Category: 96829-58-2

Hitakarun, Atitaya; Khongwichit, Sarawut; Wikan, Nitwara; Roytrakul, Sittiruk; Yoksan, Sutee; Rajakam, Supoth; Davidson, Andrew D.; Smith, Duncan R. published the artcile< Evaluation of the antiviral activity of orlistat (tetrahydrolipstatin) against dengue virus, Japanese encephalitis virus, Zika virus and chikungunya virus>, Reference of 96829-58-2, the main research area is dengue encephalitis Zika chikungunya virus orlistat antiviral.

Many mosquito transmitted viruses of the genera Alphavirus and Flavivirus are human pathogens of significant concern, and there is currently no specific antiviral for any member of these two genera. This study sought to investigate the broad utility of orlistat (tetrahydrolipstatin) in reducing virus infection for several mosquito borne viruses including flaviviruses (dengue virus (DENV; nine isolates analyzed), Japanese encephalitis virus (JEV; one isolate analyzed) and Zika virus (ZIKV; 2 isolates analyzed)) as well as an alphavirus (chikungunya virus; CHIKV; 2 isolates analyzed). Three different treatment regimens were evaluated, namely pre-treatment (only), post-treatment (only) and pre- and post-treatment, and three factors were evaluated, namely level of infection, virus titer and genome copy number Results showed that all three treatment modalities were able to significantly reduce virus titer for all viruses investigated, with the exception of three isolates of DENV in the pre-treatment only regimen. Pre- and post-treatment was more effective in reducing the level of infection and genome copy number of all viruses investigated than either pre-treatment or post-treatment alone. Collectively, these results suggest orlistat has potential as a broad-spectrum agent against multiple mosquito transmitted viruses.

Scientific Reports published new progress about Alphavirus. 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

Wasta Esmail, Vian Ahmed; Al-Nimer, Marwan S M; Mohammed, Mohammed Omer published the artcile< Effects of Orlistat or Telmisartan on the Serum Free Fatty Acids in Non-alcoholic Fatty Liver Disease Patients: An Open-Labeled Randomized Controlled Study.>, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is .

BACKGROUND: One of the important inducers of inflammatory responses and accumulation of fat in hepatocytes is free fatty acids which ultimately lead to the development of non-alcoholic fatty liver disease. Patients with non-alcoholic fatty liver disease have high levels of plasma free fatty acids which are usually associated with type 2 diabetes and components of metabolic syndrome including dyslipidemia. Objective of this research is to investigate the effects of orlistat (a lipase enzyme inhibitor) or telmisartan (an angiotensin receptor blocker) on the serum free fatty acids in non-alcoholic fatty liver disease patients taking into consideration the baseline lipid profile. METHODS: This open-label clinical trial was carried out in the Department of Pharmacology, College of Medicine at the University of Sulaimani in cooperation with Shar Teaching Hospital in Sulaimani city-Kurdistan Region of Iraq. A total number of 74 non-alcoholic fatty liver disease patients were recruited and grouped randomly into group I (n = 25) treated with orlistat (120 mg/day orally) for 12 weeks, group II (n = 24) treated with telmisartan (20 mg/day orally) for 8 weeks, and group III (n = 25) treated with placebo (carboxy- methyl cellulose) once daily. Fasting serum level of free fatty acid and lipid profile including total cholesterol, triglyceride, high-density lipoprotein, and non-high-density lipoproteins were determined. RESULTS: Orlistat and telmisartan significantly reduced the triglyceride-glucose index and free fatty acid levels (P < .001) in patients with non-alcoholic fatty liver diseases. CONCLUSION: Short-term treatment with orlistat or telmisartan produce effective and significant reductions in FFAs in patients with non-alcoholic fatty liver disease compared to placebo. Orlistat effectively reduces the free fatty acid irrespective of the baseline lipid profile. The Turkish journal of gastroenterology : the official journal of Turkish Society of Gastroenterology 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

Khedr, Naglaa F.; Ebeid, Abla M.; Khalil, Rania M. published the artcile< New insights into weight management by orlistat in comparison with cinnamon as a natural lipase inhibitor>, Reference of 96829-58-2, the main research area is obesity orlistat cinnamon weight management; Cinnamon; Dopamine; Dyslipidemia; Glutamate; Obesity; Orlistat.

Background and objectives: Orlistat which is taken by obese patients may present some therapeutic assistance through its inhibition of lipase activity. Otherwise, a natural lipase inhibitor as cinnamon is widely used traditional medicine to decrease cholesterol and body weight The current study aimed to investigate the weight management of orlistat in comparison with cinnamon through different obesity related targets. Methods: Subjects were divided into: Group 1: subjects received cinnamon capsules for 60 days. Results: Both orlistat and cinnamon groups showed a significant reduction in BMI, lipid profile, and lipase activity compared with baseline. Orlistat group showed significant elevation (p < 0.001) in glucagon, insulin-degrading enzyme (IDE) and dopamine level concomitant with the decrease of serum glutamate compared with baseline level of the same group and cinnamon group. However, cinnamon reduced serum insulin level and insulin resistance (IR) compared with baseline level of the same group and orlistat group. Conclusions: Orlistat can be used in weight management not only for its pancreatic lipase inhibition but also, due to its indirect appetite reduction effect through elevated glucagon, IDE and dopamine levels and its inhibitory effect on glutamate neurotransmitter, whereas, cinnamon improves BMI and glycemic targets. Endocrine published new progress about Blood serum. 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

Zhou, Wenjing; Zhang, Jing; Yan, Mingkun; Wu, Jin; Lian, Shuo; Sun, Kang; Li, Baiqing; Ma, Jia; Xia, Jun; Lian, Chaoqun published the artcile< Orlistat induces ferroptosis-like cell death of lung cancer cells.>, 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 FAF2; ferroptosis; lung cancer; orlistat.

Aberrant de novo lipid synthesis is involved in the progression and treatment resistance of many types of cancers, including lung cancer; however, targeting the lipogenetic pathways for cancer therapy remains an unmet clinical need. In this study, we tested the anticancer activity of orlistat, an FDA-approved anti-obesity drug, in human and mouse cancer cells in vitro and in vivo, and we found that orlistat, as a single agent, inhibited the proliferation and viabilities of lung cancer cells and induced ferroptosis-like cell death in vitro. Mechanistically, we found that orlistat reduced the expression of GPX4, a central ferroptosis regulator, and induced lipid peroxidation. In addition, we systemically analyzed the genome-wide gene expression changes affected by orlistat treatment using RNA-seq and identified FAF2, a molecule regulating the lipid droplet homeostasis, as a novel target of orlistat. Moreover, in a mouse xenograft model, orlistat significantly inhibited tumor growth and reduced the tumor volumes compared with vehicle control (P < 0.05). Our study showed a novel mechanism of the anticancer activity of orlistat and provided the rationale for repurposing this drug for the treatment of lung cancer and other types of cancer. Frontiers of 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

Czumaj, Aleksandra; Zabielska, Judyta; Pakiet, Alicja; Mika, Adriana; Rostkowska, Olga; Makarewicz, Wojciech; Kobiela, Jaroslaw; Sledzinski, Tomasz; Stelmanska, Ewa published the artcile< In vivo effectiveness of orlistat in the suppression of human colorectal cancer cell proliferation>, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is colorectal cancer cell proliferation orlistat; Colorectal cancer; fatty acid synthase; orlistat; palmitate.

Background/Aim: Fatty acid synthase (FASN) provides palmitate for cell membrane formation in colorectal cancer (CRC) cells, however, palmitate is also available in the blood of CRC patients. The aim of this study was to examine whether orlistat, a FASN inhibitor, is able to attenuate CRC cell growth despite the availability of extracellular palmitate. Materials and Methods: Palmitate concentrations were measured in serum from CRC patients and healthy controls. HT-29 CRC cells were treated with orlistat and palmitate. Results: Treatment of CRC cells with orlistat caused a dose-dependent inhibition of cell proliferation. In turn, delivery of extracellular palmitate at doses lower than those found in the serum of CRC patients reversed inhibition by orlistat concentrations of up to 10μM. Conclusion: Inhibition of CRC cell proliferation by orlistat is reversed by palmitate which is present at high levels in the serum. Therefore, orlistat may be effective in vivo only at high concentrations

Anticancer Research published new progress about Antiproliferative 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

Nguyen, Phuong Thuy Viet; Huynh, Han Ai; Van Truong, Dat; Tran, Thanh-Dao; Vo, Cam-Van Thi published the artcile< Exploring aurone derivatives as potential human pancreatic lipase inhibitors through molecular docking and molecular dynamics simulations>, Application of C29H53NO5, the main research area is aurone pancreatic lipase inhibitor anticancer agent leukemia; aurone; human pancreatic lipase; human pancreatic lipase inhibitors; molecular docking; molecular dynamics simulations.

Inhibition of human pancreatic lipase, a crucial enzyme in dietary fat digestion and absorption, is a potent therapeutic approach for obesity treatment. In this study, human pancreatic lipase inhibitory activity of aurone derivatives was explored by mol. modeling approaches. The target protein was human pancreatic lipase (PDB ID: 1LPB). The 3D structures of 82 published bioactive aurone derivatives were docked successfully into the protein catalytic active site, using AutoDock Vina 1.5.7.rc1. Of them, 62 compounds interacted with the key residues of catalytic trial Ser152-Asp176-His263. The top hit compound (A14), with a docking score of -10.6 kcal·mol-1, was subsequently submitted to mol. dynamics simulations, using GROMACS 2018.01. Mol. dynamics simulation results showed that A14 formed a stable complex with 1LPB protein via hydrogen bonds with important residues in regulating enzyme activity (Ser152 and Phe77). Compound A14 showed high potency for further studies, such as the synthesis, in vitro and in vivo tests for pancreatic lipase inhibitory activity.

Molecules published new progress about Antitumor agents. 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

Marounek, M; Volek, Z; Taubner, T; Czauderna, M published the artcile< Metabolic Effects of a Hydrophobic Alginate Derivative and Tetrahydrolipstatin in Rats Fed a Diet Supplemented with Palm Fat and Cholesterol.>, Application of C29H53NO5, the main research area is .

The effects of octadecylamide of alginic acid (amidated alginate) and tetrahydrolipstatin on serum and hepatic cholesterol, and the faecal output of fat and sterols, were investigated in rats. Amidated alginate is a sorbent of lipids, tetrahydrolipstatin is an inhibitor of pancreatic lipase. Rats were fed diets containing cholesterol and palm fat at 10 and 70 g/kg, respectively. Palm fat was provided by coconut meal. Amidated alginate at 40 g/kg diet significantly decreased serum total cholesterol, low-density lipoprotein and hepatic cholesterol, and hepatic lipids and increased the faecal output of fat and coprostanol. Tetrahydrolipstatin at 300 mg/kg diet significantly decreased low-density lipoprotein cholesterol and hepatic lipids and increased the faecal output of fat. The intake of feed was not significantly influenced; however, the weight gains in rats fed amidated alginate were lower than in rats of the control group. Both amidated alginate and tetrahydrolipstatin modified the fatty acid profile in excreta lipids. Concentrations of saturated fatty acids were decreased and those of unsaturated fatty acids increased. Despite different modes of action, amidated alginate and tetrahydrolipstatin were equally efficient in removing the dietary fat from the body.

Folia biologica 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

Harapko, Tetiana V; Mateshuk-Vatseba, Lesia R published the artcile< MORPHOMETRIC AND ELECTRON MICROSCOPIC CHANGES OF STRUCTURAL COMPONENTS OF LYMPH NODES DURING CORRECTION OF THE ACTION OF SODIUM GLUTAMATE WITH ORLISTAT.>, HPLC of Formula: 96829-58-2, the main research area is correction; endotheliocyte; lymphocyte ; orlistat ; sodium glutamate.

OBJECTIVE: The aim: To study morphometric and electron microscopic changes in the parenchyma of rat lymph nodes under the action of sodium glutamate and its correction by orlistat. PATIENTS AND METHODS: Materials and methods: The article presents and analyzes the data of an experimental study conducted on 66 white male rats and females of reproductive age. Experimental animals are divided into 4 groups. RESULTS: Results: After six weeks of exposure to monosodium glutamate, there was a significant decrease in the relative area of the cortical substance in the lymph nodes of white male and female rats by 11.95% and 9.31% and, respectively, an increase in the relative area of the medullary substance by 18.76% and 14.7% in compared with an intact group of animals. After six weeks of sodium glutamate and the next six weeks of the standard diet of vivarium and orlistat, the relative area of the cortical substance in the lymph node parenchyma was 2.55% and 0.38% more than the parameters of the intact group of animals, respectively. Accordingly, the relative area of the medullary substance decreased and was 4.01% and 0.59% less compared to the intact group of animals. CONCLUSION: Conclusions: Electron microscopic examination showed that monosodium glutamate causes changes in the parenchyma of the lymph nodes as in a high-calorie diet. The introduction of orlistat (xenical) leads to a partial restoration of the structural organization, and hence the function of this organ.

Wiadomosci lekarskie (Warsaw, Poland : 1960) published new progress about 96829-58-2. 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

Son, Jang Won; Kim, Sungrae published the artcile< Comprehensive Review of Current and Upcoming Anti-Obesity Drugs.>, Product Details of C29H53NO5, the main research area is Bupropion; Drug therapy; Liraglutide; Naltrexone; Obesity; Orlistat; Phentermine.

Obesity is among the leading causes of morbidity and mortality worldwide and its prevalence continues to increase globally. Because obesity is a chronic, complex, and heterogeneous disease influenced by genetic, developmental, biological, and environmental factors, it is necessary to approach obesity with an integrated and comprehensive treatment strategy. As it is difficult to achieve and sustain successful long-term weight loss in most patients with obesity through lifestyle modifications (e.g., diet, exercise, and behavioral therapy), pharmacological approaches to the treatment of obesity should be considered as an adjunct therapy. Currently, four drugs (orlistat, naltrexone extended-release [ER]/bupropion ER, phentermine/topiramate controlled-release, and liraglutide) can be used long-term (>12 weeks) to promote weight loss by suppressing appetite or decreasing fat absorption. Pharmacotherapy for obesity should be conducted according to a proper assessment of the clinical evidence and customized to individual patients considering the characteristics of each drug and comorbidities associated with obesity. In this review, we discuss the mechanisms of action, efficacy, and safety of these available long-term anti-obesity drugs and introduce other potential agents under investigation. Furthermore, we discuss the need for research on personalized obesity medicine.

Diabetes & metabolism journal published new progress about 96829-58-2. 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

Abou-El-Naga, I. F.; Sa, D. E.; Gaafar, M. R.; Ahmed, S. M.; El-Deeb, S. A. published the artcile< A new scope for orlistat: Effect of approved anti-obesity drug against experimental microsporidiosis>, Product Details of C29H53NO5, the main research area is antiobesity drug orlistat microsporidiosis intestine.

As the current therapies for intestinal microsporidiosis are either inconsistent in their efficacies or hampered by several adverse effects, alternative antimicrosporidial agents are being sought. The present study is the first that was designed to evaluate the potency of orlistat, an approved anti-obesity drug, against intestinal microsporidiosis caused by both Enterocytozoon bieneusi and Encephalitozoon intestinalis. Results were assessed through studying fecal and intestinal spore load, intestinal histopathol. changes, viability, and infectivity of spores from treated animals. Results showed that orlistat has promising antimicrosporidia potential, with better results in E. intestinalis than E. bieneusi. The animals that received orlistat showed statistically significant decrease in the fecal and intestinal spore load, when compared to the corresponding control infected nontreated mice. The results were insignificant compared to fumagillin and albendazole. Light microscopic examination of stained intestinal sections revealed amelioration of the pathol. changes and decreased inflammatory cells detected in the control infected nontreated mice. Spores encountered from stool of orlistat-treated E. bieneusi and E. intestinalis mice showed low viability and significant reduction of infectivity vs. their control. Thus, considering the results of the present work, orlistat proved its effectiveness against the intestinal microsporidial infection.

Medical Mycology 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