PMID- 28066137 OWN - NLM STAT- PubMed-not-MEDLINE LR - 20201001 IS - 1226-4512 (Print) IS - 2093-3827 (Electronic) IS - 1226-4512 (Linking) VI - 21 IP - 1 DP - 2017 Jan TI - Betulin suppressed interleukin-1beta-induced gene expression, secretion and proteolytic activity of matrix metalloproteinase in cultured articular chondrocytes and production of matrix metalloproteinase in the knee joint of rat. PG - 19-26 LID - 10.4196/kjpp.2017.21.1.19 [doi] AB - We investigated whether betulin affects the gene expression, secretion and proteolytic activity of matrix metalloproteinase-3 (MMP-3) in primary cultured rabbit articular chondrocytes, as well as in vivo production of MMP-3 in the rat knee joint to evaluate the potential chondroprotective effect of betulin. Rabbit articular chondrocytes were cultured and reverse transcription-polymerase chain reaction (RT-PCR) was used to measure interleukin-1beta (IL-1beta)-induced gene expression of MMP-3, MMP-1, MMP-13, a disintegrin and metalloproteinase with thrombospondin motifs-4 (ADAMTS-4), ADAMTS-5 and type II collagen. Effect of betulin on IL-1beta-induced secretion and proteolytic activity of MMP-3 was investigated using western blot analysis and casein zymography, respectively. Effect of betulin on MMP-3 protein production was also examined in vivo. The results were as follows: (1) betulin inhibited the gene expression of MMP-3, MMP-1, MMP-13, ADAMTS-4, and ADAMTS-5, but increased the gene expression of type II collagen; (2) betulin inhibited the secretion and proteolytic activity of MMP-3; (3) betulin suppressed the production of MMP-3 protein in vivo. These results suggest that betulin can regulate the gene expression, secretion, and proteolytic activity of MMP-3, by directly acting on articular chondrocytes. FAU - Ra, Ho Jong AU - Ra HJ AD - Department of Orthopedic Surgery, Gangneung Asan Hospital, College of Medicine, University of Ulsan, Gangneung 25440, Korea. FAU - Lee, Hyun Jae AU - Lee HJ AD - Department of Health Management, Sahmyook University, Seoul 01795, Korea. FAU - Jo, Ho Seung AU - Jo HS AD - Department of Orthopedic Surgery and Institute of Health Sciences, School of Medicine and Hospital, Gyeongsang National University, Jinju 52727, Korea. FAU - Nam, Dae Cheol AU - Nam DC AD - Department of Orthopedic Surgery and Institute of Health Sciences, School of Medicine and Hospital, Gyeongsang National University, Jinju 52727, Korea. FAU - Lee, Young Bok AU - Lee YB AD - Department of Orthopedic Surgery and Institute of Health Sciences, School of Medicine and Hospital, Gyeongsang National University, Jinju 52727, Korea. FAU - Kang, Byeong Hun AU - Kang BH AD - Department of Orthopedic Surgery and Institute of Health Sciences, School of Medicine and Hospital, Gyeongsang National University, Jinju 52727, Korea. FAU - Moon, Dong Kyu AU - Moon DK AD - Department of Orthopedic Surgery and Institute of Health Sciences, School of Medicine and Hospital, Gyeongsang National University, Jinju 52727, Korea. FAU - Kim, Dong Hee AU - Kim DH AD - Department of Orthopedic Surgery and Institute of Health Sciences, School of Medicine and Hospital, Gyeongsang National University, Jinju 52727, Korea. FAU - Lee, Choong Jae AU - Lee CJ AD - Department of Pharmacology, School of Medicine, Chungnam National University, Daejeon 35015, Korea. FAU - Hwang, Sun-Chul AU - Hwang SC AD - Department of Orthopedic Surgery and Institute of Health Sciences, School of Medicine and Hospital, Gyeongsang National University, Jinju 52727, Korea. LA - eng PT - Journal Article DEP - 20161221 PL - Korea (South) TA - Korean J Physiol Pharmacol JT - The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology JID - 9709505 EIN - Korean J Physiol Pharmacol. 2017 Mar;21(2):275. PMID: 28280422 PMC - PMC5214907 OTO - NOTNLM OT - Betulin OT - Chondrocyte OT - Metalloproteinase OT - Osteoarthritis COIS- The authors have no conflicts of interest to declare. EDAT- 2017/01/10 06:00 MHDA- 2017/01/10 06:01 PMCR- 2017/01/01 CRDT- 2017/01/10 06:00 PHST- 2016/06/15 00:00 [received] PHST- 2016/08/18 00:00 [revised] PHST- 2016/08/19 00:00 [accepted] PHST- 2017/01/10 06:00 [entrez] PHST- 2017/01/10 06:00 [pubmed] PHST- 2017/01/10 06:01 [medline] PHST- 2017/01/01 00:00 [pmc-release] AID - 10.4196/kjpp.2017.21.1.19 [doi] PST - ppublish SO - Korean J Physiol Pharmacol. 2017 Jan;21(1):19-26. doi: 10.4196/kjpp.2017.21.1.19. Epub 2016 Dec 21.