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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS · 2024 · IF 3.1

Simultaneous determination of five constituents of areca nut extract in rat plasma using UPLC-MS/MS and its application in a pharmacokinetic study

Mingyu Pan,Wenfeng Geng,Yuanxiao Wang,Makoto Tsunoda,Jiatong Liu,Yingxia Zhang,Haimei Yang,Lu-shuang Li,Shiwen Song,Jinqiang Liang,Yanting Song

Areca nuts have been used as a traditional Chinese medicine (TCM) for thousands of years. Recent studies have shown that it exhibits good pharmacological activity and toxicity. In this study, the pharmacokinetics of five major components of areca nut extract in rats were investigated using a highly sensitive ultra-performance liquid chromatography coupled with triple quadrupole mass spectrometry (UPLC-MS/MS) method. Arecoline, arecaidine, guvacoline, guvacine, and catechin were separated and quantified accurately using gradient elution with mobile phases of (A) water containing 0.1 % formic acid-10 mM ammonium formate, and (B) methanol. The constituents were detected under a timing switch between the positive and negative ion modes using multiple reaction monitoring (MRM). Each calibration curve had a high R 2 value of >0.99. The method accuracies ranged −7.09–11.05 % and precision values were less than 14.36 %. The recovery, matrix effect, selectivity, stability, and carry-over of the method were in accordance with the relevant requirements. It was successfully applied for the investigation of the pharmacokinetics of these five constituents after oral administration of areca nut extract. Pharmacokinetic results indirectly indicated a metabolic relationship between the four areca nut alkaloids in rats. For further clarification of its pharmacodynamic basis, this study provided a theoretical reference.

CAS / MDL: 540-69-2 64-18-6
研究领域: 药理学 · 分析化学 · 中药学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Functional Foods · 2020 · IF 3.701

Egg yolk phospholipids reverse scopolamine–induced spatial memory deficits in mice by attenuating cholinergic damage

Zhijie Bao,Penglin Zhang,Jin Chen,Jie Gao,Songyi Lin,Na Sun

This study was conducted to investigate possible mechanisms underlying egg yolk phospholipids on improving memory using scopolamine–treated mice and PC12 cells. Oral administration of egg yolk phospholipids significantly decreased latency in passageway water maze tasks and reduced error hits in passive avoidance tests for scopolamine–treated mice ( P  < 0.05). As the results presented, egg yolk phospholipids attenuated spatial memory deficits via preventing region–specific lesions in hippocampus CA1-2 and regulating the activity of cholinergic biomarkers. Egg yolk phospholipids significantly inhibited scopolamine–induced increase of acetylcholinesterase activity and decrease of choline acetyltransferase activity ( P  < 0.05), thus maintaining the release of acetylcholine at a normal level. Further analysis showed that egg yolk phospholipids downregulated scopolamine–induced MAO activity and MDA level in PC12 cells ( P  < 0.05). These data suggest that egg yolk phospholipids might exert neuroprotective effects via attenuating cholinergic damage and inhibiting the oxidative stress in vitro .

CAS / MDL: 51-34-3
研究领域: 神经科学 · 药理学 · 营养科学
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FLUID PHASE EQUILIBRIA · 2017 · IF 2.473

Ternary phase behavior of phenol + toluene + zwitterionic alkaloids for separating phenols from oil mixtures via forming deep eutectic solvents

Congfei Yao,Yucui Hou,Shuhang Ren,Youan Ji,Weize Wu

Phenols are important materials for the organic chemical industry. They mainly come from coal liquefaction oil, coal tar, petroleum and biomass pyrolysis oil, making the separation of phenols from oil mixtures of great commercial value. Two zwitterionic alkaloids, betaine and L-carnitine, biodegradable and environmentally benign ionic compounds , can efficiently separate phenols from oils by forming deep eutectic solvents (DESs). In this work, the phase equilibria of two ternary systems of toluene + phenol + betaine and toluene + phenol + L-carnitine were measured at 25.0 °C, 45.0 °C and 65.0 °C under atmospheric pressure. The phase behaviors of the two ternary systems were studied, which indicated that there were three kinds of phase regions: liquid, liquid-liquid, and liquid-liquid-solid. The separation of phenol from oil mixtures occurs at the latter two phase regions. Effects of temperature, zwitterionic alkaloid type and its dosage on the phase equilibrium were investigated. With decreasing temperature, the distribution and selectivity coefficients increase. L-carnitine shows better performance in separating phenol from oils via forming DES than betaine.

CAS / MDL: 88-72-2 108-95-2
研究领域: 化学工程 · 物理化学 · 环境科学
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JOURNAL OF ETHNOPHARMACOLOGY · 2018 · IF 3.115

The influence of compatibility of Si-Ni decoction with metabolism in intestinal bacteria on transports of toxic diterpenoid alkaloids from processed aconite root across Caco-2 monolayers

Min Zhang,Ying Peng,Mengyue Wang,Beibei Gao,Lijuan Zhao,Xiaobo Li

Ethnopharmacological relevance In traditional Chinese medicine , processed aconite root (lateral root of Aconitum carmichaelii Debx.) is used as the principle herb of the Si-Ni decoction (SND) formula due to its cardiotonic effect, while its cardiotoxicity and neurotoxicity caused by diester and monoester diterpenoid alkaloids are reduced by compatibility of dried ginger and honey-processed liquorice in SND. Aim of the study To investigate the detoxification of processed aconite root by compatibility of SND from the perspective of intestinal absorption with metabolism in intestinal bacteria . Materials and methods Decoctions of processed aconite root (AD), processed aconite root and honey-processed liquorice (ALD), and SND with the same amount of each herb were prepared, then were incubated in human intestinal bacteria juice (IBJ) in vitro for different durations. Bidirectional transmembrane transports of these decoctions and their IBJ-incubated decoctions were conducted on Caco-2 monolayers. Correlation between efflux ratios changes of benzoylmesaconine, benzoylaconine, benzoylhypaconine (monoester-diterpenoid alkaloids, MDAs) and hypaconitine (diester-diterpenoid alkaloids) from processed aconite root, and metabolic trends of compounds from honey-processed liquorice and dried ginger were also performed. Results The absorption of MDAs from processed aconite root was increased by combination with honey-processed liquorice in ALD, but they were decreased significantly by the addition of dried ginger in SND. Take benzoylhypaconine for example, the P app, AP to BL soared from ( 3.13 ± 0.18) × 10 −7 cm/s in AD to (23.32 ± 3.51) × 10 −7 cm/s in ALD, while it dropped to (1.12 ± 0.17) × 10 −7 cm/s in SND. When herb combined decoctions metabolised by intestinal bacteria for 12 h, the efflux ratio of benzoylhypaconine were both increased from 0.56 to 1.21 in ALD and from 1.10 to 2.61 in SND, which was correlative with the generation of davidigenin and glycyrrhetic acid (the metabolites of chalcones and pentacyclic triterpenoids from liquorice) in ALD and with the metabolism of [6]-gingerol (the major compound from dried ginger) in SND, respectively. Conclusions Compatibility of SND altered the intestinal absorption of toxic MDAs and hypaconitine from processed aconite root. In SND, dried ginger rather than honey-processed liquorice played the role of detoxification of these toxic compounds in the intestinal absorption. The intestinal detoxification of SND was significantly and strongly correlative with metabolism of dried ginger and honey-processed liquorice by intestinal bacteria, simultaneously.

研究领域: 药理学 · 民族药理学 · 微生物学 · 毒理学 · 中医药学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Drug Design Development and Therapy · 2022 · IF 4.319

Anti-Inflammatory Activation of Phellodendri Chinensis Cortex is Mediated by Berberine Erythrocytes Self-Assembly Targeted Delivery System

Minhua Li,Zehui Qin,Qiuxia Yu,Ziwei Huang,Juanjuan Cheng,Linjiang Zhong,Yuhong Liu,Jianhui Xie,Yucui Li,Jiannan Chen,Ruoting Zhan,Ziren Su

Background Berberine (BBR) is the primary active component of Phellodendri Chinensis Cortex (PCC), which has been traditionally used to treat inflammatory diseases. However, the discrepancy between its low bioavailability and significant therapeutic effect remains obscure. The purpose of this study was to explore the previously unsolved enigma of the low bioavailability of BBR and its appreciable anti-inflammatory effect to reveal the action mechanism of BBR and PCC. Methods The quantitative analysis of BBR and its metabolite oxyberberine (OBB) in blood and tissues was performed using high-performance liquid chromatography to investigate the conversion and distribution of BBR/OBB mediated by erythrocytes. Routine blood tests and immunohistochemical staining were used to explore the potential relationship between the amounts of monocyte/macrophage and the drug concentration in erythrocytes and tissues (liver, heart, spleen, lung, kidney, intestine, muscle, brain and pancreas). To comparatively explore the anti-inflammatory effects of BBR and OBB, the acetic acid-induced vascular permeability mice model and lipopolysaccharide-induced RAW 264.7 macrophages were employed. Results Nearly 92% of BBR existed in the erythrocytes in rats. The partition coefficient of BBR between plasma and erythrocytes (Kp/b) decreased with time. OBB was found to be the oxidative metabolite of BBR in erythrocytes. Proportion of BBR/OBB in erythrocytes changed from 9.38% to 16.30% and from 13.50% to 46.24%, respectively. There was a significant relationship between the BBR/OBB concentration in blood and monocyte depletion after a single administration of BBR. BBR/OBB was transported via erythrocytes to various tissues (liver, kidney, spleen, lung, and heart, etc), with the liver achieving the highest concentration. OBB exhibited similar anti-inflammatory effect in vitro and in vivo as BBR with much smaller dosage. Conclusion BBR was prodominantly found in erythrocytes, which was critically participated in the biodistribution, pharmacokinetics, metabolism and target delivery of BBR and its metabolite. The anti-inflammatory activity of BBR and PCC was intimately associated with the metabolism into the active congener OBB and the targeted delivery to monocytes/macrophages mediated by the erythrocytes.

研究领域: 药理学 · 中药学 · 生物化学
✓ 已验证 DOI PubMed 高影响因子
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Nature Communications · 2025 ·Vol. 16 ·期 1 ·1-13 · IF 15.7

A concise enzyme cascade enables the manufacture of natural and halogenated protoberberine alkaloids

Li Fei,Yuan Zhenbo,Gao Yue,Deng Zhiwei,Zhang Yan,Luo Zhengshan,Rao Yijian

The application and drug development of plant-derived natural products are often limited by their low abundance in medicinal plants and the lack of structural complexity and diversity. Herein, we design a concise enzyme cascade to efficiently produce natural and unnatural protoberberine alkaloids from cost-effective, readily available substrates. Through enzyme discovery and engineering, along with systematic optimization of the berberine bridge enzyme to address remaining manufacturing challenges in protoberberine alkaloid biosynthesis, the high production of drug Rotundine is achieved at an impressive gram-scale titer, demonstrating its industrial potential. More importantly, this cascade also enables the efficient biosynthesis of various unnatural halogenated protoberberine alkaloids. Thus, this work not only unlocks the potential of enzyme cascades in overcoming longstanding challenges in the efficient biosynthesis of plant-derived alkaloids, but also opens avenues to introduce structural complexity and diversity into alkaloids through synthetic biology, offering significant potential for drug development.

研究领域: 生物化学 · 合成生物学 · 药物开发
✓ 已验证 DOI PubMed 高影响因子
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ANALYTICAL BIOCHEMISTRY · 2021 · IF 3.365

Simultaneous separation and determination of three huperzine alkaloids in Huperzia serrata and its preparations by cyclodextrin-modified mixed micellar electrokinetic capillary chromatography

Yuhang Yang,Hua Wang,Haixia Yu,Hongfen Zhang,Guangbin Zhang,Ruimiao Chang,Anjia Chen

In this study, a simple and sensitive cyclodextrin-modified mixed micellar electrokinetic capillary chromatography (CD-MEKC) method has been developed for the simultaneous separation and determination of Huperzine A (HupA), Huperzine B (HupB) and Huperzine C (HupC) in Huperzia serrata (H. serrata). The optimal conditions (pH 9.3) were composed of 10 mM sodium tetraborate solution, 40 mM sodium dodecyl sulfate (SDS), 50 mM sodium cholate (SC) and 3.0 mM mono-(6-ethylenediamine-6-deoxy)-β-cyclodextrin (ED-β-CD). The separation and determination process were performed on a P/ACE MDQ capillary electrophoresis system, the separation voltage was 15 kV, the temperature was 25 °C and the detection wavelength was 308 nm. Under the optimum conditions, the migration time was less than 9 min. The LOD and LOQ were between 0.38 and 0.80 μg/mL and 1.2–2.3 μg/mL, respectively. The developed method, with excellent precision and accuracy, was applied for the determination of three alkaloids in H. serrata and its formulations.

CAS / MDL: 7704-34-9
研究领域: 植物化学 · 分析化学 · 药学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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SENSORS · 2018 ·Vol. 18 ·期 10 ·3358 · IF 2.475

Construction of Multiple Switchable Sensors and Logic Gates Based on Carboxylated Multi-Walled Carbon Nanotubes/Poly(N,N-Diethylacrylamide)

Xuemei Wu,Xiaoqing Bai,Yang Ma,Jie Wei,Juan Peng,Keren Shi,Huiqin Yao

In this work, binary hydrogel films based on carboxylated multi-walled carbon nanotubes/poly(N,N-diethylacrylamide) (c-MWCNTs/PDEA) were successfully polymerized and assembled on a glassy carbon (GC) electrode surface. The electroactive drug probes matrine and sophoridine in solution showed reversible thermal-, salt-, methanol- and pH-responsive switchable cyclic voltammetric (CV) behaviors at the film electrodes. The control experiments showed that the pH-responsive property of the system could be ascribed to the drug components of the solutions, whereas the thermal-, salt- and methanol-sensitive behaviors were attributed to the PDEA constituent of the films. The CV signals particularly, of matrine and sophoridine were significantly amplified by the electrocatalysis of c-MWCNTs in the films at 1.02 V and 0.91 V, respectively. Moreover, the addition of esterase, urease, ethyl butyrate, and urea to the solution also changed the pH of the system, and produced similar CV peaks as with dilution by HCl or NaOH. Based on these experiments, a 6-input/5-output logic gate system and 2-to-1 encoder were successfully constructed. The present system may lead to the development of novel types of molecular computing systems.Keywords:electrocatalysis;encoder;logic gate;matrine;sophoridine

CAS / MDL: 7775-27-1
研究领域: 材料科学 · 生物医学工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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CHEMISTRY & BIODIVERSITY · 2025 · IF 2.5

Three Novel Quinoline Alkaloids From Tetradium glabrifolium and Their Antibacterial Activities

Li-li Luo,Jun-lei Chen,Cai-xia Du,Lie-jun Huang,Chun-mao Yuan,Jue Yang,Zhan-Xing Hu,Xiao-jiang Hao,Wei Gu

Three novel quinoline alkaloids, tetradiunitiside A ( 1 ), tetradiunitiside B ( 2 ), and glycohaplopine-6- O -α- l -rhamnopyranoside ( 3 ), along with eight known ones ( 4–11 ), were isolated from the fruits of Tetradium glabrifolium . Their structures were inferred by IR, 1D NMR and 2D NMR, and HR–ESI–MS spectra. All the isolated compounds were evaluated for their antibacterial activities. Compounds 1–11 had potential antibacterial activities against Bacillus gasoformans , Bacillus subtilis , Pseudomonas solanacearum , and Pseudomonas aeruginosa , with minimum inhibitory concentration (MIC) values ranging from 100 to 3.125 µg/mL. Among them, compound 6 showed the most significant antibacterial activity against four strains of bacteria. These findings elucidated the pharmacological substance basis for the antibacterial activity of T. glabrifolium to some extent. Graphical Three novel quinoline alkaloids together with eight known ones were isolated from the fruits of Tetradium glabrifolium . The antibacterial activity of compounds against four bacteria strains were screened, and 11 compounds exhibited significant antibacterial activity.

研究领域: 植物化学 · 药理学 · 微生物学
✓ 已验证 DOI PubMed 高影响因子
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GOLD BULLETIN · 2020 ·Vol. 53 ·期 3 ·159-165 · IF 1.706

Gold nanorods as colorimetric probes for naked-eye recognition of carnitine enantiomers

Wang Yanwei,Zhou Xiaojuan,Liu Qiang,Jin Yan,Xu Chunli,Li Baoxin

In this work, we proposed one simple and effective chiral-sensing method for the discrimination of carnitine enantiomers. The gold nanorods (AuNRs) were used as colorimetric probes to recognize carnitine enantiomers in this method. l -Carnitine can induce rapidly the blue-to-gray change of AuNR solution color, whereas d -carnitine cannot induce the obvious change of the color. Based on this distinct difference of color, a visual method for recognition of carnitine enantiomers was suggested. This method has been applied to detect the enantiometric excess of l -carnitine in the range of − 100~100%. The presented chiral measurement can be performed with a simple ultraviolet-visible spectrometer and even the naked eyes. In this method, AuNRs need no modification with chiral molecule, and the chiral recognition is based on the inherent chirality of AuNRs. This new method opens up possibility for fast and easy assay of carnitine enantiomers. Graphical abstract

研究领域: 分析化学 · 生物化学 · 纳米技术
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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES · 2022 ·Vol. 23 ·期 18 ·10898 · IF 6.208

Transcriptome Analysis Reveals an Essential Role of Exogenous Brassinolide on the Alkaloid Biosynthesis Pathway in Pinellia Ternata

Chenchen Guo,Ying Chen,Dengyun Wu,Yu Du,Mengyue Wang,Cunqi Liu,Jianzhou Chu,Xiaoqin Yao

Pinellia ternata(Thunb.) Druce is a traditional medicinal plant containing a variety of alkaloids, which are important active ingredients. Brassinolide (BR) is a plant hormone that regulates plant response to environmental stress and promotes the accumulation of secondary metabolites in plants. However, the regulatory mechanism of BR-induced alkaloid accumulation inP. ternatais not clear. In this study, we investigated the effects of BR and BR biosynthesis inhibitor (propiconazole, Pcz) treatments on alkaloid biosynthesis in the bulbil ofP. ternata. The results showed that total alkaloid content and bulbil yield was enhanced by 90.87% and 29.67% under BR treatment, respectively, compared to the control. We identified 818 (476 up-regulated and 342 down-regulated) and 697 (389 up-regulated and 308 down-regulated) DEGs in the BR-treated and Pcz-treated groups, respectively. Through this annotated data and the Kyoto encyclopedia of genes and genomes (KEGG), the expression patterns of unigenes involved in the ephedrine alkaloid, tropane, piperidine, pyridine alkaloid, indole alkaloid, and isoquinoline alkaloid biosynthesis were observed under BR and Pcz treatments. We identified 11, 8, 2, and 13 unigenes in the ephedrine alkaloid, tropane, piperidine, and pyridine alkaloid, indole alkaloid, and isoquinoline alkaloid biosynthesis, respectively. The expression levels of these unigenes were increased by BR treatment and were decreased by Pcz treatment, compared to the control. The results provided molecular insight into the study of the molecular mechanism of BR-promoted alkaloid biosynthesis.Keywords:alkaloid;brassinolide;ephedrine;secondary metabolism;RNA-seq

研究领域: 植物学 · 药理学 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2022 · IF 5.518

Enzymatic demulsification of long-chain alkanoylcholine-based oil-in-water emulsions and microemulsions

Yanjie Xu,Hui Chen,Xuefeng Liu,Lianlian Sun,Yinjun Fang

Long-chain alkanoylcholines (LCAC) are potential candidates to limit viruses’ transmission and suitable substrates of butyrylcholinesterase (BChE) to be hydrolyzed. Thus, BChE-catalyzed LCAC hydrolysis is expected to be a safer and greener demulsification strategy in demulsifying LCAC-based emulsions and/or microemulsions . Myristoylcholine bromide (MCB)-based oil-in-water (O/W) emulsions with different oils, from hydrocarbon nonpolar oil (octane and D80) to ester-containing polar oil (jojoba oil and edible oil) as well as the complex oily mixture (crude oil), were constructed. MCB-based microemulsions were constructed by pseudo-ternary phase diagram method. The BChE-catalyzed hydrolysis of MCB was monitored by using of two-phase titration. MCB-based O/W type emulsions and microemulsion can be actively demulsified by using of BChE under mild conditions of pH = 7.4 and 37 °C. No lethal adverse effect of the oil type on the BChE-catalyzed hydrolysis of MCB was observed in demulsifying emulsions. BChE can be reused and presented an excellent reusability over five times of recycling, clarifying a promising prospect of this enzymatic demulsification strategy in the treatment of LCAC-emulsified wastewater.

研究领域: 生物化学 · 环境科学 · 医学
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