Studies on the anti-islet hypertrophy and anti-osteoporosis constituents from Formosan Fern

Purpose of this study is to use Formosan fern as rich resources for the search of active nature products, and to discover the active ingredient basis for follow-up drug development. Under the preliminary supports of the NSTP, from Hypolepis punctata, the hypoglycemic pterosins which belongs to sesquiterpene have been found, and have good hypoglycemic bioactivity. Patent application 3 pieces: TW 201039836, US 2010-0190732, PCT WO 2010/085811. This invention relates to the use of nstpbp168 derivatives for treating diabetes including type 1 and type 2, and for treating obesity. Related technology and results of the technology were transferred to ElitePharm Co., Ltd. Our previous studies revealed that PTD-IS01 and PTA-IS01 isolated from other species, also known to capable of improving the db/db diabetic mice pancreas islet enlargement, have the potential for treatment of the pancreas islet disease. PTD-IS01G, a glycoside of PTD-IS01, also have been demonstrated to improve insulin resistance, and better than nstpbp168 or PTD-IS01. In the early part of anti-osteoporosis drugs development, at lower dosage, the fern extract DEF in in vitro cell studies, show significant regulation on bone metabolism, the inhibition on osteoclast differentiation more than osteoblast differentiation. In this project, we search for the compounds of anti-islet hypertrophy and anti-osteoporosis from Formosan Fern, to improve inflammation of the pancreas and symptoms of diabetes, and as lead compounds for new drug discovery. The entail work includes: 1.The preparation of target compound and expand the derivatives from related fern species. 2.The establishment of a small scale of production methods and procedures, preparation of active ingredients supply animal experiments, pharmacological mechanism and review of toxicity of demand. 3.Chemical modification and chemical synthesis of lead compounds, and studies on pharmacokinetics of target compounds.