Top

BMC Complementary Medicine and Therapies

Published in:

Open Access 01-12-2012 | Research article

Potent α-glucosidase and α-amylase inhibitory activities of standardized 50% ethanolic extracts and sinensetin from Orthosiphon stamineus Benth as anti-diabetic mechanism

Authors: Elsnoussi Ali Hussin Mohamed, Mohammad Jamshed Ahmad Siddiqui, Lee Fung Ang, Amirin Sadikun, Sue Hay Chan, Soo Choon Tan, Mohd Zaini Asmawi, Mun Fei Yam

Published in: BMC Complementary Medicine and Therapies | Issue 1/2012

Abstract

Background

In the present study, we tested a 50% ethanolic extract of Orthosiphon stamineus plants and its isolated bioactive compound with respect to their α-glucosidase and α-amylase inhibitory activities.

Methods

Bioactive flavonoid sinensetin was isolated from 50% ethanolic extract of Orthosiphon stamineus. The structure of this pure compound was determined on the NMR data and the α-glucosidase and α-amylase inhibitory activities of isolated sinensetin and 50% ethanolic extract of Orthosiphon stamineus were evaluated.

Results

In vitro studies of a 50% ethanolic extract of O. stamineus and the isolated sinensetin compound showed inhibitory activity on α-glucosidase (IC₅₀: 4.63 and 0.66 mg/ml, respectively) and α-amylase (IC₅₀: 36.70 mg/ml and 1.13 mg/ml, respectively). Inhibition of these enzymes provides a strong biochemical basis for the management of type 2 diabetes via the control of glucose absorption.

Conclusion

Alpha-glucosidase and α-amylase inhibition could the mechanisms through which the 50% ethanolic extract of O. stamineus and sinensetin exert their antidiabetic activity, indicating that it could have potential use in the management of non-insulin-dependent diabetes.

Available only for authorised users

Harrower AD: Comparison of efficacy, secondary failure rate, and complications of sulfonylureas. J Diabetes Complications. 1994, 8: 201-203. 10.1016/1056-8727(94)90044-2.CrossRefPubMed

Reuser AJ, Wisselaar HA: An evaluation of the potential side-effects of alpha-glucosidase inhibitors used for the management of diabetes mellitus. Eur J Clin Invest. 1994, 24: 19-24.CrossRefPubMed

Campbell RK, White JR, Saulie BA: Metformin: a new oral biguanide. Clin Ther. 1996, 18: 360-371. 10.1016/S0149-2918(96)80017-8.CrossRefPubMed

Kwon YI, Apostolidis E, Shetty K: Inhibitory potential of wine and tea against α-amylase and α-glucosidase for management of hyperglycemia linked to type 2 diabetes. J Food Biochem. 2008, 32: 15-31. 10.1111/j.1745-4514.2007.00165.x.CrossRef

Gray GM: Carbohydrate digestion and absorption–role of small intestine. N Engl J Med. 1975, 292: 1225-1230. 10.1056/NEJM197506052922308.CrossRefPubMed

Krentz AJ, Baile CJ: Oral antidiabetic agents: Current role in type 2 diabetes mellitus. Drugs. 2005, 65: 385-411. 10.2165/00003495-200565030-00005.CrossRefPubMed

Jaganath L, Ng LT: Herbs: The green pharmacy of Malaysia. 2000, Kuala Lumpur: Vinpress Sdn. Bhd, 76-77.

Awale S, Tezuka Y, Banskota AH, Adnyana IK, Kadota S: Nitric oxide inhibitory isopimarane-type diterpenes from Orthosiphon stamineus of Indonesia. J Nat Prod. 2003, 66: 255-258. 10.1021/np020455x.CrossRefPubMed

Awale S, Tezuka Y, Banskota AH, Kadota S: Highly-oxygenated isopimarane-type diterpenes from Orthosiphon stamineus of Indonesia and their nitric oxide inhibitory activity. Chem Pharm Bull. 2003, 26: 268-275.CrossRef

10.

Malterud KE, Hanche-Olsen IM, Smith-Kelland I: Flavonoids from Orthosiphon spicatus. Planta Med. 1989, 55: 569-570. 10.1055/s-2006-962099.CrossRefPubMed

11.

Sumaryono W, Proksch P, Wray V, Witte L, Hartmann T: Qualitative and quantitative analysis of the phenolic constituents from Orthosiphon aristatus. Planta Med. 1991, 57: 176-180. 10.1055/s-2006-960060.CrossRefPubMed

12.

Masuda T, Masuda K, Shiragami S, Jitoe A, Nakatani N: Orthosiphols A and B, novel diterpenoid inhibitors of TPA (12-O-tetradecanoylphorbol-13-acetate)-induced inflammation, from Orthosiphon stamineus. Tetrahedron. 1992, 48: 6787-6792. 10.1016/S0040-4020(01)89868-9.CrossRef

13.

Tezuka Y, Stampoulis P, Banskota AH, Awale S, Tran KQ, Saiki I, Kadota S: Constituents of the Vietnamese medicinal plant Orthosiphon stamineus. Chem Pharm Bull. 2000, 48: 1711-1719. 10.1248/cpb.48.1711.CrossRefPubMed

14.

Olah NK, Radu L, Mogoşan C, Hanganu D, Gocan S: Phytochemical and pharmacological studies on Orthosiphon stamineus Benth. (Lamiaceae) hydroalcoholic extracts. J Pharm Biomed Anal. 2003, 33: 117-123. 10.1016/S0731-7085(03)00227-9.CrossRefPubMed

15.

Mohamed EA, Mohamed AJ, Asmawi MZ, Sadikun A, Ebrika OS, Yam MF: Antihyperglycemic Effect of Orthosiphon Stamineus benth leaves extract and its bioassay-guided fractions. Molecules. 2011, 16: 3787-3801. 10.3390/molecules16053787.CrossRefPubMed

16.

Yam MF, Asmawi MZ, Basir R: An Investigation of the anti-inflammatory and analgesic effects of Orthosiphon stamineus leaf extract. J Med Food. 2008, 11: 362-368. 10.1089/jmf.2006.065.CrossRefPubMed

17.

Yam MF, Ang LF, Salman IM, Ameer OZ, Lim V, Ong LM, Ahmad M, Asmawi MZ, Basir R: Orthosiphon stamineus leaf extract protects against ethanol-induced gastropathy in rats. J Med Food. 2009, 12: 1089-1097. 10.1089/jmf.2008.0005.CrossRefPubMed

18.

Yam MF, Mohamed EAH, Ang LF, Pei L, Darwis Y, Mahmud R, Asmawi MZ, Basir R, Ahmad M: A simple isocratic HPLC method for the simultaneous determination of sinensetin, eupatorin, and 3′-hydroxy-5,6,7,4′-tetramethoxyflavone in Orthosiphon stamineus extracts. J Acupunct Meridian Stud. 2012, 5: 176-182. 10.1016/j.jams.2012.05.005.CrossRefPubMed

19.

Yam MF, Lim V, Salman IM, Ameer OZ, Ang LF, Rosidah N, Abdulkarim MF, Abdullah GZ, Basir R, Sadikun A, Asmawi MZ: HPLC and anti-inflammatory studies of the flavonoid rich chloroform extract fraction of Orthosiphon stamineus leaves. Molecules. 2010, 15: 4452-4466. 10.3390/molecules15064452.CrossRefPubMed

20.

Apostolidis E, Kwon Y, Shetty K: Inhibitory potential of herb, fruit, and fungal-enriched cheese against key enzymes linked to type 2 diabetes and hypertension. Innovative Food Science and Emerging Technologies. 2007, 8: 46-54. 10.1016/j.ifset.2006.06.001.CrossRef

21.

Young-In K, Emmanouil A, Kalids S: Inhibitory potential of wine and tea against α-amylase and α-glucosidase for management of hyperglycemia linked to type 2 diabetes. J Food Biochem. 2008, 32: 15-31. 10.1111/j.1745-4514.2007.00165.x.CrossRef

22.

World Health Organisation Consultation: Definition, diagnosis and classification of diabetes mellitus and its complications. Part 1: diagnosis and classification of diabetes mellitus. 1999, Geneva: Report of WHO Consultation

23.

Rhabasa-Lhoret R, Chiasson JL: α-Glucosidase inhibitors. International Textbook of Diabetes Mellitus, vol. 1. Edited by: Defronzo RA, Ferrannini E, Keen H, Zimmet P. 2004, U.K: John Wiley & Sons Ltd, 901-914. 3

24.

Bailey CJ: New approaches to the pharmacotherapy of diabetes. Textbook of Diabetes, vol. 2. Edited by: Pickup JC, William G. 2003, U.K: Blackwell Science Ltd, 73.1-73.21. 3

25.

Joubert PH, Venter HL, Foukaridis GN: The effect of miglitol and acarbose after an oral glucose load: A novel hypoglycaemic mechanism. Br J Clin Pharmacol. 1990, 30: 391-396. 10.1111/j.1365-2125.1990.tb03789.x.CrossRefPubMedPubMedCentral

26.

Mariam A, Asmawi MZ, Sadikun A: Hypoglycaemic activity of the aqueous extract of Orthosiphon stamineus. Fitoterapia. 1996, 67: 465-468.

27.

Sriplang K, Adisakwattana S, Rungsipipat A, Yibchok-Anun S: Effects of Orthosiphon stamineus aqueous extract on plasma glucose concentration and lipid profile in normal and streptozotocin-induced diabetic rats. J Ethnopharmacol. 2007, 109: 510-514. 10.1016/j.jep.2006.08.027.CrossRefPubMed

28.

Cheng JT, Liu IM: Stimulatory effect of caffeic acid on alpha 1 Aadrenoceptors to increase glucose uptake into cultured C2C12 cells. Naunyn Schmiedebergs Arch Pharmacol. 2000, 362: 122-127. 10.1007/s002100000274.CrossRefPubMed

29.

Tadera K, Minami Y, Takamatsu K, Matsuoka T: Inhibition of alpha-glucosidase and alpha-amylase by flavonoids. J Nutr Sci Vitaminol. 2006, 52: 149-153. 10.3177/jnsv.52.149.CrossRefPubMed

30.

Kwon YI, Apostolidis E, Shetty K: In vitro studies of eggplant (Solanum melongena) phenolics as inhibitors of key enzymes relevant for type 2 diabetes and hypertension. Bioresour Technol. 2008, 99: 2981-2988. 10.1016/j.biortech.2007.06.035.CrossRefPubMed

The pre-publication history for this paper can be accessed here:http://www.biomedcentral.com/1472-6882/12/176/prepub

Title: Potent α-glucosidase and α-amylase inhibitory activities of standardized 50% ethanolic extracts and sinensetin from Orthosiphon stamineus Benth as anti-diabetic mechanism
Authors: Elsnoussi Ali Hussin Mohamed
Mohammad Jamshed Ahmad Siddiqui
Lee Fung Ang
Amirin Sadikun
Sue Hay Chan
Soo Choon Tan
Mohd Zaini Asmawi
Mun Fei Yam
Publication date: 01-12-2012
Publisher: BioMed Central
Published in: BMC Complementary Medicine and Therapies / Issue 1/2012
Electronic ISSN: 2662-7671
DOI: https://doi.org/10.1186/1472-6882-12-176

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Potent α-glucosidase and α-amylase inhibitory activities of standardized 50% ethanolic extracts and sinensetin from Orthosiphon stamineus Benth as anti-diabetic mechanism

Abstract

Background

Methods

Results

Conclusion

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Abstract

Background

Methods

Results

Conclusion

Please log in to get access to this content

Other articles of this Issue 1/2012

Rhodiola rosea for physical and mental fatigue: a systematic review

A gallotannin-rich fraction from Caesalpinia spinosa (Molina) Kuntze displays cytotoxic activity and raises sensitivity to doxorubicin in a leukemia cell line

Kalanchoe tubiflora extract inhibits cell proliferation by affecting the mitotic apparatus

Mindfulness-based stress reduction for low back pain. A systematic review

Evaluation of a multi-herb supplement for erectile dysfunction: a randomized double-blind, placebo-controlled study

A six-month crossover chemoprevention clinical trial of tea in smokers and non-smokers: methodological issues in a feasibility study