• Molecules and Cells
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• v.27 no.3
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• pp.291-297
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• 2009

Apolipoprotein (apo) C-III is a marker protein of triacylglycerol (TG)-rich lipoproteins and high-density lipoproteins (HDL), and has been proposed as a risk factor of coronary heart disease. To compare the physiologic role of reconstituted HDL (rHDL) with or without apoC-III, we synthesized rHDL with molar ratios of apoA-I:apoC-III of 1:0, 1:0.5, 1:1, and 1:2. Increasing the apoC-III content in rHDL produced smaller rHDL particles with a lower number of apoA-I molecules. Furthermore, increasing the molar ratio of apoC-III in rHDL enhanced the surfactant-like properties and the ability to lyse dimyristoyl phosphatidylcholine. Furthermore, rHDL containing apoC-III was found to be more resistant to particle rearrangement in the presence of low-density lipoprotein (LDL) than rHDL that contained apoA-I alone. In addition, the lecithin:cholesterol acyltransferase (LCAT) activation ability was reduced as the apoC-III content of the rHDL increased; however, the CE transfer ability was not decreased by the increase of apoC-III. Finally, rHDL containing apoC-III aggravated the production of MDA in cell culture media, which led to increased cellular uptake of LDL. Thus, the addition of apoC-III to rHDL induced changes in the structural and functional properties of the rHDL, especially in particle size and rearrangement and LCAT activation. These alterations may lead to beneficial functions of HDL, which is involved in anti-atherogenic properties in the circulation.

• Applied Chemistry for Engineering
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• v.7 no.1
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• pp.136-144
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• 1996

Polyacrylic super absorbent polymer(SAP) containing sorbitol was synthesized by inverse-suspension polymerization method. Sodium acrylate and acrylic acid were used as a monomer, ethylene glycol dimethacrylate(EGDMA) and glycerol polyglycidyl ether(GPGE) were used as a crosslinking agent, potassium persulfate(PPS) was used as an initiator, and cyclohexane was used as a solvent. Content of sorbitol was from 10mol% to 50mol% according to the mol ratio of acrylic acid monomer. The size distribution of the round shaped polymeric particle was $177{\sim}707{\mu}m$. Absorption amount of the polymer containing sorbitol was 785 to 1086 times of the polymer weight in distilled water, was 50 to 83 times in 0.9 % NaCl solution. Absorption and retention amount of the polymer were decreased with increasing the amount of sorbitol, but the polymer has an endothermic property which is +5 cal/g SAP.

• Archives of Pharmacal Research
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• v.29 no.12
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• pp.1164-1170
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• 2006

A triptolide-lysozyme (TP-LZM) conjugate was synthesized to achieve renal specific delivery and to reduce the side effects of triptolide. Triptolide was coupled to lysozyme through succinic via an ester bond with an average coupling degree of 1 mol triptolide per 1 mol lysozyme. The lysozyme can specifically accumulate in the proximal tubular cells of the kidney, making it a potential carrier for targeting drugs to the kidney. The structure of triptolide succinate (TPS) was confirmed by IR, $^{1}H-NMR$, MS and UV. The concentrations of triptolide in various samples were determined by reversed-phase high-performance liquid chromatography (HPLC). In this study, the physicochemical and stability profiles of TP-LZM under various conditions were investgated the stability and releasing profiles of triptolide-lysozyme (TP-LZM) under various conditions. In vitro release trails showed triptolide-lysozyme was relatively stable in plasma (less than 30% of free triptolide released) and could release triptolide quickly in lysosome (more than 80% of free triptolide released) at $37^{\circ}C$ for 24 h. In addition, the biological activities of the conjugate on normal rat kidney proximal tubular cells (NRK52E) were also tested. The conjugate can effectively reduce NO production in the medium of NRK52E induced by lipopolysaccharide (LPS) but with much lower toxicity. These studies suggest the possibility to promote curative effect and reduce its extra-renal toxicity of triptolide by TP-LZM conjugate.

• The Korean Journal of Pesticide Science
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• v.2 no.1
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• pp.12-17
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• 1998

Salicylic acid and 3-hydroxy benzoic acid are nitrated and esterified with some alcohols. Five phosphate and six carbamate compounds of alkyl-5-nitrosalicylate and alkyl-3-hydroxy-4-nitrobenzoate are synthesized by reacting alkyl-5-nitrosalicylate and alkyl-3-hydroxy-4-nitrobenzoate with diethyl-chlorophosphate and methyl isocyanate. As the bioassay results of synthesized compounds on five insects and six pathogens, the brown planthopper (BPH, Nilaparvata lugens) mortality of O-(2-carbomethoxy-4-nitrophenyl) O,O-diethylphosphate and O-(2-nitro-5-carbo methoxyphenyl) O,O-diethylphosphate was 96%, while four compounds including O-(2-carbo-(2-chloroethoxy)-4-nitrophenyl) O,O-diethylphosphate showed more than 95% of fungicidal activity on rice blast.

• Korean Journal of Veterinary Research
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• v.36 no.3
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• pp.599-605
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• 1996

This study was designed to examine the mechanism of penile erection in adult bull by analyzing the responses of bovine proximal retractor penile muscle strips(BRP) to electtical field stimulation(EFS), exogenous nitric oxide(NO), NO synthesis precursor(L-arginine), NO synthase inhibitors(L-NAME, L-NMMA), guanylate cyclase inhibitor(methylene blue) and nonspecific potassium channel blocker(tetraethylammonium, TEA) treatments. Isometric tension of BRP was measured using physiograph. Results were summarized as follows: 1. EFS of nonadrenergic noncholinrgic(NANC) nerve in BRP produced frequency-dependent inhibitory responses to the contraction induced by co-treatment of epinephrine, guanethidine and atropine. The inhibitory responses to EFS were blocked by tetrodotoxin(TTX, $1{\mu}M$). 2. Treatment of L-NAME ($10,\;20{\mu}M$) inhibited the relaxation to EFS whereas L-NMMA ($100{\mu}M$) had no effect. 3. Treatment of NO($20,\;40{\mu}M$; as an acidified solution of $NaNO_2$) induced concentration-dependent relaxation whereas preincubation of TTX($1{\mu}M$) and L-NAME($20{\mu}M$) had no effect on the relaxation response. 4. L-arginine treatment(10mM) blocked the inhibitory effect of L-NAME($20{\mu}M$). 5. Pretreatment of methylene blue($40{\mu}M$) reduced the NANC-induced relaxation of BRP. 6. Tetraethylammonium(TEA, 80mM) reduced NANC relaxation. These results suggest that NO may act as a NANC neurotransmitter in BRP and the effects might be mediated by cGMP and potassium channel.

• Applied Chemistry for Engineering
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• v.3 no.4
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• pp.694-700
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• 1992

Aromatic polyamides and polyesters with fexible spacers are prepared by Heck reaction with palladium catalysts In presence of carbon monoxide gas. Dichlorobis(triphenyl phosphine) plladium(II) ($PdCl_2(PPh_3)_2$) and palladium chloride ($PbCl_2$) are used as catalysts. Polyamides and polyesters prepared by his polymerization system have similar transition temperatures. Flexible spacer substituted on phenylene units are varied from hexyl to hexadecyl, the length of spacers effected on transition temperatures of substituted polymers.

• Biomolecules & Therapeutics
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• v.8 no.4
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• pp.325-331
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• 2000

The present study was designed to assess the role of spinal adenosine $A_2$ receptor in the regulation of cardiovascular functions such as mean arterial pressure (MAP) and heart rate (HR) in male Sprague-Dawley rats. Rats (250~300 g) were anesthetized with urethane and paralyzed with d-tubocurarine and artificially ventilated. blood pressure and HR were continuously monitored via a femoral catheter connected to a pressure transducer and a polygraph. Drugs were administered intrathecally using injection cannula through guide cannula which was inserted inthrathecally at lower thoracic level through a puncture of an atlantooccipital mombrane. Intrathecal injection of an adenosine $A_2$ receptor agonist, 5'-(N-cyclopropyl)-carboxamaidoadenosine (CPCA; 1, 2 and 3 nmol, respectively), produced a dose-dependent decrease in MAP and HR. Pretreatment with $N^{G}$-nitro-L-arginine methyl ester (L-NAME), a nitric oxide synthase inhibitor or 10 nmol of MDL-12,330, an adenylate cyclase inhibitor blocked significantly the depressor and bradycardic effect of 2 nmol of CPCA. But, Pretreatment with 3 nmol of bicuculline, gamma-aminobutyric acid A (GAB $A_{A}$) receptor antagonist, or 50 nmol of 5-aminovaleric acid, GAB $A_{B}$ receptor antagonist did not inhibit the depressor and bradycardic effect of 2 nmol of CPCA. These results indicate that adenosine $A_2$ receptor in the spinal cord plays an inhibitory role in the regulation of cardiovascular function and that the depressor and bradycardic action of adonosine $A_2$ receptor are mediated via the synthesis of nitric oxide and the activation of adenylate cyclase in the spinal cord of rats.s.s.s.

• Polymer(Korea)
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• v.25 no.2
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• pp.279-292
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• 2001

Two kinds of (hydroxypropyl)cellulose(HPCs) with different molar substitution (MS) and three types of derivatives based on the HPCs: (acetoxypropyl)celluloses, (ethoxypropyl)celluloses, and (cyanoethoxyprofyl)celluloses were synthesized, and their thermal and mesomorphic properties were investigated. All samples, which exhibit cholesteric reflection colours at room temperature, formed right-handed helicoidal structures whose optical pitches (λ$_{ms}$ ) increase with temperature. However, the isotropization ($T_{i}$) and glass temperatures, the magnitude of λ$_{m}$ of the mesophase at the same temperature, and the temperature dependence of λ$_{m}$ of the investigated derivatives highly depended on MS and the length and structure of the side chain introduced in HPC. The results were discussed in terms of the difference in the polarity and flexibility of the substituents and the distance between the main chains. For all derivatives, Am values approached infinity at temperatures above the $T_{i}$, of the mesophase, and no reversal in the sense of the pitch with temperature was detected.

• Polymer(Korea)
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• v.36 no.5
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• pp.643-650
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• 2012

In order to improve the thermal stability of polyurethane, we synthesized poly(adipate urethane) (PAU) and three PAU composites, PAU/30B (2.7 wt% 30B), PAU/MP (2.2 wt% MP), PAU/30B/MP (2.2 wt% 30B and 2.2 wt% MP), from poly(oxydiethylene adipate)-diol (PAD), 4,4'-methylene diphenyl diisocyanate (MDI), Cloisite 30B (30B), and melamine phosphate (MP). 30B and MP were introduced into the reactant mixture at the initial stage of the esterification between adipic acid and diethylene glycol, so 30B and MP were evenly dispersed in the PAU composites for long period. At temperatures lower than $250^{\circ}C$, the PAU composites were degraded faster than pristine PAU, mainly due to the decomposition of 30B and MP. At higher temperatures, the 30B and MP enhanced the thermal stability of the PAU composites. Compared with the pristine PAU, the thermal decomposition rates of the PAU composites decreased by 13~17%. In air, the residual weights of PAU/30B, PAU/MP, and PAU/30B/MP were 2.4, 2.3, and 7.3 wt% at $700^{\circ}C$, respectively.

• Archives of Pharmacal Research
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• v.27 no.5
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• pp.512-517
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• 2004

The structural relationship of 16 asiatic acid (AA) derivatives, including AA and asiaticoside (AS) to cytotoxicity and anti-hepatofibrotic activity in HSC-T6 cells, were investigated. Cytotoxicities of AA derivatives varied from 5.5 $\mu$M to over 2000 $\mu$M of $IC_{50}$/ depending on AA functional group modifications. Substituting the hydroxyl group at the C(2) to N≡C and substituting bulky groups for dihydroxyl groups at (3), (23) of the A-ring increased the cytotoxicity, but keto group at C(11) and benzoyl ester at C(2) were greatly reduced it. Modification of the carboxylic acid group at C28 also reduced the cytotoxicity. The collagen synthesis determined by hydroxyproline content in the cells was inhibited from a maximum of 48% (Zlx-i-85 and 87) to 15% (AS) by AA derivatives. The anti-hepatofibrotic effect of these compounds might be due to the reduced expression of prolyl 4-hydroxylase $\alpha$ and $\beta$ subunits and TIMP2. However, the inhibition of collagen by asiaticoside derivatives did not show any structural-activity relationship.