Search Results (43)

This study investigates the compositional characteristics and quantitative differences of ginsenosides across various ginseng tissues, with a particular focus on the specific accumulation patterns of malonyl ginsenosides. Five tissue samples—ginseng fruit (F), leaf (L), taproot (TR), lateral root (LR), and fibrous root (FR)—were analyzed using Orbitrap Fusion high-resolution liquid chromatography–mass spectrometry. A total of 413 ginsenosides, including 33 standards, were identified, encompassing 172 protopanaxadiol (PPD)-type, 188 protopanaxatriol (PPT)-type, 14 oleanolic acid (OA)-type, and 12 ocotillol (OT)-type ginsenosides, of which 160 were malonyl ginsenosides. Statistical analysis revealed significant variations in the relative content per unit mass of malonyl ginsenosides across tissues, with the highest levels in fibrous roots, followed by fruits, lateral roots, leaves, and taproots. Distinct tissue-specific differences in malonyl ginsenoside types and quantities were observed: fruits exhibited 51 malonyl ginsenosides with significantly higher levels, compared to 8, 14, and 17 in lateral roots, fibrous roots, and leaves, whereas TR showed no significant enrichment. This study elucidates the diversity and unique distribution of malonyl ginsenosides in ginseng roots, leaves, and fruits, providing a valuable basis for the targeted selection of tissues with high malonyl ginsenoside content and the development of functional food and medicinal products. Full article

Background/Objectives: Ginseng has been a traditional remedy for centuries, known for its diverse benefits such as anti-inflammation, antioxidant, bactericidal, fungicidal antidiabetic, and anticancer effects. This study employs a network pharmacology approach with molecular dynamics simulation to investigate the potential mechanisms through which ginseng-derived compounds control hypertension. Methods: The total of 70 bioactive compounds were identified from the literature and classified as ginsenosides, which fall under Protopanaxadiol-type ginsenosides, Protopanaxatriol-type ginsenosides, and Ocotillol-type saponins. The target proteins related to hypertension were collected from the drug bank, and interactions between proteins network were examined using STRING 12.0 and Cytoscape 3.10.1. Bioinformatics tools were used to analyze the biological enrichment of genes. The core targets extracted through network pharmacology were subjected to molecular docking studies. Similarly, the docking score below −6.0 kcal/mol was further visualized by performing molecular dynamics simulation to see the binding affinity between the complexes. Finally, pharmacokinetics and toxicity of the compounds were evaluated using computational tools. Results: Molecular docking and simulation results revealed that Floralquinquenoside C, Ginsenoside Rg6, Notoginsenoside T1, and Floralquinquenoside B exhibited strong binding and stability with Angiotensin-converting enzyme (ACE) and Carbonic Anhydrase-I (CA-I), which alters the renin–angiotensin system, calcium signaling pathway, adrenergic signaling in cardiomyocytes, c-GMP-PKG signaling pathway, etc., to regulate high blood pressure. Conclusions: The results show that the phytochemicals from ginseng could act as potential candidates for the management of hypertension, which may help minimize the side effects caused by synthetic anti-hypertensive drugs available on the market. Full article

Sixty Duroc × (Landrace × Yorkshire) castrated male finishing pigs were randomly divided into negative control (NC) and gracilaria lemaneiformis polysaccharides (GLP) groups to study the effects of GLP on the fecal microbiota and fecal metabolites of fattening pigs. The NC group was fed a basic diet, and the GLP group was fed a basic diet supplemented with 0.1% GLP. The diversity of the species and the fecal metabolites were analyzed using 16S rDNA sequencing and metabolome sequencing, respectively. The serum immune and antioxidant indices were analyzed using the ELISA assay. The abundances of hazardous bacteria such as Proteobacteria at the phylum level and Shigella at the genus level were extremely significantly decreased (p < 0.01) and those of beneficial bacteria such as Firmicutes at the phylum level (p < 0.01), Clostridium at the genus level (p < 0.01), and Lactobacillus at the genus level (p < 0.05) were significantly increased in the GLP group compared with the NC group. A total of 41 differentially expressed metabolites were identified. The expression of anti-inflammatory and antioxidant active substances, such as methyl cinnamate, protopanaxatriol, and isovanillic acid, was elevated in the GLP group. The ELISA assay showed increased GSH-Px activity (p < 0.01), T-AOC (p < 0.01), IgG (p < 0.01), IgA (p < 0.05), and IgM (p < 0.05) in the GLP group. These results indicate that dietary GLP supplementation can improve the antioxidant ability, anti-inflammatory ability, and immune level of fattening pigs by regulating fecal flora and metabolites and could be used as a functional feed additive. Full article

The intricate regulatory mechanisms governing adipocyte differentiation are pivotal in elucidating the complex pathophysiology underlying obesity. This study aims to explore the dynamic changes in gene expression during the differentiation of 3T3-L1 adipocytes using transcriptomics methods. Protopanaxatriol (PPT) significantly inhibited adipocyte differentiation. To uncover the molecular mechanisms, we conducted an extensive transcriptomic analysis of adipocytes throughout various differentiation stages, comparing gene expression profiles before and after PPT treatment. The construction of 16 co-expression modules was achieved using weighted gene co-expression network analysis (WGCNA). The 838 differentially expressed genes in the blue module were highly correlated with PPT treatment. Further analysis revealed that PIKfyve, STAT3, JAK1, CTTN, TYK2, JAK3, STAT2, STAT5b, SOCS3, and IRF9 were core genes closely associated with adipocyte differentiation. This discovery underscores the potential pivotal function of these ten genes in regulating adipocyte differentiation. This study elucidated that PPT, an active ingredient in ginseng, could reduce lipid accumulation by inhibiting the differentiation of adipocyte precursors through the negative regulation of genes such as PIKfyve, STAT3, and JAK1. Finally, molecular docking identified potential binding sites for PPT on PIKfyve and JAK1. This study provides potential drug targets for preventing obesity and related metabolic diseases. Full article

Medicinal plant-derived vesicle-like nanoparticles can carry chemical components and exert intercellular activity due to the encapsulation of nanostructures. American ginseng is well known as a traditional herb and is commonly used in clinical decoctions. However, the nano-characteristics and chemical composition of American-ginseng-derived vesicle-like nanoparticles (AGVNs) in decoctions are unclear. In this study, the gradient centrifugation method was used to extract and isolate AGVNs. A metabolomic method based on high-resolution mass spectrometry was established to analyze small molecules loaded in AGVNs. Zebrafish and RAW264.7 cells were employed to investigate the anti-inflammatory effects of AGVNs. The results showed that the particle size of AGVNs was generally 243.6 nm, and the zeta potential was −14.5 mV. AGVNs were found to contain 26 ginsenosides (14 protopanaxadiols, 11 protopanaxatriols, and 1 oleanolic acid). Ginsenoside Rb1 and malonyl-ginsenoside Rb1 tended to be enriched in AGVNs. Moreover, AGVNs were found to exert anti-inflammatory effects by reducing macrophage migration in zebrafish and regulating inflammatory factor (NO, TNF-α, IL-6, IL-10) secretion in RAW 264.7 cells. The characterization and analysis of AGVNs provide references and data that support the development of nanoscale anti-inflammatory substances from medicinal plants. Full article

Depression is one of the most common psychological disorders nowadays. Studies have shown that 20(S)-protopanaxatriol (PPT) can effectively improve depressive symptoms in mice. However, its mechanism needs to be further explored. In this study, we used an integrated approach combining network pharmacology and transcriptomics to explore the potential mechanisms of PPT for depression. First, the potential targets and pathways of PPT treatment of depression were screened through network pharmacology. Secondly, the BMKCloud platform was used to obtain brain tissue transcription data of chronic unpredictable mild stress (CUMS) model mice and screen PPT-altered differential expression genes (DEGs). Gene ontology (GO) analysis and the Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis were performed using network pharmacology and transcriptomics. Finally, the above results were verified by molecular docking, Western blotting, and quantitative real-time polymerase chain reaction (qRT-PCR). In this study, we demonstrated that PPT improved depression-like behavior and brain histopathological changes in CUMS mice, downregulated nitric oxide (NO) and interleukin-6 (IL-6) levels, and elevated serum levels of 5-hydroxytryptamine (5-HT) and brain-derived neurotrophic factor (BDNF) after PPT treatment compared to the CUMS group. Eighty-seven potential targets and 350 DEGs were identified by network pharmacology and transcriptomics. Comprehensive analysis showed that transthyretin (TTR), klotho (KL), FOS, and the phosphatidylinositol 3-kinase–protein kinase B (PI3K-AKT) signaling pathway were closely associated with the therapeutic effects of PPT. Molecular docking results showed that PPT had a high affinity for PI3K, AKT, TTR, KL, and FOS targets. Gene and protein level results showed that PPT could increase the expression of PI3K, phosphorylation of PI3K (p-PI3K), AKT, phosphorylation of AKT (p-AKT), TTR, and KL and inhibit the expression level of FOS in the brain tissue of depressed mice. Our data suggest that PPT may achieve the treatment of depression by inhibiting the expression of FOS, enhancing the expression of TTR and KL, and modulating the PI3K-AKT signaling pathway. Full article

Panax quinquefolius (PQ) has been widely used in traditional Chinese medicine and functional food. Ginsenosides are the important functional components of PQ. The ginsenosides’ diversity is deeply affected by the processing conditions. The ginsenosides in the steamed PQ have been not well-characterized yet because of the complexity of their structure. In the study, the comprehensive investigation of ginsenosides was performed on the steamed PQ with different steaming times and temperatures by UPLC-Q-TOF-MS. Based on the molecular weight, retention time and characterized fragment ions, 175 ginsenosides were unambiguously identified or tentatively characterized, including 45 protopanaxatriol type, 49 protopanaxadiol type, 19 octillol type, 6 oleanolic acid type ginsenosides, and 56 other ginsenosides. Ten new ginsenosides and three new aglycones were discovered in the steamed PQ samples through searching the database of CAS SciFinderⁿ. Principal component analysis showed the significant influence on the chemical components of PQ through different processing conditions. The steaming temperature was found to promote the transformation of ginsenosides more than the steaming time. The protoginsenosides were found to transform into the rare ginsenosides by elimination reactions. The malonyl ginsenosides were degraded into acetyl ginsenosides, and then degraded into neutral ginsenosides. The sugar chain experienced degradation, with position changes and configuration inversions. Furthermore, 20 (S/R)-ginsenoside Rh1, Rh2, Rg2, and Rh12 were found to transform from the S-configuration to the R-configuration significantly. This study could present a comprehensive ginsenosides profile of PQ with different steaming conditions, and provide technical support for the development and utilization of PQ. Full article

Saponin-rich medicinal plants, particularly ginseng and Pseudo ginseng, are valuable in traditional medical practice due to the presence of different saponins. These plants benefit from natural saponins/triterpenoids drugs, such as Ginsenosides, Gypenosides, Platycodins, and Lancemasides. Ginsenosides are highly required for research and functional materials preparation in industrial practices, and some compounds, like Compound-K, have been taken to human trials for various therapeutic applications. To elucidate the genes/transcripts profiles responsible for secondary metabolites and ginsenoside biosynthesis in Ginseng and Pseudo ginseng plant genomes, a comparative analysis was conducted in this study. Nine plant genomes with a 99% BUSCO completeness score were used, resulting in 49 KEGG secondary metabolite pathways, 571 cytochromes genes with 42 families, and 3529 carbohydrate genes with 103 superfamilies. The comparative analysis revealed 24 genes/transcripts belonging to the CYP716 family, which is involved in the ginsenoside biosynthesis pathway. Additionally, it found that various ginsenosides demonstrated strong binding affinity with twelve targets, with ginsenoside Rg3, Rg2, Rh1, Rh5, F3, Rh9, Panaxadione, Protopanaxatriol, Floral ginsenoside C, and Floral ginsenoside E exhibiting the highest binding affinities with the tested enzymes. Since these groups of enzymes are not yet fully characterized for Pseudo ginseng plants in the interconversion of triterpenoids, this comparative bioinformatics analysis could aid experimentalists in selecting and conducting characterization with practical knowledge. Full article

Age-related skeletal muscle atrophy and weakness not only reduce the quality of life of those afflicted, but also worsen the prognosis of underlying diseases. We evaluated the effect of RGX365, a protopanaxatriol-type rare ginsenoside mixture, on improving skeletal muscle atrophy. We investigated the myogenic effect of RGX365 on mouse myoblast cells (C2C12) and dexamethasone (10 µM)-induced atrophy of differentiated C2C12. RGX365-treated myotube diameters and myosin heavy chain (MyHC) expression levels were analyzed using immunofluorescence. We evaluated the myogenic effects of RGX365 in aging sarcopenic mice. RGX365 increased myoblast differentiation and MyHC expression, and attenuated the muscle atrophy-inducing F-box (Atrogin-1) and muscle RING finger 1 (MuRF1) expression. Notably, one month of oral administration of RGX365 to 23-month-old sarcopenic mice improved muscle fiber size and the expression of skeletal muscle regeneration-associated molecules. In conclusion, rare ginsenosides, agonists of steroid receptors, can ameliorate skeletal muscle atrophy during long-term administration. Full article

Compound K (CK) is one of the major metabolites found in mammalian blood and organs following oral administration of Panax plants. CK, also known as minor ginsenoside, can be absorbed in the systemic circulation. It has garnered significant attention in healthcare and medical products due to its pharmacological activities, such as antioxidation, anticancer, antiproliferation, antidiabetics, neuroprotection, and anti-atherogenic activities. However, CK is not found in natural ginseng plants but in traditional chemical synthesis, which uses toxic solvents and leads to environmental pollution during the harvest process. Moreover, enzymatic reactions are impractical for industrial CK production due to low yield and high costs. Although CK could be generated from major ginsenosides, most ginsenosides, including protopanaxatriol-oleanane and ocotillol-type, are not converted into CK by catalyzing β-glucosidase. Therefore, microbial cell systems have been used as a promising solution, providing a safe and efficient approach to CK production. This review provides a summary of various approaches for the production of CK, including chemical and enzymatic reactions, biotransformation by the human intestinal bacteria and endophytes as well as engineered microbes. Moreover, the approaches for CK production have been discussed to improve the productivity of target compounds. Full article

Panax ginseng is an ancient and very potent herb, which has a long history of medicinal use, and recent studies have shown that ginsenosides are the main active substances in its pharmacological effects. However, the saponin content of wild ginseng and cultivated ginseng can hardly meet the market supply, and the ginseng adventitious root suspension culture technology can produce ginsenosides in a targeted manner. The length of culture time is an important factor affecting the growth and development of plants and the accumulation of secondary metabolites. After transcriptome sequencing of ginseng adventitious root material at different culture times, the results showed that a total of 5784 differentially expressed genes were screened, which contained 239 transcription factors. KEGG analysis showed that these differentially expressed genes were mainly enriched in metabolic pathways and biosynthesis of secondary metabolites. A proposed temporal analysis of differentially expressed genes among the two groups distributed the differentially expressed genes under nine clusters, and the differentially expressed genes under different clusters had the same expression trends, indicating that these genes can be jointly involved in specific biological processes. Extraction of ginsenosides from ginseng adventitious roots using water-saturated n-butanol and detection of ginsenoside content by high-performance liquid chromatography revealed a significant increase in total saponins and protopanaxadiol ginsenosides (particularly significant for ginsenosides Rd and Rb1), an increase in bioaccumulation of some protopanaxatriol ginsenosides, and a decrease in some protopanaxatriol ginsenosides (S-Rh1, R-Rg3, and Rf) saponin content decreased. We also found seven genes involved in ginsenoside biosynthesis and that the changes in these genes’ expression may be related to the accumulation of ginsenosides. Full article

Ginsenosides are a group of bioactive compounds isolated from Panax ginseng. Conventional major ginsenosides have a long history of use in traditional medicine for both illness prevention and therapy. Bioconversion processes have the potential to create new and valuable products in pharmaceutical and biological activities, making them both critical for research and highly economic to implement. This has led to an increase in the number of studies that use major ginsenosides as a precursor to generate minor ones using β-glucosidase. Minor ginsenosides may also have useful properties but are difficult to isolate from raw ginseng because of their scarcity. Bioconversion processes have the potential to create novel minor ginsenosides from the more abundant major ginsenoside precursors in a cost-effective manner. While numerous bioconversion techniques have been developed, an increasing number of studies have reported that β-glucosidase can effectively and specifically generate minor ginsenosides. This paper summarizes the probable bioconversion mechanisms of two protopanaxadiol (PPD) and protopanaxatriol (PPT) types. Other high-efficiency and high-value bioconversion processes using complete proteins isolated from bacterial biomass or recombinant enzymes are also discussed in this article. This paper also discusses the various conversion and analysis methods and their potential applications. Overall, this paper offers theoretical and technical foundations for future studies that will be both scientifically and economically significant. Full article

Ginsenosides, the main active compounds in Panax species, are glycosides of protopanaxadiol (PPD) or protopanaxatriol (PPT). PPT-type ginsenosides have unique pharmacological activities on the central nervous system and cardiovascular system. As an unnatural ginsenoside, 3,12-Di-O-β-D-glucopyranosyl-dammar-24-ene-3β,6α,12β,20S-tetraol (3β,12β-Di-O-Glc-PPT) can be synthesized through enzymatic reactions but is limited by the expensive substrates and low catalytic efficiency. In the present study, we successfully produced 3β,12β-Di-O-Glc-PPT in Saccharomyces cerevisiae with a titer of 7.0 mg/L by expressing protopanaxatriol synthase (PPTS) from Panax ginseng and UGT109A1 from Bacillus subtilis in PPD-producing yeast. Then, we modified this engineered strain by replacing UGT109A1 with its mutant UGT109A1-K73A, overexpressing the cytochrome P450 reductase ATR2 from Arabidopsis thaliana and the key enzymes of UDP-glucose biosynthesis to increase the production of 3β,12β-Di-O-Glc-PPT, although these strategies did not show any positive effect on the yield of 3β,12β-Di-O-Glc-PPT. However, the unnatural ginsenoside 3β,12β-Di-O-Glc-PPT was produced in this study by constructing its biosynthetic pathway in yeast. To the best of our knowledge, this is the first report of producing 3β,12β-Di-O-Glc-PPT through yeast cell factories. Our work provides a viable route for the production of 3β,12β-Di-O-Glc-PPT, which lays a foundation for drug research and development. Full article

Light is essential for plants and plays a vital role in their growth and development. Light irradiation affects the physiological characteristics and synthesis of secondary metabolites in plants. As a semi-shade perennial plant, Panax ginseng C.A. Mey. is sensitive to changes in the light environment. Different light irradiations significantly affect the secondary metabolic processes of P. ginseng. However, few studies have investigated the changes in ginsenoside content in P. ginseng under different light irradiation conditions. In this study, 3-year-old P. ginseng was cultured under white (CK) light, blue (B) light, red (R) light, green (G) light, and natural light (NL) to explore the effects of light irradiation on the physiological characteristics and ginsenoside secondary metabolism of P. ginseng. The B and CK treatments significantly increased the photosynthetic level in P. ginseng leaves. The total saponin content under blue and red light treatments increased by 28.81% and 21.64%, respectively, compared with the CK treatment. Blue and red light improved the transcription levels of ginsenoside biosynthetic pathway genes. Blue light upregulated the expression of HMGR, SS, SE, DS, CYP716A52, and CYP716A47, and the expression of HMGR, SS, SE, DS, and CYP716A47 under red light treatment was significantly upregulated in P. ginseng roots. Principal component and correlation analyses revealed that the physiological and ecological processes of P. ginseng exhibited different responses to light irradiation. The total saponin content in the roots was positively correlated with the content of protopanaxatriol -type ginsenosides and water use efficiency in leaves. Our study indicates that light conditions can be improved by blue and red light or by blue and red film covering to facilitate the accumulation of saponin during the ecological cultivation of P. ginseng. Full article

Wound healing is the process of skin and soft tissue repair following an injury. Angiogenesis is an essential process in wound healing and plays an important role in tissue regeneration. Ginseng is mainly composed of saponins and protopanaxadiol-based ginsenosides, namely Rb1, Rb2, Rc, Re, Rg1, and Rf. 20(S)-protopanaxadiol (PPD) and 20(S)-protopanaxatriol (PPT) are aglycones of ginsenosides produced by metabolic processes and heat treatment. This study aimed to investigate the wound healing effects of active ingredients of ginseng, namely ginsenosides and aglycones, in various cellular and animal skin wound models. The angiogenic effects of ginsenosides were investigated in human umbilical vein endothelial cells (HUVECs). All experiments were conducted at increased intracellular glucose concentrations and the induction of angiogenesis through tube formation was evaluated. Among the ginsenosides and aglycones used in this study, PPD showed the strongest wound-healing activity. Cell scratch experiments confirmed that PPD increased intracellular proliferation and cell migration at high glucose concentrations, and western blotting of HUVECs showed that phosphorylated ERK, Akt, and p38 were regulated. We observed accelerated wound healing with PPD treatment in STZ-treated mice. Overall, the findings suggested that PPD could possibly help improve skin wound healing in patients with diabetes, although further research is recommended. Full article