Pharmacological Applications Research Articles

Single‐crystal X‐ray analysis of the diketo form of asymmetric curcuminoids and coupled with NMR insights into its β‐Keto‐enol tautomerization at ambient temperature

AbstractIn this study, we present a detailed analysis of the structural forms of asymmetric curcuminoids through single‐crystal X‐ray diffraction and nuclear magnetic resonance (NMR) spectroscopy. Curcuminoids substituted with electron‐withdrawing groups (Cl and Br) predominantly adopt the β‐keto‐enol form, whereas those with an OMe group exhibit both diketo and β‐keto‐enol forms. Variable‐temperature X‐ray diffraction studies confirm that the structural state of curcuminoids is influenced by temperature. Our findings also reveal that the β‐keto‐enol form is favored in acidic and neutral conditions, while the diketo form is more prevalent in basic environments. The theoretical Density Functional Theory (DFT) calculations further elucidate the energy differences between the diketo and β‐keto‐enol forms, emphasizing the significance of electronic effects and temperature on tautomeric distributions. These insights enhance our understanding of the structural dynamics of curcuminoids, with implications for their biological activity and pharmacological applications.

Exploring the Therapeutic potential of Purified Alternanthera pungens Plant Extract

This study investigates the cytotoxicity of a purified extract obtained via reverse-phase high-performance liquid chromatography (HPLC) from A. pungens. The purification procedure was particularly executed to isolate bioactive compounds. In vitro Cytotoxicity assessments were performed on MDCK (Madin-Darby canine kidney). The outcomes revealed that the purified extract exhibited no notable cytotoxicity activity against these cells. GC-MS analysis is performed to identify and elucidate the chemical composition of the purified extract this characterization offers valuable insights into the chemical profile of A. pungens and lays the foundation for further research on its pharmacological applications.

Fermentation: improvement of pharmacological effects and applications of botanical drugs.

Fermentation is an important concoction technique for botanical drugs. Fermentation transforms and enhances the active ingredients of botanical drugs through specific microbiological processes, ultimately affecting their pharmacological effects. This review explores the use of fermented botanical drugs in areas such as anti-tumor, hypolipidemic, antioxidant, antimicrobial, cosmetology, and intestinal flora regulation. It elucidates the potential pharmacological mechanisms and discusses the benefits of fermentation technology for botanical drugs, including reducing toxic side effects, enhancing drug efficacy, and creating new active ingredients. This article also discussesdelves into the common strains and factors influencing the fermentation process, which are crucial for the successful transformation and enhancement of these drugs. Taken together, this study aimed to provide a reference point for further research and wider applications of botanical drug fermentation technology.

Evaluation of genotoxicity and teratogenicity of phillyrin

Phillyrin is extracted from Forsythia suspensa (Thunb.) Vahl, is significantly higher in (unripe Forsythiae Fructus) Qing qiao than in (ripe Forsythiae Fructus) Lao qiao fruits of the plant. However, the toxicity of phillyrin has not been adequately investigated. The study investigates the genetic and teratogenic effects of phillyrin to determine its safety profile. Assessing the genotoxicity and teratogenicity of phillyrin involved various tests, such as the bacterial reverse mutation assay, mammalian erythrocyte micronucleus assay, spermatocyte chromosome aberration assay, and teratogenicity assay. The results demonstrated that phillyrin exhibited no discernible impact on the following: number of colonies that spontaneously revert for Salmonella typhimurium TA 97, TA98, TA100, TA102, and TA1535, frequency of bone marrow polychromatic erythrocytes, and the rate of chromosomal aberrations. In the teratogenicity test, the pregnant rats exhibited no signs of toxicity or abnormal changes, and the growth, embryonic development, and visual anatomy of each pup were normal. In comparison with the negative control group, there were no significant differences in fetal body weight, mortality, deformity rate, malformed nest rate, gravid uterus weight, average number of fetuses per litter, fetal body length, or visceral and skeletal development in each dose group. In conclusion, these findings provide evidence that phillyrin does not exhibit genotoxic or teratogenic effects, supporting its potential safety for pharmacological applications.

Rational synthesis of Azo ligands and copper complexes: Insights into potential therapeutic agents

In the pursuit of innovation, four distinct mono Azo dyes D1-D4 were synthesized. These dyes were crafted through a coupling reaction involving 1-naphthol, resorcinol and salicylic acid with diazonium salts derived from a diverse array of aromatic amines, including aniline and sulphanilic acid. Subsequently, they are transformed into copper Azo complexes, namely (D1CuC-D4CuC). The structural underpinnings of these mono Azo dyes and their corresponding copper complexes were unveiled using an arsenal of analytical techniques: FTIR, 1H NMR, 13C NMR, and UV-visible spectroscopy which unequivocally confirmed their synthesis. A computational protein-ligand docking approach was used to assess the binding affinity of ligands and metal complexes to an anti-oxidant receptor protein (PDB ID:2HCK) which showed excellent binding interactions. The findings from an in vitro antioxidant activity using the DPPH scavenging method exhibited: Complexes > Ligands. As an antioxidant agent, the synthesized compounds may prove to be a great therapeutic option. This research introduces a novel approach by utilizing Azo dyes as ligands, leveraging their exceptional electronic tunability and stability to form innovative copper complexes. Their pharmacological applications will be explored, potentially yielding drugs with improved efficacy and selectivity.

Eco-friendly Strategy for Producing Bio-based Silver Nanoparticles (AgNPs) Employing Sepioteuthis lessoniana ink, in Addition to Biological and Degradation of Dye Applications.

The squid, Sepioteuthis lessoniana, is a remarkable fishery product which is exported by many nations for use in industrial production or human consumption. This study focused on the synthesis of silver nanoparticles (AgNPs) from squid ink (SI) and its wide range of applications. The formation of the nanoparticles was confirmed through UV-Visible spectroscopy, FTIR, XRD, SEM with EDX, DLS, and zeta potential analysis. The results showed a strong absorbance peak at 407nm, the presence of various functional groups, a nanocrystalline structure with a crystalline size of 17.56nm, spherical-shaped particles with an average size of 76nm, and the presence of the highest % mass of Ag and uniformly dispersed particles, respectively. The bioactivity of the synthesized squid ink silver nanoparticles was analyzed through antibacterial, antioxidant, anticancer, and toxicity studies. The dye degradation assay was also analyzed as a means of wastewater treatment for different industrial dyes. The antibacterial activity showed the highest zone of inhibition of 24mm at a concentration of 100μg/ml against Escherichia coli, followed by other tested strains. The nitric oxide radical scavenging assay showed the highest antioxidant activity (92%) at a concentration of 100μg/ml. The cytotoxic ability of SI-AgNPs against the MDA-MB-231 breast cancer cell line revealed an IC50 value of 4.52μg/ml. The toxicity study revealed a dose and time-dependent activity with the LC50 value of 5.090 and 3.303mg/ml for 24 and 48h, respectively. The successful degradation of dyes by SI-AgNPs is attributed to the cooperative action of the electron relay system with Ag as a catalyst and SI as a catalytic support. These findings indicate that SI-AgNPs are a novel potential product that should be further studied to improve its pharmacological, biomedical, and environmental applications.

Pharmacokinetics of two triterpenoid saponins and three flavonoids in Astragalus membranaceus leaves by UHPLC-MS/MS

Astragalus membranaceus (A. membranaceus) leaves can be used both as a medicine and food material. Their main chemical components are flavonoids and triterpenoid saponins. The pharmacokinetics of A. membranaceus leaves are rarely reported in the literature. This study aimed to investigate the pharmacokinetics of five major bioactive components of A. membranaceus leaves [rhamnocitrin 3-glucoside (RCG), tiliroside (TIL), rhamnocitrin 3-neohesperidoside (RNH), huangqiyenin R (HuR), and huangqiyenin I (HuI)]. Simultaneously using ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method. The extract of A. membranaceus leaves was administered orally to rats, and the rat plasma was subjected to a fast, sensitive, and specific UHPLC-MS/MS method. Butylparaben served as the internal standard. The plasma samples were pretreated using isopropanol/ethyl acetate (1:1, v/v) liquid–liquid extraction. Chromatographic separations were performed at a flow rate of 0.3 mL/min on a Waters ACQUITY HSS T3 Column (2.1 mm × 100 mm, 1.8 μm) using mobile phases of 0.1 % formic acid/water and 0.1 % formic acid/acetonitrile. Mass spectrometry detection was performed using an electrospray ionization ion source in the negative-ion mode and the multiple reaction monitoring mode. All analytes had an intraday and interday relative standard deviation of less than 14.10 %. The range of accuracy was –11.94–6.920 % and –15.22–5.800 %. The lower limits of quantification for RCG, TIL, RNH, HuR, HuI was 10.24, 10.27, 10.12, 5.137, and 5.841 ng/mL, respectively. The criteria were met by stability, matrix effects, and extraction recovery. The pharmacokinetic parameters of A. membranaceus leaf extract were ultimately obtained using this analytical method. The study provides a theoretical basis for future pharmacological research, clinical application, and development of healthy food from A. membranaceus leaves.

Diverse Methods with Stereoselective Induction in the Asymmetric Biginelli Reaction.

The relevance of the asymmetric Biginelli reaction (ABR) has been increased in this century, due to the pharmacological application of its products. This review focuses predominantly on articles published in the period from 2015 to 2024 on asymmetric synthetic advances in the formation of dihydropyrimidinones (DHPMs), dihydropyrimidinethiones (DHPMTs), and related compounds. The relevant bibliography on general processes in the Biginelli reaction and some methods of separation of isomers have also been referenced.

Therapeutic and Pharmacological Applications of Essential Oils in Skin Care and Aromatherapy: Benefits, Mechanisms, and Safety Considerations

Therapeutic and Pharmacological Applications of Essential Oils in Skin Care and Aromatherapy: Benefits, Mechanisms, and Safety Considerations

Chromosome-level genome assembly and annotation of Flueggea virosa (Phyllanthaceae)

Flueggea virosa (Roxb. ex Willd.) Royle, an evergreen shrub and small tree in the Phyllanthaceae family, holds significant potential in garden landscaping and pharmacological applications. However, the lack of genomic data has hindered further scientific understanding of its horticultural and medicinal values. In this study, we have assembled a haplotype-resolved genome of F. virosa for the first time. The two haploid genomes, named haplotype A genome and haplotype B genome, are 487.33 Mb and 477.53 Mb in size, respectively, with contig N50 lengths of 31.45 Mb and 32.81 Mb. More than 99% of the assembled sequences were anchored to 13 pairs of pseudo-chromosomes. Furthermore, 21,587 and 21,533 protein-coding genes were predicted in haplotype A and haplotype B genomes, respectively. The availability of this chromosome-level genome fills the gap in genomic data for F. virosa and provides valuable resources for molecular studies of this species, supporting future research on speciation, functional genomics, and comparative genomics within the Phyllanthaceae family.

Machine learning-assisted optimization and evaluation of methylene blue adsorption kinetics on citrus aurantifolia leaves: Insights from isotherm and thermodynamic studies

BackgroundMethylene Blue (MB) is a cationic dye widely used in various industrial and pharmacological applications. However, its improper disposal poses significant environmental and health risks due to its toxicity, carcinogenicity, and resistance to biodegradation. Despite extensive efforts have been done to remove MB using green synthesis approaches, however; there remains a critical need to enhance the efficacy of these methods through proper optimization and the use of novel green sources. Addressing these challenges is essential to mitigate the environmental impact of MB. MethodsCitrus aurantifolia leaves powder (CALP), a simple, environmentally friendly, adsorbent has been utilized to remove MB dye. The adsorption kinetic efficacy of CALP was studied under different experimental conditions, including pH (3–9), contact time (2–8 min), and MB dye concentrations (10–70 mg/L). Additionally, machine learning (ML) was employed to optimize experimental conditions, predict, and validate the adsorption kinetic efficacy. The machine learning (ML) optimized experimental dataset which included parameters of pH (9), contact time (2 min), CALP adsorbent (0.3 gm), and MB dye concentration (70 mg/L) has shown maximum adsorption efficacy. To enhance and assess the extraction efficiency of MB dye, a response surface methodology (RSM) was employed utilizing a central composite design (CCD). Significant findingsThe adsorption efficacy of CALP was verified by the Freundlich isotherm model, which demonstrated an adsorption capacity of 415.05 mg/g with a coefficient of determination R2 of 0.999. The nonlinear pseudo-second-order kinetic model with an R2 value of 0.998 further confirms MB dye adsorption. In addition, spontaneous nature of the process was determined by calculating thermodynamic parameters such as ΔG°, ΔH°, and ΔS°. The outcomes demonstrate that CALP is a highly effective, reliable, and easily available adsorbent for the removal of MB dyes from wastewater. To the best of the author's knowledge, there are substantial unmet research gaps in the fields of wastewater treatment and adsorption modeling optimization. In particular, research that combine cutting-edge machine learning methods with conventional adsorption models to enhance process efficiency and prediction accuracy are scarce. This study is the first to employ CALP, a cost-effective and environmentally sustainable natural adsorbent, for the adsorption of MB dye utilizing a machine learning-optimized approach.

Real-World Application of a Quantitative Systems Pharmacology (QSP) Model to Predict Potassium Concentrations from Electronic Health Records: A Pilot Case towards Prescribing Monitoring of Spironolactone.

Quantitative systems pharmacology (QSP) models are rarely applied prospectively for decision-making in clinical practice. We therefore aimed to operationalize a QSP model for potas-sium homeostasis to predict potassium trajectories based on spironolactone administrations. For this purpose, we proposed a general workflow that was applied to electronic health records (EHR) from patients treated in a German tertiary care hospital. The workflow steps included model exploration, local and global sensitivity analyses (SA), identifiability analysis (IA) of model parameters, and specification of their inter-individual variability (IIV). Patient covariates, selected parameters, and IIV then defined prior information for the Bayesian a posteriori prediction of individual potassium trajectories of the following day. Following these steps, the successfully operationalized QSP model was interactively explored via a Shiny app. SA and IA yielded five influential and estimable parameters (extracellular fluid volume, hyperaldosteronism, mineral corticoid receptor abundance, potassium intake, sodium intake) for Bayesian prediction. The operationalized model was validated in nine pilot patients and showed satisfactory performance based on the (absolute) average fold error. This provides proof-of-principle for a Prescribing Monitoring of potassium concentrations in a hospital system, which could suggest preemptive clinical measures and therefore potentially avoid dangerous hyperkalemia or hypokalemia.

The application of rhubarb concoctions in traditional Chinese medicine and its compounds, processing methods, pharmacology, toxicology and clinical research.

This study reviews the development of rhubarb processing and the current status of pharmacological research. We summarized the effects of different processing methods on the active compounds, pharmacological effects, and toxicity of rhubarb, as well as the clinical application of different concoctions, providing reference for further pharmacological research and clinical application of rhubarb. A comprehensive literature review was conducted using databases such as Pubmed, Embase, National Science and Technology Library, Web of science, CNKI, China Science and Technology Journal Database, SinoMed, and the Pharmacopoeia of the People's Republic of China. Search terms included "rhubarb", "raw rhubarb", "wine rhubarb", "cooked rhubarb", "rhubarb charcoal", "herbal processing", "compounds", "pharmacological effects", "inflammation", "gastrointestinal bleeding", and "tumor". Historical records of rhubarb processing date back to the Han Dynasty, with continual innovations. Currently, the types of rhubarb used in traditional Chinese medicine have stabilized to three species: Rheum palmatum L., Rheum tanguticum Maxim.ex Balf. and Rheum officinale Baill. Common concoctions include raw rhubarb, wine rhubarb, cooked rhubarb and rhubarb charcoal. The active compounds of rhubarb are known to defecation, exhibit antibacterial and anti-inflammatory properties, regulate coagulation, protect the digestive system, and possess anti-tumor activities. Guided by Chinese medicine theory, the use of different rhubarb concoctions can enhance specific effects such as purgation to eliminate accumulation, clearing heat and toxins, cooling blood to stop hemorrhages, activating blood circulation to remove blood stasis, and inducing dampness to descend jaundice, thereby effectively treating various diseases. The therapeutic impact of these concoctions on diseases reflects not only in the changes to the active compounds of rhubarb but also in the formulations of traditional Chinese medicine. Processing has also shown advantages in reducing toxicity. Different processing methods alter the active compounds of rhubarb, thereby enhancing its various pharmacological effects and meeting the therapeutic needs of diverse diseases. Selecting an appropriate processing method based on the patient's specific conditions can maximize its pharmacological properties and improve clinical outcomes.

Harnessing in vivo synthesis of bioactive multiarylmethanes in Escherichia coli via oxygen-mediated free radical reaction induced by simple phenols

BackgroundXanthenes and multi-aryl carbon core containing compounds represent different types of complex and condensed architectures that have impressive wide range of pharmacological, industrial and synthetic applications. Moreover, indoles as building blocks were only found in naturally occurring metabolites with di-aryl carbon cores and in chemically synthesized tri-aryl carbon core containing compounds. Up to date, rare xanthenes with indole bearing multicaryl carbon core have been reported in natural or synthetic products. The underlying mechanism of fluorescein-like arthrocolins with tetra-arylmethyl core were synthesized in an engineered Escherichia coli fed with toluquinol remained unclear.ResultsIn this study, the Keio collection of single gene knockout strains of 3901 mutants of E. coli BW25113, together with 14 distinct E. coli strains, was applied to explore the origins of endogenous building blocks and the biogenesis for arthrocolin assemblage. Deficiency in bacterial respiratory and aromatic compound degradation genes ubiX, cydB, sucA and ssuE inhibited the mutant growth fed with toluquinol. Metabolomics of the cultures of 3897 mutants revealed that only disruption of tnaA involving in transforming tryptophan to indole, resulted in absence of arthrocolins. Further media optimization, thermal cell killing and cell free analysis indicated that a non-enzyme reaction was involved in the arthrocolin biosynthesis in E. coli. Evaluation of redox potentials and free radicals suggested that an oxygen-mediated free radical reaction was responsible for arthrocolins formation in E. coli. Regulation of oxygen combined with distinct phenol derivatives as inducer, 31 arylmethyl core containing metabolites including 13 new and 8 biological active, were isolated and characterized. Among them, novel arthrocolins with p-hydroxylbenzene ring from tyrosine were achieved through large scale of aerobic fermentation and elucidated x-ray diffraction analysis. Moreover, most of the known compounds in this study were for the first time synthesized in a microbe instead of chemical synthesis. Through feeding the rat with toluquinol after colonizing the intestines of rat with E. coli, arthrocolins also appeared in the rat blood.ConclusionOur findings provide a mechanistic insight into in vivo synthesis of complex and condensed arthrocolins induced by simple phenols and exploits a quinol based method to generate endogenous aromatic building blocks, as well as a methylidene unit, for the bacteria-facilitated synthesis of multiarylmethanes.

Fabrication of folic acid-conjugated pyrimidine-2(5H)-thione-encapsulated curdlan gum-PEGamine nanoparticles for folate receptor targeting breast cancer cells

In this study 5-((2-((3-methoxy benzylidene)-amino)-phenyl)-diazenyl)-4,6-diphenyl pyrimidine-2(5H)-thione was synthesized. The pharmacological applications of pyrimidine analogs are restricted due to their poor pharmacokinetic properties. As a solution, a microbial exopolysaccharide (curdlan gum) was used to synthesize folic acid-conjugated pyrimidine-2(5H)-thione-encapsulated curdlan gum-PEGamine nanoparticles (FA-Py-CG-PEGamine NPs). The results of physicochemical properties revealed that the fabricated FA-Py-CG-PEGamine NPs were between 100 and 400 nm in size with a majorly spherical shaped, crystalline nature, and the encapsulation efficiency and loading capacity were 79.04 ± 0.79 %, and 8.12 ± 0.39 % respectively. The drug release rate was significantly higher at pH 5.4 (80.14 ± 0.79 %) compared to pH 7.2. The cytotoxic potential of FA-Py-CG-PEGamine NPs against MCF-7 cells potentially reduced the number of cells after 24 h with 42.27 μg × mL−1 as IC50 value. The higher intracellular accumulation of pyrimidine-2(5H)-thione in MCF-7 cells leads to apoptosis, observed by AO/EBr staining and flow cytometry analysis. The highest pyrimidine-2(5H)-thione internalization in MCF-7 cells may be due to folate conjugated on the surface of curdlan gum nanoparticles. Further, internalized pyrimidine-2(5H)-thione increases the intracellular ROS level, leading to apoptosis and inducing the decalin in mitochondrial membrane potential. These outcomes demonstrated that the FA-Py-CG-PEGamine NPs were specificity-targeting folate receptors on the plasma membranes of MCF-7 Cells.

Recent Advances in the Synthesis of Antioxidant Derivatives: Pharmacological Insights for Neurological Disorders.

Neurological disorders, characterized by oxidative stress (OS) and inflammation, have become a major global health concern. Redox reactions play a vital role in regulating the balance of the neuronal microenvironment. Specifically, the imbalance leads to a significant weakening of the organism's natural defensive mechanisms. This, in turn, causes the development of harmful oxidative stress, which plays a crucial role in the onset and progression of neurodegenerative diseases. The quest for effective therapeutic agents has led to significant advancements in the synthesis of antioxidant derivatives. This review provides a comprehensive overview of the recent developments in the use of novel antioxidant compounds with potential pharmacological applications in the management of neurological disorders. The discussed compounds encompass a diverse range of chemical structures, including polyphenols, vitamins, flavonoids, and hybrid molecules, highlighting their varied mechanisms of action. This review also focuses on the mechanism of oxidative stress in developing neurodegenerative disease. The neuroprotective effects of these antioxidant derivatives are explored in the context of specific neurological disorders, including Alzheimer's disease, Parkinson's disease, and Huntington's disease. The ultimate goal is to provide effective treatments for these debilitating conditions and improve the quality of life for patients.

Comparative In Vitro Study between Biocompatible Chitosan-Based Magnetic Nanocapsules and Liposome Formulations with Potential Application in Anti-Inflammatory Therapy.

This study describes the comparison between the interaction of a series of peptide-functionalized chitosan-based nanocapsules and liposomes with two cell lines, i.e., mouse macrophages RAW 264.7 and human endothelial cells EA.hy926. Both types of nanocarriers are loaded with magnetic nanoparticles and designed for anti-inflammatory therapy. The choice of these magnetic nanostructures is argued based on their advantages in terms of size, morphology, chemical composition, and the multiple possibilities of modifying their surface. Moreover, active targeting might be ensured by using an external magnetic field. To explore the impact of chitosan-based nanocapsules and liposomes on cell cytophysiology, the cell viability, using the MTT assay, and cell morphology were investigated. The results revealed low to moderate cytotoxicity of free nanocapsules and significant cytotoxicity induced by chitosan-coated liposomes loaded with dexamethasone, confirming its release from the delivery system. Thus, after 48 h of treatment with nanocapsules, the viability of RAW 264.7 cells varied between 88.18% (OCNPM-1I, 3.125 µg/mL) and 76.37% (OCNPM-1, 25 µg/mL). In the same conditions, EA.hy926 cell viability was between 99.91% (OCNPM-3, 3.125 µg/mL) and 75.15% (OCNPM-3, 25 µg/mL) at the highest dose (25 µg/mL), the values being comparable for both cell lines. Referring to the cell reactivity after dexamethasone-loaded liposome application, the lowest viability of RAW 264.7 cells was 41.25% (CLDM5CP-1, 25 µg/mL) and 58.20% (CLDMM2CP-1 1.25 µg/mL) in the endothelial cell line, proving a selective character of action of nanocarriers. The cell morphology test, performed to support and confirm the results obtained by the MTT test, revealed a differentiated response for the two types of nano-carriers. As expected, an intense cytotoxic effect in the case of dexamethasone-loaded liposomes and a lack of cytotoxicity for drug-free nanocapsules were noticed. Therefore, our study demonstrated the biocompatible feature of the studied nanocarriers, which highlights them for future research as potential drug delivery systems for pharmacological applications, including anti-inflammatory therapy.

Study on the uptake of Gastrodin in the liver

BackgroundGastrodin is the active monomer of the Chinese herb Rhizoma Gastrodiae with the largest quantity of active components. Gastrodin is commonly used in the treatment of central nervous system disorders such as headaches and epilepsy due to its sedating and hypnotic properties. Its pharmacological mechanism and clinical application have been extensively explored due to its low toxicity. MethodsTo investigate the molecular mechanism of hepatic uptake of Gastrodin in rats, animals were randomly assigned to three groups: control group, rifampicin (RIF) group, and adrenalone (ADR) group. Blood samples were collected through the cardiac puncture 90, 180, and 300 min after injection, respectively. Rats were sacrificed 300 min after administration, and liver tissue was collected. Gastrodin concentration was determined by HPLC, and the Kp value was calculated. ResultsAfter administering the inhibitors of organic cation transporters (OCTs) and organic anion transporting polypeptides (OATPs), the KP values in the experimental groups were significantly lower compared to the blank control group (P < 0.05). ConclusionsThese findings imply that Gastrodin may be a substrate for both OCTs and OATPs.

Bile Acid-conjugate as a Promising Anticancer Agent: Recent Progress.

Bile acids have outstanding chemistry due to their amphiphilic nature and have received a lot of interest in the last few decades in the fields of biomedicine, pharmacology, and supramolecular applications. Bile acids are highly sought after by scientists looking for diverse and effective biological activity due to their chirality, rigidity, and hydroxyl group. The hydroxyl group makes it simple to alter the structure in a way that improves bioactivity and bioavailability. Bile acid-bioactive molecule conjugates are compounds in which a bile acid is linked to a bioactive molecule by a linker in order to increase the bioactivity of the bioactive molecule against the target cancer cells. This method has been used to improve the therapeutic efficacy of cytotoxic drugs while reducing their adverse side effects. These new bile acid conjugates are gaining attention because they overcome bioavailability and stability issues. The design, synthesis, and anticancer effectiveness of various bile acid conjugates are discussed together with recent advances in understanding in this review.

Pharmacological Insights of Ropivacaine and Clinical Applications: A Narrative Review.

This review focuses on ropivacaine, a long-acting amide local anaesthetic, detailing its pharmacology and clinical applications. The article highlights its applications in providing analgesia, prolonging pain relief, and improving recovery outcomes in surgical settings. Ropivacaine is particularly effective for epidural labor analgesia in obstetrics, promoting stable hemodynamics and rapid onset when used with adjuvants. Its prolonged anesthetic effects reduce the need for postoperative opioids in peripheral nerve blocks. Intrathecal administration may enhance functional recovery and postoperative analgesia in various surgical procedures. While effective in treating acute pain, its role in chronic pain management remains unclear, indicating a need for further research. The review underscores the versatility and efficacy of ropivacaine in acute pain management and the importance of exploring its potential in chronic pain treatment.