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Application of Tipranavir in anti-cancer drug and anti-cancer drug

A tipranavir, anti-cancer technology, applied in the field of medicine, can solve the problems of poor cancer suppression effect and achieve the effect of delaying the speed

Active Publication Date: 2016-07-20
CHONGQING UNIV OF TECH +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] In view of the above-mentioned deficiencies in the prior art, the technical problem to be solved in the present invention is: how to make up for the deficiency of the poor inhibitory effect of drugs on cancer in the prior art, and provide the new application of Tipranavir Tipranavir, that is, to cancer cells growth inhibition and induction of apoptosis, and further provide the application of tipranavir in the preparation of cancer drugs and anti-cancer drugs

Method used

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  • Application of Tipranavir in anti-cancer drug and anti-cancer drug
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  • Application of Tipranavir in anti-cancer drug and anti-cancer drug

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Embodiment Construction

[0070] The present invention will be described in further detail below in conjunction with accompanying drawing and specific embodiment, and the raw material used in the embodiment is common commercially available unless otherwise specified.

[0071] 1. Virtual Screening

[0072] Using the suflex-docking module in SYBYL2.0 to analyze the active site of Tipranavir (A1, the binding site of the endogenous inhibitor nicotinamide) ( figure 1 and image 3 ) and active site two (A2, the binding site of the exogenous inhibitor EX527) ( figure 2 and Figure 4 ) combination mode and amino acid residues.

[0073] For active site one and two ( Figure 5 ) after virtual screening, the top 100 molecules with the highest docking scores were obtained (deleting 24 identical molecules with different conformations), the results are shown in Table 1, and 932 is the screened SIRT1 inhibitor Tipranavir.

[0074] Table 1 Virtual Screening Results

[0075]

[0076]

[0077]

[0078] C...

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Abstract

The invention discloses application of Tipranavir in an anti-cancer drug and an anti-cancer drug , particularly relates to application of Tipranavir in the anti-cancer drug and preparation of the anti-cancer drug, and provides a Tipranavir-containing anti-cancer drug. The Tipranavir serves as a main active ingredient for resisting cancer. According to the application of the Tipranavir in the anti-cancer drug and the anti-cancer drug, molecular Tipranavir which has the highest active pocket matching degree with an SIRT1 (Silentinformation regulator 1) is selected by utilizing a computer virtual screening method; the anti-cancer effect of the Tipranavir is researched further through a cell experiment; after 72-hour treatment of the Tipranavir, the proliferation inhibition rate of breast cancer cells reaches 82.10 percent, and through 48-hour treatment of the Tipranavir, the proliferation inhibition rate of hepatoma carcinoma cells reaches 88.83 percent, so that excellent technical effects are achieved.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to the application of tipranavir (Tipranavir), in particular to the application of tipranavir in anticancer drugs and anticancer drugs. Background technique [0002] Cancer, namely malignant tumor, is a major disease that seriously endangers human life. The treatment of cancer has received widespread attention from society. Breast cancer is the most common cancer among women in China, as in most other countries. Every year, the number of new cases and deaths of breast cancer in China account for 12.2% and 9.6% of the world's respectively. Since the 1990s, the incidence of breast cancer in China has grown at more than twice the global rate, especially in urban areas. Currently, breast cancer is the most common cancer among Chinese women. Chemotherapy is one of the three basic means of breast cancer treatment. Although many advances have been made in breast cancer chemotherapy, howe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4433A61K31/427A61P35/00A61P31/18
CPCA61K9/2059A61K31/427A61K31/4433A61K2300/00
Inventor 林治华丁雪垒郭波朱波王锐林勇胡勇王远强舒茂
Owner CHONGQING UNIV OF TECH
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