Abstract
Background Orthosiphon stamineus is used traditionally to treat gout, arthritis, and inflammatory related conditions. The in vitro anti-inflammatory effects of the plant have been scientifically investigated. The goal of the present study was to evaluate the potential of the 50% ethanol extract of O. stamineus (EOS) to treat rheumatoid arthritis.MethodsAnti-arthritic activity was assessed using the in vitro heat denaturation test and the (FCA)-induced arthritis model. Efficacy was assessed by measurements of paw edema and granulation, X-ray radiography, fluorescence molecular tomography (FMT), and histological evaluation. Levels of (TNF-α), interleukin-1 (IL-1), and (COX-1 and COX-2) were analyzed in vitro in lipopolysaccharide (LPS)-stimulated human macrophage (U937). TNF-α and IL-1 levels in the serum samples of arthritic rats were also measured using an ELISA kit.ResultsTreatment with EOS resulted in dose-dependent inhibition of paw edema in acute and chronic models of inflammation. It also inhibited significantly the production of TNF-α, IL-1 COX-1, and COX-2 in the LPS-stimulated U937 macrophages. EOS significantly suppressed FCA-induced paw edema as well as the serum levels of TNF-α and IL-1. X-rays of the synovial joint of the hind leg showed considerable improvement in joint integrity and recovery of tibia-talus bones from degeneration and osteoporotic lesions. Histology of proximal interphalangeal joints of EOS-treated animals showed obvious protection of cartilage and soft tissue. Finally, FMT analysis strongly supported the anti-arthritic effect of EOS. EOS had high phenolic and total flavonoid content as well as strong antioxidant activity.ConclusionsResults illustrated that the anti-arthritic properties of O. stamineus could be beneficial for prevention and management of rheumatoid arthritis and other chronic inflammatory disorders.Graphical abstractIllustration of the Anti- arthritis efficacy of Orthosiphon Stamineus standardized extract.
Highlights
Orthosiphon stamineus is used traditionally to treat gout, arthritis, and inflammatory related conditions
Another study reported that the ethanol extract of O. stamineus inhibited vascular endothelial growth factor (VEGF) expression and VEGF receptor (VEGFR) phosphorylation, which are known to be up-regulated during new blood vessel formation
Flavonoid rich chloroform extract fraction of O. stamineus inhibits the production of prostaglandin and NO, the activity ascribed to the rich contents of flavonoids, sinensetin and eupatorin
Summary
Orthosiphon stamineus is used traditionally to treat gout, arthritis, and inflammatory related conditions. Another study reported that the ethanol extract of O. stamineus inhibited vascular endothelial growth factor (VEGF) expression and VEGF receptor (VEGFR) phosphorylation, which are known to be up-regulated during new blood vessel formation. The antinflammatory properties of O. stamineus leaf chloroform extract have been scientifically proven, it shows a potent in vitro inhibition to pro-inflammatory mediators expression such as iNOS, COX-2 and TNF-α, as well as PGE2 and NO production [10]. In vivo treatment with O. stamineus demonstrated significant inhibitions activities against TPA -induced inflammation to mouse ears [12]. Another in vivo study using hexane fraction of O. stamineus confirmed the potent inhibition of carrageenan induced paw edema in rat [13, 14]. To the best of our knowledge, there is no antiinflammatory, in vitro and in vivo anti-arthritis have been reported using 50% ethanol extract
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