Search results for "TOXICITY"

Structure determination and preliminary cytotoxicity researches of the compounds isolated from Rumex acetosella L. on leukemia cells

2017

Discovery of novel anti-inflammatory drug-like compounds by aligning in silico and in vivo screening: The nitroindazolinone chemotype

2011

In this report, we propose the combination of computational methods and in vivo primary screening in zebrafish larvae and confirmatory in mice models as a novel strategy to accelerate anti-inflammatory drug discovery. Initially, a database of 1213 organic chemicals with great structural variability - 587 of them anti-inflammatory agents plus 626 compounds with other clinical uses - was divided into training and test groups. Atom-based quadratic indices - a TOMOCOMD-CARDD molecular descriptors family - and linear discriminant analysis (LDA) were used to develop a total of 13 models to describe the anti-inflammatory activity. The best model (Eq. (13)) shows an accuracy of 87.70% in the traini…

Lipid A-Induced Responses In Vivo

2009

The lipid A analogs used in preclinical studies and clinical trials are not naturally-occurring forms of lipid A; they are synthetic molecules produced to be less toxic than lipid A itself and they do not reproduce the effects of natural lipid A molecules especially in vivo. The responses induced by lipid A analogs are summarized in this chapter: their fate in the blood stream and their toxicity as well as the lipid A tolerance and the tumor immune responses they induce. Lipid A is not found in the mammalian organism under normal circumstances so its use in cancer therapy raises important questions as to its different effects in vivo and its toxicity, particularly in cancer patients. Lipid …

Effects of nordihydroguaiaretic acid on murine antibody-dependent cellular cytotoxicity.

1996

The purpose of this study was to analyze the effects of nordihydroguaiaretic acid, an inhibitor of the lipoxygenase pathway of arachidonic acid, on antibody-dependent cellular cytotoxicity. Antibody-dependent cellular cytotoxicity mediated by murine spleen cells was significantly inhibited by concentrations of nordihydroguaiaretic acid from 10(-5) to 10(-4) M (1C50 = 2 x 10(-5) M). The inhibitory effect of nordihydroguaiaretic acid was also observed on antibody-dependent cellular cytotoxicity mediated by macrophage-depleted spleen cells as well as isolated macrophages. Nordihydroguaiaretic acid was highly effective when added at the beginning of the assay and was always present throughout t…

Isolation of two triterpenoids and a biflavanone with anti-Inflammatory activity from Schinus molle fruits.

2003

Three compounds with anti-inflammatory activity were isolated from Schinus molle fruits. Two of the compounds were identified as 3- epi-isomasticadienolalic acid ( 1), isomasticadienonalic acid ( 2) and chamaejasmin ( 3). Triterpenes 1 and 2, and biflavanone 3 were tested on two models of mice paw inflammation: one of acute inflammation, induced by subcutaneous injection of either phospholipase A (2) (PLA (2)) or carrageenan in the paws of mice, and one of chronic inflammation in the form of eczema, provoked by repeated administration of TPA to the ears of mice. On the PLA (2)-induced mouse paw oedema, only 2 was active (30 mg/kg, 66 % inhibition at 60 min), whereas all compounds reduced th…

Organometallic Palladium Complexes with a Water-Soluble Iminophosphorane Ligand As Potential Anticancer Agents

2012

The synthesis and characterization of a new water-soluble iminophosphorane ligand TPA=N-C(O)-2BrC(6)H(4) (C,N-IM; TPA = 1,3,5-triaza-7-phosphaadamantane) 1 is reported. Oxidative addition of 1 to Pd(2)(dba)(3) affords the orthopalladated dimer [Pd(μ-Br){C(6)H(4)(C(O)N=TPA-kC,N)-2}](2) (2) as a mixture of cis and trans isomers (1:1 molar ratio) where the iminophosphorane moeity behaves as a C,N-pincer ligand. By addition of different neutral or monoanionic ligands to 2, the bridging bromide can be cleaved and a variety of hydrophilic or water-soluble mononuclear organometallic palladium(II) complexes of the type [Pd{C(6)H(4)(C(O)N=TPA-kC,N)-2}(L-L)] (L-L = acac (3); S(2)CNMe(2) (4); 4,7-Diph…

Unexpected DNA damage caused by polycyclic aromatic hydrocarbons under standard laboratory conditions

2007

Abstract The genotoxicity of 15 polycyclic aromatic hydrocarbons was determined with the alkaline version of the comet assay employing V79 lung fibroblasts of the Chinese hamster as target cells. These cells lack the enzymes necessary to convert PAHs to DNA-binding metabolites. Surprisingly, 11 PAHs, i.e., benzo[ a ]pyrene (BaP), benz[ a ]anthracene, 7,12-dimethylbenz[ a ]anthracene, 3-methylcholanthrene, fluoranthene, anthanthrene, 11 H -benzo[ b ]fluorene, dibenz[ a,h ]anthracene, pyrene, benzo[ ghi ]perylene and benzo[ e ]pyrene caused DNA strand breaks even without external metabolic activation, while naphthalene, anthracene, phenanthrene and naphthacene were inactive. When the comet as…

Control of Portulaca oleracea by boldo and lemon essential oils in different soils

2015

Soil characteristics influence plant growth and can affect the phytotoxicity of the essential oils. In this study chemical composition and herbicidal activity of Peumus boldus Mol. and lemon essential oils in different growing medium against Portulaca oleracea L. was investigated. Ninety-four compounds accounting between 95.5 and 99.8% of the total essential oil were identified by gas chromatography-mass spectrometry in boldo and lemon essential oils. Ascaridole (31.56. ±. 0.15%), p-cymene (21.58. ±. 0.09%) and 1,8-cineole (12.57. ±. 0.13%) were the main compounds in P. boldus whereas large amount of limonene (59.28%) followed of β-pinene (12.96%) and γ-terpinene (10.92%) were found in lemo…

Nimbolide inhibits 2D and 3D prostate cancer cells migration, affects microtubules and angiogenesis and suppresses B-RAF/p.ERK-mediated in vivo tumor…

2021

Abstract Background Prostate cancer (PCa) is the most prominent malignancy among men worldwide. PCa cells have a high tendency to metastasize to various distant organs, and this activity is the main cause of PCa mortality. Nimbolide is a promising phytochemical constituent of neem Azadirachta indica (Meliaceae). Previous studies showed that nimbolide exhibited potent anticancer activity however, its role against PCa tumorigenesis has not been fully elucidated. Purpose Our work aims to explore the role of nimbolide in regulating the essential tumor-associated processes involved in the metastatic cascade in PCa cells. Study design Cytotoxicity assay, wound healing and spheroid invasion assays…

Cytotoxicity of botanicals and isolated phytochemicals from Araliopsis soyauxii Engl. (Rutaceae) towards a panel of human cancer cells.

2020

Abstract Ethnopharmacological relevance Araliopsis soyauxii Engl. (Rutaceae) is a Cameroonian medicinal plant traditionally used to treat lung diseases, malaria, and gonorrhea. It has been demonstrated that infectious disease contribute to about 20% of all human tumours. Aims of the study (1) To perform a phytochemical investigation of the dichloromethane-methanol 1:1 extracts of the bark (ASB), roots (ASR), and leaves (ASL) from Araliopsis soyauxii; (2) to evaluate the cytotoxicity of extracts and isolated compounds; (3) to determine the mode of induction of apoptosis of ASB and kihadanin B (12). Materials and methods Fourteen constituents of the crude extracts were isolated by column chro…