Phytochemical,Antiplasmodial, Cytotoxic and Antimicrobial Evaluation of a Southeast Brazilian Brown Propolis Produced by Apis mellifera Bees

Seven phenolic compounds (ferulic acid, caffeic acid, 4-methoxycinnamic acid, 3,4-dimethoxycinnamic acid, 3-hydroxy-4-methoxybenzaldehyde, 3-methoxy-4-hydroxypropiophenone and 1-O,2-O-digalloyl-6-O-trans-p-coumaroyl-β-D-glucopyranoside), a flavanonol (7-O-methylaromadendrin), two lignans (pinoresinol and matairesinol) and six diterpenic acids/alcohol (19-acetoxy-13-hydroxyabda-8(17),14-diene, totarol, 7-oxodehydroabietic acid, dehydroabietic acid, communic acid and isopimaric acid) were isolated from the hydroalcoholic extract of a Brazilian Brown Propolis and characterized by NMR spectral data analysis. The volatile fraction of brown propolis was characterized by CG-MS, composed mainly of monoterpenes and sesquiterpenes, being the major α-pinene (18.4 %) and β-pinene (10.3 %). This propolis chemical profile indicates that Pinus spp., Eucalyptus spp. and Araucaria angustifolia might be its primary plants source. The brown propolis displayed significant activity against Plasmodium falciparum D6 and W2 strains with IC₅₀ of 5.3 and 9.7 μg/mL, respectively. The volatile fraction was also active with IC₅₀ of 22.5 and 41.8 μg/mL, respectively. Among the compounds, 1-O,2-O-digalloyl-6-O-trans-p-coumaroyl-β-D-glucopyranoside showed IC₅₀ of 3.1 and 1.0 μg/mL against D6 and W2 strains, respectively, while communic acid showed an IC₅₀ of 4.0 μg/mL against W2 strain. Cytotoxicity was determined on four tumor cell lines (SK-MEL, KB, BT-549, and SK-OV-3) and two normal renal cell lines (LLC-PK1 and VERO). Matairesinol, 7-O-methylaromadendrin, and isopimaric acid showed an IC₅₀ range of 1.8–0.78 μg/mL, 7.3–100 μg/mL, and 17–18 μg/mL, respectively, against the tumor cell lines but they were not cytotoxic against normal cell lines. The crude extract of brown propolis displayed antimicrobial activity against C. neoformans, methicillin-resistant Staphylococcus aureus, and P. aeruginosa at 29.9 μg/mL, 178.9 μg/mL, and 160.7 μg/mL, respectively. The volatile fraction inhibited the growth of C. neoformans at 53.0 μg/mL. The compounds 3-hydroxy-4-methoxybenzaldehyde, 3-methoxy-4-hydroxypropiophenone and 7-oxodehydroabietic acid were active against C. neoformans, and caffeic and communic acids were active against methicillin-resistant Staphylococcus aureus.     

Evaluation of antioxidant and antiproliferative metabolites of <Emphasis Type="Italic">Penicillium flavigenum</Emphasis> isolated from hypersaline environment: Tuz (Salt) Lake by Xcelligence technology

The aim of the study is the determination of antioxidant and antiproliferative activities of fungal isolates’ metabolites belonging to Penicillium flavigenum isolated from Lake Tuz, Turkey. Evaluation of the antioxidant activity, the total phenolic content and antiproliferative effect were evaluated with DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging assay, Folin-ciocalteu method, Xcelligence real-time cell analysis. The total phenolic content of these isolates were found 62–82 mg/GAE. Ethyl acetate extracts from identified isolates, P. flavigenum, showed cytotoxic effects on A549, MCF7, Caco-2 cell lines. IC₅₀ values of P. flavigenum ethyl acetate extracts were found 96.7 μg/mL for A549, 33.4 μg/mL for MCF7, 43.4 μg/mL for Caco-2 and 97.3 μg/mL for 3T3. Phenolic acids in the extracts from P. flavigenum were identified with HPLC and GC-MS. Penicillium flavigenum is a new report for Turkey. According to these findings, fungi-related secondary metabolites are very important sources in terms of antioxidant and antiproliferative effects.     

Evaluation of in vitro alpha-glucosidase inhibitory,antimicrobial, and cytotoxic activities of secondary metabolites from the endophytic fungus,Nigrospora sphaerica,isolated from Helianthus annuus

This study aimed to evaluate alpha-glucosidase inhibition and antimicrobial activity as well as cytotoxic activity of extracts from the endophytic fungus, Nigrospora sp., isolated from leaves of Helianthus annuus, which is widely cultivated for food and used as a medicinal plant. The fungus (TSU-CS003) was identified based on internal transcribed spacer ribosomal DNA sequences and fungal biomass, and fermentation broth was subjected to extraction by solvents (hexane and ethyl acetate). All extracts were tested for their antimicrobial activity, alpha-glucosidase inhibition, and cytotoxicity activity. In addition, the active extract was analyzed by using gas chromatography mass spectrometry (GC-MS) TSU-CS003 was identified as Nigrospora sphaerica. The fermentation broth extract (BE) showed strong antimicrobial activity against Staphylococcus aureus and methicillin-resistant S. aureus (Gram-positive bacteria) with minimum inhibitory concentration (MIC) values in the range of 16–32 μg/mL and a few yeasts with MIC values ranging from 64 to 128 μg/mL, especially Talaromyces marneffei with an MIC value of 4 μg/mL. The effects of BE were observed by SEM. The results showed that this extract affected the cell morphology of T. marneffei. The half-maximal inhibitory concentration (IC50) of BE from alpha-glucosidase inhibition was recorded as 17.25 μg/mL and also showed significant cytotoxicity against A549 human cancer cell lines with an IC50 value of 22.41 μg/mL. Furthermore, BE was analyzed by using GC-MS and divided into three main compounds, including 5-pentyldihydrofuran-2(3H)-one, (Z)-methyl 4-(isobutyryloxy)but-3-enoate, and 2-phenylacetic acid. This was the first report of the endophytic fungus N. sphaerica from H. annuus. It is a potential source of active metabolites, which gave the strong antifungal activity, antioxidant activity, and cytotoxicity to A549 cancer cell lines.     

Isolation and evaluation of probiotic potential of lactic acid bacteria isolated from poultry intestine

The gut is a source of lactic acid bacteria with remarkable functional and technologies properties as well as a potential source of probiotics. In the present study, 13 strains of Lactobacillus were isolated from poultry intestine and identified according to their 16S rDNA sequences, as well as the evaluation of their probiotic potential. The probiotic properties were tested in aspects of antibiotic susceptibility, antimicrobial activity, exopolysaccharide production, lysozyme tolerance, gut condition tolerance (low pH, bile salt tolerance) and adhesion to human colorectal adenocarcinoma cell line (Caco-2). Most isolates were resistance to streptomycin (10 μg/mL), gentamicin (10 μg/mL), kanamycin (30 μg/mL), penicillin (10 μg/mL) and chloramphenicol (30 μg/mL). Isolates shows strong abilities to adhere to Caco-2 cell in the range of (76 to 85%). Isolates SHA101 to SHA113 showed high survival rate under gastrointestinal tract condition (>80%), indicating their potential in application of probiotics. The results of these tests indicate that the lactic acid bacteria isolated from poultry intestine have potential use as probiotic in various products.     

河南鼠尾草抑制体内外α-糖苷酶活性研究

本文采用96微孔板法,首次对河南鼠尾草抑制酵母和大鼠小肠α-葡萄糖苷酶活性进行研究。河南鼠尾草乙酸乙酯提取物(IC50=28.73μg/mL)和正丁醇提取物(IC50=73.90μg/mL)抑制酵母α-葡萄糖苷酶活性远高于阳性对照Acarbose(IC50=1081.27μg/mL),但只有乙酸乙酯提取物(IC50=366.79μg/mL)具有抑制大鼠小肠α-葡萄糖苷酶活性,阳性对照Acarbose未检测出其IC50。结果表明,河南鼠尾草乙酸乙酯提取物和正丁醇提取物均具有较好的酵母α-葡萄糖苷酶抑制活性,但只有乙酸乙酯提取物具有良好的大鼠小肠α-葡萄糖苷酶抑制活性。     

Synthesis and anticancer activity of 5'-chloromethylphosphonates of 3'-azido-3'-deoxythymidine (AZT)

A series of novel N-alkyl 5'-chloromethylphosphonates of 3'-azido-3'-deoxythymidine (6-15) was synthesized by means of phosphonylation of 3'-azido-3'-deoxythymidine (4) with P-chloromethylphosphonic ditriazolide (3) followed by a reaction with the appropriate amine. The synthesized phosphonamidates 6-15 were evaluated for their cytotoxic activity in two human cancer cell lines: oral (KB) and breast (MCF-7) using the sulforhodamine B (SRB) assay. The highest activity in KB human cancer cells was displayed by phosphonamidate 8 (IC(50)=5.8 μg/mL), however, this compound was less potent than the parent AZT (IC(50)=3.1 μg/mL). Phosphonamidate 10 showed only moderate activity (IC(50)=12.1 μg/mL) whereas the other phosphonamidates proved inactive. Similarly, the highest activity in MCF-7 human cancer cells was displayed by phosphonamidate 8 (IC(50)=3.7 μg/mL) but it proved somewhat less active than AZT (IC(50)=2.6 μg/mL). Some activity was also displayed by phosphonamidate 10 (IC(50)=12.8 μg/mL) but the other phosphonamidates were found inactive. Hydrolysis studies indicate that the synthesized phosphonamidates are likely to act as prodrugs of the parent nucleoside (AZT). Transport measurements showed that the most active phosphonamidates (8 and 10) were able to permeate across the intestinal epithelium in vitro. The apparent permeability coefficients determined in Caco-2 cell monolayers indicated that these compounds could be moderately absorbed in humans.     

凹叶厚朴抑制α-糖苷酶与抗氧化活性研究

首次采用96微孔板法检测贵州和河南产凹叶厚朴抑制α-葡萄糖苷酶活性;并采用DPPH、ABTS和FRAP三种方法测定其抗氧化活性.贵州产凹叶厚朴乙酸乙酯(IC50 =7.22 μg,/mL)和正丁醇提取部位(IC50=36.59 μg/mL),河南产凹叶厚朴石油醚(IC50=107.04 μg/mL)和乙酸乙酯提取部位(IC50=17.17μg/mL),它们的活性都远高于于阳性对照Acarhose( IC50=1081.27 μg/mL).贵州产凹叶厚朴乙酸乙酯提取部位清除ABTS自由基的能力最强(IC50=8.81 μg/mL),强于阳性对照BHT(IC50=11.94 μg/mL);其次为河南产凹叶厚朴乙酸乙酯提取部位(IC50=12.73 μg/mL).研究结果表明,贵州产凹叶厚朴乙酸乙酯提取部位抑制α-葡萄糖苷酶和抗氧化活性最好.     

Chemical Profile and Biological Activities of Fungal Strains Isolated from Piper nigrum Roots: Experimental and Computational Approaches

The current report describes the chemical investigation and biological activity of extracts produced by three fungal strains Fusarium oxysporum, Penicillium simplicissimum, and Fusarium proliferatum isolated from the roots of Piper nigrum L. growing in Vietnam. These fungi were namely determined by morphological and DNA analyses. GC/MS identification revealed that the EtOAc extracts of these fungi were associated with the presence of saturated and unsaturated fatty acids. These EtOAc extracts showed cytotoxicity towards cancer cell lines HepG2, inhibited various microbacterial organisms, especially fungus Aspergillus niger and yeast Candida albicans (the MIC values of 50–100 μg/mL). In α-glucosidase inhibitory assay, they induced the IC₅₀ values of 1.00-2.53 μg/mL were better than positive control acarbose (169.80 μg/mL). The EtOAc extract of F. oxysporum also showed strong anti-inflammatory activity against NO production and PGE-2 level. Four major compounds linoleic acid (37.346 %), oleic acid (27.520 %), palmitic acid (25.547 %), and stearic acid (7.030 %) from the EtOAc extract of F. oxysporum were selective in molecular docking study, by which linoleic and oleic acids showed higher binding affinity towards α-glucosidase than palmitic and stearic acids. In subsequent docking assay with inducible nitric oxide synthase (iNOS), palmitic acid, oleic acid and linoleic acid could be moderate inhibitors.     

黄连提取物对α-葡萄糖苷酶抑制作用研究

利用体外α-葡萄糖苷酶抑制模型对黄连不同部位提取物进行活性评价,并与阳性对照Acarbose比较,发现黄连不同部位均有一定的α-葡萄糖苷酶抑制活性.其中,黄连根茎乙酸乙酯提取物的抑制活性最高(IC_(50)=20.72 μg/mL),黄连种子石油醚部位(IC_(50)=40.86 μg/mL)和黄连叶石油醚部位(IC_(50)=62.85 μg/mL)的活性次之.3个部位的提取物活性均远大于阳性对照Acarbose(IC_(50)=1081,27 μg/mL).不同部位比较,根茎对α-葡萄糖苷酶抑制活性最好,这3种提取物抑制活性均比阳性对照高;同一部位不同提取物比较,石油醚和甲醇提取物α-葡萄糖苷酶抑制活性一般要高于乙酸乙酯提取物.     

Phytotoxic and antifungal metabolites from Curvularia sp. FH01 isolated from the gut of Atractomorpha sinensis

Two main phytotoxic and antifungal phthalic acid butyl isobutyl ester (1) and radicinin (2) were isolated from the culture of Curvularia sp. FH01, a fungus residing in the Atractomorpha sinensis gut. The structures of isolated metabolites were established on the basis of spectral analysis. Metabolites 1 and 2 exhibited significant phytotoxic activity against the radical growth of Echinochloa crusgalli with their IC(50) values of 61.9 and 5.9 μg/mL, respectively, which were comparable to that 2,4-dichlorophenoxyacetic acid (2.0 μg/mL) used as a positive control. The antifungal test results showed that compound 2 possessed strong antifungal activity against Magnaporthe grisea (IC(50)=16.3 μg/mL) and Valsa mali (IC(50)=18.2 μg/mL). The findings of the present study suggest that bioactive properties of the fungus FH01 can be attributed to its major components, phthalic acid butyl isobutyl ester and radicinin, and both agents have a potential to be used as herbicide and fungicide.     

Development of alternative medicinal sources from golden berry,bananas and carrot wastes as antioxidant,cytotoxic and antimicrobial agents

Discovering new medicinal sources from food wastes is a beneficial and valuable way instead of their disposal. Fruits and vegetables waste can be an inexpensive and readily available source of bioactive compounds to be used in pharmaceutical industries. The aim of this study is to highlight the in vitro antioxidant, cytotoxic, and antimicrobial activities of the total extracts of banana peels (Musa acuminate), carrot peels (Daucus carota) and golden berry husk (Physalis peruviana) besides evaluating their in vivo acute and chronic toxicity profiles as well as their antimutagenic activity. Also, we investigated their phenolic and flavonoid contents spectrophotometrically and by HPLC. Results showed that D. carota peels revealed the highest antioxidant activity (29.903 mg TE/g) using DPPH free radical scavenging assay. Cytotoxic outcomes (SulphoRhodamine-B method) showed that the highest cytotoxic activity of M. acuminate peels (IC₅₀: 20.7 μg/mL) was exerted on HEPG2 cell line, where D. carota peels (IC₅₀: 18.8 μg/mL) showed the highest cytotoxic activity on PC-3 cell line. In addition, pH. peruviana husk (IC₅₀: 10.5 ± 1.0 μg/mL) showed a potent cytotoxic activity on HCT-116 that is non-significant from the standard Doxorubicin (IC₅₀: 11.5 ± 0.8 μg/mL). For the antimicrobial activity (agar diffusion assay), most of the total extracts revealed notable activities against all tested pathogens relative to the standards; ciprofloxacin and ketoconazole, specially Ph. peruviana husk that showed a potent inhibitory activity (inhibition zone diameter of 29 mm.) against C. albicans even more than the standard ketoconazole (inhibition zone diameter of 28 mm.). These promising biological activities are mainly related to the high content of flavonoids and phenolic compounds identified and quantified in their total extracts. Moreover, the three extracts proved their in vivo safety on the short and long terms as well as their possible antimutagenic effect on the genotoxicity of the drug cyclophosphamide (CP) in both bone marrow cells and spermatocyte cells.     

肉桂抑制α-葡萄糖苷酶活性成分研究

为寻找肉桂中具有抑制α-葡萄糖苷酶活性的化学成分,采用高效液相色谱结合体外抑制α-葡萄糖苷酶活性筛选模型的方法,进行活性成分的跟踪分离,并对活性化合物进行酶抑制动力学研究.结果显示,肉桂石油醚提取物(IC50=350.37 μg/mL)的活性明显高于阳性对照阿卡波糖(IC50=1028.99 μg/mL),从中分离出2个活性成分,分别鉴定为桂皮醛( IC50 =277.89 μg/mL)和肉桂酸(IC50=286.22 μg/mL).酶抑制动力学结果表明它们对α-葡萄糖苷酶的抑制类型均为非竞争性抑制,Ki值分别为178.07 μg/mL和229.43 μg/mL.     

LC/MS/MS Phenolic Profile,Antioxidant Capacity,Angiotensin-Converting Enzyme (ACE) and Glutathione S Transferase (GST) Inhibitory Properties of Ultrasound-Assisted Propolis Extracts

Resinous beehive product propolis has many biological activities. It contains various aromatic substances that have great differences in their chemical composition depending on the natural flora. Thus, chemical characterization and biological properties of propolis samples is an important subject for the pharmaceutical industry. In this study, the propolis samples collected from three cities in Turkey were prepared as methanol (MEP), ethanol (EEP), chloroform (ChlEP), hexane (HxEP), and ethyl acetate (EAEP) extracts using an ultrasonic assisted technique. The antioxidant capacities of the samples were evaluated by free radical scavenging activity (DPPH), cation radical scavenging activity (ABTS), and reducing activity (CUPRAC) and (FRAP). The strongest biological activities were detected in ethanol and methanol extracts. Enzyme inhibition of the propolis samples were determined against the human glutathione S-transferase (GST) and angiotensin converting enzyme (ACE). IC₅₀ values of MEP1, MEP2, and MEP3 samples against the ACE were found as 13.9 μg/mL, 14.8 μg/mL, and 12.8 μg/mL, while against the GST IC₅₀ values of MEP1, MEP2, and MEP3 samples were as 5.92 μg/mL, 9.49 μg/mL, and 5.72 μg/mL. To know the possible causes of the biological test results advanced LC/MS/MS method was applied. trans-ferulic acid, kaempferol, and chrysin were found as the most abundant phenolic compounds in each sample. The propolis extracts obtained using the proper solvent have a good potential to be used in pharmaceuticals to treat the diseases related to oxidative damage, hypertension, and inflammation. Finally, the interactions between chrysin, trans-ferulic acid and kaempferol molecules with ACE and GST receptors were analyzed using molecular docking study. Selected molecules interact with active residues by binding to the active site of the receptors.     

细叶卷柏提取物的体外抗肿瘤活性

利用MTT法检测细叶卷柏乙酸乙酯和正丁醇提取物对HeLa细胞生长的抑制作用,利用流式细胞术(FCM)比较不同提取物对细胞凋亡的影响。结果显示:细叶卷柏的乙酸乙酯和正丁醇部位抑制细胞生长和诱导细胞凋亡作用均有明显的剂量依赖性。乙酸乙酯部位的IC50值为1.927μg/mL,正丁醇部位的IC50值为24.600μg/mL。因此,细叶卷柏乙酸乙酯部位的体外抗肿瘤活性相对较强,其次是其正丁醇部位,水提部位相对较弱。细叶卷柏是一种潜在的抗肿瘤药用植物。     

Phytochemical Profiling,Antimicrobial, Antiproliferative and Apoptotic Effects of Stemodia viscosa Roxb. of Western Ghats Region,India

The present study shows the chemical profile, antimicrobial, antiproliferative, and apoptotic effects of Stemodia viscosa extracts. Thirteen bioactive compounds were identified in the 80 % ethanolic extract by GC/MS analysis. The acetone extract exhibited a higher content of flavonoids and phenols of 805.10 μg QE/mg DW and 89.31 μg GAE/mg DW extracts, respectively. Furthermore, the acetone extract possessed the highest antioxidant activity (IC₅₀=9.96 μg/mL). The 80 % ethanolic extract exhibited significant antimicrobial activity; the highest activity was observed against Staphylococcus aureus with a zone of inhibition of 25±0.51 mm, MIC value of 4 mg/mL, and MBC value of 8 mg/mL. The antiproliferative results revealed the presence of anticancer activity with an IC₅₀=91.562 and 74.362 μg/mL against the B16F10 skin and COLO205 colon cancer cells, respectively. The flow cytometric analysis shows that the plant extracts cause cancer cell death through the induction of apoptosis. Our findings confirmed that Stemodia viscosa is a potential source of biologically active compounds.     

Actinidia arguta Pulp: Phytochemical Composition,Radical Scavenging Activity,and in Vitro Cells Effects

Hardy kiwifruit (Actinidia arguta) is a highly appreciated exotic fruit endowed with outstanding bioactive compounds. The present work proposes to characterize the pulp from A. arguta organic fruits, emphasizing its radicals scavenging capacity and effects on intestinal cells (Caco-2 and HT29-MTX). The physicochemical properties and phenolic profile were also screened. The total phenolic and flavonoid contents (TPC and TFC, respectively) of pulp were 12.21 mg GAE/g on dry weight (DW) and 5.92 mg CE/g DW, respectively. A high antioxidant activity was observed (FRAP: 151.41 μmol FSE/g DW; DPPH: 12.17 mg TE/g DW). Furthermore, the pulp did not induce a toxic effect on Caco-2 and HT29-MTX cells viability up to 1000 μg/mL. Regarding in vitro scavenging capacity, the pulp revealed the highest scavenging power against NO^. (IC₅₀=3.45 μg/mL) and HOCl (IC₅₀=12.77 μg/mL). These results emphasize the richness of A. arguta fruit pulp to be used in different food products.     

In vitro anthelmintic effect of Melia azedarach L. and Trichilia claussenii C. against sheep gastrointestinal nematodes

The control of parasitic diseases in small ruminants is mainly done with the use of synthetic anthelmintics. However, incorrect and indiscriminate use of these products has caused the emergence of parasite resistance. Plants with anthelmintic activity are used in folk veterinary medicine, but it is necessary to investigate and scientifically validate low-cost phytotherapeutic alternatives for future use to control gastrointestinal nematodes in small ruminants by family farmers. Thus, the aim of this study was to evaluate the in vitro anthelmintic effect of plant extracts from Melia azedarach and Trichilia claussenii by the egg hatch test (EHT) and larval development test (LDT) against sheep gastrointestinal nematodes. The hexane extract of M. azedarach fruits was extracted through cold percolation and the methanol extract of T. claussenii leaves was obtained by extraction at room temperature in solvents in order of increasing polarity. The efficacy results were analyzed using the Probit program of SAS. The M. azedarach extract showed a LC(50) of 572.2 μg/mL and LC(99) of 1137.8 μg/mL in the EHT, and LC(50) of 0.7 μg/mL and LC(99) of 60.8 μg/mL in the LDT. In turn, the T. claussenii extract presented a LC(50) of 263.8 μg/mL and LC(99) of 522.5 μg/mL in the EHT and LC(50) of 1.1 μg/mL and LC(99) of 26.4 μg/mL in the LDT. Comparing the extracts of the species from the Meliaceae family, T. claussenii showed greater anti-parasite potential in vitro than M. azedarach. However, studies on the isolated compounds, toxicity and administration forms to animals are also needed to validate low-cost alternative herbal remedies for use to control gastrointestinal nematodes by family farmers.     

Applications of red pigments from psychrophilic Rhodonellum psychrophilum GL8 in health,food and antimicrobial finishes on textiles

A psychrophilic bacterium (named GL8) producing red pigments was isolated from the high altitude Pangong Tso Lake located in Leh Ladakh, India. Based on 16S rDNA sequencing amplicon of 1370 bp, the psychrophilic bacterium was identified as Rhodonellum psychrophilum (R. psychrophilum GL8) and deposited in Gen Bank under accession no. MH031708.1.The red colored pigments from R. psychrophilum GL8 showed antimicrobial activity against E. coli, S. aureus, C. albicans, (MTCC 277, ATCC 90028) and S. cerevisiae (H1086) with minimum inhibitory concentrations from 31.25 μg/mL to 500 μg/mL. Red colored pigments also showed synergistic antifungal activity when combined with fluconazole and amphotericin B against C. albicans (MTCC 277 and ATCC 90028) and S. cerevisiae; vancomycin and erythromycin against E. coli and S. aureus. The red pigments showed antioxidant activity with an IC₅₀ of 13.159 μg/mL, LC–MS/MS analysis demonstrated that red pigment extracts contained a mixture of 2-methyl-3-butyl-prodigine, Prodigiosin, 2-methyl-3hexyl-prodigine, 3, 4-Didehydrorhodopsin, anhydrorhodovibrin, alloxanthin and Tetradecanoyl-hexadecanoyl compounds. Red pigment extracts were used to develop antimicrobial fabrics and did not show any cytotoxicity to U87MG human glioblastoma cell line, but showed a marginal growth inhibition to A172 human glioblastoma cell lines. In contrast, the red pigment extracts showed significant growth stimulation on L929 mouse fibroblast cell lines.     

五种苦苣苔科植物α-葡萄糖苷酶抑制活性研究

利用体外α-葡萄糖苷酶抑制模型对5种苦苣苔科植物进行活性评价,并与阳性对照Acarbose进行比较,发现5种植物不同部位均有一定的α-葡萄糖苷酶抑制活性。其中,牛耳岩白菜石油醚部位的抑制活性最高(IC50=26.19μg/mL,活性均远大于阳性对照Acarbose(IC50=1081.27μg/mL)。不同植物比较,牛耳岩白菜的α-葡萄糖苷酶抑制活性最好,其3种不同溶剂提取物与Acarbose相比均有很高抑制活性;对牛耳岩白菜提取物的α-葡萄糖苷酶抑制动力学研究结果表明,石油醚和乙酸乙酯提取物对α-葡萄糖苷酶抑制作用属于非竞争性抑制类型,Ki值分别为4.24和40.04μg/mL。正丁醇提取物则属于竞争性抑制类型(Ki=205.48μg/mL)     

<Emphasis Type="Italic">In vitro</Emphasis> leishmanicidal,antibacterial and antitumour potential of anhydrocochlioquinone A obtained from the fungus <Emphasis Type="Italic">Cochliobolus</Emphasis> sp.

The bioassay-guided fractionation of the ethyl acetate extract of the fungus Cochliobolus sp. highlighted leishmanicidal activity and allowed for anhydrocochlioquinone A (ANDC-A) isolation. MS, 1D and 2D NMR spectra of this compound were in agreement with those published in the literature. ANDC-A exhibited leishmanicidal activity with EC₅₀ value of 22.4 µg/mL (44 μM) and, when submitted to the microdilution assay against Gram-positive and Gram-negative bacteria, showed a minimal inhibitory concentration against Staphylococcus aureus ATCC 25295 of 128 μg/mL (248.7 μM). It was also active against five human cancer cell lines, showing IC₅₀ values from 5.4 to 20.3 μM. ANDC-A demonstrated a differential selectivity for HL-60 (SI 5.5) and THP-1 (SI 4.3) cell lines in comparison with Vero cells and was more selective than cisplatin and doxorubicin against MCF-7 cell line in comparison with human peripheral blood mononuclear cells. ANDC-A was able to eradicate clonogenic tumour cells at concentrations of 20 and 50 μM and induced apoptosis in all tumour cell lines at 20 μM. These results suggest that ANDC-A might be used as a biochemical tool in the study of tumour cells biochemistry as well as an anticancer agent with durable effects on tumours.