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• Clerodendrum glandulosum (CG) species have not been explored for diabetic wound healing. • This species is rich in phenylethanoid glycosides (PhGs), a subclass of polyphenols. • Verbascoside, isoverbascoside, martynoside, and isomartynoside are the four PhGs. • This study explores the diabetic wound healing property of the PhGs in CG by in-silico approaches. The diabetic wound is one of the severe complications of diabetes mellitus, accounting for 20 % of limb amputations in diabetic patients. This creates a need to search for newer natural compounds to target the different molecular pathways of diabetic wounds to accelerate the repair. The phenylethanoid glycosides (PhGs) isolated from Clerodendrum glandulosum (CG) have been shown to exhibit antioxidant, antimicrobial, and anti-inflammatory properties but have never been explored for diabetic wound healing. Thus, this study focuses on exploring the diabetic wound-repairing properties of PhGs through in-silico approaches. The PhGs present in CG were identified through extensive literature searching, which were further subjected to database searching in BindingDB, TargetNet, PharmMapper, Super-PRED, and Swiss Target Prediction to find the potential targets, which included PRKCA, PRKCG, PRKCZ, TDP1, and Pol. Subsequently, these targets were used to determine the disease IDs related to diabetic wounds from databases such as DisGeNET, Gene Expression Omnibus, GeneCards, and OMIM. A network was established using Cytoscape to study the relationship among the PhGs, the protein targets, and their associated disease IDs. The top twenty molecular pathways associated with the target proteins were determined using the ShinyGO database. Genetic enrichment analysis showed that the Sphingolipid signalling pathway included the maximum number of genes and had the lowest false discovery rate value, which concluded that this pathway is the potential target of the PhGs. PRKCA and PRKCZ were found to be the only two genes involved in this pathway, and thus, molecular docking was used to evaluate the binding affinity of the PhGs with the proteins. Docking scores were between -13.2859 and -5.10928, suggesting a strong molecular interaction between the PhGs and their targets. Thus, it is concluded that PhGs present in CG can be the potential compounds to treat diabetic wounds; however, further in-vitro and in-vivo investigations are necessary. [ABSTRACT FROM AUTHOR]

Phenylethanoid glycosides (PhGs) exhibit a multitude of structural variations linked to diverse pharmacological activities. Assembling various PhGs via multienzyme cascades represents a concise strategy over traditional synthetic methods. However, the challenge lies in identifying a comprehensive set of catalytic enzymes. This study explores biosynthetic PhG reconstruction from natural precursors, aiming to replicate and amplify their structural diversity. We discovered 12 catalytic enzymes, including four novel 6′‐OH glycosyltransferases and three new polyphenol oxidases, revealing the intricate network in PhG biosynthesis. Subsequently, the crystal structure of CmGT3 (2.62 Å) was obtained, guiding the identification of conserved residue 144# as a critical determinant for sugar donor specificity. Engineering this residue in PhG glycosyltransferases (FsGT61, CmGT3, and FsGT6) altered their sugar donor recognition. Finally, a one‐pot multienzyme cascade was established, where the combined action of glycosyltransferases and acyltransferases boosted conversion rates by up to 12.6‐fold. This cascade facilitated the reconstruction of 26 PhGs with conversion rates ranging from 5–100 %, and 20 additional PhGs detectable by mass spectrometry. PhGs with extra glycosyl and hydroxyl modules demonstrated notable liver cell protection. This work not only provides catalytic tools for PhG biosynthesis, but also serves as a proof‐of‐concept for cell‐free enzymatic construction of diverse natural products. [ABSTRACT FROM AUTHOR]

Quality control and clarifying ingredients are the foundation of pharmacodynamic material basis research. Pedicularis decora Franch. (P. decora) is clinically used to treat Alzheimer's disease and exerts significant antioxidative, anti-inflammatory and neuroprotective effects. However, there is little systematic research on the extraction and composition and the current research on P. decora focused on the quality control and extraction with aucubin as only quality marker. It reported that Iridoid glycosides (IGs) and phenylpropanoid glycosides (PeGs), which are characteristic components of the Pedicularis species, have been reported to have various anti-Alzheimer's activity. This study focused on the extraction and rapid qualitative analysis of IGs and PeGs in P. decora. First, HPLC-UV method was established to detect five IGs and PeGs analytes simultaneously and assess the effect of the extraction technology. Then, the G1-entropy method with the Box-Behnken response surface design methodology was used to optimized extraction technology. The optimum conditions were determined to be reflux with 55% methanol aqueous solutions, at 75 °C for 50 min. Finally, by establishing UPLC-Q/TOF-MS, 15 IGs and 15 PeGs in P. decora were rapidly identified and characterized for the first time. The results will provide a reverence of a higher quality standard and the pharmacodynamic material basis research. [ABSTRACT FROM AUTHOR]

Copyright of Food & Fermentation Industries is the property of Food & Fermentation Industries and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Teucrium chamaedrys L. is a typical European–Mediterranean species of the genus Teucrium. Among the phenolic compounds belonging to phenylethanoid glycosides (PGs), teucrioside (TS) is only found in this species, and it was previously demonstrated to be produced by in vitro-elicited cell cultures at levels higher than those found in leaves. However, T. chamaedrys cell suspension extracts (Cell-Ex) and pure TS have not been investigated yet for any biological effects. In this study, we evaluated the antioxidant and anti-melanogenesis activity of both Cell-Ex and TS in B16-F10 mouse melanoma cells. The results showed that Cell-Ex inhibited the reactive oxygen species formation evoked in B16-F10 cells by tert-butyl hydroperoxide and 5 J/cm2 of UVA, as well as the melanin increase stimulated by α-MSH or 20 J/cm2 of UVA. In parallel, a TS concentration equivalent to that present in Cell-Ex recorded the same biological effect profile, suggesting the main contribution of TS to the antioxidant and anti-melanogenic properties of Cell-Ex. Both Cell-Ex and TS also modulated the melanogenesis pathway through their ability to inhibit the tyrosinase activity both in a cell-free system and in B16-F10 cells stimulated by α-MSH. These results support the potential cosmeceutical use of Cell-Ex for protection against photooxidative damage and hyperpigmentation. [ABSTRACT FROM AUTHOR]

In this study, spray drying was used as a technological solution for the valorization of Teucrium montanum extract into carboxymethyl cellulose-based delivery systems (CMC), individually or in combination with collagen, guar gum, gum arabic, and kappa-carrageenan. The results showed that the process yield and morphological properties were positively influenced by the introduction of CMC binary blends. The employment of CMC resulted in a high encapsulation efficiency (77–96%) for all phenylethanoid glycosides (PGs) analyzed. Due to the low wettability of the microparticles, a relatively gradual in vitro release of the PGs was achieved. Infusion of the filling with hydrophilic T. montanum extract encapsulated in microparticles with high hydrophobic surface area proved to be a practical route for significant confectionery fortification (5–9 mg PGs per dw serving), ensuring prolonged interaction between the food matrix used and the extract under simulated gastrointestinal conditions. Based on sensory evaluation, the introduction of kudzu starch into the jelly matrix has shown a texture-modifying potential. [ABSTRACT FROM AUTHOR]

Stachys scardica Griseb. is a Balkan endemic species listed in The Red Data Book of Bulgaria with the conservation status "endangered". Successful micropropagation was achieved on MS medium supplemented with 1.5 mg/L benzyladenine (BA), followed by a subsequent ex vitro adaptation in an experimental field resulting in 92% regenerated plants. Using nuclear magnetic resonance (NMR), phenylethanoid glycosides (verbascoside, leucosceptoside A), phenolic acids (chlorogenic acid), iridoids (allobetonicoside and 8-OAc-harpagide), and alkaloids (trigonelline) were identified, characteristic of plants belonging to the genus Stachys. High antioxidant and radical scavenging activities were observed in both in situ and ex vitro acclimated S. scardica plants, correlating with the reported high concentrations of total phenols and flavonoids in these variants. Ex vitro adapted plants also exhibited a well-defined anti-inflammatory potential, demonstrating high inhibitory activity against the complement system. Employing a disk diffusion method, a 100% inhibition effect was achieved compared to positive antibiotic controls against Staphylococcus epidermidis and Propionibacterium acnes, with moderate activity against Bacillus cereus. The induced in vitro and ex vitro model systems can enable the conservation of S. scardica in nature and offer future opportunities for the targeted biosynthesis of valuable secondary metabolites, with potential applications in the pharmaceutical and cosmetic industries. [ABSTRACT FROM AUTHOR]

Health-oriented preferences, a demand for innovative food concepts, and technological advances have greatly influenced changes in the food industry and led to remarkable development of the functional food market. Incorporating herbal extracts as a rich source of bioactive compounds (BC) could be an effective solution to meet the high demand of consumers in terms of expanding the high-quality range of functional foods. The aim of this study is the valorization of the bioactive potential of T. montanum L., an understudied Mediterranean plant species, and the in-depth elucidation of a polyphenolic profile with a UHPLC-HR MS/MS and NMR analysis. The total phenolic content (TPC) and antioxidant capacity (AC) were determined on heat-assisted (HAE), microwave-assisted (MAE) and subcritical water (SWE) extracts. In terms of antioxidant capacity, SWE extracts showed the most notable potential (ABTS: 0.402–0.547 mmol eq Trolox g−1 dw, DPPH: 0.336–0.427 mmol eq Trolox g−1 dw). 12 phenolic compounds were identified in the samples of T. montanum from six microlocations in Croatia, including nine phenylethanoid glycosides (PGs) with total yields of 30.36–68.06 mg g−1 dw and 25.88–58.88 mg g−1 dw in HAE and MAE extracts, respectively. Echinacoside, teupolioside, stachysoside A, and poliumoside were the most abundant compounds HAE and MAE extracts, making T. montanum an emerging source of PGs. [ABSTRACT FROM AUTHOR]

Cymbaria daurica L. is a well-known traditional Mongolian medicine, which has been used to treat diabetes-related conditions characterized by persistent thirst and hunger, copious urination, and weight loss. We aimed to investigate the protective effects of C. daurica extracts and phenylethanoid glycosides including verbascoside and isoacteoside on INS-1 cells. We discovered phenylethanoid glycosides from n-butanol extract with large content through extraction and separation. We continue to study the protective effects of phenylethanoid glycosides including verbascoside and isoacteoside on INS-1 cells. INS-1 cells were treated with C. daurica, cell viability assay, RNA-seq technology, superoxide dismutase activity and malonaldehyde content, quantitative real time-PCR and Western blot analysis were used to study the protective effects of C. daurica. Cell viability assay resulted that n-butanol extract and verbascoside, isoacteoside showed protective effects of C. daurica. According to the RNA-seq technology to identify the differentially expressed genes in INS-1 cells, the pathway of gene enrich the protective effect of C. daurica on oxidative stress. SOD activity and the content of MDA indicated that C. daurica could enhance the antioxidant capacity of INS-1 cells. Further investigation indicated C. daurica alleviate oxidative stress by inhibiting INS-1 cell apoptosis. C. daurica may play an anti-diabetic role by inhibiting islet cell apoptosis.

Introduction: Alzheimer's disease (AD) is a major public health concern worldwide, but there are still no drugs available that treat it effectively. Previous studies have shown that phenylethanoid glycosides have pharmacological effects, which include anti-AD properties, but the underlying mechanisms by which they ameliorate AD symptoms remain unknown. Methods: In this study, we used an APP/PS1 AD mouse model to explore the function and mechanisms underlying savatiside A (SA) and torenoside B (TB) in the treatment of AD. SA or TB (100 mg·kg-1·d-1) was orally administered to 7-month-old APP/PS1 mice for 4 weeks. Cognitive and memory functions were measured using behavioral experiments (including the Morris water maze test and the Y-maze spontaneous alternation test). Molecular biology experiments (including Western blotting, immunofluorescence, and enzyme-linked immunosorbent assays) were used to detect any corresponding changes in signaling pathways. Results: The results showed that SA or TB treatment could significantly reduce cognitive impairment in APP/PS1 mice. We also showed that chronic treatment with SA/TB could prevent spine loss, synaptophysin immunoreactivity, and neuronal loss in mice, thereby improving synaptic plasticity and moderating learning and memory deficits. SA/TB administration also promoted the expression of synaptic proteins in APP/PS1 mouse brains and upregulated phosphorylation of proteins in the cyclic adenosine monophosphate (cAMP)/CREB/brain-derived neurotrophic growth factor (BDNF) pathway that are responsible for synaptic plasticity. Additionally, chronic SA/TB treatment increased the levels of BDNF and nerve growth factor (NGF) in the brains of APP/PS1 mice. Both astrocyte and microglia volumes, as well as the generation of amyloid β, were also decreased in SA/TB-treated APP/PS1 mice compared to control APP/PS1 mice. Conclusion: In summary, SA/TB treatment was associated with activation of the cAMP/CREB/BDNF pathway and increased BDNF and NGF expression, indicating that SA/TB improves cognitive functioning via nerve regeneration. SA/TB is a promising candidate drug for the treatment of AD. [ABSTRACT FROM AUTHOR]

Since the advent of Covid-19, several natural products have been investigated regarding their in silico interactions with SARS-CoV-2 proteases ˗ 3CLpro and PLpro, two of the most important pharmacological targets for antiviral development. Phenylethanoid glycosides (PG) are a class of natural products present in important medicinal plants and a drug containing this group of active ingredients has been successfully used in the treatment of Covid-19 in China. Thus, a dataset with 567 derivatives of this class was built from reviews published between 1994 and 2020, and their interaction against both SARS-CoV-2 proteases was investigated. The virtual screening was performed by filtering the PGs through the evaluation of scores based on the AutoDock Vina, GOLD/ChemPLP, and GOLD/GoldScore evaluation functions. The bRO5 pharmacokinetic parameters of the PGs ranked in the previous step were analyzed and their interaction with key amino acid residues of the 3CLpro and PLpro enzymes was evaluated. Ninety-eight compounds were identified by computational approaches against PLpro and 80 PGs against 3CLpro. Of these, four interacted with key catalytic residues of PLpro, which is an indicative of inhibitory activity, and three compounds interacted with catalytic key residues of 3CLpro. Of these, five PGs occur in plants of the Traditional Chinese Medicine (TCM), while two are components of plants/formulations currently used in the Covid-19 protocols in China. The data presented here show the potential of PGs as selective inhibitors of SARS-CoV-2 3CLpro and PLpro.

Teucrium chamaedrys L. is a typical European–Mediterranean species of the genus Teucrium. Among the phenolic compounds belonging to phenylethanoid glycosides (PGs), teucrioside (TS) is only found in this species, and it was previously demonstrated to be produced by in vitro-elicited cell cultures at levels higher than those found in leaves. However, T. chamaedrys cell suspension extracts (Cell-Ex) and pure TS have not been investigated yet for any biological effects. In this study, we evaluated the antioxidant and anti-melanogenesis activity of both Cell-Ex and TS in B16-F10 mouse melanoma cells. The results showed that Cell-Ex inhibited the reactive oxygen species formation evoked in B16-F10 cells by tert-butyl hydroperoxide and 5 J/cm2 of UVA, as well as the melanin increase stimulated by α-MSH or 20 J/cm2 of UVA. In parallel, a TS concentration equivalent to that present in Cell-Ex recorded the same biological effect profile, suggesting the main contribution of TS to the antioxidant and anti-melanogenic properties of Cell-Ex. Both Cell-Ex and TS also modulated the melanogenesis pathway through their ability to inhibit the tyrosinase activity both in a cell-free system and in B16-F10 cells stimulated by α-MSH. These results support the potential cosmeceutical use of Cell-Ex for protection against photooxidative damage and hyperpigmentation.

In this study, spray drying was used as a technological solution for the valorization of Teucrium montanum extract into carboxymethyl cellulose-based delivery systems (CMC), individually or in combination with collagen, guar gum, gum arabic, and kappa-carrageenan. The results showed that the process yield and morphological properties were positively influenced by the introduction of CMC binary blends. The employment of CMC resulted in a high encapsulation efficiency (77–96%) for all phenylethanoid glycosides (PGs) analyzed. Due to the low wettability of the microparticles, a relatively gradual in vitro release of the PGs was achieved. Infusion of the filling with hydrophilic T. montanum extract encapsulated in microparticles with high hydrophobic surface area proved to be a practical route for significant confectionery fortification (5–9 mg PGs per dw serving), ensuring prolonged interaction between the food matrix used and the extract under simulated gastrointestinal conditions. Based on sensory evaluation, the introduction of kudzu starch into the jelly matrix has shown a texture-modifying potential.

(1) Background: The aim of the study was to compare the potency of Plantago media L. (Plantaginaceae) extracts on Acanthamoeba sp. trophozoites, which are opportunistic protozoan parasites leading to several dangerous diseases; (2) Methods: The chromatographically (TLC, HPLC-DAD) characterized water fractions of the extracts from biomass from in vitro cultures (shoots and roots), leaves, and inflorescences from field cultivation were used for the study of the acanthamoebic activity in a Thoma haemocytometer chamber; (3) Results: The anti-amoebic effect at the lowest concentration (1.0 mg/mL) was demonstrated only by the extract of the leaves from the cultivation (50.50% inhibition). The remaining samples inhibited the growth of parasites from a concentration of 5.0 mg/mL in the range of 41.36% inflorescences to 63.89% shoots in vitro. Quantitative determinations of phenolic compounds in the tested extracts indicate a tendency to increase the potency of the anti-amoebic effect with the content of a phenylethanoid glycoside—acteoside. The maximum content of this compound was determined in leaves from field cultivation (6.64%) and the minimum in inflorescences (0.65%). This is confirmed by the range of the lowest IC50 values (the strongest biological activity) for the tested samples, 0.95–1.80 mg/mL for leaves from cultivation, and the high values, 9.70–5.30 mg/mL for inflorescences and in-vitro-derived roots. The strength of the biological activity of the extracts correlated with the content of acteoside, which constituted 84–93% of the sum of phenolic compounds determined; (4) Conclusions: The performed investigations proved the anti-acanthamoebic efficacy of Plantago media organs, including those obtainable by biotechnological methods, and indicated phenylethanoid glycosides, their main phenolic constituents, to be responsible for the activity. To our knowledge, this is the first report on the amoebicidal activity of Plantago media extracts from biomass produced by biotechnological methods and organs of an intact plant. [ABSTRACT FROM AUTHOR]

Five new phenylethanoid glycosides integerrima A-E (1-5) were isolated from the stem of Callicarpa integerrima for the first time. Their structures were elucidated by extensive spectroscopic analyses. In addition, cytotoxicity, anti-adipogenic and antioxidant activities were evaluated. All the phenylethanoid glycosides would be nontoxic to the normal human hepatocytes LO-2 and pre-adipocytes 3T3-L1 cell lines, significantly promote the proliferation of normal hepatocytes, thus displaying the potential for hepatoprotective. Integerrima A (1), C (3) and D (4) exhibited selectively moderate cytotoxic activity against the hepatoma cell lines Bel-7402, with the IC50 value at 72.66, 80.43 and 84.88 μmol/L, respectively. Moreover, integerrima D (4) had significant activities on reducing lipid droplet formation, with the inhibition rate of 48.02% on the concentration of 200 μg/mL. Finally, the result of FRAP assays exhibited remarkable antioxidant activity in integerrima E (5), which was close to the positive control ascorbic acid with the concentration of 100 μg/mL. [ABSTRACT FROM AUTHOR]

Objectives This study was aimed to evaluate the protective effects of phenylethanoid glycosides extract from Cistanche deserticola against atherosclerosis and its molecular mechanism. Methods Total phenylethanoid glycosides were extracted and purified from C. deserticola , and the C. deserticola extract (CDE) was used to treat a mice model of atherosclerosis. Key findings CDE containing 81.00% total phenylethanoid glycosides, with the contents of echinacoside and acteoside being 31.36% and 7.23%, respectively. A 13-week of CDE supplementation (1000 mg/kg body weight/day) significantly reduced atherosclerotic lesions in the aortic sinus and entire aorta in ApoE −/− mice fed with a high-fat diet. In addition, varying doses of CDE (250, 500 and 1000 mg/kg body weight/day) lowered plasma total cholesterol, triglyceride and non-high-density lipoprotein cholesterol levels. Transcriptomic analysis of the small intestine revealed the changes enriched in cholesterol metabolic pathway and the activation of Abca1 gene. Further validation using real-time quantitative PCR and western blot confirmed that CDE significantly increased the mRNA levels and protein expressions of ABCA1, LXRα and PPARγ. Conclusions Our results demonstrate the beneficial effects of C. deserticola on atherosclerotic plaques and lipid homeostasis, and it is, at least partially, by activating PPARγ-LXRα-ABCA1 pathway in small intestine. [ABSTRACT FROM AUTHOR]

Three new naphthoquinones, 5,6,7-trimethoxydunnione (1), 6,7-dimethoxy-α-dunnione (2), and 5,6,7-trimethoxydunniol (3) were isolated from the tubers of Sinningia mauroana Chautems, together with eleven known compounds: 5-hydroxy-6,7-dimethoxy-α-dunnione (4), 6-hydroxy-7-methoxy-α-dunnione (5), 7-hydroxy-6-methoxy-α-dunnione (6), cedrol (7), tectoquinone (8), plantainoside A (9), calceolarioside A (10), calceolarioside B (11), sanangoside (12), allo-calceolarioside A (13), and conandroside (14). The known compounds 4, 7–9 and 11–13 are being reported for the first time in this species. Hexane, ethyl acetate and ethanol extracts were tested for antioxidant activity by the ORAC-FL method, and the antioxidant capacity was measured as trolox equivalent (TE). The ethyl acetate (8808 µg TE g−1) and ethanol (7911 µg TE g−1) extracts showed high antioxidant capacity, while the hexane extract displayed weak antioxidant capacity (860 µg TE g−1). [ABSTRACT FROM AUTHOR]

Despite several studies on the Ajuga L. genus, the chemical composition of Ajuga pyramidalis, an alpine endemic species, is still largely unknown. The purpose of this study was to therefore deeper describe it, particularly from the phytochemistry and bioactivity perspectives. In that respect, A. pyramidalis was investigated and 95% of the extracted mass of the plant was characterized by chromatography and mass spectrometry. Apart from the already determined chemical compounds, namely, harpagide and 8-O-acetylharpagide, two iridoids, and neoajugapyrin A, a neo-clerodane diterpene, and three polyphenols (echinacoside, verbascoside and teupoloside) were identified for the first time in A. pyramidalis. Incidentally, the first RX structure of a harpagoside derivative is also described in this paper. The extracts and isolated compounds were then evaluated for various biochemical or biological activities; notably a targeted action on the renewal of the epidermis was highlighted with potential applications in the cosmetic field for anti-aging. [ABSTRACT FROM AUTHOR]

Cistanche deserticola Y. C. Ma (CD), known as “desert ginseng”, has been found to have hepatoprotective effect. This research aimed to investigate the quality control and its alleviating effect on alcoholic liver injury in mice. In this study, for the first time, a sensitive and efficient ultra-high-performance liquid chromatography with quadrupole ion-trap mass spectrometry (UPLC-Q-TRAP/MS) method was developed to rapidly characterize nine representative phenylethanoid glycosides (PhGs) in the CD extract within 14 min, offering a reference for the quality control standard of this plant. In addition, we found that the CD extract significantly inhibited the weight loss, decreased the liver index, and attenuated excessive lipid deposition, inflammatory and oxidative stress in the mice liver. With the help of the high-throughput lipidomics technique, we discovered that CD markedly reversed 17 lipid metabolites and their involved linoleic acid, arachidonic acid and glycerophospholipid metabolic pathways. As these metabolites are mainly associated with lipid metabolism and liver damage, we further used molecular biological tests to found that CD could regulate the upstream genes and proteins of the lipid metabolism pathway, including adenosine 5′-monophosphate-activated protein kinase (AMPK), sterol regulatory element binding protein-1c (SREBP-1c), fatty acid synthase (FAS), and peroxidase proliferators activate receptors α (PPARα). In conclusion, this study elucidates the modulatory effects of CD on lipid metabolism disorders in alcoholic fatty liver from holistic system and provides a reference for further research and development of CD as a therapeutic agent.

Health-oriented preferences, a demand for innovative food concepts, and technological advances have greatly influenced changes in the food industry and led to remarkable development of the functional food market. Incorporating herbal extracts as a rich source of bioactive compounds (BC) could be an effective solution to meet the high demand of consumers in terms of expanding the high-quality range of functional foods. The aim of this study is the valorization of the bioactive potential of T. montanum L., an understudied Mediterranean plant species, and the in-depth elucidation of a polyphenolic profile with a UHPLC-HR MS/MS and NMR analysis. The total phenolic content (TPC) and antioxidant capacity (AC) were determined on heat-assisted (HAE), microwave-assisted (MAE) and subcritical water (SWE) extracts. In terms of antioxidant capacity, SWE extracts showed the most notable potential (ABTS: 0.402–0.547 mmol eq Trolox g−1 dw, DPPH: 0.336–0.427 mmol eq Trolox g−1 dw). 12 phenolic compounds were identified in the samples of T. montanum from six microlocations in Croatia, including nine phenylethanoid glycosides (PGs) with total yields of 30.36–68.06 mg g−1 dw and 25.88–58.88 mg g−1 dw in HAE and MAE extracts, respectively. Echinacoside, teupolioside, stachysoside A, and poliumoside were the most abundant compounds HAE and MAE extracts, making T. montanum an emerging source of PGs.

Three new flavonoid glycosides, Dasuanxinoside F–H (1–3), were isolated from the aerial parts of Allium sativum, together with eight known compounds which were firstly reported in this plant, including three flavonoid glycosides (4–6) and five phenylethanoid glycosides (7–11). Their structures were identified by UV-vis, IR, 1D and 2D NMR spectra, as well as HR-ESI-MS analyses. The inhibitory effect of the isolated compounds on platelet aggregation induced by adenosine diphosphate (ADP) was evaluated in vitro. The results showed that most compounds displayed different degrees of inhibition. Among them, 2, 5, 8 and 9 exhibited the strongest activity on platelet aggregation. [ABSTRACT FROM AUTHOR]

"Desert hyacinths" are a remarkable group of parasitic plants belonging to genus Cistanche, including more than 20 accepted species typically occurring in deserts or coastal dunes parasitizing roots of shrubs. Several Cistanche species have long been a source of traditional herbal medicine or food, being C. deserticola and C. tubulosa the most used in China. This manuscript reports the isolation and identification of some phenylethanoid and iridoid glycosides, obtained from the hydroalcoholic extract of C. phelypaea collected in Spain. The present study aims to characterize the antioxidant activity of C. phelypaea metabolites in the light of their application in nutraceutical and cosmeceutical industries and the effect of acetoside, the most abundant metabolite in C. phelypaea extract, on human keratinocyte and pluripotent stem cell proliferation and differentiation. Our study demonstrated that acetoside, besides its strong antioxidant potential, can preserve the proliferative potential of human basal keratinocytes and the stemness of mesenchymal progenitors necessary for tissue morphogenesis and renewal. Therefore, acetoside can be of practical relevance for the clinical application of human stem cell cultures in tissue engineering and regenerative medicine. [ABSTRACT FROM AUTHOR]

The dried fruits of the plant Forsythia suspensa (Forsythia Fructus: Lianqiao in Chinese) are used in many herbal preparations to treat various diseases or the associated symptoms. Forsythia extracts contain phenylethanoid glycosides (PhGs) such as the forsythosides (Fst A-to-P). The leading products, Fst-A,-B and-F (arenarioside), can be found also in >90 other plants inventoried here. The pharmacological properties of Fst are reviewed, with emphasis on their anticancer, antiviral, and antibacterial activities, which essentially derive from their anti-inflammatory and antioxidant effects. Fst-B functions as a potential binder of the repressor protein Kelch-like ECH-association protein 1 (Keap 1), thus promoting the nuclear translocation of the transcription factor Nuclear factor erythroid 2-related factor 2 (Nrf2) implicated in the subsequent activation of the production of antioxidant enzymes and repression of the oxidative stress. The regulation of the Nrf2/Heme oxygenase-1 pathway is the central piece of the multifaceted mechanism of action of Fst-A/B. Their prominent antioxidant and anti-inflammatory effects support the use of these compounds in different inflammation-related diseases and conditions, from sepsis to neuroprotection and many other pathologies discussed here. In addition, these properties contribute to the antiviral action of the compounds. Fst-A/B displays activities against the influenza A virus and different Fst-containing traditional Chinese medicinal (TCMs) have revealed beneficial effects to combat the current COVID-19 pandemic. The mechanisms whereby Fst-A/B could inhibit viral multiplication are discussed. PhGs likely contribute to the anti-COVID-19 activities reported with several TCM such as Shuang-Huang-Lian oral liquid, Lianhua-Qingwen capsules, and others. This review highlights the pharmacological profile of Fst and illustrates health benefits associated with the use of Forsythia Fructus.

Infertility patients account for an astonishing proportion of individuals worldwide. Due to its complex etiology and challenging treatment, infertility has imposed significant psychological and economic burdens on many patients. C. Herba (Cistanche tubulosa (Schenk) Wight and Cistanche deserticola Ma), renowned as one of the most prominent Chinese herbal medicines (CHMs), is abundant in diverse bioactive compounds that exhibit therapeutic effects on many diseases related to oxidative stress (OS) and disorders of sex hormone levels. Due to the limited drugs currently used in clinical practice to improve reproductive outcomes and their inevitable side effects, developing safe and effective new medications for infertility is of significance. This article comprehensively reviewed the phytochemicals of C. Herba , focusing on their efficacy and mechanisms on infertility and their safety for the first time, aiming to offer valuable insights for the development and application of C. Herba , and for developing novel strategies for treating infertility. We used " Cistanche " and its known bioactive components in combination with "sperm", "testicles", "epididymis", "ovaries", "uterus", and "infertility" as keywords to search in PubMed, Web of Science, Scopus and CNKI up to November 2023. The Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) 2020 guideline was followed. The therapeutic effects of C. Herba on infertility are mainly attributed to echinacoside (ECH), verbascoside (VB), salidroside (SAL), polysaccharides, and betaine. They can effectively improve spermatogenic dysfunction, gonadal dysfunction and erectile dysfunction (ED) by exerting anti-oxidation, sex hormones regulation and anti-hypoxia. Moreover, they can also improve premature ovarian failure (POF), ovarian and uterine cancer, oocyte maturation by exerting anti-oxidation, anti-apoptosis, and anti-cancer. C. Herba and its active ingredients also exhibit pleasing safety. C. Herba is a promising source of natural medicine for infertility. Additionally, compared to current therapeutic drugs, its favorable safety also supports its development as a nutritional supplement. However, high-quality clinical studies are required to validate its effectiveness for the development of novel therapeutic strategies. [ABSTRACT FROM AUTHOR]

Copyright of Xinjiang Agricultural Sciences is the property of Xinjiang Agricultural Sciences Editorial Department and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

For the first time inflorescences of a plant species from the genus Plantago (Pantaginaceae)—Plantago lanceolata L. (Ribwort Plantain), a known medicinal plant, were subjected to studies of phenolic compounds, which resulted in an isolation of two new compounds: a flavonoid—isorhamnetin 3-O-α-L-4C1-arabinopyranosyl-(1→2)-β-D-4C1-glucopyranoside) (1) and a phenylethanoid glycoside—2-(3,4-dihydroxyphenyl)ethyl O-α-L-arabinofuranosyl-(1→2)-[α-L-1C4-rhamnopyranosyl-(1→3)][E-caffeoyl-1→4]-β-D-4C1-glucopyranoside (14), along with fourteen known compounds—eight flavonoids (2–9) and six phenylethanoid glycosides (10–13, 15–16). The chemical structures were established by 1 D and 2 D NMR and HRESIMS spectral methods. The known phenylethanoids were the same as reported for leaves or aerial parts of P. lanceolata or other Plantago species. The flavonoids appeared to be only flavonols, mainly isorhamnetin 3-O- and 3,4'-O- glycosides, and thus completely different from flavones, mainly luteolin and apigenin glucuronides, previously reported in the leaves. The possible medicinal and chemotaxonomic relevance of the phenolics found in P. lanceolata inflorescences were taken into consideration. [ABSTRACT FROM AUTHOR]

Phenylethanoid glycosides (PhGs) are naturally occurring glycosides derived from plants with various biological activities. Glycosyltransferases catalyze the production of PhGs from phenylethanols via a transglycosylation reaction. The low activity and stability of glycosyltransferase limit its industrial application. An ancestral glycosyltransferase, UGTAn85, with heat resistance, alkali resistance, and high stability was resurrected using ancestral sequence reconstruction technology. This enzyme can efficiently convert phenylethanols to PhGs. The optimal reaction temperature and pH for UGTAn85 were found to be 70 °C and pH 10.0, respectively. This study employed a combination of structure-guided rational design and co-evolution analysis to enhance its catalytic activity. Potential mutation sites were identified through computer-aided design, including homology modeling, molecular docking, Rosetta dock design, molecular dynamics simulation, and co-evolution analysis. By targeted mutagenesis, the UGTAn85 mutant Q23E/N65D exhibited a 2.2-fold increase in enzyme activity (11.85 U/mg) and elevated affinity ( K m = 0.11 mM) for 2-phenylethanol compared to UGTAn85. Following a fed-batch reaction, 36.16 g/L 2-phenylethyl-β-d-glucopyranoside and 51.49 g/L salidroside could be produced within 24 h, respectively. The findings in this study provide a new perspective on enhancing the stability and activity of glycosyltransferases, as well as a potential biocatalyst for the industrial production of PhGs.

Targeting macrophage M1 polarization is a promising strategy with fewer detrimental effects in COVID-19 curation. Phenylethanoid glycosides (PhGs) of Cistanche tubulosa are a botanical drug to possess various anti-inflammation-related functions, such as immunomodulating, hepatoprotective or neuroprotective functions, whereas their anti-inflammatory activity is rarely understood. A search into their anti-inflammatory characteristics led to the isolation of 49 PhGs along with 15 new PhGs. Their inhibitory effects against M1 polarization induced by LPS plus IFN-γ were explored in RAW264.7 macrophages. Of these PhGs, tubuloside B (Tub B) exerted substantial NO scavenging effect both in chemical- and cell-based assays, and it inhibited massive production of cytokines and chemokines. Tub B decreased ERK1/2 phosphorylation via direct binding and inhibited the MAPK signaling pathway. Tub B also directly binded to Mob1 protein, thereby increased the stability and level of Mob1 protein by inhibiting ubiquitinated degradation. Mob1 was pivotal for the anti-inflammatory activity of Tub B, and it acted independently of the canonical Hippo-YAP pathway. Moreover, ERK1/2 and Mob1 also had a synergic effect on modulating the inflammatory response. Finally, these effects of Tub B were verified in mice with LPS-induced systemic inflammatory response syndrome. Taken together, these results indicated that Tub B acted as a promising agent against M1 macrophage activation by synergistically targeting ERK1/2 and Mob1, and that it may potentially be a drug candidate to prevent/treat inflammatory diseases, especially in COVID-19.

(1) Background: The aim of the study was to compare the potency of Plantago media L. (Plantaginaceae) extracts on Acanthamoeba sp. trophozoites, which are opportunistic protozoan parasites leading to several dangerous diseases; (2) Methods: The chromatographically (TLC, HPLC-DAD) characterized water fractions of the extracts from biomass from in vitro cultures (shoots and roots), leaves, and inflorescences from field cultivation were used for the study of the acanthamoebic activity in a Thoma haemocytometer chamber; (3) Results: The anti-amoebic effect at the lowest concentration (1.0 mg/mL) was demonstrated only by the extract of the leaves from the cultivation (50.50% inhibition). The remaining samples inhibited the growth of parasites from a concentration of 5.0 mg/mL in the range of 41.36% inflorescences to 63.89% shoots in vitro. Quantitative determinations of phenolic compounds in the tested extracts indicate a tendency to increase the potency of the anti-amoebic effect with the content of a phenylethanoid glycoside—acteoside. The maximum content of this compound was determined in leaves from field cultivation (6.64%) and the minimum in inflorescences (0.65%). This is confirmed by the range of the lowest IC50 values (the strongest biological activity) for the tested samples, 0.95–1.80 mg/mL for leaves from cultivation, and the high values, 9.70–5.30 mg/mL for inflorescences and in-vitro-derived roots. The strength of the biological activity of the extracts correlated with the content of acteoside, which constituted 84–93% of the sum of phenolic compounds determined; (4) Conclusions: The performed investigations proved the anti-acanthamoebic efficacy of Plantago media organs, including those obtainable by biotechnological methods, and indicated phenylethanoid glycosides, their main phenolic constituents, to be responsible for the activity. To our knowledge, this is the first report on the amoebicidal activity of Plantago media extracts from biomass produced by biotechnological methods and organs of an intact plant.

Isoacteoside is a caffeoyl phenylethanoide glycoside found in various plant parts, such as the flower of Magnolia denudata. In particular, magnolia has been studied for its anti-obesity, anticancer, and anti-inflammatory effects. However, isoacteoside has not been extensively studied, except for its anti-inflammatory effects. In this study, the anti-obesity effects of isoacteoside were investigated in 3T3-L1 mouse pre-adipocytes. Isoacteoside treatment did not induce cytotoxicity in 3T3-L1 cells up to a concentration of 1000 μM. The anti-obesity effects on 3T3-L1 cells were confirmed using oil red O staining. In addition, the expression of obesity-related proteins and genes, such as peroxisome proliferator-activated acceptor gamma (PPARγ), CCAAT/enhancer-binding protein alpha (C/EBPα), and perilipin (PLIN1), was determined by western blotting and qRT-PCR assays to confirm the anti-obesity effects of isoacteoside. The results of this study suggest that isoacteoside, a natural substance isolated from plant extracts, is not highly toxic to normal cells, such as pre-adipocytes, and displays anti-obesity effects in vitro. [ABSTRACT FROM AUTHOR]

Psoriasis is a chronic inflammatory immune-mediated disease with skin and joint manifestations with no clear cause at present. The disease has an increasing prevalence, hence appeared to be the second largest contributor to skin-related impairment and hence affecting ca. 2-3% of the world population. A decade ago, psoriasis was recognized as a serious noncommunicable disease by the WHO. It manifests itself with characteristic skin lesions covered with silvery dry scales appearing in preferential places, such as elbows, knees and scalp and is associated with multiple comorbidities and significant negative effect on patients' quality of life. Plants and plant-derived molecules have gained considerable interest as a possible alternatives of current psoriasis treatments due to their multi-target benefits and fewer side effects compared to synthetic drugs. We explored the effect of biotechnologically-produced extracts and their bioactive principles in psoriasis (in vivo mice model) psoriasis-like inflammation (interferonγ/interleukin-17A/IL-22-stimulated HaCaT cells). Changes in key inflammatory signaling pathways, related to psoriasis development were detected by reverse transcription polymerase chain reaction and western blotting. Treatment with extracts and selected pure compounds improved psoriasis-related inflammation via suppression of the PI3K/AKT signaling in IFN-γ/IL-17A/IL-22-stimulated HaCaT cells. Overall, phenylethanoid glycosides appeared to have a therapeutic potential against psoriasis, by regulating keratinocyte differentiation, through inhibition of the PI3K/AKT signaling pathway. [ABSTRACT FROM AUTHOR]

Despite several studies on the Ajuga L. genus, the chemical composition of Ajuga pyramidalis, an alpine endemic species, is still largely unknown. The purpose of this study was to therefore deeper describe it, particularly from the phytochemistry and bioactivity perspectives. In that respect, A. pyramidalis was investigated and 95% of the extracted mass of the plant was characterized by chromatography and mass spectrometry. Apart from the already determined chemical compounds, namely, harpagide and 8-O-acetylharpagide, two iridoids, and neoajugapyrin A, a neo-clerodane diterpene, and three polyphenols (echinacoside, verbascoside and teupoloside) were identified for the first time in A. pyramidalis. Incidentally, the first RX structure of a harpagoside derivative is also described in this paper. The extracts and isolated compounds were then evaluated for various biochemical or biological activities; notably a targeted action on the renewal of the epidermis was highlighted with potential applications in the cosmetic field for anti-aging.

Stachys thracica Davidov is a Balkan endemic species distributed in Bulgaria, Greece, and Turkey. In Bulgaria, it is classified as "rare" and is under the protection of the Bulgarian biodiversity law. The aim of our study was to develop an efficient protocol for ex situ conservation of S. thracica and to perform comparative NMR-based metabolite profiling and bioactivity assays of extracts from in situ grown, in vitro cultivated, and ex vitro acclimated plants. Micropropagation of S. thracica was achieved by in vitro cultivation of mono-nodal segments on basal MS medium. Ex vitro adaptation was accomplished in the experimental field with 83% survival while conserved genetic identity between in vitro and ex vitro plants as shown by the overall sequence-related amplified polymorphism marker patterns was established. Verbascoside, chlorogenic acid, and trigonelline appeared the main secondary metabolites in in situ, in vitro cultivated, and ex vitro acclimated S. thracica. High total phenolic and flavonoid content as well as antioxidant and radical scavenging activity were observed in in situ and ex vitro plants. Further, the anti-inflammatory activity of S. thracica was tested by hemolytic assay and a high inhibition of the complement system was observed. Initiated in vitro and ex vitro cultures offer an effective tool for the management and better exploitation of the Stachys secondary metabolism and the selection of lines with high content of bioactive molecules and nutraceuticals. [ABSTRACT FROM AUTHOR]

Scrophularia striata Boiss. (Scrophulariaceae family), as an important medicinal plant, is one of the species native to Western Iran. This perennial herbaceous plant has been traditionally used to cure various diseases, including eye and ear infections, inflammation, infectious wounds, colds, and boils, and is also used to treat bacterial, fungal, and viral infections in the world. Since the COVID-19 pandemic outbreak, Ongoing efforts are proceeding worldwide to develop an efficient vaccine and use approaches to find preventive measures and effective treatment. S. striata was introduced as a phenylethanoid glycosides (PhGs) source. S. striata functions as a resistant plant under various stresses. The essential mechanism in response to abiotic and biotic stress is the production of phenolic compound precursors, which eventually leads to PhG compound accumulation, especially acteoside, in this plant. Acteoside operates as a powerful antioxidant that scavenges excess ROS content in biological systems. The study purposed to evaluate the acteoside content in response to Pb stress of S. striata. HPLC analysis was employed to identify PhGs between the untreated and Pb-treated shoots plants with three gathering times (24, 48, and 72 h). Our results indicated that acteoside increased significantly after 72 h under Pb stress, and no significant difference was observed in other time courses. In general, S. striata is a good source of PhGs, especially acteoside, with application in the pharmaceutical industry.

Echinacoside (ECH), acteoside (ACT), and isoacteoside (ISAT), the typical phenylethanoid glycosides (PhGs) in cistanches herba, have various pharmacological activities. However, the ECH, ACT and ISAT have extremely low oral bioavailability, which is related to their metabolism under the intestinal flora. Previous studies showed that intestinal metabolites were the hepatoprotective substances in vivo, but the research on whether PhGs has effects without intestinal bacteria has not been studied. In this paper, ECH, ACT and ISAT were incubated with human or rat intestinal bacteria for 36 h. After incubating with human bacteria for 36 h, three prototype compounds were not detected and were mainly biotransformed to 3-HPP and HT. In the network pharmacology, a total of 6 common targets were obtained by analysing the prototypes, the metabolites and the liver injury. It was found that the combinations of three metabolites and common targets were more stable than those of the prototypes and common targets by molecular docking. Meanwhile, hepatocellular apoptosis, proliferation, inflammation and oxidative responses might play important roles in the mechanisms of the metabolites exerting hepatoprotective activities. Then normal and pseudo-sterile mice experiments were adopted to further compare the hepatoprotective activities of prototypes and metabolites. Animal experiment results showed that the prototypes and the metabolites in the normal mice had significantly hepatoprotective activity. Interestingly, in the pseudo-germfree mice, the metabolites showed significant hepatoprotective effect, but the prototypes had not effect. It indicated that the prototype cannot exert liver protective activity without the effect of intestinal bacteria. [ABSTRACT FROM AUTHOR]

Introduction: Craterostigma plantagineum and Lindernia brevidens are resurrection plants, so these plants can tolerate desiccation of their vegetative tissues. Different components and mechanisms contribute to desiccation tolerance and secondary plant metabolites, like phenolic compounds, may play a role during these processes. Objectives: Secondary plant metabolites of the two resurrection plants, C. plantagineum and L. brevidens as well as the closely related desiccation sensitive species, L. subracemosa, were investigated regarding the polyphenol profile. Material and methods: Secondary plant compounds were extracted with acidified methanol and analysed with ultra‐high‐performance liquid chromatography electrospray ionisation mass spectrometry (UHPLC‐ESI‐MS). Phenolic compounds were identified by comparing of ultraviolet (UV) and MSn‐spectra with published data. All compounds were quantified as verbascoside equivalents by external calibration at the compound specific wavelength. Results: In total, eight compounds that belong to the subclass of phenylethanoid glycosides and one flavone, luteolin hexoside pentoside, were identified. Two of these compounds exhibited a fragmentation pattern, which is closely related to phenylethanoid glycosides. The predominantly synthesised phenylethanoid in all of the three plant species and in every stage of hydration was verbascoside. The total content of phenolic compounds during the three stages of hydration, untreated, desiccated, and rehydrated revealed differences especially between C. plantagineum and L. brevidens as the latter one lost almost all phenolic compounds during rehydration. Conclusion: The amount of verbascoside correlates with the degree of desiccation tolerance and verbascoside might play a role in the protective system in acting as an antioxidant. Verbascoside is the main phenolic compound in three selected Linderniaceae species. The amount of verbascoside correlates with the degree of desiccation tolerance in these species. Verbascoside might act as antioxidant and thus may contribute to protection mechanisms in desiccation tolerant Linderniaceae. [ABSTRACT FROM AUTHOR]

Copyright of Journal of Food Safety & Quality is the property of Journal of Food Safety & Quality Editorial Department and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

This present study was an evaluation of the antioxidant and cytotoxic activities of Incarvillea emodi (Bignoniaceae). The aqueous extracts of different parts of Incarvillea emodi, collected from different places in Pakistan, were tested for radical scavenging effects on 2,2-diphenyl-1-picrylhydrazil (DPPH), nitric oxide (NO), superoxide (SO) and [2,2"-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)] (ABTS•+) radicals. DPPH radical scavenging effects of three polyamide column fractions of one extract were also tested. The cytotoxicity of the extracts were tested against Hep-2 (human larynx epidermoid carcinoma) cancer cell line by MTT [3-(4,5- dimethylthiazol-2- yl)-2,5-diphenyltetrazolium bromide] method. In addition, an HPLC-DAD system was used to show the presence of phenylethanoid glycosides in the most active polyamide column fraction. The free radical scavenging effects of the extracts were found comparable to that of reference antioxidants, 3-t-butyl-4-hydroxyanizole (BHA), quercetin and ascorbic acid (AA). Concentration dependent cytotoxic activity was observed against Hep-2 cancer cell line. Two phenylethanoid glycosides, acteoside and leucosceptoside A, were identified in the active polyamide column fraction at HPLC-DAD system. The presence of phenylethanoid glycosides in Incarvillea emodi was shown for the first time with this study. Antioxidant and cytotoxic activity researches are important for developing new drugs. Our results supported to use of Incarvillea emodi as folk medicine due to several biological effects in Pakistan. Moreover, the use of Incarvillea genus as a traditional ethnoveterinary medicine in dyspepsia and internal diseases were reported in previous studies.

Abstract Background Cistanche tubulosa (Schenk) R. Wight is a traditional Chinese medicine that parasitizes the roots of the Tamarix plant and has been used to treat male impotence, sterility, body weakness, and as a tonic. However, its antitumor effect on hepatocellular carcinoma is still elusive. Here, we investigated the antitumor effect of C. tubulosa phenylethanoid glycosides (CTPG) on H22 hepatocellular carcinoma cells both in vitro and in vivo and its mechanisms. Methods The morphology, viability, apoptosis, cell cycle and mitochondrial membrane potential (Δψm) of H22 cells were analyzed by inverted microscopy, MTT assay and flow cytometry, respectively. The expression and activation of proteins in apoptosis pathway were detected by Western blot. The in vivo antitumor effect was evaluated in tumor mouse model established using male Kunming mice. Results CTPG treatment significantly suppressed H22 cell growth in a dose- and time-dependent manner, which was correlated with the increased apoptosis and cell cycle arrest at G0/G1 and G2/M phases. Moreover, the chromosomal condensation was observed in CTPG-treated H22 cells. CTPG treatment significantly increased Bax/Bcl-2 ratio, reduced Δψm and enhanced the release of cytochrome c. The levels of cleaved caspase-8 and caspase-9 in both extrinsic and intrinsic signaling pathways were significantly increased that sequentially activated caspase-7 and -3 to cleave PARP. Finally, CTPG inhibited the growth of H22 cells in mice and improved the survival rate of tumor mice. Conclusions These results suggested that CTPG suppressed H22 cell growth through both extrinsic and intrinsic apoptosis pathways.

Abstract Following a request from the European Commission, the EFSA Panel on Nutrition, Novel Foods and Food Allergens (NDA) was asked to deliver an opinion on water extract of Cistanche tubulosa stems as a novel food (NF) for its use in food supplements (FS) and foods for special medical purposes (FSMP). The target population is the general adult population excluding pregnant and lactating women. The applicant proposes a maximum daily intake of 2 g for FS and a maximum use level of 10% in FSMP. The characteristic components of the extract are phenylethanoid glycosides (at least 70% of the NF), in particular, echinacoside (25–45% of the NF). The NF has been authorised as a prescription drug in China in 2005 for the treatment of vascular dementia. The Panel notes that an integrated analysis of three studies covering 1,076 patients with vascular dementia treated with the proposed NF at a daily dose of 1,800 mg, reported that 12 adverse events (AEs) were classified to be ‘definitely’, ‘probably’ or ‘possibly related’ to the exposure to the NF. Two of these AE were classified as severe (cerebral haemorrhage and epilepsy). The Panel considers that the reported AEs raise safety concerns. The Panel also notes the limitations of the provided toxicological studies, in particular the non‐compliance with the EFSA approach on the genotoxicity testing strategy and the non‐compliance with good laboratory practice (GLP) and the respective OECD Guidance documents of the repeated dose toxicity studies. In view of the AEs in the human studies, the Panel considers that additional toxicological studies, following testing guidelines would not be able to overcome the concerns raised from the human studies. The Panel concludes that the safety of the NF has not been established.

Following a request from the European Commission, the EFSA Panel on Nutrition, Novel Foods and Food Allergens (NDA) was asked to deliver an opinion on water extract of Cistanche tubulosa stems as a novel food (NF) for its use in food supplements (FS) and foods for special medical purposes (FSMP). The target population is the general adult population excluding pregnant and lactating women. The applicant proposes a maximum daily intake of 2 g for FS and a maximum use level of 10% in FSMP. The characteristic components of the extract are phenylethanoid glycosides (at least 70% of the NF), in particular, echinacoside (25-45% of the NF). The NF has been authorised as a prescription drug in China in 2005 for the treatment of vascular dementia. The Panel notes that an integrated analysis of three studies covering 1,076 patients with vascular dementia treated with the proposed NF at a daily dose of 1,800 mg, reported that 12 adverse events (AEs) were classified to be 'definitely', 'probably' or 'possibly related' to the exposure to the NF. Two of these AE were classified as severe (cerebral haemorrhage and epilepsy). The Panel considers that the reported AEs raise safety concerns. The Panel also notes the limitations of the provided toxicological studies, in particular the non-compliance with the EFSA approach on the genotoxicity testing strategy and the non-compliance with good laboratory practice (GLP) and the respective OECD Guidance documents of the repeated dose toxicity studies. In view of the AEs in the human studies, the Panel considers that additional toxicological studies, following testing guidelines would not be able to overcome the concerns raised from the human studies. The Panel concludes that the safety of the NF has not been established. [ABSTRACT FROM AUTHOR]

Stachys thracica Davidov is a Balkan endemic species distributed in Bulgaria, Greece, and Turkey. In Bulgaria, it is classified as “rare” and is under the protection of the Bulgarian biodiversity law. The aim of our study was to develop an efficient protocol for ex situ conservation of S. thracica and to perform comparative NMR-based metabolite profiling and bioactivity assays of extracts from in situ grown, in vitro cultivated, and ex vitro acclimated plants. Micropropagation of S. thracica was achieved by in vitro cultivation of mono-nodal segments on basal MS medium. Ex vitro adaptation was accomplished in the experimental field with 83% survival while conserved genetic identity between in vitro and ex vitro plants as shown by the overall sequence-related amplified polymorphism marker patterns was established. Verbascoside, chlorogenic acid, and trigonelline appeared the main secondary metabolites in in situ, in vitro cultivated, and ex vitro acclimated S. thracica. High total phenolic and flavonoid content as well as antioxidant and radical scavenging activity were observed in in situ and ex vitro plants. Further, the anti-inflammatory activity of S. thracica was tested by hemolytic assay and a high inhibition of the complement system was observed. Initiated in vitro and ex vitro cultures offer an effective tool for the management and better exploitation of the Stachys secondary metabolism and the selection of lines with high content of bioactive molecules and nutraceuticals.

Phenylethanoid glycosides (PhGs) are generally water‐soluble phenolic compounds that occur in many medicinal plants. Until June 2020, more than 572 PhGs have been isolated and identified. PhGs possess antibacterial, anticancer, antidiabetic, anti‐inflammatory, antiobesity, antioxidant, antiviral, and neuroprotective properties. Despite these promising benefits, PhGs have failed to fulfill their therapeutic applications due to their poor bioavailability. The attempts to understand their metabolic pathways to improve their bioavailability are investigated. In this review article, we will first summarize the number of PhGs compounds which is not accurate in the literature. The latest information on the biological activities, structure–activity relationships, mechanisms, and especially the clinical applications of PhGs will be reviewed. The bioavailability of PhGs will be summarized and factors leading to the low bioavailability will be analyzed. Recent advances in methods such as bioenhancers and nanotechnology to improve the bioavailability of PhGs are also summarized. The existing scientific gaps of PhGs in knowledge are also discussed, highlighting research directions in the future. [ABSTRACT FROM AUTHOR]