42 results about "Dihydroartemisinin" patented technology

The invention discloses an artemisinin derivative nano assembly with anti-tumor activity and a preparation method and application thereof. The nano assembly is formed by self-assembling artemisinin derivatives through intermolecular force and modifying the artemisinin derivatives with a PEG modifier; the artemisinin derivative is artesunate or dihydroartemisinin of which the side chain is binary acid or saturated fatty alcohol or unsaturated fatty alcohol; the mass ratio of the artemisinin derivative to the PEG modifier is (10: 90)-(90: 10), so that the technical effects of high drug loading capacity, good stability, low toxic and side effects and the like are realized, the urgent demand on high-efficiency and low-toxicity preparations in clinic is met, a new strategy is provided for the assembly of homotype synergistic drug nanoparticles, and the application prospect is broad. An effective nano platform is provided for developing a carrier-free nano assembly and a high-efficiency and low-toxicity nano preparation.

The invention relates to the technical field of medical treatment, and particularly discloses dihydroartemisinin-loaded nano-hydrogel, which is prepared from the following components: 5 to 20 percent of gelatin methacryloyl, 5 to 15 percent of nano-hydroxyapatite and 0.5 to 2 percent of dihydroartemisinin, according to the invention, through the constructed Ge MA-nHA-DHA functionalized hydrogel system, the local concentration and bioavailability of dihydroartemisinin are remarkably improved, and the repair and regeneration of bone tissues are promoted. Research results show that the system can effectively inhibit inflammatory response, promote proliferation and differentiation of osteoblasts, improve the structure and function of bone tissues, slow down further collapse of femoral heads and finally improve the living quality of patients. In addition, the biological material shows good biocompatibility and appropriate drug release characteristics when applied in vivo, and a novel effective means is provided for treatment of steroid-induced femoral head necrosis.

The invention discloses an application of artemether, artesunate or dihydroartemisinin in preparation of a medicine for preventing or treating aflatoxin B1 poisoning. Belongs to the technical field of medicine. The technical problem of detoxification of aflatoxin B1 is solved. The invention provides an application of artemether, artesunate or dihydroartemisinin in preparation of a medicine for treating aflatoxin B1 poisoning diseases. The body can be promoted to detoxify the AFB1.

The present invention provides a stable composition comprising, based on the total weight of the composition: 0.01-1 wt% of dihydroartemisinin; 0.1 to 30 wt% of a nonionic surfactant, wherein the nonionic surfactant is PPG-5-cetyl alcohol polyether-20; and an aqueous carrier acceptable in the personal care field. The invention also relates to a personal care product comprising said composition.

The present invention provides a stable composition comprising, based on the total weight of the composition: 0.01-1 wt% of dihydroartemisinin; 5 to 36 wt% of a fatty acyl isethionate salt; and an aqueous carrier acceptable in the personal care field. The invention also relates to a personal care product comprising said composition.

The invention discloses application of dihydroartemisinin in construction of liver organoid, which is characterized in that by adding dihydroartemisinin into a liver organoid culture medium, the maturity of the liver organoid can be obviously improved, the maturity period is shortened, and the liver function characteristics (such as metabolic function and gene expression maturity) of the organoid are enhanced. The defects of an existing liver organ model in the aspect of simulating primary liver functions are effectively overcome, a more accurate in-vitro model is provided for research of liver related diseases, and a new platform and possibility are provided for development of liver regeneration and treatment methods.

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 invention relates to the technical field of pharmaceutical preparations, in particular to a self-nano-emulsification drug delivery system as well as a preparation method and related application thereof. The self-nano emulsifying composition comprises total glucosides of paeony, dihydroartemisinin and auxiliary materials, the auxiliary materials comprise, by mass, 10-45% of an oil phase, 20-68% of RH40 and 12-72% of ethyl alcohol, and the oil phase comprises glyceryl monooleate and medium chain triglyceride. Compared with the prior art, the self-nano-emulsion composition provided by the embodiment of the invention carries total glucosides of paeony and hydrophobic dihydroartemisinin together, realizes simultaneous administration of water-insoluble components and water-soluble components, and improves bioavailability.

The invention provides a transparent water type composition which comprises the following components in percentage by weight: 0.01-1% of dihydroartemisinin, 0.01-1% of an emulsifier, 0.01-1% of an emulsifier, 0.01-1% of an emulsifier, 0.01-1% of an emulsifier, 0.01-1% of an emulsifier and the balance of water. 5-88 wt% of an anionic surfactant, wherein the anionic surfactant is selected from a fatty alcohol sulfate salt, a fatty alcohol polyoxyethylene ether sulfate salt or a combination of the fatty alcohol sulfate salt and the fatty alcohol polyoxyethylene ether sulfate salt; and an aqueous carrier acceptable in the personal care field. The invention also relates to a personal care product comprising said composition.

The invention discloses an alkynylation dihydroartemisinic acid probe, a biotin-dihydroartemisinic acid probe and a preparation method and application of the alkynylation dihydroartemisinic acid probe. The structural formula of the alkynylated dihydroarteannuic acid is as shown in formula 1. And a'biotin-dihydroartemisinic acid 'probe structure is constructed. And co-incubating the probe and a cell lysis solution, co-incubating a lysis solution-probe mixed solution and streptavidin magnetic beads, and eluting to obtain the drug-specific binding protein. According to the invention, the action target of dihydroartemisinin in disease treatment can be quickly, simply and conveniently found.

The invention belongs to the technical field of drug loading systems, and particularly discloses a dihydroartemisinin-loaded pH response type MOF drug loading system and a preparation method and application thereof, and the preparation method comprises the following steps: preparing MIL-101-NH2; preparing HA-FA; preparing MD; and preparing MD-coated HF. According to the dihydroartemisinin-loaded pH response type MOF drug loading system as well as the preparation method and the application thereof, the drug loading system has good pH responsiveness, biocompatibility, antibacterial property and wound healing promoting capability; the preparation method is stable and controllable in process and easy for industrial production; the healing of a wound infected by the staphylococcus aureus is promoted.

The present invention belongs to the field of biomedical technology, and specifically relates to the application of Lactobacillus murinus driving GABA in the treatment of cerebral malaria in mice. The present invention found significantly enriched Lactobacillus murinus and confirmed that Lactobacillus murinus can produce GABA. Subsequently, in a mouse cerebral malaria model, the effects of Lactobacillus murinus and GABA on improving and treating mouse cerebral malaria were evaluated when Lactobacillus murinus and GABA were used alone or in conjunction with dihydroartemisinin. The results showed that whether used alone or in combination with dihydroartemisinin, the bacteria and its metabolite GABA can effectively improve mouse behavior, immune pathological damage to various organs, reduce parasitemia, and prolong mouse survival. Compared with the use of drugs alone, it can effectively treat mouse cerebral malaria. From the perspective of using probiotics to drive their metabolites to assist antimalarial drugs in the treatment of mouse cerebral malaria, the present invention provides a new solution for the treatment of severe malaria caused by falciparum malaria, especially human cerebral malaria.

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.

The invention belongs to the technical field of biological medicines, and discloses a preparation method of a heparin targeted dihydroartemisinin-loaded antimalarial nano-liposome freeze-dried powder drug, and the preparation method comprises the following steps: S1, synthesis of DSPE-PEG2000-heparin: coupling dalteparin and DSPE-PEG2000-NHS through an amination reaction, and carrying out dialysis purification and freeze-drying; s2, dissolving soybean lecithin, cholesterol, a DSPE-PEG2000-heparin polymer and dihydroartemisinin in 5mL of chloroform, evaporating by using a rotary evaporator under low pressure to form a film, and adding deionized water for dissolving; s3, deionized water is added for film hydration, ultrasonic treatment is conducted for 1 min in a water bath at the temperature of 20 DEG C, 100 nm film extrusion treatment is conducted, and HEP-DHA-coated Lips is obtained; and S4, adding a freeze-drying protective agent, and performing freeze-drying to obtain the HEP-DHA-coated Lips freeze-dried powder preparation. The heparin-dihydroartemisinin liposome nanoparticle freeze-dried powder medicine prepared by the invention has excellent anti-malarial performance, and the problems that the traditional dihydroartemisinin is poor in water solubility, short in half-life period and low in bioavailability are solved.

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 present application relates to a kind of dihydroartemisinin derivatives, its preparation method and its application. Specifically, the present application relates to a kind of dihydroartemisinin derivatives shown in general formula (I), its stereoisomer or pharmaceutically acceptable salt, its preparation method and the pharmaceutical composition containing them and the use in the preparation of drugs. The structure of general formula (I) compound is as shown below, and the definition of its group is consistent with the definition in the specification.

The invention provides an anti-dandruff composition of a natural source. The anti-dandruff composition comprises 0.1-2 wt% of dihydroartemisinin; 0.1-2 wt% of a Coptis chinensis extract; and a carrier acceptable in the personal care field. The invention further relates to application of the composition in preparation of personal care products with an anti-dandruff effect. The personal care products are selected from anti-dandruff shampoo, anti-dandruff scalp care lotion, anti-dandruff scalp care essence and scalp care hair masks.

The invention discloses application of dihydroartemisinin in preparation of a medicine for treating and / or relieving osteosarcoma, belongs to the technical field of biomedicine, and particularly relates to application of dihydroartemisinin in preparation of a medicine for treating and / or relieving osteosarcoma. The dihydroartemisinin is found to be capable of inhibiting the activity of osteosarcoma cells, inhibiting the migration ability and invasion ability of the osteosarcoma cells, inhibiting the proliferation ability of the osteosarcoma cells and inhibiting the self-renewal ability of osteosarcoma stem cell-like cells, so that the osteosarcoma is treated and / or relieved.

The present invention provides a stable composition comprising, based on the total weight of the composition: 0.01-1 wt% of dihydroartemisinin; 0.1 to 60% by weight of a nonionic surfactant, the nonionic surfactant being a polysorbate; and an aqueous carrier acceptable in the personal care field. The invention also relates to a personal care product comprising said composition.

The invention belongs to the technical field of drug carriers, and particularly relates to an ROS-responsive dual-targeting drug nano-carrier CD38-PHD / G-NP as well as a preparation method and application of the ROS-responsive dual-targeting drug nano-carrier CD38-PHD / G-NP. The dual-targeting drug nano-carrier CD38-PHD / G-NP disclosed by the invention is co-loaded with GSI and sustained-release dihydroartemisinin (DHA), and a CD38 antibody is modified. The CD38 antibody recognizes T-ALL cells, and the GSI specifically targets Notch1, so that dual targeting is realized. The double-strategy CD38-PHD / G-NPs can realize controlled release of drugs in T-ALL, repair the cytotoxicity of GSI and induce greater ferroptosis, and solves the side effects of gastrointestinal tracts through the CD38 antibody, thereby providing a new view angle for targeted therapy of T-ALL patients.

The present invention provides a stable composition comprising, based on the total weight of the composition: 0.01-1 wt% of dihydroartemisinin; 0.1-30% by weight of fatty alcohol polyoxyethylene ether carboxylic acid or a salt thereof; and an aqueous carrier acceptable in the personal care field. The invention also relates to a personal care product comprising said composition.

The invention discloses dihydroartemisinin / hollow Prussian blue nano-enzyme injectable hydrogel as well as a preparation method and application thereof, and belongs to the technical field of medicines. According to the dihydroartemisinin / hollow Prussian blue nano-enzyme injectable hydrogel provided by the invention, thermosensitive hydrogel is constructed by adopting a two-phase synthesis method, and hollow Prussian blue nano-enzyme loaded with dihydroartemisinin is uniformly loaded in the hydrogel by adopting an in-situ coating technology, so that the hydrogel is endowed with excellent anti-inflammatory and anti-tumor properties. The injectable hydrogel has a good near-infrared light response characteristic, can generate a photothermal effect under the irradiation of exogenous near-infrared light, realizes drug release and photothermal synergistic treatment, effectively improves the anti-inflammatory and anti-tumor treatment efficiency, and reduces the drug resistance risk caused by the use of a single drug.

The invention relates to an anti-tumor self-assembly targeted nano-drug as well as a preparation method and application thereof, and belongs to the technical field of nanotechnology. The self-assembled nano-drug is composed of hemin and dihydroartemisinin and is formed by self-assembling a prodrug with an ROS sensitive bond and hemin, the molar ratio of the prodrug to hemin is 1: 1-1: 10, and the prodrug molecule is formed by connecting a hemin drug molecule with an iron supplementing effect and an artemisinin derivative through the ROS sensitive bond. The invention has the advantages that: the EPR effect is utilized to passively transport to the tumor tissue, the responsive drug release in the tumor tissue is realized, the tumor cells are stimulated to generate ICD, the expression of PD-L1 protein is down-regulated, the immune escape is prevented, and the multi-mechanism tumor killing is realized, so that the immune response of the body is enhanced, the anti-tumor effect is exerted, and the drug effect is improved.

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 invention provides fluorine-modified dihydroartemisinin as well as a preparation method and application thereof, and belongs to the field of dihydroartemisinin derivatives. The fluorine-modified dihydroartemisinin provided by the invention is dihydroartemisinin of which the 12-site hydroxyl group is substituted by a fluorine atom. The dihydroartemisinin is subjected to fluorine modification, so that the combining capacity of the dihydroartemisinin and a target can be enhanced, the activity of the dihydroartemisinin is improved, and the curative effect of the dihydroartemisinin is further improved; a C-F bond formed after fluorine modification improves the metabolism resistance of dihydroartemisinin, the action time of dihydroartemisinin can be prolonged, and the treatment effect is improved. Compared with dihydroartemisinin, the fluorine modified dihydroartemisinin provided by the invention has a better treatment effect.

Disclosed are a novel artesunate-amino acid-targeting group derivative, a nano formulation and a use. The structure of the compound is represented by formula (I), wherein R is as described in the claims and the description. Further disclosed is a nano formulation prepared by means of nanoprecipitation. The target compound has anti-tumor cell proliferation activity superior to that of artesunate, dihydroartemisinin and oxaliplatin, has good therapeutic effects against tumors, and can be used for the preparation of anti-tumor drugs.

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.

The present invention provides a stable composition comprising, based on the total weight of the composition: 0.01-1 wt% of dihydroartemisinin; from 0.1 to 30% by weight of sorbitan laurate; and an aqueous carrier acceptable in the personal care field. The invention also relates to a personal care product comprising said composition.

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.