• 제목/요약/키워드: NO production inhibitors

검색결과 125건 처리시간 0.031초

Methanol Extracts of Stewartia koreana Inhibit Cyclooxygenase-2 (COX-2) and Inducible Nitric Oxide Synthase (iNOS) Gene Expression by Blocking NF-κB Transactivation in LPS-activated RAW 264.7 Cells

  • Lee, Tae Hoon;Kwak, Han Bok;Kim, Hong-Hee;Lee, Zang Hee;Chung, Dae Kyun;Baek, Nam-In;Kim, Jiyoung
    • Molecules and Cells
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    • 제23권3호
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    • pp.398-404
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    • 2007
  • Cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) are involved in various pathophysiological processes such as inflammation and carcinogenesis. In a search for inhibitors of COX-2 and iNOS production we found that extracts of Stewartia koreana strongly inhibited NO and $PGE_2$ production in LPS-treated macrophage RAW 264.7 cells. We have now shown that the mRNA and protein levels of iNOS and COX-2 are reduced by the Stewartia koreana extract (SKE). SKE inhibited expression of an NF-${\kappa}B$ reporter gene in response to LPS, and gel mobility shift assays revealed that SKE reduced NF-${\kappa}B$ DNA-binding activity. The extract also inhibited LPS-induced phosphorylation of $I{\kappa}B-{\alpha}$ and nuclear translocation of p65. Administration of the extract reduced the symptoms of arthritis in a collagen-induced arthritic mouse model. These results indicate that Stewartia extracts contain potentially useful agents for preventing and treating inflammatory diseases.

Letrozole, an aromatase inhibitor, improves seminal parameters and hormonal profile in aged endangered Markhoz bucks

  • Rezaei, Ako;Vaziry, Asaad;Farshad, Abbas
    • Animal Bioscience
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    • 제35권11호
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    • pp.1666-1674
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    • 2022
  • Objective: Letrozole, a potent aromatase inhibitor, is known to have the potential to modify male reproductive function by altering sex hormone levels. This study aimed to evaluate the semen and testicular characteristics and hormonal profile of aged Mrakhoz bucks (Capra hircus) treated with letrozole. Methods: Twelve Markhoz male goats, aged between 4.5 to 5.5 years with an average body weight (BW) of 61.05±4.97 kg were used for the study. Animals were randomly divided into two equal groups and subcutaneously received either 0.25 mg/kg BW of letrozole or a control every week for 2 months. The semen collections were performed every 10 days, and blood samples and testicular biometric records were collected at 20 days intervals. Results: Letrozole causes increased testosterone and follicle-stimulating hormone levels, testosterone to estradiol ratio, semen index and reaction time during the period from 20th to 60th days (p<0.05). Furthermore, letrozole-treated bucks had higher semen volume, sperm concentration, and total sperm per ejaculate from 30th to 60th days (p<0.05). However, no differences occurred between the groups in scrotal circumference, relative testicular volume, semen pH, abnormality, acrosome integrity, and membrane integrity of sperm during the study (p>0.05). The serum luteinizing hormone levels, sperm viability, motility, and progressive motility increased, and estradiol levels decreased after 40th to 60th days of letrozole treatment (p<0.05). Conclusion: Letrozole application to aged Markhoz bucks provokes reproductive hormonal axis which, in turn, induces enhancement of semen production and quality.

아마란스 씨앗 추출물의 항염 및 Tyrosinase 억제 효과 (Anti-inflammatory and Tyrosinase Inhibition Effects of Amaranth (Amaranthus spp L.) Seed Extract)

  • 이미란;강창희;부희정
    • 한국자원식물학회지
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    • 제30권2호
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    • pp.144-151
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    • 2017
  • 본 연구는 아마란스(Amaranthus spp L.) 씨앗 추출물의 항염 및 미백과 관련된 효능을 측정함으로써 식품, 의약품 및 화장품 등에 유용한 소재로서 활용할 수 있는 가능성을 확인하고자 수행하였다. 아마란스(Amaranthus spp L.) 씨앗 추출물의 항염증 활성 검색을 위하여 RAW 264.7 세포를 이용하고 실험을 진행하였고, 미백 효능 확인에 대하여서는 mushroom tyrosinase를 사용하였다. RAW 264.7 세포를 이용하여 NO 생성 억제, iNOS 및 COX-2 단백질 발현 억제, 염증매개인자인 $TNF-{\alpha}$$PGE_2$ 생성 억제효과 등을 확인한 결과, 에틸아세테이트 분획물이 NO 생성과 iNOS 발현을 농도 의존적으로 강하게 억제함으로써 iNOS 발현 억제를 통한 NO 생성을 억제함을 확인할 수 있었다. NO와 iNOS 억제 효과보다는 약하지만 $PGE_2$와 COX-2 단백질 발현 역시 농도 의존적으로 억제함으로써 $PGE_2$ 억제 효능이 COX-2의 발현 억제를 통하여 이루어짐을 확인하였다. 또한 염증에 의해 증가되는 아라키돈산 대사물들이 피부 멜라닌 합성의 최초 속도결정단계에 작용하는 tyrosinase 활성을 증가시킨다는 연구 결과에 근거하여 $PGE_2$의 발현을 억제하는 아마란스 EtOAc 분획물이 tyrosinase 효소 억제 활성을 측정하고 미백효능을 확인하였다. Mushroom tyrosinase 활성 억제 효능은 에틸아세테이트 분획물이 우수한 효과를 보였으며, 농도 의존적으로 tyrosinase 효소의 활성을 억제함을 확인할 수 있었다. 이상의 결과들은 향후 아마란스 씨앗의 항염 효능을 갖는 유효성분 탐색 및 멜라닌 세포를 이용하여 미백 관련 연구의 중요한 기초자료로 활용할 수 있을 것이라 사료되며, 아마란스 씨앗이 우수한 영양식품으로 알려져 있는 만큼 안전하면서도 항염과 미백 효능이 있는 소재로서 기능성 식품, 의약품, 화장품 소재로 다양하게 응용할 수 있는 가능성을 확인하였다.

해조류 바이오매스를 이용한 바이오에탄올 생산기술 (Bioethanol Production from Macroalgal Biomass)

  • 라채훈;선우인영;김성구
    • 생명과학회지
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    • 제26권8호
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    • pp.976-982
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    • 2016
  • 해조류는 성장이 빠르고, 낮은 경작지 사용, 높은 이산화탄소 흡수 및 식량자원과 경쟁하지 않는 장점이 있다. 따라서 리그닌이 없는 해조류 사용은 바이오에탄올 생산을 위한 3세대 바이오매스로 주목받고 있다. 산 촉매 열가수분해 전처리법은 해조류로부터 높은 단당을 획득할 수 있는 경제적인 방법 중 하나이다. 고온 전처리 조건들에서 3,6-anhydrogalactoe는 저해물질인 HMF로 전환되는데, 이 저해물질은 세포 성장과 에탄올 생산을 저해한다. 따라서 바이오에탄올을 생산하기 위해 해조류의 탄수화물을 분해할 때는 높은 단당 수율과 낮은 저해물질 생성을 하는 효과적인 전처리 방법이 필요하다. 혼합 당을 이용한 에탄올 발효의 효율을 향상시키기 위해, 고농도 당에 순치한 효모는 혼합 당의 사용을 통해 해조류를 이용한 바이오 에탄올의 생산을 가능하게 한다.

효모에 의한 phenol 성 물질의 자화에 관한 연구 (Studies on the Utilization of Phenolic Substance by Yeast)

  • 김상달;서정훈
    • 한국미생물·생명공학회지
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    • 제6권4호
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    • pp.155-159
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    • 1978
  • 분리된 효모에 의한 aromatic ring compound의 전환반응 실험에 앞서 phenol 자화능에 대한 환경 인자의 영향을 조사하기 위하여 phenol을 유일한 탄소원으로 사용하여 분리된 효모균을 30시간, 3$0^{\circ}C$에서 진탕배양하여 균체증식량을 측정하였다. 1) pH3.5~4.5 온도 35$^{\circ}C$에서 가장 자화능이 우수하였으며 phenol의 처음 농도 1000ppm 까지 는 쉽게 이용할 수 있었고 2000ppm에서는 5 일간 배양시켰을 때 비로소 균체증식이 나타났다. 2) pH 5.0, 배양온도 3$0^{\circ}C$에서 본 균의 maximum specific growth rate는 0.27hr-1 이었으며, phenol 을 1000ppm씩 단계적으로 첨가하면서 phenol 소비율에 대한 균체수율 정수 Y값을 구한 결과 Y=3.2였다. 3) Yeast extract를 필수영양원으로 첨가할 때 0.005~0.01% 농도에서 가장 효과적이었으며, 또 산화환원소 효소 조해제인 HgCl$_2$, phenylhydrazine 을 명명 $10^{-5}$M, $10^{-3}$M을 배지내에 첨가하면 분리된 효모균의 증식을 거의 볼 수 없었다. 4) Phenol의 자화에 명종 실소원의 효과를 비교 해 본 결과 urea가 가장 효과적이었고, 이 효모균은 phenol 외에 catechol, resorcinol, benzidine 을 자화할 수 있다

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가미사물탕(GST)의 사이토카인으로 유도된 인간 섬유아세포양 활막 세포 활성화 저해 작용 (Suppressive Effects of GST on Cytokine-induced Activation of Human Fibroblast-like Sinoviocytes)

  • 박지영;진미림;김동희
    • 혜화의학회지
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    • 제14권2호
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    • pp.45-54
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    • 2005
  • GST, an extract from 16 herbs, has been formulated and prescribed for the treatment of human rheumatoid arthritis(hRA) for many years. The present study was done to investigate whether GST has suppressive effects on activation of fibroblast-like sinoviocytes isolated from an RA patient. In tumor necrosis factor-a(TNF-a)/interleukin-1b(IL-1b) treated human sinoviocytes, The mRNA expression of molecular indicators related to pathologic changes of the sinoviocytes were examined using quantitative real-time PCR. The treatment of GST($100\;{\mu}g/ml$) suppressed the expression of proinflammatory cytokines and chemokines such as TNF-a, IL-1b, IL-6 and IL-8 compared with the control. The mRNA level of intracellular adhesion molecule-1(ICAM-1) which is known to increase in the activated sinoviocytes of RA patients, was slightly decreased by GST. The expression of NOS-II was considerably reduced, which was accompanied by a decrease in the production of nitric oxide(NO). In addition, GST considerably increased the mRNA levels of tissue inhibitors of matrix metalloproteinase-1(TIMP-1), while those of matrix metalloproteinase-3(MMP-3) were decreased. Taken together, these data suggested that GST might suppress the activation of sinoviocytes in hRA.

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Anti-inflammatory effects of a novel compound, MPQP, through the inhibition of IRAK1 signaling pathways in LPS-stimulated RAW 264.7 macrophages

  • Kim, Ba Reum;Cho, Young-Chang;Cho, Sayeon
    • BMB Reports
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    • 제51권6호
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    • pp.308-313
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    • 2018
  • Small-molecule inhibitors are widely used to treat a variety of inflammatory diseases. In this study, we found a novel anti-inflammatory compound, 1-[(2R,4S)-2-methyl-4-(phenylamino)-1,2,3,4-tetrahydroquinolin-1-yl]prop-2-en-1-one (MPQP). It showed strong anti-inflammatory effects in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. These effects were exerted through the inhibition of the production of NO and pro-inflammatory cytokines, such as interleukin (IL)-6, $IL-1{\beta}$, and tumor necrosis $factor-{\alpha}$ ($TNF-{\alpha}$). Furthermore, MPQP decreased the expression levels of inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2). Additionally, it mediated the inhibition of the phosphorylation of p38, c-Jun N-terminal kinase (JNK), the inhibitor of ${\kappa}B{\alpha}$ ($I{\kappa}B{\alpha}$), and their upstream kinases, $I{\kappa}B$ kinase (IKK) ${\alpha}/{\beta}$, mitogen-activated protein kinase kinase (MKK) 3/6, and MKK4. Furthermore, the expression of IL-1 receptor-associated kinase 1 (IRAK1) that regulates $NF-{\kappa}B$, p38, and the JNK signaling pathways, was also increased by MPQP. These results indicate that MPQP regulates the IRAK1-mediated inflammatory signaling pathways by targeting IRAK1 or its upstream factors.

완두 돌연변이체 ageotropum 뿌리의 중력불감성 (Insensitivity of the ageotropum Pea Mutant Roots to Gravity)

  • Kim, Jeong-Im;Bin G. Kang
    • 식물조직배양학회지
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    • 제22권6호
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    • pp.345-350
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    • 1995
  • 완두 돌연변이체 ageotropum 뿌리의 굴중성 결여에 대하여 조사하였다. 정상 완두의 뿌리에서 에틸렌은 굴중성 반응을 억제하였다. 돌연변이체에서는 에틸렌이나 에틸렌 생합성 억제제 또는 작용 억제제 모두 뿌리의 굴중성 반응 결여를 회복시키지 못하였다. 옥신을 비대칭으로 처리한 뿌리에서 굴성반응이 일어나는 것으로 보아 옥신의 작용은 정상적으로 일어나는 것으로 판단되었다. 내생적 또는 옥신유도에 의한 에틸렌 생성은 정상 완두나 돌연변이체에서 크게 차이가 없었다. 그러나 정상 완두에서와는 달리 돌연변이체의 뿌리에서는 굴중성 반응의 작동체계인 옥신작용의 결함이 아니고 중력의 인식 또는 전달과정에 결함이 있다는 결론을 얻었다.

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Antiallergic Effect of Two Variants of Artemisia princeps Pampanini

  • Shin, Yong-Wook;Bae, Eun-Ah;Lee, Bo-Mi;Min, Sung-Won;Lee, Jin-Hee;Baek, Nam-In;Ryu, Su-No;Chung, Hae-Gon;Kim, Nam-Jae;Kim, Dong-Hyun
    • Natural Product Sciences
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    • 제12권2호
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    • pp.67-73
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    • 2006
  • Antiallergic activities of two variants of Artemisia princeps Pampanini SJ-1 (named as Sajabalssuk) and SS-1 (named as Sajuarissuk) cultivated in Ganghwado, which contain high content of eupatilin compared to those cultured by other places, were investigated to evaluate the possibility as inhibitors against allergic diseases. Ethanol and supercritical fluid extracts of SJ-1 and SS-1 inhibited the release of ${\beta}-hexosaminidase$ from RBL-2H3 cells, although their water extracts were inactive. These extracts potently inhibited lipopolysaccharide-induced NO production of RAW264.7. However, these extracts almost did not scavenge free radicals. Oral administration of these extracts to mice inhibited passive cutaneous anaphylaxis reaction induced by IgE, and acute dermatitis induced by 12-O-tetradecanoylphorbol-13-acetate. However, these extracts did not inhibit chronic dermatitis. Scratching behaviors, vascular permeability, and writhing syndromes were weakly inhibited by these extract at a dose of 50 mg/kg. Based on these findings, we believe that SJ-1 and SS-1 can improve IgE-induced allergic diseases such as rhinitis and asthma.

Vasoactive Intestinal Polypeptide Inhibits Pacemaker Activity via the Nitric Oxide-cGMP-Protein Kinase G Pathway in the Interstitial Cells of Cajal of the Murine Small Intestine

  • Kim, Byung Joo;Lee, Jae Hwa;Jun, Jae Yeoul;Chang, In Youb;So, Insuk;Kim, Ki Whan
    • Molecules and Cells
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    • 제21권3호
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    • pp.337-342
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    • 2006
  • Interstitial cells of Cajal (ICCs) are pacemaker cells that activate the periodic spontaneous depolarization (pacemaker potentials) responsible for the production of slow waves in gastrointestinal smooth muscle. The effects of vasoactive intestinal polypeptide (VIP) on the pacemaker potentials in cultured ICCs from murine small intestine were investigated by whole-cell patch-clamp techniques. Addition of VIP (50 nM-$1{\mu}M$) decreased the amplitude of pacemaker potentials and depolarized resting membrane potentials. To examine the type of receptors involved in ICC, we examined the effects of the $VIP_1$ agonist and found that it had no effect on pacemaker potentials. Pretreatment with $VIP_1$ antagonist ($1{\mu}M$) for 10 min also did not block the VIP (50 nM)-induced effects. On the other hand exposure to 1H-(1,2,4)oxadiazolo(4,3-A)quinoxalin-1-one (ODQ, $100{\mu}M$), an inhibitor of guanylate cyclase, prevented VIP inhibition of pacemaker potentials. Similarly KT-5823 ($1{\mu}M$) or RP-8-CPT-cGMPS ($10{\mu}M$), inhibitors of protein kinase G (PKG) blocked the effect of VIP (50 nM) on pacemaker potentials as did N-nitro-L-arginine (L-NA, $100{\mu}M$), a non-selective nitric oxide synthase (NOS) inhibitor. These results imply that the inhibition of pacemaker activity by VIP depends on the NO-cGMP-PKG pathway.