College of Pharmacy, Shandong University of Traditional Chinese Medicine, 4655 Daxue Road, Jinan 250355, China.
Molecules. 2021 Dec 22;27(1):51. doi: 10.3390/molecules27010051.
Toad venom contains a large number of bufadienolides, which have a variety of pharmacological activities, including antitumor, cardiovascular, anti-inflammatory, analgesic and immunomodulatory effects. The strong antitumor effect of bufadienolides has attracted considerable attention in recent years, but the clinical application of bufadienolides is limited due to their low solubility and poor bioavailability. In order to overcome these shortcomings, many strategies have been explored, such as structural modification, solid dispersion, cyclodextrin inclusion, microemulsion and nanodrug delivery systems, etc. In this review, we have tried to summarize the pharmacological activities and structure-activity relationship of bufadienolides. Furthermore, the strategies for solubility and bioavailability enhancement of bufadienolides also are discussed. This review can provide a basis for further study on bufadienolides.
蟾蜍毒液中含有大量的蟾毒配基，具有多种药理活性，包括抗肿瘤、心血管、抗炎、镇痛和免疫调节作用。蟾毒配基的强烈抗肿瘤作用近年来引起了相当大的关注，但由于其溶解度低和生物利用度差，蟾毒配基的临床应用受到限制。为了克服这些缺点，已经探索了许多策略，如结构修饰、固体分散体、环糊精包合、微乳液和纳米药物传递系统等。在这篇综述中，我们试图总结蟾毒配基的药理活性和构效关系。此外，还讨论了提高蟾毒配基溶解度和生物利用度的策略。这篇综述可以为进一步研究蟾毒配基提供依据。
