Synthesized Phytomolecular Hybrids as Natural Interventions to Manage Hyperlipidemia and to Ameliorate Diabetes in Streptozotocin Induced Mice

Abstract

Diabetes mellitus had emerged as a metabolic menace which leads to the development of dyslipidemia, myocardial infarction, coronary artery diseases, obesity and hypertension. These are critical hallmarks for severe metabolic disorders owing to lack of proper balance between the energy intake and energy consumed. Previously, various potent biomarkers were investigated for their remarked potential against diabetes as well as hyperlipidemia. With this contextual, we synthesized different phytomolecular hybrids from the known potent biomarkers lupeol, β-sitosterol, ursolic acid, gallic acid and cinnamic acid by esterification with dicyclohexyl-carbodiimide as a coupling reagent and 4-dimethylaminopyridine as a catalyst. The compounds were purified using column chromatography and identified by mass spectroscopy, IR spectroscopy, NMR spectroscopy (¹H and ¹³C).Through in vitro screening by α-amylase assay and antioxidant assay, PMH1, PMH2 and PMH4 were found as effective phytomolecular hybrid compounds that displayed potential anti-diabetic, anti-hyperlipidemic as well as anti-oxidant properties. Amongst them, PMH4 prevailed in inhibiting the adipocyte differentiation. Our findings showed significant antidiabetic (STZ model in rats), antihyperlipidemic and antioxidant outcomes by PMH4. Synthesized phytomolecular hybrids with known potent biomarkers can be an effective strategy to design new interventions with effective bioactivity to elicit prominent in vivo performance.

Highlights

• Phytomolecular hybrids from the known potent biomarkers lupeol, β-sitosterol, ursolic acid, gallic acid and cinnamic acid were synthesized by esterification with dicyclohexylcarbodiimide as a coupling reagent and 4-dimethylaminopyridine as a catalyst.

• Synthesized effective phytomolecular hybrid compounds were screened for potential anti-diabetic, anti-hyperlipidemic as well as anti-oxidant properties invitro assays.

• Synthesized effective phytomolecular hybrid PMH4 prevailed in inhibiting the adipocyte differentiation and displayed significant antidiabetic (STZ model in rats), antihyperlipidemic and antioxidant outcomes.

• Synthesized phytomolecular hybrids with known potent biomarkers can be an effective approach to design new interventions with effective bioactivity

Keywords:

• Diabetes
• hyperlipidemia
• phytomolecules
• bioactivity
• antioxidant

Acknowledgements

Authors are thankful to Council of Science and Technology (CSIR),Department of Science and Technology (DST), New Delhi, India (INSPIRE and SERB-NPDF) for the financial support and Director CSIR-National Botanical Research Institute, Lucknow for providing facilities to carry out this work. Authors are also obliged for SAIF-Division, CSIR- Central Drug Research Institute, Lucknow for providing the spectral data.

Disclosure statement

No potential conflict of interest was reported by the authors.