Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors

A series of structurally novel stearoyl-CoA desaturase1 (SCD1) inhibitors has been identified via molecular scaffold manipulation. Preliminary structure–activity relationship (SAR) studies led to the discovery of potent, and orally bioavailable piperidine-aryl urea-based SCD1 inhibitors. 4-(2-Chlorophenoxy)-N-[3-(methyl carbamoyl)phenyl]piperidine-1-carboxamide 4c exhibited robust in vivo activity with dose-dependent desaturation index lowering effects.     

Synthesis and biological evaluation of heterocycle containing adamantane 11beta-HSD1 inhibitors

A series of metabolically stable adamantane amide 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity and good pharmacokinetic and pharmacodynamic profiles.     

Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors

Chk1 inhibitors have emerged as a novel class of neoplastic agents for abrogating the G2 DNA damage checkpoint arrest. Analogs of the Chk1 inhibitor, 3-ethylidene-1,3-dihydro-indol-2-one, were synthesized and tested in vitro for their inhibitory activities. The most promising compound identified from this series is analog 28, which possesses potent enzymatic and cellular activities.     

A second site occupied by Octopus tetricus at high densities,with notes on their ecology and behavior

We report wild octopuses (Octopus tetricus) living at high density at a rock outcrop, the second such site known. O. tetricus are often observed as solitary individuals, with the species known to exist at similar densities and exhibiting complex social behaviors at only one site other than that described here. The present site was occupied by 10–15 octopuses on eight different days. We recorded frequent interactions, signaling, mating, mate defense, eviction of octopuses from dens, and attempts to exclude individuals from the site. These observations demonstrate that high-density occupation and complex social behaviors are not unique to the earlier described site, which had been affected to some extent by remains of human activity. Behavior at this second site confirms that complex social interactions also occur in association with natural substrate, and suggest that social interactions are more wide spread among octopuses than previously recognized.     

First Report of Dragon Fruit (Hylocereus undatus) Anthracnose Caused by Colletotrichum truncatum in China

Anthracnose disease was detected from dragon fruit (Hylocereus undatus) at a market of Yuanjiang County, Yunnan Province, China. The results of pathogenicity test, morphology studies and sequence analyses based on ITS and β‐tubulin loci indicated that the disease was caused by Colletotrichum truncatum. The pathogen produced elliptic, yellow spots with chlorotic halos on the surface of the fruit, and the lesion become depressed gradually. Grey to black acervuli appeared on the lesion surface in concentric circles later. This is the first report of dragon fruit anthracnose caused by this pathogen in China.     

Television Viewing Time in Hong Kong Adult Population: Associations with Body Mass Index and Obesity

Background

Obesity is increasing dramatically in the Asia-Pacific region particularly China. The population of Hong Kong was exposed to modernization far earlier than the rest of China, reflecting conditions that are likely to be replicated as other Chinese cities undergo rapid change. This study examined the relationship between television viewing and obesity in a Hong Kong sample. Information about the relationship between a key sedentary behavior, TV viewing, and obesity, and its moderation by demographic characteristics may identify sectors of the population at highest risk for excess weight.

Methods

Data were from Hong Kong Family and Health Information Trends Survey (2009–2010), a population-based survey on the public''s use of media for health information and family communication by telephone interviews with 3,016 Hong Kong adults (age≥18 years). TV viewing time, body mass index (BMI), physical activity and other lifestyle variables were analyzed.

Results

Viewing time was longer in women, increased with age but decreased with education level and vigorous physical activity (all P<0.01). Longer TV viewing time was significantly associated with higher BMI (Coefficients B = 0.17, 95% CI: 0.11, 0.24) after adjusting for age, gender, employment status, marital status, education level, smoking activity and vigorous physical activity. This association was stronger in women than men (Coefficients B: 0.19 versus 0.15) and strongest in those aged 18 to 34 years (Coefficients B = 0.35). Furthermore, an hour increase in daily TV viewing was associated with 10% greater odds of being obese.

Conclusions

A significant socioeconomic gradient in television viewing time was observed. TV viewing time positively associated with BMI and obesity. The TV viewing – BMI associations were strongest in women and young adults, suggesting vulnerable groups to target for obesity prevention by decreasing TV viewing.     

The Trends in Excess Mortality in Winter vs. Summer in a Sub-Tropical City and Its Association with Extreme Climate Conditions

While there is literature on excess winter mortality, there are few studies examining the evolution of its trend which may be changing in parallel with global warming. This study aimed to examine the trend in the excess mortality in winter as compared to summer among the older population in a sub-tropical city and to explore its association with extreme weather. We used a retrospective study based on the registered deaths among the older population in Hong Kong during 1976-2010. An Excess Mortality for Winter versus Summer (EMWS) Index was used to quantify the excess number of deaths in winter compared to summer. Multiple linear regressions were used to analyze the trends and its association with extreme weather. Overall, the EMWS Index for ischemic heart disease, cerebrovascular diseases, chronic lower respiratory diseases, pneumonia, and other causes were 43.0%, 34.2%, 42.7%, 23.4% and 17.6%, respectively. Significant decline was observed in the EMWS Index for chronic lower respiratory diseases and other causes. The trend in the index for cerebrovascular diseases depended on the age group, with older groups showing a decline but younger groups not showing any trend. Meteorological variables, in terms of extreme weather, were associated with the trends in the EMWS Index. We concluded that shrinking excess winter mortality from cerebrovascular diseases and chronic lower respiratory diseases was found in a sub-tropical city. These trends were associated with extreme weather, which coincided with global warming.     

Multiple tandem 18-kb sequences clustered in the region of the acute promyelocytic leukemia breakpoint on chromosome 17

This paper describes the cloning of an 18-kb sequence present in approximately 30 copies on chromosome 17. Most of these are clustered in the region of the breakpoint associated with acute promyelocytic leukemia (APL). These copies map both above and below the breakpoint, and pulsed field gel analysis indicates that the majority of these sequences lie within a region of approximately 2 megabases. The organization of these sequences appears to be that of large imperfect palindromes.