18 results about "Cinobufagin" patented technology

The invention discloses an application of cinobufagin in preparation of a medicine for inhibiting bone metastasis of lung cancer. It is proved for the first time that 1) in-vitro cell experiments prove that cinobufagin can effectively inhibit proliferation and migration ability of lung cancer bone metastasis cells and promote cell apoptosis; 2) a mouse left ventricular injection bone metastasis model and a tibia injection model show that cinobufagin can significantly inhibit the development of lung cancer bone metastasis and osteolytic bone injury; (3) the specific regulation and control mechanism of cinobufagin for inhibiting bone metastasis of lung cancer is explored, and it is found through combined analysis of IP-MS proteomics and LiP-SMap proteomics that cinobufagin may target pyruvate carboxylase to play the function of cinobufagin; and 4) further verifying that cinobufagin can be combined with PC to inhibit bone metastasis of lung cancer through a drug affinity reactive target stability experiment and a heat transfer experiment. The research provides a new target spot and a treatment strategy for inhibiting bone metastasis of lung cancer.

The invention discloses a load ICGamp. The invention discloses ZIF-8 nano-particles of CBF, and belongs to the technical field of preparation of nano-drug particles. The multifunctional nanoparticles are formed by simultaneously encapsulating indocyanine green (ICG) and cinobufagin (CBF) components by ZIF-8, and the drug loading capacities of the two drugs are both not lower than 5%. The preparation method comprises the following steps: slowly adding a solution containing cinobufagin and zinc nitrate into a mixed solution containing indocyanine green, bovine serum albumin and 2-methylimidazole, and carrying out centrifugal filtration, washing and drying on a reaction product to obtain the cinobufagin zinc oxide. The multifunctional nano-particles prepared by a one-step synthesis method are uniform in particle size and good in stability, indocyanine green and cinobufagin are uniformly distributed in a carrier, the multifunctional nano-particles have pH and near-infrared light dual response drug release characteristics, triple synergy of chemotherapy, photothermal therapy and photodynamic therapy can be realized, and the multifunctional nano-particles are simple in preparation process and suitable for popularization and application.

The invention provides an application of resibufogenin or a pharmaceutically acceptable salt thereof in preparation of a medicine for treating atherosclerosis. The NLRP3 inflammasome is a multi-protein complex and participates in regulation and control of innate immune response, and abnormal activation of the NLRP3 inflammasome is related to occurrence and development of various diseases including atherosclerosis and the like. The resibufogenin targeted NLRP3 inflammasome is found for the first time and can be used for treating atherosclerosis. The NLRP3 inflammasome is used as a key regulatory factor of inflammatory response in atherosclerosis, and the abnormal activation of the NLRP3 inflammasome aggravates the disease progress. The invention provides a more effective anti-inflammatory treatment strategy by targeting the NLRP3 inflammasome.

The invention provides a toad skin extract, a traditional Chinese medicine composition, a traditional Chinese medicine gel ointment, a preparation method and application, and belongs to the technical field of traditional Chinese medicine extraction and traditional Chinese medicine preparations. The preparation method of the toad skin extract comprises the following steps: mixing dried toad skin with an ethanol solution, performing reflux extraction to obtain a toad skin extracting solution, performing centrifugation to obtain supernate, and performing concentration and drying to obtain the toad skin extract. According to the preparation method, the content of bufalin, cinobufagin, resibufogenin and indole alkaloid extracted from the toad skin is increased, the preparation method is stable and feasible, and the prepared toad skin extract can inhibit bacteria. The traditional Chinese medicine gel ointment is easy to coat, smooth and bright in ointment body, good in skin following performance and uncovering and pasting performance, free of residues in stripping, good in adhesiveness, excellent in overall quality and good in reproducibility, has the effects of diminishing swelling and treating acne, is free of acute toxicity, does not cause the conditions of skin erythema and edema, is free of irritation to skin and is high in safety.

The invention relates to a novel medical application of cinobufagin, and the cinobufagin is used as an N-myc protein inhibition / degradation agent and can be used for anti-tumor treatment of neuroblastoma and retinoblastoma.

The invention relates to the technical field of preparation of albumin nano-drugs, in particular to a preparation method and application of a cinobufagin and pentaline albumin nano-drug. When the cinobufagin and pentaline albumin nano-drug is prepared, albumin and cinobufagin and pentaline are stably cross-linked through a chemical cross-linking method to form the cinobufagin and pentaline albumin nano-drug with controllable particle size and stable release, and the invention further discloses application of the cinobufagin and pentaline albumin nano-drug in preparation of anti-pulmonary fibrosis drugs.

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 belongs to the technical field of traditional Chinese medicine quality evaluation, and relates to a quality evaluation method for cinobufagin capsules based on efficacy / toxicity synchronous analysis, which comprises the following steps: S1, screening a plurality of key efficacy / toxicity components in the cinobufagin capsules; S2, obtaining the contents of the plurality of key efficacy / toxicity components; S3, obtaining the IC 50 values of the plurality of key efficacy / toxicity components; S4, determining the weight coefficients of the plurality of key efficacy / toxicity components by using an AHP (analytic hierarchy process) method according to the IC 50 value sizes; S5, obtaining the weighted total contents of the plurality of key efficacy / toxicity components according to the contents and the weight coefficients of the plurality of key efficacy / toxicity components; and S6, comparing the weighted total contents with the clinical safety content limit to complete the quality evaluation. The method can balance the conversion relationship between the efficacy and toxicity of various components in the cinobufagin capsules, and can ensure the safety and effectiveness of the cinobufagin capsules for clinical medication by using the synchronous analysis of efficacy and toxicity.

This invention discloses a compound preparation of toad skin and its preparation method, which is made by processing dried toad skin, astragalus, and tortoise shell powder in a certain proportion. Compared with the prior art, this invention has the effects of invigorating qi and tonifying the kidney, detoxifying and relieving pain. The formulation of this invention is more reasonable, and it has significant curative effects on mid-to-late stage tumors, chronic hepatitis B and other diseases, without any toxic side effects.

The invention discloses a preparation method of a cinobufagin / ganoderan nanoparticle composite sustained-release preparation, and relates to a composite sustained-release preparation as well as a preparation method and application thereof. The invention aims to solve the problems of high toxicity and the like caused by short in-vivo half-life period and wide whole-body distribution of cinobufagin in anti-tumor application. According to the cinobufagin / ganoderan nanoparticle composite sustained-release preparation disclosed by the invention, due to introduction of gel coating, the cinobufagin / ganoderan nanoparticle composite sustained-release preparation has a more lasting sustained-release property, the treatment effect of cinobufagin can be played for a long time, toxic and side effects are reduced, the cinobufagin is prevented from being cleared by multiple organs, most of medicines act on target organs, and a very good treatment effect is achieved. The good anti-tumor effect is realized; meanwhile, the damage to organs is reduced.

The invention belongs to the technical field of biological medicines, and particularly discloses application of cinobufagin to preparation of a product for treating temozolomide drug-resistant tumors. The invention provides a novel treatment mode which is safe, exact in curative effect, low in price and simple in administration method and is used for treating temozolomide drug-resistant tumor patients, and particularly, application of cinobufagin to preparation of products for treating temozolomide drug-resistant tumor patients is discovered. Therefore, the compound has a wide application prospect in the aspects of treatment and repair of temozolomide-resistant tumors, glioma, glioblastoma and other diseases.

The invention discloses venenum bufonis, venenum bufonis active ingredients and application of a venenum bufonis active ingredient composition in relieving inflammatory pain and bone cancer pain, and belongs to the technical field of venenum bufonis analgesic active ingredient research. It is found that the venenum bufonis medicinal material can relieve inflammatory pain and bone cancer pain, and it is clear that the main active ingredients of the venenum bufonis medicinal material are cinobufagin and resibufogenin; the cinobufagin and the resibufogenin have a good analgesic effect in a certain ratio range, inflammation pain can be relieved when the mass ratio of the cinobufagin to the resibufogenin is 4: 5-5: 1, and bone cancer pain can be relieved when the mass ratio of the cinobufagin to the resibufogenin is 1: 10-5: 1. The active ingredients cinobufagin and resibufogenin are enlightenment that cinobufagin and resibufogenin can become substitutes of endangered medicinal material venenum bufonis for relieving inflammation pain and bone cancer pain; in addition, it is found for the first time that the analgesic effect of resibufogenin is similar to that of morphine, no addiction exists, and it is prompted that resibufogenin is expected to be developed into a novel analgesic drug.

The invention discloses a quality detection method of cinobufagin capsules, which is characterized in that according to active ingredients with different properties in the cinobufagin capsules, analysis conditions such as optimal mobile phase composition, gradient elution mode and mass spectrum condition are screened out through a large number of experiments. According to the UPLC-Q / TOF-MS qualitative analysis method established by the invention, 51 compounds are identified in total. Besides, the fingerprint spectrum of the cinobufagin capsule is established, the content of 11 functional components in the cinobufagin capsule is measured, the HPLC method is good in precision, repeatability and stability, the characteristics of the main components in the cinobufagin capsule are reflected more comprehensively, and reference is provided for improvement of the quality standard and comprehensive development and application of the cinobufagin capsule. The method also has important significance for controlling the quality of cinobufagin capsules and ensuring the clinical curative effect.

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 relates to the field of quality analysis and evaluation of Chinese patent medicines, and particularly provides a toad skin extract and a separation method of chemical components of a preparation of the toad skin extract or a construction method of a fingerprint spectrum and a quality control method. Octadecylsilane chemically bonded silica is used as a filler, a mobile phase comprises acetonitrile and water, gradient elution is carried out, a specific elution procedure is obtained through a large number of experiment screening, and the fingerprint spectrum is obtained. The method realizes effective separation of seven characteristic peaks of bufotalin, arenobufogenin, bufagin, deacetylcinobufotalin, telocinin, bufotalin and cinobufotalin, has the advantages of good peak shape, stable base line, complete separation of the measured components, short detection time, rapidness and high efficiency, provides a basis for quality detection and control of cinobufotalin tablets, and has a wide application prospect. The integrity and characteristics of cinobufagin tablets can be fully reflected, the operation is simple, and the specificity is strong.

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 present invention discloses the use of toad venom, its active ingredients, and a combination of its active ingredients in relieving inflammatory pain and bone cancer pain, belonging to the technical field of research on analgesic active ingredients of toad venom. The present invention discovers that toad venom can relieve inflammatory pain and bone cancer pain and clarifies that its main active ingredients are cinobufagin and resefobufogenin. Cinobufagin and resefobufogenin have a good analgesic effect within a certain ratio range. A mass ratio of cinobufagin to resefobufogenin of 4:5 to 5:1 can relieve inflammatory pain, and a mass ratio of cinobufagin to resefobufogenin of 1:10 to 5:1 can relieve bone cancer pain. The present invention also provides the suggestion that the active ingredients cinobufagin and resefobufogenin can become substitutes for the endangered medicinal material toad venom in relieving inflammatory pain and bone cancer pain. In addition, the present invention discovers for the first time that resefobufogenin has an analgesic effect similar to that of morphine and is non-addictive, suggesting that it has the potential to be developed into a new analgesic drug.

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.