Chronic Oral Administration of Tenebrio molitor Extract Exhibits Inhibitory Effect on Glucocorticoid Receptor Overexpression in the Hippocampus of Ovariectomy-Induced Estrogen Deficient Mice.

It has been reported that estrogen deficiency in female disrupts systemic endocrinologic regulatory mechanisms, finally leading to osteoporotic condition. Estrogen deficiency also down-regulates brain functions due to its deficits of its original roles in a number of neurological events. Therefore, it is necessary to find alternative materials that can prevent osteoporotic condition and maintain normal brain functions to correct such hormone deficiency. In the present study, we found that novel compounds originated from larvae of Tenebrio molitor (TM) possessed anti-osteoporotic effect. They could also prevent abnormal progressive brain function by deaccelerating enhanced HPA-axis negative feedback while maintaining neurogenesis in hippocampus. We daily administered TM to ovariectomized (OVX) ddY mice for 4 weeks and then performed histological and hormonal evaluations for its anti-osteoporotic effects. In addition, we investigated glucocorticoid receptor (GR) expression and neuroblast expression (DCX) in the hippocampal dentate gyrus morphologically by immunohistochemistry analysis. According to our results, TM has anti-osteoporotic effects. It also tends to bring interfered brain environment back to normal condition. These results suggest that TM might have anti-osteoporosis effect and enhancing effects on enrichment of environment in brain by being antidestroyed hormonal deficiency simultaneously. This is the first study to report that TM can be used as source of bioactive substance to prevent decreased neurogenesis and impaired HPA axis driven by high GR expression in the hippocampus in hormonal deficient female animals. PRACTICAL APPLICATION: Anti-osteoporosis effect and stress resistance due to improved brain function caused by the ingestion of Tenebrio molitor extract were observed in postmenopausal women. T. molitor is available as a nutritional supplement for bone and brain health, which menopausal women need most.

A novel pyrazole derivative protects from ovariectomy-induced osteoporosis through the inhibition of NADPH oxidase.

Osteoclast cells (OCs) are differentiated from bone marrow-derived macrophages (BMMs) by activation of receptor activator of nuclear factor κB (NF-κB) ligand (RANKL). Activation of NADPH oxidase (Nox) isozymes is involved in RANKL-dependent OC differentiation, implicating Nox isozymes as therapeutic targets for treatment of osteoporosis. Here, we show that a novel pyrazole derivative, Ewha-18278 has high inhibitory potency on Nox isozymes. Blocking the activity of Nox with Ewha-18278 inhibited the responses of BMMs to RANKL, including reactive oxygen species (ROS) generation, activation of mitogen-activated protein (MAP) kinases and NF-κB, and OC differentiation. To evaluate the anti-osteoporotic function of Ewha-18278, the derivative was applied to estrogen-deficient ovariectomized (OVX) ddY mice. Oral administration of Ewha-18278 (10 mg/kg/daily, 4 weeks) into the mice recovered bone mineral density, trabecular bone volume, trabecular bone length, number and thickness, compared to control OVX ddY mice. Moreover, treatment of OVX ddY mice with Ewha-18278 increased bone strength by increasing cortical bone thickness. We provide that Ewha-18278 displayed Nox inhibition and blocked the RANKL-dependent cell signaling cascade leading to reduced differentiation of OCs. Our results implicate Ewha-18278 as a novel therapeutic agent for the treatment of osteoporosis.

Application of Bioactive Natural Materials-based Products on Five Women's Diseases.

Women's health has been threatened by various diseases mainly including heart disease, breast cancer, osteoporosis, depression, and autoimmune disease. But development of medication for these diseases has been restricted by high development costs and low success rates. Herein the attempt to develop valid bioactive materials from a traditional natural material has been made. Resveratrol has been reported to be effective in treatment of breast cancer and heart disease. Goji berry has received attention as a natural based therapeutic material to treat a diabetes, cardiovascular disease, and osteoporosis. Leonurus family has been reported to be effective particularly in pregnant women due to high contents of vitamin as well as stimulation of uterine contraction. Annona family has effects such as anti-anxiety, anticonvulsant and recently it is proposed to be as a therapeutic material to cure depression based on its strong antidepressant effect. Shiraia bambusicola has been utilized to cure angiogenesis-related disease from ancient China and furthermore recently it was proved to be effective in rheumatoid arthritis. Getting an understanding of utilization of these traditional natural materials not only enhances the interest in development of therapeutic materials for preventing and treating various women's diseases, but also makes it possible to develop novel therapeutic materials.