Du Zhiyong, Liu Zhenli, Ning Zhangchi, Liu Yuanyan, Song Zhiqian, Wang Chun, Lu Aiping
Institution of Basic Theory, China Academy of Chinese Medical Sciences, Beijing, China.
School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing Municipal Key Laboratory for Basic Research of Chinese Medicine, Beijing, China.
Planta Med. 2015 Mar;81(4):259-71. doi: 10.1055/s-0034-1396313. Epub 2015 Feb 25.
Boswellic acids have long been considered the main bioactive components of frankincense, and many studies in vitro and in animals as well as several clinical studies have confirmed their various bioactivities. In particular, a large number of mechanistic studies have confirmed their anti-inflammatory and antitumor activities. However, not every boswellic acid exhibits a satisfactory pharmacological performance, which depends on the chemical structure and functional groups of the acid. To enhance the pharmacological values of boswellic acids, derivatization has been specifically applied with the aim of discovering more active derivatives of BAs. In addition, the preliminary pharmacokinetic studies of these compounds using various standard methods show their poor bioavailability in humans and rodents, which has led to questions of their pharmacological relevance and potentially limits their use in clinical practice and pharmaceutical development. To improve these effects, some approaches have shown some improvements in effectiveness, and the new formula compatibility approach is considered a very reasonable method for improving the bioavailability of boswellic acids.
乳香酸长期以来一直被认为是乳香的主要生物活性成分,许多体外、动物实验研究以及多项临床研究都证实了它们的各种生物活性。特别是,大量的机制研究证实了它们的抗炎和抗肿瘤活性。然而,并非每种乳香酸都表现出令人满意的药理性能,这取决于该酸的化学结构和官能团。为了提高乳香酸的药理价值,人们专门采用了衍生化方法,旨在发现更多活性更高的乳香酸衍生物。此外,使用各种标准方法对这些化合物进行的初步药代动力学研究表明,它们在人和啮齿动物中的生物利用度较差,这引发了对其药理相关性的质疑,并可能限制它们在临床实践和药物开发中的应用。为了改善这些效果,一些方法已显示出在有效性方面有所改进,而新的配方配伍方法被认为是提高乳香酸生物利用度的一种非常合理的方法。