A tryptamine-paeonol hybridization compound inhibits LPS-mediated inflammation in BV2 cells

Jung, Eun Hye; Hwang, Ji Sun; Kwon, Mi Youn; Kim, Kyung Hong; Cho, Hyeongjin; Lyoo, In Kyoon; Shin, Soo Jai; Park, Jeong Ho; Han, Inn Oc

doi:10.1016/j.neuint.2016.08.010

Cited by 16 publications

(7 citation statements)

References 22 publications

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“…The JAK-STAT signal pathway plays myriad and pivotal roles in the immune and inflammatory responses (17). We have previously shown that inhibition of STAT signaling reduces iNOS expression and that the inhibition of NF-κB, in turn, inhibits the activation of STAT3 and completely suppresses iNOS induction in response to LPS in BV2 cells (18). This suggests that that STAT3 is one of the many downstream targets of NF-κB that regulates iNOS transcription.…”

Section: Discussionmentioning

confidence: 99%

An alpha-lipoic acid-decursinol hybrid compound attenuates lipopolysaccharide-mediated inflammation in BV2 and RAW264.7 cells

et al. 2019

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In this study, the anti-inflammatory effects of α-lipoic acid (LA) and decursinol (Dec) hybrid compound LA-Dec were evaluated and compared with its prodrugs, LA and Dec. LA-Dec dose-dependently inhibited lipopolysaccharide (LPS)-induced nitric oxide (NO) generation in BV2 mouse microglial cells. On the other hand, no or mild inhibitory effect was shown by the Dec and LA, respectively. LA-Dec demonstrated dose-dependent protection from activation-induced cell death in BV2 cells. LA-Dec, but not LA or Dec individually, inhibited LPS-induced increased expressions of induced NO synthase (iNOS) and cyclooxygenase-2 (COX-2) proteins in a dose-dependent manner in both BV2 and mouse macrophage, RAW264.7 cells. Furthermore, LA-Dec inhibited LPS-induced expressions of iNOS, COX-2, interleukin-6, tumor necrosis factor-α, and interleukin-1β mRNA in BV2 cells, whereas the same concentration of LA or Dec was ineffective. Signaling studies demonstrated that LA-Dec inhibited LPS-activated signal transducer and activator of transcription 3 and protein kinase B activation, but not nuclear factor-kappa B or mitogen-activated protein kinase signaling. The data implicate LA-Dec hybrid compound as a potential therapeutic agent for inflammatory diseases of the peripheral and central nervous systems.

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Section: Discussionmentioning

confidence: 99%

An alpha-lipoic acid-decursinol hybrid compound attenuates lipopolysaccharide-mediated inflammation in BV2 and RAW264.7 cells

et al. 2019

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“…In this study, the inhibitory effects of geldanamycin derivatives on the productions of proinflammatory cytokines and mediators in LPS-stimulated RAW 264.7 cells were more potent than that of geldanamycin. A literaure review revealed only one study of the anti-inflammotry effects of tryptamine hybrid compounds [71]. The reason for this phenomenon is due to tryptamine group could synergize with geldanamycin in the inhibitory effects on production of inflammatory mediators and proinflammatory cytokines in LPS-stimulated RAW 264.7 cells.…”

Section: Discussionmentioning

confidence: 99%

Anti-Inflammatory Activity of Geldanamycin and Its Derivatives in LPS-Induced RAW 264.7 Cells

Taechowisan¹,

Puckdee²,

Waratchareeyakul³

et al. 2019

AiM

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Geldanamycin (1) had been isolated as a major compound from Streptomyces zerumbet W14; an endophyte of Zingiber zerumbet (L.) Smith. Two new geldanamycin derivatives; 17-(tryptamine)-17-demethoxygeldanamycin (2) and 17-(5'-methoxytryptamine)-17-demethoxygeldanamycin (3) were synthesized and their anti-inflammatory activity was evaluated in LPS-induced macrophage RAW 264.7 cells by investigating their effects on the inhibition of production of NO, PGE 2 , TNF-α, IL-1β, IL-6 and IL-10. The data obtained were consistent with the modulation of TNF-α, IL-1β, IL-6, IL-10 production by these derivatives at concentration of 1 to 5 µg/ml. A similar effect was also observed when LPS-induced NO release and PGE 2 production were tested. The inhibitory effects were shown in concentration-dependent manners. From the obtained results, it was concluded that two new geldanamycin derivatives possess anti-inflammatory activity on LPS-induced RAW 264.7 cells. They could be useful for the management of inflammatory diseases.

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“…Paeonol (2′-hydroxy-4′-methoxyacetophenone) appeared to be the main representative bioactive compound in paeonol [ 18 , 19 ] and till today, twelve derivatives of paeonol have been synthesized ( Figure 1 ). Among bioactive compounds derived from Cortex Moutan, paeonol has been extensively investigated for anti-cardiovascular activity and its mechanisms of action in CVD [ 20 , 21 , 22 , 23 , 24 , 25 , 26 , 27 , 28 , 29 , 30 ].…”

Section: Pharmacological Features Of Paeonolmentioning

confidence: 99%

Biological Activities of Paeonol in Cardiovascular Diseases: A Review

et al. 2021

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Paeonol is a naturally existing bioactive compound found in the root bark of Paeonia suffruticosa and it is traditionally used in Chinese medicine for the prevention and management of cardiovascular diseases. To date, a great deal of studies has been reported on the pharmacological effects of paeonol and its mechanisms of action in various diseases and conditions. In this review, the underlying mechanism of action of paeonol in cardiovascular disease has been elucidated. Recent studies have revealed that paeonol treatment improved endothelium injury, demoted inflammation, ameliorated oxidative stress, suppressed vascular smooth muscle cell proliferation, and repressed platelet activation. Paeonol has been reported to effectively protect the cardiovascular system either employed alone or in combination with other traditional medicines, thus, signifying it could be a hypothetically alternative or complementary atherosclerosis treatment. This review summarizes the biological and pharmacological activities of paeonol in the treatment of cardiovascular diseases and its associated underlying mechanisms for a better insight for future clinical practices.

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A tryptamine-paeonol hybridization compound inhibits LPS-mediated inflammation in BV2 cells

Cited by 16 publications

References 22 publications

An alpha-lipoic acid-decursinol hybrid compound attenuates lipopolysaccharide-mediated inflammation in BV2 and RAW264.7 cells

An alpha-lipoic acid-decursinol hybrid compound attenuates lipopolysaccharide-mediated inflammation in BV2 and RAW264.7 cells

Anti-Inflammatory Activity of Geldanamycin and Its Derivatives in LPS-Induced RAW 264.7 Cells

Biological Activities of Paeonol in Cardiovascular Diseases: A Review

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