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PLoS One. 2018 May 17;13(5):e0197563. doi: 10.1371/journal.pone.0197563. eCollection 2018.

Antitumor, antioxidant and anti-inflammatory activities of kaempferol and its corresponding glycosides and the enzymatic preparation of kaempferol.

Wang J1,2, Fang X1,2, Ge L1,2, Cao F1,2, Zhao L2,3, Wang Z4, Xiao W4.

Author information

Co-Innovation Center for Sustainable Forestry in Southern China, Nanjing Forestry University, Nanjing, China.
College of Chemical Engineering, Nanjing Forestry University, Nanjing, China.
Jiangsu Key Lab for the Chemistry & Utilization of Agricultural and Forest Biomass, Nanjing, China.
Jiangsu Kanion Pharmaceutical Co., Ltd., Lianyungang, China.


Kaempferol (kae) and its glycosides are widely distributed in nature and show multiple bioactivities, yet few reports have compared them. In this paper, we report the antitumor, antioxidant and anti-inflammatory activity differences of kae, kae-7-O-glucoside (kae-7-O-glu), kae-3-O-rhamnoside (kae-3-O-rha) and kae-3-O-rutinoside (kae-3-O-rut). Kae showed the highest antiproliferation effect on the human hepatoma cell line HepG2, mouse colon cancer cell line CT26 and mouse melanoma cell line B16F1. Kae also significantly inhibited AKT phosphorylation and cleaved caspase-9, caspase-7, caspase-3 and PARP in HepG2 cells. A kae-induced increase in DPPH and ABTS radical scavenging activity, inhibition of concanavalin A (Con A)-induced activation of T cell proliferation and NO or ROS production in LPS-induced RAW 264.7 macrophage cells were also seen. Kae glycosides were used to produce kae via environment-friendly enzymatic hydrolysis. Kae-7-O-glu and kae-3-O-rut were hydrolyzed to kae by β-glucosidase and/or α-L-rhamnosidase. This paper demonstrates the application of enzymatic catalysis to obtain highly biologically active kae. This work provides a novel and efficient preparation of high-value flavone-related products.

[Indexed for MEDLINE]
Free PMC Article

Conflict of interest statement

The authors declare the following interests: Zhenzhong Wang and Wei Xiao are employed by Jiangsu Kanion Pharmaceutical Co., Ltd. This study was funded in part by Jiangsu Kanion Pharmaceutical Co., Ltd. There are no patents, products in development or marketed products to declare. This does not alter our adherence to all the PLOS ONE policies on sharing data and materials. The authors confirm there are no other interests to declare.

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