Category: 96829-58-2

Kumar, Ashwani; Chauhan, Shilpi published the artcile< Pancreatic lipase inhibitors: The road voyaged and successes>, HPLC of Formula: 96829-58-2, the main research area is review orlistat antiobesity agent obesity; Antiobesity therapeutics; Orlistat; Pancreatic lipase enzyme; Pancreatic lipase inhibitors; Triacylglycerides.

A review. Human pancreatic lipase (triacylglycerol acyl hydrolase EC3.1.1.3) is the most widely studied member of the human lipase superfamily related to carboxyl esterase. It is secreted from the acinar cell of pancreas and has strong preference for triacylglycerides over cholesterol esters, phospholipids, and galactolipids. Apart from the hydrolysis of triacylglycerides, pancreatic lipase may cause the hydrolysis of retinyl esters in vivo. So, it is very much evidenced that pancreatic lipase with its cofactor colipase has prominent role in efficient digestion of dietary fat. Hence, the modulation of human pancreatic lipase may represent a new insight in the discovery of a number of therapeutics that can inhibit the absorption of fat in body and can be used in obesity and other related metabolic disorders. Even, the only Food and drug administration (FDA) approved antiobesity drug, orlistat, is also an inhibitor of pancreatic lipase. This review summarizes studies about structure, mechanistic approach of pancreatic lipase enzyme while emphasizing on the various synthetic pancreatic lipase inhibitors with their structure activity relationship (SAR).

Life Sciences published new progress about Antiobesity agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, HPLC of Formula: 96829-58-2.

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

Khalil, Hanan; Ellwood, Laura; Lord, Heidi; Fernandez, Ritin published the artcile< Pharmacological Treatment for Obesity in Adults: An Umbrella Review.>, Application In Synthesis of 96829-58-2, the main research area is obesity; obesity medications; pharmacotherapy; umbrella review; weight loss.

Objective: To synthesize the evidence from systematic reviews of clinical trials investigating the effectiveness of pharmacological therapies approved by the Australian Therapeutic Goods Administration and the US Food and Drug Administration for the management of obesity in adults. Data Sources: A 3-step literature search of the MEDLINE, EMBASE, CINAHL, and PubMed databases was conducted between March and May 2019. The key terms used were obesity, pharmacological therapy, antiobesity agent, antiobesity medication, weight loss, and systematic review. Study Selection and Data Extraction: Systematic reviews that evaluated the effectiveness of pharmacological therapies for the management of obesity in patients with a body mass index of or greater than 25 kg/m2. Data Synthesis: Nine systematic reviews involving three pharmacotherapies, liraglutide, orlistat, and naltrexone-bupropion were identified. The results indicate that the pharmacotherapies reduced weight when compared with placebo. Orlistat was effective in significantly reducing fasting blood glucose, HbA1c, total cholesterol, triglycerides, and systolic and diastolic blood pressure. All reviews discussed the presence or risk of gastrointestinal adverse effects including diarrhea, vomiting, and nausea related to orlistat and liraglutide. Relevance to Patient Care and Clinical Practice: This umbrella review compares the efficacy and safety of antiobesity medications for reducing weight and a discussion on their weight loss and metabolic control to guide clinicians when prescribing medications for obesity. Conclusions: All pharmacological therapies included in this review are superior to placebo in reducing weight. Clinicians should consider patient comorbidities and risk of adverse events when recommending medications for weight loss.

The Annals of pharmacotherapy published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Application In Synthesis of 96829-58-2.

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

Adel Fathy, Shrouk; Ibrahim, Amany K.; Eltamany, Enas E.; Badr, Jihan M. published the artcile< A developed high-performance thin-layer chromatographic method for the determination of orlistat in pharmaceutical preparations>, 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 high performance thin layer chromatog orlistat pharmaceutical preparation.

A sensitive and simple high-performance thin-layer chromatog. method is developed and validated according to the International Conference on Harmonisation (ICH) guidelines. The procedure was applied for the estimation of orlistat in different pharmaceutical preparations In the proposed method, thin-layer chromatog. aluminum sheets pre-coated with silica gel were employed as the stationary phase. A number of solvent mixtures were used as the mobile phase for trials to obtain compact bands of orlistat. The solvent mixture consisting of chloroform and methanol (98:2) was found to be the best. The data obtained from the calibration curves of standard orlistat showed a good linear relationship over the concentration range of 1000-3800 ng per band with respect to the area. Scanning was performed at λ = 200 nm, where the correlation coefficient (R2) was 0.970, and the linear regression equation was found to be: y = 4.1419x – 4181.1. After revealing of the spots by anisaldehyde-concentrate sulfuric acid, compact violet bands were obtained and, accordingly, scanning was performed at λ = 600 nm, where a good linear relationship over the concentration range of 600-4000 ng per band with respect to the area was obtained. The correlation coefficient (R2) was 0.991 with a linear regression equation: y = 4.025x – 1159.3. The method was evaluated regarding accuracy, precision, limits of detection and quantification, and robustness. Revealing of the spots by anisaldehyde-concentrate sulfuric acid improved the sensitivity of the method and increased the range within which a linear relationship between concentration and response occurs.

Journal of Planar Chromatography–Modern TLC 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

Joyce, Paul; Meola, Tahlia R.; Schultz, Hayley B.; Prestidge, Clive A. published the artcile< Biomaterials that regulate fat digestion for the treatment of obesity>, Application of C29H53NO5, the main research area is review biomaterial fat digestion obesity.

Obesity is a rapidly growing concern worldwide, with over one-third of the global population classified as overweight or obese. While significant research has focused on developing new and improved nutritional and dietary approaches for regulating energy intake, there has been little success in overcoming the rising obesity statistics. Consequently, increasing attention is being afforded to designing safe, inexpensive and highly efficacious food-based materials that control fat and carbohydrate bioavailability in order to successfully manage the nutritional value of our food and combat chronic diseases associated with obesity, such as heart disease and diabetes. This review focuses on bioactive and nanostructured materials that have been shown to regulate energy intake by (i) manipulating the fat digestion process, and/or (ii) restricting the absorption of fat digestion products into the systemic bloodstream. The mechanistic approach of such technologies will be discussed in detail, with corresponding preclin. and clin. findings highlighted, to provide insights for the design and development of future anti-obesity therapeutics. Bioactive materials that regulate the fat digestion and absorption process have revealed promising preclin. and clin. findings with respects to modulating calorie intake and thus, weight gain. Insights derived from this review suggest materials that adsorb fat/fat digestion products, rather than interfering with enzyme action, are the most promising therapies, due to their ability to overcome the adverse effects associated with orlistat (the only FDA approved anti-obesity therapy with a localized mechanism of action within the gastrointestinal tract).

Trends in Food Science & Technology published new progress about Homo sapiens. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Application of C29H53NO5.

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

Johnson, Adiv A. published the artcile< Lipid Hydrolase Enzymes: Pragmatic Prolongevity Targets for Improved Human Healthspan?>, Product Details of C29H53NO5, the main research area is lipase lipid hydrolase lifespan aging; aging; healthspan; lifespan; lipase; lipid hydrolase; rejuvenation.

Compelling evidence suggests that lipid metabolism, which plays critical roles in fat storage, cell membrane maintenance, and cell signaling, is intricately linked to aging. Lipid hydrolases are important enzymes that catalyze the hydrolysis of more complex lipids into simpler lipids. Diverse interventions targeting lipid hydrolases can prolong or shorten life in model organisms. For example, the genetic removal of or RNAi knockdown against a phospholipase can reduce lifespan in Caenorhabditis elegans, Drosophila melanogaster, and Mus musculus. The removal of lysosomal acid lipase results in premature death in mice, while its overexpression in nematodes generates lean, long-lived individuals. The overexpression or inhibition of diacylglycerol lipase leads to enhanced or reduced longevity, resp., in both worms and flies. Lifespan can also be extended by knocking down triacylglycerol lipases in yeast, overexpressing fatty acid amide hydrolase in worms, or removing hepatic lipase in a mouse model of coronary disease. Conversely, flies lacking the triacylglycerol lipase Brummer are obese and short lived. Linking sphingolipids and aging, removing the sphingomyelinase inositol phosphosphingolipid phospholipase shortens chronol. lifespan in Saccharomyces cerevisiae, while inhibiting an acid sphingomyelinase in worms or inactivating alk. ceramidase in flies extends lifespan. The clin. potential of manipulating these enzymes is highlighted by the FDA-approved obesity drug orlistat, which is an inhibitor of pancreatic and hepatic lipases that induces weight loss and improves insulin/glucose homeostasis. Addnl. research is warranted to better understand how these lipid hydrolases impact aging and to determine if clin. interventions targeting them are capable of improving human healthspan.

Rejuvenation Research published new progress about Caenorhabditis elegans. 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

Nascimento, Jessica; Mariot, Camila; Vianna, Debora R. B.; Kliemann, Lucia M.; Chaves, Paula S.; Loda, Massimo; Buffon, Andreia; Beck, Ruy C. R.; Pilger, Diogo A. published the artcile< Fatty acid synthase as a potential new therapeutic target for cervical cancer>, Electric Literature of 96829-58-2, the main research area is .

Fatty acid synthase (FASN) is the rate-limiting enzyme for the de novo synthesis of fatty acids in the cytoplasm of tumor cells. Many tumor cells express high levels of FASN, and its expression is associated with a poorer prognosis. Cervical cancer is a major public health problem, representing the fourth most common cancer affecting women worldwide. To date, only a few in silico studies have correlated FASN expression with cervical cancer. This study aimed to investigate in vitro FASN expression in premalignant lesions and cervical cancer samples and the effects of a FASN inhibitor on cervical cancer cells. FASN expression was observed in all cervical cancer samples with increased expression at more advanced cervical cancer stages. The FASN inhibitor (orlistat) reduced the in vitro cell viability of cervical cancer cells (C-33A, ME-180, HeLa and SiHa) in a time-dependent manner and triggered apoptosis. FASN inhibitor also led to cell cycle arrest and autophagy. FASN may be a potential therapeutic target for cervical cancer, and medicinal chemists, pharmaceutical researchers and formulators should consider this fi nding in the development of new treatment approaches for this cancer type.

Anais da Academia Brasileira de Ciencias published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Electric Literature of 96829-58-2.

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

Zhang, Qing; Zhou, Yue; Feng, Xingyu; Gao, Yuan; Huang, Chengzhi; Yao, Xueqing published the artcile< Low-dose orlistat promotes the therapeutic effect of oxaliplatin in colorectal cancer>, COA of Formula: C29H53NO5, the main research area is Apoptosis; Colorectal cancer; Low-dose Orlistat; Oxaliplatin; PDX models.

The failure of and resistance to oxaliplatin (OXA)-based chemotherapies may lead to poor prognosis in colorectal cancer (CRC) patients. It has been reported that orlistat (Orli) exhibits potent antitumor effects in several malignant tumors. Here, we identified that OXA in combination with low-dose Orli could sensitize CRC cells to OXA and induce marked synergistic apoptosis in vitro and in vivo. The potential synergistic effects were confirmed and quantified by in silico anal. Furthermore, we validated the synergistic anti-tumor effects in CRC PDX mice model. A qPCR array was performed to evaluate the changes in 85 apoptosis-related genes to elucidate the possible mol. mechanisms in combination-induced cytotoxicity. To conclude, the antitumor synergistic effects of OXA and Orli make them effective and promising candidates for cancer treatment.

Biomedicine & Pharmacotherapy published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, COA of Formula: C29H53NO5.

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

Kwon, Yu-Jin; Kwon, Go Eun; Lee, Hye Sun; Choi, Man Ho; Lee, Ji-Won published the artcile< The Effect of Orlistat on Sterol Metabolism in Obese Patients.>, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is anti-obesity drug; cardiovascular disease; obesity; orlistat; sterol.

Background: Orlistat, a reversible inhibitor of pancreatic and gastric lipase, is known to have anti-obesity and antioxidant properties. Cholesterol intermediates and metabolites have diverse and important functions in cardiovascular disease. Therefore, we aimed to evaluate the effect of orlistat on sterol metabolism in overweight and obese adults after weight loss during the intervention or weight loss at 12 weeks. Methods: A total of 51 (27 in the control group and 24 in the experimental group), patients with a BMI of 27 or greater were randomly assigned in a 1:1 ratio to receive either orlistat (120 mg) three times a day plus phentermine hydrochloride (37.5 mg) once daily or a placebo three times a day plus phentermine hydrochloride (37.5 mg) once daily. The primary study outcome was sterol metabolism. Results: The experimental group exhibited significantly decreased metabolic signatures of serum sterols, free cholesterol, sitosterol, 7α-hydroxycholesterol (7α-OHC), and 7β-OHC at 12 weeks. The experimental group also exhibited significantly decreased metabolic ratios of sitosterol and 7α-OHC to cholesterol at 12 weeks. Regarding changes in sterol signatures from baseline to 6-month follow-up, free cholesterol, plant sterols, and cholesterol precursors tended to decrease with weight loss during the intervention and increase again as the weight was regained in both groups. Conclusion: Orlistat treatment improves oxysterol metabolism in overweight and obese adults. Our findings support that orlistat plays a crucial role in the process of endothelial dysfunction and atherosclerosis via oxysterol modulation.

Frontiers in endocrinology published new progress about 96829-58-2. 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

Zhang, Cong; Sheng, Lei; Yuan, Ming; Hu, Junjie; Meng, Yan; Wu, Yong; Chen, Liang; Yu, Huifan; Li, Shan; Zheng, Guohua; Qiu, Zhenpeng published the artcile< Orlistat delays hepatocarcinogenesis in mice with hepatic co-activation of AKT and c-Met>, Reference of 96829-58-2, the main research area is orlistat AKT cMet hepatic carcinoma antitumor agent; Fatty acid synthase; Hepatocarcinogenesis; Lipogenesis; Orlistat; Proliferation.

Orlistat (Xenical), a US Food and Drug Administration (FDA)-approved anti-obesity drug, shows efficacy against multiple tumor types, including hepatocellular carcinoma (HCC), due to its ability to inhibit fatty acid synthase (FASN) activity. However, whether orlistat affects hepatocellular malignant transformation during hepatocarcinogenesis in vivo is unknown. This study assessed the antisteatotic and antitumorigenic efficacy of orlistat in a rapid HCC FVB/N mouse model established via hydrodynamic transfection of activated forms of AKT and c-Met proto-oncogenes. Human hepatoma cell lines were used for mech. validation in vitro. Hematoxylin and eosin staining, immunohistochem., and immunoblotting were applied for the mechanistic investigation. The results revealed that when orlistat was administered in the early stage of AKT/c-Met-triggered hepatocarcinogenesis, it resulted in the elimination of hepatic tumor burden. Mechanistically, orlistat efficiently elevated PTEN expression and suppressed AKT/SREBP1/FASN signaling both in vivo and in vitro, impairing AKT/c-Met-driven de novo lipogenesis and aberrant proliferation. Altogether, this study demonstrates the antilipogenic and antiproliferative efficacy of orlistat in hepatocarcinogenesis, suggesting that orlistat may be beneficial for the treatment of HCC, especially in NAFLD-related HCCs featuring activated AKT/mTOR cascade and increased lipogenesis in livers.

Toxicology and Applied Pharmacology published new progress about Antitumor agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Reference of 96829-58-2.

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

Yin, Yaguang; Kong, Xiuqi; Li, Min; Wang, Jingchao; Dai, Xiaoyu; Zhang, Yunyan; Lin, Weiying published the artcile< Development of an esterase fluorescent probe based on naphthalimide-benzothiazole conjugation and its applications for qualitative detection of esterase in orlistat-treated biosamples>, Application of C29H53NO5, the main research area is ESIPT; Esterase fluorescent probe; Fast response; Orlistat-treated cell imaging; Zebrafish imaging.

Esterase is a large hydrolysis family, and widely distributed in many kinds of cells. It is responsible for multiple physiol. and pathol. functions including metabolism, gene expression. While abnormality of esterase is associated with many pathol. activities in obesity, Wolman′s disease, and cancer. Thereby, it is essential to design an effective tool for esterase in situ detection in biol. systems. Herein, a novel fluorescent probe Y-1 for monitoring esterase in living cells was rationally designed. Probe Y-1 was synthesized by the conjugation between an acetylation of 4-hydroxy naphthalimide and benzothiazole group. Benzothiazole moiety is a typical Excited-state intramol. proton transfer (ESIPT) controller. Acetate group was selected as the responsive site and ESIPT initiator. As the acetate group could block the ESIPT effect, the probe emits no fluorescence under the excitation of 455 nm. When binding with esterase, Y-1 shows distinct fluorescence with the peak at 560 nm with short time when ESIPT is on. Y-1 displays high sensitivity (LOD is 0.216 x 10-3 U/mL), fast response (within 5 min), high selectivity and photostability towards esterase. Furthermore, the %RSD (relative standard deviation) of within-day and day-to-day precision was no more than 13.0% and the accuracy ranged from -6.5 to -12.3%. Kinetics performance of Y-1 indicates that esterase has high affinity and hydrolysis to Y-1. For biol. applications, our probe is a time-dependent visualizing esterase in living HepG2 and CoLo205 cells within 15 min. After the treatment of orlistat (1 and 5 μM) for inhibiting the activity of esterase, the bright fluorescence has also been detected using our probe. Furthermore, it has been successful in monitoring the esterase in zebrafish, the data were consistent with cellular phenomena. Therefore, all these findings indicate that the robust probe Y-1 is a useful qual. tool for detecting esterase in biol. systems.

Analytica Chimica Acta published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Application of C29H53NO5.

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