Dataset Information

Ayurvedic anti-diabetic formulation Lodhrasavam inhibits alpha-amylase, alpha-glucosidase and suppresses adipogenic activity in vitro.

ABSTRACT:

Background

The patho-physiological cross-talk between diabetes and obesity is well established. However, the choices of drugs suitable for combined treatment of diabetes and obesity are limited. Integration of complementary and alternative medicines (CAMs), like Ayurveda, with modern medicine would be a promising strategy to fill this gap. The diagnostic principles of Ayurveda define obesity as one of the predisposing factors of Madhumeha (correlated as diabetes) and recommends specific formulations for managing obese-diabetes. Lodhrasavam is one such poly-herbal formulation prescribed for obese-diabetic patients.

Objectives

The present study is an attempt to demonstrate the possible modes of action of Lodhrasavam, built on the hypothesis that the formulation can exert both anti-diabetic and anti-obesity actions.

Materials and methods

Lodhrasavam, following simulated gastro-intestinal digestion, was monitored for inhibition of ?-amylase, ?-glucosidase (key digestive enzyme targets of anti-diabetic drugs) and adipogenesis using standard in vitro model systems.

Results

Lodhrasavam digest inhibited ?-amylase (90%) and ?-glucosidase (78%) activity as well as reduced the differentiation of 3T3-L1 fibroblasts to adipocytes. Upon fractionation, the enzyme inhibitory activity and anti-adipogenic activity of the digest were found distributed in different solvent fractions. This partly indicates a potential pharmacological networking of chemically and functionally diverse bioactive molecules in Lodhrasavam.

Conclusion

The study provides a possible mode of action and an experimental support for the Ayurvedic use of Lodhrasavam for managing obese-diabetes. Generating scientific evidences and understanding the modes of action, in contemporary scientific language, would essentially help in expanding global acceptance of potentials of CAMs in the management of life style disorders.

SUBMITTER: Butala MA

PROVIDER: S-EPMC5607396 | biostudies-literature | 2017 Jul - Sep

REPOSITORIES: biostudies-literature

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Publications

Ayurvedic anti-diabetic formulation Lodhrasavam inhibits alpha-amylase, alpha-glucosidase and suppresses adipogenic activity in vitro.

Butala Megha Abhijit MA Kukkupuni Subrahmanya Kumar SK Vishnuprasad Chethala N CN

Journal of Ayurveda and integrative medicine 20170628 3

<h4>Background</h4>The patho-physiological cross-talk between diabetes and obesity is well established. However, the choices of drugs suitable for combined treatment of diabetes and obesity are limited. Integration of complementary and alternative medicines (CAMs), like Ayurveda, with modern medicine would be a promising strategy to fill this gap. The diagnostic principles of Ayurveda define obesity as one of the predisposing factors of Madhumeha (correlated as diabetes) and recommends specific ...[more]

PMID: 28668259

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Project description:BackgroundAs a traditional herbal medicine, Dracaena angustifolia Roxb has been used as an anti-inflammatory agent by the Li people in Hainan, China. In preliminary phytochemical studies conducted in our lab, its fractions were found to inhibit α-glucosidase in vitro, indicating a potential for alleviating glucose dysregulation.MethodsThrough in vitro enzymatic assays, the abilities of the separated components to affect α-glucosidase and α-amylase were evaluated. By establishing concentration gradients and generating Lineweaver-Burk plots, the corresponding inhibition modes together with kinetic parameters were assessed. Following the evaluation of the outcomes of their combination with acarbose, computational docking and molecular dynamic simulations were carried out to analyse the interaction mechanisms and perform virtual screening against human enzymes.ResultsCompared with acarbose, 7 compounds, including flavonoid derivatives, amides and aromatic derivatives, with higher α-glucosidase inhibitory efficiencies were confirmed. It was found that those competitive/mixed candidates and acarbose interacted synergistically or additively on α-glucosidase. Moreover, 3 of them were able to inhibit α-amylase in mixed mode, and additive effects were observed in combination with acarbose. Through in silico docking, it was found that the active site residues as well as adjacent residues were involved in α-glucosidase and α-amylase binding, which were mainly achieved through hydrogen bonding. Among those dual-function flavonoids, Compound 9 was predicted to be a considerable inhibitor of human enzymes, as the formation of ligand-enzyme complexes was mediated by the residues responsible for substrate recognition and catalysis, the stabilities of which were reiterated by molecular dynamics simulations.ConclusionDespite their mild effects on α-amylase, considerable α-glucosidase inhibitory efficiencies and potential synergy with acarbose were exhibited by these natural candidates. Furthermore, a stable ligand, human α-glucosidase, was predicted by the performed simulations, which provided useful information for the application of Dracaena angustifolia Roxb in diabetes treatment.

Project description:Hyperglycemia is the hallmark of type 2 diabetes mellitus, and its prevention will go a long way in managing the disease and its associated complications. Reduction of postprandial hyperglycemia through retarding carbohydrates digesting enzymes is one of the major therapeutic approaches used in the management of diabetes.The aim of the present study was to investigate the antidiabetic and cytotoxic effects of Cissus cornifolia extracts in vitro.The α-amylase and α-glucosidase inhibitory activities of ethanolic and aqueous extracts of C. cornifolia root and leaves were investigated when the cytotoxic effects of these extracts were analyzed using MTT assay on human embryonic kidney (HEK 293) cell lines.The root ethanolic extract showed a mild α-amylase inhibitory activity with IC50 value of 22.75 ± 1.23 μg/ml, but strong α-glucosidase inhibitory activity with IC50 value 2.81 ± 0.97 μg/ml and the aqueous root extract indicated moderate inhibition for both α-amylase and α-glucosidase with IC50 values of 33.70 ± 3.75 and 37.48 ± 2.35 μg/ml, respectively. The ethanolic root extract was found nontoxic at tested concentrations on HEK 293 cell lines as confirmed by the MTT assay with 93% cell viability at the highest concentration (200 μg/ml) tested. However, the aqueous extracts (leaf and root) were found cytotoxic at concentrations above 50 μg/ml.Data of this study suggest that the root ethanolic extracts of C. cornifolia possesses moderate α-amylase, but strong α-glucosidase inhibitory activity in vitro and did not show significant cytotoxicity with the tested concentrations.Present study was conducted to examine effects of antidiabetic and cyctotoxic effects of Cissus conrnifolia root and leaves extracts in vitro. Data of this study suggest that the root ethanolic extract of C. cornifolia possesses mild to moderated antidiabetic activity via inhibiting carbohydrate digesting enzymes when no significant toxicity was observed with tested concentrations. Abbreviations used: alex: Aqueous leaf extract; arex: Aqueous root extract; CC: Cissus cornifolia; DNS: Dinitrosalicylic acid; DMSO: Dimethylsulfoxide; elex: Ethanolic leaf extract; erex: Ethanolic root extract; IDF: International Diabetes Federation; MEM: Minimum essential medium; NIDDM: Noninsulin-dependent diabetes mellitus; pNPG: Para-nitrophenyl glucopyranoside; SD: Standard deviation; T2D: Type 2 diabetes.

Dataset Information

Ayurvedic anti-diabetic formulation Lodhrasavam inhibits alpha-amylase, alpha-glucosidase and suppresses adipogenic activity in vitro.

Background

Objectives

Materials and methods

Results

Conclusion

Publications

Ayurvedic anti-diabetic formulation Lodhrasavam inhibits alpha-amylase, alpha-glucosidase and suppresses adipogenic activity in vitro.

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