Zeylleucapenoids A-D, Highly Oxygenated Diterpenoids with Anti-Inflammatory Activity from Leucas zeylanica (L.) R. Br.

Four previously undescribed highly oxygenated diterpenoids (1-4), zeylleucapenoids A-D, characterized by halimane and labdane skeletons, were isolated from the aerial parts of Leucas zeylanica. Their structures were elucidated primarily via NMR experiments. The absolute configuration of 1 was established using theoretical ECD calculations and X-ray crystallographic analysis, whereas those for 2-4 were assigned using theoretical ORD calculations. Zeylleucapenoids A-D were tested for anti-inflammatory activity against nitric oxide (NO) production in RAW264.7 macrophages, of which only 4 showed significant efficacy with an IC50 value of 38.45 µM. Further, active compound 4 was also evaluated for the inhibition of the release of pro-inflammatory cytokines TNF-α and IL-6 and was found to have a dose-dependent inhibitory effect, while it showed nontoxic activity for zebrafish embryos. A subsequent Western blotting experiment revealed that 4 inhibited the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Furthermore, molecular docking analysis indicated that the possible mechanism of action for 4 may be bind to targets via hydrogen and hydrophobic bond interactions.

2,4-dichlorophenoxyacetic acid induces ROS activation in NLRP3 inflammatory body-induced autophagy disorder in microglia and the protective effect of Lycium barbarum polysaccharide.

The pesticide 2,4-dichlorophenoxyacetic acid (2,4-D) exerts neurotoxic effects; however, its action mechanism remains unclear. Here, we used BV2 cells as a model and divided them into six groups: control group (serum-free medium), lipopolysaccharide (LPS) (1 µg/mL), 2,4-D (1.2 µmol/mL), Lycium barbarum polysaccharide (LBP; 300 µg/mL LBP), LPS (1 µg/mL) + LBP (300 µg/mL), and 2,4-D (1.2 µmol/mL) + LBP (300 µg/mL) with dimethyl sulfoxide as the solvent. Our results showed that 2,4-D treatment decreased superoxide dismutase and glutathione peroxidase activities and increased malondialdehyde content. The percentage of microglial activation (co-expression of ionized calcium-binding adaptor protein-1 + CD68) in the LPS and 2,4-D groups and the levels of tumor necrosis factor alpha, interleukin (IL) 1 beta, IL-6, and IL-18 in the cell supernatant were increased. The protein and mRNA levels of Nod-like receptor protein 3 (NLRP3), apoptosis-associated speck-like protein, caspase-1, IL-1ß, IL-18, and p62 increased, whereas those of LC3II/I and Beclin-1 decreased in the 2,4-D group. The protein expression and mRNA levels of NLRP3, cleaved caspase-1, IL-1ß, IL-18, and p62 decreased significantly, whereas the protein expression and mRNA levels of LC3II/I and Beclin-1 increased in small interfering RNA of NLRP3-treated BV2 cells stimulated with 2,4-D and LPS. In conclusion, 2,4-D enhanced cell migration, promoted oxidative stress, induced excessive release of mitochondrial reactive oxygen species, promoted microglial cell activation, released inflammatory factors, activated NLRP3 inflammasomes, and inhibited autophagy. Meanwhile, LBP reduced inflammation and the release of mitochondrial reactive oxygen species, inhibited NLRP3 inflammasome activation, and regulated autophagy, thereby playing a neuroprotective role.

Effects of 2,4-dichlorophenoxyacetic acid on the expression of NLRP3 inflammasome and autophagy-related proteins as well as the protective effect of Lycium barbarum polysaccharide in neonatal rats.

The pesticide 2,4-dichlorophenoxyacetic acid (2,4-D) has neurotoxic effects, but its mechanism is not clear. In this study, a 2,4-D (75 mg/kg. b.w) exposure model was established in SD rats with colostrum. Lipopolysaccharide (1 mg/kg b.w) was used as the positive control, and Lycium barbarum polysaccharide (LBP, 50 mg/kg b.w) was used as an intervention factor to explore the neurotoxic effect of 2,4-D and the neuroprotective effect of LBP. Our research results show that 2,4-D causes a decrease in the number of hippocampal CA3 pyramidal cells and pyknosis in nuclei with a triangular or irregular shape and that rats show signs of anxiety or depression. In rat serum, superoxide dismutase, and glutathione peroxidase activity decreased, while malondialdehyde content increased. Protein and mRNA levels of TNFα, IL-6, IL-1ß, IL-18, NLRP3, ASC, caspase-1, IL-1ß, IL-18, and p62 increased, while those of LC3-II/LC3-I and Beclin-1 decreased in hippocampal tissues. In conclusion, 2,4-D increased the oxidative stress level, induced neuroinflammatory response, and decreased the autophagy level in experimental rats. LBP may have upregulated the autophagy level in the body by inhibiting the activation of the NLRP3 inflammasome, thus playing a neuroprotective role.

Responses of root architecture development to low phosphorus availability: a review.

BACKGROUND: Phosphorus (P) is an essential element for plant growth and development but it is often a limiting nutrient in soils. Hence, P acquisition from soil by plant roots is a subject of considerable interest in agriculture, ecology and plant root biology. Root architecture, with its shape and structured development, can be considered as an evolutionary response to scarcity of resources. SCOPE: This review discusses the significance of root architecture development in response to low P availability and its beneficial effects on alleviation of P stress. It also focuses on recent progress in unravelling cellular, physiological and molecular mechanisms in root developmental adaptation to P starvation. The progress in a more detailed understanding of these mechanisms might be used for developing strategies that build upon the observed explorative behaviour of plant roots. CONCLUSIONS: The role of root architecture in alleviation of P stress is well documented. However, this paper describes how plants adjust their root architecture to low-P conditions through inhibition of primary root growth, promotion of lateral root growth, enhancement of root hair development and cluster root formation, which all promote P acquisition by plants. The mechanisms for activating alterations in root architecture in response to P deprivation depend on changes in the localized P concentration, and transport of or sensitivity to growth regulators such as sugars, auxins, ethylene, cytokinins, nitric oxide (NO), reactive oxygen species (ROS) and abscisic acid (ABA). In the process, many genes are activated, which in turn trigger changes in molecular, physiological and cellular processes. As a result, root architecture is modified, allowing plants to adapt effectively to the low-P environment. This review provides a framework for understanding how P deficiency alters root architecture, with a focus on integrated physiological and molecular signalling.

[Effects of elevated CO2 concentration on the quality of agricultural products: a review].

The increasing concentration of atmospheric CO2 and the nutritional quality of human diets are the two important issues we are facing. At present, the atmospheric CO2 concentration is about 380 micromol mol(-1), and to be reached 550 micromol mol(-1) by 2050. A great deal of researches indicated that the quality of agricultural products is not only determined by inherited genes, but also affected by the crop growth environmental conditions. This paper summarized the common methods adopted at home and abroad for studying the effects of CO2 enrichment on the quality of agricultural products, and reviewed the research advances in evaluating the effects of elevated CO2 on the quality of rice, wheat, soybean, and vegetables. Many experimental results showed that elevated CO2 concentration causes a decrease of protein content in the grains of staple food crops and an overall decreasing trend of trace elements contents in the crops, but improves the quality of vegetable products to some extent. Some issues and future directions regarding the effects of elevated CO2 concentration on the quality of agricultural products were also discussed, based on the present status of related researches.

Insecticide resistance profiles and synergism in field populations of the German cockroach (Dictyoptera: Blattellidae) from Singapore.

The resistance profiles of 22 field-collected populations of the German cockroach, Blattella germanica (L.) (Dictyoptera: Blattellidae), from various localities in Singapore were determined by topical bioassay against novel and conventional insecticides from six classes: (1) pyrethroid (beta-cyfluthrin, deltamethrin), (2) carbamate (propoxur), (3) organophosphate (chlorpyrifos), (4) phenyl pyrazole (fipronil), (5) neonicotinoid (imidacloprid), and (6) oxadiazine (indoxacarb). Compared with a laboratory susceptible strain, resistance levels ranged from 3.0 to 468.0x for the pyrethroids, from 3.9 to 21.5x for the carbamate, from 1.5 to 22.8X for the organophosphate, from 1.0 to 10.0X for phenyl pyrazole, and were absent or low for the neonicotinoid (0.8-3.8x) and the oxadiazine (1.4-5.3x). One strain demonstrated broad-spectrum resistance to most of the insecticides. Synergism studies using piperonyl butoxide (PBO) and S,S,S-tributylphosphorotrithioate (DEF) in combination with a discriminating dose (LD99) of selected insecticides were conducted to test for possible resistance mechanisms. Resistance to pyrethroid was reduced with PBO and DEF, suggesting the involvement of P450 monooxygenase and esterases in conferring resistance. Propoxur resistance also was suppressed with PBO and DEF, and coadministration of both synergists resulted in complete negation of the resistance, indicating the involvement of both P450 monooxygenase and esterase. In six B. germanica field strains evaluated, esterases were found to play a role in chlorpyrifos resistance, whereas the P450 monoxygenase involvement was registered in three strains. Additional resistance mechanisms such as kdr-type and Rdl mutation contributing toward pyrethroid and fipronil resistance, respectively, also may be involved in some strains in which the resistance levels were not affected by the synergists. We conclude that insecticide resistance is prevalent in field German cockroach populations in Singapore.