• 제목/요약/키워드: indomethacin

검색결과 547건 처리시간 0.024초

청훈화담탕가형개로 인해 변동된 국소뇌혈류량 및 평균혈압의 작용기전 (Mechanism on the Changed-Regional Cerebral Blood Flow and Mean Arterial Blood Pressure by CheonghunHwadam-tang Adding Schiznepetae Herba in Rats)

  • 민병일;임광모;정현우
    • 동의생리병리학회지
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    • 제16권4호
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    • pp.701-706
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    • 2002
  • CheonghunHwadam-tang(CHT) have been used in oriental medicine for many centuries as a therapeutic agent of vertigo by wind, fire and phlegm. CHTS was CHT adding Schizonepetae Herba. The effects of CHTS on the cerebral blood flow and blood pressure is not known. The purpose of this Study was to investigate effects of CHTS on the regional cerebral blood flow(rCBF) and mean arterial blood pressure(BP), action-mechanism of CHTS-induced changed-rCBF and BP. The changes of rCBF and BP was determinated by Laser-Doppler Flowmetry(LDF). The results were as follows ; CHTS extract was increased significantly rCBF in a dose-dependent, but was not changed BP compared with CHTS non-treated group. Pretreatment with propranolol, indomethacin and methylene blue were inhibited CHTS induced increase of rCBF, propranolol(all CHTS-treated group) and indomethacin(CHTS 0.01 mg/kg) of them were significantly decreased. Pretreatment with propranonol and indomethacin were inhibited CHTS induced increase of BP, but pretreated with methylene blue was significantly accelerated BP in high dosage. This results suggest that CHTS increased rCBF by dilating pial arterial diameter and the action of CHTS is also mediated by adrenergic β -receptor and cyclooxygenase.

Witepsol 중공좌제로부터의 염산프로프라놀롤 및 인도메타신의 방출제어 (Controlled Release of Propranolol Hydrochloride and Indomethacin from Hollow Type Suppository Using Witepsol H-15)

  • 진숙영;구영순
    • 약학회지
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    • 제40권4호
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    • pp.400-410
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    • 1996
  • In oder to develop the controlled release of drugs from the suppositories, in vitro drug release and in vivo absorption in rabbits were investigated. Various suppo sitory forms with hollow cavities, into which drugs in the form of fine powder or solid dispersion system(SDS) could be placed, were utilized. The oleaginous Witepsol H-15 (WH-15) as a base, and indomethacin (IDM) of a very slightly soluble drug and propranolol-HCL (PPH) of a very soluble drug were employed as model drugs. The in vitro drug release showed that the cumulative release amount of PPH from PPH-(methylcellulose) MC-SDS and PPH-(ethylcellulose) EC-SDS hollow type suppositories reached 40% and 12% in 6 hrs,respectively. On the other hand, the drug release for a conventional suppository was 80% in 6 hrs. For the IDM suppositories,the cumulative drug release from IDM-(polyvinylpyrrolidone) PVP-SDS hollow type suppositories reached 99% in 24 hrs, whereas that from a conventional suppository reached 85%. An in vivo experiment with rabbits showed that IDM-PVP-SDS hollow type suppository delayed the absorption of IDM, significantly. The $t_{max},\;C_{max}\;and\;AUC_{0{\to}8}$ of IDM-PVP-SDS suppository were 60 min, 12.12${\mu}g$/ml and 2657${\mu}g$/ml/min, respectively. The $t_{max},\;C_{max}\;and\;AUC_{0{\to}8}$ of controlled group were 20 min, 15.49${\mu}g$/ml and 2190${\mu}g$/ml/min, respectively.

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건보단(健步丹)이 MIA로 유도된 골관절염 Rat에 미치는 영향 (Effects of Keonbodan (健步丹) on MIA-Induced Osteoarthritis in Rat)

  • 이은정;오민석
    • 한방재활의학과학회지
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    • 제24권2호
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    • pp.51-64
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    • 2014
  • Objectives This study was carried out to know the effects of Keonbodan (hereinafter referred to KBD) in osteoarthritis induced by Monosodium iodoacetate(hereinafter referred to MIA) on Wistar rat. Methods Osteoarthritis was induced by injection of MIA into left knee joint cavities of rat. Osteoarthritis rats were divided into 4 groups (normal (n=6), control (n=6), indomethacin (n=6), KBD (n=6) group). The control group was administered normal saline and indomethacin group was administered indomethacin (2 mg/kg). And the KBD group was administered KBD (142 mg/kg). Each groups were administered by orally for 4 weeks. This experiment were carried out in vivo. In vivo, at the end of the experiment (5 weeks after MIA injection), effects on hepatotoxicity and nephrotoxicity, cytokines in serum, arachidonic acid, osteocalcin, MMP-9, TIMP-1 and cartilage volume were evaluated. And histopathological examinations on the articular structures of knee joints were performed. Results 1. In weight-bearing measurement, level of weight was increased. 2. In order to hepatotoxicity and nephrotoxicity, ALT, AST, BUN and creatinine were tested. And there were no significant changes. 3. In serum, levels of TNF-$\alpha$, IL-$1{\beta}$ were significantly decreased. IL-6 was insignificantly decreased. 4. In serum, level of MMP-9 and TIMP-1 was decreased. 5. In serum, level of $LTB_4$, $PGE_2$ and osteocalcin was decreased. 6. In ${\mu}$CT-arthrography, the cartilage volume was greater than that of the control group. 7. The joint damage induced by osteoarthritis was lesser than the control group in histopathologic observation (H&E, Safranin-O staining). Conclusions These results demonstrated that KBD suppressed the osteoarthritis- inducing effects of MIA in rat. And further studies are required to find out more effective substance and anti-osteoarthritic mechanism in the future.

타히보 추출물의 흰쥐 위액 분비 및 위 손상에 미치는 영향 (The Effects of Taheebo Extracts on Gastric Secretion and Gastric Injury in Rats)

  • 서광희
    • 한국식품영양학회지
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    • 제10권3호
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    • pp.394-400
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    • 1997
  • Taheebo의 물 추출물 및 methanol 추출물이 위액 분비 및 위염, 위궤양에 미치는 영향에 대하여 검토한 바, 다음가 같은 결과를 얻었다. 1. Shay 기초위액 분비에 대하여 Taheebo methanol 추출물은 위액 분비량 감소, pH의 증가, 산도의 감소를 가져왔다. 2. 염산.aspirin 유발 위염에 대하여 Taheebo 물 추출물 1,000mg/kg의 투여는 위점막 손상을 유의적으로 억제하였다. 3. 염산.ethanol 유발 위염에 대하여 Taheebo 물 추출물과 methanol 추출물 모두 위손상지수가 유의적으로 감소하여, 뚜렷한 억제효과를 보였고, 이는 용량 의존적으로 나타났다. 4. Indomethacin으로 유발시킨 위궤양에 대하여는 Taheebo 물 추출물 1,000mg/kg 투여시에만 유의적인 억제효과를 나타내었다. 5. 구속수침 스트레스 유발 위궤양에 대하여 Taheebo 물 추출물 및 methanol 추출물 모두에게 유의적으로 궤양지수를 감소시켜 탁월한 억제효과를 보였다. 이상의 결과로 볼 때, Taheebo는 흰쥐의 위염 및 위궤양에 유효하다는 것을 인정할 수 있었다.

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치은 Arachidonic acid 대사산물의 억제약물에 관한 실험적 연구 (EFFECTS OF INHIBITORY DRUGS ON THE ARACHIDONIC ACID METABOLISM OF PERIODONTAL TISSUE)

  • 한세희;오귀옥;김형섭
    • Journal of Periodontal and Implant Science
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    • 제23권2호
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    • pp.243-259
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    • 1993
  • The bone resorbing activity of $PGE_2$ and elevated level of prostaglandins(PGs) and thromboxanes (TXs) in inflamed gingiva which are cyclooxygenase(C) metabolites have been well documented. Nonsteroidal anti-inflammatory drugs(NSAIDs) have been known to suppress gingival inflammation and bone resorption through the specific inhibitory action on the C pathway thereby decrease of various C metabolites. Recent studies provide unequivocal results that gingival tissue metabolizes arachidonic acid(AA) mainly through lipoxygenase(L) pathway. And the results of our previous experiments suggest that indomethacin may have inhibitory action on L as well as C. Thus we started this study to show the influences of several C inhibitors on the L activity at therapeutic and toxic dosage. Periodontal tissue samples were obtained from patients with advanced periodontitis and incubated with $^{14}C-AA(0.2{\mu}Ci)$ and various enzyme inhibitors. The tissue lipid extracts were separated by means of thin layer chromatography(TLC) and analyzed by means of autoradiography and TLC analyzer. Our results showed that aspirin inhibited C more selectively than L, however at higher concentration it also decreased HETEs production significantly. Indomethacin showed dose-dependent inhibition of L as well as C and all of the L metabolites were decreased to the same degree by high concentration of indomethacin. AA-861, which is an experimental tool of selective L inhibitor, showed inhibition of HETEs production but no effect on the production of $TXB_2$, PGs and $LTB_4$. Various propionic acid derivatives NSAIDs(ibuprofen, flurbiprofen, naproxen) showed the same patterns of effect on AA metabolism each other that was profound inhibition of PGs production, to the less degree HETEs and $TXB_2$ production, and of no effect on the $LTB_4$ production.

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봉독약침이 흰쥐의 국소뇌혈류량 및 평균혈압에 미치는 영향 (Effects of Bee Venom Extract Pharmacopuncture on the Regional Cerebral Blood Flow and Mean Blood Pressure in Rats)

  • 민선정;염승룡;권영달
    • 한방재활의학과학회지
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    • 제23권3호
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    • pp.37-44
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    • 2013
  • Objectives The present study was designed to investigate the effects of bee venom extract pharmacopunctureon (BVP) at 肩井 (GB21) on the changes in regional cerebral blood flow (rCBF) and mean arterial blood pressure (MABP) in normal rats, and further to determine the mechanisms. Methods We purchased rats about 300g and prepared diluted BVP with normal saline. And we injected diluted BVP to rats gradually progressed from 0.001 mg/kg to 0.1 mg/kg at corresponding region to GB21. After injection, we measured the changes in rCBF and MABP of rats. In addition, to determine the mechanisms of this changes, we did the same experiments twice more after pretreatment with indomethacin and metylene blue separately. Results BVP significantly increased rCBF but decreased MABP, suggesting that BVP potently may increase rCBF by dilating pial arterial diameter. Furthermore, the increase of BVP-induced rCBF and the decrease of BVP-induced MABP were significantly blocked by pretreatment with cyclooxygenase inhibitor, indomethacin (1 mg/kg, i.p.). But the increase of BVP-induced rCBF and the decrease of BVP-induced MABP were not blocked by pretreatment with guanylate cyclase inhibitor, methylene blue (0.01 mg/kg, i.p.). Conclusions These findings indicate that the action of BVP is mediated by cyclooxygenase. Furthermore these results suggest that BVP can increase rCBF in normal state, as well as improve the stability of rCBF in ischemic state.

Prostaglandins Involving in Blastocyst Development through Calcium Mediated Signaling Pathway

  • Lee, Ja-Myong;Kwon, Hyuck-Chan;Lee, Seung-Jea;Cheon, Yong-Pil
    • 한국발생생물학회지:발생과생식
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    • 제15권1호
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    • pp.17-24
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    • 2011
  • Lipid metabolites involved in cellular regulation as signaling mediators. Prostaglandins (PGs), metabolites of lipid are involved to pregnancy at the time of implantation but the functional roles of PGs on embryo development are still controversy and largely unknown. In previous report, the levels of $PGE_2$ and $PGF_{2a}$ at embryos of morula stage and blastocyst stage were explored (Cheon et al., 1998). In this study, the previous suggestion was confirmed and the possible downstream mediator of prostaglandin $E_2$ and prostaglandin $F_{2a}$ on the expansion and hatching of mouse embryo was examined. As expected, developmental rate of the blastocyst to expanded stage was a concentration-response curve that showed the highest expansion rate at 10 ${\mu}M$ $PGE_2$, but at 100 ${\mu}M$ $PGE_2$, the rate was decreased. In contrast to the $PGE_2$, $PGF_{2a}$ stimulated expansion without toxicity at highest concentration. Cotreatment of PGs with indomethacin overcame the inhibitory effects of indomethacin in expansion. Exogenous PGs also improved the development of expanded embryos to the hatching stage. Besides, PGs receptors' transcripts detected at blastocyst. $PGE_2$ was caused of calcium fluctuation in the blastocyst but $PGF_{2a}$ did not. The changes of intracellular calcium concentration were different between indomethacin pretreated embryos and non-treated embryos. Based on these results it is suggested that PGs work as paracrine and/or autocrine factors through calcium and the others which were not identified in this study.

자음건비탕이 국소뇌혈류량, 평균혈압, 심근수축력에 미치는 작용기전 (Mechanism of Jaeumgenby-tang on the Regional Cerebral Blood Flow, Mean Arterial Blood Pressure and Cardiac Muscle Contractile Force in Rats)

  • 정현우;김희성;양기호
    • 동의생리병리학회지
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    • 제16권3호
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    • pp.507-513
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    • 2002
  • Jaeumgenby-tang(JGT) have been used in oriental medicine for many centries as a a therapeutic agent of vertigo caused by deficiency of qi and blood. The effects of JGT on the regional cerebral blood flow(rCBF), mean arterial blood pressure(MABP) and cardiac muscle contractile force(CMF) is not known. The purpose of this Study was to investigate effects of JGT on the rCBF, MABP, CMF and mechanism of JGT induced changed rCBF, MABP, CMF. The changes of rCBF, MABP and CMF were determinated by Laser-Doppler Flowmetry(LDF). The results were as follows; JGT extract was increased rCBF, MABP and CMF in a dose-dependent, specially JGT extract was significantly increased rCBF and MABP. Pretreatment with propranolol was significantly inhibited JGT induced increase of rCBF but pretreatment with indomethacin and methylene blue were accelerated JGT induced increase of rCBF. Pretreatment with propranolol and indomethacin were inhibited JGT induced increase of MABP, but pretreatment with methylene blue was accelerated JGT induced increase of MABP. Pretreatment with propranolol was significantly inhibited JGT induced increase of CMF but pretreatment with indomethacin and methylene blue were accelerated JGT induced increase of CMF. This results suggest that JGT increased rCBF by increasing MABP and CMF and the action of JGT is mediated by adrenergic β-receptor.

Inhibitory Action of Ulmus Davidiana Planch Extract Solution to Osteoclast Cell Proliferation and Prostaglandin E2 Synthesis in Mice

  • Park, Sang-Dong;Kim, Kap-Sung;Cho, Hyun-Seok;Lee, Seung-Deok;Kim, Kyung-Ho
    • Journal of Acupuncture Research
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    • 제23권2호
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    • pp.91-102
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    • 2006
  • Objectives : Ulmus davidiana Planch (UD) has long been known to have anti-inflammatory and protective effects on damaged tissue, inflammation and bone among other functions. Methods : This study was undertaken to address whether the water extract of the bark of UD could modulate proliferation of mouse osteoclasts in vitro and to investigate its effect on cyclooxygenase-2 (COX-2), which converts arachidonic acid to prostaglandin E2 (PGE2) and is highly expressed in osteoclasts. Mouse osteoclasts were tested in vitro for growth inhibition, proliferation cell nuclear antigen expression, and COX-2 activity and expression after treatment with UD extract. Results : Its effects were compared with those of indomethacin (a nonselective COX inhibitor) and celecoxib (a selective COX-2 inhibitor) by Cell viability assay, Cell cycle analysis, Immunohistochemical analysis of PCNA expression, Western blot analysis and PGE2 Enzyme immunoassay (EIA). UD demonstrated a strong growth inhibitory action in both tested osteoclasts cells. The IC50s were $10\;{\mu}g/ml$ for UD, $6\;{\mu}M$ for celecoxib and $42\;{\mu}M$ for indomethacin. UD, as well as celecoxib and indomethacin, suppressed proliferation cell nuclear antigen expression and PGE2 synthesis in osteoclasts. UD inhibited COX-2 expression, whereas celecoxib inhibited COX-2 activity directly. Conclusion : UD selectively and effectively inhibits osteoclasts cell growth in vitro. Inhibitory action of PGE2 synthesis via suppression of COX-2 expression may be responsible for its anti-inflammatory activity.

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Collagenase로 유발된 동물모델에서 ChondroT의 진통효과에 관한 연구 (Analgesic Effects of ChondroT in Collagenase-induced Osteoarthritis Rat Model)

  • 원정윤;정지원;나창수;김선종
    • 한방재활의학과학회지
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    • 제26권3호
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    • pp.17-30
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    • 2016
  • Objectives The purpose of this study was to find out the effects of ChondroT on arthralgia of the Collagenase-induced osteoarthritis in rats. Methods Osteoarthritis was induced into rat by injecting Collagenase in its knee joint. Rats are divided into a total of 8 groups (n=6). Normal group was not induced for osteoarthritis whereas control groups were induced for osteoarthritis by Collagenase. Positive-A (Indomethacin) was injected with Collagenase and after 8 days, 2 mg/kg of Indomethacin was medicated. Positive-B (JOINS TAB) was injected with Collagenase and after 8 days, 20 mg/kg of JOINS TAB was medicated. Experimental groups (Chondro T) at three dose levels (50, 100 and 200 mg/kg) were injected with Collagenase and after 8days they were medicated with 10 ml/kg. Indomethacin, JOINS TAB and ChondroT were medicated each substances once a day for 10 days. Thereafter, the changes in plantar withdrawal response of osteoarthritis rats by dynamic plantar aesthesiometer were observed and then RT-PCR analysis was done to investigate the expression of related proteins. Results 1. ChondroT significantly decreased withdrawal response of mechanical allodynia compared with control group in all of the experimental groups (ChondroT-A, ChondroT-B, ChondroT-C). 2. ChondroT significantly reduced Bax/Bcl-2 ratio in all of the experimental groups (ChondroT-A, ChondroT-B, ChondroT-C). 3. ChondroT significantly reduced the expression of INF-${\gamma}$ compared with control group in group ChondroT-B, ChondroT-C. Conclusions This results suggest that ChondroT may be meaningful for suppressing the pain of osteoarthritis. Further study is needed to conduct a rigorous clinical research.