A New Purine Derivative from the Roots of Phyllanthus flexuosus

2018 ◽  
Vol 13 (1) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Guanlin Zhu ◽  
Hongying Wang ◽  
Kunrong Gan ◽  
Heng Gao ◽  
Wei Li
Keyword(s):  
Spectroscopic Analysis ◽  
Carcinoma Cell ◽  
Inhibitory Effect ◽  
X Ray Diffraction ◽  
Purine Derivative ◽  
X Ray ◽  
Carcinoma Cell Lines ◽  
Human Hepatocellular Carcinoma Cell ◽  
Different Levels

A new purine derivative, 1-methyl-3-isopentenylisoguanine (1), together with six known compounds (2-7), was isolated from the roots of Phyllanthus flexuosus. The newly isolated structure was established by means of extensive spectroscopic analysis and single-crystal X-ray diffraction experiment. All isolates were evaluated for their in vitro cytotoxicities against two human hepatocellular carcinoma cell lines (HepG2 and SMMC-7721) by CCK-8 assays. Among them, three cleistanthane diterpenes (2–4) exhibited different levels of cytotoxicities against these cells with IC50 values ranging from 27.34 to 53.28 μM. Furthermore, acetylcholinesterase inhibitory effect for the new purine derivative was also assessed.

scholarly journals Nanangenines: drimane sesquiterpenoids as the dominant metabolite cohort of a novel Australian fungus, Aspergillus nanangensis

2019 ◽  
Vol 15 ◽  
pp. 2631-2643 ◽  
Author(s):  
Heather J Lacey ◽  
Cameron L M Gilchrist ◽  
Andrew Crombie ◽  
John A Kalaitzis ◽  
Daniel Vuong ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Biosynthetic Pathway ◽  
Spectroscopic Analysis ◽  
Bioinformatics Analysis ◽  
Biosynthetic Gene Cluster ◽  
In Vitro Activity ◽  
X Ray Diffraction ◽  
X Ray ◽  
Drimane Sesquiterpenoids

Chemical investigation of an undescribed Australian fungus, Aspergillus nanangensis, led to the identification of the nanangenines – a family of seven new and three previously reported drimane sesquiterpenoids. The structures of the nanangenines were elucidated by detailed spectroscopic analysis supported by single crystal X-ray diffraction studies. The compounds were assayed for in vitro activity against bacteria, fungi, mammalian cells and plants. Bioinformatics analysis, including comparative analysis with other acyl drimenol-producing Aspergilli, led to the identification of a putative nanangenine biosynthetic gene cluster that corresponds to the proposed biosynthetic pathway for nanangenines.

scholarly journals Synthesis, Structure of Nitrogen-Containing Phosphinogold(I) Ferrocenes. In vitro Activity against Bladder and Colon Carcinoma Cell Lines

1995 ◽  
Vol 2 (6) ◽  
pp. 311-326 ◽  
Author(s):  
Manuella Viotte ◽  
Bernard Gautheron ◽  
Marek M. Kubicki ◽  
Ilya E. Nifant'ev ◽  
Simon P. Fricker
Keyword(s):  
Carcinoma Cell ◽  
In Vitro Activity ◽  
X Ray ◽  
Carcinoma Cell Lines ◽  
Anti Tumour Activity ◽  
Tetramethylammonium Bromide ◽  
Tumour Activity ◽  
Nitrogen Phosphorus ◽  
Good Agreement

The gold salt [(tht)AuCl] was reacted with [1-N,N-dimethylaminométhyl-2-diphenylphosphino]ferrocene (1) forming the bimetallic derivative 4. The reaction of methyl iodide and tetramethylammonium bromide on the chloride 4 produced the ammonium salt 5 and the bromide 6 respectively. New aminophosphines 2 and 3, which represent two of the rare phosphorylated metallocenes containing P(III)-N bond have also been coordinated to gold(I) to form 7 and 8. The presence of the ethoxy group in 7 provides evidence for the lability of one nitrogen-phosphorus bond. The X-ray structure of compounds 4 and 7 have been established. Both crystallize in space group P21/c, monoclinic, with a = 11.095(2) Å, b = 12.030(3) Å, c = 17.763(4) Å, β= 94.02(2)∘, Z = 4 for 4 and a = 14.863(3) Å, b = 8.036(5)Å, c = 18.062(5)Å, β =101.64(1)°, Z = 4 for 7. A197u Mössbauer data are in good agreement with those for other linear P-Au-Cl containing complexes. The compounds were evaluated for in vitro anti-tumour activity against two human tumours. Differential cytotoxicity was observed with activity comparable to cisplatin, with the exception of one compound which was significantly more cytotoxic.

scholarly journals Synthesis of a Small Library of Nature-Inspired Xanthones and Study of Their Antimicrobial Activity

Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2405 ◽  
Author(s):  
Diana I. S. P. Resende ◽  
Patrícia Pereira-Terra ◽  
Joana Moreira ◽  
Joana Freitas-Silva ◽  
Agostinho Lemos ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Biofilm Formation ◽  
Multidrug Resistant ◽  
Inhibitory Effect ◽  
X Ray Diffraction ◽  
X Ray ◽  
Xanthone Derivatives ◽  
Potent Inhibitory Effect ◽  
Resistant Strains

A series of thirteen xanthones 3–15 was prepared based on substitutional (appendage) diversity reactions. The series was structurally characterized based on their spectral data and HRMS, and the structures of xanthone derivatives 1, 7, and 8 were determined by single-crystal X-ray diffraction. This series, along with an in-house series of aminated xanthones 16–33, was tested for in-vitro antimicrobial activity against seven bacterial (including two multidrug-resistant) strains and five fungal strains. 1-(Dibromomethyl)-3,4-dimethoxy-9H-xanthen-9-one (7) and 1-(dibromomethyl)-3,4,6-trimethoxy-9H-xanthen-9-one (8) exhibited antibacterial activity against all tested strains. In addition, 3,4-dihydroxy-1-methyl-9H-xanthen-9-one (3) revealed a potent inhibitory effect on the growth of dermatophyte clinical strains (T. rubrum FF5, M. canis FF1 and E. floccosum FF9), with a MIC of 16 µg/mL for all the tested strains. Compounds 3 and 26 showed a potent inhibitory effect on two C. albicans virulence factors: germ tube and biofilm formation.

scholarly journals Synthesis, Structure and Evaluation of the N-(2-Acetyl-4-(styryl)phenyl)-4-benzenesulfonamide Derivatives for Anticholinesterase and Antioxidant Activities

Crystals ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 341
Author(s):  
Malose J. Mphahlele ◽  
Samantha Gildenhuys ◽  
Sizwe J. Zamisa
Keyword(s):  
Molecular Level ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
X Ray Diffraction ◽  
Enzymatic Assays ◽  
X Ray ◽  
Protein Ligand Interactions ◽  
Ligand Interactions

N-(2-Acetyl-4-bromophenyl)-4-methylbenzenesulfonamide (2) was transformed into 5-(4-methoxymethylstyryl)-2-(p-tolylsulfonamido)acetophenone (3a) and 5-(4- trifluoromethylstyryl)-2-(p-tolylsulfonamido)acetophenone (3b). Their structures were determined using a combination of NMR (1H & 13C) and mass spectroscopic as well as single crystal X-ray diffraction techniques. These compounds and the corresponding precursor, 2-amino-5-bromoacetophenone (1), were evaluated through enzymatic assays in vitro for inhibitory effect against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities as well as antioxidant effect through the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide (NO) free radical scavenging assays. Molecular docking was performed on 3a to determine plausible protein–ligand interactions on a molecular level. Their drug likeness properties (absorption, distribution, metabolism, and excretion) and ability to cross the blood–brain barrier (BBB) have also been predicted at theoretical level.

Salaterpene E, a eudesmane-type sesquiterpene from Salacia longipes var. camerunensis

2016 ◽  
Vol 71 (2) ◽  
pp. 87-93 ◽  
Author(s):  
Brice Mittérant Mba’ning ◽  
Bruno Lenta Ndjakou ◽  
Ferdinand Mouafo Talontsi ◽  
Alain Meli Lannang ◽  
Birger Dittrich ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Absolute Configuration ◽  
Previous Investigation ◽  
Spectroscopic Analysis ◽  
Inhibitory Concentration ◽  
Anomalous Scattering ◽  
X Ray Diffraction ◽  
Meoh Extract ◽  
X Ray

AbstractA mixture of two compounds with potent antiplasmodial activity in vitro against the W2 strain of Plasmodium falciparum (half maximal inhibitory concentration, 1.12 μg/mL) was obtained in a previous investigation of the CH2Cl2-MeOH extract of the seeds of Salacia longipes var. camerunensis. Separation by column chromatography led now to the isolation of salaterpene E (1) and (1R,2R,4S,5S,6R,7R,9S,10R)-2-acetoxy-1,6,9-tribenzoyloxy-4-hydroxy-dihydro-β-agarofuran (2). The structure of 1 was elucidated by spectroscopic analysis, and its absolute configuration was established unambiguously by means of single-crystal X-ray diffraction. Also the absolute configurations of the recently described salaterpenes A (2a) and D (2b) were determined by this method using the anomalous scattering of the oxygen atoms only.

Sign in / Sign up

Export Citation Format

Share Document