Composition comprising combination of epicatechin and Anti-cancer compound

A technology of epicatechin and compounds, applied in the direction of drug combinations, active ingredients of heterocyclic compounds, medical preparations containing active ingredients, etc., can solve the problems of long duration of treatment, high dosage, side effects of patients, etc.

Inactive Publication Date: 2019-10-08
SPHAERA PHARMA PVT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In addition, drugs and pharmaceutical compositions for the treatment of cancer are generally available to patients, and these drugs and compositions are usually very high doses and long duration of treatment, which causes various side effects in patients, and some drugs develop with drug resistance. the formation of invalid

Method used

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  • Composition comprising combination of epicatechin and Anti-cancer compound
  • Composition comprising combination of epicatechin and Anti-cancer compound
  • Composition comprising combination of epicatechin and Anti-cancer compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1: Evaluation of the synergistic effect of the combination of epicatechin and a PI3K / mTOR inhibitor (compound 1004)

[0037] The anticancer potential of epicatechin in combination with PI3K / mTOR inhibitors was evaluated for a cancer xenograft model in immunodeficient mice. CD-1 nude mice were given vehicle control, PI3K / mTOR inhibitor, and the combination of PI3K / mTOR inhibitor and epicatechin, and the administration period was 21 days. The greatest reduction in tumor volume was found in the (G-3) group, ie a tumor growth inhibition % (TGI%) of 97% when administered in combination. The results are shown in Table 2, Table 3 and Fig. 1a, Figure 1b middle.

[0038] Table 2: Results of the combination of epicatechin and compound No.1004 in HCT116-induced xenograft model in mice

[0039]

[0040] TG: Tumor Growth Inhibition

[0041] T / C: Treatment / Control on Day 21

[0042] Table 3: Results of Combination of Epicatechin and Compound No. 1004 in Reducing Tumo...

Embodiment 2

[0045] Example 2: Evaluation of the synergistic effect of the combination of (-) epicatechin and cisplatin

[0046] 2.1 Cell culture: use the Hell-299 cell line (corresponding to normal lung cells) as a normal cell control, and in 5% CO 2 A549 cell line (corresponding to lung adenocarcinoma) was cultured under standard conditions of 37°C. With different concentrations of cisplatin [CDDP (cis-diamine dichloroplatinum (II), Sigma)] [1 μM-100 μM], or (-) epicatechin (EC, Sigma) [0.1 μM to 1000 μM], or The combination of these two compounds treated the cells for 48 hours. Both compounds were dissolved in DMSO (0.9%).

[0047] 2.2 Cell viability: Cell viability was determined by MTT analysis. Briefly, cells were incubated with 0.1 mg / ml of MTT (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide) at 37°C for 40 minute. Use 0.01M HCl-isopropanol to dissolve the purple formazan. Lysates were determined spectrophotometrically at 595 nm (Bioteck Synergy HT).

[0048] Ce...

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Abstract

The present invention discloses a novel, stable and synergistic combination of epicatechin with anti-cancer compounds. The present invention also discloses a composition comprising the novel combination of epicatechin with anti-cancer compounds along with other pharmaceutically acceptable excipients.

Description

technical field [0001] The present invention relates to novel combinations of epicatechin and anticancer compounds, and compositions comprising the novel combinations. Background technique [0002] Cancer is one of the most prevalent human diseases, accounting for the highest proportion of human mortality and morbidity, causing millions of deaths every year and reducing the quality of life of patients. Cancer is a disease characterized by abnormal cell growth that may invade and / or spread to other parts of the body, and the incidence of all cancers is increasing worldwide. The incidence of cancer generally involves factors such as genetic factors, exposure to specific toxins and known carcinogens, specific substances, diet, habits such as smoking (tobacco), and the like. Alterations in genetic and metabolic pathways within cancer cells have been identified as the cause of disease. The Warburg effect observed that most cancer cells generate energy primarily through glycolys...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/00A61K36/00A61K33/243
CPCC07D311/62C07D401/04C07D417/04A61K31/337A61K31/353A61K31/44A61K31/506A61K31/517A61K31/5377A61K31/704A61K31/7068A61P3/04A61P35/00A61P43/00A61K33/243A61K2300/00A61K31/5355
Inventor 桑迪普·杜加尔
Owner SPHAERA PHARMA PVT
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