• 제목/요약/키워드: phorbol ester

검색결과 111건 처리시간 0.031초

해조류 및 해양저질에서 항 염증성의 방선균 선발 (Screening Anti-inflammatory Actinomycetes Isolated from Seaweeds and Marine Sediments)

  • 박남희;홍용기;조지영
    • 한국수산과학회지
    • /
    • 제39권4호
    • /
    • pp.333-337
    • /
    • 2006
  • The anti-inflammatory activities of marine actinomycetes were surveyed. In total, 363 strains were isolated from marine sediments, seaweed tissue, and seaweed rhizosphere. Of these, strains 16 and 291-11 showed the most potent anti-inflammatory activity in phorbol-ester-induced mouse ear edema and erythema assays. Strains 16 and 291-11 were isolated from the rhizosphere of the brown seaweeds Sargassum thunbergli and Undaria pinnatifida, respectively, and were identified as Streptomyces macrosporeus and St. praecox, respectively, using 165 rDNA sequence analysis.

Curcumin Inhibits Phorbol Ester-induced Expression of Cyclooxygenase-2 In Vivo through Suppression of Extracelluar Signal-regulated Kinase (ERK) 1/2 and NF-${\kappa}$/B in Mouse Skin

  • Chun, Kyung-Soo;Surh, Young-Joon
    • 대한약학회:학술대회논문집
    • /
    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
    • /
    • pp.322.3-323
    • /
    • 2002
  • Curcumin derived from turmeric (Curcuma longa L.. Zingiberaceae) has been shown to possess marked chemopreventive activities, but the underlying molecular mechanisms remain unclear. In the present work. curcumin was found to inhibit 12-Ο-tetradecanoylphorbol-13-acetate(TPA)-induced expression of cyclooxygenase-2 (COX-2) in female ICr mouse skin as determined by Western and Northern blot analysis as well as immunohistochemical staining. Curcumin treatment atlenuated TPA-stimulated epidermal NF-${\kappa}$B activation. which was associated with its blockade of degradation and phosphorylation of the inhibitory protein l${\kappa}$ Bu and also of subequent translocation of the p65 subunut to nucleus. (omitted)

  • PDF

Anti-inflammatory effect of indole compound, IND-6 in LPS-stimulated RAW 264.7 murine macrophage cell line

  • Park, Young-Mi;Kim, In-Tae;Jung, Jin-Hyun;Mun, Han-Seo;Lee, Kyung-Tae
    • 대한약학회:학술대회논문집
    • /
    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
    • /
    • pp.209.2-210
    • /
    • 2003
  • Nitric oxide (NO) and prostagladins(PGs) produced by inducible nitric oxide synthase(iNOS) and cyclooxygenase(COX-2) are known as inflammatory mediator. Modulation of these enzymes, induced by many stimuli(LPS, IFN-gamma, TNF-alpha, phorbol ester, etc), is a potent strategy as treatment of inflammatory diseases. Treatment of murine macrophage RAW 264.7 cell line with indole compound(IND-6) markedly reduced lipopolysacchride(LPS) stimulated NO production in a concentration-related manner. (omitted)

  • PDF

Conformationally Constrained Analogues of Diacylglycerol Having a Perhydrofuro[3,4-c]furan-1,4-dione Bis-${\gamma}$-butyrolactone Skeleton

  • Lee, Jee-Woo;Nancy-E. Lewin;Peter-M. Blumberg;Victor-E. Marquez
    • Archives of Pharmacal Research
    • /
    • 제21권2호
    • /
    • pp.164-167
    • /
    • 1998
  • Bis-${\gamma}$-lactones (1,2) having a perhydrofuro[3,4-c]furan-1,4-dione skeleton were designed as conformationally constrained diacylglycerol analogues. They were synthesized from D-apiose in 11 steps, and evaluated as $PKC-{\alpha}$ ligands by measuring their ability to displace bound $^3H$]PDBU from the enzyme. The compounds showed moderate binding affinities with $K_i$ values of 13.89 (${\pm}5.67$) ${\mu}M$ and 11.47 (${\pm}0.89$) ${\mu}M$, respectively. Their similar binding affinities indicate that these two bicyclic compounds were not effectively discriminated by $PKC-{\alpha}$ in terms of the direction of the side chain as other ligands built on similar bis-${\gamma}$-lactones.

  • PDF

저농도 및 고농도의 알코올의 투여와 혈관수축성의 조절 (Concentration Dependent Effects of Alcohol on Vasoconstriction)

  • 제현동
    • 약학회지
    • /
    • 제56권3호
    • /
    • pp.180-185
    • /
    • 2012
  • The aim of present study was to investigate the possible influence and related mechanism of alcohol on the arterial contraction. Vascular contraction involves the activation of thick or thin filament pathway. However, there are no reports addressing the question whether this pathway is involved in alcohol-induced regulation. We hypothesized that alcohol plays a role in vascular contraction evoked by a vasoconstrictor in rat aortae regardless of endothelial function. Denuded arterial rings from male rats were used and isometric contractions were recorded using a computerized data acquisition system. Interestingly, alcohol at a low concentration (3% v/v) inhibited thromboxane $A_2$ or phorbol ester-induced contraction with endothelial function but at a high concentration (10%) didn't inhibit and rather increased the contraction in the denuded muscle. Therefore, alcohol at a low concentration decreases the contraction and alcohol at a high concentration increases the contraction suggesting that additional pathways different from endothelial nitric oxide synthesis might be involved in the regulation of contractility. In conclusion, alcohol has some effect on the regulation of contractility regardless of endothelial function.

Cardamonin inhibits agonist-induced vascular contractility via Rho-kinase and MEK inhibition

  • Je, Hyun Dong;Jeong, Ji Hoon
    • The Korean Journal of Physiology and Pharmacology
    • /
    • 제20권1호
    • /
    • pp.69-74
    • /
    • 2016
  • The present study was undertaken to investigate the influence of cardamonin on vascular smooth muscle contractility and to determine the mechanism(s) involved. Denuded aortic rings from male rats were used and isometric contractions were recorded and combined with molecular experiments. Cardamonin significantly relaxed fluoride-, phenylephrine-, and phorbol ester-induced vascular contractions, suggesting that it has an anti-hypertensive effect on agonist-induced vascular contraction regardless of endothelial nitric oxide synthesis. Furthermore, cardamonin significantly inhibited the fluoride-induced increase in pMYPT1 level and phenylephrine-induced increase in pERK1/2 level, suggesting inhibition of Rho-kinase and MEK activity and subsequent phosphorylation of MYPT1 and ERK1/2. This study provides evidence that the relaxing effect of cardamonin on agonist-induced vascular contraction regardless of endothelial function involves inhibition of Rho-kinase and MEK activity.

EFFECTS OF THE SOY ISOFLAVONE GENISTEIN ON COX-2 EXPRESSION AND ACTIVATION OF ERKl/2 INDUCED BY PHORBOL ESTER AND TNF-$\alpha$ IN HUMAN BREAST EPITHELIAL CELL LINE (MCF10A)

  • Chung, Myung-Hoon;Kim, Jung-Hwan;Lee, Seung-Sei;Keum, Joo-Seob;Surh, Young-Joon
    • 한국독성학회:학술대회논문집
    • /
    • 한국독성학회 2001년도 International Symposium on Dietary and Medicinal Antimutgens and Anticarcinogens
    • /
    • pp.135-136
    • /
    • 2001
  • Genistein has been shown to exert propective effects against chemically induced carcinogenesis in animals as well as malignant transformation in cultured cells, but molecular mechanisms of its chemopreventive or chemoprotective activities remain largely unresolved. In the present sturdy, we have investigated the effects of genistein on induction of cyclooxygenase-2 (COX-2) that plays an important role in the pathophysiology of carcinogenesis as well as in cellular response to inflammatory stimuli.(omitted)

  • PDF

Celecoxib inhibits phorbol ester-induced expression of cyclooxygenase-2 and skin-tumor promotion in mouse skin: p38 and AP-1 as possible molecular targets

  • Chun, Kyung-Soo;Park, Kwang-Kyun;Chung, Won-Yoon;Kim, Su-Hyeong;Song, Yong-Sang;Surh, Young-Joon
    • 대한약학회:학술대회논문집
    • /
    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
    • /
    • pp.70.1-70.1
    • /
    • 2003
  • Celecoxib, the selective cyclooxygenase-2 (COX-2) inhibitor, has recently been reported to reduce the formation of polyps in patients with familial adenomatous polyposis. This specific COX-2 inhibitor also protects against experimentally induced carcinogenesis, but molecular mechanisms underlying its chemopreventive activities remain largely unresolved. In the present work, we found that celecoxib inhibited 12-O- tetradecanoylphorbol-13-acetate (TPA)-induced expression of COX-2 in female ICR mouse skin when applied topically 30 min prior to TPA as determined by both immunoblot and immunohistochemical analyses. (omitted)

  • PDF

Inhibitory Effect of Kaempferol on Apoptosis Induced by Phorbol Ester via the Reduction of ROS in Normal Human Dermal Fibroblast

  • Park, Su-Ji;Lee, Sei-Jung
    • 한국환경과학회:학술대회논문집
    • /
    • 한국환경과학회 2020년도 정기학술대회 발표논문집
    • /
    • pp.219-219
    • /
    • 2020
  • Kaempferol (3,4',5,7-tetrahydroxyflavone), a flavonoid found in beans, broccoli, garlic, etc., has been used in natural medicine as an anti-inflammatory and antioxidant. This experiment was carried out to evaluate the anti-apoptotic effect of kaempferol in 12-O-tetradecanoylphorbol 13-acetate (TPA)-treated Normal Human Dermal Fibroblast (NHDF). Kaempferol inhibited the production of intracellular Reactive Oxygen Species (ROS) induced by TPA in NHDF. Kaempferol significantly blocks the phosphorylation of extracellular signal-regulated kinase responsible for the activation of nuclear factor-kappa B. In addition, kaempferol significantly attenuated the expression of Bax and cleaved caspase-3 as regulated by the phosphorylation of nuclear factor-kappa B during its blockage of TPA-induced apoptotic cell death. These findings suggest that kaempferol protects the apoptotic signaling pathway induced by TPA through modulating intracellular ROS in NHDF.

  • PDF

Effect of Chrysin on Gene Expression and Production of MUC5AC Mucin from Cultured Airway Epithelial Cells

  • Shin, Hyun-Dae;Lee, Hyun Jae;Sikder, Asaduzzaman Md.;Park, Su Hyun;Ryu, Jiho;Hong, Jang-Hee;Kim, Ju-Ock;Seok, Jeong Ho;Lee, Choong Jae
    • Tuberculosis and Respiratory Diseases
    • /
    • 제73권4호
    • /
    • pp.204-209
    • /
    • 2012
  • Background: We investigated whether chrysin affected MUC5AC mucin production and gene expression induced by phorbol ester (phorbol 12-myristate 13-acetate, PMA) or epidermal growth factor (EGF) from human airway epithelial cells. Methods: Confluent NCI-H292 cells were pretreated with varying concentrations of chrysin for 30 minutes, and were then stimulated with PMA and EGF for 24 hours, respectively. MUC5AC mucin gene expression and mucin protein production were measured by reverse transcription polymerase chain reaction and enzyme-linked immunosorbent assay. Results: Concentrations of $10{\mu}M$ and $100{\mu}M$ chrysin were found to inhibit the production of MUC5AC mucin protein induced by PMA; A concentration of $100{\mu}M$ chrysin also inhibited the production of MUC5AC mucin protein induced by EGF; $100{\mu}M$ chrysin inhibited the expression of MUC5AC mucin gene induced by PMA or EGF. The cytotoxicity of chrysin was checked by lactate dehydrogenase assay, and there was no cytotoxic effect observed for chrysin. Conclusion: These results suggest that chrysin can inhibit mucin gene expression and the production of mucin protein by directly acting on airway epithelial cells.