甾体糖苷生物碱（SGAs）是茄科植物中一类重要的含氮甾体配糖体，广泛分布于马铃薯、番茄、茄子、龙葵、白英等食用或药用植物。该类化合物因苷元与糖链的组合方式不同，呈现出丰富的结构多样性，展现出抗肿瘤、抗炎、免疫调节、抗细菌、抗真菌等多种生物活性。现有研究表明，膜甾醇结合和膜结构扰动是SGAs发挥作用的早期共性机制，可进一步诱发氧化应激、线粒体功能损伤、能量代谢紊乱及程序性细胞死亡等系列效应；该机制亦与引发的胃肠道反应、神经系统症状、溶血及肠屏障损伤密切相关。目前关于SGAs的研究证据多来源于体外细胞和动物实验，其直接结合靶点、体内有效暴露范围及长期安全性尚未得到系统阐明。系统梳理SGAs的结构特征、植物分布及体内代谢转化规律，在此基础上分层归纳其药理活性，重点讨论结构差异与药理效应、体内暴露水平及毒性作用间的联系，旨在为SGAs的安全开发和先导化合物结构优化提供理论参考。

Steroidal glycoalkaloids (SGAs) are an important class of nitrogen-containing steroidal glycosides widely distributed in edible and medicinal plants of the Solanaceae family, including potato, tomato, eggplant, black nightshade, and Solanum lyratum. Owing to variations in the combinations of aglycone moieties and sugar chains, SGAs exhibit considerable structural diversity and possess a broad spectrum of biological activities, including antitumor, anti-inflammatory, immunomodulatory, antibacterial, and antifungal effects. Current evidence indicates that sterol binding and membrane disruption represent common early events in SGA action, which may subsequently induce oxidative stress, mitochondrial dysfunction, disturbances in energy metabolism, and various forms of regulated cell death. These mechanisms are also closely associated with gastrointestinal reactions, neurological symptoms, hemolysis, and intestinal barrier injury. However, most available evidence on SGAs has been derived from in vitro cell-based studies and animal experiments, while their direct molecular targets, effective in vivo exposure ranges, and long-term safety remain insufficiently characterized. This review systematically summarizes the structural characteristics, distribution patterns in plants, and in vivo metabolic transformations of SGAs, and further organizes the evidence concerning their pharmacological activities according to the level of experimental support. Particular emphasis is placed on the relationships among structural variation, pharmacological effects, systemic exposure, and toxicity, aimed at providing theoretical guidance for the safe development of SGAs and structural optimization of lead compounds.

R96;R944.1

浙江省农业新品种选育重大科技专项（2021C02065-1-3）