JOURNAL OF ETHNOPHARMACOLOGY
·
2023
·
IF 5.4
Wenxin Wang,Yinting Yu,Huixian Chen,Peijun Sun,Lujie Lu,Shuwei Yan,Xunhong Liu,Tulin Lu,Weidong Li,Jining Liu,Lihong Chen
Ethnopharmacological relevance Honey-processed licorice (HPL) is the roasted product of licorice. It is recorded in the “Shang Han Lun” that licorice has better protection on heart after honey-processed. However, researches regarding its protective effect on the heart and the distribution of HPL in vivo are still limited. Aim of the study To evaluate the cardio-protection of HPL and explore the law of ten main components distribution in vivo under physiological and pathological conditions for an attempt to clarify the pharmacological substance basis of HPL in treating arrhythmia . Materials and methods The adult zebrafish arrhythmia model was established by doxorubicin (DOX). Electrocardiogram (ECG) was used to detect the heart rate changes of zebrafish. SOD and MDA assays were used to evaluate oxidative stress levels in the myocardium. HE staining was used to observe the morphological change of myocardial tissues after HPL treatment. The UPLC-MS/MS was adapted to detect the content of ten main components of HPL in heart, liver, intestine, and brain under normal and heart injury conditions. Results Heart rate of zebrafish was decreased, the SOD activity was attenuated and MDA content was increased in myocardium after administration of DOX. Moreover, tissue vacuolation and inflammatory infiltration were detected in zebrafish myocardium induced by DOX. HPL could ameliorate heart injury and bradycardia induced by DOX to a certain extent by increasing SOD activity and reducing MDA content. In addition, the study of tissue distribution revealed that the content of liquiritin , isoliquiritin, and isoliquiritigenin in the heart was higher in the presence of arrhythmias than those in the normal condition. Under pathological conditions, the heart highly exposed to these three components could elicit anti-arrhythmic effects by regulating immunity and oxidation. Conclusion These findings indicate that the HPL is protective against heart injury induced by DOX, and its effect is associated with the alleviation of oxidative stress and tissue injury. And the cardioprotective effect of HPL under pathological conditions may be related to the high distribution of liquiritin, isoliquiritin, and isoliquiritigenin in heart tissue. This study provides an experimental basis for the cardioprotective effects and tissue distribution of HPL.
研究领域:
药理学
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心脏病学
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民族药理学
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斑马鱼模型
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氧化应激
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组织病理学
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组织分布
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DOI
PubMed
高影响因子
MOLECULES
·
2022
·Vol. 27
·期 14
·4657
·
IF 4.927
Mengxin Cao,Jiawei Zuo,Jian-Guo Yang,Chenyao Wu,Yongan Yang,Wenjian Tang,Lili Zhu
To understand that 18β-Glycyrrhetic acid 3-O-mono-β-D-glucuronide (GAMG) showed better pharmacological activity and drug-like properties than 18β-Glycyrrhizin (GL); a rapid and sensitive HPLC-MS/MS method was established for the simultaneous determination of GAMG and its metabolite 18β-Glycyrrhetinic acid (GA) in rat plasma and tissues after oral administration of GAMG or GL. This analytical method was validated by linearity, LLOQ, specificity, recovery rate, matrix effect, etc. After oral administration, GAMG exhibited excellentCmax(2377.57 ng/mL),Tmax(5 min) and AUC0-T(6625.54 mg/L*h), which was much higher than theCmax(346.03 ng/mL),Tmax(2.00 h) and AUC0-T(459.32 mg/L*h) of GL. Moreover, GAMG had wider and higher tissue distribution in the kidney, spleen, live, lung, brain, etc. These results indicated that oral GAMG can be rapidly and efficiently absorbed and be widely distributed in tissues to exert stronger and multiple pharmacological activities. This provided a physiological basis for guiding the pharmacodynamic study and clinical applications of GAMG.Keywords:GAMG;glycyrrhetic acid;glycyrrhizin;pharmacokinetics;pharmacodynamics;tissue distribution
研究领域:
药理学
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中药学
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产品关联
DOI
PubMed
高影响因子
Food & Function
·
2022
·Vol. 13
·期 7
·3931-3945
·
IF 6.317
Shan-Shan Zhang,Niu-Niu Zhang,Sen Guo,Shao-Jing Liu,Yu-Fei Hou,Shiming Li,Chi-Tang Ho,Nai-Sheng Bai
Twenty glycoside derivatives and nine flavonoids from the leaves of Pueraria (P. thomsonii) were isolated by column chromatography and characterized by nuclear magnetic resonance spectroscopy (NMR) and high performance liquid chromatography (HPLC). The contents of twenty glycosides and nine flavonoids from the extract of P. thomsonii leaf (PL) were 173.3 mg g−1 and 134.7 mg g−1, respectively. Two flavonoids with the highest content were robinin (49.28 mg g−1) and puerarin (42.87 mg g−1). Six flavonoids, i.e. puerarin, robinin, rutin, quercetin, quercitrin, and kaempferol showed more inhibitory effects against α-glucosidase than acarbose. PL could effectively increase the level of insulin, decrease the content of fasting blood glucose, reduce lipid accumulation in plasma, ameliorate oxidative injury and inflammation, and relieve liver and kidney damage in diabetic mice. Moreover, PL could increase intestinal probiotics to improve metabolic disorders caused by diabetes and decrease the level of Clostridium celatum to relieve inflammation. This study suggested that PL or its glycoside derivatives and flavonoids regulating glycolipid metabolism and inflammation levels might have the potential to be used to control type 2 diabetes.
研究领域:
药理学
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代谢组学
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微生物学
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DOI
PubMed
高影响因子
AAPS Journal
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2013
·Vol. 16
·期 1
·101-113
·
IF 4.386
Qiao Xue,Ji Shuai,Yu Si-wang,Lin Xiong-hao,Jin Hong-wei,Duan Yao-kai,Zhang Liang-ren,Guo De-an,Ye Min
Licorice has been shown to affect the activities of several cytochrome P450 enzymes. This study aims to identify the key constituents in licorice which may affect these activities. Bioactivity assay was combined with metabolic profiling to identify these compounds in several complex licorice extracts. Firstly, the inhibition potencies of 40 pure licorice compounds were tested using an liquid chromatography/tandem mass spectrometry cocktail method. Significant inhibitors of human P450 isozymes 1A2, 2C9, 2C19, 2D6, and 3A4 were then selected for examination of their structural features by molecular docking to determine their molecular interaction with several P450 isozymes. Based on the present in vitro inhibition findings, along with our previous in vivo metabolic studies and the prevalence of individual compounds in licorice extract, we identified several licorice constituents, viz ., liquiritigenin, isoliquiritigenin, together with seven isoprenylated flavonoids and arylcoumarins, which could be key components responsible for the herb–drug interaction between cytochrome P450 and licorice. In addition, hydrophilic flavonoid glycosides and saponins may be converted into these P450 inhibitors in vivo . These studies represent a comprehensive examination of the potential effects of licorice components on the metabolic activities of P450 enzymes.
研究领域:
药理学
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分析化学
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生物化学
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药学
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产品关联
DOI
PubMed
高影响因子
Analytical Methods
·
2014
·Vol. 6
·期 5
·1563-1568
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IF 1.938
Huang Yang,Li Kang,Shao Hui Kai,Liu Sheng Quan,Xiang Fei Jun
A method using molecularly imprinted solid-phase extraction combined with RP-HPLC-UV was developed for determination of liquiritin (LQR) in rat plasma after oral administration of Compound Liquorice Tablets (CLTs). To this end, molecularly imprinted polymers were prepared by in situ polymerization, using LQR as the template, acrylamide as the functional monomer, and ethylene glycol dimethacrylate as the crosslinker, whose solid-phase extraction properties for liquiritin were evaluated by HPLC-UV. The enrichment and extraction recovery were investigated in the study after the extraction procedure was optimized. The recovery was larger than 85.0% and the RSD was less than 10.0%. The calibration curve was expressed as y = 16 004x − 1.864 (r = 0.996) with a linear range of 0.007–1.683 μg mL−1. Besides, the Tmax was 0.5 h for liquiritin and the Cmax was 0.8 μg mL−1 after oral administration of compound liquorice tablets. In addition, the pharmacokinetic parameters were calculated using a two-compartment model. The results indicated that the monolithic polymer pipette presented a good extraction efficiency for liquiritin. At the same time, the results indicated that the index components could basically reveal the pharmacokinetic behavior. This study was aimed to explore an approach that could be applied to promulgate the pharmacokinetics and provide more information for clinical applications.
研究领域:
药理学
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分析化学
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生物医学工程
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产品关联
DOI
高影响因子
JOURNAL OF MICROENCAPSULATION
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2018
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IF 1.793
Chang Liu,Zijun Zhou,Ye Chen,Ju Liu,Yang Wang,Hongsheng Liu
Scavenger receptor class B type 1 (SR-B1) is over-expressed in tumour cells where it mediates the uptake of drug payload of reconstituted high density lipoprotein (rHDL) via the process of reverse cholesterol transport. In this study, rHDL was prepared to determine its function as a drug delivery carrier for targeting hepatocellular carcinoma by incorporating the anti-tumour drug garcinia glycosides (GG) into rHDL to yield rHDL/GG nano-complexes. Structural analysis indicated that the rHDL/GG nano-complex was similar to HDL in size. HepG2 cells treated with fluorescent-labelled rHDL/GG exhibited a time-dependent increase in cell death. Further experiment in which HepG2 cells were treated with rHDL/GG plus plasma-derived HDL showed reduction in cell death compared to treatment with rHDL/GG alone, suggesting that plasma-derived HDL compete with rHDL/GG for binding to the SR-B1 on the cell. We concluded that rHDL could not only incorporate GG but could also serve as a carrier, targeting the drug to HepG2 cells via SR-B1.
研究领域:
药理学
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肿瘤学
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纳米技术
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分子生物学
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产品关联
DOI
PubMed
高影响因子
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
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2021
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IF 3.232
Wen Weng,Qilong Wang,Chunmei Wei,Michael Adu-Frimpong,Elmurat Toreniyazov,Hao Ji,Jiangnan Yu,Ximing Xu
Objectives Liquiritin, as one of the main flavonoids in Glycyrrhiza, exhibits extensive pharmacological effects, such as the anti-oxidant, anti-inflammatory, anti-tumor and so on. Herein, the aqueous solubility and oral bioavailability of liquiritin was purposely enhanced via the preparation of the mixed micelles.Methods The liquiritin-loaded micelles (LLM) were fabricated via thin-film dispersion method. The optimal LLM formulation was evaluated through physical properties including particle size (PS), encapsulation efficiency (EE) and drug loading (DL). In vitro accumulate release as well as in vivo pharmacokinetics were also evaluated. Moreover, the hypolipidemic activity of LLM was observed in the hyperlipidemia mice model.Results The LLM exhibited a homogenous spherical shape with small mean PS, good stability and high encapsulation efficiency. The accumulate release rates in vitro of the LLM were obviously higher than free liquiritin. The oral bioavailability of the formulation was heightened by 3.98 times in comparison with the free liquiritin. More importantly, LLM increased the hypolipidemic and effect of alleviating lipid metabolism disorder in hepatocytes of liquiritin in hyperlipidemia mice model.Conclusions Collectively, the improved solubility of liquiritin in water coupled with its enhanced oral bioavailability and concomitant hypolipidemic activity could be attributed to the incorporation of the drug into the mixed micelles.
研究领域:
药剂学
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药理学
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药物递送系统
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产品关联
DOI
PubMed
高影响因子
Plant Signaling & Behavior
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2020
·
IF 1.671
Zhi-Qiang Yan,Jing Tan,Kai Guo,Lun-Guang Yao
As the main active ingredient of the traditional Chinese medicine Glycyrrhiza uralensis Fisch, liquiritin has multiple biological activities, including anti-inflammatory, antihepatotoxicity, immune regulation, anti-virus and anti-cancer. In addition, liquiritin has been recognized as an allelochemical that displays markedly inhibitory effects on the growth of target plants, G. uralensis and lettuce. However, its phytotoxic mechanism remains unknown. In the present study, the mode of action of liquiritin against root growth of lettuce seedling was researched. After treatments with liquiritin, the cell division in root tips of lettuce seedlings was partly arrested, and the cell viability and root vitality were obviously lost. At the same time, overproduction of reactive oxygen species (ROS), malondialdehyde (MDA) and proline (Pro) in lettuce seedlings were induced by liquiritin. The results indicated that the phytotoxic effects of liquiritin was probably dependent on the induction of ROS overproduction, resulting in membrane lipids peroxidation following with cell death and mitosis process disorder.
研究领域:
植物学
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植物生理学
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植物化学
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毒理学
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DOI
PubMed
高影响因子
FOOD RESEARCH INTERNATIONAL
·
2023
·
IF 8.1
Qifan Wang,Haolong Chang,Peng Deng,Zhiyong He,Qiuming Chen,Zhaojun Wang,Fang Qin,Fatih Oz,Emel Oz,Jie Chen,Maomao Zeng
The inhibitory effects of liquiritigenin, liquiritin and glycyrrhizic acid against the hazards during the preparation of thermal reaction beef flavoring were investigated using high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS). Liquiritigenin(1.5 mM) inhibited N ε -carboxymethyl-L-lysine and N ε -carboxyethyl-L-lysine by up to 38.69% and 61.27%, respectively; 1.5 mM liquiritin inhibited 4-methylimidazole by up to 48.28%; and 1.5 mM liquiritigenin and 1.0 mM liquiritin inhibited hydroxymethylfurfural by up to 61.20% and 59.31%, respectively. The results of the model system showed that the inhibitory effect of the 3 inhibitors could be extended to other thermal reaction flavoring systems. The 3 inhibitors can effectively block key intermediates in beef flavoring, and liquiritigenin can inhibit up to 22.97% of glyoxal and 22.89% of methylglyoxal. In addition, liquiritigenin and liquiritin can directly eliminate up to 25.87% and 21.01% of methylglyoxal by addition and other means. Free radicals in the simultaneous formation model system were measured using electron spin resonance (ESR), and the results showed that liquiritigenin, liquiritin and glycyrrhizic acid could scavenge free radicals in the system in a dose-dependent manner, with scavenging rates of up to 44.88%∼57.09%. Therefore, the inhibitory effects of the 3 inhibitors can be attributed to the intermediate blocking and free radical scavenging pathways.
研究领域:
食品科学
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化学
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药理学
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DOI
PubMed
高影响因子
Journal of Pharmaceutical Analysis
·
2022
·
IF 14.026
Xiaojuan Jiang,Yihua Lin,Yunlong Wu,Caixia Yuan,Xuli Lang,Jiayun Chen,Chunyan Zhu,Xinyi Yang,Yu Huang,Hao Wang,Caisheng Wu
Glycyrrhizae Radix et Rhizoma, a traditional Chinese medicine also known as Gan Cao (GC), is frequently included in clinical prescriptions for the treatment of pneumonia. However, the pharmacological components of GC for pneumonia treatment are rarely explored. Gan An He Ji oral liquid (GAHJ) has a simple composition and contains GC liquid extracts and paregoric, and has been used clinically for many years. Therefore, GAHJ was selected as a compound preparation for the study of GC in the treatment of pneumonia. We conducted an in vivo study of patients with pneumonia undergoing GAHJ treatments for three days. Using the intelligent mass spectrometry data-processing technologies to analyze the metabolism of GC in vivo, we obtained 168 related components of GC in humans, consisting of 24 prototype components and 144 metabolites, with 135 compounds screened in plasma and 82 in urine. After analysis of the metabolic transformation relationship and relative exposure, six components (liquiritin, liquiritigenin, glycyrrhizin, glycyrrhetinic acid, daidzin, and formononetin) were selected as potential effective components. The experimental results based on two animal pneumonia models and the inflammatory cell model showed that the mixture of these six components was effective in the treatment of pneumonia and lung injury and could effectively downregulate the level of inducible nitric oxide synthase (iNOS). Interestingly, glycyrrhetinic acid exhibited the strongest inhibition on iNOS and the highest exposure in vivo. The following molecular dynamic simulations indicated a strong bond between glycyrrhetinic acid and iNOS. Thus, the current study provides a pharmaceutical basis for GC and reveals the possible corresponding mechanisms in pneumonia treatment.
研究领域:
药理学
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中药学
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质谱学
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炎症
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分子动力学
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产品关联
DOI
PubMed
高影响因子
CHEMICAL & PHARMACEUTICAL BULLETIN
·
2023
·Vol. 71
·期 4
·269-276
·
IF 1.7
Xiaoran Ning,Yanhui Ni,Jingjing Cao,Huaxing Zhang
Rheumatoid arthritis (RA) is a common autoimmune disease with increased cardiovascular disease risk. Liquiritigenin (LG) is a triterpene with anti-inflammatory properties. Our study aimed to explore the effect of LG on RA and the cardiac complication. Collagen-induced arthritis (CIA) mice with LG treatment exhibited obvious alleviation in histopathological changes, accompanied by the decreased expression of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6, and IL-17A in synovium and serum. LG attenuated cartilage destruction by reducing matrix metalloproteinase (MMP)-3 and MMP-13 expression in the synovium of CIA mice. The echocardiography results proved the alleviation of cardiac dysfunction in CIA mice. The electrocardiogram, biochemical, and histochemical analysis proved the cardioprotection effect of LG against RA. The decreased expression of inflammatory factors (TNF-α, IL-1β, and IL-6) and fibrotic markers (fibronectin, Collagen I, and Collagen III) in cardiac tissues of CIA mice further corroborated the attenuation of myocardial inflammation and fibrosis by LG. Mechanistic studies showed that LG could inhibit transforming growth factor β-1 (TGF-β1) and phos-Smad2/3 expression in cardiac tissues of CIA mice. Our study suggested that LG could relieve RA and its cardiac complication probably by inhibiting the TGF-β1/Smad2/3 pathway. All these suggested that LG might be a potential candidate for RA and its cardiac complication therapy.
研究领域:
免疫学
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风湿病学
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心脏病学
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药理学
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产品关联
DOI
PubMed
高影响因子
PHYTOMEDICINE
·
2023
·
IF 7.9
Yinhuang Gao,Ke Ma,Zhibo Zhu,Yan Zhang,Qiong Zhou,Jing Wang,Xiaowen Guo,Liuting Luo,Haitao Wang,Kang Peng,Menghua Liu
Background Vascular dementia (VaD) is one of the most common clinical syndromes of progressive neurocognitive dysfunction with uncertain mechanisms. Modified Erchen decoction (MECD), developed from “Erchen decoction (ECD)” recorded in “Taiping Huimin Heji Jufang”, showed a good effect in the treatment of VaD. However, its therapeutic mechanism is still unclear. Purpose This study aimed to elucidate the multi-target mechanisms of MECD against VaD in vivo and in vitro . Methods VaD model was established by two-vessel obstruction (2-VO) in Sprague-Dawley rats. Six groups, including the control, 2-VO operation, MECD treatment (2.5, 5.0 and 10.0 g kg −1 d −1 ), donepezil hydrochloride (positive control, 0.45 g kg −1 d −1 ) were designed in the whole experiment. After oral administration for 4 weeks, the effects of MECD were verified by behavioral experiments, histological observation, and biochemical index analysis. The chemical profiling of MECD was performed by UHPLC-Orbitrap Fusion-HRMS, and a "compound-target-pathway" multivariate network was constructed to validate and elucidate its pharmacological mechanisms. Results Compared with 2-VO group, MECD treatment significantly alleviated anxiety and improved spatial memory in VaD rats according to the open field test (OFT) and Y-maze test. A significant increase in neuron number was observed from hematoxylin and eosin (H&E) stained images in cornu ammonis 1 (CA1) of the hippocampal region after MECD treatment. On the one hand, MECD reduced the plasma levels of triglyceride (TG), low-density lipoprotein (LDL), malondialdehyde (MDA), and amyloid-beta 42 (Aβ42), and inhibited mRNA expression of interleukin-1 beta ( Il-1β ) and Il-6 in the hippocampus. On the other hand, superoxide dismutase (SOD) and total antioxidant capacity (T-AOC) were significantly increased after treatment with MECD. Moreover, MECD reduced the mRNA expression and protein expression of janus kinase 2 (JAK2), signal transducer and activator of transcription 3 (STAT3), c-Jun N-terminal kinase (JNK), and BCL2-associated X (BAX) in the brain of 2-VO rats. Furthermore, 71 compounds were identified from the extract of MECD. Among them, liquiritin and isochlorogenic acid C gave inhibiting effects on the mRNA expression of Jnk . In addition, liquiritin and hesperetin were conformed with the inhibition of Jak2 transcription level in vitro experiments. Conclusion MECD has demonstrated a significant amelioration effect on cognitive dysfunction in VaD rats via JAK2/STAT3 and JNK/BAX signaling pathways , which represents an innovative insight into the “activate blood and eliminate phlegm” theory.
研究领域:
药理学
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神经科学
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中医药
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分子生物学
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行为科学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）