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      Simulated gastrointestinal tract metabolism and pharmacological activities of water extract of Scutellaria baicalensis roots


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          Ethnopharmacological relevance


          Scutellaria baicalensis

          Georgi (Labiatae) is a well-known traditional Chinese medicine to treat inflammation, cardiovascular diseases, respiratory and gastrointestinal infections, etc. The present study was to understand the metabolism of the root of Scutellaria baicalensis (a.k.a. Huangqin in Chinese) in the gastrointestinal tract and the correlation between the metabolites and their respective pharmacological activities.

          Materials and methods

          The water extract of the root of Scutellaria baicalensis (WESB) was incubated with simulated gastric and intestinal juices, and human fecal microflora for 24 h at 37 °C. The HPLC–DAD analysis was used to monitor the in vitro metabolic process and identify its metabolites by comparing their absorption spectrum and retention time with those of chemical references. The in vitro anticomplementary and antimicrobial activity was evaluated with hemolysis assay, agar disc-diffusion method and MIC value, respectively.


          Main constituents of WESB remain unchanged during the incubation with simulated gastric juice (pH=1.5) and intestinal juice (pH=6.8), whereas four flavones, baicalin, wogonoside, oroxyloside and norwogonoside were metabolized into their respective aglycons by human intestinal bacteria. All four metabolites were demonstrated to have higher anticomplementary and antimicrobial activity than those of WESB. The anticomplementary active metabolites were identified to be baicalein, oroxylin A and norwogonin, among them, norwogonin is the most active compound.


          The presence of intestinal bacteria is demonstrated to play an important role in the gastrointestinal metabolism of WESB, and the pharmacological effects of Scutellaria baicalensis may be dependent on the intestinal bacteria metabolism.

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          Most cited references31

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          Antimicrobial activity of flavonoids.

          Flavonoids are ubiquitous in photosynthesising cells and are commonly found in fruit, vegetables, nuts, seeds, stems, flowers, tea, wine, propolis and honey. For centuries, preparations containing these compounds as the principal physiologically active constituents have been used to treat human diseases. Increasingly, this class of natural products is becoming the subject of anti-infective research, and many groups have isolated and identified the structures of flavonoids possessing antifungal, antiviral and antibacterial activity. Moreover, several groups have demonstrated synergy between active flavonoids as well as between flavonoids and existing chemotherapeutics. Reports of activity in the field of antibacterial flavonoid research are widely conflicting, probably owing to inter- and intra-assay variation in susceptibility testing. However, several high-quality investigations have examined the relationship between flavonoid structure and antibacterial activity and these are in close agreement. In addition, numerous research groups have sought to elucidate the antibacterial mechanisms of action of selected flavonoids. The activity of quercetin, for example, has been at least partially attributed to inhibition of DNA gyrase. It has also been proposed that sophoraflavone G and (-)-epigallocatechin gallate inhibit cytoplasmic membrane function, and that licochalcones A and C inhibit energy metabolism. Other flavonoids whose mechanisms of action have been investigated include robinetin, myricetin, apigenin, rutin, galangin, 2,4,2'-trihydroxy-5'-methylchalcone and lonchocarpol A. These compounds represent novel leads, and future studies may allow the development of a pharmacologically acceptable antimicrobial agent or class of agents.
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            The gastrointestinal microbiota as a site for the biotransformation of drugs.

            There are 100 trillion microbes in the human gastrointestinal tract with numbers increasing distally. These microbiota secrete a diverse array of enzymes (primarily for carbohydrate and protein fermentation) giving them substantial metabolic potential which can have major implications for drug stability. At least thirty drugs which are, or have been, available commercially, were subsequently shown to be substrates for these bacterial enzymes, and with increasing numbers of new and existing drugs having the potential for contact with the distal gut (through modified release systems or poor solubility/permeability), many more are expected to be discovered. The major concern with bacterial drug degradation is the behaviour of the metabolite; is it more or less active than the parent compound, or has toxicity resulted? For example, there were eighteen deaths in 1993 due to a drug interaction in which a toxic drug metabolite was produced by bacterial fermentation. Thus, the objective of this review is the provision of a comprehensive overview of this area; the gastrointestinal microbiota, their drug substrates and metabolic mechanisms, and approaches to studying this further are discussed.
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              Antioxidant and anti-inflammatory activities of selected medicinal plants containing phenolic and flavonoid compounds.

              The antioxidant, anti-inflammatory, and cytotoxic activities of water and ethanol extracts of 14 Chinese medicinal plants were investigated and also their total phenolics and flavonoid contents measured. The antioxidant activity was evaluated in a biological assay using Saccharomyces cerevisiae , whereas the radical scavenging activity was measured using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method. Total phenolics and flavonoid contents were estimated by Folin-Ciocalteu and aluminum chloride methods, respectively. The anti-inflammatory activities of the plant extracts were determined by measuring the inhibition of production of nitric oxide (NO) and TNF-α in LPS and IFN-γ activated RAW 264.7 macrophages. Their cytotoxic activities against macrophages were determined by Alamar Blue assay. Four plants, namely, Scutellaria baicalensis , Taxillus chinensis , Rheum officinale , and Sophora japonica , showed significant antioxidant activity in both yeast model and also free radical scavenging methods. The ethanol extract of S. japonica showed highest levels of phenolics and flavonoids (91.33 GAE mg/g and 151.86 QE mg/g, respectively). A positive linear correlation between antioxidant activity and the total phenolics and flavonoid contents indicates that these compounds are likely to be the main antioxidants contributing to the observed activities. Five plant extracts (S. baicalensis, T. chinensis, S. japonica, Mahonia fortunei , and Sophora flavescens ) exhibited significant anti-inflammatory activity by in vitro inhibition of the production of NO and TNF-α with low IC(50) values. These findings suggest that some of the medicinal herbs studied in this paper are good sources of antioxidants.

                Author and article information

                J Ethnopharmacol
                J Ethnopharmacol
                Journal of Ethnopharmacology
                Elsevier Ireland Ltd.
                8 January 2014
                27 February 2014
                8 January 2014
                : 152
                : 1
                : 183-189
                [a ]School of Pharmacy, Shanghai Jiao Tong University, No. 800 Dongchuan Road, Minhang District, Shanghai 200240, China
                [b ]School of Pharmacy, Fudan University, No. 826 Zhangheng Road, Pudong District, Shanghai 200032, China
                Author notes
                [* ]Corresponding author. Tel.: +86 21 34204806; fax: +86 21 34204804. xbli@ 123456sjtu.edu.cn

                Contributed to this paper equally.

                Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.

                Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.

                : 8 November 2013
                : 28 December 2013
                : 31 December 2013

                Pharmacology & Pharmaceutical medicine
                baicalin (pubchem cid: 64982),wogonoside (pubchem cid: 29927693),baicalein (pubchem cid: 5281605),wogonin (pubchem cid: 5281703),oroxylin a (pubchem cid: 5320315),oroxyloside (pubchem cid: 38348319),norwogonin (pubchem cid: 5281674),norwogonoside (pubchem cid: 44258552),gastrointestinal tract,metabolism,scutellaria baicalensis,anticomplementary,antibacterial


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