苦参生物碱杀虫生物活性测定

以桃蚜等9种试虫为供试靶标，研究了苦参根提取物和苦参碱、氧化苦参碱、槐果碱、野靛碱的杀虫活性。试验结果表明：苦参生物碱具有一定的杀虫活性，9种试虫中，苦参根提取物对蚜虫的活性最高，其对蚕豆蚜的LC50为20．635mg／L；即使在最高剂量为4000mg/L时，也不能直接杀死粘虫、小菜蛾和棉铃虫。4种生物碱对朱砂叶螨活性均较低，LC50均大于2500mg／L。野靛碱是4种生物碱中杀虫活性最高的，对淡色库蚊、桃蚜、蚕豆蚜、褐飞虱和家蝇的LC50分别为172．431mg/L、207．667mg／L、85．212mg／L、266．179mg／L和763．224mg／L；而且对褐飞虱、桃蚜和家蝇的活性高于苦参根提取物，苦参碱对蚜虫的活性高于氧化苦参碱和槐果碱，槐果碱对淡色库蚊、褐飞虱和家蝇的活性高于苦参碱和氧化苦参碱。     

苦参愈伤组织诱导及继代培养条件研究

目的：研究苦参愈伤组织诱导与继代培养,为药用成分苦参碱及氧化苦参碱的来源提供新途径.方法：考察了不同外植体和激素组合对苦参愈伤组织诱导的影响和苦参愈伤组织增殖继代的最佳培养条件.结果：分别以幼芽、根、茎段、叶片为外植体,在MS＋1.0mg/L 2,4-D＋1.0mg/L 6-BA＋1.0mg/L NAA激素组合下苦参愈伤组织的诱导率分别为94.12%、74.19%、35.71%、23.08%;在MS＋0.5mg/L 2,4-D＋0.1mg/L 6-BA＋0.5mg/L NAA激素组合下,苦参愈伤组织增殖率最高,为25.3%.结论：幼芽为苦参愈伤组织诱导最佳外植体.不同激素组合对愈伤组织诱导率的影响不大,但对其增殖的影响较大,其中NAA具有显著影响.     

Development of an osmotically-driven pellet coated with acrylic copolymers (Eudragit® RS 30 D) for the sustained release of oxymatrine,a freely water soluble drug used to treat stress ulcers (I): in vitro and in vivo evaluation in rabbits

Purpose: To develop an osmotically-driven pellet coated with polymeric film for sustained release of oxymatrine (OMT), a freely water soluble drug.

Methods: Pellet containing OMT and sodium chloride (NaCl), an osmotically active agent, were prepared by extrusion/spheronization and then coated with acrylic copolymers (Eudragit^® RS 30 D) by the fluidized bed coating process. In vitro release and swelling behavior studies were employed to optimize and to evaluate the sustained-release behavior from the osmotically-driven pellets with film coated. Finally, in vivo evaluation in rabbits was employed to investigate the sustained plasma level of OMT and its active metabolite matrine.

Results: It was found that the F3 formulation, prepared with 20% NaCl and an 8% coating level, showed a continuous NaCl-induced water influx into the pellets providing a gradual sustained release of OMT for over 12?h. Finally, we confirmed that oral OMT with sustained release led to a gradual sustained plasma profile of both OMT, with a reduction in its bioavailability, and MT with an increase in the bioavailability compared with that of oral OMT with immediate release. Conclusions: The pharmaceutical parameters obtained suggested the potential usefulness of oral OMT with sustained release for the treatment of stress ulcers, as well as reducing the risk of MT-induced side effects.     

Matrine Exerts a Strong Anti-Arthritic Effect on Type II Collagen-Induced Arthritis in Rats by Inhibiting Inflammatory Responses

To investigate anti-arthritic effects of matrine isolated from the roots of S. flavescens on type II collagen-induced arthritis (CIA) in rats and to explore its related potential mechanisms, CIA rats were established and administered with matrine (20, 40 or 80 mg/kg/days, for 30 days). Subsequently, blood was collected to determine serum levels of TNF-α, IL-1β, IL-6, IL-8, IL-17A, IL-10, MMP-2, MMP-3 and MMP-9, and hind paws and knee joints were collected for histopathological examination. Furthermore, indices of the thymus and spleen were determined, and synovial tissues were collected to determine the protein expressions of p-IκB, IκB, Cox-2 and iNOS. Our results indicated that matrine significantly suppressed inflammatory reactions and synovial tissue destruction. Matrine inhibited paw swelling, arthritis indices and weight loss in CIA rats. Additionally, matrine decreased the levels of TNF-α, IL-1β, IL-6, IL-8, IL-17A, MMP-2, MMP-3 and MMP-9. Matrine also down-regulated expressions of p-IκB, Cox-2, and iNOS but up-regulated IκB in synovial tissues in CIA rats. The results suggested matrine possesses an anti-arthritic effect in CIA rats via inhibiting the release of pro-inflammatory cytokines and proteins that promote the NF-κB pathway.     

苦参碱脂质体的研究

对苦参碱脂质体的制备工艺进行了研究，并测定了包封率、渗漏率等脂质体的质量指标。以包封率为指标，优选了苦参碱脂质体的最佳制备工艺条件，结果表明：逆相蒸发法制备的脂质体包封率可达50、08％。抗肿瘤实验进行了3个剂量组对小鼠S180的抗瘤效应，结果显示，苦参碱脂质体中剂量组对小鼠S180抗瘤效应最好，对小鼠EAC亦有明显的抗肿瘤作用。     

Synthesis of a Temperature-Sensitive Matrine-Imprinted Polymer and Its Potential Application for the Selective Extraction of Matrine from Radix Sophorae Tonkinensis

A temperature-sensitive matrine-imprinted polymer was prepared in chloroform by free-radical cross-linking copolymerization of methacrylic acid at 60 °C in the presence of ethylene glycol dimethacrylate as the cross-linker, N-isopropyl acrylamide as the temperature-responsive monomer and matrine as the template molecule. Binding experiments and Scatchard analyses revealed that two classes of binding sites were formed on molecular imprinted polymer (MIP) at 50 °C. Additionally, the thermoresponsive MIP was tested for its application as a sorbent material for the selective separation of matrine from Chinese medicinal plant radix Sophorae tonkinensis. It was shown that the thermoresponsive MIP displayed different efficiency in clean-up and enrichments using the SPE protocol at different temperatures.     

高效毛细管电泳法测定四味土木香散中苦参碱和氧化苦参碱的含量

提出了同时测定四味土木香散中苦参碱和氧化苦参碱含量的方法。采用高效毛细管电泳法。实验条件为:用缓冲溶液20mmol/LTris-40mmol/LNaH2PO4-20%异丙醇(用磷酸调到pH5.5)作为电泳液,检测波长为200nm。被测样品中苦参碱和氧化苦参碱完全分离且被准确测定。其平均加样回收率分别为99.2%和100.1%,RSD分别为2.31%和1.57%(n=9)。该方法操作简便、准确,可作为四味土木香散及其制剂的质量控制方法。     

超声波辅助提取山豆根苦参碱研究

首次报道山豆根苦参碱的超声波辅助提取方法。采用单因子试验和L9(34)正交试验设计,研究了超声波功率、超声波时间、超声波温度、乙醇浓度、液料比、浸置时间、提取液pH和提取次数对山豆根苦参碱提取的影响。结果表明,影响苦参碱得率的主次因素为超声波时间、超声波温度、超声波功率及浸置时间;经正交试验确定山豆根苦参碱最佳提取工艺条件为料液比为50、超声波时间为120min、超声波温度为70℃、超声波功率为300W、浸置时间为30min、乙醇浓度为60%、提取液pH为13、提取1次,在此最佳工艺条件下,山豆根苦参碱的得率为0.562%。     

苦参碱对大麦种子萌发及幼苗生长的影响

采用室内培养皿法,以清水和油菜素内酯作对比,分析不同浓度的苦参碱制剂浸种大麦种子对大麦的种子发芽率、苗高、根长等形态指标,以及叶绿素和可溶性糖含量等的影响。结果表明,苦参碱对大麦种子萌发及幼苗生长有促进作用,且随着苦参碱质量浓度的增大,大麦的种子发芽率、苗高、根长、叶绿素和可溶性糖含量呈先升高后降低的趋势,以100 mg/L处理各指标最好。此外,100 mg/L苦参碱浸种处理对大麦幼苗各项指标的影响与25 mg/L油菜素内酯相似或比25 mg/L油菜素内酯好。     

基于QbD理念优化苦参甘草中有效成分的提取工艺

遵循"质量源于设计（quality by design,QbD）"理念,建立苦参甘草中有效成分的回流醇提工艺的设计空间并验证。以苦参总碱（total alkaloids of Sophora flavescens,TASF）、苦参碱（matrine,MT）及氧化苦参碱（oxymatrine,OMT）的提取率为关键质量属性（critical quality attributes,CQAs）,通过单因素实验确定Plackeet-Burmann设计（Plackeet-Burmann design,PBD）中各因素的高低水平,后采用PBD实验确定乙醇体积分数、甘草用量和提取温度为关键工艺参数（critical process parameters,CPPs）,再通过中心点复合实验设计优化CPPs,基于二次多项式建立CPPs和CQAs间的数学模型,计算获得设计空间。验证结果表明,在设计空间内操作能够保证苦参有效成分提取工艺品质稳定。最终获得的操作空间为：甘草用量10.00~10.50g,乙醇体积分数65%~68%,提取温度94.5~95.0℃。