Biological properties of baicalein in cardiovascular system

Current Drug Targets - Cardiovascular and Haematological Disorders

Volumn 5, Issue 2, 2005, Pages 177-184

  Huang, Yu ^a   Tsang, Suk Ying ^a   Yao, Xiaoqiang ^a   Chen, Zhen Yu ^a  

^a CHINESE UNIVERSITY OF HONG KONG   (Hong Kong)

Author keywords

Anti mitogenic; Anti proliferative; Anti thrombotic; Antioxidant; Baicalein; Hypertension; Lipoxygenase; Oxidative stress; Scutellaria baicalensis Georgi

Indexed keywords

15 HYDROXY 11ALPHA,9ALPHA EPOXYMETHANOPROSTA 5,13 DIENOIC ACID; ARACHIDONIC ACID; BAICALEIN; BAICALIN; CELL ADHESION MOLECULE; FLAVONOID; INTERLEUKIN 1BETA; LIPID; LIPOXYGENASE; NITRIC OXIDE; NORADRENALIN; PHENYLEPHRINE; PLASMINOGEN ACTIVATOR INHIBITOR 1; REACTIVE OXYGEN METABOLITE; RENIN; SCAVENGER; SCUTELLARIA BAICALENSIS EXTRACT; SEROTONIN; THROMBIN; TUMOR NECROSIS FACTOR ALPHA; VASOPRESSIN; XANTHINE OXIDASE INHIBITOR;

ANGIOGENESIS; ANTIBACTERIAL ACTIVITY; ANTINEOPLASTIC ACTIVITY; ANTIOXIDANT ACTIVITY; ANTIVIRAL ACTIVITY; ARTERIOSCLEROSIS; BLOOD PRESSURE REGULATION; CARDIOVASCULAR DISEASE; CELL CULTURE; CELL DAMAGE; CELL PROLIFERATION; CHINESE MEDICINE; CHOLERA; DOG; DRUG ACTIVITY; DRUG EFFICACY; DRUG POTENCY; DRUG STRUCTURE; DYSENTERY; ENDOTHELIUM CELL; ENTAMOEBA HISTOLYTICA; ENZYME INHIBITION; HEART PROTECTION; HUMAN; HYPERTENSION; IN VITRO STUDY; IN VIVO STUDY; INFLUENZA; INFLUENZA VIRUS; INHIBITION KINETICS; ISOLATED ARTERY; LIPID PEROXIDATION; MITOGENESIS; NONHUMAN; OXIDATIVE STRESS; PLANT ROOT; PROTEIN EXPRESSION; PROTEIN SYNTHESIS; RABBIT; RAT; REVIEW; STAPHYLOCOCCUS; STREPTOCOCCUS INFECTION; STREPTOCOCCUS PNEUMONIAE; THROMBOCYTE AGGREGATION INHIBITION; THROMBOSIS; UMBILICAL VEIN; VASCULAR ENDOTHELIUM; VASOCONSTRICTION; VASODILATATION; VIBRIO CHOLERAE;

ANIMALS; ANTIOXIDANTS; CARDIOVASCULAR DISEASES; CARDIOVASCULAR SYSTEM; FLAVANONES; HUMANS; MEDICINE, CHINESE TRADITIONAL;

EID: 18444386529     PISSN: 15680061     EISSN: None     Source Type: Journal    
DOI: 10.2174/1568006043586206     Document Type: Review

References (76)

1. Ito, N., Fukushima, S., Tsuda, H. Carcinogenicity and modification of the carcinogenic response by BRA, BHT, and other antioxidants. Crit. Rev. Toxicol., 1985, 15, 109-150.
2. Chen, Z.Y., Bi, Y.R., Su, Y.L., Tsang, S.Y., Huang, Y. Effect of baicalein and acetone extracts of Scutellaria baicalensis on canola oil oxidation. JAOCS, 2000, 77, 73-78.
3. Su, Y.L., Leung, L.K., Bi, Y.R., Huang, Y., Chen, Z.Y. Antioxidant activity of flavonoids isolated from Scutellaria rehderiana. JAOCS, 2000, 77, 807-812.
4. Gao, D., Sakurai, K., Chen, J., Ogiso, T. Protection by baicalein against ascorbic acid-induced lipid peroxidation of rat liver microsomes. Res. Commun. Mol. Pathol. Pharmacol., 1995, 90, 103-114.
5. Gabrielska, J., Oszmianski, J., Zylka, R., Komorowska, M. Antioxidant activity of flavones from Scutellaria baicalensis in lecithin liposomes. Z. Naturforsch [C], 1997, 52, 817-823.
6. Miyahara, M., Ohtaka, H., Katayama, H., Tatsumi, Y., Miyaichi, Y., Tomimori, T. Structure-activity relationship of flavonoids in suppressing rat liver lipid peroxidation. Yakugaku Zasshi, 1993, 113, 133-154.
7. Goldhaber, J.I., Weiss, J.N. Oxygen free radicals and cardiac reperfusion abnormalities. Hypertension, 1992, 20, 118-127.
8. Knight, J.A. Reactive oxygen species and the neurodegenerative disorders. Ann. Clin. Lab. Sci., 1997, 27, 11-25.
9. Abe, J., Berk, B.C. Reactive oxygen species as mediators of signal transduction in cardiovascular disease. In Antioxidants and Cardiovascular Disease. Tardif, J.C, Bourassa, M.G, Ed.; Kluwer Academic Publishers, Dordrecht, The Netherlands, 2000, pp. 57-70.
10. Shao, Z.H., Li, C.Q., Vanden Hoek, T.L., Becker, L.B., Schumacker, P.T., Wu, J.A., Attele, A.S., Yuan, C.S. Extract from Scutellaria baicalensis Georgi attenuates oxidant stress in cardiomyocytes. J. Mol. Cell Cardiol., 1999, 31, 1885-1895.
11. Shao, Z.H., Vanden Hoek, T.L., Qin, Y., Becker, L.B., Schumacker, P.T., Li, C.Q., Dey, L., Barth, E., Halpern, H., Rosen, G.M., Yuan, C.S. Baicalein attenuates oxidant stress in cardiomyocytes. Am. J. Physiol. Heart Circ. Physiol., 2002, 282, H999-H1006.
12. Zweier, J.L., Flaherty, J.T., Weisfeldt, M.L. Direct measurement of free radical generation following reperfusion of ischemic myocardium. Proc. Natl. Acad. Sci. USA, 1987, 84, 1404-407.
13. Hamada, H., Hiramatsu, M., Edamatsu, R., Mori, A. Free radical scavenging action of baicalein. Arch. Biochem. Biophys., 1993, 306, 261-266.
14. Gao, Z., Huang, K., Yang, X., Xu, H. Free radical scavenging and antioxidant activities of flavonoids extracted from the radix of Scutellaria baicalensis Georgi. Biochim. Biophys. Acta, 1999, 1472, 643-650.
15. Vanden Hoek, T.L., Becker, L.B., Shao, Z.H., Li, C.Q., Schumacker, P.T. Preconditioning in cardiomyocytes protects by attenuating oxidant stress at reperfusion. Circ. Res., 2000, 86, 541-548.
16. Halliwell, B. Antioxidant characterization, methodology and mechanism. Biochem. Pharmacol., 1995, 49, 1341-1348.
17. Afanas'ev, I.B., Dorozhko, A.I., Brodskii, V., Kostyuk, A., Potapovitch, A.I. Chelating and free radical scavenging mechanisms of inhibitory actions of rutin and quercetin in lipid peroxidation. Biochem. Pharmacol., 1989, 38, 1763-1769.
18. Hodnick, W.F., Duval, D.L., Pardini, R.S. Inhibition of mitochondrial respiration and cyanide-stimulated generation of reactive oxygen species by selected flavonoids. Biochem. Pharmacol., 1994, 47, 573-580.
19. Chang, W.S., Lee, Y.J., Lu, F.J., Chiang, H.C. Inhibitory effects of flavonoids on xanthine oxidase. Anticancer Res., 1993, 13, 2165-2170.
20. Shieh, D.E., Liu, LT., Lin, C.C. Antioxidant and free radical scavenging effects of baicalein, baicalin and wogonin. Anticancer Res., 2000, 20, 2861-2865.
21. Patel, H.H., Fryer, R.M., Gross, E.R., Bundey, R.A., Hsu, A.K., Isbell, M., Eusebi, L.O., Jensen, R.V., Gullans, S.R., Insel, P.A., Nithipatikom, K., Gross, G.J. 12-Lipoxygenase in opioid-induced delayed cardioprotection, gene array, mass spectrometric, and pharmacological analyses. Circ. Res., 2003, 92, 676-682.
22. Binggeli, C., Sudano, I., Noll, G., Luscher, T.F. Antioxidants and endothelial function: human studies. In Antioxidants and Cardiovascular Disease. Tardif, J.C, Bourassa, M.G, Ed.; Kluwer Academic Publishers, Dordrecht, The Netherlands, 2000, pp. 117-134.
23. Heitzer, T., Schlinzig, T., Krohn, K., Meinertz, T., Munzel, T. Endothelial dysfunction, oxidative stress, and risk of cardiovascular events in patients with coronary artery disease. Circulation, 2001, 104, 2673-2678.
24. Angkeow, P., Deshpande, S.S., Qi, B., Liu, Y.X., Park, Y.C., Jeon, B.H., Ozaki, M., Irani, K. Redox factor-1: an extra-nuclear role in the regulation of endothelial oxidative stress and apoptosis. Cell Death Differ., 2002, 9, 717-725.
25. Wartenberg, M., Budde, P., De Marees, M., Grunheck, F., Tsang, S.Y., Huang, Y., Chen, Z.Y., Hescheler, J., Sauer, H. Inhibition of tumor-induced angiogenesis and matrix-metalloproteinase expression in confrontation cultures of embryoid bodies and tumor spheroids by plant ingredients used in traditional chinese medicine. Lab. Invest., 2003, 83, 87-98.
26. Gao, Z., Huang, K., Xu, H. Protective effects of flavonoids in the roots of Scutellaria baicalensis Georgi against hydrogen peroxide-induced oxidative stress in HS-SY5Y cells. Pharmacol. Res., 2001, 43, 173-178.
27. Hwang, Y.S., Shin, C.Y., Huh, Y., Ryu, J.H. Hwangryun-Hae-Dok-tang (Huanglian-Jie-Du-Tang) extract and its constituents reduce ischemia-reperfusion brain injury and neutrophil infiltration in rats. Life Sci., 2002, 71, 2105-2117.
28. Zhang, J., Snyder, S.H. Nitric oxide in the nervous system. Annu. Rev. Pharmacol. Toxicol., 1995, 35, 213-233.
29. Chen, Z.Y., Su, Y.L., Lau, C.W., Law, W.I., Huang, Y. Endothelium-dependent contraction and direct relaxation induced by baicalein in rat mesenteric artery. Eur. J. Pharmacol., 1999, 374, 41-47.
30. Wakabayashi, I. Inhibitory effects of baicalein and wogonin on lipopolysaccharide-induced nitric oxide production in macrophages. Pharmacol. Toxicol., 1999, 84, 288-291.
31. Chen, Y.C., Shen, S.C., Chen, L.G., Lee, T.J., Yang, L.L. Wogonin, baicalin, and baicalein inhibition of inducible nitric oxide synthase and cyclooxygenase-2 gene expressions induced by nitric oxide synthase inhibitors and lipopolysaccharide. Biochem. Pharmacol., 2001, 61, 1417-1427.
32. 2 and cyclooxygenase/lipoxygenase pathways in the nitric oxide production by murine macrophages stimulated by lipopolysaccharides. Nitric Oxide, 2002, 6, 255-262.
33. Lin, C.C., Chang, S.K., Ting, K.S. Studies on drugs for treatment of hypertension, toxicity and experimental therapy of Scutellaria baicalensis in dogs. Acta Physiol. Sin., 1958, 22, 249-254.
34. Tang, R.Y., Zhou, W.Z. Studies on hypotensive effects of Huangqin. Acta Physiol. Sin., 1958, 22, 91-97.
35. Berger, M.E., Golub, M.S., Chang, C.T., al-Kharouf, J.A., Nyby, M.D., Hori, M., Brickman, A.S., Tuck, M.L. Flavonoid potentiation of contractile responses in rat blood vessels. J. Pharmacol. Exp. Ther., 1992, 263, 78-83.
36. Tsang, S.Y., Chen, Z.Y., Yao, X.Q., Huang, Y. Potentiating effects on contractions by purified baicalin and baicalein in the rat mesenteric artery. J. Cardiovasc. Pharmacol., 2000, 36, 263-269.
37. Huang, Y,, Yao, X.Q., Tsang, S.Y., Lau, C.W., Chen, Z.Y. Role of endothelium in vascular response to flavonoids and polyphenols isolated from Chinese medicinal plants. Acta Pharmacol. Sin., 2000, 21, 1119-1124.
38. Huang, Y., Tsang, S.Y., Yao, X.Q., Lau, CW., Su, Y.L., Chen, Z.Y. Baicalin-induced vascular response in rat mesenteric artery: role of endothelial nitric oxide. Clin. Exp. Pharmacol. Physiol., 2002, 29, 721-724.
39. Huang, Y., Wong, C.M,, Lau, C.W., Yao, X., Tsang, S.Y., Su, Y.L., Chen, Z.Y. Inhibition of nitric oxide/cyclic GMP-mediated relaxation by purified flavonoids, baicalin and baicalein, in rat aortic rings. Biochem. Pharmacol., 2004, 67, 787-794.
40. + channels. Am. J. Physiol. Regul. Integr. Comp. Physiol., 2001, 281, R246-R253.
41. Kimura, Y., Yokoi, K., Matsushita, N., Okuda, H. Effects of flavonoids isolated from Scutellariae radix on the production of tissue-type plasminogen activator and plasminogen activator inhibitor-1 induced by thrombin and thrombin receptor agonist peptide in cultured human umbilical vein endothelial cells. J. Pharm. Pharmacol., 1997, 49, 816-822.
42. Ko, W.H., Law, W.I., Yin, Y.C., Yue, G.G.L., Lau, C.W., Chen, Z.Y., Huang, Y. Stimulation of chloride secretion by baicalein in isolated rat distal colon. Am. J. Physiol. Gastrointest. Liver Physiol., 2002, 282, G508-G518.
43. 2+-mediated Cl secretion by the flavonoid baicalein in intestinal epithelia. J. Biol. Chem., 2004, 279, 39310-39316.
44. Stern, N., Golub, M., Nozawa, K., Berger, M., Knoll, E., Yanagawa, N., Natarajan, R., Nadler, J.L., Tuck, M.L. Selective inhibition of angiotensin II-mediated vasoconstriction by lipoxygenase blockade. Am. J. Physiol., 1989, 257, H434-H443.
45. Kisch, E.S., Jaffe, A., Knoll, E., Stern, N. Role of the lipoxygenase pathway in angiotensin II-induced vasoconstriction in the human placenta. Hypertension, 1997, 29, 796-801.
46. Stanke-Labesque, F., Devillier, P., Bedouch, P., Cracowski, J.L., Chavanon, O., Bessard, G. Angiotensin II-induced contractions in human internal mammary artery: effects of cyclooxygenase and lipoxygenase inhibition. Cardiovasc. Res., 2000, 47, 376-383.
47. Saito, F., Hori, M.T., Ideguchi, Y., Berger, M., Golub, M., Stern, N., Tuck, M.L. 12-Lipoxygenase products modulate calcium signals in vascular smooth muscle cells. Hypertension, 1992, 20, 138-143.
48. Lin, C.C, Shieh, D.E. The anti-inflammatory activity of Scutellaria rivularis extracts and its active components, baicalin, baicalein and wogonin. Am. J. Clin. Med., 1996, 24, 31-36.
49. Cho, H., Ueda, M., Tamaoka, M., Hamaguchi, M., Aisaka, K., Kiso, Y., Inoue, T., Ogino, R., Tatsuoka T., Ishihara, T. Novel caffeic acid derivatives: extremely potent inhibitors of 12-lipoxygenase. J. Med. Chem., 1991, 34, 1503-1505.
50. Sadik, C.D., Sies, H., Schewe, T. Inhibition of 15-lipoxygenases by flavonoids: structure-activity relations and mode of action. Biochem. Pharmacol., 2003, 65, 773-781.
51. McLean, P.G., Aston, D., Sarkar, D., Ahluwalia, A. Protease-activated receptor-2 activation causes EDHF-like coronary vasodilation: selective preservation in ischemia/reperfusion injury: involvement of lipoxygenase products, VR1 receptors, and C-fibers. Circ. Res., 2002, 90, 465-472.
52. 2 in response to norepinephrine. J. Biol. Chem., 2001, 276, 15704-15711.
53. 2 in vascular smooth muscle cells. J. Pharmacol. Exp. Ther., 2003, 304, 761-772.
54. Lacza, Z., Puskar, M., Kis, B., Perciaccante, J.V., Miller, A.W., Busija, D.W. Hydrogen peroxide acts as an EDHF in the piglet pial vasculature in response to bradykinin. Am. J. Physiol. Heart Circ. Physiol., 2002, 283, H406-H411.
55. Natarajan, R., Gu, J.L., Rossi, J., Gonzales, N., Lanting, L., Xu, L., Nadler, J. Elevated glucose and angiotensin II increase 12-lipoxygenase activity and expression in porcine aortic smooth muscle cells. Proc. Natl. Acad. Sci. USA, 1993, 90, 4947-4951.
56. Natarajan, R., Gonzales, N., Lanting, L., Nadler, J. Role of the lipoxygenase pathway in angiotensin II-induced vascular smooth muscle cell hypertrophy. Hypertension, 1994, 23(1 Suppl.), 1142-47.
57. Zafari, A.M., Ushio-Fukai, M., Minieri, C.A., Akers, M., Lassegue, B., Griendling, K.K. Arachidonic acid metabolites mediate angiotensin II-induced NADH/NADPH oxidase activity and hypertrophy in vascular smooth muscle cells. Antioxid. Redox. Signal, 1999, 1, 167-179.
58. 2-terminal kinase. Circ. Res., 1997, 81, 651-655.
59. Wen, Y., Gu, J., Liu, Y., Wang, P.H., Sun, Y., Nadler, J.L. Overexpression of 12-lipoxygenase causes cardiac fibroblast cell growth. Circ. Res., 2001, 88, 70-76.
60. + current activation in bullfrog atrial myocytes. J. Gen. Physiol., 1993, 102, 125-141.
61. Huang, H.C., Wang, H.R., Hsieh, L.M. Antiproliferative effect of baicalein, a flavonoid from a Chinese herb, on vascular smooth muscle cell. Eur. J. Pharmacol., 1994, 251, 91-93.
62. Nishio, E., Watanabe, Y. Role of the lipoxygenase pathway in phenylephrine-induced vascular smooth muscle cell proliferation and migration. Eur. J. Pharmacol., 1997, 336, 267-273.
63. Uddin, M.R., Muthalif, M.M., Karzoun, N.A., Benter, I.F., Malik, K,U. Cytochrome P-450 metabolites mediate norepinephrine-induced mitogenic signaling. Hypertension, 1998, 31, 242-247.
64. Dethlefsen, S.M., Shepro, D., D'Amore, P.A. Arachidonic acid metabolites in bFGF-, PDGF-, and serum-stimulated vascular cell growth. Exp. Cell Res., 1994, 212, 262-273.
65. Natarajan, R., Bai, W., Rangarajan, V., Gonzales, N., Gu, J.L., Lanting, L., Nadler, J.L. Platelet-derived growth factor BB mediated regulation of 12-lipoxygenase in porcine aortic smooth muscle cells. J. Cell Physiol., 1996, 169, 391-400.
66. 2+ influx. Prostaglandins Leukot. Essent. Fatty Acids, 1998, 58, 25-31
67. Wong, B.C., Wang, W.P., Cho, C.H., Fan, X.M., Lin, M.C., Kung, H.F., Lam, S.K. 12-Lipoxygenase inhibition induced apoptosis in human gastric cancer cells. Carcinogenesis, 2001, 22, 1349-1354.
68. Chan, F.L., Choi, H.L., Chen, Z.Y., Chen, P.S.F., Huang, Y. Induction of apoptosis in prostate cancer cell lines by a flavonoid, baicalin. Cancer Lett., 2000, 160, 219-227.
69. Liu, J.J., Huang, T.S., Cheng, W.F., Lu, F.J. Baicalein and baicalin are potent inhibitors of angiogenesis; Inhibition of endothelial cell proliferation, migration and differentiation. Int. J. Cancer, 2003, 106, 559-565.
70. Nyby, M.D., Sasaki, M., Ideguchi, Y., Wynne, H.E., Hori, M.T., Berger, M.E., Golub, M.S., Brickman, A.S., Tuck, M.L. Platelet lipoxygenase inhibitors attenuate thrombin- and thromboxane mimetic-induced intracellular calcium mobilization and platelet aggregation. J. Pharmacol. Exp. Ther., 1996, 278, 503-509.
71. Sekiya, K., Okuda, H. Selective inhibition of platelet lipoxygenase by baicalein. Biochem. Biophys. Res. Commun., 1982, 105, 1090-1095.
72. Michibayashi, T. Platelet aggregating response to platelet activating factor participates in activation of the 12-lipoxygenase pathway in platelets from rabbits. Int. Angiol., 2002, 21, 260-267.
73. Kubo, M., Matsuda, H., Tani, T., Arichi, S., Kimura, Y., Okuda, H. Studies on Scutellariae radix. XII. Anti-thrombic actions of various flavonoids from Scutellariae radix. Chem. Pharm. Bull. (Tokyo), 1985, 33, 2411-2415.
74. Kimura, Y., Matsushita, N., Okuda, H. Effects of baicalein isolated from Scutellaria baicalensis on interleukin 1β- and tumor necrosis factor α-induced adhesion molecule expression in cultured human umbilical vein endothelial cells. J. Ethnopharmacol., 1997, 57, 63-67.
75. Kimura, Y., Okuda, H., Ogita, Z. Effects of flavonoids isolated from Scutellariae radix on fibrinolytic system induced by trypsin in human umbilical vein endothelial cells. J. Nat. Prod., 1997, 60, 598-601.
76. Kimura, Y., Matsushita, N., Yokoi-Hayashi, K., Okuda, H., Effects of baicalein isolated from Scutellaria baicalensis Radix on adhesion molecule expression induced by thrombin and thrombin receptor agonist peptide in cultured human umbilical vein endothelial cells. Planta Med., 2001, 67, 331-334.