78 results about "Parthenolide" patented technology

The present invention relates to bioactive ingredients that include isolated bioactive fractions derived from cell juice of fresh biomass of a feverfew (Tanacetum parthenium) plant. The bioactive fractions are either free of or substantially free of α-unsaturated γ-lactones (e.g., parthenolide). Further, the bioactive fractions have anti-inflammatory and antioxidant activity. The present invention also relates to a method for isolating a bioactive fraction that is derived from cell juice of fresh biomass of a feverfew (Tanacetum parthenium) plant and that is at least substantially free of α-unsaturated γ-lactones (e.g., parthenolide). The present invention also relates to a method for preparing a stabilized cell juice serum fraction and a stabilized concentrated cell juice serum fraction that are free of α-unsaturated γ-lactones (e.g., parthenolide). The present invention also relates to a bioactive composition that includes a mixture of one or more of the isolated bioactive fractions of the present invention.

The invention relates to a method for extracting parthenolide, in particular to a method for extracting parthenolide from root barks of magnolia delavayi, magnolia liliiflora and magnolia denudate. Parthenolide is obtained by using the root barks of magnolia delavayi, magnolia liliiflora and magnolia denudate as raw materials, grinding, extracting with polar organic solvent, properly extracting with organic solvent to obtain total lactone, separating total lactone by column chromatography, collecting necessary components, and crystallizing with proper solvent. The method for extracting parthenolide from root barks of magnolia delavayi, magnolia liliiflora and magnolia denudate provided by the invention is suitable for industrial production.

The invention relates to a preparation method and an application of sphaelactone; according to the preparation method, the sphaelactone of the invention is obtained by using parthenolide as a raw material, using a proper acid as a catalyst, with a certain solvent and under a certain reaction temperature; the invention also provides a pharmaceutical application of sphaelactone, that is, the application of a pharmaceutical composition containing a treatment-effective dose of sphaelactone and a pharmaceutically acceptable carrier in the preparation of medicaments for treating cancers. The preparation method of the present invention solves the technical defect of low preparation yield of sphaelactone, provides a sphaelactone yield of up to above 60%; and the sphaelactone has almost identical effect with parthenolide in treating leukemia, and has no obvious killing effect on normal cells.

The present invention relates to a synthetic method of derivatives of parthenolide lactone. Parthenolide lactone and nitrogen-containing compounds are used as the raw materials of the reaction; ethanol sodium is used as a catalyst; the mixture reacts in a certain solvent and at a certain temperature; thus the derivatives of the parthenolide lactone can be prepared. After acidification, the salts of the derivatives can be prepared with greatly improved water solubility. The improved salts of the derivatives of the parthenolide lactone can be used for preparing injection so as to better treat tumors.

The invention relates to an extraction and preparation method of parthenolide, and particulary relates to an extraction method of parthenolide from Magnolia grandiflora root bark. The extraction and preparation method comprises: crushing Magnolia grandiflora root bark as a raw material, extracting with an appropriate polar organic solvent to obtain total lactones, separating the total lactones by column chromatography, collecting the required ingredients, and then crystallizing the collected ingredients with an appropriate solvent to obtain parthenolide. The extraction method of parthenolide from Magnolia grandiflora root bark provided by the invention is suitable for industrial production.

The present invention provides compounds of the formula (I)

wherein:

X₁, X₂ and X₃ are heteroatoms;

R₄, R₅, P₆, R₇, R₈, R₉ and R₁₀ are independently selected from H, halo, —OH, —NO₂, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and

Z is optionally substituted C_1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR¹—, —C(O)NR¹NR²—, —C(O)O—, —OC(O)—, —NR¹CO₂—, —O—, —NR¹C(O)NR²—, —OC(O)NR¹—, —NR¹NR²—, —NR¹C(O)—, —S—, —SO—, —SO₂—, —NR¹—, —SO₂NR¹—, —NR¹R², or —NR¹SO₂—, wherein R¹ and R² are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR¹R², R¹ and R² optionally together with the nitrogen atom form an optionally substituted 5-12 membered ring, said ring optionally comprising 1 or more heteroatoms or a group selected from —CO—, —SO—, —SO₂— and —PO—; or a pharmaceutically acceptable salt, ester or prodrug thereof.

Methods of treating migrainous headaches and their associated symptoms are provided by administering a composition comprising parthenolide or feverfew sublingually to a patient in need thereof. Treatments are surprisingly effective with low total administered amounts of parthenolide or feverfew. Compositions and unit dose systems are also described.

The invention discloses application of parthenolide as a platelet-activating factor (PAF) inhibitor. The parthenolide can be used as a safe PAF antagonist to be applied to treatment, auxiliary treatment and prevention of diseases such as thrombus, atherosclerosis, ischemic cardio-vascular disease, cerebral ischemia, acute pancreatitis, endotoxic shock, asthma, hepatic fibrosis and hepatocirrhosis, injury of nerve, gastrointestinal ulcer and necrosis, psoriasis, systemic lupus erythematosus and acquired immune deficiency syndrome related to platelet-activating factor.

The present invention discloses compounds for the treatment of cancer and its application. These compounds comprises one of the following compound: Ammonium pyrrolidinedithiocarbamate Bay 11-7085 BIO Brefeldin A (+)-Butaclamol Calcimycin Calmidazoliur chloride Chelerythrine chloride CK2 Inhibitor 2 CGP-74514A hydrochloride CGS-12066A meleate Dequalinium dichloride Dihydroouabain Diphenyleneiodonium chloride Emetine dihydrochloride hydrate GR 127935 hydrochloride Nifedipine 6-Nitroso-1,2-benzopyrone Palmitoyl-DL-Carnitine chloride Parthenolide PD 169316 1,10-Phenanthroline monohydrate 4-Phenyl-3-furoxancarbonitrile Prazosin hydrochloride Protoporphyrin IX disodium Quinacrine dihydrochloride Quabain Retinoic acid p-hydroxyanilide Rottlerin Sanguinarine chloride Tetraethylthium disulfide and SU 9516. The invention also provides new uses of these compounds, compounds such as for the preparation of the treatment of cancer, inhibit cancer cell, cancer stem cell growth and provides a new pharmaceutical composition for treating cancers

The invention relates to a botanical pesticide bactericide and a preparation method thereof. The bactericide is obtained through extracting whole herb of Dendranthema lauandulifolium and through processing. Main active components of the bactericide comprise 5-20wt% of parthenolide, water and a surfactant, and are processed to prepare an emulsion in water, and the emulsion in water is used to prevent and control various crop diseases after being diluted. The bactericide has the advantages of easily available raw materials, simple process, low cost, good prevention and control effect on rice bacterial leaf blight, rice bacterial streak, Bipolaris maydis and other diseases, high safety to crops, and no pollution to environment, and is a biological pesticide preparation suitable for Chinese nuisance-free agricultural product production requirements.

The invention relates to a method for preparing parthenolide, and in particular relates to a method for synthesizing parthenolide by using costunolide as a raw material through the following reaction steps in the specification.

The invention discloses an absorption-promoting facial mask, which comprises luteolin, melon seed gold saponin, parthenolide, propylene glycol, nicotinamide, glycerin, glycerol glucoside, butylene glycol and the like. Luteolin in the facial mask has strong reducing properties, can restore excess free radicals in cells, restore damaged antioxidant enzyme activity, and repair cells damaged by oxidation; melon seed gold saponin can reduce cell metabolic loss, Enhance the activity of antioxidant substances, and further assist in the repair of oxidatively damaged cells; feverfew can effectively regulate cell metabolism and promote the absorption of other active ingredients. Several ingredients work synergistically to achieve anti-oxidation, promote skin repair and promote the absorption of active ingredients; in addition, the mask with strong moisturizing effect can significantly improve skin texture, whiten skin at the same time, reduce dark yellow, spots and other skin problems.

The invention belongs to the technical field of cell culture mediums, and specifically relates to a serum-free chondrocyte culture medium and a preparation method thereof. The serum-free chondrocyte culture medium comprise a basic culture medium and an additive, wherein the additive is prepared from the following ingredients in final concentration: 24-32ng/mL of cell factor, 7-10mg/mL of polylysine, 2-5 microns of arachidonic acid, 10-15 microgram/mL of vitamin C, 5-8 microgram/mL of parthenolide, 5-9 microns of butanediamine, 7-9 microgram/mL of insulin, 3-6 microns of linoleic acid, 14-18 microgram/mL of flavone, 12-16 microgram/mL of transferrin, 20-26 microgram/mL of polyvinylpyrrolidone, 8-13 microgram/mL of glucagon, and 20-32 ng/mL of fibronectin. The serum-free chondrocyte culture medium provided by the invention does not contain serum, is low in cost and in favor of scale application.

Compounds of the formula having anti-tumor activity, wherein R₁ and R₂ are as described herein.

The invention discloses an application of parthenolide in preparation of a lung cancer treating drug. EMT (epithelial-mesenchymal transition) of lung cancer cells is reversed through parthenolide, so that growth, invasion or metastasis of the lung cancer cells is inhibited. Embodiments of the invention comprise experimental study including an MTT test, Transwell, a scratch test, immunofluorescence and the like on cells and animals, and results show that parthenolide can reverse EMT of the lung cancer cells, so that parthenolide inhibits invasion and metastasis of the lung cancer cells of small cell lung cancer and non-small cell lung cancer and can have a remarkable effect on tumor cancer treatment.

The invention provides novel application of parthenolide, luteolin, chrysoeriol and ginsenoside Rg3, and specifically relates to preparation of the compounds or derivatives of the compounds in preparation of drugs for preventing and/or treating drug-resistant BRAF (V600E) mutant-type tumors. It is found that proliferation of tumor cells resistant to BRAF (V600E)-targeted drugs can be inhibited through parthenolide, luteolin, chrysoeriol and ginsenoside Rg3, the tumor cells include inherent and acquired tolerant tumor cells, and growth of tumors is inhibited. It is shown through results that parthenolide, luteolin, chrysoeriol and ginsenoside Rg3 have the potential to be developed as the safe and effective drugs for treating the drug-resistant BRAF (V600E) mutant-type tumors.

The invention belongs to the technical field of plant extraction, and relates to a method for extracting a manglietia fordiana total sesquiterpene lactone extract. The method comprises the following steps: crushing a dry sample of a manglietia fordiana plant material, and adding hydrous lower alcohol to perform ultrasonic extraction; filtering, performing pressure reduction and solvent recovery on filtrate, and extracting to obtain a crude extract by using an ester solvent; and then performing column chromatography separation and purification on the crude extract, and collecting required components to obtain the manglietia fordiana total sesquiterpene lactone extract. The method disclosed by the invention is simple in process, can be used for avoiding parthenolide decomposition and damages caused by long-term immersion by adopting an ultrasonic extraction technology, can be used for saving the extraction time, and has the advantages of high yield, low cost and easy industrial production; and the obtained extract is high in parthenolide content and clear in effective components, has anti-tumor effects, and can be used for producing various medicinal preparations with the anti-tumor effects.

The present invention relates to derivatives of the sesquiterpene lactone micheliolide, methods and compositions for their preparation, and methods for using the micheliolide derivatives in pharmaceutical compositions as anticancer and anti-inflammatory agents. The invention also relates to methods for producing micheliolide derivatives modified at positions C2 and C14. The invention also relates to methods for producing parthenolide derivatives modified at positions C2 and C14 in conjunction with modifications at position C13, via chemoenzymatic methods. The invention further relates to methods for using parthenolide derivatives for treating cancer and inflammatory diseases.

The invention relates to a parthenolide derivative, and a medicinal composition, a preparation method and a use thereof. The parthenolide derivative is a compound represented by formula (I), is used for treating cancer diseases, the medicinal composition contains a therapeutically effective amount of the parthenolide derivative (I) and a pharmaceutically acceptable carrier or other anticancer medicines, and the use of the derivative is an application of the derivative in medicines, especially an application in the preparation of cancer treatment medicines.

A method for continuously efficiently extracting parthenolide from southern magnolia leaves comprises the steps of after crushing fresh southern magnolia leaves as a raw material, taking a polarity organic solvent as an extractant, extracting by adopting a constant temperature gradient serial extraction process, concentrating an extraction solution under reduced pressure with microwaves, and then through the simple processes of washing with water to remove impurities, decoloring, drying and the like, obtaining the parthenolide extract with the purity of 95%. Waste residue and waste liquor generated in the extraction process are subjected to the simple processes of purification, decoloring, drying and the like to make into low purity products with different parthenolide contents. Through the method, the extraction rate of the parthenolide can be furthest improved, and the prepared products with different concentrations can well adapt to different market demands. The whole extraction process is low in device requirement and high in extraction efficiency and raw material use ratio. The use level of a solvent can be reduced by 20% by the special constant temperature gradient serial extraction process, and the production cost is far lower than that of a traditional extraction process.

The invention discloses a transport preservation fluid for umbilical cord mesenchymal stem cells. The transport preservation fluid is prepared from the following raw materials: a sodium chloride injection, alpha-mangostin, hesperidin, parthenolide, glucose, adenosine and sodium dihydrogen phosphate. The transport preservation fluid for umbilical cord mesenchymal stem cells takes the sodium chloride injection as a main component, does not contain blood products such as serum, human serum albumin and the like, and has clear and safe components. Three components of alpha-mangostin, hesperidin and parthenolide are also added as protective agents, so that the cell membrane is protected, the situation that the cell internal space structure is disordered due to the fact that the local electrolyte concentration of the cell is increased after the cell is cooled is avoided, the cell is enabled to quickly adapt to a low-temperature environment, and cell inactivation is avoided. The invention further provides a transport preservation method of the umbilical cord mesenchymal stem cells, by adopting the transport preservation fluid, short-term preservation of the cells at 4-8 DEG C is achieved, the survival rate of the cells after being preserved for 3 days is 90% or above, and clinical use requirements are fully met.

The invention provides a parthenolide dithiocarbamate derivative represented by formula (I), a salt and a medicinal composition thereof, and a use of the derivative, the salt or the medicinal composition, and concretely relates to a use of the parthenolide dithiocarbamate derivative and the salt thereof in the preparation of medicines for treating cancers and assistant medicines for treating cancers.