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莱茵生物,一个有潜力的转折点?

Rhein Derivatives, A Promising Pivot?

机构信息

Department of Pharmacy, Xiangya Hospital, Central South University, Changsha 410008, China.

Department of Orthopaedics, Xiangya Hospital, Central South University, Changsha 410008, China.

出版信息

Mini Rev Med Chem. 2021;21(5):554-575. doi: 10.2174/1389557520666201109120855.

DOI:10.2174/1389557520666201109120855
PMID:33167832
Abstract

Rhein, an anthraquinone derivative, has been employed widely, especially for the treatment of intractable diseases like diabetic nephropathy, arthritis, and cancer in a unique action mechanism. In the last decades, considerable efforts have been made in structural modification of rhein. This paper reviewed patents on pharmacological activity and therapeutic application of rhein and its derivatives from 1978 to 2018. Particularly, an analysis of patents was made, with the top 10 most valuable patents presented, and the interpretation of the legal status of patents was given. Given the properties of superior pharmacological activity, rich resources, cheap price, low toxicity, and mature extraction process, it is believed that an in-depth investigation on rhein and its derivatives is worth trying.

摘要

大黄酸是蒽醌衍生物的一种,具有独特的作用机制,已被广泛应用于治疗糖尿病肾病、关节炎和癌症等疑难病症。在过去几十年中,人们对大黄酸的结构进行了大量的修饰。本文综述了 1978 年至 2018 年大黄酸及其衍生物的药理学活性和治疗应用的专利。特别地,对专利进行了分析,提出了 10 项最有价值的专利,并对专利的法律地位进行了解释。鉴于大黄酸具有优良的药理学活性、丰富的资源、低廉的价格、低毒性和成熟的提取工艺,相信对大黄酸及其衍生物进行深入研究是值得尝试的。

相似文献

1
Rhein Derivatives, A Promising Pivot?莱茵生物,一个有潜力的转折点?
Mini Rev Med Chem. 2021;21(5):554-575. doi: 10.2174/1389557520666201109120855.
2
A research update on the therapeutic potential of rhein and its derivatives.关于大黄酸及其衍生物治疗潜力的研究进展。
Eur J Pharmacol. 2021 May 15;899:173908. doi: 10.1016/j.ejphar.2021.173908. Epub 2021 Jan 27.
3
Rhein, An Anthraquinone Drug, Suppresses the NLRP3 Inflammasome and Macrophage Activation in Urate Crystal-Induced Gouty Inflammation.大黄素,一种蒽醌类药物,可抑制尿酸盐结晶诱导的痛风性炎症中的 NLRP3 炎性小体和巨噬细胞活化。
Am J Chin Med. 2019;47(1):135-151. doi: 10.1142/S0192415X19500071. Epub 2019 Jan 7.
4
A fruitful decade from 2005 to 2014 for anthraquinone patents.2005年至2014年是蒽醌专利成果丰硕的十年。
Expert Opin Ther Pat. 2015;25(9):1053-64. doi: 10.1517/13543776.2015.1050793. Epub 2015 Jun 3.
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Pharmacokinetics and pharmacodynamics of rhubarb anthraquinones extract in normal and disease rats.大黄蒽醌提取物在正常及患病大鼠体内的药代动力学和药效学
Biomed Pharmacother. 2017 Jul;91:425-435. doi: 10.1016/j.biopha.2017.04.109. Epub 2017 May 2.
6
Kidney-targeted drug delivery via rhein-loaded polyethyleneglycol--polycaprolactone--polyethylenimine nanoparticles for diabetic nephropathy therapy.载雷酚酮的聚乙二醇-聚己内酯-聚乙烯亚胺纳米粒经肾脏靶向给药用于糖尿病肾病治疗。
Int J Nanomedicine. 2018 Jun 19;13:3507-3527. doi: 10.2147/IJN.S166445. eCollection 2018.
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Potential Medicinal Value of Rhein for Diabetic Kidney Disease.大黄素治疗糖尿病肾病的潜在药用价值。
Chin J Integr Med. 2023 Oct;29(10):951-960. doi: 10.1007/s11655-022-3591-y. Epub 2023 Jan 6.
8
Rhein improves renal lesion and ameliorates dyslipidemia in db/db mice with diabetic nephropathy.瑞林改善糖尿病肾病 db/db 小鼠的肾脏病变并改善血脂异常。
Planta Med. 2010 Jan;76(1):27-33. doi: 10.1055/s-0029-1185948. Epub 2009 Jul 28.
9
Combined therapy of rhein and benazepril on the treatment of diabetic nephropathy in db/db mice.大黄酸与贝那普利联合治疗db/db小鼠糖尿病肾病的研究
Exp Clin Endocrinol Diabetes. 2007 Oct;115(9):571-6. doi: 10.1055/s-2007-981469.
10
Anthraquinones As Pharmacological Tools and Drugs.蒽醌类作为药理工具和药物。
Med Res Rev. 2016 Jul;36(4):705-48. doi: 10.1002/med.21391. Epub 2016 Apr 25.

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Rhein alleviates hepatic steatosis in NAFLD mice by activating the AMPK/ACC/SREBP1 pathway to enhance lipid metabolism.大黄酸通过激活AMPK/ACC/SREBP1通路增强脂质代谢,从而减轻非酒精性脂肪性肝病(NAFLD)小鼠的肝脂肪变性。
Mol Med. 2025 Jul 10;31(1):255. doi: 10.1186/s10020-025-01304-4.
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Recent Advances in the Application of Hydrogels as Drug Carriers in Inflammatory Bowel Disease: A Review.水凝胶作为药物载体在炎症性肠病中的应用研究进展:综述
Int J Mol Sci. 2025 Mar 22;26(7):2894. doi: 10.3390/ijms26072894.
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Bibliometric analysis of rhein in the treatment of tumors.
大黄酸治疗肿瘤的文献计量学分析
Front Oncol. 2025 Feb 6;15:1550016. doi: 10.3389/fonc.2025.1550016. eCollection 2025.
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Traditional Chinese medicine in the treatment of -related gastritis: The mechanisms of signalling pathway regulations.中医治疗相关性胃炎:信号通路调控机制
World J Gastroenterol. 2025 Jan 21;31(3):96582. doi: 10.3748/wjg.v31.i3.96582.
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Palindrome-mediated DNA nanotubes with cell-specific aptamers to improve targeted antitumor effects and reduce toxicity on non-small cell lung cancer.具有细胞特异性适配体的回文介导DNA纳米管,用于改善靶向抗肿瘤作用并降低对非小细胞肺癌的毒性。
Sci China Life Sci. 2025 Feb;68(2):454-466. doi: 10.1007/s11427-023-2556-4. Epub 2024 Nov 26.
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A Rhein-Based Derivative Targets .一种基于大黄酸的衍生物靶向……
Antibiotics (Basel). 2024 Sep 13;13(9):882. doi: 10.3390/antibiotics13090882.
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Potential application of -Rhubarb for the treatment of diabetic kidney disease based on network pharmacology and cell culture experimental verification.基于网络药理学和细胞培养实验验证大黄在糖尿病肾病治疗中的潜在应用
World J Diabetes. 2024 Mar 15;15(3):530-551. doi: 10.4239/wjd.v15.i3.530.
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Rhein alleviates advanced glycation end products (AGEs)-induced inflammatory injury of diabetic cardiomyopathy in vitro and in vivo models.雷帕霉素减轻糖尿病心肌病体外及体内模型中晚期糖基化终产物诱导的炎症损伤。
J Nat Med. 2023 Sep;77(4):898-915. doi: 10.1007/s11418-023-01741-7. Epub 2023 Aug 19.