Anti-Inflammatory Effects of Cajaninstilbene Acid and Its Derivatives

Abstract

Cajaninstilbene acid (CSA) is one of the active components isolated from pigeon pea leaves. In this study, anti-inflammatory effects of CSA and its synthesized derivatives were fully valued with regard to their activities on the production of nitric oxide (NO) and pro-inflammatory cytokines tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) in vitro cell model, as well as their impacts on the migration of neutrophils and macrophages in fluorescent protein labeled zebrafish larvae model by live image analysis. Furthermore, the anti-inflammatory mechanism of this type of compounds was clarified by western-blot and reverse transcription-polymerase chain reaction (RT-PCR). The results showed that CSA, as well as its synthesized derivatives 5c, 5e and 5h, exhibited strong inhibition activity on the release of NO and inflammatory factor TNF-α and IL-6 in lipopolysaccharides (LPS)-stimulated murine macrophages. CSA and 5c greatly inhibited the migration of neutrophils and macrophages in injury zebrafish larvae. CSA and 5c treatment greatly inhibited the phosphorylation of proteins involved in nuclear factor kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) pathways. Moreover, we found that peroxisome proliferator-activated receptor gamma (PPARγ) inhibitor GW9662 could reverse partly the roles of CSA and 5c, and CSA and 5c treatment greatly resist the decrease of PPARγ mRNA and protein induced by LPS stimulation. Our results identified the promising anti-inflammatory effects of CSA and its derivatives, which may serve as valuable anti-inflammatory lead compound. Additionally, the mechanism studies demonstrated that the anti-inflammatory activity of CSA and its derivative is associated with the inhibition of NF-κB and MAPK pathways, relying partly on resisting the LPS-induced decrease of PPARγ through improving its expression.

Cajanin Stilbene Acid Inhibited Vancomycin-Resistant Enterococcus by Inhibiting Phosphotransferase System

“…We found cajanin stilbene acid (CSA) isolated from leaves of Cajanus cajan was found to be with significant anti-VRE activity. CSA showed to have antioxidant and antimicrobial activities as well as cytotoxicity toward cancer cells in previous reports (Zu et al, 2010;Wu et al, 2011;Fu et al, 2015;Huang et al, 2016). In this study, we found for the first time that CSA could significantly inhibit VRE in vitro and in vivo.…”

Cajaninstilbene acid inhibits osteoporosis through suppressing osteoclast formation and RANKL‐induced signaling pathways

“…CSA is a natural compound extracted from cajan (a perennial legume from the family Fabaceae), with roles in the treatment of diabetes (Grover et al, ), measles (Nwodo et al, ), as an antifungal (Brito et al, ) and as an antioxidant (Wang et al, ; Wei et al, ; Zhang et al, ). CSA itself was reported as being an active anti‐inflammatory agent in RAW264.7 cells (Huang et al, ), antibacterial against methicillin‐resistant staphylococcus aureus (MRSA) (Geng et al, ), antioxidative and antiapoptotic in PC12 cells (Jiang et al, ; Y. Liu et al, ), antihepatitis (X. Y. Ji et al, ), and anticancer in MCF7 cells (Kadioglu et al, ). The present study examined CSA's influence on osteoclast activity and formation and on OVX‐induced bone loss in mice.…”

“…They also possess properties that are antifungal (Brito et al, ) and antioxidant activities (Wang et al, ; Wei et al, ; Zhang et al, ). Cajaninstilbene acid (CSA; Figure a), a bioactive compound derived from pigeon pea leaves, is reported to have effective therapeutic properties, such as anti‐inflammatory (Huang et al, ), antibacterial (Geng et al, ), antioxidative (Y. Liu et al, ), antiapoptotic (Jiang et al, ), antihepatitis (X. Y.Ji et al, ), and anticancer properties (Kadioglu et al, ). There is, however, a lack of studies to determine CSA's potential therapeutic effect on pathological bone diseases such as osteoporosis.…”

Separation of six compounds from pigeon pea leaves by elution–extrusion counter‐current chromatography

“…It acts as one of the major grain legume crops as well as a good supplement of dietary essential minerals, such as vitamin and protein . Pigeon pea has highlighted its great medicinal value for treating bronchitis, coughs, fevers, inflammation, ulcers, diarrhea, jaundice, diabetes, dermatosis, blood disorders, and plasmodium disease . Moreover, pigeon pea leaves revealed the notable therapeutic effect on femoral head necrosis in Chinese folk medicine .…”