Multidrug-resistant human cancer cell

Fiucci G, Czarny M, Lavie Y, Zhao D, Berse B, Blusztajn JK, Liscovitch M (2000) Changes in phospholipase D isoform activity and expression in multidrug-resistant human cancer cells. Int J Cancer 85 882-888... 

Analogs 38 were tested for their ability to promote in vitro tubulin polymerization, and their antiproliferative activity was assessed against the human epidermoid cancer cell lines KB-31 and KB-8511, which serve as representative examples of drug-sensitive and P-gp-overexpressing, multidrug-resistant human cancer cell lines, respectively (see, e.g.. Refs. 20 and 37). 

K Osann, P Sweet, LM Slater. (1992). Synergistic action of cyclosporin A and verapamil on vincristine and daunorubicin resistance in multidrug-resistant human leukemia cells in vitro. Cancer Chemother Pharmacol 30 152-154. 

Zaman GJ, Versantvoort CH, Smit JJ, et al. Analysis of the expression of MRP, the gene for a new putative transmembrane drug transporter, in human multidrug resistant lung cancer cell lines. Cancer Res 1993 53 1747-1750. 

The hatomarubigins, isolated from Streptomyces sp. 2238-SVT4, are antitumor antibiotics which enhance the cytotoxicity of colchicine against multidrug-resistant KB cancer cells (human squamous cell carcinoma) [142, 143], Structures 202 - 204 show a rare 11-OH group hatomarubigin C (203) is a reduc-... 

Cole SPC, Bhardwaj G, Gerlach J, Mackie J, Grant C, Almquist K et al. Overexpression of a transporter gene in a multidrug-resistant human lung cancer cell line. Science 1992 258 1650-1654. 

Lavie, Y., Cao, H-t., Volner, A., Lucci, A., Han, T. Y., Geffen, V., Giuhano, A. E., and Cabot, M. C., 1997, Agents that reverse multidrug resistance, tamoxifen, verapamil, and cyclosporin A, block glycosphingolipid metabohsm by inhibiting ceramide glycosylation in human cancer cells. J. Biol. Chem. 272 1682-1687. 

Bell SE, Quinn DM, Kellett GL, Warr JR (1998) 2-Deoxy-D-glucose preferentially kills multidrug-resistant human KB carcinoma cell lines by apoptosis. Br J Cancer 78 1464-1470... 

Scaglione-Sewell B, Abraham C, Bissonnette M, Skarosi SF, Hart J, Davidson NO, Wali RK, Davis BH, Sitrin M, Brasitus TA (1998) Decreased FKC alpha expression increases cellular proliferation, decreases differentiation, and enhances the transformed phenotype of CaCo-2 cells. Cancer Res 58 1074-1081 Scala S, Dickstein B, Regis J, Szallasi Z, Blumberg PM, Bates SE (1995) Bryostatin 1 affects P-glycoprotein phosphorylation but not function in multidrug-resistant human breast cancer cells. Clinical Cancer Res 1 15851-1587 Scanlon, KJ, Kashani-Sabet M, Tone T, Funato T (1991) Cisplatin resistance in human acancers. Pharmac Ther 52 385-406... 

Ward NE, O Brian CA (1991) Distinct patterns of phorbol ester-induced downr -lation of protein kinase C activity in adriamycin-selected multidrug resistant and parental murine fibrosarcoma cells. Cancer Lett 58 189-193 Warenius HM, Seabra LA, Maw P (1996) Sensitivity to cis-diamminedichloro-platinum in human cancer cells is related to ejq>ression of cyclin D1 but not c-raf-1 protein. Int J Cancer 67 224-231... 

Lavie, Y, Harel-Orbital, T., Gaffield, W., Liscovitch, M. (2001). Inhibitory effect of steroidal alkaloids on drug transport and multidrug resistance in human cancer cells. Anticancer Res., 21, 1189-1194. 

Oberlies, N.H., Croy, V.L., Harrison, M.L., and McLaughlin, J.L. The Annonaceous acetogenins are cytotoxic against multidrug-resistant human mammary adenocarcinoma cells. Cancer Lett., 115, 73, 1997b. 

The in vitro antitumor activity of curcumin in HPV-associated cells has been established [Roy et al., 2002]. Curcumin modulates the in vitro expression and function of Pgp in multidrug-resistant human KB-V1 cells [Anand et al., 2008 Chearwae et al., 2004] and sensitizes cisplatin-resistant SiHa cells to cisplatin-induced apoptosis [Venkatraman et al., 2005], indicating its ability to reverse MDR in cervical cancer cells. The effect of curcumin in HPV-associated cells was found to involve the down-regulation of viral oncogenes, NF-kB and AP-1 [Anand et al., 2008 Divya and Pillai, 2006],... 

The choice of a cell line to study MDR modulator potency was very important for future potential application in human cancer treatment. PhM (12) that were quite effective in resistant mouse lymphoma cells were only slightly active in drug-resistant human sarcoma cell line MES-SA/Dx5 [198]. The drug-sensitive human sarcoma cell line MES-SA and its multidrug-resistant counterpart MES-SA/Dx5 were applied as a model system for evaluation of MDR modulator activities. Examination performed by the flow cytometric Rhl23 accumulation test demonstrated that the well-known P-gp modulators verapamil (79) and TFP (5) reduced MDR in MES-SA/Dx5 cells. In resistant MES-SA/Dx5 cells, verapamil (79) and TFP (5) restored the drug accumulation pattern which was typical for sensitive cells. However, the effectiveness of PhM (12) was very low. The most active compounds were derivatives with an H atom at position 2 of the phenothiazine ring, followed by Cl-substituted and CF3-substituted compounds. 

U. Stein, W. Walther, and R. H. Shoemaker, Vincristine induction of mutant and wild-type human multidrug-resistance promoters is cell-type-specific and dose-dependent, J. Cancer Res. Clin. Oncol. 722 275 (1996). 

---