Abstract

Chemical investigation of secondary metabolites from the endophytic fungus Pseudopestalotiopsis theae led to the isolation of eighteen new polyketide derivatives, pestalotheols I–Q (1–9) and cytosporins O–W (15–23), together with eight known analogs (10–14 and 24–26). The structures of the new compounds were elucidated by HRMS and 1D and 2D NMR data, as well as by comparison with literature data. Modified Mosher’s method was applied to determine the absolute configuration of some compounds. Compound 23 showed significant cytotoxicity against the mouse lymphoma cell line L5178Y with an IC50 value of 3.0 μM. Furthermore, compounds 22 and 23 showed moderate antibacterial activity against drug-resistant Acinetobacter baumannii (ATCC BAA-1605) in combination with sublethal colistin concentrations.

Highlights

  • Since the discovery of antibacterial penicillin from Penicillium notatum, there have been tremendous achievements with regard to the development of fungal drugs [1]

  • B, two unique isoprenylated epoxyquinol rice cultures of Pestalotiopsis sp., derivatives obtained from rice cultures of derivatives

  • In previous studies from our group, cytotoxic 14-membered macrolides were obtained from the mangrove-derived fungus fungus Pestalotiopsis

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Summary

Introduction

Since the discovery of antibacterial penicillin from Penicillium notatum, there have been tremendous achievements with regard to the development of fungal drugs [1]. The antifungal medicine griseofulvin, which was initially isolated from Penicillium griseofulvum, has been applied for the treatment of ringworm in skin and nails in animals and humans [2]. Lovastatin, the first commercial statin isolated from a fermentation broth of Aspergillus terreus, has been used to treat high blood cholesterol and reduce the risk of cardiovascular disease [3]. Pestalachloride A, a new chlorinated benzophenone alkaloid produced by Pestalotiopsis adusta, showed potent antifungal activity against Fusarium culmorum with an IC50 value of 0.89 μM [10]. The first chlorinated pupukeanane derivative, chloropupukeananin, which was isolated from fermentation broth of Pestalotiopsis fici, Mar. Drugs 2020, 18, 129; doi:10.3390/md18020129 www.mdpi.com/journal/marinedrugs. 22 of of 16 isolated from fermentation broth of Pestalotiopsis fici, inhibited HIV-1 replication in C8166 cells with inhibited.

A IC and
Discussion
General Experimental Procedures
Fungal Material
Preparation of Compound 17a
Cytotoxicity and Antibacterial Assay

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