川乌植物内生真菌抗菌活性的研究

从川乌（Radix aconiti）植物的根和茎中分离获得内生真菌61株,经显微形态观察进行内生真菌的分类鉴定,同时采用纸片法进行抗菌活性筛选。结果有29株内生真菌显示抗菌活性,占菌株数的47．54％;毛壳菌属是抗菌活性菌株的优势种属;活性高且抗菌谱广的菌株有3株,主要分布在毛壳菌属和束丝菌属。结果表明：川乌植物内生真菌中广泛分布着有抗菌活性的菌株。     

抗水稻白叶枯病菌植物内生真菌的筛选、鉴定

从多种植物叶片内分离、纯化出31株植物内生真菌,活性筛选表明分离自健康水稻叶片内生真菌Bo-1菌的乙酸乙酯粗提物对水稻白叶枯病菌具有较强的抑菌活性。当供试浓度为100μg/mL时,Bo-1菌乙酸乙酯粗提物对水稻白叶枯病菌抑菌圈为22.4 mm,与同浓度的氯霉素对水稻白叶枯病菌的抑菌效果相当。通过形态学特征观察和ITS rDNA测序分析,Bo-1菌被鉴定为淡色生赤壳菌(Bionectria ochroleuca)。抗菌谱实验表明,Bo-1菌对多种细菌类病原体具有较强的拮抗能力。     

七子花内生真菌的抗菌活性筛选及其活性先导化合物的发现

【目的】从濒危植物七子花中分离出具有抗植物致病菌活性的内生真菌,并在其代谢产物中寻找具有抗菌活性的先导化合物。【方法】采用生长速率法测定内生真菌对植物病原菌的抑制活性。通过形态学和5.8S rRNA序列法对具有较好抗菌活性的内生真菌进行鉴定。运用多种色谱方法对发酵产物进行分离、纯化,利用质谱和核磁共振谱分析鉴定出化合物的结构。【结果】茄交链孢QZH 10对水稻纹枯病菌和苹果树腐烂病菌的抑制活性较好,抑制率分别为89.1%和67.9%。在供试浓度为100μg/m L时,QZH 10乙酸乙酯粗提物对稻瘟病菌具有强烈的抑制效果,抑制率为100.0%。从QZH 10中分离到2个单体化合物并分别被鉴定为altersolanol A和6-O-methylalaternin。在供试浓度为100μg/m L时,altersolanol A对稻瘟病菌具有较强的抑制效果,抑制率大于85%;6-O-methylalaternin对苹果树腐烂病菌具有强烈的抑制效果,抑制率为100.0%。【结论】当前结果表明Altersolanol A和6-O-methylalaternin具有开发成微生物源杀菌剂的潜力。     

内生芬芳镰刀菌Dzf2中两个抗菌活性成分(英文)

采用活性追踪的方法从盾叶薯蓣内生芬芳镰刀菌Dzf2中分离到两个抗菌活性成分,通过物理化学性质和波谱学特征鉴定为镰刀菌酸(1)和9,10-脱氢镰刀菌酸(2)。采用多孔板-MTT-比色法和孢子萌发法测定了化合物的抗菌活性。镰刀菌酸和9,10-脱氢镰刀菌酸对供试细菌的半抑制浓度(IC50)值为35.35μg/mL至171.29μg/mL;对稻瘟菌孢子萌发的IC50值分别为28.83μg/mL和27.06μg/mL。     

球毛壳菌H6次级代谢产物及其α-葡萄糖苷酶抑制活性

采用体外α-葡萄糖苷酶抑制模型对一株球毛壳菌H6的发酵液和菌丝体两种乙酸乙酯提取物进行活性评价,结果表明,发酵液乙酸乙酯提取物对α-葡萄糖苷酶具有较强的抑制活性,其IC₅₀值为(510.76±23.46)μg/mL。采用硅胶、Sephadex LH-20、半制备高效液相等色谱技术从其发酵液乙酸乙酯提取物中分离得到12个化合物。通过各种光谱分析,依次鉴定为chaetoviridins A-B(1-2),chaetoglobosins A-D(3-6),chaetoglobosin J(7),chaetoglobosin Q(8),prochaetogobosinsⅠ-Ⅲ(9-11),vibratilicin(12),其中化合物12为首次从毛壳属中分离得到。对化合物进行α-葡萄糖苷酶抑制活性测定发现,化合物12显示弱的抑制活性,其IC₅₀为(1 182.75±19.14)μg/mL。     

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。     

白木香内生真菌的分离鉴定及其抑菌活性

从白木香Aquilaria sinensis（Lour．）Gilg木质部的树脂形成部位和健康部位中共分离获得42株内生真菌,经初步鉴定,产孢的33株分属于3目4科7属,其余未产孢的9株暂归为无孢菌群。采用杯碟法和MTT法分别测定了各菌株的发酵上清液对3种病原菌的体外抑菌活性和2种肿瘤细胞的体外细胞毒活性。结果表明,白木香木质部健康部位内生真菌以枝顶孢霉属为优势属,而树脂形成部位的内生真菌种类比健康部位要多,且以青霉属为优势属。其中26株至少能抑制一种指示菌,占总数的61．9％;7株对指示瘤株具有细胞毒活性,占总数的16．7％。抑菌活性菌株主要分布在枝顶孢霉属和青霉属。枝顶孢霉属菌株抑菌活性较强,其抗菌活性成分值得进一步研究。     

艾纳香内生真菌粉红粘帚霉抗菌次生代谢产物

植物内生真菌一直是发现结构新颖、活性广泛的化合物的重要宝库。文中对一株艾纳香内生真菌粉红粘帚霉Clonostachysrosea进行化学研究,通过活性跟踪手段,结合硅胶柱色谱、凝胶色谱、以及半制备液相色谱技术从该菌株的发酵提取物中共分离获得6个单体化合物,经波谱学技术结合质谱鉴定其分别为verticillin A (1)、(S)-(+)-fusarinolic acid (2)、8-hydroxyfusaric acid (3)、cerebroside C (4)、3-Maleimide-5-oxime (5)以及bionectriol A(6)。所有化合物进行了体外抗大肠埃希菌、金黄色葡萄球菌、枯草芽孢杆菌以及铜绿假单胞菌4株细菌的活性评价,其中1、4和6对3株细菌表现出显著的抑菌活性,MIC值2–16μg/mL。研究结果为从黎药植物艾纳香的内生真菌中寻找新型抗生素提供重要参考。     

基于超高效液相色谱-电喷雾-质谱、天然产物词典和活性筛选的艾纳香内生真菌次生代谢产物

【背景】植物内生真菌是天然活性小分子的重要来源,但由于种类繁多,导致寻找结构新颖、活性强的化合物非常困难,重复分离已成为制约新型药源小分子发掘的瓶颈。【目的】综合各种技术,快速寻找目标活性次生代谢产物。【方法】通过对菌株分子鉴定、天然产物词典(dictionaryofnatural products,DNP)数据库检索、超高效液相色谱-电喷雾-质谱(ultraperformanceliquidchromatographyquadrupole time-of-flight mass spectrometry,UPLC-QTof-MS)分析、滤纸片法抑菌实验和色谱技术跟踪获得活性单体化合物。运用质谱和单晶衍射技术对化合物结构进行鉴定,96孔板法对单体化合物进行活性评价。【结果】分离鉴定出11株艾纳香内生真菌,筛选出一株各方面表现良好的艾纳香内生菌菌株Diaporthe sp.,从其大米培养基中获得一个单体化合物Cytochalasin H,活性评价显示其对枯草芽孢杆菌具有很好的抑制活性,MIC值为32μg/mL。【结论】将多种筛选技术相结合的方法应用于艾纳香内生真菌活性代谢产物的发掘,为快速寻找活性先导化合物提供了很好的借鉴。     

川芎内生真菌Cladosporium sp.次级代谢产物及抗菌活性研究

为了增加川芎用途,本研究从川芎中分离鉴别出了一株内生真菌Cladosporium sp. IS384,并首次对其次级代谢产物进行研究。用硅胶柱层析、制备薄层层析和重结晶等方法,从该菌发酵液的乙酸乙酯萃取相中首次分离获得4个单体化合物,运用现代波谱技术以及文献数据对照,鉴定其结构分别为cladospolide B(1),iso-cla-dospolide B(2),麦角甾醇(3),水苏碱(4)。对提取部位及单体化合物进行抗菌实验,发现乙酸乙酯部位对粪链球菌ATCC 29212的MIC值达到3. 91μg/mL,化合物1对ATCC 29212的MIC为0. 31μg/mL,化合物2对ATCC12228的MIC值为0. 63μg/mL。本文通过对川芎内生真菌的研究发现了具有一定抗菌活性的物质,为后续川芎内生真菌研究提供很好的理论依据。     

毛筒壳科真菌次级代谢产物生物活性的评价

毛筒壳科Tubeufiaceae真菌具有产新结构、新活性次级代谢产物的潜力,目前对该科真菌次级代谢产物的研究较少。为了寻找具有生物活性的新化合物,有必要对毛筒壳科真菌次级代谢产物及其活性进行系统深入的研究。本文采用平板对峙法、生长速率法和MTT法,分别测定已分离得到的19株该科真菌活体菌株抑菌活性、发酵物抑菌活性以及发酵物粗提物对不同人体肿瘤细胞株增殖的抑制作用。通过平板对峙法,试验共筛选获得13株活性菌株,其中,红棕毛筒腔菌菌株Tubeufia rubra PF02-2对7种植物病原真菌有明显的抑菌效果,抑制率均高于60%且抑菌谱广。采用生长速率法,发现红棕毛筒腔菌菌株PF02-2经液体发酵后,发酵液对其中4种植物病原真菌仍有一定的抑制作用,且菌丝体部分的乙酸乙酯提取物对马铃薯早疫病病菌Alternaria solani（ZYB）的抑制效果最好。通过MTT法,发现发酵物粗提物对3种肿瘤细胞均具有不同程度的细胞毒活性,其中在300μg/mL时,剑叶莎毛筒腔菌菌株Tubeufia machaerinae ML03-2发酵液部分的乙酸乙酯提取物对人宫颈癌细胞株HeLa和人前列腺癌细胞株PC-3的抑制率（%）分别达到了98.92±0.15和97.86±0.18,在400μg/mL时,对人肝癌细胞株HEPG2的抑制率（%）达到了98.88±0.04;在500μg/mL时,明孢新旋卷孢菌菌株Neohelicosporium hyalosporum ML05-1菌丝体部分的乙酸乙酯提取物对人宫颈癌细胞株HeLa细胞的抑制率（%）为98.32±0.02,在600μg/mL时,对人肝癌细胞株HEPG2的抑制率（%）达到了97.62±0.20,在300μg/mL时,对人前列腺癌细胞株PC-3的抑制率（%）达到了98.91±0.02。该研究结果为开发利用毛筒壳科真菌提供了科学依据。     

灵芝子实体中不同极性的三萜体外抗肿瘤及抗炎活性比较

为了解灵芝中不同极性三萜活性的差异,运用大孔树脂将灵芝总三萜根据极性大小进行分段,采用高效液相法分析各极性部分的HPLC指纹图谱和三萜含量,并比较其对不同肿瘤细胞增殖的抑制作用和抗炎活性。结果显示D-101大孔树脂可以有效地将灵芝总三萜分为中等极性和低极性两部分,两部分的三萜含量分别为(279.00±2.90)mg/g、(94.52±2.03)mg/g。其中,低极性三萜的体外抗肿瘤活性明显强于中等极性三萜,其对K562、SW620、L1210细胞增殖抑制的IC₅₀值分别为(74.12±1.94)μg/mL、(121.45±2.13)μg/mL、(13.52±1.13)μg/mL。另外,低极性三萜对RAW264.7细胞呼吸爆发的抑制作用也明显强于中等极性三萜。进一步对低极性三萜和中等极性三萜单体的抗炎活性进行比较,发现低极性三萜灵芝烯酸F、灵芝酸DM、灵芝醇B对RAW264.7细胞呼吸爆发的抑制作用明显强于极性较高的灵芝酸C₂、灵芝酸A。该研究阐明了灵芝子实体中不同极性三萜部位的抗肿瘤及抗炎活性并不相同,为将来新药开发和灵芝质量标准的改进建立了基础。     

Synthesis, characterization and in vitro biological evaluation of some novel diarylsulfonylureas as potential cytotoxic and antimicrobial agents

A series of novel diarylsulfonylureas (1-28) have been synthesized and characterized by FTIR, (1)H NMR, (13)C NMR and LC mass spectral analysis. All the synthesized compounds were evaluated for their in vitro cytotoxicity and antimicrobial activities. Among the tested compounds for cytotoxicity using Brine Shrimp Lethality assay, compounds 18 and 22 exhibited significant cytotoxicity at ED(50) values 3.96±0.21 and 4.02±0.19μg/mL, respectively. This level of activity was found comparable to that of the reference drug podophyllotoxin with ED(50) value 3.61±0.17μg/mL and it could be a remarkable starting point to develop new lead molecules with major cytotoxicity. Antimicrobial activity was screened using agar well diffusion assay method against selected Gram-positive, Gram-negative and fungal strains. Most of the compounds showed promising antibacterial and antifungal activity and the activity expressed as the minimum inhibitory concentration (MIC) in μg/mL.     

Synthesis,biological evaluations and computational studies of N-(3-(-2-(7-Chloroquinolin-2-yl)vinyl) benzylidene)anilines as fungal biofilm inhibitors

In the present investigation, new chloroquinoline derivatives bearing vinyl benzylidene aniline substituents at 2nd position were synthesized and screed for biofilm inhibitory, antifungal and antibacterial activity. The result of biofilm inhibition of C. albicans suggested that compounds 5j (IC₅₀ value?=?51.2?μM) and 5a (IC₅₀ value?=?66.2?μM) possess promising antibiofilm inhibition when compared with the standard antifungal drug fluconazole (IC₅₀?=?40.0?μM). Two compounds 5a (MIC?=?94.2?μg/mL) and 5f (MIC?=?98.8?μg/mL) also exhibited good antifungal activity comparable to standard drug fluconazole (MIC?=?50.0?μg/mL). The antibacterial screening against four strains of bacteria viz. E. coli, P. aeruginosa, B. subtilis, and S. aureus suggested their potential antibacterial activity and especially all the compounds except 5g were found more active than the standard drug ciprofloxacin against B. subtilis. To further gain insights into the possible mechanism of these compounds in biofilm inhibition through the agglutinin like protein (Als), molecular docking and molecular dynamics simulation studies were carried out. Molecular modeling studies suggested the clear role in inhibition of this protein and the resulting biofilm inhibitory activity.     

Cytotoxic,antimicrobial activities,AChE and BChE inhibitory effects of compounds from Tanacetum chiliophyllum (Fisch. & Mey.) Schultz Bip. var. oligocephalum (D.C.) Sosn. and T. chiliophyllum (Fisch. & Mey.) Schultz Bip. var. monocephalum Grierson

Tanacetum L. species traditionally used for insecticidal purposes as well as in folk medicine for their antitumor, antimicrobial, antifungal activities. In our previous study a novel sesquiterpene lactone and triterpene lactone together with 12 known flavonoids, coumarin and a triterpene were isolated from T. chiliophyllum var. oligocephalum and T. chiliophyllum var. monocephalum extracts which have insecticidal and antimicrobial activity. In this study, cytotoxic, antimicrobial activities and acetylcholinesterase (AChE), butyrylcholinesterase (BChE) inhibitory effects of pure compounds isolated from these plants were investigated. The tested compounds showed AChE and BChE inhibition which ranged between 7.20–80.37% and 9.19%–76.99% respectively. The highest AChE and BChE inhibition was observed for ulubelenolide which afforded 80.37% and 76.99% inhibition respectively. The cytotoxic effect of the compounds ranged between 22.34–49.77 μg/mL IC₅₀ values. Highest cytotoxic activity was observed against MCF-7 and HEK 293 cell line by 5–hydroxy-3′,4′,7-trimethoxy flavone and 5-hydroxy-3′,4′,6,7-tetramethoxyflavone that produced 25.80 ± 0.17 and 22.34 ± 0.70 IC₅₀ values respectively. Compounds eupatilin, cirsilineol, 5–hydroxy-3′,4′,7-trimethoxy flavone and ulubelenolide showed significant antimicrobial effect on C. albicans with 7.8 μg/mL MIC. The new compound ulubelenolide afforded high AChE and BChE inhibition as well as high antifungal activity. In our opinion activity of this substance should be evaluated further against other fungal species.     

Exploring antifungal activities of acetone extract of selected Indian medicinal plants against human dermal fungal pathogens

A broad spectrum of medicinal plants was used as traditional remedies for various infectious diseases. Fungal infectious diseases have a significant impact on public health. Fungi cause more prevalent infections in immunocompromised individuals mainly patients undergoing transplantation related therapies, and malignant cancer treatments. The present study aimed to investigate the in vitro antifungal effects of the traditional medicinal plants used in India against the fungal pathogens associated with dermal infections. Indian medicinal plants (Acalypha indica, Lawsonia inermis Allium sativum and Citrus limon) extract (acetone/crude) were tested for their antifungal effects against five fungal species isolated from skin scrapings of fungal infected patients were identified as including Alternaria spp., Curvularia spp., Fusarium spp., Trichophyton spp. and Geotrichum spp. using well diffusion test and the broth micro dilution method. All plant extracts have shown to have antifungal efficacy against dermal pathogens. Particularly, Allium sativum extract revealed a strong antifungal effect against all fungal isolates with the minimum fungicidal concentration (MFC) of 50–100 μg/mL. Strong antifungal activity against Curvularia spp., Trichophyton spp., and Geotrichum spp. was also observed for the extracts of Acalypha indica, and Lawsonia inermis with MFCs of 50–800 μg/mL respectively. The extracts of Citrus limon showed an effective antifungal activity against most of the fungal strains tested with the MFCs of 50–800 μg/mL. Our research demonstrated the strong evidence of conventional plants extracts against clinical fungal pathogens with the most promising option of employing natural-drugs for the treatment of skin infections. Furthermore, in-depth analysis of identifying the compounds responsible for the antifungal activity that could offer alternatives way to develop new natural antifungal therapeutics for combating resistant recurrent infections.     

白柄肉齿菌Sarcodon leucopus多酚生物碱提取物的体外抗氧化及降血糖活性

为探讨西藏白柄肉齿菌Sarcodon leucopus子实体多酚生物碱提取物（PAE）的抗氧化和降糖活性,本研究考察了PAE对DPPH自由基清除能力、细胞内抗氧化能力（CAA）和糖尿病关键酶（大鼠小肠来源麦芽糖酶、蔗糖酶和α-淀粉酶）活性的抑制能力。结果表明,PAE具有一定的抗氧化活性,对DPPH自由基的半数抑制浓度（IC₅₀）为(18.12±1.09)μg/mL,对细胞内抗氧化能力表现为CAA₅₀=(13.60±0.13)μg/mL;PAE对糖尿病关键酶的抑制活性有一定选择性,对麦芽糖酶和蔗糖酶具有抑制作用,并呈剂量效应关系,其IC₅₀分别(60.86±4.50)μg/mL和(64.60±4.53)μg/mL,而对α-淀粉酶抑制作用极低。研究结果表明PAE有潜在的抗氧化及降血糖活性,具有开发为安全高效的天然降血糖功能食品和药物的潜力。     

A new isoflavonol and other constituents from Cameroonian propolis and evaluation of their anti-inflammatory,antifungal and antioxidant potential

Propolis is rich in diverse bioactive compounds. Propolis samples were collected from three localities of Cameroon and used in the study. Column chromatography separation of propolis MeOH:DCM (50:50) extracts yielded a new isoflavonol, 2-hydroxy-8-prenylbiochanin A (1) alongside 2′,3′-dihydroxypropyltetraeicosanoate (2) and triacontyl p-coumarate (3) isolated from propolis for first time together with seven compounds: β-amyrine (4), oleanolic acid (5), β-amyrine acetate (6), lupeol (7), betulinic acid (8), lupeol acetate (9) and lupenone (10). These compounds were tested for their inhibitory effect on oxidative burst where intracellular reactive oxygen species (ROS) were produced from zymosan stimulated human whole blood phagocytes and on production of nitric oxide (NO) from lipopolysaccharide (LPS) stimulated J774.2 mouse macrophages. The cytotoxicity of these compounds was evaluated on NIH-3 T3 normal mouse fibroblast cells, antiradical potential on 2,2-diphenyl-1-picrylhydrazylhydrazyl (DPPH·) as well as their anti-yeast potential on four selected candida species. Compound 1 showed higher NO inhibition (IC₅₀ = 23.3 ± 0.3 µg/mL) than standard compound L-NMMA (IC₅₀ = 24.2 ± 0.8 µg/mL). Higher ROS inhibition was shown by compounds 6 (IC₅₀ = 4.3 ± 0.3 µg/mL) and 9 (IC₅₀ = 1.1 ± 0.1 µg/mL) than Ibuprofen (IC₅₀ = 11.2 ± 1.9 µg/mL). Furthermore, compound 1 displayed moderate level of cytotoxicity on NIH-3 T3 cells, with IC₅₀ = 5.8 ± 0.3 µg/mL compared to the cyclohexamide IC₅₀ = 0.13 ± 0.02 µg/mL. Compound 3 showed lower antifungal activity on Candida krusei and Candida glabrata, MIC of 125 μg/mL on each strain compared to 50 μg/mL for fuconazole. The extracts showed low antifungal activities ranging from 250 to 500 μg/mL on C. albicans, C. krusei and C. glabrata and the values of MIC on Candida parapsilosis were 500 μg/mL and above. DPPH* scavenging activity was exhibited by compounds 1 (IC₅₀ = 15.653 ± 0.335 μg/mL) and 3 (IC₅₀ = 89.077 ± 24.875 μg/mL) compared to Vitamin C (IC₅₀ = 3.343 ± 0.271 μg/mL) while extracts showed moderate antiradical activities with IC₅₀ values ranging from 309.31 ± 2.465 to 635.52 ± 11.05 µg/mL. These results indicate that compounds 1, 6 and 9 are potent anti-inflammatory drug candidates while 1 and 3 could be potent antioxidant drugs.     

Antimalarial halorosellinic acid from the marine fungus Halorosellinia oceanica.

Three known compounds, 2-hexylidene-3-methylsuccinic acid (1), cytochalasin Q (2), and 5-carboxymellein (3), together with two new derivatives, 2-hexylidene-3-methylsuccinic acid 4-methyl ester (4) and an ophiobolane sesterterpene named halorosellinic acid (5), were isolated from culture broth of the marine fungus Halorosellinia oceanica BCC 5149. Compounds 1-3 exhibited moderate cytotoxicity against KB and BC-1 cell lines with IC(50) values of 1-13 microg/mL, while compounds 2, 3, 5, and 6 showed antimalarial activity with respective IC(50) values of 17, 4, 13, and 19 microg/mL. Halorosellinic acid (5) possessed only weak antimycobacterial activity with the minimum inhibitory concentration of 200 microg/mL.