JOURNAL OF SEPARATION SCIENCE
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2022
·Vol. 45
·期 5
·1051-1058
·
IF 3.614
Chunying Song,Dongping Yu,Gaowa Jin,Junjie Ding,Han Zhou,Zhimou Guo,Xinmiao Liang
Ephedrae Herba is one of the most commonly used herbal medicines, and it has been shown that most of the clinical efficacy for cold and asthma is exerted by its alkaloidal components. A simple and sensitive high-performance liquid chromatography method was developed using a perfluorooctyl column for the simultaneous determination of five alkaloids (norephedrine, norpseudoephedrine, ephedrine, pseudoephedrine, and methylephedrine) in Ephedrae Herba . The mobile phase comprising acetonitrile and 15 mM ammonium trifluoroacetate was used to elute the targets in isocratic elution mode. The method was validated for linearity ( R 2 > 0.999), repeatability, intraday and interday precision, recoveries with trueness (93.87–110.99%), limits of detection (5.35–5.76 µg/mL), and limits of quantification (20 µg/mL). The quantitative results revealed that the developed method was precise and accurate. Then it was successfully applied to determine the difference in the contents of three batches of Ephedrae Herba from three pharmaceutical companies.
研究领域:
药学
·
分析化学
✓ 已验证
DOI
高影响因子
Journal of Functional Foods
·
2020
·
IF 3.701
Xiaomeng Xu,Rong Liang,Dongmei Li,Chengyao Jiang,Songyi Lin
To investigate the dose-effect relationship of sea cucumber peptides on memory function improvement, animal experiments, behavioral experiments, ACh content, AChE activity, hippocampal morphology, and protein modifications were detected. Sea cucumber peptides (650 mg/kg, 1300 mg/kg, 2600 mg/kg body weight) and piracetam (400 mg/kg) were gavaged into the mice. Scopolamine (5 mg/kg) were administered intraperitoneally to mice. In behavioral experiments, the escape latency and the shocked time of sea cucumber peptides (SCP) groups were significantly reduced ( P < 0.05). Determination of biochemical indicators found that ACh content and AChE activity of SCP groups were increased ( P < 0.05). The number of neurons in the hippocampus of SCP groups were larger, arranged neatly and intact. The histone acetyltransferases activity of SCP groups may be lower than that of the Scopolamine group, so the acetylation level is down-regulated and approached to dynamic equilibrium, thereby the memory activity of mice was improved.
研究领域:
神经科学
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药理学
·
分子生物学
✓ 已验证
产品关联
DOI
高影响因子
DRUG METABOLISM AND DISPOSITION
·
2020
·Vol. 48
·期 5
·345-352
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IF 3.231
Xiaohua Zhao,Hong Ma,Qiusha Pan,Haiyi Wang,Xingkai Qian,Peifang Song,Liwei Zou,Mingqing Mao,Shuyue Xia,Guangbo Ge,Ling Yang
Doxophylline (DOXO) and theophylline are widely used as bronchodilators for treating asthma and chronic obstructive pulmonary disease, and DOXO has a better safety profile than theophylline. How DOXO’s metabolism and disposition affect its antiasthmatic efficacy and safety remains to be explored. In this study, the metabolites of DOXO were characterized. A total of nine metabolites of DOXO were identified in vitro using liver microsomes from human and four other animal species. Among them, six metabolites were reported for the first time. The top three metabolites were theophylline acetaldehyde (M1), theophylline-7-acetic acid (M2), and etophylline (M4). A comparative analysis of DOXO metabolism in human using liver microsomes, S9 fraction, and plasma samples demonstrated the following: 1) The metabolism of DOXO began with a cytochrome P450 (P450)–mediated, rate-limiting step at the C ring and produced M1, the most abundant metabolite in human liver microsomes. However, in human plasma, the M1 production was rather low. 2) M1 was further converted to M2 and M4, the end products of DOXO metabolism in vivo, by non-P450 dismutase in the cytosol. This dismutation process also relied on the ratio of NADP+/NADPH in the cell. These findings for the first time elucidated the metabolic sites and routes of DOXO metabolism in human.
研究领域:
药理学
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生物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM
·
2024
·
IF 4.9
Peng Zhang,Dan Yuan,Chenglei Luo,Wenjing Guo,Fengxian Li
Cerebral perfusion is functionally regulated by neural mechanisms in addition to the systemic hemodynamic variation, vascular reactivity and cerebral metabolism. Although anesthesia is generally esteemed to suppress the overall brain neural activity and metabolism, a few inhalation anesthetics, such as isoflurane, can increase cerebral perfusion, thus heightening the risks of higher intracranial pressure, bleeding, and brain edema during surgery. With the aid of laser speckle contrast imaging, we observed a transient yet limited effect of cerebral perfusion enhancement in mice from awake to anesthetized conditions with different concentration of isoflurane. Retrograde and antegrade tracing revealed a higher proportion of parasympathetic control more than sympathetic innervation for the blood vessels. Surprisingly, isoflurane directly activated pterygopalatine ganglion (PPG) explants and induced FOS expression in the cholinergic neurons. Chemogenetic activation of cholinergic PPG neurons reduced isoflurane-related cerebral perfusion. On the contrary, ablation of the cholinergic PPG neurons resulted in further enhancement of cerebral perfusion induced by isoflurane. While blocking muscarinic cholinergic receptors resulted in the overall reduction upon isoflurane stimulation, the blockage of nicotinic cholinergic receptors enhanced the isoflurane-induced cerebral perfusion only when PPG neurons exist. Collectively, these results suggest that PPG play important roles in regulating cerebral perfusion under isoflurane inhalation.
研究领域:
神经科学
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麻醉学
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
FITOTERAPIA
·
2025
·
IF 2.6
Li-Li Ye,Meng-Yue Yang,Xiang-Hai Cai
Eight new gelsedine-type oxindole alkaloids and ten known analogues were isolated from the stems and leaves of Gelsemium elegans . Gelseansdine A ( 1 ) was an N 4 -deficient Gelsemium alkaloid, while gelseansdines E–H ( 12 , 14 , 16 – 17 ) represented a class of alkaloids polymerized with iridoid. Their structures were elucidated based on UV, HRESIMS, NMR spectroscopy, and electronic circular dichroism (ECD) data analyses. Additionally, the isolated compounds were screened for their inhibitory activity on macrophage M2 polarization.
研究领域:
植物化学
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药物化学
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免疫学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
IMMUNOPHARMACOLOGY AND IMMUNOTOXICOLOGY
·
2019
·
IF 2.086
Rui-Li Zhu,Ying-Kun Zhi,Lang Yi,Jin-Fang Luo,Jing Li,Sha-Sha Bai,Liang Liu,Pei-Xun Wang,Hua Zhou,Yan Dong
Objective: To investigate the cellular mechanism that sinomenine (SIN) inhibits inflammation in macrophages induced by LPS through α7 nicotinic acetylcholine receptor (α7nAChR).Materials and methods: RAW264.7 cells were stimulated with LPS and treated by SIN or nicotine (Nic). A selective antagonist of α7nAChR, α-bungarotoxin (BTX) was used to block α7nAChR. AG490 was used to inhibit JAK2 activation. ELISA was performed to detect the levels of TNF-α and MCP-1. Western blotting was used to analyze the expression of MIF, MMP-9, CD14, TLR4, STAT3 and p-STAT3. Intracellular-free calcium level was measured by Fluorescent probe fluo-3/AMResults: SIN inhibited the production of TNF-α, MCP-1, MIF, and MMP-9, decreased the expression of CD14 and TLR4, and inhibited the release of intracellular-free calcium from intracellular stores in RAW 264.7 cells stimulated by LPS. JAK-specific inhibitor AG490 attenuated the inhibitory effect of SIN on TNF-α. SIN increased the phosphorylation of STAT3. And the above effects of SIN were attenuated by antagonist of α7nAChR.Conclusions: SIN can decrease the expression of CD14/TLR4 and intracellular free calcium level, activate JAK2/STAT3 pathway to inhibit inflammatory response through α7nAChR in macrophages.
研究领域:
免疫学
·
药理学
·
细胞生物学
·
炎症研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
THERMOCHIMICA ACTA
·
2013
·
IF 1.989
Ning Li,Rui-Bin Zhang,Zhi-Hong Liu
Two pure mixed alkali/alkaline earth metal borates with three-dimensional framework, LiBaB 9 O 15 and NaBaB 9 O 15 , have been synthesized by high-temperature solid state reaction, and characterized by XRD, FT-IR, DTA–TG techniques and chemical analysis. The molar enthalpies of solution of LiBaB 9 O 15 and NaBaB 9 O 15 in 1 mol L −1 HCl(aq), and of LiCl·H 2 O(s)/NaCl(s) in [1 mol L −1 HCl + H 3 BO 3 + Ba(OH) 2 ·8H 2 O](aq) have been determined by microcalorimeter at 298.15 K, respectively. From these data and with the incorporation of the previously determined enthalpy of solution of H 3 BO 3 (s) in 1 mol L −1 HCl (aq), together with the use of the standard molar enthalpies of formation for Ba(OH) 2 ·8H 2 O(s), LiCl·H 2 O(s)/NaCl(s), H 3 BO 3 (s), HCl(aq) and H 2 O(l), the standard molar enthalpies of formation of −(6796.8 ± 7.3) kJ mol −1 for LiBaB 9 O 15 and −(6829.9 ± 7.3) kJ mol −1 for NaBaB 9 O 15 were obtained on the basis of the appropriate thermochemical cycles.
研究领域:
无机化学
·
物理化学
✓ 已验证
DOI
高影响因子
Journal of Chemistry
·
2017
·
IF 1.3
Xiaofei Jiang,Nengling Zhang,Nanqian Xiong,Yi Liu,Jianfeng Cao,ShengXiang Qiu
Jatrorrhizine was considered as one of the active constituents of Coptis chinensis Franch. Herein, jatrorrhizine derivatives with substituted amino groups linked at the 3-position were designed, synthesized, and biologically evaluated as inhibitors of acetylcholinesterase. Jatrorrhizine derivatives inhibited the activity of acetylcholinesterase (AChE) to a greater extent than the lead compound jatrorrhizine. All these jatrorrhizine derivatives were proved to be potent inhibitors of acetylcholinesterase (AChE) with submicromolar IC50 values, but less sensitive to butyrylcholinesterase (BuChE), which suggests that these jatrorrhizine derivatives are selective for AChE/BuChE. Compound 3g gave the most potent inhibitor activity for AChE (IC50 = 0.301 μM), which is greater than the lead compound jatrorrhizine. All these results demonstrated that these jatrorrhizine derivatives are potential inhibitors for AChE.
研究领域:
药理学
·
有机化学
·
神经科学
✓ 已验证
DOI
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2025
·
IF 4.7
Min Hong,Haobin Chen,Lei Li,Xiaoyan Liu,Qinghong Ji,Shuang Cheng,Chenzhong Li
A glutathione (GSH)-responsive amphiphilic camptothecin (CPT) prodrug, Lc-ss-CPT, was synthesized by conjugating hydrophobic CPT with hydrophilic L-carnitine (Lc) via a disulfide carbonate linker. The prodrug self-assembled into spherical nanoparticles (Lc-ss-CPT NPs, hydrodynamic diameter: ∼180 nm). In simulated gastrointestinal fluids and FBS-containing PBS, the NPs maintained stability over 24 h, with <10 % CPT leakage after 8 h. In vitro transcytosis studies using Caco-2 monolayers revealed an 188.5-fold higher apparent permeability coefficient for Lc-ss-CPT NPs than free CPT. The confocal fluorescence imaging studies demonstrated that the specific affinity between L-carnitine and organic cation transporter 2 (OCTN2) enhanced intestinal absorption of Lc-ss-CPT NPs and then transported into the bloodstream through transcytosis, facilitated by the Golgi apparatus and endoplasmic reticulum, enabling tumor accumulation. Pharmacokinetic analysis in rats showed oral administration of Lc-ss-CPT NPs achieved a higher bioavailability of 49.6 %. In HCT-116 cells, Lc-ss-CPT NPs reduced intracellular GSH to 5.4 % of baseline at 6 h, elevated ROS levels by 4.2-fold, and induced 71.2 % apoptosis. In MC38 tumor-bearing mice, oral Lc-ss-CPT NPs suppressed tumor growth by 86 % (vs. 12 % for free CPT). These data demonstrate the potential of Lc-ss-CPT NPs as an orally administrable platform for targeted CPT delivery.
研究领域:
药理学
·
肿瘤学
·
纳米医学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2025
·
IF 3.1
Xin-Nan Wang,Jian-Qun Liu,Wen-Liang Ji,Zong-Li Huo,Li-Fang Liu,Jia-Yi Zheng
Trimethylamine (TMA) metabolism comprises choline-containing compounds’ metabolization, TMA production and trimethylamine N-oxide (TMAO) generation. However, the presence of numerous compounds in the carnitine and phosphatidylcholine (PC) pool compositions complicates profiling work significantly. This study is aimed at developing an efficient method for profiling TMA metabolic pathways, including quantifying known compounds and semi-quantifying the differential metabolites in the carnitine and PC pool compositions. Pseudo-targeted metabolomics is applicable for characterization. Firstly, multivariate statistics were performed to identify valuable metabolites (variable importance in the projection ＞1) from quality control biological samples. Given that TMA metabolism involved in host-gut microbiota interaction, co-metabolites were defined as the intersections of valuable metabolites from different biological samples (serum, liver, and intestinal contents) and further screened. Finally, alterations in TMA metabolism were observed in dextran sulfate sodium-induced colitis, with semi-quantitative analysis for excavated co-metabolites including 11 PCs, 6 lyso-phosphatidylcholines, and 2 acylcarnitines and quantitative analysis for 10 known metabolites. The findings revealed increased TMA production and accumulation of choline-containing compounds in the gut during ulcerative colitis exacerbation. Correspondingly, the circulating level of TMAO was elevated in the colitis group. A comprehensive understanding of TMA metabolism can contribute to disease differential diagnoses and potential mechanism studies.
研究领域:
医学
·
微生物学
·
代谢组学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY C-TOXICOLOGY & PHARMACOLOGY
·
2025
·
IF 4.3
Lin Han,Wenzhi Liu,Fangying Yuan,Qianwen Liu,Hongyu Cheng,Xiaofeng Jin,Yanchun Sun
The ecological conditions of freshwater aquaculture are deteriorating by degrees in recent years. Consequently, the comprehensive utilization of saline-alkaline water has garnered increasing societal attention. Here, crucian carp ( Carassius auratus ) were exposed to 20, 40 mmol/L NaHCO 3 for 30 days (T, F group). Metabolomic analyses were conducted using UPLC-QTOF/MS, complemented by biochemical and microbiology profiling to elucidate the damage of the saline environment to the intestinal microbial structure, which in turn interfered with the energy metabolism. It was observed that carbonate alkalinity (CA) exposure not only caused intestine oxidative stress but also changed the levels of several digestive enzymes, including α-amylase (AMS), chymotrypsin (CHY), lipase (LPS). Metabolomic analysis identified 22 different metabolites (DEMs) in T group and 77 DEMs in F group. MetaboAnalyst analysis indicated that these metabolites are primarily involved in energy-related pathways, including the citric acid cycle, galactose metabolism, and glycine, serine, and threonine metabolism. Intestinal microbial diversity and community composition were altered under carbonate alkalinity exposure, with increase in Proteobacteria abundance and decline in Firmicutes, abundance alongside enrichment of Sphingomonas . Herein, saline-alkaline stress disrupted the physiological homeostasis of the crucian carp intestine, leading to microbial dysbiosis and energy metabolic imbalance. This study provides a theoretical foundation for understanding the stress response of the crucian carp intestine and the role of the intestinal microbiome in host resilience under adverse environmental conditions.
研究领域:
水产养殖学
·
环境生物学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
·
2021
·
IF 4.098
Yuhui Zhang,Xuanping Tan,Ligang Xing,Huan Wu,Jidong Yang
Two chiral drugs, ephedrine (EH) and pseudoephedrine (PEH), were commonly used in clinical treatment. Ephedrine (EH) and pseudoephedrine (PEH) could make different changes in resonance Rayleigh scattering spectrum of the detection system which use Ce 3+ functionalized gold nanoparticles as probe. Therefore, a new method of detecting EH and PEH separately was developed. The RRS spectrum and UV–Vis absorption spectrum of AuNPs-Ce 3+ detection system was analyzed in order to discuss the mechanism. Under optimal experimental conditions, the linear range of EH and PEH were 20–920 ng/mL and 40–520 ng/mL, respectively. The detection limit were 1.9 ng/mL and 3.8 ng/mL, respectively. Last used for actual testing, this method had obtained good results.
研究领域:
分析化学
·
药物分析
·
生物医学
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）