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Three new prenylated C 6 -C 3 compounds ( 1-3 ), together with two known prenylated C 6 -C 3 compounds ( 4-5 ) and one known C 6 -C 3 derivative ( 6 ), were isolated from the roots of Illicium brevistylum A. C. Smith. The structures of 1-3 were elucidated by spectroscopic methods including 1D and 2D NMR, HRESIMS, CD experiments and ECD calculations. The structure of illibrefunone A ( 1 ) was confirmed by single-crystal X-ray diffraction analysis. All compounds were evaluated in terms of their anti-inflammatory potential on nitric oxide (NO) generation in lipopolysaccharide-stimulated murine RAW264.7 macrophages and murine BV2 microglial cells, antiviral activity against Coxsackievirus B3 (CVB3) and influenza virus A/Hanfang/359/95 (H3N2). Compounds 3 and 4 exhibited potent inhibitory effects on the production of NO in RAW 264.7 cells with IC 50 values of 20.57 and 12.87 μM respectively, which were greater than those of dexamethasone (positive control). Compounds 1 and 4-6 exhibited weak activity against Coxsackievirus B3, with IC 50 values ranging from 25.87 to 33.33 μM.

Soil organic matter serves as a crucial indicator for soil quality. Albic soil, characterized by a barrier layer, exhibits limitations in organic matter content, which can adversely affect crop growth and development. To elucidate the impact of deep mixing of various organic materials on the redistribution of organic matter in the surface soil of albic soil could provide theoretical and technical insights for establishing suitable plough layers for albic soil in Northeast China. We conducted a two-year positioning experiment in Shuangyashan, Heilongjiang Province with five treatments, conventional shallow tillage (0-15 cm, CK), inversion tillage (0-35 cm) without or with straw return (T 35 and T 35 +S), inversion tillage with cattle manure (T 35 +M) and cattle manure plus maize straw (T 35 +S+M). The results showed that soil fertilization via deep mixing of organic materials to a depth of 35 cm significantly increased maize yield in albic soil, with the T 35 +S+M treatment demonstrating the most pronounced effect, yielding an average production of 2934.76 kg·hm -2 . Compared to CK, the T 35 treatment resulted in a significant 8.4% decrease in organic matter content in the tillage layer, a significant 7.6% increase in organic matter in the sub-tillage layer, and a relative richness degree of soil organic matter in the sub-tillage layer increased by 17.5%. Deep mixed return of organic materials following deep ploughing markedly increased organic matter content of the plough layer, with organic matter conversion ranging from 16.3% to 31.0%. In comparison to the T 35 treatment, there was no significant increase in soil organic matter content in the T 35 +S tillage layer and sub-tillage layer. Conversely, soil organic matter content increased by 4.6% and 6.9% in the T 35 +M and T 35 +S+M treatments, with corresponding increase of 11.2% and 15.4% in sub-tillage layer, respectively. Additionally, the soil organic matter richness index in sub-tillage layer increased by 2.5% and 5.1%, respectively. There was a significant positive correlation between organic matter content in the entire plough layer and maize yield, with a contribution rate of 17.5%. Therefore, the utilization of organic fertilizer or a combination of organic fertilizer and straw deep mixing can quickly fertilize albic soil by increasing soil organic matter content in both the whole tillage layer (0-35 cm) and the sub-tillage layer (15-35 cm).

Six previously undescribed prenylated C 6 -C 3 derivatives ( 1 - 6 ) were isolated from the root of Illicium ternstroemioides A. C. Smith. Their structures were elucidated based on extensive spectroscopic analyses (UV, IR, 1D and 2D NMR, and HRESIMS). The absolute configurations of 1 - 3 were determined using electronic circular dichroism (ECD), and Mo 2 (OAc) 4 induced circular dichroism (ICD). Compound 3 exhibited weak activity against Coxsackievirus B3 with an IC 50 value of 33.3 µM, and compound 5 exhibited more potent activity against Coxsackievirus B3 with an IC 50 value of 6.4 µM.

Three new cadinane sesquiterpenes ( 1 - 3 ) and three known sesquiterpenes were isolated from the stems and branches of Illicium ternstroemioides A. C. Smith. The structures of the new compounds were elucidated by extensive analysis of spectroscopic and HRESIMS data. The structures of illiternins A-C ( 1 - 3 ) were confirmed by single crystal X-ray diffraction, allowing for the determination of their absolute configurations. Compounds 3 and 6 exhibited antiviral activity against Coxsackievirus B3 with IC 50 values of 33.3 and 57.7 μM, respectively.

Fifteen unreported prenylated C 6 -C 3 derivatives (1-15) were isolated from the stems and branches of Illicium ternstroemioides A. C. Smith, including one bis-prenylated C 6 -C 3 derivative (1), three prenylated C 6 -C 3 derivative-shikimic acid ester hybrids (2-4) and 11 prenylated C 6 -C 3 monomers (5-15). The structures of compounds 1-15 were elucidated by spectroscopic analysis (UV, IR, 1D and 2D NMR, and HRESIMS). The absolute configurations of the compounds were determined using electronic circular dichroism (ECD), induced circular dichroism (ICD), and the modified Mosher's method. Among the isolates, compounds 11, 12, and 15 exhibited significant anti-inflammatory activities by inhibiting the nitric oxide with IC 50 values ranging from 1.89 to 24.83 μM in lipopolysaccharide-stimulated murine RAW 264.7 macrophages and murine BV2 microglial cells; compounds 2, 3, and 7 exhibited antiviral activitives against Coxsackievirus B3 with an IC 50 value of 33.3, 25.9, and 27.8 μM, respectively., Competing Interests: Declaration of Competing Interest The authors declare no competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023. Published by Elsevier B.V.)

Polymerase chain reaction (PCR) is commonly used to detect Listeria monocytogenes, foodborne pathogen. This study conducted in silico genomic analysis to investigate the specificity and binding efficacy of four published pairs of PCR primers targeting Listeria prfA-virulence gene cluster (pVGC) based on Listeria sequences available. We first performed comprehensive genomic analyses of the pVGC, the main pathogenicity island in Listeria spp. In total, 2961 prfA, 642 plcB, 629 mpl, and 1181 hlyA gene sequences were retrieved from the NCBI database. Multiple sequence alignments and phylogenetic trees were generated using unique (non-identical or not-shared) sequences of each represented genes, targeting four pairs of PCR primers published previously, namely 202 prfA, 82 plcB, 150 mpl, and 176 hlyA unique gene sequences. Only the hlyA gene showed strong (over 94%) primer mapping results, while prfA, plcB, and mpl genes showed weak (<50%) matching results. In addition, nucleotide variations were observed at the 3' end of the primers, indicating non-binding to the targets could potentially cause false-negative results. Thus, we propose designing degenerate primers or multiple PCR primers based on as many isolates as possible to minimize the false-negative risk and reach the aim of low tolerable limits of detection., (© His Majesty the King in Right of Canada, 2023.)

Chemical investigation of an alcohol extract from the twigs and leaves of Illicium henryi Diels resulted in the isolation of two new acorane-related seco-sesquiterpenes (1 and 3), two new acorane-related seco-norsesquiterpenes (2 and 4), one new 2-epi-cedrane sesquiterpene (5), eight new acorane-type sesquiterpenes (6-13), and a known major constituent of acorenone B (14). Their structures were established by interpreting extensive spectroscopic data, including HRESIMS, NMR ( 1 H and 13 C NMR, 1 H- 1 H COSY, HSQC, and HMBC), and NOE difference spectra analysis. The absolute configurations of 1, 2, 4-7, 9, 10, and 14 were determined by X-ray crystallography, while chemical transformation methods were performed with compound 14 as the starting material to elegantly solve the absolute configuration issue of compounds 8 and 11-13. Notably, 1 and 2 are seco-sesquiterpenes that are related to acorane and possess an unusual ketal-linked hemiacetal in a 6,8-dioxabicyclo[3.2.1]octan-7-ol scaffold ring system. Plausible biosynthetic pathways for compounds 1-14, which were derived from the acorane skeleton, were proposed. All the isolated compounds (1-14) were evaluated for their antiviral and cytotoxic activities., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2022 Elsevier Inc. All rights reserved.)

Background: 3-acetyl-11-keto-beta-boswellic acid (AKBA) and 11-keto-boswellic acid (KBA) are the main active components of frankincense as pentacyclic triterpenoids, which are designated by the European Pharmacopoeia 8.0 as the quality standard for the evaluation of Indian frankincense, 2-methoxy-8,12-epoxygermacra- 1(10),7,11-trien-6-one (MCS134) is a non-volatile sesquiterpene compound in myrrh., Objective: In this paper, the absorption pharmacokinetics and metabolites of AKBA, KBA and MCS134 after frankincense, myrrh and their compatibility were analyzed, elaborated their absorption and metabolism mechanism and provided the ideas for the research on the bioactive components of frankincense and myrrh compatibility in vivo ., Methods: The area under the blood concentration time curve (AUC), half-life (t_1/2) and drug clearance (CL) of AKBA, KBA and MCS134 in rats were analyzed by LC-TQ / MS. The metabolites of AKBA, KBA and MCS134 in rats were analyzed by ultra-high pressure liquid chromatography with a linear ion trap-high resolution Orbitrap mass spectrometry system (UHPLC-LTQ-Orbitrap-MS)., Results: The results showed that AKBA, KBA and MCS134 reached the maximum plasma concentration at about 2 h, 2 h and 15 min, respectively. AUC_0-t and t_1/2 of the three components increased in varying degrees after compatibility, and the clearance/ bioavailability (CL/F) decreased. AKBA, KBA and MCS134 were metabolized in phase I and phase II in rats, and there represented differences before and after compatibility., Conclusion: After the compatibility of frankincense and myrrh, the absorption of effective components was improved to some extent, and there were some differences in the metabolites in rats. The results provide ideas for elucidating the in vivo effect mechanism of frankincense and myrrh., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Layered Ni-rich lithium transition metal oxides are promising battery cathodes due to their high specific capacity, but their poor cycling stability due to intergranular cracks in secondary particles restricts their practical applications. Surface engineering is an effective strategy for improving a cathode's cycling stability, but most reported surface coatings cannot adapt to the dynamic volume changes of cathodes. Herein, a self-adaptive polymer (polyrotaxane-co-poly(acrylic acid)) interfacial layer is built on LiNi 0.6 Co 0.2 Mn 0.2 O 2 . The polymer layer with a slide-ring structure exhibits high toughness and can withstand the stress caused by particle volume changes, which can prevent the cracking of particles. In addition, the slide-ring polymer acts as a physicochemical barrier that suppresses surface side reactions and alleviates the dissolution of transition metallic ions, which ensures stable cycling performance. Thus, the as-prepared cathode shows significantly improved long-term cycling stability in situations in which cracks may easily occur, especially under high-rate, high-voltage, and high-temperature conditions., (© 2022 Wiley-VCH GmbH.)

The plating/stripping of Li dendrites can fracture the static solid electrolyte interphase (SEI) and cause significant dynamic volume variations in the Li anode, which give rise to poor cyclability and severe safety hazards. Herein, a tough polymer with a slide-ring structure was designed as a self-adaptive interfacial layer for Li anodes. The slide-ring polymer with a dynamically crosslinked network moves freely while maintaining its toughness and fracture resistance, which allows it can to dissipate the tension induced by Li dendrites on the interphase layer. Moreover, the slide-ring polymer is highly stretchable, elastic, and displays an ultrafast self-healing ability, which allows even pulverized Li to remain coalesced without disintegrating upon consecutive cycling. The Li anodes demonstrate greatly improved suppression of Li dendrite formation, as evidenced by the high critical current density (6 mA cm -2 ) and stable cycling for the full cells with high-areal capacity LiFePO 4 , high-voltage NCM, and S cathodes., (© 2021 Wiley-VCH GmbH.)

The construction of libraries of stereoisomers of natural products serves as an important approach to investigating the correlation between the stereostructure and biological activity. However, the total synthesis and isomerzation of polycyclic scaffolds with multiple chrial centers are rare. Spirooliganin ( 1 ), a new skeleton natural product isolated from the plant Illicium oligandrum , was structurally characterized by comprehensive analysis of NMR spectroscopic data and ECD which revealed an unprecedented 5-6-6-6-7 polycyclic framework with six chiral centers. Here we report a 17-step total synthesis to prepare a library of stereochemically diverse isomers of spirooliganin, including 16 diastereoisomers and 16 regioisomers. In addition to a regioselective hetero-Diels-Alder cycloaddition, the synthetic strategy involves a photo-induced stereoselective Diels-Alder reaction, which gives only the abnormal trans -fused product as rationalized by density functional theory calculations. Preliminary biological evaluation showed that spirooliganin and regioisomers 39 exhibited potent inhibition of Coxsackievirus B3. It also revealed the pharmacophore effect of the D-ring (16 R ,18 R ,24 R , and 26 R ) for their antiviral activities., Competing Interests: There are no conflicts to declare., (This journal is © The Royal Society of Chemistry.)

Transforming growth factor beta (TGF-β) plays an important role in the viral liver disease progression via controlling viral propagation and mediating inflammation-associated responses. However, the antiviral activities and mechanisms of TGF-β isoforms, including TGF-β1, TGF-β2 and TGF-β3, remain unclear. Here, we demonstrated that all of the three TGF-β isoforms were increased in Huh7.5 cells infected by hepatitis C virus (HCV), but in turn, the elevated TGF-β isoforms could inhibit HCV propagation with different potency in infectious HCV cell culture system. TGF-β isoforms suppressed HCV propagation through interrupting several different stages in the whole HCV life cycle, including virus entry and intracellular replication, in TGF-β/SMAD signalling pathway-dependent and TGF-β/SMAD signalling pathway-independent manners. TGF-β isoforms showed additional anti-HCV activities when combined with each other. However, the elevated TGF-β1 and TGF-β2, not TGF-β3, could also induce liver fibrosis with a high expression of type I collagen alpha-1 and α-smooth muscle actin in LX-2 cells. Our results showed a new insight into TGF-β isoforms in the HCV-related liver disease progression., (© 2021 The Authors. Journal of Cellular and Molecular Medicine published by Foundation for Cellular and Molecular Medicine and John Wiley & Sons Ltd.)

Tree regeneration is significantly affected by water deficiency, which could be alleviated by the inoculation of Trichoderma spp . In this study, the effects of rhizosphere inoculation with Trichoderma spp . on the antioxidant system and osmotic substances in the seedlings of Larix principis-rupprechtii was investigated under experimental drought stresses, with the relative water content 50%-60%, 35%-50%, and 20%-35% as the light, moderate and severe drought stress, respectively. The results showed that, with increasing drought stress, the activities of protective enzymes, SOD and POD in the needles of seedlings were significantly promoted, the contents of MDA and proline were remarkably increased, whereas the contents of soluble protein and starch showed a decreasing trend. Inoculation with Trichoderma spp . promoted much stronger increase in the activities of SOD and POD in the needles, yet the MDA content showed a lower level of increase. Under moderate drought, the activity of POD in the seedling inoculated with Trichoderma spp . was 1.8 folds of that in the control, while the content of MDA was 62.9% of the control. The contents of proline, soluble protein, soluble sugar, and starch in the inoculated seedlings were higher than that in the uninoculated seedlings. Drought-resistance of L. principis-rupprechtii seedlings inoculated by Trichoderma spp. was significantly enhanced due to the augmenting regulation of antioxidant system and osmotic adjustment substances. Therefore, under the trend of warming and drying in North China, the technique of rhizosphere inoculation of Trichoderma spp. could be popularized for forest plantation or understory tending.

Two different synthetic methods, the direct method and the substitution method, were used to synthesize the Cs-POM@MOF-199@MCM-41 (Cs-PMM), in which the modified heteropolyacid with cesium salt has been encapsulated into the pores with the mixture of MOF and MCM-41. The structural properties of the as-prepared catalysts were characterized using various analytical techniques: powder X-ray diffraction, FT-IR, SEM, TEM, XPS and BET, confirming that the Cs-POM active species retained its Keggin structure after immobilization. The substitution method of Cs-PMM exhibited more excellent catalytic performance for oxidative desulfurization of dibenzothiophene in the presence of oxygen. Under optimal conditions, the DBT conversion rate reached up to 99.6% and could be recycled 10 times without significant loss of catalytic activity, which is mainly attributed to the slow leaching of the active heteropolyacid species from the strong fixed effect of the mixture porous materials., (Copyright © 2017. Published by Elsevier B.V.)

Taxus chinensis var. mairei is a national Category 1 protective species in China, with its northernmost natural distribution to the southeast of Shanxi Province, China. This study was conducted to investigate the natural distribution of T. chinensis var. mairei in Shanxi Province. The community classification, species diversity, population structure and competition intensity of T. chinensis var. mairei were studied. The results showed that T. chinensis var. mairei mainly formed four community types, including the community of T. chinensis var. mairei + Carpinus turczaninowii, the community of T. chinensis var. mairei - Vitex negundo var. heterophylla, the community T. chinensis var. mairei - Clerodendrum trichotomum and the community of T. chinensis var. mairei + Quercus variabilis. T. chinensis var. mairei was concentratedly distributed in Mohe of Linchuan County and Manghe Nature Reserve of Yangcheng County, and scattered in some other areas. The communities had an obviously vertical structure, with T. chinensis var. mairei trees growing into main canopy which were about 8-10 m high in mixed forests and 5-6 m high in pure forests. The species diversity index and evenness index had significant difference among the four community types. The average height of T. chinensis var. mairei was 5.16 m. The individuals in tree layer and succession layer were 43.4% and 56.6%, respectively, while they were scarce in the regeneration layer. 67.6% of the trees were small-diameter (DBH＜16 cm) and only 4.0% were large-diameter (32 cm≤DBH＜40 cm). T. chinensis var. mairei was considered to be lack of seedlings because only 4 seedlings were found, which might result in the declination of this species in future. T. chinensis var. mairei in Shanxi Province showed relatively concentrated distribution, with most individuals being small-diameter, resulting in tense intraspecific competition which accounted for 61.8% of the total intensity. The interspecific competition to T. chinensis var. mairei was mainly from C. turczaninowii and Q. variabilis, which were two dominant tree species with larger population in this area.

In this paper, we design a tunable strength multiband absorber consisting of a graphene metamaterial structure and a thick dielectric interlayer deposited on a metal ground plane. We investigate the tunable conductivity properties of the graphene metamaterial and demonstrate multiband absorbers with three absorption bands using a polyimide interlayer in the 0-2.25 THz range by numerical simulation. The results show that the mix absorptivity reached 99.8% at 1.99 THz, and the absorptive strength can be tuned with the modulation depth up to 84.2%. We present a theoretical interpretation based on a standing wave field, which shows that the field energy is localized inside the thicker spacer and then dissipated, effectively trapping the light in the metamaterial absorbers with negligible near-field interactions. The standing wave field theory developed here explains all the features of the multiband metamaterial absorbers and provides a profound understanding of the underlying physics.

A series highly efficient and stable metallophthalocyanine/La0.8Ce0.2NiO3 (ML/LCNO) photocatalysts were prepared by a facile sol-gel and immersion method. The as-prepared samples were characterized by X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS), scanning electron microscopy (SEM), TEM, N2 adsorption-desorption, and UV-Vis. The results revealed that LCNO calcined at 700°C possessed a perovskite structure with porous, and phthalocyanine not only adsorbed on the surface but also loaded in the pores of the LCNO oxide. The photocatalytic activities of the samples were evaluated by the photocatalytic oxidation of dibenzothiophene (DBT) under simulated sunlight irradiation. It was found that either macrocyclic structure or center metal of phthalocyanine had great influences on the photocatalytic activity of ML/LCNO. The oxidative reactivity of the different macrocycles was found in the order of MPc/LCNO>MTAP/LCNO>MPTpz/LCNO; which of different center metals was CoL/LCNO>FeL/LCNO>MnL/LCNO>NiL/LCNO>CuL/LCNO. The catalysts were reused several times with a slight decrease in activity. Furthermore, this kinetics of photocatalytic oxidation of DBT indicated that the reaction was a pseudo-first-order reaction., (Copyright © 2015 Elsevier Inc. All rights reserved.)

Objective: To investigate the protective effect and action mechanism of petroleum ether extracts from Saussurea involucrate on brain tissues of hypoxia rats under constant pressure and closed conditions., Method: The PESI dosage-dependent experiment for hypoxia rats was conducted under constant pressure and closed conditions by intraperitoneally injecting 125, 250, 500 mg x kg(-1) to finalize that the optimum dosage is the high dose of PESI. Afterwards, 90 Wistar rats were randomly divided into the hypoxic model group, the acetazolamide 250 mg x kg(-1) group and the PESI high dose group. Each group was further divided into three subgroups according to different hypoxia times, with 10 rats in each subgroup. Under the same hypoxia and administration conditions, the rats were sacrificed after 0, 3, 6 h respectively. Their brain samples were collected for common pathological observation and immunohistochemical staining of HIF-1alpha. Real-time RT-PCR was used to detect HIF-1alpha, EPO, HO-1 and Caspase-3 gene expressions. And the Western blot assay was adopted to detect HIF-1alpha protein expression., Result: The brain tissues of the hypoxia model group were severely damaged with the increase in the hypoxia time. The acetazolamide group and the PESI high does group were damaged in a much lower degree. According to the gene expression and the Western blot assay, high dose of PESI could inhibit HIF-1alpha expression. According to the pure gene expression test, high dose of PESI could increase EPO and HO-1 mRNA expressions, but inhibit Caspase-3 mRNA expression., Conclusion: PESI's protective mechanism for brain tissues of hypoxia rats under constant pressure and closed conditions may be related to its effects in inhibiting HIF-1alpha expression, increasing EPO expression and resisting cell apoptosis.

A series of novel unsaturated five-membered benzo-heterocyclic amine derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that most of our synthesized compounds exhibited potent broad-spectrum antiviral activity. Notably, compounds 3f (IC50=3.21-5.06 μM) and 3g (IC50=0.71-34.87 μM) showed potent activity towards both RNA viruses (influenza A, HCV and Cox B3 virus) and a DNA virus (HBV) at low micromolar concentrations. An SAR study showed that electron-withdrawing substituents located on the aromatic or heteroaromatic ring favored antiviral activity towards RNA viruses.

Objective: To estimate the effect of ethanol extract from Saussurea involucrata (EES) on biochemical indicators of simulated high-altitude hypoxia induced mice and its mechanism., Methods: The oxidative stress indicator( MDA content, SOD activity) and metabolism parameters (LD content, LDH activity, ATP content, Na+ -K+ -ATPase and Ca2+ -Mg2+ -ATPase activity) in both brain and heart of the simulated high-altitude hypoxia induced mice were detected., Results: Compared with the model group, the ESS group could significantly increase the activity of SOD and LDH and decrease the content of MDA and LD in both brain and heart, the content of ATP and the activity of Na+ -K -ATPase and Ca2+ -Mg2+ -ATPase were also elevated., Conclusion: The results demonstrate that EES can increase the antioxidant ability, decrease the injury of free radical and ease the disfunction of energy metabolism caused by hypoxia.

A series of novel (5-oxazolyl)phenyl amine derivatives were synthesized and their antiviral activities against the hepatitis C virus (HCV) and the coxsackie virus B3 (CVB3) and B6 (CVB6) were evaluated in vitro. Bioassays showed that the synthesized compounds 17a1, 17a4, 17a6, 17b1, 17d1, 17e2 and 17g3 exhibited potent antiviral activity against HCV (IC₅₀ = 0.28-0.92 μM) and most synthesized compounds exhibited low cytotoxicity in Huh7.5 cells, compared to telaprevir. The compounds 17a1, 17a4, 17a5, 17a6, 17b1, 17b2, 17g1 and 17g3 showed strong activity against the CVB3 and/or CVB6 at low concentrations (IC₅₀ < 2.0 μM). The (5-oxazolyl)phenyl amines 17a1, 17a4, 17a8, 17b1, 17d1, 17e2, 17f3 and 17g3 were identified as the most active on the biological assays, and will be studied further., (Copyright © 2013 Elsevier Masson SAS. All rights reserved.)

Two novel spirooliganones A (1) and (2), a pair of spiro carbon epimers, with a rare dioxaspiro skeleton were isolated from the roots of Illicium oligandrum. The structures were fully determined by spectroscopic analysis and chemical methods, especially modified Mosher's method, and X-ray diffraction analysis. Spirooliganone B was found to exhibit more potent activities against coxsackie virus B3 and influenza virus A (H3N2) (IC50 3.70-5.05 μM) than spirooliganone A. The biosynthetic pathway involving a hetero-Diels-Alder reaction of the epimers was proposed.

A series of novel N-substituted sophocarpinic acid derivatives was designed, synthesized, and evaluated for their anti-enteroviral activities against coxsackievirus type B3 (CVB3) and coxsackievirus type B6 (CVB6) in Vero cells. Structure-activity relationship analysis revealed that the introduction of a benzenesulfonyl moiety on the 12-nitrogen atom in (E)-β,γ-sophocarpinic acid might significantly enhance anti-CVB3 activity. Among the derivatives, (E)-12-N-(m-cyanobenzenesulfonyl)-β,γ-sophocarpinic acid (11 m), possessing a meta-cyanobenzenesulfonyl group, exhibited potent activity against CVB3 with a selectivity index (SI) of 107. Furthermore, compound 11 m also showed a good oral pharmacokinetic profile, with an AUC value of 7.29 μM h⁻¹ in rats, and good safety through the oral route in mice, with an LD₅₀ value of >1000 mg kg⁻¹; these values suggest a druggable characteristic. Therefore, compound 11 m was selected for further investigation as a promising CVB3 inhibitor. We consider (E)-β,γ-N-(benzenesulfonyl)sophocarpinic acids to be a novel class of anti-CVB3 agents., (Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

The coordination features of an imidazole dicarboxylate ligand, 2-(3-methoxyphenyl)-1H-imidazole-4,5-dicarboxylic acid (m-H(3)MOPhIDC) has been explored. Consequently, seven coordination polymers, namely [Sr(m-HMOPhIDC)(H(2)O)](n) (1), [Sr(m-H(2)MOPhIDC)(2)](n) (2), [Cd(3)(m-H(2)MOPhIDC)(2)(m-HMOPhIDC)(2)(H(2)O)(2)](n) (3), [Cu(m-HMOPhIDC)(phen)](n) (phen = 1,10-phenanthroline) (4), [Cd(2)(m-HMOPhIDC)(2)(phen)(2)](n) (5) [Cd(2)(m-HMOPhIDC)(2)(2,2'-bipy)(2)](n) (2,2'-bipy = 2,2'-bipyridine) (6) and [Co(m-HMOPhIDC)(H(2)O)(2)](n) (7) have been hydro(solvo)thermally synthesized by fine control over synthetic conditions, and structurally characterized. X-ray single-crystal analyses reveal that these polymers indicate rich structural chemistry ranging from one-dimensional (4-7), two-dimensional (1 and 3) to three-dimensional (2) structures, and the m-H(3)MOPhIDC ligand in these polymers can be singly deprotonated or doubly deprotonated, and coordinates to metal ions by various modes. The thermal and fluorescence properties of the complexes 1-7 have been determined as well.

A series of novel N-phenylbenzamide derivatives were synthesized and their anti-EV 71 activities were assayed in vitro. Among the compounds tested, 3-amino-N-(4-bromophenyl)-4-methoxybenzamide (1e) was active against the EV 71 strains tested at low micromolar concentrations, with IC50 values ranging from 5.7 ± 0.8-12 ± 1.2 μM, and its cytotoxicity to Vero cells (TC50 = 620 ± 0.0 μM) was far lower than that of pirodavir (TC50 = 31 ± 2.2 μM). Based on these results, compound 1e is a promising lead compound for the development of anti-EV 71 drugs.

Currently, there is no approved antiviral drug for the infection caused by enteroviruses. A series of novel N-arylethyl isoquinoline derivatives defined with substituents on the ring A and C were designed, synthesized and evaluated in vitro for their activities against Coxsackievirus B3 (CVB3). The primary structure-activity relationship revealed that substituents on the ring A were not beneficial for the activity. Among these analogs synthesized, compound 7f bearing a methylenedioxy at the R(4) and R(5) positions afforded an anti-CVB3 activity and a reasonable selectivity index (SI=26.8); furthermore, 7f exhibited a moderate activity against enterovirus 71 (EV71) with SI value of 9.0. Thus it has been selected as an anti-enteroviral lead compound for further investigation., (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Fifteen novel six-membered azanucleoside derivatives were prepared and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in human hepatoblastoma-derived liver Hep-G2 cells. The most potent compound 16b with an IC(50) value of 2.74μg/mL (lower than 3TC) and a SI value of 13.5 was disclosed. The key synthetic steps involved the rearrangement of lactones (which were readily obtained from monosaccharides) and the Lewis acid-catalyzed condensation of nucleobases with azasugar donors. Using the versatile acetylated azasugar donors, azanucleosides covering three types of azasugars and four types of natural nucleobases were successfully obtained. The experimental results showed that some six-membered azanucleosides may find applications in the discovery of new anti-viral agents., (Copyright © 2010 Elsevier Ltd. All rights reserved.)

A series of novel glutarimide compounds were synthesized and their antiviral activities were evaluated. The compounds displaying the strongest antiviral activities included 5, 6f, 7e and 9 against coxsackievirus B3 (Cox B3), 10 and 6f against influenza virus A (influenza A) and 7a against herpes simplex virus 2 (HSV-2). However, most of the synthetic glutarimides showed comparatively much weaker activity against influenza A, Cox B3 and HSV-2 than the natural glutarimide compounds tested. Based on the results, it seemed likely that a conjugated system at the β-substituted moiety provides stronger antiviral activity.

Background: Previous studies have suggested that geldanamycin (GA) inhibits the replication of several viruses in vitro. Here, we aimed to synthesize and evaluate the antiviral activity of 17-amino-17-demethoxygeldanamycin derivatives., Methods: A series of 17-substituted and 17-,19-disubstituted GA derivatives were screened for antiviral activities against eight different viral strains, including herpesvirus, hepatitis virus, retrovirus and picornavirus., Results: Most of the tested compounds showed inhibitory activity against the viruses and showed reduced cytotoxicity in vitro as compared with the parent compound GA. In vivo efficacy evaluation results showed that compound 6 noticeably inhibited duckling hepatitis B virus DNA replication in duckling serum after oral administration. Viral rebound did not occur after termination of the treatment. The modified GA derivatives also showed median lethal dose values that were higher than that of the parent GA in mice intraperitoneally treated with the study compounds., Conclusions: Targeting heat-shock protein 90 could be a new antiviral approach that is not prone to the development of drug resistance. The 17-amino-17-demethoxygeldanamycin derivatives could be novel agents with potential antiviral activity.

Influenza virus is a virus causing upper respiratory tract infection disease with high morbidity and mortality. China is considered as an area with high rate of influenza morbidity. Prevention and treatment of influenza currently rely on vaccines and antiviral agents in the world. In addition, traditional Chinese medicines also have been used in clinical for influenza therapy. In vitro anti-influenza virus activities of 10 traditional Chinese medicines were studied by cytopathic effect (CPE). Qingre Jiedu oral liquid (factory H) had strong antiviral activity against influenza virus A/Guangdong Luohu/219/2006 (H1N1); Yinhuang oral liquid had strong antiviral activity against influenza virus A/Hanfang/359/95 and A/Yuefang/243/72 (H3N2). Qingkailing oral liquid (factory G) had strong antiviral activity against influenza virus A/Jifang/15/90 (H3N2). Qingre Jiedu oral liquid (factory H) had strong antiviral activity against influenza virus A/Jifang/15/90, A/Yuefang/243/72 (H3N2) and virus B.

Ribavirin is a broad-spectrum inhibitor against several unrelated DNA or RNA viruses in vitro and in vivo. In this paper the in vitro and in vivo study of anti-influenza virus activity of ribavirin (RBV) injection had been reported. The in vitro antiviral activity of ribavirin injection against influenza virus A and B was studied by CPE. The in vivo protective action of ribavirin injection against influenza A/FM/1/47(H1N1) mouse adapted strain infected mouse was studied with mouse model. The results showed ribavirin injection has strong inhibitory activity against 7 virus strains tested in vitro. Ribavirin injection could significantly increase virus infected mouse survival rate and survival days and improve lung pathogen and lung index.

Berberine (BBR) is a natural compound with up-regulating activity on both low-density-lipoprotein receptor (LDLR) and insulin receptor (InsR). This one-drug-multiple-target characteristic might be suitable for the treatment of metabolic syndrome. In searching for up-regulators effective for both LDLR and InsR expression, the structure-activity relationship (SAR) analysis for BBR analogues was done. Fourteen BBR analogues were designed, synthesized and biologically evaluated. SAR analysis revealed that appropriate modifications on the phenyl ring A or D of BBR might retain the up-regulatory activities on the expression of both LDLR and InsR. Among these compounds, compound 13a bearing 9-methoxy and 10-hydroxyl on the ring D showed promising activities on either LDLR or InsR gene expression. The 10-hydroxyl of 13a could be an arm to connect proper chemical groups for optimizing drug-bioavailability in vivo. Thus, 13a could be considered to be a parent compound to make pro-drugs for either blood lipids or glucose.

A new spectrophotometric determination method of hexavalent chromium in waste water and plating baths is described based on the oxidation of beryllon III by chromium(VI) in 0.02M sulphuric acid medium. The decrease in the absorbance of beryllon III was measured at 482 nm with an apparent molar absorptivity of 5.15 x 10(4)1.mole(-1).cm(-1). Beer's law was obeyed for chromium(VI) over the range 0-25 mug/25 ml. After the oxidation of Cr(III) to Cr(VI) by ammonium persulphate, total chromium can be determined. Therefore, chromium(III) can be calculated by subtracting chromium(VI) from total chromium. The detection limit is 0.015 and 0.020 mug/25 ml for chromium(VI) and total chromium, respectively. A sensitive spectrophotometric method for trace Cr(III) and Cr(VI) in waste water and plating baths was developed with good precision and accuracy. The reaction is also discussed.

In the presence of polyvinylalcohol (PVA-124) and polyethylene glycol monooctylphenyl ether (emulsifier OP), cadmium ions(II) can form a colour ion-association complex with both Bromopyrogallol Red (BPR) and Crystal Violet (CV). In the NH(3)NH(4)Cl medium, the ion-association complex has a composition of Cd:BPR:CV = 1:1:2, and its corresponding molecular formula is [CV](2)[Cd(BPR)]. The maximum absorption of the colour complex is located at 654 nm with an apparent molar absorptivity of 1.79 x 10(5) l.mole(-1).cm(-1). Beer's law is obeyed for cadmium over the range 0-10 mug/25 ml. A highly sensitive spectrophotometric method for trace cadmium in water and zinc was developed with good precision and accuracy. The mechanism of the reaction is also discussed.