苦参黄酮类成分的研究

苦参(Sphora flavescens Ait)为豆科槐属植物,根入药,具有清热、燥湿、杀虫之功效。近年来国内外对苦参的研究较为重视。我们对苦参的化学成分进行了系统的研究,从苦参总黄酮中分离出8种黄酮类化合物:高丽槐素(maackiain,1)、4-甲氧基高丽槐素(4-methoxy-maackiain,2)、三叶豆紫檀甙(trifolirhizin,3)、降脱水淫羊藿素(nor-anhydroicaritin,4)、异苦参酮(isokurarinone,5)、槐属二氢黄酮 B(sopho-raflavanone B,6)、降苦参酮(nor-kurarinone,7)和芒柄花素(formoronetin,8)。化合物1、2和6是首次从苦参中得到的。本文报道苦参黄酮类化合物的研究。     

苦参酮的热稳定性及其提取工艺研究

考察了苦参酮的热稳定性,并用正交实验方法优选了苦参酮的提取工艺。结果发现,苦参酮在50℃下较稳定;以苦参酮的相对提取率为考察指标,在所考察的范围内,影响苦参酮相对提取率的主要因素依次为：提取时间〉乙醇浓度〉温度〉溶剂用量,其中提取时间和乙醇浓度对苦参酮的相对提取率影响显著;苦参酮的最佳提取工艺为：提取温度50℃,提取时间120min,容积用量（mL/g）25：1,乙醇浓度（v／v）：80％,相对提取率达到99．6％。优化后的提取工艺能较高效率地提取苦参酮。     

苦参化学成分研究概况

本文综述了苦参的药理、临床应用情况和苦参生物碱、黄酮等化学成分的结构特点及其结构测定方法.     

苦参和苦豆子的过氧化物酶同工酶谱分析和比较

采用聚丙烯酰胺凝胶电泳技术分析和比较了5个不同产地的苦参和1种苦豆子的过氧化物酶同工酶活性。结果表明：不同产地苦参品种和苦豆子的过氧化物酶同工酶谱迁移率在0.14～0.28之间,共6条酶谱带。聚类分析表明,苦参和苦豆子的亲缘关系较远,而不同产地的苦参种质也存在一定的差异,可分为3类：甘肃成县栽培的苦参与甘肃岷县栽培的苦参为一类,河南卢氏野生苦参单独为一类,河北承德野生苦参和甘肃成县野生苦参为一类。     

苦参的化学成分及药理的研究进展

介绍苦参（Sophora flavescens)近年来的研究进展,包括苦参中生物碱和黄酮的化学结构以及其抗寄生虫、抗病毒、抗菌、抗肿瘤、抗心律失常等多种生理活性。     

苦参水提液的杀菌效果

采用悬液定量杀菌试验,对苦参水提液的杀菌效果进行实验室研究。研究发现,苦参水提液对金黄色葡萄球菌、大肠埃希菌、枯草芽胞杆菌、白假丝酵母菌和黑曲霉均具有明显的杀菌作用。通过模拟现场试验,苦参水提液起到了显著地杀菌效果。     

气候变化条件下苦参在我国潜在分布区的预测分析

为了解气候变化情景下苦参在中国的潜在分布区变化,探讨生物气候因子与苦参适宜分布格局的关系.该文通过收集苦参的地理分布点并结合19项生态因子,运用最大熵模型(MaxEnt)和地理信息系统(ArcGIS)对末次盛冰期、当前气候、未来气候三种气候情景下苦参在我国适生区的分布格局进行模拟,并分析影响苦参生长的主导生态因子.结果...     

苦参活性成分的抗肿瘤作用机制研究进展

苦参是中国传统的植物药,具有清热燥湿等多种作用,广泛地应用于抗肿瘤研究,其活性成分能够通过细胞周期阻滞抑制肿瘤细胞的增殖、诱导肿瘤细胞分化、通过细胞周期阻滞、Fas/Fasl和线粒体途径诱导肿瘤细胞凋亡,通过降低VEGF等的表达抑制肿瘤血管生成和内皮细胞增殖,抑制肿瘤侵袭和转移,通过抑制端粒酶活性、逆转多药耐药、调节免疫耐受等辅助治疗肿瘤。通过收集、分析和整理最近几年涉及苦参活性成分抗肿瘤作用的文献,综述其抗肿瘤作用机制,为临床应用苦参治疗肿瘤提供参考。     

苦参提取液诱导K_(562)细胞分化的细胞化学观察

苦参是常用的中药,广泛应用于临床各科,特别是它的抗肿瘤作用正日益受到关注。本文用苦参提取液（１２ｇ／Ｌ）作诱导分化剂,以人红白血病细胞株Ｋ５６２作实验模型,培养三天,每天作细胞化学染色。用药后Ｗｒｉｇｈｔ＇ｓ＿Ｇｉｅｍｓａ染色,细胞形态有分化成熟的趋势。髓过氧化物酶染色（ＭＰＯ）阳性,糖原反应（ＰＡＳ）阳性,ａ－醋酸荼酚酯酶（α－ＮＡＥ）阴性。对照组上述染色均为阴性。结果表明苦参有促Ｋ５６２细胞向粒系和红系分化的现象,提示苦参可能对白血病的非杀伤性治疗有作用     

苦参中黄酮类化合物成分研究

本文对苦参EtOAc提取部分进行了分离,分得3个化合物,根据光谱数据分析鉴定为sophoraflavanone G(Ⅰ),忽布素(Ⅱ),β-谷甾醇(Ⅲ),其中化台物Ⅰ为首次自苦参中分离得到。     

苦参生物碱的研究

从苦参(Sophora flavescens Ait)根中分离得到9个生物碱,用波谱等方法确定为槐果碱(sophocarpine)、苦参碱(matrine)、异苦参碱(isomatrine)、槐醇(sophoranol)、N-甲基野靛碱(N-methylcytisine)、槐定(sophoridine)、氧化苦参碱(oxymatrine)、氧化槐果碱(oxysophocarpine)和氧化槐醇(sophoranol N-oxide)。其中氧化槐醇是首次从苦参根中得到的。     

3种苦参生物碱对小鼠的毒性作用研究

以小鼠为试验对象,对3种苦参生物碱(氧化苦参碱、槐定碱、苦参碱)的毒性作用进行了系统的分析.结果显示:(1)混合后的苦参生物碱毒性增加,其中苦参碱+槐定碱的增效作用最强,协同毒力指数(c.f)值达59.1,氧化苦参碱+苦参碱混合给药,c.f值为37.3,为增效作用;氧化苦参碱+槐定碱混合给药,c.f值为13.6,为相加作用.(2)血常规检测结果显示,3种苦参生物碱处理组小鼠的白细胞计数(WBC)、血小板总数(PLT)、中粒细胞(GR)较之对照组显著增高;血液生化指标检测结果显示,槐定碱和氧化苦参碱各处理组小鼠的尿素氮(BUN)、肌酐(Cr)水平均极显著高于对照组(P＜0.01),苦参碱各处理组小鼠的丙氨酸氨基转移酶(ALT)、天门冬氨酸氨基酸转移酶(AST)水平比对照组极显著升高(P＜0.01);脏器系数的统计结果显示:槐定碱、氧化苦参碱各处理组小鼠的肾脏系数、心脏系数以及肝脏系数均极显著高于对照组(P＜0.01),苦参碱处理组小鼠的肾脏系数、心脏系数及肺脏系数显著地高于对照组(P＜0.01、P＜0.05、P＜0.05).研究表明,3种苦参生物碱对小鼠肝脏、肾脏有影响,初步确定它们作用的靶器官是肝脏和肾脏.     

Cloning and Sequencing of a Lectin Protein Gene from the Roots of Sophora flavescens (in English)

A lectin protein（SFL） with molecular weight about 32 kD which markedly agglutinated rabbit and human red blood cells was purified from the roots of Sophora flavescens Ait. This protein, and apparently inhibited the growth of Fusarium vasinfectum Atk., Gibberella saubinetii (Mont.) Sacc., and Piricularia oryzae Cav. A set of degenerate PCR primer was synthesized according to the N-terminal sequence of the purified protein. The full-length cDNA coding the lectin was cloned by RT-PCR and 5′-RACE and sequenced (GenBank AF285121). The deduced amino acid sequence indicates that a preprotein with 284 amino acid residues is firstly translated and then processed to a mature protein with 254 amino acids. A N-Glycosylation site is the Asn 182 residue.      

Selective extraction and separation of oxymatrine from Sophora flavescens Ait. extract by silica-confined ionic liquid

This study highlighted the application of a two-stepped extraction method for extraction and separation of oxymatrine from Sophora flavescens Ait. extract by utilizing silica-confined ionic liquids as sorbent. The optimized silica-confined ionic liquid was firstly mixed with plant extract to adsorb oxymatrine. Simultaneously, some interference, such as matrine, was removed. The obtained suspension was then added to a cartridge for solid phase extraction. Through these two steps, target compound was adequately separated from interferences with 93.4% recovery. In comparison with traditional solid phase extraction, this method accelerates loading and reduces the use of organic solvents during washing. Moreover, the optimization of loading volume was simplified as optimization of solid/liquid ratio.     

Purification and Characterization of Sophora flavescens Lectin

A lectin with strong hemagglutination activity was isolated from roots of Sophora flavescens Ait. by extraction, fractionation with (NH 4) 2SO 4, ion-exchange chromatography on DEAE-Sepharose and followed by gel filtration on Sephadex G-150 and HPLC assay. The purified lectin showed a single protein band on PAGE and SDS-PAGE . The molecular weight of S. flavescens lectin was 32 kD when SDS-PAGE and Sephadex G-100 was used. The lectin agglutinated rabbit red blood cells at 0.97 μg/mL and showed no specific agglutination with any type of human erythrocytes. The hemagglutination activity could be inhibited by mannose and levulose and slightly by glucose and maltose. The SFL contained 2.89% neutral saccharide. It could inhibit apparently the growth of the mycelium of Gibberlla saubinetii （Mont.） Sacc.,Piricularia oryzae Cav. and Fusarium vasinfectum Atk. at the dosage of 62 μg. It was determined by Edman that the sequence of the N-terminal thirty amino acids was: T/A/VDXLXFTFSDFDPNGEDLLFQGDAHVTSNN.     

Synergistic action between jasmonic acid and nitric oxide in inducing matrine accumulation of Sophora flavescens suspension cells

Secondary metabolites not only play important ecological roles in plants but also are important pharmaceutical and source compounds for derivative synthesis. Production of plant secondary metabolites is believed to be controlled by the endogenous signal network of plants. However, the molecular basis is still largely unknown. Here we show that matrine production of Sophora flavescens Ait. cells treated with low levels of jasmonic acid （JA） and nitric oxide （NO） is significantly increased although treatment with low concentrations of JA or NO alone has no effects on matrine production, showing that JA and NO may act synergistically in triggering matrine production. Moreover, treatment with NO triggers lipoxygenase （LOX） activity and enhances JA levels of the cells, showing that NO may activate the endogenous JA biosynthesis of S. flavescens cells. External application of JA induces nitric oxide synthase-like activities and stimulates NO generation of S. flavescens cells, which suggests that JA may trigger NO generation of the cells. Thus, the results reveal a mutually amplifying reaction between JA and NO in S. flavescens cells. Furthermore, JA and NO inhibitors suppress not only the mutually amplifying reaction between JA and NO but also the synergistic effects of NO and JA on matrine production. Therefore, the data demonstrate that the synergistic action of JA and NO in inducing matrine production might be due to the mutually amplifying reaction between JA and NO in the cells.     

苦参碱的提取分离及对小鼠的毒性研究

采用酸性乙醇提取、乙醚萃取、硅胶柱层析分离等方法从苦参中分离到苦参碱单体.以小鼠为实验动物进行毒性测定,小鼠的死亡主要集中在48h内,48h后无小鼠的死亡现象.小鼠对苦参碱的耐受量大于30mg.k-g1,小于140mg.k-g1,致死中量LD50为64.01mg.kg-1,回归方程Y=-3.2370+4.5602X,LD50标准误差SE=6.14.适口性的测定表明,苦参碱对小鼠有较好的适口性,可以作为杀鼠剂使用.     

Impact of the herbal medicine Sophora flavescens on the oral pharmacokinetics of indinavir in rats: the involvement of CYP3A and P-glycoprotein

Sophora flavescens is a Chinese medicinal herb used for the treatment of gastrointestinal hemorrhage, skin diseases, pyretic stranguria and viral hepatitis. In this study the herb-drug interactions between S. flavescens and indinavir, a protease inhibitor for HIV treatment, were evaluated in rats. Concomitant oral administration of Sophora extract (0.158 g/kg or 0.63 g/kg, p.o.) and indinavir (40 mg/kg, p.o.) in rats twice a day for 7 days resulted in a dose-dependent decrease of plasma indinavir concentrations, with 55%-83% decrease in AUC(0-∞) and 38%-78% reduction in C(max). The CL (Clearance)/F (fraction of dose available in the systemic circulation) increased up to 7.4-fold in Sophora-treated rats. Oxymatrine treatment (45 mg/kg, p.o.) also decreased indinavir concentrations, while the ethyl acetate fraction of Sophora extract had no effect. Urinary indinavir (24-h) was reduced, while the fraction of indinavir in faeces was increased after Sophora treatment. Compared to the controls, multiple dosing of Sophora extract elevated both mRNA and protein levels of P-gp in the small intestine and liver. In addition, Sophora treatment increased intestinal and hepatic mRNA expression of CYP3A1, but had less effect on CYP3A2 expression. Although protein levels of CYP3A1 and CYP3A2 were not altered by Sophora treatment, hepatic CYP3A activity increased in the Sophora-treated rats. All available data demonstrated that Sophora flavescens reduced plasma indinavir concentration after multiple concomitant doses, possibly through hepatic CYP3A activity and induction of intestinal and hepatic P-gp. The animal study would be useful for predicting potential interactions between natural products and oral pharmaceutics and understanding the mechanisms prior to human studies. Results in the current study suggest that patients using indinavir might be cautioned in the use of S. flavescens extract or Sophora-derived products.