Biological Study of Naphthalene Derivatives with Antiinflammatory Activities

Mei Han Huang, Sheng-Nan Wu, Jih Pyang Wang, Chen Hsing Lin, Shih I. Lu, Li Fang Liao, Ai Yu Shen

Research output: Contribution to journalArticle

26 Citations (Scopus)

Abstract

In this study, 18 synthetic naphthalene derivatives were tested for their inhibitory effects on the activation of neutrophils stimulated with N-formyl-methionyl-leucyl-phenylalanine (fMLP) or phorbol myristic acetate (PMA). Some of these compounds showed significant antiinflammatory activities. In general, esterification of 1-naphthalene to compound 14 (2-hydroxymethyl-1-naphthol diacetate; TAC) enhanced the antioxidant activity. Compound 15, N,N-bis(2-hydroxy-1-naphthylmethyl) amine, has moderate inhibitory activity on neutrophils stimulated with fMLP as compared to Mannich bases of naphthylene derivatives. Either substitution at 1 or 2 position, except TAC, disfavored the inhibitory effects evoked by PMA stimulation. The influence of these compounds on the release of granule enzyme lysozyme-induced by fMLP was measured. TAC had the highest potency on the inhibition of lysozyme release from rat neutrophil degranulation. The effects of TAC on ionic currents in a mouse neuroblastoma and rat glioma hybrid cell line, NG105-18, were also investigated with the aid of the whole-cell patch-clamp technique. TAC caused an inhibitory effect on voltage-dependent L-type Ca 2+ current (I Ca,L ) with an IC 50 value of 0.8 μM. The inhibitory effect of TAC on I Ca,L may not be caused by its inhibition of superoxide formation. Such an effect may, also in part, affect neuronal function.

Original languageEnglish
Pages (from-to)261-269
Number of pages9
JournalDrug Development Research
Volume60
Issue number4
DOIs
Publication statusPublished - 2003 Dec 1

Fingerprint

methionyl-leucyl-phenylalanine
Muramidase
Acetates
Neutrophils
Anti-Inflammatory Agents
Mannich Bases
N-Formylmethionine Leucyl-Phenylalanine
Neutrophil Activation
Hybrid Cells
Esterification
Patch-Clamp Techniques
Neuroblastoma
Glioma
Superoxides
Amines
Antioxidants
Cell Line
Enzymes
naphthalene
phorbol

All Science Journal Classification (ASJC) codes

  • Drug Discovery

Cite this

Huang, M. H., Wu, S-N., Wang, J. P., Lin, C. H., Lu, S. I., Liao, L. F., & Shen, A. Y. (2003). Biological Study of Naphthalene Derivatives with Antiinflammatory Activities. Drug Development Research, 60(4), 261-269. https://doi.org/10.1002/ddr.10327
Huang, Mei Han ; Wu, Sheng-Nan ; Wang, Jih Pyang ; Lin, Chen Hsing ; Lu, Shih I. ; Liao, Li Fang ; Shen, Ai Yu. / Biological Study of Naphthalene Derivatives with Antiinflammatory Activities. In: Drug Development Research. 2003 ; Vol. 60, No. 4. pp. 261-269.
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Huang, MH, Wu, S-N, Wang, JP, Lin, CH, Lu, SI, Liao, LF & Shen, AY 2003, 'Biological Study of Naphthalene Derivatives with Antiinflammatory Activities', Drug Development Research, vol. 60, no. 4, pp. 261-269. https://doi.org/10.1002/ddr.10327

Biological Study of Naphthalene Derivatives with Antiinflammatory Activities. / Huang, Mei Han; Wu, Sheng-Nan; Wang, Jih Pyang; Lin, Chen Hsing; Lu, Shih I.; Liao, Li Fang; Shen, Ai Yu.

In: Drug Development Research, Vol. 60, No. 4, 01.12.2003, p. 261-269.

Research output: Contribution to journalArticle

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T1 - Biological Study of Naphthalene Derivatives with Antiinflammatory Activities

AU - Huang, Mei Han

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AU - Shen, Ai Yu

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