• 제목/요약/키워드: I-potent

검색결과 701건 처리시간 0.027초

Synthesis of 2,6-Diaromatic Substituted Pyridine Derivatives and Their Antitumor Activities

  • Moon, Yoon-Soo;Lim, Hyun-Tae;Zhao, Long-Xuan;Basnet-Arjun;Lee, Eung-Seok
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.345.1-345.1
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    • 2002
  • ${\alpha}$-terthienyl the first isolated from natural products shows potent antitumor activity, which encouraged us to study terpyridine and its biological properties. Terpyridine has also been reported as having carcinogenicity, and it's erivatives showed high cytotoxic activities against several human cancer cell lines and topoisomerase I inhibitory ctivity. Mannich free base from condensation reaction was allowed to react with pyridinum salts to give activity. (omitted)

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Isolation and Characterization of Lectins from Stem and Leaves of Korean Mistletoe (Viscum album var. coloratum) by Affinity Chromatography

  • Park, Won-Bong;Han, Seon-Kyu;Lee, Myung-Hwang;Han, Kwang-Ho
    • Archives of Pharmacal Research
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    • 제20권4호
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    • pp.306-312
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    • 1997
  • We attempted to isolate and characterize the lectins from stem and leaves of Korean mistletoe (Viscum album var. coloratum) by affinity chromatography. Lectin I was isolated only from stem. Lectin II was not isolated from Korean mistletoe, whereas lectin III was isolated from the stem and leaves. The hemagglutinating activity of lectin I was 16HU and inhibited by D-galactose, lactose, and N-acetyl-D-galactosamine. The lectin I has molecular weight of 60, 000D being composed of two basic subunits with molecular weights of 32, 000D and 28, 000D which are linked by a disufide bond. The lectin III from stem has molecular weight of 66, 000D being two basic subunits which have molecular weights of 34, 000D and 29, 000D and are linked by a disufide bond. The activity of lectin I was stable at the pH range of 4.00-8.50 and at a wide range of temperature (0-42.deg. C). The lectin I showed more potent mitogenic activity to murine lymphocytes than concanavalin A.

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The Possible Protective Role of Korean Ginseng on Ochratoxicosis: with Special References on Chromosomal Aberrations in Rats.

  • Nada, Spomaia A.;Arbid, Mahmoud S.;Ramadan, A.I.
    • 고려인삼학회:학술대회논문집
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    • 고려인삼학회 1998년도 Advances in Ginseng Research - Proceedings of the 7th International Symposium on Ginseng -
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    • pp.253-262
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    • 1998
  • Ochratoxin A (OA) is a potent mycotoxin causing considerable health hazard and economic loss- e,i. OA is of concern as it is hepato-nephrotoxic, mutagenic, and carcinogenic to a great variety of animals. LDso of crude OA was 8.5 mgf kg.b.w., i.p. The clinical symptoms, mortalities and necropsy were recorded in rats injected with OA (LD5o, i.p.) during 10 days of daily treatment. Ginseng treatments (20 mg 1 kg. b.w., i.p.) : before, mixed with, or after OA dose, completely prevented the mortality in rats. OA-treated animals showed microcytic normochromic anaemia, lucocytosis, hypoproteinaemia and elevation of serum ALT, AST, AP, urea, and creatinine values. These findings were declined near the normal levels when ginseng injected with OA. OA (115 LDso) induced chromosomal aberrations (65.66%) compared to the control. When ginseng given 10 min before OA injection, chromosomal aberrations were reduced to be 31.66% compared to OA-treated animals. In conclusion: ginseng has a protective effect against ochratoxicosis, it has anti-genotoxic activity and it can repair the chromosomal damage induced by ochratoxin A. Key words Ochratoxicosis, Chromosomal aberrations, Mycotoxins, Ochratoxin A, Korean gin sting, Protective effect of Panax ginseng, Rat

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Vanilloid Receptor 1 Agonists, Capsaicin and Resiniferatoxin, Enhance MHC Class I-restricted Viral Antigen Presentation in Virus-infected Dendritic Cells

  • Young-Hee Lee;Sun-A Im;Ji-Wan Kim;Chong-Kil Lee
    • IMMUNE NETWORK
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    • 제16권4호
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    • pp.233-241
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    • 2016
  • DCs, like the sensory neurons, express vanilloid receptor 1 (VR1). Here we demonstrate that the VR1 agonists, capsaicin (CP) and resiniferatoxin (RTX), enhance antiviral CTL responses by increasing MHC class I-restricted viral antigen presentation in dendritic cells (DCs). Bone marrow-derived DCs (BM-DCs) were infected with a recombinant vaccinia virus (VV) expressing OVA (VV-OVA), and then treated with CP or RTX. Both CP and RTX increased MHC class I-restricted presentation of virus-encoded endogenous OVA in BM-DCs. Oral administration of CP or RTX significantly increased MHC class I-restricted OVA presentation by splenic and lymph node DCs in VV-OVA-infected mice, as assessed by directly measuring OVA peptide SIINFEKL-Kb complexes on the cell surface and by performing functional assays using OVA-specific CD8 T cells. Accordingly, oral administration of CP or RTX elicited potent OVA-specific CTL activity in VV-OVA-infected mice. The results from this study demonstrate that VR1 agonists enhance anti-viral CTL responses, as well as a neuro-immune connection in anti-viral immune responses.

마우스 섬유아세포(3T3 fibroblast cells)에서 Insulin-like Growth Factor-I(IGF-I) 및 IGF Binding Protein-3 (IGFBP-3)이 세포증식에 미치는 영향 (The Effect of Insulin-Like Growth Factor-I(IGF-I) and IGF Binding Protein-3(IGFBP-3) on Cellular Proliferation in Mouse 3T3 Fibroblast Cells)

  • 조철호;곽승민;문태훈;조재화;류정선;이홍렬
    • Tuberculosis and Respiratory Diseases
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    • 제47권5호
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    • pp.618-628
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    • 1999
  • 연구배경: 세포성장은 세포증식과 세포죽음의 균형에 의해 이루어 진다. 세포성장에 관여하는 여러 growth factor증 IGF-I은 IGF-IR와 결합하여 세포증식을 유발하는 mitogen으로 알려져 있다. 또한 IGF-I에 결합하는 IGFBPs중에 IGFBP-3는 혈액내에 가장 많은 carrier protein으로, IGF-I과 결합하여 IGF-I의 세포증식 효과를 증가 혹은 억제시킨다. 방 법: 3T3 fibroblast 세포를 이용하여 IGF-I과 IGF-IR transcripts를 northern blot으로 확인하고, IGF-I에 의한 mitogenic effect를 MTT assay 및 $^3H$-thymidine incorporation test로 관찰하고, IGF-I의 receptor인 IGF-IR의 활성화를 보기 위해 intracellular $\beta$-subunit의 tyrosine kinase domain의 phosphorylation을 western blot으로 관찰하였다. 또한 IGFBP-3가 3T3 세포에서 mitogenic effect에 미치는 영향을 보기 위해 anti-IGFBP-3와 ${\alpha}IR_3$을 단독 및 병용투여하여 관찰하였다. 결 과: 3T3 세포는 IGF-I와 IGF-IR의 mRNA expression을 보였으며, IGF-I을 투여시 IGF-IR의 intracelluar cytoplasmic protein인 $\beta$-subunit의 tyrosine kinase domain을 phosphorylation시켜 활성화시키며, 5%, 1% serum-containing media에서 세포증식을 보였으나, serum-free media에서는 세포증식을 보이지 않았다. 또한 anti-IGFBP-3 투여와 ${\alpha}IR_3$과 anti-IGFBP-3를 병용투여시는 세포종식이 각각 2배이상 증가하였으나, ${\alpha}IR_3$을 4시간 전처치후 ${\alpha}IR_3$과 anti-IGFBP-3를 병용투여시는 anti-IGFBP-3에 의한 세포종식이 보이지 않은 것으로 보아 IGF -I/IGFBP-3 결합에서 분리되는 free IGF-I어l 의해 세포증식이 유도된 것으로 생각된다. 결 론: IGF-I은 IGF-IR를 phosphorylation시켜 mitogenic effect를 보이며, IGFBP-3는 IGF-I의 mitogenic effect를 억제하는 것으로 생각된다.

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The Syntehsis and Antimicrobial Activities of Some 1,4-Naphthoquinones (II)

  • Ryu, Chung-Kyu;Kim, Dong-Hyun
    • Archives of Pharmacal Research
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    • 제15권3호
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    • pp.263-268
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    • 1992
  • In order to evaluate the antimicrobial effect of 2, 3-disubstitued-1, 4-naphtoquinone derivatives we newly synthesized several 2-bromo-3-(substituted)-1, 4 naphthoquninones. Amination reaction of 2, 3-dihalo-1, 4 naphthoquinones with aryl and aliphatic amines in ethanol gave 2-halo-3-(N-alkyl or N-aryl)1, 4-naphtoquinone derivatives (1a, b-10a, b) i 60% 90%) yield. These derivatives subjected to antibacterial and antifungal activities. in vitro, against Bacilllus subtilis ATCC 6633 Candida albicans 10231 and local, Psudomonas aeruginosa NCTC10490, Staphylococcus aureus ATCC 6538p. Escherichia coli NIHJ Aspergillus niger KCTC 1231, Tricophyton mentagrophytes KCTC 6085. Among these derivatives 1b, 6b and 7a showed the potent antibacterial activities 1b, 8b and 9b have derivatives, 1b, 6b and 7a showed the potent antibacterial activities. 1b, 8b and 9b have the antifungal activities. 1b is most effective in preventing the growth of Bacillus subtilis and Psudomonas aeruginosa. Candida albicans. Aspergillus niger. Tricophyton mentagrophytes. The several of these compounds demonstrated a broad spectrum of activities in vitro.

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Antagonistic Potential of Native Trichoderma viride Strain against Potent Tea Fungal Pathogens in North East India

  • Naglot, A.;Goswami, S.;Rahman, I.;Shrimali, D.D.;Yadav, Kamlesh K.;Gupta, Vikas K.;Rabha, Aprana Jyoti;Gogoi, H.K.;Veer, Vijay
    • The Plant Pathology Journal
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    • 제31권3호
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    • pp.278-289
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    • 2015
  • Indigenous strains of Trichoderma species isolated from rhizosphere soils of Tea gardens of Assam, north eastern state of India were assessed for in vitro antagonism against two important tea fungal pathogens namely Pestalotia theae and Fusarium solani. A potent antagonist against both tea pathogenic fungi, designated as SDRLIN1, was selected and identified as Trichoderma viride. The strain also showed substantial antifungal activity against five standard phytopathogenic fungi. Culture filtrate collected from stationary growth phase of the antagonist demonstrated a significantly higher degree of inhibitory activity against all the test fungi, demonstrating the presence of an optimal blend of extracellular antifungal metabolites. Moreover, quantitative enzyme assay of exponential and stationary culture filtrates revealed that the activity of cellulase, ${\beta}$-1,3-glucanase, pectinase, and amylase was highest in the exponential phase, whereas the activity of proteases and chitinase was noted highest in the stationary phase. Morphological changes such as hyphal swelling and distortion were also observed in the fungal pathogen grown on potato dextrose agar containing stationary phase culture filtrate. Moreover, the antifungal activity of the filtrate was significantly reduced but not entirely after heat or proteinase K treatment, demonstrating substantial role of certain unknown thermostable antifungal compound(s) in the inhibitory activity.

가감청상방풍탕(加減淸上防風湯)의 항염증 효과에 대한 실험적 연구 (Experimental study of Gagam-Cheongsang BangPungTang on the anti-inflammatory effects)

  • 서은성;황충연;김남권
    • 한방안이비인후피부과학회지
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    • 제21권2호
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    • pp.54-70
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    • 2008
  • Background and Object : This study was carried out to investigate the effects of GCSBPT (Gagam-Cheongsang BangPungTang) on the in vitro and in vivo anti-inflammatory reactions. Methods : Vascular permeability and Cyclooxygenase inhibition assay are examined in vitro and nitric oxide inhibition assay, radical scavenging activity test, $TNF-{\alpha}$, COX-2 inhibition test are examined in vivo. Results : GCSBPT showed inhibitory effects on vascular permeability and leukocyte migration in animal test. In cyclooxygenase 2 inhibition assay, an ethanol extract of GCSBPT inhibited prostaglandin E2 generation at a concentration of $10{\mu}g/ml$. Among the herbal ingredients of GCSBPT, ethanol extracts of Nepetae Spica exhibited potent inhibitory activities. Ethanol extract of GCSBPT inhibited the release of nitric oxide and the gene expression of inducible nitric oxide synthase in RAW 246.7 cells stimulated by lipopolysaccharide. Ethanol extract of GCSBPT exhibited radical scavenging activity of 54% at $100{\mu}g/ml$. Among the herbal ingredients of GCSBPT. Conclusions : According to the above results, I expected that GCSBPT was a potent anti-inflammatory prescription.

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차가버섯으로부터 분리한 페놀성 화합물의 항산화효과 (Antioxidative Activities of Phenolic Compounds Isolated from Inonotus obliquus)

  • 김형자;진창배;이용섭
    • 생약학회지
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    • 제38권2호통권149호
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    • pp.164-169
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    • 2007
  • ln our continued search for biologically active compounds from traditional medicine, we found that ethyl acetate fraction from Inonotus obliquus showed potent antioxidant activities on three different cell-free bioassay systems. Bioassay-directed chromatographic fractionation of the ethyl acetate fraction from Inonotus obliquus afforded four phenolic compounds, 4-(3,4-dihydroxyphenyl)-(E)-3-buten-2-one (1) , 3,4-dihydroxybenzaldehyde (2), protocatechuic acid (3) and caffeic acid (4) along with three sterols such as lanosterol (5), ergosterol peroxide (6) and 9,11-dehydroergosterol peroxide (7). Among isolates, phenolic compounds (1-4) were assessed for antioxidant activities. Almost phenolic compounds showed potent DPPH and superoxide anion radicals scavenging and lipid peroxidation inhibitory activities indicating that these phenolic compounds contribute to the antioxidative activities of I. obliquus. Compounds 2-3 and 7 were isolated for the first time from this plant.

Development of Anti-Melanogenic Agent for Skin Whitening

  • Ahn, Soo-Mi
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 2007년도 Proceedings of The Convention
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    • pp.129-139
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    • 2007
  • Many modalities of treatment for acquired skin hyperpigmentation are available including chemical agents or physical therapies, but none are completely satisfactory. The ideal depigmenting compound should have a potent. rapid and selective bleaching effect on hyperactivated melanocytes, carry no short- or long-term side-effects and lead to a permanent removal of undesired pigment. acting at one or more steps of the pigmentation process. Depigmentation can be achieved by regulating (i) the transcription and activity of tyrosinase, tyrosinase related protein-1 (TRP-1), tyrosinase related protein-2 (TRP-2), and/or peroxidase; (ii) the uptake and distribution of melanosomes in recipient keratinocytes and (iii) melanin and melanosome degradation and turnover of pigmented keratinocytes. One of the interesting point for development of skin whitening agent is Mitf(Microphthalmia-associated transcription factor). Mitf belongs to the basic helix-loop-helix-zip family of trabscription factors and it is crucial as it regulates both melanocyte proliferation as well as melanogenesis and is the major regulator of tyrosinase and the related enzymes (TRPs), as well as many melanosome structural proteins such as pMel17. Recently, we developed MITF-down-regulating agents from natural and synthetic sources, which have anti-melanogenic effect on in vitro and in vivo. We suggested that potent MITF-down regulating agents might be used for skin whitening cosmeceuticals.

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