37 results about "Acetogenin" patented technology

The present invention relates to a plant extract with the action of resisting diabetes, its application and preparation method. The extract is a kind of acetogenins extracted from branck, leaf, trunk, bark, root, seed and fruit skin of annona squamosa plant as raw material. The compound acetogenins can be made into various dosage forms for curing diabetes, and its preparation method can adopt oneor several processes of solvent extraction process, resin adsorption process, supercritical CO2 extraction process and conventional drying process.

The present invention relates to a process for obtaining a triglyceride-rich refined avocado oil. The invention also relates to the triglyceride-rich refined avocado oil which can be obtained by means of this process. Advantageously, the refined avocado oil according to the invention contains a sterol-enriched unsaponifiable fraction. Advantageously, the refined avocado oil according to the invention is substantially free of acetogenins and furanic lipids. The invention also relates to compositions containing such an oil. The invention also relates to such compositions for their use as a medicament, as a dermatological agent, as a cosmetic agent or as a nutraceutical agent, to be used humans or animals.

The invention provides compositions and formulations comprising catechol and / or acetogenins and various combinations thereof; including various combinations with other ingredients including botanical preparations containing acetogenin, an extract of green tea or a therapeutically active flavanoid contained in green tea; and one or more quinones. The invention includes a pharmaceutical composition including a salt of rhodizonic acid, an OH anion-generating base, a non-toxic acid, a quinone, a salt-containing sulfite, catechol and optionally, an acetogenin and an extract of green tea. The compositions and formulations demonstrate positive effects against a broad variety of cancer, autoimmune diseases, viruses and provides antioxidant protection against peroxyl hydrophilic, peroxyl lipophilic, hydroxyl, peroxynitrite and super oxide radicals. The compositions and formulations can be used for nutritional and nutraceutical uses, and used as dietary supplements.

The invention relates to the chemical compound of the chiral annonaceous acetogenins of the comformational restriction structure, the synthetic method and the purpose. The compound has the optical activity compound as the above formula: (R or S configuration) (R or S configuration). The compound of the invention has high anti-cancer activity and selectivity and has the IC50 (MuM) of the human breast duct cancer reaching less than 0.04, and the suppressive activity on the cancer cell is about 100 times that of the normal cell and has better selectivity. The compound of the invention can also be used as the anti-cancer drug and has simple preparation method, which is a method suitable for the industrial production.

The invention discloses a new application of an annonaceous acetogenin monomeric compound desacetyluvaricin in preparing medicaments for treating lung cancer and breast cancer. The results of antitumor pharmacological tests in animals indicate that the annonaceous acetogenin monomeric compound desacetyluvaricin has distinct inhibitor action on the growth of lung cancer and breast cancer cells, and has antitumor activity hundreds of times higher than the chemotherapeutic drug 5-flurouracil. The desacetyluvaricin can be used for preparing medicaments for treating lung cancer and breast cancer.

The invention provides an annonaceous acetogenin extract extracted from seeds, leaves and barks of Annona squamosa L., a preparation method thereof, an external preparation taking the annonaceous acetogenin extract as an active ingredient, and medicinal use of the external preparation in cancer resistance and relief of cancerous pain. The preparation method for the annonaceous acetogenin extract has a simple process, common, low-price and low-toxicity reagents are adopted and are environment-friendly and relatively safe for human health, the production cost is lower, and the whole preparation method is easy to implement, can effectively shorten the production cycle and is suitable for mass production. An external patch comprising the annonaceous acetogenin extract serving as the active ingredient is easy to use, and has prominent curative effect on cancerous pain and no side effect.

The invention belongs to the technical field of medicines, and in particular relates to a nanosuspension of annonaceous acetogenin drugs prepared from such amphiphilic stabilizers as mPEG PCL, mPEG PLA, mPEG PLGA, mPEG DSPE, mPEG Chol, SPC, Tween80, BSA, TPGS and the like, as well as a preparation method and an application of the nanosuspension. The annonaceous acetogenin total lactone nanosuspension is prepared by virtue of a solvent precipitation-ultrasonic injection method, and according to a prescription, the proportioning ratio of the annonaceous acetogenin drugs to the stabilizer is at 1 to (0.02-10) (in percentage by weight). The prepared annonaceous acetogenin nanosuspension can reach a load-loading capacity to 90% to the greatest extent and can reach a minimum grain size to 123.2nm, and the nanosuspension is good in polydispersity. The nanosuspension is stable in both gastrointestinal fluid and plasma, and the nanosuspension is applicable to oral administration and injection administration; the nanosuspension has a good in-vitro sustained-release effect and is free from burst release; the nanoparticle, in comparison with a crude drug solution, is more obvious in tumor cell inhibitory rate in vitro; the nanosuspension, in in-vivo tissue distribution, shows tumor passive targeting; therefore, the nanosuspension is beneficial for enhancing efficacy and reducing toxic and side effects. Meanwhile, an in-vivo efficacy experiment shows that the nanosuspension is outstanding in antineoplastic efficacy, and the nanosuspension has a broad development prospect.

A novel annonaceous acetogenin derivative used for treating cancer and preventing and eliminating diseases and pests of agricultural crops is prepared through extracting from annonaceous plant and separation, or chemical synthesis.

The invention provides compositions and formulations comprising catechol and / or acetogenins and various combinations thereof; including various combinations with other ingredients including botanical preparations containing acetogenin, an extract of green tea or a therapeutically active flavanoid contained in green tea; and one or more quinones. The invention includes a pharmaceutical composition including a salt of rhodizonic acid, an OH anion-generating base, a non-toxic acid, a quinone, a salt-containing sulfite, catechol and optionally, an acetogenin and an extract of green tea. The compositions and formulations demonstrate positive effects against a broad variety of cancer, autoimmune diseases, viruses and provides antioxidant protection against peroxyl hydrophilic, peroxyl lipophilic, hydroxyl, peroxynitrite and super oxide radicals. The compositions and formulations can be used for nutritional and nutraceutical uses, and used as dietary supplements.

A pharmaceutical composition including a salt of rhodizonic acid, an OH anion-generating base, a non-toxic acid, a quinone, a salt-containing sulfite, catechol and, optionally, an acetogenin. The formulation demonstrates positive effects against cancer, autoimmune disease, viruses and provides antioxidant protection against peroxyl, hydroxyl and super oxide radicals.

The present invention provides a novel annonaceous acetogenin derivative, whose structural formula (II) is: ∴ It is extracted and separated from the Annonaceae plant. Its use is as a drug to treat cancer.

This invention relates to an acetogenin compound linked by amide bonds, its synthesis method and its application. The acetogenin compound is an optically active or racemized compound, whose structural formula is shown in this invention, wherein, Y is C6-20 alkyl; n is 0-3; m is 7-19; R1, R2, R3 and R4 are the same or not, and are H or C1-10 alkyl; when n is 0-2, R3 and R4 are H, Cl, C1-10 alkyl or combined to form fiver-, six- or seven-membered ring shape; when n is 0, R1 and R2 are C1-10 alkyl or combined to form fiver-, six- or seven-membered ring shape. The acetogenin compound has high anticancer activity, and IC50 (mu.M) is lower than 0.04 to breast cancer (MDA-MB-435S). The can be manufactured into anticancer drugs. The synthesis method is simple, and suitable for industrial production.

The present invention relates to a plant extract with the action of resisting diabetes, its application and preparation method. The extract is a kind of acetogenins extracted from branck, leaf, trunk, bark, root, seed and fruit skin of annona squamosa plant as raw material. The compound acetogenins can be made into various dosage forms for curing diabetes, and its preparation method can adopt one or several processes of solvent extraction process, resin adsorption process, supercritical CO2 extraction process and conventional drying process.

The invention relates to a preparation method of annonanceous acetogenins, which is simple to operate and generates less pollution. The preparation method comprises the following steps: (1) taking Annona crassiflora seed, and extracting grease substances in the medicinal material with a supercritical carbon dioxide fluid; (2) carrying out continuous reflux ultrasonic extraction on the degreased medicinal material with an alcohol solution, filtering to obtain an extracting solution, concentrating and drying to obtain a crude extract; (3) separating and purifying the annonanceous acetogenins in the crude extract by high-speed counter-current chromatography, and collecting the annonanceous acetogenins component, wherein the two-phase solvent system is petroleum ether-ethyl acetate-methanol-water, the upper phase is a stationary phase, and the lower phase is a mobile phase; and (4) carrying out vacuum concentration on the annonanceous acetogenins component, precipitating crystals, filtering out the crystals, adding ethyl acetate to dissolve the crystals under reflux, and standing for recrystallization. The purity of the annonanceous acetogenins product is high; and the invention can easily implement industrialized amplification.

The invention discloses a new application of an annonaceous acetogenin monomeric compound annonareticin in preparing medicaments for treating lung cancer and breast cancer. The results of antitumor pharmacological tests in animals indicate that the annonaceous acetogenin monomeric compound annonareticin has distinct inhibitor action on the growth of lung cancer and breast cancer cells, and has antitumor activity hundreds of times higher than the chemotherapeutic drug 5-flurouracil. The annonareticin can be used for preparing medicaments for treating lung cancer and breast cancer.

The present invention relates to the use of whole soft avocados for preparing avocado oil rich in unsaponifiables, said unsaponifiables containing aliphatic acetogenins and / or derivatives thereof. Advantageously, the oil has an acid value of less than or equal to 3 mg KOH / g. The invention further relates to a method for preparing avocado oil rich in unsaponifiables from whole soft avocados, said unsaponifiables containing aliphatic acetogenins and / or derivatives thereof. The invention further relates to avocado oil which is rich in unsaponifiables and which can be prepared by said method. The invention further relates to the use of the avocado oil for preparing an avocado oil concentrate enriched with unsaponifiables, or avocado unsaponifiables that are rich in aliphatic furans. Finally, the invention relates to avocado unsaponifiables which are rich in aliphatic furans or to an avocado oil concentrate which is enriched with unsaponifiables, and which can be prepared from said avocado oil, for the use thereof as a drug, advantageously for the prevention and / or treatment of disorders of the conjunctive tissue, such as arthrosis, joint conditions, such as rheumatism, or periodontal diseases, such as gingivitis or periodontitis.

The invention discloses an epoxy type annonaceous acetogenin compound with antitumor activity; through systematic deep research on the chemical composition of Annona squamosa seeds, wave spectral and mass spectral data analysis indicates the novel epoxy annonaceous acetogenin compound is isolated from Annona squamosa seeds, in-vivo and in-vitro antitumor activity researches indicate that epoxy type annonaceous acetogenins provided herein show high antitumor activity to various tumor cells, such as lung cancer cells, breast cancer cells, and liver cancer cells and show significant inhibitory activity to the solid tumors of mouse implanted hepatic tumor HepG2 and mouse sarcoma S180, and toxicity experiment researches indicate that the epoxy type annonaceous acetogenin compound provided herein has low toxicity and is a good antitumor compound.

The invention discloses an R or S-shaped or racemic annonaceous acetogenin compound with a structure of a formula 1. In the formula, R1 is alkane of C2 to C10, five to seven-element naphthenic hydrocarbon or five-element alpha or beta unsaturated lactonic ring, or substituted benzene ring or naphthalene ring compound; R2 is H or OH; x is 0 to 5, y is 1 to 6, n is 3 to 5, and m is 7 to 19; and when x is 0, y is 1 and n is 3, R1 is alkane of C2 to C10, five to seven-element naphthenic hydrocarbon or substituted benzene ring or naphthalene ring, and R2 is H or OH; or when x is 1 to 5 and y is 6,the R1 is five-element alpha or beta unsaturated lactonic ring, and R2 is hydroxy. The preparation raw materials for the compound are cheap and easily obtained; the preparation method is simple and suitable for industrialized production; and the compound has high anti-tumor activity, and can be used for preparing anti-tumor medicaments. Formula 1.

The invention discloses an annonaceous acetogenin compound annosquacin B which is prepared from sweetsop seeds and can prevent and treat agricultural pests. A plenty of biological activity assay results verify that sweetsop annosquacin B has poisonous activities to different extends on aphis craccivora and T. cinnabarinus and particularly shows a better poisonous activity than that of abamectin, and moreover, annosquacin B is extracted from the sweetsop seeds, so that annosquacin B is low in environmental pollution and environmental-friendly, and can be developed to form novel pesticide preparations which prevent and treat agricultural pests.

The invention provides an annonaceous acetogenin extract extracted from seeds, leaves and barks of Annona squamosa L., a preparation method thereof, an external preparation taking the annonaceous acetogenin extract as an active ingredient, and medicinal use of the external preparation in cancer resistance and relief of cancerous pain. The preparation method for the annonaceous acetogenin extract has a simple process, common, low-price and low-toxicity reagents are adopted and are environment-friendly and relatively safe for human health, the production cost is lower, and the whole preparation method is easy to implement, can effectively shorten the production cycle and is suitable for mass production. An external patch comprising the annonaceous acetogenin extract serving as the active ingredient is easy to use, and has prominent curative effect on cancerous pain and no side effect.

The invention relates to the chemical compound of the chiral annonaceous acetogenins of the comformational restriction structure, the synthetic method and the purpose. The compound has the optical activity compound as the above formula: (R or S configuration) (R or S configuration). The compound of the invention has high anti-cancer activity and selectivity and has the IC50 (MuM) of the human breast duct cancer reaching less than 0.04, and the suppressive activity on the cancer cell is about 100 times that of the normal cell and has better selectivity. The compound of the invention can also be used as the anti-cancer drug and has simple preparation method, which is a method suitable for the industrial production.

The invention discloses a new application of an annonaceous acetogenin monomeric compound annonareticin in preparing medicaments for treating lung cancer and breast cancer. The results of antitumor pharmacological tests in animals indicate that the annonaceous acetogenin monomeric compound annonareticin has distinct inhibitor action on the growth of lung cancer and breast cancer cells, and has antitumor activity hundreds of times higher than the chemotherapeutic drug 5-flurouracil. The annonareticin can be used for preparing medicaments for treating lung cancer and breast cancer.

The invention discloses a preparation method of bubble-shaped annonaceous acetogenins. The method comprises the following steps of: a, taking bubble-shaped sweetsop barks and crushing, adding the crushed bubble-shaped sweetsop barks into a supercritical extraction kettle, and carrying out supercritical CO2 extraction by taking ethanol as an entrainer; b, purifying an extractive by adopting neutral magnesium oxide column chromatography, carry outing gradient elution by utilizing a petroleum ether-acetone mixing agent, collecting an elution solution and decompressing and concentrating to obtain a rough extract; and c, carrying out high-speed countercurrent chromatography separation on the rough extract, monitoring by an ultraviolet detector, collecting target components, refrigerating and crystallizing to obtain the bubble-shaped annonaceous acetogenins. When the preparation method is used for preparing the bubble-shaped annonaceous acetogenins, the process is simple and the efficiency is high, and the content of the obtained products is high, so that the preparation method is suitable for industrial production.

The invention discloses an epoxy type annonaceous acetogenin compound with antitumor activity; through systematic deep research on the chemical composition of Annona squamosa seeds, wave spectral and mass spectral data analysis indicates the novel epoxy annonaceous acetogenin compound is isolated from Annona squamosa seeds, in-vivo and in-vitro antitumor activity researches indicate that epoxy type annonaceous acetogenins provided herein show high antitumor activity to various tumor cells, such as lung cancer cells, breast cancer cells, and liver cancer cells and show significant inhibitory activity to the solid tumors of mouse implanted hepatic tumor HepG2 and mouse sarcoma S180, and toxicity experiment researches indicate that the epoxy type annonaceous acetogenin compound provided herein has low toxicity and is a good antitumor compound.

The invention relates to annonaceous acetogenins nanoparticles, which are prepared by taking cyclodextrin and lecithin as vectors, as well as a preparation method and an application of annonaceous acetogenins nanoparticles. The annonaceous acetogenins (annonaceous acetogenins total lactone or monomer ingredients thereof) nanoparticles are prepared by virtue of a solvent precipitation method; the mass ratio of the annonaceous acetogenins to the cyclodextrin to the lecithin is at 1 to (0.02-20) to (0.02-20); and in accordance with an optimal prescription, the combining proportion of the annonaceous acetogenins to the cyclodextrin to the lecithin is at 4 to 2 to 1 (in percentage by mass). The average grain size of the annonaceous acetogenins nanoparticles is 20-1000nm, and the annonaceous acetogenins nanoparticles are good in dispersity; the annonaceous acetogenins nanoparticles are stable in both gastrointestinal fluid and plasmid, and the annonaceous acetogenins nanoparticles are suitable for both oral administration and intravenous injection; with the application of the nanoparticles, the inhibitory effect of the annonaceous acetogenins on tumor cells can be significantly improved, and meanwhile, in vivo anti-tumor efficacy can be enhanced; and the annonaceous acetogenins nanoparticles have a broad development prospect.

An anticancer drug anemone lactone monomer compound, which is the anticancer lactone monomer compound expoxyrolin B extracted from the seeds of anemone apple. Its preparation method is that after the custard apple seeds are air-dried, they are crushed into coarse powder, and firstly extracted with petroleum ether cold immersion; the petroleum ether is recovered to obtain a red oily liquid, which is placed at room temperature, and a large amount of white precipitate is precipitated at the bottom, and the white precipitate is filtered out. Silica gel column chromatography; using petroleum ether, petroleum ether-ethyl acetate, ethyl acetate-methanol gradient elution, to obtain a kind of anemone lactone monomer compound. According to in vivo and in vitro anticancer pharmacological experiments, it has obvious inhibitory effect on the growth of human liver cancer cells and transplanted liver cancer in mice, and its anticancer activity is several times higher than that of chemotherapeutic drug 5-fluorouracil.

This invention relates to an acetogenin compound linked by amide bonds, its synthesis method and its application. The acetogenin compound is an optically active or racemized compound, whose structural formula is shown in this invention, wherein, Y is C6-20 alkyl; n is 0-3; m is 7-19; R1, R2, R3 and R4 are the same or not, and are H or C1-10 alkyl; when n is 0-2, R3 and R4 are H, Cl, C1-10 alkyl or combined to form fiver-, six- or seven-membered ring shape; when n is 0, R1 and R2 are C1-10 alkyl or combined to form fiver-, six- or seven-membered ring shape. The acetogenin compound has high anticancer activity, and IC50 (mu.M) is lower than 0.04 to breast cancer (MDA-MB-435S). The can be manufactured into anticancer drugs. The synthesis method is simple, and suitable for industrial production.

The invention discloses a pesticide composition containing annonaceous acetogenin and pymetrozine. The pesticide composition contains the active ingredients, pymetrozine and annonaceous acetogenin; the mass ratio of the pymetrozine to annonaceous acetogenin is 40:1 to 1:40; within the ratio range, the pymetrozine and annonaceous acetogenin are synergic to the prevention and treatment of cabbage aphids and cotton aphids; the pymetrozine and annonaceous acetogenin can be made into pesticidal preparations; the mass sum of the pymetrozine and annonaceous acetogenin accounts for 0.1-60% by weight of the total weight of the pesticidal preparations, and the otherness is pesticidal aids; the pesticide composition is applicable to the prevention and treatment of cabbage aphids and cotton aphids.

The invention discloses a method for extracting annonaceous acetogenin from atemoya, and belongs to the field of an annonaceous acetogenin extracting processes. The method comprises the following steps: pretreating an extracted raw material; drying the pretreated raw material, and then crushing by using a vacuum crusher to obtain crushed raw material powder; placing the crushed raw material powderinto a quick freezer for quick freezing to obtain ice powder, crushing the ice powder by using a crusher, unfreezing the crushed ice powder, and drying steam to obtain dry fine powder; placing the dried fine powder and water into a vacuum stirring tank for vacuum stirring; filtering to remove filter residues, and pouring filtrate into an extraction kettle for extraction; and collecting the extract after extracting for 2vh, extracting the extract with chloroform for 4 times, combining chloroform layers, carrying out vacuum filtration, recovering a solvent under reduced pressure at the temperature of 45 DEG C, and drying under reduced pressure to obtain the final product. The raw material is crushed for multiple times, and is crushed again after being frozen, so that the effect is good, theextraction efficiency of the raw material in the later period is high, a large amount of organic solvents are avoided, and the extraction efficiency is high.