22 results about "Bufalin" patented technology

The invention provides a content detection method for a salvia miltiorrhiza medicinal material, a salvia miltiorrhiza clear paste and a musk heart-dredging dropping pill. According to the method, a high performance liquid chromatography method is adopted, octadecylsilane chemically bonded silica is used as a chromatographic column filler, acetonitrile is used as a mobile phase A, 0.02%-0.1% trifluoroacetic acid is used as a mobile phase B, gradient elution is carried out, and rosmarinic acid and salvianolic acid B in the salvia miltiorrhiza medicinal material are synchronously and quantitatively detected. And synchronously and quantitatively detecting tanshinol, protocatechuic aldehyde, caffeic acid, salvianolic acid E, rosmarinic acid, alkannic acid and salvianolic acid B in the salvia miltiorrhiza clear paste, and synchronously and quantitatively detecting tanshinol, protocatechuic aldehyde, caffeic acid, salvianolic acid E, rosmarinic acid, alkannic acid, salvianolic acid B, arenobufagin and bufalin in the musk Tongxin dropping pill. The method is used for monitoring the content of specific components, can also judge the transfer rate in the medicine production process, and facilitates traceability in the production link. In addition, the method is relatively low in equipment requirement and suitable for industrial popularization.

The invention relates to the technical field of medicines, and discloses an application of combination of bufalin and heme in preparation of a cancer treatment medicine. According to the invention, by means of an active metabonomics means, a key active metabolite-heme is locked through exogenous library screening and endogenous analysis, and the drug effect of bufalin is regulated by means of the active metabolite. Through verification, it is found that heme can cooperate with the synergistic drug effect in various cancer cell lines, and a new technical normal form based on an active metabolome for improving the drug effect of bufalin is provided. The pharmaceutical composition can improve the apoptosis induction ability of bufalin to different cancer cells, and provides powerful guiding significance for developing a novel treatment scheme in clinical medicine.

This invention belongs to the field of biomedical technology, specifically relating to the application of bufalin in the preparation of drugs for treating osteoarthritis. The structure of bufalin is shown in the following formula. Research results of this invention show that bufalin can significantly inhibit the inflammatory response and matrix degradation of chondrocytes, protecting the extracellular matrix of chondrocytes, thereby effectively delaying or reversing the pathological progression of osteoarthritis. This invention uses the SW1353 human chondrosarcoma cell line and SD rat primary chondrocytes as in vitro experimental models. The two cell models mutually validated each other, fully demonstrating the protective effect of bufalin on chondrocytes and its potential application value in the treatment of osteoarthritis.

The invention aims to catalyze bufalin and resibufogenin to modify and synthesize bufadienolide compounds, and discloses five newly discovered bufo bufo gargarizans source P450 enzymes, enzyme compositions, nucleic acids, expression vectors, bioengineering strains, methods and applications. The invention also discloses reported enzymes and enzyme compositions, nucleic acids, expression vectors, bioengineering strains, methods and applications of the P450 enzyme Sth10 related to catalysis of bufalin and resibufogenin for modification and synthesis of bufadienolide compounds. The amino acid sequence of the P450 enzyme is as shown in SEQ ID NO. 1-6. According to the invention, a plurality of P450 enzymes capable of modifying bufalin and / or resibufogenin at a fixed point under a mild condition are discovered for the first time, and a bioengineering strain and a biocatalytic synthesis method are developed based on the enzymes, so that a novel biosynthesis method for synthesizing bufadienolide compounds is established.

The application belongs to the field of heart disease treatment and natural medicine compound, and provides application of bufalin or a pharmaceutically acceptable salt thereof in preparation of a medicine for treating reperfusion arrhythmia. Experiments in vitro and in vivo prove that bufalin inhibits L-type calcium channels in a concentration-dependent manner, reduces extracellular calcium ion inflow, and further reduces the incidence of ventricular arrhythmia, arrhythmia, reduces ventricular conduction time, increases left ventricular conduction velocity, and reduces ventricular conduction dispersion; and provides a new drug selection for the treatment of reperfusion arrhythmia.

The invention discloses a drug for combined treatment of breast cancer bone metastasis, the drug comprises two active components, namely a first active component and a second active component, the first active component is Bufalin and its pharmaceutically acceptable salt, prodrug and derivative, and the second active component is RANKL targeted drug; bufalin and a derivative thereof are combined with an RANKL targeted drug for use, the Bufalin and the derivative thereof are synergistically complementary, and the Bufalin is used for regulating and controlling a tumor microenvironment, reducing secretion of high bone metastatic breast cancer cells HMGB1 and inhibiting differentiation of mononuclear / macrophages in bone marrow to osteoclasts, so that occurrence and development of breast cancer bone metastasis are inhibited; the RANKL targeted drug can specifically block an OPG / RANK / RANKL signal channel, inhibit osteoclast activation, reduce bone destruction and block vicious circle of bone metastasis; when the two active ingredients are combined for use, the effect of inhibiting breast cancer bone metastasis is obviously better than that of single use of any active ingredient, the occurrence of breast cancer bone metastasis can be effectively prevented and delayed, the progress of bone metastasis focus is controlled, and the occurrence risk of bone related events is reduced.

The application discloses a nanometer preparation of bufonin for treating colon cancer, which has a core-shell structure, wherein the inner core is a nanocrystal composed of bufonin and a stabilizer, and the outer shell is a pH-responsive material and a pore-forming agent; the nanometer preparation of bufonin for treating colon cancer is prepared by using the stabilizer, the bufonin and the pH-responsive material; the in-vitro dissolution characteristics of the poorly soluble drug bufonin are improved by nanometerization treatment, and the dissolution characteristics are obviously improved compared with the raw drug; the pH responsiveness of the Eudragit L-100 protects the bufadienolides in the bufonin from being destroyed by the strong acidic condition of gastric juice, thereby improving the stability and effectiveness of the drug, reducing the initial release of bufalin, cinobufagin and resibufogenin in the stomach, making the drug target the intestinal site, making the three kinds of bufonin components achieve effective and rapid synergistic release in the intestinal site, increasing the utilization rate of the drug in the intestinal tract, and being beneficial to the treatment of colon cancer.

The present application relates to a bufalin derivative and its preparation method and application, belong to the medical technical field. The present application adopts TEMPO oxidation reaction, and selectively oxidizes the primary alcohol in 19-OH bufalin to aldehyde, successfully synthesizes 19-CHO bufalin, that is, bufalin derivative. The bufalin derivative of the present application has a significant killing effect on pancreatic cancer BxPC-3 cells, liver cancer HepG2 cells and brain glioma U-87MG cells, the IC 50 of the bufalin derivative on BxPC-3 cells is 40.63 nM, the IC 50 of the bufalin derivative on HepG2 cells is 36.74 nM, and the IC 50 of the bufalin derivative on U-87MG cells is 28.73 nM, and the IC 50 of the bufalin derivative on CHO-K1 cells is greater than 30 μM, indicating that the toxicity to the heart is weak, and the bufalin derivative can be applied to the application of anti-pancreatic cancer, anti-liver cancer and anti-brain glioma drugs.

The invention relates to an oral nano traditional Chinese medicine antigen delivery system as well as a construction method and application thereof, and belongs to the technical field of oral nano materials. The construction method comprises the following steps: (1) preparing an OM nanoparticle suspension; (2) preparing a cationic liposome suspension; (3) preparing an OM / BF loaded cationic liposome suspension; and (4) constructing an oral nano traditional Chinese medicine antigen delivery system. According to the invention, multiple barriers of gastrointestinal tracts are broken through, the bioavailability of drugs is improved, precise immune tracking is realized through an OVA tumor antigen model, and in-vivo anti-tumor CTL reaction is simulated, so that an anti-tumor effect is synergistically exerted on three levels of a cell level, a tissue level and an immune level; according to the preparation method, the problems of poor water solubility and low delivery efficiency of bufalin serving as a traditional Chinese medicine active ingredient are effectively solved, meanwhile, through macrophage-mediated immunoregulation and accurate drug release, the targeting property and the treatment efficiency are improved, and a new way is opened up for tumor immunotherapy of oral nano traditional Chinese medicines.

The invention provides application of bufalin based on an MDM2-GPX4 regulatory pathway in preparation of non-small cell lung cancer resisting drugs, and relates to the technical field of biological medicines. According to the application, the medicine induces non-small cell lung cancer cells to generate ferroptosis through an MDM2-GPX4 regulatory pathway, so that occurrence and development of the non-small cell lung cancer are inhibited, the non-small cell lung cancer is p53 mutant non-small cell lung cancer, bufalin is directly combined with MDM2 to play a role of molecular glue, MDM2 and GPX4 are promoted to form an interaction compound, and the non-small cell lung cancer can be effectively inhibited. Further, GPX4 function inhibition or degradation is mediated, and ferroptosis is induced. The GPX4 is regulated through the E3 ubiquitin ligase function of the MDM2 for the first time, p53 mutant NSCLC can be effectively treated without relying on p53 activity, the problem that the application range of a traditional MDM2 inhibitor is limited is solved, the mechanism is clear, a bufalin (drug)-MDM2 / GPX4 (target)-ferroptosis (pathway) three-level regulation network is illuminated, and the uncertainty and risk of clinical development are reduced.

The invention relates to the technical field of biological medicine, in particular to application of bufalin serving as an LINC01410 inhibitor to preparation of medicine for inhibiting growth and / or proliferation of esophageal squamous cell carcinoma. The invention provides application of bufalin in preparation of a medicine for preventing and / or treating esophageal squamous cell carcinoma. The invention also finds that bufalin can be used as an inhibitor of LINC01410 for the first time, and proliferation and migration invasion of esophageal squamous cell carcinoma are effectively inhibited by inhibiting expression of LINC01410. The invention provides a new therapeutic target and a potential therapeutic drug for the treatment of esophageal squamous cell carcinoma, and has important clinical application value.

The application belongs to the technical field of nanomedicine, and particularly relates to a composition for inhibiting ovarian cancer, nanoparticles, a preparation method and application, comprising bufalin and niraparib, wherein the molar ratio of the bufalin and the niraparib is 6.25-12.5:5000-10000, and the application can improve the inhibition effect on ovarian cancer.

The invention discloses a P450 enzyme, an enzyme composition, nucleic acid, an expression vector, a bioengineering strain, a method and application. The amino acid sequence of the P450 enzyme is as shown in SEQ ID NO. 1. According to the invention, the P450 enzyme capable of modifying bufalin and / or resibufogenin at a fixed point under a mild condition is found for the first time, and a bioengineering strain and a biocatalytic synthesis method are developed based on the P450 enzyme, so that a biosynthesis method for efficiently synthesizing bufadienolide compounds is established.

The invention belongs to the technical field of medicine synthesis, and particularly relates to a bufogenin compound derivative as well as a preparation method and application thereof. The bufogenin compound derivative provided by the invention has a structural formula as shown in a formula (I). The toad lactone compound is a series of structural compounds with 14-site hydroxyl and 15-site basic groups (containing N heterocyclic rings, aliphatic amine or aromatic amine) through ring opening by taking a toad lactone compound containing 14-site and 15-site epoxy rings as a raw material, and the IC50 inhibition concentration of the toad lactone compound to Huh-7, HN4 and HEP G2 is obviously lower than that of a toad lactone compound represented by bufalin. The compound has an excellent effect of inhibiting proliferation of liver cancer cells or laryngeal squamous cell carcinoma cells, and is expected to be developed into novel anti-liver cancer or anti-laryngeal squamous cell carcinoma drugs.

The application discloses a method for extracting bufadienolides in bufonis medicinals and application thereof, and belongs to the technical field of effective component extraction of traditional Chinese medicines. The method uses a deep eutectic solvent (DES) as an extracting agent, and solves the problems of low purity of bufadienolides, poor extraction efficiency and complicated process in traditional water extraction or alcohol extraction methods by optimizing the solvent composition, material ratio and extraction process. The method has high extraction efficiency, can significantly improve the total content of bufalin, resibufogenin and cinobufagin in the extract, and is simple in process, environment-friendly and easy for large-scale industrial production, thereby providing a new approach for efficient utilization of bufonis medicinals.

The invention belongs to the field of medicine, and relates to injectable photo-thermal response type liposome hydrogel and a preparation method thereof, the injectable photo-thermal response type liposome hydrogel comprises injectable hydrogel, IR820 and drug-containing thermosensitive liposome, and the IR820 and the drug-containing thermosensitive liposome are co-loaded on the injectable hydrogel; the drug-containing thermosensitive liposome comprises a thermosensitive liposome Lip and a pharmaceutical composition co-loaded on the thermosensitive liposome Lip, the pharmaceutical composition is prepared from bufalin Bu and apatinib Ap. The injectable photo-thermal response type liposome hydrogel for treating colon cancer and the preparation method provided by the invention have the advantages of high precision, strong persistence and good stability.

The invention provides application of venenum bufonis active molecules in preparation of cGAS-STING pathway inhibitors, and particularly belongs to the technical field of protein inhibitors. Starting from a downstream interferon regulatory factor of a cGAS-STING pathway, the venenum bufonis active molecule is found to have relatively strong inhibitory activity on the cGAS-STING pathway through screening. The ulcerative colitis resisting activity evaluation on the active molecule arenobufagin of the venenum bufonis finds that the arenobufagin has a good relieving effect on the ulcerative colitis, the colon length can be obviously improved, and release of serum inflammatory factors of mice with the ulcerative colitis can also be inhibited. Finally, the venenum bufonis active molecule can be used as a cGAS-STING pathway inhibitor, plays a role in resisting ulcerative colitis, and lays a foundation for clinically developing medicines for treating ulcerative colitis.

The invention discloses a method for extracting toad steroid total lactone in toad medicinal materials and application of the toad steroid total lactone, and belongs to the technical field of extraction of effective components of traditional Chinese medicines. According to the method, a deep eutectic solvent (DES) is taken as an extracting agent, and the problems of low purity, poor extraction efficiency and tedious process of toad sterol total lactone in a traditional water extraction or alcohol extraction method are solved by optimizing the solvent composition, the material ratio and the extraction process. The method is high in extraction efficiency, the total content of bufalin, resibufogenin and cinobufagin in the extract can be remarkably increased, the process is simple and environmentally friendly, large-scale industrial production is easy, and a new way is provided for efficient utilization of toad medicinal materials.

This invention discloses the application of PRDX1 inhibitors and ferroptosis inducers in the preparation of drugs for cancer prevention and treatment, belonging to the field of pharmaceutical technology. This invention discovers that the antitumor effect of bufalin is closely related to its upregulation of intracellular ROS. Mechanistic studies indicate that PRDX1 is the target of bufalin. Molecular docking results show that PRDX1 has a "pocket" structure that binds to bufalin; inhibiting PRDX1 weakens the regulation of ROS and the antitumor effect of bufalin. Given that inhibiting PRDX1 can enhance ferroptosis, this invention evaluates the therapeutic effect of the combination of bufalin and ferroptosis inducers. Results show that bufalin effectively promotes the antitumor effect of the ferroptosis inducer RSL3 in liver cancer, lung cancer, and colon cancer cells.

The application belongs to the field of heart disease treatment and natural medicine compound, and provides application of bufalin or a pharmaceutically acceptable salt thereof in preparation of a medicine for treating reperfusion arrhythmia. Experiments in vitro and in vivo prove that bufalin inhibits L-type calcium channels in a concentration-dependent manner, reduces extracellular calcium ion inflow, and further reduces the incidence of ventricular arrhythmia, arrhythmia, reduces ventricular conduction time, increases left ventricular conduction velocity, and reduces ventricular conduction dispersion; and provides a new drug selection for the treatment of reperfusion arrhythmia.

The invention relates to the technical field of medicines, in particular to application of a bufalin composition in preparation of a medicine for treating lung cancer. The bufalin composition comprises bufalin and a chicoric acid derivative, the molar ratio of the bufalin to the chicoric acid derivative is 1: (0.1-0.3). Experimental results show that the anti-tumor effect can be remarkably enhanced through the synergistic effect of the bufalin and the chicoric acid derivative, and the chicoric acid derivative can also achieve the dual optimization purposes of solubilization and toxicity reduction at the same time.