12 results about "Colonic Carcinoma" patented technology

The invention relates to the technical field of biomedicine, in particular to a novel target spot for resisting chikungunya virus infection and application. According to the invention, human colon cancer cells (HCT116) are taken as target cells, and retinoic acid-induced protein expression of the target cells is reduced by adopting a gene knockout technology, so that host factors capable of effectively inhibiting CHIKV infection of the human colon cancer cells are found, and the purpose of blocking CHIKV infection from the source is achieved. It is found that retinoic acid induced protein 16 (RAI16) plays an important role in CHIKV infected HCT116 cells, and CHIKV infection can be obviously promoted by down-regulating expression of RAI16. The invention provides an application of RAI16 in preparation of a medicine for preventing or treating chikungunya virus infection, and provides a new target spot and a treatment scheme for clinically preventing and treating fever, arthralgia, arthrocele, muscular pain, headache, nausea, fatigue, rash and other diseases caused by CHIKV infection.

The invention belongs to the technical field of biological pharmacy, and particularly relates to polylysine nanoparticles for delivering oxaliplatin and a preparation method of the polylysine nanoparticles. The invention discloses a preparation method of polylysine nanoparticles for delivering oxaliplatin. The polylysine nanoparticles are applied to preparation of a tumor targeting drug mPssPC-OXA NPs with small particle size, positive surface charge and excellent stability. The mPssPC-OXA NPs can respond to a tumor microenvironment with high GSH concentration to quickly release a drug, and shows an excellent HCT-116 cell uptake effect and an effective RAW264.7 cell immune escape effect in an in-vitro anti-colon cancer cell test. In addition, the mPssPC-OXA NPs also shows more remarkable cytotoxicity, cell migration inhibition, cell proliferation inhibition and HCT-116 cell apoptosis induction effects compared with free OXA.

The application discloses a class of podophyllotoxin triazole ether derivatives, a preparation method and application thereof, belongs to the technical field of chemical pharmacy, and particularly relates to a class of podophyllotoxin triazole derivatives and application thereof in preparation of antitumor drugs. The application combines a triazole structure with a podophyllotoxin parent body by using a click chemistry reaction, designs and synthesizes a series of novel 1,2,3-triazole podophyllotoxin derivatives, optimizes the kinetic characteristics of the podophyllotoxin by introducing the triazole structure, and improves the anticancer effect and drug property. Molecular docking shows that the series of compounds have strong binding energy on AKT1 and tubulin, can target inhibit tubulin / AKT1, and in-vitro antitumor activity research shows that the molecules have strong inhibitory activity on the proliferation of human colon cancer cell strains, and can provide a new strategy for structural derivatization of podophyllotoxin.

The present invention relates to a 2-amino-substituted derivative (Formula I) or an ethylenediamine-substituted derivative (Formulas II and III) of hypocrellin as a photodynamic drug for treating the following tumors: esophageal cancer, gastric cancer, lung cancer, liver cancer, cholangiocarcinoma, colon cancer cells related to digestive tract tumors; brain cancer, head and neck cancer, tongue cancer, nasal cancer, oral cancer, glioblastoma cells related to head, neck and facial tumors; basal cell carcinoma, squamous cell carcinoma, cutaneous T-cell lymphoma, melanoma cells related to skin tumors; prostate cancer, bladder cancer cells related to genitourinary tumors. At the same time, such derivatives can localize the location of tumor tissues through their own fluorescence and are used for fluorescence-guided surgical resection of tumors.

The present invention belongs to the technical field of pharmaceutical chemistry, and specifically relates to a polyethylene glycol-Rakicidin B1 derivative, and further discloses its preparation method and application. The polyethylene glycol-Rakicidin B1 derivative of the present invention connects polyethylene glycols with different degrees of polymerization to the structure of the Rakicidin B1 esterified derivative through click chemistry reactions, realizing the structural modification of the Rakicidin B1 compound, and effectively solving the problem that the poor solubility of existing Rakicidins compounds and esterified derivatives affects their applications. The activity of the polyethylene glycol-Rakicidin B1 derivative of the present invention shows that the derivative has obvious anti-neuroinflammatory effects, and also has certain in vitro inhibitory effects on human colon cancer cells HCT-8 and human pancreatic cancer cells PANC-1 under normoxic and hypoxic cultures.

A sesquiterpene acyl glycoside in rhizoma artemisiae japonicae and preparation method and application thereof. The present application belongs to the technical field of medicine, and relates to extraction and separation of a sesquiterpene acyl glycoside compound rhizoma artemisiae japonicae cembranoid I from rhizome of rhizoma artemisiae japonicae by using macroporous resin, silica gel and preparation chromatography and the like, and the preparation method is simple and easy to implement. 23 H 38 O 10 In vitro human cancer cell inhibition activity research shows that the compound has anticancer activity, including obvious inhibition on human colon cancer cells HT-29 and human breast cancer MCF-7 cells, and is expected to be developed into a new anticancer drug.

The invention discloses an electrochemical synthesis method and anticancer activity of aryl alkyl ketone, and belongs to the field of organic synthesis. A carboxylic acid derivative and a Katritzky salt are respectively used as an acyl electrophilic reagent and an alkyl free radical precursor, in the presence of a catalyst Ni (dme) Br2 and a ligand 2, 2 '-dipyridyl, a single electrolytic tank performs constant-current electrolysis, reductive coupling of the Katritzky salt and the carboxylic acid derivative is realized, the aryl alkyl ketone compounds with diversified structures are synthesized, and the highest yield is 86%. The method is mild in reaction condition, short in reaction time, good in functional group compatibility and wide in substrate application range; meanwhile, the synthesized compound has the activity of obviously inhibiting HCT-116 cancer cell proliferation, so that the compound has the anti-cancer activity on colon cancer and has potential medicinal value.

The invention discloses trifluoromethyl substituted indolinone compounds as well as a synthesis method and application thereof, and belongs to the technical field of medicine synthesis. An N-phenylpyridine-2-amine compound and a trifluoromethyl imine sulfoxide ylide compound are used as initial raw materials, the trifluoromethyl substituted indolinone compound is synthesized through a one-pot cascade reaction, and the process is simple and efficient; raw materials are cheap and easily available, reaction conditions are mild, and operation is simple; the substrate is wide in application range, and the functional group tolerance is good. An anti-cancer cell activity test verifies that the compound provided by the invention has the activity of obviously inhibiting proliferation of three cancer cells, namely Hela, A549 and HCT-116, so that the compound provided by the invention has the anti-cancer activity on cervical cancer, lung cancer and colon cancer, has potential medicinal value and provides a new structural unit for drug screening.

The invention discloses a benzo-aza compound as well as a preparation method and application thereof. The benzazepine compound and the pharmaceutically acceptable salt of the benzazepine compound prepared by the invention have relatively high sensitivity and very strong cytotoxic activity to human colon cancer cells HCT116 tumor cells. The triethylene diamine catalyst is adopted in the process of preparing the benzo-aza compound, the reaction conditions are relatively conventional, the reaction process is mild, simple and convenient, the operation is easy, the cost is low, and the method is suitable for industrial large-scale production; according to the method, various substrates are used as reactants, products with various and complex structures are obtained, the yield is high, and the application range of the method is widened. The compound prepared by the preparation method disclosed by the invention has relatively high cytotoxic activity on human colon cancer cells HCT116. Therefore, the preparation method provided by the invention can provide a basis for screening the benzazepine compound with good activity on tumor cells, and is beneficial to further screening out compounds with more excellent biological activity.

The application discloses a chiral imide derivative and a preparation method and application thereof. A simple synthesis method of NHC catalyzed imine and MBH carbonate is designed, and a chiral imide derivative is efficiently constructed by one-step method. Biological activity evaluation is carried out on the compounds, and the inhibition rates of all the compounds on three tumor cells, human lung cancer cells A549, human colon cancer cells LOVO and SW620, are enhanced with the increase of concentration, wherein, the compounds 3g, 3i, 3j and 3o show better inhibition effect on the three tumor cells, the inhibition rate of the compound 3g on the A549 cells reaches 50% at a concentration of 12.5 μg / ml, and the inhibition rates of the compounds 3i, 3j and 3o on the A549 cells are all above 70% at a concentration of 50.0 μg / ml, and the inhibition rate of the compound 3j on the A549 cells reaches 85.8%, so the compound 3j has the value of further development and research.

The invention discloses a trifluoromethyl-containing isoxazolidine compound as well as a synthesis method and pharmaceutical application thereof, and belongs to the technical field of pharmaceutical synthesis. Beta-trifluoromethyl-alpha, beta-unsaturated ketone compounds 1 and N-benzyl nitrone 2 are used as raw materials, and in the presence of chiral binaphthol ligands or tetrabenzocyclooctadiene ligands, triphenyl borate and molecular sieves, asymmetric [3 + 2] cycloaddition reaction is performed to obtain the optically active trifluoromethyl-containing isoxazolidine compounds 3. The synthesis route has the advantages of easily available raw materials, mild reaction conditions, high catalytic efficiency and the like, and the obtained product shows remarkable physiological activity on cervical cancer C33A, lung cancer A549, breast cancer MCF-7, colon cancer HCT116 cells and the like, and provides an effective way for development of novel anticancer lead compounds.

The present application relates to a kind of preparation of trifluoromethyl camptothecin compound and its use in antitumor drugs, the structural formula of the compound is shown as follows.In vitro cytotoxic activity screening results show that trifluoromethyl camptothecin compound has broad-spectrum antitumor activity, to human hepatocellular carcinoma cell (HepG2), human non-small cell lung cancer cell (A549), human colon cancer cell (SW480), human cholangiocarcinoma cell (QBC939), human breast cancer cell (MCF-7), human pancreatic cancer cell (PANC-1), human pancreatic cancer cell (BxPC-3) shows strong inhibitory activity.4 trifluoromethyl camptothecin compounds I, II, III, IV all show strong inhibition to the 7 tumor cell lines measured, IC 50 Value is 0.503-0.0112 μM, 4.8477-0.6516 μM, 1.825-0.0005 μM and 4.9043-0.4612 μM, all significantly better than control drug topotecan. Among them, the compound shows the strongest inhibitory activity to BxPC-3 cell line, IC 50 Value is in the range of 0.6516-0.0005 μM. Therefore, trifluoromethyl camptothecin compound is expected to be developed into a new antitumor drug.