Tag: M.W=250-300

Nagahori, Hirohisa; Suzuki, Noriyuki; Le Coz, Florian; Omori, Takashi; Saito, Koichi published the artcile< Prediction of in vivo developmental toxicity by combination of Hand1-Luc embryonic stem cell test and metabolic stability test with clarification of metabolically inapplicable candidates>, Formula: C7H17Cl2N2O3P, the main research area is development toxicity risk assessment Hand Luc embryo stem cell; Cytotoxicity; In-vitro toxicity; Metabolism; Reproductive toxicity.

Hand1-Luc Embryonic Stem Cell Test (Hand1-Luc EST) is a promising alternative method for evaluation of developmental toxicity. However, the problems of predictivity have remained due to appropriateness of the solubility, metabolic system, and prediction model. Therefore, we assessed the usefulness of rat liver S9 metabolic stability test using LC-MS/MS to develop new prediction model. A total of 71 chems. were analyzed by measuring cytotoxicity and differentiation toxicity, and highly reproducible (CV = 20%) results were obtained. The first prediction model was developed by discriminant anal. performed on a full dataset using Hand1-Luc EST, and 66.2% of the chems. were correctly classified by the cross-validated classification. A second model was developed with addnl. descriptors obtained from the metabolic stability test to calculate hepatic availability, and an accuracy of 83.3% was obtained with applicability domain of 50.7% (=36/71) after exclusion of 22 metabolically inapplicable candidates, which potentially have a metabolic activation property. A step-wise prediction scheme with combination of Hand1-Luc EST and metabolic stability test was therefore proposed. The current results provide a promising in vitro test method for accurately predicting in vivo developmental toxicity.

Toxicology Letters published new progress about Animal gene Role: BUU (Biological Use, Unclassified), BIOL (Biological Study), USES (Uses) (HAND1). 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Formula: C7H17Cl2N2O3P.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Logsdon, Amanda L.; Herring, Betty J.; Lockard, Jarrett E.; Miller, Brittany M.; Kim, Hanna; Hood, Ronald D.; Bailey, Melissa M. published the artcile< Exposure to Green Tea Extract Alters the Incidence of Specific Cyclophosphamide-Induced Malformations>, Category: chlorides-buliding-blocks, the main research area is green tea extract cyclophosphamide monohydrate teratogenicity fetus natural pharmaceutical.

BACKGROUND: Green tea extract (GTE) has been shown to have antioxidative properties due to its high content of polyphenols and catechin gallates. Previous studies indicated that catechin gallates scavenge free radicals and attenuate the effects of reactive oxygen species. Cyclophosphamide (CP) produces reactive oxidative species, which can have adverse effects on development, causing limb, digit, and cranial abnormalities. The current study was performed to determine if exposure to GTE can decrease teratogenic effects induced by CP in CD-1 mice. METHODS: From gestation days (GD) 6-13, mated CD-1 mice were dosed with 400 or 800 mg/kg/d GTE; 100, 200, 400, or 800 mg/kg/d GTE + CP; CP alone, or the vehicle. GTE was given by gavage. CP (20 mg/kg) was given by i.p. injection on GD 10. Dams were sacrificed on GD 17, and their litters were examined for adverse effects. RESULTS: The highest GTE dose did not effectively attenuate, and in some cases exacerbated the neg. effect of CP. GTE alone was also associated with an increased incidence of microblepharia. Conversely, moderate GTE doses (200 and/or 400 mg/kg/d) attenuated the effect of CP on fetal weight and (GTE 200 mg/kg/d) decreased the incidences of certain defects resulting from CP exposure. CONCLUSIONS: Exposure of a developing mammal to moderate doses of GTE can modulate the effects of exposure to CP during development, possibly by affecting biotransformation, while a higher GTE dose tended to exacerbate the developmental toxicity of CP. GTE alone appeared to cause an adverse effect on eyelid development.

Birth Defects Research, Part B: Developmental and Reproductive Toxicology published new progress about Arm. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Category: chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Zurlinden, Todd J.; Saili, Katerine S.; Rush, Nathaniel; Kothiya, Parth; Judson, Richard S.; Houck, Keith A.; Hunter, E. Sidney; Baker, Nancy C.; Palmer, Jessica A.; Thomas, Russell S.; Knudsen, Thomas B. published the artcile< Profiling the ToxCast library with a pluripotent human (H9) stem cell line-based biomarker assay for developmental toxicity>, Reference of 6055-19-2, the main research area is toxcast library pluripotent human stem cell line development toxicity; developmental toxicity; embryonic stem cells; predictive toxicology.

The Stemina devTOX quickPredict platform is a human pluripotent stem cell-based assay that predicts the developmental toxicity potential based on changes in cellular metabolism following chem. exposure. Using this assay, we screened 1065 ToxCast phase I and II chems. in single-concentration or concentration-response for the targeted biomarker (ratio of ornithine to cystine secreted or consumed from the media). The dataset from the Stemina (STM) assay is annotated in the ToxCast portfolio as STM. Major findings from the anal. of ToxCast_STM dataset include (1) 19% of 1065 chems. yielded a prediction of developmental toxicity, (2) assay performance reached 79%-82% accuracy with high specificity (> 84%) but modest sensitivity (< 67%) when compared with in vivo animal models of human prenatal developmental toxicity, (3) sensitivity improved as more stringent weights of evidence requirements were applied to the animal studies, and (4) statistical anal. of the most potent chem. hits on specific biochem. targets in ToxCast revealed pos. and neg. associations with the STM response, providing insights into the mechanistic underpinnings of the targeted endpoint and its biol. domain. The results of this study will be useful to improving our ability to predict in vivo developmental toxicants based on in vitro data and in silico models. Toxicological Sciences published new progress about Analysis (toxicol.). 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Reference of 6055-19-2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Ishimaru, Hiromasa; Tsuda, Yasumasa; Kage, Hidenori; Kawano, Tomoaki; Takayama, Shinji; Morimoto, Yoshihito; Goto, Kazumi; Watanabe, Kazuhiro published the artcile< Pressure compatibility test of closed system drug transfer devices for 71 anticancer drugs>, Category: chlorides-buliding-blocks, the main research area is drug transfer device pressure compatibility anticancer agent.

Occupational exposure to anticancer drugs may increase the risk of cancer and the risk of miscarriage and stillbirth, and cause other adverse events such as hypersensitivity reactions, skin/mucous reactions, and digestive symptoms. Several studies have investigated the use of closed-system drug-transfer devices (CSTDs) to reduce the environmental pollution by hazardous drugs. However, few reports have verified whether CSTDs contain the hazardous drugs within the vials. The BD PhaSeal System is a CSTD that is frequently used in Japan. However, the fit of each anti-cancer drug vial has not been investigated. We investigated the fit of 71 major anti-cancer drug vials and protectors released and frequently used in Japan by means of a pressure compatibility test that we developed. The pressure compatibility test involved attaching a three-way stopcock to a Luer lock syringe and attaching an injector in line with the syringe. The pressure tubing was connected to the other side of the three-way stopcock and connected to the pressure inlet of the pressure gauge. The pressure in the anti-cancer drug vial was raised to 100 kPa and connected/disconnected repeatedly. If the pressure fluctuation during the 10th connection was within 6%, it was defined as “”no change””, and the compatibility of the protector and the vial was evaluated. The median pressure reduction rates at the 10th connection ranged from -1.98% to -4.95%. All drugs surveyed had an error rate within 6%. The BDPhaSeal Protector was shown to be compatible with the 71 anti-cancer drugs we surveyed.

Yakugaku Zasshi published new progress about Antitumor agents. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Category: chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Tseng, Wei-Ting; Shih, Tsung-Wei; Liu, Shing-Hwa; Pan, Tzu-Ming published the artcile< Safety and mutagenicity evaluation of Vigiis 101 powder made from Lactobacillus paracasei subsp. paracasei NTU 101>, Application In Synthesis of 6055-19-2, the main research area is Lactobacillus Vigiis 101 powder safety mutagenicity; Lactobacillus paracasei subsp. paracasei NTU 101; No observed adverse effect level; Probiotic.

The aim of the present work was to assess the genotoxic activity and the potential for toxicity upon repeated dosing of “”Vigiis 101″” powder, a probiotic consisting of dried bacteria Lactobacillus paracasei subsp. paracasei NTU 101. Results of the Ames test in Salmonella typhimurium strains TA1537, TA98, TA100, TA102, and TA1535 showed that Vigiis 101 (≤5 mg per plate) was not mutagenic. We used experiments on ICR mice to evaluate the genotoxicity of Vigiis 101. Compared to the control, high-dose Vigiis 101 administration (16.72 g per kg of body weight) did not cause significant changes either in the number of reticulocytes or in the percentage (occurrence) of micronucleated reticulocytes. A mammalian chromosomal aberration test showed that the number of Chinese hamster ovary cells with abnormal chromosomes was <4% after Vigiis 101 treatment (maximal concentration was 5 mg/mL). A 28-day oral toxicity assay in Wistar rats was performed to assess the no-observed-adverse-effect level of Vigiis 101. Compared to the control, high-dose Vigiis 101 administration (5000 mg/kg/day) had no effects on mortality and body weight and did not cause toxicopathol. lesions. Taken together, these results show that Vigiis 101 has no significant mutagenic or toxic effects. Regulatory Toxicology and Pharmacology published new progress about Adrenal gland. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Application In Synthesis of 6055-19-2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Ribeiro, Rita de Cassia Lima; Botelho, Emerson Luiz Lorenco; Donadel, Guilherme; Ames, Maria Leticia; Nunes, Bruna; Tramontini, Salviano; Soares, Andreia Assuncao; Alberton, Odair; Jacomassi, Ezilda; Gasparotto, Arquimedes Junior published the artcile< Genotoxicity Study of Vitex megapotamica (Spreng.) Moldenke>, Application of C7H17Cl2N2O3P, the main research area is genotoxicity edible fruit plant Vitex megapotamica; Lamiaceae; comet test; micronucleus; safety; toxicity.

Vitex megapotamica (Spreng) Moldenke is commonly known as taruma, ∼ it is an important medicinal and edible fruit plant. It is native to regions of tropical and subtropical climate in greater proportion than temperate zones and widely distributed in Central America, South America, Asia, and Africa. In Brazil, it is present in the Atlantic Forest and Cerrado biomes. Despite its widespread use, there are no min. standards for quality control or information on genotoxicity. Therefore, the aim of this study was to present a detailed description of the short-term genotoxicity assays of V. megapotamica and to provide parameters of a preparation routinely used in traditional folk medicine. For genotoxicity assays, five groups were used with eight wistar rats in each group. For this, three doses of the V. megapotamica extract in doses (100, 300, and 900 mg/kg) or neg. control (filtered water) were administered orally and pos. control cyclophosphamide monohydrate (20 mg/kg; Sigma-Aldrich) was applied by the i.p. route after 24 h. At the end, whole blood was collected in a tube containing EDTA for the comet test and later the animals were euthanized. For the micronucleus test, femurs were removed, and bone marrow was collected. In the comet assay, V. megapotamica crude extract did not show significant DNA damage at all doses tested. The micronucleus assay showed no significant increase in the frequency of inducing micronuclei at any dose examined It can be concluded that the safety parameters in genotoxicity studies reveal that V. megapotamica has no toxicity, which characterizes the important quality control of this plant species.

Journal of Medicinal Food published new progress about Blood. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Application of C7H17Cl2N2O3P.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Rotroff, Daniel M.; Martin, Matt T.; Dix, David J.; Filer, Dayne L.; Houck, Keith A.; Knudsen, Thomas B.; Sipes, Nisha S.; Reif, David M.; Xia, Menghang; Huang, Ruili; Judson, Richard S. published the artcile< Predictive Endocrine Testing in the 21st Century Using in Vitro Assays of Estrogen Receptor Signaling Responses>, Product Details of C7H17Cl2N2O3P, the main research area is estrogen receptor signaling endocrine disrupter high throughput screening.

Thousands of environmental chems. are subject to regulatory review for their potential to be endocrine disruptors (ED). In vitro high-throughput screening (HTS) assays have emerged as a potential tool for prioritizing chems. for ED-related whole-animal tests. In this study, 1814 chems. including pesticide active and inert ingredients, industrial chems., food additives, and pharmaceuticals were evaluated in a panel of 13 in vitro HTS assays. The panel of in vitro assays interrogated multiple end points related to estrogen receptor (ER) signaling, namely binding, agonist, antagonist, and cell growth responses. The results from the in vitro assays were used to create an ER Interaction Score. For 36 reference chems., an ER Interaction Score >0 showed 100% sensitivity and 87.5% specificity for classifying potential ER activity. The magnitude of the ER Interaction Score was significantly related to the potency classification of the reference chems. ERα/ERβ selectivity was also evaluated, but relatively few chems. showed significant selectivity for a specific isoform. When applied to a broader set of chems. with in vivo uterotrophic data, the ER Interaction Scores showed 91% sensitivity and 65% specificity. Overall, this study provides a novel method for combining in vitro concentration response data from multiple assays and, when applied to a large set of ER data, accurately predicted estrogenic responses and demonstrated its utility for chem. prioritization.

Environmental Science & Technology published new progress about Anise oil Role: ADV (Adverse Effect, Including Toxicity), BIOL (Biological Study). 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Product Details of C7H17Cl2N2O3P.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Al-Katib, Ayad; Arnold, Alan A.; Aboukameel, Amro; Sosin, Angela; Smith, Peter; Mohamed, Anwar N.; Beck, Frances W.; Mohammad, Ramzi M. published the artcile< I-kappa-kinase-2 (IKK-2) inhibition potentiates vincristine cytotoxicity in non-Hodgkin's lymphoma>, Category: chlorides-buliding-blocks, the main research area is ML120B vincristine nonHodgkin lymphoma IKK2 NFkappaB anticancer.

Background: IKK-2 is an important regulator of the nuclear factor-κB (NF-κB) which has been implicated in survival, proliferation and apoptosis resistance of lymphoma cells. In this study, we investigated whether inhibition of IKK-2 impacts cell growth or cytotoxicity of selected conventional chemotherapeutic agents in non-Hodgkin’s lymphoma. Two established model systems were used; Follicular (WSU-FSCCL) and Diffuse Large Cell (WSU-DLCL2) Lymphoma, both of which constitutively express p-IκB. A novel, selective small mol. inhibitor of IKK-2, ML120B (N-[6-chloro-7-methoxy-9H-β-carbolin-8-yl]-2-methylnicotinamide) was used to perturb NF-κB in lymphoma cells. The growth inhibitory effect of ML120B (M) alone and in combination with cyclophosphamide monohydrate (C), doxorubicin (H) or vincristine (V) was evaluated in vitro using short-term culture assay. We also determined efficacy of the combination in vivo using the SCID mouse xenografts. Results: ML120B down-regulated p-IκBα protein expression in a concentration dependent manner, caused growth inhibition, increased G0/G1 cells, but did not induce apoptosis. There was no significant enhancement of cell kill in the M/C or M/H combination. However, there was strong synergy in the M/V combination where the vincristine concentration can be lowered by a hundred fold in the combination for comparable G2/M arrest and apoptosis. ML120B prevented vincristine-induced nuclear translocation of p65 subunit of NF-κB. In vivo, ML120B was effective by itself and enhanced CHOP anti-tumor activity significantly (P = 0.001) in the WSU-DLCL2-SCID model but did not prevent CNS lymphoma in the WSU-FSCCL-SCID model. Conclusions: For the first time, this study demonstrates that perturbation of IKK-2 by ML120B leads to synergistic enhancement of vincristine cytotoxicity in lymphoma. These results suggest that disruption of the NF-κB pathway is a useful adjunct to cytotoxic chemotherapy in lymphoma.

Molecular Cancer published new progress about Antitumor agents. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Category: chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Willems, Maxime; Stevens, An-Sofie; Adriaens, Els; Plusquin, Michelle; Smeets, Karen; Van Goethem, Freddy; Vanparys, Philippe; Janssen, Colin; Remon, Jean-Paul published the artcile< An Adult Stem Cell Proliferation Assay in the Flatworm Model Macrostomum lignano to Predict the Carcinogenicity of Compounds>, Formula: C7H17Cl2N2O3P, the main research area is Macrostomum stem cell proliferation chem carcinogenicity prediction model.

Flatworms possess adult pluripotent stem cells whose dynamics can easily be exptl. assessed in vivo. This feature provides the unique opportunity to be used in a pharmacol. context to test the safety of chems. The objective of this study was to develop and assess the applicability of an alternative in vivo test with a low-level organism where stem cell proliferation is used as an endpoint to predict the carcinogenicity of chems. As a start, to obtain proof of concept with this new test model, we tested 4 known carcinogens (2 DNA-reactive and 2 non-DNA-reactive) and 2 noncarcinogens as neg. controls. We evaluated our carcinogenicity prediction model and advocate for its future use in pharmacol. safety screenings.

Applied In Vitro Toxicology published new progress about Adult, nonmammalian. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Formula: C7H17Cl2N2O3P.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Ali, Shaukat; Champagne, Danielle L.; Richardson, Michael K. published the artcile< Behavioral profiling of zebrafish embryos exposed to a panel of 60 water-soluble compounds>, Electric Literature of 6055-19-2, the main research area is locomotor behavior Danio embryo water soluble compound.

The zebrafish is a powerful whole animal model which is complementary to in vitro and mammalian models. It has been shown to be applicable to the high-throughput behavioral screening of compound libraries. We have analyzed 60 water-soluble toxic compounds covering a range of common drugs, toxins and chems., and representing various pharmacol. mechanisms. Wild-type zebrafish larvae were cultured individually in defined buffer in 96 well plates. They were exposed for a 96 h period starting at 24 h post fertilization (hpf). A logarithmic concentration series was used for range-finding, followed by a narrower geometric series for LC50 determination LC50 values were determined at 24 h intervals and behavioral testing was carried out on day 5. We used the visual motor response test, in which movement of individual larvae was analyzed using automated video-tracking. For all compounds, LC50 values were found to decrease as the embryo developed. The majority of compounds (57/60) produced an effect in both the basal (lights on) and challenge phases (lights off) of the behavioral assay. These effects were either (i) suppression of locomotor activity (monotonic concentration-response); (ii) stimulation then suppression (biphasic response); (iii) stimulation (monotonic response). We conclude that behavioral assays with zebrafish embryos could be useful for pharmaceutical efficacy and toxicity screening. The precise phenotypic outcome obtained with behavioral assay varies with compound class.

Behavioural Brain Research published new progress about Aquatic toxicity. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Electric Literature of 6055-19-2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics