白芍总苷（TGP）在我国已被广泛用于治疗炎症和免疫疾病。芍药苷 (Pae) 是 TGP 的主要活性成分。虽然TGP药物不良反应少，但Pae起效慢、生物利用度低限制了其临床应用。在开发用于炎症和免疫疾病的新药剂时，追求在不增加毒性的情况下增强功效。因此，我们小组开发了源自​​ Pae 的芍药苷-6'-O-苯磺酸盐 (CP-25)，其生物利​​用度和功效优于 Pae。在这里，我们描述了 CP-25 的开发过程和研究进展。CP-25 和 Pae 的药代动力学参数在体内和体外进行了比较。CP-25 还与一线药物甲氨蝶呤、来氟米特、和羟氯喹在关节炎动物模型和实验性干燥综合征中的疗效和不良反应。我们总结了 CP-25 对炎症和免疫相关细胞的调节作用，阐明了可能的机制，并分析了 CP-25 在炎症和免疫疾病中的治疗前景，以及与其潜在靶点 G 蛋白相关的疾病-偶联受体激酶 2 (GRK2)。该综述表明 CP-25 是治疗炎症和免疫疾病的有前途的药物，未来需要进行广泛的研究。同时，该综述为抗炎免疫药物的开发提供了新的思路。阐明可能的机制，并分析CP-25在炎症和免疫疾病中的治疗前景，以及与其潜在靶标G蛋白偶联受体激酶2（GRK2）相关的疾病。该综述表明 CP-25 是治疗炎症和免疫疾病的有前途的药物，未来需要进行广泛的研究。同时，该综述为抗炎免疫药物的开发提供了新的思路。阐明可能的机制，并分析CP-25在炎症和免疫疾病中的治疗前景，以及与其潜在靶标G蛋白偶联受体激酶2（GRK2）相关的疾病。该综述表明 CP-25 是治疗炎症和免疫疾病的有前途的药物，未来需要进行广泛的研究。同时，该综述为抗炎免疫药物的开发提供了新的思路。

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Total glycoside of paeony (TGP) has been widely used to treat inflammation and immune diseases in China. Paeoniflorin (Pae) is the major active component of TGP. Although TGP has few adverse drug reactions, the slow onset and low bioavailability of Pae limit its clinical use. Enhanced efficacy without increased toxicity is pursued in developing new agents for inflammation and immune diseases. As a result, paeoniflorin-6′-O-benzene sulfonate (CP-25) derived from Pae, is developed in our group, and exhibits superior bioavailability and efficacy than Pae. Here we describe the development process and research advance on CP-25. The pharmacokinetic parameters of CP-25 and Pae were compared in vivo and in vitro. CP-25 was also compared with the first-line drugs methotrexate, leflunomide, and hydroxychloroquine in their efficacy and adverse effects in arthritis animal models and experimental Sjögren’s syndrome. We summarize the regulatory effects of CP-25 on inflammation and immune-related cells, elucidate the possible mechanisms, and analyze the therapeutic prospects of CP-25 in inflammation and immune diseases, as well as the diseases related to its potential target G-protein-coupled receptor kinases 2 (GRK2). This review suggests that CP-25 is a promising agent in the treatment of inflammation and immune diseases, which requires extensive investigation in the future. Meanwhile, this review provides new ideas about the development of anti-inflammatory immune drugs.