ovariectomized

Droloxifene (3-Hydroxytamoxifen), a tamoxifen derivative, is an oral active and selective estrogen receptor modulator.Droloxifene induced p53 expression and apoptosis in McF-7 cells.Fluroxifene has anti-estrogen and anti-implantation effects.Fluroxifene prevented bone loss in ovariectomized rats.

Raloxifene (LY-139481) is a selective oestrogen receptor modulator. It has effects on bone and breast cancer and cardiovascular disease risk.

Miroestrol is a potent phytoestrogen compound with multifaceted biological effects. It induces a mammogenic effect and demonstrates neuroprotective properties, along with the ability to prevent bone loss in ovariectomized mice. Additionally, Miroestrol has been shown to reduce the risk of cancer [4].

Methyl vanillate is Hovenia Dulcis Thunb extract and its ingredient methyl vanillate activate Wnt/β-catenin pathway and increase bone mass in growing or ovariectomized mice. Methyl vanillate is considered to be a slightly soluble (in water) acidic compound. Methyl vanillate can be synthesized from vanillic acid. Methyl vanillate has been identified in foods such as cow's milk and beer.

(-)-Epiafzelechin is a COX inhibitor with antioxidant and anti-inflammatory activity, osteoprotective effects in a mature ovariectomized mouse model, ability to stimulate osteoblast activity and inhibit osteoclast activity.

Moexiprilat, an active metabolite of the prodrug moexipril formed through side chain ester hydrolysis in vivo, functions as an angiotensin-converting enzyme (ACE; IC50 = 2.1 nM) inhibitor. At a concentration of 10 nM, it inhibits the proliferation of primary neonatal rat cardiac fibroblasts stimulated by estrone or angiotensin II. Furthermore, when given at a daily dosage of 50 mg/kg, moexiprilat reduces mean arterial blood pressure and elevates levels of atrial natriuretic peptide, an indicator of hypertension, in ovariectomized mice.

CW 008 is an activator of the cAMP/PKA/CREB pathway. It promotes osteogenic differentiation of human bone marrow derived mesenchymal stem cells in vitro and increases bone mass and bone volume density in ovariectomized mice.

17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1,500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7aro cells in a concentration-dependent manner. 17β-hydroxy Exemestane (20 mg/kg) inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae, in ovariectomized rats.

Liarozole (R75251 dihydrochloride) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.