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Application of novobiocin in preparation of drug with function of inhibiting TRPV1 (transient receptor potential cation channel, subfamily V, member 1) expression and transfer

A novobiocin and functional technology, which is used in the field of novobiocin to prepare drugs that inhibit the expression and transport function of TRPV1, and can solve the problems that no research has confirmed the interaction between novobiocin and capsaicin.

Inactive Publication Date: 2018-08-03
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, no research has yet confirmed the interaction between novobiocin and capsaicin

Method used

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  • Application of novobiocin in preparation of drug with function of inhibiting TRPV1 (transient receptor potential cation channel, subfamily V, member 1) expression and transfer
  • Application of novobiocin in preparation of drug with function of inhibiting TRPV1 (transient receptor potential cation channel, subfamily V, member 1) expression and transfer
  • Application of novobiocin in preparation of drug with function of inhibiting TRPV1 (transient receptor potential cation channel, subfamily V, member 1) expression and transfer

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Male SD rats, with a body weight within the range of 250±20g, fasted for 16-18h in advance, fasted without water, and injected intraperitoneally with 3% pentobarbital sodium (12mL·Kg -1 ) anesthetized, cut the abdomen 2.5 cm along the midline of the abdomen, removed 5 cm from the top of the small intestine, and then used the next 10 cm of the small intestine as the jejunum, and the last 10 cm as the ileum. The first 2 cm of the large intestine was removed and the next 6 cm was taken as the colon. Gently wash them with normal saline respectively, place them in a mixed gas (95% O 2 :5%CO 2 ) in ice-bathed Hepes-Tris buffer. Cut 3-4cm of the jejunum intestine, quickly peel off the serosa layer on the serosa side, ensure the operation on ice, and then fix the intestinal mucosa on the diffusion cell, the effective area of ​​the diffusion chamber is 1.78cm 2, The ileum and colon use the same method of operation as the jejunum. Add 7mL test drug solution in the diffusion c...

Embodiment 2

[0029] Male SD rats, with a body weight within the range of 250±20g, fasted for 16-18h in advance, fasted without water, and injected intraperitoneally with 3% pentobarbital sodium (12mL·Kg -1 ) anesthetized, cut the abdomen 2.5 cm along the midline of the abdomen, removed 5 cm from the top of the small intestine, and then used the next 10 cm of the small intestine as the jejunum, and the last 10 cm as the ileum. The first 2 cm of the large intestine was removed and the next 6 cm was taken as the colon. Gently wash them with normal saline respectively, place them in a mixed gas (95% O 2 :5%CO 2 ) in ice-bathed Hepes-Tris buffer. Cut 3-4cm of the jejunum intestine, quickly peel off the serosa layer on the serosa side, ensure the operation on ice, and then fix the intestinal mucosa on the diffusion cell, the effective area of ​​the diffusion chamber is 1.78cm 2 , The ileum and colon use the same method of operation as the jejunum. Add 7mL test drug solution in the diffusion ...

Embodiment 3

[0032] Male SD rats, whose body weight is within the range of 250±20g, were randomly divided into 8 groups, with 4 rats in each group. 10 μM ruthenium red and saline. According to 5mL·kg -1 The test solution of the corresponding concentration was given by intragastric administration twice a day for 14 consecutive days. Rats were sacrificed after gavage on the 15th day, and the jejunum, ileum, and colon were isolated for mRNA and protein extraction and subsequent analysis of TRPV1 in the tissue, respectively.

[0033] RT-PCR was used to measure the mRNA expression of TRPV1. Using the RNA isolation kit (Takara Shuzo, Kyoto, Japan), the total RNA in cells and tissues was extracted and its concentration was determined according to the instructions. then follow Premix Ex Taq TM Reverse transcription was performed according to the instructions of II (Takara Shuzo, Kyoto, Japan). The sequences are as follows: TRPV1 is 5'-CACAGAGTGGACCCAGATACG-3' and 5'-CACTCGAGATAGACATGCCACC-3...

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Abstract

The invention relates to an application of novobiocin in preparation of a drug with a function of inhibiting TRPV1 (transient receptor potential cation channel, subfamily V, member 1) expression and transfer. With overexpression TRPV1 cells and mice taken as study models, it is found that 5-50 mu M novobiocin can inhibit the penetration amount of capsaicin passing by intestinal mucosa in a concentration-dependent manner and also can have an inhibition function on TRPV1 protein and mRNA expression on rat intestinal mucosa tissue. In the overexpression TRPV1 cell penetration model, the novobiocin also reduces the TRPV1 expression capability in a concentration-dependent manner and reduces the accumulation function of capsaicin in overexpression cells. In an in-vivo experiment, the inhibitionfunction of the novobiocin on TRPV1 is definitely confirmed. The novobiocin is a novel TRPV1 inhibitor, the pharmacologic action of the novobiocin for inhibiting TRPV1 expression is found for the first time, and the novobiocin can also affect the transfer capability of a TRPV1 channel.

Description

technical field [0001] The invention belongs to the field of medicaments, and relates to a new use of novobiocin, in particular to the use of novobiocin for preparing a medicine for inhibiting the expression and transport function of TRPV1 (transient voltage receptor cation channel subclass V member 1). Background technique [0002] Novobiocin is a coumarin antibiotic that has a good inhibitory effect on DNA gyrase. Because it has an inhibitory effect on BCRP, it can be used in combination with anticancer drugs regulated by BCRP to reverse the resistance of anticancer drugs. Medicinal properties. Novobiocin can treat a variety of Gram-positive infections such as drug-resistant Staphylococcus aureus and Streptococcus pneumoniae, and has anti-infective properties. In the course of daily medication, there are often reminders to avoid taking it with spicy food (more capsaicin-containing). Studies have confirmed that the simultaneous use of certain antibiotics and capsaicin wil...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P1/00
CPCA61K31/7048A61P1/00
Inventor 李国锋梁倩莹赵博欣张庆任非王春霞
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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