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Microorganisms Jan 2023Tamarix aphylla is a Saudi herb, which possesses antimicrobial properties and potentially introduces a solution to the subsequent dilemma caused by agrochemicals and...
Tamarix aphylla is a Saudi herb, which possesses antimicrobial properties and potentially introduces a solution to the subsequent dilemma caused by agrochemicals and antifungal misuse. The current study aimed to assess the fungicidal properties of water and ethanolic extracts of T. aphylla leaves against Macrophomina phaseolina, Curvularia spicifera, and Fusarium spp. The chemical composition of T. aphylla was evaluated by gas chromatography/mass spectrometry technique (GC−MS) and Fourier-transform infrared spectroscopy (FTIR). The antifungal assay assessed the fungal growth inhibition using the poisoned food technique. Scanning and transmission electron microscopy (SEM and TEM) were used to evaluate the structural changes induced in the fungal species post-treatment by T. aphylla. FTIR and GC−MS analysis revealed that T. aphylla extracts were rich in aromatic and volatile compounds, such as Benzeneselenol, Gibberellic acid, and Triaziquone, which proved multiple antifungal properties. The results showed significant inhibition in the growth of all species (p < 0.05) except for F. moniliforme, where the water extract induced the highest mycelial growth inhibition at the dose of 30%. The highest inhibition was for M. phaseolina treated with the water extract (36.25 ± 1.06 mm, p < 0.001) and C. spicifera, treated with the ethanolic extract (27.25 ± 1.77 mm, p < 0.05), as compared to the untreated control and the positive control of Ridomol. SEM and TEM revealed some ultrastructural changes within the fungal growth of treated M. phaseolina, which included the thickening and mild rupture of mycelia. Those findings suggested the robust antifungal properties of T. aphylla against some filamentous fungi. The phenolic composition illustrated the potential fungicidal properties of T. aphylla. Additional studies are required to focus on more antimicrobial properties of T. aphylla against other species, particularly those that might benefit the medical field.
PubMed: 36677418
DOI: 10.3390/microorganisms11010127 -
Molecules (Basel, Switzerland) Jun 2009Aziridine-containing compounds have been of interest as anticancer agents since late 1970s. The design, synthesis and study of triaziquone (TZQ) analogues with the aim...
Aziridine-containing compounds have been of interest as anticancer agents since late 1970s. The design, synthesis and study of triaziquone (TZQ) analogues with the aim of obtaining compounds with enhanced efficacy and reduced toxicity are an ongoing research effort in our group. A series of bis-type TZQ derivatives has been prepared and their cytotoxic activities were investigated. The cytotoxicity of these bis-type TZQ derivatives were tested on three cancer lines, including breast cancer (BC-M1), oral cancer (OEC-M1), larynx epidermal cancer (Hep2) and one normal skin fibroblast (SF). Most of these synthetic derivatives displayed significant cytotoxic activities against human carcinoma cell lines, but weak activities against SF. Among tested analogues the bis-type TZQ derivative 1a showed lethal effects on larynx epidermal carcinoma cells (Hep2), with an LC(50) value of 2.02 microM, and also weak cytotoxic activity against SF cells with an LC(50) value over 10 microM for 24 hr treatment. Comparing the viability of normal fibroblast cells treated with compound 1a and TZQ, the LC(50) value of the latter was 2.52 microM, indicating more toxicity than compound 1a. This significantly decreased cytotoxicity of compound 1a towards normal SF cells, while still maintaining the anticancer activity towards Hep2 cells is an interesting feature. Among the seven compounds synthesized, compound 1c has similar toxicity effects on the three cancer cell lines and SF normal cells as the TZQ monomer.
Topics: Antineoplastic Agents; Cell Line, Tumor; Fibroblasts; Humans; Skin; Triaziquone
PubMed: 19633605
DOI: 10.3390/molecules14072306 -
British Medical Journal Jul 1967
Topics: Carcinoma, Basal Cell; Carcinoma, Squamous Cell; Colchicine; Fluorouracil; Humans; Methotrexate; Podophyllin; Skin Neoplasms; Triaziquone; Zinc
PubMed: 6028097
DOI: No ID Found -
British Journal of Cancer Jul 1974One hundred and sixteen human tumours were transplanted to thymectomized, irradiated, antilymphocyte serum-treated mice. In 12 cases the recipient mice died rapidly,...
One hundred and sixteen human tumours were transplanted to thymectomized, irradiated, antilymphocyte serum-treated mice. In 12 cases the recipient mice died rapidly, presumably from infection. With the remaining 104 tumours, three-quarters grew to a varying extent, retaining the characteristic histological features of the primary tumours. Implant nodules varied widely in composition, from solid tumour and stroma to dense fibrous tissue without recognizable tumour cells. There was no relation between degree of malignancy and ability to grow, and also some benign tumours grew.In 44 cases, mice were treated with the drug or drugs most likely to be used in the patients and the effects on the implants were assessed histologically. Two tumours were largely destroyed and one showed marked metaphase arrest. Three other tumours showed lesser changes that were attributable to the drug but were of equivocal significance.There appeared to be differences in drug sensitivity between structurally different clones of the same tumour, and some tumours treated with two alkylating agents were damaged by one and not the other, suggesting that this model may have substantial discriminatory power. Assays such as this should not be used to guide treatment of the patient without prior validation. The practical and ethical difficulties of validation by clinical trial may be insurmountable, and an alternative approach to validation is proposed which does not raise these difficulties.
Topics: Animals; Chlorambucil; Cyclophosphamide; Dactinomycin; Disease Models, Animal; Female; Fluorouracil; Gastrointestinal Neoplasms; Humans; Immunosuppression Therapy; Male; Melphalan; Methotrexate; Mice; Mice, Inbred CBA; Neoplasm Metastasis; Neoplasm Transplantation; Neoplasms, Experimental; Ovarian Neoplasms; Thiotepa; Thymectomy; Transplantation, Heterologous; Triaziquone; Urinary Bladder Neoplasms; Vinblastine; Vincristine
PubMed: 4213444
DOI: 10.1038/bjc.1974.109 -
Proceedings of the Royal Society of... Apr 1969
Topics: Antineoplastic Agents; Carcinoma; Culture Techniques; Cyclophosphamide; Female; Humans; Methotrexate; Ovarian Neoplasms; Thiotepa; Triaziquone; Vinblastine
PubMed: 4980488
DOI: No ID Found -
Genetics Sep 1977Male and female Drosophila melanogaster with special sex chromosome or special autosome constitutions were fed with the mutagenic chemicals Trenimon...
Male and female Drosophila melanogaster with special sex chromosome or special autosome constitutions were fed with the mutagenic chemicals Trenimon (2,3,5-trisethyleneimino-1,4-benzoquinone) and PDMT (1-phenyl-3, 3-dimethyltriazene) and with the toxic substance Na2PO3F (sodium monofluorophosphate). The frequency of dominant lethality was recorded among the progeny. The results clearly show that dominant lethality is dose dependent for Trenimon- or PDMT-treated chromosomes in mature sperm and mature oocytes, and an increased amount of chromosomal material per nucleus yields an enhanced lethality. In contrast, a pure toxic effect of Na2PO3F on mature oocytes was demonstrated with one type of female. --With the stocks of Drosophila used, it is possible to distinguish between mutagenic and toxic effects of chemicals on the germ cells. Therefore, dominant lethality can be used as a simple and quick screening test for chemical mutagens.
Topics: Animals; Chromosomes; Crosses, Genetic; Dose-Response Relationship, Drug; Drosophila melanogaster; Female; Fluorides; Genes, Dominant; Genes, Lethal; Male; Mutagens; Mutation; Oocytes; Phosphates; Spermatozoa; Triazenes; Triaziquone
PubMed: 410699
DOI: 10.1093/genetics/87.1.67 -
The Journal of Biological Chemistry Nov 1982Treatment of Ehrlich ascites tumor cells with the trifunctional alkylating agent 2,3-5-tris(ethyleneimino)benzoquinone-1,4 (triaziquonum) led to rapid fragmentation of...
Treatment of Ehrlich ascites tumor cells with the trifunctional alkylating agent 2,3-5-tris(ethyleneimino)benzoquinone-1,4 (triaziquonum) led to rapid fragmentation of DNA and depletion of NAD while poly(ADP-ribose) synthetase activity showed a retarded increase. Poly(ADP-ribosyl) residues in treated cells increased 4- to 30-fold, but transiently, and in a dose-dependent manner, exhibiting the same initial kinetics as the loss of NAD and the appearance of DNA strand breaks when determined by the nucleoid method. Although the amounts of "activated ADP-ribosyl" groups present in the substrate NAD (80 nmol/10(8) cells) exceeded by far basal and triaziquonum-induced poly(ADP-ribosyl) groups (up to 250 pmol/10(8) cells), accelerated formation of the polymer, nevertheless, may explain at least partially the loss of NAD seen under these conditions. Addition of benzamide, a potent inhibitor of poly(ADP-ribose) synthetase, to triaziquonum-treated cells effected an immediate drop of poly(ADP-ribose) to basal values. The data indicate a biphasic decay, the half-life of greater than 85% of the polymeric ADP-ribosyl groups exhibiting a t1/2 less than 1 min under these conditions, while the residual fraction died away with t1/2 approximately 6 min. Treatment with the DNA fragmenting agent also led to a 9-fold increase of nuclear mono(ADP-ribosyl) groups, while cytoplasmic mono(ADP-ribosyl) protein conjugates were not significantly affected. The apparent half-life of nuclear mono (ADP-ribosyl) protein conjugates (8-10 min) at peak elevation was definitely longer than that of poly(ADP-ribosyl) residues. This result is consistent with the interpretation that accumulation of mono(ADP-ribosyl) groups is due to a retarded removal of the primary ADP-ribosyl group from the acceptor protein by a separate mono(ADP-ribosyl) protein glycohydrolase, being the rate-limiting step in the overall turnover of poly(ADP-ribosyl) residues.
Topics: ADP Ribose Transferases; Adenosine Diphosphate Ribose; Animals; Carcinoma, Ehrlich Tumor; DNA, Neoplasm; Kinetics; Mice; NAD; Nucleoside Diphosphate Sugars; Poly Adenosine Diphosphate Ribose; Poly(ADP-ribose) Polymerases; Triaziquone
PubMed: 6813330
DOI: No ID Found -
Environmental Health Perspectives Dec 1973
Topics: Animals; Chromatin; Chromosome Aberrations; Cricetinae; Demecolcine; Dose-Response Relationship, Drug; Erythrocytes; Female; Genetic Techniques; Hematopoietic Stem Cells; Methods; Mitomycins; Mitosis; Mutagens; Rats; Triaziquone
PubMed: 4592366
DOI: 10.1289/ehp.7306167 -
Journal of Immunological Methods 1980Thiolation of immunoglobulin G (IgG) with DL-N-acetylhomocysteinethiolactone, catalyzed by 2-pyridinealdoxime methiodide, incorporated new sulfur groups into IgG....
Thiolation of immunoglobulin G (IgG) with DL-N-acetylhomocysteinethiolactone, catalyzed by 2-pyridinealdoxime methiodide, incorporated new sulfur groups into IgG. Triaziquinone was subsequently conjugated to the sulfur groups. Triaziquinone-IgG complex retained the alkylating activity of the drug and the immunological activity of the antibody. The conjugation procedure was inhibited by the thiol-blocking agent methyl methanethiolsulfonate.
Topics: Alkylating Agents; Animals; Antibodies, Viral; Antibody Specificity; Chemical Phenomena; Chemistry; Hemagglutinins, Viral; Immunochemistry; Immunoglobulin G; Influenza A virus; Male; Oxidation-Reduction; Pralidoxime Compounds; Rabbits; Sulfhydryl Compounds; Triaziquone
PubMed: 7204987
DOI: 10.1016/0022-1759(80)90160-x -
European Journal of Biochemistry Mar 1970
Topics: DNA; DNA Replication; Depression, Chemical; Feedback; Metabolism; Mitosis; Plant Proteins; RNA; Saccharomyces; Stimulation, Chemical; Tetrahydrofolate Dehydrogenase; Thymine; Time Factors; Triaziquone
PubMed: 5439076
DOI: 10.1111/j.1432-1033.1970.tb00909.x