Diazaquinomycins E-G, novel diaza-anthracene analogs from a marine-derived Streptomyces sp.
Diazaquinomycins E-G, novel diaza-anthracene analogs from a marine-derived Streptomyces sp.
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DOI：
10.3390/md12063574
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发表时间：
2014-06-11
期刊：
影响因子：
5.4
通讯作者：
Murphy BT
中科院分区：
文献类型：
--
作者：
Mullowney MW;Ó hAinmhire E;Shaikh A;Wei X;Tanouye U;Santarsiero BD;Burdette JE;Murphy BT
作为我们鉴定靶向耐药卵巢癌的新型次级代谢物的计划的一部分，针对顺铂耐药卵巢癌细胞系（OVCAR 5）筛选我们的水生来源的放线菌级分文库导致分离新型二氮杂蒽抗生素二氮喹霉素E（DAQE; 1）、二氮喹霉素F（DAQF; 2）和二氮喹霉素G（DAQG; 3）和已知类似物二氮喹啉霉素A（DAQA; 4）。通过对DAQF和DAQG共晶的X射线衍射数据进行解卷积，确定了DAQF和DAQG的结构。DAQE和DAQA对OVCAR 5的中等LC 50值分别为9.0和8.8 μM。在致死浓度的DAQA，DNA损伤的证据，观察到通过诱导细胞凋亡，通过切割PARP。在此，我们将讨论这些次级代谢产物的分离，结构鉴定和生物活性。
As part of our program to identify novel secondary metabolites that target drug-resistant ovarian cancers, a screening of our aquatic-derived actinomycete fraction library against a cisplatin-resistant ovarian cancer cell line (OVCAR5) led to the isolation of novel diaza-anthracene antibiotic diazaquinomycin E (DAQE; 1), the isomeric mixture of diazaquinomycin F (DAQF; 2) and diazaquinomycin G (DAQG; 3), and known analog diazaquinomycin A (DAQA; 4). The structures of DAQF and DAQG were solved through deconvolution of X-Ray diffraction data of their corresponding co-crystal. DAQE and DAQA exhibited moderate LC50 values against OVCAR5 of 9.0 and 8.8 μM, respectively. At lethal concentrations of DAQA, evidence of DNA damage was observed via induction of apoptosis through cleaved-PARP. Herein, we will discuss the isolation, structure elucidation, and biological activity of these secondary metabolites.
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影响因子：
2.2
作者：
Maskey, RP;Grün-Wollny, I;Laatsch, H
通讯作者：
Laatsch, H
影响因子：
3.3
作者：
MURATA, M;MIYASAKA, T;OMURA, S
通讯作者：
OMURA, S
DOI：
10.1099/ijs.0.019091-0
发表时间：
2011-05-01
影响因子：
2.8
作者：
Shibazaki, Azusa;Omoto, Yuta;Gonoi, Tohru
通讯作者：
Gonoi, Tohru
影响因子：
3.7
作者：
Ó hAinmhire E;Quartuccio SM;Cheng W;Ahmed RA;King SM;Burdette JE
通讯作者：
Burdette JE
DOI：
10.1107/s0907444909047337
发表时间：
2010-02-01
期刊：
ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY
影响因子：
--
作者：
Kabsch, Wolfgang
通讯作者：
Kabsch, Wolfgang