Synthesis and effects of some novel tetrahydronaphthalene derivatives on proliferation and nitric oxide production in lipopolysaccharide activated Raw 264.7 macrophages

Gürkan, Ali; Karabay, Arzu Zeynep; Büyükbingöl, Zeliha; Büyükbingöl, Erdem

doi:10.1016/j.ejmech.2010.11.021

Cited by 12 publications

(11 citation statements)

References 52 publications

(59 reference statements)

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“…Production of excessive NO has been associated with a range of inflammatory diseases including arteriosclerosis, ischemic reperfusion, hypertension and septic shock (25,26). Recent studies have demonstrated that the plant foods including fruits, vegetables and medicinal herbs are an excellent source of antioxidant molecules that effectively inhibit the inflammatory process by affecting different molecular targets (27,28). In this study, methanol extract of D. atrovirens bark exhibited a higher level of total phenolics when compared with other extracts.…”

Section: Inhibition Of Nitric Oxide Production In Lpsstimulated Raw 2mentioning

confidence: 67%

Inhibition of Nitric Oxide Production in LPS-Stimulated Raw 264.7 Cells by Dolichandrone Atrovirens Bark

Deepa¹,

Sowndhararajan

Kim

et al. 2019

krj

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In traditional systems of medicine, the bark of Dolichandroneatrovirens has been used to treat various disorders. The main aim of this study was to determine the anti-inflammatory effect of D. atrovirens bark through the inhibition of nitric oxide (NO) production in lipopolysaccharide-stimulated RAW 264.7 cells.For this purpose, preliminary phytochemical composition and in vitro antioxidant activities of various solvent extracts of D. atrovirens bark were evaluated to select the most effective extract.The methanol extract of D.atrovirens registered the highest amount of total phenolics (476.2 mg GAE/g) and flavonoid (129.0 mg RE/g)contents witha strong antioxidant activity as measured in DPPH (IC50 of 19.52 μg/mL) and ABTS (IC50of 10.82 μg/mL) scavenging activities.Hence, the methanol extract was selected for cell line study. Further, the methanol extract of D. atrovirens effectively inhibited the production of NO in RAW 264.7 cells induced by LPS (13.1 μM at the concentration of 80 μg/mL). It could be concluded that the presence of higher level of total phenolic components in the methanol extract of D. atrovirens bark might be responsible for reducing the NO level in cells.

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Section: Inhibition Of Nitric Oxide Production In Lpsstimulated Raw 2mentioning

confidence: 67%

Inhibition of Nitric Oxide Production in LPS-Stimulated Raw 264.7 Cells by Dolichandrone Atrovirens Bark

Deepa¹,

Sowndhararajan

Kim

et al. 2019

krj

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“…Cytotoxicity to A549 Cells and RAW264.7 Cells The cytotoxic activities of caffeoyl salicylaldehydes (A1-A13) and caffeoyl salicylates (B1-B13) were evaluated by the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) method 9) using adenocarcinomic human alveolar basal epithelial cells A549 and macrophage cells RAW264.7, respectively. As shown in Fig.…”

Section: Biological Activitymentioning

confidence: 99%

“…Assay for Cytotoxic Activity Compounds A1-A13, B1-B13, and D104 were assayed according to the MTT test 9) under the concentration of 50 µM against A549 cells. Moreover, compounds B1-B13 and D104 were also chosen to test the cytotoxic effects against RAW264.7 cells under the two concentrations (25 and 50 µM).…”

Section: Biological Evaluationmentioning

confidence: 99%

Structural Optimization of Caffeoyl Salicylate Scaffold as NO Production Inhibitors

Pan

Xia

et al. 2019

Chem. Pharm. Bull.

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Chlorogenic acid (CGA) has been considered as one of important active components in a number of medicinal herbs. Recently our group demonstrated that caffeoyl salicylate scaffold derived from CGA can be employed for the development of novel anti-inflammatory agents. The most active compound D104 can be a very promising starting point for the further structural optimization. A series of novel caffeoyl salicylate analogs were designed, synthesized, and evaluated by preliminary biological evaluation. The obtained results showed that the two compounds B12 and B13 can not only inhibit production of nitric oxide (NO) in RAW264.7 cells induced by lipopolysaccharides (LPS) effectively, but also have high safety in in vitro cytotoxic test, which could be comparable with D104. Molecular docking study on the peroxisome proliferatoractivated receptor γ (PPARγ) protein revealed that compounds B12 and B13 can follow the same binding mode with D104, and the carboxyl group of caffeoyl salicylate scaffold might play a key role in the interaction with protein target, which implied the carboxyl group should be retained in the further optimization.

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“…Twenty-seven newly synthesized retinoid derivatives [26], N-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalene-2-yl)-carboxamides (6-15) and 5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene-2-carboxamides (16-32) were screened for their cytotoxic activity in cancer cells by the SRB assay. T47D breast, Huh7 liver and HCT116 colon cancer cells were treated with the compounds and with ATRA, and their IC 50 values were determined (Supplementary Table 1 and Supplementary document 1).…”

Section: Cytotoxic Activity Of Retinoids In Cancer Cellsmentioning

confidence: 99%

“…In this study, we tested previously synthesized retinoid derivatives [26] for their cytotoxicity in a series of breast cancer cell lines. We then further studied compound 17, which showed the most anti-proliferative activity, to identify its mechanism of action at the molecular level.…”

Section: Introductionmentioning

confidence: 99%

Retinoid N-(1H-benzo[d]imidazol-2-yl)-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene-2-carboxamide induces p21-dependent senescence in breast cancer cells

et al. 2016

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Retinoids have been implicated as pharmacological agents for the prevention and treatment of various types of cancers, including breast cancers. We analyzed 27 newly synthesized retinoids for their bioactivity on breast, liver, and colon cancer cells. Majority of the retinoids demonstrated selective bioactivity on breast cancer cells. Retinoid 17 had a significant inhibitory activity (IC50 3.5 μM) only on breast cancer cells while no growth inhibition observed with liver and colon cancer cells. The breast cancer selective growth inhibitory action by retinoid 17 was defined as p21-dependent cell death, reminiscent of senescence, which is an indicator of targeted receptor mediated bioactivity. A comparative analysis of retinoid receptor gene expression levels in different breast cancer cells and IC50 values of 17 indicated the involvement of Retinoid X receptors in the cytotoxic bioactivity of retinoid 17 in the senescence associated cell death. Furthermore, siRNA knockdown studies with RXRγ induced decrease in cell proliferation. Therefore, we suggest that retinoid derivatives that target RXRγ, can be considered for breast cancer therapies.

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Synthesis and effects of some novel tetrahydronaphthalene derivatives on proliferation and nitric oxide production in lipopolysaccharide activated Raw 264.7 macrophages

Cited by 12 publications

References 52 publications

Inhibition of Nitric Oxide Production in LPS-Stimulated Raw 264.7 Cells by Dolichandrone Atrovirens Bark

Inhibition of Nitric Oxide Production in LPS-Stimulated Raw 264.7 Cells by Dolichandrone Atrovirens Bark

Structural Optimization of Caffeoyl Salicylate Scaffold as NO Production Inhibitors

Retinoid N-(1H-benzo[d]imidazol-2-yl)-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene-2-carboxamide induces p21-dependent senescence in breast cancer cells

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