scholarly journals The impact of β-azido(or 1-piperidinyl)methylamino acids in position 2 or 3 on biological activity and conformation of dermorphin analogues

2016 ◽  
Vol 22 (8) ◽  
pp. 545-551 ◽  
Author(s):  
Maciej Maciejczyk ◽  
Anika Lasota ◽  
Oliwia Frączak ◽  
Piotr Kosson ◽  
Aleksandra Misicka ◽  
...  
2020 ◽  
Vol 22 (1) ◽  
pp. 155
Author(s):  
Mikhail V. Diachkov ◽  
Karoll Ferrer ◽  
Jana Oklestkova ◽  
Lucie Rarova ◽  
Vaclav Bazgier ◽  
...  

Brassinosteroids are a class of plant hormones that regulate a broad range of physiological processes such as plant growth, development and immunity, including the suppression of biotic and abiotic stresses. In this paper, we report the synthesis of new brassinosteroid analogues with a nitrogen-containing side chain and their biological activity on Arabidopis thaliana. Based on molecular docking experiments, two groups of brassinosteroid analogues were prepared with short and long side chains in order to study the impact of side chain length on plants. The derivatives with a short side chain were prepared with amide, amine and ammonium functional groups. The derivatives with a long side chain were synthesized using amide and ammonium functional groups. A total of 25 new brassinosteroid analogues were prepared. All 25 compounds were tested in an Arabidopsis root sensitivity bioassay and cytotoxicity screening. The synthesized substances showed no significant inhibitory activity compared to natural 24-epibrassinolide. In contrast, in low concentration, several compounds (8a, 8b, 8e, 16e, 22a and 22e) showed interesting growth-promoting activity. The cytotoxicity assay showed no toxicity of the prepared compounds on cancer and normal cell lines.


Materials ◽  
2021 ◽  
Vol 14 (4) ◽  
pp. 1050
Author(s):  
Sylwia Cyboran-Mikołajczyk ◽  
Robert Pasławski ◽  
Urszula Pasławska ◽  
Kacper Nowak ◽  
Michał Płóciennik ◽  
...  

Long-term high fat-carbohydrates diet (HF-CD) contributes to the formation of irreversible changes in the organism that lead to the emergence of civilization diseases. In this study, the impact of three-month high-fat diet on the physical properties of erythrocytes (RBCs) was studied. Furthermore, the biological activity of Cistus incanus L. extracts, plant known with high pro-health potential, in relation to normal and HF-CD RBCs, was determined. Obtained results have shown that, applied HF-CD modified shape, membrane potential and osmotic resistance of erythrocytes causing changes in membrane lipid composition and the distribution of lipids. The impact of HF-CD on physical properties of RBCs along with atherosclerotic lesions of the artery was visible, despite the lack of statistically significant changes in blood morphology and plasma lipid profile. This suggests that erythrocytes may be good markers of obesity-related diseases. The studies of biological activity of Cistus incanus L. extracts have demonstrated that they may ameliorate the effect of HF-CD on erythrocytes through the membrane-modifying and antioxidant activity.


Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3569
Author(s):  
Yicheng Tan ◽  
Zhang Ye ◽  
Mansheng Wang ◽  
Muhammad Faisal Manzoor ◽  
Rana Muhammad Aadil ◽  
...  

In this study, the impact of different cell disruption techniques (high-pressure micro fluidization (HPMF), ionic liquids (ILs), multi-enzyme (ME), and hydrochloric acid (HCl)) on the chemical composition and biological activity of astaxanthin (AST) obtained from Haematococcus pluvialis was investigated. Results indicated that all cell disruption techniques had a significant effect on AST composition, which were confirmed by TLC and UPC2 analysis. AST recovery from HCl (HCl-AST) and ILs (ILs-AST) cell disruption techniques was dominant by free and monoesters AST, while AST recovery from HPMF (HPMF-AST) and ME (ME-AST) cell disruption techniques was composed of monoesters, diesters, and free AST. Further biological activity analysis displayed that HCl-AST showed the highest ABTS and DPPH activity, while ILs-AST showed better results against the ORAC assay. Additionally, ILs-AST exhibits a stronger anti-proliferation of HepG2 cells in a dose-dependent manner, which was ascribed to AST-induced ROS in to inhibit the proliferative of cancer cells.


Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2771
Author(s):  
Sylwia Cyboran-Mikołajczyk ◽  
Piotr Jurkiewicz ◽  
Martin Hof ◽  
Halina Kleszczyńska

Cyanidin and its O-glycosides have many important physiological functions in plants and beneficial effects on human health. Their biological activity is not entirely clear and depends on the structure of the molecule, in particular, on the number and type of sugar substituents. Therefore, in this study the detailed structure-activity relationship (SARs) of the anthocyanins/anthocyanidins in relation to their interactions with lipid bilayer was determined. On the basis of their antioxidant activity and the changes induced by them in size and Zeta potential of lipid vesicles, and mobility and order of lipid acyl chains, the impact of the number and type of sugar substituents on the biological activity of the compounds was evaluated. The obtained results have shown, that 3-O-glycosylation changes the interaction of cyanidin with lipid bilayer entirely. The 3-O-glycosides containing a monosaccharide induces greater changes in physical properties of the lipid membrane than those containing disaccharides. The presence of additional sugar significantly reduces glycoside interaction with model lipid membrane. Furthermore, O-glycosylation alters the ability of cyanidin to scavenge free radicals. This alteration depends on the type of free radicals and the sensitivity of the method used for their determination.


2014 ◽  
Vol 11 (1) ◽  
pp. 943-974 ◽  
Author(s):  
V. M. C. Rérolle ◽  
M. Ribas-Ribas ◽  
V. Kitidis ◽  
I. Brown ◽  
D. C. E. Bakker ◽  
...  

Abstract. We present here a high resolution surface water pH dataset obtained in the Northwest European shelf seas in summer 2011. This is the first time that pH has been measured at such a high spatial resolution (10 measurements h–1) in this region. The aim of our paper is to investigate the carbonate chemistry dynamics of the surface water using pH and ancillary data. The main processes controlling the pH distribution along the ship's transect, and their relative importance, were determined using a statistical approach. The study highlights the impact of biological activity, temperature and riverine inputs on the carbonate chemistry dynamics of the shelf seas surface water. For this summer cruise, the biological activity formed the main control of the pH distribution along the cruise transect. Variations in chlorophyll and nutrients explained 29% of the pH variance along the full transect and as much as 68% in the northern part of the transect. In contrast, the temperature distribution explained ca. 50% of the pH variation in the Skagerrak region. Riverine inputs were evidenced by high dissolved organic carbon (DOC) levels in the Strait of Moyle (northern Irish Sea) and the southern North Sea with consequent remineralisation processes and a reduction in pH. The DOC distribution described 15% of the pH variance along the full transect. This study highlights the high spatial variability of the surface water pH in shelf seawaters where a range of processes simultaneously impacts the carbonate chemistry.


2018 ◽  
Vol 9 ◽  
pp. 3079-3094 ◽  
Author(s):  
Przemyslaw Oberbek ◽  
Tomasz Bolek ◽  
Adrian Chlanda ◽  
Seishiro Hirano ◽  
Sylwia Kusnieruk ◽  
...  

Nanomaterials, such as hydroxyapatite nanoparticles show a great promise for medical applications due to their unique properties at the nanoscale. However, there are concerns about the safety of using these materials in biological environments. Despite a great number of published studies of nanoobjects and their aggregates or agglomerates, the impact of their physicochemical properties (such as particle size, surface area, purity, details of structure and degree of agglomeration) on living cells is not yet fully understood. Significant differences in these properties, resulting from different manufacturing methods, are yet another problem to be taken into consideration. The aim of this work was to investigate the correlation between the properties of nanoscale hydroxyapatite from different synthesis methods and biological activity represented by the viability of four cell lines: A549, CHO, BEAS-2B and J774.1 to assess the influence of the nanoparticles on immune, reproductive and respiratory systems.


Vaccine ◽  
2015 ◽  
Vol 33 (35) ◽  
pp. 4292-4299 ◽  
Author(s):  
Katia Garcia Duardo ◽  
Yadira Prieto Curbelo ◽  
Judith Raymond Pous ◽  
Estela Yamilet Rabasa Legón ◽  
Belinda Sánchez Ramírez ◽  
...  

2006 ◽  
Vol 27 (3) ◽  
pp. 260-286 ◽  
Author(s):  
Edward W. Hillhouse ◽  
Dimitris K. Grammatopoulos

The CRH receptor (CRH-R) is a member of the secretin family of G protein-coupled receptors. Wide expression of CRH-Rs in the central nervous system and periphery ensures that their cognate agonists, the family of CRH-like peptides, are capable of exerting a wide spectrum of actions that underpin their critical role in integrating the stress response and coordinating the activity of fundamental physiological functions, such as the regulation of the cardiovascular system, energy balance, and homeostasis. Two types of mammal CRH-R exist, CRH-R1 and CRH-R2, each with unique splicing patterns and remarkably distinct pharmacological properties, but similar signaling properties, probably reflecting their distinct and sometimes contrasting biological functions. The regulation of CRH-R expression and activity is not fully elucidated, and we only now begin to fully understand the impact on mammalian pathophysiology. The focus of this review is the current and evolving understanding of the molecular mechanisms controlling CRH-R biological activity and functional flexibility. This shows notable tissue-specific characteristics, highlighted by their ability to couple to distinct G proteins and activate tissue-specific signaling cascades. The type of activating agonist, receptor, and target cell appears to play a major role in determining the overall signaling and biological responses in health and disease.


2014 ◽  
Vol 9 (12) ◽  
pp. 1168-1181 ◽  
Author(s):  
Gergana Gacheva ◽  
Liliana Gigova

AbstractThe escalating levels of antibiotic resistance among pathogenic bacteria and the side effects of chemotherapeutic drugs in use forced the efforts of scientists to search for natural antimicrobial and anticancer substances with novel structures and unique mechanism of action. Focusing on bioproducts, recent trends in drug research have shown that microalgae (including the cyanobacteria) are promising organisms to furnish novel and safer biologically active compounds. Many microalgal metabolites have been found to possess potent antibacterial, antifungal, antiviral, anticancer and antiinflammatory activities, as well as antioxidant, enzyme inhibiting and immunostimulating properties. In this paper, the studies on the biological activity of microalgae associated with potential medical and pharmaceutical applications are briefly presented. Attention is focused on the impact of cultivation temperature, irradiance and growth stage on the biomass accumulation, activity and pathways of cell metabolism and the possibilities of using these variable factors to increase the diversity and quantity of biologically active substances synthesized by microalgae.


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