Studies on an enzymatically synthesized antitumor polysaccharide SPR-901

An antitumor polysaccharide SPR-901 was found in a fermented broth of a kind of lactic acid bacteria isolated from rice bran. SPR-901 is a high molecular alpha-glucan and its linkages are almost linear alpha-1,6 glucosidic ones with a small amount (ca. 5%) of branches at C-3 positions. It is a highly purified alpha-glucan and it contains no protein and no inorganic salts. SPR-901 showed significant antitumor activities against murine allogeneic and syngeneic tumors by both intraperitoneal and oral administration, and enhanced carbon clearance ability in mice, while it showed no direct cytotoxicities in vitro. The mechanism of antitumor activities of SPR-901 is supposed to be a host-mediated one, and this substance is classified as one of the biological response modifiers. These properties of SPR-901 were identical to those of RON, which was obtained from rice bran, therefore we concluded that these two polysaccharides were the same substance.     

η-π allylzirconocene derivatives: preparation of steroidal side chains

(E,E) η³-π allylzirconocene derivative 7 was generated in situ under thermodynamically equilibrated conditions and subsequently reacted with acetone to give natural andlor unnatural steroidal side chains.     

Studies on the sesquiterpenoids of hypolepis punctata mett.—II : The total synthesis of hypacrone

Hypacrone (1), a new seco-illudoid, was synthesized by several steps, including a cross aldol condensation of two major moieties, a diketone (2) and a cyclopentenone derivative (11).     

Wino LSP detection in the light of recent Higgs searches at the LHC

Recent LHC data showed excesses of Higgs-like signals at the Higgs mass of around 125 GeV. This may indicate supersymmetric models with relatively heavy scalar fermions to enhance the Higgs mass. The desired mass spectrum is realized in the anomaly-mediated supersymmetry breaking model, in which the Wino can naturally be the lightest superparticle (LSP). We discuss possibilities for confirming such a scenario, particularly detecting signals from Wino LSP at direct detection experiments, indirect searches at neutrino telescopes and at the LHC.     

Tetrakis(trifluoromethanesulfonyl)propane: highly effective Brønsted acid catalyst for vinylogous Mukaiyama-Michael reaction of alpha,beta-enones with silyloxyfurans

1,1,3,3-Tetrakis(trifluoromethanesulfonyl)propane was found as an excellent Br?nsted acid catalyst for the Mukaiyama-Michael reaction of alpha,beta-enones with 2-silyloxyfurans; using beta,beta-disubstituted enones as a Michael acceptor, an excellent yield construction of quaternary carbon centers could be achieved; in addition, very low catalyst loading of Br?nsted acid was used in a range from 0.05 to 1.0 mol%.     

Distinct roles of presynaptic dopamine receptors in the differential modulation of the intrinsic synapses of medium-spiny neurons in the nucleus accumbens

Background

In both schizophrenia and addiction, pathological changes in dopamine release appear to induce alterations in the circuitry of the nucleus accumbens that affect coordinated thought and motivation. Dopamine acts principally on medium-spiny GABA neurons, which comprise 95% of accumbens neurons and give rise to the majority of inhibitory synapses in the nucleus. To examine dopamine action at single medium-spiny neuron synapses, we imaged Ca²⁺ levels in their presynaptic varicosities in the acute brain slice using two-photon microscopy.

Results

Presynaptic Ca²⁺ rises were differentially modulated by dopamine. The D1/D5 selective agonist SKF81297 was exclusively facilitatory. The D2/D3 selective agonist quinpirole was predominantly inhibitory, but in some instances it was facilitatory. Studies using D2 and D3 receptor knockout mice revealed that quinpirole inhibition was either D2 or D3 receptor-mediated, while facilitation was mainly D3 receptor-mediated. Subsets of varicosities responded to both D1 and D2 agonists, showing that there was significant co-expression of these receptor families in single medium-spiny neurons. Neighboring presynaptic varicosities showed strikingly heterogeneous responses to DA agonists, suggesting that DA receptors may be differentially trafficked to individual varicosities on the same medium-spiny neuron axon.

Conclusion

Dopamine receptors are present on the presynaptic varicosities of medium-spiny neurons, where they potently control GABAergic synaptic transmission. While there is significant coexpression of D1 and D2 family dopamine receptors in individual neurons, at the subcellular level, these receptors appear to be heterogeneously distributed, potentially explaining the considerable controversy regarding dopamine action in the striatum, and in particular the degree of dopamine receptor segregation on these neurons. Assuming that post-receptor signaling is restricted to the microdomains of medium-spiny neuron varicosities, the heterogeneous distribution of dopamine receptors on individual varicosities is likely to encode patterns in striatal information processing.     

Unexpected reactivity of the burgess reagent with thiols: synthesis of symmetrical disulfides

Reaction of the Burgess reagent with a series of aliphatic and aromatic thiols led to the corresponding symmetrical disulfides in high yields. No olefins were detected in the reactions of aliphatic thiols.