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 language | English |
|---|---|
| Pages (from-to) | 261-269 |
| Number of pages | 9 |
| Journal | Drug Development Research |
| Volume | 60 |
| Issue number | 4 |
| DOIs | |
| Publication status | Published - 2003 Dec 1 |
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All Science Journal Classification (ASJC) codes
- Drug Discovery
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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 journal › Article
TY - JOUR
T1 - Biological Study of Naphthalene Derivatives with Antiinflammatory Activities
AU - Huang, Mei Han
AU - Wu, Sheng-Nan
AU - Wang, Jih Pyang
AU - Lin, Chen Hsing
AU - Lu, Shih I.
AU - Liao, Li Fang
AU - Shen, Ai Yu
PY - 2003/12/1
Y1 - 2003/12/1
N2 - 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.
AB - 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.
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U2 - 10.1002/ddr.10327
DO - 10.1002/ddr.10327
M3 - Article
AN - SCOPUS:0344012562
VL - 60
SP - 261
EP - 269
JO - Drug Development Research
JF - Drug Development Research
SN - 0272-4391
IS - 4
ER -