New use of methyl liensinine

A technology for the use of liensinine, which is applied in the field of new uses of liensinine, and can solve problems such as reports that there is no report on the effect of liensinine

Active Publication Date: 2010-10-20
INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] After searching the published literature of PubMed, CNKI, etc., there is no report that liensinine has an effect on TRPM8 and TRPV1

Method used

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  • New use of methyl liensinine
  • New use of methyl liensinine
  • New use of methyl liensinine

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0018] Preparation of rat dorsal root ganglion cells (DRG): DRG cells are the main afferent neurons in the peripheral nervous system of mammals and humans, and express a variety of TRP receptor channel proteins. It plays an important role in repair, transmission of noxious stimuli, pathological development and physiological processes. In order to investigate the effect of nexinine on TRPM8, rats (SD strain) suckling mice (within 5 days after birth) were selected, and the dorsal root ganglia on both sides of the spine were removed under aseptic conditions, and the remaining tissues were removed. Digest with collagenase and trypsin, centrifuge, discard the digestion solution, pipette it into a single cell suspension in conventional culture medium, count and adjust to contain 10 cells per ml 5 neurons, cultured in a culture dish pre-coated with laminin, etc., at 37°C, 5% CO 2 After culturing for 48 hours, camptothecin was used to inhibit the proliferation of other miscellaneous ...

Embodiment 1

[0025] Example 1: Under normal ambient temperature (37° C.), the effect of liensinine on the expression of TRPM8 mRNA in DRG cells

[0026] In the purified DRG cell culture, add three different concentrations of the test compound, at 37 ° C, 5% CO 2 Cultivate for 24 hours, extract total RNA immediately after stopping the cultivation, set TRPM8 agonist menthol (comparison drug group) simultaneously, no normal culture fluid (normal control group) of test article, carry out fluorescence quantitative PCR amplification and TRPM8mRNA determination. The results are shown in Table 1. Nesinine promotes the expression of TRPM8mRNA, which is related to drug concentration (correlation coefficient 0.98), greater than 5 μmol L -1 (i.e. 10 μmol·L -1 ) drug concentration, the promotion effect is significant.

[0027] Table 1: Effects of traditional Chinese medicine ingredients on TRPM8mRNA expression at 37°C (x±s) (n=8)

[0028]

Embodiment 2

[0029] Example 2: Under high temperature (39° C.) ambient temperature conditions, the effect of methyl-liensinine on the expression of TRPM8mRNA in DRG cells

[0030] It has been proved by experiments that a high temperature environment (such as 39) can inhibit the expression of TRPM8. In the purified DRG cell culture, three different concentrations of the test compound were added respectively, at 37°C, 5% CO 2 Incubate for 23 hours, then at 39°C, 5% CO 2 Cultivate for 1 hour, stop culturing, extract total RNA immediately, set TRPM8 agonist menthol (control drug group), or normal culture solution without test substance (normal control group) at the same time, carry out fluorescence quantitative PCR amplification and TRPM8mRNA determination . The results are shown in Table 2. It was not found that liensinine could up-regulate the expression of TRPM8mRNA.

[0031] Table 2: Effects of traditional Chinese medicine ingredients on TRPM8mRNA expression at 39°C (x±s) (n=8)

[0032...

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Abstract

The invention discloses a new use of methyl liensinine. Methyl liensinine respectively regulates M8 and V1 subtype transient receptor potential ion channels (TRPM8 and TRPV1 for short) of mammal including human, so as to prepare medicine for treating related diseases joined by the ion channels (such as cold hyperalgesia, parkinsonism, nociceptive bladder syndrome, chronic obstructive lung diseaseand tumours of skin, prostate, breast, lung and colon). The action strength of methyl liensinine of the invention is higher than that of menthol.

Description

technical field [0001] The invention relates to a new application of the compound liensinine derived from traditional Chinese medicine. Specifically, the present invention relates to the preparation of the compound of nexinine in the preparation of the M8 and V1 subtype of Transient Receptor Potential ion channel (M8 and V1 subtype of Transient Receptor Potential ion channel) (hereinafter referred to as TRPM8 and TRPV1) and the preparation of TRPM8 and TRPV1 Uses in drugs involved in relevant pathological processes and diseases. Background technique [0002] Transient receptor ion channel (TRP) is a type of transmembrane structure found on the cell membrane or intracellular organelle membrane in mammalian and human cells in recent years. , opening and closing calcium ion channels, allowing calcium ions from extracellular or intracellular calcium pools to enter or exit the cytoplasm, modifying cell functions through intracellular signal transduction pathways, and participati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4725A61P11/00A61P25/16A61P13/10A61P37/08A61P35/00A61P25/06A61P29/00A61P1/00A61P1/18A61P19/02A61P11/14A61P11/06A61P11/02A61P3/10A61P21/04A61P25/18
CPCA61K9/0019A61K47/44A61K9/2009A61K31/4709A61K9/10A61P1/00A61P1/04A61P1/18A61P3/10A61P11/00A61P11/02A61P11/04A61P11/06A61P11/14A61P13/10A61P19/02A61P21/04A61P25/00A61P25/06A61P25/16A61P25/18A61P29/00A61P35/00A61P35/04A61P37/08
Inventor 姜廷良隋峰霍海如李兰芳郭淑英
Owner INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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