http://www.bdpsjournal.org/index.php/bjp/issue/feed||| Bangladesh Journal of Pharmacology |||2024-03-22T21:13:52-04:00Mir Misbahuddindgdabd@gmail.comOpen Journal Systemshttp://www.bdpsjournal.org/index.php/bjp/article/view/1004Synthesis, molecular modeling, anti-cancer and COX-1/2 inhibitory activities of novel thiazolidinones containing benzothiazole core2024-03-17T22:29:15-04:00Necla Kulabaskucukguzel@hotmail.comCansu Tamniku Guvenkucukguzel@hotmail.comMerve Tamniku Duracıkkucukguzel@hotmail.comOzlem Bingol Ozakpınarkucukguzel@hotmail.comİlkay Bingol Kucukguzelkucukguzel@hotmail.com<p>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. <em>In vitro</em>, 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 <strong>3</strong>-<strong>12</strong> were also screened for their COX-1 and COX-2 inhibitory activities. Of these compounds, <strong>4</strong> 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. <em>In silico</em> 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.</p>2024-03-15T20:07:08-04:00##submission.copyrightStatement##http://www.bdpsjournal.org/index.php/bjp/article/view/1005Berberine triggers necroptosis of cervical H8 cells by activating receptor-interacting protein kinase 12024-03-22T20:10:25-04:00Mengting Wangzhouyuzhen100@sina.comHuixian Chenzhouyuzhen100@sina.comQian Wuzhouyuzhen100@sina.comYan Huangzhouyuzhen100@sina.comYuzhen Zhouzhouyuzhen100@sina.com<p>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.</p>2024-03-15T20:07:47-04:00##submission.copyrightStatement##http://www.bdpsjournal.org/index.php/bjp/article/view/1006In vitro anti-cancer activity of Epipremnum aureum2024-03-22T20:42:46-04:00Sudhir S. Patilsudhirs.pharmac@gmail.comKiran A. Wadkarsudhirs.pharmac@gmail.com<p>In the present study, <em>in vitro </em>anti-cancer activity of aerial parts of <em>Epipremnum aureum </em>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 IC<sub>50</sub> values of 32.9 and 45.8 μg/mL respectively, while the conventional medication 5-fluorouracil produced an IC<sub>50</sub> value of 19.2 μg/mL. The microscopic examination of the chloroform and ethanol extracts of <em>E. aureum</em> revealed the presence of apoptotic bodies, nuclear fragmentation, and tiny nuclei with strong chromatin condensation. These results suggest that chloroform extract of <em>E. aureum</em> is more effective against breast cancer. </p>2024-03-15T20:08:22-04:00##submission.copyrightStatement##http://www.bdpsjournal.org/index.php/bjp/article/view/1007Nigella sativa plant extract inhibits the proliferation of MDA-MB-231 breast cancer cells via apoptosis and cell cycle arrest2024-03-22T21:13:52-04:00Jie Majiema.onco@hotmail.comCong Pengjiema.onco@hotmail.com<p>The study was designed to evaluate the antiproliferative effects of <em>Nigella sativa</em> 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 <em>N. sativa</em> extract significantly (p<0.05) impeded the growth of MDA-MB-231 cells, with IC<sub>50</sub> of 12.5 μg/mL. The colony-forming potential of MDA-MB-231 was significantly (p<0.05) decreased by the <em>N. sativa</em> 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 <em>N. sativa </em>extract triggered G<sub>0</sub>/G<sub>1</sub> phase arrest in MDA-MB-231 cells. Collectively, <em>N. sativa</em> extract exhibits potent antiproliferative activity against triple-negative breast cancer cells and may be used as a source of anti-cancer agents.</p>2024-03-15T20:08:56-04:00##submission.copyrightStatement##http://www.bdpsjournal.org/index.php/bjp/article/view/1008Anti-diabetic activity of Calathea anulque2024-03-15T20:09:55-04:00Saranya Shankarsmythili@vit.ac.inChitrashalini Srinivasansmythili@vit.ac.inMythili Sathiavelusmythili@vit.ac.in<p>No abstract</p>2024-03-15T20:09:25-04:00##submission.copyrightStatement##