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Cat. No.: HY-N21818

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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.

For research use only. We do not sell to patients.

CAS No.: 172854-76-1
Formula: C₂₅H₃₆O₄
Molecular Weight:400.55

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Cacospongionolide B Chemical Structure

CAS No.: 172854-76-1

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

sPLA2

4.3 μM (IC₅₀)

iNOS

COX-2

TNF-α

All Phospholipase Isoforms :

All NO Synthase Isoforms :

All COX Isoforms :

All TNF Receptor Isoforms :

In Vitro

Bacterial InfectionCytokines & ChemokinesLipid Inflammatory MediatorsInnate Immunity

Bacterial Infection

Cacospongionolide B potently inhibits the growth of Bacillus subtilis and Micrococcus luteus, with an MIC of 0.78 μg/mL for both strains^[1].

Cytokines & Chemokines

Lipid Inflammatory Mediators

Innate Immunity

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].

Innate Immunity

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.

Western Blot Analysis^[1]

Cell Line:

Mouse peritoneal macrophages
Concentration:

0.5 μM, 1 μM, 5 μM
Incubation Time:

30 min pre-incubation followed by 60 min to 18 h reaction
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

Innate ImmunityCytokines & ChemokinesLipid Inflammatory Mediators

Innate Immunity

Cytokines & Chemokines

Lipid Inflammatory Mediators

Cacospongionolide B (50-100 nmol/pouch; administered into the air pouch; single injection; 2-12 h) reduces TNF-α release and inhibits leukocyte infiltration in a zymosan-induced mouse air pouch inflammation model^[2].

Innate Immunity

Lipid Inflammatory Mediators

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].

Innate Immunity

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.

Animal Model:

CD-1 (female, 25-30 g)^[2]
Dosage:

50 nmol/pouch (2-hour assessment; 12-hour assessment); 100 nmol/pouch (2-hour assessment; 12-hour assessment)
Administration:

o.a.; single dose (2-hour assessment); initial dose followed by second dose 8 hours later (12-hour assessment)
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.

Animal Model:

Swiss mice (20-25 g, TPA-induced ear oedema model)^[3]
Dosage:

50 μg ear^-1; 100 μg ear^-1
Administration:

topical; single dose; processed 4 h after TPA administration
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.

Animal Model:

Swiss mice (female, 20-25 g, carrageenin-induced paw oedema model)^[3]
Dosage:

5 mg/kg; 10 mg/kg; 20 mg/kg
Administration:

p.o.; single dose; observed up to 5 h post-induction
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.

Animal Model:

Lewis rats (female, 126-150 g, adjuvant-induced arthritis model)^[3]
Dosage:

20 mg/kg
Administration:

p.o.; once daily; 5 days; total 18 days
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.

Related Protocols :

Chemical Information

CAS No. 172854-76-1
Molecular Weight 400.55
Formula C₂₅H₃₆O₄
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
Structure Classification
- Terpenoids
- Sesquiterpenes
Initial Source
- Microorganism
Fasciospongia cavernosa
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. De Rosa S, et al. Cacospongionolide B, a new sesterterpene from the sponge Fasciospongia cavernosa. Journal of natural products. 1995 Nov;58(11):1776-80.

[2]. Posadas I, et al. Cacospongionolide B suppresses the expression of inflammatory enzymes and tumour necrosis factor-alpha by inhibiting nuclear factor-kappa B activation. British journal of pharmacology. 2003 Apr;138(8):1571-9.

[3]. García Pastor P, et al. Modulation of acute and chronic inflammatory processes by cacospongionolide B, a novel inhibitor of human synovial phospholipase A2. British journal of pharmacology. 1999 Jan;126(1):301-11.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Cacospongionolide B

All Phospholipase Isoforms

All NO Synthase Isoforms

All COX Isoforms

All TNF Receptor Isoforms