Synthesis and anticancer activity evaluation of some new 1,2,3,5-tetrazine derivatives attached to benzothiazole moiety

A series of novel tetrazine derivatives, containing benzothiazole framework, were prepared during the coupling reactions of some diazotized 2-aminobenzo[d]thiazole derivatives with p-acetaminophen. Their structures were elucidated based on NMR and MS spectrometry. The anticancer activity and the safety of the synthesized compounds along with the entire precursors were assessed against three human cancer cell lines and a normal cell line. All the synthesized compounds showed selective cytotoxic activity against the cancer cell lines used in comparison to the normal Vero cell line. Their IC50 values varied from 2.02 to 171.67 μM.The Cameroonian Ministry of Higher Education special research allocation, the German Academic Exchange Service (DAAD) and the University of Pretoria.https://www.arkat-usa.org/arkivoc-journalam2023Paraclinical Science

Cytotoxicity, nitric oxide and acetylcholinesterase inhibitory activity of three limonoids isolated from Trichilia welwitschii (Meliaceae)

BACKGROUND: Limonoids are highly oxygenated compounds with a prototypical structure. Their occurrence in the plant kingdom is mainly confined to plant families of Meliaceae and Rutaceae. Owing to their wide range of pharmacological and therapeutic properties, this study was aimed at investigating the potential nitric oxide (NO) and acetylcholinesterase (AChE) inhibitory activity and the cytotoxicity of three limonoids: trichilia lactone D5 (1), rohituka 3 (2) and dregeanin DM4 (3), isolated from Trichilia welwitschii C.DC RESULTS: Results indicated that the three limonoids had low cytotoxicity towards Vero cells with LC50 values ranging from 89.17 to 75.82 (μg/L. Compounds (2) and (3) had lower cytotoxicity compared to puromycin and doxorubicin used as reference cytotoxic compounds. Compound (1) (LC50 of 23.55 (μg/L) had good antiproliferative activity against RAW 264.7 cancer cells. At the lowest concentration tested (0.5 μg/mL), compound (2) and (3) released the lowest amount of nitric oxide (2.97 and 2.93 μM, respectively). The three limonoids had anti-AChE activity with IC50 values ranged of 19.13 (μg/L for (1), 34.15 (μg/L for (2) and 45.66 (μg/L for (3), compared to galantamine (IC50 of 8.22 ( g/mL) used as positive control CONCLUSION: The limonoid compounds studied in this work inhibited nitric oxide production in LPS-stimulated macrophages and had anti-AChE activity. Trichilia lactone D5 had potential antiproliferative activity against RAW 264.7 cancer cells. The limonoids had low cytotoxicity towards Vero cells lines. This study provided further examples of the importance of limonoids compounds as potential AChE inhibitors and anti-inflammatory agents targeting the inhibition of NO productio

Synthesis and antimicrobial activity of 4′,5,7-trihydroxy-3′- prenylflavanone

4′,5,7-Trihydroxy-3′-prenylflavanone was synthesized and tested for antibacterial effects against Bacillus subtilis, Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa. The synthesized compounds were characterized using UV, IR, MS and 1H and 13C NMR data. The antibacterial screening of the synthesized compounds were performed in vitro by the filter paper disc diffusion method

Anticoccidial constituents from the stem bark of Turraeanthus africanus

International audienceIn order to study some biological active products, phytochemical investigation of the stem bark of Turraeanthus africanus have led to the isolation of a novel compound 1, a new benzoic acid derivative, named turraeanthin C, and two known compounds sesamin (2) and stigmasterol. The structures of these compounds were established by spectral analysis, including two-dimensional nuclear magnetic resonance. The extract and the isolated compounds 1 and 2 showed noteworthy activity against Toxoplasma gondii intracellular parasite in mammals

<a name="home"></a>Effect of Erythrina velutina and Erythrina mulungu in rats submitted to animal models of anxiety and depression

Erythrina velutina (EV) and Erythrina mulungu (EM), popularly used in Brazil as tranquilizing agents, were studied. The effects of acute and chronic oral treatment with a water:alcohol extract of EV (7:3, plant grounded stem bark; acute = 100, 200, 400 mg/kg; chronic = 50, 100, 200 mg/kg) were evaluated in rats (N = 11-12) submitted to the elevated T-maze (for avoidance and escape measurements) model of anxiety. This model was selected for its presumed capacity to elicit specific subtypes of anxiety disorders recognized in clinical practice: avoidance has been related to generalized anxiety and escape to panic. Additionally, animals were treated with the same doses of EV and EM (water:alcohol 7:3, inflorescence extract) and submitted to the forced swim test for the evaluation of antidepressant activity (N = 7-10). Both treatment regimens with EV impaired elevated T-maze avoidance latencies, without altering escape, in a way similar to the reference drug diazepam (avoidance 1, mean ± SEM, acute study: 131.1 ± 45.5 (control), 9.0 ± 3.3 (diazepam), 12.7 ± 2.9 (200 mg/kg), 28.8 ± 15.3 (400 mg/kg); chronic study: 131.7 ± 46.9 (control), 35.8 ± 29.7 (diazepam), 24.4 ± 10.4 (50 mg/kg), 29.7 ± 11.5 (200 mg/kg)). Neither EV nor EM altered measurements performed in the forced swim test, in contrast to the reference drug imipramine that significantly decreased immobility time after chronic treatment. These results were not due to motor alterations since no significant effects were detected in an open field. These observations suggest that EV exerts anxiolytic-like effects on a specific subset of defensive behaviors which have been associated with generalized anxiety disorder