Notizen: Marginalin, a Substance from the Pygidial Glands of Dytiscus Marginalis (Coleoptera): Molecular Associations with Polyamines in vitro

1990 ◽  
Vol 45 (10) ◽  
pp. 1455-1456 ◽  
Author(s):  
Michel Barbier
Keyword(s):  
Defensive Secretion ◽  
Biological Properties ◽  
Chemical Data ◽  
Pygidial Glands ◽  
Molecular Associations ◽  
Water Beetle ◽  
Physico Chemical ◽  
Biological Interest

Marginalin, a product previously isolated from the pygidial glands of the water-beetle Dytiscus marginalis (Coleoptera), strongly reacts in vitro to form complexes with polyamines of biological interest. With spermin and spermidin, this interaction is specific giving 1:1 complexes which were isolated and studied (physico-chemical data). The results so far observed are discussed in relationship with the known biological properties of spermin and spermidin and the significance of marginalin in the defensive secretion of the beetle

Chiral Forms of 4-(2',4'-Difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic Acid (Flobufen) and Its Metabolite.Synthesis and Basic Biological Properties

1997 ◽  
Vol 62 (3) ◽  
pp. 498-509 ◽  
Author(s):  
Miroslav Kuchař ◽  
Marie Poppová ◽  
Antonín Jandera ◽  
Vladimíra Panajotovová ◽  
Hana Zůnová ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Biological Activities ◽  
Biological Properties ◽  
Optical Isomers ◽  
Clinical Testing ◽  
Chemical Parameters ◽  
Physico Chemical ◽  
Oxobutanoic Acid

4-(2',4'-Difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid (1, flobufen) is subjected to clinical testing in the treatment of rheumatoid arthritis. Owing to the occurrence of a centre of chirality, the compound exists in two enantiomers, and its major human metabolite, viz. 4-(2',4'-difluorobiphenyl-4-yl)-4-hydroxy-2-methylbutanoic acid isolated in the lactone form (2), possesses two chiral centres, making possible the existence of four stereoisomers. All of the optical isomers of the substances 1 and 2 were prepared. For flobufen (1), the racemate was separated into the stereoisomers by using the salts 3 with R-(+)- or S-(-)-1-phenylethylamine. The pairs of stereoisomers of 2, obtained by reduction of R-(+)-flobufen or the S-(-)-enantiomer, were separated by column chromatography. The physico-chemical parameters of the optical isomers were determined and some biological activities were evaluated in both in vitro and in vivo models.

In vitro elucidation of suppression effects of composts to soil-borne pathogen Phytophthora nicotianae on pepper plants using 16S amplicon sequencing and metaproteomics

2018 ◽  
Vol 35 (2) ◽  
pp. 206-214 ◽  
Author(s):  
Margarita Ros ◽  
Josefa Blaya ◽  
Petr Baldrian ◽  
Felipe Bastida ◽  
Hans H Richnow ◽  
...  
Keyword(s):  
Chemical Properties ◽  
Amplicon Sequencing ◽  
Biological Properties ◽  
Phytophthora Nicotianae ◽  
Wall Structure ◽  
Inorganic Ion ◽  
Physico Chemical ◽  
Phylogenetic Level ◽  
Pepper Plants

AbstractCompost production is a critical component of organic waste management. One of the most important properties of compost is its ability to suppress soil-borne pathogens such as Phytophthora nicotianae in pepper plants. Both the physico-chemical and biological properties of composts can be responsible for the suppression of pathogens, although biological properties are the main driver. In this study, we analyzed composts with various levels of suppressiveness against P. nicotianae. We analyzed both physico-chemical properties like pH and electrical conductivity and biological properties like microbial activity, amplicon sequencing and metaproteomics. We believed that the link between community structures and proteins could provide deep insights into the mechanism of compost suppressiveness. Our results indicate that there are differences between suppressive and non-suppressive composts at the phylogenetic level (sequencing) and at the functional level (based on analysis of the cluster of orthologous groups, COGs). The proteins identified were assigned to the carbohydrate process, cell wall structure and inorganic ion transport and metabolism. Proteobacteria could also be new indicators of P. nicotianae suppression.

scholarly journals Oleuropein-Laded Ufasomes Improve the Nutraceutical Efficacy

Nanomaterials ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 105
Author(s):  
Maria Chiara Cristiano ◽  
Francesca Froiio ◽  
Antonia Mancuso ◽  
Donato Cosco ◽  
Luciana Dini ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Cell Membranes ◽  
Unsaturated Fatty Acids ◽  
Dynamic Structure ◽  
Biological Properties ◽  
In Vitro Studies ◽  
Antioxidant Compounds ◽  
Transmission Electron ◽  
Physico Chemical

Ufasomes are unsaturated fatty acid liposomes made up of oleic and linoleic acids, natural components required in various biological processes. This kind of nanocarrier is characterized by a simple and dynamic structure and is able to improve the bioavailability of unsaturated fatty acids. The aim of this investigation was to evaluate ufasomes as natural compound delivery systems to deliver oleuropein and improve its antioxidant activity. Oleuropein is a phenolic compound mainly present in olives and olive oil, with several biological properties, such as the antioxidant activity. However, to improve their biological activity, antioxidant compounds should be able to cross cell membranes and uniformly incorporate in cells. Because of the great similarity between their constituents and cell membranes, ufasomes could be advantageous carriers for oleuropein delivery. The physico-chemical characteristics of ufasomes were investigated. A regular shape was shown by transmission electron microscopy studies, while the mean sizes were dependent on the ufasomes composition. In vitro studies highlighted that empty ufasomes did not lead to cell mortality at the tested concentrations and a good carrier internalization in CaCo-2 cells, further studies in vitro studies demonstrated that oleuropein-loaded ufasomes were able to enhance the antioxidant activity of the free active substance making this carrier a suitable one for nutraceutical application.

scholarly journals Synthesis, Characterization and Biological Evaluation of Novel Triazole Linked Chromone Biheterocycle Analogs

2021 ◽  
Vol 34 (1) ◽  
pp. 53-59
Author(s):  
Jilla Soujanya ◽  
D. Ravisankar Reddy ◽  
Gade Kalyani
Keyword(s):  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Biological Properties ◽  
Protective Role ◽  
Biological Evaluation ◽  
Biologically Active ◽  
The Novel ◽  
Spectral Techniques ◽  
Physico Chemical

The current work focused on the synthesis of novel chromone biheterocycle analogs followed by its characterization through physico-chemical and spectral techniques like FTIR, mass and NMR spectroscopy. The basic triazole heterocycle and its analogs have different biological properties. At the point when one biological active molecule is connected to another, the resultant shows improved potency (biheterocycles). Chromone and triazole are selected in this study to develop new efficient, simple, economically viable and biologically active synthetic compounds. All the novel derivatives of triazole linked chromone biheterocycles were synthesized via a click chemistry procedure and screened for in vitro antimicrobial, antifungal and antioxidant studies. Among them, the compounds CRN-F (IC50 = 35.97), CRN-H (IC50 = 28.76) and CRN-J (IC50 = 29.72) have significant free radical scavenging activity in comparison with the ascorbic acid as control standard (IC50 = 23.07). Some of these novel derivatives exhibited moderate antimicrobial and antifungal activity compared to that of the reference standards. Hence, the novel chromone biheterocycle analogs played a protective role against oxidative damage.

scholarly journals Physico-chemical–mechanical and in vitro biological properties of calcium phosphate cements with doped amorphous calcium phosphates

Biomaterials ◽  
2007 ◽  
Vol 28 (6) ◽  
pp. 956-965 ◽  
Author(s):  
Marion Julien ◽  
Ibrahim Khairoun ◽  
Racquel Z. LeGeros ◽  
Severine Delplace ◽  
Paul Pilet ◽  
...  
Keyword(s):  
Calcium Phosphate ◽  
Calcium Phosphates ◽  
Biological Properties ◽  
Calcium Phosphate Cements ◽  
Physico Chemical

scholarly journals Application of Neurokinin-1 Receptor in Targeted Strategies for Glioma Treatment. Part I: Synthesis and Evaluation of Substance P Fragments Labeled with 99mTc and 177Lu as Potential Receptor Radiopharmaceuticals

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2542 ◽  
Author(s):  
Agnieszka Majkowska-Pilip ◽  
Przemysław Koźmiński ◽  
Anna Wawrzynowska ◽  
Tadeusz Budlewski ◽  
Bogusław Kostkiewicz ◽  
...  
Keyword(s):  
Substance P ◽  
Biological Properties ◽  
Glioblastoma Cells ◽  
Who Grade ◽  
Primary Tumors ◽  
Physico Chemical ◽  
The Central Nervous System ◽  
Neurokinin 1 ◽  
Nanomolar Range

Gliomas, particularly WHO grade IV glioblastoma multiforme, are one of the most common and aggressive primary tumors of the central nervous system. The neuropeptide, substance P (SP), is the physiological ligand of the neurokinin-1 (NK-1) receptor that is consistently overexpressed in glioblastoma cells. The aim of this work was to study physico-chemical and biological properties of different SP analogues labeled with technetium-99m and lutetium-177 radionuclides. The synthesized compounds were characterized in vitro by partition coefficients (logP) and their stability was investigated in various physiological solutions. Biological properties (Kd, Bmax) were characterized using the U373 MG cell line. The obtained lipophilicity values of the [99mTc]NS3/CN-SP and [177Lu]DOTA-SP radiobioconjugates were in the range of −0.3 to +0.6 and −2.5 to −5.0, respectively. The studied radiobioconjugates were stable in PBS buffer and CSF, as well as in 10 mM histidine and/or cysteine solutions whereas in human serum showed enzymatic biodegradation. [177Lu]DOTA-[Thi8,Met(O2)11]SP(1–11), [177Lu]DOTA-SP(4–11) and [177Lu]DOTA-[Thi8,Met(O2)11]SP(5–11) radiobioconjugates bound specifically to NK-1 receptors expressed on glioblastoma cells with affinity in the nanomolar range. To conclude, the shorter analogues of SP can be used as vectors, nevertheless they still do not fulfil all requirements for preparations in nuclear medicine.

Na-doped β-tricalcium phosphate: physico-chemical and in vitro biological properties

2011 ◽  
Vol 22 (3) ◽  
pp. 593-600 ◽  
Author(s):  
Laëtitia Obadia ◽  
Marion Julien ◽  
Sophie Quillard ◽  
Thierry Rouillon ◽  
Paul Pilet ◽  
...  
Keyword(s):  
Tricalcium Phosphate ◽  
Biological Properties ◽  
Physico Chemical

THYROID STIMULATORS AND THYROID STIMULATION

1971 ◽  
Vol 66 (3) ◽  
pp. 558-576 ◽  
Author(s):  
Gerald Burke
Keyword(s):  
Regulatory System ◽  
Control Site ◽  
Thyroid Cell ◽  
Primary Control ◽  
Physico Chemical ◽  
Site Of Action ◽  
Long Acting

ABSTRACT A long-acting thyroid stimulator (LATS), distinct from pituitary thyrotrophin (TSH), is found in the serum of some patients with Graves' disease. Despite the marked physico-chemical and immunologic differences between the two stimulators, both in vivo and in vitro studies indicate that LATS and TSH act on the same thyroidal site(s) and that such stimulation does not require penetration of the thyroid cell. Although resorption of colloid and secretion of thyroid hormone are early responses to both TSH and LATS, available evidence reveals no basic metabolic pathway which must be activated by these hormones in order for iodination reactions to occur. Cyclic 3′, 5′-AMP appears to mediate TSH and LATS effects on iodination reactions but the role of this compound in activating thyroidal intermediary metabolism is less clear. Based on the evidence reviewed herein, it is suggested that the primary site of action of thyroid stimulators is at the cell membrane and that beyond the(se) primary control site(s), there exists a multifaceted regulatory system for thyroid hormonogenesis and cell growth.

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