Correlation of antioxidative properties and vaso-relaxation effects of major active constituents of traditional Chinese medicines

Meng Zhang, Shi-Lin Chen, Sai-Wang Seto, Yiu-Wa Kwan, Shun-Wan Chan
2009 Pharmaceutical Biology  
Scutellaria baicalensis Georgi ("huang qin"), Ligusticum chuanxiong Hort. ("chuang xiong"), Panax notoginseng (Burk.) F.H. Chen ("san qi"), Uncaria rhynchophylla (Miq.) Jackson. ("gou teng" ), Rhokiola rosea L. ("hong jing tian") and Stephania tetrandra S. Moore ("fang ji") are commonly used traditional Chinese medicine (TCM) for hypertensive patients. The pharmacologically active compounds found in these TCMs are: baicalin, ligustrazine, notoginsenoside R 1, rhynchophylline, salidroside and
more » ... salidroside and tetrandrine, respectively, which possess anti-hypertensive properties with diverse cellular mechanisms. In this study, we attempted to evaluate a possible correlation of the anti-oxidative activities (using the cell-free DPPH assay) and the vaso-relaxation effects (using rat isolated thoracic aorta) of these compounds. In the anti-oxidative study, a relative order of free radical scavenging capacity (SR %) of: baicalin ≥ tetradrine >> salidroside ≥ ligustrazine ≥ rhynchophylline ≈ notoginsenoside R 1 was demonstrated. In the vaso-relaxing study, a relative order of the maximum relaxation response (at 3 mM) of: tetradrine > baicalin >> ligustrazine > notoginsenoside R 1 ≈ rhynchophylline > salidroside was recorded. A positive correlation (R 2 = 0.7741) between the anti-oxidative activity and the vascular relaxation effect of the compounds evaluated was illustrated. In contrast, ascorbic acid only elicited a free radical scavenging activity with no apparent relaxation effect; 3 whereas nifedipine (a Ca 2+ channel blocker) caused a marked vascular relaxation with no obvious free radical scavenging activity. Hence, our results suggest, for the first time, that the therapeutic effect (e.g. anti-hypertensive) of these TCM-oriented drugs, unlike the Western medicine, are probably correlated with the unique anti-oxidative potential of these compounds. for their professional technical support. References Ballew JR, Fink GD (2001) : Charecterization of the antihypertensive effect of a thiazide diuretic in angiotensin II-induced hypertension. J Hypertens 19: 1601-1606. Blokhina O, Virolainen E, Fagerstedt KV (2003): Antioxidants, oxidative damage and oxygen deprivation stress: a review. Ann Bot (Lond) 91: 179-194. Cao YX, Zhang W, He JY, He LC, Xu CB (2006): Ligustilide induces vasodilatation 15 via inhibiting voltage dependent calcium channel and receptor-mediated Ca 2+ influx and release. Vascul Pharmacol 45: 171-176. Ciesielska E, Gwardys A, Metodiewa D (2002): Anticancer, antiradical and antioxidative actions of novel Antoksyd S and its major components, baicalin and baicalein. Anticancer Res 22: 2885-2891. Damiani CE, Rossoni LV, Vassallo DV (2003): Vasorelaxant effects of eugenol on rat thoracic aorta. Vascul Pharmacol 40: 59-66. Frohlich ED, Apstein C, Chobanian AV, Devereux RB, Dustan HP, Dzau V, Fauad-Tarazi F, Horan MJ, Marcus M, Massie B (1992): The heart in hypertension. N. Engl J Med 327: 998-1008. Gardon M, Raizada MK, Katovich MJ, Berecek KH, Gelband CH (2000): Gene therapy for hypertension and restenosis. J Renin Angiotensin Aldosterone Syst 1: 211-216. Giugliano D, Ceriello A, Paolisso G (1995): Diabetes mellitus, hypertension, and cardiovascular disease: which role for oxidative stress? Metabolism 44: 363-368. Griendling KK, Sorescu D, Ushio-Fukai M (2000): NAD(P)H oxidase: role in cardiovascular biology and disease. Circ Res 86: 494-501. Huang Y, Wong CM, Lau CW, Yao X, Tsang SY, Su YL, Chen ZY (2004): Inhibition of nitric oxide/cyclic GMP-mediated relaxation by purified flavonoids, baicalin and baicalein, in rat aortic rings. Biochem Pharmacol 67: 787-794. Li WY, Chan SW, Guo DJ, Yu HF (2007): Correlation between antioxidative power and anticancer activity in herbs from traditional Chinese medicine formulae with 16 anticancer therapeutic effect. Pharm Biol 45: 1-6. Li Y (2005): A clinical study on haunglian fire-purging mixture in treatment of 46 cases of primary hypertension. J Tradit Chin Med 25: 29-33. Liu QY, Li B, Gang JM, Karpinski E, Pang PK (1995): Tetrandrine, a Ca ++ antagonist: effects and mechanisms of action in vascular smooth muscle cells . J Pharmacol Exp Ther 273: 32-39. Ng TB, Liu F, Wang ZT (2000): Antioxidative activity of natural products from plants. Life Sci 66: 709-723. Oettl K, Greilberger J, Zangger K, Haslinger E, Reibnegger G, Jürgens G (2001): Radical-scavenging and iron-chelating properties of carvedilol, an antihypertensive drug with antioxidative activity. Biochem Pharmacol 62: 241-248. Qu ZC (2005): Progress of the Rhodiola herb. Chinese Journal of the Practical Chinese with Modem Medicine 18: 1063-1066. Rajagopalan S, Kurz S, Münzel T, Tarpey M, Freeman BA, Griendling KK, Harrison DG (1996): Angiotensin II-mediated hypertension in the rat increases vascular superoxide production via membrane NADH/NADPH oxidase activation. Contribution to alterations of vasomotor tone. J Clin Invest 97: 1916-1923. Redón J, Oliva MR, Tormos C, Giner V, Chaves J, Iradi A, Sáez GT (2003): Antioxidant activities and oxidative stress byproducts in human hypertension. Hypertension 41:1096-1101. Schlesier K, Harwat M, Bohm V, Bitsch R (2002): Assessment of antioxidant activity
doi:10.1080/13880200902753064 fatcat:tptttlsw4vfrtijr4bmzfzylv4