Scutellaria baicalensis

• How It Works

  Scutellaria baicalensis is used in traditional medicine to treat many medical conditions. Studies on its potential anticancer effects are underway.

  S. baicalensis, also known as Huang Qin or Chinese skullcap, is a root extract used in traditional medicine, often in combination with other herbs. Most studies have been conducted in the lab rather than in humans. Some cancer cell lines undergo cell death when exposed to extracts from this herb. However, there are some compounds in this herb that may have opposite effects. Additional studies are needed to confirm the circumstances under which this herb may be beneficial.

  S. baicalensis extracts also reduce inflammation, act as antioxidants, and kill gram-positive bacteria in the laboratory setting. In animals, the extracts help lower blood cholesterol levels under certain conditions. However, it is not yet clear if any of these effects occur in the human body.

• Purported Uses
  • To treat atherosclerosis
    Studies in animals show that extracts of this herb may help lower blood cholesterol levels under certain conditions, but human studies have not been conducted.
  • To treat cancer
    Extracts from this herb cause cell death in isolated liver cancer and leukemia cell lines, but human data are lacking. S. baicalensis has not been studied in clinical trials as a single agent, but has been studied in combination with other herbs in formulations such as PC-SPES and sho-saiko-to.
  • To treat hepatitis
    The herbal formulation sho-saiko-to, which contains Huang Qin, has been studied for its possible liver-protectant effects.
  • To treat arthritis
    An herbal supplement containing S. baicalensis has been shown to reduce symptoms of osteoarthritis. It is not known if the herb would exert similar effects by itself.
• Do Not Take If
  • You are taking warfarin or other blood thinners: Chinese skullcap can increase the risk of bruising and bleeding.
  • You are taking statins: Chinese skullcap can decrease the blood level of drugs used to lower cholesterol.
  • You are taking Cytochrome P450 substrate drugs: Chinese skullcap may increase the risk of side effects of these drugs.
• Side Effects
  • Liver damage
  • Lung inflammation due to bacterial or viral infection

  Case Report
  Acute liver injury: In patients following consumption of a formula containing baicalin derived from S. baicalensis for osteoarthritis.

• Scientific Name

  Scutellaria baicalensis

• Clinical Summary

  Scutellaria baicalensis is an herb used in traditional Chinese medicine to treat a variety of conditions including epilepsy, hepatitis, infections, and cancer. It often is used in combination with other botanicals such as PC-SPES and sho-saiko-to.

  In vitro and animal data suggest that compounds in S. baicalensis cause apoptosis in various cancer cells ^{(2) (3) (14)} or protect against doxorubicin-induced cardiotoxicity ⁽¹⁵⁾. However, both S. baicalensis root and its main flavonoid baicalin appear to have dose-dependent pro- and anti-angiogenic effects ⁽⁹⁾. Some constituents may also have neuroprotective ^(4) (5), anticonvulsant ⁽⁶⁾, and anti-inflammatory ⁽¹⁷⁾ effects.

  An herbal supplement containing S. baicalensis reduced symptoms of osteoarthritis ⁽²²⁾. It is not known if the herb would exert similar effects by itself.

• Purported Uses
  • Atherosclerosis
  • Cancer treatment
  • Epilepsy
  • Hepatitis
  • Infections
  • Inflammation
  • Insomnia
• Mechanism of Action

  The flavonoid baicalin exhibits anti-inflammatory, antioxidant, and gram-positive antibacterial activity in vitro ⁽³⁾. Its ability to attenuate asthma is attributed to reduced airway injury and restored mitochondrial function ⁽¹⁹⁾. The neuroprotective effects of flavonoids were ameliorated by diazepam, a GABA receptor agonist, suggesting that the components influence GABA receptor activity ⁽⁵⁾.

  In vitro studies suggest that certain flavonoid components of S. baicalensis have anticancer activity. Induction of apoptosis in hepatoma G2, 3B, and SK-Hep1 cell lines occurs following 48 hours of exposure to baicalein, baicalin, and wogonin at concentrations of 25-100 mcg/ml. Wogonin causes arrest at G1 phase while baicalin and baicalein cause G2/M accumulation ⁽²⁾. Additional studies show that baicalin, at concentrations of 50-200 mcg/ml, activates caspase-3, resulting in apoptosis of Jurkat cells (leukemia-derived T cells). However, low-dose baicalin upregulated expression of multiple angiogenic genes to increase cell proliferation in developing blood vessels, while high-dose baicalin inihbited angiognesis by inducing cell death, suggesting dose-dependent dual effects; the compound baicalein exhibited only inhibitory effects ⁽⁹⁾.

• Adverse Reactions

  Hepatotoxicity, pneumonitis ⁽⁷⁾

  Case Report
  Acute liver injury: In patients following consumption of a formula for osteoarthritis that contained baicalin derived from S. baicalensis ⁽¹⁸⁾.

• Herb-Drug Interactions
  • Anticoagulants / Antiplatelets: May cause additive effects ⁽¹²⁾.
  • Statins: Baicalin, an active constituent, can decrease the blood level of statin drugs used to lower cholesterol ⁽¹³⁾.
  • Cytochrome P450 substrates: Wogonin inhibits CYP1A2 and CYP2C19, and can affect the intracellular concentration of drugs metabolized by these enzymes ⁽¹⁶⁾.
  • Solute carrier (SLC) transporters: Baicalein, baicalin, and wogonin inhibit uptake of specific substrates mediated by essential SLC transporters, which are important membrane proteins responsible for the cellular influx of various drugs ⁽²¹⁾.
• References

  1. Bonham M, Posakony J, Coleman I, Montgomery B, Simon J, Nelson PS. Characterization of chemical constituents in Scutellaria baicalensis with antiandrogenic and growth-inhibitory activities toward prostate carcinoma. Clin Cancer Res 2005;11(10):3905-14.

  2. Chang WH, Chen CH, Lu, FJ. Different effects of baicalein, baicalin, and wogonin on mitochondrial function, glutathione content and cell cycle progression in human hepatoma cell lines. Planta Medica 2002;68:128-32.

  3. Ueda S, Nakamura H, Masutani H, et al. Baicalin induces apoptosis via mitochondrial pathway as prooxidant. Molecular Immunology 2002;38:781-91.

  4. Cheng Y, He G, Mu X, et al. Neuroprotective effect of baicalein against MPTP neurotoxicity: Behavioral, biochemical and immunohistochemical profile. Neurosci Lett. Aug 15 2008;441(1):16-20.

  5. Kim DH, Kim S, Jeon SJ, et al. 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.

  6. Park HG, Yoon SY, Choi JY, et al. Anticonvulsant effect of wogonin isolated from Scutellaria baicalensis. Eur J Pharmacol. Nov 28 2007;574(2-3):112-119.

  7. Takeshita K, Saisho Y, Kitamura K, et al. Pneumonitis induced by Ou-gon (scullcap). Internal Medicine 2001;40:764-8.

  8. Newall CA, Anderson LA, Phillipson JD. Herbal Medicines: A Guide for Health-Care Professionals. 1st ed. London: Pharmaceutical Press; 1996.

  9. Zhu D, Wang S, Lawless J, et al. Dose Dependent Dual Effect of Baicalin and Herb Huang Qin Extract on Angiogenesis. PLoS One. 2016;11(11):e0167125.

  10. Lai MY, Hsiu SL, Chen CC, Hou YC, Chao PD. Urinary pharmacokinetics of baicalein, wogonin and their glycosides after oral administration of Scutellariae radix in humans. Biol Pharm Bull. Jan 2003;26(1):79-83.

  11. Tarrago T, Kichik N, Claasen B, Prades R, Teixido M, Giralt E. Baicalin, a prodrug able to reach the CNS, is a prolyl oligopeptidase inhibitor. Bioorg Med Chem. Apr 29 2008.

  12. Lee W, Ku SK, Bae JS. Antiplatelet, anticoagulant, and profibrinolytic activities of baicalin. Arch Pharm Res. 2015;38(5):893-903.

  13. Fan L, Zhang W, Guo D, et al. The effect of herbal medicine baicalin on pharmacokinetics of rosuvastatin, substrate of organic anion-transporting polypeptide 1B1. Clin Pharmacol Ther. 2008 Mar;83(3):471-6.

  14. Takahashi H, Chen MC, Pham H, et al. Baicalein, a component of Scutellaria baicalensis, induces apoptosis by Mcl-1 down-regulation in human pancreatic cancer cells. Biochim Biophys Acta. 2011 Aug;1813(8):1465-74.

  15. Chang WT, Li J, Huang HH, et al. Baicalein protects against doxorubicin-induced cardiotoxicity by attenuation of mitochondrial oxidant injury and JNK activation. J Cell Biochem.2011 Oct;112(10):2873-81.

  16. Li T, Li N, Guo Q, et al. Inhibitory effects of wogonin on catalytic activity of cytochrome P450 enzyme in human liver microsomes. Eur J Drug Metab Pharmacokinet. 2011 Dec;36(4):249-56.

  17. Li L, Bao H, Wu J, et al. Baicalin is anti-inflammatory in cigarette smoke-induced inflammatory models in vivo and in vitro: A possible role for HDAC2 activity. Int Immunopharmacol. 2012 May;13(1):15-22.

  18. Chalasani N, Vuppalanchi R, Navarro V, et al. Acute liver injury due to flavocoxid (Limbrel), a medical food for osteoarthritis: a case series.A nn Intern Med. 2012 Jun 19;156(12):857-60, W297-300.

  19. Mabalirajan U, Ahmad T, Rehman R, et al. Baicalein reduces airway injury in allergen and IL-13 induced airway inflammation. PLoS One. 2013 Apr 30;8(4):e62916.

  20. Tian X, Cheng ZY, He J, Jia LJ, Qiao HL. Concentration-dependent inhibitory effects of baicalin on the metabolism of dextromethorphan, a dual probe of CYP2D and CYP3A, in rats. Chem Biol Interact.2013 Apr 25;203(2):522-9.

  21. Xu F, Li Z, Zheng J, et al. The inhibitory effects of the bioactive components isolated from Scutellaria baicalensis on the cellular uptake mediated by the essential solute carrier transporters. J Pharm Sci. 2013 Nov;102(11):4205-11.

  22. Arjmandi BH1, Ormsbee LT, Elam ML, et al. A Combination of Scutellaria baicalensis and Acacia catechu Extracts for Short-Term Symptomatic Relief of Joint Discomfort Associated with Osteoarthritis of the Knee. J Med Food. 2014 Jun;17(6):707-13.