Cytotoxicity activities carcinoma

The first screening on cytotoxic activity regarding plants of Licania genus was accomplished by Suffness et al. in 1988 on the ethanolic extract of L. heteromorpha [19]. The plant showed cytotoxic activity in vitro in colon carcinoma 38 and B16 melanoma models. 

Cytotoxic activity against human oral squamous cell carcinoma (HSC-2)... 

Gruber BM, Anuszewska EL, Bubko I, et al. Relationship between topoisomerase II-DNA cleavable complexes, apoptosis and cytotoxic activity of anthracyclines in human cervix carcinoma cells. Anticancer Res. 2005 25(3B) 2193-2198. 

Cells treated with 5-FU undergo cell cycle arrest or apoptosis by inhibition of DNA synthesis. When human oral squamous cell carcinomas (HSC-2, HSC-3, HSC-4) were treated with 5-FU, viable cell numbers declined dose-dependently (CC50 determined after 24 hours treatment 3.4,6.9 and 1.7 p,M, respectively). The intracellular putrescine concentration slightly declined (Table 2) [29]. The combination treatment of 5-FU with N(l),N(ll)-diethylnorspermine (DEN-SPM), which is an inducer of spermidine/spermine N(l)-acetyltransferase (SSAT) that depletes polyamine, has been reported to augment the cytotoxic activity of 5-FU, suggesting possible clinical application [30]. 

Further, eleven 4-phenyl-3,5-diacetyl-1,4-DHPs substituted at the C-4 phenyl ring were synthesized and compared for their cytotoxic activity and MDR reversing activity in in vitro assay systems. Among them, compound G7 (68) showed the highest cytotoxic activity against human promyelocytic leukemia HL-60 and human squamous cell carcinoma HSC-2 cells. However, no compounds tested produced radicals at pH 7.4-12.5. The activity of Pgp... 

The anticancer properties of a series of dibenzoyl dihydropyrimidines have recently been reported [40]. In particular, compound 73 (Fig. 10) showed cytotoxic activity against human oral squamous carcinoma (HSC-2) cells and also inhibited the Pgp-mediated drug efflux in (multidmg resistant) MDR cells. 

The three-component reactions of malononitrile 175, aldehydes 176 and 2-mercaptoacetic acid 177 (Scheme 33), in different molar ratios under microwave heating, in water, provided thiazolopyridine derivatives 178 and 179 in high yields [70]. The compounds were evaluated for their cytotoxic activity against the carcinoma cell line HCT 116 (ATTC CCL 247) and mice lymphocytes (Table 14). Compound 183 was the only one with selective cytotoxic activity towards the HTC 116 cells (Fig. 22). The compounds were also evaluated for their antioxidant... 

Ryrinodemins A-B Amphimedon sp. Cytotoxic activity (murine leukemia and KB epidermoid carcinoma cells)... 

The effect of tocotrienols on cancer progression was evaluated by Komi-yama and Yamaoka (177). The antitumor activity of tocotrienols was evaluated in terms of the increase in the lifespan of mice inoculated with tumor cells. a-Tocotrienols and y-tocotrienols were effective against the sarcoma cancer cell lines and Ehrlich carcinoma. When human lung carcinomas were challenged with these tocotrienols, a cytotoxic activity due to the tocotrienols was exhibited. Similarly. DMBA-treated rats responded with lower tumor numbers when their diets were supplemented with palm tocotrienols (178). Recently, a-carotene isolated from pahn oil has been shown to have antitumor activity against mouse lung cancer and against skin cancer (179). 

DS-penaustrosides A (79) and B (80) revealed cytotoxic activities against murine lymphoma L1210 and human epidermoid carcinoma KB cell lines [IC5o=0.12 (L1210) and 0.62 (KB) p.g/ml for 79 2.1 (L1210) and 4.6 (KB) ig/ml for 80] [69]. Unfortunately, the authors did not show the data on activities of relative holostane derivatives in the same experimental conditions. 

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