Natural Breviscapin, Mangiferin, and a Modified Mangostin Present Inhibitory Effect on Dipeptidyl Peptidase‐IV

Abstract

Type 2 diabetes was usually caused by inadequate secretion of insulin or insulin resistance in tissues and organs. About 90% diabetes belongs to type 2 diabetes, which is seriously harmful to human health. Dipeptidyl Peptidase‐IV (DPP‐IV) target have attracted much attention because of its ability to prevent type 2 diabetes (T2D). Clinical application of chemical synthetic medicines has different degrees of side effects. Therefore, the present evaluation aims to seek DPP‐IV inhibitors as the source of natural products. DPP‐IV inhibitory activities of eight natural products and a structural modification of mangostin (eight chromone of 1–8 and iridoid glycoside for 9) were evaluated by this manuscript at the enzyme level. As a result, three chromones of 2 (a modified mangostin), 3 (mangiferin) and 5 (breviscapin) showed moderate DPP‐IV inhibitory activities with IC50 values of 69.27 μM, 44.19 μM, and 49.53 μM via the use of the fluorescence‐based method (0.25 mM, 0.34 mM and 0.85 mM for the chromogenic substrate method). This study suggests that natural products, which mainly consist by chromone that generated from Mango and Scutellaria baicalensis may have beneficial effects on treating T2D.

Natural products from plants targeting key enzymes for the future development of antidiabetic agents

“…The most relevant aspects of this study are briey discussed in the next paragraph. Cyanidin 3-O-b-D-glucopyranoside (1), isoliquiritigenin (16), narcissoside (55), myricetin (65), and hyperoside (70) inhibited the enzyme higher than 50% at 200 mM. The IC 50 values of these avonoids were 81.05, 149.96, 166.52, 156.29, and 138.79 mM, respectively.…”

“…Kinetic analyses of cyanidin 3-O-b-D-glucopyranoside (1), isoliquiritigenin (16), narcissoside (55), and hyperoside (70) revealed that they were mixed-type inhibitors; furthermore, their competitive inhibition constants were lower than the uncompetitive ones. Thus, like most avonoids, these compounds preferred interacting with the enzyme's active site.…”

“…Representative DPP-IV inhibitory flavonoids ( 1–72 ) and other aromatic compounds ( 73–100 ) are summarized in Table 1. 42–71 …”

Novel Mannich Bases of α‐Mangostin Bearing Methoxyphenyl Moieties with Antioxidant and Membrane‐protective activity

“…In this way, a derivative with 2‐bromobenzoyl fragments at C‐3‐OH/C‐6‐OH positions demonstrated cytotoxic effects against four cancer cell lines [5a] . A derivative containing N ‐Boc‐ L– Met fragments at the same positions is a promising candidate for cardiovascular disease treatment, [5b] a derivative with 3‐methylbutane‐2,3‐diol moieties at positions C‐2 and C‐8 showed high inhibitory activity against dipeptidyl peptidase‐IV, which has been related to the development of type 2 diabetes mellitus [5c] …”