Zhang Shiwen, Wang Ruixue, Sun Mingge, Zhang Gang, Liu Mengmeng
College of Traditional Chinese Medicine, Hebei University, Baoding 071002, China.
College of Pharmacy and Shaanxi Qinling Application Development and Engineering Center of Chinese Herbal Medicine, Shaanxi University of Chinese Medicine, Xi'an 712046, China.
J Agric Food Chem. 2025 Jun 25;73(25):15733-15740. doi: 10.1021/acs.jafc.5c03727. Epub 2025 Jun 10.
The dried rhizomes and roots of are widely used in China, Russia, and Arabia for the treatment of various diseases, with anthraquinone glycosides being the principal bioactive constituents. However, the glycosyltransferases involved in the biosynthesis of these glycosides remain largely unexplored. In this study, we first report the discovery and characterization of four novel glycosyltransferases (GTs)─RpUGT8, RpUGT12, RpUGT19, and RpUGT26─responsible for anthraquinone glycosylation in . These enzymes catalyze the formation of key bioactive compounds such as emodin-6--β--glucoside and rhein-8--β--glucoside. These glycosides are important for their pharmacological activities. By performing multiple sequence alignment, molecular docking, and site-directed mutagenesis, we identified critical residues required for their catalytic activity. Additionally, these enzymes exhibit broad substrate promiscuity, facilitating glycoside formation from various compounds, such as flavonoids, chalcones, dihydroflavonoids, and dihydrochalcones. This study provides valuable insights into the glycosylation mechanisms of emodin-type anthraquinone glycosides and offers an efficient approach for synthesizing -glycosides with medicinal potential.
在中国、俄罗斯和阿拉伯地区，[植物名称]的干燥根茎被广泛用于治疗各种疾病，蒽醌糖苷是其主要的生物活性成分。然而，参与这些糖苷生物合成的糖基转移酶在很大程度上仍未被研究。在本研究中，我们首次报道了四种新型糖基转移酶（GTs）——RpUGT8、RpUGT12、RpUGT19和RpUGT26——负责[植物名称]中蒽醌的糖基化。这些酶催化关键生物活性化合物的形成，如大黄素-6-β-葡萄糖苷和大黄酸-8-β-葡萄糖苷。这些糖苷因其药理活性而重要。通过进行多序列比对、分子对接和定点诱变，我们确定了其催化活性所需的关键残基。此外，这些酶表现出广泛的底物选择性，促进了各种化合物（如黄酮类、查耳酮、二氢黄酮类和二氢查耳酮）糖苷的形成。本研究为大黄素型蒽醌糖苷的糖基化机制提供了有价值的见解，并为合成具有药用潜力的β-糖苷提供了一种有效方法。
