Cytotoxic Activity and Three-Dimensional Quantitative Structure Activity Relationship of 2-Aryl-1,8-naphthyridin-4-ones

Kim, Yong Jin; Kim, Eun Ae; Chung, Mi Lyang; Im, Chaeuk

doi:10.4196/kjpp.2009.13.6.511

Cited by 3 publications

(3 citation statements)

References 19 publications

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“…The cell viability was measured using a MTT-based colorimetric assay as a previously described method with slight modifications [ 23 ]. Briefly, after the treatment of BSA-conjugated FA, cultured cells in 24-well plates were washed with DPBS and incubated with phenol red-free DMEM containing 1 mg/ml MTT for 3 h at 37℃, and then 0.5 ml 2-propanol was added to each well for 30 min.…”

Section: Methodsmentioning

confidence: 99%

The Stimulatory Effect of Essential Fatty Acids on Glucose Uptake Involves Both Akt and AMPK Activation in C2C12 Skeletal Muscle Cells

Park

Kim

Ahn

et al. 2014

Korean J Physiol Pharmacol

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Essential fatty acid (EFA) is known to be required for the body to function normally and healthily. However, the effect of EFA on glucose uptake in skeletal muscle has not yet been fully investigated. In this study, we examined the effect of two EFAs, linoleic acid (LA) and α-linolenic acid (ALA), on glucose uptake of C2C12 skeletal muscle cells and investigated the mechanism underlying the stimulatory effect of polyunsaturated EFAs in comparison with monounsaturated oleic acid (OA). In palmitic acid (PA)-induced insulin resistant cells, the co-treatment of EFAs and OA with PA almost restored the PA-induced decrease in the basal and insulin-stimulated 2-NBDG (fluorescent D-glucose analogue) uptake, respectively. Two EFAs and OA significantly protected PA-induced suppression of insulin signaling, respectively, which was confirmed by the increased levels of Akt phosphorylation and serine/threonine kinases (PKCθ and JNK) dephosphorylation in the western blot analysis. In PA-untreated, control cells, the treatment of 500 µM EFA significantly stimulated 2-NBDG uptake, whereas OA did not. Phosphorylation of AMP-activated protein kinase (AMPK) and one of its downstream molecules, acetyl-CoA carboxylase (ACC) was markedly induced by EFA, but not OA. In addition, EFA-stimulated 2-NBDG uptake was significantly inhibited by the pre-treatment of a specific AMPK inhibitor, adenine 9-β-D-arabinofuranoside (araA). These data suggest that the restoration of suppressed insulin signaling at PA-induced insulin resistant condition and AMPK activation are involved at least in the stimulatory effect of EFA on glucose uptake in C2C12 skeletal muscle cells.

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Section: Methodsmentioning

confidence: 99%

The Stimulatory Effect of Essential Fatty Acids on Glucose Uptake Involves Both Akt and AMPK Activation in C2C12 Skeletal Muscle Cells

Park

Kim

Ahn

et al. 2014

Korean J Physiol Pharmacol

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“…The heterocyclic group of 1,8‐naphthyridin‐4‐one has played a central role in pharmacological activities showing that N ‐1 alkyl substituents influence antibacterial activity and that nitrogen at position 8 controls pharmacokinetics . Their derivatives possess cytotoxic activity against human tumor cells, anticancer effects via inhibition of tublin polymerization, and antibacterial activity . Among them, Gemifloxacin (Factive ® , LG Life Science Company, Daejeon, Korea), which contains 1,8‐naphthy‐ridin‐4‐one nuclei, is widely used for treating chronic bronchitis and pneumonia …”

Section: Methodsmentioning

confidence: 99%

A Novel Synthesis of 1‐Alkyl‐2‐phenyl‐(2,3‐dihydro‐)1,8‐naphthyridin‐4‐ones from 2‐Chloronicotinic Acid

Lee

2015

Bulletin Korean Chem Soc

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“…For example, vinca alkaloids inhibit tubulin polymerization into microtubules and taxoids promote microtubule assembly. Colchicine is another antimitotic agent, but it is not used clinically due to its high toxicity [17]. Some quinazolines are reported to interact with cytoskeleton, induce apoptosis and inhibit DNA topoisomerases [18].…”

Section: Anticancer Activitymentioning

confidence: 99%

Quinazolinone Analogs as Potential Therapeutic Agents

Sharma¹,

Kaur²,

Pahwa

et al. 2011

CMC

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Quinazolinone scaffold has been considered as a magic moiety possessing myriad spectrum of medicinal activities. Diversity of biological response profile has attracted considerable interest of several researchers across the globe to explore this skeleton for its assorted therapeutic significance. Various novel classes of structurally different quinazolinones have been designed and synthesized depicting potential interventions such as antibacterial, antifungal, antiviral, anticonvulsant, CNS depressant, antiinflammatory, antihistaminic, anticancer and so on. Moreover, the nucleus constitutes an integral structural component in a number of drugs currently employed in several clinical therapies. The present paper is an earnest attempt to provide an insight view on the current medicinal aspects of quinazolinone heterocycles alongwith brief discussion of their chemistry.

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Cytotoxic Activity and Three-Dimensional Quantitative Structure Activity Relationship of 2-Aryl-1,8-naphthyridin-4-ones

Cited by 3 publications

References 19 publications

The Stimulatory Effect of Essential Fatty Acids on Glucose Uptake Involves Both Akt and AMPK Activation in C2C12 Skeletal Muscle Cells

The Stimulatory Effect of Essential Fatty Acids on Glucose Uptake Involves Both Akt and AMPK Activation in C2C12 Skeletal Muscle Cells

A Novel Synthesis of 1‐Alkyl‐2‐phenyl‐(2,3‐dihydro‐)1,8‐naphthyridin‐4‐ones from 2‐Chloronicotinic Acid

Quinazolinone Analogs as Potential Therapeutic Agents

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