羟基积雪草苷的抗高血压作用及其特点研究

目的:探讨羟基积雪草苷(madecassoside,MC)抗高血压作用及其作用特点。方法:利用高血压模型大鼠及正常大鼠,采用清醒及麻醉状态下血压直接测量法,研究MC对血压的影响及其作用特点。结果:MC降低了高血压模型大鼠的收缩压(SBP)、舒张压(DBP)、平均动脉压(MAP)及心率(HR);而对正常大鼠血压及心率无明显影响。结论:MC具有降血压作用;但对正常大鼠血压无明显影响。     

羟基积雪草苷对转基因肌萎缩侧索硬化小鼠的治疗作用

目的探讨羟基积雪草苷对铜锌超氧化物歧化酶(Cu,Zn superox ide d ism u tase,SOD 1)-G 93A突变肌萎缩侧索硬化(am yotroph ic latera l scleros is,ALS)小鼠的治疗作用。方法通过行为学和组织学测定,观察羟基积雪草苷对SOD 1-G 93A突变ALS小鼠发病时间、生存时间、运动功能变化和神经元病理改变的影响。结果羟基积雪草苷(61.1±11.0)和(185.6±18.7)m g/(kg.d)在小鼠日龄70 d时开始给药至死亡,能分别延长SOD 1-G 93A突变ALS小鼠的生存时间11.4和9.4 d,但对发病时间无影响;同时(61.1±11.0)m g/(kg.d)组小鼠在肌力缓慢下降期运动功能降低减缓,与对照组比较差异显著(P<0.05)。120 d时L 2~5组织切片显示两治疗组脊髓前角运动神经元数明显高于SOD 1-G 93A对照组(P<0.05),多数运动神经元胞浆中仍有尼氏体存在。结论羟基积雪草苷对SOD 1-G 93A突变转基因小鼠运动神经元变性有保护作用,能延长小鼠的生存时间。     

HPLC-CAD法分离测定三金片中同分异构体积雪草苷B和羟基积雪草苷

目的 建立一种高效液相色谱-电喷雾检测器(HPLC-CAD)法分离测定三金片中积雪草苷B和羟基积雪草苷2个同分异构体含量的方法.方法 采用Thermo AcclaimTM C30色谱柱,甲醇-乙腈-水(35 ∶ 8 ∶ 57)为流动相,柱温35℃,CAD气化温度为50℃,采集频率为10Hz,分离测定积雪草苷B和羟基积雪...     

羟基积雪草苷对脂多糖诱导大鼠发热及相关炎症因子影响研究

目的:观察羟基积雪草苷的解热作用。方法:腹腔注射脂多糖100μg/kg制备大鼠发热模型,连续6h监测大鼠体温变化,6h后取血、肝脏和脑组织。羟基积雪草苷造模前连续3天灌服,对乙酰氨基酚组于造模前30min一次性腹腔注射50mg/kg。肝组织髓过氧化物酶(MPO)活性检测采用MPO试剂盒,酶联免疫法(ELISA)测脑组织前列腺素E2(PGE2)和血浆白介素-6(IL-6)含量。结果:羟基积雪草苷10、20和40mg/kg组体温明显低于模型组,其中40mg/kg组与对乙酰氨基酚组相当。与模型组比较,羟基积雪草苷3个剂量组明显降低发热后6h肝组织MPO活性、脑组织PGE2和血浆IL-6的含量。结论:羟基积雪草苷具有解热作用,该作用可能与抑制抑制炎症因子PGE,IL-6,MPO活性有关。     

Possible mechanisms of vasorelaxation for 5,7-dimethoxyflavone from Kaempferia parviflora in the rat aorta

The present study investigated the vascular effects of 5,7-dimethoxyflavone (DMF), isolated from the rhizomes of Kaempferia parviflora (KP), on rat isolated aortic rings and its possible mechanisms. DMF (1-100 μM) caused concentration-dependent relaxations in aortic rings precontracted with methoxamine. This effect was significantly reduced by removal of the endothelium, and after pretreatment with N(G)-nitro-L-arginine methyl ester (L-NAME, 300 μM), indomethacin (10 μM) and 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one (ODQ, 10 μM), but not 9-(tetrahydro-2-furanyl)-9H-purine-6-amine (SQ22536, 100 μM). Relaxant responses to DMF were significantly inhibited by high KCl (60 mM) in both endothelium-intact and -denuded rings. In addition, the relaxations to DMF were significantly reduced by pretreatment with tetraethylammonium (TEA, 5 mM), glibenclamide (10 μM), 4-aminopyridine (1 mM) or barium chloride (10 μM). Preincubation with DMF (10 and 100 μM) for 30 min significantly inhibited the contractile responses to CaCl(2) in a Ca(2+)-free, high K(+) buffer. The present study demonstrated that DMF causes endothelium-dependent relaxation that is partly mediated by NO-cGMP and cyclooxygenase pathways. Interestingly, DMF-induced responses are mainly due to increasing K(+) efflux, and inhibition of Ca(2+) influx from the extracellular space. The vasodilator effects of DMF provide experimental support for the potential use of KP as a medical plant in the treatment of cardiovascular diseases.     

Endothelium-dependent induction of vasorelaxation by the butanol extract of Phellinus igniarius in isolated rat aorta

The butanol extract of Phellinus igniarius (BPI) induced relaxation of the phenylephrin e-precontracted rat aorta in a dose-dependent manner, and its effect was abolished by the removal of functional endothelium. Pretreatment of the aortic tissues with N(G)-nitro-L-arginine methyl ester (L-NAME), methylene blue, or 1H-[1,2,4]-oxadiazole-[4,3-alpha]-quinoxalin1-one (ODQ) inhibited the vascular relaxation induced by BPI. BPI-induced vascular relaxations were also markedly attenuated by the addition of verapamil or diltiazem, while the relaxant effect of BPI was not blocked by pretreatment with indomethacine, glibenclamide, tetraethylammonium (TEA), atropine, or propranolol. Incubation of endothelium-intact rat aorta with BPI increased the production of cGMP in a dose-dependent manner. These results suggest that BPI dilates vascular smooth muscle via endothelium-dependent nitric oxide-cGMP signaling pathway, with the possible involvement of L-type Ca(2+) channels.     

Purification of a dimethyladenosine compound from silkworm pupae as a vasorelaxation substance

To identify the active substance in the male silkworm pupae that strengthens men's vitality, the vasorelaxation activity was determined by measuring the vascular endothelial nitric oxide (eNO) produced in calf pulmonary artery endothelial (CPAE) cells treated with extracts from the pupae. Dried silkworm male pupae were extracted with ethanol and suspended in water, then partitioned with hexane, chloroform, ethylacetate, and butanol, sequentially. Among these fractions, the aqueous fraction had maximal NO production (156.87 microM/200 microl well, 10 mg/ml) and minimal cytotoxicity (IC50 362.3 mg/ml). The vasorelaxation substances (VAS) from the aqueous fraction were isolated by a combination of gel filtration and anion-exchange chromatography on DEAE Sephadex A-25 and reverse phase-HPLC. Their chemical structures were determined on the basis of their spectroscopic parameters of EI-MS, MALDI-TOF MS, 1H and 13C NMR, 1H-1H COSY, and GC-MS spectral data. The active substance was subsequently identified as a dimethyladenosine and dimethyladenosine-5'-L-arabinose that has phosphodiesterase (PDE) inhibition activity. This compound was shown to inhibit PDE4 activity in a dose-dependent manner. Also, it inhibited the PDE5 activity of cyclic-GMP-specific PDE5 enzyme. These results imply that dimethyladenosine may be a lead compound for the development and improvement of vasculogenic impotence drugs through phosphodiesterase inhibition and NO production in endothelial cells.     

甲状腺功能亢进症中医证候分布规律的研究

目的 探讨甲亢的中医证候分布规律及各证候所表现的症状与激素的相关性.方法 对78例甲亢患者的中医证候进行判断,分析证候与患者一般情况(性别、年龄等)的相关性及证候中的症状与激素的相关性.结果 78例甲亢患者中阴虚阳亢占43.6%;痰火内扰占30.8%:心肝火旺占25.6%.各证候中症状的轻重与甲状腺激素均呈正相关关系(r为正值,P＜0.05),与甲状腺激素水平无直线关系(P＞0.05).结论 甲亢的中医证候以阴虚阳亢最常见;在痰火内扰、心肝火旺、阴虚阳亢三型中,甲状腺激素水平越高,则各证型对应的症状可能越重.     

甲状腺功能亢进症中医证候分布规律的研究

Objective To Analyze the distribution characteristics of Hyperthyroidism's syndrome and the relationship between symptoms and thyroid hormones. Methods The TCM syndromes of a total of 78 patients with hyperthyroidism were differentiated. The relationship between syndrome and general condition of patients (gender and age, etc.) were analyzed;correlation between symptoms and thyroid hormones were also studied. Results Of all 78 patients, patients with yin deficiency and hyperactive yang accounted for 43.6%; patients with internal disturbance of phlegm-fire accounted for 30.8 %; and patients with hypteracitivity of heart-fire and liver-fire accounted for 25.6%. The severity of all the symptoms showed positive correlation with hyroid hormones (the value of r is positive, P＜0.05); and no linear relationship with TSH (P＞0.05).Conclusion The syndrome of yin deficiency and hyperactive yangI was the most common syndrome type. Thyroid hormones had direct proportion with the severity of syndrome.     

The mechanism of vasorelaxation induced by Schisandra chinensis extract in rat thoracic aorta

Aim of the study

Schisandra chinensis (SC) is a known medical herb for the treatment of cardiovascular symptoms associated with menopausal symptoms in Korea. However, the pharmacological action mechanisms involved have not been well studied. This study was aimed to investigate the vascular effects of SC in rat thoracic aorta.

Materials and methods

We isolated the hexane, chloroform, and methanol extracts from SC and evaluated their vasodilatory effects in the rat thoracic aorta.

Results

Hexane extracts of SC (SCHE, 5 × 10⁻⁵ to 10⁻³ g/L) caused a concentration-dependent relaxation in both endothelium-intact and -denuded aortas. The relaxant effect of SCHE on the endothelium-intact aorta was more prominent than on the endothelium-denuded aorta. The former was significantly attenuated by L-NAME, a nitric oxide synthase inhibitor, and ODQ, a soluble guanyl cyclase inhibitor, but not by tetraethylammonium, a nonselective blocker of K⁺ channels, and indomethacin, a cyclooxygenase inhibitor. Furthermore, SCHE caused nitrite production as well as eNOS activation in aortic segments, suggesting implication of NO signal pathway in SCHE-induced relaxation. In endothelium-denuded aorta, SCHE-induced vasorelaxation was also attenuated by calyculin A, an inhibitor of myosin light chain (MLC) phosphatase, but not by ML-9, a MLC kinase inhibitor, suggestive of implication of MLC phosphatase activation. Phenylephrine-enhanced MLC phosphorylation ratio was significantly attenuated by SCHE, which was recovered to the control level by pretreatment with calyculin A.

Conclusions

Taken collectively, these findings suggest that the vascular relaxation evoked by SCHE was mediated by not only endothelium dependent NO pathway but also direct effect on vascular smooth muscle cell via dephosphorylation of MLC.