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Science based authentication of dietary supplements---studies on the chemical constituents, analytical method and biological activities of Scutellaria spp and Pfaffia paniculata Kuntze.

机译:基于科学的膳食补充剂认证---黄-和Pfaffia paniculata Kuntze的化学成分,分析方法和生物学活性研究。

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摘要

The primary objective of this project is to explore the chemical constituents of American skullcap, (Scutellaria lateriflora), which will be used as reference markers to develop a validated chemical fingerprinting method for the differentiation of it from its adulterant, germander. From the MeOH extract of the aerial parts of this plant sixteen compounds, including three minor coumarins in which two are new, six flavonoids, four triterpenes, two steroids, and one fatty acid were isolated and characterized. In order to compare the similarity of chemical components between American skullcap and Chinese skullcap (S. baicalensis), also to obtain more marker compounds, the chemical components of Chinese skullcap, which is the most often used herb medicine in this genus, were also studied and seventeen flavonoids have been isolated. Based on the chemical constituents, a simple HPLC-PDA fingerprinting method was developed, which can be used to authenticate S. lateriflora species, to distinguish it from its potential adulterants, to compare the chemical profiles of related species in this genus, and to assess the quality of commercial products claiming to contain S. lateriflora. In the present study three classes of compounds, including eleven flavonoids isolated from two Scutellaria species mentioned above and two phenylpropanoids, as well as one diterpene isolated from T. canadense, were used as markers simultaneously to provide comprehensive analysis for the above mentioned purposes. As part of the efforts of this project, a HPLC/ESI-MSn method was established which allowed a fast characterization of thirteen flavonoids and one stilbene derivative from American skullcap without time-consuming isolation of compounds even if reference compounds are not available. The biological activities of the two skullcap extracts and thirteen flavonoids isolated from them were evaluated on a panel of bioassays, including cytotoxicity, antioxidant, anti-inflammatory, estrogenic activity and activations on peroxisome proliferator-activated receptor-alpha and -gamma (PARPalpha and PPARgamma). Neither skullcap extracts nor pure compounds tested showed cytotoxicity against a panel of mammalian normal and solid tumor cell lines at the tested concentrations. During the investigation of chemical constituents of American skullcap no neoclerodane diterpenes, which are responsible for the hepatotoxicity in germander (Kouzi et al., 1994), were found. Taken together, these evidences suggest that the reports of hepatotoxic reactions on American skullcap might very likely be due to its adulterant germander. In the present bioassay study, the most significant finding was the identification of PPARs activation of skullcap extracts as well as several characteristic flavonoids, such as baicalein, baicalin, wogonin, and chrysin etc. that provides some information on possible new application of skullcap, especially American skullcap, for the treatment of diabetic-related diseases. Also the potent activity of these flavonoids on PPARs suggests the potential of these flavonoids as leads for PPARalpha and PPARgamma agonists.;P. paniculata Kuntze, belonging to the family Amaranthaceae, is a large, rambling, shrubby ground vine with an intricate, deep, and extensive root system. It is the most employed species in commercial preparations in Brazil as "Brazilian ginseng" and has been commonly used for three centuries with the same indications as American and Asian ginseng. More than fifty preparations, which contained or were produced from plant P. paniculata are available on USA market, but no analytical method(s) existed to assess the quality of P. paniculata raw materials, and the products claiming to contain P. paniculata. In order to develop an appropriate validated quantitative analytical method for the quality control of this plant material and dosage form the detailed phytochemical investigation of P. paniculata was carried out. Two new nortriterpenoids pfaffine A and B, one new compound pfaffine C, along with eleven known compounds were isolated and identified from the roots of this plant. These compounds will be used as markers for quality control of raw materials of P. paniculata as well as products claiming to contain this species. (Abstract shortened by UMI.)
机译:该项目的主要目的是探索美国黄skull(Scutellaria Lateriflora)的化学成分,将其用作参考标记,以开发出一种经过验证的化学指纹图谱方法,以区别于其掺假,德耳德。从该植物的地上部分的MeOH提取物中,分离并鉴定了16种化合物,其中包括3种较小的香豆素,其中有2种是新的香豆素,其中包括6种黄酮,4种三萜,2种甾体和1种脂肪酸。为了比较美国黄skull和中国黄skull(S。baicalensis)的化学成分的相似性,并且为了获得更多的标记化合物,还研究了中国黄used(该属最常用的草药)的化学成分。并已分离出十七种类黄酮。根据化学成分,开发了一种简单的HPLC-PDA指纹图谱方法,可用于鉴定红花链球菌物种,将其与可能的掺假物区分开,比较该属中相关物种的化学特征并进行评估自称含有红花链球菌的商品质量。在本研究中,三类化合物,包括从上述两种黄S中分离出的11种黄酮类化合物和两种从苯丙酸杜鹃中分离出的二萜类化合物,同时被用作标记物,以为上述目的提供全面的分析。作为该项目工作的一部分,建立了HPLC / ESI-MSn方法,该方法可以快速表征13种黄酮类化合物和一种来自美国黄的二苯乙烯衍生物,即使没有参考化合物也无需费时的分离。在一组生物测定中评估了两种黄skull提取物和从中分离出的13种类黄酮的生物活性,包括细胞毒性,抗氧化剂,抗炎性,雌激素活性以及对过氧化物酶体增殖物激活的受体α和-γ(PARPalpha和PPARgamma )。在测试浓度下,黄skull提取物或纯化合物均未显示出对一组哺乳动物正常和实体瘤细胞系的细胞毒性。在研究美国黄skull的化学成分时,未发现对德国人肝毒性负责的新环戊烷二萜(Kouzi等,1994)。综上所述,这些证据表明,关于美国黄skull肝毒性反应的报道很可能是由于其掺假的德国der鱼。在目前的生物测定研究中,最重要的发现是鉴定了黄cap提取物的PPARs活化以及黄characteristic素,黄ical苷,wogonin和chrysin等几种特征性类黄酮,这些化合物为黄skull的可能新应用提供了一些信息,尤其是美国黄skull,用于治疗糖尿病相关疾病。这些类黄酮对PPAR的有效活性也表明这些类黄酮作为PPARα和PPARgamma激动剂的潜在潜力。 paniculata Kuntze属于A菜科,是一种大型,杂乱无章的地面蔓生葡萄,具有复杂,深层和广泛的根系。它是巴西商业制剂中使用最多的物种,称为“巴西人参”,已经被使用了三个世纪,其适应症与美国和亚洲人参相同。在美国市场上可以买到包含或由植物假单胞菌生产的五十多种制剂,但是尚无分析方法来评估该假单胞菌原料的质量,并且声称该产品含有假单胞菌的产品。为了开发一种适当的经过验证的定量分析方法,以对该植物材料和剂型进行质量控制,对P. paniculata进行了详细的植物化学研究。从该植物的根中分离并鉴定了两种新的降冰片萜类药物pfaffine A和B,一种新的化合物pfaffine C,以及十一种已知的化合物。这些化合物将用作对P. paniculata原材料以及声称含有该物种的产品进行质量控制的标记。 (摘要由UMI缩短。)

著录项

  • 作者

    Li, Jing.;

  • 作者单位

    The University of Mississippi.;

  • 授予单位 The University of Mississippi.;
  • 学科 Agriculture Plant Culture.;Chemistry Biochemistry.;Chemistry Analytical.
  • 学位 Ph.D.
  • 年度 2010
  • 页码 221 p.
  • 总页数 221
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

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