荜茇及其有效成分降脂抗动脉粥样硬化研究概况

本文综述了国内外有关荜茇及其有效成分的降脂、抗动脉粥样硬化方面的研究进展,并结合本课题组的研究结果,认为荜茇及其有效成分胡椒碱、荜茇宁等具有显著的降血脂作用,特别是荜茇宁不仅降脂、抗动脉粥样硬化作用显著,而且毒性极低,是极具开发前景的降脂化合物.荜茇宁的作用机制可能是通过提高高脂血症大鼠肝脏LDLR基因表达,降低ApoB基因表达而起到降脂作用;通过调节脂代谢紊乱、增强抗氧化酶类活性、减轻脂质过氧化物对血管内皮的损伤、降低主动脉LOX-1和VCAM-1基因表达起到抗动脉粥样硬化作用.     

荜茇宁降血脂和急性毒性实验研究

目的:研究荜茇宁对动物血脂的影响及急性毒性作用。方法:以大鼠食饵性高脂血症为模型,给予高脂饲料的同时灌服荜茇宁,连续14d,测定血清中总胆固醇(TC)、甘油三酯(TG)、高密度脂蛋白胆固醇(HDL-c)、低密度脂蛋白胆固醇(LDL-c)含量;采用高脂饲料喂养建立家兔高脂血症模型,观察荜茇宁对血脂、肝脏脂质和动脉粥样硬化的改善情况.通过小鼠急性毒性实验观察其对小鼠产生的毒性反应。结果:荜茇宁显著降低大鼠血清TC、TG、LDL-c和动脉硬化指数(AI),升高HDL-c的含量;能降低家兔血清TC、TG、LDL-c和肝脏TC、TG,并且显著改善动脉粥样硬化。小鼠急性限量毒性实验显示,给药后小鼠未出现死亡及毒性反应。结论:荜茇宁具有明显地降血脂和改善动脉粥样硬化作用,而且毒性极低。     

荜茇的化学成分和药理作用研究进展

综述了荜茇的主要化学成分及其提取方法,对荜茇中挥发油的清除自由基作用、不皂化物的降血压作用、对胃黏膜的保护作用、抗动脉粥样硬化作用进行了阐述。参考文献15篇。     

荜茇的药理作用与毒性作用研究概述

由于不良反应较少,中草药在人类健康中的应用越来越多。用于治疗各种疾病的传统中草药数以万计。在这些中草药中,胡椒科植物在治疗人类多种疾病中具有重要作用。荜茇作为传统中草药至今还用于治疗各类疾病如:抗癌、保肝、抗氧化、抗炎、免疫调节、扩张冠状动脉血管、抗菌、抗血小板、抗生育、抗高血脂、减肥、止痛、杀虫、辐射防护、抑制黑色素生成、保护心肌、抗抑郁、抗真菌、抗阿米巴等药理学作用。荜茇及主要有效成分胡椒碱、荜茇环碱和荜茇宁的安全性较好。本文主要综述荜茇的植物化学、药理学作用及安全性方面的研究进展。由于荜茇具有中药的商业、经济及药用价值,对荜茇的详细研究非常有意义。     

荜茇宁对家兔实验性动脉粥样硬化的影响

目的:观察荜茇宁对家兔实验性动脉粥样硬化(AS)形成的影响,并探讨其作用机制。方法:采用高脂饲料喂养建立家兔AS模型,将兔随机分为5组:正常组,模型组,荜茇宁高、低剂量组分别给予荜茇宁5,2.5 mg.kg^-1.d^-1,辛伐他汀组给予辛伐他汀5 mg.kg^-1.d-^-1,连续喂养60 d。于实验前1 d及开始后第20,40,60天取空腹血检测血清总胆固醇(TC)、甘油三酯(TG)、高密度脂蛋白胆固醇(HDL-C)、低密度脂蛋白胆固醇(LDL-C),第60天检测血清超氧化物歧化酶(SOD)活力和丙二醛(MDA)、一氧化氮(NO)含量,随后处死动物,取主动脉和心脏做病理形态学检查。结果:与模型组相比,荜茇宁组的血清TC,TG,LDL-C水平降低(P<0.05或0.01),HDL-C有升高趋势,SOD,NO升高(P<0.05),MDA降低(P<0.05)。荜茇宁组主动脉斑块面积占总面积的百分比显著低于模型组(P<0.01);主动脉、心脏损伤程度减轻,冠状动脉狭窄程度轻于模型组(P<0.01);透射电镜观察显示荜茇宁组主动脉的超微结构病变程度明显轻于模型组。结论:荜茇宁能抑制AS斑块的形成和发展,其作用机制可能与调节血脂、抗氧化有关。     

1994～2008年国内荜茇文献计量分析

目的：分析近年来国内荜茇研究的现状以及取得的进展。方法：以中国知网网络出版总库为数据库,以“荜茇”为主题词,搜索1994—2008年有关荜茇的文献,用文献计量学的方法对其年代分布、著者分布、资金资助、研究方向等情况进行统计分析。结果：搜索到有关荜茇有效成分的分析及其药理作用研究,特别是对荜茇胡椒碱、荜茇宁的研究达到了一个新的高度。结论：从文献计量学的角度客观反映了国内15年间对荜茇研究的进展,为荜茇的进一步研究提供依据。     

荜茇对大鼠寒冷型应激性胃黏膜损伤保护作用及病理改变的观察

目的：研究荜茇对大鼠寒冷型应激性胃黏膜损伤保护作用及病理性改变。方法：实验性胃损伤是将饥饿大鼠由寒冷应激造成。应激前灌服荜茇1．0g/Kg。结果荜茇可以防治大鼠胃黏膜损伤，降低胃溃疡发生率。结论：荜茇具有抗寒冷型应激实验性胃损伤作用。     

荜茇宁对高脂血症大鼠血脂代谢及其相关基因表达的影响

目的 观察荜茇宁对实验性高脂血症大鼠血脂代谢及其相关基因表达的影响.方法 饲喂高脂饲料建立高脂血症大鼠模型,荜茇宁分别按2.5、5、10 mg/kg给大鼠连续ig 4周.实验结束,取空腹血,检测血清总胆固醇(TC)、甘油三酯(TG)、高密度脂蛋白胆固醇(HDL-C)、低密度脂蛋白胆固醇(LDL-C)、载脂蛋白Al(ApoAl)、载脂蛋白B(ApoB);利用反转录聚合酶链反应(RT-PCR)测定大鼠肝脏低密度脂蛋白受体(LDLR)、ApoB和3-羟基-3-甲基-戊二酰辅酶A还原酶(HMG-CoAR)mRNA的表达.结果 与模型组相比,荜茇宁能降低血清TC、TG、LDL-C、ApoB水平及ApoB/ApoAl的值(P<0.05),升高HDL-C、ApoAl(P<0.05),能增强高脂血症大鼠LDLR mRNA表达(P<0.05),降低ApoB mRNA表达(P<0.05),但对HMG-CoAR mRNA的影响不明显(P>0.05).结论 荜茇宁具有调节高脂血症大鼠血脂代谢的作用,其机制可能与提高LDLR基因转录水平,降低ApoB mRNA表达有关.     

荜茇酰胺的药理作用研究进展

荜茇酰胺是分离自荜茇的生物碱类化合物,具有多种药理学作用,包括抗肿瘤、调节血脂代谢、抗血小板凝集、镇痛等,是一种极具药用价值的化学物质。着重就荜茇酰胺在抗肿瘤、抗血小板凝集、镇痛、抗真菌、抗血吸虫、抗焦虑以及抗抑郁等方面药理作用的研究进展进行综述。     

HPLC同时测定荜茇中胡椒碱和荜茇明宁碱含量

目的:采用HPLC同步测定荜茇中胡椒碱和荜茇明宁碱的含量,为荜茇药材多指标质量控制奠定基础.方法:以荜茇药材中胡椒碱和荜茇明宁碱为指标成分,应用C18(4.6 mm×250 mm,5μm)柱,流动相0.25％甲酸-甲醇(35∶65),流速为1 mL·min-1,检测波长343 nm,柱温40℃.结果:胡椒碱和荜茇明宁碱的峰面积与浓度的线性关系良好(r=0.999 9),平均加样回收率为100.4％,102.2％,RSD分别为2.6％,2.5％.建立了同时对荜茇中的2个成分进行定量的测定方法,并将此方法用于不同来源的荜茇各成分的测定.结论:该方法简便快捷,重复性良好,为中药材荜茇提供了更合理、可靠的质控方法.     

Overview for various aspects of the health benefits of Piper longum linn. fruit

Herbal remedies have become popular, due in part to the lower risk of adverse reactions. Thousands of plants have been used traditionally to treat various diseases. Among them, species of the genus Piper are important medicinal plants used in various systems of medicine. The Piper longum fruit has been used in traditional medicine, including the Ayurvedic system of medicine. Although there are numerous indications for its use, controlled trials are needed to determine its efficacy. The primary constituents isolated from various parts of P. longum are piperine, piperlongumine, sylvatin, sesamin, diaeudesmin piperlonguminine, pipermonaline, and piperundecalidine. It is most commonly used to treat chronic bronchitis, asthma, constipation, gonorrhea, paralysis of the tongue, diarrhea, cholera, chronic malaria, viral hepatitis, respiratory infections, stomachache, bronchitis, diseases of the spleen, cough, and tumors. This study provides detailed information about the P. longum fruit, including phytochemistry, pharmacological profile and safety profile. In view of the commercial, economic, and medicinal importance of the P. longum plant, it is useful for researchers to study the plant in detail.     

荜茇水提取物对小鼠胃排空和肠推进的影响

目的:研究荜茇水提取物对小鼠肠推进和胃排空的影响。方法:荜茇水提取物灌胃给药6天,采用小肠炭末推进实验观察荜茇水提取物对正常小鼠小肠运动及硫酸阿托品所致小鼠小肠抑制模型的影响,采用甲基橙胃残留率的方法观察荜茇水提取物对正常小鼠胃排空的影响。结果:荜茇水提取物20g/kg和10g/kg可促进正常小鼠小肠运动,并能明显拮抗硫酸阿托品所致小鼠小肠抑制作用,荜茇水提取物20g生药/kg和10g生药/kg可促进正常小鼠胃排空。结论:荜茇水提取物对正常小鼠小肠运动及硫酸阿托品所致小鼠小肠抑制均有明显促进作用,并对正常小鼠胃排空有促进作用,其机制可能与M胆碱受体有关。     

荜拔酰胺的结构修饰与生物活性研究进展

荜拔酰胺为叔胺型酰胺类生物碱,该成分主要存在于胡椒科植物长柄胡椒以及瘤突变胡椒等的根中。荜拔酰胺具有抗血小板聚集、抗炎和抗肿瘤等多种药理活性,其衍生物也具有多种多样的活性。笔者综述了荜拔酰胺的结构修饰及其生物活性的研究进展,为荜拔酰胺类化合物的进一步研究提供参考。     

胡椒、荜茇对正常大鼠肝脏能量代谢因子的影响

目的:探讨热性中药胡椒、荜茇对正常大鼠肝脏能量代谢的影响,研究热性中药对大鼠生理活动的影响,为中药药性理论研究打下基础。方法:将30只大鼠随机分为3组,空白组给予生理盐水,胡椒组给予胡椒水提取液,荜茇组给予荜茇水提液,按10 mL·kg-1的量连续灌胃30 d,分别测定肝脏能量代谢相关酶类的变化。结果:与空白组比较,胡椒组、荜茇组能显著升高Ca2+-ATP酶、Ca2+-Mg2+-ATP酶以及LDH酶的活性,同时明显降低肝糖原含量,能够明显升高大鼠单位体重摄入能、消化能和可代谢能;胡椒组与荜茇组间结果比较无明显差异。结论:热性中药胡椒、荜茇能促进肝糖原的分解,增加LDH酶、Ca2+-ATP酶、Ca2+-Mg2+-ATP酶的活性,从而增加ATP酶的消耗,同时升高大鼠单位体重摄入能、消化能和可代谢能,进而促进大鼠肝脏能量代谢。     

Antioxidant activity of a salt-spice-herbal mixture against free radical induction

A combination of spices (Piper nigrum, Piper longum and Zingiber officinale), herbs (Cyperus rotundus and Plumbago zeylanica) and salts make up Amrita Bindu. The study was focused to evaluate the antioxidant property of individual ingredients in Amrita Bindu against the free radical 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS). The analysis revealed the antioxidant potential of the ingredients in the following order: Piper nigrum>Piper longum>Cyperus rotundus>Plumbago zeylanca>Zingiber officinale. Two different experiments were designed. In experiment I, rats were fed with normal diet whereas in experiment II rats were given feed mixed with Amrita Bindu for 3 weeks (4 g/kg of feed). Rats from both experimental groups were challenged against a single intraperitonial injection of phenylhydrazine (PHZ) (7.5 mg/kg body weight). At the end of 24 and 72 h, blood was analysed for free radicals and antioxidant levels. It was interesting to note that rats with Amrita Bindu pretreatment showed significantly lower levels of free radicals, lipid peroxidation and protein carbonyls along with significantly higher levels of antioxidants when compared with rats without Amrita Bindu pretreatment on PHZ administration. These results reveal that Amrita Bindu, a salt-spice-herbal mixture exerts a promising antioxidant potential against free radical induced oxidative damage.     

Immunomodulatory and antitumor activity of Piper longum Linn. and piperine

Alcoholic extract of the fruits of the plant Piper longum and its component piperine was studied for their immunomodulatory and antitumor activity. Alcoholic extract of the fruits was 100% toxic at a concentration of 500 microg/ml to Dalton's lymphoma ascites (DLA) cells and 250 microg/ml to Ehrlich ascites carcinoma (EAC) cells. Piperine was found to be cytotoxic towards DLA and EAC cells at a concentration of 250 microg/ml. Alcoholic extract and piperine was also found to produce cytotoxicity towards L929 cells in culture at a concentration of 100 and 50 microg/ml, respectively. Administration of alcoholic extract of Piper longum (10 mg/dose/animal) as well as piperine (1.14 mg/dose/animal) could inhibit the solid tumor development in mice induced with DLA cells and increase the life span of mice bearing Ehrlich ascites carcinoma tumor to 37.3 and 58.8%, respectively. Administration of Piper longum extract and piperine increased the total WBC count to 142.8 and 138.9%, respectively, in Balb/c mice. The number of plaque forming cells also enhanced significantly by the administration of the extract (100.3%) and piperine (71.4%) on 5th day after immunization. Bone marrow cellularity and alpha-esterase positive cells were also increased by the administration of Piper longum extract and piperine.     

荜茇提取物对大鼠骨髓间质干细胞MSC的增殖作用及与化学官能团的关系

目的:观察荜茇挥发油和水溶性部分对大鼠骨髓间质干细胞(mesenchymal stem cells,MSC)体外增殖的影响,并进一步探讨了与分子中化学官能团的关系.方法:使用密度梯度法分离大鼠骨髓间质干细胞,体外培养,经Brdu标记和CD44染色及两者双重染色鉴定后,观察在培养液中添加不同浓度荜茇挥发油及其水溶性部分的条件下MSC的生长变化.应用形态学、MTT法和5-溴脱氧尿嘧啶(5-Bromodeoxyuridine,Brdu)、增殖细胞核抗原(Proliferation cellnuclear antigen,PCNA)免疫细胞化学方法测定细胞增殖活性.结果:荜茇挥发油以浓度依赖方式促进MSC增殖活力和增加Brdu、PCNA阳性细胞数,与对照组比较有显著性(P＜0.05).经GC-MS检测,荜茇挥发油含C=C(50.66%)、-OH(27.02%)、多种官能团(5.05%)等;而荜茇水提物对MSC无增殖作用.结论:荜茇挥发油明显促进MSC的增殖,这种作用可能与分子中C=C、-OH等官能团有关.     

荜茇挥发油清除自由基作用及其与分子结构的关系

目的观察海南产荜茇挥发油清除自由基活性,探讨其与分子结构的关系。方法DPPH法检测清除自由基活性;GC-MS法分析其化学成分,并用谱库检索确定各化合物结构。结果①荜茇挥发油具有清除DPPH自由基的能力,且浓度越高,活性越强;②海南产荜茇挥发油含41个化合物,碳碳双键C=C的相对含量占绝对优势。结论碳碳双键C=C可能为荜茇挥发油清除自由基活性的必需官能团。     

荜茇三氯甲烷部位化学成分研究

目的:对胡椒科植物荜茇Piper longum的化学成分进行研究.方法:荜茇用95%乙醇提取,依次用石油醚、三氯甲烷、正丁醇萃取,对三氯甲烷萃取部分采用各种柱色谱进行分离纯化,通过波谱数据分析(MS,~1H-NMR,~(13)C-NMR)进行结构鉴定.结果:从三氯甲烷萃取部分分离鉴定了13个化合物,其中6个酰胺类生物碱,3个倍半萜,4个其他类化合物.分别鉴定为:1-(3',4'-methylenedioxyphenyl)-1E-tetradecene(1),3-(3',4'-methylenedioxophenyl)-propenal(2),胡椒酸(piperoic acid,3),3',4,-dihydroxy-biabola-1,10-diene(4),eudesm-4(15)-ene-1β,6α-diol(5),7-epi-eudesm-4(15)-ene-1',6β-diol(6),几内亚胡椒胺(guineesine,7),胡椒碱(piperine,8),胡椒酰胺(pipericide,9),2E,4E-dienamide(10),(2E,4E,8E)-N-isobutylhenicosa-2,4,8-trienamide(11),荜茇明碱(piperlonguminine,12),胡椒酸甲酯(methyl piperate,13).结论:其中化合物1-6为首次从荜茇中分离得到.     

Effects of Piper longum fruit, Piper sarmentosum root and Quercus infectoria nut gall on caecal amoebiasis in mice

The anti-amoebic effects of crude methanol extracts of Piper longum fruit, Piper sarmentosum root and Quercus infectoria nut gall against Entamoeba histolytica infecting the caecum of mice were studied. Caecal amoebiasis in mice was induced by injection of Entamoeba histolytica trophozoites directly into the caecum. The mice were then treated orally with the extract, a standard drug (metronidazole), or vehicle p.o. for five consecutive days, beginning 24 h after the infection and were examined on the sixth day. At a dose of 1000 mg/kg per day, the extracts of Piper longum fruit, Piper sarmentosum root and Quercus infectoria nut gall had a curative rate of 100, 40 and 26%, respectively. At a concentration of 500 and 250 mg/kg/day, extract from Piper longum fruit was still effective in 93 and 46% of the cases, respectively, while extract from Piper sarmentosum root at a dose of less than 1000 mg/kg per day did not cure any mice from amoebiasis. Extract of Quercus infectoria nut gall at a concentration of 500 and of 250 mg/kg per day cured 26 and 13% of mice, respectively. Metronidazole at a concentration of 125 and of 62.5 mg/kg per day had a curative rate of 100 and 60%, respectively. The severity of caecal wall ulceration was reduced in mice which received the extract and metronidazole as compared to the control animals.