JOURNAL OF ETHNOPHARMACOLOGY
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2021
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IF 4.36
Han Zhou,Tao Hou,Zhenhua Gao,Xiujie Guo,Chaoran Wang,Jixia Wang,Yanfang Liu,Xinmiao Liang
Ethnopharmacological relevance Dopamine receptors are long-standing primary targets in the treatment of mental diseases and there is growing evidence that suggests relationships between obesity and the dopamine system, especially dopamine D1 and D2 receptors. Leaves of Nelumbo nucifera Gaertn. (lotus leaves) have been medically used for helping long-term maintenance of weight loss. Whether and how components of lotus leaves function through the dopamine receptors remains unclear. Aim of the study This work aimed to discover dopamine receptor-active alkaloids isolated from the lotus leaves, to evaluate their potencies and to analyze their structure activity relationship . Materials and methods Dried lotus leaves were prepared and total extract was divided into alkaloids and flavones . Eight alkaloids were separated and characterized by a combination of high-performance liquid chromatography, quadrupole time-of-flight mass spectrometry and nuclear magnetic resonance, and assayed by a fluorometric imaging plate reader platform. Human embryonic kidney 239 cell lines expressing dopamine D1, D2 and serotonin 2A (5-HT2A) receptors, respectively, were cultured and used in the assay. Results Alkaloids in the lotus leaves were the bioactive phytochemicals and inhibited dopamine from accessing the D1 and D2 receptors. All eight compounds functioned as D1-receptor antagonists and except N-nornuciferine, seven alkaloids functioned as D2-receptor antagonists. (S)-coclaurine and (R)-coclaurine are optical isomers and antagonized both D1 and D2 with equivalent potencies, suggesting that the optical rotation of the methylene linker in the monobenzyl isoquinoline backbone did not influence their activity. Among the eight alkaloids, O-nornuciferine was the potent antagonist to both receptors (the lowest IC 50 values, D1: 2.09 ± 0.65 μM and D2: 1.14 ± 0.10 μM) while N-nornuciferine was found to be the least potent as it moderately antagonized D1 and was inactive on D2. O-nornuciferine was also a 5-HT2A antagonist (IC 50 ~20 μM) while N-nornuciferine had no activity. These hinted the importance of a methyl group attached to the nitrogen atom in the aporphine backbone. Armepavine showed a nearly 10-fold selectivity to D2. Conclusions In this work, eight alkaloids were isolated from the leaves of Nelumbo nucifera Gaertn. and assayed on the D1 and D2 receptors. They were D1/D2 antagonists with IC 50 values in the mid- to low-micromolar range and O-nornuciferine was the most potent alkaloid among the eight. This family of alkaloids was biochemically evaluated on the dopamine receptors by the same platform for the first time.
研究领域:
药理学
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植物化学
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神经科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
APPLIED SURFACE SCIENCE
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2015
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IF 2.711
Jie-Ping Fan,Bing Zheng,Yu Qin,Dan Yang,Dan-Dan Liao,Xiao-Kang Xu,Xue-Hong Zhang,Jian-Hang Zhu
In this work, a superparamagnetic Fe 3 O 4 -graphene oxide (MGO) nanocomposite was prepared by one-step chemical co-precipitation method, and characterized by transmission electron microscopy (TEM), X-ray photoelectron spectroscopy (XPS), vibrating sample magnetometer (VSM), powder X-ray diffraction (PXRD), Raman spectroscopy and nitrogen adsorption–desorption curve. The as-prepared MGO was used to adsorb nuciferine, and the adsorption kinetic, isotherm and reusability of MGO were also investigated. The results showed that the adsorption of nuciferine on MGO reached its equilibrium very quickly (within 10 min) due to the two-dimensional carbon nanostructure of GO. In comparison with MGO, five conventional sorbents, i.e., macroporous resin D-101, silica gel, reverse phase silica gel (RP-C18) and cation exchange resin and polyamide, were also used to evaluate their adsorption capabilities. Therefore, MGO combined the advantages of both superparamagnetic particle and GO, i.e., easy separation and high absorption capacity. Finally, MGO was successfully applied to enrichment and separation of nuciferine in the extract of Nelumbinis Folium (Lotus leaf).
研究领域:
材料科学
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植物化学
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药用植物研究
✓ 已验证
DOI
高影响因子
Sustainable Chemistry and Pharmacy
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2023
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IF 6
Jiahuan Xu,Lijin Peng,Jianbo Chu,Jing Shi,Qinmin Cui,Qiyuan Shi
This work aims to resolve the environmental pollution caused by petroleum ether in the production of pure nuciferine from lotus leaf by applying bio-based solvent (D-limonene) and green solvent (ethyl acetate). Some obvious advantages were observed, over 97% of nuciferine could be extracted by vortex assisted two-phase solvent extraction based on multi-stage strategy (MS-VTSE), over 90% of nuciferine could be recovered by solid phase extraction (SPE), and over 97% of nuciferine could be obtained by pH-dependent liquid-liquid extraction (pH-LLE). It follows that the newly developed method can not only avoid the use of petroleum ether, but also increase the yield of the whole process by 14% (57%) in comparing with the result of the original one (50%) reported in our previous study. As D-limonene could by recycled conveniently, solvents replacement has little effect on the cost of production. In a word, the newly proposed method has advantages in environmental protection and solvent saving, thus, is fitting for the green and low-cost production of pure nuciferine from lotus leaf.
研究领域:
药学化学
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环境科学
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分析化学
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL IMMUNOPHARMACOLOGY
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2018
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IF 3.118
Lina Zhang,Jinghua Gao,Peng Tang,Li Chong,Yue Liu,Peng Liu,Xin Zhang,Li Chen,Chen Hou
Nuciferine, a bioactive component extracted from the lotus leaf , has been reported to have various anti-inflammatory effects. In the present study, we aimed to investigate the anti-inflammatory effects and mechanism of nuciferine on lipopolysaccharide (LPS)-stimulated BV2 microglia cells . The anti-inflammatory activity of nuciferine was measured by ELISA to detect the inflammatory mrdiators secretion in LPS-simulated BV2 microglia cells. The results demonstrated that nuciferine significantly inhibited LPS-induced TNF-α, IL-1β, PGE 2 and NO secretion. LPS-induced NF-κB activation was also suppressed by nuciferine. Further studies showed that nuciferine increased the expression of PPAR-γ. Functional aspects were analyzed using PPAR-γ specific inhibitor GW9662 , which attenuated the LPS-induced secretion of proinflammatory mediators, such as TNF-α, IL-1β, PGE 2 , and NO. In conclusion, these results suggested that nuciferine activated PPAR-γ, which subsequently inhibited LPS-induced inflammation in BV2 cells.
研究领域:
药理学
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免疫学
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神经科学
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细胞生物学
✓ 已验证
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）