43 results about "DU145" patented technology

The invention relates to a crown ether cyclic quinazoline derivative and medicinal salts thereof using in tumor therapy and imaging. The crown ether cyclic quinazoline compound is characterized in that a 2-, 3-, 4- substituted aniline is disposed at one end; a 6-, 7- substituted crown ether cyclic quinazoline structure is disposed at the other end; the substituent group R1 is located on the fourth-position aniline of a quinazoline mother ring and is 2-, 3-, 4- substituted alkoxy; and the crown ether cycle is located at the 6, 7 position of the mother ring, and is a 9-crown-3, 12-crown-4 and 15-crown-5, and the structural formula is formula I. The experimental result of antitumor activity in vitro of nonradioactive isotope labeling compounds shows that the compounds are good in inhibitory effect for four kind of cancer cells namely HepG2, A549, sy5y and DU145, and have the potential as cancer treatment medicine; and the body distribution experiment of 18F or 125I labeling compounds show that the compounds are higher in ingestion and certain detention in tumors and faster in blood clearance and have potential applied to tumor imaging.

The invention provides a substituted benzofuran derivative. A chemical structure of the derivative is as shown in general formula I. The invention further provides a preparation method of the formulaI, the preparation method is as shown in the following reaction formula described in the specification, wherein R and R' are defined the same as the specification. In-vitro proliferation inhibition experiment researches of human tumor cells show that the substituted benzofuran derivative has excellent inhibition effects on tumor cells such as human hepatoma cells HLF, human intestinal cancer cellsHCT116, human breast cancer cells MDA-MB-231, human prostate cancer cells DU145, human melanoma cells A375, human colon cancer cells Lovo, human kidney cancer cells 786-o, human chronic myeloid leukemia cells K562, human gastric cancer cells MGC-803, human pancreatic cancer cells PANC-1, can be used for preparing an anti-tumor drug, has low acute toxicity and good water solubility, and has good clinical application prospects. The preparation method provided by the invention is suitable for industrial production.

The invention discloses application of a bixanthone compound FLBG-1108 or its medicinal salt in preparing anticancer medicaments. The invention, by means of experiments, finds that the bixanthone compound FLBG-1108 has an obvious inhibition effect on propagation of human non-small cell lung cancer H520, A549, H549, 1299, human breast cancer cell MCF7, human prostatic cancer cell PC3, LNcaP, DU145, as well as human intestinal cancer cell SW480 and HT-2P, can selectively inhibit the propagation of the human lung cancer cell H520, and presents good time and concentration dependence. After 48h of action, the IC50 value is 2.90 micrometers, which shows no cytotoxicity to a normal kidney epidermal cell. Further, the bixanthone compound FLBG-1108 is found to play an effective role in inducing apoptosis of the lung cancer cell H520, preventing propagation of cancer cells but showing no toxicity, and can specifically block the cell cycle of the lung cancer cell H520 in S stage, thus inhibiting the propagation of cancer cells. Therefore, the bixanthone compound FLBG-1108 can be developed into novel candidate medicaments with an anticancer effect, especially an anti-lung cancer effect.

The invention relates to the technical field of medicines, and in particular to an application of nano-microsphere containing orlistat in preparing antineoplastic drugs. The nano-microsphere consistsof the orlistat as well as any copolymer which is selected from a vitamin A methacrylate-2-methacryloyloxyethyl phosphorylcholine copolymer, a vitamin E methacrylate-2-methacryloyloxyethyl phosphorylcholine copolymer and a vitamin D methacrylate-2-methacryloyloxyethyl phosphorylcholine copolymer. Based upon in vitro test results, it is indicated that antineoplastic activity of the nano-microsphereprovided by the invention on human prostate cancer cells DU145, human melanoma cells A375 and human pancreatic cancer cell lines bxpc-3 is obviously higher than that caused by independent administration of the orlistat, and the antineoplastic activity is better than that of control nano-microsphere which is prepared by taking PMB30 as a carrier as well as nano-microsphere which contains the orlistat and polyethylene glycol-polycaprolactone.

The invention discloses an aegiceras corniculatum stem ethyl acetate extract and a preparation method thereof. The method includes: soaking aegiceras corniculatum stems into ethanol to obtain aegiceras corniculatum stem ethanol extract; after volatilization of ethanol in the aegiceras corniculatum stem ethanol extract, adding petroleum ether for extraction to obtain a lower water phase; adding ethyl acetate into the lower water phase, continuing extraction to obtain upper ethyl acetate part extract, and performing water bath drying to obtain the aegiceras corniculatum stem ethyl acetate extract. According to in-vitro molecular biological experiment researches, the aegiceras corniculatum stem ethyl acetate extract has an anti-proliferation effect on human prostatic cancer cells PC3 and DU145 and is capable of evidently inhibiting clone formation of the human prostatic cancer cells PC3 and DU145. Therefore, the aegiceras corniculatum stem ethyl acetate extract has a potential application prospect in preparation of medicines for treating prostatic cancer and can be used for preparation of the medicines for treating prostatic cancer. Deeply developing the aegiceras corniculatum stem ethyl acetate extract can expand an aegiceras corniculatum utilization range to create a novel approach for cancer treatment.

The invention provides a lead compound for a targeted human FKBP51 protein and a screening method and application thereof, belonging to the technical field of biochemical pharmacy. According to the lead compound and the screening method and application thereof, an FK1 structural domain of FKBP51 is used as a receptor; FK506 of the FKBP51 is selected to be combined with a sack; molecular docking is performed by using a Glide program; 150 small molecular compounds are obtained by virtual screening from more than 1.5 million of compounds and are used for fluorescence quenching experiments; according to the experiments, a combination action of the compounds and the FK1 is verified, and the binding property of a target protein and compounds with a strong docking effect is researched; two kinds of cells LNCaP and DU145 are selected to verify the cell viability of screened small molecular compounds resisting prostate cancer; meanwhile, the structural biology research on a compound formed by the FKBP51 and small molecular lead compounds is performed. According to the lead compound provided by the invention, a cell model and a mouse model of CRPC (Castration Resistant Prostate Cancer) are established, the effectiveness of the lead compound to the CRPC is evaluated, and an action mechanism and a rule of the lead compound and the target protein are explained at the molecular level; a foundation is provided for researching and developing new drugs for treating common prostate cancer and the CRPC.

The invention discloses an application of bixanthone compound FLBG-1108 or its pharmaceutical salts in the preparation of anti-cancer drugs. It is found in the invention through experiments that the bixanthone compound FLBG-1108 has an obvious inhibitory effect on the multiplication of human non-small cells lung cancer cells H520, A549, H549, 1299, a human breast cancer cell MCF7, human prostatic cancer cells PC3, LNcaP, and DU145 and human intestinal cancer cells SW480 and HT-2P. The multiplication of human lung cancer cells H520 can be inhibited selectively by the bixanthone compound FLBG-1108. The good time and the concentration dependence can be presented. The value of IC50 after 48 h action is 2.90 muM. The cytotoxicity is not expressed at this concentration on normal renal epidermal cells. Further, the bixanthone compound FLBG-1108 can effectively induce the apoptosis of lung cancer cells H520 and prevent the multiplication of cancer cells. Meanwhile, no toxicity will be presented. The bixanthone compound FLBG-1108 can specifically interdict the cell cycle of lung cancer cells H520 in S phase and can therefore inhibit the multiplication of cancer cells. Therefore, the bixanthone compound FLBG-1108 can be developed into a new candidate drug with an anti-cancer effect especially an anti-lung cancer effect.

The invention discloses the application of a saccharide coupled-1, 2, 3-triazole substituted polycyclic aromatic hydrocarbon derivative in the preparation of an anti-cancer drug. The structure of thesaccharide coupled-1, 2, 3-triazole substituted polycyclic aromatic hydrocarbon derivative is shown as the formula (I). A pharmacology experiment proves that the saccharide coupled-1, 2, 3-triazole substituted polycyclic aromatic hydrocarbon derivative has different degrees of inhibiting effects on lung cancer (H460), gastric cancer (HGC27), myeloma (H929), cervical cancer (Hela), liver cancer (HepG2), prostatic cancer (DU145) and colon cancer (HT29).

The invention discloses a construction method and application of a human prostate cancer radiation tolerance cell strain. The method comprises the following steps: taking a human prostate cancer cell strain DU145 in an exponential growth phase, and inoculating the human prostate cancer cell strain DU145 into a 60mm culture dish according to the density of 5 * 10<5> cells per dish; when the cells grow to 60%, carrying out X-ray irradiation, wherein the irradiation dose is 4Gy; continuously culturing the cells until the density reaches 90%, digesting with pancreatin, counting, and inoculating into a 60mm culture dish according to the density of 5 * 10 <5> cells per dish; repeating the steps of irradiation and culture, and continuing stable passage for 30 days when the accumulated irradiation dose of the cells reaches 60Gy; and after the human prostate cancer radiation-tolerant cell strain which grows stably, is subjected to passage and is resuscitated is obtained, cryopreservingthe cells in a liquid nitrogen tank in time. Small-dose X-rays are selected for cell irradiation, and the method is characterized in that the clinical radiation treatment process is simulated, the irradiation dose is small, the cell survival rate is high, and the cell drug resistance is stable.

The invention provides a compound having a general structure formula 1, and a preparation method and applications thereof in preparation of antitumor drugs. The PSMA activated prodrug CPT-HT-J-ZLn shows strong cytotoxic selectivity on tumor cells with PSMA positive expression and PSMA negative expression and is more active to tumor cells LNCaP-FGC with PSMA positive expression than to tumor cellsPC-3, DU145, HepG2, Hela and MCF-7 with PSMA negative expression; and the activity of the compound CPT-HT-J-ZLn12 to the LNCaP-FGC (IC50=1.00+/-0.20 [mu]M)(PSMA<+>) respectively is 40, 40, 21, 5 and 40 times that of the cells HepG2 (IC50>40.00 [mu]M), Hela (IC50>40.00 [mu]M), MCF-7 (IC50=21.68+/-4.96 [mu]M), DU145 (IC50=5.40+/-1.22 [mu]M) and PC-3 (IC50=42.96+/-3.69 [mu]M) with PSMA negative expression.

Glycosylated Antitumor Ether Lipids (GAELs) kill cancer cells by a nonapoptotic pathway which is an attractive strategy to avoid resistance. To further optimize the antitumor effect, we prepared various analogs of di-, and tri-cationic GAEL analogs differing in the nature of the sugar (D-giucose or L-glucose), the anomeric linkage as well as position of the glycerolipid moiety. The di- and tri-cationic GAELs were synthesized and their in vitro anticancer properties were evaluated against drug resistant and aggressively growing cancer cell lines derived from human breast, prostate, pancreatic and ovarian cancers. The most potent dicationic GAEL analogs were also studied against cancer stem cells obtained from breast BT 474, prostate DU145 and ovarian A2780cp cell lines. Our results indicate that the number of positive charges, the position of the amino substituents and the nature of the sugar have significant effects on the anticancer activities of these compounds. The most active analog kill 50% of the cells at concentration range of 0.5-5 μM and 90% of the cells at the concentration of 1-10 μM depending on type of cancer cells.

The invention relates to an application of circular RNA-circEXOC6B (Ribonucleic Acid-CircEXOC6B) in inhibiting metastasis of prostatic cancer. Low expression of circEXOC6B in prostate cancer cells and prostate cancer tissues is found for the first time, stable transfection prostate cancer DU145 and PC-3 cell lines of the over-expressed circEXOC6B are further constructed, cell Transwell migration experiments and invasion experiments find that the over-expressed circEXOC6B can significantly inhibit migration and invasion of prostate cancer cells, in addition, a nude mouse pulmonary metastatic tumor model is constructed, and the model is used for screening prostate cancer cells and prostate cancer tissues. It is found that when the circEXOC6B overexpressed DU145 cells are injected into nude mouse bodies through caudal veins, in-vivo prostatic cancer metastasis can be remarkably inhibited. Therefore, circEXOC6B can be used as a new therapeutic target for prostatic cancer, and reference is provided for development of prostatic cancer drugs.

The invention provides novel application of Java brucea fruit oil emulsion injection to the anticancer aspect, in particular to novel application to the anti-leukemia aspect. The invention respectively uses humanized leukemia U937, NB4 and HL-60 cell strains and humanized prostatic carcinoma Du145 cell strains as target cells, and studies the inhabiting effect of the Java brucea fruit oil emulsion injection on the blood system tumor and the urogenital system tumor. The invention discovers that the Java brucea fruit oil emulsion injection has the inhabiting effect on the humanized leukemia HL-60, NB4 and U937cell strains and the humanized prostatic carcinoma Du145 cell strains for the first time, and the inhabiting effect is improved along with the gradual increase of the dosage. In addition, the Java brucea fruit oil emulsion injection can also induce the apoptosis of the humanized leukemia cells, and also has the apoptosis induction effect on the primary dissociated leukemia cells. In addition, the bruceolic oil emulsion injection liquid has low cell toxic effect on peripheral blood lymphocytes of normal persons. The results show that the Java brucea fruit oil emulsion injection has certain potential in the aspect of leukemia treatment, and can provide high-efficiency and low-toxicity medicine for the leukemia treatment.

The invention provides an anti-prostatic cancer compound which is used as a VGSCs inhibitor and has a good killing effect on prostatic cancer DU145 and prostatic cancer PC3 cells. The preparation method is simple, mild in process condition and suitable for large-scale production.

The invention provides a dual inhibitor targeting JAK/STAT and NF kappa B signal channels and an application thereof, and belongs to the technical field of biology. The invention provides a novel dual inhibitor L971-0101 capable of targeting JAK/STAT and NF kappa B signal channels, which has an inhibition effect on phosphorylation of STAT3 in a prostate cancer cell line DU145 and TNF alpha-induced I kappa B degradation in a cervical cancer cell line Hela, in addition, the dual inhibitor L971-0101 can relieve symptoms of LPS-induced sepsis shock mice in vivo, and effectively improves the survival rate of the mice, therefore, the product can be used as a potential inflammation inhibitor and has the potential of treating septicemia.

The invention relates to the technical field of molecular detection, in particular to a method for detecting and treating prostatic cancers (PCa) through microRNA. The invention provides influence ofan miR-203/SNAI2 axis on in-vitro biological characteristics of the prostatic cancers, in particular to expression of miR-203 in DU145 and PC3 cells to inhibit expression of SNAI2. The miR-203 inhibits proliferation and migration of the prostatic cancer cells and the formation of endothelial cells and tumor stem cells.

The invention discloses an application of a marsdenia tenacissima extract in preparation of a medicine for treating prostatic cancer, an application of the marsdenia tenacissima extract in preparationof a medicine for inhibiting cell growth of prostatic cancer PC3 and DU145, an application of the marsdenia tenacissima extract in preparation of a medicine for inhibiting cell migration of the prostatic cancer PC3 and DU145, an application of the marsdenia tenacissima extract in preparation of a medicine for inducing cell apoptosis of the prostate cancer DU145, an application of the marsdenia tenacissima extract in preparation of a medicine for inhibiting GSK-3[beta]/STAT3 signal axis, and an application of the marsdenia tenacissima extract in preparation of a medicine for up-regulating expression of Cytochrome C, Cleaved Caspase 3 and Cleaved Caspase 7. A marsdenia tenacissima extract medicine preparation is an injection preparation or a tablet. The application range of the marsdenia tenacissima extract is widened, and a new way is provided for application of the marsdenia tenacissima extract.

The invention discloses an aegiceras corniculatum leaf n-butyl alcohol extract and a preparation method thereof. The method includes: soaking aegiceras corniculatum leaves into ethanol to obtain aegiceras corniculatum leaf ethanol extract; after volatilization of ethanol in the aegiceras corniculatum leaf ethanol extract, adding petroleum ether for extraction to obtain a lower water phase; adding ethyl acetate into the lower water phase to extract, then adding n-butyl alcohol after the lower water phase is obtained, continuing extraction to obtain upper n-butyl alcohol part extract, and performing water bath drying to obtain the aegiceras corniculatum leaf n-butyl alcohol extract. According to in-vitro molecular biological experiment researches, the aegiceras corniculatum leaf n-butyl alcohol extract has an anti-proliferation effect on human prostatic cancer cells PC3 and DU145 and is capable of evidently inhibiting metastasis of the human prostatic cancer cells PC3 and DU145. Therefore, the aegiceras corniculatum leaf n-butyl alcohol extract has a potential application prospect in preparation of medicines for treating prostatic cancer and can be used for preparation of the medicines for treating prostatic cancer. Deeply developing the aegiceras corniculatum leaf n-butyl alcohol extract can expand an aegiceras corniculatum utilization range to create a novel approach for cancer treatment.