Calenduloside E Analogues Protecting H9c2 Cardiomyocytes Against H2O2-Induced Apoptosis: Design, Synthesis and Biological Evaluation.

Abstract:

:Modulation of apoptosis is therapeutically effective in cardiomyocytes damage. Calenduloside E (CE), a naturally occurring triterpenoid saponin, is a potent anti-apoptotic agent. However, little is known about its synthetic analogues on the protective effects in apoptosis of cardiomyocytes. The present research was performed to investigate the potential protective effect of CE analogues against H2O2-induced apoptosis in H9c2 cardiomyocytes and the underlying mechanisms. Sixteen novel CE anologues have been designed, synthesized and biological evaluation. Among the 16 CE anologues, as well as the positive control CE tested, compound 5d was the most effective in improving cardiomyocytes viability. Pretreatment with anologue 5d inhibited ROS generation, maintained the mitochondrial membrane potential and reduced apoptotic cardiomyocytes. Moreover, exposure to H2O2 significantly increased the levels of Bax, cleaved caspase-3, and cleaved PARP, and decreased the level of Bcl-2, resulting in cell apoptosis. Pretreatment with anologue 5d (0.02-0.5 μg/mL) dose-dependently upregulated antiapoptotic proteins and downregulated proapoptotic proteins mentioned above during H2O2-induced apoptosis. These results suggested that CE analogues provide protection to H9c2 cardiomyocytes against H2O2-induced oxidative stress and apoptosis, most likely via anti-apoptotic mechanism, and provided the basis for the further optimization of the CE analogues.

journal_name

Front Pharmacol

authors

Tian Y,Du YY,Shang H,Wang M,Sun ZH,Wang BQ,Deng D,Wang S,Xu XD,Sun GB,Sun XB

doi

10.3389/fphar.2017.00862

subject

Has Abstract

pub_date

2017-11-23 00:00:00

pages

862

issn

1663-9812

journal_volume

8

pub_type

杂志文章
  • Orally Administered Koumine Persists Longer in the Plasma of Aged Rats Than That of Adult Rats as Assessed by Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry.

    abstract::Aging leads to changes in nearly all pharmacokinetic phases. Koumine (KM), an alkaloid derived from Gelsemium elegans Benth., is effective against age-associated chronic diseases, but its dose proportionality following oral administration in aged individuals remains unknown. Herein, we established and validated a simp...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2020.01113

    authors: Ye LX,Xu Y,Zhang SH,Cao DX,Chen LF,Su YP,Huang HH,Yu CX

    更新日期:2020-07-21 00:00:00

  • Eriodictyol Attenuates Myocardial Ischemia-Reperfusion Injury through the Activation of JAK2.

    abstract::Myocardial ischemia-reperfusion (I/R) injury remains the leading risk factor of disability and mortality worldwide. In this study, the myocardial protective effect of eriodictyol (EDT) and the underlying mechanism in an ex vivo model of global myocardial I/R was investigated. After treatment with different concentrati...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2018.00033

    authors: Li D,Lu N,Han J,Chen X,Hao W,Xu W,Liu X,Ye L,Zheng Q

    更新日期:2018-01-30 00:00:00

  • Dendrobium officinale Polysaccharide Protected CCl4-Induced Liver Fibrosis Through Intestinal Homeostasis and the LPS-TLR4-NF-κB Signaling Pathway.

    abstract::We explored the therapeutic effects of Dendrobium officinale polysaccharide (DOP) on CCl4-induced liver fibrosis with respect to the intestinal hepatic axis using a rat model. Histopathological staining results showed that DOP alleviated extensive fibrous tissue proliferation in interstitium and lessened intestinal mu...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2020.00240

    authors: Wang K,Yang X,Wu Z,Wang H,Li Q,Mei H,You R,Zhang Y

    更新日期:2020-03-12 00:00:00

  • Effect of Cognitive Style on Learning and Retrieval of Navigational Environments.

    abstract::Field independence (FI) has been found to correlate with a wide range of cognitive processes requiring cognitive restructuring. Cognitive restructuring, that is going beyond the information given by the setting, is pivotal in creating stable mental representations of the environment, the so-called "cognitive maps," an...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2017.00496

    authors: Boccia M,Vecchione F,Piccardi L,Guariglia C

    更新日期:2017-07-25 00:00:00

  • The Preoperative Supplementation With Vitamin D Attenuated Pain Intensity and Reduced the Level of Pro-inflammatory Markers in Patients After Posterior Lumbar Interbody Fusion.

    abstract::The aim of this experimental study was to assess whether 5 weeks of preoperative supplementation with vitamin D affects the intensity of pain and the level of inflammatory markers in patients undergoing posterior lumbar interbody fusion (PLIF) followed by rehabilitation. 42 patients were divided, by double-blind rando...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2019.00527

    authors: Krasowska K,Skrobot W,Liedtke E,Sawicki P,Flis DJ,Dzik KP,Libionka W,Kloc W,Kaczor JJ

    更新日期:2019-05-22 00:00:00

  • Non-linear Entropy Analysis in EEG to Predict Treatment Response to Repetitive Transcranial Magnetic Stimulation in Depression.

    abstract::Background: Biomarkers that predict clinical outcomes in depression are essential for increasing the precision of treatments and clinical outcomes. The electroencephalogram (EEG) is a non-invasive neurophysiological test that has promise as a biomarker sensitive to treatment effects. The aim of our study was to invest...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2018.01188

    authors: Shalbaf R,Brenner C,Pang C,Blumberger DM,Downar J,Daskalakis ZJ,Tham J,Lam RW,Farzan F,Vila-Rodriguez F

    更新日期:2018-10-30 00:00:00

  • Icariin Protects Hippocampal Neurons From Endoplasmic Reticulum Stress and NF-κB Mediated Apoptosis in Fetal Rat Hippocampal Neurons and Asthma Rats.

    abstract::Icariin is a main component of the Chinese medicinal plant Epimedium brevicornu Maxim, exhibits potent activity against inflammatory diseases. Our previous data demonstrated the valid bioactivity of icariin on mitigating rodent asthma. Endoplasmic reticulum (ER) stress and nuclear factor-κB (NF-κB) pathway were involv...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2019.01660

    authors: Liu J,Liu L,Sun J,Luo Q,Yan C,Zhang H,Liu F,Wei Y,Dong J

    更新日期:2020-01-31 00:00:00

  • Theranostic Attributes of Acoustic Cluster Therapy and Its Use for Enhancing the Effectiveness of Liposomal Doxorubicin Treatment of Human Triple Negative Breast Cancer in Mice.

    abstract:Introduction:Acoustic cluster therapy (ACT) comprises co-administration of a formulation containing microbubble/microdroplet clusters (PS101), together with a regular medicinal drug (e.g., a chemotherapeutic) and local ultrasound (US) insonation of the targeted pathological tissue (e.g., the tumor). PS101 is confined t...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2020.00075

    authors: Bush N,Healey A,Shah A,Box G,Kirkin V,Eccles S,Sontum PC,Kotopoulis S,Kvåle S,van Wamel A,Davies CL,Bamber J

    更新日期:2020-02-20 00:00:00

  • In Vivo Pharmacokinetic/Pharmacodynamic Profiles of Danofloxacin in Rabbits Infected With Salmonella typhimurium After Oral Administration.

    abstract::Salmonella typhimurium is a highly transmissible pathogen in rabbits that causes significant losses. Danofloxacin shows excellent efficacy against S. typhimurium infections. However, there are few reports of the pharmacokinetic/pharmacodynamic (PK/PD) modeling of danofloxacin against this pathogen. The aim of this stu...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2018.00391

    authors: Xiao X,Pei L,Jiang LJ,Lan WX,Xiao JY,Jiang YJ,Wang ZQ

    更新日期:2018-04-17 00:00:00

  • MetMaxStruct: A Tversky-Similarity-Based Strategy for Analysing the (Sub)Structural Similarities of Drugs and Endogenous Metabolites.

    abstract:BACKGROUND:Previous studies compared the molecular similarity of marketed drugs and endogenous human metabolites (endogenites), using a series of fingerprint-type encodings, variously ranked and clustered using the Tanimoto (Jaccard) similarity coefficient (TS). Because this gives equal weight to all parts of the encod...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2016.00266

    authors: O'Hagan S,Kell DB

    更新日期:2016-08-22 00:00:00

  • Integrating Strategies of Herbal Metabolomics, Network Pharmacology, and Experiment Validation to Investigate Frankincense Processing Effects.

    abstract::In-depth research on processing can promote the globalization of processed herbs. The purpose of this study is to propose an improved strategy for processing effect investigation. Frankincense and processed frankincense were used as research subjects. First, high-speed countercurrent chromatography (HSCCC) and prepara...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2018.01482

    authors: Ning Z,Wang C,Liu Y,Song Z,Ma X,Liang D,Liu Z,Lu A

    更新日期:2018-12-18 00:00:00

  • Sensorimotor gating impairments induced by MK-801 treatment may be reduced by tolerance effect and by familiarization in monkeys.

    abstract::Dizocilpine (MK-801) is a non-competitive NMDA antagonist that induces schizophreniclike effects. It is therefore widely used in experimental models of schizophrenia including prepulse inhibition (PPI) impairments in rodents. Nevertheless, MK-801 has never been tested in monkeys on a PPI paradigm. In order to evaluate...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2015.00204

    authors: Saletti PG,Maior RS,Hori E,Nishijo H,Tomaz C

    更新日期:2015-09-22 00:00:00

  • IRAP Inhibitors: M1-Aminopeptidase Family Inspiration.

    abstract::The insulin regulated aminopeptidase (IRAP) has been proposed as an important therapeutic target for indications including Alzheimer's disease and immune disorders. To date, a number of IRAP inhibitor designs have been investigated but the total number of molecules investigated remains quite small. As a member the M1 ...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章,评审

    doi:10.3389/fphar.2020.585930

    authors: Barlow N,Thompson PE

    更新日期:2020-09-25 00:00:00

  • Chemically Homogenous Compounds with Antagonistic Properties at All α1-Adrenoceptor Subtypes but not β1-Adrenoceptor Attenuate Adrenaline-Induced Arrhythmia in Rats.

    abstract::Studies proved that among all α1-adrenoceptors, cardiac myocytes functionally express only α1A- and α1B-subtype. Scientists indicated that α1A-subtype blockade might be beneficial in restoring normal heart rhythm. Therefore, we aimed to determine the role of α1-adrenoceptors subtypes (i.e., α1A and α1B) in antiarrhyth...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2016.00229

    authors: Pytka K,Lustyk K,Żmudzka E,Kotańska M,Siwek A,Zygmunt M,Dziedziczak A,Śniecikowska J,Olczyk A,Gałuszka A,Śmieja J,Waszkielewicz AM,Marona H,Filipek B,Sapa J,Mogilski S

    更新日期:2016-08-03 00:00:00

  • Monocytes, Macrophages, and Metabolic Disease in Atherosclerosis.

    abstract::Atherosclerotic cardiovascular disease (CVD) is a lipid-driven chronic inflammatory disease, in which macrophages are responsible for taking up these lipids and driving disease progression. Over the years, we and others have uncovered key pathways that regulate macrophage number/function and identified how metabolic d...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章,评审

    doi:10.3389/fphar.2019.00666

    authors: Flynn MC,Pernes G,Lee MKS,Nagareddy PR,Murphy AJ

    更新日期:2019-06-13 00:00:00

  • Cannabidiol Treatment for Refractory Epilepsies in Pediatrics.

    abstract::Cannabis extracts in oil are becoming increasingly available, and, during the last years, there has been growing public and scientific interest about therapeutic properties of these compounds for the treatment of several neurologic diseases, not just epilepsy. The discovered role of the endocannabinoid system in epile...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章,评审

    doi:10.3389/fphar.2020.586110

    authors: Raucci U,Pietrafusa N,Paolino MC,Di Nardo G,Villa MP,Pavone P,Terrin G,Specchio N,Striano P,Parisi P

    更新日期:2020-09-29 00:00:00

  • The interplay between iron accumulation, mitochondrial dysfunction, and inflammation during the execution step of neurodegenerative disorders.

    abstract::A growing set of observations points to mitochondrial dysfunction, iron accumulation, oxidative damage and chronic inflammation as common pathognomonic signs of a number of neurodegenerative diseases that includes Alzheimer's disease, Huntington disease, amyotrophic lateral sclerosis, Friedrich's ataxia and Parkinson'...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章,评审

    doi:10.3389/fphar.2014.00038

    authors: Urrutia PJ,Mena NP,Núñez MT

    更新日期:2014-03-10 00:00:00

  • Endothelin-1/Nitric Oxide Ratio as a Predictive Factor of Response to Therapy With Terlipressin and Albumin in Patients With Type-1 Hepatorenal Syndrome.

    abstract:Background and Purpose:Predictors of response to type-1 hepatorenal syndrome (HRS) therapy are urgently needed. This study's purpose is to evaluate the proposed predictors in these patients. Methods:Forty-two type-1 HRS patients with cirrhosis were treated with albumin and terlipressin. Clinical, biochemical, and demo...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2020.00009

    authors: Abdel-Razik A,Mousa N,Abdelsalam M,Abdelwahab A,Tawfik M,Tawfik AM,Hasan AS,Elhelaly R,El-Wakeel N,Eldars W

    更新日期:2020-01-31 00:00:00

  • Pathways Connecting Late-Life Depression and Dementia.

    abstract::Late-life depression is associated with significant cognitive impairment. Meta-analyses showed that depression is associated with an increased risk for Alzheimer's disease (AD) and it might be an etiological factor for AD. Since late-life depression is often connected with cognitive impairment and dementia is usually ...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章,评审

    doi:10.3389/fphar.2020.00279

    authors: Linnemann C,Lang UE

    更新日期:2020-03-13 00:00:00

  • Immunosuppressive Effects of Natural α,β-Unsaturated Carbonyl-Based Compounds, and Their Analogs and Derivatives, on Immune Cells: A Review.

    abstract::The immune system is complex and pervasive as it functions to prevent or limit infections in the human body. In a healthy organism, the immune system and the redox balance of immune cells maintain homeostasis within the body. The failure to maintain the balance may lead to impaired immune response and either over acti...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章,评审

    doi:10.3389/fphar.2017.00022

    authors: Arshad L,Jantan I,Bukhari SN,Haque MA

    更新日期:2017-01-30 00:00:00

  • Safety of Anticancer Agents Used in Children: A Focus on Their Off-Label Use Through Data From the Spontaneous Reporting System.

    abstract:Background:Among factors influencing the higher risk of developing unknown or rare adverse drug reactions (ADRs) among children and adolescents, there is the frequent off-label use of drugs that seems to be very common in pediatric oncological patients. Our study aim to collect and evaluate data on the safety profile o...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2020.00621

    authors: Mascolo A,Scavone C,Bertini M,Brusco S,Punzo F,Pota E,Di Martino M,Di Pinto D,Rossi F

    更新日期:2020-05-07 00:00:00

  • 1H NMR-Based Metabolomics Study of the Toxicological Effects in Rats Induced by "Renqing Mangjue" Pill, a Traditional Tibetan Medicine.

    abstract::"RenqingMangjue" pill (RMP), as an effective prescription of Traditional Tibetan Medicine (TTM), has been widely used in treating digestive diseases and ulcerative colitis for over a thousand years. In certain classical Tibetan Medicine, heavy metal may add as an active ingredient, but it may cause contamination unint...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2017.00602

    authors: Xu C,Rezeng C,Li J,Zhang L,Yan Y,Gao J,Wang Y,Li Z,Chen J

    更新日期:2017-09-04 00:00:00

  • Actionable Pharmacogenetic Variation in the Slovenian Genomic Database.

    abstract::Background: Genetic variability in some of the genes that affect absorption, distribution, metabolism, and elimination ("pharmacogenes") can significantly influence an individual's response to the drug and consequently the effectiveness of treatment and possible adverse drug events. The rapid development of sequencing...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2019.00240

    authors: Hočevar K,Maver A,Peterlin B

    更新日期:2019-03-14 00:00:00

  • A Novel Small Molecule GDNF Receptor RET Agonist, BT13, Promotes Neurite Growth from Sensory Neurons in Vitro and Attenuates Experimental Neuropathy in the Rat.

    abstract::Neuropathic pain caused by nerve damage is a common and severe class of chronic pain. Disease-modifying clinical therapies are needed as current treatments typically provide only symptomatic relief; show varying clinical efficacy; and most have significant adverse effects. One approach is targeting either neurotrophic...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2017.00365

    authors: Sidorova YA,Bespalov MM,Wong AW,Kambur O,Jokinen V,Lilius TO,Suleymanova I,Karelson G,Rauhala PV,Karelson M,Osborne PB,Keast JR,Kalso EA,Saarma M

    更新日期:2017-06-21 00:00:00

  • A Significant Association Between Rhein and Diabetic Nephropathy in Animals: A Systematic Review and Meta-Analysis.

    abstract::Background: Rhein is considered to have beneficial influence on diabetic nephropathy. Animal experiments suggested that the mechanisms of rhein against diabetic nephropathy may involve many processes, but the credibility of the evidence is unclear. Therefore, we conducted systematic review and meta-analysis of pre-cli...

    journal_title:Frontiers in pharmacology

    pub_type:

    doi:10.3389/fphar.2019.01473

    authors: Hu HC,Zheng LT,Yin HY,Tao Y,Luo XQ,Wei KS,Yin LP

    更新日期:2019-12-13 00:00:00

  • Metabolic Profiling of a CB2 Agonist, AM9338, Using LC-MS and Microcoil-NMR: Identification of a Novel Dihydroxy Adamantyl Metabolite.

    abstract::Adamantyl groups are key structural subunit commonly used in many marketed drugs targeting diseases ranging from viral infections to neurological disorders. The metabolic disposition of adamantyl compounds has been mostly studied using LC-MS based approaches. However, metabolite quantities isolated from biological pre...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2020.575691

    authors: Honrao C,Ma X,Kulkarni S,Joshi V,Malamas M,Zvonok A,Wood J,Strand D,Guo JJ,Makriyannis A

    更新日期:2020-09-30 00:00:00

  • Pyridoxamine Supplementation Effectively Reverses the Abnormal Phenotypes of Zebrafish Larvae With PNPO Deficiency.

    abstract::Neonatal epileptic encephalopathy (NEE), as a result of pyridoxine 5'-phosphate oxidase (PNPO) deficiency, is a rare neural disorder characterized by intractable seizures and usually leads to early infant death. The clinical phenotypes do not respond to antiepileptic drugs but are alleviated in most cases by giving la...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2019.01086

    authors: Chen PY,Tu HC,Schirch V,Safo MK,Fu TF

    更新日期:2019-09-20 00:00:00

  • Ophiopogonin D', a Natural Product From Radix Ophiopogonis, Induces in Vitro and in Vivo RIPK1-Dependent and Caspase-Independent Apoptotic Death in Androgen-Independent Human Prostate Cancer Cells.

    abstract::Objective: The purpose of this study was to evaluate the anticancer effects of Ophiopogonin D' (OPD', a natural product extracted from a traditional Chinese medicine (Radix Ophiopogonis) against androgen-independent prostate cancer cells and to explore the underlying molecular mechanism(s) of action. Methods: The CCK-...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2018.00432

    authors: Lu Z,Wang H,Zhu M,Song W,Wang J,Wu C,Kong Y,Guo J,Li N,Liu J,Li Y,Xu H

    更新日期:2018-04-30 00:00:00

  • MiR-409-3p Inhibits Cell Proliferation and Invasion of Osteosarcoma by Targeting Zinc-Finger E-Box-Binding Homeobox-1.

    abstract::Osteosarcoma (OS) is the most common bone cancer worldwide. There is evidence that microRNA-409 (miR-409-3p) is involved in tumorigenesis and cancer progression, however, its possible role in OS requires clarification. In the present study, we evaluated the expression level, clinical significance, and mode of action o...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章

    doi:10.3389/fphar.2019.00137

    authors: Wu L,Zhang Y,Huang Z,Gu H,Zhou K,Yin X,Xu J

    更新日期:2019-02-21 00:00:00

  • Animal-Free Chemical Safety Assessment.

    abstract::The exponential growth of the Internet of Things and the global popularity and remarkable decline in cost of the mobile phone is driving the digital transformation of medical practice. The rapidly maturing digital, non-medical world of mobile (wireless) devices, cloud computing and social networking is coalescing with...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章,评审

    doi:10.3389/fphar.2016.00218

    authors: Loizou GD

    更新日期:2016-07-21 00:00:00