• IMMUNE NETWORK
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• v.11 no.6
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• pp.420-423
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• 2011

Since CKD-712 has been developed as an anti-inflammatory agent, we examined the effect of CKD-712 during TLR4 signaling. Using HEK293 cells expressing TLR4, CKD-712 was pre-treated 1 hr before LPS stimulation. Activation of NF-${\kappa}B$ was assessed by promoter assay. The activation of ERK, JNK, p38, IRF3 and Akt was measured by western blotting. CKD-712 inhibited the NF-${\kappa}B$ signaling triggered by LPS. The activation of ERK, JNK, p38 or IRF3 was not inhibited by CKD-712. On the contrary the activation of these molecules was augmented slightly. The activation of Akt with stimulation of LPS was also enhanced with CKD-712 pre-treatment at lower concentration, but was inhibited at higher concentration. We suggest that during TLR4 signaling CKD-712 inhibits NF-${\kappa}B$ activation. However, CKD-712 augmented the activation of Akt as well as Map kinases. Therefore, we suggest that CKD-712 might have a role as an immunomodulator.

• KSBB Journal
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• v.10 no.3
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• pp.343-348
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• 1995

Human lipocorin-I(LCI) is a calcium ion-dependent and phospholipid-binding protein which exhibits an anti-inflammatory activity by inhibiting phospholipase A2 activity. In this study, the LCI gene containing its own terminator region was joined to GAL10 promoter-ppL (prepro-leader sequence of mating factor a). An ATG start codon of LCI gene was placed at downstream with KR endoprotease recognition site(Lys-Arg) of ppL. Recombinant S. cerevisiae harboring the LCI expression/secretion vector, pYGLPT5, was aerobicall grown on a liquid YPDG medium al $30^{\circ}C$ for 72hys. The whole cell and culture supernatant were separated after centrifugation, and the expressed LCI was analyzed by SDS-PAGE and western blotting methods. A majority fraction of the expressed LCI was found to be accumulated in the intracellular fraction, resulting in very low secretion efficiency of about 7.4%. About $500mg/\ell$ of LCI was extracellularly produced by the fed-batch culture employing the controlledfeeding of glucose and galactose. The secreted LCI was purified by ultrafiltration and hydroxylapatite column chromatography, and a purity of more than 99% was obtained.

• Journal of Pharmacopuncture
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• v.12 no.1
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• pp.43-51
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• 2009

Objective : The purpose of this study is to present the standard for practical application of ginger herbal pharmacopuncture Material and Methods : We refer to ancient literatures and the recent papers for ginger. Conclusions : The following results have been obtained 1. The effect of ginger(Zingiber officinale Roscoe) is to "release exterior", "balance nutrient & defensive qi", "resolve phlegm", "arrest coughing", "warm the lungs". So ginger herbal pharmacopuncture can be applied to treating fever, chilling sign, headchae, snuffle and gasping cough due to cold affection and treating the symptoms like sputum and asthma that be revealed by pulmonary disease. 2. The effect of ginger is to "warm spleen and stomach", "arrest vomiting" "promote normal flow of water". So ginger herbal pharmacopuncture can be applied to treating nausea, vomiting, abdominal distension and diarrhea due to phlegm & dampness and treating edema. 3. The effect of ginger is to eliminate blood stasis. So ginger herbal pharmacopuncture can be applied to treating contusion, blood stasis, sprain and gynecologic disease. 4. Ginger can treat myalgia and pain due to wind-damp and have anti-inflammatory effect in pharmacology. So ginger herbal pharmacopuncture can be applied to treating disease of joint, ligament and muscle. 5. Ginger can resolve phlegm and resuscitate. So ginger herbal pharmacopuncture can be applied to treating unconsciousness. But, treating incipient cardiovascular accident, it needs to call your special attention to the danger of blood pressure increase. 6. In pharmacology, ginger is effective for antitumor, antioxidant effects and activating immunocyte. So ginger herbal pharmacopuncture can be applied to treating broadly varieties of tumor and allergic disease.

• The Korean Journal of Pain
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• v.6 no.1
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• pp.32-39
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• 1993

Despite their sometimes fatal complications such as respiratory depression when used for postoperative pain control, intravenous and epidural narcotics remain the mainstay of treatment regimens. Because of the problems, anesthesiologists are seeking alternatives. We compared the analgesic effect and complications of continuous intravenous morphine with ketorolac. Ketorolac is a non-steroidal agent with potent analgesics and moderate anti-inflammatory activity. Forty ASA physical status I or II patients were given morphine(20 patients) or ketorolac(20 patients):In the morphine group, an initial bolus dose of 2 mg i.v. was given followed by continuous infusion at a rate of 1 mg/hr for 48 hours. The ketorolac group was given initial bolus of 30 mg i.v. This was followed by continuous infusion at a rate of 3.75 mg/hr for 48 hours using a Baxter Daymate Infuser. We checked systolic, diastolic and mean arterial pressure, heart rate, visual analogue scale(VAS) and the Prince Henry Score(PHS). This was done before the initial bolus, at 5, 15, 30 and 60 min, at 2, 6, 12, 24 and 48 hours after administration. We observed the side effects nausea and vomiting, pruritus, hypotension, somnolence, urinary retention and respiratory depression. From our study we believe ketorolac in selected patients, is as effective as morphine in alleviating postoperative pain without side effects of morphine.

• Journal of Pharmaceutical Investigation
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• v.34 no.6
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• pp.491-497
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• 2004

We investigated some important factors which affect the transdermal flux of ketoprofen, a nonsteroidal anti-inflammatory agent, as a first step to provide some basic knowledge for the development of a iontophoretic transdermal patch system. Factors such as current density, polarity, buffer (HEPES) and electrolyte concentration and pH were studied using hairless mouse skin. The effect of poly(L-lysin), which is known to affect the electro-osmotic flow through skin, on flux was also studied. Passive flux was about $20\;{\mu}g/cm^2hr$ at pH 4.0, but was negligible at pH 7.4 where all ketoprofen molecules dissolved are ionized (ketoprofen pKa=5.94). At pH 4.0, application of anodal current increased the flux further above the passive level, however anodal flux at pH 7.4 was much smaller than passive flux at pH 4.0. The application of cathodal current at pH 4.0 increased the average flux to $30-40\;{\mu}g/cm^2hr$, depending on the current density applied. At pH 7.4, cathodal flux was only about $5\;{\mu}g/cm^2hr$. Decrease in buffer and electrolyte concentration increased this cathodal flux about 10 fold. However decrease in HEPES buffer concentration 100 fold did not affect the flux. Anodal flux of acetaminophen was much larger than cathodal flux, indicating that electroosmotic flow can be playing an important role in the flux. Poly(L-lysin) increased the cathodal flux at pH 7.4. These results provide some important insights into the mechanism of transdermal flux of ketoprofen and the role of electroosmotic flow.

• Journal of Pharmaceutical Investigation
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• v.34 no.6
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• pp.477-482
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• 2004

The aim of the present study was to investigate the efficacy of a mixed gel formulation composed of sodium carboxymethyl cellulose and gellan gum (Na-CMC gel) for the prevention of adhesions after laminectomy. The anti-adhesive effect of the Na-CMC gel was tested in a controlled randomized study using an animal model of lumbar laminectomy. The animals (60 female Sprague-Dawley rats) were randomly allocated into two treatment groups to receive the Na-CMC gel on the injured area or no gel (control). The incidence of adhesions and their grade were blindly evaluated at 4, 8 and 12 weeks after surgery. The amount of scar tissue and tenacity were grossly reduced by the Na-CMC gel at postoperative 4, 8, and 12 weeks. The mean adhesion scores were 0.75, 1.25, and 1.38 at 4, 8, and 12 weeks in the gel-treated group, respectively. No significant inflammatory reaction was observed and the healing of wound was not affected by the Na-CMC gel. The Na-CMC gel reduced the amount of scar formation and tenacity in rat laminectomy model without affecting the healing of operation wound and other complications. Therefore, the Na-CMC gel may be the potential to prevent postsurgical adhesions in clinical state.

• Journal of Pharmaceutical Investigation
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• v.16 no.2
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• pp.43-54
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• 1986

To increase the bioavailability of clonixin, clonixin argininate was prepared and compared with clonixin by determining solubility, pKa, lipid-water partition coefficient, dissolution rate and in vivo tests. The results are summerized as followings; 1) The solubility of clonixin argininate was increased by 20 times in water, about 1.2 times in pH 1.2 and pH 8.0 buffer solution, and about 1.8 times in pH 6.8 buffer solution compared with that of clonixin. 2) pKa values of clonixin, clonixin lysinate and clonixin argininate were 6.32, 7.20 and 7.45, respectively. 3) The lipid-water partition coefficient of clonixin argininate was increased more than that of the clonixin in n-hexane, carbon tetrachloride, chloroform, methylene chloride, and n-butanol, but the partition coefficient of clonixin was increased more than that of clonixin argininate in benzene/pH 1.2 buffer solution, ether/pH 8.0 buffer solution, and 3-methylbutyl acetate/pH 1.2, pH 8.0 buffer solution. 4) The time required to dissolve 60% $(T_{60%},\;min.)$ of clonixin argininate was about 1.5 min. in water and pH 1.2 buffer solution, and about 5 min. in pH 6.8 buffer solution. $T_{60%}$ of clonixin lysinate was about 1.5 min. in water, about 1.8 min. in pH 6.8 buffer solution, and about 8 min. in pH 1.2 buffer solution. But $T_{60%}$ of clonixin was about 96 min. in pH 6.8 buffer solution, over 2 hours in water and pH 1.2 buffer solution. 5) Anti-inflammatory effect of clonixin argininate was increased more than that of clonixin over 6 hours, and that of clonixin lysinate was followed by lapse of time. 6) Analgesic effect of clonixin argininate was increased by 1.5 times more than that of clonixin and the effect of clonixin argininate was nearly identical with that of clonixin lysinate. 7) The absorption rates (Ka) of clonixin, clonixin lysinate and clonixin argininate were $0.169\;hr^{-1},\;0.652\;hr^{-1}$ and $0.723\;hr^{-1}$ in situ, respectively.

• Journal of Pharmaceutical Investigation
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• v.37 no.6
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• pp.359-364
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• 2007

Pine bark extract is well-known as a very powerful antioxidant, anti-inflammatory, and antibiotic material. French maritime pine bark extract ($Pycnogenol^{(R)}$) of Horphag Research has monopolized the world market over 30 years. Korean red pine bark extract ($Pinexol^{(R)}$) was first manufactured by the patent technology of NutraPharm in Korea in 2006. Feasibility of topical gel and patch formulations of Pinexol was systematically investigated by evaluating the skin absorption of catechin as a reference compound. In vitro hairless mouse skin absorption of catechin from gel formulation was higher than that from patches. However, significant amount of catechin was also deposited inside the skin from patch formulations, which were dependent on the types of pressure sensitive adhesives. Thus, it seems to be feasible to control the topical delivery of Pinexol by using both gel and patch formulations, and be necessary to conduct further systematic investigation.

• Journal of Microbiology and Biotechnology
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• v.27 no.9
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• pp.1639-1648
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• 2017

Curcumin is a natural polyphenolic compound, widely acclaimed for its antioxidant, anti-inflammatory, antibacterial, and anticancerous properties. However, its use has been limited due to its low-aqueous solubility and poor bioavailability, rapid clearance, and low cellular uptake. In order to assess the effect of glycosylation on the pharmacological properties of curcumin, one-pot multienzyme (OPME) chemoenzymatic glycosylation reactions with UDP-${\alpha}-{\text\tiny{D}}$-glucose or UDP-${\alpha}-{\text\tiny{D}}$-2-deoxyglucose as donor substrate were employed. The result indicated significant conversion of curcumin to its glycosylated derivatives: curcumin 4'-O-${\beta}$-glucoside, curcumin 4',4"-di-O-${\beta}$-glucoside, curcumin 4'-O-${\beta}$-2-deoxyglucoside, and curcumin 4',4"-di-O-${\beta}$-2-deoxyglucoside. The products were characterized by ultra-fast performance liquid chromatography, high-resolution quadruple-time-of-flight electrospray ionization-mass spectrometry, and NMR analyses. All the products showed improved water solubility and comparable antibacterial activities. Additionally, the curcumin 4'-O-${\beta}$-glucoside and curcumin 4'-O-${\beta}$-2-deoxyglucoside showed enhanced anticancer activities compared with the parent aglycone and diglycoside derivatives. This result indicates that glycosylation can be an effective approach for enhancing the pharmaceutical properties of different natural products, such as curcumin.

• Journal of Dairy Science and Biotechnology
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• v.35 no.4
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• pp.249-254
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• 2017

The purpose of this study was to investigate the acid tolerance, bile acid tolerance, and fermentation activity of lactic acid bacteria isolated from Kimchi in the presence of hydrolysates of whey protein concentrate. Kimchi isolates DK109, DK119, DK121, DK128, DK211, DK212, and DK215, which were identified as Lactobacillus sp., and L. casei DK128 showed the highest acid and bile acid tolerance. To produce whey hydrolysates, enzymes were added to a 10% (w/v) whey protein concentrate (WPC) solution at 1:50 (w/v, protein). The viabilities of the DK strains were determined in the presence of low pH and bile salts. Then, yogurt was produced via fermentation with L. casei DK128, an isolate from Kimchi, in the presence of the following additives: CPP, WPC, and WPC hydrolysates (WPCH) generated by alcalase (A) or neutrase (N). The produced yogurts were subjected to various analyses, including viable cell counts (CFU/mL), pH, titratable activity, and sensory testing. After 8 h of fermentation, the pH and titratable activity values of all test samples were 4.2 and 0.9, respectively. The viable counts of LAB were $3.49{\times}10^8$, $5.72{\times}10^8$, $7.01{\times}10^8$, and $6.97{\times}10^8$, for the Control, CPP, A, and N samples, respectively. These results suggest that whey proteins have potential as dietary supplements in functional foods and that WPCH could be used in yogurt as a low-cost alternative to CPP.