A comparison between the enzymatic oxidation method and headspace gas chromatography with a flame ionization detector in the determination of postmortem blood ethanol.

Ethanol is the most commonly encountered substance in forensic toxicology. Determining blood alcohol concentration (BAC) in autopsies accounts for the majority of work in forensic diagnosis. The most common method to assess BAC is the enzymatic oxidation method because of its low cost, easy operation, and high throughput. Still, the elevated lactate and lactate dehydrogenase (LDH) levels in postmortem blood may affect accuracy. This study uses headspace gas chromatography with a flame ionization detector (HS-GC/FID) to assess the interference of lactate and LDH levels on BAC in 110 autopsied blood samples determined by the enzymatic oxidation method. The results showed that lactate and LDH levels in postmortem blood were higher than in normal blood. There was a weak correlation between the lactate levels and BAC difference (r = 0.23, p < 0.05) and a strong correlation between LDH levels and BAC difference (r = 0.67, p < 0.001). The differentiation of BAC between the enzymatic oxidation method and HS-GC/FID was significant (p < 0.001), confirming the interference significantly. All postmortem blood samples with lactate and LDH levels higher than regular lead to a positive error in determining BAC by enzymatic oxidation method. The study results suggest that the HS-GC/FID method should be used to determine BAC in postmortem blood samples instead of the enzymatic oxidation method to avoid mistakes in forensic diagnosis.

Highly efficient green-emitting ZnO:Cu2+ phosphors for NUV-pumped white-emitting diodes.

Phosphor-converted white light-emitting diodes (WLEDs) have received significant attention; however, the leaked light from their blue InGaN chips has an undesirable effect on human health. Hence, it is necessary to develop red, green, and blue-emitting phosphors, which can be excited by an NUV chip instead of a blue chip. Herein, green-emitting ZnO:Cu2+ phosphors have been successfully synthesized by a simple and facile thermal diffusion method. The obtained powder shows a broad emission band peaking at 525 nm and a strong absorption peak at 377 nm. The ZnO:5%Cu2+ phosphor annealed at 800 °C in 2 hours revealed a lifetime of 0.57 ms, an activation energy of 0.212 eV, and the highest emission intensity with (x, y) CIE colour coordinates (0.3130, 0.5253). A WLED prototype has been fabricated by coating the ZnO:5%Cu2+ phosphor on an NUV 375 nm LED chip, where this coated phosphor shows a high quantum efficiency (QE) of 56.6%. This is, so far, the highest reported QE value for ZnO-based phosphors. These results suggest that the ZnO:Cu2+ phosphor could be an excellent candidate for NUV-pumped phosphor-converted WLED applications.

Isolation and purification of potential weed inhibitors from Mimosa pigra L.

The diversity in structure and herbicidal properties detected in natural phytotoxic compounds could bring about advantages for development bio-herbicides. The present study was carried out search for potential weed inhibitors from the parts of Mimosa pigra L. The ethyl acetate (EtOAc) extract of leaf of M. pigra showed inhibitory activity during the time that Echinochloa crus-galli (barnyardgrass) germinates and grows, which is greater than that of other extracts. From this active extract, potent growth inhibitors were isolated and identified by column chromatography (CC), gas chromatography-mass spectrometry (GC-MS) and nuclear magnetic resonance (1H and 13C NMR). The six compounds were purified in this study namely: lupeol (C1, 13.2 mg), stigmastane-3,6-dione (C2, 14.7 mg), quercetin (C3, 20.2 mg), chrysoeriol (C4, 28 mg), methyl gallate (C5, 21.5 mg) and daucosterol (C6, 16.0 mg). The C2 (quercetin) compound completely inhibited the emergency, shoot height and root length of E. crus-galli at 1 mg/mL concentration (IC50 shoot height = 0.56 mg/mL). This was also the first study to report the isolation and allelopathic activity of lupeol, chrysoeriol and daucosterol from M. pigra leaf. Findings of this study highlighted that quercetin from M. pigra may become bio-herbicide to control barnyard grass and other grass weeds for the development of safe agriculture.

ZIKV Inhibitors Based on Pyrazolo[3,4-d]pyridazine-7-one Core: Rational Design, In Vitro Evaluation, and Theoretical Studies.

The Zika virus (ZIKV) is believed to cause birth defects, and no anti-ZIKV drugs have been approved by medical organizations to date. Starting from antimicrobial lead compounds with a pyrazolo[3,4-d]pyridazine-7-one scaffold, we synthesized 16 derivatives and screened their ability to interfere with ZIKV infection utilizing a cell-based phenotypic assay. Of these, five compounds showed significant inhibition of ZIKV with a selective index value greater than 4.6. In particular, compound 9b showed the best anti-ZIKV activity with a selectivity index of 22.4 (half-maximal effective concentration = 25.6 µM and 50% cytotoxic concentration = 572.4 µM). Through the brine shrimp lethality bioassay, 9b, 10b, 12, 17a, and 19a showed median lethal dose values in a range of 87.2-100.3 µg/mL. Compound 9b was also targeted to the NS2B-NS3 protease of ZIKV using molecular docking protocols, in which it acted as a noncompetitive inhibitor and strongly bound to five key amino acids (His51, Asp75, Ser135, Ala132, Tyr161). Utilizing the pharmacophore model of 9b, the top 20 hits were identified as prospective inhibitors of NS2B-NS3 protease, and six of them were confirmed for their stability with the protease via redocking and molecular dynamics simulations.

Anti-multiple myeloma potential of resynthesized belinostat derivatives: an experimental study on cytotoxic activity, drug combination, and docking studies.

Multiple myeloma is a deadly cancer that is a complex and multifactorial disease. In the present study, 12 belinostat derivatives (four resynthesized and eight new), HDAC inhibitors, were resynthesized via either Knoevenagel condensation, or Wittig reaction, or Heck reaction. Then an evaluation of the antiproliferative activities against myeloma cells MOPC-315 was carried out. Amongst them, compound 7f was the most bioactive compound with an IC50 of 0.090 ± 0.016 µM, being 3.5-fold more potent than the reference belinostat (IC50 = 0.318 ± 0.049 µM). Furthermore, we also confirmed the inhibitory activity of 7f in a cellular model. Additionally, we found that the inhibitory activity of 7f against histone deacetylase 6 catalytic activity (HDAC6) is more potent than that of belinostat. Finally, we observed the strong synergistic interaction between the derivative 7f and the proteasome bortezomib inhibitor (CI = 0.26), while belinostat and bortezomib showed synergism with a CI value of 0.36. Taken together, the above results suggest that 7f is a promising HDAC inhibitor deserving further investigation.

Use of Essential Oils for the Control of Anthracnose Disease Caused by Colletotrichum acutatum on Post-Harvest Mangoes of Cat Hoa Loc Variety.

Anthracnose disease caused by Colletotrichum spp. makes heavy losses for post-harvest mangoes of Cat Hoa Loc variety during storage, packaging, and transportation. The synthetic fungicides are commonly used to control the disease, but they are not safe for consumers' health and environment. This study was aimed to investigate the use of essential oils (EOs) as the safe alternative control. Pathogen was isolated from the infected Cat Hoa Loc mangoes and identified by morphology and DNA sequencing of the ITS region. Six EOs (cinnamon, basil, lemongrass, peppermint, coriander, and orange) were chemically analyzed by GC-MS. The antifungal activity of EOs was studied in vitro and in vivo. The results showed that the isolated pathogen was Colletotrichum acutatum. Cinnamon, basil, and lemongrass EOs effectively inhibited the growth of C. acutatum in descending order of cinnamon, basil, and lemongrass. However, they (except basil oil) severely damaged fruit peels. The antifungal activity was closely related to the main compounds of EOs. Basil EOs effectively controlled anthracnose development on Cat Hoa Loc mangoes artificially infected with C. acutatum, and its effectiveness was comparable to that of fungicide treatment. Consequently, basil EOs can be used as a biocide to control anthracnose on post-harvest Cat Hoa Loc mangoes.

Alfa glucosidase inhibitory, anti inflammatory activities and a new furanocoumarin derivative of Ruellia tuberosa.

Rullia tuberosa L. is used for treatment of diabetes mellitus, anti-inflammation, etc. However, its hypoglycaemic and anti inflammatory activities has not been investigated so far. In the present study, the α-glucosidase inhibitory, anti inflammatory activities of the extract of this plant were investigated. Our results showed that the crude extract as well as ethyl acetate and methanol fractions showed α-glucosidase inhibitory activity with IC50 of 15.84, 4.73 and 8.27 µg/ml, respectively. In addition, the hexane and ethyl acetate fractions are capable of inhibiting LPS-induced NO production with IC50 of 17.41 and 23.95 µg/mL, respectively. From the ethyl acetate and methanol fractions, eight compounds, including isobargaptol 5-O-ß-D-glucopyranoside (1), syringaresinol (2), catechin (3), pulmatin (4), stigmast-4-en-3-on (4), verbascoside (5), hydroxymethylfurfural (6), rutin (7), and homoplantaginin (8) were extracted and isolated. Their chemical structures were elucidated by spectroscopic method including MS, 1 D and 2 D- NMR and comparison with the literature values.

A new benzofuran derivative from the leaves of Ficus pumila L.

A new benzofuran derivative, pumiloside (1), together with seven known flavonoid glycosides, afzelin (2), astragalin (3), quercitrin (4), isoquercitrin (5), kaempferol 3-O-rutinoside (6), rutin (7) and kaempferol 3-O-sophoroside (8) were isolated from the leaves of Ficus pumila. Their structures were established by spectroscopic data and comparison with the literature values.