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
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DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2019
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IF 3.414
Yuhuan Chen,Qiwen Chen,Xiaozhong Wang,Fan Sun,Yawei Fan,Xiaoru Liu,Hongyan Li,Zeyuan Deng
Ethnopharmacological relevance Nelumbo nucifera Gaertn (lotus) leaves were empirically carbonized to enhance the hemostatic effect in traditional Chinese medicines . The mechanism of this application remains unclear. Aim of the study The present study aims at exploring the transformation of phytochemical compounds in lotus leaves after heating and figuring out the phytochemical mechanism of the application of charcoal hemostatic styptics. Methods and results Raw lotus leaves were heated at 150 °C and 220 °C, respectively, and the transformation of the phytochemicals was studied. Flavonol glycosides in raw lotus leaves were found to be degraded to their corresponding aglycons in 150 °C lotus leaf charcoals (LLC) and the subsequent degradation products of aglycons in 220 °C LLC. 150 °C LLC exhibited the most desirable hemostatic effect in mice on reducing both bleeding time (BT) and clotting time (CT) by more than 30% as compared to the untreated group (P < 0.05). The extracts of 150 °C LLC were further separated by using different solvents. Ethyl acetate fraction which contained much flavonol aglycons displayed the most desirable hemostatic effect. On the contrary, petroleum ether fraction contains poor flavonoid and much alkaloid thus prolonged BT and CT. N-butanol extracts which contained only flavonol glycoside failed to shorten CT. In rats, quercetin (aglycon) standard promoted blood coagulation by shortening APTT (activated partial thromboplastin time) and increasing fibrinogen (P < 0.05). Hyperoside (glycoside) increased fibrinogen and platelet count (P < 0.05). Nuciferine was shown to prolong APTT and TT (thrombin time) and decrease fibrinogen (P > 0.05). Conclusion Degradation of flavonoids and alkaloids in lotus leaves was suggested to enhance the hemostatic effect of LLC. Flavonol aglycons were found to be more effective on blood clotting compared with their corresponding glycosides. Nuciferine, a typical alkaloid in lotus leaves which was degraded in LLC showed anticoagulation effect in rats. The content of flavonoid aglycon can be regarded as a criterion to qualify LLC.
研究领域:
药理学
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民族药理学
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传统医学
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植物化学
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DOI
PubMed
高影响因子
FOOD CHEMISTRY
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2025
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IF 9.8
Fuhui Luo,Zhongqiao Zhao,Yong He,Fenfen Zeng,Xia Yang,Fengxiang Zhang,Wei Shi
Nelumbinis Plumula, a dual-use medicinal and edible plant, has been processed into a functional drinks and exhibits pharmaceutical potential via bioactive compounds. Here, a new solvent system composed of alkaline electrolyzed water (AEW) and deep eutectic solvents (DES) (AEWDES) has been developed. Screening 30 solvents revealed AEWDESs (L-proline-1-methylurea) (LP-JJN) outperformed ultrasound assisted DESs and traditional solvents in extraction efficiency. We propose a novel hybrid framework integrating Crested porcupine optimizer-Backpropagation neural networks-Sparrow search algorithm (CPO-BP-SSA) for alkaloids extraction optimization. The yield enhancement primarily stems from AEWDES-mediated cell wall disruption increasing compound accessibility and augmented intermolecular interactions (hydrogen bonding, Van Der Waals force) between target alkaloids and DES components. Green metrics validated the method's sustainability. AEWDES extraction method is universal and can serve as a reference for the extraction of various alkaloids. Future research should prioritize the recovery of alkaloids compounds through advanced extraction and desorption techniques.
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高影响因子
Oxidative Medicine and Cellular Longevity
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2021
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IF 6.543
Jin-jin Zhu,Bin-yuan Yu,Xiao-kai Huang,Min-zhi He,Bin-wen Chen,Ting-ting Chen,Huang-yi Fang,Shang-qin Chen,Xiao-qin Fu,Pei-jun Li,Zhen-lang Lin,Jiang-hu Zhu
Hypoxic-ischemic encephalopathy (HIE) is recognized as the main cause of neonatal death, and efficient treatment strategies remain limited. Given the prevalence of HIE and the associated fatality, further studies on its pathogenesis are warranted. Oxidative stress and neuroinflammatory injury are two important factors leading to brain tissue injury and nerve cell loss in HIE. Neferine, an alkaloid extracted from lotus seed embryo, exerts considerable effects against several diseases such as cancers and myocardial injury. In this study, we demonstrated the neuroprotective effect of neferine on HIE and hypothesized that it involves the inhibition of neuronal pyroptosis, thereby ameliorating neurological inflammation and oxidative stress. We demonstrated that the mRNA levels of proteins associated with pyroptosis including caspase-1, the caspase adaptor ASC, gasdermin D, interleukin- (IL-) 18, IL-1β, and some inflammatory factors were significantly increased in neonatal HIBD model rats compared to those in the control group. The increase in these factors was significantly suppressed by treatment with neferine. We stimulated PC12 cells with CoCl2 to induce neuronal HIBD in vitro and investigated the relationship between neferine and pyroptosis by altering the expression of the NLRP3 inflammasome. The overexpression of NLRP3 partially reversed the neuroprotective effect of neferine on HIBD, whereas NLRP3 knockdown further inhibited caspase-1 activation and IL-1β and IL18 expression. In addition, simultaneous alteration of NLRP3 expression induced changes in intracellular oxidative stress levels after HIBD. These findings indicate that neferine ameliorates neuroinflammation and oxidative stress injury by inhibiting pyroptosis after HIBD. Our study provides valuable information for future studies on neferine with respect to neuroinflammation and pyroptosis.
研究领域:
神经科学
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药理学
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分子生物学
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儿科
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DOI
PubMed
高影响因子
CHEMICAL ENGINEERING & TECHNOLOGY
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2022
·Vol. 46
·期 4
·803-812
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IF 2.215
Qin Li,Lijin Peng,Jing Shi,Jianbo Chu,Xinyue Zhang,Qiyuan Shi
An efficient and sustainable expanded-bed adsorption (EBA) method was developed for the valorization of lotus leaf which is an agricultural by-product. The in-situ procedure was used to reduce the energy consumption of EBA. Comparing this in-situ process to the conventional one, some additional advantages were observed, namely, significant enhancement of nuciferine recovery, considerable reduction of processing time, etc. Furthermore, a multistage procedure was investigated to reduce running cost and minimize environmental pollution by reusing solvents and adsorbents. Reusing of D101 macroporous resin, HCl and NaOH solution had almost no influence on the yield of nuciferine.
研究领域:
农业工程
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化学工程
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药学
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环境科学
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DOI
高影响因子
JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
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2024
·Vol. 105
·期 1
·635-648
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IF 3.3
Shixiang Chen,Bochen Wei,Lili Wen,Penglian Wei,Yunlin Fu
BACKGROUND Michelia macclurei Dandy is a traditional Chinese medicinal plant, but little is understood about the bioactive compositions and biological potential of its different parts, limiting their applications. This study aims to identify the bioactive compositions and analyze differences in accumulation patterns from different parts of Michelia macclurei (heartwood, sapwood, bark, root, leaf, and fruit) using metabolomics. It also seeks to explore their biological potential and analyze the relationship between the bioactive compositions and biological potential. RESULTS A total of 63 volatile metabolites (VMs) were identified by gas chromatography–mass spectrometry (GC–MS) in six parts, and the VMs in each part were dominated by sesquiterpenes and their derivatives (71.40–88.32%). Six parts of Michelia macclurei contained structurally diverse non-volatile metabolites (NVMs) with a total of 207 bioactive compounds, including 92 alkaloids, 30 flavonoids, 19 lignans, and 18 organic acids, utilizing ultra-performance liquid chromatography–mass spectrometry (UPLC–MS) analysis. Multivariate statistical analysis showed that the accumulation patterns of bioactive compositions differed significantly among the different parts, and the 25 VMs and 72 NVMs could be considered potential markers for distinguishing the different parts of Michelia macclurei . The excellent antioxidant and enzyme inhibitory capacity of extracts of all six parts was indicated by in vitro bioactivity assays. Pearson's correlation analysis showed that the bioactive compositions in the six parts were significantly correlated with antioxidant and enzyme inhibitory activities. CONCLUSION This study offers helpful information on the distribution of bioactive compositions in different parts of Michelia macclurei and confirms the excellent antioxidant, and enzyme inhibitory potential of its extracts, which could provide scientific evidence for its potential applications in the pharmaceutical industry, cosmetics, and functional foods. © 2024 Society of Chemical Industry.
研究领域:
药理学
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代谢组学
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中医药
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植物化学
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PubMed
高影响因子
JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH
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2019
·Vol. 38
·期 1
·1-15
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IF 5.646
Li Zizhuo,Chen Yaodong,An Tingting,Liu Pengfei,Zhu Jiyuan,Yang Haichao,Zhang Wei,Dong Tianxiu,Jiang Jian,Zhang Yu,Jiang Maitao,Yang Xiuhua
Background Nuciferine (NF), extracted from the leaves of N. nucifera Gaertn, has been shown to exhibit anti-tumor and anti-viral pharmacological properties. It can also penetrate the blood brain barrier (BBB). However, the mechanism by which NF inhibits glioblastoma (GBM) progression is not well understood. We aimed to determine the anti-tumor effect of NF on GBM cell lines and clarify the potential molecular mechanism involved.Methods U87MG and U251 cell lines were used in vitro to assess the anti-tumor efficacy of NF. Cytotoxicity, viability, and proliferation were evaluated by MTT and colony formation assay. After Annexin V-FITC and PI staining, flow cytometry was performed to evaluate apoptosis and cell cycle changes in NF-treated GBM cells. Wound healing and Transwell assays were used to assess migration and invasion of GBM cells. Western blot analysis, immunofluorescence staining, immunohistochemistry, and bioinformatics were used to gain insights into the molecular mechanisms. Preclinical therapeutic efficacy was mainly estimated by ultrasound and MRI in xenograft nude mouse models.Results NF inhibited the proliferation, mobility, stemness, angiogenesis, and epithelial-to-mesenchymal transition (EMT) of GBM cells. Additionally, NF induced apoptosis and G2 cell cycle arrest. Slug expression was also decreased by NF via the AKT and STAT3 signaling pathways. Interestingly, we discovered that NF affected GBM cells partly by targeting SOX2, which may be upstream of the AKT and STAT3 pathways. Finally, NF led to significant tumor control in GBM xenograft models.Conclusion sNF inhibited the progression of GBM via the SOX2-AKT/STAT3-Slug signaling pathway. SOX2-targeting with NF may offer a novel therapeutic approach for GBM treatment.
研究领域:
肿瘤学
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药理学
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神经科学
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分子生物学
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细胞生物学
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PubMed
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
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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）