Recent Advances Research Articles

Gold-catalyzed Reactions of Substituted 1,5-diynes: Recent Advances and their Chemistry

Abstract: Diynes are identified as exceptionally potent and superior substrates in gold-catalyzed organic transformations. Gold (I) and gold (III) complexes exhibit unique activity towards diynes, encouraging the nucleophilic addition of different functional groups both inter and intra- molecularly. In this review, particularly, we focused on recent advances in gold-catalyzed reactions of 1,5-diynes along with their mechanistic aspects. These reactions are interesting for constructing molecular complexity, medicinal chemistry, and material science.

Recent Advances in Chemistry, Mechanism, and Applications of Quantum Dots in Photodynamic and Photothermal Therapy.

Semiconductor quantum dots (QD) are a kind of nanoparticle with unique optical properties that have attracted a lot of attention in recent years. In this paper, the characteristics of these nanoparticles and their applications in nanophototherapy have been reviewed. Phototherapy, including photodynamic therapy (PDT) and photothermal therapy (PTT), has gained special importance because of its high accuracy and local treatment due to the activation of the drug at the tumor site. PDT is a new way of cancer treatment that is performed by activating light-sensitive compounds named photosensitizers (PS) by light. PSs cause the destruction of diseased tissue through the production of singlet oxygen. PTT is another non-invasive method that induces cell death through the conversion of near-infrared light (NIR) into heat in the tumor situation by the photothermal agent (PA). Through using energy transfer via the FRET (Förster resonance energy transfer) process, QDs provide light absorption wavelength for both methods and cover the optical weaknesses of phototherapy agents.

Recent Advances in Biomaterial Design for Bone Regenerative Therapy: A Mini Review

Abstract: Longevity has been associated with morbidity and an increase in age-related illnesses, linked to tissue degeneration and gradual loss of biological functions. Bone is an important organ that gradually degenerates with increasing lifespan. The remodeling phase plays a huge role in maintaining the ability of bone to regenerate and maintain its stability and function throughout life. Hence, bone health represents one of the major challenges to elderly citizens due to the increase of injury associated with bone degeneration, such as fragility and risks of fractures. In the virtue of improving the regenerative function of bone tissues, a specialized field of bone tissue engineering (BTE) has been introduced to improve the current strategies in treating bone degenerative disorders. Most of the research performed in BTE focuses on the optimization of key components to generate new bone formation, including the scaffold. A scaffold plays a significant role in establishing the structural form that interconnects major elements of the tissue engineering triad. To date, many types of biomaterials have been explored in BTE, ranging from natural and synthetic materials to nanocomposites. However, ideal scaffolds that display excellent biocompatibility and mechanical properties, approved for clinical practices are yet available. This paper aims to describe the up-to-date advancements in scaffold for new bone generation, highlighting the essential elements and strategies in selecting suitable biomaterials for bone repair.

Recent Advances in Biomedical Nanotechnology Related to Natural Products.

Natural product processing via nanotechnology has opened the door to innovative and significant applications in medical fields. On one hand, plants-derived bioactive ingredients such as phenols, pentacyclic triterpenes and flavonoids exhibit significant pharmacological activities, on another hand, most of them are hydrophobic in nature, posing challenges to their use. To overcome this issue, nanoencapsulation technology is employed to encapsulate these lipophilic compounds and enhance their bioavailability. In this regard, various nano-sized vehicles, including degradable functional polymer organic compounds, mesoporous silicon or carbon materials, offer superior stability and retention for bioactive ingredients against decomposition and loss during delivery as well as sustained release. On the other hand, some naturally occurring polymers, lipids and even microorganisms, which constitute a significant portion of Earth's biomass, show promising potential for biomedical applications as well. Through nano-processing, these natural products can be developed into nano-delivery systems with desirable characteristics for encapsulation a wide range of bioactive components and therapeutic agents, facilitating in vivo drug transport. Beyond the presentation of the most recent nanoencapsulation and nano-processing advancements with formulations mainly based on natural products, this review emphasizes the importance of their physicochemical properties at the nanoscale and their potential in disease therapy.

A Complete Sojourn of Current Trends in Gastro-retentive Drug Delivery System: Recent Advances and Patent Survey.

The current work aims to provide a complete sojourn on gastro-retentive drug delivery system (GRDDS) along with formulation methods, polymer selection, and in vitro/ in vivo challenges with finished dosage forms. Ideally, a biopharmaceutical-hindered drug has a rapid clearance and erratic bioavailability due to its low aqueous solubility and permeability. Additionally, it also suffers from high first-pass metabolism and pre-systemic gut wall clearance. Gastro-retentive drug delivery systems have become an emerging technology where newer methodologies and scientific approaches have been used to provide the controlled release of drugs and provide a protective mechanism in the stomach. By the virtue of utilizing GRDDS as a dosage form, these formulations increase Gastroretention time (GRT) which prolongs the controlled release of the drug in the dosage form. GRDDS contribute to increased drug bioavailability and targeting at a site of action, which enhances therapeutic action and offers significant patient compliance. Furthermore, the present work also highlighted the critical role of polymers in favoring drug retention across GIT with the mechanism of gastro-retention and recommended concentration ranges. The emerging technology is also highlighted by the approved drug products and patented formulations in the recent decade which is depicted in a justified manner. GRDDS formulations have demonstrated clinical efficacy, which is supported by a compilation of patents for cutting-edge innovations in dosage forms that can be held in the stomach for an extended period of time.

Recent Advances in the Development of RET Inhibitors

Background: Rearranged during transfection (RET) is a receptor tyrosine kinase and a bona fide oncogene that drives various cancers. Oncogenic RET induces abnormal activation of RET kinase, causing tumorigenesis. RET can be abnormally activated through RET point mutations and RET fusions. Although RET kinase has been discovered in tumors more than 30 years ago, patients with RET-altered tumors gain limited benefits from multikinase inhibitors (MKIs). In 2020, pralsetinib and selpercatinib were approved by FDA for the treatment of RET-altered tumors. Objective: Recently reported RET inhibitors were reviewed to provide an overview of the development of novel RET inhibitors. Methods: Literatures, patents, and conference proceedings published in the past five years were collected. Only RET inhibitors with novel scaffolds or in vivo efficacy were discussed in this review. The enzymebased and cell-based activities, PK profiles, antitumor activities in vivo, and clinical efficacy of the selected RET inhibitors were described. Results: Great efforts have been spent on the development of RET inhibitors, leading to increased RETtargeted therapies. Due to high potency and specificity, pralsetinib and selpercatinib resulted in a >8- month improvement in overall survival, compared to MKIs. However, solvent-front mutants emerged and contributed to the acquired resistance to pralsetinib and selpercatinib. To overcome solvent front mutants, TPX-0046, TAS0953, and LOX-260 are investigated in early clinical studies. Conclusion: Zeteletinib, SYHA1815, TPX-0046, TAS0953, and LOX-260 are potential therapies for RET-altered cancers. In addition, macrocyclic inhibitors, allosteric inhibitors, and PROTACs are three promising strategies to address the potential drug resistance of RET.

Recent advances in copper-based catalysts for electrocatalytic CO 2 reduction toward multi-carbon products

Recent advances in copper-based catalysts for electrocatalytic CO ₂ reduction toward multi-carbon products

Applications of nanotechnology-mediated herbal nanosystems for ophthalmic drug.

In recent years, herbal nanomedicines have gained tremendous popularity for novel drug discovery. Nanotechnology has provided several advances in the healthcare sector, emerging several novel nanocarriers that potentiate the bioavailability and therapeutic efficacy of the herbal drug. The recent advances in nanotechnology with accelerated strategies of ophthalmic nanosystems have paved a new path for overcoming the limitations associated with ocular drug delivery systems, such as low bioavailability, poor absorption, stability, and precorneal drug loss. Ophthalmic drug delivery is challenging due to anatomical and physiological barriers. Due to the presence of these barriers, the herbal drug entry into the eyes can be affected when administered by following multiple routes, i.e., topical, injectables, or systemic. However, the advancement of nanotechnology with intelligent systems enables the herbal active constituent to successfully entrap within the system, which is usually difficult to reach employing conventional herbal formulations. Herbal-loaded nanocarrier drug delivery systems demonstrated enhanced herbal drug permeation and prolonged herbal drug delivery. In this current manuscript, an extensive search is conducted for original research papers using databases Viz., PubMed, Google Scholar, Science Direct, Web of Science, etc. Further painstaking efforts are made to compile and update the novel herbal nanocarriers such as liposomes, polymeric nanoparticles, solid lipid nanoparticles, nanostructure lipid carriers, micelles, niosomes, nanoemulsions, dendrimers, etc., which are mostly used for ophthalmic drug delivery system. This article presents a comprehensive survey of diverse applications used for the preventative measures and treatment therapy of varied eye disorders. Further, this article highlights the recent findings that the innovators are exclusively working on ophthalmic nanosystems for herbal drug delivery systems. The nanocarriers are promising drug delivery systems that enable an effective and supreme therapeutic potential circumventing the limitations associated with conventional ocular drug delivery systems. The nanotechnology-based approach is useful to encapsulate the herbal bioactive and prevent them from degradation and therefore providing them for controlled and sustained release with enhanced herbal drug permeation. Extensive research is still being carried out in the field of herbal nanotechnology to design an ophthalmic nanosystem with improved.

Neuroinflammation in Glioblastoma: The Role of the Microenvironment in Tumour Progression.

Glioblastoma (GBM) stands as the most aggressive and lethal among the main types of primary brain tumors. It exhibits malignant growth, infiltrating the brain tissue, and displaying resistance toward treatment. GBM is a complex disease characterized by high degrees of heterogeneity. During tumour growth, microglia and astrocytes, among other cells, infiltrate the tumour microenvironment and contribute extensively to gliomagenesis. Tumour-associated macrophages (TAMs), either of peripheral origin or representing brain-intrinsic microglia, are the most numerous nonneoplastic populations in the tumour microenvironment in GBM. The complex heterogeneous nature of GBM cells is facilitated by the local inflammatory tumour microenvironment, which mostly induces tumour aggressiveness and drug resistance. The immunosuppressive tumour microenvironment of GBM provides multiple pathways for tumour immune evasion, contributing to tumour progression. Additionally, TAMs and astrocytes can contribute to tumour progression through the release of cytokines and activation of signalling pathways. In this review, we summarize the role of the microenvironment in GBM progression, focusing on neuroinflammation. These recent advancements in research of the microenvironment hold the potential to offer a promising approach to the treatment of GBM in the coming times.

Recent Advances on PKM2 Inhibitors and Activators in Cancer Applications.

Metabolic reprogramming of cells, from the normal mode of glucose metabolism named glycolysis, is a pivotal characteristic of impending cancerous cells. Pyruvate kinase M2 (PKM2), an important enzyme that catalyzes the final rate-limiting stage during glycolysis, is highly expressed in numerous types of tumors and aids in development of favorable conditions for the survival of tumor cells. Increasing evidence has suggested that PKM2 is one of promising targets for innovative drug discovery, especially for the developments of antitumor therapeutics. Herein, we systematically summarize the recent advancement on PKM2 modulators including inhibitors and activators in cancer applications. We also discussed the classifications of pyruvate kinases in mammals and the biological functions of PKM2 in this review. We do hope that this review would provide a comprehensive understanding of the current research on PKM2 modulators, which may benefit the development of more potent PKM2-related drug candidates to treat PKM2-associated diseases including cancers in future.

Computational protein design - where it goes?

Proteins have been playing a critical role in the regulation of diverse biological processes related to human life. With the increasing demand, functional proteins are sparse in this immense sequence space. Therefore, protein design has become an important task in various fields, including medicine, food, energy, materials, etc. Directed evolution has recently led to significant achievements. Molecular modification of proteins through directed evolution technology has significantly advanced the fields of enzyme engineering, metabolic engineering, medicine, and beyond. However, it is impossible to identify desirable sequences from a large number of synthetic sequences alone. As a result, computational methods, including data-driven machine learning and physics-based molecular modeling, have been introduced to protein engineering to produce more functional proteins. This review focuses on recent advances in computational protein design, highlighting the applicability of different approaches as well as their limitations.

An Updated Review on Molecular Biomarkers in Diagnosis and Therapy of Colorectal Cancer.

Colorectal cancer is one of the most common cancer types worldwide. Since colorectal cancer takes time to develop, its incidence and mortality can be treated effectively if it is detected in its early stages. As a result, non-invasive or invasive biomarkers play an essential role in the early diagnosis of colorectal cancer. Many experimental studies have been carried out to assess genetic, epigenetic, or protein markers in feces, serum, and tissue. It may be possible to find biomarkers that will help with the diagnosis of colorectal cancer by identifying the genes, RNAs, and/or proteins indicative of cancer growth. Recent advancements in the molecular subtypes of colorectal cancer, DNA methylation, microRNAs, long noncoding RNAs, exosomes, and their involvement in colorectal cancer have led to the discovery of numerous new colorectal cancer biomarkers. In small-scale investigations, most biomarkers appear promising. However, large-scale clinical trials are required to validate their effectiveness before routine clinical implementation. Hence, this review focuses on small-scale investigations and results of big data analysis that may provide an overview of the biomarkers for the diagnosis, therapy, and prognosis of colorectal cancer.

Recent Advances in Research on Active Compounds Against Hepatic Fibrosis.

Almost all chronic liver diseases cause fibrosis, which can lead to cirrhosis and eventually liver cancer. Liver fibrosis is now considered to be a reversible pathophysiological process and suppression of fibrosis is necessary to prevent liver cancer. At present, no specific drugs have been found that have hepatic anti-fibrotic activity. The research progress of anti-hepatic fibrosis compounds in recent ten years was reviewed to provide a reference for the design and development of anti-hepatic fibrosis drugs. According to the structure of the compounds, they are divided into monocyclic compounds, fused-heterocyclic compounds, and acyclic compounds. In this article, the natural products and synthetic compounds with anti-fibrotic activity in recent ten years were reviewed, with emphasis on their pharmacological activity and structure-activity relationship (SAR). Most of these compounds are natural active products and their derivatives, and there are few researches on synthetic compounds and SAR studies on natural product.

1-Cyanoacetylthiosemicarbazides: Recent Advances in their Synthesis, Reactivity in Heterocyclization, and Bio-Applications

Abstract: The synthesis of 1-cyanoacetylthiosemicarbazides is at the apex attention of researchers due to their multifaced reactivity as versatile precursors in the synthesis of mono-, bi-, and fused_heterocyclic compounds as well as metal complexes. Despite this, no comprehensive survey was, so far, dedicated to the synthesis, chemical transformation, and bioactivities of this relevant family of synthetic organic precursors and their derivatives. The present survey aims to summarize an up-to-date record of the preparation of 1-cyanoacetylthiosemicarbazides and their chemical transformation. A particular focus is given to their metal complexes and bio-applications

Nanocrystal Materials for Resistive Memory and Artificial Synapses: Progress and Prospects.

Resistive random-access memory (RRAM) is considered to be the most promising next-generation non-volatile memory because of its low cost, low energy consumption, and excellent data storage characteristics. However, the on/off (SET/RESET) voltages of RRAM are too random to replace the traditional memory. Nanocrystals (NCs) offer an appealing option for these applications since they combine excellent electronic/optical properties and structural stability and can address the requirements of low-cost, large-area, and solution-processed technologies. Therefore, the doping NCs in the function layer of RRAM are proposed to localize the electric field and guide conductance filaments (CFs) growth. The purpose of this article is to focus on a comprehensive and systematical survey of the NC materials, which are used to improve the performance of resistive memory (RM) and optoelectronic synaptic devices and review recent experimental advances in NC-based neuromorphic devices from artificial synapses to light-sensory synaptic platforms. Extensive information related to NCs for RRAM and artificial synapses and their associated patents were collected. This review aimed to highlight the unique electrical and optical features of metal and semiconductor NCs for designing future RRAM and artificial synapses. It was demonstrated that doping NCs in the function layer of RRAM could not only improve the homogeneity of SET/RESET voltage but also reduce the threshold voltage. At the same time, it could still increase the retention time and provide the probability of mimicking the bio-synapse. NC doping can significantly enhance the overall performance of RM devices, but there are still many problems to be solved. This review highlights the relevance of NCs for RM and artificial synapses and also provides a perspective on the opportunities, challenges, and potential future directions.

Targeting TYK2 for Fighting Diseases: Recent Advance of TYK2 Inhibitors

Abstract: TYK2 (tyrosine-protein kinase 2) is a non-receptor protein kinase belonging to the JAK family and is closely associated with various diseases, such as psoriasis, inflammatory bowel disease, systemic lupus erythematosus. TYK2 activates the downstream proteins STAT1-5 by participating in the signal transduction of immune factors such as IL-12, IL-23, and IL-10, resulting in immune expression. The activity of the inhibitor TYK2 can effectively block the transduction of excessive immune signals and treat diseases. TYK2 inhibitors are divided into two types of inhibitors according to the different binding sites. One is a TYK2 inhibitor that binds to JH2 and inhibits its activity through an allosteric mechanism. The representative inhibitor is BMS-986165, developed by Bristol-Myers Squibb. The other class binds to the JH1 adenosine triphosphate (ATP) site and prevents the catalytic activity of the kinase by blocking ATP and downstream phosphorylation. This paper mainly introduces the protein structure, signaling pathway, synthesis, structure-activity relationship and clinical research of TYK2 inhibitors.

Scalable stable comb-to-tone integrated RF photonic drive for superconducting qubits

The recent advent of quantum computing has the potential to overhaul security, communications, and scientific modeling. Superconducting qubits are a leading platform that is advancing noise-tolerant intermediate-scale quantum processors. The implementation requires scaling to large numbers of superconducting qubits, circuit depths, and gate speeds, wherein high-purity RF signal generation and effective cabling transport are desirable. Fiber photonic-enhanced RF signal generation has demonstrated the principle of addressing both signal generation and transport requirements, supporting intermediate qubit numbers and robust packaging efforts; however, fiber-based approaches to RF signal distribution are often bounded by their phase instability. Here, we present a silicon photonic integrated circuit-based version of a photonic-enhanced RF signal generator that demonstrates the requisite stability, as well as a path towards the necessary signal fidelity.

Multimodal Embodiment Research of Oral Music Traditions: Electromyography in Oud Performance and Education Research of Persian Art Music

With the recent advent of research focusing on the body’s significance in music, the integration of physiological sensors in the context of empirical methodologies for music has also gained momentum. Given the recognition of covert muscular activity as a strong indicator of musical intentionality and the previously ascertained link between physical effort and various musical aspects, electromyography (EMG)—signals representing muscle activity—has also experienced a noticeable surge. While EMG technologies appear to hold good promise for sensing, capturing, and interpreting the dynamic properties of movement in music, which are considered innately linked to artistic expressive power, they also come with certain challenges, misconceptions, and predispositions. The paper engages in a critical examination regarding the utilisation of muscle force values from EMG sensors as indicators of physical effort and musical activity, particularly focusing on (the intuitively expected link to) sound levels. For this, it resides upon empirical work, namely practical insights drawn from a case study of music performance (Persian instrumental music) in the context of a music class. The findings indicate that muscle force can be explained by a small set of (six) statistically significant acoustic and movement features, the latter captured by a state-of-the-art (full-body inertial) motion capture system. However, no straightforward link to sound levels is evident.

Recent Advancements in Multicomponent Reactions of Substituted 2- Aminopyridines Synthesis: A Decade Review

Abstract: One-step synthesis of multifaceted heterocycles employing multicomponent reactions (MCRs) corresponds to a viable, innovative, and prospective strategy. In recognition of their noteworthy physiological, biological, and pharmacological behavior, 2-aminopyridines secure an exceptional spot among heterocycles. The current analysis comprises an overview of the scientific literature concerning the multicomponent reactions of substituted 2-aminopyridine synthesis. The stipulated outcomes have been thoroughly categorized according to the number and nature of the components. The past 11 years of literary work (2011–2022) are specifically incorporated. This review article will assist in advancing the development of cutting-edge and enhanced approaches towards the synthesis of 2-aminopyridines and their counterparts.

Recent advances in the study of epitopes, allergens and immunologic cross-reactivity of edible mango

Mango (Mangifera indica L.) is a tropical fruit that is widely consumed as both fresh fruits and processed products around the world. The high incidence of mango allergy, on the other hand, has sparked widespread concern. Therefore, a summary and analysis of the current status and issues in mango allergen research can guide in-depth study on the mechanism of mango allergy and reveal effective desensitization methods. We described the incidence of fruit allergy, as well as the mechanism and clinical symptoms of mango allergy, in this review. We also looked into the structural properties of mango allergens, the effect of processing methods on mango allergens, prediction methods for mango allergen epitopes, and the current state of research on mango cross-reactive allergens and preventive measures. Finally, the research directions and ideas for the future are proposed and discussed.