骆驼蓬的研究进展

通过对骆驼蓬的研究进展进行综述,认为骆驼蓬主要化学成分为生物碱类和黄酮类成分,其主要药理作用有抗肿瘤、抗癌、抗炎、镇痛、止痒、抗银屑病等,为进一步开发利用骆驼蓬的药用价值提供参考。     

抗炎免疫中药有效成分的药理学研究

综述近年来抗炎免疫中药的研究概况。将近年来研究较多的抗炎免疫中药活性成分,按苷类、生物碱类、黄酮类、挥发油类等化学结构分类简述其抗炎免疫作用,为进一步开发抗炎免疫中药和天然药物提供参考。     

中药抗炎免疫机理中对基因转录环节的调控作用研究进展

随着对抗炎免疫药理认识的逐步深入,抗炎免疫药物可以划分为非甾类抗炎免疫药(NSAIDs),甾体类抗炎免疫药(SAIDs)和疾病调修药(DMDs)。疾病调修药包括免疫抑制药、免疫增强药和免疫调节药3种[1]。由于中药“清热解毒”、“祛风除湿”、“扶正固本”等对免疫的双向调节作用与现代医学的抗炎、免疫观念密切相关,从中药中寻找抗炎免疫活性成分已成为当前抗炎免疫研究的热点。近年来,国内外的药学研究人员对具有抗炎免疫作用的中草药进行广泛研究,对具有药理活性的化学成分,如苷类、生物碱、多糖、萜类、香豆素、挥发油等的抗炎免疫作用和作…     

骆驼蓬子总生物碱改善小鼠学习记忆能力

目的采用多种小鼠记忆障碍模型筛选骆驼蓬子抗老年痴呆的有效部位(总生物碱和非生物碱部位)。方法采用避暗实验法分别对骆驼蓬子总生物碱和非生物碱部位对东莨菪碱和30%乙醇所致的记忆获得性障碍和记忆再现障碍性小鼠学习记忆能力的影响进行考察。通过小鼠跳台实验法进一步验证有效部位对东莨菪碱、30%乙醇和亚硝酸钠所致小鼠记忆获得性障碍、记忆再现障碍及记忆巩固障碍模型的改善作用。结果避暗实验结果表明总生物碱在较高剂量下对东莨菪碱和30%乙醇所致记忆获得性障碍和记忆再生性障碍有一定的改善作用(与模型组比较,可显著延长小鼠潜伏期,P0.01)。小鼠跳台实验法进一步证明高剂量骆驼蓬子总生物碱对东莨菪碱和30%乙醇诱导的学习记忆障碍具有改善作用,但对亚硝酸钠所致记忆巩固障碍无明显改善作用。结论总生物碱是骆驼蓬子改善小鼠学习记忆的有效部位。     

骆驼蓬研究现状

骆驼蓬又叫骆驼蒿、苦苦菜、臭草、臭牡丹,为蒺藜科植物骆驼蓬属多年生草本植物的全草,是西北地区重要的民族、民间药。现代药理研究发现其含有多种生物碱,生物碱基本骨架为生物碱基,包括β-咔波啉类和喹唑啉类,其中β-咔波啉类有骆驼蓬碱、去氢骆驼蓬碱、去甲氧基骆驼蓬碱等。骆驼蓬生物碱具有抗肿瘤相关作用。本文对其药用进行系统总结,并为骆驼蓬进一步研究提出建议。     

骆驼蓬有效成分的提取工艺及抗肿瘤机制研究进展

骆驼蓬(Peganum)为蒺藜科(Zygophyllaceae)植物骆驼蓬属多年生草本植物的全草,是维吾尔医使用已久的药材,现代药理研究发现其含有多种生物碱,β咔啉类生物碱是骆驼蓬中最有价值的生物碱,被证明具有良好的抗肿瘤作用,为了更好地开发骆驼蓬的药用价值,本文对骆驼蓬植物的有效成分生物碱的提取工艺及抗肿瘤机制进行综述,为其进一步开发利用提供参考。     

骆驼蓬碱对苯福林引起家兔尿道收缩的促进作用

文献报道,从骆驼蓬(Peganum harmala)种子中首次提取分离的骆驼蓬碱具有兴奋中枢神经系统作用。已知骆驼蓬的种子含有多种生物碱,其中骆驼蓬碱和去氢骆驼蓬碱还是较强的致幻剂。离体主动脉条实验显示骆驼蓬碱在未达到自身直接作用的剂量时,对苯福林和肾上腺素引起的收缩具有促进作     

痛风方不同组分抗炎镇痛及降低血尿酸作用的比较研究

目的:比较痛风方用不同工艺提取分离的各组分(总黄酮与总生物碱混合物、总黄酮、总生物碱)的抗炎镇痛和降血尿酸作用。方法:采用小鼠耳廓二甲苯致炎法和小鼠化学刺激法(扭体法)观察其抗炎镇痛作用,以次黄嘌呤建立小鼠高尿酸血症模型观察其降血尿酸作用。结果:痛风方中的总黄酮与总生物碱混合物和总黄酮具有明显的抗炎作用;痛风方中的总黄酮和总生物碱混合物、总黄酮和总生物碱对化学刺激引起的疼痛有显著的镇痛作用;痛风方中的总黄酮和总生物碱对小鼠高尿酸血症的形成有明显抑制作用。结论:痛风方中的总黄酮和总生物碱混合物具有抗炎镇痛作用;痛风方中的总生物碱具有镇痛和降血尿酸作用;痛风方中的总黄酮具有抗炎镇痛和降血尿酸作用。     

骆驼蓬总生物碱提取物溶解性能表征方法的探讨

目的:考察骆驼蓬总生物碱提取物在不同溶剂中的溶解性能,并对中药提取物溶解性的评价方法进行探讨。方法:分别采用沉淀法、指标成分测定法及粒径测定法测定骆驼蓬总生物碱提取物的溶解性及其在不同溶剂中的粒径分布情况。结果:骆驼蓬总生物碱提取物及其指标性成分骆驼蓬碱、去氢骆驼蓬碱在80%乙醇,95%乙醇及无水乙醇中均具有较好的溶解性,在60%乙醇中溶解性较差,在水中溶解性最差。骆驼蓬总生物碱提取物在不同溶剂中形成混悬液的粒径大小顺序为水95%乙醇无水乙醇80%乙醇60%乙醇。结论:骆驼蓬总生物碱提取物在80%以上的乙醇溶液中具有较好的溶解性。沉淀法和指标成分法测定结果具有一定的相关性;粒径测定法可提供提取物分散情况的信息;3种方法结合能较全面地反映中药提取物溶解性情况。     

骆驼蓬总生物碱中骆驼蓬碱、去氢骆驼蓬碱及其代谢产物大鼠体内药代动力学研究

目的研究骆驼蓬总生物碱中骆驼蓬碱、去氢骆驼蓬碱及其活性代谢产物骆驼蓬醇和骆驼蓬酚在大鼠体内的药代动力学特征。方法口服骆驼蓬总生物碱(140 mg/kg)及静脉注射骆驼蓬碱与去氢骆驼蓬碱的混合溶液(均为3.3 mg/kg),采集不同时间点的血浆,采用UPLC-MS/MS法测定大鼠血浆中骆驼蓬碱、去氢骆驼蓬碱、骆驼蓬醇、骆驼蓬酚的血药浓度,并计算药代动力学参数。结果灌胃和静脉给药后,在血浆中检测到骆驼蓬碱、去氢骆驼蓬碱、骆驼蓬醇和骆驼蓬酚,但骆驼蓬酚的血药浓度在24 h时未下降而未能计算药动参数。静注给药后,骆驼蓬碱、去氢骆驼蓬碱和骆驼蓬醇的t1/2e分别为2.554、3.116、1.899 h,MRT分别为1.700、1.311、1.880 h,AUC0-t为373.1、2033.0、8.914 ng·h/mL。口服总生物碱后骆驼蓬碱、去氢骆驼蓬碱和骆驼蓬醇的Cmax分别为347.6、184.5、32.7 ng/mL,Tmax分别为3.200、1.150、0.300 h,t1/2e分别为6.994、5.625、21.912 h,MRT分别为8.588、9.791、27.780 h,AUC0-t为2 755.5、1 202.8、129.8 ng·h/mL。口服总生物碱后骆驼蓬碱和去氢骆驼蓬碱的绝对生物利用度分别为63.22%和4.96%。结论口服总生物碱后骆驼蓬碱和去氢骆驼蓬碱均可迅速吸收并迅速代谢,骆驼蓬碱与去氢骆驼蓬碱相比较,具有更高的生物利用度,代谢产物骆驼蓬醇和骆驼蓬酚与原型骆驼蓬碱和去氢骆驼蓬碱相比较,消除速率相对较慢。此外,静注给药后,体内去氢骆驼蓬碱的初始血药浓度明显高于骆驼蓬碱。     

Inhibition of myeloperoxidase activity by the alkaloids of Peganum harmala L. (Zygophyllaceae)

Ethnopharmacological relevance

Seeds and aerial parts of Peganum harmala L. are widely used in Algeria as anti-inflammatory remedies. Evaluation of Peganum harmala total alkaloids extracts and pure β-carboline compounds as an anti-inflammatory treatment by the inhibition of an enzyme key of inflammatory, myeloperoxidase (MPO) and HPLC quantification of the alkaloids from the different parts of plant.

Materials and methods

MPO inhibition was tested using taurine chloramine test. The inhibition of LDL oxidation induced by MPO was carried out. The molecular docking analysis of Peganum harmala alkaloids on MPO was performed using the Glide XP docking protocol and scoring function and the redox potential of alkaloids was determined using an Epsilon potentiostat. The concentration of harmala alkaloids was determined using HPLC analysis.

Results

The HPLC profiling of the active total alkaloids indicates that β-carboline e.g. harmine, harmaline, harmane, harmol and harmalol are major components. As β-carbolines resemble tryptamine, of which derivatives are efficient inhibitors of MPO, the harmala alkaloids were tested for their activity on this enzyme. Total alkaloids of the seeds and of the aerial parts strongly inhibited MPO at 20 µg/mL (97±5% and 43±4%, respectively) whereas, at the same concentration, those of the roots showed very low inhibition (15±6%). Harmine, harmaline and harmane demonstrated a significant inhibition of MPO at IC₅₀ of 0.26, 0.08 and 0.72 µM respectively. These alkaloids exerted a similar inhibition effects on MPO-induced LDL oxidation. Molecular docking analysis of Peganum harmala alkaloids on MPO showed that all active Peganum harmala alkaloids have a high affinity on the active site of MPO (predicted free energies of binding up to −3.1 kcal/mol). Measurement of redox potentials versus the normal hydrogen electrode clearly differentiated (i) the high MPO inhibitory activity of harmine, harmaline and harmane (+1014, 1014 and 1003 mV, respectively); and (ii) the low activity of harmalol and harmol (+629/778 and 532/644 mV, respectively). A reverse phase HPLC method has been developed to determine simultaneously five alkaloids of Peganum harmala. Seeds contained all five β-carboline derivatives with the main active alkaloids, harmaline and harmine, being up to 3.8% and 2.9%, respectively. Up to 3.2% of harmine was determined in the roots. The four β-carboline derivatives, harmine, harmaline, harmane and harmalol were identified in the aerial parts. The highest inhibitory effect observed in seeds and the moderate effect of aerial parts could be explained by their harmine and harmaline content. In contrast, the very weak inhibition of the root extract, despite the presence of harmine, may tentatively be explained by the high concentration of harmol which can reduce Compound II of MPO to the native form.

Conclusion

The inhibition of MPO by Peganum harmala β-carboline alkaloids, herein reported for the first time, may explain the anti-inflammatory effect traditionally attributed to its herbal medicine.     

Effect of Peganum harmala or its beta-carboline alkaloids on certain antibiotic resistant strains of bacteria and protozoa from poultry

In the present study the antimicrobial potential of various extracts from 12 medicinal plants has been investigated in vitro on multiple antibiotic resistant pathogens and some selected protozoa isolated from poultry. The initial examination was performed on E. coli (n = 10) using disc and agar well diffusion assays. Only two plants, Peganum harmala (seeds) and Eucalyptus globulus (leaves) showed positive responses. The active extracts were also investigated against an additional 19 bacteria and the clonal cultures of three protozoa (Histomonas meleagridis, Tetratrichomonas gallinarum and Blastocystis sp.). Only Peganum harmala was found to inhibit the growth of all bacteria and protozoa at 0.38-1.55 mg/mL and 0.63-1.65 mg/mL, respectively. To investigate the potential role of alkaloids in crude extracts of Peganum harmala, four known beta-carbolin alkaloids were quantified and their antimicrobial activity was compared using a microdilution assay. Harmaline was found to be in the highest concentration followed by harmine and harmalol, whereas harmane could not be detected. The activity of the pure alkaloids was in the order harmane > harmaline > harmalol > or = harmine for all bacteria, while for protozoa, it was different depending on the microorganism. It is concluded that Peganum harmala or its alkaloids could probably be used for the control of antibiotic resistant isolates of bacteria as well as protozoa.     

醋制骆驼蓬可行性研究

目的本文探讨骆驼蓬全草醋与红酒炮制品中骆驼蓬碱、去氢骆驼蓬碱的含量变化,为醋制骆驼蓬的可行性提供参考。方法采用HPLC法测定骆驼蓬各炮制品中骆驼蓬碱、去氢骆驼蓬碱含量。结果传统新疆红酒煮制骆驼蓬其骆驼蓬碱、去氢骆驼蓬碱含量最低,20%、30%、40%醋液煮制骆驼蓬中骆驼蓬碱、去氢骆驼蓬碱含量均低于生品药材(P<0.01)。结论醋与红酒制骆驼蓬均可有效降低其生物碱含量,醋亦可作为骆驼蓬减毒炮制的辅料选择。     

产业化生产中草乌不同炮制品的“减毒-存效”研究

研究产业化生产中草乌不同炮制品的毒性和药效的相关性,确定"减毒-存效"的最佳炮制方法。采用HPLC测定草乌及其不同炮制品中6种乌头碱类生物碱的含量;采用Bliss法分别测定草乌及其不同炮制品对小鼠半数致死量(LD50)或最大给药剂量;以二甲苯致耳肿胀法和醋酸扭体法试验考察不同炮制品的抗炎、镇痛作用。结果显示:①草乌生品中3种双酯型生物碱总量为0.358 8%;药典水煮法炮制品中3种双酯型生物碱总量为0.002 2%,3种单酯型生物碱总量为0.036 2%;常压蒸制法炮制品中3种双酯型生物碱总量为0.006 0%,3种单酯型生物碱总量为0.056 7%;②生草乌的LD50为5.4 g·kg^-1,药典水煮法和常压蒸制法炮制品的最大给药剂量为133.34 g·kg^-1;病理观察显示,与正常组比较,2种炮制品对于小鼠的心、肝、肾均有一定的损伤;③药典水煮法和常压蒸制法炮制品均具有抗炎、镇痛作用(P<0.01或P<0.05),其抗炎镇痛作用强弱为:常压蒸制法>药典水煮法。上述结果提示:生草乌毒性较大,采用常压蒸制法炮制后毒性明显降低,同时又保留了良好的的抗炎和镇痛作用;与药典水煮法相比,常压蒸制法具有工艺可操作性强、饮片质量稳定、抗炎镇痛作用更强等优势,适用于产业化生产。     

Antitussive, expectorant and anti-inflammatory activities of four alkaloids isolated from Bulbus of Fritillaria wabuensis

Ethnopharmacological relevance

Bulbus Fritillaria Cirrhosae (BFC), known by the Chinese name “Chuan-Bei-Mu”, is used as an antitussive, antiasthmatic and expectorant drug for more than 2000 years in China, and Bulbus of Fritillaria wabuensis S. Y. Tang & S. C. Yueh (BFW) was recorded in the 2010 edition of China Pharmacopoeia as one of sources for BFC. The primary objective of this study was to evaluate the antitussive, expectorant and anti-inflammatory effects of alkaloids - imperialine, imperialine-β-N-oxide, isoverticine, and isoverticine-β-N-oxide, which were isolated from BFW, and to provide experimental evidence for its traditional use.

Materials and methods

The alkaloids were isolated using phytochemical methods, and their structures were determined by spectroscopic analysis. Their antitussive effects were measured using murine model of ammonia induced cough, the expectorant effects were evaluated by measuring mice's tracheal phenol red output, and the anti-inflammatory effects were assessed by using the murine model of xylene induced ear edema.

Results

The structures of the four alkaloids - imperialine, imperialine-β-N-oxide, isoverticine, and isoverticine-β-N-oxide isolated from BFW were confirmed. The four alkaloids significantly inhibited cough frequency and increased latent period of cough in mice induced by ammonia. Imperialine and isoverticine showed obviously antitussive activities in a dose-dependent manner. Besides, the four alkaloids markedly enhanced mice's tracheal phenol red output in expectorant assessment and significantly inhibited the development of ear edema in anti-inflammatory evaluation assay. Moreover, significant differences were found between the structure-activity relationships of the four alkaloids.

Conclusions

The four alkaloids exhibited significant antitussive, expectorant and anti-inflammatory activities. We suggest that they may be the active ingredients of BFW. The results of the present study provided evidence for BFW to be used as an antitussive and expectorant Traditional Chinese Medicine (TCM).     

多裂骆驼蓬化学成分研究

目的:对多裂骆驼蓬地上部分的化学成分进行研究。方法:应用多种色谱技术进行分离纯化,通过理化方法和波谱数据进行结构鉴定。结果:分离并鉴定了6个生物碱类成分,分别为:脱氧鸭嘴花酮碱(1)、l-鸭嘴花酮碱(2)、哈尔明碱(3)、鸭嘴花种碱(4)、吴茱萸碱(5)和fagomine(6)。结论:其中,化合物5和6为首次从该属植物中分离得到。     

板蓝根抗炎作用有效部位初步筛选

目的:分离并初步筛选板蓝根抗炎作用有效部位.方法:通过膜分离将板蓝根总提取物分为不同截留相对分子质量段,采用二甲苯致小鼠耳肿胀初步筛选,再将有效相对分子质量段用大孔树脂、离子交换树脂分离得到不同部位进一步采用二甲苯致小鼠耳肿胀、小鼠腹腔毛细血管通透性评价活性,最后通过特殊颜色反应确定有效部位化学性质.结果:板蓝根中相对分子质量小于1 000的物质对二甲苯致小鼠耳肿胀模型抑制率为40.29％,与空白组相比有显著性差异(P＜0.05).板蓝根小于1000D物质中被732阳离子交换树脂吸附部分对二甲苯致小鼠耳肿胀模型抑制率为28.20％,对醋酸致小鼠毛细血管通透性攻变模型抑制率为17.76％,与空白组相比均有显著性差异(P＜0.05).颜色反应说明该部位主要为氨基酸类及生物碱类成分.结论:板蓝根总氨基酸、总生物碱部位可能是其抗炎有效部位.     

大孔吸附树脂法富集提取废液中骆驼蓬碱和去氢骆驼蓬碱

 目的 研究大孔树脂富集骆驼蓬中总生物碱提取后废液中骆驼蓬碱和去氢骆驼蓬碱的最佳工艺条件。方法 用HPLC测定生物碱含量,以骆驼蓬碱和去氢骆驼蓬碱的吸附量和解吸率为考察指标,对6种不同类型的树脂（LSA-8b、LSA-5b、XDA-1、LSA-21、LSA-10、D101）进行评价。考察药液pH值、吸附流速、吸附温度、洗脱流速等参数对骆驼蓬碱和去氢骆驼蓬碱的吸附和洗脱效果的影响。结果 LSA-5b对骆驼蓬碱和去氢骆驼蓬碱具有较好的富集能力,最佳富集工艺条件：吸附pH值为9,吸附温度为30 ℃,上样流速为3.5 BV（倍柱体积）·h-1,骆驼蓬碱饱和吸附量为32.34 mg·g-1;最佳的洗脱溶剂为体积分数为70%乙醇,最佳洗脱流速为1.5 BV·h-1,洗脱用量为16.7 BV,骆驼蓬总生物碱洗脱率达86.3%。结论 在确定的工艺条件下,体积分数70%的乙醇洗脱液中骆驼蓬总生物碱的含量提高了10倍。     

Pharmacological effect and toxicity of alkaloids from Gelsemium elegans Benth

Gelsemium elegans Benth. (Loganiaceae), a toxic plant indigenous to southeastern Asia, is well known among hilltribes as an effective means for committing suicide. A crude alkaloidal fraction from its leaves was isolated by conventional acid-base extraction. Tests in animals showed that the alkaloids exerted analgesic and anti-inflammatory effects. At a lethal dose, the alkaloids produced violent clonic convulsions that led to respiratory failure. Since the convulsions could be prevented by pentobarbital or diazepam and potentiated by reserpine, it is postulated that the alkaloids act centrally against GABA action.     

Anti-inflammatory effect of Solanum lycocarpum fruits

The croton oil-induced mouse ear oedema test, acetic acid-induced abdominal writhing, and carrageenan-induced peritonitis were used to study the anti-inflammatory effects of the crude ethanol extract and its alkaloid fraction from Solanum lycocarpum fruits. The alkaloid fraction induced a dose-dependent reduction in ear oedema formation and leukocyte migration, suggesting that S. lycocarpum fruits may contain steroidal alkaloids accounting for the anti-inflammatory effect of the crude ethanol extract.