scholarly journals Spectro-electrochemical assessments of DNA/BSA interactions, cytotoxicity, radical scavenging and pharmacological implications of biosensitive and biologically active morpholine-based metal(ii) complexes: a combined experimental and computational investigation

RSC Advances ◽  
2019 ◽  
Vol 9 (25) ◽  
pp. 14220-14241 ◽  
Author(s):  
Karunganathan Sakthikumar ◽  
Rajadurai Vijay Solomon ◽  
Jeyaraj Dhaveethu Raja

Morpholine-based metal(ii) complexes exhibited more significant biological activities than the free ligand. Among investigations towards DNA/BSA, the copper complex revealed excellent intercalating efficacy, which suggests it may have potential as a novel anticancer agent.

2018 ◽  
Vol 46 (2) ◽  
pp. 517-524
Author(s):  
Kandhan KARTHISHWARAN ◽  
Subban KAMALRAJ ◽  
Chelliah JAYABASKARAN ◽  
Shyam S. KURUP ◽  
Sabitha SAKKIR ◽  
...  

Aerva javanica (Burm. f) Juss. ex Schult. (Family: Amaranthaceae) family is one of the traditional medicinal plant growing in the United Arab Emirates. Apart from studies related to some medicinal properties, phytochemical, GC MS compound characterization and biological activities still to be investigated. An experiment was conducted to determine the possible bioactive components with their chemical structures and elucidation of phytochemicals from the aerial parts of the plant. The macro and micro-mineral constituents and antioxidant activities were also evaluated. Aerial parts of A. javanica were extracted sequentially with hexane, chloroform, ethyl acetate, acetone, methanol by cold percolation method. Free radical scavenging and antioxidant properties of methanolic extract were evaluated by using in vitro antioxidant assays such as hydroxyl radical scavenging activity, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals, superoxide radical scavenging activity and ABTS radical scavenging activity. Primary phytochemical and micro-macro element was tested using standard protocol. The chemical characterization was done with the help of Gas Chromatography-Mass Spectrometry (GC–MS), and the mass spectra of the total compounds in the extract were matched with the National Institute of Standard and Technology (NIST) library. Mineral constituents were identified and estimated by ICP-OES. Ninety-nine metabolites were obtained by GC-MS anslysis; indole was found to be major components followed by 2-Chlorallyl diethyldithiocarbamate (CDEC), Carbaril, Bis(2-ethylhexyl) phthalate, Quinoline, 4H-Cyclopenta[def]phenanthrene,2-[Bis(2-chloroethylamino)]-tetrahydro-2H-1,3,2-oxazaphosphorine-2-oxide, Phenobarbital, 1H-Indole, 2-methyl-, 2,3,7,8-Tetrachlorodibenzo-p-dioxin Disulfide, diphenyl. The presence of various bioactive compounds in the extract validates the traditional medicinal uses of this plant.


2021 ◽  
Vol 33 (2) ◽  
pp. 314-318
Author(s):  
DO THI VIET HUONG ◽  
PHAN MINH GIANG ◽  
DO HUY HOANG ◽  
NGUYEN ANH PHUONG ◽  
TRIEU ANH TRUNG

Plantago major L. in Vietnam was investigated for its chemical composition and also evaluated the biological activities against enzyme α- glucosidase and free radicals activities. The powder mixture of dried leave and roots of this species was extracted separately by three solvents: dichloromethane, water, water:alcohol (50:50, v:v). The chemical composition of dichloromethane extract was analyzed by GC-MS system to identify eighteen components, out of which eight biologically active compounds viz. 5-hydroxymethylfurfural, n-hecxadecanoic acid, 9,12-octadecadienoic acid (Z,Z)-methyl ester, allogibberic acid, β-tocopherol, campesterol, γ-sitosterol, lup-20(29)-en-3-ol and friedenlan-3-one were presented. The concentration of radical scavenging activity DPPH expressed by IC50 for water, water:alcohol (50:50, v:v) and dichloromethane with 208.7, 89.3 and 62.05 μg/mL, respectively. The dichloromethane, water and water:alcohol (50:50, v:v) extract of Plantago major exhibited α-glucosidase inhibitory activity with IC50 values of 116.4, 302.7, 195.9 μg/mL, respectively, which was comparable with acarbose (98.4 μg/mL). Plantago major L. in Vietnam may be effective inhibitors as the antidiabetic candidate and helpful to reduce the postprandial glucose levels.


Plants ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 2626
Author(s):  
Wael Sobhy Darwish ◽  
Abada El Sayed Khadr ◽  
Maher Abd El Naby Kamel ◽  
Mabrouk A. Abd Eldaim ◽  
Ibrahim El Tantawy El Sayed ◽  
...  

Ceratonia siliqua (Carob) is an evergreen Mediterranean tree, and carob pods are potentially nutritive and have medicinal value. The present study was carried out to estimate the possible biological activities of phytochemical-characterized carob pod aqueous extract (CPAE). The phytochemical contents of CPAE were determined by using colorimetric methods and HPLC. In addition, the free radical scavenging properties and anti-diabetic, anti-hemolytic, and antimicrobial activities were estimated by using standardized in vitro protocols. The phytochemical analysis revealed that CPAE was rich in polyphenols, flavonoids, and alkaloids, where it contained a significant amount of gallic acid, catechin, and protocatechuic acid. Furthermore, CPAE exhibited strong antioxidant activity where it prevented the formation of 2, 2-Diphenyl-1-picryl hydrazyl, hydroxyl, and nitric oxide free radicals. Additionally, it had a potent inhibitory effect against digestive enzymes (amylase, maltase, sucrase, and lactase). Moreover, CPAE exhibited anti-Staph aureus, anti-Escherichia coli, anti-Candida albicans, and anti-herpes simplex type I virus (HSV-I). Finally, CPAE protected the erythrocyte membrane from hypotonic solution-induced hemolysis. Altogether, CPAE could be regarded as an interesting source of biologically active antioxidant, anti-diabetic, and antimicrobial preparation for a potential application in pharmaceutical and food supplement fields.


2021 ◽  
Vol 37 (4) ◽  
pp. 826-832
Author(s):  
Navneet Sinha ◽  
Rajnish Kumar ◽  
Vijay Pratap Singh ◽  
Deepak KUMAR ◽  
Shivadhar Sharma

3-Phenyl-4-methoxybenzaldehyde undergoes condensation with semicarbazide hydrochloride to form a Schiff-base i.e. 3-phenyl-4-methoxybenzaldehyde semicarbazone (abbreviated as MBS). It undergoes complexation with Vanadium(II), Manganese(II), and Copper(II). The comparison of FTIR-spectra of complexes with that of free ligand helps ascertain the coordination points of ligand through the nitrogen of –CH=N– group and oxygen of group. The axial ligands have been varied by chloride, acetate and nitrate ions. The UV/Visible and ESR spectra of complexes predicts their tetragonally distorted octahedral (D4h) symmetry. The tetragonal distortion parameter (Dt) is observed maximum for chloride while it is minimum for nitrate along z-axis. Both vanillin and semicarbazide are established biologically active compounds and hence their biological activities may be enhanced by their complexation and than a versatile field may be developed for further exploration.


Author(s):  
M. Marlin Risana ◽  
S. Balasubramaniyan ◽  
R. Govindharaju ◽  
V. Mukil Meenakshi ◽  
B. Jayalakshmi ◽  
...  

New Cobalt(II) and Nickel(II) metal complexes of 2-aminothiazole (ATZ) and benzoate ion (BEN) ligands were  synthesized under microwave irradiation. The empirical formulae and the structure of the complexes have been deduced from CHN analysis, electrical conductance, magnetic moment, electronic (DRS method), Infra Red spectra, TGA analysis, cyclic voltammetry and powder-XRD techniques. The low electrical conductance values indicate that the complexes are non-electrolyte (1:0) type. The electronic spectra and the magnetic moment indicate the structures of the complexes are found to be octahedral geometry. Infra Red spectra illustrate that 2-aminothiazole and benzoate ion is bonded to the metal ion in a monodentate approach. The antifungal activities of ligands and their cobalt(II) and nickel(II) metal complexes were studied aligned with the few microorganisms by agar - well diffusion method at 100,200 and 400 conc. µg/ml concentration.  The prepared cobalt(II) and nickel(II) metal complexes show prospective action against the tested fungi as compared to free 2-aminothiazole ligand. The free radical scavenging action of the prepared complexes and the ligand has been resolute by measuring their interface with the stable free radical DPPH. The complexes have larger antioxidant activity as compared to the free ligand. DNA-binding properties have been calculated by fluorescence-emissions method. The obtained results suggest that the complexes powerfully bind to DNA because of metal complexes are well-known to speed up the drug action and the capability of healing agent which can repeatedly be enhanced leading coordination with a metal ion.


Author(s):  
Harish Rajak ◽  
Murli Dhar Kharya ◽  
Pradeep Mishra

There are vast numbers of pharmacologically active heterocyclic compounds in regular clinical use. The presence of heterocyclic structures in diverse types of compounds is strongly indicative of the profound effects such structure exerts on physiologic activity, and recognition of this is abundantly reflected in efforts to find useful synthetic drugs. The 1,3,4-oxadiazole nucleus has emerged as one of the potential pharmacophore responsible for diverse pharmacological properties. Medical Literature is flooded with reports of a variety of biological activities of 2,5-Disubstituted-1,3,4-oxadiazoles. The present work is an attempt to summarize and enlist the various reports published on biologically active 2,5-disubstituted-1,3,4-oxadiazoles.


2019 ◽  
Vol 25 (37) ◽  
pp. 4888-4902 ◽  
Author(s):  
Gilda D'Urso ◽  
Sonia Piacente ◽  
Cosimo Pizza ◽  
Paola Montoro

The consumption of berry-type fruits has become very popular in recent years because of their positive effects on human health. Berries are in fact widely known for their health-promoting benefits, including prevention of chronic disease, cardiovascular disease and cancer. Berries are a rich source of bioactive metabolites, such as vitamins, minerals, and phenolic compounds, mainly anthocyanins. Numerous in vitro and in vivo studies recognized the health effects of berries and their function as bioactive modulators of various cell functions associated with oxidative stress. Plants have one of the largest metabolome databases, with over 1200 papers on plant metabolomics published only in the last decade. Mass spectrometry (MS) and NMR (Nuclear Magnetic Resonance) are the most important analytical technologies on which the emerging ''omics'' approaches are based. They may provide detection and quantization of thousands of biologically active metabolites from a tissue, working in a ''global'' or ''targeted'' manner, down to ultra-trace levels. In the present review, we highlighted the use of MS and NMR-based strategies and Multivariate Data Analysis for the valorization of berries known for their biological activities, important as food and often used in the preparation of nutraceutical formulations.


2019 ◽  
Vol 23 (8) ◽  
pp. 860-900 ◽  
Author(s):  
Chander P. Kaushik ◽  
Jyoti Sangwan ◽  
Raj Luxmi ◽  
Krishan Kumar ◽  
Ashima Pahwa

N-Heterocyclic compounds like 1,2,3-triazoles serve as a key scaffolds among organic compounds having diverse applications in the field of drug discovery, bioconjugation, material science, liquid crystals, pharmaceutical chemistry and solid phase organic synthesis. Various drugs containing 1,2,3-triazole ring which are commonly available in market includes Rufinamide, Cefatrizine, Tazobactam etc., Stability to acidic/basic hydrolysis along with significant dipole moment support triazole moiety for appreciable participation in hydrogen bonding and dipole-dipole interactions with biological targets. Huisgen 1,3-dipolar azide-alkyne cycloaddition culminate into a mixture of 1,4 and 1,5- disubstituted 1,2,3-triazoles. In 2001, Sharpless and Meldal came across with a copper(I) catalyzed regioselective synthesis of 1,4-disubstituted 1,2,3-triazoles by cycloaddition between azides and terminal alkynes. This azide-alkyne cycloaddition has been labelled as a one of the important key click reaction. Click synthesis describes chemical reactions that are simple to perform, gives high selectivity, wide in scope, fast reaction rate and high yields. Click reactions are not single specific reaction, but serve as a pathway for construction of simple to complex molecules from a variety of starting materials. In the last few decades, 1,2,3-triazoles attracted attention of researchers all over the world because of their broad spectrum of biological activities. Keeping in view the biological importance of 1,2,3-triazole, in this review we focus on the various synthetic routes for the syntheisis of 1,4-disubstituted 1,2,3-triazoles. This review involves various synthetic protocols which involves copper and non-copper catalysts, different solvents as well as substrates. It will boost synthetic chemists to explore new pathway for the development of newer biologically active 1,2,3-triazoles.


2019 ◽  
Vol 20 (15) ◽  
pp. 1309-1320 ◽  
Author(s):  
Ahmed M. Younis ◽  
Marwa M. Abdel-Aziz ◽  
Mohamed Yosri

Background:: Mushrooms are deemed as a special delicacy in many countries. They are considered an important cuisine due to their bioactive ingredients and possible health benefits. Methods: Herein, we measured selected biological properties of methanol extracts of Pleurotus citrinopileatus and Boletus edulis fruiting bodies including; in vitro antimicrobial activity, anti-α- glucosidase activity, antioxidant activity, anti-lipase activity and cytotoxic activity against different cancer cells and normal cells. Results: B. edulis methanol extracts showed high antimicrobial and anti-α-glucosidase activity. In contrast, P. citrinopileatus methanol extracts showed superior antioxidant activity indicated by (1,1- diphenyl-2-picrylhydrazyl) DPPH radical scavenging with half maximal inhibitory concentration of IC50 37.4 µg/ml, anti-lipase activities with IC50 65.2 µg/ml and high cytotoxicity activity against HepG2 and HeLa cell lines with IC50 22.8 and 36.7 µg/ml, respectively. Flow cytometric analysis of the cell cycle was used to show apoptotic effects of methanol extracts against HepG2 and HeLa cells. Conclusion: P. citrinopileatus and B. edulis methanolic extracts appear to contain biologically active compounds that might be used to treat some common human diseases.


2020 ◽  
Vol 24 (14) ◽  
pp. 1555-1581
Author(s):  
Garima Tripathi ◽  
Anil Kumar Singh ◽  
Abhijeet Kumar

Among the major class of heterocycles, the N-heterocycles, such as pyrazoles, are scaffolds of vast medicinal values. Various drugs and other biologically active molecules are known to contain these N-heterocycles as core motifs. Specifically, arylpyrazoles have exhibited a diverse range of biological activities, including anti-inflammatory, anticancerous, antimicrobial and various others. For instance, arylpyrazoles are present as core moieties in various insecticides, fungicides and drugs such as Celebrex and Trocoxil. The present review will be highlighting the significant therapeutic importance of pyrazole derivatives developed in the last few years.


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