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Anti-tumor Active Ingredient And Plant Growth Resilience Agent

Posted on:2002-01-24Degree:DoctorType:Dissertation
Country:ChinaCandidate:T WangFull Text:PDF
GTID:1114360032455462Subject:Medicinal chemistry
Abstract/Summary:PDF Full Text Request
4930 strains were isolated from 289 sample of soil collected throughout China. With morphological change of Pyricularia oryzae as active index, 142 active strains of them were screened preliminarily, 6 strains of them were found to show good batch stabilities and genetic stabilities. 13 compounds were separated from No. 100-3 (Penicillium purpurogenum stoll), 121-1 (Penicillium janthinellium Biourge) and 25 4-2 strains by the use of several kinds of chromatography (such as Silica gel chromatography, Sephadex LH-20 chromatography, PTLC, HPLC) using active guidance. From Bothriochloa ischaemum (L.) Keng which had obvious plant growth promoting activity, 6 compounds were isolated. By means of spectral methods and physical and chemical evdence, 17 compounds of them were identified as 3-(I'-carboxyvinyloxy)benzoic acid (â… ), rubratoxin B (-â…¡), m-hydroxybenzoic acid (â…¢), 2-formyl-3, 5- dihydroxy-4-methylbenzoic acid (â…£), 5-(1-methyl propyl)-3, 6-dioxo-2- piperazinepanoic acid (â…¤) and 3-(4-hydroxyphenylmethyl)-1, 2, 3, 4, 6, 7, 8, 8a-octahydropyrrolo[1, 2-a]pyrazine-l, 4-dione (â…¥), verrucarin A (â…§), verrucarin I (â…¨), roridin P (Xa), isororidin P (Xa), verruracin AV (XI), f3-sitosterol (XIII), succinic acid (XIV), hexadecanoic acid (XV), tricin (XVI), 5 -hydroxy-2-(2-hydroxy phenyl)ethylchromone(XVIL) and 5-hydroxy-6-niethoxy-2-(2-hydroxyphenyl)ethylchromone (XVIII). 5 compounds of them named as V, Xa, Xb, XVII, XVIII were new metabolites, I was a new natural product, XIII, XIV, XV, XVI were isolated from Bothriochloa genus for the first time. By now 2-phenylethylchromones have been found from Aquilaria sp. only. Bioassay experiments of these compounds were carried out, which suggested that all of these compounds isolated from three strains were bioactive. Percentage of hits was 100%. compound II, VIII, IX, Xa, Xb, had strong effect of induced deformation on Pyricularia oryzae. Compound I, III, IV, V, VI showed inhibition effect on Pyricularia oryzae. The anti-BeWo in vitro suggested compound II could inhabit the growth of tumor cells at 25 ug/mL. The results of cell cycle inhibition experiment also showed this compound could inhibit the division of cell at G2 and M period at 25 ug/mL. Compound XVII and XVIII could promote the growth of the roots of wheat evidently, and could improve the drought-resistance ability of plants. At the mean time, the anti-Pyricularia oryzae activity of phenolic acids was also checked. They were found to show certain inhibition effect on Pyricularia oryzae, The relationships between the structure of these phenolic acid and the activity of antifungus were studied. On the basis of Macrocyclic Trichochecenes and 2-phenylethyl chromones isolated and the literatures, the spectral characteristics of these two kinds of compounds were conclude.
Keywords/Search Tags:soil fungi, Pyricularia oryzae, Bothriochloa ischaemum (L.) Keng, anti-tumor, plant growth regulator, bioactivity.
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