Enhancement of detoxification of xenobiotic aromatic amine dyes by N-acetyltransferase 1 (NAT1) enzyme on human keratinocytes cells through structural modification.

The metabolic conversion of aromatic amines to N-acetylated forms in skin and keratinocytes depends on N-acetyltransferase-1 (NAT1). Common hair color ingredient such as para-phenylenediamine (PPD) causes allergic contact dermatitis. We explored how different electronic substituents on PPD aided NAT1 enzyme biotransform oxidative arylamine (AA) compounds G1-G13 by N-acetylation, NAT-1 activity assays, metabolism, and in vitro clearance investigations in human keratinocytes, while identifying NAT-1 protein levels by Western blot and qRT-PCR.

Design, synthesis, molecular modeling and evaluation of 2,4-diaminopyrimidine analogues as promising colorectal cancer drugs.

The potential of cyclin-dependent kinases (CDKs) as therapeutic targets in cancer treatment is well established. In this study, we present our investigation into a group of 2,4-diaminopyrimidine derivatives that potently inhibit CDK9 and are cytotoxic when tested in colorectal cancer cell lines. We designed and synthesized forty analogues by altering substitutions at C-2 and C-4 position of the pyrimidine system.

Design, synthesis, molecular docking, and evaluation of sulfonyl quinazoline analogues as promising liver cancer drugs.

Inhibiting cyclin-dependent kinases (CDK) offers an important arsenal for cancer treatments by interfering with apoptotic proteins related to cancer. Novel selective cyclin-dependent kinases inhibitors using the Quinazoline as the cap with multiple electronic donating (EDG) and/or electron withdrawing group (EWG) substituted Aniline chain at the C-2 position were designed, synthesized, and evaluated for activity against liver cancer. Among the tested compounds, compounds B34 and B35 emerged as potent candidates in the series, with IC values of 0.

Genetic trans-complementation of L-protease fails to rescue the infectious foot-and-mouth disease virus from the Lb defective genome.

Outbreaks of the foot-and-mouth disease (FMD) have major economic impact on the global livestock industry by affecting the animal health and product safety. L-protease, a non-structural protein of FMDV, is a papain-like cysteine proteinase involved in viral protein processing as well as cleavage of host proteins for promoting the virus growth. FMDV synthesizes two forms of leader proteinase, L (Lab and Lb), where the deletion of Lab is lethal and Lb deletion is reported to be attenuated.

A Julolidine Aldehyde Dansyl Hydrazine Schiff Base as Fluorescence Chemosensor for Zn ions Recognition and its Application.

The Schiff base fluorescent probe (Dz-Jul), containing julolidine aldehyde and dansyl hydrazine, was derived using a simple condensation. This chemosensor showed high selectivity towards Zn and quick response (170 s) in DMSO/HO solutions (8/2, v/v, pH 7.2 buffer).

The comprehensive review on 3D printing- pharmaceutical drug delivery and personalized food and nutrition.

Three-dimensional printing is one of the emerging technologies that is gaining interest from the pharmaceutical industry as it provides an opportunity to customize drugs according to each patient's needs. Combining different active pharmaceutical ingredients, using different geometries, and providing sustained release enhances the effectiveness of medicine. One of the most innovative uses of 3D printing is producing fabrics, medical devices, medical implants, orthoses, and prostheses.

A carboethoxy quinoline-Derived Schiff base chemosensor: Crystal structure, selective Hg ion detection and its computational study.

Environmental monitoring of mercury (Hg) ions has become increasingly important as a result of their detrimental effects on biological organisms at all levels. To recognize toxic metal ions, utmost effort has been devoted to developing new materials that are highly selective, ultra-sensitive, and provide rapid response. In this context, a new chemosensor, 2-imino [N - (N-amido phenyl)]-6-methoxy-3-carbethoxy quinoline (L), has been synthesized by combining 2-formyl-6-methoxy-3-carbethoxy quinoline and benzhydrazide and it has been extensively characterized by NMR, FTIR, ESI-Mass and SCXRD analysis.

Isolation, structural elucidation of bioactive compounds and their wound-healing ability, antibacterial and In silico molecular docking applications.

Andrographis echioides has been extensively utilized in traditional Indian folk medicines for several skin disorders and other biological actions such as diuretic, antimicrobial, anthelmintic, anti-ulcer, and hepatoprotective properties. Different crude extracts were extracted from A. echioides leaves using various solvents such as methanol and water.

Conjugating uncoupler compounds with hydrophobic hydrocarbon chains to achieve adipose tissue selective drug accumulation.

One potential approach for treating obesity is to increase energy expenditure in brown and white adipose tissue. Here we aimed to achieve this outcome by targeting mitochondrial uncoupler compounds selectively to adipose tissue, thus avoiding side effects from uncoupling in other tissues. Selective drug accumulation in adipose tissue has been observed with many lipophilic compounds and dyes.

Quinoline-quinoline schiff-base as an effective chromogenic, fluorogenic, and smartphone assisted RGB detection of Pb ion in near aqueous medium.

A novel multimode colorimetric and fluorescent chemosensor was developed using an 8-hydroxy quinoline carbaldehyde Schiff base with a quinoline hydrazide probe (E)-2-((2-(quinolin-2-yl)hydrazineylidene)methyl)quinolin-8-ol (L). NMR (H & C), FTIR, and HR-mass spectral characterization techniques confirmed the probe L structural conformation. As Probe L contacts Pb ions, a color change and turn-off emission can be visually detected in EtOH:HO (1:1, v/v, pH = 7.

Cell-derived nanovesicles from mesenchymal stem cells as extracellular vesicle-mimetics in wound healing.

Wound healing is a dynamic process that involves a series of molecular and cellular events aimed at replacing devitalized and missing cellular components and/or tissue layers. Recently, extracellular vesicles (EVs), naturally cell-secreted lipid membrane-bound vesicles laden with biological cargos including proteins, lipids, and nucleic acids, have drawn wide attention due to their ability to promote wound healing and tissue regeneration. However, current exploitation of EVs as therapeutic agents is limited by their low isolation yields and tedious isolation processes.

The Identification of Potential Drugs for Dengue Hemorrhagic Fever: Network-Based Drug Reprofiling Study.

Background: Dengue fever can progress to dengue hemorrhagic fever (DHF), a more serious and occasionally fatal form of the disease. Indicators of serious disease arise about the time the fever begins to reduce (typically 3 to 7 days following symptom onset). There are currently no effective antivirals available.

Plasma-derived exosomal miRNA as potential biomarker for diagnosis and prognosis of vector-borne diseases: A review.

Early disease diagnosis is critical for better management and treatment outcome of patients. Therefore, diagnostic methods should ideally be accurate, consistent, easy to perform at low cost and preferably non-invasive. In recent years, various biomarkers have been studied for the detection of cardiovascular diseases, cerebrovascular diseases, infectious diseases, diabetes mellitus and malignancies.

An improved visual closed tube Loop mediated isothermal amplification (LAMP) assay for rapid identification of orf virus in sheep and goats.

The orf virus (ORFV) is an epitheliotropic virus causing a highly contagious skin disease mainly in sheep and goats. Several diagnostics including molecular tools like Loop mediated isothermal amplification (LAMP) assay are available to detect ORFV in affected species. However, the carry-over contamination associated with LAMP as open tube format prevents the assay applicability as point of care test in field diagnostic settings.

Site-directed deuteration of dronedarone preserves cytochrome P4502J2 activity and mitigates its cardiac adverse effects in canine arrhythmic hearts.

Cytochrome P4502J2 (CYP2J2) metabolizes arachidonic acid (AA) to cardioprotective epoxyeicosatrienoic acids (EETs). Dronedarone, an antiarrhythmic drug prescribed for treatment of atrial fibrillation (AF) induces cardiac adverse effects (AEs) with poorly understood mechanisms. We previously demonstrated that dronedarone inactivates CYP2J2 potently and irreversibly, disrupts AA-EET pathway leading to cardiac mitochondrial toxicity rescuable EET enrichment.

Long-term protective immunity to goatpox in goats after a single immunization with a live attenuated goatpox vaccine.

In this study, the duration of immunity following a single-dose vaccination using an attenuated live goatpox vaccine (GTPV/Uttarkashi/1978 strain) was evaluated in goatpox-seronegative goats for 52 months. Long-term immunity was evaluated by clinical protection upon virulent virus challenge and serum neutralization assay applied to serum samples. The rise in the level of GTPV-specific antibodies was found to reach a maximum at 21 days post-vaccination, and these antibodies were maintained for 1 to 2 years after immunization, with a steady decline.

Rational deuteration of dronedarone attenuates its toxicity in human hepatic HepG2 cells.

Deuteration is a chemical modification strategy that has recently gained traction in drug development. The replacement of one or more hydrogen atom(s) in a drug molecule with its heavier stable isotope deuterium can enhance its metabolic stability and pharmacokinetic properties. However, it remains uninterrogated if rational deuteration at bioactivation "hot-spots" could attenuate its associated toxicological consequences.

Enhanced skin penetration of berberine from proniosome gel attenuates pain and inflammation in a mouse model of osteoarthritis.

Dermal delivery of bioactive molecules remains an attractive route of administration in osteoarthritis (OA) due to the local accumulation of drugs while avoiding their systemic side effects. In this study we propose a proniosome gel comprising non-ionic surfactants that self-assemble into de-hydrated vesicles for the delivery of the natural anti-inflammatory compound berberine. By modulating the hydrating ability of the proniosome gel, berberine can be efficiently released with minimal mechanical force.

The complete genome sequence of Indian sheeppox vaccine virus and comparative analysis with other capripoxviruses.

Sheeppox virus (SPPV) is responsible for a significant economic loss to sheep husbandry in enzootic regions of Africa, the Middle East, and Asia including the Indian subcontinent. In this study, we present the complete genome sequence of SPPV vaccine strain SPPV-Srin38/00 from India determined by next-generation sequencing (NGS) using Illumina technology. The attenuated Srinagar vaccine strain of SPPV (SPPV-Srin38/00) was developed by serial passaging the virus initially in lamb testes (LT) cells followed by Vero cell line.

Investigations on detoxification mechanisms of novel para-phenylenediamine analogues through N-acetyltransferase 1 (NAT-1).

Para-phenylenediamine (PPD) is one of the most used chemicals in oxidative hair dyes. However, its use has been associated with adverse effects on health, including contact dermatitis and other systemic toxicities. Novel PPD derivatives have been proposed as a safer replacement for PPD.

Lyophilization Preserves the Intrinsic Cardioprotective Activity of Bioinspired Cell-Derived Nanovesicles.

Recently, bioinspired cell-derived nanovesicles (CDNs) have gained much interest in the field of nanomedicine due to the preservation of biomolecular structure characteristics derived from their parent cells, which impart CDNs with unique properties in terms of binding and uptake by target cells and intrinsic biological activities. Although the production of CDNs can be easily and reproducibly achieved with any kind of cell culture, application of CDNs for therapeutic purposes has been greatly hampered by their physical and chemical instability during long-term storage in aqueous dispersion. In the present study, we conceived a lyophilization approach that would preserve critical characteristics regarding stability (vesicles' size and protein content), structural integrity, and biological activity of CDNs for enabling long-term storage in freeze-dried form.