Anti-inflammatory, cyclooxygenase inhibitory and antioxidant activities of standardized extracts of Tridax procumbens L.

The standardized EtOAc, MeOH and 70% EtOH extracts of Tridax procumbens aerial parts showed significant inhibition of rat paw edema at a medium dose of 200 mg/kg and the EtOAC extract was the most active. These extracts were standardized by HPLC with the help of chemical markers. Further, the extracts were evaluated for COX-1 and COX-2 inhibitory activity and EtOAc extract exhibited the highest inhibition of COX-1 and COX-2 at 50 μg/mL. Cent aurein, centaureidin and bergenin were isolated as COX-1 and COX-2 inhibitory principles from the EtOAc extract. The extracts also exhibited antioxidant activity against DPPH and ABTS free radicals. The anti-inflammatory activity of T. procumbens aerial parts could be at least in part due to COX-1, COX-2 enzyme inhibition and free radical-scavenging activities which may be attributed to the presence of flavonoids and other polyphenols in the extracts.     

Anti-inflammatory,cyclooxygenase (COX)-2, COX-1 inhibitory and antioxidant effects of Dysophylla stellata Benth.

The n-hexane and ethyl acetate extracts of whole plants of Dysophylla stellata significantly inhibited edema when applied topically at doses of 0.5 and 1 mg/ear in TPA-induced ear edema assay in mice. Further, both the extracts were evaluated for COX-1 and COX-2 inhibitory activities and showed 85.42 and 57.38%; and 71.79 and 89.27% inhibition at 50 µg/ml, respectively. Chromones (1 and 2) present in these extracts could be responsible for their COX-1 and COX-2 inhibitory and anti-inflammatory activities. The ethyl acetate extract showed antioxidant activity in DPPH and ABTS radical scavenging assay where as n-hexane extract found to be inactive.     

Semisynthesis and pharmacological investigation of lipo-alkaloids prepared from aconitine

Processed aconite drugs are widely used in Eastern medicine as painkillers and antirheumatic agents. It is known that the traditional processing of aconite drugs increases the amount of lipo-alkaloids. In order to obtain information about the pharmacological potential of these compounds, semisynthesis of 9 aconitine-derived lipo-alkaloids was carried out and their COX-1, COX-2 and LTB₄ formation inhibitory activities were investigated. It was found that compounds esterified with unsaturated fatty acids demonstrated significant COX-2 inhibitory effects, while in the COX-1 assay only 14-benzoylaconine-8-O-eicosapentaenoate exerted remarkable activity. The inhibition of LTB₄ formation was pronounced in cases of long chain fatty acid derivatives.     

Chemical constituents of Stereospermum acuminatissimum and their urease and α-chymotrypsin inhibitions

Phytochemical investigation of the stem bark of Stereospermum acuminatissimum K. Schum. resulted in the isolation of 21 compounds, including two new guanine derivatives, 1,3,7-trimethylguanin-1/3-ium (1) and 3,7-dimethylguanin-1/3-ium (2), and one new phenolic long chain ester, 2-(4-hydroxyphenyl)ethyl hentriacontanoate (3). The known compounds were identified as sterequinones A, F, and H (4, 5, and 6), zenkequinones A-B (7-8), p-coumaric acid (9), methyl caffeate (10), caffeic acid (11), psilalic acid (12), syringaldehyde (13), norviburtinal (14), specioside (15), verminoside (16), tyrosol (17), eutigoside A (18), ellagic acid (19), atranorin (20), and ursolic acid (21). The metabolites were screened for their potential against urease and α-chymotrypsin enzymes, as urease is targeted in peptic ulcer while α-chymotrypsin is used to remove protein debris in ulcer. Compound 20 was found to be excellent urease inhibitor with IC₅₀ value of 18.2 ± 0.03 μM. Compounds 13 and 18-20 are reported for the first time from the genus Stereospermum. The chemotaxonomic significance of the isolated compounds was also described.     

Isolation and structural characterization of glycosides from an anti-angiogenic extract of Monnina obtusifolia H.B.K.

Angiogenesis, the growth of new blood vessels from the pre-existing vasculature is of physiological and pathological importance. Substantial data over the last decade has implicated uncontrolled angiogenesis with various pathological states. Vascular endothelial growth factors (VEGFs) play a critical role in its regulation, and have become one of the most interesting anti-angiogenesis targets. We have investigated the anti-angiogenic potential of plant extracts in a preliminary ELISA screening. The n-BuOH extract obtained from the leaves of Monnina obtusifolia (Polygalaceae) demonstrated an inhibition of VEGF-A or Placental Growth Factor interaction with Flt-1 (VEGF receptor 1), with an inhibition over 50% in particular for VEGF-A/Flt-1 interaction at a concentration of 500 μg/mL. Successively fractionation of the bioactive n-BuOH extracts of M. obtusifolia aerial parts led to the isolation of six new compounds, 1-O-(4-hydroxy-2-methylene-butanoic acid)-6-O-β-d-(4-hydroxy-2-methylene-butanoyl)-glucopyranose (1), 1-O-(isopentenyl)-6-O-β-d-(4-hydroxy-2-methylene-butanoyl)-glucopyranose (2), 1-O-(4-hydroxy-2-methylene-butanoic acid)-6-O-β-d-(isovaleroyl)-glucopyranose (3), 1-O-(3-methylbut-3enyl)-6-O-β-d-(isovaleroyl)-glucopyranose (4), two new sucrose esters, 3,4-O-β-d-di-feruloyl-fructofuranosyl-6-O-α-d-(p-coumaroyl)-glucopyranoside (5), and 3,4-O-β-d-di-feruloyl-fructofuranosyl-6-O-α-d-(caffeoyl)-glucopyranoside (6), together with known flavonoids. Their structures were established on the basis of detailed spectral analysis. Since none of the isolated compounds showed a relevant inhibition of VEGFs, the biological activity observed for the butanolic extract might be due to the presence of a combination of compounds acting synergistically.     

Anti-inflammatory and analgesic properties of cis-mulberroside A from Ramulus mori

This study examined the analgesic and anti-inflammatory actions of cis-mulberroside A isolated from Ramulus mori in several models of inflammatory pain in mice. Cis-mulberroside A (25 and 50 mg/kg) given by p.o. route 30 min before challenge produced a dose-dependent inhibition of the acetic acid-induced pain and Evans blue leakage in mice. In addition, this compound exhibited significant systemic anti-inflammatory activity in carrageenan-induced mouse paw edema in a concentration-related manner (33.1–68.5% inhibition), and similar results were achieved in formalin test. Suppressive effects of cis-mulberroside A on the production of NO and expression of inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-stimulated macrophages were also assessed. Collectively, cis-mulberroside A showed high analgesic and anti-inflammatory activities. The above results will be the supporting evidence for the potential anti-rheumatoid activity of R.mori in Chinese traditional medicine.     

Two new glycosidated coumaramides from Clerodendron cyrtophyllum

Two new glycosidated coumaramides clerodendiod A (1) and B (2), together with seven known glycosidic compounds were isolated from the branches of Clerodendron cyrtophyllum Turcz. Clerodendiod A and B were elucidated as β-D-glucopyranosyl-(1 → 3)-β-D-glucopyranosyl-(1 → 3)-[6-O-(E)-p-methoxycinnamoyl]-β-D-glucopyranosyl-(1 → 2)-[4-O-((E)-2-(4-acetamidobutylcarbamoyl)vinyl)-phenyl]-α-L-rhamnopyranoside (1) and 6-O-(E)-p-coumaroyl-β-D-glucopyranosyl-(1 → 3)-β-D-glucopyranosyl-(1 → 3)-[6-O-(E)-p-methoxycinnamoyl]-β-D-glucopyranosyl-(1 → 2)-[4-O-((E)-2-(4-acetamidobutylcarbamoyl)vinyl)-phenyl]-α-L-rhamnopyranoside (2) on the basis of chemical and spectral evidence. The isolated new compound 2 was assayed for the inhibition of the NF-κB pathway and showed potent activity in inhibiting NF-κB which its IC₅₀ values was found to be 24.9 nM.     

A novel antifungal anthraquinone from seeds of Aegle marmelos Correa (family Rutaceae)

A new anthraquinone, 1-methyl-2-(3′-methyl-but-2′-enyloxy)-anthraquinone (1) has been isolated from seeds of Aegle marmelos Correa and was characterized on the basis of spectral analysis (UV, IR, ¹H NMR, ¹³C NMR, 2D NMR and mass spectroscopy). The compound exhibited significant antifungal activity against pathogenic strains of Aspergillus species and Candida albicans in disc diffusion assay (MIC value of 6.25 μg/disc), microbroth dilution and percent spore germination inhibition assays (MIC value of 31.25–62.5 μg/ml).     

Cytochrome P450 1 enzyme inhibition and anticancer potential of chromene amides from Amyris plumieri

Cytochrome P450 (CYP) enzyme inhibitory properties of six chromenylated amide compounds (CAs) from Amyris plumieri are described. Inhibition of CYP microsomes (CYP1A1, CYP1A2, CYP1B1, CYP2D6, CYP3A4 and CYP2C19) was monitored using a fluorescent assay. Potent inhibition was found against CYP1A1 with IC₅₀ and K_i for CA1 (acetamide), being the lowest at 1.547 ± 1.0 μM and 0.37 μM respectively, displaying non-competitive kinetics. The selectivity for CYP1A1 was increased in CA3 (butanamide), which also exhibited cytotoxicity against breast cancer cells, MCF7 with an IC₅₀ of 47.46 ± 1.62 μM. Structure-activity relationship studies provide insight at a molecular level for CAs with implications in chemoprevention and chemotherapy.     

毛竹PeAP2基因及其启动子的克隆与表达初步分析

APETALA2(AP2)基因在植物生长发育过程中发挥着重要作用.利用RT-PCR和RACE方法,从毛竹中克隆到1个AP2同源基因的全长cDNA序列,命名为PeAP2.序列分析表明:PeAP2基因全长1 750 bp,其中,5′端非编码区106bp,3′端非编码区174 bp,开放阅读框1 470 bp,编码1个489 aa的蛋白,该蛋白含有2个AP2结构域,属于AP2/EREBP家族的AP2亚家族.PeAP2蛋白与来自其它单子叶植物的AP2蛋白均有着较高同源性,其中,与二穗短柄草的AP2蛋白同源性最高,达74.85％.实时定量PCR分析显示:PeAP2基因在毛竹的根、茎、叶、鞘和节5种器官中均有表达,其中,叶片中的表达丰度最高,鞘中次之,而在根、茎、节中的表达丰度接近,均较低.利用hiTAIL-PCR方法克隆获得了PeAP2上游启动子区序列1 359 bp,分析显示其含有光、激素等多种信号应答相关的作用元件.     

Diversity of northern plantations peaks at intermediate management intensity

Tree diversity is an important component of biodiversity. Management intensification is hypothesized to affect tree diversity. However, evidence to support the relationship between management intensity and tree diversity in northern forests is lacking. This study examined the effects of fertilization, site preparation, and brush control on tree species diversity, shade tolerance diversity and size diversity of jack pine (Pinus banksiana Lamb.), black spruce (Picea mariana [Mill.] B.S.P.), white pine (Pinus strobus L.) and white spruce (Picea glauca [Moench] Voss) plantations, 15 years after planting in Ontario, Canada. Species diversity and shade tolerance diversity were highly correlated, so were diameter size diversity and height size diversity. Fertilization did not affect the tree diversity indices of any plantations. Species diversity and shade tolerance diversity was interactively influenced by site preparation and brush control in the black spruce, white pine, and white spruce plantations, showing that the highest diversity occurred on sites with intensive site preparation without brush control, whereas on sites with brush control, diversity was higher with least intensity of site preparation. However, in the jack pine plantation, neither species diversity nor shade tolerance diversity differed with management intensification, and is attributed to the fast capture of site resources by the planted crop trees of jack pine which minimized establishment of non-crop species. Tree size diversity increased with site preparation intensity in the jack pine and black spruce plantations, while it decreased with brush control in the white pine and white spruce plantations. We concluded that (1) the effects of management intensification on diversity of northern plantations differ with growth habit of planted crop tree species and (2) species diversity and tree size diversity tend to be highest at intermediate levels of silvicultural intensification during the stand establishment phase, supporting the intermediate disturbance hypothesis.     

Ocotea quixos Lam. essential oil: In vitro and in vivo investigation on its anti-inflammatory properties

Here we investigated the anti-inflammatory properties of Ocotea quixos essential oil and of its main components, trans-cinnamaldehyde and methyl cinnamate, in in vitro and in vivo models. Ocotea essential oil and trans-cinnamaldehyde but not methyl cinnamate significantly reduced LPS-induced NO release from J774 macrophages at non-toxic concentrations, inhibited LPS-induced COX-2 expression and increased forskolin-induced cAMP production. The essential oil (30–100 mg/kg os) and trans-cinnamaldehyde (10 mg/kg os) in carrageenan-induced rat paw edema showed anti-inflammatory effect without damaging gastric mucosa. In conclusion we provide the first evidence of a significant anti-inflammatory gastro-sparing activity of O.quixos essential oil.     

Predicting the severity of Swiss needle cast on Douglas-fir under current and future climate in New Zealand

Phaeocryptopus gaeumannii, the causal agent of Swiss needle cast, is widely distributed in plantations of Douglas-fir (Pseudotsuga menziesii) throughout New Zealand, causing premature abscission of needles and significant growth losses. Data were collected from 34 sites, selected to span a broad range of environmental conditions within New Zealand, to (i) develop models of infection and foliage retention, F_ret, and (ii) from these models predict F_ret by region under current and future climates, using the factorial combination of 12 Global Climate Models (GCMs) and three emission scenarios (low, B1; medium, A1B; and high, A2).     

A new fungitoxic metabolite from Spiraea alpina Pall.

The fungitoxic metabolites of Spiraea alpina Pall. were identified using inhibition of Rhizoctonia solani, Gibberella zeae, Pyricularia oryzea and Exserohilum turcicum as an end-point. The major fungitoxic constituent of S. alpina was a new diacylated sugar, structurally elucidated as 6-O-(3′,4′-dihydroxy-2′-methylenbutyryl)-1-O-trans-cinnamoyl-β-D-glucopyranose. This compound could inhibit at 0.1 mg/ml Rhizoctonia solani and Exserohilum turcicum, 87.6% and 63.2%, respectively.     

Flavonoids with prolyl oligopeptidase inhibitory activity isolated from Scutellaria racemosa Pers

Prolyl oligopeptidase (POP) is a serine protease highly expressed in the brain that hydrolyses peptide bonds at the carboxyl terminal of prolyl residues. There is evidence that this enzyme participates in several functions of the central nervous system. Scutellaria racemosa Pers demonstrated significant and selective POP inhibition. Fractionation of the hydroalcoholic extract resulted in the isolation of four main constituents identified for the first time from S. racemosa Pers, the triterpenoid lupeol (1) and the flavonoids oroxylin A (5,7-dihydroxy-6-methoxyflavone, 2), hispidulin (4′,5,7-trihydroxy-6-methoxyflavone, 3), and oroxyloside (oroxylin A 7-O-glucuronide, 4). Inhibitory assays indicated that 3 and 4 at a concentration of 100 μM inhibit 43 and 34% of total POP activity, respectively.     

猴头菌锰过氧化物酶1基因在构巢曲霉的异源转化与表达

为提高猴头菌菌株CB1锰过氧化物酶(MnP)基因的表达产量,采用PEG/CaCl2介导的原生质体转化方法,将携带有He-mnp1的重组质粒pLB01/He-mnp1转入到构巢曲霉尿嘧啶尿苷营养缺陷菌株TN02A7的原生质体中,获得了转化子菌株TN02A7-He-mnp1,并在乙醇脱氢酶启动子alcA(p)控制下实现了异源表达。将TN02A7-He-mnp1、TN02A7、构巢曲霉野生型菌株WJA01、猴头菌菌株CB1在相同的木质素环境下进行培养并检测MnP酶活性,结果表明:转化子菌株TN02A7-He-mnp1在0.05 g.L-1血红素的情况下、诱导96 h后酶活性最高为38.31 U.L-1,比不添加血红素的酶活力高8.64倍,但比猴头菌菌株CB1的酶活力低,而TN02A7与WJA01始终无MnP酶活性,说明基因He-mnp1已经成功地被转化到TN02A7-He-mnp1中,并在木质素环境下得到表达,血红素是重组MnP基因异源表达的限制性因素之一。本文为生产MnP和提高MnP产量提供了新的途径。     

白花泡桐优树试管嫁接幼化及组培快繁技术研究

以白花泡桐优树‘白优2号’为试验材料,通过组织培养和试管嫁接方法,对白花泡桐优树材料的幼化技术进行了研究.结果表明:外植体初代培养萌发的嫩芽为最适合的接穗;‘建始桐3号’为试管嫁接较合适的砧木;采用劈接进行;MS+ NAA0.3 mg·L-1+蔗糖30 g·L-1为试管嫁接培养基;继代增殖和生根培养基分别为1/2MS ...     

BACE inhibitory flavanones from Balanophora involucrata Hook. f.

One new flavanone (S)-5,7,3′,5′-tetrahydroxy-flavanone-7-O-(6″-galloyl)-β-D-glucopyranose (1), together with one known flavanone and four known dihydrochalcones were isolated from the ethyl acetate partitions from an alcoholic extract of the whole plant of Balanophora involucrata Hook. f. All of the compounds were characterized by spectroscopic methods. Their in vitro BACE inhibitory effects were evaluated. Compounds 1, 2, 4, and 5 were found to be a little more active than the positive control, although all of which are below 50% inhibition at 10 μM.     

A new triglucosylated naphthalene glycoside from Aloe vera L.

A new triglucosylated naphthalene derivative, named aloveroside A (1), together with two known anthraquinone dimers and two 6-phenyl-2-pyrone derivatives, was isolated from the Aloe vera ethanolic extracts. The structure of 1 was established as 1-(((4-(1-O-β-D-glucopyranosyl -(1→4)-β-D-xylopyranoside)-hydroxymethyl)-1-hydroxy-8-O-α-L-rhamnopyranoside)naphthalene-2-yl)-ethanone by means of spectroscopic evidences and chemical methods. All these compounds were tested for their BACE inhibitory activity but no significant activities were found.     

Chromones and coumarins from the dried fructus of Cnidium monnieri

Chemical investigations on the ethanolic extract of the dried fructus of Cnidium monnieri offered three chromones and eight coumarins. Among them, a new chromone and a new coumarin were identified and elucidated as 5,7-dihydroxy-6-[(2Z)-4-(β-d-glucopyranosyl)oxy-3- methylbut-2-enyl]-2-hydroxymethyl-4H-1-benzopyran-4-one (1, hydroxycnidimoside A) and (rel 1′S,2′R)-8-(2,3-epoxy-1-hydroxy-3-methylbutyl)-7-methoxycoumarin (8, hydroxyosthole epoxide), respectively, by extensive analyses of spectroscopic data including 1- and 2-D NMR, MS, UV, OR, IR, and HRMS data. The other known compounds were identified by analyses of spectroscopic data and by comparison with literature reported.