Search Results (8)

Valerian root extracts are widely used as mild sedatives to promote sleep, with clinical studies confirming their efficacy. Their sleep-promoting effects are associated with the adenosine A1 receptor (A1AR), a key regulator of sleep through neural activity inhibition. Adenosine, a neuromodulator that accumulates during wakefulness, activates A1ARs to facilitate sleep transitions. Using advanced analytics, we detected adenosine at 0.05% in the valerian extract Ze 911, supporting direct A1AR activation in vitro. Additionally, we explored A1ARs’ allosteric sites for modulatory activity. Valerenic acid and pinoresinol, key constituents of Ze 911, were identified as positive allosteric modulators (PAMs) of A1ARs. Valerenic acid exhibited strong PAM activity, with high cooperativity (αβ = 4.79 for adenosine and αβ = 23.38 for CPA) and intrinsic efficacy (τB = 5.98 for adenosine and τB = 3.14 for CPA). Pinoresinol displayed weaker PAM activity, with moderate cooperativity (αβ = 3.42 for adenosine and αβ = 0.79 for CPA) and limited efficacy (τB = 0.93 for adenosine and τB = 1.66 for CPA). The allosteric modulation observed in valerian extract Ze 911 suggests a mechanism of action in which valerenic acid and pinoresinol enhance receptor activation through allosteric interactions, potentially amplifying the effects of endogenous adenosine. By targeting A1ARs’ allosteric sites, valerian extract Ze 911 offers increased therapeutic selectivity and reduced off-target effects, emphasizing its potential for managing sleep disorders. Full article

Plant raw materials with a calming effect on the nervous system are increasingly used in modern phytotherapy. Lavender belongs to this group of plants, due to the content of essential oil with known therapeutic properties and other phytoconstituents that can be responsible for the sedative effect. Our studies confirmed the presence of sesquiterpenic acids characterized by sedative activity in lavender extracts. The contents of valerenic acid and acetoxyvalerenic acids in flowers and leafy stalks of two various Lavandula angustifolia cultivars—‘Blue River’ and ‘Ellagance Purple’—were determined. Analyses of methanolic extracts performed using the HPLC method showed that content of these sesquiterpenic acids varied with the cultivars and the morphological parts of the plant. The amount of acetoxyvalerenic acid was significantly higher than the amount of valerenic acid. In the ‘Blue River’ cultivar, higher levels of both compounds characterized by sedative properties were found. The content of valerenic acid in flowers ranged from 0.50 mg/100 g d.m. in the ‘Ellagance Purple’ cultivar to 1.75 mg/100 g d.m. in the ‘Blue River’ cultivar. In turn, leafy stalks contained 0.81 mg/100 g d.m. of valerenic acid in the ‘Ellagance Purple’ cultivar and 1.16 mg/100 g d.m. in the ‘Blue River’ cultivar. Interestingly, the ‘Blue River’ cultivar contained about 10 times more acetoxyvalerenic acid (65.80 mg/100 g d.m.) in flowers and four times more acetoxyvalerenic acid in leafy stalks (50.1 mg/100 g d.m.), in comparison with the ‘Ellagance Purple’ cultivar. The higher content of valerenic and acetoxyvalerenic acids in the flowers and leafy stalks of the ‘Blue River’ lavender cultivar can be important for its possible medical applications. Full article

Common valerian is a medicinal plant. The underground organs of this species are used as a mild sedative and sleeping aid. Poland is one of the largest producers of this raw material in Europe, with local cultivar ‘Lubelski’ as a primary cultivated form. Although valerian is the subject of more or less deliberate selection carried out by farmers, it is still genetically unstable. The aim of this study was to determine the diversity of the ‘Lubelski’ cultivar originating from four regions of Poland (forms: L1–L4) in relation to wild-growing populations of the species. The plants were assessed in terms of the mass of underground organs and the content of valerenic acids and essential oils (EOs). The content of valerenic acids was determined using HPLC, whereas the content of EOs was determined using hydrodistillation. The composition of EOs was assessed using GC-MS GC-FID. The ploidy level of the analyzed objects was determined as well. Wild-growing populations (diploids) were characterized by lower masses of underground organs and lower contents of valerenic acid than cultivated forms (tetraploids). However, they produced higher contents of EOs. All the cultivated forms were strongly diversified with respect to the analyzed traits, including the mass of the roots (CV 49–75%), the content of valerenic acids (CV 18–55%), and the content of EOs (CV 28–57%). A total of 44 compounds were identified in the EOs. The dominant compound of both wild-growing populations and the ‘Lubelski’ forms were: α-fenchene, bornyl acetate, and valerenal. Among ‘Lubelski’ forms, the most interesting seems to be the L2 form, which was characterized by a relatively high yield and high content of valerenic acids and EOs. Thus, it appears to be a promising source of objects for further valerian cultivar improvement. Full article

In this study, the biochemical, antioxidant properties, and antimicrobial activity of the epiphytic leafy liverwort Frullania dilatata (L.) Dumort were investigated. Due to the scarcity and difficulty in obtaining liverworts, research on their bioactivity is limited; thus, this study aimed to uncover the potential of F. dilatata. The antimicrobial activity was evaluated against various microorganisms, including food isolates, clinical isolates, multidrug-resistant strains, and standard strains, using the disk diffusion method and determining the minimum inhibitory concentration (MIC) values. This study represents the first antioxidant investigation on F. dilatata and an antimicrobial study using ethanol extract and the disk diffusion method. Notably, susceptibility was observed in Enterococcus faecalis ATCC 29212, Enterococcus faecium FI, Listeria monocytogenes ATCC 7644, Providencia rustigianii MDR, and Staphylococcus aureus ATCC 25923. The antioxidant capacity was assessed using the DPPH method, emphasizing the high scavenging performance. Gas chromatography-mass spectrometry (GC-MS) analysis identified the primary compounds as frullanolide (19.08%), 2,3-Dimethylanisole (15.21%), linoleic acid (11.11%), palmitic acid (9.83%), and valerenic acid (5.3%). The results demonstrated the significant antimicrobial activity of F. dilatata against the tested microorganisms and its potent antioxidant properties. These findings emphasize the potential of F. dilatata as a promising source of natural antimicrobial and antioxidant agents, underscoring the importance of further investigation into its bioactive compounds and elucidating the mechanisms of action in future studies. Full article

Extractions of the underground parts of valerian were prepared with water and ethanol (25–95%) at 25–75 °C. Extraction yields, bioactive compounds, and the 1,1-Diphenyl-2-picrylhydrazyl (DPPH) radical scavenging ability of lyophilized extracts were determined. The inhibitory effects of the extracts, valerenic acid derivatives and phenolic acids, on metabolic syndrome (MS)-related enzymes activities were further examined. Both roots and rhizomes extracted with 95% ethanol at 75 °C had the highest levels of bioactive compounds. The antioxidant capacity and inhibition of MS-related enzymes of the roots extract were better than those of the rhizomes. The roots extract more strongly inhibited pancreatic lipase (inhibition of 50% of enzyme activity (IC₅₀), 17.59 mg/mL), angiotensin-converting enzyme (ACE, IC₅₀, 3.75 mg/mL), α-amylase (IC₅₀, 12.53 mg/mL), and α-glucosidase (IC₅₀, 15.40 mg/mL). These four phenolic acids inhibited the activity of MS-related enzymes. Valerenic acid demonstrated more of an inhibitory ability for ACE (IC₅₀, 0.225 mg/mL, except for caffeic acid) and α-glucosidase (IC₅₀, 0.617 mg/mL) than phenolic acids. Valerian extract inhibited key enzyme activities that were associated with obesity (lipase), hypertension (ACE), and type 2 diabetes (α-amylase and α-glucosidase), suggesting that it is a potential candidate for the development of functional supplements. Full article

Valerenic acid (VA) is a sesquiterpenoid and a phytoconstituent of the plant valerian used for sleeping disorders and anxiety. The frequency of using herbal components as therapeutic nutritional agents has increased lately. Their ability to improve redox homeostasis makes them a valuable approach against harmful xenobiotics. The purpose of this study was to evaluate the putative beneficial role of VA against the redox-perturbating role of the fungicide benomyl in HepG2 human liver cells in terms of oxidative stress in the cellular environment and in endoplasmic reticulum (ER). Benomyl increased cell total oxidant status and reactive oxygen species production and decreased total antioxidant status. The expression of genes coding for antioxidant molecules, namely, heme oxygenase-1, alpha glutathione s-transferase, NF-ĸB, and liver fatty acid binding protein, were decreased due to benomyl. VA ameliorated these effects. Benomyl also increased ER-stress-related molecules such as endoplasmic reticulum to nucleus signaling 1 protein, glucose-regulated protein 78, and caspase-12 levels, and VA acted also as a preventive agent. These results indicate that VA exerts ameliorative effects after benomyl-induced oxidative stress. VA, a widely used nutritional supplement, is a compound with potent antioxidant properties, which are valuable for the protection of cells against xenobiotic-induced oxidative damage. Full article

There is growing interest for medicinal plants in the world drug market. Particularly, Matricaria recutita L., Valeriana officinalis L., Tilia spp., and Camellia sinensis (L.) Kuntze are some of the most consumed medicinal plants for treatment of minor health problems. Medicinal plants are seen as natural and safe; however, they can cause interactions and produce adverse reactions. Moreover, there is lack of consensus in medicinal plants regulation worldwide. DNA barcoding and UHPLC-MS technique are increasingly used to correctly identify medicinal plants and guarantee their quality and therapeutic safety. We analyzed 33 samples of valerian, linden, tea, and chamomile acquired in pharmacies, supermarkets, and herbal shops by DNA barcoding and UHPLC-MS. DNA barcoding, using matk as a barcode marker, revealed that CH1 sold as Camellia sinensis was Blepharocalyx tweediei, and sample TS2 sold as linden belong to Malvales. On the other hand, UHPLC-MS analysis revealed the presence of bioactive compounds (apigenin-7-glucoside, acetoxy valerenic acid, valerenic acid, epigallocatechin, and tiliroside). However, none of samples met minimum content of these active principles (except for valerenic acid in VF3) according to the European Medicines Agency (EMA) and Real Spanish Pharmacopeia. In conclusion, this study revealed the need to incorporate DNA barcoding and HPLC-MS techniques in quality controls of medicinal plants. Full article

Valeriana fauriei (V. fauriei), which emits a characteristic and unpleasant odor, is important in traditional medicine. In this study, the expression of terpenoid biosynthetic genes was investigated in different organs that were also screened for volatile compounds including valerenic acid and its derivatives. Specific expression patterns from different parts of V. fauriei were observed using quantitative real-time PCR (qRT-PCR). The highest transcript levels of biosynthetic genes involved in mevalonic acid (MVA) and methylerythritol phosphate (MEP) production were found in the stem. Although the amounts of volatile compounds were varied by organ, most of the volatile terpenoids were accumulated in the root. Gas chromatography mass spectrometry (GC-MS) analysis identified 128 volatile compounds, which represented 65.33% to 95.66% of total volatiles. Certain compounds were only found in specific organs. For example, isovalerenic acid and valerenic acid and its derivatives were restricted to the root. Organs with high transcript levels did not necessarily have high levels of the corresponding chemical constituents. According to these results, we hypothesize that translocation may occur between different organs in V. fauriei. Full article