170 results about "Cantharidin" patented technology

The invention discloses a pyrazolo N-substituted dehydronorcantharidin imide derivative as well as a synthesis method, an activity test method and application thereof, belonging to the field of cantharidin derivatives. The pyrazolo N-substituted dehydronorcantharidin imide derivative has a structural general formula shown as a formula 1: in the formula 1, R1 is H, C1, F, CH3, OCH3, OH or NO2; and R2 is 2-phenyl-2H-1,2,3-triazole-4-substituent or quinoxaline-2-substituent. The novel N-substituted dehydronorcantharidin imide derivative introduces five-membered heterocyclic pyrazole rings into norcantharidin substituted arylamine and has favorable anti-tumor activity.

The invention discloses a method for extracting cantharidin, including extraction and recrystallization process. The said extraction process includes: (1) cold maceration process: drying and meshing mylabris worms into 40-60 meshes, adding maceration solvents and stirring for 5-10 h, and vacuum-filtering at a mylabris worms/hydrochloric acid/acetone weight ratio of 1:0.01-0.05:3-9; (2) concentration and standing process: concentrating and distilling the filtrate at 40-60degreeC until no liquid flows out, cooling to room temperature, and placing for 5-9 hours; and (3) washing process: vacuum-filtering the concentrated liquid, and washing with the mixed solution of ethanol and petroleum ether for several times until the liquid clears up. Compared with the existing technology, this invention has the advantages of simplified process, short production cycles, simple operation, and high yield (increase by 50% compared with the existing technology).

The invention discloses a making technique of sodium cantharidate, which comprises the following steps: processing canthariasis; extracting cantharidin; purifying; refining; synthesizing sodium cantharidate; purifying sodium cantharidate.

Provided are methods for treating cancer in a patient, comprising administration of a therapeutically effective regimen of cantharidin or cantharidin analog of formula of formula I, II or III

wherein R¹, R², R³, R⁴, R⁵, R⁶, R⁷, R⁸, R¹¹, R¹², A, Y and Z are as set forth herein, or a pharmaceutically acceptable salt thereof, to a patient in need thereof. In some embodiments of the methods, the therapeutically effective regimen stabilizes, reduces or eliminates cancer stem cells. In some embodiments of the methods, the therapeutically effective regimen reduces or eliminates cancer cells.

The invention provides a compound having anticancer activity, which is obtained by cooperation of Norabieta cantharidin and platinum (IV) and modification of a piperazine derivative. The compound is characterized in that a Norabieta cantharidin piperazine derivative ligand is introduced, thereby cytotoxicity of a platinum (IV) compound is reduced, and high antineoplastic activity is provided. The result of the cytotoxicity experiments shows that the provided platinum (IV) compound has less destruction to normal mice fibroblast L929, but has good killing effect to cancer cells such as human breast cancer MCF-7 cell, human cervical carcinoma HeLa cell and human lung adenocarcinoma A549 cell, so that the compound having anticancer activity is capable of reducing the system toxicity and having equal anticancer activity with cisplatin. The compound having anticancer activity has good killing effect by aiming at cisplatin resistance human lung adenocarcinoma A549/DDP cell. Therefore, the toxicity is reduced, the cisplatin resistance can be reversed, and anticancer effect of the platinum medicines can be increased.

The invention provides a camptothecin-site 20 norcantharidate derivative with a structural formula as shown in I which is described in the specification, and a preparation method and antineoplastic application thereof. Results of activity test prove that the camptothecin-site 20 norcantharidate derivative as shown in I is an appropriate candidate antineoplastic drug, especially a candidate drug for resisting liver cancers, stomach cancers and colorectal cancers. Compared with positive contrast drugs, i.e., camptothecin and cantharidin, the camptothecin-site 20 norcantharidate derivative has improved water solubility and stability; and the camptothecin-site 20 norcantharidate derivative is sensitive to acid and can be easily hydrolyzed. Moreover, the preparation method for the camptothecin-site 20 norcantharidate derivative employs easily available raw materials, has high yield and is easy to operate and implement.

A method of treating acquired perforating dermatosis. The method has the step of applying an amount of cantharidin to an area of skin in need of treatment thereof.

The present invention provides a preparation method of cantharidin-loaded tumor cell membrane-encapsulated tellurium elementary substance nanoparticles and belongs to the field of nano biomedicine. The nanoparticles prepared from tellurium elementary substance as a core, cantharidin as a model drug and tumor cell membranes as an outer layer coating. The tellurium nano-material and the cantharidinhaving toxic and side effects on organisms are encapsulated by the tumor cell membranes in the nanoparticles, so that biocompatibility of the nanoparticles is improved, immune cells are effectively prevented from being cleared, and the nanoparticles have homologous targeting capability; after intravenous injection, the nanoparticles are massively gathered at tumor sites through an EPR effect and ahomologous targeting property, the tellurium elementary substance is rapidly heated under near-infrared stimulation to cause outer cell membrane rupture, and the leaked cantharidin inhibits a heat shock reaction of tumor cells, enhances a photo-thermal treatment effect of the tellurium elementary substance, and kills tumor cells. The method is reasonable in design, simple in preparation technology and wide in application prospect, and lays a foundation for design and development of a corresponding drug delivery system.

The invention discloses potassium cantharidate of a structural formula below. The preparation method comprises: adding trichloromethane or isopropanol into pure cantharidin according to a weight ratio of (30-50):1, heating to dissolve the trichloromethane or isopropanol, and adding distilled water into potassium hydroxide according to a molar ratio of the potassium hydroxide to the cantharidin of 3:(2-3) to prepare solution at a weight concentration of 10 percent; adding the solution of potassium hydroxide into the trichloromethane or isopropanol solution containing cantharidin, heating the mixed solution to 60 to 75 DEG C, volatilizing trichloromethane or isopropanol till dryness, and filtering to obtain colorless transparent solution; and adding trichloromethane or isopropanol in a volume which is 2 to 5 times that the filtrate into filtrate, separating to obtain upper colorless transparent aqueous solution, placing the colorless transparent aqueous solution in an oven for concentration and drying to obtain white crystalline powder. The potassium cantharidate has high anticancer activity, the process is simple, easy to operate and very safe, and the finished product is stable in properties and high in purity.

Disclosed is a Chinese medicament for treating ecthyma and its preparing process, which is prepared from the following medicinal materials (by weight portion): zanthoxylum piperitum 10-15, bunge corydalis herb 10-15, Chinese ephedra 10-15, banksia rose 15-20, native copper 15-20, Chinese gall 5-10, cantharidin 0.5-1, allume 5-10, orpiment 5-10, mercurous chloride 0.5-1 and red precipitate 0.5-1.

The invention discloses a process for preparing sodium cantharidinate, which comprises the following steps: treating cantharis; extracting cantharidin; purifying; refining; synthesizing the sodium cantharidinate; purifying and refining the sodium cantharidinate, and the like. The invention has the advantages of simplicity, practicability, good safety, high purity of prepared finished products, stable quality, low production cost, and the like and can be applied to the production of various dosage forms of big injections, big transfusions, tablets, granules, capsules, oral liquid, ointments, and the like.

The invention discloses a pesticide composition containing cantharidin, which comprises the following constituents (by mass percent): cantharidin 0.1-10.0%, insecticide 0.1-30.0%, and balancing auxiliary agent for pesticides.

The invention discloses a bromo-norcantharidin acid-benzyl ester shown as a structural formula I. The bromo-norcantharidin acid-benzyl ester is an open-loop 5,6-dibromo-norcantharidin acid benzyl ester, and an active test proves that the bromo-norcantharidin acid-benzyl ester has a good anti-liver-cancer effect and can be used as a high-efficiency and low-toxicity cantharidin anticancer medicine The synthesis process is excellent in selectivity, raw materials are readily available, the cost is low, the synthetic route is simple, operation is easy, a product obtained by the synthesis has low toxicity, high yield and high purity, and the process is high-efficiency, convenient and low in cost.

The invention relates to a method for extracting cantharidin from cantharides. The method is characterized by comprising the following steps of: performing continuous countercurrent ultrasonic extraction on powder of cantharides by using acetone, removing impurities from an extracting solution, concentrating under reduced pressure, evaporating to remove partial solvent, and cooling and crystallizing a concentrated solution to obtain a crude product of cantharidin; heating to dissolve the crude product by using chloroform, filtering to remove insoluble substances, and cooling and crystallizing filtrate to obtain the cantharidin. The continuous countercurrent ultrasonic extraction is adopted, the impurities are removed from the extracting solution by an elutriation method, and recrystallization is carried out by using the chloroform, so that the cantharidin with the content of over 98 percent is obtained, steps of degreasing by using an organic solvent and the like are eliminated, the operation is simple, the production is safe, the extraction yield is high, and the method is suitable for mass production.

The present invention is freeze dried demethyl sodium cantharidinate powder for injection and its preparation process, and belongs to the field of medicine technology. The freeze dried demethyl sodium cantharidinate powder for injection contains demethyl cantharidin 0.25-70 wt%, sodium hydroxide 0.1-35 wt% and excipient 0-99 wt%. The preparation process includes compounding demethyl cantharidin and sodium hydroxide in liquid compounding tank, adding injection water and heating to dissolve, adding excipient, dissolving and regulating pH value; adding proper amount of carbon for injection, stirring for 30 min for adsorption, filtering to eliminate carbon and sterilize, packing in Schering bottle, and freeze drying to obtain the freeze dried demethyl sodium cantharidinate powder for injection. The medicine is clinically used in treating liver cancer, esophagus cancer, hepatitis, etc.

The invention provides a novel process for preparing cantharidin from cantharides. The process comprises the following steps of: by using supercritical CO2 as a solvent and acetone as an entrainer, performing static immersion of the cantharides for 1 to 1.5 hours at an extraction pressure of 10 to 20MPa and an extraction temperature of between 30 and 40 DEG C, performing dynamic extraction for 2 to 3 hours at an analytic pressure of 4 to 8MPa and an analytic temperature of between 40 and 50 DEG C, removing impurities from the obtained extracts by using petroleum ether, and crystallizing the obtained extracts by using acetone. The process has the advantages of high extraction efficiency, short period, little pollution and low cost.

The invention belongs to medical domain; it has disclosed a compound medicine that contains cantharidin orits derivates and at least one kind of medicine that can improve the immunity, the preparing method and application is also mentioned in the invention. The medicine that can improve immunity is chosen from one kind or various kinds of lentinan, ganoderma and hoelen. The medicine can be used to treat liver cancer, esophageal cancer, carcinoma of gastric cardia, lung cancer, malignant lymphoma and low blood corpuscle; it can also be used to treat hepatitis, cirrhosis or HB virus; it can be used as preoperative drug for cancer operation or be used in combination chemotherapy with the function of coordinated synergistic action. The product in the invention has good stability and the effects have been greatly improved than the single application of Norcantharidin, lentinan, ganoderma and hoelen. The medicine can be made into any medically acceptable dosage with any medically acceptable accessories so it has wide prospects.

The invention relates to a freeze-dried powder of sodium norcantharidin for injection and a preparation method for the freeze-dried powder: adding the norcantharidin and mannitol into well prepared sodium hydroxide solutions and adjusting the ph; adding activated carbon and removing colors, filtering and removing the carbon and finely filtering through a 0.22Mu m filtering film and making loading separately; cooling the separately loaded medical solution rapidly to minus 60 to minus 55 DEG C with the speed of 15 to 25 DEG C per minute; preserving heat and freezing for 3 hours and pumping the vacuum of 5 to 15 Pa; heating slowly and uniformly to minus 5 to 5 DEG C with the speed of 3 to 3.5 DEG C per hour and preserving the heat for 2 to 5 hours and then heating with a uniform speed to 20 to 30 DEG C with 3 to 6 heating hours; preserving heat and drying for 5 hours and detecting, pressing a whole cover and packaging and warehousing. The freeze-dried powder obtained by the method is high in purity, beautiful in appearance and low in water content and the proportion of the nor cantharidin, the sodium hydroxide and the mannitol is provided as 2 to 1 to 20.

The invention belongs to the technical field of medicine. The invention discloses a norcantharidin liver-targeting liposome, a preparation method thereof and the application of a freeze-dried preparation. The norcantharidin liver-targeting liposome of the present invention is connected with a glycyrrhetic acid derivative on the surface of the liposome, which can be combined with the glycyrrhetic acid receptor on the surface of liver tumor cells and undergo endocytosis, thereby producing a tumor-suppressing effect. ; Norcantharidin is encapsulated in liposomes, which has better drug bioavailability and enhanced curative effect. The norcantharidin liposome freeze-dried preparation prepared by the invention has good stability, safety and reliability, is easy to store, and is beneficial to industrialized production.