Antitumor aspochalasin and antiviral benzofuran derivatives from a marine-derived fungus Aspergillus sp. SCSIO41032

Abstract

Chemical investigation of the EtOAc extract of a deep-sea derived fungus Aspergillus sp. SCSIO41032 resulted in the isolation of ten known compounds, including eight aspochalasins. Their structures were elucidated by using extensive NMR spectroscopic, mass spectrometric and single crystal X-ray diffraction analysis. The detailed crystallographic data for structures 1, 2, and 4, along with the relative configurations of aspochalasin E (3) determined by its acetonide derivative were reported for the first time. The results of antitumor and antiviral activities showed that 3 displayed moderate antitumor activities against 22Rv1, PC-3, A549, and HCT-15 cell lines with IC₅₀ values ranged from 5.9 ± 0.8 to 19.0 ± 7.7 μM, and 9 exhibited moderate antiviral activities against HSV-1/2 with EC₅₀ values of 9.5 ± 0.5 and 5.4 ± 0.6 μM, respectively. Plate clone formation assays results indicated that 3 inhibited the 22Rv1, PC-3 cells growth in a dose-dependent manner.

Graphical Abstract

Keywords:

• Aspochalasin
• Benzofuran
• acetonide derivative reaction
• antitumor
• antiviral

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

The research was supported by the Hainan Provincial Joint Project of Sanya Yazhou Bay Science and Technology City [2021CXLH0013, 2021JJLH0097], Guangdong Basic and Applied Basic Research Foundation [2021B1515120046], Hainan Provincial Natural Science Foundation of China [823CXTD393].