Phaeosphamides A and B, Cytotoxic Cyclodecadepsipeptides from the Mangrove-Derived Fungus Phaeosphaeriopsis sp. S296.
Phaeosphamides A and B, Cytotoxic Cyclodecadepsipeptides from the Mangrove-Derived Fungus Phaeosphaeriopsis sp. S296.
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Phaeosphamides A 和 B，来自红树林衍生真菌 Phaeosphaeriopsis sp 的细胞毒性环十肽。
作者：
对源自红树林的真菌Phaeosphaeriopsis sp. S296发酵液进行化学检测，分离得到两种新的环十肽，即phaeosphamides A（1）和B（2），以及一种已知的同系物Sch 217048（3）。新代谢物的结构，包括绝对构型，是在广泛的光谱数据分析、化学转化以及马尔菲法的基础上确定的。结构中的2 - 羟基 - 3 - 甲基戊酸（Hmp）部分和哌可酸（Pip）单元在自然界中很少被发现。有趣的是，化合物1 - 3是首次从Phaeosphaeriopsis属真菌中发现的肽类实例。对所有已鉴定的化合物针对AGS、BEL - 7402、HepG2、B16和BIU87五种肿瘤细胞系的细胞毒性进行了评估。其中，化合物1对这些肿瘤细胞系显示出抑制活性，IC50值在5.14至66.38 μM之间。进一步的机制研究发现，1使AGS细胞阻滞在G2期，并以剂量依赖的方式诱导其凋亡。
Chemical examination of the fermented broth of the mangrove-derived fungus Phaeosphaeriopsis sp. S296 resulted in the isolation of two new cyclodecadepsipeptides, namely phaeosphamides A (1) and B (2), as well as one known congener Sch 217048 (3). The structures of new metabolites, including absolute configurations, were established on the basis of extensive spectroscopic data analyses, chemical conversion, and Marfey’s method. The 2-hydroxy-3-methylpentanoic acid (Hmp) moiety and pipecolic acid (Pip) unit in structures were rarely discovered in nature. Interestingly, compounds 1–3 are examples of peptides discovered from the fungal genus Phaeosphaeriopsis for the first time. All identified compounds were evaluated for their cytotoxicity against five tumor cell lines of AGS, BEL-7402, HepG2, B16, and BIU87. Among them, compound 1 showed inhibitory activities against these tumor cell lines with IC50 values ranging from 5.14 to 66.38 μM. A further mechanistic investigation found that 1 arrested AGS cells in the G2 phase and induced their apoptosis in a dose-dependent manner.
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影响因子：
1.8
作者：
Shin HJ;Rashid MA;Cartner LK;Bokesch HR;Wilson JA;McMahon JB;Gustafson KR
通讯作者：
Gustafson KR
影响因子：
3.3
作者：
Grant C;Rahman F;Piekarz R;Peer C;Frye R;Robey RW;Gardner ER;Figg WD;Bates SE
通讯作者：
Bates SE
影响因子：
3.6
作者：
Hegde, VR;Puar, MS;Patel, M
通讯作者：
Patel, M
影响因子：
4
作者：
Junne, Tina;Wong, Joanne;Hoepfner, Dominic
通讯作者：
Hoepfner, Dominic
DOI：
10.3390/molecules190812368
发表时间：
2014-08-15
期刊：
Molecules (Basel, Switzerland)
影响因子：
--
作者：
Sivanathan S;Scherkenbeck J
通讯作者：
Scherkenbeck J