Extraction Of Glycosides Research Articles

Efficient ultrasonic extraction of alkaloids and glycosides from Camptotheca acuminata Decne via deep eutectic solvents: Kinetics and mechanisms

The study investigated the extraction of alkaloids and glycosides from the Camptotheca acuminata Decne using deep eutectic solvent (DES). 18 types of deep eutectic solvents (DESs) were prepared, and it was found that the extraction performance of choline chloride (ChCl)-formic acid (FA) was optimal, surpassing traditional solvents such as methanol/70 % methanol. In comparison to methanol, the extracted amount of compounds by DES was 2–3 times higher. The extraction processes involving the molar ratio of ChCl-FA, pH, DES/H2O mass ratio, solid/liquid ratio, as well as ultrasonic power were optimized. A mathematical model for solid/liquid extraction kinetics from Camptotheca acuminata Decne was developed. The extraction mechanism was investigated using scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), and 1H nuclear magnetic resonance(1H NMR). The results revealed that the DES caused dissociation in Camptotheca acuminata Decne and formed hydrogen bonds with Camptothecin (CPT). Meanwhile, density functional theory (DFT) calculations verified that FA-based exhibited the highest extracted amount for CPT. In addition, this study investigated the recovery rate of DES, and the results showed that after 10 cycles, the DES system remained effective for the extraction of alkaloids and glycosides.

Anti-Alzheimer's Potency of Rich Phenylethanoid Glycosides Extract from Marrubium vulgare L.: In Vitro and In Silico Studies.

Marrubium vulgare L. (M. vulgare), the white horehound, is well known for treating inflammation-related diseases. In this context, we investigated the efficacy of M. vulgare ingredients in treating Alzheimer's disease using various in vitro and in silico antioxidant, anti-inflammatory, anti-cholinesterase, and anti-tyrosinase mechanisms. In our results, sixty-one components were tentatively identified using gas and liquid chromatography (GC-MS and LC-MSn) and categorized as hydrocarbons, fatty acids, and polyphenolics. The extract inhibited linoleic oxidation with an IC50 value of 114.72 µg/mL, captured iron (Fe2+) ions with an IC50 value of 164.19 µg/mL, and displayed reducing power. In addition, the extract showed radical-scavenging ability towards DPPH•, NO•, ABTS•+, and H2O2 assays compared to L-ascorbic acid and butylated hydroxytoluene. The DPPH• was scavenged by 77.62% at 100 µg/mL, and NO•, ABTS•+, and H2O2 were scavenged with IC50 values of 531.66, 117.51, and 143.10 µg/mL, respectively. M. vulgare also exhibited discriminating anti-inflammatory potency against cyclooxygenase (COX-2) with IC50 values of 619.15 µg/mL compared to celecoxib (p > 0.05). Notably, three Alzheimer's biomarkers, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and tyrosinase were significantly inhibited. The molecular docking study supposed that the phenylethanoid glycosides of samioside and forsythoside B inhibited AChE and tyrosinase enzymes with low binding affinities of -9.969 and -8.804 kcal/mol, respectively. Marruboside was a proper inhibitor of COX and BChE enzymes with a binding score of -10.218 and -10.306 kcal/mol, respectively. M. vulgare extract showed significant inhibitory actions, which suggest that it could have a promising potential as an anti-Alzheimer agent.

Raman Spectroscopic Analysis of Steviol Glycosides: Spectral Database and Quality Control Algorithms

Besides all sharing an extraordinary high (i.e., up to ~450 times) sweetening power as compared to sucrose and while presenting strong similarities in their molecular structures, molecules belonging to the family of diterpene glycosides (i.e., the secondary metabolites of Stevia rebaudiana) differ in specific structural details that strongly impact on their levels of sweetness and bitter aftertaste. Given the nutritional and pharmacological benefits of steviol secondary metabolites as natural dietetic and anti-diabetic remedies, extraction and purification of steviol glycosides from plant material are nowadays widely spread among many countries. However, an unpleasant bitter aftertaste, which is linked to a genetic variation in human bitter taste receptors, hampers the full exploitation of such benefits and calls for a prompt improvement in organoleptic property control of stevia products. A deeper understanding of the molecular structure of different steviol glycosides and the consequent development of promptly measurable criteria for the organoleptic performance of their mixtures will support processing optimization and control of taste profiles within desired yields. The present research aimed at establishing Raman spectroscopic algorithms for quantitative characterizations of raw stevia-based sweetener products. First, a series of twelve high-purity diterpene glycosides were analyzed by high spectrally resolved Raman spectroscopy and their spectra analyzed in order to establish a complete Raman library of molecular structures. Then, quantitative spectroscopic parameters were built up and applied to characterize the organoleptic property of five different commercially available samples including the recently developed Rebaudioside M isoform. Raman spectroscopy was confirmed as a versatile analytical technique that could be used for quantitative quality control tasks on the production line and for prompt in situ characterizations of purchased products.

Application of natural sweetener Stevia rebaudiana in the medical field

Steviol glycoside sweeteners have been isolated and produced for hundreds of years in Bertoni, a South American Asteraceae plant prized for its sweetness. Stevia is becoming more popular among consumers and food manufacturers as a result of diabetes, rising obesity rates, and other related comorbidities, as well as global public policies calling for a reduction in intake of sugar to help control these issues. Low-calorie as well as no-calorie sweeteners, such as Stevia, have this appeal because they are plant-based, have no calories, and have a sugary flavour that is 50 to 350 times sweeter than table sugar, making them an excellent as well as suitable choice for use in foods as well as beverages with lower sugar and calorie content. This plant yields steviol glycoside sweeteners, which are isolated and processed. Current studies on Stevia rebaudiana extract, metabolism, tolerable intake, and safety, steviol glycoside extraction and purification, side effects, as well as the toxicity of Stevia extract are discussed in detail.

Ultrahigh pressure enhances the extraction efficiency, antioxidant potential, and hypoglycemic activity of flavonoids from Chinese sea buckthorn leaves

Ultrahigh pressure extraction (UHPE) is an emerging non-thermal extraction technology, but whether this technology can be used for extracting flavonoids from sea buckthorn leaves remains unelucidated. This study optimized the processing conditions for flavonoid extraction from Chinese sea buckthorn leaves through UHPE and compared the results obtained with those of ultrasonic-assisted extraction (UAE) and conventional solvent extraction (CSE). The optimum parameters for UHPE were as follows: ethanol concentration, 50%; liquid-solid ratio, 41:1; pressure, 143 MPa; temperature, 44 °C; and holding time, 3 min. Compared with the UAE and CSE extracts the UHPE extracts had a higher content of total flavonoids and flavonol monomers, and the advantages of UPHE were primarily observed in the extraction of flavonoid monosaccharide chain glycosides and flavonoid aglycones. In total, 36 flavonoids were identified in the three extracts, with 33, 30, and 28 flavonoids identified in UHPE, UAE and CSE, respectively. Additionally, the UHPE extracts had a greater ferric reducing antioxidant power (FRAP), oxygen radical absorption capacity (ORAC), α-amylase inhibitory activity, and α-glucosidase inhibitory activity. In conclusion, the efficiency of UHPE to extract flavonoids from sea buckthorn leaves was significantly higher than those of UAE and CSE.

The Influence of Sucrose on Biomass and Glycosides Content of Callus Cultured from the Leaves of Stevia rebaudiana Bertoni

Stevia rebaudiana Bertoni contains diterpenoid steviol glycosides that have no adverse impact on blood sugar levels despite being 300 times sweeter than sugar. This study aimed to investigate the rate of callus induction from stevia leaves and the content of glycosides when changing the sucrose percentage in the culture medium.. Murashige and Skoog (MS) culture medium supported by 4.0 mg/l naphthalene acetic acid (NAA) and 1.0 mg/l benzyl adenine (BA) was used, and different concentrations of sucrose (2, 3, 4, 5 and 6%) were tested .The extraction of glycosides from leaf and callus tissues was performed by using methanol. Extracted glycosides were analyzed by high-performance liquid chromatography (HPLC). The results showed significant influences of sucrose on callus initiation. The concentration of 3% sucrose had the highest fresh and dry weight. No callus was induced in the MS medium with a high concentration of sucrose (5% and 6%). However, the highest glycoside content, stevioside and rebaudioside were obtained from callus treated with 4% concentration followed by 3% sucrose the treatment . The highest fresh and dry weight average was obtained with a 3% concentration of sucrose, this treatment also increased the concentration of glycosides in the callus twice as much as in the leaves, and concentrations of 3% and 4% of sucrose gave very similar concentrations of glycosides in callus in terms of being double what was found in the leaves something which may aid in the development of a stevia glycosides based industry.

Association of enzymatic and optimized ultrasound-assisted aqueous extraction of flavonoid glycosides from dried Hippophae rhamnoides L. (Sea Buckthorn) berries

The main purpose of the present study was to determine the effect of associating an optimized ultrasound-assisted extraction (UAE) protocol with enzyme-assisted extraction (EAE) in aqueous media, using the dried berries of Hippophae rhamnoides L. (sea buckthorn) as plant material. A specialized software was used for the determination of potential optimal extraction parameters, leading to the development of four optimized extracts with different characteristics (UAE ± EAE). For these extracts, buffered or non-buffered solutions have been used, with the aim to determine the influence of adjustable pH on extractability. As enzymatic solution, a pectinase, cellulase, and hemicellulase mix (2:1:1) has been applied, acting as pre-treatment for the optimized protocol. The highest extractive yields have been identified for non-buffered extracts, and the E-UAE combination obtained extracts with the highest overall in vitro antioxidant activity. The HPLC-MSn analysis demonstrated a rich composition in different types of isorhamnetin-O-glycosides, as well as some quercetin-O-glycosides, showing a high recovery of specific flavonol-type polyphenolic species. Moreover, we have tentatively identified two flavanols (i.e., catechin and epigallocatechin) and one flavone derivative (i.e., luteolin).

A green and recyclable ternary deep eutectic solvent for extracting flavonol glycoside from Ginkgo leaves: Mechanism insights based on molecular level

A novel ternary deep eutectic solvent (DES) was designed for the green and efficient extraction of flavonol glycosides (FG) from Ginkgo leaves. The DES consisted of a molar ratio of choline chloride/acetic acid/1,2-propylene glycol of 1:2:3. The optimal extraction conditions were determined to a solid-liquid ratio of 42 mg/mL, an extraction time of 11.8 h, and an extraction temperature of 51℃. The extraction yield of FG was 7.8 mg/g, which demonstrated a notable enhancement in comparison to conventional extraction. Kinetics and morphology analysis revealed that the extraction process involved considerable dissolution and diffusion of the solute. Additionally, a molecular investigation using density functional theory (DFT) indicated that the interaction between the DES and FG was primarily governed by hydrogen bonding and van der Waals force. Notably, the ternary DES exhibited stronger interactions with FG, which were the key factors for better extraction efficiency. Furthermore, efficient recovery of FG from the DES solution was also achieved, with a recovery rate of 94.63%. Moreover, the recovered DES could be reused directly at least five cycles.

Metabolome-microbiome insights into therapeutic impact of 8-O-acetylharpagide against breast cancer in a murine model.

Iridoid glycosides extract, which is the main active extract of Ajuga decumbens Thunb, has been proved to have anti-breast cancer activity in previous studies. However, it is still unknown whether 8-O-acetylharpagide, a main active compound in the extract, has anti-breast cancer activity. In this study, 4T1 breast cancer mice model was first successfully established. Then the anti-breast cancer effect of 8-O-acetylharpagide was systematically investigated. Feces were collected for metabolomics and 16S rRNA analysis to assess the potential mechanism. The results showed that 8-O-acetylharpagide was effective in reducing 4T1 mouse tumor volume and weight compared with the model group. Metabolome analysis revealed 12 potential metabolite biomarkers in feces, mainly involved in primary bile acid biosynthesis and arachidonic acid metabolism. The 16S rRNA sequencing results demonstrated that 8-O-acetylharpagide modulated the abundance of the intestinal flora in 4T1 mice. Spearman correlation analysis showed that calcitriol and prostaglandin G2 strongly correlated with Akkermansia, Firmicutes and Muribaculum. Overall, the active compound 8-O-acetylharpagide could inhibit significantly breast cancer growth in 4T1 breast cancer model mice. The mechanism of the anti-breast cancer effect of 8-O-acetylharpagide may be related to the regulation of primary bile acid biosynthesis and arachidonic acid metabolism and modulation of the abundance of Akkermansia and Firmicutes.

Analysis of the Glycoside Composition of Calendula Extract

Purpose of research. The aim of the article is to comparatively analyse the glycoside (flavonoid) composition of liquid dosage forms containing calendula medicinalis as an initial raw material.Methods. To achieve this goal, methods for extracting medicinal plant materials were studied, scientific literature on the research topic was analyzed, qualitative and quantitative analysis was carried out, and the obtained UV spectra were examined. Obtaining liquid dosage forms from Calendula officinalis flowers was carried out using a Soxhlet extractor and the maceration method. The optimal conditions for the extraction of glycosides were determined by varying the ratio of raw materials and extractant, as well as the concentration of the extractant. For quantitative assessment, the content of extractive substances in the resulting dosage forms was calculated. Confirmation of the presence of flavonoid compounds was carried out using UV spectroscopy. A comparative analysis of the content of flavonoids in liquid dosage forms based on calendula officinalis was carried out.Results. As a result, liquid dosage forms were obtained from calendula officinalis flowers by two different methods, using different formulations, extraction was carried out by maceration and circulating extraction in a Soxlet apparatus, in ratios of 1:5 and 1:10, different concentrations of ethyl alcohol were also used (40%, 70%, 96%). Optimal extraction conditions were determined – for this raw material, the best indicators were achieved when obtaining the dosage form using the Soxlet extractor, in addition, according to the experiment, the concentration of ethyl alcohol, which extracts more target components, is 70%, the most effective ratio is 1:5.Conclusion. The study examined changes in the glycosidic (flavonoid) composition in dosage forms prepared independently according to various recipes and drugs obtained in pharmaceutical production. The use of flavonoid extraction methods provides a great opportunity for further scientific research into the extraction of dietary supplements for the purpose of their production.

Geniposide ameliorates atherosclerosis by restoring lipophagy via suppressing PARP1/PI3K/AKT signaling pathway

BackgroundAtherosclerosis (AS) is the leading cause of global death, which manifests as arterial lipid stack and plaque formation. Geniposide is an iridoid glycoside extract from Gardenia jasminoides J.Ellis that ameliorates AS by mediating autophagy. However, how Geniposide regulates autophagy and treats AS remains unclear. PurposeTo evaluate the efficacy and mechanism of Geniposide in treating AS.Study design and methods: Geniposide was administered to high-fat diet-fed ApoE−/− mice and oxidized low-density lipoprotein-incubated primary vascular smooth muscle cells (VSMCs). AS was evaluated with arterial lipid stack, plaque progression, and collagen loss in the artery. Foam cell formation was detected by lipid accumulation, inflammation, apoptosis, and the expression of foam cell markers. The mechanism of Geniposide in treating AS was assessed using network pharmacology. Lipophagy was measured by lysosomal activity, expression of lipophagy markers, and the co-localization of lipids and lipophagy markers. The effects of lipophagy were blocked using Chloroquine. The role of PARP1 was assessed by Olaparib (a PARP1 inhibitor) intervention and PARP1 overexpression. ResultsIn vivo, Geniposide reversed high-fat diet-induced hyperlipidemia, plaque progression, and inflammation. In vitro, Geniposide inhibited VSMC-derived foam cell formation by suppressing lipid stack, apoptosis, and the expressions of foam cell markers. Network pharmacological analysis and in vitro validation suggested that Geniposide treated AS by enhancing lipophagy via suppressing the PI3K/AKT signaling pathway. The benefits of Geniposide in alleviating AS were offset by Chloroquine in vivo and in vitro. Inhibiting PARP1 using Olaparib promoted lipophagy and alleviated AS progression, while PARP1 overexpression exacerbated foam cell formation and lipophagy blockage. The above effects of PARP1 were weakened by PI3K inhibitor LY294002. PARP1 also inhibited the combination of the ABCG1 and PLIN1. ConclusionGeniposide alleviated AS by restoring PARP1/PI3K/AKT signaling pathway-suppressed lipophagy. This study is the first to present the lipophagy-inducing effect of Geniposide and the binding of ABCG1 and PLIN1 inhibited by PARP1.

Total iridoid glycoside extract of Lamiophlomis rotata (Benth) Kudo accelerates diabetic wound healing by the NRF2/COX2 axis

BackgroundLamiophlomis rotata (Benth.) Kudo (L. rotata), the oral Traditional Tibetan herbal medicine, is adopted for treating knife and gun wounds for a long time. As previously demonstrated, total iridoid glycoside extract of L. rotata (IGLR) induced polarization of M2 macrophage to speed up wound healing. In diabetic wounds, high levels inflammatory and chemotactic factors are usually related to high reactive oxygen species (ROS) levels. As a ROS target gene, nuclear factor erythroid 2-related factor 2 (NRF2), influences the differentiation of monocytes to M1/M2 macrophages. Fortunately, iridoid glycosides are naturally occurring active compounds that can be used as the oxygen radical scavenger. Nevertheless, the influence of IGLR in diabetic wound healing and its associated mechanism is largely unclear.Materials and methodsWith macrophages and dermal fibroblasts in vitro, as well as a thickness excision model of db/db mouse in vivo, the role of IGLR in diabetic woundhealing and the probable mechanism of the action were investigated.ResultsOur results showed that IGLR suppressed oxidative distress and inflammation partly through the NRF2/cyclooxygenase2 (COX2) signaling pathway in vitro. The intercellular communication between macrophages and dermal fibroblasts was investigated by the conditioned medium (CM) of IGLR treatment cells. The CM increased the transcription and translation of collagen I (COL1A1) and alpha smooth muscle actin (α-SMA) within fibroblasts. With diabetic wound mice, the data demonstrated IGLR activated the NRF2/KEAP1 signaling and the downstream targets of the pathway, inhibited COX2/PEG2 signaling and decreased the interaction inflammatory targets of the axis, like interleukin-1beta (IL-1β), interleukin 6 (IL-6), apoptosis-associated speck-like protein (ASC), cysteinyl aspartate specific proteinase1 (caspase1) and NOD-like receptor-containing protein 3 (NLRP3).In addition, the deposition of COL1A1, and the level of α-SMA, and Transforming growth factor-β1 (TGF-β1) obviously elevated, whereas that of pro-inflammatory factors reduced in the diabetic wound tissue with IGLR treatment.ConclusionIGLR suppressed oxidative distress and inflammation mainly through NRF2/COX2 axis, thus promoting paracrine and accelerating wound healing in diabetes mice.Graphical

Fabrication of a bio-based polymer adsorbent and its application for extraction and determination of glycosides from Huangqi Liuyi Decoction

Huangqi Liuyi Decoction, a famous classical Chinese prescription, shows significant curative effect on diabetes and its complications, in which calycosin-7-glucoside, liquiritin and glycyrrhizic acid are the main components that playing these mentioned pharmacological activity, under the synergistic action of various other ingredients in the decoction. However, there are significant differences in the content of active compounds in Chinese medicinal materials, which mainly due to origin, picking seasons, and processing methods. Hence, the accurate content of the glycosides is the prerequisite for ensuring the pharmacological efficacy. Aiming at establishing an efficient extraction and determination method for accurate quantitative analysis of calycosin-7-glucoside, liquiritin and glycyrrhizic acid in Huangqi Liuyi Decoction, an on line solid-phase extraction-high-performance liquid chromatography method was developed, using a homemade bio-based monolithic adsorbent. The bio-based adsorbent was prepared in a stainless steel tube, using bio-monomers of methyleugenol and S-allyl-L-cysteine, which effectively reduced the dependence of the polymer field on non-renewable fossil resources and reduced carbon emissions. Furthermore, the prepared adsorbent owned abundant chemical groups, which can produce interactions of hydrogen bond, dipole-dipole, π-π and hydrophobic force with the target glycosides, thus improving the specific recognition ability of the adsorbent. The experiments were carried out on an LC-3000 HPLC instrument with a six-way valve. Methodology validation indicates that the recovery is in the range of 97.0%-103.4% with the RSD in the range of 1.6%-4.0%, due to the specific selectivity of the bio-based monolithic adsorbent for these three glycosides, and good matrix-removal ability for Huangqi Liuyi decoction. The limit of detection is 0.17, 0.50 and 0.33μg/mL for calycosin-7-glucoside, liquiritin and glycyrrhizic acid, respectively, and the limit of quantitation is 0.50, 1.50 and 1.00μg/mL, respectively, with the linear range of 2-200μg/mL for calycosin-7-glucoside, and 5-500μg/mL for liquiritin and glycyrrhizic acid. The present work provided a simple and efficient method for the extraction and determination of glycosides in complex medicinal plants.

HPLC-UV Analysis of Flavonoid Glycosides in the Herb of <i>Astragalus</i> (<i>A. dasyanthus</i>, <i>A. varius</i>, <i>A. testiculatus</i>, <i>A. henningii</i>), Growing in the Volga Region

Introduction. The search for new promising sources of biologically active substances is one of the tasks of modern pharmacognosy. Among the huge variety of species of the genus Astragalus L., only a few of them have been studied. In addition, none of them is included in the current edition of the State Pharmacopoeia of the Russian Federation. In our opinion, the study of four species of this genus of Astragalus L. (A. dasyanthus, A. varius, A. testiculatus, A. henningii) growing in the Volga region is of interest.Aim. Study of the glycoside composition of flavonoids in the astragalus herb of four species (A. dasyanthus, A. varius, A. testiculatus, A. henningii) by HPLC-UV using external standards.Materials and methods. The material was samples of astragalus grass (A. dasyanthus, A. varius, A. testiculatus, A. henningii), collected on the territory of the Saratov region in accordance with the basic rules of collection and preparation and dried to an air-dry state. Aqueous-alcoholic extracts (1 : 50) were analyzed. Qualitative and quantitative analysis of flavonoid glycosides was carried out on an Agilent 1260 chromatograph (Agilent Technologies, USA) equipped with a diode array detector, manual sample injection (Agilent G1328C manual injector, Agilent Technologies USA) and an Agilent Open Lab CDS system for collecting and processing chromatographic data. The elution gradient was selected individually using 0.1 % phosphoric acid/acetonitrile solution as solvents. Compounds were identified by retention times and UV spectra of reference standards (RS). The quantitative content of each detected component was expressed in mg/g of dry raw material. All studies were repeated five times, the results were statistically processed using MS Exсel 2010.Results and discussion. The chromatographic profiles of aqueous-alcoholic extracts from the herbs of four types of astragalus were studied. Differences were found in both the qualitative composition and quantitative content of flavonoid glycosides in the grass of the analyzed species. The largest number of compounds was found in the herb of A. varius (6 compounds), 4 compounds were identified in the herb of A. dasyanthus and A. henningii, and 3 compounds were identified in the herb of A. testiculatus. The dominant components in the herb of A. henningii are orientin and rutin, in the herb of A. testiculatus and A. varius it is cynaroside, and in A. dasyanthus it is rutin.Conclusion. A HPLC-UV method was developed for determining the quantitative content of flavonoid glycosides in extracts from the herbs of four species of astragalus (A. dasyanthus, A. varius, A. testiculatus, A. henningii) and the chromatographic profiles of the analyzed samples were studied.

Transcriptomic and proteomic investigation of the ameliorative effect of total polyphenolic glycoside extract on hepatic fibrosis in Lamiophlomis rotata Kudo via the AGE/RAGE pathway

Ethnopharmacological relevanceDuring the regression of liver fibrosis, a decrease in hepatic stellate cells (HSCs) can occur through apoptosis or inactivation of activated HSCs (aHSCs). A new approach for antifibrotic therapy involves transforming hepatic myofibroblasts into a quiescent-like state. Lamiophlomis rotata (Benth.) Kudo (L. rotata), an orally available Tibetan herb, has traditionally been used to treat skin disease, jaundice, and rheumatism. In our previous study, we found that the total polyphenolic glycoside extract of L. rotata (TPLR) promotes apoptosis in aHSCs for the treatment of hepatic fibrosis. However, whether TPLR induces aHSCs to become inactivated HSCs (iHSCs) is unclear, and the underlying mechanism remains largely unknown. PurposeThis study aimed to examine the impact of TPLR on the phenotypes of hepatic stellate cells (HSCs) during the regression of liver fibrosis and explore the potential mechanism of action. MethodsThe effect of TPLR on the phenotypes of hepatic stellate cells (HSCs) was assessed using immunofluorescence (IF) staining, reverse transcription-polymerase chain reaction (RT–PCR), and Western blotting. Transcriptomic and proteomic methods were employed to identify the main signaling pathways involved. Based on the omics results, the likely mechanism of TPLR on the phenotypes of aHSCs was confirmed through overexpression and knockdown experiments in TGF-β1-activated LX-2 cells. Using a CCl4-induced liver fibrosis mouse model, we evaluated the anti-hepatic fibrosis effect of TPLR and explored its potential mechanism based on omics findings. ResultsTPLR was found to induce the differentiation of aHSCs into iHSCs by significantly decreasing the protein expression of α-SMA and Desmin. Transcriptomic and proteomic analyses revealed that the AGE/RAGE signaling pathway plays a crucial role in the morphological transformation of HSCs following TPLR treatment. In vitro experiments using RAGE overexpression and knockdown demonstrated that the mechanism by which TPLR affects the phenotype of HSCs is closely associated with the RAGE/RAS/MAPK/NF-κB axis. In a model of liver fibrosis, TPLR obviously inhibited the generation of AGEs and alleviated liver tissue damage and fibrosis by downregulating RAGE and its downstream targets. ConclusionThe AGE/RAGE axis plays a pivotal role in the transformation of activated hepatic stellate cells (aHSCs) into inactivated hepatic stellate cells (iHSCs) following TPLR treatment, indicating the potential of TPLR as a therapeutic agent for the management of liver fibrosis.

Optimizing the Ultrasound-Assisted Extraction of Total Cardiac Glycosides from the Milk of Calotropis Gigantea with Response Surface Methodology

Optimizing the Ultrasound-Assisted Extraction of Total Cardiac Glycosides from the Milk of Calotropis Gigantea with Response Surface Methodology

DETERMINATION OPTIMAL CONDITIONS OF EXTRACTION OF SUM OF TRITERPENE GLYCOSIDES FROM FATSIA JAPONICA

Thus, as a result of the conducted studies, the optimal mode of extraction of total triterpene glycosides from the leaves of Fatsia japonica (Thunb.) Dacne et Planch., cultivated in Georgia, has been established: extraction of triterpene glycosides from raw materials should be done with 80% ethyl alcohol for 2 hours, temperature regime 75-80° С, at the ratio of solid/liquid phases (1:5), the size of the raw material particles is 0.5-7.0 mm.

The phytoestrogenic potential of flavonoid glycosides from Selaginella moellendorffii via ERα-dependent signaling pathway.

Selaginella moellendorffii (SM) has been applied as an ethnic drug to treat conditions such as osteoporosis, idiopathic thrombocytopenic purpura, and chronic inflammation. It is known to be rich in flavonoids, including apigenin glycosides and unique elements of bioflavonoids. To investigate estrogen-like constituents of SM and the possible mechanism. We identified the main components in liquid chromatography and liquid chromatography-mass spectrometry. The estrogenic effects were examined using a recombinant yeast screening assay, an E-screen cell proliferation assay, and an in vivo uterotrophic assay. Flavonoid glycosides extract, some flavonoid glycosides, and apigenin showed estrogen agonistic activity in the yeast screening assay. They also induced cell proliferation in estrogen receptor-positive (ER+) cells but not in estrogen receptor-negative (ER-) cells. Consistently, the protein expression of ERα, phosphorylation protein kinase B (p-AKT), phosphatidylinositol 3 kinase (PI3K), phosphorylation mammalian target of rapamycin (p-mTOR), phosphorylation 38,000-Da protein (p-P38), and phosphorylation extracellular-regulated kinase 1/2 (p-ERK1/2) elevated following treatment with flavonoid glycoside extract (P<0.01 or P<0.05). These effects could be blocked by ER antagonist or ERα antagonist but not be blocked by ERβ antagonist. In vivo assay, flavonoid glycoside extract could significantly increase body weight, serum estradiol level, uterine wet weight, alter uterine morphology, and promote ERα protein expression (P<0.01 or P<0.05). ERα induction via mitogen-activated protein kinases (MAPK) and PI3K/Akt/mTOR pathways might be the possible mechanism underlying the phytoestrogen effect of SM, and the flavonoid glycosides might be the critical estrogenic constituents.

In Vivo Evaluation Of Antioxidant Activity Of Flavonoid Glycoside Extract FromTamarillo (Solanum betaceum Cav)

The tamarillo fruit is thought to have strong antioxidant properties and includes vitamins and other nutrients vital to human health. A randomized posttest-only control group design was used in the experimental trial, which tested 24 Wistar rats. After ethanol and flavonoid glycoside extract was administered, Cu-ZnSOD expression was dramatically increased, and the MDA concentration was markedly decreased. Rats with the highest levels of physical activity received an oral dose of a flavonoid glycoside extract, boosted Cu, ZnSOD expression, and lowered MDA levels in the liver tissue. The findings showed that flavonoid glycoside extract’s antioxidants could maintain Cu, ZnSOD levels in the rat liver with maximum physical activity. According to the findings of this study, it can be said that in contrast to CuZnSOD expression and MDA content in Wistar rat liver tissue that did not receive flavonoid glycoside extract, flavonoid glycoside extract from tamarillo was much more able to increase CuZnSOD expression and decrease MDA content.

The total iridoid glycoside extract of Lamiophlomis rotata Kudo induces M2 macrophage polarization to accelerate wound healing by RAS/ p38 MAPK/NF-κB pathway.

Lamiophlomis rotata (Benth.) Kudo (L. rotata), a Tibetan medicinal plant, is used to treat "yellow-water diseases", such as skin disease, jaundice and rheumatism. Our previous study showed that the iridoid glycoside extract of L. rotata (IGLR) is the major constituent of skin wound healing. However, the role of IGLR in the biological process of trauma repair and the probable mechanism of the action remain largely unknown. To investigate the role of IGLR in the biological process of trauma repair and the probable mechanism of the action. The role of IGLR in wound healing was investigated by overall skin wound in mice with Hematoxylin and Eosin (H&E) and Masson trichrome staining. The anti-inflammatory, angiogenesis-promoting and fibril formation effects of IGLR were visualized in wound skin tissue by immunofluorescence staining, and the proinflammatory factors and growth factors were assayed by real-time polymerase chain reaction (RT-PCR) and enzyme-linked immunosorbent assay (ELISA). Macrophages, dermal fibroblasts, and endothelial cells were cultured to measure the direct/indirect interaction effects of IGLR on the proliferation and migration of cells, and flow cytometry was employed to assess the role of IGLR on macrophage phenotype. Network pharmacology combined with Western blot experiments were conducted to explore possible mechanisms of the actions. IGLR increased the expression of CD206 (M2 markers) through the RAS/p38 MAPK/NF-κB signaling pathway during wound injury in vivo and in vitro. IGLR suppressed the inflammatory cytokines iNOS, IL-1β and TNF-α in the early stage of wound healing. During the proliferation step of wound repair, IGLR promoted angiogenesis and fibril formation by increasing the expression of VEGF, CD31, TGF-β and α-SMA in wound tissue, and similar results were verified by RT-PCR and ELISA. In a paracrine mechanism, the extract promoted the proliferation of dermal fibroblasts, and endothelial cells were founded by the conditioned medium (CM). IGLR induced M2 macrophage polarization in the early stage of wound healing; in turn, IGLR played a key role in the transition from inflammation to cell proliferation during the biological process of wound healing.