Induced nuclear receptor TR3 expressed cardiac glycoside compounds and use thereof

Abstract

The invention relates to a cardiac glycoside compound for inducing a nuclear receptor TR3 to express. The general formula of the compound of the invention is as follows: wherein, R1 is CH3, CHO or CH2OH; R2 is H or OH; R3 is H or OH; and R4 is a linear sugar chain or a branch sugar chain consisted by saccharide. The cardiac glycoside compound of the invention can induce the nuclear receptor TR3 to express, thus being capable of being used as a revulsant to be applied to the preparation of drugs which are used for preventing and treating cancer, hepatitis and atherosclerosis, etc.

Description

technical field The invention relates to a cardiac glycoside compound for inducing expression of nuclear receptor TR3 and application thereof. Background technique TR3 is an orphan nuclear receptor encoded by the human NR4A1 gene. The currently cloned mouse genes include Nur77 (mouse) and NGF-IB (rat), which are related to two other close relatives identified in recent years, NOT-1 and NOR-1s form a striking subfamily. TR3 is an immediate early gene, many external signals, including various growth factors (such as nerve growth factor, epidermal growth factor, fibroblast growth factor, serum growth factor), calcium ionophore, KCl, phorbol ester, retinoic acid Family, Tax protein and so on can induce the expression of TR3. The structure of TR3 family members has relatively unique structural characteristics. Its transcriptional activity is mainly controlled by the transcription activation region AF1 at the N-terminus, and the pocket structure of the ligand-binding region at t...

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Problems solved by technology

In addition, the high expression of members of the TR3 subfamily in the blood vessel wall may promote the pathogenesis of atherosclerosis, and the transcriptional activation of Nur77-regulated genes is involved in the inflammatory response of macrophages and the proliferation of vascular smooth muscle cells; it can be speculated that Nur77 located in the nucleus may promote atherosclerosis, Repression of transcriptional activation when located outside the nucleus may inhibit atherosclerotic lesion progression

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