[논문]Synthetic Wogonin Derivatives Suppress Lipopolysaccharide-Induced Nitric Oxide Production and Hydrogen Peroxide-Induced Cytotoxicity

Chun Wanjoo; Lee Hee Jae; Kong Pil-Jae; Lee Gun Hee; Cheong Il-Young; Park Haeil; Kim Sung-Soo

doi:10.1007/bf02977718

Synthetic Wogonin Derivatives Suppress Lipopolysaccharide-Induced Nitric Oxide Production and Hydrogen Peroxide-Induced Cytotoxicity 원문보기

Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea, v.28 no.2, 2005년, pp.216 - 219

Chun Wanjoo (Department of Pharmacology, Kangwon National University) , Lee Hee Jae (Department of Pharmacology, Kangwon National University) , Kong Pil-Jae (Department of Pharmacology, Kangwon National University) , Lee Gun Hee (Department of Pharmacology, Kangwon National University) , Cheong Il-Young (Department of Anesthesiology, College of Medicine, Kangwon National University) , Park Haeil (College of Pharmacy, Kangwon National University) , Kim Sung-Soo (Department of Pharmacology, Kangwon National University)

Abstract ▼ AI-Helper

Wogonin (5,7-dihydroxy-8-methoxyflavone) has been reported to exhibit a variety of biological properties including anti-inflammatory and neuroprotective functions. In this study, biological activities of diverse synthetic wogonin derivatives have been evaluated in two experimental cell culture models. Inhibitory activities of wogonin derivatives on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in BV2 microglial cells and on hydrogen peroxide ($H_{2}O_2$)-induced neuronal cell death in SH-SY5Y human neuroblastoma were examined. Wogonin derivatives such as WS2 and WS3 showed more potent suppressive activities on LPS-induced NO production and $H_{2}O_2$-induced cytotoxicity than wogonin itself. In addition, thiol substitution played a minor role in enhancing the activities of the derivatives. These findings may contribute to the development of novel anti-inflammatory and neuroprotective agents derived from wogonin.

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대상 데이터

The c이Is were grown and maintained in D니becco's Modified Eagle's Medium (DMEM) supplemented with 10% fet기 bovine serum and 100 卩g/mL strepSmycin and 10 U/mL penicillin at 37°C in a humidified incubator with 5% CO₂. All experiments were carried out on s니b-confluent c니Itures.
McKinney (Mayo Clinic, Jacksonville, FL). Human neuroblastoma SH- SY5Y cells were obtained from American Type Culture Collection (Rockville, USA). The c이Is were grown and maintained in D니becco's Modified Eagle's Medium (DMEM) supplemented with 10% fet기 bovine serum and 100 卩g/mL strepSmycin and 10 U/mL penicillin at 37°C in a humidified incubator with 5% CO₂.

데이터처리

The data are expressed as mean±SEM values. The significance of the protective effects of wogonin and its derivatives was assessed by analysis of variance (ANOVA). Significant differences between drug-treated groups and control (LPS- or H₂O₂-only) were analyzed with Dunnett's test.

이론/모형

SH-SY5Y human neuroblastoma cells were challenged with 100 mM H₂O₂ for 2 hr in the presence or absence of pretreatment of each compound. Cell viability was determined using MTT assay. Data were presented as % of control value.

성능/효과

, 2004). Among 12 synthesized compounds (data not shown), only WS1 and WS2 exhibited significantly greater protec tive effects than wogonin itself, whereas other derivatives, for example, carrying chloride substit니tions failed to enhance activities (data not shown). In addition, the biological activities of derivatives were not enhanced by thiol substitutions.
In conclusion, the data demonstrated that the introchjction of certain hjnctional residues into wogonin significantly enhanced the biological activities of the parent wogonin, providing insights into the design of wogonin derivatives with optimal protective activities. However, further st니dies are necessary to determine the mechanism by which the derivatives exert greater protective actions.

후속연구

t 1999). However, further studies are necessary to determine the exact roles of diverse functional residues for the modulation of biological activities.

참고문헌 (18)

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Synthetic Wogonin Derivatives Suppress Lipopolysaccharide-Induced Nitric Oxide Production and Hydrogen Peroxide-Induced Cytotoxicity 원문보기

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Synthetic Wogonin Derivatives Suppress Lipopolysaccharide-Induced Nitric Oxide Production and Hydrogen Peroxide-Induced Cytotoxicity 원문보기

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