melphalan and Carcinoma--Ehrlich-Tumor

Topics: Animals; Antineoplastic Agents; Beryllium; Busulfan; Carcinoma, Ehrlich Tumor; Cell Nucleolus; Cell Nucleus; Chick Embryo; Chromosomes; Colchicine; Culture Techniques; Deoxyribonucleases; DNA; DNA Replication; DNA, Neoplasm; Fibroblasts; Karyotyping; Melphalan; Mice; Microscopy, Interference; Mitomycins; Mitosis; Nucleoproteins; Photometry; Polyploidy; Ribonucleases; Sulfates

A novel hyaluronic acid-poly(ethylene glycol)-poly(lactide-co-glycolide) (HA-PEG-PLGA) copolymer was synthesized and characterized by infrared and nuclear magnetic resonance spectroscopy. The nanoparticles of doxorubicin (DOX)-loaded HA-PEG-PLGA were prepared and compared with monomethoxy(polyethylene glycol) (MPEG)-PLGA nanoparticles. Nanoparticles were prepared using drug-to-polymer ratios of 1:1 to 1:3. Drug-to-polymer ratio of 1:1 is considered the optimum formulation on the basis of low particle size and high entrapment efficiency. The optimized nanoparticles were characterized for morphology, particle size measurements, differential scanning calorimetry, x-ray diffractometer measurement, drug content, hemolytic toxicity, subacute toxicity, and in vitro DOX release. The in vitro DOX release study was performed at pH 7.4 using a dialysis membrane. HA-PEG-PLGA nanoparticles were able to sustain the release for up to 15 days. The tissue distribution studies were performed with DOX-loaded HA-PEG-PLGA and MPEG-PLGA nanoparticles after intravenous (IV) injection in Ehrlich ascites tumor-bearing mice. The tissue distribution studies showed a higher concentration of DOX in the tumor as compared with MPEG-PLGA nanoparticles. The in vivo tumor inhibition study was also performed after IV injection of DOX-loaded HA-PEG-PLGA nanoparticles up to 15 days. DOX-loaded HA-PEG-PLGA nanoparticles were able to deliver a higher amount of DOX as compared with MPEG-PLGA nanoparticles. The DOX-loaded HA-PEG-PLGA nanoparticles reduced tumor volume significantly as compared with MPEG-PLGA nanoparticles.

Topics: Animals; Carcinoma, Ehrlich Tumor; Chemistry, Pharmaceutical; Delayed-Action Preparations; Diffusion; Doxorubicin; Drug Carriers; Hyaluronic Acid; Immunoglobulin G; Lactic Acid; Materials Testing; Melphalan; Metabolic Clearance Rate; Mice; Mice, Inbred BALB C; Nanoparticles; Particle Size; Polyglycolic Acid; Polylactic Acid-Polyglycolic Acid Copolymer; Polymers; Tissue Distribution

The dipeptide beta-alanyl-melphalan was synthesized and tested for its potential anticancer activity. It is shown to possess considerable toxicity toward Ehrlich ascites tumor cells and 3T3 mouse embryo cells in in vitro toxicity assays and is a potent anticancer agent when used in vivo in traditional phase I chemotherapy assays. The potential role for small peptide transport mechanisms in transportation of anticancer agents is discussed.

Topics: Animals; Antineoplastic Agents; Carcinoma, Ehrlich Tumor; Cell Division; Cell Line; Cell Survival; Dipeptides; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Melphalan; Mice

Antitumor and antimetastatic effects of an official extract of Rhodiola rosea were established in experiments on inbred and noninbred mice and rats with transplantable NK/Ly tumor, Ehrlich's adenocarcinoma, melanoma B16 and Lewis lung carcinoma. Application of the said preparation to sarcolysin-treated animals was followed by an increase in survival.

Topics: Animals; Carcinoma, Ehrlich Tumor; Drug Evaluation, Preclinical; Lymphoma, Non-Hodgkin; Male; Melanoma, Experimental; Melphalan; Mice; Mice, Inbred Strains; Neoplasm Metastasis; Neoplasm Recurrence, Local; Neoplasm Transplantation; Neoplasms, Experimental; Plant Extracts; Rats; Rats, Inbred Strains; Sarcoma 180; Time Factors

Topics: Administration, Oral; Animals; Antineoplastic Agents; Carcinoma, Ehrlich Tumor; Immunoglobulin G; Melphalan; Mice; Mice, Inbred ICR

Topics: Acinetobacter; Amidohydrolases; Animals; Carcinoma, Ehrlich Tumor; Female; Injections, Intraperitoneal; Leukemia P388; Leukemia, Experimental; Melphalan; Mice; Mice, Inbred C57BL; Mice, Inbred DBA

Diazomethyl ketone and chloromethyl ketone analogues prepared from N-tosyl amino acids have been synthesized and tested for antitumor activity in Ehrlich ascites carcinoma and P-388 lymphocytic leukemia screens in mice. The N-tosyl chloromethyl ketone analogues prepared from glycine, L-alanine, beta-alanine, L-valine, and 6-(N-tosyl-amino)caproic acid were the most potent antineoplastic agents in the Ehrlich ascites carcinoma screen. The N-tosyl diazomethyl ketone analogues synthesized from glycine, L-leucine, and L-proline were the most active of this series in the Ehrlich ascites screen, along with 5-keto-1-tosyl-2-(diazoacetyl)pyrrolidine and the diazomethyl ketone analogues prepared from 6-(N-tosylamino)caproic acid. In the P-388 lymphocytic leukemia screen, the N-tosyl chloromethyl ketone prepared from glycine and the compound 5-keto-1-tosyl-2-(diazoacetyl)pyrrolidine were the most active.

Topics: Animals; Antineoplastic Agents; Carcinoma, Ehrlich Tumor; Diazomethane; Ketones; Leukemia P388; Male; Mice; Mice, Inbred DBA; Structure-Activity Relationship; Tosyl Compounds

A series of N-protected cyanomethyl esters of various amino acids was synthesized and tested for antineoplastic and antiinflammatory activity in rodents. Utilizing the L-phenylalanine cyanomethyl ester and varying the N-protecting moiety demonstrated that the N-tosyl and the N-Cbz analogues were the most active against Ehrlich ascites cell proliferation. The N-(carbobenzyloxy)- and N-benzoyl-L-phenylalanine cyanomethyl esters were the most active against carrageenan-induced inflammation. In the N-benzoyl series of cyanomethyl esters, L-alanine, DL-valine, and L-leucine amino acid analogues were the most active against Ehrlich ascites cell proliferation. The glycine and L-alanine analogues possessed the best inhibitor activity in the antiinflammatory screen. The cyanomethyl esters also demonstrated immunosuppressive activity and the ability to suppress the writhing reflex which is associated with inflammatory pain. However, no antipyretic or narcotic analgesic activity was demonstrated by these agents.

Topics: Acetonitriles; Amino Acids; Animals; Anti-Inflammatory Agents, Non-Steroidal; Antineoplastic Agents; Body Temperature; Carcinoma, Ehrlich Tumor; Carrageenan; Esters; Immunosuppressive Agents; Lethal Dose 50; Leukemia P388; Male; Mice; Mice, Inbred DBA; Rats; Reaction Time; Structure-Activity Relationship

Topics: Animals; Antineoplastic Agents; Camptothecin; Carcinoma, Ehrlich Tumor; Cyclophosphamide; Drug Administration Schedule; Melphalan; Mice; Vincristine

A series of N-protected vinyl, 1,2-dihaloethyl, and cyanomethyl esters of phenylalanine was synthesized and these compounds were evaluated for antitumor activity against the growth of Ehrlich ascites carcinoma in CF1 male mice (33 mg/kg/day), Walker 256 carcinosarcoma in Sprague-Dawley male rats (2.5 mg/kg/day), and P388 lymphocytic leukemia in DBA/2 mice (20 mg/kg/day). Structure-activity relationships were evaluated and acute toxicity studies (LD50 determinations) in male CF1 mice were also carried out on selected compounds. Carbobenzoxy-L0phenylalanine vinyl ester (5), N-carbobenzoxy-L-phenylalanine 1,2-dibromoethyl ester (12), and N-carbobenzoxy-L-phenylalanine cyanomethyl ester (8) were found to be very potent inhibitors of Ehrlich ascites tumor growth at nontoxic doses cited above. Compounds 5 and 12 also tripled survival time in the Walker 256 system. LD50 values for compounds 5, 12, and 8 were greater than 2000 mg/kg (greater than 6.15 mmol/kg), 74 mg/kg (0.15 mmol/kg), and 150 mg/kg (0.44 mmol/kg), respectively.

Topics: Acetonitriles; Animals; Antineoplastic Agents; Carcinoma 256, Walker; Carcinoma, Ehrlich Tumor; Lethal Dose 50; Leukemia, Experimental; Male; Mice; Mice, Inbred DBA; Phenylalanine; Rats; Vinyl Compounds

Previously reported work on N-protected activated esters of phenylalanine has been extended to include N-protected vinyl, dibromoethyl, and cyanomethyl esters of several other amino acids. These compounds have been synthesized and evaluated in Ehrlich ascites carcinoma, Walker 256 carcinosarcoma, and and P388 lymphocytic leukemia tests. Among compounds tested were derivatives of tyrosine, tryptophan, glycine, leucine, proline, aspartic acid, glutamic acid, 4-aminobutyric acid, and 6-aminocaproic acid. Compounds of greatest potential interest from this study are N-carbobenzoxyglycine 1,2-dibromoethyl ester and N-carbobenzoxy-L-leucine 1,2-dibromoethyl ester. Both compounds were highly active in Ehrlich ascites test systems (33 mg/kg/day). The glycine derivative was also active in the Walker 256 test (2.5 mg/kg/day. Values for LD50's in mice were 148 mg/kg (0.37 mmol/kg) and 225 mg/kg (0.50 mmol/kg) for glycine and leucine derivatives, respectively; therefore, these compounds do not appear to be toxic at effective dose levels.

Topics: Acetonitriles; Amino Acids; Animals; Antineoplastic Agents; Carcinoma 256, Walker; Carcinoma, Ehrlich Tumor; Lethal Dose 50; Leukemia, Experimental; Mice; Structure-Activity Relationship; Vinyl Compounds

Topics: Animals; Carcinoma, Ehrlich Tumor; Gallbladder; Kidney; Male; Melphalan; Mice; Rats

Topics: Animals; Antineoplastic Agents; Carcinoma 256, Walker; Carcinoma, Ehrlich Tumor; Female; Leukemia, Experimental; Leukocyte Count; Lymphoid Tissue; Male; Mammary Neoplasms, Experimental; Melphalan; Mice; Mice, Inbred C3H; Neoplasm Transplantation; Neoplasms, Experimental; Organ Size; Ovarian Neoplasms; Rats; Sarcoma 180; Sarcoma 37; Sarcoma, Experimental; Spleen; Splenic Neoplasms; Thymus Gland; Thymus Neoplasms; Time Factors; Triazines

Topics: Animals; Carcinoma, Ehrlich Tumor; Deoxyribonucleases; Liver; Lysosomes; Male; Melphalan; Mice; Neoplasm Transplantation; Time Factors; Transplantation, Homologous

Topics: Alkylation; Animals; Carcinoma, Ehrlich Tumor; Cell Nucleolus; DNA, Neoplasm; Female; Hypertrophy; Male; Melphalan; Mice; Microscopy, Electron; Mitosis; Nucleoproteins; Polyploidy

Topics: Animals; Carcinoma 256, Walker; Carcinoma, Ehrlich Tumor; Creatinine; Female; Leukemia L1210; Male; Melanoma; Melphalan; Mice; Mice, Inbred Strains; Neoplasm Transplantation; Neoplasms, Experimental; Rats; Sarcoma 180; Sarcoma, Experimental; Serotonin

Topics: Animals; Carcinoma, Ehrlich Tumor; Cell Count; Cell Line; DNA, Neoplasm; Histocytochemistry; Melphalan; Mice; Mitosis; Neoplasm Transplantation; Polyploidy

Topics: Animals; Carcinoma, Ehrlich Tumor; Male; Melphalan; Mice; Polymers

Topics: Animals; Antineoplastic Agents; Carcinoma, Ehrlich Tumor; Cyclophosphamide; Diet Therapy; Female; Hydrochlorothiazide; Male; Mannomustine; Melphalan; Mice; Phosphines; Rats; Sarcoma 180; Sarcoma, Experimental; Serotonin; Sodium Chloride; Water

Topics: Animals; Carcinoma, Ehrlich Tumor; DNA, Neoplasm; Injections, Intraperitoneal; Melphalan; Mice; Mitosis; Peritoneal Neoplasms; Polyploidy

Topics: Animals; Anti-Bacterial Agents; Antibiotics, Antineoplastic; Antifungal Agents; Antiviral Agents; Ascites; Carcinoma 256, Walker; Carcinoma, Ehrlich Tumor; Cyclophosphamide; Depression, Chemical; Injections, Intraperitoneal; Injections, Subcutaneous; Leukemia, Experimental; Mechlorethamine; Melphalan; Mice; Neoplasms, Experimental; Nitrogen Mustard Compounds; Rats; Sarcoma; Sarcoma 180; Thiotepa; Uracil

Topics: Animals; Carcinoma 256, Walker; Carcinoma, Ehrlich Tumor; Female; Leukopenia; Lung Neoplasms; Lymphoma, Non-Hodgkin; Melphalan; Mice; Neoplasm Metastasis; Ovarian Neoplasms; Peritoneal Neoplasms; Rats; Sarcoma 180; Sarcoma, Experimental; Thiotepa; Triazines

Topics: Animals; Carcinoma, Ehrlich Tumor; Cell Line; DNA; Melphalan; Methods; Mice; Photometry

Topics: Animals; Carcinoma, Ehrlich Tumor; DNA Replication; DNA, Neoplasm; Female; Leukocytes; Melphalan; Mice; Mitosis; Photometry; Staining and Labeling; Time Factors

Topics: Animals; Carcinoma, Ehrlich Tumor; Melphalan; Mice; Mitosis; Neoplasm Transplantation; Time Factors; Transplantation, Homologous

Topics: Animals; Antineoplastic Agents; Carcinoma, Ehrlich Tumor; Female; Fluorouracil; In Vitro Techniques; Lymphoma, Non-Hodgkin; Melphalan; Mice; Neoplasms, Experimental; Ovarian Neoplasms; Rats; Thiotepa

Topics: Animals; Carcinoma, Ehrlich Tumor; Male; Melphalan; Mice; Neoplasms, Experimental; Polymers; Sarcoma 180; Sarcoma 37

Topics: Animals; Carcinoma, Ehrlich Tumor; Cell Membrane Permeability; Centrifugation, Density Gradient; DNA, Neoplasm; In Vitro Techniques; Injections, Intraperitoneal; Mechlorethamine; Melphalan; Mice; Protein Binding; Thymidine; Time Factors; Tritium

Topics: Animals; Beryllium; Busulfan; Carcinoma, Ehrlich Tumor; Cell Nucleolus; Cell Nucleus; Chick Embryo; Chromosomes; Colchicine; Culture Techniques; Deoxyribonucleases; DNA; DNA, Neoplasm; Embryo, Mammalian; Fibroblasts; Histocytochemistry; Melphalan; Mice; Microscopy, Interference; Mitomycins; Mitosis; Neoplasm Proteins; Nucleoproteins; Photometry; Rats; Ribonucleases

Topics: Animals; Antineoplastic Agents; Ascites; Carcinoma, Ehrlich Tumor; Cyclophosphamide; Electronics, Medical; Mannomustine; Melphalan; Mercaptopurine; Methods; Mice; Sarcoma 180

Topics: Alkylating Agents; Animals; Carcinoma, Ehrlich Tumor; Histamine H1 Antagonists; Mechlorethamine; Melphalan; Methyldopa; Methysergide; Mice

Topics: Animals; Antibiotics, Antineoplastic; Antineoplastic Agents; Busulfan; Carcinoma, Ehrlich Tumor; Fluorouracil; Mechlorethamine; Melphalan; Mercaptopurine; Mice; Nitrogen Mustard Compounds; Uracil

Topics: Animals; Carcinoma, Ehrlich Tumor; Lymphoma; Melphalan; Mice; Neoplasms, Experimental; Nitrogen Mustard Compounds; Sarcoma 180

Topics: Animals; Antineoplastic Agents; Carcinoma, Ehrlich Tumor; Colchicine; Mathematics; Melphalan; Mice; Mitosis; Phenols; Thiotepa

Topics: Animals; Carcinoma, Ehrlich Tumor; Diploidy; Electrophoresis; Melphalan; Mice; Research

Topics: Animals; Carcinoma, Ehrlich Tumor; Glycolysis; In Vitro Techniques; Melphalan; Mice

Topics: Amines; Animals; Antimetabolites; Ascites; Carcinoma; Carcinoma, Ehrlich Tumor; Gallic Acid; Hydrolyzable Tannins; Melphalan; Pharmacology; Protein Biosynthesis; Proteins; Research; Thiotepa

Topics: Animals; Antineoplastic Agents; Carcinoma 256, Walker; Carcinoma, Ehrlich Tumor; Carcinoma, Krebs 2; Feeding and Eating Disorders; Leukopenia; Melanoma; Melphalan; Neoplasms; Neoplasms, Experimental; Pharmacology; Research; Sarcoma; Sarcoma, Experimental

Topics: Animals; Antineoplastic Agents; Carcinoma, Ehrlich Tumor; Cyclophosphamide; Fluorouracil; Melphalan; Mice; Mitomycin; Mitomycins; Nitrogen Mustard Compounds; Pharmacology; Research; Sarcoma 180; Serotonin; Toxicology; Triethylenemelamine

Topics: Adenine Nucleotides; Adenosine Triphosphate; Animals; Carbohydrate Metabolism; Carcinoma; Carcinoma, Ehrlich Tumor; Female; Glucose; Humans; Melphalan; Metabolism; Ovarian Neoplasms; Oxidative Phosphorylation; Peptides; Pharmacology; Phosphorylation; Research; Sarcoma; Sarcoma, Experimental; Toxicology

Topics: Animals; Autoradiography; Carbon Isotopes; Carcinoma, Ehrlich Tumor; Chloramphenicol; Culture Media; DNA; DNA, Neoplasm; Female; Humans; Melphalan; Ovarian Neoplasms; Pharmacology; Phenylalanine; Proteins; Research; RNA; RNA, Neoplasm; Sarcoma; Sarcoma, Experimental

Topics: Amino Acids; Animals; Antineoplastic Agents; Carcinoma, Brown-Pearce; Carcinoma, Ehrlich Tumor; Glycine; Histocytochemistry; In Vitro Techniques; Lysine; Melphalan; Methionine; Mice; Neoplasm Proteins; Pharmacology; Proteins; Rabbits; Research; Sarcoma; Sarcoma, Experimental; Thiotepa; Tyrosine

Topics: Animals; Carcinoma, Ehrlich Tumor; DNA; DNA, Neoplasm; Melphalan; Metabolism; Mice; Neoplasm Transplantation; Neoplasms; Pharmacology; Phosphorus Isotopes; Rats; Research; RNA; RNA, Neoplasm; Sarcoma; Sarcoma, Yoshida

Topics: Animals; Carcinoma; Carcinoma, Ehrlich Tumor; Cyclophosphamide; Cytostatic Agents; Mannomustine; Mechlorethamine; Melphalan; Metabolism; Mice; Neoplasms; Neoplasms, Experimental; Nitrogen Mustard Compounds; Phosphorus Isotopes; Radiation Injuries; Radiation Injuries, Experimental; Research; Triethylenemelamine