Inhibitors of inducible nitric oxide synthase expression from<Emphasis Type="Italic">artemisia iwayomogi</Emphasis>

Nitric oxide (NO) is an important bioactive agent that mediates a wide variety of physiological and pathophysiological events. NO overproduction by inducible nitric oxide synthase (iNOS) results in severe hypotension and inflammation. This investigation is part of a study to discover new iNOS inhibitors from medicinal plants using a macrophage cell culture system. Two sesquiterpenes (1 and 2) were isolated from Artemisia iwayomogi (Compositae) and were found to inhibit NO synthesis (IC50 3.64 microg/mL and 2.81 microg/mL, respectively) in lipopolysaccharide (LPS)-activated RAW 264.7 cells. Their structures were identified as 3-O-methyl-isosecotanapartholide (1) and iso-secotanapartholide (2). Compounds 1 and 2 inhibited the LPS-induced expression of the iNOS enzyme in the RAW 264.7 cells. The inhibition of NO production via the down regulation of iNOS expression may substantially modulate the inflammatory responses.     

Constituents from leaves of Apocynum venetum L.

An analysis using HPLC–MS revealed that an extract from dried leaves of Apocynum venetum L. contained more than 15 kinds of phenolic constituents. Two malonated flavonol glycosides were further isolated, and their structures were determined to be quercetin 3-O-(6′′-O-malonyl)-β-d-glucoside (1) and quercetin 3-O-(6′′-O-malonyl)-β-d-galactoside (2) by NMR spectroscopic analysis. This is the first report describing the isolation of these malonated flavonol glycosides from A. venetum L. Both glycosides showed strong scavenging activity against 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical.     

Extracts from Rhois aromatica and Solidaginis virgaurea inhibit rat and human bladder contraction

Since extracts from the plants Rhois aromatica and Solidaginis virgaurea are being used in the phytotherapy of bladder dysfunction including the overactive bladder syndrome, and since muscarinic receptors are the main pharmacological target in the treatment of bladder dysfunction, we have investigated whether these extracts can inhibit carbachol-induced, muscarinic receptor-mediated contraction of rat and human bladder. In vitro contraction experiments were performed with rat and human bladder strips. Radioligand binding and inositol phosphate accumulation studies were done with cells transfected with human M₂ or M₃ muscarinic receptors. Both extracts concentration-dependently (final concentrations 0.01–0.1%) inhibited carbachol-induced contraction of rat and human bladder with insurmountable antagonism. Radioligand binding experiments and inositol phosphate accumulation studies with cloned receptors demonstrated direct but non-competitive effects on muscarinic receptors. Reductions of KCl-induced bladder contraction demonstrated that inhibition by the higher extract concentrations also involved receptor-independent effects. We conclude that extracts from Rhois aromatica and Solidaginis virgaurea inhibit muscarinic receptor-mediated contraction of rat and human bladder. While this could contribute to the beneficial effects of these extracts in patients with bladder dysfunction, such therapeutic effects remain to be demonstrated in controlled clinical studies.     

UHPLC同时测定进口西洋参4个化学成分的含量

目的 建立UHPLC同时测定进口西洋参中4个活性成分（人参皂苷Rg₁、人参皂苷Re、人参皂苷Rb₁和人参皂苷Rd）含量的方法。方法 采用Zorbax SB C₁₈（2.1 mm×100 mm,1.8 μm）色谱柱,以乙腈为流动相A,水为流动相B,梯度洗脱,流速0.5 mL·min^-1,柱温30℃,检测波长为203 nm。结果 4种成分的分离度良好,且在各自浓度范围内呈现良好的线性关系（r≥0.999 9）,平均回收率为95.7%~100.3%（RSD1.4%~1.8%）。结论 该方法操作简单,缩短了分析时间,重复性好,为评价进口西洋参的质量提供了可靠的方法。     

Sesquiterpenoids from Ferula fukanensis and their inhibitory effects on nitric oxide production

Six sesquiterpene derivatives, 2,3-dihydro-7-methoxy-2S*, 3R*-dimethyl-2-[4,8-dimethyl-3(E),7-nonadienyl]furo[3,2-c]coumarin (1) and 2,3-dihydro-7-methoxy-2R*,3R*-dimethyl-2-[4,8-dimethyl-3(E),7-nonadienyl]furo[3,2-c]coumarin (2), nerolidol (3), 1-(2,4-dihydroxyphenyl)-3,7,11-trimethyl-3-ninyl-6(E),10-dodecadien-1-one (4), 1-(2,4-dihydroxyphenyl)-3,7-dimethyl-3-vinyl-8-(4-methyl-2-furyl)-6(E)-octen-1-one (5) and dshamirone (6) were isolated from an 80% aqueous methanol extract of the roots of Ferula fukanensis. The sesquiterpenoids inhibited nitric oxide (NO) production and inducible NO synthase gene expression by a murine macrophage-like cell line (RAW 264.7) [1], which was activated by lipopolysaccharide and recombinant mouse interferon-.     

我国姜科药用植物研究——Ⅳ.姜三七醌(Stahlianthusone)的化学结构

从草药姜三七的挥发油得到一种新倍半萜醌,分子式C₁₅H₁₆O₂,定名为姜三七醌(Ia)(Stahlianthusone)。经光谱分析和化学反应测定了其化学结构为1,6-二甲基4-异丙基萘醌-5,8。     

附子的化学成分研究

利用各种色谱方法对毛茛科(Ranunculaceae)植物川乌(Aconitum carmichaeli Debx.) 的子根附子的化学成分进行了研究,从中分离得到了8个二萜生物碱类化合物,根据化合物的理化性质和波谱数据确定了化合物的结构,它们分别为海替生(1)、8-乙氧基-14-苯甲酰基中乌头原碱(2)、10-羟基乌头碱(3)、次乌头碱(4)、中乌头碱(5)、北草乌碱(6)、尼奥灵(7)、附子灵(8),其中化合物1～3为首次从该植物中分离得到.     

丹参柯巴基焦磷酸合酶基因的优化表达、纯化及抗体制备

用含丹参柯巴基焦磷酸合酶(Salvia miltiorrhiza copalyl diphosphate synthase，SmCPS)基因的重组质粒pET32CPS转化大肠杆菌BL21trxB (DE3)进行诱导表达，SDS-PAGE结果表明SmCPS基因在大肠杆菌中获得了表达；对影响可溶性表达的4个因素，即诱导温度、IPTG诱导浓度、诱导时宿主菌的密度(A₆₀₀)和诱导时间进行了优化。结果发现在宿主菌A₆₀₀达到1.0时加入0.4 mmol·L^-1 IPTG，在20 ℃诱导培养8 h表达的可溶性蛋白量最高，约占细胞总蛋白的35.6%。用Ni²⁺亲和色谱法纯化表达产物，纯化蛋白产率达到12.3 mg·L^-1。将纯化蛋白免疫制备兔源SmCPS抗血清，ELISA测定效价为1∶24 300，且经Western blotting鉴定该抗体可特异性识别SmCPS抗原，获得了效价高、免疫反应性好的SmCPS多克隆抗体，为进一步从蛋白水平研究SmCPS表达与丹参酮类有效成分生物合成相关性提供了物质基础。     

藜的化学成分研究

目的：对藜Chenopodium olbumL.的抗过敏活性成分进行研究。方法：利用色谱的方法分离成分。利用光谱和化学方法鉴定其化学结构。结果：从藜的种子中分离得到3个化合物。经光谱和化学分析，鉴定为28-氧-β-D-吡喃葡萄糖基-齐墩果酸-3-氧-β-D-吡喃葡萄糖醛酸甙（1），20-羟基蜕皮酮（2）和芦丁（3）。结论：化合物1，2和3均为首次从该植物分离得到。     

In vitro and ex vivo activity of new derivatives of acetohydroxyacid synthase inhibitors against Mycobacterium tuberculosis and non-tuberculous mycobacteria

Sulfometuron methyl (SM) is an inhibitor of acetohydroxyacid synthase (AHAS), the first common enzyme in the branched-chain amino acid biosynthetic pathway, and shows activity against Mycobacterium tuberculosis both in vitro and in vivo. To develop AHAS inhibitor derivatives with more potent activity, 100 sulfonylurea analogues were screened for antimycobacterial activity against M. tuberculosis and non-tuberculous mycobacteria (NTM), and then evaluated for intracellular activity using mouse macrophages. Three new compounds with antimycobacterial activity comparable with that of SM were identified. These compounds exhibit significant activity against intracellular M. tuberculosis (including the drug-resistant M. tuberculosis strains), and NTM Mycobacterium abscessus and Mycobacterium kansasii, respectively.     

Identification and characterization of nitric oxide synthase inSalmonella typhimurium

The presence of the nitric oxide synthase (NOS) enzyme from Salmonella typhimurium (S. typhimurium) was identified by measuring radiolabeled L-[3H]citrulline and NO, and Western blot analysis. NOS was partially purified by both Mono Q ion exchange and Superose 12HR size exclusion column chromatography, sequentially. The molecular weight of NOS was estimated to be 93.3 kDa by Western blot analysis. The enzyme showed a significant dependency on the typical NOS cofactors; an apparent Km for L-arginine of 34.7 mM and maximum activity between 37 degrees C and 43 degrees C. The activity was inhibited by NOS inhibitors such as aminoguanidine and N(G),N(G)-dimethyl-L-arginine. Taken together, partially purified NOS in S. typhimurium is assumed to be a different isoform of mammalian NOSs.     

维药香青兰叶的化学成分研究

对香青兰叶的化学成分进行研究,分离得到11个化合物,分别鉴定为Acacetin-7-O-β-D-glucopyranoside-6"-O-malonyl ester(1),Luteolin(2),Acacen(3),Diosmetin(4),Agastachoside(5),Kaemferol(6),Luteolin-7-O-β-D-Glucopyran-oside(7),Apigenin-7-O-β-D-glucopyranoside(8),Acacetin-7-O-β-D-glucopyranosi-de(9),β-Sitosterol(10),Esculetin(11).化合物4,7～11均为该植物中首次分离得到.     

桂郁金化学成分研究

从姜科植物桂郁金即广西莪术(Curcuma kwangsiensis)的块根分离鉴定出9个化合物,分别为:汉黄芩素(1)、木犀草素(2)、姜黄素(3)、15,16-bisnorlabda-8(17),11-dien--13-one(4),桂莪术内酯(5)、尿嘧啶(6)、3,4-二羟基苯甲酸(7),对羟基苯甲醛(8)、对羟基苯甲酸(9).其中化合物1、2、4、6为首次从本属植物中分到,化合物3、7、8为首次从该植物中分到,化合物5、9首次从桂郁金中分到.     

Constituents of the leaves and roots of Ligularia stenocephala MATSUM. et KOIDZ.

Constituents of the leaves and roots of Ligularia stenocephala MATSUM. et KOIDZ. (Compositae) were investigated. Three compounds, (2E,6E,10E,14E,18E)-2,6,10,15,19,23-hexamethyl-2,6,10,14,18,22-tetracosahexaen-1-ol, (3E,6E,10E,14E,18E)-2,6,10,15,19,23-hexamethyl-3,6,10,14,18,22-tetracosahexaen-2-ol and neophytadiene, were isolated from the leaves of L. stenocephala. Six compounds, 5-acetyl-6-hydroxy-2α-isopropenyl-3β-methoxy-2,3H-benzofuran, 3β-acetoxy-6-acetyl-5-hydroxy-2α-isopropenyl-2,3H-benzofuran, p-hydroxybenzaldehyde, vanillin, 4-hydroxyacetophenone and 4-hydroxy-3-methoxyacetophenone, were isolated from the roots of L. stenocephala. The structures were determined on the basis of spectral data.     

对叶百部中的非生物碱类成分

从百部科植物对叶百部中分离鉴定了11个化合物,分别为大黄素甲醚(1),3-羟基-4-甲氧基苯甲酸(2),对羟基苯甲酸(3),(Z)-1,1′-biindenyliden(4),胸腺嘧啶(5),2-(1′,2′,3′,4′-四羟基丁基)-6-(2′′,3′′,4′′-三羟基丁基)-吡嗪(6),掌叶半夏碱戊(7),豆甾醇(8),β-谷甾醇棕榈酸酯(9),β-谷甾醇(10)和β-胡萝卜苷(11)。其中化合物1～9均为首次从该科植物中分得。     

Mutations in dihydropteroate synthase gene of Pneumocystis carinii in HIV patients with Pneumocystis carinii pneumonia

The purpose of this study was to determine whether dihydropteroate synthase gene (DHPS) mutations were associated with the failure of sulpha/sulphone drugs used as prophylaxis agents in HIV infected patients. Results suggested that DHPS mutations were significantly associated with failure of anti-Pneumocystis carinii sulphone prophylaxis (P=0.031). An increasing number of mutant P. carinii strains have been isolated from patients no longer having prophylaxis. There was no statistically significant difference in severity or outcome of the pneumonia caused by wild-type or mutant DHPS. Moreover, two of the three patients with mutant P. carinii pneumonia (PCP) were successfully treated with sulpha drugs. We think that P. carinii drug-resistance could be an emerging problem for immunocompromised patients including those with HIV infection.     

啤酒花抗骨质疏松的应用及展望

啤酒花是我国新疆药食兼用的特色资源植物。除广泛用于啤酒酿制外,人们很早就认识到啤酒花的药用价值,尤其是将其用于绝经后骨质疏松的治疗。现代药理研究发现,啤酒花的多种活性成分在抗骨质疏松药物研发方面具有巨大潜力。然而,近年来,我国野生啤酒花资源品种退化严重,活性成分含量差异较大。保障优良的啤酒花种质资源,是啤酒花开发利用的前提。本文就啤酒花的主要化学成分及其防治骨质疏松症的作用及相关应用进行综述,并就目前存在的问题进行探讨,旨在为啤酒花抗骨质疏松的开发利用提供借鉴。     

A curcuminoid and two sesquiterpenoids from<Emphasis Type="Italic">Curcuma zedoaria</Emphasis> as Inhibitors of nitric oxide synthesis in activated macrophages

The overproduction of nitric oxide (NO) by inducible nitric oxide synthase (iNOS) is known to be responsible for vasodilation and hypotension observed in septic shock and inflammation. Inhibitors of iNOS, thus, may be useful candidates for the treatment of inflammatory diseases accompanied by overproduction of NO. In the course of screening oriental anti-inflammatory herbs for the inhibitory activity of NO synthesis, a crude methanolic extract of Curcuma zedoaria exhibited significant activity. The activity-guided fractionation and repetitive chromatographic procedures with the EtOAc soluble fraction allowed us to isolate three active compounds. They were identified as 1,7-bis (4-hydroxyphenyl)-1,4,6-heptatrien-3-one (1), procurcumenol (2) and epiprocurcumenol (3) by spectral data analyses. Their concentrations for the 50% inhibition of NO production (IC50) in lipopolysaccharide (LPS)-activated macrophages were 8, 75, 77 microM, respectively. Compound 1 showed the most potent inhibitory activity for NO production in LPS-activated macrophages, while the epimeric isomers, compound 2 and 3 showed weak and similar potency. Inhibition of NO synthesis by compound 1 was very weak when activated macrophages were treated with 1 after iNOS induction. In the immunoblot analysis, compound 1 suppressed the expression of iNOS in a dose-dependent manner. In summary, 1,7-bis (4-hydroxyphenyl)-1,4,6-heptatrien-3-one from Curcuma zedoaria inhibited NO production in LPS-activated macrophages through suppression of iNOS expression. These results imply that the traditional use of C. zedoaria rhizome as anti-inflammatory drug may be explained at least in part, by inhibition of NO production.     

Inducible nitric oxide synthase inhibitors fromMelia azedarach var.Japonica

In bioassay-guided search for inducible nitric oxide synthase (iNOS) inhibitory compounds from higher plants of South Korea, two beta-carboline alkaloids, 4-methoxy-1-vinyl-beta-carboline (1) and 4,8-dimethoxy-l-vinyl-beta-carboline (2) have been isolated from the cortex of Melia azedarach var. japonica. The structures of these compounds were elucidated on the basis of spectroscopic data. Compounds 1 and 2 showed marked inhibitory activity of iNOS on LPS- and interferon-gamma-stimulated RAW 264.7 cells.     

素馨花中一个新的环烯醚萜苷

为研究木犀科植物素馨花干燥花蕾的化学成分， 通过硅胶柱色谱、 Sephadex LH-20柱色谱、 HPLC和重结晶等方法进行分离纯化， 根据化合物的理化性质和波谱数据鉴定结构， 从素馨花干燥花蕾70%乙醇提取物中分离得到6个环烯醚萜苷类化合物， 分别鉴定为素馨花苷(I)、 jaspolyoside (II)、 8-epi-kingiside (III)、 10-羟基橄榄苦苷(IV)、 10-羟基女贞苷(V)、 oleoside-7,11-dimethyl ester (VI)。化合物I为新化合物，其余为首次从本植物中分离得到。