Month: September 2022

Hochkogler, Christina M.;Lieder, Barbara;Schachner, Daniel;Heiss, Elke;Schroeter, Annett;Hans, Joachim;Ley, Jakob P.;Krammer, Gerhard E.;Somoza, Veronika published 《Capsaicin and nonivamide similarly modulate outcome measures of mitochondrial energy metabolism in HepG2 and 3T3-L1 cells》 in 2018. The article was appeared in 《Food & Function》. They have made some progress in their research.Safety of N-Vanillylnonanamide The article mentions the following:

Capsaicin, the highly pungent principle of red pepper, has been demonstrated to have anti-obesity properties by affecting energy and lipid metabolism Recent evidence from human intervention trials shows that also less pungent capsaicin analogs, like nonivamide, may help to reduce total body fat, although mechanistic data comparing the effects of capsaicin and nonivamide on outcome measures of energy metabolism are lacking. Here, the tissue-specific effects of capsaicin and nonivamide on parameters of mitochondrial energy metabolism in 3T3-L1 and HepG2 cells are investigated. Lipid accumulation was reduced to a similar extent after treatment with both test substances during the maturation of 3T3-L1 cells by up to 6.91% for capsaicin and up to 4.89% for nonivamide (p < 0.01) at a concentration of 0.1μM or 1μM, resp. Energy-producing pathways, as indicated by the reduced mitochondrial oxygen consumption and reduced glucose and fatty acid uptake, were diminished after incubation with both capsaicinoids at a concentration of 100μM. The results from HPLC analyses revealed a reduced cellular energy charge potential after a 4 h treatment with nonivamide. In HepG2 cells, similar effects were demonstrated: the glucose uptake was reduced by 18.7% and 25.8% (p < 0.05), after a 24 h incubation with 100μM capsaicin and nonivamide, resp. In addition, the fatty acid uptake and oxygen consumption were decreased and the energy charge potential was diminished. These findings provide evidence that concentrations of capsaicin and nonivamide between 0.1 and 100μM modulate the mechanisms of cellular energy metabolism to a similar extent, independent of the investigated tissue. And N-Vanillylnonanamide (cas: 2444-46-4) was used in the research process.

N-Vanillylnonanamide(cas:2444-46-4) has antifouling properties.Safety of N-Vanillylnonanamide It acts as an nicotinamide adenine dinucleotide phosphate (NADPH) inhibitor.N-Vanillylnonanamide has been used for the preparation of spicules.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Recommanded Product: 2444-46-4《Exhaled breath condensate methods adapted from human studies using longitudinal metabolomics for predicting early health alterations in dolphins》 was published in 2017. The authors were Borras, Eva;Aksenov, Alexander A.;Baird, Mark;Novick, Brittany;Schivo, Michael;Zamuruyev, Konstantin O.;Pasamontes, Alberto;Parry, Celeste;Foutouhi, Soraya;Venn-Watson, Stephanie;Weimer, Bart C.;Davis, Cristina E., and the article was included in《Analytical and Bioanalytical Chemistry》. The author mentioned the following in the article:

Monitoring health conditions is essential to detect early asymptomatic stages of a disease. To achieve this, blood, urine and breath samples are commonly used as a routine clin. diagnostic. These samples offer the opportunity to detect specific metabolites related to diseases and provide a better understanding of their development. Although blood samples are commonly used routinely to monitor health, the implementation of a relatively noninvasive technique, such as exhaled breath condensate (EBC) anal., may further benefit the well-being of both humans and other animals. EBC anal. can be used to track possible phys. or biochem. alterations caused by common diseases of the bottlenose dolphin (Tursiops truncatus), such as infections or inflammatory-mediated processes. The authors used an untargeted metabolomic method with liquid chromatog.-mass spectrometry anal. of EBC samples to determine biomarkers related to disease development. Five dolphins under human care were followed up for 1 yr. The authors collected paired blood, phys. examination information, and EBC samples. The authors then statistically correlated this information to predict specific health alterations. Three dolphins provided promising case study information about biomarkers related to cutaneous infections, respiratory infections, dental disease, or hormonal changes (pregnancy). The use of complementary liquid chromatog. platforms, with hydrophilic interaction chromatog. and reverse-phased columns, allowed the authors to detect a wide spectrum of EBC biomarker compounds that could be related to these health alterations. Moreover, these two anal. techniques not only provided complementary metabolite information but in both cases they also provided promising diagnostic information for these health conditions. [Figure not available: see fulltext.].N-Vanillylnonanamide (cas: 2444-46-4) were involved in the experimental procedure.

N-Vanillylnonanamide(cas:2444-46-4) is a capsaicin analog that has been used to study the effects of capsaicin on energy metabolism and bowel disease.Recommanded Product: 2444-46-4 It has been shown to be effective in the treatment of bowel disease, by inhibiting the production of proinflammatory cytokines and prostaglandins.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

COA of Formula: C6H7N3O《LEADS-FRAG: A Benchmark Data Set for Assessment of Fragment Docking Performance》 was published in 2020. The authors were Chachulski, Laura;Windshuegel, Bjoern, and the article was included in《Journal of Chemical Information and Modeling》. The author mentioned the following in the article:

Fragment-based drug design is a popular approach in drug discovery, which makes use of computational methods such as mol. docking. To assess fragment placement performance of mol. docking programs, we constructed LEADS-FRAG, a benchmark data set containing 93 high-quality protein-fragment complexes that were selected from the Protein Data Bank using a rational and unbiased process. The data set contains fully prepared protein and fragment structures and is publicly available. Moreover, we used LEADS-FRAG for evaluating the small-mol. docking programs AutoDock, AutoDock Vina, FlexX, and GOLD for their fragment docking performance. GOLD in combination with the scoring function ChemPLP and AutoDock Vina performed best and generated near-native conformations (root mean square deviation <1.5 Å) for more than 50% of the data set considering the top-ranked docking pose. Taking into account all docking poses, the tested programs generated near-native conformations for up to 86% of the fragments in LEADS-FRAG. By rescoring all docking poses with the GOLD scoring functions and the Protein-Ligand Informatics force field, the number of near-native conformations increased up to 40% with respect to the top-rescored poses. Our results show that conventional small-mol. docking programs achieve a satisfactory fragment docking performance when utilizing rescoring. The experimental procedure involved many compounds, such as 6-Aminonicotinamide (cas: 329-89-5) .

6-Aminonicotinamide (cas:329-89-5)COA of Formula: C6H7N3O is an aminopyridine, which is a specific pentose inhibitor and thus inhibits the NADP production.It can be used as a reactant for the synthesis of 6-substituted imidazo[1,2-a]pyridines with potential application as chemotherapeutic drugs.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Category: amides-buliding-blocksIn 2021, Hasan, Mahmudul Md.;Tasmin, Most. Sayla;El-Shehawi, Ahmed M.;Elseehy, Mona M.;Reza, Abu Md.;Haque, Ariful published 《R. vesicarius L. exerts nephroprotective effect against cisplatin-induced oxidative stress》. 《BMC Complementary Medicine and Therapies》published the findings. The article contains the following contents:

Cisplatin is an outstanding anticancer drug, but its use has been decreased remarkably due to sever nephrotoxicity. R. vesicarius L. is a leafy vegetable that is evident with anti-angeogenic, anti-inflammatory, anti-proliferative, hepatoprotective, and nephroprotective potential. Therefore, this study was designed to inspect its methanol extract (RVE) for possible nephroprotective effect. Primarily, in vitro antioxidant activity of RVE was confirmed based on 2, 2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging aptitude. Thereafter, Swiss Albino male mice were treated with cisplatin (2.5 mg/kg) for 5 successive days to induce nephrotoxicity. Recovery from nephrotoxicity was scrutinized by treating the animals with RVE (25, 50, and 100 mg/kg) i.p. (i.p.) for the next 5 consecutive days. After completion of treatment, mice were sacrificed and kidneys were collected. Part of it was homogenized in sodium phosphate buffer for evaluating malondialdehyde (MDA) level, another part was used to evaluate gene (NQO1, p53, and Bcl-2) expression. Moreover, the hydrogen peroxide (H₂O₂) neutralizing capacity of RVE was evaluated in HK-2 cells in vitro. Finally, bioactive phytochems. in RVE were determined using gas chromatog.-mass spectrometry (GC-MS). RVE showed in vitro antioxidant activity in a dose-dependent fashion with 37.39 ± 1.89 μg/mL IC50 value. Treatment with RVE remarkably (p < 0.05) decreased MDA content in kidney tissue. Besides, the expression of NQO, p53, and Bcl-2 genes was significantly (p < 0.05) mitigated in a dose-dependent manner due to the administration of RVE. RVE significantly (p < 0.05) reversed the H2O2 level in HK-2 cells to almost normal. From GC-MS, ten compounds including three known antioxidants “4H-Pyran-4-one, 2, 3-dihydro-3,5-dihydroxy-6-methyl-“, “Hexadecanoic acid”, and “Squalene” were detected. The extract was rich with an alkaloid “13-Docosenamide”. Overall, RVE possesses a protective effect against cisplatin-induced kidney damage. And cis-13-Docosenamide (cas: 112-84-5) was used in the research process.

cis-13-Docosenoamide(cas: 112-84-5) is a primary fatty amide resulting from the formal condensation of the carboxy group of erucic acid with ammonia.Category: amides-buliding-blocks It is commonly used as a slip additive in the plastic manufacturing industry.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Mazorra Morales, Luis Miguel;Cosme Silva, Glaucia Michelle;Santana, Diederson Bortolini;Pireda, Saulo F.;Dorighetto Cogo, Antonio Jesus;Heringer, Angelo Schuabb;de Oliveira, Tadeu dos Reis;Reis, Ricardo S.;dos Santos Prado, Luis Alfredo;de Oliveira, Andre Vicente;Silveira, Vanildo;Da Cunha, Maura;Barros, Claudia F.;Facanha, Arnoldo R.;Baldet, Pierre;Bartoli, Carlos G.;da Silva, Marcelo Gomes;Oliveira, Jurandi G. published 《Mitochondrial dysfunction associated with ascorbate synthesis in plants》 in 2022. The article was appeared in 《Plant Physiology and Biochemistry (Issy-les-Moulineaux, France)》. They have made some progress in their research.Product Details of 89-73-6 The article mentions the following:

Mitochondria are the major organelles of energy production; however, active mitochondria can decline their energetic role and show a dysfunctional status. Mitochondrial dysfunction was induced by high non-physiol. level of L-galactone-1,4-lactone (L-GalL), the precursor of ascorbate (AsA), in plant mitochondria. The dysfunction induced by L-GalL was associated with the fault in the mitochondrial electron partition and reactive oxygen species (ROS) over-production Using mitochondria from RNAi-plant lines harbouring silenced L-galactone-1,4-lactone dehydrogenase (L-GalLDH) activity, it was demonstrated that such dysfunction is dependent on this enzyme activity. The capacity of alternative respiration was strongly decreased by L-GalL, probably mediated by redox-inactivation of the alternative oxidase (AOX) enzyme. Although, alternative respiration was shown to be the key factor that helps support AsA synthesis in dysfunctional mitochondria. Experiments with respiratory inhibitors showed that ROS formation and mitochondrial dysfunction were more associated with the decline in the activities of COX (cytochrome oxidase) and particularly AOX than with the lower activities of respiratory complexes I and III. The application of high L-GalL concentrations induced proteomic changes that indicated alterations in proteins related to oxidative stress and energetic status. However, supra-optimal L-GalL concentration was not deleterious for plants. Instead, the L-GalLDH activity could be pos. Indeed, it was found that wild type plants performed better growth than L-GalLDH-RNAi plants in response to high non-physiol. L-GalL concentrations The experimental procedure involved many compounds, such as N,2-Dihydroxybenzamide (cas: 89-73-6) .

N,2-Dihydroxybenzamide(cas: 89-73-6) has also been shown to be active against wild-type strains of Candida glabrata, but not against resistant mutants. Product Details of 89-73-6 This drug may have therapeutic potential for bone cancer and metabolic disorders such as obesity.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Zhou, Yanhong;Xia, Xiaojian;Yu, Gaobo;Wang, Jitao;Wu, Jingxue;Wang, Mengmeng;Yang, Youxin;Shi, Kai;Yu, Yunlong;Chen, Zhixiang;Gan, Jay;Yu, Jingquan published 《Brassinosteroids play a critical role in the regulation of pesticide metabolism in crop plants》 in 2015. The article was appeared in 《Scientific Reports》. They have made some progress in their research.Recommanded Product: 329-89-5 The article mentions the following:

Pesticide residues in agricultural produce pose a threat to human health worldwide. Although the detoxification mechanisms for xenobiotics have been extensively studied in mammalian cells, information about the regulation network in plants remains elusive. Here we show that brassinosteroids (BRs), a class of natural plant hormones, decreased residues of common organophosphorus, organochlorine and carbamate pesticides by 30-70% on tomato, rice, tea, broccoli, cucumber, strawberry, and other plants when treated externally. Genome-wide microarray anal. showed that fungicide chlorothalonil (CHT) and BR co-upregulated 301 genes, including a set of detoxifying genes encoding cytochrome P 450, oxidoreductase, hydrolase and transferase in tomato plants. The level of BRs was closely related to the respiratory burst oxidase 1 (RBOH1)-encoded NADPH oxides-dependent H₂O₂ production, glutathione biosynthesis and the redox homeostasis, and the activity of glutathione S-transferase (GST). Gene silencing treatments showed that BRs decreased pesticide residues in plants likely by promoting their metabolism through a signaling pathway involving BRs-induced H₂O₂ production and cellular redox change. Our study provided a novel approach for minimizing pesticide residues in crops by exploiting plants’ own detoxification mechanisms. The experimental procedure involved many compounds, such as 6-Aminonicotinamide (cas: 329-89-5) .

6-Aminonicotinamide (cas:329-89-5)Recommanded Product: 329-89-5 induces apoptosis in tumor cells. It is clinically used in disseminated neoplastic disease. It also acts as 6-phosphogluconate dehydrogenase inhibitor. It aids in the treatment of psoriasis. It is used as cancer chemotherapeutic drug in animals.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Duan, Y.;Chen, J.;Pang, Z.;Ye, X.;Zhang, C.;Hu, H.;Xie, J. published 《Antifungal mechanism of Streptomyces ma. FS-4 on fusarium wilt of banana》 in 2021. The article was appeared in 《Journal of Applied Microbiology》. They have made some progress in their research.Recommanded Product: cis-13-Docosenamide The article mentions the following:

In this study, antifungal mechanism of Streptomyces ma. FS-4 on fusarium wilt of banana was investigated. Methods and Results : The physiol. strain of banana fusarium pathogen Fusarium oxysporum f. sp. cubense Race 4 (FOC.4) was used as the target fungus, and the antifungal mechanism of the crude extract of Streptomyces ma. FS-4 was investigated. Eighteen different compounds identified by gas chromatog.-mass spectrometry were composed of aldehydes, Me, hydrocarbons, amides, esters and acids. FS-4 significantly inhibited the spore germination of the target fungi, with an EC50 of 22·78 μg ml-1. After treatment with 100 μg ml-1 FS-4 crude extract, the N-acetylglucosamine content in the mycelium increased 1·95-fold. However, the extract had no significant effect on β-1,3-glucanase. At the FS-4 crude extract dose of 100 μg ml-1, the total sugar and protein contents decreased by 28·6 and 29·1% resp., and the fat content was 41·3%. FS-4 significantly inhibited the activity of the mitochondrial complex III of Foc4, which was reduced by 52·45%. Moreover FS-4 reduced the activity of succinate dehydrogenase, a key enzyme in the Krebs cycle, by 60·2%. However, FS-4 had no significant effect on malate dehydrogenase. The membrane potential on the mitochondrial inner membrane was significantly reduced at the test concentration of 100 μg ml-1. ROS gradually accumulated in the Foc4 hypha, and the burst was 3·97 times higher than the control. To complete the study, the researchers used cis-13-Docosenamide (cas: 112-84-5) .

cis-13-Docosenoamide(cas: 112-84-5) was employed as: standard in determination of fatty acid amides in polyethylene packaging film by GC/MS;slip agent for polymers to reduce their friction coefficient and to make films easier to handle.Recommanded Product: cis-13-Docosenamide

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Application of 89-73-6In 2021, Chen, Tomer;Cohen, Dekel;Itkin, Maxim;Malitsky, Sergey;Fluhr, Robert published 《Lipoxygenase functions in ¹O₂ production during root responses to osmotic stress》. 《Plant Physiology》published the findings. The article contains the following contents:

Drought induces osmotic stress in roots, a condition simulated by the application of high-mol.-weight polyethylene glycol. Osmotic stress results in the reduction of Arabidopsis thaliana root growth and production of 1O2 from an unknown non-photosynthetic source. Reduced root growth can be alleviated by application of the 1O2 scavenger histidine (HIS). Here, we examined the possibility that 1O2 production involves Russell reactions occurring among the enzymic products of lipoxygenases (LOXs), the fatty acid hydroperoxides. LOX activity was measured for purified soybean (Glycine max) LOX1 and in crude Arabidopsis root extracts using linoleic acid as substrate. Formation of the 13(S)-Hydroperoxy-9(Z),11(E)-octadecadienoic acid product was inhibited by salicylhdroxamic acid, which is a LOX inhibitor, but not by HIS, whereas 1O2 production was inhibited by both. D2O, which specifically extends the half-life of 1O2, augmented the LOX-dependent generation of 1O2, as expected from a Russell-type reaction. The addition of linoleic acid to roots stimulated 1O2 production and inhibited growth, suggesting that the availability of LOX substrate is a rate-limiting step. Indeed, water stress rapidly increased linoleic and linolenic acids by 2.5-fold in roots. Mutants with root-specific microRNA repression of LOXs showed downregulation of LOX protein and activity. The lines with downregulated LOX displayed significantly less 1O2 formation, improved root growth in osmotic stress, and an altered transcriptome response compared with wild type. The results show that LOXs can serve as an enzymic source of dark 1O2 during osmotic stress and demonstrate a role for 1O2 in defining the physiol. response. To complete the study, the researchers used N,2-Dihydroxybenzamide (cas: 89-73-6) .

N,2-Dihydroxybenzamide(cas: 89-73-6) can be used:To prepare phenylboronic acid-based bioconjugates for chromatographic applications;As a ligand to synthesize Fe(III), Cu(II), Ni(II) and Zn(II) complexes.Application of 89-73-6

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Nagahori, Hirohisa;Suzuki, Noriyuki;Le Coz, Florian;Omori, Takashi;Saito, Koichi published 《Prediction of in vivo developmental toxicity by combination of Hand1-Luc embryonic stem cell test and metabolic stability test with clarification of metabolically inapplicable candidates》. The research results were published in《Toxicology Letters》 in 2016.Recommanded Product: 329-89-5 The article conveys some information:

Hand1-Luc Embryonic Stem Cell Test (Hand1-Luc EST) is a promising alternative method for evaluation of developmental toxicity. However, the problems of predictivity have remained due to appropriateness of the solubility, metabolic system, and prediction model. Therefore, we assessed the usefulness of rat liver S9 metabolic stability test using LC-MS/MS to develop new prediction model. A total of 71 chems. were analyzed by measuring cytotoxicity and differentiation toxicity, and highly reproducible (CV = 20%) results were obtained. The first prediction model was developed by discriminant anal. performed on a full dataset using Hand1-Luc EST, and 66.2% of the chems. were correctly classified by the cross-validated classification. A second model was developed with addnl. descriptors obtained from the metabolic stability test to calculate hepatic availability, and an accuracy of 83.3% was obtained with applicability domain of 50.7% (=36/71) after exclusion of 22 metabolically inapplicable candidates, which potentially have a metabolic activation property. A step-wise prediction scheme with combination of Hand1-Luc EST and metabolic stability test was therefore proposed. The current results provide a promising in vitro test method for accurately predicting in vivo developmental toxicity. And 6-Aminonicotinamide (cas: 329-89-5) was used in the research process.

6-Aminonicotinamide (cas:329-89-5)Recommanded Product: 329-89-5 is an aminopyridine, which is a specific pentose inhibitor and thus inhibits the NADP production.It can be used as a reactant for the synthesis of 6-substituted imidazo[1,2-a]pyridines with potential application as chemotherapeutic drugs.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Recommanded Product: N,2-DihydroxybenzamideIn 2020, Salerno, Elvin V.;Eliseeva, Svetlana V.;Schneider, Bernadette L.;Kampf, Jeff W.;Petoud, Stephane;Pecoraro, Vincent L. published 《Visible, Near-Infrared, and Dual-Range Luminescence Spanning the 4f Series Sensitized by a Gallium(III)/Lanthanide(III) Metallacrown Structure》. 《Journal of Physical Chemistry A》published the findings. The article contains the following contents:

Ga³⁺/Ln³⁺ metallacrowns (MCs) [LnGa₈(shi)₈(OH)₄]Na·xMeOH·yH₂O (Ln-1, Ln = Pr³⁺, Nd³⁺, Sm³⁺-Yb³⁺ and analog Y³⁺; H₃shi = salicylhydroxamic acid) is presented. Ln-1 were obtained by reacting Ga³⁺ and Ln³⁺ nitrate salts with the H₃shi ligand. X-ray single crystal unit cell anal. confirmed that all MCs are isostructural. The crystal structure was solved for the Nd³⁺ analog and revealed that Nd³⁺ is centered between 2 [12-MC_Ga^III_N(shi)-4] MC rings and bound to 8 hydroximate O ions (4 from each ring) in a pseudosquare antiprismatic fashion adopting a pseudo-D_4h symmetry. Pulsed gradient spin echo diffusion ordered ¹H NMR spectroscopy and electrospray ionization mass spectrometry confirmed that the structure of Ln-1 remains intact in MeOH solutions while mass spectrometry suggests that 4 OH^– bridges are exchanged with MeO^–/CD₃O^–. An exceptional ability of this series of MCs to sensitize the characteristic emission of Ln³⁺ was confirmed with the observation of bright red and green emission signals of Eu-1 and Tb-1, NIR emissions of Yb-1 and Nd-1, and dual-range emissions of Pr-1, Sm-1, Dy-1, Ho-1, Er-1, and Tm-1 in the solid state upon excitation into ligand-centered bands at 340 nm. The luminescence properties of Ln-1 (Ln = Nd³⁺, Sm³⁺, Eu³⁺, Tb³⁺, Dy³⁺, and Yb³⁺) were also studied in MeOH and CD₃OD solutions For Eu-1 and Yb-1 MCs, more extensive analyses of the photophys. properties were performed, which included the determination of radiative lifetimes, intrinsic quantum yields, and sensitization efficiencies. The absolute quantum yields (Q_Ln^L) of Ln-1 in the visible and NIR ranges were determined In the case of Sm-1, the values of Q_Ln^L in MeOH and CD₃OD solutions are exceptionally high, i.e., 10.1(5) and 83(1)%. Values obtained for Yb-1, i.e., 0.78(4)% in MeOH and 8.4(1)% in CD₃OD, are among the highest ones reported today for Yb³⁺ complexes formed with nondeuterated and nonhalogenated ligands. The experimental procedure involved many compounds, such as N,2-Dihydroxybenzamide (cas: 89-73-6) .

N,2-Dihydroxybenzamide(cas: 89-73-6) can be used:To prepare phenylboronic acid-based bioconjugates for chromatographic applications;As a ligand to synthesize Fe(III), Cu(II), Ni(II) and Zn(II) complexes.Recommanded Product: N,2-Dihydroxybenzamide

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics