In this article, we report two indole-based metal-free organic dyes In-T-2C (3-(5-(3-((2-carboxy-2-cyanovinyl)-1-pentyl-1-indol-5-yl)thiophen-2-yl)-2-isocyanoacrylic acid) and In-B-C (2-cyano-3-(5-(4-cyanophenyl)-1-pentyl-1-indol-3-yl)acrylic acid) with A-π-D-A architecture. The molecular structures of metal-free indole-based A-π-D-A organic dyes were elucidated using FT-IR, NMR, HRMS and single-crystal X-ray diffraction techniques. The present investigation examined the features of the synthesized dyes employing photophysical attributes, electrochemical traits and theoretical studies were executed to acquire a detailed comprehension of the geometry, electronic structure and absorption spectra of the synthesized dyes using density functional theory (DFT) and time-dependent density functional theory (TD-DFT).
View Article and Find Full Text PDFIntroduction: Among the upper limb's vascular variations, the radial artery's high origin from the axillary artery is rare, and literature regarding the same is limited. Anomalous origin of radial artery can cause failure of radial approach to coronary angiography and reconstructive surgeries of upper limbs and hence is of clinical significance. With this background, the current cadaveric study was planned to describe the branching pattern of the axillary artery and its variations.
View Article and Find Full Text PDFChalcones (trans-1,3-diphenyl-2-propen-1-ones) form simple chemical structures that act as precursors for the biogenesis of flavonoids. These are distributed in plants and have two aromatic or heteroaromatic rings connected by a three-carbon α, β-unsaturated carbonyl group. Considering the importance of chalcones as monoamine oxidase and acetylcholinesterase inhibitors, the study was designed as a comprehensive and systematic analysis to evaluate the pharmacological activities leading to the formation of drug molecules against Alzheimer's disease (AD).
View Article and Find Full Text PDFBackground: Over the last few years, the importance of leptin in energy metabolism has been extensively studied in both animal models and in humans. Very few results are available on the association between human leptin gene () variants and obesity traits in India. We designed this study to analyse the polymorphisms in human leptin gene and the association of sequence variants with obesity among the population in Kerala, South India.
View Article and Find Full Text PDFPlant-mediated nanoparticle synthesis is a revolutionary technique with numerous applications in fields, such as agriculture, food processing, and medicine. This study reports that Punica granatum leaf extract is capable of the green and eco-friendly synthesis of silica nanoparticles that provides a simple, cost-effective, and efficient methodology. P.
View Article and Find Full Text PDFIn this study, we report the development and validation of an LC-tandem mass spectrometry method for the simultaneous quantitation of bendamustine and copanlisib in mouse plasma as per the US FDA regulatory guidelines. The sample processing involves extraction of bendamustine and copanlisib along with internal standard (IS; warfarin) from 50 μL mouse plasma using a liquid-liquid extraction method. The chromatographic separation of bendamustine, copanlisib and the IS was achieved on an Atlantis dC column using an isocratic mobile phase (5 mM ammonium acetate:methanol, 20:80 v/v).
View Article and Find Full Text PDFNine compounds () containing the morpholine moiety were assessed for their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE). Most of the compounds potently inhibited MAO-B; most potently inhibited with an IC value of 0.030 µM, followed by (0.
View Article and Find Full Text PDFTreatment of inflammation using NSAIDs is coupled with a risk of severe gastric adverse events. Development of dual COX-2/5-LOX inhibitors turns out to be an imperative area devoted to safer NSAIDs. A series of thiourea, thiazole, and thiazolidene derivatives were synthesized by green synthetic approach and COX-1, COX-2 and 5-LOX inhibition screening resulted in the identification of a potent compound 6l with IC of 5.
View Article and Find Full Text PDFA hybrid pharmacophore approach is used to design and synthesize novel chalcone-thiazole hybrid molecules. Herein, thiazole has been hybridized with chalcone to obtain a new class of 5-LOX inhibitors. biological evaluation showed that most of the compounds were better 5-LOX inhibitors than the positive control, Zileuton (IC = 1.
View Article and Find Full Text PDFThe most common inflammatory disease of the airways is asthma among children affecting around 235 million people worldwide. 5-Lipoxygenase (5-LOX) is a crucial enzyme which helps in the conversion of arachidonic acid (AA) to leukotrienes (LTs), the lipid mediators. It is associated with several inflammation related disorders such as asthma, allergy, and atherosclerosis.
View Article and Find Full Text PDFHuman 5-Lipoxygenase (5-LOX) is a key enzyme targeted for asthma and inflammation. Zileuton, the only drug against 5-LOX, was withdrawn from the market due to several problems. In the present study, the performance of rationally designed conjugates of thiazole (2) and thiourea (3) scaffolds from our previously reported 2-amino-4-aryl thiazole (1) is reported.
View Article and Find Full Text PDFInflammatory mediators of the arachidonic acid cascade from cyclooxygenase (COX) and lipoxygenase (LOX) pathways are primarily responsible for many diseases in human beings. Chronic inflammation is associated with the pathogenesis and progression of cancer, arthritis, autoimmune, cardiovascular and neurological diseases. Traditional non-steroidal anti-inflammatory agents (tNSAIDs) inhibit cyclooxygenase pathway non-selectively and produce gastric mucosal damage due to COX-1 inhibition and allergic reactions and bronchospasm resulting from increased leukotriene levels.
View Article and Find Full Text PDFA series of 11 indole-based chalcones (IC1-11) with various electron donating and withdrawing groups at the para position of the phenyl ring B were synthesized. All the compounds were tested for their human monoamine oxidase (hMAO)-A and hMAO-B inhibitory potencies. Most of the synthesized candidates proved to be potent and selective inhibitors of MAO-B rather than MAO-A, with a reversible and competitive mode.
View Article and Find Full Text PDFGenerally, heterocycles occupy a prominent place in chemistry due to their wide range of applications in the fields of drug design, photochemistry, agrochemicals, dyes and so on. Among them, indole scaffolds have been found in most of the important synthetic drug molecules and paved a faithful way to develop effective targets. Privileged structures bind to multiple receptors with high affinity, thus aiding the development of novel biologically active compounds.
View Article and Find Full Text PDFThe anti-Vibrio activity of essential oils (EOs) of nine medicinal plants was tested against 28 Vibrio spp. isolated from diseased Fenneropenaeus indicus. EO of Nigella sativa exhibited anti-Vibrio activity against all Vibrio spp.
View Article and Find Full Text PDFThis study reports the biological synthesis of gold nanoparticles using essential oil of Nigella sativa (NsEO-AuNPs). The synthesized NsEO-AuNPs were characterized by UV-visible spectra, X-ray diffraction (XRD), FTIR and Transmission electron microscopy (TEM). UV-vis spectra of NsEO-AuNPs showed strong absorption peak at 540 nm.
View Article and Find Full Text PDFNovel photoactive 4-(4-chlorophenyl)-2-(1H-indol-3-yl)-6-substituted phenyl-2H-thiazolo[3,2-a][1,3,5]triazines were synthesized by the conjugate addition of ammonia to the indole-3-carbaldehyde Schiff bases followed by the condensation with 4-chlorobenzaldehyde. All the synthesized compounds were characterized by FT-IR, NMR, mass spectra and elemental analyses. Their antioxidant property, electrochemical and photophysical properties in different organic solvents were investigated.
View Article and Find Full Text PDFThe present study was aimed to investigate in vitro α-glucosidase inhibition, antioxidant, anticancer, and antimycobacterial activities of the ethyl acetate extract of A. tamilnadensis leaves. The extract recorded strong α-glucosidase inhibition with an IC50 value of 100 μg/ml.
View Article and Find Full Text PDFThe cDNA sequence of peroxinectin was obtained from the haemocytes of Indian white shrimp Fenneropenaeus indicus using RT-PCR and RACE. Fenneropenaeus indicus peroxinectin (Fi-Pxn) sequence has an open reading frame (ORF) of 2415 bp encoding a protein of 804 amino acids with 21 residues signal sequence. The mature protein has molecular mass of 89.
View Article and Find Full Text PDFAstragalin was isolated for the first time along with (-)hinokinin, aristolactam I and aristolochic acids (I & II) from the extracts of Aristolochia indica L. using a new, efficient preparative HPLC method. A reversed-phase HPLC method of analysis was developed to analyse the isolated compounds.
View Article and Find Full Text PDFBackground: The present study of 238 B-cell Chronic Lymphocytic Leukemia (B-CLL) patients were undertaken to seek the prevalence and to evaluate clinico-pathological significance of recurrent genetic abnormalities such as del(13q14.3), trisomy 12, del(11q22.3) (ATM), TP53 deletion, del(6q21) and IgH translocation/deletion.
View Article and Find Full Text PDFThe antimicrobial efficacy of two phenanthroindolizidine alkaloids, tylophorinidine hydrochloride (TdnH) and tylophorinine hydrochloride (TnnH), isolated from the plant Tylophora indica (local name, Antamul) was evaluated. These were screened for in vitro antifungal and antibacterial activities. Both compounds exhibited potent antifungal activity displaying minimum inhibitory concentrations (MIC) in the range of 2-4 microg/mL for TdnH and 0.
View Article and Find Full Text PDFCurcumin (Cur) shows low anticancer activity in vivo due to its reduced systemic bioavailability stemmed from its poor aqueous solubility and instability. Suitably functionalized nanocarriers designed to empty the drug specifically at tumor sites can potentially enhance the antitumor activity of Cur. We devised a simple method for the fabrication of water soluble Cur conjugated gold nanoparticles to target various cancer cell lines.
View Article and Find Full Text PDFBackground: Strong proof-of-principle for utilisation of diffuse reflectance spectroscopy, a non-invasive tool for early detection of malignant changes, has emerged recently. The potential of this technique in distinguishing normal tissue from hyperplastic and dysplastic tissues was explored.
Methods: Diffuse reflectance (DR) spectra in the 400-700 nm region were obtained from the buccal mucosa of 96 patients and 34 healthy volunteers.