stilbenes and Vaginosis--Bacterial

We report a turn-on tetravalent sialic acid-coated tetraphenylethene luminogen (TPE4S) with excellent hydrophilicity, good stability, high sensitivity and unique selectivity towards sialidases, and the maximum fluorescence enhancement was ∼40 fold. More importantly, TPE4S was successfully utilized for the screening of sialidase inhibitors and diagnosis of bacterial vaginosis.

Topics: Adult; Clostridium perfringens; Enzyme Inhibitors; Female; Fluorescence; Fluorescent Dyes; Fluorometry; High-Throughput Screening Assays; Humans; Hydrophobic and Hydrophilic Interactions; Kinetics; Limit of Detection; Middle Aged; N-Acetylneuraminic Acid; Neuraminidase; Oseltamivir; Sialic Acids; Stilbenes; Vaginosis, Bacterial; Vibrio cholerae; Young Adult; Zanamivir

Resveratrol (RES), chemically known as 3,5,4'-trihydroxy-trans-stilbene, is a promising multi-targeted anti-oxidative and anti-inflammatory natural polyphenol. Preclinical studies showed its biological activities against the pathogens of sexually transmitted diseases causing vaginal inflammation and infections. Due to its low solubility and poor bioavailability, the optimal therapeutic uses are limited. Therefore, a clinically acceptable topical vaginal formulation of RES exhibiting optimal therapeutic effects is highly desirable. For this purpose, we prepared and optimized chitosan-coated liposomes with RES. The coated vesicles (mean diameter 200nm) entrapped up to 77% of RES, a sufficient load to assure required therapeutic outcome. In vitro drug release study showed the ability of liposomes to provide sustained release of RES. In vitro anti-oxidative activities of RES, namely DPPH and ABTS(•+) radicals scavenging assays, confirmed RES to be as potent as standard anti-oxidants, vitamins C and E. The anti-oxidative activities of RES and its corresponding liposomal formulation were also compared by measuring enhanced superoxide dismutase (SOD) activities in lipopolysaccharide (LPS)-induced J774A.1 cells. In vitro anti-inflammatory activities were compared by measuring nitric oxide (NO), tumor necrosis factor (TNF)-α and interleukin (IL)-1β production in LPS-induced J774A.1 cells. Liposomal RES was found to exhibit stronger anti-oxidative and anti-inflammatory activities than RES solution.

Topics: Administration, Intravaginal; Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Cell Line; Female; Interleukin-1beta; Liposomes; Mice; Resveratrol; Stilbenes; Tumor Necrosis Factor-alpha; Vaginitis; Vaginosis, Bacterial

Topics: Carbohydrates; Female; Humans; Lactic Acid; Stilbenes; Vaginitis; Vaginosis, Bacterial; Vulvovaginitis