Abstract：
:The strength of inhibition of beta-hematin (synthetic hemozoin or malaria pigment) formation by the quinoline antimalarial drugs chloroquine, amodiaquine, quinidine and quinine has been investigated as a function of incubation time. In the assay used, beta-hematin formation was brought about using 4.5M acetate, pH 4.5 at 60 degrees C. Unreacted hematin was detected by formation of a spectroscopically distinct low spin pyridine complex. Although, these drugs inhibit beta-hematin formation when relatively short incubation times are used, it was found that beta-hematin eventually forms with longer incubation periods (<8h for chloroquine and >8h for quinine). This conclusion was supported by both infrared and X-ray powder diffraction observations. It was further found that the IC(50) for inhibition of beta-hematin formation increases markedly with increasing incubation times in the case of the 4-aminoquinolines chloroquine and amodiaquine. By contrast, in the presence of the quinoline methanols quinine and quinidine the IC(50) values increase much more slowly. This results in a partial reversal of the order of inhibition strengths at longer incubation times. Scanning electron microscopy indicates that beta-hematin crystals formed in the presence of chloroquine are more uniform in both size and shape than those formed in the absence of the drug, with the external morphology of these crystallites being markedly altered. The findings suggest that these drugs act by decreasing the rate of hemozoin formation, rather than irreversibly blocking its formation. This model can also explain the observation of a sigmoidal dependence of beta-hematin inhibition on drug concentration.
journal_name
J Inorg Biochemjournal_title
Journal of inorganic biochemistryauthors
Egan TJ,Ncokazi KKdoi
10.1016/j.jinorgbio.2005.04.013subject
Has Abstractpub_date
2005-07-01 00:00:00pages
1532-9issue
7eissn
0162-0134issn
1873-3344pii
S0162-0134(05)00110-8journal_volume
99pub_type
杂志文章abstract：:The preparation, spectral properties, and crystal structure of a copper(II) complex of 4-acetyl-N-[(cyclohexylamino)carbonyl]benzenesulfonamide, which is known as acetohexamide, and pyridine are reported. The complex Cu(AH)2(py)2, where AH = acetohexamide and py = pyridine, was prepared and characterized by X-ray and ...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/0162-0134(90)84012-e
更新日期：1990-03-01 00:00:00
abstract：:The novel anticancer drug ([[trans-PtCl(NH(3))(2)](2)-mu-[trans-Pt(NH(3))(2)(NH(2)(CH(2))(6)NH(2))(2)]](NO(3))(4)) (BBR3464, 1,0,1/t,t,t, TPC) forms a 1,4-interstrand cross-linked adduct with the self-complementary DNA octamer 5'-d(ATG*TACAT)(2)-3', with the two platinum atoms coordinated in the major groove at N7 pos...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2004.07.011
更新日期：2004-10-01 00:00:00
abstract：:Some new derivatives of Co(II), Co(III), Ni(II), Cu(II), and Zn(II) with 5' AMP have been obtained, characterized by elemental analysis, infrared, electronic, and fluorescence spectroscopy. The activities of these complexes as substitutes of 5' AMP as allosteric activators of glycogen phosphorylase b have been tested....
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/0162-0134(85)80011-8
更新日期：1985-11-01 00:00:00
abstract：:Protein tyrosine nitration, protein oxidation and lipid peroxidation are nitrative/oxidative modification of protein and lipids. In this paper, a BSA (bovine serum albumin)-lecithin liposome system was used to study the nature of different forms of iron, including methemoglobin, hemin and ferric citrate, in catalyzing...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2009.01.020
更新日期：2009-05-01 00:00:00
abstract：:Three novel copper(II) compounds of formulas {[Cu(Phen)(Ala)]·NO3·H2O}n (1), {[Cu(Phen)(Ala)]·NO3}n (2) and [Cu(Ala)2]n (3) have been synthesized and determined by X-ray diffraction. 1 and 2 are shown in one dimensional long-chain chiral structures, and 3 is a two dimensional checkerboard-type structure. Both 1 and 2 ...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2016.01.007
更新日期：2016-03-01 00:00:00
abstract：:An examination was made of the effects of tetrathiomolybdate (TTM), ammonium molybdate (AM), sodium sulphide, and two molybdo amino acids (cysteine-Mo, cysteine-Mo-S) on the distribution of Cu and Zn among proteins in extracts of the livers and kidneys of rats and sheep. Tetrathiomolybdate caused a shift in the chroma...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/0162-0134(87)80002-8
更新日期：1987-11-01 00:00:00
abstract：:Cadmium ions applied to either (outer or inner) surface of the isolated toad skin dose-dependently increased the short-circuit current (SCC), the potential difference (V) and the active sodium conductance (G(Na)) in the concentration range 0.07-0.50mM. Maximal stimulatory effect was over 30% with an EC(50) of about 0....
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2005.09.003
更新日期：2005-12-01 00:00:00
abstract：:We study the thermal unfolding of amicyanin by quantifying the resiliency of the native state to structural perturbations. Three signatures characterizing stages of unfolding are identified. The first signature, lateral extension of the polypeptide chain, is calculated directly from the reported crystallographic data....
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2017.11.016
更新日期：2018-02-01 00:00:00
abstract：:In this paper we present the studies on coordination abilities of two short-chain analogues of somatostatin with free N-terminal and protected amino group towards copper (II) ions. The octreotide is the most popular analogue of the somatostatin (peptide hormone) used in medicine. Somatostatin analogues are used in dia...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2012.08.023
更新日期：2012-12-01 00:00:00
abstract：:The complexation of uranium(VI) to variant functional groups of the highly phosphorylated protein phosvitin in aqueous solution was investigated by attenuated total reflection Fourier transform infrared (ATR FT-IR) spectroscopy. For the verification of the affinity of the actinyl ions to carboxyl and phosphate groups ...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2010.03.004
更新日期：2010-07-01 00:00:00
abstract：:The results are reported of a potentiometric and spectroscopic study of the H+, Cu2+, and Ni2+ complexes of luteinizing hormone-releasing hormone (LHRH, HL) at 25 degrees C and an ionic strength 0.10 mol dm-3 (KNO3), since there is much evidence that the in vivo release of LHRH is influenced by the concentration of co...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/0162-0134(88)80030-8
更新日期：1988-05-01 00:00:00
abstract：:Ti-containing alpha-Keggin polyoxometalates (POMs) have been proved with properties of both anti-tumor and anti-HIV (human immunodeficiency virus). The potential anti-SARS (severe acute respiratory syndrome) activity of the POMs [alpha-PTi(2)W(10)O(40)](7-) isomers was investigated in this paper by molecular modeling ...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2006.08.013
更新日期：2007-01-01 00:00:00
abstract：:Prion diseases are neurodegenerative disorders associated with a conformational change of the normal cellular isoform of the prion protein (PrP(C)) to an abnormal scrapie isoform (PrP(Sc)). human prion protein (hPrP(C)) is able to bind up to six Cu(II) ions. Four of them are distributed in the octarepeat domain, conta...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2015.11.015
更新日期：2016-02-01 00:00:00
abstract：:Biological studies on [Fe(L)2](NO3).0.5H2O (1), [Fe(L)2][PF6] (2), [Co(L)2](NCS) (3), [Ni(HL)2]Cl2.3H2O (4) and Cu(L)(NO3) (5), where HL=C7H8N4S, pyridine-2-carbaldehyde thiosemicarbazone, have been carried out. The crystal structure of compound 3 has been solved. It consists of discrete monomeric cationic entities co...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/s0162-0134(01)00184-2
更新日期：2001-04-01 00:00:00
abstract：:The entire polypeptide of hyperthermophilic Pyrococcus furiosus rubredoxin was synthesized in order to specifically probe structural determinants of protein thermostability. The uv-visible, circular dichroic, electron paramagnetic, and nuclear magnetic resonance spectra, and electrochemical properties, of the native a...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/s0162-0134(96)00079-7
更新日期：1997-01-01 00:00:00
abstract：:Complexes of cadmium(II) derivatives with adenine from water or by simulation of physiological conditions are obtained. The complexes have been studied by spectroscopic, conductometric, 1H-NMR, and by TG and DSC measurements. Possible coordination modes of the ligand are proposed. ...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/0162-0134(87)80023-5
更新日期：1987-02-01 00:00:00
abstract：:Preparations of cis- and trans-platinum(II) complexes of diethyl (pyridin-4-ylmethyl)phosphate (4-pmOpe) have been described. These complexes were identified and characterized by far-IR, 1H NMR, 13C NMR, 31P NMR and 195Pt NMR and microanalyses. The crystal and molecular structure of trans-platinum(II) complex i.e., tr...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2005.06.030
更新日期：2005-10-01 00:00:00
abstract：:Electrospray mass spectrometry (ESMS) of certain peptides labelled with (99m)Tc via hydrazinonicotinamide (HYNIC) with tricine as co-ligand shows one Tc-bound tricine, whereas typically two are observed. We speculated that this was due to coordination of a neighbouring histidine (His) or glutamate (Glu). To investigat...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2009.04.007
更新日期：2009-07-01 00:00:00
abstract：:A series of ethylenediamine platinum(IV) complexes of the type PtIV(en)XA2 and PtIV(en)X'2A2, where X = 1,1-cyclobutanedicarboxylato or malonato, X' = chloro, cyclobutanecarboxylato, cyclopentanecarboxylato, or cyclohexanecarboxylato, and A = acetato or trifluoroacetato were synthesized and characterized by elemental ...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/0162-0134(93)80015-2
更新日期：1993-05-01 00:00:00
abstract：:The conformation of poly[d(T-G).d(C-A)] in aqueous solution (0.1 M NaClO4, 5 mM cacodylic acid buffer, pH 6.9) was studied by circular dichroism (CD) spectroscopy in the ultraviolet. The conformation of the polynucleotide, as reflected by its chiroptical signature, changes in a highly cooperative fashion in the presen...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/0162-0134(91)84066-i
更新日期：1991-07-01 00:00:00
abstract：:A number of oxidovanadium(IV) complexes have been reported to display anticancer activity. A theranostic approach, based on the simultaneous observation of both the effect of oxidovanadium(IV) complexes on cell viability and the disclosure of their intracellular fate, is possible by using oxidovanadium(IV) complexes f...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2017.02.009
更新日期：2017-05-01 00:00:00
abstract：:The effect of Cu(II), Ni(II), Zn(II), Mg(II), and Mn(II) on the fluorescence of porcine kidney cytosol leucine aminopeptidase and three of its dansyl(Dns) peptide substrates, Leu-Gly-NHNH-Dns, Leu-Gly-NH(CH2)2NH-Dns, and Leu-Gly-NH(CH2)6NH-Dns, has been investigated. These five metal ions were chosen for study because...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/0162-0134(88)80013-8
更新日期：1988-01-01 00:00:00
abstract：:Tree laccase, a multi-copper oxidase, has been studied as a copper donor in conjunction with the demetalated forms of three blue copper proteins. Copper transfer could be observed under reducing conditions in the absence of air. Only about 10% of the total copper in laccase could be transferred regardless of the amoun...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/0162-0134(91)80017-c
更新日期：1991-03-01 00:00:00
abstract：:Recent stopped-flow kinetics demonstrated the existence of an intermediate before the occurrence of the final product of the reaction of both iron-containing microperoxidase-8 (Fe(III)MP-8) and manganese-containing microperoxidase-8 (Mn(III)MP-8) with H(2)O(2). The intermediate was assigned to be (hydro)peroxo-iron. W...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章,评审
doi：10.1016/s0162-0134(02)00393-8
更新日期：2002-07-25 00:00:00
abstract：:Aluminum salts such as aluminum chlorohydrate (ACH) are known for use as an active antiperspirant agent that blocks the secretion of sweat. A local case report of hyperaluminemia in a woman using an aluminum-containing antiperspirant for 4 years raises the problem of transdermal absorption of aluminum (Al). Only a ver...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2012.02.013
更新日期：2012-05-01 00:00:00
abstract：:Nitroxyl (HNO) has gained interest as a potential treatment of congestive heart failure through the ability of the HNO donor, Angeli's salt (AS), to evoke positive inotropic effects in canine cardiac muscle. The release of nitrite during decomposition limits the use of AS requiring other HNO sources. Acyloxy nitroso c...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2012.07.023
更新日期：2013-01-01 00:00:00
abstract：:The coordination modes of Cu(II) to alpha-casein (90-95) and alpha-casein (90-96) peptides with opioid activity isolated from pepsin hydrolisates of alpha-casein were investigated by means of electron paramagnetic resonance, absorption, and circular dichroism spectroscopy and potentiometry. The results allow the ident...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/s0162-0134(96)00147-x
更新日期：1997-04-01 00:00:00
abstract：:The antitumor activity of a ruthenium(II) polypyridyl complex, Δ-[Ru(bpy)2(HPIP)](ClO4)2 (Δ-Ru1, where bpy=2,2'-bipyridine, HPIP=2-(2-hydroxyphenyl)imidazo[4,5-f][1,10]phenanthroline), was evaluated. The in vivo experiments showed that Δ-Ru1 inhibited the growth of a human cervical carcinoma cell line (HeLa) xenotrans...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2015.02.003
更新日期：2015-05-01 00:00:00
abstract：:The importance of electrostatic interactions between buried charges in determining the properties of membrane proteins is considered. It is demonstrated that in some cases altered properties may result from the extraction of a membrane protein into an aqueous medium even when the protein conformation is unperturbed. ...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/0162-0134(85)85028-5
更新日期：1985-03-01 00:00:00
abstract：:Terpyridine-platinum(II) (TP-Pt(II)) complexes are known to possess DNA-intercalating activity and have been regarded as potential antitumor agents. However, their cytotoxic mechanism remains unclear. To investigate the possible mechanism, a series of TP-Pt(II) compounds were prepared and their biological activities a...
journal_title：Journal of inorganic biochemistry
pub_type： 杂志文章
doi：10.1016/j.jinorgbio.2009.05.006
更新日期：2009-07-01 00:00:00
