Bioactive Derivatives of Isopropylstilbene from Mutasynthesis and Chemical Synthesis
Bioactive Derivatives of Isopropylstilbene from Mutasynthesis and Chemical Synthesis
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异丙基二苯乙烯的生物活性衍生物的变合成和化学合成
DOI：
10.1002/cbic.201402447
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发表时间：
2014
期刊：
影响因子：
3.2
通讯作者：
H.B. Bode
中科院分区：
文献类型：
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作者：
M. Kronenwerth;A.O. Brachmann;M. Kaiser;H.B. Bode
异丙基二苯乙烯是发光菌TT01的天然产物，具有多种生物活性。构建了一株不能同时产生蒽醌和肉桂酸的突变株，根据紫外检测，得到了干净的背景。将该缺陷型二苯乙烯类化合物用于突变合成实验，得到了新的二苯乙烯类化合物，并对其进行了GC-MS检测。新化合物的结构经详细的MS分析得到确证，然后进行了化学合成；所有天然和合成的化合物对引起热带疾病的原虫进行了抗虫试验。通过诱变合成得到的两个化合物对恰加斯病的病原体克氏锥虫和引起利什曼病的杜氏利什曼原虫显示了最高的活性。
Isopropylstilbene is a natural product fromPhotorhabdus luminescensTT01, with multiple biological activities. A mutant deficient in the production of both anthraquinones and cinnamic acid was constructed, thus giving a clean background according to UV detection. This anthraquinone and stilbene deficient (ASD) mutant was used in mutasynthesis experiments to obtain new stilbene derivatives, which were detected by GC–MS. The structures of the new derivatives were confirmed by detailed MS analysis and then chemically synthesised; all of the natural and synthetic compounds were tested against protozoa that cause tropical diseases. Two compounds obtained by mutasynthesis showed the highest activity againstTrypanosoma cruzi, the causative agent of Chagas disease, andLeishmania donovani, which causes leishmaniasis.
影响因子：
--
作者：
S. Joyce;A. Brachmann;I. Glazer;Lea Lango;Gertrud Schwär;David J. Clarke;H. Bode
通讯作者：
H. Bode
影响因子：
3.2
作者：
Brachmann, Alexander O.;Joyce, Susan A.;Bode, Helge B.
通讯作者：
Bode, Helge B.
影响因子：
6.7
作者：
Feasey, Nick;Wansbrough-Jones, Mark;Solomon, Anthony W.
通讯作者：
Solomon, Anthony W.