scholarly journals Investigation of Galatella villosa and G. tatarica for Antioxidant, α-Amylase, Tyrosinase, Lipoxygenase and Xanthine Oxidase Inhibitory Activities

2017 ◽  
Vol 12 (8) ◽  
pp. 1934578X1701200
Author(s):  
Gülmira Özeka ◽  
Margarita Ishmuratova ◽  
Süleyman Yur ◽  
Fatih Göger ◽  
Yeşim Haliloglua ◽  
...  

In the present work two Galatella species, Galatella villosa Rchb.f. and Galatella tatarica (Less.) Novopokr collected from Kazakhstan were subjected to hydrodistillation to yield essential oils (EOs), and to maceration in methanol to yield extracts (MEs). The EOs and MEs were evaluated for antioxidant and in vitro inhibitory activities against α-amylase, tyrosinase, lipoxygenase and xanthine oxidase enzymes. The EOs of G. villosa and G. tatarica were investigated for chemical composition using GC-FID and GC/MS techniques. The composition of MEs was investigated with LC-MS/MS technique. Monoterpenes, β-pinene (23.6 %) and α-pinene (14.4 %) were the main constituents of G. tatarica essential oil, while the oil of G. villosa was characterized not only with monoterpene α-pinene (9.0 %), but also fatty acid, hexadecanoic acid (10.2%). 3-, 5-, 1,5- and 3,4-caffeoylquinic acids, 3-, 4- and 5-feruloylquinic acids, quercetin and its different glycosides were detected in MEs according to mass spectral data. G. tatarica (IC50=74.3 μg/mL) and G. villosa (IC50=78.5 μg/mL) extracts showed significant antioxidant activity. In the β-carotene bleaching test, the extracts demonstrated noteworthy activity (%Inh 44.46 and 41.14). The extracts scavenged ABTS radical as 1.85 mM and 1.27 mM of Trolox. In a concentration of 0.5 mg/mL, the oils showed 89% and 85% inhibition of α-amylase, while the extracts showed 86% and 78% inhibition at 2 mg/mL concentration, respectively. The EOs demonstrated noteworthy potent LOX enzyme inhibition ranging between 45% and 57%. In xanthine-xanthine oxidase model system, the extracts demonstrated the highest inhibitory potency ranging between 43% and 39%. The present work is the first contribution to the chemistry and biological activities of G. tatarica and G. villosa.

2014 ◽  
Vol 44 (4) ◽  
pp. 289-293
Author(s):  
S. BALUJA ◽  
S. CHANDA ◽  
R. BHALODIA ◽  
R. TALAVIYA

Dihydropyrimidinthione is an important class of heterocyclic compounds which exhibits wide spectrum of biological activities. In the present study, some bio-active dihydropyrimidinthione derivatives have been synthesized and their characterization was done by IR, NMR and mass spectral data. The antibacterial and antifungal activities of synthesized compounds have also been studied in N,N-dimethyl formamide and Dimethyl sulfoxide.


2020 ◽  
Vol 24 (14) ◽  
pp. 1610-1642 ◽  
Author(s):  
Ahmed El-Mekabaty ◽  
Hassan A. Etman ◽  
Ahmed Mosbah ◽  
Ahmed A. Fadda

Barbituric, thiobarbituric acids and their related analogs are reactive synthons for the synthesis of drugs and biologically, and pharmaceutically active pyrimidines. The present review aimed to summarize the recent advances in the synthesis of different alkylsubstituted, fused cycles, spiro-, and binary heterocycles incorporated pyrimidine skeleton based on barbituric derivatives. In this sequence, the eco-friendly techniques under catalytic conditions were used for the diverse types of multicomponent reactions under different conditions for the synthesis of various types of heterocycles. Nano-catalysts are efficient for the synthesis of these compounds in high yields and effective catalyst reusability. The compounds are potent antibacterial, cytotoxic, xanthine oxidase inhibitory activities, and attend as urease inhibitors. The projected mechanisms for the synthesis of pyranopyrimidines, benzochromenopyrimidines, chromeno-pyranopyrimidines, spiroxyindoles, oxospiro-tricyclic furopyrimidines, pyrimidine-based monoand bicyclic pyridines were discussed. The potent and diverse biological activities for instance, antioxidant, antibacterial, cytotoxic, and xanthine oxidase inhibitory activities, as well as urease inhibitors, are specified.


2019 ◽  
Vol 31 (9) ◽  
pp. 1895-1898
Author(s):  
Relangi Siva Subrahmanyam ◽  
Venkateswara Rao Anna

We report here an easy, efficient and green synthetic protocol for the (E)-1-aryl-3-(2-morpholinoquinolin-3-yl)prop-2-en-1-ones by the Claisen-Schmidt condensation of 2-morpholinoquinoline-3-carbaldehyde and different substituted acetophenones by using 1-butyl-3-methylimidazolium tetrafluoroborate (Bmim)BF4. The compounds were characterized by using 1H NMR, 13C NMR and mass spectral data and screened there in vitro antimicrobial activity against different bacterial and fungal organisms.


INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (07) ◽  
pp. 16-22
Author(s):  
N. Kumar ◽  
D Pathak ◽  

O-phenylenediamine and salicylic acid were used for the synthesis of 2-(1-(substituted phenylamino) methyl-1H benzo[d] imidazol-2-yl) phenol (2a-2h) derivatives by using various substituted aniline. In the first step, reaction of o-phenylenediamine and salicylic acid yielded 2-(1H-benzo[d]imidazol-2-yl) phenol (1), which on Mannich reaction with substituted aniline gave compounds (2a-2h). The structures of these compounds were characterized by IR, 1H NMR, mass spectral data and elemental analysis. Each analogue was tested in vitro for various types of pharmacological activity of this class of drugs including antibacterial, antifungal and anthelmintic activity. Among the synthesized compounds 2a act as vermifuge and no compound was found to be a vermicide. The compound 2c was found to be most active against E.coli and P. aeurigenosa and 2e be most active against B.subtilis and S.aureus. The derivative 2h shows good activity against C.albicans and A.niger.


2010 ◽  
Vol 13 (8) ◽  
pp. 362-368 ◽  
Author(s):  
N.T.R. Meda ◽  
A. Lamien-Med ◽  
M. Kiendrebeo ◽  
C.E. Lamien ◽  
A.Y. Coulibaly ◽  
...  

2014 ◽  
Vol 9 (5) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Rosa Tundis ◽  
Khaled Rashed ◽  
Ataa Said ◽  
Francesco Menichini ◽  
Monica R. Loizzo

The flowers of Bombax ceiba were investigated for their chemical composition, antioxidant effects and antiproliferative activity against seven human cancer cell lines. The antiproliferative responses of diethyl ether (DE) and light petroleum (PE) extracts were evaluated by sulforhodamine B (SRB) assay against MCF-7, HeLa, COR-L23, C32, A375, ACHN, and LNCaP cells in comparison with a human normal cell line, 142BR. Moreover, extracts were characterized by GC-MS analysis and tested for their antioxidant properties by different in vitro systems, namely DPPH, Fe-chelating activity and β-carotene bleaching test. Both PE and DE extracts showed the highest antiproliferative activity against human renal adenocarcinoma (ACHN) in a concentration-dependent manner. PE extract showed the highest radical scavenging activity against the DPPH radical, while DE extract was more active in the β-carotene bleaching test. The presence of β-sitosterol and some fatty acids may contribute to the bioactivity of B. ceiba flower extracts.


1973 ◽  
Vol 51 (7) ◽  
pp. 1123-1126 ◽  
Author(s):  
B. D. McLennan ◽  
A. Pater

Two known metabolites of N6-(Δ2-isopentenyl)adenosine, namely N6-(Δ2-isopentenyl)adenine and N6-(3-hydroxy-3-methylbutyl)adenine, have been shown to be oxidized by xanthine oxidase. On the basis of ultraviolet absorption and mass spectral data, the oxidation products, in each case, have been tentatively identified as the 8-hydroxy and 2,8-dihydroxy derivatives.


2007 ◽  
Vol 54 (3) ◽  
pp. 561-565 ◽  
Author(s):  
A Selcen Alpan ◽  
H Semih Gunes ◽  
Zeki Topcu

Benzimidazole is one of the most important heterocyclic groups manifesting various biological properties, such as antibacterial, antifungal, antimicrobial, antiprotozoal and antihelmintic activities. Several benzimidazole derivatives are also active as inhibitors of type I DNA topoisomerases. In this study, three 1H-benzimidazole derivatives with different electronic characteristics at position 5-, namely 5-chloro-4-(1H-benzimidazole-2-yl)phenol (Cpd I), 5-methyl-4-(1H-benzimidazole-2-yl)phenol (Cpd II) and 4-(1H-benzimidazole-2-yl)phenol (Cpd III), were synthesized and evaluated for their effects on mammalian type I DNA topoisomerase activity using quantitative in vitro plasmid supercoil relaxation assays. For the structure elucidation of the compounds, melting points, UV, IR, 1H NMR, 13C NMR, mass spectral data and elemental analyses were interpreted. Among the compounds, 5-methyl-4-(1H-benzimidazole-2-yl)phenol (Cpd II) manifested relatively potent topoisomerase I inhibition.


Author(s):  
Shraddha M. Prajapati ◽  
Rajesh H. Vekariya ◽  
Kinjal D. Patel ◽  
Shyamali N. Panchal ◽  
Hitesh D. Patel ◽  
...  

A library of quinoline analog two novel series of azetidin (SH1-5) and thiazolidin (SHa-e) derivatives were designed and synthesized with simple and eco-friendly methodologies. The structures of the compounds were elucidated with the aid of elemental analysis, IR, 1H-NMR and mass spectral data. These novel synthesized compounds were evaluated for antibacterial activity against two gram-positive bacteria (Staphylococcus aureus, Staphylococcus pyogenus) and two gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli). The title compounds were also studied for their antifungal activity with Candida albicans, Aspergillus niger, Aspergillus clavatus using the broth dilution technique. Most of the compounds were the best bio-active desired antibacterial analog with less MIC value against different tested strains.


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