Process for the synthesis of pharmacologically active …

The melanocyte-keratinocyte complex of the skinresponds quickly to a wide range of environmental stimuli, oftenthrough paracrine and/or autocrine means. IBMX is known to increasecellular cAMP through the inhibition of the cAMP-degrading enzyme,phosphodiesterase ().Guggulsterone effectively blocked the IBMX-induced increase inmelanogenesis by decreasing the expression of tyrosinase. Thiseffect occurred at the transcriptional level, suggesting its actionon the cAMP-dependent pathway. When the B16 cells were treated withα-MSH, a peptide acting on melanocortin 1-receptor (MC1-R) ofmelanocytes (), or forskolin,a direct activator of adenylate cyclase (), the cellular melanin contents weresignificantly increased. Again, guggulsterone significantlyinhibited melanogenesis induced by both α-MSH and forskolin, as inthe case of IBMX stimulation. These results also support the actionmechanism of guggulsterone on the cAMP-dependent pathway. Inaddition to the cAMP/PKA pathway, increased melanogenesis after UVirradiation was thought to occur through the activation of thediacylglycerol/protein kinase C (PKC) and nitric oxide/proteinkinase G (PKG) pathways, and SOS response to UV-induced DNA damage(). The PKC-induced activationof tyrosinase occurs through phosphorylation rather than thesynthesis of new enzymes ().However, PKG is known to increase the expression of tyrosinaseprotein (). The additionaleffects of guggulsterone on these pathways require furtherstudy.

An improved process for the synthesis of …

Guggulsterone, a mixture of cis (E) and trans (Z) isomers (7∶3 w/w) was synthesized from 16-DPA

Guggulsterone Supplier | CAS 95975-55-6 | Tocris …

In conclusion, to our knowledge, the present studydemonstrates for the first time that guggulsterone is an effectiveinhibitor of tyrosinase and inhibits melanin biosynthesis. Eventhough we have not determined its effects in conditions, guggulsterone may have beneficial effects in thetreatment of hyperpigmentation diseases.

Welcome to The Supplement Research Foundation

Since tyrosinase is the rate-limiting enzyme formelanin biosynthesis, the effect of guggulsterone on tyrosinaseactivity was determined. Cellular tyrosinase activity was decreasedby guggulsterone in a dose-dependent manner (), which was consistent with thedecreased melanin content (). The expression of tyrosinase protein was determined bywestern blot analysis ().The results showed that the tyrosinase protein was greatlyincreased by IBMX treatment, and this induction was significantlyinhibited by guggulsterone in a dose-dependent manner. Theexpression of tyrosinase mRNA determined by real-time RT-PCR alsoexhibited a significant decrease following guggulsterone treatment(). These results indicatedthat the inhibition of tyrosinase by guggulsterone was exerted atthe transcriptional level. The mRNA levels of TRP-1, TRP-2 andMITF, members of the melanogenesis-related gene family, were alsodecreased by the presence of guggulsterone ().


Guggul Gold (Guggulsterones Z & E) - NutriGold Inc

Guggulsterone is a FXR antagonist found in myrrh

Guggul Effective for Diabetes Type 2 & 1 - Diabetic …