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Novel application of vinblastine and its analogue

A technology of vinblastine and substances, which is applied to the new application field of vinblastine substances, can solve problems such as studies that have not yet been reported, and achieve the effects of significant differences in efficacy and good efficacy.

Active Publication Date: 2015-07-01
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the application and research of vinblastine substances in diabetic retinopathy and rheumatoid arthritis have not been reported yet.

Method used

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  • Novel application of vinblastine and its analogue
  • Novel application of vinblastine and its analogue
  • Novel application of vinblastine and its analogue

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Inhibitory effect of vinblastine derivatives on the invasion ability of human vascular endothelial cells HUVECs

[0039] Experimental method: HUVECs cells in the logarithmic growth phase were digested, centrifuged, counted, and 5×10 6 / mL were respectively inoculated in Transwell chambers covered with Matrigel Matrigel (BD Company), 0.1 mL per hole, placed in 5% CO 2 , 37 ℃ cell incubator after incubation for 24 hours, set up the blank control group and the drug treatment group, the drug group were added vinblastine compounds vinblastine (CCJ), vinorelbine (CCRB), vinflunine (CCFN) and vinblastine Neosine (CCXJ) and vinblastine derivatives hydrazine vinblastine (JJ-CCJ), vinblastine dipeptide (BX-CCJ), hydrazinolysis vinorelbine (JJ-CCRB), vinorelbine dipeptide (BX- CCRB), hydrazinolyzed vinflunine (JJ-CCFN), vinflunine dipeptide (BX-CCFN), hydrazinolyzed vincristine (JJ-CCXJ) and vincristine dipeptide (BX-CCXJ), final drug concentration Both were 100pmol / L....

Embodiment 2

[0042] Example 2 Inhibitory Effect of Vinblastine Derivatives on the Migration Ability of Human Vascular Endothelial Cells HUVECs

[0043] Experimental method: Take HUVECs cells in logarithmic growth phase, wash and centrifuge with PBS, and resuspend the cells in serum-free medium. Will 2×10 6 Cells / mL were inoculated in Transwell chambers, 100 μL per well, and a blank control group and a drug treatment group were set up. The vinblastine compounds vinblastine (CCJ), vinorelbine (CCRB), vinflunine (CCFN ) and vincristine (CCXJ) and vinblastine derivatives hydrazinolyzed vinblastine (JJ-CCJ), vinblastine dipeptide (BX-CCJ), hydrazinolyzed vinorelbine (JJ-CCRB), vinorelbine dipeptide (BX-CCRB), hydrazinolyzed vinflunine (JJ-CCFN), vinflunine dipeptide (BX-CCFN), hydrazinolyzed vincristine (JJ-CCXJ) and vincristine dipeptide (BX-CCXJ), The final drug concentration was 100 pmol / L, and 700 μL of 1640 culture solution containing 10% newborn bovine serum was added to the lower chamb...

Embodiment 3

[0047] Example 3 Inhibitory Effect of Vinblastine Derivatives on Lumen Formation of Human Vascular Endothelial Cells HUVECs

[0048] Experimental method: Spread Matrigel in a pre-cooled 48-well plate, add 100 μL to each well, and place it in a 37°C cell culture incubator for 20 minutes. After the Matrigel is solidified, add 1×10 5 HUVECs cells / well, the cell culture medium was pre-added with vinblastine compounds and vinblastine derivatives JJ-CCJ, BX-CCJ, JJ-CCRB, BX-CCRB, JJ-CCFN, BX-CCFN, JJ-CCXJ and BX -CCXJ (final concentration is 100pmol / L) and vascular endothelial growth factor (VEGF) (final concentration is 100ng / mL), the wells without drug and VEGF are used as blank control group. After continuing to culture for 8 hours, observe the formation of the lumen under an inverted microscope and take pictures.

[0049] The result is as image 3 .

[0050] The experimental results showed that vinblastine compounds, hydrazinolyzed vinblastine compounds and vinblastine dipep...

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PUM

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Abstract

The invention provides a novel application of a vinblastine substance, and specifically speaking, the invention provides an application of vinblastine and its analogue for preventing or treating diabetic retinopathy or rheumatoid arthritis, and especially relates to obvious effect for preventing or treating diabetic retinopathy or rheumatoid arthritis displayed by a vinblastine derivative hydrazinolyed vinblastine compound, vinblastine dipeptides and salt in vitro and vivo, wherein the hydrazinolyed vinblastine compound is the compound obtained by the vinblastine compound and hydrazine hydrate through a reaction; the vinblastine dipeptides can be the hydrazinolyed vinblastine obtained by condensation of compound formed by the vinblastine compound and hydrazine hydrate through the reaction and N-benzyloxycarbonyl dipeptides.

Description

technical field [0001] The present invention provides a new application of vinblastine substances, in particular, provides a new application of vinblastine and its analogues in preventing or treating diabetic retinopathy or rheumatoid arthritis. It belongs to the field of medicine. Background technique [0002] Diabetic retinopathy is a serious complication of diabetes (Malone J I, et al. Diabetes Care. 2001, 24(3):522-526). With the continuous improvement of people's living standards, the number of diabetic patients is increasing, and the incidence of diabetic retinopathy is also increasing, which seriously affects the quality of life of diabetic patients (Ramavat P R, et al.JClin Diagn Res.2013, 7(7 ): 1387-1390). The exact pathogenesis of diabetic retinopathy is not completely clear yet, some studies suggest that the process of retinal neovascularization is involved in the process of the disease (Jae-Seung Yun, et al. Diabetes Metab J.2013, 37: 262-269) . In recent ye...

Claims

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Application Information

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IPC IPC(8): A61K38/05A61K31/475A61P3/10A61P9/10A61P19/02A61P29/00
Inventor 叶文才张冬梅陈河如陈敏锋肖绪枝许男徽雷雪萍胡坚杨
Owner JINAN UNIVERSITY
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