Synthesis of 6-ethoxyphenyl 4-fluorobenzenesulfonate-tagged thiosemicarbazones as carbonic anhydrase inhibitors: In-vitro and in silico approach.

In this study, a series of 6-ethoxyphenyl-4-fluorobenzenesulphonate-based thiosemicarbazones (5a-w) were synthesized via a two-step process and structurally characterized by H NMR and C NMR spectroscopy. Their inhibitory activities against human carbonic anhydrase isoforms I and II (hCA I and hCA II) were evaluated, revealing potent inhibition at low nanomolar concentrations with IC values ranging from 56.36 to 230.

Synthesis, Anti-Alzheimer Evaluation and In Silico Study of 4-Methoxyphenyl)Sulfonyl Indole Hybrid Thiosemicarbazones.

Alzheimer's disease (AD) is a multifaceted neurological disorder linked to behavioral, psychological, and language abnormalities as well as memory loss. A series of 1-[(4-methoxyphenyl)sulfonyl]-1H-indole-3-carbaldehyde-based thiosemicarbazones 5(a-v) had been synthesized and screened for their potential against AD. The compounds were tested for their inhibitory effects against cholinesterases (AChE and BChE) and monoamine oxidase A (MAO-A).

Synergistic application of IAGS174 and thiamine to mitigate salinity and lead stress in .

The increasing soil contamination with salinity and heavy metals poses serious threats to the cultivation of economically and ornamentally important plants such as (Sunflower). IAGS174 and thiamine are well known for their role in increasing plant stress tolerance levels by multiple mechanisms. The present research aimed to assess the effect of IAGS174 and thiamine on under salinity and lead (Pb) stress by analyzing the growth parameters, physiological markers, and biochemical assays.

Design, synthesis, , and studies of novel isatin-hybrid hydrazones as potential triple-negative breast cancer agents.

Recent advances in cancer therapy have been made possible by monoclonal antibodies, domain antibodies, antibody drug conjugates, The most impact has come from controlling cell cycle checkpoints through checkpoint inhibitors. This manuscript explores the potential of a series of novel -benzyl isatin based hydrazones (5-25), which were synthesized and evaluated as anti-breast cancer agents. The synthesized hydrazones of -benzyl isatin were screened against two cell lines, the MDA-MB-231 breast cancer cell line and the MCF-10A breast epithelial cell line.

Unlocking Nature's Potential: Ferritin as a Universal Nanocarrier for Amplified Cancer Therapy Testing via 3D Microtissues.

In the existing development of extensive drug screening models, 3D cell cultures outshine conventional 2D monolayer cells by closely imitating the in vivo tumor microenvironment. This makes 3D culture a more physiologically relevant and convenient system in the regime of preclinical drug testing. In the nanomedicinal world, nanoconjugates as nanocarriers are largely hunted due to their capability of precisely binding to target cells and distributing essential dosages of therapeutic drugs with enhanced safety profiles.

Phytochemical Characterization and Assessment of Crude Extracts from for Phytotoxic and Cytotoxic Activity.

Background: The aim of the study was to investigate the cytotoxicity, phytotoxicity, and proximate and phytochemical analysis of methanolic extracts of the leaves of .

Methods: Methanolic leaf extract of was screened for phytotoxic activity by using root length inhibition and seed germination assays. Cytotoxic activity was calculated using brine shrimp lethality bioassay.

A Microfluidics-Assisted Double-Barreled Nanobioconjugate Synthesis Introducing Aprotinin as a New Moonlight Nanocarrier Protein: Tested toward Physiologically Relevant 3D-Spheroid Models.

Proteins are promising substances for introducing new drug carriers with efficient blood circulation due to low possibilities of clearance by macrophages. However, such natural biopolymers have highly sophisticated molecular structures, preventing them from being assembled into nanoplatforms with manipulable payload release profiles. Here, we report a novel anticancer nanodrug carrier moonlighting protein, Aprotinin, to be used as a newly identified carrier for cytotoxic drugs.

One-Step Synthesis of Ultrasmall Nanoparticles in Glycerol as a Promising Green Solvent at Room Temperature Using Omega-Shaped Microfluidic Micromixers.

Despite innovations in the synthesis protocol of nanoparticles (NPs), the size distribution and uniformity of particles still remain as crucial attributes. Homogeneous and rapid nucleation is a critical phenomenon to obtain monodisperse nanoparticles. Herein, we have carried out the synthesis of metal nanoparticles in a customized microfluidic (MF) chip, with 18 omega-shaped micromixers, by using glycerol as a promising green solvent and reducing agent at various concentrations (10-80%), and simultaneous comparison of the results from batch synthesis.

Novel Size-Tunable and Straightforward Ultra-Small Nanoparticle Synthesis in a Varying Concentration Range of Glycerol as a Green Reducing Solvent.

Despite all the possibilities available so far for the synthesis of nanoparticles (NPs), synthesizing ultra-small (<10 nm) monodispersed particles is still demanding. Getting a particular size with a straightforward method is a trial-and-error approach. To explore this prospective, in the current study, we have introduced a protocol which offers a varying concentration range of glycerol to successfully generate the NPs of repeatable and consistent particle size in each synthesis, thus giving an alternative from lengthy tentative preparations and/or testing protocols.

Viruses as tools in gene therapy, vaccine development, and cancer treatment.

Using viruses to our advantage has been a huge leap for humanity. Their ability to mediate horizontal gene transfer has made them useful tools for gene therapy, vaccine development, and cancer treatment. Adenoviruses, adeno-associated viruses, retroviruses, lentiviruses, alphaviruses, and herpesviruses are a few of the most common candidates for use as therapeutic agents or efficient gene delivery systems.

An Outline of Contributing Vaccine Technologies for SARS CoV2 Advancing in Clinical and Preclinical Phase-Trials.

Background: Severe Acute Respiratory Syndrome Coronavirus 2 (SARS CoV2) is an RNA virus involving 4 structural and 16 non-structural proteins, and exhibiting high transmission potential and fatality. The emergence of this newly encountered beta coronavirus-SARS CoV2 has brought over 2 million people to death, and more than 10 billion people got infected across the globe as yet. Consequently, the global scientific community has contributed to the synthesis and design of effective immunization technologies to combat this virus.

Natural products embedded crown ethers as potent insulin secretory agents.

Natural products embedded crown ethers were prepared by utilizing bioactive natural products including chrysin, tetrahydroisoquinoline (THIQ), and biochanin-A. The prepared crown ether scaffolds were evaluated and compared with their natural product precursors for insulin secretory activity on isolated mice islets and for their fluorescent properties. All the crown adducts were found more active as compared to their natural product precursors.

Pharmacological evaluation of Vitis vinifera and Zingiber zerumbet on electrocardiographic, biochemical alterations and antioxidant status in isoproterenol-induced myocardial infarction in rats.

The Vitis vinifera (VV) and Zingiber zerumbet (ZZ) are popular functional foods which are used for the treatment of cardiovascular ailments. These possess antiproliferative, antiplatelet and antioxidant effects. The current study has been designed to ascertain their effectiveness against Isoproterenol (ISO)-induced myocardial infarction (MI).

Functional venomics of the Big-4 snakes of Pakistan.

In South Asia, the "Big-4" venomous snakes Naja naja, Bungarus caeruleus, Daboia russelii, and Echis carinatus are so-called because they are the most medically important snakes in the region. Antivenom is the only effective treatment option for snakebite envenoming but antivenom is not produced domestically in Pakistan making the country reliant on polyvalent products imported from India and Saudi Arabia. The present study investigated the toxin composition and activity of the venoms of Pakistani specimens by means of proteomic and physio/pharmacological experiments.

Correction: Acridinedione as selective flouride ion chemosensor: a detailed spectroscopic and quantum mechanical investigation.

[This corrects the article DOI: 10.1039/C7RA11974G.].

Synthetic applications and methodology development of Chan-Lam coupling: a review.

Chan-Lam coupling is one of the most popular and easy methods to perform arylation of amines (N-arylations). This cross-coupling is generally performed by reacting aryl boronate derivatives with a variety of substrates involving nitrogen containing functional groups such as amines, amides, ureas, hydrazine, carbamates. This article summarizes the synthetic applications of this reaction and the efforts of scientists to develop novel and efficient methodologies for this reaction.

Novel acridine-based thiosemicarbazones as 'turn-on' chemosensors for selective recognition of fluoride anion: a spectroscopic and theoretical study.

New thiosemicarbazide-linked acridines were prepared and investigated as chemosensors for the detection of biologically and environmentally important anions. The compounds were found selective for fluoride (F) with no affinity for other anions, i.e.

Acridinedione as selective flouride ion chemosensor: a detailed spectroscopic and quantum mechanical investigation.

The use of small molecules as chemosensors for ion detection is rapidly gaining popularity by virtue of the advantages it offers over traditional ion sensing methods. Herein we have synthesized a series of acridine(1,8)diones (7a-7l) and explored them for their potential to act as chemosensors for the detection of various anions such as fluoride (F), acetate (OAc), bromide (Br), iodide (I), bisulfate (HSO ), chlorate (ClO ), perchlorate (ClO ), cyanide (CN), and thiocyanate (SCN). Acridinediones were found to be highly selective chemosensors for fluoride ions only.

Protein-drug nanoconjugates: Finding the alternative proteins as drug carrier.

Present study was conducted to establish the interaction of bovine fetuin-A to validate its binding modalities with doxorubicin (Dox). Fetuin-A was purified to highest purity and monodispersity. Green synthesis of fetuin-A conjugated gold nanoparticles (F-GNPs) has been performed giving typical UV-maxima with subtle variation in fourier transform infrared spectroscopy (FTIR).

Formulation and stabilization of norfloxacin in liposomal preparations.

A number of liposomal preparations of norfloxacin (NF) containing variable concentrations of phosphatidylcholine (PC) (10.8-16.2mM) have been formulated and an entrapment of NF to the extent of 41.

Formulation and stabilization of riboflavin in liposomal preparations.

A study of the formulation of liposomal preparations of riboflavin (RF) with compositional variations in the content of phosphatidylcholine (PC) and their entrapment efficiency (26-42%) have been conducted. Light transmission characteristics of the liposomal preparations have been determined to evaluate their effect on the amount of light passing through the system to initiate a photochemical reaction. Dynamic light scattering (DLS) and atomic force microscopy (AFM) have been used to study the physical characteristics of liposomes.

Pharmacological and biochemical studies on the venom of a clinically important viper snake (Echis carinatus) of Pakistan.

Echis carinatus (saw-scaled viper) has been the major culprit responsible for serious envenomation casualties throughout the subcontinent. The present study describes the electrophoretic and zymographic characterization of E. carinatus venom and its effect on mammalian smooth muscle.