Category: 96829-58-2

Kitadokoro, Kengo; Tanaka, Mutsumi; Hikima, Takaaki; Okuno, Yukiko; Yamamoto, Masaki; Kamitani, Shigeki published the artcile< Crystal structure of pathogenic Staphylococcus aureus lipase complex with the anti-obesity drug orlistat.>, Product Details of C29H53NO5, the main research area is .

Staphylococcus aureus lipase (SAL), a triacylglycerol esterase, is an important virulence factor and may be a therapeutic target for infectious diseases. Herein, we determined the 3D structure of native SAL, the mutated S116A inactive form, and the inhibitor complex using the anti-obesity drug orlistat to aid in drug development. The determined crystal structures showed a typical α/β hydrolase motif with a dimeric form. Fatty acids bound near the active site in native SAL and inactive S116A mutant structures. We found that orlistat potently inhibits SAL activity, and it covalently bound to the catalytic Ser116 residue. This is the first report detailing orlistat-lipase binding. It provides structure-based information on the production of potent anti-SAL drugs and lipase inhibitors. These results also indicated that orlistat can be repositioned to treat bacterial diseases.

Scientific reports 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

Gomaa, Adel A.; El-Sers, Dalia A.; Al-Zokeim, Nahla I.; Gomaa, Mohamed A. published the artcile< Amelioration of experimental metabolic syndrome induced in rats by orlistat and Corchorus olitorius leaf extract; role of adipo/cytokines>, 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 Corchorus olitorius leaf extract metabolic syndrome amelioration cytokines; Corchorus olitorius ; cytokines; histopathology; lipid profile; obesity.

To determine the efficacy of Corchorus olitorius (C. olitorius) leaf extract in the prevention of metabolic syndrome induced in rats by high-fat diet (HFD) and compare it with that of orlistat. Phytochem. anal. was performed. Effect of orlistat and C. olitorius extract on lipase activity and acute food intake were investigated. Body weight, biochem. parameters and histopathol. examination were demonstrated. Corchorus olitorius extract inhibited the pancreatic lipase activity, but orlistat was more potent. Cumulative food intake has not changed by the tested agents. In obese rats, C. olitorius or orlistat significantly decreased weight gain and visceral white adipose tissue. They exhibited a significant reduction in serum glucose, total cholesterol, triglycerides, low d. lipoprotein cholesterol, free fatty acids, IL-1β, tumor necrosis factor-α (TNF-α), insulin and leptin levels of obese rat groups while high d. lipoprotein cholesterol and adiponectin levels were significantly increased by them. Histopathol. examination of the liver revealed that C. olitorius was more effective than orlistat in the alleviating of steatosis and adipocyte hypertrophy shown in obese control rats. Corchorus olitorius is effective as orlistat in preventing obesity, hyperlipidemia, steatosis and insulin resistance. These actions may be mediated by inhibiting of lipase activity, TNF-α, IL-1β and leptin resistance along with increasing of adiponectin.

Journal of Pharmacy and Pharmacology published new progress about Acute toxicity. 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

Shang, Chunliang; Li, Yuan; He, Tianhui; Liao, Yuandong; Du, Qiqiao; Wang, Pan; Qiao, Jie; Guo, Hongyan published the artcile< The prognostic miR-532-5p-correlated ceRNA-mediated lipid droplet accumulation drives nodal metastasis of cervical cancer>, Category: amides-buliding-blocks, the main research area is ACC1, Acetyl-CoA carboxylase 1; ACOX1, Acyl-CoA oxidase 1; ATCC, The American Type Culture Collection; BMI, Body mass index; CC, Cervical cancer; CPAT, The coding potential assessment tool; CPT1A, Carnitine palmitoyltransferase-1A; Cervical cancer; CircRNAs, circular RNAs; DFS, Disease free survival; EMT, Epithelial-mesenchymal transition; ES, enrichment score; FA, Fatty acid; FASN; FASN, Fatty acid synthase; GEPIA, The Gene Expression Profiling Interactive Analysis; GSEA, Gene set enrichment analysis; HE, Hematoxylin-eosin; HLECs, Human lymphatic endothelial cells; IHC, immunohistochemistry; ISH, In situ hybridization; LASSO, The least absolute shrinkage and selection operator; LDs, Lipid droplets; LINC01410, Long non-coding RNA 01410; LNM, lymph node metastasis; Lipid droplet; LncRNAs, Long noncoding RNAs; Lymph node metastasis; MES, Maximum enrichment score; MREs, MiRNA response elements; Mfe, The minimum free energy; NCF2, Neutrophil cytosolic factor 2; OS, Overall survival; PLIN2, Perilipin 2; PLs, Phospholipids; RIP, RNA immunoprecipitation; ROC, The receiver operating characteristic; SNR, signal-to-noise ratio; STR, short tandem repeat; TCGA, The Cancer Genome Atlas; TGs, Triglycerides; ceRNA, Competing endogenous RNA; miRNA prognostic model; miRNAs, MicroRNAs; ncRNAs, Noncoding RNAs.

The prognosis for cervical cancer (CC) patients with lymph node metastasis (LNM) is extremely poor. Lipid droplets (LDs) have a pivotal role in promoting tumor metastasis. The crosstalk mechanism between LDs and LNM modulated in CC remains largely unknown. This study aimed to construct a miRNA-dependent progonostic model for CC patients and investigate whether miR-532-5p has a biol. impact on LNM by regualting LDs accumulation. LASSO-Cox regression was applied to establish a prognostic prediction model. miR-532-5p had the lowest P-value in RNA expression (P < 0.001) and prognostic prediction (P < 0.0001) and was selected for further study. The functional role of the prognostic miR-532-5p-correlated competing endogenous RNA (ceRNA) network was investigated to clarify the crosstalk between LDs and LNM. The underlying mechanism was determined using site-directed mutagenesis, dual luciferase reporter assays, RNA immunoprecipitation assays, and rescue experiments A xenograft LNM model was established to evaluate the effect of miR-532-5p and orlistat combination therapy on tumor growth and LNM. A novel 5-miRNAs prognostic signature was constructed to better predict the prognosis of CC patient. Further study demonstrated that miR-532-5p inhibited epithelial-mesenchymal transition and lymphangiogenesis by regulating LDs accumulation. Interestingly, we also found that LDs accumulation promoted cell metastasis in vitro. Mechanistically, we demonstrated a miR-532-5p-correlated ceRNA network in which LINC01410 was bound directly to miR-532-5p and effectively functioned as miR-532-5p sponge to disinhibit its target gene-fatty acid synthase (FASN). Combined therapy with miR-532-5p and FASN inhibitor-orlistat further inhibited tumor growth and LNM in vivo. Our findings highlight a LD accumulation-dependent mechanism of miR-532-5p-modulated LNM and support treatment with miR-532-5p/orlistat as novel strategy for treating patients with LNM in CC. Journal of Advanced Research 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

Gorgojo-Martinez, Juan J.; Basagoiti-Carreno, Belen; Sanz-Velasco, Alberto; Serrano-Moreno, Clara; Almodovar-Ruiz, Francisca published the artcile< Effectiveness and tolerability of orlistat and liraglutide in patients with obesity in a real-world setting: The XENSOR Study>, Category: amides-buliding-blocks, the main research area is obesity cardiovascular risk factor orlistat liraglutide.

To evaluate in a real-world setting the effectiveness of two drugs, orlistat and liraglutide, in patients with overweight or obesity and insufficient weight loss (WL) after a lifestyle modification program. Retrospective, observational cohort study comparing clin. outcomes of orlistat 120 mg three times a day and liraglutide (up to 3 mg daily) in adult patients with BMI =30 kg/m2 or =27 kg/m2 with at least a weight-related comorbidity who had failed to lose at least 5% of their weight after 6 mo of lifestyle modification. The co-primary end-points, assessed at 3-6 mo and at the end of the follow-up, were weight change from baseline, proportion of patients who lost at least 5% of their baseline weight and adjusted differences in WL between both drugs. Five hundred patients, 400 in the group of orlistat (age 47.0, weight 107.8 kg) and 100 in the group of liraglutide (age 51.9 years, weight 105.1 kg), were included. WL with liraglutide (-7.7 kg) was significantly greater than that observed with orlistat (-3.3 kg), and more individuals lost at least 5% of their baseline weight with liraglutide (64.7%) than with orlistat (27.4%). In this real-world study, liraglutide showed a greater effectiveness in WL compared with orlistat and improved several obesity-associated metabolic and cardiovascular risk factors.

International Journal of Clinical Practice published new progress about Antiarrhythmics. 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

Suleiman, Joseph Bagi; Nna, Victor Udo; Zakaria, Zaida; Othman, Zaidatul Akmal; Bakar, Ainul Bahiyah Abu; Mohamed, Mahaneem published the artcile< Obesity-induced testicular oxidative stress, inflammation and apoptosis: Protective and therapeutic effects of orlistat>, HPLC of Formula: 96829-58-2, the main research area is orlistat antiobesity agent testicular oxidative stress inflammation apoptosis obesity; Apoptosis; High-fat diet; Inflammation; Obesity; Orlistat; Oxidative stress.

The objective of this study was to determine effects of the anti-obesity drug orlistat, on testicular oxidative stress, inflammation and apoptosis in high-fat diet (HFD)-fed rats. Twenty-four adult male Sprague Dawley rats weighing 250-300 g were randomized into four groups (n = 6/group), namely; normal control (NC), high-fat diet (HFD), HFD plus orlistat (10 mg/kg body weight/day administered concurrently for 12 wk) (HFD + Opr) and HFD plus orlistat (10 mg/kg body weight/day administered 6 wk after induction of obesity) (HFD + Ot) groups. Antioxidant enzymes activities were significantly decreased, while mRNA levels of pro-apoptotic markers (p53, Bax/BCl-2, caspase-9, caspase-8 and caspase-3) were significantly increased in the testis of HFD group relative to NC group. Furthermore, mRNA levels of pro-inflammatory markers (nuclear factor kappa B, inducible nitric oxide synthase, tumor necrosis factor alpha and interleukin (IL)-1beta increased significantly, while anti-inflammatory marker (IL-10) decreased significantly in testis of the HFD group relative to NC group. However, in both models of orlistat intervention (protective and treatment models) up-regulated antioxidant enzymes, down-regulated inflammation and apoptosis were observed in the testis of HFD-fed rats. Orlistat ameliorated testicular dysfunction by attenuating oxidative stress, inflammation and apoptosis in HFD-fed rats, suggesting its potential protective and therapeutic effects in the testis compromised by obesity.

Reproductive Toxicology published new progress about Anti-inflammatory 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

Cohen, Jordana B.; Gadde, Kishore M. published the artcile< Weight Loss Medications in the Treatment of Obesity and Hypertension>, Related Products of 96829-58-2, the main research area is review antiobesity agent weight loss obesity hypertension; Blood pressure; Hypertension; Obesity; Weight loss; Weight loss medication; Weight loss pharmacotherapy.

A review. Purpose of Review: Weight loss is strongly associated with improvement in blood pressure; however, the mechanism of weight loss can impact the magnitude and sustainability of blood pressure reduction Recent Findings: Five drugs-orlistat, lorcaserin, liraglutide, phentermine/topiramate, and naltrexone/bupropion-are currently approved for weight loss therapy in the USA. Naltrexone/bupropion results in an increase in in-office and ambulatory blood pressure compared to placebo. Other therapies are associated with modest lowering of blood pressure, and are generally well-tolerated; nonetheless, evidence is limited regarding their effect on blood pressure, particularly longitudinally, in individuals with hypertension. Summary: Although weight loss medications can be an effective adjunct to lifestyle modifications in individuals with obesity, there is limited evidence regarding their benefit with regard to blood pressure. Future studies evaluating the effectiveness of weight loss medications should include careful assessment of their short- and long-term impact on blood pressure in individuals with hypertension.

Current Hypertension Reports 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

Miklos, Zsuzsanna; Wafa, Dina; Nadasy, Gyorgy L.; Toth, Zsuzsanna E.; Besztercei, Balazs; Dornyei, Gabriella; Laska, Zsofia; Benyo, Zoltan; Ivanics, Tamas; Hunyady, Laszlo; Szekeres, Maria published the artcile< Angiotensin II-induced cardiac effects are modulated by endocannabinoid-mediated CB1 receptor activation>, Quality Control of 96829-58-2, the main research area is Angiotensin II; CB1 cannabinoid receptor; cardiac; coronary flow; endocannabinoid; myocardial function; vasoconstriction.

Angiotensin II (Ang II) has various cardiac effects and causes vasoconstriction. Ang II activates the type-1 angiotensin receptor-Gq/11 signaling pathway resulting in the release of 2- arachidonoylglycerol (2-AG). We aimed to investigate whether cardiac Ang II effects are modulated by 2-AG-release and to identify the role of type-1 cannabinoid receptors (CB1R) in these effects. Expression of CB1R in rat cardiac tissue was confirmed by immunohistochem. To characterize short-term Ang II effects, increasing concentrations of Ang II (10-9-10-7 M); whereas to assess tachyphylaxis, repeated infusions of Ang II (10-7 M) were administered to isolated Langendorff-perfused rat hearts. Ang II infusions caused a decrease in coronary flow and ventricular inotropy, which was more pronounced during the first administration. CB agonist 2-AG and WIN55,212-2 administration to the perfusate enhanced coronary flow. The flow-reducing effect of Ang II was moderated in the presence of CB1R blocker O2050 and diacylglycerol-lipase inhibitor Orlistat. Our findings indicate that Ang II-induced cardiac effects are modulated by simultaneous CB1R-activation, most likely due to 2-AG-release during Ang II signalling. In this combined effect, the response to 2-AG via cardiac CB1R may counteract the pos. inotropic effect of Ang II, which may decrease metabolic demand and augment Ang II-induced coronary vasoconstriction.

Cells published new progress about 96829-58-2. 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

Vakhitov, D; Mella, M; Hakovirta, H; Suominen, V; Oksala, N; Saarinen, E; Romsi, P published the artcile< Prognostic Risk Factors for the Development of Compartment Syndrome in Acute Lower Limb Ischemia Patients Treated With Catheter-Directed Thrombolysis.>, 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 Compartment syndrome; Compartment syndrome after CDT; Compartment syndrome after catheter-directed thrombolysis.

BACKGROUND: To determine predisposing factors that may lead to the development of compartment syndrome (CS) in patients with acute lower limb ischemia (ALLI) managed with intra-arterial catheter-directed thrombolysis (CDT). METHODS: This is a retrospective study of patients admitted between 01/2002 and 12/2015 to three university hospitals in Tampere, Turku, and Oulu, Finland, with acute or acute-on-chronic lower limb ischemia (Rutherford I-IIb). Patients managed with CDT and aspiration thrombectomies (AT) as an adjunct to CDT were included in the study. Multivariable binary logistic regression models were used to detect possible risk factors for the development of CS and its impact on the limb salvage and survival. Amputation-free survival (AFS) rates of CS and non-CS patients were compared using Kaplan-Meier survival analysis. The length of hospitalization was calculated and compared between the CS and non-CS groups. RESULTS: A total of 292 CDTs with or without ATs were performed on patients with a mean age of 71 years (standard deviation 13 years), 151 (51.7%) being male. Altogether, 12/292 (4.1%) treatment-related CS cases were registered. Renal insufficiency (odds ratio [OR] 4.27, P = 0.07) was associated with an increased risk of CS. All CS cases were managed with fasciotomies. Treatment with fasciotomy was associated with a prolonged hospitalization of a median of 7 days versus the 4 days for non-CS patients, P < 0.001. During the median follow-up of 51 months (interquartile range 72 months), 152/292 (52.1%) patients died and 51/292 (17.5%) underwent major amputations. CS was not associated with an increased risk of mortality, but it was associated with a higher risk of major amputation (OR 3.87, P = 0.027). The AFS rates of patients with or without CS did not significantly differ from each other in the long term. CONCLUSIONS: CS after CDT for the treatment of ALLI is uncommon. Renal insufficiency is associated with an increased risk of CS. Fasciotomy prolongs the hospitalization. Patients with CS are exposed to an increased risk of major amputation. Annals of vascular surgery 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

Cheng, Ching-Feng; Ku, Hui-Chen; Cheng, Jing-Jy; Chao, Shi-Wei; Li, Hsiao-Fen; Lai, Pei-Fang; Chang, Che-Chang; Don, Ming-Jaw; Chen, Hsi-Hsien; Lin, Heng published the artcile< Adipocyte browning and resistance to obesity in mice is induced by expression of ATF3.>, Computed Properties of 96829-58-2, the main research area is Diabetes; Drug discovery; Medical research; Obesity; Transcription.

Billions of people have obesity-related metabolic syndromes such as diabetes and hyperlipidemia. Promoting the browning of white adipose tissue has been suggested as a potential strategy, but a drug still needs to be identified. Here, genetic deletion of activating transcription factor 3 (ATF3-/- ) in mice under a high-fat diet (HFD) resulted in obesity and insulin resistance, which was abrogated by virus-mediated ATF3 restoration. ST32da, a synthetic ATF3 inducer isolated from Salvia miltiorrhiza, promoted ATF3 expression to downregulate adipokine genes and induce adipocyte browning by suppressing the carbohydrate-responsive element-binding protein-stearoyl-CoA desaturase-1 axis. Furthermore, ST32da increased white adipose tissue browning and reduced lipogenesis in HFD-induced obese mice. The anti-obesity efficacy of oral ST32da administration was similar to that of the clinical drug orlistat. Our study identified the ATF3 inducer ST32da as a promising therapeutic drug for treating diet-induced obesity and related metabolic disorders.

Communications biology 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

Singh, Awadhesh Kumar; Singh, Ritu published the artcile< Pharmacotherapy in obesity: a systematic review and meta-analysis of randomized controlled trials of anti-obesity drugs>, Application In Synthesis of 96829-58-2, the main research area is meta analysis obesity orlistat phentermine lorcaserin topiramate naltrexone pharmacotherapy; Obesity; anti-obesity drugs; liraglutide 3.0 mg; lorcaserin; naltrexone plus bupropion; orlistat; phentermine plus topiramate.

Meta-anal. of obesity poses a significant increase in morbidity and mortality and thus five anti-obesity drugs have been approved currently by US FDA. Several phase 3 trials have shown a significant improvement in cardio-metabolic profile including significant weight reduction with these agents compared to placebo. We systematically searched the database of PubMed, Embase, The Cochrane Library and The ClinicalTrials.gov up to 30 Sept. 2019 and retrieved all the randomized controlled trials (RCTs) that were conducted with these five drugs for ≥1 yr and explicitly reported their efficacy vs. placebo. Subsequently, we have conducted the meta-anal. to primarily study the effect of these anti-obesity drugs on weight reduction We addnl. reviewed the effect of these drugs on other cardio-metabolic parameters including key adverse events. This meta-anal. finds a significant reduction in body weight with orlistat (N = 10,435; Δ -3.07 Kg, 95% CI, -3.76 to -2.37), phentermine plus topiramate (N = 2985; Δ -9.77 Kg; 95% CI, -11.73 to -7.81), lorcaserin (N = 16,856; Δ -3.08 Kg; 95% CI, -3.49 to -2.66), naltrexone plus bupropion (N = 3239; Δ -4.39 Kg; 95% CI, -5.05 to -3.72) and liraglutide (N = 4978; Δ -5.25 Kg; 95% CI, -6.17 to -4.32), compared to placebo (all p < 0.00001). Expert Review of Clinical Pharmacology 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