scholarly journals Search for the optimal mass profile of neuropeptides for the implementation of antihypoxic and activating actions

2020 ◽  
Author(s):  
Evgeny B. Shustov ◽  
Dmitry Y. Ivkin ◽  
Arina S. Ivkina ◽  
Alexey E. Kim ◽  
Stanislav L. Lublin ◽  
...  
Keyword(s):  
Biological Activity ◽  
Forced Swim Test ◽  
Biological Effects ◽  
Internal Standard ◽  
Mass Range ◽  
The Body ◽  
Antihypoxic Activity ◽  
Critical Height ◽  
Activity Increase ◽  
Peptide Complexes

In this study, the dependence of the pharmacological effects of neurotropic peptides of natural and synthetic origin on their structure was studied in laboratory rats. First, the study of the relative molecular profiles of peptide complexes was carried out using HPLC (gel-penetrating chromatography) with an internal standard. Then peptide complexes were administered to animals rectal and verified their biological activity on two independent models antihypoxic activity (method of altitude the lift timing of the animal's life at a critical height) and the model of assessment of physical performance (time of forced swim test of animals with a load of 10% of the body weight to failure). The obtained data on biological activity (increase) were compared with the features of the structure of peptides. To assess the effect of drug doses on their activity, a single-factor analysis of variance was performed. It has been shown that antihypoxic activity and performance stimulation are more or less inherent in all the studied peptide preparations, and are dose-dependent and related to the features of the molecular mass distribution of peptide components. It was also found that the specific antihypoxic activity of peptide preparations from brain tissues is associated with components having a mass range from 5 to 10 kDa. The optimal proportions of the peptide components for the implementation of biological activity by mass ranges were determined. In addition, the chromatographic characteristics (molecular weight distribution over mass ranges) of natural neuropeptide complexes can be used to predict the severity of their biological effects.

Current Advances in the Biological Activity of Polysaccharides in Dendrobium with Intriguing Therapeutic Potential

2018 ◽  
Vol 25 (14) ◽  
pp. 1663-1681 ◽  
Author(s):  
Chun-Ting Lee ◽  
Heng-Chun Kuo ◽  
Yung-Hsiang Chen ◽  
Ming-Yen Tsai
Keyword(s):  
Biological Activity ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Biological Effects ◽  
Herbal Medicines ◽  
Research Field ◽  
Protective Effects ◽  
Pharmacological Effects ◽  
The Family ◽  
Anti Tumor Activity

The polysaccharides in many plants are attracting worldwide attention because of their biological activities and medical properties, such as anti-viral, anti-oxidative, antichronic inflammation, anti-hypertensive, immunomodulation, and neuron-protective effects, as well as anti-tumor activity. Denodrobium species, a genus of the family orchidaceae, have been used as herbal medicines for hundreds of years in China due to their pharmacological effects. These effects include nourishing the Yin, supplementing the stomach, increasing body fluids, and clearing heat. Recently, numerous researchers have investigated possible active compounds in Denodrobium species, such as lectins, phenanthrenes, alkaloids, trigonopol A, and polysaccharides. Unlike those of other plants, the biological effects of polysaccharides in Dendrobium are a novel research field. In this review, we focus on these novel findings to give readers an overall picture of the intriguing therapeutic potential of polysaccharides in Dendrobium, especially those of the four commonly-used Denodrobium species: D. huoshanense, D. offininale, D. nobile, and D. chrysotoxum.

Biological Activity of Trans-Membrane Anion Carriers

2018 ◽  
Vol 25 (30) ◽  
pp. 3560-3576 ◽  
Author(s):  
Massimo Tosolini ◽  
Paolo Pengo ◽  
Paolo Tecilla
Keyword(s):  
Biological Activity ◽  
Membrane Transport ◽  
Anticancer Agents ◽  
Biological Effects ◽  
Structure Activity Relationship ◽  
New Drugs ◽  
Activity Relationship ◽  
Anion Channels ◽  
Cellular Homeostasis ◽  
Structure Activity

Natural and synthetic anionophores promote the trans-membrane transport of anions such as chloride and bicarbonate. This process may alter cellular homeostasis with possible effects on internal ions concentration and pH levels triggering several and diverse biological effects. In this article, an overview of the recent results on the study of aniontransporters, mainly acting with a carrier-type mechanism, is given with emphasis on the structure/activity relationship and on their biological activity as antibiotic and anticancer agents and in the development of new drugs for treating conditions derived from dysregulation of natural anion channels.

Synthesis and Biological Activity of Embelin and its Derivatives: An Overview

2020 ◽  
Vol 20 (5) ◽  
pp. 396-407 ◽  
Author(s):  
Zhaojun Sheng ◽  
Siyuan Ge ◽  
Min Gao ◽  
Rongchao Jian ◽  
Xiaole Chen ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Effects ◽  
New Drugs ◽  
Hydroxyl Groups ◽  
Carbonyl Groups ◽  
Cellular Mechanisms ◽  
Embelia Ribes ◽  
Naturally Occurring ◽  
Ic50 Value ◽  
Apoptosis Protein

Embelin is a naturally occurring para-benzoquinone isolated from Embelia ribes (Burm. f.) of the Myrsinaceae family, and contains two carbonyl groups, a methine group and two hydroxyl groups. With embelin as the lead compound, more than one hundred derivatives have been reported. Embelin is well known for its ability to antagonize the X-linked inhibitor of apoptosis protein (XIAP) with an IC50 value of 4.1 μM. The potential of embelin and its derivatives in the treatment of various cancers has been extensively studied. In addition, these compounds display a variety of other biological effects: antimicrobial, antioxidant, analgesic, anti-inflammatory, anxiolytic and antifertility activity. This paper reviews the recent progress in the synthesis and biological activity of embelin and its derivatives. Their cellular mechanisms of action and prospects in the research and development of new drugs are also discussed.

scholarly journals In Vivo and In Vitro Assays Evaluating the Biological Activity of Taurine, Glucose and Energetic Beverages

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2198
Author(s):  
Marcos Mateo-Fernández ◽  
Fernando Valenzuela-Gómez ◽  
Rafael Font ◽  
Mercedes Del Río-Celestino ◽  
Tania Merinas-Amo ◽  
...  
Keyword(s):  
Dna Damage ◽  
Drosophila Melanogaster ◽  
Biological Activity ◽  
Biological Effects ◽  
Methylation Status ◽  
Repetitive Sequences ◽  
Energy Drinks ◽  
Red Bull

Taurine is one of the main ingredients used in energy drinks which are highly consumed in adolescents for their sugary taste and stimulating effect. With energy drinks becoming a worldwide phenomenon, the biological effects of these beverages must be evaluated in order to fully comprehend the potential impact of these products on the health due to the fact nutrition is closely related to science since the population consumes food to prevent certain diseases. Therefore, the aim of this study was to evaluate the biological effects of taurine, glucose, classic Red Bull® and sugar-free Red Bull® in order to check the food safety and the nutraceutical potential of these compounds, characterising different endpoints: (i) Toxicology, antitoxicology, genotoxicology and life expectancy assays were performed in the Drosophila melanogaster model organism; (ii) The in vitro chemopreventive activity of testing compounds was determined by assessing their cytotoxicity, the proapoptotic DNA-damage capability to induce internucleosomal fragmentation, the strand breaks activity and the modulator role on the methylation status of genomic repetitive sequences of HL-60 promyelocytic cells. Whereas none tested compounds showed toxic or genotoxic effect, all tested compounds exerted antitoxic and antigenotoxic activity in Drosophila. Glucose, classic Red Bull® and sugar-free Red Bull® were cytotoxic in HL-60 cell line. Classic Red Bull® induced DNA internucleosomal fragmentation although none of them exhibited DNA damage on human leukaemia cells. In conclusion, the tested compounds are safe on Drosophila melanogaster and classic Red Bull® could overall possess nutraceutical potential in the in vivo and in vitro model used in this study. Besides, taurine could holistically be one of the bioactive compounds responsible for the biological activity of classic Red Bull®.

Evaluation of the activity of antihypoxants with an isothiourea structure in a model of hypercapnic hypoxia with a shutdown of the cerebral hemispheres

2021 ◽  
Vol 19 (1) ◽  
pp. 55-63
Author(s):  
Vera V. Marysheva ◽  
Vladimir V. Mikheev ◽  
Petr D. Shabanov
Keyword(s):  
Acute Hypoxia ◽  
Life Time ◽  
The Body ◽  
Cerebral Hemispheres ◽  
Antihypoxic Activity ◽  
Hypoxic Episode ◽  
Hypoxia With Hypercapnia ◽  
Hypercapnic Hypoxia ◽  
Outbred Mice ◽  
The Brain

PURPOSE: To study the effect of amtizol, 2-aminobenzthiazole (2-ABT) and 2-amino-4-acetylthiazolo[5,4-b]indole (BM-606) on the resistance of male outbred mice to acute hypoxia with hypercapnia under conditions of isolated functioning of one from the hemispheres, as well as both hemispheres of the brain. METHODS: A model of acute hypoxia with hypercapnia (canned hypoxia) was used in mice of the same mass, the lifespan of all animals was determined. Temporary shutdown of the cortex of one of the hemispheres or both hemispheres was achieved by epidural application of filter paper moistened with 25% potassium chloride solution, creating a spreading depression according to Leao. Amtizol, 2-aminobenzthiazole (2-ABT) and 2-amino-4-acetylthiazolo[5,4-b]indole (BM-606) at equimolar doses of 25, 32.5, and 50 mg/kg, respectively were used as pharmacological analyzers, the compounds were injected intraperitoneally 30 min before the hypoxic episode. RESULTS: It was shown that, in contrast to amtizol, 2-ABT and VM-606 increase the life time of experimental animals when any hemisphere is turned off. The use of drugs when both hemispheres were turned off revealed that amtizol has approximately equal effect on the brain and the rest of the body, in 2-ABT antihypoxic activity is 1/3 associated with the brain, in VM-606 exclusively with the brain. CONCLUSION: The experimental model used in this work makes it possible to quite easily evaluate the effect of either one drug or compare several drugs, their role in the functioning of the cerebral hemispheres, on which part of the sample highly resistant or low resistant to hypoxia they have the greatest effect.

scholarly journals Effects of Long-Term Hydrogen Intervention on Plasma Metabolites and Gut Microbiome of Rats in Health Status

2021 ◽  
Author(s):  
Fei Xie ◽  
Xue Jiang ◽  
Yang Yi ◽  
Zi-Jia Liu ◽  
Chen Ma ◽  
...  
Keyword(s):  
Health Status ◽  
Gut Microbiota ◽  
Biological Effects ◽  
Enrichment Analysis ◽  
The Body ◽  
Plasma Metabolites ◽  
Control Group ◽  
Pathway Enrichment Analysis ◽  
Rrna Gene

Abstract The potential for preventive and therapeutic applications of H2 have now been confirmed in various disease. However, the effects of H2 on health status have not been fully elucidated. Our previous study reported changes in the body weight and 13 serum biochemical parameters during the six-month hydrogen intervention. To obtain a more comprehensive understanding of the effects of long-term hydrogen consumption, the plasma metabolome and gut microbiota were investigated in this study. Compared with the control group, 14 and 10 differential metabolites (DMs) were identified in hydrogen-rich water (HRW) and hydrogen inhalation (HI) group, respectively. Pathway enrichment analysis showed that HRW intake mainly affected starch and sucrose metabolism, and DMs in HI group were mainly enriched in arginine biosynthesis. 16S rRNA gene sequencing showed that HRW intake induced significant changes in the structure of gut microbiota, while no marked bacterial community differences was observed in HI group. HRW intake mainly induced significant increase in the abundance of Lactobacillus, Ruminococcus, Clostridium XI, and decrease in Bacteroides. HI mainly induced decreased abundances of Blautia and Paraprevotella. The results of this study provide basic data for further research on hydrogen medicine. Determination of the effects of hydrogen intervention on microbiota profiles could also shed light on identification of mechanism underlying the biological effects of molecular hydrogen.

scholarly journals Peculiarities of Evaluation of Biological Effects of the Influence of Electromagnetic Radiation in Conditions of Reduced Temperature (Experiment)

2021 ◽  
Vol 6 (2) ◽  
pp. 227-235
Author(s):  
O. Litovchenko ◽  
◽  
I. Perova ◽  
Keyword(s):  
Electromagnetic Radiation ◽  
Negative Impact ◽  
Biological Effects ◽  
The Body ◽  
Combined Effect ◽  
Male Rats ◽  
Control Group ◽  
Prevention Measures ◽  
Immunological Parameters ◽  
Reduced Temperature

In modern conditions there is a high need to improve methods for establishing the nature of the combined influence of factors using modern approaches for further development of prevention measures against the negative impact of factors on the body. The purpose of the study was to investigate the combined effect of electromagnetic radiation and low temperatures with subsequent determination of the level of contribution of each factor in the formation of biological effects within the experiment by mathematical analysis of data using the method of artificial intelligence. Materials and methods. The subchronic experiment (30 days) was performed on male rats. The animals were divided into groups: combined exposure to electromagnetic radiation (70 kHz, 600 V/m) and reduced temperature (40C), isolated exposure to reduced temperature, isolated exposure to electromagnetic radiation and a control group. The establishment of biological effects was performed at stages 5, 15 and 30 days of the experiment. Changes in the body were assessed by physiological, biochemical and immunological parameters of the blood (30 indicators). Data processing was performed using computational intelligence methods (Neuro-fuzzy system). Results and discussion. The combined effect of the factors was manifested by the following biological effects: intensification of peroxidation processes with simultaneous moderate suppression of antioxidant protection, intensification of lipid metabolism was characterized by dyslipoproteinemia, manifesting in: increase in triglycerides, cholesterol and its fractions. Changes of the immune system were decrease in the ability of neutrophils to phagocytosis at different stages of the experiment, imbalance of the activation of the system of reducing the concentration of C4 at the background of increased intensity of IgM and IgG synthesis. The method of determining the intensity of the factors, developed on the basis of factor and cluster analysis, allowed to determine that during the experiment the ratios between the factors changed, but the greatest contribution was made by reduced temperature by both biochemical parameters (63%) and immunological (53%) at the same time, the level of electromagnetic radiation contribution was 37% and 47%, respectively. Thus, the reduced temperature was the leading factor in the combined effect, which added 60% to the overall biological effect throughout the study, against the effect of electromagnetic radiation for which the level of contribution was only 40%. By means of the factor analysis informative indicators, making it possible to establish the characteristics of biological effects, and therefore leading indicators in formation of biological effects were the increase in concentration of DC with simultaneous decrease in concentration of SH-groups, increase in VLDL and suppression of oxygen-dependent metabolism of neutrophil-test. Conclusion. Thus, the tested mathematical approach allowed to determine the leading role of each of the studied factors under the conditions of their combined influence in different systems, which allows to predict probable appropriate reactions of the whole organism and gives a reasonable approach to the development of preventive measures

scholarly journals Chemical constituents of Chaenomeles sinensis twigs and their biological activity

2020 ◽  
Vol 16 ◽  
pp. 3078-3085
Author(s):  
Joon Min Cha ◽  
Dong Hyun Kim ◽  
Lalita Subedi ◽  
Zahra Khan ◽  
Sang Un Choi ◽  
...  
Keyword(s):  
Biological Activity ◽  
Data Analysis ◽  
Cell Lines ◽  
Chemical Structure ◽  
Biological Effects ◽  
Chemical Constituents ◽  
2D Nmr ◽  
Nmr Data ◽  
Chaenomeles Sinensis ◽  
Modified Mosher’S Method

A new megastigmane-type norsesquiterpenoid glycoside, chaemeloside (1), was isolated from the twigs of Chaenomeles sinensis together with 11 known phytochemicals through chromatographic methods. The chemical structure of the new isolate 1 was determined by conventional 1D and 2D NMR data analysis, ECD experiment, hydrolysis followed by a modified Mosher’s method, and LC–MS analysis. The characterized compounds’ biological effects including cytotoxicity against cancer cell lines, antineuroinflammatory activity, and potential neurotrophic effect were evaluated.

scholarly journals Epac signaling protein ligands as tools for studying their biological activity and creating new original drugs

2020 ◽  
pp. 3-17
Author(s):  
G. V. Mokrov ◽  
T. D. Nikiforova ◽  
S. A. Kryzhanovskiy
Keyword(s):  
Biological Activity ◽  
Cyclic Adenosine Monophosphate ◽  
Adenosine Monophosphate ◽  
The Body ◽  
Physiological Functions ◽  
Signaling Protein ◽  
Protein Ligands ◽  
Biological Target ◽  
Effective Drugs ◽  
Structure And Functions

The review discusses modern views about the structure and functions of Epac proteins (exchange proteins directly activated by cyclic adenosine monophosphate). The involvement of Epac proteins both in the regulation of the physiological functions of the body and in the initiation of various pathological processes allows to consider them as a fundamentally new biological target for creating original, highly effective drugs. Information on existing Epac protein agonists and antagonists was collected, and the influence of Epac ligands structure on the values of their affinity and selectivity was analyzed. Presumptive mechanisms of the interaction of ligands with Epac proteins are presented.

scholarly journals The Kinetics of Peroxynitrite on Insulin Nitration Damage

2020 ◽  
Author(s):  
Congxiao Zhang ◽  
Fusheng Sun ◽  
Congjiang Zhang ◽  
Yunjing Luo
Keyword(s):  
Activation Energy ◽  
Biological Activity ◽  
Glucose Metabolism ◽  
Rate Constants ◽  
The Body ◽  
Stopped Flow ◽  
Tyrosine Nitration ◽  
Protein Nitration ◽  
Physiological Conditions ◽  
Kinetics Of

Abstract Background: Insulin is one of the most important versatile hormones that is central to regulating the energy and glucose metabolism in the body. There has been accumulating evidence supporting that diabetes was associated with peroxynitrite and protein nitration, and insulin nitration induced by peroxynitrite affected its biological activity. Methods: In this paper, the kinetics of insulin nitration by peroxynitrite in physiological conditions was studied by the stopped flow technique. Results: We determined the values of the reactive rate constants of peroxynitrite decomposition and peroxynitrite-induced tyrosine nitration in the presence of insulin. The activation energy of peroxynitrite decomposition and 3-nitrotyrosine yield in the presence of insulin is 48.8 kJ·mol−1 and 42.7 kJ·mol−1 respectively. Conclusions: It is inferred that the glutamate residue of insulin accelerated peroxynitrite decomposition and tyrosine nitration by reducing the activation energy of reactions. The results could be beneficial for exploring the molecular mechanism of diabetes and offering a new target for diabetes therapies.

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