Search results for "G2"

Cittadini e cittadinanza. Prospettive, ruolo e opportunità di Agenda 21 Locale in ambito urbano

2008

On the arithmetic and geometry of binary Hamiltonian forms

2011

Given an indefinite binary quaternionic Hermitian form $f$ with coefficients in a maximal order of a definite quaternion algebra over $\mathbb Q$, we give a precise asymptotic equivalent to the number of nonequivalent representations, satisfying some congruence properties, of the rational integers with absolute value at most $s$ by $f$, as $s$ tends to $+\infty$. We compute the volumes of hyperbolic 5-manifolds constructed by quaternions using Eisenstein series. In the Appendix, V. Emery computes these volumes using Prasad's general formula. We use hyperbolic geometry in dimension 5 to describe the reduction theory of both definite and indefinite binary quaternionic Hermitian forms.

Isopetasin and S-isopetasin as novel P-glycoprotein inhibitors against multidrug-resistant cancer cells

2019

Abstract Background A major problem of cancer treatment is the development of multidrug resistance (MDR) to chemotherapy. MDR is caused by different mechanisms such as the expression of the ABC-transporters P-glycoprotein (P-gp, MDR1, ABCB1) and breast cancer resistance protein (BCRP, ABCG2). These transporters efflux xenobiotic toxins, including chemotherapeutics, and they were found to be overexpressed in different cancer types. Purpose Identification of novel molecules that overcome MDR by targeting ABC-transporters. Methods Resazurin reduction assay was used for cytotoxicity test. AutoDock 4.2. was used for molecular docking. The function of P-gp and BCRP was tested using a doxorubicin …

Collateral sensitivity of drug-resistant ABCB5- and mutation-activated EGFR overexpressing cells towards resveratrol due to modulation of SIRT1 expre…

2019

Abstract Background In the drug discovery field, natural products deemed a precious source of novel lead compounds. They have the ability to bypass or overcome multidrug resistance (MDR) in cancer cells. Purpose In this study, the natural polyphenolic stilbene resveratrol (RES) has been studied for its cytotoxic activity toward MDR cancer cells. Methods Resazurin assay was used to investigate the cytotoxicity of RES not only against a panel of drug-resistant cancer cells overexpressing P-glycoprotein/ABCB1, BCRP/ABCG2, ABCB5 (ATP-binding cassette transporters), but also mutation-activated EGFR. The assessment of proteins expression was done by Western blot analysis. COMPARE and hierarchical…

Inhibition of ATP-Binding Cassette Transporters by Chinese Herbs and Phytochemicals

2012

The gene family of ATP-binding cassette (ABC) transporters is widely distributed over the evolutionary tree of life from bacteria to man. In cancer, several ABC transporters are involved in the transport of anticancer drugs. This leads to the development of resistance to a broad spectrum of anticancer agents, termed multidrug resistance. An attractive strategy to overcome multidrug resistance is to block the transport function of ABC transporters leading to lethal intracellular concentrations of anticancer drugs. Efforts to identify transport inhibitors lead to a huge amount of chemical substances, none of which successfully passed clinical trials in cancer patients because of high toxicity…

Cytotoxicity of cucurbitacin E from Citrullus colocynthis against multidrug-resistant cancer cells

2019

Abstract Background Cucurbitacin E (CuE) is an oxygenated tetracyclic triterpenoid isolated from the fruits of Citrullus colocynthis (L.) Schrad. Purpose This study outlines CuE's cytotoxic activity against drug-resistant tumor cell lines. Three members of ABC transporters superfamily, P-glycoprotein (P-gp), breast cancer resistance protein (BCRP) and ABCB5 were investigated, whose overexpression in tumors is tightly linked to multidrug resistance. Further factors of drug resistance studied were the tumor suppressor TP53 and the epidermal growth factor receptor (EGFR). Methods Cytotoxicity assays (resazurin assays) were used to investigate the activity of Citrullus colocynthis and CuE towar…

Liver and gastrointestinal cancers

2020

Abstract One important limitation in the treatment of liver and gastrointestinal cancers is their poor response to available chemotherapy, which is due in part to efficient mechanisms of defense against antitumor drugs. An important role in chemoresistance is played by ATP-binding cassette (ABC) proteins, normally involved in barrier/secretory functions of the digestive apparatus. ABC pumps, often up-regulated in cancers derived from these organs, actively export antitumor agents from cancer cells, thereby reducing the pharmacological effect of these drugs. Among the ABC proteins with the highest impact on the multidrug resistance (MDR) phenotype of many cancer types is MDR1 or P-glycoprote…

An Arakelov inequality in characteristic p and upper bound of p-rank zero locus

2008

In this paper we show an Arakelov inequality for semi-stable families of algebraic curves of genus $g\geq 1$ over characteristic $p$ with nontrivial Kodaira-Spencer maps. We apply this inequality to obtain an upper bound of the number of algebraic curves of $p-$rank zero in a semi-stable family over characteristic $p$ with nontrivial Kodaira-Spencer map in terms of the genus of a general closed fiber, the genus of the base curve and the number of singular fibres. An extension of the above results to smooth families of Abelian varieties over $k$ with $W_2$-lifting assumption is also included.

The activating receptor NKG2D of natural killer cells promotes resistance against enterovirus-mediated inflammatory cardiomyopathy

2014

In enterovirus-induced cardiomyopathy, information regarding the detailed impact of natural killer (NK) cells on the outcome of the disease is limited. We therefore hypothesized that NK cells and certain NK cell receptors determine the different outcome of coxsackievirus B3 (CVB3) myocarditis. Here, we demonstrate in murine models that resistance to chronic CVB3 myocarditis in immunocompetent C57BL/6 mice is characterized by significantly more mature CD11b(high) NK cells, the presence of NKG2D on NK cells, and enhanced NKG2D-dependent cytotoxicity compared to CVB3-susceptible A.BY/SnJ mice. The highly protective role of NKG2D in myocarditis was further proven by in vivo neutralization of NK…

Assessment of the cytotoxic potential of an aqueous-ethanolic extract from Thalassia testudinum angiosperm marine grown in the Caribbean Sea

2018

Abstract Objectives Reported antioxidant, anti-inflammatory and neuroprotective properties for one aqueous-ethanolic extract from Thalassia testudinum which grows in the Caribbean Sea compelled us to explore about extract cytotoxic effects. Methods Cell viability was assayed on tumour (HepG2, PC12, Caco-2 and 4T1) and non-tumour (VERO, 3T3, CHO, MCDK and BHK2) cell lines. The extract effects upon primary cultures of rat and human hepatocytes and human lymphocytes were assayed. Key findings The extract exhibited cytotoxicity against cancer cells compared to normal cells, and the IC50 values were 102 μg/ml for HepG2, 135 μg/ml for PC12, 165 μg/ml for Caco-2 and 129 μg/ml for 4T1 cells after 4…