12 results about "Bufalin" patented technology

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 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 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 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 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.

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.