bluuebunny/crossref_metadata_2025 huggingface dataset:
Reduction of Lung Metastases by Na[trans‐RuCl4(DMSO)Im] is notCoupled With the Induction of Chemical Xenogenization
Authors: Sava G. , Salerno G. , Bergamo A. , Cocchietto M. , Gagliardi R. , Alessio E. , Mestroni G.
Published: March 2007

The effects of the treatment of tumor cells of MCa mammary carcinoma and TLX5 lymphoma with
the ruthenium complex Na[trans‐RuCl4(DMSO)lm] for several transplant generations were studied on
tumor growth and metastases formation. On TLX5 lymphoma cells, treatment was performed in vitro
prior to in vivo inoculation of tumor cells in intact or immunesuppressed mice. Either considering tumor
take and growth or its capacity to invade the brain of the inoculated hosts, Na[trans‐RuCl4(DMSO)lm] did not induce any significant modification. Conversely, in mice with MCa mammary carcinoma, the
in
vivo treatment of tumor cells in immunesuppressed hosts caused a progressive increase of DNA activity
and, starting from the 4th transplant generation, a significantly increased susceptibility of lung
metastasis formation to a further treatment in intact mice. These data seem to suggest that Na[trans‐RuCl4(DMSO)Im] does not induce chemical xenogenization of tumor cells nor its repeated treatment
induces resistance in tumor cells. Conversely, it appears that Na[trans‐RuCl4(DMSO)lm] may select a
tumor cell population which maintains its capacity to metastasise to the lung but with enhanced
sensitivity to the antimetastatic properties of this compound.
Triphenyltin Ortho‐Aminophenyl‐ and 2‐Pyridyl‐Thiolates:Synthesis and In Vitro Antitumour Activity
Authors: Gielen Marcel , Bouhdid Abdeslam , Tiekink Edward R. T. , de Vos Dick , Willem Rudolph
Published: March 2007

The synthesis, spectroscopic characterization and in vitro antitumour activity of two triorganotin
compounds, triphenyltin ortho‐aminophenylthiolate (1) and triphenyltin 2‐pyridylthiolate,
compound (2) are reported. The structure of 1 is confirmed by X‐ray diffraction, with the tin atom in
a distorted tetrahedral geometry because of monodentate coordination, as a thiolate (Sn‐S
2.431(2) Å), of the ortho‐aminophenylthiolate ligand. The in vitro antitumour activities of 1 and 2,
against a number of cell lines, are comparable to those exhibited by methotrexate and doxorubicin,
and higher than those of carboplatin and cisplatin.
Complexes With Biologically Active Ligands. Part 4. CoordinationCompounds of Chlorothiazide With Transition Metal Ions Behave asStrong Carbonic Anhydrase Inhibitors
Authors: Supuran Claudiu T.
Published: March 2007

Complexes of the diuretic benzothiadiazine derivative chlorothiazide (6‐chloro‐7‐sulfamoyl‐
1,2,4‐benzothiadiazine‐1,1‐dioxide) with V(IV); Fe(II); Co(II); Ni(II); Cu(II), Ag(I) and U(VI) were
prepared and characterized by elemental analysis, spectroscopic, thermogravimetric, magnetic and
conductimetric measurements. The complexes behave as effective inhibitors for two isozymes (I and II) of
carbonic anhydrase (CA).
Genotoxicity of Some Metal‐Based Antineoplastics, Evaluated by SOS Chromotest and Cytogenetic Analysis
Authors: Socaciu Carmen , Pasca Loan , Silvestru Cristian , Haiduc Ionel
Published: March 2007

The paper reports the screening results of two metal‐based antineoplastic drugs with mutagenic
potential, such as Romcis (trademark of Cisplatinum, produced in Romania) and diphenylantimony(III)
diisopropyldithiophosphate (PADTF). Their effects were compared with those induced by
Cyclophosphamide. Two mutagenicity tests, the SOS Chromotest and cytogenetic analysis were
applied. The tests were carried out with or without metabolic activation (addition of S9‐mix), either in E.
coli PQ 37 cultures, using four doses (0.3, 3, 30 and 300 pmol compound/assay) for the SOS
Chromotest or in leukocyte cultures using 0.3 mM from each compound, for cytogenetics. The dose‐
response relationships and SOSIP values revealed an indirect mutagenic potential for
Cyclophosphamide, amplified by S9 mix in bacterial cultures and an antiproliferative, clastogenic effect
on lymphocytes. For Romcis and diphenylantimony(III) diisopropyldithiophosphate, a significant positive
response by SOS Chromotest was recorded, which correlated with increased frequencies of
chromosomal aberrations.
Metal Ions in Neuroscience
Authors: Ragan C. Ian
Published: March 2007

Metal ions are believed to participate in many neurodegenerative conditions. In excitotoxic cell death there is convincing evidence for the participation of Ca2+ and Zn2+ ions although the exact molecular mechanisms by which these metals exert their effects are unclear. Only in one instance has the metal binding site of metalloenzymes been exploited for therapeutic purposes and this is the use of Li+ in the treatment of bipolar affective disorder. Again the exact molecular target is not clear but is likely to involve a Mg2+‐dependent enzyme of an intracellular signalling pathway. In Parkinson′s disease, the selective loss of dopaminergic neurones in the substantia nigra may be caused by radical‐mediated damage and there is good evidence to suggest that Fe2+ or 3+ is important in promoting formation of radical species. The evidence that free radicals are important in mediating other neurodegenerative conditions is less strong but still substantial enough to suggest that removal of reactive oxygen species or preventing their formation may be a valid approach to therapy.
Antiviral Metal Complexes
Authors: De Clercq Erik
Published: March 2007

The initial events (virus adsorption and fusion with the cells) in the replicative cycle of
human immunodeficiency virus (HIV) can serve as targets for the antiviral action of metal‐binding
compounds such as polyanionic compounds (polysulfates, polysulfonates, polycarboxylates,
polyoxometalates, and sulfonated or carboxylated metalloporphyrins), bicyclams and G‐octet‐forming oligonucleotides. The adsorption and fusion of HIV with its target cells depends on the interaction of the viral envelope glycoproteins (gp 120) with the receptors (CD4, CXCR4) at the
outer cell membrane. We are currently investigating how the aforementioned compounds interfere
with these viral glycoproteins and/or cell receptor.
Complexes With Biologically Active Ligands. Part 101 Inhibition of Carbonic Anhydrase Isozymes I and II With Metal Complexes of Imidazo[2, 1 − b]‐1,3,4‐Thiadiazole‐2‐Sulfonamide
Authors: Scozzafava Andrea , Supuran Claudiu T.
Published: March 2007

The title compound was prepared by an improved variant of the literature procedure, and metal complexes containing its anion and the following metal ions: Zn(II), Cd(II), Hg(II), Co(II), Ni(II), Cu(II), V(IV), Fe(III) and Ag(I) were synthesized and characterized by standard procedures (elemental analysis; IR, electronic, NMR and EPR spectroscopy; TG, magnetic and conductimetric measurements). The parent sulfonamide and its metal complexes are potent inhibitors of two carbonic anhydrase (CA) isozymes, CA I and II, and they might possess applications as selective cerebrovasodilating agents.
Di‐n‐Butyl‐, Tri‐n‐Butyl‐ and Triphenyltin dl‐Terebates: Synthesis, Characterization and In Vitro Antitumour Activity
Authors: Gielen Marcel , Ma Huairang , Bouhdid Abdeslam , Dalil Hassan , Biesemans Monique , Willem Rudolph
Published: March 2007

Di‐n‐butyltin, tri‐n‐butyltin and triphenyltin terebates were screened against several human tumour cell lines and found comparably or more active than carboplatin, cis‐platin, 5‐fluorouracil, methotrexate and doxorubicin, some reference compounds used clinically.
Behaviour of the Antitumor Agent Vanadocene Dichloride in Physiological and Therapeutic Media, Blood Plasma and Human Blood ‐ An EPR Study
Authors: Vinklárek Jaromír , Pavlík Ivan , Černošek Zdenĕk
Published: March 2007

By means of EPR spectroscopy the behaviour of the vanadocene dichloride (I), Cp2VCl2 (Cp = η5‐C5H5), in various deoxygenated and non‐deoxygenated physiological media and therapeutic solution as well as in blood plasma and stabilized human blood was studied. On the basis of measured values of isotropic spectroscopic splitting factor giso and isotropic hyperfine coupling constant Aiso, the vanadocene species, (II; giso= 1.985, |Aiso| = 7.68 mT), (III; giso= 1.983, |Aiso| = 7.92 mT), Cp2V(OH) 2 (IV; giso= 1.991, |Aiso| = 6.285 mT), (V; giso= 1.985, |Aiso| = 7.69 mT), the vanadyl species (VI; giso= 1.964, |Aiso| = 10.78mT) and (VII; giso= 1.955, |Aiso| = 11.56 mT) have been identified. From the measurements it follows that I does not react in its first coordination sphere with any component of a system used other than water and DMSO, resp. As to water‐containing media, its behaviour is fully consistent with that of I in pure aqueous media. It was found the only vanadocene species present after application of the therapeutic solution of I into human blood to be IV not interacting in its first coordination sphere with any blood component.
Synthesis, Characterisation and Antifungal Activities of Some New Copper(II) Complexes of Isomeric 3,5,7,7,10,12,14,14‐Octamethyl‐1,4,8,11‐Tetraazacyclotetradecanes
Authors: Hazari Saroj K. S. , Roy Tapashi G. , Dey Benu K. , Das Suvash C. , Tiekink Edward R. T.
Published: March 2007

Three isomeric Me8[14]anes, LA, LB and LC, undergo complexation with copper(II) salts to form a series of complexes where L = LA, LB and LC; X = Cl, Br, NO3; n, x, y and z may have values of 0, 1 or 2. The complexes have been characterised on the basis of analytical, spectroscopic, magnetic and conductance data. Further, the X‐ray crystal structure of one complex, , has been determined. The antifungal activity of all three isomeric ligands and their complexes has been investigated against a range of phytopathogenic fungi.
Structural and Biological Behaviour of Co(II), Cu(II) and Ni(II) Metal Complexes of Some Amino Acid Derived Schiff‐Bases
Authors: Chohan Zahid H. , Praveen M. , Ghaffar A.
Published: March 2007

Biologically active tridentate amino acid (Alanine, Glycine & Tyrosine) derived Schiff‐bases and their Co(II), Cu(II) & Ni(II) complexes have been synthesised and characterised
on the basis of their conductance and magnetic measurements, elemental analysis and  13C‐NMR,  1H‐NMR, IR and electronic spectral data. These Schiff‐bases and their complexes have been evaluated for their antibacterial activity against bacterial species such as Staphylococcus aureus, Escherichia coli, Klebsiella pneumonae, Proteus vulgarus and Pseudomonas aeruginosa and this activity data show the metal complexes to be more
antibacterial than the Schiff‐bases against one or more bacterial species.
Antitumor Activity of the Carboplatin‐α‐Cyclodextrin Adduct
Authors: Liu Weiping , Xiong Huizhou , Yang Yikun , Li Ling , Shen Zhiqiang , Chen Zhihe
Published: March 2007

Antitumor activity of the adduct between Carboplatin and α‐cyclodextrin has been tested against Sarcoma 180 (S180) and Ehrlich ascites carcinoma (EAC) murine tumors. The preliminary toxicity has also been evaluated by histological examinations of the treated animals. The results show the adduct has less antitumor efficacy than and similar toxicity to Carboplatin.
Carbonic Anhydrase Inhibitors. Part 541: Metal Complexes of Heterocyclic Sulfonamides: A New Class of Antiglaucoma Agents
Authors: Supuran Claudiu T. , Scozzafava Andrea , Jitianu Andrei
Published: March 2007

Metal complexes of heterocyclic sulfonamides possessing carbonic anhydrase (CA) inhibitory properties were recently shown to be useful as intraocular pressure (IOP) lowering agents in experimental animals, and might be developed as a novel class of antiglaucoma drugs. Here we report the synthesis of a heterocyclic sulfonamide CA inhibitor and of the metal complexes containing main group metal ions, such as Be(II), Mg(II), Al(III), Zn(II), Cd(II) and Hg(II) and the new sulfonamide as well as 5‐amino‐1,3,4‐thiadiazole‐2‐sulfonamide as ligands. The new complexes were characterized by standard physico‐chemical procedures, and assayed as inhibitors of three CA isozymes, CA I, II and IV. Some of them (but not the parent sulfonamides) strongly lowered IOP in rabbits when administered as a 2% solution into the eye.
Reactions of Pd(II) and Pt(II) Complexes With Tetraethylthiouram Disulfide
Authors: Cervantes G. , Moreno V. , Molins E. , Miravitlles C.
Published: March 2007

The reactions of tetraethylthiouram disulfide (DTS), an inhibitor of the nephrotoxicity of Pt(II) drugs, an efficient agent in the treatment of chronic alcoholism, in the treatment of HIV infections, AIDS and heavy metal toxicity, and a fungicide and herbicide, with K2[PtCl4], in ratio 1:1 and 1:2, gave the compounds [PtCl2DTS] and respectively. The reaction of the complexes K2[PdCl4], Pd(AcO) 2 and [PdCl2(PhCN)2], where PhCN = Benzonitrile, with tetraethylthiouram disulfide in ratio 1:1 or 1:2, yielded orange crystals identified as . The crystals were suitable for study by X‐ray diffraction. The ‐S‐S‐ bridge in the tetraethylthiouram disulfude molecule was broken and the two molecules of the thiocarbamate derivative were bound to the Pd(II) by the equivalents sulfur atoms. All the compounds were characterized by IR,  1H and  13C NMR spectroscopies.
Effect of Complexes of Zinc, Cobalt and Copper With D‐Aminosugars on the Replication of Herpes Simplex Virus Type 1 (HSV‐1)
Authors: Shishkov S. , Varadinova T. , Panteva M. , Bontchev P.
Published: March 2007

Our previous results show that Zn(pic) 2 and Zn(asp) 2 inhibit key steps of the replication of HSV‐1. Anti‐HSV effect of complexes of Co(II) with aminoacids Lys and Ser was also found. In the present study we describe the effect of complexes of Zn(II), Co(II) and Cu(II) with D‐aminosugars on the replication of HSV‐1 and on the infectivity of free virions. The experiments were done using primary rabbit kidney cells (r.k.), diploid human embryonal fibroblasts (F) and Vero cells. No differences in the toxicity of metal complexes on diploid cells‐ r.k. and F, were found. Neither metal complexes, nor ligands‐galactosoxime and glucosoxime, influenced the viral replication. During 1‐4h prolonged contact only Cu(Gl.NOH) 2 inactivated HSV‐1 virions up to 90%. The results show that D‐aminosugars are not suitable ligands for Zn(II), Cu(II) and Co(II) in respect of the inhibition of viral replication. However, only Cu(Gl.NOH) 2 was able to inhibit the infectivity of free virions.
Distribution of Rhodium in Mice Submitted to Treatment With the Adduct of Rhodium Propionate and Sodium Isonicotinate
Authors: de Souza Aparecido Ribeiro , Najjar Renato , de Oliveira Elizabeth , Zyngier Szulim Ber
Published: March 2007

The distribution of rhodium in Balb/c mice following intraperitoneal (ip) administration of a solution of adduct of rhodium propionate and sodium isonicotinate has been investigated. The metal concentration was determined in blood and in the following organ tissues: brain, heart, lung, liver, spleen, kidney, testes, and uterus/ovary, and the rhodium concentration was obtained by
Inductively Coupled Argon Atomic Emission Spectroscopy (ICP‐AES). The metal was detected in all organ tissues examined, mainly in spleen, liver, uterus/ovary and heart. Nine days after the injection, traces of rhodium were found in the liver and kidneys and, twenty days after the injection,
only in the liver.
Biological Role of Cobalt(II), Copper(II) and Nickel(II) Metal Ions on the Antibacterial Properties of Some Nicotinoyl‐Hydrazine Derived Compounds
Authors: Chohan Zahid H. , Sherazi Syed K. A.
Published: March 2007

Several cobalt(II), copper(II) and nickel(II) complexes of nicotinoylhydrazine‐derived compounds were prepared and characterised by physical, spectral and analytical data. These compounds and their complexes have proven to be antibacterial. The screening data show the metal complexes to be more potential/bactericidal than the uncomplexed compounds against one or more bacterial species.
Binuclear Rhodium(II) Complexes With Selective Antibacterial Activity
Authors: Bień Małgorzata , Lachowicz Tadeusz M. , Rybka Agnieszka , Pruchnik Florian P. , Trynda Lilianna
Published: March 2007

Binuclear rhodium(II) complexes [Rh2Cl2(μ‐OOCR)2(N‐N)2] {R = H, Me; N‐N = 2,2′‐bipyridine (bpy), 1,10‐phenanthroline (phen)} and (R = Me, Et;) have been synthesized and their structure and properties have been studied by electronic, IR and  1H NMR spectroscopy. Antibacterial activity of these complexes against Escherichia coli and Staphylococcus aureus has been investigated. The most active antibacterial agents against E. coli were [Rh2Cl2(μ‐OOCR)2(N‐N)2] and {R = H and Me} which were considerably more active than the appropriate nitrogen ligands. The complexes show low activity against S. aureus. The activity of the complexes against E. coli decreases in the series: R = H≅CH3 > C2H5 > C3H7≅C4H9. The reverse order was found in the case of S. aureus.
Antineoplastic and Cytotoxic Activities of Nickel(II) Complexes of Thiosemicarbazones
Authors: Hall Iris H. , Miller Merrill C. , West Douglas X.
Published: March 2007

Nickel(II) complexes of thiosemicarbazons were observed to be potent cytotoxic agents in human and rodent tissue cultured tumor cells. Each compound demonstrated a slightly different profile in the various histological types of tumors. The nickel complex of Appip demonstrated the most potent in vivo activity in the Ehrlich ascites carcinoma. This agent selectively inhibited L1210 DNA and purine syntheses, and DNA polymerase α, PRPP‐amido transferase, IMP‐dehydrogenase, dihydrofolate reductase, TMP‐kinase and thymidylate synthetase activities. L1210 DNA strand scission was evident and DNA viscosity was reduced after 24 hr incubation. The nickel complexes were not L1210 DNA topoisomerase II inhibitors.
Complexes With Biologically Active Ligands. Part 111. Synthesis andCarbonic Anhydrase Inhibitory Activity of Metal Complexes of4,5‐Disubstituted‐3‐Mercapto‐1,2,4‐Triazole Derivatives
Authors: Scozzafava Andrea , Cavazza Christine , Supuran Claudiu T. , Saramet Ioana , Briganti Fabrizio , Banciu Mircea D.
Published: March 2007

Complexes containing five 4,5‐disubstituted‐3‐mercapto‐1,2,4‐triazoles and Zn(II), Hg(II) and
Cu(I) were synthesized and characterized by standard procedures (elemental analysis; IR, electronic and
NMR spectroscopy, conductimetry and TG analysis). Both the thione as well as the thiolate forms of the
ligands were evidenced to interact with the metal ions in the prepared complexes. The original mercaptans
and their metal complexes behave as inhibitors of three carbonic anhydrase (CA) isozymes, CA I, II and IV,
but did not lower intraocular pressure in rabbits in animal models of glaucoma.
In Vivo Nitric Oxide Synthase Inhibitors Can Be Deprived of ThisActivity: Unexpected Influence of the Tetrachloroplatinate(II) Counteranion.Crystal Structures of Bis(S‐Methyl‐Isothiouronium)‐N,N′‐Bis(3‐Guanidinopropyl)Piperazinium and HexamidiniumTetrachloroplatinates(II) Salts
Authors: Morgant Georges , Viossat Bernard , Roch-Arveiller Monique , Prognon Patrice , Giroud Jean-Paul , Lancelot Jean-Charles , Robba Max , Huy Dung Nguyen
Published: March 2007

The synthesis and crystal structures of bis(S‐methylisothiouronium) (MSTUH)+, N,N′‐bis((3‐
guanidinopropyl)piperazinium (PipeC3GuaH4) 4+ and hexamidinium (HexaH2) 2+ tetrachloro platinate(ll) salts ( called hereafter PtMSTU, PtPipeC3Gua and PtHexa respectively ) were
investigated. These compounds contain the “amidine” function (‐ C(=NH)NH2 ) in which the H
atoms supplied by the acid have become attached to the imino group of each terminal amidino
function. Moreover, in PtPipeC3Gua, the nitrogen atoms of the chair‐piperazine moiety are also
protonated. The influence of tetrachloroplatinate(ll) counteranion ( versus sulfate, nitrate and
diisethionate ) in the in vivo nitrite inhibition by the (MSTUH)+, (PipeC3GuaH4) 4+ and (HexaH2) 2+
cations was investigated. The three tetrachloroplatinate(ll) salts, unexpectedly, do not inhibit
significantly the in vivo nitrite production in comparison with the other salts (sulfate, nitrate and
diisethionate and their corresponding previous countercations) which exhibit NO synthase
inhibition, especially bis(S‐methylisothiouronium) sulfate, a selective and potent inducible NO
synthase (iNOS) inhibitor commonly used as standard.
Synthesis and Radioprotective Activity of New Organosilicon andGermanium Compounds
Authors: Rima Ghassoub , Satgé Jacques , Dagiral Rodolphe , Lion Claude , Fatome Marc , Roman Vincent , Laval Jean-Denis
Published: March 2007

Silathiazolidine and metalladithioacetals (M = Si, Ge) have been prepared by the
interaction of dialkyldichloro‐ or bis(diethylamino)dialkylsilanes and ‐germanes with 3‐[N‐(2‐
thioethyl)]amino‐propanamide (WR‐2529) and [1‐thioethyl‐2‐(1‐naphtylmethyl)]‐2‐
imidazoline. The study of these compounds in the field of chemical radioprotection has
shown a notable decrease in the toxicity and a rather large increase in the radioprotective
activity of these new derivatives in comparison with the starting organic compounds.
Cytotoxicity of Poly(Phenolic)Sulfonates and Their Sodium Salts in L1210 Lymphoid Leukemia Cells
Authors: Wang Fei , Warren Amy E. , Barnes Cheryl R. , Hall Iris H.
Published: March 2007

Poly(phenolic)‐sulfonates demonstrated very good cytotoxicity against the growth of tumor cell lines
(L1210, Tmolt‐3, HeLa‐S3) and are comparable in potency with typical clinically used anticancer drugs.
Four of the most active compounds, i.e. GL‐2021, GL‐2029, GL‐2041 and GL‐2063, were selected for a
mode of action study in L1210 lymphoid leukemia cells at concentration of 25μM to 100μM for 60 min.
The agents did not alkylate bases of ct‐DNA, cause intercalation between base pairs, produce cross linking
of ct‐DNA strands or generate free radicals although L1210 DNA fragmentation was observed after 24 hr
incubation. L1210 DNA synthesis was preferentially inhibited which was achieved by (1) suppressing DNA
polymerase α activity which reduced the synthesis of new strands of DNA, (2) reducing of de novo purine
synthesis at the regulatory enzyme PRPP amido transferase which reduced d(GMP) levels, and (3)
inhibiting of nucleoside kinase activities which further reduced DNA synthesis. DNA template activity was
altered by the poly(phenolic)sulfonates since they reduced DNA polymerase α and m‐RNA and t‐RNA
polymerase activities. The kinetic studies at 50 μM over 2 hr demonstrated that the agents’ effect on
PRPP‐amido transferase activity is probably a major target of the compounds.
Pd(II) and Pt(II) Complexes of Schiff Thiobases Derived From2‐Carbonylpyridine
Authors: Gómez-Bosquet M. , Moreno V. , Font-Bardía M. , Solans X.
Published: March 2007

Pd(ll) and Pt(ll) complexes of three series of Schiff thiobases derived from 2‐ carbonylpyridine have been synthesized and characterized. The crystal structure of the Pt(ll)
derivative of methyl‐3‐(2‐pyridylmethylene)hydrazinecarbodithioate (HFp) was resolved. The ligand
coordinates the platinum ion in tridentate fashion by heterocycle and imine nitrogen and
thiocarbonyl sulfur. The fourth ligand is a chloride ion. The structure of the complexes is suitable for
the formation of monofunctional adducts with DNA. Studies on the interaction of the complexes
with Calf thymus DNA by CD reveal modifications in the B form of lineal DNA. Interaction with
plasmid DNA was also confirmed in the images obtained by atomic force microscopy.
Effect of Copper Acyclovir Complexes on Herpes Simplex Virus Type 1and Type 2 (HSV‐1, HSV‐2) Infection in Cultured Cells
Authors: Panteva M. , Varadinova T. , Turel I.
Published: March 2007

We have found that when copper, zinc or cobalt is bound to a suitable ligand, the
appropriate complex exhibited a significant anti‐HSV effect (Varadinova et al., 1993; 1996).
Recently published data by Sagripanti et al. (1997) also show that the inhibition of HSV by
copper was enhanced by reducing agents and that mechanism of the inactivation is similar
as for copper‐mediated DNA damage (Aruoma, et al. 1991; Dizdaroglu, et al., 1991;
Toyokuni and Sagripanti, 1994). Therefore it was interesting to study the efect of Cu(ll)
coordination compounds with acyclovir (ACV) on the replication of HSV in cultured cells.
The experiments on cytotoxicity as well as on the activity of three different Cu‐ACV
complexes = (A); = (B) and
= (C) towards virus replication, with special attention on the growth of
ACV‐resistant strain R‐100 were performed on MDBK cells. ACV was used as a reference
compound. The following results were obtained: 1) Increased cell’s viability in the presence
of 20‐40(g/ml ACV and decreased one in the presence of Cu‐ACV complexes with relative
level (A) >> (B) > (C); 2) Cu‐ACV complexes are more cytotoxic than the ligand ‐ ACV and the
relative level is (C)>(B)>(A); 3) The anti‐HSV effect of ACV can be modulated by copper at
levels depending on the specificity of the particular virus strain: (i) for the ACV sensitive strain
DA (HSV‐1) ‐ ACV ((A) > (C) > (B); (ii) for the ACV sensitive strain Bja (HSV‐2) (A) > ACV > (C) > (B); (iii) for strain R‐100 ( ACVR, TKa) ‐ (A) > ACV > (C) > (B). This findings are consistent with
previously published data and undoubtedly show that Cu‐ACV complexes could be useful in
the treatment of HSV infections, especially when the causative agent is a resistant to ACV
mutant.
Steric Determinants of Pt/DNA Interactions and Anticancer Activity
Authors: Hambley Trevor W. , Berners-Price Susan J. , Davies Murray S. , Diakos Connie I. , Er Hui Meng , Fenton Ronald R. , Ling Edwina C. H. , Rezler Evonne M.
Published: March 2007

Studies directed at establishing the structural features that control Pt/DNA interactions and
the anticancer activity of Pt drugs are described. [ 1H, 15N]‐HSQC 2D NMR spectroscopic
studies of the reactions of cisplatin with oligonucleotides containing ApG and GpA binding
sites reveal dramatic differences in the rates of formation of monofunctional adducts at the
two sites. When the reactant is cis no such differences are observed
suggesting that outer‐sphere interactions between the reactant and the oligonucleotide may
play a substantial role in determining the rates. Rates of closure to the bifunctional adducts
are similar to those observed for cisplatin. Studies of the adduct profiles formed by sterically
bulky and/or optically active complexes reveal that steric interactions play a major role in
mediating the binding of Pt(ll) to DNA but that hydrogen bonds play less of a role. In vitro cytotoxic activities for these complexes do not always follow the trends that would be
expected on the basis of the adduct profiles.
Antitumour Metallocenes: Effect of DMSO on the Stability of Cp2TiX2and Implications for Anticancer Activity
Authors: Mokdsi George , Harding Margaret M.
Published: March 2007

The rate of hydrolysis of the aromatic rings of Cp2TiX2 [X = CI 1, O2CCCl3  8 and
O2CCH2NH3Cl  13], in aqueous solutions, 10%DMSO and 100% DMSO have been studied by  1HNMR spectroscopy. Rapid hydrolysis of both the carboxylate and cyclopentadienyl ligands in
Cp2TiX2[X = O2CCCl3, O2CCH2NH3Cl] occurs in DMSO to give biologically inactive species. The
rate of these reactions are concentration dependent as dilution of these samples with saline or
water to give the therapeutic conditions of 10%DMSO/90%H2O slows the hydrolysis chemistry. In
contrast, samples of Cp2TiX2 [X = CI 1, O2CCH2NH3Cl  13], dissolved in water give solutions
containing the presumed antitumour active species in which the halide or glycine ligands have
been hydrolysed but the Cp rings remain metal bound.
Antitumor Activity of Gold(I), Silver(I) and Copper(I) ComplexesContaining Chiral Tertiary Phosphines
Authors: McKeage Mark J. , Papathanasiou Peter , Salem Geoffrey , Sjaarda Allan , Swiegers Gerhard F. , Waring Paul , Wild S. Bruce
Published: March 2007

The in vitro cytotoxicities of a number of gold(I), silver(I) and copper(I) complexes containing chiral
tertiary phosphine ligands have been examined against the mouse tumour cell lines P815
mastocytoma, B16 melanoma [gold(I) and silver(I) compounds] and P388 leukaemia [gold(I)
complexes only] with many of the complexes having IC50 values comparable to that of the
reference compounds cis‐diamminedichloroplatinum(ll), cisplatin, and bis[1,2‐bis(diphenylphosphino)
ethane]gold(I) iodide. The chiral tertiary phosphine ligands used in this study include
(R)‐(2‐aminophenyl)methylphenylphosphine; (R,R)‐, (S,S)‐ and (R*, R*)‐1,2‐phenylenebis(methylphenylphosphine);
and (R,R)‐, (S,S)‐ and (R*, R*)‐bis{(2‐diphenylphosphinoethyl)phenylphosphino}ethane. The in vitro cytotoxicities of gold(I) and silver(I) complexes containing the
optically active forms of the tetra(tertiary phosphine) have also been examined against the human
ovarian carcinoma cell lines 41M and CH1, and the cisplatin resistant 41McisR, CH1cisR and
SKOV‐3 tumour models. IC50 values in the range 0.01 ‐ 0.04 μM were determined for the most
active compounds, silver(I) complexes of the tetra(tertiary phosphine). Furthermore, the chirality of
the ligand appeared to have little effect on the overall activity of the complexes: similar IC50 data
were obtained for complexes of a particular metal ion with each of the stereoisomeric forms of a
specific ligand.
Synthesis, Vasodilating, Antithrombotic and Cardioprotective Activity of Pyridyl Substituted 5‐Silyl(Germyl)Isoxazolines‐2
Authors: Lukevics E. , Arsenyan P. , Veveris M.
Published: March 2007

The reactions of [2+3] cycloaddition of pyridylnitrile oxides to vinyl‐ and allylgermanes
proceed regioselectively and afford 5‐Ge‐substituted isoxazolines‐2. We have synthesized 9 new
pyridyl substituted 5‐Si(Ge)‐isoxazolines‐2 and investigated their biological activity. The
vasodilating, anticoagulant and cardioprotective activities of 5‐Si(Ge) substituted isoxazolines‐2
have been studied in vitro and in vivo. Substitution of the silicon atom for the germanium one
leads to the significant increase in vasodilating, antithrombotic and cardioprotective activity. The
insertion of the methylene group between Ge and the isoxazoline ring reduces the vasodilating
activity. The most active isoxazoline ‐ 3‐(5 ‵ ‐triethylgermyl‐3 ‵ ‐isoxazolinyl)pyridine hydrochloride
protects the heart from rhythm disturbances and lethality during ischaemia‐reperfusion.
In Vitro and In Vivo Behaviour of  111In Complexes of TTHA,TTHA‐Bis(Butylamide) and TTHA‐Bis(Glucamide): Stability,Biodistribution and Excretion Studied by Gamma Imaging
Authors: Prata M. I. M. , Ribeiro M. J. , Santos A. C. , Peters J. A. , Nepveu F. , Geraldes C. F. G. C. , de Lima J. J. P.
Published: March 2007

Aiming at radiopharmaceutical application,  111In3+ complexes of the
polyaminocarboxylates TTHA, TTHA‐bis(butylamide) and TTHA‐bis(glucamide) were
investigated. The in vitro stability of  111In(TTHA) 3− and  111In(TTHA‐bis(butylamide)- was
evaluated by measuring the exchange of  111In3+ from the complexes to transferrin and the
results were compared with those for  111In(DTPA) 2−. We also performed biodistribution studies of
the three  111In3+ complexes by gamma‐imaging in Wistar rats and by measuring the
radioactivity in their organs. TTHA and its derivatives seem to have similar in vivo biodistribution with prevailing renal excretion.
Synthesis, Characterization and Antitumour Activity of Di‐n‐Butyltin Salicyloxamate
Authors: Gielen Marcel , Dalil Hassan , de Vos Dick , Biesemans Monique , Willem Rudolph
Published: March 2007

The synthesis and characterization of di‐n‐butyltin and dimethyltin salicyloxamate, respectively compounds 1
and 2, are reported. Compound 1 is more active than cisplatin, 5‐fluorouracil and etoposide against seven
tumoural cell lines of human origin, but less active than methotrexate and doxorubucin.
Synthesis, Crystal Structure and Interaction With DNA of N,N′‐(Butane‐1,4‐Diyl)Bis(Guanidinium) Tetrachloroplatinate (II)
Authors: Bailly Christian , Viossat Bernard , Labouze Xavier , Morgant Georges , Saturnino Carmella , Lancelot Jean Charles , Robba Max , Dung Nguyen Huy
Published: March 2007

The design, synthesis, crystal structure and interaction with DNA of the N,N′‐(butane‐1,4‐diyl)bis(guanidinium)
tetrachloroplatinate(ll) are described. Crystal data: a = 8.152(1), b = 8.889(4),
c = 10.700(3) Å , α = 81.59(3), β = 87.99(5), γ = 78.48(6)°, V = 752(1) Å3, Z = 2 , space group P‐1.
The structure was refined to R = 0.039 and Rw = 0.046 from 1853 reflections (I > 3σ(I)). This
compound, named PtC4Gua, does not exhibit a center of symmetry and the center linker chain C(2)
‐ C(3) ‐ C(4) ‐ C(5) is in gauche conformation. The cation is bisprotonated with the H+ attached to the
imine group of each terminal guanidinium function. The presence of the platinum moiety reinforces
the binding of the butane(bis)guanidinium structure with double stranded DNA as judged from
thermal denaturation studies and DNA unwinding experiments.
Synthesis and Antifungal Activity of Metal Complexes ContainingDichloro‐Tetramorpholino‐Cyclophosphazatriene
Authors: Guran Cornelia , Barboiu Mihai , Diaconescu Paula , Iluc Vlad , Bojin Mihaela , Scozzafava Andrea , Supuran Claudiu T.
Published: March 2007

Metal complexes of dichloro‐tetramorpholino‐cyclophosphazatriene containing divalent cations
such as Ni(II), Co(II), and Mn(II) have been prepared and characterised by standard physico‐chemical
procedures (elemental chemical analysis, IR and UV‐VIS spectra, conductimetric measurement). The newly
synthesised compounds possessed antifungal activity against Aspergillus and Candida spp., some of them
showing effects comparable to ketoconazole (with minimum inhibitory concentrations in the range of 2‐ 30
μg/mL) but being generally less active as compared to the azole. Best activity was detected against C.
albicans, and worst activity against A. niger. The mechanism of action of these compounds probably
involves inhibition of ergosterol biosynthesis, and interaction with lanosterol‐14‐α‐demethylase (CYP51A1),
since reduced amounts of ergosterol were evidenced by means of HPLC in cultures of the sensitive strain A. niger treated with some of these inhibitors.
Preparation and Anti‐Tumour Activity of Some Arylbismuth(III) Oxine Complexes
Authors: Smith Katharine A. , Deacon Glen B. , Jackson W. Roy , Tiekink Edward R. T. , Rainone Silvina , Webster Lorraine K.
Published: March 2007

New arylbismuth(lll) oxinates, PhBi(MeOx) 2, (p‐MeC6H4)Bi(Ox) 2, (p‐MeC6H4)Bi(MeOx) 2,
(p‐ClC6H4)Bi(Ox) 2, and (p‐ClC6H4)Bi(MeOx) 2 (Ox− = quinolin‐8‐olate and MeOx− = 2‐methylquinolin‐8‐olate) have been prepared by reaction of the appropriate diarylbismuth chlorides
with Na(Ox) or Na(MeOx) in the presence of 15‐crown‐5. An X‐ray crystallographic study has shown
PhBi(MeOx) 2 to be a five coordinate monomer with distorted square pyramidal stereochemistry.
Chelating MeOx ligands have a cisoid arrangement in the square plane and the phenyl group is
apical. The lattice is stabilised by significant π‐π interactions between centrosymmetric molecules.
A range of these complexes has been shown to have high in vitro biological activity
(comparable with or better than cisplatin) against L1210 leukaemia, the corresponding cisplatin
resistant line, and a human ovarian cell line, SKOV‐3. However, initial in vivo testing against a solid
mouse plasmacytoma (PC6) and P388 leukaemia has not revealed significant activity.
Synthesis and Crystal Structure of Diaqua(1,10‐Phenanthroline‐N,N′)(Thiosulfato‐O,S)Manganese(II). Biological Properties.
Authors: Brezeanu Maria , Badea Mikaela , Morgant Georges , Viossat Bernard , Bouttier Sylvie , Fourniat Jacky , Marinescu Dana , Huy Dung Nguyen
Published: March 2007

The synthesis of diaqua(1,10‐phenanthroline‐N,N′)(thiosulfato‐O,S)manganese(ll)
was investigated. Its structure was determined by single crystal X‐ray
diffraction from 2418 reflections (I > 3 σ(I)) to a final value of R = 0.047 and Rw = 0.054. Crystal data
are as follows: space group P21 ; a = 10.356(3), b = 7.097(3), c = 20.316(2) Å, β = 94.29(2)°, V = 1489.1(8) , Å3, Z = 2. There are two independent title compounds in the asymetric unit. Each
manganese atom has a distorted octahedral Mn(SO)N2O2 geometry with the S and O atoms (from
two neighbouring thiosulfate ligands) mutually trans, two N atoms from the 1,10‐phenanthroline
ligand and two water oxygen. The thiosulfate group behaves as a bridging ligand, connecting,
through sulfur and oxygen, Mn atoms related by the binary b translation, thus forming infinite chains
running parallel to this axis. Infrared and electronic spectra are reported.
Structure‐Activity Relationships for Some Diamine, Triamine andSchiff Base Derivatives and Their Copper(II) Complexes
Authors: Bolos C. A. , Nikolov G. St. , Ekateriniadou L. , Kortsaris A. , Kyriakidis D. A.
Published: March 2007

Ethylenediamine (en), putrescine (pu), diethylenetriamine (dien), dipropylenetriamine (dpta),
spermidine (spmd) and their CuII compounds as well as the Schiff bases with 2‐furaldehyde (dienOO), 2‐
thiophenecarboxaldehyde (dienSS) and pyrrole‐2‐carboxaldehyde (dienNN) of dien and that of dpta with 2‐
thiophenecarboxaldehyde (dptaSS), were prepared and characterised. They were tested against Bacillus substilis, Bacillus cereus, Staphylococcus aureus, Escherichia coli, Proteus vulgaris and Xanthomonas campestris as antibacterial reagents, the highest activity being exhibited by Cu(dptaSS) complex,
which acts as antibiotic. In the antiproliferative tests (vs. T47D,L929 and BHK21/c13 cell lines) the best results
were obtained with Cu(dptaSS) 2+ and Cu(dienSS) 2+. Electronic structure calculations gave for dptaSS and
dienSS the higher negative charges on the N atoms. The counter‐ions (Br-, and ) play an important
role by modulating the reagent′s selectivity versus the bacteria [Gram(+) or Gram(‐)], but they have no effect
on the antiproliferative activity.
Synthesis, Ligational and Biological Properties of Cobalt(II),Copper(II), Nickel(II) and Zinc(II) Complexes WithPyrazinedicarboxaimide Derived Furanyl, Thienyl and Pyrrolyl Compounds
Authors: Chohan Zahid H. , Sherazi S. K. A. , Praveen M. , Iqbal M. S.
Published: March 2007

Preparation, ligational and biological properties of some pyrazinedicarboxaimide derived
furanyl, thienyl and pyrrolyl compounds with Co(ll), Cu(ll), Ni(ll) and Zn(ll) metals are
described. Magnetic moments, electronic, infrared, nuclear magnetic resonance spectra and
elemental analysis data indicate that co‐ordination of the ligands with the metal ions take
place through the pyrazine ring nitrogen, azomethine nitrogen and heteroatom of
heterocyclic ring system. The compounds are all novel and are proposed to possess an
octahedral geometry for Co(ll) and Ni(ll), and a distorted octahedral geometry for Cu(ll) and
Zn(ll) complexes. The comparative biological properties of the title ligands and their metal
chelates against different bacterial species are also described.
Calcium Modulation of Toxicities Due to Cisplatin
Authors: Aggarwal Surinder K.
Published: March 2007

Cisplatin (CDDP) is a potent anti‐neoplastic agent with associated toxicities, especially
gastrointestinal and nephrotoxicity that are its dose‐limiting factors in clinical oncology. In an
attempt to elucidate its mechanism(s) of action, liver and kidney tissues from normal and CDDP
treated (1.8 mg/kg) dogs were evaluated for changes in various dehydrogenases [MDH, SDH, β‐HBDH,
IDH and G‐6‐PDH] and nonspecific lipase enzymes. CDDP treatment induced an inhibition
of all the enzymes studied except G‐6‐PDH and nonspecific lipases, where there was a significant
increase. Supplemental pretreatments with calcium 2.50 mg (150,000 USP units) ergocalciferol
plus 1000 mg of elemental calcium as Tums 500 (EffeCal; calcium carbonate)/day seemed to
retain enzyme levels close to normal with no apparent toxic side effects observed after CDDP.
Calcium supplements post‐CDDP treatment did not have any protective effect.
Toxicity Profiles In Vivo in Mice and Antitumour Activity inTumour‐Bearing Mice of Di‐ and Triorganotin Compounds
Authors: Gielen M. , Willem R. , Dalil H. , de Vos D. , Kuiper C. M. , Peters G. J.
Published: March 2007

The in vivo toxicity profiles in mice and the antitumour activity in tumour bearing mice were screened
for four di‐n‐butyltin and five triorganotin carboxylates, di‐n‐butyltin diterebate (5),
bis(phenylacetate) (6), bis(deoxycholate) (7), bis(lithocholate) (8), tri‐n‐butyltin terebate (9), cinnamate (10), and triphenyltin terebate (11).

At their maximum tolerated dosis (MTD), no antitumour effect (T/C ~1) was observed for the
compounds 5, 7, 9, 10 and 11. The compounds 6 (T/C = 0.51) and 8 (T/C = 0.42) showed clear
antitumour activity after single dose administration and might therefore be of interest for further
antitumour activity studies.
Platinum (II) Compounds With Antitumor Activity Studied by Molecular Mechanics
Authors: Trendafilova Natasha , Georgieva Ivelina , Nikolov George St.
Published: March 2007

A series of Pt(ll) complexes with antitumor properties: [1,2‐bis(2,6‐dichloro‐4‐hydroxyphenyl)ethylenediamine]PtL2 (meso‐1‐PtL2) and [erythro‐1‐(2,6‐dichloro‐4‐hydroxyphenyl)‐2‐(2‐halo‐4‐hydroxyphenyl)ethylenediamine]PtL2, ; halo = F (erythro‐8‐PtL2),
halo = Cl (erythro‐9‐PtL2)] has been modelled by molecular mechanics (MM). The MM calculations
were carried out for different isomers and ligand conformations meso‐δ, meso‐λ, d,l‐δ, d,I‐λ. The compounds with the lowest MM energies have the same geometries as those obtained by X‐ray
analysis. The calculated MMX energy orders: meso‐1‐PtL2 < erythro‐9‐PtL2 < erythro‐8‐PtL2 for L = I−, Cl− and are reverse to the known antitumor activity order ‐ the lowest energy complex
(the most stable one)is the one with the highest estrogen activity (meso‐1‐PtL2). The type of the
leaving group (L) does not alter the energy order, which is in agreement with the biological
experiments that show a slight dependence of the estrogen properties on the leaving group type.
NMR Investigation of the Copper(II)‐Ciprofloxacin System
Authors: Turel Iztok , Košmrlj Janez , Andersen Bjørn , Sletten Einar
Published: March 2007

A proton NMR study was performed on the copper(ll)‐ciprofloxacin system. The proton
relaxation times (T1)
were determined from the titration data in acidic and basic media. In
acidic medium the H5 signal is dramatically affected and it is assumed that copper is bonded
to the quinolone through carbonyl and one of the carboxyl oxygens. Such bonding is in
agreement with the X‐ray literature data for the complex [Cu(cf)2]Cl2.6H2O
isolated from the
slightly acidic solution. There are additional significant changes in T1 of H3′
and H5′
atoms
which suggest that the terminal nitrogen atom of the piperazine ring system‐N4′
also interacts
with copper in the basic conditions. Thus it is plausible that more than one species are
present in the solution at high pH values.
Radiorecovery Activity of Dicopper(II) Tetrakis(3,5‐Diisopropylsalicylate) Includes Recovery of Radiation‐Induced Loss ofBody Mass and Impaired Mouse Locomotion
Authors: Henderson Renada D. , Henderson Timothy D. , Irving Henry J. , Sorenson John R. J.
Published: March 2007

Dicopper(II) tetrakis(3,5‐diisopropylsalicylate), [Cu(II)2(3,5‐DIPS)4], is effective in increasing survival of lethally irradiated mice when it is administered after irradiation. The possibility that this radiorecovery activity might also facilitate recovery from radiation‐induced impaired increase in body mass and locomotion was examined. Cu(II)2(3,5‐DIPS)4
was used to treat LD50/30
gamma irradiated female C57BL/6 mice after irradiation. A dose of 0, 5, 10, or 20 μmol Cu(II) 2  (3, 5‐DIPS) 4
/kilogram of body mass was administered subcutaneously 3 hrs after LD50/30
irradiation and change in body mass and locomotor activity measured daily throughout the 30 day post‐irradiation period. Treatment with 5, 10, or 20 μmolCu(II)2(3,5‐DIPS)4
/kg of body mass increased survival, which was statistically significant for the 10 μmol
/kg of body mass‐treated group compared to the vehicle‐treated group (P<0.05)
, significantly (P<0.05)
increased recovery of locomotion from days 13 to 15 post‐irradiation onward for all treated groups compared to vehicle‐treated mice, and increased recovery of body mass gain from day 14 onward for the 20 μmol
/kg of body mass‐treated group (P<0.001)
and day 21, although not statistically significant, for the 10 μmol
/kg of body mass‐treated group. There were no statistically significant differences between the increase in survival, recovered increase in body mass, and recovered increase in locomotion for mice treated with 10 μmol
or 20 μmolCu(II)2(3,5‐DIPS)4
/kg on day 30 post‐irradiation. It is concluded that Cu(II)2(3,5‐DIPS)4
in addition to increasing survival of irradiated mice increases the rate of recovery of radiation‐induced decrease in body mass and locomotion.
The Hypolipidemic Activity of Heterocyclic Thiosemicarbazones,Thioureas and Their Metal Complexes in Sprague Dawley Male Rats
Authors: Hall Iris H. , Chen S. Y. , Barnes Betsy Jo , West Douglas X.
Published: March 2007

Heterocyclic thiosemicarbazones, thioureas and their copper, nickel, and cobalt complexes were shown to
be potent hypolipidemic agents in male Sprague Dawley rats at 8 mg/kg/day, orally. These agents lowered
the activity of rat hepatic rate limiting enzymes for the synthesis of cholesterol and triglycerides. The effects
of these agnets on cytoplasmic ATP‐dependent citrate lyase, acetyl CoA synthetase and HMG‐CoA
reductase activities were reduced by a magnitude to explain the reduction of serum cholesterol levels
afforded by the compounds. The reduction of acetyl CoA carboxylase, sn‐glycerol‐3‐phosphate synthetase and phosphotidylate phosphohydrolase activities caused by the derivatives is of sufficient magnitude to
explain the observed reduction in serum triglycerides after administration of the agents.
Ferrocene‐Derived Pyrazinoyl and Nicotinoyl Schiff‐Bases: TheirSynthesis, Characterization and Biological Properties
Authors: Chohan Zahid H. , Praveen M.
Published: March 2007

A novel class of acetylferrocene‐derived Schiff‐bases such as 2‐pyrazinoyl‐1‐(2‐ferroceneylmethylene)‐
hydrazide (HL1)
and 2‐nicotinoyl‐1‐(2‐ferrocenylmethylene)hydrazide (HL2)
have been synthesized and
characterized by their IR,  1H
NMR,  13C
NMR and microanalytical date. The biological effect induced due to the coupling of ferrocene molecule with the aroylhydrazines e.g., pyrazinoylhydrazine and nicotinoylhydrazine has been studied against bacterial species such as Escherichia coli, Pseudomonas aeruginosa , Staphylococcus aureus and Klebsiella pneumonae.
Kupffer Cells and Peritoneal Macrophage Activation After PlatinumCoordination Complexes
Authors: Aggarwal Surinder K. , Muenchen H. J. , Telgenhoff D. J.
Published: March 2007

Action of poly‐[(trans‐l,2‐diaminocyclohexane)platinum]‐carboxyamylose (poly‐plat) and
cisplatin (CDDP) on the immune system was studied using isolated peritoneal macrophages and
compared with liver resident macrophages from normal, CDDP and poly‐plat [10 mg/kg] treated
Swiss Webster mice for 2‐12 days. Peritoneal macrophages were treated [10 mg/L] for 2 h and
allowed to grow in normal medium at 37°C (5% CO2) for 24 h. Similarly macrophages from Swiss
Webster mice treated with CDDP and poly‐plat were isolated and cultured on normal medium.
Supernatants from cells in culture were collected at 0.5, 1, 2, and 24 h post‐treatment for various
cytolytic factors. CDDP and poly‐plat treatments induce an activation of the peritoneal
macrophages and the Kupffer cells through cell growth, development of cytoplasmic extensions,
enhanced number of lysosomes and the activity of various cytolytic factors. Poly‐plat treatment of
the macrophages induces a 500 fold increase in the number of lysosomes, compared to CDDP
treatment where there was only a 50 fold increase.
Antioxidant and Prooxidant Effects of Metal Dafonates on theNADPH‐Dependent Lipid Peroxidation in the Murine HepaticMicrosomal System
Authors: Gupta M. , Kale R. K. , Kulkarni P. P. , Padhye S. B.
Published: March 2007

Dafone inhibits the lipid peroxidation significantly in a concentration dependent manner. The
inhibition was found to be an uncompetitive type with the inhibition constant (Ki) of 62.5 μM
On the other
hand complexation with metal ions results in a significant reversal from antioxidant to pro‐oxidant properties
for the resulting complexes which are cationic and with associated halometallate anions. The nature of the
potentiation in case of the ferric compound was of competitive type with activation constant (Ka) having the
value 32.5 μM
. The neutral copper‐dafonate complex, however, inhibits lipid peroxidation with increase in
concentration.