereas a raft-inhibiting sterol (coprostanol) significantly decreased IgG-mediated phagocytosis of C. neoformans. Using a photoswitchable SM (AzoSM), we observed that the raft-promoting conformation (trans-AzoSM) resulted in efficient phagocytosis, whereas the raft-inhibiting conformation (cis-AzoSM) significantly but reversibly blunted phagocytosis. We observed that the effect on phagocytosis may be facilitated by Fcγ receptor (FcγR) function, whereby IgG immune complexes crosslink to FcγRIII, resulting in tyrosine phosphorylation of FcR γ-subunit (FcRγ), an important accessory protein in the FcγR signaling cascade. Correspondingly, cholesterol or SM depletion resulted in decreased FcRγ phosphorylation. Repletion with 7-dehydrocholesterol restored phosphorylation, whereas repletion with coprostanol showed FcRγ phosphorylation comparable to unstimulated cells. Together, these data suggest that lipid rafts are critical for facilitating FcγRIII-mediated phagocytosis of C. neoformans.

Journal of Biological Chemistry published new progress about Cryptococcus neoformans. 434-16-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C27H44O, Name: (3S,9S,10R,13R,14R,17R)-10,13-Dimethyl-17-((R)-6-methylheptan-2-yl)-2,3,4,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Sofferman, Danielle L.; Konar, Arkaprabha; Spears, Kenneth G.; Sension, Roseanne J. published the artcile< Ultrafast excited state dynamics of provitamin D3 and analogs in solution and in lipid bilayers>, Computed Properties of 434-16-2, the main research area is dynamic provitamin lipid bilayer.

The photochem. ring-opening reaction of 7-dehydrocholesterol (DHC, provitamin D3) is responsible for the light-initiated formation of vitamin D3 in mammalian skin membranes. Visible transient absorption spectroscopy was used to explore the excited state dynamics of DHC and two analogs: ergosterol (provitamin D2) and DHC acetate free in solution and confined to lipid bilayers chosen to model the biol. cell membrane. In solution, the excited state dynamics of the three compounds are nearly identical. However, when confined to lipid bilayers, the heterogeneity of the lipid membrane and packing forces imposed on the mol. by the lipid alter the excited state dynamics of these compounds When confined to lipid bilayers in liposomes formed using DPPC, two solvation environments are identified. The excited state dynamics for DHC and analogs in fluid-like regions of the liposome membrane undergo internal conversion and ring-opening on 1 ps-2 ps time scales, similar to those observed in isotropic solution In contrast, the excited state lifetime of a subpopulation in regions of lower fluidity is 7 ps-12 ps. The long decay component is unique to these liposomes and results from the structural properties of the lipid bilayer. Addnl. measurements in liposomes prepared with lipids having slightly longer or shorter alkane tails support this conclusion. In the lipid environments studied, the longest lifetimes are observed for DHC. The unsaturated sterol tail of ergosterol and the acetate group of DHC acetate disrupt the packing around the mol. and permit faster internal conversion and relaxation back to the ground state. (c) 2021 American Institute of Physics.

Journal of Chemical Physics published new progress about Bilayer biological membrane (lipid). 434-16-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C27H44O, Computed Properties of 434-16-2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Sandberg-Gertzen, H.; Ryde, M.; Jaernerot, G. published the artcile< Absorption and excretion of azodisal sodium and its metabolites in man after rectal administration of a single 2-g dose>, Safety of Sodium 5,5′-(diazene-1,2-diyl)bis(2-hydroxybenzoate), the main research area is azodisal sodium pharmacokinetics.

The behavior of azodisal sodium (ADS)(I) [6054-98-4] and its metabolites after a single 2-g rectal dose was investigated in 10 healthy volunteers. Blood samples were drawn frequently, and urine was collected during intervals of 24 h. The ADS absorption gave a mean peak serum concentration of 2.1 μg/mL. The urinary excretion of ADS was 0.8% of the given dose. After rectal administration, 5-aminosalicylic acid (5-ASA) [89-57-6] could be detected in the serum only in 2 of the subjects, with a mean concentration of <0.5 μg/mL. N-Acetyl-5-aminosalicylic acid  [51-59-2] was present in increasing serum concentrations, being 0.93 μg/mL at 24 h. The mean 24-h urinary excretion of these 2 metabolites was only 2.7% of the given dose. In another study, the azo bond of ADS has been shown to be split by anaerobic and aerobic bacteria. The low absorption of its metabolites indicates that ADS is a suitable mol. for delivering the presumed pharmacol. active moiety, 5-ASA. Scandinavian Journal of Gastroenterology published new progress about Rectum. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Safety of Sodium 5,5′-(diazene-1,2-diyl)bis(2-hydroxybenzoate).

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts