35 results about "Cucurbitacin B" patented technology

The invention relates to a cucurbitacin liposome composition and its preparation, which has rather high encapsulation efficiency, and can be administered through vein, muscle, oral and nasal. The constituent percentage by weight of the composition are, cucurbitacin BE or cucurbitacin B 0.001-0.1%, phospholipids 0.1-10%, cholesterin 0-5%, the phospholipids can be lecithin, di-stearoyl phosphatidyl choline, di- palmityl phosphatidyl choline, di-oleoyl phosphatidyl choline, di- palmityl phosphatidyl ethanolamine, di-stearoyl phosphatidylglycerol. The preparation according to the invention can be prepared in the form of injection, oral liquid, syrup, drop and nasal spray

The present invention refers to a medicament which activates gastrointestinal movement. The medicament consists essentially of Cucurbitacin D and one or more substances form the group including Cucurbitacin A, Cucurbitacin B, Cucurbitacin E, Isocucurbitacin B and Isocucurbitacin D. The medicament is made from an extract obtained from Muskmelon Base, the fruit stem of Cucumis melo L. The medicament can promote enterokinesia in both normal animals and in animal models where gastrointestinal movement is inhibited. It has also been demonstrated to activate the movements of the stomach, small and large intestines. The extract may be used alone or in combination with the other botanical ingredients or chemical substances to form the pharmaceutical preparation.

The present invention relates to uses of cucurbitacins and compositions comprising cucurbitacin B. The present invention also relates to methods for preventing or treating various diseases and disorders by administering to a subject in need thereof cucurbitacin B. The invention also encompass methods of developing a therapeutic that comprises a cucurbitacin using the signaling molecules in the Ras-Raf-Mek-Elk-STAT3 pathway.

The invention discloses a method for extracting and separating cucurbitacin B, which comprises the following steps: firstly, melon pedicels as a raw material are crushed and are refluxed and extracted by ethanol diacolation or ethanol, an extracting solution is extracted by ethyl acetate more than three times after being concentrated, and the ethyl acetate is recovered to obtain a total cucurbitacin extract; secondly, the total cucurbitacin extract is taken to be dissolved in a 25 to 45 percent of ethanol water solution, and the hydrolysis reaction is carried out in the presence of acetic acid; the pH value is adjusted to be neutral after full reaction, and the extract is concentrated to dry; and then the obtained extract is treated by purification so as to obtain a cucurbitacin B product with more than 60 percent of cucurbitacin B content, and the concentration of the acetic acid is 0.1 to 0.3 mol/L. Compared with the prior art for extracting and separating cucurbitacin B, the invention has the following advantages: the analogue (such as cucurbitacin B glucoside) of the cucurbitacin B is converted into the cucurbitacin B by the structural transformation in the process of extraction, so that the extraction rate of the cucurbitacin B is improved, the production process is simple, and the operation is simple.

The invention belongs to the technical field of medicine and discloses novel application of Cucurbitacins, namely novel application of Cucurbitacin B, Cucurbitacin B substances, Cucurbitacin BE and a pharmaceutical composition thereof in a medicine for treating ovarian cancer and improving the quantity of leukocytes of radiotherapy patients. The Cucurbitacin can also be a cucurbitacin B monomer, an isocucurbitacin B monomer, a dihydrocucurbitacin B monomer, a cucurbitacin I monomer, and a cucurbitacin O monomer. The Cucurbitacins or pharmaceutical compositions thereof can be matched with a pharmaceutically acceptable carrier and prepared into a tablet, a capsule, a granule, powder, a plaster, an ointment, an aerosol, a suspension, a syrup, an oral liquid, and an injection, and can also beprepared into special dosage forms such as a liposome, microspheres, nanoparticles and an emulsion for cavity administration, external use, oral administration and injection. The individual administration or the combined treatment can be performed, the administration dosage of the Cucurbitacins is calculated according to the total Cucurbitacins, the dosage for healthy adults is between 0.1 and 5mg/d, the best dosage is between 0.3 and 3mg/d, and the administration is performed for 1 to 4 times.

The invention relates to novel application of cucurbitacin B. Particularly, studies find that the cucurbitacin B can upregulate expression of an LATS1 gene and inhibit expression of a YAP gene and downstream related genes thereof in a colon cancer cell line. Moreover, the cucurbitacin B has the effect of inhibiting proliferation, invasion and metastasis of a human colon cancer SW620 cell line andan HT29 cell line, and can promote apoptosis thereof. The invention finds that the cucurbitacin B can be used as an activator for regulating a Hippo-YAP signaling pathway, is a novel promising effective anticancer medicine, can be used as an active component in preparation of medicines for treating cancers such as human colon cancer, and is conducive to improving the targeting ability of medicinalcancer treatment and reducing toxic and side effects of the medicines.

The present invention relates to a cucurbitacin B liposome drug and preparation thereof. The invention provides a cucurbitacin B nanometer liposome drug and a preparation method thereof. According to the present invention, a passive drug delivery way is used, and a substance polyethylene glycol containing polyhydroxy groups is linked to the phospholipid phosphoric acid group to modify so as to prepare the long-circulating nanometer liposome, wherein the structural modification effect is to protect the liposome from being identified and uptaken by opsonin in blood so as to reduce the liposome clearance rate and prolong the residence time in the blood, such that the action time of the drug is prolonged, the liposome can effectively reach the lesion, and the selectivity on the targeted tissue can be improved; the preparation prepared by the preparation method has characteristics of good physical stability, good chemical stability, long residence time in the body, small distribution volume in the body, and high blood drug concentration in the body; the drug of the present invention can be used for treatment of various types and various stages of liver cancers; and the cucurbitacin B liposome drug has characteristics of scientific formula, convenient use, good stability and low toxicity, and the preparation method is suitable for large-scale production.

The invention discloses an application of cucurbitacin B in preparation of a ferroptosis inducer and an anti-nasopharyngeal carcinoma drug. The research shows that cucurbitacin B can induce ferroptosis for the first time; death of nasopharyngeal carcinoma cells is regulated and controlled in a novel cell death promoting mode; and further research finds that cucurbitacin B can promote accumulationof iron ions, reduce the content of glutathione in the cells and down-regulate expression of GPX4 in nasopharyngeal carcinoma cells CNE1, so that lipid peroxide is increased, and iron death of the cells is induced. In in-vitro and in-vivo studies, cucurbitacin B induces the CNE1 cell cycle to be blocked in the G2/M period and inhibits cell migration and invasion. In addition, cucurbitacin B can significantly inhibit growth of mouse nasopharyngeal carcinoma tumors, and has no obvious toxic or side effect. The invention provides a new choice, namely a ferroptosis inducer, for a medicine for treating nasopharyngeal carcinoma; and meanwhile, a natural novel medicine source, namely cucurbitacin B, is provided for a ferroptosis inducer and treatment of nasopharyngeal carcinoma. The cucurbitacinB is efficient and safe and is free of toxic and side effects.

The invention discloses an extraction technology for cucurbitacin D. The extraction technology comprises the following steps that 1) muskmelon pedicels are fed into a pulverizer to be pulverized so asto obtain pulverized muskmelon pedicels; 2) ethanol reflux extraction is carried out two times on the pulverized muskmelon pedicles so as to obtain an extracting solution; 3) the extracting solutionis concentrated and separated so as to obtain an ethyl acetate layer; and 4), then the ethyl acetate layer is concentrated to be dry, then 10% of pyridine and ethanol are added, refluxing is carried out for 2.5-3.5 h, and separating is carried out so as to obtain the cucurbitacin D. According to the extraction technology, 10% of pyridine and ethanol are adopted as weak base, a large amount of cucurbitacin B in the muskmelon pedicels is converted into the cucurbitacin D, separation and extraction are carried out, so that the extraction rate of the cucurbitacin D is greatly increased, in addition, the technology is simple, and the cost is low.

The invention discloses cucumber exosome-like vesicles containing cucurbitacin B and capable of being used as anti-cancer drugs. Cucurbitacin B can be used for inhibiting proliferation of various cancer cells, but an extraction method of cucurbitacin B is complex and time-consuming. The method of separating the cucumber exosome-like vesicles to obtain cucurbitacin B has the advantages of easinessand quickness in operation and the like, and the lipid bilayer of the exosome-like vesicles is used as a natural protective film of cucurbitacin B, so that the stability of cucurbitacin B can be maintained for a long time. Moreover, through the principle of similarity and intermiscibility, the intake rate of cells to cucurbitacin B is also improved to a certain extent due to the existence of the lipid bilayer. When the cucumber exosome-like vesicles act on human alveolar basal epithelial cells (A549 cells) of adenocarcinoma, the maximum cell activity inhibition rate of the cucumber exosome-like vesicles is twice that of a cucurbitacin B standard substance, the dosage is lower, the toxicity to normal cells and the drug resistance to cancer cells can be reduced, and the cucumber exosome-likevesicles have good anti-cancer potential and industrialization prospect, and have an important significance in the clinical tumor treatment application.

The invention discloses a method of preparing a natural product cucurbitacin B. According to the method, a supercritical fluid extraction method is adopted to extract a total cucurbitacin extract product from plant, then a silica gel column separation and purification manner is adopted to obtain the cucurbitacin B, and the purity of the cucurbitacin B is higher than 90%. Compared with the prior art, the method for preparing the cucurbitacin B has advantages of short time, high efficiency, small solvent using amount, low environment pollution, and suitability for large-scale production and operation.

The invention belongs to the technical field of medicines, and relates to an exosome membrane-coated cucurbitacin B and oxidation-responsive antitumor prodrug co-loaded bionic nanoparticle, and an application thereof in the preparation of drugs for treating tumor metastasis diseases. The nanoparticle can ablate primary tumors and target circulating tumor cells so as to inhibit tumor metastasis. The exosome membrane-coated co-loaded bionic nanoparticle comprises 1-2 wt% of cucurbitacin B, 6-8 wt% of an oxidation-responsive antitumor prodrug, 60-70 wt% of a nano-carrier material, and the balanceof an exosome membrane, and the weight ratio of the cucurbitacin B to the oxidation-responsive antitumor prodrug is 1:4 to 1:8. The exosome membrane-coated cucurbitacin B and oxidation-responsive antitumor prodrug co-loaded bionic nanoparticle has an obvious effect of treating tumor metastasis, especially lung or liver metastasis of breast cancer, and can be used for preparing antitumor drugs.

Disclosed are methods for preparing a mixture of eight diasteromers of vittatalactone

Also disclosed are mixtures of eight diasteromers of vittatalactone produced by the methods described herein. In addition there are described compositions comprising a mixture of eight diasteromers of vittatalactone and optionally (2E,6Z)-nona-2,6-dienal

and optionally cucurbitacin B or cucurbitacin B, and optionally a carrier. Furthermore, there are describe methods of attracting Acalymma vittatum to an object or area, involving treating said object or area with a Acalymma vittatum attracting composition containing a Acalymma vittatum attracting effective amount of the compositions described herein.

The invention discloses a beta-glucosidase gene, a coding enzyme, an engineering bacterium and application thereof in preparation of cucurbitacin B by biotransformation of cucurbitacin B glucoside. The nucleotide sequence of the gene is shown as SEQ ID No. 1. The engineering bacterium containing the recombinant beta-glucosidase gene is subjected to induced expression culture, thalli are collected and subjected to ultrasonication, the obtained cell lysis solution is used as a catalyst, a muskmelon pedicel ethanol extract methanol solution is used as a substrate, a transformation reaction system is formed in a PBS buffer solution, and the cucurbitacin B is prepared through transformation. The beta-glucosidase gene and the engineering bacterium are derived from a streptomyces RW-2 strain, the cell lysis solution can be used as a biocatalyst, the cucurbitacin B glucoside is transformed into the cucurbitacin B, the concentration of the substrate of the reaction system is increased by 3.89 times, and the transformation rate of the cucurbitacin B glucoside into the cucurbitacin B reaches 90.2%.

The invention discloses a human dental pulp stem cell culture medium and a preparation method thereof. The culture medium is prepared from a basic culture medium and additives, wherein the basic culture medium is an alpha-MEM culture medium, and the additives are prepared from human AB serum with the volume percentage as 6 to 12%, 5 to 10mg/L of taurine, 0.1 to 0.2mg/L lipoic acid, 2 to 5mg/L of grape seed extract, 0.6 to 1.5g/L of carboxymethyl chitosan, 0.3 to 0.8mg/l of cucurbitacin B, 1 to 4mu g/L of platelet derived growth factor, 1 to 4mu g/L of epidermal growth factor, 0.6 to 1.8mg/L ofdiosgenin and 50 to 65mu M of choline chloride. The human dental pulp stem cell culture medium disclosed by the invention is prepared from specific ingredients, all the ingredients has an synergisticeffect, a dental pulp cell amplification speed can be remarkably improved, multidirectional differentiation capacity of the dental pulp stem cells is not affected, meanwhile human immune rejection isavoided, and reliable seed cells can be provided for clinical tooth repair and regeneration.