A New Inhibitor of Synovial Phospholipase A2 from Fermentations of Penicillium Sp. 62-92

1998 ◽  
Vol 53 (1-2) ◽  
pp. 60-64 ◽  
Author(s):  
Ludwig Witter ◽  
Timm Anke ◽  
Olov Sterner
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Cytotoxic Activities ◽  
Spectroscopic Methods ◽  
Submerged Cultures ◽  
Amide Bonds ◽  
Penicillium Sp ◽  
L1210 Cells ◽  
Hela S3 ◽  
Weak Antibacterial Activity

AbstractPenidiamide, a new tripetide containing dehydrotryptamine, glycine and anthranilic acid linked together by two amide bonds, and oxindole were isolated from submerged cultures of Penicillium sp. 62-92 . Both compounds preferentially inhibited human synovial phospholipase A2, penidiamide with an IC50 of 30 μᴍ and oxindole of 380 μᴍ. With the exception of U 937 cells (leukemia, human), no cytotoxic activities were detected against HL-60- (leukemia, human), HeLa S3- (epitheloid carcinoma, human), BHK 21- (kidney fibroblasts, hamster), and L1210-cells (leukemia, mouse). No antimicrobial activity was detected for oxindole, and only weak antibacterial activity for penidiamide. The structure of penidiamide was elucidated by spectroscopic methods.

Cytotoxic α-Pyrones from Xylaria hypoxylon

2007 ◽  
Vol 62 (3-4) ◽  
pp. 169-172 ◽  
Author(s):  
Anja Schüffler ◽  
Olov Sterner ◽  
Heidrun Anke
Keyword(s):  
Culture Fluid ◽  
Cytotoxic Activities ◽  
Spectroscopic Methods ◽  
Submerged Cultures

Abstract Two new α-pyrone derivatives, xylarone (1) and 8,9-dehydroxylarone (2) possessing cytotoxic activities, were isolated from the culture fluid of submerged cultures of the ascomycete Xylaria hypoxylon, strain A27-94. Their structures were elucidated by spectroscopic methods.

scholarly journals New Alkaloids and Polyketides from the Marine Sponge-Derived Fungus Penicillium sp. SCSIO41015

Marine Drugs ◽  
2019 ◽  
Vol 17 (7) ◽  
pp. 398 ◽  
Author(s):  
Xiaoyan Pang ◽  
Guodi Cai ◽  
Xiuping Lin ◽  
Limbadri Salendra ◽  
Xuefeng Zhou ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
2D Nmr ◽  
Specific Rotation ◽  
Human Gastric Cancer ◽  
X Ray Diffraction ◽  
Gastric Cancer Cells ◽  
Penicillium Sp ◽  
Ic50 Value ◽  
Rice Medium ◽  
Weak Antibacterial Activity

The sponge-derived fungus Penicillium sp. SCSIO41015 cultured on solid rice medium yielded twenty-one compounds (1–21), including two new alkaloids (1 and 2) and one new pyrone derivative (3). Their structures were elucidated by analysis of 1D/2D NMR data and HR–ESI–MS. Their absolute configurations were established by single-crystal X-ray diffraction analysis and comparison of the experimental with reported specific rotation values. Compound 16 exhibited selective cytotoxic activity against the human gastric cancer cells MGC803, with IC50 value of 5.19 μM. Compounds 9 and 18 showed weak antibacterial activity against Staphylococcus aureus and Acinetobacter baumannii, respectively, both with MIC values of 57 μg/mL. Furthermore, compound 16 displayed potent antibacterial activity against S. aureus with an MIC value of 3.75 μg/mL.

scholarly journals Phytoconstituents from Sidastrum micranthum (A. St.-Hil.) Fryxell (Malvaceae) and antimicrobial activity of pheophytin a

2015 ◽  
Vol 51 (4) ◽  
pp. 861-867 ◽  
Author(s):  
Roosevelt Albuquerque Gomes ◽  
Yanna Carolina Ferreira Teles ◽  
Fillipe de Oliveira Pereira ◽  
Luis Alberto de Sousa Rodrigues ◽  
Edeltrudes de Oliveira Lima ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Chemical Compounds ◽  
Structural Identification ◽  
2D Nmr ◽  
Spectroscopic Methods ◽  
Phytochemical Study ◽  
Pheophytin A ◽  
Chromatographic Techniques

abstract Sidastrum micranthum (A. St.-Hil.) Fryxell, a member of the Malvaceae family, is called malva preta in Brazil. As this species is commonly used to treat bronchitis, cough, and asthma, better knowledge of its chemical compounds is important. The phytochemical study of its hexane extract, using chromatographic techniques, led to isolation of six compounds: the triterpene isoarborinol, a mixture of sitosterol and stigmasterol, sitosterol-3-O-β-D-glucopyranoside, pheophytin a, and 132-hydroxy-(132-S)-pheophytin a. Structural identification of these compounds was carried out using spectroscopic methods such as IR and 1D and 2D NMR (HOMOCOSY, HMQC, HMBC, and NOESY). Compounds isolated from S. micranthum were screened for their in vitro antifungal and antibacterial activity against twenty fungal and bacterial standard strains. Pheophytin a exhibited antimicrobial action against all microorganisms tested.

Quinonoids from the barks of Cratoxylum formosum subsp.pruniflorum

2007 ◽  
Vol 85 (5) ◽  
pp. 341-345 ◽  
Author(s):  
Nawong Boonnak ◽  
Chatchanok Karalai ◽  
Suchada Chantrapromma ◽  
Chanita Ponglimanont ◽  
Akkharawit Kanjana-Opas ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Cytotoxic Activities ◽  
Spectroscopic Methods

A mixture of new bianthrones J (1a and 1b) was isolated from the barks of Cratoxylum formosum subsp. pruniflorum together with six known quinonoids, namely bianthrone A1 (2), vismones E (3) and D (4), 11-hydroxy-5-methoxy-2,2,9-trimethyl-2H-anthra[1,2-b]-pyran-7,12-dione (5), vismiaquinone (6), and 3-geranyloxy-6-methyl-1,8-dihydroxyanthraquinone (7). Their structures were assigned on the basis of spectroscopic methods. The antibacterial and cytotoxic activities of compounds 3 and 4 were also reported.Key words: Cratoxylum formosum subsp. pruniflorum, bianthrone, vismone, anthraquinone, antibacterial activity, cytotoxicity.

scholarly journals Synthesis and antimicrobial activity of azepine and thiepine derivatives

2015 ◽  
Vol 80 (7) ◽  
pp. 839-852 ◽  
Author(s):  
Nina Bozinovic ◽  
Irena Novakovic ◽  
Sladjana Kostic-Rajacic ◽  
Igor Opsenica ◽  
Bogdan Solaja
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Antibacterial And Antifungal Activity ◽  
In Vitro Antimicrobial Activity ◽  
Antibacterial And Antifungal ◽  
Weak Antibacterial Activity

A series of new 5H-pyridobenzazepine and pyridobenzothiepine derivatives was synthesized by Pd-catalyzed formation of C-N and C-S bonds. All synthesized compounds were tested for their in vitro antimicrobial activity. The 5H-pyridobenzazepine derivatives showed better antibacterial and antifungal activity than corresponding 5H-dipyridoazepine analogs. Among the synthesized azepines, derivative 8 displayed potent activity against tested bacteria (MIC = 39-78 ?g/mL), while azepine 12 showed promising antifungal activity (MIC = 156-313 ?g/mL). The synthesized thiepine derivatives exhibited weak antibacterial activity, but showed pronounced antifungal activity.

Complexes of Cu (II) with a-Ketoglutaric Acid and 1- (o-tolyl) Biguanide Synthesis, characterization and biological Activity

2019 ◽  
Vol 70 (10) ◽  
pp. 3603-3610
Author(s):  
Madalina Mihalache ◽  
Cornelia Guran ◽  
Aurelia Meghea ◽  
Vasile Bercu ◽  
Ludmila Motelica ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Biological Activity ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Copper Complexes ◽  
Substrate Adhesion ◽  
Inert Substrate

The three copper complexes having a-ketoglutaric acid (H2A) and 1- (o-tolyl) biguanide (TB) ligands have been synthesized and characterized. The proposed formulas for these complexes are: [Cu(TB)(HA)]Cl (C1), [Cu(TB)(HA)CH3COO]�H2O (C2) and [Cu(TB)(HA)](NO3) (C3) where HA represents deprotonated H2A. The complexes obtained were tested for antibacterial activity against Staphylococcus aureus ATCC 25923 and Pseudomonas aeruginosa ATCC 27853, antifungal activity on Candida albicans ATCC 10231 and antitumor activity on HeLa tumor cells. Due to the antitumor, antifungal, antimicrobial activity and inhibition of inert substrate adhesion, complexes synthesized could be used for potential therapeutic applications.

Design, Synthesis and Docking Studies of Some Novel Fluoroquinolone Compounds with Antibacterial Activity

2018 ◽  
Vol 69 (4) ◽  
pp. 815-822 ◽  
Author(s):  
Lucia Pintilie ◽  
Amalia Stefaniu ◽  
Alina Ioana Nicu ◽  
Maria Maganu ◽  
Miron Teodor Caproiu
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Molecular Docking ◽  
Drug Discovery ◽  
Elemental Analysis ◽  
Docking Studies ◽  
Receptor Protein ◽  
Chemical Methods ◽  
Design Synthesis ◽  
Gram Negative

A new series of fluoroquinolone compounds have been obtained by Gould-Jacobs method. The compounds have been characterized by physic-chemical methods (elemental analysis, FTIR, NMR, UV-Vis) and by antimicrobial activity against Gram-positive and Gram-negative microorganisms. For the synthesized compounds have been performed calculations of characteristics and molecular properties, using Spartan�14 Software from Wavefunction, Inc. Irvine, CA. and molecular docking studies using CLC Drug Discovery Workbench 2.4 software, to identify and visualize the most likely interaction ligand (fluoroquinolone) with the receptor protein.

Synthesis and Evaluation of Aromatic Surfactants as Potential Antibacterial and Cytotoxic Agents

2019 ◽  
Vol 16 (6) ◽  
pp. 478-484
Author(s):  
Kenia Barrantes ◽  
Mary Fuentes ◽  
Luz Chacón ◽  
Rosario Achí ◽  
Jorge Granados-Zuñiga ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Hela Cells ◽  
Cytotoxic Agents ◽  
Cytotoxic Activities ◽  
Hydroxybenzoic Acid ◽  
Derivatives Of

Two ether and one ester derivatives of the 4-nitro-3-hydroxybenzoic acid were synthesized and characterized. The in vitro antimicrobial and cytotoxic activities of the three novel compounds were also evaluated. The aromatic derivatives showed antibacterial activity against one of the four microorganisms tested and two compounds (C8 and NOBA) had a lower IC50 in HeLa cells.

Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihydroisoquinoline-2(1H)-yl)methyl) oxazol-5(4H)-one Derivatives Using 1,2,3,Tetrahydroisoquinoline and their Antimicrobial Activity

2020 ◽  
Vol 17 (5) ◽  
pp. 396-403
Author(s):  
Nalla Krishna Rao ◽  
Tentu Nageswara Rao ◽  
Botsa Parvatamma ◽  
Y. Prashanthi ◽  
Ravi Kumar Cheedarala
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Acetic Acid ◽  
Sodium Acetate ◽  
Good Activity ◽  
Activity Profile ◽  
Aryl Aldehydes ◽  
Chemical Structures ◽  
Novel Synthesis ◽  
Target Molecules

Aims: A series of six 4-benzylidene-2-((1-phenyl-3,4-dihydro isoquinoline-2(1H)-yl)methyloxazol- 5(4H)-one derivatives were synthesized by condensation of substituted aryl aldehydes with 2-(2-(1-phenyl-3,4- dihydro isoquinoline-2(1H)-acetamido)acetic acid in the presence of sodium acetate, acetic anhydride and zinc oxide as catalysts. Background: Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihy droisoquinoline-2(1H)-yl)methyl)oxazol- 5(4H)-one derivatives using 1,2,3,Tetrahydroisoquinoline and their antimicrobial activity. Objective: The title compounds can be synthesized from 1,2,3,4-tetrahydroisoquinoline. Methods: The target molecules, i.e., 4-benzylidene-2-((1-phenyl-3, 4-dihydro isoquinoline-2(1H)-yl) methyl) oxazol-5(4H)-one derivatives (8a-8f) have been synthesized from 1,2,3,4-tetrahydroisoquinoline which was prepared from benzoic acid in few steps. Results: All the six compounds were evaluated based on advanced spectral data (1H NMR, 13C NMR & LCMS), and the chemical structures of all compounds were determined by elemental analysis. Conclusion: Antibacterial activity of the derivatives was examined for the synthesized compounds and results indicate that compound with bromine substitution has a good activity profile.

scholarly journals Bioactive Ascochlorin Analogues from the Marine-Derived Fungus Stilbella fimetaria

Marine Drugs ◽  
2021 ◽  
Vol 19 (2) ◽  
pp. 46
Author(s):  
Karolina Subko ◽  
Sara Kildgaard ◽  
Francisca Vicente ◽  
Fernando Reyes ◽  
Olga Genilloud ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
2D Nmr ◽  
Bioactive Metabolites ◽  
Double Bonds ◽  
Relative Configuration ◽  
D 23 ◽  
Fungal Extracts

The marine-derived fungus Stilbella fimetaria is a chemically talented fungus producing several classes of bioactive metabolites, including meroterpenoids of the ascochlorin family. The targeted dereplication of fungal extracts by UHPLC-DAD-QTOF-MS revealed the presence of several new along with multiple known ascochlorin analogues (19–22). Their structures and relative configuration were characterized by 1D and 2D NMR. Further targeted dereplication based on a novel 1,4-benzoquinone sesquiterpene derivative, fimetarin A (22), resulted in the identification of three additional fimetarin analogues, fimetarins B–D (23–25), with their tentative structures proposed from detailed MS/HRMS analysis. In total, four new and eight known ascochlorin/fimetarin analogues were tested for their antimicrobial activity, identifying the analogues with a 5-chloroorcylaldehyde moiety to be more active than the benzoquinone analogue. Additionally, the presence of two conjugated double bonds at C-2′/C-3′ and C-4′/C-5′ were found to be essential for the observed antifungal activity, whereas the single, untailored bonds at C-4′/C-5′ and C-8′/C-9′ were suggested to be necessary for the observed antibacterial activity.

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