Month: December 2022

Bhattacherjee, Abhishek published the artcileArgpyrimidine-tagged rutin-encapsulated biocompatible (ethylene glycol dimers) nanoparticles: Application for targeted drug delivery in experimental diabetes (Part 2), Related Products of alcohols-buliding-blocks, the publication is International Journal of Pharmaceutics (Amsterdam, Netherlands) (2017), 528(1-2), 8-17, database is CAplus and MEDLINE.

Diabetes mellitus is characterized by hyperglycemia and associated complications. However, long-term diabetes control is not often sustained by currently available therapeutic approaches. Research on nanoparticle-mediated drug delivery systems is in progress. Here we have tested a ligand (argpyrimidine)-tagged drug (rutin)-encapsulated biocompatible (ethylene glycol dimers) nanoparticle for targeted drug delivery in streptozotocin-induced diabetic rats. Argpyrimidine, being an advanced glycation end product (AGE), directs the nanoparticles to interact with cell surface receptors of AGEs (RAGE) and delivers the drug into the cells. The bioflavonoid rutin possesses antihyperglycemic property, and has been used for nanocapsulation. Two doses of nanoparticles containing 20 mg rutin/kg body weight were administered (i.v. at 7 days interval) into streptozotocin-induced diabetic rats. Compared to free rutin, nanoparticle treatment appears to be significantly more effective in controlling the diabetogenic effects – hyperglycemia, hyperlipidemia, oxidative stress, etc, including heart-associated complications. This approach may thus be explored for drug delivery in the treatment of diabetes mellitus.

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, Related Products of alcohols-buliding-blocks.

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

Prommaban, Adchara published the artcileMicroemulsion of essential oils from citrus peels and leaves with anti-aging, whitening, and irritation reducing capacity, SDS of cas: 106-25-2, the publication is Journal of Drug Delivery Science and Technology (2022), 103188, database is CAplus.

Although citrus essential oil is frequently used in cosmetics as fragrance, the biol. activities related to skin benefits have been rarely investigated. This study aimed to investigate the anti-skin aging and anti-melanogenic effects of citrus oils and develop microemulsion system to reduce the irritation capacity of citrus oils. Oils from leaves and fruit peels of Citrus aurantifolia (Christm.) Swing and Citrus reticulata Blanco cv.Shogun were from hydro-distillation Their chem. composition was analyzed using gas chromatog./mass spectrometry. Antioxidant activities were determined in terms of free radical scavenging activities, ferric reducing antioxidant power, and lipid peroxidation inhibition. Anti-aging and anti-melanogenic activities were investigated using related enzyme activity anal. Oils with the most potent biol. activities were selected for further incorporation into microemulsion. The irritation capacity of native and citrus microemulsion were investigated in human volunteers. Citrus oils comprised a range of chems., with limonene being a key component. All citrus oils demonstrated powerful antioxidative activities. C. reticulata dried peel oil significantly inhibited collagenase and tyrosinase activities, resulting in promising anti-aging and whitening properties. C. reticulata oil derived from dried peels (CR3) had a higher yield and more potent activity than the oils taken from fresh leaves and peels. Therefore, CR3 was developed into a microemulsion in which the internal droplet size was 266.5 ± 14.1 nm and the narrowest PDI of 0.396 ± 0.068. Microemulsion could significantly reduce the skin irritation property of CR3 in human volunteers. In conclusion, CR3 microemulsion was suggested as effective and safe for further cosmeceutical applications.

Journal of Drug Delivery Science and Technology published new progress about 106-25-2. 106-25-2 belongs to alcohols-buliding-blocks, auxiliary class Natural product, name is cis-3,7-Dimethyl-2,6-Octadien-1-Ol, and the molecular formula is C10H18O, SDS of cas: 106-25-2.

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

Dubreuil, Anne-Claire published the artcileUnderstanding the impact of silicon compounds on metallic catalysts through experiments and multi-technical analysis, SDS of cas: 597-52-4, the publication is Comptes Rendus Chimie (2017), 20(1), 55-66, database is CAplus.

The presence of silicon in petroleum products is a major issue due to its poisoning effect on catalysts. The aim of this work is to combine silicon speciation and poisoning tests. Cyclic siloxanes were the main silicon species found in petroleum products. Other silicon compounds, comprising reactive groups (hydroxy, methoxy and hydroperoxy), were also recovered but at trace levels using GC-ICP/MS. Five well-chosen silicon compounds were used to poison Pd/alumina catalysts. Only dimethoxydimethylsilane poisons Pd-catalysts while polydimethylsiloxane (PDMS) has no effect on their activities in buta-1,3-diene hydrogenation. Unexpectedly, triethylsilane, triethylsilanol and even octamethylcyclotetrasiloxane (D₄) exhibit a promoting effect. An interpretation of the phenomena based on various characterizations is proposed.

Comptes Rendus Chimie published new progress about 597-52-4. 597-52-4 belongs to alcohols-buliding-blocks, auxiliary class Aliphatic Chain, name is Triethylsilanol, and the molecular formula is C6H16OSi, SDS of cas: 597-52-4.

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

Du, Boyu published the artcileEffective fractionation strategy of sugarcane bagasse lignin to fabricate quality lignin-based carbon nanofibers supercapacitors, Application of 4-Propylphenol, the publication is International Journal of Biological Macromolecules (2021), 604-617, database is CAplus and MEDLINE.

Lignin is recommended to a tempting alternative precursor of petroleum for fabricating carbon nanofibers (CNFs) due to its high carbon content, low-cost and renewable resources. However, the property of lignin-based carbon nanofibers (LCNFs) is inferior owing to the heterogeneity and 3D-network structure of lignin, which hinders its application in supercapacitors. The latest developments in fractionation technol. have shown great potential for overcoming the aforementioned shortcomings. However, most of fractionation methods mainly rely on expensive chems. and complex reaction process, such as enzymes, multiple solvents, membranes, and dialysis tubes. Herein, we proposed a controllable and effective strategy to fractionate lignin by only changing the ratio of ethanol/water (V/V) as mixture solvent. This gradient extraction method effectively removed the part of lignin with small mol. and branching structure, thus selectively getting the fractionated lignin with high mol. weight, narrow polydispersity index, and good linear structure. Fortunately, when the ratio of ethanol/water was 6:4, the corresponding LCNFs (LCNFs-L60) was obtained with large sp. surface area, independent filamentous morphol. networks and excellent electrochem. property. Its specific capacitance was up to 405.8 F/g. This way features controllable and sustainable for preparing high-quality LCNFs supercapacitors.

International Journal of Biological Macromolecules published new progress about 645-56-7. 645-56-7 belongs to alcohols-buliding-blocks, auxiliary class Liquid Crystal &OLED Materials, name is 4-Propylphenol, and the molecular formula is C9H12O, Application of 4-Propylphenol.

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

Brufani, Mario published the artcileSynthesis of phenothiazine derivatives as potential inhibitors of phospholipase C, Recommanded Product: 2-(Benzyl(methyl)amino)ethanol, the publication is Farmaco (1992), 47(5), 585-97, database is CAplus and MEDLINE.

In order to study the structure-activity relationships of phenothiazine derivatives (I, e.g., R = H, Cl, or CF₃, NHR¹R² = Me₂NH, EtNH₂, morpholino, methylpiperazino, dicyclohexylamino) inhibiting phosphatidylinositol-specific phospholipase C (PI-PLC), the synthesis of some phenothiazine amide, amine and ester derivatives was performed mainly by reacting 10H-phenothiazine-10-propanoyl chloride with some amines and alcs.; the resulting amides were reduced with borane to yield the corresponding amines. Starting from 2-chloro and 2-trifluoromethyl-10H-phenothiazine-10-propanoyl chloride two amides were synthesized. The inhibiting activity on PI-PLC from human platelets is reported. Structure-activity relations are discussed.

Farmaco published new progress about 101-98-4. 101-98-4 belongs to alcohols-buliding-blocks, auxiliary class Amine,Benzene,Alcohol, name is 2-(Benzyl(methyl)amino)ethanol, and the molecular formula is C10H15NO, Recommanded Product: 2-(Benzyl(methyl)amino)ethanol.

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

Hamala, Vojtech published the artcileThe effect of deoxyfluorination and O-acylation on the cytotoxicity of N-acetyl-D-gluco- and D-galactosamine hemiacetals, Application of 2-Phenylethanethiol, the publication is Organic & Biomolecular Chemistry (2021), 19(20), 4497-4506, database is CAplus and MEDLINE.

Fully acetylated deoxyfluorinated hexosamine analogs and non-fluorinated 3,4,6-tri-O-acylated N-acetyl-hexosamine hemiacetals have previously been shown to display moderate anti-proliferative activity. We prepared a set of deoxyfluorinated GlcNAc and GalNAc hemiacetals that comprised both features: O-acylation at the non-anomeric positions with an acetyl, propionyl and butanoyl group, and deoxyfluorination at selected positions. Determination of the in vitro cytotoxicity towards the MDA-MB-231 breast cancer and HEK-293 cell lines showed that deoxyfluorination enhanced cytotoxicity in most analogs. Increasing the ester alkyl chain length had a variable effect on the cytotoxicity of fluoro analogs, which contrasted with non-fluorinated hemiacetals where butanoyl derivatives had always higher cytotoxicity than acetates. Reaction with 2-phenylethanethiol indicated that the recently described S-glyco-modification is an unlikely cause of cytotoxicity.

Organic & Biomolecular Chemistry published new progress about 4410-99-5. 4410-99-5 belongs to alcohols-buliding-blocks, auxiliary class Thiol,Benzene, name is 2-Phenylethanethiol, and the molecular formula is C8H10S, Application of 2-Phenylethanethiol.

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

Cheuka, Peter Mubanga published the artcileNew Amidated 3,6-Diphenylated Imidazopyridazines with Potent Antiplasmodium Activity Are Dual Inhibitors of Plasmodium Phosphatidylinositol-4-kinase and cGMP-Dependent Protein Kinase, Name: 2-Aminobutan-1-ol, the publication is ACS Infectious Diseases (2021), 7(1), 34-46, database is CAplus and MEDLINE.

Recent studies on 3,6-diphenylated imidazopyridazines have demonstrated impressive in vitro activity and in vivo efficacy in mouse models of malaria infection. Herein, we report the synthesis and antiplasmodium evaluation of a new series of amidated analogs and demonstrate that these compounds potently inhibit Plasmodium phosphatidylinositol-4-kinase (PI4K) type IIIβ while moderately inhibiting cyclic guanidine monophosphate (cGMP)-dependent protein kinase (PKG) activity in vitro. Using in silico docking, we predict key binding interactions for these analogs within the ATP (ATP)-binding site of PI4K and PKG, paving the way for structure-based optimization of imidazopyridazines targeting both Plasmodium PI4K and PKG. While several derivatives showed low nanomolar antiplasmodium activity (IC₅₀ < 100 nM), some compounds, including piperazine analog I, resulted in strong dual PI4K and PKG inhibition. The compounds also demonstrated transmission-blocking potential, evident from their potent inhibition of early- and late-stage gametocytes. Finally, the current compounds generally showed improved aqueous solubility and reduced hERG (human ether-a-go-go-related gene) channel inhibition.

ACS Infectious Diseases published new progress about 96-20-8. 96-20-8 belongs to alcohols-buliding-blocks, auxiliary class Amine,Aliphatic hydrocarbon chain,Alcohol, name is 2-Aminobutan-1-ol, and the molecular formula is C4H11NO, Name: 2-Aminobutan-1-ol.

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

Semiz, Gurkan published the artcileChemical characterization of essential oil of local endemic Lamium Bilgilii Celep (Lamiaceae), Category: alcohols-buliding-blocks, the publication is Comptes Rendus de l’Academie Bulgare des Sciences (2022), 75(1), 34-42, database is CAplus.

In this study, the chem. constitution of the essential oil of Lamium bilgilii Celep, a local endemic species of Turkey, was studied by GC-MS for the first time. The essential oil was obtained by hydrodistillation method and forty-three compounds were successfully identified representing 98.2% of the oil. Bicyclogermacrene (14.22%) and linalyl acetate (8.33%) and linalool (7.86%) were the most abundant components of the essential oil. L. bilgilii essential oil was rich in sesquiterpenes (35.8%) and oxygenated monoterpenes (26.6%). The results showed that bicyclogermacrene was found, for the first time, as a most abundant component in the Lamium oils.

Comptes Rendus de l’Academie Bulgare des Sciences published new progress about 106-25-2. 106-25-2 belongs to alcohols-buliding-blocks, auxiliary class Natural product, name is cis-3,7-Dimethyl-2,6-Octadien-1-Ol, and the molecular formula is C7H5Cl2NO, Category: alcohols-buliding-blocks.

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

Ionescu, Andrei C. published the artcileSubstituted Nano-Hydroxyapatite Toothpastes Reduce Biofilm Formation on Enamel and Resin-Based Composite Surfaces, Category: alcohols-buliding-blocks, the publication is Journal of Functional Biomaterials (2020), 11(2), 36, database is CAplus and MEDLINE.

Toothpastes containing nano-hydroxyapatite (n-HAp) substituted with metal ions provide calcium and phosphate ions to dental hard tissues, reducing demineralization, and promoting remineralization. Few data are available about the effect of these bioactive compounds on oral microbiota. This in vitro study evaluated the influence of two com.-available substituted n-HAp-based toothpastes α : Zn-carbonate substituted n-HAp; β: F, Mg, Sr-carbonate substituted (n-HAp) on early colonization (EC, 12 h) and biofilm formation (BF, 24 h) by oral microbiota. Controls were brushed with distilled water. Artificial oral microcosm and Streptococcus mutans biofilms were developed using human enamel and a resin-based composite (RBC) as adherence surfaces. Two test setups, a shaking multiwell plate and a modified drip-flow reactor (MDFR), were used to simulate clin. conditions during the night (low salivary flow and clearance) and daytime, resp. Energy-dispersive X-ray spectrometry (EDS) was used to evaluate specimens’ surfaces after toothpaste treatment. Fluoride release from β toothpaste was evaluated. Viable adherent biomass was quantified by MTT assay, and biofilms’ morphol. was highlighted using confocal microscopy. EDS showed the presence of remnants from the tested toothpastes on both adherence surfaces. β toothpaste showed significantly lower EC and BF compared to control using the artificial oral microcosm model, while α toothpaste showed lower EC and BF compared to control, but higher EC and BF compared to β toothpaste. The effect shown by β toothpaste was, to a minimal extent, due to fluoride release. Interestingly, this result was seen on both adherence surfaces, meaning that the tested toothpastes significantly influenced EC and BF even on RBC surfaces. Furthermore, the effect of toothpaste treatments was higher after 12 h than 24 h, suggesting that toothbrushing twice a day is more effective than brushing once. The efficacy of these treatments in reducing microbial colonization of RBC surfaces may represent a promising possibility in the prevention of secondary caries.

Journal of Functional Biomaterials published new progress about 70445-33-9. 70445-33-9 belongs to alcohols-buliding-blocks, auxiliary class Aliphatic Chain, name is 3-((2-Ethylhexyl)oxy)propane-1,2-diol, and the molecular formula is C11H24O3, Category: alcohols-buliding-blocks.

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

De Arriba, Alberto Fernandez published the artcileInhibition of cyclooxygenase-2 expression by 4-trifluoromethyl derivatives of salicylate, triflusal, and its deacetylated metabolite, 2-hydroxy-4-trifluoromethylbenzoic acid, HPLC of Formula: 328-90-5, the publication is Molecular Pharmacology (1999), 55(4), 753-760, database is CAplus.

The therapeutic potential of drugs that block the induction of cyclooxygenase-2 has been emphasized. When two 4-trifluoromethyl salicylate derivatives [2-acetoxy-4-trifluoromethylbenzoic acid (triflusal) and its deacetylated metabolite 2-hydroxy-4-trifluoromethylbenzoic acid (HTB)] were compared with aspirin and sodium salicylate as cyclooxygenase-2 (COX-2) inhibitors, we observed that in bacterial lipopolysaccharide-activated human blood, triflusal, aspirin, and HTB, but not sodium salicylate, inhibited COX-2-mediated prostaglandin E₂ (PGE₂) production (IC₅₀ = 0.16, 0.18, 0.39, and > 10 mM, resp.). However, only triflusal and aspirin inhibited purified COX-2 enzyme. To test this apparent discrepancy, we realized that HTB and triflusal (but neither aspirin nor salicylate) produced a concentration-dependent inhibition of COX-2 protein expression in peripheral human mononuclear cells. This observation was further confirmed in a rat air pouch model in vivo, in which both aspirin and triflusal inhibited PGE₂ production (ID₅₀ = 18.9 and 11.4 mg/kg p.o., resp.) but only triflusal-treated animals showed a decrease in COX-2 expression. This different behavior may be, at least in part, due to the ability of HTB and triflusal to block the activation of the transcription factor nuclear factor-κB to a higher extent than aspirin and sodium salicylate. Thus, in addition to inhibiting the COX-2 activity at therapeutic concentrations, triflusal is able to block through its metabolite HTB the expression of new enzyme, and hence the resumption of PGE₂ synthesis. Triflusal and HTB may exert beneficial effects in processes in which de novo COX-2 expression is involved and, in a broader sense, in pathol. situations in which genes under nuclear factor-κB control are up-regulated.

Molecular Pharmacology published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C8H5F3O3, HPLC of Formula: 328-90-5.

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