New application of acevaltratum

A technology of acetyl valerian and combined drug, applied in the field of pharmacology, can solve problems such as multiple myeloma

Active Publication Date: 2021-01-22
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 acevaltratum
  • New application of acevaltratum
  • New application of acevaltratum

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Transfect Otub1, HA-c-Maf, and c-Maf-specific recognition unit (pMARE)-driven luciferase.Luci.Plasmid pMARE.Luci in HEK293T cells, and cells were cultured for 24 hours at 10,000 cells per well Inoculate into 96-well cell culture plate, add different natural compounds (all compounds are dissolved in dimethyl sulfoxide (DMSO) and then diluted to the application concentration after the cells adhere to the wall. After continuing to culture at 37°C for 24 hours, collect the cells for fluorescein Determination of enzyme activity. The relative luciferase activity (RLU) of each compound treated cells is indicated by the Log2 value of the luciferase in the treated sample divided by the luciferase in the DMSO control cell.

[0049] See results figure 1 ,according to figure 1 , acetylvalerianin significantly inhibited c-Maf-driven luciferase activity.

Embodiment 2

[0051] In order to further analyze the inhibitory effect of acetylvalerian (AVT) on the oncogene transcription factor c-Maf, the present invention first transfected Otub1, HA-c-Maf, pMARE.Luci. plasmid and internal control β-Gal in HEK293T cells . After 24 hours, the cells were inoculated into 96-well cell culture plates at a density of 10,000 cells per well. After the cells adhered to the wall, different concentrations of acetylvalerianin were added, and the cells were collected for luciferase activity assay after continuing to culture at 37°C for 24 hours. , to analyze the activity of acetylvalerianin in inhibiting luciferase.

[0052] Further, in the present invention, the multiple myeloma cell lines (RPMI-8226, LP1) are treated with different concentrations of acetylvalerian (0 μM, 1 μM, 2 μM, 4 μM, and the medicine is prepared with 100% DMSO and then diluted in serum-free IMDM. After 24 hours of treatment in the base, the final concentration of DMSO was less than 0.1%, t...

Embodiment 3

[0056] In order to analyze the inhibitory effect of acetylvalerian (AVT) on the oncogene transcription factor STAT3, the present invention transfected the luciferase plasmid (pSTAT3-Luc) driven by the STAT3 specific recognition unit and the internal control β-Gal plasmid in HEK293T cells . After 24 hours, the cells were inoculated into a 96-well cell culture plate at a density of 10,000 cells per well, and different concentrations of acetylvalerian were added after the cells adhered to the wall. The culture was continued at 37°C for 24 hours, and then the cells were collected for the determination of luciferase activity. Acetylvalerianin inhibited the activity of luciferase. In addition, after the multiple myeloma cell line LP1 was treated with different concentrations of acetylvalerianin (0, 1, 2, 4 μM) or co-treated with interleukin 6 (IL-6) or STAT3 inhibitor Stattic for 24 hours, the total cell protein was extracted , JAK2, p-STAT3 and c-Maf protein levels were detected b...

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Abstract

The invention provides a new application of acevaltratum, and particularly relates to an application of the acevaltratum to preparation of a medicine for preventing and/or treating tumors. The inventor finds that the acevaltratum has an obvious inhibiting effect on tumor cells, and the inhibiting effect is verified on cells and animal living bodies. Tests prove that the acevaltratum can induce thedegradation of c-Maf, CCND1 and JAK2 oncoproteins and inhibit Otub1, c-Maf, USP10 and STAT3 signal channels, so that the proliferation of tumor cells is effectively controlled, the apoptosis of the tumor cells is induced, and the acevaltratum has inhibiting and treating effects on tumors. Besides, as a plant extract, the acevaltratum also has the advantage of low toxicity.

Description

technical field [0001] The invention belongs to the field of pharmacology, in particular to a new application of the compound acetylvalerian. Background technique [0002] Cancer or tumor is a malignant lesion originating from human epithelial or leaf tissue. Cancer has biological characteristics such as abnormal cell differentiation and proliferation, uncontrolled growth, invasion, and metastasis. Its occurrence is a multi-factor and multi-step complex process. . Tumors can originate from almost all tissues and organs, so common different tumors can be formed, such as lung cancer, breast cancer, brain cancer, liver cancer, prostate cancer, kidney cancer, blood cancer, etc. These malignant tumors are major diseases that seriously threaten the physical and mental health of our people. According to the survey of the main causes of death of urban and rural residents in 2006 announced by the Ministry of Health of my country, the number of people who die from malignant tumors in...

Claims

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Application Information

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Patent Type & Authority Applications(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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