Next Article in Journal
Multi-Dimensional Spectrum-Effect Relationship of the Impact of Chinese Herbal Formula Lichong Shengsui Yin on Ovarian Cancer
Previous Article in Journal
A Simple Defined Medium for the Production of True Diketopiperazines in Xylella fastidiosa and Their Identification by Ultra-Fast Liquid Chromatography-Electrospray Ionization Ion Trap Mass Spectrometry
Article Menu
Issue 6 (June) cover image

Export Article

Open AccessArticle
Molecules 2017, 22(6), 986; doi:10.3390/molecules22060986

Potential of Icariin Metabolites from Epimedium koreanum Nakai as Antidiabetic Therapeutic Agents

Department of Food and Life Science, Pukyong National University, Busan 48513, Korea
Department of Food Science and Human Nutrition, Chonbuk National University, Jeonju 54896 Korea
College of Pharmacy, Seoul National University, Seoul 08826, Korea
Authors to whom correspondence should be addressed.
Received: 2 May 2017 / Revised: 12 June 2017 / Accepted: 12 June 2017 / Published: 13 June 2017
View Full-Text   |   Download PDF [1376 KB, uploaded 15 June 2017]   |  


The therapeutic properties of Epimedium koreanum are presumed to be due to the flavonoid component icariin, which has been reported to have broad pharmacological potential and has demonstrated anti-diabetic, anti-Alzheimer’s disease, anti-tumor, and hepatoprotective activities. Considering these therapeutic properties of icariin, its deglycosylated icaritin and glycosylated flavonoids (icaeriside II, epimedin A, epimedin B, and epimedin C) were evaluated for their ability to inhibit protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase. The results show that icaritin and icariside II exhibit potent inhibitory activities, with 50% inhibition concentration (IC50) values of 11.59 ± 1.39 μM and 9.94 ± 0.15 μM against PTP1B and 74.42 ± 0.01 and 106.59 ± 0.44 μM against α-glucosidase, respectively. With the exceptions of icaritin and icariside II, glycosylated flavonoids did not exhibit any inhibitory effects in the two assays. Enzyme kinetics analyses revealed that icaritin and icariside II demonstrated noncompetitive-type inhibition against PTP1B, with inhibition constant (Ki) values of 11.41 and 11.66 μM, respectively. Moreover, molecular docking analysis confirmed that icaritin and icariside II both occupy the same site as allosteric ligand. Thus, the molecular docking simulation results were in close agreement with the experimental data with respect to inhibition activity. In conclusion, deglycosylated metabolites of icariin from E. koreanum might offer therapeutic potential for the treatment of type 2 diabetes mellitus. View Full-Text
Keywords: Epimedium koreanum Nakai; icariin metabolite; PTP1B; α-glucosidase; molecular docking simulation. Epimedium koreanum Nakai; icariin metabolite; PTP1B; α-glucosidase; molecular docking simulation.

Figure 1

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. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Kim, D.H.; Jung, H.A.; Sohn, H.S.; Kim, J.W.; Choi, J.S. Potential of Icariin Metabolites from Epimedium koreanum Nakai as Antidiabetic Therapeutic Agents. Molecules 2017, 22, 986.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top