6,7-Dihydroxycoumarin(Esculetin) has various biological and pharmaceutical properties including anti-edema, anti-inflammatory, anti-tumour, hepatoprotective, anti-osteoarthritis and anti-rheumatoid arthritis effects. It inhibits lipoxygenases (LOs), p42/44 MAPK activation, PI3-kinase activation, as well as NF-kappaB and AP-1 activation, it exhibits competitive inhibition against the oxidation of 3-(3,4-dihydroxyphenyl)- alanine by mushroom, the IC50 value of is 43 microM.
Ginsenoside Ro has antioxidative properties against UV-B-induced oxidative stress in human dermal fibroblasts, it possesses a potential skin anti-photoaging property against UV-B radiation in fibroblasts. It also exerts anti-apoptosis and anti-inflammation in IL-1β-induced rat chondrocytes, which might be related to NF-κB signal pathway, it might be a potential novel drug for the treatment of osteoarthritis. Ginsenoside Ro enhances in vivo hair re-growth based on their inhibitory activity against 5αR in the androgenetic alopecia model, it shows immunomodulatory effects by regulating the production and expression of Th1/Th2 cytokines in murine splenocytes.
Chondroitin sulfate has anti-inflammatory and chondroprotective actions ,it has been widely used in the treatment of osteoarthritis. Chondroitin sulfate reduces inflammation mediators and the apoptotic process and is able to reduce protein production of inflammatory cytokines, iNOS and MMPs.Chondroitin sulfate is a regulator of neuronal patterning in the retina, in the developing mammalian retina, gradual regression of chondroitin sulfate may help control the onset of ganglion cell differentiation and initial direction of their axons.
Glucosamine sulfate has environmental antibacterial activity. Glucosamine sulfate could as a safe symptomatic Slow Acting Drug for osteoarthritis, it can stimulate proteoglycan synthesis by chondrocytes and has mild anti-inflammatory properties, it is therefore as effective as ibuprofen on symptoms of knee osteoarthritis.
Bavachin is a phytoestrogen that activates the estrogen receptors ERα and ERβ with EC50s of 320 and 680 nM, respectively. It is a cholesterol acyltransferase inhibitor, may have therapeutic potential for type 2 diabetes by activating insulin signaling pathways. Bavachin can stimulate the genetic expression of VEGF in PB,and directly help the fracture healing, and potentially protect cartilage from inflammation-mediated damage in joints of osteoarthritis patients through decreasing IL-1β-induced activation of IKK-IκBα-NF-κB signaling pathway. Bavachin has suppressive effects against pigmentation by melanin in the skin.