Inhibition of monoamine oxidase by derivatives of piperine, an alkaloid from the pepper plant Piper nigrum, for possible use in Parkinson’s disease

Piperine has shown that it has wide range of effects, including monoamine oxidase B inhibitory effect which is one the targets in treating Parkinson disease. Piperine which is an alkaloid is the active ingredient of plant of black and white pepper grain, Piper nigrum. Several compounds related to piperine was screening using monoamine oxidase B and monoamine oxidase A assays. Z-factor statistical analysis showed that monoamine oxidase (A and B) assays was greater than (0.8). Most of test compounds were selective toward monoamine oxidase B enzyme, with the most potent compound with IC-50 of 498 micro molar . To obtain insight understanding of binding of test compounds to monoamine oxidase B enzyme, each test compound was docked to the crystal structure of monoamine oxidase B enzyme using Autodock 4.2 and Auto dock tools programs. Bovine serum albumin high throughput screening assay was performed to each test compound to understand their binding pattern to this carrier protein. To estimate blood brain barrier permeability, PAMPA method was used and it was showed that most test compounds be able to pass blood brain barrier. Taking together, the date obtained here may be useful in design selective monoamine oxidase B inhibitory compound without monoamine oxidase A activity that is able pass blood brain barrier and reach an active site.