Abstract

Five new compounds called Pestalotis A–E (1–5), comprising three monoterpene-lactone compounds (1–3), one tetrahydrobenzofuran derivative (4), and one sesquiterpene (5), were isolated from the EtOAc extract of Pestalotiopsis sp. The structures of the new compounds were elucidated by analysis of their NMR, HRMS, and ECD spectra, and the absolute configurations were established through the comparison of experimental and calculated ECD spectra. All compounds were tested for antitumor activity against SW-480, LoVo, HuH-7, and MCF-7. The results showed that compounds 2 and 4 exhibited potent antitumor activity against SW-480, LoVo, and HuH-7 cell lines. Furthermore, compound 4 was assessed against HuH-7, and the results indicated that the rate of apoptosis was dose-dependent.

Highlights

  • Secondary metabolites are natural products that have been selected by evolution over millions of years, displaying a unique chemical diversity and corresponding diversity of biological activities [1,2,3]

  • Motivated by its fascinating secondary metabolites, we launched a chemical investigation of both new and bioactive compounds from Pestalotiopsis sp., which is an endophytic fungus derived from the surface-sterilized root of Ligusticum chuanxiong Hort

  • Following comparisons with BLAST, we found that this sequence exhibited a significantly high identification with Pestalotiopsis sp

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Summary

Introduction

Secondary metabolites are natural products that have been selected by evolution over millions of years, displaying a unique chemical diversity and corresponding diversity of biological activities [1,2,3]. Investigations of the fungi of Pestalotiopsis genus have made significant progress in new structure exploration, which has resulted in the discovery of various types of compounds including terpenoids, alkaloids, polyketones, and anthraquinones [10,11], and these have exhibited a broad spectrum of, among others, antitumor, anti-virus, antibacterial, and immunosuppressive activities [12,13]. Recent chemical research on the species resulted in the production of many terpenoid molecules with new structures and obvious biological activities, such as structurally complex epoxyquinols [14], polyketideterpene hybrid metabolites with highly functionalized groups [15], and unusual new bicyclic and tricyclic sesquiterpenoids that bear potent immunosuppressive and cytotoxic activity [12]. Motivated by its fascinating secondary metabolites, we launched a chemical investigation of both new and bioactive compounds from Pestalotiopsis sp., which is an endophytic fungus derived from the surface-sterilized root of Ligusticum chuanxiong Hort.

Results
Procedures
Fungal Material
Extraction and Isolation
Cell Culture
Cell Viability Assay
Statistical Analysis
Cell Cycle Assays
Conclusions
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