||| Bangladesh Journal of Pharmacology |||

Synthesis, molecular modeling, anti-cancer and COX-1/2 inhibitory activities of novel thiazolidinones containing benzothiazole core

Fri, 15 Mar 2024 20:07:08 -0400

In this study, new 1,3-thiazolidin-4-one derivatives containing arylmethylene groups in the 5-position were obtained from 6-(trifluoromethoxy)-1,3-benzothiazol-2-amine (riluzole). Synthesized compounds were characterized by spectral data and elemental analysis. In vitro, cytotoxic activities of the synthesized molecules were evaluated against the human lung cancer (A549) and human prostate cancer (PC-3) cell lines. Compounds were also tested on mouse embryonic fibroblast cells (NIH/3T3) to determine selectivity. Ten target compounds 3-12 were also screened for their COX-1 and COX-2 inhibitory activities. Of these compounds, 4 showed the highest COX-2 inhibition at 10 μM. Molecular docking calculations were performed to understand the binding interactions of compounds with COX-1 and COX-2 proteins. In silico studies of the tested compounds represented important binding modes that may be responsible for their anti-cancer activity via selective inhibition of the COX-2 enzyme. ADMET predictions were conducted to assess the drug-like properties of the novel compounds.

Berberine triggers necroptosis of cervical H8 cells by activating receptor-interacting protein kinase 1

Mengting Wang, Huixian Chen, Qian Wu, Yan Huang, Yuzhen Zhou — Fri, 15 Mar 2024 20:07:47 -0400

This study aims to investigate the effect of berberine on necroptosis in cervical H8 cells. CCK-8 assay was used to assess cell proliferation activity. The expression levels of necroptosis key markers Receptor-interacting protein kinase 1 (RIPK1), MLKL, p-MLKL, and apoptosis-related caspase-8, caspase-3 were analyzed through qRT-PCR, western blot, and immunofluorescence. Mechanistic studies were conducted using the RIPK1 kinase inhibitor necrostatin-1 (Nec-1). The results showed that berberine could inhibit H8 cell proliferation in a time- and dose-dependent manner (p<0.05). It increased the expression of RIPK1 and MLKL (p<0.05), while inhibiting the expression of caspase-8 and caspase-3 (p<0.05). Nec-1 inhibitor decreased the expression of RIPK1 and MLKL after the intervention of berberine (p<0.05). Therefore, berberine induces cervical H8 cell death through the activation of RIPK1-mediated necroptosis.

In vitro anti-cancer activity of Epipremnum aureum

Sudhir S. Patil, Kiran A. Wadkar — Fri, 15 Mar 2024 20:08:22 -0400

In the present study, in vitro anti-cancer activity of aerial parts of Epipremnum aureum extracts was performed using the MCF-7 breast cancer cell line. Soxhlet method was used with different solvents for extract preparation. The amount of apoptosis in MCF-7 cells was assessed using flow cytometry for each of the extracts. The chloroform and ethanol extracts had a considerable cytotoxic effect with IC₅₀ values of 32.9 and 45.8 μg/mL respectively, while the conventional medication 5-fluorouracil produced an IC₅₀ value of 19.2 μg/mL. The microscopic examination of the chloroform and ethanol extracts of E. aureum revealed the presence of apoptotic bodies, nuclear fragmentation, and tiny nuclei with strong chromatin condensation. These results suggest that chloroform extract of E. aureum is more effective against breast cancer.

Nigella sativa plant extract inhibits the proliferation of MDA-MB-231 breast cancer cells via apoptosis and cell cycle arrest

Jie Ma, Cong Peng — Fri, 15 Mar 2024 20:08:56 -0400

The study was designed to evaluate the antiproliferative effects of Nigella sativa plant ethanol extract against MDA-MB-231 triple-negative breast cancer cells. DAPI and annexin V/propidium iodide staining assays were used to examine apoptosis. Results showed that N. sativa extract significantly (p<0.05) impeded the growth of MDA-MB-231 cells, with IC₅₀ of 12.5 μg/mL. The colony-forming potential of MDA-MB-231 was significantly (p<0.05) decreased by the N. sativa extract-induced apoptosis. Increased expression of Bax, caspase-3, cleaved caspase-3, and cleaved PARP was also observed in the extract-treated MDA-MB-231 cells. Moreover, flow cytometric analysis showed that N. sativa extract triggered G₀/G₁ phase arrest in MDA-MB-231 cells. Collectively, N. sativa extract exhibits potent antiproliferative activity against triple-negative breast cancer cells and may be used as a source of anti-cancer agents.

Anti-diabetic activity of Calathea anulque

Saranya Shankar, Chitrashalini Srinivasan, Mythili Sathiavelu — Fri, 15 Mar 2024 20:09:25 -0400

No abstract