epidermoid carcinoma

PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin.

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

Antiproliferative agent-60 (compound 8c), an 11-Azaartemisinin derivative, exhibits outstanding anticancer activity. It demonstrates tumor selectivity up to 32 times higher when compared to normal Hek293 cells. The IC50 values for Antiproliferative agent-60 are 7.7 μM for epidermoid carcinoma (KB), 42.5 μM for HepG2, and 15.5 μM for A549 cells.

Panduratin A is a natural chalcone derivative with inhibitory activity against MMP-9 in human oral epidermoid carcinoma KB cells; inhibitory activity against the NS3 protease of DENV-2 (Ki=25 μM); significant cytotoxicity against human androgen-independent prostate cancer cells PC-3 and DU-145; and also able to activate the LKB1-AMPK- PPARα /δ signaling pathway and enhance the oxidative capacity of myocyte mitochondria.

(E)-AG 99 ((E)-Tyrphostin AG 99) is an EGFR kinase inhibitor with an IC50 of 10 μM in the human epidermoid carcinoma cell line A431.

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).

11-epi-Chaetomugilin I, a metabolite identified in Chaetomium globosum, demonstrates notable cytotoxic activity against several cell lines, including the murine P388 and L1210 leukemia cell lines, the human HL-60 leukemia cell line, and the human KB epidermoid carcinoma cell line [1].

Chaetoglobosin F is a cytochalasin-type alkaloid derived from Chaetomium globosum. It exhibits cytotoxic properties against human nasopharyngeal epidermoid carcinoma cells (KB), with an IC50 value of 52.0 µM.

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.