Disease relevance of Chuanxiongzine

• Our results indicate that tetramethylpyrazine can increase survival rate only if it is administered before the induction of cerebral ischemia [1].
• Tetramethylpyrazine, a drug originally isolated from the rhizome of Ligusticum walliichi, has been used routinely in China for the treatment of stroke and angina pectoris [1].
• Animal studies in the West have shown that tetramethylpyrazine improves coronary blood flow, is short acting, and has a low toxicity [2].
• Here, we have confirmed the beneficial effects of TMP on the hypotension, vascular hyporeactivity to noradrenaline (NA), release of tumour necrosis factor-alpha (TNF-alpha) and nitric oxide (NO) in a rat model of circulatory shock induced by bacterial endotoxin (E. coli lipopolysaccharide, LPS) [3].
• In contrast, animals pretreated with TMP (10 mg kg(-1), i.p.; at 30 min prior to LPS) maintained a significantly higher MAP but the tachycardia was further enhanced at 1-2 h when compared to rats given only LPS (LPS rats) [3].

High impact information on Chuanxiongzine

• 1. Ligustrazine (tetramethylpyrazine, TMP) is a vasodilator that has been reported to have pulmonary selective properties in vivo, but not in vitro [4].
• TMP: tetramethylpyrazine LDH: lactate dehydrogenase ROS: reactive oxygen species DCF: 2',7'-dichlorofluorescein TNF-alpha: tumor necrosis factor-alpha TUNEL: terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate nick end-labeling [5].
• Tetramethylpyrazine (TMP), a compound purified from Rhizoma Ligustici, is a widely used active ingredient in Chinese herbal medicine to treat cardiovascular diseases on account of its vasodilatory actions and antiplatelet activity [5].
• Tetramethylpyrazine (TMPZ) is an active ingredient isolated from a commonly used Chinese herb, Ligusticum wallichii Franchat, which has long been used in China for the treatment of vascular diseases [6].
• Activation of apical CFTR and basolateral Ca(2+)-activated K+ channels by tetramethylpyrazine in Caco-2 cell line [7].

Chemical compound and disease context of Chuanxiongzine

• The effects of tetramethylpyrazine on the incidence of arrhythmias and the release of PGI2 and TXA2 in the ischemic rat heart [8].
• Pretreatment with tetramethylpyrazine increased the 6-Keto-PGF1a concentration to 266 +/- 51 pg/ml (143% of control heart), 471 +/- 89 pg/ml (150% of control heart) and 332 +/- 47 pg/ml (195% of control heart) at 15 min of normoxia, 2 min of hypoxia and 5 min of reoxygenation, respectively (p < 0.05 vs control) [9].
• Anisodamine (ADM, 654-2, 30 mg/kg) and tetramethylpyrazine (TMP, 120 mg/kg) have shown an apparent preventive effect on pulmonary edema (PE) [10].
• The alpha-adrenergic nature of tetramethylpyrazine (TMPZ), a commonly used cardiovascular drug in China, was studied with a combined bradycardia and mydriasis model in the pentobarbital anesthesized rat [11].

Biological context of Chuanxiongzine

• Candidates for cognitive enhancer extracted from medicinal plants: paeoniflorin and tetramethylpyrazine [12].
• We suggest that studies in the whole animal and in the clinic might provide reasons to use tetramethylpyrazine to reduce uterine contractions and tone in pregnant women at term [2].
• Analogues of tetramethylpyrazine affect membrane fluidity of liposomes: relationship to their biological activities [13].
• The results suggest that tetramethylpyrazine and ferulic acid might be used as preventive agents against neuronal diseases associated with oxidative stress [14].
• Scatchard analysis of the effect of tetramethylpyrazine on the saturation profile of [3H]prazosin binding to vascular muscle microsomes of either arterial muscle indicated a substantial increase of Kd values (the affinity for prazosin) without a change in Bmax (maximal binding sites for prazosin) [15].

Anatomical context of Chuanxiongzine

• A possible mechanism of action of tetramethylpyrazine on vascular smooth muscle in rat aorta [16].
• Vascular effects of tetramethylpyrazine: direct interaction with smooth muscle alpha-adrenoceptors [15].
• The interaction of tetramethylpyrazine, a vasoactive ingredient of a Chinese traditional medicinal plant, with the vascular muscle alpha 1-adrenoceptors was investigated by a direct radioligand binding technique using [3H]prazosin and vascular smooth muscle microsomes isolated from dog aorta and mesenteric artery [15].
• Inhibitory mechanisms of tetramethylpyrazine in middle cerebral artery occlusion (MCAO)-induced focal cerebral ischemia in rats [6].
• Tetramethylpyrazine inhibits ATP-activated currents in rat dorsal root ganglion neurons [17].

Associations of Chuanxiongzine with other chemical compounds

• Amiloride and amiloride-related compounds, which shares a common pyrazine ring structure with tetramethylpyrazine and other related derivatives, also inhibits the binding of [3H]prazosin to aortic muscle microsomal membranes [15].
• This increment of both TNF-alpha and nitrate levels was significantly reduced in LPS rats pretreated with TMP [3].
• This study focuses on the protective effect of tetramethylpyrazine in kainate-induced excitotoxicity in rat hippocampus [18].
• Bumetanide, an inhibitor of Na(+)-K(+)-Cl(-)-cotranspoter, inhibited the TMP-induced I(SC) by 96.7% in T84 cells, but only 47.9% in Caco-2 cells [19].
• The present study aimed to investigate the differential activation of Cl(-) and HCO(3)(-) secretion by tetramethylpyrazine (TMP) in human crypt-like cell line, T84, and villus-like cell line, Caco-2, in comparison to the TMP-induced secretory response in freshly isolated rat colonic mucosa [19].

Gene context of Chuanxiongzine

• The early hypotension caused by LPS was slightly, but significantly, prevented by pretreatment with tetramethylpyrazine, suggesting that tetramethylpyrazine affects the endothelial constitutive NOS (eNOS) [20].
• Thus, TMP inhibits the expression of iNOS and mitigates the delayed circulatory failure caused by endotoxic shock in the rat [3].
• This study is to investigate the possible mechanism of beneficial effects of tetramethylpyrazine (TMP) on endotoxic shock which we showed in our preliminary study (Liao et al. 1998; Proc Natl Sci Counc Repub China B 22:46-54) [3].
• Pretreatment of the cells with 100 microM of tetramethylpyrazine or ferulic acid effectively decreased the activation of caspase 3 as well as the expression of p53 and p21(waf1/cip1), and attenuated iron-induced oxidative damage and apoptosis [14].
• 2,3,5,6-Tetramethylpyrazine also inhibits the strain-induced formation of reactive oxygen species (ROS) and phosphorylation of extracellular signal-regulated kinases (ERK) 1/2 [21].

Analytical, diagnostic and therapeutic context of Chuanxiongzine

• In traditional Chinese medicine, Ligusticum wallichii Franchat (Chuan Xiong) and its active ingredient tetramethylpyrazine (TMP) have been used to treat cardiovascular diseases and to relieve various neurological symptoms such as ischemic deficits [22].
• A simple and reliable HPLC method was developed for the determination of 2,3,5,6-tetramethylpyrazine (TMP) in Ephedrae herba [23].
• Analysis of tetramethylpyrazine in Ephedrae herba by gas chromatography-mass spectrometry and high-performance liquid chromatography [23].
• AIM: To investigate the effect of tetramethylpyrazine on hepatic/renal ischemia and reperfusion injury in rats [24].
• Pretreatment with oral administration of tetramethylpyrazine (TMP) prevented such failure [25].

References