An epipolythiodioxopiperazine alkaloid and diversified aromatic polyketides with cytotoxicity from the Beibu Gulf coral-derived fungus Emericella nidulans GXIMD 02509

J Zhejiang Univ Sci B. 2023 Mar 15;24(3):275-280. doi: 10.1631/jzus.B2200622.
[Article in English, Chinese]

Abstract

Marine microorganisms, especially marine fungi, have historically proven their value as a prolific source for structurally novel and pharmacologically active secondary metabolites (Deshmukh et al., 2018; Carroll et al., 2022). The corals constitute a dominant part of reefs with the highest biodiversity, and harbor highly diverse and abundant microbial symbionts in their tissue, skeleton, and mucus layer, with species-specific core members that are spatially partitioned across coral microhabitats (Wang WQ et al., 2022). The coral-associated fungi were very recently found to be vital producers of structurally diverse compounds, terpenes, alkaloids, peptides, aromatics, lactones, and steroids. They demonstrate a wide range of bioactivity such as anticancer, antimicrobial, and antifouling activity (Chen et al., 2022). The genetically powerful genus Emericella (Ascomycota), which has marine and terrestrial sources, includes over 30 species and is distributed worldwide. It is considered a rich source of diverse secondary metabolites with antimicrobial activity or cytotoxicity (Alburae et al., 2020). Notably, Emericella nidulans, the sexual state of a classic biosynthetic strain Aspergillus nidulans, was recently reported as an important source of highly methylated polyketides (Li et al., 2019) and isoindolone-containing meroterpenoids (Zhou et al., 2016) with unusual skeletons.

北部湾藴育着丰富且亟待研究的海洋(微)生物资源,是活性天然产物的重要来源。本研究从涠洲岛珊瑚共附生构巢裸胞壳菌GXIMD 02509中分离获得一个多硫代二酮哌嗪生物碱和系列芳香聚酮类化合物,含一个新化合物4a-O-methoxyarugosin H (1)。我们通过采用多种波、光谱学技术及对比文献方法鉴定了化合物的化学结构。化合物1-5710对786-O、SW1990和SW480等3株肿瘤细胞增殖具抑制活性,半抑制浓度(IC50)值为4.3–33.4 μmol/L。化合物emestrin J (10)具有一个二硫桥键,还能够显著抑制786-O细胞克隆及迁移,诱导786-O细胞凋亡并阻滞细胞分裂在G2/M期,是一个潜在具抗肿瘤活性的先导化合物。.

北部湾藴育着丰富且亟待研究的海洋(微)生物资源,是活性天然产物的重要来源。本研究从涠洲岛珊瑚共附生构巢裸胞壳菌GXIMD 02509中分离获得一个多硫代二酮哌嗪生物碱和系列芳香聚酮类化合物,含一个新化合物4a-O-methoxyarugosin H (1)。我们通过采用多种波、光谱学技术及对比文献方法鉴定了化合物的化学结构。化合物1-5710对786-O、SW1990和SW480等3株肿瘤细胞增殖具抑制活性,半抑制浓度(IC50)值为4.3–33.4 μmol/L。化合物emestrin J (10)具有一个二硫桥键,还能够显著抑制786-O细胞克隆及迁移,诱导786-O细胞凋亡并阻滞细胞分裂在G2/M期,是一个潜在具抗肿瘤活性的先导化合物。

MeSH terms

  • Alkaloids*
  • Animals
  • Anthozoa* / microbiology
  • Anti-Infective Agents* / pharmacology
  • Aspergillus nidulans*
  • Polyketides* / chemistry
  • Polyketides* / pharmacology

Substances

  • Polyketides
  • Anti-Infective Agents
  • Alkaloids