Curcumin, known for thousands of years as an Ayurvedic medicine, and popular as a spice in Asian cuisine, has undergone in recent times remarkable transformation into a drug candidate with prospective multipotent therapeutic applications. Characterized by high chemical reactivity, resulting from an extended conjugated double bond system prone to nucleophilic attack, curcumin has been shown to interact with a plethora of molecular targets, in numerous experimental observations based on spectral, physicochemical or biological principles. The collected preclinical pharmacological data support traditional claims concerning the medicinal potential of curcumin and its congeners but at the same time point to their suboptimal properties in the ADME (absorption, distribution, metabolism and excretion) area.

Fisetin is a flavonol that shares distinct antioxidant properties with a plethora of other plant polyphenols. Additionally, it exhibits a specific biological activity of considerable interest as regards the protection of functional macromolecules against stress which results in the sustenance of normal cells cytoprotection. Moreover, it shows potential as an anti-inflammatory, chemopreventive, chemotherapeutic and recently also senotherapeutic agent. In view of its prospective applications in healthcare and likely demand for fisetin, methods for its preparation and their suitability for pharmaceutical use are discussed herein.

Herein, we offer some perspective on the metamorphosis that has already begun to take place in substantial parts of the chemical industry, i.e., a switch from traditional resources such as crude oil to biomass. This change requires the workhorse of chemical reactants and petroleum refineries to be replaced with biorefineries. The present perspective offers a brief look at the manufacture and uses of furan platform chemicals (FPCs) directly available from biomass (furfural and 5-hydroxy-methylfurfural). Next, we discuss the difficulties encountered when a secondary FPC, 2,5-furandicarboxylic acid, moves from the lab to large-scale manufacture. The main purpose of the present article is to show the spectacular range of compounds that can be economically synthesized from biomass via FPCs. The fate of selected FPCs and their potential are shown herein as an example only, where many more simple or complex chemicals can be obtained. We believe that there are excellent applications of bio-based materials besides the broadly promoted manufacture of fuels and monomers. This perspective looks at the types of reactions applicable to FPCs and a variety of methods for the synthesis of chiral furans.

Benzylated glycals, unlike their acylated congeners which easily undergo allylic rearrangement, are frequently employed as reactive enol ether type substrates in a variety of electrophilic addition reactions.^1–4 Although these compounds are considered to be readily available substrates, reported procedures for their syntheses involve some steps of limited efficiency, chromatographic separations or costly reagents,^5–7 and experimental requirements not amenable for large scale preparations. In view of the recent applications of benzylated glycals to syntheses of O-glycosides,^1,2 C-glycosyl compounds,³ and β-lactams,⁴ we have undertaken a study aimed at efficient one step benzylation procedures applicable to pyranoid 1-enitols as well as to their acylated derivatives. This goal was eventually achieved by employing a catalytic phase transfer alkylation system with

The need to find new EGFR inhibitors for use in combination with radiotherapy in the treatment of solid tumors has drawn our attention to compounds derived from genistein, a natural isoflavonoid. The antiproliferative potential of synthetic genistein derivatives used alone or in combination with ionizing radiation was evaluated in cancer cell lines using clonogenic assay. EGFR phosphorylation was assessed with western blotting. Genistein derivatives inhibited clonogenic growth of HCT 116 cancer cells additively or synergistically when used in combination with ionizing radiation, and decreased EGFR activation. Our preclinical evaluation of genistein-derived EGFR inhibitors suggests that these compounds are much more potent sensitizers of cells to radiation than the parent isoflavonoid, genistein and indicate that these compounds may be useful in the treatment of colon cancer with radiation therapy.

Hydroxyapatite-based biomaterials are commonly used in surgery to repair bone damage. However, the introduction of biomaterials into the body can cause metabolic alterations, including redox imbalance. Because vitamins D3 and K (K1, MK-4, MK-7) have pronounced osteoinductive, anti-inflammatory, and antioxidant properties, it is suggested that they may reduce the adverse effects of biomaterials. The aim of this study was to investigate the effects of vitamins D3 and K, used alone and in combination, on the redox metabolism of human osteoblasts (hFOB 1.19 cell line) cultured in the presence of hydroxyapatite-based biomaterials (Maxgraft, Cerabone, Apatos, and Gen-Os). Culturing of the osteoblasts in the presence of hydroxyapatite-based biomaterials resulted in oxidative stress manifested by increased production of reactive oxygen species and decrease of glutathione level and glutathione peroxidase activity. Such redox imbalance leads to lipid peroxidation manifested by an increase of 4-hydroxynonenal level, which is known to influence the growth of bone cells. Vitamins D3 and K were shown to help maintain redox balance and prevent lipid peroxidation in osteoblasts cultured with hydroxyapatite-based biomaterials. The strongest effect was observed for the combination of vitamin D3 and MK-7. Moreover, vitamins promoted growth of the osteoblasts, manifested by increased DNA biosynthesis. Therefore, it is suggested that the use of vitamins D3 and K may protect redox balance and support the growth of osteoblasts affected by hydroxyapatite-based biomaterials.