Application of acetic acid-2-(1H-indol-3-yl)-ethyl ester in preparation of antitumor drugs

Abstract

The invention discloses an application of acetic acid-2-(1H-indole-3-yl)-ethyl ester in preparation of antitumor drugs, and belongs to the technical field of chemical combination drugs, SiHa, HCC94, CaSki human cervical squamous carcinoma cells, Hela human cervical adenocarcinoma cells, SKOV3 human ovarian cancer cells and Hep-G2 human hepatoma cells are inoculated into a 96-well plate, 5000 cells exist in each well, and the cells are inoculated into the 96-well plate. On the second day, replacing the culture medium with a complete culture medium containing compounds with different concentrations, incubating in the incubator for 48 hours, and replacing the culture medium with a serum-free culture medium containing 10% CCK8 solution; according to the present invention, the light absorption value of the microplate reader at the wavelength of 450 nm is determined after the incubation in the incubator for 1 h, and the compound has effects of inhibition on the proliferation of a variety of tumor cells, such that the compound acetic acid-2-(1H-indole-3-yl)-ethyl ester can be used for preparing the cancer treatment drug, and has good development and application prospects.

Description

Technical Field

[0001] The present invention belongs to the technical field of chemical drugs, and particularly relates to the use of 2-(1H-indol-3-yl)ethyl acetate in the preparation of anti-tumor drugs. Background Art

[0002] Cancer seriously endangers human health, and such major diseases have received increasing attention. With the development of disciplines such as medicinal chemistry and pharmacology, small molecule drugs are one of the effective methods for treating tumors, and anti-tumor small molecule drugs have been continuously discovered and reported in recent years. Summary of the Invention

[0003] Technical problem to be solved: Aiming at the technical defects in the prior art such as the lack of reports on inhibiting the activity of tumor cells, the present invention discloses the use of 2-(1H-indol-3-yl)ethyl acetate in the preparation of anti-tumor drugs. The use of 2-(1H-indol-3-yl)ethyl acetate involved in the present invention in the preparation of anti-tumor drugs is disclosed for the first time, has outstanding substantive features, and provides a new choice for the development of anti-tumor drugs.

[0004] Technical solution:

[0005] The use of 2-(1H-indol-3-yl)ethyl acetate in the preparation of anti-tumor drugs.

[0006] Further, the prepared anti-tumor drug is in an injectable form or a non-injectable form.

[0007] Further, the prepared anti-tumor drug is an injection, tablet, capsule, powder, pill, granule, solution, suspension, syrup, suppository or inhalant.

[0008] Further, the prepared anti-tumor drug comprises 2-(1H-indol-3-yl)ethyl acetate and pharmaceutically acceptable excipients.

[0009] Further, the excipients include one or more of a diluent, excipient, filler, binder, wetting agent, disintegrant, absorption enhancer, surfactant, adsorption carrier, lubricant.

[0010] Further, the structural formula of 2-(1H-indol-3-yl)ethyl acetate is as follows:

[0011]

[0012] Further, the anti-tumor drug inhibits human SiHa, HCC94, CaSki cervical squamous carcinoma cells, Hela human cervical adenocarcinoma cells, SKOV3 human ovarian cancer cells and Hep-G2 human liver cancer cells.

[0013] Beneficial effects:

[0014] 1. The present invention discloses the anti-tumor activity of 2-(1H-indol-3-yl)ethyl acetate. Research shows that this compound has good inhibitory effects on human cervical squamous carcinoma cells (SiHa, HCC94, CaSki), human cervical adenocarcinoma cells Hela, human ovarian cancer cells SKOV3, and human liver cancer cells HepG2, providing a basis for the development of anti-tumor drugs and being of great significance for the development of new anti-tumor drugs and tumor treatment;

[0015] 2. For the compound 2-(1H-indol-3-yl)ethyl acetate involved in the present invention, there is currently no report on its inhibitory activity against tumor cells. The use of 2-(1H-indol-3-yl)ethyl acetate involved in the present invention in the preparation of anti-tumor drugs is disclosed for the first time, with prominent substantive features, providing a new option for the development of anti-tumor drugs;

[0016] 3. Experimental results show that the compound described in the present invention has an inhibitory effect on the proliferation of various tumor cells. Therefore, the compound 2-(1H-indol-3-yl)ethyl acetate can be used to prepare drugs for the treatment of cancer and has good development and application prospects;

[0017] 4. The use of the compound involved in the present invention in inhibiting the proliferation of SiHa, HCC94, CaSki human cervical squamous carcinoma cells, Hela human cervical adenocarcinoma cells, SKOV3 human ovarian cancer cells and Hep-G2 human liver cancer cells, but not limited to the above tumor cells, is disclosed for the first time, and there is currently no report on this compound, with prominent substantive features, and can provide a new option for the treatment of related tumors. BRIEF DESCRIPTION OF THE DRAWINGS

[0018] Figure 1 It is a graph showing the effect of the 2-(1H-indol-3-yl)ethyl acetate compound of the present application on the proliferation of human cervical squamous carcinoma tumor cells SiHa at different concentrations and the IC50 concentration;

[0019] Figure 2 It is a graph showing the effect of the 2-(1H-indol-3-yl)ethyl acetate compound of the present application on the proliferation of human cervical squamous carcinoma tumor cells CaSki at different concentrations and the IC50 concentration;

[0020] Figure 3 It is a graph showing the effect of the 2-(1H-indol-3-yl)ethyl acetate compound of the present application on the proliferation of human cervical squamous carcinoma tumor cells Hcc94 at different concentrations and the IC50 concentration;

[0021] Figure 4Effect of ethyl 2-(1H-indol-3-yl)acetate compound of the present application on the proliferation of human cervical adenocarcinoma tumor cells Hela at different concentrations and IC50 concentration graph;

[0022] Figure 5 Effect of ethyl 2-(1H-indol-3-yl)acetate compound of the present application on the proliferation of human ovarian cancer tumor cells SKOV3 at different concentrations and IC50 concentration graph;

[0023] Figure 6 Effect of ethyl 2-(1H-indol-3-yl)acetate compound of the present application on the proliferation of human liver cancer tumor cells HepG2 at different concentrations and IC50 concentration graph. Detailed implementation mode

[0024] The present invention will be further described in detail below with reference to the accompanying drawings and specific embodiments.

[0025] The technical means used in the following embodiments, unless otherwise specified, are all conventional means well known to those skilled in the art. The experimental methods without specific conditions mentioned are all conventional methods in the art.

[0026] The materials, reagents, etc. used in the following embodiments, unless otherwise specified, can be obtained from commercial channels. Ethyl 2-(1H-indol-3-yl)acetate in the present application is prepared by the preparation of ethyl 2-(1H-indol-3-yl)acetate and its application in controlling Penicillium expansum disclosed in CN118530158A or the preparation method of a kind of ethyl 2-(1H-indol-3-yl)acetate disclosed in CN118530157A.

[0027] Example 1

[0028] An application of ethyl 2-(1H-indol-3-yl)acetate in the preparation of anti-tumor drugs. Through the in vitro cancer cell proliferation test CCK8, the inhibitory effects of ethyl 2-(1H-indol-3-yl)acetate compound on the proliferation of SiHa, HCC94, CaSki human cervical squamous carcinoma cells, Hela human cervical adenocarcinoma cells, SKOV3 human ovarian cancer cells and Hep-G2 human liver cancer cells are as follows:

[0029] First step: Inoculate SiHa, HCC94, CaSki human cervical squamous carcinoma cells, Hela human cervical adenocarcinoma cells, SKOV3 human ovarian cancer cells and Hep-G2 human liver cancer cells into 96-well plates containing complete medium, with 5000 cells in each well. The preparation method of the complete medium is as follows: Take DMEM medium, add 5 mL of fetal bovine serum and 0.5 mL of penicillin-streptomycin mixture to every 45 mL, mix well, and store at 4°C.

[0030] Step 2: On the second day, replace the culture medium with a complete medium containing different concentrations (800, 400, 200, 100, 50, 25, 12.5, 6.25, 3.125 μg / mL) of 2-(1H-indol-3-yl)ethyl acetate;

[0031] Step 3: After incubating in the incubator for 48 hours, replace the culture medium with a serum-free medium containing 10% CCK8 solution;

[0032] Step 4: After incubating in the incubator for 1 hour, measure the absorbance value at a wavelength of 450 nm using an enzyme-linked immunosorbent assay reader.

[0033] As shown in the accompanying drawings of the specification, Figures 1-6 They are the effects of 2-(1H-indol-3-yl)ethyl acetate on inhibiting SiHa, CaSki, Hcc94 human cervical squamous carcinoma cells, Hela human cervical adenocarcinoma cells, SKOV3 human ovarian cancer cells, and Hep-G2 human liver cancer cells, respectively. The results show that 2-(1H-indol-3-yl)ethyl acetate has an inhibitory effect on the activities of 6 types of human tumor cells. The IC50 values of 2-(1H-indol-3-yl)ethyl acetate on the activities of SiHa, CaSki, Hcc94 human cervical squamous carcinoma cells, Hela human cervical adenocarcinoma cells, SKOV3 human ovarian cancer cells, and Hep-G2 human liver cancer cells are 192.4 μg / mL, 202.1 μg / mL, 209.2 μg / mL, 288.7 μg / mL, 203.0 μg / mL, and 209.1 μg / mL, respectively.

[0034] The embodiments described above are only a part of the embodiments of the present invention, rather than all of the embodiments. The detailed description of the embodiments of the present invention is not intended to limit the scope of the present invention claimed, but merely represents the selected embodiments of the present invention. The scope of protection of the present invention shall be subject to the scope claimed in the claims. Based on the embodiments of the present invention, all other embodiments obtained by those of ordinary skill in the art without making creative efforts shall fall within the scope of protection of the present invention.

Claims

1. Use of 2-(1H-indol-3-yl)-ethyl acetate in the preparation of anti-tumor drugs.

2. The use of 2-(1H-indol-3-yl)-ethyl acetate in the preparation of anti-tumor drugs according to claim 1, characterized in that: The prepared anti-tumor drug is in an injection form or a non-injection form.

3. The use of 2-(1H-indol-3-yl)-ethyl acetate in the preparation of anti-tumor drugs according to claim 1, characterized in that: The prepared anti-tumor medicine is in the form of injection, tablet, capsule, powder, pill, granule, solution, suspension, syrup, suppository or inhalant.

4. The use of 2-(1H-indol-3-yl)-ethyl acetate in the preparation of anti-tumor drugs according to claim 1, characterized in that: The anti-tumor drug comprises 2-(1H-indol-3-yl)-ethyl acetate and pharmaceutically acceptable auxiliary materials.

5. The use of 2-(1H-indol-3-yl)-ethyl acetate in the preparation of anti-tumor drugs according to claim 4, characterized in that: The auxiliary materials include one or more of diluents, excipients, fillers, adhesives, wetting agents, disintegrants, absorption promoters, surfactants, adsorption carriers, and lubricants.

6. The use of 2-(1H-indol-3-yl)-ethyl acetate in the preparation of anti-tumor drugs according to claim 1, characterized in that: The structural formula of the acetic acid-2-(1H-indol-3-yl)-ethyl ester is as follows:

7. The use of 2-(1H-indol-3-yl)-ethyl acetate in the preparation of anti-tumor drugs according to claim 1, characterized in that: The anti-tumor drug inhibits human SiHa, HCC94, CaSki cervical squamous cell carcinoma cells, Hela human cervical adenocarcinoma cells, SKOV3 human ovarian cancer cells and Hep-G2 human liver cancer cells.

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