川乌炮制工艺优化

目的:优化川乌的炮制工艺参数.方法:以川乌中6种生物碱类成分的含量为指标,采用单因素试验考察川乌炮制时的浸泡条件、干燥条件及蒸制条件.结果:制川乌的最佳炮制工艺参数为40℃水浸泡24 h,111℃加压蒸制1 h,60℃烘干,所得样品中双酯型和单酯型生物碱含量均达到2010年版《中国药典》要求.结论:优选的炮制工艺简便、易行,适合工业化大生产应用.     

老鼠簕生物碱A及其衍生物对α-淀粉酶活性的影响

目的研究老鼠簕生物碱A及其衍生物对-淀粉酶活性的影响,以期为-淀粉酶抑制剂的进一步深入研究提供实验基础及结构依据,并拓展老鼠簕生物碱A及其衍生物的应用范围。方法以老鼠簕生物碱A及其衍生物为待测样品,阿卡波糖为阳性对照,采用Bernfeld法测定比较各化合物对-淀粉酶活性的影响。结果 a-1、a-2、a-3、a-4、a-5、b-7在样品浓度为0.625,1.25,2.5,5.0,10.0 g.L-1时均对-淀粉酶有抑制作用,且在实验浓度范围内随着浓度增加抑制率增大,浓度为10.0 g.L-1时抑制率分别为10.24%、71.52%、63.79%、19.71%、52.76%、38.96%。而a-7、b-3、b-1随浓度的增大,表现出增强-淀粉酶水解活性的趋势。结论推测老鼠簕生物碱A结构中的酚羟基是其对-淀粉酶起抑制作用的基本药效基团,对老鼠簕生物碱A进行结构修饰时,保留4-位酚羟基并在7-位引入氯原子、酰基或含羟基取代基均有利于抑制-淀粉酶的活性;而以乙酰氧基取代4-位酚羟基,并使7-位用含羧酸取代基取代或3-位无取代或以小分子基团取代时均有利于增强-淀粉酶的水解活性。     

C19型二萜生物碱药理活性和毒性研究进展

C19型二萜生物碱是一类来源广泛、结构复杂、生物活性多样的植物成分,一直以来为化学家和药理学家所重视.本文综述了近年来C19型二萜生物碱的药理活性和毒性研究进展,为其深度开发利用提供一定参考.     

Comparison of the selected secondary metabolite content present in the cancer-bush Lessertia (Sutherlandia) frutescens L. Extracts

Extracts of in vitro leaves, field leaves and seeds of the leguminous plant Lessertia frutescens were analyzed using spectrophotometric and gravimetric methods, to the effect of quantitative comparison of their phenolic, flavonoid, alkaloid and saponin contents. As compared to the field leaves and seeds, saponins were found to be most abundantly represented in in vitro leaves, followed by phenolics, flavonoids and alkaloids. The extracts were also qualitatively analyzed so as to evaluate the presence of other phytochemicals of medicinal interest. This qualitative analysis indicated the presence of tannins, phlobatannins and cardiac glycosides. Having in mind the documented therapeutic use of these phytochemicals, the results of this study offer a strong rationale for further animal and clinical investigations of L. frutescens extracts.     

青风藤中总生物碱的气相色谱-质谱联用分析

目的 采用索氏提取法对青风藤中总生物碱进行提取分离,并利用气相-质谱联用(GC-MS)方法 ,对其化学成分进行分析. 方法 采用90%无水乙醇提取,盐酸酸化后,氨水碱化后三氯甲烷萃取,利用GC-MS对总生物碱中的化学成分进行分离分析,并对其中的15种化学成分进行鉴定. 结果该方法提取时青藤碱含量高,达到80.18%,安贝灵碱3.44%,光千金藤碱3.05%. 采用峰面积归一化法计算各成分相对百分含量,所鉴定的成分占总流出峰面积的95.1%. 结论 实验结果为进一步开发研究青风藤中生物碱提供依据.     

大孔树脂分离纯化荷叶中的黄酮与生物碱

目的研究确定荷叶的最佳分离纯化工艺。方法采用不同的树脂柱进行吸附,用分光光度法测定黄酮与生物碱的含量,用HPLC验证荷叶碱的含量,对工艺进行评价。结果 D-101型树脂较适合荷叶中的生物碱与黄酮的分离与纯化,在确定的工艺下,荷叶碱转移得率达到57.2%。结论该工艺适合荷叶中的黄酮与生物碱的分离与富集。     

雷公藤总生物碱滴眼液对大鼠自身免疫性葡萄膜炎的作用

目的: 探讨雷公藤总生物碱滴眼液对大鼠葡萄膜炎的治疗作用。方法: 从昆明山海棠中提取生物碱,并制备3种浓度的雷公藤总生物碱滴眼液。将实验性葡萄膜炎Lewis大鼠80只随机分为A(生理盐水治疗组)、B(0.0125％雷公藤总生物碱滴眼液组)、C(0.025％雷公藤总生物碱滴眼液组)、D(0.05％雷公藤总生物碱滴眼液)和E(典必殊滴眼液组)5组,每组16只大鼠,并分别给予生理盐水、3种不同浓度雷公藤总生物碱滴眼液及典必殊滴眼液点眼。各组于免疫后第9 d开始每天使用滴眼液点眼,于免疫后3、6、9、12、15、18、21、24 d每组各处死 2只大鼠,取4只眼球(n=4)行常规组织切片及HE染色;根据病理切片的炎症反应程度分为5级并按炎症反应程度给予相应评分;将各组评分结果进行非参数检验统计分析。结果: 将各组大鼠炎症病理反应评分相比较,A组、B组和C组在各个时点均无显著差异;D组和E组自免疫后第15 d开始与前3组之间差异显著;D组和E组在各个时点的炎症反应均无显著差异。结论: 0.05％雷公藤总生物碱滴眼液可有效抑制Lewis大鼠实验性葡萄膜炎眼病理改变。     

Hepatoprotective effects of aqueous leaf extract and crude isolates of Murraya koenigii against in vitro ethanol-induced hepatotoxicity model

Medicinal plants constitute a principal health care resource corroborating their gradual acceptance by the global population. The ethno medicinal plant, Murraya koeniggi (Curry-leaf tree) as is native to India exhibits diverse biological activities. Unpublished data from our laboratory revealed hepatoprotective activity of its crude aqueous extract against ethanol-induced hepatotoxicity in experimental animals. Chronic ethanol consumption diminishes the cellular antioxidant levels through free radical induced injury causing hepatitis and cirrhosis with mortality in severe cases. This provided a rationale for studying its mechanistic approaches in terms of modulation of antioxidant defenses for probable hepatoprotective activity against ethanol-induced hepatotoxicity in vitro.Based on the inhibitory concentration (IC₅₀) obtained from the cell viability assay, graded concentrations of 100 μg/ml and 500 μg/ml of aqueous extract (WE), isolated carbazole alkaloids (CA) and tannin (T) fraction were chosen to study the hepatoprotective activity against ethanol-induced hepatotoxicity using liver carcinoma cell lines (Hep G₂). Their antioxidant activity with anti-lipid peroxidation potential (LPO), effects on protein content, liver metabolizing enzymes viz., glutathione (GSH), superoxide dismutase (SOD), catalase (CAT) and the morphology of the cells were studied as parameters of hepatoprotection.The tannins and the carbazole alkaloids from the aqueous extract exhibited excellent hepatoprotective activity with respect to the different parameters studied and maintained normal morphology even after ethanolic challenge to the cells as comparable to the protection offered by the standard drug l-ornithine l-aspartate (LOLA).The modulating effect of the aqueous extract and isolates on liver metabolizing enzymes, reduction in lipid peroxidation and decreased cellular damage were found to contribute to the hepatoprotective activity.     

乌药总生物碱提取工艺的优选及镇痛作用的研究

目的优选乌药总生物碱（TALR）的提取工艺并研究其镇痛作用。方法采取乙醇回流法提取,考察乙醇浓度、乙醇用量、提取时间、提取次数影响,进行L9（34）正交试验设计,以乌药总生物碱的紫外吸收峰最大吸光度A值为指标进行优选。镇痛实验取最佳提取方法所得TALR的不同浓度水溶液ig给予小鼠后,采用醋酸小鼠扭体法研究TALR的镇痛作用。结果优选工艺为：加入14倍量95%乙醇提取1h,酸溶碱沉得TALR,因其A值远高于其他工艺,故判断此法所得TALR质量分数相对最高。药理实验表明TALR可显著减少小鼠扭体次数。结论优选工艺简单可行,质量分数较高;TALR具有较强的镇痛作用。     

Effect of 3‐Alkylpyridine Marine Alkaloid Analogues in Leishmania Species Related to American Cutaneous Leishmaniasis

A series of oxygenated analogues of marine 3‐alkylpyridine alkaloids were synthesized, and their leishmanicidal activity was assayed. All compounds were prepared from 3‐pyridinepropanol in few steps and in good yields. The key step for the synthesis of these compounds was a classic Williamson etherification under phase‐transfer conditions. Besides toxicity in peritoneal macrophages, the compounds exhibited a significant leishmanicidal activity. Of twelve compounds tested, five showed a strong leishmanicidal activity against promastigote forms of Leishmania amazonensis and L. braziliensis with IC₅₀ below 10 μm . Compounds 11 , 14 , 15, and 16 showed a strong leishmanicidal activity on intracellular amastigotes (IC₅₀ values of 2.78; 0.27; 1.03, and 1.33 μm , respectively), which is unlikely to be owing to the activation of nitric oxide production by macrophages.