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Bioassay-guided fractionation and identification of α-amylase inhibitors from Syzygium cumini leaves.
Pharm Biol. 2017 Dec; 55(1):206-211.PB

Abstract

CONTEXT

Pancreatic α-amylase and α-glucosidase inhibitors serve as important strategies in the management of blood glucose. Even though Syzygium cumini (L.) Skeels (Myrtaceae) (SC) is used extensively to treat diabetes; scientific evidence on antidiabetic effects of SC leaves is scarce.

OBJECTIVE

SC leaf extract was investigated for α-amylase inhibitory effect and continued with isolation and identification of α-amylase inhibitors.

MATERIALS AND METHODS

Bioassay-guided fractionation was conducted using in vitro α-amylase inhibitory assay (with 20-1000 μg/mL test material) to isolate the inhibitory compounds from ethyl acetate extract of SC leaves. Structures of the isolated inhibitory compounds were elucidated using 1H NMR and 13C NMR spectroscopic analysis and direct TLC and HPLC comparison with authentic samples. Study period was from October 2013 to October 2015.

RESULTS

An active fraction obtained with chromatographic separation of the extract inhibited porcine pancreatic α-amylase with an IC50 of 39.9 μg/mL. Furthermore, it showed a strong inhibition on α-glucosidase with an IC50 of 28.2 μg/mL. The active fraction was determined to be a 3:1 mixture of ursolic acid and oleanolic acid. Pure ursolic acid and oleanolic acid showed IC50 values of 6.7 and 57.4 μg/mL, respectively, against α-amylase and 3.1 and 44.1 μg/mL respectively, against α-glucosidase.

DISCUSSION AND CONCLUSIONS

The present study revealed strong α-amylase and α-glucosidase inhibitory effects of ursolic acid and oleanolic acid isolated from SC leaves for the first time validating the use of SC leaves in antidiabetic therapy.

Authors+Show Affiliations

a Postgraduate Institute of Science, University of Peradeniya , Peradeniya , Sri Lanka.b Department of Biochemistry, Faculty of Medicine , University of Peradeniya , Peradeniya, Sri Lanka.c Institute of Fundamental Studies , Kandy , Sri Lanka.b Department of Biochemistry, Faculty of Medicine , University of Peradeniya , Peradeniya, Sri Lanka.b Department of Biochemistry, Faculty of Medicine , University of Peradeniya , Peradeniya, Sri Lanka.d School of Agriculture , Meiji University , Tama-ku , Kanagawa , Japan.c Institute of Fundamental Studies , Kandy , Sri Lanka. d School of Agriculture , Meiji University , Tama-ku , Kanagawa , Japan.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27927056

Citation

Poongunran, Jeyakumaran, et al. "Bioassay-guided Fractionation and Identification of Α-amylase Inhibitors From Syzygium Cumini Leaves." Pharmaceutical Biology, vol. 55, no. 1, 2017, pp. 206-211.
Poongunran J, Perera HK, Jayasinghe L, et al. Bioassay-guided fractionation and identification of α-amylase inhibitors from Syzygium cumini leaves. Pharm Biol. 2017;55(1):206-211.
Poongunran, J., Perera, H. K., Jayasinghe, L., Fernando, I. T., Sivakanesan, R., Araya, H., & Fujimoto, Y. (2017). Bioassay-guided fractionation and identification of α-amylase inhibitors from Syzygium cumini leaves. Pharmaceutical Biology, 55(1), 206-211.
Poongunran J, et al. Bioassay-guided Fractionation and Identification of Α-amylase Inhibitors From Syzygium Cumini Leaves. Pharm Biol. 2017;55(1):206-211. PubMed PMID: 27927056.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Bioassay-guided fractionation and identification of α-amylase inhibitors from Syzygium cumini leaves. AU - Poongunran,Jeyakumaran, AU - Perera,Handunge Kumudu Irani, AU - Jayasinghe,Lalith, AU - Fernando,Irushika Thushari, AU - Sivakanesan,Ramaiah, AU - Araya,Hiroshi, AU - Fujimoto,Yoshinori, PY - 2016/12/9/entrez PY - 2016/12/9/pubmed PY - 2017/3/11/medline KW - oleanolic acid KW - ursolic acid KW - α-Glucosidase SP - 206 EP - 211 JF - Pharmaceutical biology JO - Pharm Biol VL - 55 IS - 1 N2 - CONTEXT: Pancreatic α-amylase and α-glucosidase inhibitors serve as important strategies in the management of blood glucose. Even though Syzygium cumini (L.) Skeels (Myrtaceae) (SC) is used extensively to treat diabetes; scientific evidence on antidiabetic effects of SC leaves is scarce. OBJECTIVE: SC leaf extract was investigated for α-amylase inhibitory effect and continued with isolation and identification of α-amylase inhibitors. MATERIALS AND METHODS: Bioassay-guided fractionation was conducted using in vitro α-amylase inhibitory assay (with 20-1000 μg/mL test material) to isolate the inhibitory compounds from ethyl acetate extract of SC leaves. Structures of the isolated inhibitory compounds were elucidated using 1H NMR and 13C NMR spectroscopic analysis and direct TLC and HPLC comparison with authentic samples. Study period was from October 2013 to October 2015. RESULTS: An active fraction obtained with chromatographic separation of the extract inhibited porcine pancreatic α-amylase with an IC50 of 39.9 μg/mL. Furthermore, it showed a strong inhibition on α-glucosidase with an IC50 of 28.2 μg/mL. The active fraction was determined to be a 3:1 mixture of ursolic acid and oleanolic acid. Pure ursolic acid and oleanolic acid showed IC50 values of 6.7 and 57.4 μg/mL, respectively, against α-amylase and 3.1 and 44.1 μg/mL respectively, against α-glucosidase. DISCUSSION AND CONCLUSIONS: The present study revealed strong α-amylase and α-glucosidase inhibitory effects of ursolic acid and oleanolic acid isolated from SC leaves for the first time validating the use of SC leaves in antidiabetic therapy. SN - 1744-5116 UR - https://www.unboundmedicine.com/medline/citation/27927056/Bioassay_guided_fractionation_and_identification_of_α_amylase_inhibitors_from_Syzygium_cumini_leaves_ L2 - https://www.tandfonline.com/doi/full/10.1080/13880209.2016.1257031 DB - PRIME DP - Unbound Medicine ER -