37 results about "Trilobatin" patented technology

The invention discloses an active extract which is extracted from fagaceae and other plants by using 5 to 95% alcohol aqueous solution serving as a solvent, wherein the content of the trilobatin in the active extract is between 30 and 99.9%. The invention also discloses a preparation method for the active extract and application thereof in preparing a medicament for treating diabetes mellitus, diabetes nephropathy and hepatic edema.

The invention provides a mass isolation method of a natural sweetener Trilobatin. The method comprises the following steps: adding a crushed Trilobatin raw material into 30-90% (by volume) of ethanol according to the solid-to-liquid mass ratio of 1:10-50, carrying out thermal reflux for separation, filtering a separating medium to obtain filter residue and a filtrate, and carrying out vacuum concentration on the filtrate until there is no alcohol taste so as to obtain an isolate; dissolving the isolate by adding water, extracting with ethyl acetate, and carrying out vacuum concentration on an extract liquor to obtain an ethyl acetate extract; and separating the ethyl acetate extract by high-speed countercurrent chromatography so as to obtain the natural sweetener. The isolation method is simple and fast and has short isolation cycle. Monomers preparation amount is large, and monomers have multiple pharmacological activities.

A method of producing trilobatin is disclosed. The method comprising contacting a polypeptide comprising an amino acid sequence at least 90% identical to SEQ ID NO: 8 and having a 4′-O-glycosyltransferase activity with phloretin and UDP-glucose under conditions which allow the formation of trilobatin, thereby producing trilobatin. A method of producing a plant which produces trilobatin, transgenic plant or plant cell and methods of producing transgenic plants are disclosed. Composition comprising trilobatin are also disclosed.

The invention provides an application of trilobatin to a cerebral ischemia-reperfusion injury preventing and treating drug. 5 g of trilobatin, 75 g of medicinal starch and 20 g of microcrystalline cellulose are taken, the medicinal starch is dried firstly, sieved by a 120-mesh sieve and then mixed with trilobatin and microcrystalline cellulose, the mixture is sieved by the 120-mesh sieve twice, hard capsules are filled with the mixture, 1000 capsules are prepared, and each hard capsule contains 0.5 mg of the main drug ingredients. Trilobatin is used for preparing the cerebral ischemia-reperfusion injury preventing and treating drug, and animal experiments prove that prepared pharmaceutical composition can prevent and treat cerebral ischemia-reperfusion injury. Materials are widely sourcedand easily available, and trilobatin is simple, easy and good in treatment effect when used for preparing the drug.

The invention discloses an active extract which is extracted from fagaceae and other plants by using 5 to 95% alcohol aqueous solution serving as a solvent, wherein the content of the trilobatin in the active extract is between 30 and 99.9%. The invention also discloses a preparation method for the active extract and application thereof in preparing a medicament for treating diabetes mellitus, diabetes nephropathy and hepatic edema.

The invention discloses a functional sweetener and an extraction method thereof. The functional sweetener should contain a trilobatin component and is extracted from a malus plant. The extraction method comprises the following six main steps: digestion; extraction; preliminary separation; fine separation; concentration; and drying and crystallization. The eventually extracted functional sweetener is great in output and controllable in cost.

The invention provides a sodium-glucose cotransporter 2 (SGLT2) inhibitor. The SGLT2 inhibitor is trilobatin, and the specific structure of the trilobatin is shown as the following formula (please seethe specifications for the formula); and the trilobatin and the SGLT2 interact with each other, the trilobatin is in hydrogen bond connection with ASn75 and Tyr290 sites of the SGLT2, and thus the trilobatin can significantly inhibit glucose reabsorption, lowers the overall blood glucose level of an experimental subject, and meanwhile, can further improve insulin resistance of the experimental subject effectively.

The embodiment of the present invention provides Mujiangyeke Granules and a preparation method. The Mujiangyeke Granules contain Mujiangyeke extracts, sour agents and tangerine peel powder, and have high content of active ingredients and good taste. In Mujiang Yeke Granules, the content of phlorizin reaches 60%, and the content of trilobatin reaches 40%. Trilobatin is a natural sweetener. The increase of trilobatin content increases the sweetness of the product itself. On the one hand, it is beneficial to the use of diabetic patients; on the other hand, for non-diabetic patients, as a general health care product, it can improve memory , maintain normal blood sugar levels, and also have anti-infection effects. At the same time, because there are no sweeteners added, it will not increase weight and is friendly to people who lose weight.

The invention discloses a method for extracting trilobatin, which comprises the following steps: step 1, taking leaves of Cordyceps sinensis, pulverizing, adding water for heating extraction, heating and extracting and filtering while hot to obtain filtrate; step 2, freezing and refrigerating the filtrate; Step 3, take out the frozen filtrate, then thaw at a temperature below 40°C, and filter to obtain a precipitate; Step 4, dry the precipitate; Step 5, put the dried precipitate into a heated ethanol solution to dissolve, and the temperature of the ethanol solution is 60 °C. -80°C; then the ethanol solution is cooled to -20-40°C to obtain crystals; in step 6, the crystals are dried to obtain pure yellow trilobatin. The invention only needs to be filtered after freezing and redissolving, and then heat-saturated and crystallized to obtain high-purity trilobatin, which is short in time, simple in operation, easy in industrialized production, more environmentally friendly, and less harmful to the operator's body.

The invention discloses application of trilobatin in preparation of a medicine for treating acute liver injury, and belongs to the field of pharmacy. According to the invention, a D-GalN / LPS induced mouse acute liver injury model is constructed, trilobatin with different concentrations is given, and it is found that the trilobatin has the effect of preventing and treating D-GalN / LPS induced mouse acute liver injury and is dose-dependent. Therefore, the trilobatin can be used for preparing the medicine for treating the acute liver injury, so that a feasible new technical scheme is provided for clinical medicine. In addition, the trilobatin can be used as an autophagy inducer to induce cell autophagy. The functional range of the trilobatin is expanded, and new application of the trilobatin is provided. The implementation of the invention provides a new medicine for clinically treating acute liver injury, and develops a new direction for further industrial application of trilobatin.

The invention discloses a method for preparing a mixed hypoglycemic preparation of phloridzin. The auxiliary materials are made into tablets or capsules; the mass ratio of described phloridzin, trilobatin, xylitol, microcrystalline cellulose, maltodextrin and magnesium stearate is 0.1:0.15‑0.2:1‑2: 0.2‑0.4:2‑3:0.2‑0.5. In the present invention, phloridzin and trilobulin are mixed in an optimal ratio, and combined with a microcapsule process to prepare an oral tablet or capsule administration preparation, so as to exert the protective effect of trilobin on phlorizin and make phlorizin pass through Intestinal absorption, inhibiting SGLT increases the excretion of glucose from the urine, and thus uses this new target and mechanism to treat type II diabetes.

The present disclosure provides a first sweetening composition comprising a) a natural sweet-tasting carbohydrate, b) a stevia compound, c) rubusoside, a rubusoside derivative, neohesperidin, thaumatine, phloretin, trilobatin, monatin, hesperetin, an enzyme-treated steviol glycoside or any combination thereof, and d) tannin, wherein component d) is present in an amount in the range from 1 mg / l to 400 mg / l, or wherein, based on the total weight of components b), c) and d), component b) is present in an amount in the range from 45 to 75 wt-%, component c) in an amount in the range from 2 to 40 wt-%, and component d) in an amount in the range from 2 to 40 wt-%. Furthermore, the present disclosure provides a second sweetening composition comprising a) a natural sweet-tasting carbohydrate, b) a stevia compound, c) rubusoside or a rubusoside derivative, d) tannin and e) oak extract or pomegranate extract. And, the present disclosure provides a third sweetening composition comprising a) acesulfam or aspartame, b) sucralose, a stevia compound, saccharin or cyclamate, c) neohesperidin, thaumatine, rubusoside, a rubusoside derivative, phloretin, trilobatin, monatin and / or hesperetin, and d) tannin in an amount in the range from 1 mg / l to 400 mg / l or wherein, based on the total weight of components a), b), c) and d), the component a) is present in an amount in the range from 10 to 50 wt-%, component b) in an amount in the range from 15 to 65 wt-%, component c) in an amount in the range from 0.1 to 4 wt-%, and component d) in an amount in the range from 5 to 50 wt-%. The present disclosure also provides a fourth sweetening composition comprising a) 0.1 to 50 g / l of a natural sweet-tasting carbohydrate, b) 40 to 120 g / l of a natural sweet-tasting carbohydrate different from a), and c) 30 to 300 mg / l of rubusoside or a rubusoside derivative. Moreover, the present disclosure is about the use of said sweetening compositions for sweetening and preparing beverages as well as for preparing syrups as precursors and for the preparation of such beverages. The disclosure is also about a beverage comprising said sweetening compositions as well as about a process for preparing such beverage.

The invention provides a method for isolating a large amount of natural sweetener trilobatin, by adding ethanol with a volume fraction of 30-90% to the pulverized trilobatin raw material at a solid-to-liquid mass ratio of 1:10-50, and heating to reflux Separating, filtering the separating liquid, separating the filter residue and filtrate, concentrating the filtrate under reduced pressure until it has no alcohol smell, and obtaining the isolate; dissolving the isolate in water, and extracting with ethyl acetate, and concentrating the extract under reduced pressure to obtain ethyl acetate extract; The ethyl acetate extract was separated by high-speed countercurrent chromatography to obtain a natural sweetener. The separation method of the invention is simple and quick, the separation period is short, the monomer preparation amount is large, and the monomer has various pharmacological activities.