lacinartin and coumarin

Monoamine oxidase (MAO) enzyme inhibition is a crucial target for the management of depression and Alzheimer disease and inhibitors of MAO are the most important drugs for their management. Coumarins are a large family of compounds, of natural and synthetic origin, that exhibit a variety of pharmacological activities, including MAO inhibition. The current review highlights the design and synthetic methods of coumarin derivatives as well as coumarins obtained from plant source as MAO inhibitors for treatment of depression and Alzheimer disease with salient finding related to structure-activity relationship. The aim of present review is to find out natural as well as synthetic coumarins as MAO inhibitors.

Topics: Alzheimer Disease; Coumarins; Depression; Drug Design; Humans; Models, Molecular; Molecular Structure; Monoamine Oxidase; Monoamine Oxidase Inhibitors; Structure-Activity Relationship

A methanol extract of Zanthoxylum schinifolium stems at a concentration of 250 microg/ml showed potent inhibitory activity against monoamine oxidase (MAO) in a mouse brain. Activity-guided separation and purification of the extract yielded lacinartin (1) as an active coumarin compound. Lacinartin showed significant inhibitory effects on MAO in a dose-dependent manner. The IC(50) value on MAO activity was 9.2 microM. The MAO-A (IC(50) value, 5.7 microM) sensitivity to lacinartin was greater than that of MAO-B (IC(50) value, 28.6 microM). An enzyme kinetic study revealed that lacinartin inhibited MAO activity by a non-competitive mode.

Topics: Animals; Brain; Coumarins; Dose-Response Relationship, Drug; Kinetics; Male; Mice; Monoamine Oxidase; Monoamine Oxidase Inhibitors; Plant Extracts; Rutaceae