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Coleus forskholii is an important ayurvedic herb that has been a part of Indian
medicine for centuries. Its common name is makhandi. In the 1970s, researchers isolated a
chemically active ingredient in the herb and called it forskholin.
Forskholin is a diterpene (Bhat et al., 1977) isolated from the roots of Coleus froskholii. This alkaloid has a unique property of activating all hormone-sensitive adenylate
cyclase enzymes in the biological systems. Activation of adenylate cyclase raises cyclic AMP
(cAMP) levels in a variety of tissues. Cyclic AMP is an important cell-regulating compound,
which, once formed, activates many other enzymes involved in diverse cellular functions.
Under normal situations, cAMP is formed when a stimulatory hormone epinephrine (Okuda et al., 1992) binds to receptor site on the cell membrane and stimulates the activation of
adenylate cyclase. This enzyme is incorporated into all cellular membranes, and only the
specificity of the receptor determines which hormone activates it in a particular cell.
Forskholin bypasses the need for direct hormonal activation of adenylate cyclase. As a result of
this direct activation of adenylate cyclase, intracellular cAMP levels rise. The physiological
and biochemical effects of a raised intracellular cAMP levels are manifold. Forskholin
functions as a platelet aggregation inhibitor, relaxes vascular smooth muscles, decreases
intraocular pressure due to glaucoma, and has antiallergy (Rupp et al., 1986) potential since it inhibits IgE-mediated release of histamine and peptide leukotriene from human basophils and
mast cells. Forskholin was shown to be a potent inhibitor of cancer metastasis in mice
injected with malignant cells. |