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1.
Miral V. Lunagariya Khyati P. Thakor Bhargav N. Waghela Foram U. Vaidya Chadramani Pathak 《Journal of biomolecular structure & dynamics》2018,36(1):14-31
The square planar Pt(II) complexes of the type [Pt(Ln)(Cl2)] (where Ln = L1?3 = thiophene-2-carboxamide derivatives and L4?6 = thiophene-2-carbothioamide derivatives) have been synthesized and characterized by physicochemical and various spectroscopic studies. MIC method was employed to inference the antibacterial potency of complexes in reference to free ligands and metal salt. Characteristic binding constant (Kb) and binding mode of complexes with calf thymus DNA (CT-DNA) were determined using absorption titration (0.76–1.61 × 105 M?1), hydrodynamic chain length assay and fluorescence quenching analysis, deducing the partial intercalative mode of binding. Molecular docking calculation displayed free energy of binding in the range of –260.06 to –219.63 kJmol?1. The nuclease profile of complexes towards pUC19 DNA shows that the complexes cleave DNA more efficiently compared to their respective metal salt. Cytotoxicity profile of the complexes on the brine shrimp shows that all the complex exhibit noteworthy cytotoxic activity with LC50 values ranging from 7.87 to 15.94 μg/mL. The complexes have been evaluated for cell proliferation potential in human colon carcinoma cells (HCT 116) and IC50 value of complexes by MTT assay (IC50 = 125–1000 μg/mL). 相似文献
2.
3.
Hena Paul Buddhadeb Sen Tapan Kumar Mondal 《Nucleosides, nucleotides & nucleic acids》2017,36(8):520-542
Two new ruthenium(II) complexes of Schiff base ligands (L) derived from cinnamaldehyde and ethylenediamine formulated as [Ru(L)(bpy)2](ClO4)2, where L1 = N,N’-bis(4-nitrocinnamald-ehyde)ethylenediamine and L2 = N,N’-bis(2-nitrocinnamaldehyde)-ethylenediamine for complex 1 and 2, respectively, were isolated in pure form. The complexes were characterized by physicochemical and spectroscopic methods. The electrochemical behavior of the complexes showed the Ru(III)/Ru(II) couple at different potentials with quasi-reversible voltammograms. The interaction of the complexes with calf thymus DNA (CT-DNA) using absorption, emission spectral studies and electrochemical techniques have been used to determine the binding constant, Kb and the linear Stern–Volmer quenching constant, KSV. The results indicate that the ruthenium(II) complexes interact with CT-DNA strongly in a groove binding mode. The interactions of bovine serum albumin (BSA) with the complexes were also investigated with the help of absorption and fluorescence spectroscopy tools. Absorption spectroscopy proved the formation of a ground state BSA-[Ru(L)(bpy)2](ClO4)2 complex. The antibacterial study showed that the Ru(II) complexes (1 and 2) have better activity than the standard antibiotics but weak activity than the ligands. 相似文献
4.
Anna Halmikov Pavla Heringov Jana Kaprkov Francesco P. Intini Giovanni Natile Alina Nemirovski Dan Gibson Viktor Brabec 《Journal of inorganic biochemistry》2008,102(5-6):1077
Cytotoxicity and mutagenicity of trans,trans,trans-[PtCl2(CH3COO)2(NH3)(1-adamantylamine)] [trans-adamplatin(IV)] and its reduced analog trans-[PtCl2(NH3)(1-adamantylamine)] [trans-adamplatin(II)] were examined. In addition, the several factors underlying biological effects of these trans-platinum compounds using various biochemical methods were investigated. A notable feature of the growth inhibition studies was the remarkable circumvention of both acquired and intrinsic cisplatin resistance by the two lipophilic trans-compounds. Interestingly, trans-adamplatin(IV) was considerably less mutagenic than cisplatin. Consistent with the lipophilic character of trans-adamplatin complexes, their total accumulation in A2780 cells was considerably greater than that of cisplatin. The results also demonstrate that trans-adamplatin(II) exhibits DNA binding mode markedly different from that of ineffective transplatin. In addition, the reduced deactivation of trans-adamplatin(II) by glutathione seems to be an important determinant of the cytotoxic effects of the complexes tested in the present work. The factors associated with cytotoxic and mutagenic effects of trans-adamplatin complexes in tumor cell lines examined in the present work are likely to play a significant role in the overall antitumor activity of these complexes. 相似文献
5.
Studies on the synthesis,characterization, human serum albumin binding and biological activity of single chain surfactant–cobalt(III) complexes
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G. Vignesh K. Sugumar S. Arunachalam S. Vignesh R. Arthur James R. Arun K. Premkumar 《Luminescence》2016,31(2):523-532
The interaction of surfactant–cobalt(III) complexes [Co(bpy)(dien)TA](ClO4)3 · 3H2O (1) and [Co(dien)(phen)TA](ClO4)3 · 4H2O (2), where bpy = 2,2′‐bipyridine, dien = diethylenetriamine, phen = 1,10‐phenanthroline and TA = tetradecylamine with human serum albumin (HSA) under physiological conditions was analyzed using steady state, synchronous, 3D fluorescence, UV/visabsorption and circular dichroism spectroscopic techniques. The results show that these complexes cause the fluorescence quenching of HSA through a static mechanism. The binding constant (Kb) and number of binding‐sites (n) were obtained at different temperatures. The corresponding thermodynamic parameters (?G°, ?H° and ?S°) and Ea were also obtained. According to Förster's non‐radiation energy transfer theory, the binding distance (r) between the complexes and HSA were calculated. The results of synchronous and 3D fluorescence spectroscopy indicate that the binding process has changed considerably the polarity around the fluorophores, along with changes in the conformation of the protein. The antimicrobial and anticancer activities of the complexes were tested and the results show that the complexes have good activities against pathogenic microorganisms and cancer cells. Copyright © 2015 John Wiley & Sons, Ltd. 相似文献
6.
A series of complexes of Au(III) with nucleosides and nucleotides and their methyl derivatives in different stoichiometry have been prepared. Ultraviolet, visible, ir, and nmr studies have been performed to determine the site of binding of these ligands with the metal ion. In (1:4) Au(III): guanosine complex, N7 is the binding site, whereas at 1:1 complex, a bidentate type of chelation through C6O and N7 is observed. C6-NH2 is favored over N1 as coordinating site at all stoichiometry in the adenosine complex. Inosine binds through N1 at r = 1. In cytidine, N1 is the binding site, whereas thymidine reacts only at high pH. In the case of nucleotides a bidentate type of chelation through the phosphate and the ring nitrogen occurs. The phosphate binding ability of Au(III) was further confirmed by studying the interaction of Au(III) with dimethyl phosphate—a conformational analog of the phosphate backbone in DNA chain. 相似文献
7.
Li Xu Nan-Jing Zhong Hong-Liang Huang Zhen-Hua Liang Zheng-Zheng Li Yun-Jun Liu 《Nucleosides, nucleotides & nucleic acids》2013,32(8):575-591
Two new ruthenium(II) polypyridyl complexes [Ru(dmb)2(HECIP)](ClO4)2 (1) (HECIP = N-ethyl-4-[(1,10)-phenanthroline(5,6-f)imidazol-2-yl]carbazole, dmb = 4,4’-dimethyl-2,2’-bipyridine) and [Ru(dmp)2(HECIP)](ClO4)2 (2) (dmp = 2,9-dimethyl-1,10-phenanthroline) have been synthesized and characterized. The DNA-binding behaviors of the two complexes were investigated by absorption spectra, viscosity measurements, and photoactivated cleavage. The DNA-binding constants for complexes 1 and 2 were determined to be 8.03 (± 0.12) × 104 M?1 (s = 1.62) and 2.97 (± 0.15) × 104 M?1 (s = 1.82), respectively. The results suggest that these complexes interact with DNA through intercalative mode. The photocleavage of pBR322 DNA by Ru(II) complexes was investigated. The cytotoxicity of complexes 1 and 2 has been evaluated by the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide)] method. Complex 1 shows higher anticancer potency than 2 against the four tumor cell lines. Apoptosis and cellular uptake were investigated. The antioxidant activities of the ligand and these complexes were also performed. 相似文献
8.
Lucius H Haberland A Zaitsev S Dallüge R Schneider M Böttger M 《Molecular biology reports》2001,28(3):157-165
Relationships between the structure of transfecting complexes of histone H1 and DNA and their transfection efficiency were studied. Transfection activity proved to be connected to complex aggregates. Low speed centrifugation of the complexes resulted in loss of the transfection activity. The complexes/aggregates were active with high efficiency in a broad range of weight input ratios r
i (0.1<r
i<30). Using atomic force microscopy (AFM), the complexes were imaged at negative, nearly electroneutral and positive charge conditions. Electroneutral complexes at r
i=1 showed a multitude of different complex forms. Fibrillar, network-like and branched structures were frequently present in one complex. Strongly positive charged complexes had a toroidal appearance. All these different forms contributed to the high transfection efficiency. Cellular uptake is supposed to be by phagocytosis. 相似文献
9.
Darrouzet E Valkova-Valchanova M Ohnishi T Daldal F 《Journal of bioenergetics and biomembranes》1999,31(3):275-288
The ubiquinol: cytochrome c oxidoreductase, or the bc
1 complex, is a key component ofboth respiratory and photosynthetic electron transfer and contributes to the formation of anelectrochemical gradient necessary for ATP synthesis. Numerous bacteria harbor a bc
1 complexcomprised of three redox-active subunits, which bear two b-type hemes, one c-type heme, andone [2Fe–2S] cluster as prosthetic groups. Photosynthetic bacteria like Rhodobacter speciesprovide powerful models for studying the function and structure of this enzyme and are beingwidely used. In recent years, extensive use of spontaneous and site-directed mutants and theirrevertants, new inhibitors, discovery of natural variants of this enzyme in various species, andengineering of novel bc
1 complexes in species amenable to genetic manipulations have providedus with a wealth of information on the mechanism of function, nature of subunit interactions,and assembly of this important enzyme. The recent resolution of the structure of variousmitochondrial bc
1 complexes in different crystallographic forms has consolidated previousfindings, added atomic-scale precision to our knowledge, and raised new issues, such as thepossible movement of the Rieske Fe–S protein subunit during Qo site catalysis. Here, studiesperformed during the last few years using bacterial bc
1 complexes are reviewed briefly andongoing investigations and future challenges of this exciting field are mentioned. 相似文献
10.
Permentier HP Schmidt KA Kobayashi M Akiyama M Hager-Braun C Neerken S Miller M Amesz J 《Photosynthesis research》2000,64(1):27-39
Photosynthetically active reaction centre core (RCC) complexes were isolated from two species of green sulfur bacteria, Prosthecochloris (Ptc.) aestuarii strain 2K and Chlorobium (Chl.) tepidum, using the same isolation procedure. Both complexes contained the main reaction centre protein PscA and the iron–sulfur protein
PscB, but were devoid of Fenna–Matthews–Olson (FMO) protein. The Chl. tepidum RCC preparation contained in addition PscC (cytochrome c). In order to allow accurate determination of the pigment content of the RCC complexes, the extinction coefficients of bacteriochlorophyll
(BChl) a in several solvents were redetermined with high precision. They varied between 54.8 mM−1 cm−1 for methanol and 97.0 mM−1 cm−1 for diethylether in the QY maximum. Both preparations appeared to contain 16 BChls a of which two are probably the 132-epimers, 4 chlorophylls (Chls) a 670 and 2 carotenoids per RCC. The latter were of at least two different types. Quinones were virtually absent. The absorption
spectra were similar for the two species, but not identical. Eight bands were present at 6 K in the BChl a QY region, with positions varying from 777 to 837 nm. The linear dichroism spectra showed that the orientation of the BChl a QY transitions is roughly parallel to the membrane plane; most nearly parallel were transitions at 800 and 806 nm. For both
species, the circular dichroism spectra were dominated by a strong band at 807–809 nm, indicating strong interactions between
at least some of the BChls. The absorption, CD and LD spectra of the four Chls a 670 were virtually identical for both RCC complexes, indicating that their binding sites are highly conserved and that they
are an essential part of the RCC complexes, possibly as components of the electron transfer chain. Low temperature absorption
spectroscopy indicated that typical FMO–RCC complexes of Ptc. aestuarii and Chl. tepidum contain two FMO trimers per reaction centre.
This revised version was published online in June 2006 with corrections to the Cover Date. 相似文献
11.
Miral V. Lunagariya Khyati P. Thakor Bharat H. Pursuwani 《Nucleosides, nucleotides & nucleic acids》2013,32(8):455-483
AbstractSquare planar mononuclear platinum(II) complexes having general formula [Pt(Ln)Cl2], (where, Ln?=?L1–4) were synthesized with neutral bidentate heterocyclic 1,3,5-trisubstituted bipyrazole based ligands. The synthesized compounds were characterized by physicochemical method such as TGA, molar conductance, micro-elemental analysis and magnetic moment, and spectroscopic method such as, FT-IR, UV–vis, 1H NMR, 13C NMR and mass spectrometry. Biological applications of the compounds were carried out using in vitro brine shrimp lethality bioassay, in vitro antimicrobial study against five different pathogens, and cellular level cytotoxicity against Schizosaccharomyces pombe (S. Pombe) cells. Pt(II) complexes were tested for DNA interaction activities using electronic absorption titration, viscosity measurements study, fluorescence quenching technique and molecular docking assay. Binding constants (Kb) of ligands and complexes were observed in the range of 0.23–1.07?×?105?M?1 and 0.51–3.13?×?105?M?1, respectively. Pt(II) complexes (I–IV) display an excellent binding tendency to biomolecule (DNA) and possess comparatively high binding constant (Kb) values than the ligands. The DNA binding study indicate partial intercalative mode of binding in complex-DNA. The gel electrophoresis activity was carried out to examine DNA nuclease property of pUC19 plasmid DNA. 相似文献
12.
Khyati P. Thakor Miral V. Lunagariya Bhupesh S. Bhatt Mohan N. Patel 《Luminescence》2019,34(1):113-124
Novel palladium(II) complexes ( 7a–7e ) of substituted quinoline derivatives were synthesized. The complexes were characterized using various techniques such as thermogravimetric analysis (TGA), elemental analysis, conductance measurement, mass, absorption, infra‐red (IR), 1H NMR, 13C NMR and energy‐dispersive X‐ray spectroscopy (EDX). Complexes for herring sperm DNA (HS DNA) binding were explored and absorption titration and the binding constant (Kb) as well as Gibb's free energy were evaluated. Complex 7d exhibited the highest binding constant, therefore the thermodynamic parameters of 7d at different temperatures were evaluated. To support the results of the absorption titration, fluorescence titration, viscosity measurement and molecular docking studies were performed. The fluorescence quenching data as evaluated from Stern–Volmer equation were used to calculate KSV, Kf and the number of binding sites. The results of all these studies were in good agreement with the absorption study. DNA electrophoretic mobility was performed to explore the possible application of metal complexes as artificial metallonucleases. The antibacterial activity of the complexes was accessed against different pathogenic bacteria and cytotoxicity was measured using brine shrimp and S. pombe. 相似文献
13.
Sneana Rajkovi Biljana . Glii Marija D.
ivkovi Milo I. Djuran 《Bioorganic chemistry》2009,37(5):173-179
1H NMR spectroscopy was applied to study the reactions of cis-[Pd(L)(H2O)2]2+ complexes (L is en, pic and dpa) with the N-acetylated tripeptides L-methionylglycylglycine, MeCOMet–Gly–Gly, and glycyl–L-methionyl–glycine, MeCOGly–Met–Gly. All reactions were performed in the pH range 2.0–2.5 with equimolar amounts of the cis-[Pd(L)(H2O)2]2+ complex and the tripeptide at 60 °C. The hydrolytic reactions of the cis-[Pd(en)(H2O)2]2+, cis-[Pd(pic)(H2O)2]2+ and cis-[Pd(dpa)(H2O)2]2+ complexes with MeCOMet–Gly–Gly were regioselective and only the amide bond involving the carboxylic group of methionine was cleaved. However, in the reactions of these three Pd(II) complexes with MeCOGly–Met–Gly, two amide bonds, Met–Gly and MeCO–Gly, were cleaved. From UV–Vis spectrophotometry studies, it was found that the rate-determining step of these hydrolytic reactions is the monodentate coordination of the corresponding Pd(II) complex to the sulfur atom of the methionine side chain. The rate of the cleavage of these amide bonds is dependent on the nature of the bidentate coordinated diamine ligand L (en > pic > dpa). The hydrolytic reaction of cis-[Pd(L)(H2O)2]2+-type complexes with MeCOMet–Gly–Gly, containing the methionine side chain in the terminal position of the peptide, is regioselective while in the reaction of these Pd(II) complexes with MeCOGly–Met–Gly, none selective cleavage of the peptide occurs. This study contributes to a better understanding of the selective cleavage of methionine-containing peptides employing palladium(II) complexes as catalysts. 相似文献
14.
Antibacterial,antifungal and in vitro antileukaemia activity of metal complexes with thiosemicarbazones
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Elena Pahontu Felicia Julea Tudor Rosu Victor Purcarea Yurie Chumakov Petru Petrenco Aurelian Gulea 《Journal of cellular and molecular medicine》2015,19(4):865-878
1‐phenyl‐3‐methyl‐4‐benzoyl‐5‐pyrazolone 4‐ethyl‐thiosemicarbazone (HL) and its copper(II), vanadium(V) and nickel(II) complexes: [Cu(L)(Cl)]·C2H5OH·( 1 ), [Cu(L)2]·H2O ( 2 ), [Cu(L)(Br)]·H2O·CH3OH ( 3 ), [Cu(L)(NO3)]·2C2H5OH ( 4 ), [VO2(L)]·2H2O ( 5 ), [Ni(L)2]·H2O ( 6 ), were synthesized and characterized. The ligand has been characterized by elemental analyses, IR, 1H NMR and 13C NMR spectroscopy. The tridentate nature of the ligand is evident from the IR spectra. The copper(II), vanadium(V) and nickel(II) complexes have been characterized by different physico‐chemical techniques such as molar conductivity, magnetic susceptibility measurements and electronic, infrared and electron paramagnetic resonance spectral studies. The structures of the ligand and its copper(II) ( 2 , 4 ), and vanadium(V) ( 5 ) complexes have been determined by single‐crystal X‐ray diffraction. The composition of the coordination polyhedron of the central atom in 2 , 4 and 5 is different. The tetrahedral coordination geometry of Cu was found in complex 2 while in complex 4 , it is square planar, in complex 5 the coordination polyhedron of the central ion is distorted square pyramid. The in vitro antibacterial activity of the complexes against Escherichia coli, Salmonella abony, Staphylococcus aureus, Bacillus cereus and the antifungal activity against Candida albicans strains was higher for the metal complexes than for free ligand. The effect of the free ligand and its metal complexes on the proliferation of HL‐60 cells was tested. 相似文献
15.
New insights into the composition, molecular mass and stoichiometry of the protein complexes of plant mitochondria 总被引:20,自引:2,他引:18
Lothar Jänsch Volker Kruft Udo K. Schmitz Hans-Peter Braun 《The Plant journal : for cell and molecular biology》1996,9(3):357-368
Recently a powerful electrophoresis method for the native preparation and characterization of the respiratory protein complexes of mitochondria from fungi and mammals has been developed, which employs Coomassie dyes to introduce charge shifts on proteins (Schägger and von Jagow (1991) Anal. Biochem. 199, 223–231). The procedure, which is called ‘blue native-polyacrylamide gel electrophoresis’ (BN-PAGE), was modified and introduced for the analysis of mitochondria from higher plants. BN-PAGE of mitochondrial protein from potato allows the separation of nine distinct protein complexes between 100 and 1000 kDa and reveals novel results for their composition, molecular mass and stoichiometry. For the first time soluble mitochondrial protein complexes, like the HSP60 complex (750 kDa) and a complex of 200 kDa, which includes a formate dehydrogenase, are analysed by BN-PAGE. Complex I from potato (1000 kDa) is about 100 kDa larger than the corresponding enzyme from beef and can be resolved into more than 30 different subunits on a second gel dimension. The F1F0 ATP synthase (580 kDa) and the cytochrome c oxidase (160 kDa) from potato seem to contain more subunits than hitherto reported. Direct sequencing of subunits revealed that the F1 part of the F1F0 ATP synthase lacks the oligomycin sensitivity conferring protein (OSCP), which was reported to be present in F1 parts of dicotyledonous plants, but contains the ATPase inhibitory protein. N-terminal sequences of 16 mitochondrial proteins were obtained, several of which are presented for the first time from a plant source. BN-PAGE allows the preparation of mitochondrial protein complexes from gram amounts of plant tissue, as the procedure only requires milligram amounts of organelles. This potential of BN-PAGE is demonstrated by the separation and characterization of the mitochondrial enzyme complexes from Arabidopsis thaliana. Further analysis of organellar protein complexes by BN-PAGE will allow the generation of ‘protein maps’ from different tissues and developmental stages or from mutant plants. 相似文献
16.
Synthesis,Characterization, and Biological Activities of Pendant Arm‐Pyridyltetrazole Copper(II) Complexes: DNA Binding/Cleavage Activity and Cytotoxic Studies
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Shaik Mustafa Bommuluri Umamaheswara Rao Manubolu Surya Surendrababu Kalidindi Krishnam Raju Gollapalli Nageswara Rao 《化学与生物多样性》2015,12(10):1516-1534
2‐(1H‐Tetrazol‐5‐yl)pyridine ( L ) has been reacted separately with Me2NCH2CH2Cl?HCl and ClCH2CH2OH to yield two regioisomers in each case, N,N‐dimethyl‐2‐[5‐(pyridin‐2‐yl)‐1H‐tetrazol‐1‐yl]ethanamine ( L1 )/N,N‐dimethyl‐2‐[5‐(pyridin‐2‐yl)‐2H‐tetrazol‐2‐yl]ethanamine ( L2 ) and 2‐[5‐(pyridin‐2‐yl)‐1H‐tetrazol‐1‐yl]ethanol ( L3 )/2‐[5‐(pyridin‐2‐yl)‐2H‐tetrazol‐2‐yl]ethanol ( L4 ), respectively. These ligands, L1 – L4 , have been coordinated with CuCl2?H2O in 1 : 1 composition to furnish the corresponding complexes 1 – 4 . EPR Spectra of Cu complexes 1 and 3 were characteristic of square planar geometry, with nuclear hyperfine spin 3/2. Single X‐ray crystallographic studies of 3 revealed that the Cu center has a square planar structure. DNA binding studies were carried out by UV/VIS absorption; viscosity and thermal denaturation studies revealed that each of these complexes are avid binders of calf thymus DNA. Investigation of nucleolytic cleavage activities of the complexes was carried out on double‐stranded pBR322 circular plasmid DNA by using a gel electrophoresis experiment under various conditions, where cleavage of DNA takes place by oxidative free‐radical mechanism (OH ? ). In vitro anticancer activities of the complexes against MCF‐7 (human breast adenocarcinoma) cells revealed that the complexes inhibit the growth of cancer cells. The IC50 values of the complexes showed that Cu complexes exhibit comparable cytotoxic activities compared to the standard drug cisplatin. 相似文献
17.
Cristina Bolzati Nicola Salvarese Davide Carta Fiorenzo Refosco Alessandro Dolmella Hans Jürgen Pietzsch Ralf Bergmann Giuliano Bandoli 《Journal of biological inorganic chemistry》2011,16(1):137-155
This study presents the first application of a general procedure based on the use of the [Tc(N)Cl(PS)(PPh3)] species (PS is an alkyl phosphinothiolate ligand) for the preparation of Tc(N) target-specific compounds. [Tc(N)Cl(PS)(PPh3)] selectively reacts with an appropriate dithiocarbamate ligand (S∧Y) to give [Tc(N)(PS)(S∧Y)] compounds. 1-(2-Methoxyphenyl)piperazine, which displays a potent and specific affinity for 5HT1A receptors, was selected as a functional group and conjugated to the dithiocarbamate unit through different spacers (L
n
). [99mTc(N)(PS)(L
n
)] complexes were prepared in high yield (more than 90%). The chemical identity of 99mTc complexes was determined by high performance liquid chromatography comparison with the corresponding 99gTc complexes. All complexes were found to be inert toward transchelation with an excess of glutathione and cysteine. No notable
biotransformation of the native compound into different species by the in vitro action of the serum and liver enzymes was
shown. Nanomolar affinity for the 5HT1A receptor was obtained for [99mTc(N)(PSiso)L3] (IC50 = 1.5 nM); a reduction of the affinity was observed for the other complexes as a function of the shortening of the alkyl
chain interposed between the dithiocarbamate and the pharmacophore. Negligible brain uptake was found from in vivo distribution
data of [99mTc(N)(PSiso)L3]. The key finding of this study is that the complexes maintained good affinity and selectivity for 5HT1A receptors, and the IC50 value for [99gTc(N)(PSiso)L3] being comparable to the IC50 value found for WAY 100635. This result confirmed the possibility of preparing [99mTc(N)(PS)]-based target-specific compounds without affecting the affinity and selectivity of the bioactive molecules for the
corresponding receptors. 相似文献
18.
Khlood Abou Melha 《Journal of enzyme inhibition and medicinal chemistry》2013,28(2):285-295
The Schiff base ligand, oxalic bis[(2-hydroxybenzylidene)hydrazide], H2L, and its Cu(II), Ni(II), Co(II), UO2(VI) and Fe(III) complexes were prepared and tested as antibacterial agents. The Schiff base acts as a dibasic tetra- or hexadentate ligand with metal cations in molar ratio 1:1 or 2:1 (M:L) to yield either mono- or binuclear complexes, respectively. The ligand and its metal complexes were characterized by elemental analyses, IR, 1H NMR, Mass, and UV-Visible spectra and the magnetic moments and electrical conductance of the complexes were also determined. For binuclear complexes, the magnetic moments are quite low compared to the calculated value for two metal ions complexes and this shows antiferromagnetic interactions between the two adjacent metal ions. The ligand and its metal complexes were tested against a Gram + ve bacteria (Staphylococcus aureus), a Gram -ve bacteria (Escherichia coli), and a fungi (Candida albicans). The tested compounds exhibited high antibacterial activities. 相似文献
19.
Early stages in the formation of membranes and photosynthetic units were studied under growth-limiting phototrophic and chemotrophic conditions in cells of Rhodopseudomonas capsulata. The incorporation of polypeptides, forming bacteriochlorophyll-carotinoid-protein complexes in the membrane, was followed by use of pulse-labeling and immunoprecipitation techniques. The newly synthesized polypeptides were inserted into two distinct membrane fractions at both different rates and proportions. The two membrane fractions differed in sedimentation behavior, absorption spectra and activities of the respiratory chain. The individual pigment-associated proteins did not exhibit precursor-product relationship between the two membrane fractions. The data suggest that newly synthesized polypeptides were integrated both into cytoplasmic and pre-existing intracytoplasmic membranes, where the proteins and pigments were assembled to form reaction centers and light-harvesting pigment-protein complexes.Abbreviations Bchl
bacteriochlorophyll
- cpm
counts per minute
-
M
r
relative molecular mass
- P 100
pellet of 100,000xg, 60 min
- P300
pellet of 300,000xg, 90 min
-
pO2
oxygen partial pressure
-
R
Rhodopseudomonas
- dodecyl sulfate
sodium dodecyl sulfate. International standard units
- Bq
Becquerel (s-1)
- Pa
Pascal (N/m2; 1 Torr=133,3 Pa) 相似文献
20.
Mahboube Eslami Moghadam Adeleh Divsalar Abdolghafar Abolhosseini Shahrnoy Ali Akbar Saboury 《Journal of biomolecular structure & dynamics》2016,34(8):1751-1762
Imidazole analogs are the agents that attract both bioinorganic chemist and drug designer. Numerous methods have been proposed for synthesis of imidazole derivatives. In this study, a series of heterocyclic system with p-conjugated system such as 2-aryl-imidazo[4,5-f][1,10]phenanthroline analogs were synthesized. Then, three new palladium(II) complexes containing 2-(Furan-2-yl)-1H-Imidazo[4,5-f][1,10]Phenanthroline (FIP) and 2-(thiophen-2-yl)-1H-imidazo[4,5-f][1,10]phenanthroline (TIP) ligands were synthesized. The structures of the compounds, [Pd(Phen)(TIP)](NO3)2, [Pd(Phen)(FIP)](NO3)2, and [Pd(FIP)2]Cl were determined by spectroscopic methods and elemental analysis. Biological activity of the complexes synthesized was assessed against chronic myelogenous leukemia cell line, K562. Also, the interactions of human serum albumin with complexes were investigated using isothermal titration in the Tris buffer, pH 7.4. According to the results obtained, it was found that there is a set of six binding sites for these complexes on HSA with positive cooperativity in the binding process. Docking technique was also applied to confirm the experimental results. The results showed that smaller complexes have higher interaction affinity. 相似文献