Food and Biodynamic Chemistry Laboratory, Tohoku University, Sendai, Japan.
Laboratory of Pharmaceutical Analytical Chemistry, Gifu Pharmaceutical University, Gifu, Japan.
Crit Rev Food Sci Nutr. 2023;63(19):3468-3496. doi: 10.1080/10408398.2021.1989660. Epub 2021 Oct 16.
Mulberry leaves are rich in biologically active compounds, including phenolics, polysaccharides, and alkaloids. Mulberry leaf iminosugars (MLIs; a type of polyhydroxylated alkaloids), in particular, have been gaining increasing attention due to their health-promoting effects, including anti-diabetic, anti-obesity, anti-hyperglycemic, anti-hypercholesterolemic, anti-inflammatory, and gut microbiota-modulatory activities. Knowledge regarding the in vivo bioavailability and bioactivity of MLIs are crucial to understand their role and function and human health. Therefore, this review is aimed to comprehensively summarize the existing studies on the oral pharmacokinetics and the physiological significance of selected MLIs (i.e.,1-deoxynojirimycin, d-fagomine, and 2-O-ɑ-d-galactopyranosyl-DNJ). Evidence have suggested that MLIs possess relatively good uptake and safety profiles, which support their prospective use for oral intake; the therapeutic potential of these compounds against metabolic and chronic disorders and the underlying mechanisms behind these effects have also been studied in in vitro and in vivo models. Also discussed are the biosynthetic pathways of MLIs in plants, as well as the agronomic and processing factors that affect their concentration in mulberry leaves-derived products.
桑叶富含具有生物活性的化合物，包括酚类、多糖和生物碱。特别地，桑叶氨基寡糖（MLIs；一种多羟基生物碱）由于其具有促进健康的作用，包括抗糖尿病、抗肥胖、降血糖、降胆固醇、抗炎和调节肠道微生物群的作用，引起了越来越多的关注。了解 MLIs 的体内生物利用度和生物活性对于理解它们在人体健康中的作用和功能至关重要。因此，本综述旨在全面总结关于选定 MLIs（即 1-脱氧野尻霉素、d-野尻霉素和 2-O-α-d-吡喃半乳糖基-DNJ）的口服药代动力学和生理意义的现有研究。有证据表明，MLIs 具有相对良好的吸收和安全性特征，这支持了它们用于口服摄入的前景；这些化合物对代谢和慢性疾病的治疗潜力以及这些作用背后的机制也在体外和体内模型中进行了研究。还讨论了 MLIs 在植物中的生物合成途径，以及影响桑叶衍生产品中 MLIs 浓度的农艺和加工因素。
