104 results about "Artemisinins" patented technology

The invention discloses a clathrate compound of artemisinin series (artemisinin, dihydroartemisinin and artesunate) and alkaline cyclodextrin and a method for preparing the same. The alkaline cyclodextrin in the clathrate compound refers to an amido-substituted cyclodextrin; and due to the amido substituting of the cyclodextrin, an alkaline environment is formed in an aqueous solution apart from clathration between the cavity of the cyclodextrin and the artemisinin series, and forms ionic interaction with hydroxyls or carboxyls on the artemisinin series; and therefore, the artemisinin series can be dissolved in water to form a solution within an extremely wide concentration range so that liquid artemisinin series preparations can be formed. The clathrate compound provided by the invention is high in stability, high in bioavailability, simple in preparation, easy for operation, moderate in condition, and suitable for industrial production.

A new formulation and process of producing a new formulation of artemisinin in the form of a complexation of artemisinin with beta-cyclodextrins. This new formulation of artemisinin having greater aqueous solubility, a higher dissolution rate and an improved bioavailability.

The invention discloses application of artemisinin and derivatives thereof in preparing medicaments for preventing and treating neurological diseases. In the application, the nerve cell line of rat adrenal pheochromocytoma PC12, retinal nerve cell line RGC-5 and primary cortical neuron are on behalf of experiment objects, sodium nitroprusside and hydrogen peroxide are used to simulate and induce oxidative stress, cell apoptosis and other cell injuries of nerve cells. Researches discover that the artemisinin has a protective effect on sodium nitroprusside and hydrogen peroxide induced cell injury, the protective effect mechanism of the artemisinin and derivatives thereof is primarily discussed, and results indicate that the artemisinin and derivatives thereof can be used as nerve protection medicaments for preventing and treating various neurological diseases, such as various neurodegenerative diseases, acute and chronic neurodegenerative diseases, neurological eye disease and the those neurological diseases mainly related to oxidative stress injuries and cell apoptosis. The application brings a new direction to treatment and prevention of neurological diseases.

The present invention relates to an isolated DNA sequence encoding a polypeptide having the biological activity of amorpha-4,11-diene synthase. This DNA sequence can be used for the transformation of bacteria, yeasts and plants for the production of amorpha-4,11-diene, a specific precursor in the synthesis of artemisinin, in the respective organisms. The invention also relates to these organisms.

The invention discloses Artemisia annua wax handmade soap and a production method thereof. The Artemisia annua wax handmade soap includes Artemisia annua essential oil, Artemisia annua soap base, Artemisia annua extract and the like, wherein the Artemisia annua soap base is obtained by saponifying Artemisia annua wax, and the Artemisia annua extract mainly includes artemisinin and chlorophyll. The preparation process of the invention is simple and efficient, various effective substances in Artemisia annua are made full use, cost is greatly reduced, and this soap has significant effects such as sterilization, baceriostasis, skin care, and inflammation diminishing.

The invention relates to [(10S)-9,10-dihydroartemisinine-10-oxyl]benzaldehyde semicarbazones (sulfur) series substances and provides a structure, a preparation method and application of a novel artemisinine 10-locus derivative. The structural formula of the [(10S)-9,10-dihydroartemisinine-10-oxyl]benzaldehyde semicarbazones (sulfur) series substance is shown in a formula I. The invention also relates to pharmaceutically-acceptable slats, a solvate, an optical isomer or a polymorphic substance of the [(10S)-9,10-dihydroartemisinine-10-oxyl]benzaldehyde semicarbazones (sulfur) series substances and a medicinal composition by taking the compounds as active components. As novel antimalarial agents, anti-tumor agents and antifungal agents, the compounds can be used for treating or preventing malaria, mycotic infection, malignant tumor and the like. The compounds can be prepared by reacting dihydroartemisinine as an initial raw material with trifluoroacetic anhydride / triethylamine to obtain 10(R)-trifluoro-acetoxyl-9,10-dihydroartemisinine, directly reacting the 10(R)-trifluoro-acetoxyl-9,10-dihydroartemisinine with hydroxy benzaldehyde without separation to obtain (10S)-9,10-dihydroartemisinine-10-oxyl]benzaldehyde, and reacting the (10S)-9,10-dihydroartemisinine-10-oxyl]benzaldehyde with the substituted amino (sulfur) urea compounds in acid catalysts and alcohol solvents to obtain target compounds.

The present invention relates to an improved method for the preparation of Artemether. Artemether prepared from the process is useful for the treatment of uncomplicated, severe complicated and multi drug resistant malaria.

The invention provides new application of artemisinin and a derivative thereof, namely that the artemisinin or the derivative thereof is directly used as a sensitizer for thermodynamic therapy, and isused for thermodynamic therapy of tumors; or a liposome nano-composite prepared from the artemisinin and the derivative thereof and indocyanine green is used as a sensitizer for the thermodynamic therapy, and is used for thermodynamic therapy and / or photothermal therapy of the tumors. when being used for thermodynamic therapy of the tumors, the artemisinin or the derivative thereof and the liposome nano-composite not only show excellent tumor targeting performance, but also have extremely high synergistic photothermal therapy and thermodynamic therapy anti-tumor activity, and have remarkableadvantages as an anti-cancer drug.

The present invention provides a method for the preparation of arteether from artemisinin in one pot in just about 4 hours comprising reduction of artemisinin into dihydroartemisinin by less quantity of sodium borohydride in ethanol at room temperature in the presence of a novel polyhydroxy catalyst, acylation of dihydroartemisinin in the presence of an acid catalyst, extraction of arteether from an aqueous reaction mixture using 1% ethyl acetate in n-hexane followed by workup and purification of the impure arteether to yield 80-86% (w / w) pure alpha, beta arteether.

The invention provides a method for extracting scopoletin. The method comprises the following process steps of: performing heating and refluxing extraction on artemisia annua residues from which artemisinin is extracted and which serves as the raw materials by using methanol, acetone, ethyl acetate or dichloromethane under the conditions of temperature of 53 DEG C and vapor pressure of 0.06 MPa, concentrating; separating by column chromatography; and crystallizing and the like. The artemisia annua residues serve as the raw materials, so the method can be in seamless connection with the production line of industrialized extraction of the artemisinin, investment of purchasing the raw materials is saved and the cost of the raw materials is greatly reduced. The method is easy to operate. By the method, the scopoletin can be effectively extracted; and the purity of the scopoletin in the obtained extracts is high.

The invention relates to a novel fluorescence resonance energy transfer (FRET) probe Rho-Bob, which is constructed by connecting rhodamine B (Rho) with an N2O type benzopyrrole boron complex (Bobpy),and is used for OH ratio type fluorescence detection and imaging. Rho-Bob shows the characteristic of being sensitive to the hydrophilicity / hydrophobicity of the environment, and has excellent mitochondrial localization capability. Rho-Bob is successfully applied to intracellular .OH ratio type fluorescence imaging. The .OH can be generated by a Fenton reaction, and can also be generated by activation of intracellular drugs. The Rho-Bob probe has high selectivity and sensitivity to hydroxyl radicals, and the detection limit is as low as a nanomole level (680nM). According to the invention, .OHgenerated by artemisinin molecules in cell mitochondria is observed for the first time by using Rho-Bob, and endogenous hydroxyl radicals are found to exist in zebra fish gastrointestinal tracts (GI)under normal culture conditions for the first time. The invention not only provides the practical probe for .OH detection and imaging, but also provides an important thought for constructing novel ratiometric probes of other ROS.

The present invention relates to an artemisinin molecular imprinting composite film, a preparation method and applications thereof, and belongs to the technical field of environmental material preparation. The present invention especially relates to a method comprising the following steps: adopting a polyvinylidene fluoride membrane as a substrate, firstly activating the surface of the polyvinylidene fluoride membrane, then making up a combination of cupric bromide and 2, 2-bipyridine as a catalyst system, selecting artemisinin as a template molecule, acrylamide as a functional monomer and ethylene glycol dimethacrylate as a crosslinking agent, conducting activator generated by electron transfer for atom transfer radical polymerization, and synthesizing the artemisinin molecular imprinting composite film by one-step method. The adsorption balance, dynamics and selective recognition performance of the imprinting film prepared in the present invention is studied by static adsorption experiments, the results show that the imprinting film prepared in the present invention has very rapid absorption dynamic properties and superior artemisinin molecular recognition performance, and can be used for selective recognition and separation of artemisinin.

The invention discloses a ferroptosis-inducing nano-composite, a preparation method and application of the ferroptosis-inducing nano-composite in tumor treatment. The preparation method comprises the following steps of: dissolving an artemisinin medicine and an oral iron supplementing agent in an organic solvent to obtain a solution I; dispersing lactoferrin in an inorganic solvent to obtain a solution II; and adding the solution I into the solution II, and uniformly mixing under ultrasonic waves to obtain the ferroptosis-inducing nano-composite. The nano-composite prepared in the invention is loaded with the artemisinin medicine and the oral iron supplementation agent, has the characteristics of simple components and small toxic and side effects and can induce ferroptosis of tumor cells, the anti-tumor effect of the nano-composite is enhanced by regulating macrophages to be in an anti-tumor phenotype through cooperation with innate immunity, and the nano-composite can be used in the field of anti-tumor research.

The invention provides a multifunctional anti-tumor nano-drug. The synergistic effect of an artemisinin derivative and sodium nitroprusside serves as the core content of anti-tumor treatment. The nanoparticles are used as a carrier, a fluorescent / photo-thermal material, an artemisinin derivative and sodium nitroprusside are loaded or coated, and a thermal phase change material is coated outside the carrier. In a tumor environment, sodium nitroprusside reacts with glutathione overexpressed in tumor cells to generate nitric oxide gas, so that gas therapy is realized. When nitric oxide is generated, sodium nitroprusside also can generate a large amount of low-valent iron ions, so that peroxy bridged bonds of the artemisinin derivatives are triggered to break, a large amount of active oxygen is generated, and tumor cells are effectively killed. The raw materials are wide in source, the preparation process is simple and easy to operate, and the prepared nanoparticles loaded with the artemisinin derivatives and the sodium nitroprusside have good water solubility, dispersity and biocompatibility and are an ideal multifunctional cancer treatment reagent.

Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions containing the same derivatives and the use thereof are disclosed. The artemisinin derivatives have following formula I. It has been proved by pharmacological tests that these compounds and compositions have evident immuno-suppressive activities, and may be used in the preparation of novel immuno-suppressants for treating the diseases caused by hyperfunction of human immunity (e.g. the auto-immune diseases such as lupus erythematosus, rheumatoid arthritis, multiple sclerosis and the like), and for inhibiting the graft rejection after cell or organ transplantation.

The invention discloses an artemisia annua wax handmade soap and a preparation method thereof. The artemisia annua wax handmade soap includes artemisia annua volatile oil, artemisia annua wax soap base, artemisia annua extract and other components; wherein the artemisia annua wax soap base is A substance obtained by saponification of artemisia annua wax. The artemisia annua extract mainly includes artemisinin and chlorophyll. The preparation process of the invention is simple and efficient, makes full use of various effective substances in Artemisia annua, saves a lot of costs, and has significant sterilization, bacteriostasis, skin care, anti-inflammatory and other effects.

The invention relates to a method and equipment for scale production of artemisinin. The method comprises: dissolving dihydroarteannuic acid in an organic solvent, adding a photosensitizer and an acid catalyst, adopting a light source to make the dihydroarteannuic acid be subjected to light oxidation so as to obtain peroxy alcohol of the dihydroarteannuic acid, carrying out acid catalysis so as to carry out Hock cut-off, and carrying out oxidation ring closing to produce the artemisinin, wherein the whole reaction or only the light oxidation reaction is performed in photosensitive oxidation reaction equipment. The present invention further comprises the photosensitive oxidation reaction equipment for performing the method. According to the present invention, the method has characteristics of low reaction temperature and high light source utilization rate, and the equipment has characteristics of high light source utilization rate, simple structure, low manufacturing cost, and high single-batch productivity.

The present invention generally relates to sensitizer compounds and their use in combination with Tyrosine Kinase Inhibitors (TKIs) for sensitizing tumor, cancer or pre-cancerous cells to TKI treatment. In particular, the present invention relates to administration regimes that combine TKIs such as Gefitinib or Icotinib with TKI-sensitizing DZ1 esters and amides conjugated to statin or platin-based drugs, or to Artemisinin, including, without limitation: DZ1-Simvastatin amide, DZ1-Simvastatin ester, DZ1-Cisplatin ester, and DZ1-Cisplatin amide, DZ1-Artemisinin ester, and DZ1-Artemisinin amide. Furthermore, the present invention relates to improved TKI treatment of cancers by sensitizing tumor, cancer or pre-cancerous cells, in particular cancers that develop TKI resistance, including e.g. lung cancer and pancreatic cancer.

The invention relates to a method for preparing caffeoylquinic acid, which comprises the following steps of fetching 100g of artemisia annua industrial extraction remainder obtained after extracting artemisinin with chloroform, and adding into a solution of which the pH is 5.0 and the methanol-water ratio is 5:1 according to a solid-liquid ratio of 1:20 (w / w); leaching for 5 hours under the water bath effect; performing solid-liquid separation to obtain extraction liquid containing caffeoylquinic acid; performing liquid-liquid extraction separation to obtain 3.1g of caffeoylquinic acid with purity of 64%; separating through a chromatographic column and purifying to obtain 1.4g of caffeoylquinic acid with purity of 95%.

The invention discloses a phthalocyanine-artemisinin conjugate used as a sonodynamic / photodynamic sensitizer as well as a preparation method and application of the phthalocyanine-artemisinin conjugate. The phthalocyanine-artemisinin can be self-assembled in water. In water, the conjugate efficiently generates active oxygen under an ultrasonic action, and can be used as a sonosensitizer. Meanwhile, the conjugate and the self-assembly thereof can generate active oxygen under the action of light, and can also be used as a photosensitizer. The phthalocyanine-artemisinin conjugate obtained by the invention can generate an effective sonodynamic therapy anti-tumor effect, also has a remarkable sonodynamic and photodynamic synergistic anti-tumor effect, and has a remarkable application prospect in the aspect of preparing sonodynamic therapy and sonodynamic / photodynamic synergistic therapy drugs.

The invention relates to a method for selectively extracting and separating artemisinin / artemisitene by using a hydrophilic ionic liquid, which comprises the following steps: mixing an aqueous solution of an ionic liquid and an organic solvent solution of artemisinin / artemisitene, oscillating at constant temperature, standing, respectively taking an ionic liquid phase and an organic solvent phase, fixing the volume by using methanol, and detecting the concentration of artemisinin and artemisinene in the raffinate phase (organic solvent phase) and the extract phase (ionic liquid phase) to obtain separation selectivity. The ionic liquid aqueous solution can highly selectively extract artemisitene from the artemisinin crude product, and then the raffinate phase is directly cooled and crystallized to obtain the artemisinin product. The method is suitable for removing low-content artemisitene, is simple to operate, is green, and can realize high-selectivity separation of artemisinin / artemisitene.

The present invention relates to the treatment of leukemia, (e.g. acute myeloid leukemia, AML) using a triple combination of: arsenic trioxide; iron; and an artemisinin, such as artesunate.

The invention relates to a preparation method for and application of a molecularly imprinted composite membrane initiated by a surface functional monomer prepolymerization system, belonging to the technical field of material preparation. According to the invention, a regenerated cellulose membrane is used as a substrate material, artemisinin is used as a template molecule, acrylamide is used as a functional monomer, and ethylene glycol dimethacrylate is used as a cross-linking agent; and through combined usage of an imprinting prepolymerization system, the surface artemisinin molecularly imprinted composite membrane is prepared on the surface of the regenerated cellulose membrane modified by the surface functional monomer by using two-step polymerization. Static adsorption experiments are conducted to research adsorption equilibrium, kinetic performance, selective recognition performance and selective permeation performance of the prepared molecularly imprinted composite membrane. Experiment results show that the artemisinin molecularly imprinted composite membrane prepared in the invention has high adsorption capability and superior artemisinin molecule recognition and permeation performance.

The invention discloses a pharmaceutical composition for treating the Alzheimer's disease. The pharmaceutical composition is characterized in that the composition is a preparation prepared from an effective dosage of industrial cannabis leaves, artemisinin, a series of derivatives and pharmaceutically acceptable auxiliary materials thereof. The composition can effectively relieve the Alzheimer's disease. The pharmaceutical composition is large in safety dosage range and good in curative effect and has the good development prospect. By applying the medicine technology, the novel development direction is supplied to medicine application of industrial cannabis, and the good social and economical benefits are achieved.

The invention provides a composition prepared from artemisinin antimalarials and aminoquinoline antimalarials; the composition is suitable for treating the cancers, such as lung cancer, breast cancer and melanoma, has low side effect, and is effective in improving cancer treatment effect and reducing the development and progress of a patient's complications.

The invention aims to provide an artemisinin-coumarin heterozygous molecule, a method for preparing the same and application of the artemisinin-coumarin heterozygous molecule, provides pharmaceutically acceptable salt, solvate, an optical isomer or a polymorphic substance of the artemisinin-coumarin heterozygous molecule and further provides a medicine with a derivative or salt of the derivative. The derivative or the salt of the derivative is an active ingredient of the medicine. Structural formulas of compounds or the pharmaceutically acceptable salt, the solvate, the optical isomer or the polymorphic substance are shown as a formula (I), wherein an L in the formula represents O, O(CH<2>)<n>O, the n is equal to 0-3, and an R1 and an R2 in the formula independently represent hydrogen atoms, halogen, hydroxyl, C1-C10 carboxyl, C1-C10 ester, cyan, nitro, C1-C10 alkyl, C1-C10 alkoxy, C3-C7 naphthene, halogenated C1-C10 alkyl and halogenated C1-C10 alkoxy.

The invention relates to the technical field of medical materials, and discloses an anti-cancer medical adhesive. The medical adhesive is prepared from the following raw materials: artemisinin, alpha-cyanoacrylic acid n-butyl ester and alpha-cyanoacrylic acid n-octyl ester. The ratio of the artemisinin to the alpha-cyanoacrylic acid n-butyl ester to the alpha-cyanoacrylic acid n-octyl ester is any ratio. Through the anti-cancer effect of the artemisinin, the effects of stopping bleeding and closing an incision after a tumor operation and preventing tumor cell resection residues are achieved. The problems that in the prior art, the wound healing efficiency after a tumor operation is insufficient, and metastasis of tumor cells remaining on the wound and the postoperative recurrence probability are difficult to reduce are solved. Artemisinin is firstly dissolved in alpha-cyanoacrylic acid n-butyl ester, and then mutual dissolution with alpha-cyanoacrylic acid n-octyl ester in any proportion is achieved, and thus the beneficial effects of improving the healing efficiency of the postoperative wound and reducing the metastasis of tumor cells left in the wound and the postoperative recurrence probability are achieved. The invention also provides a preparation method and application of the anticancer medical adhesive.

The invention relates to a method and equipment for preparing artemisinin by adopting dihydroarteannuic acid as a raw material. The method comprises: dissolving dihydroarteannuic acid in an organic solvent, adding a photosensitizer and an acid catalyst, adopting a light source to make the dihydroarteannuic acid be subjected to light oxidation so as to obtain peroxy alcohol of the dihydroarteannuic acid, carrying out acid catalysis so as to carry out Hock cut-off, and carrying out oxidation ring closing to produce the artemisinin, wherein the whole reaction or only the light oxidation reaction is performed in the photoreactor. The present invention further comprises the photoreactor for performing the method. According to the present invention, the method has characteristics of low reaction temperature, high artemisinin yield and high light source utilization rate, and the equipment has characteristics of simple structure, low manufacturing cost, and high single-batch productivity.

The invention relates to a construction method and a process of engineering bacteria for producing amorpha-4,11-diene. According to the strain for efficiently producing an artemisinin precursor amorpha-4,11-diene, recombinant bacteria are obtained by regulating the expression / or the activity of escherichia coli and an exogenous gene, wherein the gene comprises an acetoacetyl coenzyme A thiolase atoB gene, an HMG-CoA synthase hmgS gene, an HMG-CoA reductase hmgR gene, a mevalonate kinase mevK gene, a phosphohydroxyproline kinase pmk gene, a mevalonic acid-5-pyrophosphoric acid decarboxylase pmdgene, an isopentenyl pyrophosphate isomerase idi gene, a farnesyl pyrophosphate synthase ispA gene and an amorpha-4,11-diene synthase ads gene.

Combinations of betaine and vitamin C are used to suppress or prevent malignant tumors or to treat viruses, e.g., by combining the two ingredients in a product consumed by a human, dog, or cat, such as an aqueous liquid such as grape juice, the ingredients being provided in containers with instructions for use, or in finished products, especially with support of tests demonstrating the effectiveness of the treatment for, e.g., preventing tumors in populations known to be at risk of developing tumors, or, treating existing cancers in combination with other cancer drugs such as anastrozole and / or fulvestrant and / or artemisinin either concurrently or sequentially to prevent the cancer from growing when the cancer drug is not being used, or in the treatment of viruses.