Evidence map›Paper›PMID 28983714›Full record

ArticlePharmaceutical research2017

A Novel Phenylchromane Derivative Increases the Rate of Glucose Uptake in L6 Myotubes and Augments Insulin Secretion from Pancreatic Beta-Cells by Activating AMPK.

Naomi Rozentul, Yosef Avrahami, Moran Shubely, Laura Levy, Anna Munder, Guy Cohen, Erol Cerasi, Shlomo Sasson, Arie Gruzman

Abstract read
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In one paragraph

Article in Pharmaceutical research, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
0.7field-weighted citation impact, top 26% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

0 citing papers in PubMed, 10 citations in OpenAlex.

No citing paper in PubMed yet.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors at 3 institutions in 1 country.

Naomi RozentulDivision of Medicinal Chemistry, Department of Chemistry, Faculty of Exact Sciences, Bar-Ilan University, 52900, Ramat-Gan, Israel.
Yosef AvrahamiDepartment of Pharmacology, Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, 91120, Jerusalem, Israel.
Moran ShubelyDivision of Medicinal Chemistry, Department of Chemistry, Faculty of Exact Sciences, Bar-Ilan University, 52900, Ramat-Gan, Israel.
Laura LevyDivision of Medicinal Chemistry, Department of Chemistry, Faculty of Exact Sciences, Bar-Ilan University, 52900, Ramat-Gan, Israel.
Anna MunderDivision of Medicinal Chemistry, Department of Chemistry, Faculty of Exact Sciences, Bar-Ilan University, 52900, Ramat-Gan, Israel.
Guy CohenDepartment of Pharmacology, Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, 91120, Jerusalem, Israel.
Erol CerasiThe Endocrinology and Metabolism Service, Department of Medicine, Hadassah-Hebrew University Medical Center, 91120, Jerusalem, Israel.
Shlomo SassonDepartment of Pharmacology, Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, 91120, Jerusalem, Israel. shlomo.sasson@mail.huji.ac.il.
Arie GruzmanDivision of Medicinal Chemistry, Department of Chemistry, Faculty of Exact Sciences, Bar-Ilan University, 52900, Ramat-Gan, Israel. gruzmaa@biu.ac.il.ORCID http://orcid.org/0000-0002-8006-4201
Bar-Ilan University · ILHebrew University of Jerusalem · ILHadassah Medical Center · IL

Funding

Bar-Ilan University new faculty grant 12the Applied Research Program A of the Hebrew University 18the Israel Science Foundation of The Israel Academy of Sciences and Humanities 683/10
6 · The paper itself

Abstract

purposeA series of novel polycyclic aromatic compounds that augment the rate of glucose uptake in L6 myotubes and increase glucose-stimulated insulin secretion from beta-cells were synthesized. Designing these molecules, we have aimed at the two main pathogenic mechanisms of T2D, deficient insulin secretion and diminished glucose clearance. The ultimate purpose of this work was to create a novel antidiabetic drug candidate with bi-functional mode of action.

methodsAll presented compounds were synthesized, and characterized in house. INS-1E cells and L6 myoblasts were used for the experiments. The rate of glucose uptake, mechanism of action, level of insulin secretion and the druggability of the lead compound were studied.

resultsThe lead compound (6-(1,3-dithiepan-2-yl)-2-phenylchromane), dose- and time-dependently at the low μM range increased the rate of glucose uptake in L6 myotubes and insulin secretion in INS-1E cells. The compound exerted its effects through the activation of the LKB1 (Liver Kinase B1)-AMPK pathway. In vitro metabolic parameters of this lead compound exhibited good druggability.

conclusionsWe anticipate that bi-functionality (increased rate of glucose uptake and augmented insulin secretion) will allow the lead compound to be a starting point for the development of a novel class of antidiabetic drugs.

Indexed as

AMP-Activated Protein KinasesAnimalsBiological TransportCell LineCells, CulturedChromansDrug DiscoveryEnzyme ActivationGlucoseHumansHypoglycemic AgentsInsulinInsulin-Secreting CellsMuscle Fibers, SkeletalRatsAMP-Activated Protein KinasesChromansGlucoseHypoglycemic AgentsInsulinAMPK activationglucose uptakeinsulin secretionLKB1 activationphenylchromane scaffold

Identifiers

PMID28983714
OpenAlexW2760970174

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.