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Background & Objective: Diclofenac is a non-steroidal, anti-inflamatory drug that is prescribed as an analgesic. However, there is little known about the effects of diclofenac on the neural cells. In this study, we investigated the effects of diclofenac as sodium salt on the proliferation and differentiation of PC12 cells.

 

Materials & Methods: This expeimental study was done in Kerman neuroscience research center during 2004. The cell proliferation was evaluated by using XTT assay in the both free-serum neurobasal medium supplemented with B27 supplement and DMEM/F12 medium containing 10% FBS. The nerve growth factor(NGF) – induced differentiation was assessed  by measuring the neurite length for each treatment.

 

Results: The drug toxicity was exhibited at the higher concentrations of 310 mM in the supplemented neurobasal medium. The treatment of cells in the DMEM/F12 medium increased their sensitivity to diclofenac, with 40 and 85% growth inhibition at the 155 and 310 mM concentrations, respectively. The different generics of drug exhibited a equal toxic effects on the PC12 cells. The NGF- induced differentiation was not reduced by toxic and subtoxic concentrations of diclofenac.

 

Conclusion: This study indicated that diclofenac may be able to exhibit its neurotoxic effects through growth inhibition, but not differentiation inhibition. B27 supplement has several antioxidant compounds. Therefore, the difference of diclofenac cytotoxic effects in two culture media suggest that drug cytotoxicity may be related to the oxidative stress.

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Background and Objective: Mirtazapine is a norepinephrine and serotonergic antidepressant that is used in the theraphy of major depressive disorders. This study was carried out to determine the genotoxic and cytotoxic effect of mirtazapine using chromosome aberration and mitotic index tests in human peripheral blood lymphocytes. Methods: In this descriptive -analytic study genotoxic and cytotoxic effect of mirtazapine at 24 and 48 hours treatment periods on four concentration (10, 25, 40, and 55µg/ml) was performed on peripheral blood lymphocyte of four subjects. Results: Mirtazapine significantly reduced the mitotic index in the all concentrations but it non-significantly increased the chromosome aberration at 24-hours and 48-hours treatment periods. Conclusion: Mirtazapine has cytotoxic effect but it has no genotoxic effect on human lymphocyte.

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Background and Objective: HIV treatment influences the global health and finding new compounds against HIV virus is increased. This study was done to evaluate anti-HIV activity of 8-phenyl-4-quinolone derivatives containing different substituents at position 3.

Methods: In this descriptive study, single cycle replicable (SCR) HIV Virions were produced by co-transfecting HEK 293T cells with pmzNL4-3, pSPAX.2, pMD2.G plasmids. HeLa cells were infected with the SCR virions and then inhibit of virus replication by compounds were measured by p24 Antigen with ELISA kit. The cytotoxicity of these compounds on HeLa cells were measured by XTT method.

Results: All compounds including NPZ_4F, NPZ-2F, NPZ-4CL and NPZ-2CL had the best inhibitory effect at a concentration of 100µM with the inhibition rate of respectively 51%, 48%, 33%, and 25%, respectively. The compounds of NPZ-4F and NPZ-2CL had negligible cellular toxicity and have inhibited HIV replication at the highest concentration. This issue can make them a valuable compound since they are better compounds in therapeutic terms, which at a suitable concentration, they have the lowest rate of cellular toxicity and highest power to inhibit HIV replication.

Conclusion: Novel compounds derived from 8-phenyl-4-quinolone containing different substituents at position 3 can prevent HIV replication which is capable of high anti-viral and low cellular toxicity and suitable candidates for further investigation in antiviral studies.

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Background and Objective: Curcumin is a combination of active polyphenol from the Curcuma Langa plant, which has extensive biological activities including effects anti-inflammatory, anti-bacterial and cytotoxic markers for multiple cancer cells. Berberine is an alkaloied isokinolin that is present in berberine and suppresses the growth of many tumor cells. This study was designed to determine the antibacterial effect of berberine and indium curcumin and indium diastile curcumin complexes against E-coli and Bacillus pumilus and comparison of their cytotoxicity on the cell lines of the bladder and stomach cancer cells.
Methods: In this descriptive-analytic study, antimicrobial activity and cytotoxicity effect of berberine and indium curcumin and indium diastile curcumin complexes was investigated by MTT and dilution test method respectively. E-coli [BL21 (DE 3)], Bacillus pumilus (PTCC 1529), cell lines of bladder (5637) and stomach (AGS) were evaluated.
Results: The minimum inhibitory concentration (MIC) of berberin for E-coli was determined 5 mM. At 100 micromolar concentration of berberine approximately 100% of the bladder cancer cells have disappeared. Cytotoxic effect of curcumin complexes on two bladder and stomach cancer cell lines showed that both complexes have different inhibitory effects on cell line life. Cytotoxicity of 20μM indium curcumin and indium diastile curcumin complexes for bladder cancer cells were 58% and 55%, respectively, and for stomach cancer cells were 61% and 34 %, respectively. Antibacterial activity of complexes against Bacillus pumilus and E-coli showed that none of the complexes has antimicrobial effect against Bacillus Pamilus, but both complexes inhibited the growth of E-coli bacteria. The bacteria population in the presence of indium curcumin and indium diastile curcumin complexes was reduced to 40% and 24%, respectively.
Conclusion: This study indicated that indium complexes of curcumin and diacetyl curcumin have a potential for anticancer and antibacterial therapy. Furthermore, berberine as an alkaloid has anticancer and antibacterial activity.

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Background and Objective: Increasing interest has been devoted to the design and discovery of more effective anticancer agents in current medicinal chemistry because of the high prevalence of cancer in different societies and resistance occurrence to existing anticancer drugs. The aim of this study was to evaluate the anticancer activity of two novel quinoline compounds (RQ1 and RQ2) on human gastric cancer cells.
Methods: In this descriptive - analytic study, the anticancer effects of the compounds were evaluated by MTT assay. This test was performed on two categories of gastric cancer cells sensitive to Danorubicin (EPG85-257P) and resistant to Danorubicin (EPG85-257RDB). The arresting mechanism in the G2 / M phase of the cell cycle and the induction of apoptosis by the compounds was investigated using the PI test and flow cytometric analysis.
Results: Novel quinoline derivatives RQ1 and RQ2 showed good anticancer effects on both sensitive and resistant human gastric cancer cells (IC50=25-38mM). Compound RQ2 showed the most cytotoxic activity on the Danorubicin-sensitive cancer cell line with IC50=25mM. The percentage of Danorubicin resistant gastric cancer cells (EPG85-257RDB) in the G2 / M phase at 25mm concentration of RQ1 and RQ2 was 35.95 and 34.88, respectively, and 41.1% and 42.89% of these cells, after treatment with 50mm concentration of RQ1 and RQ2 arrested at the G2 / M phase respectively.
Conclusion: The two novel quinoline compounds, RQ1 and RQ2 showed strong anticancer effect on both sensitive and resistant human gastric cancer cell lines.

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Background and Objective: In medical sciences, identifying the anticancer properties of plumbagin is of special importance. For this reason, this study investigated the anticancer activity of polymeric nanoparticles loaded by plumbagin against breast cancer cells.
Methods: In this descriptive study, the diblock copolymer mPEG–PCL was synthesized by ring-opening polymerization of caprolactone in the presence of mPEG as the initiator and Sn(oct)2 as the catalyst. The synthesized copolymers were characterized by Fourier-transform infrared spectroscopy, proton nuclear magnetic resonance, gel permeation chromatography, and differential scanning calorimetry. The nanoprecipitation method was used for preparing nanoparticles loaded with plumbagin. The characteristics of these nanoparticles were investigated by various techniques including dynamic light scattering. The cytotoxicity of plumbagin, copolymer, and the nanoparticles loaded with plumbagin on MCF7 and HFF2 cells was evaluated by MTT assay.
Results: The average diameter of the nanoparticles was less than 115 nm. The loading capacity and encapsulation efficiencies were 15.4±0.13% and 79.1±0.65%, respectively. Drug release was slow, controlled, and almost dependent on pH. The results of the MTT assay showed strong and dose-dependent inhibition of cell growth by the plumbagin-loaded micelles compared with plumbagin alone in a way that the half maximal inhibitory concentration of this nanoparticle against MCF7 cells after 48 and 72 hours was 10.78 and 24.03 μM, respectively.
Conclusion: The mPEG-PCL nanoparticles can be an efficient carrier for plumbagin, and plumbagin can be an effective drug on breast cancer cells, without toxicity on healthy cells.