| Description: |
Brazilin exhibits cancer preventive, anti-hepatotoxicity, antiplatelet activity, and anti-inflammatory activities, it also inhibits UVB-induced MMP-1/3 expressions and secretions by suppressing of NF-κB activation in human dermal fibroblasts, thus, it might be used as a potential agent for treatment of UV-induced skin photoaging. Brazilin has anti-IKK activity, can selectively disrupt proximal IL-1 receptor signaling complex formation by targeting an IKK-upstream signaling components. Brazilin induces vasorelaxation by the increasing intracellular Ca(2+) concentration in endothelial cells of blood vessels and hence activating Ca(2+)/calmodulin-dependent NO synthesis. |
| In vitro: |
| Eur J Pharmacol. 2012 Jan 15;674(2-3):80-6. | | Brazilin inhibits UVB-induced MMP-1/3 expressions and secretions by suppressing the NF-κB pathway in human dermal fibroblasts.[Pubmed: 22044921 ] | Brazilin (7, 11b-dihydrobenz[b]indeno[1,2-d]pyran-3,6a,9,10 (6H)-tetrol), the major component of Caesalpinia sappan L., is a natural red pigment used for histological staining.
METHODS AND RESULTS:
Recent studies have shown that Brazilin exhibits distinct biological effects, including anti-hepatotoxicity, antiplatelet activity, and anti-inflammatory activities. In the present study, we evaluated the effects of Brazilin on MMP-1 and -3 expressions in human dermal fibroblasts exposed to ultraviolet B (UVB) irradiation. Brazilin showed protective effect on UVB-induced loss of cell viability of fibroblasts. Brazilin also blocked significantly UVB-induced Reactive Oxygen Species generation in fibroblasts. Brazilin inhibited UVB-induced MMP-1/3 expressions and secretions in a dose-dependent manner. Moreover, UVB-induced NF-κB activation was completely blocked by treatment with Brazilin.
CONCLUSIONS:
These findings suggest that Brazilin inhibits UVB-induced MMP-1/3 expressions and secretions by suppressing of NF-κB activation in human dermal fibroblasts. Thus, Brazilin might be used as a potential agent for treatment of UV-induced skin photoaging. | | Eur J Pharmacol. 2003 May 2;468(1):37-45. | | Induction of vasorelaxation through activation of nitric oxide synthase in endothelial cells by brazilin.[Pubmed: 12729841] | The vasorelaxant activity of Caesalpinia sappan L., a traditional Chinese medicine, and its major component Brazilin were investigated in isolated rat aorta and human umbilical vein endothelial cells.
METHODS AND RESULTS:
In isolated rat aorta, C. sappan L. extract and Brazilin relaxed phenylephrine-induced vasocontraction and increased cyclic guanosine 3',5'-monophosphate (cGMP) content. Induction of vasorelaxation of Brazilin was endothelium-dependent and could be markedly blocked by pretreatment with nitric oxide synthase (NOS) inhibitor, N(G)-nitro-L-arginine methyl ester (L-NAME); N(G)-monomethyl-L-arginine acetate (L-NMMA) and guanylyl cyclase inhibitor, methylene blue; 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ) and nitric oxide (NO) scavenger, hemoglobin. The increasing cGMP content induced by Brazilin was also blocked by pretreatment with L-NAME, methylene blue, and the removal of extracellular Ca(2+). In human umbilical vein endothelial cells, Brazilin dose-dependently induced an increase in NO formation and NOS activity, which were greatly attenuated by either the removal of extracellular Ca(2+) or the chelating of intracellular Ca(2+) chelator, 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA-AM). Moreover, Brazilin dose-dependently induced the influx of extracellular Ca(2+) in human umbilical vein endothelial cells.
CONCLUSIONS:
Collectively, these results suggest that Brazilin induces vasorelaxation by the increasing intracellular Ca(2+) concentration in endothelial cells of blood vessels and hence activating Ca(2+)/calmodulin-dependent NO synthesis. The NO is released and then transferred into smooth muscle cells to activate guanylyl cyclase and increase cGMP content, resulting in vasorelaxation. | | Br J Pharmacol . 2011 Jun; | | In vitro and in vivo evaluation of the anti-angiogenic actions of 4-hydroxybenzyl alcohol[Pubmed: 21366552] | | Abstract
Background and purpose: 4-Hydroxybenzyl alcohol (HBA) is a phenolic plant compound, which has been shown to influence many cellular mechanisms. In the present study, we analysed in vitro and in vivo the anti-angiogenic actions of this pleiotropic agent.
Experimental approach: Migration and protein expression of HBA- and vehicle-treated endothelial-like eEND2 cells was assessed by cell migration assay and Western blot analyses. HBA action on vascular sprouting was analysed in an aortic ring assay. In vivo anti-angiogenic actions of HBA were studied in the dorsal skinfold chamber model of endometriosis in mice.
Key results: Western blot analyses demonstrated that HBA inhibited proliferation of eEND2 cells, as indicated by down-regulation of proliferating cell nuclear antigen expression, and reduced expression of vascular endothelial growth factor and matrix metalloproteinase 9. HBA suppressed the migration of eEND2 cells, accompanied by inhibition of actin filament reorganization, revealed by fluorescence staining of the cytoskeleton. In addition, HBA reduced vascular sprouting in the aortic ring assay. Finally, we found, in the dorsal skinfold chamber model in vivo using intravital fluorescence microscopy, that HBA inhibited the vascularization of developing endometriotic lesions, as indicated by a decreased functional capillary density of lesions in HBA-treated mice and a reduced lesion size, compared with control animals.
Conclusions and implications: HBA targets several angiogenic mechanisms and therefore represents a promising anti-angiogenic agent for the treatment of angiogenic diseases, such as endometriosis. |
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| In vivo: |
| Int Immunopharmacol. 2015 Jul;27(1):130-7. | | Brazilin plays an anti-inflammatory role with regulating Toll-like receptor 2 and TLR 2 downstream pathways in Staphylococcus aureus-induced mastitis in mice.[Pubmed: 25939535] | Mastitis, which commonly occurs during the postpartum period, is caused by the infection of the mammary glands. The most common infectious bacterial pathogen of mastitis is Staphylococcus aureus (S. aureus) in both human and animals. Brazilin, a compound isolated from the traditional herbal medicine Caesalpinia sappan L., has been shown to exhibit multiple biological properties.
METHODS AND RESULTS:
The present study was performed to determine the effect of Brazilin on the inflammatory response in the mouse model of S. aureus mastitis and to confirm the mechanism of action involved. Brazilin treatment was applied in both a mouse model and cells. After Brazilin treatment of cells, Western blotting and qPCR were performed to detect the protein levels and mRNA levels, respectively. Brazilin treatment significantly attenuated inflammatory cell infiltration and inhibited the expressions of TNF-α, IL-1β and IL-6 in a dose-dependent manner. Administration of Brazilin in mice suppressed S. aureus-induced inflammatory injury and the production of proinflammatory mediators. This suppression was achieved by reducing the increased expression of TLR2 and regulating the NF-κB and MAPK signaling pathways in the mammary gland tissues and cells with S. aureus-induced mastitis.
CONCLUSIONS:
These results suggest that Brazilin appears to be an effective drug for the treatment of mastitis and may be applied as a clinical therapy. |
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