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Osteoarthritis (OA), caused by the long-term use of joints, is a representative degenerative disease in the elderly. However, recently, the age of onset has been decreasing owing to excessive activities among young people in their 20s and 30s. Gynostemma pentaphyllum (Thunb.) Makino (GP), a perennial herb of the Cucurbitaceae family, has been used since the Ming dynasty as a medicinal material to treat various ailments, such as rheumatism, liver disease, and diabetes. In this study, we investigated the anti-arthritic effects of heat-processed Gynostemma pentaphyllum extract (Actiponin (AP)) and its derivatives, damulin A (DA) and damulin B (DB), using in vitro (primary rat chondrocytes and SW1353 cells) and in vivo (destabilization of the medial meniscus (DMM)-induced OA model) systems. Histological analysis results from the in vivo study showed that the group that underwent DMM surgery induced degeneration by the loss of proteoglycan and the destruction of cartilage (OARSI score 14 ± 0.57), whereas the group that received AP daily for 8 weeks maintained an intact condition (OARSI score 5 ± 0.28 at 200 mg/kg, p < 0.001). In addition, cartilage thickness and chondrocytes were reduced in the DMM group, but were restored in the AP-administered group. Furthermore, the von Frey analysis results showed that the pain threshold of the DMM group was considerably low (54.5 g at 8 weeks), whereas that of the AP group was dose-dependently increased (65.5, 69.5, 70.3, and 71.8 at 8 weeks for 30, 50, 100, and 200 mg/kg, respectively). In vitro studies showed that AP, DA, and DB reduced the expression of interleukin-1β alone-induced nitrite; inducible nitric oxide synthase; cyclooxygenase-2; matrix metallopeptidase 1/3/13; and a disintegrin and metalloproteinase with thrombospondin motifs 4/5. They also restored the expression of collagen type II and aggrecan, which are components of the extracellular matrix. The anti-arthritic effects of AP, DA, and DB were confirmed to be mediated by the mitogen-activated protein kinase and nuclear factor kappa-light-chain-enhancer of activated B cell signaling pathways. Collectively, these results suggest that AP is a potential therapeutic agent for mitigating OA progression and chondroprotection. [ABSTRACT FROM AUTHOR] more...

Objective: To observe the protective effects of Gynostemma pentaphyllum saponins (GPs) on liver injury in guinea pigs of hyperlipemia based on oxidative stress. Methods: A total of 32 guinea pigs were randomly divided into a model group, a low dose GPs group (85 mg/kg), a high dose GPs group (170 mg/kg), and a simvastatin group (1.5 mg/kg), with 8 animals in each group. All animals were fed with high-fat diet for 5 weeks to prepare a hyperlipemia model. At the same time, 8 guinea pigs were set up as a normal group and given regular feed. From the 6 th week onwards, hyperlipemia model guinea pigs were fed with high-fat diet go on, and were given intragastric administration at the same time, once a day for 4 consecutive weeks. The normal group and model group were given equal amount of normal saline. The body mass, body length, and Lee's index of each group of guinea pigs were measured weekly. After the experiment, the levels of total TC, TG, HDL and LDL of guinea pigs were measured. The liver mass, liver to body ratio, and fasting blood glucose of guinea pigs were measured. The levels of SOD, MDA, CAT and GSH-px in the liver were detected. HE and oil red staining were used to observe the pathological and morphological changes of guinea pig liver tissue. Immunofluorescence method was used to observe the protein expression of Nrf2 and HO-1 in the liver of guinea pigs. Results: At the end of the experiment, compared with the model group, the high dose and low dose group of GPs significantly decreased the level of the body mass (P<0.01) in hyperlipidemic guinea pigs. The low dose group of GPs significantly decreased the Lee's index (P<0.05). The high dose group of GPs significantly decreased the Lee's index (P<0.01). The low dose group of GPs significantly decreased the levels of TG and LDL in serum (P<0.05, P<0.01). The high dose group of GPs significantly decreased the levels of TC, TG, and LDL in serum (P<0.05, P<0.01). The low dose group of GPs significantly decreased the level of MDA in the liver tissue (P<0.05). The high dose group of GPs significantly increased the level of SOD (P<0.05), and decreased the level of MDA (P<0.01) in the liver tissue. Pathology showed that the high dose group of GPs reduced the fatty degeneration and lipid droplet accumulation in the hepatocytes of hyperlipidemic guinea pigs. The fluorescence expression of Nrf2 and HO-1 proteins in both the high and low dose groups of GPs significantly increased (P<0.01). Conclusion: GPs would have a good hepatic protective effect through significantly improve oxidative stress levels by activate the Nrf2/HO-1 signaling pathway in guinea pigs of hyperlipemia. [ABSTRACT FROM AUTHOR] more...

In Vietnam, many herbal plants with various medicinal activities can support different diseases such as anti-anemic and antimicrobial etc including diabetic treatments. Diabetes mellitus is a group of metabolic disorders that is characterized by elevated levels of glucose in the blood. When combining the herbs following a formula, the healing effect will be more effective due to synergetic actions. Our present study assesses acute toxicity and antidiabetic activity of a new polyherbal preparation, CHMTieu duong, in the form of capsules. It was developed based on the traditional use of six indigenous plants from the South-Western region of Vietnam, effective in fighting diabetes, namely Andrographis paniculata (leaves), Centella asiatica (leaves), Dioscorea opposite (tuberous rhizomes), Gymnema sylvestre (leaves), Gynostemma pentaphyllum (herbs), and Morus alba (leaves). Methods: The acute toxicity was evaluated following the Organization for Economic Cooperation and Development (OECD) guidelines No. 420 using five lots of female BALB/c albino mice. The antidiabetic activity was studied using an alloxan-induced diabetic mice model on thirty BALB/c albino mice of either sex. The mice were divided into five groups, namely normal mice control group with normal saline, diabetic mice fasted control group with normal saline, diabetic mice positive control group treated with the standard drug, metformin at a dose of 100 mg/kgP, and two diabetic mice groups treated with different doses of herbal combination at 500 and 1000 mg/kgP. Resutls: The acute toxicity analysis showed that CHM-Tieu duong was orally non-toxic at a single dose of 5000 mg/kgP as it did not cause any pre-clinical changes in experimental mice. The results of the antidiabetic study showed that CHM-Tieu duong exhibited the lowering glucose levels in the alloxan-induced diabetic mice model at the high dose of 1000 mg/kgP dose. Conclusion: The findings demonstrated that CHM-Tieu duong could serve as safe and effective antidiabetic polyherbal combination. [ABSTRACT FROM AUTHOR] more...

Introduction: Traditional Eastern medicine (TEM) is becoming increasingly more popular in highly developed Western countries as an alternative form of supporting health and body care. Many herbs used in this medical practice possess antioxidant, anti-inflammatory and immunomodulatory effects. The skin aging process may progress with age, when collagen and elastin fibers gradually decrease. Excessive exposure to UV radiation, resulting in an increase in the production of free radicals, leads to damage at the molecular level to numerous structures in the body including the acceleration of skin aging. Material and methods: The content of polyphenolic compounds (among others: phenolic acids and flavonoids), antioxidant potential (ABTS, DPPH and FRAP assays) as well as the influence on the activity of enzymes, collagenase and elastase, were determined in infusions obtained from Gynostemma pentaphyllum, Tinospora cordifolia, Astragalus membranaceus, Codonopsis pilosula, Asparagus racemosus and Ocimum sanctum. Results: The highest content of polyphenolic compounds and the strongest antioxidant properties were observed in the infusions obtained from the O. sanctum herb, while the greatest ability to inhibit collagenase and elastase was observed in the infusions obtained from the T. cordifolia leaves. Conclusions: Infusions from the O. sanctum herb and T. cordifolia leaves may have a potentially beneficial effect on the skin and may be used in anti-aging formulations. more...

Medicinal plants have long played a crucial role in healthcare systems, but limited genomic information on these species has impeded the integration of modern biological technologies into medicinal plant research. In this study, we selected nine common medicinal plants, each belonging to a different plant family, including Sarcandra glabra (Chloranthaceae), Nekemias grossedentata (Vitaceae), Uraria crinita (Fabaceae), Gynostemma pentaphyllum (Cucurbitaceae), Reynoutria japonica (Polygonaceae), Pseudostellaria heterophylla (Caryophyllaceae), Morinda officinalis (Rubiaceae), Vitex rotundifolia (Lamiaceae), and Gynura formosana (Asteraceae), to estimate their genome sizes and conduct preliminary genomic surveys. The estimated genome sizes by flow cytometry were 3.66 Gb, 0.65 Gb, 0.58 Gb, 1.02 Gb, 3.96 Gb, 2.99 Gb, 0.43 Gb, 0.78 Gb, and 7.27 Gb, respectively. The genome sizes of M. officinalis, R. japonica, and G. pentaphyllum have been previously reported. Comparative analyses suggest that variations in genome size may arise due to differences in measurement methods and sample sources. Therefore, employing multiple approaches to assess genome size is necessary to provide more reliable information for further genomic research. Based on the genome survey, species with considerable genome size variation or polyploidy, such as G. pentaphyllum, should undergo a ploidy analysis in conjunction with population genomics studies to elucidate the development of the diversified genome size. Additionally, a genome survey of U. crinita, a medicinal plant with a relatively small genome size (509.08 Mb) and of considerable interest in southern China, revealed a low heterozygosity rate (0.382%) and moderate repeat content (51.24%). Given the limited research costs, this species represents a suitable candidate for further genomic studies on Leguminous medicinal plants characteristic of southern China. This foundational genomic information will serve as a critical reference for the sustainable development and utilization of these medicinal plants. [ABSTRACT FROM AUTHOR] more...

Gynostemma pentaphyllum is a traditional Chinese medicinal plant of considerable application value and commercial potential, primarily due to its production of various bioactive compounds, particularly dammarane-type triterpenoid saponins that are structurally analogous to ginsenosides. Oxidosqualene cyclase (OSC), a pivotal enzyme in the biosynthesis of triterpenoid metabolites in plants, catalyzes the conversion of oxidosqualene into triterpenoid precursors, which are essential components of the secondary metabolites found in G. pentaphyllum. To elucidate the role of OSC gene family members in the synthesis of gypenosides within G. pentaphyllum, this study undertook a comprehensive genome-wide identification and characterization of OSC genes within G. pentaphyllum and compared their expression levels across populations distributed over different geographical regions by both transcriptome sequencing and qRT-PCR experimental validation. The results identified a total of 11 members of the OSC gene family within the genome of G. pentaphyllum. These genes encode proteins ranging from 356 to 767 amino acids, exhibiting minor variations in their physicochemical properties, and are localized in peroxisomes, cytoplasm, plasma membranes, and lysosomes. All GpOSCs contain highly conserved DCTAE and QW sequences that are characteristic of the OSC gene family. A phylogenetic analysis categorized the GpOSCs into four distinct subfamilies. A cis-element analysis of the GpOSC promoters revealed a substantial number of abiotic stress-related elements, indicating that these genes may respond to drought conditions, low temperatures, and anaerobic environments, thus potentially contributing to the stress resistance observed in G. pentaphyllum. Expression analyses across different G. pentaphyllum populations demonstrated significant variability in OSC gene expression among geographically diverse samples of G. pentaphyllum, likely attributable to genetic variation or external factors such as environmental conditions and soil composition. These differences may lead to the synthesis of various types of gypenosides within geographically distinct G. pentaphyllum populations. The findings from this study enhance our understanding of both the evolutionary history of the OSC gene family in G. pentaphyllum and the biosynthetic mechanisms underlying triterpenoid compounds. This knowledge is essential for investigating molecular mechanisms involved in forming dammarane-type triterpenoid saponins as well as comprehending geographical variations within G. pentaphyllum populations. Furthermore, this research lays a foundation for employing plant genetic engineering techniques aimed at increasing gypenoside content. [ABSTRACT FROM AUTHOR] more...

Hydrogen-rich Gynostemma pentaphyllum Makino distillate (HRGD) is produced by distilling G. pentaphyllum Makino, with the addition of hydrogen gas. This study sought to explore the pharmacological and biological impacts of HRGD on the generation of pro-inflammatory cytokines and mediators in macrophages. The cells were treated with various concentrations of HRGD (2, 4 and 8 μg/mL) in the absence or presence of lipopolysaccharide (LPS) (1 μg/mL) for 24 h. The results indicated that HRGD is an effective inhibitor of LPS-induced nitric oxide (NO·) production in RAW 264.7 cells: The NO· concentration was reduced dramatically after treatment with 8 μg/m98L HRGD (11.8 μM) compared to the LPS-induced group (28.4 μM). These inhibitory effects of HRGD included a dose-dependent decrease in the expression of cyclooxygenase-2 (COX-2) and prostaglandin E2 (PGE2) proteins. To evaluate the inhibitory effects of HRGD on other cytokines, we also measured cytokines tumor necrosis factor-α (TNF-α) level in the cell supernatants of LPS-stimulated RAW 264.7 macrophages by enzyme-linked immunosorbent assay. In this assay, HRGD significantly decreased the expression of TNF-α in a dose-dependent manner (p < 0.05). The study also performed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on macrophages. HRGD did not display any cytotoxicity in this assay. The findings demonstrated that HRGD could modulate macrophage-mediated inflammatory functions such as the overproduction of cytokines, NO· and PGE2 without any cytotoxic. [ABSTRACT FROM AUTHOR] more...

This study aims to investigate selected medicinal plants' anti-oxidative and antihyperglycemic activities to develop an effective remedy for lowering blood glucose levels and/or reducing diabetes complications. Thai medicinal plants, reported to have blood sugar-lowering effects, were selected for the study: Coccinia grandis, Gymnema inodorum, Gynostemma pentaphyllum, Hibiscus sabdariffa, Momordica charantia, Morus alba, and Zingiber officinale. Each species was extracted by Soxhlet's extraction using ethanol as solvent. The ethanolic crude extract of each species was then evaluated for its phytochemicals, anti-oxidant, and antihyperglycemic activities. The results showed that the extract of Z. officinale gave the highest values of total phenolic and total flavonoid content (167.95 mg gallic acid equivalents (GAE)/g and 81.70 mg CE/g, respectively). Anti-oxidant activity was determined using DPPH and ABTS radical scavenging activity. Among the ethanolic extracts, Z. officinale exhibited the highest anti-oxidant activity with IC50 values of 19.16 and 8.53 µg/mL, respectively. The antihyperglycemic activity was assessed using α-glucosidase inhibitory and glucose consumption activities. M. alba and G. pentaphyllum demonstrated the highest α-glucosidase inhibitory activity among the ethanolic extracts, with IC50 values of 134.40 and 329.97 µg/mL, respectively. Z. officinale and H. sabdariffa showed the highest percentage of glucose consumption activity in induced insulin-resistant HepG2 cells at a concentration of 50 µg/mL with 145.16 and 107.03%, respectively. The results from α-glucosidase inhibitory and glucose consumption activities were developed as an effective antihyperglycemic remedy. Among the remedies tested, the R1 remedy exhibited the highest potential for reducing blood glucose levels, with an IC50 value of 122.10 µg/mL. Therefore, the R1 remedy should be further studied for its effects on animals. [ABSTRACT FROM AUTHOR] more...

Gynostemma pentaphyllum, a traditional Chinese medicine, is widely used to treat various diseases, but its therapeutic effects and mechanisms of action on hyperlipidemia remain unclear. This study aims to investigate the effects of Danshen leaf on hyperlipidemia through network pharmacology, molecular docking, and cellular experiments, elucidating its multifaceted mechanism of action within the LOX1‐PI3K‐AKT‐eNOS pathway. First, the active ingredients and targets of G. pentaphyllum were screened using the Traditional Chinese Medicine Systems Pharmacology database. Then, targets for hyperlipidemia were identified using the OMIM and GeneCards databases, and potential therapeutic targets for G. pentaphyllum in treating hyperlipidemia were determined. An active ingredient‐target network was constructed using Cytoscape software, and a protein–protein interaction (PPI) network was built and visualized using the STRING database and Cytoscape software. Finally, GO functional and KEGG pathway enrichment analyses were performed, and the predicted mechanisms were validated through molecular docking and cell experiments. 85 targets for G. pentaphyllum and 1556 for Hyperlipidemia were screened, with 53 common targets. Twenty‐four active ingredients of G. pentaphyllum were found to be involved in the treatment of hyperlipidemia. Key nodes such as Rhamnazin, Isofucosterol, and quercetin, and targets NCOA2, NR3C2, PGR, and PPARG showed high relevance. In the PPI network, 8 nodes, including IL6, PPARG, and VEGFA, exhibited high centrality. GO functional and KEGG pathway enrichment analyses indicated that G. pentaphyllum may treat hyperlipidemia by influencing various biological functions and pathways, such as DNA‐binding transcription factor binding, RNA polymerase II‐specific DNA‐binding transcription factor binding, and lipid and atherosclerosis. Cell experiments demonstrated that G. pentaphyllum significantly regulated the expression of key proteins in the LOX1‐PI3K‐AKT‐eNOS pathway, thereby improving hyperlipidemia. G. pentaphyllum improves hyperlipidemia by mediating the LOX1‐PI3K‐AKT‐eNOS pathway. This study provides a new theoretical basis and experimental evidence for applying G. pentaphyllum to treating hyperlipidemia. [ABSTRACT FROM AUTHOR] more...

ABSTRACT: Gynostemma pentaphyllum (Thunb.) Makino (G. pentaphyllum) is used in traditional Chinese medicine to stimulate immune responses and reduce blood lipid concentrations, and has broad market growth prospects. In this study, a nutrient liquid culture method has been modified by adding nitrogen and or chemical mimic of saponin precursor to stimulate rooting from stem cuttings. Furthermore, total nitrogen concentration and ammonia/nitrate ratio in the nutrient solution has been optimized; And, the concentration of three ginsenosides precursors that applicated in nutrition solution together with total nitrogen and ammonium/nitrate ratio were studied. The results showed that, after 10 days of culture, adventitious roots developed from stem cuttings to form complete regenerated plantlets. The addition of 1 mg·L-1 indole acetic acid in hydroponic solution could effectively increase the length and number of adventitious roots. The optimal total nitrogen concentration in the nutrient solution for increase in fresh biomass of G. pentaphyllum was 7.0 mmol·L-1 and the optimal ammonium/nitrate ratio was 2:3 for increase in the plant fresh weight, and chlorophyll a, chlorophyll b, and total chlorophyll contents of G. pentaphyllum rooted cuttings. Addition to the nutrient solution of three chemical mimics of saponin precursors sodium acetate (0.5 mmol·L-1), geraniol (0.5 mmol·L-1), and DL-mevalonolactone (0.3 mmol·L-1) increased the content and yield of total saponins. more...

Non-alcoholic fatty liver disease (NAFLD) is one of the most common metabolic diseases encountered in clinical practice, which is characterized by the excessive accumulation of triglycerides (steatosis), and a variety of metabolic abnormalities including lipid metabolism and bile acid metabolism are closely related to NAFLD. In China, Gynostemma pentaphyllum is used as functional food and Chinese medicine to treat various diseases, especially NAFLD, for a long time. However, the active components that exert the main therapeutic effects and their mechanisms remain unclear. In this study, Gypensapogenin A was isolated from the total saponins of G. pentaphyllum and prepared as a liposomal delivery system. Gypensapogenin A liposomes could activate FXR, inhibit the expression of CYP7A1 and CYP8B1, increase the expression of CYP27A1, modulate the ratio of CA and CDCA, decrease the content of CA, and increase the content of CDCA, thus forming a virtuous cycle of activating FXR to play a role in lowering blood lipid levels. [ABSTRACT FROM AUTHOR] more...

Osteoarthritis (OA) is an age-related disease characterized by inflammation, pain, articular cartilage damage, synovitis, and irreversible disability. Gynostemma pentaphyllum (Thunb.) Makino (GP), a herbal medicine traditionally used in East Asia for its anti-inflammatory properties, was investigated for its potential to modulate OA pathology and symptoms. This study evaluated GP's efficacy in inhibiting pain, functional decline, and cartilage destruction in monosodium iodoacetate-induced OA and acetic acid-induced writhing models. Additionally, the effects of GP on OA-related inflammatory targets were assessed via mRNA and protein expression in rat knee cartilage and lipopolysaccharide-induced RAW 264.7 cells. The GP group demonstrated significant pain relief, functional improvement, and cartilage protection. Notably, GP inhibited key inflammatory mediators, including interleukin (IL)-1β, IL-6, matrix metalloproteinases (MMP)-3 and MMP-13, cyclooxygenase-2, and prostaglandin E receptor 2, surpassing the effects of active controls. These findings suggest that GP is a promising candidate for disease-modifying OA drugs and warrants further comprehensive studies. [ABSTRACT FROM AUTHOR] more...

Indoor greening is becoming popular because it provides many benefits for people. However, plant selection for indoor greening is limited to shade-tolerant tropical plants internationally, and little research has been performed to expand the use of native herb plant species. The aim of this research was to study growth characteristics of Japanese native herbs under common light intensity regimes in office buildings. Eight species of Japanese native herbs (Acorus gramineus, Cameilla sinensis, Farfugium japonicum, Gynostemma pentaphyllum, Perilla frutescens var. crispa f. viridis, Petasites japonicus, Sasa veitchii, and Saxifraga stolonifera) were examined in an open growth chamber with light-emitting diode light tape under three light intensities [photosynthetic photon flux densities of 3 µmol⋅m-2⋅s-1 (250 lx), 6 µmol⋅m-2⋅s-1 (500 lx), and 12 µmol⋅m-2⋅s-1 (750 lx)] from 8 AM to 10 PM every day from Jun 2021 to Oct 2021 in an office. Farfugium japonicum and Saxifraga stolonifera were as shade-tolerant as typical tropical plants and grew well under all light intensities. Sasa veitchii performed well under high and medium light intensity. The other plant species require supplemental lightning to achieve sufficient growth indoors. [ABSTRACT FROM AUTHOR] more...

Ginsenoside F2 is a protopanaxadiol saponin compound with various biological activities, including antioxidant, anti-inflammatory, and anticancer properties. Ginsenoside F2 can be found in ginseng, but in low quantities. Therefore, ginsenoside F2 production predominantly relies on the biotransformation of various ginsenosides, such as ginsenosides Rb1 and Rd. In this study, we reported the production of ginsenoside F2 by gypenoside biotransformation with Aspergillus niger JGL8, isolated from Gynostemma pentaphyllum. Ginsenoside F2 could be produced by two different biotransformation pathways, namely Gyp-V–Rd–F2 and Gyp-XVII–F2. The product exhibited antioxidant activity against free radicals (DPPH) with IC50 value of 29.54 µg/mL. Optimal biotransformation conditions were a pH of 5.0, temperature of 40 °C, and 2 mg/mL of substrate. Enzyme kinetic parameters revealed that the hydrolysis rate of Gyp-V, Rd, and Gyp-XVII was 0.625, 0.588, and 0.417 mM/h, respectively. In conclusion, we demonstrated that gypenoside is a substitutable substrate for ginsenoside F2 biotransformation. [ABSTRACT FROM AUTHOR] more...

Chronic liver disease, a long-term condition resulting from various causes such as alcohol abuse, metabolic disorders, and viral hepatitis, is becoming a significant global health challenge. Gypenosides (GPs), derived from the traditional Chinese medicine Gynostemma pentaphyllum (Thunb.) Makino, exhibited hepatoprotective properties in recent years, yet the precise therapeutic mechanism remains unclear. In this study, label-free and parallel reaction monitoring (PRM) proteomics were used to elucidate the hepatoprotective mechanism of GPs in liver injury rats. Through label-free proteomics, we identified 2104 differentially expressed proteins (DEPs) associated with liver injury, along with 1974 DEPs related to the effects of GPs. Bioinformatics analysis revealed that GPs primarily restored metabolic processes involving valine, leucine, and isoleucine degradation, as well as propanoate and butanoate metabolism, and steroid hormone biosynthesis during liver injury. Subsequently, overlapping the two groups of DEPs identified 1508 proteins reversed following GPs treatment, with key targets further validated by PRM. Eight target proteins were identified for GPs treatment of liver injury, including Lgals3, Psat1, Phgdh, Cyp3a9, Cyp2c11, Cyp4a2, Glul, and Ces1d. These findings not only elucidated the hepatoprotective mechanism of GPs, but may also serve as potential therapeutic targets of chronic liver disease. [ABSTRACT FROM AUTHOR] more...

Gynostemma pentaphyllum is commonly used to treat various tumors in China. The aim of the study is to explore the pharmacological mechanism of Gynostemma pentaphyllum in gastric cancer using joint network pharmacology, molecular docking and in vitro experimental verification. First, the active constituents and potential targets of Gynostemma pentaphyllum were screened from a public database and screening of core targets anti-gastric cancer using protein-protein interaction networks. The Cancer Genome Atlas and Human Protein Atlas databases were used to evaluate the messenger ribonucleic acid and protein expression of core target genes in normal gastric epithelium and gastric cancer tissues and their relationship with overall survival in gastric cancer. Functional and pathway enrichment analyses of the potential targets were performed using gene ontology and Kyoto encyclopedia of genes and genomes. Fifteen active components and all related targets of Gynostemma pentaphyllum were retrieved from the Traditional Chinese Medicine Systems Pharmacology database and 127 potential targets were identified by intersection with colorectal cancer-related targets. Protein-protein interaction network analysis showed that six target genes, AKT serine/threonine kinase 1, Jun proto-oncogene and B-cell lymphoma 2 proteins were key genes. Gene ontology enrichment analysis involved 1892 BP, 37 CC and 142 MF. Kyoto encyclopedia of genes and genomes enrichment analysis showed that the anti-cancer effects of Gynostemma pentaphyllum were mediated by advanced glycation end products-receptor for advanced glycation end products, interleukin-17, hypoxia inducible factor 1 and transforming growth factor signalling pathways. Molecular docking revealed that the three core target proteins stably bound to quercetin and rhamnazin. The results of the in vitro experiments showed that both quercetin and rhamnazin inhibited the activity of gastric cancer cells, up-regulated the messenger ribonucleic acid and protein AKT serine/threonine kinase 1 and down-regulated Jun proto-oncogene and B-cell lymphoma 2 protein activities at the specified concentrations. This study revealed the potential role of Gynostemma pentaphyllum in the treatment of gastric using network pharmacology, molecular docking and in vitro experiments. [ABSTRACT FROM AUTHOR] more...

Type 2 diabetes mellitus (T2DM) is a chronic metabolic disease mainly caused by insulin resistance, which can lead to a series of complications such as cardiovascular disease, retinopathy, and its typical clinical symptom is hyperglycaemia. Glucosidase inhibitors, including Acarbose, Miglitol, are commonly used in the clinical treatment of hypoglycaemia. In addition, Protein tyrosine phosphatase 1B (PTP1B) is also an important promising target for the treatment of T2DM. Gynostemma pentaphyllum is a well-known oriental traditional medicinal herbal plant, and has many beneficial effects on glucose and lipid metabolism. In the present study, three new and nine known dammarane triterpenoids isolated from G. pentaphyllum, and their structures were elucidated by spectroscopic methods including HR-ESI-MS,1H and 13C NMR and X-ray crystallography. All these compounds were evaluated for inhibitory activity against α-glucosidase, α-amylase and PTP1B. The results suggested that compounds 7∼10 were potential antidiabetic agents with significantly inhibition activity against PTP1B in a dose-dependent manner. more...

Abstract Background Gynostemma pentaphyllum (Thunb.) Makino, commonly known as “southern ginseng”, contains high amounts of ginsenoside derivatives and exhibits similar biological activities with Panax ginseng (C. A. MEY) (ginseng), which is usually used as a low-cost alternative to ginseng. G. pentaphyllum has therapeutic effects on liver diseases. However, the mechanisms underlying its hepatoprotective action have not been fully elucidated. Methods The protective effects of the ethanolic extract of G. pentaphyllum (GPE) were evaluated using an experimental carbon tetrachloride (CCl4)-induced liver disease model. Potential targets of GPE were predicted using the “Drug-Disease” bioinformatic analysis. Furthermore, comprehensive network pharmacology and transcriptomic approaches were employed to investigate the underlying mechanisms of GPE in the treatment of liver disease. Results The pathological examinations showed that GPE significantly alleviated hepatocyte necrosis and liver injury. GPE significantly downregulated Bax and cleaved-PARP expression and upregulated Bcl-2 expression during CCl4-induced hepatocyte apoptosis. We compared the effects of four typical compounds in GPE -a ginsenoside (Rb3) shared by both GPE and ginseng and three unique gypenosides in GPE. Notably, Gypenoside A (GPA), a unique saponin in GPE, markedly reduced hepatocyte apoptosis. In contrast, ginsenoside Rb3 had a weaker effect. Network pharmacology and transcriptomic analyses suggested that this anti-apoptotic effect was achieved by upregulating the PI3K/Akt signaling pathway mediated by PDK1. Conclusions These results suggested that G. pentaphyllum had a promising hepatoprotective effect, with its mechanism primarily involving the upregulation of the PDK1/Bcl-2 signaling pathway by GPA, thereby preventing cell apoptosis. Graphic Abstract more...

Abstract Gynostemma pentaphyllum (Thunb.) Makino (G. pentaphyllum) is a medicinal and edible plant with multiple functions of liver protection, anti-tumor, anti-inflammation, balancing blood sugar and blood lipids. The nutritional value of the G. pentaphyllum plant is mainly due to its rich variety of biologically active substances, such as flavonoids, terpenes and polysaccharides. In this study, we performed a comprehensive analysis combining metabolomics and root, stem and leaf transcriptomic data of G. pentaphyllum. We used transcriptomics and metabolomics data to construct a dynamic regulatory network diagram of G. pentaphyllum flavonoids and terpenoids, and screened the transcription factors involved in flavonoids and terpenoids, including basic helix-loop-helix (bHLH), myb-related, WRKY, AP2/ERF. Transcriptome analysis results showed that among the DEGs related to the synthesis of flavonoids and terpenoids, dihydroflavonol 4-reductase (DFR) and geranylgeranyl diphosphate synthases (GGPPS) were core genes. This study presents a dynamic image of gene expression in different tissues of G. pentaphyllum, elucidating the key genes and metabolites of flavonoids and terpenoids. This study is beneficial to a deeper understanding of the medicinal plants of G. pentaphyllum, and also provides a scientific basis for further regulatory mechanisms of plant natural product synthesis pathways and drug development. more...

This article provides an analysis of the vascular plant resources and diversity in Fanjing Mountain, Guizhou Province. The study found 284 species of vascular plants in the region, with dominant families including Liliaceae, Asteraceae, Polygonaceae, Leguminosae, Ranunculaceae, and Polygonum. Perennial herbs were the most dominant life type, and 222 species were identified as medicinal vascular plants. The article emphasizes the importance of conserving and utilizing these plant resources in the Fanjing Mountain Nature Reserve. The document also includes a table listing various plant species and their scientific names, organized by family and genus, contributing to research on traditional medicines and biodiversity in the region. [Extracted from the article] more...

Background: Gynostemma pentaphyllum (Thunb.) Makino, a well-known edible and medicinal plant, has anti-aging properties and is used to treataging-associated conditions such as diabetes, metabolic syndrome, and cardiovascular diseases. Gypenosides (GYPs) are the primary constituents of G. pentaphyllum. Increasing evidence indicates that GYPs are effective at preserving mitochondrial homeostasis and preventing heart failure (HF). This study aimed to uncover the cardioprotective mechanisms of GYPs related to mitochondrial regulation. Methods: The bioactive components in GYPs and the potential targets in treating HF were obtained and screened using the network pharmacology approach, followed by drug-disease target prediction and enrichment analyses. The pharmacological effects of GYPs in cardioprotection, mitochondrial function, mitochondrial quality control, and underlying mechanisms were further investigated in Doxorubicin (Dox)-stimulated H9c2 cardiomyocytes. Results: A total of 88 bioactive compounds of GYPs and their respective 71 drug-disease targets were identified. The hub targets covered MAPK, EGFR, PI3KCA, and Mcl-1. Enrichment analysis revealed that the pathways primarily contained PI3K/Akt, MAPK, and FoxO signalings, as well as calcium regulation, protein phosphorylation, apoptosis, and mitophagy process. In Dox-stimulated H9c2 rat cardiomyocytes, pretreatment with GYPs increased cell viability, enhanced cellular ATP content, restored basal oxygen consumption rate (OCR), and improved mitochondrial membrane potential (MMP). Furthermore, GYPs improved PINK1/parkin-mediated mitophagy without influencing mitochondrial fission/fusion proteins and the autophagic LC3 levels. Mechanistically, the phosphorylation of PI3K, Akt, GSK-3β, and the protein level of Mcl-1 was upregulated by GYP treatment. Conclusion: Our findings reveal that GYPs exert cardioprotective effects by rescuing the defective mitophagy, and PI3K/Akt/GSK-3β/Mcl-1 signaling is potentially involved in this process. [ABSTRACT FROM AUTHOR] more...

Medicinal plants, are resources of traditional medicines, have played a significant role in human culture throughout history. The connect of traditional knowledge with contemporary scientific findings, display the potential of these plants for nutritional and pharmaceutical applications. This study aimed to investigates the antioxidant activity and phenolic compositions of seven medicinal plants (Kaempferia parviflora, Hibiscus sabdariffa, Phyllanthus emblica, Terminalia chebula, Terminalia bellirica, Gynostemma pentaphyllum, and Stevia rebaudiana) from Kalasin Province, Thailand. 1,1-diphenyl-2-picrylhydrazyl (DPPH) and ferric-reducing antioxidant power (FRAP) assays were used to evaluate the the antioxidant activities. The qualitative method was used for the phytochemical screening. Additionally, reverse-phase high-performance liquid chromatography (RP-HPLC) analysis reveals their phenolic compositions. Results revealed that phenols, flavonoids, and terpenoids were found in all medicinal plants studied, with flavonoids and phenols most predominant. Notably, P. emblica and T. bellirica show significant antioxidant properties and high levels of phenolics and flavonoids. P. emblica had the highest phenolic acid concentrations, with ρ-coumaric (79.43 µg/g), chlorogenic (45.22 µg/g), and ferulic acid (29.58 µg/g) being dominant. The research emphasizes the value of these plants in developing functional foods and pharmaceuticals, underlining the importance of conserving biodiversity and traditional knowledge for future health product innovation. [ABSTRACT FROM AUTHOR] more...

NASH (non-alcoholic steatohepatitis) is a severe liver disease characterized by hepatic chronic inflammation that can be associated with the gut microbiota. In this study, we explored the therapeutic effect of Gynostemma pentaphyllum extract (GPE), a Chinese herbal extract, on methionine- and choline-deficient (MCD) diet-induced NASH mice. Based on the peak area, the top ten compounds in GPE were hydroxylinolenic acid, rutin, hydroxylinoleic acid, vanillic acid, methyl vanillate, quercetin, pheophorbide A, protocatechuic acid, aurantiamide acetate, and iso-rhamnetin. We found that four weeks of GPE treatment alleviated hepatic confluent zone inflammation, hepatocyte lipid accumulation, and lipid peroxidation in the mouse model. According to the 16S rRNA gene V3–V4 region sequencing of the colonic contents, the gut microbiota structure of the mice was significantly changed after GPE supplementation. Especially, GPE enriched the abundance of potentially beneficial bacteria such as Akkerrmansia and decreased the abundance of opportunistic pathogens such as Klebsiella. Moreover, RNA sequencing revealed that the GPE group showed an anti-inflammatory liver characterized by the repression of the NF-kappa B signaling pathway compared with the MCD group. Ingenuity Pathway Analysis (IPA) also showed that GPE downregulated the pathogen-induced cytokine storm pathway, which was associated with inflammation. A high dose of GPE (HGPE) significantly downregulated the expression levels of the tumor necrosis factor-α (TNF-α), myeloid differentiation factor 88 (Myd88), cluster of differentiation 14 (CD14), and Toll-like receptor 4 (TLR4) genes, as verified by real-time quantitative PCR (RT-qPCR). Our results suggested that the therapeutic potential of GPE for NASH mice may be related to improvements in the intestinal microenvironment and a reduction in liver inflammation. [ABSTRACT FROM AUTHOR] more...

Gynostemma pentaphyllum (Thunb.) Makino is an important producer of dammarene-type triterpenoid saponins. These saponins (gypenosides) exhibit diverse pharmacological benefits such as anticancer, antidiabetic, and immunomodulatory effects, and have major potential in the pharmaceutical and health care industries. Here, we employed single-cell RNA sequencing (scRNA-seq) to profile the transcriptomes of more than 50,000 cells derived from G. pentaphyllum shoot apexes and leaves. Following cell clustering and annotation, we identified five major cell types in shoot apexes and four in leaves. Each cell type displayed substantial transcriptomic heterogeneity both within and between tissues. Examining gene expression patterns across various cell types revealed that gypenoside biosynthesis predominantly occurred in mesophyll cells, with heightened activity observed in shoot apexes compared to leaves. Furthermore, we explored the impact of transposable elements (TEs) on G. pentaphyllum transcriptomic landscapes. Our findings the highlighted the unbalanced expression of certain TE families across different cell types in shoot apexes and leaves, marking the first investigation of TE expression at the single-cell level in plants. Additionally, we observed dynamic expression of genes involved in gypenoside biosynthesis and specific TE families during epidermal and vascular cell development. The involvement of TE expression in regulating cell differentiation and gypenoside biosynthesis warrant further exploration. Overall, this study not only provides new insights into the spatiotemporal organization of gypenoside biosynthesis and TE activity in G. pentaphyllum shoot apexes and leaves but also offers valuable cellular and genetic resources for a deeper understanding of developmental and physiological processes at singlecell resolution in this species. [ABSTRACT FROM AUTHOR] more...

Background: Gynostemma pentaphyllum (Thunb.) Makino, commonly known as "southern ginseng", contains high amounts of ginsenoside derivatives and exhibits similar biological activities with Panax ginseng (C. A. MEY) (ginseng), which is usually used as a low-cost alternative to ginseng. G. pentaphyllum has therapeutic effects on liver diseases. However, the mechanisms underlying its hepatoprotective action have not been fully elucidated. Methods: The protective effects of the ethanolic extract of G. pentaphyllum (GPE) were evaluated using an experimental carbon tetrachloride (CCl4)-induced liver disease model. Potential targets of GPE were predicted using the "Drug-Disease" bioinformatic analysis. Furthermore, comprehensive network pharmacology and transcriptomic approaches were employed to investigate the underlying mechanisms of GPE in the treatment of liver disease. Results: The pathological examinations showed that GPE significantly alleviated hepatocyte necrosis and liver injury. GPE significantly downregulated Bax and cleaved-PARP expression and upregulated Bcl-2 expression during CCl4-induced hepatocyte apoptosis. We compared the effects of four typical compounds in GPE -a ginsenoside (Rb3) shared by both GPE and ginseng and three unique gypenosides in GPE. Notably, Gypenoside A (GPA), a unique saponin in GPE, markedly reduced hepatocyte apoptosis. In contrast, ginsenoside Rb3 had a weaker effect. Network pharmacology and transcriptomic analyses suggested that this anti-apoptotic effect was achieved by upregulating the PI3K/Akt signaling pathway mediated by PDK1. Conclusions: These results suggested that G. pentaphyllum had a promising hepatoprotective effect, with its mechanism primarily involving the upregulation of the PDK1/Bcl-2 signaling pathway by GPA, thereby preventing cell apoptosis. [ABSTRACT FROM AUTHOR] more...

Ischemia/reperfusion (I/R) injury is one of the major causes of cardiovascular disease. Gypenoside A (GP), the main active component of Gynostemma pentaphyllum, alleviates myocardial I/R injury. Circular RNAs (circRNAs) and microRNAs (miRNAs) are involved in the I/R injury. We explored the protective effect of GP on human cardiomyocytes (HCMs) via the circ_0010729/miR-370-3p/RUNX1 axis. Overexpression of circ_0010729 abolished the effects of GP on HMC, such as suppression of apoptosis and increase in cell viability and proliferation. Overexpression of miR-370-3p reversed the effect of circ_0010729 overexpression, resulting in the stimulation of HMC viability and proliferation and inhibition of apoptosis. The knockdown of miR-370-3p suppressed the effects of GP in HCMs. RUNX1 silencing counteracted the effect of miR-370-3p knockdown and maintained GP-induced suppression of apoptosis and stimulation of HMC viability and proliferation. The levels of RUNX1 mRNA and protein were reduced in cells expressing miR-370-3p. In conclusion, this study confirmed that GP alleviated the I/R injury of myocardial cell via the circ_0010729/miR-370-3p/RUNX1 axis. [ABSTRACT FROM AUTHOR] more...

Alopecia, a prevalent yet challenging condition with limited FDA-approved treatments which is accompanied by notable side effects, necessitates the exploration of natural alternatives. This study elucidated the hair growth properties of Gynostemma pentaphyllum leaf hydrodistillate (GPHD) both in vitro and in vivo. Furthermore, damulin B, a major component of GPHD, demonstrated hair growth-promoting properties in vitro. Beyond its established anti-diabetic, anti-obesity, and anti-inflammatory attributes, GPHD exhibited hair growth induction in mice parallel to minoxidil. Moreover, it upregulated the expression of autocrine factors associated with hair growth, including VEGF, IGF-1, KGF, and HGF. Biochemical assays revealed that minoxidil, GPHD, and damulin B induced hair growth via the Wnt/β-catenin pathway through AKT signaling, aligning with in vivo experiments demonstrating improved expression of growth factors. These findings suggest that GPHD and damulin B contribute to the hair growth-inducing properties of dermal papilla cells through the AKT/β-catenin signaling pathway. [ABSTRACT FROM AUTHOR] more...

Abstract Background Gynostemma pentaphyllum, an ancient Chinese herbal medicine, serves as a natural source of gypenosides with significant medicinal properties. Basic helix-loop-helix (bHLH) transcription factors play pivotal roles in numerous biological processes, especially in the regulation of secondary metabolism in plants. However, the characteristics and functions of the bHLH genes in G. pentaphyllum remain unexplored, and their regulatory role in gypenoside biosynthesis remains poorly elucidated. Results This study identified a total of 111 bHLH members in G. pentaphyllum (GpbHLHs), categorizing them into 26 subgroups based on shared conserved motif compositions and gene structures. Collinearity analysis illustrated that segmental duplications predominately lead to the evolution of GpbHLHs, with most duplicated GpbHLH gene pairs undergoing purifying selection. Among the nine gypenoside-related GpbHLH genes, two GpbHLHs (GpbHLH15 and GpbHLH58) were selected for further investigation based on co-expression analysis and functional prediction. The expression of these two selected GpbHLHs was dramatically induced by methyl jasmonate, and their nuclear localization was confirmed. Furthermore, yeast one-hybrid and dual-luciferase assays demonstrated that GpbHLH15 and GpbHLH58 could bind to the promoters of the gypenoside biosynthesis pathway genes, such as GpFPS1, GpSS1, and GpOSC1, and activate their promoter activity to varying degrees. Conclusions In conclusion, our findings provide a detailed analysis of the bHLH family and valuable insights into the potential use of GpbHLHs to enhance the accumulation of gypenosides in G. pentaphyllum. more...

The extraction process of gypenosides by using ultrasonic-assisted aqueous two-phase system and its hypoglycemic activity were investigated. Six kinds of aqueous two-phase systems (ATPS) composed with different components were prepared. The yield of gypenosides served as an indicator, and ATPS with the highest yield were selected. According to the single factor experiments and response surface methods, liquid material ratio, ultrasonic time and extraction temperature were optimized for the optimum extraction parameters of gypenosides. Meanwhile, the advantages of aqueous two-phase extraction was evaluated by principal component analysis, molecular docking and hypoglycemic activity. As results, 30% ethanol-20% ammonium sulfate was chosen as the optimal extraction solvent system of gypenoside, and the optimum extraction parameters were as follow: Liquid-solid ratio (28:1 mL/g), ultrasonic time (52 min) and extraction temperature (52 ℃). Under the above extraction condition, the yield of gypenoside and the inhibition IC50 value of gypenoside on α-glucosidase were 7.91% and 20.2 μg/mL, respectively. The yield of gypenoside XLIX, ginsenoside Rb3, gypenoside A and gypenoside XVII were 0.83%, 0.09%, 1.42% and 4.04%, respectively. And the binding energy between gypenoside XLIX, ginsenoside Rb3, gypenoside A and gypenoside XVII and α-glucosidase were −9.4, −7.7, −7.7, −7.7 kcal/mol, respectively. Compared with the ethanol extract, the yield and content of gypenoside, the hypoglycemic activity of ATPS extract was enhanced. Therefore, ATPS could effectively improve the extraction of gypenosides, and would provide the scientific evidence for the resource development and utilization of Gynostemma pentaphyllum. more...

Background: Gynostemma pentaphyllum, an ancient Chinese herbal medicine, serves as a natural source of gypenosides with significant medicinal properties. Basic helix-loop-helix (bHLH) transcription factors play pivotal roles in numerous biological processes, especially in the regulation of secondary metabolism in plants. However, the characteristics and functions of the bHLH genes in G. pentaphyllum remain unexplored, and their regulatory role in gypenoside biosynthesis remains poorly elucidated. Results: This study identified a total of 111 bHLH members in G. pentaphyllum (GpbHLHs), categorizing them into 26 subgroups based on shared conserved motif compositions and gene structures. Collinearity analysis illustrated that segmental duplications predominately lead to the evolution of GpbHLHs, with most duplicated GpbHLH gene pairs undergoing purifying selection. Among the nine gypenoside-related GpbHLH genes, two GpbHLHs (GpbHLH15 and GpbHLH58) were selected for further investigation based on co-expression analysis and functional prediction. The expression of these two selected GpbHLHs was dramatically induced by methyl jasmonate, and their nuclear localization was confirmed. Furthermore, yeast one-hybrid and dual-luciferase assays demonstrated that GpbHLH15 and GpbHLH58 could bind to the promoters of the gypenoside biosynthesis pathway genes, such as GpFPS1, GpSS1, and GpOSC1, and activate their promoter activity to varying degrees. Conclusions: In conclusion, our findings provide a detailed analysis of the bHLH family and valuable insights into the potential use of GpbHLHs to enhance the accumulation of gypenosides in G. pentaphyllum. [ABSTRACT FROM AUTHOR] more...

Introduction: Gypenoside is a natural extract of Gynostemma pentaphyllum (Thunb.) Makino, a plant in the Cucurbitaceae family. It has been reported to have antitumor effects on the proliferation, migration and apoptosis of various types of cancer cells. However, the use of gypenoside in the treatment of gastric cancer has not been studied. In the present study, we explored the therapeutic effect of gypenoside on gastric cancer and the potential molecular mechanism. Methods and Results: Our results showed that gypenoside induced apoptosis in HGC-27 and SGC-7901 cells in a time-dependent and dose-dependent manner. Network pharmacology analyses predicted that gypenoside exerts its therapeutic effects through the PI3K/AKT/mTOR signaling pathway. Furthermore, molecular docking and western blot experiments confirmed that gypenoside induced the apoptosis of gastric cancer cells through the PI3K/AKT/mTOR signaling pathway. In addition, network pharmacological analysis revealed that the common targets of gypenoside in gastric cancer were enriched in the immune effector process, PD-L1 expression, the PD-1 checkpoint pathway, and the Jak-STAT signaling pathway. Furthermore, molecular docking and western blot assays demonstrated that gypenoside could bind to STAT3 and reduce its phosphorylation. Thus, the transcription of PD-L1 was inhibited in gastric cancer cells. Moreover, coculture experiments of gastric cancer cells with gypenoside and primary mouse CD8+ T cells showed that gastric cancer cells treated with gypenoside could enhance the antitumor ability of T cells. Animal experiments confirmed the antitumor effect of gypenoside, and the expression of PD-L1 was significantly downregulated in the gypenoside-treated group. Conclusion: Gypenoside induced the apoptosis of gastric cancer cells by inhibiting the PI3K/AKT/mTOR pathway and simultaneously inhibited the expression of PD-L1 in gastric cancer cells, thus enhancing the antitumor immunity of T cells. This study provides a theoretical basis for applying gypenoside as a new therapeutic agent to enhance the efficacy of immunotherapy in gastric cancer. [ABSTRACT FROM AUTHOR] more...

Background: In traditional Asian medicine, Gynostemma pentaphyllum Makino leaf extract (Gp) is used to treat aging, metabolic syndrome, diabetes, and neurodegenerative diseases. Hair loss and hair‐graying are common phenomena that haunt everyone. However, whether Gp activities on inhibition of hair loss and getting gray have been rarely studied. Aim: Study the Gp activity and mechanism by in vivo and in vitro experiments to explore its application on hair health. Methods: In the present study, we determined the effects of Gp on the expression of hair growth‐related genes and proliferation of human dermal papilla cells (hDPCs). Furthermore, Gp was topically applied to the hair‐shaved skin of male C57BL/6 mice, and the histological profile of the skin was studied. Because emotional stress may lead to melanocyte disappearance, norepinephrine‐exposed mice B16 melanocytes were treated with Gp to elucidate the anti‐hair graying capacity of Gp in response to this stress type. Results: Gp stimulated the proliferation of hDPCs and the Wnt signaling pathways associated with hair growth; furthermore, the expression of the hair loss‐related gene transforming growth factor‐β1 was suppressed. Gp treatment significantly increased the size of hair follicles in the treated mice and stimulated them. Moreover, Gp not only increased melanin synthesis but also tyrosinase activity in B16 cells. Quantitative real‐time polymerase chain reaction revealed that Gp increased melanin synthesis by increasing the expression of tyrosine‐related protein‐1, tyrosine‐related protein‐2, tyrosinase, and microphthalmia‐associated transcription factor. Conclusion: Our study provides preclinical evidence regarding the potential of Gp as a promising hair growth and anti‐graying agent. [ABSTRACT FROM AUTHOR] more...

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

Gynostemma pentaphyllum belongs to the family Cucurbitaceae which is native to China where it is also termed an immortal herb. It is an emerging herb gaining fame for its rich phytochemistry. It is loaded with superior phytochemicals with immense therapeutic potential. The key phytochemicals include saponins and sterols. Saponins are a wide class of bioactive found in Gynostemma pentaphyllum and 100 different saponins have been reported to date by different researchers in this herb. Several sterols have been demonstrated in this plant including ergostanol, sitosterol and stigmasterol. All these bioactive substances possess superior therapeutic and pharmacological properties that have been investigated in different studies as presented in this comprehensive review. Taxonomic classification, botanical description, and geographical distribution are briefly covered in the first section of this review. In contrast, the phytochemistry, therapeutic properties, and pharmacological features of Gynostemma pentaphyllum are thoroughly explained in the second section. more...

Protein tyrosine phosphatase 1B (PTP1B) is a key factor and regulator of glucose, lipid metabolism throughout the body, and a promising target for treatment of type 2 diabetes mellitus (T2DM). Gynostemma pentaphyllum is a famous oriental traditional medicinal herbal plant and functional food, which has shown many beneficial effects on glucose and lipid metabolism. The aim of the present study is to assess the inhibitory activity of five new and four known dammarane triterpenoids isolated from the hydrolysate product of total G. pentaphyllum saponins. The bioassay data showed that all the compounds exhibited significant inhibitory activity against PTP1B. The structure-activity relationship showed that the strength of PTP1B inhibitory activity was mainly related to the electron-donating group on its side chain. Molecular docking analysis suggested that its mechanism may be due to the formation of competitive hydrogen bonding between the electron-donating moiety and the Asp48 amino acid residues on the PTP1B protein. [ABSTRACT FROM AUTHOR] more...

Gynostemma pentaphyllum an important medicinal herb, can absorb high amounts of cadmium (Cd) which can lead to excessive Cd contamination during the production of medicines and tea. Hence, it is crucial to investigate the response mechanism of G. pentaphyllum under Cd stress to develop varieties with low Cd accumulation and high tolerance. Physiological response analysis, transcriptomics and metabolomics were performed on G. pentaphyllum seedlings exposed to Cd stress. Herein, G. pentaphyllum seedlings could significantly enhance antioxidant enzyme activities (POD, CAT and APX), proline and polysaccharide content subject to Cd stress. Transcriptomics analysis identified the secondary metabolites, carbohydrate metabolism, amino acid metabolism, lipid metabolism, and signal transduction pathways associated with Cd stress, which mainly involved the XTH, EXP and GST genes. Metabolomics analysis identified 126 differentially expressed metabolites, including citric acid, flavonoid and amino acids metabolites, which were accumulated under Cd stress. Multi-omics integrative analysis unraveled that the phenylpropanoid biosynthesis, starch, and sucrose metabolism, alphalinolenic acid metabolism, and ABC transporter were significantly enriched at the gene and metabolic levels in response to Cd stress in G. pentaphyllum. In conclusion, the genetic regulatory network sheds light on Cd response mechanisms in G. pentaphyllum. [ABSTRACT FROM AUTHOR] more...

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

Aim: We aimed to systematically evaluate the prevalence and clinical characteristics of adverse events associated with the adaptogens and antidepressant drug interactions in a retrospective chart review. Methodology: A total of 1,816 reports of adverse events were evaluated. Cases were included in the analysis if the pharmacoepidemiological analysis showed the presence of a high probability of a causal relationship between an adaptogen and antidepressant interaction and the occurrence of adverse events. The following data were extracted from the reports: age, sex, antidepressant, plant products containing adaptogens, other concomitant medications, and clinical consequences of the interactions and their possible mechanisms. Results: Adaptogens were involved in 9% of adverse events associated with the concomitant use of antidepressants and other preparations. We identified 30 reports in which side effects presented a causal relationship with the use of antidepressants and adaptogens. Here, we present the list of adaptogens with the corresponding antidepressants and the side effects caused by their interactions: Withania somnifera: reboxetine (testicle pain and ejaculatory dysfunctions), sertraline (severe diarrhea), escitalopram (myalgia, epigastric pain, nausea, vomiting, restless legs syndrome, and severe cough), and paroxetine (generalized myalgia, ophthalmalgia, and ocular hypertension); Eleutherococcus senticosus: duloxetine (upper gastrointestinal bleeding), paroxetine (epistaxis), sertraline (vaginal hemorrhage), and agomelatine (irritability, agitation, headache, and dizziness); Schisandra chinensis: bupropion (arthralgia and thrombocytopenia), amitriptyline (delirium), and fluoxetine (dysuria); Tribulus terrestris: citalopram (generalized pruritus), escitalopram (galactorrhea), and trazodone (psoriasis relapse); Coptis chinensis: mianserin (arrhythmias), mirtazapine (edema of lower limbs and myalgia), and fluoxetine (gynecomastia); Cimicifuga racemosa: mianserin (restless legs syndrome), paroxetine (gynecomastia and mastalgia), and venlafaxine (myocardial infarction); Gynostemma pentaphyllum: duloxetine (back pain); Cordyceps sinensis: sertraline (upper gastrointestinal bleeding); Lepidium meyenii: mianserin (restless legs syndrome); and Scutellaria baicalensis: bupropion (seizures). Conclusion: Clinicians should monitor the adverse events associated with the concomitant use of adaptogens and antidepressant drugs in patients with mental disorders. Aggregation of side effects and pharmacokinetic interactions (inhibition of CYP and p-glycoprotein) between those medicines may result in clinically significant adverse events. [ABSTRACT FROM AUTHOR] more...

Glucose metabolic disorders (GMD) can promote insulin resistance (IR) and diabetes, and damage liver and kidney. Gynostemma pentaphyllum is commonly used in the clinical treatment of diabetes, but the research on its main active constituents and GMD has not been reported yet. This study explores the therapeutic potential of gypenosides of heat-processed Gynostemma pentaphyllum (HGyp) on high-fat diet-induced GMD in mice. HGyp was administered at different doses for 12 weeks. The investigation encompassed an array of parameters, including body weight, blood lipids, blood glucose, and liver tissue components. Metabolomic and network analyses were conducted to uncover potential targets and pathways associated with HGyp treatment. The results revealed that HGyp alleviated GMD by reducing body weight, blood glucose, and improving blood lipids levels, while increasing liver glycogen and antioxidant enzyme levels. Additionally, HGyp exhibited protective effects on liver and kidney health by reducing tissue damage. Fourteen blood components were detected by LC-MS. Metabolomic and network analyses indicated the potential engagement of the AGE-RAGE signaling pathway in the therapeutic effects of HGyp.Furthermore, Western blot and ELISA assays confirmed that HGyp upregulated GLO1 and GLUT4 while down-regulating AGEs and RAGE expression in liver tissue. In light of these findings, HGyp demonstrates promise as a potential therapeutic candidate for combating GMD, warranting further exploration in the development of therapeutic strategies or functional products. [ABSTRACT FROM AUTHOR] more...

Background: Gynostemma pentaphyllum (GP), also called Giao-co-lam, is a traditional Vietnamese herb, also known as the "Herb of Immortality", that grows throughout Asian countries and is used for the treatment of hematuria, edema in the pharynx and neck, tumors, and trauma. Methods: In this study, we investigated the effects of culture conditions on cell growth and total gypenoside accumulation in the GP suspension cells. Cells were cultured on Murashige and Skoog (MS) medium supplemented with 2.0 mg/L KIN and 0.5 mg/L IBA, and different inoculum sizes (2-4 g) for 10-24 days. Results: The results showed that the optimum inoculum size and shaking speed were 3 g of callus and 120 rpm, respectively. The highest cell biomass reached was 5.833 g of fresh weight, corresponding to 0.136 g of dry weight after 20 days of culture. The total gypenoside and Rb1 accumulation was the highest after 18 days of culture, with 46.498 mg/g and 0.038 mg/g dry weight, respectively. In addition, the crude extract from GP cell suspension cultures remarkably improved pathological changes in mouse testicular tissue after scrotal heat exposure. Blood testosterone levels were significantly increased in heat-exposed mice treated with the GP cell suspension culture extract. Conclusion: Taken together, these results suggest that GP bio-mass production by cell suspension cultures leads to the accumulation of gypenosides in large amounts, and provides the potential for the recovery of spermatogenesis following heat stress. [ABSTRACT FROM AUTHOR] more...

Gynostemma pentaphyllum (Thunb.) Makino represents the popular health food and supplemental product with broad pharmacological activities. The highly polar glycosides, including flavonoids and saponins, are major effective active components that contain diverse sugar positions and quantities, which result in diverse chemical polarities, making it challenging to separate and isolate these components. The present work described the rapid and efficient linear gradient counter‐current chromatography to preparatively separate glycosides from aboveground parts of G. pentaphyllum. Besides, the ethyl acetate and n‐butanol binary mobile phases were achieved through adjusting associated proportions. Six glycosides, including quercetin‐3‐O‐neohesperidoside (1), kaempferol‐3‐O‐robinobioside (2), kaempferol‐3‐O‐neohesperidoside (3), gypenoside LVI (4), ginsenoside Rb3 (5), and gypenoside XLVI (6), were isolated at the purities greater than 98%. Moreover, electrospray ionization mass spectrometry and nuclear magnetic resonance tandem mass spectrometry were conducted for structural identification. According to our findings, the established linear gradient counter‐current chromatography was an efficient approach to separate the highly polar glycosides from aboveground parts of G. pentaphyllum. Our proposed strategy can be used to separate active compounds from other complex natural products. [ABSTRACT FROM AUTHOR] more...

Alzheimer's disease (AD) is a neurodegenerative disease with clinical hallmarks of progressive cognitive impairment and memory loss. Gynostemma pentaphyllum ameliorates cognitive impairment, but the mechanisms remain obscure. Here, we determine the effect of triterpene saponin NPLC0393 from G. pentaphyllum on AD‐like pathology in 3×Tg‐AD mice and elucidate the underlying mechanisms. NPLC0393 was administered daily in vivo by intraperitoneal injection for 3 months and its amelioration on the cognitive impairment in 3×Tg‐AD mice was assessed by new object recognition (NOR), Y‐maze, Morris water maze (MWM), and elevated plus‐maze (EPM) tests. The mechanisms were investigated by RT‐PCR, western blot, and immunohistochemistry techniques, while verified by the 3×Tg‐AD mice with protein phosphatase magnesium‐dependent 1A (PPM1A) knockdown (KD) through brain‐specific injection of adeno‐associated virus (AAV)‐ePHP‐KD‐PPM1A. NPLC0393 ameliorated AD‐like pathology targeting PPM1A. It repressed microglial NLRP3 inflammasome activation by reducing NLRP3 transcription during priming and promoting PPM1A binding to NLRP3 to disrupt NLRP3 assembly with apoptosis‐associated speck‐like protein containing a CARD and pro‐caspase‐1. Moreover, NPLC0393 suppressed tauopathy by inhibiting tau hyperphosphorylation through PPM1A/NLRP3/tau axis and promoting microglial phagocytosis of tau oligomers through PPM1A/nuclear factor‐κB/CX3CR1 pathway. PPM1A mediates microglia/neurons crosstalk in AD pathology, whose activation by NPLC0393 represents a promising therapeutic strategy for AD. [ABSTRACT FROM AUTHOR] more...

Gynostemma pentaphylla, one of the traditional Chinese medicinal materials, which has gradually become a research hotspot due to its rich pharmacological activities such as hypolipidemic properties, anti-inflammatory, anti-cancer and etc. The main active ingredients of Gynostemma pentaphyllum are saponins (gypenoside), flavonoids and polysaccharides. The pharmacologically active dose depends on the content of the active ingredient, so it is necessary to establish a reliable quality evaluation standard for Gynostemma pentaphyllum. However, the existing Gynostemma pentaphyllum quality control methods are not perfect, Ginsenoside Rb1 was regarded as a signature ingredient of Gynostemma pentaphylla in local standards. Surprisingly, the high-performance liquid chromatogram results displayed that the content of Ginsenoside Rb1 was not suitable as a quality marker. Therefore, a triple quadrupole time-of-flight tandem mass spectrometer method was developed to explore other potential quality markers in Gynostemma pentaphylla. As a result, a total of 24 compounds was identified tentatively. While another stable and reliable component Gypenoside XLVI was found and the content was carried out. It was expected to replace Ginsenoside Rb1 to establish a more reliable and precise quality standard of Gynostemma pentaphylla. [ABSTRACT FROM AUTHOR] more...

Ginsenoside Rg3, Rk1, and Rg5, rare ginsenosides from Panax ginseng, have many pharmacological effects, which have attracted extensive attention. They can be obtained through the heat treatment of Gynostemma pentaphyllum. In this study, scanning electron microscopy (SEM) and thermal gravity-differential thermal gravity (TG-DTG) were employed to investigate this process and the content change in ginsenosides was analyzed using liquid chromatography-mass spectrometry (LC-MS). SEM and TG-DTG were used to compare the changes in the ginsenosides before and after treatment. In SEM, the presence of hydrogen bond rearrangement was indicated by the observed deformation of vascular bundles and ducts. The before-and-after changes in the peak patterns and peaks values in TG-DTG indicated that the content of different kinds of compounds produced changes, which all revealed that the formation of new saponins before and after the heat treatment was due to the breakage or rearrangement of chemical bonds. Additionally, the deformation of vascular bundles and vessels indicated the presence of hydrogen bond rearrangement. The glycosidic bond at the 20 positions could be cleaved by ginsenoside Rb3 to form ginsenoside Rd, which, in turn, gave rise to ginsenoside Rg3(S) and Rg3(R). They were further dehydrated to form ginsenoside Rk1 and Rg5. This transformation process occurs in a weak acidic environment provided by G. pentaphyllum itself, without the involvement of endogenous enzymes. In addition, the LC-MS analysis results showed that the content of ginsenoside Rb3 decreased from 2.25 mg/g to 1.80 mg/g, while the contents of ginsenoside Rk1 and Rg5 increased from 0.08 and 0.01 mg/g to 3.36 and 3.35 mg/g, respectively. Ginsenoside Rg3(S) and Rg3(R) were almost not detected in G. pentaphyllum, and the contents of them increased to 0.035 and 0.23 mg/g after heat treatment. Therefore, the rare ginsenosides Rg3(S), Rg3(R), Rk1, and Rg5 can be obtained from G. pentaphyllum via heat treatment. [ABSTRACT FROM AUTHOR] more...