scholarly journals The activity of peroxidases and superoxide dismutases in transgenic phosphinothricin-resistant lotus corniculatus shoots

2010 ◽  
Vol 62 (4) ◽  
pp. 1063-1070 ◽  
Author(s):  
Jelena Savic ◽  
Jelena Platisa ◽  
M. Dragicevic ◽  
Radomirka Nikolic ◽  
Nevena Mitic ◽  
...  
Keyword(s):  
Antioxidative Enzymes ◽  
Active Compound ◽  
Genetically Modified ◽  
Lotus Corniculatus ◽  
Superoxide Dismutases ◽  
Herbicide Application ◽  
Physiological Processes ◽  
Oxidative Balance ◽  
Selective Herbicide

The aim of this study was to investigate the effect of the non-selective herbicide Basta?, with phosphinothricin (PPT) as active compound, on antioxidative enzymes in transgenic PPT-resistant Lotus corniculatus cv. Bokor shoots grown under in vitro conditions. Analysis of peroxidases (POD) and superoxide dismutases (SOD) showed that the activity of these enzymes was affected by herbicide application more in control PPT-sensitive than in transformed resistant shoots. These results confirmed the capacity of genetically modified resistant shoots to reduce the influence of PPT on the physiological processes and disturbance of oxidative balance in cells.

Relations between Structure and Antituberculotic Activity of 4-Alkoxybenzoic Acids

1993 ◽  
Vol 58 (1) ◽  
pp. 191-196 ◽  
Author(s):  
Karel Waisser ◽  
Jiří Kuneš ◽  
Jiří Klimeš ◽  
Miroslav Polášek ◽  
Želmíra Odlerová
Keyword(s):  
Active Compound ◽  
Antimycobacterial Activity ◽  
Methoxybenzoic Acid

Antimycobacterial activity of a series of alkoxybenzoic acids including 4-methoxybenzoic acid (II), 4-ethoxybenzoic acid (III), 4-propoxybenzoic acid (IV), 4-butoxybenzoic acid (V), 4-pentoxybenzoic acid (VI), 4-allyloxybenzoic acid (IX), 4-isopropoxybenzoic acid (VII), 4-isobutoxybenzoic acid (VIII) and 4-benzyloxybenzoic acid (X) has been determined and found to increase with the lipophilicity of the compounds expressed by the corresponding HPLC capacity factors. Also determined were the pKa values of the compounds mentioned. The most active compound, 4-pentoxybenzoic acid (VI), is comparable with commercial antituberculotics when tested in vitro.

scholarly journals Effects of Substituents on Photophysical and CO-Photoreleasing Properties of 2,6-Substituted meso-Carboxy BODIPY Derivatives

Chemistry ◽  
2021 ◽  
Vol 3 (1) ◽  
pp. 238-255
Author(s):  
Esther M. Sánchez-Carnerero ◽  
Marina Russo ◽  
Andreas Jakob ◽  
Lucie Muchová ◽  
Libor Vítek ◽  
...  
Keyword(s):  
Carbon Monoxide ◽  
Absorption Spectra ◽  
Wavelength Range ◽  
Toxic Effects ◽  
Biological Research ◽  
In Vitro Experiments ◽  
Vast Array ◽  
Physiological Processes ◽  
Photochemical Properties

Carbon monoxide (CO) is an endogenously produced signaling molecule involved in the control of a vast array of physiological processes. One of the strategies to administer therapeutic amounts of CO is the precise spatial and temporal control over its release from photoactivatable CO-releasing molecules (photoCORMs). Here we present the synthesis and photophysical and photochemical properties of a small library of meso-carboxy BODIPY derivatives bearing different substituents at positions 2 and 6. We show that the nature of substituents has a major impact on both their photophysics and the efficiency of CO photorelease. CO was found to be efficiently released from π-extended 2,6-arylethynyl BODIPY derivatives possessing absorption spectra shifted to a more biologically desirable wavelength range. Selected photoCORMs were subjected to in vitro experiments that did not reveal any serious toxic effects, suggesting their potential for further biological research.

Effects of Maternal Nutrient Restriction During Gestation on LH Production in the Female Bovine Fetus

2021 ◽  
Vol 99 (Supplement_2) ◽  
pp. 25-26
Author(s):  
Sterling H Fahey ◽  
Sarah West ◽  
John M Long ◽  
Carey Satterfield ◽  
Rodolfo C Cardoso
Keyword(s):  
Protein Content ◽  
Fetal Development ◽  
Monozygotic Twins ◽  
Late Gestation ◽  
Nutrient Restriction ◽  
Western Blots ◽  
Physiological Processes ◽  
Individual Potential ◽  
The Individual

Abstract Gestational nutrient restriction causes epigenetic and phenotypic changes that affect multiple physiological processes in the offspring. Gonadotropes, the cells in the anterior pituitary that secrete luteinizing hormone (LH) and follicle-stimulating hormone (FSH), are particularly sensitive to nutritional changes during fetal development. Our objective herein was to investigate the effects of gestational nutrient restriction on LH protein content and number of gonadotropes in the fetal bovine pituitary. We hypothesized that moderate nutrient restriction during mid to late gestation decreases pituitary LH production, which is associated with a reduced number of gonadotropes. Embryos were produced in vitro with X-bearing semen from a single sire then split to generate monozygotic twins. Each identical twin was transferred to a virgin dam yielding four sets of female twins. At gestational d 158, the dams were randomly assigned into two groups, one fed 100% NRC requirements (control) and the other fed 70% of NRC requirements (restricted) during the last trimester of gestation, ensuring each pair of twins had one twin in each group. At gestational d 265, the fetuses (n = 4/group) were euthanized by barbiturate overdose, and the pituitaries were collected. Western blots were performed using an ovine LH-specific antibody (Dr. A.F. Parlow, NIDDK). The total LH protein content in the pituitary tended to be decreased in the restricted fetuses compared to controls (P < 0.10). However, immunohistochemistry analysis of the pituitary did not reveal any significant changes in the total number of LH-positive cells (control = 460±23 cells/0.5 mm2; restricted = 496±45 cells/0.5 mm2, P = 0.58). In conclusion, while maternal nutrient restriction during gestation resulted in a trend of reduced LH content in the fetal pituitary, immunohistological findings suggest that these changes are likely related to the individual potential of each gonadotrope to produce LH, rather than alterations in cell differentiation during fetal development.

scholarly journals Glucocorticoid resistance conferring mutation in the C-terminus of GR alters the receptor conformational dynamics

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Anna Kaziales ◽  
Florian Rührnößl ◽  
Klaus Richter
Keyword(s):  
Glucocorticoid Receptor ◽  
Steroid Hormones ◽  
In Silico ◽  
Conformational Dynamics ◽  
Glucocorticoid Resistance ◽  
Physiological Processes ◽  
C Terminus ◽  
Hsp90 Chaperone ◽  
In Silico Methods

AbstractThe glucocorticoid receptor is a key regulator of essential physiological processes, which under the control of the Hsp90 chaperone machinery, binds to steroid hormones and steroid-like molecules and in a rather complicated and elusive response, regulates a set of glucocorticoid responsive genes. We here examine a human glucocorticoid receptor variant, harboring a point mutation in the last C-terminal residues, L773P, that was associated to Primary Generalized Glucocorticoid Resistance, a condition originating from decreased affinity to hormone, impairing one or multiple aspects of GR action. Using in vitro and in silico methods, we assign the conformational consequences of this mutation to particular GR elements and report on the altered receptor properties regarding its binding to dexamethasone, a NCOA-2 coactivator-derived peptide, DNA, and importantly, its interaction with the chaperone machinery of Hsp90.

scholarly journals Point-Substitution of Phenylalanine Residues of 26RFa Neuropeptide: A Structure-Activity Relationship Study

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4312
Author(s):  
Benjamin Lefranc ◽  
Karima Alim ◽  
Cindy Neveu ◽  
Olivier Le Marec ◽  
Christophe Dubessy ◽  
...  
Keyword(s):  
Receptor Activation ◽  
Pharmacological Profile ◽  
Acid Moiety ◽  
Structural Determinants ◽  
Physiological Processes ◽  
Structure Activity ◽  
Peptide Derivatives ◽  
Targeting Peptide ◽  
G Protein Coupled

26RFa is a neuropeptide that activates the rhodopsin-like G protein-coupled receptor QRFPR/GPR103. This peptidergic system is involved in the regulation of a wide array of physiological processes including feeding behavior and glucose homeostasis. Herein, the pharmacological profile of a homogenous library of QRFPR-targeting peptide derivatives was investigated in vitro on human QRFPR-transfected cells with the aim to provide possible insights into the structural determinants of the Phe residues to govern receptor activation. Our work advocates to include in next generations of 26RFa(20–26)-based QRFPR agonists effective substitutions for each Phe unit, i.e., replacement of the Phe22 residue by a constrained 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid moiety, and substitution of both Phe24 and Phe26 by their para-chloro counterpart. Taken as a whole, this study emphasizes that optimized modifications in the C-terminal part of 26RFa are mandatory to design selective and potent peptide agonists for human QRFPR.

scholarly journals DPP3/CDK1 contributes to the progression of colorectal cancer through regulating cell proliferation, cell apoptosis, and cell migration

2021 ◽  
Vol 12 (6) ◽  
Author(s):  
Yixin Tong ◽  
Yuan Huang ◽  
Yuchao Zhang ◽  
Xiangtai Zeng ◽  
Mei Yan ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Cell Proliferation ◽  
Cell Migration ◽  
Cell Apoptosis ◽  
Downstream Target ◽  
Normal Tissues ◽  
Physiological Processes ◽  
Mutual Regulation

AbstractAt present, colorectal cancer (CRC) has become a serious threat to human health in the world. Dipeptidyl peptidase 3 (DPP3) is a zinc-dependent hydrolase that may be involved in several physiological processes. However, whether DPP3 affects the development and progression of CRC remains a mystery. This study is the first to demonstrate the role of DPP3 in CRC. Firstly, the results of immunohistochemistry analysis showed the upregulation of DPP3 in CRC tissues compared with normal tissues, which is statistically analyzed to be positively correlated with lymphatic metastasis, pathological stage, positive number of lymph nodes. Moreover, the high expression of DPP3 predicts poor prognosis in CRC patients. In addition, the results of cell dysfunction experiments clarified that the downregulation of DPP3 significantly inhibited cell proliferation, colony formation, cell migration, and promoted apoptosis in vitro. DPP3 depletion could induce cell apoptosis by upregulating the expression of BID, BIM, Caspase3, Caspase8, HSP60, p21, p27, p53, and SMAC. In addition, downregulation of DPP3 can reduce tumorigenicity of CRC cells in vivo. Furthermore, CDK1 is determined to be a downstream target of DPP3-mediated regulation of CRC by RNA-seq, qPCR, and WB. The interaction between DPP3 and CDK1 shows mutual regulation. Specifically, downregulation of DPP3 can accentuate the effects of CDK1 knockdown on the function of CRC cells. Overexpression of CDK1 alleviates the inhibitory effects of DPP3 knockdown in CRC cells. In summary, DPP3 has oncogene-like functions in the development and progression of CRC by targeting CDK1, which may be an effective molecular target for the prognosis and treatment of CRC.

scholarly journals Disruption of inositol biosynthesis through targeted mutagenesis in Dictyostelium discoideum: generation and characterization of inositol-auxotrophic mutants

2006 ◽  
Vol 397 (3) ◽  
pp. 509-518 ◽  
Author(s):  
Andreas Fischbach ◽  
Stephan Adelt ◽  
Alexander Müller ◽  
Günter Vogel
Keyword(s):  
Dictyostelium Discoideum ◽  
Genetic Manipulation ◽  
Inositol Phosphate ◽  
Targeted Mutagenesis ◽  
Inositol Polyphosphate ◽  
Fluid Medium ◽  
Physiological Processes ◽  
Evolutionarily Conserved ◽  
Cellular Slime

myo-Inositol and its downstream metabolites participate in diverse physiological processes. Nevertheless, considering their variety, it is likely that additional roles are yet to be uncovered. Biosynthesis of myo-inositol takes place via an evolutionarily conserved metabolic pathway and is strictly dependent on inositol-3-phosphate synthase (EC 5.5.1.4). Genetic manipulation of this enzyme will disrupt the cellular inositol supply. Two methods, based on gene deletion and antisense strategy, were used to generate mutants of the cellular slime mould Dictyostelium discoideum. These mutants are inositol-auxotrophic and show phenotypic changes under inositol starvation. One remarkable attribute is their inability to live by phagocytosis of bacteria, which is the exclusive nutrient source in their natural environment. Cultivated on fluid medium, the mutants lose their viability when deprived of inositol for longer than 24 h. Here, we report a study of the alterations in the first 24 h in cellular inositol, inositol phosphate and phosphoinositide concentrations, whereby a rapidly accumulating phosphorylated compound was detected. After its identification as 2,3-BPG (2,3-bisphosphoglycerate), evidence could be found that the internal disturbances of inositol homoeostasis trigger the accumulation. In a first attempt to characterize this as a physiologically relevant response, the efficient in vitro inhibition of a D. discoideum inositol-polyphosphate 5-phosphatase (EC 3.1.3.56) by 2,3-BPG is presented.

scholarly journals Differential Processing of Propeptide Inhibitors of Rap Phosphatases in Bacillus subtilis

2000 ◽  
Vol 182 (2) ◽  
pp. 303-310 ◽  
Author(s):  
Min Jiang ◽  
Roberto Grau ◽  
Marta Perego
Keyword(s):  
Bacillus Subtilis ◽  
Phosphatase Activity ◽  
Response Regulators ◽  
Histidine Kinases ◽  
Physiological Processes ◽  
Carboxy Terminal Domain ◽  
Activation Level ◽  
Sporulation Initiation ◽  
Carboxy Terminal

ABSTRACT In the phosphorelay signal transduction system for sporulation initiation in Bacillus subtilis, the opposing activities of histidine kinases and aspartyl phosphate phosphatases determine the cell's decision whether to continue with vegetative growth or to initiate the differentiation process. Regulated dephosphorylation of the Spo0A and Spo0F response regulators allows a variety of negative signals from physiological processes that are antithetical to sporulation to impact on the activation level of the phosphorelay. Spo0F∼P is the known target of two related phosphatases, RapA and RapB. In addition to RapA and RapB, a third member of the Rap family of phosphatases, RapE, specifically dephosphorylated the Spo0F∼P intermediate in response to competence development. RapE phosphatase activity was found to be controlled by a pentapeptide (SRNVT) generated from within the carboxy-terminal domain of the phrE gene product. A synthetic PhrE pentapeptide could (i) complement the sporulation deficiency caused by deregulated RapE activity of aphrE mutant and (ii) inhibit RapE-dependent dephosphorylation of Spo0F∼P in in vitro experiments. The PhrE pentapeptide did not inhibit the phosphatase activity of RapA and RapB. These results confirm previous conclusions that the specificity for recognition of the target phosphatase is contained within the amino acid sequence of the pentapeptide inhibitor.

scholarly journals In Vitro Activities of DC-159a, a Novel Fluoroquinolone, against Mycobacterium Species

2010 ◽  
Vol 54 (6) ◽  
pp. 2684-2686 ◽  
Author(s):  
Areeya Disratthakit ◽  
Norio Doi
Keyword(s):  
Active Compound ◽  
Nontuberculous Mycobacteria ◽  
Multidrug Resistant ◽  
Mycobacterium Species

ABSTRACT The in vitro activities of DC-159a against seven species of Mycobacterium were compared with moxifloxacin, gatifloxacin, levofloxacin, and rifampin. DC-159a was the most active compound against quinolone-resistant multidrug-resistant M. tuberculosis (MIC90, 0.5 μg/ml) as well as drug-susceptible isolates (MIC90, 0.06 μg/ml). The anti-tubercle bacilli activity of DC-159a was 4- to 32-fold more potent than those of currently available quinolones. DC-159a also demonstrated the highest activities against clinically important nontuberculous mycobacteria.

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