• 제목/요약/키워드: natural products

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Structure Activity Relationships of PAF Receptor Binding Antagonists from Natural Products

  • B.H. Han;H.O. Yang;Kim, Y.C.;Y.H. Kang;H.J. Go;D.Y. Suh
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1995년도 춘계학술대회
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    • pp.60-60
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    • 1995
  • 새로운 혈소판 활성화인자 (PAF) 수용체 결합 저해활성 유효성분인 pinusolide ($IC_{50}$/=2.5$\times$$10^{-7}$M)와 arctigenin($IC_{50}$/=5.2$\times$$10^{-6}$M)을 측백엽(Biota orientalis)과 우방자(Arctium lappa)로부터 분리하여 이미 보고한 바 있다. PAF 수용체에 대한 구조활성 상관관계를 규명하고자 또한 용해도가 우수한 강력한 PAF 길항제를 개발하고자 이 길항제들의 유도체들을 다양한 유기화학반응을 이용하여 합성하였고 in vitro PAF receptor binding assay로 그 활성의 강도를 비교 검토하였다. 그 결과, lactone ring 부분은 unsaturated lactone이 saturated lactone보다 활성이 강하였고 ring이 개열되면 활성이 현저히 감소하였다. pinusolide 경우 exocylclic double bond 부분은 sp$^2$구조의 hydrophobic한 유도체가 활성이 강하였으며, methyl ester 부분은 hydrophobic한 유도체가 활성이 강하였다. Arctigenin의 경우 aromatic unit가 hydrophobic할수록 활성이 강하였다.

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임상가를 위한 특집 1 - 충치예방과 관련된 천연물(natural products) 연구의 현황 (Natural Product Research in Dental Caries Prevention)

  • 전재규
    • 대한치과의사협회지
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    • 제50권9호
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    • pp.544-551
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    • 2012
  • Dental caries is a biofilm-related oral disease, and continues to afflict the majority of the world's population. Although fluoride, delivered in various modalities, remains the mainstay for the prevention of caries, additional approaches are required to enhance its effectiveness. Natural products have been used as a major source of innovative and effective therapeutic agents throughout human history, and have shown promise as a source of components for the development of new drugs. In addition. studies using natural products to prevent or treat oral diseases such as dental caries have received a great deal of attention. A number of compounds, such as epicatechin, allicin and sanguinarine, isolated from natural products, have also been investigated for their efficacy against oral microbial pathogens. However, the use of natural products as an anti-caries agent in clinical practice was controversial because of inadequate knowledge concerning their mechanisms of action and chemical characterization. This study focuses on the current knowledge of natural products in dental caries prevention and suggests natural products are importance sources for the prevention of dental caries.

Chemical Genomics with Natural Products

  • Jung, Hye-Jin;Ho, Jeong-Kwon
    • Journal of Microbiology and Biotechnology
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    • 제16권5호
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    • pp.651-660
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    • 2006
  • Natural products are a rich source of biologically active small molecules and a fertile area for lead discovery of new drugs [10, 52]. For instance, 5% of the 1,031 new chemical entities approved as drugs by the US Food and Drug Administration (FDA) were natural products between 1981 and 2002, and another 23% were natural product-derived molecules [53]. These molecules have evolved through millions of years of natural selection to interact with biomolecules in the cells or organisms and offer unrivaled chemical and structural diversity [14, 37]. Nonetheless, a large percentage of nature remains unexplored, in particular, in the marine and microbial environments. Therefore, natural products are still major valuable sources of innovative therapeutic agents for human diseases. However, even when a natural product is found to exhibit biological activity, the cellular target and mode of action of the compound are mostly mysterious. This is also true of many natural products that are currently under clinical trials or have already been approved as clinical drugs [11]. The lack of information on a definitive cellular target for a biologically active natural product prevents the rational design and development of more potent therapeutics. Therefore, there is a great need for new techniques to expedite the rapid identification and validation of cellular targets for biologically active natural products. Chemical genomics is a new integrated research engine toward functional studies of genome and drug discovery [40, 69]. The identification and validation of cellular receptors of biologically active small molecules is one of the key goals of the discipline. This eventually facilitates subsequent rational drug design, and provides valuable information on the receptors in cellular processes. Indeed, several biologically crucial proteins have already been identified as targets for natural products using chemical genomics approach (Table 1). Herein, the representative case studies of chemical genomics using natural products derived from microbes, marine sources, and plants will be introduced.

Analgesic and Hypothermic Activities of Melandrin

  • Lee, Eun-Bang;Cheon, Seon-Ah;Lee, Young-Soon;Chung, Ha-Sook;Woo, Won-Sick
    • Archives of Pharmacal Research
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    • 제18권1호
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    • pp.38-40
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    • 1995
  • melandrin exhibited an analgesic activity as assessed by inhibition of writhing syndromein mice and by pressure method of inflamed paws of arts and inflamed tails of mmice, and showed a hypothermic effect. However, no anti-inflammatory activity was shown.

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