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48 results about "Cisplatin resistance" patented technology

Vanadium-based nano-drug capable of reversing cisplatin resistance of multiple targets and preparation method thereof

The application discloses a vanadium-based nano drug capable of reversing cisplatin drug resistance through multiple targets and a preparation method thereof.The preparation method of the drug comprises the following steps: (1) preparation of mesoporous silica; (2) vanadium ion doping; (3) surface amino modification; (4) loading of a Pt(IV) prodrug; and (5) PDGF modification on the surface of the drug-loaded nanoparticles, thereby obtaining the vanadium-based nano drug.The vanadium-based nano drug prepared by the method has excellent performance, can reverse cisplatin drug resistance through multiple targets, and provides a new idea for constructing a lung cancer precision treatment scheme for reversing cisplatin drug resistance through multiple targets.
Owner:BINZHOU MEDICAL COLLEGE

Human bladder cancer cell line ZSZB1 and application thereof

The invention belongs to the technical field of biomedicine, and relates to a human bladder cancer cell line ZSZB1 with primary cis-platinum drug resistance and application thereof. The cell line is preserved in the China Center for Type Culture Collection (CCTCC), the preservation number is CCTCC No: C2024120, and the cell line is derived from a radical operation specimen of primary chemotherapy drug-resistant bladder cancer patients of Chinese population, and has stable in-vitro multiplication capacity and primary cis-platinum drug-resistant characteristic. The ZSZB1 provides an ideal experimental model for bladder cancer pathogenesis research, cis-platinum drug resistance mechanism exploration and novel antitumor drug screening. Establishment of the cell line can effectively promote transformation from basic research of bladder cancer to clinical application, and the cell line is of great significance to promotion of precise medical development.
Owner:LANZHOU UNIV

Application of small molecule compound in preparation of medicine for treating ovarian cancer

The invention discloses application of a small molecule compound in preparation of a medicine for treating ovarian cancer, and belongs to the technical field of biological medicine. The small molecule compound comprises a structure as shown in a formula (I) or an isomer, a pharmaceutically acceptable solvate or salt thereof, it is found for the first time that the small molecule compound can effectively reduce protein expression of YBX1, and meanwhile in-vitro verification experiments prove that the small molecule compound has a remarkable inhibition effect on proliferation of ovarian cancer cells. In addition, it is found that the small molecule compound can improve the cytotoxicity of cis-platinum and significantly enhance the anti-tumor effect of cis-platinum. The application of the small molecule compound YB-B1 targeting YBX1 in preparation of the medicine for treating the ovarian cancer is disclosed for the first time, a new method and a new idea are provided for clinical treatment of the ovarian cancer, and the small molecule compound YB-B1 particularly has remarkable significance in auxiliary treatment and prevention and treatment of cis-platinum drug-resistant ovarian cancer.
Owner:SHANDONG UNIV QILU HOSPITAL

Antibody for specifically recognizing 1147th acetylation of ribosome biosynthetic factor 1 protein as well as preparation method and application of antibody

The invention discloses an antibody for specifically recognizing 1147th acetylation of ribosome biosynthetic factor 1 protein as well as a preparation method and application of the antibody. According to the protein sequence and the modification type of the ribosome biosynthetic factor 1, two modified antigen polypeptides A and B are designed, and through detection, the antibody obtained by immunizing animals with the two polypeptides has high specificity and affinity, can accurately recognize the acetylation modification form of the 1147th site of BMS1, and avoids recognition of an unmodified form or other modification sites. The antibody is suitable for various immunological detection methods, is high in repeatability and low in background, has mass production potential, can realize industrialization, not only can be used for evaluating the cis-platinum drug resistance condition in esophageal cancer treatment, but also can be used for various scenes such as basic research, disease mechanism analysis, biomarker development and drug target screening, and is wide in application range.
Owner:SOUTHERN MEDICAL UNIVERSITY

Ruthenium complex for inducing mitochondrial DNA polycondensation to overcome tumor drug resistance, anti-tumor drug and preparation method and application thereof

The invention discloses a ruthenium complex for inducing mitochondrial DNA polycondensation to overcome tumor drug resistance, an anti-tumor drug and a preparation method and application of the ruthenium complex and the anti-tumor drug. The ruthenium complex is connected with a triphenylphosphine structure-modified bipyridine diazo-anthracene ligand through an alkyl chain, so that the fat solubility of the complex is improved, and the complex can enter cells more easily; the complex has a mitochondrial enrichment function and can be enriched in mitochondria; the complex induces mitochondrial DNA polycondensation so as to cause cancer cell death; the targeting property on tumor cells is effectively improved; the IC50 of the compound on human non-small cell lung cancer cell strains and cis-platinum drug-resistant strains thereof is far lower than that of cis-platinum, and the compound can be used as an excellent anti-tumor drug. The complex takes a ruthenium-coordinated ruthenium precursor compound as a raw material, and the raw material is economical and easy to obtain; the selectivity of the ruthenium complex can be improved, and the cost is saved.
Owner:GUANGDONG UNIV OF TECH

Application of copper carrier in medicine for enhancing drug resistance of copper death reversing liver cancer cells

The invention discloses application of a copper carrier in a medicine for enhancing drug resistance of copper death reversing liver cancer cells, and relates to the technical field of medicines. The copper carrier provided by the invention can activate copper death in cisplatin-resistant liver cancer cells in a manner of'three-arrow simultaneous shooting '. The method mainly comprises the following steps: increasing the number of copper ions entering cells (a first'arrow '), consuming GSH to reduce the loss of copper ions in the cells (a second'arrow'), and down-regulating the expression of ATP7B to inhibit the outflow of copper ions (a third'arrow '). Besides, the copper carrier down-regulates copper death related proteins (FDX1, DLAT, ATP7B and LIAS), also down-regulates drug resistance related proteins (ATP7B and P-gp), and shows a remarkable anti-liver cancer curative effect. Particularly, the bCCM can target mitochondria, improve the mitochondrial copper ion level, consume mitochondrial GSH and cause mitochondrial dysfunction mediated by copper death, and the bCCM and the cis-platinum have a remarkable synergistic effect and can reverse the drug resistance of the cis-platinum.
Owner:HUNAN UNIV OF CHINESE MEDICINE

Application of antibody for detecting phosphorylation of Tyr165 site of CPT1A protein in preparation of product for detecting sensitivity of head and neck squamous cell carcinoma to cis-platinum

The invention relates to application of an antibody for detecting phosphorylation of a Tyr165 site of CPT1A protein in preparation of a product for detecting the sensitivity of head and neck squamous cell carcinoma to cis-platinum. The CPT1A protein Tyr165 site is obtained through cisplatin stress and phosphorylation mass spectrometry identification, the phosphorylation level of the CPT1A protein Tyr165 site is increased along with the increase of cisplatin stress time, and the drug resistance degree of the head and neck squamous cell carcinoma to cisplatin is enhanced. Therefore, the CPT1A protein Tyr165 site is phosphorylated to serve as the biomarker of the cis-platinum drug resistance of the head and neck squamous cell carcinoma. The invention further provides a specific antibody for phosphorylation of the Tyr165 site of the CPT1A protein, the antibody is used for detecting whether the Tyr165 site of the CPT1A protein is phosphorylated or not, whether the head and neck squamous cell carcinoma has drug resistance to cis-platinum or not is determined, and a basis is provided for targeted selection of chemotherapeutic drugs for the head and neck squamous cell carcinoma.
Owner:SHANGHAI FIRST PEOPLES HOSPITAL

Application of DNASE1L3, CYP4B1 and / or FAM65B in enhancing nasopharyngeal carcinoma cis-platinum sensitivity

The invention discloses application of DNASE1L3, CYP4B1 and / or FAM65B in enhancing the cisplatin sensitivity of nasopharyngeal carcinoma, and belongs to the field of biological medicine. The invention proves that overexpression of the DNASE1L3 gene, the CYP4B1 gene and / or the FAM65B gene can obviously inhibit the activity of nasopharyngeal carcinoma cells and obviously enhance the sensitivity of the nasopharyngeal carcinoma cells to cis-platinum. An in-vivo xenotransplantation tumor model further proves that the in-vivo anti-tumor effect of the cis-platinum can be remarkably enhanced by combining the overexpressed DNASE1L3 gene, the CYP4B1 gene or the FAM65B gene with the cis-platinum, and tumor growth is effectively inhibited. The invention provides a brand new molecular target for overcoming the cisplatin resistance of nasopharynx cancer, provides a new strategy for preparing high-efficiency and low-toxicity nasopharynx cancer treatment drugs and cisplatin sensitizers, and has important clinical application prospects and market values.
Owner:CHANGSHA MEDICAL UNIV

Substituted benzenesulfonamide compound and application thereof

ActiveCN120504619AOrganic chemistryAmide active ingredientsPharmaceutical drugAntiproliferative effect
The invention relates to the field of medicinal chemistry, in particular to a substituted benzenesulfonamide compound and application thereof. Pharmacological experiment results show that the benzenesulfonamide compounds have strong inhibitory activity on GSTP1-1 protein, and part of the compounds have anti-proliferation effects on tumor cells of human lung cancer, cis-platinum drug-resistant lung cancer and the like, and have a certain degree of cis-platinum drug resistance reversing capability.
Owner:SHANDONG FIRST MEDICAL UNIVERSITY FIRST AFFILIATED HOSPITAL (QIANFO MOUNTAIN HOSPITAL OF SHANDONG PROVINCE)

Pharmaceutical composition for inhibiting growth of cisplatin-resistant tumors and application thereof

The invention belongs to the field of medicines, and discloses a pharmaceutical composition for inhibiting the growth of cisplatin-resistant tumors, which comprises a TGFR2 inhibitor, a PD-1 antibody and auxiliary components, and the auxiliary components are 2-amino-2-norbornic acid and / or 4-methylumbelliferone. The composition can effectively relieve the growth of the positive drug-resistant tumor of the Pars2 caused by cis-platinum, and experiments prove that the TGFR2 inhibitor, the PD-1 antibody and the auxiliary components have obvious synergy. In addition, the invention also discloses application of the composition.
Owner:HUANZHOU (GUANGDONG HENGQIN) BIOTECHNOLOGY CO LTD

Combined tumor marker for noninvasive detection of oral cancer and application thereof

The invention belongs to the technical field of biological medicine, and particularly discloses a combined tumor marker for noninvasive detection of oral cancer and application of the combined tumor marker. The invention provides application of a reagent for detecting a biomarker in preparation of a product for diagnosing or predicting oral cancer. The biomarker is an RBMX gene and / or an NEK2 gene. The invention finds that the two oral cancer carcinogenic key molecules are significantly highly expressed in oral cancer tissues, and the activity, migration and invasion ability of oral cancer cells can be inhibited by knocking down the expression of RBMX or NEK2, and the cis-platinum drug resistance of the oral cancer cells can be inhibited. According to the invention, RBMX or NEK2 is taken as a tumor marker to detect the oral cancer and has good diagnostic efficacy, and the RBMX and the NEK2 are combined for use, so that the sensitivity and the specificity of diagnosis can be further improved, and the risk of the oral cancer can be more comprehensively judged. The invention also provides application of the two pathogenic factors as inhibition targets in preparation of drugs for oral cancer.
Owner:HUNAN NORMAL UNIVERSITY

Composition for preventing or treating cisplatin-resistant cancer comprising DUSP23 expression or activity inhibitor as an active ingredient

PendingKR1020260115834ASOX2Inducer Cells
The present invention relates to a composition for the prevention or treatment of cisplatin-resistant cancer comprising an inhibitor of DUSP23 expression or activity as an active ingredient. It was found that DUSP23 expression is upregulated in cell clusters exhibiting characteristics of cancer stem cells, and that knocking down DUSP23 significantly reduces cell cluster formation as well as decreases the expression of SOX2, a major stem cell marker. Furthermore, DUSP23 expression was increased in lung cancer cells that had developed cisplatin resistance, and it was confirmed that the downregulation of DUSP23 inhibits self-renewal and invasive capabilities during the induction of cancer cell death. In addition, it was confirmed that DUSP23 plays an important role in promoting cancer stem cell characteristics through SOX2 expression. In conclusion, it has been shown that targeting DUSP23 can be a promising therapeutic strategy to overcome anticancer drug resistance in lung cancer, and the composition of the present invention is expected to be usefully utilized as a treatment for lung cancer cells with cisplatin resistance.
Owner:CHUNG ANG UNIV IND ACADEMIC COOP FOUND

Preparation method and application of nasal administration compound preparation for relieving cisplatin drug resistance

The invention discloses a preparation method and application of a nasal administration compound preparation for relieving the drug resistance of cisplatin, belongs to the field of precision medicine, and particularly relates to the nasal administration compound preparation for relieving the drug resistance of cisplatin. Comprising stem cell exosome, zanthoxylum polysaccharide, cis-platinum and normal saline, the stem cell exosome is a human adipose-derived stem cell exosome; the concentration of the human adipose-derived stem cell exosome is (2-5) * 10 < 7 > parts / mL. The nasal delivery compound preparation for relieving the cisplatin resistance has the advantages that the exosome is low in cytotoxicity and good in anti-tumor activity, the E2F8 / PDK1 axis can be adjusted, the cisplatin resistance of lung adenocarcinoma cells can be weakened, the lung adenocarcinoma cells can be effectively killed, the good lung adenocarcinoma treatment effect of the nasal delivery compound preparation is reflected, and the application prospect is wide. The compound is expected to be applied to development and use of medicines for clinically treating lung adenocarcinoma.
Owner:HANGZHOU LUOXI BIOTECHNOLOGY CO LTD

Novel human-derived distal bile duct cancer cell line with TP53 missense mutation and application of novel human-derived distal bile duct cancer cell line

The invention provides a novel human distal bile duct cancer cell line with TP53 missense mutation and application, the novel human distal bile duct cancer cell line CBC3T-3 is established, the cell line is preserved in the China Center for Type Culture Collection (the preservation number is CCTCC NO: C202555), the uniqueness and stability of the cell line are proved through STR typing and karyotype analysis, and the TP53 missense mutation novel human distal bile duct cancer cell line has the advantages that the TP53 missense mutation novel human distal bile duct cancer cell line CBC3T-3 can be used for preparing the TP53 missense mutation novel human distal bile duct cancer cell line CBC3T-3; and a plurality of driver gene mutations including TP53 missense mutation are carried. The CBC3T-3 has strong proliferation, invasion and migration capabilities, has high tumor formation rate in immunodeficient mice, is resistant to cis-platinum and sensitive to paclitaxel and gemcitabine, and provides an experimental basis for selection of clinical chemotherapy regimens. According to the model, the TP53 missense mutation type distal bile duct cancer in-vitro model is successfully established, and a key experimental platform is provided for deeply researching the drug resistance mechanism of the TP53 missense mutation type distal bile duct cancer and developing an individualized treatment strategy aiming at the subtype of the TP53 missense mutation type distal bile duct cancer.
Owner:THE FIRST HOSPITAL OF LANZHOU UNIV

Gold (I) complex containing alkyne ligand, preparation method of gold (I) complex and application of gold (I) complex in preparation of antitumor drugs

The invention discloses a gold (I) complex containing an alkyne ligand, a preparation method of the gold (I) complex and application of the gold (I) complex in preparation of antitumor drugs, the gold (I) complex has a structure as shown in a general formula I, a phosphorus ligand is selected from diphenyl-2-pyridine phosphine or tricyclohexylphosphine, and Rx is an organic group selected from a specific alkyne ligand; according to the preparation method, chloroauric acid is taken as an initial raw material, sequentially reacts with dimethyl sulfide and an organic phosphine ligand, and finally is coupled with an alkyne ligand under an alkaline condition, so that the steps are simple and convenient, the conditions are mild, and the yield is high; in-vitro activity experiments show that the complex shows remarkable proliferation inhibition activity on ovarian cancer, malignant melanoma, non-small cell lung cancer and cisplatin-resistant cell strains thereof, the effect of the complex is superior to that of cisplatin and auronafine, and a candidate compound is provided for developing a novel targeted anti-tumor drug for overcoming the drug resistance of platinum drugs.
Owner:THE AFFILIATED HOSPITAL OF SOUTHWEST MEDICAL UNIV

Use of alkaloid derivatives in the preparation of drugs against cisplatin-resistant non-small cell lung cancer

PendingCN122624483ATherapeutic effectOncology
The application discloses application of an alkaloid derivative or a medicinal salt thereof in preparation of a medicine for resisting non-small cell lung cancer cisplatin resistance, and a structure of the alkaloid derivative is as follows: The application finds that compound A45 can induce K48 connection type polyubiquitination of TNKS, and is degraded through a proteasome pathway, triggers a DNA damage response, activates a p53 pathway, and induces autophagic cell death, so that a specific action mechanism is achieved to achieve a treatment effect of resisting non-small cell lung cancer cisplatin resistance. Therefore, the compound A45 can be used as a candidate compound for the non-small cell lung cancer cisplatin resistance, a major treatment dilemma, has important development prospects and clinical application value, and provides a scientific basis and an experimental basis for development of an antitumor effect of other Aaptamine alkaloid derivatives and exploration of a strategy for overcoming the non-small cell lung cancer cisplatin resistance.
Owner:RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE +1

Nano-drug for oral cancer as well as preparation method and application of nano-drug

The invention belongs to the technical field of biological medicines, and particularly discloses a nano-drug for oral cancer as well as a preparation method and application of the nano-drug. The nano-drug provided by the invention is a drug-loaded mesoporous polydopamine nano-particle wrapped by a lipidosome modified by RGD peptide; wherein the load components of the mesoporous polydopamine nanoparticles comprise a cis-platinum drug and an RBMX gene expression inhibitor. The molecular RBMX related to regulation and control of oral cancer progress and cis-platinum drug resistance is screened, a nano biomimetic material drug loading system is constructed to load si-RBMX and cis-platinum to synergistically resist oral cancer treatment, and a novel nano drug with strong targeting property, good biological safety and excellent tumor lethality is obtained. The invention also provides a preparation method and application of the nano-drug.
Owner:HUNAN NORMAL UNIVERSITY

Application of 2-phenyl oxoindole in preparation of medicine for reversing cis-platinum drug resistance or treating tumors

The invention belongs to the technical field of tumor drug research, and particularly relates to application of 2-phenyl oxindole in preparation of a drug for reversing cis-platinum drug resistance or treating tumors. In-vitro experiments and in-vivo experiments prove that the 2-phenyl oxoindole can effectively inhibit proliferation of triple negative breast cancer cells and can remarkably improve the sensitivity of the cells to cis-platinum with a series of concentrations, and pathological staining results of visceral organs and tissues of mice show that the 2-phenyl oxoindole can effectively inhibit proliferation of the triple negative breast cancer cells and remarkably improve the sensitivity of the cells to cis-platinum with a series of concentrations. The 2-phenyl oxoindole does not cause obvious injury to main organs such as liver, kidney and the like.
Owner:THE FIRST AFFILIATED HOSPITAL OF MEDICAL COLLEGE OF XIAN JIAOTONG UNIV

Divalent platinum complexes and their derivatives, preparation methods, pharmaceutical compositions and uses

The present invention discloses a class of divalent platinum complexes containing non-steroidal anti-inflammatory drug structural units, their derivatives, preparation methods, pharmaceutical compositions and applications. The structure of this class of divalent platinum complexes is as follows: The derivatives of this class of divalent platinum complexes refer to isomers of the said divalent platinum complexes or mixtures thereof. When this class of divalent platinum complexes and their derivatives act on cancer cells, they can cause apoptosis by inducing DNA damage and the production of reactive oxygen species, and can also effectively inhibit the growth of cancer cells by down-regulating the expression of cyclooxygenase 2 to reduce inflammation. At the same time, this class of divalent platinum complexes with C=N double bonds can also target tumors using the acidic microenvironment of tumors, reduce tissue toxicity, show the characteristics of high efficiency and low toxicity in anti-tumor, and can overcome cisplatin resistance to a certain extent, and can be prepared into anti-tumor drugs. In addition, the synthesis method of this class of divalent platinum complexes is simple and easy to operate.
Owner:SOUTHEAST UNIV

Application of tripterine in preparation of bladder cancer resisting medicine

The invention discloses a new application of tripterine, namely application of the tripterine in preparation of bladder cancer resisting drugs, in-vitro cell experiments prove that the tripterine shows remarkable proliferation inhibition activity on various bladder cancer cell strains including cell strains UM-UC-3, TCCSUP and T24 and a cis-platinum drug-resistant strain T24CDDP, the median inhibitory concentration (IC50) of the tripterine is 0.2688-0.5870 mu M, and the tripterine shows remarkable proliferation inhibition activity on various bladder cancer cell strains including cell strains UM-UC-3, TCCSUP and T24 and a cis-platinum drug-resistant strain T24CDDP. The further mechanism research shows that the tripterine can regulate and control the cell cycle by down-regulating the expression levels of CDK1 and CDC5L proteins in bladder cancer cells and up-regulating the expression of phosphorylated p53 (p-p53) proteins at the same time, thereby playing a role in resisting bladder cancer; the invention provides a new effective candidate drug for clinical treatment of bladder cancer, especially cis-platinum resistant bladder cancer, and has important clinical application value.
Owner:KUNMING UNIV OF SCI & TECH

Engineered exosome targeting bladder cancer cells as well as preparation method and application of engineered exosome

The invention relates to an engineered exosome for targeting bladder cancer cells as well as a preparation method and application of the engineered exosome, and the engineered exosome is specific siRNA (small interfering Ribonucleic Acid) which is subjected to surface modification with concanavalin A and loaded with CASC11, and is marked as ConA-EXO-siCASC11. According to the invention, the engineered exosome is modified by ConA, so that the CASC11-siRNA is effectively delivered to the BLCA cells, the therapeutic effect of the CASC11-siRNA on the BLCA cis-platinum resistance is explored, an emerging therapeutic scheme is provided for the cis-platinum resistance BLCA, and the development of the field of precise treatment based on the engineered exosome is promoted.
Owner:SHANGHAI TONGJI HOSPITAL

Substituted benzenesulfonamide compounds and their applications

ActiveCN120504619BOrganic chemistryAmide active ingredientsPharmaceutical drugAntiproliferative effect
The present invention relates to the field of medicinal chemistry, specifically to a class of substituted benzenesulfonamide compounds and their applications. Pharmacological experiments have shown that the benzenesulfonamide compounds of the present invention have strong inhibitory activity against GSTP1-1 protein. Some compounds have anti-proliferative effects on tumor cells, including human lung cancer and cisplatin-resistant lung cancer, and have a certain degree of ability to reverse cisplatin resistance.
Owner:SHANDONG FIRST MEDICAL UNIVERSITY FIRST AFFILIATED HOSPITAL (QIANFO MOUNTAIN HOSPITAL OF SHANDONG PROVINCE)

An antibody specifically recognizing acetylation at position 1147 of ribosomal protein S6 kinase 1 and preparation method and application thereof

The application discloses an antibody capable of specifically recognizing acetylation of ribosome biogenesis factor 1 protein at the 1147th position, and a preparation method and application thereof. According to the protein sequence and modification type of ribosome biogenesis factor 1, two modified antigen polypeptides A and B are designed. It is detected that the antibody obtained by immunizing animals by using the two polypeptides has high specificity and affinity, and can accurately recognize the acetylation modification form of the 1147th position of BMS1, and avoid recognizing the unmodified form or other modification sites. The antibody is suitable for various immunological detection methods, has high repeatability, low background, has mass production potential, can be industrialized, and is not only used for evaluating the cisplatin resistance in esophageal cancer treatment, but also used for various scenes such as basic research, disease mechanism analysis, biomarker development, drug target screening, and has a wide application range.
Owner:SOUTHERN MEDICAL UNIVERSITY

Pt (IV) complex containing nitrogen donor, preparation method of Pt (IV) complex and application of Pt (IV) complex in preparation of antitumor drugs

The invention discloses a Pt (IV) complex containing a nitrogen donor, a preparation method of the Pt (IV) complex and application of the Pt (IV) complex in preparation of antitumor drugs, and belongs to the field of medicines. A Pt (IV) metal anticancer agent based on an N-containing donor (leflunomide) as an axial ligand for regulating and controlling the drug resistance of the liver cancer by constructing a LOXL3-DHODH axis signal channel is a complex 1 with a chemical structural formula shown as a formula I or a complex 2 with a chemical structural formula shown as a formula II; the complex 1 and the complex 2 have good cytotoxic activity on a cisplatin-resistant hepatoma cell line at a cellular level, and have lower toxicity on normal hepatoma cells than cisplatin. Therefore, the problems of toxicity and drug resistance of traditional platinum drugs can be effectively solved, and the anti-cancer effect of platinum-based drugs is improved. # imgabs0 #
Owner:HENAN UNIV OF URBAN CONSTR

Gold (I) complex containing benzene ring ligand, preparation method of gold (I) complex and application of gold (I) complex in preparation of antitumor drugs

The invention discloses gold (I) complexes containing benzene ring ligands, a preparation method of the gold (I) complexes and application of the gold (I) complexes in preparation of antitumor drugs. The gold (I) complex has a structure as shown in a general formula I, wherein Rx in the general formula I is a group containing a benzene ring; the preparation method comprises the following steps: enabling chloroauric acid to react with dimethyl sulfide to obtain an intermediate Au (Me2S) Cl, then enabling the intermediate Au (Me2S) Cl to react with an organic phosphine ligand to generate a phosphine-chlorine-gold intermediate, and finally enabling the phosphine-chlorine-gold intermediate to react with a sulfydryl ligand under an alkaline condition to obtain a target product. The series of complexes show remarkable proliferation inhibition activity on ovarian cancer cells, melanoma cells, non-small cell lung cancer cells and cis-platinum drug-resistant strains thereof in vitro, the effect of the complexes is superior to that of cis-platinum and Jinnofen, and candidate compounds are provided for developing novel anti-drug-resistant tumor drugs.
Owner:THE AFFILIATED HOSPITAL OF SOUTHWEST MEDICAL UNIV

Application of DNPEP inhibitor in preparation of medicine for reducing tolerance of cis-platinum to tongue squamous carcinoma cells

The invention relates to the technical field of tongue squamous cell carcinoma cis-platinum chemotherapy treatment, and provides application of a DNPEP inhibitor in preparation of a medicine for reducing the tolerance of cis-platinum to tongue squamous cell carcinoma cells. The DNPEP inhibitor is applied to preparation of the medicine for reducing the tolerance of the cis-platinum to the tongue squamous carcinoma cells, and the tolerance of the tongue squamous carcinoma cells to the cis-platinum is reduced by inhibiting expression of DNPEP in the tongue squamous carcinoma cells. The DNPEP can be used as a treatment target for overcoming the chemotherapy drug resistance of the tongue squamous carcinoma, and the DNPEP inhibitor and cis-platinum are combined for treating the tongue squamous carcinoma, especially for treating patients with cis-platinum resistance type tongue squamous carcinoma.
Owner:南昌大学第一附属医院

Au(II) dimers and methods of their use in cancer treatment

Synthesis and characterization of Au(II) dimeric complexes with pyridine dipyrrolinone (H2PyDP) ligands. Unique stability of these Au(II) dimers is disclosed when tested against thiol-containing reductants and other biomolecules. In addition, these complexes present antiproliferative activity at sub-micromolar levels in ovarian carcinoma cells, including cisplatin-resistant cells.
Owner:THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZONA

Platinum (IV) prodrug taking small molecule TrxR inhibitor as ligand as well as preparation method and application of platinum (IV) prodrug

The invention belongs to the technical field of medicinal chemistry, and particularly discloses a platinum (IV) prodrug with a small molecule TrxR inhibitor as a ligand and a preparation method and application of the platinum (IV) prodrug, the synthesized platinum (IV) prodrug shows good anti-proliferative activity on cancer cells such as MDA-MB-231, MCF-7, 4T1 and MDA-MB-231 / CDDP, and the anticancer activity of a compound 6b is optimal. In an in-vivo anti-tumor activity test, the compound 6b can effectively inhibit proliferation of cis-platinum sensitive and cis-platinum drug-resistant triple negative breast cancer xenotransplantation tumors, the tumor inhibition rates of the compound 6b are 73.8% and 66.3%, and the curative effect of the compound 6b is superior to that of a positive drug cis-platinum. In addition, the compound 6b can effectively inhibit proliferation of homotransplantation tumors of mouse breast cancer cells 4T1, and the tumor inhibition rate of the compound 6b is 76.8% and is obviously higher than that of a cis-platinum treatment group. And the compound 6b shows a powerful immunoregulation effect in vivo, which indicates that the design successfully realizes effective combination of chemotherapy and immunotherapy, and the compound disclosed by the invention has potential application prospects in treatment of triple negative breast cancer.
Owner:HUAIYIN INSTITUTE OF TECHNOLOGY

Application of a DCUN1D5 expression inhibitor in the preparation of cisplatin-resistant osteosarcoma drugs

The present invention relates to the field of bioengineering technology, and specifically to the use of a DCUN1D5 expression inhibitor in the preparation of a drug for cisplatin-resistant osteosarcoma. The present invention provides the use of a DCUN1D5 expression inhibitor in the preparation of a drug for cisplatin-resistant osteosarcoma, comprising a DCUN1D5 expression inhibitor. This invention establishes for the first time the key role of DCUN1D5 in osteosarcoma drug resistance and discovers the traditional Chinese medicine active ingredient, physalisin A, that selectively inhibits DCUN1D5. This ingredient not only synergizes with cisplatin to reverse cisplatin resistance in osteosarcoma but also provides a new target site and molecular marker for clinically predicting and improving patient treatment outcomes. This innovative strategy offers new hope for osteosarcoma treatment, particularly by providing a more effective solution to the problem of cisplatin resistance.
Owner:THE THIRD XIANGYA HOSPITAL OF CENT SOUTH UNIV +1

Fe (III)-nitroquinoline complex as well as preparation method and application thereof

The invention discloses design and synthesis of a novel lipophilic Fe (III) complex. The chemical formula of the complex is [Fe-5NO2-8HQ]. The Fe (III) complex shows strong in-vitro anticancer activity on various human tumor cells (including cis-platinum sensitive type and cis-platinum resistant type ovarian cancer cells); particularly, the compound still has a remarkable growth inhibition effect on platinum-resistant tumor cells, and shows the advantage of overcoming the drug resistance of cis-platinum. In addition, the [Fe-5NO2-8HQ] shows effective antibacterial activity on different strains of gram-positive pathogenic bacteria such as staphylococcus aureus and the like. Compared with a free ligand, the complex has the advantages that the antibacterial effect is greatly improved, and the complex is also applicable to drug-resistant strains. The preparation method of the complex is simple and efficient, and the product is stable and easy to separate. The complex can be used as an active pharmaceutical ingredient for preparing anti-cancer drugs and antibacterial drugs, and has potential application value in the aspects of anti-tumor treatment (especially aiming at drug-resistant tumors) and drug-resistant bacterial infection resistance.
Owner:SHENZHEN DAMEI KANGQIAO BIOMEDICAL CO LTD