Wednesday, October 28, 2009

Gum Guggl

Gugglesterone doesn't seem like a potential height increasing compound and seems mostly catabolic in effects.

Pharmacological properties of guggulsterones, the major active components of gum guggul.

"ommiphora mukul is a short thorny shrub that is native to the Indian subcontinent. Oleo gum resin extracted by incision of the bark is a very complex mixture of gum, minerals, essential oils, terpenes, sterols, ferrulates, flavanones and sterones. Its active constituents, the Z- and E-guggulsterones, have been demonstrated to exhibit their biological activities by binding to nuclear receptors and modulating the expression of proteins involved in carcinogenic activities. Guggulsterones have also been reported to regulate gene expression by exhibiting control over other molecular targets including transcription factors such as nuclear factor (NF)-κB, signal transducer and activator of transcription (STAT) and steroid receptors."

"Gum guggul is tapped from C. mukul trees by making incisions at the bark."

"guggulsterone is the bioactive principle in gum guggul responsible for its pharmacological action"

"Guggulsterone inhibits the activation of NF-κB and down-regulates the expression of the above-mentioned proinflammatory mediators"<-However NF-kappaB can be pro height increase.  Guggulsterone also inhibits IL-1B.

"guggulsterone blocks RANKL signalling and osteoclastogenesis induced by RANKL by inhibiting the activity of IκBα kinase. Guggulsterone treatment also induces phosphorylation and further degradation of IκBα, which is an inhibitor of NF-κB. Dose-dependent and time-dependent treatment with guggulsterone suggested suppression of monocyte differentiation into osteoclasts"

"Guggulsterone at a concentration of 25 µ m induces S-phase arrest of the cells in the cell cycle through down-regulation of the much-required cyclin D1 and cdc2 and through up-regulation of cyclin-dependent kinase inhibitors p21 and p27 in a time-dependent manner. "

Guggulsterone increases apoptosis.

"Guggulsterone has been found to stimulate the thyroid gland. Of the two hormones, tri-iodothyronine (T3) and serum thyroxine (T4), produced by the thyroid gland, T4 is considered to be active. T4 is converted to T3 in the peripheral tissues. The administration of guggulsterone (10 mg/kg b.w.) in hypothyroid rats could restore the lost thyroid activity. Administration of guggulsterone in albino rats (10 mg/kg b.w.) increased thyroid function. There was an increased uptake of iodine by the thyroid gland. As a result, thyroid peroxidase and protease activities increased in albino rats with a concomitant increase in oxygen consumption"

"guggulsterone activates PR[progesterone receptor] (EC50 = 5.9 µ m compared with progesterone), PXR (half-maximal effective concentration (EC50) = 2.4 µ m compared with rifampicin) and ERα (EC50 = 4.6 μM compared with β-eostradiol)."

"Guggulsterone prevents phosphorylation of STAT-3, which suppresses protein tyrosine kinases activation. Guggulsterone stimulates the transcription of mRNA of SHP-1 and its translation product, tyrosine protein phosphatase. Moreover, guggulsterone was found to down-regulate the expression of antiapoptotic, proliferative and angiogenic gene products regulated by STAT-3. Further study suggested its use in the suppression of cell proliferation, accumulation and induction of apoptosis"

Gugglsterone also inhibits phosphorylation of MAPK and Akt.

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