Month: November 2022

SL010110, a lead compound, inhibits gluconeogenesis via SIRT2-p300-mediated PEPCK1 degradation and improves glucose homeostasis in diabetic mice was written by Ren, Yu-ran;Ye, Yang-liang;Feng, Ying;Xu, Ti-fei;Shen, Yu;Liu, Jia;Huang, Su-ling;Shen, Jian-hua;Leng, Ying. And the article was included in Acta Pharmacologica Sinica in 2021.Electric Literature of C11H15N2O8P The following contents are mentioned in the article:

Abstract: Suppression of excessive hepatic gluconeogenesis is an effective strategy for controlling hyperglycemia in type 2 diabetes (T2D). In the present study, we screened our compounds library to discover the active mols. inhibiting gluconeogenesis in primary mouse hepatocytes. We found that SL010110 (5-((4-allyl-2-methoxyphenoxy) methyl) furan-2-carboxylic acid) potently inhibited gluconeogenesis with 3μM and 10μM leading to a reduction of 45.5% and 67.5%, resp. Moreover, SL010110 caused suppression of gluconeogenesis resulted from downregulating the protein level of phosphoenolpyruvate carboxykinase 1 (PEPCK1), but not from affecting the gene expressions of PEPCK, glucose-6-phosphatase, and fructose-1,6-bisphosphatase. Furthermore, SL010110 increased PEPCK1 acetylation, and promoted PEPCK1 ubiquitination and degradation SL010110 activated p300 acetyltransferase activity in primary mouse hepatocytes. The enhanced PEPCK1 acetylation and suppressed gluconeogenesis caused by SL010110 were blocked by C646, a histone acetyltransferase p300 inhibitor, suggested that SL010110 inhibited gluconeogenesis by activating p300. SL010110 decreased NAD⁺/NADH ratio, inhibited SIRT2 activity, and further promoted p300 acetyltransferase activation and PEPCK1 acetylation. These effects were blocked by NMN, an NAD⁺ precursor, suggested that SL010110 inhibited gluconeogenesis by inhibiting SIRT2, activating p300, and subsequently promoting PEPCK1 acetylation. In type 2 diabetic ob/ob mice, single oral dose of SL010110 (100 mg/kg) suppressed gluconeogenesis accompanied by the suppressed hepatic SIRT2 activity, increased p300 activity, enhanced PEPCK1 acetylation and degradation Chronic oral administration of SL010110 (15 or 50 mg/kg) significantly reduced the blood glucose levels in ob/ob and db/db mice. This study reveals that SL010110 is a lead compound with a distinct mechanism of suppressing gluconeogenesis via SIRT2-p300-mediated PEPCK1 degradation and potent anti-hyperglycemic activity for the treatment of T2D. This study involved multiple reactions and reactants, such as ((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate (cas: 1094-61-7Electric Literature of C11H15N2O8P).

((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate (cas: 1094-61-7) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. In simple aromatic amides, fragmentation occurs on both sides of the carbonyl group. If a hydrogen is available in N-substituted aromatic amides, it tends to migrate and form an aromatic amine and the loss of a ketene.Electric Literature of C11H15N2O8P

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

Effects of temperature on growth performance and metabolism of juvenile sea bass (Dicentrarchus labrax) was written by Zhou, Cheng;Zhang, Zhi-qiang;Zhang, Lei;Liu, Ying;Liu, Peng-fei. And the article was included in Aquaculture in 2021.COA of Formula: C11H15N2O8P The following contents are mentioned in the article:

The European sea bass (Dicentrarchus labrax) has become an increasingly important aquaculture species due to the rapid expansion of farming in China and its com. popularity in Asia. A 60 day growth trial was conducted to investigate the impact of temperature on growth and ingestion performance and metabolism of the European sea bass (Dicentrarchus labrax). Juvenile European sea bass were stocked in triplicate at 3 temperature conditions (10°, 15°, and 20°). The specific growth rate and feeding rate of European sea bass in both 10° and 15° were all significantly lower than fish in 20° (P < 0.05). The feed conversion rate of European sea bass was 20° > 15° (P > 0.05), and 20° > 10° (P < 0.05). We measured the levels of muscle metabolites of European sea bass, using liquid chromatog. with tandem mass spectrometry-(LC-MS/MS) and compared the data among groups using principal component anal. and orthogonal partial least-squares discriminant anal. (OPLS-DA). We also conducted Kyoto Encyclopedia of Genes and Genomes (KEGG) metabolic pathway anal. OPLS-DA clearly discriminated the muscle metabolites of European sea bass under the three temperature conditions. The important differential metabolites mainly included β-NMN, nicotinic acid adenine dinucleotide, nicotinic acid, UDP-glucose, glycerophosphatidylcholine, (±)-17-hydroxy-4Z, 7Z, 10Z, 13Z, 15E, 19Z-docosahexaenoic acid, (±)-15-hydroxy-5Z, 8Z, 11Z, 13E, 17Z-eicosapentaenoic acid, γ-linolenic acid, L-serine, inositol, L-citrulline, and succinic acid. The KEGG metabolic pathway anal. showed that lipid metabolism, glucose metabolism, the tricarboxylic acid cycle, the urea cycle, and nicotinate and nicotinamide metabolism may closely related to temperature conditions. The findings of this research suggest that the growth and food intake of European sea bass can be promoted and production can be improved at a culture temperature of 20°. Our results provide a theor. basis and tech. guidance for formulating temperature control strategies for industrial recirculating aquaculture of European sea bass. This study involved multiple reactions and reactants, such as ((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate (cas: 1094-61-7COA of Formula: C11H15N2O8P).

((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate (cas: 1094-61-7) belongs to amides. Amides can be viewed as a derivative of a carboxylic acid RC(=O)OH with the hydroxyl group –OH replaced by an amine group −NR′R″; or, equivalently, an acyl (alkanoyl) group RC(=O)− joined to an amine group. Amides are not in general accessible by the direct condensation of amines with carboxylic acids for two reasons: first, both components are readily deactivated by a transfer of a proton from the acid to the amine and second, the hydroxy unit on the carbonyl of the acid is a relatively poor leaving group. Nevertheless, the formation of five- and six-membered rings is often surprisingly simple provided that other factors can be brought into play to assist in the condensation.COA of Formula: C11H15N2O8P

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

Anion-recognition studies of a Re(I)-based square containing the dipyridyl-amide ligand was written by Tzeng, Biing-Chiau;Chen, Yen-Fei;Wu, Chia-Chin;Hu, Cho-Chun;Chang, Ya-Ting;Chen, Chang-Kai. And the article was included in New Journal of Chemistry in 2007.Recommanded Product: N1,N2-Di(pyridin-4-yl)oxalamide The following contents are mentioned in the article:

The mol. square [Re(CO)₃Cl(L)]₄ (1) containing the dipyridyl-amide ligand, N,N’-4-dipyridyloxalamide (L), was constructed from Re(CO)₅Cl and L for the purpose of anion-recognition studies. Upon addition of fluoride anions to a THF solution of 1, a remarkable spectral change is observed, and indeed a new absorption band grows at ∼348 nm. The authors reasoned that upon addition of fluoride, the hydrogen bonds between F^– and -NH groups of L would first form and increase the electron densities of nitrogen atoms. This in turn increases the conjugation throughout the L ligand, which is responsible for the new growing absorption band. Finally, a proton-transfer process occurs upon addition of excess F^– anions, corroborated by the ¹H NMR titration experiment due to the occurrence of HF₂^–. The binding constants based on a 1:1 complex (1-X^–, X^– = anions) follow the order: F^– > CN^– > OAc^– > Cl^– > Br^–, PF₆^–, BF₄^–, ClO₄^–, NO₃^– and HSO₄^–. The most electroneg. F^– anion shows the largest binding constant, followed by CN^–, OAc^– and Cl^– anions. The less electroneg. Br^– anion and bigger PF₆^–, BF₄^–, ClO₄^–, NO₃^– and HSO₄^– anions do not show any binding affinity with 1. The control titrations carried out using L and the same series of anions showed that the basicity of anions also possibly lends some contribution to the sensing events. However, the binding affinity of 1 toward various anions can be mostly correlated with the electronegativity as well as cavity size of the mol. square, and hence 1 can be expected to be a sensor for F^–. This study involved multiple reactions and reactants, such as N1,N2-Di(pyridin-4-yl)oxalamide (cas: 53118-43-7Recommanded Product: N1,N2-Di(pyridin-4-yl)oxalamide).

N1,N2-Di(pyridin-4-yl)oxalamide (cas: 53118-43-7) belongs to amides. Amides include many other important biological compounds, as well as many drugs like paracetamol, penicillin and LSD. Low-molecular-weight amides, such as dimethylformamide, are common solvents. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.Recommanded Product: N1,N2-Di(pyridin-4-yl)oxalamide

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

Bioactive compounds from medicinal plants: Focus on Piper species was written by Mgbeahuruike, E. E.;Yrjonen, T.;Vuorela, H.;Holm, Y.. And the article was included in South African Journal of Botany in 2017.Formula: C14H25NO The following contents are mentioned in the article:

This article reviews new discoveries related to the phytochem. and biol. activities of bioactive compounds from Piper species. It outlines the anticancer, anti-parasitic, and antimicrobial activities of Piper species in relation to drug discovery. The use of bioactive compounds from medicinal plants as therapeutic agents has been an important area in biomedical and natural product research. Piper species are effective medicinal plants used in folk medicine. They have traditionally been used to treat stomach ache, rheumatoid arthritis, diarrhea and other general infections, and their efficacy has been attributed to their bioactive compounds Bioactive compounds and extracts from Piper species have been examined and found to be of clin. importance for both malignant and non-malignant diseases. They have displayed pronounced efficacy as anticancer, antitumor and antimicrobial agents in various pharmacol. studies. They have been reported to possess anti-inflammatory, antioxidant, antibacterial, antifungal, and antimalarial activities. The alkaloids piperine, piperlongumine, guineensine, chabamide and pellitorine, which have been isolated from most Piper species, are able to inhibit the growth of cancer cell lines inducing apoptosis and acting as nuclear export inhibitors. These bioactive compounds can improve the effectiveness of chemotherapeutic drugs with minimal systemic toxicity to normal cells in cancer therapy. Pinoresinol, guineensine and other bioactive compounds from this species exhibited strong antimicrobial efficacy against various microorganisms including pathogenic Vibrio strains, which are often involved in host cell invasion during Vibrio cholera infection. The anticancer, antimicrobial and antimalarial properties of Piper species are compiled to support further exploration of their bioactive compounds for drug discovery. Biomedical and pharmacol. discoveries concerning their anticancer and antimicrobial properties are highlighted here for further clin. applications, which could pave the way for the proper therapeutic use of bioactive compounds and extracts from this plant species. This study involved multiple reactions and reactants, such as (2E,4E)-N-Isobutyldeca-2,4-dienamide (cas: 18836-52-7Formula: C14H25NO).

(2E,4E)-N-Isobutyldeca-2,4-dienamide (cas: 18836-52-7) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.Formula: C14H25NO

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

Bioactivity-guided isolation of alkamides from a cytotoxic fraction of the ethyl acetate extract of Anacyclus pyrethrum (L.) DC. roots. was written by Hamimed, Souad;Boulebda, Nadji;Laouer, Hocine;Belkhiri, Abdelmalik. And the article was included in Current Issues in Pharmacy and Medical Sciences in 2018.Recommanded Product: 18836-52-7 The following contents are mentioned in the article:

The alc. extract of Pellitory (Anacyclus pyrethrum) roots has been previously shown to exert anticancer activities on the Human Colorectal Cancer Cell Line (HCT) by targeting apoptosis, metastasis and cell cycle arrest. However, the nature of the cytotoxic mols. associated with this activity remains unexplored. This study aims to reinvestigate Pellitory root extract as regard to its cytotoxic activity and to proceed to a bioguided fractionation to explore its active fraction and to give new insight in their phytochem. constituents. Powd. roots were subjected to repeated extraction with Petroleum ether (Pe), Chloroform (Ch), Et acetate (Ea) and Methanol (Me). Pellitory extracts were then screened for cytotoxic activity using the Brine Shrimp Lethality (BSL) bioassay. Ea extract exhibited a marked cytotoxic activity, with LC₅₀ of 249.26 μg/mL in the BSL bioassay. The remaining extracts (Pe,Ch,Me) treated groups exhibited no or low mortality in the range of tested concentrations (1-1000 μg/mL). BSL assay-guided chromatog. fractionation of Ea active Extract revealed a highly cytotoxic fraction (F11) with LC₅₀ of 42.5 μg/mL. Multistep purifications of the active F11 fraction afforded four alkamides, namely N-isobutyldeca-2,4-dienamide or Pellitorine (I), N-propyldodeca- -2,8-dienamide (II), N-isobutyltetradeca-2,4-dienamide (III) and N-propylnona-2,5- -dienamide (IV). This study suggests that cytotoxic activity is localized mainly in the Et acetate extract (Ea) of pellitory roots. BSL assay fractionation of this active extract leads to the isolation of four alkamides, including pellitorine (I). While this iso-Bu alkamide has previously shown strong cytotoxic activities against human cancer cell lines, the other compounds (II to IV) were not previously reported as cytotoxic. Subsequently, the isolated alkamides will be considered in future study as candidates for in depth in-vitro evaluation of their cytotoxicity against cancer and normal cell lines. Finally, through this study, BSL assay demonstrate again its usefulness as bench-top assay in exploring plant extracts for cytotoxic compounds This study involved multiple reactions and reactants, such as (2E,4E)-N-Isobutyldeca-2,4-dienamide (cas: 18836-52-7Recommanded Product: 18836-52-7).

(2E,4E)-N-Isobutyldeca-2,4-dienamide (cas: 18836-52-7) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.Recommanded Product: 18836-52-7

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

Novel Strategy for Untargeted Chiral Metabolomics using Liquid Chromatography-High Resolution Tandem Mass Spectrometry was written by Pandey, Renu;Collins, Meghan;Lu, Xiyuan;Sweeney, Shannon R.;Chiou, Jennifer;Lodi, Alessia;Tiziani, Stefano. And the article was included in Analytical Chemistry (Washington, DC, United States) in 2021.Safety of ((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate The following contents are mentioned in the article:

Stereospecific recognition of metabolites plays a significant role in the detection of potential disease biomarkers thereby providing new insights in diagnosis and prognosis. D-Hdroxy/amino acids are recognized as potential biomarkers in several metabolic disorders. Despite continuous advances in metabolomics technologies, the simultaneous measurement of different classes of enantiomeric metabolites in a single anal. run remains challenging. Here, we develop a novel strategy for untargeted chiral metabolomics of hydroxy/amine groups (-OH/-NH₂) containing metabolites, including all hydroxy acids (HAs) and amino acids (AAs), by chiral derivatization coupled with liquid chromatog.-high resolution tandem mass spectrometry (LC-HR-MS/MS). Diacetyl-tartaric anhydride (DATAN) was used for the simultaneous derivatization of-OH/-NH₂ containing metabolites as well as the resulting diastereomers, and all the derivatized metabolites were resolved in a single anal. run. Data independent MS/MS acquisition (DIA) was applied to pos. identify DATAN-labeled metabolites based on reagent specific diagnostic fragment ions. We discriminated chiral from achiral metabolites based on the reversal of elution order of D and L isomers derivatized with the enantiomeric pair (±) of DATAN in an untargeted manner. Using the developed strategy, a library of 301 standards that consisted of 214 chiral and 87 achiral metabolites were separated and detected in a single anal. run. This approach was then applied to investigate the enantioselective metabolic profile of the bone marrow (BM) and peripheral blood (PB) plasma samples from patients with acute myeloid leukemia (AML) at diagnosis and following completion of the induction phase of chemotherapeutic treatment. The sensitivity and selectivity of the developed method enabled the detection of trace levels of the D-enantiomer of HAs and AAs in primary plasma patient samples. Several of these metabolites were significantly altered in response to chemotherapy. The developed LC-HR-MS method entails a valuable step forward in chiral metabolomics. This study involved multiple reactions and reactants, such as ((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate (cas: 1094-61-7Safety of ((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate).

((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate (cas: 1094-61-7) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. Amides can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.Safety of ((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate

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

Simultaneous determination of five N-alkylamides in the root of Anacyclus pyrethrum by HPLC and profiling of components in its methanolic root extract by UPLC/Q-TOF-MS was written by Ji, Ruifang;Quan, Qinghua;Guo, Xiaoyu;Zhang, Jiamei;Song, Yongli;Zhu, Mengting;Tan, Peng;Han, Jing;Liu, Yonggang. And the article was included in Revista Brasileira de Farmacognosia in 2019.Formula: C14H25NO The following contents are mentioned in the article:

The root of Anacyclus pyrethrum (L.) Lag., Asteraceae, is very widely used for treating various diseases in Traditional Uygur Medicine, particularly in the treatment of vitiligo. However, there have been few studies on the quality standards of A. pyrethrum in China. A. pyrethrum contains abundant N-alkylamides, which are considered to be the principal components. Therefore, based on the previous research in our group, six N-alkylamides were obtained by using column chromatog. We used ultra-performance liquid chromatog. quadrupole time-of-flight mass spectrometry to determine the mass spectrometry cleavage mechanism of these six monomer components and established the mass spectrometry cleavage law of N-alkylamides. Then, we used the ultra-performance liquid chromatog. quadrupole time-of-flight mass spectrometry method to rapidly identify and analyze the N-alkylamide components of the A. pyrethrum methanol extract Finally, twenty N-alkylamides were identified, including eleven N-isobutylamides, two N-Me isobutylamides, six 4-hydroxyphenylethyl-amide and one 2-phenylethylamide. Five of these compounds were identified as new compounds that have not been reported to date. Two of these compounds were identified for the first time in this herb. Therefore, this work provides an approach for the quality anal. of N-alkylamides in the root of A. pyrethrum. A search of the literature showed that the content determination in the A. pyrethrum quality standard is still a remaining problem. N-alkylamides are the main components of A. pyrethrum. Even though ultra-performance liquid chromatog. quadrupole time-of-flight mass spectrometry has the advantages of lower time and higher efficiency compared to high-performance liquid chromatog., considering the ease of repeatability and universality of the quality control method, we chose to use high-performance liquid chromatog. for content determination In this experiment, high-performance liquid chromatog. was used for the first time to establish a simple, rapid and accurate method for evaluating the N-alkylamide content in A. pyrethrum with five N-alkylamides used as the standards Finally, this work provides a qual. and quant. method for the anal. of N-alkylamides in A. pyrethrum, improving the quality control standards for A. pyrethrum. This study involved multiple reactions and reactants, such as (2E,4E)-N-Isobutyldeca-2,4-dienamide (cas: 18836-52-7Formula: C14H25NO).

(2E,4E)-N-Isobutyldeca-2,4-dienamide (cas: 18836-52-7) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Formula: C14H25NO

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

HIV-1 Reverse Transcriptase Inhibition by Major Compounds in a Kenyan Multi-Herbal Composition (CareVid): In Vitro and In Silico Contrast was written by Rotich, Winnie;Sadgrove, Nicholas J.;Mas-Claret, Eduard;Padilla-Gonzalez, Guillermo F.;Guantai, Anastasia;Langat, Moses K.. And the article was included in Pharmaceuticals in 2021.Formula: C14H25NO The following contents are mentioned in the article:

CareVid is a multi-herbal product used in southwest Kenya as an immune booster and health tonic and has been anecdotally described as improving the condition of HIV-pos. patients. The product is made up of roots, barks and whole plant of 14 African medicinal plants: Acacia nilotica (L.) Willd. ex Delile (currently, Vachelia nilotica (L.) P.J.H Hurter & Mabb.), Adenia gummifera (Harv.) Harms, Anthocleista grandiflora Gilg, Asparagus africanus Lam., Bersama abyssinica Fresen., Clematis hirsuta Guill. & Perr., Croton macrostachyus Hochst. ex Delile, Clutia robusta Pax (accepted as Clutia kilimandscharica Engl.), Dovyalis abyssinica (A. Rich.) Warb, Ekebergia capensis Sparm., Periploca linearifolia Qt.-Dill. & A. Rich., Plantago palmata Hook.f., Prunus africana Hook.f. Kalkman and Rhamnus prinoides L′Her. The objective of this study was to determine the major chem. constituents of CareVid solvent extracts and screen them for in vitro and in silico activity against the HIV-1 reverse transcriptase enzyme. To achieve this, CareVid was sep. extracted using CH2Cl2, MeOH, 80% EtOH in H2O, cold H2O, hot H2O and acidified H2O (pH 1.5-3.5). The extracts were analyzed using HPLC-MS equipped with UV diode array detection. HIV-1 reverse transcriptase inhibition was performed in vitro and compared to in silico HIV-1 reverse transcriptase inhibition, with the latter carried out using MOE software, placing the docking on the hydrophobic pocket in the subdomain of p66, the NNRTI pocket. The MeOH and 80% EtOH extracts showed strong in vitro HIV-1 reverse transcriptase inhibition, with an EC50 of 7 μg·mL-1. The major components were identified as sucrose, citric acid, ellagic acid, catechin 3-hexoside, epicatechin 3-hexoside, procyanidin B, hesperetin O-rutinoside, pellitorine, mangiferin, isomangiferin, 4-O-coumaroulquinic acid, ellagic acid, ellagic acid O-pentoside, crotepoxide, oleuropein, magnoflorine, tremulacin and an isomer of dammarane tetrol. Ellagic acid and procyanidin B inhibited the HIV-1 reverse transcription process at 15 and 3.2 μg/mL-1, resp. Docking studies did not agree with in vitro results because the best scoring ligand was crotepoxide (ΔG = -8.55 kcal/mol), followed by magnoflorine (ΔG = -8.39 kcal/mol). This study showed that CareVid has contrasting in vitro and in silico activity against HIV-1 reverse transcriptase. However, the strongest in vitro inhibitors were ellagic acid and procyanidin B. This study involved multiple reactions and reactants, such as (2E,4E)-N-Isobutyldeca-2,4-dienamide (cas: 18836-52-7Formula: C14H25NO).

(2E,4E)-N-Isobutyldeca-2,4-dienamide (cas: 18836-52-7) belongs to amides. Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis. In simple aromatic amides, fragmentation occurs on both sides of the carbonyl group. If a hydrogen is available in N-substituted aromatic amides, it tends to migrate and form an aromatic amine and the loss of a ketene.Formula: C14H25NO

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

Nicotinic acid mononucleotide is an allosteric SARM1 inhibitor promoting axonal protection was written by Sasaki, Yo;Zhu, Jian;Shi, Yun;Gu, Weixi;Kobe, Bostjan;Ve, Thomas;DiAntonio, Aaron;Milbrandt, Jeffrey. And the article was included in Experimental Neurology in 2021.Quality Control of ((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate The following contents are mentioned in the article:

SARM1 is an inducible NAD⁺ hydrolase that is the central executioner of pathol. axon loss. Recently, we elucidated the mol. mechanism of SARM1 activation, demonstrating that SARM1 is a metabolic sensor regulated by the levels of NAD⁺ and its precursor, NMN (NMN), via their competitive binding to an allosteric site within the SARM1 N-terminal ARM domain. In healthy neurons with abundant NAD⁺, binding of NAD⁺ blocks access of NMN to this allosteric site. However, with injury or disease the levels of the NAD⁺ biosynthetic enzyme NMNAT2 drop, increasing the NMN/ NAD⁺ ratio and thereby promoting NMN binding to the SARM1 allosteric site, which in turn induces a conformational change activating the SARM1 NAD⁺ hydrolase. Hence, NAD⁺ metabolites both regulate the activation of SARM1 and, in turn, are regulated by the SARM1 NAD⁺ hydrolase. This dual upstream and downstream role for NAD⁺ metabolites in SARM1 function has hindered mechanistic understanding of axoprotective mechanisms that manipulate the NAD⁺ metabolome. Here we reevaluate two methods that potently block axon degeneration via modulation of NAD⁺ related metabolites, 1) the administration of the NMN biosynthesis inhibitor FK866 in conjunction with the NAD⁺ precursor nicotinic acid riboside (NaR) and 2) the neuronal expression of the bacterial enzyme NMN deamidase. We find that these approaches not only lead to a decrease in the levels of the SARM1 activator NMN, but also an increase in the levels of the NAD⁺ precursor nicotinic acid mononucleotide (NaMN). We show that NaMN inhibits SARM1 activation, and demonstrate that this NaMN-mediated inhibition is important for the long-term axon protection induced by these treatments. Anal. of the NaMN-ARM domain co-crystal structure shows that NaMN competes with NMN for binding to the SARM1 allosteric site and promotes the open, autoinhibited configuration of SARM1 ARM domain. Together, these results demonstrate that the SARM1 allosteric pocket can bind a diverse set of metabolites including NMN, NAD⁺, and NaMN to monitor cellular NAD⁺ homeostasis and regulate SARM1 NAD⁺ hydrolase activity. The relative promiscuity of the allosteric site may enable the development of potent pharmacol. inhibitors of SARM1 activation for the treatment of neurodegenerative disorders. This study involved multiple reactions and reactants, such as ((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate (cas: 1094-61-7Quality Control of ((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate).

((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate (cas: 1094-61-7) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.Quality Control of ((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate

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

Nicotinic acid mononucleotide is an allosteric SARM1 inhibitor promoting axonal protection was written by Sasaki, Yo;Zhu, Jian;Shi, Yun;Gu, Weixi;Kobe, Bostjan;Ve, Thomas;DiAntonio, Aaron;Milbrandt, Jeffrey. And the article was included in Experimental Neurology in 2021.Category: amides-buliding-blocks The following contents are mentioned in the article:

SARM1 is an inducible NAD⁺ hydrolase that is the central executioner of pathol. axon loss. Recently, we elucidated the mol. mechanism of SARM1 activation, demonstrating that SARM1 is a metabolic sensor regulated by the levels of NAD⁺ and its precursor, NMN (NMN), via their competitive binding to an allosteric site within the SARM1 N-terminal ARM domain. In healthy neurons with abundant NAD⁺, binding of NAD⁺ blocks access of NMN to this allosteric site. However, with injury or disease the levels of the NAD⁺ biosynthetic enzyme NMNAT2 drop, increasing the NMN/ NAD⁺ ratio and thereby promoting NMN binding to the SARM1 allosteric site, which in turn induces a conformational change activating the SARM1 NAD⁺ hydrolase. Hence, NAD⁺ metabolites both regulate the activation of SARM1 and, in turn, are regulated by the SARM1 NAD⁺ hydrolase. This dual upstream and downstream role for NAD⁺ metabolites in SARM1 function has hindered mechanistic understanding of axoprotective mechanisms that manipulate the NAD⁺ metabolome. Here we reevaluate two methods that potently block axon degeneration via modulation of NAD⁺ related metabolites, 1) the administration of the NMN biosynthesis inhibitor FK866 in conjunction with the NAD⁺ precursor nicotinic acid riboside (NaR) and 2) the neuronal expression of the bacterial enzyme NMN deamidase. We find that these approaches not only lead to a decrease in the levels of the SARM1 activator NMN, but also an increase in the levels of the NAD⁺ precursor nicotinic acid mononucleotide (NaMN). We show that NaMN inhibits SARM1 activation, and demonstrate that this NaMN-mediated inhibition is important for the long-term axon protection induced by these treatments. Anal. of the NaMN-ARM domain co-crystal structure shows that NaMN competes with NMN for binding to the SARM1 allosteric site and promotes the open, autoinhibited configuration of SARM1 ARM domain. Together, these results demonstrate that the SARM1 allosteric pocket can bind a diverse set of metabolites including NMN, NAD⁺, and NaMN to monitor cellular NAD⁺ homeostasis and regulate SARM1 NAD⁺ hydrolase activity. The relative promiscuity of the allosteric site may enable the development of potent pharmacol. inhibitors of SARM1 activation for the treatment of neurodegenerative disorders. This study involved multiple reactions and reactants, such as ((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate (cas: 1094-61-7Category: amides-buliding-blocks).

((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate (cas: 1094-61-7) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole. The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Category: amides-buliding-blocks

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Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics