Page 171 - 2025中醫藥與天然藥物聯合學術研討會-中醫藥與天然藥物的挑戰Ｘ機遇與未來大會手冊

PC-53

Brominated azaphilones with anti-angiogenic activity produced by algicolous

fungus Penicillium sclerotiorum

+,1
1
1
Limbadri Salendra, Shih-Wei Wang, +,2,3 Tzi-Yi Ke , Pei-Ting Chiang, Ming-Ya
1
5
Cheng, Yu-Chi Lin, Ching-Yeu Chen, Yuan-Bin Cheng* ,1,3
4

1 Department of Marine Biotechnology and Resources, National Sun Yat-sen University,
Kaohsiung, Taiwan
2 Institute of Biomedical Sciences, MacKay Medical College, New Taipei City, Taiwan
3 Graduate Institute of Natural Products, College of Pharmacy, Kaohsiung Medical University,
Kaohsiung, Taiwan
4 National Research Institute of Chinese Medicine, Ministry of Health and Welfare, Taipei,
Taiwan
5 Department of Physical Therapy, Tzu-Hui Institute of Technology, Pingtung, Taiwan
+ These authors contributed equally to this work.
* E-mail: jmb@mail.nsysu.edu.tw

Abstract
The fungus Penicillium sclerotiorum, derived from the marine alga Grateloupia sp., was
fermented in a liquid medium supplemented with 3.5% excess NaBr, leading to the isolation of
seven new brominated compounds, bromophilones A–G (1–7) and one new 11Z-
sclerazaphilone G (8). Notably, compound (6) features a pyridine ring in place of the typical
pyrone core. The planar structures and relative configurations of the new compounds were
established through comprehensive spectroscopic analyses, including 1D, 2D NMR, and ECD
spectra. All isolated compounds were evaluated for their anti-angiogenetic effects. Interestingly,
compounds 4 and 5 exhibited significant inhibitory activity against human endothelial
progenitor cells (EPCs), with IC50 values of 2.5 and 4.7 µg/mL, respectively. Comparison of
halogenated and non-halogenated azaphilones revealed that halogenated derivatives generally
exhibit potent anti-angiogenic activity, with chlorine-and bromine-substituted azaphilones
displaying similar activity.

Keywords: Penicillium sclerotiorum; Brominated azaphilones; Angiogenesis activity