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Application of piperine in preparation of agonist of human bitter receptor 14 subtype

The technology of a bitter receptor and piperine is applied in the field of application of piperine in the preparation of an agonist of the human bitter receptor 14 subtype, which can solve the problems of no piperine and other problems, and achieve the purpose of suppressing appetite, promoting secretion, Improve the effect of metabolic diseases

Active Publication Date: 2021-12-17
XUZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, piperine has not been reported as a bitter taste receptor 14 agonist

Method used

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  • Application of piperine in preparation of agonist of human bitter receptor 14 subtype
  • Application of piperine in preparation of agonist of human bitter receptor 14 subtype
  • Application of piperine in preparation of agonist of human bitter receptor 14 subtype

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Effects of piperine and flufenamic acid on intracellular calcium mobilization and GLP-1 secretion in Caco-2 cells

[0024] 1 Materials and methods

[0025] 1.1 Cell lines

[0026] Caco-2 cells (FH0029) were purchased from Shanghai Fuheng Biotechnology Co., Ltd.

[0027]1.2 Drugs and main reagents

[0028] 1.2.1 Drugs: piperine (purity>98%) was purchased from Chengdu Pusi Biotechnology Co., Ltd.; flufenamic acid (purity>99%) was purchased from Shanghai Yuanye Biotechnology Co., Ltd.

[0029] 1.2.2 Reagents: DMEM high-glucose medium (4.5g / L glucose) was purchased from Beijing Suo Laibao Technology Co., Ltd.; Trizol reagent (15596-026) was purchased from Invitrogen, USA; PrimeScript RT reagent Kit (Perfect Real Time) ( RR037A) and SYBR Premix Ex Taq II were purchased from Dalian TaKaRa Company; DNase / RNase-FreeH 2 O(T121-02) was purchased from Tiangen Biochemical Technology (Beijing) Co., Ltd.; CCK-8 kit was purchased from Shanghai Dongren Chemical Technolog...

Embodiment 2

[0070] Example 2: Effect of piperine on hTAS2R14 signaling pathway in Caco-2 cells

[0071] 1 Materials and methods

[0072]1.1 Cell Lines Example 1.

[0073] 1.2 Drugs and main reagents BCA protein analysis kit (23225) was purchased from Thermo-Scientific (Rockford, IL, USA); rabbit hTAS2R14 antibody (DF5159) was purchased from Affinity Antibody Company; rabbit PLCβ2 antibody (A8141) was purchased from ABclonal Antibody Company; Rabbit TRPM5 antibody (18027-1-AP) was purchased from Proteintech Antibody Company; rabbit β-actin (#AP0060) antibody was purchased from BioworldTechnology Antibody Company; goat anti-rabbit Dylight 594 Affinipure IgG (H+L) secondary antibody (#V926-32211) was purchased from From Li-Cor, Inc. (Lincoln, NE); others are the same as in Example 1.

[0074] 1.3 Method

[0075] 1.3.1 Grouping and administration: Same as Example 1.

[0076] 1.3.2 Determination of protein expression (Western blot method): the protein concentration of the cell homogenate s...

Embodiment 3

[0108] Example 3: Inhibition of the hTAS2R14 pathway in Caco-2 cells and the effect of its agonist piperine

[0109] 1 Materials and methods

[0110] 1.1 Cell Lines Example 1.

[0111] 1.2 Drugs and main reagents: Gallein (GC13945, purity>98%) was purchased from Glpbio Company of the United States; U73122 (T6243, purity=97.98%) was purchased from TargetMol Company of the United States; 6-methoxyflavone (6-methoxyflavone, 6-MF ,purity>98%) was purchased from Shanghai Yuanye Biotechnology Co., Ltd. Others are with embodiment 1, example 2.

[0112] 1.3 Method

[0113] 1.3.1 Grouping and administration: Caco-2 was routinely cultured in DMEM high-glucose medium containing 10% FBS and 1% double-antibody (penicillin and streptomycin) in 5% CO 2 , Cultured in a constant temperature incubator at 37°C. When the growth status is good, change to the serum-free medium to synchronize the cell cycle for 12 hours, divide into the Pip high concentration group (Pip-50), and the co-treatmen...

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Abstract

The invention relates to new use of piperine and application of the piperine in preparation of an agonist of a human bitter receptor 14 subtype (hTAS2R14). The piperine can be used for increasing an mRNA level and protein expression of the hTAS2R14 in enteroendocrine cell cells Caco-2, increasing protein expression of downstream phospholipase C beta 2 and transient receptor potential ion channel protein M5, and increasing mobilization of intracellular calcium, and then, the gene expression of a glucagon-like peptide 1 (GLP-1) precursor proglucagon and the secretion of the GLP-1 are improved. The hTAS2R14 agonist 6-methoxyflavone does not weaken the mobilization effect of the piperine on the intracellular calcium, but promotes the mobilization of the piperine on the intracellular calcium. A G beta gamma subunit inhibitor of the G protein coupled with the hTAS2R14 obviously weakens the secretion of the piperine to the GLP-1, and the phospholipase C beta 2 inhibitor obviously weakens the secretion of the piperine to the GLP-1. The research shows that the piperine is an efficient agonist of the hTAS2R14.

Description

[0001] The invention relates to the discovery of the action target of piperine. Piperine can activate human bitter taste receptor 14 subtype (hTAS2R14), and is a high-efficiency agonist of hTAS2R14. Specifically, piperine can activate digestive tract endocrine cells hTAS2R14, and can be used in the preparation of therapeutic and preventive drugs for diabetes and obesity. Background technique [0002] Taste strongly affects food preference and intake. The receptors for food or compounds in vertebrates are different taste receptors (taste receptors, TASRs), which were originally discovered in the taste buds of the oral cavity. Human taste receptors include two types, sweet taste receptors (hTAS1Rs) and bitter taste receptors (hTAS2Rs). hTAS2Rs are a class of G protein-coupled receptors (GPCRs), which consist of a hydrophobic seven-time transmembrane region, an extracellular short amino terminus, an intracellular carboxyl terminus, three extracellular loops and three intracellula...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4525A61P3/00A61P3/10A61P3/04A61P11/00
CPCA61K31/4525A61P3/00A61P3/10A61P3/04A61P11/00
Inventor 刘耀武黄婷婷
Owner XUZHOU MEDICAL UNIV
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