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Special Issue "Silymarin and Derivatives: From Biosynthesis to Health Benefits"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: 31 March 2019

Special Issue Editor

Guest Editor
Prof. Dominique Delmas

INSERM Research Center U1231 – “Cancer and Adpatative Immune Response” Team, “Bioactive Molecules and Health” research group, Dijon, France
Interests: polyhenols; flavonoids; degenerative age-related diseases; inflammation; cancers; chemosensitization; lipid metabolism

Special Issue Information

Dear Colleagues,

Numerous epidemiological studies show that some nutrients may protect against vascular diseases, cancers, degenerative diseases, and associated inflammatory effects. Among these compounds, flavonolignans are a family of natural products present in plants, composed of a flavonoid moiety and a phenylpropanoid or lignan part, that could contribute to the development of new strategies to fight various modern pathologies. In this context, one of the most important compounds among flavonolignans is silymarin which is extracted from milk thistle seeds and could act as a chemopreventive compound or a therapeutic adjuvant.

This Special Issue will cover areas related to the biosynthesis of silymarin and its derivatives, its bioavailability, and its health benefits. More particularly, this Special Issue will highlight the biological properties of silymarin and its derivatives in major fields in terms of public health, including cardiovascular diseases, metabolic syndrome, cancers, degenerative age-related diseases, and inflammatory and immune pathologies.

I cordially invite authors to contribute original articles, as well as review articles, that will give the readers of Molecules an updated and new perspective about silymarin and its derivatives, helping establish new interests in the development of natural compounds for health.

Prof. Dominique Delmas
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.


  • Silymarin: sources and biosynthesis
  • Secondary metabolites and silymarin derivatives
  • Silymarin bioavaibility
  • Silymarin and cardiovascular diseases
  • Silymarin and metabolic syndrome
  • Silymarin and cancer
  • Silymarin and inflammation and immune diseases
  • Silymarin and degenerative age-related diseases

Published Papers (1 paper)

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Open AccessFeature PaperCommunication Selective Synthesis of 3-O-Palmitoyl-Silybin, a New-to-Nature Flavonolignan with Increased Protective Action against Oxidative Damages in Lipophilic Media
Molecules 2018, 23(10), 2594; https://doi.org/10.3390/molecules23102594
Received: 3 September 2018 / Revised: 22 September 2018 / Accepted: 9 October 2018 / Published: 10 October 2018
PDF Full-text (564 KB) | HTML Full-text | XML Full-text | Supplementary Files
A selective acylation protocol using cerium chloride (CeCl3) as catalyst was applied to functionalize silybinin (1), a natural antioxidant flavonolignan from milk thistle fruit, in order to increase its solubility in lipophilic media while retaining its strong antioxidant activity.
[...] Read more.
A selective acylation protocol using cerium chloride (CeCl3) as catalyst was applied to functionalize silybinin (1), a natural antioxidant flavonolignan from milk thistle fruit, in order to increase its solubility in lipophilic media while retaining its strong antioxidant activity. The selective esterification of 1 at the position 3-OH with a palmitate acyl chain leading to the formation of the 3-O-palmitoyl-silybin (2) was confirmed by both mass spectroscopy (MS) and nuclear magnetic resonance (NMR) analyses. The antioxidant activity of 1 was at least retained and even increased with the CUPRAC assay designed to estimate the antioxidant activity of both hydrophilic and lipophilic compounds. Finally, the 3-O-palmitoylation of 1, resulting in the formation of 2, also increased its anti-lipoperoxidant activity (i.e., inhibition of conjugated diene production) in two different lipophilic media (bulk oil and o/w emulsion) subjected to accelerated storage test. Full article
(This article belongs to the Special Issue Silymarin and Derivatives: From Biosynthesis to Health Benefits)

Graphical abstract

Planned Papers

The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.

Authors: Mariana Leticia Matias 2; Virginia Juliani Gomes 2; Mariana Romao-Veiga 1; Vanessa Rocha Ribeiro 2; Priscila Rezeck Nunes 2; Mariane Font Fernandes 1; Jose Carlos Peracoli 2; Maria Terezinha Serrao Peracoli 1
Affiliations: 1 Institute of Biosciences
2 Medical School – Botucatu Sao Paulo State University, UNESP; Botucatu, Sao Paulo, Brazil
Tentative title: Silibinin Downregulates the NF-κB Pathway and NLRP1/NLRP3 Inflammasomes Induced by Monosodium Urate in Monocytes from Pregnant Women with Preeclampsia
Abstract: Objective: To evaluate whether silibinin (SB) treatment of monocytes obtained from preeclamptic women and from normotensive pregnant women stimulated in vitro with monosodium urate (MSU) can modulate the NLRP1 and NLRP3 inflammasomes and NF-κB pathway activation.
Study Design: Twenty preeclamptic women and 20 normotensive pregnant women (NT) were studied. Peripheral blood monocytes from pregnant women and THP-1 cells were cultured in the presence or absence of urate monosodium or silibinin. Gene expression of NLRP1, NLRP3, Caspase-1, TLR4, MyD88, NF-κB, IL-1β, IL-18, TNF-α and IL-10 was performed by qPCR and inflammatory cytokines production was evaluated by ELISA. Addiotionally, p65NF-κB activity in monocytes from pregnant women was determined by transcription factor ELISA kit.
Results: Monocytes from women with PE showed endogenous activation of NLRP1 and NLRP3 inflammasomes components and NF-κB pathway, expressed high amounts of IL-1β, IL-18 and TNF-α mRNA and lower gene expression of IL-10. The stimulation of monocytes with MSU increased the inflammation-related genes, while treatment with SB reduced the expression of those. p65NF-κB basal activity was higher on PE group and after stimuli with MSU. However, SB-treated monocytes showed decrease in p65NF-κB activity. Additionally, THP-1 cells had a similar immunological response profile of monocytes from preeclamptic women when cultured with or without urate monosodium and silibinin.
Conclusion: These results suggest MSU participation in the systemic inflammatory response characteristic of preeclampsia and that silibinin treatment is capable of modulating the sterile inflammation established in monocytes of preeclamptic women, demonstrating a relevant role of this flavonoid on the regulation of the inflammatory response in this disease.
Keywords: monocytes, preeclampsia, urate monosodium, NF-kB, NLRP1/NLRP3 inflammasome, silibinin

Authors: Alfonso Di Costanzo 1, Antonella Angiolillo 1, Ruggero Angelico 2
Affiliations: 1 Centre for Research and Training in Medicine for Aging, Department of Medicine and Health Sciences "Vincenzo Tiberio", University of Molise, I-86100 Campobasso, (Italy);
2 Department of Agriculture, Environmental and Food Sciences (DIAAA), University of Molise, I-86100 Campobasso, (Italy).
Tentative title: Advanced nanotechnologies for enhancing the bioavailability of silymarin: a state of the art.
Tentative abstract: Silymarin, a mixture of flavonolignan and flavonoid polyphenolic compounds extractable from the milk thistle seed, Silybum marianum, has anti-oxidant, anti-inflammatory, anti-cancer and anti-viral activities potentially useful in the treatment of several liver disorders, such as chronic liver diseases, cirrhosis and hepatocellular carcinoma. Equally promising are the effects of silymarin in protecting the brain from the inflammatory and oxidative stress effects by which metabolic syndrome contributes to Alzheimer's Disease. However, despite clinical trials have proved that silymarin is safe at high doses (>1500 mg/day) in humans, it suffers limiting factors such as low solubility in water (< 50 μg/mL), low bioavailability and poor intestinal absorption. To improve its bioavailability and provide a prolonged silymarin release at the site of absorption, the use of nanotechnological strategies appears to be a promising method to potentiate the therapeutic action and promote sustained release of the active herbal extract. The purpose of this study is to review nanostructured systems as efficient delivery formulations for enhanced absorption and bioavailability of silymarin.
Keywords: Silymarin; oral and parenteral delivery formulations; lipid nanoparticles; nanohybrid delivery systems; enhanced bioavailability

Authors: Valeria Romanucci, Giovanni Di Fabio and Armando Zarrelli*
Affiliations: Department of Chemical Sciences, University of Napoli - Federico II, Via Cintia 4, 80126 Napoli, Italy
Tentative title: A new class of synthetic flavonolignan-like dimers: still few but with attractive properties
Tentative abstract:During the years, there is an increasing interest together to a strong curiosity for dimeric molecules that have been reported to exert a promising therapeutic value for the treatment of numerous diseases (cancer, HIV, Alzheimer, malaria). Many reports in literature have highlighted the ability of these molecules to interact not only with specific biologic receptors, but also to induce a biological response that results more than twice times of the corresponding monomeric counterpart.
In this regard, bi-flavonolignans are an emerging class of dimeric compounds that unlike bi-flavonoids, which are very widespread in nature, they are mainly consist of synthetic dimers of some flavonolignans isolated from the milk thistle Silybum marianum.
In light of emerging medicinal chemistry strategies (Multi-Ligand Drugs), this review will discuss the recent developments in the synthesis, characterization and antioxidant activity of a family of flavonolignan dimers.

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