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Application of bifid pregnane-type steroid compound in preparation of medicine for resisting erythroleukemia

A technology of steroidal compounds and erythroleukemia, applied in the fields of biology and medicine, can solve problems such as cell damage, toxic side effects, and lack of high selectivity

Active Publication Date: 2020-07-17
THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the lack of high selectivity, traditional chemotherapy drugs can also cause serious damage to normal cells and produce toxic side effects
At the same time, due to the heterogeneity of the disease, this treatment has certain limitations and even drug resistance

Method used

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  • Application of bifid pregnane-type steroid compound in preparation of medicine for resisting erythroleukemia
  • Application of bifid pregnane-type steroid compound in preparation of medicine for resisting erythroleukemia
  • Application of bifid pregnane-type steroid compound in preparation of medicine for resisting erythroleukemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] MTT assay was used to determine the inhibitory effect of different concentrations of BW18 on the proliferation of HEL cells.

[0034] Dilute erythroleukemia cells HEL according to 8×10 3 The density of cells / well was planted in a 96-well plate, and BW18 solutions of different concentrations of 20 μM, 10 μM, 5 μM and 2.5 μM were added immediately for treatment. In addition, a control group was set, and 0.1% DMSO was added to the control group. After culturing for 72 hours, add 20 μL of MTT solution with a concentration of 5 mg / mL to each well, incubate at 37°C for 4 hours, centrifuge to discard the supernatant, and add 160 μL DMSO to each well to dissolve. After the blue-purple crystal formazan is completely dissolved, use a microplate reader to measure the different treatments The absorbance value OD at 490nm of the group and the control group was calculated to obtain the corresponding inhibition rate, and obtained figure 1 .

[0035] The calculation method of inhibi...

Embodiment 2

[0039] HEL cells were divided into 6×10 3 The density of each well was planted in a 96-well plate, and BW18 at different concentrations of 20 μM, 10 μM and 5 μM was immediately added for treatment, and a control group was set at the same time, and 0.1% DMSO was added to the control group. After culturing for 72 hours, the morphological changes of the cells in each group were observed by photographing with an inverted microscope, and obtained figure 2 .

[0040] figure 2 The results showed that with the increase of BW18 concentration, the number of HEL cells decreased significantly, and the cell volume became larger, and BW18 at a concentration of 10 μM and 20 μM significantly inhibited cell growth, indicating that BW18 inhibited HEL cells in a concentration-dependent manner.

Embodiment 3

[0042] HEL cells were divided into 6×10 3 The density of cells / well was planted in a 96-well plate, and BW18 at different concentrations of 20 μM, 10 μM and 5 μM were immediately added for treatment, and a control group was set at the same time, in which 0.1% DMSO was added. The OD values ​​at 490nm in the treatment group and the control group were detected by MTT method at 0h, 12h, 24h, 36h, 48h, 72h and 96h, and the growth curve was drawn to obtain image 3 .

[0043] according to image 3 It can be seen that compared with the control group, different concentrations of BW18 can inhibit the proliferation of HEL cells, and as the concentration of BW18 increases, the growth rate of cells gradually slows down, indicating that BW18 has a concentration- and time-dependent effect on the proliferation of HEL cells.

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Abstract

The invention discloses an application of a bifid pregnane-type steroid compound in the preparation of a medicine for resisting erythroleukemia, and belongs to the technical field of biology and medicine and pharmacy. The bifid pregnane-type steroid compound disclosed by the invention is C21 steroid saponin BW18. MTT assay shows that the BW18 at different concentrations could inhibit the cell viability of HEL and is concentration dependent. The results of a flow cytometer and Western blot show that the BW18 induces the G2 phase cycle block of HEL cells by up-regulating P27 and down-regulatingthe expression of c-Myc, cyclin E1, CDK1 and CDK2 cycle-related proteins, regulates the expression of differentiation-related genes of erythroid and megakaryocyte lines, promotes the differentiation of cells to erythroid and megakaryocyte lines, thus inhibits the development of erythroleukemia. The BW18 can be used as a potential small molecule for treating the erythroleukemia, and provides a research basis for the development of the medicine for treating the erythroleukemia.

Description

technical field [0001] The invention relates to the technical fields of biology and medicine, in particular to the application of a biscispregnane-type steroid compound in the preparation of anti-erythroleukemia drugs. Background technique [0002] Acute erythroid leukemia (AEL) is a subtype of acute myeloid leukemia. Although the incidence of acute erythroid leukemia is low, its prognosis and survival rate are extremely poor, with an average survival period of only 4 to 14 months. The current treatment methods for acute erythroid leukemia mainly include conventional chemotherapy and hematopoietic stem cell transplantation. Hematopoietic stem cell transplantation is difficult to be widely used clinically due to various factors such as matching restrictions and high medical expenses. At present, acute erythroid leukemia is still dominated by conventional chemotherapy, and the clinical standard chemotherapy regimen is anthracycline combined with cytarabine. However, due to ...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P35/02A61K36/27A61K125/00
CPCA61K31/7048A61P35/02A61K36/27
Inventor 杨珏李艳梅郝小江晏英邱剑飞饶青宋晶睿
Owner THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI
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