30 results about "Human prostate" patented technology

The invention relates to the field of natural products, in particular to a dimer compound of guaiane type sesquiterpenes and uric acid as well as an extraction and separation method and application of the dimer compound. According to the invention, a new dimer compound of guaiane type sesquiterpene and uric acid is extracted and separated from carpesium abrotanoides in Guizhou, and it is found that the dimer compound has relatively strong anti-tumor activity. The compound has strong inhibitory activity on breast cancer, prostate cancer, nasopharynx cancer, liver cancer, lung cancer, leukemia, pancreatic cancer, glioma, osteosarcoma, skin cancer, cervical cancer, ovarian cancer, kidney cancer and esophageal cancer, and provides an optional scheme for broad-spectrum anti-cancer drugs. Moreover, in human prostate cancer cells PC3, human cervical cancer cells Hela, human liver cancer cells HepG2 and human glioma cells U87 which are resistant to paclitaxel, the compound also shows strong anti-cancer activity, which indicates that the compound has the potential of treating patients resistant to paclitaxel.

The invention discloses a preparation method of a gold-silicon SERS (Surface Enhanced Raman Scattering) substrate based on femtosecond laser processing and application of a micro-fluidic chip adopting the gold-silicon SERS substrate prepared based on femtosecond laser processing in capture and detection of cancer cells. The base preparation method comprises the following basic steps: S1, processing a micro-pit array on the surface of a silicon wafer through femtosecond laser processing; s2, electrochemically depositing a gold nano spine-shaped structure at the micro-pit array after femtosecond laser processing to prepare an SERS substrate; s3, testing the SERS performance of the substrate; and S4, incubating the substrate aptamer and capturing cancer cells. According to the gold-silicon SERS substrate based on femtosecond laser processing, SERS signals of an object to be detected can be remarkably improved, a large specific surface area is provided, and more detection sites are provided for molecules to be detected. Besides, the micro-pit array and the surface nano spine structure of the SERS substrate can effectively capture the cancer cells, a new method is provided for capturing and detecting the cancer cells, and the SERS substrate has great significance in early screening and diagnosis of human prostate cancer and analysis and research of heterogeneity of the cancer cells.

The invention belongs to the technical field of antibody preparation, and particularly relates to an anti-human prostate specific membrane antigen (PSMA) antibody and application thereof. The amino acid sequences of CDR1-3 on a light chain variable region of the antibody are respectively shown as SEQ ID NO.3-5, and the amino acid sequences of CDR1-3 on a heavy chain variable region of the antibody are respectively shown as SEQ ID NO.8-10. The antibody with the complementarity determining region sequence provided by the invention can specifically recognize PSMA expressed by cells and tissues, has good affinity in combination with the PSMA, has high recognition sensitivity, can effectively resist the interference of complex non-target protein components in the cells / tissues, has no specific combination with non-target antigens, is suitable for immunological detection of the PSMA, and has good application prospects. The kit is especially suitable for western blot detection and immunohistochemical methods, and can reduce the occurrence rate of false positive and false negative results and improve the accuracy of immunodiagnosis.

A kind of ethenyl indole and medium ring compound and its synthesis method, compound includes axial chiral ethenyl indole and nine-membered ring compound and ethenyl indole and eight-membered ring compound, structural formula is as shown in formula 3 and formula 6 respectively;Synthesis method: with formula 1 compound 3-ethynyl-2-indole methanol and formula 2 compound 2-indole ethanol / formula 5 compound 2-indole methanol as reaction raw material is added to organic solvent, additive is added, under the catalysis of catalyst and under certain temperature condition stirring reaction, TLC is tracked to complete reaction, filter, concentrate, purify and obtain.The ethenyl indole and medium ring compound synthesized in the application, through biological activity test, shows that the two types of derivatives have high sensitivity and strong cytotoxic activity to human prostate cancer cell PC-3.The reaction condition of the application is relatively conventional, the reaction process is mild, simple, low in cost, suitable for industrial large-scale production, and the application range of the method is widened.

Microfluidic devices, organ-on-a-chip platforms (e.g. mimicking the human prostate gland), and uses thereof are described herein. The microfluidic device includes at least two layers and a porous membrane therebetween. Each layer includes a channel, and the first channel and the second channel are aligned such that a first region of a first channel overlaps with a region of the second channel, and a second region of the first channel does not overlap a second region of the second channel. A disease model using the microfluidic devices includes (i) placing a first type of cells in the first channel and (ii) flowing a first cell culture medium through the first channel. Optionally, in step (i) a second type of cells in the second channel and in step (ii) a second cell culture medium flows through the second channel. The microfluidic devices can be used in drug screening and testing.

Inventors have firstly demonstrated that the transcriptomic signature of PTENpc- / - LSCmed cells is enriched in human MSPC signature, associated to metastases and ADT resistance. Using scRNAseq specifically with sorted PTENpc- / - LSCmed cells, they identified three distinct LSCmed clusters and showed that castration favors the emergence of the most stem-like LSCmed subpopulation by cell plasticity. In the latter, they identified the transcription factor FOSL1 / AP-1 and the kinase PIM1 as relevant therapeutic targets, and they showed that combined inhibition using JQ1, a BET / AP-1 inhibitor, and CX-6258, a pan-PIM kinase inhibitor, efficiently prevents PTENpc / - LSCmed cell growth in organoids. These findings were confirmed in the human prostate HPV10 cell line here identified as a robust model of Club / Hillock cells. Combined drug delivery to castrated PTEN-null mice induced a significant prostate weight decrease associated with the reduction of histopathological phenotypes and dramatically altered organoid-formation capacity of LSCmed cells sorted from these tumors. Accordingly, the drug combination significantly delayed tumor growth of MSPC-like human PC-3 cells subcutaneously injected into castrated immunodeficient mice. Altogether, this work shows a new therapeutic potential of combined FOSL1 and PIM1 targeting to prevent, or at least delay, the growth of MSPC-like cells. Accordingly, the invention relates to i) an inhibitor of FOSL1 and ii) an inhibitor of PIM1, as a combined preparation for use in the treatment of prostate cancer in a subject in need thereof.

The invention belongs to the technical field of prostate cancer diagnosis, and particularly relates to serum 7-dehydrocholesterol as a prostate cancer metastasis and endocrine treatment drug resistance diagnosis marker and application thereof. 7-dehydrocholesterol provided by the invention has different levels in human prostate cancer cell lines such as LNCaP, Du145, PC3 and the like, and is abnormally increased in PC3, so that the 7-dehydrocholesterol can be used as a drug resistance diagnosis marker for prostate cancer metastasis and endocrine therapy; the reagent composition capable of specifically recognizing 7-dehydrocholesterol and generating detectable signals can be used for preparing a prostate cancer detection kit; the 7-dehydrocholesterol provided by the invention has non-invasive, non-invasive and efficient effects as a diagnostic marker, and solves the technical problem of lack of a prostate cancer diagnostic marker in the prior art.

The invention belongs to the technical field of organic synthesis and medicinal chemistry, and discloses efficient synthesis of a novel polycyclic aromatic hydrocarbon derivative 5, 9-di-tert-butyl-12-mesitylene naphtho indolizine phenothiazine and an anti-cancer application of the novel polycyclic aromatic hydrocarbon derivative 5, 9-di-tert-butyl-12-mesitylene naphtho indolizine phenothiazine. According to the compound, a mesitylene group is introduced for the first time on the basis of a naphthoindolizine phenothiazine skeleton. The synthesis conditions are mild, and the yield is as high as 91%. In-vitro anti-cancer activity research shows that the compound has remarkable broad-spectrum anti-cancer activity and shows strong proliferation inhibition on human cervical cancer Hela cells (IC50 = 1.6 mu M), human lung cancer A549 cells (IC50 = 13.29 mu M) and human prostatic cancer PC-3 cells (IC50 = 19.1 mu M). Particularly, the activity on Hela cells is obviously superior to that of a clinical first-line drug cis-platinum. Preliminary toxicity evaluation shows that the toxicity of the compound to human normal umbilical vein endothelial cells (HUVEC) is far lower than that of cancer cells, and the selectivity is good.

The invention relates to BRD4 and p300 / CBP double-target PROTAC molecules as well as a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. The compound has a general formula shown in the specification, wherein L is preferably selected from one of the group; and E is preferably selected from one of the group. The compound disclosed by the invention has remarkable anti-tumor activity on human prostatic cancer cell strains PC-3, DU145 and 22Rv1 in vitro, the IC50 values are all lower than 20nM, and particularly, the IC50 values are all lower than 10nM in the cells PC-3 and DU145. The compound I-c shows the optimal activity, the IC50 values of the compound I-c in PC-3 and DU145 cells are 2.80 nM and 6.62 nM respectively, and the IC50 values of the compound I-c are obviously superior to those of positive control drugs NEO2734, paclitaxel and ARV-771. As a novel BRD4 and p300 / CBP double-target PROTAC molecule, the compound disclosed by the invention has a definite action mechanism and excellent anti-tumor activity, and can be used as a candidate or lead compound for research and development of anti-tumor drugs; the synthesis method is simple and convenient, and has good popularization and application prospects.

A vapor delivery needle and method is provided that is adapted for treating prostate cancer. The energy delivery probe can apply condensable vapor energy to tissue, such as a peripheral zone tissue in a human prostate. In one method, a needle is introduced into peripheral zone tissue of a human prostate, and vapor media is delivered through the needle to ablate peripheral zone tissue without ablating non-peripheral zone tissue. Systems for treating prostate cancer with vapor therapy are also provided.

The present invention provides an anti-tumor compound, an anti-tumor drug, a preparation method and an application thereof, belonging to the technical field of pharmaceutical preparation. The general structural formula of the compound provided by the present invention is #imgabs0#. In vitro anti-tumor activity tests of this type of compound found that it has an obvious inhibitory effect on the growth of human prostate cancer cell PC3. Among them, compound D17 has significant anti-tumor activity against five human prostate cancer cells (PC3, DU145, C42B, LNCAP, 22RV1) and shows concentration dependence, and can be used as a lead compound or a candidate compound for the development of anti-tumor drugs.

The invention relates to an aporphine-benzylisoquinoline alkaloid dimer as well as a preparation method and application thereof, and belongs to the field of natural medicines and biological medicines. The aporphine-benzylisoquinoline alkaloid dimer has a structural general formula shown in the specification, in the formula, R1, R2, R3, R4, R5, R6, R7 and R8 are independently selected from hydrogen, methoxyl, hydroxyl or two adjacent substituent groups are methylenedioxy, so that a five-membered ring is formed; and R9 is selected from hydrogen, methoxyl or hydroxyl. Six novel aporphine-benzylisoquinoline alkaloid dimers are extracted and separated from roots of thalictrum omeiensis, and through detection, the aporphine-benzylisoquinoline alkaloid dimers have obvious growth inhibition effects on human acute promyelocytic leukemia cells HL-60 and human prostate cancer cells PC-3, and have the prospect of preparing medicines for preventing and treating tumors.

The invention relates to a vinyl indole ring compound and a synthesis method thereof, the compound comprises an axial chiral vinyl indole nine-membered ring compound and a vinyl indole eight-membered ring compound, and the structural formulas are respectively shown as a formula 3 and a formula 6; the synthesis method comprises the following steps: adding a compound 3-ethynyl-2-indolyl carbinol in a formula 1 and a compound 2-indolyl carbinol in a formula 2 / 2-indolyl carbinol in a formula 5 as reaction raw materials into an organic solvent, adding an additive, carrying out a stirring reaction under the catalysis of a catalyst and a certain temperature condition, tracking the reaction by TLC until the reaction is complete, filtering, concentrating, and purifying to obtain the compound 3-ethynyl-2-indolyl carbinol. According to the vinyl indole ring compound synthesized by the invention, biological activity tests show that the two derivatives have relatively high sensitivity and very strong cytotoxic activity to human prostate cancer cells PC-3. The method is relatively conventional in reaction condition, mild and simple in reaction process, low in cost and suitable for industrial large-scale production, and the application range of the method is widened.

A vapor delivery needle and method is provided that is adapted for treating prostate cancer. The energy delivery probe can apply condensable vapor energy to tissue, such as a peripheral zone tissue in a human prostate. In one method, a needle is introduced into peripheral zone tissue of a human prostate, and vapor media is delivered through the needle to ablate peripheral zone tissue without ablating non-peripheral zone tissue. Systems for treating prostate cancer with vapor therapy are also provided.

This invention provides a substituted tetrahydroquinoline derivative and its application, which is a class of compounds with AR antagonistic activity. These compounds competitively bind to androgens, blocking AR activation and inhibiting the AR signaling pathway. Experiments have confirmed that the synthesized compounds all possess excellent AR antagonistic activity, showing strong inhibitory activity in the human prostate cancer cell line LNCaP. Therefore, they can be used to prepare drugs for treating diseases with abnormal androgen receptor expression, such as tumors including but not limited to prostate cancer, metastatic prostate cancer, castration-resistant prostate cancer, breast cancer, and ovarian cancer. The general structural formula of the compounds is shown in formula (a):

The present invention discloses a tertiary amide compound containing a naphthyl group, a preparation method, and an application thereof, belonging to the field of pharmaceutical technology. In vitro antitumor activity tests show that the tertiary amide compound containing a naphthyl group has a significant inhibitory effect on the growth of various tumor cells (human esophageal cancer cell line EC9706, human gastric cancer cell line SGC7901, human colorectal adenocarcinoma cell line HT-29, human gastric cancer cell line MGC-803, human breast cancer cell line MCF7, and human prostate cancer cell line PC-3). Its activity is significantly superior to that of the antitumor drug 5-fluorouracil, and it can be used as a lead compound or candidate compound for the development of broad-spectrum antitumor drugs.

The invention relates to a preparation method and application of aporphine-protoberberine alkaloid dimers, and belongs to the field of natural medicines and biological medicines. The aporphine-protoberberine alkaloid dimer disclosed by the invention has a structural general formula shown in the specification, in the formula, R1, R2, R3, R5, R6, R7, R8 and R9 are independently selected from hydrogen, methoxyl, hydroxyl or two adjacent substituent groups are methylenedioxy, so that a five-membered ring is formed; r4 is selected from hydrogen, methoxyl or hydroxyl. Six novel aporphine-protoberberine alkaloid dimers are extracted and separated from thalictrum omeiensis roots, and tests show that the aporphine-protoberberine alkaloid dimers have obvious growth inhibition effects on human acute promyelocytic leukemia cells HL-60 and human prostate cancer cells PC-3, can cause HL-60 cell cycle arrest in an S phase, induce HL-60 cell apoptosis, and can be used for preparing the aporphine-protoberberine alkaloid dimers. The compound has a prospect of preparing medicines for preventing and treating tumors.

A surgical training model for simulating human prostate surgery may include a harvested porcine urethra. A harvested porcine vagina surrounds a portion of the harvested porcine urethra to define a simulated human prostate.

The utility model relates to the technical field of medical equipment, and discloses a teaching model for simulating prostate laser vaporization or enucleation, which comprises a shell model in a human prostate shape and used for simulating a human prostate surgery envelope structure and a blood vessel structure of an envelope walking towards an inner gland, the prostate surgery envelope structure and the blood vessel structure are integrally formed; the upper portion of the shell model is provided with a first pipe opening used for being connected with a bladder model, the two sides of the upper portion of the shell model are each provided with a second pipe opening, internal ports of the second pipe openings are communicated with a vascular structure, and external ports of the second pipe openings are used for being connected with an external infusion apparatus to simulate blood circulation. The lower portion of the shell model is provided with a third pipe opening used for being connected with the urethra model. The internal model comprises a prostate urethra part and a prostate internal gland structure. The model is closer to a real hyperplasia gland in texture and physical characteristics, so that a doctor can obtain touch and force feedback which is very similar to that of actual operation when performing resectoscope combined laser vaporization or enucleation training.

The invention discloses a composition for treating prostatic cancer and application thereof. The composition is prepared from naringenin and cis-platinum. The application is the application of the composition for treating the prostatic cancer in preparation of drugs for treating the prostatic cancer. When the naringenin is combined with the cis-platinum, the inhibition effect on human prostate cancer cells DU-145 is obviously enhanced, a synergistic effect is achieved, and the naringenin and the cis-platinum have very small toxicity on normal HL-7702 cells. The naringenin combined with clinical drugs shows excellent in-vivo and in-vitro anti-tumor activity on human prostate cancer cells, has potential medicinal value and is expected to be used for preparing various anti-tumor drugs.

The present invention provides the use of Cistancheside F or a pharmaceutically acceptable salt thereof in the preparation of an anti-tumor drug. In vitro experiments show that Cistancheside F has significant inhibitory activity against a variety of tumor strains, including human lung cancer cells A549, human gastric adenocarcinoma cells AGS-CAS9, human liver cancer cells SK-HEP-1, human bladder cancer cells RT112, human cervical cancer cells Hela, human prostate cancer cells PC-3, and human neuroblastoma cells SH-SY5Y. Animal experiments show that Cistancheside F has a good in vivo anti-tumor effect and has a significant therapeutic effect on a variety of tumors, such as bladder cancer and liver cancer. Cistancheside F has strong anti-tumor activity and has broad application prospects.

The application discloses a pentacyclic triterpene derivative shown in a general formula I or a pharmaceutically acceptable salt thereof, and further discloses a method for preparing the pentacyclic triterpene derivative by a chemical enzyme method, and application of the pentacyclic triterpene derivative or the pharmaceutically acceptable salt thereof in preparation of a drug for treating and preventing tumors. The hydroxyl group is used to further derive the B ring and / or the D ring of glycyrrhetinic acid for the first time; the novel pentacyclic triterpene molecule containing multiple Michael reaction acceptor modules in the structure is synthesized by taking the synthetic electrophilic warhead as the basis for the derivation of glycyrrhetinic acid; and through cell toxicity screening of the novel compound in the application, a drug lead compound with good inhibitory effect on human prostate cancer cells PC-3, human breast cancer cells MCF-7, human colon cancer cells SW480 and human cervical cancer cells Hela is found.

The invention belongs to the field of biological medicine, and particularly discloses a reversible immortalized human prostate cancer fibroblast and a construction method thereof. The method comprises the following steps: introducing an SV40 large T antigen gene controlled by a tetracycline response element into primary prostate cancer fibroblasts through a lentiviral vector, and carrying out puromycin screening and monoclonal culture to obtain the reversible immortalized cell line. The cell line can efficiently express the SV40 large T antigen under the induction of doxycycline, and infinite proliferation is realized; after the inducer is removed, the cell cycle is quitted, the fibroblast enters an aging state again, and specific marker expression of the fibroblast is kept all the time. The cell line can be used for prostate cancer tumor microenvironment research, high-throughput drug screening and matrix-epithelial cell interaction mechanism research, solves the problems of limited primary cell proliferation, large batch-to-batch difference and the like, and has good stability and reversible regulation.

The present application relates to the field of natural products, in particular to a sesquiterpene and uric acid dimer compound of guaiane type and an extraction and separation method and application thereof. A new sesquiterpene and uric acid dimer compound of guaiane type is extracted and separated from Guizhoutianmingjing, and it is found that the compound has strong antitumor activity. The compound has strong inhibitory activity on breast cancer, prostate cancer, nasopharyngeal carcinoma, liver cancer, lung cancer, leukemia, pancreatic cancer, glioma, osteosarcoma, skin cancer, cervical cancer, ovarian cancer, kidney cancer and esophageal cancer, and provides an alternative for broad-spectrum anticancer drugs. Moreover, in the paclitaxel-resistant human prostate cancer cell PC3, human cervical cancer cell Hela, human hepatoma cell HepG2 and human glioma cell U87, the compound also exhibits strong anticancer activity, indicating that it has the potential to treat paclitaxel-resistant patients.

The present invention relates to a lentiviral vector comprising a nucleic acid sequence encoding at least one antigen sequence selected from the group consisting of human prostatic acid phosphatase, human prostate specific antigen, human prostate-specific membrane antigen, human prostate stem cell antigen, human six-transmembrane epithelial antigen of the prostate-1 and fragments thereof. It further relates to lentiviral vector particles, isolated cells or pharmaceutical compositions comprising a lentiviral vector according to the invention. The invention further provides a combinatory treatment comprising at least one lentiviral vector, lentiviral vector particle, isolated cell or pharmaceutical composition according to the invention, and at least one anticancer agent or treatment and / or at least one immunotherapy agent or treatment. Finally, the invention provides any of the above for use in the treatment and / or prevention of prostate cancers, in particular of metastatic prostate cancers, more particularly of metastatic castration-resistant prostate cancers.

The invention discloses a xanthomonas oryzae exopolysaccharide as well as a preparation method and application thereof, and the weight-average molecular weight of the xanthomonas oryzae exopolysaccharide is 1 * 1052 * 107000. The preparation method comprises the following steps: inoculating a bacterial liquid into an NA liquid culture medium, removing small molecular impurities from the fermented bacterial liquid, freeze-drying to obtain refined xanthomonas oryzae extracellular crude polysaccharide, separating the xanthomonas oryzae extracellular polysaccharide, respectively taking 0.2 mol / L NaCl and 0.3 mol / L NaCl as eluents, and determining the content of the xanthomonas oryzae extracellular polysaccharide according to a chromatogram drawn by a phenol-sulfuric acid method. And collecting fractions with the same signal peak, concentrating, dialyzing by using a 3500 Da dialysis bag, and freeze-drying to obtain the xanthomonas oryzae exopolysaccharide. The pharmaceutical composition can resist A549 non-small cell lung cancer and PC-3 human prostate cancer cells, and the preparation method is simple.

This invention relates to the fields of tumor biology and cell engineering, specifically disclosing the construction and application of a human prostate cancer cell line. The human prostate cancer cell line is derived from primary prostate cancer tissue, expresses prostate-specific antigen and α-methylacyl-CoA racemic enzyme, and has a 46,XY karyotype. The construction method employs an innovative strategy of co-culturing fully digested cell suspensions with incompletely digested tissue blocks, significantly improving the success rate of establishing the cell line from the primary lesion. This cell line can stably proliferate in conventional culture media supplemented with testosterone and has been successfully applied to subcutaneous tumorigenesis models in immunodeficient mice and in vivo migration models in zebrafish. The primary lesion-derived prostate cancer cell line provided by this invention offers a highly relevant, stable, and reliable new experimental tool for studying the biological characteristics of primary prostate cancer, drug screening, and personalized treatment.

The application discloses an indole and medium ring lactam compound and a synthesis method thereof, and a chemical structural formula of the indole and medium ring lactam compound is shown as formula 3; the synthesis method comprises the following steps: adding a compound 2-indole acetate of formula 1 and an o-chloromethyl aniline compound of formula 2 as reaction raw materials into an organic solvent, adding a base, stirring and reacting under a temperature condition of 0-40 DEG C, tracking the reaction to completion through TLC, and filtering, concentrating and purifying to obtain the indole and medium ring lactam compound. The indole and medium ring lactam compound synthesized by the application has high sensitivity and strong cytotoxicity to human prostate cancer cell PC-3 through a biological activity test. The reaction condition is very conventional, the reaction is carried out near room temperature, no metal is needed, and the operation is simple; the method can be used for large-scale amplification reaction of a gram level, and proves the potential of practical application; a plurality of kinds of substrates are used as reactants in the application, the indole and medium ring lactam compound with diversified structure is efficiently constructed, and the yield is high.

A silybin derivative with anti-prostate cancer activity and a preparation method thereof, relates to an anti-cancer silybin derivative and a preparation method thereof, the invention transforms and modifies the chemical structure of the natural product silybin, takes silybin as a lead compound, first uses propionic anhydride to esterify five hydroxyl groups, recrystallizes to obtain an intermediate 3,5,20,23-tetrapropionic acid silybin ester, and further reacts the intermediate with acyl chloride, halogenated hydrocarbon and sulfonyl chloride to synthesize 12 ester, ether and sulfonate silybin derivatives I1 to I12. The results of the MTT experiment show that the synthesized silybin derivatives exhibit inhibitory activity against human prostate cancer cells PC-3 and DU145, and the inhibitory activity is significantly higher than that of the parent silybin, among which the inhibitory activity of the derivative I3 is the best, which is better than the positive control drug Flutamide. Studies have shown that such compounds can enhance anti-tumor activity.

The present invention relates to treatment methods for prostate cancer using a combination of an anti-androgen compound and a T-cell engaging molecule that specifically binds to human prostate-specific membrane antigen (PSMA) and human CD3. In particular, the present invention relates to methods for treating prostate cancer, including metastatic castration-resistant prostate cancer, in a patient in need thereof comprising administering to the patient one or more cycles of an anti-androgen compound in combination with a PSMA-targeted T-cell engaging molecule, wherein administration of the first dose of the anti-androgen compound is delayed relative to administration of the first therapeutic dose of the PSMA-targeted T-cell engaging molecule in the first cycle.