895results about How to "High anticancer activity" patented technology

Disclosed is a compound represented by the Structural Formula (I):

• • Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R₇R₈)—.
  • R₁ and R₂ are independently an aryl group or a substituted aryl group, R₃ and R₄ are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.
  • R₅-R₆ are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.
  • R₇ and R₈ are each independently —H, an aliphatic or substituted aliphatic group, or R₇ is —H and R₈ is a substituted or unsubstituted aryl group, or, R₇ and R₈, taken together, are a C2-C6 substituted or unsubstituted alkylene group.
  • Z is ═O or ═S.

Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject with cancer by administering to the subject a compound of Structural Formula (I) in combination with taxol or an analog of taxol.

One embodiment of the present invention is a method of treating a subject with a multi-drug resistant cancer. The method comprises administering to the subject an effective amount of a compound represented by Structural Formula (I):

In accordance with the present invention, there are provided compositions and methods useful for the in vivo delivery of substantially water insoluble pharmacologically active agents (such as the anticancer drug paclitaxel) in which the pharmacologically active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacologically active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diameter of less than about 1 micron. The use of specific composition and preparation conditions (e.g., addition of a polar solvent to the organic phase), and careful selection of the proper organic phase and phase fraction, enables the reproducible production of unusually small nanoparticles of less than 200 nm diameter, which can be sterile-filtered. The particulate system produced according to the invention can be converted into a redispersible dry powder comprising nanoparticles of water-insoluble drug coated with a protein, and free protein to which molecules of the pharmacological agent are bound. This results in a unique delivery system, in which part of the pharmacologically active agent is readily bioavailable (in the form of molecules bound to the protein), and part of the agent is present within particles without any polymeric matrix therein.

The present invention relates to a group of glycosyl transferase and applications thereof, and specifically provides applications of the glycosyl transferase gGT29-7 and a derived polypeptide thereof in terpene compound glycosylation catalysis and new saponin synthesis, wherein the glycosyl transferase can specifically and efficiently transfer the glycosyl from a glycosyl donor to the first glycosyl on C-3 site and/or C-6 site of a tetracyclic triterpene compound so as to extend the sugar chain. The glycosyl transferase of the present invention can further be used for constructing artificial ly-synthesized rare ginsenosides and a variety of new ginsenosides and derivatives thereof.

The invention discloses a chrysin nitrogen-containing derivative. Nitrogen-containing groups are introduced to a chrysin structure to synthesize the chrysin nitrogen-containing derivative with a novel structure. The molecular structure of the chrysin nitrogen-containing derivative is shown as (I), wherein R represents fatty amidogens of C1-C20, aromatic amidogens of C6-C20, heterocycle-containing amidogens of C1-C20 and alcohol amidogens or benzyl amidogens of C1-C20, and n represents the carbon chains of C2-C20. The derivative can have the biological activities of some similar alkaloids and simultaneously enlarge polarities, and the synthesized derivative presents a certain alkalinity, which is convenient to achieve the purpose of improving the water solubility with inorganic acid or organic acid finished salts.

The invention is a pyrrol alkyl matrix metalloproteinase inhibitor and preparing method, relating to the corresponding compound preparation, active test of inhibiting matrix metalloproteinase and the drug combination in which it acts as active component.

The invention relates to a method for extracting and preparing medlar leaf flavone. The method comprises the following steps of: (1) after picking and removing impurities manually, drying medlar leaves indoor to obtain a medlar leaf dry sample; (2) crushing the medlar leaf dry sample and screening the crushed medlar leaf dry sample to obtain medlar powder; (3) leaching the medlar powder by using ethanol to obtain leaching liquor; (4) grinding the leaching liquor by using a colloid grinder to obtain colloidal medlar leaf leaching solution; (5) homogenizing and separating the colloidal medlar leaf leaching solution to obtain liquid supernatant and filter residue; (6) removing impurities from the liquid supernatant by using a ceramic membrane to obtain filtrate; (7) adsorbing the filtrate by using weak-polarity macroporous adsorption resin and eluting the filtrate by using ethanol solution to obtain medlar leaf flavone-containing eluent; and (8) after concentrating and drying the medlar leaf flavone-containing eluent under a reduced pressure in a vacuum, obtaining the medlar leaf flavone powder. The method has low cost and high extraction rate; and the obtained medlar leaf flavone has stable properties, high content, and high biological activity of heart head blood-vessel disease resistance, cancer resistance, oxidation resistance and the like.

Disclosed is an anticancer pharmaceutical composition comprising phenformin or a pharmaceutically acceptable salt thereof, and 2-deoxy-D-glucose as active ingredients. These ingredients act in synergy with each other, thus exhibiting more potent inhibitory activity against the growth of cancer cells, compared to individual ingredients. Also, the synergistic anticancer activity allows the individual drugs to be used in lower amounts, which leads to a reduction in the occurrence of adverse effects. In addition, the time-lag release or administration of the ingredients decreases blood lactic acid levels to significantly mitigate the adverse effect of lactic acidosis, as well as exerting high anticancer effects. Particularly, the pharmaceutical composition can be formulated to dosage forms effective for therapy, increasing the drug compliance of the subject.

The invention relates to a novel piperazidine or homopiperazine oxalyl hydrazine class compound as represented by formula I, wherein each symbol has meanings defined in the description. The invention further relates to the preparation of the piperazidine or homopiperazine oxalyl hydrazine class compound, use of the piperazidine or homopiperazine oxalyl hydrazine class compound in preparing medicament for treating and/or preventing tumor and/or cancer, medicament composition containing the piperazidine or homopiperazine oxalyl hydrazine class compound. The piperzzidine or homopiperazine oxalyl hydrazine class compound has effective anti-tumor activity.

The invention relates to a tobacco additive for increasing smoke concentration and a preparation method and application thereof. Shortleaf kyllinga herb, lysimachia foenum-graecum and murraya kwangsiensis are used as main raw materials. The preparation method comprises the following steps: soaking a raw material mixture in an organic solvent or performing reflux extraction for 1 to 360 hours; leaching the mixture by using qualitative filter paper and filtering off residues to obtain natural tobacco additive extracting solution; performing concentration on the extracting solution under reduced pressure in a water bath at the temperature of between 50 and 80 DEG C; recycling a solvent of the extracting solution to obtain a natural tobacco additive; dissolving the tobacco additive in a certain amount of single or mixed solution consisting of water, ethanol and propylene glycol; and spraying the mixture accounting for 0.005 to 2.5 percent of the weight of cigarette cut tobacco, cut stems or thin tobacco slices onto sample cut tobacco according to the conventional flavoring process. The tobacco additive can remarkably enrich tobacco flavor, effectively increase the smoke concentration of the cigarette, enhance sweet feeling in an oral cavity and achieve fine and soft smoke. The additive has the advantages of simple preparation process, low cost and wide market prospect.

The invention provides a pectin manufacture technology. The pectin manufacture technology comprises the following steps: firstly, cleaning and washing peel pomace; secondly, performing hydrolysis; thirdly, performing separation and concentration; fourthly, performing enzymolysis on pectin: adjusting the pH value of the concentrate C to be 3.0-5.0, adding pectolase of 0.2-0.5 permillage, insulating at 30-45 DEG C for 4-6 hours, wherein during the insulation process, the pectolase can act on the specific position of the pectin molecular chain, a D-galacturonic acid Alpha-1,4-glucosidic bond locates and decomposes the original pectin into small molecules, and the molecular weight of the pectin is 10,000-20,000 g/mol; and fifthly, performing vacuum drying, adopting vacuum low-temperature drying with the vacuity of -0.70 to -0.80 MPa and the temperature of 60-70 DEG C to obtain the end product. According to the invention, an enzymic method degradation bio-engineering technology is adopted to reduce the molecule weight of the pectin to 10,000-20,000 g/mol; and the pectin after selective modification of the molecule chain has an obvious antitumor activity, and functions of removing in vivo heavy metal and adjusting blood sugar and blood fat.

The present invention relates to a method for selecting pharmacological compounds for selective inhibition of cancer cells comprising identifying a compound, determining the reduction potential (E_R) of the compound, and selecting the compound which has a reduction potential from −1.1 to −0.8 volts. The invention also relates to a pharmacological compound comprising at least one cyanine dye or merocyanine dye, wherein the dye has at least one cationic substituent, wherein the dye has a reduction potential of from—1.1 to 0.8 volts, and wherein the pharmacological compound demonstrates selective inhibition of cancer cells.

The invention relates to a process for extracting and refining anthocyanin in coarse rice, rice bran of black rice. According to the technical scheme, the process comprises the following steps of: extracting raw materials by using an acidic aqueous solution under the condition of keeping temperature, filtering, mixing extracting solutions, adsorbing by macroporous adsorbent resin, washing the resin by using water, desorbing by using an alcohol aqueous solution with appropriate concentration, concentrating a desorbed solution until the relative density is 1.1 to 1.2, and performing spray drying or vacuum drying to obtain an anthocyanin extract, wherein the content of the anthocyanin is more than 25 percent.

In accordance with the present invention, there are provided compositions and methods useful for the in vivo delivery of a pharmaceutically active agent, wherein the agent is associated with a polymeric biocompatible material.

Disclosed is a compound represented by the Structural Formula (I):

• • Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R₇R₈)—.
  • R₁ and R₂ are independently an aryl group or a substituted aryl group, R₃ and R₄ are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.
  • R₅-R₆ are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.
  • R₇ and R₈ are each independently —H, an aliphatic or substituted aliphatic group, or R₇ is —H and R₈ is a substituted or unsubstituted aryl group, or, R₇ and R₈, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ═0 or ═S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject with cancer by administering to the subject a compound of Structural Formula (I) in combination with taxol or an analog of taxol.