• Title/Summary/Keyword: ANTI-INFLAMMATORY ACTIVITY

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Metabolic profiling study of ketoprofen-induced toxicity using 1H NMR spectroscopy coupled with multivariate analysis

  • Jung, Jee-Youn;Hwang, Geum-Sook
    • Journal of the Korean Magnetic Resonance Society
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    • v.15 no.1
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    • pp.54-68
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    • 2011
  • $^1H$ nuclear magnetic resonance (NMR) spectroscopy of biological samples has been proven to be an effective and nondestructive approach to probe drug toxicity within an organism. In this study, ketoprofen toxicity was investigated using $^1H$-NMR spectroscopy coupled with multivariate statistical analysis. Histopathologic test of ketoprofen-induced acute gastrointestinal damage in rats demonstrated a significant dose-dependent effect. Furthermore, principal component analysis (PCA) derived from $^1H$-NMR spectra of urinary samples showed clear separation between the vehicle-treated control and ketoprofen-treated groups. Moreover, PCA derived from endogenous metabolite concentrations through targeted profiling revealed a dose-dependent metabolic shift between the vehicle-treated control, low-dose ketoprofen-treated (10 mg/kg body weight), and high-dose ketoprofen-treated (50 mg/kg) groups coinciding with their gastric damage scores after ketoprofen administration. The resultant metabolic profiles demonstrated that the ketoprofen-induced gastric damage exhibited energy metabolism perturbations that increased urinary levels of citrate, cis-aconitate, succinate, and phosphocreatine. In addition, ketoprofen administration induced an enhancement of xenobiotic activity in fatty oxidation, which caused increase levels of N-isovalerylglycine, adipate, phenylacetylglycine, dimethylamine, betaine, hippurate, 3-indoxylsulfate, N,N-dimethylglycine, trimethyl-N-oxide, and glycine. These findings demonstrate that $^1H$-NMR-based urinary metabolic profiling can be used for noninvasive and rapid way to diagnose adverse drug effects and is suitable for explaining the possible biological pathways perturbed by nonsteroidal anti-inflammatory drug toxicity.

Deoxyribonucleic Acid Was Responsible for the Anticoagulatory Effect of an Earthworm, Lumbricus rubellus

  • Paik, Seung-R.;Woo, Jeong-Im;Kim, Gyoung-Mi;Cho, Jin-Mo;Yu, Kyoung-Hee;Chang, Chung-Soon
    • BMB Reports
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    • v.30 no.1
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    • pp.37-40
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    • 1997
  • Earthworm extracts are known for anti-inflammatory, analgesic. antipyretic, and anticancer effects but can also influence blood circulation. It was previously shown that an earthworm, Lumbricus rubelius. contained a water-extractable anticoagulant which was a heat- and acid-stable molecule with hydrophilic property. In order to uncover the biochemical nature of this molecule, the anticoagulant was processed with various hydrolases such as trypsin, DNase, RNase. and lysozome. When the digested samples were analyzed with an in vitro coagulation test measuring activated partial thromboplastin time (APTT) and agarose gel electrophoresis, the anticoagulant proved to be a relatively homogeneous DNA fragment with relative molecular size around 72 base pairs. Interestingly, the activity was further stimulated with a trypsin digestion. RNA. on the other hand, did not prolong the APTT. It was also demonstrated that the DNA accelerated the antithrombin III (AT-III) inhibition of thrombin from $IC_{50}$ of 0.34 to 0.16 unit determined with S-2238 as a substrate, whereas heparin, a popular anticoagulant. shifted the value to 0.05. Therefore, it is suggested that the DNA could be considered as an alternative antithrombotic agent to heparin, which would exhibits bleeding side effects.

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Oleanolic acid regulates NF-κB signaling by suppressing MafK expression in RAW 264.7 cells

  • Hwang, Yu-Jin;Song, Jaewhan;Kim, Haeng-Ran;Hwang, Kyung-A
    • BMB Reports
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    • v.47 no.9
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    • pp.524-529
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    • 2014
  • Oxidative stress and inflammation are common to many pathological conditions. Defense mechanisms protect cells from oxidative stress, but can become over-activated following injury and inflammation. NF-${\kappa}B$ and Nrf2 transcription factors regulate proinflammatory and antioxidant gene expression, respectively. Studies have shown that many natural dietary compounds regulate NF-${\kappa}B$ and Nrf2, preventing inflammation and oxidative stress. Here, we report major compounds of Prunella vulgaris var. lilacina such as rosmarinic acid, oleanolic acid, ursolic acid and caffeic acid as a potential therapeutic for oxidative stress and inflammation. The major compounds exhibited high anti-inflammatory activity, inhibiting NO, PGE2 production, NF-${\kappa}B$ expression and activating Nrf2 expression. In addition, we examined the effect of major compounds on MafK expression. Among the compounds, oleanolic acid significantly decreased MafK expression and MafK-mediated p65 acetylation. These findings suggest that oleanolic acid as NF-${\kappa}B$ inhibitors can potentially be used in therapeutic applications for the treatment of oxidative stress-induced diseases.

In vitro Modulation of Proliferation and Melanization of B16/F10 Melanoma Cells by Quercetin (Quercetin이 B16/F10 멜라닌세포의 중식 및 멜라닌화에 미치는 영향)

  • 천현자;백승화;우원홍;황상구;김춘관;김춘관
    • YAKHAK HOEJI
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    • v.46 no.1
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    • pp.75-80
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    • 2002
  • Quercetin is one of the bioflavonoid compounds and has multiple biological effects such as antioxidant and effective anti-inflammatory agent. Melanin has an important role in protecting human skin from the damaging effects of ultra-violet W) radiation. We studied the effect of quercetin on proliferation of B16/F10 melanoma cells. After 48h treatment of cells with quercetin, the cells exhibited a dose-dependent inhibition in their proliferation without apoptosis. Therefore, the decrease in cell numbers may be due to cell growth arrest, not due to cell death by cytotoxicity. We also investigated the effect of quercetin on melanogenesis of this cells. B16/F10 melanoma cells were grown for 48h in the presence of 0.01~50$\mu\textrm{g}$/ml quercetin and the total melanin contents were measured. Quercetin stimulated melanization of the cells in low concentrations (0.01~20$\mu\textrm{g}$/ml), whereas it inhibited melanization in high concentrations (30~50$\mu\textrm{g}$/ml). It was observed that quercetin differently regulates melanogenesis of B16/F10 melanoma cells dependent on its concentrations.

Anticarcinogenic Activity of Resveratrol, a Major Antioxidant Presnet in Red Wine : Induction of Apoptosis in Human Cancer Cells (적포도의 주 항산화물질, 레스베라트롤의 항암작용: 아폽토시스 의한 인체 암세포 사멸 유도)

  • 허연진;김정환;서효정;공구;서영준
    • Environmental Mutagens and Carcinogens
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    • v.19 no.1
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    • pp.56-62
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    • 1999
  • Resveratrol (3,5,4'-trihydroxy-trans-stilbene) has been considered to be as one of major antioxidants present in grapes responsible for beneficial effects of red wine consumption on coronary heart disease. This triphenolic stilbene has been suggested as a potential cancer chemopreventive agent based on its striking inhiitory effects on diverse cellular events associated with tumor initiation, promotion, and progression. The compound has strong antioxidative and anti-inflammatory activities which amy contribute to its chemopreventive/chemoprotective properties. In the present work, we have found that resveratrol reduces viability and DNA synthesis capability of cultured human promyelocytic leukemia (HL-60) cells. Likewise, the viability of human breast cancer cell line, MCF-7 was reduced by resveratrol treatment. The growth inhibitory and antiproliferative properties of resveratrol appear to be associated with its induction of apoptotic cell death as determined by morphological and ultrastructural changes, agarose gel electrphoretic analysis of internucleosomal DNA fragmentation, and in situ terminal end-labeling of fragmented DNA (TUNEL). This compound also inhibited the phorbol ester-induced expression of cyclooxygenase-2 (COX-2) protein in immortalized human mammary epithelial MCF-10A cells. These results suggest that resveratrol has the promising cancer therapeutic/chemopreventive potential.

EFFECT OF DIETARY GINSENG ON THE ACTIVITIES OF SERUM GLUTAMIC-PYRUVIC AND GLUTAMIC-OXALOACETIC TRANSAMINASES (식이성(食餌性) 인삼(人蔘)이 혈청(血淸) GOT 및 GPT 활성(活性)에 미치는 영향(影響))

  • Kim, Hong-Ki
    • The Journal of Internal Korean Medicine
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    • v.1 no.1
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    • pp.85-91
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    • 1976
  • A chronical intake of Substantial amount of alcohol would disrupt anormal function of liver if not develop liver diseases in relatively short period. In order to out whether ginseng or ginseng plus high protein diet have any protective effects on the liver of chronical alcoholist from developing malfunction enzymatic activities of both glutamic-pyruvic and glutamic-oxaloacetic transaminases were measured on serum of rats maintained with basal low protein diet, basal diet plus 1 percent ginseng and high protein (40%) plus 1 percent ginseng and administered intraperitoneally with a Constant amount of ethanol either periodically or chronically. It was found that, unlike human subject GOT content was exceedingly high and significant difference was found either among treatment or among sexes thus indicating that either ginseng intake or high protein diet plus ginseng has a protective effect on the liver function of ethanol treated rats. From these results, it was suggested that the dietary ginseng might, have a protective effect on the alcohol hepatic disturbance. As one of probable mechanisms for the characteristic pharmacological activity, it was considered that a secondary action of the saponin of the dietary ginseng would result in the anti-inflammatory through the stimulation of de nove synthesis of certain functional proteins in hepatic organs.

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Chemical Constituents from the Bark of Phellodendron amurense and Their Cytotoxic Effects on HL-60 Human Leukemia Cells

  • Li, Wei;Sun, Ya Nan;Yan, Xi Tao;Yang, Seo Young;Choi, Chun Whan;Kim, Eun Ji;Kang, Hee Kyoung;Kim, Young Ho
    • Natural Product Sciences
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    • v.18 no.4
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    • pp.250-253
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    • 2012
  • Phellodendri Cortex, phellodendron bark, has been used as a stomachic for intestinal function control and as an antimicro and anti-inflammatory agent. In this phytochemical study, eight compounds, berberine (1), palmatine (2), syringin (3), (+)-syringaresinol di-O-${\beta}$-D-glucopyranoside (4), salvadoraside (5), citrusin B (6), osmanthuside H (7), and kelampayoside A (8), were isolated from the bark of Phellodendron amurense. Their structures were elucidated by comparing spectroscopic data with reported values. Compounds 1 - 8 were evaluated for cytotoxic activity against HL-60 human promyelocytic leukemia cells in vitro. Among them, compounds 1 and 2 reduced the viability of HL-60 cells significantly, with $IC_{50}$ values of 26.0 and $18.5{\mu}M$, respectively.

악관절 질환 환자에 대한 초기치료의 효과: 상담 및 투약

  • Kim, Yeong-Gyun;Kim, Hyeon-Tae;Kim, In-Su
    • The Journal of the Korean dental association
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    • v.38 no.6 s.373
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    • pp.549-557
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    • 2000
  • ㆍPurpose: This study was performed to investigate the initial conservative treatment for TMD patients using careful counselling and medication prospectively. ㆍMaterials and Methods: Careful counselling and medication were performed in 51 TMD patients and 27 patients had follow-up check 2 months or more. Diagnosis of TMD was based on medical history and, physical and radiographic examination. TMD included masticatory disorder, internal derangement, degenerative joint disease, inflammatory joint disorder. and problems resulting from extrinsic trauma. All patients had chief complaints of TMJ pain, mouth-opening limitation. joint noise, and/or referred pain. We counselled and explained to the patient about the pathogenesis, etiologic factors, diagnosis and treatment plan for abut 10 minutes. We prescribed nonsteroidal anti-inflammatorv analgesic(Somalgen) and amitriptyline 10mg per day for 2 weeks. We informed the patient of the attention sheet and taught self-exercise of jaw. The patient were assessed by answering the questionnaire of subjective evaluation of TMD & maxillofacial pain. Questionnaire of an activity limitation. Questionnaire of a jaw function, and Questionnaire for the evaluation of TMD. ㆍResults: In questionnaire for the evaluation of TMD, 88.5% of 26 patients answered that the treatment was efficacious. 71.4% of 21 patients answered no problem in everyday life. There were significant differences between pretreatment and final follow-up in the evaluation of the subjective pain in the following sections: opening widely, chewing, resting, morning, masticatory muscle, and temporal portion(SAS program, paired T-test, P = 0.05). ㆍConclusions: Considerate counselling and proper medication could be significantly effectve in the initial treatment of TMD.

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The Effects of Pyeongwibunsoeum Extract on Indomethacin-induced Gastric Mucosal lesions (평위분소음의 Indomethacin 유발 위점막 손상에 대한 효과)

  • 백태현
    • The Journal of Korean Medicine
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    • v.24 no.2
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    • pp.94-108
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    • 2003
  • Objectives : This study was carried out to investigate the anti-ulcer effects of Pyeongwibunsoeum extract and Misoprostol on indomethacin-induced gastric mucosal lesions of mice. Methods : Experimental groups were classified into non-treated group, non-administered group, Misoprostol-administered group and Pyeongwibunsoeum-extract-administered group. This study examined the morphological change, distribution of mast cells and apoptic cells, PNA reaction, COX-1, BrdU, NF-B p50, COX-2, IL-2R-, and ICAM-1of gastric mucosa. Results : 1. The hemorrhagic erosion of gastric mucosa was reduced in the Misoprostol-administered and Pyeongwibunsoeum-extract-administered groups. 2. The Misoprostol-administered group and Pyeongwibunsoeum-extract-administered group showed positive reaction on the PNA distribution. 3. The distribution of apoptic cells, activity of NF-B p50, COX-2, IL-2R-, and ICAM-1 decreased in both the Misoprostol-administered group and Pyeongwibunsoeum-extract-administered group. 4. The Misoprostol-administered and Pyeongwibunsoeum-extract-administered groups showed increase on COX-1, BrdU. Conclusions : As the results indicate, hemorrhagic erosion of gastric mucosa were reduced in both the Misoprostol-administeredand Pyeongwibunsoeum-extract-administered groups, and severe inflammatory reaction of gastric mucosa was reduced. The effects on the Pyeongwibunsoeum-extract-administered group were superior to those on the Misoprostol-administered group. Pyeongwibunsoeum extract can be widely administered for gastric ulcer disease in clinical treatments.

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Effect of the Geijibokryunghwan on human hepatocarcinoma cells

  • Lee Soo Kyung;Kim Han Geu;Ahan Jong Chan;Chung Tae Wook;Moon Jin Young;Park Sun Dong;Kim June Ki;Choi Dall Yeong;Kim Cherl Ho;Park Won Hwan
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.17 no.2
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    • pp.568-573
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    • 2003
  • We invesgated the GBH water extracts can be used as a potential cancer chemopreventive agent in humans, especially in hepatological cancer cell lines. The GBH was found to act as an potent inhibitor of COX-I only, but not as COX-2 inhibitor. Furthermore, the extract mediated anti-inflammatory effects and inhibited COX-associated hydroperoxidase functions(antipromotion activity). Inhibitory effect of the GBH water extracts on the growth of cancer cell lines such as HepG2 cell and Hep3B cell was shown.