Casuarinin 

Casuarinin is an orally active antiproliferative, anti-inflammatory, antifungal, virucidal and gastroprotective agent. Casuarinin upregulates the expression of p21/WAF1, Fas/APO‑1, mFasL, sFasL and HSP‑70, arrests cell cycle, induces apoptosis and inhibits cancer cell proliferation. Casuarinin inhibits TNF‑α-induced phosphorylation of MAPK and activation of NF‑κB, downregulates the expression of iNOS, NF‑κB, COX‑2 and ICAM‑1, and reduces the production of proinflammatory mediators. Casuarinin attenuates ethanol-induced activation of caspase‑3 and elevation of TNF‑α, inhibits the growth of Candida albicans, and inhibits HSV‑2. Casuarinin can be used in research related to mammary adenocarcinoma, inflammatory skin diseases, gastric ulcers, candidiasis and herpes simplex virus infections^{[1][2][3][4][5]}.

Casuarinin (0.5-10 μM; 48 h) dose-dependently inhibits the proliferation of human breast adenocarcinoma MCF-7 cells with an IC₅₀ of 6.04 μM^[1].
Casuarinin (5-10 μM; 24 h) induces G0/G1 phase cell cycle arrest in human breast adenocarcinoma MCF-7 cells^[1].
Casuarinin (0.5-10 μM; 48 h) increases the percentage of apoptotic nuclei in human breast adenocarcinoma MCF-7 cells in a dose-independent manner^[1].
Casuarinin (5-10 μM; 6-48 h) time- and dose-dependently induces DNA fragmentation and apoptosis in human breast adenocarcinoma MCF-7 cells, with maximal effects observed at 48 h, while showing no effect on p53 protein expression at concentrations up to 10 μM within 48 h; it also time- and dose-dependently upregulates p21/WAF1, Fas/APO-1 receptor, mFasL and sFasL expression, with maximal induction detected at 24 h^[1].
Casuarinin (10 μM; 48 h) exerts antiproliferative and proapoptotic effects in human breast adenocarcinoma MCF-7 cells, and these effects are significantly attenuated by pre-incubation with 250 ng/mL ZB4 (to block the Fas/FasL system) or 10 μM Z-IETD-FMK (to inhibit caspase-8) for 1 h prior to treatment^[1].
Casuarinin (10 μM; 48 h, preceded by 1 h pre-incubation with 10 μM Z-IETD-FMK) has its antiproliferative and proapoptotic effects significantly reduced by blocking caspase-8 with Z-IETD-FMK in human breast adenocarcinoma MCF-7 cells after 48 h^[1].
Casuarinin (5-10 μM; 12-48 h) time- and dose-dependently activates caspase-8 in human breast adenocarcinoma MCF-7 cells^[1].
Casuarinin (5-20 μg/mL; 1 h pretreatment) dose-dependently inhibits TNF-α-induced ICAM-1 mRNA and protein expression in HaCaT human keratinocyte cells prior to TNF-α stimulation^[2].
Casuarinin (5-20 μg/mL) dose-dependently reduces TNF-α-induced THP-1 monocyte adhesion to HaCaT human keratinocyte cells^[2].
Casuarinin (5-20 μg/mL) blocks TNF-α-induced NF-κB activation in HaCaT human keratinocyte cells by inhibiting IκBα degradation, p65 phosphorylation and nuclear translocation, NF-κB DNA binding, and NF-κB promoter activity^[2].
Casuarinin (5-20 μg/mL) dose-dependently inhibits TNF-α-induced phosphorylation of ERK and p38 MAPK (but not JNK) in HaCaT human keratinocyte cells, and also suppresses TNF-α-induced mRNA and protein expression of IL-6, IL-1β, IL-8, and MCP-1 in a concentration-dependent manner in the same cell line^[2].
Casuarinin (24-48 h) exhibits antifungal activity against Candida albicans ATCC 64548, Candida albicans SC5314, Candida krusei ATCC 6258, Candida parapsilosis ATCC 22019, and Candida tropicalis ATCC 750, with the lowest MIC of 26 μg/mL against Candida krusei ATCC 6258^[4].
Casuarinin (72 h) potently inhibits HSV-2 growth in Vero cells with an IC₅₀ of 3.6 μM, has a CC₅₀ of 89 μM in Vero cells, and exhibits a selectivity index of 25 in the XTT assay^[5].
Casuarinin (1 h adsorption, 2 days total post-overlay) inhibits HSV-2 plaque formation in Vero cells with an IC₅₀ of 1.5 μM and exhibits a selectivity index of 59 in the plaque reduction assay^[5].
Casuarinin (0.5-50 μM; 6 h) exhibits potent virucidal activity against cell-free HSV-2 at 25 μM^[5].
Casuarinin (10 μM; added 0-12 h post-infection, total 24 h infection time) inhibits HSV-2 yield in Vero cells by at least 90% even when added up to 12 h post-infection, indicating activity against late events of HSV-2 infection^[5].
Casuarinin (3 h at 4°C, 48 h total post-overlay) inhibits HSV-2 attachment to Vero cells in a dose-dependent manner^[5].
Casuarinin (10 μM; added after 3 h attachment, evaluated 10-minute intervals post-warming) inhibits HSV-2 penetration into Vero cells by over 85% within 10 minutes of treatment^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Casuarinin (25-100 mg/kg; p.o.; single dose) exhibits dose-dependent gastroprotective activity against ethanol-induced gastric ulcer in male Sprague Dawley rats, with the 100 mg/kg dose providing 98.90% ulcer area reduction, restoring oxidative stress, inflammatory, apoptotic, and histopathological parameters to near-normal levels^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

936.65

C₄₁H₂₈O₂₆

79786-01-9

Solid

Light yellow to light brown

OC1=C(O)C(O)=C(C2=C(C(O3)=O)C=C(O)C(O)=C2O)C(C(OC[C@@H](OC(C4=CC(O)=C(O)C(O)=C4)=O)[C@@H]3[C@H](OC(C5=C6C(O)=C(O)C(O)=C5)=O)[C@@H](O7)[C@@H](O)C8=C(C6=C(O)C(O)=C8O)C7=O)=O)=C1

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [1]. Kuo PL, et al. Casuarinin from the bark of Terminalia arjuna induces apoptosis and cell cycle arrest in human breast adenocarcinoma MCF-7 cells. Planta Med. 2005;71(3):237-243.  [Content Brief]

  [2]. Kwon DJ, et al. Casuarinin suppresses TNF-α-induced ICAM-1 expression via blockade of NF-κB activation in HaCaT cells. Biochem Biophys Res Commun. 2011;409(4):780-785.  [Content Brief]

  [3]. Al-Sayed E, et al. Protective Role of Casuarinin from Melaleuca leucadendra against Ethanol-Induced Gastric Ulcer in Rats. Planta Med. 2020;86(1):32-44.  [Content Brief]

  [4]. Souza-Moreira TM, et al. Anti-Candida targets and cytotoxicity of casuarinin isolated from Plinia cauliflora leaves in a bioactivity-guided study. Molecules. 2013;18(7):8095-8108. Published 2013 Jul 9.  [Content Brief]

  [5]. Cheng HY, et al. Antiherpes simplex virus type 2 activity of casuarinin from the bark of Terminalia arjuna Linn. Antiviral Res. 2002;55(3):447-455.  [Content Brief]