Black cohosh (Actaea racemosa, Cimicifuga racemosa) behaves as a mixed competitive ligand and partial agonist at the human mu opiate receptor

Black cohosh is a commonly used botanical dietary supplement for the treatment of climacteric complaints. Because the opiate system in the brain is intimately associated with mood, temperature, and sex hormonal levels, the activity of black cohosh extracts at the human mu opiate receptor (hMOR) expressed in Chinese hamster ovary cells was investigated. The 100% methanol, 75% ethanol, and 40% 2-propanol extracts of black cohosh effectively displaced the specific binding of [3H]DAMGO to hMOR. Further studies of the clinically used ethanol extract indicated that black cohosh acted as a mixed competitive ligand, displacing 77 +/- 4% [3H]DAMGO to hMOR (Ki = 62.9 microg/mL). Using the [35S]GTPgammaS assay, the action of black cohosh was found to be consistent with an agonist, with an EC50 of 68.8 +/- 7.7 microg/mL. These results demonstrate for the first time that black cohosh contains active principle(s) that activate hMOR, supporting its beneficial role in alleviating menopausal symptoms.     

Bathymetric modeling of sediments and organic carbon of polluted rivers in southeastern China

Purpose

Rivers in low plains in the subtropical regions of China, where the population is dense and economies are active and well-developed, might be a large terrestrial carbon pool. This present study of the Sanyang wetlands in Wenzhou, southeastern China, aims to quantitatively estimate the volume of sediments in this region’s polluted river systems and their carbon storage.

Materials and methods

The bathymetry of river sections were surveyed using an echo sounder equipped with a differential GPS. An underwater digital elevation model (DEM) was then developed using the anisotropic ordinary Kriging method. Sediment samples were collected and analyzed for carbon content and sediment properties. Carbon storage in sediments was calculated using bathymetric and sediment analysis data.

Results and discussion

The studied rivers have been receiving organic pollutants from local residences and industries for decades. Results from a river network of 1.2 km² revealed a total carbon storage of 46.7 million kg in the sediments which had a volume of 1.4 million m³, with the upper 20 cm depth of sediments contributing about one third of this carbon storage.

Conclusions

The present work demonstrated that GIS technologies can be used to create digital river sediment surfaces and assess sediment amounts as well as determine the spatial distribution of sediments and their components. This could provide further insight into river restoration planning and other options from a carbon-balance perspective.

     

Efficacy of postemergence herbicides tankmixes in aryloxyphenoxypropionate-resistant grain sorghum

The development of aryloxyphenoxypropionate (APP)-resistant grain sorghum could provide additional opportunities for postemergence herbicide grass control in grain sorghum. Field experiments were conducted in Texas (Bushland, and Yoakum), Kansas (Dodge City, Garden City, Hays, Manhattan, Colby, Ottawa, and Tribune), and South Dakota (Highmore) to evaluate the efficacy of quizalofop tank mixes in APP-resistant grain sorghum. Quizalofop was applied alone or in combination with dicamba, 2,4-D, prosulfuron, 2,4-D + metsulfuron methyl, or halosulfuron methyl + dicamba. Herbicides were applied when sorghum was 12–50 cm in height. Overall weed control was greater when quizalofop was applied with other herbicides than when applied alone. At 2 and 4 weeks after treatment (WAT), large crabgrass [Digitaria sanguinalis (L.) Scop.], giant foxtail (Setaria faberi Herrm.), and green foxtail [Setaria viridis (L.) Beauv.] control were greater than 90% when quizalofop was applied alone or in combination with dicamba, halosulfuron methyl + dicamba, or prosulfuron. Palmer amaranth (Amaranthus palmeri S. Wats.), puncturevine (Tribulus terrestris L.), and tumble pigweed (Amaranthus albus L.) control were greater than 90% in all treatments except when quizalofop was applied alone. Herbicide treatments, except those that included 2,4-D, caused slight to no sorghum injury. Grain sorghum yield was greater for all herbicide treatments compared to the weedy check. This research showed that application of quizalofop in combination with broadleaf weed herbicides provided excellent weed control in sorghum.     

Asteroid 1950 DA's encounter with Earth in 2880: physical limits of collision probability prediction

Integration of the orbit of asteroid (29075) 1950 DA, which is based on radar and optical measurements spanning 51 years, reveals a 20-minute interval in March 2880 when there could be a nonnegligible probability of the 1-kilometer object colliding with Earth. Trajectory knowledge remains accurate until then because of extensive astrometric data, an inclined orbit geometry that reduces in-plane perturbations, and an orbit uncertainty space modulated by gravitational resonance. The approach distance uncertainty in 2880 is determined primarily by uncertainty in the accelerations arising from thermal re-radiation of solar energy absorbed by the asteroid. Those accelerations depend on the spin axis, composition, and surface properties of the asteroid, so that refining the collision probability may require direct inspection by a spacecraft.     

Race, ethnicity, and NIH research awards

We investigated the association between a U.S. National Institutes of Health (NIH) R01 applicant's self-identified race or ethnicity and the probability of receiving an award by using data from the NIH IMPAC II grant database, the Thomson Reuters Web of Science, and other sources. Although proposals with strong priority scores were equally likely to be funded regardless of race, we find that Asians are 4 percentage points and black or African-American applicants are 13 percentage points less likely to receive NIH investigator-initiated research funding compared with whites. After controlling for the applicant's educational background, country of origin, training, previous research awards, publication record, and employer characteristics, we find that black applicants remain 10 percentage points less likely than whites to be awarded NIH research funding. Our results suggest some leverage points for policy intervention.     

Observations of solar irradiance variability

High-precision measurements of total solar irradiance, made by the active cavity radiometer irradiance monitor on the Solar Maximum Mission satellite, show the irradiance to have been variable throughout the first 153 days of observations. The corrected data resolve orbit-to-orbit variations with uncertainties as small as 0.001 percent. Irradiance fluctuations are typical of a band-limited noise spectrum with high-frequency cutoff near 0.15 day(-1) their amplitudes about the mean value of 1368.31 watts per square meter approach +/- 0.05 percent. Two large decreases in irrradiance of up to 0.2 percent lasting about 1 week are highly correlated with the development of sunspot groups. The magnitude and time scale of the irradiance variability suggest that considerable energy storage occurs within the convection zone in solar active regions.     

Effects and Interactions of Medium Components on Laccase from a Marine-Derived Fungus Using Response Surface Methodology

The effects of various synthetic medium components and their interactions with each other ultimately impact laccase production in fungi. This was studied using a laccase-hyper-producing marine-derived basidiomycete, Cerrena unicolor MTCC 5159. Inducible laccases were produced in the idiophase only after addition of an inducer such as CuSO₄. Concentration of carbon and nitrogen acted antagonistically with respect to laccase production. A combination of low nitrogen and high carbon concentration favored both biomass and laccase production. The most favorable combination resulted in 917 U L⁻¹ of laccase. After sufficient growth had occurred, addition of a surfactant such as Tween 80 positively impacted biomass and increased the laccase activity to around 1,300 U L⁻¹. Increasing the surface to volume ratio of the culture vessel further increased its activity to almost 2,000 U L⁻¹.     

Chemistry and phytotoxicity of thaxtomin A alkyl ethers

The thaxtomin phytotoxins (1 and 2) from scab-producing Streptomyces pathogens of the potato are 2,5-dioxopiperazines consisting of modified l-tryptophanyl and l-phenylalanyl units. Thaxtomin A (1) is hydroxylated at C-14, the alpha carbon of the modified l-phenylalanyl moiety. Refluxing thaxtomin A in acidified MeOH, EtOH, and i-PrOH afforded C-14 thaxtomin A methyl- (3a and 3b), ethyl- (4a and 4b), and isopropyl- (5a and 5b) ethers, respectively, in both the 11S,14R (3a, 4a, and 5a) and 11S,14S (3b, 4b, and 5b) configurations. Crystal structures were determined for 3a and 4a. Extensive NMR as well as other spectroscopic data supported structural assignments for all of the derivatives. The 11S,14R-configured derivatives were slightly less potent than the natural products (1 and 2) as inhibitors of lettuce seedling root growth, whereas the activity of the 11S,14S epimers was much reduced, indicating that the configuration at C-14 found in the naturally occurring thaxtomins is essential for biological activity. Among the 11S,14R-configured compounds, potency decreased with an increasing size of the substituted alkoxy group.     

Cis-acting regulatory variation in the human genome

The systematic screening of the human genome for genetic variants that affect gene regulation should advance our fundamental understanding of phenotypic diversity and lead to the identification of alleles that modify disease risk. There are several challenges in localizing regulatory polymorphisms, including the wide spectrum of cis-acting regulatory mechanisms, the inconsistent effects of regulatory variants in different tissues, and the difficulty in isolating the causal variants that are in linkage disequilibrium with many other variants. We discuss the current state of knowledge and technologies used for mapping and characterizing genetic variation controlling human gene expression.