Effect of Levels of Fertilizer Application on Vine Growth and Fruit Development of 'Kyoho' Grape Planted on a Restricted Rooting Volume

根域制限栽培のブドウ‘巨峰’に対する適切な施肥法を知るために,ベッド植えの1年生の木苗に液肥を週に1～3回与え,果実の発育段階に応じてその濃度を調節した.基肥としてナタネ粕を1樹当たり200g与えた区を対照区とした. 1.ナタネ粕区では開花期前に新梢の生育が弱まり,結実期後には新根の発育が1時停止した.N:60ppmを含む液肥を与えた区では新梢,根ともに正常に生育した.結実はいずれの区でも良好であった. 2.硬核期から液肥の濃度を1/3に下げると,副梢の生長が抑えられ,果粒の肥大と着色及び糖の蓄積が優れた.着色期から液肥の濃度を下げてもある程度同様の効果がみられた.N:60ppmの液肥を収穫期まで与えた区では,着色が劣り,酸含量も高かった.一方,ナタネ粕区では硬核期中の副梢の生長が旺盛で,果粒の肥大が悪かった. 3.落葉期の熱枝と根の窒素含量を比較したところ,液肥を与えた各区の方がナタネ粕区よりも明らかに高く,他の無機成分も同様の傾向であった. 4.以上の結果から,て‘巨峰’の根域制限栽培には発芽期前から液肥を施与し,着色期の前から窒素濃度を低くするのが適当であると考えられる

Inhibitory effects of flavonoids on human immunodeficiency virus type-I integrase

One hundred and eighty-three flavonoids were screened for their inhibitory effects on HIV-l integrase (IN) using a multiplate integration assay (MIA). Of the tested flavonoids, 6-hydroxyluteolin, scutellarein, pedalitin, scutellarin, baicalein dimer, hypolaetin, 7-O-benzyl-6-hydroxyluteolin and baicalein showed appreciable inhibition with IC_ values of 0.4, 0.6, 1.3, 1.7, 2.0, 2.1, 3.0 and 3.6 μM, respectively. The potent inhibition was observed with flavonoids having at least one pair of vicinal hydroxyl groups and the activity was highly dependent on the number of vicinal hydroxyl groups. On the other hand, the inhibitory activity tended to be decreased by replacing a hydroxyl group with one of methoxyl, acetoxyl, isopropoxyl, isopentenyl, benzyloxyl, glucuronyl and glycosyl groups. No flavanones, flavanonols and chalcones examined in this experiment showed any significant inhibitory activity. マルチプレートインテグレーション法を用いて183種のフラボノイド類のHIV-1インテグラーゼ阻害効果を検討した。これらのうち6-hydroxyluteolin, scutellarein, pedalitin, scutellarin, baicalein二量体,hypolaetin,7-O-benzyl-6-hydroxyluteolinおよびbaicaleinは強い阻害を示し,それらの50%阻害濃度はそれぞれ0.4, 0.6, 1.3, 1.7, 2.0 ,2.1 ,3.0および3.6μMであった。フラボノイド類による阻害には少なくとも一対の隣接したヒドロキシル基が必要であった。また,隣接したヒドロキシル基の数が増加するに従い,HIV-1インテダラーゼ阻害活性も上昇した。他方,ヒドロキシル基がmethoxyl基, acetoxyl基, isopropoxyl基, isopentenyl基, benzyloxyl基, glucuronyl基 及びglycosyl基に置換されると阻害活性は減少あるいは消失した。試験したフラバノン,フラバノール,カルコン類には顕著な阻害活性は認められなかった

Isospin character of low-lying states in 56Fe.

Low-lying states in {sup 56}Fe, up to an excitation energy of about 4 MeV, have been investigated by means of inelastic proton and deuteron scattering experiments at {ital E}{sub {ital p}}=65 and 400 MeV and at {ital E}{sub {ital d}}=56 MeV, respectively. Measured cross sections and analyzing powers have been compared with coupled-channels calculations using collective form factors; calculations in both the Schr{umlt o}dinger and Dirac formalisms have been carried out for the proton data. For each probe, the matrix elements have been deduced for transitions from the ground state and from the 2{sub 1}{sup +} state to six quadrupole (2{sup +}) states to one octupole (3{sub 1}{sup {minus}}) and two hexadecapole (4{sub 1}{sup +} and 4{sub 2}{sup +}) states. The obtained matrix elements and the previous values from {gamma} decay or electron inelastic scattering have been used to evaluate the isospin character of the transitions. To discuss the quadrupole mixed-symmetry states in {sup 56}Fe, the deduced neutron ({ital M}{sub {ital n}}) and proton ({ital M}{sub {ital p}}) components of the matrix elements, or equivalently the isoscalar ({ital M}{sub {ital s}}) and isovector ({ital M}{sub {ital v}}) parts, have been compared with theoretical calculations based on the neutron-proton interacting bosonmore » model and on the shell model evaluated in a full {ital f}-{ital p} configuration space. {copyright} {ital 1996 The American Physical Society.}« les

Safety and Efficacy of Dolutegravir in Treatment-Experienced Subjects With Raltegravir-Resistant HIV Type 1 Infection: 24-Week Results of the VIKING Study

Background. Dolutegravir (DTG; S/GSK1349572), a human immunodeficiency virus type 1 (HIV-1) integrase inhibitor, has limited cross-resistance to raltegravir (RAL) and elvitegravir in vitro. This phase IIb study assessed the activity of DTG in HIV-1–infected subjects with genotypic evidence of RAL resistance.Methods. Subjects received DTG 50 mg once daily (cohort I) or 50 mg twice daily (cohort II) while continuing a failing regimen (without RAL) through day 10, after which the background regimen was optimized, when feasible, for cohort I, and at least 1 fully active drug was mandated for cohort II. The primary efficacy end point was the proportion of subjects on day 11 in whom the plasma HIV-1 RNA load decreased by ≥0.7 log10 copies/mL from baseline or was <400 copies/mL.Results. A rapid antiviral response was observed. More subjects achieved the primary end point in cohort II (23 of 24 [96%]), compared with cohort I (21 of 27 [78%]) at day 11. At week 24, 41% and 75% of subjects had an HIV-1 RNA load of <50 copies/mL in cohorts I and II, respectively. Further integrase genotypic evolution was uncommon. Dolutegravir had a good, similar safety profile with each dosing regimen.Conclusion. Dolutegravir 50 mg twice daily with an optimized background provided greater and more durable benefit than the once-daily regimen. These data are the first clinical demonstration of the activity of any integrase inhibitor in subjects with HIV-1 resistant to RAL

The Activity of the Integrase Inhibitor Dolutegravir Against HIV-1 Variants Isolated From Raltegravir-Treated Adults

BackgroundDolutegravir (DTG, S/GSK1349572) is an integrase inhibitor with low nanomolar potency. Susceptibility to dolutegravir and raltegravir was determined for raltegravir-resistant clinical isolates.MethodsGenotypic and phenotypic susceptibility to integrase inhibitors was examined using 39 clinical isolate samples obtained from 18 adults who had exhibited incomplete viral suppression on a raltegravir-based regimen.ResultsOf 39 samples evaluated, 30 had genotypic and phenotypic resistance to raltegravir. All samples lacking raltegravir resistance retained complete susceptibility to dolutegravir. Of the 30 samples with genotypic evidence of raltegravir resistance, the median level of phenotypic resistance to raltegravir was high (median fold change in inhibitory concentration at 50%, &gt;81; range, 3.7 to &gt;87), while the level of resistance to dolutegravir was close to that of wild-type variants (median fold change, 1.5; range, 0.9-19.0). Longitudinal samples from 5 subjects collected during long-term failure of raltegravir revealed time-dependent general decreases in phenotypic susceptibility to raltegravir, with minimal changes in phenotypic susceptibility to dolutegravir. The median fold change to dolutegravir for isolates containing changes at G140S + Q148H, G140S + Q148R, T97A + Y143R, and N155H (thus including raltegravir signature resistance codons) were 3.75, 13.3, 1.05, and 1.37, respectively.ConclusionsDolutegravir retained in vitro activity against clinical isolates obtained from subjects who failed raltegravir-based therapy at near wild-type levels for variants containing the Y143 and N155 resistance mutations. Isolates with Q148 plus additional integrase mutations possessed a broader range of and more reduced susceptibility to dolutegravir