Undescribed chalcone and stilbene constituents from <i>Lysimachia baviensis</i> and their anti-inflammatory effect

Hưng, Nguyễn Quang; Anh, Nguyễn Thị Hoàng; Khang, Nguyen Sinh; Hương, Nguyễn Thị Thanh; Luyenb, Nguyen Thi; Hau, Dang Viet; Dat, Nguyen Tien

doi:10.1080/14786419.2021.1994564

Cited by 6 publications

(4 citation statements)

References 19 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The LPS-triggered nuclear translocation of NF-κB and ROS increase were also prevented [79]. Bavienside A treatment resulted in a significantly reduced amount of NO that LPS-induced RAW264.7 cells produced, with an IC 50 value of 6.23 µM [80]. Bone marrow-derived macrophages (BMDMs) were stimulated with LPS (1 µg/mL).…”

Section: Inflammation In the Livermentioning

confidence: 99%

Stilbenes, a Versatile Class of Natural Metabolites for Inflammation—An Overview

et al. 2023

View full text Add to dashboard Cite

Stilbenes are polyphenolic allelochemicals synthesized by plants, especially grapes, peanuts, rhubarb, berries, etc., to defend themselves under stressful conditions. They are now exploited in medicine for their antioxidant, anti-proliferative and anti-inflammatory properties. Inflammation is the immune system’s response to invading bacteria, toxic chemicals or even nutrient-deprived conditions. It is characterized by the release of cytokines which can wreak havoc on healthy tissues, worsening the disease condition. Stilbenes modulate NF-κB, MAPK and JAK/STAT pathways, and reduce the transcription of inflammatory factors which result in maintenance of homeostatic conditions. Resveratrol, the most studied stilbene, lowers the Michaelis constant of SIRT1, and occupies the substrate binding pocket. Gigantol interferes with the complement system. Besides these, oxyresveratrol, pterostilbene, polydatin, viniferins, etc., are front runners as drug candidates due to their diverse effects from different functional groups that affect bioavailability and molecular interactions. However, they each have different thresholds for toxicity to various cells of the human body, and thus a careful review of their properties must be conducted. In animal models of autoinflammatory diseases, the mode of application of stilbenes is important to their absorption and curative effects, as seen with topical and microemulsion gel methods. This review covers the diversity seen among stilbenes in the plant kingdom and their mechanism of action on the different inflammatory pathways. In detail, macrophages’ contribution to inflamed conditions in the liver, the cardiac, connective and neural tissues, in the nephrons, intestine, lungs and in myriad other body cells is explored, along with detailed explanation on how stilbenes alleviate the symptoms specific to body site. A section on the bioavailability of stilbenes is included for understanding the limitations of the natural compounds as directly used drugs due to their rapid metabolism. Current delivery mechanisms include sulphonamides, or using specially designed synthetic drugs. It is hoped that further research may be fueled by this comprehensive work that makes a compelling argument for the exploitation of these compounds in medicine.

show abstract

Section: Inflammation In the Livermentioning

confidence: 99%

Stilbenes, a Versatile Class of Natural Metabolites for Inflammation—An Overview

et al. 2023

View full text Add to dashboard Cite

show abstract

“…Chalcone skeleton comprises of two aryl/heteroaryl entities separated by three carbon atoms, generating an α,β-unsaturated carbonyl compound. Chalcone compounds have been well documented in the literature to exhibit several pharmacological activities such as anti-inflammatory [ [21] , [22] , [23] ], antiviral [ 24 ], anticancer [ [25] , [26] , [27] ], antibacterial [ [28] , [29] , [30] , [31] ], and antioxidant [ 32 , 33 ].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, pharmacological evaluation, and in silico study of new 3-furan-1-thiophene-based chalcones as antibacterial and anticancer agents

Abdula,

Mohsen,

Jasim

et al. 2024

Heliyon

View full text Add to dashboard Cite

“…Chalcones are 1,3-diaryl propenone, which comprises two aryl moieties separated by three carbon atoms, furnishing α,βunsaturated ketone derivatives. Chalcones have been reported to exhibit a wide range of pharmacological activities such as antimicrobial [10][11][12][13], anticancer [14][15][16], anti-inflammatory [17][18][19], antiviral [20], and antioxidant [21,22]. Furthermore, heterocyclic compounds each bearing a pyrazoline scaffold have been reported as antimicrobial [23][24][25], anticancer [26][27][28], anti-inflammatory [29][30][31], antiviral [32], and antioxidant [33].…”

Section: Introductionmentioning

confidence: 99%

“…The most active compounds in vitro were subjected to a molecular docking study targeting GlcN-6-P synthase. matory [17][18][19], antiviral [20], and antioxidant [21,22]. Furthermore, heterocyclic compounds bearing pyrazoline scaffolds have been reported as antimicrobial [23][24][25], anticancer [26][27][28], anti-inflammatory [29][30][31], antiviral [32], and antioxidant [33].…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, Antimicrobial Properties, and Molecular Docking of Novel Furan-Derived Chalcones and Their 3,5-Diaryl-∆2-pyrazoline Derivatives

Mahdi,

Abdula,

Jassim

et al. 2023

Antibiotics

View full text Add to dashboard Cite

The present work focuses on the synthesis and preliminary structure activity relationships (SARs) of furan-derived chalcones and their corresponding ∆2-pyrazoline derivatives as antimicrobial agents. Eight novel chalcone derivatives and eight ∆2-pyrazoline compounds were synthesized in moderate to good isolated yields. The target compounds were evaluated as antimicrobial agents against two Gram-positive (Staphylococcus aureus and Staphylococcus epidermidis), two Gram-negative (Escherichia coli and Klebsiella pneumoniae), and fungi (Candida albicans) species. Based on the SARs, chalcones 2a and 2h showed inhibition activity on all tested microbial species, while ∆2-pyrazoline 3d was found to be selective for some microbial species. The most potent compounds (2a, 2h, and 3d) were docked into glucosamine-6-phosphate synthase (GlcN-6-P), the molecular target enzyme for antimicrobial agents, utilizing the Autodock 4.2 program, in order to study their virtual affinity and binding mode with the target enzyme. The selected potent compounds were found to bind to the active site of the enzyme probably in a similar way to that of the substrate as suggested by the docking study. In summary, the newly developed furan-derived chalcones and their ∆2-pyrazoline derivatives could serve as potent leads toward the development of novel antimicrobial agents.

show abstract

Undescribed chalcone and stilbene constituents from Lysimachia baviensis and their anti-inflammatory effect

Cited by 6 publications

References 19 publications

Stilbenes, a Versatile Class of Natural Metabolites for Inflammation—An Overview

Stilbenes, a Versatile Class of Natural Metabolites for Inflammation—An Overview

Synthesis, pharmacological evaluation, and in silico study of new 3-furan-1-thiophene-based chalcones as antibacterial and anticancer agents

Design, Synthesis, Antimicrobial Properties, and Molecular Docking of Novel Furan-Derived Chalcones and Their 3,5-Diaryl-∆2-pyrazoline Derivatives

Contact Info

Product

Resources

About