Tag: M.W=400-600

Othman, Zaidatul Akmal; Zakaria, Zaida; Suleiman, Joseph Bagi; Ghazali, Wan Syaheedah Wan; Mohamed, Mahaneem published the artcile< Anti-atherogenic effects of orlistat on obesity-induced vascular oxidative stress rat model>, Computed Properties of 96829-58-2, the main research area is orlistat antiatherogenic antioxidant glutathione peroxidase obesity oxidative stress; anti-inflammatory; antioxidant; atherosclerosis; obesity; orlistat.

Obesity is typically linked to oxidative stress and inflammation, which lead to vascular damage and initiate the progression of atherosclerosis. The aim of this study was to determine the anti-atherosclerotic effect of orlistat on obesity-induced vascular oxidative stress in obese male rats. Twenty-four male Sprague-Dawley rats were categorized into two groups: normal (Normal group, n = 6) and high-fat diet (HFD group, n = 12). After six weeks, obese rats in the HFD group were administered either with distilled water (OB group) or orlistat 10 mg/kg/day (OB/OR group) for another six weeks. The OB group had a significant increase in lipid profiles (total cholesterol (TC), triglyceride (TG), low-d. lipoprotein (LDL)) and decrease in high-d. lipoprotein (HDL) level compared to the Normal group. The aortic antioxidants enzymes activities (superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GR), glutathione S-transferase (GST), and catalase (CAT)) as well as total glutathione (GSH) and total antioxidant capacity (TAC) of the OB group were significantly decreased compared to the Normal group. Furthermore, pro-inflammatory atherosclerotic markers (tumor necrosis factor-alpha (TNF-a), vascular cell adhesion mol.-1 (VCAM-1), and intercellular cell adhesion mol.-1 (ICAM-1)) expressions were increased significantly, and anti-inflammatory marker (interleukin-10 (IL-10)) was decreased significantly in the OB group compared to the Normal group. Treatment with orlistat significantly improved lipid profile, increased antioxidant enzymes and expression of anti-inflammatory markers, and decreased the expression of the pro-inflammatory marker compared to the OB group. These findings may suggest the therapeutic effect of orlistat in attenuating the progression of the atherosclerotic stage in obesity.

Antioxidants published new progress about Anti-inflammatory agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Computed Properties of 96829-58-2.

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

Liu, Jingying; Werner, Ulrich; Funke, Mario; Besenius, Melissa; Saaby, Lasse; Fanoe, Mathias; Mu, Huiling; Mullertz, Anette published the artcile< SEDDS for intestinal absorption of insulin: Application of Caco-2 and Caco-2/HT29 co-culture monolayers and intra-jejunal instillation in rats>, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is insulin emulsion intestine; Caco-2 monolayers; Caco-2/HT29-MTX co-culture monolayers; Insulin; Intestinal barrier; Intra-jejunal administration; Monoacyl phosphatidylcholine; Self-emulsifying drug delivery systems.

To face the challenges of oral delivery of peptide and protein (P/P) drugs, self-emulsifying drug delivery systems (SEDDSs) containing monoacyl phosphatidylcholine (MAPC), Labrasol (LAB) and medium-chain (MC) monoglycerides as permeation enhancers (PEs) were evaluated for their effect on intestinal absorption of insulin. In this study, insulin was complexed with phosphatidylcholine (SPC) to form an insulin-SPC complex (ins-SPC) with increased lipophilicity. The following three SEDDSs: MCT(MAPC) (MC triglycerides and MAPC included), MCT(RH40) (MC triglycerides and Kolliphor RH40 included) and LCT(MAPC) (long-chain triglycerides and MAPC included) were loading with ins-SPC (4% or 8% weight/weight of SPC). Three SEDDSs generated emulsions with droplet sizes between 50 and 470 nm and with zeta potentials between -5 to -25 mV in a simulated intestinal medium. Mucus-secreting Caco-2/HT29-MTX-E12 co-culture and Caco-2 monolayers were used as in vitro cell transport models to investigate insulin permeability. In comparison to insulin HBSS solution, MCT(MAPC) significantly increased the insulin permeability across co-culture and Caco-2 monolayers (2.0-2.5 × 10-7 cm/s). In an intra-jejunal (i.j.) instillation model in rats, MCT(RH40) significantly decreased the rat blood glucose after 0.5 h by 17.0 ± 2.5% and for MCT(MAPC), it was 23.6 ± 10.6%. Furthermore, a lipase inhibitor orlistat was incorporated into MCT(MAPC) to evaluate the effect of lipid digestion on insulin absorption. Results indicated that the incorporation of orlistat did not significantly alter the in vivo insulin absorption. Overall, the SEDDS MCT(MAPC) composed of natural PEs (MAPC and MC glycerides) and synthetic PE (LAB) significantly increased the intestinal absorption of insulin upon i.j. instillation. Although it is not possible to conclude if a single PE is dominating the intestinal absorption of insulin, MCT(MAPC) seems to have the potential for oral insulin delivery.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about Antidiabetic agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

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

Kumar, Nitheesh; J., Narayanan; V., Chitra published the artcile< A mechanistic review of anti-obesity drugs>, Product Details of C29H53NO5, the main research area is review antiobesity drug.

A review. Obesity is a complicated disease, characterized by an immoderate amount of fat in a human body. Obesity is not alone a point of concern from a cosmetic sector, also affect health problems. The different factor involves in obesity such as genetic factor, environment factor, energy balance dysregulation, metabolic factor. It can be determined by Body Mass Index as well as Body Adiposity Index value and can be controlled by different methods like drugs and nature compounds This paper reviews on the Food and Drug Administration approved drugs for obesity recently like Semaglutide, bupropion naltrexone, liraglutide, lorcaserin, orlistat, and phentermine topiramate. The natural compounds Salvia officinalis (Lamiaceae), Vitis vinifera (Vitaceae), Arachis hypogaea (Fabaceae), Panax japonicus (Araliaceae).

Natural Volatiles & Essential Oils published new progress about Antiobesity agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Product Details of C29H53NO5.

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

Mandal, Sumit Kumar; Kumar, Banoth Karan; Sharma, Pankaj Kumar; Murugesan, Sankaranarayanan; Deepa, P. R. published the artcile< In silico and in vitro analysis of PPAR - α / γ dual agonists: Comparative evaluation of potential phytochemicals with anti-obesity drug orlistat>, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is Molecular docking; Molecular dynamics; Obesity; Orlistat; Peroxisome proliferator activated receptor alpha/ gamma; Phytochemicals.

Obesity is an abnormal fat accumulation disorder in the metabolic syndrome constellation, and a risk factor for diabetes, cardiovascular disorders, non-alc. fatty liver disease (NAFLD), and cancer. Nuclear receptors (Peroxisome proliferator-activated receptor, PPAR) are implicated in metabolic syndrome and NAFLD, and have potential for therapeutic targeting. Nuclear receptors are ligand-dependent transcription factors that have diverse roles in metabolism, including regulating genes involved in lipid and glucose metabolism, modulating inflammatory genes, and are crucial for maintaining metabolic flexibility. PPAR activates adipose triglyceride lipase, which then releases fatty acids as ligands for PPAR, indicating the interdependency of nuclear receptors and lipases. Here, mol. docking was performed with selected phytochem. ligands that can bind with PPAR-α/γ (PDB ID: 2ZNN and 2ATH, resp.) using Glide module of Schrodinger software followed by mol. dynamics simulation study using Desmond module, and ADMET anal. Interestingly, orlistat which is a well-known lipase and fatty acid synthase inhibitor also demonstrated favorable binding affinity with both PPAR-α/γ (-10.96 kcal/mol against PPARα and -10.26 kcal/mol against PPARγ). The highest docking scores were however shown by the flavonoids – rutin (-14.88 kcal/mol against PPARα and -13.64 kcal/mol against PPARγ), and its aglycon, quercetin (-10.08 kcal/mol in PPARα and -9.89 kcal/mol in PPARγ). The other phytochems. (genistein, esculin, daidzin, naringenin, daidzein, dihydroxy coumarin, hydroquinone) showed lower binding affinity as dual agonists. The anti-obesity effects were exptl. validated in cultured adipocytes, which revealed better lipid inhibition by rutin and quercetin than orlistat (quercetin > rutin > orlistat) pointing to their strong potential in anti-obesity treatment.

Computers in Biology and Medicine published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

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

Subandi; Nurowidah, Anis published the artcile< The Potency of Carica papaya L. seeds powder as antiobesity 'coffee' drinks>, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is antiobesity Carica papaya seed pancreatic lipase inhibitor.

Previous studies have shown that papaya seed contained flavonoids, tannins, and saponins Those compounds are potential as an inhibitor for pancreatic lipase, an enzyme that plays an important role for lipid absorption into the body. The aims of this study are to produce ‘coffee’ powder of papaya seeds for drinks; to test the organoleptic properties and the activity as a pancreatic lipase inhibitor. The seed was made into a powder by washing, sun drying, roasting, and then grinding. An organoleptic test was performed at 50 respondents and one trained respondent. Inhibitor activity for pancreatic lipase was measured relative to anti-obesity drugs of Orlistat (Xenical), using titrimetric method. The results showed that every 1.42 g of papaya seeds powder have an inhibitory activity equivalent to 1 tablet (120 mg) of Orlistat. Most of the respondents like with the texture, color, and flavor of the drinks.

IOP Conference Series: Materials Science and Engineering published new progress about Antiobesity agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

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

Huo, Peng-Chao; Hu, Qing; Shu, Sheng; Zhou, Qi-Hang; He, Rong-Jing; Hou, Jie; Guan, Xiao-Qing; Tu, Dong-Zhu; Hou, Xu-Dong; Liu, Peng; Zhang, Nan; Liu, Zhi-Guo; Ge, Guang-Bo published the artcile< Design, synthesis and biological evaluation of novel chalcone-like compounds as potent and reversible pancreatic lipase inhibitors>, Product Details of C29H53NO5, the main research area is pancreatic lipase inhibition chalcone antiobesity agent; Anti-obesity agent; Chalcone-like compounds; Inhibition; Pancreatic lipase (PL).

Pancreatic lipase (PL), a crucial enzyme responsible for hydrolysis of dietary lipids, has been validated as a key therapeutic target to prevent and treat obesity-associated metabolic disorders. Herein, we report the design, synthesis and biol. evaluation of a series of chalcone-like compounds as potent and reversible PL inhibitors. Following two rounds of structural modifications at both A and B rings of a chalcone-like skeleton, structure-PL inhibition relationships of the chalcone-like compounds were studied, while the key substituents that would be beneficial for PL inhibition were revealed. Among all tested chalcone-like compounds, compound B13 (a novel chalcone-like compound bearing two long carbon chains) displayed the most potent PL inhibition activity, with an IC50 value of 0.33 μM. Inhibition kinetic analyses demonstrated that B13 could potently inhibit PL-mediated 4-MUO hydrolysis in a mixed inhibition manner, with the Ki value of 0.12 μM. Mol. docking simulations suggested that B13 could tightly bind on PL at both the catalytic site and a non-catalytic site that was located on the surface of PL, which was consistent with the mixed inhibition mode of this agent. In addition, B13 displayed excellent stability in artificial gastrointestinal fluids and good metabolic stability in human liver preparations Collectively, our findings suggested that chalcone-like compounds were good choices for design and development of orally administrated PL inhibitors, while B13 could be served as a promising lead compound to develop novel anti-obesity agents via targeting on PL.

Bioorganic & Medicinal Chemistry published new progress about Antiobesity agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Product Details of C29H53NO5.

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

Zhou, Xiaqing; Chang, Tzu-Lan; Chen, Shuang; Liu, Tianchi; Wang, Haoyu; Liang, Jun F. published the artcile< Polydopamine-Decorated Orlistat-Loaded Hollow Capsules with an Enhanced Cytotoxicity against Cancer Cell Lines>, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is polydopamine orlistat capsule cancer antitumor; cancer therapy; controlled release; hollow capsule; nanoparticle; orlistat; polydopamine.

Orlistat, an FDA-approved antiobesity drug, has recently been shown to have anticancer effects. However, orlistat is extremely hydrophobic with low absorption. Therefore, new approaches are needed to effectively deliver orlistat for cancer therapy. Herein, we developed a fast and simple method to use polydopamine-coated hollow capsule (PHC) as a drug nanocarrier for enhancing the therapeutic effects of orlistat. Orlistat-loaded PHC had an average size of 200 nm, which was characterized by using dynamic light scattering and scanning electron microscope. Furthermore, the polydopamine layer provided an excellent control of orlistat release because it was extremely sensitive to pH values. The cellular uptake and cytotoxicity experiments were performed to show that orlistat packaged in PHC could be endocytosed into cells and then significantly improved the cytotoxic activity against cancer cell lines in a short time compared with free orlistat. Moreover, dynamic study of cell membrane lysis was performed by staining with the LIVE/DEAD kit to demonstrate the cancer-killing mechanism. The size of the cell surface area has also been proven to be a key parameter which affected drug efficacy. Taken all together, these results present that orlistat-loaded PHC is a very promising formula for cancer treatments.

Molecular Pharmaceutics published new progress about Antitumor agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

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

Noori, Soheila; Mirzababaei, Atieh; Amini, Mohammad Reza; Clark, Cain C. T.; Mirzaei, Khadijeh published the artcile< Effect of orlistat on serum uric acid level in adults: A systematic review and meta-analysis of randomised controlled trials>, Quality Control of 96829-58-2, the main research area is meta analysis orlistat uric acid reducing agent hyperuricemia.

Hyperuricemia increases the risk of gout and cardiovascular diseases. Obesity increases the risk of hyperuricemia while weight loss (>5 kg) has been reported to decrease urate. The effects of orlistat on serum uric acid (SUA) are still controversial. The aim of this meta-anal. was to evaluate the influence of orlistat on SUA levels in adults. Relevant studies, published up to May 2020, were searched systematically through PubMed/Medline, Scopus and Google Scholar. All relevant randomised controlled clin. trials were included. Meta-anal. was performed using random-effect model. Subgroup anal., sensitivity anal. and meta-regression were also carried out. Overall 7 trials (9 datasets) that enrolled 1786 subjects were included. Orlistat showed in a significant change in SUA level (Difference in means: -17.661μmol, 95% CI: -31.615 to -3.707, P = .01). A low heterogeneity observed across the studies (I2 = 25.119%). After categorising studies on the basis of duration and sample size, the effect of orlistat on SUA was significant. The results of meta-regression were showed that significant relationships were not found between orlistat and SUA in the duration of intervention. We found a significant reduction in SUA following orlistat therapy in adults.

International Journal of Clinical Practice published new progress about Adult, mammalian. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Quality Control of 96829-58-2.

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

Polyzos, Stergios A.; Kountouras, Jannis; Mantzoros, Christos S. published the artcile< Obesity and nonalcoholic fatty liver disease: From pathophysiology to therapeutics>, Safety of (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is review obesity nonalcoholic fatty liver disease pathophysiol therapeutic; Adipose tissue; Metabolic syndrome; Nonalcoholic fatty liver disease; Nonalcoholic steatohepatitis; Obesity; Treatment.

A review. The obesity epidemic is closely associated with the rising prevalence and severity of nonalcoholic fatty liver disease (NAFLD): obesity has been linked not only with simple steatosis (SS), but also with advanced disease, i.e., nonalcoholic steatohepatitis (NASH), NASH-related cirrhosis and hepatocellular carcinoma. As a consequence, apart from increasing all-cause mortality, obesity seems to increase liver-specific mortality in NAFLD patients. Given the lack of approved pharmacol. interventions for NAFLD, targeting obesity is a rational option for its management. As the first step, lifestyle modification (diet and exercise) is recommended, although it is difficult to achieve and sustain. When the first step fails, adding pharmacotherapy is recommended. Several anti-obesity medications have been investigated in NAFLD (e.g., orlistat, glucagon-like peptide-1 analogs), other anti-obesity medications have not been investigated (e.g., lorcaserin, phentermine hydrochloric, phentermine/topiramate and naltrexone/bupropion), whereas some medications with weight-lowering efficacy have not been approved for obesity (e.g., sodium-glucose cotransporter-2 inhibitors, farnesoid X receptor ligands). If the combination of lifestyle modification and pharmacotherapy also fails, then bariatric surgery should be considered in selected morbidly obese individuals. This review summarizes best evidence linking obesity with NAFLD and presents related therapeutic options.

Metabolism, Clinical and Experimental published new progress about Antiobesity agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Safety of (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

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