Steroidal Saponins Research Articles

Polyphyllin II inhibits NLPR3 inflammasome activation and inflammatory response of Mycobacterium tuberculosis-infected human bronchial epithelial cells.

The bronchial infection by Mycobacterium tuberculosis (Mtb) is increasing in prevalence and severity worldwide. Despite appropriate tuberculosis treatment, most patients still develop bronchial stenosis, which often leads to disability. Polyphyllin II (PP2) is a steroidal saponin extracted from Rhizoma Paridis. In this study, we aimed to explore the effect of PP2 on the advancement of Mtb-induced bronchial infection. The effects of PP2 on cell viability were measured by using MTT and lactate dehydrogenase (LDH) kit. The mRNA and protein levels of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-8 were elucidated by RT-qPCR and ELISA, respectively. The expression of NLR family pyrin domain containing 3 (NLRP3) related inflammasome (NLRP3, IL-1β, and cleaved-caspase-1) and the activated degree of protein kinase B (AKT)/nuclear factor-kappa B (NF-kB; p-AKT and p-NF-κB) were detected by Western blotting. PP2 at 0, 1, 5, and 10 μM had little cytotoxicity on 16HBE cells. PP2 inhibited Mtb-induced cell proliferation and decreased LDH levels. We further found that PP2 could suppress Mtb-induced inflammatory responses and activation of NLPR3 inflammasome. Additionally, the role of PP2 in Mtb is associated with the AKT/NF-kB signaling pathway. PP2 inhibited Mtb infection in bronchial epithelial cells, by inhibiting Mtb-induced inflammatory reactions and activation of NLPR3 inflammasome. These effects may be exerted by suppressing the AKT/NF-kB pathway, which will provide a prospective treatment.

Quantitative Determination of Steroidal Saponins of Semen Allii Fistulosi Using HPLC-ELSD and HPLC-MS.

In this study, high-performance liquid chromatography-evaporative light scattering detection (HPLC-ELSD) and HPLC-mass spectrometry (HPLC-MS) were employed for the quantitative analysis of steroidal saponins of Semen Allii Fistulosi. The HPLC-ELSD method was simple, accurate, and repeatable, and the recoveries were 97.91%∼99.77%. Similarly, the HPLC-MS method was rapid, sensitive, accurate, and reproducible, and the recoveries ranging from 95.61% to 99.70% in the control samples. The sensitivity of the HPLC-MS method was several times higher than that of the HPLC-ELSD method. These results collectively demonstrated that these methods are suitable for the content determination of steroidal saponins of Semen Allii Fistulosi and the identification of its plant source.

Timosaponin AIII induces lipid peroxidation and ferroptosis by enhancing Rab7-mediated lipophagy in colorectal cancer cells.

Colorectal cancer (CRC) is a common digestive system malignancy, and despite significant therapeutic advancements, more effective treatments are needed. Timosaponin AIII (TA-III), a major steroidal saponin derived from Anemarrhena asphodeloides Bge, is a potential anticancer agent. Ferroptosis plays an important role in cancer treatment. To investigate the molecular mechanism of TA-III as a novel ferroptosis inducer in suppressing CRC through lipophagy. Ferroptosis, an autophagy-dependent mode of cell death, has been implicated in CRC. CRC cells were treated with TA-III, and lipophagy levels were evaluated via BODIPY493/503 staining and western blotting. Autophagy turnover was tracked using GFP-RFP-LC3B. Lipid peroxidation was quantified using an malondialdehyde kit and C11-BODIPY flow assay. Mitochondrial morphology was observed using transmission electron microscopy. GC-MS/MS was used to detect lipid metabolism changes. The role of ras related protein Rab 7a (Rab7) was assessed by western blotting and glutathione S-transferase pull-down assays. In vivo, the anticancer efficacy of TA-III was tested using a xenograft model. RNA-seq analysis unveiled the potential of TA-III as an anticancer agent through ferroptosis. In vivo experiments revealed how TA-III treatment triggered degradation of lipid droplets in CRC cells, resulting in an accumulation of FFAs, heightened unsaturated free fatty acids, and increased lipid peroxidation. These events ultimately lead to mitochondrial shrinkage and downregulation of ferroptosis markers (FSP1 and GPX4). Intriguingly, the Rab7 protein emerged as a crucial bridge between lipophagy and ferroptosis, underlining its significance in the anticancer mechanism of TA-III. Moreover, TA-III treatment in a xenograft tumour model substantially reduced tumour volume via ferroptosis, underscoring its therapeutic efficacy. Our study is the first to establish that TA-III triggers lipophagy in CRC cells via the Rab7 gene, subsequently promoting ferroptosis. This suggests its potential use as an antitumour agent.

Antibacteria Activities of Guava (Psidium guajava) and Orange (Citrus sinensis) Leaves Extracts on Staphylococcus aureus and Escherichia coli

his study aimed at determining the antibacterial activities of Psidium guajava and Citrus sinensis leaves extracts of aqueous, ethanol, and methanol on Staphylococcus aureus and Escherichia coli. Dimethyl sulfoxide was used for dissolving the leaves extracts and the minimum inhibitory concentration (MIC) of the extracts was determined using broth dilution technique to observe their antibacterial activities against S. aureus and E. coli. The phytochemical screening revealed the presence of metabolites (flavonoids, tannins, steroid saponins, saponins and alkaloids). The inhibition zone of the aqueous, ethanol and methanol extracts of P. guajava and C. sinensis against Staphylococcus aureus and Escherichia coli was highest at 200mg/ml (18mm and 17mm), while the least inhibition zone was at 12.5mg/ml (7mm and 0mm) respectively. The aqueous extracts of P. guajava and C. sinensis against E. coli and S. aureus had its MIC at 50g/ml and 100mg/ml respectively, while ethanol extracts of P. guajava and C. sinensis against the bacterial (E. coli and S. aureus) had its MIC at 50g/ml. The methanol extracts of P. guajava and C. sinensis showed the growth of S. aureus in all concentrations (12.5g/ml, 25g/ml, 50g/ml, 100mg/ml and 200mg/ml) while E. coli had no growth from 100mg/ml above concentrations and 50g/ml (MIC) of P. guajava leaf extracts. These findings, therefore support the traditional use of Psidium guajava and Citrus sinensis for its curative potential to synthetic drugs which are expensive, not easily accessible with potential side effects.

Four new steroidal glycosides from Lilium lancifolium Thunb. and their antitumor activity

Four new steroidal glycosides (1–4), including two steroidal saponins named lililancifoloside B and C (1–2), one pregnane glycoside named lililancifoloside D (3), and one C22-steroidal lactone glycoside named lililancifoloside E (4), together with five known ones (5–9), were isolated from the bulbs of Lilium lancifolium Thunb. By using spectroscopic analysis, including 1D, 2D NMR, and HR-ESI-MS, the structures of 1–4 were elucidated. All isolates were tested for their cytotoxic potential against the MCF-7, MDA-MB-231, HepG2, and A549 cell lines. Compound 6 distinguished out among them, IC50 values of 3.31, 5.23, 1.78, and 1.49 μM against the four cell lines, respectively. Other compounds such as compound 3, 5, and 9 have also shown specific cytotoxic activity. Next, studies showed that compound 6 might cause HepG2 cells to undergo a cell cycle arrest during the G2/M phase and apoptosis.

Trilliumosides K and L, two novel steroidal saponins from rhizomes of Trillium govanianum, as potent anti-cancer agents targeting apoptosis in the A-549 cancer cell line.

Two novel steroidal saponins, trilliumosides K (1) and L (2), were isolated from the rhizomes of Trillium govanianum led by bioactivity-guided phytochemical investigation along with seven known compounds: govanoside D (3), protodioscin (4), borassoside E (5), 20-hydroxyecdysone (6), 5,20-hydroxyecdysone (7), govanic acid (8), and diosgenin (9). The structure of novel compounds 1-2 was established using analysis of spectroscopic data including 1D and 2D nuclear magnetic resonance (NMR) and high resolution mass spectrometry (HR-ESI-MS) data. All isolated compounds were evaluated for in vitro cytotoxic activity against a panel of human cancer cell lines. Compound 1 showed significant cytotoxic activity against the A-549 (Lung) and SW-620 (Colon) cancer cell lines with IC50 values of 1.83 and 1.85µM, respectively whereas the IC50 value of Compound 2 against the A-549 cell line was found to be 1.79µM. Among the previously known compounds 3, 5, and 9, the cytotoxic IC50 values were found to be in the range of 5-10µM. Comprehensive anti-cancer investigation revealed that Compound 2 inhibited in vitro migration and colony-forming capability in the A-549 cell line. Additionally, the mechanistic analysis of Compound 2 on the A-549 cell line indicated distinctive alterations in nuclear morphology, increased reactive oxygen species (ROS) production, and decreased levels of mitochondrial membrane potential (MMP). By upregulating the pro-apoptotic protein BAX and downregulating the anti-apoptotic protein BCL-2, the aforementioned actions eventually cause apoptosis, a crucial hallmark in cancer research, which activates Caspase-3. To the best of our knowledge, this study reports the first mechanistic anti-cancer evaluation of the compounds isolated from the rhizomes of T. govanianum with remarkable cytotoxic activity in the desired micromolar range.

Gut microbiota modification by diosgenin mediates antiepileptic effects in a mouse model of epilepsy.

Diosgenin, a natural steroid saponin, holds promise as a multitarget therapeutic for various diseases, including neurodegenerative conditions. Its efficacy in slowing Alzheimer's disease, Parkinson's disease, multiple sclerosis, and stroke progression has been demonstrated. However, the role of diosgenin in anti-epilepsy and its potential connection to the modulation of the intestinal microbiota remain poorly understood. In this study, exogenous diosgenin significantly mitigated pentylenetetrazole (PTZ)-induced seizures, learning and memory deficits, and hippocampal neuronal injury. 16S ribosomal RNA (16S rRNA) sequencing revealed a reversal in the decrease of Bacteroides and Parabacteroides genera in the PTZ-induced mouse epileptic model following diosgenin treatment. Fecal microbiota transplantation (FMT) experiments illustrated the involvement of diosgenin in modulating gut microbiota and providing neuroprotection against epilepsy. Our results further indicated the repression of enteric glial cells (EGCs) activation and the TLR4-MyD88 pathway, coupled with reduced production of inflammatory cytokines in the colonic lumen, and improved intestinal barrier function in epilepsy mice treated with diosgenin or FMT. This study suggests that diosgenin plays a role in modifying gut microbiota, contributing to the alleviation of intestinal inflammation and neuroinflammation, ultimately inhibiting epilepsy progression in a PTZ-induced mouse model. Diosgenin emerges as a potential therapeutic option for managing epilepsy and its associated comorbidities.

Chemical Comparison and Identification of Xanthine Oxidase Inhibitors of Dioscoreae Hypoglaucae Rhizoma and Dioscoreae Spongiosae Rhizoma by Chemometric Analysis and Spectrum-Effect Relationship.

Dioscoreae hypoglaucae Rhizoma (DH) and Dioscoreae spongiosae Rhizoma (DS) are two similar Chinese herbal medicines derived from the Dioscorea family. DH and DS have been used as medicines in China and other Asian countries for a long time, but study on their phytochemicals and bioactive composition is limited. This present study aimed to compare the chemical compositions of DH and DS, and explore the anti-xanthine oxidase components based on chemometric analysis and spectrum-effect relationship. Firstly, an HPLC method was used to establish the chemical fingerprints of DH and DS samples, and nine common peaks were selected. Then, hierarchical clustering analysis, principal component analysis and orthogonal partial least squares discriminant analysis were employed to compare and discriminate DH and DS samples based on the fingerprints data, and four steroidal saponins compounds (protodioscin, protogracillin, dioscin, gracillin) could be chemical markers responsible for the differences between DH and DS. Meanwhile, the anti-xanthine oxidase activities of these two herbal medicines were evaluated by xanthine oxidase inhibitory assay in vitro. Pearson correlation analysis and partial least squares regression analysis were subsequently used to investigate the spectrum-effect relationship between chemical fingerprints and xanthine oxidase inhibitory activities. The results showed that four steroidal saponins, including protodioscin, protogracillin, methyl protodioscin and pseudoprogracillin could be potential anti-xanthine oxidase compounds in DH and DS. Furthermore, the xanthine oxidase inhibitory activities of the four selected inhibitors were validated by anti-xanthine oxidase inhibitory assessment and molecular docking experiments. The present work provided evidence for understanding of the chemical differences and the discovery of the anti-xanthine oxidase constituent of DH and DS, which could be useful for quality evaluation and bioactive components screening of these two herbal medicines.

Four Steroidal Saponins from the Trunks of Dracaena cambodiana with Inhibition of NO Production in LPS Activated RAW264.7 Cells.

Dracaena cambodiana Pierre ex Gagnep. is well known as a medicinal plant and widely distributed in Vietnam. Phytochemical investigation on the trunks of D. cambodiana lead to the isolation of four undescribed compounds (1-4) together with seven known ones (5-11). Their structures were determined to be pennogenin-24-yl-O-β-D-glucopyranoside (1), 17α-hydroxycambodianoside C (2), (25R)-27-hydroxypenogenin 3-O-α-L-rhamnopyranosyl-(1→3)-[α-L-rhamnopyranosyl-(1→2)]-β-D-glucopyranoside (3), (3β,25R)-17α,22α-dihydroxy-furost-5-en-3-yl-O-α-L-rhamnopyranosyl-(1→3)-[α-L-rhamnopyranosyl-(1→2)]-β-D-glucopyranoside (4), dracagenin A (5), 1-O-β-D-glucopyranosyl-2-hydroxy-4-allylbenzene (6), 1-O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranosyl-2-hydroxy-allylbenzene (7), 2-O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranosyl-1-hydroxy-allylbenzene (8), cinnamrutinoside A (9), icariside D1 (10), and seco-isolariciresinol 9-O-β-glucopyranoside (11) by extensive spectroscopic investigation, HR-ESI-MS, 1D and 2D NMR spectra. The anti-inflammatory activity of the isolated compounds was evaluated on macrophages. Compounds 1-6 significantly inhibited nitric oxide production in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. Among them, compound 1 showed the best inhibitory activity with an IC50 value of 8.90±0.56 μM.

Chemical constituents from the leaves of Viburnum odoratissimum and their chemotaxonomic significance

Phytochemical investigation on the leaves of Viburnum odoratissimum Ker.-Gawl. led to the isolation of fourteen compounds, including eight triterpenes (1-8), one steroidal saponin(9), one butanolide (10), two monoterpenes (11, 12) and two sesquiterpenoids (13, 14). The existence of compounds 3, 6, 7, 9, 10 and 12 in Viburnum genus has been reported for the first time. The structures of these compounds were elucidated on the basis of spectroscopic analysis as well as comparison with previously reported data. In addition, the chemotaxonomic significance of isolated compounds from V. odoratissimum was also discussed in this thesis.

Oat (Avena sativa L.) Sprouts Restore Skin Barrier Function by Modulating the Expression of the Epidermal Differentiation Complex in Models of Skin Irritation.

Oats (Avena sativa L.) are used as therapeutic plants, particularly in dermatology. Despite numerous studies on their skin moisturization, anti-inflammation, and antioxidation effects, the precise molecular mechanisms of these effects are only partially understood. In this study, the efficacy of oat sprouts in the treatment of allergic contact dermatitis (ACD) was investigated, and their specific phytoconstituents and exact mechanisms of action were identified. In the in vivo ACD model, by stimulating the mitogen-activated protein kinase signaling pathway, oat sprouts increased the expression levels of proteins associated with skin barrier formation, which are produced during the differentiation of keratinocytes. In addition, in a lipopolysaccharide-induced skin irritation model using HaCaT, steroidal saponins (avenacoside B and 26-deglucoavenacoside B) and a flavonoid (isovitexin-2-o-arabinoside) of oat sprouts regulated the genetic expression of the same proteins located on the adjacent locus of human chromosomes known as the epidermal differentiation complex (EDC). Furthermore, oat sprouts showed immunomodulatory functions. These findings suggest the potential for expanding the use of oat sprouts as a treatment option for various diseases characterized by skin barrier disruption.

Steroidal saponins from the roots of Paris verticillata and their anti-proliferative and anti-inflammatory activities

Thirteen previously undescribed steroidal saponins, named parisverticilloside A-M (1–13) and twenty known steroidal saponins (14–33) were isolated from ethanol extract of the roots of Paris verticillata. Their structures were identified by a series of spectroscopic methods, including 1D and 2D NMR, HR-ESI-MS, optical rotatory dispersion and chemical processes. The anti-proliferative activities of all compounds against LN229, HepG2, MDA-MB-231 and 4T1 cell lines were evaluated using the CCK8 assay with cisplatin or capecitabine as the positive control. The anti-inflammatory activities of all compounds were measured by inhibition of LPS-induced NO release from BV2 cell lines, with dexamethasone as the positive control.

Protective effect of steroidal saponins on heat stress in the liver of largemouth bass (Micropterus salmoides) revealed by metabolomic analysis

With global warming, high water temperature events are becoming more frequent in summer. The liver of the largemouth bass (Micropterus salmoides) is particularly sensitive to heat stress, especially in the rapid growth period with high nutrient concentration. In this experiment, a metabolomic analysis was conducted to reveal how steroidal saponins alleviated high temperature stress in largemouth bass. Fish were divided into three groups, two groups fed the basic diet, the third group fed the experimental diet contained steroidal saponins. After the fish ingested the diets for four weeks, the heat temperature stress test began. The first group fed basic diet without the heat stress (C), and the second group fed basic diet with the heat stress (H), and the third group fed experimental diet containing steroidal saponins with heat stress (HS). After 1-week of heat stress, metabolic analysis showed that high temperature stress mainly affected phospholipid metabolism, fatty acid metabolism, glutathione metabolism and bile metabolism in the fish livers of H group. The expression of genes glutathione peroxidase and heme oxygenase-1 were decreased and the nuclear factor kappa-B activated inflammation in fish feeding in group H. The adenosine 5′-monophosphate-activated protein kinase pathway was activated in the HS group. Compare to the fish in H group, those metabolism observed in fish in HS group were greatly improved, similar to the C group. Thus, steroidal saponins could help relieve the liver burden when largemouth bass facing heat stress in summer.

Review on Bioactive Metabolites of <i>Asparagus racemosus</i> and its Pharmacological Significance

Naturally, genealogical people for different symptoms are nearly new to therapeutic traditional plant active components, Shatavari, a valuable plant growing worldwide. This review provides an overview of Asparagus racemosus and the components of Asparagus racemosus used in entirely new combination of ingredients, have applications in industry as well as medicine. This plant is growing in popularity because to its nutrient-rich root, leaves, blossoms, and fruits. It also has a long history of medical use and is known to possess qualities that are beneficial to medicine. Asparagus racemosus, usually in therapeutic approach for the cancer of the liver, brain disorder, has the main role in milk secretion in pregnant women and regulate sexual behavior. This plant may be a reliable source of bioactive constituents like steroidal saponins, Shatavarins the most important bioactive parts in an exceedingly. A. Racemosus are finding applications due to various potential functions like immunomodulant, galactagogue, antioxidant, anti - inflammatory, antimutagenic, inhibitor, or antiulcer, boosting the lifestyle for humans. Ayurveda suggested it is for interference and treatment of gastrointestinal ulcers, dyspepsia and galactagogue. There has been no scientific proof detected in Shatavari based mostly Nutra beverage considering the range of secondary metabolites present in it their bioavailability and their health advantages. Therefore, the fermentation of Shatavari in Nutra beverages is a developed area of research for the event of different Nutra beverages, which may cause not only supply a lot of nutrition but prevent and therapeutic common diseases additionally.

Diosgenin alters LPS-induced macrophage polarization by activating PPARγ/NF-κB signaling pathway

Diosgenin (DG) is a steroidal saponin derived from plants, and it exhibits anti-inflammatory properties. In this study, we employed an in vitro model of P.g.-LPS-stimulated mouse macrophage cell line RAW264.7 to investigate the anti-inflammatory effects and mechanism of DG under the condition of altered polarization of macrophages. The RAW264.7 cells were subjected to pre-treatment with DG with or without P.g.-LPS. In cultured macrophages, DG inhibited P.g.-LPS-induced pro-inflammatory M1 macrophages, and increased anti-inflammatory M2 macrophages. Notably, DG reduced the expression of phosphorylation levels of NF-κB p65 and IκB while increasing the expression of PPARγ. Further studies revealed that PPARγ inhibitor GW9662 or PPARγ siRNA reversed the inhibitory effect of DG on M1 phenotype. Collectively, the anti-inflammatory mechanism of DG is related to altering macrophage polarization by activating PPARγ and inhibiting NF-κB signaling pathways.

Thermal degradation kinetics of cynatratoside-C and its antiparasitic efficacy after being stored in sterile water and aquaculture water

Cynatratoside-C (CyC), a C-21 steroidal saponin isolated from Cynanchum atratum, is a promising candidate for treating freshwater fish infected with the ciliated parasite Ichthyophthirius multifiliis. To promote the drug development process of CyC, the present study investigated the stability of CyC under heating, sterile water, and aquaculture water treatments. An accelerated stability test demonstrated that the thermal degradation kinetics followed a first-order reaction with a predicted half-life (t0.5) of 3472 days (9.5 years) at a temperature of 25 °C. According to the Arrhenius model, the activation energy Ea of CyC was calculated as 91.7 kJ/mol. When CyC was stored in sterile water for 3 years, the mortality rates of theronts and nonencysted tomonts were decreased significantly in the low CyC concentration treatment group, and the minimum concentration that inhibited the production of encysted tomonts increased from 0.06 mg/L to 0.125 mg/L. When CyC was stored in sterile water for 6 years, it showed a nearly complete loss of antiparasitic efficacy, indicating that water may promote the degradation of CyC. When CyC was stored in aquaculture water, the antiparasitic efficacy of CyC against theronts and tomonts was decreased significantly at 2 days post-storage, indicating that microorganisms in aquaculture water could absorb and degrade CyC. The present study provides important information concerning the stability of CyC and the drug approval process.

Unraveling the mechanisms of Fenugreek seed for managing different gynecological disorders: steroidal saponins and isoflavones revealed as key bioactive metabolites

This study employed network pharmacology-based analysis and reverse molecular docking to investigate the molecular targets and pathways associated with gynecological disorders, particularly those related to steroidal hormones and their receptors, and the potential therapeutic effects of fenugreek (Trigonella foenum-graecum L.) constituents. The STITCH 5.0 database was utilized to identify potential molecular targets, and a compound-target network was constructed. The main targets associated with gynecological disorders included estrogen receptor beta (ESR2), estrogen-related receptor gamma (GPER1), oxytocin receptor (OXTR), progesterone receptor (PGR), prolactin receptor (PRLR), and several enzymes involved in sex hormone biosynthesis. Additionally, network topological analysis revealed that specific compounds, such as quercetin, luteolin, genistein, and vitexin, had significant interactions with the identified targets. Reverse molecular docking analysis confirmed the interactions between the identified compounds and target proteins where quercetin, luteolin, genistein, 4'-methylgenistein, trigoneoside IIB, diosgenin, and vitexin possessed the highest combined docking scores, indicating their multi-target nature. The results highlighted the potential of steroidal saponins, isoflavones, and flavones as active constituents of fenugreek with implications for lactation, reproductive processes, and estrogenic activity. The chemical profiling of saponin-enriched and flavonoid-enriched fractions using UPLC/MS/MS further supported the presence of these bioactive compounds. In an animal model study, the steroidal saponins-enriched fraction of fenugreek seed exhibited a significant increase in the body weight of lactating female rats and serum prolactin levels while the flavonoids-enriched fraction showed an increase in serum estradiol levels and improved the histological structure of ovaries.

Transcriptome analysis of three medicinal plants of the genus Polygonatum: identification of genes involved in polysaccharide and steroidal saponins biosynthesis.

Polysaccharides and saponins are the main active components of Polygonati Rhizoma. Studying the molecular mechanism of their synthesis pathway is helpful in improving the content of active components at the molecular level. At present, transcriptome analysis of three Polygonatum species (Polygonatum sibiricum Red., Polygonatum cyrtonema Hua, Polygonatum kingianum Coll. et Hemsl.) has been reported, but no comparative study has been found on the transcriptome data of the three species. Transcriptome sequencing was performed on the rhizomes of three Polygonatum species based on high-throughput sequencing technology, and all transcripts were assembled. A total of 168,108 unigenes were generated after the removal of redundancy, of which 121,642 were annotated in seven databases. Through differential analysis and expression analysis of key enzyme genes in the synthesis pathway of three Polygonatum polysaccharides and steroidal saponins, 135 differentially expressed genes encoding 18 enzymes and 128 differentially expressed genes encoding 28 enzymes were identified, respectively. Numerous transcription factors are involved in the carbohydrate synthesis pathway. Quantitative real-time PCR was used to further verify the gene expression level. In this paper, we present a public transcriptome dataset of three medicinal plants of the genus Polygonatum, and analyze the key enzyme genes of polysaccharide and steroidal saponins synthesis pathway, which lays a foundation for improving the active component content of Polygonati Rhizoma by molecular means.

Cytotoxic, antioxidant, and antiglycation activities, and tyrosinase inhibition using silver nanoparticles synthesized by leaf extract of Solanum aculeatissimum Jacq

ABSTRACT The present study aimed to determine the biological properties of an extract of Solanum aculeatissimum aqueous extract (SaCE) alone as well as silver nanoparticles (AgNPs) generated by green synthesis utilizing S. aculeatissimum aqueous extract (SaCE). These synthesized SaCE AgNPs were characterized using UV-VIS spectrophotometry, scanning transmission electron microscopy (TEM), energy dispersive spectroscopy (EDS), zeta potential (ZP), dynamic light scattering (DLS). Determination of total polyphenols, flavonoids, saponins content was conducted. In addition, high performance liquid chromatography-mass spectrometry (HPLC-MS) was employed to identify constituents in this extract. Antioxidant activity was determined by DPPH radical scavenging and ferric ion reducing power (FRAP) methods. Antiglycation activity was demonstrated through relative mobility in electrophoresis (RME) and determination of free amino groups. The inhibitory activity on tyrosinase was also examined. Molecular docking analyses were performed to assess the molecular interactions with DNA and tyrosinase. The antitumor activity SaCE was also measured. Phytochemical analysis of SaCE and AgNPs showed presence polyphenols (1000.41 and 293.37 mg gallic acid equivalent/g), flavonoids (954.87 and 479.87 mg rutin equivalent/g), saponins (37.89 and 23.01% total saponins), in particular steroidal saponins (aculeatiside A and B). Both SaCE and AgNPs exhibited significant antioxidant (respectively, 73.97%, 56.27% in DPPH test, 874.67 and 837.67 μM Trolox Equivalent/g in FRAP test) and antiglycation activities (72.81 and 67.98% free amino groups, results observed in RME). SaCE and AgNPs presented 33.2, 36.1% inhibitory activity on tyrosinase, respectively. In silico assay demonstrated interaction between steroidal saponins, DNA or tyrosinase. SaCE exhibited antitumor action against various human tumor cells. Data demonstrated that extracts SaCE alone and AgNPs synthesized from SaCE presented biological properties of interest for application in new therapeutic formulations in medicine.

Unraveling the serial glycosylation in the biosynthesis of steroidal saponins in the medicinal plant Paris polyphylla and their antifungal action.

Sugar-sugar glycosyltransferases play important roles in constructing complex and bioactive saponins. Here, we characterized a series of UDP-glycosyltransferases responsible for biosynthesizing the branched sugar chain of bioactive steroidal saponins from a widely known medicinal plant Paris polyphylla var. yunnanensis. Among them, a 2'-O-rhamnosyltransferase and three 6'-O-glucosyltrasferases catalyzed a cascade of glycosylation to produce steroidal diglycosides and triglycosides, respectively. These UDP-glycosyltransferases showed astonishing substrate promiscuity, resulting in the generation of a panel of 24 terpenoid glycosides including 15 previously undescribed compounds. A mutant library containing 44 variants was constructed based on the identification of critical residues by molecular docking simulations and protein model alignments, and a mutant UGT91AH1Y187A with increased catalytic efficiency was obtained. The steroidal saponins exhibited remarkable antifungal activity against four widespread strains of human pathogenic fungi attributed to ergosterol-dependent damage of fungal cell membranes, and 2'-O-rhamnosylation appeared to correlate with strong antifungal effects. The findings elucidated the biosynthetic machinery for their production of steroidal saponins and revealed their potential as new antifungal agents.