共查询到13条相似文献,搜索用时 46 毫秒
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农药作用靶标或作用机制的创新是农药科学研究需要解决的关键科学问题之一。对羟苯基丙酮酸双加氧酶(4-hydroxyphenylpyruvate dioxygenase, HPPD)是生物体酪氨酸代谢途径中的关键酶,在不同的生物体内参与的代谢路径不同。前期的研究表明,HPPD抑制剂在医药和除草方面发挥了较大的作用,而近期的研究发现其在抑菌和杀蚊等方面也表现出了潜在的应用价值。本文概述了HPPD在不同生物体中的生理功能,介绍了HPPD在人、植物、吸血节肢动物、真菌体内参与的代谢过程,总结了不同种属来源HPPD的三维结构,概述了HPPD作为靶标在医药以及农药(除草、杀虫、杀菌等)方面的研究现状并进行了展望。
相似文献4.
Herbicide pyrazolate causes cessation of carotenoids synthesis in early watergrass by inhibiting 4-hydroxyphenylpyruvate dioxygenase 总被引:1,自引:0,他引:1
HIROSHI MATSUMOTO MORIHIRO MIZUTANI TAKAHIRO YAMAGUCHI JUNJI KADOTANI 《Weed Biology and Management》2002,2(1):39-45
In aqueous solution, the herbicide pyrazolate [4‐(2,4‐dichlorobenzoyl)‐1,3‐dimethyl‐5‐pyrazolyl p‐toluenesulfonate] is rapidly hydrolyzed to destosyl pyrazolate (DTP), 4‐(2,4‐dichlorobenzoyl)‐1,3‐dimethyl‐5‐hydroxypyrazole, which is an active form of the herbicide. The objective of this study was to examine the effect of pyrazolate and DTP on carotenoids synthesis in susceptible weed, early watergrass (Echinochloa oryzicola Vasing.). Furthermore, their in vitro effect on 4‐hydroxyphenylpyruvate dioxygenase (HPPD) was determined. Roots of the plants at the two‐leaf stage were soaked for 24 h into pyrazolate (5 × 10–5 mol L?1) or norflurazon (10–6 mol L?1) solution containing 0.5% volume of acetone. At the first sampling time (3 days after treatment: 3 DAT), the chlorophyll content in the third leaves of pyrazolate‐treated plants were not different compared with the untreated control, but it was decreased between 3 and 6 DAT. The declining pattern of β‐carotene in the third leaf of early watergrass was very similar to that of chlorophyll. Both herbicides induced greater accumulation of phytoene in the third leaves of early watergrass 3 DAT, and the levels were kept until 9 DAT. However, feeding of homogentisate reduced the phytoene accumulation only in pyrazolate‐treated plants, suggesting the site of action of the herbicide located in the pathway of plastoquinone synthesis. In a HPPD assay, DTP revealed to inhibit the enzyme with an IC50 value of 13 nmol L?1 and that of pyrazolate was 52 nmol L?1. In the pyrazolate solution used in the assay, some of the herbicide possibly has been hydrolyzed to DTP. From the all results obtained, it is strongly suggested that pyrazolate inhibits carotenoids synthesis and causes bleaching on the developing leaves by the similar mechanism with norflurazon, but its action site is not phytoene desaturase and is HPPD. 相似文献
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Masamitsu Tsukamoto Hiroshi Kikugawa Souichiro Nagayama Taketo Suganuma Tatsuya Okita Hidenori Miyamoto 《Journal of Pesticide Science》2021,46(2):152
Tolpyralate, a new selective postemergence herbicide developed for the weed control in corn, possesses a unique chemical structure with a 1-alkoxyethyl methyl carbonate group on the N-ethyl pyrazole moiety. This compound shows high herbicidal activity against many weed species, including glyphosate-resistant Amaranthus tuberculatus. Tolpyralate targets 4-hydroxyphenylpyruvate dioxygenase (4-HPPD), which is involved in the tyrosine degradation pathway. Inhibition of the enzyme destroys the chlorophyll, thereby killing the susceptible weeds. Details of tolpyralate discovery, structure optimization, and biological activities are described. 相似文献
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Shunsuke Yamamoto Yoshitaka Tanetani Chihiro Uchiyama Atsushi Nagamatsu Masami Kobayashi Mitsumasa Ikeda Kiyoshi Kawai 《Journal of Pesticide Science》2021,46(3):249
Fenquinotrione is a novel herbicide that can control a wide range of broadleaf and sedge weeds with excellent rice selectivity. We revealed that fenquinotrione potently inhibited the 4-hydroxyphenylpyruvate dioxygenase (HPPD) activity in Arabidopsis thaliana with an IC50 of 44.7 nM. The docking study suggested that the 1,3-diketone moiety of fenquinotrione formed a bidentate interaction with Fe(II) at the active site. Furthermore, π–π stacking interactions occurred between the oxoquinoxaline ring and the conserved Phe409 and Phe452 rings, indicating that fenquinotrione competes with the substrate, similar to existing HPPD inhibitors. A more than 16-fold difference in the herbicidal activity of fenquinotrione in rice and the sedge, Schoenoplectus juncoides, was observed. However, fenquinotrione showed high inhibitory activity against rice HPPD. Comparative metabolism study suggested that the potent demethylating metabolism followed by glucose conjugation in rice was responsible for the selectivity of fenquinotrione. 相似文献
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The proposed target enzyme for benzoylcyclohexanedione herbicides, 4-hydroxyphenylpyruvate dioxygenase (HPPD) was purified from etiolated maize seedlings with a purification factor of 105. Enzyme activity was measured by detection of carbon dioxide formed from radiolabelled substrate. The enzyme has a pH optimum of 7·3 and an apparent molecular mass of 43 kDa, similar to that of the mammalian liver enzyme. Activity needs the presence of a reducing system glutathione/dichlorophenol indophenol or ascorbate and catalase. Surprisingly, a commercial catalase preparation of low specific activity—generally used for the enzyme assay—showed HPPD activity which was separable from the catalase activity on a gel filtration column. According to kinetic studies with purified maize HPPD, experimental herbicides from the family mentioned were strong competitive inhibitors of the plant enzyme in nanomolar range withKi values of 5 and 15 nM for 2-(2-nitro-4-chlorobenzoyl)-5-(2-methoxyethyl) cyclohexane- 1,3-dione and 2-(2-chloro-4-methanesulfonylbenzoyl)- cyclohexane-1,3-dione (SC-0051; sulcotrione), respectively. 相似文献
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Hausman NE Singh S Tranel PJ Riechers DE Kaundun SS Polge ND Thomas DA Hager AG 《Pest management science》2011,67(3):258-261
BACKGROUND: A population of waterhemp in a seed maize production field in central Illinois, United States, was not adequately controlled after post‐emergence applications of herbicides that inhibit 4‐hydroxyphenylpyruvate dioxygenase (HPPD). RESULTS: Progeny from the field population survived following treatment with mesotrione, tembotrione or topramezone applied to the foliage either alone or in combination with atrazine in greenhouse experiments. Dose–response experiments indicated that the level of resistance to the HPPD inhibitor mesotrione is at least tenfold relative to sensitive biotypes. CONCLUSION: These studies confirm that waterhemp has evolved resistance to HPPD‐inhibiting herbicides. Copyright © 2011 Society of Chemical Industry 相似文献
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Zlatina Naydenova Gerd-Joachim Krauss Evgeny Golovinsky Konstantin Grancharov 《Pest management science》1999,55(8):825-830
Twelve herbicides, representatives of two chemical groups, substituted phenoxyalkanoic acids and s-triazines, were tested for their inhibitory effect on the glucuronidation of 4-nitrophenol (4-NP), phenolphthalein (PPh) and 4-methylumbelliferone (4-MU) by rat liver microsomes. One millimole MCPA, ametryn and cyanazine significantly decreased PPh UDP-glucuronosyltransferase (UGT) activity, while propazine was found to be a most potent inhibitor of 4-NP glucuronidation. Concentrations of 0.1 mM dichlorprop and cyanazine were still inhibitory against PPh-UGT. The inhibition of 4-MU glucuronidation by the herbicides was low and not specific. As a whole, s-triazine derivatives were more inhibitory than the substituted phenoxyalkanoic acids. Kinetic studies with propazine revealed a non-competitive type of inhibition towards the acceptor substrate 4-NP, with an apparent Ki value of 0.540 mM . With ametryn, an uncompetitive type of inhibition against PPh and a mixed type of inhibition towards UDPGA were found, with apparent Ki values of 0.330 mM and 0.380 mM , respectively. © 1999 Society of Chemical Industry 相似文献
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Total labor time on paddy rice has been decreasing year by year with the development and introduction of appropriate herbicides, especially ‘one‐shot' herbicides. However, in the case of application of granules, it is still difficult for a farmer to apply herbicides while carrying heavy power backpack sprayers. New formulation recipes and different application technology such as a throw‐in type formulation on jumbo granules or flowable has improved heavy workloads in comparison with granule application by using heavy power backpack sprayers. In addition, other advantageous points such as application volume and elimination of the drift problems of this new application technology were introduced and confirmed. As a result of this introduction, these formulations were used in 830 000 ha and reached 30% of the total treatment area in paddy rice in 2000. 相似文献