Anti-depression new small molecule found in Chinese medicine Magnolia

Anti-depression new small molecule found in Chinese medicine Magnolia

July 18, 2018 Source: Science and Technology Daily Author: Zhao Hanbin

Depression is a common mental illness with more than 300 million people worldwide suffering from depression and is distributed across all ages. On the 17th, from the Kunming Institute of Botany, Chinese Academy of Sciences, the researchers found a new type of small molecule with antidepressant effect on melatonin receptors through the study of traditional Chinese medicine Magnolia, which can be used for new antidepressants. Research and development.

Previously, the research team of Chen Jijun of the Kunming Institute of Botany, Chinese Academy of Sciences, used the anti-psychotic cells and the whole animal research platform established by this research group to study traditional Chinese medicines such as red peony root, Bupleurum, jujube kernel, acacia flower, and polygala. A series of active compounds.

Melatonin is mainly a steroid hormone produced by the pineal gland. Its abnormal secretion or the expression and activity of the corresponding receptors may cause a series of mental illnesses such as depression and sleep disorders. Using the in vitro screening model of melatonin receptors, the researchers found that magnolol has a certain agonistic effect on the receptor from Magnolia. In order to find highly active compounds, they structurally modify and optimize magnolol to synthesize a series of derivatives. By in vitro activity assays, they found that magnolol glucoside (7c) was the most potent and the stimulatory effect of honokiol on melatonin receptors was enhanced by 2.5 to 7.5 fold. At the same time, the results of in vivo pharmacodynamic evaluation also showed that compound 7c can exert potential antidepressant effects by affecting the level of neurotransmitters in the brain of mice.

Subsequently, compound 7c was subjected to in vivo metabolite research and preliminary safety evaluation. A total of 25 metabolites were detected from mouse plasma, urine and feces. Acute toxicity experiments showed that the compound has good safety and developed into a new anti-resistant product. Potential application prospects for depression drugs.

This achievement has been published in the leading journal of the European Journal of Medicinal Chemistry, and applied for the application of “honokiol-4-O-β-D-glucopyranoside in the preparation of drugs for the treatment of central nervous system diseases”. And two Chinese patents for the application of "honokiol derivatives in the preparation of drugs for the treatment of diseases of the central nervous system". (Reporter Zhao Hanbin correspondent Yang Tonghua)

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