The production of fungal metabolites can be remarkably influenced by various cultivation parameters. To explore the biosynthetic potentials of the marine fungus, Neosartorya pseudofischeri, which was isolated from the inner tissue of starfish Acanthaster planci, glycerol-peptone-yeast extract (GlyPY) and glucose-peptone-yeast extract (GluPY) media were used to culture this fungus. When cultured in GlyPY medium, this fungus produced two novel diketopiperazines, neosartins A and B (1 and 2), together with six biogenetically-related known diketopiperazines,1,2,3,4-tetrahydro-2,3-dimethyl-1,4-dioxopyrazino[1,2-a]indole (3), 1,2,3,4-tetrahydro-2-methyl-3-methylene-1,4-dioxopyrazino[1,2-a]indole (4), 1,2,3,4-tetrahydro-2-methyl-1,3,4-trioxopyrazino[1,2-a] indole (5), 6-acetylbis(methylthio)gliotoxin (10), bisdethiobis(methylthio)gliotoxin (11), didehydrobisdethiobis(methylthio)gliotoxin (12) and N-methyl-1H-indole-2-carboxamide (6). However, a novel tetracyclic-fused alkaloid, neosartin C (14), a meroterpenoid, pyripyropene A (15), gliotoxin (7) and five known gliotoxin analogues, acetylgliotoxin (8), reduced gliotoxin (9), 6-acetylbis(methylthio)gliotoxin (10), bisdethiobis(methylthio) gliotoxin (11) and bis-N-norgliovictin (13), were obtained when grown in glucose-containing medium (GluPY medium). This is the first report of compounds 3, 4, 6, 9, 10 and 12 as naturally occurring. Their structures were determined mainly by MS, 1D and 2D NMR data. The possible biosynthetic pathways of gliotoxin-related analogues and neosartin C were proposed. The antibacterial activity of compounds 2–14 and the cytotoxic activity of compounds 4, 5 and 7–13 were evaluated. Their structure-activity relationships are also preliminarily discussed.

Twenty-five compounds with chemical diversity including five new compounds were isolated from the marine-derived fungus Pseudallescheria boydii F19-1. Five compounds displayed significant cytotoxicity against Sf9 cells.

In Asia, processed Atractylodis Rhizoma, the dried rhizome of Atractylodes ovata DE CANDOLLE (Compositae), is widely used as a tonic agent in herbal diets; stir-frying with soil is the most common processing method. In this study, we focused on determining variations in the function and concentrations of sesquiterpenoids in processed Atractylodis Rhizoma. Raw Atractylodis Rhizoma was processed by stir-frying it with different assistant substrates (i.e., red soil and burnt clay). The results indicated that there was less atractylon in stir-fried materials than in raw materials. However, there were higher levels of atractylenolides II and III in stir-fried materials than in raw materials. We also found that the heavy-metal content in burnt clay exceeded regulations set by the Taiwanese government. Moreover, commercial Atractylodis Rhizoma in Taiwan exhibited great differences in concentrations of the active components. In addition, atractylon showed stronger cytotoxicity than atractylenolides II and III in various cell lines. Therefore, we suggest that the toxic effects of atractylon are reduced following atractylon degradation to atractylenolides II and III. In conclusion, the toxicity of Atractylodis Rhizoma is reduced through processing.Key words Atractylodis Rhizoma; Atractylodes ovata; Compositae; processing; sesquiterpenoid; cytotoxicity © 2007 Pharmaceutical Society of Japan * To whom correspondence should be addressed. e-mail: crystal@tmu.edu.tw quantity of the active components. The quality control of Atractylodis Rhizoma is an important question, making it necessary to establish standardized analytical methods.In this study, the sesquiterpenoid concentrations of Atractylodis Rhizoma processed by different methods and with different assistant substrates were detected with an HPLC system. We ignored atractylenolide I because of its low concentrations. In addition, the cell cytotoxicity of these three major active components was also further examined. The aim of our study was to investigate the effect of stir-fry of Atractylodis Rhizoma to obtain a better understanding of the pharmacological effects of the processing procedures. Moreover, we collected commercially processed Atractylodis Rhizoma from different areas of Taiwan and analyzed the sesquiterpenoid contents in this herb to authenticate the quality of this useful Chinese drug in Taiwan. ExperimentalChemical and Reagents HPLC grade acetonitrile and tetrahydrofuran (THF) were purchased from Merck (Darmstadt, Germany) and Lab-Scan (Dublin, Ireland). Penicillin-Streptomycin, trypsin-EDTA and fetal bovine serum (FBS) were purchased from Gibco (Gibco-BRL, U.K.). Dimethyl sulfoxide (DMSO), adriamycin and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) were obtained from Sigma-Aldrich (St. Louis, MO, U.S.A.). Cell culture mediums, Dulbecco's MEM (DMEM) and Nutrient mixture F12 HAM, Kaighn's (Ham's F12K) were purchased from Merck (Darmstadt, Germany) and Sigma-Aldrich (St. Louis, MO, U.S.A.). Purified deionized water was prepared by Millip...

The rhizome of Atractylodes ovata De Candolle is rich in essential oils, which are usually removed by processing. In this study, anti-oxidative abilities of essential oils and aqueous extracts of A. ovata rhizome were explored, and the influence of processing on the anti-oxidative abilities was examined. Essential oils and aqueous extracts of A. ovata were extracted by boiling water and steam distillation, respectively. Quality of these two A. ovata samples was controlled by HPLC and GC-MS system, and anti-oxidative abilities were then evaluated. Results showed that surface color of A. ovata turned to brown and chemical components were changed by processing. Contents of both atractylon and atractylenolide II decreased in the essential oils, but only the contents of atractylon decreased by processing. Atractylenolide III increased in both A. ovata samples. However, A. ovata essential oils displayed stronger anti-oxidative abilities than aqueous extracts in DPPH-scavenging, TBH-induced lipid peroxidation and catalase activity assays. Moreover, the bioactivity of essential oils from raw A. ovata was stronger than oils from processed A. ovata. On the other hand, cytotoxicity of A. ovata essential oils was stronger than that of aqueous extracts, and was more sensitive on H9C2 cell than NIH-3T3 and WI-38 cells. In contrast, stir-frying processing method increased cytotoxicity of essential oils, but the cytotoxicity was ameliorated when processed with assistant substances. The results suggested that phytochemical components and bioactivity of A. ovata were changed after processing and the essential oils from raw A. ovata showed better anti-oxidative and fewer cytotoxicity effects.