• Title/Summary/Keyword: Pt(II) complex

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Investigation of effects of newly synthesized Pt(II) complex against human serum albumin and leukemia cell line of K562

  • Divsalar, Adeleh;Saboury, Ali A.;Ahadi, Leila;Zemanatiyar, Elham;Mansouri-Torshizi, Hassan
    • BMB Reports
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    • v.43 no.11
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    • pp.766-771
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    • 2010
  • The biological evaluation of a new synthesized Pt(II)-complex, 2,2'-bipyridin Butylglycinato Pt(II) nitrate, an anti-tumor component, was studied at different temperatures by fluorescence and far UV circular dichroism (CD) spectroscopic methods. Human serum albumin (HSA) and human tumor cell line K562 were as targets. The Pt(II)-complex has a strong ability to quench the intrinsic fluorescence of HSA. Binding and thermodynamic parameters of the interaction were calculated by fluorescence quenching method. Far-UV-CD results showed that Pt(II)-complex induced increasing in content of $\alpha$ helical structure of the protein and stabilized it. The 50% cytotoxic concentration ($Cc_{50}$) of complex was determined using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay at different incubation times. Also, fluorescence staining with DAPI (4,6-diamidino-2-phenylindole) revealed some typical nuclear changes, which are characteristic of apoptosis. Above results suggest that Pt (II) complex is a promising anti-proliferative agent and should execute its biological effects by inducing apoptosis.

A New Class of Platinum (II) Complexes [Pt (trans-1-daeh) (DPPP)] $2NO_3$ and [Pt (trans-1-daeh)(DPPE)] $2NO_3$ Exhibiting Antitumor Activity and Nephrotoxieity (새로운 Platinum (II) Complex ([Pt (II)(trans-1-dach)(DPPP)] $(NO_3)_2$와 [Pt (II)(trans-1-dach)(DPPE)] $(NO_3)_2$의 항암효과 및 신독성에 관한연구)

  • Jung, Jee-Chang;Yoon, Chin-Hee;Chang, Sung-Goo;Lee, Kyung-Tae;Rho, Young-Soo
    • The Korean Journal of Pharmacology
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    • v.29 no.2
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    • pp.283-295
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    • 1993
  • Pt-complexes is currently one of the most compounds used in the treatment of solid tumors. However, its used is limited by severe side effects such as renal toxicity. Our platinum-based drug discovery program is aimed at developing drugs capable of diminishing toxicity and improving antitumor activity. We synthesized new Pt (II) complex analogues containing 1, 2-diaminocyclohexane (dach) as carrier ligand and 1, 3-bis (diphenylphosphino) propane (DPPP)/1,2-bis (diphenylphosphino) ethane (DPPE) as a leaving group. Furthermore, nitrate was added to improve the solubility. A new series of (KHPC-001) [Pt (trans-1-dach)(DPPP)] $2NO_3$ and (KHPC-002) [Pt (trans-1-dach)(DPPE)] $2NO_3$ were synthesized and characterized by their elemental analysis and by various spectroscopic techniques [infrared (IR), $^{13}carbon$ nuclear magnetic resonance (NMR)]. KHPC-001 and KHPC-002 demonstrated acceptable antitumor activity aganist P-388, L-1210 lymphocytic leukemia cells and significant activity as compared with that of cisplatin. The toxicity of KHPC-001 and KHPC-002 was found quite less than that of cisplatin using MTT, $[^3H]$ thymidine uptake and glucose consumption tests in rabbit proximal tubule cells and human kidney cortical cells.

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Synthesis of Platinum(II) Complex of Diethanolamine Dithiocarbamate and Rescue of cis-[$Pt(NH_{3})_{2}Cl_{2}$] Nephrotoxicity in Rats (디에탄올아민 디티오카바메이트의 백급(II)착물 합성 및 쥐의 cis-[$Pt(NH_{3})_{2}Cl_{2}$]에 의한 신장독성 회복)

  • 우상철;김창수
    • Journal of Environmental Health Sciences
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    • v.24 no.3
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    • pp.26-34
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    • 1998
  • Diethanolamine Dithiocarbamate containing OH groups which gave water-soluble [Pt(dtc)$_{2}$] (diethanolamine dithiocarbamate) were synthesized from the reaction of CS$_{2}$ with diethanolamine. The complex has been characterized by elemental analysis, electrical conductivity, and spectroscopic results. Diethanolamine dithiocarbamate is effective as rescue and inhibition of cis-[$Pt(NH_{3})_{2}Cl_{2}$] nephrotoxicity in rats. It is suggested that diethanolamine dithiocarbamare removes platinum(II) complex coordinated to -SH groups of protein of kidney tubule cells.

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In Vitro Antitumor Activity and Nephrotoxicity of the Novel Platinum(II) Coordination Complex Containing Cis-dach/Diphosphine (새로운 Platinum(II)Complex ([Pt(II)(cis-dach)(DPPP)].$(NO_3)_2$의 항암효과 및 신독성)

  • Jung, Jee-Chang;Yim, Sung-Vin;Park, Seung-Joon;Chung, Joo-Ho;Ko, Kye-Chang;Chang, Sung-Goo;Rho, Young-Soo
    • The Korean Journal of Pharmacology
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    • v.32 no.1
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    • pp.93-102
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    • 1996
  • Platinum coordination complexes are currently one of the most compounds used in the treatment of solid tumors. However, its use is limited by severe side effects such as nephrotoxicity. Our platinum-based drug discovery program is aimed at developing drugs capable of diminishing toxicity and broadening the clinical spectrum of activity of cisplatin. We synthesized new Pt(II) complex analogue containing 1,2-diaminocyclohexane (dach) as carrier ligand and 1,3-bis(diphenyl phosphino)propane (DPPP) as a leaving group. Furthermore, nitrate was added to improve the solubility. A new series of PC-1 [Pt(cis-dach) (DPPP)]. $2NO_3_2$ was synthesized and characterized by their elemental analysis and by various spectroscopic techniques [infrared (IR), $^{13}carbon$ nuclear magnetic resonance (NMR)]. PC-1 was demonstrated acceptable antitumor activity aganist SKOV -3, OVCAR-3 human ovarian adenocarcinomacells and significant activity as compared with that of cisplatin. The toxicity of PC-1 was found quite less than that of cisplatin using MTT, $[^3H]thymidine$ uptake and glucose consumption tests in rabbit proximal tubule cells, human kidney cortical cells and human renal cortical tissues. Based on these results, this novel platinum compound represent a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low toxicity.

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Synthesis of Pt(II) Complexes containing Flavin mononucleotide as Leaving Ligand and their Anticancer Activity (Flavin mononucleotide를 탈리기로한 백금 (II) 착체의 합성과 그 항암활성)

  • 권영이;황규자
    • YAKHAK HOEJI
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    • v.43 no.6
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    • pp.762-770
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    • 1999
  • A series of vitamin-containing Pt(II) complexes of the type [Pt (FMN) (L)] (FMN=flavin mononucleotide, L=ethylenediamine, 1,3-propanediamine, 1,4-bu-tanediamine) was synthesizd and characterized by IR, electronic absorption, elemental analysis and FAB=Mass. The coordination sites of FMN to Pt(II) ions were determined to be N(5) and O(6) with resultant chelate ring formation. Theses compounds have much better water solubility (30-35 mg/ml) than cisplatin (1 mg/ml). The anticancer activity of this vitamin-containing Pt(II) series was investigated by MTT assay against mouse and human leukemia cell lines in vitro. Among these compounds, FMN (1,4-butanediamine) Pt(II) having seven-membered ring structure as amine ligand showed moderate anticancer activity.

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Flow cytometry of cell-cycle on Flavin mononucleotide (1,4-butanediamine) Pt(II) Complex and Cisplatin and Their Biochemical Analysis of Nephrotoxicity in ICR Mice (Flavin mononucleotide (1,4-butanediamine) Pt(II) Complex와 Cisplatin의 세포주기에 대한 유세포 분석 및 ICR계 생쥐에서의 신장독성에 대한 생화학적 분석)

  • 권영이;황규자;김안근;김국환;김원규;안동춘
    • YAKHAK HOEJI
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    • v.44 no.2
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    • pp.149-154
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    • 2000
  • Flavin mononucleotide (1,4-butanediamine) Pt(II) complex (7FMN) was synthesized and screened anticancer activity [J. Pharm. Soc. Korea 43(6),762-770 (1999)]. 7FMN have good water solubility and moderate anticancer activiy In this paper cell-cycle specificity and nephrotoxicity were studied. Interaction of DNA with cisplatin and synthesized 7FMN was analyzed by flow cytometry and showed G2 arrest in L1210 cell line. It means that cell-cycle on L1210 was inhibit in S phase by cisplatin and 7FMN. In order to biochemically analyze nephrotoxicity of cisplatin and 7FMN, after injecting each agent intraperitoneally, blood was exsanguinated after 6 hours, 1 day, 3 days and 7 days, respectively. Then, serum was separated from the blood. The serum level of BUN, creatinine and uric acid in cisplatin and 7FMN administated mice (25~35 g, ICR strain, a dose each 8,12 and 16 times of the $IC_{50}$/ value, cisplatin; 7 times) were determined by autochemistry analyzer. In cisplatinadministered mice group, BUN level was elevated than normal control group at 3rd day and repaired at 7th day. In 7FMN administrated group was not elevated. Creatinine and uric acid level were no difference with the normal control group. Therefore synthesized 7FMN is less toxic than cisplatin in nephrotoxiciaty.

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Synthesis of a Platinum-Pincer Complex and Application to Catalytic Silylcyanation (백금 핀서 화합물의 합성 및 Silylcyanation 촉매반응에 대한 응용)

  • Kim, Yun Tae;Yoon, Myeong Sik
    • Applied Chemistry for Engineering
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    • v.27 no.4
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    • pp.366-370
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    • 2016
  • A platinum(II) pincer complex composed of two six-membered fused metallacycles was directly synthesized using 1,3-bis(2-pyridyloxy)benzene and $K_2PtCl_4$. The structure of the complex was elucidated via NMR and X-ray crystallography analysis. The stable complex was formed due to the six-membered fused cycle structure around the Pt(II) center which reduced the bond angle strain. The complex was applied to the silylcyanation reaction of aldehydes and imines and showed an efficient catalytic activity with 99% yield.