Emerging Biomedical Applications of Algal Polysaccharides.

BACKGROUND: Over the past two decades, there have been substantial progress and a growing body of research on using natural polymeric biomaterials in emerging biomedical applications. Among different natural biopolymers, polysaccharides have gained considerable attraction among biomedical scientists and surgeons due to their biocompatibility, biodegradability, anti-inflammatory, and antimicrobial properties. In recent years, algalbased polysaccharides including agar, alginate, and carrageenan, have been broadly suggested for different biomedical applications. METHODS: The aim of this paper is discussing various possible applications of algal-based polysaccharides in biomedical engineering particularly in controlled drug delivery systems. The main properties of each algal polysaccharide will be discussed, and particular drug delivery applications will be presented. RESULTS: Algal polysaccharides can be detected in a group of photosynthetic unite as their key biomass constituents. They provide a range of variety in their size, shape, liquefaction, chemical stability, and crosslinking ability. In addition, algal polysaccharides have shown exceptional gelling properties including stimuli-responsive behavior, softness, and swelling properties. CONCLUSION: All the mentioned properties of alga polysaccharides lead to their successful usage in biomedical applications specially targeted and controlled drug delivery systems such as particles, capsules, and gels.

Synthesis and antibacterial activity of novel levofloxacin derivatives containing a substituted thienylethyl moiety.

BACKGROUND AND THE PURPOSE OF THE STUDY: Piperazinyl quinolones such as ciprofloxacin, ofloxacin and levofloxacin are an important group of quinolone antimicrobials which are widely used in the treatment of various infectious diseases. In the present study, we synthesized a new series of levofloxacin derivatives and evaluated their antibacterial activities. METHODS: The N-substituted analogs of levofloxacin 6a-j were prepared by nucleophilic reaction of N-desmethyl levofloxacin 11 with thienylethyl bromide derivatives 8 or 9. All target compounds were tested using conventional agar dilution method in comparison to levofloxacin and N-desmethyl levofloxacin and their MIC values were determined against a panel of Gram-positive and Gram-negative bacteria. RESULTS: All compounds showed significant antibacterial activities against Gram-positive bacteria (MIC = 0.04-6.25 µg/mL); however, the activity against Gram-negative bacteria was lower (MIC = 1.56-100 µg/mL). As is evident from the data, oxime derivatives 6e, 6h and 6i are superior in inhibiting the growth of Gram-positive bacteria (MIC = 0.04-0.19 µg/mL), and their activities were found to be 5-25 times better than N-desmethyl levofloxacin 11 and equal or better than levofloxacin 4. CONCLUSION: We have designed and synthesized novel quinolone derivatives bearing functionalized thienylethyl moiety on the piperazine ring of levofloxacin. The results of antibacterial screening against Gram-positive and Gram-negative bacteria revealed that the introduction of functionalized thienylethyl moiety on the piperazine ring of levofloxacin can improve the activity against Gram-positive bacteria. Gram-positive bacteria are responsible for a wide range of infectious diseases, and rising resistance in this group is causing increasing concern. Thus, this study introduces structural features of levofloxacin scaffold for development of new candidates in the field of anti-Gram positive chemotherapy.