卡瓦胡椒的医药用途

卡瓦胡椒含有多种内酯成分,具有抗痉挛、抗颠痫、局部麻醉、抗炎及抑制真菌等多种生理药理效应。临床上用于治疗精神抑郁症、神经衰弱、多发性关节炎、疼痛、消化不良等。并可能用作毒品替代物,但无成瘾性。     

卡瓦胡椒的医药用途

卡瓦胡椒含有多种内酯成分,具有抗痉挛、抗癫痫、局部麻醉、抗炎及抑制真菌等多种生理药理效应.临床上用于治疗精神抑郁症、神经衰弱、多发性关节炎、疼痛、消化不良等.并可能用作毒品替代物,但无成瘾性.     

卡瓦胡椒提取物和卡瓦内酯对细胞色素P4503A4的抑制作用

由于卡瓦胡椒Piper methysticaum存在肝毒性,该植物制品最近已从德国市场撤消,但其肝毒性的原因尚不清楚。鉴于细胞色素P450酶在肝代谢和清除外来抗生素中起重要作用,作者研究了该植物提取物对细胞色素P450 3A4(CYP3A4)的影响。     

HPLC法测定卡瓦胡椒内酯的含量

目的 :建立测定 6种卡瓦胡椒内酯含量的HPLC法。方法 :采用硅胶色谱柱 ( 15cm× 3 9mm ,4μm) ,以正已烷 二烷( 82∶18,V/V)为流动相测定。结果 :去甲氧基醉椒素、二氢醉椒素、甲氧基醉椒素、醉椒素、二氢麻醉椒苦素、麻醉椒苦素 6种内酯依次在 0 10 4～ 2 0 8,0 10 9～ 2 18,0 117～ 2 3 4,0 12 6～ 2 5 2 ,0 10 2～ 2 0 4,0 113～ 0 2 6μg·mL-1范围内呈良好线性。加样回收率分别为 97 7% (RSD =1 6% ) ;99 0 % (RSD =1 9% ) ;96 8% (RSD =0 9% ) ;98 8% (RSD =1 0 % ) ;97 5 % (RSD =1 9% ) ;98 3 % (RSD =1 7% )。结论 :本方法可用于含卡瓦胡椒内酯药物的含量测定及质量控制     

药食两用植物卡瓦胡椒

卡瓦胡椒（Piper methysticum Forst）是胡椒科多年生直立灌木类药用植物，产于南太平洋诸岛，野生或栽培，根和根茎入药，有效部位为脂溶性树脂部分。卡瓦胡椒的主要药效成分是卡瓦内酯（Kavalactones）、麻醉椒碱、醉椒素（Kawain）等，能够双向调节神经递质，具有抗焦虑和抑郁、镇静催眠、局部麻醉、抗惊厥等多种作用，且未观察到药物依赖性。早在1990年，德国联邦卫生局就批准卡瓦胡椒用于治疗焦虑症，目前英国将其收入《植物药典》，美国将其收入新版《美国药典》，欧美许多国家将卡瓦胡椒列为非处方药或处方药。     

卡瓦胡椒的安全性遭受质疑

继广防己和关木通导致肾毒案之后,卡瓦胡椒的安全问题再次引起了世界的关注。数十例肝毒性报告导致欧美很多国家政府采取了断然措施,或暂停销售或干脆取缔,尽管权威科学家们认为卡瓦胡椒与肝毒性间的因果关系证据不足。本文将这一事件的起因、各国政府的对策和权威专家的观点呈献给读者,旨在引起国内消费者、生产者、药品监督管理部门和医生的关注或采取应对措施。     

天然抗焦虑药卡瓦胡椒的研究进展

目前草药疗法已在世界各国比较流行。欧亚许多国家用多种草药制成补充物投入市场,并进行了大量研究;据统计,在美国大约有500万人服用各种草药制成的补充物。胡椒科植物卡瓦胡椒具有抗焦虑、镇静催眠、局部麻醉、抗惊厥等作用,且未观察到药物依赖性等优点而在欧洲和美国临床应用。1990年,德国联邦卫生局批准卡瓦胡椒治疗焦虑症。本文介绍卡瓦胡椒的化学成分、临床前药理学研究、临床研究和药物耐受性及不良反应等研究进展。     

卡瓦胡椒提取物对经“群居-隔离-抑郁”处理后小鸡的抗焦虑作用

卡瓦胡椒Pipper methysticum提取物的抗焦虑作用是否与其总卡瓦内酯含量或其中1种或多种主要的卡瓦内酯类成分有关还不清楚。作者采用小鸡抗焦虑筛选模型——“群居-隔离-抑郁”进行了3个试验：1)4个卡瓦胡椒提取物(卡瓦内酯含量分别为12．8％、21.1％、53．2％和100．0％)或赋形剂给隔离     

卡瓦胡椒对c-DNA已表达的细胞色素P450酶及低温贮存的人肝细胞的影响

有研究显示卡瓦胡椒Piper methysticum Forster f．中的几种化合物对P450酶显示强抑制作用,并可能通过其活性代谢物的生成产生致死性肝毒性。作者研究了该植物根乙醇提取物及3种卡瓦内酯类成分醉人素（methysticin）、去甲氧基麻醉椒素（desmethoxyyangonin）和麻醉椒素（yangonin）体外对在杆状病毒／昆虫细胞系（重组CYPs）和低温保存的人肝细胞中已表达的P450酶活性的抑制作用。     

Three new kavalactone dimers from Piper methysticum (kava)

Abstract

Three new dimeric kavalactones, designated as diyangonins A–C (1–3), along with two known analogs were isolated from the roots of Piper methysticum. Their structures were elucidated by means of extensive analysis of their 1D, 2D NMR, and mass spectroscopic data. All these dimers possess a skeleton featuring a cyclobutane ring connecting two kavalactone units in head-to-tail or head-to-head mode. Compounds 1–5 were evaluated for their cytotoxic activities against human tumor cell lines.     

Safety review of kava (Piper methysticum) by the Natural Standard Research Collaboration

This systematic review discusses the proposed uses, dosing parameters, adverse effects, toxicology, interactions and mechanism of action of kava. The widespread concern regarding the potential hepatotoxicity of kava is discussed. A recommendation is made to consolidate and analyse available reports and to continue postmarket surveillance in an international repository to prevent duplicates and promote collection of thorough details at the time of each report so that any association with kava is clearly defined.     

Anxiolytic effects of kava extract and kavalactones in the chick social separation-stress paradigm

RATIONALE: Piper methysticum extract (kava kava) possesses numerous therapeutic properties, but it is unknown which of its principle constituents (kavalactones) subserve such effects. OBJECTIVES: This experiment sought to characterize the putative anxiolytic properties of P. methysticum extract and its six principle kavalactones in the chick social separation-stress paradigm. METHODS: Eight-day-old chicks received intraperitoneal injections of either vehicle, chlordiazepoxide (5.0 mg/ml per kg), P. methysticum extract (containing 30% kavalactones), kavain, dihydrokavain, methysticin, dihydromethysticin, yangonin, or desmethoxyyangonin (30 mg/ml per kg for kava compounds) 30 min prior to being tested in the presence of two conspecifics or in isolation for a 3-min observation period. Latency to adopt a ventral recumbent posture to index sedation, number of vocalizations to index separation distress, and a composite pain score (in response to 50 microliters 0.10% formalin injection into the plantar surface of the foot) to index stress-induced analgesia served as dependent measures. RESULTS: Both chlordiazepoxide and P. methysticum extract attenuated separation-induced distress vocalizations and stress-induced analgesia. Dihydrokavain attenuated separation-induced distress vocalizations. CONCLUSIONS: These findings suggest that the anxiolytic effects of P. methysticum extract may be mediated, in part, by dihydrokavain.     

品管圈在护理工作中的应用效果评价

目的探讨品管圈在护理工作中的应用效果。方法采用发放问卷调查的方式来调查在开展"品管圈"活动的前后对泌尿外科患者留置导尿管感染率、病房红灯率、护理操作正确率、患者对护理工作的满意度以及患者的生活质量进行对比。结果 "品管圈"活动实施之前留置导尿管感染率、病房红灯率、护理操作正确率、患者对护理工作的满意度分别为22.50%、23.75%、67.50%、73.75%,实施后分别为6.25%、8.75%、97.50%、91.25%,二者差异具有统计学意义(P<0.05);根据QLQC-30生活质量评分标准,实施前后患者生活质量各指标评分均具有统计学差异(P<0.05,P<0.01)。结论品管圈活动能够明显降低留置导尿管感染率与病房红灯率,以及护理操作的正确率、患者对护理工作的满意度以及患者的生活质量等,应在临床护理中加以推广并应用。     

虎杖及其化学成分的质量控制

虎杖为中国传统中草药,已在多种中药制剂中应用,临床用途广泛,含有多种活性药理成分。根据有关文献,对虎杖及其质量控制状况作一综述,为其进一步研究及开发利用提供依据。     

Interaction of various Piper methysticum cultivars with CNS receptors in vitro.

Methanolic leaf and root extracts of the Hawaiian kava (Piper methysticum Forst.) cultivars, Mahakea, Nene, Purple Moi and PNG, were tested on binding affinities to CNS receptors including GABAA (GABA and benzodiazepine binding site), dopamine D2, opioid (mu and delta), serotonin (5-HT6 and 5-HT7) and histamine (H1 and H2). HPLC analysis was carried out in order to determine the amount of the main kavalactones kavain, 7,8-dihydrokavain, methysticin, 7,8-dihydromethysticin, yangonin and 5,6-demethoxyyangonin. The most potent binding inhibition was observed for leaf extracts to GABAA receptors (GABA binding site) with IC50 values of approximately 3 micrograms/ml, whereas root extracts were less active with IC50 values ranging from 5 micrograms/ml (Nene) to 87 micrograms/ml (Mahakea). Since the leaf extracts generally contained lower amounts of the kavalactones than the root extracts, there might exist additional substances responsible for these activities. Leaf extracts also inhibited binding to dopamine D2, opioid (mu and delta) and histamine (H1 and H2) receptors more potently than the corresponding root extracts with IC50 values ranging from 1 to 100 micrograms/ml vs. > or = 100 micrograms/l, respectively. Significant differences in the potential of binding inhibition were also observed between cultivars. Binding to serotonin (5-HT6 and 5-HT7) and benzodiazepine receptors was only weakly inhibited by both root and leaf extracts of all four cultivars. In conclusion, our investigation indicates that the GABAA, dopamine D2, opioid (mu and delta) and histamine (H1 and H2) receptors might be involved in the pharmacological action of kava extracts. Since the cultivars contained similar amounts of kavalactones, while their pharmacological activities differed markedly, other constituents may play a role in the observed activities. Additionally, leaves generally exhibited more potent binding inhibition than roots, therefore leaf of P. methysticum might be an interesting subject for further pharmacological studies.     

荜茇中胡椒碱提取工艺研究

目的:研究荜茇中胡椒碱的提取工艺。方法:以胡椒碱含量及其提取率为指标,比较不同提取方法对其的影响;采用均匀试验优选最佳提取工艺。结果:采用超临界CO2萃取法提取到的胡椒碱的含量及其提取率最高;最佳提取工艺为萃取压力27.5MPa,萃取温度50℃,解析压力6MPa,解析温度50℃,夹带剂为50%药材量的乙醇,动态萃取4h。结论:该提取工艺合理、可行,可为含荜茇制剂的工业化生产提供试验依据。