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Molecular Catalysis · 2024 · IF 3.9

Strong Lewis acid MOF material for efficient and clean diosgenin extraction from total saponins in D. zingiberensis C. H. Wright

XiaoNing Gao,YanXiao Zhang,Wei Fu,Hong Zhou,Lu Feng

Conventional hydrolysis of total saponins for the extraction of diosgenin, an essential ingredient in the production of steroid hormones, has caused significant ecological pollution, making efficient and clean extraction methods necessary. Here, UiO-66-NH 2 with defect sites containing Zr-coordinated hydroxide and water groups was synthesized using concentrated HCl as a crystal modulator, which was further treated with trimethylsilyl trifluoromethanesulfonate (Me 3 SiOTf) to afford UiO-66-NH 2 OTf using the oxygen affinity of the Me 3 Si group. The strong Lewis acid UiO-66-NH 2 OTf was used to extract diosgenin from the total saponin, and the extraction temperature, extraction time and amount of addition were optimized using single-factor experiments and the response surface method. In addition, high-resolution mass spectrometry has been used to analyze the resulting compounds, thus suggesting an alcoholysis pathway and an alcoholysis mechanism for the total saponins.

研究领域: 药用植物化学 · 环境科学 · 药物化学
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BRAIN RESEARCH BULLETIN · 2025 · IF 3.7

Jujuboside A improves insomnia by maintaining mitochondrial homeostasis in prefrontal neurons

Zhen Zhang,Xinyue Che,Tingyu Feng,Juntao Zou,Guangpei Chen,Wenping Guo,Chunmei Ma,Haozhe Yuan,Jingying Chen,Xiaowu Xu

Objective Jujuboside A (JB-A) is the major component of Semen Ziziphi Spinosae (SZS), a traditional Chinese herbal medicine used to treat sleep with clinical efficacy. This is the first study to investigate the effects of JB-A on mitochondrial structure and function in the prefrontal cortex of the insomnia model mice. Methods Young adult C57BL/6 mice were induced to develop insomnia by P-chlorophenylalanine. After 14 d of JB-A treatment via gavage, anxiety level was assessed using the open field and elevated plus maze tests. Next, the mitochondrial metabolic activity and morphological changes in the prefrontal cortex of each group of mice, as well as their effects on mitochondrial membrane potential, oxidative phosphorylation levels, and cytochrome c (Cyt c) content in neurons were measured. Results In our mouse model, JB-A ameliorated anxiety-like behaviors; up-regulated the membrane potential (Δψm) and had a therapeutic effect on the metabolic activity and damaged microscopic structure of mitochondria in the prefrontal cortex; effectively improved mitochondrial function by increasing the expression of Cyt c oxidase I and IV proteins, ATPase activity, and ATP content; and reduced the accumulation of Cyt c in the neuronal cytoplasm while inhibiting mitochondrial permeability transition pore (mPTP) opening. Conclusions JB-A can improve insomnia by restoring mitochondrial intracellular oxidative phosphorylation, regulating mPTP to maintain mitochondrial homeostasis, and alleviating structural damage, providing a scientific basis for finding new targets for insomnia treatment.

CAS / MDL: 55466-04-1
研究领域: 神经科学 · 药理学 · 传统中医研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES · 2025 · IF 2.8

Total ginsenosides from wild ginseng improve immune regulation in a rat model of spleen qi deficiency by modulating fecal-bacteria-associated short-chain fatty acids and intestinal barrier integrity

Ruobing Bai,Liting Ma,Fangtong Li,Lijia Pan,Yuwen Bao,Xinze Li,Shen Wang,Hao Yue,Fei Zheng

For thousands of years, traditional Chinese medicine (TCM) has made extensive use of wild ginseng. It is thought to provide vital energy effects and to boost immunity. This study aimed to clarify the processes by which short-chain fatty acids (SCFAs) metabolites and the intestinal barrier are used by total ginsenosides wild ginseng (TWG) to modulate immunity. In this study, we analyzed and identified ginsenosides in the colon using UPLC-Q-TOF-MS E methods. In the meantime, a rat model of spleen qi deficiency (SQD) was created using reserpine, and the effects of TWG on intestinal barrier function and short-chain fatty acids in the feces of SQD-affected rats were examined. 28 ginsenosides were found in the colon during this experiment, and the main components were measured. TWG considerably increased fecal concentrations of acetic, propionic and 6 others, according to SCFAs analysis. According to serum immunological markers, TWG reduced IL-17 and IL-1β levels, increased IL-10, IL-22, and TGF-β concentrations, balanced Th17/Treg ratios, and reduced toxicants such DAO and LPS in rats with SQD. TWG improved barrier function, reduced permeability, increased tight junction protein expression, and lessened intestinal injury. A favorable correlation between intestinal barrier proteins and fatty acids was shown by correlation studies. The gut barrier and SCFAs perspectives helped to clarify the mechanism by which TWG controls immune activity. This study offers a fresh theoretical framework for TWG's future advancement and application.

CAS / MDL: 64-18-6
研究领域: 中医药学 · 免疫学 · 胃肠病学 · 微生物组研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Frontiers in Cellular and Infection Microbiology · 2021 · IF 5.293

Pulsatilla chinensis Saponins Ameliorate Inflammation and DSS-Induced Ulcerative Colitis in Rats by Regulating the Composition and Diversity of Intestinal Flora

Liu Yali,Zhou Mingyue,Yang Ming,Jin Chen,Song Yonggui,Chen Jingbin,Gao Meng,Ai Zhifu,Su Dan

Pulsatilla chinensis (Bunge) Regel is a commonly used Chinese medicine for clearing away heat and detoxification, cooling blood, stopping dysentery, and anti-inflammatory effects. Pulsatilla chinensis saponins (PRS) have been identified to be responsible for producing these pharmacological activities. Studies have shown that Pulsatilla decoction has a good therapeutic effect on ulcerative colitis (UC), however, the therapeutic effect of PRS on UC has not been reported. Therefore, the purpose of this study was to investigate the possible anti-UC activity of PRS using a dextran sulfate sodium (DSS)-induced rat model, and further study the mechanism of PRS in the treatment of UC. The fecal and colon samples were collected from rats to monitor the changes in the composition and diversity of the intestinal flora, and pathological colon sections were also made to examine the mesenteric hemorheological characteristics. The results showed that PRS significantly reduced the mesenteric blood flow in UC rats and significantly alleviated the inflammatory response, which indicates that saponins are involved in the anti-UC effects of PRS. At the same time, it is also suggested that the regulation of intestinal flora by Pulsatilla chinensis saponins is an important pathway for its anti-UC activity, which may be ascribed to the increase in beneficial bacteria like norank_F_Muribaculaceae and norank_F_norank_O_Clostridia_UCG-014, and decrease in the harmful Bacteroides.

CAS / MDL: 30525-89-4 302-17-0
研究领域: 药理学 · 微生物学 · 胃肠病学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Food Bioscience · 2025 · IF 5.9

Total saponins from Siraitiae Fructus alleviate lung and intestinal injuries in rats with acute lung injury and mice infected with the influenza virus by regulating cytokines and enhancing the mucosal barrier.

Zongjin Pu,Yuhang Ma,Xiaonan Chen,Yixin Liu,Zhen Fang,Ying Peng,Xiaobo Li

Siraitiae Fructus (SF), the dried fruit of Siraitia grosuenorii (Swingle) C. Jeffreyex A. M. Lu et Z. Y. Zhan g , a traditional medicinal and edible herb, is known for its properties in dissipating heat, moistening the lungs and intestines, and promoting defecation, which contains saponins, flavonoids, and polysaccharides. However, the effective substances of SF have not been fully identified. This study systematically evaluated therapeutic efficacy of aqueous extract of Siraitiae Fructus (SFE) and its three fractions: Siraitiae Fructus total saponins (SFTS), polysaccharides (SFP), low-polarity saponins (SFLS). In lipopolysaccharide (LPS)-induced acute lung injury (ALI) rats, both SFE and SFTS demonstrated significant protective effects against pulmonary and colonic tissue damage. SFTS is more advantageous in regulating IL-1β and IL-17A in serum, W/D and TNF-α in lung tissues, and IL-1β, IL-17A in colon tissues, compared with SFLS and SFP. Subsequent validation in influenza A virus (IAV)-infected mice confirmed SFTS's ability to improve survival rates while alleviating viral pneumonia and enterocolitis. The quantitative analysis revealed that Mogroside V (399.728 mg/g) and 11-O-Mogroside V (202.660 mg/g) constituted 60.23% of SFTS. In summary, Both SFE and SFTS could alleviate the lung and colon injury induced by LPS and IAV by restoring the mucosal barrier, reducing the immune response, and decreasing the expression of inflammatory cytokines in the systemic circulation, thereby exerting "lung-gut co-treatment" effect. This study provides a foundation for the further investigation on the effective substances of SF, and also supports the "Lung-gut axis" theory.

CAS / MDL: 56570-89-9 91510-62-2
研究领域: 药理学 · 免疫学 · 中医药学
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Drug Design Development and Therapy · 2025 · IF 5.1

Ginsenoside Reshapes Intestinal Microecology to Alleviate Microgravity Stress

Yanli Wang,Tian Chen,Zhe Shi,Lijinchuan Dong,Mengting Li,Bo Peng,Qi Li,Ruile Pan,Shuiming Xiao,Qing Yang,Ning Jiang,Xinmin Liu,Qin Hu,Ying Chen

Background During medium- to long-duration spaceflights, real-time microgravity can increase the health risks of astronauts. In particular, the disruption of intestinal homeostasis is closely related to other health problems, and it is necessary to monitor related treatment strategies. Ginseng is a well-known Chinese herbal medicine often used to maintain health. Ginseng total saponins (GTSs), which are the bioactive components of ginseng, have been reported to regulate immune homeostasis, anti-inflammation, and anti-oxidation. This study focused on the regulation of GTSs in intestinal homeostasis imbalance caused by microgravity.Methods A hindlimb suspension (HLS) rat model was established to evaluate the intestinal protective effects of GTSs. Differentially expressed genes (DEGs) were screened using RNA-Seq. RT-PCR was performed to further focus and verify these results. The gut microbiome composition was examined based on 16S rRNA gene amplicon sequencing, and the short-chain fatty acids produced were further analyzed.Results We found that GTSs intervention effectively improved the intestinal injury caused by simulated weightlessness, including reducing the pathological damage, increasing the expression of tight junction proteins and reducing the levels of inflammatory factors. Moreover, GTSs treatment significantly restored the levels of intestinal immunity-related genes and remodeled the gut microbiota. In particular, GTSs significantly increased the abundance of short-chain fatty acid metabolism-related bacteria, thereby increasing the level of propionic acid, butyric acid, isobutyric acid.Conclusion Our results revealed that GTSs improved intestinal microecological disorders and impaired immune function caused by the weightlessness simulation. The underlying mechanism may be related to the “intestinal immune -microbiota-metabolic” pathway. These findings provide a theoretical basis for the precise design and development of GTSs for space-health products.

CAS / MDL: 107-92-6 64-19-7 79-09-4
研究领域: 航天医学 · 分子生物学 · 免疫学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ACS Omega · 2021 · IF 3.512

Green Conversion of Saponins to Diosgenin in an Alcoholysis System Catalyzed by Solid Acid Derived from Phosphorus Tailings

Bowei Shen,XueJun Yu,Wenxiu Jiang,Hui Yuan,Mengqi Zhao,Hong Zhou,Zhiquan Pan

This work proposed to prepare solid acid from phosphorus tailings and successfully convert Dioscorea zingiberensis C.H. Wright (DZW) into diosgenin from the perspective of solid waste resource reuse and clean production. The results showed that SiO2–SO3H solid acid could catalyze the production of diosgenin from total saponins under solvothermal reaction conditions. In addition, the parameters of a single factor, such as the amount of SiO2–SO3H, solvent volume, reaction temperature, and reaction time, were optimized to confirm the optimal range of reaction conditions, and the optimal process conditions were determined by the response surface method. The yield of diosgenin was 2.45 ± 0.17% under the optimum conditions, and the yield of diosgenin was increased by 12.90% compared with the traditional acid hydrolysis process. Except the relatively higher catalytic activity, the alcoholysis approach for the production of diosgenin has no waste liquid to discharge. The products were analyzed by high-performance liquid chromatography-mass spectrometry, and the pathway to convert total saponins into diosgenin under SiO2–SO3H has been proposed. Moreover, the adopted catalyst can be prepared with very low cost from phosphorus tailings. Considering the obvious superiorities, the alcoholysis approach in this work could be a promising strategy for green production of diosgenin as well as a possible utilization pathway of phosphorus tailings.

研究领域: 中药化学 · 环境科学 · 催化化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS · 2025 · IF 3.1

Simultaneous determination of 13 representative saponins from the total saponins of Gynostemma pentaphyllum in rat plasma using LC-MS/MS for pharmacokinetic study

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.

CAS / MDL: 64-18-6
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
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MOLECULES · 2023 ·Vol. 28 ·期 5 ·2416 · IF 4.6

Anti-Inflammatory Activity of Panax notoginseng Flower Saponins Quantified Using LC/MS/MS

Junchen Liu,Yuehang Wu,Wenrui Ma,Hongyan Zhang,Xianyao Meng,Huirong Zhang,Miaomiao Guo,Xiao Ling,Li Li

Panax notoginseng(Burk) F. H. Chen is a traditional Chinese medicinal and edible plant. However,Panax notoginsengflower (PNF) is rarely used. Therefore, the purpose of this study was to explore the main saponins and the anti-inflammatory bioactivity of PNF saponins (PNFS). We explored the regulation of cyclooxygenase 2 (COX–2), a key mediator of inflammatory pathways, in human keratinocyte cells treated with PNFS. A cell model of UVB-irradiation-induced inflammation was established to determine the influence of PNFS on inflammatory factors and their relationship with LL–37 expression. An enzyme-linked immunosorbent assay and Western blotting analysis were used to detect the production of inflammatory factors and LL37. Finally, liquid chromatography–tandem mass spectrometry was employed to quantify the main active components (ginsenosides Rb1, Rb2, Rb3, Rc, Rd, Re, Rg1, and notoginsenoside R1) in PNF. The results show that PNFS substantially inhibited COX–2 activity and downregulated the production of inflammatory factors, indicating that they can be used to reduce skin inflammation. PNFS also increased the expression of LL-37. The contents of ginsenosides Rb1, Rb2, Rb3, Rc, and Rd in PNF were much higher than those of Rg1, and notoginsenoside R1. This paper provides data in support of the application of PNF in cosmetics.Keywords:Panax notoginsengflower;UVB;inflammatory factor;antibacterial peptide LL-37;total saponin;LC/MS/MS

CAS / MDL: 75-05-8 67-56-1
研究领域: 药理学 · 生物化学 · 药物化学 · 化妆品
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Drug Design Development and Therapy · 2022 · IF 4.319

Ultrasound-Assisted Extraction of Total Saponins from Aralia taibaiensis: Process Optimization, Phytochemical Characterization, and Mechanism of α-Glucosidase Inhibition

Huan Li,Bingtao Zhai,Jing Sun,Yu Fan,Junbo Zou,Jiangxue Cheng,Xiaofei Zhang,Yajun Shi,Dongyan Guo

Purpose Aralia taibaiensis, a medicinal food plant, and total saponins from its root bark extract inhibit α-glucosidase activity, which is associated with type 2 diabetes; however, the inhibitory mechanism is unknown. Furthermore, a green extraction technique superior to conventional hot reflux extraction (HRE) is needed for the rapid and easy extraction of A. taibaiensis total saponins (TSAT) to exploit and utilize this resource. Our aim was to develop a green extraction method for obtaining TSAT and to investigate the mechanism by which TSAT inhibits α-glucosidase.Materials and Methods In this study, the ultrasound-assisted extraction (UAE) process was optimized using a Box–Behnken design, and the extraction mechanism was investigated using scanning electron microscopy (SEM). High-performance liquid chromatography (HPLC) was used for qualitative and quantitative analyses of TSAT. In vitro glycosylation assays, enzyme kinetics, fluorescence spectroscopy measurements, atomic force microscopy (AFM), Fourier transform infrared spectroscopy (FT-IR) and molecular docking techniques were used to investigate the mechanism by which the A. taibaiensis active ingredients inhibit α-glucosidase.Results The optimal parameters for the extraction yield were obtained as an ethanol concentration of 73%, ultrasound time of 34 min, ultrasound temperature of 61 °C and solid–liquid ratio of 16 g/mL, which were better than HRE. The SEM analysis showed that UAE effectively disrupted plant cells, thus increasing the TSAT yield. In vitro α-glucosidase inhibition experiments showed that both TSAT and its active ingredient, araloside A, inhibited α-glucosidase activity by binding to α-glucosidase, thereby changing the conformation and microenvironment of α-glucosidase to subsequently inhibit enzyme activity.Conclusion The optimal extraction conditions identified here established a basis for future scale-up of ultrasound extraction parameters with the potential for obtaining maximum yields. In vitro enzyme inhibition experiments investigated the mechanism of the TSAT interaction with α-glucosidase and further explored whether araloside A may be the main contributor to the good inhibition of α-glucosidase activity by TSAT.

研究领域: 药用植物学 · 天然产物化学 · 糖尿病研究
✓ 已验证 DOI 高影响因子
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MICROCHEMICAL JOURNAL · 2024 · IF 4.9

Rapid on-site multi-indicator detection of Polygonatum cyrtonema Hua by handheld near-infrared spectroscopy with wavelength selection

Shuanglin Deng,Fang Wang,Meng Xiong,Bangxing Han,Hui Yan

The rapid, accurate, and on-site quantitative evaluation of the 3 components (total polysaccharide, total flavonoid, and total saponin) of Polygonatum cyrtonema Hua (PCH) is of great significance to ensure the value of its medicine and food, for this purpose, a handheld near-infrared (NIR) spectrometer was used. The raw NIR spectra were preprocessed by seven methods and their combinations, then three kinds of wavelength selection algorithms, the competitive adaptive reweighted sampling (CARS), random frog (RF) sampling, and Monte Carlo uninformative variable elimination (MCUVE) were applied, and the characteristic wavelengths for total polysaccharide, total saponin, and total flavonoid in PCH were obtained, respectively. Subsequently, the partial least squares (PLS) regression models were developed. The results showed that the combination of first derivative and standard normal variate was the optimal pretreatment method, and CARS had the highest performance of the wavelength selection for total polysaccharide and total flavonoid, while RF was the highest for total saponin. With these selected wavelengths, 3 PLS prediction models were built, and their performances were validated with unknown samples, the results showed that the determination coefficient of the prediction set (R 2 P ) of total polysaccharide, total saponin, and total flavonoid were 0.980, 0.948, and 0.942, respectively, and the corresponding root mean square error of prediction set (RMSEP) were 0.162, 0.142, and 0.052. Furthermore, the residual prediction deviations (RPDs) of the three components were all larger than 3, demonstrating the prediction performance of the models was high. Therefore, the three active functional components in PCH could be rapidly determined by a handheld NIR spectrometer, which would be beneficial for ensuring the quality of PCH.

研究领域: 中药分析 · 光谱学
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS · 2016 · IF 3.169

Metabonomic identification of the effects of the Zhimu-Baihe saponins on a chronic unpredictable mild stress-induced rat model of depression

Hongli Du,Keqing Wang,Li Su,Hongxia Zhao,Songyan Gao,Qishan Lin,Xiaofang Ma,Baokang Zhu,Xin Dong,Ziyang Lou

The herbal pair Zhimu-Baihe (Zhimu: Anemarrhena asphodeloides ; Baihe: Lilium brownii var. viridulum ) is a traditional Chinese medicament used for the treatment of depression. However, the relevant mechanisms of action has not been clarified. This study investigated the anti-depressant activity of the total saponins from Zhimu and Baihe and the mechanisms underlying using a chronic unpredictable mild stress (CUMS)-induced rat model of depression. High performance liquid chromatography with electrochemical detection (HPLC-ECD) was applied to determine the levels of three monoamine neurotransmitters, 5-hydroxytryptamine (5-HT), noradrenaline (NE) and dopamine (DA), in the rat hippocampus. Optimized pretreatment of samples and mass spectrometry conditions were used to analyse the metabonomic profile of the hippocampus. The 5-HT and NE levels in the CUMS group were reduced compared with the control group, whereas all groups had similar DA levels. The metabonomic profile of the hippocampus revealed 32 differential metabolites between the CUMS and control group, among which 18 metabolites were significantly recovered in the Anemarrhena saponins and Lilium saponins (AL) combination intervention group. These results suggested an anti-depressant effect of AL. Moreover, 24 metabolites in AL group were better recovered compared with the Anemarrhena saponins (AS) or Lilium saponins (LS) intervention groups, suggesting a synergetic effect of AS and LS in the treatment of depression. The anti-depressant effect might be related to the regulation of several metabolic pathways, including monoamine neurotransmitter synthesis (especially 5-HT and NE), and amino acid, fatty acid, and phospholipid metabolism in rats.

CAS / MDL: 103616-89-3
研究领域: 中药学 · 神经科学 · 代谢组学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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