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.
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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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