Safety and toxicological evaluation of a novel, standardized 3-O-acetyl-11-keto-beta-boswellic acid (AKBA)-enriched Boswellia serrata extract (5-Loxin (R))

The novel anti-inflammatory properties of the gum resin derived from Boswellia serrata, also known as Salai guggal in Ayurvedic medicine, are well recognized and highly recommended for human consumption. The active constituents of the gum resin are boswellic acids (BAs). Among the BAs, AKBA potently inhibits 5-lipoxygenase product formation with an IC50 of 1.5 m μM. We developed a novel Boswellia serrata extract (5-Loxin®) enriched with 30% AKBA (US Patent 2004/0073060A1). The genetic basis of the anti-inflammatory effects of 5-Loxin® was explored in a system of TNFα-induced gene expression in human microvascular endothelial cells. 5-Loxin® significantly prevented the TNFα-induced expression of matrix metalloproteinases and adhesion molecules (ICAM-1 and VCAM-1), and inducible expression of the mediators of apoptosis. With such interesting findings, we planned to determine the broad-spectrum safety of 5-Loxin®. Acute oral, acute dermal, primary skin and eye irritation, and dose-dependent 90-day subchronic...