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首頁(yè)> 美國(guó)衛(wèi)生研究院文獻(xiàn)>Marine Drugs >Potential Chemopreventive Activity of a New Macrolide Antibiotic from a Marine-Derived Micromonospora sp
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Potential Chemopreventive Activity of a New Macrolide Antibiotic from a Marine-Derived Micromonospora sp

機(jī)譯:海洋衍生的Micromonospora sp的一種新的大環(huán)內(nèi)酯類抗生素的潛在化學(xué)預(yù)防活性。

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摘要

Agents capable of inducing phase II enzymes such as quinone reductase 1 (QR1) are known to have the potential of mediating cancer chemopreventive activity. As part of a program to discover novel phase II enzyme-inducing molecules, we identified a marine-derived actinomycete strain (CNJ-878) that exhibited activity with cultured Hepa 1c1c7 cells. Based on this activity, a new macrolide, juvenimicin C (>1), as well as 5-O-α-l-rhamnosyltylactone (>2), were isolated from the culture broth of a Micromonospora sp. Compound >1 enhanced QR1 enzyme activity and glutathione levels by two-fold with CD values of 10.1 and 27.7 μM, respectively. In addition, glutathione reductase and glutathione peroxidase activities were elevated. This is the first reported member of the macrolide class of antibiotics found to mediate these responses.
機(jī)譯:已知能夠誘導(dǎo)II期酶(例如醌還原酶1(QR1))的藥物具有介導(dǎo)癌癥化學(xué)預(yù)防活性的潛力。作為發(fā)現(xiàn)新型II期酶誘導(dǎo)分子程序的一部分,我們鑒定了一種海洋來(lái)源的放線菌菌株(CNJ-878),該菌株對(duì)培養(yǎng)的Hepa 1c1c7細(xì)胞具有活性。基于這種活性,從培養(yǎng)物中分離出了一種新的大環(huán)內(nèi)酯類幼蟲(chóng)素C(> 1 )以及5-O-α-1-鼠李糖基內(nèi)酯(> 2 )。 Micromonospora sp。的肉湯?;衔? 1 將QR1酶活性和谷胱甘肽水平提高了兩倍,CD值分別為10.1和27.7μM。另外,谷胱甘肽還原酶和谷胱甘肽過(guò)氧化物酶活性升高。這是首次發(fā)現(xiàn)大環(huán)內(nèi)酯類抗生素介導(dǎo)這些反應(yīng)。

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