59 results about "Fluorouracil" patented technology

The invention belongs to the technical field of natural medicines, and particularly relates to application of spermidine alkaloid in preparation of anti-tumor medicines and / or reversion of drug resistance. The invention provides an application of macrocyclic spermidine alkaloid in preparation of anti-tumor drugs and / or reverse drug resistance. The macrocyclic spermidine alkaloid comprises one or more than two of 13-oxo-furan celastrus orbiculatus, furan celastrus orbiculatus, benzene-substituted celastrus orbiculatus and celastrus orbiculatus cinnamamide alkali. The macrocyclic spermidine alkaloid disclosed by the invention has the characteristics of broad-spectrum anti-tumor effect, good anti-tumor effect, relatively low toxic and side effects, capability of reversing 5-fluorouracil drug resistance, relatively high water solubility, relatively easy source, simple structure, only one chiral carbon in the structure, relatively easy artificial synthesis, intervention in cell autophagy mechanism and the like, so that the overall treatment cost is relatively low; the method has a potential important clinical application prospect.

The application discloses a kind of 2-substituted benzylhydrazine-4-indole pyrimidine-5-carbonitrile derivatives and preparation method and application thereof.The derivative has general formula (I) structure: wherein R is hydroxyl or C1-C4 alkoxy, n=1~3.Preferred compound is 2-hydroxy, 4-hydroxy-3-methoxy, 2,3-dihydroxy or 2,4-dihydroxy substituted benzylhydrazine derivative.The application also provides key intermediate 2-hydrazine-4-(1H-indole-3-carbonyl) pyrimidine-5-carbonitrile and preparation method thereof.In vitro antitumor activity shows that the derivative has excellent inhibitory activity on human gastric cancer cell MGC-803, and the inhibition rate is up to 96.3% at 10 μmol / L, which is better than positive control doxorubicin.In vivo combination test shows synergistic effect with 5-fluorouracil or anti-PD-1 antibody.The compound of the application has mild synthesis route, high yield, various preparation forms, good safety, and can be applied in the preparation of anti-gastric cancer drugs.

The invention relates to the technical field of production of flurala drops, in particular to a flurala drop preparation method based on online monitoring. The preparation method comprises the following preparation processes: sequentially adding weighed dimethylacetamide and acetone into a liquid preparation tank, adding fluralana and tetrahydrofuran polyglycol ether into the liquid preparation tank, stirring until the materials are uniformly mixed, monitoring raw material data, production data and product data by using a monitoring and collecting system in the preparation process, and recording and storing the raw material data, production data and product data through a monitoring and recording system. Data collected by the monitoring and collecting system is used as a reference, production is controlled and commanded through the monitoring and controlling system, and the monitoring and recording system records and stores the data and sends the data to the monitoring and analyzing system for statistical analysis and machine learning training. Key links such as raw material parameters, environmental process parameters and intermediate product and finished product quality data are monitored online in real time through the monitoring and collecting system, the production dynamic state is comprehensively mastered, and it is guaranteed that all procedures are strictly executed according to the process requirements.

The invention relates to the technical field of biological medicines, in particular to application of dauricine in preparation of medicines for inhibiting ovarian cancer SKOV3 cell proliferation and treating ovarian cancer. The invention finds that dauricine has a remarkable inhibition effect on drug-resistant ovarian cancer cells, the dauricine has a clear dose-dependent relationship on the inhibition activity of the ovarian cancer cells SKOV3 in a concentration range of 1-50 mu M, and the IC50 value is 2 mu M. Meanwhile, the effect of inhibiting SKOV3 cell proliferation of the dauricine can be remarkably improved by combining the dauricine with paclitaxel or 5-fluorouracil. Therefore, dauricine can be used for preparing medicines for inhibiting ovarian cancer SKOV3 cell proliferation and improving ovarian cancer multidrug resistance, and has a good clinical application prospect.

The invention relates to an application of Quercetin (QUE) or a derivative thereof in a medicine for resisting vocal cord fibrosis and a preparation of the Quercetin or the derivative thereof. The quercetin can significantly inhibit abnormal deposition of extracellular matrix (ECM) after vocal cord injury, improve reduction of hyaluronic acid (HA) and elastic fibers (EF), and reduce overexpression of type I collagen (COL1A1) and fibronectin (FN1). Besides, by regulating PI3K / AKT and MAPK signal channels, the quercetin inhibits proliferation and migration of fibroblasts and promotes apoptosis of the fibroblasts, so that vocal cord fibrosis is effectively relieved. The invention also provides an application of a preparation of the quercetin and the derivative thereof combined or not combined with other anti-fibrosis drugs (such as 5-fluorouracil and dexamethasone) in treatment of vocal cord fibrosis, wherein the dosage forms of the preparation comprise an oral preparation, an injection, a spray or a local gel preparation.

The invention belongs to the technical field of medicines, and relates to application of minocycline in preparation of an anti-tumor synergist. The minocycline is used as an anti-tumor synergist and has a synergistic effect with the 5-fluorouracil and the gemcitabine, so that the curative effect of the anti-tumor medicine is remarkably enhanced, the dosage of the anti-tumor medicine is reduced, and the body side effect caused by the anti-tumor medicine or the damage to normal tissue cells is reduced.

The present application relates to the application of ocanin in the preparation of anti-tumor drugs, and the ocanin is used in the anti-tumor drugs alone or in combination with 5-fluorouracil, and the concentration of the ocanin used in the preparation of anti-intestinal cancer drugs is 20-500 uMol. It is found that the ocanin can inhibit the growth of intestinal cancer cells in vivo and in vitro, and the naked mice have good tolerance to the natural compound. The ocanin has better anti-intestinal cancer effect than other extracts of goldeneye and devil's needle, and has better anti-cancer effect and smaller toxicity than the current conventional intestinal cancer drug 5-fluorouracil. Therefore, the ocanin can be developed into a new anti-cancer drug.

The present disclosure provides double stranded nucleic acid compositions incorporating uracil, gemcitabine, and methotrexate (MTX). More specifically, the present disclosure reveals that modification of a double-stranded microRNA nucleotide sequence with 5-fluorouracil, gemcitabine, and methotrexate (MTX) enhances the therapeutic efficacy and tumor specificity of tumor suppression. Thus, the present disclosure provides various nucleic acid (e.g., microRNA) compositions having 5-fluorouracil, gemcitabine, and methotrexate (MTX) incorporated into their nucleic acid sequences, as well as methods of using the same. The disclosure further provides pharmaceutical compositions (e.g., formulations) comprising the modified nucleic acid compositions, and methods for treating cancer, e.g., pancreatic cancer. The method is a platform technology which can be applied to other tumor suppressor genes miRNA and siRNA.

The present disclosure provides an anti-cancer lipid-based composition that kills very aggressive colorectal cancer cells. This composition is a concoction of an anti- cancer agent, 5-Fluorouracil and a glucocorticoid receptor (GR)-targeting cationic lipid delivery system, D1X. The uptake studies of these formulations have showed that formulations with dexamethasone enter into nucleus, bind GRE region and upregulate CYP3a5 gene. The intensity of upregulation is better than liposome without dexamethasone. Same results found in in vivo studies, the D1X5-FU shows better tumor regression and survivability than FOLFOX and FOLFIRI. The biodistribution studies showed that D1X5-FU targets only tumor tissues, not other organs. The pilot studies of tumor regression by other liposomal formulations- D1XLeucovorin, D1XOxaliplatin has showed better tumor regression than FOLFOX and FOLFIRI.

The application discloses application of a pharmaceutical composition taking GL-V9 and a chemotherapeutic drug as active ingredients in treatment of tumors. When GL-V9 is combined with a classical chemotherapeutic drug to treat tumors, a drug synergistic effect can be obviously achieved, and the effect is obviously superior to combination of similar drugs and the chemotherapeutic drug. The chemotherapeutic drugs include 5-fluorouracil; and the tumor types include leukemia, colorectal cancer and lung cancer.

The invention belongs to the technical field of biological medicines, and particularly relates to application of saikoside D in preparation of medicines for inhibiting colorectal cancer Caco-2 cell proliferation and treating colorectal cancer. The invention finds that saikoside D has a remarkable inhibition effect on colorectal cancer cells, and in a concentration range of 1-50 [mu] M, the saikoside D has a definite dose-dependent relationship on the inhibition activity on the proliferation of colorectal cancer Caco-2 cells, and the inhibition activity is higher than that of paclitaxel and 5-fluorouracil. Meanwhile, the combination of saikoside D and paclitaxel can significantly improve the Caco-2 cell proliferation inhibition effect, which may be related to P-gp protein expression inhibition. Therefore, saikosaponin D can be used for preparing the medicine for inhibiting the proliferation of colorectal cancer Caco-2 cells and improving the drug resistance of paclitaxel to colorectal cancer, and has a good clinical application prospect.

This invention belongs to the field of molecular biology technology, specifically involving tRF5-22-SeCTCA-1, tRF5-22-SeCTCA-1 detection reagents, kits, and their applications. This invention discovers and verifies that tRF5-22-SeCTCA-1 plays a key regulatory role in the process of 5-fluorouracil (5-FU) chemotherapy resistance in colorectal cancer, filling a gap in the research of tRNA-derived fragments (tRFs) in colorectal cancer chemotherapy resistance. It is the first tRF molecule reported to be associated with 5-FU chemotherapy resistance in colorectal cancer, providing a novel molecular target and research direction for predicting chemotherapy resistance in colorectal cancer. This invention also provides a therapeutic strategy targeting tRF5-22-SeCTCA-1 and establishes α-ketoglutarate as an independent reversal agent, providing multi-dimensional technical solutions for the precision diagnosis and treatment of colorectal cancer and the reversal of chemotherapy resistance.

The invention discloses an acylhydrazone compound containing a quinazolinone fragment as well as a preparation method and application thereof, and relates to the technical field of medicinal chemistry, the acylhydrazone compound containing the quinazolinone fragment or pharmaceutically acceptable salt, isomer, hydrate, solvate, crystal form and prodrug of the acylhydrazone compound, and the structural formula of the acylhydrazone compound containing the quinazolinone fragment or pharmaceutically acceptable salt, isomer, hydrate, solvate, crystal form and prodrug of the acylhydrazone compound containing the quinazolinone fragment is shown in the specification. According to the invention, acylhydrazone compounds containing quinazolinone fragments are designed and synthesized by utilizing a splicing principle, the compounds are subjected to anticancer activity test, and the compounds with anticancer activity superior to that of 5-fluorouracil are screened out from the acylhydrazone compounds.

The invention discloses application of miR-30a-5p and a target gene thereof in diagnosis and treatment of hepatocellular carcinoma, according to the scheme, tests prove that the toxic and side effects of an anti-hepatocellular carcinoma drug 5-fluorouracil can be remarkably reduced by reducing the expression quantity of miR-30a-5p, so that miR-30a-5p becomes a potential target for screening drugs for reducing the toxic and side effects of 5-fluorouracil; and when the target gene Thbs2 of the miR-30a-5p is in low expression, immunohistochemical (IHC) staining data is further retrieved from an HPA database, and the expression level of the Thbs2 obtained from the perspective of protein is medium in staining in normal liver tissues and relatively high in staining in liver cancer tissues, so that the Thbs2 can be used as a molecular marker for liver cancer diagnosis. The research provides an important basis for clinical early diagnosis and differential diagnosis of liver cancer and effective observation and alleviation of side effects of anti-cancer drugs, provides a brand new idea for accurate diagnosis of liver cancer and alleviation of side effects of anti-cancer drugs from the molecular level, and expands the cognition of the occurrence and development mechanism of liver cancer in the theoretical level. The obvious practical value and transformation potential are also shown in clinical application.

A probiotic composition for treating or preventing metabolic dysfunction-associated steatotic liver disease-associated hepatocellular carcinoma(MASLD-HCC) or colorectal cancer, comprises one or more microbiota selected from a group consisting of Lactobacillus helveticus, Lactobacillus plantarum, Lactobacillus rhamnosus GG, Lactobacillus paracasei, Lactobacillus acidophilus, Bifidobacterium breve, Bifidobacterium animalis subsp. Lactis, Streptococcus thermophilus or any combination thereof. The probiotic composition demonstrates improved therapeutic effects when combined with low-dose Sorafenib for MASLD-HCC and outperforms 5-Fluorouracil in colorectal cancer models.

The invention provides a capecitabine prodrug for reducing liver metabolism burden and application thereof, a derivative formed by introducing a masking group R capable of enzymolysis or chemical hydrolysis into 5 '-hydroxyl or N-amino of a capecitabine molecule, and the R is selected from amino-acid ester, phosphate, polyethylene glycol chain or cholic acid conjugation group. The prodrug can be selectively activated in intestinal tracts or tumor tissues through a non-UGT1A1 dependent pathway, and 5-fluorouracil is finally released through metabolism. Due to the characteristic, the competitive inhibition of the prototype capecitabine on liver UGT1A1 enzyme is obviously reduced, and the interference on bilirubin binding and excretion pathways is fundamentally reduced. The pharmaceutical composition disclosed by the invention is suitable for patients with UGT1A1 gene defects or liver insufficiency. While good anti-tumor activity is maintained, the hepatotoxicity is remarkably reduced, the medication safety is improved, and good clinical application prospects are achieved.

The invention relates to a pharmaceutical composition, a preparation method thereof and application of the pharmaceutical composition in treatment of gastric cancer. The invention further relates to a kit for treating gastric cancer and a packaging method. The pharmaceutical composition comprises: 3-epiursolic acid or a pharmaceutically acceptable salt thereof; 5-fluorouracil or a pharmaceutically acceptable salt thereof; and a liposome as a carrier.

The present invention discloses a five-membered sulfur-containing heterocyclic nucleoside lead compound and its application in anti-cervical cancer and pancreatic cancer activities, belonging to the field of pharmaceutical chemistry technology. A series of five-membered sulfur-containing heterocyclic nucleoside compounds were synthesized by a two-step Michael addition reaction, including racemate, (3S, 4R) and (3R, 4S): (* is a chiral center). The results showed that in in vitro cervical cancer (HeLa) and pancreatic cancer (PANC-1) cell tests, the anti-tumor activity of the racemate and the enantiomer configuration were similar. Among them: the chiral five-membered sulfur-containing heterocyclic nucleoside lead compound (3R, 4S)-15ab showed a strong ability to inhibit proliferation in cervical cancer cell lines, IC 50 reached 2.78 μM, which was significantly better than the control drugs 5-fluorouracil and cisplatin (IC 50 9.75 μM and 7.99 μM, respectively).

The disclosure relates generally to compositions comprising a CDA inhibitor, e.g., tetrahydrouridine or an analog or derivative thereof, and methods for treating, reducing or inhibiting a symptom, complication or side effect, such as palmar-plantar erythrodysesthesia, caused by chemotherapy, such as 5-fluorouracil chemotherapy, especially, capecitabine chemotherapy, by administering a CDA inhibitor, e.g., tetrahydrouridine or an analog or derivative thereof. The disclosure also relates to treating cancer by co-administering capecitabine and a CDA inhibitor, e.g., tetrahydrouridine or an analog or derivative thereof to a subject.

The invention discloses a (9β-H)-pimarane skeleton diterpenoids with anti-colon cancer activity and a derivative thereof, and further discloses a preparation method and application of the compounds above; the invention finds that novel skeleton compounds 1 and 2 have certain inhibition effects on colon cancer cells, wherein the compound 2 has remarkable anti-proliferation effects on two colon cancer cell lines HT-29 and SW620, and the effects are both stronger than those of a positive drug 5-fluorouracil, so that the compound has the potential of being developed into a new anti-colon cancer drug.

Provided herein are compositions comprising disodium levofolinate. Also provided are processes for preparing compositions comprising disodium levofolinate. Also provided are compositions comprising disodium levofolinate prepared by the processes provided herein. Also provided are methods of treating folic acid deficiency in a subject in need thereof, comprising administering a composition provided herein to the subject. Also provided are methods of treating cancer in a subject in need thereof, comprising administering 5-fluorouracil and a composition provided herein to the subject. Also provided are methods of reducing the immediate toxic effects of methotrexate overdose in a subject in need thereof, comprising administering a composition provided herein to the subject. Also provided are methods of treating cancer in a subject in need thereof, comprising administering high-dose methotrexate and a composition provided herein to the subject. Also provided are methods of treating megaloblastic anemia in a subject in need thereof, comprising administering a composition provided herein to the subject.

The application discloses application of a pharmaceutical composition with GL-V9 and a chemotherapeutic drug as active ingredients in treatment of tumors, and the GL-V9 can obviously achieve a drug synergistic effect when the GL-V9 is combined with a classical chemotherapeutic drug to treat tumors, and the effect is obviously superior to combination of similar drugs and the chemotherapeutic drug. The chemotherapeutic drugs include PARP1 inhibitors, capecitabine, irinotecan, sorafenib, cisplatin or 5-fluorouracil; and the tumor types include leukemia, colorectal cancer and lung cancer.

The application discloses a method, system and device for evaluating the treatment effect of PTT on pancreatic cancer. The application first discovers that PTT can treat pancreatic cancer by regulating the caspase-1 / GSDMD pathway, and discovers that the expression level of GSDMD is positively correlated with the drug resistance of pancreatic cancer cells to 5-fluorouracil, irinotecan, paclitaxel and cisplatin, which indicates that for patients with high expression of GSDMD, a local treatment method of photothermal therapy can be adopted instead of traditional chemotherapy. In addition, the application provides a method, system and device for evaluating the treatment effect of PTT on pancreatic cancer and a method, system and device for predicting the sensitivity of a pancreatic cancer patient to a chemotherapeutic drug, thereby assisting doctors in evaluating the treatment effect on the pancreatic cancer patient and guiding a clinician to formulate an individualized treatment plan for the patient.

Provided herein are compositions comprising disodium levofolinate. Also provided are processes for preparing compositions comprising disodium levofolinate. Also provided are compositions comprising disodium levofolinate prepared by the processes provided herein.Also provided are methods of treating folic acid deficiency in a subject in need thereof, comprising administering a composition provided herein to the subject. Also provided are methods of treating cancer in a subject in need thereof, comprising administering 5-fluorouracil and a composition provided herein to the subject. Also provided are methods of reducing the immediate toxic effects of methotrexate overdose in a subject in need thereof, comprisingadministering a composition provided herein to the subject. Also provided are methods of treating cancer in a subject in need thereof, comprising administering high-dose methotrexate and a composition provided herein to the subject. Also provided are methods of treating megaloblastic anemia in a subject in need thereof, comprising administering a composition provided herein to the subject.

The invention relates to the technical field of pharmaceutical preparations, and provides a pharmaceutical composition for preventing and / or treating leucopenia caused by chemotherapy and a preparation method of the pharmaceutical composition. The pharmaceutical composition is prepared from the following raw materials: red ginseng, prepared rehmannia root, morinda officinalis, pericarpium citri reticulatae, semen cuscutae, rhizoma atractylodis macrocephalae, Chinese yam, astragalus membranaceus, poria cocos, radix achyranthis bidentatae, cistanche, cinnamon, angelica sinensis, fructus lycii, cornu cervi pantotrichum, fennel, radix paeoniae alba and liquorice. The pharmaceutical composition provided by the invention realizes prevention and / or treatment of leucopenia caused by chemotherapy, specifically, the pharmaceutical composition is combined with the chemotherapeutic drug 5-fluorouracil for use, and is applied before, during or after chemotherapeutic drug administration, and the leucocyte level of a subject is increased by promoting lymphocyte and / or monocyte proliferation.

The invention discloses a pharmaceutical composition of a pentacyclic triterpenoid and capecitabine and application of the pharmaceutical composition, and belongs to the technical field of biological medicines. By reducing the hydrolysis of capecitabine in gastrointestinal tracts and livers, the pharmaceutical composition not only slows down the early release of capecitabine drug bodies in gastrointestinal tracts and livers, increases the total bioavailability of the drug bodies and 5-fluorouracil, reduces the non-uniform high distribution of capecitabine in normal tissues such as gastrointestinal tissues, but also improves the bioavailability of capecitabine in gastrointestinal tracts and livers. Reducing toxicity in these tissues; meanwhile, the effectiveness of the medicine is improved by relatively increasing the medicine distribution of the targeted tumor part. The combination will be suitable for all tumor treatment, especially solid tumor treatment.

The invention relates to the field of medicinal chemistry, in particular to dronedarone derivatives with broad-spectrum anticancer activity and a preparation method and application thereof. The invention designs and synthesizes a dronedarone derivative, and the derivative has broad-spectrum anticancer activity and shows good treatment potential for resisting cancers such as gastric cancer, liver cancer, pancreatic cancer, colorectal cancer, cervical cancer and ampulla cancer. The derivative has remarkable anti-tumor cell proliferation activity, the effect of the derivative is better than that of a clinical drug fluorouracil, and the derivative can be used for preparing novel anti-tumor drugs and has wide application prospects.

The application belongs to the field of textiles, and discloses a fabric for adjuvant therapy of breast cancer and a preparation method thereof. The preparation method comprises the following steps: firstly, preparing a fluorouracil FU and collagen tripeptide CTP compound FU-CTP, incorporating the compound into a core layer spinning solution, preparing a core-shell nanofiber membrane through electrospinning, and finally obtaining the fabric for adjuvant therapy of breast cancer. The fabric can release the compound FU-CTP in the form of micelles, CTP can carry FU, promote the transdermal penetration ability of FU, and enrich FU in the local breast to reach a therapeutic concentration, so that most side effects such as gastrointestinal side effects and bone marrow suppression caused by oral and intravenous administration of FU can be reduced.

The present application relates to a composition for diagnosing resistance to ECF combination therapy (epirubicin, cisplatin, and 5-fluorouracil; ECF) for treating gastric cancer, and a diagnostic kit using the same. In order to solve the problem of recurrence and resistance, NINJ2 can be inhibited by early detection of the occurrence of resistance, thereby inhibiting the recurrence and treatment resistance of gastric cancer.