Dual biological functions of the apoptotic activity and anti-inflammatory effect by alcyonolide congeners from the Okinawan soft coral, Cespitularia sp.
In our current study, alcyonolide and its congeners isolated from the Okinawan soft coral, Cespitularia sp., have shown an antitumor activity in HCT116 colon cancer cells. This study investigated the biological activities of these compounds (1-12) for the apoptotic activity in the HCT116 cells and the anti-inflammatory effect in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. As a result, the apoptotic cells with a nuclear condensation were detected by treatment with these compounds. The apoptotic cells dependent on the caspase 3/7 activation was also induced in the low concentration range of 2.5-10 μM. While a similar concentration of the compounds inhibited the NO production in the LPS-stimulated inflammatory RAW264.7 cells, the pro-inflammatory gene expressions of the iNOS and COX-2 mRNA were also suppressed. The structurally unique alcyonolides (5, 12) having the dual biological activity of apoptotic activity and anti-inflammatory effect could be a potential development as pharmaceutical agents.
Okinawa National College of Technology, Nago, Okinawa 905-2192, Japan. Electronic address: taira@okinawa-ct.ac.jp.
Junsei
J
Taira
Okinawa National College of Technology, Nago, Okinawa 905-2192, Japan.
Eito
E
Tsuchida
Okinawa National College of Technology, Nago, Okinawa 905-2192, Japan.
Masatsugu
M
Uehara
Okinawa National College of Technology, Nago, Okinawa 905-2192, Japan.
Yuki
Y
Kinjyo
University of the Ryukyus, Nishihara, Okinawa 903-2013, Japan.
Prodip K
PK
Roy
University of the Ryukyus, Nishihara, Okinawa 903-2013, Japan.
Katsuhiro
K
Ueda
D000818:Animals; D037421:Anthozoa / Q000737:chemistry*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D051546:Cyclooxygenase 2 / Q000235:genetics / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D045325:HCT116 Cells; D006801:Humans; D007783:Lactones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D008070:Lipopolysaccharides / Q000037:antagonists & inhibitors / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure; D009569:Nitric Oxide / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D052247:Nitric Oxide Synthase Type II / Q000037:antagonists & inhibitors / Q000235:genetics; D011753:Pyrones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; D007783:Lactones; D008070:Lipopolysaccharides; D011753:Pyrones; D009569:Nitric Oxide; C496319:NOS2 protein, human; D052247:Nitric Oxide Synthase Type II; D051546:Cyclooxygenase 2
Alcyonolide; Anti-inflammatory; Apoptosis; Nitric oxide; iNOS