Baidya Ritika, Sarkar Biswatrish
Group Polyphenol-BIT, Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Mesra, Ranchi, 835215, India.
Naunyn Schmiedebergs Arch Pharmacol. 2025 Mar;398(3):2071-2106. doi: 10.1007/s00210-024-03460-6. Epub 2024 Oct 3.
Echinacoside (ECH), a naturally occurring water-soluble phenylethanoid glycoside, is one of the primary bioactive compounds present in several plant species, such as Echinacea, Cistanche, Plantago, Rosa, Buddleja, and Rehmannia. Research has revealed that these plants, rich in ECH, have diverse traditional uses and pharmacological activities, like anti-diabetic, anti-inflammatory, anti-fatigue, anti-allergic, anti-ageing, anti-skin glycation, analgesic, wound healing, and aphrodisiac properties. Among other activities, ophthalmic, haematopoiesis, pulmonary, anti-bacterial, anti-protozoal, anti-fungal, and anti-viral effects of ECH have been reported. Chemically, the compound comprises caffeic acid glycoside containing a trisaccharide that includes two glucose and one rhamnose unit. These units are linked through glycosidic bonds to a caffeic acid and a dihydroxyphenylethanol (hydroxytyrosol) residue, which are connected to the central rhamnose. The biosynthesis of ECH has been reported to start with forming L-phenylalanine and tyrosine precursors via the shikimic acid pathway. The structure-activity relationship of ECH has shown that various functional groups in the structure, particularly phenolic hydroxyl groups, are crucial for antioxidant activities. Similarly, in silico studies have revealed that ECH binds to different receptors, like Kelch-like ECH-associated protein 1 (Keap1), receptor for advanced glycation end products (RAGE), etc., to affect various pharmacological activities. The ECH contents in the reported plants often own these multifaceted properties, highlighting their importance in clinical research. Evident from its therapeutic efficacy, there is a huge potential for a comprehensive understanding of the mechanisms of actions of ECH, which underscores the need for more research in this area. Thus, this review is a compendium of the latest literature to analyse the existing knowledge on ECH, encompassing its distribution, traditional uses, extraction, chemical constituents, biosynthesis, pharmacological activities, structure-activity relationship, and in silico studies, following Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) guidelines.
紫锥菊苷（ECH）是一种天然存在的水溶性苯乙醇苷，是几种植物物种中存在的主要生物活性化合物之一，如紫锥菊、肉苁蓉、车前草、蔷薇、醉鱼草和地黄。研究表明，这些富含紫锥菊苷的植物具有多种传统用途和药理活性，如抗糖尿病、抗炎、抗疲劳、抗过敏、抗衰老、抗皮肤糖化、止痛、伤口愈合和壮阳特性。在其他活性中，紫锥菊苷的眼科、造血、肺部、抗菌、抗原虫、抗真菌和抗病毒作用也有报道。在化学结构上，该化合物由含有三糖的咖啡酸苷组成，三糖包括两个葡萄糖单元和一个鼠李糖单元。这些单元通过糖苷键与咖啡酸和二羟基苯乙醇（羟基酪醇）残基相连，它们与中心鼠李糖相连。据报道，紫锥菊苷的生物合成始于通过莽草酸途径形成L-苯丙氨酸和酪氨酸前体。紫锥菊苷的构效关系表明，结构中的各种官能团，特别是酚羟基，对抗氧化活性至关重要。同样，计算机模拟研究表明，紫锥菊苷与不同的受体结合，如 Kelch样ECH相关蛋白1（Keap1）、晚期糖基化终产物受体（RAGE）等，以影响各种药理活性。报道的植物中的紫锥菊苷含量通常具有这些多方面的特性，突出了它们在临床研究中的重要性。从其治疗效果可以明显看出，全面了解紫锥菊苷的作用机制具有巨大潜力，这凸显了该领域更多研究的必要性。因此，本综述是最新文献的汇编，旨在分析关于紫锥菊苷的现有知识，包括其分布、传统用途、提取、化学成分、生物合成、药理活性、构效关系和计算机模拟研究，遵循系统评价和Meta分析的首选报告项目（PRISMA）指南。
