Cytotoxicity of Libyan Juniperus phoenicea against Human Cancer Cell Lines A549, EJ138, Hepg2 and MCF7

Background: The current study was undertaken to assess the cytotoxicity of the leaves of Libyan Juniperus phoenicea (Cupressaceae) against human cancer cell lines. Methods: The cytotoxicity of the n-hexane, dichloromethane (DCM) and methanol (MeOH) extracts of the leaves of J. phoenicea (JP), obtained from sequential Soxhlet extractions, was assessed against four human cancer cell lines: EJ138 (human bladder carcinoma), HepG2 (human liver hepatocellular carcinoma), A549 (human lung carcinoma) and MCF7 (human breast adenocarcinoma) using the MTT assay. Results: The cell line A549 was the most sensitive to the JP extracts, with the highest level of cytotoxicity with the IC50 values of 16, 13 and 100 μg/mL for the DCM, n-hexane and MeOH extracts, respectively. However, generally the most potent cytotoxic extract across the other cells tested was the n-hexane extract, followed by the DCM extract, whilst the MeOH extracts showed little or no cytotoxicity. The percentage of viability of cells decreased as the concentration of test compounds increased. The cytotoxicity of various chromatographic fractions from the extracts was also studied against the A459 cells. For the n-hexane fractions, the IC50 values were 160, 62, 90, 30, 9.5 and 40 μg/mL for fractions 1 to 5 and 7, respectively. Fractions 4 and 5 showed the greatest effect. DCM fractions 2, 3 and 4 had the IC50 values of 60, 92 and 19 μg/mL, respectively, and DCM fractions 5 to 8 were non-cytotoxic. Fractions 1 and 2 of the MeOH extract were non-cytotoxic, whereas cytotoxicity was observed for fractions 3 and 4 with IC50 values of 50 and 85 μg/mL, respectively. Conclusion: The outcome of the present study suggested that the JP leaves possess cytotoxic activities. The high level of cytotoxicity of the n-hexane and DCM extracts suggested that lipophilicity might affect the cytotoxicity of JP, where the less polar compounds had the strongest cytotoxicity

A biochemical, theoretical and immunohistochemical study comparing the therapeutic efficacy of curcumin and taurine on T-2 toxin induced hepatotoxicity in rats

Introduction: Foodborne trichothecene T-2 Toxin, is a highly toxic metabolite produced by Fusarium species contaminating animal and human food, causing multiple organ failure and health hazards. T-2 toxins induce hepatotoxicity via oxidative stress causing hepatocytes cytotoxicity and genotoxicity. In this study, curcumin and taurine were investigated and compared as antioxidants against T-2-provoked hepatotoxicity.Methods: Wistar rats were administrated T-2 toxin sublethal oral dose (0.1 mg/kg) for 2 months, followed by curcumin (80 mg/kg) and taurine (50 mg/kg) for 3 weeks. Biochemical assessment of liver enzymes, lipid profiles, thiobarbituric acid reactive substances (TBARs), AFU, TNF-α, total glutathione, molecular docking, histological and immunohistochemical markers for anti-transforming growth factor-β1 (TGFβ1), double-strand DNA damage (H2AX), regeneration (KI67) and apoptosis (Active caspase3) were done.Results and Discussion: Compared to T-2 toxin, curcumin and taurine treatment significantly ameliorated hepatoxicity as; hemoglobin, hematocrit and glutathione, hepatic glycogen, and KI-67 immune-reactive hepatocytes were significantly increased. Although, liver enzymes, inflammation, fibrosis, TGFβ1 immunoexpressing and H2AX and active caspase 3 positive hepatocytes were significantly decreased. Noteworthy, curcumin’s therapeutic effect was superior to taurine by histomorphometry parameters. Furthermore, molecular docking of the structural influence of curcumin and taurine on the DNA sequence showed curcumin’s higher binding affinity than taurine.Conclusion: Both curcumin and taurine ameliorated T-2 induced hepatotoxicity as strong antioxidative agents with more effectiveness for curcumin

Phenolic Compounds and Bioactivity of Leaves of Mayodendron Igneum Kurz

Four apigenin glycosides were isolated from the ethyl acetate extract of the leaves of Mayodendron igneum Fam.Bignoniaceae. They were identified as apigenin 7-O-glucoside; 6-methoxy apigenin-7-O-glucoside; 6-methoxy apigenin-7-O-rhamnoglucoside and 6-hydroxy apigenin-7-O-rhamnoglucoside. In addition an isoflavone glycoside was isolated, and identified as genistin 5,4‵-methyl ether. Ethanol (80%) extract of Mayodendron igneum leaves exhibited significant anti-inflammatory and analgesic activities. LD50 determination of the extract indicated the safety of the leaves of the plant

Reaction of C-aroyl-N-aryl nitrilimines with selected aliphatic keto-hydrazones and keto-methylhydrazones

C-Benzoyl-and C-2-naphthoyl nitrilimines (2) react with methylhydrazones of aliphatic ketones (3, R1= CH3) to afford the cyclocondensation products 1, 2, 4, 5-tetrazines (4, 5). The reaction of simple hydrazones (3, R1= H) with the same nitrilimines gives the acyclic electrophilic addition products (6, 7), rather than the cyclocondensation tetrazine products

Synthesis of Dihydro-and Tetrahydro-1, 2, 4, 5-tetrazines from the Reaction of Nitrilimines with 1-Substituted-1-methylhydrazine

The reaction of nitrilimines (2) with 1-substituted-1-methylhydrazines (3–6) led to the formation of the respective amidrazones (7) when R = CH3, Ph, and to the acyclic adducts (8,9) when R = CHO and COCH3. The acyclic adducts underwent thermal oxidative cyclization at CH3 to give the unexpected 1,2,4,5-tetrazines (10,11). Dihydro-l,2,4,5-tetrazines (12) were also seperated when R = CHO

1, 2, 4-Triazoles from 1, 3-dipolar cycloaddition reaction of nitrilimines with aliphatic ketohydrazones carrying electron withdrawing groups

Alkanone and cycloalkanone hydrazones (3) carrying electron withdrawing groups (OCOCH3, COCH3, COPh) react with C-benzoyl-and C-2-naphthoylnitrilimines to give the cycloaddition triazole products (6-11). IR, 1H NMR, 13C NMR and mass spectral data are consistent with the assigned triazole ring system. Compounds (8, 9) having an acetyl group, show signal doubling in their 13C NMR spectra, apparently owing to their presence in two different mesomeric structures