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Tylophora ovata base analogs with anti-tumor activity and preparation method and use thereof

A technology of anti-tumor activity and seraphine, which is applied in the direction of anti-tumor drugs, organic active ingredients, medical preparations containing active ingredients, etc., can solve the problems of low alkaloid content, few plant resources, poor stability, etc., and achieve Simple synthetic route, significant inhibitory effect, low cost effect

Inactive Publication Date: 2010-12-01
NANJING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, such alkaloid plants have few resources, low alkaloid content, and problems such as poor stability and toxic side effects, resulting in failure to obtain better development and application. Pharmacists and synthetic chemists are committed to solving the stability of this type of compound. Researches on properties without loss of activity or improvement of activity and reduction of toxicity, many total synthesis works have been completed

Method used

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  • Tylophora ovata base analogs with anti-tumor activity and preparation method and use thereof
  • Tylophora ovata base analogs with anti-tumor activity and preparation method and use thereof
  • Tylophora ovata base analogs with anti-tumor activity and preparation method and use thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0024] Inhibition of TDH on the proliferation of human cervical cancer cell line Hela

[0025] Get the human cervical cancer cell line Hela in the logarithmic growth phase, digest with trypsin, centrifuge at 1000r / min for 5min, count with trypan blue staining (percentage of living cells > 95%), and use 5×10 4 Cell density per ml was seeded in 96-well culture plate, 180 μl / well, cultivated for 24 hours, and added different concentrations of 2,3-dimethoxy-6,7-methylenedioxy-phenanthrene-[9,10- b]-indolizidine (TDH) (the drug is dissolved in DMSO, and the final concentration of DMSO in the system 50 The value is 4.05±0.22, which is only 50% of that of seraphine.

Embodiment 2

[0027] Inhibition of BMPI on the proliferation of human lung adenocarcinoma cell line A549

[0028] Get the human lung adenocarcinoma cell line A549 in the logarithmic growth phase, digest with trypsin, centrifuge at 1000r / min for 5min, count with trypan blue staining (percentage of viable cells > 95%), and measure 5×10 4 Cell density per ml was inoculated in 96-well culture plate, 180 μl / well, cultivated for 24 hours, and added different concentrations of 2,3,6,7-dimethylenedioxy-phenanthrene-[9,10-b]-indole Dorisidine (BMPI) (the drug is dissolved in DMSO, and the final concentration of DMSO in the system <0.1%, this concentration has no effect on cell growth), so that the final mass concentration is 0.25, 0.5, 1.0, 2.5, 5.0 μg / ml. There are 5 replicate wells in each group. At the same time, a solvent control group, namely a negative control group (containing DMSO required to dissolve the drug at the maximum concentration), and a zeroing group (containing an equal volume o...

Embodiment 3

[0030] Effects of BMPI on A549 Cell Division and Colony Formation Ability

[0031] Take A549 cells in the logarithmic growth phase, digest with 0.5% trypsin and blow into single cells, suspend the cells in RPMI-1640 culture medium containing 10% fetal bovine serum, count, and dilute the cell concentration with culture medium to 1 ×10 3 cells / ml, seeded in a six-well plate, 1×10 per well 3 cells, the total volume in the well is 2ml, shake well and place in CO 2In the incubator, incubate at 37°C for 24 hours, remove the culture medium, add BMPI (dissolved in DMSO, the final concentration of DMSO is less than 0.1%), the final concentration is 0.25, 0.5, 1.0, 2.5, 5.0 μg / ml. At the same time, a negative control group was set up. Shake well and incubate in a carbon dioxide incubator for 24 hours, remove the liquid medicine, replace with fresh culture medium, and continue to cultivate for 10 days. Discard the culture medium, wash twice with phosphate buffer (0.01mol / L, pH 7.4), ...

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Abstract

The invention discloses tylophora ovata base analogs with anti-tumor activity and a preparation method and a use thereof. The tylophora ovata base analogs can be applied in the preparation of drugs for treating malignant tumors, leukemia and cancers, and the compound structural formula is as follows: R1, R2, R3 or R4 can be CH3O, R1R2, R3R4 and OCH2O, and R1, R2, R3 and R4 can not be CH3O at the same time. The tylophora ovata base analogs have the characteristics of high efficiency, low toxicity and significant role of inhibiting tumor cells, and can be applied in anti-cancer new drugs; the tylophora ovata base analogs are synthesized by adopting the one kettle way, the process is not separated, and final products are separated; and PIDA is added for synthesis, the synthesis route is simple, the efficiency is high and the cost is low.

Description

technical field [0001] The invention belongs to a class of seraphine analogues, in particular to a class of siraphrine analogues with antitumor activity and a preparation method and use thereof. Background technique [0002] Malignant tumors are major diseases that endanger human health and life. my country is a high-incidence area for liver cancer, gastric cancer, esophageal cancer, breast cancer, lung cancer and other cancers, and the number of deaths due to cancer is increasing year by year. The treatment of cancer has always been a difficult problem in the medical field. Governments, research institutions and pharmaceutical companies of various countries have long attached great importance to anti-tumor drugs. However, the existing anti-cancer chemotherapy drugs have different degrees of side effects. In recent years, the anti-tumor active ingredients extracted from Chinese herbal medicines have been paid more and more attention. Dozens of anti-cancer drugs such as vinbl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61K31/437A61P35/00A61P35/02
Inventor 方志杰王远兴
Owner NANJING UNIV OF SCI & TECH
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