ABSTRACT
This investigation aimed to evaluate the in vitro and in vivo antitumor potential of a Moroccan propolis extracts. For in vitro assays, three mammalian tumor cell lines were used: BSR (hamster renal adenocarcinoma), Hep-2 (human laryngeal carcinoma) and P815 (murin mastocytoma). The propolis ethanolic extract as well as the ethyl acetate extract, exert an in vitro cytotoxic activity in dose-dependent manner. The IC50 values were ranging from 15 µg/mL to 38 µg/mL. This activity depends not only on the extract's chemical composition (analysed by HPLC/ESI-MS), but also on the target tumor cells. Interestingly, the cytotoxic effect of these extracts on the normal human peripheral blood mononuclear cells (PBMC) was weak when compared to that induced on tumor cells. On the other hand, oral route treatment of P815 tumor-bearing mice (DBA2/P815) with propolis ethanolic extract (5 mg per mouse every fourth day, five times for group A, and 2.5 mg per mouse every fourth day, five times for group B) significantly reduced the tumor volume (1.2 cm³ for group A and 2.7 cm³ for group B at the 22nd day after tumor graft). These effects are statistically significant as compared to those obtained with the control untreated mice (tumor volume 3.5 cm³ at day 22).
ABSTRACT
The evaluation of the in vitro cytotoxic properties of two pyrazole compounds: 1-(4-nitrophényl)-3,5-diméthylpyrazole (1) and 1,1'-di(4-nitrophényl)-5,5'-diisopropyl-3,3'-bipyrazole (2) was investigated against Hep cell line (Human laryngeal carcinoma). These two compounds showed an important cytotoxic activity on the Hep cell line, with IC(50): 8.25 microg mL(-1) for the compound 1; IC(50): 10.20 microg mL(-1) for the compound 2 while the IC(50) for adriamycine used as positive control was 3.62 microg mL(-1).
Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Pyrazoles/chemical synthesis , Pyrazoles/pharmacology , Antineoplastic Agents/chemistry , Cell Line, Tumor , Cell Survival/drug effects , Cytotoxins/chemical synthesis , Cytotoxins/chemistry , Cytotoxins/pharmacology , Drug Screening Assays, Antitumor , Formazans/chemistry , Humans , Magnetic Resonance Spectroscopy , Mass Spectrometry , Pyrazoles/chemistry , Spectrophotometry, Infrared , Tetrazolium Salts/chemistryABSTRACT
The evaluation of the cytotoxic properties in vitro of three synthetic tripods containing pyrazole: N,N-bis[(3,5-dimethylpyrazol-1-yl)methyl]aniline (1); N,N-tetrakis[(3,5-dimethylpyrazol-1-yl)methyl]-para-phenylenediamine (2); and N,N-tetrakis-[(1,5-dimethylpyrazol-3-yl)methyl]-para-phenylenediamine (3), was examined for their cytotoxic activity on two tumor cell lines: P815 (murin mastocytoma) and Hep (human laryngeal carcinome). While the compound 2 shows a small cytotoxic activity, compounds 1 and 3 are more cytotoxic against both cell lines. However, this cytotoxicity is more pronounced against Hep cell line (IC50: 3.25 microg mL(-1) for compound 1 and 6.92 microg mL(-1) for compound 3) than P815 cell line (IC50: 17.82 microg mL(-1) for compound 1 and 37.21 microg mL(-1) for compound 3). Statistical analysis shows that the compound 1 is two- to threefold more cytotoxic than compound 3 (P < 0.05). Interestingly, the cytotoxicity induced by compound 1 against Hep cell line is more important than that induced by adriamycin used as a positive control.
