scholarly journals Synthesis, Characterization, and Pharmacological Evaluation of Selected Aromatic Amines

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Hammad Ismail ◽  
Bushra Mirza ◽  
Ihsan-ul Haq ◽  
Muhammad Shabbir ◽  
Zareen Akhter ◽  
...  

Aromatic amines 1-amino-4-phenoxybenzene (A-1A), 2-(4-aminophenoxy) naphthalene (A-2A), and 1-(4-aminophenoxy) naphthalene (A-3A) were synthesized by the reduction of corresponding nitroaromatics with hydrazine monohydrate and Pd/C 5% (w/w). The newly synthesized compounds were characterized by FTIR,1H NMR,13C NMR, UV-visible spectrophotometer, and mass spectrometry and their biological activities were investigated along with structurally similar 4-(4-aminophenyloxy) biphenyl (A-A). Results of brine shrimp cytotoxicity assay showed that almost all of the compounds had LD50values <1 μg/mL. The compounds also showed significant antitumor activity with IC50values ranging from 67.45 to 12.2 µgmL−1. The cytotoxicity and antitumor studies correlate the results which suggests the anticancerous nature of compounds. During the interaction study of these compounds with DNA, all of the compounds showed hyperchromic effect indicating strong interaction through binding with the grooves of DNA. Moreover, A-3A also showed decrease inλmaxconfirming higher propensity for DNA groove binding. In DPPH free radical scavenging assay, all the compounds showed potential antioxidant capability. The compounds were highly active in protecting DNA against hydroxyl free radicals. DNA interaction and antioxidant results back up each other indicating that these compounds have potential to be used as cancer chemopreventive agents. Additionally, one compound (A-1A) showed significant antibacterial and antifungal activity as well.

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
P. R. Chetana ◽  
M. N. Somashekar ◽  
B. S. Srinatha ◽  
R. S. Policegoudra ◽  
S. M. Aradhya ◽  
...  

Three new Ni(II) square planar complexes of 4-methoxy-3-benzyloxybenzaldehyde thiosemicarbazide(4m3BTSC) having polypyridyl bases of general formulation [ML2] (1) and [MLB] (2, 3), where L = 4m3BTSC and B is N,N-donor heterocyclic bases, namely, 1,10-phenanthroline (phen, 2), 2,2′-bipyridine (bpy, 3), are synthesized and characterized. The free radical scavenging assay results showed that complex 1 possesses significant activity when compared to complexes 2 and 3. The biological studies showed that the ligand and its complexes exhibited significant and different biological activities and also the prepared compounds are nonmutagenic. They may be potential commercial antioxidants because of their nonmutagenic and nontoxic nature. The DNA interaction of the new complexes is evaluated by absorption, emission, and melting temperature methods, and the results suggested that the binding affinity of the complexes increases with the presence of planar ligand in the molecule. The nickel (II) complexes with planar phenanthroline bases show moderate DNA binding and cleavage ability.


2021 ◽  
Vol 43 (2) ◽  
pp. 227-227
Author(s):  
Muhammad Anwar Saeed Muhammad Anwar Saeed ◽  
Hizbullah Khan Hizbullah Khan ◽  
Muhammad Sirajuddin Muhammad Sirajuddin ◽  
Syed Muhammad Salman Syed Muhammad Salman

The manuscript describes the binding of DNA as well as biological studies of some mixed ligand dithiocarbamate Palladium (II) complexes (1-5). The observed compounds are of general formulae [PdCl(DT)(PR3)]. The dithiocarbamate “DT” and “PR3” groups are varied among the studied complexes as DT = bis[(2-methoxyethyl) dithiocarbamate)] (1 and 2), dibutyl dithiocarbamate (4 and 5), bis[(2-ethyl) hexyl dithiocarbamate)] (3); PR3 = triphenyl phosphine (1), benzy diphenyl phosphine (2), diphenyl-tert-butyl phpsphine (3), diphenyl-p-tolyl phosphine (4) and diphenyl-2-methoxy phenyl phosphine (5). The synthesized complexes were screened for DNA binding study via (UV Visible spectrophotometry and Viscometery) and biological activities such as anti-bacterial and anti-fungal, Molinspiration calculations and antioxidant potencies stimulated by hydrogen peroxide in human blood lymphocytes. In case of drug DNA interaction, complexes showed some sort of interaction with DNA solution. Almost all the complexes exhibited moderate antifungal and antibacterial behavior (against Gram positive and negative bacterial strains). The Molinspiration calculation study revealed that the said Pd (II) mixed complexes are biologically significant drugs having adequate molecular properties regarding drug likeness, except the log P values of complexes 3-5 because some structural adjustments must be done for enhancement of their bioavailability and hydrophilic nature. Regarding the antioxidant potential of complexes 1, 2 and 4, the H2O2 treatment of complexes violently decreased the action of antioxidant enzymes, superoxide dismutase and catalase and enhanced the level of thiobarbituric acid-reacting substances. Under experimental conditions, we conclude that all complexes act as anti-mutagens as they significantly suppress H2O2-induced oxidative damage at non-genotoxic concentrations.


Molecules ◽  
2019 ◽  
Vol 24 (10) ◽  
pp. 1904 ◽  
Author(s):  
Magdalena de J. Rostro-Alanis ◽  
Juan Báez-González ◽  
Cynthia Torres-Alvarez ◽  
Roberto Parra-Saldívar ◽  
José Rodriguez-Rodriguez ◽  
...  

Oregano (Poliomintha longiflora) essential oil (Ooil) is a product of high commercial value and many applications, including chemotherapy. Aiming to achieve the best use of this resource, the present study focuses on the characterization of separated fractions of Ooil by fractional vacuum distillation at low pressure. Four fractions (F1–F4) and undistilled oil (Unoil) were separated from Ooil and analyzed for their chemical composition and biological activities, such as antioxidant and antimicrobial activities. Gas chromatography–mass spectrometry shows differences in the composition among the fractions and Ooil. The amount of monoterpenes oxygenated (MO), sesquiterpenes hydrocarbon (SeH) and monoterpenes hydrocarbon (MH) varied between the fractions in ranges of 1.51–68.08, 3.31–25.12 and 1.91–97.75%, respectively. The major concentrations of MO and SeH were observed in F4 and Unoil. On the other hand, the highest concentrations of MH were found in F1 and F2, while the lowest were in F4 and Unoil. These results were correlated with the biological activity. Free-radical scavenging activity varied among fractions, with F4 and Unoil showing the highest activity. The antimicrobial test showed that F4 and Unoil had the highest activity in almost all cases. The correlation between the variables studied in the different fractions allows the definition of the particular properties for each one of them.


Horticulturae ◽  
2021 ◽  
Vol 7 (10) ◽  
pp. 364
Author(s):  
Dario Kremer ◽  
Marijana Zovko Končić ◽  
Ivan Kosalec ◽  
Iztok Jože Košir ◽  
Tanja Potočnik ◽  
...  

Eryngium amethystinum L. is a wild vegetable used in Croatia. Both E. amethystinum and E. alpinum L. are decorative plants that can also be used in horticulture. To find out the hidden qualities of these two species, the following biological activities were studied: essential oil (EO) composition, analyzed by gas chromatography and gas chromatography with mass spectrometry (GC, GC–MS); phenolic compound content (PC), analyzed by high performance liquid chromatography (HPLC); total phenols as well as total flavonoids, analyzed by ultraviolet–visible spectrophotometry (UV/Vis); antioxidants, analyzed by 2,2-diphenyl-1-picrylhydrazyl radical-scavenging activity (DPPH), b-carotene-linoleic acid assay, chelating activity and reducing power of the extracts; and antimicrobial evaluation by micro-dilution assay and inhibition of Candida albicans blastospore germination. The major constituents of EO were β-caryophyllene (15.2%), α-pinene (10.2%) and 2,3,6-trimethylbenzaldehyde (9.3%) for E. amethystinum and caryophyllene oxide (27.9%), bicyclogermacrene (13.2%) and germacrene D (8.2%) for E. alpinum. The methanol extracts of both species showed a broad spectrum of antibacterial and antifungal activity with minimum inhibitory concentrations (MIC) less than or equal to 1.944 and 1.11 mg/mL, respectively.


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.


Molecules ◽  
2020 ◽  
Vol 25 (19) ◽  
pp. 4415 ◽  
Author(s):  
Halina Ekiert ◽  
Joanna Pajor ◽  
Paweł Klin ◽  
Agnieszka Rzepiela ◽  
Halina Ślesak ◽  
...  

Artemisia vulgaris L. (common mugwort) is a species with great importance in the history of medicine and was called the “mother of herbs” in the Middle Ages. It is a common herbaceous plant that exhibits high morphological and phytochemical variability depending on the location where it occurs. This species is well known almost all over the world. Its herb—Artemisiae vulgaris herba—is used as a raw material due to the presence of essential oil, flavonoids, and sesquiterpenoids lactones and their associated biological activities. The European Pharmacopoeia has listed this species as a potential homeopathic raw material. Moreover, this species has been used in traditional Chinese, Hindu, and European medicine to regulate the functioning of the gastrointestinal system and treat various gynecological diseases. The general aim of this review was to analyze the progress of phytochemical and pharmacological as well as professional scientific studies focusing on A. vulgaris. Thus far, numerous authors have confirmed the beneficial properties of A. vulgaris herb extracts, including their antioxidant, hepatoprotective, antispasmolytic, antinociceptive, estrogenic, cytotoxic, antibacterial, and antifungal effects. In addition, several works have reviewed the use of this species in the production of cosmetics and its role as a valuable spice in the food industry. Furthermore, biotechnological micropropagation of A. vulgaris has been analyzed.


2021 ◽  
Vol 33 (6) ◽  
pp. 1396-1402
Author(s):  
Somepalli Venkateswarlu ◽  
Gandrotu Narasimha Murty ◽  
Meka Satyanarayana ◽  
Vidavalur Siddaiah

To widen aurones applicability in achromatic food and cosmetic applications, a series of dihydroaurones were designed to mimic natural aurones as well as synthetic aurones. Dihydroaurones have been synthesized from the corresponding aurones by hydrogenation. These dihydroaurones and their corresponding aurones were screened for antioxidant, anti-inflammatory and tyrosinase enzyme inhibitory activity. Synthesized dihydroaurones (3b-f) displayed superior antioxidant activity in superoxide free radical scavenging assay than the standard gallic acid. Dihydroaurones (3b-f) also exhibited significant tyrosinase enzyme inhibitory activity and two dihydroaurones (3h, 3j) showed promising 5-lipoxygenase inhibitory activity.


Author(s):  
V.V. Bhuva ◽  
V.N. Bhadani ◽  
H.D. Purohit ◽  
Dipak M. Purohit

Pyridine nucleus plays an important role in medicine, agriculture and industrial chemistry. With a view of biological activities and variety of industrial applications, some new 2" – methoxy - 4" - [2 - ( 4' -chlorophenyl)-6-methyl imidazo [1, 2-a] pyridin-3-yl]-6"-aryl nicotinonitrile( 4a-4l ) has been synthesized. The products have been assayed for their biological activity against Gram +ve, Gram –ve bacteria and fungi. Some of the products showed moderate activity in concentration 50µg/ml. The structures of the products have been elucidated by IR, 1H-NMR, Mass spectral data, elemental analysis and thin layer chromatography.


2020 ◽  
Vol 2 (1) ◽  
pp. 74

Algae is a simple and vast group of photosynthetic organisms. Algae grow in most of the natural environments, including water, rocks, and soil, but interestingly also grow on and in other organisms. Their main habitats are freshwater, brackish and marine ecosystems, Also volcanic waters and salt waters. Among them, marine algae are recognized as a rich source of beneficial bioactive compounds. Marine algal originated compounds have been reported to exhibit various biological activities such as anticoagulant, anti-viral, antioxidant, anti-allergic, anti-cancer, anti-inflammatory, anti-obesity, etc. Phycocyanin is a blue-colored naturally existing phycobiliprotein pigment, which is abundant in cyanobacteria, blue-green algae. In this study, phycocyanin was extracted from the Geitlerinema sp. UV-Vis spectroscopic analysis and HPLC analysis confirmed the presence of phycocyanin. The extracted pigment was assessed for their antioxidant property by various methods such as Phosphomolybdenum assay, Ferric ions reducing power assay, DPPH radical scavenging activity, Hydrogen peroxide free radical scavenging assay, Anti-lipid peroxidation activity. The study reveals that the phycocyanin pigments possess the antioxidant property, and it can be used as a promising pharmaceutical and nutraceutical compound.


2017 ◽  
Vol 30 (1) ◽  
pp. 5-8 ◽  
Author(s):  
Mostefa Lefahal ◽  
Nabila Zaabat ◽  
Lakhdar Djarri ◽  
Merzoug Benahmed ◽  
Kamel Medjroubi ◽  
...  

Abstract The aim of the present work was to evaluate the antioxidant activity of extracts and four flavonoids that had been isolated from the aerial parts of Bunium alpinum Waldst. et Kit. (Apiaceae) and Tamarix gallica L. (Tamaricaceae). In this work, the four flavonoids were first extracted via various solvents, then purified through column chromatography (CC) and thin layer chromatography (TLC). The four compounds were subsequently identified by spectroscopic methods, including: UV, mass spectrum 1H NMR and 13C NMR. The EtOAc extract of Bunium alpinum Waldst. et Kit yielded quercetin-3-O-β-glucoside (3’,4’,5,7-Tetrahydroxyflavone-3-β-D-glucopyranoside) (1), while the EtOAc and n-BuOH extracts of Tamarix gallica L. afforded 3,5,3’-trihydroxy-7,4’-dimethoxyflavone (2), 3,5,7-trihydroxy-4’-methoxyflavone (3) and 5-hydroxy-3,7,4’-trimethoxyflavone (4). The antioxidant activity of the extracts and the flavonoids were then evaluated through DPPH free radical-scavenging assay. Of all studied extracts, the n-Butanol extract of Bunium alpinum (EC50 = 1.84 μg/ml) showed the best antioxidant activity against (DPPH). In contrast, the isolates demonstrated varying degrees of antioxidant activity: compound (1) was the more active (EC50 = 0.28 μg/ml), followed by compound (3) and (2) (EC50 = 0.309μg/ml, EC50 = 0.406 μg/ml, respectively), compound (4) showed the lowest activity. All the isolated flavonoids exhibited antioxidant activity, but this was lower than the control (Trolox). In conclusion, due to the presence of flavonoids in their ariel parts, the studied plants could be natural sources of several important antioxidant agents


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