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sitagliptin in patients with non-alcoholic steatohepatitis: A randomized, placebo-controlled trial

World Journal of Gastroenterology 2017年第1期23卷 141-150页

作者： Tisha R Joy Charles A McKenzie Rommel G Tirona Kelly Summers Shannon Seney Subrata Chakrabarti Neel Malhotra Melanie D Beaton Department of Medicine Division of EndocrinologySt.Joseph’s HospitalWestern University Department of Medical Biophysics Western University Department of Physiology and Pharmacology Western University Department of Microbiology and Immunology Western University Department of Pathology and Laboratory Medicine Western University Department of Medicine Division of GastroenterologyLondon Health Sciences CentreWestern University

AIMTo evaluate the effect of sitagliptin vs placebo on histologic and non-histologic parameters of non-alcoholic steatohepatitis (NASH).METHODSTwelve patients with biopsy-proven NASH were randomized to sitagliptin (100 mg daily) (n = 6) or placebo (n = 6) for 24 wk. The primary outcome was improvement in liver fibrosis after 24 wk. Secondary outcomes included evaluation of changes in NAFLD activity score (NAS), individual components of NAS (hepatocyte ballooning, lobular inflammation, and steatosis), glycemic control and insulin resistance [including measurements of glycated hemoglobin (HbA1C) and adipocytokines], lipid profile including free fatty acids, adipose distribution measured using magnetic resonance imaging (MRI), and thrombosis markers (platelet aggregation and plasminogen activator inhibitor 1 levels). We also sought to determine the correlation between changes in hepatic fat fraction (%) [as measured using the Iterative Decomposition of water and fat with Echo Asymmetry and Least-squares estimation (IDEAL) MRI technique] and changes in hepatic steatosis on liver *** was not significantly better than placebo at reducing liver fibrosis score as measured on liver biopsy (mean difference between sitagliptin and placebo arms, 0.40, P = 0.82). There were no significant improvements evident with the use of sitagliptin vs placebo for the secondary histologic outcomes of NAS total score as well as for the individual components of NAS. Compared to baseline, those patients who received sitagliptin demonstrated improved HbA1C (6.7% ± 0.4% vs 7.9% ± 1.0%, P = 0.02), and trended towards improved adiponectin levels (4.7 ± 3.5 μg/mL vs 3.9 ± 2.7 μg/mL, P = 0.06) and triglyceride levels (1.26 ± 0.43 mmol/L vs 2.80 ± 1.64 mmol/L, P = 0.08). However, when compared with placebo, sitagliptin did not cause a statistically significant improvement in HbA1C (mean difference, -0.7%, P = 0.19) n

关键词： sitagliptin Randomized controlled trial Non-alcoholic fatty liver disease Non-alcoholic steatohepatitis Fibrosis Magnetic resonance imaging Hepatic steatosis Insulin resistance Platelet aggregation

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A practical synthesis of trifluorophenyl R-amino acid:The key precursor for the new anti-diabetic drug sitagliptin

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Chinese Chemical Letters 2009年第12期20卷 1397-1399页

作者： Li Li Zeng Ying Jie Ding Gui Cheng Zhang Hong Rui Song Wen Hui Hu Laboratory of Anti-diabetic Drug Discovery Center for Synthetic and Natural Drugs Guangzhou Institute of Biomedicine and Health Chinese Academy of Sciences Guangzhou 510663 China The School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 China

sitagliptin is the first new anti-diabetic drug in DPP-Ⅳ inhibitor class. The general synthesis of sitagliptin is by coupling of the β-amino acid fragment with the heterocycle fragment. Though the specific β-amino acid can be easily made from the corresponding R-amino acid by Arndt-Eistert hornologation, the optically pure precursor R-amino acid is difficult to prepare. We herein reported a practical protocol to make the trifluorophenyl substituted R-amino acid 4 in 〉99.9% ee and 40.3% yield by the enzymatic resolution employing enantioselective hydrolysis and a general separation procedure. This protocol requires only cheap starting materials and friendly reaction condition. The procedure not only allows people to prepare the drug substance, but also provides an alternative method for prepareing the rare α-amino acid and the subsequent β-amino acid.

关键词： sitagliptin β-Amino acid DPP-Ⅳ inhibitor Practical synthesis

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Efficacy of sitagliptin on Nonalcoholic Fatty Liver Disease in High-fat-diet-fed Diabetic Mice

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Current Medical Science 2022年第3期42卷 513-519页

作者： Shu-tong ZHOU Wen CUI Li KONG Xun YANG Department of Gastroenterology Beijing Friendship HospitalCapital Medical UniversityBeijing100050China Department of Cardiology Fuwai HospitalChinese Academy of Medical SciencesBeijing 100037China Department of Quality Management Zhumadian Central HospitalHuanghuai UniversityZhumadian 463000China

Objective Nonalcoholic fatty liver disease(NAFLD)is a common cause of clinical liver dysfunction and an important prepathological change of liver *** obesity,type 2 diabetes mellitus,dyslipidemia,and metabolic syndrome are the major risk factors for ***(Sig)is a novel hypoglycemic agent that improves blood glucose levels by increasing the level of active *** has been shown to prevent the development of fatty livers in mice on a fructose-rich *** purpose of this study was to observe the efficacy of Sig on NAFLD in type 2 diabetic *** The diet-induced obesity mouse model was established,and the diabetic mice were screened by an intraperitoneal glucose tolerance *** mice were randomly divided into four groups for 8 weeks of intervention:high-fat diet(HFD)group,Sig group,metformin(Met)group,and Sig+Met *** the intervention,the liver function indexes as well as the blood glucose and blood lipid levels of the mice were *** addition,the wet weight of the liver was measured;the pathological sections of the liver tissues were stained to observe the hepatocyte fatty degeneration,inflammation,necrosis,and fibrosis;and the hepatic histological injury was recorded as the NAFLD activity score(NAS).Results Compared with the normal control group,the body weight,liver weight,blood glucose level,insulin resistance(IR),blood lipid level,and transaminase level of the mice in the HFD group were significantly increased,showing typical metabolic *** treatment with Sig and/or Met,the mice gained less weight,had lower levels of blood glucose,triglyceride(TG),low-density lipoprotein cholesterol(LDL-C),and transaminase,and had improved IR compared with the HFD *** liver pathological NASs in the Sig group(P=0.01),Met group(P=0.028),and Sig+Met group(P<0.001)were lower than those in the HFD group(P<0.05),suggesting that the use of the two drugs alone or in combination can improve the state of liver inflamm

关键词： nonalcoholic fatty liver disease sitagliptin insulin resistance nonalcoholic fatty liver disease activity score

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Anti-cancer effects of sitagliptin,vildagliptin,and exendin-4 on triple-negative breast cancer cells via mitochondrial modulation

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BIOCELL 2022年第12期46卷 2645-2657页

作者： POOJA JAISWAL VERSHA TRIPATHI ANSHUL ASSAIYA DHARMENDRA KASHYAP RAHUL DUBEY ANAMIKA SINGH JANESH KUMAR HEM CHANDRA JHA RAJESH SHARMA AMIT KUMAR DIXIT HAMENDRA SINGH PARMAR School of Biotechnology Devi Ahilya UniversityIndore452001India Laboratory of Membrane Protein Biology National Centre for Cell SciencePune411007India Department of Biosciences and Biomedical Engineering Indian Institute of TechnologyIndore452020India Department of Biotechnology IPS AcademyIndore452012India School of Pharmacy Devi Ahilya UniversityIndore452001India Central Council for Research in Ayurvedic Sciences Kolkata263645India

Triple-negative breast cancer(TNBC)cell line MDA-MB-231 is known for Warburg metabolism and defects in *** the other hand,dipeptidyl peptidase-IV(DPP-IV)inhibitors such as sitagliptin and vildagliptin and GLP-1 agonist exendin-4 are known to improve mitochondrial functions as well as biogenesis,but no study has evaluated the influence of these drugs on mitochondrial biogenesis on metastatic breast cancer cell *** have recently reported anticancer effects of 5-aminoimidazole-4-carboxamide riboside on MDA-MB-231 cells via activation of AMP-dependent kinase(AMPK),which activates the downstream transcription factors PGC-1α,PGC-1β,or FOXO1 for mitochondrial biogenesis;above-mentioned incretin-based therapies are also known to activate *** study evaluated the effects of sitagliptin,vildagliptin,and exendin-4 on MDA-MB-231 cells and the underlying changes in mitochondrial biogenesis,were *** with sitagliptin(100μM),vildagliptin(100μM),and exendin-4(10 nM)for 72 h to MDA-MB-231 cells led to a decrease in viability indicated by MTT assay,cell migration by scratch,and transwell migration assays,accompanied with marginal reduction in cell numbers along with the apoptotic appearance,the rate of apoptosis,and decreased lactate content in conditioned *** changes in the cancer phenotype were accompanied by an increase in the mitochondrial DNA to nuclear DNA ratio,increased MitoTracker green and red staining,and increased expression of transcription factors PGC-1α,NRF-1,NRF-2,TFAM,and ***-treatment of cells with these incretin-based drugs followed by 48 h treatment with 1μM doxorubicin increased doxorubicin sensitivity as observed by a decrease in viability by MTT ***,sitagliptin,vildagliptin,and exendin-4 exert their beneficial effects on TNBC cells via an increase in mitochondrial biogenesis that helps to switch Warburg metabolism into anti-Warburg *** response was in the order of:sitagliptin>vildagliptin>ex

关键词： sitagliptin Vildagliptin Exendin-4 Apoptosis Migration Viability Chemo-sensitivity Mitochondrial biogenesis

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Changes of adipocytokine expression after diabetic rats received sitagliptin and the molecular mechanism

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Asian Pacific Journal of Tropical Medicine 2016年第9期9卷 872-875页

作者： Qiao-Min Wu Hai-Xiang Ni Xiao Lu Endocrinology Department First Affiliated Hospital of Zhejiang Chinese Medical University Zhejiang Chinese Medical University

Objective:To study the effect of sitagliptin on adipocytokines expression in diabetic rats and its molecular ***:Male SD rats were chosen and randomly divided into NC group,T2DM group,SP group and SP+LY *** group received conventional breeding,T2DM group,SP group and SP+LY group received intraperitoneal injection of streptozotocin after 12 weeks of high-fat diet to establish diabetes animal model,SP group received sitagliptin intervention and SP+LY group received sitagliptin combined with PI3 K inhibitor LY294002 intervention.6 weeks after the intervention,serum was collected to determine the levels of biochemical indexes and adipocytokines,and visceral adipose tissue was collected to determine expression levels of ***:Serum TC,TG,LDL-C,FBG,FINS,Leptin and Chemerin levels as well as HOMA-IR of T2DM group were higher than those of NC group,and HDL-C,Adiponectin and Omentin-1 levels were significantly lower than those of NC group; serum TC,TG,LDL-C,FBG,FINS,Leptin and Chemerin levels as well as HOMA-IR of SP group were lower than those of T2DM group,and HDL-C,Adiponectin and Omentin-1 levels were significantly higher than those of T2DM group; Leptin and Chemerin levels in serum and visceral adipose tissue of SP+LY group were higher than those of SP group while Adiponectin and Omentin-1 levels were significantly lower than those of SP ***:sitagliptin can regulate the expression of adipocytokines in adipose tissue of diabetic rats through PI3K-AKT pathway.

关键词： Diabetes mellitus sitagliptin Adipocytokines Phosphatidylcholine 3-kinase

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Effect of sitagliptin combined with Yiqi yangyin huoxue decoction on clinical efficacy and hemorheology in early diabetic nephropathy

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World Journal of Diabetes 2023年第9期14卷 1412-1421页

作者： Jun Ling Yan-Hua Yang Department of Pharmacy Changzhou Geriatric Hospital Affiliated to Soochow UniversityChangzhou NO.7 People’s HospitalChangzhou 213000Jiangsu ProvinceChina

BACKGROUND Early diabetic nephropathy(DN)is a complication of diabetes *** mainly affects kidney microvessels and glomerular function,and its timely and effective treatment is critical for early ***,the effects of treatments comprising simple Western medicine are not *** the promotion and implementation of integrated Chinese and western medicine treatments,remarkable results have been achieved for many *** this end,we explored the clinical efficacy of integrated traditional Chinese and western medicines for the treatment of early *** To investigate the effect of sitagliptin tablets combined with Yiqi yangyin huoxue decoction on clinical efficacy and hemorheology in patients with early *** Through a retrospective analysis,123 patients with early DN were admitted to the endocrinology clinic of the Changzhou NO.7 People’s Hospital from January 2021 to October 2022 and were selected as study *** rigorous screening,100 patients with early DN were *** control group(CG,n=50)and the observation group(OG,n=50)were divided according to the treatment *** CG were treated with sitagliptin,and the OG were treated with sitagliptin plus the Yiqi yangyin huoxue *** groups were treated for 3 *** both groups,the baseline data and clinical efficacy were compared,and changes in blood glucose levels,lipid levels,renal function,and hematological indicators before(T0)and after(T1)treatment were *** The total effective rate for the OG was 94.00%and that of the CG was 80.00%(P<0.05).After treatment(T1),the levels of fasting blood glucose,2 h postprandial glucose,total cholesterol,triacylglycerol,and low-density lipoprotein cholesterol in OG patients were obviously lower than those in the CG(P<0.05),and cystatin C,homocysteine,urinary microalbumin,and blood creatinine values in OG patients were also obviously lower than those in the CG(P<0.05);erythrocyte deposition,plasma viscosity,whole blood hig

关键词： sitagliptin Yiqi yangyin huoxue decoction Early diabetic nephropathy Renal function Clinical effects Hemorheology

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sitagliptin improves vascular endothelial function in Japanese type 2 diabetes patients without cardiovascular disease

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Journal of Diabetes Mellitus 2012年第3期2卷 338-345页

作者： Kazunari Suzuki Kentaro Watanabe Tatsuya Suzuki Motoshi Ouchi Shoko Futami-Suda Yoshimasa Igari Hiroshi Nakano Kenzo Oba Department of Internal Medicine (Divisions of Cardiology Hepatology Geriatrics and Integrated Medicine) Nippon Medical School Tokyo Japan

We evaluated the effect of sitagliptin on vascular endothelial function in Japanese type 2 diabetes patients without cardiovascular disease. Subjects included 24 Japanese type 2 diabetes patients without cardiovascular disease. This study was a prospective, open-label, randomized clinical trial. We divided the study subjects into 2 groups: subjects who received sitagliptin 50 mg daily (sitagliptin group, n = 12) and subjects who did not receive sitagliptin (control group, n = 12). Brachial artery flow-mediated dilation (FMD) was measured after overnight fasting. sitagliptin administration was initiated at 1 month after enrollment in study (baseline). FMD and level of biochemical variables in the sitagliptin and control groups were measured at baseline and 3 months from baseline (3 months). We evaluated the effect of sitagliptin on vascular endothelial function by measuring FMD. FMD at 3 months was significantly higher in the sitagliptin group than in the control group (5.36% ± 2.18% vs 3.41% ± 2.29%, P = 0.040), while FMD at baseline was not significantly different between the 2 groups. In addition, FMD of the sitagliptin group at 3 months was significantly higher than that at baseline (5.36% ± 2.18% vs 3.67% ± 2.30%, P = 0.004), while no significant differences were observed in the FMD of the control group during the study period. The change in the adiponectin from baseline to 3 months was significantly higher in the sitagliptin group than that in the control group (0.82 ± 2.18 μg/mL vs 0.01 ± 0.55 μg/mL, P = 0.039). sitagliptin improves vascular endothelial function of the brachial artery in Japanese type 2 diabetes patients without cardiovascular disease. Furthermore, elevation of adiponectin may induce reduction of endothelial dysfunction in type 2 diabetes patients treated with sitagliptin.

关键词： sitagliptin Endothelial Function Flow-Mediated Dilation Type 2 Diabetes Mellitus Adiponectin

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sitagliptin for Elderly Patients Aged 75 Years or Older with Inadequately Controlled Type 2 Diabetes with Common Antidiabetes Treatments

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International Journal of Clinical Medicine 2015年第9期6卷 672-681页

作者： Katsunori Suzuki Yurie Mistuma Takaaki Sato Mariko Hatta Division of Endocrinology and Metabolism Saiseikai Niigata Daini Hospital Niigata Japan Department of Nutrition Saiseikai Niigata Daini Hospital Niigata Japan

Background: The purpose of this study was to evaluate the effects of sitagliptin in elderly patients with type 2 diabetes aged 75 years or older versus those aged 65 - 74 years. Methods: Outpatients aged 65 years or older with type 2 diabetes who received sitagliptin at a dose of 50 mg daily for 6 months were divided into two groups: those who were 75 years and older and those who were 65 - 74 years. The efficacy and safety were retrospectively evaluated by comparison of laboratory values before and after the administration of sitagliptin and by review of adverse events after treatment. Results: One hundred and twelve older patients with type 2 diabetes were studied. Six months after the initiation of sitagliptin, participants’ hemoglobin A1c was significantly decreased by 1.09% ± 0.8% in 65 - 74-year-olds (66 patients;mean age, 69.1 ± 3.0 years;mean HbA1c before administration, 8.4% ± 0.8%) and by 1.05% ± 0.8% in patients 75 years or older (46 patients;mean age, 79.8 ± 4.1 years;mean HbA1c before administration, 8.5% ± 0.7%). There was no significant difference in hemoglobin A1c between the two groups. Furthermore, sitagliptin was well tolerated in both age groups. Conclusions: In elderly patients (75 years or older) with type 2 diabetes, the effect of sitagliptin was similar that in older patients (younger than 75 years) with type 2 diabetes.

关键词： Elderly sitagliptin Type 2 Diabetes Mellitus

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sitagliptin counteracts seasonal fluctuation of glycemic control

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World Journal of Diabetes 2012年第6期3卷 118-122页

作者： Tomohiro Matsuhashi Motoaki Sano Keiichi Fukuda Shun Kohsaka Yoshihiko Suzuki Department of Cardiology Keio University School of MedicineTokyo 160-8582Japan Division of Cardiovascular Inflammation Department of MedicineKeio University School of MedicineTokyo 160-8582Japan HDC Atlas Clinic Tokyo 102-0082Japan

AIM:To assess the effect of sitagliptin therapy on seasonal fluctuation of glycemic control in Japanese type 2 diabetic ***:Participating patients(age:29-80 years) had been treated with conventional oral antidiabetic agents and/or diet and exercise therapy for over 6 *** December 2009,35 patients were additionally prescribed oral sitagliptin starting from 50 mg once daily,while 19 patients taking-glucosidase inhibitors were switched to ***-four patients who refused sitagliptin formed the control *** of mean monthly hemoglobin A 1c(HbA 1c) during the "winter holiday season" were compared between groups using Student's t-test(2008-2009 vs 2009-2010).Statistical significance was accepted at P sitagliptin use was associated with deterioration or improvement of glycemic ***:Both add-on sitagliptin and switching from-glucosidase inhibitors to sitagliptin prevented the seasonal deterioration of glycemic control and tended to improve HbA *** analysis revealed that both adding and switching to sitagliptin were negatively correlated with deterioration of glycemic *** 44 patients who continued sitagliptin therapy for another year,elevation of HbA 1c was suppressed without adverse ***:sitagliptin is a suitable oral agent for preventing deterioration of glycemic control during the winter holiday season.

关键词： Type 2 diabetes mellitus Dipeptidyl-peptidase 4 inhibitors sitagliptin Seasonal variation Hemoglobin A 1c

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sitagliptin,sitagliptin and metformin,or sitagliptin and amitriptyline attenuate streptozotocin-nicotinamide induced diabetic neuropathy in rats

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The Journal of Biomedical Research 2012年第3期26卷 200-210页

作者： Ashish Kumar Sharma Akash Sharma Rita Kumari Kunal Kishore Divya Sharma Bharthu Parthsarthi Srinivasan Ashok Sharma Santosh Kumar Singh Samir Gaur Vijay Singh Jatav Prashant Sharma Varnika Srivastava Sneha Joshi Megha Joshi Prashant Kumar Dhakad Davender Singh Kanawat Akanksha Mishra Anil Sharma Dharmendra Singh Ravinder Pal Singh Himmat Singh Chawda Rambir Singh Sachin Kumar Raikwar Muneem Kumar Kurmi Pankaj Khatri Ashutosh Agarwal Arshee Munajjam Department of Pharmacology Gyan Vihar School of PharmacySuresh Gyan Vihar UniversityJagatpuraJaipur(Rajasthan)302025India Department of Pharmacology Delhi Institute of Pharmaceutical Sciences&ResearchPushpviharNew Delhi 110017India Department of Pharmacology Kota Collage of PharmacyRIICO Industrial AreaRanpurKota(Rajasthan)Pincode 302025India

Diabetic neuropathies are a family of nerve disorders caused by diabetes. Symptoms of the disease include nerve palsy, mononeuropathy, mononeuropathy multiplex, diabetic amyotrophy, painful polyneuropathy, autonomic neu- ropathy, and thoracoabdominal neuropathy. In this study, type 2 diabetes in rats was induced with nicotinamide- streptozotocin. Drug treatment was initiated on the d 15, with the combination regimen of metformin, pioglitazone and glimipiride or metformin and sitagliptin or sitagliptin, amitriptyline and sitagliptin and led to significantly im- proved glycemic control, increased grip strength and paw jumping response on d 21, 28 and 35 （P 〈 0.001）. Signif- icant increases in blood protein levels and decreases in urinary protein levels were observed in the animals treated with the different regimens on d 21, 28 and 35 （P 〈 0.001）. Combined treatment of streptozotocin and nicotinamide caused marked degeneration of nerve cells, while administration of metformin and sitagliptin showed tissue regen- eration and no body weight gain. In conclusion, treatment with sitagliptin and sitagliptin combined with metformin or amitriptyline results in no body weight gain, but causes an increase in grip strength and pain sensitivity, exhibits neural protection, and reverses the alteration of biochemical parameters in rats with streptozotocin-nicotinamide induced type 2 diabetes.

关键词： diabetic neuropathy nicotinamide-streptozotocin metformin pioglitazone glimipiride sitagliptin amitriptyline

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