Limonoids from Swietenia macrophylla and S. aubrevilleana

An investigation of the seeds of Swietenia macrophylla and S. aubrevilleana (Meliaceae) is reported. Three new compounds, augustineolide (1) and 3beta,6-dihydroxydihydrocarapin (2) from S. macrophylla and 6-acetoxyhumilinolide C (3) from S. aubrevilleana were isolated and characterized along with fifteen known compounds. Four of the compounds were subjected to an antifeedant bioassay on the final instar larvae of Spodoptera frugiperda. The antifeedant activity was comparable to that of bicyclononanolides previously tested.     

Swietenia macrophylla extract promotes the ability of Caenorhabditis elegans to survive Pseudomonas aeruginosa infection

Ethnopharmacological relevance

Swietenia macrophylla or commonly known as big leaf mahogany, has been traditionally used as an antibacterial and antifungal agent.

Aim of the study

The unwanted problem of antibiotic resistance in many bacterial species advocates the need for the discovery of the new anti-infective drugs. Here, we investigated the anti-infective properties of Swietenia macrophylla with an assay involving lethal infection of Caenorhabditis elegans with the opportunistic human pathogen Pseudomonas aeruginosa.

Materials and methods

Using a slow killing assay, Caenorhabditis elegans was challenged with an infective strain of Pseudomonas aeruginosa (PA14). The ability of Swietenia macrophylla seed ethyl acetate extract to promote the survival of infected worms was assessed by comparing the percentage of survival between extract treated and non-treated worm populations. The effect of Swietenia macrophylla towards PA14 growth, Caenorhabditis elegans feeding rate and degree of PA14 colonization in the worm gut was also evaluated. Lastly, using a fluorescent transgenic Caenorhabditis elegans strain and real time PCR, the effect of Swietenia macrophylla on the expression of lys-7, an immune response gene was also investigated.

Results

Our results demonstrate the ability of Swietenia macrophylla seed ethyl acetate extract in rescuing Caenorhabditis elegans from fatal PA14 infection. Consequently, we showed that the extract promotes the survival without exhibiting any bactericidal effect or perturbation of Caenorhabditis elegans feeding rate. We also showed that Swietenia macrophylla was able to restore the initially repressed lys-7 level in PA14 infected Caenorhabditis elegans.

Conclusion

Swietenia macrophylla extract is able to enhance the ability of Caenorhabditis elegans to survive PA14 infection without directly killing the pathogen. We further showed that the extract boosted the expression of a gene pivotal for innate immunity in Caenorhabditis elegans. Collectively, these findings strongly suggest the presence of compounds within Swietenia macrophylla seed that either reduces Pseudomonas aeruginosa virulence and/or enhance host resistance.     

A human immunodeficiency virus protease inhibitory substance from Swietenia mahagoni

For the purpose of finding anti-HIV agents from natural sources, various plant extracts were screened for their inhibitory activity against HIV-protease, an enzyme essential for viral proliferation. By bioassay-directed fractionation of the methanol extract of Swietenia mahagoni (bark) which had shown inhibitory activity against this enzyme, we isolated and identified chlorogenic acid methyl ester as a inhibitory substance, its 50% inhibitory concentration being less than 40 μg/ml. © 1997 John Wiley & Sons, Ltd.     

陕西产秦艽脂溶部位化学成分研究

目的对陕西产秦艽Gentiana macrophylla的化学成分进行系统研究。方法利用硅胶柱及其他多种色谱手段对秦艽的化学成分进行分离；用UV、IR、MS、^1H-NMR、^13C-NMR等技术及与对照品对照进行鉴定。结果从脂溶部位得到5个化合物，分别鉴定为：N-正二十五烷基-2-羧基苯甲酰胺(N-pentacosy1-2-carboxy-benzoyl amide，I)、5-羧基-3，4-二氢-1H-2-苯并吡喃-1-酮(5-carboxyl-3，4-dihydrogen-1H-2-benzopyran-1-one，Ⅱ)、红百金花内酯(erythrocentaurin，Ⅲ)、栎瘿酸(roburicacid，Ⅳ)，齐墩果酸(oleanolicacid，Ⅴ)。结论Ⅰ、Ⅱ为两个新化合物，分别命名为秦艽酰胺和红百金花酸，Ⅲ为首次从本属植物中分得。     

秦艽愈伤组织的培养及其龙胆苦苷含量的研究

目的:为扩大和提高甘肃道地药材秦艽资源的利用效率。方法:以秦艽种子的萌发所获得的幼芽作为外植体,诱导形成愈伤组织;筛选诱导愈伤组织产生的不同培养基和培养条件,并继代培养;应用HPLC法测定龙胆苦苷的含量。结果:秦艽愈伤组织生长的最佳培养基为MS+2,4-D(1.0 mg/L)+6-BA(0.5 mg/L),最佳继代培养基为MS+2,4-D(1.0 mg/L)+6-BA(0.5 mg/L)+NAA(0.5 mg/L),最佳继代时间为30 d。龙胆苦苷积累量在指数生长后期(28～30 d)达最高,为0.78 mg/g DW。结论:筛选出了适宜的秦艽愈伤组织培养方法。秦艽愈伤组织在固体培养基上的生长曲线呈"S"型,且愈伤组织中龙胆苦苷的积累量随愈伤组织增殖而不断增加。     

秦艽中龙胆苦苷纯化工艺的正交实验法优选

目的优选大孔吸附树脂纯化秦艽中龙胆苦苷的工艺条件。方法应用正交法安排实验因素,以龙胆苦苷转移率和含量为指标,比较不同工艺条件对龙胆苦苷的分离效果。结果 ADS-7型大孔树脂对龙胆苦苷的比上柱量为22.7mg/g(湿树脂),比吸附量为20.5mg/g(湿树脂),并且通过L9(34)正交实验及验证实验,用40%乙醇溶液洗脱、上样量为12mg/g(龙胆苦苷计)和药液浓度为18.5mg/ml(龙胆苦苷计)时产品中龙胆苦苷的转移率大于91%,其含量可达75%以上。结论 ADS-7型大孔树脂纯化工艺对龙胆苦苷有良好的富集效果,其工艺参数可供放大生产参考。     

正交实验法优选秦艽中龙胆苦苷提取工艺

目的优选出秦艽中龙胆苦苷的提取最佳工艺。方法采用正交试验法,以龙胆苦苷含量为指标,考察了乙醇浓度、浸取时间、溶媒用量及提取次数对秦艽中龙胆苦苷提取率的影响,优选出合理的提取工艺。结果用乙醇浓度为70%,浸取时间为36 h,溶媒用量为药材的10倍,提取次数为3次为最佳。结论经验证性实验证明所优选条件可靠,适合秦艽中龙胆苦苷的提取工艺参考。     

甘肃不同地区秦艽的龙胆苦苷含量比较

目的:测定甘肃不同地区秦艽的龙胆苦苷含量,以评价药材质量。方法:采用高效液相色谱法。结果:龙胆苦苷在0.52-5.2μg范围内具良好的线性关系(r=0.9991),平均回收率为99.2%(RSD=1.23%,n=5)。结论:甘肃不同地区秦艽龙胆苦苷的含量有差异,但均高于《中国药典》规定。栽培秦艽龙胆苦苷含量高于野生秦艽,为人工栽培秦艽、保护秦艽野生资源提供了科学依据。     

西藏地产藏药大叶秦艽的抗溃疡病作用研究

目的观察西藏地产藏药大叶秦艽的抗溃疡病作用,同时研究其初步作用机理。方法采用预防性给药,观察大叶秦艽乙醇提取物(石油醚脱脂)组分对阿司匹林诱导大鼠胃溃疡模型及无水乙醇诱导大鼠胃粘膜损伤胃溃疡模型的作用。结果西藏地产藏药大叶秦艽乙醇提取物(石油醚脱脂)组分能明显缩小阿司匹林及乙醇诱导大鼠胃溃疡模型的溃疡面积,大剂量有减少胃液总量作用和胃蛋白总量分泌作用,与对照组相比有显著性差异。结论该提取物有预防溃疡病作用,其机理有待进一步研究。     

大叶千斤拔根的化学成分

目的 研究大叶千斤拔根的化学成分.方法 采用柱色谱及薄层色谱进行分离纯化,根据其理化性质及波谱数据鉴定化学结构.结果 分离得到11个化合物,其中异黄酮4个,双氢黄酮3个,黄烷醇1个,分别是染料木素(I)、5,7.3',4'-四羟基异黄酮(II)、5,7,4'-三羟基异黄酮-7-O-β-D吡喃葡萄糖苷(III)、5,7,4'-三羟基-8,3'-二异戊烯基双氢黄酮(IV)、5,7,4'-三羟基-6-异戊烯基异黄酮(V)、云南千斤拔素(flemichin D,VI)、胡枝子黄烷酮A(lespedezaflavanone A,Ⅶ)、赛金莲木儿茶精(ouratea-catechin,Ⅷ)、3.4,5-三甲氧基苯-O-β-D-葡萄糖苷(Ⅸ)、豆甾醇-3-O-β-D-吡喃葡萄糖苷(X)、豆甾醇(XI).结论 化合物Ⅲ～V、Ⅶ～Ⅺ为首次从该种植物中得到.化合物I～Ⅺ为首次从该植物根中得到,其中以生理活性成分染料木素为代表的异黄酮为该植物根的主要成分.     

HPLC Fingerprint and LC-TOF-MS Analysis on Extract from Roots of Gentiana macrophylla

Objective Establishing a fingerprint method to identify the characteristic chemicals in the roots of Gentiana macrophylla and evaluate their quality. Methods RP-HPLC was developed for fingerprint analysis and determination of four ingredients in G. macrophylla roots from different sources. LC-ESI-TOF-MS was employed to identify the chromatographic peaks of the fingerprint. Results Five common peaks were identified by comparing their retention time with reference secoiridoid glucosides. Eight major peaks in chromatographic fingerprint were analyzed by on-line LC-ESI-TOF-MS. Four secoiridoid glucosides were identified based on their MS data. Conclusion The method is specific and could be served for the quality identification and comprehensive evaluation of G. macrophylla.     

抗痛风性关节炎中草药小叶菝葜中白藜芦醇的含量测定方法

目的：小叶菝葜是抗痛风性关节炎的中草药,探讨行质量评价方法很有必要。菝葜科植物中的标志性化合物—白藜芦醇是公认的具有明确疗效的化合物。方法：高效液相色谱（HPLC）,流动相乙腈-水（25颐75）;检测波长320 nm。结果：该方法可以用于小叶菝葜中白藜芦醇的含量测定。结论：本研究可建立小叶菝葜中白藜芦醇的测定含量方法,为进一步制定该中草药的质量标准奠定基础。     

超声提取秦艽中龙胆苦苷的工艺优选

目的:优选提取秦艽中龙胆苦苷的最佳工艺。方法:采用正交试验法,以龙胆苦苷含量为指标,考察了乙醇用量、提取时间、提取次数及提取温度对秦艽中龙胆苦苷提取率的影响,优选出合理的提取工艺。结果:以乙醇用量为30 ml、提取时间为20 min、提取次数为4次、提取温度为50℃最佳。结论:经验证性实验证明所优选条件可靠,适合秦艽中龙胆苦苷的提取工艺参考。     

云南地区大叶千斤拔不同种质的异黄酮含量比较

目的：建立大叶千斤拔中异黄酮含量测定方法,对比云南不同地区大叶千斤拔的药材质量,初步明确影响异黄酮含量的因素。方法：以染料木素为对照品,对紫外分光光度法测定大叶千斤拔中异黄酮的含量进行方法学考察,并用此方法测定采自云南不同地区野生及栽培的26份大叶千斤拔中异黄酮的含量。结果：采集野生样品中异黄酮的平均含量为0．990‰,其中屏边县的种质含量最高,为1．553‰,而绿春县（B）的种质含量最低,为0．652‰。分别栽培在3个地点的同一份大叶千斤拔种质,异黄酮含量有明显差异;在同一栽培条件下不同来源的大叶千斤拔种质异黄酮含量也有明显差异。结论：种质和环境因子对大叶千斤拔有效成分的积累均有影响。     

云南地区大叶千斤拔不同种质的异黄酮含量比较△

目的:建立大叶千斤拔中异黄酮含量测定方法,对比云南不同地区大叶千斤拔的药材质量,初步明确影响异黄酮含量的因素.方法:以染料木素为对照品,对紫外分光光度法测定大叶千斤拔中异黄酮的含量进行方法学考察,并用此方法测定采自云南不同地区野生及栽培的26份大叶千斤拔中异黄酮的含量.结果:采集野生样品中异黄酮的平均含量为0.990‰,其中屏边县的种质含量最高,为1.553‰,而绿春县(B)的种质含量最低,为0.652‰.分别栽培在3个地点的同一份大叶千斤拔种质,异黄酮含量有明显差异;在同一栽培条件下不同来源的大叶千斤拔种质异黄酮含量也有明显差异.结论:种质和环境因子对大叶千斤拔有效成分的积累均有影响.     

Studies on the antidiarrhoeal properties of Pentaclethra macrophylla leaf extracts

The aqueous (WE) and ethanol (EE) leaf extracts of Pentaclethra macrophylla were tested for antidiarrhoeal activity using experimental animal models. The i.p. LD₅₀ values were established to be 770 mg/kg and 280 mg/kg for the aqueous (WE) and ethanol (EE) extracts, respectively. Antidiarrhoeal potential of the extracts was evidenced by a significant reduction in faecal output and protection from castor oil‐induced diarrhoea in rats treated with the extracts. In addition the extracts significantly (p < 0.05) decreased propulsive movement of gastrointestinal contents in mice. On isolated tissue preparations, the extracts significantly reduced in a non‐specific manner contractions evoked by acetylcholine, nicotine and histamine. The extracts inhibited the growth of common pathogenic microorganisms. The antispasmodic as well as the antimicrobial effects of the extracts may explain the rationale for the use of the plant in traditional medicine as a popular antidiarrhoeal recipe. Copyright © 1999 John Wiley & Sons, Ltd.     

大叶胡颓子叶抗菌活性部位的研究

目的 筛选大叶胡颓子叶的抗菌活性部位,研究活性部位的抑菌作用.方法 大叶胡颓子叶经乙醇提取,系统溶剂萃取分离得到5个部位.采用滤纸片法检测各部位的抗菌活性,用平板法测定活性部位的最小抑菌浓度.结果 大叶胡颓子叶醋酸乙酯、正丁醇部位对5种常见呼吸道致病菌(金黄色葡萄球菌、大肠杆菌、铜绿假单胞菌、肺炎克氏杆菌、鲍曼不动杆菌)均有较强的体外抑制作用,最小抑菌浓度为0.357 2～1.428 6 mg/ml.结论 大叶胡颓子叶醋酸乙酯、正丁醇部具有较强的广谱抗菌活性,醋酸乙酯部的抗菌效果更为显著.     

秦艽细胞悬浮培养研究(Ⅰ)

目的建立秦艽细胞悬浮培养体系。方法通过小细胞团法优选细胞系并考察不同培养基、细胞种龄、初始pH值、培养温度、摇床转速对秦艽悬浮细胞生长及龙胆苦苷积累的影响。结果适于秦艽细胞悬浮培养条件为:MS培养基为基本培养基,用15d种龄的细胞接种,初始pH7、25℃,110r/min,摇瓶培养。结论通过摇瓶培养建立了良好的秦艽细胞悬浮培养体系。不同培养基对细胞生长及龙胆苦苷积累的显著影响提示某些无机离子有重要的调控作用。     

大叶钩藤植物不同部位中钩藤碱分析

目的 分析广西不同产地大叶钩藤植物不同部位所含钩藤碱.方法 应用HPLC分别对21批不同产地大叶钩藤植物的带钩茎枝、无茎枝钩、无钩茎枝、主杆和叶的钩藤碱进行测定,并分析评价各部位的药材质量.Gemini C18色谱柱(4.6 mm×250mm,5μm),流动相为甲醇-水(含0.002mol/L三乙胺,冰乙酸调pH至7.5)(64∶36),体积流量1.0 mL/min,检测波长254 nm.结果 21批大叶钩滕植物中的上述各部位均可检出钩藤碱成分,整体上带钩茎枝、无茎枝钩、无钩茎枝和主杆各部位含有量相近,叶含有量大于上述四个部位.结论 大叶钩藤植物的不同部位均具有进一步开发利用的价值,应当物尽其材.     

高效液相色谱法测定秦艽不同部位龙胆苦苷的含量

目的测定秦艽不同部位龙胆苦苷的含量。方法以C18反相柱为色谱柱,甲醇-水(1∶4)为流动相。检测波长254nm,用甲醇作提取剂。结果秦艽药材芦头中含有龙胆苦苷,但含量仅为根外皮部的10%,根心材龙胆苦苷约为外皮部的2倍。结论秦艽龙胆苦苷主要集中在根心材部分。