New medical application of baicalein and its prodrugs

The technology of a prodrug, baicalein, applied in the field of medicine, can solve the problem of not finding the application of baicalein, and achieve the effects of good prospects, economic benefits, controllable costs, and convenient sources

Inactive Publication Date: 2015-05-20
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The application of baicalein in relieving delayed diarrhea caused by chemotherapeutic drugs such as irinotecan hydrochloride was not found before the disclosure of the present invention

Method used

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  • New medical application of baicalein and its prodrugs
  • New medical application of baicalein and its prodrugs
  • New medical application of baicalein and its prodrugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Baicalein or baicalein triethyl ester relieves irinotecan-induced diarrhea model experiment: 36 Balb / c mice were randomly divided into 6 groups: solvent control group, irinotecan model group, irinotecan + baicalein or baicalein Triethyl ester (30, 60, 120 mg / kg) group, baicalein or baicalein triethyl ester group, 6 rats in each group. The diarrhea model adopts intraperitoneal injection of irinotecan (100mg / kg / d) for 3 consecutive days. The delayed diarrhea appears on the 4th day and becomes the most serious on the 5th day. One day before irinotecan injection, baicalein or baicalein triethyl ester was given by intragastric administration (twice a day). The diarrhea status of the mice in each group was observed separately, and the mice were killed on the 6th day, and the intestinal tissue was collected, and the tissue section was stained for examination.

[0033] (1) Evaluation of diarrhea in mice

[0034] Record the diarrhea situation of the mice in each group on the 4...

Embodiment 2

[0044] Baicalein glucuronide conjugate relieves the diarrhea model experiment caused by cisplatin: 36 Balb / c mice were randomly divided into 6 groups: solvent control group, cisplatin model group, cisplatin + baicalein glucuronide conjugate (40 , 80, 120mg / kg) group, baicalein glucuronide group, 6 rats in each group. Diarrhea model adopts intraperitoneal injection of cisplatin (10mg / kg / d) for 3 consecutive days. Delayed diarrhea appears on the 4th day and is most severe on the 5th day. One day before the injection of cisplatin, baicalein glucuronide was given by intragastric administration (twice a day). The diarrhea status of the mice in each group was observed separately, and the mice were killed on the 6th day, and the intestinal tissue was collected, and the tissue section was stained for inspection.

[0045] (1) Evaluation of diarrhea in mice

[0046] Record the diarrhea situation of the mice in each group on the 4th and 5th day after the injection of cisplatin, observe...

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Abstract

The invention provides new medical application of baicalein and its prodrugs, i.e. application of baicalein in easing delayed diarrhea caused by irinotecan hydrochloride (Irinotecan, CPT-11) and other clinical chemotherapy drugs. Baicalein shows very good attenuation effect on irinotecan hydrochloride caused mouse delayed diarrhea model. In terms of the therapeutic effect, by inhibiting glucuronosyl transferase (UGTs) and carboxylesterase (CES2) two drug metablic enzymes and inhibiting the expression of TNF-alpha, IL-1beta, IL-6 and other inflammatory factors, baicalein and its prodrugs can play a role of intestinal mucosa protection.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a new medical application of baicalein (Baicalein, B) and its prodrug. Background technique [0002] Clinically, many chemotherapeutic drugs are accompanied by serious gastrointestinal side effects, such as fatal delayed diarrhea. Among them, irinotecan hydrochloride and 5-fluorouracil are more common. Irinotecan is a prodrug of camptothecin derivative SN-38, which is widely used in the treatment of solid tumors such as colorectal cancer. It is activated into SN-38 by carboxylesterase in vivo to exert anti-tumor activity. However, the drug is accompanied by serious adverse reactions, mainly including: neutropenia and delayed diarrhea. In particular, the incidence of delayed diarrhea is about 60-87%, of which grade 3 / 4 severe diarrhea accounts for about 20-39%. [0003] At present, the main treatment for diarrhea caused by irinotecan is to give loperamide (imodium...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P1/12
Inventor 杨凌刘兆明葛广波王平
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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