Highly Efficient Biotransformation of Notoginsenoside R1 into Ginsenoside Rg1 by Dictyoglomus thermophilum β-xylosidase Xln-DT

Abstract

Notoginsenoside R1 and ginsenoside Rg1 are the main active ingredients of Panax notoginseng, exhibiting anti-fatigue, anti-tumor, anti-inflammatory, and other activities. In a previous study, a GH39 β-xylosidase Xln-DT was responsible for the bioconversion of saponin, a natural active substance with a xylose group, with high selectivity for cleaving the outer xylose moiety of notoginsenoside R1 at the C-6 position, producing ginsenoside Rg1 with potent anti-fatigue activity. The optimal bioconversion temperature, pH, and enzyme dosage were obtained by optimizing the transformation conditions. Under optimal conditions (pH 6.0, 75 o C, enzyme dosage 1.0 U/ml), 1.0 g/l of notoginsenoside R1 was converted into 0.86 g/l of ginsenoside Rg1 within 30 min, with a molar conversion rate of approximately 100%. Furthermore, the in vivo anti-fatigue activity of notoginsenoside R1 and ginsenoside Rg1 were compared using a suitable rat model. Compared with the control group, the forced swimming time to exhaustion was prolonged in mice by 17.3% in the Rg1 high group (20 mg/kg•d). Additionally, the levels of hepatic glycogen (69.9-83.3% increase) and muscle glycogen (36.9-93.6% increase) were increased. In the Rg1 group, hemoglobin levels were also distinctly increased by treatment concentrations. Our findings indicate that treatment with ginsenoside Rg1 enhances the anti-fatigue effects. In this study, we reveal a GH39 βxylosidase displaying excellent hydrolytic activity to produce ginsenoside Rg1 in the pharmaceutical and food industries.

Streptomyces albidoflavus Q antifungal metabolites inhibit the ergosterol biosynthesis pathway and yeast growth in fluconazole-resistant Candida glabrata : phylogenomic and metabolomic analyses

“…Notoginsenoside J (compound 6), the other S. albidoflavus Q metabolite identified as a potential antifungal agent, has been previously evaluated for antioxidant ( 40 ), anti-tumor, anti-fatigue, anti-inflammatory ( 41 ), and anti-atherosclerosis activities ( 42 ). However, the molecular target of notoginsenoside is unknown ( 43 ).…”

Natural products of pentacyclic triterpenoids: from discovery to heterologous biosynthesis

“…73 Ginsenosides have many effects such as anti-fatigue, anti-tumor, antiaging, and anti-oxidant. 74 2.3.2 Anti-cardiovascular and cerebrovascular disease and cholesterol-lowering effects. Cardiovascular and cerebrovascular diseases are mainly caused by hypertension, diabetes, and dyslipidemia syndrome, which are manifested as ischemic or hemorrhagic lesions in the brain, heart and whole body.…”

“…73 Ginsenosides have many effects such as anti-fatigue, anti-tumor, anti-aging, and anti-oxidant. 74…”

Pharmacokinetics study of ginsenoside Rg1 liposome by pulmonary administration

“…Ginsenoside Rg1 (Rg1, Fig. 1 ) is one of the most abundant components in Panaxnotoginseng saponins [ 2 ], and it is also a pharmacologically active component for clinical application. Ginsenoside Rg1 is a monomer saponin extracted from Panaxnotoginseng, which is dammarane-type saponin [ 3 ].…”