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Baicalin and its aglycone: a novel approach for treatment of metabolic disorders

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Abstract

Background

The current strategies for prevention and treatment of insulin resistance and type 2 diabetes are not fully effective and frequently accompanied by many negative effects. Therefore, novel ways to prevent insulin resistance and type 2 diabetes are urgently needed. The roots of Scutellaria radix are commonly used in traditional Chinese medicines for prevention and treatment of type 2 diabetes, atherosclerosis, hypertension, hyperlipidemia, dysentery, and other respiratory disorders. Baicalin and baicalein are the major and active ingredient extracts from Scutellaria baicalensis.

Methods

A comprehensive and systematic review of literature on baicalin and baicalein was carried out.

Results

Emerging evidence indicated that baicalin and baicalein possessed hepatoprotective, anti-oxidative, anti-dyslipidemic, anti-lipogenic, anti-obese, anti-inflammatory, and anti-diabetic effects, being effective for treating obesity, insulin resistance, non-alcoholic fatty liver, and dyslipidemia. Besides, baicalin and baicalein are almost non-toxic to epithelial, peripheral, and myeloid cells.

Conclusion

The purpose of this study is to focus on the therapeutic applications and accompanying molecular mechanisms of baicalin and baicalein against hyperglycemia, insulin resistance, type 2 diabetes, hyperlipidemia, obesity, and non-alcoholic fatty liver, and trying to establish a novel anti-obese and anti-diabetic strategy.

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Abbreviations

AST:

Aspartate aminotransferase

ALT:

Glutamic pyruvic transaminase

AUC:

Areas under the curve

CREB:

cAMP-responsive element binding protein

CHO:

Cholesterol

G6Pase:

Glucose-6-phosphate

GTT:

Glucose tolerance test

HNF4a:

Hepatocyte nuclear factor 4-alpha

ITT:

Insulin tolerance test

NAFLD:

Nonalcoholic fatty liver disease

NASH:

Nonalcoholic steatohepatitis

PGC-1α:

Peroxisome proliferator-activated receptor gamma co-activator-1α

PEPCK:

Phosphoenolpyruvate carboxykinase

P38MAPK:

P38 mitogen-activated protein kinase

SR:

Scutellariae radix

SIRT1:

Sirtuin 1

SIRT6:

Sirtuin 6

TG:

Triglyceride

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Acknowledgements

The authors thank all co-authors of their papers that have been reviewed here.

Funding

This work was supported by the National Natural Scientific Fund of China (Nos. 81673736; 81803792) and the Natural Scientific Fund of Jiangsu (No. BK20171319) and Qing Lan Project of Jiangsu.

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Authors and Affiliations

  1. Department of Physiology, Hanlin College, Nanjing University of Chinese Medicine, Taizhou, 225300, Jiangsu, China

    Penghua Fang & Mei Yu

  2. Department of Endocrinology, Clinical Medical College, Yangzhou University, Yangzhou, 225001, Jiangsu, China

    Ping Bo & Zhenwen Zhang

  3. Jiangsu Key Laboratory of Integrated Traditional Chinese and Western Medicine for Prevention and Treatment of Senile Diseases, Medical College, Yangzhou University, Yangzhou, 225001, China

    Penghua Fang, Mingyi Shi & Ping Bo

  4. Department of Pathology, Clinical Medical College, Yangzhou University, Yangzhou, 225001, Jiangsu, China

    Xuewen Gu

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  1. Penghua Fang
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FP, YM, ZZ, GX and BP contributed equally to the preparation of the manuscript. Each author has approved the final version of the manuscript.

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Correspondence to Zhenwen Zhang.

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Fang, P., Yu, M., Shi, M. et al. Baicalin and its aglycone: a novel approach for treatment of metabolic disorders. Pharmacol. Rep 72, 13–23 (2020). https://doi.org/10.1007/s43440-019-00024-x

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