Flavonoids as a scaffold for development of novel anti-angiogenic agents: An experimental and computational enquiry

Gacche, Rajesh N.; Meshram, Rohan J.; Shegokar, Harshala D.; Gond, Dhananjay S.; Kamble, Sonali S.; Dhabadge, V.N.; Utage, Bhimashankar; Patil, Kapil; More, Rahul A.

doi:10.1016/j.abb.2015.04.009

Cited by 29 publications

(16 citation statements)

References 84 publications

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“…In 2015 a group of researchers (Gacche et al., 2015) has published a study on flavonoids (flavones, flavonones, and flavonols) with antiangiogenic, cytotoxic, antioxidant, and cyclooxygenase (COX) inhibitory activities. To study the biological effects of these flavonoids, in vivo chorioallantoic membrane model (CAM) was used together with computational methods such as in silico docking to calculate the different atomic interactions and to design novel and active flavonoid derivatives.…”

Section: Biological Activitiesmentioning

confidence: 99%

“…To study the biological effects of these flavonoids, in vivo chorioallantoic membrane model (CAM) was used together with computational methods such as in silico docking to calculate the different atomic interactions and to design novel and active flavonoid derivatives. Furthermore, this research describes the cytotoxicity of flavonoids against selected cancer cell lines using 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) cell viability assay (Gacche et al., 2015). Flavonoids can affect inflammation.…”

Section: Biological Activitiesmentioning

confidence: 99%

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Evaluation of the status quo of polyphenols analysis: Part I—phytochemistry, bioactivity, interactions, and industrial uses

Sanches-Silva

Reboredo‐Rodríguez

Süntar

et al. 2020

Comp Rev Food Sci Food Safe

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Phytochemicals, especially polyphenols, are gaining more attention from both the scientific community and food, pharmaceutical, and cosmetics industries due to their implications in human health. In this line, lately new applications have emerged, and of great importance is the selection of accurate and reliable analytical methods for better evaluation of the quality of the end-products, which depends on diverse process variables as well as on the matrices and on the physicochemical properties of different polyphenols. The first of a two-part review on polyphenols will address the phytochemistry and biological activities of different classes of polyphenols including flavonoids, lignans and flavanolignans, stilbenoids, tannins, curcuminoids, and coumarins. Moreover, the possible interactions of polyphenols and current and potential industrial applications of polyphenols are discussed. K E Y W O R D S bioactivity, flavonoid, industrial uses, phytochemistry, plant-based food, polyphenol, possible interactions How to cite this article: Silva AS, Reboredo-Rodríguez P, Süntar I, et al. Evaluation of the status quo of polyphenols analysis: part iphytochemistry, bioactivity, interactions and industrial uses.

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Section: Biological Activitiesmentioning

confidence: 99%

Section: Biological Activitiesmentioning

confidence: 99%

Evaluation of the status quo of polyphenols analysis: Part I—phytochemistry, bioactivity, interactions, and industrial uses

Sanches-Silva

Reboredo‐Rodríguez

Süntar

et al. 2020

Comp Rev Food Sci Food Safe

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show abstract

“…Thus, truancy of oxo group can be considered as an important factor that determines the thermodynamic stability of flavonoids in AR active site. Moreover, presence of 2-3 double bond is considered as a key determinant of bioactivity in case of flavonoids (Gacche et al 2015). This preposition is again supported by in vitro experimental observations from current study that catechin and epigallocatechin gallate has higher IC 50 values in comparison with remaining compounds.…”

Section: Molecular Docking Studiesmentioning

confidence: 99%

Dietary flavonoids inhibit the glycation of lens proteins: implications in the management of diabetic cataract

et al. 2019

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The intervention of functional foods as complementary therapeutic approach for the amelioration of diabetes and sugar induced cataractogenesis is more appreciated over the present day chemotherapy agents owing to their nontoxic and increased bioavailability concerns. Dietary flavonoids, a class of bioactive phytochemicals is known to have wide range of biological activities against variety of human ailments. In the present study, we demonstrate anti-cataract effect of eight dietary flavonoids in sugar induced lens organ culture study. We present data on processes like inhibition of glycation-induced lens cloudiness, lens protein aggregation, glycation reaction and advanced glycation end products formation that can act as biochemical markers for this disease. The selected flavonoids were also tested for their aldose reductase (AR) inhibition (experimental and in silico). The molecular dynamics simulation results shed light on mechanistic details of flavonoid induced AR inhibition. The outcome of the present study clearly focuses the significance of kaempferol, taxifolin and quercetin as potential candidates for controlling diabetic cataract.

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“…10 Due to their anti-oxidant and anti-inflammatory activities, flavones have long been used to treat inflammatory diseases such as arthritis and asthma 11 Chromone, 1,4-benzopyrone-4-one, is a central chemical scaffold for flavones, 12 with chromone scaffoldcontaining derivatives (CSD) being a diverse family, with branching chemical residues coupled to this core chemical scaffold. 13 We recently reported that eupatilin, a CSD from an Artemisia species, dramatically inhibits lipopolysaccharide (LPS)-induced osteoporosis, partially via actin depolymerization 14 and the downregulation of multiple genes associated with the epithelial-mesenchymal transition (EMT). The present study shows that a noble CSD, ONG41008, can block the induction of Type 2 EMT, also called fibrogenesis, arrest cell growth and alter cell morphology, thereby substantially ameliorating lung fibrosis.…”

Section: Introductionmentioning

confidence: 99%

A noble TGF beta biogenesis inhibitor exhibits both potent anti-fibrotic and anti-inflammatory capabilities

Kim

Meang²,

Kim³

et al. 2019

Preprint

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Fibrosis is caused by the proliferation of pathogenic myofibroblasts and the deposition of massive amounts of soluble collagen, altering the homeostasis of extracellular matrix (ECM) biogenesis and resulting in tissue scarring. Because a chromone scaffold (CS)-containing small molecule called eupatilin was shown to curb lung fibrosis, a new CS-containing analog, ONG41008, was generated. Plasma exposure was significantly increased. Orally-administered ONG41008 was more potent than pirfenidone at ameliorating fibrosis in a bleomycin-induced lung fibrosis model (BLM). ONG41008 also completely inhibited the trans-differentiation to myofibroblasts of ONGHEPA1, being a primary hepatic stellate cells (HSC) cell line, and of primary diseased human lung fibroblasts (DHLFs) derived from patients with idiopathic pulmonary fibrosis. ONG41008 inhibited the expression of LTBP1 and LAP, dismantling the latent TGF complex, likely limiting binding of TGF to TGF receptors I and II. ONG41008 also markedly inhibited the phosphorylation of SMAD2 and SMAD3, the induction of NADPH oxidase 4 (NOX4) in both cell types, and the production of reactive oxygen species.ONG41008 also completely inhibited the induction of chemokine ligands 2 (Ccl2) and 7 (Ccl7) and induced robust autophagy, suggesting that ONG41008 could curb liver inflammation and fibrosis. STAM mice model was orally administered with 50 mg/kg (mpk) ONG41008 exhibited high nonalcoholic fatty liver disease scores, suggesting that ONG41008, together with anti-diabetic drugs like GLP1 and peroxisome proliferator-activated receptor agonists, could reduce the development of nonalcoholic steatohepatitis (NASH).Treatment of macrophages with ONG41008 and lipopolysaccharide (LPS) markedly inhibited the expression of TNF, Interleukin 1, CHOP, CCL2, CCL7, and CXCL2.

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Flavonoids as a scaffold for development of novel anti-angiogenic agents: An experimental and computational enquiry

Cited by 29 publications

References 84 publications

Evaluation of the status quo of polyphenols analysis: Part I—phytochemistry, bioactivity, interactions, and industrial uses

Evaluation of the status quo of polyphenols analysis: Part I—phytochemistry, bioactivity, interactions, and industrial uses

Dietary flavonoids inhibit the glycation of lens proteins: implications in the management of diabetic cataract

A noble TGF beta biogenesis inhibitor exhibits both potent anti-fibrotic and anti-inflammatory capabilities

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