Evaluation of Lipase Inhibitory Activity and Formulation of Polyherbal Syrup for Hyperlipidemia.

Abstract

Background: Since synthetic medications used in hyperlipidemia cause undesirable side effects upon long term administration, prompting interest in natural remedies for their non-toxic properties. Thus, Kalanchoe pinnata and Atalantia ceylanica plants which were scientifically proven with serum cholesterol reducing activity were considered in this study.

Objectives: To evaluate the lipase inhibitory activity and toxicity profile of the aqueous leaf extracts of K. pinnata and A. ceylanica, to formulate a polyherbal syrup and evaluate physicochemical properties and stability

Methods: The aqueous macerated products of each fresh leaves were freeze-dried and test samples of (15000, 12000, 11000, 10000, 5000, 2500 ppm) were prepared to evaluate in vitro lipase inhibitory and brine shrimp lethality assays. The lipase inhibitory assay was triplicated using Orlistat as the positive control. The 1 mg/mL of 1.5 mL porcine pancreatic lipase enzyme and 1.5 mL of each test sample were mixed and incubated at 30℃ for 1hour. Then 3 µL of 10mM P-nitro phenyl butyrate substrate was added, re-incubated for 5 minutes at 30℃ and absorption was measured at 405 nm. Five different syrup bases were prepared using distilled water, saccharin, sodium benzoate, citric acid and subjected to evaluate stability and physicochemical properties at room temperature. Three different extract ratios of K. pinnata and A. ceylanica were incorporated to the stable base and three polyherbal syrups were prepared and evaluated lipase inhibitory activity, color, odor, appearance and pH along with long-term and short-term stability. Results: The 15000 ppm concentration showed the highest lipase inhibition for the K. pinnata and A. ceylanica (36.68%±0.002 and 76.02%±0.004, respectively) compared to the positive control (IC50 1224.75 ppm). The polyherbal syrup with extraction ratio of 1.5: 1.1 showed the highest enzyme inhibition (63.06%±0.008) with non-toxic nature. This formulation was stable at room temperature to date with odorless, clear pale green appearance and the pH was at the acceptance range of pH 4.0-6.9. Conclusion: The stable polyherbal syrup which showed 63% of lipase inhibition with no toxic effects can be considered for further development to treat hyperlipidemia.