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The Potent Inhibitors of Protein Tyrosine Phosphatase 1B from the Fruits of Melaleuca leucadendron

1★, 2, 3★ Corresponding author

  1. 1Laboratory of Pharmacognosy, Faculty of Pharmacy, UniversitasMuhammadiyah Surakarta, Pabelan, KTS Solo, Central Java 57102
  2. 2Laboratory of Phytochemistry, Faculty of Pharmacy, Hasanudin University, Tamalanrea No. 9, Makassar, South Sulawesi 90245, Indonesia
  3. 3Laboratory of Natural Products Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University, Ho 3, Kanagawa Machi, Kanazawa 920 1181, Japan

CORRESPONDENCE

Azis Saifudin

Laboratory of Pharmacognosy, Faculty of Pharmacy, UniversitasMuhammadiyah Surakarta, Pabelan, KTS Solo, Central Java 57102

azis.saifudin@ums.ac.id

Volume 8, Issue 5s · pp. S38-S41 · 2016 · DOI: 10.4103/0974-8490.178644

ABSTRACT

Melaleuca leucadendron (Myrtaceae) is a kind of fruit used as Indonesian medicinal component and recorded in Jamu (tonic made of medical herbs) prescription records for the diabetes treatment. Its methanol extract exhibited a strong inhibitory activity with the half maximal inhibitory concentration (IC50) value of 2.05 mg/mL, while it is the same value with positive control RK-682. To isolate the chemical constituents of M. leucadendron and to evaluate their activity against protein tyrosine phosphatase 1B (PTP1B). Further, determine their toxicity potential against T-cell protein tyrosine phosphatase (TCPTP). Methanol extract was fractionated using silica column chromatography, and the obtained fraction was purified using Sephadex 20-LH. The structure of isolated compounds was identified based on 1H and 13Nuclear Magnetic Resonance Spectrometry. Furthermore, the compounds were examined against PTP1B and TCPTP. Methanol extract of M. leucadendron (Myrtaceae) afforded two triterpenes: Betulinic acid and ursolic acid in high quantities. Both compounds exhibited a strong inhibitory activity against PTP1B inhibition with IC50 value of 1.5 and 2.3 mg/mL, respectively (positive control RK-682, IC50 = 2.05 mg/mL). Their activity toward TCPTP, on the other hand, were at 2.4 and 3.1 mg/ mL, respectively. Based on this purification work, betulinic acid and ursolic acid presented 7.6% and 2.4%, respectively, as markedly M. leucadendron most potential for betulinic acid source among Indonesian plants. The result should have demonstrated that the antidiabetes of M. dendron could be through the inhibition of PTP1B.

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    Saifudin, A., Lallo, S. A., & Tezuka, Y. (2016). The Potent Inhibitors of Protein Tyrosine Phosphatase 1B from the Fruits of Melaleuca leucadendron. Pharmacognosy Research, 8(5s), S38-S41. https://doi.org/10.4103/0974-8490.178644

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    © 2016 Author(s)

    This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms. CC BY-NC-SA 4.0