scholarly journals Correlation of Physical and Biological Properties of Mouse Mammary Tumor Agent

1959 ◽  
Vol 5 (1) ◽  
pp. 85-92 ◽  
Author(s):  
Dan H. Moore ◽  
E. Y. Lasfargues ◽  
Margaret R. Murray ◽  
Cushman D. Haagensen ◽  
E. C. Pollard
Keyword(s):  
Active Agent ◽  
Biological Properties ◽  
Biologically Active ◽  
Mammary Adenocarcinoma ◽  
Complex Nature ◽  
Pore Sizes ◽  
Physical Measurements ◽  
Mouse Mammary Tumor ◽  
Internal Core ◽  
Large Agent

Biophysical procedures have been used to determine the size and structure of the biologically active agent responsible for the transmission, through milk, of mouse mammary adenocarcinoma. Filtration of milk from RIII high-breast-cancer mice through gradocol membranes with decreasing pore sizes indicated that a minimum of activity passed through intermediate pore sizes (100 to 160 mµ). Filtrates through smaller pores were significantly active. Milk treated with small doses of deuteron irradiation produced more tumors than the control, unirradiated milk; larger doses indicated a particle size much less than 100 mµ. Free diffusion experiments indicated that the activity was associated with particles of two different sizes. Altogether the data denoted the presence of a large agent about 100 mµ in diameter and a small agent 20 to 30 mµ in diameter or possibly smaller. Furthermore, the presence in the milk of an inhibitor 40 to 60 mµ is indicated by the results of all three approaches. The complex nature of the milk agent disclosed by the physical measurements agrees with the picture of one of the structures revealed by electron microscopy as well as with seemingly conflicting measurements reported in the literature. The large agent defined by these indirect methods corresponds to the whole particle seen in the electron microscope and the small agent corresponds to its internal core or nucleoid. It is suggested that the nucleoid is essentially a nucleic acid which may, in the absence of the "inhibitor," retain its activity after being stripped of its outer membrane or sac.

The Molecular Diversity Scope of Urazole in the Synthesis of Organic Compounds

2019 ◽  
Vol 16 (7) ◽  
pp. 953-967 ◽  
Author(s):  
Ghodsi M. Ziarani ◽  
Fatemeh Mohajer ◽  
Razieh Moradi ◽  
Parisa Mofatehnia
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Biologically Active ◽  
Microtubule Assembly ◽  
Heterocyclic Molecules ◽  
Biological Perspective ◽  
Highly Active ◽  
Anti Inflammatory ◽  
High Yields ◽  
Short Time

Background: As a matter of fact, nitrogen as a hetero atom among other atoms has had an important role in active biological compounds. Since heterocyclic molecules with nitrogen are highly demanded due to biological properties, 4-phenylurazole as a compound containing nitrogen might be important in the multicomponent reaction used in agrochemicals, and pharmaceuticals. Considering the case of fused derivatives “pyrazolourazoles” which are highly applicable because of their application for analgesic, antibacterial, anti-inflammatory and antidiabetic activities as HSP-72 induction inhibitors (I and III) and novel microtubule assembly inhibitors. It should be mentioned that spiro-pyrazole also has biological activities like cytotoxic, antimicrobial, anticonvulsant, antifungal, anticancer, anti-inflammatory, and cardiotonic activities. Objective: Urazole has been used in many heterocyclic compounds which are valuable in organic syntheses. This review disclosed the advances in the use of urazole as the starting material in the synthesis of various biologically active molecules from 2006 to 2019. Conclusion: Compounds of urazole (1,2,4-triazolidine-3,5-dione) are the most important molecules which are highly active from the biological perspective in the pharmaceuticals as well as polymers. In summary, many protocols for preparations of the urazole derivatives from various substrates in multi-component reactions have been reported from different aromatic and aliphatic groups which have had carbonyl groups in their structures. It is noted that several catalysts have been synthesized to afford applicable molecules with urazole scaffolds. In some papers, being environmentally friendly, short time reactions and high yields are highlighted in the protocols. There is a room to synthesize new catalysts and perform new reactions by manipulating urazole to produce biologically active compounds, even producing chiral urazole component as many groups of chiral urazole compounds are important from biological perspective.

scholarly journals Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3579
Author(s):  
Svetlana A. Popova ◽  
Evgenia V. Pavlova ◽  
Oksana G. Shevchenko ◽  
Irina Yu. Chukicheva ◽  
Aleksandr V. Kutchin
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
High Reactivity ◽  
Biologically Active ◽  
Brain Lipids ◽  
Wide Range ◽  
Privileged Structure ◽  
Vitro Model

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.

Novel Anti-Cancer, Anti-Bacterial Coatings for Biomaterial Applications: Selenium Nanoclusters

2009 ◽  
Vol 1209 ◽  
Author(s):  
Phong Anh Tran ◽  
Erik Taylor ◽  
Love Sarin ◽  
Robert H. Hurt ◽  
Thomas J Webster
Keyword(s):  
Bone Cells ◽  
Tumor Resection ◽  
Active Agent ◽  
In Vitro Study ◽  
Biologically Active ◽  
Elemental Selenium ◽  
Orthopedic Implant ◽  
Functional Coating ◽  
Anti Cancer

AbstractTwo common problems with implantation after cancerous tumor resection are cancer recurrence and bacteria infection at the implant site. Tumor resection surgery sometimes can not remove all the cancerous cells, thus, cancer can return after implantation. In addition, bacteria infection is one of the leading causes of implant failure. Therefore, it is desirable to have anti-cancer and anti-bacterial molecules which both rapidly (for anti-infection purposes) and continuously (for anti-cancer purposes) are available at the implant site following implantation. Therefore, the objective of the present in vitro study was to create a multi-functional coating for anti-cancer and anti-bacterial orthopedic implant applications. Elemental selenium was chosen as the biologically active agent in this effort because of its known chemopreventive and anti-bacterial properties. To achieve that objective, titanium (Ti), a conventional orthopedic implant material was coated with selenium (Se) nanoclusters. Different coating densities were achieved by varying Se concentration in the reaction mixture. Titanium substrates coated with Se nanoclusters were shown to enhance healthy osteoblast (bone-forming cell) and inhibit cancerous osteoblast proliferation in co-culture experiments. Functions of S. epidermidis (one of the leading bacteria that infect implants) were inhibited on Ti coated with Se-nanoclusters compared to uncoated materials. Thus, this study provided for the first time a coating material (selenium nanoclusters) to the biomaterials’ community to promote healthy bone cells’ functions, inhibit cancer growth and prevent bacteria infection.

scholarly journals Antimicrobial Peptides: Versatile Biological Properties

2013 ◽  
Vol 2013 ◽  
pp. 1-15 ◽  
Author(s):  
Muthuirulan Pushpanathan ◽  
Paramasamy Gunasekaran ◽  
Jeyaprakash Rajendhran
Keyword(s):  
Antimicrobial Peptides ◽  
Recombinant Expression ◽  
Biological Properties ◽  
Biologically Active ◽  
Drug Candidate ◽  
Plant Host ◽  
Immune Modulators ◽  
Signalling Molecule ◽  
Interesting Candidate ◽  
Pharmaceutical Industries

Antimicrobial peptides are diverse group of biologically active molecules with multidimensional properties. In recent past, a wide variety of AMPs with diverse structures have been reported from different sources such as plants, animals, mammals, and microorganisms. The presence of unusual amino acids and structural motifs in AMPs confers unique structural properties to the peptide that attribute for their specific mode of action. The ability of these active AMPs to act as multifunctional effector molecules such as signalling molecule, immune modulators, mitogen, antitumor, and contraceptive agent makes it an interesting candidate to study every aspect of their structural and biological properties for prophylactic and therapeutic applications. In addition, easy cloning and recombinant expression of AMPs in heterologous plant host systems provided a pipeline for production of disease resistant transgenic plants. Besides these properties, AMPs were also used as drug delivery vectors to deliver cell impermeable drugs to cell interior. The present review focuses on the diversity and broad spectrum antimicrobial activity of AMPs along with its multidimensional properties that could be exploited for the application of these bioactive peptides as a potential and promising drug candidate in pharmaceutical industries.

scholarly journals Constitutive and Regulated Shedding of Soluble FGF Receptors Releases Biologically Active Inhibitors of FGF-2

2021 ◽  
Vol 22 (5) ◽  
pp. 2712
Author(s):  
Anne Hanneken ◽  
Maluz Mercado ◽  
Pamela Maher
Keyword(s):  
Cell Surface ◽  
Ligand Binding ◽  
Cellular Proliferation ◽  
Biological Activities ◽  
Biological Properties ◽  
Matrix Metalloproteases ◽  
Biologically Active ◽  
Ectodomain Shedding ◽  
High Affinity

The identification of soluble fibroblast growth factor (FGF) receptors in blood and the extracellular matrix has led to the prediction that these proteins modulate the diverse biological activities of the FGF family of ligands in vivo. A recent structural characterization of the soluble FGF receptors revealed that they are primarily generated by proteolytic cleavage of the FGFR-1 ectodomain. Efforts to examine their biological properties are now focused on understanding the functional consequences of FGFR-1 ectodomain shedding and how the shedding event is regulated. We have purified an FGFR-1 ectodomain that is constitutively cleaved from the full-length FGFR-1(IIIc) receptor and released into conditioned media. This shed receptor binds FGF-2; inhibits FGF-2-induced cellular proliferation; and competes with high affinity, cell surface FGF receptors for ligand binding. FGFR-1 ectodomain shedding downregulates the number of high affinity receptors from the cell surface. The shedding mechanism is regulated by ligand binding and by activators of PKC, and the two signaling pathways appear to be independent of each other. Deletions and substitutions at the proposed cleavage site of FGFR-1 do not prevent ectodomain shedding. Broad spectrum inhibitors of matrix metalloproteases decrease FGFR-1 ectodomain shedding, suggesting that the enzyme responsible for constitutive, ligand-activated, and protein kinase C-activated shedding is a matrix metalloprotease. In summary, shedding of the FGFR-1 ectodomain is a highly regulated event, sharing many features with a common system that governs the release of diverse membrane proteins from the cell surface. Most importantly, the FGFR ectodomains are biologically active after shedding and are capable of functioning as inhibitors of FGF-2.

scholarly journals RECENTES AVANÇOS NA FUNCIONALIZAÇÃO SELETIVA DE QUINOLINAS

Química Nova ◽  
2021 ◽  
Author(s):  
Dartagnan Ferreira ◽  
Valter Murie ◽  
Thiago Santos ◽  
Paulo Vieira ◽  
Giuliano Clososki
Keyword(s):  
Wide Spectrum ◽  
Structural Diversity ◽  
Biological Properties ◽  
Biologically Active ◽  
Chemical Transformations ◽  
Heterocyclic Molecules ◽  
Point Of Interest ◽  
Selective Functionalization ◽  
Biological Interest ◽  
Approved Drugs

RECENT ADVANCES IN SELECTIVE FUNCTIONALIZATION OF QUINOLINES. Heterocyclic compounds form an important and extensive group of organic substances. Among nitrogenous heterocyclic molecules, quinolines stand out for exhibiting attractive chemical and biological properties. These substances can be used as ligands, sensors, luminescent and agrochemical materials. In addition, quinoline-containing compounds can exhibit a wide spectrum of pharmacological properties, allowing their use in several approved drugs nowadays. Due to its importance, the synthesis of molecules containing this nucleus becomes a point of interest for synthetic chemists. In this way, several methodologies have been recently developed to prepare quinoline derivatives with high structural diversity. Such chemical transformations allow the chemical modification of these rings with high selectivity and tolerance to diverse functional groups and these properties have been conveniently used in the preparation of biologically active molecules containing this unit. Herein, we present a review of the main methodologies employed in the selective functionalization of quinolines in the last twenty years. In this context, a brief introduction addressing general synthetic and medicinal aspects related to the functionalization positions of the quinoline ring is presented. Several methodologies used in the functionalization of this moiety are discussed, as well relevant synthetic applications, both in the preparation and functionalization of substances of biological interest.

scholarly journals Secondary metabolites of a marine-derived Penicillium ochrochloron

2021 ◽  
Vol 13 (3) ◽  
pp. 11020
Author(s):  
Peter M. EZE ◽  
Ying GAO ◽  
Yang LIU ◽  
Lasse Van GEELEN ◽  
Chika P. EJIKEUGWU ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Secondary Metabolites ◽  
Biological Properties ◽  
Industrial Applications ◽  
Biologically Active ◽  
Fungal Isolation ◽  
The North ◽  
Wide Range ◽  
Extremophilic Fungi ◽  
Fungal Secondary Metabolites

Extremophilic fungi have received considerable attention recently as new promising sources of biologically active compounds with potential pharmaceutical applications. This study investigated the secondary metabolites of a marine-derived Penicillium ochrochloron isolated from underwater sea sand collected from the North Sea in St. Peter-Ording, Germany. Standard techniques were used for fungal isolation, taxonomic identification, fermentation, extraction, and isolation of fungal secondary metabolites. Chromatographic separation and spectroscopic analyses of the fungal secondary metabolites yielded eight compounds: talumarin A (1), aspergillumarin A (2), andrastin A (3), clavatol (4), 3-acetylphenol (5), methyl 2,5-dihydro-4-hydroxy-5-oxo-3-phenyl-2-furanpropanoate (6), emodin (7) and 2-chloroemodin (8). After co-cultivation with Bacillus subtilis, the fungus was induced to express (-)-striatisporolide A (9). Compound 1 was evaluated for antibacterial activity against Staphylococcus aureus, Acinetobacter baumannii, Mycobacterium smegmatis, and M. tuberculosis, as well as cytotoxicity against THP-1 cells. The compound, however, was not cytotoxic to THP-1 cells and had no antibacterial activity against the microorganisms tested. The compounds isolated from P. ochrochloron in this study are well-known compounds with a wide range of beneficial biological properties that can be explored for pharmaceutical, agricultural, or industrial applications. This study highlights the bioprospecting potential of marine fungi and confirms co-cultivation as a useful strategy for the discovery of new natural products.

scholarly journals Biological Properties of IRIM, the Iridium(III) Analogue of (Imidazolium (Bisimidazole) Tetrachlororuthenate) (ICR)

2000 ◽  
Vol 7 (4) ◽  
pp. 195-200 ◽  
Author(s):  
G. Marcon ◽  
A. Casini ◽  
P. Mura ◽  
L. Messori ◽  
A. Bergamo ◽  
...  
Keyword(s):  
Cell Lines ◽  
Biological Effects ◽  
Direct Interaction ◽  
Biological Properties ◽  
Mammary Adenocarcinoma ◽  
Interstrand Crosslinks ◽  
Conformational Effects ◽  
Calf Thymus ◽  
Human Ovarian Carcinoma ◽  
Dna Thermal Denaturation

Some biological aspects of the new complex imidazolium bisimidazole tetrachloro iridate(III)-IRIM- the iridium(III) analogue of ICR, were considered. More in detail the conformational effects produced by IRIM on DNA and the cytotoxic properties of IRIM on some selected human cell lines were measured. Dialysis experiments and DNA thermal denaturation studies are suggestive of poor binding of IRIM to DNA; formation of interstrand crosslinks is not observed. In any case CD measurements suggest that addition of increasing amounts of IRIM to calf thymus DNA results into significant spectral changes, that are diagnostic of a direct interaction with DNA. A number of experiments carried out on the A2780 human ovarian carcinoma, B16 murine melanoma, MCF7 and TS mammary adenocarcinoma tumor cell lines strongly point out that IRIM does not exhibit significant growth inhibition effects within the concentration range 10-4-10-6 M. It is suggested that the lower biological effects of IRIM compared to ICR are a consequence of the larger kinetic inertness of the iridium(III) center with respect to ruthenium(III).

Przeciwnowotworowe działanie składników propolisu. Cz. 1. Ester fenyloetylowy kwasu kawowego (CAPE)

2020 ◽  
Vol 21 (3) ◽  
Author(s):  
Bogdan Kędzia ◽  
Elżbieta Hołderna-Kędzia
Keyword(s):  
Human Colon ◽  
Caffeic Acid Phenethyl Ester ◽  
Biological Properties ◽  
Biologically Active ◽  
Significant Activity ◽  
Colon Adenoma ◽  
Cancer Cell Survival ◽  
Ht 29

The paper presents a review of the publications on the anticancerogenic activity of the biologically active component of propolis – caffeic acid phenethyl ester (CAPE). Literature data indicate numerous biological properties of CAPE, namely: antioxidant, anti-inflammatory, antiviral, immunostimulatory, anti-angiogenic and others. In numerous tests, both in vitro and in vivo, the significant activity of CAPE has been confirmed, including an action against HT-29 human colon adenoma cells, and five: human, murine and other tumor cell cultures. The authors also emphasize that CAPE supports the anticancerogenic effect of drugs, including doxorubicin and cisplatin, due to the reduction of cancer cell survival by 45% and 34%, respectively, compared to the above-mentioned drugs used alone. The conducted research indicates that the induction of apoptosis in cells, i.e. programmed cell death, can be mentioned among the main mechanisms of the anticancerogenic activity of CAPE.

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