- Resveratrol, found in black grapes, berries and red wine) and curcumin (found in turmeric) are proven anti-inflammatory, antioxidant and anti-ageing natural molecules, but heir absorption and instability limit their clinical use.
- Liposomal and other enhanced absorption and stability forms are already sued in supplements and cosmetics with the combination of the two natural chemicals providing synergistic results.
- Now scientists have created hybrids of curcumin and resveratrol which possess increased anti-inflammatory activity and proved their efficacy on acute lung injury, hoping that these compounds can lead to the development of new drugs against inflammatory conditions.
- In the meantime, the stabilised forms of high purity resveratrol and curcumin already provide valuable anti-ageing, anti-inflammatory and antioxidant benefits in a group of select skin care products, if used in high concentrations.
- Source: Development of resveratrol-curcumin hybrids as potential therapeutic agents for inflammatory lung diseases.
- Abstract: Acute lung injury (ALI) is a major cause of acute respiratory failure in critically-ill patients. Resveratrol and curcumin are proven to have potent anti-inflammatory efficacy, but their clinical application is limited by their metabolic instability. Here, a series of resveratrol and the Mono-carbonyl analogs of curcumin (MCAs) hybrids were designed and synthesized by efficient aldol construction strategy, and then screened for anti-inflammatory activities in vitro and in vivo. The results showed that the majority of analogs effectively inhibited the LPS-induced production of IL-6 and TNF-α. Five analogs, a9, a18, a19, a20 and a24 exhibited excellent anti-inflammatory activity in a dose-dependent manner along with low toxicity in vitro. Structure activity relationship study revealed that the electron-withdrawing groups at meta-position and methoxyl group (OCH3) at the para position of the phenyl ring were important for anti-inflammatory activities. The most promising compound a18 decreased LPS induced TNF-α, IL-6, IL-12, and IL-33 mRNA expression. Additionally, a18 significantly protected against LPS-induced acute lung injury in the in vivo mouse model. The research of resveratrol and MCAs hybrids could bring insight into the treatment of inflammatory diseases and compound a18 may serve as a lead compound for the development of anti-ALI agents.
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