Prenylated arylbenzofuran derivatives from Morus mesozygia with antioxidant activity

Five prenylated arylbenzofurans, moracins Q-U, were isolated from Morus mesozygia (Moraceae). Their structures were elucidated on the basis of spectroscopic evidence. Along with these compounds, 3β-acetoxyurs-12-en-11-one, marsformoxide, moracin C, moracin M, moracin K, artocarpesin, cycloartocarpesin, morachalcone A were also isolated. Four of the five compounds, (moracins R-U) displayed potent antioxidant activity.     

Secondary metabolites of Bagassa guianensis Aubl. wood: A study of the chemotaxonomy of the Moraceae family

In order to explain the durability of the Moraceae plant family, phytochemistry of Bagassa guianensis was performed. Ethyl acetate extract was obtained from the heartwood and 18 secondary metabolites were isolated, including 6 moracins [6-O-methyl-moracin M, 6-O-methyl-moracin N and moracin Z; previously identified: moracin M, moracin N and moracin P], 8 stilbenoids [presently identified: (?)-epialboctalol and arachidin 4; previously identified: alboctalol, trans-resveratrol, arachidin 2, trans-oxyresveratrol and artogomezianol], 3 previously identified flavonoids, steppogenin, katuranin and dihydromorin, β-sitosterol and resorcinol. Previous studies suggest that stilbenoids are responsible for the natural durability of wood. Our study has determined that B. guianensis is closely related to Morus sp. in phylogeny and should be included in the Moreae sensu stricto tribe of the Moraceae family.     

SWATH‐based quantitative proteomics reveals the mechanism of enhanced Bombyx mori nucleopolyhedrovirus‐resistance in silkworm reared on UV‐B treated mulberry leaves

Bombyx mori nucleopolyhedrovirus (BmNPV) is one of the most acute infectious diseases in silkworm, which has led to great economic loss in sericulture. Previous study showed that the content of secondary metabolites in mulberry leaves, particularly for moracin N, was increased after UV‐B irradiation. In this study, the BmNPV resistance of silkworms reared on UV‐B treated and moracin N spread mulberry leaves was improved. To uncover the mechanism of enhanced BmNPV resistance, silkworm midguts from UV‐B treated mulberry leaves (BUM) and moracin N (BNM) groups were analyzed by SWATH‐based proteomic technique. Of note, the abundance of ribosomal proteins in BUM and BNM groups was significantly changed to maintain the synthesis of total protein levels and cell survival. While, cytochrome c oxidase subunit II, calcium ATPase and programmed cell death 4 involved in apoptotic process were up‐regulated in BNM group. Expressions of lipase‐1, serine protease precursor, Rab1 protein, and histone genes were increased significantly in BNM group. These results suggest that moracin N might be the main active component in UV‐B treated mulberry leaves which could improve the BmNPV‐resistance of silkworm through promoting apoptotic cell death, enhancing the organism immunity, and regulating the intercellular environment of cells in silkworm. It also presents an innovative process to reduce the mortality rate of silkworms infected with BmNPV.     

Scavenger receptors and atherosclerosis

Scavenger receptors were discovered as cell surface proteins capable of binding and internalization of modified lipoproteins. These receptors exhibit a broad ligand binding specificity including potential physiological and pathophysiological ligands other than modified lipoproteins. Different classes of scavenger receptors have been identified, and their relevance in normal and pathological conditions is under investigation. Recent in vitro and in vivo studies strongly support the role of class A and class B scavenger receptors in lipid transport and atherogenesis.     

Moracin M from Morus alba L. is a natural phosphodiesterase-4 inhibitor

Phosphodiesterase-4 (PDE4) has been identified to be a promising target for treatment of asthma. Moracin M extracted from Chinese herbal drug 'Sang-Bai-Pi' (Morus alba L.) was studied for the inhibitory affinity towards PDE4. It inhibited PDE4D2, PDE4B2, PDE5A1, and PDE9A2 with the IC(50) values of 2.9, 4.5, >40, and >100 μM, respectively. Our molecular docking and 8ns molecular dynamics (MD) simulations demonstrated that moracin M forms three hydrogen bonds with Gln369, Asn321, and Asp318 in the active site and stacks against Phe372. In addition, comparative kinetics analysis of its analog moracin C was carried out to qualitatively validate their inhibitory potency as predicted by the binding free energy calculations after MD simulations.     

Selection for Growth Performance in Broiler Chickens Associates with Less Diet Flexibility

Global competition for high standard feed-food resources between man and livestock, such as industrial broilers, is a concerning problem. In addition, the low productivity of scavenger chickens in developing countries leaves much to be desired. Changing the ingredients, and therefore, the nutrient composition of feed intake by commercial fed as well as scavenger chickens seems like an obvious solution. In this study, the ability of four broiler chicken breeds to perform on a commercial versus a scavenger diet was tested. The four broiler breeds differed genetically in growth potential. A significant (P < 0.01) negative effect of the scavenger diet on the bodyweight of the fast growing breeds was found and this effect decreased with decreasing growth rate in the other breeds. These differences in bodyweight gain could not be explained by differences in nutrient digestibility but were caused by the lack of ability of the fast growing breeds to increase their feed intake sufficiently.     

2-Arylbenzo[b]furan derivatives as potent human lipoxygenase inhibitors

Abstract

Human lipoxygenases (LOXs) have been emerging as effective therapeutic targets for inflammatory diseases. In this study, we found that four natural 2-arylbenzo[b]furan derivatives isolated from Artocarpus heterophyllus exhibited potent inhibitory activities against human LOXs, including moracin C (1), artoindonesianin B-1 (2), moracin D (3), moracin M (4). In our in vitro experiments, compound 1 was identified as the most potent LOX inhibitor and the moderate subtype selective inhibitor of 12-LOX. Compounds 1 and 2 act as competitive inhibitors of LOXs. Moreover, 1 significantly inhibits LTB4 production and chemotactic capacity of neutrophils, and is capable of protecting vascular barrier from plasma leakage in vivo. In addition, the preliminary structure–activity relationship analysis was performed based on the above four naturally occurring (1–4) and six additional synthetic 2-arylbenzo[b]furan derivatives. Taken together, these 2-arylbenzo[b]furan derivatives, as LOXs inhibitors, could represent valuable leads for the future development of therapeutic agents for inflammatory diseases.     

The molecular basis for the inhibition of phosphodiesterase-4D by three natural resveratrol analogs. Isolation,molecular docking,molecular dynamics simulations,binding free energy,and bioassay

The phosphodiesterase-4 (PDE4) enzyme is a promising therapeutic target for several diseases. Our previous studies found resveratrol and moracin M to be natural PDE4 inhibitors. In the present study, three natural resveratrol analogs [pterostilbene, (E)-2′,3,5′,5-tetrahydroxystilbene (THSB), and oxyresveratrol] are structurally related to resveratrol and moracin M, but their inhibition and mechanism against PDE4 are still unclear. A combined method consisting of molecular docking, molecular dynamics (MD) simulations, binding free energy, and bioassay was performed to better understand their inhibitory mechanism. The binding pattern of pterostilbene demonstrates that it involves hydrophobic/aromatic interactions with Phe340 and Phe372, and forms hydrogen bond(s) with His160 and Gln369 in the active site pocket. The present work also reveals that oxyresveratrol and THSB can bind to PDE4D and exhibits less negative predicted binding free energies than pterostilbene, which was qualitatively validated by bioassay (IC₅₀ = 96.6, 36.1, and 27.0 μM, respectively). Additionally, a linear correlation (R² = 0.953) is achieved for five PDE4D/ligand complexes between the predicted binding free energies and the experimental counterparts approximately estimated from their IC₅₀ values (≈RT ln IC₅₀). Our results imply that hydrophobic/aromatic forces are the primary factors in explaining the mechanism of inhibition by the three products. Results of the study help to understand the inhibitory mechanism of the three natural products, and thus help the discovery of novel PDE4 inhibitors from resveratrol, moracin M, and other natural products.     

冷害过程中黄瓜叶片SOD、CAT和POD活性的变化

实验选用3个耐冷力不同的黄瓜品种研究其叶片超氧化物歧化酶（SOD）、过氧化氢酶（CAT）和过氧化物酶（POD）等3种抗氧化酶活性在冷害过程中的变化。结果表明：低温胁迫期间的CAT和POD活性与黄瓜叶片的耐冷力表现一致,SOD活性则与其耐冷力表现相反。低温胁迫后,3个品种的所有3种抗氧化酶活性均降低,叶片表现出明显的冷害症状,但耐冷力较高的津优10号仍然具有相对较高的CAT活性。恢复期的SOD活性无显著性变化;耐冷力最弱的津研4号和耐冷力中等的津绿3号的CAT活性上升而津优10号的CAT活性降低;3个品种的POD活性都增高,但津研4号的上升幅度明显高于其它2个品种,可能与POD能催化活性氧（ROS）产生有关。     

Protein tyrosine phosphatase 1B inhibitors from Morus root bark

An organic layer prepared from the Chinese crude drug 'Sang-Bai-Pi' (Morus root bark) was studied in order to identify the inhibitory compounds for protein tyrosine phosphatase 1B (PTP1B). Bioassay-guided fractionation resulted in the isolation of sanggenon C (1), sanggenon G (2), mulberrofuran C (3) and kuwanon L (4) as PTP1B inhibitors, along with moracin O (5) and moracin P (6). Compounds 1-4 inhibited PTP1B with IC(50) values ranging from 1.6+/-0.3 microM to 16.9+/-1.1 microM.     

Role of nitric oxide dependence on nitric oxide synthase-like activity in the water stress signaling of maize seedling

Nitric oxide (NO) has been known as an important signal in plant antioxidative defense but its production and roles in water stress are less known. The present study investigated whether NO dependence on a NO synthase-lika (NOS) activity is involved in the signaling of drought-induced protective responses in maize seedlings. NOS activity, rate of NO release and drought responses were analyzed when NO donor sodium nitroprusside (SNP), NO scavenger c-PTIO (2-(4-carboxyphenyl)-4,4,5,5-tetramathylimidazoline-1-oxyl-3-oxide) and NOS inhibitor L-NAME (NG-nitro-L-arginine methyl ester) were applied to both detached maize leaves and whole plants. Both NOS activity and the rate of NO release increased substantially under dehydration stress. The high NOS activity induced by c-PTIO as NO scavenger and NO accumulation Inhibited by NOS inhibitor L-NAME In dehydration-treated maize seedlings Indicated that most NO production under water deficit stress may be generated from NOS-like activity. After dehydration stress for 3 h, detached maize leaves pretreated with NO donor SNP maintained more water content than that of control leaves pretreated with water. This result was consistent with the decrease in the transpiration rate of SNP-treated leaves subjected to drought treatment for 3 h. Membrane permeability, a cell injury index, was lower in SNP-trested maize leaves under dehydration stress for 4 h when compared with the control leaves. Also, superoxide dismutsse (SOD) activity of SNP combined drought treatment maize leaves was higher than that of drought treatment alone, indicating that exogenous NO treatment alleviated the water loss and oxidative damage of maize leaves under water deficit stress. When c-PTIO as a specific NO scavenger was applied, the effects of applied SNP were overridden. Treatment with L-NAME on leaves also led to higher membrane permeability, higher transpiration rate and lower SOD activities than those of control leaves, indicating that NOS-like activity was involved in the antioxidative defense under water stress. These results suggested that NO dependence on NOS-like activity serves as a signaling component in the induction of protective responses and is associated with drought tolerance in maize seedlings.     

一氧化氮在光延缓小麦叶片衰老中的作用

以小麦(Triticum aestivum L.)离体叶片为材料,采用药理学实验和激光扫描共聚焦显微镜技术,对内源一氧化氮(NO)在光延缓离体小麦叶片衰老过程中的作用进行了研究.结果显示:光照处理的同时添加NO清除剂血红蛋白(Hb)或硝酸还原酶抑制剂钨酸钠(Na2WO4)后,光抑制离体小麦叶片叶绿素和可溶性蛋白含量降低及丙二醛累积的效应均显著减弱;光照处理下小麦叶片硝酸还原酶活性和内源NO水平均明显高于黑暗条件下,而Na2WO4处理不仅能抑制光诱导的硝酸还原酶活性提高,还与Hb处理一样能显著降低光下叶片内源NO水平.结果表明,硝酸还原酶途径来源的NO参与了光抑制离体小麦叶片衰老的过程.     

Photosynthate translocation in Capsicum annuum

Summary The leaves of Capsicum annuum L. cv. California Wonder function as efficient carbon exporting organs for a large part of their life span. Young and old leaves export the same percentage of fixed carbon (74% within 24 hours) although fixation rates per unit area of young leaves may be three times that of old leaves. A constant feature of translocate distribution is a supply to the roots and to the terminal fruit of the main axis from both the main axis leaves and branch leaves. Carbon supply to branch fruit is flexible in that main axis leaves supply carbon to the very small fruit, but the subtending branch leaves supply more as the fruit grows and the branch node becomes more self-sufficient. Fruit are capable of carbon fixation but translocation to terminal fruit from main axis leaves supplies about 7.5 times as much carbon as direct fixation.     

Metal ion and antioxidant alterations in leaves between different sexes of Ginkgo biloba L

A comparative study was carried out to determine some valuable phytochemical components, macro- and microelement and redox parameters in leaves of male and female Ginkgo biloba trees and in extracts made from them. G. biloba extracts have become more popular as a therapeutic agent in the modern pharmacology in neurodegenerative diseases, in which increased brain metal levels can be observed and free radical reactions are involved. Macro- and microelement components, total phenol content, H-donating activity and reducing power as well as total scavenger capacity were determined in the samples. Well detectable differences were obtained for micro- and macroelement contents between male and female samples, but no toxic elements could be detected in the extracts. Male extracts contained more hazardous metals (e.g. Fe) compared to the female ones, while extracts from female leaves had higher levels of ions, which are known to have beneficial effects in neurodegenerative diseases. The ethanolic extracts of male leaves showed the highest H-donating activity, reducing power and total phenol content, as well as the best total scavenger activity. Ginkgo extracts due to the antioxidant properties may have favourable effects as dietary supplements in several neurodegenerative diseases, but this study draws the attention that critical evaluation is required in view of the potential hazard induced by their metal ion constitution. Our results lead us to the conclusion that although the aqueous extracts of female leaves are characterized by relatively lower antioxidant properties, they may be more eligible for these purposes due to their favourable metal ion constitution.     

Effects of urate, a natural inhibitor of peroxynitrite-mediated toxicity, in the response of Arabidopsis thaliana to the bacterial pathogen Pseudomonas syringae

Urate, a natural peroxynitrite scavenger, has been used to investigate the possible role of peroxynitrite during plant-pathogen interactions. Urate greatly reduced lesion formation in Arabidopsis leaves treated with an abiotic peroxynitrite-generating system or with a peroxynitrite solution, indicating that it can act as an effective scavenger in planta. In the interaction with the avirulent Pseudomonas syringae pv. phaseolicola (avrRPM1+), cell death in the inoculated area was strongly reduced by urate, without compromising disease resistance. In contrast, urate promoted discrete cell death in response to an isogenic Pseudomonas syringae (avrRPM1-), which did not trigger an HR when inoculated alone, and it induced resistance and arrest of pathogen growth. Scavenging of peroxynitrite did not modify the response of Arabidopsis to an avirulent strain of Xanthomonas campestris pv campestris, that showed a high resistance to NO and peroxynitrite. Our data indicate that peroxynitrite plays a significant role in the responses of plants to Pseudomonas syringae.     

Food choice from endemic North Carolina tree species by captive prosimians (Lemur fulvus)

Seven captive-born lemurs (Lemur fulvus) at the Duke University Primate Center were presented with leaves of different maturity from five species of North Carolina trees. The animals demonstrated three distinct behaviors toward the novel plant material. They sniffed, tasted, and/or ingested it. New leaves were sniffed, but little tasting and ingestion was observed. Intermediate pine needles were sniffed and ingested but little tasted. Mature leaves were sniffed equally, but the mature leaves of tulip trees and honeysuckle were tasted significantly more than pine, sweetgum, and red maple. Pine, sweetgum, and red maple were ingested significantly more than tulip trees and honeysuckle. Male lemurs ate significantly more mature pine needles and new sweetgum leaves than did the females. Chemical analysis of these plant materials indicated that the new and mature leaves of tulip tree and honeysuckle contained alkaloids. Captive-born lemurs apparently use their sense of smell and taste in choosing what to eat and seem just as capable as free-ranging animals in finding food when faced with the chemical defenses that protect trees from insect predation.     

干旱胁迫下紫花苜蓿幼苗非结构性碳水化合物代谢对NO的响应

以紫花苜蓿（Medicago sativa）为材料,采用盆栽试验方法,用聚乙二醇（PEG-6000）作为渗透介质模拟干旱胁迫,外源喷施NO供体硝普钠,NO清除剂（carboxy-PTIO,cPTIO）,对紫花苜蓿幼苗叶片、根系中非结构性碳水化合物含量及相关酶活性的变化进行研究,探讨NO对紫花苜蓿耐旱机制的作用。结果表明：外源NO促进了紫花苜蓿叶片中淀粉的分解、根系中淀粉的积累,提高叶片及根系中可溶性糖（蔗糖、果糖和葡萄糖）含量,降低了渗透势,促进细胞吸水,缓解干旱造成的损伤。此外,外源NO能提高干旱胁迫下紫花苜蓿叶片中蔗糖合成酶（SS）、酸性转化酶（AI）和中性转化酶（NI）活性,降低了蔗糖磷酸合成酶（SPS）的活性,提高根系中SS、SPS和转化酶活性,使蔗糖的合成与分解处于高水平的动态平衡,增强了紫花苜蓿的抗旱性。而NO清除剂cPTIO则会不同程度的抑制紫花苜蓿幼苗中非结构性碳水化合物（NSC）及其相关酶活性。因此,NO可以通过调控NSC的代谢响应干旱胁迫,缓解干旱胁迫造成的不利影响,在紫花苜蓿的抗旱中扮演着重要的角色。     

Stomatal closure in sweet potato leaves induced by sulfur dioxide involves H2S and NO signaling pathways

Sulfur dioxide (SO₂) is a well-known and widespread air pollutant but it also acts as signaling molecule in various processes in animals. However, there is limited information on the role of SO₂ in plants except of its toxicity. Here we studied the role of SO₂ on stomatal movements in sweet potato (Ipomoea batatas) leaves. SO₂, generated by Na₂SO₃/NaHSO₃ solutions, was applied on epidermal strips. We found that the SO₂ donor induced stomatal closure in a dose-dependent manner. Rapid increases in endogenous hydrogen sulfide and nitric oxide content levels were observed in leaves after the treatment with the SO₂ donor. The SO₂-induced stomatal closure was reversed by the H₂S scavenger hypotaurine and the NO-specific scavenger cPTIO. Our results indicate that the SO₂-induced stomatal closure was likely mediated by the H₂S and NO signaling pathways.     

Induction of ethylene synthesis and lipid peroxidation in damaged or TMV-infected tobacco leaf tissues by light

The effect of light on ethylene and ethane production in damaged leaf tissues was investigated. When whole leaves of tobacco cv. Samsun NN were damaged with liquid nitrogen, the ethylene formation was the highest, if 100?% of leaves were injured and were kept in the light, the lowest when leaves after 100?% injury were kept in darkness. Ethane production (lipid peroxidation) could be detected only in damaged, but not in control leaves, and was much higher in light than in darkness. In addition, there was a strong degradation of chlorophyll of damaged leaves kept in light. In light aminoethoxy-vinylglycine (AVG) inhibited ethylene formation in control, non-damaged whole leaves effectively, but in leaves with 100?% damage the inhibitory effect was much weaker and similar to the effect of propyl gallate (PG), a free radical scavenger. Both AVG and PG treatments decreased ethylene formation by control leaf discs and discs with 100?% damage. Ethane production was significantly inhibited by PG and slightly by AVG in the case of 100?% damage. Tiron, another free radical scavenger gave similar results on leaf discs as PG did. Paraquat (methylviologen, Pq), as a photosynthesis inhibiting and reactive oxygen species (ROS) producing herbicide produced a large amount of ethylene and ethane in light but very small amount in darkness. In accordance, tobacco mosaic virus (TMV) infection on the necrotic host resulted in significantly larger amount of ethylene and ethane formation in light than in darkness. We conclude that ethylene and ethane production of damaged plant tissues is strongly induced by light and ROS that are involved in this induction.