Chinese Journal of Integrative Medicine
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2017
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IF 1.116
Wei Ping,Tang Qing-fa,Huo Hui-ling,Chen Fei-long,Song Shuai,Xing Xue-feng,Luo Jia-bo
Objective To investigate the pharmacokinetic characteristics of three phenylpropanoids (cinnamic acid, cinnamic alcohol and coumarin) in Ramulus Cinnamomi (GZ) and Ramulus Cinnamomi-Ephedrae Herba (MH) herb-couple (GZMH). Methods Twelve male Sprague-Dawley rats were randomly and equally divided into the GZ and GZMH herb-couple groups. Blood samples were collected at 0, 0.08, 0.25, 0.5, 0.75, 1.5, 3, 4, 6, 8, 12, 24, 36 and 48 h after oral administration. The three phenylpropanoids in rat plasma were quantified using an ultra-performance liquid-chromatography with tandem mass spectrometry (UPLC-MS/MS) method for pharmacokinetic study. Results In GZMH group, the area under the curve (AUC), mean retention time (MRT) of cinnamic acid and coumarin were increased significantly ( P <0.01, respectively), and biological half-life (t 1/2z ) was obviously shorter ( P <0.05) compared with the GZ group. There were no significant differences in the mean retention time from 0 to ∞ (MRT 0-∞ ), the peak concentration (C max ), the time to peak (T max ) and t 1/2z , except for AUC and MRT 0-t (the mean retention time from 0 to t) of cinnamic alcohol in the GZMH group by comparison to the GZ group ( P <0.01, respectively). The AUC, MRT (both P <0.01) and t 1/2z ( P <0.05) of coumarin were increased significantly, while C max , and T max were decreased slightly by comparison to the GZ group ( P >0.05). Conclusions There were statistically significant differences in some pharmacokinetic parameters of the three compounds between GZ and GZMH groups, which meant that MH could affect the absorption and elimination of the three compounds.
研究领域:
中药学
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药理学
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分析化学
✓ 已验证
DOI
PubMed
高影响因子
Journal of Food Measurement and Characterization
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2024
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IF 2.9
Zhou Zhen,Liu Shengkai,Cui Liying,Liu Zhongkai,Li Xiaoyu,Liu Zhiguo,Fu Yujie
This study explored the ultrasonic-microwave synergistic extraction technique for obtaining cinnamaldehyde and cinnamic acid from cinnamon twigs, and determined the most favorable extraction conditions. The optimization of extraction parameters, including extraction time, ethanol concentration, liquid-to-solid ratio, and microwave power, was achieved through single-factor experiments and the response surface method. The results of the significance analysis indicated that ethanol concentration and extraction power were the two primary factors affecting the extraction rates of cinnamaldehyde and cinnamic acid. Under the optimal conditions—600 W microwave power, 75% ethanol concentration, a liquid-to-solid ratio of 1:15, and a 20-min extraction time——the extraction efficiency of cinnamaldehyde and cinnamic acid was significantly improved compared to traditional methods. Moreover, the use of the ultrasonic-microwave synergistic extraction technique demonstrated higher efficiency and lower environmental impact due to reduced waste production. The study also revealed that cinnamaldehyde and cinnamic acid in cinnamon twigs exhibited strong polarity characteristics and microwave absorption capacity, contributing to enhanced cell disruption and increased natural product release. These findings provide a robust basis for the development of an efficient and environmentally friendly extraction process for these valuable bioactive compounds.
研究领域:
化学工程
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药学
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环境科学
✓ 已验证
产品关联
DOI
高影响因子
Frontiers in Pharmacology
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2025
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IF 4.8
Yuhang Xu,Jing Li,Mengyao Cui,Xiaoliang Li,Hongyan Zhai,Deling Wu,Xiaoqin Chu
Introduction: Cinnamomi Ramulus (CR) is the dried bark of Cinnamomum cassia Presl, Lauraceae. Puerariae Lobatae Radix (PLR) is the dried root of the Pueraria lobata (Wild.) Ohwi, Leguminosae. This Chinese herb couple come from the classic formula “Gui Zhi Ge Gen Tang,” which is included in the TCM classic “Treatise on Febrile Diseases.” Our previous studies have found that CR related herbal compound and PLR related herbal compound are useful in improving type 2 diabetes mellitus (T2DM), which is expected to be an antidiabetic candidate with fewer side effects. However the mechanism of action of CR-PLR on T2DM has not yet been fully elucidated.Methods: The decoction of CR-PLR was prepared by aqueous extraction method and the composition of it was analyzed using UPLC-Q-TOF-MS and HPLC. The T2DM model was established by intraperitoneal injection of streptozotocin, and the groups of drug administration were metformin, CR, PLR and CR-PLR groups, with continuous gastric gavage for 6 weeks, and the serological indexes were detected by ELISA. The abundance of rats’ gut flora was detected by 16s rDNA sequencing, and changes in the content of short-chain fatty acids (SCFAs) in feces of rats were detected by GC-MS; and the expression of G protein-coupled receptor43 (GPR43) and glucagon-like peptide-1 (GLP-1) proteins in colonic tissues of rats were detected by Western Blot. The pharmacokinetic behavior of CR-PLR was investigated in both normal and T2DM model rats. Caco-2/HT29 co-culture cell model was established in vitro, transepithelial electrical resistance (TEER) and ALP activity of epithelial cells were measured to evaluate cell model integrity and cell polarization, Alcian blue staining was used to verify the presence of mucus production, and CCK-8 was used to screen drug safe concentration. The bidirectional transport of puerarin was studied to investigate the transport mechanism of puerarin and the effect of leuric acid on puerarin transport.Results and discussion: The results indicated that CR-PLR can stimulate intestinal flora, increase the content of SCFAs, activate intestinal GPR43 protein, and promote the secretion of GLP-1 in intestinal L cells, which plays a therapeutic role in the treatment of T2DM. Additionally, cytology and pharmacokinetics experiments have proved that cinnamic acid (CA) can enhance the absorption and transport of puerarin (PUR) by inhibiting the efflux effects mediated by P-gp and MRP efflux transporters. The present study exhibites the scientific and reasonable menaning of this novel Chinese herb couple treating T2DM from the perspecives of pharmacodynamics and pharmacokinetics.
研究领域:
中药学
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代谢病研究
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药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2023
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IF 5.4
Wei Jia,Xiwen He,Wenhui Jin,Jinping Gu,Siyu Yu,Jianlin He,Zhiwei Yi,Bing Cai,Huiyuan Gao,Longhe Yang
Ethnopharmacological relevance Ramulus Cinnamomi , the dried twig of Cinnamomum cassia (L.) J.Presl., is a traditional Chinese medicine (TCM) with anti-inflammatory effects. The medicinal functions of Ramulus Cinnamomi essential oil (RCEO) have been confirmed, although the potential mechanisms by which RCEO exerts its anti-inflammatory effects have not been fully elucidated. Aim of the study To investigate whether N -acylethanolamine acid amidase (NAAA) mediates the anti-inflammatory effects of RCEO. Materials and methods RCEO was extracted by steam distillation of Ramulus Cinnamomi , and NAAA activity was detected using HEK293 cells overexpressing NAAA. N -Palmitoylethanolamide (PEA) and N -oleoylethanolamide (OEA), both of which are NAAA endogenous substrates, were detected by liquid chromatography with tandem mass spectrometry (HPLC-MS/MS). The anti-inflammatory effects of RCEO were analyzed in lipopolysaccharide (LPS)-stimulated RAW264.7 cells, and the cell viability was measured with a Cell Counting Kit-8 (CCK-8) kit. The nitric oxide (NO) in the cell supernatant was measured using the Griess method. The level of tumor necrosis factor-α (TNF-α) in the RAW264.7 cell supernatant was determined using an enzyme-linked immunosorbent assay (ELISA) kit. The chemical composition of RCEO was assessed by gas chromatography-mass spectroscopy (GC-MS). The molecular docking study for (E)- cinnamaldehyde and NAAA was performed by using Discovery Studio 2019 software (DS2019). Results We established a cell model for evaluating NAAA activity, and we found that RCEO inhibited the NAAA activity with an IC 50 of 5.64 ± 0.62 μg/mL. RCEO significantly elevated PEA and OEA levels in NAAA-overexpressing HEK293 cells, suggesting that RCEO might prevent the degradation of cellular PEA and OEA by inhibiting the NAAA activity in NAAA-overexpressing HEK293 cells. In addition, RCEO also decreased NO and TNF-α cytokines in lipopolysaccharide (LPS)-stimulated macrophages. Interestingly, the GC-MS assay revealed that more than 93 components were identified in RCEO, of which (E)- cinnamaldehyde accounted for 64.88%. Further experiments showed that (E)- cinnamaldehyde and O -methoxycinnamaldehyde inhibited NAAA activity with an IC 50 of 3.21 ± 0.03 and 9.62 ± 0.30 μg/mL, respectively, which may represent key components of RCEO that inhibit NAAA activity. Meanwhile, docking assays revealed that (E)- cinnamaldehyde occupies the catalytic cavity of NAAA and engages in a hydrogen bond interaction with the TRP181 and hydrophobic-related interactions with LEU152 of human NAAA. Conclusions RCEO showed anti-inflammatory effects by inhibiting NAAA activity and elevating cellular PEA and OEA levels in NAAA-overexpressing HEK293 cells. (E) -cinnamaldehyde and O- methoxycinnamaldehyde, two components in RCEO, were identified as the main contributors of the anti-inflammatory effects of RCEO by modulating cellular PEA levels through NAAA inhibition.
研究领域:
药理学
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免疫学
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细胞生物学
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生物化学
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中医
✓ 已验证
产品关联
DOI
PubMed
高影响因子
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