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Bioorg Med Chem Lett. 2014 Feb 15;24(4):1192-6. doi: 10.1016/j.bmcl.2013.12.098. Epub 2014 Jan 3.

Rat intestinal sucrase inhibition of constituents from the roots of Rosa rugosa Thunb.

Author information

1
College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea; Institute of Marine Biochemistry (IMBC), Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Nghiado, Caugiay, Hanoi, Viet Nam.
2
Institute of Marine Biochemistry (IMBC), Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Nghiado, Caugiay, Hanoi, Viet Nam.
3
College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea.
4
Department of Food and Nutrition, Hannam University, Daejeon 305-811, Republic of Korea.
5
College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea. Electronic address: yhk@cnu.ac.kr.

Abstract

A new octanordammarane triterpene, 3β,15α-dihydroxymansumbinol (1) and a novel A-ring contracted oleanane triterpenoid, 2-formyl-(A)1-19α-hydroxy-1-norolean-2,12-dien-28-oic acid (2) were isolated from the roots extract of Rosa rugosa along with fifteen known compounds (3-17). Their structures were elucidated by extensive spectroscopic analysis, including 1D and 2D NMR, and FTICRMS. The MeOH extract, as well as CH2Cl2 and EtOAc fractions at a concentration of 0.5mg/mL showed potent sucrase inhibitory activity, with inhibition percentage values of 84.67±5.37%, 87.50±2.78%, and 81.91±2.90%, respectively. In addition, compounds 7-13 (1.0 mM) showed potent sucrase inhibitory activity (61.88±3.19% to 84.70±3.07% inhibition), which was comparable to that of the positive control, acarbose, with an inhibition percentage value of 50.96±2.97%. Compounds 1, 2, 4, and 14-17 showed moderate and/or weak inhibitory activities at the same concentration. The α-glucosidase inhibitory activities of the extracts and purified compounds may provide a novel opportunity to develop a new class of antidiabetic agents.

KEYWORDS:

A-ring contracted oleanane triterpenoid; Rosa rugosa; Rosaceae; Rosanol A; Rusaic acid B; α-Glucosidase inhibition

PMID:
24461297
DOI:
10.1016/j.bmcl.2013.12.098
[Indexed for MEDLINE]

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