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

• Published in: PloS one 2018-05, Vol.13 (5), p.e0197563-e0197563
• Main Authors: Wang, Jingqiu, Fang, Xianying, Ge, Lin, Cao, Fuliang, Zhao, Linguo, Wang, Zhenzhong, Xiao, Wei
• Format: Article
• Language: English
• Subjects: AKT protein; Animals; Anti-inflammatory agents; Anti-Inflammatory Agents - pharmacology; Anticancer properties; Antineoplastic Agents, Phytogenic - pharmacology; Antioxidants; Antioxidants (Nutrients); Antioxidants - pharmacology; Apoptosis; Apoptosis - drug effects; beta-Glucosidase - metabolism; Biological activity; Biology and Life Sciences; Biotechnology; Cancer; Cancer cells; Caspase; Caspase-3; Caspase-7; Caspase-9; Catalysis; Cell activation; Cell Division - drug effects; Cell Line, Tumor; Cell proliferation; Chemical engineering; Colon; Colon cancer; Concanavalin A; Drug Evaluation, Preclinical; Enzymes; Fibroblasts; Flavonoids; Forestry; Free Radicals; Glucosidase; Glucosides - pharmacology; Glycoside Hydrolases - metabolism; Glycosides; Glycosides - pharmacology; Hepatoma; Humans; Hydrolysis; Inflammation; Kaempferol; Kaempferols - isolation & purification; Kaempferols - pharmacology; Kinases; L-Rhamnosidase; Lipopolysaccharides; Lymphocyte Activation - drug effects; Lymphocytes T; Macrophages; Medicine and Health Sciences; Melanoma; Methods; Mice; Nitric oxide; Nitric Oxide - metabolism; Phosphorylation; Physical Sciences; Poly(ADP-ribose) polymerase; Potassium; Properties; Proteins; Reactive Oxygen Species - metabolism; Recombinant Proteins - metabolism; Research and analysis methods; Rodents; Tumor necrosis factor-TNF; Zingiberaceae
• ISSN: 1932-6203; 1932-6203
• DOI: 10.1371/journal.pone.0197563

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.