13 results about "Dihydroartemisinin" patented technology

This invention belongs to the field of pharmaceutical technology and relates to a composite nanoparticle that synergistically induces ferroptosis and antitumor immune responses, as well as its preparation method. The invention first provides a dihydroartemisinin dimer prodrug or a pharmaceutically acceptable salt thereof with the following structure. Then, composite nanoparticles are prepared using the aforementioned dihydroartemisinin dimer prodrug or its pharmaceutically acceptable salt as the main drug component. The composite nanoparticles are prepared by covalently binding an albumin-manganese dioxide complex and ferritin, while simultaneously co-encapsulating the dihydroartemisinin dimer prodrug or its pharmaceutically acceptable salt and a photosensitizer. The composite nanoparticles prepared by this invention can disrupt the reducing homeostasis of tumor cells by simultaneously enhancing ROS generation and GSH consumption. PDT and CDT synergistically enhance ROS generation, and manganese dioxide can also promote GSH consumption. These composite nanoparticles can significantly improve drug targeting and significantly enhance antitumor activity.

The application belongs to the field of colorectal cancer treatment, and particularly relates to application of dihydroartemisinin in preparation of colorectal cancer liver metastasis drugs. The application research finds that dihydroartemisinin (DHA) can inhibit expression of mutant KRAS, reshape tumor immune microenvironment, thereby enhancing therapeutic effect of regorafenib combined with PD-1 inhibitor. These findings provide new insights for overcoming drug resistance in KRAS mutant colorectal cancer liver metastasis (CRCLM), and support further development of DHA as an adjuvant drug for combination therapy to improve patient prognosis.

This invention discloses a sensitizer for PD-1 antibody drugs and its application, as well as an antitumor drug composition and its application. The sensitizer comprises dihydroartemisinin and niraparib, and the antitumor drug composition comprises dihydroartemisinin, niraparib, and a PD-1 antibody. This invention is the first to experimentally discover that dihydroartemisinin possesses a dual mechanism of action: "non-HRD-dependent PD-L1 upregulation" and "tumor-selective ferroptosis induction." This mechanism complements and synergizes with niraparib's "HRD-dependent PD-L1 upregulation + synthetic lethality" mechanism and the PD-1 antibody's "immune activation" mechanism. The antitumor drug composition formed by combining these three components can effectively reshape the tumor immune microenvironment, exerting a potent antitumor effect by upregulating PD-L1 expression in tumor cells, increasing the number of cytotoxic T cells, and inhibiting the proportion of regulatory T cells.

The invention relates to the technical field of biological medicine, in particular to a CD90-targeted nano-drug delivery system and application of the CD90-targeted nano-drug delivery system in preparation of a drug for treating alopecia senescens. Efficient loading and stable release of an anti-aging drug dihydroartemisinin (DHA) are realized through the dendritic ordered porous structure; furthermore, the surfaces of the nano-particles are covalently modified by using a CD90-targeting aptamer A15518, so that the nano-particles are endowed with the targeting capability of selectively recognizing the senescent hair follicle stem cells and the microenvironment of the senescent hair follicle stem cells. The nano-drug delivery system provided by the invention can significantly improve the enrichment efficiency of the drug at the hair follicle part, enhance the regulation effect of the drug on the aging-related pathway, and promote the aging hair follicle to enter the growth period, so that the nano-drug delivery system can be used for preparing drugs or related preparations for treating aging alopecia.

The application relates to the field of biological medicine, and discloses a co-crystal drug ZM851 and application thereof in resisting lung cancer, and a preparation method of the co-crystal drug ZM851, which comprises the following steps: mixing osimertinib, dihydroartemisinin and a mixed solvent, heating, stirring and dissolving, and then adding n-hexane; and yellow solid separated out is the co-crystal drug ZM851. The anti-tumor activity of the co-crystal molecule ZM851 is more than ten times that of a non-co-crystal mixture. In addition, in an in-vitro experiment, the ZM851 shows a significant inhibitory effect on an osimertinib-resistant cell strain. The significant inhibitory effect of the co-crystal drug ZM851 on the osimertinib-resistant cell strain in the in-vitro experiment indicates that the co-crystal drug ZM851 can provide a new treatment scheme for lung cancer patients in clinical treatment.

Dihydroartemisinin (“DHA”) derivatives that contain a stereospecific C-10 ether linkage and an aryl pharmacophore moiety are disclosed. In some forms, the DHA derivatives possess anticancer properties that are comparable to or better than the parent DHA and / or an existing anticancer drug (e.g., Cisplatin), and are useful in anticancer treatments (such as ovarian cancer and colon cancer). Methods of synthesizing the DHA derivatives that are cost effective are disclosed. Methods of using the DHA derivatives for treating a cancer, such as ovarian cancer and / or colon cancer, in a subject in need thereof are also disclosed.

The present application relates to a kind of dihydroartemisinin derivatives of structure shown in formula (I) or its pharmaceutically acceptable salt or its stereoisomer, and its application.The dihydroartemisinin derivative synthesized in the present application can significantly inhibit the expression of NLRP3 inflammasome, inhibit the activation of NLRP3 pathway;In the cell model of NLRP3 inflammasome activation, this kind of dihydroartemisinin derivative can inhibit the secretion and release of IL-1β and TNF-α in concentration-dependent manner, so as to be used for treating the disease related to NLRP3 inflammasome activation.

This invention provides the application of dihydroartemisinin in the preparation of drugs for the prevention or treatment of acute lung injury, relating to the field of pharmaceutical technology. The prevention or treatment of acute lung injury includes: reducing lung damage and / or pulmonary edema in lung tissue, decreasing the levels of inflammatory factors in serum and / or bronchoalveolar lavage fluid, reducing oxidative stress markers in lung tissue, reducing the production of reactive oxygen species and / or NO in BEAS-2B cells, and reducing the expression of inflammatory factors in BEAS-2B cells. This invention has verified through in vitro and in vivo experiments that dihydroartemisinin has a good protective effect against acute lung injury, significantly improving lung damage, and possesses anti-inflammatory and oxidative stress-reducing effects, providing a theoretical basis for the development of drugs for acute lung injury.

The invention discloses a sensitizer of a PD-1 antibody drug, an application of the sensitizer, an anti-tumor drug composition and an application of the anti-tumor drug composition. The sensitizer is prepared from dihydroartemisinin and niraparil, and the anti-tumor medicine composition is prepared from dihydroartemisinin, niraparil and a PD-1 antibody. It is found through experiments for the first time that dihydroartemisinin has a double-acting mechanism of'non-HRD dependent PD-L1 up-regulation 'and'tumor selective ferroptosis induction', and functional complementation and effect synergy are formed by dihydroartemisinin, an'HRD dependent PD-L1 up-regulation + synthetic lethal 'mechanism of nirapalide and an'immune activation' mechanism of a PD-1 antibody. The antineoplastic pharmaceutical composition formed by combined use of the three can effectively remodel a tumor immune microenvironment, and synergistically exerts a powerful antineoplastic effect by up-regulating expression of tumor cells PD-L1, increasing the number of killer T cells and inhibiting the proportion of regulatory T cells.

The disclosure belongs to the technical field of biomedicine, and specifically relates to an application of Akkermansia muciniphila (AKK) in the amelioration and treatment of cerebral malaria caused by Plasmodium berghei. The disclosure aims to evaluate the efficacy of AKK alone or in combination with adjuvant drugs (dihydroartemisinin, rapamycin, and atorvastatin) in ameliorating and treating experimental cerebral malaria in an experimental cerebral malaria model. The results indicate that AKK, whether used alone or in combination with drugs, can effectively ameliorate behavioral deficits and immunopathological damage of each organ, lower parasitemia levels, and prolong survival period of mice. Compared with the use of drug alone, the combination therapy can effectively treat the experimental cerebral malaria. The disclosure is the first to propose the concept of bacterial-drug synergy concept, and provides a solution to the treatment of human cerebral malaria on the basis of the concept.

The invention relates to an application of dihydroartemisinin in preparation of medicines for preventing, delaying and / or treating ovarian senescence and related diseases thereof. It is found for the first time that dihydroartemisinin can effectively prevent, delay and / or treat ovarian senescence, including ovarian fibrosis and age-related fertility decline caused by ovarian fibrosis. Dihydroartemisinin significantly improves the ovary structure and function through the multi-target synergistic effect of regulating reproductive endocrine, inhibiting senescence-related phenotypes, resisting ovarian fibrosis and the like, specifically, the oestrus cycle is recovered, the ovary weight is increased, and the ovulation number and the litter size are increased. Moreover, the invention also proves that dihydroartemisinin has the potential of preventing fertility decline in a middle-aged model, is good in safety, does not cause injury to main visceral organs and reproductive organs, has normal liver and kidney function indexes, and provides a new strategy for clinical intervention of ovarian senescence.