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Polypeptide derivative ruthenium complex and its preparation method and application

A technology of peptide derivatives and derivatives, applied in the field of biomedicine, can solve the problems of no inhibitory effect on primary tumors, biological activity to be improved, severe liver and kidney toxicity, etc.

Active Publication Date: 2022-05-31
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Cisplatin is a metal complex antineoplastic drug widely used clinically, but it has severe liver and kidney toxicity
In addition to platinum-based antitumor drugs, ruthenium-based metal complexes have been extensively studied in the past few decades due to their unique biochemical characteristics, and some ruthenium metal complexes, such as NAMI-A (Pelillo, C. ; Mollica, H.; Eble, J.A.; Grosche, J.; Herzog, L.; Codan, B.; the rutheniumdrug NAMI-A.J.Inorg.Biochem.2016,160,225-235) and KP1339 (Trondl, R.; Heffeter, P.; Kowol, C.R.; Jakupec, M.A.; Berger, W.; Keppler, B.K. ruthenium-based anticancer drug on the edge to clinical application.Chem.Sci 2014,5,2925-2932), has been proven to inhibit tumor metastasis, but has no inhibitory effect on primary tumors, and its biological activity still needs to be improved

Method used

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  • Polypeptide derivative ruthenium complex and its preparation method and application
  • Polypeptide derivative ruthenium complex and its preparation method and application
  • Polypeptide derivative ruthenium complex and its preparation method and application

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preparation example Construction

[0037]

[0038] In the present invention, if no special instructions, the preparation raw materials used are commercially available commodities well known to those skilled in the art.

[0044]

[0055]

[0071]

Embodiment 1

2

)GD(OBzl)S‑OBzl.

[0077] ESI / MS (m / z): 754 [M+H]

+

Embodiment 2

[0081] ESI / MS (m / z): 659 [M+H]

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Abstract

The invention provides a polypeptide derivative ruthenium complex and its preparation method and application, which belong to the technical field of biomedicine. The ruthenium complexes of the present invention can target integrin receptors highly expressed on the surface of tumor cells and platelets, have selective killing effect on tumor cells, and can promote the entry of drugs (ie, the ruthenium complexes) into tumors Cells; in vivo experiments, the BABL / C Nude mouse A549 tumor-bearing model was used to evaluate the inhibitory effect of ruthenium complexes on primary tumors and tumor metastasis, and their distribution in vivo was determined by ICP‑MS. The tumor tissues were analyzed by immunohistochemistry and immunofluorescence, and the activity of ruthenium complexes against arterial thrombosis was evaluated by using the rat external carotid artery cardiopulmonary bypass model. The results show that the ruthenium complex of the present invention has inhibitory effects on both primary tumors and tumor metastasis, has high biological activity, and can inhibit the formation of arterial thrombus in a dose-dependent manner.

Description

Polypeptide derivative ruthenium complex and its preparation method and application technical field The present invention relates to the technical field of biomedicine, particularly to polypeptide derivative ruthenium complex and preparation method thereof and application. Background technique [0002] With the increasing incidence of tumors year by year, the research and development of antitumor drugs has received more and more attention. Cisplatin is a It is a widely used metal complex antitumor drug in clinic, but it has serious liver and kidney toxicity. In addition to platinum anti-tumor In addition to oncology drugs, ruthenium-based metal complexes have been extensively investigated in the past few decades due to their unique biochemical characteristics. Research, some ruthenium metal complexes, such as NAMI-A (Pelillo, C.; Mollica, H.; Eble, J.A.; Grosche, J.; Herzog, L.; Codan, B.; Sava, G.; Bergamo, A. Inhibition of adhesion, migration and of α 5β1integr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06C07K1/02C07K1/107A61K47/64A61P7/02A61P35/00A61P35/04
CPCC07K7/06A61K47/64A61P35/00A61P35/04A61P7/02Y02P20/55
Inventor 王玉记陈溯卢玉朱迪阿依江·塔勒道汗玛尔玛尔·托汉
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES