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Dec 2025
Liu LipingCorresponding author
The incidence rate of melasma is notably high among patients with anxiety disorders. Aromatherapy primarily influences the physiological and psychological states of individuals through the inhalation or application of essential oils, thereby facilitating the treatment or alleviation of various conditions. This study aims to explore the action mechanism of complex lemon-angelica sinensis -boswellia essential oil (CEO) in treating anxiety disorders with melasma. We investigated the active ingredients, targets, and pathways of CEO in relation to anxiety and melasma using network pharmacology. We employed cell assays and conducted nebulized essential oil inhalation tests on CUMS mice to validate the intervention effects of CEO on anxiety. A total of 28 active components, including neryl acetate, 3-butenylphthalide and octyl acetate, and 26 cross-targets, such as ESR1, CCND1 and PIK3CA, were identified. GO and KEGG pathway analyses indicated that these cross-targets were primarily involved in endocrine regulation, cell proliferation, and apoptosis, specifically through PI3K/Akt signaling pathway and calcium signaling pathway. The experimental results demonstrated that CEO significantly reduced the secretion of NO, TNF-a and IL-6, as well as the mRNA expressions of ESR1, CCND1 and PIK3CA in cells compared to the inflammatory cell model. Furthermore, CEO notably decreased the forced swimming immobility time of mice and the levels of IL-1β, ESR1 and CCND1 in hippocampus when compared to model mice. These findings suggest that CEO may regulate ESR1, CCND1 and PIK3CA through its citral, 3-butylphthalate and neryl acetate, thereby influencing endocrine function, cell proliferation and apoptosis, inhibiting inflammation and anxiety-like behavior in CUMS-induced mice.
May 2024 DOI 10.14302/issn.2470-0436.jos-23-4493
Sun KexinCorresponding author
Background Beta-Sitosterol (SIT) is an active TCM compound employed to treat diabetic retinopathy (DR). A network pharmacology approach to understanding the active ingredients and the therapeutic mechanisms underlying DR has not been pursued. Methods The potential targets for DM were identified according to the MedGene, Gendome, HGNC, OMIM, GeneCards, PheGenI, GEO, and STRING database. The herb and components were predicted and screened by network pharmacology through oral bioavailability and drug-likeness filtration using the Traditional Chinese Medicine Systems Pharmacology Analysis Platform database. A network pharmacology prediction and network analysis were used to predict the active potential targets and pathways of SIT application to DR. Results We found the Top 15 DR-related genes by screening in 9 databases. 26 kinds of TCM and nearly 300 kinds of active ingredients. SIT exists in 10 kinds of DR-treat TCM. The comprehensive network pharmacology approach was successful in identifying 23 kinds of core genes for SIT treating DR. ERBB3 and IGF2-related PI3K-Akt signaling pathway or EDN3, IGF2 and SPP1-related receptor ligand activity pathway might be the main pharmacological targets, and pathways in DR. We speculated that SIT was effective for the treatment of DR. Conclusion Based on the network pharmacology, we predicted the potential targets of SIT in treating DR and helped to illustrate the mechanism of action. Our study identifies key genes and pathways associated with the prognosis and pathogenesis of DR from new insights.
Jan 2019 DOI 10.14302/issn.2574-612X.ijpr-18-2503
M Keppel Hesselink JanCorresponding author
Department of Health, University of Witten/Herdecke, Germany
Since the 2nd part of last century neo-shamanic rituals using mind-altering extracts from plants or animals have become increasingly popular in Europe and the USA. The first rituals coming to the west were based on drinking a special Amazonian tea, Ayahuasca, based on 2 different plants, with active compounds belonging to the class of the beta-carbolines (harmala alkaloids) and tryptamines. The use of such compounds will be described from the perspective of the transformative psychopharmacology: that part of psychopharmacology studying the use of psychoactive compounds to achieve a new balance, a transformation or healing and sometimes even leading to a cure. Examples of curing are meanwhile well documented, for instance the positive influence on drug abuse and addiction, alcoholism. The importance of the healing aspects of these rituals however are often neglected or overlooked. For users, these are key however. As medicine becomes more and more personalized and postmodern, it will be relevant to understand why patients and healthy people decide to participate in healing rituals based on psycho-active compounds. We will present the pharmacology, the transformative psychopharmacology, the effects and adverse events of 5-methoxy-N, N-dimethyltryptamine (5-MeO-DMT) and its place in postmodern medicine.
Dec 2025 DOI 10.14302/issn.2329-9487.jhc-25-5778
S Kallistratos ManolisCorresponding author
Calcium channel blockers (CCBs) are widely used for the treatment of arterial hypertension, but they differ in terms of pharmacology, tolerability, and pleiotropic actions. Lercanidipine, a highly lipophilic third generation dihydropyridine, reduces blood pressure (BP) effectively as monotherapy and in combination without inferiority to other major antihypertensive classes. We systematically searched PubMed and the Cochrane Library (last update: September 1, 2025) and screened reference lists for additional studies. Evidence from dose finding trials, randomized controlled studies, large observational cohorts, and meta analyses shows clinically meaningful reductions in office, home, and ambulatory BP with lercanidipine, including in patients with diabetes, obesity, chronic kidney disease, or high cardiovascular (CV) risk. Fixed- dose combinations with renin angiotensin system blockers (e.g., enalapril) provide greater BP reductions than monotherapy and are associated with favorable neurometabolic profiles. Beyond BP control, lercanidipine improves central hemodynamics and arterial stiffness, favors endothelial biology, and contributes to left ventricular hypertrophy regression. Across comparative trials, lercanidipine is generally better tolerated than older dihydropyridines. Presents lower rates of vasodilatory adverse events, less sympathetic activation, while discontinuations due to adverse events are uncommon. Overall, lercanidipine particularly within single pill combinations offers effective, durable BP lowering across diverse patient profiles with a favorable safety and tolerability profile and pleiotropic benefits that extend beyond BP reduction. Figure 1. Graphical Abstract: Pleiotropic effects of Lercanidipine
Jun 2019 DOI 10.14302/issn.2379-7835.ijn-19-2845
J. Johnson JeremyCorresponding author
University of Illinois at Chicago, College of Pharmacy, Department of Pharmacy Practice
The mangosteen fruit is a popular Southeast Asian fruit consumed for centuries. There have been a variety of xanthones isolated from the fruit, bark, roots and leaves with each having unique chemical and physical properties. Previously, the most abundant xanthone α-mangostin has been shown to inhibit CDK4. Herein we describe the role of selected xanthones from the mangosteen inhibiting CDK4. The evidence we provide here is that key functional groups are required to inhibit the CDK4 protein to prevent the phosphorylation of downstream targets critical to inhibiting uncontrolled cell cycle progression. To define the properties of xanthones for inhibiting CDK4 we utilized a cell free biochemical assay to identify inhibitors of CDK4. The following xanthones were used for the analysis: α-mangostin, β-mangostin, γ-mangostin, gartanin, 8-desoxygartanin, garcinone C and garcinone D, 9-hydroxycalabaxanthone, and 3-isomangostin These results further substantiate the unique pharmacological properties of individual xanthones and how a mixture of xanthones may be responsible for a multi-targeted effect in cell based pharmacology systems.
Aug 2018
Bai QifengCorresponding author
Key Lab of Preclinical Study for New Drugs of Gansu Province, School of Basic Medical Sciences, Lanzhou University, Lanzhou, Gansu 730000, P. R. China
Drug design, referred to the fields of pharmacology, biotechnology and medicine, is in silico, in vitro and in vivo assay processes of finding new candidate medications based on the biological targets. The in silicoexperiments of drug discovery are involved in the macromolecular structure databases, small molecule databases, molecular docking, de novo drug design and molecular dynamics simulations. The in vitro experiments of drug discovery need evaluate the direct interaction information between ligands and targets as well as the function of ligands on signaling pathway in the cell. The in vivo experiments of drug discovery give the convincing evidence for preclinical trial at the physiological level. In this review, we outline the drug design components of databases, virtual screening tools, biochemical assays, cell-based system and animal models.
Nov 2017 DOI 10.14302/issn.2576-9383.jhhr-17-1816
Abu Syed Md. MosaddekCorresponding author
Background: Disorders of lipid metabolism are manifested by elevation of the plasma concentration of the various lipid and lipoprotein fractions and the result, predominantly cardiovascular diseases. Lipid research clinic’s coronary primary prevention trial has provided useful information on the reduction of plasma cholesterol level in hyperlipidemic subjects by diet and drug therapy and thus the reduction in risk of myocardial infarction and death. Conventional lipid lowering drugs are used for lowering lipid level. But in the last few years’ herbal drugs are gaining popularity in the management of hyperlipidemia. In this study we compare the hypolipidemic effect of MomordicaCharantia (MC) with atorvastatin, a commonly used hypolipidemic drug. Methods: The present experimental study was done in the pharmacology department of Dhaka Medical College during the period of July, 2011 to June, 2012. For this study a total number of 30 Norwegian rats of either sex were selected. They were divided into 5 groups each comprises of 6 rats. In the experiment group A was given normal diet with high fatty diet (1.5 ml olive oil plus 1% cholesterol) which was control group and other experimental groups (B,C,D,) were allowed to feed a high fatty diet along with fresh juice of MomordicaCharantia (in different doses) for 10 days. Another experimental group, E was given high fatty diet along with atorvastatin (0.14mg/kg/day) for 10 days. Rats were sacrificed on 11th day and blood was collected by cardiac puncture for estimation of serum lipid profile. Results: After administration of fatty diet in group A for 10 days, there was significant increased total cholesterol (TCL), low density lipoprotein (LDL) and triglyceride (TG) levels. Concomitant administration of fatty diet and fresh juice of MC (in different doses) daily for 10 days in group B,C,D reduced serum TCL, LDL and TG levels which was more significant in higher doses in comparison to atorvastatin given group E. Conclusion: The present study provides a rationale for use a new herbal medicine much needed for the reduction of serum lipid levels.MomordicaCharantia could be useful in hyperlipidemic conditions. They are as effective as a standard lipid lowering agent- atorvastatin.