ChemInform Abstract: BIOLOGICAL ACTIVITY OF TRANSFORMED STEROIDS. V. SYNTHESIS AND COMPARATIVE STUDY OF THE BIOLOGICAL PROPERTIES OF 16α, 17α-DIOXOLANES AND OXATHIOLANES OF THE PREGNANE SERIES

1977 ◽  
Vol 8 (28) ◽  
pp. no-no
Author(s):  
N. E. VOISHVILLO ◽  
YU. B. VOL'KENSHTEIN ◽  
I. V. GANINA ◽  
G. I. GRITSINA ◽  
Z. I. ISTOMNINA ◽  
...  
1976 ◽  
Vol 10 (6) ◽  
pp. 741-745
Author(s):  
N. E. Voishvillo ◽  
Yu. B. Vol'kenshtein ◽  
I. V. Ganina ◽  
G. I. Gritsina ◽  
Z. I. Istomina ◽  
...  

2008 ◽  
Vol 59 (1) ◽  
pp. 101-105
Author(s):  
Irina Zarafu ◽  
Lucia Veronica Ivan ◽  
Iuliana Harasim

3,5-disubstituted-1,2,4-tiadiazoles with substituted-styril and heterocycle-vinyl were obtained by extending the method which implies the use of 3,5-disubstituted-1,2,4-ditiazolium salts as precursors [1-4]. A comparative study of the reaction process in the case of perchlorates, diacide phosphates, tribromides and 3,5-distyrile-dithiazolium triiodides, taken as etalon, was perfomed. Good yields were obtained when using perchlorates, phosphates and triiodides. The reaction was made by heating the reaction mixture and by ultrasound exposure. The structure of the compounds was confirmed by chemical and physical analysis and the data obtained were identical to those of 3,5-disubstituted-1,2,4-tiadiazoles obtained by another methods [5,6]. The biological (antibacterial and anticancer) activity of the synthesized compounds was tested and the results indicated a medium activity.


1999 ◽  
Vol 64 (8) ◽  
pp. 1211-1252 ◽  
Author(s):  
Jan Hlaváček ◽  
Renáta Marcová

The first part of this review deals with the biosynthesis and a biological function of strongly vasoactive peptides named endothelins (ETs) including vasoactive intestinal contractor. Where it was useful, snake venoms sarafotoxins which are structural endothelin derivatives, were also mentioned. In the second part, an attention is paid to structural basis of the ETs biological activity, with respect to alterations of amino acid residues in the parent peptides modifying the conformation and consequently the physico-chemical and biological properties in corresponding ETs analogs. Special attention is focussed on the area of ETs receptors and their interaction with peptide and non peptide agonists and antagonists, important in designing selective inhibitors of ETs receptors potentially applicable as drugs in a medicine. A review with 182 references.


2021 ◽  
Vol 22 (1) ◽  
Author(s):  
Magdalena Woźniak ◽  
Anna Kwiatkowska ◽  
Elżbieta Hołderna-Kędzia ◽  
Katarzyna Sosnowska ◽  
Lucyna Mrówczyńska ◽  
...  

Introduction. Propolis, also known as bee glue, is a resinous material collected by honeybees with numerous biological properties, including antibacterial, antifungal, antioxidant and anticancer effects. Due to its health-promoting properties, propolis is a component of many products, including dietary supplements, cosmetics and healthy food. Aim. The aim of the study was to determine the antibacterial, antifungal and antioxidant activity of propolis extracts, as well as to compare the biological activity of propolis extracts, depending on the solvent used – ethyl alcohol or propylene glycol. Material and methods. Two propolis extracts were used in the research – the first was prepared in ethyl alcohol, and the second in propylene glycol. The antimicrobial activity of the examined extracts was determined against S. aureus, E. coli and C. albicans. The antioxidant activity was determined on the basis of the evaluation of their antiradical activity in the DPPH· test and Fe2+ chelating activity. Moreover, the total content of phenolic compounds and flavonoids in the tested extracts was determined using the colorimetric method. Results. The tested propolis extracts, regardless of the solvent used (ethyl alcohol or propylene glycol), showed high antibacterial (against S. aureus), antifungal (against C. albicans) and antioxidant (antiradical activity in the DPPH· test and ferrous iron chelating potency in the ferrozine test) activity. Moreover, both tested extracts were characterized by a high and similar content of bioactive compounds – phenolic compounds and flavonoids. Conclusions. The results of the conducted tests showed that the solvent used did not affect determined biological activity and the content of bioactive substances in the tested propolis extracts.


2021 ◽  
Author(s):  
Yuliya Akimenko

Abstract In model laboratory and field conditions, the influence of pollution by antibiotics (benzylpenicillin, ampicillin, streptomycin, oxytetracycline, tylosin, pharmasin, tromexin, aliseryl, and nystatin) on the biological properties of ordinary chernozem was examined in concentrations of 1-1000 mg/kg. A decrease in the majority of the basic biological parameters of chernozem occurs when the concentration of antibiotics is 100 mg/kg of soil. In most cases, there was a direct relationship between the content of antibiotics in the soil and the scale of a decrease in the studied parameters. The degree of the influence of antibiotics was determined by their nature, concentration and time of exposure. Antibacterial antibiotics had more negative impact on the studied indicators than fungicidal ones. By the degree of inhibiting the biological properties of chernozem, antibiotics formed the following sequence: ampicillin > benzylpenicillin ≥ streptomycin ≥ oxytetracycline > tylosin ≥ pharmasin > nystatin > tromexin > aliseryl. Among the examined biological parameters when polluted by antibiotics, the most informative one was the number of ammonifying bacteria and the activity of dehydrogenases. The least informative was the indicator of catalase activity. The abundance of bacteria of the genus Azotobacter in case of pollution by antibiotics was not informative. The degree of a decrease in biological indicators was more pronounced in laboratory conditions than in the field ones. The rate of the biological activity recovery of chernozem after pollution in the field was 2 times higher. According to the degree of resistance to antibiotics, the investigated microorganisms of chernozem formed the following sequence: bacteria of the genus Azotobacter > micromycetes > amylolytic bacteria > ammonifying bacteria. Enzymes formed the following sequence: peroxidase ≥ polyphenol oxidase > catalase > dehydrogenase > invertase ≥ phosphatase. Antibiotics had prolonged influence on the biological properties of ordinary chernozem. The examined parameters were observed not to be recovered to control values even on the 120th day after the pollution.


2021 ◽  
Vol 26 (3) ◽  
pp. 100-108
Author(s):  
Ahmed Mouard ◽  
Hassan Mesbah ◽  
Rehab AlAssar ◽  
Khaled Abd ElHamid

1988 ◽  
Vol 8 (7) ◽  
pp. 2933-2941
Author(s):  
P Delli-Bovi ◽  
A M Curatola ◽  
K M Newman ◽  
Y Sato ◽  
D Moscatelli ◽  
...  

We recently reported that the protein encoded in a novel human oncogene isolated from Kaposi sarcoma DNA was a growth factor with significant homology to basic and acidic fibroblast growth factors (FGFs). To study the properties of this growth factor (referred to as K-FGF) and the mechanism by which the K-fgf oncogene transforms cells, we have studied the production and processing of K-FGF in COS-1 cells transfected with a plasmid encoding the K-fgf cDNA. The results show that, unlike basic and acidic FGFs, the K-FGF protein is cleaved after a signal peptide, glycosylated, and efficiently secreted as a mature protein of 176 or 175 amino acids. Inhibition of glycosylation impaired secretion, and the stability of the secreted K-FGF was greatly enhanced by the presence of heparin in the cultured medium. We have used the conditioned medium from transfected COS-1 cells to test K-FGF biological activity. Similar to basic FGF, the K-FGF protein was mitogenic for fibroblasts and endothelial cells and induced the growth of NIH 3T3 mouse cells in serum-free medium. Accordingly, K-fgf-transformed NIH 3T3 cells grew in serum-free medium, consistent with an autocrine mechanism of growth. We have also expressed the protein encoded in the K-fgf protooncogene in COS-1 cells, and it was indistinguishable in its molecular weight, glycosylation, secretion, and biological activity from K-FGF. Taken together, these results suggest that the mechanism of activation of this oncogene is due to overexpression rather than to mutations in the coding sequences.


2008 ◽  
Vol 3 (10) ◽  
pp. 1934578X0800301 ◽  
Author(s):  
Maria I. Bilan ◽  
Anatolii I. Usov

Sulfated polysaccharides of brown algae (“fucoidans”) constitute a wide variety of biopolymers from simple sulfated fucans up to complex heteropolysaccharides composed of several neutral monosaccharides, uronic acid and sulfate. The increased interest in this class of polysaccharides is explained by their high and versatile biological activities, and hence, by their possible use in new drug design. Structural analysis of several fucoidans demonstrates that their biological properties are determined not only by charge density, but also by fine chemical structure, although distinct correlations between structure and biological activity cannot be formulated at present. The aim of this review is to describe the methods of structural analysis currently used in fucoidan chemistry, and to discuss some new information on the structures of fucoidans presented in recent publications.


2019 ◽  
Vol 45 (1) ◽  
pp. 15-28 ◽  
Author(s):  
Murugan Rajan ◽  
Allen Joseph Anthuvan ◽  
Kasipandi Muniyandi ◽  
Naveen Kumar Kalagatur ◽  
Saravanan Shanmugam ◽  
...  

Tetrahedron ◽  
2020 ◽  
Vol 76 (42) ◽  
pp. 131517
Author(s):  
Shuang Zhao ◽  
Shixin Zhang ◽  
Jintao Xu ◽  
Lei Hu

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