小叶榕化学成分和质量标准研究

【作者】 李彦文；

【导师】 阎玉凝；

【作者基本信息】 北京中医药大学 ， 中药学， 2008， 博士

【摘要】 桑科(Moraceae)榕属(Ficus)植物榕树(Ficus microcarpa Linn.f.),别名小叶榕、细叶榕、赤榕、万年青等,以其气生根和叶入药。气生根入药者称为榕须,叶入药者称为小叶榕,是岭南常用中草药,有着广泛民间用药基础。具有清热祛湿,止咳化痰,活血散瘀的功效。用于治疗支气管炎、流感、百日咳、扁桃体炎、菌痢、肠炎、目赤、牙痛、跌打损伤等症。目前小叶榕尚未收入药典,其化学成分及质量标准研究也未见报道。本课题对小叶榕的化学成分和质量标准进行了较为系统的研究,同时还对其镇咳、祛痰、抗炎等药效指标进行了探讨,从而为其临床应用和进一步研究开发提供了科学依据。研究内容主要包括以下几方面:1.化学成分的提取分离利用多种色谱技术对小叶榕化学成分进行提取分离,确定了17个化合物的结构。包括黄酮类成分3个、三萜及甾醇类成分8个、醇、酸及酯类成分6个,分别为牡荆素(Vitexin)、荭草苷(orientin)、异牡荆苷(isovitexin)、十八烷酸(stearic acid)、十五烷酸(pentadecyl acid)、三十二烷醇(dotriacontanol)、二十八烷醇(octacosanol)、二十六烷酸(hexacosanoicacid)、β-香树酯酮(β-amyrone)、β-谷甾醇(β-sitosterol)、羽扇豆醇(lupeol)、羽扇豆醇乙酸酯(lupeopl acetate)、β-香树酯醇(β-amyrin)、胡萝卜苷(daucosterol)、β-香树酯醇乙酸酯(β-amyrin acetate)、马斯里酸(maslinic acid)、表木栓醇(epifriedelinol)。这些化合物中,除β-谷甾醇、胡萝卜苷、羽扇豆醇乙酸酯、表木栓醇、马斯里酸外,其余化合物均是首次从小叶榕中分离得到,牡荆素、荭草苷、异牡荆苷为首次从榕属植物分离得到。2.挥发油成分的分析小叶榕挥发油共鉴定出29个化合物,占挥发油总量的95.13%,其中以萜类及其氧化物为主,叶绿醇和广藿香醇含量比较高。3.药效活性的研究采用三种体内动物实验(小鼠喷雾致咳法、小鼠酚红祛痰法、小鼠耳肿胀抗炎法),考察了小叶榕在镇咳、祛痰、抗炎相关模型中的作用。结果表明,小叶榕水提物、乙酸乙酯萃取物均有明显的镇咳、祛痰和抗炎作用,且从整体趋势来看,乙酸乙酯萃取物的作用强于水提物,因此确定乙酸乙酯部位为小叶榕镇咳、祛痰和抗炎的有效部位。并且乙酸乙酯萃取物中主要含黄酮类化合物,证明黄酮类成分是小叶榕镇咳、祛痰、抗炎的有效成分之一。4.质量标准的研究包括性状、显微、理化鉴别和定量分析,根据小叶榕中所含化学成分和药效分析,采用紫外—可见分光光度法,对药材中的总黄酮进行了含量测定;采用HPLC法,对药材中的牡荆素进行了含量测定;并考察了小叶榕的有效成分动态积累情况,确立了最佳采收期和适宜采收年限。在上述工作基础上,起草了小叶榕药材的质量标准(草案)。所起草的质量标准草案能较好的控制该药材的质量。综上,通过对小叶榕药材较为系统的成分分析和鉴别研究,获知了其部分物质基础,进一步充实了对小叶榕性状、显微鉴别、薄层色谱鉴别、含量测定和药理活性等方面的研究内容,建立了小叶榕药材的质量标准(草案)。为小叶榕的研究开发及临床应用提供了物质基础和理论依据。更多还原

【Abstract】 Ficus microcarpa Linn.f.belongs to the genus Ficus of family Moraceae, which is also called Xiaoyerong,Xiyerong,Wannianqing,etc.It’s aerial root and leaves both can be used as medicine,the former called as Rongxu and the latter called as Xiaoyerong.It is widely distributed in the tropical and subtropical areas in China.Due to the effects of clearing heat,removing damp,relieving cough and eliminating phlegm,promoting blood circulation to remove blood stasis, Xiaoyerong has been widely used for the treatment of bronchitis,influenza, pertussis,tonsillitis,bacterial dysentery,enteritis,conjunctival congestion, toothache,traumatic injury,etc.But Xiaoyerong has not been adopted by the Chinese pharmacopea and it’s chemical constituents have been scarcely reported. So in this research,systematically studies on it’s chemical constituents and quality control were carried out,and antitussive,expectorant and anti-imflammatory effects were investigated.So as to provide theoretical proof and practical reference for its clinical application and further research.1.Extraction and SeparationIn this thesis,studies on the chemical constituents of Xiaoyerong,17 compounds had been isolated from the dried folium of Ficus microcarpa Linn.f. Based on their physicochemical and spectroscopic evidence,17 structures were elucidated as follows:3 flavonoids:vitexin,orientin,isovitexin;8 triterpenoids and sterols:β-amyrone,β-sitosterol,lupeol,lupeopl acetate,β-amyrin,β-amyrin acetate,daucosterol,maslinic acid;6 alcohol,acid and esters:stearic acid, pentadecyl acid,n-Octacosanol,n-Octacosanol,hexacosanoic acid.Among these compounds,exceptβ-sitosterol,daucosterol,epifriedelinol,maslinic acid,the other compounds were isolated for the first time from this plant;and vitexin, orientin and isovitexin were isolated for the first time from genus Ficus.2.Volatile oil Components AnalysisVolatile oil in Xiaoyerong was also analyzed,29 compounds had been identificated.The main constituents of this oil were terpenoids and their oxides, which accounts for 95.13 percent of the total volatile oil.Phytol and patchouli alcohol were the higher contents.3.Study on the Pharmacological EffectsThree methods had been used in experiments,which were investigated the effects of antitussive,apophlegmatic and anti-inflammatory effects of Xiaoyerong. The results showed that water extract and ethyl acetate extract had obviously antitussive apophlegmatic and anti-inflammatory activities,and the latter’s effect was stronger than the former.So ethyl acetate extract is the effective fraction of Xiaoyerong,and flavonoid is effective components of Xiaoyerong4.Study on Quality StandardsIn this thesis,studies on the quality control of Xiaoyerong were performed, including characteristics,microconstruction and physical and chemical character, quantitative determination of total flavonoid by UV-VIS,vitexin by HPLC. Through the investigation of variations of effective components,optimum collecting time and harvest periods were established.And based on those,a quality standard of Xiaoyerong was drafted to provide reference for clinical practice.In summary,in this thesis,through the systematical studies mentioned above on Xiaoyerong,part of its chemical constituents has been determinde.Its characteristics,microconstruction,physical and chemical character,quantitative determination and pharmacological effects have been studied.These provided the theoretical basis and scientific reference for further study,development and application of Ficus microcarpa Linn.f.更多还原