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Evidence-Based Complementary and Alternative Medicine
Volume 2013 (2013), Article ID 685642, 13 pages
Research Article

Antidiabetic Effect and Mode of Action of Cytopiloyne

1Department of Veterinary Medicine, National Chung Hsing University, 402 Taichung, Taiwan
2Agricultural Biotechnology Research Center, Academia Sinica, 128 Academia Road, Section 2, Nankang, 115 Taipei, Taiwan
3Research Center, China Medical University and Hospital, Graduate Institute of Clinical Medical Sciences, China Medical University, 40402 Taichung, Taiwan
4Institute of Zoology, National Taiwan University, 10617 Taipei, Taiwan
5Department of Life Sciences, National Chung Hsing University, 402 Taichung, Taiwan

Received 3 November 2012; Accepted 29 January 2013

Academic Editor: Srinivas Nammi

Copyright © 2013 Cicero Lee-Tian Chang et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


Cytopiloyne was identified as a novel polyacetylenic compound. However, its antidiabetic properties are poorly understood. The aim of the present study was to investigate the anti-diabetic effect and mode of action of cytopiloyne on type 2 diabetes (T2D). We first evaluated the therapeutic effect of cytopiloyne on T2D in db/db mice. We found that one dose of cytopiloyne reduced postprandial glucose levels while increasing blood insulin levels. Accordingly, long-term treatment with cytopiloyne reduced postprandial blood glucose levels, increased blood insulin, improved glucose tolerance, suppressed the level of glycosylated hemoglobin ( ), and protected pancreatic islets in db/db mice. Next, we studied the anti-diabetic mechanism of action of cytopiloyne. We showed that cytopiloyne failed to decrease blood glucose in streptozocin- (STZ-)treated mice whose β cells were already destroyed. Additionally, cytopiloyne dose dependently increased insulin secretion and expression in β cells. The increase of insulin secretion/expression of cytopiloyne was regulated by protein kinase Cα (PKCα) and its activators, calcium, and diacylglycerol (DAG). Overall, our data suggest that cytopiloyne treats T2D via regulation of insulin production involving the calcium/DAG/PKCα cascade in β cells. These data thus identify the molecular mechanism of action of cytopiloyne and prove its therapeutic potential in T2D.