Yang Eun-Joo, Kim Tae-Hun, Shin Kyung-Chul, Oh Deok-Kun
Department of Bioscience and Biotechnology, Konkuk University, Seoul, 05029, Republic of Korea.
AMB Express. 2018 Jan 24;8(1):8. doi: 10.1186/s13568-018-0543-1.
Aglycon protopanaxatriol (APPT) has valuable pharmacological effects such as anti-inflammatory and anti-stress activities. However, the complete conversion of all typical glycosylated protopanaxatriol ginsenosides to APPT has not been achieved to date. β-Glycosidase from the hyperthermophilic bacterium Dictyoglomus turgidum (DT-bgl) hydrolyzes the glucose residues at C-6 and the inner glucose at C-20 in protopanaxatriol (PPT), but not the outer rhamnose residues at C-6. In contrast, β-glycosidase from the hyperthermophilic bacterium Pyrococcus furiosus (PF-bgl) hydrolyzes the outer rhamnose residue at C-6 but not the inner glucose residues at C-6 and C-20 in PPT. Thus, the combined use of DT-bgl and PF-bgl resulted in the complete the conversion of all typical glycosylated PPT ginsenosides, including R1, R2, Re, Rg1, Rg2, Rh1, Rf, F1, F3, and F5, to APPT. DT-bgl combined with PF-bgl completely hydrolyzed 1.0 mg ml R1 and 1.0 mg ml total PPT-type ginsenosides in Panax notoginseng root extract to 0.5 and 0.63 mg ml APPT for 4 and 3 h, with molar conversions of 100% and productivities of 125 and 210 mg l h, respectively. To the best of our knowledge, this is the first report of the complete conversion of all typical glycosylated PPT ginsenosides to APPT and the highest productivity of APPT obtained from ginseng extract achieved to date.
原人参三醇苷元(APPT)具有抗炎和抗应激等重要药理作用。然而,迄今为止,所有典型的糖基化原人参三醇人参皂苷尚未完全转化为APPT。来自嗜热细菌膨胀网柄菌(DT-bgl)的β-糖苷酶可水解原人参三醇(PPT)中C-6位的葡萄糖残基和C-20位的内部葡萄糖,但不能水解C-6位的外部鼠李糖残基。相比之下,来自嗜热栖热菌(PF-bgl)的β-糖苷酶可水解PPT中C-6位的外部鼠李糖残基,但不能水解C-6和C-20位的内部葡萄糖残基。因此,联合使用DT-bgl和PF-bgl可使包括R1、R2、Re、Rg1、Rg2、Rh1、Rf、F1、F3和F5在内的所有典型糖基化PPT人参皂苷完全转化为APPT。DT-bgl与PF-bgl联合使用,在4小时和3小时内,可将三七根提取物中1.0mg/ml的R1和1.0mg/ml的总PPT型人参皂苷分别完全水解为0.5mg/ml和0.63mg/ml的APPT,摩尔转化率为100%,生产率分别为125mg·l·h和210mg·l·h。据我们所知,这是首次报道所有典型糖基化PPT人参皂苷完全转化为APPT,也是迄今为止从人参提取物中获得的APPT的最高生产率。