Anticancer and antiangiogenesis activities of novel synthesized 2-substitutedbenzimidazoles molecules

Güner, Adem; Polatlı, Elifsu; Akkan, Tamer; Bektaş, Hakan; Albay, Canan

doi:10.3906/kim-1904-46

Cited by 14 publications

(6 citation statements)

References 38 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The new 2-substituted benzimidazole molecules with heterocyclic were synthesized, in which compound 2 had the best activity of anti-proliferation without genotoxicity in PC-3 and SK-BR-3 cancer cells (IC50 < 20 μg/ml) and anti-angiogenesis in CAM assay ( Güner et al, 2019 ). The IPA(8k), a novel indolephenoxyacetamide analog with anti-proliferative activity against A549 (IC50 ∼5 uM), performed anti-angiogenic activity in vivo and in vitro through inhibiting HIF-1 alpha, VEGF, MMP-2 and -9, and P53 ( Al-Ostoot et al, 2021 ).…”

Section: The Analogs From Medical Chemistrymentioning

confidence: 99%

Co-Targeting Tumor Angiogenesis and Immunosuppressive Tumor Microenvironment: A Perspective in Ethnopharmacology

et al. 2022

View full text Add to dashboard Cite

Tumor angiogenesis is one of the most important processes of cancer deterioration via nurturing an immunosuppressive tumor environment (TME). Targeting tumor angiogenesis has been widely accepted as a cancer intervention approach, which is also synergistically associated with immune therapy. However, drug resistance is the biggest challenge of anti-angiogenesis therapy, which affects the outcomes of anti-angiogeneic agents, and even combined with immunotherapy. Here, emerging targets and representative candidate molecules from ethnopharmacology (including traditional Chinese medicine, TCM) have been focused, and they have been proved to regulate tumor angiogenesis. Further investigations on derivatives and delivery systems of these molecules will provide a comprehensive landscape in preclinical studies. More importantly, the molecule library of ethnopharmacology meets the viability for targeting angiogenesis and TME simultaneously, which is attributed to the pleiotropy of pro-angiogenic factors (such as VEGF) toward cancer cells, endothelial cells, and immune cells. We primarily shed light on the potentiality of ethnopharmacology against tumor angiogenesis, particularly TCM. More research studies concerning the crosstalk between angiogenesis and TME remodeling from the perspective of botanical medicine are awaited.

show abstract

Section: The Analogs From Medical Chemistrymentioning

confidence: 99%

Co-Targeting Tumor Angiogenesis and Immunosuppressive Tumor Microenvironment: A Perspective in Ethnopharmacology

et al. 2022

View full text Add to dashboard Cite

show abstract

“…The anti-angiogenic potential of compounds 3c-f, cisplatin, and their combinations were determined by a chorioallantoic membrane model on fertilized hen eggs with a slight change of the procedure of [11]. Fertile Leghorn chicken eggs weighing 50-60 g purchased from commercial sources (Giresun, Turkey).…”

Section: Antiangiogenic Activitymentioning

confidence: 99%

Novel coumarin compounds potentiate the effect of cisplatin on lung cancer cells by enhancing pro-apoptotic gene expressions, G2/M cell arrest, oxidative and antiangiogenic effects

Güner¹,

Bektaş²,

Menteşe³

2021

Preprint

Self Cite

View full text Add to dashboard Cite

Coumarin is a functional compound with a pronounced wide range of biological activities and has recently been shown to have anticancer effects on various human cancer cells. Cisplatin is widely used in the treatment of many cancers but its effectiveness is limited due to acquired resistance and dose-related side effects. This study aimed to reveal the chemosensitizing ability of novel synthesized coumarin-triazole hybrid compounds (3a-f) alone or their combination with cisplatin in A549 cells.MTT assay was used for cytotoxic effects. Lactate dehydrogenase (LDH), antioxidant/oxidant status, DNA fragmentation were determined spectrophotometrically by using commercial kits. Muse™ Cell Analyzer was used to assess cell cycle progression. Pro/anti-apoptotic gene expressions were determined by Real-Time qPCR. The antiangiogenic activity was determined by VEGF expression and Hen's chorioallantoic membrane model. Compounds 3c, d, e, and f potentiated the cisplatin-induced cytotoxicity through the increase of LDH release and DNA fragmentation, induced G2/M cell cycle arrest, overproduction of oxidative stress, and decrease of cellular antioxidant levels. These compounds combined with cisplatin caused upregulation in the pro-apoptotic Bax, Bıd, caspase-3, caspase-8, caspase-9, Fas, and p53 gene expressions while downregulating anti-apoptotic DFFA, NFkB1, and Bcl2 gene expressions. These combinations caused vascular loss and a reduction in VEGF expression. These results suggest that a combinational regimen of coumarin compounds with cisplatin overcome the acquired resistance of cancer cells to cisplatin and, considering compounds have relatively low toxicity in normal cells, decrease the dose requirement of cisplatin in cancer treatments.

show abstract

“…The irritation effects of DMAA and cDMAA were assessed by using the chorioallantoic membrane model on fertilized hen eggs, with a slight modification of the described protocol [29]. Fertile Leghorn chicken eggs weighing 50-60 g were obtained from commercial sources.…”

Section: Hen's Egg Chorioallantoic Membrane (Het-cam) Irritation Testmentioning

confidence: 99%

Examination of some toxicological parameters of dimethylamylamine when consumed alone or with caffeine

Güner

Türkez

2020

Arch biol sci (Beogr)

Self Cite

View full text Add to dashboard Cite

Dimethylamylamine (DMAA) is a bodybuilding supplement with fat-burner or performanceenhancing properties. DMAA is often combined with caffeine to enhance its effectiveness and this can have serious adverse effects on health. In this study, we examined for the first time the cytotoxic, oxidative and genotoxic effects of DMAA in the presence or absence of caffeine in lymphocytes cultured from human blood, and its vascular irritant effects in a hen's chorioallantoic membrane egg test. Cytotoxic effects were observed by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT), lactate dehydrogenase release (LDH), which serves as a measure of cell membrane damage, changes in the mitotic index (MI) and proliferative rate index (PRI) assays. Oxidative changes were evaluated by the total antioxidant activity and the total oxidative status assay. Genotoxic damage was analyzed by chromosomal aberration and micronucleus assays. DMAA and its combination with caffeine (cDMAA) had no genotoxic effects. DMAA (1000 mg/L) and cDMAA (500 and 1000 mg/L) decreased cell viability while significantly increasing LDH activity, MI and the oxidative level. DMAA and cDMAA caused weak and moderate vascular irritant effects, respectively. In conclusion, DMAA exhibits cytotoxic effects via membrane dysfunction and mitotic disturbance following increased oxidative stress in a dose- and caffeine-dependent manner.

show abstract

Anticancer and antiangiogenesis activities of novel synthesized 2-substitutedbenzimidazoles molecules

Cited by 14 publications

References 38 publications

Co-Targeting Tumor Angiogenesis and Immunosuppressive Tumor Microenvironment: A Perspective in Ethnopharmacology

Co-Targeting Tumor Angiogenesis and Immunosuppressive Tumor Microenvironment: A Perspective in Ethnopharmacology

Novel coumarin compounds potentiate the effect of cisplatin on lung cancer cells by enhancing pro-apoptotic gene expressions, G2/M cell arrest, oxidative and antiangiogenic effects

Examination of some toxicological parameters of dimethylamylamine when consumed alone or with caffeine

Contact Info

Product

Resources

About