161 results about "Nsclc cell" patented technology

The invention provides an alkaloid compound as well as a preparation method and an application thereof in tumor resistance. The alkaloid compound provided by the invention shows a remarkable cytotoxic effect on human non-small cell lung cancer cells A549, mouse lung adenocarcinoma cells Lewis, human triple negative breast cancer cells MDA-MB-231 and mouse breast cancer cells 4T1, and can be used for preparing medicines for treating breast cancer, lung cancer and the like.

The invention discloses a coumarin KRAS-G12C inhibitor as well as preparation and application of the coumarin KRAS-G12C inhibitor. The coumarin compound disclosed by the invention has a remarkable inhibition effect on non-small cell lung cancer cells (NCI-H23 and NCI-H358) with high expression of KRAS-G12C and pancreatic cancer cells (MIAPaCa-2), is particularly used for preparing medicines for treating and / or preventing non-small cell lung cancer and pancreatic cancer, and has a good prospect of development and application of antitumor medicines.

Disclosed is an anticancer composition using a flavone derivative. In the present invention, the flavone derivative exhibits cytotoxicity against: H827, H1299, H522, and A549, which are human non-small cell lung cancer cell lines; MCF-7, which is a human breast cancer cell line; and PANC-1, which is a human pancreatic cancer cell line, in a time-dependent manner and in a treatment concentration-dependent manner, and not only exhibits a synergistic effect when used in combination with other conventional anticancer agents, such as osimertinib, which is an anticancer agent targeting for lung cancer, tamoxifen, which is a hormone agent against breast cancer, and gemcitabine, which is a cytotoxic anticancer agent against pancreatic cancer, but also exhibits the effect of synergistically inhibiting the expression of HIF-1α when used alone or in combination with an existing anticancer agent.

The invention provides application of a copper death inducer in preparation of a medicine for treating osimertinib-resistant non-small cell lung cancer, and belongs to the technical field of treatment of non-small cell lung cancer. According to the invention, through high-throughput drug screening, the copper death inducer copper diethyl dithiocarbamate (CuET) and osimertinib are combined for use, so that a remarkable synergistic anti-cancer effect is achieved; furthermore, through detection of a wild type and osimertinib drug-resistant cell line model, an osimertinib sensitive and drug-resistant patient-derived organoid and a mouse xenotransplantation model, it is found that the anti-tumor effect of osimertinib can be remarkably enhanced through copper death induction, and osimertinib drug resistance is overcome. According to the technical scheme provided by the invention, osimertinib drug-resistant non-small cell lung cancer cells can be effectively killed, the curative effect of osimertinib in sensitive and drug-resistant models is remarkably enhanced, and an application scene is provided for copper death in tumor treatment.

The invention belongs to the technical field of biology, and discloses a bioactive peptide which is a micromolecular anti-tumor bioactive peptide derived from sea cucumber, and the amino acid sequence of the bioactive peptide is FNPDTFD. Sephadex G-15 gel chromatography and mass spectrometry technologies are used for separating, purifying and structurally identifying the sea cucumber flower enzymolysis peptide, so that the small molecule peptide with a potential anti-tumor effect is obtained. A cell viability experiment verifies that the small molecule peptide can selectively inhibit the proliferation of EGFR mutant non-small cell lung cancer cells. Besides, molecular docking and protein immunoblotting results show that the peptide can be combined with EGFR mutant protein, and the activation of a downstream Akt / mTOR signal channel is inhibited by targeting the EGFR mutant protein, so that the biological activity of resisting the non-small cell lung cancer is exerted. The bioactive peptide not only has the potential of being developed into a new generation of EGFR targeting antitumor drugs, but also has wide application prospects in the field of functional health food. The preparation process is simple, and is suitable for industrial production and market popularization and application.

The invention discloses an SOD2 knockout cell line and application of the SOD2 knockout cell line in anti-poxvirus, and relates to the technical field of antiviral research. According to the invention, sgRNA of targeted superoxide dismutase 2 (SOD2) is designed, the sequence of the sgRNA is shown as SEQ ID NO.1-SEQ ID NO.2, then a stable SOD2 knockout human-derived non-small cell lung cancer A549 cell line is established by combining CRISPR / Cas9 gene editing with a lentiviral vector delivery technology, single-cell cloning is obtained through multiple rounds of puromycin screening, and the SOD2 gene knockout A549 cell strain is successfully constructed. Vaccinia virus Tian Tan strain infection shows that the number of plaques of SOD2 knockout cells is obviously greater than that of the plaques (about 2.3 times) of normal cell infection, and the plaques are relatively large, so that fine SOD2 has the effect of limiting intercellular transmission of poxvirus. The invention lays a foundation for research and preparation of antiviral drugs.

The invention relates to a 5, 9-di-tert-butyl naphtho-indolizine phenothiazine compound as well as a preparation method and medical application thereof. The compound is efficiently synthesized through Ullmann coupling and palladium-catalyzed intramolecular arylation reaction. In-vitro anti-tumor activity research shows that the compound has remarkable selective inhibitory activity on various human tumor cell lines, and particularly, the inhibitory effect on non-small cell lung cancer A549 cells (IC50 = 0.21 mu M) is improved by two orders of magnitude compared with that of cis-platinum; iC50 (half maximal inhibitory concentration) of other cell lines are as follows: 1.26 mu M of prostate cancer PC-3 cells, 6.78 mu M of liver cancer HepG2 cells, 7.99 mu M of cervical cancer Hela cells and 25.46 mu M of breast cancer MCF-7 cells. Preliminary toxicity experiments prove that the compound has the characteristic of low cytotoxicity. The compound can be used as a novel high-efficiency low-toxicity anti-tumor lead compound, and provides an important structural basis for the development of anti-cancer drugs.

The invention discloses a polyketone compound derived from actinomycetes as well as a preparation method and application thereof, and relates to the technical field of microbial natural product mining and biological medicine, and the key point of the technical scheme is that the invention discloses a novel polyketone compound Strepactone derived from actinomycetes Streptomyces sp. DP0001, and the molecular formula of the novel polyketone compound Strepactone is C25H38O5. The compound is obtained through strain fermentation, ethyl acetate extraction and multi-step chromatographic purification, and the structure is identified through ESI-MS, 1H NMR and 13C NMR. Experiments show that Strepactone has an inhibition effect on staphylococcus aureus and methicillin-resistant staphylococcus aureus and has remarkable inhibition activity on human non-small cell lung cancer A549 cells, the half inhibitory concentration IC50 of the Strepactone is 5.36 mu M, and the Strepactone has no obvious cytotoxic activity on human embryo kidney cells 293T cells at the concentration of 30 mu M. The compound provided by the invention can be used for preparing anti-drug-resistant bacteria drugs and anti-human non-small cell lung cancer drugs, and also provides a structural basis for the development of novel antibacterial and anti-tumor leading drugs.

The invention discloses a capsaicin compound and a preparation method and application thereof, the molecular formula of capsaicin Capsivaryine is C16H21NO3, the chemical structure of capsaicin Capsivaryine is as follows, and the capsaicin Capsivaryine compound is a new compound reported for the first time and is prepared by taking mature and dry fruits of capsicum as raw materials through crushing, sieving, silica gel column treatment, D101 macroporous resin treatment and HPLC (High Performance Liquid Chromatography). The compound disclosed by the invention has a certain in-vitro inhibition effect on human breast cancer cells MCF-7, human liver cancer cells HEPG2, human non-small cell lung cancer cells A549 and human ovarian cancer cells SKOV3, and has no toxicity on human normal liver cells L02. The compound is a natural product which is novel in structure and good in activity, has great potential in the anti-tumor aspect, enriches diversity of pepper plants, and provides guidance for research of chemical components of pepper. # imgabs0 #

The invention relates to the field of biological medicines, and discloses application of patinopectin-like in preparation of a medicine for relieving and / or treating non-small cell lung cancer. Tests find that on the cellular level, the activity of non-small cell lung cancer cells can be reduced, cell migration can be inhibited, and the cell apoptosis process can be activated through treatment with the patinopectin-like; on the protein expression level, apoptosis-related protein can be remarkably activated, non-small cell lung cancer can be effectively treated by adjusting signal channels such as EGFR / PI3K / AKT, the possibility that tumor cells escape in treatment can be reduced, and therefore the clinical treatment efficiency is improved, and the application prospect is extremely good.

The invention discloses a novel pyrimidine KRAS-G12C inhibitor as well as a preparation method and application of the novel pyrimidine KRAS-G12C inhibitor. The pyrimidine compound disclosed by the invention has a remarkable inhibition effect on non-small cell lung cancer cells (NCI-H23 and NCI-H358) with high expression of KRAS-G12C, is particularly used as a medicine for treating and / or preventing the non-small cell lung cancer, is simple and efficient in preparation route, and has a good antitumor medicine development and application prospect.

The present application provides the use of raltitrexed in the manufacture of a medicament for the treatment of diseases caused by adenovirus infection, including but not limited to respiratory tract infection, gastrointestinal infection and keratitis caused by adenovirus. When raltitrexed was tested for its anti-adenovirus activity at the cellular level, using a viral infection dose of 100 TCID50, the viral infectivity was determined on a human non-small cell lung cancer cell line (A549 cell) model, and the results showed that raltitrexed had a significant inhibitory effect on adenovirus, with an EC 50 = 8.98 nM, a CC 50 > 187.5 nM, and it was found that it had a significant inhibitory effect on the entry of the virus into the cell; and in the hDSG2 mouse model, a significant inhibitory effect of raltitrexed on viral replication was also observed. Therefore, raltitrexed can be used to treat diseases caused by adenovirus infection.

The present application relates to the technical field of medicine (IPC classification A61P31 / 22), and particularly relates to a preparation method and application of a tetrahydroindazole antitumor compound, the preparation method comprising: reacting a compound of formula I with adamantanol to obtain a 4-(4-hydrazone-3,6,6-trimethyl-1-tetrahydroindazole)-2-(4-hydroxycyclohexylamino) benzamide compound, compared with a 4-(4-hydrazone-3,6,6-trimethyl-1-tetrahydroindazole)-2-(4-hydroxycyclohexylamino) benzamide compound in the prior art, the compound has stronger inhibition of tumor cell growth activity, has generally lower IC50 values, and in particular can significantly reduce the clonogenicity of non-small cell lung cancer at a low concentration, and causes apoptosis of non-small cell lung cancer cells, and has great significance for development of a novel antitumor drug.

The invention belongs to the field of gene engineering, and particularly designs oligonucleotide and application thereof in preparation of a medicine for treating osimertinib drug-resistant non-small cell lung cancer. Research finds that 3 'tRF-mtAsnGTT is highly expressed in osimertinib drug-resistant non-small cell lung cancer cells, and the inventor designs an effective oligonucleotide capable of specifically inhibiting the function of 3' tRF-mtAsnGTT, so that tumor cell proliferation is inhibited, cell apoptosis is promoted, and the drug sensitivity of the cells to osimertinib is remarkably improved. The invention provides a novel targeting strategy and application approach for molecular intervention and combined treatment of osimertinib resistance of non-small cell lung cancer.

The invention belongs to the technical field of biological medicine, and particularly relates to application of LncRNA as a non-small cell lung cancer biomarker and a treatment target spot, and the nucleotide sequence of the LncRNA is shown as SEQ ID NO. 1. Experimental results show that proliferation, survival and migration of non-small cell lung cancer cells can be prevented by inhibiting expression of the LncRNA, so that the LncRNA can be used as a non-small cell lung cancer biomarker and a therapeutic target.

The invention discloses a heterocyclic compound as well as a pharmaceutical composition and application thereof. Specifically, the present invention discloses a heterocyclic compound represented by formula (I), a pharmaceutically acceptable salt thereof, a solvate thereof or a solvate of the pharmaceutically acceptable salt thereof. The compound provided by the invention has inhibitory activity on proliferation of one or more of stably transfected cells Ba / F3 KRAS G12C, Ba / F3 KRAS G12D, Ba / F3 KRAS G12V, human pancreatic cancer cells Capan-1, human non-small cell lung cancer cells NCI-H358 (KRAS G12C mutation) and human metastatic pancreatic adenocarcinoma cells AsPC-1 (KRAS G12D mutation) containing KRAS mutation, or the compound provided by the invention has relatively weak inhibitory activity on proliferation of wild PC-9 cells of KRAS. # imgabs0 #

The present invention discloses a metal complex tailed with an immunologically active molecule, as well as its preparation method and application. The metal complex tailed with an immunologically active molecule exhibits significant anticancer activity. On the one hand, the metal complex exerts cytotoxicity against rapidly growing cancer cells through its active ingredient with anti-tumor immune efficacy. On the other hand, it can also induce immunogenic cell death, enabling the host immune system to attack tumor cells and induce a tumor-specific immune response. (The metal complex of the present invention has been shown to effectively induce immunogenic cell death in non-small cell lung cancer cells and successfully activate anti-tumor immunity in mice in vaccine experiments.) Therefore, the metal complex of the present invention has outstanding effects in anti-cancer, anti-inflammatory, inducing immunogenic cell death, and achieving anti-tumor immunity, and has broad application prospects.

Provided are methods for treating treatment-resistant non-small-cell lung cancer (NSCLC) in a patient in need thereof comprising administering a chimeric antigen receptor (CAR) cell therapy, antibody drug conjugate (ADC), or bispecific T cell engager (BiTE) targeting ALPP and / or ALPPL2 in the NSCLC cell, and / or a therapy targeting a genetic mutation selected from an EGFR mutation, a KRAS mutation, a RET mutation, an ALK mutation, a HER2 mutation, a MET mutation, a MEK mutation, an AKT mutation, an ERK mutation, a CDK4 / 6 mutation, a BRAF mutation, and an FGFR mutation.

The invention discloses an agonist of a retinoic acid receptor beta and application of the agonist in preparation of a non-small cell lung cancer medicine in the technical field of biological medicine. The agonist of the retinoic acid receptor beta is saturated odd fatty acid heptadecanoic acid C17: 0; according to the research, the expression of a retinoic acid receptor beta can be up-regulated by adding heptadecanoic acid into the NSCLC cells, so that the sensitivity of the NSCLC cells to retinoic acid treatment is improved. When heptadecanoic acid and retinoic acid are combined for use, the activity and migration ability of NSCLC cells can be further inhibited, and apoptosis of the cells is promoted. The result shows that the heptadecanoic acid plays an important role in controlling the sensitivity of the NSCLC cells to the retinoic acid, the combined use of the heptadecanoic acid and the retinoic acid provides a new drug treatment means for treating the NSCLC, and the heptadecanoic acid and the retinoic acid have potential application value in preparing the drug for treating the non-small cell lung cancer.

The invention discloses a nucleotide for inhibiting expression of ILKAP (Interleukin-7-Kinase Associated Protein) related circular RNA (Ribonucleic Acid) and application of the nucleotide, and the nucleotide is characterized in that the nucleotide sequence is CGUCAGUACUCGGGUUUCA, and the expression level of hsacirc0001116 can be specifically and obviously reduced. Experimental results prove that the nucleic acid molecule can effectively interfere with the expression of hsacirc0001116 in human non-small cell lung cancer A549 cells, and can significantly inhibit the survival of lung cancer cells. In addition, when the nucleic acid molecule is combined with an existing antitumor drug for use, a synergistic treatment effect can be generated.

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.

The present invention relates to the application of targeting the HNRNPC-HNF1A regulatory axis in the treatment of non-small cell lung cancer. The HNRNPC-HNF1A regulatory axis includes the HNRNPC gene and the HNF1A gene, and the nucleotide sequences of the mRNA of the HNRNPC gene and the mRNA of the HNF1A gene are shown in SEQ ID NO.1 and SEQ ID NO.2 respectively. The present invention discovers for the first time that simultaneously targeting and intervening the key genes of the HNRNPC-HNF1A signaling pathway shows a more effective anti-proliferation and anti-metastasis effect on non-small cell lung cancer compared with separately inhibiting the expression levels of the HNRNPC or HNF1A gene. The present invention designs siRNA (siMIX) that can specifically and efficiently knockdown the mRNA levels of HNRNPC and HNF1A. The results of cell function experiments show that when the same dose of siRNA is transfected into non-small cell lung cancer cells, siMIX has a better anti-cell proliferation, migration and invasion effect than siHNRNPC or siHNF1A. Therefore, targeted inhibition of the HNRNPC-HNF1A pathway axis can be applied to the research and preparation of anti-tumor drugs for non-small cell lung cancer.

The present application relates to a kind of anti-non-small cell lung cancer for strengthening healthy qi and resolving stasis and preparation method thereof, strengthening healthy qi and resolving stasis is made from the following weight proportion of raw medicinal materials: Ficus pumila 2g~50g / portion, radix pseudostellariae 2g~50g / portion, poria cocos 2g~50g / portion, atractylodes 2g~50g / portion, radix scutellariae 2g~50g / portion, oldenlandia 2g~50g / portion, cat's paw grass 2g~50g / portion, giant knotweed 2g~50g / portion, curcuma zedoary 2g~50g / portion, oyster 2g~50g / portion, platycodon 2g~50g / portion, mountain bitterling 2g~50g / portion, half branch orchid 2g~50g / portion. By cell test and the construction NSCLC osimertin drug resistance animal model prove, strengthening healthy qi and resolving stasis of the present application can adjust tumor microenvironment (TME) and inhibit non-small cell lung cancer cell growth of osimertin drug resistance. Not only this, strengthening healthy qi and resolving stasis of the present application can also inhibit common non-small cell lung cancer cell growth. While clinical observation finds, strengthening healthy qi and resolving stasis of the present application can improve insomnia, skin rash, diarrhea and other symptoms of lung accumulation (lung cancer, lung nodule) patient, improve its quality of life.

A method for improving the survival of a subject with cancer is disclosed, comprising applying an alternating electric field having a predetermined frequency and electric field intensity to a target site of the subject containing one or more cancer cells for a predetermined period of time, and administering the subject a therapeutically effective amount of a checkpoint inhibitor. A method for treating a subject with cancer is disclosed, comprising applying an alternating electric field having a predetermined frequency and electric field intensity to a target site of the subject containing one or more cancer cells for a predetermined period of time, and administering the subject a therapeutically effective amount of a checkpoint inhibitor. In some embodiments, the checkpoint inhibitor is nivolumab, pembrolizumab, or atezolizumab. Furthermore, a method for improving the survival of a subject with non-small cell lung cancer is disclosed, comprising applying an alternating electric field having a predetermined frequency and electric field intensity to a target site of the subject containing one or more non-small cell lung cancer cells for a predetermined period of time, and administering the subject a therapeutically effective amount of a checkpoint inhibitor. A method for treating a subject having non-small cell lung cancer is disclosed, the method comprising applying an alternating electric field having a predetermined frequency and electric field intensity to a target site of the subject containing one or more non-small cell lung cancer cells for a predetermined period of time, and administering to the subject a therapeutically effective amount of a checkpoint inhibitor. In some embodiments, the checkpoint inhibitor is ipilimumab (Yervoy), pembrolizumab (Keytruda), nivolumab (Opdivo), semiprimab (brand name Ributayo), dostallimab (Jemperli), atezolizumab (Tecentriq), durvalumab (Imfinzi), or avelumab (Bavencio).

The application relates to the technical field of aspirin pharmaceutical chemistry, in particular to an aspirin-sulfonamide hybrid, a preparation method and application thereof. The preparation method can synthesize a plurality of novel aspirin-sulfonamide hybrids by taking piperazine as a bridge, and by a three-step continuous method of "acyl chlorination, sulfonamidation and N-acylation" according to a "molecular hybridization principle". In the process, only one separation and purification is performed, and the preparation steps are simple. The aspirin-sulfonamide hybrid prepared by the method is most effective on human non-small cell lung cancer cells A549, and the activity is more than 33 times higher than that of a parent aspirin, and is similar to the activity of an anticancer drug irinotecan. The aspirin-sulfonamide hybrid 3k prepared by the method has a certain inhibitory effect on various cancer cells. The hybrid can induce human non-small cell lung cancer A549 cell apoptosis in a concentration-dependent manner, and can induce human non-small cell lung cancer A549 cell cycle arrest in the G0 / G1 phase, and inhibit cell growth.

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 invention discloses a semicarbazide derivative and its preparation method and application, which belongs to the technical field of anti-lung cancer targeted drugs. The semicarbazide derivative of the present invention can inhibit the growth of H1299 cells in a dose-dependent manner, but has little toxicity to normal lung epithelial cells BEAS-2B. The semicarbazide derivative of the present invention can significantly inhibit the cloning of non-small cell lung cancer cells A549 and H1299, so it has a significant inhibitory effect on the proliferation of non-small cell lung cancer. The semicarbazide derivative provided by the present invention can inhibit the protein expression of GPX4 in non-small cell lung cancer A549 cells, and by inhibiting the protein expression of GPX4, promote the ferroptosis of non-small cell lung cancer cells, thereby playing a role in suppressing tumors.

The invention relates to the field of pharmaceutical preparations, and provides a TPGS modified CPD12C15 liposome as well as a preparation method and application thereof. The TPGS-modified CPD12C15 liposome is of a vesicle-shaped structure and comprises a lipid bilayer membrane which is of a closed membrane structure jointly formed by DPPC, SPC and cholesterol and forms a basic skeleton of the vesicle, and a TPGS-modified CPD12C15 liposome which is of a vesicle-shaped structure. The surface modification layer is formed by TPGS on the surface of the lipidosome, the hydrophobic end of the TPGS is inserted into the outer layer of the lipid bilayer membrane, and the hydrophilic end of the TPGS extends and is exposed on the outer surface of the lipidosome; and an internal aqueous phase, an aqueous chamber surrounded by a lipid bilayer, in which the active ingredient CPD12C15 is encapsulated; the structure of the CPD12C15 is # imgabs0 #. The liposome is prepared through a calcium acetate gradient method, the encapsulation efficiency reaches up to 79.84%, the drug loading capacity reaches 17.24%, the particle size is about 91 nm, and the PDI is lower than 0.2. The combination of the liposome and copper ions shows an excellent inhibition effect on non-small cell lung cancer cells, the IC50 value is 0.1331-0.199 [mu] mol / L and is far lower than that of docetaxel, and the multi-drug resistance of tumors can be effectively overcome.

The invention relates to the technical field of biological medicines, in particular to gold nanoparticles modified by arylamine derivatives as well as a preparation method and application of the gold nanoparticles. The gold nanoparticles modified by the arylamine derivatives provided by the invention can improve the endoplasmic reticulum stress level of non-small cell lung cancer cells, can also improve the sensitivity of the non-small cell lung cancer cells to chemotherapeutic drugs, and can improve the death rate of the non-small cell lung cancer cells in cooperation with the chemotherapeutic drugs.