A Method for the Rapid Discovery of Naturally Occurring Products by Proteins Immobilized on Magnetic Beads and Reverse Affinity Chromatography

Abstract

A highly efficient screening method for naturally occurring products that bind to a specific target protein was demonstrated by using hVDR magnetic beads. The native ligand 1alpha,25(OH)2 VD3 (1) was selectively bound by hVDR magnetic beads when present in a mixture of natural compounds. Furthermore, this method was shown to be applicable to the identification of natural products that interact with a specific protein immobilized on the beads from an extract of a natural resource. Two new natural compounds were isolated by this method. This approach will be helpful for the discovery of novel, naturally occurring products that bind to specific target proteins. This method has the further advantages that it can identify the HPLC peak corresponding to the target compound for isolation, as well as provide important UV, CD, or MS profile information.

Matching the power of high throughput screening to the chemical diversity of natural products

“…156 Their work has focused on plant and myxomycete products, and has included a variety of assays for apoptotic targets. 142,178,179,180 …”

Hes1 inhibitor isolated by target protein oriented natural products isolation (TPO-NAPI) of differentiation activators of neural stem cells

“…27 – 30 However, in contrast to the rapid innovations in large-scale screening, innovations in “target protein oriented natural product isolation” (TPO-NAPI) have developed more slowly. 31 – 39 We previously reported an isolation of new natural products which bind a target protein using protein-immobilized beads-HPLC method. 39 The ability of a natural product to bind to a target protein is important for estimating the bioactivity of the natural product.…”

“… 31 – 39 We previously reported an isolation of new natural products which bind a target protein using protein-immobilized beads-HPLC method. 39 The ability of a natural product to bind to a target protein is important for estimating the bioactivity of the natural product. Thus, a target protein-beads-HPLC method would be a powerful approach for isolating bioactive natural compounds from natural product extracts.…”

Approaches to Neural Stem Cells and Cancer Cells Based on Natural Products

“…(Fig. 1) 4) There is a strong demand for the "quick" discovery of novel natural products which are potential candidates for new medicines. To this end, we developed a method for the rapid discovery of natural products using protein magnetic beads.…”