Application of tanshinone compound used as specific inhibitor for CYP1 family

Technology of a compound, tanshinone, in the application field of vitality

Inactive Publication Date: 2009-09-02
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no research report on selectively inhibiting the activity of CYP1B1 subtype enzymes and reversing the expression of CYP1 enzymes induced by B[a]p (benzo[a]pyrene)

Method used

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  • Application of tanshinone compound used as specific inhibitor for CYP1 family
  • Application of tanshinone compound used as specific inhibitor for CYP1 family
  • Application of tanshinone compound used as specific inhibitor for CYP1 family

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Recombinant enzyme experiments were used to investigate the effects of tanshinone components on CYP1A1 metabolism (calculation of IC50 value).

[0018] Experimental materials and instruments:

[0019] The human recombinant enzyme CYP1A1 expressed by cDNA was purchased from gentest company, ETRF (7-ethoxyresorufin), NADP, 6-phosphate glucose, and 6-phosphate glucose dehydrogenase were all purchased from Sigma company, tanshinone I (tanshinone I), tanshinone IIA (tanshinone II A), cryptotanshinone (cryptotanshinone), dihydrotanshinone I (dihydrotanshinone I) standard products were all purchased from China Institute for the Control of Pharmaceutical and Biological Products, and the instrument used Tecan Safire 2 High Throughput Reader.

[0020] experimental method:

[0021] experimental method:

[0022] 1. In a 0.2ml incubation system, contain 0.25pmol CYP1A1, 1.3mM NADP, 3.3mM glucose-6-phosphate, 0.4U / ml glucose-6-phosphate dehydrogenase, 3.3mM magnesium chloride and ...

Embodiment 2

[0026] Recombinant enzyme experiments were used to investigate the effects of tanshinone components on CYP1A2 metabolism (calculation of IC50 value).

[0027] Experimental materials and instruments:

[0028] The human recombinant enzyme CYP1A2 expressed by cDNA was purchased from gentest company, ETRF (7-ethoxyresorufin), NADP, 6-phosphate glucose, and 6-phosphate glucose dehydrogenase were all purchased from Sigma company, tanshinone I (tanshinone I), tanshinone IIA (tanshinone II A), cryptotanshinone (cryptotanshinone), dihydrotanshinone I (dihydrotanshinone I) standard products were all purchased from China Institute for the Control of Pharmaceutical and Biological Products, and the instrument used Tecan Safire 2 High Throughput Reader.

[0029] experimental method:

[0030] 1. In a 0.2ml incubation system, contain 2pmol CYP1A2, 1.3mM NADP, 3.3mM 6-phosphate glucose, 0.4U / ml 6-phosphate glucose dehydrogenase, 3.3mM magnesium chloride and 0.2μM ETRF. The reaction system was...

Embodiment 3

[0034] Recombinant enzyme experiments were used to investigate the effects of tanshinone components on CYP1B1 metabolism (calculation of IC50 value).

[0035] Experimental materials and instruments:

[0036] The human recombinant enzyme CYP1B1 expressed in cDNA was purchased from gentest company, ETRF (7-ethoxyresorufin), NADP, 6-phosphorus A (tanshinone II A), cryptotanshinone (cryptotanshinone), and dihydrotanshinone I (dihydrotanshinone I) standard products were purchased from China National Institute for the Control of Pharmaceutical and Biological Products, the instrument adopts Tecan Safire 2 High Throughput Reader.

[0037] experimental method:

[0038] 1. In a 0.2ml incubation system, contain 1pmol CYP1B1, 1.3mM NADP, 3.3mM 6-phosphate glucose, 0.4U / ml 6-phosphate glucose dehydrogenase, 3.3mM magnesium chloride and 0.05μM ETRF. The reaction system was mixed in 100mM PBS.

[0039] 2. Add different concentrations of tanshinone (0~10000nM) to the reaction system, and ...

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Abstract

The invention relates to the field of natural medicaments, in particular to a diterpenes compound in a radix salviae miltiorrhizae extract, mainly relates to the expression of a tanshinone compound in a reversal benzoapyrene-induced CYP1 enzyme, as well as application in the direct inhibition of the CYP1 enzyme activity. The invention discloses new pharmacological application of four types of tanshinones including tanshinone I, tanshinone II A, cryptotanshinone and dihydrotanshinone I, namely the four tanshinones not only can directly inhibit the activities of various subtype enzymes in the CYP1 family but also can reverse the up-regulation of a benzoapyrene-induced CYP1 function in Hep-G2 cells. The tanshinone compound has the development application prospect that the tanshinone compound can be developed into a supplementary drug for the treatment of cancer as a multi-drug resistant reversal agent and an anti-cancer health care product.

Description

technical field [0001] The invention relates to the field of natural medicines, in particular to the application of a compound (tanshinone) in salvia miltiorrhiza extract in reversing the expression of CYP1 enzyme induced by B[a]p and directly inhibiting the activity of CYP1 enzyme. Background technique [0002] With the development of the economy and the aggravation of environmental pollution, the incidence of malignant tumors has been increasing year by year. It has been clinically defined as a common disease and frequently-occurring disease, which seriously threatens human health. Cytochrome P450 (CYP) is a superfamily enzyme system composed of structurally and functionally related gene superfamily (superfamily) encoded isoenzymes, involved in the biotransformation of many endogenous and exogenous substances, in the regulation of the body It plays a very important role in the interaction with the external environment and in maintaining the homeostasis of the internal envi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61P35/00
Inventor 张荣孙建国王广基吴晓兰周芳艾华彭英尚丽丽
Owner CHINA PHARM UNIV
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