High-Performance Thin-Layer Chromatography Hyphenated with Microchemical and Biochemical Derivatizations in Bioactivity Profiling of Marine Species.

Snezana Agatonovic-Kustrin,Vladimir Gegechkori,David Morton,Ella Kustrin

doi:10.3390/md17030148

Snezana Agatonovic-Kustrin, Vladimir Gegechkori + Show 2 more

Open Access

https://doi.org/10.3390/md17030148

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Journal: Marine Drugs	Publication Date: Mar 3, 2019
Citations: 35	License type: CC BY 4.0

Affiliation: Sechenov University, La Trobe University

Abstract

Marine organisms produce an array of biologically active natural products, many of which have unique structures that have not been found in terrestrial organisms. Hence, marine algae provide a unique source of bioactive compounds. The present study investigated 19 marine algae and one seagrass collected from Torquay beach, Victoria, Australia. High-performance thin-layer chromatography (HPTLC) hyphenated with microchemical (DPPH•, p-anisaldehyde, and Fast Blue B) and biochemical (α-amylase and acetylcholine esterase (AChE) enzymatic) derivatizations was used to evaluate antioxidant activity, presence of phytosterols and phenolic lipids, α-amylase and AChE inhibitory activities of extract components. Significant α-amylase and AChE inhibitory activities were observed in samples 2, 6, 8 and 10. Antioxidant activities in the samples were found to be correlated to phytosterol content (R2 = 0.78), but was not found to be related to either α-amylase or AChE inhibitory activities. α-Amylase inhibitory activities were correlated to AChE inhibition (R2 = 0.77) and attributed to the phytosterol content, based on the similar peak position in the chromatograms with the β-sitosterol chromatogram. Samples 1, 8, and especially sample 20, were found to contain phenolic lipids (alkyl resorcinol derivatives) with significant antioxidant activities. The results suggest that these marine species have a significant number of bioactive compounds that warrant further investigation.

Highlights

Effect-directed analysis (EDA), based on the combination of chromatography with chemical and biochemical analyses, is widely used in drug discovery, especially in target-directed identification of biologically active molecules in complex samples [1,2,3]
The dried chromatographic plates were subjected to non-targeted chemical derivatizations with p-anisaldehyde and Fast Blue B, and targeted assays using an antioxidant Diphenyl-1-picrylhydrazyl free radical (DPPH) free radical, assay and enzymatic assays with α-amylase and AChE
After derivatization with DPPH, compounds with radical-scavenging activity are visualized as bright yellow zones against a purple background on the chromatographic plate (Figure 1A)

Summary

Introduction

Effect-directed analysis (EDA), based on the combination of chromatography with chemical and biochemical analyses, is widely used in drug discovery, especially in target-directed identification of biologically active molecules in complex samples [1,2,3]. Diabetes, dementia, and Alzheimer’s disease (AD) can be improved with drugs showing selective enzymatic inhibition/induction and antioxidant activity. The main purpose of diabetic therapies is to control the blood glucose level and to prevent complications such as cardiovascular disease. Mar. Drugs 2019, 17, 148; doi:10.3390/md17030148 www.mdpi.com/journal/marinedrugs.

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