Health Care Professional Information
Ku Shen Gen, bitter root, yellow sophora root
Sophora flavescens is a deciduous shrub related to peas. The root known as “Ku Shen” which means “bitter root” in Chinese, has been used in Traditional Medicine for two thousand years to treat a variety of conditions, including diarrhea, jaundice, skin rashes, and to kill parasites (1). Although this herb is generally not consumed as a dietary supplement in the West, recent lab studies indicate that it has antitumor properties and patients are using it as a natural cancer treatment.
Matrine, an alkaloid present in Sophora flavescens, demonstrated antitumor effects against liver (10) (18), breast (19), pancreas (20), myeloma (21) and gastric (22) (23) cancer cell lines. Other flavonoids such as kuraninone and sophoraflavonone are thought to be biologically active as well and may have vasodilatory and antiviral effects (5) (6) (7). However, large scale clinical studies are needed at confirm these effects in humans.
Sophora flavescens acts as a phytoestrogen (24) (25) (26). Patients with hormone-sensitive cancer should avoid this product.
- Alkaloids (matrine, oxymatrine, sophocarpine, sophoramine, sophoridine, sophoranol, anagyrine, N-methylcystine, baptifoline) (1)
- Flavonoids (kushenols, kuraninol, formononetin) (1)
- Triterpenoids (soyasaponin) (1)
- Lectins (8)
- Chalcones (9)
Mechanism of Action
The mechanism of action is not entirely understood. In rats, the antiviral properties of sophoridine, an alkaloid constituent, appear to be mediated via up-regulation of the cytokines IL-10 and IFN-gamma (11). Other animal studies suggest that Sophora flavescens flavonoids may promote vasodilation by inhibiting Ca2+ influx through a voltage-gated channel (12). The flavonoids sophoraflavonone G and kurarinone appear to be responsible for antioxidant effects, which are mediated through free radical scavenging (4). Sophoraflavonone G may also play a role in Sophora flavescens's anti-inflammatory effects, by inhibiting prostaglandin E2 formation via down-regulation of COX-2 (13).
Most of the reported antineoplastic effects of Sophora flavescens are due to the pro-apoptotic activity of Matrine, the main alkaloid constituent. In human hepatocellular carcinoma cells, matrine inhibits matrix metalloproteinase-9 (MMP-9) by downregulating the NF-kappa B pathway (18). It has also been shown to demonstrate anti-angiogenic effects by inhibiting VEGF and VEGFR-2 (19). Matrine triggers the mitochondrial pathway, in which cytochrome C release induces caspase-9 and -3 activation and subsequently induces apoptosis (2) (3) (10) (21) (2).
A study done in rats suggests 85-90% bioavailability of matrine, oxymatrine, and oxysophocarpine (all alkaloid constituents) following oral administration. Matrine appears to be absorbed well and eliminated slowly from the plasma, and is therefore the most active constituent of the three (14). Sophoridine, another active alkaloid, also appears in measurable amounts in the blood stream after oral administration (11).
- Patients with hormone-sensitive cancers should avoid taking Sophora flavescens as it demonstrated estrogenic effects in vitro (24) (25) (26), and can stimulate the proliferation of hormone-sensitive cancer cells.
- Taxol: In mice, Sophora flavescens flavonoids may enhance the effects of Taxol against certain tumors (16).
- Ampicillin/Gentamicin: In vitro, sophoraflavanone G may increase the activity of these antibiotics against oral bacteria (17).
- P-Glycoprotein substrates: Sophora flavaescens does not appear to have any effects on the action of P-glycoprotein (27).
Literature Summary and Critique
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- Chen JK and Chen TT. Chinese Medical Herbology and Pharmacology. First ed. 2004, City of Industry, CA: Art of Medicine Press, Inc.
- Jiang H, Hou C, Zhang S, et al. Matrine upregulates the cell cycle protein E2F-1 and triggers apoptosis via the mitochondrial pathway in K562 cells. Eur J Pharmacol. 2007 Mar 22;559(2-3):98-108.
- Liu XS, et al. Matrine-induced apoptosis in leukemia U937 cells: involvement of caspases activation and MAPK-independent pathways. Planta Med. 2006;2(6): 501-6.
- Piao XL, et al. Identification and characterization of antioxidants from Sophora flavescens. Biol Pharm Bull. 2006;9(9): 1911-5.
- Hoang BX, et al. New approach in asthma treatment using excitatory modulator. Phytotherapy research. 2007;21(6): p. 554-7.
- Chen C, et al. A randomized controlled trial of kurorinone versus interferon-alpha2a treatment in patients with chronic hepatitis B. Journal of viral hepatitis. 2000;7(3): p. 225-9.
- Chen SX, et al. [Therapeutic effect of kangke injection on viral myocarditis and its anticoxsackie virus mechanism]. Zhong Guo Zhong Xi Yi Jie He Za Zhi. 1997. 17(4): p. 207-9.
- Liu Z, et al. A mannose-binding lectin from Sophora flavescens induces apoptosis in HeLa cells. Phytomedicine. 2008;15(10):867-75.
- Lee JH, et al. A new cytotoxic prenylated chalcone from Sophora flavescens. Arch Pharm Res. 2007;30(4): 408-11.
- Ma L, et al., Anticancer effects of the chinese medicine matrine on murine hepatocellular carcinoma cells. Planta Med. 2008;74(3): 245-51.
- Zhang Y, et al. Antiviral effects of sophoridine against coxsackievirus B3 and its pharmacokinetics in rats. Life Sci. 2006; 78(17):1998-2005.
- Yamahara J, et al. Vasodilatory active principles of Sophora flavescens root.J Ethnopharmacol. 1990;29(1): p. 79-85.
- Kim DW, et al. Effects of sophoraflavanone G, a prenylated flavonoid from Sophora flavescens, on cyclooxygenase-2 and in vivo inflammatory response. Arch Pharm Res. 2002;25(3): 329-35.
- Zhang L, et al. Pharmacokinetic study of matrine, oxymatrine and oxysophocarpine in rat plasma after oral administration of Sophora flavescens Ait. extract by liquid chromatography tandem mass spectrometry. Journal of Pharmaceutical and Biomedical Analysis. 2008;47(4-5): 892-898.
- Xiang Q, et al. [Anti-leukemia effect of sophora flavescens combined with the low molecular weight natural tumor suppressor of the human fetal liver and its mechanism]. Hunan Yi Ke Da Xue Xue Bao. 2002;27(2): 108-10.
- Sun M, et al. Novel antitumor activities of Kushen flavonoids in vitro and in vivo. Phytother Res. 2007;21(3): 269-77.
- Cha JD, et al. Antibacterial activity of sophoraflavanone G isolated from the roots of Sophora flavescens. J Microbiol Biotechnol. 2007;17(5): 858-64.
- Yu HB, Zhang HF, Li DY, et al. Matrine inhibits matrix metalloproteinase-9 expression and invasion of human hepatocellular carcinoma cells. J Asian Nat Prod Res. 2011 Mar;13(3):242-50.
- Li H, Tan G, Jiang X, et al. Therapeutic effects of matrine on primary and metastatic breast cancer. Am J Chin Med. 2010;38(6):1115-30.
- Liu T, Song Y, Chen H, Pan S, Sun X. Matrine inhibits proliferation and induces apoptosis of pancreatic cancer cells in vitro and in vivo. Biol Pharm Bull. 2010;33(10):1740-5.
- Han Y, Zhang S, Wu J, et al. Matrine induces apoptosis of human multiple myeloma cells via activation of the mitochondrial pathway. Leuk Lymphoma. 2010 Jul;51(7):1337-46.
- Dai ZJ, Gao J, Ji ZZ, et al. Matrine induces apoptosis in gastric carcinoma cells via alteration of Fas/FasL and activation of caspase-3. J Ethnopharmacol. 2009 May 4;123(1):91-6.
- Jiang T, Zhu Y, Luo C, et al. Matrine inhibits the activity of translation factor eIF4E through dephosphorylation of 4E-BP1 in gastric MKN45 cells. Planta Med. 2007 Sep;73(11):1176-81.
- Kang SC, Lee CM, Choi H, et al. Evaluation of oriental medicinal herbs for estrogenic and antiproliferative activities. Phytother Res. 2006 Nov;20(11):1017-9.
- De Naeyer A, Vanden Berghe W, Pocock V, et al. Estrogenic and anticarcinogenic properties of kurarinone, a lavandulyl flavanone from the roots of Sophora flavescens. J Nat Prod. 2004 Nov;67(11):1829-32.
- Yoo HH, Kim T, Ahn S, et al. Evaluation of the estrogenic activity of Leguminosae plants. Biol Pharm Bull. 2005 Mar;28(3):538-40.
- Choi SU, Kim KH, Choi EJ, et al. P-glycoprotein (Pgp) does not affect the cytotoxicity of flavonoids from Sophora flavescens, which also have no effects on Pgp action. Anticancer Res. 1999 May-Jun;19(3A):2035-40.
How It Works
Bottom line: Sophora flavescens has shown anticancer effects in lab studies. But it has not been studied as a cancer preventive or treatment in humans.
Sophora flavescens or Ku Shen, which in Chinese means “bitter root,” is an herb used in Traditional medicine to treat a wide variety of symptoms, with purported effects on the heart, liver, intestinal tract, and skin. Lab and animal studies have shown that some compounds can kill cancer cells and help fight certain viruses. However, human data are lacking.
Sophora flavescens may act like an estrogen in the body. Patients with hormone-sensitive cancer should avoid this product.
Lab studies show anticancer activities through different mechanisms. Despite positive lab results, this use has not been proven by clinical trials.
This claim is not supported by research.
Limited evidence suggests that Sophora flavescens may be a useful treatment for hepatitis B and coxsackie B viruses, but more data are necessary to support this use.
A single non-randomized trial supports this use, but more data are needed.
- Skin disorders
Sophora flavescens is used to treat skin disorder in Traditional Medicine. But this use has not been proven in clinical trials.
Do Not Take If
- You are taking Taxol (In mice, Sophora flavescens flavonoids increased the effects of Taxol against certain tumors).
- You are taking Ampicillin/Gentamicin (In vitro, sophoraflavanone G may increase the activity of these antibiotics against oral bacteria).
- You have hormone-sensitive cancer (Sophora flavescens has estrogenic effects and can stimulate the proliferation of hormone-sensitive cancer cells).
Last updated: September 30, 2012