37 results about "Selective cytotoxicity" patented technology

Immunoconjugates comprising a targeting agent selectively targeting cell-surface expressed syndecan-1 and at least one effector molecule as well as in vitro and in vivo methods of using those immunocomjugates are disclosed. The effector molecule may have, in its native form, high non-selective cytotoxicity, but substantially no non-selective cytotoxicity when part of said immunoconjugate. Targeting agents include the antibody B-B4 as well as other agents that bind cell-surface expressed syndecan-1.

Disclosed herein are angiogenesis inhibitors represented by formula (I) or formula (II): The variables for formulas (I) and (II) are defined herein.

Immunoconjugates comprising a targeting agent selectively targeting cell-surface expressed syndecan-1 and at least one effector molecule as well as in vitro and in vivo methods of using those immunocomjugates are disclosed. The effector molecule may have, in its native form, high non-selective cytotoxicity, but substantially no non-selective cytotoxicity when part of said immunoconjugate. Targeting agents include the antibody B-B4 as well as other agents that bind cell-surface expressed syndecan-1.

Enhancers which preferentially increase the transcription of cis-linked coding sequences in prostate cells are provided. Methods of using DNA constructs comprising the enhancers to control transcription of heterologous polynucleotides are also provided. Delivery vehicles comprising the enhancers and methods of using the vehicles are also provided. Adenovirus vectors in which one or more genes are under transcriptional control of the enhancers of the invention are also provided. Further provided are methods of using the adenovirus vectors of the invention to confer selective cytotoxicity in mammalian cells.

The invention provides bispecific antibodies with selective cytotoxicity against malignant B-cells. The bispecific antibodies bind to an effector cell antigen and to a 28 / 32 kDa heterodimeric protein on the surface of malignant B-cells. The invention also includes the monospecific components of the bispecific antibodies, humanized versions thereof, and humanized bispecific antibodies. The invention further provides therapeutic and diagnostic methods employing these antibodies.

The invention herein describes a procedure for organically extracting the lipophilic components from plants of the Family Euphorbaciae, specifically but not limited to the genus Croton. The extraction (CGO 110), is deplete of the normal proanthocyanidin content found in the parent material, yet retains its pharmacocological abilities and unlike the parent material, is selectively cytotoxic to cancer cells. The depletion of the proanthocyanidin components makes the product more amenable to preparations for the benefit of ameliorating both human and animal disease.

The present invention relates to a pharmaceutical composition comprising mono- meric alpha-lactalbumin complex, preferably LAC, which is an active complex of alpha-lactalbumin and a fatty acid or lipid with selective cytotoxic activity. The composition of the invention comprises insignificant amounts of oligomeric / multi- meric alpha-lactalbumin complex, preferably LAC. Based on the selective cyto- toxicity of the alpha-lactalbumin complex, preferably LAC composition such compositions are suitable for use in the manufacture of medicaments for use in therapy. Medicaments, comprising monomeric LAC are for use in the treatment of bacterial and viral infections and in particular cancer due to the selective cytotoxic activity. The application further relates to methods of producing a composition comprising monomeric alpha-lactalbumin complex, preferably LAC with cytotoxic activity.

The present invention relates to a pharmaceutical composition comprising monomeric alpha-lactalbumin complex, preferably LAC, which is an active complex of alpha-lactalbumin and a fatty acid or lipid with selective cytotoxic activity. The composition of the invention comprises insignificant amounts of oligomeric / multimeric alpha-lactalbumin complex, preferably LAC. Based on the selective cytotoxicity of the alpha-lactalbumin complex, preferably LAC composition such compositions are suitable for use in the manufacture of medicaments for use in therapy. Medicaments, comprising monomeric LAC are for use in the treatment of bacterial and viral infections and in particular cancer due to the selective cytotoxic activity. The application further relates to methods of producing a composition comprising monomeric alpha-lactalbumin complex, preferably LAC with cytotoxic activity.

The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.

The presently claimed subject matter provides conditionally replication competent adenoviral vectors that confer selective cytotoxicity on cells expressing HIF-1 by infecting cells that allow HIF-1 inducible promoters present within the vectors to function. Also provided are compositions and host cells based upon the vectors, as well as methods of propagating and using the vectors. The presently claimed subject matter further provides a method of inhibiting tumor growth by co-infecting cells in a tumor with a conditionally replication competent adenovirus vector in conjunction with a replication deficient adenovirus vector.

The present invention relates to fluoro sugar and other sugar derivatives of indolopyrrolocarbazoles, their salts and hydrates, which exhibit selective topoisomerase I (topo I) activity, are useful in inhibiting the proliferation of tumor cells and exhibit an antitumor effect, as well as processes for their preparation.

Folate modified cholesterol-bearing pullulan (FA-CHP) was synthesized by the reaction of folic acid γ-2-aminoethylamide and 4-nitorophenyl chloroformate-activated cholesterol-bearing pullulan, wherein folate and pullulan are connected through a NH—CH2—CH2—NH group. Approximately 0.5-1 folates are connected per about 100 glycoside units of pullulan. Then, several combinations of FA-CHP, cholesterol-bearing pullulan (CHP) and doxorubicin (DOX) mixture were tested for cancer selective cytotoxicity. A mixture of FA-CHP, CHP and DOX of 1:4:0.02 (weight ratio) gave sharp and selective damage to cells of a human epidermoid cancer KB known as expressing a high level of folate receptor. The same mixture inhibited the growth of HuH7 cells, which is a human hepatocellular carcinoma and is unknown as a folate receptor.

The presently claimed subject matter provides conditionally replication competent adenoviral vectors that confer selective cytotoxicity on cells expressing HIF-1 by infecting cells that allow HIF-1 inducible promoters present within the vectors to function. Also provided are compositions and host cells based upon the vectors, as well as methods of propagating and using the vectors. The presently claimed subject matter further provides a method of inhibiting tumor growth by co-infecting cells in a tumor with a conditionally replication competent adenovirus vector in conjunction with a replication deficient adenovirus vector.

Immunoconjugates comprising a targeting agent selectively targeting cell-surface expressed syndecan-1 and at least one effector molecule as well as in vitro and in vivo methods of using those immunocomjugates are disclosed. The effector molecule may have, in its native form, high non-selective cytotoxicity, but substantially no non-selective cytotoxicity when part of said immunoconjugate. Targeting agents include the antibody B-B4 as well as other agents that bind cell-surface expressed syndecan-1.

This invention encompasses an expeditious method and compositions that have been found to show selective cytotoxicity against several different cancer cell lines. for treating a wide variety cancer neoplasms that have tumor microenvironments by administering a stand-alone anti-tumor chemotherapeutic composition or administered as an adjunct with chemotherapy and / or radiotherapy with enhanced tumor site affinity that preferentially elevates the pH at the tumor site to suppress and eliminates the acidic tumor microenvironment, administered as chemosensitizing and / or radiosensitizers enhancing the tumor, suppression, remission and inhibit tumor metastisis. The invention encompasses controlling mechanisms of intracellular and extracellular ionic physiology through the administration of alkali salts for pH modulating and for restoring and enhancing ionic physiology. The compositions are useful in effective treatment of cancers, particularly malignant melanomas and squamous cell carcinomas (SCCs), thereby inhibiting angiogenesis, reducing metastatic proliferation, supressing tumor generated induced acidotic pain.

The invention discloses a hybrid subtype tumor targeted nano-micelle and a purpose thereof. The micelle is obtained through mixing and self assembly of a polymer 1 and a polymer 2, wherein the hydrophilic ends of the polymer 1 and the polymer 2 are respectively L-valine-L-valine dipeptide and raloxifene-modified polyethyleneglycol embedding sections; the hydrophobic end is polymer histidine or polymer lactamine. The micelle belongs to a kind of nano-micelle based on PepT1 and ER as the target, and can coat hydrophobic anti-tumor medicine; in-vitro study shows that the stability of the micelle is obviously superior to non-hybrid micelle; meanwhile, the type of nano-micelle medication system can be selectively taken by PepT1 and ER high-expression tumor cells; the tumor cells shows selective cell toxicity, and can be applied to preparation of tumor targeted treatment medicine.

The invention relates to an antitumor composition based on hydrophobized hyaluronan and inorganic nanoparticles stabilized by oleic acid. The hydrophobized hyaluronan in the form of an acylated hyaluronan serves in the composition as a carrier of inorganic nanoparticles. Out of the group of inorganic nanoparticles, the composition may comprise superparamagnetic nanoparticles, nanoparticles of ZnO and moreover, upconversion nanoparticles. Said composition is selectively cytotoxic with respect to both suspension and adherent tumor cell lines, especially with respect to tumor cell lines of colorectum carcinoma and adenocarcinoma, lung carcinoma, hepatocellular carcinoma and breast adenocarcinoma. The highest cytotoxic effects were observed in case of the composition based on an oleyl derivative of hyaluronan with SPIONs. The composition of acylated hyaluronan with SPIONs may also be advantageously used for an in vivo detection of accumulation of the composition in the body, preferably in a tumor or in liver. Said composition is sterilizable in the final package.

The invention provides a mica two-dimensional nanosheet as a drug carrier, and a preparation method of a mica two-dimensional nanosheet drug carrier containing a drug component. The low long-term toxicity, good biocompatibility and good biodegradability of mica are used, so that the mica two-dimensional nanosheet drug carrier containing a drug component can reduce multidrug resistance and systemictoxicity, and has pH-responsive drug release and selective cytotoxicity. Compared with a non-exfoliated mica powder, the mica two-dimensional nanosheet drug carrier containing a drug component has asmaller particle size, and is more easily swallowed by tumor cells.

To conduct a search for natural drugs and their formulae derived from natural substances that hardly cause side effects and drug tolerance, based on quite a new idea having departed from conventional drugs such as Chinese galenicals, Chinese medicine formulae, etc. and to develop a composition that has an anticancer activity and is selectively cytotoxic to cancer cells. A composition having an anticancer effect is obtained, which comprises therapeutically effective amounts of a dry product of Angelica keiskei and a dry product of Theaceae Camellia. Also, a composition having an anticancer activity is obtained, which comprises therapeutically effective amounts of a dry product of Angelica keiskei and / or a dry product of Theaceae Camellia together with a dry product of defatted whole egg of eggs of a fowl bred by feeding a feed having blended therein an additive comprising a dry product of Angelica keiskei, a dry product of brown algae, and optionally a dry product of Theaceae Camellia.

The invention discloses a rana chensinensis functional gene Rd-RNase3 sequence which is characterized by being a nucleotide sequence shown in a sequence table SEQ ID No.1. In the invention, a tumor cell agglutination mediated by the rana chensinensis ribonuclease is not relevant to the selective cytotoxicity of tumor cells and the existence of the wild-type p53 tumor restraint substance, cannot produce gene mutation, and has better stability compared with the prior art. Long-term tumor restraint experiment proves that the Rd-RNase3 gene recombination fusion protein of the invention has strong cytotoxicity on the tumor cells under extremely low concentration, but has no cytotoxicity on normal cells, and thereby having the great advantage on preparing antitumor drugs compared with the existing gene drugs.

The invention provides application of bis-imidazolium salt and a drug loading system as an anticancer preparation and the anticancer preparation, and relates to the technical field of anticancer drugs. The invention provides the bis-imidazolium salt C20 / C22 as a glycosyl transferase inhibitor and the drug loading system containing the bis-imidazolium salt C20 / C22, and researches the selective cytotoxicity of the bis-imidazolium salt C20 / C22 on a human umbilical vein endothelial cell (HUVEC) lines and a series of cancer cell lines; and results show that the C20 / C22 and the drug loading system containing the C20 / C22 have clinical potential as the novel anticancer preparation, and are worthy of further development as an auxiliary anticancer drug.

The invention discloses a hybrid subtype tumor targeted nano-micelle and a purpose thereof. The micelle is obtained through mixing and self assembly of a polymer 1 and a polymer 2, wherein the hydrophilic ends of the polymer 1 and the polymer 2 are respectively L-valine-L-valine dipeptide and raloxifene-modified polyethyleneglycol embedding sections; the hydrophobic end is polymer histidine or polymer lactamine. The micelle belongs to a kind of nano-micelle based on PepT1 and ER as the target, and can coat hydrophobic anti-tumor medicine; in-vitro study shows that the stability of the micelle is obviously superior to non-hybrid micelle; meanwhile, the type of nano-micelle medication system can be selectively taken by PepT1 and ER high-expression tumor cells; the tumor cells shows selective cell toxicity, and can be applied to preparation of tumor targeted treatment medicine.

A method of using 1,2,4-benzotriazine oxides, some of which are novel compounds, as radiosensitizers and selective cytotoxic agents is disclosed. These compounds are shown to specifically radiosensitize hypoxic tumor cells. Some are additionally disclosed to be useful as specific cytotoxic agents for these cells. They also show an unexpected ability to radiosensitize aerobic cells following or preceding a hypoxic incubation of the cells with the drug. This provides a basis for selective radiosensitization of tumors compared to normal cells. A novel method for preparing the 1,2,4-benzotriazine oxides is also disclosed.

The present disclosure is directed to pyridinone derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV nave cells, and for the treatment of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).

This invention belongs to the chemical-pharmaceutical field. New compounds of pterocarpanquinone family presented in formula (I) according to this invention are capable to be activated by reduction generating alkylating species intracellularly. It presents selective cytotoxic effects particularly on mammalian human and nonhuman cells that divide constantly and are useful in treating diseases and dysfunctions related to the phenomenon of undesired cell proliferation. Such compounds are also effective for the treatment of diseases or dysfunctions related to high levels of TNF-α in human and nonhuman mammals.

A substituted benzene propylene derivative and the salt are provided, which is that the phenylacrylate substituted by the corresponding group gains the correspondingly substituted phenylallyl compound through the deoxidization of the lithium aluminium hydride and the aluminium trichloride compound. The invention has certain selective cytotoxicity activeness compound from the natural erucic based alcohol compound and has low toxic effect on the normal cells, while the compounds reconstructed by structure and the important midbodies all have better cytotoxicity activeness and can be prepared in the drugs preventing and curing the tumor diseases. The prepared drugs contain the drug excipients or carriers allowed by the preparation. The drug preparation is in a form of liquid, solid, aerial fog spray, drop, gelatin pearl, nano, controlled release and sustained-release preparation. The compound related to by the invention has simple synthetic method and lower cost, therefore having feasible marketalization prospect. The invention has the above general formula.

This invention belongs to the chemical-pharmaceutical field. New compounds of pterocarpanquinone family presented in formula (I) according to this invention are capable to be activated by reduction generating alkylating species intracellularly. It presents selective cytotoxic effects particularly on mammalian human and nonhuman cells that divide constantly and are useful in treating diseases and dysfunctions related to the phenomenon of undesired cell proliferation. Such compounds are also effective for the treatment of diseases or dysfunctions related to high levels of TNF-α in human and nonhuman mammals.