• 제목/요약/키워드: Lead(II) complex

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In Vitro Cytotoxicity of a Novel Platinum(II) Coordination Complex Containing Diaminocyclohexane and Dichloropropane

  • Rho, Young-Soo;Chang, Sung-Goo;Lee, Woo-Tae;Jung, Jee-Chang
    • The Korean Journal of Physiology and Pharmacology
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    • 제5권4호
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    • pp.359-366
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    • 2001
  • We have synthesized a novel platinum(II) coordination complex containing cis-1,2-diaminocyclohexane (DACH) as a carrier ligand and 1,3-dichloropropane (DCP) as a leaving group. A new series of [Pt(cis- DACH)(DCP)](PC) was evaluated for its cytotoxic activity on MKN-45 human gastric adenocarcinoma cells and normal primary cultured kidney cells. The new platinum complex has demonstrated high efficacy in the cytotoxicity against MKN-45/P, MKN-45/ADM and MKN-45/CDDP cell-lines. The cytotoxicity of PC against rabbit proximal renal tubular cells, human renal cortical cells and human renal cortical tissues, determined by MTT assay, the $[^3H]-thymidine$ uptake and glucose consumption tests, was found to be quite less than those of cisplatin. Based on these results, this novel platinum(II) coordination complex appears to be better for improving antitumor activities with low nephrotoxicity and is a valuable lead in the development of new, clinically available anticancer chemotherapeutic agents.

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In Vitro Cytotoxicity of a Novel Platinum(II) Coordination Complex Containing Diaminocyclohexane

  • Jung, Jee-Chang;Kim, Soon-Ae;Kim, Young-Kyu;Chang, Sung-Goo;Rho, Young-Soo
    • Biomolecules & Therapeutics
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    • 제8권3호
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    • pp.228-234
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    • 2000
  • We have synthesized a novel platinum(II) coordination complex containing trans-ι-1,2-diaminocy-clohexane (DACH) as a carrier ligand and 1,2-dichloroethane (DCE) as a leaving group. A new series of [Pt(trans-ι-DACH)(DCE)](PC) was evaluated for its cytotoxic activity on MKN-45 human gastric adenocar-cinoma cells and normal primary cultured kidney cells. The new platinum complex has demonstrated high efficacy in the cytotoxicity against MKN-45/P, MKN-45/ADM and MKN-45/CDDP cell-lines. The cytotoxicity of PC against rabbit proximal renal tubular cells, human renal cortical cells and human renal cortical tissues, determined by MTT assay, the [$^3H$]-thymidine uptake arid glucose consumption tests, was found to be quite less than those of cisplatin. Based on these results, this novel platinum(II) coordination complex appears to be better for improving antitumor activities with low nephrotoxicity and is a valuable lead in the development of new, clinically available anticancer chemotherapeutic agents.

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Cis-Diaminocyclohexan을 배위자로 하는 배금(II)착체의 선택적 세포독성 (Selective Cytotoxicity Platinum (II) Complex Containing Carrier Ligand of cis-1,2-Diaminocyclohexane)

  • 노영수;정세영;정지창
    • Environmental Analysis Health and Toxicology
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    • 제13권3_4호
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    • pp.87-94
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    • 1998
  • The use of cisplatin is limited by severe side effects such as renal toxicity. Our platinum-base drug discovery is aimed at developing drugs capable of diminishing toxicity and improving antitumor activity. We synthesized new Pt (II) complex analogue [Pt (cis-DACH)(DPPP)]. 2NO$_3$ (PC) containing cis-1,2-diaminocyclohexane as a carrier ligand and 1,3-bis(diphenylphosphino) propane as a leaving group. Furthermore, nitrate was added to improved the solubility. In this study, its structure was determined and its antitumor activity against SKOV-3 and NIH-OVCAR-3 human ovarian adenocarcinoma, and in vitro cytotoxicity was determined against primary cultured rabbit kidney proximal tubular and renal cortical cells of human kidney using colorimetric MTT assay. PC demonstrated acceptable antitumor activity against SKOV-3 and NIH-OVCAR-3 human ovarian adenocarcinoma and significant activity as compared with that of cisplatin. The toxicity of PC was found quite less than that of cisplatin using MTT and $^3$H-thymidine uptake tests in rabbit proximal tubular cells and human kidney cortical cells. PC was used for human cortical tissue in 7 weeks hitoculture by the glucose-consumption tests. We determined that the new platinum drug has lower nephrotoxicity than cisplatin. Based on these results, this novel platinum (II) complex compound (PC) represent a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low nephrotoxicity.

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DL-2 하이드록시 3-메틸 부틸산물 배위자로 한 새로운 항암성 백금(II) 착체의 위암세포와 정상신장세포에 대한 선택적 세포독성 (Selective Cytotoxicity of Novel Platinum(II) Coordination Complexes Containing DL-2-Hydroxy 3-Methylbutyric Acid)

  • 정지창;홍언표;최승기;장성구;육창수;노영수
    • Biomolecules & Therapeutics
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    • 제11권2호
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    • pp.91-98
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    • 2003
  • A new series of highly water soluble platinum(II) complexes[Pt(II)(DL-2-hydroxy-3-methylbutyrate)(trans-l-1,2-dimninocyc1ohexane)] (PC-1) and [Pt(II)DL-2-hydroxy-3-methylbutyrate](cis-1,2-diaminocyclohexane)](PC-2) were synthesized and characterized by their elemental analysis and by various spectroscopic techniques [infrared(IR), $^{13}C$-nuclear magnetic resonance (NMR)]. In vitro antitumor activity of new Pt(II)complexes was tested against MKN-45, MKN/ADM and MKN/CDDP human gastric adenocarcinoma cell lines using colorimetric MTT[3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyltetrazoliumbromide] assay for cell survival and proliferation. PC-1 and PC-2 showed active against MKN-45/P, MKN/ADM and MKN/CDDP human gastric cancer cell lines, and the antitumor activity of these compounds were comparable or superior to that of cisplatin. The nephrotoxicities of PC-1 and PC-2 were found quite less then that of cisplatin using MTT and [$^3H$] thymidine uptake tests in rabbit proximal tubule cells, human kidney cortical cells human renal cortical tissues. Based on these results, these novel platinum(II) complex compounds(PC-1 & PC-2) represent a valuable lead in the development of the new anticancer chemotherapeutic agents capable of improving antitumor activity and low nephrotoxicity.

Selective Cytotoxicity of a Novel Platinum(II) Coordination Complex on Human Bladder Cancer Cell Lines and Normal Kidney Cells

  • Jung, Jee-Chang;Chung, Joo-Ho;Chang, Sung-Goo;Rho, Young-Soo
    • The Korean Journal of Physiology and Pharmacology
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    • 제4권2호
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    • pp.159-167
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    • 2000
  • We have synthesized a novel platinum(II) coordination complex containing cis-1,2-diaminocyclohexane (DACH) as a carrier ligand and 1,2-dichloroethane (DCE) as a leaving group. In addition, nitrate was added to improve the water-solubility. A new series of [Pt(cis-DACH)(DCE)] $2NO_3(PC)$ was evaluated for its cytotoxic activity on T-24 and J-82 human bladder carcinoma cells and normal primary cultured kidney cells. PC has demonstrated high levels of cytotoxicity against T-24 and J-82 cells. The cytotoxicity of PC against rabbit proximal renal tubular cells, human renal cortical cells and human renal cortical tissues, determined using the MTT assaying technique, the $[^3H]-thymidine$ uptake and glucose consumption tests, was found to be quite less than those of cisplatin. Based on these results, this novel platinum(II) coordination complex appears to be better for improving antitumor activities with low nephrotoxicity and is a valuable lead in the development of new clinically available anticancer chemotherapeutic agents.

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

  • 정지창;임성빈;박승준;정주호;고계창;장성구;노영수
    • 대한약리학회지
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    • 제32권1호
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    • pp.93-102
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    • 1996
  • 일부 malignant tumor에 Pt-complex의 임상 응용 과정에서 신장독성등의 심한 부작용이 문제점으로 지적되고 있다. 이 연구에서는 기존의 cisplatin보다 항암효과는 우수하면서, 부작용을 감소시킨 새로운 Pt complex의 개발에 역점을 두었다. 본 연구에서 합성한 Pt(II) complex는 carrier ligand로서 1,2-diaminocyclohexane(dach)을 사용하였고, leaving group으로는 diphosphine류인 1,3-bis (diphenylphosphine의 propane(DPPP) 을 도입하였으며, 물에 대한 용해도를 높이기 위해 dinitrate로 만들었다. 새로이 합성한 [Pt(II)(cia-dach)(DPPP)].$(NO_3)_2$ 은 원소 분석, IR 및 $^{13}C-NMR$ 분석 data에 의하여 위의 물질임이 확인되었다. PC-1은 MTT assay method에 의한 항암활성 연구를 통하여 SKOV-3, OVCAR-3 human ovarian adenocarcinoma cells에서 항암효과가 인정되었으며, 이 항암효과는 대조 약물로 사용된 cisplatin과 유사하였다. PC-1은 토끼의 신세뇨관 세포와 인체의 신피질 세포를 이용한 cytotoxity 및 thymidine 섭취율과 인체 신피질 조직 배양을 이용한 glucose consumption 실험을 통하여 모두 cisplatin보다 신장독성이 현저히 감소되었다. 이상의 결과로 보아 Pt(II) complex는 carrier ligand와 leaving group의 선택에 따라 항암활성의 증가와 신독성의 감소를 일으키는 요인으로 보여지며, 이 연구에서 만들어진 새로운 Pt(II) complex는 앞으로 다각적인 검토를 거쳐 새로운 anticancer chemotherapeutic agent로 개발될 가능성이 있을 것으로 생각된다.

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Selective Cytotoxicity of Novel Platinum(II) Coordination Complexes on Human Bladder Cancer Cell-Lines and Normal Kidney Cells

  • Kim, Jung-Tae;Rho, Young-Soo;Jung, Jee-Chang
    • The Korean Journal of Physiology and Pharmacology
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    • 제7권2호
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    • pp.111-117
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    • 2003
  • Cisplatin is often effective in cancer treatment, but its clinical use is limited because of its nephrotoxicity. We have synthesized new platinum(II) coordination complexes (PC-1 & PC-2) containing trans-${\iota}$ and cis-1,2-diaminocyclohexane (DACH) as carrier ligands and L-3 -phenyllactic acid (PLA) as a leaving group with the aim of reducing nephrotoxicity but maintaining its anticancer activity. In this study, new platinum(II) complex compounds were evaluated for selective cytotoxicity on cancer cell-lines and normal kidney cells. The new platinum complexes have demonstrated high efficacy in the cytotoxicity against human bladder carcinoma cell-lines (T-24/HT-1376). The cytotoxicity of these compounds against rabbit proximal renal tubular cells and human renal cortical tissues, was determined by MTT assay, the [3H]-thymidine uptake and glucose consumption test, and found to be quite less than those of cisplatin. Based on our results, these novel platinum compounds appear to be valuable lead compounds with high efficacy and low nephrotoxicity.

Anodic Stripping Differential Pulse Voltammetric Determination of Trace Amounts of Lead after Preconcentration of Its Complex with 2-(5-Bromo-2-pyridylazo)-5-diethylaminophenol onto Natural Analcime Zeolite by Column Method

  • Taher, Mohammad Ali;Mostafavi, Ali;Afzali, Darush;Rezaeipour, Ebrahim
    • Bulletin of the Korean Chemical Society
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    • 제25권8호
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    • pp.1125-1129
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    • 2004
  • This work assesses the potential of natural Analcime Zeolite as an adsorbent for preconcentration of lead (II) traces. Lead is quantitatively retained on 2-(5-bromo-2-pyridylazo)-5-diethylaminophenol by column method with Analcime in the pH range of 5-6.5 and 2 mL $min^{?1}$ flow rate. Lead was removed from the column with 10.0 mL of 4 M hydrochloric acid and was determined by anodic stripping differential pulse voltammetry. 0.5ppb detection limit was obtained and linear dynamic range was 3 to $1.2{\times}10^5$ ppb in final solution with correlation coefficient of 0.999 and relative standard deviation of ${\pm}$ 1.2% (for eight replicate determination of 2.5 ${\mu}g\;mL^{?1}$ of lead). Various parameters such as the effect of pH, flow rate, instrumental conditions and interferences of some ions on the determination of lead have been studied in detail for optimization of conditions. The method was successfully applied for determination of lead in various samples.

정상적인 한국 흑염소의 심전도에 관한 연구 1. 표전지유도와 단극지유도 (Studies on- Electrocardiogram of the Normal Korean Native Goat 1. Standard Limb Leads and Unipolar Limb Leads)

  • 최인혁;김선기;김추철;최인방;김남수
    • 한국임상수의학회지
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    • 제14권2호
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    • pp.319-337
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    • 1997
  • The electrocardiographic (ECG) parameters in the normal Korean black goat have been measured with a 3-channel Electrocardiograph and computed, analyzed. ECG in 243 black goats were made with the limb leads (I, II, III, aVR, aVL, aVF), that were recorded conduction parameters of wave and interval, and were analyzed as to shape and amplitude of the P and T waves and the components of the QRS complex. Heart rate were recorded by the ECG which were a mean of 106.1$\pm $21.8 beats/min. Average conduction times in the PR, the QRS complex and the QTc interval were recorded 103.9$\pm $34.9 msec., 58.3$\pm $23.2 msec. and 302.6$\pm $67.8 msec., in the P and T wave duration recorded 24.8$\pm $6.4 msec. and 51.7$\pm $10.8 msec. respectively. The shape of wave in each leads were observed various types, and any spacial wave type appeared the highest frequency in each lead that ware shown less than 60%, and these frequent rate and average amplitudes as fallow: 1. In P waver the frequent rate and average amplitudes of the positive type showed in leads I, II and aVL that were 54.8% (93.0$\pm $ 33.2 $\mu $V), 50.5% (90.1$\pm $30.5 $\mu $V) and 41.7% (58.5$\pm $ 31.1 $\mu $V). Average amplitude of the negative type showed the frequent rate of 49.8% in lead aVE which was -77.6$\pm$ 25.2 $\mu $V. Biphasic type in leads III and aVF were 46.1% (108.4 $\mu $V, -90.2 $\mu $V.) and 45.7% (137.4 $\mu $V, -105.4 $\mu $V.), and amplitudes between positive and negative of it were significant difference. 2. The highest amplitudes of the QRS complex in all leads were 534.8$\pm $ 232.3 $\mu $V of lead II. The frequent rate and amplitudes of the R wave type in the I, II, III and aVF were 30.2% (277.8 $\pm $131.3 $\mu $V), 45.1% (393.1$\pm $114.2 $\mu $V), 48.5% (349.3$\pm $178.3 $\mu $V) and 54.9% (334.4$\pm $129.7 $\mu $V), and QS ways type in the lead aVL was 49.5% (359.2$\pm $195.5$\mu $V), and RS and QS wave types in the lead a VR were 43.3% (312.4 $\mu $V, -212.7 $\mu $V.) and 41.1% (399.2$\pm $92.2 $\mu $V), respectively. 3. In T wave, the frequent rata and amplitudes of the positive type in the leads I, II, III and aVF were 44.6% (207.9$\pm $ 97.1 $\mu $V), 41.6% (245.1$\pm $92.1 $\mu $V), 46.9% (189.8$\pm $ 82.7 $\mu $V) and 53.0% (195.4197.8 $\mu $V), and the negative in the lead aVR was 41.2% (-230.7$\pm$ 103.1 $\mu $V), respectively. The positive and negative types in the lead aVe appeared with same frequent rate of 43.2%.4. Frontal plane vectors for P, QRS, and T were found to lie at 38.1$\pm $ 21.5, 142.0$\pm $ 57.2, and 117.2$\pm $ 63.9 degrees, respectively. These results in ECG of goats may be served to the limited purposes as to conduction parameters, arrhythmias except abnormal ECG because of waveforms, amplitudes and electrical axis of it were variability.

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Selective Cytotoxicity of a Novel Platinum (II) Coordination Complex on Human Gastric Cancer Cell Lines and Normal Kidney Cells

  • Jung, Jee-Chang;Kim, Young-Kyu;Yim, Sung-Vin;Park, Seung-Joon;Chung, Joo-Ho;Chang, Sung-Goo;Lee, Kyung-Tae;Rho, Young-Soo
    • The Korean Journal of Physiology and Pharmacology
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    • 제3권3호
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    • pp.283-291
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    • 1999
  • We have synthesized novel platinum (II) coordination complex containing cis-1,2-diaminocyclohexane (DACH) as a carrier ligand and 1,2-bis(diphenylphosphino)ethane (DPPE) as leaving group. Furthermore, nitrate was added to improve the water-solubility. A new series of [Pt(cis-DACH)(DPPE)] $2NO_3(PC)$ was evaluated its antitumor activity on various MKN-45 human gastric adenocarcinoma cell-lines and normal primary cultured kidney cells. The new platinum complex demonstrated high efficacy in the cytotoxicity on MKN-45 cell-lines as well as adriamycin-resistant (MKN-45/ADR) and cisplatin-resistant (MKN-45/CDDP) cells. The cytotoxicities of PC were found quite less than those of cisplatin in rabbit proximal renal tubular cells, human renal cortical cells and human renal cortical tissues using MTT assay, $[^3H]-thymidine$ uptake and glucose consumption tests. Based on these results, this novel platinum (II) coordination complex, was considered as better a valuable lead for improving antitumor activities with low nephrotoxicities in the development of a new clinically available anticancer chemotherapeutic agents.

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