39 results about "Cisplatin" patented technology

The application discloses application of Ophisaurus apodus in preparation of a drug for reversing drug resistance of gastric cancer and belongs to the technical field of medicines. The application can reduce tumor volume and size, promote drug resistance cell apoptosis, and reverse the chemotherapeutic drug resistance of a nude mouse with gastric cancer by jointly using Ophisaurus apodus in different parts of the body and cisplatin, by down-regulating P-gp, MRP1 and Bcl-2 protein expression, and by up-regulating Bax protein expression. The effect of the tail + cisplatin group is the most significant.

The application provides a combination drug of a PLA2G7 inhibitor and a chemotherapeutic drug and its use in resisting triple-negative breast cancer, and belongs to the technical field of medicines. The combination drug is a PLA2G7 inhibitor and a chemotherapeutic drug in the same or different specifications of unit preparations for simultaneous or separate administration, and a pharmaceutically acceptable carrier. The application first discovers and proves that the PLA2G7 inhibitor Darapladib can significantly enhance the anti-tumor activity of paclitaxel, 5-fluorouracil or cisplatin on triple-negative breast cancer, and meanwhile, the combination of the PLA2G7 inhibitor and paclitaxel has a synergistic effect in down-regulating the phosphorylation level of STAT3 protein in cancer cells and inhibiting the growth and proliferation of cancer cells; the combination of the PLA2G7 inhibitor and 5-fluorouracil also shows a synergistic effect in inhibiting the growth and proliferation of cancer cells. The application provides a new and effective combination drug strategy for improving the treatment effect of the chemotherapeutic drug on triple-negative breast cancer.

This invention provides the application of Lycium barbarum polysaccharide (LBP) in the preparation of drugs for the prevention or treatment of intestinal flora and metabolic disorders. Research results show that LBP can significantly improve cisplatin-induced intestinal microbiota and metabolic disorders in rats, manifested by a significant reduction in CDDP-induced serum AST and ALT levels, and improvement in the degree of liver tissue lesions. Furthermore, LBP did not exhibit toxicity in rats. LBP enhanced the diversity and richness of the gut microbiota, restored the structure of dominant symbiotic bacteria, inhibited the proliferation of potentially pathogenic bacteria, and promoted the enrichment of functional bacteria related to SCFAs generation. LBP also restored abnormal metabolism in branched-chain amino acid and aromatic amino acid metabolism, one-carbon metabolism, and lipid metabolism. This invention provides a theoretical basis for the application of natural active polysaccharides in the prevention and treatment of intestinal microbiota and metabolic disorders.

This invention discloses a novel class of β-carboline quaternary ammonium salt derivatives, their preparation methods, and applications. The derivatives have the structure shown in Formula I, where R1, R2, and R3 are various substituents, and X... ‑ It is a halide ion. Its preparation method uses substituted indole-2-methylamine and substituted α-haloacetophenone as starting materials, and constructs them through a one-step cyclization reaction in an aprotic solvent mediated by a catalytic protic acid (such as p-toluenesulfonic acid). This method is mild, simple to operate, requires no metal catalyst, eliminates the risk of metal residue, and has good functional group compatibility. Activity tests of the obtained series of compounds showed that they have significant inhibitory activity against the proliferation of non-small cell lung cancer cell lines (such as A549 and H1299), with some compounds exhibiting activity superior to the positive control drug cisplatin. Therefore, this compound has important application value in the preparation of antitumor drugs, especially anti-lung cancer drugs.

The present application belongs to the technical field of biological medicine, and particularly relates to Hermetia illucens extract, an extraction method thereof and application thereof in preventing and treating tumors. The present application extracts polar components from Hermetia illucens powder, and the obtained Hermetia illucens extract has a significantly better inhibitory activity on the proliferation of Cal27 human tongue squamous cell carcinoma cells, Colo205 human colorectal cancer cells and U87 MG human brain astrocytoma cells than the Hermetia illucens powder without separation under the same mass concentration. In animal experiments, the Hermetia illucens extract can significantly prolong the survival cycle of MOC-1 tongue squamous cell carcinoma mice, and has a significantly better treatment effect than the Hermetia illucens powder and is close to the positive drug cisplatin.

The application discloses application of a rehmannia glutinosa extract in preparation of drugs for treating kidney injury caused by cisplatin. The application of the rehmannia glutinosa extract in preparation of drugs for preventing and / or treating kidney injury caused by cisplatin; a preparation method of the rehmannia glutinosa extract, comprising the following steps: S1, adding water to the rehmannia glutinosa to perform extraction, to obtain a rehmannia glutinosa water extract; S2, adding ethyl acetate to the rehmannia glutinosa water extract to perform extraction, separating ethyl acetate phase and water phase, to obtain the rehmannia glutinosa extract. The application constructs an animal model by inducing mouse kidney injury by cisplatin, and it is found that the rehmannia glutinosa extract obtained by further separating the rehmannia glutinosa water extract by using solvents such as ethyl acetate and ethanol can improve acute kidney injury caused by cisplatin, and the effect is better than that of the rehmannia glutinosa water extract.

The application discloses a kind of block copolymer and its preparation method and application, the application designs and synthesizes a kind of block copolymer mPEG-PLG-COOH-CD, utilize the host molecule β-CD with guest molecule IDO-1 inhibitor (such as Epa) and Pt class chemotherapy drug (such as cisplatin) with large cavity structure, by hydrophilic and hydrophobic interaction, host-guest recognition, coordination effect common assembly into supramolecular nanomedicine.Supramolecular nanomedicine simultaneously carries Pt class chemotherapy drug and IDO-1 inhibitor.Under the action of weak acid in tumor cell, nanomedicine swells, expose drug, and high concentration of Cl- will destroy the non-covalent bond force inside nanomedicine, quickly release chemotherapy drug and IDO-1 inhibitor, while activating chemotherapy and immunotherapy, realize the efficient combination of two kinds of therapy.In situ activation of chemotherapy not only directly kills cancer cells, but also activates the anti-tumor immunity of body.

This invention discloses a synergistic antitumor drug composition and its application. The composition consists of cisplatin and atorvastatin, with a molar ratio of cisplatin to atorvastatin of 1:1.5. This invention provides a combination of drug concentrations at low concentrations to treat cancer cells, inhibit cancer cell proliferation, activate and induce apoptosis. Compared with traditional methods, this method reduces cellular drug resistance, has a lower concentration, is safer and more effective, and reduces the toxic reactions caused by high concentrations of drugs.

This invention provides the use of CX6258 or its salts in medicaments for the prevention and / or treatment of lung cancer, belonging to the field of biomedicine. This invention is the first to discover that CX6258HCl can effectively inhibit the growth of lung squamous cell carcinoma cell lines and organoids, and that CX6258HCl can also be combined with cisplatin to treat lung squamous cell carcinoma. Therefore, CX6258 or its salts have broad application prospects in medicaments for the prevention and / or treatment of lung cancer, especially lung squamous cell carcinoma.

Disclosed herein is a method for predicting whether a subject with cancer will exhibit a beneficial response to arginine deficiency therapy. The method includes the step of determining the plasma concentration of arginine in the subject, followed by administering arginine deficiency therapy to the subject alone or in combination with an anticancer agent, based on the determined plasma concentration of arginine. According to some embodiments of this disclosure, the anticancer agent is selected from the group consisting of FOLFOX, docetaxel, cisplatin, pemetrexed, pembrolizumab, and combinations thereof.

The application discloses an IGF2BP2-m6A-VCAN-TLR2 signal axis in the preparation of a drug for treating intrahepatic cholangiocarcinoma lymphatic metastasis. In view of the problems of unknown intrahepatic cholangiocarcinoma lymphatic metastasis mechanism and lack of effective target, the application finds and verifies a new pathway that from insulin-like growth factor 2 mRNA binding protein 2, m6A modification regulates the expression of multi-functional proteoglycan, and then activates Toll-like receptor 2 signal, promotes macrophage secretion of vascular endothelial growth factor C and drives lymphatic metastasis. Based on this, the application provides an inhibitor targeting the signal axis, in particular, a small molecule compound 8010-8498. Experiments show that the compound can significantly inhibit cholangiocarcinoma cell migration, invasion and epithelial mesenchymal transition, reduce macrophage secretion of vascular endothelial growth factor C, and effectively inhibit tumor growth and lymphatic metastasis in a naked mouse popliteal lymph node metastasis model and a spontaneous cholangiocarcinoma model. The compound presents a synergistic effect in combination with gemcitabine and cisplatin.

The application discloses application of a pharmaceutical composition with GL-V9 and a chemotherapeutic drug as active ingredients in treatment of tumors, and the GL-V9 can obviously achieve a drug synergistic effect when the GL-V9 is combined with a classical chemotherapeutic drug to treat tumors, and the effect is obviously superior to combination of similar drugs and the chemotherapeutic drug. The chemotherapeutic drugs include PARP1 inhibitors, capecitabine, irinotecan, sorafenib, cisplatin or 5-fluorouracil; and the tumor types include leukemia, colorectal cancer and lung cancer.

This invention discloses the application of Tiaoqi Jiedu Tongyou granules in the preparation of anti-esophageal cancer drugs targeting the IL1B / AHR / PSMD3 axis, belonging to the field of biomedical technology. Experiments have demonstrated that Tiaoqi Jiedu Tongyou granules can significantly downregulate the expression of IL1B, AHR, and PSMD3 proteins in cisplatin-induced esophageal cancer cells, inhibit cisplatin-induced treatment-related aging and aging-related secretory phenotypes, reduce the secretion of IL-6, IL-8, CXCL2, and TNF-α, and inhibit cell proliferation, migration, and invasion in a concentration-dependent manner. It can intervene in high-risk esophageal cancer patients identified by the IL1B / AHR / PSMD3 trigene prognostic model. This invention also discloses an anti-esophageal cancer drug containing the active ingredients of the granules and pharmaceutically acceptable excipients, which can intervene in high-risk esophageal cancer patients identified by the IL1B / AHR / PSMD3 trigene prognostic model. This invention provides a new drug intervention pathway for aging-related inflammation and recurrence after esophageal cancer chemotherapy, and has significant clinical application value.

This invention belongs to the field of organic chemistry, specifically relating to a method for preparing and applying a class of bis(trichloromethyl)S-triazine compounds. The method provides that benzonitrile compounds are used as starting materials, undergoing a cyclotrimerization reaction with trichloroacetonitrile, followed by a Knevengel reaction with benzaldehyde compounds to obtain bis(trichloromethyl)S-triazine compounds. The preparation method of this invention is simple, with easily controllable temperature and few impurities throughout the process; it significantly reduces costs and greatly improves purity and yield, achieving purities >99% and yields >70%; the products have good solubility; more importantly, almost all compounds exhibit more active inhibitory effects on HepG2 human liver cancer cells than the control cisplatin; making these compounds not only suitable as photochemical agents in the chemical industry but also beneficial for screening tumor therapeutic drugs.

This invention relates to the application of *Bifidobacterium longum* BL21 in the preparation of formulations to alleviate multi-organ damage induced by cisplatin chemotherapy, namely, a novel microbial strategy for preventing or alleviating multi-organ damage induced by cisplatin chemotherapy. This invention creatively discovers that *Bifidobacterium longum* BL21 can alleviate kidney damage, intestinal damage, and bone marrow suppression without interfering with the antitumor activity of cisplatin. Specifically, it can reverse the increase in serum creatinine and blood urea nitrogen levels caused by cisplatin chemotherapy, reverse the increase in inflammatory factor levels in kidney tissue caused by cisplatin chemotherapy, and alleviate oxidative stress damage in kidney tissue caused by cisplatin chemotherapy; it can reverse the increase in intestinal permeability caused by cisplatin chemotherapy, reverse the downregulation of intestinal tight junction protein expression caused by cisplatin chemotherapy, reverse the increase in serum endotoxin levels caused by cisplatin chemotherapy, and reverse the decrease in beneficial intestinal bacteria caused by cisplatin chemotherapy; it can improve hematopoietic dysfunction caused by cisplatin chemotherapy and restore white blood cell count.

This invention relates to the field of photodynamic therapy for keloids, and discloses a mitochondrial-targeted photodynamic keloid therapeutic agent based on platinum complexes and its application. The agent is prepared by coordinating the organic ligand TBQQ with an activated cisplatin derivative in a 1:1 molar ratio, followed by column chromatography purification to produce a high-purity TBQQPt powder with an active ingredient purity ≥98%. The prepared TBQQPt powder is then administered through a standardized drug formulation, intratumoral administration, and photo-activation process, combined with a multi-dimensional efficacy monitoring and safety evaluation system. Leveraging the D-A type planar square coordination structure of TBQQPt, which endows it with type I / II mixed photodynamic reaction characteristics, mitochondrial targeting, and photocatalytic oxidation of NADH, it synergistically exerts a dual effect of energy deprivation and genome disruption, effectively inducing mitochondrial dysfunction and apoptosis of keloid fibroblasts, and inhibiting their proliferation.

This invention belongs to the field of biomedicine and nanomedicine delivery technology, and relates to a precise renal-targeted delivery system for gambogeylic acid mediated by the β-lactoglobulin reabsorption mechanism, its synthesis method, and applications. The system comprises β-lactoglobulin-PEG-gambogeylic acid nanoparticles, containing β-lactoglobulin as a targeting carrier and gambogeylic acid as the active ingredient, covalently linked by a polyethylene glycol chain. This invention utilizes the suitable molecular size of β-lactoglobulin and its ability to be recognized and reabsorbed by the megalin / cubilin receptor system of renal tubular epithelial cells to construct a nanodelivery system that mimics the physiological process of endogenous protein "filtration-reabsorption." Experiments have shown that this system significantly improves the water solubility and biocompatibility of gambogeylic acid, enabling selective accumulation in the kidneys and efficient capture by renal tubular epithelial cells in vivo. It exhibits superior therapeutic effects in a mouse model of cisplatin- and glycerol-induced acute kidney injury, significantly outperforming the positive control drug NAC.

This invention discloses a novel application of undecanoic acid in inducing ferroptosis in laryngeal cancer cells and in the preparation of anti-laryngeal cancer drugs. For the first time, it was discovered that the known compound undecanoic acid can specifically target the mitochondria of laryngeal cancer cells, inducing mitochondrial structural damage and dysfunction. This, in turn, activates the ferroptosis pathway through multiple mechanisms, including increasing intracellular ferrous ion accumulation, increasing lipid peroxide levels, downregulating GPX4 / SLC7A11 expression, and upregulating ACSL4 expression, thereby effectively inhibiting the proliferation of laryngeal cancer cells. Based on this mechanism, this invention provides a pharmaceutical composition with undecanoic acid as the active ingredient, and its combined application with platinum-based drugs (such as cisplatin). This combined treatment exhibits a significant synergistic effect, particularly overcoming the platinum resistance of laryngeal cancer cells. This invention provides a novel drug selection and combination therapy strategy for the treatment and prevention of laryngeal cancer and precancerous lesions.

Acquired hearing loss due to chemotherapy or noise exposure is a major health problem, and Cisplatin chemotherapy often causes permanent hearing loss in cancer patients. However, there are no FDA-approved drugs for the treatment or prevention of Cisplatin- or noise-induced hearing loss. In one aspect, use of Niclosamide, Ingenol, and Elesclomol as an active agent to treat a hearing impairment and to prevent a hearing impairment, and methods of treating and / or preventing hearing impairments or disorders using the compositions are disclosed. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

This invention discloses an anti-drug-resistant lung cancer compound, its preparation method, and its applications. The invention involves reacting 5-chloro-8-hydroxyquinoline, dichloro(pentamethylcyclopentadienyl)rhodium(III) dimer, methanol, dimethyl sulfoxide, and triethylamine under sealed conditions at 80 °C for 3 days. After cooling to 37 °C, the mixture is filtered and dried to obtain the final product. The 5-chloro-8-hydroxyquinoline rhodium complex exhibits superior antitumor activity by targeting and inhibiting the growth of lung cancer cells A549 and cisplatin-resistant lung cancer cells A549 / DDP, while showing low toxicity to normal HL-7702 cells. It possesses potential pharmaceutical value and is expected to be used in the preparation of various antitumor drugs.

A benzimidazole heteroatom-containing spiro compound and a medicinal use thereof are provided. Activity test results show that the benzimidazole heteroatom-containing spiro compound provided by the present disclosure has a significant antiproliferative activity for human liver tumor cells HepG2, human colon cancer cells HCT116, and / or human gastric adenocarcinoma cells AGS, and most of the compounds involved in the present disclosure exhibit a stronger antiproliferative activity than cisplatin and / or Nutlin-3a. Therefore, the benzimidazole heteroatom-containing spiro compound provided by the present disclosure has a prospect of being developed into an antitumor drug, such as for liver cancer, colon cancer, or gastric cancer.

This invention discloses an aminothiourea iridium complex. It also discloses a method for preparing and applying a lysosomal-targeted iridium complex based on an aminothiourea ligand. The complex is constructed from a coumarin-thiourea ligand and an iridium dimer under alkaline conditions via in-situ isomerization and co-coordination. Under sodium bicarbonate regulation, the ligand undergoes intramolecular cyclization rearrangement to form a five-membered heterocyclic intermediate containing S and N atoms, which further rearranges with the iridium center to ultimately generate N. ^ S-type bidentate chelated semi-sandwich iridium complexes. The complexes described in this invention exhibit good chemical stability and significant antitumor activity, with inhibitory effects on tumor cells approaching or exceeding those of cisplatin. Furthermore, these complexes demonstrate lysosomal targeting properties, showing promising application prospects in anticancer drug development.

In the course of this invention, the inventors have demonstrated that intracellular ATP and mitochondrial membrane potential in cells isolated from hearing-impaired patients with BCAP31 gene mutations are significantly lower than in normal individuals. This finding indicates that hearing-impaired patients with BCAP31 gene mutations have significantly impaired mitochondrial function. Furthermore, increased susceptibility to cisplatin-induced cytotoxicity has also been demonstrated. On the other hand, treatment of lymphoid cell lines from these hearing-impaired patients with stem cell-derived isolated mitochondria has been shown to increase intracellular mitochondrial activity and reduce cisplatin-induced cytotoxicity. Moreover, it has been demonstrated that when stem cell-derived isolated mitochondria are applied to lymphocyte cell lines from hearing-impaired patients with ferredoxin reductase (FDXR) gene mutations, and to fibroblasts from hearing-impaired patients with mitochondrial gene mutations (m.A1555G), intracellular mitochondrial function is also restored. Therefore, the mitochondria according to the present invention can effectively alleviate or treat hereditary hearing loss.

This invention discloses the application of an inhibitor of the BEX4-XRCC5 interaction in the preparation of an anti-hepatoblastoma drug, belonging to the field of biomedical technology. The inhibitor, F35-303, specifically disrupts the direct interaction between BEX4 and XRCC5 proteins, inhibiting the DNA non-homologous end joining repair pathway, thereby targeting hepatoblastoma tumor stem cells and overcoming the limitations of existing therapies. It is particularly suitable for treating platinum-resistant or recurrent hepatoblastoma. The inhibitor is a small molecule compound named F35-303. This invention also provides pharmaceutical compositions containing this inhibitor and their combination therapy with platinum-based chemotherapy drugs (such as cisplatin), which can synergistically enhance efficacy and reduce toxic side effects. This invention provides a novel targeted therapy strategy for hepatoblastoma.

The present disclosure relates to a composition for preventing or treating lung cancer, comprising a compound isolated from a Cephalotaxus extract as an active ingredient. Isoharringtonine, which is the compound isolated from the Cephalotaxus extract according to the present disclosure, induces apoptosis and exhibits the effect of inhibiting the growth of non-small cell lung cancer cell lines, and thus can be useful in the prevention or treatment of lung cancer.In addition, the combined treatment of isoharringtonine and siNR4A1 enhances anticancer activity, and the combined treatment of isoharringtonine and cisplatin, which is a conventional anticancer drug, induces a high anticancer effect at a low concentration of cisplatin, thereby reducing side effects of anticancer treatment.

The application belongs to the technical field of microorganisms and relates to application of Bifidobacterium longum subsp. longum in preparation of a product for enhancing the antitumor effect of cisplatin, wherein the Bifidobacterium longum subsp. longum is Bifidobacterium longum subsp. longum BL21 strain with a preservation number of CGMCC No. 10452. The application overcomes the limited effect of cisplatin monotherapy due to an immunosuppressive tumor microenvironment, provides a safe, convenient and non-drug strategy, and synergistically amplifies the killing effect of cisplatin by activating host anti-tumor immunity.