12 results about "Temozolomida" patented technology

Through extensive and deep research, a new path Parkin / Park / Mul1 / Mfn2 for regulating and controlling the drug resistance of a tumor chemotherapy temozolomide (TMZ) drug by the TRPC5 is found, and the new path has a close relationship with the generation of the drug resistance of the tumor chemotherapy temozolomide (TMZ) drug. Compared with primary cells U87 and U251, the expression level of the TRPC5 in temozolomide tolerant cells U87R and U251R is remarkably improved, and a mitochondrial autophagy pathway is activated. By reducing the expression of the TRPC5 gene, the sensitivity of a cell strain to a temozolomide drug can be enhanced, and the proliferation capacity of tumor cells can be inhibited. According to the invention, not only is new data provided for a malignant glioma drug resistance mechanism, but also a new target spot is provided for the design of anti-tumor drug resistance drugs.

A single-cell transcriptome-guided multimodal synergistic injectable magnetically responsive biomimetic hydrogel system, its preparation method, and its application are described. This hydrogel platform is a three-level composite system of "matrix-microsphere-nanoparticle": the primary structure is a photocrosslinked methacryloyl hyaluronic acid three-dimensional network matrix; the secondary structure is GelMA microspheres loaded with MTPT nanoparticles prepared by microfluidic control; and the tertiary structure consists of bevacizumab and magnetite nanoparticles dispersed in the HAMA matrix. The MTPT nanoparticles have a mesoporous silica core, which is sequentially coated with temozolomide, a polydopamine coating, and a T7 targeting peptide. Under the activation of an alternating magnetic field, Fe3O4 generates a magnetothermal effect, which not only achieves local hyperthermia but also accelerates the time-sequential release of bevacizumab and MTPT, synergistically exerting the effects of chemotherapy, anti-angiogenic therapy, and hyperthermia.

Methods of treating glioma using a WEE1 inhibitor are disclosed.

The invention relates to the technical field of biomedical engineering and brain drug delivery, in particular to a phase-change controlled-release multi-stage implantable brain drug delivery device and a preparation method thereof. The system is specially designed for postoperative treatment of brain malignant tumors and is composed of a fibroin nanofiber substrate, a drug-loaded phase change material nanoparticle layer, a degradable packaging layer and a wireless heating module. Fatty acid mixtures with different melting points are used as phase change matrixes to wrap chemotherapeutic drugs (such as temozolomide) and anti-aging drugs (such as ABT-263) respectively, and nano-drug carriers with specific thermal response temperatures (such as 39 DEG C and 42 DEG C) are constructed. After the system is implanted into a brain tumor excision lacuna, under the action of an external radio frequency magnetic field, accurate heat is generated through the wireless heating module, the phase change material is triggered to be melted in a graded mode, programmed sequential release of medicine to brain tissue is achieved, collaborative treatment of'chemotherapy-senescent cell removal 'in the brain is achieved, the limitation of a blood brain barrier is effectively broken through, and the treatment effect is good. The brain tumor recurrence problem is solved.

The application discloses a monomer compound DTA and application thereof in preparation of a temozolomide-sensitive glioma inhibiting drug. Through a glioma primary cell model, it is proved that the monomer compound Demethylenedelcoine A (DTA) can produce a better anti-chemotherapy resistant glioma effect than a clinical first-line chemotherapy drug temozolomide and carmustine. Therefore, in clinical treatment of temozolomide chemotherapy resistance and radiotherapy failure recurrent glioma, the monomer compound DTA can have a potential treatment advantage, and therefore has a potential drug development value.

The invention discloses an application of a small molecule inhibitor HY-Q66655 in preparation of a medicine for treating glioma. The compound HY-Q66655 capable of targeting YRDC is obtained by taking YRDC as a target spot and utilizing a virtual screening technology. In-vivo and in-vitro experiments show that the HY-Q66655 can significantly inhibit the proliferation ability of glioma stem cells and temozolomide-resistant glioma cells, and enhance the sensitivity of the cells to a first-line chemotherapeutic drug temozolomide, and is high in safety; the combination of HY-Q66655 and TMZ shows a good synergistic inhibition effect on the proliferation of glioma stem cells and glioma cells with drug resistance to temozolomide. Therefore, the invention provides a small-molecule inhibitor HY-Q66655 capable of targeting YRDC and inhibiting proliferation of glioma stem cells and drug-resistant cells thereof, and a brand new candidate drug and a promising combined treatment strategy are provided for treating glioma and overcoming TMZ drug resistance of glioma.

This invention belongs to the field of biopharmaceuticals, specifically referring to a photo-environment-targeted antitumor nanoparticle IUR, its preparation method, and its application. In this application, HA and RVG29 peptides are chemically linked to generate HA-RVG29. Then, HA-RVG29 is coated onto nanoparticles self-assembled from UA and the photosensitizer IR820 via electrostatic interactions, forming photosensitive nanoparticle IURs with glioma-targeting activity. This IUR exerts a therapeutic effect on gliomas through combination with temozolomide. Cell and animal experiments demonstrate that the combination of these nanoparticles and TMZ has a good antitumor effect. In vivo experiments, using TUNEL cell apoptosis detection, flow cytometry, inverted fluorescence microscopy, and other methods, show that the combination of IUR and TMZ can promote cell apoptosis, inhibit cell proliferation, and has a good inhibitory effect on gliomas.

The invention belongs to the technical field of biological medicine, and particularly relates to pachysandra terminalis alkaloid Pactermine Q as well as a preparation method and application thereof. The invention provides a pachysandra terminalis alkaloid Pactermine Q with anti-tumor biological activity, the compound is a new alkaloid separated from pachysandra terminalis, and the inhibition effect on human brain glioma cells is obviously better than that of temozolomide.

The invention relates to the technical field of biological medicine, discloses application of RasGRP3 as a glioma drug-resistant target, a pharmaceutical composition and a screening method, and aims at solving the problems that the drug-resistant mechanism of glioblastoma (GBM) temozolomide (TMZ) is not clear and effective treatment means are lacked by constructing a TMZ drug-resistant organ model. By utilizing multi-omics conjoint analysis of ChIP-seq, Hi-C and transcriptome sequencing and combining CRISPRi library screening, it is identified for the first time that RasGRP3 is a core gene driving GBM to generate tolerance to TMZ, and it is revealed that enhancer-mediated chromatin space reconstruction is a key regulation mechanism of the enhancer-mediated chromatin space reconstruction. According to the invention, the small-molecule inhibitor Punicalin specifically targeting the RasGRP3 is obtained through further screening. In-vivo and in-vitro experiments prove that Punicalin can inhibit phosphorylation of RasGRP3, tumor growth can be remarkably inhibited when Punicalin is combined with temozolomide, and chemotherapy drug resistance of glioma is effectively reversed. The invention provides a new target spot and a drug combination scheme for clinical treatment of GBM.

The application belongs to the technical field of pharmaceutical cocrystal, and particularly relates to a temozolomide-coffee acid pharmaceutical cocrystal and a preparation method thereof. The molecular formula of the temozolomide-coffee acid pharmaceutical cocrystal is 2C6H6N6O2.C9H8O4.0.5H2O, the crystal structure belongs to a monoclinic system, a space group is P2(1) / c, cell parameters are alpha=90 degrees, beta=113.631(5) degrees, gamma=90 degrees, a cell volume is V=2.019(2) nm3, and a minimum asymmetric unit number in the cell is Z=8. Temozolomide, coffee acid and acetone are uniformly mixed to obtain a temozolomide-coffee acid mixed solution, and then the temozolomide-coffee acid pharmaceutical cocrystal is obtained by performing volatilization crystallization on the temozolomide-coffee acid mixed solution. The temozolomide-coffee acid pharmaceutical cocrystal prepared by the application can effectively improve the stability and solubility of temozolomide and coffee acid single raw medicine. The preparation method of the temozolomide-coffee acid pharmaceutical cocrystal prepared by the application is simple and easy for industrial development and production.

Malignant glioma has a poor prognosis, despite current therapeutic modalities. Standard of care therapy consists of surgical resection, fractionated radiotherapy concurrently administered with temozolomide (TMZ), a DNA-alkylating chemotherapeutic agent, followed by adjuvant cycles of TMZ. O6-methylguanine DNA methyltransferase (MGMT) is a DNA repair enzyme which removes alkylated lesions from tumor DNA, thereby promoting chemoresistance. MGMT promoter methylation is a known predictor of temozolomide responsiveness; patients with unmethylated MGMT have a poorer prognosis. We employed deactivated Cas9-CRISPR technology to effectively target methylation in the vicinity of the MGMT methylation-specific polymerase chain reaction (MSP) region, as mediated by the catalytic domain of DNA methyltransferase DNMT3A. In doing so, we discovered that the selected dCas9 / CRISPR-mediated methylation of certain regions of MGMT gene sequences can be used to enhance chemosensitivity in malignant glioma cells.

The invention discloses a preparation method of a double-response cellulose aerogel drug carrier, and the aerogel drug carrier prepared by the method has pH and photo-thermal double-response characteristics, and can realize the synergistic tumor inhibition effect of chemotherapeutic drugs. The preparation method of the double-response cellulose aerogel drug carrier mainly comprises the following steps: firstly, preparing ultra-small Fe3O4 nanoparticles; preparing a modified cellulose precursor solution; and finally, dissolving temozolomide and a poly (lactic-co-glycolic acid) in an organic solvent, adding the modified cellulose aerogel precursor solution after dissolving, stirring until the organic solvent is volatilized, adding the ultra-small Fe3O4 nanoparticles into the precursor solution, uniformly dispersing, pouring the solution into a mold, irradiating with UV light, and drying, thereby obtaining the temozolomide / poly (lactic-co-glycolic acid) composite material. And freezing and drying to obtain the double-response cellulose aerogel drug carrier.