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SUMMARY Ilex is known for its rich content of secondary metabolites, particularly triterpenoid saponins. These compounds hold significant value in natural remedies and herbal medicine. However, the molecular mechanisms responsible for triterpenoid biosynthesis in plants of this genus remain largely unexplored. In this study, we successfully generated the first chromosome‐scale genome of Ilex hylonoma. The assembly, comprising 20 anchored chromosomes, has an N50 contig size of 2.13 Mb and a scaffold size of 33.68 Mb. Comparative genome analyses with two other congeners with available chromosome‐level genomes suggested that an end‐to‐end chromosome fusion event likely contributed to the reduction in chromosome number from n = 20 to n = 19 within this genus. By integrating transcriptomic and metabolomic data, we identified the gene expression patterns and metabolite profiles of I. hylonoma across three commonly utilized medicinal tissues. We subsequently pinpointed candidate genes involved in the regulation of triterpenoid saponin biosynthesis, including CYP450 genes, UGT genes, and associated transcription factors. Furthermore, yeast heterologous expression analysis revealed that ihyl08363 catalyzed the conversion of β‐amyrin into oleanolic acid, while ihyl04303 catalyzed the C‐2α hydroxylation of oleanolic acid to produce maslinic acid. This integrated analysis provides valuable insights into the biosynthesis of important triterpenoid saponins in medicinal Ilex plants. [ABSTRACT FROM AUTHOR]

BACKGROUND RESULTS CONCLUSION Climate change results in an increased occurrence of drought periods, which affect the performance of Mediterranean legumes such as sulla. To evaluate the effects of drought stress on the antioxidant capacity and the accumulation of phytochemicals in sulla shoots, rainfed and drought‐stressed plants (RAI) and watered plants with timely vegetative regeneration (STI) were cultivated in parallel in a field experiment and sampled at four different times.Drought stress strongly and positively affected the antioxidant capacity and the accumulation of polyphenols in sulla shoots, with key differences at wintertime. These findings were supported through untargeted and targeted metabolomics of RAI and STI samples, which detailed the accumulation of about 300 secondary metabolites in RAI, mostly polyphenols and saponins.This study provided new insights into the changes in secondary metabolites in sulla due to drought stress, which can be used to produce forages or raw plant extracts with enhanced biological effects. © 2024 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

ABSTRACT Biosynthesis of specific secondary metabolites in plants involves fine regulation of gene expression. Camellia chekiangoleosa has important economic value: the seeds contain high‐quality unsaturated fatty acids and the pericarp is rich in tea saponins. As an important posttranscriptional regulator, the role of microRNAs (miRNAs) in controlling secondary metabolism in C. chekiangoleosa is not fully studied. Here, we investigated the role of miRNAs and their targets in the secondary metabolic regulatory network by comprehensively analyzing small RNAs, transcriptomes, and degradomes from different tissues. We identified 168 known miRNAs and 74 novel miRNAs in the C. chekiangoleosa genome and revealed 15 tandem clusters containing 35 miRNAs. By establishing a gene regulatory network containing miRNAs, target genes, and transcription factors, we unravelled the multiplicity of miRNA tissue‐specific regulation of gene expression, which may be tightly linked to the synthesis of secondary metabolites. Furthermore, we characterized a novel long‐noncoding miRNA gene (cch‐miR3633) that targeted a UDP‐transferase gene (CchUGT94E5). We showed that, ectopic expression of CchUGT94E5 caused outgrowth of shoot branching and changes in cytokinin contents in Arabidopsis, indicating a potential role of regulating secondary metabolism. This work provides valuable information for the study of miRNA regulation of secondary metabolism. [ABSTRACT FROM AUTHOR]

Background and purpose Experimental approach Key results Conclusion and implications Atherosclerosis is the basis of cardiovascular disease. Ferroptosis is a form of programmed cell death characterized by lipid peroxidation, which contributes to atherogenesis. The plant extract PNS (Panax notoginseng saponins), containing the main active ingredients of Panax notoginseng, exhibits anti‐atherogenic properties. Herein, we determined whether PNS and its major components could attenuate atherosclerosis by suppressing ferroptosis and revealed the underlying mechanism(s).The anti‐atherogenic effects of PNS and their association with inhibition of ferroptosis was determined in apoE−/− mice. In vitro, the anti‐ferroptotic effect and mechanism(s) of PNS components were demonstrated in the presence of ferroptosis inducers. Expression of ferroptosis markers and the ubiquitination of Keap1 were evaluated in USP2−/− macrophages. Finally, the anti‐atherogenic effect of USP2 knockout was determined by using USP2−/− mice treated with high‐fat diet (HFD) and AAV‐PCSK9.PNS inhibited ferroptosis and atherosclerosis in vivo. PNS suppressed ferroptosis and ferroptosis‐aggravated foam cell formation and inflammation in vitro. Mechanistically, PNS and its components activated Nrf2 by antagonizing Keap1, which was attributed to the inhibition of USP2 expression. USP2 knockout antagonized ferroptosis and ferroptosis‐aggravated foam cell formation and inflammation, thus mitigating atherosclerosis. USP2 knockout abolished inhibitory effects of PNS on foam cell formation and inflammation in vitro.PNS reduced USP2‐mediated Keap1 de‐ubiquitination and promoted Keap1 degradation, thereby activating Nrf2, improving iron metabolism and reducing lipid peroxidation, thus contributing to an anti‐atherosclerotic outcome. Our study revealed the mechanism(s) underlying inhibition of ferroptosis and atherosclerosis by PNS. [ABSTRACT FROM AUTHOR]

Polygalae Radix is a commonly used traditional Chinese medicine with multiple pharmacological activities. Modern research have revealed that saponins, xanthones, and oligosaccharide esters are its effective component groups. However, up to date the chemical substances in these effective component groups are still unclear, which has become a fundamental scientific issue needing to be addressed. In our study, an analysis strategy based on targeted tandem mass spectrometry (MS/MS) analysis was proposed to comprehensively identify the chemical substances in effective component groups. First, the extract of the Polygalae Radix was detected by ultra‐performance liquid chromatography coupled with electrospray ionization–orbitrap mass spectrometry in a full MS scan mode to minimize the losses of signals; second, the precursor ions of all compounds were extracted from the obtained full MS scan data using Compound Discoverer software; third, the interested precursor ions were locked based on their molecular features and constructed in a precursor ion list; finally, each precursor ion in the list was subjected to targeted MS/MS analysis for structure characterization. Using our analysis strategy, a total of 565 components were successfully identified. [ABSTRACT FROM AUTHOR]

Saponins are glycosides widely distributed in the plant kingdom and have many pharmacological activities. However, their tendency to bind to cell membranes can cause cell rupture, limiting their clinical use. In the previous study, aristatoside C and davisianoside B were isolated from Cephalaria species. Cytotoxicity assays showed that they are more active on A‐549 cell lines than doxorubicin but caused hemolysis. In the current research, aristatoside C and davisianoside B were loaded to phytosomes called ALPs and DLPs respectively, and characterized for particle size, zeta potential, encapsulation efficiency, release kinetic, hemolytic activity, and cytotoxicity on A‐549 cell line. DLPs maintained the cytotoxic activity of the free saponins against A‐549 cells with IC50 of 9,64±0,02 μg/ml but dramatically reduced their hemolytic activity. Furthermore, temperature and time‐dependent stability studies based on the size and zeta potential of ALPs and DLPs revealed that the phytosomes have sustained release properties over 2 weeks. Overall, DLPs displayed cytotoxicity against A‐549 cells with minimal hemolysis and sustained release, highlighting their potential as nanotherapeutics for clinical applications. [ABSTRACT FROM AUTHOR]

Objective: Radiation proctitis (RP) refers to rectal injury caused by radiation treatment of pelvic and retroperitoneal malignancies, which has a major impact on the treatment prognosis and quality of life of patients with cancer. The tetracyclic triterpene saponin monomer ginsenoside Rg3 (GRg3), the primary bioactive ingredient in ginseng extracts, has therapeutic effects against RP in rats. Here, we validated its efficacy and elucidated its mechanism of action. Methods: A rat RP model was established in 48 Wistar rats. Rats were randomly divided into control (untreated), irradiation, irradiation + dexamethasone, and irradiation + GRg3 (low‐, medium‐, and high‐dose) groups. After 2 weeks' treatment, serum IL‐4, IL‐10, and TNF‐α levels were tested by enzyme‐linked immunosorbent assays. In rectal tissue, Ikbkb, Ikka, and Casp8 mRNA expression was detected by a reverse transcription‐quantitative polymerase chain reaction. IKK‐β, IκB‐α, p‐IκB‐α, p50, and caspase‐8 protein levels were determined by western blot analysis. Results: GRg3 significantly improved the general condition and histopathological damage in rats with RP. Moreover, GRg3 decreased the levels of factors that promote inflammation (TNF‐α) and increased the levels of factors that reduce inflammation (IL‐4 and IL‐10). GRg3 markedly reduced the activation of NF‐κB and caspase‐8 signaling pathways. Conclusions: Thus, GRg3 may reduce the inflammatory response by blocking the NF‐κB signaling pathway and improving the balance of inflammation‐related factors. GRg3 may also inhibit intestinal cell apoptosis by suppressing the TNF‐α/caspase‐8 signaling cascade, thereby reducing radiological rectal injury. Our results verify that GRg3 is a promising therapeutic agent for RP treatment and shed light on its mechanism. [ABSTRACT FROM AUTHOR]

BACKGROUND: In this study, the content and structure of Polygonatum sibiricum polysaccharides and saponins during different processing stages were determined. RESULTS: After processing of Polygonatum, the content of polysaccharide and glucose decreased, and the content of galactose, glucuronic acid and sugar substitution gradually increased. The content of total saponins increased significantly. Only 18 compounds were found in raw Polygonatum and 17 new compounds were presented in processed Polygonatum. During the processing of Polygonatum, the polysaccharide was partially degraded into oligosaccharides, the molecular weight gradually decreased, and the neutral sugar was converted into uronic acid, resulting in a decrease in polysaccharide content. The saponins were partially degraded into sapogenins or modified. CONCLUSION: This study clarifies the changes in the content and structure of polysaccharides and saponins in processed Polygonatum, which will pave the way for elucidating the processing mechanism. © 2024 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

Background Aim Methods Results Conclusion The investigations of snail slime and its possible biological activities have been performed recently.This study aimed to evaluate the properties of Helix aspersa snail slime (HAS), and carotenoids‐fortified slime (HASC).Snails were fed with carrots for 10 days. Slime was collected and extracted using water. Saponins identification, antioxidant, collagenase, and tyrosinase enzyme inhibition activities, carotenoids, total phenols, and flavonoids content, were determined. UHPLC–MS/MS analysis was performed for phytochemical characterization.Saponins were detected in the HAS extract only. However, HASC was shown to contain a higher carotenoid content than HAS (29.51 ± 0.4 vs. 18.11 ± 0.2 μg/g). similarly, total phenolic and flavonoid content were higher for the the HASC extract compared to the HAS (182.3 ± 5.2 vs. 150.28 ± 3.3 mg/g equivalent to gallic acid), and (77.62 ± 1.2 vs. 14.19 ± 0.9 mg/g equivalent to quercetin). As expected, the HASC extract exhibited higher antioxidant activity compared to the HAS, using DPPH and the ABTS assays (IC50 = 7.75 ± 0.14 vs. 20.1 ± 0.4 μg/mL), and (IC50 = 7.6 ± 0.26 vs. 19.57 ± 1.4 μg/mL). UHPLC–MS/MS analysis revealed the presence of several phytocomponents of which, hexadecanoic acid and ascorbic acid, were observed in the HASC extract. Furthermore, HASC extract exhibited superior inhibitory activity compared to HAS against collagenase and tyrosinase enzymes (IC50 = 8.4 ± 1.19 vs. 15.3 ± 1.12 μg/mL) and (IC50 = 30.1 ± 0.91 vs. 35 ± 1.3 μg/mL).These findings highlight the potential of HASC as a valuable ingredient in various pharmaceutical applications, due to their content of various phenolic, antioxidants, carotenoids, hexadecanoic, and ascorbic acids. The latter is well known for its great cosmeceutical applications used for slowing the process of skin aging. [ABSTRACT FROM AUTHOR]

Solanaceous plants, such as Solanum dulcamara, produce steroidal glycosides (SGs). Leaf SG profiles vary among S. dulcamara individuals, leading to distinct phytochemical phenotypes (‘chemotypes’) and intraspecific phytochemical diversity (‘chemodiversity’). However, if and how SG chemodiversity varies among organs and across ontogeny, and how this relates to SG metabolism gene expression is unknown. Among organs and across ontogeny, S. dulcamara plants with saturated (S) and unsaturated (U) SG leaf chemotypes were selected and clonally propagated. Roots, stems and leaves were harvested from vegetative and flowering plants. Extracts were analysed using untargeted LC–MS. Expression of candidate genes in SG metabolism (SdGAME9, SdGAME4, SdGAME25, SdS5αR2 and SdDPS) was analysed using RT‐qPCRs. Our analyses showed that SG chemodiversity varies among organs and across ontogeny in S. dulcamara; SG richness (Dmg) was higher in flowering than vegetative plants. In vegetative plants, Dmg was higher for leaves than for roots. Lack of SdGAME25 expression in U‐chemotype leaves, while readily expressed in roots and stems, suggests a pivotal role for SdGAME25 in differentiation of leaf chemotypes in vegetative and flowering plants. By acting as an ontogeny‐dependent chemotypic switch, differential regulation of SdGAME25 enables adaptive allocation of SGs, thereby increasing SG chemodiversity in leaves. This indicates that differential expression and/or regulation of glycoalkaloid metabolism genes, rather than their presence or absence, explains observed chemotypic variation in SG chemodiversity among organs and across ontogeny. [ABSTRACT FROM AUTHOR]

Objective: Solanum nigrum L. (SNL) is a natural drugwith diverse bioactive components and multi‐targeted anti‐tumor effects, gaining increasing attention in clinical application. Method and Results: This paper reviews the studies on SNL by searching academic databases (Google Scholar, PubMed, Science Direct,and Web of Science, among others), analyzing its chemical compositions (alkaloids, saponins, polysaccharides, and polyphenols, among others), andbriefly describes the anti‐tumor mechanisms of the main components. Discussion: This paper discusses the shortcomings of the current research on SNL and proposes corresponding solutions, providing theoretical support for further research on its biological functions and clinical efficacy. [ABSTRACT FROM AUTHOR]

BACKGROUND RESULTS CONCLUSION Sanqi, the root of Panax notoginseng, has long been recognized for its therapeutic effects on cardiovascular diseases. Saponins, including ginsenosides and notoginsenosides, are the main bioactive components of P. notoginseng. The biosynthesis of saponins is closely related to the defense responses orchestrated by endogenous hormones.To provide new insights into the underlying role of phytohormone jasmonic acid (JA) in the synthesis and regulation of saponins, we performed an ultra‐performance liquid chromatography analysis of different tissues of P. notoginseng aged 2–4 years. Moreover, by combined evaluation of saponin content and transcriptome profiling of each tissue, the spatial and temporal distribution of saponins was analyzed. N notoginsenoside R1, ginsenoside Rb1 and ginsenoside Rd accumulated in the underground tissues, including the root, tuqi, fibril and rhizome. In agreement with this data, the corresponding genes of the endogenous hormone JAs, especially coronatine insensitive 1 (COI1) and myelocytomatosis proteins 2 (MYC2), were predominantly expressed in the underground tissues. The tissue‐ and age‐specific distribution of saponins was consistent with the expression of genes involved in JA biosynthetic, metabolic and signaling pathways.The present study has revealed the temporal and spatial effects of endogenous phtohormones in the synthesis and regulation of notoginsenosides, which will provide a significant impact on improving the ecological planting technology, cultivating new high‐quality varieties and protecting the rare resources of medicinal P. notoginseng. © 2024 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

Summary: Climate change may result in a drier climate and increased salinization, threatening agricultural productivity worldwide. Quinoa (Chenopodium quinoa) produces highly nutritious seeds and tolerates abiotic stresses such as drought and high salinity, making it a promising future food source. However, the presence of antinutritional saponins in their seeds is an undesirable trait. We mapped genes controlling seed saponin content to a genomic region that includes TSARL1. We isolated desired genetic variation in this gene by producing a large mutant library of a commercial quinoa cultivar and screening the library for specific nucleotide substitutions using droplet digital PCR. We were able to rapidly isolate two independent tsarl1 mutants, which retained saponins in the leaves and roots for defence, but saponins were undetectable in the seed coat. We further could show that TSARL1 specifically controls seed saponin biosynthesis in the committed step after 2,3‐oxidosqualene. Our work provides new important knowledge on the function of TSARL1 and represents a breakthrough for quinoa breeding. [ABSTRACT FROM AUTHOR]

Aim: The vasorelaxant saponins jujuboside A(1), A1(2), B(3), and acetyljujuboside B(4) were isolated from 50% MeOH extracts of seeds of Zizyphus jujuba Mill. var. spinosa Hu ex H.F. Chou (Rhamnaceae), and their effects were studied using isolated rat aortic rings. Method: Dried jujube seeds were crushed and extracted with 50% MeOH, and the extracts were concentrated under reduced pressure. Vasorelaxant effects of this extracts were assessed on rat isolated aorta rings. The aorta rings were placed in a well‐oxygenated bath of modified Krebs–Henseleit solution and the mechanical tension was measured isometrically. Results: The crude extract was fractionated by chromatographic methods with the guidance of vasorelaxant activity, and four saponins (1~4) were isolated. These compounds were identified using nuclear magnetic resonance (NMR) studies. Compounds 1~4 showed slow relaxation activity against norepinephrine (NE)‐induced contractions of rat aorta with/without endothelium. Treatment with 1~4 did not significantly inhibit NE‐induced vasoconstrictions. Compounds 1~4 inhibited vasoconstriction induced by high‐concentration potassium (60 mM) and NE in the presence of nicardipine but did not affect phorbol 12‐myristate 13‐acetate‐induced vasoconstriction. Conclusion: These results suggest that inhibition of NE‐induced vasoconstriction by 1~4 is due to the inhibition of receptor‐operated Ca2+ channels and voltage‐dependent Ca2+ channels or inhibition of intracellular calcium modulations. [ABSTRACT FROM AUTHOR]

Taxus contorta (family Taxaceae) is a native plant of temperate region of western Himalaya. The current study investigated the effect of altitude on the phytochemical composition and mycorrhizal diversity, associated with distribution of T. contorta in Shimla district, Himachal Pradesh, India. Quantitative phytochemical analysis of the leaf extracts indicated that alkaloid levels decreased with altitude, with the highest value in Himri's methanol extracts (72.79 ± 1.08 mg/g) while phenol content increased with altitude, peaking in Nankhari's methanol extracts (118.83 ± 5.90 mg/g). Saponin content was higher in methanol extracts (78.13 ± 1.66 mg/g in Nankhari, 68.06 ± 1.92 mg/g in Pabbas, and 56.32 ± 1.93 mg/g in Himri). Flavonoid levels were notably higher in chloroform extracts, particularly in Nankhari (219.97 ± 2.99 mg/g), and positively correlated with altitude. Terpenoids were higher in chloroform extracts at Himri (11.34 ± 0.10 mg/g) and decreased with altitude. Taxol content showed minimal variation between solvents and altitudes (4.53–6.98 ppm), while rutin was only detected in methanol extracts (1.31–1.46 ppm). Mycorrhizal spore counts in T. contorta's rhizosphere varied with altitude: highest at Himri (77.83 ± 2.20 spores/50 g soil), decreasing to Pabbas (68.06 ± 1.96 spores/50 g soil) and lowest at Nankhari (66.00 ± 2.77 spores/50 g soil), with 17 AMF species identified overall, showing significant altitudinal influence on spore density. The rhizosphere of T. contorta was shown to be dominated by the Glomus species. The rhizospheric soil of the plant was found to be slightly acidic. Organic carbon and available potassium content decreased contrasting with increasing available nitrogen and phosphorus with altitude. Correlation data showed strong negative links between organic carbon (−0.83), moderate positive for nitrogen (0.46) and phosphorus (0.414), and moderate negative for potassium (−0.56) with the altitude. This study provides a comprehensive insight into changes in phytochemical constituents, mycorrhizal diversity and soil composition of T. contorta along a range of altitude. [ABSTRACT FROM AUTHOR]

ABSTRACT Breast cancer ranks as a leading cause of mortality, primarily affecting females. With the reported side effects of conventional anticancer drugs, herbal sources have emerged as an effective alternative for the treatment of various severe diseases like cancer. Hydrocotyle javanica Thunb. (H. javanica) is a perennial herb belonging to Araliaceae family. This study explored the ethnobotanical use of H. javanica, its pharmacognosy, antioxidant, and phytochemical characterization using liquid chromatography‐mass spectrometry tool, and molecular docking against breast cancer receptor, human epidermal growth factor receptor‐2 (HER2). The study revealed morphological, microscopic diagnostic features, and physicochemical properties of H. javanica. Methanolic extract of H. javanica (MEHJ) displayed dose‐dependent antioxidant activities. LC–MS analysis characterized metabolites of flavonoids, phenolic acids, triterpenoid, and triterpenoid saponin. Phytochemicals including chlorogenic acid, astragalin, and hyperoside, displayed the most favorable binding affinity with HER2 during molecular docking. These phytochemicals also possessed significant drug‐likeness characteristics. Furthermore, molecular dynamic simulation demonstrated stable interaction between these phytochemicals and HER2, suggesting a potential inhibitor of HER2, a crucial target in breast cancer treatment. Therefore, the present study offers an opportunity for further research and development of anticancer drugs derived from H. javanica. [ABSTRACT FROM AUTHOR]

Analysis of noncovalent interactions between natural products and proteins is important for rapid screening of active ingredients and understanding their pharmacological activities. In this work, the intensity fading MALDI‐TOF mass spectrometry (IF‐MALDI‐MS) method with improved reproducibility was implemented to investigate the binding interactions between saponins from Panax notoginseng and lysozyme. The benchmark IF‐MALDI‐MS experiment was established using N,N′,N″‐triacetylchitotriose‐lysozyme as a model system. The reproducibility of ion intensities in IF‐MALDI‐MS was improved by scanning the whole sample deposition with a focused laser beam. The relative standard deviation (RSD) of deposition scanning IF‐MALDI‐MS is 5.7%. Similar decay trends of the relative intensities of notoginseng saponins against increasing amounts of lysozyme were observed for all six notoginseng saponins. The half‐maximal fading concentration (FC50) was calculated to quantitatively characterize the binding affinity of each ligand based on the decay curve. According to the FC50 values obtained, the binding affinities of the six notoginseng saponins were evaluated in the following order: notoginsenoside S > notoginsenoside Fc > ginsenoside Rb1 > ginsenoside Rd > notoginsenoside Ft1 > ginsenoside Rg1. The binding order was in accordance with molecular docking studies, which showed hydrogen bonding might play a key role in stabilizing the binding interaction. Our results demonstrated that deposition scanning IF‐MALDI‐MS can provide valuable information on the noncovalent interactions between ligands and proteins. [ABSTRACT FROM AUTHOR]

Introduction: This research explores sustainable applications for waste generated from fenugreek (Trigonella foenum‐graecum), a plant with both nutritional and medicinal uses. The study specifically targets waste components as potential sources of nutrients and bioactive compounds. Objectives: The focus is to conduct detailed metabolic profiling of fenugreek waste, assess its anti‐inflammatory properties by studying its cyclooxygenase (COX) inhibitory effect, and correlate this effect to the metabolite fingerprint. Materials and Methods: Ethanolic extracts of fenugreek fruit pericarp and a combination of leaves and stems were subjected to untargeted metabolic profiling using liquid chromatography–mass spectrometry integrated with online database searches and molecular networking as an effective dereplication strategy. The study also scrutinized the COX inhibitory capabilities of these extracts and saponin‐rich fractions prepared therefrom. Molecular docking was employed to investigate the specific interactions between the identified saponins and COX enzymes. Results: The analysis led to the annotation of 81 metabolites, among which saponins were predominant. The saponin‐rich fraction of the fruit pericarp extract displayed the strongest COX‐II inhibitory activity in the in vitro inhibition assay (IC50 value of 81.64 ± 3.98 μg/mL). The molecular docking study supported the selectivity of the identified saponins towards COX‐II. The two major identified saponins, namely, proto‐yamogenin 3‐O‐[deoxyhexosyl (1 → 2)] [hexosyl (1 → 4)] hexoside 26‐O‐hexoside and trigofenoside A, were predicted to have the highest affinity to the COX‐II receptor site. Conclusion: In the present study, we focused on the identification of COX‐II inhibitory saponins in fenugreek waste through an integrated approach. The findings offer valuable insights into potential anti‐inflammatory and cancer chemoprotective applications of fenugreek waste. The ethanolic extracts of fenugreek wastes were subjected to LC‐MS/MS untargeted metabolic profiling and molecular networking, leading to the annotation of 81 metabolites, with saponins being major constituents. A saponin‐rich fraction was prepared from each waste extract. The COX inhibitory effect of the waste extracts and saponin‐rich fractions was evaluated. The saponin‐rich fractions showed a preferential COX‐II inhibition that was stronger than the ethanolic extracts. Molecular docking proved the selectivity of the identified saponins towards COX‐II enzyme. [ABSTRACT FROM AUTHOR]

Starfish provide important saponins with diverse bioactivities as the secondary metabolites, among which 2‐O‐glycosylated glycosides are commonly found. Preparation of those 1,2‐trans 2‐O‐glycosylated glycosides usually relies on 2‐O‐acyl participation requiring the selective installation and cleavage of 2‐O‐acyl groups. A convergent synthesis using 2‐O‐glycosylated oligosaccharide donors would be more straightforward but also pose greater challenges. Herein, we report a convergent synthesis of a distinctive tetrasaccharide isolated from starfish Asterias rollestoni Bell. Dual 2‐(diphenylphosphinoyl)acetyl (DPPA) groups at O3 and O4 on galactose moiety led to high β‐selectivities (β/α=12/1 or β only) in the challenging [2+2] glycosylation, giving the desired tetrasaccharides in >90 % yields from the 2‐O‐glycosylated disaccharide donors. These synthetic studies have also unambiguously revised the structure of these natural tetrasaccharides. This work would facilitate further studies on new inhibitors of α‐glucosidase as hypoglycemic drugs. [ABSTRACT FROM AUTHOR]

BACKGROUND: Foamulsions have become increasingly popular in the food industry due to their ability to enhance the textural, sensory and health‐promoting properties of food products. This study was therefore aimed to design and prepare a novel gelled structure, foamulsion gel containing 0–600 g L−1 oil, with gellan gum (GG; 7, 10 and 13 g L−1) and saponin‐rich antioxidant Acanthophyllum glandulosum extract (AGE; 2, 6 and 10 g L−1). RESULTS: The interaction between components was confirmed by infrared spectroscopy. The overrun and porosity of the foamulsion gels increased with antioxidant AGE (1.30 times) and reduced with oil (up to ca 70% and 30%, respectively) and GG levels. The systems were highly stable, and no water or oil was released during the physical stability experiments. Microscopic images showed that the size of air cells was significantly larger than that of oil droplets. The foamulsion gels based on 13 g L−1 GG and 10 g L−1 AGE had markedly higher elastic (G′) and viscous (G′′) moduli than other samples, and exhibited an elastic and solid‐like behavior (G′ > G′′). The highest gel firmness was found in oil‐free sample, and the presence of oil resulted in a lower firmness induced by the larger size and lubrication effect of oil droplets. CONCLUSION: As a result, the interactions between AGE, GG and oil could lead to the creation of new aerated structures known as bioactive foamulsion gels. These gels exhibit excellent foamability, stability and viscoelasticity and may find applications in the development of novel, healthy and low‐calorie aerated foods. © 2024 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

In contrast to its widespread traditional and popular culinary use to reduce weight, Vigna angularis (adzuki beans) was not subjected to sufficient scientific scrutiny. Particularly, its saponins whose role was never investigated before to unveil the beans' antidiabetic and anti‐obesity effects. Four vital pancreatic and intestinal carbohydrate enzymes were selected to assess the potency of the triterpenoidal saponins of V. angularis to bind and activate these proteins through high‐precision molecular modeling and dynamics mechanisms with accurate molecular mechanics Generalized Born Surface Area (MMGBSA) energy calculations; thus, recognizing their anti‐obesity potential. Our results showed that adzukisaponin VI and adzukisaponin IV were the best compounds in the α‐amylase and α‐glucosidase enzymatic grooves, respectively. Adzukisaponin VI and angulasaponin C were the best fitting in the N‐termini of sucrase‐isomaltose (SI) enzyme, and angulasaponin C was the best scoring compound in maltase‐glucoamylase C‐termini. All of them outperformed the standard drug acarbose. These compounds in their protein complexes were selected to undergo molecular simulations of the drug‐bound protein compared to the apo‐protein through 100 ns, which confirmed the consistency of binding to the key amino acid residues in the four enzyme pockets with the least propensity of unfolding. Detailed analysis is given of the different polar and hydrophobic binding interactions of docked compounds. While maltase–adzukisaponin VI complex scored the lowest MMGBSA free energy of −67.77 Kcal/mol, α‐amylase complex with angulasaponin B revealed the free binding energy of −74.18 Kcal/mol with a dominance of van der Waals energy (ΔEVDW) and the least change from the start to the end of the simulation time. This study will direct researchers to the significance of isolating the pure adzuki saponin components to conduct future in vitro and in vivo experimental works and even clinical trials. [ABSTRACT FROM AUTHOR]

Yupingfeng granules (YPFG) is commonly used in the treatment of immunological diseases, inflammations, and pulmonary diseases. Several studies have found that chromones, flavones, and saponins were the major bioactive compounds of YPFG. However, few studies have reported accurate quantification methods of these compounds. This study aimed to establish a simple and rapid method by using liquid chromatography–tandem mass spectrometry (LC–MS/MS) to determine 15 bioactive compounds in YPFG. The experimental parameters including extraction methods, extraction solvents, extraction time, solid–liquid ratio, and LC–MS/MS condition were optimized. The linearity, precision, repeatability, stability, and recovery of the established method were evaluated. The contents of 15 bioactive compounds in seven batches of YPFG samples were analyzed by the established method and the results were compared with the values determined by HPLC. The optimal extraction condition was to extract 0.1 g of YPFG by ultrasound with 50 mL 50% ethanol for 30 min. A Waters ACQUITY UPLCBEH C18 column using the 0.1% formic acid water solution and acetonitrile as mobile phase with a gradient elution was applied to the chromatographic separation. The linearity, precision, repeatability, stability, and recovery of the method were within acceptable ranges. Compared with HPLC analysis methods in Chinese Pharmacopoeia and literature, the established method was faster, simpler, more accurate, and more reliable. The method of simultaneous determination of 15 components in YPFG by LC–MS might provide a basis for the study of the bioactive compounds and the improvement of the quality standard of YPFG. [ABSTRACT FROM AUTHOR]

An effective method by high‐speed countercurrent chromatography coordinated with silver nitrate for the preparative separation of sterones and triterpenoid saponins from Achyranthes bidentata Blume was developed. Methyl tert‐butyl ether/n‐butanol/acetonitrile/water (4:2:3:8, v/v/v/v) was selected for 20‐hydroxyecdysone (compound 1), chikusetsusaponin IVa methyl ester (compound 4), 2′‐glycan‐11‐keto‐pigmented saponin V (compound 5), as well as a pair of isomers of 25S‐inokosterone (compound 2) and 25R‐inokosterone (compound 3), which were further purified by silver nitrate coordinated high‐speed countercurrent chromatography. What is more, dichloromethane/methanol/isopropanol/water (6:6:1:4, v/v/v/v) was applied for calenduloside E (compound 6), 3β‐[(O‐β‐d‐glucuronopyranosyl)‐oxy]‐oleana‐11,13‐dien‐28‐oic acid (compound 7), zingibroside R1 (compound 8) and chikusetsusaponin IVa (compound 9). Adding Ag+ to the solvent system resulted in unique selectivity for 25R/25S isomers of inokosterone, which increased the complexing capability and stability of Ag+ coordinated 25S‐inokosterone, as well as the α value between them. These results were further confirmed by the computational calculation of geometry optimization and frontier molecular orbitals assay. Comprehensive mass spectrometry and nuclear magnetic resonance analysis demonstrated the structures of the obtained compounds. [ABSTRACT FROM AUTHOR]

This review highlights the increasing interest in one of the natural compounds called saponins, for their potential therapeutic applications in addressing inflammation which is a key factor in various chronic diseases. It delves into the molecular mechanisms responsible for the anti‐inflammatory effects of these amphiphilic compounds, prevalent in plant‐based foods and marine organisms. Their structures vary with soap‐like properties influencing historical uses in traditional medicine and sparking renewed scientific interest. Recent research focuses on their potential in chronic inflammatory diseases, unveiling molecular actions such as NF‐κB and MAPK pathway regulation and COX/LOX enzyme inhibition. Saponin‐containing sources like Panax ginseng and soybeans suggest novel anti‐inflammatory therapies. The review explores their emerging role in shaping the gut microbiome, influencing composition and activity, and contributing to anti‐inflammatory effects. Specific examples, such as Panax notoginseng and Gynostemma pentaphyllum, illustrate the intricate relationship between saponins, the gut microbiome, and their collective impact on immune regulation and metabolic health. Despite promising findings, the review emphasizes the need for further research to comprehend the mechanisms behind anti‐inflammatory effects and their interactions with the gut microbiome, underscoring the crucial role of a balanced gut microbiome for optimal health and positioning saponins as potential dietary interventions for managing chronic inflammatory conditions. [ABSTRACT FROM AUTHOR]

Background: Hyperlipidemia is characterized by abnormally elevated blood lipids. Quinoa saponins (QS) have multiple pharmacological activities, including antitumor, bactericidal and immune‐enhancing effects. However, the lipid‐lowering effect and mechanisms of QS in vivo have been scarcely reported. Methods: The effect of QS against hyperlipidemia induced by high‐fat diet in rats was explored based on gut microbiota and serum non‐targeted metabolomics. Results: The study demonstrated that the supplementation of QS could reduce serum lipids, body weight, liver injury and inflammation. 16S rRNA sequencing demonstrated that QS mildly increased alpha‐diversity, altered the overall structure of intestinal flora, decreased the relative richness of Firmicutes, the ratio of Firmicutes/Bacteroidetes (P < 0.05) and increased the relative richness of Actinobacteria, Bacteroidetes, Bifidobacterium, Roseburia and Coprococcus (P < 0.05). Simultaneously, metabolomics analysis showed that QS altered serum functional metabolites with respect to bile acid biosynthesis, arachidonic acid metabolism and taurine and hypotaurine metabolism, which were closely related to bile acid metabolism and fatty acid β‐oxidation. Furthermore, QS increased protein levels of farnesoid X receptor, peroxisome proliferator‐activated receptor α and carnitine palmitoyltransferase 1, which were related to the screened metabolic pathways. Spearman correlation analysis showed that there was a correlation between gut microbiota and differential metabolites. Conclusion: QS could prevent lipid metabolism disorders in hyperlipidemic rats, which may be closely associated with the regulation of the gut microbiota and multiple metabolic pathways. This study may provide new evidence for QS as natural active substances for the prevention of hyperlipidemia. © 2023 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

Acne vulgaris represents a chronic inflammatory condition, the pathogenesis of which is closely associated with the altered skin microbiome. Recent studies have implicated a profound role of Gram‐negative bacteria in acne development, but there is a lack of antiacne agents targeting these bacteria. Polyphyllins are major components of Rhizoma Paridis with great anti‐inflammatory potential. In this study, we aimed to evaluate the antiacne effects and the underlying mechanisms of PPH and a PPH‐enriched Rhizoma Paridis extract (RPE) in treating the Gram‐negative bacteria‐induced acne. PPH and RPE treatments significantly suppressed the mRNA and protein expressions of interleukin (IL)‐1β and IL‐6 in lipopolysaccharide (LPS)‐induced RAW 264.7 and HaCaT cells, along with the intracellular reactive oxygen species (ROS) generation. Furthermore, PPH and RPE inhibited the nuclear translocation of nuclear factor kappa‐B (NF‐κB) P65 in LPS‐induced RAW 264.7 cells. Based on molecular docking, PPH could bind to kelch‐like ECH‐associated protein 1 (KEAP1) protein. PPH and RPE treatments could activate nuclear factor erythroid 2‐related factor 2 (NRF2) and upregulate haem oxygenase‐1 (HO‐1). Moreover, RPE suppressed the mitogen‐activated protein kinase (MAPK) pathway. Therefore, PPH‐enriched RPE showed anti‐inflammatory and antioxidative effects in vitro, which is promising for alternative antiacne therapeutic. [ABSTRACT FROM AUTHOR]

Drug development for atherosclerosis, the underlying pathological state of ischemic cardiovascular diseases, has posed a longstanding challenge. Saponins, classified as steroid or triterpenoid glycosides, have shown promising therapeutic potential in the treatment of atherosclerosis. Through an exhaustive examination of scientific literature spanning from May 2013 to May 2023, we identified 82 references evaluating 37 types of saponins in terms of their prospective impacts on atherosclerosis. These studies suggest that saponins have the potential to ameliorate atherosclerosis by regulating lipid metabolism, inhibiting inflammation, suppressing apoptosis, reducing oxidative stress, and modulating smooth muscle cell proliferation and migration, as well as regulating gut microbiota, autophagy, endothelial senescence, and angiogenesis. Notably, ginsenosides exhibit significant potential and manifest essential pharmacological attributes, including lipid‐lowering, anti‐inflammatory, anti‐apoptotic, and anti‐oxidative stress effects. This review provides a comprehensive examination of the pharmacological attributes of saponins in atherosclerosis, with particular emphasis on their role in the regulation of lipid metabolism regulation and anti‐inflammatory effects. Thus, saponins may warrant further investigation as a potential therapy for atherosclerosis. However, due to various reasons such as low oral bioavailability, the clinical application of saponins in the treatment of atherosclerosis still needs further exploration. [ABSTRACT FROM AUTHOR]

An Indian traditional medicinal plant, Boerhaavia diffusa (Punarnava), is reported for its diuretic activity and helps in impaired kidney function. The present study indicates that alkaloids, carbohydrates, saponins, phytosterols, flavonoids, and glycosides are absent in the petroleum ether extract and present chiefly in the methanolic extract of roots. The phytosterols were found to be present in the ethyl acetate extract, while other phytochemical constituents, that is, alkaloids, carbohydrates, saponins, flavonoids, and glycosides, were absent. From high‐performance thin‐layer chromatography, the results indicated that out of all the three extracts and two marketed formulations, ethyl acetate root extract (LEA) has the highest amount of Boeravinone B content. Further, different root extracts of B. diffusa and two marketed formulations were evaluated on the human embryonic kidney cell line to understand pharmacological safety. From the results, it was observed that LEA and petroleum ether root extracts showed a higher percentage of cell survival and a better safety profile up to the dose of 1 mg/mL. The overall results indicated that further preclinical evaluation of B. diffusa is needed to understand the mechanism behind nephroprotective potential which can further expedite the drug discovery process of nephroprotective molecules. [ABSTRACT FROM AUTHOR]

In the present study, twelve compounds from Dioscorea spongiosa were successfully purified by an efficient technique combined bioassay‐guided fractionation macroporous resin column chromatography (MRCC) pretreatment and high‐speed counter‐current chromatography (HSCCC) separation for the first time. Then, D101 MRCC was used to fractionate the crude extract into five parts, which further applied the bioassay‐guided fractionation strategy to screen the active fractions of 2 and 4. As for the separation, 200 mg Fr.2 was purified by HSCCC using EtOAc/n‐BuOH/H2O (2:2:3, v/v), leading to annulatomarin (1), dioscoresides C (2), diosniponol C (3), methyl protodioscin (4), pseudoprotodioscin (5), protogracillin (6), as well as 200 mg Fr.4 yielding montroumarin (7), dioscorone A (8), diosniponol D (9), protodioscin (10), gracillin (11), and dioscin (12) using CH2Cl2/MeOH/H2O (3:3:2, v/v) with the purities over 95.0%. Finally, the isolates were assayed for their anti‐inflammatory, urico‐lowering, and anti‐diabetic activities in vitro, which indicated that the steroidal saponins of 5, 6, and 11 showed all these three activities. [ABSTRACT FROM AUTHOR]

Ischemic stroke is one of the leading causes of death and disability among adults worldwide. Intravenous thrombolysis is the only approved pharmacological treatment for acute ischemic stroke. However, reperfusion by thrombolysis will lead to the rapid activation of microglia cells which induces interferon‐inflammatory response in the ischemic brain tissues. Panax quinquefolium saponins (PQS) has been proven to be effective in acute ischemic stroke, but there is no unified understanding about its specific mechanism. Here, we will report for the first time that PQS can significantly inhibit the activation of microglia cells in cerebral of MCAO rats via activation of Nrf2/miR‐103‐3p/TANK axis. Our results showed that PQS can directly bind to Nrf2 protein and inhibit its ubiquitination, which result in the indirectly enhancing the expression of TANK protein via transcriptional regulation on miR‐103‐3p, and finally to suppress the nuclear factor kappa‐B dominated rapid activation of microglial cells induced by oxygen–glucose deprivation/reoxygenation vitro and cerebral ischemia‐reperfusion injury in vivo. In conclusion, our study not only revealed the new mechanism of PQS in protecting against the inflammatory activation of microglia cells caused by cerebral ischemia‐reperfusion injury, but also suggested that Nrf2 is a potential target for development of new drugs of ischemic stroke. More importantly, our study also reminded that miR‐103‐3p might be used as a prognostic biomarker for patients with ischemic stroke. [ABSTRACT FROM AUTHOR]

Diabetes mellitus (DM) is one of the most prevalent, fatal, and non‐contagious diseases. Therefore, researchers are making attempts to develop novel anti‐diabetic drugs using various organic compounds and biomolecules. The idea of using nano‐materials as anti‐diabetic agents seems interesting. The current study aims to develop Kickxia elatine (KE) extract‐based nano‐silver (KE‐AgNPs) and to evaluate their in vivo anti‐diabetic potency in female Sprague Dawley rats. KE‐AgNPs were characterized using UV spectroscopy, X‐ray diffractometer (XRD), scanning electron microscopy (SEM), Electron Diffraction X‐ray Spectroscopy (EDX), and Fourier transforms infrared (FTIR) techniques. The crystalline nature of KE‐AgNPs with a size of 42.47 nm is confirmed by XRD screening. Spherical‐shaped mono‐dispersed KE‐AgNPs with a mean size of 50 nm are validated by SEM examination. The different phyto‐compounds (tannins, alkaloids, flavonoids, proteins, saponins, phenols, carbohydrates, quinones, sterols, fats, and oils) that contribute to the stabilization and reduction of KE‐AgNPs are confirmed by FTIR analysis. EDX showed a strong peak (3.2 keV) that identified Ag as the main component with a 61.67% contribution. The use of Alloxan to induce diabetes resulted in elevated levels of blood sugar, HbA1c, liver, and lipid profile, as well as a drastic reduction in body weight, body organ weight, and Hemoglobin. These modifications were switched following 21 days of treatment of diabetic rats, and a dosage range of 150–450 mg kg−1 BW of KE extract and KE‐AgNPs demonstrated significant inhibition as compared with the diabetic untreated group. The phytochemical analysis of the KE plant was also assessed to examine the phyto‐compounds involved in the anti‐diabetic potential of KE extract and KE‐AgNPs. These findings suggested that, in comparison with the KE extract, KE‐AgNPs have demonstrated promising anti‐diabetic action. [ABSTRACT FROM AUTHOR]

Several industrial fields use emulsifiers in their products, with the ones of natural origin gaining increasing relevance. Identifying and using diversified sources for their extraction is a pertinent topic regarding sustainability principles, biodiversity preservation, or cost rationalization. This is the case of Quillaja bark saponin (QS), for which saponin‐rich extracts, for example, Tribulus terrestris (TT), are being highlighted as viable alternatives, even though constraints like performance are still on the table. In this context, an experimental design using binary emulsifier mixtures of TT with pure QS was carried out by changing their composition (50–90%wt. TT), content (1.5–4.5%wt.), and high‐pressure homogenization conditions (5–15 cycles). The emulsions were characterized by zeta potential, morphology, droplet size, and stability (expressed as the number of days without creaming formation). Moreover, the cream index for 30 days was determined to indicate the destabilization extent. The zeta potential showed stable emulsions (values below −41 mV); even still, creaming formed for samples using a low emulsifier and high TT contents. The emulsions' mean droplet diameter (D [3, 2]) was between 78 and 921 nm, with smaller sizes agreeing with higher stability. The statistical analysis indicated an optimum composition range comprising an emulsifier content between 3.9 and 4.5%wt. and TT content between 50 and 56%wt. to reach stable products. Overall, TT can provide an effective solution when combined with QS, decreasing the dependence on Quillaja bark. [ABSTRACT FROM AUTHOR]

Diabetic retinopathy (DR) is one of the most frequently occurring diabetic complications associated with inflammation and oxidative stress. Platycodin D (PLD) is a bio‐active saponin that has been reported to exhibit anti‐inflammation, anti‐oxidative, and antidiabetic activities. Therefore, we speculated the protective effects of PLD on DR in the present study. Our results demonstrated that PLD attenuated high glucose (HG)‐induced inflammation, as evidenced by decreased production of TNF‐α, IL‐1β, IL‐6. The HG‐induced oxidative stress was prevented by PLD with decreased ROS production and malondialdehyde (MDA) level, as well as increased activities of superoxide dismutase and glutathione (GSH). In addition, treatment of PLD significantly decreased the apoptotic rate in HG‐induced ARPE‐19 cells. The HG‐caused increases in expression of bax and cleaved capsase‐3, as well a decrease in bcl‐2 expression were attenuated by PLD. Furthermore, PLD suppressed the activation of TLR4/MyD88/NF‐κB and enhanced the activation of Nrf2/HO‐1 pathway in HG‐induced ARPE‐19 cells. Additionally, overexpression of TLR4 attenuated the anti‐inflammatory, while knockdown of Nrf2 reversed the anti‐oxidative and anti‐apoptotic activities of PLD in HG‐stimulated ARPE‐19 cells. Furthermore, PLD attenuates retinal damage in DR rats. Finally, we demonstrated that PLD weakened the TLR4/MyD88/NF‐κB p65 pathway and promoted the Nrf2/HO‐1 pathway in vivo. Taken together, these findings indicated that PLD exerted protective effects against DR, which were attributed to the regulation of TLR4/MyD88/NF‐κB and Nrf2/HO‐1 signaling pathways. [ABSTRACT FROM AUTHOR]

Simiao pill is one of the most commonly used prescriptions in traditional Chinese medicine for the treatment of hyperuricemia and gout. However, methods based on more accurate and comprehensive qualitative and quantitative analyses of the active ingredients are not yet perfect due to limited methodology. This not only hinders the elucidation of the pharmacological mechanism of Simiao pill, but also its comprehensive clinical development and utilization. In this study, we employed ultra‐high‐performance liquid chromatography‐Q Exactive Orbitrap‐mass spectrometry technology to perform rapid analysis and identification of the chemical constituents in Simiao pill. A total of 101 chemical components were identified, including 26 alkaloids, 15 terpenoids, 11 flavonoids, eight steroids, six fatty acids, five limonoids, four saponins, five phenylpropanoids, and 21 other compounds. In addition, we established a new method by high‐throughput ultra‐high‐performance liquid chromatography‐Q Exactive Orbitrap‐mass spectrometry combined with ultra‐high‐performance liquid chromatography‐triple quadrupole‐tandem mass spectrometry technology for quantification of 14 main active ingredients, such as adenosine (1), phellodendrine (2), mangnoflorine (3), β‐ecdysterone (4), 25R‐inokosterone (5), 25S‐inokosterone (6), jatrorrhizine (7), palmatine (8), chikusetsu saponin IVa (9), limonin (10), atractylenolide III (11), atractylenolide I (12), obacunone (13), and atractylenolide II (14) in Simiao pill. This work laid a foundation for further analysis and quality control of effective components in Simiao pill. [ABSTRACT FROM AUTHOR]

Lingbao Huxin Dan (LBHX) is an effective prescription for treating various cardiovascular diseases. However, its systematic chemical composition analysis and important marker components remain unclear, which hinders the development of standards or guidelines for quality evaluation. Herein, a high‐resolution and efficient method was established to comprehensively investigate the chemical ingredients and metabolites of LBHX by using gas chromatography‐tandem mass spectrometry and ultra‐high‐performance liquid chromatography coupled with quadrupole time‐of‐flight mass spectrometry. AutoDock Vina was applied to conduct visual screening for identifying potential active compounds targeting two important sick sinus syndrome‐associated proteins. As a result, 53 volatile compounds, as well as 191 non‐volatile chemical components, including bufadienolides, diterpenoids, bile acids, phenolic acids, and triterpenoid saponins, were unambiguously characterized or tentatively identified. Fifty prototypes and 62 metabolites were identified in the plasma of rats, whilst metabolism reactions included phase I reactions (hydrolysis, oxidation, and hydroxylation) and phase II reactions (glucuronidation and methylation). Eleven compounds with good binding affinity have been observed by docking with key proteins. It is the first systematic study on the pharmacodynamic material basis of LBHX and the result consolidates the foundation for further study regarding the mechanism in treating cardiovascular diseases. [ABSTRACT FROM AUTHOR]

Throughout the world, the prevalence of metabolic diseases in general and type 2 diabetes (T2DM) in particular is constantly growing, and sub‐Saharan Africa (SSA) is not spared. The use of functional foods is a more practical option among the different approaches used in the management of T2DM owing to the fact that they are relatively less costly, safer, and more accessible. In addition to their low glycemic index just like foods currently used to manage diabetes, functional foods contain bioactive compounds such as polyphenols, dietary fibers, saponins, and peptides. They are so named because they have additional health advantages beyond their basic nutritional worth. Bioactive compounds can be found in a variety of SSA plant‐based foods, such as spices, fruits, vegetables, legumes, starchy foods, prepared foods, mixed foods, and prepared dishes. The goal of this review is to highlight some of the investigations into the effectiveness of local food and their antidiabetic mechanisms that have been studied in various SSA regions. Using the literature review as a basis, the authors state that SSA foods are rich in various bioactive compounds capable of regulating blood sugar through enhanced glucose tolerance, antioxidant effects, insulin sensitivity, and inhibition or activation of some key enzymes of the glucose metabolism that are linked to the prevention and management of T2DM. Many of the cited findings are preliminary, obtained from cell and preclinical studies, and therefore other studies need to be done to demonstrate the full potential of these foods to serve as bases for dietary guidelines. [ABSTRACT FROM AUTHOR]

Dry pea (Pisum sativum) seeds are valuable sources of plant protein, dietary fiber, and starch, but their uses in food products are restricted to some extent due to several off‐flavor compounds. Saponins are glycosylated triterpenoids and are a major source of bitter, astringent, and metallic off‐flavors in pea products. β‐amyrin synthase (BAS) is the entry point enzyme for saponin biosynthesis in pea and therefore is an ideal target for knock‐out using CRISPR/Cas9 genome editing to produce saponin deficient pea varieties. Here, in an elite yellow pea cultivar (CDC Inca), LC/MS analysis identified embryo tissue, not seed coat, as the main location of saponin storage in pea seeds. Differential expression analysis determined that PsBAS1 was preferentially expressed in embryo tissue relative to seed coat and was selected for CRISPR/Cas9 genome editing. The efficiency of CRISPR/Cas9 genome editing of PsBAS1 was systematically optimized in pea hairy roots. From these optimization procedures, the AtU6‐26 promoter was found to be superior to the CaMV35S promoter for gRNA expression, and the use of 37°C was determined to increase the efficiency of CRISPR/Cas9 genome editing. These promoter and culture conditions were then applied to stable transformations. As a result, a bi‐allelic mutation (deletion and inversion mutations) was generated in the PsBAS1 coding sequence in a T1 plant, and the segregated psbas1 plants from the T2 population showed a 99.8% reduction of saponins in their seeds. Interestingly, a small but statistically significant increase (~12%) in protein content with a slight decrease (~5%) in starch content was observed in the psbas1 mutants under phytotron growth conditions. This work demonstrated that flavor‐improved traits can be readily introduced in any pea cultivar of interest using CRISPR/Cas9. Further field trials and sensory tests for improved flavor are necessary to assess the practical implications of the saponin‐free pea seeds in food applications. [ABSTRACT FROM AUTHOR]

Our previous studies confirmed the efficacy of gross saponins of Tribulus terrestris L. fruit in treating cerebral ischemia. This study aimed to investigate the related mechanisms in vitro. The lipopolysaccharide‐induced BV2 cells model was constructed and treated with gross saponins at different concentrations to explore its anti‐inflammatory activity. The cell metabolite changes were tracked by liquid chromatography‐mass spectrometry (LC‐MS)‐based metabolomics, and the metabolic biomarkers and related metabolic pathways were analyzed. Molecular biochemistry analysis was further used to verify the relevant inflammatory pathways. The results showed that the saponins reduced nitric oxide release and the secretion of tumor necrosis factor‐alpha, interleukin‐1β, and interleukin‐6 from lipopolysaccharide‐induced BV2 cells. Metabolic perturbations occurred in lipopolysaccharide‐treated BV2 cells, which could be reversed by drug treatment via mainly regulating glycerophospholipid metabolism, tryptophan metabolism, purine metabolism pathways, etc. The western blot analysis demonstrated that saponin could suppress the activation of the inflammatory‐related signaling pathway. The present study explored the in vitro anti‐inflammatory mechanism of gross saponins of Tribulus terrestris L. fruit using an LC‐MS‐based cell metabolomics approach, which confirms the great potential of LC‐MS for drug efficacy evaluation and can be applied in other herbal medicine‐related analyses. [ABSTRACT FROM AUTHOR]

The interest in bioactives especially from botanicals to treat vancomycin‐resistant enterococcal (VRE) infections is increased. Many species of Ocimum have a long history in folk medicinal and food industries. Nevertheless, their bioactive compounds remain unexplored. This study is aimed to assess the antimicrobial and antioxidant activity of basil leaf extract prepared using ethanol, methanol, and water. The ethanol and methanol extract have all the phytochemicals (alkaloids, flavonoids, phenolic compounds, tannins, saponins, quinones, carbohydrates, and proteins) except steroids and terpenoids. In addition to steroids and terpenoids, tannin was also absent in the aqueous extract. Total phenolic and flavonoid content was high in ethanol and followed by methanol and aqueous extract. Similarly, ethanol and methanol extract showed strong antimicrobial activity against VRE and MTCC strains at a concentration of 20 mg/mL than aqueous extract. Among the 10 indicators, Staphylococcus aureus is highly susceptible to ethanol extract at a concentration of 8 mg/mL and followed by other MTCC strains. Vancomycin‐resistant enterococci pathogens were inhibited at the minimum inhibitory concentration of 14, 16, and 20 mg/mL of ethanol, methanol, and aqueous extract. Further, on the basis of determining the absorbing material (nucleic acid and protein) at 260 nm and scanning electron microscopic, it was confirmed that the loss of cell membrane integrity and cell membrane damage were the effective mechanisms of plant extract antimicrobial activity. All three solvents have shown remarkable antioxidant activity. Gas chromatography–mass spectrometry analysis of basil leaves ethanol extract identified 19 compounds with various therapeutic and food applications. [ABSTRACT FROM AUTHOR]

Moringa oleifera is an important medicinal plant in several countries; for example, Nigeria, the USA, Turkey, Germany, Greece, and Ukraine. The abundant bioactive and nutritional properties of this plant make it useful in many and diverse areas of life, including the health, cosmetic, agricultural, and food industries to mention but a few. Research has found that the presence of proteins, carbohydrates, lipids, vitamins, minerals, flavonoids, phenols, alkaloids, fatty acids, saponins, essential oils, folate, aromatic hydrocarbons, sterols, glucosinolates, and glycosides, among others, characterize the moringa nutrient profile and, as a result, give rise to its remedial effects on ailments such as wounds, stomach and duodenal ulcers, allergies, obesity, diabetes, inflammation, asthma, and so on. It is the aim of this review to provide an insight into such medicinal and pharmacological remedies attributed to moringa, stating both the past and recent discoveries. This review article also takes a look into the botanical features, bioactive compounds, antinutrients, food applications, bacterial fermentation products, biosafety, industrial applications, and other uses of moringa. Finally, with the belief that knowledge is progressive, we acknowledge that there are things yet undiscovered about this wonder plant that will be of value both to medicine and general life; we therefore recommend that research work continues on the moringa plant. © 2023 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

Diabetic nephropathy is a major complication of diabetes mellitus and is related to dysfunction of renal cells. Hederagenin is a triterpenoid saponin from some Chinese herbs with anti‐inflammatory and anti‐diabetic activities. However, its role in diabetic nephropathy progression is still obscure. This study aimed to explore the effects of hederagenin on renal cell dysfunction in vitro. Human renal mesangial cells (HRMCs) and human renal proximal tubular epithelial cells (HRPTEpiCs) were cultured under high glucose (HG) conditions to mimic diabetic nephropathy‐like injury. Cell proliferation was evaluated by CCK‐8. mRNA and protein levels were determined by qRT‐PCR and western blotting, respectively. The secretion levels of fibrosis‐related biomarkers were analyzed by ELISA. Results showed that hederagenin reduced HG‐induced proliferation increase in HRMCs and HRPTEpiCs. Hederagenin attenuated HG‐induced increase in mRNA and protein expression of NLRP3, ASC, and IL‐1β. Hederagenin also suppressed HG‐induced increase in mRNA and secretion levels of FN, Col. IV, PAI‐1, and TGF‐β1. NLRP3 inhibitor MCC950 attenuated HG‐induced fibrosis of renal cells, and its activator nigericin reversed the suppressive effect of hederagenin on HG‐induced fibrosis. Bioinformatics analysis predicted cathepsin B (CTSB) as a target of hederagenin to modulate NOD‐like receptor (NLR) pathway. Hederagenin decreased CTSB level, and CTSB overexpression reversed the suppressive effect of hederagenin on HG‐induced NLRP3 inflammasome activation and fibrosis in HRMCs and HRPTEpiCs. In conclusion, hederagenin attenuates HG‐induced fibrosis of renal cells by inhibiting NLRP3 inflammasome activation via reducing CTSB expression, indicating a therapeutic potential of hederagenin in diabetic nephropathy. [ABSTRACT FROM AUTHOR]

The antidiabetic activity of saponins extracted from Momordica charantia (MCS) on streptozotocin‐induced diabetic mice was investigated in order to elucidate the mechanism of MCS for exerting hypoglycemic effects. Saponins were first extracted from M. charantia L. and their composition was analyzed. The diabetic Kunming mice were fed low‐dose saponins from M. charantia L. and high‐dose MCS, using normal mice and diabetic mice as controls. Body weight, blood glucose level, oral glucose tolerance, serum C‐peptide level, hepatic antioxidant capacity, hepatic glycogen and hexokinase in liver tissues, serum blood lipid level, and alpha‐glucosidase activity in small intestines were measured, and microstructure of pancreatic islet was analyzed. The results showed that the total content of seven triterpenoid compounds in MCS was 18.24 μg/mg, with Momordicoside K having the highest content at 11.66 μg/mg. Diabetic mice treated with MCS at 100 and 200 mg/kg body weight daily for 30 days showed a maximum glucose reduction (p <.05) of 12.63% and 26.47%, respectively. MCS significantly decreased levels of postprandial hyperglycemia, serum lipid, α‐glucosidase activity, and liver malondialdehyde. Additionally, levels of serum C‐peptide and liver glycogen, as well as hexokinase and antioxidant enzyme activity, were significantly increased compared to the diabetic control groups. Histopathological results showed that MCS markedly reduced degenerative changes in islet β‐cells. It is concluded that MCS exerts antidiabetic effects by improved hypoglycemic, hypolipidemic, and antioxidant effects, increased hexokinase activity and glycogen synthesis, and enhanced reparative effects on the histological architecture and insulin secretion function of the pancreas. [ABSTRACT FROM AUTHOR]

The effects of two fermentation processes (common fermentation with Saccharomyces cerevisiae and fermentation by Lacticaseibacillus casei subsp. casei PTCC 1608 and Lactiplantibacillus plantarum subsp. plantarum PTCC 1745) on pH, titratable acidity, total phenolic and flavonoid contents, antioxidant capacity, saponin content, as well as phytic acid content of quinoa dough were investigated during the 24‐h fermentation (4‐h interval). According to the results, the highest titratable acidity was observed in the samples fermented by L. casei subsp. casei. Moreover, the highest antioxidant capacity was observed after 12 h of fermentation by L. plantarum subsp. plantarum (31.22% for DPPH, 104.67% for FRAP) due to a higher concentration of phenolic compounds produced (170.5% for total phenolic content). Also, all samples have been able to reduce saponin by 67% on average. Furthermore, the samples fermented by L. plantarum subsp. plantarum showed the most significant decrease in phytic acid content (64.64%) during 24‐h fermentation. By considering the reduction of the antinutritional compounds and improvement in the antioxidant properties of quinoa flour, the Lactiplantibacillus plantarum strain was recommended. [ABSTRACT FROM AUTHOR]

The purpose of this review is to explore the underutilized and underexploited Burmese grape (Baccaurea ramiflora) as a valuable plant food crop grown in the northeastern region of India. Despite its seasonal availability, this fruit is used in various culinary applications and local delicacies. It is noteworthy for its abundant natural bioactive compounds that offer diverse health benefits. These bioactive compounds have demonstrated properties such as anti‐inflammatory, antiobesity, cytotoxic, and antidiabetic effects. This review compiles and analyzes the most recent research findings concerning the bioactive compounds found in Burmese grape's leaves, fruit, and seeds. Additionally, it investigates the physicochemical properties and nutritional composition of the fruit pulp and seed oil. The synthesis of this information provides a comprehensive understanding of the plant's phytochemical content, including essential components like vitamin C, iron, potassium, alkaloids, saponins, and phenolic acids, which contribute to its medicinal and health‐promoting attributes. The results presented in this review shed light on the potential applications of the Burmese grape and its bioactive compounds in various industrial sectors. With the growing interest in functional and nutraceutical products, the insights gathered here offer promising opportunities for leveraging the nutritional and health‐enhancing benefits of this fruit in the food and pharmaceutical industries. [ABSTRACT FROM AUTHOR]

In recent years, saponins have increasingly attracted researchers' attention owing to their multiple biological activities such as antifungal, cytotoxic, immunomodulatory and antimicrobial effects. In this study, targeted biologically active saponins from Cephalaria species were obtained by extraction, isolation and purification processes; additionally, the structures of saponins were elucidated by advanced spectroscopic methods. Optimisation studies were performed by using a UV–Vis spectrophotometer on three different saponins namely, elmalienoside B, sumbulianoside A and α‐hederin, isolated from Cephalaria species. The α‐hederin saponin‐loaded chitosan nanoparticles (SPCSNPs) were synthesised by employing an ionic gelation technique; subsequently, they were characterised. The encapsulation efficiency, loading capacity, and particle size of SPCSNPs were found to be 38 %, 3.7 % and 183.00±41.01 nm, respectively. In vitro cytotoxicity studies were conducted on SHSY‐5Y, CCD34LU, Panc‐1, PC‐3 and HL‐60 cell lines. When looking at the cytotoxic efficacy of SPCSNPs measured in percentage (3.65 %) in all cell lines, it was found that the efficacy of SPCSNPs was significantly higher than that of pure saponin. Consequently, the bioavailability and stability of biologically active saponins may increase thanks to the chitosan drug delivery system synthesized in this study and it is evident that saponin based chitosan nanoparticles have potential candidate for cancer researches. [ABSTRACT FROM AUTHOR]

A selective and sensitive ultra‐high‐performance liquid chromatography‐tandem mass spectrometry method was developed and validated for the determination of three triterpenoid saponins isolated from Astragalus membranaceus leaf extract. In this article, a method for simultaneous determination of Huangqiyenin A, Huangqiyenin E, and Huangqiyenin K was established for the first time. The method was successfully applied to the pharmacokinetic study of Astragalus membranaceus leaf extract after oral administration. Liquid–liquid extraction was applied to plasma sample preparation. Multiple reaction monitoring mode with an electrospray ion source in positive electrospray ionization was chosen to quantify the analytes. Chromatographic separation was performed on a Waters HSS T3 column, using gradient elution with a mobile phase composed of acetonitrile and 5 mM ammonium acetate/water. The pharmacokinetic results showed that all three compounds had the characteristics of rapid absorption‐slow metabolism trend. The time of maximum plasma concentration of Huangqiyenin A is higher than Huangqiyenin E and Huangqiyenin K. And the maximum plasma concentration of Huangqiyenin A is higher as well. The pharmacokinetic results revealed the pharmacokinetic characteristics of the three analytes in rat plasma, which could provide a helpful reference for the further study of Astragalus membranaceus leaf extract. [ABSTRACT FROM AUTHOR]

BACKGROUND: Recovery of high‐purity tea saponin (TS), a promising non‐ionic surfactant with well‐documented properties, is one of the major challenges to broadening its industrial applications. In this study, an innovative and sustainable strategy for the highly‐efficient purification of TS was developed by using well‐designed highly‐porous polymeric adsorbents. RESULTS: The prepared Pp‐A with controllable macropores (~96 nm) and appropriate surface hydrophobic properties was found more favorable for achieving high adsorption efficiency towards TS/TS‐micelles. Kinetic results showed the adsorption follows the pseudo‐second‐order model (R2 = 0.9800), and the Langmuir model is more qualified to explicate the adsorption isotherms with Qe‐TS ~ 675 mg g−1. Thermodynamic studies revealed the monolayer adsorption of TS was an endothermic process that was conducted spontaneously. Interestingly, ethanol‐driven desorption (90% v/v ethanol) of TS was rapidly (< 30 min) complete due to the possible ethanol‐mediated disassembling of TS‐micelles. A possible mechanism that involves the interactions between the adsorbents and TS/TS‐micelles, the formation and disassembling of TS‐micelles was proposed to account for the highly efficient purification of TS. Afterwards, Pp‐A‐based adsorption method was developed to purify TS directly from industrial camellia oil production. Through selective adsorption, pre‐washing, and ethanol‐driven desorption, the applied Pp‐A enabled the direct isolation of high‐purity TS (~96%) with a recovery ratio > 90%. Notably, Pp‐A exhibited excellent operational stability and is of high potential for long‐term industrial application. CONCLUSION: Results ensured the practical feasibility of the prepared porous adsorbents in purifying TS, and the proposed methodology is a promising industrial‐scale purification strategy. © 2023 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

SUMMARY: Steroidal saponins are a class of specialized metabolites essential for plant's response to biotic and abiotic stresses. They are also important raw materials for the industrial production of steroid drugs. Steroidal saponins are present in some monocots, such as Dioscorea and Paris, but their distribution, origin, and evolution in plants remain poorly understood. By reconstructing the evolutionary history of the steroidal saponin‐associated module (SSAM) in plants, we reveal that the steroidal saponin pathway has its origin in Asparagus and Dioscorea. Through evaluating the distribution and evolutionary pattern of steroidal saponins in angiosperms, we further show that steroidal saponins originated multiple times in angiosperms, and exist in early diverged lineages of certain monocot lineages including Asparagales, Dioscoreales, and Liliales. In these lineages, steroidal saponins are synthesized through the high copy and/or high expression mechanisms of key genes in SSAM. Together with shifts in gene evolutionary rates and amino acid usage, these molecular mechanisms shape the current distribution and diversity of steroidal saponins in plants. Consequently, our results provide new insights into the distribution, diversity and evolutionary history of steroidal saponins in plants, and enhance our understanding of plants' resistance to abiotic and biotic stresses. Additionally, fundamental understanding of the steroidal saponin biosynthesis will facilitate their industrial production and pharmacological applications. Significance Statement: Understanding the origin, evolution and diversity of plant‐specialized metabolites is fundamental to our understanding on the development of plants' resistance to abiotic and biotic stresses and has been a long‐standing goal of plant biology. We used a chemical trait‐genome‐phylogenetic approach to reveal the molecular mechanisms of multiple origins and evolution of steroidal saponins, a class of plant‐specialized metabolites renowned for their significant medicinal value. [ABSTRACT FROM AUTHOR]

Ling‐gui‐zhu‐gan decoction has significant therapeutic effects in the treatment of diseases related to phlegm and fluid retention. In this study, we aimed to qualitatively characterize the chemical constituents of Ling‐gui‐zhu‐gan decoction in vitro and in vivo by HPLC coupled to Fourier transform ion cyclotron resonance MS, and quantitively determine the contents of typical chemical constituents by HPLC method. As a result, a total of 75 chemical constituents were discovered including 37 flavonoids and their glycosides, 20 saponins, 9 sterols, 3 organic acids and their derivatives, 3 lactones, 2 coumarins, and 1 alcohol. Among them, 17 chemical constituents were specifically identified. Subsequently, an HPLC method was established for simultaneous determination of seven chemical constituents. Finally, a total of 40 prototype components were initially detected by HPLC‐MS method in the biological samples of rats after their water extract was orally administrated. Among them, 29, 27, 12, and 32 prototype components were detected in plasma, bile, urine, and feces, respectively. Moreover, 34 metabolites, including 16 phase II metabolites, were detected for the first time. In conclusion, this study lays the foundation for the identification of chemical components in vitro and in vivo and the elucidation of the potential pharmacodynamic components of Ling‐gui‐zhu‐gan decoction. [ABSTRACT FROM AUTHOR]

Hugan tablet is a Chinese medicine preparation. It is composed of Bupleuri Radix, Artemisiae Scopariae Herba, Isatidis Radix, Schisandrae Chinensis Fructus, Suis Fellis Pulvis, and Vigna radiata L. It has the effects of dispersing stagnated liver qi, strengthening the spleen and eliminating food to be used for the treatment of chronic hepatitis and early cirrhosis. However, the chemical composition of Hugan tablet is complex and not fully understood, which hampers the research in pharmacology. In this study, a reliable method for the rapid analysis and identification of the chemical components in Hugan tablet by their characteristic fragments and neutral losses using ultra‐performance liquid chromatography‐quadrupole‐exactive orbitrap mass spectrometry was developed. A total of 144 chemical components were tentatively identified, including 57 organic acids, 19 flavonoids, 23 alkaloids, 18 lignans, 7 saponins, and 20 others. These components may be the active ingredients of Hugan tablet. The established method can systematically and rapidly analyze the chemical components in Hugan tablet, which provides a basis for the pharmacodynamic substance study and is meaningful for the quality control of Hugan tablet. [ABSTRACT FROM AUTHOR]