• Raynor Juhl posted an update 4 hours, 35 minutes ago

    Results Herein, a review has been taken from the latest and more efficient halogenation protocols of flavones and isoflavones previously built cores. Selective halogenation and the greener methodologies, including enzymatic and microbial halogenations, were reported. Nevertheless, some interesting protocols that allowed the synthesis of halogenated flavone and isoflavone derivatives in specific positions using halogenated reagents were also summarized. Conclusion Halogenated flavones and isoflavones have risen as noticeable structures; however, most of the time, the synthetic procedures involve toxic reagents and harsh reaction conditions. Therefore, the development of new synthetic routes with low environmental impact is desirable.Worldwide epidemic of cancer have raised a global effort for the development and production of various anticancer drugs, which are prescribed for the treatment and control of cancer disease. Unfortunately, high potential toxicity, mutagenic and carcinogenic side effects were confirmed for most of anticancer drugs, which cause many problems for the patient even at slight dosage. At this point, thanks to their outstanding features such as high sensitivity, selectivity, and cheapness, electrochemical methods attracted much attention in development of quick, precise and reliable (bio) sensors for the monitoring anticancer drugs. Enhancement of effective surface area, acceleration of the electron transfer, reduction of the electrode passivation, electrocatalysis of the redox reactions are some fascinating properties that emerged from the nanomaterials based developed modified electrodes. Morphological control and type of nanostructures and their functionalization offer intelligent engineering of the modified elect delivery systems will be presented. Not only explaining the applications of nanomaterials in electrochemical sensors but also considering them from a different angle by investigating their use in anticancer drug delivery systems was aimed.Background Oseltamivir Phosphate (OP) is an ethyl ester prodrug prescribed for the treatment of influenza virus infection. Current marketed formulations of OP supplemented with an adverse effect observed during postmarketing surveillance. These prerequisites are sufficed by developing a sustained release Dry Powder for Inhalation (DPI). Objectives Objective of the present study was to develop OP-DPI by an innovative formulation approach comprising of Immediate (IR) and Sustained (SR) Release portions. Autophagy inhibitor Methods DPI formulation comprised of an IR and SR portions were prepared by spray drying technique using Hydroxy Propyl Methyl Cellulose (HPMC) as the rate-controlling polymer for SR portion. The spray-dried product further characterized for various pharmaco-technical, in-vitro and in-vivo parameters. Results OP-DPI showed burst release of 49% within 15 min and further sustaining the drug release up to 9 hrs. The in-vitro aerodynamic performance of OP-DPI showed maximum deposition at stage 3 and Fine Particle Dose (FPD) of 1.08 mg indicating deposition in the upper respiratory tract. Solid state characterization by DSC and XRD indicated the partial amorphization OP due to spray drying. In-vivo toxicological examination revealed no sign of inflammation, indicating the safety of the developed formulation. Accelerated stability study as per ICH guidelines displayed no significant change in the solid-state characterization and drug related performance of OP-DPI. Conclusion Prepared novel and scalable OP-DPI may have potential to overcome the problems associated with existing marketed dosage forms of OP. Further, localized drug delivery of the antiviral drug through pulmonary route might be clinically benefited in controlling the viral proliferation.Objective We aim to investigate the anticancer effects and mechanisms of icaritin against breast cancer. Materials and methods Both estrogen receptor (ER) positive breast cancer cells MCF-7 and ER-negative MDA-MB-231 cells were employed. We examined the effects of icaritin on the proliferation and migration by wound healing assay and transwell assay. Cell apoptosis and cell cycle of MCF-7 and MDA-MB-231 cells were analyzed using Flow cytometry. Cell autophagy of MCF-7 and MDA-MB-231 cells was assessed by western blotting, acridine orange staining and confocal microscopy. We also detected the expression of apoptosis related genes by western blotting. In addition, an autophagy inhibitor was used to investigate whether cytoprotective autophagy was induced. Meanwhile, an ER inhibitor was utilized to explore whether ER was involved in autophagy. Results Icaritin inhibited the proliferation and migration, and induced cell cycle arrest of both MDA-MB-231 and MCF7 cells. Icaritin significantly induced apoptosis of MDA-MB-231 cells by activating caspase-3. And icaritin stimulated autophagy in MCF-7 cells, as evidenced by increased LC3II/LC3I, enhanced p62 degradation, the accumulation of endogenous LC3 puncta formation, and the increased autophagy flux. Icaritin induced autophagy through upregulating the phosphorylation of AMPK and ULK1. Chloroquine, an autophagy inhibitor, increased icaritin-induced apoptosis and proliferation inhibition of MCF-7 cells. Meanwhile, tamoxifen, an ER inhibitor, reversed icaritin-induced autophagy and proliferation inhibition of MCF-7 cells. Conclusion Our study demonstrated that the antitumor effects of icaritin against breast cancer are related with ER, which suggested that the status of ER should be considered in clinical application of icaritin.Imidazole containing compounds have been a very much explored field since ancient times. Subsequently, it constitutes a significant moiety for the new drug development. A variety of compounds having imidazole moiety have been synthesized, evaluated and marketed for the treatment of various diseases such as antifungal, antiepileptic, ACE inhibitors and so on as shown in figure. The search for imidazole containing compounds with more selective biological potency with low side effects continue to be an active area of research in medicinal chemistry. This review is in an effort to highlight the marketed drugs with imidazole ring. The article also demonstrates the future prospective of marketed imidazoles as antifungal with potential activity targeting 14α-demethylase enzyme.