Hydroxygenkwanin

Chem Biol Interact. 2013 Nov 25;206(2):346-55.

Synergistic anti-glioma effect of Hydroxygenkwanin and Apigenin in vitro.[Pubmed: 24144774]

Apigenin (AP) and Hydroxygenkwanin (HGK) are two natural flavonoid compounds. Previous studies have already demonstrated the anti-tumor capability of AP. However, it is not clear whether Hydroxygenkwanin has such property.
METHODS AND RESULTS:
In the current study, the anti-glioma activities of Hydroxygenkwanin and its synergistic anti-glioma effects with AP on C6 glioma cells were investigated. In addition, the possible mechanisms were also studied. MTT assay and morphologic analysis including acridine orange/ethidium bromide (AO/EB) and 4',6-diamidino-2-phenylindole (DAPI) staining were used in the research, and the results indicated that the treatment with AP or Hydroxygenkwanin could inhibit C6 glioma cell proliferation respectively. Moreover, when AP was administrated simultaneously, the anti-glioma effect of Hydroxygenkwanin was dramatically enhanced in a dose-dependent manner, which is obviously better than that of carmustine (BCNU) at the concentration 25μM for treating of 24h. Compared with control, mitochondrial membrane potential (MPP) loss and mitochondrion damage were detected by JC-1 fluorescence probes (JC-1) and transmission electron microscopy (TEM) after treatment. Obvious DNA damage and cell cycle S phase arrest were detected by alkaline comet assay and flow cytometric analysis (FCM). Additionally, up regulation of TNF-α level, activations of caspase-3, -8, over expressions of BID and BAK protein and BCL-XL protein down expression were also observed after treatment by the combination of AP and Hydroxygenkwanin .
CONCLUSIONS:
The results indicate that Hydroxygenkwanin may be an effective natural product to treat glioma, and the combination of AP and Hydroxygenkwanin may be a promising method for glioma chemotherapy.

Front Oncol . 2019 Sep 18;9:911.

Anticancer Effect and Mechanism of Hydroxygenkwanin in Oral Squamous Cell Carcinoma[Pubmed: 31620368]

Abstract The incidence and mortality of oral squamous cell carcinoma (OSCC) are high, and the number of oral cancers had risen in the world. However, chemotherapy drugs have numerous side effects. There is an urgent requirement to develop a novel drug that can be used to treat oral cancer. Hydroxygenkwanin (HGK) is a nature flavonoid extracted from Daphne genkwa Sieb. et Zucc. (Thymelaeaceae). Previous studies had demonstrated that HGK exhibits anticancer effect, but the effect is still unclear in oral cancer. HGK inhibited cell growth dose-dependently in SAS and OCEM1 cells. The functional enrichment analysis showed the significant pathway in cellular movement, cell cycle and cellular growth and proliferation. We further demonstrated the HGK induced the cell cycle arrest by flow cytometry and inhibited colony formation ability and cell movement. The western blot showed that HGK induced cell cycle arrest through p21 activation and caused intrinsic cell apoptosis pathway. HGK inhibited the cell invasion and migration through down-regulation vimentin. HGK might be an effective natural product for oral cancer therapy. Keywords: RNA sequencing; apoptosis; cell cycle; invasion; migration; oral cancer.