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Heat Shock Protein 90 (Hsp90) Inhibitory Potentials of Some Chalcone Compounds as Novel Anti-Proliferative Candidates
Published in P. Mereena Luke, K. R. Dhanya, Didier Rouxel, Nandakumar Kalarikkal, Sabu Thomas, Advanced Studies in Experimental and Clinical Medicine, 2021
Debarshi Kar Mahapatra, Sayan Dutta Gupta, Sanjay Kumar Bharti, Tomy Muringayil Joseph, Józef T. Haponiuk, Sabu Thomas
Various natural chalcones like liquiritigenin, xanthohumol, flavokawain B, xanthoangelol, isoliquiritigenin, cardamonin, echinatin, licochalcone, kuwanon, 4-hydroxyderricin, broussochalcone, macdentichalcone, etc., are the eminent candidates with wide pharmacological perspectives in cancer, diabetes, infection, inflammation, and many other activities [39]. The benzylideneacetophenone scaffold is the open chain intermediates in aurones synthesis of flavones and acts as precursors of flavonoids and isoflavonoids. Chalcones and flavonones are isomeric in nature and in the presence of acid or base, they readily undergo interconversion. The edible chalcones have been found to play a pivotal role as Michael acceptor in Michael addition reaction. This small template aids in the structure elucidation of flavanone, flavonoid, chromanochromane, and tannins [40]. Chalcone or chalconoids exist in two forms; cis and trans, where the trans isomeric form is thermodynamically more stable than the cis form. The conjugated double bond system with a delocalized π-electron system facilitates several electron transfer reactions and produces a decrease in redox potential which promotes numerous interactions with the biological targets [41].
Ethnomedicinal and Pharmacological Importance of Glycyrrhiza glabra L
Published in Mahendra Rai, Shandesh Bhattarai, Chistiane M. Feitosa, Wild Plants, 2020
Ashish K. Bhattarai, Sanjaya M. Dixit
Licorice has been used as an antitussive and expectorant herbal medicine for a long time. Cough is produced in different medical conditions, such as common cold, bronchitis, and other respiratory illnesses. Expectorants help to bring up mucus and other materials from the lung, bronchi, and trachea. The activities of 14 major compounds and crude extracts of licorice, using the classical ammonia-induced cough model and phenol red secretion model in mice was evaluated. Liquiritinapioside, liquiritin, and liquiritigenin at 50 mg/kg (i.g.) could significantly decrease cough frequency by 30–78% (p < .01). The compounds Liquiritinapioside, liquiritin, and liquiritigenin showed potent expectorant activities after 3 days of treatment (p < .05). The water and ethanol extracts of licorice, which contain abundant Liquiritinapioside and liquiritin, could decrease cough frequency at 200 mg/kg by 25–59% (p < .05). The result indicates liquiritinapioside and liquiritin are the major antitussive and expectorant compounds of licorice. Their antitussive effects depend on both peripheral and central mechanisms (Kuang et al. 2018). Glycyrrhizin is responsible for demulcent action of licorice. Liquiritinapioside, an active compound present in the methanolic extract of licorice, is found to inhibit capsaicin-induced cough (Kamei et al. 2003).
Medicinal Plants of China Focusing on Tibet and Surrounding Regions
Published in Raymond Cooper, Jeffrey John Deakin, Natural Products of Silk Road Plants, 2020
Jiangqun Jin, Chunlin Long, Edward J. Kennelly
Chemical constituents: Flavanones: liquiritigenin, liquiritin, liquiritinapioside; chalcones: isoliquiritigenin, isoliquiritigenin apioside (Figure 2.7), isoliquiritin, neoisoliquiritin; saponins: glycyrrhizic acid (Figure 2.7), licorice-saponin A3, licorice-saponin G2; isoflavans; isoflavenes; flavones; isoflavones; coumarins; and phenolics (Hosseinzadeh and Nassiri-Asl, 2015).
Research progress of natural products and their derivatives against Alzheimer’s disease
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Jin-Ying Liu, Hong-Yan Guo, Zhe-Shan Quan, Qing-Kun Shen, Hong Cui, Xiaoting Li
Both liquiritigenin and isoliquiritigenin are dihydro- flavonoid monomer compounds extracted from the natural plant liquorice. As these two compounds have similar structures, their pharmacological activities are also similar. In recent years, researchers have found that liquiritigenin and isoliquiritigenin are promising agents for the treatment of AD. Studies have shown that liquiritigenin can be a potent inhibitor of tau amyloid fibril formation by preventing structural transitions in its structure and exposure of hydrophobic groups. Therefore, reducing tau aggregation-mediated neurotoxicity42. Aβ levels can also be reduced by modulating the M1/M2 phenotype transition in microglia, thereby reducing memory decline during AD43. Isoliquiritigenin attenuated Aβ25-35 induced neuronal damage in rat cortical neurons by interfering with [Ca2+]i and ROS production44. Isoliquiritigenin reduces neuronal damage by inhibiting 5-lipoxygenase (5-LO). The activity of 5-LO is regulated by 5-lipoxygenase-activating protein (FLAP), and targeting the 5-LO/FLAP pathway is considered an effective strategy for the treatment of AD. 5-LO is involved in AD pathological changes, and its activity is significantly enhanced. Studies have shown that activation of 5-LO promotes Aβ amyloid deposition and tau hyperphosphorylation45 (Figure 5, Table 2).
The kidney antifibrotic effects of 5,7,3′,4′,5′-pentamethoxyflavone from Bauhinia championii in streptozotocin-induced diabetic rats: in vivo and in vitro experiments
Published in Pharmaceutical Biology, 2023
Jialin Li, Xiaocui Huang, Kailun He, Suzhen Wu
Liquiritigenin, a flavonoid compound, has been found to have the potential to inhibit the accumulation of extracellular matrix (ECM) in high glucose-induced HBZY-1 mesangial cell line by the suppression of the NF-κB and NLRP3 inflammasome pathways (Zhu et al. 2018). The present study discovered that PMF derived from B. championii can prevent STZ-induced ECM accumulation via a different signal pathway known as the TGF-β/Smads signal pathway. Smad2 and Smad3 are important downstream effectors of this pathway, and their phosphorylation is triggered by high glucose and TGF-β. Then the phosphorylated Smad2 and Smad3 are translocated to the nucleus as transcriptional factors to promote the expression of FN and Col IV.
Extensive metabolism of flavonoids relevant to their potential efficacy on Alzheimer’s disease
Published in Drug Metabolism Reviews, 2021
Liquiritin (liquiritigenin-4′-O-β-D-glucoside) is a flavanone glucoside, and was converted to liquiritigenin and the flavone luteolin in mice (Zhang et al. 2020), and to liquiritigenin, and the chalcones isoliquiritin and isoliquiritigenin in rats (Jiang et al. 2021) after oral administration. In addition, it was mono-acetylated, or hydrolyzed to liquiritigenin prior to further hydrogenation, dehydroxylation and methylation by human intestinal bacteria Bacillus sp. 46, Veillonella sp. 31 and 48, Clostridium sp. 51 and Bacteroides sp.57 (Zhang et al. 2014b).