Search Results (9)

The current trend in microbiological research aimed at limiting the development of biofilms of multidrug-resistant microorganisms is increasingly towards the search for possible synergistic effects between various compounds. This work presents a combination of a naturally occurring compound, β-aescin, newly synthesized alkylamidobetaines (AABs) with a general structure—C_nTMDAB, and antifungal drugs. The research we conducted consists of several stages. The first stage concerns determining biological activity (antifungal) against selected multidrug-resistant strains of Candida glabrata (C. glabrata) with the highest ability to form biofilms. The second stage of this study determined the activity of β-aescin combinations with antifungal compounds and alkylamidobetaines. In the next stage of this study, the ability to eradicate a biofilm on the polystyrene surface of the combination of β-aescin with alkylamidobetaines was examined. It has been shown that the combination of β-aescin and alkylamidobetaine can firmly remove biofilms and reduce their viability. The last stage of this research was to determine the safety regarding the cytotoxicity of both β-aescin and alkylamidobetaines. Previous studies on the fibroblast cell line have shown that C9 alkylamidobetaine can be safely used as a component of anti-biofilm compounds. This research increases the level of knowledge about the practical possibilities of using anti-biofilm compounds in combined therapies against C. glabrata. Full article

The cultivation and enrichment of different soils in a vineyard yielded 95 yeast species. Among them, seven strains capable of producing β-glucosidases were identified using the aescin colorimetric method. One non-Saccharomyces yeast strain was isolated from a plate containing lysine and identified using internal transcription (ITS) as Candida cf. sorbosivorans (C. cf. sorbosivorans), which was named Candida cf. sorbosivorans X1. Additionally, the enzymatic characteristics of the β-glucosidases produced by this strain were investigated. The β-glucosidases generated by C. cf. sorbosivorans X1 displayed high enzymatic activity and enzyme-activity retention in a pH range of 3.0 to 5.4 and at temperatures of 30 °C to 35 °C. Using non-targeted metabolomics methods, we investigated the alterations in metabolites during the fermentation of mango juice. The strain C. cf. sorbosivorans X1 demonstrated activity against phenols and terpenes. In the fermented mango juice (X1FMJ), we identified 41 differential metabolites. These included 14 esters, 4 hydrocarbons, 3 aldehydes, 5 ketones, 4 terpenoids, 4 alcohols, 1 aromatic hydrocarbon, 2 amines, 1 acid, and 3 heterocyclic compounds. The metabolic pathways of these differential metabolites were analyzed, revealing four key pathways: tyrosine metabolism, phenylpropanoid biosynthesis, monoterpene biosynthesis, and α-linolenic acid metabolism, which promoted the formation of aroma compounds in the fermented mango juice. Full article

In this study, the interplay among the phospholipid 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) as a model membrane, the nonsteroidal anti-inflammatory drug naproxen, and the saponin $\beta$-aescin are investigated. The naproxen amount was fixed to 10 mol%, and the saponin amount varies from 0.0 to 1.0 mol%. Both substances are common ingredients in pharmaceutics; therefore, it is important to obtain deeper knowledge of their impact on lipid membranes. The size and properties of the DMPC model membrane upon naproxen and aescin addition were characterized with differential scanning calorimetry (DSC), small- and wide-angle X-ray scattering (SAXS, WAXS), and photon correlation spectroscopy (PCS) in a temperature-dependent study. The interaction of all substances was dependent on the lipid phase state, which itself depends on the lipid’s main phase transition temperature $T_{\mathrm{m}}$. The incorporation of naproxen and aescin distorted the lipid membrane structure and lowers $T_{\mathrm{m}}$. Below $T_{\mathrm{m}}$, the DMPC–naproxen–aescin mixtures showed a vesicle structure, and the insertion of naproxen and aescin influenced neither the lipid chain–chain correlation distance nor the membrane thickness. Above $T_{\mathrm{m}}$, the insertion of both molecules instead induced the formation of correlated bilayers and a decrease in the chain–chain correlation distance. The presented data clearly confirm the interaction of naproxen and aescin with DMPC model membranes. Moreover, the incorporation of both additives into the model membranes is evidenced. Full article

Background: Benign prostatic hyperplasia (BPH) is the most common urogenital condition in aging males, while inflammation and tissue proliferation constitute the main pathophysiological factors. The adverse effects of currently available BPH medications limit patient compliance. We tested the protective effect of aescin against the development of BPH in rats. Methods: A total of 18 male Wistar rats were divided into 3 groups: control (sesame oil 1 mL/kg, s.c.); BPH (testosterone oenanthate 3 mg/kg, s.c., in sesame oil), and BPH-aescin rats (testosterone oenanthate 3 mg/kg, s.c. + aescin 10 mg/kg/day, p.o.). All treatments continued for 4 weeks. Serum and prostatic samples were harvested for biochemical and histopathological examination. Results: Induction of BPH by testosterone increased the prostate weight and prostate weight index, serum testosterone, prostate expression of inflammatory (IL-1β, TNF-α, and COX-2), and proliferative markers (PCNA and TGF-β1). Concurrent treatment with aescin decreased the testosterone-induced increase in prostatic IL-1β, TNF-α, and COX-2 expression by 47.9%, 71.2%, and 64.4%, respectively. Moreover, aescin reduced the prostatic proliferation markers TGF-β1 and PCNA by 58.3% and 71.9%, respectively, and normalized the prostate weight. Conclusion: The results of this study showed, for the first time, that aescin protected against the development of experimental BPH in rats via its anti-inflammatory and antiproliferative effects. These findings warrant further studies to clinically repurpose aescin in the management of BPH. Full article

Fruit from A. hippocastanum L. are used commercially for chronic venous insufficiency (CVI). The isomeric mixture of pentacyclic triterpenoid saponins (β-aescin) exert anti-inflammatory effects. Hence, research has focused on β-aescin, yet the diversity, accumulation, and bioactivity of organ-specific secondary metabolites represent missed pharmacological opportunities. To this end, we applied an untargeted metabolomics approach by liquid chromatography—tandem mass spectrometry (LC–MS/MS) to the chemical profiles of flowers, immature fruits, and pedicels from 40 specimens across 18 species of Aesculus. Principal component analysis (PCA), orthogonal partial least squares (OPLS-DA), and molecular networking revealed stronger chemical differences between plant organs, than between species. Flowers are rich in glycosylated flavonoids, pedicels in organic acids and flavonoid aglycones, and immature fruits in monomeric flavan-3-ols and procyanidins. Although a high diversity of flavonoids and procyanidins was observed, the relative amounts differed by plant organ. Fruit extracts demonstrated the strongest antifungal (Saccharomyces cerevisiae) and antioxidant activity, likely from the procyanidins. Overall, secondary metabolite profiles are organ-specific, and fruits accumulate antifungal and antioxidant compounds. Due to the chemical similarity between species, similar effects may be achieved between species. This creates incentives for further exploration of the entire genus, in bioprospecting for potential therapeutic leads. Full article

The dissociation constant is an important physicochemical property of drug molecules that affects the pharmacokinetic and pharmacodynamic properties of drugs. In this study, the distribution coefficients of 16 active ingredients extracted from herbal materials were determined at different pH values in liquid–liquid equilibrium systems; the active ingredients were sinomenine, aescin A, aescin B, aescin C, aescin D, chlorogenic acid, neochlorogenic acid, cryptochlorogenic acid, isochlorogenic acid A, isochlorogenic acid B, isochlorogenic acid C, baicalin, wogonoside, calycosin-7-glucoside, astraisoflavan-7-O-β-D-glucoside, and isomucronulatol 7-O-glucoside. The dissociation constants of these active ingredients were calibrated and compared with reported values. The dissociation constants obtained were close to those reported in other studies, which means that the results of this work are reliable. Full article

$\beta$ -aescin is a versatile biosurfactant extracted from the seeds of the horse chestnut tree Aesculus hippocastanum with anti-cancer potential and is commonly used in the food and pharmaceutical and cosmetic industries. In this article, wide-angle X-ray scattering (WAXS) is used in order to study the modifications of the structural parameters at the molecular scale of lipid bilayers in the form of bicelles composed of 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) and the triterpenoid saponin $\beta$ -aescin. In particular, the impact on the cooperative phase transition and the structural parameters of the DMPC bilayers at different compositions and temperatures is of special interest. Moreover, we show how cholesterol and the non-steroidal anti-inflammatory drug (NSAID) ibuprofen modulate the structural parameters of the $\beta$ -aescin-DMPC assemblies on a molecular scale. Ibuprofen and cholesterol interact with different parts of the bilayer, namely the head-region in the former and the tail-region in the latter case allowing for specific molecular packing and phase formation in the binary and ternary mixtures. Full article

This review discusses recent progress in physicochemical understanding of the action of the saponin $\beta$ -aescin (also called $\beta$ -escin), the biologically active component in the seeds of the horse chestnut tree Aesculus hippocastanum. $\beta$ -Aescin is used in pharmacological and cosmetic applications showing strong surface activity. In this review, we outline the most important findings describing the behavior of $\beta$ -aescin in solution (e.g., critical micelle concentration ( $cmc$ ) and micelle shape) and special physicochemical properties of adsorbed $\beta$ -aescin monolayers at the air–water and oil–water interface. Such monolayers were found to posses very special viscoelastic properties. The presentation of the experimental findings is complemented by discussing recent molecular dynamics simulations. These simulations do not only quantify the predominant interactions in adsorbed monolayers but also highlight the different behavior of neutral and ionized $\beta$ -aescin molecules. The review concludes on the interaction of $\beta$ -aescin with phospholipid model membranes in the form of bilayers and Langmuir monolayers. The interaction of $\beta$ -aescin with lipid bilayers was found to strongly depend on its $cmc$ . At concentrations below the $cmc$ , membrane parameters are modified whereas above the $cmc$ , complete solubilization of the bilayers occurs, depending on lipid phase state and concentration. In the presence of gel-phase phospholipids, discoidal bicelles form; these are tunable in size by composition. The phase behavior of $\beta$ -aescin with lipid membranes can also be modified by addition of other molecules such as cholesterol or drug molecules. The lipid phase state also determines the penetration rate of $\beta$ -aescin molecules into lipid monolayers. The strongest interaction was always found in the presence of gel-phase phospholipid molecules. Full article

Oxidative stress is involved in the development and progression of disease. Because sodium aescinate has been reported to have immunity enhancing and antioxidative effects, we investigated its activity by employing a hepatocellular carcinoma (HCC) mouse model. Sixty BALB/c mice were randomly divided into four groups, including a 1.4 mg/kg treated group (n = 15), a 2.8 mg/kg treated group (n = 15), an untreated hepatocellular carcinoma control group (n = 15) and a normal control group (n = 15). After H22 cells were cultured for one week, we collected 2 × 10⁶ cells and injected them subcutaneously as 0.2 mL cell suspensions in sterile saline into the right shoulder region of every mouse. The animals were monitored for changes in activity, physical condition and body weight during the experiment. The next day after injection of H22 cells, animals in these test groups received one intraperitoneal injection of drug or physiological saline for 13 days. Results showed that in the sodium aescinate injection liquid (SAIL)-treated HCC mice, serum interleukin-1 beta (IL-1β), interleukin-6 (IL-6), tumor necrosis factor-alpha (TNF-α), interferon-gamma (IFN-γ), Gamma-glutamyltransferase (γ-GT), alanine transaminase (ALT), aspartate transaminase (AST) and alkaline phosphatase (ALP) levels were significantly decreased compared with normal control mice. In addition, treatment with sodium aescinate injection liquid significantly decreased blood and liver malondialdehyde (MDA) levels, increased glutathione (GSH) levels, and antioxidant enzyme [superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GSH-Px)] activities in a dose-dependent manner. We conclude that sodium aescinate injection liquid can decrease oxidative injury and enhance immunity functions in HCC mice. Full article