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Losing weight has significant impact on chronic disease management. Orlistat, a lipase inhibitor, has alternative effect for weight controlling. To find more candidates, we conducted a review of chalcone and xanthine derivatives regarding their anti-lipase activity. Eight databases were searched including PubMed, Scopus, Web of Science (ISI), Virtual Health Library (VHL), System for Information on Grey Literature in Europe (SIGLE), Global Health Library (GHL), EMBASE, and Google Scholar in August 2018. We found chalcone scaffold was more effective on lipase inhibition than xanthine scaffold. Among 19 investigated chalcones, only isoliquiritigenin and licuroside demonstrated an effect on preventing weight gain and increase in the total cholesterol and total triglycerides aside apart from their high activity on inhibiting lipase. Effect and type of inhibition of individual chalcones differed depending on their structure. In addition, very few studies investigated xanthine compounds and their activities were inconsistent. We suggest more studies investigate the ability of chalcones and modifying their structure to find out other compounds with higher efficacy.
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http://dx.doi.org/10.1111/cbdd.13626 | DOI Listing |
Bioorg Chem
August 2025
Department of Pharmaceutics & Bioengineering, School of Chemical Engineering, Sichuan University, Chengdu 610065, China. Electronic address:
2',4'-dimethoxy-4-hydroxychalcone (15b) has been previously reported as a reversible competitive inhibitor of xanthine oxidase (XOD) with potent activity (> 10-fold vs. allopurinol), but its molecular interactions with the enzyme active site remain uncharacterized. In this research, an integrated approach consisting of multiple spectroscopic methods, isothermal titration calorimetry (ITC), and computer simulations was employed to investigate the binding mode of 15b on XOD.
View Article and Find Full Text PDFRSC Adv
June 2025
Department of Chemistry, Government College University Faisalabad Faisalabad 38000 Pakistan
Cancer remains a major global health concern, necessitating the continuous development of novel anticancer agents with enhanced efficacy and reduced side effects. Purine derivatives are privileged bioactive scaffolds that play a crucial role in drug discovery due to their presence in essential biomolecules such as DNA, RNA, ATP, and coenzymes. This review highlights the synthesis, structure-activity relationships (SARs), and anticancer evaluations of various purine hybrids, including aryl piperazine, triazole-hybrid piperidine/pyrrolidine, and diazenyl-containing purines, from 2020 to 2024.
View Article and Find Full Text PDFSpectrochim Acta A Mol Biomol Spectrosc
March 2025
Centro de Química Estrutural, Institute of Moleculars Sciences, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais, 1049-001 Lisboa, Portugal.
This article presents the synthesis of chalcone allied 1,2,3-triazole via an aldol-click reaction. The newly synthesized compound chalcogenyl based 1,2,3-triazole (7) selectively detects Co (II) ion over other metal cations by UV-visible photophysical study with the limit of detection value of 1.24 × 10 M.
View Article and Find Full Text PDFChin Med
November 2024
School of Pharmacy, Anhui University of Chinese Medicine, 350 Shaoquan Rd, Hefei, 230012, People's Republic of China.
Background: Chrysanthemi Flos is a traditional Chinese medicine with a long history of medicinal use. Prior research suggests that the intrinsic composition of Chrysanthemi Flos is affected by shade-drying and oven-drying methods. Nevertheless, the effects of these methods on the proteins and metabolites of Chrysanthemi Flos have not been extensively studied.
View Article and Find Full Text PDFACS Omega
October 2024
Department of Chemistry and Chemical Engineering, SBASSE, Lahore University of Management Sciences (LUMS), DHA, Lahore-54792, Pakistan.
Originating from the basic chalcone structure, bis-chalcones are characterized by their dual ,-unsaturated carbonyl systems and carry a range of biological activities that include antimicrobial, antiviral, antiparasitic, antioxidant, antiproliferative, and chemical reactivities that warrant a review to cover recent progress. Thus, this review presents the significant potential demonstrated by bis-chalcones in various biological applications. For example, compounds showed excellent antiparasitic activity against leishmania with good selectivity index, and compounds - showed submicromolar activity against SupT1 cells.
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