Cytochalasans from the fungus Chaetomium globosum with cytotoxic activities against HepG2 cell line

IF 3.4 2区 生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Hong-Fei Li , Tian Jin , Jiao-Xian Du , Xin-Wen Luo , Guo Zhang , Wang-Qiu Deng , Juan He , Tao Feng
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Abstract

Five previously undescribed cytochalasans, chaetomichalasins A–E, along with seventeen known analogues, have been isolated from the solid culture of the fungus Chaetomium globosum. Their structures were elucidated by extensive spectroscopic analysis, with absolute configurations confirmed by electronic circular dichroism calculations. All compounds were assessed for their cytotoxicity against HepG2 cell line, with nine exhibiting cytotoxic activity with IC50 values ranging from 2.36 to 36.23 μM. Preliminary structure-activity relationship analysis suggested that the double bond between C-6 and C-7 should play a key role in the cytotoxicity of these active compounds. Further pharmacological studies revealed that chaetomichalasin C induced G2/M cell cycle arrest and apoptosis in HepG2 cells dose dependently.

Abstract Image

对HepG2细胞系具有细胞毒活性的球形毛藻细胞链
五种先前描述的细胞chalasans, chaetomichalasins A-E,以及17种已知的类似物,已经从真菌chetomium globosum的固体培养中分离出来。它们的结构被广泛的光谱分析所阐明,其绝对构型被电子圆二色性计算所证实。所有化合物对HepG2细胞株的细胞毒性进行了评估,其中9种化合物具有细胞毒活性,IC50值在2.36 ~ 36.23 μM之间。初步的构效关系分析表明,C-6和C-7之间的双键可能在这些活性化合物的细胞毒性中起关键作用。进一步药理研究发现chaetomichalasin C对HepG2细胞的G2/M细胞周期阻滞和凋亡具有剂量依赖性。
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来源期刊
Phytochemistry
Phytochemistry 生物-植物科学
CiteScore
6.40
自引率
7.90%
发文量
443
审稿时长
39 days
期刊介绍: Phytochemistry is a leading international journal publishing studies of plant chemistry, biochemistry, molecular biology and genetics, structure and bioactivities of phytochemicals, including ''-omics'' and bioinformatics/computational biology approaches. Phytochemistry is a primary source for papers dealing with phytochemicals, especially reports concerning their biosynthesis, regulation, and biological properties both in planta and as bioactive principles. Articles are published online as soon as possible as Articles-in-Press and in 12 volumes per year. Occasional topic-focussed special issues are published composed of papers from invited authors.
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