Lipoxygenase inhibitors flavonoids from Cyperus rotundus aerial parts

Ibrahim, Sabrin R. M.; Mohamed, Gamal A.; Alshali, Khalid Z.; Haidari, Rwaida A. Al; El-Kholy, Amal A.; Zayed, Mohamed F.

doi:10.1016/j.bjp.2018.04.002

Cited by 24 publications

(12 citation statements)

References 39 publications

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“…The medicinal target, 5-lipoxygenase, catalyzes the biosynthesis of inflammatory mediators (leukotrienes), in chronic inflammatory diseases [ 111 ]. In an invitro study, 5-lipoxygenase enzyme was shown to be moderately inhibited by vitexin with IC 50 = 5.1 μ M, referenced to indomethacin (IC 50 = 0.98 M) [ 112 ]. Vitexin exerted a powerful reduction of adenosine deaminase and myeloperox expression as they relate to the release of cytokines (TNF- α and IL-17) in mice [ 113 ].…”

Section: Resultsmentioning

confidence: 99%

Multitargeted Effects of Vitexin and Isovitexin on Diabetes Mellitus and Its Complications

Abdulai

Kwofie

Gbewonyo

et al. 2021

The Scientific World Journal

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Background. Till date, there is no known antidote to cure diabetes mellitus despite the discovery and development of diverse pharmacotherapeutic agents many years ago. Technological advancement in natural product chemistry has led to the isolation of analogs of vitexin and isovitexin found in diverse bioresources. These compounds have been extensively studied to explore their pharmacological relevance in diabetes mellitus. Aim of the Study. The present review was to compile results from in vitro and in vivo studies performed with vitexin and isovitexin derivatives relating to diabetes mellitus and its complications. A systematic online literature query was executed to collect all relevant articles published up to March 2020. Results. In this piece, we have collected data and presented it in a one-stop document to support the multitargeted mechanistic actions of vitexin and isovitexin in controlling diabetes mellitus and its complications. Conclusion. Data collected hint that vitexin and isovitexin work by targeting diverse pathophysiological and metabolic pathways and molecular drug points involved in the clinical manifestations of diabetes mellitus. This is expected to provide a deeper understanding of its actions and also serve as a catapult for clinical trials and application research.

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Section: Resultsmentioning

confidence: 99%

Multitargeted Effects of Vitexin and Isovitexin on Diabetes Mellitus and Its Complications

Abdulai

Kwofie

Gbewonyo

et al. 2021

The Scientific World Journal

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“…It is also worth mentioning the possible interference of the identified apigenin derivatives on the stem bark extract that were not detected in the leaves. While there are no available studies on the inhibitory capacity of vicenin-2 ( 8 ), both vitexin ( 16 ) and isovitexin ( 18 ) have already been reported as soybean 5-LOX [37] and 15-LOX inhibitors [38], with IC 50 values of 5.1 and 107.1 µM, respectively. Hence, it is conceivable to assume the observed inhibitory effects towards 5-LOX to be related, at least partially, with the identified phenolic compounds.…”

Section: Discussionmentioning

confidence: 99%

Phenolic Profiling and Biological Potential of Ficus curtipes Corner Leaves and Stem Bark: 5-Lipoxygenase Inhibition and Interference with NO Levels in LPS-Stimulated RAW 264.7 Macrophages

et al. 2019

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The economic value of fig trees has been globally acknowledged due to their utilization in the food industry, being also frequently used in traditional medicine. While ubiquitously distributed in Southeast Asia, Ficus curtipes Corner remains uninvestigated concerning its biological properties and chemical profile. HPLC-DAD-ESI/MSn characterization of methanol extracts obtained from the stem bark and leaves allowed the identification and quantitation of 21 phenolic compounds for the first time; the stem bark was predominantly rich in flavan-3-ols and apigenin derivatives, while solely apigenin-di-glycosides have been identified and quantitated on the leaf extract. Both extracts inhibited 5-lipoxygenase (5-LOX) activity in a concentration-dependent manner, the one obtained from the stem bark being significantly more active (IC50 = 10.75 μg/mL). The effect of both extracts on lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages was evaluated, and while the stem bark extract did not lead to a noticeable interference on nitric oxide (NO) levels, the extract obtained from the leaves notably decreased NO and L-citrulline levels at concentrations ranging from 250 to 500 μg/mL. Herein, F. curtipes is valorized due to its modulatory effects on inflammatory mediators and also as a source of bioactive phenols, which may fuel further studies on the development of nutraceuticals.

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“…During the last few years, flavonoids, including flavones, have attracted much interest because of their diverse bioactivities [ 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 ]. Recent studies have indicated the abilities of flavones in inhibiting many enzymes [ 25 , 26 , 27 , 28 , 29 ], especially AChE [ 30 ] and BACE-1 [ 31 , 32 ]. Studies on the bioactivity of flavone derivatives against AChE and BACE-1 are thus promising for the discovery of novel therapeutic agents for AD.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, In Silico and In Vitro Evaluation of Some Flavone Derivatives for Acetylcholinesterase and BACE-1 Inhibitory Activity

Tran

et al. 2020

Molecules

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Acetylcholinesterase (AChE) and β-secretase (BACE-1) have become attractive therapeutic targets for Alzheimer’s disease (AD). Flavones are flavonoid derivatives with various bioactive effects, including AChE and BACE-1 inhibition. In the present work, a series of 14 flavone derivatives was synthesized in relatively high yields (35–85%). Six of the synthetic flavones (B4, B5, B6, B8, D6 and D7) had completely new structures. The AChE and BACE-1 inhibitory activities were tested, giving pIC50 3.47–4.59 (AChE) and 4.15–5.80 (BACE-1). Three compounds (B3, D5 and D6) exhibited the highest biological effects on both AChE and BACE-1. A molecular docking investigation was conducted to explain the experimental results. These molecules could be employed for further studies to discover new structures with dual action on both AChE and BACE-1 that could serve as novel therapies for AD.

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Lipoxygenase inhibitors flavonoids from Cyperus rotundus aerial parts

Cited by 24 publications

References 39 publications

Multitargeted Effects of Vitexin and Isovitexin on Diabetes Mellitus and Its Complications

Multitargeted Effects of Vitexin and Isovitexin on Diabetes Mellitus and Its Complications

Phenolic Profiling and Biological Potential of Ficus curtipes Corner Leaves and Stem Bark: 5-Lipoxygenase Inhibition and Interference with NO Levels in LPS-Stimulated RAW 264.7 Macrophages

Synthesis, In Silico and In Vitro Evaluation of Some Flavone Derivatives for Acetylcholinesterase and BACE-1 Inhibitory Activity

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