Fisetin and polymeric micelles encapsulating fisetin exhibit potent cytotoxic effects towards ovarian cancer cells.

BACKGROUND: The anti-tumor activities of Natural compounds and their derivatives are of great interest to pharmaceutical industries. Fisetin is one of prospective natural compounds in this regard but unfortunately with poor hydrophilicity. METHODS: The effects of unmodified and modified fisetin in cultured ovarian cancer cells were compared by transmission electronmicroscopy to determine apoptotic bodies, MTT assay to quantitate cell numbers, and fluorescence activated cell sorting analyse of various markers to determine the apoptotic state. In addition, the efficacy of fisetin and fisetin-micelles in vivo was determined by using immunocompromised mice. Apoptosis was measured by established markers using both western blot analysis and immunochemistry. Angiogenesis in a xenograft mouse model carring SKOV3 cells was evaluated by color Doppler ultrasound and immunohistochemistry. RESULT: Multiple lines of evidence indicated that fisetin and fisetin micelles induce apoptosis in ovarian cancer cells in a dose-dependent manner. Histological analysis, terminal deoxynucleotidyltransferase-mediated nick-end labeling assay, western blot, immunohistochemical detection and microvessel density detection demonstrated that fisetin and fisetin micelles induced increased tumor apoptosis, proliferation suppression and antiangiogenesis activities. CONCLUSION: As far as we know, the present study is the first time to demonstrate the potency of both fisetin and fisetin micelles inducing apoptosis in ovarian cancer cells. Further studies will be needed to validate the therapeutic potential of fisetin and fisetin micelles in ovarian cancer treatment.

Henrin A: A New Anti-HIV Ent-Kaurane Diterpene from Pteris henryi.

Henrin A (1), a new ent-kaurane diterpene, was isolated from the leaves of Pteris henryi. The chemical structure was elucidated by analysis of the spectroscopic data including one-dimensional (1D) and two-dimensional (2D) NMR spectra, and was further confirmed by X-ray crystallographic analysis. The compound was evaluated for its biological activities against a panel of cancer cell lines, dental bacterial biofilm formation, and HIV. It displayed anti-HIV potential with an IC50 value of 9.1 µM (SI = 12.2).

Rubesanolides C-E: abietane diterpenoids isolated from Isodon rubescens and evaluation of their anti-biofilm activity.

Phytochemical study of the leaves of the medicinal plant Isodon rubescens led to the isolation of three novel abietane diterpenoids, rubesanolides C-E (1-3). These diterpenes contain a unique γ-lactone subgroup formed between C-8 and C-20. Their structures were determined from analysis of spectroscopic data, and were further confirmed by X-ray crystallographic data. The compounds were evaluated for their antibacterial activity, and rubesanolide D (2) demonstrated inhibition activity against biofilm formation of the dental bacterium Streptococcus mutans.

Immunotherapy with regulatory T and B cells in periodontitis.

Periodontitis (PD), also known as gum disease, is a condition causing inflammatory bone resorption and tooth loss. Regulatory T cells (Tregs) and regulatory B cells (Bregs) are vital in controlling the immune response and hence play a role in infections and peripheral tolerance adjustment. These cells have immunosuppressive and tissue-repairing capabilities that are important for periodontal health; however, in inflammatory circumstances, Tregs may become unstable and dysfunctional, accelerating tissue deterioration. In recent years, Regulatory cell-mediated immunotherapy has been shown to be effective in many inflammatory diseases. Considering the roles of Tregs and Bregs in shaping immune responses, this study aimed to review the published articles in this field to provide a comprehensive view of the existing knowledge about the role of regulatory T and B cells, as well as their therapeutic applications in PD.