细胞毒性腺苷类似物是最早用于癌症治疗的化疗药物之一。虫草素是在真菌冬虫夏草中发现的腺苷的天然衍生物，不仅可以通过阻碍生物合成、诱导细胞凋亡或自噬、调节细胞周期、减少肿瘤侵袭和转移来直接抑制肿瘤，还可以调节肿瘤微环境内的免疫反应。此外，广泛的研究强调了虫草素在缓解高脂血症和调节葡萄糖代谢方面的显着治疗潜力。该综述全面分析了虫草素及其类似物的构效关系，概述了其药代动力学特性以及提高其生物利用度的策略。深入分子生物学，探索虫草素在肿瘤抑制和代谢紊乱治疗中的药理机制，从而强调其在这些领域药物开发的巨大潜力，为创新治疗策略奠定基础。版权所有 © 2024 张，杨，赵和张。

Cytotoxic adenosine analogues were among the earliest chemotherapeutic agents utilised in cancer treatment. Cordycepin, a natural derivative of adenosine discovered in the fungus Ophiocordyceps sinensis, directly inhibits tumours not only by impeding biosynthesis, inducing apoptosis or autophagy, regulating the cell cycle, and curtailing tumour invasion and metastasis but also modulates the immune response within the tumour microenvironment. Furthermore, extensive research highlights cordycepin's significant therapeutic potential in alleviating hyperlipidaemia and regulating glucose metabolism. This review comprehensively analyses the structure-activity relationship of cordycepin and its analogues, outlines its pharmacokinetic properties, and strategies to enhance its bioavailability. Delving into the molecular biology, it explores the pharmacological mechanisms of cordycepin in tumour suppression and metabolic disorder treatment, thereby underscoring its immense potential in drug development within these domains and laying the groundwork for innovative treatment strategies.Copyright © 2024 Zhang, Yang, Zhao and Zhang.