Studies On The Chemical Constituents Of Petasites Japonicus And Preparation Of Capsules

The basic issue to the development of the traditional Chinese medicine (TCM) is to elucidate effective substance of the preparations of the TCM. As the key of development of the TCM preparations, effective substances of preparations will affect rationality and clinical curative effects directly. Besides, the effective substances of preparations is also the one way to make the TCM modernization, which plays an important role in development of the TCM and related efficacy material base of Chinese medicines should be elucidated clearly, which will ensure the preparations to be highly active, safe, stable, controllable, convenient and provide theoretical foundations for the development and utilization of the TCMPetasites japonicus, belonging to the Compositae family and is a perennial herbaceous plant, distributed in many provinces, such as Jiangxi, Anhui, Heilongjiang, Jilin. The rhizomes and whole plants have been used as the TCM for the treatment of wounds, contusion and snakebites. P. japonicus have been used as a medicine homologous food also.Through the methanol extract, petroleum extract, a variety of chromatographic methods, such as MPLC, silica gel c.c, HPLC etc for the P. japonicus, and 15 compounds were isolated by these methods. The structures of the 15 compounds were identified as following:3β-hydroxyl-6β-methoxyl-10β-furanoeremophilane (1), bakkenolide-X (2), bakkenolide III (3), japonipene B (4), homofukinolide (5), valerilactones A (6), (8S)-2-tigloyloxyeremophil-7(11)-en-12,8-olide (7),3β-angeloyloxy-6β-hydroxyeremophil-7(11)-en-12,8β-olide (8), (8S)-2-tigloyloxy-8-hydoxyeremophil-7(11)-en-12,8-olide (9), (8S)-2-tigloyloxy-8-methoxyeremophil-7(11)-en-12,8-olide (10), eremopetasitenin C3 (11),3β-hydroxy-6β-methoxyeremophil-7(11)-en-12,8β-olide (12),6β-angeloyloxy-3β hydoxyeremophil-7(11)-en-12,8β-olide (13),3β-hydroxy-6β,8a-dimethoxyeremophil-7(11)-12,8β-olide (14), eremopetasitenin D3 (15). Among them, compound 1 is a new compound,6, 7,8,9,10 were isolated from Petasites genus for the first time.In order to search the bioactive substances from the compounds which were isolated from the P. japonicus. The biological studies in the PC 12 cells, and the result is that compounds 5,6, 8,12,14 and 15 were able to promote neurite outgrowth.In addition, according to the mono-factor test that the optimum conditions of making pellet for the capsule preparation have been confirmed and provide reference for the capsule preparation of P. japonicus.