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牛蒡子苷的药理学和毒理学研究综述。

A review of the pharmacology and toxicology of aucubin.

机构信息

Department of Clinical Pharmacology, Xiangya Hospital, Central South University, 87 Xiangya Road, Changsha 410008, PR China; Institute of Clinical Pharmacology, Central South University, Hunan Key Laboratory of Pharmacogenetics, 110 Xiangya Road, Changsha 410078, PR China; Engineering Research Center of Applied Technology of Pharmacogenomics, Ministry of Education, 110 Xiangya Road, Changsha 410078, PR China; National Clinical Research Center for Geriatric Disorders, 87 Xiangya Road, Changsha 410008, Hunan, PR China.

Department of Clinical Pharmacology, Xiangya Hospital, Central South University, 87 Xiangya Road, Changsha 410008, PR China; Institute of Clinical Pharmacology, Central South University, Hunan Key Laboratory of Pharmacogenetics, 110 Xiangya Road, Changsha 410078, PR China; Engineering Research Center of Applied Technology of Pharmacogenomics, Ministry of Education, 110 Xiangya Road, Changsha 410078, PR China; National Clinical Research Center for Geriatric Disorders, 87 Xiangya Road, Changsha 410008, Hunan, PR China; Hunan Key Laboratory for Bioanalysis of Complex Matrix Samples, Changsha Duxact Biotech Co., Ltd., Changsha 411000, PR China.

出版信息

Fitoterapia. 2020 Jan;140:104443. doi: 10.1016/j.fitote.2019.104443. Epub 2019 Nov 29.

DOI:10.1016/j.fitote.2019.104443
PMID:31790767
Abstract

Aucubin is an iridoid glycoside that is widely prevalent in traditional medicinal herbs, such as Eucommia ulmoides Oliv., Aucuba japonica Thunb. and Plantago asiatica L. This review aims to provide a comprehensive summary of the source, biological activity, pharmacokinetics and toxicology of aucubin with the ultimate objective of providing a guide for future drug development and potential clinical applications of aucubin. Aucubin is a highly active compound possessing extensive biological effects including antioxidant, anti-aging, anti-inflammatory, anti-fibrotic, anti-cancer, hepatoprotective, neuroprotective and osteoprotective properties. Although aucubin has been shown to have poor oral bioavailability in rats, aucubin is widely distributed in multiple organs including kidney, liver, heart, spleen and lung, and there is a sex difference in the absorption of aucubin. Tolerance of aucubin is good and no serious adverse reactions have been observed to date. In short, aucubin is a compound with abundant potential sources, good safety and numerous beneficial biological activities, which exhibits high potential value for use in health care products and pharmaceuticals. In order to accelerate the development and utilization of aucubin-related products, in-depth studies should be focused on the following questions of interest. First, it is necessary to introduce advanced separation and formulation technologies to improve the yield and stability of aucubin products. Second, studies should focus on the specific pharmacological activities of aucubin to determine the structure-activity relationship so as to improve the efficacy and reduce side effects. Finally, clinical studies are needed to confirm the efficacy of aucubin in specific diseases.

摘要

桃叶珊瑚苷是一种广泛存在于传统药用植物中的环烯醚萜苷,如杜仲、桃叶珊瑚和车前草。本综述旨在全面总结桃叶珊瑚苷的来源、生物活性、药代动力学和毒理学,以期为桃叶珊瑚苷的未来药物开发和潜在临床应用提供指导。桃叶珊瑚苷是一种具有广泛生物活性的高活性化合物,具有抗氧化、抗衰老、抗炎、抗纤维化、抗癌、保肝、神经保护和护骨作用。尽管桃叶珊瑚苷在大鼠体内的口服生物利用度较差,但桃叶珊瑚苷广泛分布于肾脏、肝脏、心脏、脾脏和肺部等多个器官,且桃叶珊瑚苷的吸收存在性别差异。桃叶珊瑚苷的耐受性良好,迄今为止尚未观察到严重的不良反应。总之,桃叶珊瑚苷是一种具有丰富潜在来源、良好安全性和多种有益生物活性的化合物,具有较高的应用于保健品和药品的潜在价值。为了加速桃叶珊瑚苷相关产品的开发和利用,应深入研究以下几个感兴趣的问题。首先,有必要引入先进的分离和制剂技术,以提高桃叶珊瑚苷产品的产量和稳定性。其次,应研究桃叶珊瑚苷的具体药理活性,确定构效关系,以提高疗效,减少副作用。最后,需要进行临床研究以确认桃叶珊瑚苷在特定疾病中的疗效。

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