Mechanism of Action of Brazilin on Gluconeogenesis in Isolated Rat Hepatocytes

Abstract

The present study was undertaken to investigate the mechanism of action of brazilin on gluconeogenesis and ketogenesis in isolated rat hepatocytes and to elucidate the hypoglycemic mechanism of brazilin. Brazilin decreased gluconeogenesis at 100 micro M in hepatocytes isolated from diabetic rats. Brazilin also decreased basal and glucagon-induced gluconeogenesis in hepatocytes from normal rats. Fatty acids (octanoate or oleate)-induced gluconeogenesis was significantly reduced by brazilin, but ketogenesis was not influenced. The depletion of extracellular or intracellular calcium decreased gluconeogenesis in calcium-depleted media. Brazilin lowered dibutyryl cAMP (Bt2cAMP)-induced gluconeogenesis and the intracellular adenosine 3',5'-cyclic monophosphate (cAMP) level in glucagon-treated hepatocytes. It was also found that brazilin does not require calcium for inhibition of gluconeogenesis, but may inhibit the down-stream of cAMP signaling pathways. These data suggest that a decreased gluconeogenic flux in hepatocytes might at least partly contribute to the hypoglycemic effects of brazilin.

In Vitro Study for Inhibition of NO Production about Constituents of Sappan Lignum

“…Whereas pharmacological studies have been conducted on brazilin, 20,21) no work has been done on the other compounds because it is difficult to isolate them and their chemical structures are difficult to elucidate. Thus, we expected effects that are different from and stronger than that of brazilin.…”

Evaluation of Su Fu’ning Lotion’s Inhibitory Effects on Bladder Cancer Cells In Vitro and In Vivo by Intravesical Instillation

“…Brazilin (in SFN) has been reported to have many biological activities, including immune regulation, 19,20 blood vessel dilatation, 3,11,14 anticoagulation, 8,17 hypoglycemic effect, 10,13,15,16,26,27 oxidative damage inhibition, 6,28 antibiosis, 9 and anti-inflammatory effects. 4,5,7 In addition, it was demonstrated that brazilin powerfully broke deoxynucleic acid chains in anticancer screening.…”

“…13 Brazilin has been reported to have a wide range of biological activities, which includes potent antibacterial activity against antibiotic-resistant bacteria such as methicillin-resistant Staphylococcus aureus, vancomycin-resistant enterococci, multidrug-resistant Burkholderia cepacia, and other bacteria, 14 inducing vasorelaxation as well as release of alpha-1-adrenergic receptor agonists in phenylephrineprecontracted rat aortic rings, 15,16 antiplatelet activity, 17 inducing cellular immune response, 18 decreasing suppressor cell activity, 19 and regulating T-cell function. 20 Based on the impressive wealth of data on brazilin, cytotoxic effects of Su Fu'ning Lotion (SFN), a lotion produced from sappan wood extract (with brazilin content >52%), on human bladder carcinoma cell line T24, mouse bladder transitional cancer cell line (BTT cells), and human bladder cancer cell line BIU-87 were assessed.…”

Brazilin Isolated fromCaesalpinia sappanSuppresses Nuclear Envelope Reassembly by Inhibiting Barrier-to-Autointegration Factor Phosphorylation

“…C. sappan heartwood has been used as a traditional medicine for various diseases. Brazilin, one of the main C. sappan components (Puchtler et al, 1986), is reported to possess various biologic effects, including anti-inflammatory activity (Hikino et al, 1977;Bae et al, 2005), antihepatotoxicity activity (Moon et al, 1992), induction of immunologic tolerance (Choi and Moon, 1997;Mok et al, 1998), inhibition of downstream cAMP signaling (Won et al, 2004), inhibition of protein kinase C and insulin receptor kinase , and antiplatelet activity (Hwang et al, 1998). Indeed, its cytotoxic properties as an antitumor agent have previously been reported (Kim et al, 2012).…”