MEMBRANSTABILIZING ACTIVITY OF HUMIC SUBSTANCES AS THE INTEGRAL INDEX OF THEIR HEPATOPROTECTIVE PROPERTIES

The article presents the results of the development of technology for obtaining and evaluating the biological activity of a feed additive containing humic acids. The technology of obtaining humic derivatives of high quality and with high stability of components from organic livestock wastes has been optimized. A humic feed additive has been developed and an estimation of its biological activity in vitro using a cell level test system (Paramecium caudatum) has been made. The presence of membrane-protective properties in humic derivatives has been revealed, which discovers the prospects of their use in animal husbandry and veterinary medicine as the means, possessing a hepatoprotective orientation and increasing the resistance of the organism to various unfavorable factors.

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Lithium-induced modiphication of the physicochemical state of membrane proteins and lipids in human erythrocytes

Proceedings of the National Academy of Sciences of Belarus Biological Series ◽

10.29235/1029-8940-2021-66-3-295-301 ◽

2021 ◽

Vol 66 (3) ◽

pp. 295-301

Author(s):

G. P. Zubritskaya ◽

E. I. Slobozhanina

Keyword(s):

Lithium Salt ◽

Test System ◽

Human Erythrocytes ◽

Lithium Ions ◽

Physicochemical State ◽

A Cell ◽

Cell Test ◽

Membrane Bound ◽

Toxic Concentrations

The effect of various concentrations of lithium sulfate on human erythrocytes in vitro has been studied. It has been shown that the effect of lithium salt in maximum pharmacological and toxic concentrations on cells leads to a modification of the physicochemical state of membrane-bound proteins and lipids. It was found that in human erythrocytes exposed to lithium ions, there is a decrease in the activity of membrane-bound acetylcholinesterase and methgemoglobin reductase, as well as a change in the microviscosity of the lipid bilayer of membranes. The results obtained can be used to create a cell test system for assessing the toxicity of lithium compounds.

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In Vitro Biological Activity of Adriamycin

Tumori Journal ◽

10.1177/030089167005600301 ◽

1970 ◽

Vol 56 (3) ◽

pp. 137-148 ◽

Cited By ~ 36

Author(s):

Rosella Silvestrini ◽

Carmela Gambarucci ◽

Teresa Dasdia

Keyword(s):

Biological Activity ◽

Cellular Proliferation ◽

Therapeutic Index ◽

Dna And Rna ◽

Total Inhibition ◽

A Cell ◽

Nuclear Structures ◽

Higher Doses

Adriamycin is an antibiotic, isolated from cultures of a mutant of Streptomyces peucetius, var. caesius, with a chemical structure very similar to daunomycin but with a higher therapeutic index in experimental tumors. The biological activity of this antibiotic has been studied in vitro on the HeLa cell strain. Adriamycin quickly penetrates into the cells and fixes to the nuclear structures with a marked localization at the level of the perinucleolar chromatin. It causes a marked and immediate disturbance of the mitotic process, viz. pre-prophasic inhibition at the low doses and mitotic block at the higher doses. Even the synthesis of DNA and RNA, evaluated autoradiographically as incorporation of 3H-thymidine and 3H-uridine, appear markedly inhibited. The viability of the cells, tested both as regards capacity to give rise to colonies and as regards proliferative activity of a cell population, was seriously reduced, in a degree proportional to the period of treatment and to the concentration of the antibiotic, until total inhibition. In comparison with daunomycin, adriamycin exerts an immediate antimitotic and anti-metabolic effect which, at equivalent doses, is slightly lower than that of daunomycin. The long-term antiproliferative activity on cellular proliferation is however, identical for the two antibiotics.

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Phosphoramidate Derivatives of AZT as Inhibitors of HIV: Studies on the Carboxyl Terminus

Antiviral Chemistry and Chemotherapy ◽

10.1177/095632029300400204 ◽

1993 ◽

Vol 4 (2) ◽

pp. 97-101 ◽

Cited By ~ 13

Author(s):

C. McGuigan ◽

R. N. Pathirana ◽

S. S.-M. Choi ◽

D. Kinchington ◽

T. J. O'Connor

Keyword(s):

Amino Acids ◽

Biological Activity ◽

Carboxyl Terminus ◽

Amino Ester ◽

Carboxy Terminus ◽

Free Nucleotides ◽

Derivatives Of ◽

Anti Hiv ◽

Ester Lead

Novel phosphoramidate derivatives of the anti-HIV nucleoside analogue AZT have been prepared by phosphorochloridate chemistry. These materials carry carboxy-protected, amino acids, and are designed to act as membrane-soluble prodrugs of the bio-active free nucleotides. In vitro evaluation revealed the compounds to have a pronounced, selective antiviral activity. In particular, variation in the carboxy terminus region is studied. For alkyl phosphates small changes in the structure of the amino ester lead to marked changes in biological activity. However, for analogous aryl phosphates there is little dependence on the structure of the ester. This suggests a different mechanism of action for these two categories of phosphate prodrug.

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Vesicular disruption of lysosomal targeting organometallic polyarginine bioconjugates

Metallomics ◽

10.1039/c4mt00255e ◽

2015 ◽

Vol 7 (2) ◽

pp. 371-384 ◽

Cited By ~ 13

Author(s):

Annika Gross ◽

Hamed Alborzinia ◽

Stefania Piantavigna ◽

Lisandra L. Martin ◽

Stefan Wölfl ◽

...

Keyword(s):

Biological Activity ◽

Cancer Therapy ◽

Membrane Permeabilization ◽

Lysosomal Membrane ◽

Lysosomal Membrane Permeabilization ◽

Cell Penetrating ◽

A Cell ◽

Lysosomal Targeting ◽

Derivatives Of ◽

Metallocene Derivatives

Targeting of lysosomes is an interesting, novel pathway for cancer therapy. in this work, novel metallocene derivatives (of ferrocene and ruthenocene) of a cell penetrating polyarginine peptide are presented as lysosomal membrane permeabilization (LMP) agents and their localization and biological activity is investigated in detail.

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Aspergillus flavus as a Model System to Test the Biological Activity of Botanicals: An Example on Citrullus colocynthis L. Schrad. Organic Extracts

Toxins ◽

10.3390/toxins11050286 ◽

2019 ◽

Vol 11 (5) ◽

pp. 286 ◽

Cited By ~ 2

Author(s):

Francesca Degola ◽

Belsem Marzouk ◽

Antonella Gori ◽

Cecilia Brunetti ◽

Lucia Dramis ◽

...

Keyword(s):

Biological Activity ◽

Aspergillus Flavus ◽

Folk Medicine ◽

Inhibitory Effect ◽

Phytopathogenic Fungus ◽

Citrullus Colocynthis ◽

Desert Areas ◽

Derivatives Of ◽

Stem Leaf

Citrullus colocynthis L. Schrader is an annual plant belonging to the Cucurbitaceae family, widely distributed in the desert areas of the Mediterranean basin. Many pharmacological properties (anti-inflammatory, anti-diabetic, analgesic, anti-epileptic) are ascribed to different organs of this plant; extracts and derivatives of C. colocynthis are used in folk Berber medicine for the treatment of numerous diseases—such as rheumatism arthritis, hypertension bronchitis, mastitis, and even cancer. Clinical studies aimed at confirming the chemical and biological bases of pharmacological activity assigned to many plant/herb extracts used in folk medicine often rely on results obtained from laboratory preliminary tests. We investigated the biological activity of some C. colocynthis stem, leaf, and root extracts on the mycotoxigenic and phytopathogenic fungus Aspergillus flavus, testing a possible correlation between the inhibitory effect on aflatoxin biosynthesis, the phytochemical composition of extracts, and their in vitro antioxidant capacities.

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The Search for New Antibacterial Agents among 1,2,3-Triazole Functionalized Ciprofloxacin and Norfloxacin Hybrids: Synthesis, Docking Studies, and Biological Activity Evaluation

Scientia Pharmaceutica ◽

10.3390/scipharm90010002 ◽

2021 ◽

Vol 90 (1) ◽

pp. 2

Author(s):

Halyna Hryhoriv ◽

Illia Mariutsa ◽

Sergiy M. Kovalenko ◽

Victoriya Georgiyants ◽

Lina Perekhoda ◽

...

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Biological Activity ◽

Antibacterial Agents ◽

Docking Studies ◽

Synthetic Method ◽

Bacillus Subtilis Atcc ◽

Resistant Strains ◽

Derivatives Of

Among all modern antibiotics, fluoroquinolones are well known for their broad spectrums of activity and efficiency toward microorganisms and viruses. However, antibiotic resistance is still a problem, which has encouraged medicinal chemists to modify the initial structures in order to combat resistant strains. Our current work is aimed at synthesizing novel hybrid derivatives of ciprofloxacin and norfloxacin and applying docking studies and biological activity evaluations in order to find active promising molecules. We succeeded in the development of a synthetic method towards 1,2,3-triazole-substituted ciprofloxacin and norfloxacin derivatives. The structure and purity of the obtained compounds were confirmed by 1H NMR, 13C NMR, 19F NMR, LC/MS, UV-, IR- spectroscopy. Docking studies, together with in vitro research against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Bacillus subtilis ATCC 6633, Pseudomonas aeruginosa ATCC 27853, Candida albicans NCTC 885-653 revealed compounds in which activity exceeded the initial molecules.

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Synthesis and In Vitro Biological Activity Evaluation of Novel Imidazo [2,1-B][1,3,4] Thiadiazole as Anti-Alzheimer Agents

Letters in Drug Design & Discovery ◽

10.2174/1570180816666181108115510 ◽

2020 ◽

Vol 17 (5) ◽

pp. 610-617

Author(s):

Sara Azimi ◽

Omidreza Firuzi ◽

Aida Iraji ◽

Afsaneh Zonouzi ◽

Mahsima Khoshneviszadeh ◽

...

Keyword(s):

Biological Activity ◽

Inhibitory Activity ◽

Phenyl Ring ◽

Activity Evaluation ◽

Butyryl Cholinesterase ◽

Thiadiazole Derivatives ◽

Derivatives Of

Background: Considering that AD is multifactorial in nature, novel series of imidazo [2,1-b][1,3,4] thiadiazole derivatives were designed to address the basic factors responsible for the disease. <p> Methods: These compounds were investigated as inhibitors of beta-site APP cleaving enzyme 1, acetylcholinesterase and butyryl cholinesterase. <p> Results: The BACE1 inhibitory results indicated that nitro phenyl substituted derivatives of imidazo [2,1-b][1,3,4] thiadiazole scaffold (R2 = m-NO2) demonstrated superior BACE1 inhibitory activity compared to other substituted moieties. In the BuChE assay, compounds 4h and 4l carrying meta NO2 at R2 of phenyl ring turned out to be potent inhibitors. <p> Conclusion: In conclusion, these novel synthesized derivatives seem to be promising anti-Alzheimer agents.

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