Insect antifeedant activity of flavones and chromones against Spodoptera litura

The antifeedant polymethylated flavones 5-hydroxy-3,6,7,8,4'-heptamethoxyflavone, 5-hydroxy-3,6,7,8-tetramethoxyflavone, and 5,6-dihydroxy-3,7-dimethoxyflavone have been isolated from the cudweed, Gnaphalium affine D. Don (Compositae). These flavonoids and authentic analogues showed insect antifeedant activity against the common cutworm (Spodoptera litura F.). In a previous paper, it was suggested that there was no substituent on the B-ring of the flavonoid for the beneficial antifeedant activity against the common cutworm. These flavonoids having a phenyl group as the B-ring and the chromone as elimination of the B-ring from the flavonoids were used to test the hypothesis of the previously described B-ring effect. The known fact is that Sculletaria baicarensis (Rutaceae) produced the 2-phenyl flavone. Test compounds and their methylated derivatives were prepared from this material for the structure-activity relationship (SAR) study of insect antifeedant activity. In spite of the 2-phenyl flavonoids, some tested compounds did not show any insect antifeedant activity against the common cutworm, although these inactive flavonoids were deficient in the 6-substituent group on the A-ring of the flavonoid. This 6-position-substituted derivative almost showed strong insect antifeedant activity against common cutworm. Moreover, the tested flavonoids having a hydroxyl group as a substituent on any of the positions tended to increase the activity. These results suggested the importance of the 6-position substitution on the flavonoid; however, hydrophilic substituents decreased the activity. Baicalein (5,6,7-trihydroxyflavone) derivatives did not show any activity despite having the 6-substituent derivative. Although the activity of some chromones increased the activity of the flavone, the bulky B-ring was a disadvantage for the antifeedant activity. It was suggested that the charge on C(3) and C(5) of the flavonoid was important for the biological activity. Additionally, an adequate hydrogen bonding property, which is different from lipophilicity, was an advantage for the activity on the basis of a QSAR analysis.     

Inhibitory actions of several natural products on proliferation of rat vascular smooth muscle cells induced by Hsp60 from Chlamydia pneumoniae J138

Atherosclerosis is a vascular disorder involving inflammation, a narrowed vascular lumen in the entire tunica intima, and reduced elasticity of the arterial wall. It has been found that Hsp60 from Chlamydia pneumoniae, an obligate bacterial pathogen associated with atheroma lesions, mimics human Hsp60, thereby causing attacks by immune cells on stressed endothelial cells expressing endogenous Hsp60 on their surface. Furthermore, Hsp60 from C. pneumoniae has been shown to promote the growth of vascular smooth muscle cells (VSMCs). To explore probes that can be used for studying signal transduction elicited by the chlamydial Hsp60, we have tested several natural products for their inhibitory actions on the Hsp60-induced proliferation of rat arterial smooth muscle cells. Sesamol, vanillyl alcohol, and trans-ferulic acid exhibited moderate inhibitory actions on the Hsp60-induced cell proliferation; zerumbone, humulene, and caryophylene effectively inhibited it at low concentrations with IC(50) values of 529, 122, and 110 nM, respectively. The results indicated that the 11-membered alicyclic ring is favorable for interactions with receptors involved in the Hsp60-induced VSMC proliferation.     

Temporal change in spatial variability of soil respiration on a slope of Japanese cedar (Cryptomeria japonica D. Don) forest

Although information regarding the spatial variability of soil respiration is important for understanding carbon cycling and developing a suitable sampling design for estimating average soil respiration, it remains relatively understudied compared to temporal changes. In this study, soil respiration was measured at 35 locations by season on a slope of Japanese cedar forest in order to examine temporal changes in the spatial distribution of soil respiration. Spatial variability of soil respiration varied between seasons, with the highest coefficient variation in winter (42%) and lowest in summer (26%). Semivariogram analysis and kriged maps revealed different patterns of spatial distribution in each season. Factors affecting the spatial variability were relief index (autumn), soil hardness of the A layer (winter), soil hardness at 50 cm depth (spring) and the altitude and relief index (summer). Annual soil respiration (average: 39 mol m⁻² y⁻¹) varied from 26 mol m⁻² y⁻¹ to 55 mol m⁻² y⁻¹ between the 35 locations and was higher in the upper part of the slope and lower in the lower part. The average Q₁₀ value was 2.3, varying from 1.3 to 3.0 among the locations. These findings suggest that insufficient information on the spatial variability of soil respiration and imbalanced sampling could bias estimates of current and future carbon budgets.     

Relationship between trace elements status in mane hair and atrial fibrillation in horse

To investigate the relationships between trace elements concentrations in hair and atrial fibrillation (AF) in horses, concentrations of nineteen trace elements were detected in hair using the particle induced X-ray emission (PIXE) method. The horses were assigned to either control (n=22, no abnormalities) or AF groups (n=5) based on electrocardiograph findings. The mean concentrations of Ca and Zn in the hair of the AF group were significantly higher than those in the control group. The Zn/Cu ratio of the hair in the AF group (29.8 +/- 5.5) was significantly higher than that in the control group (23.4 +/- 2.2, P<0.05). The results of the present study suggest that there is a relationship between elevated concentrations of Ca and Zn in hair and AF.     

Synthesis and insect antifeedant activity of aurones against Spodoptera litura larvae

A series of aurones were prepared from various phenols via phenoxy acetic acids and coumaranones and evaluated for insect antifeedant activity against the common cutworm (Spodoptera litura). The naturally occurring aurone was most active at an ED50 of 0.12 micromol/cm2. The synthetic precursor, coumaranones, showed that the introduction of methoxyl and methyl groups to the benzene ring increased insect antifeedant activity. Similarly, the tested aurones showed that the introduction of methoxyl group to the A and/or B rings increased the insect antifeedant activity, but 4,5,6- and 3',4',5'-trisubstituted compounds did not show this activity in this test. The hydroxylation of aurones in the B ring should be disadvantageous for insect antifeedant activity against S. litura. Although the melting points did not correlate well with the insect antifeedant activity, compounds that were nearly inactive had high melting points. A significant correlation was noted between biological activity (pED50) and a hydrogen-bonding parameter calculated from the Rf value obtained from SiOH thin-layer chromatography and a lipophilicity parameter (log k) calculated from the retention time in ODS high-performance liquid chromatography. The respective correlation coefficients (r) were -0.83 and -0.70. The introduction of alkoxy and alkyl groups along with adequate hydrogen bonding seems to contribute to the antifeedant activity of the compounds tested.     

Effect of iron-quercetin complex on reduction of nitrite in in vitro and in vivo systems

This study investigated whether reducing agents such as quercetin and iron(II) facilitate formation of nitric oxide (NO) gas from orally ingested nitrite in an vivo study. When 3 mg/kg Na (15)NO2 was orally administered to rats with or without iron(II) or quercetin, Hb (15)NO, which is indicative of systemic (15)NO, was detected in the blood, with the maximum blood concentration of Hb (15)NO at 15 min after nitrite or nitrite plus quercetin treatment, whereas after administration of nitrite plus iron(II) or nitrite plus iron(II) and quercetin, the time was shortened to 10 min. Interestingly, iron(II), quercetin, or iron(II) plus quercetin did not affect the total amount of Hb (15)NO generated from orally administered Na (15)NO2. However, the systemic nitrite concentration was significantly decreased in the presence of iron(II) or iron(II) plus quercetin. These results may indicate that iron(II) is critical to the generation of NO gas from nitrite, whereas quercetin contributed little under the in vivo experimental conditions.     

Influence of B-ring hydroxylation on interactions of flavonols with bovine serum albumin

The B-ring substitution pattern of flavonols is a significant structural feature for their function as free radical scavengers and antioxidants. In this paper, four differently substituted B-ring hydroxylation flavonols (galangin, kaempferol, quercetin, and myricetin) and a flavonol glycoside (quercitrin) were studied for their ability to bind BSA by quenching the protein intrinsic fluorescence. From the spectra obtained, the biomolecular quenching constants, the apparent static binding constants, and the binding site values were calculated. The B-ring hydroxylation of flavonols significantly affected the binding/quenching process; in general, the binding affinity increased with the number of hydroxyl groups on the B-ring. The binding constants ( Ka) were determined as myricetin (4.90 x 10(8) L/mol) > quercetin (3.65 x 10(7) L/mol) > kaempferol (2.57 x 10(6) L/mol) > galangin (6.43 x 10(5) L/mol). The glycoside substitute at the C-ring position decreased the binding affinity. The chromatographic retention factor ( K') and logarithms of apparent partition coefficient (log Kow) were linear to the logarithms of apparent binding constants (log Ka) for flavonols with increasing hydroxyl groups on the B-ring. These results showed that the hydrogen bond force play an important role in binding flavonols to BSA. These results are also in agreement with the generally accepted structure-dependent free radical scavenger and antioxidant abilities of flavonols.     

Relationship between clamp force and pull-out strength in lag screw timber joints

This study empirically examines the relationship between clamp force and pull-out strength in lag screw joints of timber members, using data obtained in tightening tests and pull-out tests. Maximum clamp force per unit screw length as determined from the tightening tests was lower than the lower bound for the 95% tolerance range for pull-out strength per unit screw length as determined from the pull-out tests. Moreover, X-ray CT (computed tomography) observations of anchor members from both tests revealed that failure behavior clearly differed between the tightening test and the pull-out test: tightening caused damage to the wooden, female thread in addition to major splitting damage in the wood perpendicular to the grain near the tip of the lag screw.     

Effects of the presence of grazing‐experienced heifers on the development of foraging behavior at the feeding station scale for first‐grazing season calves

In this study, effects of grazing‐experienced heifer presence on foraging behavior development at the feeding station (FS) scale for first‐grazing season calves were determined. A group of four calves grazing alone (C), and another comprising four calves (Wc) and three grazing‐experienced heifers (Wh), were alternately stocked every day for 2 h on the same pasture for 26 days. The foraging time budget for Wc was significantly longer than that for C (P < 0.05) on day 7, and was similar to that for Wh on all days. Bite rate per FS was significantly higher for Wc (15.5 bite/min) than for C (13.2 bite/min) from day 1 to 14 (33.4 vs. 29.0 bite/min, respectively; P < 0.01) and significantly lower than that for Wh on all days. The number of steps taken between adjacent FSs by Wc (4.7) was significantly lower than that for C (7.2) on days 1 and 14 (2.1 vs. 2.9 steps, respectively; P < 0.01) and was similar to Wh on all days. This suggests that grazing‐experienced heifers have positive effects on the foraging behavior development of new‐season grazing calves through 14 days after the start of stocking.