참두릅 잎의 Protein Tyrosine Phosphatase 1B와 a-Glucosidase 저해 활성 (Inhibitory Activity of Aralia elata Leaves on Protein Tyrosine Phosphatase 1B and a-Glucosidase)

서지정보

· 발행기관 : 한국생약학회
· 수록지 정보 : 생약학회지 / 47권 / 1호 / 29 ~ 37페이지
· 저자명 : 조윤숙, 최재수, 성수희, 바크타 히만수 쿠마르, 정희진, 문경호

초록

Anti-diabetic potential of the leaves of A. elata through the inhibitory activity on PTP1B and a-glucosidase has not been reported. In this study, the EtOAc fraction of methanolic extract from the leaves of A. elata showed potent inhibitory activity against the PTP1B and a-glucosidase with IC50 value of 96.29±0.3 and 264.71±14.87 mg/mL, respectively. Three known triterpenoids, oleanolic acid, oleanolic acid-28-O-b-D-glucopyranoside and oleanolic acid-3-O-b-D-glucopyranoside were isolated from the most active EtOAc fraction. We determined the chemical structure of these triterpenoids through comparisons of published nuclear magnetic resonance (NMR) spectroscopic data. Furthermore, we screened these triterpenoids for their ability to inhibit PTP1B and a-glucosidase over a range of concentrations (12.5-50 mM). All three terpenoids significantly inhibited PTP1B in a concentration dependent manner and oleanolic acid effectively inhibited a-glucosidase. In addition, these compounds revealed potent inhibitory activity with negative binding energies toward PTP1B, showing high affinity and tight binding capacity in the molecular docking studies. Therefore, the results of the present study clearly demonstrate that A. elata leaves and its triterpenoid constituents might be beneficial in the prevention or treatment of diabetic disease.

영어초록

Anti-diabetic potential of the leaves of A. elata through the inhibitory activity on PTP1B and a-glucosidase has not been reported. In this study, the EtOAc fraction of methanolic extract from the leaves of A. elata showed potent inhibitory activity against the PTP1B and a-glucosidase with IC50 value of 96.29±0.3 and 264.71±14.87 mg/mL, respectively. Three known triterpenoids, oleanolic acid, oleanolic acid-28-O-b-D-glucopyranoside and oleanolic acid-3-O-b-D-glucopyranoside were isolated from the most active EtOAc fraction. We determined the chemical structure of these triterpenoids through comparisons of published nuclear magnetic resonance (NMR) spectroscopic data. Furthermore, we screened these triterpenoids for their ability to inhibit PTP1B and a-glucosidase over a range of concentrations (12.5-50 mM). All three terpenoids significantly inhibited PTP1B in a concentration dependent manner and oleanolic acid effectively inhibited a-glucosidase. In addition, these compounds revealed potent inhibitory activity with negative binding energies toward PTP1B, showing high affinity and tight binding capacity in the molecular docking studies. Therefore, the results of the present study clearly demonstrate that A. elata leaves and its triterpenoid constituents might be beneficial in the prevention or treatment of diabetic disease.

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