Category: 96829-58-2

Shirai, Kohji; Fujita, Toru; Tanaka, Michitaka; Fujii, Yuka; Shimomasuda, Masatsugu; Sakai, Soichi; Samukawa, Yoshishige published the artcile< Efficacy and Safety of Lipase Inhibitor Orlistat in Japanese with Excessive Visceral Fat Accumulation: 24-Week, Double-Blind, Randomized, Placebo-Controlled Study>, 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 orlistat lipase inhibitor efficacy safety visceral fat accumulation; Body weight; Double-blind; Efficacy; Japanese; Lipase inhibitor; Obesity; Orlistat; Placebo-controlled; Randomized; Safety; Visceral fat; Waist circumference.

Orlistat is an inhibitor of pancreatic lipase and is used as an anti-obesity drug in many countries. Therefore, this comparative, placebo-controlled, double-blind, randomized study aimed to evaluate the efficacy and safety of orlistat in Japanese participants with excessive visceral fat accumulation and without dyslipidemia, diabetes mellitus, and hypertension (“”metabolic diseases””). The study population included Japanese participants with excessive visceral fat accumulation (waist circumference ≥ 85 cm in males and ≥ 90 cm in females, which corresponds to a visceral fat area of 100 cm2) and without metabolic diseases. Both drugs were administered orally three times daily for 24 wk. Visceral fat area, s.c. fat area, waist circumference, body weight, body mass index, adverse reactions, laboratory tests, and blood pressure were regularly assessed. Visceral fat area, waist circumference, and body weight were significantly reduced in the orlistat group (mean ± standard error, – 13.50 ± 1.52%, – 2.51 ± 0.25%, and – 2.79 ± 0.30%, resp.) compared to the placebo group (- 5.45 ± 1.50%, – 1.55 ± 0.26%, and – 1.22 ± 0.28%, resp.) at the last assessment. Most adverse reactions were mild, and none were serious or severe. Orlistat administration reduced visceral fat area, waist circumference, and body weight in Japanese participants with excessive visceral fat and without metabolic diseases.

Advances in Therapy published new progress about Blood. 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

Chao, Ariana M.; Wadden, Thomas A.; Berkowitz, Robert I.; Quigley, Kerry; Silvestry, Frank published the artcile< The risk of cardiovascular complications with current obesity drugs>, SDS of cas: 96829-58-2, the main research area is cardiovascular complication obesity drug pharmacotherapy; Cardiovascular; cardiovascular disease outcomes; obesity; pharmacotherapy; weight loss.

IntroductionObesity is associated with an increased risk of cardiovascular morbidity and mortality. Four medications are approved by the US Food and Drug Administration (FDA) for chronic weight management when used as an adjunct to a reduced-calorie diet and increased phys. activity in adults. These medications result in clin. significant weight losses, as well as improvements in some cardiometabolic risk factors. Areas coveredWe briefly review the history of anti-obesity medications (AOMs) as related to cardiovascular safety, and summarize weight loss efficacy and cardiovascular data from clin. trials of orlistat, phentermine/topiramate, naltrexone/bupropion, and liraglutide. Expert opinionCurrent AOMs approved for chronic weight management have generally favorable effects on some cardiometabolic parameters. However, the long-term safety of orlistat, phentermine/topiramate, and naltrexone/bupropion on cardiovascular morbidity and mortality have not been established. The cardiovascular safety of liraglutide, at a dose of 1.8 mg/d, was demonstrated in a large randomized outcomes trial in participants with type 2 diabetes.

Expert Opinion on Drug Safety published new progress about Antiobesity agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, SDS of cas: 96829-58-2.

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

Tyan, Yeu-Sheng; Lee, Yen-Po; Chuang, Hui-Yen; Wang, Wei-Hsun; Hwang, Jeng-Jong published the artcile< Effects of orlistat combined with enzalutamide and castration through inhibition of fatty acid synthase in a PC3 tumor-bearing mouse model>, Formula: C29H53NO5, the main research area is prostate cancer orlistat enzalutamide fatty acid synthase cell cycle; NF-kB; castration therapy; enzalutamide; fatty acid synthase; orlistat; prostate cancer.

Androgen deprivation therapy (ADT) is one of the typical treatments used for patients with prostate cancer (PCa). ADT, however, may fail when PCa develops castration-resistance. Fatty acid synthase (FASN), a critical enzyme involved in fatty acid synthesis, is found to be up-regulated in PCa. Since enzalutamide and ADT are frequently used for the treatment of PCa, the present study aimed to unravel the underlying mechanism of combination of orlistat, an FASN inhibitor, and enzalutamide using PC3 cell line; and orlistat and castration in PC3 tumor-bearing animal model. Cytotoxicity was determined by AlamarBlue assay. Drug effects on the cell cycle and protein expressions were assayed by the flow cytometry and Western blot. Electromobility shift assay was used to evaluate the NF-κB activity. The tumor growth delay, expressions of the signaling-related proteins, and histopathol. post treatments of orlistat and castration were evaluated in PC3 tumor-bearing mouse model. The results showed that orlistat arrested the PC3 cells at the G1 phase of the cell cycle and enhanced the cytotoxic effects of enzalutamide synergistically. Pretreatment with orlistat combined with castration inhibited the tumor growth significantly compared with those of castration and orlistat treatments alone in PC3 tumor-bearing mice. Combination treatment reduced both FASN and NF-κB activities and their downstream effector proteins. The present study demonstrated the synergistic effects of orlistat combined with enzalutamide in vitro and castration in vivo on human PCa.

Bioscience Reports published new progress about Androgen deprivation therapy. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Formula: C29H53NO5.

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

Yu, Zhou; Fan, Wufa; Wang, Luting; He, Haisheng; Lv, Yongjiu; Qi, Jianping; Lu, Yi; Wu, Wei published the artcile< Slowing down lipolysis significantly enhances the oral absorption of intact solid lipid nanoparticles>, SDS of cas: 96829-58-2, the main research area is solid lipid nanoparticle lipolysis oral absorption.

Only a limited amount of orally administered lipid nanoparticles are absorbed as intact particles due to lipolysis by lipases in the gastrointestinal tract. It is hypothesized that by counteracting lipolysis, more particles will survive gastrointestinal digestion and be absorbed as intact particles. In this study, incorporation of a lipase inhibitor orlistat (OLST), as well as polyethylene glycol (PEG) coating, is employed to slow down the lipolysis using solid lipid nanoparticles (SLNs) as model particles. To explore the in vivo behaviors of the particles, near-IR fluorescent probes with absolute aggregation-caused quenching (ACQ) properties are used to label and track the unmodified, PEG-coated and OLST-loaded SLNs. The in vitro lipolysis study indicates very fast first-order degradation of unmodified SLNs and significantly decreased degradation of OLST-SLNs. Live imaging reveals the same trend of slowed-down lipolysis in vivo which correlates well with the in vitro lipolysis. The scanning of ex vivo gastrointestinal segments confirms the considerably prolonged residence time of OLST-SLNs, mirroring the significantly decreased lipolysis rate. The observation of fluorescence in the blood, though very weak, and in the liver speaks of the oral absorption of intact SLNs. Similarly, slowing down lipolysis also contributes to the significantly enhanced cumulative lymphatic transport of OLST-SLNs (7.56% vs. 1.27% for the unmodified SLNs).

Biomaterials Science published new progress about Biomacromolecular compounds Role: TEM (Technical or Engineered Material Use), USES (Uses). 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, SDS of cas: 96829-58-2.

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

Huang, Eunchong; Kim, Seulki; Park, Haryung; Park, Soyoung; Ji, Yosep; Todorov, Svetoslav Dimitrov; Lim, Sang-Dong; Holzapfel, Wilhelm Heinrich published the artcile< Modulation of the Gut Microbiome and Obesity Biomarkers by Lactobacillus Plantarum KC28 in a Diet-Induced Obesity Murine Model>, Formula: C29H53NO5, the main research area is Adipose tissue; Anti-obesity effect; Gut microbiome; Lactobacillus plantarum; Murine model.

Abstract: Lactobacillus plantarum KC28 showed a beneficial (anti-obesity) effect in a diet-induced obese (DIO) C57BL/6 murine model receiving an intermediate high-fat diet (IF). This diet was selected for probiotic studies by prior comparisons of different combinations of basic (carbohydrate, protein and fat) components for optimized induction of dietary obesity in a murine model. Prior selection of Lact. plantarum strain KC28 was based on different physiol. tests for safety and functionality including cell line adhesion and anti-adipogenic activity. The strain was administered at 5.0 x 109 CFU/mouse/day to the DIO mice (control mice received a normal diet). The anti-obesity effect of KC28 and the well-known probiotic strains Lact. rhamnosus GG (LGG) and Lact. plantarum 299v was assessed over 12 wk. Xenical served as anti-obesity control. The high-fat diet groups receiving strains KC28 and LGG and the control Xenical group showed significant weight loss and notable changes in some obesity-related biomarkers in the liver (significant up-regulation of PGC1-α and CPT1-α only by KC28; p < 0.05) and mesenteric adipose tissue (significant down-regulation of ACOX-1, PPAR-γ, and FAS; KC28 p < 0.001 for PPAR-γ and FAS), compared with the IF control. Favorable changes in the studied biomarkers suggest a similar beneficial influence of Lact. plantarum KC28 on the alleviation of obesity comparable with that of the two well-studied probiotic strains, LGG and 299v. This probably resulted from a modulation in the cecal microbiota of the IF group by either probiotic strain, yet in a different manner, showing a highly significant increase in the families Desulfovibrionaceae and Lactobacillaceae only in the group receiving Lact. plantarum KC28. Probiotics and Antimicrobial Proteins published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Formula: C29H53NO5.

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

Aiswarya, Ms; Venkateswaramurthy, N.; Sambathkumar, R. published the artcile< Long term effect of obesity treatment: a review>, Computed Properties of 96829-58-2, the main research area is review orlistat lorcaserine phentermine sibutramine rimonabant antiobesity agent obesity.

A review. Obesity is a significant issue that can lead to multiple serious diseases such as osteoarthritis, obstructive sleep apnea, gallstones, fatty liver disease, reproductive and gastrointestinal cancers, dyslipidemia, hypertension, type II diabetes, cardiac failure, CAD and stroke. When these non-pharmacol. procedures are ineffective, lifestyle modification such as diet and exercise is essential for the prevention and management of obesity, pharmacotherapy may be regarded. The lifestyle and phys. needs of individualized patients should be altered as the original therapy for obesity that concentrated mainly on diet and exercise. Many drugs used in obesity, including orlistat, lorcaserine, phentermine, sibutramine and rimonabant, but long-term use of above drug may cause several life-threatening side effects. Discontinuation of these anti-obesity drugs leads to weight regaining, in which the treatment will be ineffective. Due to enhanced danger of psychiatric disorders and non-fatal myocardial infarction or stroke, permits for rimonabant and sibutramine were withdrawn. Although orlistat is not as efficient in decreasing body weight as other drugs, orlistat is currently the only option available for treating obesity due to its safety for cardiovascular events and beneficial impacts on diabetic control. The aim of this study is to review the long-term effects of obesity treatment.

Research Journal of Pharmaceutical, Biological and Chemical Sciences published new progress about Antiobesity 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

Lumsden, Rebecca H; Pagidipati, Neha J; Phelan, Matthew P; Chiswell, Karen; Peterson, Eric D published the artcile< Prevalence and Management of Adult Obesity in a Large U.S. Academic Health System.>, Computed Properties of 96829-58-2, the main research area is .

INTRODUCTION: Both medication and surgical interventions can be used to treat obesity, yet their use and effectiveness in routine clinical practice are not clear. This study sought to characterize the prevalence and management of patients with obesity within a large U.S. academic medical center. METHODS: All patients aged ≥18 years who were seen in a primary care clinic within the Duke Health System between 2013 and 2016 were included. Patients were categorized according to baseline BMI as underweight or normal weight (<25 kg/m2), overweight (25-29.9 kg/m2), Class I obesity (30-34.9 kg/m2), Class II obesity (35-39.9 kg/m2), and Class III obesity (≥40 kg/m2). Baseline characteristics and use of weight loss medication were assessed by BMI category. Predicted change in BMI was modeled over 3 years. All data were analyzed between 2017 and 2018. RESULTS: Of the 173,462 included patients, most were overweight (32%) or obese (40%). Overall, <1% (n=295) of obese patients were prescribed medication for weight loss or underwent bariatric surgery within the 3-year study period. Most patients had no change in BMI class (70%) at 3 years. CONCLUSIONS: Despite a high prevalence of obesity within primary care clinics of a large, U.S. academic health center, the use of pharmacologic and surgical therapies was low, and most patients had no weight change over 3 years. This highlights the significant need for improvement in obesity care at a health system level. American journal of preventive medicine 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

Gruden, Stefan; Forslund, Anders; Alderborn, Goran; Soderhall, Arvid; Hellstrom, Per M.; Holmback, Ulf published the artcile< Safety of a Novel Weight Loss Combination Product Containing Orlistat and Acarbose>, COA of Formula: C29H53NO5, the main research area is obesity orlistat acarbose combination weight loss; fixed-dose combination; gastrointestinal tolerability; modified release; obesity treatment; weight loss product.

The safety of a novel modified-release oral capsule with orlistat and acarbose (MR-OA) was investigated in 67 obese middle-aged White men with a body mass index of 32 to 40 kg/m2 or 30 to 32 kg/m2 plus waist circumference >102 cm. The purpose of this investigation was to compare MR-OA with the existing conventional orlistat regarding systemic safety defined as plasma orlistat concentration at the end of the treatment period of 14 days. Participants took the MR-OA fixed-dose combination formulation 3 times a day together with a major meal. Three different doses of MR-OA were evaluated-60/20, 90/30, and 120/40 (mg orlistat/mg acarbose)-as well as 1 reference group who received the conventional orlistat, Xenical, with 120 mg of orlistat. Blood plasma was sampled on days 1 and 14. The orlistat plasma concentrations of the MR-OA dose showed a delayed absorption and were lower compared with conventional orlistat at the end of the study. All doses were safe and well tolerated without any unexpected adverse events and no serious adverse events. The delay in the rise of orlistat plasma concentration indicates that the modified-release properties of the MR-OA formulation are effective. The systemic exposure of orlistat resulting from MR-OA was similar, albeit a bit lower than the conventional orlistat with 120 mg of orlistat. We can therefore assume that the safety profile regarding the orlistat moiety of MR-OA is comparable to the conventional orlistat and a promising approach for weight control in obese patients. Further clin. evaluation is underway.

Clinical Pharmacology in Drug Development published new progress about Body mass index. 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

Manu, Peter; Lăcătuşu, Cristina-Mihaela; Rogozea, Liliana M; Cernea, Simona published the artcile< Pharmacological Management of Obesity: A Century of Expert Opinions in Cecil Textbook of Medicine.>, Synthetic Route of 96829-58-2, the main research area is .

BACKGROUND: Innovations in drug therapy for obesity have had a limited impact on the body mass index, prevalence of medical complications, quality of life, and work potential of a substantial majority of affected persons. STUDY QUESTION: What are the milestones of the changes in the expert approach to the pharmacological management of obesity in the past century? STUDY DESIGN: To determine the changes in the experts’ approach to the management of obesity, as presented in a widely used textbook in the United States. DATA SOURCES: The primary sources were chapters describing the management of obesity in the 26 editions of Cecil Textbook of Medicine published from 1927 through 2020. Secondary sources were publications retrieved from Medline that clarified technical issues related to the development, regulatory approval, and use of the drugs mentioned in the Cecil Textbook of Medicine. RESULTS: Pharmacological interventions aimed at increasing caloric expenditures through thermogenesis were recommended from 1927 through 1943. Thyroid extracts were prescribed even in the absence of demonstrated hypothyroidism or decreased basal metabolic rate throughout this period. Dinitrophenol was mentioned in 1937, but was banned soon thereafter. Appetite suppression with amphetamine was considered useful from 1943 through 1988, after which the drug was replaced with other centrally acting molecules, such as fenfluramine in 1988, sibutramine in 2000, and rimonabant in 2008, which were in turn withdrawn because of major adverse effects. In the past decade, obesity has been treated with the appetite suppressants phentermine-topiramate, bupropion-naltrexone, lorcaserin, and liraglutide, and with orlistat, a drug promoting fat malabsorption. The change in weight produced by these drugs is generally modest and transient. CONCLUSIONS: The pharmacological management of obesity has remained frustratingly inefficient. The reasons for the relative lack of success may reside in the ever-growing access to dense, palatable, and relatively inexpensive food, coupled with the decrease in energy expenditure created by a sedentary lifestyle.

American journal of therapeutics published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Synthetic Route of 96829-58-2.

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

Permatasari, Happy Kurnia; Firani, Novi Khila; Prijadi, Bambang; Irnandi, Dicky Faizal; Riawan, Wibi; Yusuf, Muhammad; Amar, Nasim; Chandra, Liani Amelia; Yusuf, Vincentius Mario; Subali, Anita Dominique; Nurkolis, Fahrul published the artcile< Kombucha drink enriched with sea grapes (Caulerpa racemosa) as potential functional beverage to contrast obesity: An in vivo and in vitro approach.>, Application In Synthesis of 96829-58-2, the main research area is Caulerpa racemosa; Dyslipidemia; Kombucha; Nutraceuticals; Obesity.

BACKGROUND AND AIMS: Obesity is currently a global issue and is a major cause of the metabolic disorder, including dyslipidemia. However, currently approved treatments have various limitations including serious side effects, numerous contraindications, and lack of acceptance. Caulerpa racemosa, also referred as Sea grapes, is a seaweed known for its various benefits. C. racemosa extract has the potential to improve lipid profile and role as an anti-obese agent. In order to maximize its health benefits, C. racemosa was made using kombucha drink as a carrier medium. This study aims to assess the effect of Sea grapes kombucha drink on lipase activity in vitro and lipid profile in vivo. METHODS: A lipase inhibition test was carried out by incubating Sea grapes kombucha drink compared with orlistat as the control in porcine pancreatic lipase and p-nitrophenyl butyrate in reaction buffer. A total of four groups were made, each containing 10 male swiss webster albino mice; group A received standard dry pellet diet as control, group B received cholesterol and fat-enriched diets (CFED), group C and D received CFED and 150 and 300 mg/kgBW of kombucha drink from Sea grapes respectively for 4 weeks. RESULTS: Sea grapes kombucha drink improved lipid profiles in the way of reducing total cholesterol, triglyceride, LDL, and increasing HDL levels compared to CFED and normal groups. The effect was more robust following the incrementing dose of the Sea grapes excluding total cholesterol. The lipase inhibitory activity of Sea grapes kombucha drink was similar to orlistat at a dose of 250 μg/mL, otherwise, orlistat was superior in the lower doses. CONCLUSIONS: Sea grapes kombucha drink treatment also induced weight loss and increased level of liver SOD. Kombucha drink from C. racemosa has good potential as a functional beverage with anti-obese and lipid improving activity.

Clinical nutrition ESPEN 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