Endothelium as a Therapeutic Target in Diabetes Mellitus: From Basic Mechanisms to Clinical Practice.

Abstract:

:Endothelium plays an essential role in human homeostasis by regulating arterial blood pressure, distributing nutrients and hormones as well as providing a smooth surface that modulates coagulation, fibrinolysis and inflammation. Endothelial dysfunction is present in Diabetes Mellitus (DM) and contributes to the development and progression of macrovascular disease, while it is also associated with most of the microvascular complications such as diabetic retinopathy, nephropathy and neuropathy. Hyperglycemia, insulin resistance, hyperinsulinemia and dyslipidemia are the main factors involved in the pathogenesis of endothelial dysfunction. Regarding antidiabetic medication, metformin, gliclazide, pioglitazone, exenatide and dapagliflozin exert a beneficial effect on Endothelial Function (EF); glimepiride and glibenclamide, dipeptidyl peptidase-4 inhibitors and liraglutide have a neutral effect, while studies examining the effect of insulin analogues, empagliflozin and canagliflozin on EF are limited. In terms of lipid-lowering medication, statins improve EF in subjects with DM, while data from short-term trials suggest that fenofibrate improves EF; ezetimibe also improves EF but further studies are required in people with DM. The effect of acetylsalicylic acid on EF is dose-dependent and lower doses improve EF while higher ones do not. Clopidogrel improves EF, but more studies in subjects with DM are required. Furthermore, angiotensin- converting-enzyme inhibitors /angiotensin II receptor blockers improve EF. Phosphodiesterase type 5 inhibitors improve EF locally in the corpus cavernosum. Finally, cilostazol exerts favorable effect on EF, nevertheless, more data in people with DM are required.

journal_name

Curr Med Chem

authors

Tentolouris A,Eleftheriadou I,Tzeravini E,Tsilingiris D,Paschou SA,Siasos G,Tentolouris N

doi

10.2174/0929867326666190119154152

subject

Has Abstract

pub_date

2020-01-01 00:00:00

pages

1089-1131

issue

7

eissn

0929-8673

issn

1875-533X

pii

CMC-EPUB-95948

journal_volume

27

pub_type

杂志文章
  • The efficacy of viral capsid inhibitors in human enterovirus infection and associated diseases.

    abstract::Enteroviruses are members of picornavirus family which causes diverse and severe diseases in humans and animals. Clinical manifestations of enterovirus infections include fever, hand, foot, and mouth disease, and herpangina. Enteroviruses also cause potentially severe and life-threatening infections such as meningitis...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986707780363032

    authors: Li C,Wang H,Shih SR,Chen TC,Li ML

    更新日期:2007-01-01 00:00:00

  • Update on the Molecular Mechanisms Underlying the Effect of Cholecystokinin and Cholecystokinin-1 Receptor on the Formation of Cholesterol Gallstones.

    abstract::Cholecystokinin (CCK) is an important neuro-intestinal peptide hormone produced by the enteroendocrine I-cells in the upper part of small intestine. Protein- and fat-enriched food plays an important role in triggering CCK secretion from the intestine. Carbohydrates stimulate only small amounts of CCK release. The CCK-...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867324666170619104801

    authors: Wang HH,Portincasa P,Wang DQ

    更新日期:2019-01-01 00:00:00

  • Neurotrophins' Modulation by Olive Polyphenols.

    abstract:BACKGROUND:Polyphenols are probably the most known and investigated molecules of nutritional interest as micronutrients present in abundance in our diet. Some of the most important food sources of polyphenols in the Mediterranean diet are olives and olive oil. A growing body of evidence from animal models to clinical s...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867323666160627104022

    authors: Carito V,Ceccanti M,Tarani L,Ferraguti G,Chaldakov GN,Fiore M

    更新日期:2016-01-01 00:00:00

  • The structure and pharmacological functions of coumarins and their derivatives.

    abstract::Coumarins are of many different structures. They constitute an important class of pharmacological agents possessing a range of different physiological activities including anti-cancer, anti-oxidant, anti- inflammation, anti-HIV, anti-coagulant, anti-bacterial, analgesic and comparative immune-modulation. Recently, cou...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986709789578187

    authors: Wu L,Wang X,Xu W,Farzaneh F,Xu R

    更新日期:2009-01-01 00:00:00

  • Antidiabetic agents from medicinal plants.

    abstract::Currently available therapeutic options for non-insulin-dependent diabetes mellitus, such as dietary modification, oral hypoglycemics, and insulin, have limitations of their own. Many natural products and herbal medicines have been recommended for the treatment of diabetes. The present paper reviews medicinal plants t...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986706776360860

    authors: Jung M,Park M,Lee HC,Kang YH,Kang ES,Kim SK

    更新日期:2006-01-01 00:00:00

  • Aminopeptidase N (APN/CD13) as a target for anti-cancer agent design.

    abstract::APN is an important zinc dependent metallo-exopeptidase; it has been considered as a suitable target for anti-cancer drug design. In this review we focus on the most effective and the most promising inhibitors of aminopeptidase N. Their binding modes to the enzyme, the attempt to explain the origin of the inhibitory a...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986708786242840

    authors: Zhang X,Xu W

    更新日期:2008-01-01 00:00:00

  • Therapeutic Macromolecular Iron Chelators.

    abstract::Iron is a key element for every single living process. On a fundamental level, targeting iron is a valuable approach for the treatment of disorders caused by iron overload. Utilizing iron chelators as therapeutic agents has received expanding consideration in chelation therapy. Approved low molecular weight (MW) iron ...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/0929867325666180904104318

    authors: Bulbake U,Singh A,Domb AJ,Khan W

    更新日期:2019-01-01 00:00:00

  • Cardiac Arrhythmias in Patients with Chronic Kidney Disease: Implications of Renal Failure for Antiarrhythmic Drug Therapy.

    abstract::The kidney has numerous complex interactions with the heart, including shared risk factors (e.g., hypertension, dyslipidemia, etc.) and mutual amplification of morbidity and mortality. Both cardiovascular diseases and chronic kidney disease (CKD) may cause various alterations in cardiovascular system, metabolic homeos...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867323666160309114246

    authors: Potpara TS,Jokic V,Dagres N,Marin F,Prostran MS,Blomstrom-Lundqvist C,Lip GY

    更新日期:2016-01-01 00:00:00

  • Synthetic strategies and medicinal properties of beta-lactams.

    abstract::More than five decades since the Discovery of Penicillin, the chemistry and biological activity of b-lactams continue to attract the wide spread attention of research workers. Owing to high efficacy and extremely safe toxicological profile, they are agents of choice in the current therapeutic index for the bacterial i...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:

    authors: Kidwai M,Sapra P,Bhushan KR

    更新日期:1999-03-01 00:00:00

  • Synthesis and applications for unnatural sugar nucleotides.

    abstract::The synthesis and biological evaluation of carbohydrate mimetics has begun to more clearly define the diverse roles of carbohydrates in nature. Often the strategy invoves the design and synthesis of glycosyltransferase and glycosidase inhibitors both as tools to elucidate the mechanism of action of these enzymes and a...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:

    authors: Elhalabi JM,Rice KG

    更新日期:1999-02-01 00:00:00

  • A possible target of antioxidative therapy for diabetic vascular complications-vascular NAD(P)H oxidase.

    abstract::A growing body of evidence has shown that oxidative stress may be involved in the development of vascular complications associated with diabetes. However, the molecular mechanism for increased reactive oxygen species (ROS) production in diabetes remains uncertain. Among various possible mechanisms, attention have incr...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867033457133

    authors: Inoguchi T,Tsubouchi H,Etoh T,Kakimoto M,Sonta T,Utsumi H,Sumimoto H,Yu HY,Sonoda N,Inuo M,Sato N,Sekiguchi N,Kobayashi K,Nawata H

    更新日期:2003-09-01 00:00:00

  • Strategies for the stereocontrolled formation of oxygen analogues of penicillins and cephalosporins.

    abstract::The synthesis of oxacephalotin and oxacephamandol, which are more active than natural, sulfur-containing congeners, and the isolation of clavulanic acid, a potent inhibitor of beta-lactamase enzymes, directed attention of many academic and industrial laboratories the synthesis of oxygen analogues of penicillins and ce...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867043364883

    authors: Łysek R,Borsuk K,Furman B,Kałuza Z,Kazimierski A,Chmielewski M

    更新日期:2004-07-01 00:00:00

  • Synthesis, electrophilic substitution and structure-activity relationship studies of polycyclic aromatic compounds towards the development of anticancer agents.

    abstract::Polycyclic aromatic hydrocarbons (PAH) are considered potentially carcinogenic. Substituted PAH derivatives, in contrast, may serve as anticancer agents, and as chemotherapeutics. This article presents a review of their use. Particular emphasis is placed on the synthesis of these new compounds, electrophilic substitut...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867013372120

    authors: Banik BK,Becker FF

    更新日期:2001-10-01 00:00:00

  • Salvianolic acid B inhibits atherogenesis of vascular cells through induction of Nrf2-dependent heme oxygenase-1.

    abstract:AIMS:Salvianolic acid B (Sal B), one of the most active components of Danshen extracts, has beneficial roles in the prevention and treatment of cardiovascular diseases. However, the precise mechanism by which Sal B exerts its effects on vascular cells is unclear. We aimed to elucidate the effects of Sal B on vascular c...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/0929867321666140601195940

    authors: Lee HJ,Seo M,Lee EJ

    更新日期:2014-01-01 00:00:00

  • Essentiality, toxicology and chelation therapy of zinc and copper.

    abstract::Both zinc and copper are essential minerals that are required for various cellular functions. Although these metals are essential, they can be toxic at excess amounts, especially in certain genetic disorders. Zinc and copper homeostasis results from a coordinated regulation by different proteins involved in uptake, ex...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986705774462950

    authors: Cai L,Li XK,Song Y,Cherian MG

    更新日期:2005-01-01 00:00:00

  • Targeting the nucleotide metabolism proteins of the NUDIX family and SAMHD1 in cancer.

    abstract::The nucleotide metabolism has been targeted for many years and in various clinical settings, including cancer. The increased knowledge of certain enzymes involved in this metabolism and in associated cellular processes accumulated over the last few years, gives important information to the druggability of certain prot...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/0929867328666201125120422

    authors: Forey P,Cros-Perrial E,Dumontet C,Jordheim LP

    更新日期:2020-11-25 00:00:00

  • Proteasome inhibition: a promising strategy for treating cancer, but what about neurotoxicity?

    abstract::The inhibition of protein degradation through the ubiquitin-proteasome pathway is a recently developed approach to cancer treatment which extends the range of cellular targets for chemotherapy. This therapeutic strategy is very interesting since the proteasomes carry out the regulated degradation of unnecessary or dam...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986708786848622

    authors: Gilardini A,Marmiroli P,Cavaletti G

    更新日期:2008-01-01 00:00:00

  • Drug excipients.

    abstract::The therapeutical use of drugs involves the application of dosage forms, serving as carrier systems together with several excipients to deliver the active ingredient to the site of action. Drug delivery technology combines an understanding of medicinal chemistry and pharmacology with the skill of formulation, aiming t...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986706778201648

    authors: Kalász H,Antal I

    更新日期:2006-01-01 00:00:00

  • Progress towards the discovery of orally active thrombin inhibitors.

    abstract::The serine protease thrombin is a key enzyme in the control of blood coagulation and displays numerous other effects on platelet, endothelial and smooth muscle cell function. The pre-eminence of thrombin in the coagulation cascade has made the enzyme a popular drug target in the search for more clinically acceptable a...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:

    authors: Menear K

    更新日期:1998-12-01 00:00:00

  • Molecular modeling and computer aided drug design. Examples of their applications in medicinal chemistry.

    abstract::The development of new drugs with potential therapeutic applications is one of the most complex and difficult process in the pharmaceutical industry. Millions of dollars and man-hours are devoted to the discovery of new therapeutical agents. As, the activity of a drug is the result of a multitude of factors such as bi...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867003375317

    authors: Ooms F

    更新日期:2000-02-01 00:00:00

  • Monoclonal antibody "gold rush".

    abstract::The market, sales and regulatory approval of new human medicines, during the past few years, indicates increasing number and share of new biologics and emergence of new multibillion dollar molecules. The global sale of monoclonal antibodies in 2006 were $20.6 billion. Remicade had annual sales gain of $1 billion durin...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986707781368504

    authors: Maggon K

    更新日期:2007-01-01 00:00:00

  • Genistein aglycone: a dual mode of action anti-osteoporotic soy isoflavone rebalancing bone turnover towards bone formation.

    abstract::Osteoporosis is characterized by reduced bone mass and structural deterioration of bone tissue leading to enhanced bone fragility and a consequent increase in fracture risk. Bone loss further increases in postmenopausal women when the ovaries stop making estrogens. Women undergoing treatment for osteoporosis require l...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986710791959738

    authors: Bitto A,Polito F,Squadrito F,Marini H,D'Anna R,Irrera N,Minutoli L,Granese R,Altavilla D

    更新日期:2010-01-01 00:00:00

  • Pharmacological inhibition of protein tyrosine phosphatase 1B: a promising strategy for the treatment of obesity and type 2 diabetes mellitus.

    abstract::Obesity and metabolic syndrome represent major public health problems, and are the biggest preventable causes of death worldwide. Obesity is the leading risk factor for type 2 diabetes mellitus (T2DM), cardiovascular diseases and non-alcoholic fatty liver disease. Obesity-associated insulin resistance, which is charac...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867311320210001

    authors: Panzhinskiy E,Ren J,Nair S

    更新日期:2013-01-01 00:00:00

  • Fullerenes for applications in biology and medicine.

    abstract::Fullerenes as a unique class of carbon allotropes have been studied extensively for their distinctive material properties and potential technological applications, including those in biology and medicine. Since a major focus in the latter has been on drug development and formulation, in this paper we highlight some re...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/092986711795656225

    authors: Anilkumar P,Lu F,Cao L,Luo PG,Liu JH,Sahu S,Tackett KN,Wang Y,Sun YP

    更新日期:2011-01-01 00:00:00

  • Potential use of polymeric nanoparticles for drug delivery across the blood-brain barrier.

    abstract::Nanomedicine is certainly one of the scientific and technological challenges of the coming years. In particular, biodegradable nanoparticles formulated from poly (D,L-lactide-co-glycolide) (PLGA) have been extensively investigated for sustained and targeted delivery of different agents, including recombinant proteins,...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867311320170006

    authors: Tosi G,Bortot B,Ruozi B,Dolcetta D,Vandelli MA,Forni F,Severini GM

    更新日期:2013-01-01 00:00:00

  • Targeting epidermal growth factor receptor in solid tumors: critical evaluation of the biological importance of therapeutic monoclonal antibodies.

    abstract::Numerous cellular pathways have a significant impact in the growth and metastatic potential of tumors. Essential element of such pathways is the epidermal growth factor receptor (EGFR), a member of the HER family of receptor tyrosine kinases. One of the most important issues in cancer, which attracted the attention of...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986709789177984

    authors: Gialeli Ch,Kletsas D,Mavroudis D,Kalofonos HP,Tzanakakis GN,Karamanos NK

    更新日期:2009-01-01 00:00:00

  • Biological and chemical diversity of coral-derived microorganisms.

    abstract::Coral-derived microorganisms have been a major focus of many research efforts on marine ecology in recent decades. Importantly, research on bioactive compounds from these diverse microorganisms, which include fungi and bacteria, has experienced an explosive growth during the past five years. This has unveiled the ecol...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867322666151006093755

    authors: Hou XM,Xu RF,Gu YC,Wang CY,Shao CL

    更新日期:2015-01-01 00:00:00

  • Thermosensitive polymeric hydrogels as drug delivery systems.

    abstract::Thermosensitive hydrogels are very important biomaterials used in drug delivery systems (DDSs), which gained increasing attention of researchers. Thermosensitive hydrogels have great potential in various applications, such as drug delivery, cell encapsulation, tissue engineering, and etc. Especially, injectable thermo...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:

    authors: Gong C,Qi T,Wei X,Qu Y,Wu Q,Luo F,Qian Z

    更新日期:2013-01-01 00:00:00

  • Structural approaches to explain the selectivity of COX-2 inhibitors: is there a common pharmacophore?

    abstract::The identification and characterisation of the isoenzyme cyclooxygenase 2 (COX-2) stimulated investigations to develop efficient non-steroidal anti-inflammatory drugs with reduced side effects compared to standard NSAIDs. This review will focus on the structural features needed to achieve COX-2 selectivity. Five struc...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867003374237

    authors: Dannhardt G,Laufer S

    更新日期:2000-11-01 00:00:00

  • Fine-tuning of microRNAs in Type 2 Diabetes Mellitus.

    abstract::Type 2 diabetes mellitus is a metabolic disease widely spread across industrialized countries. Sedentary lifestyle and unhealthy alimentary habits lead to obesity, boosting both glucose and fatty acid in the bloodstream and eventually, insulin resistance, pancreas inflammation and faulty insulin production or secretio...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867325666171205163944

    authors: Rosado JA,Diez-Bello R,Salido GM,Jardin I

    更新日期:2019-01-01 00:00:00