100 results about "Alkannin" patented technology

The invention relates to an action of ferulic acid on enhancing the drug effect of some medicaments and a purpose thereof, wherein the medicaments mainly comprise alkaloid medicaments including matrine, kushenin, sophocarpine, hyoscyamine, narceine, hanfangchin A, jamaicin, morphine, codeine, evodiamine, strychnine, catharanthine, vincristine, taxol, verticine, peimine, peiminine, ephedrine, pseudoephedrine, wilfordine, triptolide, tripdiolide and the like, and flavonoid medicaments including puerarin, ginsenoside, ginsengenin, mangiferin, scutelloside, alkannin, meletin, rutin, hesperidin, daidzin, soybean isoflavone, daidzein, carthamin, catechin and the like. The ferulic acid and the medicaments can form a compound or a medicament compound, or the ferulic acid and the medicaments can generate a chemical reaction (including salification, esterification, amidation, ketonization, etherification and the like), and / or the ferulic acid and the medicaments can generate a synergistic effect and an additive effect.

The invention relates to application of alkannin serving as a dye, which comprises the following steps of: (1) extracting the alkannin from lithospermum; and (2) printing and dyeing the alkannin on atextile for dyeing. Compared with the prior art, the application uses the alkannin extracted from natural lithospermum as the dye to print and dye the textile, has an environmentally-friendly extraction process, and prevents the wide use of organic solvents with large hazard; and the extracted alkannin is natural and nontoxic, has mild performance, has the effects of clearing heat and releasing toxin, is environmentally-friendly and natural, is favorable for health, and can be taken as a purple dye to be widely applied in the garment sector.

The invention discloses a preparation method of high optical purity shikonin and alkannin, and derivatives thereof. According to the invention, an intermediate separation means is used to prepare the high optical purity shikonin and alkannin, and the derivatives thereof, wherein the intermediate separation is that an amide diastereomer is formed from a carboxyl-contained intermediate and chiral amine, and separation is carried out through column chromatography or a recrystallization process. The derivatives of shikonin and alkannin are tetramethoxylated derivatives with shikonin and alkannin as mother nuclei, dimethoxylated-2-sidechainisomer derivatives and dimethoxylated-6-sidechainisomer derivatives with shikonin and alkannin as mother nuclei, 1,4-diacetoxylated-5,8-dimethoxylated-2-sidechainisomer derivatives and 1,4-diacetoxylated-5,8-dimethoxylated-6-sidechainisomer derivatives with shikonin and alkannin as mother nuclei, and diacetoxylated-6-sidechainisomer derivatives and diacetoxylated-2-sidechainisomer derivatives with shikonin and alkannin as mother nuclei. The preparation method of the invention, which has the advantages of easily available raw material, low price and high yield of each step reaction, is suitable for the large scale preparation.

The invention relates to an extraction method of alkannin. In the extraction method, after extracting lithospermum with organic menstruum, aqueous alkali is used for processing. The method is characterized in that after the lithospermum is fully extracted with nonpolar organic menstruum in a backflow mode, aqueous alkali containing sodium hydroxide or potassium hydroxide with the concentration of 0.6-5.5M is used for fully leaching an organic solution after the fully extracting, then the pH value of aqueous alkali extraction solution is acidized to be smaller than or equal to 2, then the lithospermum is fully precipitated and collected. By using the extraction method in the invention, the lithospermum with high purity and yield can be obtained and can be applied to the commercial process.

The invention relates to a method for producing alkannin by utilizing Arnebia euchroma(Royle)Johnst hairy root. The method includes selection and processing of Arnebia euchroma(Royle)Johnst explant, activation culture of agrobacterium rhizogene, infection of cotyledon explant and induction of hairy root, obtaining of sterile Arnebia euchroma(Royle)Johnst hairy root system and liquid culture of Arnebia euchroma(Royle)Johnst hairy root as well as alkannin production. The used hairy root has the characteristic of rapid and autonomous growth on culture medium without exogenous hormones, thus the method not only can overcome the defects that cell culture grows slowly and hormone is required to be additionally added to maintain the growth thereof when utilizing cell culture to produce alkannin, and the method has the advantages of stable alkannin throughput, simple operation in cultivation, lower cost and no restriction of climate and land natural conditions. Especially the invention provides a stable and continuable novel medicine source for producing alkannin by utilizing hairy root culture method and provides reliable source and material basis for alkannin mass production by applying bioreactor in the future.

The invention relates to an oxygen alkylated derivative of a parent nucleus of alkannin naphthazarin and a preparation method and application thereof. The structural formula of the oxygen alkylated derivative of the parent nucleus of alkannin naphthazarin is particularly shown as in the following formula, wherein R is H, alkane with 1-10 carbon atom(s), olefin, acrne or COR', R' is H, alkane with 1-10 carbon atom(s), olefin or acrne. The invention also relates to the application of the oxygen alkylated derivative of the parent nucleus of alkannin naphthazarin in preparation of anticancer drugs. The preparation method of the invention has the advantages of easily accessible raw materials, short synthetic route and high reaction yield, and the prepared compound can be used as a prodrug for treatment of malignant tumors.

An alkannin derivative as immuno-suppressive agent and its metallic complex compound with a chemical constitution formulas III and IV disclosed in the specification, wherein in formula III, R is C1-6 saturated, unsaturated and aromatic acyl, in formula IV, R is hydrogen, C1-6 saturated, unsaturated and aromatic acyl, M is metallic Cu, Ca, Zn. The present invention realizes immunological suppression effect, thus can be used for treating diseases relating to human body autoimmune including chronic infectious arthritis, scleredema, lupus erythematosus, HIV infection and malignant tumor.

The present invention relates to a total synthesis method for preparing racemate alkannin. Said invention uses naphthaldehyde protected by protecting group as raw material and adopts the following steps: heating said raw material and metal oxide of 1-halogeno-3-methyl-2-butylene and making then produce reaction in aprotic polar solvent, zone-selectively making alpha-addition reaction, and introducing side chain of alkannni to obtain 2-(1-hydroxy-4-methyl-3-pentenyl)-1,4,5,8-tetramethoxy- aphthalene or 2-(1-hydroxy-4-methyl-3-pentenyl)-1,8:4,5-bis( methylene-dioxy) naphthalene, then making oxidation to remove protecting group so as to obtain racemic alkannin.

The invention provides application of naphthoquinones compound in preparing multidrug resistant tumor drug. The naphthoquinones compound is extracted or synthesized from gromwell plant by the prior art; the effective components of the naphthoquinones compound comprise iso-alkannin which is antimer of the gromwell and derivatives thereof. The naphthoquinones compound can take effect on the multidrug resistant tumor cells without being influenced by such tumor drug-resistant proteins as P-gp, MRP1 and BCRP, etc. and high expressions of anti-apoptotic proteins of Bc1-2 and Bc1-XL; the compound has lethal effects on the multidrug resistant tumor cells obviously superior to the presently common used and typical tumor resistant drugs; the lethal effects of the naphthoquinones compound on the multidrug resistant tumor cells is consistent with the parent drug-sensitive cells; the naphthoquinones compound is low toxic and has promising clinical application prospect therefore.

The present invention is a synthesis method of the shikonin dimethyl ester derivative in the pharmaceutical and chemical technological field. The synthesis method of the second-level side-chain isomer and the sixth-level side-chain isomer of the shikonin dimethyl ester of the present invention uses the shikonin as the raw material; the shikonin is first cyclized; then the cyclized shikomin is in the tetramethyl and ring-opening reaction; in the process, the absolute configuration of the shikonin is maintained; then the esterification or etherification is done; at last, the methyls are selectively doffed to get the target compound. The reagent in each step of the reaction is easy to get; the conditions are mild; the collection rates of the reaction all surpass 65 percent; the total collection rate is 33.2 percent (calculated by the shikonin). The reaction process has no racemic reaction.

The invention discloses alkannin acetyl glucose and a preparation method and an application thereof. The method comprises the following steps: adding 1 mol of 1- trichloroacetamido-acetyl glucose and 1-2 mol of alkannin into dichloromethane solution, and reacting at the temperature of minus 20-minus 40 DEG C under the existence of 4angstrom of molecular sieve and boron trifluoride diethyl etherate, thus obtaining alkannin acetyl glucose. The alkannin acetyl glucose is used for the medicines with tumor activity resistance and drug resistance. In the invention, the alkannin acetyl glucose is prepared simply and effectively by four steps of reaction, the tumor activity resistance and drug resistance of the alkannin acetyl glucose are inspected, therefore, the alkannin acetyl glucose which has strong inhibiting action to the tumor cell lines is showed, and the good drug resistance of the alkannin acetyl glucose are also proved, and the alkannin acetyl glucose is a prospecting medicine for resisting tumor.

The extracting process of alkannin includes the following steps: extracting alkannin from gromwell by using liquid CO2 with 20-32 MPa pressure as entrainer; and sepg alkannin from liquid CO2 in the conditions of 15-20 MPa pressure and 30-40 deg.c temperature. The extracting process at special pressure and temperature is simple and has extracting yield as high as 1.6%. The product has high purity and no any residue.

The invention discloses a microemulsion composition containing alkannin, which comprises alkannin or alkannin ramification, emulsifier, assistant emulsifier, oil and water. The composition can greatly improve the solubility of the alkannin.

The invention relates to an antineoplastic derivative of the medical technology field, which contains sulfur alkannin and naphthaquinone, i. e., 6-substituted 5, 8-dimethoxy-1, 4-naphthaquinone derivative and 2-substituted 5, 8-dimethoxy-1, 4-naphthaquinone derivative having a structure formula, wherein, R1 is 3-methyl-2-butenyl, methyl, n-propyl, n-pentyl; R2 is alkanoylindoles, aroyl and alkyl. The formula I is 6-substituted 5, 8-dimethoxy-1, 4-naphthaquinone and the formula II is 2-substituted 5, 8-dimethoxy-1, 4-naphthaquinone.

The invention provides a process for preparing alkannin or isoalkannin which consists of, subjecting the alkannin or isoalkannin ester derivative to lithium hydroxide hydrolysis. Compared with the conventional hydrolytic method by sodium-hydroxide, the present invention has the advantages of high yield, less by-product and easy after-treatment, thus can be applied into mass production.

The invention discloses a composition containing alkannin and lemon grass essential oil. The composition comprises an active ingredient which comprises alkannin and lemon grass essential oil. In the composition disclosed by the invention, the alkannin and the lemon grass essential oil are natural ingredients and have obvious effects of increasing efficiency, resisting bacteria and diminishing inflammation. The composition is used for treating diseases of dermatitis and eczema and various skin injuries, does not contain unknown and known toxic components undefined in medicine effect, and is definite in curative effect, controllable in quality and safe in use.

The invention discloses a method for extracting an alkannin naphthoquinone pigment extract and series products thereof by combining subcritical 1,1,1,2-tetrafluoroethane (R134a) extraction and molecular distillation technology. The method has the characteristics of high extraction rate, low extraction temperature, short production cycle, high product quality, low production cost and the like; andthe prepared alkannin naphthoquinone pigment extract and the refined alkannin naphthoquinone derivative series products can be used for pharmaceutical industry, food industry, cosmetics industry, printing and dyeing coloring agents and the like.

The invention provides an application of alkannin derivant for preparing drug treating cancers, and the drug takes orphan receptor Nur77 as an effect target. The invention also provides the application of the orphan receptor Nur77 which serves as an effect target to screen alkannin derivant. The alkannin derivant of the invention clarifies the mechanism of the anti-tumour effect of alkannin derivant via a great discovery that tumour cells are induced to apoptosis by acting on the orphan receptor Nur77, and provides effective target spots for decorating and optimizing the structure.

The invention provides personal care essence oil containing alkannin. The personal care essence oil contains alkannin and an extracting solvent, wherein the extracting solvent is synthetized oil. The personal care essence oil has better light and heat stability and is lighter and thinner in skin feeling. The problem that existing lithospermum oil is unstable and easily rancidifies is also solved while the used extracting solvent ensures that the alkannin is effectively extracted. In addition, the sterilization temperature can be properly improved, the risk of microbe breeding can be reduced and the product quality can be comprehensively improved by adopting a preparation process. The invention further provides a preparation method and application of the personal care essence oil containing the alkannin and a cosmetic compound containing the personal care essence oil containing the alkannin.

The invention discloses an acid-base indicator and a preparation method thereof. The acid-base indicator is a solution containing alkannin and curcumin, wherein the mass ratio of alkannin to curcumin is 80 to (45-100). The preparation method of the acid-base indicator comprises the following steps: dispersing alkannin and curcumin into an organic solvent; and dissolving and filtering impurities to obtain the acid-base indicator. Alkannin and curcumin display different colors in an acid-base solution; alkannin and curcumin are mixed in the solution in a certain ratio, so that an indication range of the acid-base indicator is expanded, a mutational range is narrow and the acid-base indicator is sensitive to pH change indication; and meanwhile, the change of the colors is obvious so that the intensity of acid-base properties of the solution can be easily identified.

The invention discloses naphthoquinone compound alkannin, which can be used for quantitatively testing the enzyme activity of glucuronic acid transferase UGT1A9 and UGT1A8 as UGT1A9 and UGT1A8 specific probe substrate. The use is implemented by the following step of: selecting alkannin as a specific probe substrate, carrying out the UGT catalytic reaction of a specific substrate by using a UGT in-vitro incubation system, quantitatively testing the enzyme activity of UGT1A9 and UGT1A8 in biological samples and cells by quantitatively testing the lost amount of the substrate or the generated amount of the product. The substrate can be used for quantitative evaluation of the enzyme activity of UGT1A9 / 1A8 in different species, individuals and biological samples, calibration of propofol anesthetic metabolizing capacity of certain tissues, and calibration and estimation of the elimination rate of compounds which are mainly metabolized by UGT1A9 in specific organisms based on in-vitro metabolism dynamic data.

The invention provides an Arnebia euchroma mauve cell line for stable and high yield of alkannin, wherein, the content of alkannin compounds can reach 6 to 8 percent of the dry weight of culture and is 5 to 9 times of that of wild and natural Arnebia euchroma. The invention also provides a culture technique for the cell line and a method for mass and quick production of the culture of the cell line. The method breaks the routine lithospermum cell two-step culture method, adopts one-step culture method to cultivate the lithospermum cell culture and then realizes production of Arnebia euchroma cells through the method of combination of cell suspension culture and culture of solid culture medium and quick production of effective compositions. The method adopts combination of liquid culture and solid culture, produces seeds through liquid culture, obtains the culture through solid culture and selects and uses reserved seeds with good comprehensive properties for liquid culture, and the steps are repeated. Moreover, the production of the Arnebia euchroma cells by adoption of the method does not occupy arable lands and destroy wild resources of Arnebia euchroma, thereby the environment is protected and the problem of shortage of Arnebia euchroma resources is solved.

The invention discloses CYP76B74 protein participating in biological synthesis of alkannin as well as an encoding gene and application thereof. An amino acid sequence of the CYP76B74 protein is shownas a sequence 1 in a sequence table. An experiment proves that the CYP76B74 protein is closely related to the synthesis of alkannin type compounds and can be used for catalyzing hydroquinone2-geranylquinone into 3''-hydroxyl-hydroquinone2-geranylquinone. The CYP76B74 protein disclosed by the invention has important theoretical and practical significance of adjusting and producing plant naphthoquinones compounds and improving the content of a naphthoquinones active component, i.e., alkannins, in arnebiae through a biological technology.

The invention discloses lithospermum ketoxime derivant which can be used for resisting tumour in the technology field of medicine. The lithospermum ketoxime derivant is 5, 8-dimethoxy-1, 4-naphthoquinone derivant which is replaced by 6-, and has the following structural formula, wherein, R is alkyl and aralkyl. The lithospermum ketoxime derivant is synthesized, and the antitumor activity thereof is measured; alkannin is structurally modified and reorganized, so that an antitumor compound with lowered toxicity and increased water-solubility is obtained.

The invention belongs to the technical field of chemical drug intermediate extraction, and discloses a method for extracting cannabidiol by purple sulfur bacteria fermentation. The method comprises the following steps: by using one or more of flowers, leaves and hemp bran of industrial hemp as raw materials, drying and pulverizing to obtain a hemp raw material of which the water content does not exceed 5%; adding water and a cultured purple sulfur bacterium fermentation liquor into a transparent organic glass tank filled with the crushed hemp raw material, and irradiating, sealing and standingfor 24-30 hours to obtain a hemp fermentation liquor; filtering the fermentation liquor to remove residues; performing low-temperature reduced-pressure concentration to obtain a primary extract containing cannabidiol; and removing impurities by using macroporous resin, and purifying by using silica gel column chromatography to obtain cannabidiol with the purity of more than 80%. The method is simple to operate and low in cost, and has good popularization and application values. The invention also discloses application of cannabidiol as a main component, and alkannin, essential oil and other components are added or not added, so that the traditional Chinese medicine composition has the effects of treating infantile red buttocks, eczema, urination rash, saliva rash and the like.

The invention relates to an application of alkannin and its derivative in the preparation of a gene therapy sensitizer. The alkannin and its derivative as a gene therapy sensitizer has small toxicity; and when the alkannin and its derivative and gene therapy are combined to carry out malignant tumor treatment, the superposing of the anticancer effect of the alkannin and its derivative and the enhanced gene therapy effect maximally display an antitumor effect.

The invention discloses a preparation method of a traditional Chinese medicine composition, belonging to the field of traditional Chinese medicines. The preparation method comprises the following steps of: mixing 100-900 parts of remote lemongrass herbs, 100-900 parts of lithospermum and 100-900 parts of wormwood; adding distilled water for the first time according to the mass ratio of 1:8, decocting for 2.5 h, and collecting the decoction liquid; adding distilled water according to the ratio of 1:6, decocting the raw materials for the second time for 2 h, and collecting the decoction liquid; and merging the two decoction liquids, filtering, collecting the extraction liquid and concentrating to obtain the traditional Chinese medicine composition. The preparation method increases the transfer rates of medicinal active ingredients of rutin, psoralen, beta, beta'-dimethylacryl alkannin and eucalyptol in remote lemongrass herbs, lithospermum and wormwood to be above 95% which is obviously higher than the transfer rates of effective ingredients of the traditional method. The preparation method improves medicinal effect and reduces cost.

The invention discloses a preparation method of a botanical mice composite sterilant Nongda-1, which belongs to the technical field of medicine compound. By researching reasonable ratio and synergism of the medicinal materials, the medicines prepared by the pharmaceutical composition of the invention have good effect for controlling mice fertility, alkannin extracted from roots of Macrotomia euchroma is combined with quinsetrol, an unique technology is employed, so that the botanical mice composite sterilant can be prepared, and the botanical mice composite sterilant has good effect for controlling mice fertility.

The invention relates to a method for increasing the alkannin content of the cultured cells of onosma paniculatum. The operating steps of the method mainly comprise: 1. the subculture of onosma paniculatum cells; 2. the process of liquid culture and ultra sonication of the onosma paniculatum cells; and 3. the process of measuring alkannin content. Utilizing ultrasonic to stimulate the suspension cultured onosma paniculatum cells is an effective means to increase the alkannin content of cells. The method is characterized by simple and easy operation, good effect and strong expansibility and can be applied to a large-scale bioreactor for plant cells to improve the content of the effective secondary metabolites.