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204 results about "Drug toxicity" patented technology

Definition. Drug toxicity refers to the level of damage that a compound can cause to an organism. The toxic effects of a drug are dose-dependent and can affect an entire system as in the CNS or a specific organ such as the liver. Drug toxicity usually occurs at doses that exceed the therapeutic efficacy of a drug; however,...

Application of cycloastragenol in delaying cell senescence and increasing passage times of cell senescence

PendingCN119082004Aanti agingReduce the number of passagesAntinoxious agentsSkeletal/connective tissue cellsTelomeraseDecreased telomerase activity
The invention relates to the technical field of biology, in particular to application of cycloastragenol in delaying cell senescence and increasing passage times of the cell senescence, and the cycloastragenol can delay the cell senescence and increase the passage times of the cell senescence by improving the relative telomerase activity of the cell. Cell experiments prove that the natural telomerase activator cycloastragenol used in the invention has no toxic or side effect on cells under the conditions of low-concentration (25-100 [mu] M) and short-time (12-24 h) incubation. Finally, a culture scheme of cycloastragenol is determined through drug toxicity and anti-aging tests: P3 and P6 generation cells are cultured for 24 hours by using 100 [mu] M cycloastragenol, P9 generation cells are cultured for 12 hours by using 100 [mu] M cycloastragenol, and under the culture condition, the relative telomerase activity of the cells can be remarkably improved, the aging level of the cells can be delayed, and the passage frequency of the cells can be remarkably prolonged.
Owner:CHONGQING ACAD OF ANIMAL SCI

Magnetic nanoparticles and methods of drug release

Described herein are compositions, systems, and methods for targeted and controlled drug release. In some embodiments, the compositions, systems, and methods may comprise magnetoelectric silica nanoparticles for targeted and controlled release of chemotherapeutic drugs for cancer treatment. In some embodiments, an external magnetic field may be used to release one or more drugs from the magnetoelectric silica nanoparticles. The disclosed compositions, systems, and methods may improve drug targeting and reduce systemic drug toxicity.
Owner:UNIV OF NOTRE DAME DU LAC

Composite hydrogel targeting macrophage mitochondria as well as preparation method and application of composite hydrogel

The invention relates to the field of nano drug delivery systems, in particular to composite hydrogel targeting macrophage mitochondria as well as a preparation method and application of the composite hydrogel. The ROS response type liposome composite injectable hydrogel targeting the macrophage mitochondria is prepared by compounding the cationic liposome and the hydrogel, can be used as a nano drug delivery system suitable for oral local drug delivery, has good biocompatibility, and can target the mitochondria. The composite hydrogel is easy to prepare, easy to administrate and high in viscosity, has the characteristics of continuous drug release mode, minimum dosage frequency, low drug toxicity and the like, and is beneficial to being widely applied to treatment of periodontitis related diseases.
Owner:THE AFFILIATED STOMATOLOGICAL HOSPITAL OF KUNMING MEDICAL UNIV

Evaluation method for testing toxic and side effects of medicine through biological organ model

The invention relates to the technical field of drug toxicity evaluation, in particular to an evaluation method for examining toxic and side effects of drugs through a biological organ model. The method comprises the following steps: pretreating a cell line, and carrying out mixed culture with a skeleton structure; connecting an organ model through a biochip; designing a micro-channel network to form a circulation simulation system, and adjusting micro-environment parameters; embedding a biosensor into the biological organ model, and collecting data; adding drugs with different concentrations, and evaluating according to data. According to the method, firstly, the liver, the kidney and the heart are constructed, then the three organ models are connected through the microfluidic technology, microenvironment factors such as micro blood vessels and lymphatic vessels are introduced into the connecting positions, finally, the biosensor technology is introduced, the cell state, metabolites and microenvironment parameters in all the organ models are monitored in real time, and the three organ models are obtained. Through the multi-dimensional biological organ model, the influence of the medicine on different organs can be evaluated more comprehensively.
Owner:SHENZHEN MINGJIAN TESTING PROFESSIONAL TECH CO LTD

Application of combination of Cd1 and Mdr1 double-target inhibitor and azole drugs in preparation of antifungal drugs

The invention relates to the technical field of biological medicine, in particular to application of a combination of a Cd1 and Mdr1 double-target inhibitor and an azole drug in preparation of an antifungal drug. Based on the fact that the compound as shown in the formula (I) can be used as a CCd1 and Mdr1 double-target inhibitor, the inhibition effect of the compound on candida albicans, candida auricula, candida glabrata, candida tropicalis, trichophyton rubrum and trichophyton indicus when the compound is combined with azole drugs is further evaluated, and the result shows that the compound as shown in the formula (I) has no obvious antibacterial activity on various fungi, and can be used for preparing a medicine for treating various fungi. The drug resistance of CCd1 and Mdr1 overexpression drug-resistant fungi can be reversed, the activity of Candida albicans, Candida auricula, Candida glabrata, Candida tropicalis, Trichophyton rubrum and Trichophyton indicus can be synergistically inhibited when the drug is combined with azole drugs, the treatment dosage of the azole drugs is effectively reduced, and the drug toxicity is small. Therefore, the compound shown in the formula (I) can improve the antifungal effect of azole drugs and reduce the drug resistance of the azole drugs.
Owner:SHANDONG UNIV

Phage lyase and application thereof

The invention discloses a bacteriophage lyase and application thereof, and particularly relates to a bacteriophage lyase with an amino acid sequence as shown in SEQ INNO.2. The bacteriophage lyase can inhibit the growth of escherichia coli, staphylococcus and salmonella, can be used as an antibacterial substance in splitting gram-negative bacteria and can be used for preparing drugs for resisting gram-negative bacteria. The lyase can be used independently or compounded with other substances, the use concentration of antibiotics can be reduced by combining the lyase with the antibiotics, toxic and side effects (such as renal toxicity of polymyxin) of drugs are reduced, and meanwhile, generation of bacterial drug resistance is delayed. After the lyase and the chitosan are combined for use, remarkable antibacterial activity is generated, the antibacterial effect can be achieved without pre-treatment on bacteria, and the practicability is improved.
Owner:GUANGDONG MEDICAL UNIV

Composition for composite hydrogel as well as preparation method and application of composition

The invention provides a composition for composite hydrogel as well as a preparation method and application of the composition. Comprising an ionic compound, methacrylated hyaluronic acid (HAMA), a photoinitiator and a solvent, and the ionic compound comprises one or two of carboxymethyl cellulose and sodium alginate. The ink dots prepared from the composite hydrogel have high adhesion to a substrate, are stable, are not easy to disperse, have high elasticity, and can be used in the aspects of drug screening, drug toxicity and test and the like.
Owner:INST OF CHEM CHINESE ACAD OF SCI

Novel compound rapid surface anesthetic and preparation method thereof

The invention discloses a novel compound rapid surface anesthetic and a preparation method thereof, and belongs to the field of pharmaceutical preparations. According to the anesthetic, core anesthetic components of lidocaine and tetracaine are compounded with propylene glycol-laurocapram synergistic penetration enhancer, menthol auxiliary penetration enhancer, carbomer 980 gel matrix, triethanolamine pH regulator, glycerol humectant, panthenol soothing agent, purified water and the like, a surface smearing agent is prepared through a specific process, and the anesthetic can be administered in combination with an iontophoresis technology. Compared with the existing surface anesthetic for the cosmetic surgery, the surface anesthetic disclosed by the invention solves the problems of slow effect taking and poor effect, can realize rapid penetration of local skin, has short anesthesia effect taking time, long duration and good effect, has no obvious irritation to the skin, has good product stability, can effectively reduce the drug toxicity, and has a good application prospect. The device is suitable for surface anesthesia of non-surgical medical beauty items such as skin beauty, laser treatment and water-light micro-needles.
Owner:AFFILIATED RENHE HOSPITAL OF CHINA THREE GORGES UNIV

Method for evaluating combined toxicity of nano plastic and tamoxifen based on caenorhabditis elegans and method for resisting drug toxicity caused by nano plastic

The invention discloses a method for evaluating combined toxicity of nano plastic and tamoxifen based on caenorhabditis elegans and a method for resisting drug toxicity caused by the nano plastic, a sample to be detected is an NGM solid culture medium of a mixture of the nano plastic and tamoxifen, and the caenorhabditis elegans is inoculated into the sample to be detected. The toxic effect of the joint exposure of the nano plastic and the tamoxifen on nematode movement, nerve, development and reproduction under the actual environment condition can be quickly and accurately evaluated, and a basis is provided for evaluation of human health risks. The invention provides a combined toxicity detection method which is suitable for laboratories, simple and convenient to operate and high in applicability by fully considering the problems that the toxicity is changed due to the chemical effect generated by nano-plastics and medicines and the in-vivo conditions are complicated and are difficult to observe, and provides a combined toxicity detection method which is suitable for laboratories and can be used for detecting the toxicity by supplementing N-acetylcysteine through diet. The effect of N-acetylcysteine in relieving tamoxifen toxicity caused by nano-plastics is further evaluated.
Owner:CHANGZHOU UNIV

Traditional Chinese medicine composition for treating Parkinson's disease and application thereof

The invention relates to the technical field of traditional Chinese medicines, and provides a traditional Chinese medicine composition for treating Parkinson's disease, namely tremor syndrome of traditional Chinese medicine, which comprises the following raw materials by weight: 390-470g of liver calming and wind calming medicine, 140-160g of radix rehmanniae, 280-320g of radix paeoniae alba, 840-960g of first decoction medicine, 390-450g of blood activating and qi regulating and tendon and collateral dredging medicine, and 305-355g of antidote. The traditional Chinese medicine composition has remarkable effects of relaxing tendons and detoxifying, and calming endogenous wind and arresting fibrillation, can play a role in solving the problems of head shaking, limb tremor, muscle stiffness, dyskinesia and the like caused by liver wind internal movement and kidney deficiency and toxic damage of Parkinson's disease, and can nourish liver and kidney, relieve tendon and vessel contracture and relieve pain due to the synergistic effect of various traditional Chinese medicinal materials contained in the traditional Chinese medicine composition. The traditional Chinese medicine composition is especially suitable for Parkinson patients with liver-wind internal movement and kidney deficiency and toxicity loss, and can gradually improve the neurotransmitter level in the brain after being taken. The traditional Chinese medicine composition has an outstanding detoxification effect, can effectively remove accumulation of pathological products such as phlegm and blood stasis in the body of the Parkinson's disease patient, prevents phlegm and blood stasis from generating toxins, and can relieve medicine poison generated by long-term medicine taking of the patient.
Owner:SHAANXI UNIV OF CHINESE MEDICINE

Application of ackermania muciniphila composition in preparation of medicine for treating Wilson's disease

InactiveCN119074932ARestoring intestinal microecological imbalancegood curative effectOrganic active ingredientsMetabolism disorderDiseaseEcological environment
The invention discloses an application of an Ackermania muciniphila composition in preparation of a drug for treating Wilson's disease, and relates to the technical field of biological medicines, and the key points of the technical scheme are as follows: Ackermania muciniphila can regulate intestinal flora and micro-ecological environment of WD patients, improve copper expelling and reduce the biological activity and availability of copper absorption drugs, and can be used for preparing a drug for treating Wilson's disease. The drug toxicity is reduced, and adverse events are reduced; therefore, the effects of removing copper, reducing copper absorption medicine and reducing copper accumulation in the body of a WD patient are enhanced. The Ackermania muciniphila can be Ackermania muciniphila viable bacteria, Ackermania muciniphila thermal inactivation thalli or fragments thereof, culture supernatant freeze-dried powder and a composition of the Ackermania muciniphila viable bacteria, the Ackermania muciniphila thermal inactivation thalli or the fragments thereof and the culture supernatant freeze-dried powder. The copper accumulation level in the body of a WD patient is reduced from multiple dimensions, the clinical WD treatment efficiency is improved, meanwhile, the steady-state time of copper in the body of the patient is prolonged, and adverse drug events are reduced.
Owner:ZHEJIANG UNIV

A platform for using iPSC-derived cardiomyocytes carrying gene variants as models of cardiac disease and drug response

The present disclosure is in the field of cardiac disease.For example, the present disclosure provides a new platform that includes iPSC and cardiomyocyte carrying one or more gene mutations, and a model for studying the effect of those gene mutations on cardiomyocyte and on drug toxicity.This platform is herein identified as PREDICT PLATFORM.
Owner:SRI INTERNATIONAL

A processing device for concentrating traditional Chinese medicine and a method of using the same

The invention relates to the technical field of traditional Chinese medicine processing, and in particular to a processing device for concentrating traditional Chinese medicine and a method for using the same. The processing device comprises a processing shell, wherein a screening component for filtering medicinal residues is arranged inside the processing shell, a blocking component for blocking medicinal residues is arranged on a filter plate, a defoaming component for removing floating foam when the medicinal residues are boiled is arranged on the top of a movable column, a starting component for promoting the collection of fine medicinal residues at the bottom of the processing shell is arranged on a first transmission shaft, and two adsorption components for adsorbing the fine medicinal residues at the bottom of the processing shell are arranged inside the processing shell. The invention prevents impurities and pollutants in the medicinal residues from accelerating the degradation and failure of the medicine, reducing the stability of the medicine, and causing the patient to need to take more medicine to achieve the expected therapeutic effect, thereby increasing the economic burden of the patient and the risk of drug toxicity and side effects.
Owner:NO 703 RES INST OF CHINA SHIPBUILDING IND CORP

Application of psoralen A in preparation of medicine for treating vitiligo and system for treating vitiligo

The invention provides application of psoralen A in preparation of a medicine for treating vitiligo and a system for treating vitiligo, and belongs to the technical field of medicines. According to the application of the psoralen A in preparing the medicine for treating the vitiligo, the medicine for treating the vitiligo is prepared by adopting the flavone compound psoralen A, the toxicity is low, and the medicine has a good curative effect on the vitiligo in combination with ultraviolet light (such as UVA).
Owner:SHIHEZI UNIVERSITY

Cellulose copolymer-based hydrogel as well as preparation and application thereof

The invention relates to a cellulose-based hydrogel prepared based on a cellulose copolymer, a cellulose derivative copolymer or a blend thereof, ultramicro fibers of cellulose form a net structure, and the cellulose-based hydrogel has a highly-ordered three-dimensional micro-nano structure, is better in transparency and is more beneficial to observation of a cell state. The cellulose-based hydrogel is suitable for culture of 3D cell culture tissues and organoids, the stem cells cultured by the cellulose-based hydrogel can form cluster culture stem cells and organoids, the operation is simple, compact fused monolayer endoderm cells are formed, non-directional differentiation of the stem cells can be inhibited, and the formed organoids are thick in vesicle wall and are in a solid shape. And the obtained product is a differentiated mature organ and can be used for high-throughput drug screening, drug toxicity testing and regenerative medicine.
Owner:BEIJING GREEN MICRO & NANO TECHNOLOGY CO LTD

Antibody-conjugated drugs of N-oxacycloalkyl-substituted camptothecin derivatives

The present invention relates to an antibody-drug conjugate represented by formula (I) having an oxacycloalkyl-substituted camptothecin derivative as a drug toxic moiety, wherein the definitions of each group in the formula are as described in the specification, and the antibody-drug conjugate has a significant antitumor effect. [Formula 1] JPEG2026502963000098.jpg54170
Owner:HANGZHOU ADCORIS BIOPHARMA CO LTD

Anti-tumor nanoparticles and their preparation method and application

The present invention belongs to the field of biomedical materials and specifically relates to anti-tumor nanoparticles, their preparation methods, and applications. The present invention claims protection for an anti-tumor nanoparticle comprising compound PTe N25, wherein the nanoparticles are simultaneously encapsulated with a camptothecin compound and compound PTe N25 using a phospholipid. The structural formula of compound PTe N25 is: #imgabs0# The present invention utilizes cRGD and camptothecin compounds in conjunction with an organic conjugated polymer material to prepare a dual-targeted chemotherapy-photothermal therapy combined treatment system. This system achieves cRGD-targeted recognition of cancer cells, controlled drug release responsive to spatiotemporal light dual stimulation in the context of a diseased environment, and integrated chemotherapy and photothermal therapy synergistic treatment, significantly reducing drug toxicity and side effects while maintaining anti-tumor efficacy.
Owner:CENT SOUTH UNIV

Drug toxicity detection method based on kidney organoids

The invention discloses a drug toxicity detection method based on kidney organoid. The method comprises the following steps: performing target drug treatment on kidney organoid cultured in advance; determining the estimated toxicity of the target drug based on the morphological difference before and after the drug administration of the kidney organoid; performing cell viability detection on the kidney organoid to obtain the cell viability inhibition ratio of the kidney organoid; and based on the estimated toxicity and the cell activity inhibition ratio, performing molecular pathology detection on the kidney organoid, and determining the real toxicity of the target drug. The toxicity of the target drug is preliminarily estimated according to the morphological difference before and after drug administration of the kidney organoid, then the cell activity inhibition rate of the kidney organoid is obtained, molecular pathology detection is performed on the kidney organoid based on the preliminarily estimated toxicity and the cell activity inhibition rate, and finally the toxicity of the target drug is determined. Through differential gradient classification comparison detection, the toxicity of a target drug is accurately detected.
Owner:SOUTHEAST UNIV NANJING INST OF BIOMATERIALS & MEDICAL DEVICES

ROS (reactive oxygen species) response type nano prodrug based on dynamic differentiation of monocytes as well as preparation method and application of ROS response type nano prodrug

The invention relates to an ROS (reactive oxygen species) response type nano prodrug based on dynamic differentiation of monocytes as well as a preparation method and application of the ROS response type nano prodrug. According to the preparation method, citral and captopril react to form a captopril-citral prodrug molecule (Citopril) through a thioketal bond, and then the prodrug molecule and polyethylene glycol lipid are self-assembled in a water-containing solvent, so that the ROS response type nano prodrug (Citopp-NM) capable of being efficiently taken in by blood monocytes is prepared. According to the nano prodrug, dynamic differentiation of mononuclear cells is fully utilized, a nano drug delivery strategy of the mononuclear cells and the ROS responsive activation characteristic of the nano prodrug are combined, more efficient enrichment of the nano prodrug in AS plaques is achieved, activation of the nano prodrug is controlled through differentiation of the mononuclear cells, and the nano prodrug has a good application prospect. Therefore, distribution and activation of drugs in normal tissues can be reduced, the drug effect is improved, and toxic and side effects of the drugs are reduced.
Owner:GUANGZHOU MEDICAL UNIV

Liver organoid compositions and methods of making and using the same

ActiveJP2024174893AOrganic active ingredientsHepatocytesThyroidFAILURE LIVER
To provide methods of inducing formation of liver organoids from precursor cells, such as iPSC cells, which can be used for screening for a serious adverse event (SAE), such as liver failure and / or drug induced liver injury (DILI), and / or drug toxicity.SOLUTION: This method comprises the steps of a) contacting definitive endoderm (DE) derived from iPSC cells with a FGF pathway activator and a GSK3 inhibitor, for a period of time sufficient to form posterior foregut spheroids, and b) incubating the posterior foregut spheroids obtained in the step a in the presence of retinoic acid (RA) for a period of time sufficient to form the liver organoid.SELECTED DRAWING: Figure 1
Owner:CHILDRENS HOSPITAL MEDICAL CENT CINCINNATI +1

A supramolecular tightening dropsordry containing pelvic floor muscle repair composition and a method for preparing the same

The present application relates to the technical field of health care products, in particular to a pelvic floor muscle repairing composition containing supermolecular tightening Dropsordry and a preparation method thereof, which comprises the following components in mass fraction: 10-14 parts of protein composition, 20-24 parts of chitosan modified Dropsordry, 5-7 parts of freeze-dried powder of Lactobacillus bulgaricus, 10-12 parts of hyaluronic acid, 6-8 parts of glycine and 15-17 parts of proline; each part of the protein composition comprises 20-30 parts of myosin, 30-34 parts of actin, 5-10 parts of hydrolyzed collagen and 240-280 parts of deionized water. The pelvic floor muscle repairing composition can reduce drug toxicity, reduce the amount of drug administration, continuously supplement the required elements of the body during treatment, and quickly relieve the constipation problem caused by the functional damage of the pelvic floor muscle.
Owner:SHENZHEN YUANLINGZHIJI BIOTECHNOLOGY CO LTD

Antigen-binding protein targeting PD-l1 and CD40, preparation therefor, and use thereof

Disclosed are an antigen-binding protein targeting PD-L1 and CD40, preparation therefor, and use thereof. The antigen-binding protein targeting PD-L1 and CD40, by means of blocking a PD-1 / PD-L1 inhibitory signaling pathway, acting on an activated CD40 receptor, and simultaneously activating an antigen-presenting cell and a lymphocyte, achieves a significant synergistic anti-tumor effect; meanwhile, the activation of the antigen-binding protein targeting PD-L1 and CD40 on an immune cell only occurs at a tumor microenvironment site, so that problems of systemic drug toxicity and side effects are significantly solved, which enables the antigen-binding protein targeting PD-L1 and CD40 to exert an excellent anti-tumor efficacy under very safe conditions.
Owner:HARBOUR BIOMED (SHANGHAI) CO LTD

Doxorubicin-loaded anti-tumor hemostatic microspheres and preparation and use thereof

The present application relates to providing a doxorubicin-loaded anti-tumor hemostatic microsphere constructed by a simple, safe and low-cost method and its preparation and application, the doxorubicin-loaded anti-tumor hemostatic microsphere comprises alginate, hemostatic component A, doxorubicin or doxorubicin liposome, crosslinking agent, the hemostatic component A is selected from one or more of carboxymethyl chitosan, hyaluronic acid, collagen, silk fibroin, solve the practical pain point problems such as easy bleeding in tumor resection surgery, large toxicity of chemotherapeutic drugs, large drug dose, frequent drug administration, etc., realize rapid hemostasis in operation, postoperative precise targeted drug delivery, reduce toxic side effects, long-acting drug sustained release, at the same time, all components of the system are safe and reliable, and have good biocompatibility.
Owner:ZHEJIANG SCI-TECH UNIV

Raltitrexed composition and preparation method thereof

The invention relates to the technical field of medicine, and discloses a raltitrexed composition and a preparation method thereof.The raltitrexed composition is prepared by taking a full-biodegradable amphiphilic polymer grafted with hydrophilic chitosan and hydrophobic polylactic acid as a carrier, a raltitrexed drug is embedded in a micelle core of a copolymer by virtue of the large specific surface area and strong adsorption capacity of the carbon nano tube, the targeting function of folic acid and the hydrophobicity of a long chain of polylactic acid under the action of pi-pi action and electrostatic adsorption with the carbon nano tube and chitosan in the composition, so that the encapsulation efficiency is greatly improved; raltitrexed molecules contain elements such as O, N and S, hydrogen bonds can be easily formed by the Raltitrexed molecules and the amphiphilic copolymer, the drug release time can be prolonged through a hydrophobic end polylactic acid side chain, the purpose of slow release is achieved, drug toxicity and adverse reactions are reduced, and the prepared composition is stable in release and ideal in slow release effect.
Owner:HONGGUAN BIO PHARMA CO LTD

Polymer with pH responsiveness and active targeting property as well as preparation method and application thereof

The invention discloses a polymer with pH responsiveness and active targeting as well as a preparation method and application of the polymer. The polymer has the following chemical structural formula: # imgabs0 #, in the formula, the value of n is 37, and the value range of m is 20-43. The polymer not only can realize pH responsiveness and active targeting at the same time, but also has good biocompatibility and biodegradability, can be self-assembled in an aqueous medium to form a polymer micelle with a core-shell structure to be used as a targeting carrier of an antitumor drug, and has excellent drug loading performance. Therefore, the active targeting release of the anti-tumor drug is realized, so that the drug toxicity is reduced, and the targeting treatment effect is improved.
Owner:SHANGHAI UNIV OF ENG SCI

Application of loratadine in preparation of medicine for preventing and treating vascular calcification

The invention relates to an application of loratadine in preparation of drugs for preventing and treating vascular calcification. The structural formula of the loratadine is as follows: # imgabs0. The loratadine used in the invention can significantly reduce the level of mouse aortic vascular calcification, and the experimental result proves that the loratadine has the effects of preventing and treating vascular calcification. The medicine disclosed by the invention is relatively low in toxicity and relatively high in safety.
Owner:HEFEI UNIV OF TECH

Method of using human spheroids for drug discovery

The present invention discloses, in one embodiment, a method of using human induced pluripotent stem cells to generate three-dimensional human organ tissue for therapeutic drug toxicity and discoveryâ‹…. In one embodiment, a high throughput microtiter plate is loaded with both wild type and Rett disease 3D spheroids and exposed to a drug library, and activity is measured and analyzed for disease rescue to wild type cell behavior.
Owner:AXOSIM INC

Near-infrared light activated nitrogen mustard drug compound as well as preparation method and application thereof

The invention discloses a near-infrared light activated nitrogen mustard drug compound as well as a preparation method and application thereof. The structural general formula of the near-infrared light activated nitrogen mustard drug compound is as follows: # imgabs0 #, wherein R1 and R2 are both selected from methyl, ethyl, n-propyl, n-butyl, n-amyl and n-hexyl. The compound reduces the toxic and side effects of nitrogen mustard through a prodrug strategy. According to the compound, the synergistic effect of chemotherapy of nitrogen mustard and photodynamic therapy of the photosensitizer is utilized, and effective inhibition on tumor growth is achieved. Meanwhile, due to the introduction of the photosensitizer, the fluorescence change before and after the nitrogen mustard drug is released is also given, and the visualization of drug release is realized. The compound has wide application prospects in the aspects of drug toxicity reduction and tumor resistance. The preparation method of the near-infrared light activated nitrogen mustard prodrug / drug is simple, raw materials are cheap and easy to obtain, the synthesis process is simple and convenient, separation and purification are easy, and the preparation method is suitable for large-scale production, popularization and application.
Owner:CENT SOUTH UNIV