Chemical Analysis of the Sugar Moiety of Monohexosylceramide Contained in Koji, Japanese Traditional Rice Fermented with Aspergillus
Hiroshi HamajimaAyami FujikawaMikako YamashiroTakatoshi OgamiSeiichi KitamuraMasahito TsubataSei TanHaruka MatsunagaKazutaka SawadaSatoshi KumagaiNobuyuki HayashiKoji NagaoTeruyoshi YanagitaTakuji OkaSusumu MitsutakeHiroshi Kitagaki
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Abstract:
Koji, rice fermented with Aspergillus, is used for saccharification of starch contained in crops during the manufacturing of many of Japanese traditional foods and drinks. Japanese people have long eaten koji, and many beneficial substances have been reported to be contained in koji. However, there has been no report on the existence or content of galactosylceramide in koji. To address this issue, we analyzed the chemical composition of the sugar moiety of monohexosylceramide contained in koji, and elucidate that 30.3% of yellow koji is galactosylceramide, 69.7% of that is glucosylceramide, 19.2% of white koji is galactosylceramide, and 80.8% of that is glucosylceramide. This is the first report of the existence and content of galactosylceramide in koji.Keywords:
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Nine new derivatives containing plant growth regulator moietyand nitroxyl radical moiety were synthesized. Preliminary tests showed that thecompounds 14a, b, 15c, and 16 possessed in vitro inhibitory activity against P388leukemia cell.
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Abstract Silaazacycles (or azasilacycles), containing both nitrogen and silicon atoms, are appealing ring structures in the development of silicon-containing functional molecules. The development of general and efficient methods towards these motifs has therefore attracted considerable attention from synthetic chemists. This short review intends to highlight representative advances in the synthesis of five- and six-membered silaazacycles. 1 Introduction 2 Five-Membered Silaazacycles 2.1 Five-Membered Silaazacycles bearing a 1,2-N/Si Moiety 2.2 Five-Membered Silaazacycles bearing a 1,3-N/Si Moiety 3 Six-Membered Silaazacycles 3.1 Six-Membered Silaazacycles bearing a 1,2-N/Si Moiety 3.2 Six-Membered Silaazacycles bearing a 1,3-N/Si Moiety 3.3 Six-Membered Silaazacycles bearing a 1,4-N/Si Moiety 4 Conclusion
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We synthesized [2]rotaxanes with a pyrrole moiety from a [2]rotaxane with a 1,3-diynyl moiety. The conversion of the 1,3-diynyl moiety of the axle component to the pyrrole moiety was accomplished by a Cu-mediated cycloaddition of anilines. The cycloaddition reaction was accelerated when the [2]rotaxane was used as the substrate. The effect of the structure of the pyrrole moiety on the rate of the shuttling was studied.
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Abstract The structure–activity relationships of 31 xanthones were analyzed by using the ferric reducing antioxidant power (FRAP) assay to determine their electron‐transfer (ET) potential. It was proven that the ET potential of xanthones was dominated by four moieties (i.e. hydroquinone moiety, 5,6‐catechol moiety, 6,7‐catechol moiety, and 7,8‐catechol moiety) and was only slightly affected by other structural features, including a single phenolic OH group, the resorcinol moiety, the transannular dihydroxy moiety, a methoxy group, a sugar residue, an isoprenyl group, a cyclized isoprenyl group, and an isopentanol group. The results could be used to predict the ET potentials of other antioxidant xanthones.
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Hydroquinone
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Objective To develop a new series of hydroxyethylamine (HEA) BACE1 inhibitors with nitrogen heterocyclic moiety at N-terminal and find new N-terminal moiety for enhancing BACE1 inhibition activity. Methods New HEA compounds with nitrogen heterocyclic moiety at N-terminal were synthesized and evaluated as BACE1 inhibitors,with (-)-epigallocatechin-3gallate EGCG as a positive control. Results All new compounds were characterized by 1H NMR and ESI-MS. Evaluation of BACE1 inhibition activity showed that the compound Ⅰ6 with indole moiety at N-terminal had BACE1 inhibition activity. Conclusion The results suggested that the indole moiety at N-terminal interact with S2 pocket of BACE1 and be favorable for enhancing BACE1 inhibition activity, Thus, the indole moiety at N-terminal can be used as lead structure for further finding more effient BACE1 inhibitors.
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The total semi‐empirical conformational analysis of the oxytocin molecule has been carried out. It has been revealed the two main types of stable structures of cyclic moiety backbone and the great lability of the tail. The optimal spacing of cyclic moiety side chains has been found for every backbone structure. The calculation results are in good agreement with the data of physico‐chemical investigations. Among the set of stable molecule structures reported in the present study are structures with β‐turn conformation of the cyclic moiety backbone and without closer spacing of the cyclic moiety and the tail, as well as structures with closely spaced N‐ and C‐terminal parts which, however, lack β‐turn in the cyclic moiety.
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Objective:To study the inclusion complex of lactone moiety of 10-hydroxycamptothecin and SBE-β-CD for keeping its lactone moiety and improving its solubility.Methods:The formulary of the inclusion complex of 10-hydroxycamptothecin's lactone moiety and ring cleavage moiety with SBE-β-CD was calculated by computer simulation and UV spectra method,respectively.The inclusion compound was prepared by acid-base method.The solubility and stability of inclusion complex was determined by UV method.The content of lactone moiety of 10-hydroxycamptothecin was determined by HPLC method.Results:The results showed that the solubility of 10-hydroxycamptothecin was increased by 5 000 times from 0.22 μg·mL-1 to 1.01 mg·mL-1 after being included into SBE-β-CD with lactone moiety.The content of lactone moiety was increased from 63.2% to 96.8%.The inclusion complex was stable within 12 months at room temperature.Conclusion:SBE-β-CD could improve the solubility of 10-hydroxycamptothecin and keep its lactone moiety.It is feasible that SBE-β-CD could be used to improve the performance of 10-hydroxycamptothecin hydrochloride formulary.
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Hydrochloride
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