• Polymer(Korea)
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• v.33 no.3
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• pp.213-218
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• 2009

A cationic lipid emulsion containing 1,2-dioleoyl-3-trimethylammonium-propane(DOTAP), Tween80, squalene has been prepared as a gene delivery system. In order to increase the transfection efficiency of gene carrier, folate was used as the tumor-targeting ligand that was attached on PEG-DPPE. HeLa and 293 cells were used for the in vitro transfection experiment. HeLa cell is a folate-positive cell line. The mean particle sizes of polymeric lipid system and DNA/lipid complex system were 206.6 nm and 150.5 nm, respectively. The transfection efficiencies of our carriers(4:l(w:w) complex ratio)were 100 times higher than that of DOTAP only emulsion due to the targeting effect of folate.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1995.04a
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• pp.73-73
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• 1995

We investigated the effect of derivatized phospholipid, P-pyridoxyl dipalmiuylphosphatidylethanolamine (P-pyr-DPPE), on the catalytic activity of purified porcine brain glutamate decarboxylase(GAD) which catalyzes the synthesis of GABA known as major inhibitory neurotransmitter in CNS. When the P-pyr-DPPE was incorporated into dipalmitdylphosphatidylcholine(DPPC) or phosphatidylserine(PS) vesicles, these vesicles enhanced the catalytic activity of GAD. P-pyr-DPPE also interacted with apoglutamate decarboxylase(apoGAD) and produced the free pyridoxal-5-phosphate(PLP) which is the natural cofactor of GAD. This result indicated that apoGAD catalyzed the cleavage reaction of the P-pyridoxyl moiety of the derivatized phopholipid to generate free PLP, and then free PLP bound to the apoGAD resulting in restroration of the catalytic activity of the enzyme.

• 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.

• Journal of the Korean Chemical Society
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• v.36 no.2
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• pp.248-254
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• 1992

Bis(phosphine)ruthenium derivatives $({\eta}^5-C_5Me_5)RuCl(PR_3)_2(PR_3=PMe_3,\; PMe_2Ph,\;PEt_3,\;PMePh_2$, 1/2DPPE, 1/2DPPB) (2a${\sim}$2f) have been synthesized by the reaction of $[({\eta}^5-C_5Me_5)RuCl_2]_2$ (1) with excessive phosphine in ethanol. The reaction of complexes $({\eta}^5-C_5Me_5)Ru(PR_3)_2Cl\;with\;NaBH_4$ in ethanol gave the corresponding hydride complexes $({\eta}^5-C_5Me_5)Ru(PR_3)_2H (PR_3=PMe_3, PEt_3, PMePh_2$, 1/2 DPPE, 1/2DPPB) (3a${\sim}$3e). Chloride complexes (2a${\sim}$2f) and hydride complexes (3a${\sim}$3e) were isolated as crystals, which were characterized by IR, $^1H-NMR$ , and elemental analysis.

• Macromolecular Research
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• v.15 no.6
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• pp.547-552
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• 2007

Water soluble polymer, poly(vinyl pyrrolidone) was chosen to conjugate with 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine-N-(succinyl) (N-succinyl DPPE) to make a new drug delivery system. PVP with an amine group (amino-PVP) was polymerized by free radical polymerization. The amine group of amino-PVP was conjugated with the carboxylic group of N-succinyl DPPE. The resultant conjugate could form nanoparticles in the aqueous solution; these nanoparticles were termed a lipid-polymer system. The critical aggregation concentration was measured with pyrene to give a value of $1{\times}10^{-3}g/L$. The particle size of the lipid-polymer system, as measured by DLS, AFM and TEM, was about 70 nm. Lipophilic component in the inner part of the lipid-polymer system could derive the physical interaction with hydrophobic drugs. Griseofulvin was used as a model drug in this study. The loading efficiency and release profile of the drug were measured by HPLC. The loading efficiency was about 54%. The release behavior was sustained for a prolonged time of 12 days. The proposed lipid-polymer system with biodegradable and biocompatible properties has promising potential as a passive-targeting drug delivery carrier because of its small particle size.

• The Korean Journal of Pharmacology
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• v.31 no.1 s.57
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• pp.103-114
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• 1995

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 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 analogue containing 1,2-diaminocyclohexane (dach) as carrier ligand and 1,2-bis(diphenylphosphino) ethane (DPPE) as a leaving group. Furthermore, nitrate was added to improve the solubility. A new series of [Pt(trans-ddach)(DPPE).$2NO_3(PC)$ was synthesized and characterized by their elemental analysis and by various spectroscopic techniques [infrared (IR), $^{13}carbon$ nuclear magnetic resonance (NMR)]. PC demonstrated acceptable antitumor activity aganist P388, L-1210 lymphocytic leukemia cells and SK=OV3 human ovarian adenocarcinoma cells, and significant. activity as compared with that. cisplatin. The toxicity of PC was found quite less than thar 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.

• Bulletin of the Korean Chemical Society
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• v.17 no.2
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• pp.125-127
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• 1996

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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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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• v.6 no.3
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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.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1995.04a
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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.