Ku Shen (Sophora flavescens) Antitumor Properties

The dried roots of Sophora flavescens Aiton, known as Ku Shen, are used in traditional Chinese medicine and have been studied for their antitumor properties. The active components in Ku Shen, primarily Kushen alkaloids (KS-As) like oxymatrine and matrine, and Kushen flavonoids (KS-Fs), have shown potential as anticancer agents by targeting cancer cells while minimizing harm to healthy cells. KS-Fs, in particular, demonstrate strong antitumor effects in both in vitro and in vivo experiments.

Research on Kushen Components

Various studies have investigated the components of Ku Shen:

• Alkaloids: Research has developed and validated an HPLC method to analyze key alkaloids in Ku Shen. These include matrine, sophoridine, and oxymatrine, with the method showing good precision and recovery rates. This method has been used for the determination of these alkaloids in different samples of Sophora flavescens Ait.
• Flavonoids: Studies have isolated 23 chemical compounds from the roots of Ku Shen, identifying several new compounds with antibacterial and antiandrogenic activities. These compounds have potential for clinical applications in cancer therapy.
• Polysaccharides: A polysaccharide extracted from Ku Shen, termed SFPW1, demonstrated antitumor and immune-boosting effects in cell and mouse models, suggesting its ability to stimulate an immune response against tumors.

Clinical Applications and Pharmacokinetics

Research has extended to the clinical applications and pharmacokinetics of Ku Shen compounds:

• Studies have measured the levels of matrine and other alkaloids in rat plasma post-administration, providing insights into their potential for clinical use.
• The pharmacokinetics of matrine have been studied using PBPK models, revealing how the compound is absorbed and cleared in the body, which is valuable for drug development.

Potential Therapeutic Uses

Ku Shen's compounds have been investigated for their therapeutic uses in various medical conditions:

• The inhibition of growth of cancer cells and expression of genes driven by NFκB pathways by compounds like kurarinone.
• The potential use of sophoflavescenol as a selective inhibitor of PDE5, which is relevant for conditions like erectile dysfunction.
• The promising neuroprotective effects of matrine and oxymatrine against cerebral ischemia.
• The anticancer effects of matrine on various cancer cell types, including breast, lung, gastric, prostate, and leukemia cells, often involving apoptosis and cell cycle arrest.

Conclusion

The body of research on Ku Shen highlights its rich variety of bioactive compounds with significant antitumor and medicinal properties. The findings from these studies support the potential of Ku Shen as a source of new anticancer agents and its use in traditional medicine.

References:

1. Antitumor activities of kushen: literature review
2. Simultaneous determination of matrine, sophoridine and oxymatrine in Sophora flavescens Ait. by high performance liquid chromatography
3. Pharmacokinetic study of matrine, oxymatrine and oxysophocarpine in rat plasma after oral administration of Sophora flavescens Ait. extract by liquid chromatography tandem mass spectrometry
4. Antibacterial and antiandrogen flavonoids from Sophora flavescens
5. Attenuation of ERK/RSK2-driven NFκB gene expression and cancer cell proliferation by kurarinone, a lavandulyl flavanone isolated from Sophora flavescens ait. roots
6. A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5
7. [Studies on the chemical constituents from Sophora flavescens ait]
8. A new prenylated flavonol from the roots of Sophora flavescens
9. Antidiabetic complications and anti-Alzheimer activities of sophoflavescenol, a prenylated flavonol from Sophora flavescens, and its structure-activity relationship
10. Antitumor and immunomodulating activity of a polysaccharide from Sophora flavescens Ait
11. Study of the antipyretic activity of matrine. A lupin alkaloid isolated from Sophora subprostrata
12. Physiologically based pharmacokinetics of matrine in the rat after oral administration of pure chemical and ACAPHA
13. Comparative analysis of quinolizidine alkaloids from different parts of Sophora alopecuroides seeds by UPLC-MS/MS
14. Challenges and scientific issues in the standardization of botanicals and their preparations. United States Pharmacopeia's dietary supplement verification program--a public health program
15. Determination of matrine in rat plasma by high-performance liquid chromatography and its application to pharmacokinetic studies
16. Oxymatrine metabolic fate
17. Determination and pharmacokinetic study of oxymatrine and its metabolite matrine in human plasma by liquid chromatography tandem mass spectrometry
18. [Effects of inhibitor of protein kinase C on brain edema formation evoked by experimental cerebral ischemia in gerbils and rats]
19. Direct protection of neurons and astrocytes by matrine via inhibition of the NF-κB signaling pathway contributes to neuroprotection against focal cerebral ischemia
20. Neuroprotection and underlying mechanisms of oxymatrine in cerebral ischemia of rats
21. Oxymatrine downregulates TLR4, TLR2, MyD88, and NF-kappaB and protects rat brains against focal ischemia
22. The protective role of oxymatrine on neuronal cell apoptosis in the hemorrhagic rat brain
23. Neuroprotective effects of oxymatrine against excitotoxicity partially through down-regulation of NR2B-containing NMDA receptors
24. [Effects of matrine on proliferation and telomerase activity of colon cancer SW1116 cells]
25. Kinetics and molecular docking studies of kaempferol and its prenylated derivatives as aldose reductase inhibitors
26. Anti-inflammatory and PPAR transactivational properties of flavonoids from the roots of Sophora flavescens
27. Matrine suppresses breast cancer cell proliferation and invasion via VEGF-Akt-NF-kappaB signaling
28. Matrine inhibits breast cancer growth via miR-21/PTEN/Akt pathway in MCF-7 cells
29. Effects of matrine against the growth of human lung cancer and hepatoma cells as well as lung cancer cell migration
30. Matrine inhibits the activity of translation factor eIF4E through dephosphorylation of 4E-BP1 in gastric MKN45 cells
31. Autophagy is involved in anticancer effects of matrine on SGC-7901 human gastric cancer cells
32. Matrine induces apoptosis in gastric carcinoma cells via alteration of Fas/FasL and activation of caspase-3
33. Matrine induces apoptosis in human acute myeloid leukemia cells via the mitochondrial pathway and Akt inactivation
34. Antitumor effect of matrine in human hepatoma G2 cells by inducing apoptosis and autophagy
35. Matrine inhibits proliferation and induces apoptosis of the androgen‑independent prostate cancer cell line PC-3
36. Inhibitory effect of matrine on the expression of PSA and AR in prostate cancer cell line LNCaP
37. [Matrine inhibits the proliferation of prostate cancer cells and the activity of androgen receptor]
38. Matrine-induced apoptosis in leukemia U937 cells: involvement of caspases activation and MAPK-independent pathways
39. Matrine upregulates the cell cycle protein E2F-1 and triggers apoptosis via the mitochondrial pathway in K562 cells
40. Matrine inhibits invasiveness and metastasis of human malignant melanoma cell line A375 in vitro
41. VEGFA upregulates FLJ10540 and modulates migration and invasion of lung cancer via PI3K/AKT pathway
42. The hair growth promoting effect of Sophora flavescens extract and its molecular regulation
43. Isolation of flavonoids and a cerebroside from the stem bark of Albizzia julibrissin
44. Prenylated flavonoids as tyrosinase inhibitors
45. Tyrosinase inhibitory prenylated flavonoids from Sophora flavescens
46. Prenylated flavonoids from the roots of Sophora flavescens with tyrosinase inhibitory activity
47. Kurarinol, tyrosinase inhibitor isolated from the root of Sophora flavescens
48. Inhibitory effects of kurarinol, kuraridinol, and trifolirhizin from Sophora flavescens on tyrosinase and melanin synthesis
49. Inhibitory effects of plant extracts on tyrosinase, L-DOPA oxidation, and melanin synthesis
50. Studies on medicamentous inhibitory therapy for esophageal precancerous lesions--3- and 5-year inhibitory effects of antitumor-B, retinamide and riboflavin
51. Cancer chemopreventive activity of a mixture of Chinese herbs (antitumor B) in mouse lung tumor models
52. Gas chromatography-mass spectrometry determination of matrine in human plasma