Effects of treatments with different doses of the chalcone (<i>E</i>)-1-(2-hydroxyphenyl)-3-(4-methylphenyl)-prop-2-en-1-one) (2HMC) on the frequency of micronucleated polychromatic erythrocytes (MNPCE) and polychromatic/normochromatic erythrocyte ratio (PCE/NCE) in bone marrow cells of mice.

<p>Effects of treatments with different doses of the chalcone (<i>E</i>)-1-(2-hydroxyphenyl)-3-(4-methylphenyl)-prop-2-en-1-one) (2HMC) on the frequency of micronucleated polychromatic erythrocytes (MNPCE) and polychromatic/normochromatic erythrocyte ratio (PCE/NCE) in bone marrow cells of mice.</p

Synthetic route of chalcone 2HMC (1).

<p>Reagents and conditions: (a) 50% NaOH (w/w), EtOH, 12 h (room temperature).</p

Evaluation of cytotoxic and genotoxic activities in the bone marrow of mice treated with sulfonamide chalcone N-{4-[3-(4-nitrophenyl)prop-2-enoyl]phenyl}-benzenesulfonamide (CPN) based on MNPCE and PCE/NCE frequency.

<p>¹ Negative control: dimethylsulfoxide (DMSO) 0.1 mL/10 g body weight (b.w.).</p><p>² Positive control: mitomycin C (MMC) 4 mg/kg (80% LD₅₀).</p><p>All values are mean ± SD of five mice.</p><p>³ Statistical analysis: one-way ANOVA and the Tukey’s test.</p><p>⁴ Statistical analysis: chi-square (χ^<b>2</b>) test.</p><p>Mean values followed by the same letter in the column do not present significant difference at 5% probability.</p><p>^{a, b, c, d} Letter in common in the same column do not present significant difference (<i>p</i> > 0.05). Different letters in the same column present significant difference (<i>p</i> < 0.05).</p><p>Evaluation of cytotoxic and genotoxic activities in the bone marrow of mice treated with sulfonamide chalcone N-{4-[3-(4-nitrophenyl)prop-2-enoyl]phenyl}-benzenesulfonamide (CPN) based on MNPCE and PCE/NCE frequency.</p

Means ± standard deviation (SD) of histidine revertant colonies (obtained from three independent experiments carried out in triplicate), mutagenic index (MI), and inhibition percentage of mutagenicity (IP) for two tester strains of <i>Salmonella typhimurium</i>, TA98 and TA100, after treatment with different doses of the chalcone (<i>E</i>)-1-(2-hydroxyphenyl)-3-(4-methylphenyl)-prop-2-en-1-one) (2HMC).

<p>Means ± standard deviation (SD) of histidine revertant colonies (obtained from three independent experiments carried out in triplicate), mutagenic index (MI), and inhibition percentage of mutagenicity (IP) for two tester strains of <i>Salmonella typhimurium</i>, TA98 and TA100, after treatment with different doses of the chalcone (<i>E</i>)-1-(2-hydroxyphenyl)-3-(4-methylphenyl)-prop-2-en-1-one) (2HMC).</p

Assessment of the genotoxic and antigenotoxic activities of the chalcone (<i>E</i>)-1-(2-hydroxyphenyl)-3-(4-methylphenyl)-prop-2-en-1-one) (2HMC) at different doses in mice bone marrow cells using the comet assay estimated by the parameter %DNA in tail.

<p>DMSO, dimethylsulfoxide (negative control); CPA, cyclophosphamide (50 mg/kg BW) (positive control). ANOVA and the Tukey’s test: *significant compared to the positive control (<i>p</i> < 0.05). Groups 3 and 4, treated only with 2HMC, were compared to the negative control. Groups 5, 6, 7, 8, 9, and 10, co-, pre-, or post-treated were compared to the positive control.</p

Means ± standard deviation (SD) of histidine revertant colonies, mutagenic index (MI), and inhibition percentage (IP) of mutagenicity for two tester strains of <i>Salmonella typhimurium</i>, TA98 and TA100, after treatment with different doses of sulfonamide chalcone N-{4-[3-(4-nitrophenyl)prop-2-enoyl]phenyl}-benzenesulfonamide (CPN).

<p>¹ Negative control: 20 μL dimethylsulfoxide (DMSO).</p><p>² Positive control: 0.5 μg 4-nitroquinoline 1-oxide (4-NQO)/plate for TA98 and 1.5 μg sodium azide/plate for TA100.</p><p>All values are means ± SD of three independent experiments.</p><p>³ Statistical analysis: one-way ANOVA and the Tukey’s test.</p><p>^{a, b, c, d} Letter in common in the same column do not present significant difference (<i>p</i> > 0.05). Different letters in the same column present significant difference (<i>p</i> < 0.05).</p><p>Means ± standard deviation (SD) of histidine revertant colonies, mutagenic index (MI), and inhibition percentage (IP) of mutagenicity for two tester strains of <i>Salmonella typhimurium</i>, TA98 and TA100, after treatment with different doses of sulfonamide chalcone N-{4-[3-(4-nitrophenyl)prop-2-enoyl]phenyl}-benzenesulfonamide (CPN).</p

Yield, physical state, melting point, purity, and spectroscopic data (GS-MS, IR, ¹H-NMR) of N-(4-acetylphenyl)benzenesulfonamide (1) and N-{4-[(<i>E</i>)-3-(4-nitrophenyl)prop-2-enoyl]phenyl}-benzenesulfonamide (2).

<p>¹ Retention time.</p><p>² Mobile phase used: CH₃CN:aqueous buffer containing chloroacetic acid 0.1% (55:45).</p><p>Yield, physical state, melting point, purity, and spectroscopic data (GS-MS, IR, ¹H-NMR) of N-(4-acetylphenyl)benzenesulfonamide (1) and N-{4-[(<i>E</i>)-3-(4-nitrophenyl)prop-2-enoyl]phenyl}-benzenesulfonamide (2).</p

Tellimagrandin-I and camptothin a exhibit chemopreventive effects in <i>Salmonella enterica</i> serovar Typhimurium strains and human lymphocytes

Tellimagrandin-I (TL) and camptothin A (CA) are ellagitannins widely found in diverse plant species. Numerous studies demonstrated their significant biological activities, which include antitumor, antioxidant, and hepatoprotective properties. Despite this protective profile, the effects of TL and CA on DNA have not been comprehensively investigated. Thus, the aim of this study was to determine the mutagenic and antimutagenic effects attributed to TL and CA exposure on Salmonella enterica serovar Typhimurium strains using the Ames test. In addition, the cytotoxic and genotoxic effects were examined on human lymphocytes, employing both trypan blue exclusion and CometChip assay. The antigenotoxic effect was determined following TL and CA exposure in the presence of co-treatment with doxorubicin (DXR). Our results from the Ames test indicated that TL or CA did not display marked mutagenic activity. However, TL or CA demonstrated an ability to protect DNA against the damaging effects of the mutagens 4-nitroquinoline-1-oxide and sodium azide, thereby exhibiting antimutagenic properties. In relation to human lymphocytes, TL or CA did not induce significant cytotoxic or genotoxic actions on these cells. Further, these ellagitannins exhibited an ability to protect DNA from damage induced by DOX during co-treatment, indicating their potential beneficial usefulness as antigenotoxic agents. In conclusion, the protective effects of TL or CA against mutagens, coupled with their absence of genotoxic and cytotoxic effects on human lymphocytes, emphasize their potential therapeutic value in chemopreventive strategies.</p

Comet assay analysis in bone marrow cells of mice treated with two antiretroviral combinations and their respective controls.

<p>Comet assay analysis in bone marrow cells of mice treated with two antiretroviral combinations and their respective controls.</p