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Prevention of Lens Protein–, Endotoxin– , and Interleukin– 1– induced uveitis with chalcone derivatives

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Yao Q-S, Varma RS, Liu SXL, Chiou GCY. Prevention of lens protein-, endotoxin-, and interleukin-1-induced uveitis with chalcone derivatives. Inflammopharmacology. 1994;2:401-409.

In order to develop potent non-steroidal anti-inflammatory agents, a new class of agents unrelated to those known to inhibit the arachidonate cascade were investigated. Most of the chalcone derivatives studied, including flavanone hydrazone (RCV/FLV 574), 2’-(o-hydroxyphenol)-5-phenylpyrazoline (RCV-556Pz), 2’-acetoxychalcone-iV-monoacetylhydrazone (RVC-576) and 7V-(o-hydroxybenzoyl) morpholine (RVC-570), inhibited lens protein-induced ocular inflammation effectively at a dose level of 1% (50 μ1 as did prednisolone. Flavanone hydrazone (RCV/FLV 574) was the only compound among all these derivatives which inhibited endotoxin- and interleukin-1 (IL-1)-induced uveitis at 3 mg/kg ip tid this being approximately 7-fold more potent than prednisolone at 20 mg/kg ip tid. It is concluded that a non-steroidal non-arachidonate-mediated potent anti-inflammatory agent based on this compound could be developed with IL-1 blocking activity. However, flavanone hydrazone was rather toxic at effective doses tested. Modification of the chemical structure to reduce its side-effects would, therefore seem essential.

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Authors and Affiliations

  1. Institute of Ocular Pharmacology and Department of Medical Pharmacology and Toxicology, Texas A&M University College of Medicine, College Station, 77843, Texas, USA

    Q. -S. Yao, S. X. L. Liu & G. C. Y. Chiou

  2. DNA Technology Laboratory, Houston Advanced Research Center, 4800 Research Forest Drive, 77381, The Woodlands, Texas, USA

    R. S. Varma

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  1. Q. -S. Yao
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  2. R. S. Varma
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  3. S. X. L. Liu
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  4. G. C. Y. Chiou
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Yao, Q.S., Varma, R.S., Liu, S.X.L. et al. Prevention of Lens Protein–, Endotoxin– , and Interleukin– 1– induced uveitis with chalcone derivatives. Inflammopharmacology 2, 401–409 (1994). https://doi.org/10.1007/BF02678606

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