Determination of Benzoylaconitine Compounds in the Decoctions of Aconiti Lateralis Radix Praeparata(Heishun Pieces),Trichosanthis Fructus and Their Combination

[Objectives]This study was conducted to determine the contents of benzoylmesaconine,benzoylaconitine and benzoylhypacoitine in the decoctions of Heishun pieces,Trichosanthis Fructus and their combination.[Methods]Heishun pieces,Trichosanthis Fructus and their combination were extracted for different time periods,and then grouped.HPLC was performed using an Agilent ZORBAX SB-C 18 chromatographic column(4.6 mm×250 mm,5μm)and acetonitrile-0.02 mol/L sodium dihydrogen phosphate as the mobile phase at a flow rate of 1 mL/min and a column temperature of 30℃,and the sample volume was 20μL.The detection wavelength was 230 nm.[Results]The total amounts of benzoylmesaconine,benzoylaconitine and benzoylhypacoitine in the single decoction group of Heishun pieces were all significantly different from those in the combined decoction group at corresponding time.[Conclusions]The total content of the benzoylaconitine type increased significantly after the combined decoction of Heishun pieces and Fructus Trichosanthis,which proves the scientificity of"eighteen incompatible medicaments,19 counteraction"in traditional Chinese medicine to some extent.

Advances in Research of Anti-tumor Effect of Aconiti Radix

In this paper,the anti-tumor effects of Aconiti Radix were reviewed and summarized,and the clinical feasibility of Aconiti Radix as a potential anti-tumor drug was analyzed,in order to provide a useful reference for the future research and development of new anti-cancer drugs of Aconiti Radix.

Research progress on synergetic effects of Fuzi(Radix Aconiti Lateralis Preparata)and Tubeimu(Rhizoma Bolbostemmatis)/Gualou(Trichosanthes kirilowii Maxim)

The compatibility of Chinese herbs is the focus and the difficulty in traditional Chinese medicine research,and it has an important guiding role for clinical medicine.Some scholars believe that the Fuzi(Radix Aconiti Lateralis Preparata,FZ)compatibility with Tubeimu(Rhizoma Bolbostemmatis,TBM)/Gualou(Trichosanthes kirilowii Maxim,GL)does not meet the Chinese medicine theory of“eighteen incompatibilities”.However,this combination has been used many times in many clinical medications.This study reviewed the research progress of pharmacological effects of FZ,and FZ compatibility with TBM/GL,in order to correctly understand and apply the“eighteen incompatibilities”drugs,and provide a reference for further exploration of the combined application in clinical treatment.

Study on Processing Technology for Aconiti Kusnezoffii Radix by Bean Curd

[Objectives] The aim was to explore the best parameters for processing Aconiti Kusnezoffii Radix by bean curd. [Methods] Orthogonal test( L_(16)(4~3)) was designed to investigate the optimal soaking time,decocting time and bean curd proportion for processing Aconiti Kusnezoffii Radix by bean curd. The contents of monoester alkaloids and diester-alkaloids were measured as the evaluation indexes. [Results]The contents of monoester alkaloids were 0. 11%,0. 07%,0. 062% and 0. 048% respectively under the four levels of soaking time,were0. 081%,0. 066%,0. 074% and 0. 067% respectively under the four levels of decocting time,and were 0. 070%,0. 072%,0. 080% and0. 073% respectively under the four levels of bean curd proportion. The content of diester-alkaloids was all below 0. 034%. The influence intensity of the three factors on the content of monoester alkaloids ranked as soaking time > decocting time > bean curd proportion. Under any of the above conditions,the content of diester-alkaloids was below the limit of Chinese Pharmacopoeia. The content of diester-alkaloids was reduced obviously with the increased use of bean curd. [Conclusions] The optimum processing conditions for Aconiti Kusnezoffii Radix were A_3B_3C_2,i. e.,soaking time of 6 d,decocting time of 5 h and bean curd proportion of 25%.

Optimization of the Ethanol Extraction Method of Monoester Alkaloids from Radix Aconiti Preparata Based on HPLC-MS and Orthogonal Test

[Objectives] This study was conducted to optimize the ethanol extraction technology of monoester alkaloids from Radix Aconiti Preparata. [Methods]On the basis of defined extraction times,ethanol concentration,ethanol times and extraction time were investigated by HPLC-MS combined with orthogonal test to optimize extraction process using the content of monoester alkaloids( the sum of benzoyl neoaconitine,benzoyl hypoaconitine and benzoyl aconitine) as an index.[Results]The optimum ethanol extraction technology was as follows: 75% ethanol,ethanol amount 25 times of the medicinal material,and each extraction for 1. 5 h.[Conclusions] The optimal extraction technology is simple,feasible,stable and reliable. It can provide reference for the industrial production and quality control of monoester alkaloids from Radix Aconiti Preparata.

Research Progress in Toxicity and Toxicity-reducing and Efficacy-enhancing Compatibility of Radix Aconiti Lateralis Praeparata

Radix Aconiti Lateralis Praeparata contains alkaloids,flavonoids,polysaccharides,organic acids and organic alkalis,among which diester alkaloids are important effective ingredients,which can be used for treating heart failure,rheumatic heart disease,coronary heart disease,hypotension,shock and other diseases.However,it also contains the main ingredients that produce toxic effects and are highly toxic to the cardiovascular system,nervous system,digestive system,reproductive system,embryos,and livers and kidneys.In this study,we analyzed the toxicity-reducing and efficacy-enhancing effects of the compatibility of Radix Aconiti Lateralis Praeparata with with single herbs Glycyrrhiza uralensis Fisch.,Panax ginseng C.A.Meyer,Zingiber ojjicinale Rosc.and Rheum palmatum L.,aiming to provide references for further exploring the appropriate compatibility conditions of traditional Chinese medicine in the future and improving the safety of the clinical application of Radix Aconiti Lateralis Praeparata.

Energy pharmacology of aconite(Radix aconiti lateralis reparata)

Objective:To study the energy pharmacology of aconite(Radix aconiti lateralis reparata).Methods:Literature induction method was applied to study the energy properties,energy pharmacological connotation,and energy pharmacological effects of aconite(Radix aconiti lateralis reparata).Results:The warm and hot properties of aconite(Radix aconiti lateralis reparata)are exactly its energy properties.The energy pharmacology of aconite(Radix aconiti lateralis reparata)is based on its energy properties,which is different from the modern aconite(Radix aconiti lateralis reparata)pharmacology that is based on the chemical composition of aconite(Radix aconiti lateralis reparata).In addition,the energy pharmacology of aconite(Radix aconiti lateralis reparata)includes not only the traditional energy pharmacology but also the modern energy pharmacology of aconite(Radix aconiti lateralis reparata).The traditional energy pharmacology of aconite(Radix aconiti lateralis reparata)is mainly manifested as the energy effect of aconite(Radix aconiti lateralis reparata)at the whole-body level,warm yang and dissipate cold,whereas the modern energy pharmacology of aconite(Radix aconiti lateralis reparata)is manifested as the physiological and pathological energy effect of warm and thermal energy properties of aconite(Radix aconiti lateralis reparata)at the tissue,cellular,and molecular levels of the body,mainly strengthening the heart,protecting cardiac muscles,dilating blood vessels,and having anti-arrhythmia,anti-shock,anti-inflammatory,analgesic,and antineoplastic effects.The traditional energy pharmacology and modern energy pharmacology of aconite(Radix aconiti lateralis reparata)constitute the basic connotation of aconite(Radix aconiti lateralis reparata)energy pharmacology.For the aconite(Radix aconiti lateralis reparata)energy pharmacology,there is a substantial foundation,its chemical components such as alkaloids.In addition,the toxicity of aconite(Radix aconiti lateralis reparata)is a manifestation of its energy pharmacology.Conclusion:aconite(Radix aconiti lateralis reparata)has energy properties that have substantial foundation.The energy pharmacology of aconite(Radix aconiti lateralis reparata)is based on its high energy and hot properties and includes the traditional energy pharmacology and modern energy pharmacology of aconite(Radix aconiti lateralis reparata).

Comparative study of anti-inflammatory effects of different processed products through the COX-2/PGE2 signaling pathway: based on network pharmacology and molecular docking

Background:Radix Aconiti Lateralis Preparata(Fu-zi)is a traditional Chinese medicinal herb,which has been widely used in the clinic and has potent anti-inflammatory activities.we aimed to explore the mechanisms of extract containing alkaloids from different Fu-zi Processed Products(FPP)in treating inflammation,especially rheumatoid arthritis(RA).Methods:Firstly,using network pharmacology technology,the ingredients,and targets of Fu-zi were obtained by searching and screening,the targets involving RA were acquired,the intersection targets were constructed a"component-target-pathway"network.A comprehensive investigation was conducted on the anti-rheumatoid arthritis mechanisms of 5 FPPs in lipopolysaccharide(LPS)induced RAW264.7 cells,which serve as a model for RA.The production of NO and inflammatory cytokines were measured by ELISA kit.Quantitative Real-time PCR(qRT-PCR)was utilized to measure the mRNA levels.COX-2/PGE2 signaling pathway-associated proteins were determined by western blot.Results:According to a network pharmacological study,16 chemical components and 43 common targets were found in Fu-zi and 6 key targets including PTGS2 were closely related to the mechanism of Fu-zi in treating RA.The in vitro study revealed that the levels of NO,TNF-α,and IL-1βwere substantially decreased by the 5 FPPs.The 5 FPPs significantly suppressed the expression of proteins COX-2,iNOS,and NF-κB,with particularly notable effects observed for PFZ and XFZ.Conclusion:Altogether,these results demonstrated that the 5 PPS containing alkaloids have a good anti-RA-related inflammatory effect,and the mechanism may be related to COX-2/PGE2 signaling pathway,particularly,Fu-zi prepared utilizing a traditional Chinese technique.

SCX-SPE结合UHPLC-Q-Exactive Orbitrap MS分析草乌中的四类二萜生物碱

目的对草乌中的二萜生物碱进行表征分析。方法以强酸性阳离子交换树脂固相萃取(SCX-SPE)分离纯化草乌中的二萜生物碱,并结合超高效液相色谱串联四极杆静电场轨道阱质谱(UHPLC-Q-Exactive Orbitrap MS)进行结构鉴定。结果结合精确分子质量、多级质谱裂解规律、对照品对比、Clog P值及文献报道,共从草乌中鉴定了99个二萜生物碱类成分,包括双酯型二萜生物碱(DDA)27个,单酯型二萜生物碱(MDA)29个,酰胺型二萜生物碱(ADA)40个,多酯型二萜生物碱(PDA)2个,以及长链型二萜生物碱(LDA)1个。结论本文所建立的SCX-SPE结合UHPLC-Q-Exactive Orbitrap MS方法能快速地鉴定草乌中的二萜生物碱类成分,可为草乌的药效物质基础及质量控制研究提供科学依据。

陕产附子炮制前后急性毒性及强心作用研究

目的:考察陕产附子炮制前后的急性毒性和强心作用。方法:通过对生附子LD_(50)的测定和自制黑顺片最大耐受量实验比较生附子和自制黑顺片的急性毒性;通过复制慢性心衰大鼠模型,检测大鼠体质量、心脏指数、血流动力学指标,检测血清BNP及cTnI含量以及组织病理学检查比较其强心作用。结果:生附子的半数致死量(LD_(50))为9.45 g/kg,黑顺片的最大耐受量为27.39 g/kg,经炮制后毒性降低。与模型组相比,自制黑顺片组大鼠症状及体征均有改善,能够降低心脏指数、左心室指数降低和左心室舒张压(LVEDP),升高左心室收缩压(LVSP)、收缩期左心室内压上升最大变化速率(+dp/dt_(max))和舒张期左心室内压下降最大变化速率(-dp/dt_(max))(P<0.05,P<0.01);降低血清中脑钠肽(BNP)、心肌肌钙蛋白I(cTnI)含量(P<0.05);心肌纤维排列相对紧密,胞核清晰可见,但有一定断裂,其中有少量空泡存在,未发现炎性细胞浸润,各指标有明显差异。生附子组各指标有一定程度的改善,但差异无统计学意义(P>0.05)。结论:生附子经炮制后,毒性降低,起到减毒的作用;自制黑顺片较生附子强心作用有显著增强。

王世强运用小青龙汤加附子或石膏经验介绍

介绍王世强教授化裁运用小青龙汤加附子或石膏的临床经验。王世强教授认为小青龙汤证之根结在于“水气”,即水液代谢失常。治疗小青龙汤证,就是“治水”,即“青龙治水”,让“水气”从体内排出。方法无外乎使寒化之水气温热蒸腾,因汗而出,即小青龙汤加附子;热化之水气遇寒,凝结成有形之水从小便排出,即小青龙汤加石膏;三焦阳气不足,气化无力,体内水气又出现热化之象,需在用附子温肾阳助小青龙汤温通三焦之时,再使热化之水气遇寒凝结成有形之水从小便而出,即小青龙汤加附子、石膏。

草乌致大鼠肝肾亚急性毒性的代谢组学研究

目的基于代谢组学技术分析和探讨草乌致大鼠肝肾亚急性毒性的生物标志物和可能的作用机制。方法以草乌为示例药物,以大鼠为研究对象,除正常组外,给药组灌胃相应溶液,连续给予28 d。通过代谢组学技术对采集的大鼠血清、肝、肾样本进行检测,用主成分分析结合偏最小二乘判别分析筛选肝肾亚急性毒性敏感标志物及代谢通路。结果代谢组学分析显示,与正常组比较,草乌组血清、肝、肾样本中分别鉴定得到34、23和30个差异代谢物,主要富集于ABC转运蛋白、精氨酸和脯氨酸代谢、癌症的中心碳代谢、烟酸和烟酰胺代谢等通路。结论初步认为草乌通过影响ABC转运蛋白、精氨酸和脯氨酸代谢、癌症的中心碳代谢等对肝肾造成损伤,亚精胺、羟脯氨酸、葡萄糖、L-亮氨酸和尿素可作为潜在的肝肾毒性敏感生物标志物。

关白附炮制前后对缺血性中风沙鼠药效学和代谢组学的影响

目的研究关白附生品及其炮制品对沙鼠缺血性脑中风的保护作用及对尿液代谢物的影响。方法将36只沙鼠随机分成空白组(CG)、模型组(MG)、阳性药组(PG)、生关白附组(RA)、蒸关白附组(SA)和姜矾制关白附组(GA),每组6只,除空白组沙鼠外,其余各组采用右侧单侧结扎沙鼠颈动脉造成中风模型。造模成功后,关白附给药组分别灌胃对应的饮片全粉混悬液(0.586 mg/g),阳性药组灌胃脑络通颗粒混悬液(0.390 mg/g),空白组灌胃生理盐水,共给药14 d。分别采用Longa评分法、氯化三苯基四氮唑(TTC)染色法、酶联免疫法检测关白附生品及其炮制品对神经功能学评分、脑组织梗死面积、氧化应激水平、炎症因子表达;采用超高效液相色谱-四极杆/静电场轨道阱高分辨质谱法(UHPLC-Q-Orbitrap-MS)分析空白组、模型组、阳性药组、生关白附组、蒸关白附组和姜矾制关白附组沙鼠尿液样品;采用多元统计方法对数据进行处理,筛选差异代谢物;采用京都基因与基因组百科全书(KEGG)数据库结合MetaboAnalyst 5.0软件对筛选出的差异代谢物进行代谢通路分析。结果关白附及其炮制品可显著改善脑组织梗死面积;明显降低脑组织和血清中丙二醛(MDA),白细胞介素-6(IL-6)和肿瘤坏死因子-α(TNF-α)活性(P<0.05),明显升高超氧化物歧化酶(SOD)、谷胱甘肽(GSH)、一氧化氮(NO)活性(P<0.05);代谢组学研究发现L-脯氨酸(L-Proline)、核黄素(Riboflavin)、白三烯D4(Leukotriene D4)、7-甲基黄嘌呤(7-Methylxanthine)等112种差异代谢物可作为缺血性脑中风潜在生物标志物,涉及核黄素代谢、嘧啶代谢、嘌呤代谢等14条代谢通路。生关白附回调了其中的核黄素代谢、嘧啶代谢等4条代谢通路;蒸关白附回调了其中的核黄素代谢、嘧啶代谢、精氨酸和脯氨酸代谢等5条代谢通路;姜矾制关白附回调了其中的咖啡因代谢和乙醛和二羧酸代谢2条代谢通路。结论通过比较药效学实验结果发现蒸制关白附效果较好,并明确了生品和炮制品对缺血性脑中风潜在生物标志物调节作用的异同。

草乌炮制研究概况

乌头类中药草乌是我国广泛使用的毒性药材,性热有大毒,归心、肝、脾、肾经,具有祛风散寒、温经止痛等功效。草乌毒性主要表现为可引发心律失常的心肌毒性,伴有心脏血管系统异常等问题,中毒严重时可导致死亡。因其毒性剧烈,乌头类药材生品不入药使用,需经炮制后入药。草乌炮制方法并无统一标准,差异表现在药材前期处理、蒸煮工艺、辅料选择等方面。本文对草乌毒性研究进展及炮制方法沿革进行归纳,为今后草乌的炮制方法等研究提供参考。

诃子在藏药炮制中的应用

通过查阅近年来国内外文献,归纳、分析了诃子在藏药炮制中的应用以及诃子炮制一些矿物药和有毒植物药过程的研究进展,根据诃子化学成分推测诃子炮制铁粉、草乌的原理及减毒机制,为进一步深入探讨藏药诃子炮制矿物药、有毒植物药的机制提供参考。

附子及其药对治疗慢性心力衰竭研究进展

慢性心力衰竭(CHF)是多种心血管疾病的终末阶段。中医认为CHF多属本虚标实,病机关键是心肾阳虚。心气虚日久累及心阳,心阳虚贯穿整个病理过程;辨证可分为阳虚血瘀证、阳虚水泛证、心肾阳虚证、阳气虚脱证;治则重在益气温阳。附子为温阳要药,药性刚燥,走而不守,上助心阳以通脉,故在使用温阳法治疗CHF时,多取附子,回阳救逆,常配伍人参、黄芪、干姜、桂枝、甘草等增强补阳功效。本文查阅近年相关文献,重点综述附子及其常用药对治疗CHF的临床应用及机制研究进展,并分析现代医家治疗CHF的临证经验,以期为中医临床治疗CHF提供指导和帮助。

Identification of Xunxi Shujin Decoction by TLC

[Objectives]To establish a TLC qualitative method for the determination of Radix Aconiti,Radix Aconiti Kusnezoffii,Caesalpinia sappan L.and Radix zanthoxyli.[Methods]TLC was used to study the quality of Radix Aconiti,Radix Aconiti Kusnezoffii and C.sappan L.in Xunxi Shujin Decoction,and the influencing factors were investigated to optimize the TLC conditions.[Results]In the TLC identification test of Radix Aconiti,Radix Aconiti Kusnezoffii,C.sappan L.and R.zanthoxyli in Xunxi Shujin Decoction,the spots were clear,the resolution was good,the specific value was moderate,the negative control was not disturbed,and the specificity was strong.[Conclusions]The established TLC method was simple,specific and reproducible,and could be used for the quality control of Xunxi Shujin Decoction.

从古今角度探析半夏附子配伍应用

“半夏反附子”历来是多数医者谨守的一条中药配伍禁忌,但随着临床实践的验证,一些医者对半夏附子不可配伍的态度也逐渐有了改变,历代医家使用半夏附子药对治疗顽疾的医案不胜枚举。中医药学界经过长年累月的研究,改良了附子的品种和改变了附子的品性,使得附子烈性减缓,毒性减弱;此外,饮片炮制技术的改进以及减毒中药的配伍应用,使得半夏附子配伍变得更加具备可能性与安全性。半夏附子配伍时需注意煎煮时间、剂量与比例等用药安全性因素。医者结合众多医家的用药经验,抓住“阳虚”及“湿盛”的核心病机,在脾胃、肾系、癌痛、妇科、心系、肺系等各系病症中配伍半夏附子均有不错的疗效。本文旨在拓宽临床用药思路,提高临床疗效,并为附子半夏药对临床应用及相关法律法规的修订提供理论依据。

淡附片标准汤剂质量标准研究

目的制备淡附片标准汤剂,进行含量测定及指纹图谱分析。方法制备15批淡附片标准汤剂,通过检测单酯型生物碱的含量计算其转移率;采用HPLC建立淡附片标准汤剂指纹图谱,计算指纹图谱相似度。结果15批淡附片标准汤剂的单酯型生物碱转移率为56.93%~94.06%,平均转移率为78.03%。经HPLC指纹图谱分析,发现共有峰9个,确认其中3个;15批淡附片标准汤剂的指纹图谱与对照指纹图谱相似度均大于0.95。结论本研究建立了淡附片标准汤剂HPLC含量测定和指纹图谱分析方法,可为淡附片中药配方颗粒的质量控制提供参考。

川乌水提取物及其单体成分对金黄色葡萄球菌α-溶血素分泌的抑制作用

目的探讨川乌水提取物及其单体成分对金黄色葡萄球菌α-溶血素分泌的抑制作用。方法采用转录组测序技术(RNAseq)分析川乌水提取物对金黄色葡萄球菌USA300 hla,psma,isda基因转录水平的影响。采用反转录-实时荧光定量聚合酶链式反应(RT-qPCR)法测定川乌水提取物及质量浓度分别为0.01,0.1,1 mg/mL的乌头原碱、次乌头碱、新乌头碱单体成分对hla,psma,isda基因表达水平的影响,采用溶血定量试验考察溶血活性。采用免疫印迹(Western blot)法考察质量浓度分别为0.01,0.1,1 mg/mL的乌头原碱、次乌头碱、新乌头碱单体成分对金黄色葡萄球菌菌液上清液中α-溶血素分泌的影响。结果USA300经250 mg/mL川乌水提取物处理后,α-溶血素、δ-溶血素、酚溶性调节蛋白等毒力因子相关基因的表达均显著下调(P<0.005)。USA300经250 mg/mL川乌水提取物及1 mg/mL乌头原碱、次乌头碱、新乌头碱单体成分处理后,hla,psma,isda基因转录水平均受到显著抑制(P<0.05),其中对hla基因的抑制作用最显著;金黄色葡萄球菌的溶血活性均受到显著抑制(P<0.01)。USA300经0.01,0.1,1 mg/mL乌头原碱、次乌头碱、新乌头碱单体成分处理后,金黄色葡萄球菌菌液上清液中α-溶血素分泌量与乌头原碱呈浓度依赖性降低,但经次乌头碱、新乌头碱单体成分处理后的趋势不明显。结论川乌水提取物及其单体成分可抑制金黄色葡萄球菌中α-溶血素的分泌,尤其是单体成分乌头原碱有用于抗金黄色葡萄球菌感染的潜能。