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Bioorg Med Chem. 2017 Oct 15;25(20):5506-5512. doi: 10.1016/j.bmc.2017.08.013. Epub 2017 Aug 9.

The design and synthesis of a novel compound of berberine and baicalein that inhibits the efficacy of lipid accumulation in 3T3-L1 adipocytes.

Author information

1
School of Chinese Herbal Medicine, Guangzhou University of Chinese Medicine, Guangzhou 510006, People's Republic of China.
2
Guangzhou Pi & Pi Technology Inc, Guangzhou 510006, People's Republic of China.
3
First School of Clinical Medicine, Guangzhou University of Chinese Medicine, Guangzhou 510405, People's Republic of China.
4
School of Chinese Herbal Medicine, Guangzhou University of Chinese Medicine, Guangzhou 510006, People's Republic of China. Electronic address: liweimin@gzucm.edu.cn.

Abstract

The combination of berberine and baicalein may have a better therapeutic effect against disease. To explore the combined effect of baicalein and berberine in the treatment of obesity, we designed and synthesized a hybrid compound, and its biological activities were evaluated in 3T3-L1 adipocytes. The structures of the berberine-baicalein (BBS) compounds were confirmed by 1H NMR, 13C NMR, ultraviolet spectroscopy and high resolution mass spectrometry (HRMS). The present study showed that the IC50 values of the inhibitory effects of baicalein, berberine and BBS against 3T3-L1 cells were 29.81±0.90, 21.84±1.67 and 9.42±0.60µM, respectively. The expression of mRNAs related to lipolysis and lipogenesis were examined by quantitative real-time PCR. The results showed that BBS could up-regulate the expression of the Atgl gene and down-regulate the mRNA expression of Srebp-1c, Fasn, Scd1, and Acc in 3T3-L1 adipocytes. These results indicate that BBS may have a stronger effect than baicalein and berberine on the viability of 3T3-L1 preadipocytes. In addition, BBS may have therapeutic effects and pharmacological activities against obesity. This "medicine couple" may be beneficial for studies of traditional Chinese medicine.

KEYWORDS:

Baicalein; Berberine; Obesity; Synthesis

PMID:
28818460
DOI:
10.1016/j.bmc.2017.08.013
[Indexed for MEDLINE]

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