Transformation of Bioactive Compounds by Fusarium sacchari Fungus Isolated from the Soil-Cultivated Ginseng

Abstract

Ginsenoside bioactive compounds, namely, compound K (C-K), compound Mx (C-Mx), and ginsenoside Mc (G-Mc), were the metabolites of ginsenosides Rb 1, Rb 2, Rb 3, and Rc by intestinal microflora of humans or rats, microorganisms, and enzymes, and C-K showed beneficial effects in vitro and in vivo as an antitumoral agent. The objective of this work was to explore an efficient procedure for biotransformation of these bioactive compounds. Thus, a filamentous fungus, Fusarium sacchari, was first obtained from the soil-cultivated ginseng, which was verified to possess a potent capacity of transformation of C-K, C-Mx, and G-Mc. The optimal biotransformation conditions of F. sacchari with C-K, C-Mx, and G-Mc were obtained as follows: transforming temperature, 30 degrees C; transforming time, 6 days; rotary speed, 160 rpm; pH of the medium, 5.5. HPLC analysis indicated that these three bioactive compounds were key metabolites and their structures were confirmed by (1)H and (13)C NMR analysis. Moreover, the in vitro antitumor activities of C-K, C-Mx, and G-Mc and the in vivo antitumor activities of the transformed product mainly containing these compounds were also evaluated. Among C-K, C-Mx, and G-Mc, C-K exhibited the most potent antitumor activities. The in vivo study showed that the transformed products by F. sacchari had much more antitumor activity than those of commonly used ginsenoside Rg3 and Paclitaxel.

Production of the Rare Ginsenosides Compound K, Compound Y, and Compound Mc by a Thermostable .BETA.-Glycosidase from Sulfolobus acidocaldarius

“…13) b-Glycosidase from S. acidocaldarius utilized three path- The reactions were performed using 10% (w/v) ginseng root extract in 50 mM citrate buffer (pH 5.5) at 85°C with 30 U/ml enzyme for 24 h. Data represent the means of three experiments and error bars represent standard deviation.…”

Simultaneous Enrichment of Deglycosylated Ginsenosides and Monacolin K in Red Ginseng by Fermentation withMonascus pilosus

“…Other approaches have been adopted involving fermentation with intestinal bacteria such as Bifidobacterium 25) or lactic acid bacteria, 26) but these methods require expensive media and result in low yields and poor productivity. 16) Several reports have stated that ginsenosides can be converted by fungal strains such as Rhizopus stolonifer, 27) Aspergillus niger, 28) Fusarium sacchari, 29) and Curvularia lunata, 27) but many of these fungi are not generally regarded as safe, which limits their application in foods.…”

Targeted delivery of ginsenoside compound K using TPGS/PEG-PCL mixed micelles for effective treatment of lung cancer

“…After the size of the tumors reached 60 mm 3 , DiR-loaded micelles were injected into the blood stream via the tail vein of the tumor-bearing mice at a dose of 5 mg/kg. Following anesthetization, the mice were imaged at 0, 1, 2, 4, 6, 8, and 24 h.…”

“…When the tumor size reached 60 mm 3 , the male athymic nude mice (22±2 g) were randomly divided into four groups (n=6): control group for treatment with saline solution, positive control group for treatment with cisplatin (2 mg/kg), and one each for treatment with CK (15 mg/kg) and CK-M (15 mg/kg) solutions. Mice were injected with the treatment drug through the tail vein one time every 3 days for 15 days.…”

“…1,2 Furthermore, CK was the strongest antitumor agent of the ginsenosides. 3 Various tumor cells are inhibited by CK, including human colorectal cancer cells, human hepatoblastoma HepG2 cells, human breast cancer MCF-7 cells, and lung adenocarcinoma A549 cells. [4][5][6] CK acts by various antitumor mechanisms including inhibition of tumor cell proliferation, promotion of tumor cell apoptosis, and inhibition of tumor cell invasion and metastasis.…”