Characterization of Cladosporols from the Marine Algal-Derived Endophytic Fungus Cladosporium cladosporioides EN-399 and Configurational Revision of the Previously Reported Cladosporol Derivatives

J Org Chem. 2017 Oct 6;82(19):9946-9954. doi: 10.1021/acs.joc.7b01277. Epub 2017 Sep 20.

Abstract

Four new cladosporol derivatives, cladosporols F-I (1-4), the known cladosporol C (5), and its new epimer, cladosporol J (6), were isolated and identified from the marine algal-derived endophytic fungus Cladosporium cladosporioides EN-399. Their structures were determined by detailed interpretation of NMR and MS data, and the absolute configurations were established on the basis of TDDFT-ECD and OR calculations. The configurational assignment of cladosporols F (1) and G (2) showed that the previously reported absolute configuration of cladosporol A and all the related cladosporols need to be revised from (4'R) to (4'S). Compounds 1-6 showed antibacterial activity against Escherichia coli, Micrococcus luteus, and Vibrio harveyi with MIC values ranging from 4 to 128 μg/mL. Compound 3 showed significant cytotoxicity against A549, Huh7, and LM3 cell lines with IC50 values of 5.0, 1.0, and 4.1 μM, respectively, and compound 5 showed activity against H446 cell line with IC50 value of 4.0 μM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / isolation & purification
  • Anti-Bacterial Agents / pharmacology*
  • Cladosporium / chemistry*
  • Dose-Response Relationship, Drug
  • Escherichia coli / drug effects*
  • Microbial Sensitivity Tests
  • Micrococcus luteus / drug effects*
  • Molecular Structure
  • Naphthalenes / chemistry
  • Naphthalenes / isolation & purification
  • Naphthalenes / pharmacology*
  • Structure-Activity Relationship
  • Vibrio / drug effects*

Substances

  • Anti-Bacterial Agents
  • Naphthalenes
  • cladosporol