Department of Environmental and Plant Protection, University of Agricultural Sciences and Veterinary Medicine Cluj-Napoca, Calea Mănăştur 3-5, 400372 Cluj-Napoca, Romania.
Faculty of Chemistry and Chemical Engineering, Babeș-Bolyai University of Cluj-Napoca, Arany János 11, 400028 Cluj-Napoca, Romania.
Int J Mol Sci. 2022 Jul 7;23(14):7519. doi: 10.3390/ijms23147519.
In recent years, there has been considerable interest in icariin (ICA) and its derivates, icariside II (ICS) and icaritin (ICT), due to their wide range of potential applications in preventing cancer, cardiovascular disease, osteoporosis, delaying the effects of Alzheimer's disease, treating erectile dysfunction, etc. However, their poor water solubility and membrane permeability, resulting in low bioavailability, dampens their potential beneficial effects. In this regard, several strategies have been developed, such as pharmaceutical technologies, structural transformations, and absorption enhancers. All these strategies manage to improve the bioavailability of the above-mentioned flavonoids, thus increasing their concentration in the desired places. This paper focuses on gathering the latest knowledge on strategies to improve bioavailability for enhancing the efficacy of icariin, icariside II, and icaritin. We conclude that there is an opportunity for many further improvements in this field. To the best of our knowledge, no such review articles scoping the bioavailability improvement of icariin and its derivates have been published to date. Therefore, this paper can be a good starting point for all those who want to deepen their understanding of the field.
近年来，淫羊藿素（ICA）及其衍生物淫羊藿次苷 II（ICS）和淫羊藿苷（ICT）因其在预防癌症、心血管疾病、骨质疏松症、延缓阿尔茨海默病的影响、治疗勃起功能障碍等方面的广泛应用潜力而引起了相当大的兴趣。然而，它们较差的水溶性和膜透过性导致生物利用度低，从而抑制了它们的潜在有益作用。在这方面，已经开发了几种策略，如药物技术、结构转化和吸收增强剂。所有这些策略都设法提高了上述类黄酮的生物利用度，从而增加了它们在所需部位的浓度。本文重点收集了提高生物利用度以增强淫羊藿素、淫羊藿次苷 II 和淫羊藿苷功效的最新知识。我们得出的结论是，在这一领域还有许多进一步改进的机会。据我们所知，迄今为止，还没有专门针对淫羊藿素及其衍生物生物利用度提高的综述文章。因此，本文可以作为所有希望深入了解该领域的人的一个良好起点。
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