New diterpene pyrone-type compounds, metarhizins A and B, isolated from entomopathogenic fungus, Metarhizium flavoviride and their inhibitory effects on cellular proliferation

New diterpene pyrone-type compounds, metarhizins A and B, isolated from entomopathogenic fungus, Metarhizium flavoviride and their inhibitory effects on cellular proliferation
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DOI:
10.1016/j.tet.2008.11.014
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发表时间:
2009-01-10
期刊:
影响因子:
2.1
通讯作者:
Oshima, Yoshiteru
Oshima, Yoshiteru
中科院分区:
化学3区
文献类型:
--
作者:
Kikuchi, Haruhisa;Hoshi, Tomoko;Oshima, Yoshiteru

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到目前为止,昆虫病原真菌还没有得到天然产品化学家的广泛研究。在这项研究中,我们从昆虫病原真菌绿僵菌的甲醇提取物中分离得到了新的吡喃酮二萜类化合物,绿僵菌A(1)和绿僵菌B(2)。它们对昆虫和人类癌细胞都表现出了强大的和选择性的抗增殖活性。这些结果表明,Metarhizins A(1)和B(2)可以作为抗癌药物的新型先导化合物和细胞周期调节的探针。为了进一步研究这种抑制活性的结构要求,我们合成了许多Metarhizin衍生物,并评价了它们的抗增殖活性。(C)2008爱思唯尔有限公司。保留所有权利。
To date, entomopathogenic fungi have not been extensively examined by natural product chemists. In this study, we isolated novel pyrone diterpene-type compounds, metarhizins A (1) and B (2), from methanol extracts of entomopathogenic fungus, Metarhizium flavoviride. They showed potent and selective antiproliferative activity against both insect and human cancer cell lines. These results indicate that metarhizins A (1) and B (2) can be used as novel lead compounds for anti-cancer agents and probes for cell cycle regulation. To further investigate the structural requirements for this inhibitory activity, we synthesized many metarhizin derivatives and evaluated their antiproliferative activities. (C) 2008 Elsevier Ltd. All rights reserved.