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Baikal skullcap (Scutellaria baicalensis)


Baikal skullcap (Scutellaria baicalensis) Image
Synonyms / Common Names / Related Terms
Apigenin, apigenin-7-O-beta-glucoside, apigenin-7-O-neohesperidoside, baicalin, ban-ji-ryun (Korean), banjiryun (Korean), ban-zhi-lian (Chinese), barbatin A, barbatin B, barbatin C, benzyaldehyde, berberine, BZL101, carthamidin, ethyl-7-O-apigenin-glucuronate, flavonoidglycoside, flavonoids, Herba Scutellariae barbatae, hexahydrofarnesylacetone, isocarthamidin, Lamiaceae (family), luteolin, menthol, neo-clerodane diterpenoids, PC-SPES, pheophorbide A, resveratrol, SBJ, scutebarbatine B, scutellarein, Scutelleria baicalensis, Scutellaria baicalensis Georgi, Scutellaria bardata, Scutellaria barbata D. Don, Scutellaria rivularis Wall., scutellarin, wogonin.

Combination product (example): (chrysanthemum, dyers woad, licorice, reishi, san-qi ginseng, rabdosia, saw palmetto, Baikal skullcap).

Note: Avoid confusion between Baikal skullcap (Scutellaria barbata) and Scutellaria lateriflora, which is known as scullcap.

Mechanism of Action

Pharmacology:

  • Constituents: In assays, Scutellaria barbata has been found to contain barbatin A, barbatin B, barbatin C, scutebarbatine B, resveratrol, baicalin, berberine, apigenin, luteolin, ethyl-7-O-apigenin-glucuronate, apigenin-7-O-beta-glucoside, apigenin-7-O-neohesperidoside, and benzyaldehyde.4,18,10,37 The major active constituent is scutellarin. 38 The essential oil of Scutellaria barbata has been found to contain hexahydrofarnesylacetone (11.0%), 3,7,11,15-tetramethyl-2-hexadecen-1-ol (7.8%), menthol (7.7%), and 1-octen-3-ol (7.1%).27
  • Anticancer effects: Scutellaria barbata has been used in numerous in vitro and animal studies to determine whether or not it has anticancer properties in hepatocellular carcinoma, hepatoma, uterine cancer, skin cancer, leukemia, renal cell carcinoma, hepatoblastoma, breast cancer, lung cancer, cervical cancer, nasopharyngeal cancer, oral epidermoid cancer, colorectal cancer, pancreas cancer, and prostate cancer.4,5,6,2,7,8,9,1,10,11,12,13,14,15,16,3,17,18,19,20 Most of the studies indicate that Baikal skullcap inhibits proliferation and induces apoptosis4,5,6,2,7,8,10,1,11,13,16,3,18, possibly in a time- and dose-dependent manner6,13,15,19. One study also found that Baikal skullcap may induce differentiation in uterine carcinoma cells.8 Another study found that combined treatment with cyclophosphamide modulated cytotoxic activity of natural killer cells and peritoneal macrophages during tumor growth.12 A third study found that Baikal skullcap dose-dependently augmented a macrophage oxidative burst to inhibit tumor growth.15 In addition, Baikal skullcap showed antimetastic activity in Pliss' lymphosarcoma in rats, with a possible relationship between functional activity of thrombocytes and the degree of tumor advancement and its metastatic activity.21
  • Antifungal properties: A laboratory study indicated that Baikal skullcap may have anti-Candida properties.29
  • Antihyperlipidemia effects: In an animal study, rats fed a high-fat, high-cholesterol diet and 0.05% Scutellaria baicalensis radix extract had a lower atherogenic index value in the group fed with fresh oil, and a lower atherogenic index value in the group fed with oxidized lard.30
  • Antihypoxia effects: Baikal skullcap extract's antihypoxia properties may be due to a mitochondrial mechanism.33 In addition, it may prevent diminution of energy of the brain mitochondria in hypoxia, inhibit restriction of succinate dependent energy production, and preserve intactness of the mitochondrial membranes.34
  • Antimetastatic effects: Thrombocyte aggregation may function in the mechanism of the antimetastatic action of Baikal skullcap extracts.21 The advancement of Pliss' lymphosarcoma in rats was shown to be associated with disorders of platelet-mediated hemostasis presenting with either lowered or increased aggregation activity of platelets.21 In the latter case, a direct correlation was observed between functional activity of thrombocytes, on the one hand, and degree of tumor advancement and its metastatic activity, on the other. Extract of Scutellaria baicalensis Georgi was shown to produce a normalizing effect on platelet-mediated hemostasis whatever the pattern of alteration, which points to the adaptogenic activity of the drug. This activity is thought to be responsible for the drug's antitumor and, particularly, metastasis-preventing effects.
  • Antimicrobial effects: In a laboratory study, apigenin and luteolin isolated from Scutellaria barbata showed antibacterial activity against methicillin-resistant Staphylococcus aureus.28 The Gram-positive bacteria, including methicillin-resistant Staphlococcus aureus, were more sensitive to the oil than Gram-negative bacteria and yeasts.27
  • Antimutagenic activity: Baikal skullcap has shown antimutagenic activity in a few in vitro studies. In one study, 125g/L of Scutellaria barbata inhibited the DNA damage in lymphocytes caused by the total particle material extracted from cigarette tar.22 In a set of studies, Wong et al. determined that Baikal skullcap inhibited mutagenesis caused by benzo[a]pyrene in bacteria and rat liver supernatant.23,24,25 These effects may be due to inhibition of cytochrome P-450IA1-linked EROD activity of the supernatant. In an animal study, Scutellaria bardata inhibited the development of preneoplastic lesions in carcinogen-treated mouse mammary glands.1
  • Aromatase inhibition activity: In an in vitro study, Scutellaria barbata D. Don. inhibited both cell-free and intracellular aromatase activity in myometrial and leiomyomal cells.13 Enzyme activity was inhibited in a time-and dose-dependent fashion by either 1-50nM TPA or 0.01-0.5ng/mL TGF-beta1, with maximal responses two to three hours after exposure.
  • CYP-450 effects: In two mutagenesis studies by the same authors, Baikal skullcap may have inhibited mutagenesis by inhibiting CYP3- and CYP450IA1-mediated metabolism.36,23
  • Hemopoietic effects: Scutellaria baicalensis dry extract and baicalin stimulate erythropoiesis, which is depressed when the paradoxical phase of sleep is deprived.26 In addition, both the dry extract and baicalin activate and normalize hemopoiesis after a conflict situation. These effects may be related to their influence on the adrenergic structures.
  • Hepatoprotective effects: In two animal studies by Lin et al., ban-zhi-lian derived from Scutellaria rivularis Benth showed hepatoprotective effects against hepatotoxicity induced by carbon tetrachloride, D-galactosamine, or acetaminophen.31,32
  • Neural activity: Baikal skullcap extract produced a dose-dependent stimulating effect on neurite growth in neurons of dorsal root ganglia from 1-2 day-old rats.35

Pharmacodynamics/Kinetics:

  • Metabolism: Zhang et al. conducted a pharmacokinetic study of the metabolism of scutellarin in rats.38 The authors identified scutellarin as the major active constituent of Scutellaria barbata D. After administration, the authors separated and analyzed five metabolites (M1-M5) of Baikal skullcap. M1 and M3 were conjugates of scutellarin with two sulfate groups; M2 was scutellarin; M4 was 6-methyl-scutellarin; and M5 was 6-methyl-scutellarein. The authors also proposed a metabolic pathway.

References

  1. Suh, S. J., Yoon, J. W., Lee, T. K., Jin, U. H., Kim, S. L., Kim, M. S., Kwon, D. Y., Lee, Y. C., and Kim, C. H. Chemoprevention of Scutellaria bardata on human cancer cells and tumorigenesis in skin cancer. Phytother Res 2007;21(2):135-141. 17128438
  2. Chan, J. Y., Tang, P. M., Hon, P. M., Au, S. W., Tsui, S. K., Waye, M. M., Kong, S. K., Mak, T. C., and Fung, K. P. Pheophorbide a, a major antitumor component purified from Scutellaria barbata, induces apoptosis in human hepatocellular carcinoma cells. Planta Med 2006;72(1):28-33. 16450292
  3. Yin, X., Zhou, J., Jie, C., Xing, D., and Zhang, Y. Anticancer activity and mechanism of Scutellaria barbata extract on human lung cancer cell line A549. Life Sci 9-17-2004;75(18):2233-2244. 15325848
  4. Kim, J. H., Lee, E. O., Lee, H. J., Ku, J. S., Lee, M. H., Yang, D. C., and Kim, S. H. Caspase activation and extracellular signal-regulated kinase/Akt inhibition were involved in luteolin-induced apoptosis in Lewis lung carcinoma cells. Ann N Y Acad Sci 2006;1090:147-160. 17384257
  5. Tang, P. M., Chan, J. Y., Au, S. W., Kong, S. K., Tsui, S. K., Waye, M. M., Mak, T. C., Fong, W. P., and Fung, K. P. Pheophorbide a, an active compound isolated from Scutellaria barbata, possesses photodynamic activities by inducing apoptosis in human hepatocellular carcinoma. Cancer Biol Ther 2006;5(9):1111-1116. 16880732
  6. Lin, J. M., Liu, Y., and Luo, R. C. [Effect of Scutellaria barbata extract against human hepatocellular Hep-G2 cell proliferation and its mechanism]. Nan Fang Yi Ke Da Xue Xue Bao  2006;26(7):975-977. 16864090
  7. Lee, T. K., Cho, H. L., Kim, D. I., Lee, Y. C., and Kim, C. H. Scutellaria barbata D. Don induces c-fos gene expression in human uterine leiomyomal cells by activating beta2-adrenergic receptors. Int J Gynecol Cancer 2004;14(3):526-531. 15228428
  8. Lee, T. K., Lee, D. K., Kim, D. I., Lee, Y. C., Chang, Y. C., and Kim, C. H. Inhibitory effects of Scutellaria barbata D. Don on human uterine leiomyomal smooth muscle cell proliferation through cell cycle analysis. Int Immunopharmacol  2004;4(3):447-454. 15072097
  9. Udintsev, S. N., Razina, T. G., and Iaremenko, K. V. [The antitumor effect of Baikal skullcap]. Vopr Onkol  1990;36(5):602-607. 2198692
  10. Kim, D. I., Lee, T. K., Lim, I. S., Kim, H., Lee, Y. C., and Kim, C. H. Regulation of IGF-I production and proliferation of human leiomyomal smooth muscle cells by Scutellaria barbata D. Don in vitro: isolation of flavonoids of apigenin and luteolin as acting compounds. Toxicol Appl Pharmacol 6-15-2005;205(3):213-224. 15922007
  11. Lee, T. K., Kim, D. I., Song, Y. L., Lee, Y. C., Kim, H. M., and Kim, C. H. Differential inhibition of Scutellaria barbata D. Don (Lamiaceae) on HCG-promoted proliferation of cultured uterine leiomyomal and myometrial smooth muscle cells. Immunopharmacol Immunotoxicol  2004;26(3):329-342. 15518168
  12. Kaplya, O. A., Sherstoboev, E. Y., Zueva, E. P., Razina, T. G., Amosova, E. N., and Krylova, S. G. Effect of baikal skullcap extract administered alone or in combination with cyclophosphamide on natural cytotoxicity system in mice with Lewis lung carcinoma. Bull Exp Biol Med 2004;137(5):471-474. 15455121
  13. Cha, Y. Y., Lee, E. O., Lee, H. J., Park, Y. D., Ko, S. G., Kim, D. H., Kim, H. M., Kang, I. C., and Kim, S. H. Methylene chloride fraction of Scutellaria barbata induces apoptosis in human U937 leukemia cells via the mitochondrial signaling pathway. Clin Chim Acta 2004;348(1-2):41-48. 15369734
  14. Razina, T. G., Zueva, E. P., Litvinenko, V. I., and Kovalev, I. P. [A semisynthetic flavonoid from the Baikal skullcap (Scutellaria baicalensis) as an agent to enhance the efficacy of chemotherapy in experimental tumors]. Eksp Klin Farmakol  1998;61(2):54-56. 9621177
  15. Wong, B. Y., Lau, B. H., Jia, T. Y., and Wan, C. P. Oldenlandia diffusa and Scutellaria barbata augment macrophage oxidative burst and inhibit tumor growth. Cancer Biother Radiopharm  1996;11(1):51-56. 10851520
  16. Chui, C. H., Lau, F. Y., Tang, J. C., Kan, K. L., Cheng, G. Y., Wong, R. S., Kok, S. H., Lai, P. B., Ho, R., Gambari, R., and Chan, A. S. Activities of fresh juice of Scutellaria barbata and warmed water extract of Radix Sophorae Tonkinensis on anti-proliferation and apoptosis of human cancer cell lines. Int J Mol Med 2005;16(2):337-341. 16012772
  17. Gao, D., Gao, Y., and Bai, P. [Influence of Scutellaria barbata on calcium beaconage of cervix cancer cells]. Zhong Yao Cai  2003;26(10):730-733. 14768391
  18. Dai, S. J., Tao, J. Y., Liu, K., Jiang, Y. T., and Shen, L. neo-Clerodane diterpenoids from Scutellaria barbata with cytotoxic activities. Phytochemistry 2006;67(13):1326-1330. 16769097
  19. Goh, D., Lee, Y. H., and Ong, E. S. Inhibitory effects of a chemically standardized extract from Scutellaria barbata in human colon cancer cell lines, LoVo. J Agric Food Chem 10-19-2005;53(21):8197-8204. 16218664
  20. Shoemaker, M., Hamilton, B., Dairkee, S. H., Cohen, I., and Campbell, M. J. In vitro anticancer activity of twelve Chinese medicinal herbs. Phytother Res 2005;19(7):649-651. 16161030
  21. Razina, T. G., Udintsev, S. N., Tiutrin, I. I., Borovskaia, T. G., and Iaremenko, K. V. [The role of thrombocyte aggregation function in the mechanism of the antimetastatic action of an extract of Baikal skullcap]. Vopr Onkol  1989;35(3):331-335. 2705316
  22. Han, F., Hu, J., and Xu, H. [Effects of some Chinese herbal medicine and green tea antagonizing mutagenesis caused by cigarette tar]. Zhonghua Yu Fang Yi Xue Za Zhi  1997;31(2):71-74. 9812614
  23. Wong, B. Y., Lau, B. H., Yamasaki, T., and Teel, R. W. Modulation of cytochrome P-450IA1-mediated mutagenicity, DNA binding and metabolism of benzo[a]pyrene by Chinese medicinal herbs. Cancer Lett 1-15-1993;68(1):75-82. 8422652
  24. Wong, B. Y., Lau, B. H., and Teel, R. W. Chinese medicinal herbs modulate mutagenesis, DNA binding and metabolism of benzo[a]pyrene 7,8-dihydrodiol and benzo[a]pyrene 7,8-dihydrodiol-9,10-epoxide. Cancer Lett 2-29-1992;62(2):123-131. 1540939
  25. Wong, B. Y., Lau, B. H., Tadi, P. P., and Teel, R. W. Chinese medicinal herbs modulate mutagenesis, DNA binding and metabolism of aflatoxin B1. Mutat Res 6-1-1992;279(3):209-216. 1377337
  26. Dygai, A. M., Suslov, N. I., Skurikhin, E. G., Churin, A. A., and Provalova, N. V. [The modulating effects of preparations of Baikal skullcap (Scutellaria baicalensis) on erythron reactions under conditions of neurotic exposures]. Eksp Klin Farmakol  1998;61(1):37-39. 9575410
  27. Yu, J., Lei, J., Yu, H., Cai, X., and Zou, G. Chemical composition and antimicrobial activity of the essential oil of Scutellaria barbata. Phytochemistry 2004;65(7):881-884. 15081288
  28. Sato, Y., Suzaki, S., Nishikawa, T., Kihara, M., Shibata, H., and Higuti, T. Phytochemical flavones isolated from Scutellaria barbata and antibacterial activity against methicillin-resistant Staphylococcus aureus. J Ethnopharmacol 2000;72(3):483-488. 10996290
  29. Zhao, M., Zhou, Z. T., and Zhang, W. D. [Antifugal susceptibility testing and antifugal traditional Chinese medicines screening of oral Candida isolated from head and neck cancer patients treated with radiotherapy or chemotherapy]. Hua Xi Kou Qiang Yi Xue Za Zhi  2006;24(2):131-134. 16704090
  30. Regulska-Ilow, B., Biernat, J., Grajeta, H., Ilow, R., and Drzewicka, M. Influence of bioflavonoids from the radix extract of Scutellaria baicalensis on the level of serum lipids, and the development of laboratory rats fed with fresh and oxidized fats. Nahrung 2004;48(2):123-128. 15146969
  31. Lin, C. C., Shieh, D. E., and Yen, M. H. Hepatoprotective effect of the fractions of Ban-zhi-lian on experimental liver injuries in rats. J Ethnopharmacol 1997;56(3):193-200. 9201608
  32. Lin, S. C., Lin, C. C., Lin, Y. H., and Chen, C. H. Protective and therapeutic effects of ban-zhi-lian on hepatotoxin-induced liver injuries. Am J Chin Med 1994;22(1):29-42. 8030617
  33. Khazanov, V. A. and Saifutdinov, R. R. [Mitochondrial mechanism of the anti-hypoxia effect of the Baikal scullcap extract]. Biull Eksp Biol Med 1999;128(9):327-329. 10560058
  34. Saifutdinov, R. R. and Khazanov, V. A. [The effect of an extract of Baikal skullcap (Scutelleria baicalensis) on succinic acid oxidation by the brain mitochondria in rats with hypoxia]. Eksp Klin Farmakol 1998;61(5):27-29. 9854629
  35. Shurygin, A. Y., Bezzubov, N. V., Ignatova, E. A., Nikolaev, S. M., and Viktorov, I. V. Baikal skullcap extract stimulates neurite growth in cultures of rat dorsal root Ganglia. Bull Exp Biol Med 2002;134(1):47-49. 12459867
  36. Wong, B. Y., Lau, B. H., Yamasaki, T., and Teel, R. W. Inhibition of dexamethasone-induced cytochrome P450-mediated mutagenicity and metabolism of aflatoxin B1 by Chinese medicinal herbs. Eur J Cancer Prev  1993;2(4):351-356. 8358288
  37. Wang, W. S., Zhou, Y. W., Ye, Y. H., and Du, N. [Studies on the flavonoids in herb from Scutellaria barbata]. Zhongguo Zhong Yao Za Zhi  2004;29(10):957-959. 15631081
  38. Zhang, J. L., Che, Q. M., Li, S. Z., and Zhou, T. H. Study on metabolism of scutellarin in rats by HPLC-MS and HPLC-NMR. J Asian Nat Prod Res 2003;5(4):249-256. 14604233




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