74 results about "Aldose reductase" patented technology

The invention discloses an alpha-cyano-4-hydroxy cinnamic acid derivative with aldose reductase inhibition activity and a preparation method and application thereof. The structure of the compound is as shown in formula I. The preparation method comprises the following steps: firstly reacting alpha-cyano-4-hydroxy cinnamic acid with a diamine compound protected by N-tert-butyloxycarbonyl (Boc) to obtain N-Boc-protected alpha-cyanocinnamic carbamide. After removal of a protective group, namely Boc from the compound, the alpha-cyano-4-hydroxy cinnamic acid derivative is obtained by reaction with N-acyl alpha-amino acid (natural or unnatural). The compound disclosed by the invention has inhibition activity against aldose reductase, and can be applied to preparation of medicaments for treating diabetic complications, such as diabetic retinopathy, diabetic senile dementia, disorders of nerve endings and other diseases.

The invention discloses a method for preparing a nebivolol hydrochloride epoxy intermediate 6-fluoro-2-epoxy ethyl chroman. The method includes the following steps that firstly, under the conditions that water, phosphate, inorganic alkali B1, zinc chloride, a hydrogen source, aldose reductase and NADPH exist, the temperature is 30-70 DEG C and the pH value is 6.0-8.0, a reduction reaction happens to 2-chloro-1-(6-fluorochromane-2-yl)-ethanon, and 2-chloro-1-(6-fluorochromane-2-yl)-alcohol is obtained; secondly, 2-chloro-1-(6-fluorochromane-2-yl)-alcohol is heated in a C1-C6 alkanol solvent and inorganic alkali B2 for a reflux reaction, an organic ester solvent is added dropwise for crystallization after the reaction ends, and 6-fluoro-2-epoxy ethyl chroman is obtained. The preparation method is mild in reaction condition, raw materials and solvents are easy to obtain, and the method is suitable for industrial production.

The invention discloses Ganoderma triterpene and a pharmaceutical composition and application thereof. The Ganoderma triterpene has a chemical formula shown in general formula (I) that is shown in the description. The Ganoderma triterpene is active to inhibit aldose reductase and has a promising application prospect.

A medical application of general cactus flavone in preparing the natural medicine or health-care food acting to suppress aldose reductase for preventing and treating the complication of diabetes suchas the healing defect of corneal injury, cataract, neuropathy, retinopathy and renal disfunction. The said general cactus flavone is prepared by the solvent extraction method or resin adsorption method and conventional drying method.

The invention relates to the use of human bendazac lysine in pharmaceutical industry, wherein the bendazac lysine possesses substantial actions for reducing hypoglycemia and saccharifying hemoglobin and urine protein, thus can be applied to the prevention and treatment of diabetes.

The invention relates to an azepine brazilin compound and a synthesis method thereof. By using the structure of a natural product brazilin as a simulation object, a series of brazilin structure compounds containing nitrogen atoms are designed; and substituted cinnamic acid is used as a raw material, and a series of azepine brazilin compounds is obtained through serial chemical conversion and synthesis. Partial azepine brazilin compounds have strong anti-cancer activity, partial compounds have anti-HIV (Human Immunodeficiency Virus) activity, and partial compounds have aldose reductase suppressive activity and obviously reduce the blood sugar level. Medical compositions prepared from the compounds and at least one pharmaceutically acceptable excipient or carrier can be used for treating cancer and resist virus infections.

The invention relates to the technical field of pharmaceutical chemistry, and especially relates to an apigenin-7-O-beta-D-glucuronide derivative, and a preparation method and application thereof. The provided apigenin-7-O-beta-D-glucuronide derivative has the structure shown as the formula I, and is relatively high in water solubility, and thus the characteristic that apigenin-7-O-beta-D-glucuronide is not easy to dissolve in water is changed. The provided preparation method comprises: taking apigenin-7-O-beta-D-glucuronide as a raw material, and using an inorganic-base or organic-base reaction to generate the provided apigenin-7-O-beta-D-glucuronide derivative. The preparation method is simple and easily practicable in technology. Experiments show that the provided apigenin-7-O-beta-D-glucuronide derivative has high inhibition rate on aldose reductase compared with apigenin-7-O-beta-D-glucuronide, and the apigenin-7-O-beta-D-glucuronide derivative prepared by employing the preparation method has the purity larger than 99% and the yield larger than 79%.

The invention discloses a meroterpenoid compound, a medical composite thereof and the application thereof. The compound has the structure shown as chemical formula (I). The compound has the activity on inhibiting aldose reductase and has a good application prospect.

Disclosed herein are a leaf and stem extract of Aster koraiensis, a root extract of Aster koraiensis, a flower extract of Aster koraiensis, a pharmaceutical composition for the prevention or treatment of diabetic complications, a health functional food for the improvement of diabetic complications, and a pharmaceutical composition and health functional food for the prevention or delay of aging, in which each of the compositions and the foods contain, as an active ingredient, at least one of the Aster koraiensis extracts. Each of the extracts is obtained by drying and finely cutting each of the leaf and stem part, root and flower of Aster koraiensis, extracting the cut plant with alcohol or aqueous alcohol solution, filtering the extracted solution and concentrating the filtrate under reduced pressure. Also disclosed are a pharmaceutical composition for the prevention or treatment of diabetic complications, a health functional food for the improvement of diabetic complications, and a pharmaceutical composition and health functional food for the prevention or delay of aging, which contain, as an active ingredient, at least one of fractions obtained by fractionating each of the Aster koraiensis extracts in the order of hexane, ethyl acetate, n-butanol and water fractions. The leaf and stem extract of Aster koraiensis, the root extract of Aster koraiensis and the flower extract of Aster koraiensis have the effect of inhibiting the production of advanced glycation endproducts (AGEs), the causes of diabetic complications, and effectively inhibit aldose reductase (AR) activity. Thus, the disclosed extracts will be highly useful for the prevention or treatment of diabetic complications and the prevention of aging.

The invention belongs to the field of natural medicines and discloses a beta-sitosterol and epalrestat conjugate, a preparation method and application of the conjugate. The conjugate is formed by coupling beta-sitosterol with epalrestat. The structure is shown as formula (I) described in the specification. The preparation method comprises the following steps: dissolving beta-sitosterol and epalrestat in anhydrous dichloromethane, reacting under room temperature overnight under the catalytic effect of pyridine and 4-dimethylamino pyridine, filtering, pouring onto a silica gel chromatographic column, performing rotary steaming and drying, thereby acquiring a target compound. An in vitro MTT detection experiment proves that the beta-sitosterol and epalrestat conjugate has an excellent restraining effect on tumor cell lines, has an IC50 value being 3-6 times that of beta-sitosterol but has low toxicity to normal liver cells L-O2. The compound is used for treating tumor in the manner of conjugating two drug molecules into prodrug, the problems of insufficient antitumor capacity of beta-sitosterol and synergic targeted inhibition for cancer cell aldose reductase target are solved and the effect of clearing away tumor cells in the manner of enhancing cell apoptosis can be achieved.

The invention relates to a method and application of extracting naringenin from the Chinese traditional medicine, bamboo brier. The method includes pulverizing the Chinese traditional medicine bamboo brier, cold soaking in 70% ethanol to obtain the leach solution, concentrating to obtain the extract, suspending in distilled water, extracting and defatting with the petroleum ether, and extracting the defatted water phase with ethyl acetate; performing chromatography on the ethyl acetate phase in a silica gel column, eluting with ethyl acetate-methanol system (9:1), collecting the eluent part by part, combining and concentrating the frontmost segment, gradient eluting with chloroform: methanol with the silica gel column, collecting in a sectional manner, and concentrating to separate the precipitate; and repeatedly purifying with column, and re-crystallizing with methanol to obtain white needle crystal. In the method, pure 3(S)-5,7, 4'-trihydroxy flavanone, i.e., naringenin, extracted from the Chinese traditional medicine bamboo brier, has aldose reductase and Alpha-glucosidase inhibiting activity and is effective in adjusting and controlling glucose absorption of small intestine and preventing and treating diabetic complication. The purified monomer has clear structure and remarkable effect, which facilitates the quality control and the Chinese traditional medicine modernization process; and the naringenin can be further chemically modified to deeply study occurrence and development mechanism of diabetes and complication thereof so as to develop the new drug for treating diabetes and complication thereof.

Embodiments of the invention include methods and compositions for the inhibition of Aldose Reductase by nitric oxide. Certain embodiments of the invention include the induction of nitric oxide by administration of a nitric oxide donor, nitric oxide precursor, inhibitor of a nitric oxide synthase inhibitor, and/or an activator of nitric oxide synthase. Methods may include the treatment of various disease states by inhibiting Aldose Reductase.

The invention discloses a preparation method of sophora flower buds both used as medicines and foods and relates to the field of processing of foods both used as medicines and foods. The preparation method comprises the following steps: washing fresh sophora flower buds; baking the sophora flower bud at 35 DEG C to 45 DEG C for 1.5h to 2h; then baking at 75 DEG C to 85 DEG C for 1h; then frying at110 DEG C to 120 DEG C for 35min to 45min; then cooling to 10 DEG C to 15 DEG C within 5min to 10min; sealing. According to the preparation method disclosed by the invention, different baking temperature and different baking time are adopted, and water, bitter glycoside, triterpenoid saponin, sophoradiol and volatile oil in the sophora flower buds are released or decomposed in sequence under three temperature gradients; meanwhile, flavonoid, betulin, rutin, vitamin P and inhibiting aldose reductase, which have a main health-care effect, in the sophora flower buds are protected through technology operation including rapid cooling and sealing, so that the sophora flower buds are combined with the health-care effect of the other components.

The invention discloses a pharmaceutical composition for treating diabetes and indications thereof. The effective component of the medical composition for diabetes and indications consists of a medicinal extract, a coenzyme Q and folic acid. The medicinal extract consists of extracts of radix curcumae, rheum officinale, rhizoma curcumae longae, aloe and Polygonum cuspidatum. The medical composition for treating diabetes and indications can greatly inhibit the activities of three target enzymes: alpha-glucosidase, hexokinase and aldose reductase, and can effectively inhibit rise of blood sugar and blood fat in a diabetic animal model as well as treat indications induced by diabetes such as hyperlipidemia and retinopathy.