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Aim: Currently, no information regarding the sennosides A and B content is provided on bofutsushosan extract products for ethical use. In this study, sennosides A and B in bofutsushosan extract products from eight different pharmaceutical companies and those in bofutsushosan decoction were quantitatively analyzed. Additionally, since it has been reported that sennoside A is unstable to heat, the relationship between the different decoction times of Rhubarb and the total extracted amounts of sennosides A and B was investigated. Finally, nuclear magnetic resonance (NMR)‐based metabolomics analysis was performed on Rhubarb extracts to evaluate the variability in the quality of Rhubarb. Methods: Solutions of bofutsushosan extract products, bofutsushosan decoction, and Rhubarb decoction were subjected to solid‐phase extraction, and then were analyzed using HPLC. The five Rhubarb extracts prepared from five different lots were subjected to NMR‐based metabolomics analysis. Results: The quantities of sennosides A and B varied among the bofutsushosan extract products, with a maximum interproduct variation of approximately five‐fold. Sennosides A and B were not significantly unstable to heat up to 60 min. The five Rhubarb samples were classified into three independent clusters. Conclusion: It is recommended that the quantities of sennosides A and B in Kampo extract products, including Rhubarb, be described in the package insert. When preparing Rhubarb‐containing Kampo medicines, sennosides A and B decomposition can be ignored for decoction times of up to 60 min. Further studies on the biological activity of secondary metabolites other than sennosides A and B are necessary for Rhubarb quality control. [ABSTRACT FROM AUTHOR]

The total synthesis of catunaregin in both racemic and optically active forms was accomplished. The enantioselective synthesis uses the Evans aldol strategy, with an oxazolidinone or thiazolidinethione as the chiral auxiliary. The key features include a syn‐selective aldol reaction to form the Evans‐syn or non‐Evans‐syn product, and a successive ketalization reaction of a furanyl diol derivative under acidic conditions. The biological properties of the synthetic racemate and both enantiomers were evaluated against A549 and HL‐60 human cancer cells. [ABSTRACT FROM AUTHOR]

Actin fibers (F-actin) control the shape and internal organization of cells, and generate force. It has been long appreciated that these functions are tightly coupled, and in some cases drive cell behavior and cell fate. The distribution and dynamics of F-actin is different in cancer versus normal cells and in response to small molecules, including actin-targeting natural products and anticancer drugs. Therefore, quantifying actin structural changes from high resolution fluorescence micrographs is necessary for further understanding actin cytoskeleton dynamics and phenotypic consequences of drug interactions on cells. We applied an artificial neural network algorithm, which used image intensity and anisotropy measurements, to quantitatively classify F-actin subcellular features into actin along the edges of cells, actin at the protrusions of cells, internal fibers and punctate signals. The algorithm measured significant increase in F-actin at cell edges with concomitant decrease in internal punctate actin in astrocytoma cells lacking functional neurofibromin and p53 when treated with three structurally-distinct anticancer small molecules: OSW1, Schweinfurthin A (SA) and a synthetic marine compound 23'-dehydroxycephalostatin 1. Distinctly different changes were measured in cells treated with the actin inhibitor cytochalasin B. These measurements support published reports that SA acts on F-actin in NF1−/− neurofibromin deficient cancer cells through changes in Rho signaling. Quantitative pattern analysis of cells has wide applications for understanding mechanisms of small molecules, because many anti-cancer drugs directly or indirectly target cytoskeletal proteins. Furthermore, quantitative information about the actin cytoskeleton may make it possible to further understand cell fate decisions using mathematically testable models. Published 2014 Wiley Periodicals Inc. [ABSTRACT FROM AUTHOR]

ABSTRACT Aim Our pilot clinical study suggested that nobiletin-rich Citrus reticulata peel, also known as nchinpi, has the potential to be beneficial as a kampo medicine for Alzheimer's disease. The nchinpi extract has a high content of polymethoxyflavones, including nobiletin and sinensetin. Our previous pharmacological study using cultured hippocampal neurons showed that the nchinpi extract more potently facilitated cAMP-response element ( CRE)-mediated transcription associated with long-term memory formation than did nobiletin alone, via a mechanism in which nobiletin and four other polymethoxyflavones, one being sinensetin, a potently CRE-mediated transcription-facilitating substance, cooperated. It remained unclear, however, whether nchinpi could be more effective in vivo in preventing memory deficits than could nobiletin alone. Here, we compared the impacts of the respective samples on N-methyl- D-aspartate receptor antagonism-induced learning and memory disability. Methods The nchinpi extract or nobiletin was orally given to mice for 7 consecutive days to examine their respective impacts on this impairment on contextual fear conditioning test. In a separate analysis, sinensetin's impact was evaluated. Results Nchinpi extract at a dose corresponding to that of 25 mg/kg/day nobiletin prevented impaired memory formation, whereas nobiletin failed to exhibit such beneficial effects even when given at 50 mg/kg/day. Oral sinensetin prevented memory deficits at 25 mg/kg/day, unlike nobiletin. Conclusion Nchinpi acting in a multicomponent drug-like fashion in vitro has an obvious advantage over nobiletin alone in the ability to prevent memory dysfunction in animals as well and, hence, might be beneficial in patients with dementia. [ABSTRACT FROM AUTHOR]