Molecular Analysis of the Superior Efficacy of a Dual Epidermal Growth Factor Receptor (EGFR)-DNA-Targeting Combi-Molecule in Comparison with Its Putative Prodrugs 6-Mono-Alkylamino- and 6,6-Dialkylaminoquinazoline in a Human Osteosarcoma Xenograft Model.

: ZR2002 is a dual EGFR-DNA-targeting combi-molecule that carries a chloroethyl group at the six-position of the quinazoline ring designed to alkylate DNA. Despite its good pharmacokinetics, ZR2002 is metabolized in vivo into dechlorinated metabolites, losing the DNA-alkylating function required to damage DNA. To increase the DNA damage activity in tumor cells in vivo, we compared ZR2002 with two of its 6-N,N-disubstituted analogs: "JS61", with a nitrogen mustard function at the six-position of the quinazoline ring, and "JS84", with an N-methyl group.

Prophylactic effect of resveratrol and piperine on pristane-induced murine model of lupus-like disease.

Systemic lupus erythematosus is a multisystem autoimmune disease. Apart from usual treatments, approximately 50% of lupus patients use complementary medicine. Resveratrol is a phytoalexin with various pharmacological properties.

Oxidative stress and immune complexes: Pathogenic mechanisms in pristane induced murine model of lupus.

Systemic lupus erythematosus is a systemic autoimmune inflammatory disease with a broad spectrum of clinical presentations. Mouse models play an indispensible role in understanding the disease pathology and for developing new therapeutics. This study investigated the effect of pristane administration on female BALB/c mice.

Combinatorial therapeutic effect of resveratrol and piperine on murine model of systemic lupus erythematosus.

Systemic lupus erythematosus (SLE) is a chronic multi-system inflammatory disease associated with autoantibody formation. Clinical management of lupus is associated with multiple adverse events. Resveratrol is a phytoalexin with several pharmacological properties.

Altered Tregs and oxidative stress in pregnancy associated lupus.

Aim: SLE is a systemic autoimmune disease generally affecting woman in the reproductive age. It is associated with an altered level of Tregs and oxidative stress while an increase in Tregs, and different antioxidant mechanisms to combat oxidative stress are essential for successful pregnancy. Hence, this study aims to determine the level of CD4 and CD8 Tregs and oxidative stress in pregnant lupus patients.

Resveratrol: from enhanced biosynthesis and bioavailability to multitargeting chronic diseases.

Resveratrol, a phytoalexin with a wide range of pharmacological properties is synthesised by plants in response to stress, injury, infection or UV radiations. As it is a secondary metabolite with many health promoting properties, various methods employing microorganisms and genetic manipulation of different synthetic enzymes, have been comprehensively studied to increase its production. Its rapid metabolism and low bioavailability have been addressed by the use of bio enhancers and nano-formulations.