159 results about "Podophyllotoxin" patented technology

The present invention discloses compositions comprising podophyllotoxins, analogs thereof, or derivatives thereof, and a surfactant. The invention also discloses a podophyllotoxin composition further comprising a targeting moiety. The present invention also discloses a method of delivering a podophyllotoxin, an analog thereof or a derivative thereof, to a cell by administering the described podophylootoxin compositions. Further, the present invention discloses a method of making the podophyllotoxin compositions.

The invention discloses a Chinese traditional medicine composition for treating cancer and its preparation. The composition comprises the following traditional Chinese medicines by weight ratio: 500 to 1000 of American ginseng, 500 to 1000g of radix astragali, 500 to 1000g of Radix aristolochiae, 200 to 1200 of cordyceps sinensis, 120 to 1000 of sappan wood, podophyllotoxin, radix bupleuri, turmeric, heydyotis, common pleione pseudobulb, tulipa edulis and barbat skullcap, 500 to 1500 of airpotato yam rhizome, curcuma rhizome, rhizoma paridis, pseudo-ginseng, salvia chinensis and mythic fungus, 50 to 100 of licorice, 1 to 20 of gamboge and 500 to 2000 of ligustrum lucidum. A traditional Chinese medicine preparation prepared by the invention has the advantages of controllable and stable quality, convenient taking, and is used for the treatment and the auxiliary treatment of various types of cancers, the composition provided in the invention has definite therapeutic effect and small toxicity and side effect.

The invention relates to a series of novel 4'-nordeoxypodophyllotoxin aromatic acid esters, substituted benzene sulfonates, and ether derivatives and application thereof in preparing a botanical insecticide. The 4'-nordeoxypodophyllotoxin aromatic acid esters, the substituted benzene sulfonates, and the ether derivatives have a general chemical formula shown at the right. An experiment proves that the 4'-nordeoxypodophyllotoxin aromatic acid esters, the substituted benzene sulfonates, and the ether derivatives are partially higher than podophyllotoxin and deoxypodophyllotoxin, wherein insecticidal activities of certain compounds are all higher than that of a botanical insecticide-toosendanin which has come into the market, and the compounds can be used for preparing the botanical insecticides with high-efficiency and low-toxicity.

The invention relates to a method for extracting podophyllotoxin from dysosma versipellis. The method comprises the steps as follows: extracting with waveform to obtain extract; adding the extract to macroreticular resin column to absorb; eluting; recovering alcohol in a pressure reduced way; concentrating; adding the concentrate to polyamide chromatographic column; eluting; carrying out support detection with homogenous polyamide film by utilizing the eluant; collecting; recovering the solvent in a pressure reduced way; adding acetone to crystallize; separating and crystallizing; washing; and drying to obtain the product. The method provided by the invention is simple in operation, less in consumption of solvent, low in production cost, stable in technology, low in energy consumption and pollution, and high in purity of the obtained product (99%), and is suitable for experiment and industrial preparation and preparative production.

Etoposide analogs with improved water-solubility such as 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4β-(4″-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4β-(4″-fluoroanilino)-4-desoxy-podophyllotoxin (9) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

The invention discloses a 4-amino oxadiazole epipodophyllotoxin derivative and a preparation method and application thereof. The 4-amino oxadiazole epipodophyllotoxin derivative has a structure shown as a Formula (1), wherein R1 represents hydrogen or methyl, and R2 represents hydrogen, alkyl, aryl, heteroaryl or heteroaryl alkyl. The derivative is prepared according to the following steps of: firstly, subjecting podophyllotoxin serving as a raw material to azido reaction, reduction, addition and elimination to obtain isothiocyanate epipodophyllotoxin; secondly, reacting an isothiocyanate epipodophyllotoxin intermediate with a hydrazide compound to obtain a thiosemicarbazide derivative; and finally, subjecting to cyclization, and thus obtaining a corresponding 4-amino oxadiazole derivative. The preparation method is simple and is easy to operate. Initial in-vitro screening tests show that the toxicity of the derivative on normal cells is obviously reduced, meanwhile, certain compounds have better anti-tumor activity, and high-efficiency and low-toxicity anti-tumor drugs can be expected to be prepared.

The invention relates to a method for extracting podophyllotoxin from umbrella leaves, comprising the following steps of: using the umbrella leaves as raw materials; ultrasonically extracting 75-85 percent of methanol; decompressing and condensing to obtain extract; ultrasonically extracting by using ethyl acetate; concentrating an extracting solution; placing crystals; dissolving the crystals by using absolute ethyl alcohol; refluxing and decoloring by adding active carbon; filtering, extracting an organic solvent; concentrating, crystallizing; and recrystallizing and drying absolute methanol to obtain the podophyllotoxin. The invention has simple technical operation and low cost.

The invention discloses a nitrogen-substituted podophyllotoxin derivative with anti-tumor activity and a preparation method and use thereof. According to the method, 2-aminopyrimidine, 2-aminopyridine, 2-amino-3-methylpyridine, 2-amino-4-methylpyridine, 2-amino-5-methylpyridine, 2-amino-4,6-dimethyl pyridine, 3-aminopyridine, 3-amino-4-methylpyridine, 5-amino-2-methylpyridine, 3-amino-2-chloropyridine or 4-amino-2-chloropyridine is respectively introduced to an activated C-ring fourth position of a podophyllotoxin compound through nitrogen substitution reaction, so as to obtain the nitrogen-substituted podophyllotoxin derivative, represented by a formula (V) shown in the specification, with excellent anti-tumor activity. The nitrogen-substituted podophyllotoxin derivative disclosed by the invention acts on tumor cells through multiple ways and multiple target points, and the anti-tumor activity of the nitrogen-substituted podophyllotoxin derivative is remarkably improved compared with that of the podophyllotoxin compound. The compound disclosed by the invention can be used for preparing anti-tumor drugs and is clinically applied to anti-tumor treatment.

The invention provides a deoxidized podophyllotoxin polymer micelle freeze-drying preparation. Polymer micelle consists of an amphiphilic block polymer, and a polyethylene glycol monomethyl ether-poly (D,L) lactide block copolymer is optimal. A preparation method of the preparation comprises the steps that deoxidized podophyllotoxin and the block polymer are dissolved in an organic solvent; the solvent is flooded to be gel; the gel is hydrated; the micelle is obtained; and the freeze-drying preparation is prepared further. The freeze-drying preparation can be used for treating a tumor; a medicine carrying encapsulation rate is above 90%; the particle size of the redissolved micelle is 40-70nm; and a redissolved micelle solution can be stabilized for 4-24h at 25 DEG C.

The invention relates to a preparation method for natural product podophyllotoxin, which comprises the following steps of pulverizing raw materials into 20 to 60 meshes; taking CO2 and chloroform as solvents; super-critically extracting for 1 to 3 hours; washing analytic matters by utilizing deionized water; dissolving by utilizing chloroform; carrying out a medium-pressure alumina column chromatography; carrying out gradient elution by utilizing a petroleum ether-methanol chloroform mixing solution; collecting high-concentration fraction, concentrating and crystallizing; and recrystallizing the methanol chloroform mixing solution. The method for producing the podophyllotoxin has the advantages of less pollution, high extraction efficiency and less usage of organic solvents.

The invention discloses a deoxy-podophyllotoxin type compound, and a preparation method and a use of the compound. The structural formula of the compound is as shown in formula I, and a substituting group NR1R2 in the formula I is a piperazine type compound as shown in formula II, or the NR1R2 is an amino acid amide type compound as shown in formula III. The compound of the invention can be applied in the preparation of anti-tumor medicaments. The formula I, the formula II and the formula III are as follows.

An application of the solid liposome nanoparticles as the carrier of podophyllotoxin and its derivative and a composite medicine containing podophyllotoxin or its derivative and said solid liposome nanoparticles as carrier are disclosed. Its advantages are higher curative effect, high stability and low cost.

The invention discloses a podophyllotoxin preparation formula for external use for the treatment of condyloma acuminatum and genital herpes, a series of formulations and a preparation method, and belongs to the field of pharmacy. The weights or the volumes of all the ingredients of the formula of 100ml of the podophyllotoxin preparation for external use are as follows: 0.5g of podophyllotoxin, 20ml-80ml of main solvent, 1ml-3ml of penetration enhancer 1, 0.5g-2.5g of penetration enhancer 2, 20ml-80ml of cosolvent and 0.03-0.5g of preservative. The podophyllotoxin preparation for external use has the advantages that the types and the amount of excipients and the proportion of main drugs are reasonable, the drug administration is carried out by a liniment, a spray or other formulations which are applicable to the external use, the main drug can be rapidly absorbed by the horny layer and the epidermis, the efficacy is significant, the local toxicity or side effects are small, the skin acute toxicity is very low, and the podophyllotoxin preparation has no irritation and weak allergy and does not hinder the skin normal functions; the podophyllotoxin preparation has no systemic toxicity or side effects, thereby being safe and effective. The preparation prepared by the formula has the advantages of good appearance, moderate viscosity, easy coating, spraying drug administration, feasible process, controllable quality, simple preparation process, and suitability for industrial batch production.

The invention relates to the field of natural drugs and chemical drugs, in particular to a manufacturing method for deoxypodophyllotoxin. The manufacturing method provided by the invention has the characteristics that the deoxypodophyllotoxin can be obtained through the reaction of podophyllotoxin with NaBH4 and CF3COOH, namely, podophylotoxin is reduced to deoxypodophyllotoxin by addition of with a reducing reagent and protonic acid. According to the invention, the applied materials have wide source and low price, so that the manufacturing method is applicable in industrial production.

The invention relates to a dysosma versipellis extract, a medicine composite containing the extract as well as a preparation method and application thereof. The dysosma versipellis extract with specific chemical components contains active components, such as general lignans, general flavones and the like; and the impurities of the extract are reduced, and contents of effective components are high. The dysosma versipellis extract comprises the following components in percentage by weight: 20-50 percent of podophyllotoxin, 3-8 percent of kaempferol and 8-15 percent of general flavones. The dysosma versipellis extract is high in contents of the effective components and low in impurities; and the dysosma versipellis extract or the medicine composite containing the extract is obvious in effect and low in side effects during skin sterilization and treatment in verruca acuminate. Compared with the prior art, the preparation method has the advantages of advanced process, high production, high practicability, relatively low cost and low environment pollution.

The present invention provides genetic engineering technological process of transforming Tibetan Dysosma versipellis to obtain hairy roots of Tibetan Dysosma versipellis for producing podophyllotoxin. The technological process includes genetic transformation of rooting agrobacterium to Tibetan Dysosma versipellis to obtain hairy roots of Tibetan Dysosma versipellis. The hairy roots of Tibetan Dysosma versipellis is, molecular detection shows, genetically transformed hairy roots, and may be, HPLC detection shows, used in producing podophyllotoxin. The present invention provides one new way of producing podophyllotoxin.

The invention discloses a series of new 2beta-chloropodophyllotoxin aromatic acid ester compounds, a preparation method and application in preparing botanical pesticide by using the compounds. Chemical general formulas of the 2beta-chloropodophyllotoxin aromatic acid ester compounds are as figures. The series of compounds are prepared by using podophyllotoxin as a raw material, the material is prepared into 2beta-chloropodophyllotoxin through C-4 site hydroxy group protection, C-2 site beta-chloro substitution and C-4 site protection removal, and then the 2beta-chloropodophyllotoxin reacts with eight aromatic acids to form the 2beta-chloropodophyllotoxin aromatic acid ester compounds. Proved by experiments, the 2beta-chloropodophyllotoxin aromatic acid ester compounds of the invention have good insecticidal activities which are partially higher than that of podophyllotoxin, and the insecticidal activities of some compounds are higher than those of the prior commercial botanical pesticide toosendanin; and proved by the experiments, the compounds can be used for preparing the botanical pesticide with high efficiency and low toxicity.

The invention relates to the multi-drug resistance (MDR) of Lapatinib (formula 1) in reversing tumour cells which are mediated by membrane transport proteins (ABC) families such as P-glycoprotein (P-gp), multi-drug resistance related protein (MRP1), breast cancer multi-drug resistance related proteins (ABCG2 and BCRP) and the like. The Lapatinib is used together with anti-cancer drugs such as anthracyclines, catharanthines, taxols, podophyllotoxins, camptothecins and the like to restore the sensitivity of MDR tumor cells to the anticancer drugs. The Lapatinib is applied to combination chemotherapy of drug-resistant patients in clinical chemotherapy or the prevention of drug-resistance generation for the tumor cells.

An insecticide in the form of microemulsion is prepared from the sand-land cypress' extract containing podophyllotoxin, emulsifier, antifreezing agent and water through adding emulsifier to said extract, high-speed stirring while adding others, and stirring while heating at 70-80 deg.C. Its advantages are high effect and high safety.

In this invention, aminoic potassium salt reacts with N1-bromoalkyl 5-Fu, under the protection of N, to produce L-aminoic 5-Fu alcoholate type compound. Said compound is then reacting with 4 beta-Br-4-deoxy-4-demethylepipodophyllum which being produced from podophyllo to obtain 4 beta-4-deoxy-nitrogen substituted aminoic 5 Fu ester-4-demethyl epipodophyllum. This invention compound is used for preparing anti-tumor medicine.