Anti-Inflammatory Effects of Aurantio-Obtusin from Seed of Cassia obtusifolia L. through Modulation of the NF-κB Pathway

Abstract

Aurantio-obtusin, an anthraquinone compound, isolated from dried seeds of Cassia obtusifolia L. (syn. Senna obtusifolia; Fabaceae) and Cassia tora L. (syn. Senna tora). Although the biological activities of Semen Cassiae have been reported, the anti-inflammatory mechanism of aurantio-obtusin, its main compound, on RAW264.7 cells, remained unknown. We investigated the anti-inflammatory effect of aurantio-obtusin on lipopolysaccharide- (LPS)-induced RAW264.7 cells in vitro and elucidated the possible underlying molecular mechanisms. Nitric oxide production (NO) and prostaglandin E2 (PGE2) were measured by the Griess colorimetric method and enzyme-linked immunosorbent assay (ELISA), respectively. Protein expression levels of cyclooxygenase 2 (COX-2) were monitored by cell-based ELISA. Interleukin 6 (IL-6) and tumor necrosis factor-alpha (TNF-α) synthesis were analyzed using ELISA. The mRNA expression of nitric oxide synthase (iNOS), COX-2, and the critical pro-inflammatory cytokines (IL-6 and TNF-α) were detected by quantitative real-time PCR. Aurantio-obtusin significantly decreased the production of NO, PGE2, and inhibited the protein expression of COX-2, TNF-α and IL-6, which were similar to those gene expression of iNOS, COX-2, TNF-α and IL-6 (p < 0.01). Consistent with the pro-inflammatory gene expression, the Aurantio-obtusin efficiently reduced the LPS-induced activation of nuclear factor-κB in RAW264.7 cells. These results suggested that aurantio-obtusin may function as a therapeutic agent and can be considered in the further development of treatments for a variety of inflammatory diseases. Further studies may provide scientific evidence for the use of aurantio-obstusin as a new therapeutic agent for inflammation-related diseases.

Jinmaitong, a Traditional Chinese Compound Prescription, Ameliorates the Streptozocin-Induced Diabetic Peripheral Neuropathy Rats by Increasing Sciatic Nerve IGF-1 and IGF-1R Expression

“…Rhein, chrysophanol, and aurantio-obstusin were identified from Semen Cassiae. Studies highlight their effects on improving insulin secretion (Du et al, 2012), enhancing insulin-dependent glucose transport (Lee and Sohn, 2008), anti-oxidative, anti-hypertension, anti-mutagenic, anti-genotoxic, anti-allergic, and neuroprotective effects (Hou et al, 2018). Hyperoside, astragalin, quercetin, isoquercitrin, and kaempferol were all identified from Semen Cuscutae.…”

Urine Metabolomics Study on Potential Hepatoxic Biomarkers Identification in Rats Induced by Aurantio-Obtusin

“…It was firstly used as the quality standard of Cassiae semen in 2010 edition of Chinese Pharmacopoeia, and the content of aurantio-obtusin in Cassiae semen should not be less than 0.080%. At present, the research of aurantio-obtusin is mainly focused on its anti-inflammatory effect ( Hou et al., 2018 ; Kwon et al., 2018 ), and there is little toxicological evaluation on aurantio-obtusin. Anthraquinones are the main active components of Cassiae semen, mainly including rhein, emodin, aloe-emodin, chrysophanol, physcion, chryso-obtusin, obtusifolin, obtusin, and aurantio-obtusin ( Xie et al., 2019 ).…”

Antidiabetic potential of anthraquinones: A review

“…Obtusifolin and gluco‐obtusifolin were shown to inhibit the activities of α‐glucosidases (IC 50 obtusifolin: 142.12 μM; gluco‐obtusifolin: 23.77 μM; Jung et al, ). Hou et al () have reported that aurantio‐obtusin attenuated cytokine‐induced pancreatic β‐cell damage in RAW264.7 cells. Jang et al () have reported the potential of aurantio‐obtusin to inhibit aldose reductase activity with IC 50 value of 13.6 μM.…”