38 results about "Quercetin derivatives" patented technology

The invention discloses quercetin or quercetin derivative and platinum complexes and salts thereof in the filed of medicines. The chemical structural formula of the complexes is the formula (I) or formula (II). The invention also discloses methods for preparing the complexes and the salts thereof and uses of the complexes and the salts thereof in the preparation of drugs for treating cancers.

The invention discloses an extract of an active anti-fatigue part of okra, and a preparation method and application thereof. The extract of the active anti-fatigue part of okra uses total polyphenols as a main active anti-fatigue component, wherein the total polyphenols account for 11.79 to 23.34% of the total mass of the extract of active anti-fatigue part and mainly comprise catechin derivatives and quercetin derivatives, and the quercetin derivatives are mainly composed of quercetin-3-O-gentiobioside, quercetin-3-O-glucose-xyloside, isoquercitrin, quercetin-3-O-malonyl-glucoside, rutin and quercetin. The extract of the active anti-fatigue part of okra provided by the invention can substantially prolong the load swimming time of mice, eliminate lactic acid accumulation after sports, reduce the content of serum urea nitrogen, increase hepatic glycogen and improve the antioxidation capability of mice in a stress state, and has substantial anti-fatigue effect.

The invention relates to bola type quercetin derivatives and a preparation method thereof. A bola type amphiphilic molecule is formed by connecting two polar head groups by using a hydrophobic chain; and unique natures such as better stability and compatibility in a plasma membrane are given to the bola type amphiphilic molecule through the special structure. The bola type quercetin derivatives shown as general formulas I-V are developed by utilizing bola type characteristics to increase the water solubility and the bioavailability of the derivatives; meanwhile, proved by research results, compared with non-bola type quercetin lipid derivatives, the bola type quercetin derivatives are capable of better inhibiting the growth activity of tumor cells; the bola type quercetin derivatives are transformed into nanometer drugs through micromolecule self-assembly on the basis of the structure to improve the physicochemical property of compounds; the ability of targeting focal tissues is enhanced and the damage of the drugs to normal tissues and cells is reduced; and R and n in the general formulas are defined as the claim.

The invention relates to a nitrogen mustard quercetin derivative comprising a stereisomer or a tautomer, a preparation method of the nitrogen mustard quercetin derivative, a medicinal composition taking the derivative as an active component, and application of the medicine to cancer treatment. The preparation method of the derivative comprises the following steps: preparing Mannich alkali of quercetin from the quercetin, formaldehyde and chlorethamin, and performing reaction on the Mannich alkali and substituted phosphoramidic dichloride to prepare the nitrogen mustard quercetin derivative. The nitrogen mustard quercetin derivative has an anti-tumor effect.

The invention discloses a quercetin derivative and a preparation method thereof, and belongs to the field of pharmaceutical synthesis. The invention aims to solve the problems of poor water solubility and low bioavailability of quercetin in the prior art, and provides a quercetin derivative Derivatives, the fat solubility of the obtained quercetin derivatives is far better than that of quercetin, and the bioavailability is greatly improved, which can be used for treating cardiovascular and cerebrovascular diseases, anti-cancer and anti-cancer. Another object of the present invention is to provide a method for synthesizing the quercetin derivative, using quercetin to protect the hydroxyl group, then performing a substitution reaction and a hydrogenation reaction to prepare the quercetin derivative, and obtaining a high-purity quercetin derivative, The present invention chemically modifies natural quercetin, and through the substitution reaction at the 5-OH hydroxyl position, it is beneficial to improve its water solubility and fat solubility, and improve its bioavailability. The method has simple principle, high product yield, and high product yield. 37%‑57%, purity 96%‑98%, R f = 0.2 to 0.5.

The invention discloses application of a compound (QB) shown in a formula I in preparation of medicines for prevention and / or treatment. The MTT experiment displays that the proliferation inhibition effects of the compound QB on the four tumor cells, such as human esophageal squamous carcinoma cell EC109, the human esophageal squamous carcinoma cell EC9706, the human gastric carcinoma cell SGC7901 and mouse melanoma cell B16-F10, are obviously superior to those of quercetin. The inhibition effect of (IC50=5.201mu g / mL) on the EC109 cells is equivalent to that of fluorouracil 5-FU(IC50=5.426mu g / mL), the toxic or side effect is relatively small, and the compound is a potential antitumor candidate compound.

The invention discloses a derivative of quercetin and its preparation method and application. In the preparation method, dichlorodiphenylmethane is used to protect the quercetin o-diphenol hydroxyl group, and combined with a benzyl protecting group to obtain selective protection. The quercetin derivatives are separately reacted with dimethyl sulfate, diethyl sulfate, allyl bromide, p-toluenesulfonyl chloride and acetic anhydride to generate corresponding quercetin derivatives. The prepared derivative compounds all showed better inhibitory activity of NRK-49F proliferation than quercetin. Among them, quercetin derivatives 20a‑1, 14a‑2 and 23d‑1, which were substituted by methyl group and p-toluenesulfonyl group, exhibited better inhibitory activity on NRK‑49F proliferation, and the inhibition rates reached 86.33%, 78.04%, 75.91%. It can be seen that the currently obtained quercetin-derived products have a significant inhibitory effect on the proliferation of renal fibroblast NRK-49F.

The invention provides a quercetin derivative nano-micelle, including quercetin derivatives, lecithin, sodium taurocholate, etc.; the quercetin derivatives are 2-hydroxyl-4-(3,5,7 -Trihydroxy-4-oxo-4H-benzopyran-2-yl)phenyl dodecanoate. The quercetin derivative nano micelles prepared by the invention have better encapsulation efficiency and drug loading capacity, and higher bioavailability.

The invention discloses a quercetin derivative chemically modified by dodecanoyl chloride and a synthesis method thereof, which belongs to the field of pharmaceutical synthesis. The method is as follows: adding quercetin and dodecanoyl chloride as raw materials into a solvent, adding an appropriate amount of catalyst and Acidity regulator, under the condition of ice-water bath to room temperature, react for 8-10 hours, after the reaction, adjust the pH value to 6-7 with acid, add water, extract with ethyl acetate, separate liquid, continue to use acetic acid in the water layer Ethyl was extracted 2-3 times, the ethyl acetate layers were combined, water-absorbing agent was added, overnight, suction filtration, ethyl acetate was distilled off, and the crude product was purified by 200-300 mesh silica gel column chromatography, and the preparative liquid phase was purified again to prepare High-purity quercetin derivatives were obtained. The quercetin derivative obtained in the present invention chemically modifies the natural quercetin, and through a substitution reaction at the 4'-OH hydroxyl position, it is beneficial to improve its water solubility and fat solubility, and improve its bioavailability. This quercetin derivative can be used to treat diseases such as hypertension, myocardial ischemia and cancer.

A method for treating cancer with a combination of a chemotherapy agent and a composition that includes a quercetin, vitamin B3, and vitamin C. The quercetin can be quercetin aglycon or a quercetin derivative, and the composition can also include folic acid.