Cacospongionolide B
Cacospongionolide B is an orally active sesterterpene compound that can be isolated from Fasciospongia cavernosa. Cacospongionolide B is a secreted phospholipase A2 (sPLA2) inhibitor with an IC50 of 4.3 μM. Cacospongionolide B exhibits antibacterial activity. Cacospongionolide B downregulates the expression of iNOS, COX-2 and TNF-α by inhibiting NF-κB nuclear translocation and its DNA binding, and simultaneously selectively and irreversibly inhibits sPLA2 enzymatic activity. Cacospongionolide B can be used in studies related to bacterial infection and adjuvant arthritis.
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- CAS No.: 172854-76-1
- Formule: C25H36O4
- Masse moléculaire:400.55
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
sPLA2 4.3 μM (IC50) |
iNOS |
COX-2 |
TNF-α |
In Vitro
Cacospongionolide B potently inhibits the growth of Bacillus subtilis and Micrococcus luteus, with an MIC of 0.78 μg/mL for both strains[1].
Cacospongionolide B (0.5-5 μM; 2-18 h) concentration-dependently reduces the release of TNF-α (IC50 = 260 nM), Nitrite (IC50 = 330 nM), and PGE2 (IC50 = 197 nM), inhibits the protein expression of iNOS and COX-2, significantly decreases TNF-α mRNA expression, suppresses NF-κB DNA-binding activity, blocks the nuclear translocation of the p65 subunit, and interferes with the phosphorylation of IκB-α at serine 32 in Zymosan (HY-159069)-stimulated mouse peritoneal macrophages; it also reduces the production of TNF-α and PGE2 in Zymosan-stimulated human monocytes[2].
Cacospongionolide B irreversibly and selectively inhibits sPLA2 in vitro, and exhibits the strongest inhibitory potency against human recombinant synovial sPLA2 (IC50 = 4.3 μM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse peritoneal macrophages
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Concentration:0.5 μM, 1 μM, 5 μM
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Incubation Time:30 min pre-incubation followed by 60 min to 18 h reaction
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Result:Decreased Zymosan-induced iNOS and COX-2 protein expression.
Retained the p65 subunit in the cytoplasm, preventing its nuclear translocation, while reducing IκB-α phosphorylation at Ser32 and increasing IκB-α expression in the NF-κB pathway.
In Vivo
Cacospongionolide B (50-100 μg/ear; topical application to the ear; single administration; 4 h treatment) exerts anti-inflammatory and anti-edema effects and reduces myeloperoxidase levels in a TPA (HY-18739)-induced mouse ear edema model[3].
Cacospongionolide B (20 mg/kg; oral administration; once daily from day 13 to day 17; treatment continues until day 18) reduces paw edema volume and inhibits sPLA2 activity to alleviate chronic inflammation in a Mycobacterium-induced rat adjuvant arthritis model[3].
Cacospongionolide B (5-20 mg/kg; oral administration; single dose) exerts significant anti-acute inflammatory and edema-reducing effects in a Carrageenan (HY-125474)-induced mouse paw edema model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 (female, 25-30 g)[2]
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Dosage:50 nmol/pouch (2-hour assessment; 12-hour assessment); 100 nmol/pouch (2-hour assessment; 12-hour assessment)
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Administration:o.a.; single dose (2-hour assessment); initial dose followed by second dose 8 hours later (12-hour assessment)
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Result:Reduced TNF-α levels in air pouch exudates at 2 hours post-zymosan administration, without significantly affecting leukocyte infiltration.
Reduced leukocyte infiltration, nitrite levels, and PGE2 levels in air pouch exudates at 12 hours post-zymosan administration.
Reduced iNOS and COX-2 protein expression in cells isolated from 12-hour zymosan-stimulated air pouch exudates.
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Animal Model:Swiss mice (20-25 g, TPA-induced ear oedema model)[3]
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Dosage:50 μg ear-1; 100 μg ear-1
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Administration:topical; single dose; processed 4 h after TPA administration
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Result:Achieved 43.4% oedema inhibition and 64.3% myeloperoxidase inhibition at 50 μg ear-1.
Achieved 54.6% oedema inhibition and 70.9% myeloperoxidase inhibition at 100 μg ear-1.
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Animal Model:Swiss mice (female, 20-25 g, carrageenin-induced paw oedema model)[3]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:p.o.; single dose; observed up to 5 h post-induction
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Result:Significantly reduced paw oedema at 1 and 3 hours at 5 mg/kg.
Significantly reduced paw oedema at 1, 3, and 5 hours at 10 mg/kg.
Significantly reduced paw oedema at 1, 3, and 5 hours at 20 mg/kg.
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Animal Model:Lewis rats (female, 126-150 g, adjuvant-induced arthritis model)[3]
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Dosage:20 mg/kg
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Administration:p.o.; once daily; 5 days; total 18 days
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Result:Significantly reduced mean paw oedema on days 15 and 18.
Significantly inhibited elevated sPLA2 activity in paw homogenates.
Did not modify eicosanoid levels in serum, stomach, or paw homogenates.
Caused no toxic effects in treated rats.
Chemical Information
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CAS No. 172854-76-1
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Masse moléculaire 400.55
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Formule C25H36O4
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SMILES
O=C(O[C@H]1O)C=C1[C@H](OC2)CC=C2CC[C@@]3([C@]4([H])[C@@](CC[C@@H]3C)(C(CCC4)=C)C)C
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Structure Classification
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Initial Source
Fasciospongia cavernosa
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Cacospongionolide B Related Classifications
HY-N21818 Related Classifications
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