一株渤海来源真菌Pleosporales sp.中嗜氮酮类化合物及其生物活性△

目的 对一株渤海来源真菌Pleosporales sp.中嗜氮酮类化合物进行分离鉴定,并探讨其生物活性。方法 利用硅胶柱层析和高效液相色谱等分离手段对化合物进行分离和纯化;运用NMR和MS等现代波谱方法,并结合相关文献,对化合物的结构进行鉴定;运用抗真菌活性模型对化合物的生物活性进行评价。结果 从该真菌中分离获得了6个嗜氮酮类化合物isochromophilone I, VI, IX (1–3), (+)-sclerotiorin (4), 5-chloroisorotiorin (5), hypocrellone A (6)。化合物1–6对三株农业致病真菌Thielaviopsis paradoxa, Pestalotia calabae, 和Glorosprium musarum均显示出中等强度的抑制活性。结论 化合物1–6均为首次从Pleosporales属真菌中分离得到,具有作为抗农业致病真菌药的研究价值。     

一株海洋真菌Penicillium chrysogenum次级代谢产物及其抗菌活性研究

目的 研究一株南海来源真菌Penicillium chrysogenum的次级代谢产物及抗菌活性。方法 运用硅胶柱层析、Sephadex LH-20凝胶柱层析和HPLC半制备等方法对次级代谢产物进行分离和纯化;通过NMR、MS等方法鉴定化合物结构;利用抗菌活性模型对其进行活性评价。结果 从真菌P. chrysogenum中分离鉴定了5个化合物,包括一个结构复杂的生物碱taichunamide H (1),一个带有脂肪链的蒽醌1-O-methyl-averantin (2),两个聚酮类化合物versicone A (3)和 versicone B (4) 以及一个联苯醚diorcinol (5);其中,2对致病菌Canidia albicans和 Staphylococcus aureus具有显著的抑制活性,MIC值分别为6.25 μM和12.5 μM;5对海洋污损菌Photobacterium halotolerans显示抑制活性,MIC值为 50 μM。结论 化合物3和 4为首次从青霉菌中分离得到;化合物2具有显著的抗菌活性,具有重要的研究和潜在开发价值。     

1株红树来源真菌Penicillium sp.次级代谢产物及其生物活性研究

目的 研究1株红树来源真菌Penicillium sp.中的次级代谢产物及生物活性。方法 综合运用硅胶柱层析和半制备型HPLC等方法分离纯化次级代谢产物,利用NMR及MS等现代波谱分析方法鉴定化合物结构,以斑马鱼血管抑制模型对其进行活性评价。结果 在细胞毒活性的指导下,从Penicillium sp.中分离出抗肿瘤活性化合物brefeldin A,同时还分离出5个天然产物,分别是 (+)-semivioxanthin (1)、(-)-striatisporolide A (2)、dibutyl phthalate (3)、bisdethiobis (methylthio)-acetylapoaranotin (4) 和alternarosin A (5)。其中化合物1和3分别在1 μmol/L和10 μmol/L浓度下显示出斑马鱼血管抑制活性,但同时会导致一定的脊柱弯曲。化合物3还具有抑制硅藻附着的潜在防污活性。结论 化合物4和5为首次从真菌Penicillium sp.中分离获得。化合物1和3具有潜在的生物活性。     

一株海洋真菌Talaromyces sp.的次级代谢产物及抗细菌活性研究

目的 研究一株浙江舟山东海沉积物来源真菌Talaromyces sp. ZHS32次级代谢产物及其抗菌活性。方法 利用硅胶柱层析、Sephadex LH-20凝胶柱层析和半制备高效液相色谱等分离方法对该菌株发酵粗提物进行分离纯化;通过核磁共振波谱（NMR）、质谱（MS）等方法并结合相关文献数据比对鉴定化合物结构;采用肉汤微量稀释法对化合物进行抗菌活性评价。结果 从海洋真菌Talaromyces sp. ZHS32中分离鉴定了7个已知化合物,分别为dankasterone A（1）、penifupyrone（2）、3-O-methylfunicone（3）、alternariol（4）、rubralactone（5）、orsellinic acid（6）和2-formyl-3,5-dihydroxy-6-methylbenzoic acid（7）;体外抗菌活性测试结果表明,化合物1对幽门螺杆菌有较好的抑制作用。结论 从海洋真菌Talaromyces sp. ZHS32中分离得到7个化合物,化合物1具有抑制幽门螺杆菌生长的活性。     

中国东海及东太平洋海山区来源抗菌活性海洋微生物的筛选研究

摘要：目的 研究中国东海及东太平洋区域来源微生物的抗菌活性,意在筛选具有良好抗菌活性的海洋微生物,并初步研究活性菌株代谢产物的结构,为探求新型抗生素提供基础。方法 以金黄色葡萄球菌、大肠杆菌和白色念珠菌为指示菌株,采用牛津杯法进行抗菌活性微生物初筛和复筛。通过HPLC-DAD结合TLC对活性突出的4株真菌及1株细菌进行活性提取物指纹图谱分析。对广谱抗菌活性菌株WBX-38进行菌种鉴定及活性代谢产物分离纯化,利用核磁共振和质谱等手段对活性化合物进行结构鉴定。采用微量稀释法测定活性化合物的最小抑菌浓度（MIC）。结果与结论 从中国东海及东太平洋来源样品中共筛选90株海洋来源菌株,获得抗菌活性菌株16株,4株为海洋细菌,12株为海洋真菌。通过HPLC-DAD结合TLC分析,发现5株活性菌株均具有独特的色谱行为。海洋真菌WBX-38通过菌种鉴定,确认为海洋来源曲霉（Aspergillus sp.）。从其发酵液提取物中分离获得1个活性化合物5-hydroxymethylfuran-3-carboxylic acid,该化合物对3种指示菌均具有一定生长抑制活性。     

一株海兔来源真菌 Aspergillus terreus丁内酯类化合物及其生物活性研究

摘要：目的 在生物活性和化学方法指导下,从1株海兔来源真菌 Aspergillus terreus (RA29-5)中分离鉴定海洋天然产物,并对其进行生物活性评价。方法 运用硅胶柱层析、Sephadex LH-20凝胶柱层析和HPLC等方法分离纯化化合物,利用NMR等现代波谱分析方法,对化合物进行结构鉴定,并对化合物进行抗菌、卤虫致死和斑马鱼胚胎毒性活性评价。结果 鉴定了 9 个丁内酯类化合物 (1～9) 的结构;抗菌活性表明,除化合物 6 和 9 外,所有化合物对四株致病细菌白色葡萄球菌 Staphylococcus epidermidis、金黄色葡萄球菌 Staphylococcus aureus、蜡状芽孢杆菌 Bacillus subtilis 和四联球菌 Tetragenococcus halophilus 都显示一定的抗菌活性;化合物 1～4 和7均对真菌芒果叶枯菌 Pestalotia mangiferae 显示抗菌活性;特别的,化合物 7 对测试的13株致病菌都具有广谱地抗菌活性,其MIC值在1.11~8.88 μmol/L之间;此外,还对化合物的抗菌活性构效关系进行了初步探讨。结论 海兔来源真菌 A. terreus (RA29-5) 可产生结构多样的丁内酯类化合物,该类化合物具有开发成抗菌剂的潜力。     

一种西沙群岛软珊瑚来源真菌中新天然产物pestalalactone的化学与生物活性研究

目的 从一株中国南海西沙群岛软珊瑚来源的真菌Pestalotiopsis sp. (ZJ-2009-7-6) 中分离鉴定具有生物活性的3-苯基苯并呋喃酮化合物。方法 运用多种色谱分离手段和现代波谱分析方法分离和鉴定化合物,最终得到了一个3-苯基苯并呋喃酮类新天然产物pestalalactone (1),并研究了该化合物在不同温度、不同溶剂条件下的优势构象变化;此外,还对化合物的抗藤壶幼虫Balanua amphitrite附着和抗细菌活性进行了评价。结果 分离鉴定了1个新天然产物 pestalalactone (1),发现该化合物以两种不可拆分的阻转异构体的形式 (1a/1b) 并存;核磁共振氢谱研究后发现在氘代吡啶和氘代氯仿中以1a优势构象存在,在氘代甲醇、氘代丙酮和氘代二甲亚砜中的优势构象却是1b,而温度的变化 (25°C–80°C) 并不引起该化合物构象的变化;该化合物显示出强的抗藤壶幼虫B. amphitrite附着活性,其EC₅₀值为2.30 μg/mL,同时也显示出较强的抗细菌活性,特别是对金黄色葡萄球菌Staphylococcus aureus的最小抑制活性为0.45 μg/mL。结论 从一株西沙群岛软珊瑚来源真菌中发现了一个具有重要抗藤壶幼虫B. amphitrite附着和抗菌活性的新天然产物pestalalactone (1),表明西沙群岛来源的海洋微生物具有重要的药用研究价值和应用开发前景。     

海洋真菌Aspergillus sp. SCS-KFD03化学成分研究

目的 对海洋真菌Aspergillus sp. SCS-KFD03的发酵液中化学成分进行分离鉴定,并测定其生物活性。 方法 采用硅胶柱色谱、Sephadex LH-20凝胶柱色谱和高效液相色谱等技术进行分离纯化,运用各种波谱方法对分离所得化合物进行结构鉴定,并测定化合物乙酰胆碱酯酶和α-糖苷酶抑制活性。结果 分离鉴定了9个化合物,经鉴定为phomaligol A1（1）、5-（乙酰氧基甲基）呋喃-3-酸（2）、 phomapyrone C（3）、4-羟基异苯并呋喃-1(3H)-酮（4）、penicillivinacine（5）、22(E)-5α,8α-epidioxyergosta-6,22-dien-3β-ol（6）、lucidal（7）、dankasterone A（8）、bis-(2-methylheptyl)-phthalate（9）,其中化合物4为新天然产物。化合物5、6、7和9具有较弱的乙酰胆碱酯酶抑制的活性,化合物5具有强于阳性药阿卡波糖的α-糖苷酶抑制活性,8和9的α-糖苷酶抑制活性与阳性药相当。结论 化合物1~9均为首次从海洋曲霉属真菌Aspergillus sp. SCS-KFD03中分离得到,部分化合物具有乙酰胆碱酯酶和α-糖苷酶的抑制活性。     

南海深海沉积环境来源真菌Aspergillus sp. SCSIO F063的次生代谢产物研究

目的 采用单株菌多次级代谢产物(OSMAC)策略对一株南海深海沉积环境来源真菌的次生代谢产物进行分离、鉴定及活性研究。方法 通过改变培养基组成并筛选合适的发酵条件,采用硅胶柱层析、反相ODS柱层析、半制备高效液相等色谱学方法对真菌Aspergillus sp. SCSIO F063的发酵产物进行化学分离,利用NMR, MS等波谱学技术并结合文献进行化合物的结构鉴定,并对化合物进行初步的抗氧化活性测试。结果 从菌株SCSIO F063中新增分离鉴定5个单体化合物： 6-O-methyl-averythrin(1), (2,4-dichlorophenyl)-2,4-dichlorobenzoate(2),dibutyl phthalate(3),folipastatin(4),di-(2-ethylhexyl)-phthalate(5)。结论 改变培养基组成可以刺激该菌株产生不同类型的化合物,化合物1-5为首次从真菌SCSIO F063中分离得到。     

1 株海洋真菌Talaromyces sp. HK1-18次级代谢产物及其抗菌活性研究

目的 研究 1 株分离于海南东寨港红树林自然保护区海桑根际土壤的真菌Talaromyces sp. HK1-18的次级代谢产物及其抗菌活性。方法 利用正、反相硅胶柱层析、凝胶柱层析和半制备高效液相色谱等色谱分离方法,对该菌的次级代谢产物进行分离纯化；利用核磁共振波谱以及参考文献等方法,鉴定化合物的结构；采用MIC法对化合物进行抗菌活性评价。结果 从该真菌中分离获得 8个化合物 (1～8),结构分别鉴定为 penicillide(1)、purpactin A(2)、vermistatin(3)、deoxyfunicone(4)、dankasterone A(5)、fortisterol(6)、过氧化麦角甾醇(7)、radiclonic acid(8)。结论 化合物6为首次从Talaromyces属真菌中分离得到。化合物1和8对多药耐药金黄色葡萄球菌(S. aureus ATCC 43300)显示出较强的抑制活性,MIC值均为0.78 μg/mL。化合物6对耐甲氧西林金黄色葡萄球菌(S. aureus ATCC 33591)显示出较强的抑制活性,MIC值为0.78 μg/mL。     

Pharmacological study on piperine

Systematic pharmacological studies on piperine have revealed that this compound elicited diverse pharmacological activities; CNS depressant activity characterized by antagonism against electroshock seizure and by muscle relaxant activity in mice; antipyretic activity in typhoid vaccinated rabbits; analgesic activity as evaluated by tail-clip pressure and writhing syndrome in mice; antiinflammatory activity in carrageenin-induced edema in rats.     

Synthesis of new thiazolylthiazolidinylbenzothiazoles and thiazolylazetidinylbenzothiazoles as potential insecticidal, antifungal, and antibacterial agents

A series of 2-{[2'-(3'-chloro-2'-oxo-4'-substitutedaryl-1'-azetidinyl)-1',3'-thiazol-4'-yl] thio}benzothiazoles (4a-4e) and 2-{[(2'-(2'-substitutedaryl-4'-thiazolidinon-3'-yl)-1',3'-thiazol-4'-yl]thio}benzothiazoles (5a-5e) have been synthesized from 2-[(2'-substitutedarylidenylimino-1',3'-thiazol-4'-yl)thio]benzothiazoles (3a-3e). The structure of these compounds has been elucidated by elemental (C, H, N) and spectral (IR, (1)H-NMR, Mass) analysis. Furthermore, compounds 3a-3e, 4a-4e, and 5a-5e were screened for insecticidal activity against Periplaneta americana and antifungal, antibacterial activities in vitro against different strains of fungi and bacteria. Out of the fifteen compounds tested, compound 5b, 2-{[2'-(2'-p-hydroxy-m-methoxyphenyl)-4'-thiazolidinon-3'-yl)-1',3'-thiazol-4'-yl]thio}benzothiazole, was found to possess most prominent insecticidal activity.     

Juniperus oxycedrus L. subsp. oxycedrus and Juniperus oxycedrus L. subsp. macrocarpa (Sibth. & Sm.) Ball. “berries” from Turkey: Comparative evaluation of phenolic profile,antioxidant, cytotoxic and antimicrobial activities

This work aimed to evaluate and compare the phenolic profile and some biological properties of the ripe “berries” methanol extracts of Juniperus oxycedrus L. subsp. oxycedrus (Joo) and Juniperus oxycedrus L. subsp. macrocarpa (Sibth. & Sm.) Ball. (Jom) from Turkey. The total phenolic content resulted about 3-fold higher in Jom (17.89 ± 0.23 mg GAE/g extract) than in Joo (5.14 ± 0.06 mg GAE/g extract). The HPLC–DAD–ESI–MS analysis revealed a similar flavonoid fingerprint in Joo and Jom, whereas a difference in their quantitative content was found (4632 μg/g extract and 12644 μg/g extract). In addition, three phenolic acids were detected in Jom only (5765 μg/g extract), and protocatechuic acid was the most abundant one. The antioxidant capacity of the extracts was evaluated by different in vitro assays: in the DPPH and in the TBA tests a stronger activity in Jom was highlighted, while Joo exhibited higher reducing power and metal chelating activity. Joo and Jom did not affect HepG2 cell viability and both extracts resulted virtually non-toxic against Artemia salina. The extracts were also studied for their antimicrobial potential, displaying efficacy against Gram-positive bacteria.     

Antinociceptive,anti-inflammatory,and antioxidant properties of Phoradendron piperoides leaves

Phoradendron piperoides (Kunth) Trel. (Viscaceae) is a parasitic plant widely distributed in regions of the Brazilian northeast. Different species of Phoradendron are used in folk medicine for the treatment of cough, influenza, gastrointestinal and female disorders, and pain. In order to evaluate the actions of this plant, studies were performed on antinociceptive, anti-inflammatory, and antioxidant activities. The methanol extract (ME) and dichloromethane, ethyl acetate, and methanol partitions of P. piperoides leaves were used in the following experiments. Oral treatment with the ME elicited inhibitory activity (p?<?0.01) on the acetic acid effect at 100 (32.08%), 200 (34.46%), and 400?mg/kg (49.50%). P. piperoides ME reduced the formalin effect at the second phase (200 and 400?mg/kg, p?<?0.05); however, the ME did not elicit any inhibitory effect on the hot-plate test. Edema formation induced by carrageenan was reduced (p?<?0.05) with the ME by 28% (200?mg/kg) and 33% (400?mg/kg). ME, dichloromethane, ethyl acetate, and methanol partitions reacted with the DPPH radical and reduced the DPPH radical by 94.5, 37.2, 77.2, and 95.7%, respectively. ME, ethyl acetate, and methanol partitions exhibited low IC₅₀ values.     

Anti-inflammatory,Antinociceptive, and Neuropharmacological Activities of Clerodendron viscosum.

Abstract

The crude methanol extract of Clerodendron viscosum. Vent. (Verbenaceae) leaves was evaluated for its anti-inflammatory, antinociceptive, and neuropharmacological activities. When given orally to rats at doses of 200 and 400 mg/kg of body weight, the extract showed a significant (p < 0.001) anti-inflammatory activity against carrageenan-induced rat paw edema comparable with the standard drug phenylbutazone at the dose of 100 mg/kg of body weight. It also produced a significant writhing inhibition in acetic acid–induced writhing in mice at the oral dose of 250 and 500 mg/kg of body weight (p < 0.001), which was comparable with the standard drug diclofenac sodium at the dose of 25 mg/kg of body weight. Moreover, when given intraperitoneally to albino mice, it potentiated the pentobarbital-induced sleeping time (p < 0.001), decreased the open field score in open field test (p < 0.001), decreased the number of holes crossed from one chamber to the other in the hole-cross test (p < 0.001), and decreased the head dip responses in the hole-board test (p < 0.001) at the dose of 250 and 500 mg/kg of body weight. The overall results tend to suggest the anti-inflammatory, antinociceptive, and central nervous system depressant activities of the crude methanol extract of Clerodendron viscosum..     

Hemorrhagic activity of the Duvernoy''s gland secretion of the xenodontine colubrid Philodryas patagoniensis from the north-east region of Argentina

Colubrid snakes belonging to Philodryas genus, widespread all over South America, bring about lesions (swelling, ecchymosis, transient bleeding from the bite site punctures), that are similar to those produced by Bothrops species (yarará). In the present work we began the characterization of Philodryas patagoniensis venom. We examined if this venom produces hemorrhagic lesions as those observed in victims bitten by Philodryas olfersii. Hemorrhagic, proteolytic and fibrinogenolytic activities were evaluated, and histological observations in samples of gastrocnemius muscle were carried out. Inhibition studies were carried out in metal chelator (ethylenediaminetetraacetic acid) presence. Our results show a small Minimum Hemorrhagic Dose (MHD=0.035 μg) and a high proteolytic activity (143 U/mg), and prove the capacity of this venom to degrade fibrinogen in vitro rendering it unclottable by thrombin, supporting the presence of proteases, principally metalloproteases, in P. patagoniensis venom that are able to alterate the vascular wall and degrade fibrinogen, being both activities responsible of a high hemorrhagic activity.     

Structure-antibacterial,antitumor and hemolytic activity relationships of cecropin A-magainin 2 and cecropin A-melittin hybrid peptides

In order to elucidate the structure-antibiotic activity relationship of cecropin A-magainin 2 and cecropin A-melittin hybrid peptides, several truncated peptides and the analogues with amino acid substitutions were synthesized and their antibacterial, antitumor and hemolytic activities of were examined. Cecropin A-magainin 2 hybrid analog, L¹⁶-CA(1–8)-MA(1–12) (termed as L-CA-MA in this study: KWKLFKKIGIGKFLHLAKKF-NH₂), is known to have potent antibacterial and antitumor activity with less hemolytic activity. We found that the C-terminal region of L-CA-MA is more involved in the α-helical structure on cell membrane-like environment than N-terminal one by circular dichroism analysis. Deletion of the Gly-lle-Gly sequence, the central hinge region of L-CA-MA, produced a considerable reduction in antitumor and hemolytic activity rather than an antibacterial one. The insertion of Pro, Gly-lle or Gly-Pro in this hinge region of L-CA-MA caused retention of both antibacterial and antitumor activity while causing a significant decrease in hemolytic activity. However, the substitution with Gly-Pro-Gly instead of the Gly-lle-Gly in CA(1–8)-MA(1–12), CA(1–8)-ME(1–12), CA(1–13)-MA(1–13) and CA(1–13)-ME(1–13) hybrids resulted in a drastic decrease in antibacterial, antitumor and hemolytic activity. The increase of hydrophobicity at position 16 in CA(1–8)-MA(1–12) by substituting Trp or Phe induced a significant increase in hemolytic activity without a considerable change in either antibacterial or antitumor activity. Therefore, these results suggested that the appropriate flexibility in the hinge region of CA-MA and CA-ME hybrid peptides and the appropriate hydrophobicity at position 16 in the hydrophobic region of CA (1–8)-MA(1–12) are important in potent antibacterial and antitumor activity with no hemolytic effect.     

Antimicrobial activity of 5-arylidene aromatic derivatives of hydantoin. Part 2

Various 5-chloroarylidene-2-amino substituted derivatives of imidazoline-4-one were synthesized and evaluated for their activity in vitro against Mycobacterium tuberculosis and other type strains of bacteria and fungi. 2-Chloro- and 2,4-dichlorobenzylidene substituted hydantoins exhibited antimycobacterial effect. The most potent compounds 3i, 3j, 3o, 3q and 3s were classified for further tests. The antimitotic effect of the investigated hydantoins was also examined.     

Resveratrol isoforms and conjugates: A review from biosynthesis in plants to elimination from the human body

The natural isomers of resveratrol, cis- and trans-resveratrol, are natural phenolic substances synthetized via the shikimate pathway and found in many sources, including grapes, peanuts, blackberries, pistachios, cacao, cranberries, and jackfruits. They have functional and pharmacological properties such as anticarcinogenic, antidiabetic, anti-inflammatory, and cardioprotective activities. The aim of this article is to review the data published on resveratrol and its isomers, and their biosynthesis in plants, food sources, health and toxic effects, and the excretion of their metabolites. Due to its contribution to the promotion of human health, it is convenient to gather more knowledge about its functional properties, food sources, and the interactions with the human body during the processes of eating, digestion, absorption, biotransformation, and excretion, to combine this information to improve the understanding of these substances.