Comparison of analytical techniques for the identification of bioactive compounds from natural products

Abstract

Natural product extracts are a rich source of bioactive compounds. As a result, the screening of natural products for the identification of novel biologically active metabolites has been an essential part of several drug discovery programs. It is estimated that more than 70% of all drugs approved from 1981 and 2006, were either derived from or structurally similar to nature based compounds indicating the necessity for the development of a rapid method for the identification of novel compounds from plant extracts. The screening of biological matrices for the identification of novel modulators is nevertheless still challenging. In this review we discuss current techniques in phytochemical analysis and the identification of biologically active components.

Screening and Binding Analysis of Flavonoids with Alpha-Amylase Inhibitory Activity from Lotus Leaf

“…As a result, these flavonoids exhibited various inhibition on alpha-amylase and DPPH free radical scavenging activities. Apigenin, kaempferol and (2), isoquercitrin (3), taxifolin (4), luteolin (5), quercetin (6), apigenin (7), naringenin (8), kaempferol (9) and isorhamnetin (10)); (b) lotus leaf extract. isorhamnetin showed relatively higher inhibition on alphaamylase, which exhibited higher binding degrees as well.…”

“…5 In recent years, many methods and technologies were used in the screening and analysis of active compounds such as filtration, solid phase extraction and hyphenated instruments. [6][7][8][9] Centrifugal ultrafiltration is a kind of membrane separation technique, which could retain high molecular weight compounds on the membrane, and low molecular weight compounds could pass through the membrane during centrifugation. 10 Centrifugal ultrafiltration could be used for the screening of bioactive constituents for target biomolecules from complexes.…”

“…12 This method also exhibited advantages like simple operation steps, low sample consumption and simultaneous screening ability. 9 In human body, alpha-amylase could hydrolyze starch into oligosaccharides and become one of the therapeutic targets for treating many diseases, 13 especially diabetes, because they could effectively block the digestion and assimilation of carbohydrate at the early digestive absorption in body.…”

Cellular membrane affinity chromatography (CMAC) in drug discovery from complex natural matrices

“…Unfortunately, plants do not reveal their secrets easily as the identification of pharmacologically active phytochemicals is usually a difficult and time-consuming process [7]. Many pharmaceutical companies have abandoned drug discovery from natural products, considering it as a demanding high resource commitment and often leading to disappointing results (identification of known compounds and poor biological activity).…”

“…This step often leads to obtaining compounds which are easily isolated with reasonable quantities needed to run biological activity assays. The most abundant secondary metabolites are usually isolated and many of them have already well-established and known pharmacological activity profiles [7]. The use of bio-guided fractionation has provided some solutions by narrowing down the isolation process to subfractions that have been identified as having the highest activity.…”