Hiba Zalloum

University of Jordan | UJ

Abstract Chemoresistance is the major cause of cancer recurrence, relapse and eventual death. Doxorubicin resistance is one such challenge in breast cancer. The use of quercetin, an antioxidant, in combination with doxorubicin has been investigated for offering protection to normal cells from the toxic side effects of doxorubicin in addition to mod...

Three Schiff base ligands, NQ, CQ and HQ, were prepared from the reaction of quinoline-3-carbohydrazide with 2-nitrobenzaldehyde, 2-chlorobenzaldehyde and 2,4-dihydroxybenzaldehyde, respectively, and were investigated for their coordination to Cu (II), Ni(II), Co(II), Cd(II), Cr(III) and Fe(III) chlorides. The NQ preparation and the X-ray structure...

Background: Lysine-specific demethylase is a demethylase enzyme that can remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cell metastasis and invasiveness, and is associated with inferior prognosis. LSD1 is associated with its...

Lysine-specific demethylase is a demethylase enzyme that can remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cell metastasis and is associated with inferior prognosis. LSD1 is associated with its corepressor protein CoREST, an...

Quinones are a class of cyclic organic compounds that are widely distributed in nature and have been shown to exhibit anti-inflammatory, antioxidant, and anticancerous activities. However, the molecular mechanisms/signaling by which these molecules exert their effect are still not fully understood. In this study, a group of quinone-derived compound...

Plant polyphenols have attracted attention in recent years due to their ability to undergo oxidative coupling reactions enabled by the presence of multiple phenolic hydroxyl groups, forming chemically versatile coatings and biocompatible nanoparticles (NPs) for various applications. The aim of this study was to investigate whether coffee bean aqueo...

Intense efforts by pharmaceutical industry have been made to identify new targets for obesity-diabetes (Diabesity). Pancreatic triacylglycerol lipase (PL) inhibition is an interesting putative target for obesity management. Fluoroquinolones (FQs) have been identified as potent inhibitors of PL. The aim of this research was to synthesize novel FQs a...

Plant polyphenols have received considerable attention in recent years due to their ability to undergo oxidation-triggered self-polymerization, forming biocompatible versatile coatings and templated nanoparticles (NPs) that can be leveraged for a variety of biomedical applications. Here we show for the first time that untemplated NPs can be conveni...

Background: Breast cancer is one of the most lethal types of cancer in women worldwide. The human epidermal growth factor receptor 2 (HER2) is considered as a validated target in breast cancer therapy. Previously, we have used quantitative structure activity relationship QSAR equations and their associated pharmacophore models to screen for new pr...

Lysine-specific demethylase is a demethylase enzyme that can remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cell metastasis and invasiveness, and is associated with inferior prognosis. LSD1 is associated with its corepressor...

Twenty-five structurally diverse compounds have been tested in vitro for their pancreatic lipase (PL) inhibitory activity. Despite the diversity of tested compounds, the relationship comprising structural attributes of the compounds could be established to correlate with the observed inhibitory activity. Compounds that exerted inhibitory action thr...

A new series of novel N1-anthraquinon-2-yl amidrazones incorporating N-piperazines and related congeners were synthesized via reaction of the hydrazonoyl chloride derived from 2-qaminoanthraquinone with the appropriate piperazine (secondary amine). Structures of the new compounds were confirmed by a panel of spectroscopic methods including IR, NMR,...

Epigenetic targeting of cancer is a recent era to manipulate the gene without destroying the genetic material. Lysine-specific demethylase 1 (LSD1) is one of the enzymes associated with the chromatin for post-translational modifications, where it demethylates lysine amino acid in the chromatin H3 tail. Many studies showed that inhibiting LSD1 could...

Purpose: Pancreatic triacylglycerol lipase (PL) is a noteworthy pharmacological target for the management of dyslipidemia, and diabetes and obesity. This study was aimed to evaluate the modulatory effects of Salvia triloba L.f. (Lamiaceae) leaves methanol extract (ME) on a high fat diet (HFD)-induced hypertriglyceridemia in rats, with complementary...

ABSTRACT The epidemic of obesity as a disease is alarmingly escalating. Pancreatic triacylglycerol lipase (PL) inhibition is an interesting pharmacotherapy target for the management of obesity and related metabolic disorders. As fluoroquinolones (FQ) have been identified as potent inhibitors of PL; three novel FQs (3, 4 and 5) were synthesized and...

Curcumin inhibited efficaciously and dose dependently the pancreatic triacylglycerol lipase (PL) activity with an IC50 value of 7.3 μg/mL (19.8 μM). Its PL-catalysis inhibition propensities have been studied to draw further on structure-potency enhancement. Enzyme kinetics study proved that curcumin inhibits PL in a competitive manner. The observed...

The general use of antioxidants is to retard the reaction of organic materials, such as synthetic polymers, with atmospheric oxygen; such reaction can cause degradation of the polymer and can alter many of its properties which could lead to loss of flavor and development of rancidity in foods, to an increase in viscosity and acidity, and to formati...

The adsorption behavior of Cu(II) ions onto poly(2-hydroxy-4-acryloyloxybenzophenone), polymer I, and onto poly(2-hydroxy-4-acryloyloxybenzophenone) crosslinked with different amounts of divinylbenzene (DVB), polymers II, III, and IV, in aqueous solutions was investigated using batch adsorption experiments as a func-tion of contact time, pH, and te...

Antioxidants are generally used to retard the reaction of organic materials, such as synthetic polymers, with atmospheric oxygen. Such a reaction can cause the degradation of the polymer and can alter many of its properties. This in turn could lead to loss of flavor and the development of rancidity in foods, to an increase in viscosity and acidity,...

N-Myristoyl transferase is an essential enzyme for fungal growth and survival. The continuous interest in the development of new antifungal agents prompted recent interest in developing new potent inhibitors of fungal N-myristoyl transferase. In this context, we combined pharmacophore and QSAR modeling to explore the structural requirements for pot...

The pharmacophoric space of estrogen receptor beta (ERbeta) was explored using a set of 119 known ligands. Subsequently, genetic algorithm and multiple linear regression analysis were employed to select optimal combinations of pharmacophoric models and physicochemical descriptors in self-consistent and predictive quantitative structure-activity rel...

Homology modeling is becoming a valid method for obtaining three-dimensional coordinates for proteins. However, it is hard to judge the qualities of the resulting models warranting robust subsequent validations. In an attempt to evaluate the quality of Melanin-concentrating hormone 1 receptor (MCH1R) homology models, a number of homology structures...

The adsorption of Cu(II) ions onto the chitosan derived Schiff bases obtained from the condensation of chitosan with salicyaldehyde (polymer I), 2,4-dihydroxybenzaldehyde (polymer II) and with 4-(diethylamino) salicyaldehyde (polymer III) in aqueous solutions was investigated. Batch adsorption experiments were carried out as a function of contact t...

Hormone sensitive lipase (HSL) has been recently implicated in diabetes and obesity, prompting attempts to discover new HSL inhibitors. Toward this end, we explored the pharmacophoric space of HSL inhibitors using four diverse sets of compounds. Subsequently, genetic algorithm and multiple linear regression analysis were employed to select optimal...

P-glycoprotein (Pgp) is implicated in multiple drug resistance (MDR) exhibited by several types of cancer against a multitude of anticancer chemotherapeutic agents. This problem prompted several research groups to search for effective P-gp inhibitors. Cyclosporine A (CsA), aureobasidin A (AbA) and related analogues were reported to possess potent i...

The pharmacophoric space of glycogen synthase kinase-3beta (GSK-3beta) was explored using two diverse sets of inhibitors. Subsequently, genetic algorithm and multiple linear regression analysis were employed to select optimal combination of pharmacophores and physicochemical descriptors that access self-consistent and predictive quantitative struct...

The pharmacophoric space of streptococcal MurF was explored using a set of 39 known inhibitors. Subsequently, genetic algorithm and multiple linear regression analysis were employed to select an optimal combination of pharmacophoric models and physicochemical descriptors that access self-consistent quantitative structure-activity relationship (QSAR...