Ganoderol B is a potent α-glucosidase and angiotensin-converting enzyme inhibitor, with an IC(50) of α-glucosidase is 119.8 uM. It may be useful in prostate cancer and benign prostatic hyperplasia (BPH) therapy through suppressing the function of androgen and its receptor.
Bis(2-ethylhexyl) phthalate (DEHP) is a compound widely used in plastics technology to impart flexibility to rigid polymers, DEHP has oral toxicity during pregnancy and suckling in the Long-Evans rat.It can induce antiandrogenic effects in Spague-Dawley (SD) rats.
|CFN99815||Ganoderic acid DM
Ganoderic acid DM is an antiandrogenic osteoclastogenesis inhibitor, it especially suppresses the expression of c-Fos and nuclear factor of activated T cells c1 (NFATc1), this suppression leads to the inhibition of dendritic cell-specific transmembrane protein (DC-STAMP) expression and reduces osteoclast fusion. Ganoderic acid DM has shown toxicity to both androgen-dependent and independent prostate cancer cells with reduced osteoclastogenesis in late stage metastatic disease, it may an alternative agent for the treatment of advanced prostate cancer.
Myricanone has antioxidant, and anticancer activities, it has apoptosis-promoting ability by triggering caspase activation, and suppression of cell proliferation by down-regulation of NF-κB and STAT3 signalling cascades. Myricanone shows in vitro testosterone 5alpha-reductase inhibitory activity and in vivo anti-androgenic activity using growth of flank organ in castrated Syrian hamsters and/or hair regrowth after shaving in testosterone-treated C57Black/6CrSlc mice.
Cryptotanshinone is a potent STAT3 inhibitor with IC50 of 4.6 μM, and inhibits STAT3 Tyr705 phosphorylation in DU145 prostate cancer cells. It is also an AR inhibitor to suppress androgen/AR-mediated cell growth and PSA expression by blocking AR dimerization and the AR-coregulator complex formation. Cryptotanshinone has anti-atherosclerosis, neuroprotective, anti-cancer,and anti-neointimal formation activities. Cryptotanshinone reverses DEX-induced androgen excess and ovarian IR in mice through activation of insulin signaling and the regulation of glucose transporters and hormone-synthesizing enzymes, it has an inhibitory effect on MMP-9 production and migration of human aortic smooth muscle cells treated with TNF-alpha in a dose-dependent manner.