Inhibition of Pro‐Inflammatory Functions of Human Neutrophils by Constituents of <i>Melodorum fruticosum</i> Leaves

Engels, Nora S.; Waltenberger, Birgit; Michalak, Barbara; Huynh, Loi; Tran, Hung; Kiss, Anna K.; Stuppner, Hermann

doi:10.1002/cbdv.201800269

Cited by 7 publications

(4 citation statements)

References 55 publications

(61 reference statements)

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“…As 10 μM (−)-NRG-DM did not affect TRPA1 currents, the neuronal desensitization could not be ascribed to its modulation on the channels ( Figure S1 ). The suppression of neuron activity produced by (−)-NRG-DM is in agreement with the study of (+)-naringenin 4′,7-dimethyl ether ((+)-NRG-DM), a naturally occurring naringenin derivative that has been isolated many times from plants, that showed analgesic activity in vivo and that did not influence the production and release of pro-inflammatory factors compared to other naringenin derivatives [ 44 ]. Additionally, radioligand binding assay demonstrated that (+)-NRG-DM does not show affinity to endocannabinoid or opioid receptors [ 22 ].…”

Section: Discussionsupporting

confidence: 85%

(−)-Naringenin 4′,7-dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain through Inhibition of Multiple Channels

Meng

Zhang

et al. 2022

Molecules

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(−)-Naringenin 4′,7-dimethyl ether ((−)-NRG-DM) was isolated for the first time by our lab from Nardostachys jatamansi DC, a traditional medicinal plant frequently used to attenuate pain in Asia. As a natural derivative of analgesic, the current study was designed to test the potential analgesic activity of (−)-NRG-DM and its implicated mechanism. The analgesic activity of (−)-NRG-DM was assessed in a formalin-induced mouse inflammatory pain model and mustard oil-induced mouse colorectal pain model, in which the mice were intraperitoneally administrated with vehicle or (−)-NRG-DM (30 or 50 mg/kg) (n = 10 for each group). Our data showed that (−)-NRG-DM can dose dependently (30~50 mg/kg) relieve the pain behaviors. Notably, (−)-NRG-DM did not affect motor coordination in mice evaluated by the rotarod test, in which the animals were intraperitoneally injected with vehicle or (−)-NRG-DM (100, 200, or 400 mg/kg) (n = 10 for each group). In acutely isolated mouse dorsal root ganglion neurons, (−)-NRG-DM (1~30 μM) potently dampened the stimulated firing, reduced the action potential threshold and amplitude. In addition, the neuronal delayed rectifier potassium currents (IK) and voltage-gated sodium currents (INa) were significantly suppressed. Consistently, (−)-NRG-DM dramatically inhibited heterologously expressed Kv2.1 and Nav1.8 channels which represent the major components of the endogenous IK and INa. A pharmacokinetic study revealed the plasma concentration of (−)-NRG-DM is around 7 µM, which was higher than the effective concentrations for the IK and INa. Taken together, our study showed that (−)-NRG-DM is a potential analgesic candidate with inhibition of multiple neuronal channels (mediating IK and INa).

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Section: Discussionsupporting

confidence: 85%

(−)-Naringenin 4′,7-dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain through Inhibition of Multiple Channels

Meng

Zhang

et al. 2022

Molecules

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“…All the spectroscopic data are compatible with the structure of 4 -hydroxy-5,7-dimethoxyflavanone, also named naringenin 5,7-dimethyl ether. Although compound 5 is not new, [50,51], to the best of our knowledge, the full spectroscopic data are reported here for the first time.…”

Section: Chalcones and Flavanones Synthesismentioning

confidence: 87%

Chalcones and Flavanones Bearing Hydroxyl and/or Methoxyl Groups: Synthesis and Biological Assessments

et al. 2019

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Chalcones and flavanones are isomeric structures and also classes of natural products, belonging to the flavonoid family. Moreover, their wide range of biological activities makes them key scaffolds for the synthesis of new and more efficient drugs. In this work, the synthesis of hydroxy and/or methoxychalcones was studied using less common bases, such as sodium hydride (NaH) and lithium bis(trimethylsilyl)amide (LiHMDS), in the aldol condensation. The results show that the use of NaH was more effective for the synthesis of 2 -hydroxychalcone derivatives, while LiHMDS led to the synthesis of polyhydroxylated chalcones in a one-pot process. During this study, it was also possible to establish the conditions that favor their isomerization into flavanones, allowing at the same time the synthesis of hydroxy and/or methoxyflavanones. The chalcones and flavanones obtained were evaluated to disclose their antioxidant, anticholinesterasic, antibacterial and antitumor activities. 2 ,4 ,4-Trihydroxychalcone was the most active compound in terms of antioxidant, anti-butyrylcholinesterase (IC 50 26.55 ± 0.55 µg/mL, similar to control drug donepezil, IC 50 28.94 ± 1.76 µg/mL) and antimicrobial activity. 4 ,7-Dihydroxyflavanone presented dual inhibition, that is, the ability to inhibit both cholinesterases. 4 -Hydroxy-5,7-dimethoxyflavanone and 2 -hydroxy-4-methoxychalcone were the compounds with the best antitumor activity. The substitution pattern and the biological assay results allowed the establishment of some structure/activity relationships.

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“…The anti-inflammatory potency and efficacy of the tested compounds can be evaluated based on the IC 50 value of positive controls. For example, a well-known anti-inflammatory natural compound, quercetin, has shown an IC 50 value of 10 µM for the inhibition of TNF-α production [31], and indomethacin, one of the NSAIDs drug, has been found to inhibit PGE2 production with IC 50 = 0.45 µM [32]. Although the IC 50 value was not measured in this study, the anti-inflammatory activity of 1-3 was moderate at a concentration of 10 µM or higher compared with other anti-inflammatory agents in previous studies.…”

Section: Nf-κb Target Gene Expressionmentioning

confidence: 99%

Anti-Inflammatory Activity of the Constituents from the Leaves of Perilla frutescens var. acuta

Youn,

Han,

Jung

et al. 2023

Pharmaceuticals

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Perilla frutense var. acuta (Lamiaceae) has been used to treat indigestion, asthma, and allergies in traditional medicine. In this study, luteolin 7-O-diglucuronide (1), apigenin 7-O-diglucuronide (2), and rosmarinic acid (3) were isolated from the leaves of P. frutescens var. acuta through various chromatographic purification techniques. Several approaches were used to investigate the anti-inflammatory activity of the constituents (1–3) and their working mechanisms. In silico docking simulation demonstrated that 1–3 would work as a PPAR-α/δ/γ agonist, and in vitro PPAR-α/δ/γ transcriptional assay showed that the Perilla water extract (PWE) and 3 increased PPAR-α luciferase activity (1.71 and 1.61 times of the control (PPAR-α + PPRE, p < 0.001)). In the NF-κB luciferase assay, 1 suppressed NF-κB activity the most (56.83% at 5 µM; 74.96% at 10 µM; 79.86% at 50 µM). In addition, 1 and 2 inhibited the mRNA expression of NF-κB target genes, including Il6, Mcp1, and Tnfa, at 50 µM, and 3 suppressed the genes at the mRNA level in a dose-dependent manner. We report that 1 and 2 exert anti-inflammatory effects through NF-κB inhibition, and the PPAR-α/NF-κB signaling pathway is related to the anti-inflammatory activity of 3.

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Inhibition of Pro‐Inflammatory Functions of Human Neutrophils by Constituents of Melodorum fruticosum Leaves

Cited by 7 publications

References 55 publications

(−)-Naringenin 4′,7-dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain through Inhibition of Multiple Channels

(−)-Naringenin 4′,7-dimethyl Ether Isolated from Nardostachys jatamansi Relieves Pain through Inhibition of Multiple Channels

Chalcones and Flavanones Bearing Hydroxyl and/or Methoxyl Groups: Synthesis and Biological Assessments

Anti-Inflammatory Activity of the Constituents from the Leaves of Perilla frutescens var. acuta

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