Month: December 2022

Bresciani, Letizia published the artcileIn vitro (poly)phenol catabolism of unformulated- and phytosome-formulated cranberry (Vaccinium macrocarpon) extracts, Recommanded Product: 3-Hydroxyphenylacetic acid, the publication is Food Research International (2021), 110137, database is CAplus and MEDLINE.

Cranberries (Vaccinium macrocarpon) represent an important source of anthocyanins, flavan-3-ols and flavonols. This study aimed at investigating in vitro the human microbial metabolism of (poly)phenols, principally flavan-3-ols, of unformulated- and phytosome-formulated cranberry extracts After powder characterization, a 24-h fermentation with human faecal slurries was performed, standardizing the concentration of incubated proanthocyanidins. Cranberry (poly)phenol metabolites were quantified by uHPLC-MS2 analyses. The native compounds of both unformulated- and phytosome-formulated cranberry extracts were metabolized under faecal microbiota activity, resulting in twenty-four microbial metabolites. Although some differences appeared when considering different classes of colonic metabolites, no significant differences in the total amount of metabolites were established after 24 h of incubation period. These results suggested that a different formulation had no effect on flavan-3-ol colonic metabolism of cranberry and both unformulated- and phytosome-formulated extract Both formulations displayed the capability to be a potential source of compounds which could lead to a wide array of gut microbiota metabolites in vitro.

Food Research International published new progress about 621-37-4. 621-37-4 belongs to alcohols-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Phenol,Natural product, name is 3-Hydroxyphenylacetic acid, and the molecular formula is C8H8O3, Recommanded Product: 3-Hydroxyphenylacetic acid.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Kuduk, Scott D. published the artcileDevelopment of Orally Bioavailable and CNS Penetrant Biphenylaminocyclopropane Carboxamide Bradykinin B₁ Receptor Antagonists, Product Details of C6H13BO3, the publication is Journal of Medicinal Chemistry (2007), 50(2), 272-282, database is CAplus and MEDLINE.

A series of biphenylaminocyclopropane carboxamide based bradykinin B₁ receptor antagonists has been developed that possesses good pharmacokinetic properties and is CNS penetrant. Discovery that the replacement of the trifluoropropionamide in the lead structure with polyhaloacetamides, particularly a trifluoroacetamide, significantly reduced P-glycoprotein mediated efflux for the series proved essential. One of these novel bradykinin B₁ antagonists (13b) also exhibited suitable pharmacokinetic properties and efficient ex vivo receptor occupancy for further development as a novel approach for the treatment of pain and inflammation.

Journal of Medicinal Chemistry published new progress about 25240-59-9. 25240-59-9 belongs to alcohols-buliding-blocks, auxiliary class Boronic acid and ester,Boronic Acids,Boronate Esters, name is 4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-ol, and the molecular formula is C6H13BO3, Product Details of C6H13BO3.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

D’Amato, Alfonsina published the artcileFaecal microbiota transplant from aged donor mice affects spatial learning and memory via modulating hippocampal synaptic plasticity- and neurotransmission-related proteins in young recipients, Recommanded Product: 3-Hydroxyphenylacetic acid, the publication is Microbiome (2020), 8(1), 140, database is CAplus and MEDLINE.

The gut-brain axis and the intestinal microbiota are emerging as key players in health and disease. Shifts in intestinal microbiota composition affect a variety of systems; however, evidence of their direct impact on cognitive functions is still lacking. We tested whether faecal microbiota transplant (FMT) from aged donor mice into young adult recipients altered the hippocampus, an area of the central nervous system (CNS) known to be affected by the ageing process and related functions. Young adult mice were transplanted with the microbiota from either aged or age-matched donor mice. Following transplantation, characterization of the microbiotas and metabolomics profiles along with a battery of cognitive and behavioral tests were performed. Label-free quant. proteomics was employed to monitor protein expression in the hippocampus of the recipients. We report that FMT from aged donors led to impaired spatial learning and memory in young adult recipients, whereas anxiety, explorative behavior and locomotor activity remained unaffected. This was paralleled by altered expression of proteins involved in synaptic plasticity and neurotransmission in the hippocampus. Also, a strong reduction of bacteria associated with short-chain fatty acids (SCFAs) production (Lachnospiraceae, Faecalibaculum, and Ruminococcaceae) and disorders of the CNS (Prevotellaceae and Ruminococcaceae) was observed Finally, the detrimental effect of FMT from aged donors on the CNS was confirmed by the observation that microglia cells of the hippocampus fimbria, acquired an ageing-like phenotype; on the contrary, gut permeability and levels of systemic and local (hippocampus) cytokines were not affected. These results demonstrate that age-associated shifts of the microbiota have an impact on protein expression and key functions of the CNS. Furthermore, these results highlight the paramount importance of the gut-brain axis in ageing and provide a strong rationale to devise therapies aiming to restore a young-like microbiota to improve cognitive functions and the declining quality of life in the elderly.

Microbiome published new progress about 621-37-4. 621-37-4 belongs to alcohols-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Phenol,Natural product, name is 3-Hydroxyphenylacetic acid, and the molecular formula is C8H8O3, Recommanded Product: 3-Hydroxyphenylacetic acid.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Bhattacherjee, Abhishek published the artcileArgpyrimidine-tagged rutin-encapsulated biocompatible (ethylene glycol dimers) nanoparticles: Synthesis, characterization and evaluation for targeted drug delivery, Recommanded Product: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, the publication is International Journal of Pharmaceutics (Amsterdam, Netherlands) (2016), 509(1-2), 507-517, database is CAplus and MEDLINE.

Diabetes mellitus represents a major metabolic disorder affecting millions of people all over the world. Currently available therapeutic treatments are not good enough to control the long-term complications of diabetes. Active targeting via inclusion of a specific ligand on the nanoparticles provides effective therapeutic approach in different diseases. However, such specific drug delivery systems have not been explored much in diabetes due to lack of suitable biol. targets in this disorder. Our objective is to synthesize a ligand-tagged drug-loaded nanoparticle for delivery of the drug at specific sites to enhance its therapeutic efficiency in diabetic condition. The nanoparticles have been prepared by using biocompatible ethylene glycol-bis (succinic acid N-hydroxysuccinimide ester) dimers. Although advanced glycation end products (AGEs) are the root causes of diabetic complications, argpyrimidine, an AGE, possesses antioxidant and reducing activities. AGE interacts selectively with its cell surface receptors (RAGE), which are significantly increased in diabetic condition. We have selected RAGE as the target of argpyrimidine, which is tagged on the nanoparticles as a ligand. Rutin, having anti-hyperglycemic and anti-glycating activities, has been used for nanoencapsulation. Rutin-loaded argpyrimidine-tagged nanoparticles have been synthesized and characterized. We have demonstrated the drug releasing capacity and target specificity of the synthesized drug delivery system under ex vivo and in vivo conditions.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C18H20N2O12, Recommanded Product: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Poddar, Sailendra N. published the artcileSpectrophotometric determination of vanadium with Schiff’s base derived from 1-amino-8-hydroxynaphth-3,6-disulfonic acid and salicylaldehyde, SDS of cas: 5941-07-1, the publication is Indian Journal of Chemistry (1966), 4(8), 371-2, database is CAplus.

A spectrophotometric method for the determination of 0.000168 g. V/ml. is described. The method is based on the formation of a reddish yellow-colored complex when a solution containing VO3- is added to an aqueous solution of Schiff’s base (I) derived from o-HOC6H4-CHO and mono-Na 1-amino-2-hydroxynaphthalene-3,6-disulfonate (II) at pH 4.22-9.1. The color [λmax. 420 mμ and sensitivity 0.0048 γ V/cm.2] of the complex is quite stable and obeyed Beer’s law over a wide range (1.34-13.40 ppm.) of VO3- concentration By using Job’s method of continuous variation, a metal-ligand ratio of 1:2 is found. Halides, NO3-, NO2-, SO42-, WO42-, MoO42-, PO43-, citrate, OAc-, C2O42-, F-, alkali metals, and alk. earth metals do not interfere with the estimation when present at ±550 ppm. I was prepared by refluxing a mixture of II and o-OHC6H4CHO on water-bath for 2 hrs.; the mixture is left over night and the separated I is washed with dilute EtOH and dried (CaCl2).

Indian Journal of Chemistry published new progress about 5941-07-1. 5941-07-1 belongs to alcohols-buliding-blocks, auxiliary class Salt,Benzene,Naphthalene,Phenol,Inhibitor, name is 8-Hydroxy-1-(salicylideneamino)naphthalene-3,6-disulfonic acid monosodium Salt, and the molecular formula is C17H12NNaO8S2, SDS of cas: 5941-07-1.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Poddar, S. N. published the artcileSpectrophotometric determination of thorium(IV) with the Schiff base derived from 1-amino-8-naphthol-3,6-disulfonic acid and salicylaldehyde, Name: 8-Hydroxy-1-(salicylideneamino)naphthalene-3,6-disulfonic acid monosodium Salt, the publication is Indian Journal of Chemistry (1965), 3(9), 407-8, database is CAplus.

A spectrophotometric method for the determination of 0.0003913 g. Th/ml. solution is described. Th⁴⁺ gives a red color with the Schiff base (I) derived from ο-HOC₆H₄CHO and 1-amino-8-naphtnol-3,6-disulfonic acid (mono-Na salt) at pH 3.2-5.2. The color (450 mμ; sensitivity 0.032 γ Th/cm.²) of the complex is stable and obeys Beer’s law over 1 to 95 ppm. Th. A mixture of 10 ml. 10% aqueous Th(NO₃)₄ and 15 ml. 10% I was heated to give a red solution This on treatment with a few drops of aqueous KOH produced a bright red precipitate of the Th-I complex (II), which was filtered, washed with aqueous alc. and dried. II was soluble in H₂O, but insoluble in EtOH, Me₂CO, CHCl₃, and Et₂O. On heating with alk. solution, II decomposed to form hydrated ThO₂. The composition of II was Th(SB)₂, where SBH₂ is a mol. of I. Cl^–, Br^–, I^–, NO₃^–, Na⁺, K⁺, alk. earth metals, Cu(II), Co(II), Hg(II), Pd(II), Zn(II), Al(III), Mn(II), Cr(III), and U have no effect on the color system. SO₄^— tungstate, citrate, PO₄^—, Ac^–, OAc^–, and C₂O₄^— do not interfere when present in small quantities but lower the intensity of the color when present in large excess. Fe(III) interferes due to the formation of a violet color but Fe(II) does not. Interference due to Fe(III) can be avoided by reducing it by passing the solution through a Jones reductor and then developing the color with Th. F^– bleaches the Th-reagent color quant. VO₃^–, CrO₄^—, and Fe(III) form colored products with the reagent and should be removed beforehand.

Indian Journal of Chemistry published new progress about 5941-07-1. 5941-07-1 belongs to alcohols-buliding-blocks, auxiliary class Salt,Benzene,Naphthalene,Phenol,Inhibitor, name is 8-Hydroxy-1-(salicylideneamino)naphthalene-3,6-disulfonic acid monosodium Salt, and the molecular formula is C17H12NNaO8S2, Name: 8-Hydroxy-1-(salicylideneamino)naphthalene-3,6-disulfonic acid monosodium Salt.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Chowdhury, Amiya K. Roy published the artcileR.S.(P), a new isolate from the root of Rauwolfia serpentina, Application of N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, the publication is Indian Medical Journal (1964), 58(12), 241-52, database is CAplus.

The pharmacol. actions of a nonalkaloidal fraction isolated from the root of R. serpentina are given. This fraction, R.S.(P), was less potent than reserpine but equipotent to Rauwolfia total extract (1%) in lowering the blood pressure in anesthetized cats. In suitable doses it increased the pentobarbital sleeping time, reduced the spontaneous motility, postponed Metrazol convulsion and lethality, and affected the conditioned behavior in rats (maze test). Coordinated muscular movements were least affected, except when very high doses were used. Electroencephalogram studies in unanesthetized rabbits revealed considerable slowing of the brain wave pattern with the calming and quieting effect on the animals. Sometimes behavioral nonreactivity was seen. The drug appeared to have a central site of action. Its action differed from that of reserpine in many respects. It may possibly be used as an antihypertensive and anticonvulsant or sedative agent.

Indian Medical Journal published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, Application of N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Saxena, A. K. published the artcileModelling the binding affinity of steroids to zebrafish sex hormone-binding globulin, Synthetic Route of 1139-46-4, the publication is SAR and QSAR in Environmental Research (2014), 25(5), 407-421, database is CAplus and MEDLINE.

The circulating endogenous steroids are transported in the bloodstream. These are bound to a highly specific sex hormone-binding globulin (SHBG) and in lower affinity to proteins such as the corticosteroid-binding protein and albumin in vertebrates, including fish. It is generally believed that the glycoprotein SHBG protects these steroids from rapid metabolic degradation and thus intervenes in its availability at the target tissues. Endocrine disrupters binding to SHBG affect the normal activity of natural steroids. Since xenobiotics are primarily released in the aquatic environment, there is a need to evaluate the binding affinity of xenosteroid mimics on fish SHBG, especially in zebrafish (Danio rerio), a small freshwater fish originating in India and widely employed in ecotoxicol., toxicol., and genetics. In this context, a zebrafish SHBG (zfSHBG) homol. model was developed using the human SHBG (hSHBG) receptor structure as template. It was shown that interactions with amino acids Ser-36, Asp-59 and Thr-54 were important for binding affinity. A ligand-based pharmacophore model was also developed for both zfSHBG and hSHBG inhibitors that differentiated binders from non-binders, but also demonstrated structural requirements for zfSHBG and hSHBG ligands. The study provides insights into the mechanism of action of endocrine disruptors in zebrafish as well as providing a useful tool for identifying anthropogenic compounds inhibiting zfSHBG.

SAR and QSAR in Environmental Research published new progress about 1139-46-4. 1139-46-4 belongs to alcohols-buliding-blocks, auxiliary class Benzene,Phenol, name is 4-(2,4,4-Trimethylpentan-2-yl)benzene-1,2-diol, and the molecular formula is C14H22O2, Synthetic Route of 1139-46-4.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Spell, Mark L. published the artcileA Visible-Light-Promoted O-Glycosylation with a Thioglycoside Donor, Quality Control of 85618-21-9, the publication is Angewandte Chemie, International Edition (2016), 55(22), 6515-6519, database is CAplus and MEDLINE.

Visible-light irradiation of 4-p-methoxyphenyl-3-butenylthioglucoside donors in the presence of Umemoto’s reagent and alc. acceptors serves as a mild approach to O-glycosylation. Visible-light photocatalysts are not required for activation, and alkyl- and arylthioglycosides not bearing the p-methoxystyrene are inert to these conditions. Exptl. and computational evidence for an intervening electron donor-acceptor complex, which is necessary for reactivity, is provided. Yields with primary, secondary, and tertiary alc. acceptors range from moderate to high. Complete β-selectivity can be attained through neighboring-group participation.

Angewandte Chemie, International Edition published new progress about 85618-21-9. 85618-21-9 belongs to alcohols-buliding-blocks, auxiliary class Tetrahydropyran,Chiral,sulfides,Alcohol, name is (2R,3S,4S,5R,6S)-2-(Hydroxymethyl)-6-(octylthio)tetrahydro-2H-pyran-3,4,5-triol, and the molecular formula is C8H7N3, Quality Control of 85618-21-9.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Shi, An-Guo published the artcilePrecoupling of alpha-2B adrenergic receptors and G-proteins in transfected PC-12 cell membranes: influence of pertussis toxin and a lysine-directed cross-linker, Synthetic Route of 70539-42-3, the publication is Journal of Pharmacology and Experimental Therapeutics (1994), 271(3), 1520-7, database is CAplus and MEDLINE.

The ability of pertussis toxin (PTX) pretreatment to alter the binding of [³H]rauwolscine (RAU) to alpha-2B adrenergic receptors expressed in PC12 cells was examined PTX caused a 30% increase in the B_max for [³H]RAU and reduced its K_D, whereas in the added presence of Na⁺ and Gpp(NH)p binding was increased to 75% above the level in untreated membranes. Because all three agents act to reduce receptor/G-protein affinity, the increased binding may reflect extensive precoupling of the alpha-2B receptor. The affinity of the agonist epinephrine in displacing [³H]RAU was normally reduced by both Na⁺ and Gpp(NH)p; however, in PTX-treated membranes the effect of Gpp(NH)p was eliminated, and Na⁺ remained effective. The lysine-directed crosslinking reagent ethyleneglycol bis(succinimidyl)succinate (EGS) was utilized to cross-link precoupled receptor and G-protein. Maximal [³H]RAU binding was reduced by EGS in a time- and dose-dependent manner, and this action was reversed by prior incubation with Na⁺ and Gpp(NH)p, suggesting that EGS did indeed cross-link receptor and G-protein. RAU and epinephrine each provided protection against the effect of EGS. The inclusion of Na⁺ and Gpp(NH)p during [³H]RAU binding studies was able to restore maximal binding in EGS-treated membranes to the same level as untreated membranes. These results indicate that in the absence of Na⁺ and Gpp(NH)p at least 40% of the total alpha-2B adrenergic receptors in these membranes exist as a precoupled receptor/G-protein complex which fails to bind [³H]RAU.

Journal of Pharmacology and Experimental Therapeutics published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C25H47NO8, Synthetic Route of 70539-42-3.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts