Norditerpenoids with Selective Anti-Cholinesterase Activity from the Roots of Perovskia atriplicifolia Benth.

Abstract:

:Inhibition of cholinesterases remains one of a few available treatment strategies for neurodegenerative dementias such as Alzheimer's disease and related conditions. The current study was inspired by previous data on anticholinesterase properties of diterpenoids from Perovskia atriplicifolia and other Lamiaceae species. The acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition by the three new natural compounds-(1R,15R)-1-acetoxycryptotanshinone (1), (1R)-1-acetoxytanshinone IIA (2), and (15R)-1-oxoaegyptinone A (3)-as well as, new for this genus, isograndifoliol (4) were assessed. Three of these compounds exhibited profound inhibition of butyrylcholinesterase (BChE) and much weaker inhibition of acetylcholinesterase (AChE). All compounds (1-4) selectively inhibited BChE (IC50 = 2.4, 7.9, 50.8, and 0.9 µM, respectively), whereas only compounds 3 and 4 moderately inhibited AChE (IC50 329.8 µM and 342.9 µM). Molecular docking and in silico toxicology prediction studies were also performed on the active compounds. Natural oxygenated norditerpenoids from the traditional Central Asian medicinal plant P. atriplicifolia are selective BChE inhibitors. Their high potential makes them useful candidate molecules for further investigation as lead compounds in the development of a natural drug against dementia caused by neurodegenerative diseases.

journal_name

Int J Mol Sci

authors

Ślusarczyk S,Senol Deniz FS,Abel R,Pecio Ł,Pérez-Sánchez H,Cerón-Carrasco JP,den-Haan H,Banerjee P,Preissner R,Krzyżak E,Oleszek W,E Orhan I,Matkowski A

doi

10.3390/ijms21124475

subject

Has Abstract

pub_date

2020-06-23 00:00:00

issue

12

issn

1422-0067

pii

ijms21124475

journal_volume

21

pub_type

杂志文章
  • Cell adhesion and in vivo osseointegration of sandblasted/acid etched/anodized dental implants.

    abstract::The authors describe a new type of titanium (Ti) implant as a Modi-anodized (ANO) Ti implant, the surface of which was treated by sandblasting, acid etching (SLA), and anodized techniques. The aim of the present study was to evaluate the adhesion of MG-63 cells to Modi-ANO surface treated Ti in vitro and to investigat...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms160510324

    authors: Kim MH,Park K,Choi KH,Kim SH,Kim SE,Jeong CM,Huh JB

    更新日期:2015-05-06 00:00:00

  • Pharmacogenomics of Antibiotics.

    abstract::Although the introduction of antibiotics in medicine has resulted in one of the most successful events and in a major breakthrough to reduce morbidity and mortality caused by infectious disease, response to these agents is not always predictable, leading to differences in their efficacy, and sometimes to the occurrenc...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章,评审

    doi:10.3390/ijms21175975

    authors: Stocco G,Lucafò M,Decorti G

    更新日期:2020-08-19 00:00:00

  • The voltage-dependent anion channel 1 (AtVDAC1) negatively regulates plant cold responses during germination and seedling development in Arabidopsis and interacts with calcium sensor CBL1.

    abstract::The voltage-dependent anion channel (VDAC), a highly conserved major mitochondrial outer membrane protein, plays crucial roles in energy metabolism and metabolite transport. However, knowledge about the roles of the VDAC family in plants is limited. In this study, we investigated the expression pattern of VDAC1 in Ara...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms14010701

    authors: Li ZY,Xu ZS,He GY,Yang GX,Chen M,Li LC,Ma Y

    更新日期:2013-01-04 00:00:00

  • Regulation of miRNA expression by low-level laser therapy (LLLT) and photodynamic therapy (PDT).

    abstract::Applications of laser therapy, including low-level laser therapy (LLLT), phototherapy and photodynamic therapy (PDT), have been proven to be beneficial and relatively less invasive therapeutic modalities for numerous diseases and disease conditions. Using specific types of laser irradiation, specific cellular activiti...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms140713542

    authors: Kushibiki T,Hirasawa T,Okawa S,Ishihara M

    更新日期:2013-06-27 00:00:00

  • An Exploratory Pilot Study of Genetic Marker for IgE-Mediated Allergic Diseases with Expressions of FcεR1α and Cε.

    abstract::The high affinity immunoglobulin E (IgE) receptor-FcεR1 is mainly expressed on the surface of effector cells. Cross-linking of IgE Abs bound to FcεR1 by multi-valent antigens can induce the activation of these cells and the secretion of inflammatory mediators. Since FcεR1 plays a central role in the induction and main...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms16059504

    authors: Liao EC,Chang CY,Hsieh CW,Yu SJ,Yin SC,Tsai JJ

    更新日期:2015-04-27 00:00:00

  • The Triple Amino Acid Substitution TAP-IVS in the EPSPS Gene Confers High Glyphosate Resistance to the Superweed Amaranthus hybridus.

    abstract::The introduction of glyphosate-resistant (GR) crops revolutionized weed management; however, the improper use of this technology has selected for a wide range of weeds resistant to glyphosate, referred to as superweeds. We characterized the high glyphosate resistance level of an Amaranthus hybridus population (GRH)-a ...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms20102396

    authors: García MJ,Palma-Bautista C,Rojano-Delgado AM,Bracamonte E,Portugal J,Alcántara-de la Cruz R,De Prado R

    更新日期:2019-05-15 00:00:00

  • A new approach on estimation of solubility and n-octanol/water partition coefficient for organohalogen compounds.

    abstract::The aqueous solubility (logW) and n-octanol/water partition coefficient (logP(OW)) are important properties for pharmacology, toxicology and medicinal chemistry. Based on an understanding of the dissolution process, the frontier orbital interaction model was suggested in the present paper to describe the solvent-solut...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms9060962

    authors: Gao S,Cao C

    更新日期:2008-06-01 00:00:00

  • Protective Effects of Peroxiredoxin 4 (PRDX4) on Cholestatic Liver Injury.

    abstract::Accumulating evidence indicates that oxidative stress plays a critical role in initiating the progression of inflammatory and fibrotic liver diseases, including cholestatic hepatitis. Peroxiredoxin 4 (PRDX4) is a secretory antioxidase that protects against oxidative damage by scavenging reactive oxygen species (ROS) i...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms19092509

    authors: Zhang J,Guo X,Hamada T,Yokoyama S,Nakamura Y,Zheng J,Kurose N,Ishigaki Y,Uramoto H,Tanimoto A,Yamada S

    更新日期:2018-08-24 00:00:00

  • A Single Nucleotide Polymorphism near the CYP17A1 Gene Is Associated with Left Ventricular Mass in Hypertensive Patients under Pharmacotherapy.

    abstract::Cytochrome P450 17A1 (CYP17A1) catalyses the formation and metabolism of steroid hormones. They are involved in blood pressure (BP) regulation and in the pathogenesis of left ventricular hypertrophy. Therefore, altered function of CYP17A1 due to genetic variants may influence BP and left ventricular mass. Notably, gen...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms160817456

    authors: Huber M,Lezius S,Reibis R,Treszl A,Kujawinska D,Jakob S,Wegscheider K,Völler H,Kreutz R

    更新日期:2015-07-30 00:00:00

  • Overview of Epstein-Barr-Virus-Associated Gastric Cancer Correlated with Prognostic Classification and Development of Therapeutic Options.

    abstract::Gastric cancer (GC) is a deadly disease with poor prognosis that is characterized by heterogeneity. New classifications based on histologic features, genotypes, and molecular phenotypes, for example, the Cancer Genome Atlas subtypes and those by the Asian Cancer Research Group, help understand the carcinogenic differe...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章,评审

    doi:10.3390/ijms21249400

    authors: Re V,Brisotto G,Repetto O,De Zorzi M,Caggiari L,Zanussi S,Alessandrini L,Canzonieri V,Miolo G,Puglisi F,Belluco C,Steffan A,Cannizzaro R

    更新日期:2020-12-10 00:00:00

  • Expanding the Toolkit of Fluorescent Biosensors for Studying Mitogen Activated Protein Kinases in Plants.

    abstract::Mitogen-activated protein kinases (MAPKs) are key regulators of numerous biological processes in plants. To better understand the mechanisms by which these kinases function, high resolution measurement of MAPK activation kinetics in different biological contexts would be beneficial. One method to measure MAPK activati...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms21155350

    authors: Seitz K,Krysan PJ

    更新日期:2020-07-28 00:00:00

  • RAGE Signaling in Melanoma Tumors.

    abstract::Despite recent progresses in its treatment, malignant cutaneous melanoma remains a cancer with very poor prognosis. Emerging evidences suggest that the receptor for advance glycation end products (RAGE) plays a key role in melanoma progression through its activation in both cancer and stromal cells. In tumors, RAGE ac...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章,评审

    doi:10.3390/ijms21238989

    authors: Olaoba OT,Kadasah S,Vetter SW,Leclerc E

    更新日期:2020-11-26 00:00:00

  • Lower Exposure to Busulfan Allows for Stable Engraftment of Donor Hematopoietic Stem Cells in Children with Mucopolysaccharidosis Type I: A Case Report of Four Patients.

    abstract::Busulfan is an alkylating agent routinely used in conditioning regimens prior to allogeneic hematopoietic cell transplantation (HCT) for various nonmalignant disorders, including inborn errors of metabolism. The combination of model-based dosing and therapeutic drug monitoring (TDM) of busulfan pharmacokinetics (PK) t...

    journal_title:International journal of molecular sciences

    pub_type:

    doi:10.3390/ijms21165634

    authors: Shukla P,Dvorak CC,Long-Boyle J,Kharbanda S

    更新日期:2020-08-06 00:00:00

  • Surface Modification by Nano-Structures Reduces Viable Bacterial Biofilm in Aerobic and Anaerobic Environments.

    abstract::Bacterial biofilm formation on wet surfaces represents a significant problem in medicine and environmental sciences. One of the strategies to prevent or eliminate surface adhesion of organisms is surface modification and coating. However, the current coating technologies possess several drawbacks, including limited du...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms21197370

    authors: Ya'ari S,Halperin-Sternfeld M,Rosin B,Adler-Abramovich L

    更新日期:2020-10-06 00:00:00

  • The Constipation-Relieving Property of d-Tagatose by Modulating the Composition of Gut Microbiota.

    abstract::d-tagatose, a monosaccharide as well as a dietary supplement, has been reported as having a wide range of applicability in the food industry, however, the prebiotic activity, anticonstipation effects, and related mechanisms are still unclear. In this study, using the loperamide-induced constipation Kunming mice as the...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms20225721

    authors: Liang YX,Wen P,Wang Y,OuYang DM,Wang D,Chen YZ,Song Y,Deng J,Sun YM,Wang H

    更新日期:2019-11-14 00:00:00

  • Real-Time 3D Imaging and Inhibition Analysis of Various Amyloid Aggregations Using Quantum Dots.

    abstract::Amyloidosis refers to aggregates of protein that accumulate and are deposited as amyloid fibrils into plaques. When these are detected in organs, they are the main hallmark of Alzheimer's disease, Parkinson's disease, and other related diseases. Recent medical advances have shown that many precursors and proteins can ...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms21061978

    authors: Lin X,Galaqin N,Tainaka R,Shimamori K,Kuragano M,Noguchi TQP,Tokuraku K

    更新日期:2020-03-13 00:00:00

  • A Novel Mutation of the NARROW LEAF 1 Gene Adversely Affects Plant Architecture in Rice (Oryza sativa L.).

    abstract::Plant architecture is critical for enhancing the adaptability and productivity of crop plants. Mutants with an altered plant architecture allow researchers to elucidate the genetic network and the underlying mechanisms. In this study, we characterized a novel nal1 rice mutant with short height, small panicle, and narr...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms21218106

    authors: Subudhi PK,Garcia RS,Coronejo S,De Leon TB

    更新日期:2020-10-30 00:00:00

  • l-Glutamine Attenuates Apoptosis Induced by Endoplasmic Reticulum Stress by Activating the IRE1α-XBP1 Axis in IPEC-J2: A Novel Mechanism of l-Glutamine in Promoting Intestinal Health.

    abstract::Intestinal absorption and barrier malfunctions are associated with endoplasmic reticulum stress (ERS) in the intestine. We induced ERS by exposing the intestinal porcine epithelial cell line J2 (IPEC-J2) to tunicamycin (TUNI) to explore the potential of l-glutamine to reduce ERS-induced apoptosis. Our experiments demo...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms18122617

    authors: Jiang Q,Chen J,Liu S,Liu G,Yao K,Yin Y

    更新日期:2017-12-05 00:00:00

  • Adult Renal Stem/Progenitor Cells Can Modulate T Regulatory Cells and Double Negative T Cells.

    abstract::Adult Renal Stem/Progenitor Cells (ARPCs) have been recently identified in the human kidney and several studies show their active role in kidney repair processes during acute or chronic injury. However, little is known about their immunomodulatory properties and their capacity to regulate specific T cell subpopulation...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms22010274

    authors: Curci C,Picerno A,Chaoul N,Stasi A,De Palma G,Franzin R,Pontrelli P,Castellano G,Pertosa GB,Macchia L,Di Lorenzo VF,Sabbà C,Gallone A,Gesualdo L,Sallustio F

    更新日期:2020-12-29 00:00:00

  • Combinatorial Drug Treatments Reveal Promising Anticytomegaloviral Profiles for Clinically Relevant Pharmaceutical Kinase Inhibitors (PKIs).

    abstract::Human cytomegalovirus (HCMV) is a human pathogenic herpesvirus associated with a variety of clinical symptoms. Current antiviral therapy is not always effective, so that improved drug classes and drug-targeting strategies are needed. Particularly host-directed antivirals, including pharmaceutical kinase inhibitors (PK...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms22020575

    authors: Wild M,Kicuntod J,Seyler L,Wangen C,Bertzbach LD,Conradie AM,Kaufer BB,Wagner S,Michel D,Eickhoff J,Tsogoeva SB,Bäuerle T,Hahn F,Marschall M

    更新日期:2021-01-08 00:00:00

  • Molecular Signature of Indeterminate Thyroid Lesions: Current Methods to Improve Fine Needle Aspiration Cytology (FNAC) Diagnosis.

    abstract::Fine needle aspiration cytology (FNAC) represents the gold standard for determining the nature of thyroid nodules. It is a reliable method with good sensitivity and specificity. However, indeterminate lesions remain a diagnostic challenge and researchers have contributed molecular markers to search for in cytological ...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章,评审

    doi:10.3390/ijms18040775

    authors: Cantara S,Marzocchi C,Pilli T,Cardinale S,Forleo R,Castagna MG,Pacini F

    更新日期:2017-04-06 00:00:00

  • Regulating the Regulators: The Role of Histone Deacetylase 1 (HDAC1) in Erythropoiesis.

    abstract::Histone deacetylases (HDACs) play important roles in transcriptional regulation in eukaryotic cells. Class I deacetylase HDAC1/2 often associates with repressor complexes, such as Sin3 (Switch Independent 3), NuRD (Nucleosome remodeling and deacetylase) and CoREST (Corepressor of RE1 silencing transcription factor) co...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章,评审

    doi:10.3390/ijms21228460

    authors: Kim MY,Yan B,Huang S,Qiu Y

    更新日期:2020-11-11 00:00:00

  • Single Crystal FLIM Characterization of Clofazimine Loaded in Silica-Based Mesoporous Materials and Zeolites.

    abstract::Clofazimine (CLZ) is an effective antibiotic used against a wide spectrum of Gram-positive bacteria and leprosy. One of its main drawbacks is its poor solubility in water. Silica based materials are used as drug delivery carriers that can increase the solubility of different hydrophobic drugs. Here, we studied how the...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms20122859

    authors: Angiolini L,Cohen B,Douhal A

    更新日期:2019-06-12 00:00:00

  • Interventional Left Atrial Appendage Closure Affects the Metabolism of Acylcarnitines.

    abstract:BACKGROUND:Left atrial appendage closure (LAAC) represents the interventional alternative to oral anticoagulation for stroke prevention in atrial fibrillation (AF). The metabolism of acylcarnitines was shown to affect cardiovascular diseases. This study evaluates the influence of successful LAAC on the metabolism of ac...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms19020500

    authors: Fastner C,Behnes M,Sartorius B,Wenke A,Lang S,Yücel G,Sattler K,Rusnak J,Saleh A,Barth C,Mashayekhi K,Hoffmann U,Borggrefe M,Akin I

    更新日期:2018-02-07 00:00:00

  • Roles Played by Biomarkers of Kidney Injury in Patients with Upper Urinary Tract Obstruction.

    abstract::Partial or complete obstruction of the urinary tract is a common and challenging urological condition caused by a variety of conditions, including ureteral calculi, ureteral pelvic junction obstruction, ureteral stricture, and malignant ureteral obstruction. The condition, which may develop in patients of any age, ind...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章,评审

    doi:10.3390/ijms21155490

    authors: Washino S,Hosohata K,Miyagawa T

    更新日期:2020-07-31 00:00:00

  • Discrimination of CpG Methylation Status and Nucleotide Differences in Tissue Specimen DNA by Oligoribonucleotide Interference-PCR.

    abstract::Oligoribonucleotide (ORN) interference-PCR (ORNi-PCR) is a method in which PCR amplification of a target sequence is inhibited in a sequence-specific manner by the hybridization of an ORN with the target sequence. Previously, we reported that ORNi-PCR could detect nucleotide mutations in DNA purified from cultured can...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms21145119

    authors: Shimizu T,Fujita T,Fukushi S,Horino Y,Fujii H

    更新日期:2020-07-20 00:00:00

  • Therapeutic Application of Drug-Conjugated HER2 Oligobody (HER2-DOligobody).

    abstract::Antibody drug conjugates (ADCs), consisting of a cancer-specific antibody and cytotoxic payload, are shown to be a potent class of anticancer therapeutics, with enhanced therapeutic efficacy and reduced "off-target" side effects. However, the therapeutic window of ADCs is narrowed by problems such as difficulty in sit...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms21093286

    authors: Kim HJ,Sung HJ,Lee YM,Choi SI,Kim YH,Heo K,Kim IH

    更新日期:2020-05-06 00:00:00

  • In Silico Finding of Key Interaction Mediated α3β4 and α7 Nicotinic Acetylcholine Receptor Ligand Selectivity of Quinuclidine-Triazole Chemotype.

    abstract::The selective binding of six (S)-quinuclidine-triazoles and their (R)-enantiomers to nicotinic acetylcholine receptor (nAChR) subtypes α3β4 and α7, respectively, were analyzed by in silico docking to provide the insight into the molecular basis for the observed stereospecific subtype discrimination. Homology modeling ...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章

    doi:10.3390/ijms21176189

    authors: Arunrungvichian K,Chongruchiroj S,Sarasamkan J,Schüürmann G,Brust P,Vajragupta O

    更新日期:2020-08-27 00:00:00

  • Role of Forkhead Box O Transcription Factors in Oxidative Stress-Induced Chondrocyte Dysfunction: Possible Therapeutic Target for Osteoarthritis?

    abstract::Chondrocyte dysfunction occurs during the development of osteoarthritis (OA), typically resulting from a deleterious increase in oxidative stress. Accordingly, strategies for arresting oxidative stress-induced chondrocyte dysfunction may lead to new potential therapeutic targets for OA treatment. Forkhead box O (FoxO)...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章,评审

    doi:10.3390/ijms19123794

    authors: Wang R,Zhang S,Previn R,Chen D,Jin Y,Zhou G

    更新日期:2018-11-28 00:00:00

  • Characteristics and Cryopreservation of Semen of Sex-Reversed Females of Salmonid Fish.

    abstract::Sex reversal has been used as a breeding strategy by salmonid fish to produce genetically and phenotypically single sex populations. Production of all-female fish has great importance for the creation of monosex female triploids of salmonid fish, which are valued for their sterility, lack of female maturation, and lar...

    journal_title:International journal of molecular sciences

    pub_type: 杂志文章,评审

    doi:10.3390/ijms22020964

    authors: Judycka S,Nynca J,Hliwa P,Ciereszko A

    更新日期:2021-01-19 00:00:00