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Application of abietane tricyclic diterpene active compound in preparation of antitumor drugs

An anti-tumor drug and tricyclic diterpene technology, which is applied in anti-tumor drugs, drug combinations, inorganic active ingredients, etc., can solve the problems of tumor cell apoptosis and chemotherapeutic drug sensitization.

Active Publication Date: 2019-11-08
浙江中医药大学附属第一医院 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006]But so far, there are no research reports on abietane tricyclic diterpene active compounds inhibiting STAT3 transcription activity, inducing tumor cell apoptosis and chemotherapeutic drug sensitization

Method used

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  • Application of abietane tricyclic diterpene active compound in preparation of antitumor drugs
  • Application of abietane tricyclic diterpene active compound in preparation of antitumor drugs
  • Application of abietane tricyclic diterpene active compound in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Example 1: Separation and extraction of dehydrotanshinone, 1-oxytanshinone and 4-methylenetanshinone

[0062] For the extraction process, refer to the patent document CN 103845314 A.

Embodiment 2

[0063] Example 2: Test of dehydrotanshinone on STAT3 transcriptional activity

[0064] Experimental method: Human 293T cells were treated with DMEM containing 10% FBS (GIBCO) at 37°C and 5% CO 2 nourish. Lentivirus STAT3 Luciferase Reporter STAT3-Luc reporter gene lentiviral particles were used to infect 293T cells to establish a STAT3-Luc stably transfected cell line. After dehydrotanshinone (0, 2.5 μM, 5 μM, 10 μM) was treated for 8 hours, the cells were collected and used The dual-luciferase reporter gene assay kit was used to determine the level of firefly luciferase according to the protocol described by the manufacturer (Promega).

[0065] The results of the luciferase reporter gene detection showed that dehydrotanshinone had an inhibitory effect on the transcriptional activity of STAT3, and 2.5 μM, 5 μM, and 10 μM dehydrotanshinone acted on human embryonic kidney cells stably transfected with the luciferase reporter gene plasmid The activities of STAT3 after 293T we...

Embodiment 3

[0066] Example 3: 1-oxotanshinone test for STAT3 transcriptional activity

[0067] Experimental method is the same as embodiment 2.

[0068] The results of the luciferase reporter gene detection showed that 1-oxotanshinone had an inhibitory effect on the transcriptional activity of STAT3, and 2.5 μM, 5 μM, and 10 μM 1-oxotanshinone acted on human embryonic kidney cells stably transfected with the luciferase reporter gene plasmid The activities of STAT3 after 293T were 74.2%, 38.2%, and 20.5%, respectively. The inhibitory effect of 1-oxytanshinone on STAT3 activity was concentration-dependent.

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Abstract

The invention discloses an application of an abietane tricyclic diterpene active compound in preparation of antitumor drugs. The abietane tricyclic diterpene active compound is selected from 1,2-didehydromiltirone, 1-oxomiltirone or 4-methylenemiltirone. Tests find that: the abietane tricyclic diterpene active compound has a remarkable inhibition effect on the transcriptional activity of STAT3, can remarkably inhibit proliferation of tumor cells too, induce apoptosis of the tumor cells and remarkably increase the expression level of tumor cell apoptosis pathway marker protein shear-type caspase3 and PARP, and can be used for preparing anti-tumor drugs.

Description

technical field [0001] The invention relates to the application of an abietane tricyclic diterpene active compound in the field of medicine, in particular to the application of a class of abietane tricyclic diterpene active compound in the preparation of antitumor drugs. Background technique [0002] Malignant tumors and their complications seriously endanger human life and health. In recent years, the morbidity and mortality of most malignant tumors such as lung cancer, colorectal cancer, gastric cancer, pancreatic cancer, and leukemia have been on the rise. Surgical treatment is the first choice for cancer patients, but most cancer patients are already in the middle and advanced stages and lose the opportunity for surgery. At the same time, some patients with early stage limited surgically resectable tumors are often accompanied by postoperative recurrence and metastasis. Chemotherapy and radiotherapy are the main means of current tumor treatment. Although chemotherapy and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61K31/519A61K33/243A61K31/704A61P35/00A61P35/02
CPCA61K31/122A61K31/519A61K33/243A61K31/704A61P35/00A61P35/02A61K2300/00
Inventor 陈喆尹一飞马忠俊王亿平刘培戴春艳王曦葛宇清
Owner 浙江中医药大学附属第一医院