Pharmacological Effects Research Articles

Study on the mechanism of hyperoside in affecting the biological progression and radiosensitivity of esophageal carcinoma by modulating the STAT3/AKT/ERK pathway

Hyperoside (HYP) exhibits diverse pharmacological effects and holds potential for enhancing chemotherapy sensitivity. However, few studies have reported the impact of HYP on the malignant progression of esophageal carcinoma (EC) and its sensitivity to radiotherapy. The impact of HYP on the viability of esophageal carcinoma cells (TE-1 and KYSE-150) was assessed using Cell Counting Kit-8 (CCK-8) assays. The biological characteristics and radiosensitivity of esophageal carcinoma cells following HYP treatment were evaluated through colony formation experiments, flow cytometry, scratch wound-healing assays, and transwell migration and invasion assays. Western blot analysis was performed to determine the levels of proteins associated with cell death and epithelial-mesenchymal transition (EMT), as well as to explore whether HYP interferes with the radiosensitivity of esophageal carcinoma cells via the STAT3/AKT/ERK pathways. Finally, a subcutaneous graft tumor model was constructed to investigate the effects of HYP and X-ray treatments on in vivo tumor growth. The findings indicated a dose-dependent decrease in the survival rate of KYSE-150 and TE-1 cells following HYP treatment. HYP treatment also inhibited cell proliferation, invasion, migration, and EMT, while increasing the apoptotic rate and radiosensitivity of the cells. Notably, HYP suppressed the malignant progression of EC and enhanced radiosensitivity via the STAT3/AKT/ERK pathway. Moreover, HYP impaired the growth of esophageal carcinoma tumors in mice, with the combined HYP and X-ray treatment exerting a stronger inhibitory effect. In conclusion, HYP increases the radiosensitivity of esophageal carcinoma cells, offering considerable promise for application in the clinical treatment of EC.

The role and mechanism of “eight famous herbals in Zhejiang” in cancer via network pharmacology and experimental validation

In recent years, some components and active ingredients from the herbal formula “eight famous herbals in Zhejiang” (Zhe-Ba-Wei) have been reported to possess antitumor properties. However, there is still no systemic study on the role and mechanism of Zhe-Ba-Wei in cancer. To systematically investigate the anticancer efficacy of Zhe-Ba-Wei, we first identified 16 reported active ingredients with gene targets associated with various types of tumors. Second, we screened these active ingredients and their responding multiple shared targets by analyzing the convergence of diverse and tumor-specific target sites and identified four crucial active ingredients (ferulic acid, quercetin, rutin, luteolin), which were characterized by 27 overlapping gene targets. Third, these 27 gene targets were subsequently mapped onto the Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway and Gene Ontology term, and among the 27 total potential targets, 12 were involved in plasma membrane function. Fourth, we investigated the binding affinities between the four crucial active ingredients and their potential targets such as EGFR and MET, both of which are well-known oncogenes in various cancers. Subsequently, an investigation of the computational ADMET properties showed that most of these four ingredients exhibited good ADMET properties. Finally, we found that three active ingredients (ferulic acid, luteolin, and quercetin) could inhibit the proliferation of NSCLC cells and decrease the protein expression of EGFR in a concentration-dependent manner. All these results shed light on the bioactive components, pharmacological effects, and drug development and utilization of Zhe-Ba-Wei, aiming to provide useful support for its further research and clinical application.

The potential of kaempferol in digestive system tumors: recent advances and mechanistic insights.

Digestive system neoplasms are a heterogeneous group of cancers characterized by diverse symptoms, complex diagnosis, and treatment. Prognosis is poor and influenced by multiple factors, making early detection and comprehensive treatment crucial for patient survival. Kaempferol, a flavonoid compound, has attracted attention due to its anti-tumor biological activity, holding promise as a potential drug for treating digestive system neoplasms. Derived from various plants such as cabbage, propolis, and grapefruit, this compound's anti-inflammatory, antioxidant, and other pharmacological effects have been confirmed. Research has found that kaempferol inhibits the occurrence and development of digestive system neoplasms by inducing apoptosis in cancer cells, inhibiting tumor cell proliferation, suppressing tumor metastasis and invasion, and enhancing the effects of other cancer treatment methods. This paper summarizes the role and mechanisms of kaempferol in the study of digestive system neoplasms, providing valuable insights for both scientists and clinical physicians engaged in this field. By detailing the various pathways through which kaempferol exerts its anticancer effects, the paper not only highlights its potential as a therapeutic agent but also opens avenues for further research into its applications.

Quantitative Trait Locus Mapping and Candidate Gene Analysis of the Contents of Three Tanshinone Components in Salvia miltiorrhiza Bunge.

Tanshinones are abietane diterpenoid quinone compounds with diverse biological activities and pharmacological effects found in Salvia miltiorrhiza. Leveraging the high-density genetic map established through our prior research endeavors, we conducted a quantitative trait locus (QTL) analysis pertaining to the concentrations of three major tanshinone components, cryptotanshinone, tanshinone I, and tanshinone IIA, in S. miltiorrhiza. This extensive investigation was conducted across three distinct planting environments, ultimately identifying a comprehensive repertoire of 27 discernible QTLs. These QTLs were mapped onto four distinct linkage groups (LG), namely LG1, LG5, LG6, and LG7, which explained 3.11%-37.85% phenotypic variation. Candidate genes were projected based on consistent QTLs detected for each active ingredient in three environments. Nineteen putative candidate genes involved in the regulation of tanshinone biosynthesis were identified. These genes participate in primary metabolic and multiple branching terpenoid biosynthesis pathways, forming a complex regulatory network. Our findings have the potential to offer novel insights into advancing the understanding of the regulatory mechanisms governing tanshinone biosynthesis. Furthermore, these results establish crucial groundwork for gene discovery, marker-assisted selection breeding, and map-based cloning of functional genes associated with tanshinone content in S. miltiorrhiza.

Khajur (Phoenix dactylifera L.): Medicinal importance in perspective of Unani medicine and pharmacological studies

The date palm (Phoenix dactylifera L.) is recognized as one of humanity's earliest cultivated plants, having served as a food source for over 6000 years. It holds a prominent status as the most favoured fruit in the Middle East and North Africa. Date fruit has a long history of consumption and traditional medicinal use. Whether eaten fresh or dried, dates offer a rich source of energy due to their exceptional nutritional content and extended shelf life. They provide an economical means of obtaining essential nutrients including carbohydrates, proteins, vitamins, minerals and dietary fibers. Furthermore, date fruit exhibits a diverse range of pharmacological effects including antimicrobial, anti-inflammatory, anti-diabetic, anticancer, antihyperlipidemic and many more. It is also beneficial in disorders of paralysis, sexual debility, fever etc. Date palm fruits offer a natural and safe alternative or complement to synthetic drugs in managing numerous health conditions. Keywords: Dates, Phoenix dactylifera, Arecaceae/Palmae, Khajur, Unani Medicine.

The Underrepresented Quinolinone Alkaloids in Genera Penicillium and Aspergillus: Structure, Biology, and Biosynthetic Machinery.

Quinolone alkaloids are N-heterocycles with extensive structural diversity, mainly derived from in fungi from anthranilic acid and amino acids as precursors with a wide range of biological activities as antifungal, antimicrobial, anti-inflammatory, and insecticidal activities. The quinolone basic skeleton comprised of either 2-quinolones or 4-quinolones generated more than one hundred compounds. Several reviews discussed quinolones; particularly, the fluoroquinolones, yet few studies tackled natural quinolones. Many of these quinolones were not assayed for their antimicrobial potential despite their unique stereospecificity, which can supersede synthetic quinolones if their discovery is coupled with OMICS techniques, biochemical and molecular strategies as heterologous expression to maximize their yield. Herein, we conducted a comprehensive review of the quinolone's family in Aspergillus and Penicillium species, the exclusive producers of quinolones whether they are soil, endophytic or marine derived highlighting their isolation, chemical structures, pharmacological effects, structure activity relationships if any, and biosynthetic machinery. We believe that our initiative will pave the way for further development of natural quinolones as future antimicrobial agents.

Cobalt‐Catalyzed Hydroarylation of 2,3‐Dihydrofuran to Access α‐Arylated Tetrahydrofurans

AbstractThe α‐arylated tetrahydrofurans, commonly found in biologically active molecules, exhibit diverse biological activities and pharmacological effects. The functionalization of 2,3‐dihydrofuran offers a potential route for the synthesis of substituted tetrahydrofurans. Nevertheless, the development of earth‐abundant metal‐catalyzed regioselective hydrofunctionalization of 2,3‐dihydrofuran for the synthesis of substituted tetrahydrofurans remains to be pursued. Herein, we report a cobalt‐catalyzed hydroarylation of 2,3‐dihydrofuran, which serves as the first example of cobalt hydride‐catalyzed alkene hydroarylation. This reaction provides an efficient method for the synthesis of α‐arylated tetrahydrofurans with high reaction efficiency, exclusive α‐arylation selectivity, and remarkable functional group compatibility.

Identification of Active Ingredients in Ginseng Volatile Oil: A Strategy Combining Computer Virtual Screening With Experimental Validation.

Ginseng volatile oil (GVO) is a valuable active ingredient in ginseng (Panax ginseng C. A. Mey.) with high research potential. Drying procedures alter the real composition of the fresh material, for example, the evaporation of compounds with low boiling point. In this study, the composition of volatile oil in fresh ginseng (FG), sun-dried ginseng (SDG), and red ginseng (RD) was systematically analyzed to clarify the dominant components of FG and their potential pharmacological effects, which provides a basis for application and development of FG. GVO was obtained through water vapor distillation and analyzed using GC-MS. Pattern recognition analysis was employed to differentiate components in three processed types of ginseng. Based on this analysis, the active ingredients and key targets were screened. The binding mode and affinity were verified using molecular docking technology. Finally, the anticancer activity of GVO was verified by cell experiments. A total of 53 components were identified in three processed types of ginseng by GC-MS. Among them, 32 differential components were screened by pattern recognition analysis. Ultimately, 6 active ingredients (panaxydol, nerolidyl acetate, falcarinol, cis-β-farnesene, γ-elemene, and β-elemene) and 15 key targets were determined by network pharmacology analysis. Molecular docking results revealed that β-elemene exhibited a higher affinity with EGFR, ESR1, and ERK2. Cell experiments indicated that GVO promotes apoptosis in cancer cells. This research proposed a strategy that integrated "component detection-virtual multitarget screening-active component prediction-experimental verification" to expedite the identification of active ingredients, providing insights for application of FG and the development of functional products.

A Pharmacovigilance Study on Psychotropic Agent-Induced Urinary Retention Using the Japanese Adverse Drug Event Report Database.

Psychotropic drugs have been reported to cause urinary retention (UR) via anticholinergic and other mechanisms. However, UR has not received much attention because of its non-fatal symptoms. We investigated the occurrence of UR associated with psychotropic drugs using the Japanese Adverse Drug Event Report (JADER) database. Using the JADER database, we calculated reporting odds ratios for UR for 74 psychotropic drugs. Multivariate logistic regression analysis was used to adjust for the effects of sex, underlying disease, and age on UR. Variable selection included forced entry for sex, age, benign prostatic hyperplasia (BPH), depression, and backward-forward stepwise selection for each drug. A total of 887,704 cases were reported, of which 4653 (0.52%) had UR. In terms of sex, 0.79% (3401/429,372 cases) and 0.43% (1797/415,358 cases) of male and female patients had UR. In terms of age, 0.31% (892/288,676 cases) and 0.68% (3463/506,907 cases) of patients aged < 60 years and 60 years or older had UR. Among the underlying diseases, 8.22% (930/11,316 cases) and 0.43% (3723/876,388 cases) of patients with BPH and without BPH had UR, respectively. Further, 1.99% (337/16,959 cases) and 0.50% (4316/870,745 cases) of patients with depression and without depression had UR, respectively. Overall, 38 psychotropic drugs met the criteria for signal detection. In logistic regression, a total of 783,083 patients of discernible age and sex were included. The selected variables were sex, age, BPH, depression, and 23 drugs, including quetiapine [adjusted reporting odds ratio (ROR) 95% confidence interval (CI): 1.46-2.81], chlorpromazine (adjusted ROR 95%CI: 1.29-3.13), etizolam (adjusted ROR 95%CI: 1.47-3.09), maprotiline (adjusted ROR 95%CI: 1.99-8.34), mirtazapine (adjusted ROR 95%CI: 1.37-2.88), and duloxetine (adjusted ROR 95%CI: 2.15-4.21). Many psychotropic drugs induce UR, which may be owing to their pharmacological effects. Appropriate monitoring is needed, especially in patients with other risk factors for UR.

Influence of intestinal microbiota on the metabolism of main cardiotropic drugs

The intestinal microbiota is one of the most important pathogenetic links in the development of cardiovascular diseases. Every year the world scientific community finds new interactions at the level of signaling molecules, metabolites and microorganisms, identifying more and more patterns and cause-and-effect relationships which indicate the commonality of the intestinal microbiota (GM) and cardiovascular diseases. The state of the host's intestinal community, its qualitative and quantitative composition, directly and indirectly affects the fundamental pathogenetic mechanisms of the development of cardiovascular diseases. Despite the fact that there are scientifically based methods of treatment, cardiovascular diseases remain the leading cause of death in the world. This phenomenon is partly due to wide variations in individual response to cardiovascular drugs. The pharmacological effects of cardiotropic drugs are quite different even within groups of patients comparable in age and gender. Every year intestinal microbiota is more and more evident to be responsible for this intraspecific variability. Gut microbes influence drug metabolism in several pharmacokinetic ways, and conversely, drugs can have significant effects on the microbiome and therefore pharmacodynamic processes. Drugs can alter the gut microenvironment and microbial metabolism, influence bacterial growth, thereby changing the composition and functions of the microbial community. One of the most important functions of GM, related to “intestinal-cardiovascular system”, is participation in the metabolism of major cardiotropic medications, such as digoxin, statins, ezetimibe, antithrombotic drugs, calcium channel blockers (CCBs), beta blockers (BB), gliflozins and inhibitors of the renin-angiotensin-aldosterone system (RAAS).

Calycosin alleviates ferroptosis and attenuates doxorubicin-induced myocardial injury via the Nrf2/SLC7A11/GPX4 signaling pathway

BackgroundHeart failure is primarily characterized by damage to the structure and function of the heart. Ferroptosis represents a form of programmed cell death, and studies indicate that it constitutes one of the primary mechanisms underlying cardiomyocyte death in heart failure. Calycosin, a natural compound derived from astragalus, exhibits various pharmacological properties, including anti-ferroptosis, antioxidant effects, and cardiovascular protection. Nonetheless, the specific role of Calycosin in the treatment of ferroptosis in heart failure remains poorly understood.ObjectiveThis study aims to elucidate the regulatory effect of Calycosin on ferroptosis and its influence on the treatment mechanisms of heart failure through in vivo and in vitro experiments.MethodsA rat model of heart failure was induced using doxorubicin, and the cardiac function was evaluated through cardiac ultrasound examination and NT-Pro BNP detection. Myocardial injury was assessed using H&amp;amp;E staining and Masson staining. The extent of mitochondrial damage was evaluated through transmission electron microscopy. Concurrently, the level of ferroptosis was analyzed by measuring ferroptosis markers, including MDA, ferrous ions, the GSH/GSSG ratio, and GPX4 activity. Subsequently, the molecular mechanism by which Calycosin exerts its therapeutic effects in heart failure was investigated through immunofluorescence and Western blotting. Finally, H9c2 cardiomyocytes were treated with doxorubicin to simulate myocardial injury, and the mechanism by which Calycosin mediates its effects in the treatment of heart failure was further verified through Nrf2 gene silencing.ResultsCalycosin significantly improves cardiac function in rats, reduces serum NT-Pro BNP levels, and alleviates myocardial cell damage. Additionally, it significantly decreases the levels of ferroptosis in myocardial tissue, as confirmed through transmission electron microscopy and the assessment of ferroptosis markers, including MDA, ferrous ions, GSH, and GPX4 activity. At the molecular level, Calycosin exerts its effects by activating the Nrf2/SLC7A11/GPX4 signaling pathway, evidenced by the upregulation of Nrf2, SLC7A11, GPX4, GSS, and GCL protein expression. This process substantially enhances the antioxidant capacity of rat myocardial tissue and effectively suppresses ferroptosis in myocardial cells. The results obtained from both in vivo and in vitro experiments are consistent. Notably, when Nrf2 is silenced, the protective effect of Calycosin on the myocardium is markedly diminished.ConclusionCalycosin effectively treats doxorubicin-induced cardiac injury, and its therapeutic effect is likely closely associated with the activation of the Nrf2/SLC7A11/GPX4 signaling pathway and the inhibition of ferroptosis in myocardial cells. Consequently, Calycosin, as a promising compound against doxorubicin-induced cardiotoxicity, warrants further investigation.

Abstract 4138716: A novel Urocortin-2 analog COR-1167 corrects cardiac and renal dysfunction on top of Empagliflozin in a rat model of acute decompensated heart failure

Introduction: Urocortin-2 (UCN-2) is a peptide belonging to the corticotropin-releasing factor family that has cardiovascular, renal, metabolic and anti-inflammatory actions and improves cardiac function in human heart failure (HF) and cardiorenal dysfunction in chronic HF models. However, UCN-2 has a short half-life and intravenous delivery limits its therapeutic use. COR-1167 was discovered as a stable UCN-2 analog with qd pharmacological effects when injected subcutaneously. Hypothesis: Whether COR-1167 exerts chronic cardiorenal protection in Acute Decompensated HF (ADHF) is unknown, and in particular on background of SGLT2 inhibition, therefore both treatments were tested in a rat model of ADHF. Methods: Rats had coronary artery ligation to induce MI and a reduced ejection fraction phenotype. Three months later, rats were treated with vehicle or Empagliflozin (Empa) at 10 mg/kg/day PO. One month after starting Empa, two acute decompensation events were induced by administrating NaCl solution (1.8 g/kg, PO) on Day 0 and Day 14. Empa treated ADHF rats received vehicle or COR-1167 (3 µg/kg/day) by SC injections starting at 12 hours after the first decompensation and all treatments continued for 14 days. The groups were ADHF, ADHF + Empa and ADHF + Empa + COR-1167 (n=7-10/group). Left ventricular (LV) hemodynamics (cardiac catheters), cardiac output (echocardiography) and LV tissue perfusion (magnetic resonance imaging), cardiac mitochondrial coupling and ATP production (Seahorse) were measured 1 day after the second decompensation, while urine volume (uVol) and urine Na + excretion (uNa + ) collected from metabolic cages were analyzed 7 days after the first decompensation. Results: Compared to ADHF control rats, Empa treatment had no effect on systolic blood pressure (SBP), cardiac output (CO), LV end systolic pressure volume relationship (LVESPVR), LV end diastolic pressure volume relationship (LVEDPR), mitochondrial coupling and ATP production, but it increased myocardial perfusion, uVol and uNa + excretion. Compared to ADHF + Empa rats, COR-1167 treatment increased SBP, CO, LVESPVR, myocardial perfusion, mitochondrial coupling and ATP production, uVol, uNa + , while decreasing LVEDPVR. Conclusion: In the setting of ADHF, significant cardiorenal benefits and decongestion occurred when COR-1167 was administered on top of an SGLT2 inhibitor.

The Genus Commiphora: An Overview of Its Traditional Uses, Phytochemistry, Pharmacology, and Quality Control

Myrrh is the resinous substance secreted by plants of the genus Commiphora. In traditional Chinese medicine, Ayurvedic medicine, and traditional Arabic medicine, myrrh is regarded as an important medicinal material, widely used in the treatment of trauma, arthritis, hyperlipidemia, and other diseases. This review explores the evolving scientific understanding of the genus Commiphora, covering facets of ethnopharmacology, phytochemistry, pharmacology, artificial cultivation, and quality control. In particular, the chemical constituents and pharmacological research are reviewed. More than 300 types of secondary metabolites have been identified through phytochemical studies of this genus. Guggulsterone is a bioactive steroid isolated mainly from Commiphora mukul. The two isomers, Z- and E-guggulsterone, have shown a wide range of in vitro and in vivo pharmacological effects, including anti-proliferation, antioxidant, anti-inflammatory, and antibacterial. However, the current scientific research on quality control of medicinal materials and identification of original plants is insufficient, which limits the reproducibility and accuracy of biological activity evaluation experiments. Therefore, the establishment of analytical protocols and standardization of extracts is an important step before biological evaluation. At the same time, in order to find more bioactive substances, it is necessary to strengthen the research on the stems, barks, and leaves of this genus. The sources used in this study include PubMed, CNKI, Web of Science, Google Scholar, and other databases, as well as multinational pharmacopoeias, ancient books of traditional medicine, herbal classics, and modern monographs.

Research Progress on Pharmacological and Toxicological Effects of Bavachin

Objective: To analyze and summarize the latest research progress regarding pharmacological and toxicological effects of bavachin. Methods: Through retrieval of all bavachin-related reports on pubmed, CNKI, Wanfang database and other databases, the pharmacologic and toxicological effects of bavachin were sorted out and concluded accordingly. Results: The study showed that bavachin had a wide range of pharmacological activities, including estrogen-like, anti-inflammatory, anti-tumor, immunoregulatory, anti-diabetes and its complications effects. The toxicological effects of bavachin were mainly manifested in three aspects: hepatotoxicity, reproductive toxicity and nephrotoxicity. Conclusions: Bavachin has the characteristics of multi-function and multi-target monomer similar to traditional Chinese medicine, and broad application prospects, but also has certain toxicological effects. How to avoid toxicity, as well as enhance strengths and avoid weaknesses is the direction of development and utilization of bavachin. This review provides reference for further development and utilization of bavachin.

Influence of saponin tauroside Sx1 on lifespan and expression of vitamin D receptors in the liver tissue of mice with influenza infection

Introduction. Respiratory infections, including influenza, are often accompanied by hepatitis in humans which pathogenesis is not fully understood. According to the available datan D deficiency is presumably a risk factor in the occurrence of acute respiratory viral infections due to its modulation of immune response. Recent studies indicate that several plant compounds can interact with vitamin D receptors (VDRs) and modulate the activity of VDRs. The biologically active components saponins have found widespread use in clinical practice due to their wide range of biological and pharmacological effects which mechanisms are still largely unclear.Aim. To study the effect of oral administration of saponin tauroside Sx1, obtained from Crimean ivy, on life expectancy and activation of vitamin D receptors in the liver of mice during experimental viral infection of varying severity.Materials and methods. The 11 subgroups were formed from male BALB/c mice, were used in the experiment depending on the infectious dose of influenza virus, 5 LD50 virus or 10 LD50 virus, respectively, including control. Saponin tauroside Sx1 was used as a corrector. Immunohistochemical studies were carried out automatically in a BOND-MAX immunohistainer (Leica, Germany). Primary rabbit polyclonal antibodies to the vitamin D receptor were used.Results and discussion. Due to the administration of tauroside Sx1 at a dose of 200 μg/mouse/day increases the average life expectancy of animals receiving saponin by 4.6 days. Reducing the infectious dose of IV from 10 LD50 to 5 LD50 also changed the onset of death of animals by 2 days in both groups. With different infectious doses of the virus, on the 10th day of the experiment in the subgroups, the expression of vitamin D receptors changes without correction. In subgroup 2V, the number of total positive cells was lower than the control group. Moreover, in the 2Vir subgroup, VDR expression was significantly higher than the control group.Conclusion. The saponin tauroside Sx1 at a dose of 200 µg/mouse/day has a fairly pronounced antiviral effect during experimental infection of mice with the influenza A/H1N1 virus, which is manifested by an increase in the average life expectancy of animals (for 4.6 days) and a decrease in the mortality rate during severe influenza infection, compared with the control group, where 100 % mortality was observed by the 14th day of the experiment. The introduction of saponin on the 4th day of the experiment in all subgroups reduces the total number of immune cells that intensively express VDR.

Preliminary Exploration of the Protective Mechanism of Eugenol Against Acute Liver Injury Induced by Thioacetamide Based on Metabolomics

Acute liver injury (ALI) is a significant global public health issue that can rapidly develop into acute liver failure, seriously endangering the safety of patients. Eugenol has various pharmacological effects such as antioxidant, anti-inflammatory, antibacterial, and neuroprotective properties. Through pathological section observation, eugenol can alleviate the degree of liver damage caused by thioacetamide. Based on metabolomics, a total of 87 metabolites were found to have differences in content between the control group and the thioacetamide group. Compared with the control group, the contents of 42 metabolites had increased and 45 metabolites had decreased in the thioacetamide group. These differential expressed metabolites mainly indicate inflammatory damage, oxidative damage, and abnormal energy metabolism. There were 269 metabolites with differences in content between the eugenol intervention group and the thioacetamide group. Compared with the thioacetamide group, there were 101 metabolites with increased content and 168 metabolites with decreased content in the eugenol intervention group. These differential expressed metabolites suggest that eugenol intervention can correct inflammation damage, oxidative damage, and energy metabolism abnormalities caused by TAA. This study found through pathological section observation and metabolomics that eugenol has a protective effect on acute liver injury caused by thioacetamide, and the protective mechanism may be related to the antioxidant and anti-inflammatory effects of eugenol.

Global research hotspots and trends of Buyang huanwu decoction: A visual analysis of the literature based on CiteSpace.

Buyang huanwu decoction (BYHWD) has shown significant clinical efficacy in the treatment of several diseases, particularly stroke. However, bibliometric research has not been comprehensive. BYHWD articles were collected from literature databases published from January 1, 1915, to March 31, 2024, including the China National Knowledge Infrastructure, Weipu, Wanfang, Pubmed, Scopus, and Web of Science Core Collection. Knowledge network graphs of annual publication volume, authors, institutions, countries, keywords, and references were constructed. Nine thousand two hundred thirty-eight Chinese literature and 559 English articles published between 1915 and 2024 showed an overall upward trend. The countries, institutions, journals, and authors with the highest output were China, Hunan University of Chinese Medicine, Guangzhou University of Chinese Medicine, Guangxian Cai, and Changqing Deng, respectively. Research teams outside China were located at Daejeon University, Gachon University, Aga Khan University, Yale University, etc. The results of keyword co-occurrence and burst analysis included clinical applications, animal experiments, action mechanisms, clinical efficacy, and safety evaluations based on systematic reviews and meta-analyses. Literature co-citation analysis revealed that BYHWD was highly correlated with neuroprotection and reduction of cerebral ischemia/reperfusion injury. Both Chinese and English literature have shown overall growth trend since 1984 and 1989, respectively. Clinical applications, pharmacological effects, mechanisms, active ingredients, evaluation of clinical efficacy and safety, modified BYHWD, methods, and biological techniques may be hotspots and focus of future research on BYHWD. Hotspot analytical methods and biological techniques include systematic reviews, meta-analyses, data mining, network pharmacology, and molecular docking. Future valuable research fields may include studies on neuroprotection, anti-inflammatory activity, ischemic stroke, bioactive compounds, and their underlying mechanisms.

Analgosedation in Pediatric Emergency Care: A Comprehensive Scoping Review

Effective management of pain and anxiety in pediatric emergency room is crucial for ensuring both the physical and emotional well-being of young patients. Analgosedation, a combination of analgesia and sedation, is commonly used to facilitate various procedures in children. However, selecting the optimal agent and administration route remains challenging due to the unique pharmacological profiles and side effects of available drugs. This scoping review aims to provide a comprehensive analysis of the pharmacological agents used for procedural analgosedation in pediatric emergency settings, focusing on their efficacy, safety, administration routes, and potential side effects. A systematic review of the literature was conducted, focusing on key agents such as ketamine, midazolam, dexmedetomidine, fentanyl, and nitrous oxide. Studies were included based on their relevance to pediatric procedural sedation, particularly in emergency settings. Literature analysis showed that ketamine and fentanyl are effective for managing moderate to severe pain, with a rapid onset of action. Fentanyl is preferred for acute pain management following fractures and burns, while ketamine and midazolam are commonly used for emergency analgosedation. Dexmedetomidine, which induces sedation similar to natural sleep, is particularly effective in preventing pain and agitation during procedures and is well tolerated in children, especially those with developmental disorders. Nitrous oxide, when used in a 50% oxygen mixture, offers a valuable option for conscious sedation during mildly to moderately painful procedures, maintaining respiratory and airway reflexes. No single drug is ideal for all pediatric patients and procedures and the choice of agent should be tailored to the specific clinical scenario, considering both the sensory and affective components of pain. Future research should prioritize large-scale comparative studies, the exploration of combination therapies, and the development of non-pharmacological adjuncts to enhance the safety and efficacy of pediatric analgosedation.

Sulfonated Penta-Galloyl Glucose (SPGG): The Pharmacological Effects of Promiscuous Glycosaminoglycan Small Molecule Mimetic.

Sulfated glycosaminoglycans (SGAGs), such as heparin, are complex linear polysaccharides attached to core proteins via covalent bonds to form proteoglycans. SGAGs are crucial in assembling extracellular matrix, the regulation of cell signaling and cell behavior, hemostasis, development, and various diseases, including thrombosis, cancer, infectious diseases, and neurodegenerative disorders, through their binding with diverse proteins. Despite the abundant SGAG-protein interactions provided by nature, the development of small SGAG-like molecules remains underexplored. However, sulfonated penta-galloyl glucose (SPGG) represents a promising, easily synthesized, small-molecule mimetic of SGAGs, capable of harnessing these interactions. This minireview discusses the chemical synthesis and characterization of SPGG, along with its pharmacological effects derived from modulating the SGAG-protein interface.

Rapid Raman spectroscopy analysis assisted with machine learning: a case study on Radix Bupleuri.

Radix Bupleuri has been widely used for its plentiful pharmacological effects. But it is hard to evaluate their safety and efficacy because the concentrations of components are tightly affected by the surrounding environment. Thus, Radix Bupleuri samples from different regions and varieties were collected. Based on the experimental and computational Raman spectrum, machine learning is emphasized for certain obscured characteristics; for example, linear discriminant analysis (LDA), support vector machine (SVM), eXtreme gradient boosting (XGBoost) and light gradient boosting machine (LightGBM). After dimension reduction by LDA, models of SVM, XGBoost and LightGBM were trained for classification and regression prediction of Bupleurum production regions. Support vector classifiers achieved the best accuracy of 98% and an F1 score above 0.96 on the test set. Support vector regression has a good fitting performance with an R2 score above 0.90 and a relatively low mean square error. However, complex models were prone to overfitting, resulting in poor generalization ability. Among these machine learning models, the typical LDA-SVM models, consistent with the high-performance liquid chromatography results, demonstrate great performance and stability. We envision that this rapid classification and regression technique can be extended to predictions for other herbs. © 2024 Society of Chemical Industry.