DEVELOPMENT AND CHARACTERIZATION OF POLYHERBAL FORMULATIONS FOR BIOACTIVE PROPERTIES TO TARGET DIABETES MELLITUS

The present study was conducted to develop and characterize two polyherbal formulations (S11 and S12) against alpha amylase, intestinal glucosidase, Advanced Glycation End-products to find a potential multi-targeted inhibitor. Cytotoxicity was evaluated for ABCB1 (P-glycoprotein) overexpressing cells. It is a multi-drug resistant ATP- binding cassette transporter protein. Physiologically it exports toxins out of the cell, however, in diabetic condition it showed altered expression mainly in the intestine thus affecting the absorption properties of drugs. In control five individual plants Chichorium Intybus (S3), Trigonella foenum graecum (S5), Saussaurea Lappa (S6), Lipidium Sativum (S7), Nigella Sativum (S8) have also been evaluated in certain assays. Amylase, glucosidase and AGEs inhibition were measured spectrophotmetrically. Cell proliferation inhibition was measured using ELISA and phytochemical determination was carried out spectrophotometrically. Results revealed potent activity of both S11 [combination of S3 (1g) and S8 (9g)] and S12 [combination of S3 (1.5g), S5 (1g), S6 (1g), S7 (1g), S8 (5.5g)] against alpha amylase (6.740 +/- 0.02 mu g/mL and 11 +/- 0.05 mu g/mL) and intestinal glucosidase (947 +/- 0.07 mu g/mL and 522 +/- 0.03 mu g/mL). In antiglycation assays both S11 and S12 showed comparable activity with IC50 values of 31 +/- 0.24 and 35 +/- 0.28 mu g/mL respectively. MTT assays also revealed potent inhibition of ABCB1 overexpressing cells proliferation by S11 and S12 with IC50 values of 2.497 +/- 0.12 mu g/mL and 2.279 +/- 0.36 mu g/mL respectively. When the data were correlated with phytoactive class of compounds it has been noticed that flavonoids (S11: 1312 +/- 29.3 mu g/mL and S12: 1450 +/- 56.8 mu g/mL) are found in much more concentration as compared to total phenolic content (S11:575 +/- 83 mu g/mL and S12: 403 +/- 99.03 mu g/mL). To the best of our knowledge this is the very first study to report these novel formulations as potent multi-targeted antidiabetic drug candidates. novel formulations as potent multi-targeted antidiabetic drug candidates.