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ELECTROPHORESIS · 2018 ·Vol. 40 ·期 4 ·582-586 · IF 2.569

Far infrared-assisted removal of extraction solvent for capillary electrophoretic determination of the bioactive constituents in Plumula Nelumbinis

Danjing Wan,Yu Han,Farui Li,Hua Mao,Gang Chen

Far infrared radiation was employed in the rapid removal of the solvents in the extracts of Plumula Nelumbinis and standard mixture solutions to prevent the interference of the solvent peaks toward their capillary electrophoretic measurements. The sample solutions in small vials were exposed to far infrared ray at 60°C for 3 min to remove solvent. The dried samples in the vials were each dissolved into running buffer with the aid of ultrasonication for capillary electrophoresis analysis. The far infrared-assisted solvent removal approach was sucessfully applied in the rapid determination of neferine, liensinine, isoliensinine, rutin and hyperoside in Plumula Nelumbinis . The five analytes could be well separated within 12 min in a 40 cm long fused silica capillary at a separation voltage of 12 kV in a 50 mM borate buffer (pH 9.2). The results indicated that the interferences of the solvent peaks in the capillary electropherograms of the herbal drugs were eliminated completely.

研究领域: 分析化学 · 中药学
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ANALYTICA CHIMICA ACTA · 2024 · IF 5.7

Development of CO2-switchable deep eutectic solvent-based liquid-liquid microextraction approach: Application in urinary excretion and tissue distribution studies

Lin Yang,Xiaoyue Yang,Erxu Wang,Bin Lu,Li Duan

Background Pharmacokinetic studies are pivotal in drug development , focusing on absorption, distribution, and excretion of active compounds. Effective sample preparation methods play a crucial role in these studies. Traditional techniques like protein precipitation and liquid-liquid extraction often involve toxic solvents and are time-consuming. Recently, deep eutectic solvent (DES) has emerged as an eco-friendly alternative due to its high efficiency, low cost, and low toxicity. This study introduces a novel sample pretreatment method using CO 2 -switchable DES in liquid-liquid microextraction (LLME) to enhance speed, accuracy, and sensitivity in complex biological samples analysis. Results A liquid-liquid microextraction sample pretreatment method based on switchable DES combined with high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) was established for the analysis of urine and tissue samples. The method was optimized through systematic investigation of key parameters, including DES type, volume, molar ratio, pH, vortex time, gas purge time, and salt addition. The resulting procedure exhibited satisfying linearity (r 2  ≥ 0.9958), good precision (RSD ≤6.01 %), desirable recovery (52.44%–98.12 %) and matrix effect (86.22%–119.30 %), and the accuracy and precision of stability were within the ±15 % limit. The proven methods were further applied to urinary excretion study and tissue distribution study of Nelumbinis plumula (NP) extract. The results indicated that the total cumulative excretion of liensinine, isoliensinine and neferine in urine within 240 h was 4.96 %, 0.66 % and 0.44 %, respectively. The tissue distribution study showed that alkaloids mainly distribute in liver, kidney, and spleen. Significance This research introduces a groundbreaking technique distinguished by its simplicity, speed, cost-effectiveness, and environmental friendliness. This approach, utilizing CO 2 -switchable DES as an extraction solvent for LLME, integrates deproteinization and removal of interfering molecules into a single step. This integration showcases its efficiency and convenience, demonstrating significant promise for various applications in the analysis of biological samples. Additionally, this study provides the first report on urinary excretion and tissue distribution of alkaloids from NP using a DES-LLME method. These findings offer valuable insights into the in vivo behavior of herbal medicine, enhancing understanding of pharmacological actions and facilitating clinical rational administration.

研究领域: 药物分析 · 中药学 · 分析化学
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JOURNAL OF ETHNOPHARMACOLOGY · 2023 · IF 5.4

Liensinine improves AngII-induced vascular remodeling via MAPK/TGF-β1/Smad2/3 signaling

Peizhi Jia,Daxin Chen,Ying Zhu,Meiling Wang,Jianwei Zeng,Ling Zhang,Qiaoyan Cai,Dawei Lian,Chunyu Zhao,Yaoyao Xu,Jianfeng Chu,Shan Lin,Jun Peng,Wei Lin

Ethnopharmacological relevance Liensinine(Lien, C 37 H 42 N 2 O 6 ) is an alkaloid compound from plumula nelumbinis that demonstrates an antihypertensive effect. The protective effects of Lien on target organs during hypertension are still unclear. Aim of the study : This study aimed to understand the mechanism of Lien during the treatment of hypertension, with emphasis on vascular protection. Materials and methods Lien was extracted and isolated from plumula nelumbinis for further study. In vivo model of Ang II-induced hypertension, non-invasive sphygmomanometer was used to detect the blood pressure in and out of the context of Lien intervention. Ultrasound was used to detect the abdominal aorta pulse wave and media thickness of hypertensive mice, and RNA sequencing was used to detect the differential genes and pathways of blood vessels. The intersection of Lien and MAPK protein molecules was detected by molecular interconnecting technique. The pathological conditions of abdominal aorta vessels of mice were observed by HE staining. The expression of PCNA, α-SMA, Collagen Type Ⅰ and Collagen Type Ⅲ proteins were detected by IHC. The collagen expression in the abdominal aorta was detected by Sirius red staining. The MAPK/TGF-β1/Smad2/3 signaling and the protein expression of PCNA and α-SMA was detected by Western blot. In vitro , MAPK/TGF-β1/Smad2/3 signaling and the protein expression of PCNA and α-SMA were detected by Western blot, and the expression of α-SMA was detected by immunofluorescence; ELISA was used to detect the effect of ERK/MAPK inhibitor PD98059 on Ang Ⅱ-induced TGF-β1secrete; and the detection TGF-β1and α-SMA protein expression by Western blot; Western blot was used to detect the effect of ERK/MAPK stimulant12-O-tetradecanoyl phorbol-13-acetate (TPA) on the protein expression of TGF-β1 and α-SMA. Results Lien displayed an antihypertensive effect on Ang Ⅱ-induced hypertension, reducing the pulse wave conduction velocity of the abdominal aorta and the thickness of the abdominal aorta vessel wall, ultimately improving the pathological state of blood vessels. RNA sequencing further indicated that the differential pathways expressed in the abdominal aorta of hypertensive mice were enriched in proliferation-related markers compared with the Control group. The profile of differentially expressed pathways was ultimately reversed by Lien. Particularly, MAPK protein demonstrated good binding with the Lien molecule. In vivo, Lien inhibited Ang Ⅱ-induced abdominal aorta wall thickening, reduced collagen deposition in the ventral aortic vessel, and prevented the occurrence of vascular remodeling by inhibiting MAPK/TGF-β1/Smad2/3 signaling activation. In addition, Lien inhibited the activation of Ang II-induced MAPK and TGF-β1/Smad2/3 signaling, attenuating the expression of PCNA and inhibiting the reduction of α-SMA, collectively playing a role in the inhibition of Ang Ⅱ-induced hypertensive vascular remodeling. PD98059 alone could inhibit Ang Ⅱ-induced elevation of TGF-β1 and the decrease of α-SMA expression. Further, PD98059 combined with Lien had no discrepancy with the inhibitors alone. Simultaneously TPA alone could significantly increase the expression of TGF-β1 and decrease the expression of α-SMA. Further, Lien could inhibit the effect of TPA. Conclusion This study helped clarify the protective mechanism of Lien during hypertension, elucidating its role as an inhibitor of vascular remodeling and providing an experimental basis for the research and development of novel antihypertensive therapies.

CAS / MDL: 9048-46-8
研究领域: 药理学 · 心血管疾病 · 分子生物学 · 民族药理学
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2023 · IF 6.1

Antimelanogenic Effect of Isoquinoline Alkaloids from Plumula Nelumbinis

Yi-Chi Chen,Yang-Yang Liu,Liqiang Chen,Dong-Mei Tang,YunLi Zhao,Xiao-Dong Luo

Plumula Nelumbinis, the green embryo of a lotus seed, is widely consumed in China as a well-known food with medicinal effects. In this study, 14 alkaloids, including 4 new and 10 known alkaloids, were isolated from it, which were elucidated by comprehensive spectroscopic analysis, and were investigated for their antimelanogenic effects in vitro and in vivo. As a result, melanogenesis in α-MSH-stimulated B16F10 cells was reduced significantly by a new compound 4 and known compound 12 at a concentration of 0.5 μg/mL, and the tyrosinase (TYR) activities were inhibited by 78.7 and 82.0% at 4 μg/mL, prior to α-arbutin (41.3%). Additionally, compounds 4 and 12 also exhibited superior antimelanogenic effects compared to α-arbutin on a zebrafish assay model at equivalent concentrations. Mechanistically, our preliminary findings suggested that compounds 4 and 12 exerted antimelanogenesis effect probably by inhibiting key proteins involved in melanin production such as microphthalmia-associated transcription factor, TYR, TRP-1, and TRP-2. The findings highlight the potential use of Plumula Nelumbinis containing compounds 4 and 12 as functional foods for treating hyperpigmentation.

CAS / MDL: 84380-01-8 298-93-1
研究领域: 药理学 · 生物化学 · 药物化学
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JOURNAL OF FOOD BIOCHEMISTRY · 2022 ·Vol. 46 ·期 8 ·e14194 · IF 3.654

The anticardiac fibrosis of total alkaloids of Plumula nelumbinis by regulating circulating lipidomic profile: In vivo study

Xuping Li,Shuotao Shi,Ying Yang,Yanmei Lou,Sixuan Chen,Yixin Guo,Xiaoxiao Qi,Ying Wang,Zhongqiu Liu,Yuanyuan Cheng

Plumula nelumbinis has great medicinal potential as a herbal tea and traditional drug in China. This study was aimed to evaluate the anticardiac fibrosis of the total alkaloids of P. nelumbinis (TAP). TAP at 50 mg/kg/day significantly ameliorated isoproterenol-induced cardiac fibrosis in mice ( p < .05). The circulating lipidomics study revealed that TAP improved the lipid metabolism dysfunction in cardiac fibrosis. Meanwhile, TAP suppressed the lipid accumulation, decreased MDA level ( p < .01) in heart, and increased FFA level ( p < .01). Furthermore, integrating lipidomics, chemical profiles and pharmacology network analysis found that AMPK and PI3K/Akt signaling pathways were the potential targeted pathway by TAP to regulate lipid metabolism dysfunction including glycerophospholipid metabolism. Above all, TAP provided a potential anticardiac fibrosis effect partly through regulation of lipid profiles. Practical applications The total alkaloids of Plumula nelumbinis (TAP) suppressed ISO-induced cardiac fibrosis in mice. Network pharmacology analysis and experiments revealed that TAP-regulated AMPK and PI3K/Akt signaling pathway to improve lipid metabolism disorder in cardiac fibrosis. This study provides evidence to the therapeutic potential of TAP in the treatment of ISO-induced cardiac fibrosis and could be a drug candidate for prevention and treatment of cardiac fibrosis.

CAS / MDL: 51-30-9
研究领域: 药理学 · 心脏病学 · 脂质组学 · 中药学
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS · 2025 · IF 3.1

Acetylcholinesterase immobilized on MIL-88B-NH2 MOF for rapid screening inhibitors from herbal medicines: ligand fishing coupled with mass spectrometry

Erxu Wang,Huiran Zhang,Xiangchuan Li,Lili Geng,Zhen Wang,Airong Chu,Bin Lu,Li Duan

Alzheimer’s disease (AD) is a common neurodegenerative disease, and is characterized by impaired acetylcholine-mediated neurotransmission. Acetylcholinesterase (AChE) inhibition is a well-established therapeutic strategy for AD. Medicinal plants exhibit multi-target effects, low toxicity, and cost-effectiveness. Therefore, screening AChE inhibitors from botanical sources holds considerable pharmacological potential. In this study, a metal-organic framework was used as a novel support for immobilizing AChE, resulting in the creation of AChE@MIL-88B-NH 2 , which served as a tool for screening potential AChE inhibitors. The immobilized enzyme exhibited excellent reusability, stability against pH fluctuations and thermal stress, and resistance to organic solvents. The constructed AChE@MIL-88B-NH 2 -based ligand fishing strategy coupled with mass spectrometry was applied to screen for AChE inhibitors in Nelumbinis plumula extracts. Seven compounds were identified as potent AChE inhibitors. Enzyme kinetic assays revealed that these ligands exhibit a mixed inhibition mechanism against AChE. Molecular docking demonstrated that the seven compounds effectively bound to the AChE active site, with binding affinities ranging from -9.7 to -8.5   kcal/mol. The established AChE@MIL-88B-NH 2 -based ligand fishing strategy provides a simple and efficient approach for screening potential AChE inhibitors from complex botanical matrices, offering a promising avenue for discovering novel therapeutic agents for AD.

CAS / MDL: 10312-55-7
研究领域: 神经药理学 · 酶学 · 药物发现 · 生物有机化学 · 分析化学 · 材料科学 · 植物化学 · 结构生物学
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