77 results about "Beta-elemene" patented technology

The invention discloses an essence with moss faint scent and applications thereof. The essence with moss faint scent comprises following ingredients: orcinol monomethyl ether, divarinol monomethyl ether, ethyl everninate, methyl divaricatinate, beta-orcinol carboxylic acid methyl ester, orcinol carboxylic acid ethyl ester, ethyl divaricatinate, pinocarveol, bata-elemene, propylene glycol, and the like. Inherent aroma compounds of natural plant essences with moss faint scent are applied in the preparation of the essence of the invention, and the essence with moss faint scent is prepared by such steps: dissolving the ingredients, and allowing the mixture to stand. Technologies are simple and are easy to operate; ingredients are easy to obtain; cost is low; operability is high; scent lasting time is long; scent quality is high; the moss faint scent is true to nature; the essence of the invention can be used as a substitute of natural moss faint scent essences so as to reduce the demand for natural essences, and possesses promising application prospect in the fields of daily use essences and cigarette essences.

This invention discloses beta-elemene nitrogen contained derivant. Nitrogen contain hetero atomic ring is brought in beta-elemene nitrogen structure to synthesize new structure beta-elemene nitrogen contained derivant. Its molecular structure formula is (I), R represents C1-C20 fatty amine group and aromatic amine group, C1-C20 contains hetero atomic ring amido group, cyclohexane backbone has three chirality centers. The derivent has some biological activities like alkaloid, it can increase polar at the same time, and make the synthesized derivent display certain alkalinity, so the goal of improve water-solubility by it with mineral acid or organic acid salt.

The invention provides a method for preparing high-purity beta elemene from natural plants containing the beta elemene such as curcuma zedoary (earthnuts or tubers of the curcuma zedoary), cedronella (fresh leaves of the cedronella), yellowtop (roots, stems, leaves, flowers and seeds of the yellowtop) and so on, which can improve the production efficiency from starting materials to the high-purity beta elemene and reduce production cost. Compared with the prior art, the method is mainly different in that the roots, stems, leaves, flowers and seeds of the natural plants are taken as raw materials; oleum volatile of specific parts of the natural plants is obtained by methods for extracting different oleum volatiles, and is distilled by molecular distillation method to remove compositions with high boiling points and non-volatile compositions; impurity compositions are removed by the ethanol extraction method and silver nitrate complex extraction method; and finally the beta elemene with the content between 95.0 and 99.9 percent is obtained through reduced pressure distillation or rectification. The bulk pharmaceutical chemicals not only can be prepared into oral dosing preparation such as emulsion oral liquid, self-emulsifying / self-microemulsifying capsules, soft capsules and so on, but also can be prepared into non-alimentary dosing preparation such as emulsion injection, liquid drugs injection, transdermal absorbent, lung sprays, suppository and so on. The method has the advantages of novel design, concise operating steps, mild operating conditions and improvement of the production efficiency of the beta elemene.

The invention discloses an A-elemene nitrogenous derivant, it providing the preparation and usage of A-elemene nitrogenous derivant, the structural formula is as picture shows, wherein R represent aliphatic amido of C1-C20, aromatic amido; amido of C1-C20 containing heterocycle; wherein cyclohexane skeleton has three chirality center. This derivant may has some physiologically active like alkaloid; meanwhile, it can increase polarity and making the synthesized derivant has certain alkalinity and it can reach the purpose of improving water-solubility salt-forming with inorganic acid or organic acid.

A beta-elemene pyrimidine derivative series is disclosd, which is prepared through reaction of beta-elemene on hypochlorite or NBS to obtain intermediate, and reacting on the pyrimidine's cyclic derivative in DMF or DMSO solvent.

The present invention discloses a kind of high-purity elemene medicine, which features the beta-elemene content as high as 98-99.9 wt%. One of its preparation process includes twice precise fractionation of elemene material containing beta-elemene of 80-92 wt% inside one heating reactor in precise fractionating tower with stainless steel cylinders as stuffing at vacuum degree of 200-500 Pa, flow rate ratio of 5 to 1 to collect the fraction at temperature of 82-83 deg.c. One other preparation process includes twice precise fractionation, and column chromatographic separation to eliminate impurity with the chromatographic column stuffed with silica gel after activation at 115-125 deg.c for 1.5 hr, and has even high beta-elemene content.

The invention provides beta-elemene polyamide derivatives containing phthalazinone having the structural features disclosed in the specification. The invention discloses a high-activity beta-elemene derivative with novel structures, thus can be used for preparing medicaments containing beta-elemene derivatives with better curative effects.

The invention provides a method for preparing high-purity beta elemene from natural plants containing the beta elemene such as curcuma zedoary (earthnuts or tubers of the curcuma zedoary), cedronella (fresh leaves of the cedronella), yellowtop (roots, stems, leaves, flowers and seeds of the yellowtop) and so on, which can improve the production efficiency from starting materials to the high-purity beta elemene and reduce the production cost. Compared with the prior art, the method is mainly different in that the roots, stems, leaves, flowers and seeds of the natural plants are taken as raw materials; oleum volatile of specific parts of the natural plants is obtained by methods for extracting different oleum volatiles, and is rectified by the rectification method to obtain the beta elemene with high content; impurity compositions are removed by the macroporous adsorption resin separation method or macroporous adsorption resin combined with the ethanol extraction method, and the silver nitrate complex extraction method in turn; and finally the beta elemene with the content between 95.0 and 99.9 percent is obtained through reduced pressure distillation or rectification. The bulk pharmaceutical chemicals not only can be prepared into oral dosing preparation such as emulsion oral liquid, self-emulsifying / self-microemulsifying capsules, soft capsules and so on, but also can be prepared into non-alimentary dosing preparation such as emulsion injection, liquid drugs injection, transdermal absorbent, lung sprays, suppository and so on. The method has the advantages of novel design, simple apparatus, concise operating steps, obvious shortened operating time, improvement of the production efficiency and high yield coefficient, and is suitable for industrialized production.

The invention provides a method for preparing high-purity beta-Elemene from natural plants containing beta-Elemene such as curcuma zedoary (root tubers or stem tubers of the curcuma zedoary), Cymbopogon citratus (fresh leaves of the Cymbopogon citrates), Solidago virgaurea (roots, stems, leaves, flowers and seeds of the Solidago virgaurea) and the like so as to improve production efficiency from the initial raw materials to the high-purity beta-Elemene and reduce production cost. Compared with the prior art, the method is mainly characterized in that: the roots, stems, leaves, flowers and seeds of the natural plants are taken as raw materials, and volatile oil of specific parts of the natural plants is prepared by methods for extracting different volatile oil, and then is rectified by a rectification method to prepare high-content beta-Elemene; then impurity components are removed by an ethanol extraction method and a silver nitrate complexing extraction method; finally the beta-Elemene with the content between 95.0 and 99.9 percent is prepared by distillation under reduced pressure; and the beta-Elemene not only can be prepared into oral administrative preparations such as emulsion oral liquid, capsules and the like, but also can be prepared into parenteral administrative preparations such as emulsion parenteral solution, injection, cutaneous permeable agents, lung spray preparations, suppositories and the like. The method has novel design of experimental methods, simple instruments and equipment, concise operation steps and obviously shortened operation time, improves production efficiency and is suitable for industrial production.

The invention provides a method for preparing high-purity beta-elemene from a low-content (over 1 percent) elemene raw material, which simplifies the steps of process operation, improves the production efficiency from an initial raw material to the high-purity beta-elemene, and reduces production cost. Compared with the prior art, the method comprises the following main different points: volatile oil constituents with large polarity is removed from the elemene raw material with the content over 1 percent under the action of silica gel column chromatography; then impurity constituents with small polarity is removed form a residual oil phase by a silver nitrate complexation extraction method and silver nitrate bonded silica gel column chromatography; and finally the beta-elemene with the content of between 95.0 and 99.9 percent is obtained through distillation under reduced pressure or rectification. The raw material medicament can be produced into oral administration preparations such as oral emulsions, capsules and the like, and can also be produced into non-intestinal administration preparations such as emulsion injections, water injections, cutaneous permeable agents, lung spray formulations, suppositories and the like. The experimental method has novel design and concise operating steps, obviously improves the yield, and reduces production cost.

The invention relates to a method for extracting and separating beta-elemene, a device thereof and a method for preparing a filling thereof. The method for extracting and separating the beta-elemene provided by the embodiment of the invention comprises the steps as follows: the raw material of the beta-elemene is added to the upper end of a chromatography column, wherein, the chromatography column is provided with silver nitrate surface modification filling; eluent is added into the chromatography column to elute the mixed raw material of the beta-elemene and the filling; solution after the elution is collected at times; and silver ion in the solution which is collected at times after the elution is removed. In addition, the embodiment of the invention also provides the device used for extracting and separating the beta-elemene and the method for preparing the silver nitrate surface modification filling which is used in the method for extracting and separating the beta-elemene.

The invention provides a method for preparing Beta-elemene with a high purity from a by-product of citronella oil so as to improve the production ratio of the high purity Beta-elemene obtained from the initial raw material and reduce the production cost. The invention is characterized in that the citronella oil by-product with the Beta-elemene contents of no more than 5 percent is taken as the raw material. Rectification is carried out by adopting the vacuum distillation method and the Beta-elemene with a high content is then obtained; the Beta-elemene with a content of 95.0 to 99.9 percent is obtained by the preparation method of high vacuum distillation. The invention has the advantages of wide resources of raw material, simple device and equipment and low cost. The invention reduces the times of the rectification and shortens the operation time, thus improving the production ratio and being applicable to the industrial production.

The invention relates to the field of organic synthesis and medicinal chemistry, and particularly relates to a beta-elemene 14-site ramification (I) or (II), wherein R1 and R2 are defined in the specification. The invention also discloses a preparation method of the beta-elemene 14-site ramification and application of the beta-elemene 14-site ramification on the aspect of resisting atherosclerosis. The ramifications I and II are as shown in the specification.

The invention discloses sesquiterpene synthase from eupatorium adenophorum spreng, a gene, a vector, an engineering bacterium and application of the sesquiterpene synthase. Amino acid sequences of the sesquiterpene synthase are shown as SEQ ID NO.2. The sesquiterpene synthase, the gene, the vector, the engineering bacterium and the application have the advantages that catalysts come from the eupatorium adenophorum spreng which is a high-yield medicinal plant for beta-elemene, as proved by in-vitro activity, substrates FPP (Farnesyl pyrophosphate) can be catalyzed by the catalysts to generate the beta-elemene, and the final yield of the beta-elemene can ultimately reach 7.499 micro-grams / mL.

The invention provides a beta-elemene synthetase, an encoding gene thereof, a carrier with the encoding gene, an engineering bacterium with the encoding gene and an application of the beta-elemene synthetase. The beta-elemene synthetase has an amino acid sequence as shown in SEQ ID No.1, and the encoding gene of the beta-elemene synthetase has a sequence as shown in SEQ ID No.2. The invention provides the beta-elemene synthetase and the encoding gene thereof and provides the basis for producing the beta-elemene synthetase by using a biological enzyme method; the quality of a beta-elemene synthetase product can be improved, the production cost of the beta-elemene synthetase can be reduced, the production efficiency can be increased, and the technical precondition is provided for the industrial biosynthesis of the beta-elemene synthetase.

The invention belongs to the technical field of the preparation of beta-elemene derivatives, and specifically discloses a nitric oxide donor type beta-elemene derivative and a preparation method and application thereof. The beta-elemene derivative and pharmaceutical salts thereof have a general formula M, wherein X is O or radical simultaneously containing ester group and amido; R1 represents C1-10 alkyl, C6-12 cycloalkyl, C6-12 aryl, C2-10 alkenyl, C2-10 alkynyl or C2-10 ether group, each not containing or optionally containing one to three substituents; R2 represents C1-10 alkyl, C6-12 cycloalkyl, C6-12 aryl, C2-10 alkenyl, C2-10 alkynyl or C4-22 ether group, each not containing or optionally containing one to three substituents. The nitric oxide donor type beta-elemene derivative and the pharmaceutical salts thereof can be used for preparing anti-tumor drugs.

The invention discloses a detection method for a sesquiterpene component in radix curcumae. The method comprises the following steps: volatilizing and drying a solvent of a radix curcumae extracting solution and carrying out buffering solution re-dissolution by utilizing electrophoresis; filtering the solution with a 0.22mu m filter membrane and taking filtrate as a sample to be detected; detecting peak area of each effective component in the sample to be detected by adopting a micro-emulsion electrokinetic capillary chromatography; obtaining the content of curdione, curcumol, germacrone, furanodiene and beta-elemene in the sample to be detected of the radix curcumae respectively according to each reference substance standard curve of the curdione, the curcumol, the germacrone, the furanodiene and the beta-elemene. The invention innovatively provides a micro-extraction detection method of volatile oil type components in traditional Chinese medicines. According to the method disclosed by the invention, a matrix solid-phase dispersion and extraction technology taking a molecular sieve as an adsorbent is combined with a micro-emulsion electrokinetic capillary chromatography technology, so that the content of the volatile oil type effective components in the medicinal material radix curcumae can be efficiently and environmentally friendly extracted and detected.

The invention discloses Beta-elemene amino acid derivatives as shown in the formula I and the salt accepted pharmaceutically, the synthesis method of the Beta-elemene amino acid derivatives and the usage in preparing anticancer drugs; wherein, in the formula I, R[1], R[2] are independently H or amino acid with one hydrogen atom substituted on amino; the condition is H when R[1] and R[2] are different. The synthesis method of the Beta-elemene amino acid derivatives in the formula I and the salt accepted pharmaceutically has the advantages of having good water soluble and biocompatibility and higher anticancer activity compared with Beta-elemene and an important reaction intermediate. The synthesis method can be used as synthesizing other Beta-elemene derivatives.

The invention discloses a comprehensive extraction method of Curcuma wenyujin active ingredients. The method comprises the following steps of: 1) total extraction of Curcuma wenyujin; 2) concentration of total extract; 3) extraction of beta-elemene in total extract; 4) extraction of curcumenol in total extract; 5) extraction of curcumin in total extract; 6) preparation of Curcuma wenyujin polysaccharide; 7) refining of curcumenol; 8) refining of beta-elemene. According to the invention,the active ingredients are extracted simultaneously by the comprehensive extraction method, and then, the extract is further separated and purified, the comprehensive extraction method has the advantages of high extraction rate, advanced and special technology, high daily capacity, high yield and low cost, and is suitable for industrialized production.

The present invention provides convergent processes for preparing beta-elemene, and analogues thereof. Also provided are analogues related to beta-elemene and intermediates useful for preparing the same. The present invention further provides novel compositions based on analogues of beta-elemene and methods for the treatment of cancer, such as brain tumor, lung cancer, colorectal cancer, gastric intestional cancer, and stomach cancer.

The invention relates to the field of new medicine research and development and tumor therapy, in particular to a novel beta-elemene derivative containing a dihydropyridine structure, particularly a derivative directly or indirectly introducing the brain-targeted dihydropyridine structure through a connecting arm in a beta-elemene 13 bit. The invention also discloses a preparation method of the beta-elemene derivative with the brain-targeted function, and a purpose of the novel derivative for treating gliomas.

The invention beta-elemene diamine derivatives represented by formula I, and pharmaceutically acceptable salts thereof, wherein, R1 and R2 are H or -NH(CH2CH2O)n(CH2CH2)mNH-Boc independently, but are not H at the same time; Boc is t-butoxycarbonyl; m is an integer of 1-3; n is an integer of 0-112. The also discloses a synthesis method of beta-elemene diamine derivatives, comprising: dissolving beta-elemene chlorine substitutes and NH2(Ch2CH2O)n(CH2CH2)mNHBoc in solvent, and adding alkali catalysts to perform reaction. The invention further dicloses application of beta-elemene diamine derivatives in preparing anticancer drugs, and as reaction intermediates in preparing other beta-elemene derivatives. The beta-elemene monosubstituted amine derivatives of the invention have good water-solubility and higher anticancer activity than that of beta-elemene.

The invention belongs to the field of plant extraction, and aims to provide a method for extracting and separating beta-elemene from a noxious weed plant Lantana camara. The method provided by the invention comprises the following steps: A. raw material preparation: carrying out pulping, or drying and pulverizing on fresh stems and leaves of Lantana camara as a raw material; B. volatile oil extraction: acquiring volatile oil from the raw material acquired in the step A; C. column chromatography: carrying out column chromatography on the volatile oil acquired in the step B, collecting an eluate, and removing solvent in the eluate to acquire a crude beta-elemene product; and D. refinement: refining the volatile oil acquired in the step B or the crude product acquired in the step C by a molecular distillation or preparation-type high efficiency liquid chromatography system to acquire the high-purity beta-elemene. The invention has the advantages of high product purity, high yield and low cost, and provides a brand-new, cheap and effective way for the development and treatment of Lantana camara and the acquisition of beta-elemene.

The invention relates to the field of natural medicines, and particularly relates to use of beta-elemene and derivatives thereof in preventing atherosclerosis, and in particular relates to an application in preparation of medicines for treating atherosclerosis. Test results show that beta-elemene and derivatives can remarkably reduce the atherosclerotic plaque area in the coronary artery of an animal model, and meanwhile has remarkable improving effect on two key links in development process of atherosclerosis: adhesion of leukocyte and endothelial cells and peroxidation of lipids. Expression of adherence factors closely related to atherosclerosis can be reduced, so that peroxidation damage of endothelial cells in vitro and in vivo caused by high fat and H2O2 is avoided.

The invention relates to an isopropanolamine substituted beta-elemene derivative and a preparation method and an application of the isopropanolamine substituted beta-elemene derivative. Particularly, the invention relates the novel isopropanolamine substituted beta-elemene derivative shown in the general formula (I) or (II), the preparation method of the isopropanolamine substituted beta-elemene derivative, and the application of the isopropanolamine substituted beta-elemene derivative to preparation of antitumor drugs.

The present invention discloses monosubstituted beta-elemene ether derivative as shown and its pharmaceutically acceptable salt. The present invention also discloses the synthesis process and application in preparing anticancer medicine of the monosubstituted beta-elemene ether derivative. The monosubstituted beta-elemene ether derivative of the present invention has high water solubility, high anticancer activity, no toxicity, high medicine effect and high bioavailability.

The invention belongs to the technical field of medicines and provides a pharmaceutical composition. The pharmaceutical composition comprises germacrone, furanodiene, curdione, beta-elemene, curcumol, curzerene and borneol. The components of the pharmaceutical composition are definite, and the quality can be controlled. The pharmaceutical composition can be used for preparing vaginal or rectal preparations and has a good effect of treating HR-HPV (high risk human papillomavirus) and / or LR-HPV (low risk human papillomavirus) infection and cervical diseases and can be used widely clinically.

The invention discloses an extraction and enrichment method for a sesquiterpene component in curcuma wenyujin. The sesquiterpene component is a mixture of Germacrone, Furanodiene and beta-elemene. Themethod comprises the following steps of: 1) extraction: mixing curcuma wenyujin powder and ionic liquid water solution, carrying out microwave extraction to obtain suspension, carrying out centrifugation to obtain supernatant, and carrying out filtration to obtain filtrate, so as to obtain curcuma wenyujin extracting solution; and 2) enrichment: mixing lauryl sodium sulfate, a fluorinated carbonnanotube and water, carrying out ultrasonic treatment to obtain dispersion liquid, adding the dispersion liquid into the curcuma wenyujin extracting solution, carrying out vortex and filtration aftermixing, diluting the obtained solid, and collecting the dilution liquid to obtain enrichment solution. The method is simple and low in solvent dosage, is capable of effectively avoiding the using of toxic and harmful reagents, is green and environment-friendly, is capable of avoiding the loss of the low-boiling point sesquiterpene component due to high-temperature extraction, and is suitable for large-scale popularization and application.

The invention provides (1S, 2S, 4S)-beta-elemene. The (1S, 2S, 4S)-beta-elemene is characterized in that a novel beta-elemene stereisomer is successfully separated from a crude product containing beta-elemene; the novel beta-elemene stereisomer is subjected to physicochemical property analysis and structural identification and is identified as beta-elemene stereisomer 1R-methyl-1-vinyl-2R, R4-diisopropyl cyclohexane, and the specific structure is identified as (1S, 2S, 4S)-beta-elemene. The compound has the same planar structure as beta-elemene. The pharmacological toxicological activity testshows that the side effect of the beta-elemene stereisomer 1R-methyl-1-vinyl-2R, R4-diisopropyl cyclohexane is less than that of the beta-elemene, and the antitumor activity of the beta-elemene stereisomer 1R-methyl-1-vinyl-2R, R4-diisopropyl cyclohexane is beyond that of the beta-elemene. Therefore, a new research direction is supplied to research antitumor drugs, and meanwhile, the configurational isomer of the beta-elemene is enriched.

The invention discloses beta-elemene monosubstituted amine derivatives represented by formula I, and pharmaceutically acceptable salts thereof, wherein, R1 is H, R2 is n-butyl, tert-butyl, cyclohexyl, cyclopentyl, cyclooctyl, isopropyl, p-carboxylphenyl, p-carboxy phenoxyphenylmethyl or phenylmethyl; or both R1 and R2 are ethyl or -CH2COOH; or R1NR2 is imidazole. The invention also discloses a synthesis method of beta-elemene monosubstituted amine derivatives, comprising: dissolving beta-elemene chlorine substitutes and amine in solvent, and adding alkali catalysts to perform reaction. The invention further dicloses application of beta-elemene monosubstituted amine derivatives as reaction intermediates in synthesizing other beta-elemene derivatives, and in preparing anticancer drugs. Compared with beta-elemene, the beta-elemene monosubstituted amine derivatives of the invention have better water-solubility and higher anticancer activity.