Abstract：
BACKGROUND: Pancreatitis is a common exocrine inflammatory disease of the pancreas and lacks specific medication currently. Rhei Radix et Rhizoma (RR) and its anthraquinone derivatives (AQs) have been successively reported for their pharmacological effects and molecular mechanisms in experimental and clinical pancreatitis. However, an overview of the anti-pancreatitis potential of RR and its AQs is limited.
OBJECTIVE: To summarize and analyze the pharmacological effects of RR and its AQs on pancreatitis and the underlying mechanisms, and discuss their drug-like properties and future perspectives.
METHODS: The articles related to RR and its AQs were collected from the Chinese National Knowledge Infrastructure, Wanfang data, PubMed, and the Web of Science using relevant keywords from the study\'s inception until April first, 2024. Studies involving RR or its AQs in cell or animal pancreatitis models as well as structure-activity relationship, pharmacokinetics, toxicology, and clinical trials were included.
RESULTS: Most experimental studies are based on severe acute pancreatitis rat models and a few on chronic pancreatitis. Several bioactive anthraquinone derivatives of Rhei Radix et Rhizoma (RRAQs) exert local protective effects on the pancreas by maintaining pancreatic acinar cell homeostasis, inhibiting inflammatory signaling, and anti-fibrosis, and they improve systemic organ function by alleviating intestinal and lung injury. Pharmacokinetic and toxicity studies have revealed the low bioavailability and wide distribution of RRAQs, as well as hepatotoxicity and nephrotoxicity. However, there is insufficient research on the clinical application of RRAQs in pancreatitis. Furthermore, we propose effective strategies for subsequent improvement in terms of balancing effectiveness and safety.
CONCLUSIONS: RRAQs can be developed as either candidate drugs or novel lead structures for pancreatitis treatment. The comprehensive review of RR and its AQs provides references for optimizing drugs, developing therapies, and conducting future studies on pancreatitis.
OBJECTIVE: To summarize and analyze the pharmacological effects of RR and its AQs on pancreatitis and the underlying mechanisms, and discuss their drug-like properties and future perspectives.
METHODS: The articles related to RR and its AQs were collected from the Chinese National Knowledge Infrastructure, Wanfang data, PubMed, and the Web of Science using relevant keywords from the study\'s inception until April first, 2024. Studies involving RR or its AQs in cell or animal pancreatitis models as well as structure-activity relationship, pharmacokinetics, toxicology, and clinical trials were included.
RESULTS: Most experimental studies are based on severe acute pancreatitis rat models and a few on chronic pancreatitis. Several bioactive anthraquinone derivatives of Rhei Radix et Rhizoma (RRAQs) exert local protective effects on the pancreas by maintaining pancreatic acinar cell homeostasis, inhibiting inflammatory signaling, and anti-fibrosis, and they improve systemic organ function by alleviating intestinal and lung injury. Pharmacokinetic and toxicity studies have revealed the low bioavailability and wide distribution of RRAQs, as well as hepatotoxicity and nephrotoxicity. However, there is insufficient research on the clinical application of RRAQs in pancreatitis. Furthermore, we propose effective strategies for subsequent improvement in terms of balancing effectiveness and safety.
CONCLUSIONS: RRAQs can be developed as either candidate drugs or novel lead structures for pancreatitis treatment. The comprehensive review of RR and its AQs provides references for optimizing drugs, developing therapies, and conducting future studies on pancreatitis.
摘要：
背景：胰腺炎是一种常见的胰腺外分泌炎症性疾病，目前缺乏特异性药物治疗。大黄（RR）及其蒽醌衍生物（AQs）在实验和临床胰腺炎中的药理作用和分子机制已被相继报道。然而,关于RR及其AQs的抗胰腺炎潜能的概述有限.
目的：总结分析RR及其AQs对胰腺炎的药理作用及其机制。并讨论它们的药物特性和未来前景。
方法：与RR及其AQs相关的文章来自中国国家知识基础设施，万方数据,PubMed,从研究开始到4月1日，WebofScience使用相关关键词，2024.涉及细胞或动物胰腺炎模型中RR或其AQs的研究以及结构-活性关系，药代动力学，毒理学,并纳入临床试验。
结果：大多数实验研究基于重症急性胰腺炎大鼠模型，一些实验研究基于慢性胰腺炎。大黄的几种生物活性蒽醌衍生物（RRAQs）通过维持胰腺腺泡细胞稳态对胰腺发挥局部保护作用，抑制炎症信号，和抗纤维化，它们通过减轻肠和肺损伤来改善全身器官功能。药代动力学和毒性研究揭示了低生物利用度和广泛分布的RRAQ，以及肝毒性和肾毒性。然而,关于RRAQs在胰腺炎中的临床应用研究不足。此外，我们在平衡有效性和安全性方面提出了有效的后续改进策略。
结论：RRAQ可作为胰腺炎治疗的候选药物或新型导联结构。RR及其AQs的综合评价为优化药物、开发疗法，并对胰腺炎进行未来的研究。
目的：总结分析RR及其AQs对胰腺炎的药理作用及其机制。并讨论它们的药物特性和未来前景。
方法：与RR及其AQs相关的文章来自中国国家知识基础设施，万方数据,PubMed,从研究开始到4月1日，WebofScience使用相关关键词，2024.涉及细胞或动物胰腺炎模型中RR或其AQs的研究以及结构-活性关系，药代动力学，毒理学,并纳入临床试验。
结果：大多数实验研究基于重症急性胰腺炎大鼠模型，一些实验研究基于慢性胰腺炎。大黄的几种生物活性蒽醌衍生物（RRAQs）通过维持胰腺腺泡细胞稳态对胰腺发挥局部保护作用，抑制炎症信号，和抗纤维化，它们通过减轻肠和肺损伤来改善全身器官功能。药代动力学和毒性研究揭示了低生物利用度和广泛分布的RRAQ，以及肝毒性和肾毒性。然而,关于RRAQs在胰腺炎中的临床应用研究不足。此外，我们在平衡有效性和安全性方面提出了有效的后续改进策略。
结论：RRAQ可作为胰腺炎治疗的候选药物或新型导联结构。RR及其AQs的综合评价为优化药物、开发疗法，并对胰腺炎进行未来的研究。
