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Yun Zhu, Lijuan Wen, Shihong Shao, Yanan Tan, Tingting Meng, Xiqin Yang, Yupeng Liu, Xuan Liu, Hong Yuan, Fuqiang Hu
Cancer associated fibroblasts (CAFs) are the most abundant, genetically stable stroma cells and localize near blood vessels within "finger-like" collagen-rich stroma, which lead to restrained drug transport in dense stroma instead of tumor cells inside tumor mass, especially for targeting micelles. Meanwhile, the bioactive cytokines secreted by stroma cells result in microenvironment mediated drug resistance (TMDR). Hence, a biologically inspired Telmisartan (Tel) grafting glycolipid micelles (Tel-CSOSA) are constructed, which can sequentially target angiotensin II type I receptor (AT1R) overexpressed on both CAFs and tumor cells...
January 18, 2018: Biomaterials
Rui-Juan Zhuang, Wei-Dong Jin, Xiao-Yan Wang, Xue-Ming Wu
Olmesartan (OL) is the pharmacologically active metabolite of Olmesartan medoxomil (OM), an FDA-approved angiotensin II receptor antagonist for administrating cardiovascular diseases. The drug has been found to have potential effects on diverse protein kinase signaling involved in the pathogenesis of atherosclerosis, either by directly inhibiting the hub kinases or by indirectly modulating marginal members in the signaling pathways. In the present study, we computationally model the kinase-chemical Interaction Profile between six OL-related chemicals (i...
January 30, 2018: Journal of Molecular Graphics & Modelling
Pinaki Sengupta, Bappaditya Chatterjee, Uttam Kumar Mandal, Bapi Gorain, Tapan Kumar Pal
Management of cardiovascular risk factors in diabetes demands special attention due to their co-existence. Pioglitazone (PIO) and telmisartan (TLM) combination can be beneficial in effective control of cardiovascular complication in diabetes. In this research, we developed and validated a high throughput LC-MS/MS method for simultaneous quantitation of PIO and TLM in rat plasma. This developed method is more sensitive and can quantitate the analytes in relatively shorter period of time compared to the previously reported methods for their individual quantification...
December 2017: Journal of Pharmaceutical Analysis
Netanya S Utay, Douglas W Kitch, Eunice Yeh, Carl J Fichtenbaum, Michael M Lederman, Jacob D Estes, Claire Deleage, Clara Magyar, Scott D Nelson, Karen L Klingman, Barbara Bastow, Amneris E Luque, Grace A McComsey, Daniel C Douek, Judith S Currier, Jordan E Lake
Background: Fibrosis in lymph nodes may limit CD4+ T-cell recovery and lymph node and adipose tissue fibrosis may contribute to inflammation and comorbidities despite antiretroviral therapy (ART). We hypothesized that the angiotensin receptor blocker and PPAR-γ agonist telmisartan would decrease lymph node or adipose tissue fibrosis in treated HIV-1 infection. Methods: In this 48-week, randomized-controlled trial, adults continued suppressive ART and received telmisartan or no drug...
February 1, 2018: Journal of Infectious Diseases
Tao Chen, Jieyong Xing, Yanshao Liu
The aim of the present study was to investigate the effects of telmisartan on vascular endothelial functions, inflammatory factors and insulin resistance of coronary heart disease patients complicated with diabetes mellitus. In total, 80 coronary heart disease patients complicated with type 2 diabetes mellitus, admitted and treated in the Zhangqiu Hospital from January 2016 to March 2017 were enrolled in the study. Each patient was randomly assigned to an observation (n=40) or a control group (n=40) using a random number table...
January 2018: Experimental and Therapeutic Medicine
Yi-Zhi Xu, Yun Wang, Dai-Ying He, Liang Zhang
OBJECTIVE: To investigate the effects of 4 renin-angiotensin system's(RAS) regulators (losartan, telmisartan, aliskiren and angiotenisin) on the human leukemia HEL cell growth. METHODS: The HEL cells were treated with losartan, telmisartan, aliskiren and Angiotensin-(1-7) (Ang-(1-7)) for 12 days, respectively. The cell proliferation was measured by CCK-8 kit, the cell cycle and apoptosis were measured by flow cytometry. RESULTS: The 10-7 mol/L Ang-(1-7) markedly inhibited the growth of HEL cells, blocked cells at G0/G1 phase and markedly increased the late apoptotic cells (P< 0...
February 2018: Zhongguo Shi Yan Xue Ye Xue za Zhi
Tzu-Tung Chang, Chia-Jung Yang, Yu-Chi Lee, Sheng-Nan Wu
Telmisartan (Tel) is recognized as a non-peptide blocker of angiotensin II type-1 receptor. Whether this agent has any direct effects on ion currents remains unexplored. In whole-cell current recordings, addition of Tel increased the peak amplitude of voltage-gated Na⁺ current (INa) accompanied by the increased time constant of INa inactivation in differentiated NSC-34 motor neuron-like cells. Tel-stimulated INa in these cells is unlinked to either blockade of angiotensin II receptors or activation of PPAR-γ...
January 29, 2018: Chinese Journal of Physiology
Abdul Ahad, Mohammad Raish, Ajaz Ahmad, Fahad I Al-Jenoobi, Abdullah M Al-Mohizea
The aim of present study was to develop and evaluate vesicles containing bile salt formulation of telmisartan for the treatment of diabetic nephropathy. Different vesicles containing bile salt formulations were developed by varying ratios of soybean phosphatidylcholine and sodium deoxycholate. Prepared formulations were characterized for their size, polydispersity index, zeta potential, morphology and entrapment efficiency. Further, the renoprotective outcome of optimized formulation was studied in streptozotocin-induced diabetic nephropathy rat model...
January 26, 2018: Artificial Cells, Nanomedicine, and Biotechnology
Ryo Sato, Chika Hiraishi, Hiroshi Yoshida
Matrix metalloproteinase (MMP), which is secreted from vascular cells, is an enzyme degrading extracellular matrix protein. MMP molecules, including MMP-2, are involved in the destabilization of atherosclerotic plaque and plaque rupture during the development of cardiovascular disease (CVD). Angiotensin II (Ang-II), a vascular stimulant associated with CVD progression, has been demonstrated to be mainly involved in cardiovascular remodeling of atherosclerosis and cardiac hypertrophy. This study was performed to investigate the regulation of MMP-2 by Ang-II in human umbilical vein endothelial cells (HUVECs)...
January 23, 2018: Journal of Cardiovascular Pharmacology
Jamol Uzokov, Anis Alyavi, Baxrom Alyavi
No abstract text is available yet for this article.
August 2017: Atherosclerosis
Baohui Xu, Haojun Xuan, Yasunori Iida, Masaaki Miyata, Ronald L Dalman
BACKGROUND: Abdominal aortic aneurysm (AAA) is a chronic degenerative inflammatory disease. Multi-factors including genetic, environmental and lifestyles determine the onsets and progression of AAAs. Currently surgical repair remains the only effective aneurysm treatment, but no pharmacological therapy is available for limiting further enlargement of small AAAs and fetal rupture. OBJECTIVE: This article is to review our current understanding of angiotensin II (Ang II) and its type 1 receptor (AT1) in AAA pathogenesis as well as the translational potential of AT1 receptor blocker (ARB) treatment for treating clinical AAA disease...
January 22, 2018: Current Drug Targets
Junichi Takano, Kazuya Maeda, Hiroyuki Kusuhara, Yuichi Sugiyama
Among organic anion transporting polypeptide (Oatp) family transporters expressed in the rodent liver, such as Oatp1a1, Oatp1a4, Oatp1b2, and Oatp2b1, Oatp1a4 has a unique character to recognize neutral cardiac glycosides as substrate in addition to organic anions. The relative contribution of Oatp1a4 to the substrate uptake into hepatocytes has not been clarified. In this study, we investigated the importance of Oatp1a4 in the hepatic uptake of its substrate drugs using Slco1a4-/- mice. The hepatic mRNA expression of Slco1a4 was decreased significantly in Slco1a4-/- mice, whereas no differences were seen in other hepatic transporters between wild-type and Slco1a4-/- mice...
January 18, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Zhe Jin, Qindong Tan, Bei Sun
Coronary slow flow phenomenon (CSFP) is a coronary microvascular disorder with an increasing morbidity, and currently, available therapies are of limited clinical value for its cure. Hence, it is urgent to find a novel approach to CSFP treatment. Several studies show that endothelial dysfunction plays a critical role in the aetiology of CSFP. Telmisartan (TMST) is a clinically available anti-hypertensive medicine and has shown its potential properties for improving vascular endothelial function. Thus, we aimed to investigate the effect of TMST on endothelial dysfunction in CSFP, Endothelial-dependent flow-mediated vasodilation, serum levels of nitric oxide, adiponectin, and endothelin-1 were surveyed before and after 3 months of TMST treatment...
January 2018: Cell Biochemistry and Function
Edmund Cheung So, Sheng-Nan Wu, Yi-Ching Lo, Kevin Su
Voltage-gated Na+ currents (INa), known to contain many components (e.g., transient, resurgent and persistent INa) with unique gating properties, are involved in the generation and propagation of action potentials in excitable cells. In this study, how tefluthrin (Tef), a synthetic pyrethoid, and telmisartan (TEL), blocker of angiotensin II receptors can perturb those components of INa was investigated. The presence of either Tef or TEL increased the values of the gating charges of INa involved in the activation (za) and inactivation (za)...
January 3, 2018: Toxicology Letters
Enikő Borbás, Zsombor K Nagy, Brigitta Nagy, Attila Balogh, Balázs Farkas, Oksana Tsinman, Konstantin Tsinman, Bálint Sinkó
In this study, brand and four generic formulations of telmisartan, an antihypertensive drug, were used in in vitro simultaneous dissolution-absorption, investigating the effect of different formulation additives on dissolution and on absorption through an artificial membrane. The in vitro test was found to be sensitive enough to show even small differences between brand and generic formulations caused by the use of different excipients. By only changing the type of filler from sorbitol to mannitol in the formulation, the flux through the membrane was reduced by approximately 10%...
January 3, 2018: European Journal of Pharmaceutical Sciences
Csaba Varga, Tamás Malina, Viktória Alföldi, Gergely Bilics, Ferenc Nagy, Tibor Oláh
We report a severe envenoming associated with minimal local symptoms following a Balkan adder (Vipera berus bosniensis) bite in South-Western Hungary. A 63-year-old male with a history of hypertension and sinus bradycardia (45/min) was bitten by a sub-adult specimen of V. b. bosniensis in Somogy County on 04 May 2017. The patient was transported to and treated at the Emergency Department of Somogy County "Moritz Kaposi" General Hospital, Kaposvár. Locally only pain and minimal swelling with a small haematoma developed on the bitten finger...
January 2, 2018: Toxicon: Official Journal of the International Society on Toxinology
Naira da Silva Mansano, Isabela Fernandes Jorge, Agnaldo Bruno Chies, Gustavo Arruda Viani, Maria Angélica Spadella
AIMS: To analyze the effects of radiation on the reproductive tissue of male Wistar rats and to evaluate whether treatment with the Ang II AT1 receptor antagonists telmisartan and losartan mitigate the dysfunctions resulting from this exposure. MAIN METHODS: Rats were randomly divided into groups: Control, Irradiated, Telmisartan, Losartan, Irradiated+Telmisartan, and Irradiated+Losartan. Single dose of 5Gy was administered directly into the scrotum, followed by treatment with telmisartan (12mg/kg/day) or losartan (34mg/kg/two times/day) for 60days...
December 26, 2017: Life Sciences
Sophie E Rowbotham, Smriti M Krishna, Corey S Moran, Jonathan Golledge
Objective This mini-review provides the rationale and updated progress for ongoing randomized controlled trials assessing fenofibrate and telmisartan efficacy to limit abdominal aortic aneurysm (AAA) growth. Methods / Results Data from preclinical and human studies investigating the efficacy of fenofibrate and telmisartan to limit AAA growth is presented and provides the rationale for three current randomized controlled trials assessing these medications as potential interventions to limit aneurysm growth in AAA patients...
December 27, 2017: Current Drug Targets
Yen Ping Ng, Ganesh Pandian Balasubramanian, Yi Ping Heng, Meera Kalaiselvan, Yu Wen Teh, Kin Man Cheong, Muhammad Faiz Bin Abdul Hadi, Rosmaliza Bt Othman
AIMS: Recent data showed an alarming rise of new dialysis cases secondary to diabetic nephropathy despite the growing usage of RAAS blockers. Primary objective of this study is to explore the prevalence of RAAS blockers usage among type II diabetic patients, secondary objectives are to compare the prescribing pattern of RAAS blocker between primary and tertiary care center and to explore if the dose of RAAS blocker prescribed was at optimal dose as suggested by trials. MATERIALS AND METHODS: This is a retrospective study conducted at one public tertiary referral hospital and one public health clinic in Sungai Petani, Kedah, Malaysia...
December 21, 2017: Diabetes & Metabolic Syndrome
V I Podzolkov, N A Dragomiretskaya
We present in this paper modern views on components, physiological and pathophysiological effects of the renin-angiotensin system, pathways of its hyperactivation at various stages of the cardiovascular continuum. Special emphasis is made on angiotensin receptor blockers (sartans). Basing on results of analysis of randomized clinical trials of these agents we have outlined clinical situations in which prescription of one or another drug from this group is preferable. For patients with multiple risk factors of cardiovascular complications preferable agent is telmisartan, for patients with nephropathy - irbesartan, for survivors of acute myocardial infarction - valsartan, while for patients with clinical signs of chronic heart failure with low ejection fraction 3 agents can be designated as preferrable - losartan, valsartan, and candesartan...
October 2017: Kardiologiia
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