Chemical Composition, Larvicidal and Adult Emergence Inhibition Activities of Balanites aegyptiaca Del. Seed and Aristolochia albida Duch. Root Extracts against Malaria Vector, Anopheles gambiae Giles

Background: Anopheles gambiae is enemy number one of mankind in Africa and particularly in Cameroon due to its ability of transmitting malaria which is the deadliest disease in this part of the world. Synthetic insecticides have been used to control malaria vectors but they have negative effects on non-target organisms and are environmentally unfriendly. Control of mosquitoes at larval stages using phytochemicals is currently the leading tool to reduce the mosquito population and so the reduction of malaria transmission rates. Therefore, the present study was to evaluate the phytochemical contents, larvicidal and adult emergence inhibition activities of Balanites aegyptiaca seed and Aristolochia albida root solvents extracts against Anopheles gambiae larvae. Methods: The World Health Organization standard protocols were followed for the different bioassays. Concentrations ranging from 500 - 2000 ppm for larvicidal and 500 - 1500 ppm for IGRs were used. Results: Both plants showed the presence of alkaloids, flavonoids, saponins, tannins, phenols, terpenoids and oils except the absence of phenols in Aristolochia albida. The larvicidal activity of Aristolochia albida extracts showed that hexane and methanol fractions were the most active killing relatively all exposed larvae with the LC50 values of 420.1 and 453 ppm, respectively. The same observation was made in hexane fraction from Balanites aegyptiaca (LC50 = 588 ppm). The insect growth inhibitory activity of Aristolochia albida extracts proved that hexane and methanol fractions relatively caused a 100% inhibition in the mosquito development, recording the EI50 values of 482.4 and 555.6 ppm, respectively. The same trend was observed with Balanites aegyptiaca hexane fraction registering better EI50 of 623.9 ppm. Conclusions: Our findings demonstrate that Balanites aegyptiaca seed and Aristolochia albida seed extracts are rich in phytochemicals capable of killing mosquito larvae and disrupting mosquito larval development. This could contribute to the control of mosquito populations and improved management of malaria.

金沙江流域4种特有植物野生资源现状及受威胁等级评估

物种受威胁状况的及时评估是调整物种濒危状态,继而实施有效保护措施的重要依据。该文以金沙江流域特有植物贯叶马兜铃(Aristolochia delavayi)、旱地木槿(Hibiscus aridicola)、云南百部(Stemona mairei)和白魔芋(Amorphophallus albus)为调查评估对象,通过多年野外调查,依据《IUCN物种红色名录等级和标准:3.1版》和《使用指南:15.1版》对4物种的濒危现状进行了重新分析和评估。结果表明,在现有野生种群资源下贯叶马兜铃被列为易危(VU),旱地木槿和白魔芋被列为濒危(EN),云南百部为近危(NT)。与4物种现行濒危等级的比较表明,贯叶马兜铃的濒危等级由濒危降级为易危,旱地木槿由易危上调为濒危,白魔芋由近危上调为濒危,云南百部的濒危状态则维持不变。这为4种特有植物的野生资源现状了解、濒危状态更新以及适时调整有效保护策略提供了科学参考。

超高效液相色谱串联质谱法测定木香马兜铃中马兜铃酸Ⅰ及马兜铃酸Ⅱ的含量

目的:建立测定木香马兜铃中马兜铃酸Ⅰ(AA-Ⅰ)及AA-Ⅱ含量的超高效液相色谱-质谱法。方法:色谱柱为Agilent Poroshell SB-C18(100 mm×2.1 mm,2.7μm),流动相为乙腈-0.1%甲酸水溶液(含5 mmol·L^(–1)甲酸铵),梯度洗脱,流速0.3 mL·min^(–1),柱温35℃,离子源为电喷雾离子源,扫描方式为正离子扫描,多反应离子监测模式。结果:AA-Ⅰ在质量浓度为1.036~207.310 ng·mL^(–1)时与峰面积线性关系良好(r=0.9995);AA-Ⅱ在质量浓度为1.1~110.0 ng·mL^(–1)时与峰面积线性关系良好(r=0.9991);AA-Ⅰ的定量限、检测限分别为0.3287、0.0986 pg;AA-Ⅱ的定量限、检测限分别为0.6506、0.1952 pg;AA-Ⅰ的精密度、稳定性、重复性试验RSD均小于5.0%;AA-Ⅱ的精密度、稳定性、重复性试验RSD均小于5.0%;AA-Ⅰ的平均加样回收率为92.50%,RSD为4.3%;AA-Ⅱ的平均加样回收率为104.97%,RSD为3.7%。15批木香马兜铃药材中1批未检出AA-Ⅰ,8批未检出AA-Ⅱ,其余批次的AA-Ⅰ质量分数为5.94×10^(–4)~2.86 mg·g^(–1),AA-Ⅱ质量分数为0.09~0.50 mg·g^(–1)。结论:所建立的方法专属性强、快速、灵敏,可用于木香马兜铃中AA-Ⅰ及AA-Ⅱ的含量测定。

马兜铃属(Aristolochia L)药用植物研究概况

总结了常见马兜铃属药用植物的化学成分及生物活性研究情况。

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。

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.

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。

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.

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。

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.

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.

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

Differentiation and Analysis of Nephrotoxicity Between Caulis Clematidis Armandii(Chuan Mu Tong)and Aristolochia Manshuriensis(Guan Mu Tong)

Mutong is a kind of medicine for promoting water circulation and drenching.There are many kinds of Aristolochia manshuriensis(Guan Mu Tong),which are commonly used in clinic,such as Mutong,Caulis Clematidis Armandii(Chuan Mu Tong)and Mutong.After the event of"Longdan Xiegan pill",the doctor made Chuanmu general taboo,or replaced it with other drugs,or did not dare to use it for a long time,which affected the clinical effect.This paper discusses the toxicity of Mutong.

藏药材“巴力嘎”本草考证

为明确藏药材巴力嘎的基原及用药情况,系统查阅《月王药诊》《四部医典》《蓝琉璃》和《晶珠本草》等藏医药古籍文献及汉译本著作,对藏药材巴力嘎的名称、基原、产地及采收季节、功能主治等进行本草考证。发现藏药材巴力嘎的基原主要为西藏亚东、错那、樟木等西藏南部生产的马兜铃科植物西藏马兜铃Aristolochia griffithii Hook.f.et Thomes.ex Duchartre的干燥茎枝。对藏医临床中“巴力嘎”的应用规范化和质量标准、药效学研究提供参考。

丝带凤蝶与马兜铃的适应关系及其应用价值研究

马兜铃属的植物因其马兜铃酸含量高而著名,然而这种化合物对许多动物具有致癌性。丝带凤蝶是少数能够以这些有毒寄主植物为食的蝴蝶之一。探讨了丝带凤蝶和马兜铃的分布规律,论述马兜铃酸的化学结构和致病机制;讨论了丝带凤蝶适应马兜铃酸的分子生物机制;对比分析了这些防御性代谢物对其他食草昆虫的影响。因此,丝带凤蝶及其肠道微生物对含马兜铃酸特异性的降毒机制对富含马兜铃酸的马兜铃属、细辛属等中药材的降毒应用前景。

中药关木通中总马兜铃酸的含量测定

目的：测定关木通中总马兜铃酸的含量，保证临床用药安全有 效。方法：紫外分光光度法，检测波长为310 nm。结果：20 批关木通样品中总马兜铃酸含 量为0.63%～2.84%。结论：各地所用商品关木通中总马兜铃酸含量差异较大，且与药材性 状具一定关系。

木通所致大鼠急性肾损伤的实验观察

目的：观察木通所致大鼠急性肾损伤作用的功能变化及组织形态学特点。 方法：用木通水煎剂（６０ｇ／ｋｇ·ｄ －１） 给大鼠灌胃，建立大鼠急性肾损伤动物模型，检测有关肾功能指标，进行组织形态学观察。 结果：木通组大鼠的主要功能改变为：氮质血症、低渗尿、蛋白尿、糖尿、尿ＮＡＧ 酶升高。组织形态学改变主要表现为：急性肾小管坏死，以皮、髓交界区小管损伤为主。 结论：大剂量木通可导致大鼠急性肾功能衰竭。

雷公藤、关木通、益母草对大鼠肾毒性的比较研究

目的比较观察雷公藤、关木通、益母草对大鼠的肾毒性。方法雷公藤、关木通、益母草给大鼠连续灌胃90天,观察动物的一般情况、尿常规、尿微量蛋白、肝肾功能、肾脏病理形态学改变。剩余1/3大鼠进行停药30天恢复期观察。结果雷公藤、关木通、益母草三种药物都会造成不同程度的尿常规异常、尿微量蛋白异常和肾功能改变,停药后肾功能指标有的可复,有的不可恢复。雷公藤、关木通、益母草三种药物的大剂量都会造成不同程度的肾脏形态学改变,但损害部位有所不同。停药后,肾实质损伤多数为可逆性,间质纤维化难于恢复。结论雷公藤、关木通、益母草一定剂量均可以造成不同性质、不同程度的大鼠实验性肾损伤,有必要对益母草“非马兜铃酸性”肾脏毒性作用机制进行深入的系统研究。

木通致大鼠肿瘤作用的实验研究

目的 :观察木通所致大鼠肿瘤的发生演变过程、生物学行为、病理学及免疫组化特征。方法 :用不同剂量木通水煎剂给大鼠灌胃建立急性肾损伤模型 ,进行组织形态学及免疫组化的动态观察。结果 :( 1)实验头 3个月组织形态学未见大鼠发生肿瘤及肾脏发生明显肿瘤样增生改变。 ( 2 )实验 6个月 3个剂量组肾脏肿瘤样增生发生率均为 10 0 0 %。其中 2例进行免疫组化研究 ,波形蛋白 (vimentin)、增殖细胞核抗原 (PCNA)均表达阳性 ,平滑肌肌动蛋白 (SMA)、p53均表达阴性。 ( 3)实验 6个月 3个剂量组肾脏肿瘤发生率分别为 4 2 8%、2 5 0 %及 0 ,包括 4例肾脏间叶性肿瘤及 1例肾母细胞瘤。其中 3例肾脏间叶性肿瘤免疫组化研究显示 ,vimentin、PCNA :肿瘤细胞均表达阳性。SMA、p53:分化成熟的肿瘤细胞表达阳性。 ( 4 )实验6个月 3个剂量组肾外肿瘤发生率分别为 14 3%、12 5%和 12 5% ,其中乳腺导管上皮肿瘤、甲状腺滤泡上皮肿瘤和皮肤附件上皮肿瘤各发生 1例。对照组未见肿瘤发生。结论 :大剂量木通具有致大鼠肿瘤作用。其中肾脏肿瘤发生率相对较高 ,组织学类型以肾脏间叶性肿瘤为主。分化成熟的肾脏间叶性肿瘤伴有vi mentin、SMA、p53和PCNA的阳性表达。肾外肿瘤发生率相对较低。