Human colon carcinoma HCT

The above three equations (Eqs. 10-12) for the different cell lines are very similar to each other, which suggests that the inhibition against DNA topo I is probably one of the most important antitumor mechanisms for these compounds (CPT, CPT-11, SN-38, TPT, and EGCG) against the three human colon carcinoma (HCT 116, VACO 241, and SW 480) cell lines. In these equations, the number of data points (four or five) is small, but the correlations are statistically significant. 

Four new cytotoxic disulfides, rostratins A-D 57-60, were isolated from the broth of the marine-derived fungus Exserohilum rostratum (Drechsler), a fungal strain found associated with a marine cyanobacterial mat. These compounds showed in vitro cytotoxicity against human colon carcinoma (HCT-116) with IC50 values of 8.5, 1.9, 0.76, and 16.5 pg mL, respectively. 

Inhibition of DNA topo I activity in HCT 116 (human colon carcinoma) cells by CPT, CPT-11, SN-38, TPT, and EGCG (Table 8) ... 

HCT-116 human colon carcinoma (ATCC, Bethesda MD) cells were grown in McCoy s 5A) and were routinely subcultured twice weekly. Antiproliferative assay was performed by chemoluminescence assay based on quantification of ATP. Cells in their exponential phase of growth were treated at different times (lh or 24h) with different concentrations of edotecarin or SN-38. For post-treatment recovery studies, cells were washed with PBS and left in drug-free culture medium. Then, cell medium was collected to avoid any cell loss. Cells in monolayer were washed, detached with trypsin, and collected in the medium. Cells were counted in a Multisizer 3 Coulter Counter to measure the drug s effects on growth inhibition. Samples were fixed either... 

Figure 1-2. Molecular structures of cyclopropane- and aziridine-based analogs of epothilones. Numbers in parentheses are ICso-values for growth inhibition of the human colon carcinoma cell line HCT-116. Data are from Johnson et al. (12 and 13) and Regueiro-Ren et al. " (14 and 15).

A new sesterterpene epoxide-diol, aspergilloxide 25, was isolated from the extract of a cultured marine-derived fungus (strain CNM-713), a member of the genus Aspergillus 25 showed little in vitro cytotoxicity toward HCT-116 human colon carcinoma. 

A series of fifty-three isoquinoline alkaloids were tested for cytotoxicity against A-549 (human lung carcinoma), HCT-8 (human colon carcinoma), KB, P-388, and L-1210 cells in vitro. Liriodenine showed potent and wide spectrum activity against all five cell lines tested A-549 (EDJ0 0.72 pg/ml), HCT-8 (0.70), KB (1.00), P-388 (0.57), and L-121-0 (2.33)[299]. 

A triorganotin quinolizidine compound, triethyitin Iupinyisulfide hydrochloride (Figure 4.4.7), has been reported to show quite good solubility in ethanol/water and to be a potent anti-proliferative against three different human cancer cell lines teratocarcinoma of the ovary (PA-1), colon carcinoma (HCT-8), and glioblastoma (A-172).2 The cytocidal effects due to this compound seem consistent with necrosis or delayed cell death rather than apoptosis. 

Trichodermamides A and B (207), two modified dipeptides, have been isolated from cultures of the marine-derived fungus Trichoderma virens [226], Trichodermamide B displayed significant in vitro cytotoxicity against HCT-116 human colon carcinoma with an ICso of 0.32 pg/ml. TTiis metabolite also exhibited moderate antimicrobial activities against amphoterocin-resistant C. albicans, methacillin-resistant S. aureus, and vancomycin-resistant E. faecium with MIC values of ca. 15 (xg/ml against... 

Further investigation of the B. antidysenterica extract [10] led to the isolation of three new quassinoids bmceanol-D (17), -E (18), -F (19), and known a diSsmoiAs yadanzioside-N A), bruceantin (1), and isobnicein-B (5). Bruceanol-D (17) and -F (19) were both obtained as colorless amorphous solids and bruceanol-E (18) was obtained as colorless needles. They showed cytotoxicity for tumor cells such as KB (nasopharynx carcinoma), A-549 (human lung carcinoma), HCT-8 (human colon tumor), P-388 (murine lymphocytic lei emia), TE-671 (human medulloblastoma), and RPMI-7951 (human melanoma), as shown in Table 1. 

A new quassinoid % vlq,os 6.q, picrasinoside-H (35), was isolated from the same plant as a colorless amorphous solid. An in vitro cytotoxicity assay was carried out according to the NCI procedure [4] Picrasinoside-A (26), -B (27), -C (28), -D (29), -E (30), and -G (32) were tested against KB (nasal pharingeal carcinoma), TE-671 (human medulloblastoma), A-549 (human lung carcinoma), HCT-8 (human colon carcinoma), RPMI (human melanoma), and P-388 (murine leukemia) tumor cells. But, no significant (ED50 < 4 [ig/ml) cytotoxicity was observed in these quassinoids [16]. 

---