骆驼蓬生物碱抗炎和免疫调节的药理作用机制研究进展

综述骆驼蓬生物碱的抗炎和免疫作用机制研究进展。骆驼蓬属植物的化学成分主要为生物碱类成分,具有DNA拓扑异构酶活性及细胞毒作用,对淋巴细胞、细胞因子有免疫作用,同时具有抗炎和镇痛作用。     

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。     

延胡索中生物碱成分的研究

目的 提取分离延胡索中的生物碱供延胡索种质评价使用。方法 运用色谱学和波谱学方法分离鉴定延胡索中的生物碱。结果 从延胡索总碱中分离得到了13种生物碱，鉴定了其中12种生物碱的结构，分别为:d-紫堇碱，四氢巴马亭，脱氢紫堇碱，四氢黄连碱，四氢小檗碱，异紫堇球碱，原托品碱，四氢非洲防己胺，氯仿巴马亭，saulatine，海罂粟碱，脱氢海罂粟碱。结论 生物碱saulatine为首次从罂粟科植物中分得，异紫堇球碱为首次从延胡索中分得。     

巴豆生物碱部位HPLC特征指纹图谱研究

目的:建立巴豆生物碱部位的高效液相指纹图谱。方法:色谱柱Waters Symmetry C18(4.6 mm×250 mm,5μm),甲醇-0.2%乙酸水流动相系统梯度洗脱,流速0.8 mL.min-1,检测波长292 nm,温度28℃。结果:对10批巴豆药材进行了测定,建立了巴豆生物碱部位的指纹图谱,共有13个共有峰,指认了两种主要生物碱巴豆苷和木兰花碱。结论:该方法可为巴豆的研究和质量控制提供依据。     

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.     

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 Unpublished data from our laboratory revealed hepatoprotective activity of its crude aqueous extract against ethanol-induced hepatotoxicity in experimental animals.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。     

秃疮花生物碱类化学成分研究

目的 为明确秃疮花Dicranostigma leptopodum的药效物质基础,系统研究秃疮花生物碱类化学成分。方法 利用普通硅胶柱色谱对秃疮花的生物碱类化学成分进行提取、分离和纯化,并利用超导核磁共振等现代光谱和波谱技术鉴定化合物的结构。结果 从秃疮花中发现11个异喹啉类生物碱,其中2个萘菲啶类、1个吗啡烷类、4个阿扑菲类和4个普罗托品类生物碱化合物,结构分别鉴定为：二氢血根碱（1）、6-丙酮基-5, 6-二氢血根碱（2）、青风藤碱（3）、秃疮花红碱（4）、异紫堇碱（5）、紫堇碱（6）、N-甲基莲叶桐文碱（7）、顺式普罗托品季铵盐（8）、反式普罗托品季铵盐（9）、原阿片碱（10）、别隐品碱（11）。结论 除化合物5、6、10和11,其余化合物均为首次从该植物中分离得到。     

NKA-9型大孔树脂纯化蟾皮总生物碱工艺

目的:建立NKA-9型大孔树脂纯化蟾皮总生物碱的工艺条件。方法:以蟾皮总生物碱含量(5-羟色胺计)作为考察指标,优化NKA-9型大孔树脂吸附与解析的工艺条件。结果:优选出的最佳纯化工艺为NKA-9型大孔树脂在25℃进行吸附,样品溶液pH 9,上样量为4 BV,吸附时间为8～10 h,先用6 BV水洗,然后用3 BV70%的乙醇洗脱。结论:该工艺可用于蟾皮总生物碱的纯化。     

Developmental patterns of phenylpropylamino alkaloids accumulation in khat (Catha edulis, Forsk.)

Khat (Catha edulis Forsk., Celastraceae) is a perennial shrub that was introduced to Israel by Yemenite immigrants. Khat young leaves are chewed as a stimulant. The main stimulating active principles in this plant are the phenylpropylamino alkaloids (-)-cathinone [(S)-alpha-aminopropiophenone], (+)-cathine [(+)-norpseudoephedrine] and (-)-norephedrine. A novel GC-MS analysis method for the quantitative determination of phenylpropylamino alkaloids and their putative precursor 1-phenyl-1,2-propanedione in khat leaves was developed. We found a marked diversity in the phenylpropylamino alkaloids content and composition in 9 different accessions originated in seedlings and in the commercial cultivar "Mahanaim". The highest 1-phenyl-1,2-propanedione and (-)-cathinone levels occur in young leaves, the part traditionally chewed for its psycho-stimulating properties. Older leaves lack (-)-cathinone but contain the less active (+)-cathine and (-)-norephedrine. Young stems and flowers also contain 1-phenyl-1,2-propanedione, (-)-cathinone, (+)-cathine and (-)-norephedrine. We report the presence of a (-)-cathinone reductase in khat leaves capable of reducing (-)-cathinone to (+)-cathine in the presence of NADPH. We propose that (-)-cathinone is a biosynthetic precursor of (+)-cathine and (-)-norephedrine in khat leaves.