RESUMO
6-Thioguanine encapsulated chitosan nanoparticles (6-TG-CNPs) has formulated by the ionic-gelation method. Morphologically, the 6-TG-CNPs were spherical and showed mean size, PDI, zeta potential, and entrapment efficiency of 261.63 ± 6.01 nm, 0.34 ± 0.10, +15.97 ± 0.46 mV and 44.27%, respectively. The IR spectra confirmed the 6-TG complex with chitosan. The in vitro drug release profile of 6-TG-CNPs revealed an increase in sustained-release (91.40 ± 1.08% at 48 h) at pH 4.8 compared to less sustained-release (73.96 ± 1.12% at 48 h) at pH 7.4. The MTT assay was conducted on MCF-7 and PA-1 cell lines at 48 h incubation to determine % cell viability. The IC50 values of 6-TG, 6-TG-CNPs, and curcumin for MCF-7 were 23.09, 17.82, and 15.73 µM, respectively. Likewise, IC50 values of 6-TG, 6-TG-CNPs, and curcumin for PA-1 were 5.81, 3.92, and 12.89 µM, respectively. A combination of 6-TG-CNPs (IC25) with curcumin (IC25) on PA-1 and MCF-7 showed % cell viability of 43.67 ± 0.02 and 49.77 ± 0.05, respectively. The in vitro cytotoxicity potential in terms of % cell viability, early apoptosis, G2/M phase arrest, and DNA demethylating activity of 6-TG-CNPs alone and combination with curcumin proved to be more effective than that of 6-TG on PA-1 cells.
Assuntos
Antineoplásicos/farmacologia , Quitosana/química , Curcumina/química , Nanopartículas/química , Tioguanina/farmacologia , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Humanos , Células MCF-7 , Tamanho da Partícula , Tioguanina/químicaRESUMO
An experiment was conducted to evaluate the effects of methanolic extracts of Murraya koenigii Spreng. (Curry leaf) and Morus alba Linn. (Mulberry leaf) on the age of attainment of puberty, relative ovary and uterus weight and the number of ovarian surface follicles in female Wistar albino rats. The rats were reared from 20 to 70 days of age in six groups consisting of eight rats in each group. Group I and II were orally administered with 0.5 ml distilled water and 0.5 ml 10% DMSO, respectively. Group III, IV, V and VI were orally administered with methanolic extracts of Murraya koenigii at 500 mg/kg b.w. and 1000 mg/kg b.w. and methanolic extracts of Morus alba at 250 mg/kg b.w. and 500 mg/kg b.w, respectively. The significant advancement in the mean age of attainment of puberty was observed along with increase in number of surface follicles on both the ovaries in Group III, IV and VI. Whereas, the relative ovary weight was non significant (P>0.05) in all the treated groups, the relative uterus weight was significant (P<0.05) in Group IV and Group VI. These observations were attributed to the effects of phytoestrogens present in the methanolic extracts of Murraya koenigii Spreng. and Morus alba Linn.