Synthesis of Magnolol and Honokiol Derivatives and Their Effect Against Hepatocarcinoma Cells

Overview

Journal PLoS One

Specialties General Medicine
Science

Date 2018 Feb 8

PMID 29415009

Citations 22

Authors

Margherita Maioli

Valentina Basoli

Paola Carta

Davide Fabbri

Maria Antonietta Dettori

Sara Cruciani

Pier Andrea Serra

Giovanna Delogu

Affiliations

Soon will be listed here.

Abstract

The hepatocellular carcinoma is one of the most common malignant tumour with high level of mortality rate due to its rapid progression and high resistance to conventional chemotherapies. Thus, the search for novel therapeutic leads is of global interest. Herein, a small set of derivatives of magnolol 1 and honokiol 2, the main components of Magnolia grandiflora and Magnolia obovata, were evaluated in in vitro assay using tumoral hepatocytes. The pro-drug approach was applied as versatile strategy to the improve bioactivity of the compounds by careful transformation of the hydroxyl groups of magnolol 1 and honokiol 2 in suitable ester derivatives. Compounds 10 and 11 resulted to be more potent than the parental honokiol 2 at concentration down to 1 μM with complete viability of treated fibroblast cells up to concentrations of 80 μM. The combination of a butyrate ester and a bare phenol-OH group in the honokiol structure seemed to play a significant role in the antiproliferative activity identifying an interesting pharmacological clue against hepatocellular carcinoma.

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