DNA Interaction and Biological Activities of Heteroleptic Palladium (II) Complexes

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
Keyword(s):  
Biological Activities ◽  
Thiobarbituric Acid ◽  
Dna Interaction ◽  
Log P ◽  
Bacterial Strains ◽  
Experimental Conditions ◽  
H2o2 Treatment ◽  
Biological Studies ◽  
Almost All ◽  
Anti Fungal

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.

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 ◽  
...  
Keyword(s):  
Aromatic Amines ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Dna Interaction ◽  
Chemopreventive Agents ◽  
H Nmr ◽  
Highly Active ◽  
Free Radical Scavenging Assay ◽  
Almost All ◽  
Antibacterial And Antifungal

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.

scholarly journals Synthesis, Crystal Structure, Antioxidant, Antimicrobial, and Mutagenic Activities and DNA Interaction Studies of Ni(II) Schiff Base 4-Methoxy-3-benzyloxybenzaldehyde Thiosemicarbazide Complexes

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
P. R. Chetana ◽  
M. N. Somashekar ◽  
B. S. Srinatha ◽  
R. S. Policegoudra ◽  
S. M. Aradhya ◽  
...  
Keyword(s):  
Biological Activities ◽  
Radical Scavenging ◽  
Dna Interaction ◽  
Significant Activity ◽  
Square Planar ◽  
Biological Studies ◽  
Square Planar Complexes ◽  
Free Radical Scavenging Assay ◽  
Heterocyclic Bases ◽  
Dna Binding And Cleavage

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.

MICROWAVE ASSISTED SYNTHESIS OF BIPHENYL BASED SCHIFF’S BASES AND THEIR ANTIMICROBIAL EVALUATION

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (03) ◽  
pp. 13-18
Author(s):  
R. Somani ◽  
◽  
P. Dubey ◽  
S. Zine
Keyword(s):  
Biological Activities ◽  
Biological Membrane ◽  
Log P ◽  
Microwave Assisted Synthesis ◽  
Schiff’S Bases ◽  
Schiff’S Base ◽  
Schiff's Bases ◽  
Phenyl Rings ◽  
Antimicrobial Evaluation ◽  
Anti Fungal

Schiff’s base constitutes a significant class of compounds for new drug development. They are widely used for industrial purposes and also exhibit a broad range of biological activities. The search for Schiff’s base containing compounds with more selective activity and lower side effects continues to be an active area of argument examination in medicinal chemistry. The biphenyl molecule consists of two connected phenyl rings. Biphenyl ring scaffolds are fairly non-reactive in nature. They enhance the log-P values; increase the tropical polar surface area (TPSA) of the molecule, act as hydrophobic carrier across biological membrane, thus, increasing the bioavailability of compounds. In the present work, a series of Schiff’s bases of biphenyl-4-carboxylic acid have been synthesized. These derivatives were characterized by elemental analysis, IR, and 1H NMR spectral data and have been explored for anti-bacterial, anti-fungal and anti-tubercular activities. The synthesized compounds have shown excellent anti-fungal potential, making them good candidates for future studies in antifungal research.

A Simple Method for Estimation of Lipoxygenase and Cyclo-Oxygenase Pathways in Human Platelets - the Use of Thiobarbituric Acid Reaction

1980 ◽  
Vol 44 (02) ◽  
pp. 111-114 ◽  
Author(s):  
Hiroshi Takayama ◽  
Minoru Okuma ◽  
Haruto Uchino
Keyword(s):  
Time Course ◽  
Normal Values ◽  
Human Platelet ◽  
Thiobarbituric Acid ◽  
Human Platelets ◽  
Optimal Conditions ◽  
Experimental Conditions ◽  
Simple Method ◽  
Acid Reaction ◽  
Optimal Ph

SummaryTo develop a simple method for estimation of platelet lipoxygenase (PLO) and cyclo-oxygenase (PCO) pathways, the arachidonic acid (AA) metabolism of human platelet was investigated under various experimental conditions by the use of the thiobarbituric acid (TBA) reaction and a radioisotope technique. A TBA-reactive substance different from malondialdehyde (MDA) via PCO pathway was detected and shown to be derived from the PLO pathway. Since the optimal pH and time course of its formation were different from those of MDA formation via PCO pathway, PLO and PCO pathways were estimated by quantitating the TBA-reactive substances produced by the incubation of AA either with aspirin-treated platelets or with untreated ones, respectively, each under optimal conditions. Normal values expressed in terms of nmol MDA/108 platelets were 1.17±0.34 (M±SD, n = 31) and 0.79±0.15 (n = 31) for PLO and PCO pathways, respectively.

Recent Developments on Synthesis of Indole Derivatives Through Green Approaches and Their Pharmaceutical Applications

2020 ◽  
Vol 24 (22) ◽  
pp. 2665-2693
Author(s):  
Dipayan Mondal ◽  
Pankaj Lal Kalar ◽  
Shivam Kori ◽  
Shovanlal Gayen ◽  
Kalpataru Das
Keyword(s):  
Biological Activities ◽  
Synthetic Methods ◽  
Pharmaceutical Chemistry ◽  
Indole Derivatives ◽  
Biological Studies ◽  
Recent Developments ◽  
Pharmaceutical Industries ◽  
Green Methodology ◽  
Conventional Methods ◽  
High Yields

Indole moiety is often found in different classes of pharmaceutically active molecules having various biological activities including anticancer, anti-viral, anti-psychotic, antihypertensive, anti-migraine, anti-arthritis and analgesic activities. Due to enormous applications of indole derivatives in pharmaceutical chemistry, a number of conventional synthetic methods as well as green methodology have been developed for their synthesis. Green methodology has many advantages including high yields, short reaction time, and inexpensive reagents, highly efficient and environmentally benign over conventional methods. Currently, the researchers in academia as well as in pharmaceutical industries have been developing various methods for the chemical synthesis of indole based compounds via green approaches to overcome the drawbacks of conventional methods. This review reflects the last ten years developments of the various greener methods for the synthesis of indole derivatives by using microwave, ionic liquids, water, ultrasound, nanocatalyst, green catalyst, multicomponent reaction and solvent-free reactions etc. (please see the scheme below). Furthermore, the applications of green chemistry towards developments of indole containing pharmaceuticals and their biological studies have been represented in this review.

Studies on antibacterial potential and phytochemical screening of different extract of Achyranthes aspera

2016 ◽  
Vol 5 (12) ◽  
pp. 5138
Author(s):  
Shyamji Shukla* ◽  
Priyanka Soni ◽  
Harish K. Kewat
Keyword(s):  
Methanolic Extract ◽  
Salmonella Typhi ◽  
Maximum Activity ◽  
Phytochemical Screening ◽  
Bacterial Strains ◽  
Antibacterial Compounds ◽  
Achyranthes Aspera ◽  
Biological Sources ◽  
Almost All ◽  
Antibacterial Potential

There is an alarming increase in the problem of resistance towards antibiotics amongst most of the pathogenic bacterial strains in recent years. This has drawn the attention of researchers around the world to search for novel and eco-friendly antibacterial compounds. Several biological sources have been explored in this respect but medicinal plants have taken a centre stage out of all. Plants have been known as a reservoir of number of bioactive compounds specially the antibacterial ones since time immemorial. Therefore, the present investigation was undertaken to analyze the antibacterial potential of the medicinal plant Achyranthes aspera. This study revealed that highest antibacterial activity was observed in the methanolic extract of stem against almost all test Bacteria. It showed maximum activity against E.coli (30 mm), followed by S. aureus (28 mm), Enterococcus sp.(25mm), Salmonella typhi ( 20 mm) and least activity was recorded in same extract against K.pneumoniae (6 mm). Four phytochemicals were screened in various solvent extracts. They are alkaloid, flavonoids, saponins and tannins.

scholarly journals Protein tyrosine phosphatase receptor type C (PTPRC or CD45)

2021 ◽  
pp. jclinpath-2020-206927
Author(s):  
Maryam Ahmed Al Barashdi ◽  
Ahlam Ali ◽  
Mary Frances McMullin ◽  
Ken Mills
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Protein Tyrosine Kinase ◽  
Biological Activities ◽  
Tyrosine Phosphatase ◽  
Cell Types ◽  
Receptor Type ◽  
Future Research ◽  
Protein Tyrosine ◽  
Type C ◽  
Almost All

The leucocyte common antigen, protein tyrosine phosphatase receptor type C (PTPRC), also known as CD45, is a transmembrane glycoprotein, expressed on almost all haematopoietic cells except for mature erythrocytes, and is an essential regulator of T and B cell antigen receptor-mediated activation. Disruption of the equilibrium between protein tyrosine kinase and phosphatase activity (from CD45 and others) can result in immunodeficiency, autoimmunity, or malignancy. CD45 is normally present on the cell surface, therefore it works upstream of a large signalling network which differs between cell types, and thus the effects of CD45 on these cells are also different. However, it is becoming clear that CD45 plays an essential role in the innate immune system and this is likely to be a key area for future research. In this review of PTPRC (CD45), its structure and biological activities as well as abnormal expression of CD45 in leukaemia and lymphoma will be discussed.

scholarly journals Diversity of Biodeteriorative Bacterial and Fungal Consortia in Winter and Summer on Historical Sandstone of the Northern Pergola, Museum of King John III’s Palace at Wilanow, Poland

2021 ◽  
Vol 11 (2) ◽  
pp. 620
Author(s):  
Magdalena Dyda ◽  
Agnieszka Laudy ◽  
Przemyslaw Decewicz ◽  
Krzysztof Romaniuk ◽  
Martyna Ciezkowska ◽  
...  
Keyword(s):  
Seasonal Changes ◽  
Microbial Community Composition ◽  
Fungal Communities ◽  
Bacterial Strains ◽  
Microbial Biodiversity ◽  
Acidophilic Bacteria ◽  
Almost All ◽  
Generation Sequencing ◽  
King John

The aim of the presented investigation was to describe seasonal changes of microbial community composition in situ in different biocenoses on historical sandstone of the Northern Pergola in the Museum of King John III’s Palace at Wilanow (Poland). The microbial biodiversity was analyzed by the application of Illumina-based next-generation sequencing methods. The metabarcoding analysis allowed for detecting lichenized fungi taxa with the clear domination of two genera: Lecania and Rhinocladiella. It was also observed that, during winter, the richness of fungal communities increased in the biocenoses dominated by lichens and mosses. The metabarcoding analysis showed 34 bacterial genera, with a clear domination of Sphingomonas spp. across almost all biocenoses. Acidophilic bacteria from Acidobacteriaceae and Acetobacteraceae families were also identified, and the results showed that a significant number of bacterial strains isolated during the summer displayed the ability to acidification in contrast to strains isolated in winter, when a large number of isolates displayed alkalizing activity. Other bacteria capable of nitrogen fixation and hydrocarbon utilization (including aromatic hydrocarbons) as well as halophilic microorganisms were also found. The diversity of organisms in the biofilm ensures its stability throughout the year despite the differences recorded between winter and summer.

scholarly journals Beehive Products as Antibacterial Agents: A Review

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 717
Author(s):  
Rita Abou Nader ◽  
Rawan Mackieh ◽  
Rim Wehbe ◽  
Dany El El Obeid ◽  
Jean Marc Sabatier ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Honey Bee ◽  
Antibacterial Agents ◽  
Royal Jelly ◽  
Biological Activities ◽  
Vital Role ◽  
Bee Venom ◽  
Bacterial Strains ◽  
Wide Range ◽  
Life Threatening

Honeybees are one of the most marvelous and economically beneficial insects. As pollinators, they play a vital role in every aspect of the ecosystem. Beehive products have been used for thousands of years in many cultures for the treatment of various diseases. Their healing properties have been documented in many religious texts like the Noble Quran and the Holy Bible. Honey, bee venom, propolis, pollen and royal jelly all demonstrated a richness in their bioactive compounds which make them effective against a variety of bacterial strains. Furthermore, many studies showed that honey and bee venom work as powerful antibacterial agents against a wide range of bacteria including life-threatening bacteria. Several reports documented the biological activities of honeybee products but none of them emphasized on the antibacterial activity of all beehive products. Therefore, this review aims to highlight the antibacterial activity of honey, bee venom, propolis, pollen and royal jelly, that are produced by honeybees.

scholarly journals Spectroscopic Study of the Molecular Structure of the New Hybrid with a Potential Two-Way Antibacterial Effect

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1442
Author(s):  
Dorota Kowalczuk ◽  
Agata Gładysz ◽  
Monika Pitucha ◽  
Daniel M. Kamiński ◽  
Agnieszka Barańska ◽  
...  
Keyword(s):  
Spectroscopic Study ◽  
Good Alternative ◽  
Structure Characterization ◽  
Resonance Spectroscopy ◽  
Spectroscopic Techniques ◽  
Bacterial Strains ◽  
Active Components ◽  
Hybrid Compound ◽  
Coordination Sites ◽  
Almost All

Bacterial strains become resistant to almost all classes of antibiotics, which makes it necessary to look for new substitutes. The non-absorbable ciprofloxacin–biguanide bismuth complex, used locally, may be a good alternative to a conventional therapy. The purpose of this study was to study the structure of the proposed ciprofloxacin (CIP) -bismuth(III)—chlorhexidine (CHX) composite (CIP-Bi-CHX). The spectroscopic techniques such as UV-VIS (ultraviolet-visible) spectroscopy, FTIR (Fourier-transform infrared) spectroscopy and NMR (Nuclear Magnetic Resonance) spectroscopy were used for structure characterization of the hybrid compound. The performed analysis confirmed the presence of the two active components—CIP and CHX and revealed the possible coordination sites of the ligands with bismuth ion in the metallo-organic structure. Spectroscopic study showed that the complexation between Bi(III) and CIP occurs through the carboxylate and ketone groups of the quinolone ring, while CHX combines with the central ion via the biguanide moieties.

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