Mini Reviews in Medicinal Chemistry - Volume 19, Issue 20, 2019

Metal-Organic Frameworks (MOFs) have aroused great interest in the field of nanoscience and nanotechnology particularly in biomedical domains, such as Drug Delivery System (DDS), Biomedical Imaging (BI) and Photodynamic Therapy (PDT). As an emerging material, MOFs possess extraordinarily high surface area, controllable particle size and good biocompatibility. With extraordinary flexibility in the selection of organic and inorganic components, MOFs can rationally be tuned to obtain the materials having versatile structures and porosities. MOFs can serve as ideal vehicles for DDS, BI and PDT through modification and function. In this review, we summarized the design and synthetic strategies for preparing MOFs and introduced their recent advanced usage in DDS, BI and PDT. Finally, the prospect and future challenges of these nanomaterials are also documented.

Background: Leaves of Spinacia oleracea have been widely used as vegetarian foods. Some studies on the chemical composition of spinach have shown that it contains a high content of micronutrients (vitamins and minerals), and has an important economic value with some agronomic advantages. S. oleracea in traditional medicine is reported to cure more than one health problem. Objective: This review focuses on the ethnopharmacological uses and pharmacological and phytochemical studies of Spinacia oleracea. Methods: Information on S. oleracea was obtained via electronic search of scientific databases such as Scopus, PubMed, Google Scholar, Scirus, Science Direct, Scielo, Web of Science, Medline, Springerlink, BioMed Central (BMC), and SciFinder for publications on this plant. In addition, books on medicinal herbs were also consulted. Results: Approximately 100 chemical compounds were isolated and characterized from S. oleracea. The major active components of the plant are flavones, flavanols, methylenedioxyflavonol glucuronides, glucuronides, and carotenoids, which were extensively investigated. This review revealed potential pharmacological properties of these isolated compounds such as anti-obesity, anti-α-amylase, bileacid binding capacity, anti-mutagenic, anti-oxidant, anticancer, anti-inflammatory, cognitive and mood effect, hypoglycemic, and anti-hypertriglyceridemia. Conclusion: S. oleracea is an important edible plant also used for ethnomedical therapy of obesity, inflammation of lungs, lumbago, flatulence, and treatment of urinary calculi. Pharmacological and phytochemical studies of this plant including bioactives, which have been adequately studied, support its uses in traditional medicine. Additionally, prospects and future trends of this plant are proposed.

Many phenolic compounds found in foods and medicinal plants have shown interesting therapeutic potential and have attracted the attention of the pharmaceutical industry as promising pharmacologically active compounds in health promotion and disease prevention. Vanillin is a phenolic aldehyde, widely used as a flavoring agent in the food, pharmaceutical, and cosmetics industries. A variety of pharmacological activities has been attributed to this compound and its main metabolites, vanillic acid and vanillyl alcohol, including their anti-inflammatory ability. The relationship of the anti- inflammatory effects of vanillin, vanillic acid, and vanillyl alcohol and their actions on oxidative stress is well established. Considering that the inflammatory process is related to several pathologies, including new diseases with few therapeutic options, and limited efficiency, the search for effective treatment strategies and discovery of new anti-inflammatory agents capable of modulating inflammation becomes necessary. Therefore, in this review, we discuss the therapeutic potential of vanillin and its main metabolites for the treatment of inflammatory diseases and their actions on redox status. In addition, the molecular docking evaluation of vanillin, its metabolites and isoeugenol were carried out into the phospholipase A2 binding site.

Botulinum neurotoxins (BoNTs) are the most toxic category A biological warfare agents. There is no therapeutics available for BoNT intoxication yet, necessitating the development of a medical countermeasure against these neurotoxins. The discovery of small molecule-based drugs has revolutionized in the last two decades resulting in the identification of several small molecule inhibitors of BoNTs. However, none progressed to clinical trials. 8-Hydroxyquinolines scaffold-based molecules are important ‘privileged structures’ that can be exploited as inhibitors of a diverse range of targets. In this review, our study of recent reports suggests the development of 8-hydroxyquinoline derived molecules as a potential drug may be on the horizon.

MiRNAs play an important role in cancers. As a potent tumor suppressor, miRNA-7(miR-7) has been demonstrated to inhibit the diverse fundamental biological processes in multiple cancer types including initiation, growth and metastasis by targeting a number of molecules and signaling pathways. This current review summarizes and discusses the relationship between miR-7 and cancers and the therapeutic potential of miR-7 in cancers. It may provide new integrative understanding for future study on the role of miR-7 in cancers.

Background & Objective: A new series of thiazoles substituted on the chromene scaffold were prepared by facial approaches starting from (E)-1-(2,3-Dihydrochromen-4-ylidene)thiosemicarbazide derivatives (2a,b). The thiosemicarbazides (2a,b) were reacted with a series of α-halo carbonyl compounds to give the corresponding rhodanine analogues and reacted also with C-acetyl-or Cethoxy- N-hydrazonoyl chlorides to afford the corresponding tri- and tetra-substituted hybrid hydrazinyl thiazole substituted chromenes. Methods: The newly synthesized compounds were screened for their in vitro antimicrobial and antitumor activities by agar diffusion method and MTT assay, respectively. Results: The results of the antimicrobial activity revealed that some of the new compounds exhibited excellent activity against pathogenic microorganism; Candida albicans compared with Ciprofloxacin and nystatin, as the reference drugs. All of the tested compounds exhibited significant cytotoxic activities comparable to that of the reference drug; Doxorubicin® (on HCT116 (colorectal carcinoma human cell line).