98 results about "Dihydroartemisinin" patented technology

The invention discloses a deoxyartemisinin B synthase and an application of an isoenzyme A0A2U1PPI9 of the deoxyartemisinin B synthase in catalysis of dihydroartemisinin acid for biosynthesis of dihydrodeoxyartemisinin B. The invention further discloses a preparation method of the deoxyartemisinin B synthase. The invention discloses a process for biosynthesizing dihydrodeoxidized artemisinin B from dihydroartemisinin for the first time in a biosynthesis pathway of artemisinin, and bioinformatics analysis and in-vitro activity verification of candidate enzymes show that both the deoxidized artemisinin B synthase and the isoenzyme A0A2U1PPI9 have a new function of catalyzing the biosynthesis of dihydrodeoxidized artemisinin B from dihydroartemisinin, so that the application of the deoxidized artemisinin B synthase and the isoenzyme A0A2U1PPI9 to the biosynthesis of dihydrodeoxidized artemisinin B is developed. Lines of artemisinin biosynthetic pathways are enriched, and a theoretical basis is provided for analysis of terminal biosynthetic pathways of artemisinin and heterologous synthesis of artemisinin compounds.

The invention belongs to the technical field of biomedicine, and particularly relates to application of GABA (gamma-aminobutyric acid) driven by lactobacillus rhamnosus to treatment of cerebral malaria of mice. According to the invention, the obviously enriched lactobacillus muricatum is found, and the lactobacillus muricatum is proved to be capable of generating GABA (gamma-aminobutyric acid). Afterwards, on the mouse cerebral malaria model, under the condition that the lactobacillus rhamnosus and the GABA are independently used or auxiliary dihydroartemisinin is used, the effect of the lactobacillus rhamnosus and the GABA on improving and treating the mouse cerebral malaria is evaluated. Results show that the strain and the metabolite GABA thereof can effectively improve behavioristics of mice and immune pathological injuries of all organs, reduce protozoemia and prolong the lifetime of the mice whether the strain is independently used or combined with dihydroartemisinin, and can effectively treat cerebral malaria of the mice compared with the strain which is independently used with drugs. The invention provides a brand-new solution for treating severe malaria, especially human brain malaria, caused by malignant malaria from the perspective that the probiotics drive metabolites of the probiotics to assist the anti-malarial drug in treating rat brain malaria.

The invention belongs to the technical field of biomedicine, and particularly relates to application of Ackermania muciniphila in improvement and treatment of cerebral malaria caused by Plasmodium berghei. The invention tries to evaluate the effect of the AKK bacterium on improving and treating the cerebral malaria of a mouse under the condition that the AKK bacterium or auxiliary medicines (dihydroartemisinin, rapamycin and atorvastatin) are independently used on a cerebral malaria model of the mouse. Results indicate that the strain can effectively improve behavioristics of mice and immune pathological injuries of all organs, reduce protozoemia and prolong the lifetime of the mice whether the strain is independently used or combined with the drugs, and compared with the strain which is independently used with the drugs, the strain can effectively treat cerebral malaria of the mice. As ackermania muciniphila is common probiotics in human intestinal tracts, the three drugs (dihydroartemisinin, rapamycin and atorvastatin) used in the invention are all clinically used drugs, and if the drugs are clinically transformed to treat human brain malaria caused by plasmodium falciparum, the feasibility is high, and meanwhile, the transformation time can be shortened. According to the invention, a bacterium-medicine synergistic concept is provided for the first time, that is, probiotics can assist medicines in treating diseases, and a solution is provided for treating human cerebral malaria under the guidance of the concept.

The invention relates to a nano assembly for self-synergistically enhancing ferroptosis as well as a preparation method and application of the nano assembly, and belongs to the technical field of pharmaceutical preparation combined treatment of new auxiliary materials and new dosage forms. The invention firstly provides a functional conjugate linker capable of automatically generating ROS, the functional conjugate linker comprises artesunate-ferrocene or dihydroartemisinin-ferrocene, and the structural formulas of the functional conjugate linker and the artesunate-ferrocene or dihydroartemisinin-ferrocene are respectively shown as a and b. According to the present invention, the ROS self-generating functional conjugate linker and the ferroptosis inducer are co-assembled to form the nanometer assembly, such that the ROS level in the tumor cells can be effectively and synergistically improved by the ROS self-generating functional conjugate linker and the ferroptosis inducer so as to cause the tumor cell lipid peroxidation storm, and the ferroptosis induction effect can be significantly improved. The co-assembled nano preparation provided by the invention provides a new strategy and more choices for developing the delivery of drugs, and meets the urgent requirements of efficient and diversified ferroptosis-based cancer treatment strategies on preparations in clinic. # imgabs0 #

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 present invention belongs to the field of biomedical technology and specifically relates to the use of Akkermansia muciniphila in ameliorating and treating cerebral malaria caused by Plasmodium berghei. This study evaluated the efficacy of Akkermansia muciniphila alone or in combination with adjuvant drugs (dihydroartemisinin, rapamycin, and atorvastatin) in ameliorating and treating cerebral malaria in a mouse cerebral malaria model. The results suggest that the bacteria, whether used alone or in combination with other drugs, effectively improved mouse behavior, immune pathological damage to various organs, reduced parasitemia, and prolonged mouse survival, demonstrating its effectiveness in treating cerebral malaria in mice compared to using the drugs alone. Because Akkermansia muciniphila is a common probiotic in the human gut, the three drugs used in this study (dihydroartemisinin, rapamycin, and atorvastatin) are all currently in clinical use. Clinical translation for the treatment of human cerebral malaria caused by Plasmodium falciparum is highly feasible and can also shorten the conversion time. This study proposes for the first time the concept of bacterial-drug synergy, whereby probiotics can complement drug treatments, and provides a solution for the treatment of human cerebral malaria based on this concept.

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 present invention discloses the application of deoxyartemisinin B synthase and its isoenzyme A0A2U1PPI9 in catalyzing the biosynthesis of dihydrodeoxyartemisinin B from dihydroartemisinin acid. In the biosynthetic pathway of artemisinin, the present invention for the first time discloses the process of the biosynthesis of dihydrodeoxyartemisinin B from dihydroartemisinin acid. Through bioinformatics analysis and in vitro activity verification of candidate enzymes, it is shown that both deoxyartemisinin B synthase and its isoenzyme A0A2U1PPI9 have the new function of catalyzing the biosynthesis of dihydrodeoxyartemisinin B from dihydroartemisinin acid, enriching the route of the artemisinin biosynthetic pathway and providing a theoretical basis for the analysis of the terminal biosynthetic pathway of artemisinin and the heterologous synthesis of artemisinin compounds.

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 relates to a high-stability dihydroartemisinin emulsion which is prepared by the following steps: preparing a mixed solution from dihydroartemisinin, sodium bicarbonate and polyethylene glycol 600, carrying out loading treatment in a carbon dioxide supercritical extraction instrument by taking glycerol and n-butyl alcohol as a composite solvent to form an intermediate product, and specifically, after running for 1-2 hours under the conditions that the CO2 flow is 10-15kg / h, the pressure is 15-20Mpa and the temperature is 35 DEG C, increasing the pressure to 25-30Mpa, keeping the temperature for 1-2 hours, and carrying out constant-temperature extraction to obtain the dihydroartemisinin emulsion. The temperature is raised to 45-50 DEG C and kept for 30-60 min, a product is collected and placed at the room temperature after the temperature is raised to 45-50 DEG C, an intermediate product is obtained, and the intermediate product is added into an emulsion matrix to form the nano-emulsion. The transfer rate of the dihydroartemisinin in the prepared intermediate product reaches 94.37%, the particle size of the loaded nano intermediate product is uniformly distributed at about 50nm, the prepared emulsion is uniform, the dihydroartemisinin has excellent stability in the system, the dihydroartemisinin is not easy to decompose in environments of long-term high temperature, high-humidity illumination and the like, the stability of the emulsion property is excellent, and the stability of the product is good. The problems of layering, sedimentation and the like are avoided, and the bioavailability is excellent.

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 invention provides a dihydroartemisinin water-soluble derivative and a preparation method thereof, and belongs to the field of chemical synthesis. The stachyose is functional tetraoligosaccharide composed of two alpha-galactose, one alpha-glucose and one beta-fructosyl, has good stability, is very easy to dissolve in water, and is insoluble in organic solvents such as ethanol and the like; and the stachyose, as a functional oligosaccharide, has the effects of improving gastrointestinal health, protecting the liver, improving the immunity of the organism, delaying senescence, reducing blood fat and blood pressure, resisting tumors and the like, so that the stachyose can effectively stimulate the growth of bifidobacteria and other beneficial bacteria in intestinal tracts. Based on the fact, stachyose is selected to modify the structure of dihydroartemisinin, so that the water solubility, the stability and the bioavailability of dihydroartemisinin are remarkably improved on the basis of keeping the original activity, and absorption of intestinal tracts and preparation of oral medicines are facilitated.

The invention discloses a PLGA (poly (lactic-co-glycolic acid)) targeted drug composite material as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The preparation method of the PLGA targeted drug composite material comprises the following steps: dissolving astaxanthin, dihydroartemisinin and a polylactic acid-glycolic acid copolymer in an organic solvent to obtain a mixed solution, adding the mixed solution into a surfactant solution, loading the astaxanthin and dihydroartemisinin on the polylactic acid-glycolic acid copolymer to form drug-loaded PLGA, and preparing a dispersion liquid; and adding an activated hyaluronic acid solution into the dispersion liquid, and stirring to wrap the hyaluronic acid on the drug-loaded PLGA to obtain the PLGA targeted drug composite material. The dihydroartemisinin and the astaxanthin are loaded on the polylactic acid-glycolic acid copolymer and coat the hyaluronic acid, and the active targeting function of the hyaluronic acid targets inflammatory macrophages at a focus part, so that the nano composite material is effectively utilized by target cells, and the atherosclerosis prevention and treatment effect of the nano composite material is improved.

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 invention discloses an active oxygen response type polymer prodrug micelle, and further discloses a polymer prodrug micelle loaded with oridonin or dihydroartemisinin and a polymer prodrug micelle loaded with the oridonin and the dihydroartemisinin at the same time. The invention further provides a preparation method of the polymer prodrug micelle. The ORI and DHA co-loaded active oxygen responsive polymer prodrug micelle provided by the invention can significantly improve the water solubility and biocompatibility of ORI and DHA, can effectively eliminate reduced glutathione in gastric cancer cells AGS cells and amplify active oxygen, and finally causes the generation of a large amount of lipid peroxides, thereby killing tumor cells and inducing cell ferroptosis, and has a good application prospect. And finally, tumor proliferation is inhibited.

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 relates to the technical field of biological medicine, and discloses a co-crystal medicine ZM851 and application thereof in lung cancer resistance, a preparation method of the co-crystal medicine ZM851 comprises the following steps: mixing osimertinib, dihydroartemisinin and a mixed solvent, heating, stirring and dissolving, then adding normal hexane, and separating out a yellow solid, namely the co-crystal medicine ZM851. The antitumor activity shown by the eutectic molecule ZM851 in the invention is more than ten times that shown by a non-eutectic mixture of the eutectic molecule ZM851. In addition, in an in-vitro experiment, the ZM851 shows a remarkable inhibition effect on an osimertinib drug-resistant cell strain. The eutectic drug ZM851 has a remarkable inhibition effect on osimertinib drug-resistant cell strains in an in-vitro experiment, which indicates that the eutectic drug ZM851 possibly provides a new treatment scheme for clinical treatment of lung cancer patients.

The present invention provides a pharmaceutical composition for preventing and / or treating neuropathic pain or complications, wherein the active ingredients of the pharmaceutical composition include an artemisinin compound and pregabalin, wherein the artemisinin compound is selected from one or more of dihydroartemisinin, artemether and artesunate, preferably dihydroartemisinin. The combined use of dihydroartemisinin and pregabalin of the present invention has obvious advantages in treating the core symptoms of neuropathic pain, reducing drug side effects and reducing drug tolerance.

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.

The invention relates to a crystallizing tank for preparing dihydroartemisinin, which comprises a tank body and a crystallizing reaction shell positioned in the tank body, a mixed solution is positioned in the crystallizing reaction shell, and the crystallizing reaction shell is connected with the tank body through a central shaft. After the crystallization reaction shell is controlled to rotate in the tank body by taking the central shaft as a central axis, a mixed solution in the crystallization reaction shell rolls, and insoluble substances in the mixed solution are filtered out by the separation and filtration assembly; compared with the prior art, the device has the beneficial effects that when the dihydroartemisinin crude product is purified and processed, the dihydroartemisinin crude product and an ethanol solvent are put into the crystallization reaction shell, and then the lower half part of the crystallization reaction shell is heated through the heating assembly, so that dihydroartemisinin is promoted to be dissolved in the ethanol solvent; in the process, the crystallization reaction shell rotates, so that the mixed solution rolls back and forth in the crystallization reaction shell, and the dissolution of the dihydroartemisinin crude product is facilitated.

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.