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Application of protoopioid alkaloids in the preparation of medicines for inhibiting p-gp

A proto-opioid and alkaloid technology, applied in the field of pharmaceutical research, can solve the problem that pro-opioid alkaloids inhibit P-gp activity, etc.

Active Publication Date: 2016-12-28
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there has been no report on the inhibition of P-gp activity by pro-opioid alkaloids

Method used

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  • Application of protoopioid alkaloids in the preparation of medicines for inhibiting p-gp
  • Application of protoopioid alkaloids in the preparation of medicines for inhibiting p-gp
  • Application of protoopioid alkaloids in the preparation of medicines for inhibiting p-gp

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1 Inhibition of Calcein-AM Efflux Transport by Protopine

[0050] Calcein-AM is a cytoplasmic fluorescent marker that is not itself fluorescent. The methyl acetate of Calcein-AM has a high lipophilicity, making it permeable to the cell membrane, and after penetrating into the cell, it is catalyzed by the esterase in the cell to remove the AM group, and the water-soluble Calcein (calcein) produced becomes P The substrate of -gp can emit green fluorescent substance under the excitation light of 494nm.

[0051] P-gp is an energy (ATP)-dependent membrane protein encoded by the multidrug resistance protein 1 (MDR1) gene, which can actively transport exogenous substances such as drugs out of cells by using the energy released by ATP hydrolysis extracellular, resulting in multidrug resistance. Since Calcein is the substrate of P-gp, P-gp can actively transport Calcein from the inside of the cell to the outside of the cell. When the function of P-gp is inhibited, t...

Embodiment 2

[0058] Example 2 Inhibition of Rho123 efflux transport by protopine

[0059] Experimental Materials and Instruments

[0060] The MDCK and MDR1-MDCK cell lines used in this experiment were donated by the School of Pharmacy, Zhejiang University. Rhodamine 123 (Rho123) was purchased from Sigma Company (USA); the original opioid was purchased from Tianjin Institute of Drug Control; DMEM medium was purchased from Hyclone Company of the United States; G418 was purchased from Sangon Bioengineering (Shanghai) Co., Ltd.; Hank's balanced salt powder, trypsin (0.25% Trypsin-0.02% EDTA), non-essential amino acids, and DMSO were purchased from Sigma Company in the United States; fetal bovine serum was purchased from GIBCO Company in the United States; penicillin-streptomycin was purchased from Biologcal Industries.

[0061] FlexStation ELISA (Molecular Devices).

[0062] experimental method

[0063] MDCK-MDR1 / MDCK cells in 8×10 4 piece / cm 2 The density was planted on the Millicell p...

Embodiment 3

[0065] Example 3 Antitumor sensitization effect of proopiate on paclitaxel

[0066] Experimental Materials and Instruments

[0067] The MCF-7 and MCF-7 / ADR cell lines used in this experiment were purchased from the Tumor Cell Bank of the Chinese Academy of Medical Sciences. Paclitaxel was purchased from China Food and Drug Inspection Institute, and original opioid was purchased from Tianjin Drug Inspection Institute; DMEM medium, trypsin (0.25% Trypsin-0.02% EDTA), DMSO, and XTT were purchased from Sigma Company in the United States; fetal bovine serum, purchased from In the United States GIBCO company; penicillin - streptomycin, purchased from Biologcal Industries.

[0068] FlexStation ELISA (Molecular Devices)

[0069] experimental method

[0070] 1. MCF-7 cells in 4 x 10 4 piece / cm 2 The density was planted in a 96-well plate, the medium was changed every 24 hours, cultured for 72 hours, and washed twice with PBS. Divided into three groups: 1) Control group, only ad...

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Abstract

The present invention provides proto-opioid alkaloids and pharmaceutically acceptable salts, solvates, polymorphs, enantiomers or racemic mixture salts, polymorphs, optical isomers, racemates, and Application of Corydalis Corydalis and its extracts containing proto-opioid alkaloids, Xia Wu and its extracts, Boluohui and its extracts in the preparation of drugs for inhibiting P-gp function. The present invention also provides proto-opioid alkaloids and pharmaceutically acceptable salts, solvates, polymorphs, enantiomers or racemic mixture salts, polymorphs, optical isomers, and racemates, And the application of Corydalis Corydalis and its extracts containing original opioid alkaloids, Xia Wu and its extracts, Boluohui and its extracts in the preparation of drugs for adjuvant tumor treatment, the adjuvant tumor treatment refers to the reversal of the combination of P ‑Gp high expression related tumor multidrug resistance, synergistic antitumor drugs.

Description

technical field [0001] The invention belongs to the field of pharmaceutical research, and in particular relates to a new medical application of the original opioid alkaloid as a P-gp specific inhibitor. Background technique [0002] P-glycoprotein (P-glycoprotein, P-gp) is a glycoprotein encoded and expressed by the multidrug resistance (MDR) gene. As an efflux transporter widely distributed in body tissues, it affects the absorption, distribution, metabolism and excretion of drugs in the human body. The biological essence of P-gp efflux is that the cells repel the cytotoxic substances (or drugs) that may be encountered in the living environment, and reduce the accumulation of the toxic substances (or drugs) in the cells to achieve self-protection. The cross-resistance of tumor cells to a variety of chemotherapeutic drugs is called tumor multidrug resistance. Tumor multidrug resistance is a kind of MDR, which is an important reason for the failure of tumor chemotherapy. T...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/395A61K36/66A61P35/00
Inventor 何新邢海艳翟毅然
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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