| Description: |
Sappanchalcone shows xanthine oxidase inhibitory activity, is a xanthine oxidase inhibitor. Sappanchalcone has cytoprotective, and anti-inflammatory effects, it could be used as an anti-inflammatory and bone-protective agent during the treatment of rheumatoid arthritis. Sappanchalcone blocks cell cycle progression in the G2/M phase, it suppresses oral cancer cell growth and induces apoptosis through the activation of p53-dependent mitochondrial, p38, ERK, JNK, and NF-κB signaling, could potentially used to treat periodontal, pulpal , periapical inflammatory lesion and oral cancer. Sappanchalcone possesses the most potent effect against allergic reaction in basophilic leukemic (RBL-2H3) cells with an inhibitory concentration (IC50) value of 7.6 uM, it may have anti-allergic activity. |
| Targets: |
TNF-α | IL Receptor | Bcl-2/Bax | Caspase | p53 | NF-kB | ERK | JNK | p38MAPK | HO-1 | Nrf2 | NO | PGE | STAT | NOS |
| In vitro: |
| Chin J Nat Med. 2014 Aug;12(8):607-12. | | Inhibitory activities of Lignum Sappan extractives on growth and growth-related signaling of tumor cells.[Pubmed: 25156286] | To investigate the active constituents of Lignum Sappan (Caesalpinia sappan L.) on growth-related signaling and cell mitosis.
METHODS AND RESULTS:
The influence of the ethyl acetate (EtOAc) extract of Lignum Sappan and its constituents on growth-related signaling were evaluated by a luciferase assay in cells stably-transfected with NF-κB, STAT1, or STAT3 responsive luciferase reporter plasmid. The inhibitory effect on the cell cycle was determined by flow cytometric analysis. The anti-tumor activities were assessed in vitro and in vivo.
The EtOAc extract of Lignum Sappan had inhibitory activities on growth-related signaling and cell mitosis. Three major active compounds were sappanchalcone, brazilin, and butein. Sappanchalcone blocked cell cycle progression in the G2/M phase, brazilin inhibited TNFα/NF-κB signaling, while butein inhibited IL-6/STAT3 signaling, as well as TNFα/NF-κB signaling. The three compounds all demonstrated cytotoxic activities against human tumor cells in vitro. In a S180 tumor cell-bearing mice model, the anti-tumor efficacy of the EtOAc extract was better than the individual compounds acting alone.
CONCLUSIONS:
These results indicate that Lignum Sappan contains multiple active compounds with different antitumor activities, which act synergistically to enhance their anti-tumor effects. The EtOAc extract of Lignum Sappan may be better than individual active constituent as a novel medicine for the treatment of cancer. | | Phytother. Res., 2009, 23(7):1028-31. | | Anti-allergic activity of principles from the roots and heartwood of Caesalpinia sappan on antigen-induced β-hexosaminidase release.[Reference: WebLink] |
METHODS AND RESULTS:
The dichloromethane extract of the roots and heartwood of Caesalpinia sappan exhibited potent inhibitory activity against beta-hexosaminidase release as marker of degranulation in rat basophilic leukemic (RBL-2H3) cells, with inhibition of 98.7% and 87.5% at concentration of 100 microg/ml, respectively. These extracts were further separated by chromatographic techniques to give two chalcones and seven homoisoflavones. Among the compounds tested, Sappanchalcone (2) possessed the most potent effect against allergic reaction in RBL-2H3 cells with an inhibitory concentration (IC50) value of 7.6 microM, followed by 3-deoxySappanchalcone (1, IC50 = 15.3 microM), whereas other compounds showed moderate and mild effects.
CONCLUSIONS:
The results suggested the following structural requirements of chalcones (1 and 2) and homoisoflavones (3-9) for anti-allergic activity: (i) chalcone exhibited higher activity than homoisoflavone (ii) vicinal hydroxylation at B-ring of chalcone conferred higher activity than one hydroxylation; and (iii) for homoisoflavone, the hydroxyl groups at C-3 and C-4 positions decreased the activity. This is the first report of C. sappan for anti-allergic activity. |
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| In vivo: |
| Arch Pharm Res. 2015 Jun;38(6):973-83. | | Anti-inflammatory activity of sappanchalcone isolated from Caesalpinia sappan L. in a collagen-induced arthritis mouse model.[Pubmed: 25586964] | Sappanchalcone, a bioactive flavonoid isolated from the heartwood of Caesalpinia sappan L. possesses anti-inflammatory effects.
We studied the efficacy of Sappanchalcone in attenuating collagen-induced arthritis (CIA) in a mouse model of rheumatoid arthritis.
METHODS AND RESULTS:
Sappanchalcone was purified to homogeneity from the chloroform fraction of the methanolic extract of C. sappan, and identified using mass spectrometry and (1)H-nuclear magnetic resonance spectroscopy. CIA-induced male DBA/1J mice were divided into control, Sappanchalcone-treated, and methotrexate-treated groups (n = 10 per group). Paw swelling, arthritis severity, radiographic and histomorphometric changes were assessed to measure the protective role of Sappanchalcone against chronic disease progression. Sappanchalcone administration significantly reduced clinical arthritis and inflammatory edema in paws. Bone mineral density and trabecular structure were maintained in CIA mice administered Sappanchalcone. The levels of pro-inflammatory cytokines (TNF-α, IL-6, and 1L-1β) were significantly lower in the serum of Sappanchalcone-treated mice as compared with the control group.
CONCLUSIONS:
Our results suggest that Sappanchalcone could be used as an anti-inflammatory and bone-protective agent during the treatment of rheumatoid arthritis. |
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