Abstract
Four new streptoglycerides E–H (1–4), with a rare 6/5/5/-membered ring system, were isolated from a marine-derived actinomycete Streptomyces specialis. The structures of 1–4 were elucidated by detailed analysis of HRESIMS, 1D and 2D NMR data and ECD spectra as well as comparison of their spectroscopic data with those reported in literature. Compounds 1–4 showed significant anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-induced nitric oxide (NO) production in Raw 264.7 cells with IC50 values ranging from 3.5 to 10.9 µM. Especially, 2 suppressed mRNA expression levels of iNOS and IL-6 without cytotoxicity.
Highlights
Inflammation is a normal defense mechanism that occurs to cope with tissue damage and microbial infection [1]
When tissues are exposed to LPS, nitric oxide (NO) and cytokines such as interleukins (IL-6 and IL-1β), and tumor necrosis factor-α (TNF-α) are produced naturally [2,3]
To further investigate whether the effects of 2 were due to its effects on the mRNA expression of cognate genes, we examined the effect of 2 on the mRNA expression of inducible nitric oxide synthase and IL-6 by qPCR
Summary
Inflammation is a normal defense mechanism that occurs to cope with tissue damage and microbial infection [1]. When tissues are exposed to LPS, NO and cytokines such as interleukins (IL-6 and IL-1β), and tumor necrosis factor-α (TNF-α) are produced naturally [2,3]. The uncontrolled cytokine overproduction promotes a variety of diseases [4]. NO and interleukins play a central role in the pathogenesis of inflammation owing to overproduction under abnormal physiological conditions [5,6]. There have been many reports on marine natural products with antiinflammatory activity [9,10,11]. Marine organisms inhabiting extreme environments have adopted unique survival strategies for growing and reproducing under hostile conditions, biosynthesizing molecules valuable for pharmaceutical applications [12,13].
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