Cancer cell lines

WS-7528 [132147-69-4][VI] a nonsteroidal estrogen, is an isoflavone which has been isolated from Streptomjces sp. No. 7528 and is an estrogen agonist. It inhibits [3ff]-estradiol binding to its receptor in rat uterine cytosol at an inhibitor for 50% of the rats tested (IC q) concentration of 5.7 nM. It also induces the growth of estrogen-dependent human breast cancer cell line MCE-7 (7). 

Hsu J-T, Ying C, Lan H-C. 1998. The effects of pesticides chlordane, dieldrin and endosulfan on the growth of human breast cancer cell lines MCF-7 and SK-BR-3. J Chinese Agri Chem Soc 36(6) 535-546. 

Legler J, van den Brink C, Brouwer A, et al. 1998. Assessment of (anti-)estrogenic compounds using a stably transfected luciferase reporter gene assay in the human T47-D breast cancer cell line. Organohalogen Compounds 37 265. 

LUND E K, SMITH T K, CLARKE R G and JOHNSON I T (2001) Cell death in the colorectal cancer cell line HT29 in response to glucosinolate metabolites , J i FoodAgric, 81 959-61. 

HASHIMOTO S, XU M, MASUDA Y, AIUCHI T, NAKAJO S, CAO J, MIYAKOSHI M, IDA Y and NAKAYA K (1999) Beta-hydroxyisovalerylshikonin inhibits the cell growth of various cancer cell lines and induces apoptosis in leukemia HL-60 cells through a mechanism different from those of Fas and etoposide , J Biochem (Tokyo), 125 17-23. 

TWADDLE G M, TURBOV J, LIU N, MURTHY s (1999) Tyrosine kinase inhibitors as antiprohferative agents against estrogen-dependent breast cancer cell line in vitro. JSurg Oncol. 70 ... 

YANAGIHARA K, ITO A, TOGE T, NUMOTO M (1993) Antiprolferative effects of isoflavones on human cancer cell lines established from gastrointestinal tract. Cancer Res. 53 5815-21. 

OKABE s, SUGANUMA M, HAYASHi M, SUEOKA E, KOMORI A and FUJIKI H (1997) Mechanisms of growth inhibition of hmnan lung cancer cell line, PC-9, by tea polyphenols , Jpn J Cancer Res, 88 (7), 639-43. 

PASCHKA A G, BUTLER R and YOUNG c Y (1998) luductiou of apoptosis in prostate cancer cell lines by the green tea component, (-)-epigallocatechin-3-gallate . Cancer Lett, 130, 1-7. 

SUGANUMA M, OKABE s, KAi Y, suEOKA N, suEOKA E and FUJiKi H (1999) Synergistic effects of (-)-epigallocatechin gallate with (-)-epicatechin, sulindac, or tamoxifen on cancer-preventive activity in human lung cancer cell line PC-9 , Cancer Res, 59, 44-7. 

AVIVI-GREEN c, PLOAK-CHARCON s, MADAR z, SCHWARTZ B (2002) Different molecule events account for butyrate-induced apoptosis in tiw human colon cancer cell line. J. Nutr. 132 1812-18. 

GAMET L, DAViAUD D, DENis-POUXViEL 0, REMESY 0, MURAT J 0 (1992) Effects of shoit-chain fatty acids on growth and differentiation of the human colon-cancer cell line HT29. Int J Cancer. 52 286-9. 

Haliclonacyclamine F (25), arenosclerin D (26), and arenosclerin E (27) have been recently isolated from the sponge Pachychalina alcaloidifera endemic in Brazil [26]. The alkaloids 25-27 were isolated from the cytotoxic, antibiotic, and antituberculosis MeOH crude extract of P. alcaloidifera by a series of separations on silica-gel and cyanopropyl-bonded silica-gel columns. The structures of compounds 25-27 were established by the same approach employed for the structural elucidation of haliclonacyclamine E (13) and arenosclerins A-C (14-16) [18], as well as by comparison with NMR data for this last series of alkaloids. The alkaloids 25-27 displayed moderate cytotoxic activity against SF295 (human CNS), MDA-MB435 (human breast), HCT8 (colon), and HL60 (leukemia) cancer cell lines. 

FIGURE 5.35 Growth inhibition assay of three human cancerous cell lines, with dendritic prodrug 38 in the presence ( ) and absence ( ) of PGA cells were incubated for 72 h. 

Table 7.3 shows the concentrations of 1-5 that result in 50% growth inhibition (GI50) of five human cancer cell lines. Inspection of these data reveals that cytostatic activity of 1 and 3-5 depends on the thermodynamic favorability of the quinone methide species compared to the corresponding keto form. The most cytostatic prekinamycins 1 and 5 are associated with the thermodynamically stable quinone methides. In contrast, the inactive prekinamycins 3 and 4 are associated with thermodynamically stable keto tautomers. The exception is prekinamycin 2, which is cytostatic and possesses a relatively stable keto tautomer 3 compared to its quinone methide. Although the AE value for quinone methide tautomerization can predict cytostatic properties, prekinamycin 2 shows that there must be other factors determining biological activity. 

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