Baicalein

Baicalein is a flavone, a type of polyphenolic flavonoid, that is extracted from the roots of Scutellaria baicalensis and Scutellaria lateriflora (glidkruid) that have a wide variety of health benefits.

Baicalin is a flavone glycoside, the glucuronide of baicalein, which is obtained through the binding of glucuronic acid to baicalein. It is primarily used in Asian countries as an herbal supplement.

1) Baicalein and Baicalin Lowers Anxiety

Baicalein and baicalin inhibit the action potential of the neurons that raise anxiety (R).

In mice, baicalin produces anxiety-lowering effects without causing drowsiness or muscle relaxation (R).

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2) Baicalein and Baicalin are Neuroprotective

Baicalin improved cognitive dysfunction via its anti-neuroinflammatory activity, and may be a potential candidate for the treatment of Alzheimer’s Disease (AD) (R).

It improved Amyloid beta-induced learning and memory deficit, hippocampus injury and neuron apoptosis (R).

Baicalin improves learning and memory impairment induced by brain injury in mammals (R).

Treatment with this flavonoid, post-stroke, promotes neuron development in damaged sections of the brain, including the new formation of cells in the hippocampus (R).

3) Baicalein and Baicalin Fight Cancer

Short-term treatment (48 hours) with baicalein inhibits the proliferation of human ovarian cancer cells. An increase in cell death was observed when combined with Taxol (a chemotherapy drug) (R).

Baicalein suppressed proliferation, migration, and invasion of breast cancer cells in a time and dose-dependent manner. It had the potential to suppress breast cancer metastasis (R).

Baicalein, when ingested, is metabolized and inhibits the proliferation of human colorectal cancer cells (R).

It destroys the S cycle of colorectal cancer cells, which promotes cell death and prevents further replication (R).

Baicalin ingested at a dose of 100 mg/kg for 28 days decreases tumor growth and replication in mice with colon cancer cells (R).

When taken orally for 7 days it increases the activity of T helper cells and T regulatory cells to fight chemically-induced colon cancer (R).

Baicalin applied as a topical cream protects the skin with antioxidant effects. It also reduces UV-related apoptosis (cell death) (R1, R2).

4) Baicalin Protects the Liver

Baicalin administered in rats decreased the production of disease promoting proteins in the liver, reducing the effects of NAFLD (R).

It decreases cholesterol, alanine transaminase, low-density lipoproteins, and TNF levels.

Rats with alcohol-induced liver damage treated with this flavonoid before consuming alcohol had protective effects on the liver. It also decreased liver cell apoptosis (R).

5) Baicalin Improves Lung Function

Pure baicalin is successful at improving lung function in rats which suffer from allergic diseases (R).

When administered to rats suffering from asthma as a pretreatment, showed a healthy remodeling of the airway (R).

Baicalein reduces inflammation in silica-induced lung inflammation by inhibiting Th17 cells in the lungs (R).

6) Baicalein and Baicalin Help Your Eyes

Daily intake of baicalin or baicalein helps prevent eye diseases such as cataracts or age-related macular degeneration in animals (R).

Oral intake reduces stress on the eyes and muscles, decreasing the chance of contracting an eye disease (R).

7) Baicalin Improves Fertility

Baicalin significantly enhances endometrial reproduction (R).

In mice embryos, it increases development and quality of blastocysts (R).

REFERENCES

[1] Baicalein mediates inhibition of migration and invasiveness of skin carcinoma through Ezrin in A431 cells. Wu B, Li J, Huang D, Wang W, Chen Y, Liao Y, Tang X, Xie H, Tang F. Department of Dermatology, Xiangya Hospital, Central South University, Changsha 410008, P,R, China.

[2] Polyphenols and Neuroprotection against Ischemia and Neurodegeneration. Lin B. Department of Neurology, University of Miami, Miller School of Medicine, Miami, Florida, USA

[3] Baicalein inhibits oxidative stress-induced cellular damage via antioxidant effects. Kang KA, Zhang R, Piao MJ, Chae S, Kim HS, Park JH, Jung KS, Hyun JW. School of Medicine and Applied Radiological Science Research Institute, Jeju National University, Jeju, Korea.

[4] Role of phenolic compounds in peptic ulcer: An overview. Sumbul S, Ahmad MA, Mohd A, Mohd A. Department of Ilmul Advia (Pharmacology), Faculty of Unani Medicine, Hamdard University, New Delhi, India.

[5] Baicalein inhibits oxidative stress-induced cellular damage via antioxidant effects. Kang KA, Zhang R, Piao MJ, Chae S, Kim HS, Park JH, Jung KS, Hyun JW. School of Medicine and Applied Radiological Science Research Institute, Jeju National University, Jeju, Korea.

[6] Antidepressant effects of a plant-derived flavonoid baicalein involving extracellular signal-regulated kinases cascade. Xiong Z, Jiang B, Wu PF, Tian J, Shi LL, Gu J, Hu ZL, Fu H, Wang F, Chen JG. Department of Pharmacology, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.

[7] Mechanistic study of the structure-activity relationship for the free radical scavenging activity of baicalein. Marković ZS, Dimitrić Marković JM, Milenković D, Filipović N. Department of Biochemical and Medical Sciences, State University of Novi Pazar, Vuka Karadžića bb, Novi Pazar 36300, Republic of Serbia

[7] Baicalein significantly protects human retinal pigment epithelium cells against H₂O₂-induced oxidative stress by scavenging reactive oxygen species and downregulating the expression of matrix metalloproteinase-9 and vascular endothelial growth factor. Liu JH, Wann H, Chen MM, Pan WH, Chen YC, Liu CM, Yeh MY, Tsai SK, Young MS, Chuang HY, Chao FP, Chao HM. Department of Ophthalmology, Cheng Hsin General Hospital , Taipei, Taiwan, Republic of China.

[8] Inhibitory effects of baicalein on the influenza virus in vivo is determined by baicalin in the serum. Xu G, Dou J, Zhang L, Guo Q, Zhou C. School of Life Science & Technology, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing, Jiangsu 210009, P.R. China.

[9] The combination of baicalin and baicalein enhances apoptosis via the ERK/p38 MAPK pathway in human breast cancer cells. Zhou QM, Wang S, Zhang H, Lu YY, Wang XF, Motoo Y, Su SB. Research Center for Traditional Chinese Medicine Complexity System, Shanghai University of Traditional Chinese Medicine, Shanghai, China

[10] Cytotoxic effect of flavonoids on leukemia cells and normal cells of human blood. Romanouskaya TV, Grinev VV. Belarussian State University, Minsk, Belarussia.

[11] Selective fraction of Scutellaria baicalensis and its chemopreventive effects on MCF-7 human breast cancer cells. Wang CZ, Li XL, Wang QF, Mehendale SR, Yuan CS. Tang Center for Herbal Medicine Research, The Pritzker School of Medicine, University of Chicago, Chicago, IL 60637, USA.

[12] Baicalein induces proliferation inhibition in B16F10 melanoma cells by generating reactive oxygen species via 12-lipoxygenase. Chou DS, Hsiao G, Lai YA, Tsai YJ, Sheu JR. Department of Pharmacology, Taipei Medical University, Taipei, Taiwan.

[13] Baicalein exerts neuroprotective effects in 6-hydroxydopamine-induced experimental parkinsonism in vivo and in vitro. Mu X, He G, Cheng Y, Li X, Xu B, Du G. Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

[14] Synergistic anti-cancer effect of baicalein and silymarin on human hepatoma HepG2 Cells. Chen CH, Huang TS, Wong CH, Hong CL, Tsai YH, Liang CC, Lu FJ, Chang WH. Graduate Institute of Biomedical and Biopharmaceutical Sciences, College of Life Sciences, National Chiayi University, 300 Syuefu Road, Chiayi 600, Taiwan.

[15] Baicalein induces apoptosis in SCC-4 human tongue cancer cells via a Ca2+-dependent mitochondrial pathway. Lin YT, Yang JS, Lin HJ, Tan TW, Tang NY, Chaing JH, Chang YH, Lu HF, Chung JG. Department of Nursing and Management, Jen-Teh Junior College of Medicine, Taiwan, ROC.

[16] Scutellaria baicalensis and a constituent flavonoid, baicalein, attenuate ritonavir-induced gastrointestinal side-effects. Mehendale S, Aung H, Wang CZ, Tong R, Foo A, Xie JT, Yuan CS. Tang Center for Herbal Medicine Research, The Pritzker School of Medicine, University of Chicago, Chicago, IL 60637, USA.

[17] Baicalein improves cognitive deficits induced by chronic cerebral hypoperfusion in rats. Liu C, Wu J, Gu J, Xiong Z, Wang F, Wang J, Wang W, Chen J. Department of Pharmacology, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, PR China.

[18] Studies on the constituents of roots of Scutellaria planipes. Zhang YY, Guo YZ, Ageta H, Harigaya Y, Onda M, Hashimoto K, Ikeya Y, Okada M, Maruno M. Shenyang Pharmaceutical University, Shenyang 110015, China.

[19] Baicalein, a flavonoid extracted from a methanolic extract of Oroxylum indicum inhibits proliferation of a cancer cell line in vitro via induction of apoptosis. Roy MK, Nakahara K, Na TV, Trakoontivakorn G, Takenaka M, Isobe S, Tsushida T. National Food Research InstituteFood Function Laboratory, Tsukuba, Japan.