Month: December 2022

Batista, Ellencristina Silva published the artcileOmega-3 mechanism of action in inflammation and endoplasmic reticulum stress in mononuclear cells from overweight non-alcoholic fatty liver disease participants: study protocol for the “”Brazilian Omega Study”” (BROS)-a randomized controlled trial, SDS of cas: 111-11-5, the main research area is omega action mechanism inflammation endoplasmic reticulum stress; mononuclear cell overweight non alc fatty liver disease human; Endoplasmic reticulum stress; GPR120; Inflammation; NAFLD; Omega-3; Overweight.

The low-grade inflammation is pivotal in obesity and its comorbidities; however, the inflammatory proteins are out of target for traditional drug therapy. Omega-3 (ω3) fatty acids can modulate the downstream signaling of Toll-like receptor (TLR) and tumor necrosis factor-α receptor (TNFα) through GPR120, a G-protein-coupled receptor, a mechanism not yet elucidated in humans. This work aims to investigate if the ω3 supplementation, at a feasible level below the previously recommended level in the literature, is enough to disrupt the inflammation and endoplasmic reticulum stress (ER-stress), and also if in acute treatment (3 h) ω3 can activate the GPR120 in peripheral blood mononuclear cells (PBMC) and leukocytes from overweight non-alc. fatty liver disease (NAFLD) participants. The R270H variant of the Ffar4 (GPR120 gene) will also be explored about mol. responses and blood lipid profiles. A triple-blind, prospective clin. trial will be conducted in overweight men and women, aged 19-75 years, randomized into placebo or supplemented (2.2 g of ω3 [EPA+DHA]) groups for 28 days. For sample calculation, it was considered the variation of TNFα protein and a 40% dropout rate, obtaining 22 individuals in each group. Volunteers will be recruited among patients with NAFLD diagnosis. Anthropometric parameters, food intake, phys. activity, total serum lipids, complete fatty acid blood profile, and glycemia will be evaluated pre- and post-supplementation. In the PBMC and neutrophils, the protein content and gene expression of markers related to inflammation (TNFα, MCP1, IL1α, IL6, IL10, JNK, and TAK1), ER-stress (ATF1, ATF6, IRE1, XBP1, CHOP, eIF2α, eIF4, HSP), and ω3 pathway (GPR120, β-arrestin2, Tab1/2, and TAK1) will be evaluated using Western blot and RT-qPCR. Participants will be genotyped for the R270H (rs116454156) variant using the TaqMan assay. It is hypothesized that attenuation of inflammation and ER-stress signaling pathways in overweight and NAFLD participants will be achieved through ω3 supplementation through binding to the GPR120 receptor.

Trials published new progress about Activating transcription factor 6α Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 111-11-5 belongs to class esters-buliding-blocks, name is Methyl octanoate, and the molecular formula is C9H18O2, SDS of cas: 111-11-5.

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

Batista, Ellencristina Silva published the artcileOmega-3 mechanism of action in inflammation and endoplasmic reticulum stress in mononuclear cells from overweight non-alcoholic fatty liver disease participants: study protocol for the “”Brazilian Omega Study”” (BROS)-a randomized controlled trial, Recommanded Product: Methyl decanoate, the main research area is omega action mechanism inflammation endoplasmic reticulum stress; mononuclear cell overweight non alc fatty liver disease human; Endoplasmic reticulum stress; GPR120; Inflammation; NAFLD; Omega-3; Overweight.

The low-grade inflammation is pivotal in obesity and its comorbidities; however, the inflammatory proteins are out of target for traditional drug therapy. Omega-3 (ω3) fatty acids can modulate the downstream signaling of Toll-like receptor (TLR) and tumor necrosis factor-α receptor (TNFα) through GPR120, a G-protein-coupled receptor, a mechanism not yet elucidated in humans. This work aims to investigate if the ω3 supplementation, at a feasible level below the previously recommended level in the literature, is enough to disrupt the inflammation and endoplasmic reticulum stress (ER-stress), and also if in acute treatment (3 h) ω3 can activate the GPR120 in peripheral blood mononuclear cells (PBMC) and leukocytes from overweight non-alc. fatty liver disease (NAFLD) participants. The R270H variant of the Ffar4 (GPR120 gene) will also be explored about mol. responses and blood lipid profiles. A triple-blind, prospective clin. trial will be conducted in overweight men and women, aged 19-75 years, randomized into placebo or supplemented (2.2 g of ω3 [EPA+DHA]) groups for 28 days. For sample calculation, it was considered the variation of TNFα protein and a 40% dropout rate, obtaining 22 individuals in each group. Volunteers will be recruited among patients with NAFLD diagnosis. Anthropometric parameters, food intake, phys. activity, total serum lipids, complete fatty acid blood profile, and glycemia will be evaluated pre- and post-supplementation. In the PBMC and neutrophils, the protein content and gene expression of markers related to inflammation (TNFα, MCP1, IL1α, IL6, IL10, JNK, and TAK1), ER-stress (ATF1, ATF6, IRE1, XBP1, CHOP, eIF2α, eIF4, HSP), and ω3 pathway (GPR120, β-arrestin2, Tab1/2, and TAK1) will be evaluated using Western blot and RT-qPCR. Participants will be genotyped for the R270H (rs116454156) variant using the TaqMan assay. It is hypothesized that attenuation of inflammation and ER-stress signaling pathways in overweight and NAFLD participants will be achieved through ω3 supplementation through binding to the GPR120 receptor.

Trials published new progress about Activating transcription factor 6α Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 110-42-9 belongs to class esters-buliding-blocks, name is Methyl decanoate, and the molecular formula is C11H22O2, Recommanded Product: Methyl decanoate.

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

Alexpandi, Rajaiah published the artcileAnti-QS mediated anti-infection efficacy of probiotic culture-supernatant against Vibrio campbellii infection and the identification of active compounds through in vitro and in silico analyses, Recommanded Product: Methyl decanoate, the main research area is Vibrio campbellii infection probiotic culture supernatant active compound QS.

The main intent of the present study was to identify the novel anti-quorum sensing (anti-QS) compounds from probiotic product (Rhodomax) and assess their anti-infection effect of against Vibrio campbellii infection using tomato clownfish (Amphiprion frenatus). In this study, rhodomax probiotic-product was investigated for its active compounds’ prediction through in silico anal. Initially, anti-QS activity of probiotic-supernatant was authenticated by decrease in bioluminescence production of V. campbellii. As expected, the probiotic-supernatant effectively inhibited the biofilm formation, swimming motility, and hydrophobicity of V. campbellii at 20μg/mL concentration During in vivo trail with tomato clownfish, probiotic-supernatant (20 ppm) treatment showed a significant increase in the survival rates to the level of 88% against V. campbellii infection. Further, the reduced colonization of V. campbellii inside the probiotic-supernatant treated animals correlates the anti-infection activity. The histopathol. differences in tissue levels such as the gill, intestine, and kidney of infected and probiotic-supernatant treated animals were also support the in-vivo trial, which strongly revealed the disease protection of rhodomax-supernatant against V. campbellii infection. Notably, the docking anal. revealed that the anti-QS mediated anti-infection activity of rhodomax-supernatant against V. campbellii infection is accomplished by the presence of active metabolites such as,4-Dihydro-7-methoxy-2,2-dimethyl-2H-1-benzopyran-3,4-diol and Pyrrolo(1,2-a)pyrazine-1,4-dione, hexahydro-3-(1-methylethyl). Hence, we suggest that these two active metabolites could be the novel alternative agents to control V. campbellii-associated infections in aquaculture.

Biocatalysis and Agricultural Biotechnology published new progress about Amino acids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 110-42-9 belongs to class esters-buliding-blocks, name is Methyl decanoate, and the molecular formula is C11H22O2, Recommanded Product: Methyl decanoate.

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

Belouzard, Sandrine published the artcileClofoctol inhibits SARS-CoV-2 replication and reduces lung pathology in mice, Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is clofoctol antiviral agent SARSCoV2 replication therapy COVID19.

Drug repurposing has the advantage of shortening regulatory preclin. development steps. Here, we screened a library of drug compounds, already registered in one or several geog. areas, to identify those exhibiting antiviral activity against SARS-CoV-2 with relevant potency. Of the 1,942 compounds tested, 21 exhibited a substantial antiviral activity in Vero-81 cells. Among them, clofoctol, an antibacterial drug used for the treatment of bacterial respiratory tract infections, was further investigated due to its favorable safety profile and pharmacokinetic properties. Notably, the peak concentration of clofoctol that can be achieved in human lungs is more than 20 times higher than its IC50 measured against SARS-CoV-2 in human pulmonary cells. This compound inhibits SARS-CoV-2 at a post-entry step. Lastly, therapeutic treatment of human ACE2 receptor transgenic mice decreased viral load, reduced inflammatory gene expression and lowered pulmonary pathol. Altogether, these data strongly support clofoctol as a therapeutic candidate for the treatment of COVID-19 patients.

PLoS Pathogens published new progress about Animal gene Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study) (Ifi44). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Mhlongo, Msizi I. published the artcileProfiling of Volatile Organic Compounds from Four Plant Growth-Promoting Rhizobacteria by SPME-GC-MS: A Metabolomics Study, Safety of Methyl decanoate, the main research area is PGPR volatile organic compound metabolomics profiling SPME GCMS; metabolomics profiling; multivariate data analysis (MVDA); plant growth promoting rhizobacteria (PGPR); solid-phase micro-extraction gas chromatography mass spectrometry (SPME–GC–MS); volatile organic compounds (VOCs).

The rhizosphere microbiome is a major determinant of plant health. Plant-beneficial or plant growth-promoting rhizobacteria (PGPR) influence plant growth, plant development and adaptive responses, such as induced resistance/priming. These new eco-friendly choices have highlighted volatile organic compounds (biogenic VOCs) as a potentially inexpensive, effective and efficient substitute for the use of agrochems. Secreted bacterial VOCs are low mol. weight lipophilic compounds with a low b.p. and high vapor pressures. As such, they can act as short- or long-distance signals in the rhizosphere, affecting competing microorganisms and impacting plant health. In this study, secreted VOCs from four PGPR strains (Pseudomonas koreensis (N19), Ps. fluorescens (N04), Lysinibacillus sphaericus (T19) and Paenibacillus alvei (T22)) were profiled by solid-phase micro-extraction gas chromatog. mass spectrometry (SPME-GC-MS) combined with a multivariate data anal. Metabolomic profiling with chemometric analyses revealed novel data on the composition of the secreted VOC blends of the four PGPR strains. Of the 121 annotated metabolites, most are known as bioactives which are able to affect metabolism in plant hosts. These VOCs belong to the following classes: alcs., aldehydes, ketones, alkanes, alkenes, acids, amines, salicylic acid derivatives, pyrazines, furans, sulfides and terpenoids. The results further demonstrated the presence of species-specific and strain-specific VOCs, characterized by either the absence or presence of specific VOCs in the different strains. These mols. could be further investigated as biomarkers for the classification of an organism as a PGPR and selection for agricultural use.

Metabolites published new progress about Alcohols Role: ANT (Analyte), PUR (Purification or Recovery), ANST (Analytical Study), PREP (Preparation). 110-42-9 belongs to class esters-buliding-blocks, name is Methyl decanoate, and the molecular formula is C11H22O2, Safety of Methyl decanoate.

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

Mhlongo, Msizi I. published the artcileProfiling of Volatile Organic Compounds from Four Plant Growth-Promoting Rhizobacteria by SPME-GC-MS: A Metabolomics Study, Quality Control of 6259-76-3, the main research area is PGPR volatile organic compound metabolomics profiling SPME GCMS; metabolomics profiling; multivariate data analysis (MVDA); plant growth promoting rhizobacteria (PGPR); solid-phase micro-extraction gas chromatography mass spectrometry (SPME–GC–MS); volatile organic compounds (VOCs).

The rhizosphere microbiome is a major determinant of plant health. Plant-beneficial or plant growth-promoting rhizobacteria (PGPR) influence plant growth, plant development and adaptive responses, such as induced resistance/priming. These new eco-friendly choices have highlighted volatile organic compounds (biogenic VOCs) as a potentially inexpensive, effective and efficient substitute for the use of agrochems. Secreted bacterial VOCs are low mol. weight lipophilic compounds with a low b.p. and high vapor pressures. As such, they can act as short- or long-distance signals in the rhizosphere, affecting competing microorganisms and impacting plant health. In this study, secreted VOCs from four PGPR strains (Pseudomonas koreensis (N19), Ps. fluorescens (N04), Lysinibacillus sphaericus (T19) and Paenibacillus alvei (T22)) were profiled by solid-phase micro-extraction gas chromatog. mass spectrometry (SPME-GC-MS) combined with a multivariate data anal. Metabolomic profiling with chemometric analyses revealed novel data on the composition of the secreted VOC blends of the four PGPR strains. Of the 121 annotated metabolites, most are known as bioactives which are able to affect metabolism in plant hosts. These VOCs belong to the following classes: alcs., aldehydes, ketones, alkanes, alkenes, acids, amines, salicylic acid derivatives, pyrazines, furans, sulfides and terpenoids. The results further demonstrated the presence of species-specific and strain-specific VOCs, characterized by either the absence or presence of specific VOCs in the different strains. These mols. could be further investigated as biomarkers for the classification of an organism as a PGPR and selection for agricultural use.

Metabolites published new progress about Alcohols Role: ANT (Analyte), PUR (Purification or Recovery), ANST (Analytical Study), PREP (Preparation). 6259-76-3 belongs to class esters-buliding-blocks, name is Hexyl 2-hydroxybenzoate, and the molecular formula is C13H18O3, Quality Control of 6259-76-3.

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

Zhou, Hongzhuan published the artcileInhibitory effects of antiviral drug candidates on canine parvovirus in F81 cells, Related Products of esters-buliding-blocks, the main research area is canine parvovirus antiviral drug candidate inhibitory effect; FDA-approved drug library; antiviral inhibitors; canine parvovirus; cytopathic effect (CPE)-based high-throughput screening assay.

Canine parvovirus (CPV) is a common etiol. agent of acute enteritis, which occurs globally in domestic and wild carnivores. Despite the widespread use of inactivated or live attenuated vaccines, the emergence of antigenic variants and the influence of maternal antibodies have raised some concerns regarding the efficacy of com. vaccines. While no specific antiviral therapy for CPV infection exists, the only treatment option for the infection is supportive therapy based on symptoms. Thus, there is an urgent medical need to develop antiviral therapeutic options to reduce the burden of CPV-related disease. In this study, a cytopathic effect (CPE)-based high-throughput screening assay was used to screen CPV inhibitors from a Food and Drug Administration (FDA)-approved drug library. After two rounds of screening, seven out of 1430 screened drugs were found to have >50% CPE inhibition. Three drugs-Nitazoxanide, Closantel Sodium, and Closantel-with higher anti-CPV effects were further evaluated in F81 cells by absolute PCR quantification and indirect immunofluorescence assay (IFA). The inhibitory effects of all three drugs were dose-dependent. Time of addition assay indicated that the drugs inhibited the early processes of the CPV replication cycle, and the inhibition effects were relatively high within 2 h postinfection. Western blot assay also showed that the three drugs had broad-spectrum antiviral activity against different subspecies of three CPV variants. In addition, antiapoptotic effects were observed within 12 h in Nitazoxanide-treated F81 cells regardless of CPV infection, while Closantel Sodium- or Closantel-treated cells had no proof antiapoptotic effects. In conclusion, Nitazoxanide, Closantel Sodium, and Closantel can effectively inhibit different subspecies of CPV. Since the safety profiles of FDA-approved drugs have already been extensively studied, these three drugs can potentially become specific and effective anti-CPV drugs.

Viruses published new progress about Anti-apoptotic agents. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Related Products of esters-buliding-blocks.

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

Kim, Juewon published the artcileIntense pulsed light attenuates UV-induced hyperimmune response and pigmentation in human skin cells, Related Products of esters-buliding-blocks, the main research area is irradiation immune response oxidative stress hperimmune reaction; antioxidative enzyme activity; inflammation; intense pulsed light; melanogenesis; oxidative stress; photoaging.

The skin of an organism is affected by various environmental factors and fights against aging stress via mech. and biochem. responses. Photoaging induced by UV B (UVB) irradiation is common and is the most vital factor in the senescence phenotype of skin, and so, suppression of UVB stress-induced damage is critical To lessen the UVB-induced hyperimmune response and hyperpigmentation, we investigated the ameliorative effects of intense pulsed light (IPL) treatment on the photoaged phenotype of skin cells. Normal human epidermal keratinocytes and human epidermal melanocytes were exposed to 20 mJ/cm2 of UVB. After UVB irradiation, the cells were treated with green (525-530 nm) and yellow (585-592 nm) IPL at various time points prior to the harvest step. Subsequently, various signs of excessive immune response, including expression of proinflammatory and melanogenic genes and proteins, cellular oxidative stress level, and antioxidative enzyme activity, were examined We found that IPL treatment reduced excessive cutaneous immune reactions by suppressing UVB-induced proinflammatory cytokine expression. IPL treatment prevented hyperpigmentation, and combined treatment with green and yellow IPL synergistically attenuated both processes. IPL treatment may exert protective effects against UVB injury in skin cells by attenuating inflammatory cytokine and melanogenic gene overexpression, possibly by reducing intracellular oxidative stress. IPL treatment also preserves antioxidative enzyme activity under UVB irradiation This study suggests that IPL treatment is a useful strategy against photoaging, and provides evidence supporting clin. approaches with non-invasive light therapy.

International Journal of Molecular Sciences published new progress about Animal gene Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study) (IFNG). 2044-85-1 belongs to class esters-buliding-blocks, name is 2′,7′-Dichloro-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-diyl diacetate, and the molecular formula is C24H14Cl2O7, Related Products of esters-buliding-blocks.

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

Li, Hongxia published the artcileThe combination of HT-ac and HBET improves the cognitive and learning abilities of heat-stressed mice by maintaining mitochondrial function through the PKA-CREB-BDNF pathway, Application In Synthesis of 5405-41-4, the main research area is PKA CREB BDNF signaling mitochondria heat stress learning cognition.

The aim was to investigate whether the combination of hydroxytyrosol acetate (HT-ac) and Et β-hydroxybutyrate (HBET) can improve the cognition of heat-stressed mice, meanwhile exploring the mechanism of action. Mice were divided into 5 groups: control, heat-stressed, HT-ac, HBET, and HT-ac + HBET. Mice were gavaged for 21 days and exposed to heat (42.5 ± 0.5°C, RH 60 ± 10%, 1 h day-1) on days 15-21, except for the control group. Results showed that the combination of HT-ac + HBET improved the cognitive and learning abilities of heat-stressed mice, which were tested by Morris water maze, shuttle box, and jumping stage tests. The combination of HT-ac + HBET maintained the integrity of neurons and mitochondria of heat-stressed mice. Likewise, this combination increased the mitochondrial membrane potential, the ATP content, the expression of phosphorylated PKA, BDNF, phosphorylated CREB and Bcl-2, and decreased the expression of Bax, caspase-3, and intracytoplasmic Cyt C in heat-stressed mice.

Food & Function published new progress about Antioxidants. 5405-41-4 belongs to class esters-buliding-blocks, name is Ethyl 3-hydroxybutanoate, and the molecular formula is C6H12O3, Application In Synthesis of 5405-41-4.

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

Hsieh, Dennis Jine-Yuan published the artcileDiallyl trisulfide (DATS) suppresses AGE-induced cardiomyocyte apoptosis by targeting ROS-mediated PKCδ activation, Application In Synthesis of 2044-85-1, the main research area is diallyl trisulfide antiapoptotic agent AGE ROS PKCgamma cardiomyocyte apoptosis; AGE; DATS; PKCδ; apoptosis; cardiomyocyte.

Chronic high-glucose exposure results in the production of advanced glycation end-products (AGEs) leading to reactive oxygen species (ROS) generation, which contributes to the development of diabetic cardiomyopathy. PKCδ activation leading to ROS production and mitochondrial dysfunction involved in AGE-induced cardiomyocyte apoptosis was reported in our previous study. Diallyl trisulfide (DATS) is a natural cytoprotective compound under various stress conditions. In this study, the cardioprotective effect of DATS against rat streptozotocin (STZ)-induced diabetic mellitus (DM) and AGE-induced H9c2 cardiomyoblast cell/neonatal rat ventricular myocyte (NRVM) damage was assessed. We observed that DATS treatment led to a dose-dependent increase in cell viability and decreased levels of ROS, inhibition of PKCδ activation, and recuded apoptosis-related proteins. Most importantly, DATS reduced PKCδ mitochondrial translocation induced by AGE. However, apoptosis was not inhibited by DATS in cells transfected with PKCδ-wild type (WT). Inhibition of PKCδ by PKCδ-kinase-deficient (KD) or rottlerin not only inhibited cardiac PKCδ activation but also attenuated cardiac cell apoptosis. Interestingly, overexpression of PKCδ-WT plasmids reversed the inhibitory effects of DATS on PKCδ activation and apoptosis in cardiac cells exposed to AGE, indicating that DATS may inhibit AGE-induced apoptosis by downregulating PKCδ activation. Similar results were observed in AGE-induced NRVM cells and STZ-treated DM rats following DATS administration. Taken together, our results suggested that DATS reduced AGE-induced cardiomyocyte apoptosis by eliminating ROS and downstream PKCδ signaling, suggesting that DATS has potential in diabetic cardiomyopathy (DCM) treatment.

International Journal of Molecular Sciences published new progress about Anti-apoptotic agents. 2044-85-1 belongs to class esters-buliding-blocks, name is 2′,7′-Dichloro-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-diyl diacetate, and the molecular formula is C24H14Cl2O7, Application In Synthesis of 2044-85-1.

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