Category: 96829-58-2

Shamarao, Nagashree; Chethankumar, Mukunda published the artcile< Antiobesity drug-likeness properties and pancreatic lipase inhibition of a novel low molecular weight lutein oxidized product, LOP6>, Application In Synthesis of 96829-58-2, the main research area is lutein oxidized product antiobesity pancreatic lipase inhibition obesity.

Elevated expression of peroxisome proliferator-activated receptor-gamma (PPAR-γ), a key regulator of adipogenesis, leads to lipid accumulation and obesity. Although orlistat is effective for obesity, flatus with discharge, faecal urgency, oily evacuation and other allied side effects limit its usage. Thus, natural product-based drug intervention is the future of research and development of novel treatment. We synthesized and characterized total lutein oxidized products (LOPs) by exposing lutein to direct sunlight with a solar intensity of 5.89 kW h m-2 day-1 and at 31 ± 2 °C for 1-10 days. Total LOPs were analyzed on C18 and structural elucidation was carried on LCMS/MS-TOF. The pancreatic lipase inhibition kinetics was estimated The binding effects of LOP6 (fragmented peak 6) on PPAR-γ, pancreatic lipase, pharmacokinetic properties and inhibition studies were analyzed. Histol. evaluation of liver and adipose tissues was performed to confirm the antiobesity effect of total LOPs. The yield of extracted lutein purified from shade-dried marigold flower petals was 6%. Total LOPs were formed on the 10th day upon exposure of lutein to direct sunlight. Total LOPs on the C18 column fragmented into eight oxidized products (LOP1 to LOP8). The total LOPs showed significant inhibition of pancreatic lipase activity with an IC50 of 1.6953 μg ml-1, and Km and Vmax of 3.05 μg and 1.19 μg s-1 resp. following mixed type of inhibition. The LOP6 [4-((1E,3E,5E)-3,7-dimethylocta-1,3,5,7-tetraen-1-yl)-3,5,5-trimethylcyclohex-3-enol] with an approx. mol. mass of 274.25 showed a binding energy of -5.40 kcal mol-1 with a Ki of 109.43 μM for PPAR-γ and a docking score of -5.35 kcal mol-1 with a Ki of 119.4 μM for pancreatic lipase. The IC50 of LOP6 was 11.8420 μg ml-1, and Km and Vmax were 2.519 μg and 1.294 μg s-1. The pharmacokinetic properties such as solubility, permeability, bioavailability, and topol. polar surface area when tested with LOP6 were significantly better than those of lutein alone. The histol. examination of the liver and adipose tissue revealed that all three doses of total LOPs were effective in alleviating the ballooning and vesicular degeneration of hepatocytes and invasion of inflammatory cells in the adipose tissue. Total LOPs and LOP6 inhibited pancreatic lipase activity in vitro. LOP6 showed a better docking score for PPAR-γ and pancreatic lipase in comparison to orlistat. Histol. data showed that the total LOPs exerted antiobesity activity. Thus, LOPs might provide a novel treatment approach for obesity.

Food & Function published new progress about Adipose tissue. 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

Tong, Jing; Xiang, Lulu; Niu, Yichao; Zhang, Ting published the artcile< Effect of orlistat intervention on in vitro fertilization/intracytoplasmic sperm injection outcome in overweight/obese infertile women>, Quality Control of 96829-58-2, the main research area is CRP fertilization overweight obese infertile; Orlistat; clinical pregnancy rate; in vitro fertilization/intracytoplasmic sperm injection; obese; overweight.

ObjectiveThis retrospective study sought to evaluate the effect of orlistat intervention on the outcome of in vitro fertilization/intracytoplasmic sperm injection (IVF/ICSI) in overweight/obese infertile women. MethodsTwenty-nine overweight/obese patients undergoing IVF/ICSI for the first time were treated with orlistat intervention (orlistat group). Another 29 patients with matched age and body mass index (BMI) were included in the control group at a ratio of 1:1. Clin. data of both groups were collected, and the clin. baseline data, IVF/ICSI cycle information and embryo transfer outcome were compared between groups by Students t-test or chi-square test when appropriate. ResultsThe 29 patients in the orlistat group completed 37 embryo transfer cycles, and the 29 subjects in the control group completed 38 embryo transfer cycles. There was no significant difference in the clin. baseline data or IVF/ICSI cycle data between the two groups (p > .05). In the end, 22 transfer cycles in orlistat group obtained clin. pregnancies, 5 obtained biochem. pregnancies and 10 had non-pregnancies. As for the control group, 15 transfer cycles obtained clin. pregnancies, 15 achieved biochem. pregnancies and 8 had non-pregnancies. The clin. pregnancy rate of the orlistat group was significantly higher than that of the control group (59.46% vs. 39.47%, p = .004), but there was no significant difference in the live birth rate between the two groups (54.05% vs. 36.84%, p > .05). ConclusionsOrlistat intervention for overweight/obese infertile women receiving IVF/ICSI treatment will increase the clin. pregnancy rate, without affecting the total amount of gonadotropins, ovarian stimulation time or the follicular output rate (FORT).

Gynecological Endocrinology published new progress about Adiponectins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Martínez Insfran, Luis Alberto; Alconchel Gago, Felipe; Parrilla Paricio, Pascual published the artcile< Fulminant liver failure secondary to submassive hepatic necrosis in a patient treated with Orlistat. A case report.>, 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 is an intestinal lipase inhibitor drug that is recommended in obese patients along with a hypocaloric diet. Although the most frequent secondary effect is steatorrhea, fulminant liver failure has also been associated with this drug, which has required liver transplantation in 3 patients. We present the case of a 42-year-old obese male.

Revista espanola de enfermedades digestivas : organo oficial de la Sociedad Espanola de Patologia Digestiva 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

You, Bang-Jau; Chen, Li-Yun; Hsu, Po-Hsiang; Sung, Pei-Hsuan; Hung, Yu-Ching; Lee, Hong-Zin published the artcile< Orlistat Displays Antitumor Activity and Enhances the Efficacy of Paclitaxel in Human Hepatoma Hep3B Cells>, COA of Formula: C29H53NO5, the main research area is orlistat antitumor activity paclitaxel human Hep3B.

Orlistat has been proved to be an effective fatty acid synthase inhibitor that is able to inhibit the proliferation and induce apoptosis in many cancer cell types. However, the anticancer effects of orlistat on hepatocellular carcinoma are undefined. The authors found that orlistat inhibited cell growth and induced G0/G1 cell cycle arrest with increased cyclin D, cyclin E, and p21 expression in human hepatoma Hep3B cells. Furthermore, protein expression of cyclin A, cyclin B, Cdk1, Cdk2, and Cdk4 was reduced by orlistat. This study investigated the role of lipid metabolism on orlistat-induced human hepatoma Hep3B cell death. The decrease in the expression of key enzymes in fatty acid metabolism, including FASN, ACOT8, PPT1, FABP1, CPT1 and CPT2, was observed after orlistat treatment. The authors also demonstrated that peroxisomal activity was involved in the orlistat-induced Hep3B cell death. In this study, the authors established an in vitro model to investigate the effect of orlistat on lipid accumulation. The authors found that orlistat significantly inhibited the cellular lipid content when administered in fatty acid overload conditions in Hep3B cells. Combination treatment of orlistat and paclitaxel was able to induce a synergistic effect on growth inhibition and cell apoptosis in Hep3B cells. The authors’ data suggested that orlistat displays antitumor activity and enhances the efficacy of paclitaxel in Hep3B cells.

Chemical Research in Toxicology published new progress about Antitumor agents. 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

Murshed, Mubtasim; Pham, Anna; Vithani, Kapilkumar; Salim, Malinda; Boyd, Ben J. published the artcile< Controlling drug release by introducing lipase inhibitor within a lipid formulation>, HPLC of Formula: 96829-58-2, the main research area is Controlled-release; Drug overdose prevention; In vitro lipolysis; Lipase inhibitor; Lipid-based drug delivery systems (LBDDS); Oral formulation.

Drug overdose connected to marketed pharmaceutical products, particularly opioids, occurs at an alarming rate. Novel strategies through innovative formulation approaches that reduce the likelihood of overdose while allowing safe therapeutic outcomes are urgently required. The current study provides a proof-of-concept for a new formulation approach by co-formulating drug with a lipase inhibitor within a solid lipid formulation in order to prevent or reduce the harmful effects of taking multiple doses of an oral solid dose form. Lipase inhibitor controlled-release (LICR) formulations were created using a simple hot melt method to co-formulate the inhibitor (orlistat) and ibuprofen, as the model drug, within the lipid matrix. The digestion and drug release kinetics were determined using an in vitro lipolysis model. Above a threshold level of orlistat there was decreased digestibility of multiple doses of the LICR formulations, leading to reduced drug release. Upon administration of the formulations in capsules to rats, the LICR formulation displayed the lowest exposure of ibuprofen during the pharmacokinetic studies. This novel formulation approach shows promise in preventing accidental drug overdose after oral administration of multiple doses of formulation.

International Journal of Pharmaceutics (Amsterdam, Netherlands) 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

Braeckmans, Marlies; Brouwers, Joachim; Mols, Raf; Servais, Cecile; Tack, Jan; Augustijns, Patrick published the artcile< Orlistat disposition in the human jejunum and the effect of lipolysis inhibition on bile salt concentrations and composition>, Application In Synthesis of 96829-58-2, the main research area is Bile salts; Fed state; Fenofibrate; Intestinal drug absorption; Jejunum; Orlistat.

The lipolysis-mediated postprandial small intestinal environment is known to influence the solubilisation and subsequent absorption of lipophilic drugs. In a previously performed small-scale clin. study in healthy volunteers, co-administration of the lipase inhibitor orlistat increased jejunal solubilisation and systemic absorption of fenofibrate after intake of the lipid-based formulation Fenogal. In the present study, the jejunal disposition of the locally acting orlistat was assessed and linked to fenofibrate solubilisation. In addition, the effect of orlistat-induced lipolysis inhibition on bile salt concentrations and composition was evaluated. Orlistat was distributed predominantly in the lipid layer, as indicated by a 5- to 14-fold higher AUC0-320 min in the total jejunal samples as compared to the micellar layers. No effect of orally administered orlistat on bile salt composition or total concentrations (ranging from 1.5 to 24.8 mM and 1.8 to 33.2 mM with and without orlistat co-administration, resp.) could be observed The intraluminal presence of orlistat in the total jejunal samples correlated with the increased fenofibrate solubilisation in the jejunum (r = 0.9344) and enhanced absorption (r = 0.8184), highlighting the importance of the intraluminal lipid phase in lipophilic drug absorption.

International Journal of Pharmaceutics (Amsterdam, Netherlands) 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

Kim, Dae Hun; Maharjan, Pooja; Kim, Jae Yeol; Jang, Dong-Jin; Koo, Tae-Sung; Min, Kyoung Ah; Cho, Kwan Hyung published the artcile< Enhanced solubility, in-vitro dissolution and lipase inhibition of a self-nanoemulsifying drug delivery system containing 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 orlistat lipase solubility dissolution gastrointestinal lumen SNEDDS.

The aim of this work was to prepare and assess a self-nanoemulsifying drug delivery system (SNEDDS) containing water-insoluble orlistat that was used for the inhibition of lipase activity in gastrointestinal lumen. The pseudo-ternary phase diagram, composed of orlistat and medium chain triglycerides (MCT) as oil phase and Cremophor EL as surfactant, was made for the confirmation of giving SNEDDS preconc. The phys. state, particle size dispersed in water, dissolution and lipase inhibition of SNEDDS preconcs. were investigated. The appointed SNEDDS preconcs. in the pseudo-ternary phase diagram showed no endothermic peak of orlistat and a liquid state. The particle sizes of SNEDDS dispersed with water were uniform and in the range of <200 nm. In the dissolution test, the liquid SNEDDS preconc. and solid state mixture exhibited 90.89 ± 2.03% vs. 22.42 ± 3.71% at 60 min., resp., whereas the raw orlistat showed no significant dissolution rate. The SNEDDS preconc. showed a lipase inhibition of 92.42 ± 1.58% until 60 min., with no significant inhibition activity of orlistat. Therefore, the SNEDDS preconc. presented in this work solubilized orlistat and increased its dissolution rate, and resulted in sufficient inhibitory action on lipase. Journal of Nanoscience and Nanotechnology published new progress about Castor oil, ethoxylated Role: MOA (Modifier or Additive Use), PAC (Pharmacological Activity), THU (Therapeutic Use), USES (Uses), BIOL (Biological Study). 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

Wang, Ze; Zhao, Junli; Ma, Xiang; Sun, Yun; Hao, Guimin; Yang, Aijun; Ren, Wenchao; Jin, Lei; Lu, Qun; Wu, Gengxiang; Ling, Xiufeng; Hao, Cuifang; Zhang, Bo; Liu, Xinyu; Yang, Dongzi; Zhu, Yimin; Li, Jing; Bao, Hongchu; Wang, Ancong; Liu, Jianqiao; Chen, Zi-Jiang; Tan, Jichun; Shi, Yuhua published the artcile< Effect of Orlistat on Live Birth Rate in Overweight or Obese Women Undergoing IVF-ET: A Randomized Clinical Trial.>, 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 IVF; live birth; obesity management; orlistat; weight loss.

CONTEXT: Obesity management prior to infertility treatment remains a challenge. To date, results from randomized clinical trials involving weight loss by lifestyle interventions have shown no evidence of improved live birth rate. OBJECTIVE: This work aimed to determine whether pharmacologic weight-loss intervention before in vitro fertilization and embryo transfer (IVF-ET) can improve live birth rate among overweight or obese women. METHODS: We conducted a randomized, double-blinded, placebo-controlled trial across 19 reproductive medical centers in China, from July 2017 to January 2019. A total of 877 infertile women scheduled for IVF who had a body mass index of 25 or greater were randomly assigned to receive orlistat (n = 439) or placebo (n = 438) treatment for 4 to 12 weeks. The main outcome measurement was the live birth rate after fresh ET. RESULTS: The live birth rate was not significantly different between the 2 groups (112 of 439 [25.5%] with orlistat and 112 of 438 [25.6%] with placebo; P = .984). No significant differences existed between the groups as to the rates of conception, clinical pregnancy, or pregnancy loss. A statistically significant increase in singleton birth weight was observed after orlistat treatment (3487.50 g vs 3285.17 g in the placebo group; P = .039). The mean change in body weight during the intervention was -2.49 kg in the orlistat group, as compared to -1.22 kg in the placebo group, with a significant difference (P = .005). CONCLUSION: Orlistat treatment, prior to IVF-ET, did not improve the live birth rate among overweight or obese women, although it was beneficial for weight reduction.

The Journal of clinical endocrinology and metabolism 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

Sawami, Kosuke; Tanaka, Atsushi; Node, Koichi published the artcile< Anti-obesity therapy for cardiovascular disease prevention: potential expected roles of glucagon-like peptide-1 receptor agonists.>, 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 Anti-obesity; Glucagon-like peptide-1 receptor agonists; Liraglutide; Obesity-related cardiovascular disease; Semaglutide.

Obesity is characterized by visceral fat accumulation and various metabolic disturbances that cause metabolic syndrome and obesity-related cardiovascular diseases (ORCVDs). Hence, treatments targeting obesity should also prevent ORCVDs. Nonetheless, lifestyle modification therapy alone is still insufficient to reduce the risk of ORCVDs, although most cardiovascular guidelines still list it as the only treatment for obesity. Additionally, conventional anti-obesity drugs, such as orlistat, phentermine-topiramate, and naltrexone-bupropion, can reduce body weight but have not demonstrated a clear reduction in the risk of ORCVDs. To overcome this unmet clinical need, newer anti-obesity drugs must exhibit not only sufficient and long-lasting weight loss but also obvious cardiovascular benefits. Given recent clinical findings and evidences, in this context glucagon-like peptide-1 receptor agonist is currently available as a candidate that is clinically positioned as a first-line anti-obesity agent for the effective prevention of ORCVDs in people with obesity.

Cardiovascular diabetology 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

Knoke, Sabrina; Bunjes, Heike published the artcile< Transfer investigations of lipophilic drugs from lipid nanoemulsions to lipophilic acceptors: contributing effects of cholesteryl esters and albumin as acceptor structures>, 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 lipophilic drug acceptor lipid nanoemulsion cholesteryl ester albumin; bovine serum albumin; cholesteryl nonanoate; colloidal drug carriers; drug transfer; hydrogel beads; in vitro release; lipid nanoparticles.

When studying the release of poorly water-soluble drugs from colloidal drug delivery systems designed for i.v. administration, the release media should preferentially contain lipophilic components that represent the physiol. acceptors present in vivo. In this study, the effect of different acceptor structures was investigated by comparing the transfer of fenofibrate, retinyl acetate, and orlistat from trimyristin nanoemulsion droplets into lipid-containing hydrogel particles, as well as to bovine serum albumin (BSA). A nanodispersion based on trimyristin and cholesteryl nonanoate was incorporated into the hydrogel particles (mean diameter ~40μm) in order to mimic the composition of lipoproteins. The course of transfer observed utilizing the lipid-containing hydrogel particles as an acceptor was in relation to the lipophilicity of the drugs: the higher the logP value, the slower the transfer. There was no detectable amount of the drugs transferred to BSA in liquid solution, demonstrating clearly that albumin alone does not contribute substantially as acceptor for the lipophilic drugs under investigation in this study. In contrast, cholesteryl nonanoate contributes to a much greater extent. However, in all cases, the partition equilibrium of the drugs under investigation was in favor of the trimyristin emulsion droplets.

Pharmaceuticals published new progress about Albumins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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