Search Results (63)

Acmella radicans, commonly known as the “toothache plant,” is traditionally attributed with medicinal properties, although few studies have validated its biological effects. In the present study, a chemical analysis of the wild plant was performed using gas chromatography–mass spectrometry (GC-MS). In addition, the antioxidant, anti-inflammatory, and antibacterial potential of ethanolic extracts from the roots (RE) and aerial parts (AE), as well as their respective fractions, was evaluated. The dichloromethane fractions of the aerial parts (DFAE) and root extracts (DFRE) at a concentration of 25 μg/mL demonstrated the highest inhibition of nitric oxide (NO) production, reducing levels to 22.2 ± 1.9 and 22.2 ± 2.9 μM, respectively. Moreover, these fractions exhibited a notable inhibition of TNF-α production, lowering its concentration to 22.6 ± 3.3 pg/mL (DFAE) and 24.8 ± 5.3 pg/mL (DFRE) at 25 µg/mL. GC-MS chemical profiling revealed the presence of alkamides such as N-isobutyl-2E,6Z,8E-decatrienamide, N-(2-methylbutyl)-2E,6Z,8E-decatrienamide, and N-(2-phenylethyl)-2E,4Z-octadienamide in both root and aerial part extracts. The dichloromethane fractions showed a higher abundance of alkamides compared to the hexane fractions, suggesting that these compounds may be at least partially responsible for the observed anti-inflammatory activity. Additionally, AE showed moderate activity against S. typhimurium and low activity against other bacteria, while RE was especially effective against a resistant strain of S. aureus, indicating an MIC of 31.25 μg/mL, likely due to its high content of alkamides, particularly spilanthol. Several fractions also inhibited bacteria such as P. aeruginosa, S. aureus, and E. coli, possibly because of the presence of alkamides and compounds like β-amyrin. Full article

Plant-derived pharmaceuticals represent a highly compelling area of research and continue to attract significant interest from countries, regions, scientific communities, and pharmaceutical companies worldwide. Among these, α- and β-amyrins have been identified as high-value triterpenoid compounds with a broad spectrum of potential therapeutic properties, including anti-inflammatory, antidiabetic, antiatherosclerotic, analgesic, antigout, neuroprotective, anti-Parkinsonian, anticancer, antibacterial, and anti-HIV activities. Relevant information and data were obtained through comprehensive searches of major scientific databases, including Web of Science, Elsevier, and the National Library of Medicine. This study highlighted the pharmaceutical potential of α- and β-amyrins, supported by specific evidence from in vivo, in vitro, and clinical trials. Various extraction methods for α- and β-amyrins are discussed, followed by recommendations for future directions in the development of these compounds as pharmaceutical agents and functional food ingredients. This review highlights the therapeutic of α- and β-amyrin compounds in the prevention and treatment of various serious diseases worldwide, potentially opening new opportunities and directions for the pharmaceutical industry. Full article

Viticis Fructus (VF), a fruit known for its unique flavor profile and various health benefits, demonstrates substantial quality variations depending on its area of production. Traditional methods of production area verification based on internal compound analysis are hampered by a number of technical limitations. This investigation systematically characterized the cuticular wax composition of VF sample from a diverse variety of production areas. Quantitative analyses were conducted to evaluate the spatial distribution patterns of the wax constituents. Significant regional variations were observed: Anhui sample exhibited the highest total wax content (21.39 μg/cm²), with n-alkanes dominating at 76.67%. High-latitude regions showed elevated triterpenoid acid levels, with maslinic acid (0.53 μg/cm²) and ursolic acid (0.34 μg/cm²) concentrations exceeding those of their low-latitude counterparts by four- and three-fold, respectively. Altitudinal influence manifested in long-chain alcohol accumulation, as triacontanol reached 0.87 μg/cm² in high-altitude sample. Five key biomarkers demonstrated direct quality correlations: eicosanoic acid, n-triacontane, dotriacontanol, β-amyrin, and α-amyrin. This study established three novel origin identification protocols: single-component quantification, multi-component wax profiling, and wax ratio analysis. This work not only reveals the latitudinal dependence of VF wax composition, but also provides a scientific framework for geographical authentication. Our findings advance wax-based quality evaluation methodologies for fruit products, offering practical solutions for production area verification challenges in food raw materials. Full article

Fire is a natural disturbance in the Brazilian Cerrado that modulates the vegetation structure. Protium heptaphyllum, a woody species of the family Burseraceae, is common in this biome. The resin produced in secretory canals immersed in the phloem of the stem and leaves of this species plays important ecological and industrial roles. The aim of this study was to investigate the influence of fire on the development of resin canals in the leaves and stem of P. heptaphyllum and on the chemical profile of substances produced in the leaves. Young plants were subjected to controlled fire experiments. Leaf and stem portions were analyzed using light microscopy; the chemical compounds in the leaves were identified through gas chromatography–mass spectrometry. The percentage area occupied by secretory canals in the leaf midrib was higher in fire-treated plants than in control plants. Similarly, the density of secretory canals and their lumen area were higher in young stems (primary growth) of fire-treated plants. By contrast, although the canal density in the secondary phloem was lower in older stem portions (secondary growth) in fire-treated plants, their lumens were larger, resulting in similar data regarding the total lumen area of the secretory canals in fire-treated and control plants. The main chemical compounds identified in the leaves were vitamin E, sitosterol, α-amyrin, squalene, and β-amyrin. Three compounds showed significant increases in fire-treated plants, with vitamin E being the only one reduced by fire. Our findings reveal the plasticity of the secretory system and of the biochemical properties of the leaves of P. heptaphyllum in response to fire. These results are important when considering the current increase in fires caused by climate change and human activity in different ecosystems around the world. Full article

Erica spiculifolia Salisb. (formerly Bruckenthalia spiculifolia Benth.) (Balkan heath) is renowned for its traditional usage as a diuretic, anti-inflammatory and antioxidant agent. For the first time, acylquinic acids, flavonoids and numerous proanthocyanidin oligomers were annotated/dereplicated by liquid chromatography–high-resolution mass spectrometry in methanol–aqueous extracts from E. spiculifolia aerial parts harvested at the early and full flowering stage. Chlorogenic acid and proanthocyanidin tetra- and trimer A, B-type together with quercitrin and (+) catechin were the predominant compounds in the semi-quantitative analysis. Neutral triterpenoids, triterpenoid acids and phytosterols were determined in apolar extracts by gas chromatography–mass spectrometry. Triterpenoid acids accounted for 80% of the total triterpenoid content, dominated by ursolic and oleanolic acid, reaching up to 32.2 and 6.1 mg/g dw, respectively. Ursa/olean-2,12-dien-28-oic acids and 3-keto-derivatives together with α-amyrin acetate as a chemotaxonomic marker, α-amyrenone, α- and β-amyrin were evaluated. Total phenolic and flavonoid contents were 83.85 ± 0.89 mg gallic acid equivalents/g and 78.91 ± 0.41 mg rutin equivalents/g, respectively. The extract actively scavenged DPPH and ABTS radicals (540.01 and 639.11 mg Trolox equivalents (TE)/g), possessed high potential to reduce copper and iron ions (660.32 and 869.22 mg TE/g, respectively), and demonstrated high metal chelating capacity (15.57 Ethylenediaminetetraacetic acid equivalents/g). It exhibited prominent anti-lipase (18.32 mg orlistat equivalents/g) and anti-tyrosinase (71.90 mg kojic acid equivalents/g) activity. The extract inhibited α-glucoside (1.35 mmol acarbose equivalents/g) and acetylcholinesterase (2.56 mg galanthamin equivalents/g), and had moderate effects on α-amylase, elastase, collagenase and hyaluronidase. Balkan heath could be recommended for raw material production with antioxidant and enzyme inhibitory properties. Full article

Neopicrorhiza scrophulariiflora (Pennell) D.Y.Hong, an endangered perennial herb, is rich in triterpenes, iridoids, and phenolic compounds, which exhibit significant pharmacological effects. However, the molecular mechanisms of triterpenoid biosynthesis in N. scrophulariiflora remain unclear. Here, transcriptomic and metabolomic analyses were performed to investigate the triterpene content in different tissues and the expression patterns of key enzyme-encoding genes related to triterpenoid biosynthesis. We functionally characterized eight upstream oxidosqualene cyclases (OSCs) involved in triterpenoid biosynthesis, among which NsOSC2 is a bifunctional enzyme capable of catalyzing the conversion of 2,3-oxidosqualene to β-amyrin and α-amyrin. Additionally, an efficient regeneration system and a stable genetic transformation system were established for N. scrophulariiflora. These findings reveal key genes in triterpenoid biosynthesis, providing a theoretical foundation for the future production of key triterpenoids in N. scrophulariiflora through synthetic biology approaches. Full article

Melanoma is one of the most aggressive forms of skin cancer, characterized by high metastatic potential and resistance to conventional therapies. Natural compounds, particularly terpenoids, have gained attention for their chemopreventive potential and anticancer properties. These plant-derived compounds exhibit diverse biological activities, e.g., cell viability and proliferation inhibition, apoptosis induction, cell cycle regulation, and immune system modulation. The review evaluates the current state of the art on the chemopreventive and anticancer activity of lupane- (betulinic acid), oleanane- (oleanolic acid, β-amyrin, escin, hederagenin, glycyrrhetinic acid), and ursane-type (ursolic acid, asiatic acid, madecassic acid, α-amyrin) triterpenoids in melanoma, highlighting their mechanisms of action, therapeutic potential, and challenges in clinical application. Full article

Rheumatoid arthritis (RA) is a chronic autoimmune inflammatory disease characterized by the inflammation of synovial fluid. The incidence of cardiovascular diseases (CVDs) is increasing in RA patients. This research is the first report to investigate the anti-arthritic effect of avocado peel nutraceutical (APN) and its potential in mitigating the cardiovascular risk associated with RA. The antioxidant activity and phytochemical composition of APN were assessed. The potential interaction of APN’s active compounds with protein tyrosine phosphatase non-receptor type 22 (PTPN22) was studied using molecular docking. The impact of APN on the plasma lipid profile, oxidative and inflammatory markers, and the indices of coronary risk and atherogenicity as CVD markers were evaluated. The gene expression of COX-2, IL-6, IL-1β, IL-10, and TNF-α in liver and spleen tissues were measured. The rat gut microbiota profile was investigated using 16S rRNA amplicon sequencing. APN exhibited high antioxidant activity, low atherogenicity and thrombogenicity indices, and a high ratio of hypocholesterolemic to hypercholesterolemic fatty acids indicating its cardioprotective potential. The administration of APN led to a reduction in oxidative stress markers, inflammatory markers, dyslipidemia, and CVD markers. APN administration downregulated the expression of COX-2, IL-6, IL-1β, and TNF-α genes, while the IL-10 gene was significantly upregulated in the liver and spleen. Treatment with APN was favorable in restoring eubiosis in the gut by modulating RA-associated bacterial taxa linked to impaired immune function and cardiometabolic diseases. In molecular docking, β-amyrin and ellagic acid showed the highest binding affinity for PTPN22. APN may represent a promising approach to ameliorating the cardiovascular risk of RA. The present results will be offering a foundation for future in-depth research in nutraceuticals from agriculture by-products. Additionally, they will be supporting the public health policies aimed at preventing and controlling rheumatoid arthritis. Full article

The propolis produced by stingless bees is a complex mixture of natural sticky components mixed with soil or clay. Global research on propolis has focused on studying the biological and pharmacological properties and chemical composition of stingless bee propolis from Brazil, Indonesia, and other regions. However, studies of stingless bee propolis produced in Mexico are scarce. This study aimed to determine the chemical composition of the geopropolis of Scaptotrigona mexicana collected in the Totonacapan region and to evaluate its antioxidant and antibacterial activities. The phenolic contents of the ethanolic extract of the collected propolis ranged from 2.45 ± 0.03 mg GAE/g to 3.48 ± 0.56 mg GAE/g of dry extract. The total flavonoid content ranged from 0.69 ± 0.03 mg QE/g to 0.84 ± 0.009 mg QE/g of dry extract. The antioxidant activity of the ethanolic extracts was assessed via DPPH, ABTS, and FRAP assays. The minimum inhibitory concentration values exhibited by the ethanolic extract (>512 g/mL) for Gram-negative bacteria (Pseudomonas aerugunosa and Phorphyromonas gingivalis) were higher than those of Gram-positive bacteria. The stingless bee propolis extract showed the highest antibacterial activity against Streptococcus mutans (256 g/mL). Five known compounds, taraxeryl acetate (1), lupeol (3), cicloart-23-en-3β,25-diol (5), mangiferoic acid (6), and 5-(11’Z-heptadecenyl)-resorcinol (7), and two irresoluble mixtures of 3-O-acetyl-α-(2a) and 3-O-acetyl-β-amyrins (2b), and α- (4a) and -amyrins (4b), were identified by nuclear magnetic resonance spectroscopy and mass spectrometry. Additionally, 39 volatile compounds were identified via headspace-solid phase microextraction using the hyphenated gas chromatography coupled to mass spectrometry time-of-flight. The main volatile compounds detected include trans-α-bergamotene (8.15%), hexanal (7.17%), 2-heptanone (7.60%), and α-copaene (7.09%). Full article

This study aimed to determine the optimal pressure and temperature for the maximum extraction yield and recovery of lipophilic bioactive compounds (BACs) during the supercritical carbon dioxide extraction (SCO₂) of fennel seeds. For this purpose, the SCO₂ pressure (78.6–361.4 bar) and temperature (35.9–64.1 °C) were varied and optimized, and all of the extracts obtained were analyzed for the volatiles, fatty acids, sterols, tocochromanols and carotenoids. The results showed that the maximum extract yield and content of all of the compounds analyzed favored a higher pressure (320 bar) and lower temperature (40 °C), except for the volatiles, which were the highest at 120 bar and 42 °C. However, the optimal SCO₂ conditions for obtaining the highest overall total lipophilic fraction were 320 bar and 40 °C, respectively. The fennel SCO₂ extract obtained under these conditions contained 18 volatiles (trans-anethole as the major component), 12 fatty acids (oleic and petroselinic as the major compounds), 12 sterols (β-sitosterol and stigmasterol as the major compounds), two pentacyclic triterpenoids (α-, β-amyrin), one tocopherol (α-tocopherol), two tocotrienols (γ-, δ-tocotrienol) as well as two carotenoids (lutein and β-carotene). The SCO₂ proved to be very efficient for the isolation of various lipophilic BACs from fennel, and the results of this study may be of interest to academia and industry. Full article

Yataprasen (YTPS) remedy formulary, a national Thai traditional medicine formulary, comprises 13 herbal plants. It has been extensively prescribed to relieve osteoarthritis and musculoskeletal pain in the Thai traditional medicine healthcare system. The aim of this study was to investigate the antioxidant and anti-inflammatory properties of the bioactive compounds (β-amyrin and stigmasterol) of YTPS remedy formulary ethanolic extract, along with its composition. The YTPS formulary extract contains 70.30 nM of β-amyrin and 605.76 nM of stigmasterol. The YTPS formulary extract exhibited ABTS and DPPH free radical scavenging activity, with IC₅₀ values of 144.50 ± 2.82 and 31.85 ± 0.18 µg/mL, respectively. The ethanolic extract of YTPS at a concentration of 1000 µg/mL showed a significant (p < 0.01) anti-inflammatory effect, mainly by reducing IL-6 and TNF-α release in response to LPS. NO production was prominently lowered by 50% at 24.76 ± 1.48 µg/mL, 55.52 ± 24.40 µM, and more than 570 µM of YTPS formulary extract, β-amyrin, and stigmasterol, respectively. Major components of YTPS, β-amyrin, and stigmasterol exerted significant anti-inflammatory effects by inhibiting LPS-induced IL-1β, IL-6, TNF-α secretion in THP-1 cells. Our findings suggest that the ethanolic extract from YTPS holds promise as an alternative topical treatment for osteoarthritis and inflammatory disorders, potentially with fewer side effects than non-steroidal anti-inflammatory medications (NSAIDs). Full article

Background and aim: Chamomile tea, renowned for its exquisite taste, has been appreciated for centuries not only for its flavor but also for its myriad health benefits. In this study, we investigated the preventive potential of chamomile (Matricaria chamomilla L.) towards cancer by focusing on its anti-inflammatory activity. Methods and results: A virtual drug screening of 212 phytochemicals from chamomile revealed β-amyrin, β-eudesmol, β-sitosterol, apigenin, daucosterol, and myricetin as potent NF-κB inhibitors. The in silico results were verified through microscale thermophoresis, reporter cell line experiments, and flow cytometric determination of reactive oxygen species and mitochondrial membrane potential. An oncobiogram generated through comparison of 91 anticancer agents with known modes of action using the NCI tumor cell line panel revealed significant relationships of cytotoxic chamomile compounds, lupeol, and quercetin to microtubule inhibitors. This hypothesis was verified by confocal microscopy using α-tubulin-GFP-transfected U2OS cells and molecular docking of lupeol and quercetin to tubulins. Both compounds induced G2/M cell cycle arrest and necrosis rather than apoptosis. Interestingly, lupeol and quercetin were not involved in major mechanisms of resistance to established anticancer drugs (ABC transporters, TP53, or EGFR). Performing hierarchical cluster analyses of proteomic expression data of the NCI cell line panel identified two sets of 40 proteins determining sensitivity and resistance to lupeol and quercetin, further pointing to the multi-specific nature of chamomile compounds. Furthermore, lupeol, quercetin, and β-amyrin inhibited the mRNA expression of the proinflammatory cytokines IL-1β and IL6 in NF-κB reporter cells (HEK-Blue Null1). Moreover, Kaplan–Meier-based survival analyses with NF-κB as the target protein of these compounds were performed by mining the TCGA-based KM-Plotter repository with 7489 cancer patients. Renal clear cell carcinomas (grade 3, low mutational rate, low neoantigen load) were significantly associated with shorter survival of patients, indicating that these subgroups of tumors might benefit from NF-κB inhibition by chamomile compounds. Conclusion: This study revealed the potential of chamomile, positioning it as a promising preventive agent against inflammation and cancer. Further research and clinical studies are recommended. Full article

Panama boasts an expansive mangrove area and stands as one of the most biodiverse countries in America. While mangrove plants have long been utilized in traditional medicine, there are still unstudied species whose potential medicinal applications remain unknown. This study aimed to extract bioactive compounds from Mora oleifera (Triana ex Hemsl.) Ducke, an understudied mangrove species. Through bioassay-guided fractionation of the crude extract, we isolated seven active compounds identified as lupenone (1), lupeol (2), α-amyrin (3), β-amyrin (4), palmitic acid (5), sitosterol (6), and stigmasterol (7). Compound structures were determined using spectroscopic analyses, including APCI-HR-MS and NMR. Compounds 1–7 displayed concentration-dependent inhibition of the alpha-glucosidase enzyme, with IC₅₀ values of 0.72, 1.05, 2.13, 1.22, 240.20, 18.70, and 163.10 µM, respectively. Their inhibitory activity surpassed acarbose, the positive control (IC₅₀ 241.6 µM). Kinetic analysis revealed that all compounds acted as competitive inhibitors. Docking analysis predicted that all triterpenes bonded to the same site as acarbose in human intestinal alpha-glucosidase (PDB: 3TOP). A complementary metabolomic analysis of M. oleifera active fractions revealed the presence of 64 compounds, shedding new light on the plant’s chemical composition. These findings suggest that M. oleifera holds promise as a valuable botanical source for developing compounds for managing blood sugar levels in individuals with diabetes. Full article

Knowing that biomolecules, such as β-amyrin and α-amyrin, have some pharmacological effects, the aim of this study was directed towards exploring the protective effect of Tomato Peel and Seed Extract (TPSE) for its soothing function but also for its capacity to modulate the adrenal axis, which is involved in stress response. Ex vivo tests were carried out on skin explants to evaluate the effectiveness of TPSE formulated at 0.5% on Calcitonin Gene-Related Peptide (CGRP) and IL-10 release, Kappa Opioid Receptor (KOR), and Caspase 14 expression. An in vivo study combined a clinical evaluation of skin homogeneity and psychological parameters as well as an analysis of salivary cortisol and dehydroepiandrosterone concentrations. All measurements were carried out at the beginning and after 28 days of applying a TPSE face cream. TPSE regulated not only the release of CGRP, IL-10, and the expression of Caspase 14, reflecting anti-neurogenic and anti-inflammatory properties, but also modulated KORs. Twenty-eight days of TPSE application induced a significant decrease in intensity and extent erythrosis, a lower output of salivary cortisol, and a significant increase in pleasant emotions when compared to placebo. These results provide encouragement to continue exploring the impact of cosmetic ingredients on psychophysiological parameters to improve skin health and well-being. Full article

Mental and neurological disorders are conditions that affect thoughts, emotions, behavior, and relationships. Malpighia mexicana A. Juss. is a plant used in Mexican traditional medicine for the treatment of such disorders. This work aimed to investigate the antidepressant, anxiolytic, sedative, hypnotic, and anticonvulsant effects of the acetonic extract (MmAE) of M. mexicana and its fractions (F3, F4-10, F14) using the forced swimming test (FST), elevated plus maze (EPM), open field test (OFT), pentobarbital-induced sleep test (PBTt), and pentylenetetrazol-induced seizure test (PTZt). MmAE, F3, F4-10, F14, and vehicle were administrated orally 24, 18, and 1 h prior to the evaluations. Imipramine (15 mg/kg, p.o.) was administrated 1 h prior to the evaluations as a positive control for the FST, while diazepam (1 mg/kg, p.o.) was administrated 1 h prior to the evaluations as a positive control for the EPM, OFT, PBTt, and PTZt. MmAE had an anxiolytic effect; MmAE and F3, F4-10, and F14 showed an antidepressant effect, sedative effect, hypnotic effect, and anticonvulsant effect. Using HPLC, we identified the compounds quercetin 3-O-rutinoside (1), kaempferol 3-O-glucoside (2), luteolin 7-O-glucoside (3), quercetin (4), and kaempferol (5) in MmAE and compounds (1), (2), and (3) in F14. Using GC-MS, we identified α-tocopherol, phytol, and β-amyrin in F3; β-tocopherol, phytol, β-sitosterol, and β-amyrin in F4-10; and α- tocopherol, phytol, β-sitosterol, and β-amyrin in F4-10. The neuropharmacological effects found in this work may be due to the presence of vitamins, phytosterols, terpenes, and flavonoids. This research requires further study to clarify the mechanisms of action of the identified compounds. Full article