Emodin as inhibitor of activated molecules p-Akt and p-mTOR of PI3K/Akt/mTOR signal transduction pathway and application thereof

Abstract

The invention discloses emodin as an inhibitor of activated molecules p-Akt and p-mTOR of a PI3K / Akt / mTOR signal transduction pathway and application thereof, wherein the emodin is a purely natural anthraquinone monomer compound extracted from rhubarb as a Chinese traditional medicine and has multiple biologic activities such as anti-microbes, anti-inflammation, antioxidation, immune regulation, liver protection and the like. The invention finds that after acute leukemia multidrug-resistance cells HL-60 / ADR, acute promyelocytic leukemia retinoic acid drug-resistant cells MR2 as well as corresponding sensitive cells NB4 and acute leukemia primary cells are acted by the rhubarb, key signal activated molecules of the PI3K / Akt / mTOR signal transduction pathway, particularly p-Akt and p-mTOR, are inhabited with specificity; in vivo researches verify that after the emodin is dosed, all the key activated molecules p-Akt, p-p65 and p-mTOR of the PI3K / Akt / mTOR signal pathway in acute leukemia nude mouse transplanted tumor tissue protein are expressed and downwards regulated, which indicates that the emodin can be used as a novel targeting inhibitor for PI3K / Akt / mTOR signal transduction activated molecules, particularly p-Akt and p-mTOR, and is applied to treating malignant tumors of a blood system.

Description

Technical field: [0001] The invention belongs to the field of medicine, and relates to emodin as an inhibitor of PI3K / Akt / mTOR signal transduction pathway activation molecules p-Akt and p-mTOR, especially for effects on acute leukemia drug-resistant cells PI3K / Akt / mTOR signal transduction pathway application. Background technique: [0002] Phosphatidylinositol-3 Kinase (PI3K for short) is an important molecule in the signal transduction process of the growth factor superfamily, and serine / threonine protein kinase (Akt for short) and its downstream signaling molecules in mammals PI3K / Akt / mTOR composed of the target of rapamycin (mTOR for short) is one of the important signal transduction pathways in the body. By regulating the activation state of key signaling molecules, it can promote proliferation and inhibit cell apoptosis in cells. Nearly 70% of acute myeloid leukemia (AML) patients have abnormal activation of PI3K / Akt / mTOR signaling pathway, and the continuous activatio...

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Problems solved by technology

The application defect of rapamycin and its analogs is the inhibition of mTOR and the feedback activation of Akt at the same time

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