白皮锦鸡儿黄酮醇类化合物及其抗菌和抗氧化活性(英文)

从豆科植物白皮锦鸡儿(Caragana leucophloea Pojark.)地上部分分离到3个黄酮醇类化合物,经理化和波谱分析鉴定为3-O-甲基山奈酚(1)、3-O-甲基槲皮素(2)和槲皮素(3)。活性测定表明,1表现出较强的抗细菌活性,对大肠杆菌和番茄疮痂病菌的半抑制浓度分别为9.00μg/mL和7.42μg/mL,最低抑制浓度均为12.5μg/mL;而2和3则表现出较强的抗氧化活性,对DPPH还原的半抑制浓度分别为14.39μg/mL和13.64μg/mL;对β-胡萝卜素-亚油酸氧化的半抑制浓度分别为10.26μg/mL和9.87μg/mL。上述黄酮醇类化合物均为首次从白皮锦鸡儿中分离得到。     

An anti-inflammatory isoflavone from soybean inoculated with a marine fungus Aspergillus terreus C23-3

ABSTRACT

A new isoflavone derivative compound 1 (psoralenone) was isolated from soybean inoculated with a marine fungus Aspergillus terreus C23-3, together with seven known compounds including isoflavones 2–6, butyrolactone I (7) and blumenol A (8). Their structures were elucidated by MS, NMR, and ECD. Psoralenone displayed moderate in vitro anti-inflammatory activity in the LPS-induced RAW264.7 cell model. Compound 2 (genistein) showed moderate acetylcholinesterase (AChE) inhibitory activity whereas compounds 2, 5 (biochanin A), 6 (psoralenol), and 7 exhibited potent larvicidal activity against brine shrimp. Compounds 3 (daidzein), 4 (4?-hydroxy-6,7-dimethoxyisoflavone), and 5–7 showed broad-spectrum anti-microbial activity, and compound 7 also showed moderate 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity.     

Flemiphyllin,an isoflavone from stems of Flemingia macrophylla

A new isoflavone, designated flemiphyllin, was isolated from a petrol extract of the stems of Flemingia macrophylla. Its structure was established as 5,7,4′-trihydroxy-3′,5′,8-tri(3-methylbut-2-enyl) isoflavone on the basis of physical and chemical evidence.     

Dual antioxidant structures with potent anti-inflammatory,hypolipidemic and cytoprotective properties

Novel amide derivatives of trolox, 3,5-di-tert-butyl-4-hydroxybenzoic acid, (E)-3-(3,5-di-tert-butyl-4-hydroxyphenyl)acrylic acid and cinnamic acid with cysteamine and l-cysteine ethyl ester were synthesised. In four cases, the disulfide derivatives were also isolated and tested. All compounds were examined for antioxidant activity, expressed as their ability to inhibit lipid peroxidation and to scavenge free radicals. They were found to demonstrate up to 17-fold better activity than that of the parent antioxidant acids. They could reduce acute inflammation up to 87%. The most active antioxidant compounds were further tested for their in vivo hypolipidemic effect, which ranged from 47% to 73%, and for their ability to protect the liver against oxidative toxicity caused by high paracetamol dose. The disulfide derivatives of 3,5-di-tert-butyl-4-hydroxybenzoic acid and cinnamic acid had no antioxidant activity and presented equal or lower anti-inflammatory effect than their thiol analogues, indicating that their molecular characteristics may not permit biological barrier penetration.     

Viridiflorin,an isoflavone from Tephrosia viridiflora

A new isoflavone, viridiflorin, has been isolated from Tephrosia viridiflora. Its structure was established as 4′,5,7-trihydroxy-2′,5′-dimethoxy-6-prenylisoflavone based on spectral evidence and chemical transformation.     

子树分析和TASS程序及其在锦鸡儿属植物中的应用

子树分析和三分法 (TASS)程序是历史生物地理学中分布区关系的一种分析途径。它以分类群分支图为基础 ,以剔除其中分布区关系相悖理的结点并确定具信息的子树为目标 ,以便更有效地利用分布区信息。对分布区关系可以用若干子树和一个分布区分支图来表示。对锦鸡儿属 (Caragana)植物 72种和 13个分布区的子树分析和TASS程序运算后 ,得到 7个具信息的子树 ,它们分别表达了锦鸡儿属属内组、系所具有的分布区关系。属的分布区分支图也表达了 13个分布区的关系。与以前我们对本属成分分析的结果相吻合。     

子树分析和TASS程序及其在锦鸡儿属植物中的应用

子树分析和三分法(TASS)程序是历史生物地理学中分布区关系的一种分析途径.它以分类群分支图为基础,以剔除其中分布区关系相悖理的结点并确定具信息的子树为目标,以便更有效地利用分布区信息.对分布区关系可以用若干子树和一个分布区分支图来表示.对锦鸡儿属(Caragana)植物72种和13个分布区的子树分析和TASS程序运算后,得到7个具信息的子树,它们分别表达了锦鸡儿属属内组、系所具有的分布区关系.属的分布区分支图也表达了13个分布区的关系.与以前我们对本属成分分析的结果相吻合.     

Evaluation of anti-inflammatory and antioxidant activities of Copper (II) Schiff mono-base and Copper(II) Schiff base coordination compounds of dien with heterocyclic aldehydes and 2-amino-5-methyl-thiazole

Highly reactive radicals are implicated in many pathological conditions. The quest for radical scavengers or antioxidants, spans the previous decades. A new series of complexes of the type [Cu (dien) (2a-2tzn) Y₂] and [Cu (dienXXY₂) (2a-5mt)] and of the type [Cu (dptaS) Cl₂] and [Cu (dptaS) Br₂] (dptaS = 1, 3-propanediamine) or Schiff mono-base of dipropylenetriamine with 2-thiophene-carboxaldehyde, has been tested for anti-inflammatory and antioxidant activity. The tested compounds inhibit the carrageenin-induced rat paw edema (52.0–82.6%) and present important scavenging activity. Compound 6 is the most potent (82.6%) in the in vivo experiment. Lipophilicity-as R_M values – has been determined. The results support that in general, adducts of the type [Cu (dienXXY₂) (2a-5mt)] exhibit increased activity compared to the starting material of type [Cu (dienXXY₂)]. An attempt to correlate the biological results with their structural characteristics and physicochemical parameters has been made     

Modulation of cyclophosphamide-induced early lung injury by curcumin,an anti-inflammatory antioxidant

Cyclophosphamide causes lung injury in rats through its ability to generate free radicals with subsequent endothelial and epithelial cell damage. In order to observe the protective effects of a potent anti-inflammatory antioxidant, curcumin (diferuloyl methane) on cyclophosphamide-induced early lung injury, healthy pathogen free male Wistar rats were exposed to 20 mg/100 g body weight of cyclophosphamide, intraperitoneally as a single injection. Prior to cyclophosphamide intoxication oral administration of curcumin was performed daily for 7 days. At various time intervals (2, 3, 5 and 7 days post insult) serum and lung samples were analyzed for angiotensin converting enzyme, lipid peroxidation, reduced glutathione and ascorbic acid. Bronchoalveolar lavage fluid was analyzed for biochemical constituents. The lavage cells were examined for lipid peroxidation and glutathione content. Excised lungs were analyzed for antioxidant enzyme levels. Biochemical analyses revealed time course increases in lavage fluid total protein, albumin, angiotensin converting enzyme (ACE), lactate dehydrogenase, N-acetyl--D-glucosaminidase, alkaline phosphatase, acid phosphatase, lipid peroxide levels and decreased levels of glutathione (GSH) and ascorbic acid 2, 3, 5 and 7 days after cyclophosphamide intoxication. Increased levels of lipid peroxidation and decreased levels of glutathione and ascorbic acid were seen in serum, lung tissue and lavage cells of cyclophosphamide groups. Serum angiotensin converting enzyme activity increased which coincided with the decrease in lung tissue levels. Activities of antioxidant enzymes were reduced with time in the lungs of cyclophosphamide groups. However, a significant reduction in lavage fluid biochemical constituents, lipid peroxidation products in serum, lung and lavage cells with concomitant increase in antioxidant defense mechanisms occurred in curcumin fed cyclophosphamide rats. Therefore, our results suggest that curcumin is effective in moderating the cyclophosphamide induced early lung injury and the oxidant-antioxidant imbalance was partly abolished by restoring the glutathione (GSH) with decreased levels of lipid peroxidation.     

Novel depsides as potential anti-inflammatory agents with potent inhibitory activity against Escherichia coli-induced interleukin-8 production

Sixteen novel depsides were synthesized for the first time. Their chemical structures were clearly determined by ¹H NMR, ESI mass spectra, and elemental analyses. All the compounds were assayed for antibacterial activities against three Gram-positive bacterial strains (Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 6538, and Streptococcus faecalis ATCC 9790) and three Gram-negative bacterial strains (Escherichia coli ATCC 35218, Pseudomonas aeruginosa ATCC 13525, and Enterobacter cloacae ATCC 13047) by the MTT method. Compound 2-(2-methoxy-2-oxoethyl)phenyl 5-bromonicotinate (5) exhibited significant antibacterial activities against E. coli ATCC 35218 with an MIC of 0.78 μg/mL, which was superior to the positive control kanamycin B. In addition, compound 5 showed potent inhibitory activity against E. coli-induced interleukin-8 production.     

极东锦鸡儿幼胚子叶的体细胞胚胎发生和植株再生

以极东锦鸡儿未成熟合子胚子叶为外植体进行其体细胞胚胎发生和植株再生研究。在添加不同BA与NAA或2,4-D,外加500mg·L~（-1）水解酪蛋白、30g·L~（-1）蔗糖和8g·L~（-1）琼脂的MS培养基上诱导产生了体细胞胚。在5mg·L~（-1）NAA＋5mg·L~（-1）BA和5mg·L~（-1）2,4-D＋1mg·L~（-1）BA处理中体胚诱导率分别为14%和10%;NAA处理每外植体上诱导出的体胚数量最多为4.3个,而2,4-D为10.5个。体细胞胚经成熟培养后,在添加0.01mg·L~（-1）NAA、20g·L~（-1）蔗糖和6g·L~（-1）琼脂的MS培养基上萌发率达到58.94%。萌发的体胚在MS培养基上长成正常小植株,再生率为87%。经炼苗后的体胚苗移植到草炭土：蛭石：珍珠岩=5：4：1（V/V/V）的栽培基质中,可以正常生长,移栽成活率为40%。     

小叶锦鸡儿花提取物和不同极性黄酮组分的抗氧化活性(英文)

测定了小叶锦鸡儿(Caragana microphylla Lam.)花粗提物和不同极性组分总黄酮含量和各项抗氧化能力指标。结果表明:小叶锦鸡儿花不同极性的黄酮组分的抗氧化活性有明显差别,其总抗氧化能力与溶剂极性之间有显著正相关性(P<0.05),但其它抗氧化活性与溶剂极性之间均无显著相关性(P>0.05)。同一极性黄酮组分在不同抗氧化体系中的抗氧化活性有较大差别。对DPPH.自由基的清除能力最强的为乙酸乙酯层(EC50=0.11 mg/mL),其次是二氯甲烷层(EC50=0.38 mg/mL)和乙醇粗提物(EC50=0.56 mg/mL)。总抗氧化能力(T-AOC)最强的为水层,在1 mg/mL时为1.482个T-AOC能力单位。清除羟自由基.OH能力最强的为水层,其次为正己烷层和乙醇粗提物,在3.57 mg/mL时清除率分别为86.23%、66.04%和64.63%。清除超氧阴离子自由基O2-.能力最强的为水层,其次为乙醇粗提物,在1 mg/mL时其清除率分别相当于0.15 mg/mL Vc清除率的336.17%和318.20%。可见,小叶锦鸡儿花的粗提物和不同极性黄酮组分具有较好的抗氧化活性,可用于提取、制备抗氧化特性和作用不同的天然抗氧化剂。     

柠条锦鸡儿籽油体外抗真菌作用及其机制研究(英文)

参照美国临床实验室标准化委员会(NCCLS)推荐的《产孢丝状真菌的液基稀释法抗真菌药物敏感性试验方案》(M38-A),测定超临界CO2萃取的柠条锦鸡儿籽油对3种(每种15株)临床常见的皮肤癣菌的最低抑菌浓度(MIC);高效液相色谱法研究柠条锦鸡儿籽油对真菌细胞膜麦角甾醇生物合成的影响以探讨其作用机制。结果表明柠条锦鸡儿籽油对犬小孢子菌、须癣毛癣菌、红色毛癣菌的MIC范围分别为64～512μg/mL、32～512μg/mL、64～1024μg/mL;高效液相色谱法检测显示,与其生长对照菌相比,籽油作用的皮肤癣菌细胞膜上麦角甾醇含量明显降低,且具有剂量依赖性。柠条锦鸡儿籽油主要是通过影响真菌细胞膜上麦角甾醇的合成而发挥抗真菌作用。     

柠条锦鸡儿肌动蛋白基因的克隆和表达稳定性分析

以几种豆科植物中肌动蛋白的氨基酸保守序列设计简并引物,采用RT—PCR结合RACE扩增技术,从柠条锦鸡儿叶片中克隆到一个编码肌动蛋白的基因,命名为CkACT。该基因cDNA全长为1655bp,开放阅读框1134bp,编码377个氨基酸。氨基酸比对分析表明,该基因编码的氨基酸与其他植物肌动蛋白基因具有较高的同源性。不同组织中的表达基本上一致,不同发育时期的基因表达相似,低温、NaCl、干旱和ABA处理后的表达强度没有明显差异,说明CkACT基因表达稳定。     

Crystal structure of isoflavone reductase from alfalfa (Medicago sativa L.)

Isoflavonoids play important roles in plant defense and exhibit a range of mammalian health-promoting activities. Isoflavone reductase (IFR) specifically recognizes isoflavones and catalyzes a stereospecific NADPH-dependent reduction to (3R)-isoflavanone. The crystal structure of Medicago sativa IFR with deletion of residues 39-47 has been determined at 1.6A resolution. Structural analysis, molecular modeling and docking, and comparison with the structures of other NADPH-dependent enzymes, defined the putative binding sites for co-factor and substrate and potential key residues for enzyme activity and substrate specificity. Further mutagenesis has confirmed the role of Lys144 as a catalytic residue. This study provides a structural basis for understanding the enzymatic mechanism and substrate specificity of IFRs as well as the functions of IFR-like proteins.