An LC-MS/MS Method for Determination of Imperatorin and Isoimperatorin in Rat Plasma and Application to a Pharmacokinetic Study

A highly sensitive liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed for the de-termination of imperatorin and isoimperatorin in rat plasma using psoralen as internal standard. Analyses were performed on a Shimadzu HPLC system using a Shimadzu C18 column eluted with a mobile phase of methanol-water (25:75), containing 0.1% formic acid at a flow rate of 0.4 ml/min. The detection was performed by positive ion elec-trospray ionization in multiple reactions monitoring mode, monitoring the transitions m/z 203→147 and m/z 203→159 for imperatorin and isoimperatorin, respectively. The method was validated over the concentration range of 2.5 -1000.0 ng/mL for imperatorin and isoimperatorin. The limits of detection and quantification were 1.0 and 3.0 ng/mL, repectively for both analytes. The intra-day and inter-day accuracy and precision of the assay were less than 10.9%. This method has been applied successfully to a pharmacokinetic study involving the intragastric administration of extract of Angelicae Dahuricae Radix to rats.

Protective effects of imperatorin against cerebral ischemia/reperfusion-induced oxidative stress through Nrf2 signaling pathway in rats

OBJECTIVE To investigates the effects of imperatorin on the oxidative stress in the cerebral cortex and hippocampus after focal cerebral ischemia/reperfusion injury.METHODS Transient focal cerebral ischemia/reperfusion model in male Sprague-Dawley rats was induced by 2 h middle cerebral artery occlusion followed by 24 h reperfusion.Imperatorin(1.25 and 2.5 mg·kg-1)or vehicle were administered intraperitoneally at 1,5 and 9 h after the onset of ischemia.At 24 h after reperfusion,the biomarkers of oxidative stress such as the levels of reactive oxygen species(ROS),lipid peroxidation products malondialdehyde(MDA),nitric oxide(NO)and total antioxidant capacity(T-AOC),the activities of inducible nitric oxide synthase(iN OS),superoxide dismutase(SOD)and catalase(CAT)in the cerebral cortex and hippocampus were observed.We also assessed the nuclear factor erythroid 2-related factor 2(Nrf2),heme oxygenase-1(HO-1),and the NAD(P)H-quinone oxidoreductase 1(NQO-1)protein expression by Western blot.RESULTS As compared to vehicle-treated animals,imperatorin treatment significantly reduced the ROS,MDA,NO levels and i NOS activity,increased T-AOC and the activities of SOD and CAT.Furthermore,imperatorin treatment also significantly induced the nuclear translocation of Nrf2,enhanced the protein expression of HO-1 and NQO-1 in the cerebral cortex and hippocampus.CONCLUSION Our findings indicate that imperatorin can protect the brain against the excessive oxidative stress induced by cerebral ischemia/reperfusion through activation of Nrf2 signaling pathway.

Identification of Herbal Compound Imperatorin with Adverse Effects on ANO1 and CFTR Chloride Channels

Calcium-activated chloride channels（CaCCs） are the crucial regulators of transepithelial fluid secretion, smooth muscle contraction and sensory transduction. Recently, compelling evidence has indicated that TMEM16A（ANO1 or anoctamin-1） is a bona fide calcium-acvtivated chloride channel. A few small molecule CaCCs regulators are available for functional and therapeutic studies. We screened 126 natural compounds from Chinese herbs. Screening was performed with an iodide influx assay in Fischer rat thyroid epithelial cells to coexpress ANO1 and an iodide-sensitive fluorescent indicator（EYFP-H148Q/I152L）. Imperatorin, a coumarin compound, was identified to inhibit ANO1-mediated chloride transport activated by multiple calcium-elevating agonists. The inhibitory effect is dose-dependent with IC50～14.63 μmol/L. Interestingly, imperatorin activated CFTR chloride channel with EC50～35.52 μmol/L. The adverse effects of imperatorin on CaCC and CFTR chloride channels will make it useful in pharmacological dissection of chloride transport in airway and intestinal epithelium. Further studies are required to evaluate the therapeutic effects of imperatorin on hypertension, asthma and certain tumors.

Mechanisms of imperatorin on regulating Pglycoprotein in blood-brain barrier based on network pharmacology and in vitro experiment

OBJECTIVE To explore mecha⁃nisms of imperatorin on regulating P-glycoprotein(P-gp)in blood-brain barrier(BBB)based on net⁃work pharmacology combined with in vitro experi⁃ment.METHODS Drug targets were predicted using the Pharmapper and Swiss targets data⁃bases;disease targets were obtained through the Genecards database;intersections between drugs and disease targets were screened by Cytoscape software;the obtained core targets were used to construct protein-protein interaction(PPI)network,gene ontology(GO)functions,and Kyoto encyclopedia of genes and genomes(KEGG)pathway enrichment analysis.The effects of imperatorin(20,50,100μmol·L^(-1))on P-gp activity were monitored in hCMEC/D3 in vitro BBB model,and the effects of imperatorin on the expression of target proteins were verified using Western blot method.RESULTS 55 drug targets and 3102 disease targets were obtained from the network pharmacology screening,and 37 core targets were obtained after the combination.Enrichment analysis showed that core targets were closely related to chemical synaptic trans⁃mission regulation,neurotransmitter receptor activity,protein kinase regulation activity,G proteincoupled receptor signaling pathway,neural active ligand receptor interaction pathway,PI3K-Akt sig⁃naling pathway,VEGF signaling pathway,etc..In vitro experimental validation suggested that all tested concentration groups of imperatorin signifi⁃cantly reduced the activity and expression of P-gp,which were achieved by significantly downregu⁃lating the phosphorylation levels of PI3K and Akt,and repressing the expression of VEGFR2 pro⁃tein.CONCLUSION Network pharmacology was used to predict the core targets and signaling pathways of imperatorin on regulating P-gp in BBB and relevant validation was conducted through in vitro experiments,providing a refer⁃ence basis for further exploration of the mecha⁃nisms of imperatorin on regulating P-gp in BBB.

Imperatorin alleviates Aβ-induced spatial learning memory impairment and neuroinflam⁃mation in model mice of Alzheimer disease

OBJECTIVE To investigate the effects of imperatorin on the spatial learning memory impairment and neuroinflammation in model mice of Alzheimer disease(AD)induced by intracerebroventricular injection of Aβ1-42.METHODS Mouse model of AD was established by injection of Aβ1-42 into the lateral ventricles.Im⁃peratorin(2.5 and 5.0 mg·kg-1,daily)was inject⁃ed by intraperitoneally 1 h after intracerebroven⁃tricular injection for 13 d.The effect of imperato⁃rin on the spatial learning and memory impair⁃ment was assessed by eight arm maze tests.The levels of cytokines TNF-α,IL-1β,IL-6,IL-18 and chemokines MCP-1 in mouse cortex and hip⁃pocampus were detected by ELISA.The protein expression of NF-κB P65,TLR4,MyD88,p-P38,p-ERK,and p-JNK were detected by Western blotting.RESULTS As compared with the AD model group,imperatorin treatment significantly attenuated Aβ1-42-induced spatial learning and memory impairment assessed by eight arm maze tests.In addition,imperatorin significantly reduced the levels of cytokines TNF-α,IL-1β,IL-6,IL-18 and chemokines MCP-1 in the cerebral cortex and hippocampus.Meanwhile,Western blotting results showed that imperatorin treat⁃ment significantly down-regulated the protein expression of NF-κB P65,TLR4,MyD88,p-P38,p-ERK,and p-JNK.CONCLUSION Imperatorin has neuroprotective effects in the Aβ1-42 induced AD model mice and its mechanism may be partially associated with the inhibition of inflam⁃matory response in the cortex and hippocampus.

Estrogenic activity of osthole and imperatorin in MCF-7 cells and their osteoblastic effects in Saos-2 cells

There is an increasing interest in phytoestrogens due to their potential medical usage in hormone replacement therapy(HRT). The present study was designed to investigate the in vitro effects of estrogen-like activities of two widespread coumarins, osthole and imperatorin, using the MCF-7 cell proliferation assay and their alkaline phosphatase(ALP) activities in osteoblasts Saos-2 cells. The two compounds were found to strongly stimulate the proliferation of MCF-7 cells. The estrogen receptor-regulated ERα, progesterone receptor(PR) and PS2 m RNA levels were increased by treatment with osthole and imperatorin. All these effects were significantly inhibited by the specific estrogen receptor antagonist ICI182, 780. Cell cycle analysis revealed that their proliferation stimulatory effect was associated with a marked increase in the number of MCF-7 cells in S phase, which was similar to that observed with estradiol. It was also observed that they significantly increased ALP activity, which was reversed by ICI182,780. These results suggested that osthole and imperatorin could stimulate osteoblastic activity by displaying estrogenic properties or through the ER pathway. In conclusion, osthole and imperatorin may represent new pharmacological tools for the treatment of osteoporosis.

川芎白芷药对对偏头痛小鼠行为学及血清NO、CGRP和IL-6含量的影响

目的 考察川芎白芷药对对偏头痛小鼠行为学及血清一氧化氮(nitric oxide, NO)、降钙素基因相关肽(calcitonin gene related peptide, CGRP)和白细胞介素-6(interleukin-6, IL-6)含量的影响,探讨川芎白芷药对对偏头痛的作用机制。方法 选取广西医科大学第二附属医院购买的56只SPF级雄性C57BL/6小鼠为研究对象,选取川芎白芷药对的指标性成分阿魏酸、欧前胡素为治疗药物,按处理方法不同将健康雄性小鼠随机分为7组,即空白组、模型组、阳性对照组、阿魏酸组、欧前胡素组、阿魏酸+欧前胡素低剂量组和阿魏酸+欧前胡素高剂量组,每组8只。采用硝酸甘油腹腔注射的方法制作偏头痛小鼠模型。造模成功后,对各组小鼠进行行为学考察,并检测血清中的NO、CGRP和IL-6的含量。结果 与对照组偏头次数(9.25±2.77)次比较,0~30 min内模型组小鼠挠头次数(26.25±4.60)次增加,阳性对照组(13.25±3.23)次,欧前胡素组(19.13±3.89)次,阿魏酸组(18.75±2.77)次,阿魏酸+欧前胡素低剂量组(16.88±2.52)次,阿魏酸+欧前胡素高剂量组(12.38±2.18)次,组间比较,差异有统计学意义(F=23.89,P<0.01)。模型组小鼠血清中NO、CGRP和IL-6的含量升高,差异有统计学意义(P均<0.05)。给予阿魏酸、欧前胡素或低、高剂量的阿魏酸+欧前胡素联合治疗后均能减少受试小鼠的挠头次数,并降低小鼠血清中NO、CGRP和IL-6的含量,其中阿魏酸+欧前胡素高剂量组的降幅最大,差异有统计学意义(P均<0.05)。结论 阿魏酸配伍欧前胡素后可有效改善偏头痛小鼠的症状,提示川芎白芷药对对偏头痛小鼠的作用机制可能与减少偏头痛小鼠血清NO、CGRP和IL-6水平含量有关。

基于网络药理学与分子对接的欧前胡素治疗宫颈癌的作用机制

目的探讨欧前胡素治疗宫颈癌的活性成分和作用机制。方法通过使用网络药理学筛选欧前胡素药用成分和疾病宫颈癌靶点并进行相关的分子对接技术验证。中草药系统药理平台查找欧前胡素的有效成分和作用靶点,采用OMIM和Gen⁃eCards数据库,对宫颈癌相关的目标基因进行交叉筛选,Cytoscape软件分析宫颈癌和欧前胡素的共同靶点,String数据库分析并建构PPI网络分析,Rstudo 4.0软件分析并绘图,DAVID生物信息数据库统计,GO富集、KEGG富集分析。分子对接使用AutoDock分析。结果PPI网络结果显示TERT、ESR1、PTGS2、PGR、PPARG、CA9、ESR2、AR、CASP9、ALPL、CLK1可能为欧前胡素和宫颈癌的核心靶点。GO富集得到26个生物过程,KEGG富集得到6条主要通路,包括Chemical cancer recep⁃tor activation、Estrogen、Breast cancer、VEGF、Prolactin等信号通路。分子对接结果显示LYS-243、ARG-240和GLU-272等化合物能与宫颈癌的核心靶点有良好的结合力。结论欧前胡素可能通过与ESR1、PGR、PTGS2、ESR2、CASP9等结合,在VEGE、雌激素、孕激素等信号通路发挥抗治疗宫颈癌的作用。

欧前胡素调节ERK/MAPK信号通路对肺结核大鼠炎症反应的影响

目的 探讨欧前胡素(Imp)调节细胞外调节蛋白激酶(ERK)/有丝分裂原激活蛋白激酶(MAPK)信号通路对肺结核大鼠炎症反应的影响。方法 64只大鼠随机分为对照组12只及造模组52只,造模组大鼠通过尾部注射结核杆菌方法建立肺结核大鼠模型,之后随机分为模型组、Imp低(Imp-L,25 mg/kg)、中(Imp-M,50 mg/kg)、高剂量(Imp-H,100 mg/kg)组、Imp-H+ERK特异性激活剂(EGF,100 mg/kg Imp+25 mg/kg EGF)组。干预结束后,主动脉采血,ELISA检测各组大鼠血清中白细胞介素-6(IL-6)、γ干扰素(IFN-γ)、环氧化酶-2(COX-2)水平;分离肺组织,HE、Tunel分别检测大鼠肺组织病理学变化及细胞凋亡情况;统计肺组织中结核杆菌菌落数;Western blot检测p-ERK1/2/ERK1/2、p38 MAPK表达水平。结果 与对照组相比,模型组肺组织严重病变,IL-6、IFN-γ、COX-2、细胞凋亡率、结核杆菌菌落数、p-ERK1/2/ERK1/2、p38 MAPK表达均显著增加(P<0.05);与模型组相比,Imp-L组、Imp-M组、Imp-H组病理损伤得到缓解,IL-6、IFN-γ、COX-2、细胞凋亡率、结核杆菌菌落数、p-ERK1/2/ERK1/2、p38 MAPK表达显著降低,以Imp-H组变化最为显著(P<0.05);与Imp-H组相比,Imp-H+EGF组病理损伤进一步加重,IL-6、IFN-γ、COX-2、细胞凋亡率、结核杆菌菌落数、p-ERK1/2/ERK1/2、p38 MAPK表达显著增加(P<0.05)。结论 Imp可降低肺结核炎症反应,与抑制ERK/MAPK信号通路的激活有关。

欧前胡素对高脂型蛋氨酸-胆碱缺乏饲粮诱导的非酒精性脂肪性肝病小鼠血清生化指标和肝脏的影响

本试验旨在研究欧前胡素(IMP)对高脂型蛋氨酸-胆碱缺乏饲粮(MCD-HFD)引起的小鼠非酒精性脂肪性肝病(NAFLD)的影响。将50只9周龄雄性C57BL/6小鼠随机分为5组,每组10只。MCS-LFD组(对照组)饲喂蛋氨酸-胆碱充分低脂饲粮(MCS-LFD),MCD-HFD组(模型组)、MCD-HFD+IMP25组、MCD-HFD+IMP50组和MCD-HFD+IMP100组小鼠饲喂MCD-HFD,连续喂养8周。各组均在喂养4周后对小鼠进行灌胃处理,连续4周。MCD-HFD+IMP25组、MCD-HFD+IMP50组和MCD-HFD+IMP100组小鼠分别灌胃25、50和100 mg/(kg·d)IMP,MCS-LFD组和MCD-HFD组小鼠灌胃等量生理盐水。饲喂8周后处死,取血清检测天门冬氨酸氨基转移酶(AST)、丙氨酸氨基转移酶(ALT)活性和甘油三酯(TG)、总胆固醇(TC)含量;通过苏木精-伊红(HE)染色以及Masson染色检测肝脏组织脂肪变性和纤维化;称量肝脏湿重,计算肝脏指数;通过Western blot法检测肝脏中肉碱棕榈酰基转移酶1A(CPT1A)的蛋白表达量。结果显示:1)与MCS-LFD组相比,MCD-HFD组小鼠体重和增重显著降低(P<0.05),肝脏湿重显著增加(P<0.05),肝脏指数极显著升高(P<0.01),血清中AST、ALT活性和TG、TC含量均极显著升高(P<0.01),肝脏中CPT1A的蛋白表达量极显著降低(P<0.01)。2)切片结果显示,与MCS-LFD组相比,MCD-HFD组小鼠肝细胞排列紊乱,发生气球样变性,出现大量脂肪性空泡,且肝细胞周围纤维化。3)与MCD-HFD组相比,MCD-HFD+IMP50组小鼠的体重和增重显著升高(P<0.05),肝脏湿重显著降低(P<0.05),肝脏指数极显著降低(P<0.01),血清AST和ALT活性极显著下降(P<0.01),TG和TC含量显著下降(P<0.05),肝脏中CPT1A的蛋白表达量显著升高(P<0.05)。4)与MCD-HFD组相比,MCD-HFD+IMP100组小鼠体重无显著变化(P>0.05),肝脏湿重和肝脏指数均极显著降低(P<0.01),血清AST、ALT活性和TG、TC含量均极显著下降(P<0.01)。5)与MCD-HFD组相比,IMP处理能够减少肝脏中空泡数量,改善肝细胞气球样变性和纤维化程度,且呈剂量依赖性。由此可见,IMP能够缓解MCD-HFD诱导的NAFLD小鼠的肝脏损伤,改善体内脂肪代谢,缓解脂质沉积,对肝脏具有保护作用。

风湿定胶囊中徐长卿和白芷质量控制研究

目的:研究风湿定胶囊中徐长卿和白芷的质量控制方法。方法:采用薄层色谱法对风湿定胶囊中徐长卿和白芷进行鉴别研究,采用高效液相色谱法测定风湿定胶囊中徐长卿中丹皮酚和白芷中欧前胡素、异欧前胡素的含量,色谱柱waters Xbridge C_(18)(250 mm×4.6 mm,5μm),流动相乙腈-2%冰乙酸(50∶50)溶液,流速1.0 mL/min,柱温30℃,检测波长250 nm(欧前胡素、异欧前胡素)和274 nm(丹皮酚)。结果:薄层色谱斑点清晰,分离度较好;采用高效液相色谱同时测定欧前胡素、异欧前胡素、丹皮酚,分别在0.0106μg~0.2128μg、0.0031μg~0.0620μg、0.0147μg~1.4660μg范围内线性关系良好;平均回收率分别为100.0%(RSD=0.5%)、101.2%(RSD=0.9%)、98.9%(RSD=1.1%)。结论:该方法准确可靠,重复性好,可用于风湿定胶囊中徐长卿和白芷的质量控制。

欧前胡素衍生物对COPD肺泡Ⅱ型细胞活性及耐药蛋白的影响

目的探究欧前胡素衍生物(IMP-1)对慢性阻塞性肺疾病(COPD)肺泡Ⅱ(ATⅡ)型细胞活性及耐药蛋白的影响。方法ATⅡ型细胞分为空白组(常规培养基进行培养的生长良好的ATⅡ型细胞)、香烟烟雾提取物(CSE)组(加入2%CSE诱导培养)、IMP-1组(采用10μmol/L的IMP-1干预经CSE诱导的ATⅡ型细胞)。采用四甲基偶氮唑盐(MTT)法测定ATⅡ型细胞24 h、48 h、72 h增殖率,Hoechst 33342染色法检测ATⅡ型细胞凋亡率,流式细胞分析仪分析各周期细胞占比,软琼脂克隆形成实验检测ATⅡ型细胞克隆数量,Western blot法检测多耐药基因1(MDR1)及多药耐药相关蛋白1(MRP1)蛋白表达水平。结果与空白组比较,CSE组细胞凋亡率、ATⅡ型细胞周期G0/G_(1)期占比升高,在24 h、48 h、72 h细胞的增殖率和S、G_(2)/M期占比降低(P<0.05);与CSE组比较,IMP-1组细胞增殖率和S、G_(2)/M期占比及细胞克隆数量升高,ATⅡ型细胞周期G0/G_(1)期占比和MDR1、MRP1蛋白降低(P<0.05)。结论IMP-1可能通过下调CSE诱导的ATⅡ型细胞的MDR1、MRP1蛋白表达,从而抑制细胞的异常活化,增加其凋亡。

利鼻片HPLC指纹图谱及多组分含量测定

目的建立多组分含量测定结合化学计量学分析,评价利鼻片质量。方法采用高效液相色谱法,Waters SunFire C18色谱柱(4.6 mm×250 mm,5μm);乙腈(A)-0.55%磷酸水溶液(B)为流动相;梯度洗脱,流速:1.0 ml·min^(-1);切换检测波长:323、280、248 nm;柱温:35℃,进样量:10μl。采用中药色谱指纹图谱相似度评价系统结合聚类分析与正交偏最小二乘判别分析评价15批利鼻片质量。结果建立的利鼻片HPLC指纹图谱共确定了19个共有峰,并指认出其中7个色谱峰;利鼻片中菊苣酸、绿原酸、咖啡酸、黄芩苷、木兰脂素、欧前胡素、异欧前胡素的平均回收率分别为100.30%、99.87%、99.25%、99.45%、99.08%、98.75%和98.58%,RSD均<1.5%(n=6)。15批利鼻片中上述7个成分的含量测定结果分别为15.05~17.93、10.17~12.51、7.03~9.30、4.42~6.50、1.08~2.76、1.01~1.76、1.00~1.90 mg·g^(-1)。不同批次利鼻片存在差异,区分的特征峰为菊苣酸、绿原酸和木兰脂素。聚类分析结果表明3家企业的样品各自聚为一类,S1~S4(陕西康惠)聚为一类,S5~S10(通化民泰)聚为一类,S11~S15(长春银诺克)聚为一类。正交偏最小二乘法判别分析结果表明这4种化学成分〔10号峰菊苣酸(VIP值为2.216)、6号峰未知(VIP值为1.934)、4号峰绿原酸(VIP值为1.438)、13号峰木兰脂素(VIP值为1.013)〕显著影响利鼻片的分类,是引起该制剂质量差异的潜在标志性成分,可以考虑将这些差异标志性成分作为指标成分监控利鼻片的质量。结论建立的综合质量评价法简便、专属、准确,可客观评价利鼻片质量。

四倍体白芷药材中欧前胡素的含量测定

目的 :测定四倍体白芷药材中欧前胡素的含量 ,并与原二倍体白芷相比较。方法 :采用高效液相色谱法 ,色谱柱Nova pak 4 .6mm× 2 0 0mm ,5 μm ,流动相乙腈 水 ,流速 1mL·min-1,检测波长 2 4 8nm ,柱温 2 5℃。结果 :四倍体白芷药材中欧前胡素含量达 0 .4 6 % ,二倍体对照药材仅为 0 .2 2 5 % ,含量增加了 10 4 .4 %。结论

白芷质量标准研究

目的 :对白芷药材进行质量标准研究。方法 :TLC法检定白芷药材中 4个香豆素类成分 ,HPLC法测定白芷中 2个主要成分的含量。结果与结论 :白芷药材中同时检定出欧前胡素、异欧前胡素、比克白芷素及水化氧合前胡素 ,欧前胡素和异欧前胡素的含量分别不得低于 0 .1%和 0 .0 4 %。

HPLC测定13种白芷中欧前胡素和异欧前胡素的含量

目的 建立一种控制白芷药材质量的方法。方法 采用HPLC法 ,甲醇 -水 (70∶30 )为流动相 ,检测波长 2 5 4nm。结果 欧前胡素在 0 .974～ 3.896 μg范围内线性关系良好 ;异欧前胡素在 0 .36 0～ 2 .6 4 0 μg范围内线性关系良好。精密度及加样回收率良好。结论 该方法准确、迅速、重复性好 。

不同产地白芷中欧前胡素含量及HPLC指纹图谱的对比研究

目的:比较不同产地白芷中欧前胡素含量的差异,同时对不同产地白芷药材进行HPLC指纹图谱对比研究。方法:收集7省市15个白芷主产区对口药材及种子,并将种子种植在四川遂宁白芷种质资源圃中,于次年正常采收期采挖、干燥,对其及与之相对应的白芷对口药材进行欧前胡素含量测定及HPLC指纹图谱对比研究。结果:不同产地白芷中欧前胡素含量存在差异;不同产地样品栽种于同一环境后,欧前胡素含量整体有明显提高;化学表达也随产地及栽培方法的一致而趋同。结论:白芷中香豆素类成分与产地环境密切相关,产地生境及栽培技术可能是决定其质量的关键因素。

白芷中四种线型呋喃香豆素类成分药理作用研究

研究了白芷中异欧前胡素、欧前胡素、水合氧化前胡素、白当归素等4种主要线型呋喃香豆素类成分的药理作用。分别采用热板法、醋酸扭体法观察镇痛活性;家兔离体回肠法观察解痉活性;MTT法观察抗肿瘤活性。发现异欧前胡素、欧前胡素具有明显的镇痛作用,能明显抑制热板、醋酸所致小鼠疼痛,为白芷镇痛的活性成分;异欧前胡素、欧前胡素、水合氧化前胡素均能明显缓解BaCl2所致兔肠平滑肌痉挛,为白芷解痉的活性成分;异欧前胡素、水合氧化前胡素具有显著抗肿瘤作用,对HL-60、P388、HELA、A549等细胞株的生长均有明显抑制作用。

HPLC法同时测定蛇床子中蛇床子素和欧前胡素含量

目的用高效液相色谱法同时测定中药蛇床子中蛇床子素和欧前胡素的含量。方法采用KromasilC8(2 5 0mm× 4 6mm ,5 μm)为色谱柱 ,以甲醇 水 (体积比 6 5∶35 )为流动相的HPLC法 ,检测波长为 310nm ,流速为 0 8mL·min-1,柱温为室温。结果以醋酸氟轻松为内标 ,蛇床子素和欧前胡素分别在 13～ 2 0 8mg·L-1和 8～ 12 8mg·L-1内 ,线性关系良好 (r≥ 0 9998) ;平均回收率分别为 98 2 %和 97 5 % ;RSD分别为 1 7%和 2 0 % (n =9)。结论本法简便快速 ,回收率及重现性良好 。

北沙参栽培品种与药材质量的相关性研究

目的:探讨北沙参不同栽培品种与药材质量的关系。方法:接文献方法和药典规定检测北沙参不同栽培品种的多糖、欧前胡素、浸出物等成分含量。结果:白条参的可溶性糖、粗多糖、总糖、水浸出物、醇浸出物等含量较另两个品种高(P<0.05),欧前胡素以大红袍含量最高(P<0.05)。结论:用于抑制体液免疫和细胞免疫以及抑制T、B细胞的增生作用时,用白条参效果较好;用于镇静、解痉、平喘等作用时,用大红袍入药更加科学。