Interference RNA for inhibiting Rac1 expression and application thereof in increasing chemosensitivity to breast cancer

A breast cancer, sensitivity technology, applied in the direction of organic active ingredients, inorganic active ingredients, medical preparations of non-active ingredients, etc., can solve the problems of single treatment mode and uncontrollable drug release, achieve high enrichment, improve Sensitivity to chemotherapy and the effect of improving the effect of tumor chemotherapy

CN109718242AActive Publication Date: 2019-05-07SUN YAT SEN MEMORIAL HOSPITAL SUN YAT SEN UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Publication Date
2019-05-07

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Abstract

The invention relates to the field of biological medicines, in particular to interference RNA for inhibiting the Rac1 expression and an application thereof in increasing the chemosensitivity to breastcancer, and also discloses a breast cancer chemotherapeutic drug. The invention comprises the interference RNA for inhibiting the Rac1 expression and the chemotherapeutic drug, and a carrier of tumormicroenvironment response for transporting the interference RNA and the chemotherapeutic drug. According to the invention, an acid-sensitive nano-material is used as the carrier, can efficiently convey the siRNA and the chemotherapeutic drug into tumor cells, has a long circulation time in blood, and has high enrichment amount in tumors. Meanwhile, the nano-material encapsulates the siRNA and thechemotherapeutic pro-drug, can effectively silence the target gene and effectively inhibit the expression of drug-resistant genes, enhances the killing effect on tumor cells at the same time, obviously improves the tumor chemotherapy effect, has small toxic and side effects on normal tissue cells, and has no obvious damage to important organs such as heart and liver.
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Description

technical field

[0001] The invention relates to the field of biology, in particular to an interfering RNA for inhibiting the expression of Rac1 and its application in increasing the chemosensitivity of breast cancer. Background technique

[0002] The incidence of cancer is increasing year by year, and it has become one of the most serious diseases threatening human health.

[0003] At present, chemotherapy is still the cornerstone of cancer treatment, but chemotherapy drugs lack targeting, which kills tumor cells and also greatly damages normal cells, which leads to some patients who cannot tolerate the side effects of chemotherapy and discontinue treatment. Moreover, many patients receiving chemotherapy are prone to develop drug resistance after a period of treatment.

[0004] At present, some new anti-cancer drugs have been developed, such as molecular targeted drugs, antibody-drug conjugates, RNA interference technology, and nano-drugs.

[0005] It has been found that t...

Examples

Embodiment

[0037] This embodiment provides a chemotherapeutic drug for breast cancer, including nanocarriers responsive to the acidic pH of endosomes, the nanocarriers are loaded with siRNA and chemotherapeutic drugs, and the siRNA can knock down the expression of the drug resistance gene Rac1 of cancer cells.

[0038] Wherein, the siRNA is an interfering RNA that inhibits the expression of Rac1, and its gene sequence can be 5'-AGACGGAGCTGTAGGTAAA-3' (siRac1-1), as shown in SEQ NO.1, and its gene sequence can also be 5'-CCTTTGTACGCTTTGCTCA-3 '(siRac1-2), as shown in SEQ NO.2.

[0039] In this embodiment, what the nanocarrier adopts is polyethylene glycol-b-poly(2-(diisopropylamino)ethyl methacrylate) (PEG-b-PDPA), and its response pH value is The matrix environment of the cell endosome has a pH value range, that is to say, the response pH value of the nanocarrier is 6.0-6.5. In practical applications, nanocarriers are not limited to PEG-b-PDPA, as long as the response pH is within the pH ...