ENZYME AND MICROBIAL TECHNOLOGY
·
2022
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IF 3.705
Cheng Zeng,Xiangqing Ji,Yu Shi,Siyu Mu,Yicheng Huang,Meiqiao Zhong,Yan Han,Cuicui Duan,Xiaolei Li,Dan Li
To develop a new method for enzymatic preparation of minor ginsenosides , T. stercorarium β-glucosidase (Tsbgl) was characterized and its activities of deglycosylation towards natural ginsenosides were examined. The substrates of 1 mmol l −1 were incubated with the enzyme of 38.3 U ml −1 at 65 ℃ and pH 5.0. The K m values of Tsbgl for ginsenosides Rb 1 , Rg 1 and p NPG were 0.37 ± 0.03, 3.26 ± 0.19, and 1.24 ± 0.03 mmol l −1 , and the V max values were 183.63 ± 7.15, 85.03 ± 4.90, and 117.66 ± 1.96 μmol mg −1 min −1 , respectively. The molar conversion of ginsenosides Rb 1 , Rb 2 , Rb 3 , Rc, Re, Rg 1 , and Rf by Tsbgl within 6 h was 100%, 50.1%, 42.7%, 92.0%, 57.3%, 67.9%, and 76.8%, respectively. The yield of aglycone protopanaxadiol was 35.5 μmol l −1 h −1 for Rb 1 , while the yields of aglycone protopanaxatriol were 64.2 and 70.4 μmol l −1 h −1 for Rg 1 and Rf. Tsbgl with good organic solvent tolerance, mild reaction conditions and broad substrate specificity , could completely remove all outer glucosyls at the C-3 and C-20 hydroxyls of protopanaxadiol-type ginsenosides, and the C-6 and C-20 hydroxyls of protopanaxatriol-type ginsenosides through various pathways, providing a specific and efficient way to produce minor ginsenosides.
研究领域:
生物化学
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药理学
·
酶学
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DOI
PubMed
高影响因子
FITOTERAPIA
·
2024
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IF 2.5
Hongliu Xie,Fang Lin,Fei Shi,Elaine Johnstone,Yaqi Wang,Yang An,Jun Su,Jiayin Liu,Qinghai Dong,Jihua Liu
As one of the metabolites of ginseng, 20( S )-protopanaxadiol (PPD) is a compound with dammarane-type tetracyclic triterpene, which performs a wide range of anticancer activities. In this study, PPD was used as a lead. A series of compounds were synthesized respectively with 11 amino acids through esterification and were evaluated for their cytotoxicity against several cancer cell lines. One of the synthetic products (PL) exhibited potent inhibitory effect on Huh-7 cells relative to that of PPD in vitro. Subsequently, the Annexin V-FITC /PI staining assay was used to verify that PL induced apoptosis of Huh-7 cells in a dose-dependent manner. A UPLC-Q/TOF-MS analysis method was established and validated for assessing pharmacokinetic properties after the administration of PPD and PL in rats. The results showed that compared with PPD, T 1/2 of PL in rats was prolonged, and the peak time was delayed, resulting in broader tissue distribution of the compound in the body. In addition, the targets of PL against several cancers were predicted and analyzed via network pharmacology. Molecular docking simulations demonstrated that PL interacted with the active sites of the above targets. In conclusion, this study provided a theoretical basis for the development and clinical application of anti-tumor activity of PPD.
研究领域:
药理学
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肿瘤学
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中药化学
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产品关联
DOI
PubMed
高影响因子
Journal of Biomedical Nanotechnology
·
2024
·Vol. 20
·期 6
·1041-1048
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IF 2.9
Li Shizheng,Lv Yanwei,Liu Xiaoying,Yuan Yuan
Chronic wounds in diabetic patients have become a common complication. However, current wound management tends to yield unsatisfactory outcomes and may give rise to complications. Therefore, we prepare a nano-structured lipid carrier by incorporating a 20(S)-Protopanaxadiol (PPD)-loaded
lipid nanoparticles (PPD-N) into a silicone elastomer (PPD-NS) for treating chronic diabetic wounds and assess its therapeutic efficacy in promoting diabetic wound healing and vascular regeneration in a mouse model. Our findings revealed that the prepared PPD-N showed uniform distribution
with spherical morphology and an average diameter of approximately 130 nm. Moreover, PPD-NS exhibited a wound closure rate of 92.1% after 48 hours of treatment and demonstrated enhanced vascular regeneration. Therefore, it can be concluded that the prepared PPD-NS can effectively be used in
diabetic wound repair and vascular regeneration. This study provides a promising potential therapeutic option for diabetic wounds.
研究领域:
药学
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生物医学工程
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伤口护理
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糖尿病研究
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DOI
高影响因子
Food Frontiers
·
2023
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IF 9.9
Pengde Lu,Jinfen Chen,Ying Chen,Xingping Quan,Jiayue Liu,Yan Han,Yiyang Li,Li Yang,Jian-Bo Wan,Yonghua Zhao
Ulcerative colitis (UC) is a digestive disease with a high incidence and is difficult to be cured due to its complex etiology. It has evidenced that intestinal barrier dysfunction plays a predominant role in UC. 20( S )-protopanaxadiol saponins (PDS) isolated from Panax notoginseng possess anti-inflammatory and antioxidative activities, suggesting its potential of treating UC. Herein, the therapeutic effects of PDS against UC and underlying mechanisms in the aspect of intestinal barrier dysfunction were investigated in vivo and in vitro. The results showed PDS had protective effects against dextran sulfate sodium–induced colitis, including attenuating weight loss, disease activity index score elevation, colon length shortening, and histological lesions. Additionally, PDS reduced the colonic activity of myeloperoxidase and the cytokine levels of TNF-α, IL-6, and IL-1β, decreased MDA production, and elevated colonic activities of SOD and GSH-Px in the colitis mice. The expressions of proteins related to tight junction (TJ), including ZO-1, claudin-5, occludin, caveolin-1 (Cav-1), and Nrf2 were downregulated, whereas that of Keap1 was upregulated after colitis induction. These changes were reversed by PDS. Cav-1 expression was downregulated in lipopolysaccharides (LPS)- and H 2 O 2 -induced HCT116 cells, and the expressions of ZO-1, claudin-5, and occludin were suppressed in HCT116 cells stimulated by LPS and H 2 O 2 combined with Cav-1 small interfering RNA transfection, which were ameliorated by PDS, suggesting PDS targeted Cav-1 against intestinal barrier damage. Collectively, PDS alleviates inflammatory injury and oxidative stress by regulating the Nrf2/Keap1 pathway, contributing to targeting Cav-1 against intestinal epithelial TJ proteins loss. It suggests PDS might be a promising therapeutic natural product for UC treatment.
研究领域:
药理学
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胃肠病学
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免疫学
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分子生物学
✓ 已验证
DOI
高影响因子
Food Bioscience
·
2024
·
IF 4.8
Yanbo Hu,Yiming Li,Yuzhu Shen,Baochun Zhang,Jiaxin Liu,Yi Cao,Jun Zhao
In this study, six rare protopanaxadiol (PPD)-type ginsenosides, namely, F2, CK, C-Mc1, C-Mc, CO, and CY, were prepared using enzymatic hydrolysis. Firstly, major (PPD)-type ginsenosides, including Rb1, Rb2, Rc, and Rd, were biotransformed by employing single and combined β-glucosidases BaBgl1A and BaBgl3A. Thin-layer chromatography (TLC) and high-performance liquid chromatography (HPLC) analyses revealed that ginsenosides F2, CO, and C-Mc1 could be produced by BaBgl1A, while rare ginsenosides CK, CY, and C-Mc could be produced by the combined use of BaBgl1A and BaBgl3A. Furthermore, optimal preparation conditions for these rare ginsenosides were elucidated, with yields exceeding 76.34%. Additionally, large quantities of rare ginsenosides were prepared to determine their structures. Characteristic absorption peaks in 13 C NMR spectra and ion peaks in MALDI-TOF-MS suggested that the six high-purity rare ginsenosides (i.e., F2, CO and C-Mc1, CK, CY, and C-Mc) could be produced at high-efficiency. The findings of this study offer insights into novel enzymolysis methods for the targeted preparation of rare PPD-type ginsenosides, thus widening the range of raw materials that could be directed to in-depth biological activity research.
研究领域:
生物化学
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药理学
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生物技术
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DOI
高影响因子
JOURNAL OF PHARMACY AND PHARMACOLOGY
·
2024
·
IF 2.8
Song Zeyu,Li Zhenyuan,Pan Tao,Liu Teng,Gong Baifang,Wang Zhixia,Liu Ke,Fan Huaying
ObjectivesAcute kidney injury (AKI) caused by cisplatin (CDDP) is a complex, critical illness with no effective or specific treatment. The purpose of the study was to assess the protective effect of protopanaxadiol (PPD) on the kidneys in CDDP-induced AKI models and its possible mechanisms.MethodsIn vitro, the protection of PPD was assessed in HK-2. KM mice were injected with CDDP to induce AKI models in vivo. The determination of blood urea nitrogen and serum creatinine (SCr) was performed, and pathological changes were examined by histopathological examination. Immunostaining and western blot analyses were used to analyze the expression levels of proteins.ResultsPPD can increase the viability of HK-2 cells damaged by CDDP, improve cell morphology, and alleviate the symptoms of AKI in mice. In addition, PPD can down-regulate the protein expression of TRF and up-regulate the protein expression of Ferritin heavy chain, Glutathione peroxidase 4, and ferroptosis suppressor protein 1 reduce the iron content in cells and kidney tissues, and restore the antioxidant defense system.ConclusionPPD has an inhibitory effect on cisplatin-induced nephrotoxicity, which may be related to the inhibition of ferroptosis by regulating iron metabolism and lipid peroxidation.
研究领域:
药理学
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肾病学
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细胞生物学
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分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ENZYME AND MICROBIAL TECHNOLOGY
·
2026
·
IF 3.9
Fan Xu,Yuting Liao,Yulei Zhang,Nanyu Han,Junmei Ding,Li Wan,Wanmeng Mu
Ginsenoside Rh2, a potential anticancer agent originally isolated from the medicinal plant Panax ginseng , has low natural abundance and is difficult to extract, making biosynthetic production a promising alternative. UDP-glycosyltransferases (UGTs) that specifically catalyze protopanaxadiol (PPD) glycosylation to produce Rh2 have been widely identified in plants and microorganisms. In this study, we report that Barbarea vulgaris UGT73C21 effectively catalyzes this reaction. The enzyme was expressed in Escherichia coli and purified to electrophoretic homogeneity via Ni 2 ⁺-affinity chromatography. It exhibited optimal activity at pH 8.0 (100 mM HEPES) and 45 °C. Mn 2 ⁺, Mg 2 ⁺, and Ca 2 ⁺ significantly enhanced enzyme activity, whereas other tested metal ions reduced it. The kinetic parameters K m , V max , k cat , and k cat / K m were determined as 231.92 μM, 5.68 μM min −1 , 0.053 s −1 , and 228 M −1 s −1 , respectively. In a reaction containing 0.2 mg/mL UGT73C21, 1 mM PPD, and 5 mM UDP-Glucose in HEPES buffer (pH 8.0), 0.55 mM Rh2 was produced within 1 h, corresponding to a 55% conversion rate. These results demonstrate that B. vulgaris UGT73C21 is an efficient biocatalyst for ginsenoside Rh2 biosynthesis.
✓ 已验证
产品关联
DOI
高影响因子
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