• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1996년도 춘계학술대회
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• pp.241-241
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• 1996

새로운 항암성 백금(II)착제 SA: ([Pt( trans-1-dach) (DPPE)]ㆍ2NO$_3$, SB: [Pt (cis-dach)(DPPP)]ㆍ2NO$_3$, SC: [Pt(cis-dach)(DPPE)]ㆍ2NO$_3$에 대한 일반 약리작용이 rat, mouse 및 rabbit에서 검토되었다. Rota-rod test에 의한 운동 협조능, thiopental-Na의 수면 작용, 현수에 의한 근이완 작용, 정상체온, strychnine 유발 경련, 담즙분비, 수정관, 자궁각, 피부혈관 투과성, 국소마취, 용혈 및 심전도에 대하여 SA, SB. SC는 별다른 영향을 미치지 않았단. 적출회장과 십이지장에 대하여 SA는 수축반응을 나타내었으나 SB와 SC는 하등의 영향이 없었으며 혈액 응고에 대하여 SA는 prothrombine time을 단축시켰으나 SB, SC는 별다른 영향이 없었고 호흡에 대해서는 SA, SB, SC 다같이 호흡수를 억제하였다. 적출심장 기능에 대하여 SA, SB, SC 다같이 고농도에서 억제적으로 작용하였다.

• Biomolecules & Therapeutics
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• 제6권3호
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• pp.303-311
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• 1998

The general pharmacological properties of new platinum (II) coordination complexes, SA : [Pt(trans-ι-DACH)(DPPE)] . 2NO$_3$, SB : [Pt(cia-DACH)(DPPP)] 2NO$_3$ and SC : [Pt(cia-DACH)(DPPE)] 2NO$_3$on central nervous, respiratory, cardiovascular and digestive systems were studied in various experimental animals. These platinum (II) anticancer agents had no effects on analgesia, thiopental-induced sleeping time, body temperature, strychnine-induced convulsion, inflammation and local anesthetic action in mice and rats. Intestinal motility, stomach-ulcer induced by serotonin and bile-secretion of rats were not influenced by the dose of 30 mg/kg. However SB and SC induced a mild decrease in heart rate in anesthetized rats. Based on these results, these new platinum (II) complexes may be regarded as a valuable lead compound in the development of new anticancer chemotherapeutic agents with marked antitumor activity and low toxicity.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1995년도 춘계학술대회
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• pp.119-119
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• 1995

This study was performed to evaluate the general toxicity of novel Pt(II) complexes, (KHPC-002: [Pt(trans-1-dach) (DPPE)].2NO$_3$, KHPC-005: [Pt(cis-dach)(DPPE)].2NO$_3$ and KHPC-006: [Pt(cis-dach)(DPPP)]. 2NO$_3$). In the acute toxicity study in rats, three dosing groups of Sprague-Dawley male rats in each compounds were given a single intraperitoneal injection of KHPC-002, KHPC-005 and KHPC-006. In order to compare the toxic effects of these novel Pt(II) complexes with those of cisplatin, one group Sprague-Dawley male rats were given 7mg/kg i.p injection of cisplatin. Body weights showed dose-related decrease in all treatment groups when compared wi th the control group.

• Macromolecular Research
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• 제13권4호
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• pp.334-338
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• 2005

A three-layered poly(benzyl ether) dendrimer having a bis-ethynylbenzene core was synthesized and characterized with $^{1}H$ NMR and MALDI-TOF-MS spectroscopy. The dendrimer was reacted with platinum complexes to obtain platinum-acetylide based organometallic polymers. When the dendrimer was reacted with trans-[$PtCl_{2}(PEt_{3})_{2}$], a high molecular weight polymeric compound was formed, whereas, with cis-[$PtCl_{2}dppp$], a uniform molecular weight compound was formed, which was found to be a dimeric metallacycle by $^{1}H\;NMR,\;^{31}P\;NMR$ and ESI-TOF-MS spectroscopy. Both these complexes exhibited relatively a strong emission around 440 nm, indicating that they could be potential candidates for blue emitting polymer LEDs.

• Journal of Pharmaceutical Investigation
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• 제20권4호
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• pp.217-222
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• 1990

New antitumor-active pt(II) complexes of trans-l-diamine cyclohexane containing diphosphines as a leaving group were synthesized. The structures of the pt(II) complexes were determined by analyzing the infrared and $^{31}P-nuclear$ magnetic resonance spectra. Antitumor activities of the pt(II) complexes were tested against murine leukemia $L_{l210}$ according to the protocol of the National Cancer Institute. All the pt(II) complexes Synthesized were antitumor-active. In particular, water-soluble $[pt(trans-l-dach) (DPPP)](NO_3)_2$ exhibited excellent antitumor activity, giving T/C % values of 341 and 356 respectively, each with four cured mice out of six at a dose of 25 mg/kg. These pt(II) complexes are considered to be worthy of further development.

• Bulletin of the Korean Chemical Society
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• 제16권3호
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• pp.211-214
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• 1995

The catalytic activities of palladium(0,Ⅰ,Ⅱ)-diphosphine complexes were investigated in styrene oxidation using H2O2 as terminal oxidant. The rates showed a dependence on the chelate ring patterns of complexes (PdCl2L); 5-membered ring (L=dppe: 1,2-bis(diphenylphosphino)ethane) < 6-membered ring (L=dppp: 1,3-bis(diphenylphosphino)propane) < 4-membered ring (L= dppm: bis(diphenylphosphino)methane). This sequence correlates with the ligand field strength and interactions between metal and phosphine ligands. Pd(Ⅱ,Ⅰ)-diphosphine complexes which are capable of making 4-membered chelate ring showed an enhancement of catalytic activities for styrene oxidation. The catalytic activities of Pd(0,Ⅰ,Ⅱ)-diphosphine complexes are described in terms of electronic and steric factors.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1995년도 춘계학술대회
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• pp.120-120
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• 1995

This study was conducted to examine novel Pt(II) complexes, (KHPC-002; [Pt(trans-1-dach) (DPPE)]. 2NO$_3$, KHPC-005;[Pt(cis-1-dach)(DPPP)]. 2NO$_3$ and KHPC-006; [Pt(cis-1-dach) (DPPE)]. 2NO$_3$) for their acute toxicities and toxicological profiles in preclinical studies. In male and female mice given a single intraperitoneal administration of KHPC-002, KHPC-005 and LHPC-006, we determined that LD$\_$50/ values of pt(II) complexes were 295.5mg/kg(M), 350.4mg/kg(F);KHPC-002, 158.7mg/kg(M), 157.7mg/kg(F); KHPC-005, 574.8mg/kg(M), 596.5 mg/kg (F); KHPC-006, respectively. In gross and histopathological examination on dead animals, no abnormal changes were observed in any organs.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1995년도 춘계학술대회
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• pp.121-121
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• 1995

This study was conducted to examine novel Pt(II) complexes, (KHPC-002: [Pt(trans-1-dach) (DPPE)]. 2N0$_3$, KHPC-005: [Pt(cis-dach) (DPPE)] 2NO$_3$ and KHPC-006: [Pt(cis-dach) (DPPP)]. 2NO$_3$) for their acute toxicities. In male and female mice given a single intraperitoneal administration of KHPC-002, KHPC-005 and KHPC-006, we determined that LD$\_$50/ values of Pt(II) complexes were 295.5mg/kg(M), 350.4mg/kg(F) : KHPC-002, 596.5mg/kg(M), 674,8mg/kg(F): KHPC-005, 158.7mg/kg(M), 157.7mg/kg(F); KHPC-006, respectively. The signs of toxicity in mice observed fellowing the administration of these compounds included the followings: decreased mortor activity: abnormal gait: salviation, trasient decreased body weight. There were no treatment related specific changes in growth examination.

• 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.

• 생명과학회지
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• 제21권9호
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• pp.1214-1218
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• 2011

식물자원으로부터 항산화 물질을 확보 하기위해 한국 등에서 전통적으로 phytotherapy로 이용되어 온 Rubus crataegifolius Bge. 열매를 조사하였다. R. crataegifolius의 열매를 메탄올로 추출하였고 순차적으로 n-hexane, diethyl ether, and ethyl acetate로 분획화하였다. 각 분획물의 항산화 활성은 DPPH와 $H_2O_2$에 대항 인간 primary 세포인 keratinocyte (HK)를 이용하여 세포 독성 및 효능을 검증하였다. R. crataegifolius 열매 추출물은 비타민 C와 비슷한 강력한 DPPH (75.04%, 50%)와 $H_2O_2$ (79.9%, 54.1%) 소거능을 보였다. 분획물의 DPPP에 대한 소거능을 측정하였는데 n-hexane fraction (HF)은 20.3%, diethyl ether fraction (DF)은 68.8%, ethyl acetate fraction (EF)는 67.1% 그리고 residue fraction (RE)은 67.1%의 소거능을 보였으며 $H_2O_2$에 대해서는 2.2%, 1.6%, 10%, 그리고 50%로 각각 나타내었다. H2O2에 대한 HK의 세포 보호능을 확인하기 위해 산화적 스트레스 모델을 확립하였고(1 mM) 0.005-0.02%의 RE 분획물에서 $H_2O_2$에 대한 보호능을 발휘하였다. 따라서, R. crataegifolius의 열매 추출물은 $H_2O_2$유발 상처에 대하여 HK세포의 보호능을 가지며 강력한 항산화 활성을 가지고 있다.