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Application of bakuchiol compound

A technology of bakuchiol and compound is applied in the application field of bakuchiol compound in the preparation of medicines, and can solve the problems of ineffectiveness of patients with psychotic neurological diseases, sexual dysfunction of patients, no curative effect, etc., and achieves good Market prospects, excellent efficacy

Inactive Publication Date: 2007-12-19
上海国联干细胞技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, studies have found that existing drugs have no effect on many patients with psychoneurological diseases. For example, clinical surveys have shown that more than 30% of patients with depression have no effect on existing drugs
In addition, some neurological drugs on the market have unbearable side effects. For example, SSRI drugs have selective effects on monoamine neurotransmitter receptors, which lead to side effects during treatment. The main adverse reactions are gastrointestinal disorders. Some patients have insomnia, anxiety, sexual dysfunction

Method used

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  • Application of bakuchiol compound
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  • Application of bakuchiol compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] The establishment of embodiment 1 in vitro screening model

[0053] The present invention relates to experimental methods of conventional molecular biology, which are widely known in the art and described in, for example, Molecular Cloning: a laboratory Manual 3rd edition, edited by Sambrook et al., Cold Spring Harbor laboratory Press, Clod Spring Harbor, N.Y. , 2001 and Current Protocols in Molecular Biology, method reference books edited by Ausubel etc. have detailed introductions. Establishment of activity screening cell lines targeting serotonin, norepinephrine, dopamine, and γ-aminobutyric acid four neurotransporters (5-HTT, NET, DAT, GAT-1). By cloning the full-length coding sequences of 5-HTT, NET, DAT, and GAT-1 of rats (the cDNA sequences are derived from GeneBank on the PnbMed website) into the pCDNA3 vector (Invitrogen, USA), transfection into Chinese hamsters by electroporation Ovary cell (CHO) cells were cultured in 1640 medium containing G418 after 48 hou...

Embodiment 2

[0054] Example 2 Determination of 13-hydroxybakuchiol selection specificity

[0055] S6, NET, D8, and GAT-1 cells were cultured in 48-well plates (Costar) until the plates were confluent (approximately 60,000 cells per well). Discard the culture medium, wash once with PBS, suck off the PBS solution, add 90ul HBS (10mM Hepes, 100mM NaCl, pH8.0) to each well, incubate at 25°C for 10 minutes, and add 10ul HBS reaction solution to each well. The experimental group and the positive control drug were added with 80ul HBS, 10ul of different concentrations of 13-hydroxybakuchiol (B310) and the positive control drug bupropion (BPR), and 10ul 3 H-labeled substrate (S6 uses 3 H-5-HT; NET adopted 3H-NE; D8 adopted 3 H-DA), 100 μM vitamin C and 100 μM parjiline. Incubate at 25°C for 20 minutes, wash three times with ice-bathed PBS solution, lyse with lysate for 60 minutes, absorb the lysate from each well, add it to 1.2ml scintillation fluid, and put it into a liquid scintillation count...

Embodiment 3

[0062] Example 3 Cytotoxicity test of 13-hydroxybakuchiol

[0063] CHO cells were cultured in 1640 medium (containing 10% calf serum). After the culture dish was overgrown, trypsinized, seeded in a 48-well cell plate, and continued to culture until the number of cells reached 10. 5 Left and right, respectively, were treated as follows: after the liquid was changed, 10 μl of control solution (HBS containing 1% DMSO) was added to the control group, and 10 μl of 13-hydroxybakuchiol with different concentrations were added to the drug groups with different doses, so that the final concentration was 1 mM respectively. , 0.1 mM and 0.01 mM. Continue culturing for 24 hours, and add MTT at the 20th hour to make the final concentration 0.8 mg / ml. After the reaction, the culture solution was sucked off, 100% DMSO was added, and incubated at 37° C. for 10 minutes. Transfer to a 96-well plate, and measure the OD value of each well with an enzyme label detector at a wavelength of 570 nm....

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Abstract

The present invention discloses the application of bakuchiol compound in preparing medicine for treating psychogenic diseases and neurogenic diseases. Extracorporeal experiment and animal experiment show that the bakuchiol compound can suppressing dopamine transport protein, noradrenalin transport protein and 5-hydroxy tryptamine transport protein selectively, and no influence on gamma-aminobutyric acid transport protein and L-glytamic acid transport protein, no cytotoxicity, and antidepressant effect higher than available antidepressant medicine amfebutamoe hydrochloride. Therefore, the bakuchiol compound has excellent marketability in preparing medicine for treating psychogenic diseases and neurogenic diseases.

Description

technical field [0001] The invention relates to a new application of bakuchiol compounds, in particular to the application of bakuchiol compounds in the preparation of medicines. technical background [0002] Mental and / or neurological diseases seriously affect the health of millions of people around the world. Depression is one of the mental diseases that are depressed, moody, pessimistic, negative, and can be accompanied by suicidal tendencies in severe cases. It is the most common mental disease that endangers human physical and mental health today, and its incidence accounts for about 11% of the world's population. . The annual report released by the World Health Organization not long ago shows that depression has now ranked fourth among the top ten diseases in the world. It is estimated that by 2020, it will be ranked second after cardiovascular disease and ahead of cancer, and become the second largest disease that endangers human health and shortens life expectancy. ...

Claims

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Application Information

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IPC IPC(8): A61K31/05A61K31/085A61P25/04A61P25/06A61P25/08A61P25/14A61P25/18A61P25/20A61P25/22A61P25/24A61P3/04
CPCA61K31/05A61P3/04A61P9/10A61P15/12A61P25/00A61P25/04A61P25/06A61P25/08A61P25/14A61P25/16A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P25/30
Inventor 郭礼和赵刚王雪松
Owner 上海国联干细胞技术有限公司
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