scholarly journals Bioactivities by a crude extract from the GreenlandicPseudomonassp. In5 involves the nonribosomal peptides, nunamycin and nunapeptin

PeerJ ◽  
2015 ◽  
Vol 3 ◽  
pp. e1476 ◽  
Author(s):  
Charlotte F. Michelsen ◽  
Helle Jensen ◽  
Vincent J. Venditto ◽  
Rosanna C. Hennessy ◽  
Peter Stougaard

Background.Bioactive microbial metabolites provide a successful source of novel compounds with pharmaceutical potentials. The bacteriumPseudomonassp. In5 is a biocontrol strain isolated from a plant disease suppressive soil in Greenland, which produces two antimicrobial nonribosomal peptides (NRPs), nunapeptin and nunamycin.Methods.In this study, we usedin vitroantimicrobial and anticancer bioassays to evaluate the potential bioactivities of both a crude extract derived fromPseudomonassp. In5 and NRPs purified from the crude extract.Results.We verified that the crude extract derived fromPseudomonassp. In5 showed suppressive activity against the basidiomyceteRhizoctonia solaniby inducing a mitochondrial stress-response. Furthermore, we confirmed suppressive activity against the oomycetePythium aphanidermatumby thePseudomonassp. In5 crude extract, and that the purified nunamycin and nunapeptin displayed distinct antimicrobial activities. In addition to the antimicrobial activity, we found that treatment of the cancer cell lines, Jurkat T-cells, Granta cells, and melanoma cells, with thePseudomonassp. In5 crude extract increased staining with the apoptotic marker Annexin V while no staining of healthy normal cells, i.e., naïve or activated CD4 T-cells, was observed. Treatment with either of the NRPs alone did not increase Annexin V staining of the Jurkat T-cells, despite individually showing robust antimicrobial activity, whereas an anticancer activity was detected when nunamycin and nunapeptin were used in combination.Discussion.Our results suggest that the bioactivity of a crude extract derived fromPseudomonassp. In5 involves the presence of both nunamycin and nunapeptin and highlight the possibility of synergy between multiple microbial metabolites.

1996 ◽  
Vol 317 (2) ◽  
pp. 343-346 ◽  
Author(s):  
Jiamin QU ◽  
Louise A. CONROY ◽  
John H. WALKER ◽  
F. B. Peter WOODING ◽  
Jack A. LUCY

Phosphatidylserine was exposed on the surface of human umbilical endothelial cells (ECV304) a few minutes after adding thrombin in vitro, as monitored by prothrombinase assays with and without annexin V. Jurkat T cells adhered to the thrombin-treated cells. The adhesion was inhibited by annexin V, indicating that it was mediated by exposed phosphatidylserine on the endothelial cells.


2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Larissa M. Magnibou ◽  
Peron B. Leutcha ◽  
Billy T. Tchegnitegni ◽  
Steven C. N. Wouamba ◽  
Cyrille Y. F. F. Magne ◽  
...  

Abstract Entada abyssinica Steud. Ex A. Rich (Leguminosae) is a medicinal plant used traditionally for the treatment of infections. A phytochemical investigation of the methanol extract of E. abyssinica root bark led to the isolation of a new phenanthrene derivative named phenentada (1), together with seven known compounds (8 S, 13 E)-kolavic acid 15-methyl ester (2) and 8 S-kolavic acid 15-methyl ester (3) obtained as mixture, 8 S-kolavic acid 15-methyl ester (3), 8 S-kolavic acid 18-methyl ester (4), 13,14,15,16-tetranorclerod-3-ene-12,18-dioic acid (5), 1′,26′-bis-[(S)-2,3-dihydroxypropyl] hexacosanedioate (6), campesterol (7) and 3-O-β -d-glucopyranosylstigmasterol (8). Their structures were determined by NMR spectroscopy (1D and 2D), mass spectrometry (HRESIMS) and by comparison with previously reported data. The crude extract and some isolated compounds were evaluated for their in vitro antimicrobial activities by the microdilution method while, the antioxidant activity was evaluated by the DPPH methods. Regarding the antimicrobial activity, the crude extract showed significant inhibitory activities against bacteria strains (MIC 7.81–31.3 μg mL−1) and yeasts (MIC 15.6–31.3 μg mL−1) whereas all compounds tested exhibited significant activity against Staphylococcus epidermidis. Moreover, compounds 4, 5 and 6 and the mixture 2/3 showed significant antimicrobial activity on Candida parapsilosis strain (MIC = 3.12 μg mL−1), as well as selected antifungal property against candida pathogenic fungi strains. On the other hand, compounds (1) demonstrated the best bioactivities against Candida albicans and Salmonella enterica with MIC = 3.12 μg mL−1 while the mixture 2/3 appeared to have the highest inhibition on gram (+) bacteria strain S. epidermidis with MIC of 0.78 μg mL−1 and compound 5 (MIC = 1.56 μg mL−1) against the gram (−) bacteria strain. Furthermore, the SC50 values measured by the antioxidant test for all samples varied between 47.21 and 52.44 μg mL−1 for DPPH. These results support the traditional uses of E. abyssinica in the management of several diseases including the claim in the skin disease treatment. Additionally, here is reported the first time isolation of a phenanthrene derivative in the Fabaceae family to the best of our knowledge.


2019 ◽  
Vol 15 (1) ◽  
pp. 63-70
Author(s):  
Shiv Dev Singh ◽  
Arvind Kumar ◽  
Firoz Babar ◽  
Neetu Sachan ◽  
Arun Kumar Sharma

Background: Thienopyrimidines are the bioisoster of quinazoline and unlike quinazoline exist in three isomeric forms corresponding to the three possible types annulation of thiophene to the pyrimidine ring viz thieno[2,3-d] pyrimidine, thieno[3,2-d] pyrimidine and thieno[3,4-d]pyrimidine. Heterocyclic containing the thienopyrimidinone moiety exhibits various pronounced activities such as anti-hypertensive, analgesic and anti-inflammatory, antiviral, platelet aggregation inhibitory, antiprotozoal bronchodilatory, phosphodiesterase inhibitory, antihistaminic, antipsychotic and antimicrobial activity. Objective: Synthesis of novel 3(N,N-dialkylamino)alkyl/phenyl substituted thieno[2,3-d]pyrimidinones as H1-anti-histaminic and antimicrobial agents. Methods: A series of 3-[(N,N-dialkylamino)alkyl/phenyl]-2-(1H)thioxo-5,6,7,8-tetrahydrobenzo(b) thieno(2,3-d)pyrimidine-4(3H)-ones[4a-d], their oxo analogous [5a-d] and 3-[(N,N-dialkylamino)alkyl]- 2-chlorophenyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d)pyrimidine- 4 (3H)-ones[6a-d]derivative were synthesized from 2-amino-4,5,6,7-tetrahydrobenzo(b)thiophene-3-carboxylic acid by nucleophilic substitution of different N,N-dialkyl alkylene/phenylene diamines on activated 3-acylchloride moiety followed by cyclocondensation with carbon disulfide and ethanolic potassium hydroxide to get [4a-d] and in second reaction by condensation with 4-chlorobenzoyl chloride to get [6a-d] by single pot novel innovative route. The oxo analogous [5a-d] were prepared by treating derivatives [4a-d] with potassium permagnate in ethanolic KOH. The synthesized compound were evaluated for H1-antihistaminic and antimicrobial activities. Results: All synthesized compounds exhibited significant H1-antihistaminic activity by in vitro and in vivo screening methods and data were verified analytically and statistically. The compound 4a, 4b, 5a and 5b showed significant H1-antihistaminiic activity than the reference standard chlorpheniramine maleate. The compound 6d, 6c, 5c and 4c exhibited significant antimicrobial activity.


Materials ◽  
2021 ◽  
Vol 14 (13) ◽  
pp. 3693
Author(s):  
Yurii P. Sharkeev ◽  
Ekaterina G. Komarova ◽  
Valentina V. Chebodaeva ◽  
Mariya B. Sedelnikova ◽  
Aleksandr M. Zakharenko ◽  
...  

A modern trend in traumatology, orthopedics, and implantology is the development of materials and coatings with an amorphous–crystalline structure that exhibits excellent biocopatibility. The structure and physico–chemical and biological properties of calcium phosphate (CaP) coatings deposited on Ti plates using the micro-arc oxidation (MAO) method under different voltages (200, 250, and 300 V) were studied. Amorphous, nanocrystalline, and microcrystalline statesof CaHPO4 and β-Ca2P2O7were observed in the coatings using TEM and XRD. The increase in MAO voltage resulted in augmentation of the surface roughness Ra from 2.5 to 6.5 µm, mass from 10 to 25 mg, thickness from 50 to 105 µm, and Ca/P ratio from 0.3 to 0.6. The electrical potential (EP) of the CaP coatings changed from −456 to −535 mV, while the zeta potential (ZP) decreased from −53 to −40 mV following an increase in the values of the MAO voltage. Numerous correlations of physical and chemical indices of CaP coatings were estimated. A decrease in the ZP magnitudes of CaP coatings deposited at 200–250 V was strongly associated with elevated hTERT expression in tumor-derived Jurkat T cells preliminarily activated with anti-CD2/CD3/CD28 antibodies and then contacted in vitro with CaP-coated samples for 14 days. In turn, in vitro survival of CD4+ subsets was enhanced, with proinflammatory cytokine secretion of activated Jurkat T cells. Thus, the applied MAO voltage allowed the regulation of the physicochemical properties of amorphous–crystalline CaP-coatings on Ti substrates to a certain extent. This method may be used as a technological mechanism to trigger the behavior of cells through contact with micro-arc CaP coatings. The possible role of negative ZP and Ca2+ as effectors of the biological effects of amorphous–crystalline CaP coatings is discussed. Micro-arc CaP coatings should be carefully tested to determine their suitability for use in patients with chronic lymphoid malignancies.


Author(s):  
Nektarios Moraitis ◽  
Maria Christopoulou ◽  
Konstantina S. Nikita ◽  
Georgia-Persephoni Voulgaridou ◽  
Ioannis Anestopoulos ◽  
...  

Plants ◽  
2020 ◽  
Vol 9 (4) ◽  
pp. 453 ◽  
Author(s):  
Nhan Trong Le ◽  
Duc Viet Ho ◽  
Tuan Quoc Doan ◽  
Anh Tuan Le ◽  
Ain Raal ◽  
...  

The present study aimed to determine the antimicrobial activity and chemical composition of leaves-extracted essential oil of Leoheo domatiophorus Chaowasku, D.T. Ngo and H.T. Le (L. domatiophorus), including antibacterial, antimycotic, antitrichomonas and antiviral effects. The essential oil was obtained using hydrodistillation, with an average yield of 0.34 ± 0.01% (v/w, dry leaves). There were 52 constituents as identified by GC/MS with available authentic standards, representing 96.74% of the entire leaves oil. The essential oil was comprised of three main components, namely viridiflorene (16.47%), (-)-δ-cadinene (15.58%) and γ-muurolene (8.00%). The oil showed good antimicrobial activities against several species: Gram-positive strains: Staphylococcus aureus (two strains) and Enterococcus faecalis, with Minimum Inhibitory Concentration (MIC) and Minimum Lethal Concentration (MLC) values from 0.25 to 1% (v/v); Gram-negative strains such as Escherichia coli (two strains), Pseudomonas aeruginosa (two strains) and Klebsiella pneumoniae, with MIC and MLC values between 2% and 8% (v/v); and finally Candida species, having MIC and MLC between 0.12 and 4% (v/v).Antitrichomonas activity of the oil was also undertaken, showing IC50, IC90 and MLC values of 0.008%, 0.016% and 0.03% (v/v), respectively, after 48h of incubation. The essential oil resultedin being completely ineffective against tested viruses, ssRNA+ (HIV-1, YFV, BVDV, Sb-1, CV-B4), ssRNA- (hRSVA2, VSV), dsRNA (Reo-1), and dsDNA (HSV-1, VV) viruses with EC50 values over 100 µg/mL. This is the first, yet comprehensive, scientific report about the chemical composition and pharmacological properties of the essential oil in L. domatiophorus.


2012 ◽  
Vol 10 (2) ◽  
pp. 131-135 ◽  
Author(s):  
Tanjina Hoque ◽  
Md Al Amin Sikder ◽  
Mohammad A Kaisar ◽  
Abu Asad Chowdhury ◽  
Mohammad A Rashid

Two Bangladeshi medicinal plants from Araceae family, Alocasia indica and Steudnera virosa, have been investigated for their in vitro thrombolytic, membrane stabilizing antimicrobial activities and generalized    toxicity. The total phenolic content was also determined and expressed in gallic acid equivalent. The membrane stabilizing activity was assessed by heat and hypotonic solution induced methods. The carbon tetrachloride soluble  fraction (CTCSF) of A. indica and aqueous soluble fraction (AQSF) of S. virosa demonstrated strong membrane stabilizing activity. Different extractives of A. indica and S. virosa showed moderate thrombolytic activity. Among the two plants, the methanoic crude extract and its chloroform soluble partitionate of S. virosa revealed moderate inhibition of microbial growth. In brine shrimp lethality bioassay, the pet-ether and carbon tetrachloride soluble fractions of A. indica and the crude extract and its pet-ether soluble fraction of S. virosa were found to be as lethal as    Vincristine sulphate after 24 hours observation on shrimp nauplii.   DOI: http://dx.doi.org/10.3329/dujps.v10i2.11794   Dhaka Univ. J. Pharm. Sci. 10(2): 131-135, 2011(December)  


2013 ◽  
Vol 68 (5-6) ◽  
pp. 191-197 ◽  
Author(s):  
Birkan Açıkgöz ◽  
İskender Karaltı ◽  
Melike Ersöz ◽  
Zeynep M. Coşkun ◽  
Gülşah Çobanoğlu ◽  
...  

The present study explores the antimicrobial activity and cytotoxic effects in culture assays of two fruticose soil lichens, Cladonia rangiformis Hoffm. and Cladonia convoluta (Lamkey) Cout., to contribute to possible pharmacological uses of lichens. In vitro antimicrobial activities of methanol and chloroform extracts against two Gram-negative bacteria (Pseudomonas aeruginosa and Escherichia coli), two Gram-positive bacteria (Enterococcus faecalis and Staphylococcus aureus), and the yeast Candida albicans were examined using the paper disc method and through determination of minimal inhibitory concentrations (MICs). The data showed the presence of antibiotic substances in the chloroform and the methanol extracts of the lichen species. The chloroform extracts exhibited more signifi cant antimicrobial activity than the methanol extracts. However, a higher antifungal activity was noted in the methanol extract of C. rangiformis. The maximum antimicrobial activity was recorded for the chloroform extract of C. convoluta against E. coli. The cytotoxic effects of the lichen extracts on human breast cancer MCF-7 cells were evaluated by the trypan blue assay yielding IC50 values of ca. 173 and 167 μg/ml for the extracts from C. rangiformis and C. convoluta, respectively.


2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Ana Carolina Oliveira Silva ◽  
Elidiane Fonseca Santana ◽  
Antonio Marcos Saraiva ◽  
Felipe Neves Coutinho ◽  
Ricardo Henrique Acre Castro ◽  
...  

The development of the present study was based on selections using random, direct ethnopharmacological, and indirect ethnopharmacological approaches, aiming to evaluate which method is the best for bioprospecting new antimicrobial plant drugs. A crude extract of 53 species of herbaceous plants collected in the semiarid region of Northeast Brazil was tested against 11 microorganisms. Well-agar diffusion and minimum inhibitory concentration (MIC) techniques were used. Ten extracts from direct, six from random, and three from indirect ethnopharmacological selections exhibited activities that ranged from weak to very active against the organisms tested. The strain most susceptible to the evaluated extracts wasStaphylococcus aureus. The MIC analysis revealed the best result for the direct ethnopharmacological approach, considering that some species yielded extracts classified as active or moderately active (MICs between 250 and 1000 µg/mL). Furthermore, one species from this approach inhibited the growth of the threeCandidastrains. Thus, it was concluded that the direct ethnopharmacological approach is the most effective when selecting species for bioprospecting new plant drugs with antimicrobial activities.


2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Suganthi Appalasamy ◽  
Kiah Yann Lo ◽  
Song Jin Ch'ng ◽  
Ku Nornadia ◽  
Ahmad Sofiman Othman ◽  
...  

Artemisia annuaL., a medicinal herb, produces secondary metabolites with antimicrobial property. In Malaysia due to the tropical hot climate,A. annuacould not be planted for production of artemisinin, the main bioactive compound. In this study, the leaves of threein vitro A. annuaL. clones were, extracted and two bioactive compounds, artemisinin and a precursor, were isolated by thin layer chromatography. These compounds were found to be effective in inhibiting the growth of Gram-positive and Gram-negative bacteria but notCandida albicans. Their antimicrobial activity was similar to that of antibactericidal antibiotic streptomycin. They were found to inhibit the growth of the tested microbes at the minimum inhibition concentration of 0.09 mg/mL, and toxicity test using brine shrimp showed that even the low concentration of 0.09 mg/mL was very lethal towards the brine shrimps with 100% mortality rate. This study hence indicated thatin vitrocultured plantlets ofA. annuacan be used as the alternative method for production of artemisinin and its precursor with antimicrobial activities.


Sign in / Sign up

Export Citation Format

Share Document