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Year : 2016  |  Volume : 8  |  Issue : 5  |  Page : 38-41

The potent inhibitors of protein tyrosine phosphatase 1B from the fruits of Melaleuca leucadendron

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

Correspondence Address:
Azis Saifudin
Faculty of Pharmacy, Universitas Muhammadiyah Surakarta, Pabelan, KTS Solo, Jawa Tengah 57102
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Source of Support: None, Conflict of Interest: None

DOI: 10.4103/0974-8490.178644

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Background: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 μg/mL, while it is the same value with positive control RK-682. Objective: 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). Materials and Methods: 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. Results: 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 IC50value of 1.5 and 2.3 μg/mL, respectively (positive control RK-682, IC50 =2.05 μg/mL). Their activity toward TCPTP, on the other hand, were at 2.4 and 3.1 μg/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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