Category: 96829-58-2

Del Castillo-Santaella, Teresa; Hernandez-Morante, Juan Jose; Suarez-Olmos, Jesus; Maldonado-Valderrama, Julia; Pena-Garcia, Jorge; Martinez-Cortes, Carlos; Perez-Sanchez, Horacio published the artcile< Identification of the thistle milk component Silibinin(A) and Glutathione-disulphide as potential inhibitors of the pancreatic lipase: Potential implications on weight loss>, HPLC of Formula: 96829-58-2, the main research area is silibinin glutathione disulfide antiobesity agent obesity.

Peripheral targets like pancreatic-lipase appear to be the most suitable pharmacol. alternative for obesity, as with orlistat, although its adverse effects limit its use. Therefore, the aim of this work was to identify new natural compounds able to inhibit pancreatic-lipase in an in vitro model. The DrugBank database was used to perform docking calculations The best fitting-score compounds were further evaluated in vitro. Our data revealed that glutathione-disulfide (GSSG) and silibinin(A) inhibit pancreatic-lipase. This was confirmed by measuring hydrolysis in an emulsion model, obtaining that the suppression of lipid digestion by silibinin(A) was higher than that of GSSG and close to the effect of orlistat. Combined anal. established the existence of different inhibition mechanisms for each compound In summary, silibinin(A) and GSSG inhibited pancreatic-lipase and, therefore, may be served as promise natural compounds to face with obesity. Further studies comprise the next step to fully validate the suitability of these compounds

Journal of Functional Foods published new progress about Antiobesity 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

Natour, Abdul Kader; Rteil, Ali; Shepard, Alexander; Weaver, Mitchell; Nypaver, Timothy; Nemeh, Hassan; Tanaka, Daizo; Kabbani, Loay published the artcile< Outcomes of patients with acute type A aortic dissection and concomitant lower extremity malperfusion.>, HPLC of Formula: 96829-58-2, the main research area is ATAD; Acute limb ischemia; Acute type A aortic dissection; Malperfusion syndromes.

OBJECTIVE: The occurrence of acute lower limb ischemia (ALLI) is a serious risk within the context of aortic dissection repair. The aim of the present study was to examine the outcomes of patients with acute type A aortic dissection (ATAD) and concomitant lower extremity malperfusion. METHODS: We performed a retrospective medical record review at our tertiary referral center of patients who underwent ATAD repair from January 2002 to June 2018. We used univariate and multivariate analyses to compare the outcomes of patients with and without lower extremity malperfusion. The primary outcomes were 30-day and 1-year mortality. RESULTS: A total of 378 patients underwent ATAD repair during the study period. Their mean age was 57 years, 68% were men, and 51% were White. A total of 62 patients (16%) presented with concomitant ALLI, including 35 (9%) who presented with isolated ALLI and 27 (7%) who presented with ALLI and concomitant malperfusion of at least one other organ. Of the 62 patients with ALLI, 46 underwent only proximal aortic repair. Of the 378 patients, 6 died within the first 24 hours, and their limb perfusion was not assessed. Among the 40 patients who underwent isolated proximal repair and survived >24 hours, 34 (85%) had resolution of their ALLI. Of the 16 patients who underwent concomitant lower extremity peripheral vascular procedures, 10 had bypass procedures and 1 died within 24 hours due to refractory coagulopathy and hypotension. All six patients with adequate follow-up imaging studies had asymptomatic occlusion of the bypass graft with recanalization of the occluded native arteries. Patients who presented with any organ malperfusion had increased 30-day (odds ratio, 1.8; P = .04) and 1-year (odds ratio, 1.8; P = .04) mortality and decreased overall survival (P < .01). For the patients with isolated ALLI, no significant differences were found in 30-day or 1-year mortality or overall survival (P = .57). CONCLUSIONS: Proximal repair of ATAD resolves most cases of associated ALLI, and isolated ALLI does not affect short- or long-term survival. All patients with follow-up in our study who underwent extra-anatomic bypass developed asymptomatic graft occlusion, which could be attributed to competitive flow from the remodeled native arterial system. We believe that rapid and aggressive restoration of flow to the lower extremity is the best method to treat ALLI malperfusion syndrome. Close monitoring for the development of compartment syndrome is recommended. Journal 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, HPLC of Formula: 96829-58-2.

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

Zhao, Jing; Zhang, Zhanwen; Nie, Dahong; Ma, Hui; Yuan, Gongjun; Su, Shu; Liu, Shaoyu; Liu, Sheng; Tang, Ganghua published the artcile< PET imaging of hepatocellular carcinomas: 18F-fluoropropionic acid as a complementary radiotracer for 18F-fluorodeoxyglucose>, Formula: C29H53NO5, the main research area is F-fluorodeoxyglucose (F-FDG); F-fluoropropionic acid (F-FPA); hepatocellular carcinoma (HCC); positron emission tomography (PET).

Objective: To evaluate the preclin. value of 18F-fluoropropionic acid (18F-FPA) and 18F-fluorodeoxyglucose (18F-FDG) positron emission tomog. (PET) for imaging HCCs. Methods: The 18F-FPAand 18F-FDGuptake patterns in 3HCCcell lines (Hep3B,HepG2, and SK-Hep1) were assessed in vitro and in vivo. The 18F-FPAuptakemechanismwas investigated using inhibition experimentswith orlistat and 5-tetradecyloxy-2-furoic acid.The 18F-FPAPET imagingwas performed in different tumor animalmodels and compared with 18F-FDG.We also evaluated the expressions of glucose transporter-1 (GLUT1), fatty acid synthase (FASN), and matrix metalloproteinase-2 (MMP2) in these cell lines. Results: In vitro experiments showed that the radiotracer uptake patterns were complementary in the HCC cell lines. Orlistat and 5-tetradecyloxy-2-furoic acid decreased the uptake of 18F-FPA. The tumor-to-liver ratio of 18F-FPA was superior to that of 18F-FDG in the SK-Hep1 and HepG2 tumors (P < .05). However, in the Hep3B tumors, the tumor-to-liver normalized uptake of 18F-FDG was higher than 18F-FPA (P < .01). FASN was highly expressed in cell lines with high 18F-FPA uptake, whereas GLUT1 was highly expressed in cell lines with high 18F-FDG uptake. The 18F-FPA uptake correlated with FASN (r = 0.89, P = .014) and MMP2 (r = 0.77, P = .002) expressions. Conclusions: PET imaging with 18F-FPA combined with 18F-FDG can be an alternative for detecting HCC. Molecular Imaging 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

Chuang, Hui-Yen; Lee, Yen-Po; Lin, Wei-Chan; Lin, Yi-Hsien; Hwang, Jeng-Jong published the artcile< Fatty Acid Inhibition Sensitizes Androgen-Dependent and -Independent Prostate Cancer to Radiotherapy via FASN/NF-κB Pathway>, HPLC of Formula: 96829-58-2, the main research area is ionizing radiation androgen receptor FASN NFkappaB signaling radiotherapy.

Elevated fatty acid synthase (FASN) has been reported in both androgen-dependent and -independent prostate cancers. Conventional treatment for prostate cancer is radiotherapy (RT); however, the following radiation-induced radioresistance often causes treatment failure. Upstream proteins of FASN such as Akt and NF-κB are found increased in the radioresistant prostate cancer cells. Nevertheless, whether inhibition of FASN could improve RT outcomes and reverse radiosensitivity of prostate cancer cells is still unknown. Here, we hypothesized that orlistat, a FASN inhibitor, could improve RT outcomes in prostate cancer. Orlistat treatment significantly reduced the S phase population in both androgen-dependent and -independent prostate cancer cells. Combination of orlistat and RT significantly decreased NF-κB activity and related downstream proteins in both prostate cancer cells. Combination effect of orlistat and RT was further investigated in both LNCaP and PC3 tumor-bearing mice. Combination treatment showed the best tumor inhibition compared to that of orlistat alone or RT alone. These results suggest that prostate cancer treated by conventional RT could be improved by orlistat via inhibition of FASN.

Scientific Reports published new progress about Androgen receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Pilitsi, Eleni; Farr, Olivia M.; Polyzos, Stergios A.; Perakakis, Nikolaos; Nolen-Doerr, Eric; Papathanasiou, Aimilia-Eirini; Mantzoros, Christos S. published the artcile< Pharmacotherapy of obesity: Available medications and drugs under investigation>, COA of Formula: C29H53NO5, the main research area is adult obesity pharmacol management FDA approved medication drug review; Liraglutide; Lorcaserin; Naltrexone/bupropion; Obesity; Orlistat; Personalized therapy phentermine/topiramate.

A review. Obesity is a chronic disease with a continuously rising prevalence that currently affects more than half a billion people worldwide. Energy balance and appetite are highly regulated via central and peripheral mechanisms, and weight loss triggers a homeostatic response leading to weight regain. Lifestyle and behavioral modifications are the cornerstones of obesity management; however, they often fail to achieve or sustain long-term weight loss. Pharmacotherapy added onto lifestyle modifications results in an addnl., albeit limited, weight reduction Regardless, this weight reduction of 5-10% conveys multiple cardiovascular and metabolic benefits. In this review, evidence on the food and drug administration (FDA)-approved medications, i.e., orlistat, lorcaserin, phentermine/topiramate, liraglutide and naltrexone/bupropion, is summarized. Furthermore, anti-obesity agents in the pipeline for potential future therapeutic use are presented.

Metabolism, Clinical and Experimental published new progress about Pipelines. 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

Tak, Young Jin; Lee, Sang Yeoup published the artcile< Long-Term Efficacy and Safety of Anti-Obesity Treatment: Where Do We Stand?>, 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 drugs; Liraglutide; Naltrexone/bupropion; Orlistat; Phentermine/topiramate; Weight loss medications.

PURPOSE OF REVIEW: As a chronic and relapsing disease, obesity impairs metabolism and causes cardiovascular diseases. Although behavioral modification is important for the treatment of obesity, it is difficult to achieve an ideal weight or sustain the process of long-term weight loss. Therefore, the obesity control guidelines strongly recommend lifestyle interventions along with medical treatment for patients who are overweight. There is sufficient evidence supporting that pharmacotherapy in combination with behavior-based interventions can result in significant weight loss and improved cardiometabolism. RECENT FINDINGS: Recent meta-analyses of new anti-obesity drugs and their weight-loss efficacy have shown that the overall placebo-subtracted weight reduction (%) for at least 12 months ranged from 2.9 to 6.8% for the following drugs: phentermine/topiramate (6.8%), liraglutide (5.4%), naltrexone/bupropion (4.0%), orlistat (2.9%), and lorcaserin (3.1%). However, very recently, on February 13, 2020, the US Food and Drug Administration (FDA) ordered the withdrawal of lorcaserin from markets, as a clinical trial to assess drug safety showed an increased risk of cancer. Currently, the anti-obesity medications that have been approved by the FDA for chronic weight management are orlistat, phentermine/topiramate, naltrexone/bupropion, and liraglutide. However, they are costly and may have adverse effects in some individuals. Therefore, drug therapy should be initiated in obese individuals after weighing its benefits and risks. One of the strategies for long-term obesity control is that anti-obesity medications should be tailored for specific patients depending on their chronic conditions, comorbidities, and preferences.

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, 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

Saleh, Amira; ElFayoumi, Hassan M.; Youns, Mahmoud; Barakat, Waleed published the artcile< Rutin and orlistat produce antitumor effects via antioxidant and apoptotic actions>, Product Details of C29H53NO5, the main research area is rutin orlistat antitumor antioxidant apoptosis; Ehrlich ascites carcinoma; MCF-7; Mice; Orlistat; PANC-1; Rutin.

Cancer is a broad term used to describe a large number of diseases characterized by uncontrolled cell proliferation that leads to tumor production Cancer is associated with mutations in genes controlling proliferation and apoptosis, oxidative stress, fatty acid synthase (FAS) expression, and other mechanisms. Currently, most antineoplastic drugs have severe adverse effects and new effective and safe drugs are needed. This study aims to investigate the possible anticancer activity of rutin and orlistat which are both safely used clin. in humans against two breast cancer models (in vivo EAC and in vitro MCF7) and the pancreatic cancer cell line (PANC-1). Our results have shown that both rutin and orlistat exerted an in vivo anticancer activity as evidenced by the decrease in tumor volume, CEA level, cholesterol content, FAS, and the exerted antioxidant action (reduced MDA level and increased GSH content) and through histopathol. examination In addition, both were cytotoxic to MCF-7 and Panc-1 cell lines by promoting apoptosis. In conclusion, the anticancer activity of rutin and orlistat makes them promising candidates for cancer treatment alone or in combination with other anticancer drugs specially that they are used clin. with an acceptable safety profile.

Naunyn-Schmiedeberg’s Archives of Pharmacology published new progress about Antioxidants Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Chu, Junjun; Xing, Changsheng; Du, Yang; Duan, Tianhao; Liu, Siyao; Zhang, Pengfei; Cheng, Chumeng; Henley, Jill; Liu, Xin; Qian, Chen; Yin, Bingnan; Wang, Helen Yicheng; Wang, Rong-Fu published the artcile< Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication>, Reference of 96829-58-2, the main research area is pharmacol inhibition fatty acid synthesis replication SARSCoV2 COVID19.

Caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), COVID-19 is a virus-induced inflammatory disease of the airways and lungs that leads to severe multi-organ damage and death. Here we show that cellular lipid synthesis is required for SARS-CoV-2 replication and offers an opportunity for pharmacol. intervention. Screening a short-hairpin RNA sublibrary that targets metabolic genes, we identified genes that either inhibit or promote SARS-CoV-2 viral infection, including two key candidate genes, ACACA and FASN, which operate in the same lipid synthesis pathway. We further screened and identified several potent inhibitors of fatty acid synthase (encoded by FASN), including the US Food and Drug Administration-approved anti-obesity drug orlistat, and found that it inhibits in vitro replication of SARS-CoV-2 variants, including more contagious new variants, such as Delta. In a mouse model of SARS-CoV-2 infection (K18-hACE2 transgenic mice), injections of orlistat resulted in lower SARS-CoV-2 viral levels in the lung, reduced lung pathol. and increased mouse survival. Our findings identify fatty acid synthase inhibitors as drug candidates for the prevention and treatment of COVID-19 by inhibiting SARS-CoV-2 replication. Clin. trials are needed to evaluate the efficacy of repurposing fatty acid synthase inhibitors for severe COVID-19 in humans.

Nature Metabolism published new progress about Animal gene Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study) (FASN). 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

Yoo, Euna; Schulze, Christopher J.; Stokes, Barbara H.; Onguka, Ouma; Yeo, Tomas; Mok, Sachel; Gnadig, Nina F.; Zhou, Yani; Kurita, Kenji; Foe, Ian T.; Terrell, Stephanie M.; Boucher, Michael J.; Cieplak, Piotr; Kumpornsin, Krittikorn; Lee, Marcus C. S.; Linington, Roger G.; Long, Jonathan Z.; Uhlemann, Anne-Catrin; Weerapana, Eranthie; Fidock, David A.; Bogyo, Matthew published the artcile< The Antimalarial Natural Product Salinipostin A Identifies Essential α/β Serine Hydrolases Involved in Lipid Metabolism in P. falciparum Parasites>, Application In Synthesis of 96829-58-2, the main research area is Plasmodium falciparum; Salinipostin A; activity-based probes; chemical proteomics; lipid metabolism; malaria; natural products; serine hydrolases.

Salinipostin A (Sal A) is a potent antiplasmodial marine natural product with an undefined mechanism of action. Using a Sal A-derived activity-based probe, we identify its targets in the Plasmodium falciparum parasite. All of the identified proteins contain α/β serine hydrolase domains and several are essential for parasite growth. One of the essential targets displays a high degree of homol. to human monoacylglycerol lipase (MAGL) and is able to process lipid esters including a MAGL acylglyceride substrate. This Sal A target is inhibited by the anti-obesity drug Orlistat, which disrupts lipid metabolism Resistance selections yielded parasites that showed only minor reductions in sensitivity and that acquired mutations in a PRELI domain-containing protein linked to drug resistance in Toxoplasma gondii. This inability to evolve efficient resistance mechanisms combined with the non-essentiality of human homologs makes the serine hydrolases identified here promising antimalarial targets.

Cell Chemical Biology 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

Jin, Bo-Ram; Kim, Hyo-Jung; Sim, Seo-Ah; Lee, Minho; An, Hyo-Jin published the artcile< Anti-Obesity Drug Orlistat Alleviates Western-Diet-Driven Colitis-Associated Colon Cancer via Inhibition of STAT3 and NF-κB-Mediated Signaling>, 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 NF-κB; STAT3; Western diet; azoxymethane (AOM)/dextran sulfate sodium (DSS) model; colitis-associated colon cancer (CAC); orlistat.

Many researchers have argued that Western diet (WD)-induced obesity accelerates inflammation and that inflammation is a link between obesity and colorectal cancer (CRC). This study investigated the effect of WDs on the development and progression of colitis-associated colon cancer (CAC) and the efficacy of the anti-obesity agent orlistat on WD-driven CAC in mice. The results revealed that the WD exacerbated CAC in azoxymethane (AOM)/dextran sulfate sodium (DSS)-induced mice, which showed increased mortality, tumor formation, and aggravation of tumor progression. Furthermore, WD feeding also upregulated inflammation, hyperplasia, and tumorigenicity levels through the activation of STAT3 and NF-κB signaling in an AOM/DSS-induced mouse model. In contrast, treatment with orlistat increased the survival rate and alleviated the symptoms of CAC, including a recovery in colon length and tumor production decreases in WD-driven AOM/DSS-induced mice. Addnl., orlistat inhibited the extent of inflammation, hyperplasia, and tumor progression via the inhibition of STAT3 and NF-κB activation. Treatment with orlistat also suppressed the β-catenin, slug, XIAP, Cdk4, cyclin D, and Bcl-2 protein levels in WD-driven AOM/DSS-induced mice. The results of this study indicate that orlistat alleviates colon cancer promotion in WD-driven CAC mice by suppressing inflammation, especially by inhibiting STAT3 and NF-κB activation.

Cells 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