斑马鱼模型评价何首乌中18种成分的肝脏毒性

首次用斑马鱼模型探索何首乌中18种成分的肝脏毒性作用,为何首乌的肝毒性物质基础研究提供依据。对肝脏荧光转基因斑马鱼给以高、中、低剂量的18种何首乌主要成分72 h,并分别于给药后24、48、72 h用荧光显微镜对其进行拍照。拍好的图片通过Image J软件进行肝脏面积和荧光强度分析。大黄素组、大黄酸组、芦荟大黄素组、大黄素-1-O-葡萄糖苷组、大黄素甲醚-8-O-葡萄糖苷组、芦荟大黄素-8-O-葡萄糖苷组及阳性对照组(对乙酰氨基酚)的肝脏面积和肝脏荧光强度与空白组相比显著降低;而大黄酚组、大黄素甲醚组、大黄素-8-O-葡萄糖苷组、大黄酸-8-O-葡萄糖苷组、大黄酚-1-O-葡萄糖苷组、大黄酚-8-O-葡萄糖苷组、芦荟大黄素-3-羟甲基葡萄糖苷组、白藜芦醇组、没食子酸组、儿茶素组、表儿茶素组的肝脏面积和肝脏荧光强度与空白组相比无显著差异;此外,二苯乙烯苷组的肝脏荧光强度与空白组相比显著增高。由此可见大黄素、大黄酸、芦荟大黄素、大黄素-1-O-葡萄糖苷、大黄素甲醚-8-O-葡萄糖苷、芦荟大黄素-8-O-葡萄糖苷对斑马鱼幼鱼肝脏具有一定毒性作用。何首乌的肝毒性作用可能还是由蒽醌类化合物介导,其物质基础与上述6种蒽醌成分有关,并以结合蒽醌为主。     

化学修饰L02肝细胞膜生物亲和材料快速筛选大黄降血脂活性成分CSCD

为增加细胞膜生物亲和材料使用寿命,建立以APTES修饰硅胶为载体的L02细胞膜生物亲和材料,并将其应用于大黄降血脂活性成分的快速筛选。采用油酸刺激L02肝细胞,建立肝脂肪变性模型;硅胶与APTES、戊二醛发生反应,在硅胶表面引入醛基,游离醛基与细胞膜上富含的氨基通过共价键连接;扫描电镜和红外光谱进行表征;对大黄30%乙醇提取液进行吸附,HPLC分析吸附结果。通过扫描电镜证实材料表面覆盖有一层细胞膜,红外光谱也出现3442、2942 cm^(-1)的-NH键特征吸收峰,表明材料制备成功;HPLC分析表明:11种化学成分被特异性吸附,分别为:芦荟大黄素-8-O-β-D-葡萄糖苷、大黄酸-8-O-β-D-葡萄糖苷、大黄酚-8-O-β-D-葡萄糖苷、大黄素甲醚-8-O-β-D-葡萄糖苷、芦荟大黄素、大黄酸、大黄素、大黄酚、大黄素甲醚及2种未知成分。制备的化学修饰L02肝细胞膜生物亲和材料能够延长使用次数,也可用于大黄及其他中药降血脂活性成分的快速筛选。     

粗柄独尾草不同器官蒽醌类成分的消长规律

采用高效液相色谱法对沙生类短命植物粗柄独尾草苗期、营养生长期、初花期、盛花期、果期各器官中大黄素、大黄酚、大黄酸、芦荟大黄素含量的消长规律进行了研究。结果表明:叶中,芦荟大黄素的含量在苗期和初花期都较高,在盛花期时最低;大黄酸的含量在苗期最高,盛花期时最低;大黄素的含量在苗期达到最高,初花期和盛花期最低;大黄酚的含量也以苗期最高,盛花期和果期最低。且在初花期时,4种蒽醌类物质含量均呈现明显的叶先端>叶中部>叶基部的空间差异性。根中,芦荟大黄素的含量在苗期和营养生长期较高,而以盛花期和果期较低;大黄酸的含量在果期最高,其余时期差异不显著;大黄素的含量以苗期和初花期较高;大黄酚的含量在果期达最高,而盛花期时最低。同时期的根叶蒽醌含量相比,叶中的芦荟大黄素要高于根,而根中大黄酚含量要高于叶。同时期各器官蒽醌总量相比:叶>根>花>花葶。故若选取粗柄独尾草作为蒽醌类药材利用,建议最佳采集方式为采集初花期的叶先端部分。     

连花清瘟胶囊原料药的化学成分研究北大核心CSCD

采用硅胶柱层析、Sephadex LH-20凝胶、制备液相等方法从连花清瘟胶囊原料药中分离得到17个化合物。通过IR、MS、1H NMR、13C NMR等波谱手段鉴定为(+)-松脂素(1)、连翘苷(2)、表松脂素-4'-O-β-D-葡萄糖苷(3)、罗汉松脂素-4'-O-β-D-葡萄糖苷(4)、大黄酚-1-O-β-D-葡萄糖苷(5)、芦荟大黄素-8-O-β-D-葡萄糖苷(6)、大黄酚(7)、大黄素(8)、大黄素甲醚(9)、芦荟大黄素(10)、芦荟大黄素乙酸酯(11)、槲皮素-3-O-α-L-鼠李糖苷(12)、山柰酚-3-O-α-L-鼠李糖苷(13)、五福花苷酸(14)、没食子酸(15)、苯甲酸(16)和β-谷甾醇(17)。本研究首次通过系统化学分离、鉴定手段从连花清瘟胶囊原料药中分离、鉴定17个化合物,为阐明连花清瘟胶囊的化学物质基础提供了重要的科学研究数据。     

连花清瘟胶囊原料药的化学成分研究

采用硅胶柱层析、Sephadex LH-20凝胶、制备液相等方法从连花清瘟胶囊原料药中分离得到17个化合物。通过IR、MS、1H NMR、13C NMR等波谱手段鉴定为(+)-松脂素(1)、连翘苷(2)、表松脂素-4'-O-β-D-葡萄糖苷(3)、罗汉松脂素-4'-O-β-D-葡萄糖苷(4)、大黄酚-1-O-β-D-葡萄糖苷(5)、芦荟大黄素-8-O-β-D-葡萄糖苷(6)、大黄酚(7)、大黄素(8)、大黄素甲醚(9)、芦荟大黄素(10)、芦荟大黄素乙酸酯(11)、槲皮素-3-O-α-L-鼠李糖苷(12)、山柰酚-3-O-α-L-鼠李糖苷(13)、五福花苷酸(14)、没食子酸(15)、苯甲酸(16)和β-谷甾醇(17)。本研究首次通过系统化学分离、鉴定手段从连花清瘟胶囊原料药中分离、鉴定17个化合物,为阐明连花清瘟胶囊的化学物质基础提供了重要的科学研究数据。     

毛脉酸模不同器官中几种生物活性物质的含量及生长季节对其的影响

为确定毛脉酸模(Rumex gmelini)最佳药用部位和最佳采收期,从而为新药源开发提供科学依据,我们采用HPLC法和梯度洗脱,研究了一年生和二年生毛脉酸模不同生长发育期、不同器官、组织中7种生物活性成分(白藜芦醇、白藜芦醇苷、大黄酚苷、酸模素、大黄素、大黄酚和大黄素甲醚)的动态分布规律.结果表明毛脉酸模根部含有生物活性成分的种类及含量均多于其他部位,为最佳药用部位.一年生毛脉酸模根部不含有酸模素.二年生毛脉酸模根部含有全部7种生物活性成分,且在8～9月份含量最高,为最佳采收期.     

毛脉酸模不同器官中几种生物活性物质的含量及生长季节对其的影响

为确定毛脉酸模(Rumex gmelini)最佳药用部位和最佳采收期, 从而为新药源开发提供科学依据, 我们采用HPLC法和梯度洗脱, 研究了一年生和二年生毛脉酸模不同生长发育期、不同器官、组织中7种生物活性成分(白藜芦醇、白藜芦醇苷、大黄酚苷、酸模素、大黄素、大黄酚和大黄素甲醚)的动态分布规律。结果表明毛脉酸模根部含有生物活性成分的种类及含量均多于其他部位, 为最佳药用部 位。一年生毛脉酸模根部不含有酸模素。二年生毛脉酸模根部含有全部7种生物活性成分, 且在8~9月份含量最高, 为最佳采收期。     

天山雪莲不同器官中黄酮、总酚含量和抗氧化活性分析

研究了天山雪莲不同部位的总黄酮、总酚含量及抗氧化活性。以天山雪莲根、茎、叶、花、花苞片为材料,测定其80%乙醇提取物的总黄酮含量、总酚含量、Fe3+还原力和对DPPH自由基的清除率。结果表明,天山雪莲中总黄酮和总酚的含量高低依次为叶花苞片≈花根茎;对Fe3+还原能力大小次序是叶花苞片花根茎;对DPPH的清除能力依次为叶≈花苞片花根茎。实验结果表明叶片可以作为天山雪莲采摘和药用的主要部位;天山雪莲花苞片中可能含有黄酮和酚类之外的抗氧化物质。     

大黄属3种大黄植物不同部分蒽醌含量的测定与比较

采用C18反相柱高效液相色谱方法分离、外标法定量对大黄属掌叶组唐古特大黄、波叶组波叶大黄、穗序组穗序大黄的根（及根茎）、叶片、叶柄、主茎四部分的芦荟大黄素、大黄酸、大黄素、大黄酚4种游离和结合蒽醌的含量进行了测定和比较。结果表明：唐古特大黄中,叶片中的游离蒽醌含量高于其它部分,游离蒽醌总量地上部分远高于地下部分;结合蒽醌则根中最高,蒽醌总量地下部分远高于地上部分。波叶大黄和穗序大黄中,游离和结合蒽醌均为根中最高,穗序大黄蒽醌总量地下部分远高于地上部分,而波叶大黄中,游离蒽醌总量地上部分高于地下部分,结合蒽醌总量地上部分与地下部分相差不大,地上部分略高于地下部分。     

毛脉酸模内生真菌蒽醌类次生代谢产物的筛选及含量分析

本文通过对毛脉酸模内生真菌的发酵培养得到其次生代谢产物,采用HPLC法对内生真菌中蒽醌类成分进行筛选。以大黄素、大黄酸、大黄酚、大黄素甲醚、芦荟大黄素五种蒽醌类成分为参照,筛选出3株真菌含大黄素、3株真菌含大黄酸、5株真菌含芦荟大黄素,其中含量最高为683μg/g、最低为8μg/g。将各菌株所含成分与各菌株分离部位的相应成分进行比较,相对宿主植物而言各菌株均有较高的含量。本实验分析方法准确、快捷,适用于毛脉酸模内生真菌的代谢产物研究。     

Emodin with PPARgamma ligand-binding activity promotes adipocyte differentiation and increases glucose uptake in 3T3-Ll cells

Emodin, one of the main active components in the root and rhizome of Rheum palmatum L, promoted the conversion of 3T3-L1 fibroblasts to adipocytes, as evidenced by increased glycerol-3-phosphate dehydrogenase (GPDH) activity and the expression of adipocyte aP2 mRNA, as well as accelerated triacylglycerol (TG) accumulation, which was associated with increased mRNA expression levels of both C/EBPalpha and PPARgamma2. By using surface plasmon resonance (SPR) experiment, it was showed that emodin exhibited a very high binding affinity to PPARgamma. In differentiated 3T3-L1 adipocytes, emodin induced a time- and dose-dependent increase in glucose uptake as well as GLUT1 and GLUT4 mRNA expression, and the rate of uptake was partly abrogated by wortmannin (phosphoinositide 3-kinase inhibitor). Meanwhile, insulin-stimulated glucose uptake was increased significantly after treatment with low doses of emodin, and the degree of potentiation was decreased thereafter in response to increasing concentrations. Furthermore, 50 microM emodin profoundly inhibited insulin-stimulated glucose uptake by 25%. These data suggest a new role for emodin as a PPARgamma agonist in 3T3-L1 cells. Besides, it is possible that emodin may also possess other properties contribute to glucose utilization in the adipocytes.     

Soluble Protein Content,Bioactive Compounds and the Antioxidant Activity in Seeds of Ten Rheum tanguticum Lines from Qinghai-Tibet Plateau

Rheum tanguticum (Rh. tanguticum) is a Chinese medicinal plant traditionally used in the treatment of constipation. As a byproduct, the seeds of this plant are rich in nutrients and phytochemicals. This study aimed to determine and assess seed germination ability, seed physical characteristics, soluble protein content, chemical constituents and antioxidant capacity from different breeding lines, to promote the development and utilization of seed resources. Significant differences were observed for the soluble protein content and antioxidant assays among the ten lines. The contents of aloe-emodin, rhein and catechins accumulated in seeds were extremely low and significantly different from those in roots. In contrast, emodin and chrysophanol were abundant in seeds, and significant differences were observed between seeds and roots. It was found that associations between gallic acid and catechins were not significant for either soluble protein or antioxidant capacity. There was a significantly positive correlation between the contents of four anthraquinones (aloe-emodin, rhein, emodin and chrysophanol) and soluble protein. Seeds have potent antioxidative capacity and relatively high levels of soluble protein content. The rich chemical composition of seeds can be widely used in the medical industry for further development.     

神农箭竹开花前后植物体内N、P、K元素的动态

对神农箭竹(Fargesia murielae)N、P、K的含量进行分析,结果表明:N、P、K在竹子植物体内呈非均匀分布。N和P在各器官中的分布规律为:叶>鞭、根>竿;K在未开花竹和正开花竹中分布规律为:鞭>根>叶>竿,在已开花竹中分布规律为:叶>鞭>竿>根。随着开花过程的进行,N的含量在叶、竿、鞭和根等器官中逐渐减少;P的含量在竿、鞭和根等器官中逐渐降低,在叶片中先升高后降低;K的含量在鞭和根中呈下降趋势,在竿和叶中先降低后升高。     

复方五倍子有效成分的分离鉴定及抑菌活性研究

对渔用抗菌剂复方五倍子有效成分进行薄层色谱与柱层析分离检测,以鉴定出复方中的各种有效成分;选用几种水产动物常见致病菌进行体外抑菌和联合用药试验,以确定各有效成分抑菌活性强弱和各成分间的药物关系,为分析复方五倍子抗菌剂的药物作用机理奠定理论基础,并为其质量控制提供参考依据。用薄层析硅胶GF254制板,以苯:乙醇:甲酸(7:3:1)为展开剂,用氨熏-三氯化铁显色,日光下观察层析结果;通过干法装硅柱,以苯:乙醇:甲酸(7:3:1)作为洗脱液进行洗脱,分离得到各单体,参照理化性质分析及薄层分析,鉴定出复方五倍子抗菌剂总有效成分。结果表明;复方五倍子抗菌剂有效成分为鞣质、没食子酸、槲皮素、黄芩苷、芦荟大黄素、大黄素和1,8-二羟基蒽醌,其中没食子酸含量最大,紫外分光光度法测定为10.47%。用复方的各有效成分别对温和气单胞菌、豚鼠气单胞菌、迟缓爱德华菌和柱状黄杆菌进行抑菌试验,以温和气单胞菌为菌种将复方主要有效成分两两配对进行体外联合抑菌试验,得出复方五倍子各有效成分抑菌活性顺序为:没食子酸>蒽醌(含1,8-二羟基蒽醌、大黄素、芦荟大黄素)>黄芩苷>槲皮素>鞣质。没食子酸和蒽醌具有协同作用,没食子酸和黄芩苷、没食子酸和槲皮素、蒽醌和黄芩苷三组同属于累加作用。       

Identification and quantification of galloyl derivatives,flavonoid glycosides and anthocyanins in leaves of Pistacia lentiscus L

Separation, identification and quantification of polyphenols was carried out on leaves of Pistacia lentiscus L., an evergreen member of the family Anacardiaceae, using semi-preparative HPLC, HPLC-photodiode array detection and HPLC-MS analysis, together with 1H- and 13C NMR. Three major classes of secondary metabolites were detected: (i) gallic acid and galloyl derivatives of both glucose and quinic acid; (ii) flavonol glycosides, i.e. myricetin and quercetin glycosides; and (iii) anthocyanins, namely delphinidin 3-O-glucoside and cyanidin 3-O-glucoside. Low amounts of catechin were also detected. The concentration of galloyl derivatives was extremely high, representing 5.3% of the leaf dry weight, and appreciable amounts of myricetin derivatives were also detected (1.5% on a dry weight basis). These findings may be useful in establishing a relationship between the chemical composition of the leaf extract and the previously reported biological activity of P. lentiscus, and may also assign a new potential role of P. lentiscus tissue extracts in human health care.     

六种彩叶植物营养成分及有害元素含量分析

以六种彩叶植物紫叶李、红花木、红叶石楠、红枫、鸡爪槭和金叶女贞的叶片为材料,对其营养成分及有害元素含量进行了测定及分析。结果表明:蛋白质和可溶性糖含量以红花木为最高,维生素C含量以红枫为最高,β-胡萝卜素含量差异最大,紫叶李最高达15.99mg·kg-1。六种彩叶植物矿质营养元素种类齐全,其中红花木的营养元素总量最高。六种彩叶植物均含有18种氨基酸成分,必需氨基酸和总氨基酸含量各不相同,但必需氨基酸占总氨基酸的比例却较为一致,且都高于40%。六种彩叶植物叶片内均含有一定量的铅、镉、砷、汞等有害元素,但有害元素尤其是砷和汞的含量均低于允许量。     

Cellular absorption of anthraquinones emodin and chrysophanol in human intestinal Caco-2 cells

The intestinal absorption characteristics of anthraquinones emodin and chrysophanol were observed by measuring the intracellular accumulation across Caco-2 cells by the reverse-phase high performance liquid chromatography. The intracellular accumulation of chrysophanol was much greater than that of emodin, the maximum absorption of emodin and chrysophanol being 414.02+/-15.28 and 105.56+/-11.57 nmol/l x mg x protein, respectively. The absorption of each anthraquinone was significantly lower at 4 degrees C than that of 37 degrees C. The effects of the transport inhibitors, verapamil, cyclosporine and phloridzin, on the intracellular accumulation were also examined. Verapamil and cyclosporine increased the absorption of emodin and chrysophanol, while phloridzin inhibited their absorption, all in a dose-dependent manner. These results suggest that the absorption characteristics of emodin and chrysophanol were closely related to their special structure with the hydroxy groups. It is also likely that a specific transport system mediated the intracellular accumulation of emodin and chrysophanol across the Caco-2 cells.     

Involvement of Matrix Metalloproteinases on the Inhibition of Cells Invasion and Migration by Emodin in Human Neuroblastoma SH-SY5Y Cells

Emodin (1,3,8-trihydroxy-6-methylanthaquinone), an active component present in the root and rhizome of Rheum palmatum L. (Polygonaceae) has anti-bacterial, anti-tumor, diuretic and vasorelaxant effects. However, its mechanism of action on the cell migration and invasion of human neuroblastoma cancer SH-SY5Y cells is not fully understood. In this study, firstly, the effects of emodin on the percentage of viable cells were examined by using MTT assay and it was found that emodin induced dose-and time-dependent inhibition in human neuroblastoma SH-SY5Y cells. Second, the effects of emodin on the migration and invasion of SH-SY5Y cells were examined by using wound assay and matrigel counting and the results showed that emodin suppressed the migration and invasion of SH-SY5Y cells. Third, we examined the effect of emodin on the levels of associated proteins by using Western blotting and the results indicated that emodin inhibited the levels of GRB2, RhoA, HIF-1α, VEGF, FAK, iNOS, COX2, p-p38, p-c-jun, MMP2, MMP9 and MMP7 but promoted the levels of PKC, PI3K, MEKK3 and NF-κB p65 that led to the inhibition of migration and invasion of SH-SY5Y cells in vitro.