Ferula is a genus of flowering plants known for its edible and medicinal properties. The gum of the Ferula kokanica was selected for this study based on its traditional uses. From the gum of F. kokanica, an undescribed sesquiterpene coumarin was isolated, named kokanin A, along with 22 known compounds. Structure elucidation of the isolated compounds was carried out by one- and two-dimensional nuclear magnetic resonance and high-resolution-electrospray ionization-mass spectrometry data analysis. Using NOE correlation, the relative configurations of the isolated compounds were established. The absolute configurations of isolates were established by electronic circular dichroism calculation. Cytotoxicity and anti-vitiligo activity of the isolated compounds were tested. Gummosin demonstrated strong cytotoxicity against the HT-29 cell line with IC50 values of 6.96 ± 0.38 µM. Colladonin, farnesiferol A, and feshurin provided greater relative melanin content than that of the positive control at 50 µM. The elemental composition of the gum of F. kokanica using the inductively coupled plasma mass spectrometry method allowed the determination of trace levels of As, Cd, Cu, Hg, Pb, Na, Mg, K, and Ca. The toxic elements were determined in the sample, and their content was found to be lower than the maximum acceptable concentration established by the World Health Organization. This study showed that some isolated compounds demonstrated significant anti-vitiligo activity and showed promise for future drug discovery. To our knowledge, this is the first report on the chemical composition and the bioactivities of the gum of F. kokanica.
The fruits of rose hips (Rosa canina L.) have been of great interest in the food and pharmaceutical industries because of their high content of valuable components such as vitamins, carotenes and fatty acids. Rose hip fruits are very popular in central Asian countries, especially in Tajikistan. In this country, the fruits of rose hips are mainly collected from the wild rosehip species. This present work demonstrates the fatty acid compositions of the oil of rose hip fruits obtained with supercritical fluid extraction, maceration, and ultrasound-assisted methods. The fatty acids in extracts of the rose hip fruits were converted to their methyl esters using a two-step methylation method and analyzed via gas chromatography mass spectrometry. Linoleic and oleic acids were identified as the major fatty acids in the rose hip fruit extracts. Overall, the fatty acid profile of the investigated rose hip oil was in agreement with previously published data. To our best knowledge, there is no information about the Tajikistani origin of rose hip oil. The obtained oil from the rose hips of Tajikistani origin is of potential interest for its application in the food, cosmetic and pharmaceutical industries. Purification of the rose hip extract was achieved via adsorption and desorption of the extract on the surface of AB-8 and HPD450 macroporous resins. The retreatment of rose hip extract resulted in improvement regarding quality, which was experimentally confirmed by iodometric titration and assays for the determination of the total phenol and flavonoid contents, and antioxidant activity of the rose hip extracts before and after purification. The macroporous resin purification method of the rose hip extract is simple, cheap, and efficient for the preparation of high-quality bioadditives (BAD) from natural rose hip extract containing the biologically active fraction.
Laetrile, known as vitamin B17, is often used interchangeably with amygdalin. Laetrile is a semi-synthesis product of amygdalin, whereas amygdalin is a naturally occurring substance in many plants. Both compounds have a nitrile functional group that, when activated by the intestinal enzyme β-glucosidases, releases hydrogen cyanide. The two compounds have been considered for a long time as alternative therapy for cancer treatment however, findings available in the literature are discordant on the real efficacy of laetrile/amygdalin for the treatment of cancer, often highlighting a negative benefit-risk ratio. In this regard, the study aimed to comprehensively analyze the scientific data on laetrile/amygdalin, with a special emphasis on their pharmacokinetics, underlying pharmacological properties, mode of action as a potent antitumor agent, and effect on human health. The results showed that there is no clear evidence on the efficacy of cancer therapy following laetrile/amygdalin administration, especially at the clinical trial level. However, the in vitro studies of the biological activity of these compounds showed positive effects related to their antifibrotic, anti-inflammatory, antiasthmatic, and immunoregulatory processes. Laetrile's mechanism of action closely resembles amygdalin, affecting cancer signaling pathways. However, due to its cyanide toxicity, it was banned by the food and drug administration (FDA) due to safety concerns. Despite not receiving permission from the FDA, laetrile emerged as an alternative therapy in the 1970s. Nonetheless, continuing research is investigating safer methods of activating Laetrile for targeted cancer treatment. This opens interesting prospects in using these compounds in alternative medical therapies, for which, however, further research is needed.
There was an error in the original publication [...]
Natural compounds with multitargeted actions are gaining prominence in oncology for their potential to complement and transcend the limitations of conventional therapies. Among them, baicalein and baicalin, two flavonoids primarily isolated from Scutellaria baicalensis, have attracted attention for their broad-spectrum anticancer properties. This review synthesizes current evidence from cellular systems, animal models, and early-phase clinical studies, exploring their pharmacological potential and translational relevance. Both molecules interfere with key hallmarks of cancer, including proliferation, survival, angiogenesis, metastasis, and immune evasion. Mechanistically, they modulate interconnected signaling cascades governing apoptosis, inflammation, and cell cycle control, and they enhance tumor sensitivity to chemotherapy and radiotherapy. In-vivo models consistently demonstrate tumor growth inhibition, while clinical data suggest a favorable safety profile, even at relatively high oral doses. However, their clinical translation remains hampered by limited solubility, poor oral bioavailability, and rapid metabolism, factors that continue to constrain their therapeutic window. Efforts to overcome these barriers through structural modification, encapsulation strategies, and advanced delivery systems are underway, yet few have advanced beyond preclinical validation. Despite these pharmacokinetic limitations, baicalein and baicalin remain compelling candidates for integrative oncological approaches. Their pleiotropic mechanisms, combined with low toxicity and synergistic behavior with standard therapies, position them as prototypes for a new generation of phytochemical-based anticancer agents. Continued work is needed to resolve formulation challenges and define precise molecular targets, but their trajectory reflects the growing scientific and clinical momentum around rationally designed natural compound therapeutics.
Pinus mugo Turra is a coniferous species of shrub or small tree typical of central and south-eastern Europe. It is commonly called mugo pine, mountain pine, or dwarf mountain pine referring to its habit and small size. Indeed, this plant lives at higher altitude above 1400 m above the see level where it deals with harsh conditions typical of high mountain. From an ethnotraditional point of view, P. mugo is mainly used for respiratory disorders and wound healing. In particular, its essential oils have been shown to possess interesting antimicrobial and antioxidant activities, which can substantiate its potential therapeutic effect in pulmonary and urinary tract diseases, as well as antinflammatory and antitumor effects. This review also offers a summary on the chemical constituents of P. mugo that contribute to its therapeutic potential.
HS-1793 is a novel derivative of resveratrol, a compound known for its numerous beneficial effects, including anticancer activity, anti-inflammatory response, antimicrobial, antiaging, anti-cardiovascular disease activity, neuroprotective activity, etc. Despite its wide and interesting properties, resveratrol suffers from a crucial flaw because it is low bioavailable. For this reason, many other derivatives were explored and among them, HS-1793 has caught the attention of researchers. HS-1793 is a synthetic derivative of resveratrol discovered in 2007 that has been shown to have anti-cancer and anti-inflammatory properties. In addition, the compound showed a positive profile in metabolic processes, with adequate pharmacokinetics and pharmacodynamics. This review highlights current research on HS-1793, evaluating in vitro and in vivo works and lays the foundation for novel explorative trials in human diseases.
Pinus mugo Turra is a coniferous species of shrub or small tree typical of central and south-eastern Europe. It is commonly called mugo pine, mountain pine, or dwarf mountain pine referring to its habit and small size. Indeed, this plant lives at higher altitude above 1400 m above the see level where it deals with harsh conditions typical of high mountain. From an ethnotraditional point of view, P. mugo is mainly used for respiratory disorders and wound healing. In particular, its essential oils have been shown to possess interesting antimicrobial and antioxidant activities, which can substantiate its potential therapeutic effect in pulmonary and urinary tract diseases, as well as antinflammatory and antitumor effects. This review also offers a summary on the chemical constituents of P. mugo that contribute to its therapeutic potential. Keywords bioactivity , dwarf mountain , mugo pine , phytotherapy , Pinaceae
Objective: To study the mechanism of Artemisia in the treatment of respiratory tract infection (RTI) by network pharmacology and molecular docking. Methods: The active constituents and targets of Artemisia were screened by the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP). Gene Cards database to obtain disease targets associated with RTI. The key targets of intersection were used to construct the protein–protein interaction (PPI) network, and the hub gene was obtained through topological analysis to construct the pharmacology regulation network of traditional Chinese medicine. The key targets were analyzed by R language enrichment, and the regulatory network diagram of the key target function/pathway was constructed. Molecular docking verifies the binding of the drug to the target predicted by network pharmacology. Results: 144 active components of Artemisia regulated 133 target proteins related to RTI, the core components were β-sitosterol, quercetin, isorhamnetin, artemisinin, etc. Gene ontology enrichment analysis showed that Artemisia regulates receptor ligand activity, cytokine activity, and other molecular functions by acting on membrane region, membrane raft and other cellular structures in the treatment of RTI, thus affecting biological processes such as the response to drugs and bacteria-derived molecules. Kyoto Encyclopedia of Genes and Genomes enrichment analysis indicated that phosphatidylinositol 3-kinase (PI3K)-protein kinase B (Akt), tumor necrosis factor, interleukin-17 (IL-17) signaling pathway was the main pathway for RTI treatment. The molecular docking method confirmed the high affinity between the active ingredient and the RTI target. Conclusions: Artemisia species, a multitarget medication, has been shown to be a viable therapy option for RTI by network pharmacology techniques based on data mining and molecular docking approaches. Keywords , , respiratory tract infections , network pharmacology , severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) , sesquiterpene lactones
Objective: To study the mechanism of Artemisia in the treatment of respiratory tract infection (RTI) by network pharmacology and molecular docking. Methods: The active constituents and targets of Artemisia were screened by the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP). Gene Cards database to obtain disease targets associated with RTI. The key targets of intersection were used to construct the protein–protein interaction (PPI) network, and the hub gene was obtained through topological analysis to construct the pharmacology regulation network of traditional Chinese medicine. The key targets were analyzed by R language enrichment, and the regulatory network diagram of the key target function/pathway was constructed. Molecular docking verifies the binding of the drug to the target predicted by network pharmacology. Results: 144 active components of Artemisia regulated 133 target proteins related to RTI, the core components were β-sitosterol, quercetin, isorhamnetin, artemisinin, etc. Gene ontology enrichment analysis showed that Artemisia regulates receptor ligand activity, cytokine activity, and other molecular functions by acting on membrane region, membrane raft and other cellular structures in the treatment of RTI, thus affecting biological processes such as the response to drugs and bacteria-derived molecules. Kyoto Encyclopedia of Genes and Genomes enrichment analysis indicated that phosphatidylinositol 3-kinase (PI3K)-protein kinase B (Akt), tumor necrosis factor, interleukin-17 (IL-17) signaling pathway was the main pathway for RTI treatment. The molecular docking method confirmed the high affinity between the active ingredient and the RTI target. Conclusions: Artemisia species, a multitarget medication, has been shown to be a viable therapy option for RTI by network pharmacology techniques based on data mining and molecular docking approaches.
A crude methanol extract of the roots of Allochrusa gypsophiloides (syn. Acanthophyllum gypsophiloides) (collected from the Tashkent region of Uzbekistan) was chemically characterised by UHPLC-ESI-QTOF-MS/MS analysis. The results indicate the presence of six major bisdesmosidic saponins derived from gypsogenin, gypsogenic and quillaic acids, including five compounds reported for the first time for this species. The chloroform, methanol and water extracts of A. gypsophiloides showed weak antioxidant and anthelmintic activities. Among the tested extracts, the water extract exhibited the highest level of cytotoxicity in CCRF-CEM and CEM/ADR5000 cell lines with IC50 values of 23.6 and 31.9 µg/mL, respectively.
Mitochondria, pivotal organelles crucial for energy generation, apoptosis regulation, and cellular metabolism, have spurred remarkable advancements in targeted material development. This review surveys recent breakthroughs in targeted mitochondrial nanomaterials, illuminating their potential in drug delivery, disease management, and biomedical imaging. This review approaches from various application perspectives, introducing the specific applications of mitochondria-targeted materials in cancer treatment, probes and imaging, and diseases treated with mitochondria as a therapeutic target. Addressing extant challenges and elucidating potential therapeutic mechanisms, it also outlines future development trajectories and obstacles. By comprehensively exploring the diverse applications of targeted mitochondrial nanomaterials, this review aims to catalyze innovative treatment modalities and diagnostic approaches in medical research. Statement of Significance This review presents the latest advancements in mitochondria-targeted nanomaterials for biomedical applications, covering diverse fields such as cancer therapy, bioprobes, imaging, and the treatment of various systemic diseases. The novelty and significance of this work lie in its systematic analysis of the intricate relationship between mitochondria and different diseases, as well as the ingenious design strategies employed to harness the therapeutic potential of nanomaterials. By providing crucial insights into the development of mitochondria-targeted nanomaterials and their applications, this review offers a valuable resource for researchers working on innovative treatment modalities and diagnostic approaches. The scientific impact and interest to the readership lie in the identification of promising avenues for future research and the potential for clinical translation of these cutting-edge technologies.
The glycoprotein (GP) IIb/IIIa receptor is found integrin present in platelet aggregations. GP IIb/IIIa antagonists interfere with platelet cross-linking and platelet-derived thrombus formation through the competition with fibrinogen and von Willebrand factor. Currently, three parenteral GP IIb/IIIa competitors (tirofiban, eptifibatide, and abciximab) are approved for clinical use in patients affected by percutaneous coronary interventions (PCI) in the location of acute coronary syndrome (ACS). GP IIb/IIIa antagonists have their mechanism of action in platelet aggregation prevention, distal thromboembolism, and thrombus formation, whereas the initial platelet binding to damage vascular areas is preserved. This work is aimed to provide a comprehensive review of the significance of GP IIb/IIIa inhibitors as a sort of antiplatelet agent. Their mechanism of action is based on factors that affect their efficacy. On the other hand, drugs that inhibit GP IIb/IIIa already approved by the FDA were reviewed in detail. Results from major clinical trials and regulatory practices and guidelines to deal with GP IIb/IIIa inhibitors were deeply investigated. The cardiovascular pathology and neuro-interventional surgical application of GP IIb/IIIa inhibitors as a class of antiplatelet agents were developed in detail. The therapeutic risk/benefit balance of currently available GP IIb/IIa receptor antagonists is not yet well elucidated in patients with ACS who are not clinically evaluated regularly for early cardiovascular revascularization. On the other hand, in patients who have benefited from PCI, the antiplatelet therapy intensification by the addition of a GP IIb/IIIa receptor antagonist (intravenously) may be an appropriate therapeutic strategy in reducing the occurrence of risks of thrombotic complications related to the intervention. Development of GP IIb/IIIa inhibitors with oral administration has the potential to include short-term antiplatelet benefits compared with intravenous GP IIb/IIIa inhibitors for long-term secondary preventive therapy in cardiovascular disease. But studies showed that long-term oral administration of GP IIb/IIIa receptor inhibitors has been ineffective in preventing ischemic events. Paradoxically, they have been linked to a high risk of side effects by producing prothrombotic and pro-inflammatory events.
Cocoa is rich in polyphenols, mainly flavonoids, which correlate with several health benefits mediated by their antioxidant, anti-inflammatory and immunomodulatory properties. Cocoa and chocolate consumption have been reported to impact the regulation of the immune system, both in preclinical studies and in human trials. The mechanisms for immunomodulation can involve different effects of cocoa polyphenols on the immune system, acting as anti-inflammatory, antioxidant and anti-allergic agents, as well as the direct influence of cocoa on innate and acquired immunity, with cytokines production and activation of both lymphocyte-dependent and -independent pathways. Cocoa intake has been also correlated to changes in gut microbiota ecology and composition, also affecting the intestinal immune system. This review summarises the updates of the last two decades on cocoa as immunomodulatory agent and explores the health-related benefits of cocoa and chocolate intake.
Bromelain is a key enzyme found in pineapple (Ananas comosus (L.) Merr.); a proteolytic substance with multiple beneficial effects for human health such as anti-inflammatory, immunomodulatory, antioxidant and anticarcinogenic, traditionally used in many countries for its potential therapeutic value. The aim of this updated and comprehensive review focuses on the potential anticancer benefits of bromelain, analyzing the cytotoxic, apoptotic, necrotic, autophagic, immunomodulating, and anti-inflammatory effects in cancer cells and animal models. Detailed information about Bromelain and its anticancer effects at the cellular, molecular and signaling levels were collected from online databases such as PubMed/MedLine, TRIP database, GeenMedical, Scopus, Web of Science and Google Scholar. The results of the analyzed studies showed that Bromelain possesses corroborated pharmacological activities, such as anticancer, anti-edema, anti-inflammatory, anti-microbial, anti-coagulant, anti-osteoarthritis, anti-trauma pain, anti-diarrhea, wound repair. Nonetheless, bromelain clinical studies are scarce and still more research is needed to validate the scientific value of this enzyme in human cancer diseases.
Artemisinin (ART) is a bioactive compound isolated from the plant Artemisia annua and has been traditionally used to treat conditions such as malaria, cancer, viral infections, bacterial infections, and some cardiovascular diseases, especially in Asia, North America, Europe and other parts of the world. This comprehensive review aims to update the biomedical potential of ART and its derivatives for treating human diseases highlighting its pharmacokinetic and pharmacological properties based on the results of experimental pharmacological studies in vitro and in vivo. Cellular and molecular mechanisms of action, tested doses and toxic effects of artemisinin were also described. The analysis of data based on an up-to-date literature search showed that ART and its derivatives display anticancer effects along with a wide range of pharmacological activities such as antibacterial, antiviral, antimalarial, antioxidant and cardioprotective effects. These compounds have great potential for discovering new drugs used as adjunctive therapies in cancer and various other diseases. Detailed translational and exper-imental studies are however needed to fully understand the pharmacological effects of these compounds.
Lycorine, an isoquinoline alkaloid can exhibit significant anti-cancer effects. The present study was conducted to illustrate the underlying mechanisms of action of lycorine on breast carcinoma under in vitro and in vivo settings Tandem Mass Tag assay and Kyoto Encyclopedia of Genes and Genomes analysis revealed that 20 signaling pathways were closely related to tumorigenesis, especially Wnt signaling pathway and tight junctions. The results demonstrated that lycorine evidently inhibited the proliferation of MDA-MB-231 and MCF-7 cells with IC50 values of 1.84 ± 0.21 μM and 7.76 ± 1.16 μM, respectively. It also blocked cell cycle in G2/M phase, caused a decrease in mitochondrial membrane potential, and induced apoptosis pathways through regulating caspase-3, caspase-8, caspase-9, and PARP expression. Moreover, lycorine effectively repressed the β-catenin signaling and reversed epithelial-mesenchymal transition (EMT) process. Furthermore, 4T1/Luc homograft tumor model was used to further demonstrate that lycorine significantly inhibited the growth and metastasis of breast tumor. These findings highlight the significance of lycorine as potential anti-neoplastic agent to combat breast cancer.
AbstractAttention deficit hyperactivity disorder (ADHD) is among the most common neurodevelopmental disorders characterized by motor hyperactivity, attention deficit, distraction, impulsive behavior, and relationship difficulties. It affects children, and thus over the years, there has been growing attention on the use of natural product formulations and their naturally‐occurring bioactive for overcoming the problem of ADHD. Concerning this issue, this review aims to discuss the ADHD treatment potential of natural products/formulations in vitro, in vivo as well as in clinical trials. To gather the most relevant data regarding bioactive compounds with potential therapeutic effects in the management of ADHD, the following databases were searched: PubMed/MedLine, ScienceDirect, and Google Scholar for articles in English. Various medicinal plants and their isolated biomolecules have been evaluated in vitro, in vivo, and in clinical trials for their ability to treat ADHD. Most of the analyzed research results showed an improvement of ADHD signs and symptoms in in vivo models, but the molecular mechanisms of action of the bioactive compounds are unclear and incompletely elucidated. Further studies are needed to determine the bioactive compound responsible for health‐promoting effects in ADHD. In addition, clinical studies should be performed over longer periods with more participants.