Pharmacological Potential Research Articles

Isolation of Bacillus Velezensis from Leepuram Sea Sediment and Its Bioactive Compound and Antimicrobial Activity

Research into marine bacteria in India for their potential active chemicals is essential for the creation of medications derived from marine sources. The objective of this research was to collect Bacillus velezensis from Leepuram Sea Sediment, test their antibacterial efficacy with the agar diffusion method, and find secondary metabolites by GC-MS spectroscopy.Traditional microbiological methods and phylogenetic analysis of 16S rRNA sequences were used to successfully identify Bacillus velezensis from sediment samples obtained in the Leepuram Sea, Kanyakumari. Using the agar well diffusion method, we tested the isolated metabolites for their antibacterial activity against Gram-positive and Gram-negative bacteria. The results showed that the extract had a strong antibacterial effect, inhibiting the growth of harmful bacteria with zones of inhibition as large as 19 mm for E. coli and Pseudomonas.Bacillus velezensis produces secondary metabolites with pharmacological potential, according to this study. These metabolites may have useful uses in biocontrol, agriculture, and medicine. The implications of these results for human health and the creation of new antimicrobial drugs are likely to grow substantially when more worldwide research is carried out.

Unraveling neuroprotection with Kv1.3 potassium channel blockade by a scorpion venom peptide.

Voltage-gated potassium channels play a crucial role in cellular repolarization and are potential therapeutic targets in neuroinflammatory disorders and neurodegenerative diseases. This study explores Tityus bahiensis scorpion venom for neuroactive peptides. We identified the αKtx12 peptide as a potent neuroprotective agent. In SH-SY5Y cells, αKtx12 significantly enhances viability, validating its pharmacological potential. And in the animal model, we elucidate central nervous system (CNS) mechanism of αKtx12 through neuroproteomic analyses highlighting αKtx12 as a valuable tool for characterizing neuroplasticity and neurotropism, revealing its ability to elicit more physiological responses. The peptide's potential to promote cell proliferation and neuroprotection suggests a role in functional recovery from nervous system injury or disease. This research unveils the neuroactive potential of scorpion venom-derived αKtx12's, offering insights into its pharmacological utility. The peptide's impact on neuronal processes suggests a promising avenue for therapeutic development, particularly in neurodegenerative conditions.

Unveiling the Biological Activities, Pharmacological Potential, and Health Benefits of Sorbifolin: A Comprehensive Review.

Bioactive phytochemicals act as important factors with preventive and therapeutic potential in the pathogenesis of several disorders, often related to oxidative stress. Many dietary plant secondary metabolites could lower these conditions. Sorbifolin is one of these metabolites. This work is the first review of sorbifolin, a flavone detected in various plant matrices as a major compound. The present study discussed the natural sources, extraction, purification, quantification, and assessment of the biological activities of sorbifolin. Several databases including Google Scholar, Web of Sciences, and Science-Direct were consulted for relevant English articles related to sorbifolin, the phytochemical profiles of several medicinal plants containing this compound, and its biological activities, such as antioxidant, anticancer, antimicrobial, anti-inflammatory, and antidiabetic. The positive in vitro and in silico outcomes reported in the literature should be followed by additional in vivo and clinical investigations to further research the mechanisms of action, pharmacokinetic/pharmacodynamic activities, toxicological effects, pharmacological properties, and therapeutic potential of sorbifolin.

Anti-diabetic effects of marine natural products through redox modulation via Nrf2/HO-1 cytoprotective pathways

Diabetes mellitus (DM), a major global health concern, is a chronic metabolic disorder. Bioactive compounds sourced from numerous marine natural products recently have drawn attention as novel therapeutic approaches. Considering these chemicals and their role in cellular redox modulation by involving the nuclear factor erythroid 2-related factor 2 (Nrf2)/heme oxygenase 1 (HO-1) pathway, the current study attempts to highlight their anti-diabetic effects and the molecular mechanisms involved. Reactive oxygen species (ROS)-mediated oxidative stress, inflammation, and cellular damage are linked to most human pathologies specifically DM. The Nrf2/HO-1 pathway is a key defense mechanism developed by the cells to combat ROS burst. Marine natural compounds have strong pharmacological potential in triggering cellular antioxidant defense mechanisms by declining oxidative damage and inflammation linked to DM. How marine natural products potentially alleviate DM specifically type 2 diabetes (T2D) and its related issues is especially focused on. The literature was thoroughly analyzed to open a discussion about specific marine compounds and their well-established anti-diabetic effects to elucidate possible therapeutic applications. Furthermore, opportunities and the pros and cons of using these marine bioactive compounds as complementary treatment for DM are also discussed. The diverse characteristics of marine natural products, specifically with regard to redox control, offer promising opportunities for drug discovery and therapeutic interventions in clinical trials.

Biochemical Analysis of Fruiting Bodies of Cordyceps Militaris Grown on Brown Rice

Cordyceps militaris is a medicinal fungus known for its diverse biofunctional properties. This subject has been extensively analyzed over the past decade. The diverse pharmacological potential of C. militaris has garnered significant global interest recently. This research aims to determine the proximate composition of in vitro cultivated C. militaris fruit bodies. The analysis of proximate composition included measurements of crude protein, fat, crude fiber, ash, total carbohydrate, and moisture content. The research focused on quantifying the overall nutritional value of the fruit bodies and evaluating biological efficiency, in addition to key bioactive compounds including cordycepin, ergosterol, and Vitamin D2. The results demonstrated that the carbohydrate content constituted 47.67% of dry weight, the protein content was 30.41%, and the fiber content accounted for 15%. The fruit bodies contained 39.82 mg/kg of cordycepin and 61.73 mg/100g of ergosterol, whereas vitamin D2 was absent in the cordyceps mushroom sample. The findings demonstrate that in-vitro-cultivated C. militaris fruit bodies exhibit considerable nutritional and therapeutic potential.

Ameliorative Potential of Sudachitin Against Paraquat Induced Renal Toxicity in Rats Via Regulating Nrf2/Keap1 Pathway: An Inflammatory, Apoptotic and Histopathological Assessment

AbstractParaquat (PQ) is a noxious herbicide which is well known for its adverse effects on vital organs including kidneys. Sudachitin (SCN) is a plant derived flavone that is obtained from Citrus sudachi and demonstrates a range of pharmacological potentials. This investigation was executed to assess the protective effects of SCN to counteract PQ instigated renal damage in albino rats (Rattus norvegicus). Twenty‐four rats were apportioned in 4 different groups i. e., control group, PQ (5 mg/kg) intoxicated group, PQ (5 mg/kg)+SCN (20 mg/kg) cotreated group and SCN (20 mg/kg) only administrated group. Our findings revealed that exposure to PQ reduced the expressions of Nrf2 (nuclear factor erythroid 2–related factor 2) and its cytoprotective genes while escalating the expression of keap1. Furthermore, PQ intoxication reduced the activities of superoxide dismutase (SOD), catalase (CAT), glutathione reductase (GSR), heme‐oxygenase‐1 (HO‐1) and glutathione (GSH) contents while increasing the levels of malondialdehyde (MDA) and reactive oxygen species (ROS). Moreover, PQ exposure significantly increased the levels of neutrophil gelatinous‐associated lipocalin (NGAL), urea, kidney injury molecule‐1(KIM‐1) as well as creatine while reducing creatine clearance. Additionally, PQ upregulated the levels of inflammatory markers including interleukin‐6 (IL‐6), tumor necrosis‐ α (TNF‐ α), nuclear factor‐ κB (NF‐κB), interleukin 1beta (IL‐1β), and cyclo‐oxygenase‐2 (COX‐2). Moreover, PQ administration upregulated the expression of Bax (Bcl‐2–associated X protein) and (cysteine–aspartic acid protease) Caspase‐3 while downregulating the expressions of (B‐cell lymphoma 2 protein) Bcl‐2. Besides, PQ exposure prompted various histopathological damages in renal tissues. Nonetheless, SCN substantially restored aforementioned alterations in the renal tissues owing to its anti‐oxidative, anti‐inflammatory and anti‐apoptotic potential.

In silico prediction of the pharmacological potential of new 7-alkyl-8-hydrazine derivatives of 1,3-dimethylxanthine

The development of new drug-like molecules based on 7-R-8-hydrazine derivatives of 1,3-dimethylxanthine is promising in view of the known pharmacological effect of theophylline and functional hydrazine derivatives. In silico methods make it possible to rationalize the synthesis and reduce the number of chemical compounds at the stage of virtual screening by eliminating potentially ineffective molecules. The aim of the work was to carry out а virtual design and predictive evaluation of pharmacological activity of new 7-alkyl-8-hydrazine derivatives of 1,3-dimethylxanthine by in silico methods. Materials and methods. To perform in silico prediction of the pharmacological potential of several new 7-alkyl-8-hydrazine derivatives of 1,3-dimethylxanthine, we used the online services. As 12 model compounds, we chose 12 derivatives of 5-(2-(1,3-dimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl)hydrazine)-5-phenylpentanoic acid with linear and branched alkyl substituents at the 7th position of the basic heterocycle: methyl-, ethyl-, n-propyl-, n-butyl, i-butyl, n-amyl, i-amyl, n-hexyl, n-heptyl, n-octyl, n-nonyl, n-decyl. The use of the freely available web tool SwissADME made it possible to calculate physicochemical parameters and to determine the drug-likeness properties of molecules. And other Internet platforms allowed to predict the spectrum of biological activity of the target compounds. Results. In silico analysis of the pharmacological potential of model compounds was performed. Three biological actions (peripheral vasodilator, kidney function stimulant, lipoprotein lipase inhibitor) with high Pa values are predicted for all derivatives of the series. The ADME parameters of the molecules were evaluated and their potential drug-like properties were determined. Conclusions. It was established that the extension of the alkyl substituent at the 7th position of the basic heterocycle should lead to a deterioration of the ADME parameters of the molecules, potentially reduce their oral bioavailability, but should not radically affect their biological activity profile. Compounds 1–3 and 5 are predicted to be orally bioavailable. They should be characterized by a wide spectrum of biological activity with the highest probability of vasodilator effect on peripheral vessels. In the future, it is advisable to carry out targeted synthesis of hit compounds and thorough in vitro, in vivo studies, and for compounds with violated physicochemical criteria – structural optimization of molecules in order to find a lead compound.

Exploring the mechanism of sesamin for the treatment of PM2.5-induced cardiomyocyte damage based on transcriptomics, network pharmacology and experimental verification

IntroductionExposure to fine particulate matter (PM2.5) is known to be associated with cardiovascular diseases. Sesamin (Ses) is a natural phenolic compound found in sesame seeds and sesame oil. Ferroptosis is a novel mode of cell death characterised by iron-dependent lipid peroxidation. This study aims to explore whether PM2.5 can induce ferroptosis in H9C2 cells and to investigate the precise protective mechanism of Ses.MethodsBased on transcriptomic data, PM2.5 may induce ferroptosis in cardiomyocytes. The ferroptosis inducer erastin and ferroptosis inhibitor ferrostatin-1 (Fer-1) were used to illustrate the mechanisms involved in PM2.5-induced H9C2 cell injury. Using network pharmacology, the pharmacological mechanism and potential therapy targets of Ses were explored for the treatment of PM2.5-induced cardiomyocyte injury. H9C2 cells were cultured and pretreated with Fer-1 or different concentrations of Ses, and then cardiomyocyte injury model was established using erastin or PM2.5. Indicators of oxidative responses, including total superoxide dismutase, reduced glutathione, glutathione peroxidase and malondialdehyde, were measured. The expression levels of ferroptosis-related proteins were determined through Western blot analysis.ResultsResults demonstrate that PM2.5 induces ferroptosis in H9C2 cells and Ses exerts a protective effect by suppressing ACSL4-mediated ferroptosis.DiscussionOverall, these findings elucidate a novel mechanism by which Ses ameliorates the detrimental effects of PM2.5 on cardiomyocytes.

Antibacterial Properties in Fermentate Extracts of Endophytic Fungus Derived from Marine Algae Caulerpa lentillifera Against Gastrointestinal Pathogenic Bacteria

Endophytic fungi, residing symbiotically within living plant tissues, are a promising source of novel bioactive compounds. These fungi are known to produce secondary metabolites with a wide range of biological activities, including antibacterial properties. This study explored the antibacterial potential of fermented extracts from endophytic fungi isolated from the marine alga Caulerpa lentillifera, a food source consumed by coastal communities and traditionally used for medicinal purposes. Thin-layer chromatography (TLC) bioautography was employed to identify extracts with activity against common gastrointestinal pathogenic bacteria, such as Escherichia coli, Shigella dysenteriae, and Salmonella typhi. Two endophytic fungal isolates displayed promising antibacterial activity against these pathogens. TLC analysis tentatively identified the presence of flavonoids and alkaloids, potentially responsible for the observed effects. This research sheds light on the pharmacological potential of endophytic fungi and their applications in combating bacterial infections.

Effects of Arnica Phytotherapeutic and Homeopathic Formulations on Traumatic Injuries and Inflammatory Conditions: A Systematic Review.

Arnica L. genus (Asteraceae) comprises perennial herbs native to the temperate and boreal parts of the northern hemisphere. Arnica montana is the main species. It shows different biological activities, such as antioxidant, anti-inflammatory, antibacterial, antifungal, and antitumor effects. The Arnica formulations are mainly used for pain management. This systematic review is aimed at summarizing the studies focusing on the use of Arnica products on pain and inflammatory signs due to traumatic injuries related to sport and surgical interventions as well as to arthritis and other inflammatory conditions. Both phytotherapeutic and homeopathic formulations are taken into account. This paper only includes manuscripts published in mainstream journals. A literature search from Scopus, Web of Science, and PubMed databases has been carried out using a combination of the keywords "Arnica", "trauma", "sport", "injury", "injuries", and "pain". According to the search strategy and inclusion criteria for this study, 42 eligible papers, focusing on both Arnica alone and formulations containing a mixture of plant extracts, have been finally selected. This review critically discusses the in vitro, in vivo, and clinical studies dealing with Arnica products, reporting both positive and negative outcomes, thus providing perspectives for future research on the plant pharmacological potential.

Machine Learning Framework for Conotoxin Class and Molecular Target Prediction

Conotoxins are small and highly potent neurotoxic peptides derived from the venom of marine cone snails which have captured the interest of the scientific community due to their pharmacological potential. These toxins display significant sequence and structure diversity, which results in a wide range of specificities for several different ion channels and receptors. Despite the recognized importance of these compounds, our ability to determine their binding targets and toxicities remains a significant challenge. Predicting the target receptors of conotoxins, based solely on their amino acid sequence, remains a challenge due to the intricate relationships between structure, function, target specificity, and the significant conformational heterogeneity observed in conotoxins with the same primary sequence. We have previously demonstrated that the inclusion of post-translational modifications, collisional cross sections values, and other structural features, when added to the standard primary sequence features, improves the prediction accuracy of conotoxins against non-toxic and other toxic peptides across varied datasets and several different commonly used machine learning classifiers. Here, we present the effects of these features on conotoxin class and molecular target predictions, in particular, predicting conotoxins that bind to nicotinic acetylcholine receptors (nAChRs). We also demonstrate the use of the Synthetic Minority Oversampling Technique (SMOTE)-Tomek in balancing the datasets while simultaneously making the different classes more distinct by reducing the number of ambiguous samples which nearly overlap between the classes. In predicting the alpha, mu, and omega conotoxin classes, the SMOTE-Tomek PCA PLR model, using the combination of the SS and P feature sets establishes the best performance with an overall accuracy (OA) of 95.95%, with an average accuracy (AA) of 93.04%, and an f1 score of 0.959. Using this model, we obtained sensitivities of 98.98%, 89.66%, and 90.48% when predicting alpha, mu, and omega conotoxin classes, respectively. Similarly, in predicting conotoxins that bind to nAChRs, the SMOTE-Tomek PCA SVM model, which used the collisional cross sections (CCSs) and the P feature sets, demonstrated the highest performance with 91.3% OA, 91.32% AA, and an f1 score of 0.9131. The sensitivity when predicting conotoxins that bind to nAChRs is 91.46% with a 91.18% sensitivity when predicting conotoxins that do not bind to nAChRs.

Pharmacological Potential of Sulindac and Its Active Metabolite: A Comprehensive Review

: In this review, we describe and discuss the pharmaceutical aspects, pharmacokinetic profile, and preclinical and clinical studies of sulindac and its active metabolite and emphasise their potential activity not only in anti-inflammation strategies but also as chemoprevention drug candidates. Though they are widely validated through in vitro and in vivo models, to date, no efforts have been made to compile in a single review on their pharmacologically potential, pharmacokinetics and toxicity profiles. Key databases such as PubMed, Science Direct, Scopus, and Google Scholar, among others, were probed for a systematic search using keywords to retrieve relevant publications. An exhaustive electronic survey of the related literature on the pharmacologically potential activity and the pharmacokinetic and toxicity profiles of sulindac resulted in around 200 articles (1975 and 2023) being included. The studies conducted on sulindac sulphide and sulindac sulfone metabolites reported a varied range of biological effects deployed in this review. The review concluded that there is scope for repurposing sulindac using computer-aided drug design and biological study to find out possible new targets for strengthening the potency and selectivity of the metabolites.

The antisickling agent, 5-hydroxymethyl-2-furfural: Other potential pharmacological applications.

For the last two decades, the aromatic aldehyde 5-hydroxymethyl-furfural (5-HMF) has been the subject of several investigations for its pharmacologic potential. In 2004, the Safo group reported that 5-HMF has potent antisickling activity by targeting and ameliorating the primary pathophysiology of hypoxia-induced sickling of erythrocytes (red blood cells [RBC]). Following the encouraging outcome of the preclinical and phase I/II clinical studies of 5-HMF for the treatment of sickle cell disease (SCD), there have been multiple studies suggesting 5-HMF has several other biological or pharmacologic activities, including anti-allergic, antioxidant, anti-hypoxic, anti-ischemic, cognitive improvement, anti-tyrosinase, anti-proliferation, cytoprotective, and anti-inflammatory activities. The wide range of its effects makes 5-HMF a potential candidate for treating a variety of diseases including cognitive disorders, gout, allergic disorders, anemia, hypoxia, cancers, ischemia, hemorrhagic shock, liver fibrosis, and oxidative injury. Several of these therapeutic claims are currently under investigation and, while promising, vary in terms of the strength of their evidence. This review presents the research regarding the therapeutic potential of 5-HMF in addition to its sources, physicochemical properties, safety, absorption, distribution, metabolism, and excretion (ADME) profiles.

Identifying Dental Pulp Stem Cell as a Novel Therapeutic trategy for Digestive Diseases.

Mesenchymal stem cells (MSCs) have been identified as potential therapeutics for various diseases. In contrast to other sources of MSCs, dental stem cells (DSCs) have received increased attention due to their high activity and easy accessibility. Among them, dental pulp stem cells (DPSCs) exhibit superior self-renewal, multipotency, immunomodulatory, and regenerative capacities. Following their inspiring performance in animal models and clinical trials, DPSCs show pharmacological potential in regenerative medicine. In this review, we have generalized the sources, heterogeneity, and biological characteristics of DPSCs, as well as compared them with other types of dental stem cells. In addition, we summarized the application of DPSCs in digestive diseases (such as liver, esophageal, and intestinal diseases), highlighting their regenerative and pharmacological potential based on the existing preclinical and clinical evidence. Specifically, DPSCs can be home to injured or inflamed tissues and exert repair and regeneration functions by facilitating immune regulation, anti-inflammation, and directional differentiation. Although DPSCs have a rosy prospect, future studies should handle the underlying drawbacks and pave the way for the identification of DPSCs as novel regenerative medicine.

Phytochemical and toxicological evaluation of aqueous leaf extract of Premna integrifolia L. in male balb/c mice.

BackgroundPhytoconstituents present in plants provide a natural and comprehensive method for combating oxidative stress and various ailments. Safety evaluation of these herbal medications is necessary, so acute and sub-acute toxicity of plant leaf extract Premna integrifolia has been performed to standardize its dose regarding its therapeutic application in male fertility. PurposeToxicological evaluation Aqueous leaf extract of Premna integrifolia (ALEPI), a known herbal medicine, for its utilization in male fertility enhancement use. Study design and methodsTo assess the safety and pharmacological potential of the ALEPI, acute and subacute toxicity studies were carried out in compliance with the OECD guidelines No. 425 and 407, respectively. Identification of pharmacologically active compounds in ALEPI was performed using UHPLC-HRMS analysis. In vitro,estimation of Polyphenol Content, Total Flavonoid Content, saponins and Antioxidant Properties of ALEPI was performed. The oral acute toxicity of the ALEPI was conducted using male mice. The study involved administering single doses of ALEPI at 300, 2000, and 5000 mg/kg b.wt., followed by a fourteen-day observation period to monitor any signs of toxicity or adverse effects. In the oral subacute toxicity study, mice received daily oral gavage of the ALEPI at doses of 400, 800, and 1000 mg/kg b.wt. for twenty-eight days. The parameters studied included total reactive oxygen species (ROS) production, apoptosis, cell viability percentage, and cellular morphology. ResultsThe UHPLC-HRMS analysis of the ALEPI reveals the presence of various bioactive compounds with significant antioxidant, anti-inflammatory, and anticancer properties. The acute and subacute toxicity studies of the ALEPI provided a comprehensive evaluation of its safety profile. Both studies demonstrated no mortality and only minor alterations in relative organ weights, hematology, and serum biochemistry, suggesting a low toxicity profile. Additionally, the normal histoarchitecture of vital organs indicates the absence of significant morphological changes. Significant reduction in total ROS, necrosis percentage, and apoptosis in testicular tissue compared to the control group highlights the antioxidant properties of the extract. ConclusionBased on the findings from both the acute and subacute toxicity studies, it is evident that the ALEPI does not actuate adverse effects of toxicological significance at the tested doses and hence can be used at appropriate concentrations in therapeutic application.

Isoliquiritigenin alleviates SLC7A11-mediated efferocytosis inhibition to promote wounds healing in diabetes

The healing process of chronic wounds often progresses slowly and is fraught with challenges, imposing increasing economic burdens and physical suffering on patients. Managing persistent wound inflammation and stimulating angiogenesis are crucial elements in promoting wound healing. Plants have been playing a key role in traditional medicine, and their abundant bioactive components continually inspire the development and innovation of new drugs. Isoliquiritigenin (ISL), a flavonoid compound derived from licorice roots known as chalcone, has demonstrated multifaceted pharmacological potential. However, its effects on diabetic wounds and the detailed mechanisms remain to be investigated. Through in-depth exploration using network pharmacology, we successfully predicted potential therapeutic targets of ISL for ischemic diseases. The revealed mechanisms primarily focused on the critical pathway of efferocytosis. Subsequent in vivo experiments demonstrated that ISL significantly enhanced the efferocytosis of dendritic cells (DC), improving the functional behaviors of endothelial cells. Further research indicated that ISL promoted DC efferocytosis by regulating SLC7A11-mediated glycolysis. Notably, the overexpression of SLC7A11 diminished the positive effects of ISL, suggesting a potential antagonistic role of SLC7A11 in the regulatory process. In the wounds of diabetic mice, we observed that ISL accelerated DC efferocytosis and angiogenesis, resulting in faster wound closure and better tissue repair. In summary, this study not only demonstrates the broad potential of ISL in managing diabetic wounds but also delves deeply into its mechanisms, laying a solid theoretical foundation for future clinical applications.

Regulatory Effects of Ishige okamurae extract and Diphlorethohydroxycarmalol on Skin Barrier Function

Ethnopharmacological relevanceThe pharmacological potential of marine organisms remains largely unexplored. Ishige Okamurae, commonly known as Pae, is extensively distributed over Asia. Its antioxidant, antibacterial, antiobesity, and anti-inflammatory properties are also being investigated. Aim of the studyIn most cases of atopic dermatitis, the stratum corneum, the outermost layer of the epidermis, is damaged, causing symptoms such as dryness and hyperproliferation of the epidermis. In particular, the disruption of cell junctions leads to damage of the skin barrier, exacerbating the disease and becoming a target for therapeutic development. Our study aims to investigate of Ishige okamurae extract (IOE) and a major compound derived from it, called Diphlorethohydroxycarmalol (DPHC), can help strengthen the skin barrier in animals with atopic dermatitis induced by 2,4-dinitrochlorobenzene (DNCB). Materials and methodsIn keratinocyte cell lines, HaCaT cells, the cytotoxicity of IOE and DPHC was assessed by MTT analysis. The gene expression of skin barrier factors and tight junctions were determined by real-time PCR in tumor necrosis factor-α/interferon-γ-stimulated HaCaT cells. In addition, JAK/STAT signaling pathway was performed to evaluating the mechanism of drugs by Western blot. Next, we studied the effects of IOE and DPHC on the skin of animals with DNCB-induced atopic dermatitis. We measured the expression of genes related of the skin barrier and tight junctions in their ear tissue. ResultsAs a result, IOE and DPHC confirmed that the expression of skin barrier proteins (thymic stromal lymphopoietin, filaggrin, loricrin, and involucrin) was improved in the DNCB-induced atopic dermatitis model and HaCaT cells. In addition, the expression of tight junction-related proteins (claudin, occludin, and tight junction protein-1) were improved. ConclusionIOE and DPHC ameliorated the atopic dermatitis lesions through alleviating the pro-inflammatory responses and tight junction protein destruction. Our results suggest that IOE and DPHC could be promising candidates for enhancing skin barrier function.

Synthesis and pharmacological activity evaluation of 2-(2-Phenylethyl)chromone analogues: The principal components in agarwood.

2-(2-Phenylethyl)chromones (PECs), the pivotal constituents responsible for the distinctive aroma and pharmacological potential of agarwood, are primarily obtained through extraction from natural materials. The restricted availability of agarwood has, however, hindered a comprehensive and systematic evaluation of their biological properties. In this study, we have chemically synthesized a total of 38 PEC derivatives, including 23 new compounds that had not been previously isolated from agarwood. These compounds were then evaluated for their inhibitory effects on nitric oxide release, neutrophil superoxide production, as well as their activities against tyrosinase, acetylcholinesterase, and α-glucosidase. The preliminary screening resulted in the identification of promising leads with potential therapeutic activities, and the structure-activity relationship of the synthesized PECs have also been briefly discussed. The results provide a foundation for the synthesis and pharmacological exploration of PECs, which sheds light on the pharmacological potential of agarwood's secondary metabolites.

Diverse Pharmacological Potential of different Substituted Pyrazole Derivatives.

The chemistry of heterocyclic compounds has been a topic of research interest. Some five-membered heterocyclic compounds have been the subject of extensive research due to their different types of pharmacological effects. The five-membered nitrogen-containing heterocyclic compounds pyrazole, pyrazoline, and pyrazolone derivatives have a lot of interest in the fields of medical and agricultural chemistry due to their diverse spectrum of therapeutic activities. Various substituted pyrazole, pyrazoline, and pyrazolone compounds exhibited diverse pharmacological effects like Anti-microbial, anti-inflammatory, anti-tubercular, anti-fungal, anti-malarial, anti-diabetic, diuretic, anti-depressant, anticonvulsant, antioxidant, anti-leishmanial, antidiabetic, and antiviral, etc. In recent decades, the synthesis of numerous pyrazole, pyrazoline, and pyrazolone derivatives by different synthetic methods as well as research into their chemical and biological behavior have become more important. This review focuses on synthetic methods of the pyrazole, pyrazoline, and pyrazolone derivatives, which have significant biological properties and a variety of applications.

Ethnobotany, Phytochemistry, and Pharmacological Activity of Dioscorea bulbifera: A Comprehensive Review.

Dioscorea bulbifera (Family: Dioscoreaceae) also referred to as 'Air potato,' carries significant importance in the traditional medicine of China, West Africa and India. It is a common ingredient in numerous herbals and Ayurvedic formulations used to treat a variety of ailments. The literature review extensively examined the historical usage, phytoconstituents, characterisation of phytoconstituents, and medicinal uses of tubers, leaves, rhizomes and bulbils, with a particular focus on comparing research findings. Among the bioactive constituents, aglycone forms of steroidal saponins such as dioscorine, dioscin, diosbulbins, and diosgenin exhibit significant biological activities. Extracts from different parts of the plant exhibited pharmacological activities like anti-viral, anti-malarial, analgesic, antidiabetic, and anticancer. It is necessary to conduct an in-depth investigation to bridge between traditional knowledge and scientific evidence. This comprehensive review aims to provide a detailed understanding of the ethnobotany, phytoconstituent, chemical characterization and pharmacological potential of D. bulbifera, highlighting its prospects and challenges for future research and medicinal application.