Search Results (361)

Helicobacter pylori, a spiral-shaped bacterium found in the stomach, is associated with various gastrointestinal and systemic health conditions. Effective suppression of H. pylori is therefore critical for managing gastrointestinal diseases. In a search for natural products with anti-H. pylori activity, the extract of Atractylodes macrocephala rhizoma showed significant inhibitory effects. Chromatographic purification of A. macrocephala extract yielded thirteen compounds, which were identified as ten sesquiterpenes and three polyacetylenes by spectroscopic analysis. The sesquiterpene compounds belong to the eudesmane or eudesmane lactone types and exhibited structure-dependent efficacy. The major eudesmane lactone sesquiterpene, atractylenolide I (1), showed strong inhibitory activity comparable to metronidazole, a positive control, and atractylenolide III (3) also showed good efficacy. However, structural modification such as hydroxylation, methylation, or acetylation of the sesquiterpenes led to reduced activity. In contrast, polyacetylene derivatives displayed only mild inhibitory effects. Further evaluation of the active compounds against three H. pylori strains such as 51, 43504, and 26695 showed that atractylenolide I (1) had potent inhibitory effects against all three strains, with MIC₅₀ values of ranging from 27.3 to 48.6 μM and MIC₉₀ values from 45.4 to 87.2 μM. Atractylenolide III (3) exhibited selective activity against strain 51 with MIC₅₀ value of 89.9 μM. Both compounds also exhibited anti-inflammatory activity with IC₉₀ values of 23.3 and 31.1 μM, respectively, although they showed little effect on urease. This is the first report on the anti-H. pylori efficacy of various constituents of A. macrocephala and comparative analysis of inhibitory effects against several strains, which will provide scientific evidence supporting its potential as therapeutic agent for H. pylori-related infection. Full article

Tanacetum parthenium (Asteraceae) has been traditionally used worldwide for medicinal purposes, and some of its therapeutic uses have been attributed to the pharmacological effects of its secondary metabolites. The root culture of this species might represent a sustainable source of several pharmacologically active compounds. The biomass of a root T. parthenium culture was extracted with methanol and fractionated using column chromatography. Three selected fractions (4TP, 5TP, and 8TP) were analyzed via spectrophotometric, chromatographic, and mass spectrometry techniques and in vitro pharmacological assays. The greatest values for total phenolic and phenolic acid contents and antibacterial activity against Escherichia coli were determined for 4TP. The highest values for total flavonoid and sesquiterpene lactone contents, antioxidant potential, and α-amylase inhibitory effect were determined for 8TP. The antibacterial effect against Staphylococcus aureus was not significantly different among the three fractions. The root culture of T. parthenium is a potential source of several metabolites, such as phenolic acids, fatty acids, coumarins, sesquiterpenoids, and triterpenoids, which are capable of exerting α-amylase inhibition and antioxidant, antibacterial, and cytotoxic effects. Among eight phenolic compounds detected and quantified in the fractions, chlorogenic acid was the most abundant. Full article

Cichorium intybus L. (common chicory) is a medicinal plant valued for health-promoting effects. Although analgesic properties are known for chicory sesquiterpenes, the effects of extracts need yet to be explored. This study aimed to evaluate for the first time the analgesic effect (against nociceptive pain) of the root extract from C. intybus var. foliosum. The target evaluation was preceded by toxicity tests in vivo and phytochemical standardization of root extracts prepared with different extraction methods—pectinase-assisted, pressure-assisted, and a combination of both—to choose the most effective one. The phytochemical profiling involved UHPLC-PDA-ESI-MS/MS and UHPLC-PDA analyses. The toxicity and the analgesic effects were tested in mice following the OECD 423 guideline and the hot-plate test, respectively. The highest recovery of bioactive compounds was achieved for the pressure-assisted extract: 642.5 mg sesquiterpene lactones, 187.1 mg phenolic acids, and 47.3 g inulin/100 g of dry matter. The extract showed no toxic effects at the oral dose of 2000 mg/kg body weight, including no histopathologic changes, in mice within two weeks (GHS Category 5/Uncategorized). The maximum analgesic effect (MAE) of the extract at 600 mg/kg was 6.75% for rearing and 13.7% for jumping, with the impact on the nocifensive reactions not differing significantly from those of paracetamol at 60 mg/kg. Despite the relatively low effects at 600 mg/kg, the verified safety and abundance of active compounds encourage further studies on the extract and its active fractions as potential approaches to complementary pain therapy, with special concern for their mechanisms of action. Full article

Chrysanthemum species represent an economically important group of flowering plants. Many species also present a medicinal interest, notably for the treatment of inflammatory pathologies. This is the case for Chrysanthemum boreale Makino, endemic to Japan and widespread in Eastern Asia. This perennial plant has long been used in folk medicine to treat inflammatory diseases and bacterial infections. An extensive review of the scientific literature pertaining to C. boreale has been performed to analyze the origin of the plant, its genetic traits, the traditional usages, and the properties of aqueous or organic plant extracts and essential oils derived from this species. Aqueous extracts and the associated flavonoids, such as acacetin and glycoside derivatives, display potent antioxidant activities. These aqueous extracts and floral waters are used mainly as cytoprotective agents. Organic extracts, in particular those made from methanol or ethanol, essentially display antioxidant and anti-inflammatory properties useful to protect organs from oxidative damage. They can be used for neuroprotection. Essential oils from C. boreale have been used as cytoprotective or antibacterial agents. The main bioactive natural products isolated from the plant include flavonoids such as acacetin and related glycosides (notably linarin), and diverse sesquiterpene lactones (SLs). Among monomeric SLs, cumambrins and borenolide are the main products of interest, with cumambrin A targeting covalently the transcription factor NF-κB to regulate proinflammatory gene expression to limit osteoclastic bone resorption. The dimeric SL handelin, which is characteristic of C. boreale, exhibits a prominent anti-inflammatory action, with a capacity to target key proteins like kinase TAK1 and chaperone Hsp70. A few other natural products isolated from the plant (tulipinolide, polyacetylenic derivatives) are discussed. Altogether, the review explores all medicinal usages of the plant and the associated phytochemical panorama, with the objective of promoting further botanical and chemical studies of this ancestral medicinal species. Full article

Objectives: Nanosized polymeric micelles (PMs) with an average size of about 80 nm and moderately positive ζ potential, based on an amphiphilic poly(4-methyl-piperazin-1-yl)-propenone)-b-polylactide (PMPP-PLA) block copolymer, were prepared. They were used as platforms for the delivery of bioactive sesquiterpene lactones from Inula helenium L. root extract. Methods: The PMs were characterized with good encapsulation efficiency as a maximum value of 72% was reached at a polymer-to-extract mass ratio of 10:1. The loaded micelles exhibited good colloidal stability. An in vitro release was performed showing a burst release profile. The biocompatibility of the resulting PMs was confirmed by assessing their cytotoxic effect on human keratinocytes in vitro by colorimetric assay and flow cytometry. Results: The systems demonstrated the capability to reduce the biomass of pre-formed Gram-positive and Gram-negative bacterial biofilms. Conclusions: The obtained data clearly determine a trend for a strong combined effect between the PMs and the root extract, distinguishing them with an excellent anti-biofilm potential and prospects for future applications in medical practice. Full article

The globe artichoke (Cynara cardunculus L. var. scolymus) is a Mediterranean crop valued for its edible capitula and bioactive compounds. Post-harvest residual leaves are among the main by-products of artichoke cultivation and remain largely underutilized. This study reports a comprehensive characterization of the residual leaves of Carciofo di Malegno, an Alpine artichoke landrace. Comparative analysis was conducted against leaves from two commercial cultivars and a commercial herbal tea product. HPLC analysis revealed that Carciofo di Malegno exhibited the lowest levels of secondary metabolites. Cynaropicrin content was 0.52 ± 0.03 mg/g, lower than in the commercial samples, while the phenolic compounds were below the quantification limit. Proximate analysis indicated a distinctive nutritional profile, with significantly higher ash (8.01 ± 0.04%) and crude fiber (35.75 ± 0.29%) contents compared to all reference samples. These findings highlight the potential of Carciofo di Malegno residual leaves as a sustainable source of nutrients for functional food and nutraceutical applications. Their low content of bitter sesquiterpene lactones may enhance palatability, supporting their valorisation within circular economy frameworks. Moreover, their use may contribute to the in situ conservation of this landrace, reinforcing the link between agrobiodiversity preservation and the sustainable exploitation of agricultural by-products. Full article

In light of the increasing demand for laurel, driven by renewed interest in natural products and traditional medicinal usage of this plant, our study aimed to investigate the in vitro antimicrobial activity of essential oils from leaves and fruits of laurel (EOL and EOF, respectively) collected in the National Park Skadar Lake, Montenegro, as it related to their chemical composition, assessing the possibility of their usage in cosmetics and pharmaceuticals. Also, fatty oil from the remaining laurel fruit after EOF isolation was investigated as a possible source of bioactive compounds. The most abundant components in EOL and EOF were 1,8-cineol (35.1% and 33.3%, respectively) and α-terpinyl acetate (10.4% and 7.0%, respectively). Linalool (7.6%) was found in EOL, while α- pinene (5.8%) and β-elemene (5.7%) were present in significant amounts in EOF. Antibacterial and antifungal properties of EOL and EOF showed strong antibacterial activity against Staphylococcus aureus, Enterococcus faecalis, and Bacillus subtilis, and potent antifungal effects against Candida albicans, opening the door for their application as antimicrobial agents. Chemical analysis of fatty oil unexpectedly revealed prominent content of sesquiterpene lactone dehydrocostunolide and phenylpropanoid derivative (E)-2-hexyl-cinnamaldehyde (21% and 5%, respectively), suggesting further investigations of this waste material as the source of valuable compounds with proven health benefits. Full article

Achillea nobilis and its subspecies (A. nobilis subsp. neilreichii and A. nobilis subsp. sipylea) have been traditionally used in various ethnomedical systems across Eurasia. However, comprehensive studies on their phytochemical composition and pharmacological properties are still insufficient. This review aims to provide a critical synthesis of current knowledge regarding the botanical characteristics, geographic distribution, traditional applications, chemical constituents, and pharmacological effects of A. nobilis A structured search was conducted using eight scientific platforms, including Scopus, PubMed, Web of Science, Google Scholar, Science.gov, ScienceDirect, JSTOR, and BASE. Keywords related to phytochemistry, pharmacology, and ethnomedicine were applied, and a total of 28,000 records were initially retrieved. After a multi-stage screening process based on inclusion and exclusion criteria, 167 peer-reviewed publications from 1952 to 2023 were selected for detailed evaluation. Findings reveal a diverse range of bioactive compounds, such as flavonoids, monoterpenes, sesquiterpenes, and sesquiterpene lactones, which demonstrate antioxidant, antimicrobial, anti-inflammatory, antinociceptive, antispasmodic, and anticonvulsant activities. Most studies have focused on aerial parts and water-based extracts, while the root chemistry and organ-specific metabolite profiles remain largely unexplored. This review highlights the therapeutic potential of A. nobilis and underscores the need for future studies using multi-omics and advanced analytical techniques to support its development in pharmaceutical and nutraceutical applications. Full article

Colon cancer is the second leading cause of cancer-related deaths in the world. This is commonly observed among older adults, and the occurrence of colon cancer is mainly influenced by unhealthy lifestyle factors. Edible medicinal mushrooms have been demonstrated to have anti-colon cancer effects both individually and in combination with conventional therapies, including synergistically enhancing the efficacy of chemotherapy medications such as 5-fluorouracil in preclinical models. Medicinal mushrooms such as Lentinus edodes, Phellinus linteus, Ganoderma lucidum, Inonotus obliquus, Pleurotus ostreatus, Hericium erinaceus, Pleurotus eryngii, Gloeostereum incarnatum, and Termitomyces heimii are emerging as promising candidates, not only because conventional treatments for colon cancer face significant limitations, including side effects, psychological impacts on patients, high cost, limited specificity toward cancer and healthy cells, and the development of drug resistance, but also due to the diverse array of bioactive compounds present within them. Therefore, there is a strong demand for innovative, affordable, and minimally invasive treatments such as medicinal mushrooms. Their bioactive compounds, including terpenoids, sterols, phenols, polysaccharides, acids, sesquiterpenes, alkaloids, lactones, metal-chelating agents, nucleotide analogs, glycoproteins, β-glucan, cerebrosides, steroids, terpenes, quinolones, anthraquinones, benzoic acid derivatives, linoleic acid, ascorbic acid, glycosides, organic acids, flavonoids, grifolin, tocopherols, proteins, indoles, lectin, and laccases, exert anti-colon cancer activities through various mechanisms, including anti-proliferative effects, cell cycle arrest, anti-inflammatory effects, antioxidant effects, induction of apoptosis, cytotoxic effects, and antimigratory effects. Further research is needed to elucidate the molecular mechanisms and confirm the safety and efficacy of medicinal mushrooms as a holistic anti-colon cancer treatment. Full article

Neurodegenerative diseases are characterised by the progressive loss of neurons, leading to a decline in specific brain functions. Alzheimer’s disease (AD) and Parkinson’s disease (PD) are the most prevalent, affecting approximately 60 million people worldwide. The pathogenesis of these diseases is complex, combining inflammatory, oxidative, and excitotoxic processes that result in neuronal dysfunction and death. Despite recent advances, there is currently no cure for AD and PD. Available therapies demonstrate limited efficacy, highlighting the continuing need for novel therapeutic approaches. Ergolide, a naturally occurring sesquiterpene lactone from the Inula brittanica plant, has shown immunoregulatory properties in systemic immune cells and potential applications in certain cancers. This study examines whether the therapeutic effects of ergolide extend to the brain. We explored its mechanisms of action in vitro, and its capacity to restore behavioural integrity in zebrafish models of inflammation and neurotoxicity in vivo. We report the ability of ergolide to attenuate inflammatory cytokine and nitric oxide (NO) production from microglia in response to toll-like receptor activation. We further propose a role for the NFκB and cysteinyl leukotriene (CysLT) pathways in ergolide-mediated regulation of microglial activation. Ergolide did not protect against oxidative-induced neuronal death in vitro or mitigate seizure activity in zebrafish. Instead, we revealed a pro-oxidant and cytotoxic effect on neuroblastoma cells. Importantly, ergolide improved survival and alleviated the dysfunction in sensorimotor behaviour in a zebrafish model of inflammation. Our findings reveal a neuroprotective effect of ergolide, likely stemming from its immunoregulatory capacity. We also support further investigation of the CysLT pathway as a therapeutic target for neuroinflammatory-related disease. Full article

This study compares the antioxidant properties and phytochemical profiles of three pairs of widely used medicinal plant species to their counterparts from Provence, France: Arnica montana with Pentanema montanum (formerly known as Inula montana), Helichrysum italicum with Helichrysum stoechas, and Satureja hortensis with Satureja montana. Phytochemical composition has been investigated using UHPLC-HRMS/MS and molecular networking, revealing chemical profiles dominated by phenylpropanoids and flavonoids, with lignans, sesquiterpene lactones, or polyketides aside. Well-plate DPPH/ABTS assays were used to evaluate the antioxidant activity of extracts, and post-column assays were used to identify antioxidant compounds. The three Provence species demonstrated comparable or superior antioxidant activities to their counterparts, primarily attributed to phenolic compounds such as mono- and di-caffeoylquinic acids, quercetagetin-7-O-glucoside, and myricetin acetylhexoside. These findings show the potential of Provence species to be substituted for some overharvested medicinal plants. This research supports biodiversity conservation while promoting the integration of these local species into pharmaceutical, nutraceutical, cosmetic, and food industries. Full article

Background: Multidrug resistance (MDR) in triple-negative breast cancer (TNBC) leads to treatment failure and tumor recurrence. Dysregulation of the MYC oncogene is associated with the pathogenesis of TNBC and the development of chemoresistance via overexpression of ATP-binding cassette (ABC) transporters. Therefore, in the present study, we aimed to identify molecules from a natural product origin that prevent the development of MDR in TNBC by targeting the MYC signaling. Methods: The cell viability of TNBC was evaluated using sulforhodamine assay. Protein levels were detected by western blots or enzyme-linked immunosorbent assays. Intracellular calcein and hoechst33342 accumulation assay aimed to evaluate the inhibitory ability of phytocompounds on drug-efflux functions of ABCB1 and ABCG2 transporters. The Cancer Genome Atlas (TCGA) database was used to explore clinical genomic data. Furthermore, the zebrafish xenotransplantation model bearing Dil-labeled TNBC cells was applied to testify the in vivo effects of phyto-sesquiterpene lactones. Results: The results of the present study demonstrated that the phyto-sesquiterpene lactones exhibited an MDR prevention effect by repressing efflux activities of ABCB1 and ABCG2 transporters. Mechanistic studies showed that phyto-sesquiterpene lactones inducted TNBC cell apoptosis and cell cycle G2/M arrested by blocking the STAT3/MYC pathway. Clinical genomic data demonstrated that the percentages of MYC amplification and mRNA were upregulated approximately two-fold higher in the TNBC patients than the non-TNBC breast cancer patients. The survival of patients with an alteration in MYC was significantly lower in TNBC as compared to other subtypes. Moreover, the results of the zebrafish xenograft model confirmed that phyto-sesquiterpene lactones exerted stronger inhibitory effects on TNBC tumor growth in vivo. Conclusions: In conclusion, these three phyto-sesquiterpene lactones were promising candidates for TNBC treatment and shed light on the prevention of developing MDR TNBC. Full article

Grossheimin, a guaiane-type sesquiterpene lactone, displayed a diverse range of biological activities, including anticancer, anti-inflammatory and antimicrobial effects. Various amino analogues of grossheimin were prepared through a Michael addition at its highly active α-methylene-γ-lactone motif. On the other hand, grossheimin was reduced to diol, which was then subjected to nucleophilic addition or acetylation to introduce heteroatoms associated with oxygen, sulfur or nitrogen functionalities. All of the synthesised Michael and acetylated adducts were evaluated for their in vitro cytotoxic action on human colon adenocarcinoma lines, including Colo205 and Colo320. The bioassay results indicated that the acetylated adducts displayed a potent cytotoxic effect compared to grossheimin, the parent molecule. A docking study was also performed to exploit the observed results. Full article

Considering the resistance of weeds to different herbicides with different mechanisms of action, the search for new, more selective compounds with low toxicity to other species in nature has been very important for the development of agriculture. Because of that, considering the biological activity of allelochemicals and natural epoxides, four new epoxy compounds derived from dehydrocostus lactone were synthetized and evaluated for their potential herbicide activity against three species of seeds, Allium cepa (onion), Lepidium sativum (garden cress), and Lactuca sativa (lettuce). In assays with A. cepa, compound 4 inhibited radicle length by 80% at 100 μM. Notably, for L. sativum, compound 4 showed significant inhibition, reducing stalk and radicle lengths by 80% at 100 μM, surpassing the performance of the commercial herbicide Logran. However, diol 5 notably inhibited radicle growth by 28% at 100 μM, making the most significant observed effect. One of the noteworthy lactones studied is epoxide 4. This highlights the importance of the epoxide functional group in affecting both radicle and shoot lengths of seeds. Therefore, the synthesis of these compounds has proven advantageous and holds great potential for the development of new herbicides. Full article