A comprehensive review on xanthone derivatives as α-glucosidase inhibitors

Abstract

a-Glucosidase plays an important role in carbohydrate metabolism and is therefore an attractive therapeutic target for the treatment of diabetes, obesity and other related complications. In the last two decades, considerable interest has been given to natural and synthetic xanthone derivatives in this field of research. Herein, a comprehensive review of the literature on xanthones as inhibitors of a-glucosidase activity, their mechanism of action, experimental procedures and structure-activity relationships have been reviewed for more than 280 analogs. With this overview we intend to motivate and challenge researchers (e.g. chemistry, biology, pharmaceutical and medicinal areas) for the design of novel xanthones as multipotent drugs and exploit the properties of this class of compounds in the management of diabetic complications.

A Review on Recent Advances in Nitrogen-Containing Molecules and Their Biological Applications

“…In addition, compound 17a also strongly inhibited TGF-β1-induced Smad signaling in SPC-A1 and HepG2 cells. It showed however very low aqueous solubility, which Series of benzo [1,2,5]thiadiazole-imidazole derivatives 17 were prepared and tested for their activin receptor-like kinase 5 (ALK5) inhibitory activity [70]. Among the series of compounds, the derivative 17a substituted with a meta-fluoro group on the phenyl ring exhibited excellent inhibitiory activity (IC 50 = 0.008 µM) against ALK5 kinase ( Figure 20).…”

“…These molecules have received increasing attention over the past two decades. They contributed to the development of numerous organic synthesis protocols and found abundant applications in the chemical sciences [1][2][3][4][5]. Many N-heterocyclic compounds that are broadly distributed in Nature, possess physiological and pharmacological properties and are constituents of many biologically important molecules, including many vitamins, nucleic acids, pharmaceuticals, antibiotics, dyes and agrochemicals, amongst many others [6][7][8][9][10].…”

Study on Synthesis and Biological Evaluation of 3-Aryl Substituted Xanthone Derivatives as Novel and Potent Tyrosinase Inhibitors

“…18) In recent years, xanthone derivatives have been received considerable attention in the field of medicinal chemistry because of their diversely biological functions, 20,21) such as anti-oxidant, 22) anti-hypertensive, 23) anti-convulsant, 24) anti-cholinesterase, 25) anti-malarial, 26) antimicrobial, 27) anti-inflammatory, 28) and anti-cancer activities. 29) Besides, they also served as the effective inhibitors of several enzymes like α-glycosidase, 30,31) topoisomerase, 32) proteinkinase, 33) aromatase. 34) Driven by both the biologically applied powers and the favorable pharmacological properties, indeed, xanthone skeleton has been defined as one of the privileged structural motifs for next stage of certain new drug screening and discovery.…”

Rooibos (Aspalathus linearis) and Honeybush (Cyclopiaspp.): From Bush Teas to Potential Therapy for Cardiovascular Disease

“…The mechanism for the amelioration of diabetic complications in rodents by rooibos and honeybush may also be due α-glucosidase inhibition; or SGLT2 inhibiting potential of rooibos and honeybush or their respective flavonoids [119,[149][150][151]. α-Glucosidase is an enzyme present on the intestinal brush border where it digests starch, increasing blood glucose [152]. Anti-diabetic drugs, therefore commonly utilize strategies such as α-glucosidase inhibition or SGLT2 inhibition to facilitate their actions [152,153].…”

“…α-Glucosidase is an enzyme present on the intestinal brush border where it digests starch, increasing blood glucose [152]. Anti-diabetic drugs, therefore commonly utilize strategies such as α-glucosidase inhibition or SGLT2 inhibition to facilitate their actions [152,153]. The dihydrochalcone phlorizin, an SGLT2 inhibitor, provides a basis to explore natural plant based agents for use in the management of diabetes [154].…”