Search results for "DISCOVERY"

New bioactive alkaloids from the marine sponge Stylissa sp.

2012

Abstract Chemical investigation of the Indonesian marine sponge Stylissa species, which was collected at 2008 from Derawan Islands, Berau, NE Kalimantan, Indonesia offered four new brominated alkaloids, including 12-N-methyl stevensine (1), 12-N-methyl-2-debromostevensine (2), 3-debromolatonduine B methyl ester (3), 3-debromolatonduine A (4) together with eight known alkaloids identified as Z-hymenialdisine, Z-debromohymenialdisine, Stevensine, 2-debromostevensine, 3-bromoaldizine, 3,4-dibromopyrrole-2-carbamide, latonduine A, and latonduine B methyl ester (5–12), respectively. The structures of all isolated compounds were unambiguously elucidated based on extensive 1D and 2D NMR spectrosco…

Artalbic acid, a sesquiterpene with an unusual skeleton from Artemisia alba (Asteraceae) from Sicily

2011

Abstract From the aerial parts of Artemisia alba (Asteraceae) artalbic acid ( 1 ), a sesquiterpene with an unusual skeleton, was isolated. Its structure was elucidated on the basis of extensive proton, 13 C and two-dimensional NMR experiments, as well as by transformation in its methyl ester derivative.

Donellanic acids A–C: new cyclopropanic oleanane derivatives from Donella ubanguiensis (Sapotaceae)

2012

Abstract Three new cyclopropanic oleanane triterpenoids and ten known compounds were obtained from Donella ubanguiensis using chromatographic methods. The structures were established on the basis of mass spectrometric and NMR data and by comparison with values reported in the literature. The structures of the new compounds were confirmed by X-ray crystallography. A part of the isolated compounds was evaluated for cytotoxic and antimicrobial activities.

Polyketides and nitrogenous metabolites from the endophytic fungus Phomopsis sp. D15a2a

2019

Abstract Three new polyketides, phomopones A−C (1–3), one new cyclic tetrapeptide, 18-hydroxydihydrotentoxin (4), and a new amide, 6-hydroxyenamidin (5) together with a known derivative, enamindin (6) were obtained from the endophytic fungus Phomopsis sp. D15a2a isolated from the plant Alternanthera bettzickiana. The structures of the new compounds were elucidated by 1D, 2D NMR and HRMS data. The absolute configurations of the isolated metabolites were determined either by X-ray crystallography, Marfey’s method or by converting the compounds to Mosher esters.

THE ROLE OF THROMBIN IN CENTRAL NERVOUS SYSTEM ACTIVITY AND STROKE

2018

Background. Thrombin is a key factor of hemostasis, mediating the conversion of fibrinogen into fibrin. Along with prothrombin, of which thrombin is the active derivative, it has been found locally expressed in the central nervous system. This article aims to describe the role of thrombin in the normal functioning of the central nervous system and stroke.Methods. In this mini-review, the specialized databases Medscape, PubMed, and Web of Science, from the years 2003-2018, were used to find relevant documents by using MeSH terms: ”thrombin” and ”stroke”.Results. Prothrombin and thrombin influence neural development, protection and regeneration, thrombin being a relatively strong regulating f…

Heterocyclisch anellierte Steroide aus 2-Hydroxymethylen-canrenon

1995

A-ring annulated heterocycles, the isoxazole 6, the pyrazoles 8 and the pyrimidines 9 are prepared starting from 2-hydroxymethylene canrenone 1. Binding studies were carried out with the compounds 1 and 6-8 using estrogen, progesterone, androgen, gluco- and mineralocorticoid receptors as well as the serum proteins SHBG and CBG: the substances were inactive on the receptor level. 1, 7 and 8a show weak binding affinity to CBG.

Potentiation of the cytotoxic activity of copper by polyphosphate on biofilm-producing bacteria: A bioinspired approach

2012

Adhesion and accumulation of organic molecules represent an ecologically and economically massive problem. Adhesion of organic molecules is followed by microorganisms, unicellular organisms and plants together with their secreted soluble and structure-associated byproducts, which damage unprotected surfaces of submerged marine structures, including ship hulls and heat exchangers of power plants. This is termed biofouling. The search for less toxic anti-biofilm strategies has intensified since the ban of efficient and cost-effective anti-fouling paints, enriched with the organotin compound tributyltin, not least because of our finding of the ubiquitous toxic/pro-apoptotic effects displayed b…

Cytotoxicity of the Urokinase-Plasminogen Activator Inhibitor Carbamimidothioic Acid (4-Boronophenyl) Methyl Ester Hydrobromide (BC-11) on Triple-Neg…

2015

BC-11 is an easily synthesized simple thiouronium-substituted phenylboronic acid, which has been shown to be cytotoxic on triple negative MDA-MB231 breast cancer cells by inducing a perturbation of cell cycle when administered at a concentration equal to its ED50 at 72 h (117 μM). Exposure of cells to BC-11, either pre-absorbed with a soluble preparation of the N-terminal fragment of urokinase-plasminogen activator (uPa), or in co-treatment with two different EGFR inhibitors, indicated that: (i) BC-11 acts via binding to the N-terminus of the enzyme where uPa- and EGF receptor-recognizing sites are present, thereby abrogating the growth-sustaining effect resulting from receptor binding

�ber den Nachweis des Erythropoetins in der Gewebekultur

1958

Autoantikörper gegen die Komplementkomponente C1q beim Systemischen Lupus Erythematodes

1990

Autoantibodies against C1q, a subcomponent of the first complement component C1, could be detected in 49.4% of sera from patients with systemic lupus erythematosus (SLE). They are directed against the collagen-like portion of the C1q molecule and recognize only bound, but not fluid-phase C1q. The appearance of these autoantibodies in the course of SLE correlates with the detection of IgG in the C1q-Solid-Phase-Bindingassay, with high titres of dsDNA-antibodies and with depressed total complement activity (CH50) and C1q-values. Our investigations show that autoantibodies against the collagen-like portion of bound C1q but not immune complexes are the main constituent of C1q-binding IgG in SLE.