79 results about "Epipodophyllotoxin" 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.

The invention discloses a phospholipid complex albumin nanoparticle containing epipodophyllotoxins medicine. The nanoparticle contains a complex formed by epipodophyllotoxins medicine and phospholipid and albumin. The nanoparticle comprises the following raw materials in parts by weight: 1 part of epipodophyllotoxins medicine, 1-50 parts of phospholipid and 2-100 parts of albumin. The phospholipid complex albumin nanoparticle can be used for remarkably reducing the toxicity of the epipodophyllotoxins medicine, especially bone marrow suppression; meanwhile, the phospholipid complex albumin nanoparticle has liver-lung targeting property.

The invention discloses an anticancer 4'-nor-anthricin and a preparation method thereof, and belongs to the field of medicine. The anticancer 4'-nor-anthricin is prepared by the following steps of taking podophyllotoxin as raw material, dissolving the podophyllotoxin in acetic acid in an autoclave, adding a palladium-carbon catalyst, carrying out reaction between the podophyllotoxin and hydrogen at the hydrogen pressure of 1.1-2 and at the temperature of 90-100 DEG C to obtain anthricin, and finally carrying out reaction between the anthricin and hydrogen bromide in an acetic acid solution to obtain the 4'-nor-anthricin. Researches find that the anticancer 4'-nor-anthricin has obvious suppressing and apoptosis inducing functions for the cervical cancer cell Hela and the mice melanoma cell B16; the preparation method of the 4'-nor-anthricin is simple, easy to control, low in cost and high in yield.

The invention relates to improvements in the field of drug delivery. More particularly, the invention relates to polypeptides having a hydrolyzable covalent bond to a therapeutic agent that includes, etoposide, etoposide 4′-dimethylglycine or doxorubicin. These polypeptide conjugates can be used as vectors to transport the podophyllotoxin derivative across the blood brain barrier (BBB) or into particular cell types such as ovary, liver, lung, or kidney. The invention also relates to pharmaceutical compositions that include the compounds of the invention and to uses thereof in methods of treatment.

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.

The invention discloses a 4-sydnone substituted phenyl epipodophyllotoxin derivative and a preparation method and application of compounds thereof. The invention additionally relates to salts formed by physiologically acceptable and chemically formable inorganic acid or organic acid of the compounds. The compounds provided by the invention can be applied to formulas of anti-tumor drugs. The structural general formula of the compounds provided by the invention is as shown by the accompanying drawing.

The invention relates to 4-deoxidized-iso-podophyllotoxin derivatives displayed by formula (1) and the intermediate series of compounds of 4-deoxidized-iso-podophyllotoxin derivatives or the pharmaceutical salt or solvates of the 4-deoxidized-iso-podophyllotoxin derivatives. The invention also relates to the preparation method, the drug combinations, and the pharmaceutical applications of compounds in the formula (1). The compounds possess strong activity in inhibiting tumor cell growth, some of which having stronger cytotoxic activity to human body tumor cell lines in vitro than etoposide, the prior first class anti-tumor drug, thereby the compounds are expected to serve the purpose of such cancer drugs as anti-lung cancer drugs, anti-hepatoma drugs, and anti-cerbical cancer drugs; since the cytotoxicity of the related compounds to KB cells and PC-3 cells is approximate to or equivalent to etoposide, and meanwhile the compounds have strong etoposide to CNE cells, the compounds are expected to used in anti-tumor drugs, such as, anti-oral epithelial carcinoma drugs, nasopharyngeal carcinoma drugs, and prostate cancer drugs.

The invention relates to novel podophyllotoxins compound the use of the compound and the process for preparing the compound.

The invention discloses 2,3,6-trideoxyglycosyl demethylepipodophyllotoxin compound or pharmaceutically acceptable ester thereof. The chemical structural formula of the 2,3,6-trideoxyglycosyl demethylepipodophyllotoxin compound is as shown in the figure I in the specification, wherein R represents C1-C6 alkyl, -OH, -NH2, NO2 and halogen groups. The compound has the advantage of being capable of remarkably improving the cytotoxic activity on human lung cancer cells (A549), human hepatoma cells (HepG2), human cervical cancer cells (HeLa), human neuroblastoma cells (SH-SY5Y) and oral cancer vinblastine-resistant cells (KB-VCR) compared with clinical medication of etoposide and has the potential of being developed into anti-tumor drugs.

The invention relates to a medicine preparation, in particular to a medicine preparation for treating brain diseases. The medicine preparation is prepared from effective components and auxiliary materials. The effective components comprises one or a combination of Eevans blue, adriamycin, camptothecin, paclitaxel, camptothecin with the mass percentage different from the previous camptothecin, podophyllotoxin, echidnotoxin, indomethacin, guaianolide, parthenolide, arglabin, aFGF, BDNF, NGF, EPO, insulin, insulin amyloids, oxytocin or GLP-1. The invention discloses a medicine delivery method for treating brain diseases. The method has the advantages of innovativeness, high efficiency and targeting performance, toxic and side effects are reduced, a blood brain barrier way is not used, the amount of medicine entering the brain is increased, and the brain disease treatment effect is remarkable.

The invention discloses an aspergillus fumigatus which can produce podophyllotoxin, epipodophyllotoxin biglucoside and astragaloside, and application thereof. The aspergillus fumigatus TEQA CGMCC No. 3115 has the function of producing podophyllotoxin, epipodophyllotoxin biglucoside and flavonoids astragaloside which have the physiological property the same as that of Chinese podophyllum root. Theaspergillus fumigatus can be used for preparing podophyllotoxin and astragaloside. The method for preparing podophyllotoxin, epipodophyllotoxin biglucoside and astragaloside has the advantages of simple fermentation conditions, easy bacterium culture and short production period, with potential application for industrialized mass production. Besides, the aspergillus fumigatus provides a new way forresource development of podophyllotoxin and has important meaning to protect ecological diversity of plants.

The invention relates to a combination drug used for killing genitals microorganisms of female Tibetan mastiffs and assisting reproduction. The combination drug contains matrine, podophyllotoxin, berberine, vitamin C, etoposide and antifungal drugs in western medicine.

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 provides a podophyllotoxin lipid derivative, a nano-carrier, a preparation method thereof and an application of the podophyllotoxin lipid derivative and the nano-carrier in tumor treatment. The podophyllotoxin lipid derivative is prepared by adopting a podophyllotoxin drug mother nucleus as a hydrophobic nucleus, linking a micromolecular hydrophilic group on the podophyllotoxin drug mother nucleus to form the podophyllotoxin derivative, and introducing a highly hydrophobic long-chain fat-soluble substance to play a stabilizing role. The podophyllotoxin lipid nano-carriers with different structures can be synthesized by changing the types and sizes of the small molecules and the fat-soluble substances and the feeding ratio of the fat-soluble substances to the podophyllotoxin derivatives. The podophyllotoxin lipid derivative provided by the invention overcomes the limitations of low solubility and toxic and side effects of podophyllotoxin, and meanwhile, the podophyllotoxin lipid nano-carrier prepared by the invention has a lipid bilayer structure and an acid / enzyme sensitive connecting bond, and has the characteristic of regulating PD-L1 expression; therefore, the product has the application of tumor microenvironment response and immune escape prevention, and has a wide application prospect in the fields of chemotherapy and immunotherapy in tumor treatment.

Disclosed is the novel use of some Aza-podophyllotoxin derivatives (AZPs) for modulation of the immune system (immunomodulation), including a method for modulating an immune response comprising administering to a subject an effective amount of at least one Aza-podophyllotoxin derivative of general formula wherein A-ring is selected from the group consisting of 1,3-dioxolane, cyclopentane, 1,4-dioxane, one methoxy, two methoxys, and ethyl; and wherein E-ring is selected from the group consisting of dimethoxyanisole, veratrol, anisole, benzene, syringol, bromobenzene, chlorobenzene, 1,2-dichlorobenzene, 2,3-dimethoxybenzene, 3,4,5-trimethoxybenzene.

The invention relates to a composite material for selectively separating and enriching podophyllotoxin and a preparation method thereof. The preparation method comprises the following steps: adding podophyllotoxin as a template molecule, graphene oxide, modified hydroxy propyl cellulose, a functional monomer, a cross-linking agent and an initiator into a polymerization solvent; then reacting in an inert atmosphere to synthesize a molecularly imprinted polymer, and washing off the template molecule podophyllotoxin to obtain the composite material, wherein the modified hydroxy propyl cellulose is prepared by the following steps: under the catalytic action of triethylamine, modifying hydroxy propyl cellulose by using acryloyl chloride, so as to obtain methacryloyl-hydroxy propyl cellulose containing a carbon-carbon double bond. The composite material prepared by the invention has the advantages of stable selectivity, relatively high extraction efficiency, rapid detection and the like, and can realize selective separation and enrichment of podophyllotoxin in complex samples such as a water sample and the like.