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Baicalein

  • Calming and Anti-Stress
  • Powerful Anti-inflammatory
  • Supports a Healthy Circulatory System

 

Abstract

 

Baicalein (5,6,7 trihydroxyflavone) is the primary active component from the Baikal Skullcap (Blue Skullcap). This powerful phytochemical is best known for its effects on GABA receptors and corresponding anti-stress and relaxation-promoting effects. It is also a powerful anti-inflammatory and antioxidant supplement and helps to promote a healthy circulatory system.

 

The recommended serving size for this supplement is around 200 – 350 mg, taken once to twice per day. Skullcap extracts have been used for centuries as traditional remedies for health. However, this supplement contains a very powerful isolated compound and should be used correctly. Do not exceed the recommended serving size. Do not use if you are taking medication.

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Baicalein Reviews

 

 

 

  • Baicalein is the aglycone derivative of Baicalin, and both compounds occur in the herb called Blue Skullcap, Scutellaria baicalensis.

  • This compound has 2-3 times better efficacy than Baicalin and is best known for its calming and anti-stress benefits, as well as its antioxidant and anti-inflammatory effects.

  • Recommended serving size is 200 – 350 mg, taken once to twice per day.  
  • Do not exceed the recommended serving size for this supplement, and do not use if you are taking medication

     

 

Background

 

Baicalein (5,6,7 trihydroxyflavone, Skullcap, Huang qin, Scutellariae radix, Golden root, Scutellaria baicalensis) is one of two key active components of the Skullcap plant, with a long history of use in Traditional Chinese Medicine (TCM). Baicalein and Baicalin are very similar compounds, with similar effects. This compound has been shown to have a better bioavailability when taken by mouth but is more difficult and costly to produce.

 

Scutellaria baicalensis, the plant that researchers originally derived this supplement from, is a member of the mint family. In China and Japan, traditional healers have used this plant for the treatment of a number of ailments, and in the tonics Huang qin (China) and Sho-saiko-to (Japan). Over 50 alkaloids have been identified in the Skullcap plant, but Baicalein and Baicalin appear to be the most effective for health benefits.[1]

 

Today, this compound is available online as a health-promoting supplement used for its antioxidant, anti-inflammatory, and anti-stress benefits. Numerous animal studies have confirmed these results, but there is still room for further investigation into its benefits for humans. As a result, there is rapidly growing scientific interest in this compound and scientists around the world are conducting studies to further elucidate its potential future benefits.[2]

 

Baicalein vs. Baicalin

 

So, what is the difference between Baicalein and Baicalin? In terms of their origin, both these compounds are found naturally in the Blue Skullcap plant. Their key difference lies in the chemical structure. Baicalin is called the gluconuride derivative of Baicalein and is the most common form in plants. When people take plant extracts that are high in Baicalin content, the chemical gets converted into Baicalein in the gut.

 

In terms of its effects, Baicalein tends to be around 2-3 times more effective (in terms of absorption). However, manufacturing this compound is around 3-4 times more costly than the naturally occurring form. That’s not to say that Baicalein doesn’t occur in plants. Baicalin just occurs at a greater concentration, making it easier (and cheaper) to produce. In terms of its effects, Baicalein has very similar benefits to Baicalin. Interestingly, many human studies have preferred using the more expensive form due to its better bioavailability.

 

baicalein-for-mood

Baicalein Effects & Benefits

 

1.     Promotes Relaxation and Calming 

 

This powerful phytochemical has a strong ability to help reduce feelings of stress and to promote relaxation. These effects are attained primarily through its interactions with GABA receptors in the brain, primarily GABA-A sub-types.[3] Baicalin has not been shown to have any effects on these receptors. However, it is converted into Baicalein in the gut and is therefore believed to have similar effects, albeit at a lower efficacy.[4]

 

For those interested in the scientific particulars, this compound has the greatest affinity for α2- and α3-containing subtypes of the GABA-A receptors.[5] Animal studies have shown powerful calming and stress-reducing effects, even at low serving sizes. These benefits are known to occur without the usual side-effects of sedation or muscle relaxation, making it a potentially very useful natural stress-reducing supplement. [6]

 

Although studies have suggested that sedative-like side-effects are not felt, research has shown that this supplement can help to improve sleep quality. Animal studies have shown that this supplement increased sleep time by 108 – 120% compared to the control groups.[7]

 

2.     Powerful Anti-inflammatory Benefits   

 

Skullcap extracts are well-known for their ability to help fight inflammation. Both the active components of this powerful plant species have been shown to possess potent anti-inflammatory effects.[8] Inflammation is the body’s response to illness, infections, and injuries. Inflammation is sometimes visible around cuts and sores, as red, warm, and swollen area. Throat infections can also cause inflammation, experienced as redness and a scratchy feeling in the throat.[9]

 

However, internal inflammation – especially in the blood vessels – is often not felt directly. This kind of inflammation results primarily from lifestyle choices like poor diet, lack of sufficient exercise, smoking, and drinking.[10] Anti-inflammatory substances help to limit inflammation in the circulatory system. If you’re interested in learning about the science behind how this supplement helps to suppress inflammation, here’s some information for you:

 

Studies show that both the active components found in Blue Skullcap are effective at temporarily acting on estrogen receptors and suppressing the activation of NF-kB enzymes – which trigger the body to produce inflammation-causing cytokines.[11]  Secondary effects involve suppressing the activity of macrophages (‘fighter cells’ involved in immune response) and acting on oestrogen receptors.[12]

 

3.     Potent Antioxidant Effects 

 

Researchers have known about the powerful antioxidant effects of this natural supplement for some time already. Antioxidants are substances that prevent oxidation reactions with ‘free-radical’ compounds in the body. Free-radicals are produced from natural biochemical processes within the body, and your body has a host of natural antioxidant compounds to keep these in check.[13] However, lifestyle choices and environmental factors like pollution can result in the production of excess free-radicals.[14] These can be dangerous if they react with cellular or mitochondrial DNA, which is where antioxidant supplements come into play.

 

Recent studies have indicated that this supplement is able to attenuate mitochondrial oxidative stress by destroying reactive oxygen species (ROS) and by activating certain transcription factors, thereby inhibiting the DNA damage that usually occurs as a result of reactions with free-radicals like ‘superoxide’.[15] Further studies have indicated that this supplement can help to protect against a process called lipid peroxidation, which is involved in the formation of ‘bad’ LDL-cholesterol, thereby supporting a healthy circulatory system and protecting important cellular components.[16]

 



Importantly, according to the US Department of Health, decades of research has shown that antioxidant supplements alone do not necessarily protect against negative health problems.[17] Antioxidants are best taken in addition to a healthy diet that is rich in fruits and vegetables, alongside sufficient exercise. There is no magic bullet for health, and although antioxidant supplements are effective at supporting a healthy body, their effects are always more noticeable when used IN ADDITION to healthy lifestyle choices.

 

4.     Helps to Support Healthy Cognitive Function 

 

Researchers have spent a lot of time looking into the potential benefits of Scutellaria baicalensis extracts for learning, memory, and attention. The results point toward positive benefits for cognitive performance. For example, one study examined the benefits of using Scutellaria baicalensis extracts to counteract the negative effects of ibotenic acid – a potent neurotoxin. The results showed effective protection against the memory-depleting effects of the toxin.[18]

 

Further research looked into the protective effects on memory against numerous toxins, including beta-amyloid proteins,[19] chronic lipopolysaccharide infusion[20], ischemia (reduced blood flow to the brain),[21] and animal models of ageing.[22] All these studies pointed towards protection of memory and support of cognitive functions, to various degrees. As a result, researchers now consider this supplement to be an effective natural cognitive enhancer, comparable to some Nootropic compounds.[23]

 

5.     Helps to Support a Healthy Circulatory System

 

As a result of developments in understanding this supplement’s antioxidant and anti-inflammatory effects, researchers began trying to understand its potential benefits for supporting a healthy circulatory system. Theoretically, any supplement with potent antioxidant and anti-inflammatory effects should have the potential to help support a healthy circulatory system.

 

A few studies have been published on this topic. In one study, researchers used the powerful anti-inflammatory effects of this supplement as a basis for their research, which looked into its potential to protect endothelial function and to protect against oxidative stress-induced cellular injury. They found that it helps to support a healthy circulatory system, but may have unwanted interactions with a variety of medicines.[24] In another study, researchers found that its effects against reactive oxygen species (ROS) helped to confer protective effects to the circulatory system.[25]

 

6.     Further Use in Research

 

Researchers are using this supplement compound to explore potential therapeutic options in future. Most of the studies being conducted are still very preliminary but are interesting nonetheless. Note that there is not yet conclusive evidence to determine the efficacy of this supplement for the uses being researched. Scutellaria baicalensis extracts, and the active components, are sold as dietary supplements and are not intended to treat, cure, or diagnose any disease or ailment.

 

Some research is being conducted using human cell-lines to determine this supplement’s effects on the immune system.[26] Further research is currently underway to explore the effects of the active compounds found in Skullcap extracts on human cancer cell lines.[27] Some research shows that there may be a potential for developing this compound for skin protection, in the future.[28] Finally, researchers are examining the potential use of this compound against a variety of forms of bacteria, especially in the destruction of bacterial cells walls of Staphylococcus aureus.[29]

 

baikal-skullcap-chinese-medicine

Baicalein Recommended Usage

 

There is still room for further research into the effects of this supplement in humans, and to find the ideal serving size. Most studies suggest that a serving size of around 100 - 250 mg of strong Baicalein is sufficient to experience the benefits of this fine supplement.

 

There is a big difference between taking a Skullcap extract and a 95+% pure Baicalein supplement. Skullcap extracts are expressed as a multiple – for example, 10x, 20x, 30x extract, and so on. It is difficult to standardise the concentration of active compounds in a plant extract, which is why we sell this high-quality, standardised compound (as opposed to an extract form).

 

Baicalein Side Effects & Warnings

 

Skullcap extracts have been used for hundreds of years in Traditional Chinese Medicine. In this natural form, very few side effects have been said to occur, if any. However, this supplement is a much stronger form and contains a very high concentration of potent Baicalein. Therefore, it is important to use this supplement correctly. Do not exceed the recommended serving size.

WebMD, a conservative source of information about supplements and medicines, states that Baikal Skullcap is POSSIBLY SAFE for use by most adults when taken by mouth. An intravenous preparation that included Skullcap was given to children for 7 days and did not produce any noticeable side effects.[30]

 

It is very important to consult your doctor before using this supplement if you have any underlying medical conditions. This supplement may affect people with bleeding disorders, diabetes, low blood pressure, and hormone-sensitive disorders. Additionally, it may not be safe to use before surgery. If you are taking any medication, do not use this supplement without first speaking to your doctor. There may be a potential for adverse effects resulting from interactions between this supplement and medicine.

There is not enough information regarding the safety of this supplement for women who are pregnant or breastfeeding. Do not exceed the recommended serving size for this supplement.

 

baicalein-for-circulatory-system

Conclusion

 

In summary, this supplement is a powerful isolated active alkaloid compound from the Blue Skullcap plant species, which is endemic to China. It is effective as an anti-stress supplement to help promote relaxation and has strong health-promoting benefits due to its antioxidant and anti-inflammatory effects in the body. Research suggests that, when taken in addition to a healthy diet and lifestyle, this supplement can help support a healthy circulatory system.



The recommended serving size is 200 – 350 mg, once to twice per day. It is not recommended to exceed the serving size for this supplement, due to the low number of human studies conducted and the strength of the compound. If you have any underlying medical conditions or are using any medication, please speak to your doctor before using this supplement.

 

References

 



[1] Donald G, Hertzer K, Eibl G. Baicalein – An Intriguing Therapeutic Phytochemical in Pancreatic Cancer. Current drug targets. 2012;13(14):1772-1776.

[2] Scutellaria baicalensis, Examine.com, available online from https://examine.com/supplements/scutellaria-baicalensis/ [Accessed 15 June 2018]

[3] Wang H, Hui KM, Xu S, Chen Y, Wong JT, Xue H. Two flavones from Scutellaria baicalensis Georgi and their binding affinities to the benzodiazepine site of the GABAA receptor complex. Pharmazie. 2002 Dec;57(12):857-8.

[4] Yoon SY1, dela Peña IC, Shin CY, Son KH, Lee YS, Ryu JH, Cheong JH, Ko KH. Convulsion-related activities of Scutellaria flavones are related to the 5,7-dihydroxyl structures. Eur J Pharmacol. 2011 Jun 1;659(2-3):155-60

[5] Wang F, Xu Z, Ren L, Tsang SY, Xue H. GABAA receptor subtype selectivity underlying selective anxiolytic effect of Baicalin. Neuropharmacology, Volume 55, Issue 7, December 2008, Pages 1231-1237

[6] Yu X, He GR, Sun L, Lan X, Shi LL, Xuan ZH, Du GH. Assessment of the treatment effect of baicalein on a model of Parkinsonian tremor and elucidation of the mechanism. Life Sci. 2012 Jul 26;91(1-2):5-13

[7] de Carvalho RS, Duarte FS, de Lima TC. Involvement of GABAergic non-benzodiazepine sites in the anxiolytic-like and sedative effects of the flavonoid baicalein in mice. Behav Brain Res. 2011 Aug 1;221(1):75-82

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

ment to help promote relaxation,frome online from oment. u have any underlying medical conditions or are using any medication, p

[9] Everything you need to know about inflammation. By Christian Nordqvist, Medical News Today, available from https://www.medicalnewstoday.com/articles/248423.php [Accessed 15 June, 2018]

[10] Inflammation and Heart Disease. American Heart Association. Available online from http://www.heart.org/HEARTORG/Conditions/Inflammation-and-Heart-Disease_UCM_432150_Article.jsp#.WyPAi1OWQxh [Accessed 15 June, 2018]

[11] Patwardhan RS, Sharma D, Thoh M, Checker R, Sandur SK. Baicalein exhibits anti-inflammatory effects via inhibition of NF-κB transactivation. Biochem Pharmacol. 2016 May 15;108:75-89.

[12] Fan GW1, Zhang Y, Jiang X, Zhu Y, Wang B, Su L, Cao W, Zhang H, Gao X. Anti-inflammatory activity of baicalein in LPS-stimulated RAW264.7 macrophages via estrogen receptor and NF-κB-dependent pathways. Inflammation. 2013 Dec;36(6):1584-91.

[13] Lobo V, Patil A, Phatak A, Chandra N. Free radicals, antioxidants and functional foods: Impact on human health. Pharmacognosy Reviews. 2010;4(8):118-126.

[14] Pham-Huy LA, He H, Pham-Huy C. Free Radicals, Antioxidants in Disease and Health. International Journal of Biomedical Science : IJBS. 2008;4(2):89-96.

[15] Shieh DE, Liu LT, Lin CC. Antioxidant and free radical scavenging effects of baicalein, baicalin and wogonin. Anticancer Res. 2000 Sep-Oct;20(5A):2861-5.

[16] Kang KA, Zhang R, Piao MJ, Chae S, Kim HS, Park JH, Jung KS, Hyun JW. Baicalein inhibits oxidative stress-induced cellular damage via antioxidant effects. Toxicol Ind Health. 2012 Jun;28(5):412-21.

[17] Antioxidants: In Depth, US Department of Health, NCCIH.gov, available from https://nccih.nih.gov/health/antioxidants/introduction.htm [Accessed June 15, 2018]

[18] Heo H, Shin Y, Cho W, Choi Y, Kim H, Kwon YK. Memory improvement in ibotenic acid induced model rats by extracts of Scutellaria baicalensis. J Ethnopharmacol. 2009 Feb 25;122(1):20-7.

[19] Kim DH, Kim S, Jeon SJ, Son KH, Lee S, Yoon BH, Cheong JH, Ko KH, Ryu JH. The effects of acute and repeated oroxylin A treatments on Abeta(25-35)-induced memory impairment in mice. Neuropharmacology. 2008 Oct;55(5):639-47

[20] Hwang YK1, Jinhua M, Choi BR, Cui CA, Jeon WK, Kim H, Kim HY, Han SH, Han JS. Effects of Scutellaria baicalensis on chronic cerebral hypoperfusion-induced memory impairments and chronic lipopolysaccharide infusion-induced memory impairments. J Ethnopharmacol. 2011 Sep 1;137(1):681-9

[21] Shang Y, Cheng J, Qi J, Miao H. Scutellaria flavonoid reduced memory dysfunction and neuronal injury caused by permanent global ischemia in rats. Pharmacol Biochem Behav. 2005 Sep;82(1):67-73. Epub 2005 Aug 29.

[22] Song HR, Cheng JJ, Miao H, Shang YZ. Scutellaria flavonoid supplementation reverses ageing-related cognitive impairment and neuronal changes in aged rats. Brain Inj. 2009 Feb;23(2):146-53.

[23] Shang YZ, Gong MY, Zhou XX, Li ST, Wang BY. Improving effects of SSF on memory deficits and pathological changes of neural and immunological systems in senescent mice. Acta Pharmacol Sin. 2001 Dec;22(12):1078-83.

[24] Huang Y, Tsang SY, Yao X, Chen ZY. Biological properties of baicalein in cardiovascular system. Curr Drug Targets Cardiovasc Haematol Disord. 2005 Apr;5(2):177-84.

[25] Chen H-M, Hsu J-H, Liou S-F, et al. Baicalein, an active component of Scutellaria baicalensis Georgi, prevents lysophosphatidylcholine-induced cardiac injury by reducing reactive oxygen species production, calcium overload and apoptosis via MAPK pathways. BMC Complementary and Alternative Medicine. 2014;14:233.

[26] Deschamps JD, Kenyon VA, Holman TR. Baicalein is a potent in vitro inhibitor against both reticulocyte 15-human and platelet 12-human lipoxygenases. Bioorg Med Chem. 2006 Jun 15;14(12):4295-301

[27] Miocinovic R, McCabe NP, Keck RW, Jankun J, Hampton JA, Selman SH. In vivo and in vitro effect of baicalein on human prostate cancer cells. Int J Oncol. 2005 Jan;26(1):241-6.

[28] Oh MC, Piao MJ, Fernando PM, Han X, Madduma Hewage SR, Park JE, Ko MS, Jung U, Kim IG, Hyun JW. Baicalein Protects Human Skin Cells against Ultraviolet B-Induced Oxidative Stress. Biomol Ther (Seoul). 2016 Nov 1;24(6):616-622.

[29] Yun BY, Zhou L, Xie KP, Wang YJ, Xie MJ. [Antibacterial activity and mechanism of baicalein]. (Article in Chinese). Yao Xue Xue Bao. 2012 Dec;47(12):1587-92.

[30]Baikal Skullcap”, WebMD.com, available from https://www.webmd.com/vitamins/ai/ingredientmono-903/baikal-skullcap [Accessed June 15, 2018]

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