Phloretin,as a Potent Anticancer Compound: From Chemistry to Cellular Interactions

Phloretin is a natural dihydrochalcone found in many fruits and vegetables, especially in apple tree leaves and the Manchurian apricots, exhibiting several therapeutic properties, such as antioxidant, antidiabetic, anti-inflammatory, and antitumor activities. In this review article, the diverse aspects of the anticancer potential of phloretin are addressed, presenting its antiproliferative, proapoptotic, antimetastatic, and antiangiogenic activities in many different preclinical cancer models. The fact that phloretin is a planar lipophilic polyphenol and, thus, a membrane-disrupting Pan-Assay Interference compound (PAIN) compromises the validity of the cell-based anticancer activities. Phloretin significantly reduces membrane dipole potential and, therefore, is expected to be able to activate a number of cellular signaling pathways in a non-specific way. In this way, the effects of this minor flavonoid on Bax and Bcl-2 proteins, caspases and MMPs, cytokines, and inflammatory enzymes are all analyzed in the current review. Moreover, besides the anticancer activities exerted by phloretin alone, its co-effects with conventional anticancer drugs are also under discussion. Therefore, this review presents a thorough overview of the preclinical anticancer potential of phloretin, allowing one to take the next steps in the development of novel drug candidates and move on to clinical trials.     

High-performance thin-layer chromatographic standardization and quantification of marker compounds in an Ayurvedic polyherbal formulation: Krishnadi Churna

JPC – Journal of Planar Chromatography – Modern TLC - The present era is witnessed by the increasing demand for herbal medicine. Therefore, the preparation of herbal drugs is warranted...     

Quinoline Carbonitriles as Novel Inhibitors for N80 Steel Corrosion in Oil-Well Acidizing: Experimental and Computational Insights

Russian Journal of Electrochemistry - Three quinoline derivatives as corrosion inhibitors for N80 steel 15% HCl solutions. Influence of the –H, –OCH3 groups and the introduction of...     

The precipitation of alkaline-earth metal and transition metal oxalates from aqueous solution. Induction periods and nucleation rates

The precipitation of magnesium, calcium, strontium and barium oxalates and of manganous, ferrous, cobalt, nickel and copper oxalates was studied from equivalent aqueous solutions at 22°C: the initial overall concentrations (C) generally varied from 0.001 to 0.2 M and the saturation ratios (S_mox) varied from <10 to >3000. The induction periods before the main growth surge were measured and nucleation rates were determined from final crystal numbers and induction periods. Precipitation occurred through homogenous nucleation: the critical nuclei in supersaturated alkaline-earth metal oxalate solutions were formed by aggregation of 6–8 M⁺⁺Ox⁻ ion-pairs while the critical nuclei in supersaturated transition metal oxalate solutions were formed by aggregation of 6–8 MOx complexes (to units of 3–4 M⁺⁺MOx₂⁻ ion-pairs). Over the range studied, the nucleation rates then varied with saturation ratios according to the relation, Nucleation rates at any saturation ratio decreased in the order Mg > Sr, Ba > Ca and Fe > Mn > Co, Cu > Ni; that is, generally in the order of increasing M⁺⁺–Ox⁻ and M⁺⁺–MOx₂⁻ bond strengths and increasing surface energies of the metal oxalate crystals. Induction periods decreased with increasing-concentration and saturation ratio; over The factors t _C1 and t _S1 depended in turn on the ‘rate constants’ for nucleation and growth during the induction periods and on metal oxalate solubilities.     

Synthesis and self aggregation properties of ester-functionalized heterocyclic pyrrolidinium surfactants

Linear fatty alcohols on reaction with chloro/bromo acetic acid in the presence of catalytic amount of p-toluene sulphonic acid monohydrate under solvent-free conditions are converted into alkyl-2-haloacetate which on reaction with N-methyl pyrrolidine gives ester-functionalized pyrrolidinium surfactants. Thus, new series of ester-functionalized heterocyclic pyrrolidinium head group containing cationic surfactants have been synthesized by green approach via energy saving and cost effective methodology. These new surfactants have been investigated for their surface properties by surface tension, conductivity, and fluorescence method. Surface properties of these surfactants have been found to be far better compared to conventional heterocyclic cationic surfactants having similar hydrophobic alkyl chain length.     

Chemical composition and antimicrobial activity of the inflorescence essential oil of Capillipedium parviflorum (R. Br.) Stapf. from India

Essential oil isolated from the inflorescences of Capillipedium parviflorum (R. Br.) Stapf., collected from Kumaon region of Western Himalaya, India, was investigated by GC and GC-MS. A total of 45 constituents representing 99.0% of the essential oil were identified. The major components of this oil were 4-undecanone (33.2%), 4-undecanol (29.7%), 4-nonanol (13.9%), α-muurolol (5.3%), 4-tridecanone (3.6%), methyl-2-oxo-nonanoate (3.1%), trans-2-hexenyl butanoate (1.1%) and 1-tetradecanol (1.0%). The antimicrobial activity of the essential oil was determined against eight Gram-positive and Gram-negative bacterial strains, as well as two fungal strains. The bioassay showed that the essential oil possessed good antibacterial activity.     

Synthesis of Pyrazole Derivatives Possessing Anticancer Activity: Current Status

Pyrazole is a versatile lead compound to design potent bioactive molecules for drug discovery and development, particularly in cancer therapy. The aim of this review is to present the most recent deeds in the field of synthetic route made for functionalized pyrazole derivatives active against cell proliferation disease. The review article covers the synthesis of 1H-pyrazole, synthesis of N-substituted pyrazoles, synthesis of pyrazolopyrazoles, and synthesis of pyrazoles fused with a naturally occurring moiety. Some of these reported compounds have passed the preclinical or initial-phase clinical trials for their anticancer activity.