Design, synthesis and exploring the quantitative structure–activity relationship of some antioxidant flavonoid analogues

Das, Shantanu; Mitra, Indrajit; Batuta, Shaikh; Alam, Md. Niharul; Roy, Kunal; Begum, Naznin Ara

doi:10.1016/j.bmcl.2014.09.028

Cited by 52 publications

(23 citation statements)

References 13 publications

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“…Very recently, quantitative structure-activity data have been generated, regarding antioxidant (Das et al, 2014) and anti-cancer (Jung et al, 2015) effects of flavonoids and analogues. While this is valuable data, we followed a broader approach, addressing multiple cellular properties related to cell-toxicity, caused by several structurally related chalcones.…”

Section: Introductionmentioning

confidence: 99%

In vitro structure-toxicity relationship of chalcones in human hepatic stellate cells

et al. 2015

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CitationIn vitro structure-toxicity relationship of chalcones in human hepatic stellate cells 2015 Toxicology This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. In vitro AbstractXanthohumol (XN), the major prenylated chalcone from hops (Humulus lupulus L.), has received much attention within the last years, due to its multiple pharmacological activities including anti-proliferative, anti-inflammatory, antioxidant, pro-apoptotic, anti-bacterial and anti-adhesive effects. However, there exists a huge number of metabolites and structurallyrelated chalcones, which can be expected, or are already known, to exhibit various effects on cells. We have therefore analyzed the effects of XN and 18 other chalcones in a panel, consisting of multiple cell-based assays. Readouts of these assays addressed distinct aspects of cell-toxicity, like proliferation, mitochondrial health, cell cycle and other cellular features. Besides known active structural elements of chalcones, like the Michael system, we have identified several moieties that seem to have an impact on specific effects and toxicity in human liver cells in vitro. Based on these observations, we present a structure-toxicity model, which will be crucial to understand the molecular mechanisms of wanted effects and unwanted side-effects of chalcones.

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Section: Introductionmentioning

confidence: 99%

In vitro structure-toxicity relationship of chalcones in human hepatic stellate cells

et al. 2015

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“…Basically, flavonoids and its classes bears low molecular weight, which exists various biodynamic properties such as antioxidant, antimicrobial activity, anti-allergic, anti-inflammatory, hepatoprotective, antimutagenic effects and also inhibit various enzymes. [3][4][5][6][7][8][9] There are many herbal extracts having reported anti-diabetic potentials. 10 Among these phytochemicals, flavonoids and their related natural compounds are known to possess anti-diabetic activity, established in various animal models.…”

Section: Introductionmentioning

confidence: 99%

Antidiabetic Potential of Flavones on Streptozotocin-induced Diabetes Mellitus in Rat

Inam

Verma

et al. 2019

IJPI

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Objectives: The objective of the study was to develop new antidiabetic agents from synthetic route. Methods: An attempt was made to synthesize various flavones. The structures of the compounds were elucidated by UV, IR, 1 H-NMR and mass spectrometry. Furthermore, an in vivo antidiabetic activity study was carried out by streptozotocin induced model. Biochemical parameters were extensively studied to support anti-diabetic potential of synthesized flavones. Results: The study reveals that flavones such as F1, F2, F3, F5 and F8 were potentially considered for in-vivo antidiabetic activity. Fasting blood glucose and biochemical parameters like total protein, urea and creatinine, SGOT, SALP and SGPT were performed for the biological evaluation and compared with that of standard glibenclamide (5 mg/kg). Among the five consolidated flavones, F8 possess high significant (p < 0.01) results and restores the blood glucose level, liver enzymes and renal parameters. Based on these results, a promising potent drug would be developed in the management of diabetes mellitus. Conclusion: In-vivo evaluations of selected compounds were carried out for its antidiabetic activity considering different biochemical parameters. Some of the selected flavones showed excellent and noticeable antidiabetic activity.

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“…Apart from these commonly known applications, QSAR has also been used to model and design chemicals with special uses (such as antioxidants [1,2], odorants [3,4], sweetening agents [5,6]). However, in combination with receptor-based approaches, it has demonstrated useful applications and has had success for the optimization of ligands in the context of drug discovery.…”

Section: Introductionmentioning

confidence: 99%

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Understanding the Basics of QSAR for Applications in Pharmaceutical Sciences and Risk Assessment

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Design, synthesis and exploring the quantitative structure–activity relationship of some antioxidant flavonoid analogues

Cited by 52 publications

References 13 publications

In vitro structure-toxicity relationship of chalcones in human hepatic stellate cells

In vitro structure-toxicity relationship of chalcones in human hepatic stellate cells

Antidiabetic Potential of Flavones on Streptozotocin-induced Diabetes Mellitus in Rat

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