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天然抗肿瘤药物的微生物转化:使用增溶剂提高羟基化玫瑰树碱的产量

Microbial transformations of natural antitumor agents: use of solubilizing agents to improve yields of hydroxylated ellipticines.

作者信息

Chien M M, Rosazza J P

出版信息

Appl Environ Microbiol. 1980 Oct;40(4):741-5. doi: 10.1128/aem.40.4.741-745.1980.

DOI:10.1128/aem.40.4.741-745.1980
PMID:7425624
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC291654/
Abstract

Aromatic hydroxylation of the antitumor alkaloid ellipticine by Aspergillus alliaceus results in the formation of both 8- and 9-hydroxyellipticines. Experiments designed to increase yields of microbial hydroxylation focused on enhancing the water solubility of ellipticine in aqueous fermentation media by use of wetting agents or solubilizing polymers, or both. Yields of hydroxylated metabolites were determined by high-performance liquid chromatography with the use of a mu-Bondapak-phenyl column and a mobile phase of acetonitrile--0.1% (NH4)2CO3 (1:1). Polyvinylpyrrolidone (molecular weight, 40,000) and polyoxyethylated vegetable oil (Emulphor 620) increased the water solubility of ellipticine and the yield of hydroxylated metabolites.

摘要

蒜曲霉对抗肿瘤生物碱玫瑰树碱的芳族羟基化作用会生成8-羟基玫瑰树碱和9-羟基玫瑰树碱。旨在提高微生物羟基化产量的实验着重于通过使用湿润剂或增溶聚合物或两者兼用来提高玫瑰树碱在水发酵培养基中的水溶性。羟基化代谢物的产量通过高效液相色谱法测定,使用μ-Bondapak-苯基柱和乙腈–0.1% (NH4)2CO3 (1:1)的流动相。聚乙烯吡咯烷酮(分子量40,000)和聚氧乙烯化植物油(乳化剂620)提高了玫瑰树碱的水溶性以及羟基化代谢物的产量。

相似文献

1
Microbial transformations of natural antitumor agents: use of solubilizing agents to improve yields of hydroxylated ellipticines.天然抗肿瘤药物的微生物转化:使用增溶剂提高羟基化玫瑰树碱的产量
Appl Environ Microbiol. 1980 Oct;40(4):741-5. doi: 10.1128/aem.40.4.741-745.1980.
2
Microbial transformations of natural antitumor agents. VIII. Formation of 8- and 9-hydroxyellipticines.
Drug Metab Dispos. 1979 Jul-Aug;7(4):211-4.
3
Dissolution and absorption of the antineoplastic agent ellipticine.抗肿瘤药物玫瑰树碱的溶解与吸收
J Pharm Sci. 1978 May;67(5):611-4. doi: 10.1002/jps.2600670509.
4
Aromatic hydroxylation of ellipticine in rats: lack of an NIH shift.
Biomed Mass Spectrom. 1976 Dec;3(6):335-9. doi: 10.1002/bms.1200030612.
5
Bioactivation of the antitumor drugs 9-hydroxyellipticine and derivatives by a peroxidase-hydrogen peroxide system.过氧化物酶-过氧化氢体系对抗肿瘤药物9-羟基玫瑰树碱及其衍生物的生物活化作用。
J Med Chem. 1981 Mar;24(3):289-95. doi: 10.1021/jm00135a010.
6
Characterization of the metabolites of ellipticine in rat bile.
Drug Metab Dispos. 1978 Sep-Oct;6(5):542-8.
7
The hydroxylation of the antitumor agent, ellipticine, by liver microsomes from differently pretreated rats.
Biochem Pharmacol. 1977 Nov 15;26(22):2169-73. doi: 10.1016/0006-2952(77)90270-2.
8
Effects of the 6-alkyl substitution of ellipticine on the uptake by NIH-3T3 cells and on the cytotoxicity.玫瑰树碱的6-烷基取代对NIH-3T3细胞摄取及细胞毒性的影响。
Anticancer Res. 1988 Jan-Feb;8(1):191-6.
9
Evidence for electrophilic properties of N2-methyl-9-hydroxy ellipticinium acetate (Celiptium) from human biliary metabolites.
Cancer Chemother Pharmacol. 1985;15(1):63-5. doi: 10.1007/BF00257297.
10
Microbial transformations of natural antitumor agents. 9. O-Demethylation of 9-methoxyellipticine.天然抗肿瘤药物的微生物转化。9. 9-甲氧基玫瑰树碱的O-去甲基化反应
J Nat Prod. 1979 Nov-Dec;42(6):643-7. doi: 10.1021/np50006a010.

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Dissolution and absorption of the antineoplastic agent ellipticine.抗肿瘤药物玫瑰树碱的溶解与吸收
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