Dataset Information

Antischistosomal activities of mefloquine-related arylmethanols.

ABSTRACT: Interesting antischistosomal properties have been documented for the antimalarial mefloquine, a 4-quinolinemethanol. We evaluated the antischistosomal activities of nine mefloquine-related compounds belonging to the 4-pyridinemethanols, 9-phenanthrenmethanols, and 4-quinolinemethanols. Eight compounds revealed high activities against Schistosoma mansoni in vitro, with two drugs (the 4-quinolinemethanols WR7573 and WR7930) characterized by significantly lower half-maximal inhibitory concentrations (IC(50)s) (2.7 and 3.5 ?M, respectively) compared to mefloquine (11.4 ?M). Mefloquine and WR7930 showed significantly decreased IC(50)s when incubated in the presence of hemoglobin. High worm burden reductions (WBR) were obtained with enpiroline (WBR, 82.7%; dosage, 200 mg/kg of body weight) and its threo isomers (+)-threo (WBR, 100%) and (-)-threo (WBR, 89%) and with WR7930 (WBR, 87%; dosage, 100 mg/kg) against adult S. mansoni in mice. Furthermore, excellent in vitro and in vivo antischistosomal activity was observed for two WR7930-related structures (WR29252 and WR7524). In addition, mefloquine (WBR, 81%), enpiroline (WBR, 77%), and WR7930 (WBR, 100%) showed high activities against S. haematobium harbored in mice following single oral doses of 200 mg/kg. These results provide a deeper insight into the structural features of the arylmethanols that rule antischistosomal activity. Further studies should be launched with enpiroline and WR7930.

SUBMITTER: Ingram K

PROVIDER: S-EPMC3370792 | biostudies-other | 2012 Jun

REPOSITORIES: biostudies-other

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Antischistosomal activities of mefloquine-related arylmethanols.

Ingram Katrin K Ellis William W Keiser Jennifer J

Antimicrobial agents and chemotherapy 20120402 6

Interesting antischistosomal properties have been documented for the antimalarial mefloquine, a 4-quinolinemethanol. We evaluated the antischistosomal activities of nine mefloquine-related compounds belonging to the 4-pyridinemethanols, 9-phenanthrenmethanols, and 4-quinolinemethanols. Eight compounds revealed high activities against Schistosoma mansoni in vitro, with two drugs (the 4-quinolinemethanols WR7573 and WR7930) characterized by significantly lower half-maximal inhibitory concentration ...[more]

PMID: 22470113

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Project description:BackgroundAlthough a number of studies have investigated how consumers use social media for health-related purposes, there is a paucity of studies in the Australian context.ObjectiveThis study aimed to explore how Australian consumers used social media for health-related purposes, specifically how they identified social media platforms, which were used, and which health-related activities commonly took place.MethodsA total of 5 focus groups (n=36 participants), each lasting 60 to 90 minutes, were conducted in the Sydney metropolitan area. The group discussions were audiorecorded and transcribed verbatim. The transcripts were coded line-by-line and thematically analyzed.ResultsParticipants used general search engines to locate health-related social media platforms. They accessed a wide range of social media on a daily basis, using several electronic devices (in particular, mobile phones). Although privacy was a concern, it did not prevent consumers from fully engaging in social media for health-related purposes. Blogs were used to learn from other people's experiences with the same condition. Facebook allowed consumers to follow health-related pages and to participate in disease-specific group discussions. Wikipedia was used for factual information about diseases and treatments. YouTube was accessed to learn about medical procedures such as surgery. No participant reported editing or contributing to Wikipedia or posting YouTube videos related to health topics. Twitter was rarely used for health-related purposes. Social media allowed consumers to obtain and provide disease and treatment-related information and social and emotional support for those living with the same condition. Most considered their participation as observational, but some also contributed (eg, responded to people's questions).ConclusionsParticipants used a wide range of social media for health-related purposes. Medical information exchange (eg, disease and treatment) and social and emotional support were the cornerstones of their online activities. Social media appears to be used as a key tool to support disease self-management.

Project description:BACKGROUND:Health-related quality of life (HRQOL) reflects a patient's perceived disease burden, treatment effectiveness, and health status. Given the time burden and physiologic effects of hemodialysis, patients who spend dialysis time (9-15 h/week) physically or intellectually engaged may have better HRQOL. We characterized the intradialytic activities and explored their association with HRQOL. METHODS:In a cross-sectional study of 431 hemodialysis patients, we ascertained kidney-disease-specific quality of life, measured frailty, and surveyed participants about their usual active intradialytic activities (reading, playing games, doing puzzles, chatting, or other) and passive intradialytic activities (watching TV or sleeping). We used adjusted ordered logistic regression to identify correlates of the activity index (the sum of active intradialytic activities) and adjusted linear regression to quantify the association between the activity index and physical-, mental-, and kidney-disease-specific HRQOL. RESULTS:The 2 most common intradialytic activities were passive activities (watching TV = 87.9%; sleeping = 72.4%). Participants who were female (aOR 1.85, 95% CI 1.28-2.66; p = 0.001), nonfrail (aOR 1.70, 95% CI 1.06-2.70; p = 0.03), and nonsmokers (aOR 2.61, 95% CI 1.39-4.90; p = 0.003) had a higher intradialytic activity index after adjustment. Higher intradialytic activity index was associated with better mental- (0.83 points, 95% CI 0.04-1.62; p = 0.04) and kidney-disease-specific HRQOL (1.70 points, 95% CI 0.47-2.93; p = 0.007), but not physical HRQOL. CONCLUSIONS:Hemodialysis patients with more active intradialytic activities report better mental and kidney-disease-specific HRQOL. These results should be confirmed in a prospective study with a broader cohort of hemodialysis patients. Dialysis providers may consider offering patients with low levels of activity additional support and opportunities to engage in beneficial intradialytic activities.

Dataset Information

Antischistosomal activities of mefloquine-related arylmethanols.

Publications

Antischistosomal activities of mefloquine-related arylmethanols.

Similar Datasets

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