6. Medicinal properties of forskolin

Traditionally, the roots have been used as condiments in pickles, for preparation of pickles. Forskolin has positive effect against a wide range of conditions such as asthma, glaucoma, hypertension, hair loss, cancer, and obesity [51]. C. forskohlii extract (standardized to contain 95% forskolin) is potentially useful in skin care formulations, particularly as a conditioning age. In traditional Indian systems of medicine, the roots of C. forskohlii are used as a tonic. Other therapeutically relevant properties include anthelmintic action and efficacy in the management of skin infections and eruptions. The plant is also used traditionally in veterinary practice (Table 1). Essential oil in tubers of this plant has potential uses in food flavoring industry and can be used as an antimicrobial agent and has very attractive and delicate odor with spicy note. A labdane diterpenoid is considered the active secondary metabolite because of its ability to activate the enzyme adenylyl cyclase (Ac) thereby increasing the intracellular level of cAMP and leading to various physiological effects [52]. FSK is shown to exert a 6–400 fold increase in levels of cAMP. Cyclic AMP is a "second messenger" hormone signaling system as its synthesis triggers the action of various hormones, enzymes and other biological activities that have profound effects on local cells, as well as systemic effects, in some instances, on the entire body [53]. FSK by passes the adrenoreceptors, increasing cAMP levels directly, thereby stimulating lipolysis. FSK has also been shown to counteract the decreased response of fat cells to epinephrine, associated with aging. FSK also accelerates lipolysis through the activation of hormonesensitive lipase [54]. It is primarily via the increased synthesis of cyclic AMP that C. Forskohlii may exert its medicinal influences on a significant number of common health conditions.


7. FSK and brain

tubule

Anti-cystic fibrosis

Table 1. Pharmacological action of FSK.

xiii. Inhibition

of human neutrophil degranulation

xv. Hydrodynamic alterations in collecting

Anti-histaminic activity

7.1. FSK-binding sites

3H-forskolin has, for example, been found to bind to both a high and a low affinity site in rat brain membranes [55] and the capacity of the high affinity forskolin-binding site has been shown to be increased by the activation of N-proteins by guanine nucleotides [56]. High affinity [3H] FSK-binding sites have been mapped autoradiographically in rat brain area such as caudate-putamen, nucleus accumbens, olfactory tubercle, globus pallidus, substantia nigra and the hilus of the area dentata [57] and exhibit a markedly heterogeneous distribution.

S.No. Pharmacological activity Mechanism of action Ref. No

stimulates lipolysis.

response to FSK

xi. Anti-diabetic activity FSK predominantly decreased basal glucose in healthy rats

xii. Anti-platelet aggregation Antagonizes the action of platelet-activating factor (PAF).

AC

xiv. Smooth muscle relaxant Increase both the cytosolic Ca2+ concentration and the

proliferation and thus decrease cell division. Normalizing the cAMP /cGMP ratio

Forskolin increases cAMP accumulation, and therefore

Overexpression of TANK-binding kinase 1 (TBK1) reduced phosphorylation of hormone-sensitive lipase (HSL) in

and attenuated the severity of hyperglycemia in diabetic rats FSK increase intracellular cAMP, which, together with the increase in ATP, enhance the priming of insulin granules

Reduction in the histamine release from human basophiles and mast cells by modulating the release of mediators of the immediate hypersensitivity reaction, through activation of

cytosolic NO concentration ([NO]c) in the endothelial cells

FSK resulted in increase in osmotic water flux and hydraulic conductivity of the rabbit cortical collecting tubule FSK leads to cyst formation in culture media

Reduction in the extent of platelet aggregation Induced a partial deaggregation of ADP- or collagen-

cAMP-mediated phosphodiesterase inhibition.

inflammatory hepatic and necrosis

Neuroprotective Strategies of Blood-Brain Barrier Penetrant "Forskolin" (AC/cAMP/PKA/CREB Activator)…

Inhibit mast cell degranulation

aggregated human platelets

leads to cause vasodilatation Increases uterine smooth muscle AC 99

13

http://dx.doi.org/10.5772/intechopen.80046

100

101

102

103

104

105

106

viii. Anti-psoriasis Decreased cGMP levels that are associated with cell

ix. Hepatoprotective activity Repair of hepatic tissue damage, normalization of

x. Anti-inflammatory Reduction in the level of Interleukin-1β, 6 and 8


Table 1. Pharmacological action of FSK.
