JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
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2020
·
IF 3.209
Xin Qiao,Cheng Qu,Qiming Luo,Yuanzhong Wang,Jie Yang,Hua Yang,Xiaodong Wen
Rhizoma Paridis (RP) with significant anti-tumor and haemostatic effects, has been used as the raw material of many Traditional Chinese preparations. However, its active ingredients are still unclear. The present study aimed to discover bioactive ingredients from RP based on spectrum-relationship and chemometric methods. Firstly, the saponins extract was prepared by phytochemical methods. Furthermore, UHPLC-QTOF-MS and UHPLC-qMS were incorporated to establish an efficient and sensitive method for obtaining the chemical profiles of RP. A total of 34 saponins were characterized in RP and 13 of them were assigned as common peaks in 25 batches of samples. After evaluation of the anti-tumor and haemostatic activities of samples, spectrum-effect relationships were investigated by the grey relational analysis (GRA), orthogonal projections to latent structures (OPLS) and back propagation artificial neural network (BP-ANN). These analyses showed that polyphyllin VII (P27), polyphyllin II (P30), dioscin (P31) and polyphyllin I (P33) play a role in the haemostatic effects of RP whereas polyphyllin VII (P27), dioscin (P31), polyphyllin I (P33), progenin III (P34) were assigned as candidate ingredients accounting for the anti-tumor activity of RP. The anti-tumor and haemostatic activities of these screened ingredients were subsequently verified in vitro . Collectively, the present study established the spectrum-effect relationship mode of RP and discovered the bioactive compounds of RP, which could be also used for exploration of bioactive compounds in herbal medicines, especially for trace compounds.
研究领域:
药理学
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分析化学
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中药学
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产品关联
DOI
PubMed
高影响因子
MOLECULES
·
2017
·Vol. 22
·期 12
·2067
·
IF 2.861
Fan-Cheng Meng,Qiu-Shuang Wu,Ruibing Wang,Shao-Ping Li,Li-Gen Lin,Ping Chen,Qing-Wen Zhang
Panacis Japonici Rhizoma (Zhu-Jie-Shen in Chinese), the root ofP. japonicusC.A. Mey., is commonly used in traditional Chinese Medicine. Saponins are the major bioactive compounds in this herb. The similarity of polarity and structure of the natural products in herb caused the difficulty of purification and resulted in the shortage and high cost of the reference compounds, which has greatly hindered efforts toward quantification in quality control. A novel strategy using a standardized reference fraction for qualification of the major saponins in Panacis Japonici Rhizoma was proposed to easily and effectively control the quality of PJR. The strategy is feasible and reliable, and the methodology of the developed approach is also validated. The standardized reference fraction was used for quantification, which might solve the shortage of the pure reference compounds in the quality control of herbal medicines.Keywords:Panax japonicusC. A. Mey.;Panacis Japonici Rhizoma;triterpenoid saponin;ginsenoside;chikusetsusaponin;pseudoginsenoside;standardized reference fraction;quantification;quality control;HPLC
研究领域:
中药学
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植物化学
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药理学
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产品关联
DOI
PubMed
高影响因子
ARCHIVES OF MICROBIOLOGY
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2024
·Vol. 206
·期 4
·1-10
·
IF 2.3
Diao Mengxue,Chen Yanchi,Meng Lijun,Li Jianxiu,Xie Nengzhong
The stems and leaves of Panax notoginseng contain high saponins, but they are often discarded as agricultural waste. In this study, the predominant ginsenosides Rg1, Rc, and Rb2, presented in the stems and leaves of ginseng plants, were biotransformed into value-added rare ginsenosides F1, compound Mc1 (C-Mc1), and Rd2, respectively. A fungal strain YMS6 ( Penicillium sp.) was screened from the soil as a biocatalyst with high selectivity for the deglycosylation of major ginsenosides. Under the optimal fermentation conditions, the yields of F1, C-Mc1, and Rd2 were 97.95, 68.64, and 79.58%, respectively. This study provides a new microbial resource for the selective conversion of protopanaxadiol-type and protopanaxatriol-type major saponins into rare ginsenosides via the whole-cell biotransformation and offers a solution for the better utilization of P . notoginseng waste.
研究领域:
药用植物学
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微生物学
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天然产物化学
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DOI
PubMed
高影响因子
Chinese Journal of Natural Medicines
·
2025
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IF 4.9
Yongsheng Fang,Zhiyun Zhu,Chun Xie,Dazhen Xia,Huimin Zhao,Zihui Wang,Qian Lu,Caimei Zhang,Wenyong Xiong,Xiaodong Yang
Saponins associated with Panax notoginseng ( P. notoginseng ) demonstrate significant therapeutic efficacy across multiple diseases. However, certain high-yield saponins face limited clinical applications due to their reduced pharmacological efficacy. This study synthesized and evaluated 36 saponin-1,2,3-triazole derivatives of ginsenosides Rg1/Rb1 and notoginsenoside R1 for anti-adipogenesis activity in vitro . The research revealed that the ginsenosides Rg1-1,2,3-triazole derivative a17 demonstrates superior adipogenesis inhibitory effects. Structure-activity relationships (SARs) analysis indicates that incorporating an amidyl-substituted 1,2,3-triazole into the saponin side chain via Click reaction enhances anti-adipogenesis activity. Additionally, several other derivatives exhibit general adipogenesis inhibition. Compound a17 demonstrated enhanced potency compared to the parent ginsenoside Rg1. Mechanistic investigations revealed that a17 exhibits dose-dependent inhibition of adipogenesis in vitro , accompanied by decreased expression of preadipocytes. Peroxisome proliferator-activated receptor γ (PPARγ), fatty acid synthase (FAS), and fatty acid binding protein 4 (FABP4) adipogenesis regulators. These findings establish the ginsenoside Rg1-1,2,3-triazole derivative a17 as a promising adipocyte differentiation inhibitor and potential therapeutic agent for obesity and associated metabolic disorders. This research provides a foundation for developing effective therapeutic approaches for various metabolic syndromes.
研究领域:
药物化学
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药理学
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天然产物
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生物有机化学
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代谢性疾病研究
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DOI
PubMed
高影响因子
Frontiers in Pharmacology
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2022
·
IF 5.988
Dong Rong,Zhang Yougang,Chen Shanjun,Wang Huan,Hu Kaiqing,Zhao Huanxin,Tian Qingping,Zeng Kewu,Wang Songsong,Han Liwen
Background: American ginseng (Panax quinquefolium L., AG) is a traditional Chinese medicine with multiple cardiovascular protective properties. Many bioactive components have been discovered in AG over these years. However, the understanding of these key pharmacodynamic components of activity against heart failure is insufficient.Methods: A heart failure model was established using AB line wild-type zebrafish (Danio rerio) to evaluate the anti-heart failure activity of AG. Untargeted metabolomics analysis based on ultra-high performance liquid chromatography-quadrupole electrostatic field orbitrap-mass spectrometry technology (UHPLC-QE-Orbitrap-MS) was performed to screen differential components from AG samples. The potential active components were verified using the zebrafish model. Simultaneously, network pharmacology and molecular docking techniques were used to predict the possible mechanism. Finally, the key targets of six key pharmacodynamic components were verified in zebrafish using quantitative real-time-polymerase chain reaction (Q-PCR) techniques.Results: The heart failure model was successfully established in 48 h of post-fertilization (hpf) zebrafish larvae by treating with verapamil hydrochloride. The zebrafish assay showed that the anti-heart failure effects of AG varied with producing regions. The result of the herbal metabolomic analysis based on UHPLC-QE-Orbitrap-MS indicated that ginsenoside Rg3, ginsenoside Rg5, ginsenoside Rg6, malic acid, quinic acid, L-argininosuccinic acid, 3-methyl-3-butenyl-apinosyl (1→6) glucoside, pseudoginsenoside F11, and annonaine were differential components, which might be responsible for variation in efficacy. Further analysis using zebrafish models, network pharmacology, and Q-PCR techniques showed that ginsenoside Rg3, ginsenoside Rg5, ginsenoside Rg6, malic acid, quinic acid, and pseudoginsenoside F11 were the pharmacodynamic markers (P-markers) responsible for anti-heart failure.Conclusion: We have rapidly identified the P-markers against heart failure in AG using the zebrafish model and metabolomics technology. These P-markers may provide new reference standards for quality control and new drug development of AG.
研究领域:
药理学
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心脏病学
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代谢组学
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斑马鱼模型
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2024
·
IF 5.7
Jia-Yue Liu,Li-Juan Ma,Ru-Jie Yang,Yu Liu,Zheng Shu,Yong-Qing Cai,Qing-Wen Zhang,Feng-Qing Yang,Jian-Bo Wan
Rare dehydrated ginsenosides barely exist in natural ginseng plants. Herein, the confined microwave technique was utilized to transform the main ginsenosides of Panax notoginseng leaves (PNL) into dehydrated ginsenosides. The main microwave-treated products of dried PNL are dehydrated ginsenoside Rk1, Rg5, notoginsenoside SFt3, and SFt4. Comparatively, the main microwave-treated products of water preimmersed PNL are dehydrated ginsenoside Rk2, Rh3, notoginsenoside SFt3, and SFt4. The impacts of solvent, solid–liquid ratio, microwave temperature and duration on the yield of dehydrated ginsenosides were explored. Based on theoretical calculation, primary ginsenosides in water preimmersed PNL are more prone to deglycosylation at the C-20 site and dehydration elimination reactions at the side chain during microwave treatment. Moreover, reference compounds were used to verify ginsenoside transformation pathway, and the dehydrated ginsenosides were individually purified and identified. In short, this study elucidates novel approach for preparing rare Δ20(21)- and Δ20(22)-dehydrated protopanoxadiol ginsenosides.
研究领域:
植物化学
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药用植物学
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天然产物化学
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产品关联
DOI
PubMed
高影响因子
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
·
2020
·
IF 2.365
Bing Zhang,Wenli Pan,Yaxin Deng,Haibing He,Jingxin Gou,Yanjiao Wang,Yu Zhang,Tian Yin,Dongchun Liu,Xing Tang
Panax quinquefolium saponin (PQS) composed of 45% pseudo-ginsenoside F11 (PF11), is a natural mixture of sterol compounds obtained from the American ginseng plant, having numerous promising benefits for health. However, low solubility and permeability limit the development of PQS as a therapeutic agent for oral administration. In this study, PQS liposomes (PQS-Lips) were prepared by thin layer hydration, an in situ single-pass intestinal perfusion (SPIP) model was used to verify the improvement of membrane permeability of PQS-Lips. PQS-Lips had a high encapsulation efficiency (EE) of 65%∼70%, a particle size about 100.0 nm, and a zeta potential of −60 mV with regular spherical surface. FTIR and DSC showed the PQS in liposomes were amorphous, indicating that hydrogen bonds formed between one or several hydroxyl groups in PQS and C-O group at the phospholipid polar terminal. In addition, PQS-Lips showed sustained release in vitro than PQS at pH 1.2 and pH 6.8, and PQS-Lips had good stability in simulated gastric and intestinal fluid. Then, the absorption rate (Ka) and effective permeability coefficient (Peff) of PQS-Lips in the whole small intestine were significantly higher than those in PQS solution (PQS-Sol), which proved that the PQS-Lips could significantly increase the membrane permeability of PQS and promote its absorption in the small intestine. From the experimental results, it could be known that liposome technology could effectively improve the absorption of PQS in the small intestine.
研究领域:
药剂学
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生物药剂学
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中药学
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产品关联
DOI
PubMed
高影响因子
APPLIED MICROBIOLOGY AND BIOTECHNOLOGY
·
2024
·Vol. 108
·期 1
·1-13
·
IF 3.9
Wu Zongzhan,Dou Wenyu,Yang Xiaolin,Niu Tengfei,Han Zhuzhen,Yang Li,Wang Rufeng,Wang Zhengtao
Abstract Oleanane-type ginsenosides are a class of compounds with remarkable pharmacological activities. However, the lack of effective preparation methods for specific rare ginsenosides has hindered the exploration of their pharmacological properties. In this study, a novel glycoside hydrolase Pl GH3 was cloned from Paenibacillus lactis 154 and heterologous expressed in Escherichia coli . Sequence analysis revealed that Pl GH3 consists of 749 amino acids with a molecular weight of 89.5 kDa, exhibiting the characteristic features of the glycoside hydrolase 3 family. The enzymatic characterization results of Pl GH3 showed that the optimal reaction pH and temperature was 8 and 50 °C by using p -nitrophenyl- β - d -glucopyranoside as a substrate, respectively. The K m and k cat values towards ginsenoside Ro were 79.59 ± 3.42 µM and 18.52 s −1 , respectively. Pl GH3 exhibits a highly specific activity on hydrolyzing the 28- O - β - d -glucopyranosyl ester bond of oleanane-type saponins. The mechanism of hydrolysis specificity was then presumably elucidated through molecular docking. Eventually, four kinds of rare oleanane-type ginsenosides (calenduloside E, pseudoginsenoside RP1, zingibroside R1, and tarasaponin VI) were successfully prepared by biotransforming total saponins extracted from Panax japonicus . This study contributes to understanding the mechanism of enzymatic hydrolysis of the GH3 family and provides a practical route for the preparation of rare oleanane-type ginsenosides through biotransformation. Key points • The glucose at C-28 in oleanane-type saponins can be directionally hydrolyzed. • Mechanisms to interpret PlGH3 substrate specificity by molecular docking. • Case of preparation of low-sugar alternative saponins by directed hydrolysis.
研究领域:
生物化学
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药理学
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微生物学
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产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2015
·Vol. 5
·期 96
·78874-78879
·
IF 3.84
Hui-da Wan,Dan Li
A preliminary study on the enzymatic biotransformation of ginsenosides is evaluated. β-Galactosidase from Aspergillus sp. displayed β-glucosidase activity, which was responsible for its ability to transform major ginsenoside Rb1 to rare ginsenoside F2 via ginsenoside Rd. The Rb1 conversion, Rd and F2 yields reached 100%, 80.7% and 14.3% after 60 h at 60 °C, respectively. Ginsenoside Rg3 can be selectively hydrolyzed and only Rh2 was obtained with this β-galactosidase as well. Before hydrolysis, an Rg3 inclusion complex was prepared with hydroxypropyl-β-cyclodextrin (HP-β-CD) to improve the aqueous solubility. The solubility of Rg3 increased 74.6 fold, and the phase solubility curve displayed a typical AL-type, which indicates the formation of a 1 : 1 inclusion complex. Using an enzyme loading of 500 U g−1 Rg3, the highest Rg3 conversion of 90.6% and Rh2 yield of 88.5% were obtained after 24 h at 60 °C. These results indicate that β-galactosidase from Aspergillus sp. could be useful for the mass production of rare ginsenosides.
研究领域:
生物化学
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药学
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酶学
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产品关联
DOI
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
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分析化学
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药理学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2016
·
IF 3.169
Yang Huang,Tingting Zhang,Haibo Zhou,Ying Feng,Chunlin Fan,Weijia Chen,Jacques Crommen,Zhengjin Jiang
Triterpenoid saponins (TSs) are the most important components of some traditional Chinese medicines (TCMs) and have exhibited valuable pharmacological properties. In this study, a rapid and efficient method was developed for the separation of kudinosides, stauntosides and ginsenosides using supercritical fluid chromatography coupled with single quadrupole mass spectrometry (SFC-MS). The separation conditions for the selected TSs were carefully optimized after the initial screening of eight stationary phases. The best compromise for all compounds in terms of chromatographic performance and MS sensitivity was obtained when water (5–10%) and formic acid (0.05%) were added to the supercritical carbon dioxide/MeOH mobile phase. Beside the composition of the mobile phase, the nature of the make-up solvent for interfacing SFC with MS was also evaluated. Compared to reversed phase liquid chromatography, the SFC approach showed higher resolution and shorter running time. The developed SFC-MS methods were successfully applied to the separation and identification of TSs present in Ilex latifolia Thunb. , Panax quinquefolius L. and Panax ginseng C.A. Meyer . These results suggest that this SFC-MS approach could be employed as a useful tool for the quality assessment of natural products containing TSs as active components.
研究领域:
分析化学
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中药学
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植物化学
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DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2024
·
IF 5.7
Wenqi Xu,Cuicui Duan,Fumin Ma,Dan Li,Xiaolei Li
To convert ginsenosides Rb1, Rb2, Rb3, and Rc into Rd by a single enzyme, a putative β-glycosidase (Pxbgl) from the xylan-degrading bacterium Petroclostridium xylanilyticum was identified and used. The kcat/Km value of Pxbgl for Rb3 was 18.18 ± 0.07 mM–1/s, which was significantly higher than those of Pxbgl for other ginsenosides. Pxbgl converted almost all Rb3 to Rd with a productivity of 5884 μM/h, which was 346-fold higher than that of only β-xylosidase from Thermoascus aurantiacus. The productivity of Rd from the Panax ginseng root and Panax notoginseng leaf was 146 and 995 μM/h, respectively. Mutants N293 K and I447L from site-directed mutagenesis based on bioinformatics analysis showed an increase in specific activity of 29 and 7% toward Rb3, respectively. This is the first report of a β-glycosidase that can simultaneously remove four different glycosyls at the C–20 position of natural PPD-type ginsenosides and produce Rd as the sole product from P. notoginseng leaf extracts with the highest productivity.
研究领域:
生物化学
·
生物技术
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药理学
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微生物学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）