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Phthalides Isolated from the Endolichenic Arthrinium sp. EL000127 Exhibits Antiangiogenic Activity

Gamage, Chathurika D B ; Lee, Kyungha ; Park, So-Yeon ; Varlı, Mücahit ; Lee, Chang Wook ; Kim, Seong-Min ; Zhou, Rui ; Pulat, Sultan ; Yang, Yi and Taş, İsa LU orcid , et al. (2023) In ACS Omega 8(13). p.12548-12557
Abstract

Endolichenic fungi (ELF) produce specialized metabolites that have various medicinal properties. Inhibition of tumor angiogenesis efficaciously suppresses many types of cancer. This study aimed to discover novel antiangiogenic agents from specialized metabolite extracts of ELF strains isolated from Korean lichens. The EtOAc extracts of 51 ELF strains were subjected to a screening pipeline consisting of cell viability, scratch wound healing, and Transwell migration assays. The EtOAc extract of Arthrinium sp. EL000127 showed the most potent inhibitory activity against the chemotactic migration of human umbilical vein endothelial cells (HUVEC). Targeted isolation on the major LC-MS peaks exhibited a previously known phthalide,... (More)

Endolichenic fungi (ELF) produce specialized metabolites that have various medicinal properties. Inhibition of tumor angiogenesis efficaciously suppresses many types of cancer. This study aimed to discover novel antiangiogenic agents from specialized metabolite extracts of ELF strains isolated from Korean lichens. The EtOAc extracts of 51 ELF strains were subjected to a screening pipeline consisting of cell viability, scratch wound healing, and Transwell migration assays. The EtOAc extract of Arthrinium sp. EL000127 showed the most potent inhibitory activity against the chemotactic migration of human umbilical vein endothelial cells (HUVEC). Targeted isolation on the major LC-MS peaks exhibited a previously known phthalide, 3-O-methylcyclopolic acid (1), and two unknown analogues of 1, 3-O-phenylethylcyclopolic acid (2) and 3-O-p-hydroxyphenylethylcyclopolic acid (3). The structures were characterized by MS and NMR analyses. All the isolates were acquired and applied to bioassays as racemates due to spontaneous racemization. Among the isolates, compound 3 effectively inhibits HUVEC motility by suppressing mRNA expressions of genes regulating epithelial cell survival and motility, which suggested that compound 3 is a potent antiangiogenic agent suitable for further exploration as a potential novel therapeutic against cancers.

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publishing date
type
Contribution to journal
publication status
published
in
ACS Omega
volume
8
issue
13
pages
12548 - 12557
publisher
The American Chemical Society (ACS)
external identifiers
  • scopus:85151292215
  • pmid:37033794
ISSN
2470-1343
DOI
10.1021/acsomega.3c00876
language
English
LU publication?
no
additional info
© 2023 The Authors. Published by American Chemical Society.
id
54568a74-9152-4700-bc29-c33622c9638c
date added to LUP
2026-09-23 15:59:44
date last changed
2026-09-24 04:01:33
@article{54568a74-9152-4700-bc29-c33622c9638c,
  abstract     = {{<p>Endolichenic fungi (ELF) produce specialized metabolites that have various medicinal properties. Inhibition of tumor angiogenesis efficaciously suppresses many types of cancer. This study aimed to discover novel antiangiogenic agents from specialized metabolite extracts of ELF strains isolated from Korean lichens. The EtOAc extracts of 51 ELF strains were subjected to a screening pipeline consisting of cell viability, scratch wound healing, and Transwell migration assays. The EtOAc extract of Arthrinium sp. EL000127 showed the most potent inhibitory activity against the chemotactic migration of human umbilical vein endothelial cells (HUVEC). Targeted isolation on the major LC-MS peaks exhibited a previously known phthalide, 3-O-methylcyclopolic acid (1), and two unknown analogues of 1, 3-O-phenylethylcyclopolic acid (2) and 3-O-p-hydroxyphenylethylcyclopolic acid (3). The structures were characterized by MS and NMR analyses. All the isolates were acquired and applied to bioassays as racemates due to spontaneous racemization. Among the isolates, compound 3 effectively inhibits HUVEC motility by suppressing mRNA expressions of genes regulating epithelial cell survival and motility, which suggested that compound 3 is a potent antiangiogenic agent suitable for further exploration as a potential novel therapeutic against cancers.</p>}},
  author       = {{Gamage, Chathurika D B and Lee, Kyungha and Park, So-Yeon and Varlı, Mücahit and Lee, Chang Wook and Kim, Seong-Min and Zhou, Rui and Pulat, Sultan and Yang, Yi and Taş, İsa and Hur, Jae-Seoun and Kang, Kyo Bin and Kim, Hangun}},
  issn         = {{2470-1343}},
  language     = {{eng}},
  month        = {{04}},
  number       = {{13}},
  pages        = {{12548--12557}},
  publisher    = {{The American Chemical Society (ACS)}},
  series       = {{ACS Omega}},
  title        = {{Phthalides Isolated from the Endolichenic Arthrinium sp. EL000127 Exhibits Antiangiogenic Activity}},
  url          = {{http://dx.doi.org/10.1021/acsomega.3c00876}},
  doi          = {{10.1021/acsomega.3c00876}},
  volume       = {{8}},
  year         = {{2023}},
}