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Chemical Structure| 553-21-9 Chemical Structure| 553-21-9

Structure of Costunolide
CAS No.: 553-21-9

Chemical Structure| 553-21-9

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CAS No.: 553-21-9

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Costunolide shows anti-inflammatory and anti-oxidant activities and also induces apoptosis. It is a sesquiterpene lactone isolated from stem bark of Magnolia sieboldii,

Synonyms: Costus lactone; Melampolide; CCRIS 6754

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Product Citations

Product Citations

Krueger, Nadine ; Kronenberger, Thales ; Xie, Hang ; Rocha, Cheila ; Poehlmann, Stefan ; Su, Haixia , et al.

Abstract: The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has forced the development of direct-acting antiviral drugs due to the coronavirus disease 2019 (COVID-19) pandemic. The main protease of SARS-CoV-2 is a crucial enzyme that breaks down polyproteins synthesized from the viral RNA, making it a validated target for the development of SARS-CoV-2 therapeutics. New chem. phenotypes are frequently discovered in natural goods. In the current study, we used a fluorogenic assay to test a variety of natural products for their ability to inhibit SARS-CoV-2 Mpro. Several compounds were discovered to inhibit Mpro at low micromolar concentrations It was possible to crystallize robinetin together with SARS-CoV-2 Mpro, and the X-ray structure revealed covalent interaction with the protease's catalytic Cys145 site. Selected potent mols. also exhibited antiviral properties without cytotoxicity. Some of these powerful inhibitors might be utilized as lead compounds for future COVID-19 research.

Keywords: COVID-19 ; antivirals ; coronavirus ; covalent drugs ; dynamic light scattering ; inhibitors ; main protease ; natural products

Alternative Products

Product Details of Costunolide

CAS No. :553-21-9
Formula : C15H20O2
M.W : 232.32
SMILES Code : O=C(O[C@@]1([H])[C@@]2([H])CC/C(C)=C/CC/C(C)=C/1)C2=C
Synonyms :
Costus lactone; Melampolide; CCRIS 6754
MDL No. :MFCD00210262

Safety of Costunolide

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H317-H319-H335
Precautionary Statements:P261-P280-P305+P351+P338

Related Pathways of Costunolide

DNA

Isoform Comparison

Biological Activity

Target

  • Telomerase

    Telomerase (MDA-MB-231), IC50:65 μM

    Telomerase (MCF-7), IC50:90 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
RAW264.7 cells (mouse macrophage cell line) 2.5, 5, 10 μM 1 h pretreatment, followed by stimulation for 6 h CTD dose-dependently reduced oxLDL-induced NF-κB activity, as validated in RAW264.7 cells stably expressing NF-κB EGFP reporter. PMC9813247
Mouse primary peritoneal macrophages (MPMs) 2.5, 5, 10 μM 1 h pretreatment, followed by stimulation for 6 or 24 h CTD pretreatment significantly inhibited oxLDL-induced inflammatory responses, including reducing mRNA and protein levels of pro-inflammatory cytokines (TNF-α, IL-6), decreasing transcriptional levels of chemokines and adhesion molecules, and suppressing oxLDL uptake and foam cell formation. PMC9813247
JB6 cells 5, 10, 20 μM 14 days Assess the inhibitory effect of COS on TPA-induced cell transformation, showing concentration-dependent inhibition of cell transformation and proliferation. PMC11927231
JB6 cells 5, 10, 20 μM 18 hours Evaluate the effect of COS on the cell cycle, showing induction of G2/M phase cell cycle arrest. PMC11927231
Primary rat hepatic stellate cells 10, 20, 30 μM 24 hours To evaluate the effects of Costunolide on HSC activation and glycolysis. Results showed that Costunolide reduced HSC viability, inhibited the expression of α-SMA and collagen I, decreased glucose uptake and consumption, reduced lactate levels, and suppressed HK2 expression and activity. PMC6694499
T98G 30 μM 24 hours Costunolide had no effect on the viability of p53 mutant glioma cell T98G. PMC4917655
U87MG 30 μM 24 hours Costunolide induced glioma cell apoptosis in an ROS-dependent manner, increased p53 levels, and abrogated telomerase activity. PMC4917655
A172 30 μM 24 hours Costunolide induced glioma cell apoptosis in an ROS-dependent manner, increased p53 levels, and abrogated telomerase activity. PMC4917655
Human erythrocytes 1-80 μM 24 hours To investigate the effects of Costunolide on eryptosis, results showed that Costunolide dose-dependently increased phosphatidylserine exposure and cell shrinkage, and completely inhibited G6PDH activity. PMC7527323
JB6 cells 5, 10, 20 μM 24 hours Evaluate the effect of COS on apoptosis, showing a concentration-dependent increase in apoptotic cell proportion. PMC11927231
SH-SY5Y cells 50 μg/mL 24 hours Investigation of the neuroprotective effects of Costunolide against MPP+-induced cytotoxicity, showing that 50 μg/mL Costunolide significantly improved cell viability. PMC10093699
SH-SY5Y cells 100 μg/mL 24 hours Investigation of the neuroprotective effects of Costunolide against MPP+-induced cytotoxicity, showing that 100 μg/mL Costunolide significantly improved cell viability. PMC10093699
HOMF 20 μM 24 hours Evaluated in vitro toxicity PMC8305390
YD-9 39.6 μM (IC50) 24 hours Inhibited cell proliferation and induced apoptosis PMC8305390
Ca9-22 7.9 μM (IC50) 24 hours Inhibited cell proliferation and induced apoptosis PMC8305390
YD-10B 9.2 μM (IC50) 24 hours Inhibited cell proliferation and induced apoptosis PMC8305390
MCF-7 cells 15 μM 24 hours CTL activated PINK1/Parkin-dependent mitophagy to remove damaged mitochondria, preventing ROS elevation and reducing sensitivity to CTL. PMC9965698
SK-BR-3 cells 15 μM 24 hours CTL significantly increased intracellular ROS levels, leading to lysosomal membrane permeabilization and cathepsin D release, subsequently activating the mitochondrial-dependent apoptotic pathway. PMC9965698
A549 cells 0.39 μM, 1.56 μM, 6.26 μM, 25 μM, 100 μM 24 hours To evaluate the effect of CTD and CTD-GNE on the viability of A549 cells. CTD-GNE significantly reduced cell viability with an IC50 value of 6.1 ± 0.8 μM, while CTD had an IC50 value of 13.4 ± 1.5 μM. PMC8880633
JB6 cells 5, 10, 20 μM 24, 48 hours Evaluate the cytotoxicity of COS on JB6 cells, showing no cytotoxicity at all tested concentrations. PMC11927231
Bone marrow-derived macrophages (BMDMs) 1, 2, 5 μM 30 minutes Inhibited NLRP3 inflammasome activation, reduced IL-1β and p20 secretion PMC9978959
Alveolar macrophages (AMs) 10 μM 30 minutes Costunolide significantly inhibited HKSA-induced production of IL-6, TNF-α, IL-1β, and KC. PMC6786317
Mouse bone marrow-derived macrophages (BMDMs) 0, 3, 10, and 30 μM 30 minutes Costunolide significantly inhibited HKSA-induced production of IL-6, TNF-α, IL-1β, and KC in a dose-dependent manner. PMC6786317
HEKn cells 0.2, 0.4, 0.6, 0.8, 1 μM 48 hours Costunolide showed no significant impact on the viability of HEKn cells at concentrations below 1 μM. PMC7922093
A431 cells 0.2, 0.4, 0.6, 0.8, 1 μM 48 hours Costunolide significantly reduced the viability of A431 cells with an IC50 value of 0.8 μM. PMC7922093
H1975-Osi 0, 5, 10, 20 μM 6 hours Inhibited the kinase activity of MEK1 and AKT1/2, restrained downstream ERK-RSK2 and GSK3β signal transduction and significantly induced cell apoptosis PMC9535870
HCC827-Osi 0, 5, 10, 20 μM 6 hours Inhibited the kinase activity of MEK1 and AKT1/2, restrained downstream ERK-RSK2 and GSK3β signal transduction and significantly induced cell apoptosis PMC9535870
PC9-Osi 0, 5, 10, 20 μM 6 hours Inhibited the kinase activity of MEK1 and AKT1/2, restrained downstream ERK-RSK2 and GSK3β signal transduction and significantly induced cell apoptosis PMC9535870
MDA-MB-436 10 μM, 25 μM 6 hours Costunolide significantly reduced detyrosinated tubulin levels without inducing apoptosis. PMC3979133
Bt-549 10 μM, 25 μM 6 hours Costunolide significantly reduced detyrosinated tubulin levels without inducing apoptosis. PMC3979133
MDA-MB-157 10 μM, 25 μM 6 hours Costunolide significantly reduced detyrosinated tubulin levels without inducing apoptosis. PMC3979133

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
ICR female mice DMBA/TPA-induced skin cancer model Topical administration 0.5 μmol/200 μL, 1 μmol/200 μL Twice a week for 21 weeks Evaluate the preventive effect of COS on skin cancer, showing significant reduction in papilloma formation and inhibition of tissue hyperplasia. PMC11927231
Nude mice Cell-derived xenograft model Intraperitoneal injection 10 mg/kg Once every two days for 21 days Inhibited tumor growth PMC8305390
ApoE?/? mice High-fat diet-induced atherosclerosis model Intragastric administration 10, 20 mg/kg Every 2 days for 8 weeks CTD dose-dependently alleviated atherosclerosis in HFD-fed ApoE?/? mice, reducing aortic plaque area and collagen deposition, inhibiting infiltration of inflammatory cells (macrophages, neutrophils, monocytes), and decreasing expression of pro-inflammatory cytokines (TNF-α, IL-6). PMC9813247
NOD/SCID mice HLG57-Osi PDX model Oral 20 mg/kg Once daily, continuous treatment Costunolide inhibited tumor growth, and combination treatment with osimertinib showed a more obvious growth inhibitory effect PMC9535870
C57BL/6J mice HKSA-induced acute lung injury model Intraperitoneal injection 30 mg/kg Single dose, evaluated after 8 hours Costunolide significantly attenuated HKSA-induced lung tissue damage, reduced lung edema and neutrophil infiltration, and significantly decreased the production of pro-inflammatory cytokines. PMC6786317
C57BL/6J mice Gouty arthritis model Intraperitoneal injection 40 mg/kg Twice, 30 minutes apart Reduced joint swelling, decreased IL-1β and p20 production PMC9978959
Nude mice Heterotypic xenograft glioma mouse model Intraperitoneally 5 mg/kg Every alternate day for 20 days Costunolide significantly reduced tumor volume and weight, downregulated telomerase activity, increased ROS levels, and elevated caspase 3/8 activity. PMC4917655
Sprague-Dawley rats Bile duct ligation (BDL)-induced hepatic fibrosis model Oral gavage 80 mg/kg Once daily for 14 days COS administration significantly attenuated hepatic histopathological injury and collagen accumulation and reduced the expression of fibrogenic genes. PMC6989949

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.30mL

0.86mL

0.43mL

21.52mL

4.30mL

2.15mL

43.04mL

8.61mL

4.30mL

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