Category: 96829-58-2

de Almeida, Luciana Y.; Mariano, Flavia S.; Bastos, Debora C.; Cavassani, Karen A.; Raphelson, Janna; Mariano, Vania S.; Agostini, Michelle; Moreira, Fernanda S.; Coletta, Ricardo D.; Mattos-Graner, Renata O.; Graner, Edgard published the artcile< The antimetastatic activity of orlistat is accompanied by an antitumoral immune response in mouse melanoma>, 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 antimetastatic activity antitumoral immune response melanoma; Experimental melanoma; Fatty acid synthase; Immune response; Metastasis; Orlistat.

Our group has previously shown that pharmacol. inhibition of FASN with orlistat decreases proliferation, promotes apoptosis, and reduces the metastatic spread of B16-F10 cells in exptl. models of melanoma. While most of the orlistat antitumor properties seem to be closely related to direct effects on malignant cells, its impact on the host immune system is still unknown. The effects of orlistat on the phenotype and activation status of infiltrating leukocytes in primary tumors and metastatic lymph nodes were assessed using a model of spontaneous melanoma metastasis (B16-F10 cells/C57BL/6 mice). Cells from the primary tumors and lymph nodes were mech. dissociated and immune cells phenotyped by flow cytometry. The expression of IL-12p35, IL-12p40, and inducible nitric oxide synthase (iNOS) was analyzed by qRT-PCR and production of nitrite (NO2-) evaluated in serum samples with the Griess method. Orlistat-treated mice exhibited a 25% reduction in the number of mediastinal lymph node metastases (mean 3.96 ± 0.78, 95% CI 3.63-4.28) compared to the controls (mean 5.7 ± 1.72; 95% CI 5.01-6.43). Taken together, these findings suggest that orlistat supports an antitumor response against exptl. melanomas by increasing CD80/CD81-pos. and IL-12-pos. DC populations, granzyme b/NKG2D-pos. NK populations, and perforin/granzyme b-pos. CD8 T lymphocytes as well as reducing Tregs counts within exptl. melanomas.

Cancer Chemotherapy and Pharmacology published new progress about Antitumor agents. 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

El-Shal, Laila Moustafa; El-Star, Alyaa A. Abd; Azmy, Abeer M.; Elnegris, Heba M. published the artcile< The possible protective role of N-acetyl cysteine on duodenal mucosa of high fat diet and orlistat treated adult male albino rats and the active role of tumor necrosis factor α (TNFα) and Interleukin 6 (IL6) (histological and biochemical study)>, 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 HFD; IL6; N-acetyl cysteine; Orlistat; TNFα; duodenal mucosa.

BackgroundObesity is a major universal health issue linked to a majority of illness. AimTo evaluate the histol. and biochem. changes occurred in the duodenal mucosa of high fat diet HFD and orlistat fed rats and to assess the possible protective role of N-acetyl cysteine NAC supplementation. Material and methodSixty male albino rats weighing 180-200 g were classified randomly into control group I and three exptl. groups (HFD group II, HFD + orlistat group III, and HFD + orlistat + NAC group IV). All exptl. groups received HFD alone/and treatment for 6 wk. Group III received orlistat (32 mg/kg/day) before meals and group IV received the same regimen as group III in addition to NAC (230 mg/kg/day) after meals. After completion of the experiment, duodenal sections were processed for histol. examination, oxidative stress parameters, and semiqualitative real time PCR for proinflammatory mediators TNFα and IL6 evaluation. Also, plasma lipid parameters were assessed and morphometric duodenal results were analyzed statistically. ResultsBy histol. examination of HFD and (HFD + orlistat) groups, we found severe to moderate duodenal structural disturbances, increased goblet cells, collagen fibers, and BAX and iNOS immunostaining. By Biochem. examination, both groups showed increased proinflammatory markers level (TNFα and IL6) with decreased all antioxidant parameters and increased MDA. Moreover, NAC treatment in group IV significantly reduced all structural changes, levels of proinflammatory mediators and increased all antioxidant parameter levels and decreased MDA. ConclusionAll findings elucidated that NAC could be accounted to be a useful drug for protection of duodenal mucosa of HFD and orlistat treated animals.

Ultrastructural Pathology 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

Bakhache, William; Neyret, Aymeric; McKellar, Joe; Clop, Camille; Bernard, Eric; Weger-Lucarelli, James; Briant, Laurence published the artcile< Fatty acid synthase and stearoyl-CoA desaturase-1 are conserved druggable cofactors of Old World Alphavirus genome replication>, SDS of cas: 96829-58-2, the main research area is Chikungunya virus; Fatty acid synthase; Genome replication; Lipid metabolism; Mayaro virus; Stearoyl-CoA desaturase-1.

Chikungunya virus (CHIKV) is a rapidly emerging mosquito-borne RNA virus that causes epidemics of debilitating disease in tropical and sub-tropical regions with autochtonous transmission in regions with temperate climate. Currently, there is no licensed vaccine or specific antiviral drug available against CHIKV infection. In this study, we examine the role, in the CHIKV viral cycle, of fatty acid synthase (FASN) and stearoyl-CoA desaturase (SCD1), two key lipogenic enzymes required for fatty acid production and early desaturation We show that both enzymes and their upstream regulator PI3K are required for optimal CHIKV infection. We demonstrate that pharmacol. manipulation of FASN or SCD1 enzymic activity by non-toxic concentrations of cerulenin or CAY10566 decreases CHIKV genome replication. Interestingly, a similar inhibitory effect was also obtained with Orlistat, an FDA-approved anti-obesity drug that targets FASN activity. These drugs were also effective against Mayaro virus (MAYV), an under-studied arthritogenic Old world Alphavirus endemic in South American countries with potential risk of emergence, urbanization and dispersion to other regions. Altogether, our results identify FASN and SCD1 as conserved druggable cofactors of Alphavirus genome replication and support the broad-spectrum activity of drugs targeting the host fatty acids metabolism

Antiviral Research published new progress about 96829-58-2. 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

Shirai, Kohji; Tanaka, Michitaka; Fujita, Toru; Fujii, Yuka; Shimomasuda, Masatsugu; Sakai, Soichi; Samukawa, Yoshishige published the artcile< Safety of Excessive Visceral Fat Reduction with 52-Week Administration of Lipase Inhibitor Orlistat in Japanese Individuals: A Long Term Clinical 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 visceral fat antiobesity agent; Body weight; Efficacy; Japanese; Lipase inhibitor; Long-term administration; Obesity; Orlistat; Safety; Visceral fat; Waist circumference.

Introduction: Orlistat is an inhibitor of pancreatic lipase and is used as an anti-obesity drug in many countries. However, there are no data available regarding the effects of orlistat on visceral fat (VF) accumulation in Japanese individuals. Therefore, this study aimed to analyze the efficacy and safety of 52 wk of orlistat administration in Japanese individuals. Methods: Orlistat 60 mg was administered orally three times daily for 52 wk to Japanese participants with excessive VF accumulation and without dyslipidemia, diabetes mellitus, and hypertension (metabolic diseases). Participants were also counseled to improve their diet and to maintain exercise habits. We defined excessive VF accumulation as a waist circumference (WC) of ≥ 85 cm for males and ≥ 90 cm for females, which corresponds to a VF area of 100 cm2. Adverse reactions, clin. laboratory tests, VF, WC, body weight (BW), etc., were monitored throughout the study period. Results: VF, WC, and BW were significantly reduced at week 52 from baseline; the mean ± standard error rate of change was – 21.52% ± 1.89%, – 4.89% ± 0.45%, and – 5.36% ± 0.56%, resp., and continued to reduce throughout the 52 wk; these significantly reduced at whole term compared with baseline. Most adverse reactions were defecation-related symptoms such as oily spotting and flatus with discharge (flatus with small amounts of stool or oil) due to the pharmacol. effects of the lipase inhibitor. These symptoms were mostly mild, reversible, and recognizable by the participants; none were serious or severe. No participants discontinued by medical judgment about adverse reactions, and the drug could be administered continuously. Conclusion: VF, WC, and BW were reduced from week 4 to week 52, indicating the effect of long-term orlistat administration. Moreover, it was well tolerated with an acceptable safety profile. Long-term administration of orlistat may be efficacious in reducing VF accumulation with safety when used in combination with diet and exercise. Trial Registration: This study is registered with the Japan Pharmaceutical Information Center (identifier: JapicCTI-184004). Funding: Funding for this study was provided by Taisho Pharmaceutical Co., Ltd.

Advances in Therapy published new progress about Antiobesity agents. 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

Dutta, Deep; Jaisani, Ritu; Khandelwal, Deepak; Ghosh, Soumitra; Malhotra, Rajiv; Kalra, Sanjay published the artcile< Role of metformin, sodium-glucose cotransporter-2 (SGLT2) Inhibitors, glucagon-like peptide-1 (GLP-1) receptor agonists, and orlistat based multidrug therapy in glycemic control, weight loss, and euglycemia in diabesity: a real-world experience>, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is diabetes metformin SGLT2 GLP1 weight loss multi drug therapy; Diabesity; GLP1 receptor agonists; SGLT2 inhibitors; diabetes reversal; metformin; orlistat; weight loss.

Results: In total, 5,336 patient records were screened; 2,442 with prediabetes/diabetes were considered; 1,509 patients who fulfilled all criteria were analyzed. Use of metformin, SGLT2i, sulfonylureas, DPP4i, pioglitazone, orlistat, and GLP1a was 85.35%, 74.95%, 68.32%, 60%, 39.16%, 9.08%, and 4.17%, resp. However, 365, 970, and 104 patients were on one of 4 concerned medications (Group-1; 24.18%), dual MDT (Group-2; 64.28%), and triple/quadruple MDT (Group-3; 6.89%). Metformin with SGLT2i was most commonly used dual MDT (94.12%). Anal. according to weight-loss quartiles from 558 patients showed 6.9 kg weight-loss in the highest quartile. People losing maximum weight were significantly younger; had higher use of metformin, SGLT2i, GLP1, orlistat, and lower pioglitazone use; greatest HbA1c reduction (-1.3 vs. -0.3; quartile-1 vs. quartile -4; P < 0.001); and significantly higher occurrence of HbA1c<5.7% (16.8% vs. 6.29%; quartile-1 vs. 4; P < 0.001). Patients in Group-3 had the highest baseline BMI and maximum weight loss with highest number of patients with HbA1c<5.7% (19.44% vs. 10.34%; Group-3 vs. Group-1; P < 0.001). Conclusion: Greater weight loss with HbA1c reduction along with a greater number of patients attaining HbA1c <5.7% highlights that MDT is the way forward to tackle diabesity in India. Indian Journal of Endocrinology and Metabolism published new progress about Body mass index. 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

Esmail, Vian Ahmed Wasta; Mohammed, Mohammed Omer; Al-Nimer, Marwan S M published the artcile< Short-term orlistat therapy improves fatty infiltration indices and liver fibrosis scores in patients with non-alcoholic fatty liver disease and metabolic syndrome.>, SDS of cas: 96829-58-2, the main research area is Lipid indices; Liver fibrosis scores; Metabolic syndrome; Non-alcoholic fatty liver disease.

BACKGROUND AND STUDY AIMS: Patients with non-alcoholic fatty liver disease (NAFLD) exhibit features of metabolic syndrome, including a high body mass index, central obesity, high blood pressure, and abnormal lipid profile values. Orlistat, an intestinal lipase enzyme inhibitor, improves insulin resistance. We aimed to investigate the effects of short-term therapy with orlistat on the components of metabolic syndrome associated with NAFLD and explore its effect on liver fibrosis scores. PATIENTS AND METHODS: An open-label placebo-controlled clinical study using orlistat for 12 weeks was carried out on 50 patients with NAFLD. They were divided into a placebo group (Group I) and an orlistat treatment group (120 mg per day, Group II). The diagnosis of NAFLD was made by ultrasonography and laboratory investigations. Anthropometric and blood pressure measurements and hepatic liver enzymes, fasting lipids, and blood glucose levels were determined before and after treatment. Lipid indices including cholesterol (Chol-I), triglyceride (TG-I), triglyceride-glucose (TYG-I), and the scores for lipid fibrosis using the NAFLD fibrosis score (NFS) and Fibrosis-4 score (Fib-4) were also determined. RESULTS: Orlistat significantly improved the anthropometric and metabolic indices (TG-I, TYG-I) and liver enzymes. Orlistat demonstrated a favorable impact on the NAS and Fib-4 scores for liver fibrosis. CONCLUSION: Orlistat improves the components of metabolic syndrome, leading to the improvement of insulin resistance and thereby improves fatty infiltration of the liver. To a lesser extent, orlistat improved the liver fibrosis scores.

Arab journal of gastroenterology : the official publication of the Pan-Arab Association of Gastroenterology published new progress about 96829-58-2. 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

Liu, Tengfei; Yu, Junming; Ge, Chao; Zhao, Fangyu; Chen, Jing; Miao, Chunxiao; Jin, Wenjiao; Zhou, Qingqing; Geng, Qin; Lin, Hechun; Tian, Hua; Chen, Taoyang; Xie, Haiyang; Cui, Ying; Yao, Ming; Xiao, Xiuying; Li, Jinjun; Li, Hong published the artcile< Sperm associated antigen 4 promotes SREBP1-mediated de novo lipogenesis via interaction with lamin A/C and contributes to tumor progression in hepatocellular carcinoma>, Reference of 96829-58-2, the main research area is Hepatocellular carcinoma; Lamin A/C; Lipogenesis; SPAG4; SREBP1.

Hepatocellular carcinoma (HCC) is a highly malignant tumor and its progression is associated with altered lipid metabolism in precancerous lesions, such as non-alc. fatty liver disease. Here, we identified sperm associated antigen 4 (SPAG4), and explored its oncogenic role in HCC progression. Database anal. and immunohistochem. indicated increased level of SPAG4 in HCC tissues which was of prognostic value. Gain/loss-of-function experiments showed that SPAG4 exerted oncogenic roles in HCC growth both in vitro and in vivo. RNA sequencing revealed activation of a lipogenic state and SREBP1-mediated pathway following SPAG4 overexpression. Mechanistically, the N-terminal region of SPAG4 bound to lamin A/C, which increased SREBP1 expression, nuclear translocation, and transcriptional activity. Treatment with orlistat, a lipid synthesis inhibitor, reversed SPAG4-mediated oncogenic effects, and its efficacy varied with SPAG4 level. The effect of orlistat was further amplified when combined with sorafenib in tumor xenograft mouse models. Our study provides evidence that SPAG4 mediates HCC progression by affecting lipid metabolism Administration of orlistat combined with sorafenib reverses SPAG4-mediated oncogenesis in HCC cells and ectopic xenograft tumors in mice, suggesting that this pathway represents a potential target for HCC treatment.

Cancer Letters (New York, NY, United States) published new progress about 96829-58-2. 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

Qu, Zhen; Ren, Yuning; Shen, Hongyu; Wang, Huihui; Shi, Lijie; Tong, Deyong published the artcile< Combination Therapy of Metastatic Castration-Recurrent Prostate Cancer: Hyaluronic Acid Decorated, Cabazitaxel-Prodrug and Orlistat Co-Loaded Nano-System.>, Related Products of 96829-58-2, the main research area is cabazitaxel; hyaluronic acid; metastatic castration-recurrent prostate cancer; orlistat; prodrug technology.

PURPOSE: Prostate cancer (PCa) is the second leading cause of cancer-related death among men in developed countries. Cabazitaxel (CBZ) is recommended as one of the most active chemotherapy agents for PCa. This study aimed to develop a hyaluronic acid (HA) decorated, cabazitaxel-prodrug (HA-CBZ) and orlistat (ORL) co-loaded nano-system against the prostate cancer in vitro and in vivo. METHODS: Cabazitaxel-prodrug was firstly synthesized by conjugating HA with CBZ through the formation of ester bonds. HA contained ORL and CBZ prodrug co-loaded lipid-polymer hybrid nanoparticles (ORL/HA-CBZ/LPNs) were constructed and characterized in terms of particle size, zeta potential, drug loading capacity and stability. The antitumor efficiency and systemic toxicity of LPNs were evaluated in vitro and in vivo. RESULTS: The resulting ORL/HA-CBZ/LPNs were 150.9 nm in particle size with narrow distribution and high entrapment efficiency. The minimum combination index of 0.57 was found at a drug ratio of 1:2 (ORL:HA-CBZ, w/w) in the drug co-loaded formulations, indicating the strongest synergism effect. ORL/HA-CBZ/LPNs demonstrated an enhanced in vitro and in vivo antitumor effect compared with single drug loaded LPNs and free drug formulations. CONCLUSION: ORL/HA-CBZ/LPNs showed remarkable synergism cytotoxicity and the best tumor inhibition efficiency in mice with negligible systemic toxicity. ORL/HA-CBZ/LPNs can be highly useful for targeted prostate cancer therapy.

Drug design, development and therapy published new progress about 96829-58-2. 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

Suleiman, Joseph Bagi; Nna, Victor Udo; Othman, Zaidatul Akmal; Zakaria, Zaida; Bakar, Ainul Bahiyah Abu; Mohamed, Mahaneem published the artcile< Orlistat attenuates obesity-induced decline in steroidogenesis and spermatogenesis by up-regulating steroidogenic genes>, Computed Properties of 96829-58-2, the main research area is orlistat spermatogenesis steroidogenesis epididymal malondialdehyde; DNA fragmentation; high-fat diet; obesity; orlistat; spermatogenesis; steroidogenesis.

We explored the possible preventive/therapeutic effects of orlistat (a medication prescribed for weight loss) on obesity-induced steroidogenesis and spermatogenesis decline. Twenty-four adult male Sprague Dawley rats weighing 250-300 g were randomized into four groups (n = 6/group), namely; normal control, high-fat diet, high-fat diet plus orlistat preventive group and high-fat diet plus orlistat treatment group. Orlistat was either concurrently administered with high-fat diet for 12 wk or administered from week 7-12 post- high-fat diet feeding. Obesity increased serum leptin and decreased adiponectin levels, decreased serum and intra-testicular levels of FSH, luteinising hormone and testosterone, sperm count, motility, viability, normal morphol. and epididymal antioxidants, but increased epididymal malondialdehyde level and sperm nDNA fragmentation. Further, the levels of steroidogenic acute regulatory protein protein and enzymic activities of CYP11A1, 3β-hydroxysteroid dehydrogenase and 17β-hydroxysteroid dehydrogenase were also significantly decreased in the testes of the high-fat diet group. Orlistat attenuated impaired spermatogenesis and steroidogenesis decline by up-regulating steroidogenic genes. This may not be unconnected to its significant effect in lowering serum leptin levels, since the hormone is known to dampen fertility potential. Therefore, orlistat may improve fertility potential in overweight/obese men.

Andrology 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, Computed Properties of 96829-58-2.

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

Marques-Vidal, Pedro published the artcile< Comparison of lifestyle changes and pharmacological treatment on cardiovascular risk factors>, Reference of 96829-58-2, the main research area is cardiovascular disease dyslipidemia diabetes hypertension LDL HDL orlistat glucose; diabetes; hypertension; lipoproteins and hyperlipidaemia; smoking cessation.

Cardiovascular disease is the leading cause of morbidity mortality in Europe and world wide. The major modifiable risk afactors are Obesity, Hypertension, Smoking, Dyslipidemia and Diabetes. In this paper, we will make a overview of the effect of life style changes on CVD rik factors and compare them with the effect of pharmacoogical treatment. Weight loss led to a consistent reduction in BP level, smoking cessation leads to an increase in BP levels. Potassium supplementation in Hypertensive subjects decreases BP levels. Any weight loss decreased low-d. lipoprotein(LDL)-cholesterol but had no effect on triglycerides. Drug induced weight loss led to a slight decrease in lipid levels, Orlistat exerting a stronger effect than other drugs. Weight loss decreased both plasma glucose and HbA1c. The risk factors of diabetes increased in the first 3 years after smoking cessation. A low-carbohydrate diet reduced HbA1c together with SBP and triglyceride levels, while increasing HDL-cholesterol levels in patients with diabetes. Adequately implemented, changes in lIfestyle acheive reductions in cardiovascular risk factors close to those of single-drug therapies.

Heart (London, United Kingdom) published new progress about Blood triglycerides Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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