黄麦颗粒制备工艺研究

摘 要 目的： 研究黄麦颗粒的制备工艺,确定最佳工艺条件。方法: 采用单因素筛选法和正交设计法,进行提取工艺和成型工艺优选。结果:最佳工艺为处方量的7味药材,加8倍量水,煎煮2 h,提取3次,合并水提液,减压浓缩、干燥成干浸膏。干膏粉与适量糊精混合均匀后,加40%乙醇湿法制粒,干燥后整粒,即得。结论: 所选工艺科学、合理、稳定,适合工业化生产。     

补肾通络方中马钱苷、阿魏酸和二苯乙烯苷的体内药代动力学研究

研究灌胃补肾通络方后大鼠血浆中马钱苷、阿魏酸和二苯乙烯苷药代动力学特征。采用液-液萃取法处理血浆样品;HPLC-UV检测含量,色谱柱为Johnson spherigel C₁₈(4.6 mm×250 mm, 5 μm),流动相为甲醇-0.01%冰醋酸水溶液,梯度洗脱,流速为1 mL·min^-1,柱温为30 ℃,检测波长:马钱苷为235 nm,阿魏酸和二苯乙烯苷为320 nm,进样量为10 μL。采用DAS 2.0软件对所测数据进行处理,得到大鼠血浆中马钱苷、阿魏酸和二苯乙烯苷的主要药动学参数如下:C_max分别为(0.369±0.042),(0.387±0.071),(0.233±0.044) mg·L^-1;t_max分别为(0.226±0.022),(0.282±0.031),(0.233±0.044) h;t_1/2β分别为(6.89±0.20),(10.7±0.11),(6.93±0.090) h;AUC_0-∞分别为(1.91±0.36),(3.22±0.52),(1.52±0.33) mg·h·L^-1;AUC_0-t分别为(1.62±0.33),(2.58±0.43),(1.30±0.30) mg·h·L^-1;CL分别为(20.2±4.0),(1.39±0.23),(31.7±6.9) L·h^-1·kg^-1。药代动力学研究结果表明,灌胃补肾通络方后马钱苷、阿魏酸和二苯乙烯苷药动学曲线均符合血管外给药二室模型,且3种成分吸收快,马钱苷和二苯乙烯苷消除速度中等,阿魏酸消除慢(但生物利用度为最高),每天给药3次能维持血药浓度,适合制成普通口服制剂。     

A new lignan glucoside from the stems of <Emphasis Type="Italic">Callicarpa japonica</Emphasis> Thunb. var. <Emphasis Type="Italic">luxurians</Emphasis> Rehd.

A new lignan glucoside (1) was isolated from the stems of Callicarpa japonica Thunb. var. luxurians Rehd. (Verbenaceae), along with six known lignan glucosides and three known triterpenoids. The chemical structure of 1 was characterized as (+)-lyoniresinol 3α-O-(6″-3,5-dimethoxy-4-hydroxybenzoyl)-β-d-glucopyranoside on the basis of spectroscopic data. In addition, the radical-scavenging effect of four lignans on the stable free radical 1,1-diphenyl-2-picrylhydrazyl was examined. Among the tested compounds, three compounds, including 1, showed almost the same scavenging activity as that of α-tocopherol.     

Norditerpenoid and dianthramide glucoside alkaloids from cultivated<Emphasis Type="Italic">aconitum</Emphasis> species from Korea

A new norditerpene alkaloid named 8-O-methylhypaconine (1) was isolated along with twelve known alkaloids from the underground parts of an unknown species of Aconitum plant culti vated in Korea. Among the known alkaloids, two dianthramide glucosides, N-(2'-beta-glucopyra nosyl-5'-hydroxysalicyl)-5-hydroxyanthranilic acid methyl ester (2) and N-(2'-beta-glucopyranosyl-5'-hydroxysalicyl)-5-hydroxy-6-methoxyanthranilic acid methyl ester (3), were isolated from Aconitum plants for the first time. The structures were established on the basis of chemical and spectroscopic methods.     

Isolation of constituents and anti-complement activity from<Emphasis Type="Italic">Acer okamotoanum</Emphasis>

A novel acylated sterol glucoside (1) along with four known compounds, beta-amyrin acetate (2), 3beta,24-dihydroxytaraxer-14-ene (3), cleomiscosin A (4), and cleomiscosin C (5), were isolated from the leaf and twig of Acer okamotoanum Nakai (Aceraceae). The structure of the new compound was determined to be beta-sitosterol glucoside-3'-O-hexacosanoicate based on chemical and spectroscopic analyses. In addition, the novel compound was found to exhibit a significant inhibitory effect (IC50 value of 0.2 microM) on the complement system activated by the classical pathway.     

Chronic cyanidin-3-glucoside administration improves short-term spatial recognition memory but not passive avoidance learning and memory in streptozotocin-diabetic rats

This research study was conducted to evaluate the efficacy of chronic cyanidin‐3‐glucoside (C3G) on alleviation of learning and memory deficits in diabetic rats as a result of the observed antidiabetic and antioxidant activity of C3G. Male Wistar rats were divided into control, diabetic, C3G‐treated‐control and ‐diabetic groups. The C3G was administered i.p. at a dose of 10 mg/kg on alternate days for eight weeks. For evaluation of learning and memory, initial latency (IL) and step‐through latency (STL) were determined at the end of study using passive avoidance test. Meanwhile, spatial recognition memory was assessed as alternation in the Y‐maze task. Oxidative stress markers in brain tissue were also measured. It was found that the alternation score of the diabetic rats was lower than that of control (p < 0.01) and C3G‐treated diabetic rats showed a higher alternation score as compared to diabetic group (p < 0.05). Diabetic rats also developed a significant impairment in retention and recall in passive avoidance test (p < 0.01) and C3G treatment of diabetic rats did not produce any significant improvement. Meanwhile, increased level of malondialdehyde (MDA) in diabetic rats was significantly reduced following C3G treatment (p < 0.05). Taken together, chronic C3G could improve short‐term spatial recognition memory disturbance in the Y‐maze test but not retention and recall capability in passive avoidance test in STZ‐diabetic rats. Copyright © 2012 John Wiley & Sons, Ltd.     

固相萃取-HPLC法测定延年康口服液中二苯乙烯苷的含量

目的建立延年康口服液中二苯乙烯苷的含量测定方法。方法采用固相萃取-HPLC法,色谱柱为XTerra RP18（5μm 3.9mm×150mm）,流速0.8 mL.min-1,乙腈∶水（20∶80）为流动相,检测波长为320nm。结果二苯乙烯苷的线性范围为0.0504μg～0.3024μg,r=0.9992,平均回收率为98.77%,RSD=1.64%（n=6）。结论方法简便、快速、准确,适合该口服液中二苯乙烯苷的含量测定。     

Tetrahydroxy stilbene glucoside reduces the cognitive impairment and overexpression of amyloid precursor protein induced by aluminum exposure

Objective

Excessive aluminum (Al) exposure impairs neurocognitive function in humans and animals. Epidemiologic studies have shown a potential linkage between chronic Al exposure and Alzheimer’s disease. The present study aims to evaluate the effects of tetrahydroxy stilbene glucoside (TSG), the extract from herbal medicine Polygoni Multiflori, on cognitive impairment and the over-expression of hippocampal amyloid precursor protein (APP) induced by chronic exposure to Al in rats

Methods

Rats were treated with 0.3% aluminum chloride (AlCl3) prepared in the drinking water for 90 d. AlCl₃-treated animals were then randomly assigned to receive vehicle, TSG (4 g/kg), or Vitamin E (VE; 40 mg/kg) treatment for 5 months. VE served as a positive control. The effect of TSG was evaluated by passive avoidance task, and APP expression was evaluated by Western blotting.

Results

Following exposure to AlCl₃ for 90 d, animals displayed a striking decrease (>80%) in step-through latency in the passive avoidance task and a significant increase in the expression of APP in the hippocampus. Both TSG and VE significantly ameliorated the performance impairment in the passive avoidance task, and suppressed the over-expression of APP. Moreover, the effects of TSG, but not of VE, were in a time-dependent manner.

Conclusion

TSG may possess therapeutic effects against Alzheimer’s disease.     

HPLC法测定安神补脑液中2，3，5，4′-四羟基二苯乙烯-2-O-β-D-葡萄糖苷的含量

目的：建立高效液相色谱法测定安神补脑液中2,3,5,4’-四羟基-苯乙烯-2-O-β-D-葡萄精苷的方法。方法：色谱柱为Hypersil ODS2（4．6mill×150mill,5μm）,流动相为乙腈-水（25：75）,检测波长为320nm,梓温25℃。结果：二苯乙烯苷在0．0108～0．0540mg／nd范围内呈良好线性天系（R2=0.9991）,平均回收率为98．7％,RSD为2．5％。结论：本法简单,准确,重现性好,可用于安神补脑液的质量控制。     

Pharmacological studies on hypotensive, diuretic and vasodilator activities of chrysin glucoside from Calycotome villosa in rats

The present study was undertaken in normotensive anaesthetized male rats that received a continuous perfusion of a chrysin glucoside isolated from the flowers and leaves of Calycotome villosa subsp intermedia at a dose of 2.5 mg/kg, or furosemide (control diuretic) at a dose of 0.5 mg/kg. Compared with the control rats receiving NaCl (0.9%), the urine flow, glomerular filtration and electrolyte excretion (Na+, K+) increased significantly in rats treated with chrysin glucoside (p < 0.001). A similar effect was observed in the rats perfused with furosemide. Intravenous injections of bolus doses (1-3 mg/kg) of the chrysin glucoside to anaesthetized rats elicited an immediate and dose-dependent decrease in mean arterial blood pressure (MABP). Pretreatment of the rats with the nitric oxide synthase inhibitor, l-NOArg (10 mg/kg), reduced partially, but significantly (p < 0.01), the maximal decrease in MABP elicited by chrysin glucoside. In the rat isolated aorta preparation, chrysin glucoside (10-100 microm) inhibited in a concentration-dependent manner the noradrenaline (1 microm) induced contractions (IC(50) = 52 microm). This relaxant activity of chrysin glucoside was significantly reduced by incubation of the endothelium-intact rings with l-NOArg (100 microm), (80 +/- 4.7% vs 48 +/- 5.06% in the absence of L-NOArg). In conclusion, these results demonstrate a diuretic and hypotensive action of a chrysin glucoside from Calycotome villosa in anaesthetized rats and indicating an action on renal function, and an active vascular relaxation mediated partially through nitric oxide release.