Pseudo five-component process for the synthesis of functionalized tricarboxamides using CuI nanoparticles as reusable catalyst

An efficient and multicomponent method has been developed for the synthesis of functionalized tricarboxamides at room temperature using CuI nanoparticles as catalyst. This method involved fivecomponent coupling reactions of Meldrum's acid, isocyanides with aromatic aldehydes and amines at room temperature. Atom economy, wide range of products, excellent yields in short time and mild reaction conditions are some of the important features of this protocol. Notably, this catalyst could be recycled and reused for several times without significantly decreasing the catalytic activity.     

Genesis and Mechanism of Some Cancer Types and an Overview on the Role of Diet and Nutrition in Cancer Prevention

Cancer is a major disease with a high mortality rate worldwide. In many countries, cancer is considered to be the second most common cause of death after cardiovascular disease. The clinical management of cancer continues to be a challenge as conventional treatments, such as chemotherapy and radiation therapy, have limitations due to their toxicity profiles. Unhealthy lifestyle and poor dietary habits are the key risk factors for cancer; having a healthy diet and lifestyle may minimize the risk. Epidemiological studies have shown that a high fruit and vegetable intake in our regular diet can effectively reduce the risk of developing certain types of cancers due to the high contents of antioxidants and phytochemicals. In vitro and in vivo studies have shown that phytochemicals exert significant anticancer effects due to their free radical scavenging capacity potential. There has been extensive research on the protective effects of phytochemicals in different types of cancers. This review attempts to give an overview of the etiology of different types of cancers and assesses the role of phytonutrients in the prevention of cancers, which makes the present review distinct from the others available.     

Clinical,Nutritional, and Functional Evaluation of Chia Seed-Fortified Muffins

Health-protective functional foods are gaining popularity in the world of nutrition because they promote excellent health while decreasing pharmaceutical burdens. Chia seeds (CS) (Salvia hispanica L.), the greatest vegetative source of α-linolenic acid, bioactive proteins, and fibers, are among the top unconventional oilseeds shown to have bounteous benefits against various non-communicable diseases. Purposely, this study was designed to integrate roasted CS powder into white-flour-based ordinary bakery goods to improve their nutritional and nutraceutical profiles. CS efficacy in normal and hyperlipidemic Sprague-Dawley rats resulted in mitigating blood glucose, triglycerides, total cholesterol, and low-density lipoprotein cholesterol while elevating high-density lipoprotein cholesterol, hematocrit, hemoglobin, red blood cell counts, and platelets. The nutritional profiling of chia-fortified muffins indicated significant increases of 47% in fat, 92% in fiber, 15% in protein, and 62% in minerals. The farinographic experiments of CS-blends revealed generally improved dough quality features with a significant rise in the degree of softening as fortification levels increased. A marketable recipe for CSF-muffins with several degrees of fortification demonstrated a significant rise in fat, 92% rise in fiber, 15% rise in protein, and 62% rise in minerals. Sensorial evaluation by trained taste panelists revealed a maximum appraisal of the 15% chia-fortified muffins due to aroma, appearance, and overall acceptability, and were forwarded for being acceptable for commercialization.     

High Performance Liquid Chromatography (HPLC) with Fluorescence Detection for Quantification of Steroids in Clinical,Pharmaceutical, and Environmental Samples: A Review

Steroids are compounds widely available in nature and synthesized for therapeutic and medical purposes. Although several analytical techniques are available for the quantification of steroids, their analysis is challenging due to their low levels and complex matrices of the samples. The efficiency and quick separation of the HPLC combined with the sensitivity, selectivity, simplicity, and cost-efficiency of fluorescence, make HPLC coupled to fluorescence detection (HPLC-FLD) an ideal tool for routine measurement and detection of steroids. In this review, we covered HPLC-FLD methods reported in the literature for the steroids quantification in clinical, pharmaceutical, and environmental applications, focusing on the various approaches of fluorescent derivatization. The aspects related to analytical methodology including sample preparation, derivatization reagents, and chromatographic conditions will be discussed.     

Bursatella leachii Purple Ink Secretion Concentrate Exerts Cytotoxic Properties against Human Hepatocarcinoma Cell Line (HepG2): In Vitro and In Silico Studies

Liver cancer is a leading cause of cancer death globally. Marine mollusc-derived drugs have gained attention as potential natural-based anti-cancer agents to overcome the side effects caused by conventional chemotherapeutic drugs during cancer therapy. Using liquid chromatography-mass spectrometry, the main biomolecules in the purple ink secretion released by the sea hare, named Bursatella leachii (B. leachii), were identified as hectochlorin, malyngamide X, malyngolide S, bursatellin and lyngbyatoxin A. The cytotoxic effects of B. leachii ink concentrate against human hepatocarcinoma (HepG2) cells were determined to be dose- and time-dependent, and further exploration of the underlying mechanisms causing the programmed cell death (apoptosis) were performed. The expression of cleaved-caspase-8 and cleaved-caspase-3, key cysteine-aspartic proteases involved in the initiation and completion of the apoptosis process, appeared after HepG2 cell exposure to the B. leachii ink concentrate. The gene expression levels of pro-apoptotic BAX, TP53 and Cyclin D1 were increased after treatment with the B. leachii ink concentrate. Applying in silico approaches, the high scores predicted that bioactivities for the five compounds were protease and kinase inhibitors. The ADME and cytochrome profiles for the compounds were also predicted. Altogether, the B. leachii ink concentrate has high pro-apoptotic potentials, suggesting it as a promising safe natural product-based drug for the treatment of liver cancer.     

Synthesis and characterization of polylactides with different branched architectures

Star‐shaped and comb‐like poly(L‐Lactide)s (PLA) are produced by employing multifunctional initiators, and hyperbranched structure is prepared using a cyclic co‐monomer with hydroxyl group. FTIR, size exclusion chromatography, and H‐NMR techniques are employed to characterize the synthesized polymers, validating the formation of desired structures with chain lengths above the critical length for entanglement. After characterization of the synthesized polymers, the effect of branching on PLA properties is investigated by comparing the crystallization and rheological behavior of branched PLAs to those of a linear commercial grade. Differential scanning calorimetry and optical microscopy observations reveal a remarkable improvement in PLA crystallization due to the nucleation role of branching points. Moreover, synthesized polylactides exhibit strain hardening behavior during elongational viscosity measurements by a sentmanat extension rheometer platform. Significant improvements in crystallization and elongational rheology behavior of the synthesized polymers support the achievement of branched polymer structures. © 2015 Wiley Periodicals, Inc. J. Polym. Sci., Part B: Polym. Phys. 2015 , 53, 522–531     

Multistep Continuous‐Flow Synthesis in Medicinal Chemistry: Discovery and Preliminary Structure–Activity Relationships of CCR8 Ligands

A three‐step continuous‐flow synthesis system and its application to the assembly of a new series of chemokine receptor ligands directly from commercial building blocks is reported. No scavenger columns or solvent switches are necessary to recover the desired test compounds, which were obtained in overall yields of 49–94 %. The system is modular and flexible, and the individual steps of the sequence can be interchanged with similar outcome, extending the scope of the chemistry. Biological evaluation confirmed activity on the chemokine CCR8 receptor and provided initial structure–activity‐relationship (SAR) information for this new ligand series, with the most potent member displaying full agonist activity with single‐digit nanomolar potency. To the best of our knowledge, this represents the first published example of efficient use of multistep flow synthesis combined with biological testing and SAR studies in medicinal chemistry.     

Ultrasound-promoted Friedel-Crafts acylation of arenes and cyclic anhydrides catalyzed by ionic liquid of [bmim]Br/AlCl3

A simple and efficient method of Friedel-Crafts acylation of arenes with succinic anhydride, phthalic anhydride and glutaric anhydride under the action of 1-butyl-3-ethylimidazolium ([bmim]Br/AlCl₃ ([bmim]⁺) cation (ionic liquid) and ultrasound irradiation is presented. Thy purity of products was tested by GC-MS and their structures evaluated by IR and ¹H NMR spectroscopy.     

室温下Cu掺杂的ZnO纳米粉末催化多组分一锅法合成完全取代的茚并[1,2-b]吡啶(英文)

Cu doped ZnO nanocrystalline powder(10 mol%) has been found to be an efficient catalyst for the one‐pot multi‐component synthesis of fully substituted new indeno[1,2‐b]pyridines through a com-bination of 1,3‐indandione, propiophenone or acetophenone derivatives, aromatic aldehydes, and ammonium acetate in ethanol/H2 O at room temperature. The methodology is mild, efficient and high to excellent yielding.     

Hexadecyltrimethylammonium bromide micellization in glycine,diglycine, and triglycine aqueous solutions as a function of surfactant concentration and temperatures

Micellization behavior of hexadecyltrimethylammonium bromide (HTAB) was investigated conductometrically in aqueous solutions containing 0.02 mol kg^?1glycine (Gly), diglycine (Gly-Gly), and triglycine (Gly-Gly-Gly) as a function of surfactant concentration at different temperatures. The critical micelle concentration (CMC) of HTAB exhibits a decreasing trend as the number of carbon atoms increases from Gly to Gly-Gly-Gly, favoring the micelle formation. The values of CMC and the degree of counterion dissociation of the micelles were utilized to evaluate the standard free energy for transferring the surfactant hydrophobic chain out of the solvent to the interior of the micelle, ΔG _HP ^○ , free energy associated with the surface contributions, ΔG _S ^○ , standard free energy, ΔG _m ^○ , enthalpy, ΔH _m ^○ , and entropy, ΔS _m ^○ of micellization were also calculated. The results show that the micellization of HTAB in aqueous solutions as well as in aqueous Gly/Gly-Gly/Gly-Gly-Gly solutions is primarily governed by the entropy gain due to the transfer of the hydrophobic groups of the surfactant from the solvent to the interior part of the micelle. The CMC obtained by fluorometric method is in close agreement with those obtained conductometrically. Furthermore, decrease in the I ₁/I ₃ ratio of pyrene fluorescence intensity suggests the solubilization of the additives by the surfactant micelles and that this solubilization increases as the hydrophobicity increases from Gly to Gly-Gly-Gly.