Next Article in Journal
Preparation and Identification of ACE Inhibitory Peptides from the Marine Macroalga Ulva intestinalis
Previous Article in Journal
Transcriptomic-Proteomic Correlation in the Predation-Evoked Venom of the Cone Snail, Conus imperialis
Previous Article in Special Issue
New 9α-Hydroxy-5α,6α-epoxysterols from the Vietnamese Marine Sponge Ircinia echinata
Article Menu
Issue 3 (March) cover image

Export Article

Open AccessArticle
Mar. Drugs 2019, 17(3), 178; https://doi.org/10.3390/md17030178

Steroids from the Deep-Sea-Derived Fungus Penicillium granulatum MCCC 3A00475 Induced Apoptosis via Retinoid X Receptor (RXR)-α Pathway

1
School of Pharmaceutical Sciences, Xiamen University, South Xiangan Road, Xiamen 361005, China
2
Key Laboratory of Marine Biogenetic Resources, South China Sea Bio-Resource Exploitation and Utilization Collaborative Innovation Center, Third Institute of Oceanography, Ministry of Natural Resources, 184 Daxue Road, Xiamen 361005, China
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Received: 24 February 2019 / Revised: 13 March 2019 / Accepted: 15 March 2019 / Published: 19 March 2019
(This article belongs to the Special Issue Steroids from Marine Sources)
  |  
PDF [5914 KB, uploaded 19 March 2019]
  |     |  

Abstract

Five new ergostanes, penicisteroids D−H (15), were isolated from the liquid culture of the deep-sea-derived fungus Penicillium granulatum MCCC 3A00475, along with 27 known compounds. The structures of the new steroids were established mainly on the basis of extensive analysis of 1D and 2D NMR as well as HRESIMS data. Moreover, the absolute configurations of 1 were confirmed unambiguously by the single-crystal X-ray crystallography. Compounds 2 and 47 showed moderate antiproliferative effects selectively against 12 different cancer cell lines with IC50 values of around 5 μM. Compounds 2 and 6, potent RXRα binders with Kd values of 13.8 and 12.9 μM, respectively, could induce apoptosis by a Retinoid X Receptor (RXR)-α-dependent mechanism by regulating RXRα transcriptional expression and promoting the poly-ADP-ribose polymerase (PARP) cleavage. Moreover, they could inhibit proliferation by cell cycle arrest at the G0/G1 phase. View Full-Text
Keywords: marine-derived fungus; Penicillium granulatum; ergostanes; anti-tumor; nuclear receptor marine-derived fungus; Penicillium granulatum; ergostanes; anti-tumor; nuclear receptor
Figures

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Supplementary material

SciFeed

Share & Cite This Article

MDPI and ACS Style

Xie, C.-L.; Zhang, D.; Xia, J.-M.; Hu, C.-C.; Lin, T.; Lin, Y.-K.; Wang, G.-H.; Tian, W.-J.; Li, Z.-P.; Zhang, X.-K.; Yang, X.-W.; Chen, H.-F. Steroids from the Deep-Sea-Derived Fungus Penicillium granulatum MCCC 3A00475 Induced Apoptosis via Retinoid X Receptor (RXR)-α Pathway. Mar. Drugs 2019, 17, 178.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Mar. Drugs EISSN 1660-3397 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top