scholarly journals In VitroEnzyme Inhibition Potentials and Antioxidant Activity of Synthetic Flavone Derivatives

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Mohammad Shoaib ◽  
Syed Wadood Ali Shah ◽  
Niaz Ali ◽  
Ismail Shah ◽  
Muhammad Naveed Umar ◽  
...  

Free radicals are produced by an important chemical process known as oxidation that in turn initiates chain reactions to damage the cells and originate oxidative stress. Flavones have got special position in research field of natural and synthetic organic chemistry due to their biological capabilities as antioxidant. The antioxidants are known to possess extensive biological effects that include antiviral, antibacterial, anti-inflammatory, antithrombotic, and vasodilatory activities. The simple flavone (F1) and substituted flavone derivatives (F2–F5) have been synthesized fromo-hydroxyacetophenone and benzaldehyde derivatives in good yield. The structures have been established by different spectroscopic techniques like1H NMR,13C NMR, IR, and elemental analysis. Antioxidant profile of these compounds was established using DPPH and H2O2free radical scavenging assay. The findings showed that halogenated flavones showed more enzyme inhibitions and antioxidant activities than simple flavones and are potential candidates for the treatment of wide range of diseases.

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
M. K. Prashanth ◽  
M. Madaiah ◽  
H. D. Revanasiddappa ◽  
K. N. Amruthesh

Condensation of amine 1 with aldehyde 2 gives Schiff base, N-(4-((benzofuran-2-ylmethylene) amino)phenyl)acetamide 3. Schiff base on N-acylation with different substituted acid chlorides in the presence of triethylamine gives the corresponding benzamides, N-acetyl-N-(4-((benzofuran-2-ylmethylene)amino)phenyl)substitutedbenzamide (NABP) 5a–j. The structures of newly synthesized compounds were characterized by elemental analysis, 1H NMR, 13C NMR FT-IR, and mass spectral studies. Compounds 3 and 5a–j have been screened for their antimicrobial activity using the disc diffusion and minimum inhibitory concentration (MIC) method against the selected bacterial and fungal strain. Compounds 5a, 5e, 5g, and 5h were found to be more active against all tested strains. The antioxidant properties were evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide radical scavenging methods. Compounds 5i and 5j showed predominant antioxidant activities among the synthesized analogues. The interaction between NABP and bovine serum albumin (BSA) was investigated using fluorescence and ultraviolet spectroscopic techniques at 298 K under imitated physiological conditions. The results revealed that NABP caused the fluorescence quenching of BSA through a static quenching procedure. The binding constants and the number of binding sites were calculated. The binding distance between the donor (BSA) and acceptor (NABP) was determined based on Forster’s theory.


2020 ◽  
Vol 2 (1) ◽  
pp. 66

Lipid fractions of gonads present in sea urchins serves as a source of bioactive agents with potent pharmaceutical properties. The present study reports the in-vitro biological effects of lipids isolated from gonads of sea urchin: Stomopneustes variolaris collected from the East coast of India. The extracted lipids were characterized by spectroscopic techniques such as GCMS and FTIR and tested for in-vitro biological effects. GCMS analysis of the lipid extract detected high levels of hexa triacontane (17.023 %), tetratetracontane (15.913%), and octacosane (15.628%) and low concentrations of oleic acid (2.206%) and sulfurous acid, pentadecy 2-propyl ester (1.744%). FTIR analysis identified rich composition of functional groups present in the lipids such as 3418.93 cm-1 (hydroxyl), 2921.08cm-1 and 2854.81 cm-1 (alkane), 2660.69 cm-1 (carboxylic acid), 1596.11 cm-1 (amine), 1291.76 cm-1 (aromatic amine). The lipid fraction evaluated by agar diffusion assay measured in terms of zone of inhibition showed bactericidal effects against gram-positive bacteria: Streptococcus aureus (30 mm); Pseudomonas aeruginosa (28.5 mm) and gram-negative bacteria: Escherichia coli (29.5 mm); Klebsiella pneumonia (27.5 mm) and Vibrio cholera (28 mm) respectively. The lipid fraction also showed an effective anti-fungal effect against C.albicans (25 mm). Further, the lipid fractions showed good radical scavenging effect against total phenolic, flavonoid content (15.12 mg GAE/g and 32.72 mg QE/g), and hydrogen peroxide radicals (IC50- 48.28mg/ml) confirming its anti-oxidant potential. Based on the observed results, it was identified that the lipid fraction of gonads of Stomopneustes variolaris demonstrated various biological effects such as bactericidal, anti-fungal and radical scavenging activities which could have a great scope in the formulation of biopharmaceutical agents.


Data in Brief ◽  
2018 ◽  
Vol 17 ◽  
pp. 870-875 ◽  
Author(s):  
Kotaro Hara ◽  
Takao Someya ◽  
Katsura Sano ◽  
Yoshimasa Sagane ◽  
Toshihiro Watanabe ◽  
...  

2019 ◽  
Vol 31 (11) ◽  
pp. 2448-2452
Author(s):  
Somashekara Bhadrachar ◽  
Giriyapura R. Vijayakumar ◽  
Kittappa M. Mahadevan ◽  
Thippeswamy Basavaraja

A series of 1,2,4,5-tetrasubstituted imidazoles (2a-g) were synthesized using 1,2-diketone, 1-naphthaldehyde, substituted aromatic amine and ammonium acetate in the presence of ceric ammonium nitrate as a catalyst. The synthesized compounds were characterized by FT-IR, 1H NMR, Mass spectra and explored for their antioxidant activity by DPPH free radical scavenging assay method. Among the synthesized compounds 2a, 2e and 2f exhibit good antioxidant activities. Molecular docking study was also been performed to know the possible interactions between the synthesized compound and antioxidant receptor 3MNG.


Molecules ◽  
2019 ◽  
Vol 24 (20) ◽  
pp. 3795 ◽  
Author(s):  
Laura Guedes ◽  
Pedro B. P. S. Reis ◽  
Miguel Machuqueiro ◽  
Asma Ressaissi ◽  
Rita Pacheco ◽  
...  

Centaurium erythraea is recommended for the treatment of gastrointestinal disorders and to reduce hypercholesterolemia in ethno-medicinal practice. To perform a top-down study that could give some insight into the molecular basis of these bioactivities, decoctions from C. erythraea leaves were prepared and the compounds were identified by liquid chromatography-high resolution tandem mass spectrometry (LC–MS/MS). Secoiridoids glycosides, like gentiopicroside and sweroside, and several xanthones, such as di-hydroxy-dimethoxyxanthone, were identified. Following some of the bioactivities previously ascribed to C. erythraea, we have studied its antioxidant capacity and the ability to inhibit acetylcholinesterase (AChE) and 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR). Significant antioxidant activities were observed, following three assays: free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH) reduction; lipoperoxidation; and NO radical scavenging capacity. The AChE and HMGR inhibitory activities for the decoction were also measured (56% at 500 μg/mL and 48% at 10 μg/mL, respectively). Molecular docking studies indicated that xanthones are better AChE inhibitors than gentiopicroside, while this compound exhibits a better shape complementarity with the HMGR active site than xanthones. To the extent of our knowledge, this is the first report on AChE and HMGR activities by C. erythraea decoctions, in a top-down analysis, complemented with in silico molecular docking, which aims to understand, at the molecular level, some of the biological effects ascribed to infusions from this plant.


2003 ◽  
Vol 58 (9-10) ◽  
pp. 704-707 ◽  
Author(s):  
Rilka Taskova ◽  
Maya Mitova ◽  
Bozhanka Mikhova ◽  
Helmut Duddeck

AbstractTwo flavonoid aglycons, eight flavonoid glycosides, chlorogenic acid and syringin were isolated from aerial parts of Carthamus lanatus. Isorhamnetin 3-O-β-ᴅ-glucoside and chlorogenic acid were found for the first time in the genus Carthamus and respectively, quercimeritrin, astragalin, kaempferol 3-O-β-ᴅ-sophoroside and syringin in the species. The ethyl acetate fraction of the methanol extract exhibited a higher antioxidant activity than the butanol fraction measured by the α,α-diphenyl-β-picrazylhydrazyl (DPPH) free radical scavenging assay. Cytotoxicity and antioxidant activities of the main constituent, luteolin 7-O-β-D-glucoside, were evaluated.


2020 ◽  
Vol 50 (5) ◽  
Author(s):  
Tianyao Zhao ◽  
Wenjin Su ◽  
Yang Qin ◽  
Liyun Wang ◽  
Yufan Kang

ABSTRACT: Pea (Pisum sativum L.) is the fourth leading legume crop in the world, and its demand is increasing. In this study, the morphological characteristics (seed shape, seed surface, seed coat color, hilum color, cotyledon color, 100-seed weight and color values), total phenolic content (TPC), total flavonoid content (TFC), 2,2’-azinobis-(3-ethylbenzthiazoline-6-sulphonate) (ABTS) free radical scavenging capacity and ferric reducing antioxidant power (FRAP) of 75 pea cultivars were investigated. Results showed rich genetic diversity and a wide range of phenolic contents and antioxidant activities. Sixteen varieties enriched with phenolic contents and high antioxidant activities were screened out. A significant correlation was reported among color values, TPC, TFC, ABTS and FRAP. Principal component analysis (PCA) extracted four principal components with a total cumulative contribution of 81.29%. Hierarchical cluster analysis based on the four extracted principal components resulted in a dendrogram dividing the peas into three groups. In addition, dark pea seeds have potential as a functional food in addition to their traditional role in providing dietary protein and fibre. This study provided a scientific basis for the breeding of pea varieties, development of new products and improvement of pea resource utilization.


2020 ◽  
Vol 8 (3) ◽  
pp. 9-13
Author(s):  
Purnamasari Nur Aini ◽  
Dzakwan Muhammad ◽  
Pramukantoro Ganet Eko ◽  
Mauludin Rachmat ◽  
El Fahmi

Background: Phytosomes are recently introduced drug delivery system and novel botanical formulation to produce lipophilic molecular complex to improve absorption and bioavailability of phytoconstituent. Myricetin is a well-known flavonoid with different biological effects and contributed in food preserving by free radical scavenging activity. However, bioavailability of myricetin is an important limiting factor for its antioxidant activities. Purpose: To overcome this limitation, in the present study we aimed to produce myricetin-loaded nano phytosomes to improve its physicochemical stability and bioavailability. Methods: myricetin-loaded nano phytosome was prepared by using phosphatidylcholine (PC) and cholesterol (CH). Myricetin nanophytosomes system was characterized by particle size analyzer, particle size distribution (PDI), encapsulation efficiency and potential antioxidant activity. Results: Results showed that formulation with the myricetin: PC: CH molar ratio of 1: 2: 0.8 had lower particle size (291.11 nm) and higher encapsulation efficiency percent (93%). Morphology analysis showed that myricetin nanophytosome spherical shape. The potential antioxidant data showed that incorporation myricetin in the phospholipid myricetin remained unchanged even after encapsulation of myricetin in binarynanophytosome formulation. Conclusion: Nano phytosomal formulation of myricetin showed promising potential in fortification of nutraceutical with water insoluble antioxidants.  


2021 ◽  
Vol 34 (3) ◽  
pp. 501-521
Author(s):  
N. S. Awwad ◽  
H. A. Ibrahium ◽  
A. A. Shati ◽  
M. Y. Alfaifi ◽  
Y. H. Ju ◽  
...  

A number of some main group and transition metal nicotine complexes were synthesized and fully characterized using detailed structural and spectroscopic analysis techniques such as elemental analysis, molar conductivities, magnetic susceptibilities, IR, Raman and NMR techniques. Moreover, scanning electron micrographs and thermogravimetric analyses were also done. Cytotoxic activities of the binary nicotine metal complexes were tested and evaluated against HepG2 (human hepatocellular carcinoma), HPC3 (human prostate cancer), and HCT116 (human colorectal carcinoma) tumor cell lines. The antioxidant activities were examined by free radical scavenging assay. The antimicrobial activities of the synthesized complexes were evaluated against Escherichia coli (gram-negative) and Staphylococcus aureus (gram-positive) microbes. The relationship between the chemical structure of the synthesized complexes and their biological influence as antimicrobial drugs was studied and evaluated.                     KEY WORDS: Nicotine metal complexes, Cytotoxicity, Antioxidant, Antimicrobial   Bull. Chem. Soc. Ethiop. 2020, 34(3), 501-521. DOI: https://dx.doi.org/10.4314/bcse.v34i3.7


2019 ◽  
Vol 20 (2) ◽  
pp. 90-96
Author(s):  
Nurul Azizah ◽  
Euis Filaila ◽  
Salahuddin Salahuddin ◽  
Egi Agustian ◽  
Anny Sulaswatty ◽  
...  

The rhizome of ginger is commonly used as a spice, food, beverage as well as medicine. Plant essential oils including from ginger have been widely used for food preservation, pharmaceutical and alternative medicines.  Currently there are growing interest of consumer for natural sources such as essential oils for natural antibacterial and antioxidant.  Jahe emprit (Zingiber officinale var. Amarum) is one of Indonesian ginger variety used to obtain ginger essential oil. The objective of current study was to investigate the effect of solvent to feed (SF) ratio in hydrodistillation process on yield, chemicals content, antibacterial and antioxidant activities of ginger essential oils from jahe emprit.  SF ratio used in this study is 0.7: 1, 1.7: 1, 2.7: 1.  Chemicals content was conducted using GCMS analysis.  Antibacterial assay was conducted using disc diffusion method against Escherichia coli and Staphylococcus aureus.  Antioxidant assay was conducted using DPPH free radical scavenging assay.  The results show that the highest essential oil yield was obtained from SF ratio 1.7:1 which gave yield of 3.7%.  GCMS analysis shows that camphene was always the major compound present in those 3 SF ratio, although the amount present was differed.  Besides, 4 other major compounds present were varied.  Antibacterial assay using 1% concentration showed ginger oil obtained from SF 0.7:1 and 2.7:1 have the same activities for S. aureus, whereas SF ratio 1.7:1 has the lowest activities.  However for E. coli, all SF ratio gave same results.  For antioxidant activities at 1000 ppm concentration, the highest activity was obtained from SF ratio 2.7:1


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