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Organic gold complexes have different biological activity, depending on their potential for interactions with key functional molecules.The aim of this study was to investigate potential of several newly synthesized organic gold complexes to influence spontaneous motility of the Fallopian tubes.The effects of [Au(bipy)Cl(2)](+) (dichloride(2,2'-bipy...
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... for 5 h at room temperature and the obtained yellow solution was left in the darkness to evaporate. After few days formed dark yellow crystals were filtrated, washed with cold water and dried. Found: H, 1.87; C, 7.21; S, 7.18. Calc. for AuC 4 S 2 O 2 H 12 Cl 3 : H, 1.84; C, 7.32; S, 7.76 %. Structures of the investigated com- plexes are shown in Fig. ...
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Citations
... With their intrinsic, highly potent tumor anti proliferative potential, gold (III) complexes have recently attained an important role. Their mechanism of action is different from cisplatin [6], but they are electronically and structurally homogenous to platinum (II) compounds [7]. The actual breakthrough for the use of gold compounds will come when these compounds are designed to be more clinically effective and potent, with enhanced cancer cell specificity and selectivity along with diminished organ toxicity [1]. ...
Bipyridine gold (III) dithiocarbamate compounds are Gold-III complexes with promising cytotoxic properties. In this study, the subacute toxicity of a Gold (III) complex with dithiocarbamate ligand was evaluated. In the acute toxicity component, an initial LD50 (38.46 mg/kg) was calculated by the administration of 50, 100, 200, 400, and 800 mg/kg of the compound to five groups of rats, respectively (n = 4 each). The sixth group was the control. The sub-acute toxicity component comprised the control group A (n = 6) and the study groups B (n = 10) and C (n = 4), which were administered 1 mL distilled water, 1/10 LD50 (3.8 mg/kg), and 1/5 LD50 (7.6 mg/kg), respectively, daily for 6 weeks. The alive animals were then sacrificed. Autopsy; preservation of renal, hepatic and cardiac tissue in buffered formalin; histopathological processing; microscopic evaluation; and comparison with the controls were sequentially conducted. In the subacute toxicity study at dosages of 3.8 mg/kg and 7.6 mg/kg, the renal tubules remained unaffected with no necrosis or vacuolization. Mild to moderate renal interstitial, hepatic capsular, lobular and portal inflammation along with mild focal hepatic vacuolization were present. At 3.8 mg/kg, the cardiac muscle fibers were unremarkable in 80% (n = 8) of the specimens, with mild focal hyalinization in 20% (n = 2) of the specimens. The same was observed in 50% (n = 2) of the specimens at 7.6 mg/kg. Variable congestion was evident in all of the groups. In the subacute toxicity study, the absence of renal tubular necrosis or vacuolization, the presence of mild inflammatory hepatic and renal alterations, and predominantly unremarkable cardiac muscle fibers suggest that Bipyridine gold (III)-dithiocarbamate is safe in animal studies and is a potential candidate for clinical trials.
... The structural and electronic profiles of gold (III) compounds bear similarity to platinum (II) compounds (4). Gold (III) being isoelectronic and isostructural to platinum became the potential candidate for investigations and research as a new anticancerous compound. ...
Objective(s)
Newer organo-metallic, specifically gold (III) complexes with multiple ligands are currently being formulated with primary focus of having increased anti-cancerous properties and decreased cytotoxicity. In this study, histological toxicity profile of a newly formulated anti-cancerous gold (III) compound [trans-(±)-1,2-(DACH)2Au]Cl3 Bis(trans-1,2-Diaminocyclohexane) was investigated by evaluation of kidney and liver tissues of rats treated by the compound.
Materials and Methods
This is a quasi-experimental study. In acute toxicity component of the study, (n = 16) male rats weighing between 200–250 g were administered single, variable concentration of the gold (III) compound, [trans-(±)-1,2-(DACH)2Au]Cl3 Bis(trans-1,2-Diaminocyclohexane) to determine LD50 (dose that is lethal to 50% of rats). An IP injection of 2.3 mg/kg (equivalent to 1/10 of LD50) was injected for 14 consecutive days to (n=10) male rats in the sub-acute component of the study. Autopsy preservation of liver and kidney tissue in buffered formalin, sample processing, histopathological evaluation, and comparison with unremarkable controls (n=5) was conducted sequentially.
Results
A dose of 2.3 mg/kg did not produce any tubular necrosis in kidney specimens. Mild interstitial inflammation with prominence of plasma cells was the main histological alteration. Plasmacytic pyelitis was also seen. Varying extents of cytoplasmic vacuolization and mild focal lobular and portal inflammation were predominant hepatic microscopic findings.
Conclusion
[trans-(±)-1,2-(DACH)2Au]Cl3 Bis(trans-1,2-Diaminocyclohexane) produced no histological damage in renal and hepatic tissues of rats. This very limited sample animal-based study points to the relative safety of this new gold compound. However, there is a need to compare this compound with established drugs in a comparative non-animal based study.
... Gold complexes have recently gained significant attention as a class of compounds with different pharmacodynamic and kinetic properties than cisplatin with strong cell growth inhibiting effects [53,54]. The cell growth inhibiting effects, in many cases, could be related to anti-mitochondrial effects that make the gold complexes interesting [53,55,56]. However, the NPs can be incorporated with dual targets, the androgen receptor (AR1) which is a target for prostatic cancer therapy and a G protein receptor (GRC6A), which is seen upregulated in cancer prostate. ...
The application of nanotechnology in various fields of science has earned a great concern over the past decades. The natural
products and surface-modified polymers and metallic nanoparticles (NPs) have evolved as promising nanomaterials for targeted
prostate cancer treatment. In the present study, Chitosan/poly (vinyl alcohol) (Cs/PVA) blend was synthesized by gamma radiation
which could behave a nanoreactor for silver (Ag) and gold (Au) nanoparticle with promising anticancer applications. (Cs/PVA/Ag) and
(Cs/PVA/Au) nanocomposites were confirmed by SEM (scanning electron microscope) and TEM (transmission electron microscope)
analysis. The swelling properties have been investigated as a function of time and pH. The anti-cancer activity of the prepared
nanocomposites was demonstrated in prostatic cancer cell line. It has a significant effect against prostatic cancer. However, metal
nanoparticles have shown a good experimental success in the field of nanomedicine especially in cancer treatment, which has always
been an area of high concern. The collaboration of biomedical research in the identification and characterization of biomedical
strategies using the interesting metal nanocomposite will impact the future nanomedicine greatly.
Key words: Chitosan, nanocomposite, silver nanoparticles, gold nanoparticles, prostatic model.
... Gold complexes have recently gained significant attention as a class of compounds with different pharmacodynamic and kinetic properties than cisplatin with strong cell growth inhibiting effects [53,54]. The cell growth inhibiting effects, in many cases, could be related to anti-mitochondrial effects that make the gold complexes interesting [53,55,56]. However, the NPs can be incorporated with dual targets, the androgen receptor (AR1) which is a target for prostatic cancer therapy and a G protein receptor (GRC6A), which is seen upregulated in cancer prostate. ...
... The development of new metallodrugs with a pharmacological activity different from platinum drugs is one of the major goals of modern bioinorganic and bio-organometallic medicinal chemistry research (Janković et al. 2012;Arsenijević et al. 2013;Kouroulis et al. 2009;Altaf et al. 2014;Hartinger and Dyson 2009). Among these non-platinum anticancer drugs, gold complexes have recently gained significant attention as a class of compounds with different pharmacodynamic and kinetic properties than cisplatin with strong cell growth inhibiting effects (Kouroulis et al. 2009;Altaf et al. 2014). ...
... Among these non-platinum anticancer drugs, gold complexes have recently gained significant attention as a class of compounds with different pharmacodynamic and kinetic properties than cisplatin with strong cell growth inhibiting effects (Kouroulis et al. 2009;Altaf et al. 2014). The cell growth inhibiting effects, in many cases, could be related to anti-mitochondrial effects that make the gold complexes interesting (Janković et al. 2012;Arsenijević et al. 2013;Kouroulis et al. 2009). ...
A new series of mononuclear [t-Bu3PAuS2CN(C7H7)2] (1), and binuclear [(DPPM)Au2(S2CN(CH3)2)2] (2), [(DPPM)Au2(S2CN(C2H5)2)2] (3) and [(DPPM)Au2(S2CN(C7H7)2)2] (4) [where DPPM = 1,1-bis(diphenylphosphino)methane, S2CN(CH3)2=dimethyldithiocarbamate, S2CN(C2H5)2= diethyldithiocarbamate and S2CN(C7H7)2 = dibenzyldithiocarbamate] gold(I) complexes have been prepared by reacting gold(I) precursors and dialkyl/diaryl dithiocarbamate ligands. The complexes were characterized by analytical technique and spectroscopic methods such as CHNS analysis, FTIR spectroscopy; 1H, 13C and 31P NMR measurements. The molecular structure of [t-Bu3PAuS2CN(C7H7)2] (1) complex was determined by X-ray diffraction. The gold(I) complexes (2 and 3) were found particularly better potent in vitro cytotoxic agents in comparison to cisplatin against HeLa, HCT15 and A549 cancer cell lines. These metal complexes could serve as attractive anticancer agents for the developments of novel therapeutic strategies and to treat cervix, lung and colon cancers.
The gold(III) complexes of the type [(DACH)Au(en)]Cl3, 1,2-Diaminocyclohexane ethylenediamine gold(III) chloride [where 1,2-DACH = cis-, trans-1,2- and S,S-1,2diaminocyclohexane and en = ethylenediamine] have been synthesized and characterized using various analytical and spectroscopic techniques including elemental analysis, UV-Vis and FTIR spectra; and solution as well as solid-state NMR measurements. The solid-state (13)C NMR shows that 1,2-diaminocyclohexane (1,2-DACH) and ethylenediamine (en) are strongly bound to the gold(III) center via N donor atoms. The stability of the mixed diamine ligand gold(III) was determined by (1)H and (13)C NMR spectra. Their electrochemical behavior was studied by cyclic voltammetry. The structural details and relative stabilities of the four possible isomers of the complexes were also reported at the B3LYP/LANL2DZ level of theory. The coordination sphere of these complexes around gold(III) center adopts distorted square planar geometry. The computational study also demonstrates that trans- conformations is slightly more stable than the cis-conformations. The antiproliferative effects and cytotoxic properties of the mixed diamine ligand gold(III) complexes were evaluated in vitro on human gastric SGC7901 and prostate PC3 cancer cells using MTT assay. The antiproliferative study of the gold(III) complexes on PC3 and SGC7901 cells indicate that complex 1 is the most effective antiproliferative agent among mixed ligand based gold(III) complexes 1-3. The IC50 data reveal that the in vitro cytotoxicity of complexes 1 and 3 against SGC7901 cancer cells are fairly better than that of cisplatin.
New gold (III) compounds with chemical formulae [Au{cis-(1,2-DACH)}2]Cl3 1, [Au{trans-(±)-(1,2-DACH)}2]Cl3 2 and [Au{(S,S)-(+)-1,2-(DACH)}2]Cl3 3 (where 1,2-DACH = 1,2-Diaminocyclohexane) have been synthesized. The synthesized compounds were characterized using elemental analysis, various spectroscopic techniques including UV-Vis, FTIR spectroscopy, solution and solid-state NMR measurements; and X-ray crystallography. The stability of compounds 1, 2 and 3 was checked by UV-Vis spectroscopy and NMR measurements. The electrochemical behavior was also investigated through cyclic voltammetry. The potential of the three compounds as anticancer agents was investigated by measuring in vitro cytotoxicity in terms of IC50 and inhibitory effect on growth of human prostate (PC3) and gastric (SGC7901) cancer cell lines. [Au{(trans-(±)-(1,2-DACH)}2]Cl3 (2) showed better in vitro inhibitory effect on growth of human prostate (PC3) and gastric (SGC7901) cancer cell lines than [Au{(cis-(1,2-DACH)}2]Cl3 (1) and [Au{(S,S)-(+)-(1,2-DACH)}2]Cl3 (3).
