6 results about "Evodiamine" patented technology

The application belongs to the technical field of medicines, and particularly relates to an ester group substituted evodiamine derivative, a preparation method and application, and a structural formula is as follows: The application shows excellent inhibitory activity on HT-29, HTC-116, LOVO, RKO, HGC-27, MGC-803, SGC-7901, Huh7, SK-EP1 and MCF-7 tumor cell lines, and can show good antitumor activity at an animal level.

This invention belongs to the field of pharmaceutical application technology, specifically relating to an antifungal evodiamine derivative and its use in the preparation of antifungal substances. The structural formula of the evodiamine derivative is as follows: R1, R2, and R3 are independently H, halogen, or C1-3 alkyl groups; n1 is 1-3; the group is located at the 1, 3, or 4 position of the benzene ring; R4, R5, and R6 are independently C1-3 alkyl groups. The evodiamine derivative has an antifungal effect, especially against Trichophyton rubrum or Trichophyton mentagrophytes, expanding the selection range of antifungal drugs, reducing the possibility of drug-resistant strains, and improving the inhibitory effect on drug-resistant bacteria.

The invention belongs to the field of biological pharmacy, and particularly discloses application of evodiamine in inhibition of migration and invasion of gallbladder cancer cells and metastatic tumor growth. Aiming at the problems of poor drug targeting, high toxicity, easy drug resistance and the like in gallbladder cancer hepatic metastasis treatment, the invention provides various application forms of evodiamine: 1) an evodiamine single-drug sustained release preparation (PLGA or chitosan carrier) realizes long-acting sustained release through local intervention or intratumor injection; 2) the evodiamine liposome preparation (the ratio of DPPC to cholesterol is 3: 1, and the particle size is 80-150nm) can improve the enrichment rate of hepatic metastatic focus to 5.8% or above; (3) the evodiamine and chemotherapeutic drugs (oxaliplatin, 5-FU and the like) are combined to form a composition, and the synergy index is Cilt; 0.8, the toxicity of the system is obviously reduced; animal experiments show that the liver metastasis inhibition rate reaches 82.7% and the weight loss rate is only 10.5% when the liposome (3 mg / kg of evodiamine and 6 mg / kg of oxaliplatin) is combined, and a high-efficiency and low-toxicity solution is provided for gallbladder carcinoma metastasis.

The present application relates to a kind of methods based on transcriptome sequencing, machine learning and molecular docking analysis of evodiamine treatment vestibular schwannoma (VS), the present application is analyzed by integrating transcriptome sequencing technology and GEO database, combined with machine learning algorithm, molecular docking and molecular dynamics simulation method, the potential key target and signal pathway of evodiamine treatment VS are systematically analyzed, provide technical support for the mechanism research of evodiamine, and provide reference basis for future individualized treatment strategy of VS.

The invention discloses a method for analyzing a toxic target of evodiamine based on a network toxicology system. The method comprises the following steps: SA, locking the toxic target; wherein the step SA comprises the following steps: step SA1, obtaining a potential toxic target spot of evodiamine of each toxic object in at least two toxic objects; sA2, locking a core toxic target spot of each toxic object; step SA3, locking a comprehensive core toxicity target spot; the comprehensive core toxicity target spot is a core toxicity target spot simultaneously existing in all toxic objects; wherein the sequence of the step SA1 and the step SA2 is not different. Based on the steps, the method not only locks the core toxicity target spot of each toxicity redemption, but also further locks the core toxicity target spots existing in all toxic objects at the same time, and can help to guide subsequent research to preferentially and sequentially determine research key points, improve research efficiency and save manpower and material resources.

This invention belongs to the field of pharmaceutical technology, specifically relating to a water-soluble evodiamine derivative and its application, with the following structural formula: wherein X is a C1-6 alkylene group or X together with R forms R1 and R2 independently selected from hydroxyl or C1-20 alkoxy groups; R is a hydroxyl group with or without alkylene group, a carboxyl group with or without alkylene group, a C1-20 oxane group, an amino group, a substituted amino group with or without alkylene group, or a heterocyclic amino group with or without alkylene group. This invention can improve its water solubility and antitumor effect.