• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.20 no.2 s.33
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• pp.1-9
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• 2007

Objective : In this study, the ethanol extract from flowers of Lespedeza bicolor was investigated for their dermal bioactive properties related to cosmeceuticals such as depigmentation and radical scavenging effect. Results : The ethanol extract from flowers of Lespedeza bicolor showed considerable radical scavenging activity ($SC_{50}:\;10\;{\mu}g/ml$) and inhibited the production of nitric oxide (NO) in Raw 264.7 macrophages activated with the endotoxin lipopolysaccharide (LPS). Although the proliferation of B16/F10 cells was slightly decreased by the ethanol extract from flowers of Lespedeza bicolor at the concentration of $100\;{\mu}g/ml$, it did not appear necrosis. The ethanol extract from flowers of Lespedeza bicolor down-regulated melanin formation effectively. Methods : The free radical scavenging activity of Lespedeza bicolor was assayed in cell free systems using a stable free radical, 1,l-diphenyl-2-picrylhydrazyl (DPPH). Nitrite accumulated in culture medium was measured as an indicator of NO production using a Griess reaction. Cell viability was measured by MTT assay and melanin content was assessed using the method of Hosei with some modifications. Conclusions : These results suggest that the ethanol extract from flowers of Lespedeza bicolor is a potent depigmetation agent and it may be a candidate for antioxidant and anti-inflammatory agent.

• Journal of Life Science
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• v.18 no.4
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• pp.509-514
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• 2008

Tremendous natural product extracts were used as a herb medicine remedy or therapy for centuries. Because these extracts have various biological activities, we examined the effects of Gryllotalpa orientalis extract for anti-oxidant and anti-inflammation activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric reducing ability of plasma (FRAP), hydroxy radical scarvenging and cyclooxygenase-2 promoter assays. Gryllotalpa orientalis extracts were prepared from solvents such as distilled water (DW), dimethyl sulfoxide (DMSO), ethanol and methanol. The results showed that Gryllotalpa orientalis extracts have potent DPPH (methanol extract), FRAP (DW extract) and hydroxy radical scavenging (DW and methanol extracts) activity than any other extracts used. A significant inhibition of cyclooxygenase-2 (Cox-2) promoter activity was detected in the presence of DMSO extract or ethanol extract. Collectively, the present results suggested that Gryllotalpa orientalis extract could be used for anti-oxidant and/or anti-inflammation agent for human or agricultural purposes.

• Childhood Kidney Diseases
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• v.6 no.1
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• pp.75-84
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• 2002

Purpose Acute pyelonephritis of growing kidneys may result in renal scarring. TGF-${\beta}1$, inflammatory cytokine, has been suggested to play an important role in promoting renal scarring through apoptosis, suppression of cellular proliferation and fibrosis. We observed the effects of a potent anti-inflammatory agent, methylprednisolone on apoptosis and renal scarring in experimentally induced acute pyelonephritic weaning rats. Materials and Methods: To induce ascending pyelonephritis a saline solution containing Escherichia coli type ATCC No. 25922, pili- form (107 bacteria/mL) was infused into the bladder through the 16-guage silicone cannula for 48 hours to 102 three-week-old Sprague-Dawley rats (50-60g). Experimental groups were divided into three groups according to the treatment protocols, group I (ceftriaxone only, n=3l), group II (methylprednisolone+ceftriaxone n=28), control group (n=43) was not treated. Histopathologic scores of inflammatory changes, fibrosis and tubular atrophy, the apoptosis index and TGF-${\beta}1$ expression score were observed at post-infection 1 and 3 week. Datas were analysed using ANOVA test and P value below 0.05 was interpreted as significant. Results: The mortality rate ($21.4\%$) of group II was not different to the control group ($41.9\%$) and group I ($32.3\%$). The inflammatory score of group II ($0.8{\pm}0.87$) at week 1 was significantly lower than those of the control group ($2.3{\pm}0.87$) and Group I ($1.7{\pm}0.79$) (P<0.05). Apoptosis index of group II ($2.9{\pm}2.15$) at week 1 was significantly lower than those of the control group ($10.0{\pm}1.95$) and group 1 ($8.3{\pm}2.53$) (P<0.05). TCF-${\beta}1$ expression score of group II ($0.8{\pm}0.72$) at week 1 was significantly lower than those of the control group ($1.9{\pm}0.68$) and group I ($1.8{\pm}0.60$) (P<0.05). The fibrosis score of group II ($1.1{\pm}1.10$) at week 3 was significantly lower than that of the group I ($1.8{\pm}0.83$) (P<0.05) Conclusion: Conclusion Combined treatment with methylprednisolone and ceftriaxone reduced inflammation, fibrosis, apoptosis and TGF-${\beta}1$ expression in acute pyelonephritic weaning rats, compared to ceftriaxone alone. Anti-inflammatory agent supplemented to antibiotics could prevent renal scarring more effectively. (J Korean Soc Pediatr Nephrol 2002 ; 6 : 75-84)

• 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.33 no.1
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• pp.21-28
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• 2003

Ketorolac tromethamine(KT) is a nonsteroidal agent with potent analgesic and moderate anti-inflammatory activity. The lipid-water partition coefficient of KT was evaluated and KT gel was formulated as a gel containing different pH, different concentrations of polymer (poloxamer 407, carbopol 941), propylene glycol, ethanol and various enhancers. The resulting KT gels were evaluated with respect to their viscosity, in vitro drug permeation rate through hairless mouse skin and stability. In n-octanol and chloroform, the lipid-water partition coefficient of KT was the highest at pH 4 phosphate buffer. The apparent viscosity of KT gel increased with an increase in gel pH, polymer and enhancer concentration. But the apparent viscosity of KT gel decreased with an increase in ethanol concentration. The permeation rate of KT through hairless mouse skin from gels different pH was maximum at pH 4 which is close to KT $pK_{a}$ 3.54. The permeation rate decreased with an increase in polymer, propylene glycol concentration. But the permeation rate increased with an increase in ethanol. The increase of drug concentration from 1 to 3% induced linear increase in permeation rate. The best enhancer was the combination of $Labrasol^{\circledR},\;Transcutol^{\circledR}$, oleic acid and l-menthol. In the accelerated stability test(25, 40 and $50{\circ}C$), pH 5 gel was most stable and pH 4 gel was most unstable for 90 days.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.4
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• pp.1807-1810
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• 2014

Background: It is known that inducible nitric oxide synthase (iNOS)/nitric oxide (NO) plays an integral role during intestinal inflammation, an important factor for colon cancer development. Natural compounds from Curcuma longa L. (Zingiberaceae) have long been a potential source of bioactive materials with various beneficial biological functions. Among them, a major active curcuminoid, demethoxycurcumin (DMC) has been shown to possess anti-inflammatory properties in lipopolysaccharide (LPS)-activated macrophages or microglia cells. However, the role of DMC on iNOS expression and NO production in an in vitro inflamed human intestinal mucosa model has not yet been elucidated. This study concerned inhibitory effects on iNOS expression and NO production of DMC in inflamed human intestinal Caco-2 cells. An in vitro model was generated and inhibitory effects on NO production of DMC at 65 ${\mu}M$ for 24-96 h were assessed by monitoring nitrite levels. Expression of iNOS mRNA and protein was also investigated. DMC significantly decreased NO secretion by 35-41% in our inflamed cell model. Decrease in NO production by DMC was concomitant with down-regulation of iNOS at mRNA and protein levels compared to proinflammatory cytokine cocktail and LPS-treated controls. Mechanism of action of DMC may be partly due to its potent inhibition of the iNOS pathway. Our findings suggest that DMC may have potential as a therapeutic agent against inflammation-related diseases, especially in the gut.

• BMB Reports
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• v.47 no.1
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• pp.45-50
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• 2014

Aspirin has been demonstrated to be effective in inhibiting COX-2 and $PGE_2$ in Alveolar macrophages (AMs). However, the mechanisms have not been fully understood. In the present study, we found that pretreatment with aspirin inhibited LPS-induced COX-2 and$PGE_2$ upregulation, $I{\kappa}B{\alpha}$ degradation, NF-${\kappa}B$ activation and the increase of PKC activity, but elevated LPS-induced the decrease of PTP activity. The PKC inhibitor calphostin C dramatically reduced the COX-2 mRNA and $PGE_2$ levels, but the PTP inhibitor peroxovanadium (POV) significantly increased the COX-2 mRNA and$PGE_2$ levels. Furthermore, the PTP inhibitor mitigated the inhibitory effect of aspirin on COX-2 and$PGE_2$ upregulation and NF-${\kappa}B$ activation, whereas the PKC inhibitor enhanced the inhibitory effects of aspirin on the production of COX-2 and$PGE_2$. Our data indicate a novel mechanism by which aspirin acts as a potent anti-inflammatory agent in alveolus macrophages and ALI.

• Archives of Pharmacal Research
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• v.29 no.6
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• pp.508-513
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• 2006

The effect of acteoside, a phenylpropanoid glycoside isolated from Clerodendron trichotomum Thunberg, on histamine and arachidonic acid release was investigated in RBL 2H3 cells. Histamine was dose-dependently released from RBL 2H3 cells by melittin, arachidonic acid and thapsigargin. In extracellular $Ca^{2+}-free$ solution, basal secretion of histamins increased by two fold. The response of histamine release to melittin and thapsigargin in $Ca^{2+}-free$ solution was significantly decreased, whereas the response to arachidonic acid was significantly increased as compared with those in normal solution. Acteoside inhibited histamine release induced by melittin, arachidonic acid and thapsigargin in a dose-dependent manner in the presence or absence of extracellular $Ca^{2+}$. However, the inhibitory activity of acteoside was more potent in normal solution than that in $Ca^{2+}-free$ solution. These data suggest that inhibitory mechanism of acteoside on histamine release may be related to extracellular $Ca^{2+}$. On the other hand, acteoside significantly inhibited arachidonic acid release and prostaglandin $E_2$ production Induced by $0.5\;{\mu}M$ melittin. It is possible that acteoside may be developed as an anti-inflammatory agent.

• Journal of Nutrition and Health
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• v.53 no.1
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• pp.1-12
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• 2020

Purpose: Diabetic nephropathy is one of the most important diabetic complications prompted by chronic hyperglycemia, characterized by glomerulosclerosis, tubular fibrosis, and it eventually causes kidney failure. Nobiletin is a polymethoxyflavone present in tangerine and other citrus peels, and has anti-cancer and anti-inflammatory effects. This study investigated the effects of nobiletin on glomerular fibrosis through inhibition of the transforming growth factor (TGF)-β1-Src-caveolin-1 pathway. Methods: Human renal mesangial cells (HRMC) were incubated in media containing 33 mM glucose with or without 1-20 uM nobiletin for 3 day. The cellular expression levels of fibrogenic collagen IV, fibronectin, connective tissue growth factor (CTGF), TGF-β1, Src and caveolin-1 were all examined. In addition, TGF-β1, Src and caveolin-1 proteins were screened to reveal the relationship among TGF-β1-Src-caveolin-1 signaling in glomerular fibrosis. Results: High glucose promoted the production of collagen IV, fibronectin and CTGF in HRMC, which was inhibited in a dose dependent manner by 1-20 uM nobiletin. The Western blot data showed that high glucose elevated the expression of TGF-β1, Src, caveolin-1 and Rho GTPase. When nobiletin was treated to the HRMC exposed to high glucose, the expression of TGF-β1-Src-caveolin-1 was dampened. Finally, TGF-β1-Src-caveolin-1 signaling pathway was activated in high glucose-exposed HRMC, and such activation was encumbered by nobiletin. Conclusion: These result demonstrated that nobiletin blunted high glucose-induced extracellular matrix accumulation via inhibition of the TGF-β1-Src-caveolin-1 related intracellular signaling pathway. Nobiletin may be a potent renoprotective agent to counteract diabetes-associated glomerular fibrosis that leads to kidney failure.

• Journal of Life Science
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• v.24 no.10
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• pp.1132-1136
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• 2014

A yellow-colored pigment is found in turmeric, or Curcuma longa L. (Zingiberaceae), a perennial herb distributed mainly throughout tropical and subtropical regions. C. longa has potent antiviral, antimutagenic, anti-inflammatory, anticancer, and antioxidant properties. However, pharmacological mechanisms of ethanol extract derived from C. longa remain poorly understood. The aim of this study was to investigate the potential acute toxicity of C. longa (Curcuma longa L.) extract in BALB/c mice administered a single oral dose of 0, 20, 200, and 2,000 mg/kg by gavage. After the administration of the agent, signs of toxicity were observed every hour for the first 6 hr and every day for 14 days. No mortality, abnormal clinical signs, or pathological changes were observed compared to a control group, and there were no differences in the body weights of the control and treatment groups. Biological serum activities were not significantly changed in the treatment group compared to the control group. These results indicate that a single oral administration of C. longa extract does not exert any toxic effects at a dose of 2,000 mg/kg body weight and that the $LD_{50}$ of C. longa extract is greater than 2,000 mg/kg body weight. Accordingly, C. longa appears to have potential in various functional agents or foods, without toxicity.