Pharmacokinetica studies of aristolochic acid-I and-II in rats after intragastrical administration of Radix Aristolochiae and Muskone

The pharmacokinetic parameters of aristolochic acid-Ⅰ （AA-Ⅰ） and -Ⅱ （AA-Ⅱ） in rat serum after intragastrical administration of the crude drug powders of Radix Aristolochiae （RA） and Muskone containing equal amounts of RA were compared. The pharmacokinetic profiles of AA-Ⅰ and AA-Ⅱ could be fitted with a two-compartment model The elimination half time （T1/2β） of AA-Ⅰ in Muskone was 1573.2 min and that of AA-Ⅰ in RA was 475.8 min; T1/2β of AA-Ⅱ in Muskone was 2344.8 min and that of AA-Ⅱ in RA was 427.8 rain. The area under the concentration-time curve （AUC） of AA-Ⅰ in Muskone was 13.07 μg/h/mL and that of AA-Ⅰ in RA was 3.86 μg/h/mL; AUC of AA-Ⅱ in Muskone was 67.67 μg/h/mL and that of AA-Ⅱ in RA was 23.93 μg/h/mL. The bioavailabilities of AA-Ⅰ and AA-Ⅱ in Muskone were markedly increased compared with that in RA based on the elimination half-time and A UC values.

Characterization and quantitation of aristolochic acid analogs in different parts of Aristolochiae Fructus, using UHPLC-Q/TOF-MS and UHPLC-Qq Q-MS

Aristolochiae Fructus, a Chinese herbal medicine derived from the fruit of Aristolochia contorta Bge., contains nephrotoxic aristolochic acid analogues(AAAs). According to ancient medical texts, various medicinal parts of the fruit of A. contorta were ever used. In order to reveal which part could be safely and effectively used, it is necessary to analyze the chemical profiles of different medicinal parts. Herein we compared the chemical compositions and determined aristolochic acid I(AA-I) and aristolochic acid II(AA-II) in the four parts viz. outer pericarp, inner pericarp, septum, and seed. Ultra-high performance liquid chromatography equipped with quadrupole time-of-flight mass spectrometry(UHPLC-QTOF-MS) was applied for chemical profiling. Ultra-high performance liquid coupled with triple quadrupole mass spectrometry(UHPLC-Qq Q-MS) was employed to quantify AA-I and AA-II in different parts. It was found that the chemical compositions of the four parts varied both qualitatively and quantitatively. A total of 10 AAAs, including 5 aristolochic acids and 5 aristolactams, together with 3 alkaloids, were unambiguously or tentatively identified by UHPLC-QTOF-MS. The quantitatively analytical results obtained by UHPLC-Qq Q-MS showed that AA-I and AA-II exclusively accumulate in the seeds of A. contorta. These findings provide supporting data for the rational selection of medicinal parts.

马兜铃属(Aristolochia)植物的化学成分

马兜铃属(Aristolochia)植物全世界约有200种,有37种进行过化学成分研究。自该属植物中得到并签定的化学成分有140种,分别属于马兜铃酸类及其衍生物、生物碱类、萜类及甾体化合物、黄酮类、苯丙素酚类和其它类化合物。本文介绍了这些化合物的名称、结构式及存在的植物等。重点介绍了植物界中罕见的含硝基菲类有机酸(马兜铃酸类)及其衍生物,并指出这类化合物结构规律性。在马兜铃属植物中以马兜铃酸A、B、C、D(aristolochic acid A、B、C、D)、马兜铃内酰胺(aristololactam)、木兰碱(magnoflorine)、β-谷甾醇(β-sitosterol)及尿囊素(all-antoin)分布较普遍,尤以马兜铃酸A存在最广泛。

广防己挥发油的GC-MS指纹图谱研究

防己药材主要分粉防己和木防己两类,木防己包括广防己和汉中防己.广防己为马兜铃科植物广防己Aristolochia fangchi Y.C.WuexL.D.Chou.et S.M.Hwang的干燥根[1],习称"木防己"、"水防己",主产于广东、广西,具有祛风止痛、清热利水之功效[2].……

药用植物北马兜铃的开发利用价值与栽培技术概述

根据目前国内学者的研究成果,该研究集中介绍了北马兜铃的植物学和生物学特性,种子、茎、根的主要化学成分及药用价值,总结了北马兜铃播种繁殖的栽培技术及后期田间管理、病虫害防治及采收和加工的具体方法,为今后合理开发利用这一植物资源提供理论依据。

青木香(Aristolochia debillis Sieb. et Zucc.)的抗菌活性(英文)

通过琼脂平板扩散试验和双倍稀释试验,对青木香(Aristolochia debillis Sieb. et Zucc.)的石油醚提取物、乙酸乙酯提取物和甲醇提取物进行了抗细菌和抗真菌作用的研究,在三种提取物中,只有甲醇提取物对试验的所有革兰氏阳性和革兰氏阴性细菌都表现出显著的抗菌作用,乙酸乙酯提取物只对测试的部分细菌显示出抗菌作用,石油醚提取物不具有抗菌活性.甲醇提取物比乙酸乙酯提取物具有更强的抗菌作用和更广的抗菌谱.三种提取物对所有试验的真菌都没有显示出抗菌作用.

绵毛马兜铃油的镇痛和中枢抑制作用

绵毛马兜铃〔Aristolochia mollissima ance〕为马兜铃科马兜铃属植物,药材名为寻骨风。全草入药,可祛风湿、通经络、治筋骨痛等病。马兜铃地下茎含马兜铃酸和挥发油等成分。挥发油成分复杂,已知含有马兜铃内酯、马兜铃酮等20多种成分。挥发油有较好的抗炎作用。本文对马兜铃油的镇痛作用和中枢抑制作用进行了研究。报告如下。

青木香(Aristolochia debillis Sieb.et Zucc.)的消炎和镇痛活性(英文)

目的:检测青木香(AristolochiadebillisSieb.etZucc.)的块根水提取液的消炎和镇痛效果及毒性。方法:用蛋清诱导法、热板法和扭体法。结果:青木香的块根水提取液无毒性,1000mg/kg,i.g.的青木香块根水提取液比生理盐水的消炎和镇痛效果明显,比200mg/kg,i.g.乙酰水杨酸的消炎效果好,2000mg/kg,i.g.的青木香块根水提取液比乙酰水杨酸的消炎效果更加显著。结论:青木香具有较好消炎和镇痛活性,无毒性。

四种杀虫剂防治红珠凤蝶小斑亚种的田间药效试验

研究了40%辛硫磷乳油、2%阿维菌素乳油、Bt可湿性粉剂和5%氯氰菊酯乳油4种杀虫剂对红珠凤蝶小斑亚种[Pachliopta aristolochiae adaeus(Rothschild)]的田间药效试验。结果表明,药后3 d,5%氯氰菊酯乳油防效为91.95%;药后7 d,5%氯氰菊酯乳油和40%辛硫磷乳油防效分别为95.21%和93.36%;药后10 d,5%氯氰菊酯乳油、40%辛硫磷乳油和Bt可湿性粉剂防效极显著高于2%阿维菌素乳油,分别为99.28%、98.35%、87.79%。

HPLC法测定藏药帕栗嘎不同品种及其代用品中马兜铃酸A的含量

目的:测定4种常用藏药帕栗嘎品种(藏马兜铃、Aristolochia sp.、小木通和绣球藤)中马兜铃酸A的含量,明确藏药帕栗嘎不同品种中马兜铃酸A的含量分布情况,为藏药帕栗嘎的临床安全用药提供科学依据。方法:采用高效液相色谱法(high performance liquid chromatography,HPLC),色谱柱:Thermo ODS HYPERSIL(4.6 mm×200 mm,5μm);流动相:甲醇-1.0%甲酸水溶液(70∶30);流速:1.0 mL/min;检测波长:315 nm;柱温:25℃。结果:马兜铃酸A在20~180μg有良好的线性关系;平均加样回收率为95.89%,RSD为1.26%;藏药帕栗嘎4个品种中藏马兜铃中马兜铃酸A的含量为3.5818 mg/g,Aristolochia sp.、小木通和绣球藤中未检测出马兜铃酸A。Aristolochia sp.尚无统一命名和草本考证,为本文首次提出。结论:藏马兜铃中马兜铃酸A含量较高,临床应慎用,应由功效相同而不含马兜铃酸A的“Aristolochia sp.”和毛茛科植物川木通代替。

Alkaloids from the Roots of Aristolochia Triangularis(I)

From the roots of Aristolochia triangularis, two new alkaloids triangularine A and triangularine B together with thirteen known alkaloids namely aristololactam AII, AIIIa, AIA, Ia, IIA, BII, CII, cepharadione A, 4,5 dioxodehydroasimilobine; aristolochic acid D (IVa), magnoflorine; N, N dimethyllindcarpine and oblongine were isolated, their structures were identified by means of spectral analysis and chemical conversion.

响应面法优化马兜铃药材中AAs及AL超声提取方法研究

为了探索超声提取马兜铃药材中马兜铃酸(AAs,Aristolochic Acids)及马兜铃内酰胺(AL,Aristololactam)的最佳提取工艺,通过单因素实验考察超声提取时间、超声功率、甲醇浓度、提取温度4个因素对目标化合物提取量的影响;在此基础上,采用响应面分析法对提取时间、超声功率、甲醇浓度进行优化。当液料比为20 m L/g、提取温度30℃时,优化的工艺参数为甲醇浓度(v/v)53%、提取时间59 min、超声功率85%。实验结果表明,曲面回归方程拟合性好,实验误差小,可用于马兜铃药材中AAs及AL的提取,并对马兜铃药理毒理作用的进一步研究具有重要的参考价值。

Plants as concept generators for biomimetic light-weight structures with variable stiffness and self-repair mechanisms

Plants possess many structural and functional properties that have a high potential to serve as concept generators for the production of biomimetic technical materials and structures. We present data on two features of plants (variable stiffness due to pressure changes in cellular structures and rapid self-repair functions) that may be used as models for biomimetic projects.

Genetic diversity and structure of the endemic and endangered species Aristolochia delavayi growing along the Jinsha River

The traditional medicinal plant,and endangered species Aristolochia delavayi(Aristolochiaceae)is an endemic species in China and occurs in the warm and dry areas along the Jinsha river.It is also a specific host of the larvae of Byasa daemonius,a vulnerable butterfly.In this study,15 pairs of polymorphic microsatellite primers of A.delavayi were designed and screened based on the Simple Sequence Repeats(SSR)loci found by using the results of genome skimming.Based on these 15 SSR markers,the genetic diversity and structure of 193 individuals from ten natural populations were analyzed in detail.In comparison to other endemic and endangered plants in the region,the population of A.delavayi possess a relatively high genetic diversity(He=0.550,I=1.112).AMOVA analysis showed that 68.4%of the total genetic diversity was within populations and 31.6%of the variation occurred among populations.There was a significant genetic differentiation among natural populations of A.delavayi detectable,with low gene flow(Nm=0.591).This might be attributed to geographical barriers and limited seed dispersal.To test the isolation by distance(IBD),we performed Mantel test,which showed a significant correlation between the geographic and genetic distances.In order to cope with the possible biases caused by IBD,we additionally performed Bayesian genetic cluster analyses and principal coordinate analysis(PCoA).The final cluster analysis revealed three groups with distinct geographical distribution.Habitat fragmentation and limited gene flow between these populations may be the main reasons for the current genetic structure.For conservation of this species,we suggest to divide its populations into three protection management units,with subsequent focus on the Yongsheng and Luquan populations which experienced a genetic bottleneck event in the past.

防已利尿作用初步试验

防已为常用中药,具有祛风止痛、利水消肿功效。中国药典(1977年版)收载有两类:一类为防已科植物粉防已Stephania tetrandra S Moore的根;一类为马兜铃科植物广防己Aristolochiafangch Wu的根。此外。各地使用的尚有四川的川防已、云南的理防已、陕西的汉中防已等。防已为疗风水要药,而利尿作用尚未见文献报导。我们对两个科的六个品种防已作了利尿作用初步试验,结果汇报如下。

Aristolochia gehrtii inhibits liver toxicity and apoptosis in Schistosoma malayensis infection

Objective:To evaluate a protective effect of Aristolochia gehrtii(A.gehrtii)leaves to inhibit liver toxicity and apoptosis in Schistosoma malayensis(S.malayensis)infection.Methods:Forty male albino mice were divided into four equal groups:group 1 control including noninfected healthy mice and groups 2,3&4 subcutaneously infected with S.malayensvs cercariae where groups 3&4 pretreated with A.gehrtii leaves(200 mg/kg,bwt)&cinnamoylamide(250mg/kg,bwt),respectively.Results:5.malayensis caused a significant increase in serum AST,ALT,ALP,MDA,NO,bilirubin,urea,creatinine,total cholesterol,LDL,triglycerides,and HDL levels.The pretreatment of A,gehrtii leaves and cinnamoylamide significantly inhibited that increase.On the other hand,S.malayensis induced a significant decrease in serum total protein,albumin,globulin,albumin/globulin ratio,blood SOD and GPx,while A.gehrtii leaves and cinnamoylamide pretreatment increased the above parameters.Treatment with A.gehrtii leaves and cinnamoylamide to S.malayensis infected mice increased p53 expression but decreased bcl-2expression.These results were supported by hislopalholqgical investigations.Conclusions:A.gehrtii inhibits liver toxicity and apoptosis in S.malayensvs infection and this effect is associated with the major cinnamoylamide ingredient of A.gehrtii leaves.

越南马兜铃属植物分布新记录——凹脉马兜铃（英文）

凹脉马兜铃(Aristolochia impressinervis C.F.Liang)曾被认为是中国广西的特有种。该文首次报道了越南植物区系中凹脉马兜铃的分布新纪录,并讨论了凹脉马兜铃的分类及其与A.pierrei L.的区别特征。

Evaluation of Antimycobacterial Activity of Higenamine Using Galleria mellonella as an In Vivo Infection Model

The Phytochemical investigation on MeOH extract on the bark of Aristolochia brasiliensis Mart.&Zucc(Aristolochi-aceae)led to the isolation of major compound(1)as light brown grainy crystals.The compound was identified as 1-(4-hydroxybenzyl)-1,2,3,4-tetrahydroisoquinoline-6,7-diol(higenamine)on the basis of spectroscopic analysis,including 1D and 2D NMR spectroscopy.The compound was evaluated for its antimycobacterial activity against Mycobacterium indicus pranii(MIP),using Galleria mellonella larva as an in vivo infection model.The survival of MIP infected larvae after a single dose treatment of 100 mg/kg body weight of higenamine was 80%after 24 h.Quantitatively the compound exhibited a dose dependent activity,as evidenced by the reduction of colony density from 10^(5) to 10^(3) CFU for test concentrations of 50,100,150 and 200 mg/kg body weight respectively.The IC50 value for higenamine was 161.6 mg/kg body weight as calculated from a calibration curve.Further analysis showed that,a complete inhibition of MIP in the G.mellonella could be achieved at 334 mg/kg body weight.Despite the fact that MIP has been found to be highly resistant against isoniazid(INH)in an in vitro assay model,in this study the microbe was highly susceptible to this standard anti-TB drug.The isolation of higenamine from the genus Aristolochia and the method used to evaluate its in vivo antimycobacterial activity in G.mellonella are herein reported for the first time.

Protective effects of Aristolochia longa and Aquilaria malaccensis against lead induced acute liver injury in rats

Objective: To investigate the protective effects of Aristolochia longa (A. longa) and Aquilaria malaccensis (A. malaccensis) on acute hepatotoxicity induced by lead in female albino rats. Methods: Twenty five (25) apparently healthy female Wistar rats were randomly divided into five groups of five rats in each: control, Pb, Pb + A. longa (Ar), Pb+ A. malaccensis (Aq), and Pb+ A. longa (Ar) + A. malaccensis (Aq) lead (100 mg/kg b.w.) as Pb (C2H3O2)2 added in their drinking water for 75 days. A. longa (rhizome powder at a dose of 10 g/kg of diet ) and A. malaccensis (heartwood powder at a dose 10 g/kg of diet) were added to the feed during the last 15 days of lead exposed in the animals. Results: Obtained results revealed that lead treatment caused a significant increase in serum GOT, GPT and ALP activities and in liver of MDA level and CAT activity. In contrast, it led to an decrease in the liver GOT, GPT and GST activities and in GSH level in rats. Also, the results clearly showed that lead causes alterations of hepatic tissue in comparison with controls. Our results showed that treatment with A. malaccensis and A. longa a partial correction of the previous parameters. The histological observations confirmed the hepatoprotection results by the biochemical parameters. Conclusions: Results demonstrated beneficial effects of A. longa and A. malaccensis treatment in Pb-induced oxidative stress and tissue damage in liver.

A NEW ARISTOLOCHIC ACID FROM ARISTOLOCHIA CINNABARINA

A new compound, aristolochoc acid Ⅲ a- 6-0-β-D-glucoside, was isolated along with four known compounds from Aristolochia cinnabarina. The structure of the new,compound was elucidated on the basis of spectral evidences