• Title/Summary/Keyword: ANTI-INFLAMMATORY ACTIVITY

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Formulation Design and Evaluation of Ketorolac Tromethamine Hydrogel for Transdermal Delivery System (경피흡수를 위한 케토롤락 하이드로겔의 제제설계 및 평가)

  • Cho, In-Sook;Lee, Gye-Won;Lee, Jong-Hwa;Jee, Ung-Kil
    • 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.

The Effect of Bee Venom on Scopolamine Induced Memorial Impairment (봉약침액(蜂藥鍼液)이 Scopolamine으로 유발(誘發)된 기억(記憶) 장애(障碍)에 미치는 영향(影響))

  • Song, Jeong-Yeon;Song, Ho-Sueb
    • Journal of Acupuncture Research
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    • v.23 no.3
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    • pp.103-115
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    • 2006
  • Alzheimer's disease (AD) is the most prevalent form of neurodegenerative disease associated with aging in the human population. This disease is characterized by the following 4 structural changes : Atrophy of the Cortex, Parasympathetic, and other neural cells, the existence of Neurofibrillary tangles (NFTs), and the accumulation of Senile plaques. NFTs and Senile plaques is known to be the index of this disease. Senile plaques disturbs the neutro transmission and depletes of Acetylcholine. So, Recovery of Acetylcholine is the primal objective for treating Alzheimer's disease. So, Inhibiting the activity of Acetylcholine Esterase (AChE), which causes the hydrolysus of acetylcholine into choline and acetate, can be seen as a key role for treating Alzheimer's disease. Increasing body of evidence has been demonstrated that Bee Venom Acupuncture (BV) could compete with complex protein involving in multiple step of $NF-_{\kappa}B$ activation and exert the anti -inflammatory potential of combined inhibition of the prostanoid and nitric oxide synthesis systems by inhibition of IKK and $NF-_{\kappa}B$. The effect of BV through behavioral tests after memory impairment induced by Scopolamine. We examined the improving effect of BV on the Scopolamine (1 mg/Kg, i.p.)-induced memorial impairment using passive avoidance response and water maze tests in the mice. BV (0.84, $1.67\;{\mu}g/ml$) reversed the Scopolamine-induced memorial impairment in dose dependent manner. This study therefore suggests that BV acupuncture method may be useful for prevention of development or progression of AD.

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Effects of Cheonggisan and Gagamcheonggisan on the anti-allegic and immune responses in mice (청기산(淸肌散)과 가미청기산(加味淸肌散)이 마우스의 항(抗)알레르기 및 면역반응(免疫反應)에 미치는 영향(影響))

  • Park Eun-Jeong;Kim Yang-Gwi
    • The Journal of Pediatrics of Korean Medicine
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    • v.12 no.1
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    • pp.183-210
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    • 1998
  • Cheonggisan(CGS) is well known for its effect on such allergic disease as urticaria and atopic dermatitis. Gagamcheonggisan(GCGS) was formulated by subtracting several herbs from CGS and adding several herbs to CGS. Even though it is being used frequently in the clinicai medicine for the treatment of above hypersensitivity diseases, basic study to make sure the mechanism of its action is rare. In this study the author tried to know the effect of CGS and GCGS on the vascular permeability, contact dermatitis, granular secretion from mast cells and function of macrophages. The results obtained in this study are as follows : 1. Administration of CGS and GCGS decreased the vascular permeability induced by serotonin and histamine. The decrease by serotonin is more typical and dose-dependent. 2. Administration of CGS and GCGS inhibited foot-pad and ear swelling responses induced by sheep red blood cells and picryl chloride respectively, the inhibition of foot-pad swelling responses is bigger than that of ear swelling responses and both of them are not dependent on the dose3. Treatment of peritoneal mast cells with CGS and GCGS water extract decreased the histamine release triggered by compound 48/80 in a dose dependent fashion 4. Administration of CGS and GCGS increased the phagocvtic activity of peritoneal macrophages and treatment of peritoneal macrophages with CGS activated phagocytic function in a dose dependent fashion. 5. Administration of CGS and GCGS enhanced such reactive oxygen intermediates(ROIs) as superoxide and hydrogen peroxide production from peritoneal macrophages. 6. Treatment of CGS and GCGS activated peritoneal macrophages for the production of ROIs. The above results show that CGS and GCGS decreased the hypersensitivity reactions by inhibiting non-specific inflammatory mediator release and vascular permeability without affecting general immune responsiveness.

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The Effect of Bojungykgitang-Chunbang on Activity of CD4+ T cell

  • Lee Tae Hyong;Kang Hee;Myung Eu Gene;Shim Bum Sang;Choi Seung Hoon;Kim Sung Hun;Ahn Kyoo Seok
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.18 no.2
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    • pp.580-585
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    • 2004
  • BJYGC is often clinically used as a treatment of allergic rhinitis. This study was aimed to find out the effect BJYGC would have on the helper T cell, and how it can promote the subsets of helper T cells to regain their balance that they lost due to immunological diseases. Splenocytes were prepared from BALB/c mice was cultured without stimulation in the presence of BJYGC for 48 hr. The viability of CD4 T cells from Balb/c mouse were measured at various concentrations of BJYGC using the MTS assay. It was somewhat increased up to concentration of 400 ㎍/ml, but did not show any significant difference. Proliferation was measured using the MTS assay, CD4 Th cells were stimulated with anti-CD3/28 in the presence of BJYGC for 48 hr. As evidence for rapid T cell activation, CD25 expression by flow cytometry was evaluated at 10, 50, 100 and 200 ㎍/㎖ of BJYGC. Th cell differentiation experiments were performed to examine whether BJYGC can affect the Th polarization process. CD4 T cells were activated in culture under neutral, Th1-polarized or Th2-polarized conditions in the presence of BJYGC at 10, 100 and 200 ㎍/㎖. Cytokine production was measured by ELISA. This experiment proved that BJYGC could inhibit the secretion of both IL-4 and IFN-γ in neutral condition and polarized condition, too. Considering that BJYGC shows an excellent effect on treating allergies, the author can conclude that its pharmacological action may be associated with decreased IL-4 and, it may also regulate IFN-γ depending the host's need. Also, it was discovered that Th1 cell was pathologic in chronic inflammatory tissue specific diseases, such as insulin dependent diabetes mellitus, multiple sclerosis, RA, and uveitis. We are counting on the BJYGC to be able to control the tendency of Th1 cell predominancy in an immune reaction.

Inhibitory Effect of Gallic acid on Production of Interleukins in Mouse Macrophage Stimulated by Lipopolysaccharide (Gallic acid가 Lipopolysaccharide로 활성화된 마우스 대식세포의 인터루킨 생성에 미치는 영향)

  • Park, Wan-Su
    • Journal of Pharmacopuncture
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    • v.13 no.3
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    • pp.63-71
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    • 2010
  • Objectives: Gallic acid (GA) is the major component of tannin which could be easily founded in various natural materials such as green tea, red tea, grape juice, and Corni Fructus. The purpose of this study is to investigate the effect of Gallic acid (GA) on production of interleukin (IL) in mouse macrophage Raw 264.7 cells stimulated by lipopolysaccharide (LPS). Methods: Productions of interleukins were measured by High-throughput Multiplex Bead based Assay with Bio-plex Suspension Array System based on $xMAP^{(R)}$ (multi-analyte profiling beads) technology. Firstly, cell culture supernatant was obtained after treatment with LPS and GA for 24 hour. Then, it was incubated with the antibody-conjugated beads for 30 minutes. And detection antibody was added and incubated for 30 minutes. And Strepavidin-conjugated Phycoerythrin (SAPE) was added. After incubation for 30 minutes, the level of SAPE fluorescence was analyzed on Bio-plex Suspension Array System and concentration of interleukin was determined. Results: The results of the experiment are as follows. 1. GA significantly inhibited the production of IL-3, IL-10, IL-12p40, and IL-17 in LPS-induced mouse macrophage RAW 264.7 cells at the concentration of 25, 50, 100, 200 uM (p<0.05). 2. GA significantly inhibited the production of IL-6 in LPS-induced mouse macrophage RAW 264.7 cells at the concentration of 50, 100, 200 uM (p<0.05). 3. GA diminished the production of some cytokine such as IL-4, IL-5, and IL-13 in LPS-induced mouse macrophage RAW 264.7 cells. 4. GA did not show the inhibitory effect on the production of IL-$1{\alpha}$ and IL-9 in LPS-induced mouse macrophage RAW 264.7 cells. Conclusions: These results suggest that GA has anti-inflammatory activity related with its inhibitory effects on the production of interleukins such as IL-3, IL-10, IL-12p40, IL-17, and IL-6 in LPS-induced macrophages.

Influence of Ointment Base on In Vitro Release Characteristics of Oregonin (오레고닌의 in vitro 방출 특성에 미치는 연고기제의 영향)

  • Im, Tae-Jong;Oh, Il-Young;Park, Young-Mi;Park, Jong-Hyeok;Lee, Min-Won;Cho, Jae-Youl;Lee, Jae-Hwi;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.37 no.4
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    • pp.211-216
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    • 2007
  • The bark of Alnus japonica has been used for the treatment of fever, hemorrhage and diarrehea in oriental traditional medicine. Recently, it was revealed that the diarylheptanoids from the bark of Alnus japonica possess anti-inflammatory activity and are expected to be applicable for atopic dermatitis. In this study, oregonin, one of major active components in the bark of Alnus japonica, was developed in the form of semisolid formulations for topical delivery. Oregonin was incorporated into four ointment bases: O/W cream, W/O cream, hydrophilic ointment and lipophilic ointment. Oregonin release from all formulation prepared was evaluated. Franz cell method and immersion method were employed to characterize the release patterns of drug from each formulation based on solvent availability. O/W cream showed a better release profile than the other formulations when evaluated with Franz cell method with an order of O/W cream, hydrophilic ointment, W/O cream and lipophilic ointment. In the immersion method, hydrophilic ointment showed the greatest release rate at times 1 hour exceeding compared to other bases with an order of hydrophilic ointment, O/W cream, W/O cream and lipophilic ointment. Hydrophilicity and solvent availability of formulation seems to significantly influence the release rate of oregonin from ointment bases. In this study, we successfully characterized the oregon in ointment and found that o/w cream is a promising formulation for the topical delivery of oregonin.

Oxytocin Ameliorates Remote Liver Injury Induced by Renal Ischemia-Reperfusion in Rats

  • Hekimoglu, Askin Tas;Toprak, Gulten;Akkoc, Hasan;Evliyaoglu, Osman;Ozekinci, Selver;Kelle, Ilker
    • The Korean Journal of Physiology and Pharmacology
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    • v.17 no.2
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    • pp.169-173
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    • 2013
  • Renal ischemia-reperfusion (IR) causes remote liver damage. Oxytocin has anti-inflammatory and antioxidant effects. The main purpose of this study was to evaluate the protective function of oxytocin (OT) in remote liver damage triggered by renal IR in rats. Twenty four rats were randomly divided into four different groups, each containing 8 rats. The groups were as follows: (1) Sham operated group; (2) Sham operated+OT group (3) Renal IR group; (4) Renal IR+OT group. OT ($500{\mu}g/kg$) was administered subcutaneously 12 and 24 hours before and immediately after ischemia. At the end of experimental procedure, the rats were sacrificed, and liver specimens were taken for histological assessment or determination of malondialdehyde (MDA), total oxidant status (TOS), total antioxidant status (TAS), paraoxonase (PON-1) activity and nitric oxide (NO). The results showed that renal IR injury constituted a notable elevation in MDA, TOS, Oxidative stress index (OSI) and significantly decreased TAS, PON-1 actvity and NO in liver tissue (p<0.05). Additionally renal IR provoked significant augmentation in hepatic microscopic damage scores. However, alterations in these biochemical and histopathological indices due to IR injury were attenuated by OT treatment (p<0.05). These findings show that OT ameliorates remote liver damage triggered by renal ischemia-reperfusion and this preservation involves suppression of inflammation and regulation of oxidant-antioxidant status.

Wound Healing Effect of Curcumin Gel for Transdermal Delivery (경피전달을 위한 커큐민 젤의 창상치유효과)

  • Kim, Jin;Kim, Man Jong;Lee, Ki-Young
    • Polymer(Korea)
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    • v.37 no.3
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    • pp.387-392
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    • 2013
  • The aim of this study was to investigate the effect of trasdermal delivery of the curcumin gel on healing of the rats' dorsum wounds. Carbopol 934 and propylene glycol were used to prepare gels containing 1% curcumin. Curcumin gel was evaluated for various properties such as antioxidant, cell viability, anti-inflammatory, in vivo wound healing. The free radical scavenging activity using 1,1-diphenyl-2-picryl hydrazyl (DPPH) was 50% at 12.5 ppm concentration. Inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells by curcumin gel. In the curcumin gel-treated group, the re-epithelialization in wounds was significantly increased compared to the control group throughout the experimental period. These results suggested that curcumin may be helpful for the promotion of wound healing.

Inhibitory Constituents against Cyclooxygenases from Aralia cordata Thunb

  • Dang Nguyen Hai;Zhang XinFeng;Zheng MingShan;Son Kun Ho;Chang Hyeun Wook;Kim Hyun Pyo;Bae KiHwan;Kang Sam Sik
    • Archives of Pharmacal Research
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    • v.28 no.1
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    • pp.28-33
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    • 2005
  • Seven diterpenes, four polyacetylenes, a lipid glycerol, and two sterols were isolated from the methylene chloride fraction of the root of Aralia cordata. Their chemical structures were determined as (-)-pimara-8(14), 15-dien-19-oic acid (2), pimaric acid (3), (-)-kaur-16-en-19-oic acid (4), 17-hydroxy-ent-kaur-15-en-19-oic acid (9), $7{\alpha}$-hydroxy-(-)-pimara-8(14), 15-dien-19-oic acid (10), $16\alpha$, 17 -dihydroxy-(-)-kauran-19-oic acid (11), 16-hydroxy-17-isovaleroyloxy-ent-kauran-19­oic acid (12), falcarindiol (5), dehydrofalcarindiol (6), dehydrofalcarindiol-8-acetate (7), falcarin­diol-8-acetate (8), alpha-mono palmitin (13), stigmasterol (1), and daucosterol (14) by the spectral evidences. These compounds were tested with COX-1 and COX-2 inhibition assays. This study found that compounds 2, 4, 5, 6, 7, 8, and 10 inhibited COX-1 dependent conversion of the exogenous arachidonic acid to $PGE_2$ in a dose-dependent manner with $IC_{50}$ values of $134.2{\mu}M$, $121.6{\mu}M$, $170{\mu}M$, $50.4{\mu}M$, $11.7{\mu}M$, $99.6{\mu}M$, and $69.6{\mu}M$, respectively. But, most of these compounds weakly inhibited COX-2 dependent $PGE_2$ generation. Among them, only compound 4 showed relatively significant inhibitory activity $(IC_{50}\;:\;127.6{\mu}M)$.

Herbal anti-inflammatory immunomodulators as host modulators in chronic periodontitis patients: a randomised, double-blind, placebo-controlled, clinical trial

  • Deore, Girish D.;Gurav, Abhijit N.;Patil, Rahul;Shete, Abhijeet R.;Naiktari, Ritam S.;Inamdar, Saurabh P.
    • Journal of Periodontal and Implant Science
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    • v.44 no.2
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    • pp.71-78
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    • 2014
  • Purpose: Host modulatory therapy has been proposed as a treatment for periodontal diseases. A class of herbal medicines, known to be immunomodulators, alters the activity of immune function through the regulation of informational molecules such as cytokines. In the current study, we tested the hypothesis that herbal immunomodulator drugs act as an adjuvant to scaling and root planing (SRP) in alleviating periodontal inflammation by improving clinical and biochemical parameters. Methods: Sixty healthy subjects (30 in each group) with moderate and severe chronic periodontitis were enrolled in a double-blind, placebo-controlled, double-masked randomised controlled trial. The control group was treated with SRP and a placebo, whereas the test group was treated with SRP followed by dietary supplementation of Septilin for 3 weeks. Periodontal clinical parameters and serum C-reactive protein (CRP) levels were evaluated for all patients at the baseline, 3 weeks, and 6 weeks. Results: Improved gingival index scores found in the test group as compared to the control group were found to be statistically significant only after 3 weeks (P<0.001). In contrast, the decrease in the sulcus bleeding index and pocket depth scores was statistically highly significant in the test group as compared to the control group after 3 weeks and 6 weeks (P<0.001). However, reduced clinical attachment level and CRP scores, as reflected in the test group as compared to the control group, were not found to be statistically significant after both 3 weeks (P>0.05) and 6 weeks (P>0.05). Conclusions: The results of this clinical-biochemical study suggest that dietary supplementation with herbal immunomodulatory agents may be a promising adjunct to SRP and may aid in improving periodontal treatment outcomes.