POSTHARVEST BIOLOGY AND TECHNOLOGY
·
2024
·
IF 6.4
Yujie Liu,Xinyv Li,Chu Gong,Yonghong Cao,Jun Wang,Min Han,Jun-Li Yang
Anthracnose is a plant disease caused by Colletotrichum spp ., known for its widespread infectivity and extreme destructiveness. Colletotrichum gloeosporioides is a representative pathogen of anthracnose in China. Gypenosides GP4 - GP7 , derived from Gynostemma pentaphyllum (Thunb.) Makino, could significantly inhibit the growth of C. gloeosporioides mycelial, with EC 50 values of 96.98, 27.5, 38.48, and 61.59 mg L −1 . The inhibitory effect of these compounds surpassed the commonly used chemical pesticide chlorothalonant and plant-derived pesticide matrine. Among them, the most active compound GP5 also showed a significant inhibitory effect on spore germination and bud tube elongation of C. gloeosporioides . In addition, GP5 could effectively suppress the spread of anthracnose spots in postharvest fruit. Transmission electron microscopy and fluorescence microscopy demonstrated that GP5 primarily exerted its antifungal function by activating cellular autophagy. Additionally, proteomics analysis revealed that GP5 had an antifungal effect against C. gloeosporioides by enhancing cellular autophagy through upregulation of the expression of the autophagy-related protein Atg8. This study presents a novel approach for the control and management of anthracnose in C. gloeosporioides . Consequently, GP5 has the potential to be developed as a plant-derived fungicide for the biological control of anthracnose.
研究领域:
植物病理学
·
分子生物学
·
植物化学
·
农学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF CHROMATOGRAPHIC SCIENCE
·
2018
·Vol. 57
·期 3
·265-271
·
IF 1.037
Pan Conglei,Lü Haitao
An efficient method for the preparative separation of quercetin, ombuin and kaempferide from Gynostemma pentaphyllum by high-speed countercurrent chromatography (HSCCC) was successfully developed for the first time. The extraction conditions were optimized by an orthogonal array design L9 (34), while quercetin, ombuin and kaempferide were efficiently released from rutin, ombuoside and kaempferide glucoside by hydrochloric acid hydrolysis, respectively. Quercetin was purified by HSCCC with two-phase solvent system composed of n-hexane–ethyl acetate–methanol–water (4:5:4:5, v/v) in a single run. From 164.7 mg of the crude extract, 90.5 mg quercetin at 99.23% purity was obtained. Ombuin and kaempferide were purified by HSCCC with two-phase solvent system composed of n-hexane–ethyl acetate–methanol–water (8:2:5:5, v/v) in a single run. From 50 mg of the crude extract, 0.4 mg of ombuin at 95.46% purity and 1.1 mg of kaempferide at 98.78% purity were obtained, respectively. Their structures were identified by ultraviolet, Fourier transform infrared, electrospray ionization mass spectrometry (ESI-MS), 1H nuclear magnetic resonance (NMR) and 13C NMR spectra. The purified quercetin had the strongest 1,1-diphenyl-2-picrylhydrazyl and hydroxyl free radical scavenging activities.
研究领域:
植物化学
·
药物化学
·
分离科学
✓ 已验证
DOI
高影响因子
JOURNAL OF FOOD SCIENCE
·
2020
·Vol. 85
·期 5
·1586-1595
·
IF 2.479
Yonglu Li,Yong Jiang,Qiang Chu,Xiaodong Zheng
Radix Tetrastigma (RT) is a medicinal plant and functional food in China, distributed in various places in the south of China. Radix Tetrastigma extract (RTE) from different origins were collected and analyzed for their anti-inflammatory effects. Different RTEs showed different abilities to suppress shape deformation, decrease the nitric oxide (NO) production, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression in RAW 264.7 cells. Subsequently, their bioactive components were compared, and results showed RTEs are rich in flavonoid (85.25-436.70 mg RE/g DW), polysaccharides (100.45-349.26 mg glucose/g DW), phenolic (12.92-225.40 mg GAE/g DW) and protein contents (4.429-7.719 mg/g DW). Principal component analysis (PCA) and correlation studies indicated that anti-inflammatory capacity could be more associated with total flavonoid contents. High-performance liquid chromatography (HPLC) and Ultraperformance liquid chromatography-time-of flight mass spectrometry (UPLC-TOF/MS) analysis were conducted, and results showed that rutin, isoquercitrin, kaempferol-3-O-rutinoside and astragalin were main flavonoid compounds, among them astragalin exhibited a prior protective effect, suggesting it might be responsible for RTE's excellent anti-inflammatory capacity.
研究领域:
药理学
·
免疫学
·
植物化学
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Mingwang Ren,Guoqing Sun,Xiaoyu Ding,Xiaolin Yu,Li He,Shiji Xiao,Minjian Dong,Jianwen Yang,Kan Ding,Chengxin Sun
Polysaccharides are among the key bioactive components of Gynostemma pentaphyllum (Thunb.) Makino . In this study, a novel polysaccharide fraction, GPPA1-1, was isolated from G. pentaphyllum and purified using DEAE-Sepharose Fast Flow, Sephadex G-75, and Sepharose CL-6B column chromatography. GPPA1-1 was determined to have a molecular weight of 3.7 × 10 4 Da and was composed of mannose (Man), glucuronic acid (GlcA), rhamnose (Rha), glucose (Glc), galactose (Gal), and arabinose (Ara) in a molar ratio of 3.88:3.97:21.77:7.02:45.65:17.71. Comprehensive structural characterization was conducted using Congo red staining, FT-IR spectroscopy, Methylation analysis, and NMR analysis. The backbone of GPPA1-1 was identified as comprising →4)-α-Gal p- (1→, →4)-α-Gal p- (3,1→, →2)-α-Rha p- (4,1→, and →2)-α-Rha p- (1→, with branch chains containing α-Ara f -(1→, →5)-α-Ara f -(1→, →3)-α-Galp-(1→, and -α-GlcA-(1→. Biological assays demonstrated that GPPA1-1 effectively alleviates insulin resistance by inhibiting Galectin-3. This activity was confirmed through various experiments, including Galectin-3-mediated hemagglutination, Western blotting, CETSA, and glucose uptake assays. These findings highlight the potential of GPPA1-1 as a promising therapeutic agent for managing insulin resistance.
研究领域:
植物化学
·
代谢生物学
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PHARMACOLOGICAL RESEARCH
·
2021
·
IF 7.658
Qiao Zhang,Xiaomin Guo,Cao Xie,Zhonglian Cao,Xin Wang,Li Liu,Ping Yang
Trimethylamine-N-oxide (TMAO) has emerged as a promising new therapeutic target for the treatment of central nervous system diseases , atherosclerosis and other diseases. However, its origin in the brain is unclear. Gynostemma pentaphyllum (Thunb.) Makino can reduce the increase of TMAO level caused by a high fat diet. But its effective chemical composition and specific mechanism have not been reported. The study confirmed that TMA was more easily to penetrate blood brain barrier than TMAO, the MAO enzyme was partly involved in the transformation of the TMA in brain, which further supplemented the choline-TMA-TMAO pathway. Based on the above metabolic pathway, using multi-omics approaches, such as microbiodiversity, metagenomics and lipidomics, it was demonstrated that the reduction of plasma TMAO levels by gypenosides did not act on FMO3 and MAO in the pathway, but remodeled the microbiota and affected the trimethylamine lyase needed in the conversion of choline to TMA in intestinal flora . At the same time, gypenosides interfered with enzymes associated with TCA and lipid metabolism, thus affecting TMAO and lipid metabolism. Considering the bidirectional transformation of phosphatidycholine and choline, lipid metabolism and TMAO metabolism could affected each other to some extent. In conclusion, our study revealed the intrinsic correlation between long-term application of gypenosides to lipid reduction and nervous system protection, and explained why gypenosides were used to treat brain diseases, even though they had a poor ability to enter the brain. Besides, it provided a theoretical basis for clinical application of gypenosides and the development of new drugs.
研究领域:
药理学
·
代谢学
·
神经科学
·
微生物学
·
生物化学
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2023
·Vol. 24
·期 2
·1454
·
IF 5.6
Juan Chen,Lin Qin,Xingdong Wu,Daopeng Tan,Yanliu Lu,Yimei Du,Di Wu,Yuqi He
Gypensapogenin C (GPC) is one of the important aglycones ofGynostemma pentaphyllum(GP), which is structurally glucuronidated and is highly likely to bind to UGT enzymes in vivo. Due to the important role of glucuronidation in the metabolism of GPC, the UDP-glucuronosyltransferase metabolic pathway of GPC in human and other species’ liver microsomes is investigated in this study. In the present study, metabolites were detected using high-performance liquid chromatography–tandem mass spectrometry (LC–MS/MS). The results show that GPC could generate a metabolite through glucuronidation in the human liver microsomes (HLMs). Additionally, chemical inhibitors combined with recombinant human UGT enzymes clarified that UGT1A4 is the primary metabolic enzyme for GPC glucuronidation in HLMs according to the kinetic analysis of the enzyme. Metabolic differential analysis in seven other species indicated that rats exhibited the most similar metabolic rate to that of humans. In conclusion, UGT1A4 is a major enzyme responsible for the glucuronidation of GPC in HLMs, and rats may be an appropriate animal model to evaluate the GPC metabolism.Keywords:gypensapogenin C;glucuronidation;human liver microsomes;UGT1A4;species differences
研究领域:
药理学
·
代谢研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Foods
·
2024
·
IF 4.7
Yang Zhang,Lei Zeng,Kehui Ouyang,Wenjun Wang
In this study, a new component of Cyclocarya paliurus polysaccharides (CPP20) was precipitated by the gradient ethanol method, and the protective effect of CPP20 on hypercholesterolemia mice was investigated. In vitro, CPP20 had the ability to bind bile salts and inhibit cholesterol micelle solubility, and it could effectively clear free radicals (DPPH•, •OH, and ABTS+). In vivo, CPP20 effectively alleviated hypercholesterolemia and liver damage in mice. After CPP20 intervention, the activity of antioxidant enzymes (SOD, CAT, and GSH-Px) and the level of HDL-C in liver and serum were increased, and the activity of aminotransferase (ALT and AST) and the level of MDA, TC, TG, LDL-C, and TBA were decreased. Molecular experiments showed that CPP20 reduced cholesterol by regulating the mRNA expression of antioxidation-related genes (SOD, GSH-Px, and CAT) and genes related to the cholesterol metabolism (CYP7A1, CYP27A1, SREBP-2, HMGCR, and FXR) in liver. In addition, CPP20 alleviated intestinal microbiota disturbances in mice with hypercholesterolemia and increased levels of SCFAs. Therefore, CPP20 alleviates hypercholesterolemia by alleviating oxidative damage, maintaining cholesterol homeostasis, and regulating gut microbiota.
研究领域:
营养学
·
分子生物学
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2025
·
IF 3.1
Lili Liu,Yaping Huang,Qingqing Wang,Ziyuan Wang,Ke Pan,Jian Zhang,Ying Peng,Guangji Wang,Zhiqi Yin,Jianguo Sun
As a plant with a rich history of medicinal and dietary use, Gynostemma pentaphyllum (Thunb.) Makino is predominantly characterized by the gypenosides. Contemporary research has demonstrated that these saponins possess significant hypolipidemic and hypoglycemic effects. This study focused on developing an LC-MS/MS approach to elucidate the pharmacokinetic profiles of 13 gypenosides in rat models. The separation was accomplished using a ZORBAX Eclipse Plus C18 column (2.1 mm × 100 mm, 1.8 µm). Detection was facilitated by employing positive electrospray ionization (ESI) in multiple reaction monitoring (MRM) mode. The analytical method was fully validated, including selectivity, linear response, measurement precision, analytical accuracy, extraction efficiency, matrix interference, and sample stability. The lower limit of quantification (LLOQ) for all compounds was 10 ng/mL, with each exhibiting a favorable linear relationship (r ≥ 0.9960). The precision, as measured by the relative standard deviation (RSD) for intra-day and inter-day variability, did not exceed 8.41 %. The accuracy, expressed as the relative error (RE), varied from −4.42–8.42 %. The recovery rate of the extraction process was between 92.02 % and 114.77 %, and no notable matrix effects were detected. The stability of the compounds was confirmed under four distinct storage conditions. Pharmacokinetic results indicated that all analytes displayed rapid absorption, prolonged retention, and slow elimination in rats, and exhibited nonlinear pharmacokinetics at low, medium, and high dosage levels. This study has established a quantification method for 13 gypenosides and successfully applied it to their pharmacokinetic studies in rats, providing a foundation for their further development and utilization.
研究领域:
中药学
·
分析化学
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Cancer Research and Therapeutics
·
2024
·Vol. 20
·期 2
·684
·
IF 1.4
Lai Zongqiang,Bai Facheng,Pu Tao,Li Jun,Wu Lining,Zhou Zhou,Yang Nuo
Objectives: Gypenoside (Gyp) is easily degraded in the gastrointestinal tract, resulting in its low bioavailability. We aimed to develop a tumor-targeted Gyp nanodrug delivery system and to investigate its antitumor effect in vitro. Materials and Methods: We used Gyp as the therapeutic drug molecule, mesoporous silica (MSN) and liposome (Lipo) as the drug carrier and protective layers, and aptamer SYL3C as the targeting element to establish a tumor-targeted nanodrug delivery system (i.e., SYL3C-Lipo@Gyp-MSN). The characteristics of SYL3C-Lipo@Gyp-MSN were investigated, and its drug release performance, cell uptake, and antitumor activity in vitro were evaluated. Results: A tumor-targeted Gyp nanodrug delivery system was successfully prepared. The SYL3C-Lipo@Gyp-MSN was spherical or ellipsoidal; had good dispersion, which enabled it to specifically target and kill the liver tumor cell HepG2; and effectively protected the early leakage of Gyp. Conclusions: We have established a tumor-targeted nanodrug delivery system that can target and kill liver cancer cells and may provide a strategy for preparing new nanodrug-loaded preparations of traditional Chinese medicine.
研究领域:
药剂学
·
肿瘤学
·
纳米医学
✓ 已验证
DOI
PubMed
高影响因子
Phytochemistry Letters
·
2019
·
IF 1.338
Jun Wang,Cai-Hong Li,Mahdi Moridi Farimani,Jun-Li Yang
To search for potential candidate anti-AD agents, the gypenosideson the aerial parts of Gynostemma pentaphyllum were phytochemically investigated, yielding two undescribed ( 1 - 2 ) and five known ( 3 - 7 ) dammarane saponins. Their molecular structures were unambiguously elucidated via spectroscopic analyses (1D and 2D NMR, HR-ESI-MS, IR, and optical rotation) chemical transformations. All of the compounds possessed a 21- O - n -butyl-20,21-dihydroxy-21,23-epoxydammar-24-ene moiety in their structures. The short-term memory assay on a transgenic fly Alzheimer’s disease (AD) model revealed that all of the compounds displayed potential anti-AD activity. Of the compounds, 1 and 6 at 10 μM showed comparable short-term memory rescue ability to memantine, the positive control, at 100 μM. This study revealed the potent antagonistic effect of dammarane-type saponins 1 and 6 against Alzheimer’s disease.
研究领域:
植物化学
·
神经科学
·
药物开发
✓ 已验证
DOI
高影响因子
Antioxidants
·
2023
·Vol. 12
·期 8
·1505
·
IF 7
Xuechun Zhang,Shi Li,Zhibin Zhang,Kin Weng Kong,Zhenxing Wang,Xiahong He
To assess the effects of microbial fermentation onGynostemma pentaphyllumleaves (GPL), four probiotics were used to ferment GPL (FGPL) for 7 days. At different stages of fermentation, changes in the active components and biological activities of FGPL were determined. The findings suggest that short-term fermentation with probiotics can enhance both the content and bioactivity of active components in GPL. However, prolonged fermentation may lead to a decline in these aspects. Among them, the best effect was observed with SWFU D16 fermentation for 2 days. This significantly improved the total phenolic and total flavonoid content, antioxidant capacity, and inhibitory ability against α-glucosidase activity with an increase of 28%, 114.82%, 7.42%, and 31.8%, respectively. The high-performance liquid chromatography (HPLC) analysis results also supported this trend. Untargeted metabolomics analysis revealed metabolite changes between GPL and FGPL and the key metabolites associated with these functional activities. These key metabolites are mainly organic acids, flavonoids, carbohydrates, terpenoids, and other substances. KEGG analysis demonstrated that microbial metabolism in diverse environments and carbon metabolism were the most significantly enriched pathways. Among them, 3-(3-hydroxyphenyl) propanoic acid, d-glucose, gallic acid, gluconic acid, l-lactic acid, and l-malic acid were mostly involved in the microbial metabolism of diverse environmental pathways. In contrast, D-glucose, gluconic acid, and l-malic acid were mainly related to the carbon metabolism pathway. This study revealed the positive effect of probiotic fermentation on GPL and its potential metabolism mechanism, which could provide supporting data for further research.Keywords:Gynostemma pentaphyllumleaves;probiotic fermentation;antioxidant capacity;α-glucosidase inhibitory activity;metabolomics
研究领域:
药理学
·
生物化学
·
微生物学
·
代谢组学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Oncotarget
·
2018
·
IF 0
Wenxia Bai,Shudong Wang,Shanshan An,Mengjie Guo,Guangming Gong,Wenya Liu,Shaoxin Ma,Xin Li,Jihua Fu,Wenbing Yao
This study aimed to investigate the effect of single and combination therapy using chitosan (K), gynostemma (J), and motherwort (Y) on an experimental rat model of chronic renal failure (CRF) induced by adenine and the underlying mechanisms. CRF rats were treated with individual or combinational therapy with two or three of these agents. Biochemical indicators showed that the levels of blood urea nitrogen, creatinine and uric acid decreased and the levels of albumin and hemoglobin increased by single or combination therapy of these drugs. Drug treatment also decreased oxidative stress damage of renal tissues in CRF rats. Histopathological lesions were attenuated in each drug treatment group by various degrees. Additionally, drug treatment affected the expression of extracellular matrix (ECM) proteins including plasminogen activator inhibitor 1, collagen I, matrix metalloprotease-1, and tissue inhibitor of metalloproteinases 1. In particular, the combination therapy of K, J, and Y was superior to the respective monotherapy, which supported the prescription of KJY combination. We further studied the inhibitory effect of KJY on LPS-induced inflammation in RAW264.7 macrophages. The results showed that KJY inhibited LPS-induced secretion of inflammatory cytokines (Interferon-gamma, Interleukin-1 Beta, chemokine (C-X-C motif) ligand 10, cyclooxygenase-2 and Tumor necrosis factor-α in RAW264.7 macrophages. Combination therapy of KJY suppressed the protein expression of Cyclooxygenase-2 and inducible nitric oxide synthase in vivo and in vitro . Further study indicated that KJY inhibited STAT1 activation by down regulating p-STAT1 to exert anti-inflammatory effect and improve renal function in rats with chronic renal failure.
研究领域:
药理学
·
肾病学
·
免疫学
✓ 已验证
产品关联
DOI
PubMed