Structure–activity relationships and the cytotoxic effects of novel diterpenoid alkaloid derivatives against A549 human lung carcinoma cells

The cytotoxicity of three alkaloids from the roots of Aconitum yesoense var. macroyesoense as well as 36 semi-synthetic C20-diterpenoid atisine-type alkaloid derivatives against A549 human lung carcinoma cells was examined. Ten acylated alkaloid derivatives, pseudokobusine 11-veratroate (9), 11-anisoate (12), 6,11-dianisoate (14), 11-p-nitrobenzoate (18), 11,15-di-p-nitrobenzoate (22), 11-cinnamate (25) and 11-m-trifluoromethylbenzoate (27), and kobusine 11-p-trifluoromethylbenzoate (35), 11-m-trifluoromethylbenzoate (36) and 11,15-di-p-nitrobenzoate (39), exhibited cytotoxic activity, and 11,15-dianisoylpseudokobusine (16) was found to be the most potent cytotoxic agent. Their IC50 values against A549 cells ranged from 1.72 to 5.44 μM. In the occurrence of cytotoxic effects of atisine-type alkaloids, replacement by an acyl group at both C-11 and C-15 resulted in the enhancement of activity of the parent alkaloids compared to that from having hydroxy groups at this position, and the presence of a hydroxy group at the C-6 position was required for the cytotoxic effects. These acylated alkaloid derivatives inhibit cell growth through G1 arrest

Female Urethral Reconstruction

Female urethral strictures are rare; thus, the literature describing stricture management in women is sparse. Although urethral dilation continues to be performed at a high frequency in women despite lack of proven efficacy, this procedure is used for a variety of voiding complaints other than stricture. Hence, the long-term utility of dilation and urethrotomy for urethral stricture in women is unknown. This review describes the various urethroplasty techniques used in the management of female urethral stricture. Although grafts using a dorsal approach have been shown to be feasible in women, ventral flap techniques offer good long-term outcomes with minimal morbidity. Acute and delayed management of pelvic fracture–associated urethral distraction defects in women is also described. Unlike in men, immediate urethroplasty in women should be performed once the patient is hemodynamically stable

Multi-messenger observations of a binary neutron star merger

On 2017 August 17 a binary neutron star coalescence candidate (later designated GW170817) with merger time 12:41:04 UTC was observed through gravitational waves by the Advanced LIGO and Advanced Virgo detectors. The Fermi Gamma-ray Burst Monitor independently detected a gamma-ray burst (GRB 170817A) with a time delay of ~1.7 s with respect to the merger time. From the gravitational-wave signal, the source was initially localized to a sky region of 31 deg2 at a luminosity distance of 40+8-8 Mpc and with component masses consistent with neutron stars. The component masses were later measured to be in the range 0.86 to 2.26 Mo. An extensive observing campaign was launched across the electromagnetic spectrum leading to the discovery of a bright optical transient (SSS17a, now with the IAU identification of AT 2017gfo) in NGC 4993 (at ~40 Mpc) less than 11 hours after the merger by the One- Meter, Two Hemisphere (1M2H) team using the 1 m Swope Telescope. The optical transient was independently detected by multiple teams within an hour. Subsequent observations targeted the object and its environment. Early ultraviolet observations revealed a blue transient that faded within 48 hours. Optical and infrared observations showed a redward evolution over ~10 days. Following early non-detections, X-ray and radio emission were discovered at the transient’s position ~9 and ~16 days, respectively, after the merger. Both the X-ray and radio emission likely arise from a physical process that is distinct from the one that generates the UV/optical/near-infrared emission. No ultra-high-energy gamma-rays and no neutrino candidates consistent with the source were found in follow-up searches. These observations support the hypothesis that GW170817 was produced by the merger of two neutron stars in NGC4993 followed by a short gamma-ray burst (GRB 170817A) and a kilonova/macronova powered by the radioactive decay of r-process nuclei synthesized in the ejecta

Plant zonation in a tropical irregular estuary: can large occurrence zones be explained by a tradeoff model?

AbstractEstuaries present an environmental gradient that ranges from almost fresh water conditions to almost marine conditions. Salinity and flooding are the main abiotic drivers for plants. Therefore, plant zonation in estuaries is closely related to the tidal cycles. It is expected that the competitive abilities of plants would be inversely related to the tolerance toward environmental stress (tradeoff). Thus, in estuaries, plant zonation tends to be controlled by the environment near the sandbar and by competition away from it. This zonation pattern has been proposed for regular non-tropical estuaries. For tropical estuaries, the relative importance of rain is higher, and it is not clear to what extent this model can be extrapolated. We measured the tidal influence along the environmental gradient of a tropical irregular estuary and quantified the relative importance of the environment and the co-occurrence degree. Contrary to the narrow occurrence zone that would be expected for regular estuaries, plants presented large occurrence zones. However, the relative importance of the environment and competition followed the same patterns proposed for regular estuaries. The environmental conditions allow plants to occur in larger zones, but these zones arise from smaller and infrequent patches distributed across a larger area, and most species populations are concentrated in relatively narrow zones. Thus, we concluded that the zonation pattern in the Massaguaçu River estuary agrees with the tradeoff model

Plant zonation in a tropical irregular estuary: can large occurrence zones be explained by a tradeoff model?

AbstractEstuaries present an environmental gradient that ranges from almost fresh water conditions to almost marine conditions. Salinity and flooding are the main abiotic drivers for plants. Therefore, plant zonation in estuaries is closely related to the tidal cycles. It is expected that the competitive abilities of plants would be inversely related to the tolerance toward environmental stress (tradeoff). Thus, in estuaries, plant zonation tends to be controlled by the environment near the sandbar and by competition away from it. This zonation pattern has been proposed for regular non-tropical estuaries. For tropical estuaries, the relative importance of rain is higher, and it is not clear to what extent this model can be extrapolated. We measured the tidal influence along the environmental gradient of a tropical irregular estuary and quantified the relative importance of the environment and the co-occurrence degree. Contrary to the narrow occurrence zone that would be expected for regular estuaries, plants presented large occurrence zones. However, the relative importance of the environment and competition followed the same patterns proposed for regular estuaries. The environmental conditions allow plants to occur in larger zones, but these zones arise from smaller and infrequent patches distributed across a larger area, and most species populations are concentrated in relatively narrow zones. Thus, we concluded that the zonation pattern in the Massaguaçu River estuary agrees with the tradeoff model

Seasonality effect on the allelopathy of cerrado species

The Brazilian cerrado presents strong climate seasonality. During the dry season, plants may be exposed to stressful situations, such as a soil surface water deficit, that stimulate their chemical defenses. However, the seasonality effect on the production of allelopathic compounds of cerrado plant species is poorly understood. In this study, the phytotoxic activities of common native cerrado plants were evaluated during rainy and dry seasons. Crude leaves extracts (10% concentration: weight/volume, with dry leaves and distilled water) from eleven species were tested on lettuce and sesame germination. The negative effects on germination percentages, rates and informational entropies of the target species were higher when submitted to plant extracts from the dry season, where the germination rate was the most sensible parameter. The higher sensibility of lettuce and the germination rate parameter showed this difference. Only two exceptions had higher effects for rainy season extracts; one species showed higher negative effects on germination informational entropy of lettuce and another species on the germination rate of sesame. Thus, increases in the allelopathic activity were seen in the majority of the studied cerrado plant species during the dry season. These distinct responses to stressful situations in a complex environment such as the Brazilian cerrado may support the establishment and survival of some species

Seasonality effect on the allelopathy of cerrado species

The Brazilian cerrado presents strong climate seasonality. During the dry season, plants may be exposed to stressful situations, such as a soil surface water deficit, that stimulate their chemical defenses. However, the seasonality effect on the production of allelopathic compounds of cerrado plant species is poorly understood. In this study, the phytotoxic activities of common native cerrado plants were evaluated during rainy and dry seasons. Crude leaves extracts (10% concentration: weight/volume, with dry leaves and distilled water) from eleven species were tested on lettuce and sesame germination. The negative effects on germination percentages, rates and informational entropies of the target species were higher when submitted to plant extracts from the dry season, where the germination rate was the most sensible parameter. The higher sensibility of lettuce and the germination rate parameter showed this difference. Only two exceptions had higher effects for rainy season extracts; one species showed higher negative effects on germination informational entropy of lettuce and another species on the germination rate of sesame. Thus, increases in the allelopathic activity were seen in the majority of the studied cerrado plant species during the dry season. These distinct responses to stressful situations in a complex environment such as the Brazilian cerrado may support the establishment and survival of some species