Next Article in Journal
Direct Observation of Hydrangea Blue-Complex Composed of 3-O-Glucosyldelphinidin, Al3+ and 5-O-Acylquinic Acid by ESI-Mass Spectrometry
Next Article in Special Issue
Structure-Dependent Activity of Natural GABA(A) Receptor Modulators
Previous Article in Journal
(-)-Shikimic Acid as a Chiral Building Block for the Synthesis of New Cytotoxic 6-Aza-Analogues of Angucyclinones
Previous Article in Special Issue
Synthesis and Promotion of the Osteoblast Proliferation Effect of Morroniside Derivatives
Article Menu
Issue 6 (June) cover image

Export Article

Open AccessFeature PaperArticle
Molecules 2018, 23(6), 1423; https://doi.org/10.3390/molecules23061423

Natural Aromatic Compounds as Scaffolds to Develop Selective G-Quadruplex Ligands: From Previously Reported Berberine Derivatives to New Palmatine Analogues

1
Dipartimento di Chimica, Università di Roma “La Sapienza”, Piazzale Aldo Moro 5, 00185 Rome, Italy
2
Dipartimento di Biologia e Biotecnologie, Università di Roma “La Sapienza”, Piazzale Aldo Moro 5, 00185 Rome, Italy
3
Dipartimento di Biologia Ambientale, Università di Roma “La Sapienza”, Piazzale Aldo Moro 5, 00185 Rome, Italy
4
School of Pharmaceutical Sciences, Shenzhen University Health Science Center, Shenzhen 518060, China
5
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510275, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Antonio Evidente
Received: 12 May 2018 / Revised: 2 June 2018 / Accepted: 8 June 2018 / Published: 12 June 2018
(This article belongs to the Special Issue Structure-Activity Relationship of Natural Products 2018)
Full-Text   |   PDF [1356 KB, uploaded 12 June 2018]   |  

Abstract

In this paper, the selective interactions of synthetic derivatives of two natural compounds, berberine and palmatine, with DNA G-quadruplex structures were reported. In particular, the previous works on this subject concerning berberine were further presented and discussed, whereas the results concerning palmatine are presented here for the first time. In detail, these palmatine derivatives were developed by inserting seven different small peptide basic chains, giving several new compounds that have never been reported before. The preliminary studies of the interactions of these compounds with various G-quadruplex-forming sequences were carried out by means of various structural and biochemical techniques, which showed that the presence of suitable side chains is very useful for improving the interaction of the ligands with G-quadruplex structures. Thus, these new palmatine derivatives might act as potential anticancer drugs. View Full-Text
Keywords: G-quadruplex DNA; interactions; berberine and palmatine derivatives; NMR; FRET and MST assays G-quadruplex DNA; interactions; berberine and palmatine derivatives; NMR; FRET and MST assays
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).
SciFeed

Share & Cite This Article

MDPI and ACS Style

Franceschin, M.; Cianni, L.; Pitorri, M.; Micheli, E.; Cacchione, S.; Frezza, C.; Serafini, M.; Hu, M.-H.; Su, H.; Huang, Z.; Gu, L.; Bianco, A. Natural Aromatic Compounds as Scaffolds to Develop Selective G-Quadruplex Ligands: From Previously Reported Berberine Derivatives to New Palmatine Analogues. Molecules 2018, 23, 1423.

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]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top