PD153035 is a ATP-competitive EGFR inhibitor with an IC50 and Ki of 25 and 6 pM. PD153035 effectively blocks the enhancement of mitogenesis, induction of early gene expression, and oncogenic transformation that occur in response to EGF receptor stimulation. With human fibroblasts and epidermoid carcinoma cells, PD153035 at nanomolar concentrations rapidly inhibits EGFR autophosphorylation. With breast and ovarian cancer cells, PD153035 not only blocks cell growth via inhibition of EGFR, but also upregulates the expression of the tumor suppressor retinoic acid receptor-beta 2 (RAR-beta2).
6-O-Nicotinoylscutebarbatine G shows cytotoxic activities against three human tumor cell lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, and with IC50 values in the range of 2.1 5.7 μM.
Aglinin A displays moderate cytotoxicity against all the three cancer cell lines((NCI-H187), epidermoid carcinoma (KB) and breast cancer (BC) cell lines).
Dehydrovomifoliol could be a marker of Polish heather honey. Dehydrovomifoliol exhibits moderate acetylcholinesterase (AChE) inhibitory activities. Dehydrovomifoliol shows significant cytotoxic activities against three human cancer cell lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, and the IC(50) values in the range 3.7-8.1 microM.
Heliangin shows anti-inflammatory effects, it can inhibit lipopolysaccharide-induced inflammation through signaling NF-κB pathway on LPS-induced RAW 264.7 cells. Heliangin has anti-cancer activity, it exhibits cytotoxicity against human oral epidermoid (
Taiwanhomoflavone A is cytotoxic with ED50 values of 3.4, 1.0, 2.0 and 2.5 microg/ml, respectively, against KB epidermoid carcinoma of nasopharynx, COLO-205 colon carcinoma, Hepa-3B hepatoma, and Hela cervix tumor cells.
Taiwanhomoflavone B is cytotoxic with ED(50) values of 3.8 and 3.5 microg/ml, against KB oral epidermoid carcinoma and Hepa-3B hepatoma cells, respectively.
Streptimidone, a metabolite produced by Streptomyces, exhibits various biological activities, including inhibiting protein synthesis at 50 µg/ml in cell-free assays and reducing tumor growth in rat xenograft models of H.S. No. 1 human sarcoma and H.Ep. No. 3 human epidermoid carcinoma at daily doses of 12.5 and 25 mg/kg.