• Title/Summary/Keyword: cyclooxygenase inhibitory activity

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Responsiveness of Muscarinic and Alpha Adrenergic Activation on Endothelial Cell in Isolated Canine Renal Arteries (개 신동맥 내피세포의 무스카린성 및 알파 아드레날린성 수용체에 대한 작용)

  • Chung, Soo-Youn;Chang, Ki-Churl;Lim, Jung-Kyoo
    • The Korean Journal of Pharmacology
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    • v.25 no.1
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    • pp.43-51
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    • 1989
  • Responsiveness of muscarinic and alpha adrenoceptor activation on endothelial cells was studied in isolated canine renal artery rings. Ach (10-100 nM), dose dependently, relaxes endothelial intact rings precontracted with phenylephrine ($IC_{50}$ of Ach was 34.5 nM). Selective mechanical destruction of the endothelium transformed the activity of this substance from vasodilatation to vasoconstriction. Acetylcholine induced relaxations could be selectively inhibited competitively by atropine, but could not be inhibited by cyclooxygenase inhibitor. Methylene blue, however, an inhibitor of soluble guanylate cyclase activity, inhibited Ach as well as sodium nitroprusside (SNP) induced relaxation. Relaxation produced by prostacyclin was not modified by methylene blue. On the other hand, alpha adrenoceptor agonist did not relax but contract canine renal artery rings possessing an intact intima precontracted with U-46619. Clonidine, however, selective alpha-2 adrenergic agonist, is more susceptible than phenylepherine, selective alpha-1 adrenergic agonist, to the inhibitory effect of contraction. These results suggest that in canine renal artery rings, 1) muscarinic receptor is responsible for releasing endothelium dependent relaxation factor (EDRF). 2) alpha-1 and alpha-2 adrenergic receptors are present in canine renal artery. 3) relaxation via EDRF is antagonized by methylene blue, providing further evidence that EDRF acts through a cGMP mechanism.

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Protection of UV-derived Skin Cell Damage and Anti-irritation Effect of Juniperus chinensis Xylem Extract (향나무추출물의 광손상으로부터 피부세포 보호와 자극완화 효과에 대한 연구)

  • 김진화;박성민;심관섭;이범천;표형배
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.30 no.1
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    • pp.63-71
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    • 2004
  • The human skin is constantly exposed to environmental irritants such as ultraviolet, smoke, chemicals. Free radicals and reactive oxygen species (ROS) caused by these environmental facts play critical roles in cellular damage. These irritants are in themselves damaging to the skin structure but they also participate the immensely complex inflammatory reaction. The purpose of this study was to investigate the skin cell protective effect of Juniperus chinensis xylem extract on the UV and SLS-induced skin cell damages. We tested free radical and superoxide scavenging effect in vitro. We found that Juniperus chinensis xylem extracts had potent radical scavenging effect by 98% at 100 $\mu\textrm{g}$/mL. Fluorometric assays of the proteolytic activities of matrix metalloproteinase-l(MMP-1, collagenase) were performed using fluorescent collagen substrates. UV A induced MMP-1 synthesis and activity were analyzed by enzyme-linked immunosorbent assay (ELISA) and gelatin-based zymography in skin fibroblasts. The extract of Juniperus chinensis showed strong inhibitory effect on MMP-1 activities by 97% at 100 $\mu\textrm{g}$/mL and suppressed the UVA induced expression of MMP-1 by 79% at 25 $\mu\textrm{g}$/mL. This extract also showed strong inhibition on MMP-2 activity in UVA irradiated fibroblast by zymography. We also examined anti-inflammatory effects by the determination test of proinflammatory cytokine, interleukin 6 in HaCaT keratinocytes. In this test Juniperus chinensis decreased expression of interleukin 6 about 30%. Expression of prostaglandin E$_2$, (PGE$_2$) after UVB irradiation was measured by competitive enzyme immunoassay (EIA) using PGE$_2$ monoclonal antibody. At the concentrations of 5-50 $\mu\textrm{g}$/mL of the extracts, the production of PGE$_2$ by HaCaT keratinocytes (24 hours after 10 mJ/$\textrm{cm}^2$ UVB irradiation) was significantly inhibited in culture supernatants (p〈0.05). The viability of cultured HaCaT keratinocytes was significantly reduced at the doses of above 10 mJ/$\textrm{cm}^2$ of UVB irradiation, but the presence of these extracts improved cell viability comparing to control after UVB irradiation. We also investigated the protective effect of this extract in sodium lauryl sulfate (SLS)-induced irritant skin reactions from 24 hour exposure. Twice a day application of the extract for reducing local inflammation in human skin was done. Irritant reactions were assessed by various aspects of skin condition, that is, erythema (skin color reflectance) and transepidermal water loss (TEWL). After 5 days the extract was found to reduce SLS-induced skin erythema and improve barrier regeneration when compared to untreated symmetrical test site. In conclusion, our results suggest that Juniperus chinensis can be effectively used for the prevention of UV and SLS-induced adverse skin reactions such as radical production, inflammation and skin cell damage.

Photoprotection and Anti-inflammatory Effects of Chinese Medical Plants (약용식물추출물의 광보호 효과와 항염증 효과 연구)

  • Jin-Hwa, Kim;Sung-Min, Park;Gwan-Sub, Sim;Bum-Chun , Lee;Hyeong-Bae, Pyo
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.30 no.2
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    • pp.227-233
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    • 2004
  • Chronic exposure to solar radiation, particularly ultraviolet (UV) light, causes a variety of adverse reactions on human skin, such as sunburn, photoaging and photocarcinogenesis. Free radicals and reactive oxygen species (ROS) caused by UV exposure or other environmental facts play critical roles in cellular damage. And, repeated-UV irradiation activated the expression of the matrix metalloproteinase (MMP) and induced skin irritation. Therefore, the development of effective and safe photoprotectants that can reduce and improve the skin damage has been required. The purpose of this study was to investigate the photo-protective effect of several chinese medical plants (Juniperus chinensis) on the UV -induced skin cell damages. We tested free radical and superoxide scavenging effect in vitro. Fluorometric assays of the proteolytic activities of MMP-1 (collagenase) were performed using fluorescent collagen substrates. UVA induced MMP-1 synthesis and activity were analyzed by enzyme-linked immunosorbent assay (ELISA) and gelatin-based zymography in skin fibroblasts. We also examined anti-inflammatory effects by the determination test of proinflammatory cytokine, interleukin 6 in HaCaT keratinocytes. Expression of prostaglandin E$_2$ (PGE$_2$) after UVB irradiation was measured by competitive enzyme immunoassay(EIA) using PGE$_2$ monoclonal antibody. In the human skin we tested anti-irritation effect on the SLS-induced damage skin after appling the extract containing emulsion. We found that Juniperus chinensis extract had potent radical scavenging effect by 98% at 100$\mu\textrm{g}$/mL. The extract of Juniperus chinensis showed strong inhibitory effect on MMP-1 activities by 97% at 100 $\mu\textrm{g}$/mL and suppressed the UVA induced expression of MMP-1 by 79% at 25$\mu\textrm{g}$/mL. This extract also showed strong inhibition on MMP-2 activity in UVA irradiated fibroblast by zymography. In the test of proinflammatory cytokines of human keratinocytes Juniperus chinensis extract decreased expression of interleukin 6 about 30%. The amount of PGE$_2$ by HaCaT keratinocytes was significantly increased at the doses of above 10 mJ/$\textrm{cm}^2$ of UVB (p < 0.05). At the concentrations of 3.2-25$\mu\textrm{g}$/mL of this extract, the production of PGE$_2$ by HaCaT keratinocytes (24 h after 10mJ/$\textrm{cm}^2$ UVB irradiation) was significantly inhibited in culture supernatants (p < 0.05). In SLS-induced skin irritation model in vivo, we found to reduce skin erythema and improve barrier recovery after appling Juniperus chinensis extract containing emulsion when compared to irritated non-treated and placebo-treated skin. Our results suggest that Juniperus chinensis extract can be effectively used for the prevention of UV and SLS-induced adverse skin reactions and applied as anti-aging and anti-irritation cosmetics.

Anti-Inflammatory Effect of Wheat Germ Oil on Lipopolysaccharide-stimulated RAW 264.7 Cells and Mouse Ear Edema (LPS로 유도한 RAW 264.7 세포 및 귀부종 동물 모델에 대한 밀배아유의 항염증 효과)

  • Kang, Bo-Kyeong;Kim, Min-Ji;Jeong, Da-Hyun;Kim, Koth-Bong-Woo-Ri;Bae, Nan-Young;Park, Ji-Hye;Park, Sun-Hee;Ahn, Dong-Hyun
    • Microbiology and Biotechnology Letters
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    • v.44 no.3
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    • pp.236-245
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    • 2016
  • This study investigated the anti-inflammatory effects of wheat germ oil (WGO) on RAW 264.7 cells. It was shown that WGO had no cytotoxicity against the treated cells or negative effect on their proliferation. WGO suppressed nitric oxide (NO) secretion considerably and had inhibitory effects on the production of LPS-induced NO and pro-inflammatory cytokines (IL-6, TNF-α, and IL-1β). In particular, the IL-6 and TNF-α inhibition activities were over 90% at 100 μg/ml concentration of the oil. WGO also inhibited the LPS-induced expression of cyclooxygenase-2, inducible nitric oxide synthase, and nuclear factor-kappa B (NF-κB), and reduced the expression of phosphorylated ERK and JNK. Moreover, the croton-oil-induced edema in mouse ears was reduced by WGO, and no mortalities occurred in mice administered 5,000 mg/kg body weight of WGO over a 2-week observation period. In conclusion, these results provide evidence for the anti-inflammatory effect of WGO that likely occurs via modulation of NF-κB and the JNK/ERK MAPK signaling pathway.

Protective effects of quality certified traditional Doenjang in Korea on TNF-α-induced vascular inflammation in human umbilical vein endothelial cells (혈관내피세포에서 TNF-α 자극에 의해 유도되는 혈관염증에 대한 전통식품 품질인증 된장의 효능 평가)

  • Kim, Eun-Ju;Jang, Yeon-Jeong;Kim, So-Young;Choi, Hye-Sun;Park, Shin-Young
    • Food Science and Preservation
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    • v.23 no.3
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    • pp.378-386
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    • 2016
  • Anti-atherogenic effects in tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$)-stimulated human umbilical vein endothelial cells (HUVEC) are involved in the suppression of oxidative stress, cell adhesion molecules, and pro-inflammatory factors. This study investigated the vascular inflammation inhibitory activity of traditional Doenjang plays a key role in the pathogenesis and progression of atherosclerosis. The protective effects of Korean Deonjang was investigated on the expression of cell adhesion molecules (CAMs) in tumor necrosis factor (TNF)-${\alpha}$-induced human umbilical vascular endothelial cells (HUVECs). Deonjang extracts (20, 50, $100{\mu}g/mL$) decreased the expression of 20 ng/mL TNF-${\alpha}$-induced vascular cell adhesion molecule (VCAM)-1 intracellular adhesion molecule (ICAM)-1 proteins, and their corresponding mRNA levels. Nitric oxides (NO) produced by endothlial nitric oxides synthase (eNOS) dilated blood vessels, which had protective effects against platelet and leukocyte adhesion. While TNF-${\alpha}$-induced suppressed the production of nitric oxide in HUVECs, Doenjang restored NO production in HUVECs. In addition, Deonjang reduced the TNF-${\alpha}$-induced expression of inducible NO synthase (iNOS) and cyclooxygenase (COX)-2 mRNA levels. These results suggested that Doenjang can inhibited the production of cell adhesion molecules and inflammatory mediators, which could be a potential candidate for preventing atherosclerosis.

Cytotoxicity of Particulate Matter in Various Human Cells Lines (미세먼지가 다양한 사람 세포주에 미치는 세포 독성)

  • Lee, Ji-Hyeon;Lee, Joo-Yeong;Kim, Mi-Jeong;Kim, Hyeon-Ji;Lee, Sung-Ho;Jeon, Byeong-Gyun
    • Journal of Life Science
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    • v.29 no.6
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    • pp.724-734
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    • 2019
  • The present study investigated the cytotoxicity of particulate matter (PM) derived from car air filter (outdoor PM) and home cleaner filter (indoor PM) in the various human cell lines. Each outdoor and indoor PM were harvested by ethanol extraction method, subsequently sieved with 10 um filter paper, sterilized with autoclave and added to culture media. The half maximal inhibitory concentration ($IC_{50}$) values was significantly (p<0.05) lower in the outdoor PM, compared with indoor PM, and the significantly (p<0.05) higher $IC_{50}$ values were observed in the cancer cell lines (A-549 lung adenocarcinoma and AGS stomach adenocarcinoma), than those of normal MRC-5 fibroblasts and dental papilla tissue derived-mesenchymal stem cells (DSC). After being exposed to $100{\mu}g/ml$ outdoor PM for 7 days, the population doubling time (PDT) was significantly (p<0.05) increased in especially MRC-5 and DSC cell lines, compared with untreated cell lines. Further, the expression of senescence-associated ${\beta}$-galactosidase activity was up-regulated in all the cells exposed to outdoor PM than those of untreated control. Besides, the expression level of inflammation-associated genes, such as cyclooxygenase-2 (COX-2) and interleukin-6 (IL-6) was found to be significantly (p<0.05) increased in the outdoor PM-treated cell lines than those of untreated cell lines. Our results showed that PM induces the cytotoxicity via arrest of cell growth, cell damage and inflammation response.

Effect of Boswellia serrata Extracts on Degenerative Osteoarthritis in vitro and in vivo Models (보스웰리아 추출물의 골관절염 억제 효과 연구)

  • Nam, Da-Eun;Kim, Ok Kyung;Shim, Tae Jin;Kim, Ji Hoon;Lee, Jeongmin
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.43 no.5
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    • pp.631-640
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    • 2014
  • The inhibitory effects of Boswellia serrata (BW) extracts on degenerative osteoarthritis were investigated in primary-cultured rat cartilage cells and a monosodium-iodoacetate (MIA)-induced osteoarthritis rat model. To identify the protective effects of BW extract against $H_2O_2$ ($800{\mu}M$, 2 hr) in vitro, cell survival was measured by MTT assay. Cell survival after $H_2O_2$ treatment was elevated by BW extract at a concentration of $20{\mu}g/mL$. In addition, BW extract treatment significantly reduced and normalized the productions of pro-inflammatory factors, nuclear transcription factor ${\kappa}B$, cyclooxygenase-2, tumor necrosis factor-${\alpha}$, and interleukin-6 at a concentration of $20{\mu}g/mL$. Treatment of chondrocytes with BW extract significantly reduced 5-lipoxygenase activity and production of prostaglandin E2, especially at a concentration of $10{\sim}20{\mu}g/mL$. For the in vivo animal study, osteoarthritis was induced by intra-articular injection of MIA into knee joints of rats. Consumption of a diet containing BW extract (100 and 200 mg/kg) for 35 days significantly inhibited the development and severity of osteoarthritis in rats. To determine the genetic expression of arthritic factors in articular cartilage, real-time PCR was applied to measure matrix metalloproteinases (MMP-3, MMP-9, and MMP-13), collagen type I, collagen type II, and aggrecan, and BW extract had protective effects at a concentration of 200 mg/kg. In conclusion, BW extract was able to inhibit articular cartilage degeneration by preventing extracellular matrix degradation and chondrocyte injury. One can consider that BW extract may be a potential therapeutic treatment for degenerative osteoarthritis.