Antidiabetic xanthones with α-glucosidase inhibitory activities from an endophytic Penicillium canescens

Malik, Abd. (2020) Antidiabetic xanthones with α-glucosidase inhibitory activities from an endophytic Penicillium canescens. Fitoterapia, 142 (04552). pp. 1-8. ISSN 0367326X, 18736971

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Official URL: https://www.journals.elsevier.com/fitoterapia

Abstract

Worldwide, 463 million people are a ected by diabetes of which the majority is diagnosed with Type 2 Diabetes (T2D). T2D can ultimately lead to retinopathy, nephropathy, nerve damage, and amputation of the lower ex- tremities. α-Glucosidase, responsible for converting starch to monosaccharides, is a key therapeutic target for the management of T2D. However, due to substantial side e ects of currently marketed drugs, there is an urgent need for the discovery of new α-glucosidase inhibitors. In our ongoing e orts to identify novel α-glucosidase inhibitors from Nature, we are investigating the potential of endophytic lamentous fungi as sustainable sources of hits and/or leads for future antihyperglycemic drugs. Here we report one previously unreported xanthone (5) and two known xanthones (7 and 11) as α-glucosidase inhibitors, isolated from an endophytic Penicillium ca- nescens, recovered from fruits of Juniperus polycarpos. The three xanthones 5, 7, and 11 showed inhibitory ac- tivities against α-glucosidase with IC50 values of 38.80 ± 1.01 μM, 32.32 ± 1.01 μM, and 75.20 ± 1.02 μM, respectively. Further pharmacological characterization revealed a mixed-mode inhibition for 5, a competitive inhibition for 7, while 11 acted as a non-competitive inhibitor

Item Type:	Article
Subjects:	R Medicine > RS Pharmacy and materia medica
Divisions:	FAKULTAS FARMASI
Depositing User:	Unnamed user with email admin@umi.ac.id
Date Deposited:	12 Jul 2021 11:39
Last Modified:	27 Oct 2021 00:58
URI:	http://repository.umi.ac.id/id/eprint/306

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