JOURNAL OF DISPERSION SCIENCE AND TECHNOLOGY
·
2021
·
IF 2.262
Jialiang Lin,Min Tang,Manjunath D. Meti,Yong Liu,Qingguo Han,Xu Xu,Yuan Zheng,Zhendan He,Zhangli Hu,Hong Xu
The interaction of bovine serum albumin (BSA) with Ginsenoside Rd (GSRd) was studied using multiple spectroscopic methods, isothermal titration calorimetry (ITC), molecular docking and density functional theory (DFT) calculation. The fluorescence experiments showed that GSRd quenched BSA intrinsic fluorescence via a static quenching process because of the formation of the GSRd-BSA complex. UV-visible and circular dichroism (CD) spectral studies indicated that the binding of GSRd to BSA resulted in the loosening and unfolding of BSA backbone, with the loss of partial α-helix structures. Also, thermodynamic parameters obtained from ITC experiment suggested that BSA-binding of GSRd was a spontaneous endothermic reaction driven by entropy, and that hydrophobic interactions were the main forces within the BSA-GSRd complex. Additionally, docking studies and DFT calculation further implied that hydrogen bonds also helped stabilize the GSRd-BSA system. These research results could help us better understand the pharmacokinetic behavior of GSRd, and provide useful conformational change information of BSA induced by the bound drugs, to the design of analogues drugs with more effective pharmacological properties.
研究领域:
药理学
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生物化学
·
计算生物学
✓ 已验证
DOI
高影响因子
Frontiers in Cellular and Infection Microbiology
·
2022
·
IF 6.073
Zhou Shuhui,Ji Yaoting,Yao Hantao,Guo Haiying,Zhang Zichen,Wang Zijun,Du Minquan
Periodontitis is a worldwide oral disease induced by the interaction of subgingival bacteria and host response and is characterized by local inflammation, bone resorption, and tooth loss. Ginsenoside Rd (Rd) is a biologically active component derived from Panax ginseng and has been demonstrated to exert antibacterial and anti-inflammatory activities. This study aims to investigate the inhibitory efficiency of Rd towards Porphyromonas gingivalis (P. gingivalis), periodontal inflammatory response, and osteoclastogenesis in vitro and to further validate the results in a mouse periodontitis model, thus, evaluate the potential effects of Rd on the control and prevention of periodontitis. According to the results, Rd exerted excellent antibacterial activities against planktonic P. gingivalis, along with attenuating P. gingivalis virulence and inhibiting its biofilms. Meanwhile, the inflammatory cytokine production and osteoclastogenesis were remarkably inhibited by Rd both in vitro and in vivo. Furthermore, Rd efficiently ameliorated the subgingival P. gingivalis abundance and suppressed the alveolar bone resorption in vivo as well. In conclusion, Rd has the potential to be developed as a promising medication in the control and prevention of periodontitis.
研究领域:
口腔科学
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药理学
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微生物学
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DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2024
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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
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生物技术
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药理学
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微生物学
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DOI
PubMed
高影响因子
WORLD JOURNAL OF MICROBIOLOGY & BIOTECHNOLOGY
·
2011
·Vol. 28
·期 3
·857-863
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IF 1.214
Ye Li,Zhang Chunyan,Li Jiyang,Shi Xunlong,Feng Meiqing
Calcium is a known signalling molecule in eukaryotic cells and plays a central role in the regulation of many cellular processes. In the following study, we report on the effect of external calcium treatments on the biotransformation of ginsenoside Rb1 to ginsenoside Rd by Paecilomyces bainier 229-7. We observed that the intracellular calcium content of P . bainier 229-7 mycelia was increased in response to exposure to high external Ca 2+ concentrations. Both ginsenoside Rd biotransformation and β-glucosidase activity were both found to be dependent on the external calcium concentration. At an optimal Ca 2+ concentration of 45 mM, maximal ginsenoside Rd bioconversion rate of 92.44% was observed and maximal β-glucosidase activity of 0.1778 U was reached in a 72-h biotransformation. The Ca 2+ channel blocker Verapamil blocked the trans-membrane influx of calcium and decreased ginsenoside Rd biotransformatiom. In addition, β-glucosidase activity and ginsenoside Rd content decreased by 36.0 and 29.2% respectively after a 72-h incubation in the presence of 0.05 mM Calmodulin (CaM) antagonist Perphenazine. These results suggest that both Ca 2+ channels and CaM are involved in ginsenoside Rd biotransformation via regulation of β-glucosidase activity. This is the first report regarding the effects of calcium signal transduction on biotransformation and enzyme activity in fungi.
研究领域:
药理学
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微生物学
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生物化学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2022
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IF 5.195
Jinxia Hou,Lanping Zhong,Jianming Liu,Fanglan Liu,Chunhua Xia
Ethnopharmacological relevance Shengmai formula (SMF) is a classical traditional Chinese medicine prescription, which is widely used in the treatment of cardiovascular and cerebrovascular diseases . Our previous studies have demonstrated that some components in SMF can interact with each other through breast cancer resistance protein , sodium taurocholate co-transporting polypeptide , organic anion transporting polypeptide 1B1 and 1B3. Organic anion transporter 1 (OAT1) is highly expressed in kidney, mediating the elimination of many endogenous and exogenous substances. However, the interaction between the main active components in SMF and OAT1 is not clear. Aim of the study This study aimed to investigate the interactions of the major bioactive components in SMF mediated by OAT1. Materials and methods Four main fractions, namely, ginseng total saponins (GTS), ophiopogon total saponins (OTS), ophiopogon total flavonoids (OTF), fructus schisandrae total lignans (STL), and 12 active components, namely, ginsenoside Rg1, Re, Rd and Rb1, ophiopogonin D and Dˊ, methylophiopogonanone A and B, schizandrol A and B, schizandrin A and B, were selected to explore the interactions of SMF with OAT1 using cell and rat models. Results The above four main fractions in SMF all exhibited inhibitory effects on the uptake of 6-carboxyfluorescein (6-CF), a classic substrate of OAT1. Among the 12 main effective components, only ginsenoside Re , Rd, and methylophiopogonanone A showed inhibition of 6-CF uptake. Additionally, we found that schizandrin B was transported by HEK293-OAT1 cells, and schizandrin B uptake was markedly inhibited by GTS, OTS, OTF, ginsenoside Re, Rd, and methylophiopogonanone A. In rats, ginsenoside Re, Rd, and methylophiopogonanone A jointly increased the AUC (0-t) , AUC (0-∞) , and C max of schizandrin B, but they decreased its clearance in plasma and excretion in urine. Conclusions Ginsenoside Re, Rd, and methylophiopogonanone A were the potential inhibitors of OAT1, and may interact with some drugs serving as OAT1 substrates clinically. Schizandrin B was a potential OAT1 substrate, and its OAT1-mediated transport was inhibited by ginsenoside Re, Rd, and methylophiopogonanone A. OAT1-mediated interactions of the main active components in SMF can be regarded as one of the important compatibility mechanisms of traditional Chinese medicine preparations.
研究领域:
药理学
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中药学
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分子生物学
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药物代谢
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产品关联
DOI
PubMed
高影响因子
SEPARATION AND PURIFICATION TECHNOLOGY
·
2024
·
IF 8.1
Wenqing Zhang,Lu Yin,Qiuyu Han,Jinhui Xu,Yanyu Xiang,Ziyang Zhang,Liping Fan,Pingyuan Ge,Yufan Shang,Xinyuan Wang,Yue Zhang,Zhishu Tang,Mianhua Wu,Bo Li,Huaxu Zhu
This study presents a novel biocatalytic membrane (BM) system for the continuous production of high-purity ginsenoside Rd. Recognizing that enzymes concentrated on one side of BM caused by reverse filtration hinder substrate access and catalytic efficiency, polyethyleneimine (PEI) and polyallylamine hydrochloride (PAH) were added during dopamine (DA) deposition. They effectively disrupted the clustering of enzyme molecules, enabling a more homogeneous enzyme distribution within BMs, as confirmed by microscopy, activity assays, and simulations. This controlled dispersion, facilitated by Protein-Polyelectrolyte Complexes (PPCs) formation, significantly improved substrate accessibility and catalytic performance. Exceptional catalytic performance was exhibited by the optimized PDA/PEI BM (using 1800 Da PEI), enabling highly efficient conversion of Rb1 to Rd. This high conversion efficiency, coupled with the inherent temperature-dependent solubility of Rd, enables a remarkably simple purification process. By exploiting Rd precipitation upon cooling, high-purity (93.1 %) Rd was achieved at a 55.6 % recovery from a 70 % purity Rb1 feed using a simple solid–liquid separation, eliminating the need for other separation techniques. This study provides new insights into the preparation of BMs and offers innovative strategies for the transformation and purification of ginsenosides.
研究领域:
生物技术
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药学
·
化学工程
·
生物化学
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）