Wighteone

HSP90 expression and its association with wighteone metabolite response in HER2-positive breast cancer cells.[Pubmed:27313682]

Oncol Lett. 2016 Jun;11(6):3719-3722.

It is well known that heat shock protein 90 (HSP90) overexpression is correlated with poor prognosis and chemo-resistance in human malignant cancers. At the same time, Wighteone, or 6-prenyl-5,7,4'-trihydroxyisoflavone, a major isoflavone component of the ornamental tall tree Erythrina suberosa, has been demonstrated to exhibit a potent anti-proliferative effect on human leukemia HL-60 cancer cell lines. In this study, the effects of Wighteone on the proliferation of HER2-positive breast cancer cells were investigated, and the action mechanism was explored. MCF-7 HER2-positive breast cancer cells were treated with various concentrations of Wighteone. The growth inhibitory rate of the cells was calculated by MTT assay, apoptosis was detected by flow cytometry, and the expression level of HSP90 was assessed by western blot analysis. The addition of Wighteone at concentrations ranging from 1-10 g/ml in the medium for 48 h had a marked inhibition on the proliferation of HER2-positive cancer cell lines. The growth inhibitory rates with 0.5, 2 or 8 mM Wighteone were significantly higher compared with the control group. Apoptosis in the Wighteone-treated cells was also significantly higher compared with the control group. The expression level of HSP90 in the Wighteone group was significantly lower than that in the control group. Our findings demonstrated that Wighteone effectively inhibited the proliferation of HER2-positive cancer cell lines, and this is considered to be the result of downregulating HSP90 receptor and downstream signaling.

Cytotoxic isoflavones from Erythrina indica.[Pubmed:11730876]

Phytochemistry. 2001 Dec;58(7):1113-20.

Bioassay-directed fractionation of the CH(2)Cl(2)-MeOH (1:1) extract of the stem bark of Erythrina indica, has resulted in the isolation of two new isoflavone derivatives named indicanines D and E together with 11 known compounds including: six isoflavones (genistein, Wighteone, alpinumisoflavone, dimethylalpinumisoflavone, 8-prenyl erythrinin C, and erysenegalensein E), one cinnamate (erythrinassinate B), two pentacyclic triterpenes (oleanolic acid and erythrodiol), and two phytosterols (stigmasterol and its 3-O-beta-D-glucopyranoside). The structures of the new compounds were elucidated by means of spectroscopic analysis. The in vitro cytocidal activity against KB cells of some of the isolated compounds is also reported.

Genome-wide analysis of the expression profile of Saccharomyces cerevisiae in response to treatment with the plant isoflavone, wighteone, as a potential antifungal agent.[Pubmed:16369693]

Biotechnol Lett. 2006 Jan;28(2):99-105.

The limitations of currently available antifungal agents and the rapid emergence of drug-resistant strains necessitate more efficient approaches to screening and developing novel antifungal drugs. The antifungal activity of the natural products of a series of plants was evaluated and Wighteone, 5, 7, 4'-trihydroxy-6-(gamma,gamma-dimethylallyl)isoflavone showed excellent anti-yeast activity (MIC against Saccharomyces cerevisiae was 4 microg/ml). Transcriptome profiling of Wighteone-treated S. cerevisiae indicated that Wighteone is different from commonly used antifungal compounds in its mode of action.