Active Ingredients Research Articles

In-Silico discovery of 17alpha-hydroxywithanolide-D as potential neuroprotective allosteric modulator of NMDA receptor targeting Alzheimer’s disease

Alzheimer’s disease (AD) is a progressive neurodegenerative disorder marked by cognitive decline, memory impairment, and behavioral alterations. The N-methyl-D-aspartate (NMDA) receptor has emerged as a promising target for AD pharmacotherapy due to its role in the disease’s pathogenesis. This study leverages advanced computational methods to screen 80 active constituents of Withania somnifera (Ashwagandha), a traditional herb known for its neuroprotective effects, against the NMDA receptor, using FDA-approved Ifenprodil as a reference. Our blind virtual screening results demonstrated that all tested compounds could bind to various domains of the NMDA receptor, with binding energies ranging from − 4.1 to -11.9 kcal/mol, compared to Ifenprodil’s -7.8 kcal/mol. Binding preference analysis revealed 7 compounds bound to the A-chain, 37 to the B-chain, 7 to the C-chain, and 29 to the D-chain of the receptor. Notable binding was observed predominantly at the Amino Terminal Domain (ATD) core site, some at the ATD-Ligand Binding Domain (LBD) interface, and a few at the Transmembrane Domain (TMD). Particularly, 17alpha-hydroxywithanolide D, with a binding energy of -11.9 kcal/mol, emerged as a prime candidate for further investigation. Molecular dynamics simulations of this compound revealed key interactions, including direct hydrogen bonding with residues ASP165, ARG431, THR433, LYS466, and TYR476 on the D-chain, as well as additional hydrophobic and water-bridging interactions. These simulations highlighted the compound’s influence on dynamic conformational states of the GluN1b-GluN2B receptor complex, modulating interactions between GluN1b Lys178 and GluN2B Asn184. Furthermore, the compound affected the distance between LBD heterodimers and the tension within the LBD-M30 linker, demonstrating its potential to modulate NMDA receptor activity. This comprehensive study not only underscores the therapeutic promise of Withania somnifera derivatives for AD but also provides a detailed molecular basis for their efficacy, offering valuable insights for targeted drug development and innovative therapeutic strategies against Alzheimer’s disease.

Modification of Ceritinib Crystal Morphology via Spherical Crystallization

The formulation process for some drugs can be challenging, due to their unfavorable physical and mechanical properties and poor water solubility. Powder technology has made a significant impact in regard to the modification of the particles in active pharmaceutical ingredients (APIs) to produce high-quality granules. Spherical particles are preferred over other shapes, due to their high tap and bulk density, reduced dustiness, better flowability, strong anti-caking properties, and better mechanical performance during tableting. The present study investigates the possibility of obtaining spherical crystals of ceritinib, a drug used for the treatment of anaplastic lymphoma kinase (ALK)-positive advanced non-small cell lung cancer, which belongs to BCS class IV drugs and has a platy crystal structure. Ceritinib spheres were prepared by spherical agglomeration, in a ternary system, and quasi-emulsion solvent diffusion, with the addition of polyvinylpyrrolidone, as well as a combination of these two methods. With the combined method of spherical crystallization, crystals with the most favorable morphology and the narrowest distribution of particle sizes were obtained, which was the reason for further optimization. The influence of different impeller geometries and mixing rates on the morphology of the obtained crystals was examined and the optimal conditions for the process were selected. Using empirical correlations and a visual criterion, the process was scaled up from a 0.1 L to a 1 L batch crystallizer. The obtained crystals were characterized by light and scanning electron microscopy. The addition of a bridging liquid and/or a polymer additive did not change the internal structure of the ceritinib crystals, which was confirmed by X-ray powder diffraction.

Emergence of multiple resistance to EPSPS and ALS herbicides in smooth pigweed (Amaranthus hybridus): a growing concern in Brazil

Abstract Recently, farmers in Brazil have observed a decline in efficacy of glyphosate, chlorimuron, and imazethapyr control of smooth pigweed (Amaranthus hybridus L.). The objectives of this study were to quantify the resistance of Amaranthus in Brazil to glyphosate and acetolactate synthase (ALS)-inhibiting herbicides, elucidate the mechanism of resistance, and assess the frequency of sensitivity shifts to glyphosate and chlorimuron in Brazil. Dose–response assays were conducted in a greenhouse with glyphosate, chlorimuron, and imazethapyr. This was followed by sequencing of the EPSPS and ALS genes. Additionally , 740 Amaranthus populations across several Brazilian states were monitored over 4 yr, subjected to a single discriminatory dose of glyphosate and chlorimuron. The populations BR18Asp051 and BR21Asp205 were resistant to glyphosate, chlorimuron, and imazethapyr. The elevated resistance level to glyphosate in these populations is attributed to multiple amino acid substitutions (TAP-IVS) in the EPSPS gene; and cross-resistance to sulfonylureas and imidazolinones is conferred by the Trp-574-Leu substitution in the ALS gene in both populations. Overall, resistance distribution indicated that 88% of the sampled populations were considered sensitive to glyphosate, while 66% were sensitive to chlorimuron. Furthermore, 10% of the samples demonstrated multiple resistance to both active ingredients. A shift in glyphosate sensitivity was observed in four states in Brazil; however, sensitivity shifts to chlorimuron were more widely dispersed in Brazilian agricultural regions.

Inulae Flos is a potential herbal medicine to treat glioma: a study based on gene expression profile analysis, network pharmacology and molecular docking

Inulae Flos is a promising herbal medicine; however, its underlying mechanism in treating glioma remains unclear. This study aimed to elucidate the potential active ingredients and mechanisms of Inulae Flos in glioma treatment. Differentially expressed genes (DEGs) associated with gliomas were identified by analyzing the GSE186057 dataset. The bioactive components of Inulae Flos were searched in the Traditional Chinese Medicine Systems Pharmacology database, and related targets were obtained from the Swiss Target Prediction database. A protein-protein interaction (PPI) network was constructed using the STRING database. Next, the Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) of these common targets were analyzed using the DAVID database. Finally, AutoDock Vina was used for molecular docking analysis. The tumor-suppressive properties of the crude extract of Inulae Flos (XFH) and britanin were then evaluated with in vitro and in vivo assays. Nineteen active ingredients were obtained from Inulae Flos, and 20 DEGs were identified as the targets of Inulae Flos in glioma treatment. Britanin, luteolin and 1-O-Acetylbritannilactone were identified as the key ingredients. PIK3R1, CDK2, CCNB1, MAPK1, MAPK8, CCNA2, and AR were considered to be the hub target genes of Inulae Flos in glioma treatment. Good binding affinity was observed between the key components and hub targets. In addition, in vitro studies showed that XFH and britanin, a key component of Inulae Flos, could inhibit the growth, migration and invasion glioma cell lines U87 and U138, and repress the tumorigenesis of U138 cells in nude mice. Inulae Flos is promising for glioma treatment, and it exerts its anti-tumor activities via multiple components, targets and pathways.

The role of hydroponic solution of Ulva fasciata in modulating the antibiotic resistance of Vibrio alginolyticus.

This study aimed to ascertain the active substances in the hydroponic solution of Ulva (U.) fasciata (HSUF) and their effects on antibiotics resistance of pathogenic bacteria Vibrio alginolyticus (Va.) at environmental levels. Analytical results of HSUF by solid-phase extraction and gas chromatography-mass spectrometry showed that HSUF contained rich active substances and dominated by 2,4,6-tribromophenol, acetal, mono (2-ethylhexyl) phthalate and 2- (4-hydroxybenzene) ethanol, etc. Thereinto, 2,4,6-tribromophenol had the lowest minimal inhibitory concentrations (MICs) of 64-128μg mL-1 for Va. strains. The rich antibacterial substances of HSUF inhibited 47%-63% of isolated Va. strains. After 20 generations of subculture for Va. strains in three dilutes (1/2 (HT), 1/20 (MT) and 1/50 (LT)) of HSUF (20g L-1), the resistance to streptomycin of Va. S1 and Va. M3 changed from intermediate resistance ability to susceptible level. The large promotion of reactive oxygen species was observed in different HSUF levels, but the biofilm formation of Va. S1 did not changed significantly. Transcriptome sequencing of Va. S1 demonstrated that antibiotic resistance gene lpxA was down-regulated at different HSUF levels. Live U. fasciata excreted a variety of active secondary metabolites (SMs) in HSUF, which exhibited strong inhibitory effects on three isolated Va. strains. HSUF changed the antibiotic resistance of Va. Strain, especially at a higher HSUF concentrations.

Evaluation of the potential anti-arthritic effects and evaluation of acute oral toxicity of the active fraction of Eclipta prostrata leaves in rat model

The primary goal of this research was to isolate and assess the bioactive compounds within Eclipta prostrata Linn’s chloroform extract, with a focus on their potential to combat arthritis, validating its traditional use. Initially, antioxidant characteristics were evaluated, followed by fractionation through column chromatography. The in-vivo safety assessment, following OECD TG 425 Guidelines, showed no mortality at doses up to 2000 mg/kg, confirming the fraction’s safety. Subsequently, the active fraction was assessed in a complete Freund’s adjuvant-induced arthritis model. It demonstrated a dose-dependent inhibitory effect on inflammation and improved various parameters, including thermal latency time, dorsal flexion, motility, and motor coordination. Active bio constituents like rutin, stigmasterol, quercetin, and beta-sitosterol were estimated in the active fraction. The findings provide validation for the traditional use of E. prostrata as a potential plant with anti-arthritic properties, suggesting its potential suitability for rheumatoid arthritis treatment.

Abstract 4120749: GPR39 Orchestrates the Myogenic Response in Coronary Autoregulation

Background: Coronary autoregulation is the ability of a normal heart to maintain constant coronary blood flow (CBF) over a wide range of coronary driving pressures (CDPs) provided cardiac work remains constant. It is based on the myogenic response, the molecular mechanism of which is unknown. We recently described the presence of a G-protein coupled receptor (GPR39) in the vascular smooth muscle cells (VSMCs) of coronary arterioles in the mouse heart. We showed that endogenous eicosanoids, the vasoconstrictor 15-hydroxyeicosatetraenoic acid (15-HETE) and the vasodilator 14,15-epoxyeicosatrienoic acid (14,15 EET). act through this receptor to maintain coronary vascular tone. Hypothesis: We, therefore, hypothesized that GPR39 is the molecular switch responsible for the coronary myogenic response and autoregulation. Methods: We studied 6 anesthetized dogs at baseline and after administration of VC-108, a specific, potent GPR39 antagonist. Both during baseline and drug administration multiple coronary stenoses were created on the left anterior descending coronary artery (LAD). At each stage, heart rate, mean aortic pressure, distal LAD pressure, and right atrial pressure (RAP) were measured, as was CBF. Stenosis severity was defined by the CDP (LAD pressure minus RAP). Results: Mean basal coronary hyperemic response was 3.0 in all anesthetized animals indicating normal vasomotor function. Systemic hemodynamics did not differ between baseline and drug stages. Figure 1 is an example from a single dog where, at baseline, CBF remained constant over a CDP of 40-90 mm Hg indicating intact autoregulation. As expected, CBF declined when CDP fell below the autoregulatory range. After VC-108 administration CBF correlated linearly with CDP, indicating abolishment of the myogenic response. Baseline CDP vs. CBF data from all 6 animals within the autoregulatory range is depicted in Figure 2. No relation is noted between the two indicating intact autoregulation. In contrast, CDP vs. CBF relation is linear in all animals after VC108 is administered over the entire range of CDP’s measured, indicating abolishment of autoregulation (Figure 3). Conclusions: Our results indicate that GPR39 is a potential molecular switch for the regulation of the myogenic response underlying coronary autoregulation. Pharmacological blockage of GPR39 abolishes the myogenic tone. These novel findings set the stage for development of novel pharmacological agents for treatment of coronary artery disease.

Netupitant Inhibits the Proliferation of Breast Cancer Cells by Targeting AGK.

Background: Currently, there is a significant lack of effective pharmacological agents for the treatment of breast cancer. Acylglycerol Kinase (AGK), a lipid kinase, has been found to be aberrantly expressed in breast cancer and is closely associated with tumor proliferation, migration, and invasion. However, no clinical anti-tumor drugs specifically targeting this kinase have been developed. Methods: siRNA was utilized to knock down the AGK gene; CCK8 and colony formation assays were employed to evaluate the in vitro proliferative capacity of tumor cells. Molecular dynamics simulations and BIL assays were conducted to analyze drug binding affinity. Annexin V/PI staining was used to assess apoptotic phenomena; subcutaneous xenograft tumor experiments in nude mice were performed to confirm the in vivo anti-tumor efficacy of the drug. Results: Netupitant exhibited stable binding affinity for AGK and interacted with amino acids within the ATP-binding region of the enzyme. The IC50 values for the SK-BR-3 and MDA-MB-231 cell lines were determined as 16.15 ± 4.25 µmol/L and 24.02 ± 4.19 µmol/L, respectively; at a concentration of 2.5 µmol/L, Netupitant effectively inhibited clonogenic capacity in breast cancer cells; furthermore, treatment with 10 µmol/L significantly induced apoptosis in these cells. Doses of 50 mg/kg and 100 mg/kg Netupitant markedly suppressed growth rates of subcutaneous xenograft tumors in nude mice while also promoting apoptotic processes. Both in vivo and in vitro studies indicated that Netupitant could inhibit the activation of the PI3K/AKT/mTOR signaling pathway. Conclusions: By targeting AGK, Netupitant inhibits its kinase activity, which leads to reduced phosphorylation levels of PTEN, thereby suppressing the activation of the PI3K/AKT/mTOR signaling pathway and ultimately resulting in apoptosis in breast cancer cells.

Formulation, Evaluation and Medicinal Properties of Medicated Herbal Cream Containing Extract of Tridax Procumbens

At present, herbal medicine has a great impact on human health and diseases herbal medicine plays an important role in general aspects such as economy and medicine. The use of this herbal medicine is increasing day by day due to its quality, efficacy and safety. The present study explored a novel formulation containing extracts of Tridax procumbens, Ficus religiosa, Azadirachta indica and Curcuma longa in cream form (O/W). The formulation was characterized by determining the pharmaceutical properties such as pH, appearance, viscosity, spreadability, etc. The chemical constituents such as carbohydrates, alkaloids, steroids, etc. were detected using identification assays. The cream formulation was designed using excipients such as stearyl alcohol, beeswax, sorbitol monooleate, methylparaben, propylparaben and liquid paraffin. Compared with the control drug, the herbal drug was found to be safer. While allergy medications are associated with some side effects, the formulation of cream is much better than other formulations in terms of absorption and penetration of the active ingredient in the tropics.

A new exvivo human skin model for the topographic and biological analysis of cosmetic formulas.

Existing methods to evaluate skin care products suffer limitations. This is the case for exvivo skin explants, a first-choice 3D model. While essential to analyse mid- to long-term biological effects, this classical model hinders assessing microrelief variations. To circumvent these limitations, we developed an exvivo PERFused EXplant setup (Perfex) that maintains the outer skin surface in the open air, closely mirroring physiological conditions. A custom-designed reservoir enables perfusing the dermal side of explants with buffered, temperature-controlled medium, while the epidermis is subjected to "normal" conditions. Skin tension and characteristics of the stratum corneum, microrelief, histology and immunohistology (collagen types I and III, elastin and fibrillin-1) were analysed and compared to those of explants maintained under conventional conditions or invivo skin. The effects of skin care formulas intended to induce short- and/or mid- to long-term effects were also assessed. Skin explants maintained with the Perfex setup exhibit characteristics (firmness, elasticity, hydration and barrier function) closer to those of invivo skin than with conventional conditions. Moreover, Perfex-maintained explants present no alteration in histology after 7 days and slight variation in the expression of key protein markers. Microrelief characteristics also remain mostly stable over 7 days. Formula applications corroborate that skin tensor-containing products primarily induce short-term changes in the microrelief, while those with biologically active ingredients mainly lead to mid- to long-term effects on the histology and expression of molecular markers. Furthermore, maintaining skin explants with a physiologically relevant skin surface enabled analysing the relationship between microrelief and key markers, showing that fibrillin-1 is the protein most correlated with microrelief characteristics. The Perfex setup allows for similar preservation of skin explant histology and key protein expression as the conventional system, yet it maintains a skin surface close to that of invivo skin. Therefore, it is valuable to analyse both the short- and mid- to long-term impacts of skin care formulas and better comprehend their effects. The Perfex system also offers a new tool for investigating fundamental questions, such as the link that can exist between dermal proteins and skin surface properties.

Ibuprofen encapsulation inside non-conventional O/W Pickering emulsions stabilized with partially hydrophobized silica

The encapsulation of active ingredients is an important process in various industrial sectors including pharmaceutics, foods and cosmetics. For the first time, the capacity of non-conventional anti-Bancroft oil-in-water Pickering emulsions stabilized by partially hydrophobized silica to encapsulate an apolar active is addressed. A dispersed phase volume of paraffin oil of 50% coupled to 0.5 wt.% of silica has been employed to avoid excess of silica in the continuous phase and encapsulate higher amount of ibuprofen (the model drug). Three ibuprofen contents ranging from 100 mg (1.6 mg/mL of paraffin) to 420 mg (6 mg/mL of paraffin) have been tested. The encapsulation efficiency as well as the emulsions properties are investigated by the means of light diffusion, microscopy, rheology, and HPLC coupled to mass balance. The Pickering emulsion is very efficient for the encapsulation of ibuprofen with encapsulation rates of 99% obtained inside droplets of 30 µm for all the 3 ibuprofen concentrations. This encapsulation ability is perfectly maintained, whether during ageing (during 90 days), or when the emulsion is diluted by a factor 100 inside physiological media at basic and acidic pH.

Substantial non-compliance of online pharmacy catalogues with guidelines.

Online pharmacies are popular worldwide. In Germany, there were 150 active online pharmacies in 2022. As the competition is therefore fierce and new customers need to be acquired, some of these online pharmacies create catalogues that advertise products in self-medication to attract the interest of potential customers. This study analyzed the allergy, cold, and gastrointestinal tract categories from the summer/spring 2023 catalogues of two different online pharmacies in Germany. A comparison of the active ingredients in both catalogues and an analysis of the product's conformity with the German AWMF (Association of the Scientific Medical Societies in Germany) guidelines as well as international guidelines were carried out. In medicine, guidelines serve as evidence-based decision-making aids tools to ensure adequate patient care. The online catalogue of online pharmacy 1 showed conformity of 65% with AWMF guidelines, and the online catalogue of online pharmacy 2 showed conformity of 59% with AWMF guidelines. The online catalogue of online pharmacy 1 showed conformity of 44% with international guidelines, and the online catalogue of online pharmacy 2 showed conformity of just only 17% with international guidelines. Thus, there is a substantial lack of conformity of online pharmacy self-medication catalogues with national and international guidelines. For several indication areas including market-relevant rhinosinusitis and irritable bowel syndrome, consensus between AWMF and international guidelines was poor. The lack of evidence-based presentation of online pharmacy catalogues constitutes a risk for consumer safety. This risk must be assessed in future studies, for example by studies on intoxications caused by self-medication that is non-compliant with guidelines. Our results also underline the necessity of a stricter surveillance of the German self-medication market.

Pivoting: Responding to the Mental Health Needs of Youth of Color With Technology

Mental health treatments currently available to address racial discrimination for 21 million youth of color are inadequate. Given the nascent but promising mechanisms found within behavioral health interventions via racial socialization, or the process through which children acquire knowledge about race, developing effective and scalable therapeutic strategies to contend with the stress from racism and discrimination is possible. We outline the active ingredients that facilitate behavioral change for youth psychosocial outcomes impacted by racial discrimination and describe how technology is being utilized for current and future implementation efforts. We argue that technological advancement, in addition to ecological considerations, is crucial for the reduction of structural and interpersonal risk factors negatively influencing the psychological wellness of youth of color. Technology integration across implementation and assessment will be critical, particularly given the potential for technology to further exacerbate mental health disparities.

Nanocarrier mediated delivery of insecticides into tarsi enhances stink bug mortality

Current delivery practices for insecticide active ingredients are inefficient with only a fraction reaching their intended target. Herein, we developed carbon dot based nanocarriers with molecular baskets (γ-cyclodextrin) that enhance the delivery of active ingredients into insects (southern green stink bugs, Nezara viridula L.) via their tarsal pores. Nezara viridula feeds on leguminous plants worldwide and is a primary pest of soybeans. After two days of exposure, most of the nanocarriers and their active ingredient cargo (>85%) remained on the soybean leaf surface, rendering them available to the insects. The nanocarriers enter stink bugs through their tarsi, enhancing the delivery of a fluorescent chemical cargo by 2.6 times. The insecticide active ingredient nanoformulation (10 ppm) was 25% more effective in controlling the stink bugs than the active ingredient alone. Styletectomy experiments indicated that the improved active ingredient efficacy was due to the nanoformulation entering through the insect tarsal pores, consistent with fluorescent chemical cargo assays. This new nanopesticide approach offers efficient active ingredient delivery and improved integrated pest management for a more sustainable agriculture.

Adjuvants for Drone-Based Aerial Chemical Applications to Mitigate Off-Target Drift

Off-target drift from aerial pesticide applications in croplands can be a major source of pesticide exposure to pollinators. Pesticide adjuvants (PAs) are added to pesticides but can be as toxic as pesticides’ active ingredients. Ongoing experiments have identified sodium alginate (SA) as a drift-reducing PA less toxic to honeybees. Hence, SA and fenugreek polymer (FP) have been tested as drift-reducing PAs for aerial applications using the Remotely Piloted Aerial Application System (RPAAS). Two spray experiments were carried out in the field: (i) water only (W) and (ii) water and adjuvant (WA). Droplet spectrum and on-target coverage were collected using a VisiSize P15 image analyzer and kromekote cards, respectively. The drift reduction potentials (DRPs) of the adjuvants were analyzed based on droplet size (diameters of 10%, 50%, and 90% volume) and the proportion of driftable volume with droplets < 200 µm. Compared to the W only, the W-A treatment produced larger droplets, suggesting the presence of DRP. There were 14.5%, 8.3% to 14.4%, and 2.3% to 7.7% driftable fines in the W, WA (SA), and WA (FP) treatments, respectively. The FP treatment improved the on-target coverage (3.0% to 3.1%) compared to water (2.7%). Our results indicate that SA and FP have the potential to mitigate off-target drift and protect pollinator health.

Theoretical Study on Intramolecular Hydrogen Bonds of Flavonoid Cocrystals.

This study investigates the role of intramolecular hydrogen bonds in the formation of cocrystals involving flavonoid molecules, focusing on three active pharmaceutical ingredients (APIs): chrysin (CHR), isoliquiritigenin (ISO), and kaempferol (KAE). These APIs form cocrystals with different cocrystal formers (CCFs) through intramolecular hydrogen bonding. We found that disruption of these intramolecular hydrogen bonds leads to decreased stability compared to molecules with intact bonds. The extrema of molecular electrostatic potential surfaces (MEPS) show that flavonoid molecules with disrupted intramolecular hydrogen bonds have stronger hydrogen bond donors and acceptors than those with intact bonds. Using the artificial bee colony algorithm, dimeric structures of these flavonoid molecules were explored, representing early-stage structures in cocrystal formation, including API-API, API-CCF, and CCF-CCF dimers. It was observed that the number and strength of dimeric interactions significantly increased, and the types of interactions changed when intramolecular hydrogen bonds were disrupted. These findings suggest that disrupting intramolecular hydrogen bonds generally hinders the formation of cocrystals. This theoretical study provides deeper insight into the role of intramolecular hydrogen bonds in the cocrystal formation of flavonoids.

A General Strategy to Rapid and Sensitive Determination of Five High Boiling Point Solvents in Pharmaceuticals by RP-HPLC Combined with Precipitation Method.

The difficulty on determination of high boiling point solvents, always exist due to their low vapor pressure in headspace (HS) vial. What's worse, the commonly used GC diluents, such as N, N-dimethylacetamide, 1,3-dimethyl-2-imidazolidinone, dimethyl sulfoxide, N, N-dimethylformamide and N-methylpyrrolidone are often remained in HS instrument after frequent injection into HS, thus would result in terrible positive interference problem. In this work, a fast and sensitive HPLC method in combination with a sample precipitation method, was proposed for the determination of above five high boiling point solvents in drug substances within 14.5min. The final method was validated with regard to limit of detection and limit of quantitation, precision, linearity and accuracy in accordance with ICH Q2 (R1). Finally, the proposed strategy was successfully applied for the analysis of high boiling point solvents used in three active pharmaceutical ingredients. The established generic strategy would provide another choice for the determination of high boiling point solvents in pharmaceuticals.

Therapeutic Potential of Chinese Herbal Medicine and Underlying Mechanism for the Treatment of Myocardial Infarction.

Myocardial infarction (MI) is a prevalent disease with high mortality rates worldwide. The course of MI is intricate and variable, necessitating personalized treatment strategies based on different mechanisms. However, variety of postoperative complications and rejections, such as heart failure, arrhythmias, cardiac rupture, and left ventricular thrombus, contribute to a poor prognosis. Despite the inclusion of antiplatelet agents and statins in the conventional treatment regimen, their clinical applicability is constrained by potential adverse effects and limited efficacy. Additionally, the mechanisms leading to MI are complex and diverse. Therefore, the development of novel compounds for MI treatment. The use of traditional Chinese medicine (TCM) in the prevention and treatment of cardiovascular diseases, including MI, is grounded in its profound historical background, comprehensive theoretical system, and accumulated knowledge. An increasing number of contemporary evidence-based medical studies have demonstrated that TCM plays a significant role in alleviating symptoms and improving the quality of life for MI patients. Chinese herbal formulations and active ingredients can intervene in the pathological process of MI through key factors such as inflammation, oxidative stress, apoptosis, ferroptosis, pyroptosis, myocardial fibrosis, angiogenesis, and autophagy. This article critically reviews existing herbal formulations from an evidence-based medicine perspective, evaluating their research status and potential clinical applications. Additionally, it explores recent advancements in the use of herbal medicines and their components for the prevention and treatment of MI, offering detailed insights into their mechanisms of action.

The appearance, active components, antioxidant activities, and their markers in fibrous roots of Bletilla striata.

This study explores the potential medicinal properties of Bletilla striata fibrous roots by comparing their active ingredient contents and antioxidant activity with those in tubers. The study further examines the effects of growth age and origin on the distribution characteristics of medicinal properties in fibrous roots and identifies biomarkers that distinguish these characteristics. The Δ E value of fibrous roots significantly increases with age and is significantly influenced by origin; both the age and origin also significantly affect militarine content and antioxidant activity; a positive correlation exists between appearance quality, active ingredients, and antioxidant activity. The total phenolic content and antioxidant activity of fibrous roots significantly exceed those of tubers. The militarine content in both 1-year-old and 2-year-old fibrous roots complies with the 2020 edition of the Chinese Pharmacopoeia, suggesting that the fibrous roots possess medicinal potential. Additionally, this study demonstrates that the OPLS-DA model can differentiate 1-year-old and non-1-year-old fibrous roots of Bletilla striata and distinguish between their origin.

A comprehensive update on over the counter artificial tears.

Artificial tears play a critical role in the management of dry eye disease (DED), providing patient symptomatic relief and improving ocular surface health. Its clinical importance has driven pharmaceutical innovation in terms of its formula and ingredients. The following article is an overview of the artificial tear products on the market. The artificial tears on the market vary in terms of their active ingredients, inactive ingredients, preservatives, and formulation. The particular chemical composition of ingredients and formulation plays a clinical role in treating ocular pathology. Conversely, certain ingredients can cause more ocular damage than other ingredients. Upon review of the artificial tears on the market, the authors conclude that clinicians should consider the products' composition when designating a treatment for DED. Different artificial tear composition may benefit specific causes of DED such as evaporative, aqueous-deficient, glaucoma, ocular surface tumors, corneal ulcers, and viral conjunctivitis.