• Title/Summary/Keyword: Antiinflammatory

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Enantiomeric Profiling Analysis of NSAIDs by Capillary Electrophoresis Using TM $\beta$-Cyclodextrin as the Chiral Selector

  • Kim, Ji-Young;La, Sookie;Kim, Jung-Han;Kim, Kyoung-Rae
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.400.1-400.1
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    • 2002
  • Because of the differences in pharmacological properties between enantiomers of chiral acidic non-steroidal antiinflammatory drugs (NSAIDs) in human body. accurate determinations of their optical purities have been in great need. An efficient capillary electrophoretic (CE) profiling method was developed for the enantioseparation of NSAIDs. Capillary electrophoretic conditions were optimized using TM$\beta$-cyclodextrin as the chiral selectors under MES buffer. (omitted)

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A facile synthesis of simple alkaloids - Synthesis of 2,3-polymethylene-4(3H)-quinazolinones and related alkaloids -

  • Park, Jae-Gyu;Lee, Eung-Seok;Jahng, Yurng-Dong
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.251.2-251.2
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    • 2003
  • The 2,3-trimethylene-4(3H)-quinazolinone and 2,3-tetramethylene-4(3H)-quinazolinone are not the only alkaloids isolated from plants. but are the part of a family of intriguing alkaloids including the bronchodilator vasicinone, anti-endotoxic isaindigotone, cytotoxic luotonins, antibiotic tryptanthrin, and antiinflammatory rutacearpine as well as related alkaloids. (omitted)

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Isolation of Ginkgolides and the Effect of These Components on Inflammation in Mice Induced by Complete Freund's Adjuvant.

  • Lee, Soon-Hyun;Han, Yong-Moon
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.137.3-138
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    • 2003
  • The major active components of EGb 761, extract of Ginkgo biloba leaves, include flavonoid glycosides and unique diterpenes known as ginkgolides. Ginkgolides are potent inhibitors of platelet activating factor. In this study, we investigated antiinflammatory activity of ginkgolides on the Complete Freund"s Adjuvant (CFA)-induced mice. The ginkgolides were extracted from commercially available EGb 761. This extracting procedure was done by sequential treatments of the EGb 761 with chloroform, methanol, and water. (omitted)tted)

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Antidiabetic activity of Cultivated Cordyceps pruinosa

  • Kim, Tae-Woong;Sung, Jae-Mo;Yang, Ki-Sook
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.209.3-209.3
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    • 2003
  • Cordyceps species has been used as antiinflammatory, antitoxic, diuretic in folk remedies. Recent research has been reported the effect of anticancer, antidiabetic, antimutagenic, antilipid peroxidation. We examined the antidiabetic activity of cultivated Cordyceps pruinosa on streptozotocin-induced diabetic rats. The blood glucose level was recovered by treatment with Cordyceps pruinosa ethanol extract. The contents of GPT, total cholesterol and xanthine oxidase, glutathione peroxidase, catalase activities of the cytosol were significantly decreased as compared to the diabetic group. (omitted)

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Antiinflammatory Effect of Lactic Acid Bacteria: Inhibition of Cyclooxygenase-2 by Suppressing Nuclear Factor-${\kappa}B$ in Raw264.7 Macrophage Cells

  • Lee, Jeong-Min;Hwang, Kwon-Tack;Jun, Woo-Jin;Park, Chang-Soo;Lee, Myung-Yul
    • Journal of Microbiology and Biotechnology
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    • v.18 no.10
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    • pp.1683-1688
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    • 2008
  • Lactobacillus casei 3260 (L. casei 3260) was evaluated in relation to the inflammatory response mediated by lipopolysaccharide (LPS)-induced nuclear factor-${\kappa}B$ (NF-${\kappa}B$) and cyclooxygenase-2 (COX-2) expression in Raw264.7 macrophage cells. The treatment of Raw264.7 cells with L. casei 3260 significantly inhibited the secretion of tumor necrosis factor-$\alpha$ (TNF-$\alpha$) and prostaglandins $E_{2}\;(PGE_{2})$, followed by suppression of COX-2. To clarify the molecular mechanism, the inhibitory effect of L. casei 3260 on the NF-${\kappa}B$ signaling pathway was examined based on the luciferase reporter activity. Although the treatment of Raw264.7 cells with L. casei 3260 did not affect the transcriptional activity of NF-${\kappa}B$, it did inhibit NF-${\kappa}B$ activation, as determined by the cytosolic p65 release and degradation of I-${\kappa}B{\alpha}$. Therefore, these findings suggest that the suppression of COX-2 through inhibiting the NF-${\kappa}B$ activation by LPS may be associated with the antiinflammatory effects of L. casei 3260 on Raw264.7 cells.

The Effects of Sophorae radix Extracts on CGRP Immunoreactive Neurons of Spinal Cord and Ganglia in Experimental Arthritic Rat Model (실험적 관절염 흰쥐 모델에서 고삼추출액이 척수와 척수신경절의 CGRP 면역반응 신경원에 미치는 영향)

  • Shin Hyun Jong;Lee Kwang Gyu;Ryuk Sang Won;Lee Sang Ryong;Ko Byung Moon;Lee Chang Hyun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.16 no.1
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    • pp.117-123
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    • 2002
  • To investigate the antiinflammatory and analgesic effects of Sophorae radix extracts administered to the arthritic rat model, immunohistochemical stains for CGRP in the L4, L5 and L6 spinal cord and ganglia were done, and paw swelling thickness were measured. Complete Freund,s Adjuvant(CFA) were injected to subcutaneous tissue of left foot paw of rats to induce arthritis. Sophorae radix extracts was administered immediately after CFA injection for 10 days. The spinal cord and ganglia were frozen sectioned(30㎛). These sections were stained by CGRP immunohistochemical staining method, and observed with light microscope. The results were as follows : 1. The change of paw swelling thickness of experimental group decreased from 4 day to 10day after CFA injection compared to control group. 2. The change of differential leukocytes counts of experimental group increased the ratio of lymphocytes. and decreased the ratio of neutrophils compared to control group. 3. The change of CGRP immunoreactive nerve fiber of dorsal horn of experimental group was dense stained compared to control group. 4. The number of CGRP immunoreactive neurons of L4 and L5 spinal cord of experimental group was less than in those control group. These results suggested that Sophorae radix extracts reduces the number of CGRP immunoreactive neurons and nerve fibers of spinal cord and ganglia, and decrease paw swelling thickness in arthritic rat model, which may be closely related to analgesic and antiinflammatory effects of Sophorae radix.

High Throughput Screening for Natural Products to Find Biologically Active Compounds : Natural Products versus Combinatorial Chemistry

  • Sankawa, Ushio
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.11a
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    • pp.47-50
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    • 1997
  • Drug development began with the finding of biologically active compounds which are obtained by chemical synthesis or from natural sources. The advent of Combinatorial Chemistry is recognized as a strategy which has a potential to change the methodology of research and development(R&D) of new drugs. Drug development has been carried out with diverse strategies. In the past several decades a variety of new methodology have been introduced in R&D. Random screening of accumulated synthetic samples which had been synthesized for development of other drugs led to the discovery of new drugs. The typical examples are anti-asthma drug trimethoquinol and calcium antagonist diltiazem. (herbesser). In particular the latter drug has been used as a calcium antagonist worldwide, however it was first synthesized to find new tranquilizer and this is the reason why diltiazem has benzodiazepam skeleton. The random screening contributed in the finding of new drugs were carried out with whole animal test and it is a standard methodology in R&D of new drugs. Aspirin is the first synthetic non-steroidal antiinflammatory drug(NSAID) and has been used for more than one hundred years. It is the first example of drug developed from natural product. Salicin is the main constituent of willow bark which had been used in Europe for a long time to treat arthritis and aspirin was developed from salicin. Most of NSAID used clinically were developed from the structure of aspirin, however it took 70 years to clarify why aspirin exhibits its antiinflammatory, analgesic and antipyretic activities. The target of aspirin is cyclooxygenase(COX)which is the first enzyme involved in arachidonate cascade leading to the production of prostaglandins(PG) and thromboxan(TX). Side effect of aspirin causing ulcer in stomach is rather serious problem, since aspirin is so popular drug easily obtained in drug store(OTP). This problem is now going to be solved by a new finding on COX, which have two different types, one is constitutionally expressed COX 1 in almost all organs and the other is inducible COX 2. COX 2 is the responsible enzyme in inflammation etc and now the search of COX 2 specific inhibitors is the target of R&D of next generation NSAID.

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Study on pharmacological activities of the roots of Cicorium intibus

  • Yim, Dong-sool;Kim, Kwang-sub;Cheong, Jae-hoon;Lee, Sook-yeun
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.04a
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    • pp.74-74
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    • 1997
  • Chicory is used popularly. We use leaves of the plant as ordinary mea1, and roots as a substitute of tea materials. It also has been asserted that it has clinical effects on weakness, hepatic disease, diabetes, etc. However, experimental evidences are so insufficient that we started these studies. For antiinflammatory activity, MeOH Ex. was orally administered to rats, and decreased amounts of paw edema induced by carrageenan injection were measured. For bile secretion increament, rats were administered total MeOH, EtOAc fraction, and BuOH fraction Ex. respectively. One hour later, bile ducts were cannulated, and we collected bile every 20 minutes for 4 hours. For hepatoprotective activity, CCl$_4$-intoxicated mouse were treated with MeOH Ex., then s-GPT, S-GOT, and liver weight were measured. For antidiabetic activity, rats were induced diabetes by streptozocin 45mg/kg(i.v) injection. One week later, 1000mg/kg of total MeOH Ex. of chicory root was orally administered. We divided rats into three groups. Group 1 rats were administered only once, group 2 ones once a day for one week, and group 3 ones for three weeks. The concentrations of serum glucose were measured before and after administration. For antihypertensive activity, SHR were administrated total MeOH Ex. of chicory once a day for 8 days, and were measured blood pressure on 1st, 3rd, 6th and 8th day. Total MeOH, EtOAc fraction, and BuOH fraction Ex. increased bile secretion in rats, and decreased liver toxicity induced by CCl$_4$ in mouse. Total MeOH, Ex. of chicory roots has antiinflammatory effect, and decreased blood glucose concentration in group 2 and 3 rats. It was revealed not lowering blood pressure significantly in SHR.

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Experimental Study on the Antiinflammatory Activities of Bojeasodok-um subtracted Scrophulariae Radix, Lasiosphaera seu Calvatia, Isatidis Radix added indigo Naturalis, Lithospermi Radix (보제소독음가감방(普濟消毒飮加減方)의 소염작용(消炎作用)에 관한 실험적(實驗的) 연구(硏究))

  • Kim, Sung-Hak;Park, Jong-Hyung;Kim, Kyung-Jum
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.23 no.3
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    • pp.1-10
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    • 2010
  • Objective : Erysipelas is an acute inflammation caused by pyogenic bacteria. This mainly involves the upper part of dermis. It begins as erythematous patches with tenderness, followed by fever, headache, chills and fatigue etc. It may results in edema, obstruction of lymphatics and sepsis. So this experiment is carried out for test whether the Bojeasodok-um subtracted Scrophulariae Radix, Lasiosphaera seu Calvatia, Isatidis Radix added indigo Naturalis, Lithospermi Radix have an anti-inflammatory effect and have suppression effect on immunocyte in the state of inflammation which induced by Erysipelas. Method : Experimental animals made use of 4-5 week-age(weight 20-25g) ICR(male) mouse. In the breeding farm, the lighting time was controlled from 7:00 am till 7:00 pm, the temperature was controlled So we concluded that BS is prospected as an anti-inflammatory agent to cure inflammation induced bywithin 18-23$23^{\circ}C$ and water and food were not limited.The freezing lyophilization powder which were extracted from Bojesodok-Um divided low dose group(200mg/kg-BSL) and high dose group(500mg/kg-BSH) and after melting in water, it was orally administered to the mouse. Compared with inflammation induced group which were induced by triggering-inflammation reagent Carageenan and Zymosan and normal contrast group, we measured the edema decrement effect,macrophage and spleen cell activation. Result : 1. BS has suppress inflammatory reaction induced by Carageenan. 2. BS has suppress increasing activation of abdominal cavity macrophage in the Carageenan and Zymosan induced inflammation. 3. BS has suppress increasing activation of spleen cell in the Carageenan and Zymosan induced inflammation. Based on the above result, BS was improved its suppression effect to the inflammatory reaction through the suppression of spleen cell and macrophage activation. So we concluded that BS is prospected as an anti-inflammatory agent to cure inflammation induced by Erysipelas.

Subacute Toxicity of SKI306X, an Antiinflammatory Herbal Extracts, in Rats (생약복합제 SKI306X의 랫드에 대한 4주 경구 반복투여 독성연구)

  • 김훈택;안재석;정인호;김택수;류근호;임광진;조용백;김대기;김환수
    • Biomolecules & Therapeutics
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    • v.4 no.1
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    • pp.19-31
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    • 1996
  • This study was performed to determine the subacute toxicities of SKI306X, an antiinflammatory herbal extract, in rats. SKI306X was administered orally to rats once a day for 4 weeks at doses of 0.3, 1.0, and 3.0 g/kg/ day. Each group consisted of 20 male and 20 female rats, including 5 male and 5 female rats per group for an interim study at the end of 2-week administration and for a 2-week recovery study, respectively. Throughout the study, all rats survived and no adverse clinical signs were observed. Although male rats treated with high dose (3.0 g/kg/day) of SKI306X showed slight loss of body weight (approximately 5%) in comparison with control animals during the administration period, their body weight loss was normally restored during the recovery period. No significant change was found in all hematological parameters of SKI306X-treated groups except for the decreased number of red blood cells in all female groups at the interim study. Statistically significant changes were observed in several blood enzyme levels of SKI306X-treated groups; however, most of these significant changes were within normal range and statistically significant values did not show dose-related responses. In SKI306X-treated groups, the absolute and relative weights of liver, heart, and stomach were statistically different from those of control group, but these differences disappeared at the end of recovery period and also drug-related gross and histopathological findings in these organs were not found. No other drug-related gross and histopathological findings were observed. It is concluded from the results of this study that non-toxic dose of SKI306X was estimated to be between 0.3 and 1.0 g/kg/day and the maximum tolerated dose of SKI306X was assumed to be higher than 3.0 g/kg/day.

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