Abstract
The fruit of Arctium lappa L. (Arctii Fructus) is one of the most popularly used medicinal plant components in Asia. To enhance the functionality of Arctii Fructus extract, a bioconversion method was developed to produce arctigenin from arctiin. Treatment with β‐glucosidase increased the arctigenin content by >5 fold in Arctii Fructus extracts. The bioconversion products enhanced the apoptosis of cancer cells. The cell viabilities of gefitinib‐resistant lung cancer HCC827 (HCC827GR) cells and colon cancer cells (DLD1) were decreased by 40% and 35%, respectively. The bioconversion products also decreased anchorage‐independent growth of cancer cells. In addition, the increase of apoptosis in cancer cells by bioconversion was confirmed by the flow cytometry analysis. These results indicated that arctigenin exerts anticancer effects on lung and colon cancer cells and that Arctii Fructus can potentially function as a chemopreventive agent. In addition, bioconverted Arctii Fructus extract displayed higher anticancer activity than the same levels of purified arctigenin, indicating the advantage of consuming Arctii Fructus itself as a food or medicinal material.
Highlights
Arctium lappa L. contains various active compounds such as arctiin, arctigenin, tannins, lappaols, and diarctigenin (Chan et al, 2011)
We developed a method for the enzymatic bioconversion of arctiin to arctigenin, using β-glucosidase. β-glucosidase (E.C. 3.2.1.21) is an enzyme that catalyzes the hydrolysis of β-1,4-glycosidic linkages from the nonreducing ends of glycosides
40 μM isoliquiritigenin suppressed anchorage-independent growth by 40% in HCC827GR cells (Jung et al, 2014). These findings indicate that Arctii Fructus is more effective than these already known anticancer substances and support a role for arctigenin in suppressing cancer cell growth
Summary
Arctium lappa L. contains various active compounds such as arctiin, arctigenin, tannins, lappaols, and diarctigenin (Chan et al, 2011) These compounds are known to have antioxidant (Wu, Sun, et al, 2014), anti-inflammatory (Lee & Kim, 2010; Zhao, Wang, & Liu, 2009), antitumor (Awale et al, 2006), and antiproliferative (Ryu, Ahn, Kang, & Han, 1995) activities. We developed a method for the enzymatic bioconversion of arctiin to arctigenin, using β-glucosidase. Several previous reports have described enzymatic reactions that can be used to convert arctiin to arctigenin (Jung, Lee, Hyun, & Kim, 2012; Kim et al, 2010; Zhao et al, 2009) These reactions were not very efficient due to low substrate concentrations and long reaction times, probably caused by the low solubility of arctiin. The results confirmed the possibility of using Arctii Fructus as a source of anticancer materials, highlighting the possibility of increasing their functionality through enzymatic bioconversion
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