Category: 96829-58-2

Cope, Rebecca J.; Fischetti, Briann S.; Kavanagh, Rebecca K.; Lepa, Trisha M.; Sorbera, Maria A. published the artcile< Safety and Efficacy of Weight-Loss Pharmacotherapy in Persons Living with HIV: A Review of the Literature and Potential Drug-Drug Interactions with Antiretroviral Therapy>, Application In Synthesis of 96829-58-2, the main research area is review immunodeficiency virus pharmacotherapy weight loss; HIV; antiretroviral; drug-drug interaction; obesity; weight loss.

A review. The prevalence of obesity among persons living with human immunodeficiency virus (HIV) has increased significantly and may be linked to the use of antiretroviral therapy. Although weight-loss medications approved by the U.S. Food and Drug Administration are recommended as an adjunct to diet and exercise to treat obesity in the general population, little is known about the safety and efficacy of these drugs specifically in persons living with HIV. We review the available evidence regarding the effective use of weight-loss pharmacotherapy in persons living with HIV and its potential to interact with antiretroviral therapy. Persons living with HIV are frequently not reported or included in clin. trials for weight-loss medications; however, treatment efficacy is likely similar to the general population. Several important reported or theor. drug-drug interactions exist between antiobesity pharmacotherapy and antiretroviral therapy. Orlistat is a weight-loss drug available in the United States without a prescription and was linked to HIV viral rebound in several case reports. Clinicians should be aware of the potential for loss of HIV viremia control when certain weight-loss pharmacotherapies are used in combination with antiretrovirals.

Pharmacotherapy published new progress about Antiobesity agents. 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

Shueng, Pei-Wei; Chan, Hui-Wen; Lin, Wei-Chan; Kuo, Deng-Yu; Chuang, Hui-Yen published the artcile< Orlistat Resensitizes Sorafenib-Resistance in Hepatocellular Carcinoma Cells through Modulating Metabolism>, Application In Synthesis of 96829-58-2, the main research area is fatty acid synthase; hepatocellular carcinoma; metabolism; sorafenib resistance.

Sorafenib is one of the options for advanced hepatocellular carcinoma treatment and has been shown to extend median overall survival. However, sorafenib resistance often develops a few months after treatment. Hence, developing various strategies to overcome sorafenib resistance and understand the possible mechanisms is urgently needed. We first established sorafenib-resistant hepatocellular carcinoma (HCC) cells. Then, we found that sorafenib-resistant Huh7 cells (Huh7/SR) exhibit higher glucose uptakes and express elevated fatty acid synthesis and glucose metabolism-related proteins than their parental counterparts (Huh7). The current study investigated whether sorafenib resistance could be reversed by suppressing fatty acid synthesis, using a fatty acid synthase (FASN) inhibitor, orlistat, in HCC cells. FASN inhibition-caused changes in protein expressions and cell cycle distribution were analyzed by Western blot and flow cytometry, and changes in glucose uptakes were also evaluated by 18F-FDG uptake. Orlistat remarkably enhanced the cytotoxicity of sorafenib in both Huh7 and Huh7/SR cells, and flow cytometry showed that combination treatment significantly increased the sub-G1 population in both cell lines. Western blot revealed that the combination treatment effectively increased the ratio of Bax/Bcl-2 and decreased expressions of pERK; addnl., the combination treatment also strongly suppressed fatty acid synthesis-related proteins (e.g., FASN and SCD) in both cell lines. Lastly, the 18F-FDG uptake was repressed by the combination treatment in both cell lines. Our results indicated that orlistat-mediated FASN inhibition could overcome sorafenib resistance and enhance cell killing in HCC by changing cell metabolism

International Journal of Molecular Sciences 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

Polyzos, Stergios A; Goulis, Dimitrios G; Giouleme, Olga; Germanidis, Georgios S; Goulas, Antonis published the artcile< Anti-obesity Medications for the Management of Nonalcoholic Fatty Liver Disease.>, 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 Glucagon-like peptide-1 analog; Nonalcoholic fatty liver disease; Nonalcoholic steatohepatitis; Obesity; Orlistat; Sodium-glucose cotransporter-2 inhibitor.

PURPOSE OF REVIEW: Obesity is closely associated with nonalcoholic fatty liver disease (NAFLD), a highly prevalent disease without any approved medication. The aim of this review was to summarize the evidence on the effect of anti-obesity medications on NAFLD, especially focusing on hepatic histology. RECENT FINDINGS: Orlistat and some glucagon-like peptide-1 receptor analogs, including liraglutide and semaglutide, have beneficial effects on hepatic steatosis and inflammation, but not fibrosis. Other anti-obesity medications, including lorcaserin, setmelanotide, phentermine hydrochloric, phentermine/topiramate, and naltrexone/bupropion, have been minimally investigated in NAFLD. Furthermore, medications like sodium-glucose cotransporter-2 inhibitors and farnesoid X receptor have shown beneficial effects in both NAFLD and obesity, but they have not been licensed for either disease. Liraglutide, semaglutide, and orlistat may be currently used in selected patients with obesity and NAFLD. Further research is warranted, since targeting obesity may provide additional benefits on its comorbidities, including NAFLD.

Current obesity reports published new progress about 96829-58-2. 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

Singh, Y; Gupta, G; Anand, K; Kumar Jha, N; Thangavelu, L; Kumar Chellappan, D; Dua, K published the artcile< Molecular exploration of combinational therapy of orlistat with metformin prevents the COVID-19 consequences in obese diabetic patients.>, 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 .

There is no abstract available for this document.

European review for medical and pharmacological sciences published new progress about 96829-58-2. 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

Wang, Lei; Riel, Louis P.; Bajrami, Bekim; Deng, Bin; Howell, Amy R.; Yao, Xudong published the artcile< α-Methylene-β-Lactone Scaffold for Developing Chemical Probes at the Two Ends of the Selectivity Spectrum>, Computed Properties of 96829-58-2, the main research area is chemical proteomics; glutathione S-transferase; methylenelactone; orlistat; parthenolide.

The utilities of an α-methylene-β-lactone (MeLac) moiety as a warhead composed of multiple electrophilic sites are reported. We demonstrate that a MeLac-alkyne not only reacts with diverse proteins as a broadly reactive measurement probe, but also recruits reduced endogenous glutathione (GSH) to assemble a selective chemical probe of GSH-β-lactone (GSH-Lac)-alkyne in live cells. Tandem mass spectrometry reveals that MeLac reacts with nucleophilic cysteine, serine, lysine, threonine, and tyrosine residues, through either Michael or acyl addition. A peptide-centric proteomics platform demonstrates that the proteomic selectivity profiles of orlistat and parthenolide, which have distinct reactivities, are measurable by MeLac-alkyne as a high-coverage probe. The GSH-Lac-alkyne selectively probes the glutathione S-transferase P responsible for multidrug resistance. The assembly of the GSH-Lac probe exemplifies a modular and scalable route to develop selective probes with different recognizing moieties.

ChemBioChem published new progress about 96829-58-2. 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

Joyce, Paul; Dening, Tahnee J.; Meola, Tahlia R.; Gustafsson, Hanna; Kovalainen, Miia; Prestidge, Clive A. published the artcile< Nanostructured clay particles supplement orlistat action in inhibiting lipid digestion: An in vitro evaluation for the treatment of obesity>, 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 obesity orlistat antiobesity agent nanostructured clay particle lipid digestion; Anti-obesity; Fat digestion; Lipid digestion; Lipolysis; Obesity; Orlistat.

In this study, nanostructured clay (NSC) particles, fabricated by spray drying delaminated dispersions technologies that regulate energy uptake, to curb the rising trend in obesity statistics. In this study, nanostructured clay (NSC) particles, fabricated by spray drying delaminated dispersions of com. clay platelets (Veegum HS and LAPONITE XLG), were delivered as complimentary, bioactive excipients with the potent lipase inhibitor, orlistat, for the inhibition of fat (lipid) hydrolysis. Simulated intestinal lipolysis studies were performed by observing changes in free fatty acid concentration and revealed that a combinatorial effect existed when NSC particles were co-administered with orlistat, as evidenced by a 1.2- to 1.6-fold greater inhibitory response over 60 min, compared to dosing orlistat alone. Subsequently, it was determined that a multifaceted approach to lipolysis inhibition was presented, whereby NSC particles adsorbed high degrees of lipid (up to 80% of all lipid species present in lipolysis media) and thus phys. shielded the lipid-in-water interface from lipase access, while orlistat covalently attached and blocked the lipase enzyme active site. Thus, the ability for NSC particles to enhance the biopharmaceutical performance and potency of orlistat is hypothesised to translate into promising in vivo pharmacodynamics, where this novel approach is predicted to lead to considerably greater weight reductions for obese patients, compared to dosing orlistat alone.

European Journal of Pharmaceutical Sciences published new progress about Adsorption. 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

Wijaya, Mely; Subandi published the artcile< In silico analysis of saponin isolates from mesocarp of cucumber (Cucumic sativus L.) and purple eggplant (Solanum melongena L.) as pancreatic lipase inhibitor>, Related Products of 96829-58-2, the main research area is Cucumic Solanum mesocarp anti obesity pancreatic lipase inhibitor.

Currently orlistat has been widely used as anti-obesity drug, because of its activity as a pancreatic lipase inhibitor. Two saponin isolates, from cucumber mesocarp and purple eggplant, also proved to be active as pancreatic lipase inhibitors in vitro. Based on spectrophotometric anal., the two saponin isolates are thought to be Silphioside F and Cesdiurins I-III. The purpose of this study is to confirm the ability of the two compounds as pancreatic lipase inhibitor through in silico anal., relative to orlistat. This study uses Python Mol. Viewer (PyMol), Python Prescription (PyRx) 0.8, and Discovery Studio software. As a ligand, 3D structure of Silphioside F and Cesdiurins I-III have been used. The orlistat as a comparative ligand mol. have also been used. 3D structure of porsine pancreatic lipase has been used as receptor mol. The result of the anal. shown that the binding site of pancreatic lipase is relatively same as orlistat of Cesdiurins I-III mol., but different for the Silphioside F mol. The data indicated that in inhibiting pancreatic lipase, the two isolate compounds used different mechanism. However, against pancreatic lipase, both mols. have greater binding affinities each, compared to orlistat, which were -9.7 kcal/mol for Silhphioside F and -9.5 kcal/mol for Cesdiurins I-III, and orlistat only -7.6 kcal/mol. The latest data were in line with the in vitro anal., that both isolates have greater inhibition power than orlistat.

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, Related Products of 96829-58-2.

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

Hall, Michael E.; Cohen, Jordana B.; Ard, Jamy D.; Egan, Brent M.; Hall, John E.; Lavie, Carl J.; Ma, Jun; Ndumele, Chiadi E.; Schauer, Philip R.; Shimbo, Daichi published the artcile< Weight-Loss Strategies for Prevention and Treatment of Hypertension: A Scientific Statement From the American Heart Association>, Category: amides-buliding-blocks, the main research area is AHA Scientific Statements; blood pressure; metabolic surgery; obesity.

Hypertension is a major risk factor for cardiovascular and renal diseases in the United States and worldwide. Obesity accounts for much of the risk for primary hypertension through several mechanisms, including neurohormonal activation, inflammation, and kidney dysfunction. As the prevalence of obesity continues to increase, hypertension and associated cardiorenal diseases will also increase unless more effective strategies to prevent and treat obesity are developed. Lifestyle modification, including diet, reduced sedentariness, and increased phys. activity, is usually recommended for patients with obesity; however, the long-term success of these strategies for reducing adiposity, maintaining weight loss, and reducing blood pressure has been limited. Effective pharmacotherapeutic and procedural strategies, including metabolic surgeries, are addnl. options to treat obesity and prevent or attenuate obesity hypertension, target organ damage, and subsequent disease. Medications can be useful for short- and long-term obesity treatment; however, prescription of these drugs is limited. Metabolic surgery is effective for producing sustained weight loss and for treating hypertension and metabolic disorders in many patients with severe obesity. Unanswered questions remain related to the mechanisms of obesity-related diseases, long-term efficacy of different treatment and prevention strategies, and timing of these interventions to prevent obesity and hypertension-mediated target organ damage. Further investigation, including randomized controlled trials, is essential to addressing these questions, and emphasis should be placed on the prevention of obesity to reduce the burden of hypertensive cardiovascular and kidney diseases and subsequent mortality.

Hypertension published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Category: amides-buliding-blocks.

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

Jorgensen, Megan M.; Burrell, Brian D. published the artcile< Approaches to studying injury-induced sensitization and the potential role of an endocannabinoid transmitter>, HPLC of Formula: 96829-58-2, the main research area is endocannabinoid transmitter nociception agent nociceptive; Endocannabinoid; Hirudo; Leech; Nociception; Sensitization.

Abstract: Endocannabinoids are traditionally thought to have an analgesic effect. However, it has been shown that while endocannabinoids can depress nociceptive signaling, they can also enhance non-nociceptive signaling. Therefore, endocannabinoids have the potential to contribute to non-nociceptive sensitization after an injury. Using Hirudo verbana (the medicinal leech), a model of injury-induced sensitization was developed in which a reproducible piercing injury was delivered to the posterior sucker of Hirudo. Injury-induced changes in the non-nociceptive threshold of Hirudo were determined through testing with Von Frey filaments and changes in the response to nociceptive stimuli were tested by measuring the latency to withdraw to a nociceptive thermal stimulus (Hargreaves apparatus). To test the potential role of endocannabinoids in mediating injury-induced sensitization, animals were injected with tetrahydrolipstatin (THL), which inhibits synthesis of the endocannabinoid transmitter 2-arachidonoylglycerol (2-AG). Following injury, a significant decrease in the non-nociceptive response threshold (consistent with non-nociceptive sensitization) and a significant decrease in the response latency to nociceptive stimulation (consistent with nociceptive sensitization) were observed In animals injected with THL, a decrease in non-nociceptive sensitization in injured animals was observed, but no effect on nociceptive sensitization was observed

Journal of Comparative Physiology, A: Neuroethology, Sensory, Neural, and Behavioral Physiology published new progress about Analgesia. 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

Park, Yea-Jin; Seo, Dong-Wook; Ju, Jae-Yun; Cha, Yun-Yeop; An, Hyo-Jin published the artcile< The antiobesity effects of Buginawa in 3T3-L1 preadipocytes and in a mouse model of high-fat diet-induced obesity>, Electric Literature of 96829-58-2, the main research area is high fat diet obesity antiobesity bugi preadipocytes.

There has been a remarkable interest in finding lipid inhibitors from natural products to replace synthetic compounds, and a variety of oriental medicinal herbs are reported to have biol. activity with regard to lipid inhibition. Buginawa (Bugi) is a novel combined formula that contains twelve medicinal herbs with potential for weight loss induction. We hypothesized that Bugi may have antiobesity effects in 3T3-L1 preadipocytes and in a high-fat diet- (HFD-) induced mouse model. In this study, 3T3-L1 cells were treated with varied concentrations of Bugi (62.5, 125, or 250μg/mL). Bugi treatment inhibited adipocyte differentiation by suppressing adipogenic transcription genes, including peroxisome proliferator-activated receptor γ protein (PPARγ), CCAAT/enhancer-binding protein α (C/EBPα), sterol regulatory element-binding protein 1 (SREBP1), and CCAAT/enhancer-binding protein β (C/EBPβ).Mice were fed a normal diet or an HFD for 11 wk, and Bugi was simultaneously administered at 50 or 100mg/kg. Bugi administration significantly reduced body weight gain and white adipose tissue (WAT) weight and effectively inhibited lipid droplet accumulation in epididymal white adipose tissue (eWAT) and liver tissue. Further, Bugi treatment suppressed mRNA levels of PPARγ, C/EBPα, and SREBP1 in eWAT and liver tissue. Our findings demonstrate that Bugi could be an effective candidate for preventing obesity and relatedmetabolic disorders.

BioMed Research International published new progress about Adipocyte. 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