The two cationic palladium(ii) complexes, [Pd(Len)2][OTf]2 (4) and [Pd(Lphen)2][OTf]2 (5), were synthesized by treatment of bis(benzonitrile)dichloropalladium(ii) with [H2Len][OTf]2 (2) or [H2Lphen][OTf]2 (3), respectively, in the presence of a weak base. The pro-ligands 2 and 3 were synthesized by melt reactions between N-methyl-4-chloropyridinium triflate (1) and the amines ethylenediamine or phenylenediamine, respectively. The water-soluble compounds 2-5 were fully characterized, including by single-crystal X-ray crystal structure determinations for 2-4. UV-Vis and fluorescence spectroscopy were used to study the binding interactions of 2-5 with CT-DNA. The spectroscopic data suggested the presence of intercalative and groove binding modes and this was supported by molecular docking studies. The in vitro cytotoxicity studies (IC50 values) showed that the human breast cancer cell lines MCF-7 and T47D were more sensitive towards 3, 4 and 5 than cisplatin. The cytotoxicity of the new compounds decreased in the order 5 > 4 > 3 > 2. Furthermore, the annexin V-FITC staining method strongly suggested the presence of phosphatidylserine (PS) on the outer membrane of the treated cells, which is a hallmark of apoptosis.
A polystyrene (PS)-anchored Pd(II) metal complex was synthesized on cross-linked polymer by heating a mixture of chlorometylated polystyrene with phenyldithiocarbazate and carbon disulfide in the presence of potassium hydroxide (KOH) in dimethylformamide (DMF). The reaction mixture was heated at 80 °C to form the corresponding phenyldithiocarbazate-functionalized polymer. Then, it was treated with bis(benzonitrile)palladium(II) chloride. The properties of dark colored polymer, impregnated with the metal complex was then characterized by various spectroscopic technique such as Fourier Transform Infrared (FTIR), Scanning Electron Microscopy/Energy Dispersive X-ray (SEM/EDX), CHNS elemental analysis, BET surface area, X-ray Diffraction (XRD), Thermogravimetric (TGA) and Inductively Coupled Plasma-Optical Emission (ICP-OES) spectroscopy.
The present study aimed to investigate standardized ethanol extracts of fruit and leaves of Piper sarmentosum for their in vivo antioxidant activity in rats using a CCl (4)-induced oxidative stress model. The standardization was based on the quantification of the markers pellitorine, sarmentine and sarmentosine by high performance liquid chromatography (HPLC), and determination of total primary and secondary metabolites. The rats, divided into 7 groups each (n = 6), were used as follows: group 1 (CCl (4), negative control), group 2 (untreated, control), groups 3 and 4 (fruit extract 250 and 500 mg/kg, respectively), groups 5 and 6 (leaf extract 250 and 500 mg/kg, respectively) and group 7 (vitamin-E 100 mg/kg, positive control). The doses were administered orally for 14 days; 4 h following the last dose, a single dose of CCl (4) (1.5 mg/kg) was given orally to all the groups except group 2, and after 24 h, blood and liver of each animal were obtained. Analysis of plasma and liver homogenate exhibited significant preservation of markers of antioxidant activity, total plasma antioxidant activity (TPAA), total protein (TP), superoxide dismutase (SOD), catalase (CAT), and thiobarbituric acid reactive species (TBARS), in the pretreated groups as compared to the CCl (4) group (p < 0.05). Histology of the liver also evidenced the protection of hepatocytes against CCl (4) metabolites in the pretreated groups. The results of this study indicate the IN VIVO antioxidant activity of both extracts of the plant, which may be valuable to combat diseases involving free radicals.
Cynoff 25ULV (cypermethrin 25 g/l) and Solfac UL015 (cyfluthrin 1.5% w/v) were evaluated against the sentinel sugar-fed adults and 4th-instar larvae of Aedes aegypti in a housing estate endemic of dengue in Malaysia. The impact of both pyrethroids on field populations of Aedes albopictus and Aedes aegypti larvae was monitored weekly using bottle containers. Both Cynoff 25ULV and Solfac UL015 showed adulticidal effects and larvicidal effects. This field trial using Cynoff 25ULV against dengue vectors showed its potential for use in dengue vector control programs.
Deltacide (S-bioallethrin 0.71% w/v, deltamethrin 0.5% w/v, piperonyl butoxide 8.9% w/v excipients to 100% w/v) and Solfac UL 015 (cyfluthrin 1.5% w/v) were evaluated against the sentinel sugar-fed adults and 4th-instar larvae of Aedes aegypti at 17 storey high-rise apartments in Malaysia using ULV applications. The impact of both insecticides on field populations of Ae. aegypti and Ae. albopictus larvae was monitored weekly using bottle containers. Both Deltacide and Solfac UL 015 showed adulticidal and larvicidal effects. This was the first field trial using Deltacide against dengue vectors in Malaysia and showed its potential for use in dengue vector control programs.
The efficacy of three insecticides, fipronil 3G, lambda-cyhalothrin 10%CS, and sumithion 50EC were evaluated against the dengue vector Aedes albopictus in discarded tires in Kuala Lumpur, Malaysia. The dosage given for each insecticide was 0.01 g of active ingredient/m2. Fipronil 3G was the most effective larvicide with a residual activity of up to two weeks, causing 88% mortality in Aedes albopictus. Lambda-cyhalothrin 10%CS was effective for one week causing 92% larval mortality and two weeks with 63% larval mortality. Sumithion 50EC had a residual efficacy of one week with 79% larval mortality.
Cyfluthrin (Solfac ULO15) and malathion 96 TG were evaluated against sentinel sugar-fed adults and 4th-instar larvae of Aedes aegypti at high-rise flats in Malaysia by ULV spraying. The impact of both insecticides on field populations of Aedes spp. (Ae. aegypti and Ae. albopictus) larvae were monitored weekly using containers. Both cyfluthrin and malathion 96 TG showed adulticidal effects but cyfluthrin showed more significant larvicidal effect than malathion 96 TG (P < 0.05).
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.
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.