Key parameter optimization using multivariable linear model for the evaluation of the in vitro estrogenic activity assay in T47D cell lines (CXCL‐test)

2021 ◽  
Author(s):  
Lucie Linhartova ◽  
Nathalie Costet ◽  
Farzad Pakdel ◽  
Tomas Cajthaml ◽  
Denis Habauzit
Keyword(s):  
Linear Model ◽  
Cell Lines ◽  
Parameter Optimization ◽  
Estrogenic Activity ◽  
T47d Cell ◽  
Activity Assay ◽  
Key Parameter

scholarly journals A Structural and in Vitro Characterization of Asoprisnil: A Selective Progesterone Receptor Modulator

2007 ◽  
Vol 21 (5) ◽  
pp. 1066-1081 ◽  
Author(s):  
Kevin P. Madauss ◽  
Eugene T. Grygielko ◽  
Su-Jun Deng ◽  
Anthony C. Sulpizio ◽  
Thomas B. Stanley ◽  
...  
Keyword(s):  
Gene Expression ◽  
Progesterone Receptor ◽  
Crystal Structures ◽  
Nuclear Receptor ◽  
Estrogenic Activity ◽  
Uterine Fibroids ◽  
T47d Cell ◽  
Gynecological Disorders ◽  
Receptor Modulator

Abstract Selective progesterone receptor modulators (SPRMs) have been suggested as therapeutic agents for treatment of gynecological disorders. One such SPRM, asoprisnil, was recently in clinical trials for treatment of uterine fibroids and endometriosis. We present the crystal structures of progesterone receptor (PR) ligand binding domain complexed with asoprisnil and the corepressors nuclear receptor corepressor (NCoR) and SMRT. This is the first report of steroid nuclear receptor crystal structures with ligand and corepressors. These structures show PR in a different conformation than PR complexed with progesterone (P4). We profiled asoprisnil in PR-dependent assays to understand further the PR-mediated mechanism of action. We confirmed previous findings that asoprisnil demonstrated antagonism, but not agonism, in a PR-B transfection assay and the T47D breast cancer cell alkaline phosphatase activity assay. Asoprisnil, but not RU486, weakly recruited the coactivators SRC-1 and AIB1. However, asoprisnil strongly recruited the corepressor NCoR in a manner similar to RU486. Unlike RU486, NCoR binding to asoprisnil-bound PR could be displaced with equal affinity by NCoR or TIF2 peptides. We further showed that it weakly activated T47D cell gene expression of Sgk-1 and PPL and antagonized P4-induced expression of both genes. In rat leiomyoma ELT3 cells, asoprisnil demonstrated partial P4-like inhibition of cyclooxygenase (COX) enzymatic activity and COX-2 gene expression. In the rat uterotrophic assay, asoprisnil demonstrated no P4-like ability to oppose estrogen. Our data suggest that asoprisnil differentially recruits coactivators and corepressors compared to RU486 or P4, and this specific cofactor interaction profile is apparently insufficient to oppose estrogenic activity in rat uterus.

scholarly journals Sitotoksisitas in vitro ekstrak etanolik buah parijoto (Medinilla speciosa, reinw.ex bl.) terhadap sel kanker payudara T47D

2014 ◽  
Vol 2 (2) ◽  
pp. 53-58 ◽  
Author(s):  
Iin Tusanti ◽  
Andrew Johan ◽  
RA Kisdjamiatun
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Colorimetric Assay ◽  
Ethanolic Extract ◽  
T47d Cell ◽  
Ic50 Value ◽  
T47d Cell Line

Background: Several studies focused on phytochemical as agents of cancer prevention and co-chemotherapy. One of Indonesian plant which has edible fruit but it hasn’t been completely explored is Medinilla speciosa (Reinw.ex Bl.). Objective : The aim of this study is to examine the cytotoxic activity (IC50 value) of Medinilla speciosa (Reinw.ex Bl.) fruit ethanolic extract. Methods : Medinilla speciosa (Reinw.ex Bl.) fruit ethanolic extract was used in this study. The cytotoxic activity was investigated in vitro on human breast cancer T47D cell-line. The cells viability were assessed using MTT colorimetric assay. Breast cancer T47D cell lines was treated with fruit ethanolic extract (10, 25, 50, 100, 250, 500 and 1000 µg/ml) for 24 hour of incubation. This study also identified phytochemical compound of the fruit with thin layer chromatography (TLC). Results: The result showed that ethanolic extract of Medinilla speciosa (Reinw.ex Bl.) has moderate cytotoxicity on breast cancer T47D cell line with IC50 value of 614.50 µg/ml and yield the decrease of cell viability at higher concentration. Medinilla speciosa fruit can not be used as anticancer agent but chemoprevention agent. Phytochemical test showed that the fruit extract contain flavonoid and saponin compound. Conclusion: Ethanolic extract of Medinilla speciosa fruit exhibited moderate cytotocicity on breast cancer T47D cell lines with IC50 value was 614,50 µg/ml thus it can be used as chemopreventioan agent.

Author response for "Combining T‐cell‐based immunotherapy with venetoclax elicits synergistic cytotoxicity to B‐cell lines in vitro"

2020 ◽  
Author(s):  
Satsuki Murakami ◽  
Susumu Suzuki ◽  
Ichiro Hanamura ◽  
Kazuhiro Yoshikawa ◽  
Ryuzo Ueda ◽  
...  
Keyword(s):  
T Cell ◽  
B Cell ◽  
Cell Lines ◽  
Author Response ◽  
Synergistic Cytotoxicity

Bestimmung der DNA-Schädigung in vitro

2010 ◽  
Vol 49 (S 01) ◽  
pp. S64-S68
Author(s):  
E. Dikomey
Keyword(s):  
Dna Damage ◽  
Cell Lines ◽  
Chromosome Aberrations ◽  
Genetic Factors ◽  
Double Strand Breaks ◽  
Strand Breaks ◽  
Cell Inactivation ◽  
Repair Mechanisms ◽  
Break Repair

SummaryIonising irradiation acts primarily via induction of DNA damage, among which doublestrand breaks are the most important lesions. These lesions may lead to lethal chromosome aberrations, which are the main reason for cell inactivation. Double-strand breaks can be repaired by several different mechanisms. The regulation of these mechanisms appears be fairly different for normal and tumour cells. Among different cell lines capacity of doublestrand break repair varies by only few percents and is known to be determined mostly by genetic factors. Knowledge about doublestrand break repair mechanisms and their regulation is important for the optimal application of ionising irradiation in medicine.

Effect of black seeds (Nigella sativa) volatile oil on the cervical cancer: In vitro study, on Hela cell lines

2019 ◽  
Vol 7 (4) ◽  
pp. 91-96
Author(s):  
Isra'a Al-sobhi ◽  
◽  
Rawan Al-Ghabban ◽  
Soad Shaker Ali ◽  
Jehan Al-Amri ◽  
...  
Keyword(s):  
Cervical Cancer ◽  
Hela Cell ◽  
Cell Lines ◽  
Nigella Sativa ◽  
In Vitro Study ◽  
Volatile Oil ◽  
Vitro Study ◽  
Hela Cell Lines ◽  
Black Seeds

Screening, Fabrication and Evaluation of Pharmaceutical Dosage Forms using P-Glycoprotein Modulators

2017 ◽  
Vol 10 (2) ◽  
pp. 3688-3699
Author(s):  
Joshi Vedamurthy ◽  
Shivakumar Inamdar ◽  
Ankit Acharya ◽  
Rajesh Kowti
Keyword(s):  
Cell Lines ◽  
Tinospora Cordifolia ◽  
Absorption Enhancement ◽  
Synergistic Activity ◽  
Capsicum Frutescens ◽  
Plumbago Zeylanica ◽  
Pharmaceutical Dosage Forms ◽  
Holarrhena Antidysenterica ◽  
Trachyspermum Ammi

In this project, in vitro absorption enhancement activity of P-gp substrates Fexofenadine (Fx) and Ciprofloxacin (Cp) were evaluated in everted rat gut sac model and Caco-2 cell lines. Verapamil was used as P-gp inhibitor. Piper betel, Trachyspermum ammi, Plumbago zeylanica, Trikatu, Moringaoleifera, Murraya koenigii,  Ferulafoitida  Zingiber officinale, Cheilocostus speciosus, Capsicum frutescens Operculina turpethum Holarrhena antidysenterica Mesuaferrea, Tinospora cordifolia,  and Picrorhiza kurroa, were selected and extracted with 99% alcohol and fresh juices of Citrus limon, Punica granatum seeds were also studied. In-vitro studies depicted that Fexofenadine and Ciprofloxacin absorption was increased greater than 20% in the presence of Operculinaturpethum, Capsicum frutescens, Holarrhena Antidysenterica, Tinospora cordifolia, Trikatu, Trachyspermum ammi, Plumbago zeylanica. The flux of the ciprofloxacin transport was in the range of 9-23 mcg/min and Papp         2.6 × 10-5 cm/sec to 4.1 × 10-5  cm/sec whereas Fexofenadine flux was in the range of 2-7.7 mcg/min and Papp 4.16 × 10–6 cm/sec to 1.62 ×       10-5 cm/sec.  In vitro antimicrobial activity of ciprofloxacin on selected microbes in presence of extracts also depicted synergistic activity. Histological studies revealed that there is no significant variation observed in the isolated sac in presence of the extracts. CaCo2 cell lines studies showed that, formulation enhanced the absorption of fexofenadine greater than 50%. Tablets were prepared and evaluated using the plant extracts which yielded >20% absorption enhancement of the substrates. In conclusion, tablet formulation containing the alcoholic extracts of Trachyspermum ammi, Plumbago zylanicum, Capsicum frutescens, Operculina turpethum, Holarrhena Antidysenterica, Tinospora cordifolia and Trikatu can act as an absorption enhancer for fexofenadine and ciprofloxacin. The mechanism of action of these herbs could be due to    P-gp inhibition. Further clinical studies are needed to prove its efficacy in humans.     

ANTITUMOR EFFECT OF SUNITINIB AND BORTEZOMIB ON BREAST CANCER CELL LINE IN VITRO

2017 ◽  
Vol 63 (1) ◽  
pp. 141-145
Author(s):  
Yuliya Khochenkova ◽  
Eliso Solomko ◽  
Oksana Ryabaya ◽  
Yevgeniya Stepanova ◽  
Dmitriy Khochenkov
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Antitumor Effect ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Actual Problem

The discovery for effective combinations of anticancer drugs for treatment for breast cancer is the actual problem in the experimental chemotherapy. In this paper we conducted a study of antitumor effect of the combination of sunitinib and bortezomib against MDA-MB-231 and SKBR-3 breast cancer cell lines in vitro. We found that bortezomib in non-toxic concentrations can potentiate the antitumor activity of sunitinib. MDA-MB-231 cell line has showed great sensitivity to the combination of bortezomib and sunitinib in vitro. Bortezomib and sunitinib caused reduced expression of receptor tyrosine kinases VEGFR1, VEGFR2, PDGFRa, PDGFRß and c-Kit on HER2- and HER2+ breast cancer cell lines

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