Synthesis and inhibitory effect of cis-guggulsterone on lipopolysaccharide-induced production of nitric oxide in macrophages |
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| Institution: | 1. Department of Food Science and Biotechnology, Kyonggi University, Suwon 16227, Republic of Korea;2. Natural Product Research Center, Korea Institute of Science and Technology, Gangneung 25451, Republic of Korea;3. Convergent Research Center for Dementia, Korea Institute of Science and Technology, Seoul 02792, Republic of Korea;4. Department of Biological Chemistry, Korea University of Science and Technology, Daejeon 34113, Republic of Korea;5. Research Group of Functional Food Materials, Korea Food Research Institute, Wanju 55365, Republic of Korea;6. Department of Food and Nutrition, Gachon University, Gyeonggi-do 13120, Republic of Korea;7. College of Korean Medicine, Gachon University, Seongnam 13120, Republic of Korea;1. Convergence Research Center for Dementia, Korea Institute of Science and Technology, Seoul 02792, Republic of Korea;2. Department of Biochemistry and Molecular Biology, College of Dentistry, Institute of Oral Science, Gangneung Wonju National University, Gangneung 25457, Republic of Korea;3. Department of Anatomy, College of Dentistry, Institute of Oral Science, Gangneung Wonju National University, Gangneung 25457, Republic of Korea;4. Natural Product Research Center, Korea Institute of Science and Technology, Gangneung 25451, Republic of Korea;5. Natural Product Informatics Research Center, Korea Institute of Science and Technology, Gangneung 25451, Republic of Korea;6. Division of Bio-medical Science & Technology, University of Science and Technology, Daejun 34113, Republic of Korea.;1. Institute of Food Industrialization, Institutes of Green Bio Science & Technology and Graduate School of International Agricultural Technology, Seoul National University, Pyeongchang-gun, Gangwon-do, 25354, Republic of Korea;2. Convergence Research Center for Dementia, KIST, Seoul, 02792, Republic of Korea;3. Natural Constituent Research Center, KIST Gangneung Institute of Natural Products, Gangneung, Gangwon-do, 25451, Republic of Korea;4. Radiation Research Division, Korea Atomic Energy Research Institute, Jeongeup, 56212, Republic of Korea;5. National Instrumentation Center for Environmental Management, Seoul, 151-742, Republic of Korea;6. Department of English, Hongik University, Seoul, 04066, Republic of Korea;7. Department of Biotechnology and Medical Engineering, National Institute of Technology, Rourkela, 769008, India;1. Natural Product Research Center, Korea Institute of Science and Technology (KIST), Gangneung 25451, Republic of Korea;2. Convergent Research Center for Diagnosis, Treatment, and Care System of Dementia, Korea Institute of Science and Technology (KIST), Seoul 02792, Republic of Korea;3. Natural Product Informatics Research Center, Korea Institute of Science and Technology (KIST), Gangneung 25451, Republic of Korea;4. Department of Biotechnology, Vietnam-Korea Institute of Science and Technology (VKIST), Hanoi, Viet Nam;5. Institute of Food Industrialization, Institutes of Green Bio Science & Technology and Graduate School of International Agricultural Technology, Seoul National University, Pyeongchang-gun, Gangwon-do 25354, Republic of Korea;6. Department of Anatomy, College of Dentistry, Gangnueng Wonju National University (GWNU), Gangneung 25457, Republic of Korea;7. Department of Biochemistry and Molecular Biology, College of Dentistry, Gangneung Wonju National University (GWNU), Gangneung 25457, Republic of Korea;8. Division of Bio-Medical Science and Technology, University of Science and Technology (UST), Daejun 34113, Republic of Korea;1. Dipartimento di Scienze Chimiche e Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17, I-44121, Ferrara, Italy;2. Servicio de NMR, Centro de Química y Materiales de Aragón (CEQMA), Universidad de Zaragoza, CSIC, E-50009, Zaragoza, Aragón, Spain;3. Departamento de Síntesis y Estructura de Biomoléculas, Instituto de Síntesis Química y Catálisis Homogénea (ISQCH), Universidad de Zaragoza, CSIC, E-50009, Zaragoza, Aragón, Spain;1. College of Korean Medicine, Gachon University, Seongnam 13120, South Korea;2. Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University, Seoul 02447, South Korea;3. Department of Fundamental Pharmaceutical Sciences, Graduate School, Kyung Hee University, Seoul 02447, South Korea;4. Department of Pediatrics, College of Korean Medicine, Daejeon University, Daejeon, South Korea;5. Department of Herbal Pharmacology, College of Korean Medicine, Kyung Hee University, Seoul 02447, South Korea |
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| Abstract: | Guggulsterone is a bioactive plant sterol naturally found in migratory plants. It exists in various forms, and its active compounds include the isomers cis-guggulsterone (E-GS) and trans-guggulsterone (Z-GS). In this study, the anti-inflammatory effects of these two isomeric pregnadienedione steroids were investigated against lipopolysaccharide-induced inflammatory reaction in RAW264.7 mouse macrophages. Our results showed that both guggulsterones inhibited the production of NO in macrophages treated with lipopolysaccharide, with IC50 values ranging from 3.0 to 6.7 μM. E-GS exerted higher efficacy than Z-GS, and its anti-inflammatory effects was mediated through inhibition of iNOS and COX-2 expression. |
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| Keywords: | Guggulsterone Inflammation iNOS COX-2 RAW264 7 |
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