Anti-allergic effects of sesquiterpene lactones from Saussurea costus (Falc.) Lipsch. determined using in vivo and in vitro experiments

Lee, Bo-Kyung; Park, Soojin; Nam, So‐Yeon; Kang, Su-Tae; Hwang, Jiyoung; Lee, Seung-Jin; Im, Dong‐Soon

doi:10.1016/j.jep.2017.11.018

Cited by 54 publications

(30 citation statements)

References 31 publications

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“…In particular, the increase of eosinophil count in BALF (bronchoalveolar lavage fluid) by OVA was significantly inhibited by costunolide. Moreover, the compound decreased the expression and secretion of Th2 cytokines (IL-4 and IL-13) in BALF and lung tissue [26]. Costunolide reduced the activity of β-hexosaminidase, an enzyme involved in mast cell degranulation, and decreased IL-4 mRNA transcript in IgE-sensitized rat basophilic leukemia (RBL-2H3) cells.…”

Section: Therapeutic Potential Of Costunolidementioning

confidence: 99%

Costunolide—A Bioactive Sesquiterpene Lactone with Diverse Therapeutic Potential

Kim

Choi

2019

IJMS

103

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Sesquiterpene lactones constitute a major class of bioactive natural products. One of the naturally occurring sesquiterpene lactones is costunolide, which has been extensively investigated for a wide range of biological activities. Multiple lines of preclinical studies have reported that the compound possesses antioxidative, anti-inflammatory, antiallergic, bone remodeling, neuroprotective, hair growth promoting, anticancer, and antidiabetic properties. Many of these bioactivities are supported by mechanistic details, such as the modulation of various intracellular signaling pathways involved in precipitating tissue inflammation, tumor growth and progression, bone loss, and neurodegeneration. The key molecular targets of costunolide include, but are not limited to, intracellular kinases, such as mitogen-activated protein kinases, Akt kinase, telomerase, cyclins and cyclin-dependent kinases, and redox-regulated transcription factors, such as nuclear factor-kappaB, signal transducer and activator of transcription, activator protein-1. The compound also diminished the production and/expression of proinflammatory mediators, such as cyclooxygenase-2, inducible nitric oxide synthase, nitric oxide, prostaglandins, and cytokines. This review provides an overview of the therapeutic potential of costunolide in the management of various diseases and their underlying mechanisms.

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Section: Therapeutic Potential Of Costunolidementioning

confidence: 99%

Costunolide—A Bioactive Sesquiterpene Lactone with Diverse Therapeutic Potential

Kim

Choi

2019

IJMS

103

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“…1A), which is extracted from various plant species, including genus Saussurea, Aucklandia and Inula (8)(9)(10). Costunolide exhibits a series of pharmacological activities, including anti-inflammatory (11), anti-allergic (12) and antimicrobial (13) effects. Notably, potent anticancer properties of costunolide have been identified in lung cancer and leukemia (14,15).…”

Section: Introductionmentioning

confidence: 99%

Costunolide induces apoptosis and inhibits migration and invasion in H1299 lung cancer cells

Wei

Qiu

et al. 2020

Oncol Rep

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Costunolide being a sesquiterpene lactone, is known to have anticancer properties. The present study investigated the anticancer effects of costunolide against the H1299 human non-small-cell lung cancer (NSCLC) cell line. Inhibition of cell viability by costunolide was assessed via a MTT assay. Furthermore, the apoptotic rate was detected using Annexin V/propidium iodide labeling. A colony forming cell assay was performed to investigate the antiproliferative effects of costunolide. Wound healing and Transwell assays were performed to determine the inhibitory effects of costunolide on migration and invasion, respectively. Western blot analysis was undertaken to determine protein expression, and reverse transcription-quantitative PCR was performed to assess mRNA expression levels. The results demonstrated that costunolide inhibited the viability of H1299 cells, with a half maximal inhibitory concentration value of 23.93±1.67 µM and induced cellular apoptosis in a dose-dependent manner. Furthermore, the colony formation, migrative and invasive abilities of the H1299 cells were inhibited in a dose-or time-dependent manner. The protein expression levels of E-cadherin increased and those of N-cadherin decreased following treatment with costunolide, which suggested that costunolide inhibited epithelial-to-mesenchymal transition. The mRNA levels of B-Raf, E-cadherin, N-cadherin, integrins α2 and β1, as well as matrix metalloproteinases 2 were also found to be regulated costunolide. These findings indicate the potential of costunolide in the treatment of NSCLC.

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“…Costunolide (CTL) is a principal active sesquiterpene lactone from medicinal plant Aucklandia lappa Decne [ 7 ]. CTL has been reported to exhibit various health benefits including anti-inflammatory [ 8 ], antioxidative [ 9 ], anticarcinogenic [ 10 , 11 , 12 ], and antiallergic properties [ 13 ]. Recently, the anti-inflammatory activity of CTL has especially attracted great attention.…”

Section: Introductionmentioning

confidence: 99%

Costunolide Plays an Anti-Neuroinflammation Role in Lipopolysaccharide-Induced BV2 Microglial Activation by Targeting Cyclin-Dependent Kinase 2

Liu

Feng

et al. 2020

Molecules

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Hyperactivation of microglia in the brain is closely related to neuroinflammation and leads to neuronal dysfunction. Costunolide (CTL) is a natural sesquiterpene lactone with wide pharmacological activities including anti-inflammation and antioxidation. In this study, we found that CTL significantly inhibited the production of inflammatory mediators including nitric oxide, IL-6, TNF-α, and PGE2 in lipopolysaccharide (LPS)-stimulated BV2 microglia. Moreover, CTL effectively attenuated IKKβ/NF-κB signaling pathway activation. To identify direct cellular target of CTL, we performed high-throughput reverse virtual screening assay using scPDB protein structure library, and found cyclin-dependent kinase 2 (CDK2) was the most specific binding protein for CTL. We further confirmed the binding ability of CTL with CDK2 using cellular thermal shift assay (CETSA) and drug affinity responsive target stability (DARTS) assays. Surface plasmon resonance analysis also supported that CTL specifically bound to CDK2 with a dissociation constant at micromole level. Furthermore, knocking down CDK2 obviously reversed the anti-inflammation effect of CTL via AKT/IKKβ/NF-κB signaling pathway on BV-2 cells. Collectively, these results indicate that CTL inhibits microglia-mediated neuroinflammation through directly targeting CDK2, and provide insights into the role of CDK2 as a promising anti-neuroinflammation therapeutic target.

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Anti-allergic effects of sesquiterpene lactones from Saussurea costus (Falc.) Lipsch. determined using in vivo and in vitro experiments

Cited by 54 publications

References 31 publications

Costunolide—A Bioactive Sesquiterpene Lactone with Diverse Therapeutic Potential

Costunolide—A Bioactive Sesquiterpene Lactone with Diverse Therapeutic Potential

Costunolide induces apoptosis and inhibits migration and invasion in H1299 lung cancer cells

Costunolide Plays an Anti-Neuroinflammation Role in Lipopolysaccharide-Induced BV2 Microglial Activation by Targeting Cyclin-Dependent Kinase 2

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