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RISS 인기검색어
- 검색키워드
- 저자 : Nobutoshi Murakami (검색결과 2 건)
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Total Synthesis, Structure-activity Relationships and Molecular Target of a Cytot
Murakami, Nobutoshi 전남대학교 약품개발연구소 1999 약품개발연구지 Vol.8 No.1
During the course of our investigation searching for new bioactive substances from marine organisms, we isolated an extremely potent cytotoxic polyketide designated callystatin A (1) from the marine sponge Callyspongia truncata and determined its absolute stereostructure by synthetic means. Furthermore, the first total synthesis of 1 was performed to confirm our presented absolute streostructure. In order to create a new anti-tumor lead compound, the structure-activity relationships of 1 using several synthetic analogues have been studied. As a result of evaluating their cytotoxicities, the following crucial factors have been disclosed ; 1) α, β-unsaturated d-lactone moiety is a conclusive pharmacophore ; 2) 5-R configuration, asymmetric center at C-10, and b-hydroxy ketone moiety contribute to affinity to receptor molecule. From the experiment utilizing the fission yeast expressing an NES-GFP-NLS fusion protein, callystatin A (1) was found to inhibit nuclear export signals (NES) dependent transport of proteins from the nucleus to the cytoplasm as well as leptomycin B (2). In addition, 1 was shown to inhibit direct binding between NES and CRM1 through the competitive experiment by use of the biotinylated leptomycin B. [그림]
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Hiroshi Shimoda,Shao-Jie Shan,Junji Tanaka,Azusa Seki,서정욱,Naoki Kasajima,Satoru Tamura,Yan Ke,Nobutoshi Murakami 한국식품영양과학회 2010 Journal of medicinal food Vol.13 No.1
Red ginger (Zingiber officinale var. Rubra) has been prescribed as an analgesic for arthritis pain in Indonesian traditional medicine. The surface color of the rhizome is purple because of the anthocyanidins in its peel. We prepared 40% ethanolic extract from dried red ginger (red ginger extract [RGE]) and evaluated its anti-inflammatory activity using acute and chronic inflammation models. In an acetic acid-induced mouse writhing model, RGE (10–100mg/kg) suppressed both the frequency of writhing and the increase in permeability of abdominal capillaries. On the other hand, continuous treatment with RGE (10mg/kg) significantly (P<.05) suppressed footpad edema in a rat adjuvant arthritis model. To clarify the anti-inflammatory mechanism of RGE, we examined the effect on prostaglandin (PG) and nitric oxide (NO) production from mouse leukemic monocytes (RAW264 cells) stimulated by lipopolysaccharide. RGE (3 and 10μg/mL) significantly (P<.05) suppressed PGE2 production, while it also suppressed NO production at 100μg/mL. After bioassay-guided separation of RGE, we found that [6]-shogaol and gingerdiols suppressed NO production. Red dye fractions presumed to be proanthocyanidins also suppressed NO production at 100μg/mL. Consequently, we found a potent suppressive effect of RGE on acute and chronic inflammation, and inhibition of macrophage activation seems to be involved in this anti-inflammatory effect. [6]-Shogaol, gingerdiols, and proanthocyanidins were identified as constituents that inhibited NO production.
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