title

ساختار بتا لاکتام 4-(4-(Methylsulfonyl) phenyl)-1-pentyl-3-phenoxyazetidin-2-one به طور انتخابی میتوکندری های B لنفوسیت های سرطانی را مورد هدف قرار میدهند.

پیراحمدی, نهال and زرقی, افشین and سلیمی, احمد and عارفی, هادی and پوراحمد, جلال (1396) ساختار بتا لاکتام 4-(4-(Methylsulfonyl) phenyl)-1-pentyl-3-phenoxyazetidin-2-one به طور انتخابی میتوکندری های B لنفوسیت های سرطانی را مورد هدف قرار میدهند. Anti-Cancer Agents in Medicinal Chemistry ــ 17 (9). pp. 1292-1301. شاپا 1871-5206

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Title

β-lactam Structured, 4-(4-(Methylsulfonyl) phenyl)-1-pentyl-3-phenoxyazetidin-2-one: Selectively Targets Cancerous B Lymphocyte Mitochondria

English Abstract

Background: β lactam-structured Cox-2 inhibitors, possesses anti-proliferative and anti-inflammatory effects. Objective: In this research, the actions of a synthetic β lactam-structured Cox-2 inhibitor with 4-(4- (Methylsulfonyl) phenyl)-1-pentyl-3-phenoxyazetidin-2-one on cellular viability of cancerous lymphoblast obtained from patients with acute lymphocytic leukemia (ALL) and normal lymphocytes obtained from healthy donors were compared. Methods: % the cell viability of cancerouslymphoblasts and normal lymphocytes treated with β lactam derivatives were assayed with MTT test. Early apoptosis and necrosis were detected by double staining of annexin V/ propidium iodide and activity of caspase 3 as the final mediator in apoptotic mode of cell death was evaluated by colorimetric assay. Results: Our results showed that β lactam derivatives inhibited the proliferation of cancerous lymphoblast but not normal lymphocytes in a concentration-dependent mode by inducing apoptosis. Treatment with β lactam derivatives resulted in a rapid loss of mitochondrial trans-membrane potential and induction of reactive oxygen species (ROS) formation, and cytochrome c release in cytosol of mitochondria resulted in activation of procaspase-9 and formation of active apoptosome. Conclusion: These findings suggest that 4-(4-(Methylsulfonyl)phenyl)-1-pentyl-3-phenoxyazetidin-2-one as a β lactam could induce ROS-mediated death signaling throughmitochondrial pathway that results in apoptosis in only cancerous lymphoblast cells. The stimulationof apoptosis by β lactams may provide a pivotal mechanismfor their anticancer effect in acute lymphocytic leukemia cells

Item Type:Article
زبان سند : انگلیسی
نویسنده اول :نهال پیراحمدی
نویسنده :افشین زرقی
نویسنده :احمد سلیمی
نویسنده :هادی عارفی
نویسنده مسئول :جلال پوراحمد
Additional Information:IF:2.556 Indexed in: ISI, PubMed/Medline, Scopus, EMBASE
کلیدواژه ها (انگلیسی):Mitochondria; acute lymphocytic leukemia; apoptosis; cox-2 inhibitors; β lactam
Subjects:QV pharmacology > QV 600 Toxicology
QV pharmacology
Divisions:School of Pharmacy > Department of Toxicology
ID Code:9472
Deposited By: Dr Ahmad Salimi
Deposited On:18 Sep 1396 10:20
Last Modified:24 Jan 1401 11:25

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  • ساختار بتا لاکتام 4-(4-(Methylsulfonyl) phenyl)-1-pentyl-3-phenoxyazetidin-2-one به طور انتخابی میتوکندری های B لنفوسیت های سرطانی را مورد هدف قرار میدهند. (deposited 18 Sep 1396 10:20) [Currently Displayed]

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