In the title salt, C14H18N2(2+) · 2C9H5N4O(-), the 1,1'-diethyl-4,4'-bipyridine-1,1'-diium dication lies across a centre of inversion in the space group P21/c. In the 1,1,3,3-tetracyano-2-ethoxypropenide anion, the two independent -C(CN)2 units are rotated, in conrotatory fashion, out of the plane of the central propenide unit, making dihedral angles with the central unit of 16.0(2) and 23.0(2)°. The ionic components are linked by C-H...N hydrogen bonds to form a complex sheet structure, within which each cation acts as a sixfold donor of hydrogen bonds and each anion acts as a threefold acceptor of hydrogen bonds.
A urea precursor was used for the first time to prepare mesoporous carbon nitride (MCN) by a thermal polymerization process with silica nanospheres as a hard template. Although the prepared MCN samples have similar structures and optical properties, it was revealed that the specific surface area, pore-size distribution, and morphology of the MCN samples depend on the initial mass ratio of urea to silica. Compared to the bulk carbon nitride (BCN) that only gave 20% phenol removal (6 h of irradiation), the activities can be enhanced up to 74% on MCN samples for photocatalytic removal of phenol under visible-light irradiation. The highest conversion was obtained on MCN with an initial mass ratio of urea to silica of 5, which has high surface area of 191 m(2) g(-1) and a nanoporous structure with uniform pore-size distribution of 7 nm. In addition to the high activity, the MCN sample also showed high photocatalytic stability.
The sorption and desorption of cyfluthrin mixture isomers were determined using batch equilibration method and mobility was studied under laboratory conditions, using packed soil column. The soil types used in the study were clayey, clay loam and sandy clay loam obtained from three tomato farms in Cameron Highlands. A low Freundlich adsorption distribution coefficient K(ads(f)) for cyfluthrin was observed for clayey, clay loam and sandy clay loam soils (95.69, 21.64 and 8.99 l/kg, respectively). Results showed that cyfluthrin had high Freundlich organic matter (OM) distribution coefficient K(oc) values of 5799, 2278 and 1635 lkg(-1) for clayey, clay loam and sandy clay loam soils, respectively. These values indicate that cyfluthrin is considered immobile in Malaysian soils with different textures, based on the value of K(oc) by McCall. Adsorption of cyfluthrin was significantly (P < 0.05) affected with soil pH, fertilizer NPK, organic matter content and temperature. It was observed that approximately 95.8%, 93.8% and 91.8% of the adsorbed cyfluthrin remained sorbed after four successive rinses for clayey, clay loam and sandy clay loam soils. Soil column test showed that cyfluthrin was not detected in leachate. Cyfluthrin was detected in topsoil and its concentration decreased with depth. The downward movement of cyfluthrin in sandy clay loam soil was more than that in clay loam and clayey soils. Approximately, 80.9%, 77.8% and 67.3% cyfluthrin was observed at the depth of 0-5 cm (rainfall 350 mm) for clayey, clay loam and sandy clay loam soils respectively. Mobility of cyfluthrin showed that the percentage of cyfluthrin leached into soil was not affected by the amount of rainfall. The result clearly showed that cyfluthrin molecules were bound strongly to all the three Malaysian soil types.
Insecticide-based vector control approaches are facing challenges due to the development of resistance in vector mosquitoes. Therefore, a proper resistance surveillance program using baseline lethal concentrations is crucial for resistance management strategies. Currently, the World Health Organization's (WHO) diagnostic doses established for Aedes aegypti and Anopheles species are being used to study the resistance status of Aedes albopictus. In this study, we established the diagnostic doses for permethrin, deltamethrin, and malathion using a known susceptible reference strain. Five field-collected populations were screened against these doses, following the WHO protocol. This study established the diagnostic dose of malathion at 2.4%, permethrin at 0.95%, and deltamethrin at 0.28%, which differ from the WHO doses for Aedes aegypti and Anopheles spp. Among the insecticides tested on the 5 wild populations, only deltamethrin showed high effectiveness. Different susceptibility and resistance patterns were observed with permethrin, malathion, and dichloro-diphenyl-trichloroethane (DDT) at 4%. This study may assist the health authorities to improve future chemical-based vector control operations in dengue-endemic areas.
The efficacy of two formulations, wettable powder and emulsifiable concentrate, of cyfluthrin sprayed on plywood [10 mg (ai)/m2] was assessed against six species of mosquitos. The bioassay followed the WHO standard method, with some modification for the bioassay of insecticidal deposits on wall surfaces. The results indicated that these two formulations of cyfluthrin were effective against Anopheles dirus and Mansonia uniformis, moderately toxic to Aedes aegypti and Ae. albopictus in decreasing mortality through out the study period. It was least effective against Culex quinquefasciatus and An. maculatus, respectively. There was no statistically significant difference between these two formulations.
The occurrence of n-alkanoic acids, amides, and nitriles in samples of aerosol particulate matter from Kuala Lumpur and Santiago suggests that emissions from cooking and biomass burning are the primary sources of these organic markers in the atmosphere. It is proposed that fatty acids react with ammonia during biomass burning or combustion to produce amides and nitriles, which can be applied as useful biomarker tracers. To test this hypothesis, nonadecanoic acid and hexadecanamide were used as reactants in hydrous pyrolysis experiments. These experiments produced amides and nitriles and indicated that ammonia is an essential agent in their formation. Thus amides and nitriles are of utility as indicators for input from combustion and biomass burning in the ambient atmosphere.
Glove wearing during patient treatment has been central to dental surgery infection control for over 15 years. However, little is known about the cutaneous effects of glove wearing on the hands of dental healthcare workers (DHCWs). The objective of this project was to assess the hand skin health of DHCWs before and after wearing gloves of two types and to compare this with a control group of non-DHCWs.
An alternative superovulator to replace clomiphene citrate (CC) is needed as it is unsuitable for women with polycystic ovarian syndrome and is associated with low pregnancy rates. Anastrozole is an effective superovulator, but has not been well researched. The aim of this study was to determine the optimal dose of anastrozole as a superovulator and ascertain its effects on implantation and uterine ultrastructure during early pregnancy in Wistar rats using scanning electron microscopy. The uterine morphological characteristics which were studied in day 1 and 6 pregnant rats include microvilli density, length, surface "beads", surface glycocalyx, cell borders and apices, uterine surface fording and large surface protrusions. A significant increase in implantation sites is seen in the 15 mg/kg anastrozole group, compared to control. Day 1 and 6 anastrozole groups have similar morphology to the control and different to the CC group. At day 6, large surface protrusions are mostly noted but not limited to anastrozole-treated rats; anastrozole also appears to retain glycocalyx to some extent. The increased number of implantation sites in the 15 mg/kg anastrozole group suggests that this dose superovulates and favors implantation. Anastrozole is probably dose-/species-specific and additionally the surface uterine morphology suggests that anastrozole is implantation friendly.
Routine surveillance on resistant status of field mosquito populations is important to implement suitable strategies in order to prevent pest outbreaks. WHO test kit bioassay is the most frequent bioassay used to investigate the susceptibility status of field-collected mosquitoes, as it is relatively convenient to be carried out in the field. In contrast, the topical application of active ingredient is less popular in investigating the susceptibility status of mosquitoes. In this study, we accessed the susceptibility status of Aedes albopictus Skuse collected from two dengue hotspots on Penang Island: Sungai Dua and Persiaran Mayang Pasir. Two active ingredients: permethrin and deltamethrin, were used. WHO test kit bioassay showed that both wild strains collected were susceptible to the two active ingredients; while topical application assay showed that they were resistant. This indicated that WHO test kit bioassay less sensitive to low level of resistance compared to topical application assay. Hence, topical application is expected to be more indicative when used in a resistance surveillance programme.
Antibiotic resistance is a problem that continues to challenge the healthcare sector, especially in clinically significant pathogens like methicillin-resistant Staphylococcus aureus (MRSA). Herein is described the isolation and structure elucidation of a bioactive compound from Allium stipitatum with antimicrobial activity. Crude Allium stipitatum dichloromethane extract (ASDE) was subjected to systematic purification by chromatographic procedures to afford various bioactive fractions. A fraction that exhibited anti-MRSA activity (4 µg·mL-1) was further characterized to determine the structure. The structure of the compound was elucidated as 2-(methyldithio)pyridine-3-carbonitrile (2-Medpy-3-CN). The 2-Medpy-3-CN compound, which was screened for antimicrobial activity, exhibited minimum inhibitory concentrations (MICs) in the range of 0.5 to >64 µg·mL-1 for tested bacterial species and 0.25 to 2 µg·mL-1 for Candida spp. Further studies are important to confirm the drug target and mechanism of action.
In vitro assays are economical and easy to perform but to establish relevance of their results to real clinical outcome in animals or human, pharmacokinetics is prerequisite. Despite various in vitro pharmacological activities of extracts of Piper sarmentosum, there is no report of pharmacokinetics. Therefore, the present study aimed to evaluate ethanol extract of fruit of the plant in dose of 500 mg kg(-1) orally for pharmacokinetics. Sprague-Dawley rats were randomly divided into groups 1, 2, and 3 (each n = 6) to study absorption, distribution and excretion, respectively. High performance liquid chromatography (HPLC) with ultraviolet detection was applied to quantify pellitorine, sarmentine and sarmentosine in plasma, tissues, feces and urine to calculate pharmacokinetic parameters. Pellitorine exhibited maximum plasma concentration (C(max)) 34.77 ng mL(-1) ± 1.040, time to achieve C(max) (T(max)) 8 h, mean resident time (MRT) 26.00 ± 0.149 h and half life (t(1/2)) 18.64 ± 1.65 h. Sarmentine showed C(max) 191.50 ± 12.69 ng mL(-1), T(max) 6 h, MRT 11.12 ± 0.44 h and t(1/2) 10.30 ± 1.98 h. Sarmentosine exhibited zero oral bioavailability because it was neither detected in plasma nor in tissues, and in urine. Pellitorine was found to be distributed in intestinal wall, liver, lungs, kidney, and heart, whereas sarmentine was found only in intestinal wall and heart. The cumulative excretion of pellitorine, sarmentine and sarmentosine in feces in 72 h was 0.0773, 0.976, and 0.438 μg, respectively. This study shows that pellitorine and sarmentine have good oral bioavailability while sarmentosine is not absorbed from the gastrointestinal tract.
In the present study, we have investigated potential cardioprotective properties of Isosteviol analogue we recently synthesized and named JC105. Treatment of heart embryonic H9c2 cells with JC105 (10 μM) significantly increased survival of cells exposed to hypoxia-reoxygenation. JC105 (10 μM) activated ERK1/2, DRP1 and increased levels of cardioprotective SUR2A in hypoxia-reoxygenation, but did not have any effects on ERK1/2, DRP1 and/or SUR2A in normoxia. U0126 (10 μM) inhibited JC105-mediated phosphorylation of ERK1/2 and DRP1 without affecting AKT or AMPK, which were also not regulated by JC105. Seahorse bioenergetic analysis demonstrated that JC105 (10 μM) did not affect mitochondria at rest, but it counteracted all mitochondrial effects of hypoxia-reoxygenation. Cytoprotection afforded by JC105 was inhibited by U0126 (10 μM). Taken all together, these demonstrate that (a) JC105 protects H9c2 cells against hypoxia-reoxygenation and that (b) this effect is mediated via ERK1/2. The unique property of JC105 is that selectively activates ERK1/2 in cells exposed to stress, but not in cells under non-stress conditions.
Phyllagathis rotundifolia (Jack) Bl. (Melastomataceae) is a creeping herb found in Peninsular Malaysia and Sumatra. Traditionally, a decoction of the leaves is used in the treatment of malaria, fever and stomach ache.
Many insect species display daily variation of sensitivity to insecticides when they are exposed to the same concentration at different times during the day. To date, this has not been investigated in bed bugs. To address this, we explored circadian rhythms in insecticide susceptibility, xenobiotic metabolizing (XM) gene expressions, and metabolic detoxification in the common bed bug, Cimex lectularius. An insecticide susceptible Monheim strain of C. lectularius was most tolerant of deltamethrin during the late photophase at ZT9 (i.e. nine hours after light is present in the light-dark cycle (LD) cycle) and similarly repeated at CT9 (i.e. nine hours into the subjective day in constant darkness (DD)) suggesting endogenous circadian involvement in susceptibility to deltamethrin. No diel rhythm was observed against imidacloprid insecticide despite significant daily susceptibility in both LD and DD conditions. Rhythmic expressions of metabolic detoxification genes, GSTs1 and CYP397A1 displayed similar expression patterns with total GST and P450 enzyme activities in LD and DD conditions, respectively. The oscillation of mRNA levels of GSTs1 and CYP397A1 was found consistent with peak phases of deltamethrin susceptibility in C. lectularius. This study demonstrates that circadian patterns of metabolic detoxification gene expression occur within C. lectularius. As a consequence, insecticide efficacy can vary dramatically throughout a 24 hour period.
The bioefficacy of indoor residual-sprayed deltamethrin wettable granule (WG) formulation at 25 mg a.i./m2 and 20 mg a.i./m2 for the control of malaria was compared with the current dose of 20 mg/m2 deltamethrin wettable powder (WP) in aboriginal settlements in Kuala Lipis, Pahang, Malaysia. The malaria vector has been previously identified as Anopheles maculatus. The assessment period for the 20 mg/m2 dosage was six months, but for the 25 mg/m2 dosage, the period was 9 months. Collections of mosquitoes using the bare-leg techniques were carried out indoors and outdoors from 7:00 PM to 7:00 AM. All mosquitoes were dissected for sporozoites and parity. Larval collections were carried out at various locations to assess the extent and distribution of breeding of vectors. A high incidence of human feeds was detected during May 2005 and a low incidence during January 2005 for all the study areas. Our study showed that deltamethrin WG at 25 mg/m2 suppressed An. maculatus biting activity. More An. maculatus were caught in outdoor landing catches than indoor landing catches for all the study areas. The results indicate that 25 mg/m2 WG is good for controlling malaria for up to 9 months. Where residual spraying is envisaged, the usual two spraying cycles per year with 20 mg/m2 deltamethrin may be replaced with 25 mg/m2 deltamethrin WG every 9 months.
Solid phase extraction (SPE) and dispersive solid-phase extraction (d-SPE) were compared and evaluated for the determination of λ-cyhalothrin and cypermethrin in palm oil matrices by gas chromatography with an electron capture detector (GC-ECD). Several SPE sorbents such as graphitised carbon black (GCB), primary secondary amine (PSA), C(18), silica, and florisil were tested in order to minimise fat residues. The results show that mixed sorbents using GCB and PSA obtained cleaner extracts than a single GCB and PSA sorbents. The average recoveries obtained for each pesticide ranged between 81% and 114% at five fortification levels with the relative standard deviation of less than 7% in all cases. The limits of detection for these pesticides were ranged between 0.025 and 0.05 μg/g. The proposed method was applied successfully for the residue determination of both λ-cyhalothrin and cypermethrin in crude palm oil samples obtained from local mills throughout Malaysia.
Design of neutral receptor molecules (ionophores) for beryllium(II) using unsaturated carbonitrile models has been carried out via density functional theory, G3, and G4 calculations. The first part of this work focuses on gas phase binding energies between beryllium(II) and 2-cyano butadiene (2-CN BD), 3-cyano propene (3-CN P), and simpler models with two separate fragments; acrylonitrile and ethylene. Interactions between beryllium(II) and cyano nitrogen and terminal olefin in the models have been examined in terms of geometrical changes, distribution of charge over the entire π-system, and rehybridization of vinyl carbon orbitals. NMR shieldings and vibrational frequencies probed charge centers and strength of interactions. The six-membered cyclic complexes have planar structures with the rehybridized carbon slightly out of plane (16° in 2-CN BD). G3 results show that in 2-CN BD complex participation of vinyl carbon further stabilizes the cyclic adduct by 16.3 kcal mol(-1), whereas, in simpler models, interaction between beryllium(II) and acetonitrile is favorable by 46.4 kcal mol(-1) compared with that of ethylene. The terminal vinyl carbon in 2-CN BD rehybridizes to sp (3) with an increase of 7 % of s character to allow interaction with beryllium(II). G4 calculations show that the Be(II) and 2-CN BD complex is more strongly bound than those with Mg(II) and Ca(II) by 98.5 and 139.2 kcal mol(-1) (-1), respectively. QST2 method shows that the cyclic and acyclic forms of Be(II)-2-CN BD complexes are separated by 12.3 kcal mol(-1) barrier height. Overlap population analysis reveals that Ca(II) can be discriminated based on its tendency to form ionic interaction with the receptor models.
Insecticide-treated mosquito nets were first put to practical use in the Western Pacific Region. Less than a decade after conducting workshops and other promotional activities, millions of people were protected by 1989. This occurred before the availability of commercially produced pretreated nets and before global funding for mass net distribution. This paper describes the sequence of steps leading to regional control success. The beginning stages in 1979 recognized that treating torn mosquito nets was a viable control option. Basic net treatment procedures were established by 1983 and workshops were held the next 2 years in China, Cambodia, Laos, Malaysia, Papua New Guinea, Philippines, Solomon Islands, Vanuatu, and Vietnam. Malaria staff became convinced of net benefits and were motivated to impart their knowledge to others. Village inhabitants soaked the nets in washbasins containing permethrin or deltamethrin solution, then dried them horizontally on mats. By the 1990s, the population protected by nets had appreciably increased, and regional malaria cases confirmed by microscopy were markedly reduced. This coincided with commercial interest to mass-produce pretreated mosquito nets for worldwide use.
Although anastrozole (Anas) plays a key role in the management of endocrine sensitive post-menopausal (PM) breast cancer (BC), there is much variability in its efficacy and tolerability. Anas-associated musculoskeletal symptoms (MS) and other adverse reactions, such as hot flashes (HF) and vaginal dryness/dyspareunia (VDD), are common and can affect the quality of life of BC patients, even sometimes leading to treatment withdrawal. The aim of this study was to determine the clinical and demographic factors associated with these adverse events. This is a cross-sectional study in estrogen receptor (ER) positive PM women (n = 92) with stages I to III BC receiving Anas. Multivariate analyses were performed to investigate the factors associated with Anas-induced adverse effects such as MS, HF and VDD. A serum estradiol concentration was undetectable (< 36.7 pmol/L) in 68.1% of patients but was detectable within a normal range (>36.7-88.1 pmol/L) in the other 31.9% of patients, and this group was found to have a lower odds of having at least one adverse effect (AE) compared to those with undetectable levels [adjusted odds ratio (AOR) 0.12, 95% confidence interval (CI) 0.02 to 0.64, p = 0.013]. Women with grades II and III tumors and a family history of BC had a higher odds of AE (grade II: AOR 12.22, CI 1.48 to 100.80, p = 0.020; grade III: AOR 12.95, CI 1.25 to 134.33, p = 0.032) and VDD (AOR 5.99, CI 1.30 to 27.52, p = 0.021), respectively. Patients who received Anas treatment for more than one year had a higher odds of VDD (one to three years: AOR 34.57, CI 3.86, 309.50, p = 0.002; more than 3 years: AOR 27.90, CI 2.21 to 351.84, p = 0.010). Advanced age also lowered the odds of HF (AOR 0.90, CI 0.83 to 1.00, p = 0.049). In conclusion, patients' hormonal environments and durations of Anas treatment may play a role in developing Anas-induced adverse effects.