ABSTRACT
Recently, there has been much effort to find effective ingredients which can prevent or retard cutaneous skin aging after topical or systemic use. Here, we investigated the effects of the atomic hydrogen surrounded by water molecules, H(H2O)m, on acute UV-induced responses and as well as skin aging. Interestingly, we observed that H(H2O)m application to human skin prevented UV-induced erythema and DNA damage. And H(H2O)m significantly prevented UV-induced MMP-1, COX-2, IL-6 and IL-1ß mRNA expressions in human skin in vivo. We found that H(H2O)m prevented UV-induced ROS generation and inhibited UV-induced MMP-1, COX-2 and IL-6 expressions, and UV-induced JNK and c-Jun phosphorylation in HaCaT cells. Next, we investigated the effects of H(H2O)m on intrinsically aged or photoaged skin of elderly subjects. In intrinsically aged skin, H(H2O)m application significantly reduced constitutive expressions of MMP-1, IL-6, and IL-1ß mRNA. Additionally, H(H2O)m significantly increased procollagen mRNA and also decreased MMP-1 and IL-6 mRNA expressions in photoaged facial skin. These results demonstrated that local application of H(H2O)m may prevent UV-induced skin inflammation and can modulate intrinsic skin aging and photoaging processes. Therefore, we suggest that modifying the atmospheric gas environment within a room may be a new way to regulate skin functions or skin aging.
Subject(s)
Gene Expression Regulation/drug effects , Gene Expression Regulation/radiation effects , Hydrogen/pharmacology , Skin Aging/genetics , Skin/metabolism , Ultraviolet Rays/adverse effects , Age Factors , Cell Line, Transformed , Cyclooxygenase 2/genetics , Cyclooxygenase 2/metabolism , Environmental Exposure , Enzyme Activation/drug effects , Enzyme Activation/radiation effects , Erythema/etiology , Erythema/prevention & control , Humans , Interleukin-1beta/genetics , Interleukin-1beta/metabolism , Interleukin-6/genetics , Interleukin-6/metabolism , MAP Kinase Kinase 4/metabolism , Matrix Metalloproteinase 1/genetics , Matrix Metalloproteinase 1/metabolism , Phosphorylation/drug effects , Phosphorylation/radiation effects , Procollagen/genetics , Procollagen/metabolism , Proto-Oncogene Proteins c-jun/metabolism , Reactive Oxygen Species/metabolism , Skin Aging/drug effects , Skin Aging/radiation effects , Thymidine/chemistry , Thymidine/radiation effects , Water/chemistryABSTRACT
6-Arylamino-phthalazine-5,8-diones and 6,7-bis(arylthio)-phthalazine-5,8-diones were synthesized and tested for in vitro antifungal activity against two pathogenic strains of fungi. Among those tested, many compounds showed good antifungal activity. The results suggest that phthalazine-5,8-diones would be potent antifungal agents.
Subject(s)
Antifungal Agents/chemical synthesis , Chemistry, Pharmaceutical/methods , Phthalazines/chemistry , Phthalazines/chemical synthesis , Antifungal Agents/pharmacology , Candida/metabolism , Candida albicans/metabolism , Drug Design , Inhibitory Concentration 50 , Microbial Sensitivity Tests , Models, Chemical , Molecular Conformation , Molecular Structure , Structure-Activity RelationshipABSTRACT
1H-Indole-4,7-diones were synthesized and tested for in vitro antifungal activity against fungi. The synthesized 1H-indole-4,7-diones generally showed good antifungal activity against Candida krusei, Cryptococcus neoformans, and Aspergillus niger. The results suggest that 1H-indole-4,7-diones would be potent antifungal agents.
Subject(s)
Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Indoles/chemistry , Indoles/pharmacology , Mitosporic Fungi/drug effects , Antifungal Agents/chemical synthesis , Indoles/chemical synthesisABSTRACT
A novel atmospheric pressure plasma device releasing atomic hydrogen has been developed. This device has specific properties such as (1) deactivation of airborne microbial-contaminants, (2) neutralization of indoor OH radicals and (3) being harmless to the human body. It consists of a ceramic plate as a positive ion generation electrode and a needle-shaped electrode as an electron emission electrode. Release of atomic hydrogen from the device has been investigated by the spectroscopic method. Optical emission of atomic hydrogen probably due to recombination of positive ions, H+(H2O)n, generated from the ceramic plate electrode and electrons emitted from the needle-shaped electrode have been clearly observed in the He gas (including water vapour) environment. The efficacy of the device to reduce airborne concentrations of influenza virus, bacteria, mould fungi and allergens has been evaluated. 99.6% of airborne influenza virus has been deactivated with the operation of the device compared with the control test in a 1 m3 chamber after 60 min. The neutralization of the OH radical has been investigated by spectroscopic and biological methods. A remarkable reduction of the OH radical in the air by operation of the device has been observed by laser-induced fluorescence spectroscopy. The cell protection effects of the device against OH radicals in the air have been observed. Furthermore, the side effects have been checked by animal experiments. The harmlessness of the device has been confirmed.
ABSTRACT
A series of 5-arylamino-6-chloro-1H-indazole-4,7-diones were synthesized and evaluated for their inhibitory activity on protein kinase B/Akt. The compounds exhibited a potent Akt1 inhibitory activity. Further mechanistic study revealed that they might have dual inhibitory effects on both activity and phosphorylation of Akt1 in PC-3 tumor cell line.
Subject(s)
Chlorine/chemistry , Indazoles/chemistry , Indazoles/pharmacology , Protein Kinase Inhibitors/chemical synthesis , Protein Kinase Inhibitors/pharmacology , Proto-Oncogene Proteins c-akt/antagonists & inhibitors , Amination , Animals , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Antineoplastic Agents/therapeutic use , Catalysis , Cell Line, Tumor , Glycogen Synthase Kinase 3/metabolism , Glycogen Synthase Kinase 3 beta , Humans , Indazoles/chemical synthesis , Mice , Mice, Nude , Molecular Structure , Neoplasms/drug therapy , Neoplasms/pathology , Phosphorylation/drug effects , Protein Kinase Inhibitors/chemistry , Proto-Oncogene Proteins c-akt/metabolism , Structure-Activity Relationship , Xenograft Model Antitumor AssaysABSTRACT
5-Arylamino-1H-benzo[d]imidazole-4,7-diones were synthesized and tested for their inhibitory activities on the proliferation of human umbilical vein endothelial cells (HUVECs) and the smooth muscle cells (SMCs). Among them, several 1H-benzo[d]imidazole-4,7-diones exhibited the selective antiproliferative activity on the HUVECs. Further mechanistic study revealed that the inhibitory effect of one representative 1H-benzo[d]imidazole-4,7-dione 2b on HUVEC proliferation was mediated by the activation of p38 signaling pathway in the HUVECs.
