Three Novel Biphenanthrene Derivatives and a New Phenylpropanoid Ester from  Aerides multiflora  and Their  α -Glucosidase Inhibitory Activity

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Abstract

A phytochemical investigation on the whole plants of Aerides multiflora revealed the presence of three new biphenanthrene derivatives named aerimultins A–C ( 1– 3) and a new natural phenylpropanoid ester dihydrosinapyl dihydroferulate ( 4), together with six known compounds ( 5– 10). The structures of the new compounds were elucidated by analysis of their spectroscopic data. All of the isolates were evaluated for their α-glucosidase inhibitory activity. Aerimultin C ( 3) showed the most potent activity. The other compounds, except for compound 4, also exhibited stronger activity than the positive control acarbose. Compound 3 showed non-competitive inhibition of the enzyme as determined from a Lineweaver–Burk plot. This study is the first phytochemical and biological investigation of A. multiflora.

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Clinical Review of Antidiabetic Drugs: Implications for Type 2 Diabetes Mellitus Management

Arun Chaudhury, Chitharanjan Duvoor, Vijaya Sena Reddy Dendi … (2017)

Type 2 diabetes mellitus (T2DM) is a global pandemic, as evident from the global cartographic picture of diabetes by the International Diabetes Federation (http://www.diabetesatlas.org/). Diabetes mellitus is a chronic, progressive, incompletely understood metabolic condition chiefly characterized by hyperglycemia. Impaired insulin secretion, resistance to tissue actions of insulin, or a combination of both are thought to be the commonest reasons contributing to the pathophysiology of T2DM, a spectrum of disease originally arising from tissue insulin resistance and gradually progressing to a state characterized by complete loss of secretory activity of the beta cells of the pancreas. T2DM is a major contributor to the very large rise in the rate of non-communicable diseases affecting developed as well as developing nations. In this mini review, we endeavor to outline the current management principles, including the spectrum of medications that are currently used for pharmacologic management, for lowering the elevated blood glucose in T2DM.

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Cinnamaldehyde--a potential antidiabetic agent.

S. Prabuseenivasan, Pani P Subash, S. Ignacimuthu (2006)

Cinnamonum zeylanicum (cinnamon) is widely used in traditional system of medicine to treat diabetes in India. The present study was carried out to isolate and identify the putative antidiabetic compounds based on bioassay-guided fractionation; the compound identified decreased the plasma glucose levels. The active compound was purified by repeat column and structure of cinnamaldehyde was determined on the basis of chemical and physiochemical evidence. The LD(50) value of cinnamaldehyde was determined as 1850+/-37 mg/kg bw. Cinnamaldehyde was administered at different doses (5, 10 and 20 mg/kg bw) for 45 days to streptozotocin (STZ) (60 mg/kg bw)-induced male diabetic wistar rats. It was found that plasma glucose concentration was significantly (p<0.05) decreased in a dose-dependent manner (63.29%) compared to the control. In addition, oral administration of cinnamaldehyde (20 mg/kg bw) significantly decreased glycosylated hemoglobin (HbA(1C)), serum total cholesterol, triglyceride levels and at the same time markedly increased plasma insulin, hepatic glycogen and high-density lipoprotein-cholesterol levels. Also cinnamaldehyde restored the altered plasma enzyme (aspartate aminotransferase, alanine aminotransferase, lactate dehydrogenase, alkaline phosphatase and acid phosphatase) levels to near normal. Administration of glibenclamide, a reference drug (0.6 mg/kg bw) also produced a significant (p<0.05) reduction in blood glucose concentration in STZ-induced diabetic rats. The results of this experimental study indicate that cinnamaldehyde possesses hypoglycemic and hypolipidemic effects in STZ-induced diabetic rats.

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α-Glucosidase inhibition by flavonoids: an in vitro and in silico structure–activity relationship study

Carina Proença, Marisa Freitas, Daniela Ribeiro … (2017)

Abstract α-Glucosidase inhibitors are described as the most effective in reducing post-prandial hyperglycaemia (PPHG) from all available anti-diabetic drugs used in the management of type 2 diabetes mellitus. As flavonoids are promising modulators of this enzyme’s activity, a panel of 44 flavonoids, organised in five groups, was screened for their inhibitory activity of α-glucosidase, based on in vitro structure–activity relationship studies. Inhibitory kinetic analysis and molecular docking calculations were also applied for selected compounds. A flavonoid with two catechol groups in A- and B-rings, together with a 3-OH group at C-ring, was the most active, presenting an IC50 much lower than the one found for the most widely prescribed α-glucosidase inhibitor, acarbose. The present work suggests that several of the studied flavonoids have the potential to be used as alternatives for the regulation of PPHG.

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Stefania Lamponi: Role: Academic Editor

Journal

Journal ID (nlm-ta): Plants (Basel)

Journal ID (iso-abbrev): Plants (Basel)

Journal ID (publisher-id): plants

Title: Plants

Publisher: MDPI

ISSN (Electronic): 2223-7747

Publication date (Electronic): 17 February 2021

Publication date Collection: February 2021

Volume: 10

Issue: 2

Electronic Location Identifier: 385

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[1 ]Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand; maythazinthant@ 123456mohs.edu.mm (M.T.T.); Kittisak.L@ 123456chula.ac.th (K.L.)

[2 ]Department of Pharmacognosy, University of Pharmacy, Yangon 11031, Myanmar

[3 ]Natural Products for Ageing and Chronic Diseases Research Unit, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand

[4 ]Department of Pharmacognosy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand; nutputsorn.cha@ 123456mahidol.ac.th

[5 ]Scientific and Technological Research Equipment Centre, Chulalongkorn University, Bangkok 10330, Thailand; wanwimon.m@ 123456chula.ac.th

[6 ]Department of Agriculture, Kasetsart University, Bangkok 10900, Thailand; cyyp01@ 123456hotmail.co.th

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[* ]Correspondence: boonchoo.sr@ 123456chula.ac.th ; Tel.: +66-2218-8356

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Boonchoo Sritularak https://orcid.org/0000-0001-8352-4122

Kittisak Likhitwitayawuid https://orcid.org/0000-0002-0861-7617

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Publisher ID: plants-10-00385

DOI: 10.3390/plants10020385

PMC ID: 7922108

PubMed ID: 33671404

SO-VID: 98d8360a-5498-4d6c-94bc-a673ed9e5a7f

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Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

Three Novel Biphenanthrene Derivatives and a New Phenylpropanoid Ester from Aerides multiflora and Their α-Glucosidase Inhibitory Activity

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Clinical Review of Antidiabetic Drugs: Implications for Type 2 Diabetes Mellitus Management

Cinnamaldehyde--a potential antidiabetic agent.

α-Glucosidase inhibition by flavonoids: an in vitro and in silico structure–activity relationship study

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