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In-Vitro and In-Silico Alpha Amylase and Alpha Glucosidase Inhibitory Activity of Baicaelin


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1 Department of Pharmacology, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (Deemed to be university), Porur, Chennai – 600116, Tamil Nadu, India
 

Diabetes mellitus is a metabolic disorder characterized by high blood glucose level in the body. It occurs due to the inadequate amount of insulin secreted in the body or resistance of insulin receptors. In the present study, Baicalein a flavone glycoside was evaluated for its effect on alpha-amylase and alpha-glucosidase enzymes using in-vitro assays by extracting respective enzymes from whole wheat and barley in combination with in-silico analysis. In-vitro alpha amylase inhibitory activity and in-vitro alpha glucosidase inhibitory activity was performed using acarbose as a standard drug. The molecular docking study was performed using Schrodinger (Maestro V 11.5) software. The parameters glide score, Lipinski rule for drug likeliness, bioactive scoring and ADME properties were assessed in the docking study. Further, the antioxidant activity of baicalein was performed using DPPH assay, Nitric oxide scavenging activity. The cytotoxicity of baicalein was evaluated using the Brine shrimp lethality assay. The alpha-amylase assay performed showed IC50 value of 48.40 μg/ml for baicalein whereas alpha-glucosidase assay showed an IC50 value of 16.03 μg/ml. Baicalein shows the glide score of-5.565 with 5EOF and glide score of -5.339 with 5NN8 in the molecular docking study. The highest percentage of DPPH radical scavenging activity and nitrous oxide scavenging activity were found to be 27% at 160 μg/ml and 50.02% at 160 μg/ml respectively. Based on further in vivo and clinical trials, baicalein may be used for the management of hyperglycaemia.


Keywords

Alpha-amylase, Alpha-glucosidase, Baicalein, Insilico, Diabetes Mellitus
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  • Wade DM, Hankins M, Smyth DA, Rhone EE, Mythen MG, Howell DC, Weinman JA. Detecting acute distress and risk of future psychological morbidity in critically ill patients: Validation of the intensive care psychological assessment tool. 2014; Crit. Care; 18(5):519. https://doi.org/10.1186/ s13054-014-0519-8. PMid:25248614. PMCid:PMC4207352
  • Laoufi H, Benariba N, Adjdir S, Djaziri R. In vitro α-amylase and α-glucosidase inhibitory activity of Ononis angustis- sima extracts. J. Appli. Pharm. Sci. 2017; 7(2):191–8.
  • Vinayagam R, Xu B. Antidiabetic properties of dietary flavonoids: a cellular mechanism review. Nutr. Metab. 2015; 12(1):60. https://doi.org/10.1186/s12986-015-0057-7 PMid:26705405 PMCid:PMC4690284
  • Sama K, Murugesan K, Sivaraj R. In vitro alpha amylase and alpha glucosidase inhibition activity of crude ethanol extract of Cissus arnottiana. Asian Journal of Plant Science and Research. 2012; 2(4):550–53.
  • Proença C, Freitas M, Ribeiro D, Oliveira EF, Sousa JL, Tomé SM. α-Glucosidase Inhibition by Flavonoids; 2017. p. 1216–28. https://doi.org/10.1080/14756366.2017.1368503. PMid:28933564. PMCid:PMC6009965
  • Fu Y, Luo J, Jia Z, Zhen W, Zhou K, Gilbert E, Liu D. Baicalein protects against type 2 diabetes via promoting islet β-cell function in obese diabetic mice. International journal of Endocrinology. 2014. https://doi.org/10.1155/2014/846742. PMid:25147566. PMCid:PMC4132321
  • Waisundara VY, Hsu A, Huang D, Tan BKH. Scutellaria baicalensis enhances the anti-diabetic activity of metformin in streptozotocin-induced diabetic Wistar rats. The Am. J. Chin. Med. 2008; 36(03):517–40. https://doi.org/10.1142/ S0192415X08005953. Mid:18543386
  • Zhang B, Sun W, Yu N, Sun J, Yu X, Li X, Dong Y. Anti-diabetic effect of baicalein is associated with the modulation of gut microbiota in streptozotocin and high-fat-diet induced dia- betic rats. J. Funct. Foods. 2018; 46:256–67.
  • Nair SS, Kavrekar V, Mishra A. In vitro studies on alpha amylase and alpha glucosidase inhibitory activities of selected plant extracts. Eur. J. Exp. Biol. 2013; 3(1):128–32.
  • Stark JR, Yin XS. Evidence for the presence of maltase and α‐glucosidase isoenzymes in barley. J. Inst. Brew. 1987; 93(2):108–12. https://doi.org/10.1002/j.2050-0416.1987. tb04485.x
  • Mahrous R, Ghareeb DA, Fathy HM, EL-Khair RMA, Omar AA. The protective effect of Egyptian Withania somnifera against Alzheimer’s. Med. Aromat. Plants. 2017; 6(285). https://doi.org/10.4172/2167-0412.1000285
  • McLaughlin JL. Brine shrimp: A convenient general bio- assay for active constituents. Planta Med. 1982; 45:31–2. https://doi.org/10.1055/s-2007-971236
  • Sarah QS, Anny FC, Mir M. Brine shrimp lethality assay. Bangladesh Journal of Pharmacology. 2017; 12(2):186–9. https://doi.org/10.3329/bjp.v12i2.32796
  • Nachammai V, Srikanth J, Lavanya R, Reddy C, Maheswara U. In-vitro and in Silico Alpha Amylase and Alpha- Glucosidase Inhibitory Activity of Emblica officinalis. Res. J. Pharm. Biol. Chem. Sci. 2018; 9(5):1784–94.
  • Barua J, Sany MA, Barua L, Hossen M, Absar N, Hossain Z, Akther S. Insilico molecular docking of some isolated selected compounds of Phoenix sylvestris (L.) against Diabetes. Biomed J Sci Tech Res. 2019; 16(2):11883–6. https://doi.org/10.26717/BJSTR.2019.16.002819
  • Jackie B, Sagar S, Alamgir H, Razowanul MF, Sumaiya F, Emon D, et al. In silico Molecular Docking and ADME/T Analysis of Some Selected Isolated Compounds of Phyllanthus emblica against Type 2 Diabetics. Am. J. Ethnomed. 2018; 5(2):9.
  • Singh J, Kakkar P. Modulation of liver function, antioxi- dant responses, insulin resistance and glucose transport by Oroxylum indicum stem bark in STZ induced diabetic rats. Food Chem. Toxicol. 2013; 62:722–31. https://doi. org/10.1016/j.fct.2013.09.035. PMid:24140466

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  • In-Vitro and In-Silico Alpha Amylase and Alpha Glucosidase Inhibitory Activity of Baicaelin

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Authors

A. A. Dinesh
Department of Pharmacology, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (Deemed to be university), Porur, Chennai – 600116, Tamil Nadu, India
Srikanth Logesh Kumar
Department of Pharmacology, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (Deemed to be university), Porur, Chennai – 600116, Tamil Nadu, India
T. Geethanjali
Department of Pharmacology, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (Deemed to be university), Porur, Chennai – 600116, Tamil Nadu, India
S. C. Dhanalakshmi
Department of Pharmacology, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (Deemed to be university), Porur, Chennai – 600116, Tamil Nadu, India
V. Iyyappan
Department of Pharmacology, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (Deemed to be university), Porur, Chennai – 600116, Tamil Nadu, India
P. Aravind
Department of Pharmacology, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (Deemed to be university), Porur, Chennai – 600116, Tamil Nadu, India
V. Hemapriya
Department of Pharmacology, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (Deemed to be university), Porur, Chennai – 600116, Tamil Nadu, India
D. Arulmozhi
Department of Pharmacology, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (Deemed to be university), Porur, Chennai – 600116, Tamil Nadu, India
J. Srikanth
Department of Pharmacology, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (Deemed to be university), Porur, Chennai – 600116, Tamil Nadu, India

Abstract


Diabetes mellitus is a metabolic disorder characterized by high blood glucose level in the body. It occurs due to the inadequate amount of insulin secreted in the body or resistance of insulin receptors. In the present study, Baicalein a flavone glycoside was evaluated for its effect on alpha-amylase and alpha-glucosidase enzymes using in-vitro assays by extracting respective enzymes from whole wheat and barley in combination with in-silico analysis. In-vitro alpha amylase inhibitory activity and in-vitro alpha glucosidase inhibitory activity was performed using acarbose as a standard drug. The molecular docking study was performed using Schrodinger (Maestro V 11.5) software. The parameters glide score, Lipinski rule for drug likeliness, bioactive scoring and ADME properties were assessed in the docking study. Further, the antioxidant activity of baicalein was performed using DPPH assay, Nitric oxide scavenging activity. The cytotoxicity of baicalein was evaluated using the Brine shrimp lethality assay. The alpha-amylase assay performed showed IC50 value of 48.40 μg/ml for baicalein whereas alpha-glucosidase assay showed an IC50 value of 16.03 μg/ml. Baicalein shows the glide score of-5.565 with 5EOF and glide score of -5.339 with 5NN8 in the molecular docking study. The highest percentage of DPPH radical scavenging activity and nitrous oxide scavenging activity were found to be 27% at 160 μg/ml and 50.02% at 160 μg/ml respectively. Based on further in vivo and clinical trials, baicalein may be used for the management of hyperglycaemia.


Keywords


Alpha-amylase, Alpha-glucosidase, Baicalein, Insilico, Diabetes Mellitus

References





DOI: https://doi.org/10.18311/jnr%2F2022%2F26819