88results about How to "Low dark toxicity" patented technology

The invention discloses a photosensitizer phospholipid compound, a preparation method of the photosensitizer phospholipid compound, a pharmaceutical composition and application of the photosensitizer phospholipid compound. The pharmaceutical composition is the photosensitizer phospholipid or a combined pharmaceutical composition of the photosensitizer phospholipid and a pharmacologically acceptable carrier, and the pharmaceutical composition is in the form of a liquid preparation, a solid preparation, a semisolid preparation, a capsule, granules, a gel or an injection. The photosensitizer phospholipid compound or a liposome of the photosensitizer phospholipid is applicable to the photodynamic therapy of tumors; the photosensitizer phospholipid compound or the liposome of the photosensitizer phospholipid compound can be rapidly taken by cells and can release a photosensitizer crude drug, and under laser action, the photosensitizer phospholipid compound or the liposome of the photosensitizer phospholipid compound can rapidly release active oxygen to take a strong anti-tumor effect. The photosensitizer phospholipid compound and a liposome nanoparticle thereof can serve as a liquid preparation, a solid preparation, a semisolid preparation, a sterilized preparation and a sterile preparation; and the photosensitizer phospholipid compound and the liposome nanoparticle are low in toxicity and are applicable to the efficient treatment of various tumors.

The invention relates to a tyrosine phthalocyanine derivative which has a structural general formula as the right, in the formula, M is equal to Zn or Al, R is equal to H, Na or CH2CH3. The preparation method for the tyrosine phthalocyanine derivative is: (1) an intermediate II is obtained through the reaction of tyrosine and 4-nitrophthalic nitrile with protected amino group; (2) an intermediate III can be obtained by detracting Boc in the solution of dichloromethane and trifluoroacetic acid; (3) the tyrosine phthalocyanine derivative I can be obtained by cyclizing of the dinitriles intermediate that comprises the tyrosine; wherein, the Boc is di-tert-butyl dicarbonate, a DMF is N, N-dimethylformamide, and a DBU is 1,8-diazacyclo(5,4,0)hendecene-7. The invention also comprises the application of the tyrosine phthalocyanine photosensitizers in preparing photodynamic medicines.

Asymmetrically substituted metal-phthalocyanine compounds are disclosed. These compounds and other phthalo-cyanine-derivatives are used in bioimaging, bioanalysis, FRET and quenching techniques, photodynamic therapy, DNA analysis for cells, proteins, tissues and other biological entities, and other applications. Near-infrared fluorescence minimizes matrix effects typically seen in other methods of analyzing biochemical entities in cells, proteins, tissues and other biological entities.

The invention discloses a preparing method of soluble bamboo bacterioruberin titanium oxide nanometer particle, which comprises the following steps: hydrolyzing organic titanium compound in the alcohol, acetic acid and distilled water; dripping the alcohol solution of bamboo bacterioruberin slowly; stirring; reacting to add the distilled water; adjusting the pH value of the solution to 7. 0; dialyzing to remove alcohol and small molecular compound; freezing; drying; obtaining the product; setting the weight rate of organic titanium compound and acetic acid at 1: 2-6; setting the weight rate of organic titanium compound and alcohol and distilled water at 1: 10-20: 1-3. The bamboo bacterioruberin is the bamboo bacterioruberin methyl, bamboo bacterioruberin ethyl or derivant of two compounds and the organic titanium compound is titanic acid tetraacetate, titanic acid tetra-n-propyl ester, tetraisopropoxy titanium, titanic acid tetera-n-butoyl or polytitanium acid butoyl. The invention has simple, easy and stable operation with diameter of soluble nanometer particle less than 150nm, which is beneficial to prepare and reserve the product.

The invention belongs to the field of heterocyclic compounds and particularly relates to a chlorophyllin salt compound and a preparation method thereof. The chlorophyllin salt compound is a novel photosensitizer which is stable in nature, high in photodynamic activity, low in skin toxicity and controllable in quality and is used for photodynamic treatment of cancers, infections and other diseasesrequired to be treated by optical radiation. In the invention, the substituent of R3 is inform of a carboxylate, so the water solubility is high and the preparation of subsequent medicinal preparations is promoted; the absorption wavelength is more than 650 nanometers; the quantum yield of triplet state and the quantum yield of low singlet oxygen are high; the toxicity in darkness is low, and health of human body can be improved; the selectivity is high; the structure is clear and the performance is stable; and the fat water compatibility is high.

The invention discloses cationic phthalocyanine. A structural formula is shown in the figure. The cationic phthalocyanine derivative disclosed by the invention has good water solubility and low aggregation degree, has good photosensitive activity and antitumor activity, and is applicable to being used as a photosensitizer for diphtheria/pertussis/tetanus (DPT) treatment. The invention also relates to a preparation method and an application of the cationic phthalocyanine.

The invention discloses a novel metal iridium (III) complex. The chemical structural formula of the metal iridium (III) complex is shown in a formula (I); and the metal iridium (III) complex has no toxicity to tumor cells and normal cells in the dark, but has strong growth inhibition ability to the tumor cells under light conditions, has a photo-catalytic oxidation effect on NADH, and is of greatsignificance to the study of a high-efficiency and low-toxicity iridium complex photosensitizer, anti-tumor drugs can further be prepared, and great application prospects are achieved.

The invention discloses a method for preparing a medicament-nanometer calcium phosphate composite system taking a fat soluble photosensitizer as a framework, which comprises the following steps of: under the condition that phosphoryl-containing organic matters exist or do not exist, adding distilled water and aqueous solution of calcium salt, and stirring uniformly to prepare a system A; adding the distilled water and aqueous solution of phosphate, and stirring uniformly to prepare a system B; and adding fat soluble photosensitizer solution into the system A or the system B or adding the fat soluble photosensitizer solution into the systems A and B simultaneously, stirring uniformly, and mixing the system A and the system B to obtain the medicament-nanometer calcium phosphate composite system taking the fat soluble photosensitizer as the framework. The administration system prepared by the method is high in water solubility and dispersibility and can promote the effective transmission of the fat soluble photosensitizer in blood, and the medicine loading rate of the administration system is increased. Simultaneously, the preparation method is simple, easy to operate, high in stability and low in cost. The invention also relates to application of the administration system prepared by the method in the preparation of medicaments for photodynamic therapy.

The invention discloses polyamidoamine-dendrimers (PAMAM-CD)/HP(haematoporphyrin)/ICG(indocyanine green) nanometer medicine with controllable photodynamic treatment effects, and a preparation method thereof. The nanometer medicine is characterized in that the HP and the ICG are coated and loaded into PAMAM-CD; the ICG is used as a switch of the HP; the fluorescence of the HP is quenched by ICG; meanwhile, the photodynamic treatment is switched off. When the nanometer medicine is exposed in 808nm laser, the ICG is decomposed; the HP fluorescence is restored; the photodynamic treatment is opened; meanwhile, the ICG photothermal treatment is accompanied. The medicine solves the problem of dark toxicity of the HP, and also realizes the combination of the controlled photodynamic treatment and the photothermal therapy through the switch effect of the ICG.

The invention relates to a mitochondria-targeting BODIPY compound and a preparation method and application of liposome-coated nanoparticles of the BODIPY compound. The BODIPY compound contains a cationic group which is easily combined with a mitochondrial membrane with negative electricity in cells, so that the BODIPY compound is targeted to mitochondrial organelles of the cells. The BODIPY compound is wrapped by liposome, and liposome nanoparticles with uniform particle size are prepared in an aqueous solution. The nanoparticles have high stability and good biocompatibility in an aqueous solution. After the nanoparticles are taken by tumor cells, the liposome structure is destroyed, and the released BODIPY compound is targeted to cell mitochondria. Besides, under the 665nm illumination condition, active oxygen generated by the BODIPY compound causes oxidative damage to active molecules in mitochondria, so that tumor cells are killed. The liposome nanoparticles can be applied to tumorphotodynamic therapy as a drug for delivering various photosensitizers.

The embodiment of the invention discloses a fullerene phthalocyanine derivative as well as a preparation method and application thereof. The fullerene phthalocyanine derivative has the advantages of novel structure, small possibility of generating photobleaching, light degradation and aggregation, high phototoxicity and low dark toxicity and is more stable under an illumination condition.

The present invention discloses fatty chain end group diamine substituted hypocrellin derivatives, including 2-site amino substituted hypocrellin A, 2-site amino substituted hypocrellin B, and Schiff base formed with hypocrellin A or hypocrellin B with diamine in the site-17. Compared with hypocrellin A and hypocrellin B, the products of the present invention has stronger absorption in phototherapeutic window of 600-900 nm, can produce active oxygen in photosensitive condition, and has powerful photodynamic effect and low dark toxicity. The present invention also discloses the preparation process and the use in preparing medicine for treating cancer and AIDS.

The invention discloses polyamine phthalocyanine and a derivative thereof. The structural general formula of the derivative of polyamine phthalocyanine is shown in descriptions. The derivative of polyamine phthalocyanine, disclosed by the invention, has relatively good solubility and photosensitive activity, has a certain targeting function and is suitable for serving as a photosensitizer for PDT (Photodynamic Therapy). The invention further relates to preparation methods and application of polyamine phthalocyanine and the derivative thereof.

A photosensitizer and derivative, application thereof. The photosensitizer has the structure of general formula I, wherein X is S or Se, Y is organic or inorganic ion, R₁ and R₂ are independently selected from H, alkyl, alkoxy, alkyl amido, alkyl azide and the like; R₃ is selected from H, alkyl, alkoxy, amino sulfonyl, hydroxyl, carboxyl and the like, and L₁ is a linker selected from —(CH₂)_n1— or —(CH₂CH₂O)_n2—. The derivatives are molecular medicines with drug molecules of anticancer and chemotherapy or tumor targeting function connected to the said photosensitizer. The photosensitizer has excellent near infrared characteristics and low dark toxicity and is used in the field of photodynamic tumor therapy. The introduction of benzophenothiazine or benzophenoselenazine into derivatives with tumor-targeting function could improve the specific uptake of photosensitizer in tumor tissues. Moreover, clinical anticancer drugs can be introduced into the structure of benzophenothiazine or benzophenoselenazine to achieve the purpose of combining therapy of photodynamic therapy and chemotherapy.

The invention relates to the technical field of medicine, in particular to a ruthenium coordination compound with near-infrared fluorescence, a preparation method and application thereof. After a chromophore-pyrene is introduced, the coordination compound has obvious phototoxicity (IC50 = 0.040 [mu]M) and small dark toxicity (IC50 = 9.402 [mu]M) when applied to cervical cancer (HeLa cells) under the irradiation of 635 nm red light, the photodynamic therapy index (PI) is 235.05, and the photodynamic therapy has a remarkable curative effect. The ruthenium metal coordination compound can generate singlet oxygen under the irradiation of a 635 nm light source, and can photocatalytically oxidize NADH and NADPH. According to the invention, the ruthenium coordination compound has important significance for promoting the research of a high-efficiency novel anti-tumor ruthenium metal coordination compound photosensitizer, can be further used for preparing anti-tumor drugs, and has a relatively great application prospect.

The invention discloses application of water-soluble porphyrin in preparing photodynamic therapy medicine. The chemical name of water-soluble porphyrin is tetraiodide 5, 10, 15, 20-tetra {4-[2-(1-methyl-1-piperidine)ethyoxyl][phenyl}porphyrin, water-soluble porphyrin (I) has quite strong recognition effect on G-quadruplex and is high in targeting performance when being applied in photodynamic therapy. TMPipEOPP almost has no cutting activity to G-quadruplex in darkness but presents quite high photosensitive cutting activity to G-quadruplex under light by generating 1O2 and .OH. This shows that TMPipEOPP can serve as a PDT photosensitizer of G-quadruplex under physiological conditions. In addition, cytotoxicity experiments show that TMPipEOOP almost has no dark toxicity or is extremely low in dark toxicity but has quite high photoinduced cytotoxicity, and this also shows that TMPipEOOP is a PDT photosensitizer with quite low dark toxicity.

The invention discloses a sorafenib-ruthenium complex as well as a preparation method and application thereof. The sorafenib-ruthenium complex contains cations as shown in a chemical structural formula 1. The preparation method of the sorafenib-ruthenium complex comprises the following steps: dissolving sorafenib and a ruthenium complex in a reaction solvent to prepare a mixed solution; and carrying out a coordination reaction on the mixed solution in a dark and protective atmosphere to generate the sorafenib-ruthenium complex, and the like. The sorafenib-ruthenium complex disclosed by the invention shows low toxicity to Hep-G2 liver tumor cells and normal liver cells in a dark environment; and the toxicity to liver tumor cells is enhanced under the illumination condition, and the compound can be used for photoactivation chemotherapy of tumors and can be applied to preparation of liver cancer targeted drugs.

The invention provides an iridium (III) complex and a preparation method and application thereof. The anti-tumor iridium (III) complex with a structure as shown in a formula (1) or a formula (2) in the invention can specifically target mitochondria or lysosome, has low dark toxicity and high phototoxicity, and has a very high phototoxicity index in tumor cells, particularly in non-small cell lung cancer cells Meanwhile, the anti-tumor metal iridium (III) complex can be used as a photosensitizer to participate in photodynamic therapy. Compared with a traditional photosensitizer, the anti-tumor metal iridium (III) complex has the advantages of being good in water solubility, high in light stability, low in dark toxicity and the like, and can realize integration of diagnosis and treatment.