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New application of acetylvalerian

A technology of acetyl valerian and polyethylene glycol, applied in the field of pharmacology, can solve problems such as multiple myeloma, and achieve the effect of controlling proliferation and low toxicity

Active Publication Date: 2021-09-07
GUANGZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But in the MGUS phase (monoclonal gammopathy of undetermined significance, early stage of multiple myeloma), IgH translocations rarely accumulate 4p16t(4,14) and 16q23t(14,16), suggesting that these two translocations It may promote the development of pathological conditions such as MGUS and SMM, and eventually lead to the occurrence of multiple myeloma, or it may be related to the rapid development of MGUS into multiple myeloma

Method used

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  • New application of acetylvalerian
  • New application of acetylvalerian
  • New application of acetylvalerian

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] In HEK293T cells transfected Otub1, HA-c-Maf and c-Maf specifically recognizing means (pMARE) driven luciferase .Luci. Plasmid pMARE.Luci, the cells after 24 hours of incubation, 000 cells per well after inoculated into 96-well cell culture plates, adherent cells are added to different natural compounds (all compounds were dissolved in the dimethylsulfoxide (DMSO) was diluted to a concentration of the application. incubation was continued at 37 ℃ 24 hour collection cells fluorescein enzyme activity assay. cells were treated after each compound relative luciferase activity (RLU) using treated samples divided by luciferase Log2 of the DMSO control cells luciferase label.

[0049] See figure 1 ,according to figure 1 , Acetyl valerian hormone significantly inhibit luciferase activity driven by c-Maf.

Embodiment 2

[0051] To further analyze the inhibitory effect of valerian acetyl hormone (the AVT) oncogene transcription factor c-Maf, the present invention first in HEK293T cells transfected Otub1, HA-c-Maf, pMARE.Luci. Plasmid and internal control β-Gal . After 24 hours, the cell density per well 10,000 cells were seeded into a cell culture plate 96 well, cells adhered with different concentrations of acetyl valerian respective voxel, cultured cells were collected for luciferase activity was measured after 24 hours at 37 [deg.] C analysis acetyl valerian inhibits luciferase activity.

[0052] Further, the present invention is multiple myeloma cell line (RPMI-8226, LP1), 1μM, 2μM, 4μM, drugs were diluted in a serum-free after 100% DMSO with different concentrations of formulated acetyl valerian hormone (0μM IMDM culture group, DMSO final concentration less than 0.1%) 24 hours after treatment, total protein was extracted, and detection of c-Maf protein levels of target gene regulation.

[0053...

Embodiment 3

[0056] For inhibition of transcription factor STAT3 oncogene analysis acetyl valerian hormone (AVT), the present invention is in HEK293T cells transfected luciferase plasmid (pSTAT3-Luc) STAT3 specifically recognizing the control unit for driving and β-Gal plasmid . After 24 hours, the cell density of 10000 cells per well were seeded into 96-well cell culture plates, adherent cells were added at different concentrations acetyl valerian respective voxel. Incubation was continued at 37 ℃ 24 hours and then the cells were collected for luciferase activity assay, acetyl valerian inhibits luciferase activity. In addition, multiple myeloma cell lines treated with different concentrations of acetyl LP1 valerian hormone (0,1,2,4μM), or interleukin-6 (IL-6) or STAT3 inhibitor Stattic After 24 hours co-treatment, total protein was extracted detection JAK2, p-STAT3 and c-Maf protein levels by Western blot.

[0057] See image 3 , In particular: The results show that acetylation valerian hormon...

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Abstract

The invention provides a new application of acetylvalerian, in particular to the application of acetylvalerian in the preparation of drugs for preventing and / or treating tumors. The present invention finds that acetylvalerian has obvious inhibitory effect on tumor cells, and the inhibitory effect is verified on cells and animal living bodies. It has been verified that acetylvalerianin can induce the degradation of c-Maf, CCND1, and JAK2 oncoproteins, inhibit Otub1, c-Maf, USP10, and STAT3 signaling pathways, thereby effectively controlling the proliferation of tumor cells and inducing their apoptosis. inhibitory and therapeutic effects. At the same time, as a plant extract, acetylvalerian also has the advantage of low toxicity.

Description

Technical field [0001] The present invention belongs to the field of pharmacology, in particular to a new use of a compound acetyl valerian pigment. Background technique [0002] Cancer or a tumor, a human epithelial origin or leaf tissue malignancy, cancers with biological features abnormal cell differentiation and proliferation, loss of control growth, invasive and metastatic, etc., which occurs more than one factor, the complex multi-step process . Tumors can originate from almost all tissues and organs, it is possible to form different common tumors, such as lung cancer, breast cancer, brain cancer, liver cancer, prostate cancer, kidney cancer, leukemia and so on. Cancer is a serious threat to these major diseases of our people's physical and mental health, the Ministry of Health announced the 2006 major cause of death in urban and rural residents survey show that: my country die each year nearly 2 million cancer, cancer has become the number one the cause of death, but the v...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61K45/06A61P35/00
CPCA61K31/352A61K45/06A61P35/00
Inventor 毛新良孙彤徐宇嘉
Owner GUANGZHOU MEDICAL UNIV
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