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Use of tanshinone IIA derivatives in preparation of drug for protecting endothelial cells

A technology of endothelial cells and derivatives, applied in drug combinations, pharmaceutical formulations, steroids, etc., can solve the problems of increasing druggability and poor water solubility of tanshinone IIA

Active Publication Date: 2016-08-10
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, tanshinone IIA has poor water solubility, so the preparation of tanshinone IIA derivatives with good water solubility and high activity can increase its druggability

Method used

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  • Use of tanshinone IIA derivatives in preparation of drug for protecting endothelial cells
  • Use of tanshinone IIA derivatives in preparation of drug for protecting endothelial cells
  • Use of tanshinone IIA derivatives in preparation of drug for protecting endothelial cells

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Effects of Tanshinone IIA Derivatives on SOD and MDA Contents in EA.hy926 Cells

[0027] 1.1 Test method: take EA.hy926 cells in the growth phase, and use 2*10 5 Inoculated in 50ml cell flasks, cultured for 24 hours, discarded the culture medium, added fresh serum-free DMEM high-glucose medium to the blank group and injured group, and carried out routine culture. On this basis, the treatment group was added various drugs at a concentration of 1 μg / ml, and after continuing to culture for 24 hours, the contents of malondialdehyde (MDA) and superoxide dismutase (SOD) in the cells were detected.

[0028] SOD increase rate=(administration group-model group) / administration group*100%

[0029] MDA reduction rate=(model group-administration group) / model group*100%

[0030] 1.2 Experimental results: as described in Table 1

[0031] Tanshinone IIA derivatives can increase the content of SOD and reduce the content of MDA in EA.hy926 cells

[0032]

[0033]

[0034]

...

Embodiment 2

[0037] MTT method to test tanshinone IIA derivatives to reduce H 2 o 2 reduce cell viability.

[0038] 2.1 Test method: EA.Hy926 was inoculated in a 96-well plate, and after 12 hours of normal culture, it was replaced with serum-free DMEM and continued to culture for 12 hours to synchronize the cells. Aspirate and discard the original culture solution, add different concentrations of test compounds for pre-protection for 12 hours, and replace with 900uM H 2 o 2 Serum-free DMEM medium, 100uL per well, and a normal control group, with three parallel wells for each group. After continuing to culture for 2 hours, the supernatant was collected, and the three wells were enriched in one tube for later LDH determination. Fresh serum-free medium was added to each well, and 10uL MTT was added to each well, and culture was continued for 4h, and the absorbance value (OD490) was detected at 490nm with a microplate reader. Calculate the cell viability value of each group.

[0039] 2.2...

Embodiment 3

[0047]Three compounds, WL-3, WL-4 and Tanshinone IIA, increased the mRNA expression of Nrf2-ARE downstream antioxidant proteins HO-1, Nrf2, GCLC and GCLM.

[0048] Cultivation and passage of A549 cells: A549 cells were cultured in DMEM medium containing 10% fetal bovine serum, 100U / mL penicillin, and 100U / mL streptomycin at saturated humidity and 5% CO at 37°C. 2 cultured in an incubator. A549 cells were subcultured after being treated with 0.25% trypsin containing EDTA. On average, the cells were subcultured every two days in the experiment. The specific operation is as follows: absorb the old culture medium in the cell culture dish, wash it once with PBS, then add an appropriate amount of trypsin to digest it for 1-2 minutes, and transfer the cells to a new culture medium in an appropriate proportion according to the proliferation speed of the cells and the needs of your own experiments. cultured in a 37°C incubator.

[0049] Drug preparation: take 2×10 5 A549 cells were...

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Abstract

The invention relates to the field of natural drugs and mainly relates to a use of tanshinone IIA derivatives shown in the general formula (I) and the general formula (II) in preparation of a drug for protecting endothelial cells. An experiment result shows that the tanshinone IIA derivatives shown in the general formula (I) and the general formula (II) obviously reduce H2O2-caused endothelial cell damage and reduces H2O2-caused endothelial cell apoptosis. A mechanism research result shows that the tanshinone IIA derivatives shown in the general formula (I) and the general formula (II) produce oxidation resistance through Nrf2-ARE passage activation.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry and pharmaceutical technology, and specifically relates to a class of tanshinone IIA derivatives, which are pharmaceutical compositions of active ingredients, a preparation method thereof, and the use of such compounds and other pharmaceutical compositions in preparing and treating diseases caused by endothelial cells drug application. Background technique [0002] Salvia Miltiorrhiza is the dry root and rhizome of Salvia Miltiorrhiza Bunge, which has the functions of dispelling blood stasis and relieving pain, promoting blood circulation and regulating menstruation, nourishing the heart and eliminating troubles. Salvia miltiorrhiza is widely used clinically for diseases of the cardiovascular system. It has the functions of dilating coronary arteries, increasing coronary blood flow, improving microcirculation, reducing myocardial oxygen consumption, and preventing myocardial ischemia and myocard...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/77A61K31/4525A61K31/5377A61K31/343A61P9/00A61P9/10A61P9/12A61P39/06
CPCC07J73/00
Inventor 王进欣陈君何龙
Owner CHINA PHARM UNIV
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