Baicalin

Baicalin is a phytochemical and bioflavonoid found in the Baikal Skullcap plant. [1, 2] It has been used in Traditional Chinese Medicine (TCM) for hundreds of years. It has well-established antioxidant and anti-inflammatory properties and acts as a GABA agonist to promote calmness, relaxation, and healthy sleep. [3, 4, 5]

 

 

Benefits and Effects on Humans

Based on Available Scientific Research and Anecdotal Evidence

Used For:	Efficacy
Reducing Stress	★★★★★
Cognitive Enhancement	★★★★
Improving Mood	★★★★
Natural sleep aid	★★★★
Neuroprotective	★★★
Synergy with caffeine	★★★★★
Supporting a healthy metabolism	★★★

 

 

How to Use

Recommended Serving Size and Application

 

Serving size

For a potent, 95-99+% purity extract, the optimal serving size is between 250 – 750 mg, taken once to twice daily.

 

Application

 

1.  ‘Toss-and-wash’ method:
   1. Measure the correct serving size of Baicalin with a measuring scoop or scale.
   2. Pour this onto a credit card, spoon, or piece of paper.
   3. Toss the powder into the back of your mouth.
   4. Wash it down with a glass of water.

 

2. Baicalin breakfast smoothie:

1. 1. Measure the correct serving size of Baicalin with a measuring scoop or scale.
   2. Cut up 3-4 servings of your favorite fruits – bananas, apples, berries, dates, or oranges.
   3. Add the Baicalin powder and fruit into a blender.
   4. Add 1 glass of water or fruit juice.
   5. Blend until smooth and drinkable.
   6. Enjoy as a healthy breakfast smoothie.

 

Evidence-Based Research

 

1. Summary

Baicalin is an active component of Chinese Skullcap (sometimes referred to as Scutellaria baicalensis, Huang qin, or Scutellariae radix). It has a long history of use in Chinese herbal medicine from over 1000 years ago, where Baicalin was extracted using ethanol. It is a metabolite of the flavonoid Baicalein, which is also found in the Skullcap species and the two molecules have synergistic properties.[1] [2]

Baikal Skullcap extract is best known for its potent antioxidant and anti-inflammatory effects, while also supporting a healthy circulatory system and promoting stress-reduction as well as a relaxed state of mind. [1 – 5]

Baicalin supplementation is beneficial in a wide variety of ways. It can help to promote a feeling of healthy well-being and promote a healthy circulatory system. [3] Many people also use this supplement to help reduce stress, improve sleep, and to promote feelings of calmness and relaxation.[4][5]

The Chinese Skullcap plant contains a number of active compounds, of which Baicalin is the most active in humans. Important phytochemicals found in the Skullcap plant include: [1] [6]

• Baicalin (Baicalein-7-glucuronide) and Baicalein, as well as another glycoside known as baicalein-7-O-glucoside.
• Wogonoside (wogonin-7-glucuronide) and Wogonin, as well as another glycoside known as Wogonin-5-O-glucoside.
• Oroxylin A (5,7-dihydroxy-6-methoxyflavone) and 7-O-glucoside.
• Neobaicalein, Scutellarin and Isoscutellarein.
• Chrysin
• Viscidulin I and Visdulin III
• Skullcapflavone I and II

 

The recommended serving size for this supplement is between 250 – 750 mg, taken once to two times per day. Adverse effects are said to be very mild and rare if present at all. However, larger serving sizes may increase the chances of experiencing adverse effects. Do not exceed the recommended serving size for this supplement. Please speak to your doctor if you’re using any medication or have any underlying medical conditions.

 

 

2. Human Effects

2.1. Powerful Anti-inflammatory & Immune Supporting Effects

One of the best-known benefits of this great natural dietary supplement is its ability to act as a powerful anti-inflammatory agent. More specifically, research indicates that Baicalin targets inflammation in the body, thereby helping to promote good health.[7] In several animal model and cell-line studies, researchers have used Baicalin to effectively reduce inflammation markers.[8]

Reducing inflammation is a great way to promote good health. However, unhealthy lifestyle habits can cause an increase in inflammation in the body because inflammation is quite often the body’s response to threats. Indeed, when the immune system detects toxins, stressors, or infectious agents, it responds with inflammation, which is the immune system’s defense mechanism taking effect. If the immune system is in a constant battle against toxins and stressors, it can be very detrimental to your health, and this has been linked to numerous health issues such as gut problems, sleep disturbances, mood changes, joint problems, and even heart disease.[9]

In terms of the underlying biochemical mechanisms, this supplement has been found to inhibit the binding of leukocytes to chemokines and to disrupt cell migration (a characteristic cause of inflammation). However, it does not interfere directly with chemokines but rather binds to chemokine ligands to prevent chemokine-leukocyte binding.[10]

 

2.2. Anti-Stress and Calming Benefits

Baicalin is a fascinating supplement that is known for its ability to help alleviate feelings of stress and promote a relaxed state of mind. A very similar compound, Baicalein (also found in the Chinese Skullcap) has been shown to bind to GABA receptors, which is known to promote relaxation.[11] However, Baicalin’s calming effects may not work through this same mechanism.

In fact, the mechanisms behind this supplement’s stress-reducing effects are not yet fully understood. Nevertheless, Baicalin supplementation has definitely demonstrated the potential to help reduce stress.[12] In animal models, for example, both this supplement and its glycoside Baicalein were found to effectively lessen stress due to its anxiolytic-like properties.[13] In other studies, Baicalin was compared to other well-known stress-reducing compounds such as L-Tetrahydropalmatine (L-THP), and it was found to have potent relaxation-promoting effects.[14]

Through additional research, scientists have demonstrated that Baicalin acts on the GABA_A receptor, specifically at the receptor’s benzodiazepine (BZ) site, although this effect may be very mild ⁵. Nevertheless, this supplement is known for its ability to induce stress-reduction and improve mood without causing sedation or muscle relaxation that is characteristic of most GABA agonists.[15] This means that Baicalin provides the same relaxing feelings as other substances (e.g. L-THP), but it does not cause unpleasant side effects such as drowsiness.

 

2.3. Potent Antioxidant – Bioflavonoid

Recent studies regarding the effects of this great dietary supplement for health have also pointed to its powerful antioxidant properties. In a 2000 study that evaluated the antioxidant activity of Baicalin, Baicalein, and Wogonin (all of which are extracts from the Skullcap species), researchers found that the Baicalin effectively reduced the levels of cytochrome c and eliminated superoxide free-radicals, thereby demonstrating its powerful antioxidant nature.[16]

Free-radicals are reactive chemical compounds in the body that form during a chemical reaction with oxygen. They form naturally as a part of the body’s metabolic system but are also generated in response to unhealthy lifestyle choices that include smoking and excessive alcohol consumption. Free-radicals react with important cellular components such as DNA or the cell membrane, which can cause apoptosis (cell death). In response to free radicals, the body uses antioxidants to protect cells against these harmful agents.[17]

Natural antioxidants include Vitamin E, Vitamin C, and Beta-Carotene (Vitamin A), all of which are found in high concentrations in plant foods such as fruits and vegetables. Research has shown that people who consume more vegetables and fruits tend to experience enhanced health benefits due to the increased intake of minerals, vitamins, and antioxidants. [18]

Increasing your intake of antioxidants is definitely a great way to improve vitality and well-being. Interestingly, recent research has indicated that Baicalin has far greater free-radical scavenging (antioxidant) benefits than other natural antioxidants such as Vitamin C as well as the synthetic antioxidant butylated hydroxytoluene (BHT). [19]

 

2.4. Supports a Healthy Circulatory System

Recently, interesting research has pointed to Baicalin’s ability to help support a healthy circulatory system. There are a few mechanisms through which this supplement provides this benefit.

Firstly, scientists have found that Baicalin can enhance the phosphorylation of the AMPK enzyme.[20] This effect may help to regulate the levels of hormones found in the blood. AMPK activation is known to help regulate hormone levels as well as to reduce the formation of fat. [21] Indeed, research has shown that animals that were given this supplement over a long period of time (16 weeks) had reduced fat content compared to animals that received a placebo. [22]

Secondly, research suggests that this Baicalin may help to support a healthy circulatory system through its ability to stimulate the synthesis of nitric oxide (NO).[23] Nitric oxide is responsible for a number of effects on the circulatory system, but most significantly vasodilation (increasing the diameter of blood vessels) which allows for better blood circulation.[24] Furthermore, animal studies have indicated that this supplement may help regulate the levels of hormones in the body and to promote a healthy metabolism.[25]

 

2.5. Further Use in Research

Baicalin is being used in a number of studies that are focussing on its potential future benefits for human health. Many of these studies are still very preliminary in their nature. However, it is important that prospective users of Baicalin be made aware of the ongoing research that is being conducted on this highly interesting natural phytochemical.

Significant in vitro research is being conducted on this supplement and similar antioxidant derivatives, with a focus on their potential future use for suppressing the growth of malignant cell lines. For example, a recent study – published in the Cancer Letters journal in 2014 – pointed to an interesting possibility for further research that focuses on reducing the growth of hematologic malignancies.[26]

Furthermore, research that involves the evaluation of potentially using Baicalin to target bacterial infections and viral replication is currently being conducted. For example, recent in vitro and in vivo studies focused on the dose-dependent inhibitory effects of Baicalin on virulence phenotypes in the Pseudomonas aeruginosa bacteria due to the ability of this supplement to reduce biofilm formation.[27] Furthermore, some studies have pointed to a synergistic relationship of Baicalin with oxytetracycline and tetracycline antibiotics against Staphylococcus aureus infections including methicillin- and tetracycline-resistant strains. [28]

 

3. Safety and Toxicity

3.1. Side Effects

Even after hundreds of years of use in TCM remedies, this supplement only appears to be associated with very few noticeable adverse effects when it is used in accordance with the recommended serving sizes. WebMD (a well-known medical advice website) suggests that there is not enough information currently available to assess this supplement’s potential for adverse effects. However, any adverse effects are likely to become more noticeable at larger serving sizes. [29]

There is not enough information regarding the safety of this supplement for women who are pregnant or breastfeeding. If you have any underlying medical conditions, please consult with your doctor before using this supplement. Do not take Baicalin supplements if you are using any prescription or OTC medication. Do not exceed the recommended serving size for this supplement.

 

 

Scientific Support and References:

 

[1] Bochoráková, H., Paulová, H., Slanina, J., Musil, P., Táborská, E. (2003). Main flavonoids in the root of Scutellaria baicalensis cultivated in Europe and their comparative antiradical properties. Phytother Res, 17(6):640-4.

[2] Gao, Z., Huang, K., Yang, X., Xu, H. (1999). Free radical scavenging and antioxidant activities of flavonoids extracted from the radix of Scutellaria baicalensis Georgi.  Biochim Biophys Acta, 1472(3):643-50.

[3] Huang, S., Chen, P., Shui, X., et al. (2014). Baicalin attenuates transforming growth factor-β1-induced human pulmonary artery smooth muscle cell proliferation and phenotypic switch by inhibiting hypoxia inducible factor-1α and aryl hydrocarbon receptor expression. J Pharm Pharmacol. 2014;66(10):1469-77.

[4] Zhao, Q., Chen, X.Y., Martin C. (2016). Scutellaria baicalensis, the golden herb from the garden of Chinese medicinal plants. Sci Bull (Beijing). 2016;61(18):1391-1398.

[5] Hui, K.M., Wang, X.H., Xue, H. (2000). Interaction of flavones from the roots of Scutellaria baicalensis with the benzodiazepine site. Planta Med. 2000; 66(1):91-3.

[6] Wang, H., Hui, K.M., Chen, Y., Xu, S., Wong, J.T., Xue, H. (2002). Structure-activity relationships of flavonoids, isolated from Scutellaria baicalensis, binding to benzodiazepine site of GABA(A) receptor complex. Planta Med, 68(12):1059-62.

[7] Lee, W., Ku, S.K., Bae, J.S. (2015). Anti-inflammatory effects of Baicalin, Baicalein, and Wogonin in vitro and in vivo. Inflammation. 38(1):110-25

[8] Guo, M., Zhang, N., Li, D., Liang, D., Liu, Z., Li, F., Fu, Y., Cao, Y., Deng, X., Yang, Z. (2013). Baicalin plays an anti-inflammatory role through reducing nuclear factor-κB and p38 phosphorylation in S. aureus-induced mastitis. Int Immunopharmacol, 16(2):125-30.

[9] Minihane, A.M., Vinoy, S., Russell, W.R., et al. (2015). Low-grade inflammation, diet composition and health: current research evidence and its translation. Br J Nutr, 114(7):999-1012.

[10] Li, B.Q., Fu, T., Gong, W.H., Dunlop, N., Kung, H., Yan, Y., Kang, J., Wang, J.M. (2000).  The flavonoid baicalin exhibits anti-inflammatory activity by binding to chemokines. Immunopharmacology. 49(3):295-306.

[11] de Carvalho, R.S., Duarte, F.S., de Lima, T.C. (2011). Involvement of GABAergic non-benzodiazepine sites in the anxiolytic-like and sedative effects of the flavonoid baicalein in mice. Behav Brain Res, 221(1):75-82

[12] New use of baicalin for treating anxiety WO2004103386A1, WO Application, Patent, available online from https://patents.google.com/patent/WO2004103386A1/en

[13] Liao, J.F., Hung, W.Y., Chen, C.F. (2003). Anxiolytic-like effects of baicalein and baicalin in the Vogel conflict test in mice. Eur J Pharmacol. 464(2-3):141-6.

[14] Xu, Z., Wang, F., Tsang, S.Y., Ho, K.H., Zheng, H., Yuen, C.T., Chow, C..Y, Xue, H. (2006). Anxiolytic-Like Effect of baicalin and its additivity with other anxiolytics. Planta Med, 72(2):189-92.

[15] Wang, F., Xu, Z., Ren, L., Tsang, S.Y., Xue, H. (2008). GABA A receptor subtype selectivity underlying selective anxiolytic effect of baicalin. Neuropharmacology. 55(7):1231-7

[16] Shieh, D.E., Liu, L.T., Lin, C.C. (2000). Antioxidant and free radical scavenging effects of baicalein, baicalin, and wogonin. Anticancer Research, 20(5A):2861-2865.

[17] Pham-Huy, L.A., He, H., Pham-Huy, C. (2008). Free radicals, antioxidants in disease and health. Int J Biomed Sci, 4(2):89-96.

[18] Dinu, M., Abbate, R., Gensini, G.F., Casini, A., Sofi, F. (2017). Vegetarian, vegan diets and multiple health outcomes: A systematic review with meta-analysis of observational studies. Crit Rev Food Sci Nutr, 57(17):3640-3649.

[19] Peng-fei, L., Fu-gen, H., Bin-bin, D., Tian-sheng, D., Xiang-lin, H., Ming-qin, Z. (2013). Purification and antioxidant activities of baicalin isolated from the root of huangqin (Scutellaria baicalensis gcorsi). Journal of Food Science and Technology, 50(3):615-619.

[20] Ma, Y, Yang, F., Wang, Y., Du, Z., Liu, D., Guo, H., Shen, J., Peng, H. (2012). CaMKKβ is involved in AMP-activated protein kinase activation by baicalin in LKB1 deficient cell lines. PLoS One, 7(10):e47900.

[21] Kim, J., Yang, G., Kim, Y., Kim, J., Ha, J. (2016). AMPK activators: mechanisms of action and physiological activities. Experimental & Molecular Medicine, 48(4):e224.

[22] Guo, H.X., Liu, D.H., Ma, Y., Liu, J.F., Wang, Y., Du, Z.Y., Wang, X., Shen, J.K., Peng, H.L. (2009). Long-term baicalin administration ameliorates metabolic disorders and hepatic steatosis in rats given a high-fat diet. Acta Pharmacol Sin. 30(11):1505-12.

[23] Chen, Z., Nihei, K., Tanaka, H., Uda, Y., Kabuyama, Y. (2013). Identification of a nitric oxide generation-stimulative principle in Scutellariae radix. Biosci Biotechnol Biochem, 77(3):657-9.

[24] Chen, K., Pittman, R.N., Popel, A.S. (2008). Nitric oxide in the vasculature: where does it come from and where does it go? A quantitative perspective. Antioxid Redox Signal, 10(7):1185-98.

[25] Song, K.H., Lee, S.H., Kim, B.Y., Park, A.Y., Kim, J.Y. (2013). Extracts of Scutellaria baicalensis reduced body weight and blood triglyceride in db/db Mice. Phytother Res, 27(2):244-50.

[26] Chen, H., Gao, Y., Wu, J., Chen, Y., Chen, B., Hu, J., Zhou, J. (2014). Exploring Therapeutic Potentials of Baicalin and Its Aglycone Baicalein for Hematological Malignancies. Cancer letters, 354(1):5-11.

[27] Luo, J., Dong, B., Wang, K., Cai, S., Liu, T., Cheng, X., Lei, D., Chen, Y., Li, Y., Kong, J., Chen, Y. (2017). Baicalin inhibits biofilm formation, attenuates the quorum sensing-controlled virulence and enhances Pseudomonas aeruginosa clearance in a mouse peritoneal implant infection model. Seleem MN, ed. PLoS ONE, 12(4):e0176883.

[28] Novy, P., Urban, J., Leuner, O., Vadlejch, J., Kokoska, L. (2011). In vitro synergistic effects of baicalin with oxytetracycline and tetracycline against Staphylococcus aureus. J Antimicrob Chemother, 66(6):1298-300.

[29] “Skullcap”, WebMD.com, available online from https://www.webmd.com/vitamins-supplements/ingredientmono-986-skullcap.aspx?activeingredientid=986&activeingredientname=skullcap [Accessed February 8, 2019]