ABSTRACT
The present study was designed to isolate and purify chemical constituents from solid culture of endophyte Aspergillus terreus LQ, using silica gel column chromatography, gel filtration with Sephadex LH-20, and HPLC. Fumigaclavine I (1), a new alkaloid, was obtained, along with seven known compounds, including fumigaclavine C (2), rhizoctonic acid (3), monomethylsulochrin (4), chaetominine (5), spirotryprostatin A (6), asperfumoid (7), and lumichrome (8). The structure of compound 1 was elucidated by various spectroscopic analyses (UV, MS, 1D and 2D NMR). The in vitro cytotoxicity of compound 1 was determined by MTT assay in human hepatocarcinoma cell line SMMC-7721, showing weaker cytotoxicity, compared with cisplatin, a clinically used cancer chemotherapeutic agent.
Subject(s)
Humans , Antineoplastic Agents , Chemistry , Aspergillus , Chemistry , Cell Line, Tumor , Cell Survival , Endophytes , Chemistry , Ergot Alkaloids , Chemistry , Magnetic Resonance Spectroscopy , Molecular Structure , Oryza , MicrobiologyABSTRACT
Three compounds were isolated from solid culture of endophyte Myrothecium roridum IFB-E091 in Artemisia annua. Their structures were determined as (S)-(-)-N-[2-(3-hydroxy-2-oxo-2,3-dihydro-1H-indol-3-yl)-ethyl]-acetamide (1), N-(4-hydroxyphenethyl)acetamide (2) and asperfumoid (3), in which compound 1 was a new indole derivative. In cytotoxicity assay, the compound 1 had no obvious inhibition activity in human hepatoma cell line SMMC-7721 and human cervical carcinoma cell line HeLa.
Subject(s)
Humans , Artemisia annua , Microbiology , Cell Line, Tumor , Endophytes , Chemistry , Hypocreales , Chemistry , Indoles , ChemistryABSTRACT
Isolation and purification of chemical constituents from solid culture of endophyte Chaetomium globosum in Imperata cylindrical was performed through silica gel column chromatography, gel filtration over Sephadex LH-20 and preparative HPLC. Nine compounds were obtained and their structures were determined as chaetoglobosin F(1), chaetoglobosin Fex(2), chaetoglobosin E(3) cytoglobosin A(4), penochalasin C(S), isochaetoglobosin D (6), N-benzoylphenylalaninyl-N-benzoyphenylalaninate(7), uracil(8) and 5-methyluracil(9), respectively, based on HR-MS and NMR data and comparison with literatures. Compound 7 was isolated from Chaeeomium sp. for the first time. In vitro cytotoxicity of compounds was evaluated using MTT mothed and 1,3,4 and 5 showed inhibition activity to the human cervical carcinoma cell HeLa with IC50 values of 99.43, 23.77, 97.92, 86.25 micromol x L(-1), while positive cotolocisnin Ad apno1ch alse IC50 24.33 micromol x L(-1).
Subject(s)
Humans , Biological Factors , Chemistry , Pharmacology , Cell Line , Cell Survival , Chaetomium , Chemistry , Endophytes , Chemistry , Molecular Structure , Poaceae , Microbiology , Spectrometry, Mass, Electrospray IonizationABSTRACT
AIM@#To study the chemical constituents of the solid culture of the endophyte Phomopsis sp. IFB-E060 in Vatica mangachapoi.@*METHOD@#Isolation and purification were performed through silica gel column chromatography, gel filtration over Sephadex LH-20, ODS column chromatography, and HPLC. Structures of the isolated compounds were elucidated by a combination of spectroscopic analyses (UV, CD, IR, MS, 1D, and 2D NMR). The cytotoxicity of the isolates was evaluated in vitro by the MTT method against the human hepatocarcinoma cell line SMMC-7721.@*RESULTS@#Five compounds were isolated from the solid culture of the endophyte Phomopsis sp. IFB-E060 and their structures were identified as 18-methoxy cytochalasin J (1), cytochalasin H (2), (22E, 24S)-cerevisterol (3), ergosterol (4), and nicotinic acid (5). Compound 1 had an inhibition rate of 24.4% at 10 μg·mL(-1) and 2 had an IC50 value of 15.0 μg·mL(-1), while a positive control 5-fluorouracil had an inhibition rate of 28.7% at 10 μg·mL(-1).@*CONCLUSION@#18-Methoxy cytochalasin J (1), produced by endophytic Phomopsis sp. IFB-E060, is a new cytochalasin with weak cytotoxicity to the human hepatocarcinoma cell line SMMC-7721.
Subject(s)
Humans , Ascomycota , Chemistry , Cell Line, Tumor , Cell Survival , Cytochalasins , Chemistry , Toxicity , Endophytes , Chemistry , Magnoliopsida , Microbiology , Molecular Structure , Plant Bark , MicrobiologyABSTRACT
<p><b>OBJECTIVE</b>To study the responses of different pancreatic cancer cells to stimulations by nerve growth factor (NGF) and explore the role of Trk-A in such responses.</p><p><b>METHODS</b>Five pancreatic cancer cell lines (MIA-PaCa-2, PANC-1, SW-1990, AsPC-1, and BxPC-3) were exposed to different concentrations of NGF (0, 4, 20, 100, and 500 ng/ml). MTT and Matrigel invasion method were used to observe the changes in the cell proliferation and invasion ability. Trk-A expression in these cells was detected by PCR and Western blotting, and the relations of Trk-A expression to the cell proliferative and invasive abilities following NGF treatment were analyzed.</p><p><b>RESULTS</b>NGF at 100 ng/ml most obviously stimulated the cell proliferation, and PANC-1 cells showed the highest while AsPC-1 cells showed the least sensitivity to 100 ng/ml NGF stimulation. Matrigel invasion test showed that NGF enhanced the invasiveness of PANC-1 and MIA-PaCa-2 cells but produced only limited effect on AsPC-1 cells; the effect of NGF was completely inhibited by the Trk-A inhibitor CEP701. The expression levels of Trk-A mRNA and protein were the highest in PANC-1 cells and the lowest in AsPC-1 cells.</p><p><b>CONCLUSION</b>NGF can enhance the proliferation and invasiveness of pancreatic cancer cells, and this effect is possibly mediated by Trk-A protein.</p>
Subject(s)
Humans , Cell Line, Tumor , Cell Movement , Cell Proliferation , Neoplasm Invasiveness , Nerve Growth Factor , Pharmacology , Pancreatic Neoplasms , Metabolism , Pathology , Receptor, trkA , Genetics , MetabolismABSTRACT
<p><b>OBJECTIVE</b>To study the efficacy and toxicity of cyberknife radiosurgery for primary hepatic carcinoma.</p><p><b>METHODS</b>From September 2006 to March 2008, 17 patients with clinical stage I-III primary hepatic carcinoma were treated with cyberknife at Tianjin Cancer Hospital. 12 patients received previous treatment of surgery, or interventional therapy or radiofrequency therapy before the cyberknife radiosurgery. Totally 23 lesions in the liver were treatment. The median planning target volume (PTV) was 75 ml (13 - 351 ml). Fiducials were placed in or adjacent to the tumor one week before the CT scan simulation. The median total prescription dose was 45 Gy (range: 39 - 52 Gy) at 3-8 fractions and the median prescription isodose lines was of 78.0% (range: 75.0% - 81.0%.</p><p><b>RESULTS</b>The follow-up time was 3-30 months (median: 14 months). All patients finished the treatment and slightly fatigue was the most common complain. There were 12 patients alive and 5 patients died. All the lesions in liver treated by the cyberknife radiosurgery achieved local control.</p><p><b>CONCLUSION</b>The cyberknife radiosurgery for primary hepatic carcinoma showed a high rate of local control and minimal toxicity. Long time follow-up is necessary to evaluate the survival data and late toxicity.</p>