Triterpenoid saponins from the roots of Rosa rugosa Thunb. as rat intestinal sucrase inhibitors
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Medicinal plants constitute an important source of potential therapeutic agents for diabetes. The purpose of present study is to investigate the effect of root extract of Rosa rugosa Thunb. on inhibition of sucrase related to diabetes mellitus (DM). Bioassay-guided fractionation of the methanol extract led to the identification of 13 triterpenoid saponins (1–13). Their structures were elucidated on the basis of extensive spectroscopic analysis, including 1D, 2D NMR, and MS. The n-butanol fraction showed potent rat intestinal sucrase inhibitory activity with value of 87.62 ± 5.84 % inhibition compared to the positive control acarbose (50.96 ± 2.97 % inhibition at 0.02 mM). Subsequently, compounds 11–13 (1.0 mM) exhibited significant sucrase inhibitory activity, with inhibition percentage values of 41.17 ± 3.52, 46.80 ± 4.00, and 39.39 ± 4.19 %, respectively. Whereas, compounds 2–6, 8, and 10 showed moderate sucrase inhibitory activity (ranging from 13.26 ± 7.00 to 32.08 ± 6.04 % inhibition) at a same concentration. The data provide a starting point for creating new sucrase inhibitors, which may be useful for the development of effective therapies for the treatment of DM.
KeywordsRosa rugosa Rosaceae Triterpenoid saponins Sucrase inhibition α-Glucosidase inhibition Anti-diabetic activity
This work was supported by a grant from the Priority Research Center Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science, and Technology (2009-0093815), Republic of Korea.
- An, H.J., I.T. Kim, H.J. Park, H.M. Kim, J.H. Choi, and K.T. Lee. 2011. Tormentic acid, a triterpenoid saponin, isolated from Rosa rugosa, inhibited LPS-induced iNOS, COX-2, and TNF-α expression through inactivation of the nuclear factor-κB pathway in RAW 264.7 macrophages. International Immunopharmacology 11: 504–510.PubMedCrossRefGoogle Scholar
- Kavishankar, G.B., N. Lakshmidevi, S.M. Murthy, H.S. Prakash, and S.R. Niranjana. 2011. Diabetes and medicinal plants: A review. International Journal of Pharmacy and Biomedical Sciences 2: 65–80.Google Scholar
- Lee, Y.H., M.G. Jung, H.B. Kang, K.C. Choi, S. Haam, W. June, Y.J. Kim, H.Y. Cho, and H.G. Yoon. 2008. Effect of anti-histone acetyltransferase activity from Rosa rugosa Thunb. (Rosaceae) extracts on androgen receptor-mediated transcriptional regulation. Journal of Ethnopharmacology 118: 412–417.PubMedCrossRefGoogle Scholar
- Li, D.Q., J. Zhao, J. Xie, and S.P. Li. 2014. A novel sample preparation and on-line HPLC–DAD–MS/MS–BCD analysis for rapid screening and characterization of specific enzyme inhibitors in herbal extracts: Case study of α-glucosidase. Journal of Pharmaceutical and Biomedical Analysis 88: 130–135.PubMedCrossRefGoogle Scholar
- Li, W., Y. Ding, Y.N. Sun, X.T. Yan, S.Y. Yang, C.W. Choi, J.Y. Cha, Y.M. Lee, and Y.H. Kim. 2013b. Triterpenoid saponins of Pulsatilla koreana root have inhibition effects of tumor necrosis factor-α secretion in lipopolysaccharide-induced RAW264.7 cells. Chemical and Pharmaceutical Bulletin 61: 471–476.PubMedCrossRefGoogle Scholar
- Sano, K., S. Sanada, T. Ida, and J. Shoji. 1991. Studies on the constituents of the bark of Kalopanax pictus Nakai. Chemical and Pharmaceutical Bulletin 39: 856–870.Google Scholar
- Yu, D.J., L.T. Lu, K.J. Guan, and C.L. Li. 1985. Flora reipublicae popularis sinicae, Vol. 37, 385–388. Weberling: Science Press.Google Scholar