<p>The genus <i>Bupleurum</i> has high medicinal value and has been widely used as a traditional herbal medicine in Asia, Europe, and North Africa over the past 2000&#xa0;years. Despite its medicinal importance, in-depth research on the chemical composition and pharmacological activity of <i>Bupleurum</i> is lacking. This review aimed to comprehensively summarize the phytochemistry, pharmacology, and saponin biosynthesis of <i>Bupleurum</i> to provide a novel basis for future research. Information was retrieved from electronic resources including SciFinder, PubMed, Web of Science, Chinese National Knowledge Infrastructure, Google Scholar, Baidu Scholar, Science Direct, from March 1953 to March 2023. The keyword used for literature retrieval was “<i>Bupleurum</i>”. Presently, over 557 compounds (excluding volatile oils), including saponins, terpenoids, flavonoids, lignans, phenylpropanoids, coumarins, sterols, polyenes, polyalkynes, and polysaccharides, have been isolated or identified from 67 species of <i>Bupleurum</i>. To the best of our knowledge, this is the most comprehensive summary of chemical components in <i>Bupleurum</i> to date. Modern studies have proven that <i>Bupleurum</i> and its active compounds possessed a wide range of pharmacological effects, such as anti-inflammatory, cytotoxic, hepatoprotective, and antiviral activities. Furthermore, analysis of the primary structure–activity relationship indicated that the C13,28-epoxy bridge may be importantly associated with several pharmacological activities. Multiomic studies have identified several candidate genes for saponin biosynthesis, such as <i>β</i>-amyrin synthase (<i>BcBAS1</i>, <i>Bc61215</i>) and cytochrome P450 (<i>Bc95697</i>, <i>Bc35434</i>) genes. Future research may place greater emphasis on the study of concrete pharmacological mechanisms.</p>

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A comprehensive review of the phytochemistry, pharmacology, and saponin biosynthesis of the genus Bupleurum

  • Changsheng Yuan,
  • Yanmeng Liu,
  • Yihan Wang,
  • Tiegui Nan,
  • Liping Kang,
  • Huaizhu Li,
  • Zhilai Zhan,
  • Luqi Huang

摘要

The genus Bupleurum has high medicinal value and has been widely used as a traditional herbal medicine in Asia, Europe, and North Africa over the past 2000 years. Despite its medicinal importance, in-depth research on the chemical composition and pharmacological activity of Bupleurum is lacking. This review aimed to comprehensively summarize the phytochemistry, pharmacology, and saponin biosynthesis of Bupleurum to provide a novel basis for future research. Information was retrieved from electronic resources including SciFinder, PubMed, Web of Science, Chinese National Knowledge Infrastructure, Google Scholar, Baidu Scholar, Science Direct, from March 1953 to March 2023. The keyword used for literature retrieval was “Bupleurum”. Presently, over 557 compounds (excluding volatile oils), including saponins, terpenoids, flavonoids, lignans, phenylpropanoids, coumarins, sterols, polyenes, polyalkynes, and polysaccharides, have been isolated or identified from 67 species of Bupleurum. To the best of our knowledge, this is the most comprehensive summary of chemical components in Bupleurum to date. Modern studies have proven that Bupleurum and its active compounds possessed a wide range of pharmacological effects, such as anti-inflammatory, cytotoxic, hepatoprotective, and antiviral activities. Furthermore, analysis of the primary structure–activity relationship indicated that the C13,28-epoxy bridge may be importantly associated with several pharmacological activities. Multiomic studies have identified several candidate genes for saponin biosynthesis, such as β-amyrin synthase (BcBAS1, Bc61215) and cytochrome P450 (Bc95697, Bc35434) genes. Future research may place greater emphasis on the study of concrete pharmacological mechanisms.