Identification of Cytotoxic Constituents ofNarthecium ossifragumUsing Bioassay-Guided Fractionation

2007 ◽  
Vol 55 (15) ◽  
pp. 6018-6026 ◽  
Author(s):  
Silvio Uhlig ◽  
Helene Wisløff ◽  
Dirk Petersen
Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
A Derksen ◽  
J Sendker ◽  
W Hafezi ◽  
C Nauert ◽  
J Kühn ◽  
...  

Author(s):  
Kolathuru Puttamadaiah Ramesha ◽  
Nagabhushana Chandra Mohana ◽  
Bettadapura Rameshgowda Nuthan ◽  
Devaraju Rakshith ◽  
Sreedharamurthy Satish

Abstract Background Endophyte bestows beneficial aspects to its inhabiting host, along with a contribution to diverse structural attributes with biological potential. In this regard, antimicrobial profiling of fungal endophytes from medicinal plant Adiantum philippense revealed bioactive Nigrospora sphaerica from the leaf segment. Chemical and biological profiling through TLC–bioautography and hyphenated spectroscopic techniques confirmed the presence of phomalactone as an antimicrobial metabolite. Results The chemical investigation of the broth extract by bioassay-guided fractionation confirmed phomalactone as a bioactive antimicrobial secondary metabolite. The antimicrobial activity of phomalactone was found to be highest against Escherichia coli by disc diffusion assay. The MIC was found to be significant against both Escherichia coli and Xanthomonas campestris in the case of bacteria and dermatophyte Candida albicans at 150 μg/ml, respectively. Conclusions Overall, the results highlighted the antimicrobial potential of phomalactone from the endophyte Nigrospora sphaerica exhibiting a broad spectrum of antimicrobial activity against human and phytopathogenic bacteria and fungi. This work is the first report regarding the antibacterial activity of phomalactone.


Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1094
Author(s):  
Melissa M. Cadelis ◽  
Soeren Geese ◽  
Benedict B. Uy ◽  
Daniel R. Mulholland ◽  
Shara J. van de Pas ◽  
...  

Antimicrobial bioassay-guided fractionation of the endophytic fungi Neofusicoccum australe led to the isolation of a new unsymmetrical naphthoquinone dimer, neofusnaphthoquinone B (1), along with four known natural products (2–5). Structure elucidation was conducted by nuclear magnetic resonance (NMR) spectroscopic methods, and the antimicrobial activity of all the natural products was investigated, revealing 1 to be moderately active towards methicillin-resistant Staphylococcus aureus (MRSA) with a minimum inhibitory concentration (MIC) of 16 µg/mL.


2007 ◽  
Vol 21 (11) ◽  
pp. 982-989 ◽  
Author(s):  
Xiaoxue Zhang ◽  
Feng Han ◽  
Ping Gao ◽  
Dong Yu ◽  
Shigui Liu

2014 ◽  
Vol 49 (2) ◽  
pp. 88-94 ◽  
Author(s):  
Emmanuelle Rodrigues Araújo ◽  
Wolfgang Harand ◽  
Iwanne Coelho Lima ◽  
Fernanda Carolina Ribeiro Dias ◽  
Adelmo Adriane Duarte de Santana ◽  
...  

O objetivo deste trabalho foi avaliar o efeito de extratos de capeba (Piper marginatum) e nim (Azadirachta indica) sobre o fungo Colletotrichum scovillei e determinar o componente mais ativo no controle pós-colheita da antracnose em pimentão. A atividade de extratos metanólicos das folhas (P.marginatum e A. indica) e das sementes (A. indica) a 0, 125, 250, 500, 1.000 e 2.000 ppm, na inibição do crescimento micelial de C. scovillei in vitro foram avaliadas. O extrato metanólico de folhas de P.marginatum foi o mais ativo e, consequentemente, foi submetido ao fracionamento biomonitorado ("bioassay-guided fractionation"). Esse processo rendeu 10 frações majoritárias, obtidas por cromatografia líquida de alta performance, das quais a fração à concentração de 1,5 ppm inibiu o desenvolvimento de C. scovillei de forma mais eficiente do que o fungicida mancozeb.


Molecules ◽  
2018 ◽  
Vol 24 (1) ◽  
pp. 8 ◽  
Author(s):  
Mayra Antúnez-Mojica ◽  
Andrés Rojas-Sepúlveda ◽  
Mario Mendieta-Serrano ◽  
Leticia Gonzalez-Maya ◽  
Silvia Marquina ◽  
...  

By using a zebrafish embryo model to guide the chromatographic fractionation of antimitotic secondary metabolites, seven podophyllotoxin-type lignans were isolated from a hydroalcoholic extract obtained from the steam bark of Bursera fagaroides. The compounds were identified as podophyllotoxin (1), β-peltatin-A-methylether (2), 5′-desmethoxy-β-peltatin-A-methylether (3), desmethoxy-yatein (4), desoxypodophyllotoxin (5), burseranin (6), and acetyl podophyllotoxin (7). The biological effects on mitosis, cell migration, and microtubule cytoskeleton remodeling of lignans 1–7 were further evaluated in zebrafish embryos by whole-mount immunolocalization of the mitotic marker phospho-histone H3 and by a tubulin antibody. We found that lignans 1, 2, 4, and 7 induced mitotic arrest, delayed cell migration, and disrupted the microtubule cytoskeleton in zebrafish embryos. Furthermore, microtubule cytoskeleton destabilization was observed also in PC3 cells, except for 7. Therefore, these results demonstrate that the cytotoxic activity of 1, 2, and 4 is mediated by their microtubule-destabilizing activity. In general, the in vivo and in vitro models here used displayed equivalent mitotic effects, which allows us to conclude that the zebrafish model can be a fast and cheap in vivo model that can be used to identify antimitotic natural products through bioassay-guided fractionation.


2019 ◽  
Vol 14 (1) ◽  
pp. 1934578X1901400 ◽  
Author(s):  
Yelkaira Vásquez ◽  
Jianping Zhao ◽  
Shabana I. Khan ◽  
Mahabir P. Gupta ◽  
Ikhlas A. Khan

This study is focused on the isolation and characterization of bioactive secondary metabolites from the ethanolic extract of stems of the Panamanian plant Talisia nervosa Radlk, through a series of target-based cellular assays related to the metabolic syndrome (MetS): a combination of type 2 Diabetes Mellitus (T2DM), hypercholesterolemia, inflammation, and obesity. Bioassay guided fractionation allowed the isolation of four known compounds: (-)-catechin (1), methyl gallate (2), ethyl gallate (3), and ß-D-glucopyranose,1,4,6-tris(3,4,5-trihydroxybenzoate) (4). This is the first report of (-)-catechin (1) and ß-D-glucopyranose,1,4,6-tris (3,4,5-trihydroxybenzoate) (4) from T. nervosa. Among the isolates, 1 activated PPARγ, but had no effect on PPARα. Compounds 2 -4 activated PPARα, PPARγ and LXR. Interestingly, 2 was stronger than 3 towards all three targets. Methyl gallate (2) showed the most potent effect toward both PPARα and PPARγ with an increase of 3.0 and 13-fold, respectively, while 4 was most potent in activating LXR with a fold induction of 5.3 at concentrations of 100 μg/mL. The nitric oxide (NO) production was reduced by compounds 2 and 3 with IC50 values of 7.0 and 7.5 μg/mL, respectively. ß-D-glucopyranose,1,4,6-tris (3,4,5-trihydroxybenzoate) 4) did not cause a significant increase in adipogenesis despite its strong PPARγ agonistic action (8 6-fold increase) and may represent a good candidate for the treatment of MetS without the undesirable side effect of weight gain.


2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Tae Hyeon Kim ◽  
Jin Kyu Kim ◽  
Young-Hee Kang ◽  
Jae-Yong Lee ◽  
Il Jun Kang ◽  
...  

Aldose reductase (AR) inhibitors have a considerable therapeutic potential against diabetes complications and do not increase the risk of hypoglycemia. Through bioassay-guided fractionation of an EtOH extract of the kernel from purple corn (Zea maysL.), 7 nonanthocyanin phenolic compounds (compound1–7) and 5 anthocyanins (compound8–12) were isolated. These compounds were investigated by rat lens aldose reductase (RLAR) inhibitory assays. Kinetic analyses of recombinant human aldose reductase (rhAR) were performed, and intracellular galactitol levels were measured. Hirsutrin, one of 12 isolated compounds, showed the most potent RLAR inhibitory activity (IC50, 4.78 μM). In the kinetic analyses using Lineweaver-Burk plots of 1/velocity and 1/substrate concentration, hirsutrin showed competitive inhibition against rhAR. Furthermore, hirsutrin inhibited galactitol formation in rat lens and erythrocytes sample incubated with a high concentration of galactose; this finding indicates that hirsutrin may effectively prevent osmotic stress in hyperglycemia. Therefore, hirsutrin derived fromZea maysL. may be a potential therapeutic agent against diabetes complications.


2018 ◽  
Vol 16 (1) ◽  
pp. 324-332 ◽  
Author(s):  
Nurhayat Tabanca ◽  
Zulfiqar Ali ◽  
Ulrich R. Bernier ◽  
Nancy Epsky ◽  
Ayse Nalbantsoy ◽  
...  

AbstractAn ethanol extract fromVeratrum lobelianumBernh. rhizomes showed larvicidal activity with LC50values of 11.79 ppm and 89.9 ppm against 1stand 4thinstar larvae, respectively, at 24 h post-treatment. The extract also showed proportion not biting (PNB) value of 0.76 at 100 μg/cm2against females ofAe.aegypti. Systematic bioassay-guided fractionation ofV.lobelianumextract resulted in the isolation of five compounds that were identified as ethyl palmitate (1), ethyl linoleate (2), β-sitosterol (3), resveratrol (4) and oxyresveratrol (5) by GC-MS,1H-NMR, and13C-NMR techniques, comparison with literature data, and confirmation with authentic compounds. Compound2exhibited larvicidal activity with an LC50value of 24.1 (22.0-26.2) ppm whereas1was inactive. β-Sitosterol (3) displayed the highest larvicidal activity with LC50= 1.7 (1.3-12.3) ppm and LC90= 5.1 (3.4-13.8) ppm. Compounds4and5had larvicidal activity with LC50values of 18.5 (15.3-23.3) and 22.6 (19.0-26.8) ppm, respectively, and had an equivalent PNB values of 0.75 at 25 nmol/cm2. In addition,4and5were explored for their human-based repellency againstAe.aegypti, attractiveness against male medfliesCeratitis capitata, and also evaluated against series of human carcinoma cells (A549, HEK293, HeLa, SH-SY5Y); however, no significant activity was found.


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