Search results for "ALK"

Vascular Activity of (-)-Anonaine, (-)-Roemerine and (-)-Pukateine, Three Natural 6a(R)-1,2-Methylenedioxyaporphines with Different Affinities for α1…

2004

We have studied the mechanism of action of three 6a( R)-1,2-methylenedioxyaporphines as vasorelaxant compounds. The alkaloids assayed showed different affinities for the three human cloned alpha (1)-adrenoceptor (AR) subtypes stably expressed in rat-1 fibroblasts, showing lower affinity for alpha(1B)-AR with regard to the alpha(1A)- or alpha(1D)-subtypes. These three natural compounds are more potent inhibitors of [ (3)H]-prazosin binding than of [ (3)H]-diltiazem binding to rat cerebral cortical membranes. As all these alkaloids inhibited noradrenaline (NA)-induced [ (3)H]-inositol phosphate formation in cerebral cortex and rat tail artery, they may be safely viewed as alpha (1)-AR antagon…

A possible structural determinant of selectivity of boldine and derivatives for the alpha 1A-adrenoceptor subtype.

1996

1. The selectivity of action of boldine and the related aporphine alkaloids, predicentrine (9-O-methylboldine) and glaucine (2,9-O-dimethylboldine) and alpha 1-adrenoceptor subtypes was studied by examining [3H]-prazosin competition binding in rat cerebral cortex. WB 4101 and benoxathian were used as selective alpha 1A-adrenoceptor antagonists. 2. In the competition experiments [3H]-prazosin (0.2 nM) binding was inhibited by WB 4101 and benoxathian. The inhibition curves displayed shallow slopes which could be subdivided into high and low affinity components (pKi = 9.92 and 8.29 for WB 4101, 9.35 and 7.94 for benoxathian). The two antagonists recognized approximately 37% of the sites with h…

Reactive oxygen species (ROS) generation inhibited by aporphine and phenanthrene alkaloids semi-synthesized from natural boldine.

2004

Four phenanthrene and one aporphine alkaloids semi-synthesized from boldine were evaluated for their inhibitory effect on reactive oxygen species (ROS) generation. ROS generation by neutrophils stimulated with N-formyl-methionyl-leucyl-phenylalanine was inhibited in a concentration dependent manner. Alkaloids exerted similar inhibitory effect in the hypoxanthine-xanthine oxidase system than in stimulated neutrophils, which could be attributed to a direct ROS scavenging activity. None of the alkaloids assayed had any effect on xanthine oxidase activity. Therefore the synthesized alkaloids might constitute an alternative therapy in inflammation disorders in which ROS generation is involved.

2020

Abstract This paper shows global uniqueness in two inverse problems for a fractional conductivity equation: an unknown conductivity in a bounded domain is uniquely determined by measurements of solutions taken in arbitrary open, possibly disjoint subsets of the exterior. Both the cases of infinitely many measurements and a single measurement are addressed. The results are based on a reduction from the fractional conductivity equation to the fractional Schrodinger equation, and as such represent extensions of previous works. Moreover, a simple application is shown in which the fractional conductivity equation is put into relation with a long jump random walk with weights.

Marine Pyrrole Alkaloids

2021

Nitrogen heterocycles are essential parts of the chemical machinery of life and often reveal intriguing structures. They are not only widespread in terrestrial habitats but can also frequently be found as natural products in the marine environment. This review highlights the important class of marine pyrrole alkaloids, well-known for their diverse biological activities. A broad overview of the marine pyrrole alkaloids with a focus on their isolation, biological activities, chemical synthesis, and derivatization covering the decade from 2010 to 2020 is provided. With relevant structural subclasses categorized, this review shall provide a clear and timely synopsis of this area.

Effects of high intensity resistance aquatic training on body composition and walking speed in women with mild knee osteoarthritis : a 4-month RCT wi…

2017

Objective: To investigate the effects of 4-months intensive aquatic resistance training on body composition and walking speed in post-menopausal women with mild knee osteoarthritis (OA), immediately after intervention and after 12-months follow-up. Additionally, influence of leisure time physical activity (LTPA) will be investigated. Design: This randomised clinical trial assigned eighty-seven volunteer postmenopausal women into two study arms. The intervention group (n = 43) participated in 48 supervised intensive aquatic resistance training sessions over 4-months while the control group (n = 44) maintained normal physical activity. Eighty four participants continued into the 12-months' fo…

Gas-liquid chromatographic analyses

1983

Abstract The gas chromatography of mixtures of n -alkyl acetates (CH 3 COOR, R = C 1 —C 8 ) and methyl esters of aliphatic n -carboxylic acids (R′COOCH 3 , R′ = C 1 —C 8 ) and certain of their monochlorinated derivatives has been studied on Carbowax 20M and SE-30 glass capillary columns under the same operating conditions. The separation of the isomeric monochlorinated esters was complete on Carbowax 20M, whereas on SE-30 the peaks of 6- and 7-chlorooctyl acetates and methyl (ω − 1)- and (ω − 2)-chlorooctanoates and -nonanoates partly overlapped. The complete separation of the mixtures could not be achieved, however, on Carbowax 20M, in spite of the use of various operating conditions. The …

Speciation of Organic Matter in Natural Waters-interaction of polyacrylates and polymethacrylates with major cation components of seawater

2004

Abstract The speciation of some high molecular weight polycarboxylates was studied in different ionic media. Polyacrylates here investigated ( W =2.0, 5.1 and 20.0 kDa) form weak species with alkali metal cations ( K =10 2 mol l −1 , t =25 °C, I =0 mol l −1 ) and quite stable complexes with alkaline earth metal cations ( K >10 6 mol l −1 , t =25 °C, I =0 mol l −1 ). Results are reported from experiments performed in a multicomponent electrolyte solution simulating the major composition of seawater (artificial seawater). Protonation constants in this medium are expressed as a polynomial function of S 1/2 ( S =salinity) and the sharp lowering with respect to values obtained in non-interacting…

Polyacrylate Protonation in Various Aqueous Ionic Media at Different Temperatures and Ionic Strengths

2000

The protonation constants of the polyacrylate anion (molecular mass 2000 Da) in Et4NI, Me4NCl, LiCl, LiNO3, NaCl, NaNO3, and KCl aqueous solution, were determined in a wide range of ionic strengths. A three-parameter approximation was used to express protonation constants as a function of the dissociation degree α, and their dependence on ionic strength was considered using a simple polynomial expansion. Differences in log KH between different data in different media were interpreted in terms of weak complex formation between polyacrylate and alkali metal cations. Measurements were also performed at different temperatures (15 ≤ T/°C ≤ 55) in order to calculate enthalpy and entropy changes f…

Sequestration of alkyltin(IV) cations by complexation with amino-polycarboxylic chelating agents

2013

Abstract The binding capacity of four amino-polycarboxylic ligands (APCs) [nitrilotriacetate (NTA), ethylenediamine- N , N , N′ , N′ -tetraacetate (EDTA), (S,S)-ethylenediamine- N , N ′-disuccinic acid (S,S-EDDS) and diethylenetriamine- N , N , N′ , N″ , N″ -pentaacetate (DTPA)] towards mono-, di- and tri-alkyltin(IV) cations [(CH 3 )Sn 3 + , (CH 3 ) 2 Sn 2 + , (C 2 H 5 ) 2 Sn 2 + , (CH 3 ) 3 Sn + or (C 2 H 5 ) 3 Sn + ] was studied, in aqueous solutions, by ISE-H + potentiometry, at I  = 0.1 mol L − 1 (NaCl) and at T  = 298.15 K. In all the systems R x Sn (4 − x)+  − APC (R = CH 3 or C 2 H 5 ) a strong 1:1 species is formed together with protonated, hydroxo and dinuclear complexes. The valu…