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Promising anti-diabetic potential of capillin and capillinol isolated from Artemisia capillaris

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Abstract

Caffeoylquinic acids, flavonoids, and coumarins isolated from Artemisia capillaris have recently emerged as therapeutic candidates for diabetes and diabetic complications; however, there have been very few studies of the anti-diabetic potential of polyacetylenes. In the present study, we investigated the anti-diabetic potential of two polyacetylenes isolated from A. capillaris, namely capillin and capillinol by investigating their ability to inhibit α-glucosidase, protein tyrosine phosphatase 1B (PTP1B), and rat lens aldose reductase (RLAR). Capillin displayed potent inhibitory activity against α-glucosidase, PTP1B, and RLAR, while capillinol showed moderate inhibitory activity against α-glucosidase and PTP1B at the concentrations tested. In addition, a kinetic study revealed that capillin inhibited α-glucosidase and RLAR in a noncompetitive manner, while inhibited PTP1B in a mixed-type manner. Capillinol inhibited α-glucosidase and PTP1B in a mixed-type manner. Docking simulations of these compounds demonstrated negative binding energies and close proximity to residues in the binding pocket of PTP1B, indicating that these polyacetylenes have a high affinity and tight binding capacity for the active site of the enzyme. Furthermore, capillin dose-dependently inhibited peroxynitrite (ONOO−)-mediated tyrosine nitration. The results clearly demonstrate the promising potential of capillin and capillinol as therapeutic interventions for the management of diabetes as well as diabetes-associated complications.

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Acknowledgments

This research was supported by the Basic Science Research Program through the National Research Foundation of Korea (NRF) and by the Ministry of Education (2012R1A6A1028677) and was also partially assisted by the Korean Bioinformation Center (KOBIC) Research Support Program.

Conflict of Interest

The authors declare no conflict of interest.

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    Authors and Affiliations

    1. Department of Pharmacy, Mawlana Bhashani Science and Technology University, Santosh, Tangail, 1902, Bangladesh

      Md. Nurul Islam

    2. Angiogenesis & Chinese Medicine Laboratory, Department of Pharmacology, University of Cambridge, Cambridge, UK

      Ran Joo Choi

    3. Department of Food Science and Human Nutrition, Chonbuk National University, Jeonju, 561-756, Republic of Korea

      Hyun Ah Jung

    4. Korean BioInformation Center (KOBIC), Daejeon, 305-806, Republic of Korea

      Sang Ho Oh

    5. Department of Food and Life Science, Pukyong National University, Busan, 608-737, Republic of Korea

      Jae Sue Choi

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    1. Md. Nurul Islam
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    Correspondence to Hyun Ah Jung or Jae Sue Choi.

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    Md. Nurul Islam and Ran Joo Choi have contributed equally to this work.

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    Islam, M.N., Choi, R.J., Jung, H.A. et al. Promising anti-diabetic potential of capillin and capillinol isolated from Artemisia capillaris . Arch. Pharm. Res. 39, 340–349 (2016). https://doi.org/10.1007/s12272-016-0715-y

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