Chondroprotective Effects of 4,5-Dicaffeoylquinic Acid in Osteoarthritis through NF-κB Signaling Inhibition

Abstract

Osteoarthritis (OA) is characterized by cartilage degradation, inflammation, and pain. The dicaffeoylquinic acid (diCQA) isomer, 4,5-diCQA, exhibits antioxidant activity and various other health-promoting benefits, but its chondroprotective effects have yet to be elucidated. In this study, we aimed to investigate the chondroprotective effects of 4,5-diCQA on OA both in vitro and in vivo. Primary rat chondrocytes were pre-treated with 4,5-diCQA for 1 h before stimulation with interleukin (IL)-1β (5 ng/mL). The accumulation of nitrite, PGE2, and aggrecan was observed using the Griess reagent and ELISA. The protein levels of iNOS, COX-2, MMP-3, MMP-13, ADMATS-4, MAPKs, and the NF-κB p65 subunit were measured by Western blotting. In vivo, the effects of 4,5-diCQA were evaluated for 2 weeks in a destabilization of the medial meniscus (DMM)-surgery-induced OA rat model. 4,5-diCQA significantly inhibited IL-1β-induced expression of nitrite, iNOS, PGE2, COX-2, MMP-3, MMP-13, and ADAMTS-4. 4,5-diCQA also decreased the IL-1β-induced degradation of aggrecan. It also suppressed the IL-1β-induced phosphorylation of MAPKs and translocation of the NF-κB p65 subunit to the nucleus. These findings indicate that 4,5-diCQA inhibits DMM-surgery-induced cartilage destruction and proteoglycan loss in vivo. 4,5-diCQA may be a potential therapeutic agent for the alleviation of OA progression. In this study, diclofenac was set to be administered once every two days, but it showed an effect on OA. These results may be used as basic data to suggest a new dosing method for diclofenac.

In vitro Evaluation of Polyphenol Rich Fraction of Ipomea batatas (Mother delight) Leaf Extract as Anti-inflammatory Agents and its LCMS Profile

“…They reported that it involved a series of control processes, including transcription, posttranscription and post-translation, and the corresponding protein levels were dramatically reduced by naringenin treatment. The presence of 4,5-dicaffeolquinic acid was observed in this study, and its anti-inflammatory, antihepatotoxic and neuroprotective potentials were reported by Jang et al, (2022). Additionally, Kim et al, (2011) demonstrated that dicaffeolquinic acids have higher antioxidant properties, which are associated with the presence of catechol groups.…”

Quality evaluation of Lonicerae Japonicae Flos from different origins based on high‐performance liquid chromatography (HPLC) fingerprinting and multicomponent quantitative analysis combined with chemical pattern recognition

“…Chlorogenic acid, 3,5-dicaffeoylquinic acid, and 4,5-dicaffeoylquinic acid are the three phenolic acids with the highest contents in LJF, and many studies have shown that they have abundant pharmacological activity, exerting anti-inflammatory, antioxidant, antiobesity, antitumor, and antihypertensive effects. 20,21 Therefore, the total content of these three compounds was included in the Chinese Pharmacopoeia (2020 edition) as a quality control index for LJF. Taking the total content of these three compounds as evaluation index, the extraction solvent (30%, 50%, 75%, and 95% methanol) was optimized, and the results showed that the sample extracted using 75% methanol contained the largest amount (61.83 mg g À1 ), while the total content of the samples extracted using 30%, 50%, and 90% methanol was relatively low (28.45, 48.61, and 58.01 mg g À1 , respectively).…”

“…The detailed information and similarity of 39 batches of LJF. (20), (E)-aldosecologanin ( 22), 4,5-dicaffeoylquinic acid (23), and (Z)aldosecologanin (24). The chromatographic peaks were identified by comparing the PDA spectra and retention times of chromatograms between the standard substance and the samples.…”

Polysaccharides fromBalanophora harlandiiHook: Isolation, Characterization, and Anti-Inflammation Activities

“…The NO production of RAW 264.7 cells was determined according to a published protocol (Jang et al, 2022). The RAW 264.7 cells were incubated for 24 h with 1 μg/mL LPS in DMEM in 96-well plates (5 × 10 5 cells/mL) to simulate inflammation, and then incubated with crude BHPs or BHPs-W-S3 (25-100 μg) for another 24 h. The positive control group was Dexamethasone (DEX).…”