Boswellin: An Alternative to NonSteroidal Anti-Inflammatory Drugs
An Alternative to NonSteroidal Anti-Inflammatory Drugs
Nowhere is the role of prolonged anti-inflammatory treatment more important than in chronic inflammatory conditions best exemplified by the various forms of arthritis. And nowhere is the safety factor of such prolonged treatment more paramount than in the treatment of arthritis. In fact, aspirin, or acetylsalicylic acid, was developed in the 19th century by a chemist whose father suffered from gastric ulcerations due to a chronic intake of crude salicylates for arthritis. Although aspirin and other new generation nonsteroidal antiinflammatory drugs (NSAIDs) are better tolerated than the historic salicylates, their effectiveness and safety from longterm use still is elusive. The search for new anti-inflammatory compounds has resulted in a growing interest in Boswellia serrata, a timetested botanical compound well recognized in Ayurveda Materia Medica.
Boswellia serrata (N.O. Burseraceae) is a large, branching, deciduous tree that grows abundantly in the dry, hilly parts of India. The gum resin exudate of Boswellia serrata, known in the vernacular as "Salai guggal," has been used in the Ayurvedic system of medicine for the management of arthritis, respiratory diseases and liver disorders.
The active principles of the gum resin, boswellic acids, emerge as leading non-steroidal anti-inflammatory compounds (drugs) with broad biological activities and without NSAIDs’ characteristic side effects-namely, gastrointestinal irritation. In one experiment, boswellic acids were compared with anti-inflammatory drug phenylbutazone, and unlike phenylbutazone, boswellic acids did not produce the usual gastric ulceration. This safety factor is very important since, as mentioned previously, NSAIDs are notorious for their damaging effect on stomach and intestinal mucosa.
Studies designed to determine the anti-inflammatory mechanism of boswellic acids indicate that the primary mode of action involves the inhibition of 5-lipoxygenase, the key enzyme responsible in the formation of inflammatory compounds called leukotrienes. Furthermore, treatment with boswellic acids may reduce the activity of various tissue destructive enzymes [beta-glucuronidase, beta-N-acetylglucosaminidase, cathepsin B1, cathepsin B2, cathepsin D and human leukocyte elastase (HLE)]. One of the reasons that boswellic acids may be both safe and effective is that they operate through a very specific mechanism that inhibits one enzyme predominantly, 5-lipoxygenase.
Analysis of boswellic acids shows that there are four beta-boswellic acids involved in the inhibition of 5-lipoxygenase and related antiinflammatory events. These are:
* Beta-boswellic acid (I)
* Acetyl-beta-boswellic acid (II)
* 11-keto-beta-boswellic acid (III)
* Acetyl-11-keto-beta-boswellic acid (IV)
Seeking Better Understanding
Despite the recognized potential of boswellic acids as NSAIDs, there have been two major obstacles that stand in the way of utilizing boswellic acids more frequently in health care: 1) a poorly understood relationship between structure/composition of boswellic acids and their biological utility, and 2) the lack of a standardized boswellic acids product on the basis of a clearly defined structure-function claim.
Recently, Sabinsa Corporation, along with investigators from Rutgers University, in New Brunswick, NJ, published a study in Planta Medica (1998) that addressed the above mentioned shortcomings. This study evaluated the anti-inflammatory properties of purified boswellic acids (Boswellin) in an in vitro experimental model. Comparisons of the biological potential of the four boswellic acids<