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新格里斯酚A,一种来自新记录真菌的潜在卵巢癌抑制剂。

Neogrisphenol A, a Potential Ovarian Cancer Inhibitor from a New Record Fungus .

作者信息

Zhang Li-Juan, Yang Ming-Fei, Ma Jian, Xiao Xing-Juan, Ma Xiao-Yan, Zheng De-Ge, Han Mei-Yan, Xia Ming-Lei, Jayawardena Ruvishika S, Mapook Ausana, Xiao Yuan-Pin, Kang Ji-Chuan, Lu Yong-Zhong

机构信息

School of Food and Pharmaceutical Engineering, Guizhou Institute of Technology, Guiyang 550003, China.

Center of Excellence in Fungal Research, Mae Fah Luang University, Chiang Rai 57100, Thailand.

出版信息

Metabolites. 2023 Mar 16;13(3):435. doi: 10.3390/metabo13030435.

Abstract

From the rice fermentation product of a new record fungus, , two new polyketides, neogrisphenol A () and neogrisphenol B (), one new isochroman-1-one, ()-6-hydroxy-7-methoxy-3,5-dimethylisochroman-1-one (), and four known compounds (-) were isolated. Their structures were determined using 1D- and 2D-NMR, mass spectrometry, and chemical calculations. The C-3~C-2' polymerization mode between the two -naphthalenone derivative moieties is uncommon in compounds and . Meanwhile, compounds - and exhibited antibacterial activity against , , , and , with MIC values ranging between 16 and 31 µg/mL. In addition, compound showed antifungal activity against and , with respective IC values of 88.14 ± 2.21 µg/mL and 52.36 ± 1.38 µg/mL. Compound showed significant cytotoxicity against A2780, PC-3, and MBA-MD-231 cell lines with respective IC values of 3.20, 10.68, and 16.30 µM, and the cytotoxicity against A2780 cells was even higher than that of cisplatin (CDDP). With an IC value of 10.13 µM, compound also exhibited cytotoxicity against A2780. The in vitro results showed that compound inhibited A2780 cell proliferation, induced apoptosis, and arrested the cell cycle at the S-phase in a concentration-dependent manner.

摘要

从一种新记录真菌的大米发酵产物中,分离出了两种新的聚酮化合物,新格里斯酚A()和新格里斯酚B(),一种新的异苯并呋喃-1-酮,()-6-羟基-7-甲氧基-3,5-二甲基异苯并呋喃-1-酮(),以及四种已知化合物(-)。通过一维和二维核磁共振、质谱和化学计算确定了它们的结构。在化合物和中,两个萘醌衍生物部分之间的C-3~C-2'聚合模式并不常见。同时,化合物-和对、、、表现出抗菌活性,最小抑菌浓度(MIC)值在16至31μg/mL之间。此外,化合物对和表现出抗真菌活性,其半数抑制浓度(IC)值分别为88.14±2.21μg/mL和52.36±1.38μg/mL。化合物对A2780、PC-3和MBA-MD-231细胞系表现出显著的细胞毒性,其IC值分别为3.20、10.68和16.30μM,对A2780细胞的细胞毒性甚至高于顺铂(CDDP)。化合物对A2780也表现出细胞毒性,IC值为10.13μM。体外实验结果表明,化合物抑制A2780细胞增殖,诱导细胞凋亡,并以浓度依赖的方式使细胞周期停滞在S期。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14ba/10055829/8f293996044a/metabolites-13-00435-g001.jpg

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