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Published in: BMC Complementary Medicine and Therapies 1/2020

Open Access 01-12-2020 | Research article

Synthesis of crocetin derivatives and their potent inhibition in multiple tumor cells proliferation and inflammatory property of macrophage

Authors: Mao-Ze Wang, Jin Gao, Yang Chu, Jie Niu, Ming Chen, Qiang Shang, Li-Hua Peng, Zhi-Hong Jiang

Published in: BMC Complementary Medicine and Therapies | Issue 1/2020

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Abstract

Background

Crocetin is a major active component of saffron, which has a wide range of pharmacological effects. However, due to its low solubility, the pharmacological effects of crocetin cannot be better utilized.

Methods

In this study, we modified the chemical structure of crocetin by conjugating with ethylamine and 4-Fluorbenzylamine to enhance its solubility and biological activities. The solubility and the influence of synthesized derivatives on the proliferation of tumor cells and the inflammatory effect of macrophage were investigated.

Results

It was shown that, compared with the crocetin, the synthesized derivatives have much higher solubility. Moreover, the inhibitory effect of the derivatives on varieties of tumor cells, including human ovarian carcinoma cell line, human lung cancer cell line, rat melanoma cell line was enhanced after the modification. Besides that, the derivatives were improved for the anti-inflammatory efficacy with the cytotoxicity decreased.

Conclusions

The synthesized derivatives were shown for their good solubility and the great potential in tumor and inflammation treatment.
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Metadata
Title
Synthesis of crocetin derivatives and their potent inhibition in multiple tumor cells proliferation and inflammatory property of macrophage
Authors
Mao-Ze Wang
Jin Gao
Yang Chu
Jie Niu
Ming Chen
Qiang Shang
Li-Hua Peng
Zhi-Hong Jiang
Publication date
01-12-2020
Publisher
BioMed Central
Published in
BMC Complementary Medicine and Therapies / Issue 1/2020
Electronic ISSN: 2662-7671
DOI
https://doi.org/10.1186/s12906-020-2831-y

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