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Authors Zhuang MJ, Qiu HH, Li P, Hu LH, Wang YY, Rao L
Received 12 October 2017
Accepted for publication 8 February 2018
Published 23 April 2018 Volume 2018:12 Pages 955—966
DOI https://doi.org/10.2147/DDDT.S153898
Checked for plagiarism Yes
Review by Single-blind
Peer reviewers approved by Dr Justinn Cochran
Peer reviewer comments 2
Editor who approved publication: Professor Manfred Ogris
Background and
purpose: The traditional Chinese medicine –
the flower of Edgeworthia gardneri –
is reported as an effective therapeutic for type 2 diabetes mellitus (T2DM).
Nevertheless, most constituents of the flowers of E. gardneri have not yet been
studied. This study was conducted to investigate the effect of quercetin
extracted from the flowers of E. gardneri on
islet protection and amelioration in T2DM and explore its mechanism.
Method: Quercetin was extracted from the flowers of E. gardneri and verified by
high-performance liquid chromatography. Quercetin or crude extract’s effect on
insulin secretion was investigated. ERK1/2 and phospho-ERK1/2 were detected by
Western blot analysis, and fluo-3 AM was used to detect intracellular Ca2+. The anti-apoptosis effect of quercetin or crude extract on MIN-6 cells
was investigated by thiazolyl blue tetrazolium bromide (MTT) assay and flow
cytometry analysis. Activation of caspases and expression of Bcl-2 and BAX were
tested by Western blot analysis. In addition, the mitochondrial membrane
potential was determined by JC-1 probe. Moreover, in vivo activity was also
tested in db/db mice.
Results: A quercetin level of >10 μmol/L could induce insulin secretion.
Intracellular Ca2+ and ERK1/2 were
involved in the signaling pathway of quercetin-induced insulin secretion. We
also observed that quercetin could inhibit palmitic acid-induced cell apoptosis
via suppressing the activation of caspase-3, -9, -12; increasing the ratio of
Bcl-2/BAX and reversing the impaired mitochondrial membrane potential. Crude
extract’s effect on insulin secretion was similar to that of pure extracted
quercetin, while it possessed higher anti-apoptosis activity. Additionally,
intraperitoneal glucose tolerance, plasma insulin level, hepatic triglyceride,
hepatic glycogen and the pathological histology of both pancreatic islet and
liver in db/db mice were significantly improved by the administration of the
extracted quercetin.
Conclusion: Our study indicated that quercetin extracted from the flowers
of E. gardneri exerted excellent
properties in islet protection and amelioration.
Keywords: quercetin, Edgeworthia gardneri ,
insulin secretion, anti-apoptosis, type 2 diabetes mellitus