5 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.

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.

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.