サイエンスショップ イナガワ モガワ プロジェクト チュカン ホウコク

第2 部 コミュニケーションデザイン論集論文・実践報

サイエンス ショップ ノ キョウイクテキ イギ ショート ターム リサーチ ノ シンチョク ジョウキョウ

第2 部 コミュニケーションデザイン論集論文・実践報

Antitumor agents 270. Novel substituted 6-phenyl-4H-furo[3,2-c]pyran-4-one derivatives as potent and highly selective anti-breast cancer agents

6-Phenyl-4H-furo[3,2-c]pyran-4-one derivatives based on neo-tashinlactone (1) were synthesized and evaluated as novel anti-breast cancer agents. Compounds 10-13, 23, 25, and 27 showed potent inhibition against the SK-BR-3 breast cancer cell line. Importantly, 25 and 27 showed the highest cancer cell line selectivity, being approximately 100- to 250-fold more potent against SK-BR-3 (ED50 0.28 and 0.44 μM, respectively) compared with other cancer cell lines tested. In addition, 25 displayed low cytotoxicity against normal breast cell lines 184A1 and MCF10A. Compounds 25 and 27 merit further investigation in our continuing program to generate and develop selective anti-breast cancer agents

Antitumor agents. 258. Syntheses and evaluation of dietary antioxidant—taxoid conjugates as novel cytotoxic agents

Various dietary antioxidants, including vitamins, flavonoids, curcumin, and a coumarin, were conjugated with paclitaxel (1) through an ester linkage. The newly synthesized compounds were evaluated for cytotoxic activity against several human tumor cell lines as well as the corresponding normal cell lines. Interestingly, most tested conjugates selectively inhibited the growth of 1A9 (ovarian) and KB (nasopharyngeal) tumor cells without activity against other cell lines. Particularly, conjugates 16 and 20 were highly active against 1A9 (ED50 value of 0.005 μg/mL) as well as KB (ED50 values of 0.005 and 0.14 μg/mL, respectively) cells. Compound 22b, the glycinate ester salt of vitamin E conjugated with 1, appears to be a promising lead for further development as a clinical trial candidate as it exhibited strong inhibitory activity against Panc-1 (pancreatic cancer) with less effect on the related E6E7 (normal) cell line

Complete Genetic Correction of iPS Cells From Duchenne Muscular Dystrophy

Human artificial chromosome (HAC) has several advantages as a gene therapy vector, including stable episomal maintenance that avoids insertional mutations and the ability to carry large gene inserts including the regulatory elements. Induced pluripotent stem (iPS) cells have great potential for gene therapy, as such cells can be generated from the individual's own tissues, and when reintroduced can contribute to the specialized function of any tissue. As a proof of concept, we show herein the complete correction of a genetic deficiency in iPS cells derived from Duchenne muscular dystrophy (DMD) model (mdx) mice and a human DMD patient using a HAC with a complete genomic dystrophin sequence (DYS-HAC). Deletion or mutation of dystrophin in iPS cells was corrected by transferring the DYS-HAC via microcell-mediated chromosome transfer (MMCT). DMD patient- and mdx-specific iPS cells with the DYS-HAC gave rise to differentiation of three germ layers in the teratoma, and human dystrophin expression was detected in muscle-like tissues. Furthermore, chimeric mice from mdx-iPS (DYS-HAC) cells were produced and DYS-HAC was detected in all tissues examined, with tissue-specific expression of dystrophin. Therefore, the combination of patient-specific iPS cells and HAC-containing defective genes represents a powerful tool for gene and cell therapies

Use of Human Senses as Sensors

This paper is an overview of our recent findings obtained by the use of human senses as sensors, suggesting that human senses might be indispensable sensors, not only for practical uses but also for gaining a deeper understanding of humans. From this point of view, two kinds of studies, both based on semantic responses of participants, deserve emphasis. One study assessed the efficacy of the photocatalytic elimination of stains or bio-aerosols from an air environment using TiO2 as well as the photocatalytic deodorizing efficacy of a TiO2-type deodorizer; the other study evaluated the changes in perception of a given aroma while inhaling the fragrance of essential oils. In the latter study, we employed a sensory test for evaluating changes in perception of a given aroma. Sensory tests were conducted twice, when participants were undergoing the Kraepelin mental performance test (mental arithmetic) or an auditory task (listening to environmental natural sounds), once before the task (pre-task) and once after the task (post-task). The perception of fragrance was assessed by 13 contrasting pairs of adjectives as a function of the task assigned to participants. The obtained findings illustrate subtle nuances regarding how essential oils manifest their potency and how olfactory discrimination and responses occur in humans

Antitumor Agents. 282. 2′-( R )- O -Acetylglaucarubinone, a Quassinoid from Odyendyea gabonensis As a Potential Anti-Breast and Anti-Ovarian Cancer Agent

A new quassinoid, designated 2′-(R)-O-acetylglaucarubinone (1), and seven known quassinoids (2–8) were isolated, using bioactivity-guided separation, from the bark of Odyendyea gabonensis (Pierre) Engler [syn. Quassia gabonensis Pierre (Simaroubaceae)]. The structure of 1 was determined by spectroscopic analysis, and by semi-synthesis from glaucarubolone. Complete 1H and 13C NMR assignments of compounds 1–8 were also established from detailed analysis of two-dimensional NMR spectra, and the reported configurations in odyendene (7) and odyendane (8) were corrected. Compound 1 showed potent cytotoxicity against multiple cancer cell lines. Further investigation using various types of breast and ovarian cancer cell lines suggested that 1 does not target the estrogen receptor (ER) or progesterone receptor (PR). When tested against mammary epithelial proliferation in vivo using a Brca1/p53-deficient mice model, 1 also caused significant reduction in mammary duct branching