160 results about "Podophyllotoxin" patented technology

The invention relates to conjugates of anti-integrin specific antibodies with cytotoxic compounds, the synthesis, selection, and use of such conjugates for use in cancer therapy or other diseases mediated by cell proliferation, cell migration, or inflammation and which pathology involves angiogenesis or neovascularization of new tissue. In addition the invention relates to combination therapy of such diseases wherein the treatment comprises use of said conjugates in combination with one or more other treatment modalities including but not limited to: chemotherapy, surgery or radiation therapy. The preferred conjugates contain maytansinoid compounds linked to the antibody by a disulfide linkage, and preferred chemotherapeutic agents are doxorubicin, a taxane, a camptothecin, a podophyllotoxin, a nucleoside analog, or a pyrimidine analog.

[PROBLEMS] A novel podophyllotoxin derivative, which is capable of releasing a drug without depending on biological enzymes and can be expected to have an effective therapeutic effect and is soluble in water has been demanded.[MEANS FOR SOLVING PROBLEMS] A polymer having a polyethyleneglycol structural unit and two or more succinic monoamide structural units, particularly a polymer conjugate of a podophyllotoxin in which a carboxylic acid group of polyethyleneglycol / polyaspartic acid copolymer and a hydroxyl group of podophyllotoxin and linked via an ester bond is provided.

The invention relates to a podophyllotoxin vesicle and a preparation method thereof. The preparation method takes a non-ionic surfactant and modification lipids as vesicle materials, and adds cholesterol, dicetyl phosphate and the like as stabilizers. The vesicle having the advantage of good preparation stability is a novel preparation easy to industrialize.

The invention discloses a sulfur-substituted podophyllotoxin derivative as well as a synthetic method and application thereof. The podophyllotoxin derivative, shown by a formula (V), with significantly improved anti-tumor activity and reduced toxic or side effect is obtained by introducing an aromatic heterocyclic compound with rigidity and a further sulfonamide product of 3-amino-5-mercapto-1,2,4-triazole, 2-amino-5-mercapto-1,3,4-thiadiazole, and 4-methyl benzenesulfonyl chloride or 4-methoxy benzenesulfonyl chloride, serving as substituent groups, into the fourth position of a C ring of podophyllotoxin or 4'-demethylepipodophyllotoxin respectively. An activity inhibition experiment of tumor cells in vitro shows that the anti-tumor activity of the compound shown by the formula (V) is significantly improved as compared with that of podophyllotoxin or 4'-demethylepipodophyllotoxin.

The invention discloses a method for preparing desoxy-podophyllotoxin, which comprises the following steps of: 1) smashing radix podophylli raw material into middlings, quenching and percolating or extracting in a backflow way to obtain radix podophylli extract liquid; 2) concentrating the radix podophylli extract liquid obtained by the step 1) to obtain the concentration liquid of the radix podophylli extract liquid, evenly mixing with silica gel, drying, grinding, and filling into a chromatographic column, wherein the chromatographic column is filled with blank silica gel for column chromatography; and 3) eluting the chromatographic column with eluent, taking effluent liquid, the volume of which is equal to that of blank silica gel in the chromatographic column, as one fraction, collecting desoxy-podophyllotoxin-containing fraction, removing the eluent in the desoxy-podophyllotoxin-containing fraction, dissolving residue with dichloromethane or trichloromethane, and recrystallizing to obtain the desoxy-podophyllotoxin. The purity of the desoxy-podophyllotoxin obtained by the method is more than 70%, so that the method is suitable for not only laboratory preparation in small scale but also industrial preparation in large scale.

The invention relates to a prodrug of a compound podophyllotoxin PPT with an anti-tumour activity and a preparation method thereof. The preparation method comprises the following steps: converting the hydroxyl group of C4 of the C-ring of the PPT to chloro-carbonic ester, and reacting the group with the addition product DCM-S of 2-hydroxyethyl disulphide and a benzopyranyl nitrile amino derivative DCM-NH2 to generate a GSH-sensitive PPT-S-DCM prodrug compound. The compound obtained by the preparation method disclosed by the invention has the characteristic of selectively releasing the PPT in vitro and in vivo through tumour cell targeting (GSH sensitivity), and a clinical application prospect; meanwhile, the release behaviour of the PPT prodrug compound can be detected and researched by virtue of the near-infrared fluorophore of benzopyranyl nitrile.

The invention relates to a process for extracting and purifying podophyllotoxin from Dysosma difformis, which comprises the following steps: crushing rhizomes of the Dysosma difformis into coarse powder, pretreating the Dysosma difformis coarse powder with organic solvents, extracting with hot water by reflux, continuously extracting filter residue by hot reflux, filtering again, merging the two filtrates, recovering the organic solvents, adding a defined amount of water to maintain a constant volume so as to obtain a podophyllotoxin extracting solution; and preparing the podophyllotoxin extracting solution into a solution the crude drug content of which is 0.12-0.18g / mL, selecting a purified macroporous adsorptive resin as the adsorption column resin to sufficiently adsorb the solution acting as a sample solution, respectively and sequentially washing off impurities with water and 10% ethanol, eluting with a strippant, collecting the eluted part, recovering the strippant, and adding a defined amount of water to maintain a constant volume so as to obtain a podophyllotoxin purified solution. The organic solvents used in the process are nonpoisonous and can be recovered, and no three wastes polluting the environment are produced. The whole process is green and environment friendly and has the advantages of simple operation and easy industrialization, and the purity of the podophyllotoxin obtained by the process is above 98%.

A novel podophyllotoxin derivative, which is capable of releasing a drug without depending on biological enzymes and can be expected to have an effective therapeutic effect and is soluble in water has been demanded. A polymer having a polyethyleneglycol structural unit and two or more succinic monoamide structural units, particularly a polymer conjugate of a podophyllotoxin in which a carboxylic acid group of polyethyleneglycol / polyaspartic acid copolymer and a hydroxyl group of podophyllotoxin and linked via an ester bond is provided.

The invention relates to a podophyllotoxin-retinoic acid heterocomplex synthesis method and application of a podophyllotoxin-retinoic acid heterocomplex in a medicine for preventing and curing tumors. The podophyllotoxin-retinoic acid heterocomplex has a structural formula as shown in a formula I (shown in the description); a preparation method of the compound as shown in the formula (I) is as follows (shown in the description), wherein a to b represent reaction conditions: a: a reagent is oxalyl chloride, a solvent is methylbenzene, and reaction temperature is 20 to 35 DEG C; b: a solvent is dichloromethane, a catalyst is triethylamine, and reaction temperature is 10 to 30 DEG C. A solvate is a complex prepared from the compound as shown in the formula (I), ethyl alcohol, diethyl ether, n-butyl alcohol, water, acetone or an isopropanol solvent. An experimental result shows that the podophyllotoxin-retinoic acid heterocomplex has a strong inhibiting effect on two human gastric cancer cell strains, and has an IC50 value in a nano-mole level, which is remarkably better than that of positive control agents: retinoic acid and etoposide. The compound as shown in the general formula (I) has the highest antiproliferative activity on human gastric cancer BGC-823 cells, is used for preventing and curing cell proliferation abnormity related diseases, and is particularly applied in the medicine for preventing or curing the tumors.

The invention relates to a pH and temperature dual responsive copolymer and a preparation method and an application thereof, which belong to the technical field of pharmaceutical polymers. A molecular structure of the copolymer is shown as follows, and the molecular weight is 10000 to 30000. The copolymer is prepared in the following steps of (a) preparing a copolymer of diethyl allylmalonate and N-vinylcaprolactam; (b) preparing a copolymer of allylmalonic acid and N-vinylcaprolactam. The copolymer is used for self assembly in water to form nanomicelles as controlled release carriers of podophyllotoxin drugs. Raw materials are low in price and are easy to obtain, a synthetic method is simple, products are easy to separate and purify, and the operability is strong. The copolymer can be assembled by self in a water solution to form stable spherical nanomicelles which have high drug loading capacity and encapsulation efficiency on podophyllotoxin and have pH and temperature dual responsive controlled release performance on the podophyllotoxin, and the copolymer can be used for constructing an intelligent drug controlled release system.