Rose Bengal (RB) is a photosensitizer (PS) used in anti-cancer and anti-bacterial photodynamic therapy (PDT). The specific excitation of this PS allows the production of singlet oxygen and oxygen reactive species that kill bacteria and tumor cells. In this review, we summarize the history of the use of RB as a PS coupled by chemical or physical means to nanoparticles (NPs). The studies are divided into PDT and PDT excited by X-rays (X-PDT), and subdivided on the basis of NP type. On the basis of the papers examined, it can be noted that RB used as a PS shows remarkable cytotoxicity under the effect of light, and RB loaded onto NPs is an excellent candidate for nanomedical applications in PDT and X-PDT.
1 April 2015 in European Journal of Medicinal Chemistry
Essential oils from the inflorescence of Cymbopogon schoenanthus and C. nervatus growing in Northern Sudan were examined for their chemical composition, antiproliferative activity against human breast carcinoma and human colon adenocarcinoma cell lines, antioxidant activity (phosphomolybdenum, antiradical, reducing power, and ferrous chelating), and enzyme inhibition activity against acetylcholinesterase butyrylcholinesterase, tyrosinase, α‐glucosidase, and α‐amylase. In silico study on the inhibition of tyrosinase and α‐amylase was also performed. Piperitone (59.1%) and isomers of para‐menthadienols (35.3%) were the main compounds in C. schoenanthus and C. nervatus oils, respectively. Oil from C. nervatus possessed higher antioxidant activity than that from C. schoenanthus except for its metal chelating ability. Both oils showed high antiproliferative activity. In silico study showed that trans‐p‐mentha‐2,8‐dien‐1‐ol and piperitone (both isomers) revealed the best docking scores for α‐amylase and tyrosinase, respectively. In conclusion, oils from these two Cymbopogon species could be new natural agents with functional properties for food, cosmetics, and pharmaceutical industries. Practical applications Recently, there is a growing tendency to replace synthetic oils by natural ones in the cosmetic, food, and pharmaceutical products. In this context, we investigated the chemical characterization and biological activities of two Cymbopogon species essential oils (C. schoenanthus (L.) Spreng. and C. nervatus). Antioxidant capacity, enzyme inhibition, and antiproliferative effects were tested for biological activities. Chemical characterization was identified by GC‐MS. Based on our findings, the Cymbopogon species may be utilized as sources of natural bioactive agents in food industries.
X-ray-induced photodynamic therapy is based on the energy transfer from a nanoscintillator to a photosensitizer molecule, whose activation leads to singlet oxygen and radical species generation, triggering cancer cells to cell death. Herein, we synthesized ultra-small nanoparticle chelated with Terbium (Tb) as a nanoscintillator and 5-(4-carboxyphenyl succinimide ester)-10,15,20-triphenyl porphyrin (P1) as a photosensitizer (AGuIX@Tb-P1). The synthesis was based on the AGuIX@ platform design. AGuIX@Tb-P1 was characterised for its photo-physical and physico-chemical properties. The effect of the nanoparticles was studied using human glioblastoma U-251 MG cells and was compared to treatment with AGuIX@ nanoparticles doped with Gadolinium (Gd) and P1 (AGuIX@Gd-P1). We demonstrated that the AGuIX@Tb-P1 design was consistent with X-ray photon energy transfer from Terbium to P1. Both nanoparticles had similar dark cytotoxicity and they were absorbed in a similar rate within the cells. Pre-treated cells exposure to X-rays was related to reactive species production. Using clonogenic assays, establishment of survival curves allowed discrimination of the impact of radiation treatment from X-ray-induced photodynamic effect. We showed that cell growth arrest was increased (35%-increase) when cells were treated with AGuIX@Tb-P1 compared to the nanoparticle doped with Gd.