Sinularamides A-G, Terpenoid-Derived Spermidine and Spermine Conjugates with Casitas B-Lineage Lymphoma Proto-Oncogene B (Cbl-b) Inhibitory Activities from a Sinularia sp. Soft Coral.

Sinularamides A-G, Terpenoid-Derived Spermidine and Spermine Conjugates with Casitas B-Lineage Lymphoma Proto-Oncogene B (Cbl-b) Inhibitory Activities from a Sinularia sp. Soft Coral.
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DOI:
10.1021/acs.jnatprod.1c00367
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发表时间:
2021-06-25
影响因子:
5.1
通讯作者:
Gustafson, Kirk R.
Gustafson, Kirk R.
中科院分区:
生物学2区
文献类型:
--
作者:
Jiang, Wei;Wang, Dongdong;Wilson, Brice A. P.;Voeller, Donna;Bokesch, Heidi R.;Smith, Emily A.;Lipkowitz, Stanley;O'Keefe, Barry R.;Gustafson, Kirk R.

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一种Sinularia sp.软珊瑚的提取物显示出对E3-泛素连接酶Casitas B系淋巴瘤原癌基因B(Cbl-B)的抑制活性。随后的生物测定引导的提取物分离提供了一系列萜类衍生的亚精胺和精胺酰胺,命名为sinularamides A-G(1-7)。化合物1-7代表新的天然产物;然而,sinularamide A(1)先前被报道为合成的最终产物。通过NMR、IR和HRESIMS的光谱和光谱数据分析并与文献数据比较,确定了Sinularamides A-G(1-7)的结构。所有分离的化合物均显示出Cbl-b抑制活性,IC 50值范围约为6.5至33 μM。
An extract of a Sinularia sp. soft coral showed inhibitory activity against the E3-ubiquitin ligase casitas B-lineage lymphoma proto-oncogene B (Cbl-b). Subsequent bioassay-guided separation of the extract provided a series of terpenoid-derived spermidine and spermine amides that were named sinularamides A–G (1–7). Compounds 1–7 represent new natural products; however, sinularamide A (1) was previously reported as a synthetic end product. The structures of sinularamides A–G (1–7) were elucidated by analysis of spectroscopic and spectrometric data from NMR, IR, and HRESIMS experiments and by comparison with literature data. All of the isolated compounds showed Cbl-b inhibitory activities with IC50 values that ranged from approximately 6.5 to 33 μM.
实体瘤表达的自抗原不会有效刺激天真或活化的T细胞:对免疫疗法的影响。
DOI: 10.1084/jem.186.5.645
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