• Title/Summary/Keyword: bromotyrosine

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Studies on the ${\beta}-Tyrosinase$ -Part 2. On the Synthesis of Halo-tyrosine by ${\beta}-Tyrosinase$- (${\beta}-Tyrosinase$에 관한 연구 -제2보 ${\beta}-Tyrosinase$에 의한 Halogen화(化) Tyrosine의 합성(合成)-)

  • Kim, Chan-Jo;Nagasawa, Toru;Tani, Yoshiki;Yamada, Hideaki
    • Applied Biological Chemistry
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    • v.22 no.4
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    • pp.198-209
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    • 1979
  • L-Tyrosine, 2-chloro-L-tyrosine, 2-bromo-L-tyrosine, and 2-iodo-L-tyrosine were synthesized by ${\beta}-tyrosinase$ obtained from cells of Escherichia intermedia A-21, through the reversal of the ${\alpha},{\beta}-elimination$ reaction, and their molecular structures were analyzed by element analysis, NMR spectroscopy, mass spectrometry and IR spectroscopy. Rates of synthesis and hydrolysis of halogenated tyrosines by ${\beta}-tyrosinase$, inhibition of the enzyme activity by halogenated phenols, and effects of addition of m-bromophenol on the synthesis of 2-bromotyrosine were determined. The results obtained were as follows: 1) In the synthesis of halogenated tyrosines, the yield of 2-chlorotyrosine from m-chlorophenol were approximately 15 per cent, that of 2-bromotyrosine from m-bromophenol 13.8 per cent, and that of 2-iodotyrosine from m-iodophenol 9.8 per cent. 2) Rate of synthesis of halogenated tyrosines by ${\beta}-tyrosinase$ was slower than that of tyrosine and the rates were decreased in the order of chlorine, bromine and iodine, that is, by increasing the atomic radius. Relative rate of 2-chlorotyrosine synthesis was determined to be 28.2, that of 2-bromotyrosine to be 8.13, and that of 2-iodotyrosine to be 0.98, respectively, against 100 of tyrosine. However 3-iodotyrosine was not synthesized by the enzyme. 3) The relative rate of 2-chlorotyrosine hydrolysis by ${\beta}-tyrosinase$ was 70.7, that of 2-bromotyrosine was 39.0, and that of 2-iodotyrosine was 12.6 against 100 of tyrosine, respectively. The rate of hydrolysis appeared to be decreased in the order of chlorine, bromine and iodine, that is, by increasing the atomic radius or by decreasing the electronegativity. But 3-iodotyrosine was not hydrolyzed by the enzyme. 4) The activity of ${\beta}-tyrosinase$ was inhibited by phenol markedly. Of the halogenated phenols, o-, or m-chlorophenol and o-bromophenol gave marked inhibition on the enzyme action, however inhibition by iodophenol was not strong. Plotting by Lineweaver-Burk method, a mixed-type inhibition by m-chlorophenol was observed and its Ki value was found to be $5.46{\times}10^{-4}M$. 5) During the synthesizing reaction of 2-bromotyrosine by the enzyme, sequential addition of substrate which was m-bromophenol with time intervals and in a small amount resulted in better yield of the product. 6) The halogenated tyrosines which were produced by ${\beta}-tyrosinase$ from pyruvate, ammonia and m-halogenated phenols were analysed to determine their molecular structures by element analysis, NMR spectroscopy, mass spectrometry, and IR spectroscopy. The result indicated that they were 2-chloro-L-tyrosine, 2-bromo-L-tyrosine, and 2-iodo-L-tyrosine, respectively.

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Cytotoxic Effects of Furanosesterterpenes, Cyclitol Derivatives, and Bromotyrosine Derivative Isolated from Marine Sponges

  • Sohn, Jae-Hak;Oh, Hyun-Cheol;Jung, Jee-H.;Bae, Song-Ja
    • Preventive Nutrition and Food Science
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    • v.10 no.3
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    • pp.257-261
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    • 2005
  • Marine sponges are known to produce a number of cytotoxic secondary metabolites. In the course of searching for cytotoxic metabolites from marine organisms, we have evaluated cytotoxic activities of six marine secondary metabolites isolated from various sponges. The cytotoxic compounds 1-6 were isolated by the application of various chromatographic methods, including column chromatography and HPLC. The molecular structures were mostly determined using mass spectrometry (MS) and Nuclear Magnetic Resonance (NMR) Spectroscopy. Furanosestererpenes (compounds 1-3) from Psammocinia sp., cyclitol derivatives (compounds 4 and 5) from Sarcotragus sp., and bromotyrosine-type compound (6) from an association of two sponges Jaspis wondoensis and Poecillastra wondoensis were evaluated for their cytotoxic activity against three cancer cell lines; Hep G2, HeLa, and MCF-7. All tested compounds exhibited cyctoxicity at concentrations ranging from $5\;\mug/mL\;to\;25\;\mug/mL.$ Particularly, among the tested compounds, compound 6 showed the highest potency displaying at least $80\%$ of cytotoxicity at $5\;\mug/mL$ level against all three cancer cell lines.

Psammaplin A, a Natural Bromotyrosine Derivative from a Sponge, Possesses the Antibacterial Activity against Methicillin-resistant Staphylococcus aureus and the DNA Gyrase-inhibitory Activity

  • Kim, Do-Yeob;Lee, Il-Sun;Jung, Jee-Hyung;Yang, Sung-Il
    • Archives of Pharmacal Research
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    • v.22 no.1
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    • pp.25-29
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    • 1999
  • Psammaplin A, a natural bromotyrosine derivative from an associated form of two sponges (Poecillastra sp. and jaspis sp.) was found to possess the antimicrobial effect on the Gram-positive bacteria, especially on methicillin-resistant Staphylococcus aureus (MRSA). The minimal inhibitory concentration of psammaplin A against twenty one MRSAs ranged from 0.781 to 6.25 ${\mu}g/ml$, which that of ciprofloxacin was 0.391~3.125${\mu}g/ml$. Psammaplin A could not bind to penicillin binding protein, but inhibited the DNA synthesis and the DNA gyrase activity with the respective 50% (DNA synthesis) and 100% (DNA gyrase) inhibitory concentration 2.83 and 100 ${\mu}g/ml$. These results indicate that psammaplin A has a considerable antibacterial activity, although restricted to a somewhat narrow range of bacteria, probably by inhibiting DNA gyrase.

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Bioactive Metabolites from Selected Sponges of Korean and Tropical Waters

  • Shin, Jong-Heon;Park, Jung-Rae;Seo, Young-Wan;Lee, Hyi-Seung;Cho, Ki-Woong
    • Proceedings of the PSK Conference
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    • 2001.04a
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    • pp.90-94
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    • 2001
  • Wondonins A and B, aromatic alkaloids of an unprecedented skeletal class have been isolated form and association of the sponges Poecillastra wondoensis and Jaspis sp. In addition, four novel bromotyrosine-derived metabolites, psammaplins $A_1$ and $A_2$, aplysinellins A and B, have been isolated from the tropical sponge Aplysinella rhax. The structures of these compounds have been determined on the basis of combined chemical and spectral analyses. The new compounds exhibited significant cytotoxicity and antiangiogenic activity as well as inhibitory activities against farnesyl protein transferase and leucine aminopeptidase. In addition to these compounds, several bioactive metabolites have been isolated from sponges of Korean and tropical waters.

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