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telmisartan

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https://www.readbyqxmd.com/read/29048654/telmisartan-inhibits-hepatocellular-carcinoma-cell-proliferation-in-vitro-by-inducing-cell-cycle-arrest
#1
Kyoko Oura, Tomoko Tadokoro, Shintaro Fujihara, Asahiro Morishita, Taiga Chiyo, Eri Samukawa, Yoshimi Yamana, Koji Fujita, Teppei Sakamoto, Takako Nomura, Hirohito Yoneyama, Hideki Kobara, Hirohito Mori, Hisakazu Iwama, Keiichi Okano, Yasuyuki Suzuki, Tsutomu Masaki
Hepatocellular carcinoma (HCC) is the most common primary malignancy of the liver and the third leading cause of cancer-related death. Telmisartan, a widely used antihypertensive drug, is an angiotensin II type 1 (AT1) receptor blocker (ARB) that might inhibit cancer cell proliferation, but the mechanisms through which telmisartan affects various cancers remain unknown. The aim of the present study was to evaluate the effects of telmisartan on human HCC and to assess the expression of microRNAs (miRNAs). We studied the effects of telmisartan on HCC cells using the HLF, HLE, HepG2, HuH-7 and PLC/PRF/5 cell lines...
September 20, 2017: Oncology Reports
https://www.readbyqxmd.com/read/29031980/quality-by-design-qbd-approach-to-optimize-the-formulation-of-a-bilayer-combination-tablet-telmiduo-%C3%A2-manufactured-via-high-shear-wet-granulation
#2
Ah Ram Lee, Seok Young Kwon, Du Hyung Choi, Eun Seok Park
A bilayer tablet, which consisted of telmisartan and amlodipine besylate, was formulated based on a Quality by Design (QbD) approach. The control and response factors were determined based on primary knowledge and the target values of the control tablet (Twynsta(®)). A D-optimal mixture design was used to obtain the optimal formulations in terms of D-mannitol, crospovidone, and MCC for the telmisartan layer, and CCM-Na, PVP K25, and Prosolv for the amlodipine layer. The quantitative effects of the different formulation factors on the response factors were accurately predicted using the equations of best fit and a strong linearity was observed between the predicted and actual values of the response factors...
October 12, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28979698/stachydrine-ameliorates-pressure-overload-induced-diastolic-heart-failure-by-suppressing-myocardial-fibrosis
#3
Hui-Hua Chen, Pei Zhao, Wen-Xia Zhao, Jing Tian, Wei Guo, Ming Xu, Chen Zhang, Rong Lu
Stachydrine (Sta), a major constituent of Leonurus japonicus Houtt, has been reported to possess numerous cardioprotective effects. In this study, we evaluated the effect of Sta on pressure overload-induced diastolic heart failure in rats and investigated the mechanisms underlying the effect. Wistar rats were randomized to transverse aortic constriction (TAC) or sham operation. After 3 days, the rats that underwent TAC were randomized to treatment for a total of four experimental groups (n=10 each group): sham operation, TAC only, TAC + telmisartan (Tel), and TAC + stachydrine (Sta)...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28974567/relative-and-combined-prognostic-importance-of-on-treatment-mean-and-visit-to-visit-blood-pressure-variability-in-ontarget-and-transcend-patients
#4
RANDOMIZED CONTROLLED TRIAL
Giuseppe Mancia, Helmut Schumacher, Michael Böhm, Josep Redon, Roland E Schmieder, Paolo Verdecchia, Peter Sleight, Koon Teo, Salim Yusuf
In 28 790 patients recruited for the ONTARGET (Ongoing Treatment Alone and in Combination With Ramipril Global End Point Trials) and TRANSCEND (Telmisartan Randomized Assessment Study in ACE Intolerant Subjects With Cardiovascular Disease) trials, we investigated the prognostic value for cardiovascular events (primary outcome) of (1)on-treatment visit-to-visit systolic blood pressure (SBP) variability versus mean SBP and (2) the 2 measures together. SBP variability was measured by the coefficient of variation (CV) of mean SBP to which it was unrelated...
November 2017: Hypertension
https://www.readbyqxmd.com/read/28962213/effects-of-telmisartan-on-improving-leptin-resistance-and-inhibiting-hepatic-fibrosis-in-rats-with-non-alcoholic-fatty-liver-disease
#5
Qiu-Zan Zhang, Ying-Li Liu, Yan-Rong Wang, Li-Na Fu, Jing Zhang, Xiu-Ru Wang, Bang-Mao Wang
The present study aimed to investigate the impacts of telmisartan (TEL) on hepatic fibrosis, serum leptin, leptin protein in liver tissue and its mRNA expression level in rats with non-alcoholic fatty liver disease (NAFLD). Male Sprague Dawley rats were randomly divided into the control (N), model (M), polyene phosphatidylcholine (P) and TEL (T) groups. Group M and the intervention groups were given a high-fat diet for 12 weeks to induce NAFLD, followed by 4 weeks of intragastric administration of normal saline (1...
September 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28955302/temporal-changes-in-cortical-and-hippocampal-expression-of-genes-important-for-brain-glucose-metabolism-following-controlled-cortical-impact-injury-in-mice
#6
June Zhou, Mark P Burns, Linda Huynh, Sonia Villapol, Daniel D Taub, Juan M Saavedra, Marc R Blackman
Traumatic brain injury (TBI) causes transient increases and subsequent decreases in brain glucose utilization. The underlying molecular pathways are orchestrated processes and poorly understood. In the current study, we determined temporal changes in cortical and hippocampal expression of genes important for brain glucose/lactate metabolism and the effect of a known neuroprotective drug telmisartan on the expression of these genes after experimental TBI. Adult male C57BL/6J mice (n = 6/group) underwent sham or unilateral controlled cortical impact (CCI) injury...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28933256/combined-effect-of-telmisartan-and-fluvastatin-on-arachidonic-acid-metabolism-in-human-liver-microsomes
#7
Yuka Kato, Yuji Mukai, Anders Rane, Nobuo Inotsume, Takaki Toda
Epoxyeicosatrienoic acids (EETs), metabolites of arachidonic acid (AA) via cytochrome P450s, have a protective effect on the cardiovascular system involving vasodilation. We have previously demonstrated that telmisartan (TEL) inhibits EETs production from AA in vitro. The objectives of the study were to examine the inhibitory effect of fluvastatin (FLU), an inhibitor of CYP2C9, and the combined effect of TEL and FLU on the production of EETs using human liver microsomes. The combined effect of TEL and FLU was evaluated using two methods, the fixed concentration method and the fixed ratio method...
September 21, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28904053/cardiovascular-biomarkers-in-hypertensive-patients-with-medical-treatment-results-from-the-randomized-teamsta-protect-i-trial
#8
Annika Jagodzinski, Johannes Tobias Neumann, Francisco Ojeda, Nils Arne Sörensen, Philipp Wild, Thomas Münzel, Tanja Zeller, Dirk Westermann, Stefan Blankenberg
BACKGROUND: High blood pressure (BP) is associated with an increased rate of cardiovascular events and mortality. Cardiovascular biomarkers are able to predict long-term risk in the general population, particularly in diseased cohorts. We undertook an investigation of the effect of 2 different antihypertensive treatments on cardiovascular biomarkers in a randomized trial. METHODS: The TEAMSTA study included 481 hypertensive patients. They were randomized to either 80-mg telmisartan + 5-mg amlodipine (TA) or 40-mg olmesartan + 12...
September 13, 2017: Clinical Chemistry
https://www.readbyqxmd.com/read/28868047/in-premature-newborns-intraventricular-hemorrhage-causes-cerebral-vasospasm-and-associated-neurodisability-via-heme-induced-inflammasome-mediated-interleukin-1-production-and-nitric-oxide-depletion
#9
Michael Eisenhut, Samyami Choudhury
BACKGROUND: Intraventricular hemorrhage (IVH) occurs in 60-70% of neonates weighing 500-750 g and 10-20% of those weighing 1,000-1,500 g. All forms of IVH have been associated with neurocognitive deficits. Both subarachnoid and IVHs have been associated with delayed vasospasm leading to neurological deficits. Pathways linking hemoglobin release from blood clots to vasospasm include heme-induced activation of inflammasomes releasing interleukin-1 (IL-1) that can cause calcium dependent and independent vasospasm...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28867723/the-inhibitory-effect-of-telmisartan-on-the-metabolism-of-arachidonic-acid-by-cyp2c9-and-cyp2c8-an-in-vitro-study
#10
Yuka Kato, Yuji Mukai, Anders Rane, Nobuo Inotsume, Takaki Toda
Epoxyeicosatorienoic acids (EETs) are generated from arachidonic acid (AA) by CYPs. EETs comprise four regioisomers (14,15-, 11,12-, 8,9-, and 5,6-EET). EETs show potent physiological effects, including vasodilation, anti-inflammation, myocardial preconditioning, and anti-platelet aggregation effects. We recently demonstrated that telmisartan, one of angiotensin II receptor blockers, inhibits AA metabolism by CYP enzymes, including CYP2C8, CYP2C9, and CYP2J2. We conducted studies of AA metabolism using recombinant CYP enzymes to estimate the inhibition constant and the type of inhibition by telmisartan of CYP2C9 and CYP2C8...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28865366/buyanghuanwu-decoction-alleviated-pressure-overload-induced-cardiac-remodeling-by-suppressing-tgf-%C3%AE-smads-and-mapks-signaling-activated-fibrosis
#11
Huihua Chen, Haiyan Song, Xiao Liu, Jing Tian, Wenzhu Tang, Tongtong Cao, Pei Zhao, Chen Zhang, Wei Guo, Ming Xu, Rong Lu
Buyanghuanwu Decoction (BHD), a traditional Chinese medicine recipe, is a representative prescription for the treatment of qi-deficiency and blood-stasis syndrome. In this study, the effect of BHD on pressure overload induced cardiac remodeling was investigated and possible mechanism underlying was explored. Rats were randomly divided into four groups: sham, transverse aorta constriction (TAC) with saline, TAC with telmisartan (TAC+Tel), and TAC with BHD (TAC+BHD) for 16 weeks (n=6∼8 in each group). Cardiac morphological and functional changes were evaluated by echocardiography and histological methods, the molecular alterations were detected by western blotting...
August 30, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28837879/telmisartan-ameliorates-adipor1-and-adipor2-expression-via-ppar-%C3%AE-activation-in-the-coronary-artery-and-vsmcs
#12
Xuhua Shen, Hongwei Li, Weiping Li, Xing Wu, Zhijun Sun, Xiaosong Ding
The effects of telmisartan on insulin-resistant properties and expression of adiponectin receptors (AdipoRs) were investigated. A diabetic rat model was established using a high-fat diet and streptozotocin (25mg/kg) and primary rat coronary vascular smooth muscle cells (VSMCs) were used to elucidate the underlying mechanisms. The diabetic rats were insulin-resistant and exhibited weight gain, elevated blood pressures, and increased plasma triglyceride levels. These manifestations were ameliorated by elmisartan treatment...
August 21, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28836869/renin-angiotensin-system-as-a-potential-target-for-new-therapeutic-approaches-in-parkinson-s-disease
#13
REVIEW
Santiago Perez-Lloret, Matilde Otero-Losada, Jorge E Toblli, Francisco Capani
Currently, available therapies for Parkinson's disease (PD) are symptomatic. Therefore, the search for neuroprotective drugs remains a top priority. Areas covered: In this review, the potential symptomatic or disease-modifying effect of drugs targeting the Renin-Angiotensin System (RAS) in PD will be explored. Expert opinion: The importance of nigrostriatal local RAS has only begun to be unraveled in the last decades. On one hand, there is a complex feedback cycle between RAS and dopamine (DA). On the other hand, RAS affects dopaminergic neurons vulnerability...
October 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28829147/comprehensive-evaluation-of-the-binding-of-lipocalin-type-prostaglandin-d-synthase-to-poorly-water-soluble-drugs
#14
Yoshiaki Teraoka, Satoshi Kume, Yuxi Lin, Shogo Atsuji, Takashi Inui
Low water solubility of candidate drug compounds is a major problem in pharmaceutical research and development. We developed a novel drug delivery system (DDS) for poorly water-soluble drugs using lipocalin-type prostaglandin D synthase (L-PGDS), which belongs to the lipocalin superfamily and binds a large variety of hydrophobic molecules. In this study, we comprehensively evaluated the capability of L-PGDS to bind and solubilize various poorly water-soluble drugs using structure-based docking. Docking simulations of 2892 commercially available approved drugs indicated that L-PGDS shows higher binding affinities for various drugs compared with 2-hydroxypropyl-β-cyclodextrin...
October 2, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28805311/mechanistic-model-for-blood-pressure-and-heart-rate-changes-produced-by-telmisartan-in-humans
#15
Dong Woo Chae, Mijeong Son, Yukyung Kim, Hankil Son, Kyungsoo Park
Telmisartan, an angiotensin receptor blocker (ARB), is indicated for the treatment of essential hypertension. This study aimed to develop a mechanistic model of telmisartan drug effect in human using non-invasive markers. Data were acquired from a previous study where telmisartan 80 mg was given once daily for 6 days. Systolic (SBP) and diastolic blood pressure (DBP) and heart rate (HR) were measured before dosing for day 1 to 5 and serially after the last dose. Mean arterial pressure (MAP) and pulse pressure (PP) were calculated from SBP and DBP...
August 14, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28798804/sinomenine-hydrochloride-attenuates-renal-fibrosis-by-inhibiting-excessive-autophagy-induced-by-adriamycin-an-experimental-study
#16
Ming-Ming Zhao, Bin Yang, Qiu Zhang, Jin-Hu Wang, Jin-Ning Zhao, Yu Zhang
The objective of this study is to investigate if sinomenine hydrochloride (SIN-HCl) could be effective against adriamycin-induced renal fibrosis by regulating autophagy in a rat model. Forty male Sprague-Dawley (SD) rats were randomly divided into control group, model group, telmisartan group, and SIN-HCl group; rat model was induced by adriamycin; all rats were given intragastric administration for 6 weeks. Urine was collected from rats in metabolic cages to determine 24 h protein level. This was done after intragastric administration for the first two weeks and then once for every two weeks...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28791353/telmisartan-improves-vascular-remodeling-through-ameliorating-prooxidant-and-profibrotic-mechanisms-in-hypertension-via-the-involvement-of-transforming-growth-factor-%C3%AE-1
#17
Peijin Shang, Tianlong Liu, Wenxing Liu, Yuwen Li, Fang Dou, Yikai Zhang, Lijuan Sun, Tiejun Zhang, Zhihui Zhu, Fei Mu, Yi Ding, Aidong Wen
Vascular remodeling is a common complication and pathological basis of hypertension. Transforming growth factor‑β1 (TGF‑β1)/small mothers against decapentaplegic 3 (Smad3) is considered a potential therapeutic target for vascular remodeling in hypertension. The present study aimed to demonstrate the antifibrotic effects of telmisartan and examined the potential mechanisms associated with its prevention of vascular remodeling. Spontaneously hypertensive rats (SHRs) were treated with telmisartan (20 mg/kg), and vascular contractility, reactivity and oxidative stress were preliminarily evaluated...
October 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28754590/telmisartan-mitigates-hyperglycemia-induced-vascular-inflammation-by-increasing-gsk3%C3%AE-ser-9-phosphorylation-in-endothelial-cells-and-mouse-aortas
#18
Kee-Ho Song, Sun-Ju Bae, Jiyeon Chang, Jung-Hyun Park, Inho Jo, Kae Won Cho, Du-Hyong Cho
Telmisartan, an angiotensin II type 1 receptor blocker (ARB), attenuates hyperglycemia-aggravated vascular inflammation by decreasing IκB kinase β (IKKβ) expression in endothelial cells. Because glycogen synthase 3β (GSK3β) is involved in inflammatory process by regulating nuclear factor-κB (NF-κB) activity, we investigated whether GSK3β mediates telmisartan-ameliorated vascular inflammation in hyperglycemia-treated endothelial cells and high-fat diet (HFD)-fed mice. Telmisartan remarkably induced GSK3β-Ser(9) phosphorylation in hyperglycemia-treated endothelial cells that accompanied a decrease in hyperglycemia-induced NF-κB p65-Ser(536) phosphorylation, vascular cell adhesion molecule-1 (VCAM-1) expression, and THP-1 monocyte adhesion...
September 30, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28747068/a-dual-ampk-nrf2-activator-reduces-brain-inflammation-after-stroke-by-enhancing-microglia-m2-polarization
#19
Yunjie Wang, Yun Huang, Yazhou Xu, Wenchen Ruan, Haojie Wang, Yihua Zhang, Juan M Saavedra, Luyong Zhang, Zhangjian Huang, Tao Pang
AIMS: Microglia-mediated neuroinflammation plays an important role in focal ischemic stroke, a disorder with no effective therapeutic agents. Since microglial polarization to the M2 phenotype and reduction of oxidative stress are mediated through AMPK and Nrf2 activation, we assessed the dual therapeutic effect of AMPK and Nrf2 activation by a novel neuroprotectant HP-1c in the treatment of ischemic stroke. RESULTS: We developed a novel class of hybrids (HP-1a-HP-1f) of telmisartan and 2-(1-hydroxypentyl)-benzoate (HPBA) as a ring-opening derivative of NBP...
July 26, 2017: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/28745698/-telmisartan-in-the-treatment-of-hypertensive-patients
#20
REVIEW
V I Podzolkov, A I Tarzimanova
The paper highlights the use of telmisartan, one of the currently available angiotensin receptor blockers, for the treatment of patients with hypertension, metabolic syndrome, and those at high cardiovascular risk. Telmisartan treatment allows blood pressure control, provides organ protection at different stages of the cardiovascular continuum, and reduces the risk of cardiovascular diseases and death. The additional properties and pleiotropic activity of the drug determines its wide range of applications in cardiology...
2017: Terapevticheskiĭ Arkhiv
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