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FITOTERAPIA · 2023 · IF 3.4

Investigations of the gingerol oil colon targeting pellets for the treatment of ulcerative colitis

Yajing Wang,Tao Zhang,Jie Liu,Xianfeng Huang,Xiaojing Yan

The clinical treatment of ulcerative colitis (UC) faces great challenges due to lifetime medication. In this study, Gingerol oil was extracted and purified by the process easily scale-up and cost effective, with productivity 2.72 ± 0.38% ( w /w, versus crude drugs). The quality control of gingerol oil was fully established by HPLC fingerprint with 4 common peaks identified as 6-gingerol, 8-gingerol, 6-shogaol and 10-gingerol. The similarities of 6 batches of gingerol oil are within 0.931–0.999. The protective effects of gingerol oil are equivalent to or even stronger than that of 6-gingerol on inflammation and oxidative stress of HT-29 cells induced by lipopolysaccharide and H 2 O 2 , as well as on UC in mice caused by dextran sulfate sodium salt (DSS). Our research conclusions coincide well with the holistic view of Traditional Chinese Medicine and network pharmacology . The absorption kinetics of gingerol oil were conducted using the in situ intestinal perfusion in rats and comparable absorption were achieved in the jejunum , ileum and colon segments within 2 h. Thus, gingerol oil colon targeting pellets were prepared by extrusion-spherization technique. The cumulative dissolution behaviors and mechanisms were observed and analyzed by fitting to dissolution model. Our studies provided reliable theoretical and experimental support for the gingerol oil as reliable therapeutic choice of UC.

CAS / MDL: 599-79-1 93572-42-0
研究领域: 药理学 · 胃肠病学 · 传统中药 · 药物递送系统
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PHYTOCHEMICAL ANALYSIS · 2024 · IF 3

Analytical quality by design based on knowledge organization: A case study of developing an ultrahigh-performance liquid chromatography method for the detection of phenolic compounds

Yanni Tai,Mintong Zhao,Feng Ding,Gelin Wu,Haibin Qu,Ping Gong,Yongjian Xie,Peng Zhou,Xingchu Gong

Introduction Despite numerous successful cases, there are still some challenges in using analytical quality by design (AQbD) for the development of analytical methods. Knowledge organization helps to enhance the objectivity of risk assessment, reduce the number of preliminary exploratory experiments, identify potential critical method parameters (CMPs) and their scope. Objective In the present study, we aimed to develop a simple, rapid, and robust analytical method for detecting phenolic compounds in Xiaochaihu capsule intermediates utilizing knowledge organization. Methods Knowledge organization and AQbD were combined to obtain the initial analytical conditions through knowledge collection, extraction, reorganization, and analysis. The quantitative relationship between critical method attributes (CMAs) and CMPs was then established by a definitive screening design. The method operable design region was calculated using an exhaustive Monte Carlo approach based on the probability of reaching the standard. Robustness investigation and methodological validation were finally performed. Results Analytical target profiles, CMAs, potential CMPs, and initial analytical conditions were initially identified, and the optimized ranges of operating parameters were obtained. A UHPLC method was successfully established for the analysis of phenolic compounds in ginger–ginger pinellia percolate, and the method validation outcomes were also satisfactory. Conclusion The developed method can be a reliable means to detect the phenolic compounds of Xiaochaihu capsule intermediates. Knowledge organization provides a new approach for making better use of prior knowledge, significantly enhancing the efficiency of analytical method development. The approach is versatile and can be similarly applied to the development of other methods.

研究领域: 分析化学 · 药学 · 化学计量学 · 质量保证
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Processes · 2025 ·Vol. 13 ·期 7 ·2149 · IF 2.8

Optimized High-Pressure Ultrasonic-Microwave-Assisted Extraction of Gingerol from Ginger: Process Design and Performance Evaluation

Yang Zhang,Siyi Yang,Wensi Li,Xiaoyan Li,Xiangqin Lai,Xiang Li,Wuwan Xiong,Bo Zhang

This study employed high-pressure ultrasonic-microwave-assisted extraction (HP-UMAE) to extract gingerols from ginger. The extraction yield and total polyphenol content of the extracts were determined. Their antioxidant activity was assessed by DPPH and ABTS radical scavenging assays, and compared with extracts obtained by leaching extraction, reflux extraction, ultrasonic-assisted extraction (UAE), microwave-assisted extraction (MAE), and ultrasonic-microwave-assisted extraction (UMAE). The results demonstrated that HP-UMAE achieved the highest extraction yield and the strongest ABTS radical scavenging activity among the evaluated methods. Furthermore, HP-UMAE extracts exhibited the highest concentrations of key gingerol constituents: 6-gingerol (14.29 mg/L), 8-gingerol (0.38 mg/L), 10-gingerol (1.95 mg/L), and 6-shogaol (4.32 mg/L). This enhanced efficacy is attributed to the synergistic combination of ultrasonic cavitation and microwave-induced thermal effects under elevated pressure. This synergy creates conditions promoting cellular wall disruption, facilitating the release of intracellular components, while concurrently enhancing solvent penetration and gingerol solubility. Scanning electron microscopy (SEM) analysis confirmed the significant structural damage inflicted on ginger cell walls following HP-UMAE treatment. The process parameters for HP-UMAE were optimized using single-factor experiments. The optimal extraction conditions were determined as follows: microwave power 800 W, ultrasonic power 1000 W, liquid-to-solid ratio 55:1, and temperature 100 °C (corresponding pressure 2 MPa). Under these optimized parameters, the extraction yield and ABTS radical scavenging rate reached their peak performance, yielding values of 4.52% and 43.23%, respectively.

研究领域: 食品科学 · 植物化学 · 分析化学 · 生物技术
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2020 · IF 2.734

Improved oral bioavailability and target delivery of 6-shogaol via vitamin E TPGS-modified liposomes: Preparation, in-vitro and in-vivo characterizations

Rui Bao,Qi-Long Wang,Ran Li,Michael Adu-Frimpong,Elmurat Toreniyazov,Hao Ji,Xi-Ming Xu,Jiang-Nan Yu

6-Shogaol is one component of ginger, which has been described to possess various health-promoting effects including anticancer, antiinflammatory, antioxidant and antiatherogenic. However, poor water solubility has limited the aforementioned health benefits and clinical applications of the drug. Herein, the aforementioned drawback was circumvented by the preparation of 6-shogaol-loaded liposome through thin-film dispersion method with TPGS as the carrier, in comparison with 6-shogaol liposome and free 6-shogaol. Appropriate indices were used for the characterization of the developed liposomes viz., particle size (PS), zeta potential (Z-potential), polydispersity index (PDI), entrapment efficiency (EE) and loading capacity (LC) while their morphologies were observed under the transmission electron microscopy (TEM). In-vitro dissolution investigation showed a substantial improvement in the accumulative release rates of liposomes comparable to the free 6-shogaol. The TPGS-modified 6-shogaol and 6-shogaol liposomes had oral relative bioavailability (RBA) of 580.04% and 281.55%, respectively, with improved t 1/2 , MRT, C max , AUC 0-t and T max . Pertinently, the TPGS coated 6-shogaol liposome may enhance the targeting of the drug to the brain. Therefore, the TPGS coated 6-shogaol liposome could potentially improve oral bioavailability of lipophilic drug in-vivo . More importantly, the results of tissue distribution investigation suggest that TPGS coated 6-shogaol liposome may act as promising carrier for brain delivery in future.

研究领域: 药剂学 · 药理学 · 纳米技术 · 药物递送系统
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Pharmaceutics · 2019 ·Vol. 11 ·期 3 ·107 · IF 4.773

Enhanced Oral Bioavailability, Anti-Tumor Activity and Hepatoprotective Effect of 6-Shogaol Loaded in a Type of Novel Micelles of Polyethylene Glycol and Linoleic Acid Conjugate

Huiyun Zhang,Qilong Wang,Congyong Sun,Yuan Zhu,Qiuxuan Yang,Qiuyu Wei,Jiaxin Chen,Wenwen Deng,Michael Adu-Frimpong,Jiangnan Yu,Ximing Xu

6-shogaol is a promising anti-cancer and anti-inflammatory agent. However, the treatment effectiveness of 6-shogaol is limited by poor water solubility, poor oral absorption and rapid metabolism. Herein, 6-shogaol loaded in micelles (SMs) were designed to improve 6-shogaol’s solubility and bioavailability. The micelles of a PEG derivative of linoleic acid (mPEG2k-LA) were prepared by the nanoprecipitation method with a particle size of 76.8 nm, and entrapment of 81.6 %. Intriguingly, SMs showed a slower release in phosphate buffer saline (PBS) (pH = 7.4) compared to free 6-shogaol while its oral bioavailability increased by 3.2–fold in vivo. More importantly, the in vitro cytotoxic effect in HepG2 cells of SMs was significantly higher than free 6-shogaol. Furthermore, SMs could significantly improve the tissue distribution of 6-shogaol, especially liver and brain. Finally, SMs showed a better hepatoprotective effect against carbon tetrachloride (CCl4)-induced hepatic injury in vivo than free 6-shogaol. These results suggest that the novel micelles could potentiate the activities of 6-shogaol in cancer treatment and hepatoprotection.Keywords:6-shogaol;cytotoxic effect;HepG2 cells;micelles;hepatoprotection

CAS / MDL: 555-66-8 23513-13-5
研究领域: 药学 · 肿瘤学 · 肝病学
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JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE · 2023 ·Vol. 103 ·期 6 ·2838-2847 · IF 4.1

Inhibition of benzo[a]pyrene formation in charcoal-grilled pork sausages by ginger and its key compounds

Xiaomin Zhang,Gaofeng Hu,Chaoyang Xu,Wen Nie,Kezhou Cai,Hongmei Fang,Baocai Xu

BACKGROUND Ginger and its extracts have been frequently used in food processing and pharmaceuticals. However, the influence of ginger and its key compounds on benzo[a]pyrene (BaP) production in meat processing has not been investigated. The purpose of this study was to explore the effect of application of ginger and its important active ingredients on BaP formation and the mechanism of inhibiting BaP formation in charcoal-grilled pork sausages. RESULTS The DPPH scavenging (23.59–59.67%) activity and the inhibition rate of BaP (42.1–68.9%) were significantly increased ( P < 0.05) with increasing ginger addition. The active components extracted by supercritical carbon dioxide from ginger were identified by gas chromatography–mass spectrometry and 14 representative compounds (four terpenes, two alcohols, two aldehydes, four phenols and two other compounds, totaling 77.57% of the detected compounds) were selected. The phenolic compounds (eugenol, 6-gingerol, 6-paradol and 6-shogaol, accounting for 29.73% of the total composition) in ginger played a key role and had the strongest inhibitory effect on BaP (61.2–68.2%), whereas four other kinds of compound showed obviously feeble inhibitory activity (6.47–17.9%). Charcoal-grilled sausages with phenolic substances had lower values of thiobarbituric acid-reactive substances, carbonyl and diene (three classic indicators of lipid oxidation) ( P < 0.05). CONCLUSION Ginger and its key compounds could effectively inhibit the formation of BaP in charcoal-grilled pork sausages. Phenolic compounds make the strongest contribution to the inhibition of Bap formation, and the inhibitory mechanism was related to the inhibition of lipid oxidation. © 2023 Society of Chemical Industry.

研究领域: 食品科学 · 毒理学 · 化学
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