Research Institute of Bioactive-Metabolome Network, Konkuk University, Seoul 05029, Korea.
Forest Plant Industry Department, Baekdudaegan National Arboretum, Bonghwa 36209, Korea.
Int J Mol Sci. 2020 Feb 11;21(4):1207. doi: 10.3390/ijms21041207.
Platycosides, the saponins abundant in Platycodi radix (the root of ), have diverse pharmacological activities and have been used as food supplements. Since deglycosylated saponins exhibit higher biological activity than glycosylated saponins, efforts are on to enzymatically convert glycosylated platycosides to deglycosylated platycosides; however, the lack of diversity and specificities of these enzymes has limited the kinds of platycosides that can be deglycosylated. In the present study, we examined the enzymatic conversion of platycosides and showed that Cytolase PCL5 completely converted platycoside E and polygalacin D3 into deapiose-xylosylated platycodin D and deapiose-xylosylated polygalacin D, respectively, which were identified by LC-MS analysis. The platycoside substrates were hydrolyzed through the following novel hydrolytic pathways: platycoside E → platycodin D3 → platycodin D → deapiosylated platycodin D → deapiose-xylosylated platycodin D; and polygalacin D3 → polygalacin D → deapiosylated polygalacin D → deapiose-xylosylated polygalacin D. Our results show that cytolast PCL5 may have a potential role in the development of biologically active platycosides that may be used for their diverse pharmacological activities.
远志皂苷,大量存在于桔梗(桔梗根)中的皂苷,具有多种药理活性,并被用作膳食补充剂。由于去糖基皂苷比糖基皂苷具有更高的生物活性,因此人们一直在努力通过酶促转化将糖基远志皂苷转化为去糖基远志皂苷;然而,这些酶的多样性和特异性的缺乏限制了可去糖基化的远志皂苷的种类。在本研究中,我们研究了远志皂苷的酶促转化,并表明 Cytolase PCL5 可将远志皂苷 E 和远志山酮 D3 分别完全转化为去表阿糖基-木糖基远志皂苷 D 和去表阿糖基-木糖基远志山酮 D,通过 LC-MS 分析鉴定。通过以下新型水解途径水解远志皂苷底物:远志皂苷 E→远志山酮 D3→远志山酮 D→去表阿糖基远志山酮 D→去表阿糖基-木糖基远志山酮 D;和远志山酮 D3→远志山酮 D→去表阿糖基远志山酮 D→去表阿糖基-木糖基远志山酮 D。我们的结果表明 Cytolase PCL5 可能在具有多种药理活性的生物活性去糖基远志皂苷的开发中具有潜在作用。