41 results about "Radiosensitizer" patented technology

The present invention relates to intracellular copper zinc superoxide dismutase inhibitors for protecting a subject from damage caused by radiation outbreak. The invention also relates to kits comprising SOD1 inhibitors and radiosensitizers for cancer cells, to the in vitro use of SOD1 inhibitors for protecting non-cancer cells from ionizing radiation, and to methods, compositions and uses related thereto.

The invention belongs to the technical field of radiotherapy sensitizers, and relates to a hafnium-titanium composite nano radiosensitizer as well as a preparation method and application thereof. The invention discloses a preparation method of a hafnium-titanium composite nano radiosensitizer, which comprises the following steps: (1) mixing a titanium-based metal frame compound Ti-MOF and hafnium-based oxide HfO2 with water according to a mass ratio of 2: 1-1: 2, putting the mixture into a reaction kettle, and carrying out hydrothermal reaction at 80-130 DEG C for 6-48 hours to obtain hafnium-titanium nanoparticles; and (2) dispersing the hafnium-titanium nanoparticles in the hydrophilic modification material solution, and stirring at room temperature for 6-48 hours to obtain the hafnium-titanium composite nano radiosensitizer. The invention also discloses application of the hafnium-titanium composite nano radiosensitizer in the field of imaging and preparation of medicines for treating colorectal cancer.

The present application relates to a kind of radiotherapy sensitization microneedle and its preparation method and application, belong to biological medicine technical field.The radiotherapy sensitization microneedle of the present application includes hyaluronic acid and nano radiosensitizer;The radiotherapy sensitization microneedle is obtained by drying after hyaluronic acid and nano radiosensitizer solution are mixed;The nano radiosensitizer solution is prepared by the following method: hafnium salt, 1,1'-ferrocene dicarboxylic acid and benzoic acid are mixed in organic solvent and stirred, centrifugal;The supernatant obtained is dialyzed, extracted, and the liquid phase obtained after solid-liquid separation is nano radiosensitizer solution.The radiotherapy sensitization microneedle of the present application is applied to the growth inhibition and radiotherapy sensitization of mouse melanoma cell B16F10 cell, can fully play the role of radiotherapy sensitization while overcoming the limitation of prior art, and preparation route is simple, and have certain conversion prospect.

The invention discloses an absorbable particle cannula loaded with double radiosensitizers, and aims to effectively improve the internal radiation radiotherapy effect and facilitate implantation of radioactive particles, and the whole material can be degraded and absorbed in vivo and does not need to be taken out through a secondary operation. The absorbable particle sleeve mainly comprises an absorbable particle sleeve body for packaging radioactive particles, a spacer which is arranged in the sleeve body and is used for spacing the radioactive particles, and a polydopamine coating which is loaded with a double radiosensitizer of metal nanoparticles and aromatic ring structure drugs. In the polydopamine coating, the metal nanoparticles are nanoparticles formed by reducing metal ions on the surface of the coating in situ through catechol groups of polydopamine; and the medicine is loaded on the surface of the coating through non-covalent acting force (pi-pi stacking action, hydrophobic interaction and / or electrostatic attraction).

The application of poly(D-lactic acid) and poly(D-lactic acid-glycolic acid) copolymers in constructing micro / nanocarriers for antitumor drugs belongs to the field of biomedical polymer materials and nanomedicine. The antitumor drugs are small-molecule chemotherapeutic agents, small-molecule photosensitizers, small-molecule immunotherapeutic agents, and small-molecule radiosensitizers. The particle size of the poly(D-lactic acid) and poly(D-lactic acid-glycolic acid) copolymers is 10–5000 nm. The effective concentration of the poly(D-lactic acid) and poly(D-lactic acid-glycolic acid) copolymers is 1–500 mg / kg. The antitumor mechanism of the poly(D-lactic acid) and poly(D-lactic acid-glycolic acid) copolymers includes increasing the activity of effector T cells in the tumor microenvironment and increasing the concentration of cytokines such as IFN-γ at the tumor site. In the field of tumor therapy, PLA and PLGA materials composed of D-lactic acid have shown good effects in inhibiting tumor growth, prolonging the survival period of tumor-bearing mice, and activating antitumor immune responses.

The invention belongs to the field of biological medicine, and particularly relates to a high-selectivity sensitizer for solid tumor radiotherapy and a preparation method thereof.The sensitizer comprises two newly-designed modified compounds: a derivative based on a diamino-anthraquinone structure and capable of enhancing radiation energy deposition and relieving tumor hypoxia; and the other one is a cystamine derivative containing a diselenide bond, and can effectively consume overexpressed glutathione in tumor cells and enhance the generation of active oxygen. The preparation method comprises the following steps: dissolving the two modified compounds and the biodegradable polymer in an organic solvent to form an organic phase, dissolving phospholipid polyethylene glycol amino in warm water, blending with a stabilizer in a buffer solution to form a water phase, dropwise adding the organic phase into the water phase through a nano-precipitation method, self-assembling to form nano-particles, and filtering and purifying to obtain a final product. The sensitizer can specifically target tumor tissues, the radiotherapy effect is remarkably improved through a multiple synergistic mechanism, meanwhile, the damage to normal tissues is reduced, the preparation process is simple and convenient, and the reproducibility is good.

Systems and methods for radiation therapy for cancerous tumors using biocompatible quantum dots to provide radiation dose enhancement and resistance to metastasis are described. In an aspect, a method for radiation therapy treatment of cancer cells, includes, but is not limited to, preparing a radiosensitizer fluid, the radiosensitizer fluid including a plurality of biocompatible quantum dots; introducing the radiosensitizer fluid to cancer cells; and irradiating the cancer cells with the radiosensitizer fluid to promote generation of reactive oxygen species and inhibit radiation-induced enhancement of cell-migration.

Disclosed herein is a radio-afterglow nanoparticle (RANP) comprising ABCD, wherein: A represents a radioabsorber; B represents a radiosensitizer; C represents a luminescent component; and D represents an amphiphilic polymeric matrix. Also disclosed herein are a method for the detection of cancer in vivo, a method of treating cancer, a method of treating cancer in a patient by administering the aforementioned radio-afterglow nanoparticle, uses of the aforementioned radio-afterglow nanoparticle, and a drug comprising the aforementioned radio-afterglow nanoparticle.

The invention discloses a sensitizing drug for resisting breast cancer by radiotherapy and a screening method and application thereof, and belongs to the field of biomedicine.The method comprises the steps that an in-vitro radiotherapy resistance model is constructed, a clinical segmentation radiotherapy dose increasing mode is simulated, stable acquired radiotherapy resistance is induced to be generated, and a carrier is provided for drug screening; natural plant small molecule compounds are used for treatment, and through concentration and time gradient dual control, the reversion ability of the natural plant small molecule compounds to radiotherapy resistance phenotypes is investigated; a multi-dimensional joint detection system is established, multi-level comprehensive evaluation is performed from cell survival and the like, the limitation of a single index is broken through, and the screening accuracy and reliability are improved; dNA damage repair is dynamically monitored through immunofluorescence, comet electrophoresis and the like, and the drug action mechanism is revealed. The medicine screened by the method is suitable for primary and acquired radiotherapy resistance patients, can effectively improve the radiotherapy curative effect, provides a new medicine source and scheme for clinical problems, and opens up the application of the compound in preparation of radiosensitizers or adjuvant therapy medicines.

The invention relates to an application of suramine in promoting tumor radiotherapy sensitization. The invention fully proves that suramin can effectively prepare tumor cells in a state highly sensitive to ferroptosis through a novel metabolic reprogramming mechanism of inhibiting IPPK, reducing IP6 and releasing Fe < 2 + > chelated with an iron pool in cells, thereby creating necessary biochemical conditions for ferroptosis; and the sensitivity of cells to ferroptosis induced stimulation is fundamentally changed. Therefore, the compound can be used as a ferroptosis inducer and a potent sensitizer for radiotherapy at the same time. The discovery not only provides a new combined strategy for overcoming tumor treatment resistance, but also perfectly explains the transformation medicine concept of new use of old medicines, and provides a new active ingredient for human tumor treatment, thereby providing a new direction for subsequent medicine research and development, clinical treatment and the like, and having extremely high social value and market application prospects.

The application provides a preparation method of selenium-doped Prussian blue nanoparticles modified by a targeting polypeptide, and comprises the following steps: (1) synthesizing Prussian blue nanoparticles by a microwave method; (2) synthesizing selenium-containing Prussian blue by a gas-phase atomic deposition method; and (3) preparing selenium-doped Prussian blue nanoparticles modified by a targeting polypeptide: dissolving a tumor-targeting RGD cyclic peptide in ultrapure water, adding a catalyst N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and then stirring, then performing dialysis, adding the selenium-containing Prussian blue into the dialysate, stirring, centrifuging, resuspending and obtaining the selenium-doped Prussian blue nanoparticles modified by the targeting polypeptide. According to the preparation method, the selenium is naturally deposited on the surface of the Prussian blue by the gas-phase atomic deposition method, monodisperse selenium with controllable doping amount is formed, and the selenium-doped Prussian blue modified by the targeting polypeptide is prepared.

The subject of the application is a 2'-deoxyadenosine derivative in the form of 8-(4-trifluorothio)benzylamino-2'-deoxyadenosine of formula 1 and its use as a radiosensitizer of DNA damage, which sensitizes cancer cells to ionizing radiation. The application also covers a method for obtaining 8-(4-trifluorothio)benzylamino-2'-deoxyadenosine of formula 1, characterized in that 8-bromo-2'-deoxyadenosine of formula 2 is mixed with 4-trifluorothiobenzylamine of formula 3 in a molar ratio of 1:8, in the presence of methanol, and then the mixture is heated to reflux and stirred for 72 h.

The present invention relates to an inhibitor of intracellular copper-zinc superoxide dismutase for use in protecting subjects from radiation burst injury. The present invention also relates to a kit comprising an SOD1 inhibitor and a radiosensitizer for cancer cells, the in vitro use of an SOD1 inhibitor for protecting non-cancer cells from ionizing radiation, and methods, compositions, and uses relating thereto.

The invention belongs to the technical field of biological catalytic materials, and particularly relates to a gold monatomic radiosensitizer with multienzyme activity as well as a preparation method and application of the gold monatomic radiosensitizer. The gold monatomic radiosensitizer is a coordination complex formed by a gold source containing tetrachloro gold (III) acid radical ions and 2, 4, 6-tri (4-pyridyl)-1, 3, 5-triazine through a coordination substitution reaction of Au and pyridine nitrogen. The gold monatomic radiosensitizer disclosed by the invention is a biocatalyst which is newly designed, has multi-enzyme activity biological catalysis performance and can be activated by radiation, and can be used as a polymer artificial enzyme for efficient and controllable tumor treatment.

Radiosensitizer prodrugs and formulations and methods of use thereof are provided. Typically, the radiosensitizer prodrug is an analog of a radiosensitizer parent compound having one or more S-nitrosothiol moieties. Typically, the S—N bond of the S-nitrosothiol moiety can be cleaved by radiation during radiotherapy, releasing the parent compound and nitric oxide. One or preferably both the parent compound and the nitric oxide can contribute to death of tumor cells exposed to radiotherapy. Nanoparticle formulations for delivery of the prodrug, and methods of using them in combination with radiotherapy to treat tumors and cancer are also provided.

Conjugates of the formula T-L-A wherein T is a ligand targeting prostate specific membrane antigen (PSMA), L is a linker, and A is a radiosensitizer; a pharmaceutical composition comprising the conjugate and a pharmaceutically acceptable carrier; and methods of treating prostate cancer or metastases thereof in a patient using radiotherapy. A conjugate of formula T-L-A can be administered prior to or after administration of a conjugate of formula T-L-X, wherein X is or comprises a radiotherapy or (radiation) imaging agent. Conjugates of formula T-L-(X) A, pharmaceutical compositions comprising the same, and methods of use are also disclosed.

The invention discloses application of USP15 in preparation of a bladder cancer radiotherapy sensitizer, and belongs to the technical field of biological medicine. The objective of the invention is to improve the radiotherapy sensitivity of bladder cancer. The invention relates to an application of USP15 in preparation of a bladder cancer radiotherapy sensitizer. The USP15 is used for preparing the bladder cancer radiotherapy sensitizer. The radiotherapy sensitivity of the bladder cancer is improved by overexpressing the USP15. The USP15 can regulate and control the stability of FIS1 protein through ubiquitination modification so as to inhibit the mitochondrial function, and the activation of the regulation and control pathway is the core mechanism of the USP15 for exerting the radiotherapy sensitization effect. In conclusion, the invention not only provides a new thought for molecular mechanism research of bladder cancer radiotherapy sensitization, but also provides a potential strategy for treatment of clinical radiotherapy resistant bladder cancer patients, and has important drug development value and clinical application prospect.

This invention discloses the application of disulfiram or its pharmaceutical salt in the preparation of radiosensitizers, wherein the radiosensitizer refers to a radiosensitizer for malignant tumors, specifically osteosarcoma. The radiation involved in the radiosensitizer is selected from alpha, beta, gamma, or X-ray radiation. This invention is the first to discover and confirm a novel use of disulfiram in enhancing the radiosensitivity of malignant tumors, significantly inhibiting the proliferation of osteosarcoma cells after radiotherapy and promoting cell death in vitro. It also demonstrates outstanding efficacy in inhibiting the growth of subcutaneously implanted osteosarcoma in mice after radiotherapy.

The invention relates to the technical field of radiotherapy drugs. The invention provides an application of frankincense diene alcohol acid in preparation of a tumor radiosensitizer. According to the application disclosed by the invention, the frankincense dienol acid can promote apoptosis induced by radioactive rays, so that the radiotherapy sensitivity is remarkably enhanced.

The present invention provides a radiosensitizer or anti-cancer chemotherapy sensitizer including a combination of (a) hydrogen peroxide and (b) hyaluronic acid or a salt thereof, wherein the hydrogen peroxide content in a final formulation is 0.1 to 3.5 weight percent.

Radiosensitizer prodrugs, and formulations and methods of use thereof are provided. Typically, the radiosensitizer prodrugs are analogs of a radiosensitizer parent compound having one or more S-nitrosothiol moieties. Typically, the S-N bond of the S-nitrosothiol moiety can be radiocleaved during radiation therapy, releasing the parent compound and nitric oxide. One, or preferably both, of the parent compound and nitric oxide can promote death of tumor cells exposed to radiation therapy. Also provided are nanoparticle formulations for delivery of the prodrugs, and methods of using them in combination with radiation therapy to treat tumors and cancers.

The invention addresses radioresistance in cancer treatment involving radiotherapy and, in particular, limitations associated with the use of the drug sulfasalazine. Specifically, it provides a series of compounds for use as radiosensitizers in the treatment of cancers such as glioblastomas which are lethal and inherently resistant to radiotherapy. In one embodiment, the invention provides compounds of general formula (I), their stereoisomers and pharmaceutically acceptable salts for use as radiosensitizers in the treatment of cancer:wherein ring A is selected from optionally substituted phenyl, biphenyl and fluorenyl; each X is independently selected from: —C1-6 alkyl (preferably C1-3 alkyl, e.g. —CH3), —O—C1-6 alkyl (preferably —O—C1-3 alkyl, e.g. —OCH3), —S—C1-6 alkyl (preferably —S—C1-3 alkyl, e.g. —SCH3), —OH, —SH, —CO2R1 (where R1 is H or C1-6 alkyl, preferably C1-3 alkyl, e.g. —CH3), —SO2—C1-6 alkyl (preferably —SO2—C1-3 alkyl, e.g. —SO2—CH3), —SO2—NR2R3 (where R2 is H and R3 is optionally substituted phenyl), —NR4R5 (wherein R4 and R5 are independently selected from H, C1-6 alkyl (preferably C1-3 alkyl, e.g. —CH3), and —CO—C1-6 alkyl (preferably —CO—C1-3 alkyl, e.g. —CO—CH3), halogen (e.g. F, Cl or Br), and optionally substituted tetrazolyl; n is an integer from 0 to 5, preferably 0 to 2, e.g. 1 or 2; and denotes an E or Z double bond.

Compounds and pharmaceutically acceptable salts thereof of Formula (I) are disclosed. Certain compounds and salts of Formula (I) are active as TDP1 inhibitors and radiosensitizers of cancer cells. The disclosure provides pharmaceutical compositions containing a compound of Formula (I) as the only active agent, or optionally containing one or more additional active agents. Methods of using compounds of Formula (I) to treat a cancer are provided in this disclosure. The disclosed compounds of Formula (I) may be used alone to treat cancer, but may also be used in combination with another active agent, such as a TOPI inhibitor, for example, camptothecin or a camptothecin analogue, and / or ionizing radiation.

This invention discloses a radiosensitizer with multi-enzyme activity, its preparation method, and its application in the preparation of antitumor agents. The radiosensitizer comprises rhodium-copper alloy nanoparticles, trithiol-terminated polymethacrylic acid modified on the surface of the rhodium-copper alloy nanoparticles, and lactate oxidase bound to the trithiol-terminated polymethacrylic acid. The preparation method involves mixing rhodium-copper alloy nanoparticles with trithiol-terminated polymethacrylic acid bound to their surface, 1-ethyl-(3-dimethylaminopropyl)carbodiimide, and N-hydroxysuccinimide ester, stirring, adding lactate oxidase, and continuing stirring to obtain the radiosensitizer. This invention achieves precise assembly of the nanocarrier and enzyme-active components through modular design. This invention provides an efficient and safe solution for integrated tumor diagnosis and treatment, and has significant potential for industrial production.

The invention relates to the technical field of biological medicines, and particularly discloses application of a PPAR pathway regulator in preparation of a nasopharyngeal carcinoma radiotherapy sensitizer. In-vitro experiments prove that after the expression of the MAP2K7 gene in nasopharynx cancer cells is silenced by utilizing shRNA, the sensitivity of the cancer cells to radioactive rays can be remarkably enhanced. Mechanism research is carried out by using a transcriptome sequencing technology, it is found that MAP2K7 silently up-regulates the activity of a PPAR pathway, that is, MAP2K7 influences the radiotherapy sensitivity by regulating a PPAR signal pathway, and the activity of the PPAR pathway is in positive correlation with the radiotherapy sensitivity of nasopharyngeal carcinoma. The invention provides a new therapeutic target and a solution for nasopharyngeal carcinoma radiotherapy resistance, and lays a theoretical basis and an experimental basis for developing a novel radiotherapy sensitizer based on an MAP2K7-PPAR pathway.

The invention relates to a radiotherapy sensitization microneedle and a preparation method and application thereof, and belongs to the technical field of biological medicine. The radiotherapy sensitization microneedle provided by the invention comprises hyaluronic acid and a nano radiosensitizer, the radiotherapy sensitization microneedle is obtained by mixing hyaluronic acid and a nano radiosensitizer solution and then drying; the nano radiosensitizer solution is prepared by the following steps: mixing hafnium salt, 1, 1 '-ferrocene dicarboxylic acid and benzoic acid in an organic solvent, stirring, and centrifuging; and dialyzing and extracting the obtained supernate, and carrying out solid-liquid separation to obtain a liquid phase which is a nano radiosensitizer solution. The radiotherapy sensitization microneedle is applied to growth inhibition and radiotherapy sensitization of mouse melanoma cells B16F10, the radiotherapy sensitization effect can be brought into full play, meanwhile, the limitation of the prior art is overcome, the preparation route is simple, and the radiotherapy sensitization microneedle has a certain conversion prospect.

Compounds and pharmaceutically acceptable salts thereof of Formula (I) are disclosed. Certain compounds and salts of Formula (I) are active as TDP1 inhibitors and radiosensitizers of cancer cells. The disclosure provides pharmaceutical compositions containing a compound of Formula (I) as the only active agent, or optionally containing one or more additional active agents. Methods of using compounds of Formula (I) to treat a cancer are provided in this disclosure. The disclosed compounds of Formula (I) may be used alone to treat cancer, but may also be used in combination with another active agent, such as a TOPI inhibitor, for example, camptothecin or a camptothecin analogue, and / or ionizing radiation.

The application discloses a radio-sensitizing functionalized probiotic hybrid material and a preparation method and application thereof, and belongs to the technical field of medical preparations. Black phosphorus nanosheets and bismuth nanoparticles are prepared first; then the bismuth nanoparticles are blended with the black phosphorus nanosheets in an aqueous solution environment, NH2-PEG 2000 -MAL and MMP-2 enzyme-responsive polypeptides are added and reacted to obtain a black phosphorus-based radio-sensitizer; finally, clostridium butyricum is blended with the black phosphorus-based radio-sensitizer, then N-hydroxysuccinimide and 1-ethyl-(3-dimethylaminopropyl) carbonyldiimidazole hydrochloride are added and incubated to obtain the radio-sensitizing functionalized probiotic hybrid material. The method has the advantages of simple process and high operability. The prepared radio-sensitizing functionalized probiotic hybrid material can effectively improve the targeting accuracy of the radio-sensitizer under the driving of anaerobic probiotics, reduce off-target toxic side effects, has the characteristics of high tumor inhibition efficiency, and has a wide application prospect in the field of anti-tumor.

The application belongs to the technical field of biological catalytic materials, and particularly relates to a gold monatomic radiosensitizer with multiple enzyme activities and a preparation method and application thereof. The gold monatomic radiosensitizer is a coordination complex formed by a coordination substitution reaction of a gold source containing a tetrachlorogold (III) acid radical ion and 2,4,6-tris (4-pyridyl) -1,3,5-triazine through Au and pyridine nitrogen. The gold monatomic radiosensitizer disclosed in the application is a newly designed biological catalyst with multiple enzyme activities and radioactivation, and can be used as a polymer artificial enzyme for efficient and controllable tumor treatment.