Constituents of Limonia acidissima inhibit LPS-induced nitric oxide production in BV-2 microglia

The ethyl acetate (EtOAc) soluble fraction of the 85% ethanol (EtOH) extract of the dried bark of Limonia acidissima potently inhibited nitric oxide (NO) production in lipopolysaccharide (LPS) activated BV-2 cells, a microglial cell line. Bioassay-guided column chromatography separation afforded a new stereoisomer of neolignan, (7’E)-(7R,8S)-4-hydroxy-3,5’-dimethoxy-4’,7-epoxy-8,3’-neolig-7’-en-9,9’-diyil diacetate (1), together with two known lignans, (+)-yangambin (2) and (+)-syringaresinol (3), three known triterpenoids, hederatriol (4), basic acid methyl ester (5), and 3β-hydroxyolean-12-en-11-one (6), and four known fatty acid derivatives, cascarillic acid (7), (+)-α-dimorphecolic acid (8), 8(R)-hydroxylinoleic acid (9), and (6Z,9Z,12Z)-pentadecatrienoic acid (10). The structure of the new compound 1 was elucidated by detailed analysis of spectroscopic data and circular dichroism (CD) spectroscopy. Compounds 1, 3-6, and 8-10 isolated from L. acidissima significantly reduced NO production in LPS-stimulated BV-2 microglia cells.     

Inhibition of Real-Time PCR in DNA Extracts from Aquifer Sediment

Variation in inhibition of real-time PCR was investigated with DNA extracts from 50 aquifer sediment core samples of 5 cm length collected through a 2.5 meter vertical profile across a landfill leachate plume. The inhibition was quantified using an internal control of the green fluorescent protein ( gfp ) gene, which was spiked into the real-time PCR reactions. The inhibition was investigated at two gfp gene concentrations: at 1.7 · 10 ⁷ gfp gene copies/g sediment (5.1 · 10 ⁴ gfp gene copies/PCR reaction) and at 1.7 · 10 ⁵ gfp gene copies/g sediment (5.1 · 10 ² gfp gene copies/PCR reaction). Despite the low TOC content of the sediment (average 0.4 mg C/g dw) the average real-time PCR response was partially inhibited, compared to a reference (pure water), at both high and low gfp concentrations. The relative amplification (reference = 1) was 0.85 ± 0.20 (high) and 0.66 ± 0.23 (low), showing significantly (P < 0.05) stronger inhibition at the lower target gene concentration. The inhibition of the real-time PCR did not show a systematic variation in the vertical profile related to plume position but variations were significant on a small scale of 5–15 cm depth intervals. One of the 50 samples failed to produce a signal with either concentration of the gfp internal control and three other samples inhibited real-time PCR at both high and low gfp concentration. These 4 samples, which were the samples with the highest inhibition, were the only DNA extracts with a visible brown colouration, indicating contents of humic-like substances. Elevated absorbance at 400 nm of these samples also indicated that humic-like substances were responsible for inhibition. However, other factors not associated with either absorbance or TOC may have contributed to the inhibition in less inhibited samples since the variation in real-time PCR response could not be sufficiently explained by absorbance or TOC. The results of this study suggest that an internal control is needed in real-time PCR reactions with DNA from environmental samples due to variation in inhibition to correctly quantify the number of target genes, especially at low target gene concentrations, when dilution of DNA extracts is not practical.     

Art in the Making

Abstract

There's Pigs and Pigs: Erik Blegvad, The Three Little Pigs, Atheneum: New York, 1980, 32 pages, $8.95.

There's Pigs and Pigs: Joseph Jacobs, The Story of the Three Little Pigs (illust. by Lorinda B. Cauley), Putnam: New York, 1980, unpaged, $8.95.

There's Pigs and Pigs: Margaret Wise Brown (illust. by Ann Strugnell), Once Upon a Time in a Pigpen, Addison-Wesley: Reading, Mass., 1980, 64 pages, $10.95.

There's Pigs and Pigs: Miska Miles (illust. by Leslie Morrill), This Little Pig, Dutton: New York, 1980, unpaged, $6.95.

Picture Books: William Steig, Gorky Rising, Farrar, Strauss &; Giroux: New York, 1980, unpaged, $10.95.

Picture Books: Charles Keeping, Willie's Fire-Engine, Oxford University: New York, 1980, unpaged, $10.95 (boards).

Picture Books: Lydia Pender (illust. by Judith Cowell), The Useless Donkeys, Warne: New York, 1979, unpaged, $9.95.

Picture Books: Lillie D. Chaffin (illust. by Lloyd Bloom), We Be Warm Till Springtime Comes, Macmillan: New York, 1980, unpaged, $9.95.

Picture Books: Kate Canning, A Painted Tale, Barrons: Woodbury, N.Y.: 1979, unpaged, $6.95 (boards).

Historical Explorations: Maurice Boutet de Monvel, Joan of Arc, Viking: New York, 1980, 55 pages, $12.95.

Historical Explorations: Mitsumasa, Anno, Anno's Medieval World, Philomel Books: New York, 1980, 48 pages, $9.99.

Historical Explorations: Peter Spier, People, Doubleday: New York, 1980, unpaged, $10.00.

Historical Explorations: John S. Goodall, An Edwardian Season, Atheneum: New York, 1980, unpaged, $7.95.

Historical Explorations: Miriam Schlein (illust. by Erik Hilgert), I, Tut, Four Winds Press: New York, 1979, unpaged, $7.95.     

Preparation of Optically Pure cis-2,4-Dimethyl-l-cyclohexanones,the Key Intermediates in Cycloheximide Synthesis,Using Microbial Resolution

Asymmetric hydrolysis of acetate (10) of (±)-t-2,t-4-dimethyl-r-l-cyclohexanol with Bacillus subtilis var. niger gave (?)-(lS,2S,4S)-2,4-dimethyl-l-cyclohexanol (6a) and (+)-(1R,2R,4R)-acetate (10b) with high optical purities. Optically pure (?) and (+)-alcohols (6a and 6b) were prepared via corresponding 3,5-dinitrobenzoates. Oxidation of alcohols (6a and 6b) with chromic acid gave optically pure (?)-(2S,4S) and (+)-(2R,4R)-2,4-dimethyl-l-cyclohexanones (2a and 2b), respectively.     

Inhibitory alkaloids from Dictamnus dasycarpus root barks on lipopolysaccharide-induced nitric oxide production in BV2 cells

The methanolic extract of Dictamnus dasycarpus root barks afforded one new glycosidic quinoline alkaloid, 3-[1β-hydroxy-2-(β-D-glucopyranosyloxy)-ethyl)-4-methoxy-2(1H)-quinolinone (1), together with nine known compounds, preskimmianine (2), 8-methoxy-N-methylflindersine (3), dictamine (4), γ-fagarine (5), halopine (6), skimmianine (7), dictangustine-A (8), iso-γ-fagarine (9), isomaculosidine (10). The isolated alkaloids significantly inhibited nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated BV2 cells. Among them, compounds 3 and 7 showed the most potent inhibitory activities on LPS-induced NO production.     

Phylogenetic relationships of species in <Emphasis Type="Italic">Pseudoroegneria</Emphasis> (Poaceae: Triticeae) and related genera inferred from nuclear rDNA ITS (internal transcribed spacer) sequences

To evaluate the phylogenetic relationships of species in Pseudoroegneria and related genera, the nuclear ribosomal internal transcribed spacer (ITS) sequences were analyzed for eighteen Pseudoroegneria (St), two Elytrigia (E ^e St), two Douglasdeweya (StP), three Lophopyrum (E ^e and E ^b ), three Agropyron (P), two Hordeum (H), two Australopyrum (W) and two Psathyrostachys (Ns) accessions. The main results were: (i) Pseudoroegneria gracillima, P. stipifolia, P. cognata and P. strigosa (2x) were in one clade, while P. libanotica, P. tauri and P. spicata (2x) were in the other clade, indicating there are the differentiations of St genome among diploid Pseudoroegneria species; (ii) P. geniculata ssp. scythica, P. geniculata ssp. pruinifera, Elytriga caespitosa and Et. caespitosa ssp. nodosa formed the E ^e St clade with 6-bp indel in ITS1 regions; and (iii) Douglasdeweya wangii, D. deweyi, Agropyron cristatum and A. puberulum comprised the P clade. It is unreasonable to treat P. geniculata ssp. scythica and P. geniculata ssp. pruinifera as the subspecies of P. geniculata, and they should be transferred to a new genus Trichopyrum, which consists of species with E ^e St genomes. It is also suggested that one of the diploid donor of D. wangii and D. deweyi is derived from Agropyron species, and it is reasonable to treat tetraploid species with StP genomes into Douglasdeweya.     

Design,synthesis and in vivo/in vitro screening of novel chlorokojic acid derivatives

A series of novel Mannich bases of chlorokojic acid (2-chloromethyl-5-hydroxy-4H-pyran-4-one) were synthesized and their biological activities were investigated. Anticonvulsant activity results according to phase-I tests of Antiepileptic Drug Development (ADD) Program revealed that compound 13 was the most effective one at 4?h against subcutaneous pentylenetetrazole (scPTZ)-induced seizure test. Antimicrobial activities were evaluated in vitro against bacteria and fungi by using broth microdilution method. The antitubercular activities against Mycobacterium tuberculosis and M. avium were discussed with Resazurin microplate assay (REMA). The antimicrobial activity results indicated that compounds 1 and 12 (MIC: 8–16 µg/mL) showed higher activity against Gram negative bacteria while compound 12 had MIC: 4–16 µg/mL against Gram positive bacteria. Compound 1 was the most active one with MIC values of 8–32 µg/mL against fungi. Mannich bases also exhibit significant antitubercular activity in a MIC range of 4 to 32 µg/mL, especially compound 18 against M. avium.     

Biomineralization of Fungal Hyphae with Calcite (CaCO3) and Calcium Oxalate Mono- and Dihydrate in Carboniferous Limestone Microcosms

The formation of biogenic fabrics in limestone by two fungi, Serpula himantioides and a polymorphic fungal isolate from limestone identified as a Cephalotrichum (syn. Doratomyces) sp., was investigated. The fungal cultures were grown in laboratory microcosms consisting of Carboniferous limestone and after 21 d incubation at 25°C, biomineralization of fungal filaments was observed. Environmental electron scanning microscopy (ESEM) and X-ray micro-analysis (EDXA) of crystalline precipitates on the hyphae of S. himantioides demonstrated that the secondary crystals exhibited different crystalline forms but were similar in elemental composition to the original limestone. Powder X-ray diffraction (XRD) of crystalline precipitates showed they were composed of a mixture of calcite (CaCO ₃ ) and calcium oxalate monohydrate (CaC ₂ O ₄ · H ₂ O). Analysis of crystals precipitated on the hyphae of the limestone isolate, using ESEM and EDXA, showed that the crystals exhibited similar morphological characteristics and elemental composition to the original limestone. XRD showed that they were composed solely of calcite (CaCO ₃ ) or of calcite with some calcium oxalate dihydrate (CaC ₂ O ₄ · 2H ₂ O). These results provide direct experimental evidence for the precipitation of calcite (CaCO ₃ ) and also secondary mycogenic minerals, on fungal hyphae in low nutrient calcareous environments, and suggest that fungi may play a wider role in the biogeochemical carbon cycle than has previously been appreciated.     

Chemical constituents of Hericium erinaceum associated with the inhibitory activity against cellular senescence in human umbilical vascular endothelial cells

Abstract

Hericium erinaceum is an edible and medicinal mushroom widely used in Korea, Japan, and China. On the search for biologically active compounds supporting the medicinal usage, the MeOH extract of the fruiting bodies of H. erinaceum was investigated for its chemical constituents. Six compounds were isolated and identified as hericenone D (1), (22E,24R)-5α,8α-epidioxyergosta-6,22-dien-3β-ol (2), erinacerin B (3), hericenone E (4), hericenone F (5) and isohericerin (6) by comparing their spectroscopic data with previously reported values. The inhibitory effects on adriamycin-induced cellular senescence in human dermal fibroblasts (HDFs) and human umbilical vein endothelial cells (HUVECs) of the isolates (1–6) were studied. Among the isolated compounds, ergosterol peroxide (2) reduced senescence associated β-galactosidase (SA-β-gal) activity increased in HUVECs treated with adriamycin. According to experimental data obtained, the active compound may inspire the development of a new pharmacologically useful substance to be used in the treatment and prevention of age-related diseases.     

Conjugated Serotonins and Phenolic Constituents in Safflower Seed (Carthamus tinctorius L.)

New three conjugated serotonins were isolated from safflower meal (carthamus tinctorius L.). On the basis of spectral properties and chemical evidence, their structures were determined as N-feruloylserotonin (4), N-(p-coumaroyl)serotonin (5) and N-(p-coumaroyl)serotonin mono-β-d-glucopyranoside (6), The known compounds, 2-hydroxyarctiin (2), matairesinol mono-β-d-glucoside (1) and acacetin (3) were also isolated and identified.     

Anti-inflammatory phenolics isolated from Juniperus rigida leaves and twigs in lipopolysaccharide-stimulated RAW264.7 macrophage cells

Inflammation is an essential host defense system particularly in response to infection and injury; however, excessive or undesirable inflammatory responses contribute to acute and chronic human diseases. A high-throughput screening effort searching for anti-inflammatory compounds from medicinal plants deduced that the methanolic extract of Juniperus rigida S. et L. (Cupressaceae) inhibited significantly nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells. Activity-guided fractionation and isolation yielded 13 phenolic compounds, including one new phenylpropanoid glycosides, 3,4-dimethoxycinnamyl 9-O-β-D-glucopyranoside (1). Among the isolated compounds, phenylpropanoid glycosides with p-hydroxy group (2, 4) and massoniaside A (7), (+)-catechin (10), amentoflavone (11) effectively inhibited LPS-induced NO production in RAW264.7 cells.     

Synthesis,in vitro and in vivo antitumor and antiviral activity of novel 1-substituted benzimidazole derivatives

Abstract

A novel series of 5-nitro-1H-benzimidazole derivatives substituted at position 1 by heterocyclic rings was synthesized. Cytotoxicity and antiviral activity of the new compounds were tested. Compound 3 was more active than doxorubicin against A-549, HCT-116 and MCF-7. However, compound 3 showed no activity against human liver carcinoma Hep G-2 cell line. Compounds 9 and 17b (E) showed potency near to doxorubicin against the four cell lines. The acute toxicity of compound 9 on liver cancer induced in rats was determined in vivo. Interestingly, it showed restoration activity of liver function and pathology towards normal as compared to the cancer-bearing rats induced by DENA. Compounds 17a (Z), 17b (E) and 18a (Z) were the most promising compounds for their antiviral activity against rotavirus Wa strain.     

土壤理化性质驱动烤烟根际细菌群落的组配及其共现性网络互作

【目的】解析土壤微生物在植物根际的组配机制对于认识和维护农田生态系统的稳定性至关重要。【方法】通过Illumina高通量测序和生物信息学分析方法明确了我国主要种植烟草生态区烤烟根际土壤细菌群落与土壤理化性质的互作关系。【结果】烤烟根际细菌类群主要为放线菌纲(Actinobacteria)、α-变形菌纲(Alphaproteobacteria)、γ-变形菌纲(Gammaproteobacteria)和嗜热油菌纲(Thermoleophilia)。细菌群落组成按生态区聚类,且样本空间距离和细菌群落相似度显著负相关。共现性网络分析表明,烤烟根际细菌群落间协同作用大于拮抗作用,武陵秦巴生态区、黄淮平原生态区、南岭丘陵生态区和沂蒙丘陵生态区细菌群落高度模块化,小单胞菌属(Micromonospora)为南岭丘陵生态区和黄淮生态区细菌共现性网络的网络中心,Bryobacter和气单胞菌属(Arenimonas)为南岭丘陵生态区细菌网络的模块核心,其菌群特性而非相对丰度决定了其在稳定细菌网络中的重要作用。冗余分析结果证实pH、有效铁、交换性镁和有效锰能显著影响烤烟根际细菌群落结构。【结论】烤烟根际细...     

Ruthenium(III) dimethyl sulfoxide pyridinehydroxamic acid complexes as potential antimetastatic agents: synthesis,characterisation and in vitro pharmacological evaluation

Reaction of 3-pyridinehydroxamic acid and 4-pyridinehydroxamic acid (3-pyha and 4-pyha) with either [NBu₄][RuCl₄(dmso-S)₂] or [(dmso)₂H][RuCl₄(dmso-S)₂] (dmso is dimethyl sulfoxide) in acetone afforded three new ruthenium(III) dimethyl sulfoxide pyridinehydroxamic acid complexes: [NBu₄][trans-RuCl₄(dmso-S)(4-pyha)]·CH₃COCH₃ (1), [3-pyhaH][trans-RuCl₄(dmso-S)(3-pyha)] (2) and [4-pyhaH][trans-RuCl₄(dmso-S)(4-pyha)] (3). The solid-state structure of [NBu₄][trans-RuCl₄(dmso-S)(4-pyha)]·CH₃COCH₃ (1) was determined by X-ray crystallography. 2 and 3 were pharmacologically evaluated for their in vitro cytotoxicity, their ability to inhibit cell invasion and their gelatinase activity. 2 and 3 were devoid of cytotoxicity against the cell lines tested. 2 inhibited invasion of the highly invasive MDA-MB-231 cells to a much greater extent than 3. Contrary to expectations, neither 2 nor 3 had any inhibitory effect on matrix metalloproteinase (MMP) production and/or activity and in fact 3 was found to enhance the production and/or activity of both MMP-2 and MMP-9.     

专项整治对综合医院抗菌药物使用强度的影响

??????? 目的 探讨抗菌药物临床应用专项整治活动对综合医院住院患者抗菌药物使用强度的影响。方法 以限定日剂量（DDD）为单位,对某综合性医院在实施专项整治前、后住院患者抗菌药物使用强度（AUD）进行统计、分析。结果 专项整治活动降低了住院患者累计AUD值,大环内酯类等药物AUD明显下降,第二代、第三代和第四代头孢菌素和不同管理级别抗菌药物AUD均下降。但还存在用药集中、注射用头孢哌酮钠舒巴坦钠AUD下降不明显等问题。结论 专项整治有效降低了综合医院住院患者AUD,但与卫生行政部门标准仍存在差距,应进一步加强管理。     

哈尼梯田稻鲤共作与单养模式下福瑞鲤肠道菌群结构比较研究

【目的】分析不同养殖模式的福瑞鲤肠道菌群结构组成和群落特征。【方法】通过16S rRNA高通量测序技术,分析比较哈尼梯田稻鲤共作、传统池单养、水泥池单养模式下的福瑞鲤肠道菌群的结构组成和丰度差异。【结果】梯田稻鲤组(RCIC)、传统池鲤组(YPIC)和水泥池鲤组(HPIC)分别获得了2345、238和118个OTU。RCIC组的Sobs指数及PD指数最高,显著高于YPIC组(P<0.05),极其显著高于HPIC组(P<0.01);池塘单养模式下,两组之间多样性指数也存在显著差异,YPIC组大于HPIC组(P<0.05)。含量大于10%优势菌门：RCIC组主要为变形菌门(39.39%)、梭杆菌门(38.55%)和厚壁菌门(15.4%);YPIC组为变形菌门(21.87%)、梭杆菌门(58.27%);HPIC组为变形菌门(46.63%)、梭杆菌门(53.14%)。变形菌和梭杆菌为3组福瑞鲤肠道样品的优势菌群,其中的鲸杆菌属(Cetobacterium)、气单胞菌属(Aeromonas)为核心优势菌属。LEfSe线性判别分析(LDA>3)显示17个具有差异的标记菌属,...     

Association between gestational diabetes and biomarkers: a role in diagnosis

Background: We investigated the association between markers of insulin resistance, chronic inflammation, and adipokines and GDM.

Methods: In our case-cohort study in Johannesburg we included women with GDM and controls. We tested the ability of biomarkers to identify women at high risk of GDM.

Results: Of the 262 pregnant women, 83 (31.7%) had GDM. Women with GDM were heavier (p?=?0.04) and had more clinical risk factors (p?=?0.008). We found a significant difference in fasting insulin (p?p?=?0.046), HOMA (p?p?Conclusions: Insulin sensitivity markers are promising tools to identify women at high risk of GDM.     

Hypoglycemic activity of curcumin synthetic analogues in alloxan-induced diabetic rats

The currently available therapies for type 2 diabetes have been unable to achieve normoglycemic status in the majority of patients. The reason may be attributed to the limitations of the drug itself or its side effects. In an effort to develop potent and safe oral antidiabetic agents, we evaluated the in vitro and in vivo hypoglycemic effects of 10 synthetic polyphenolic curcumin analogues on alloxan-induced male diabetic albino rats. In vitro studies showed 7-bis(3,4-dimethoxyphenyl)hepta-1,6-diene-3,5-dione (4) to be the most potential hypoglycemic agent followed by 1,5-bis(4-hydroxy-3-methoxyphenyl)penta-1,4-dien-3-one (10). Structure activity relationship (SAR) of the tested compounds was elucidated and the results were interpreted in terms of in vitro hypoglycemic activities. Furthermore, oral glucose tolerance test (OGTT) with compounds 4, 10 and reference hypoglycemic drug glipizide showed that compound 4 and glipizide had relatively similar effects on the reduction of blood glucose levels within 2?h. Thus, compound 4 might be regarded as a potential hypoglycemic agent being able to reduce glucose concentration both in vitro and in vivo.     

Regioselective biooxidation of (+)-valencene by recombinant E. coli expressing CYP109B1 from Bacillus subtilis in a two-liquid-phase system

Background  

(+)-Nootkatone (4) is a high added-value compound found in grapefruit juice. Allylic oxidation of the sesquiterpene (+)-valencene (1) provides an attractive route to this sought-after flavoring. So far, chemical methods to produce (+)-nootkatone (4) from (+)-valencene (1) involve unsafe toxic compounds, whereas several biotechnological approaches applied yield large amounts of undesirable byproducts. In the present work 125 cytochrome P450 enzymes from bacteria were tested for regioselective oxidation of (+)-valencene (1) at allylic C2-position to produce (+)-nootkatone (4) via cis- (2) or trans-nootkatol (3). The P450 activity was supported by the co-expression of putidaredoxin reductase (PdR) and putidaredoxin (Pdx) from Pseudomonas putida in Escherichia coli.