• Korean Journal of Pharmacognosy
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• v.50 no.1
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• pp.11-17
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• 2019

Cassia tora L. have been used as a folk medicine in Korea. This study investigated anti-inflammatory effect of aurantio-obtusin isolated from C. tora. We isolated aurantio-obtusin from 50% ethanol extracts of C. tora L. We investigated the anti-inflammatory effects of aurantio-obtusin on the lipopolysaccharide (LPS)-stimulated inflammatory response in murine macrophage cell line (Raw 264.7). To investigate the cytotoxicity of aurantio-obtusin on RAW 264.7 cells, MTS assay was performed. RAW 264.7 cells were treated with aurantio-obtusin at different concentrations (12.5, 25, 50, $100{\mu}M$) for 30 h. The result showed that aurantio-obtusin had no cytotoxic effect in a concentration range of $12.5-100{\mu}M$. To determine the effect of aurantio-obtusin on LPS-induced NO production, the NO concentration measurement was performed. RAW 264.7 cells were treated with aurantio-obtusin at 12.5, 25, 50 and $100{\mu}M$ for 24 h, and the results showed that the NO production of aurantio-obtusin-treated cells compared to LPS alone treated group was significantly decreased in a dose-dependent manner. Pretreatment of aurantio-obtusin inhibited LPS-induced NO production in a dose-dependent manner. To find out inhibitory mechanisms of aurantio-obtusin on inflammatory mediators, we examined the $PGE_2$ pathways. As a result, $PGE_2$ were decreased in a dose-dependent manner by aurantio-obtusin. The release of interleukin-$1{\beta}$ (IL-$1{\beta}$) and IL-6 were also reduced. Moreover, aurantio-obtusin suppressed LPL-induced $I{\kappa}B-{\alpha}$ degradation. These results suggest that the down regulation of NO, $PGE_2$, IL-$1{\beta}$ and IL-6 expression by aurantio-obtusin are achieved by the downregulation of NF-${\kappa}B$ activity.

• Korean Journal of Pharmacognosy
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• v.32 no.2 s.125
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• pp.157-162
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• 2001

For the quality control of Cassiae Semen, anthraquinone compound, aurantio-obtusin, was isolated from the MeOH extract of Cassiae Semen (Leguminosae) and identified by the spectroscopic analysis. A quantitative analysis of aurantio-obtusin using HPLC method showed that the average contents of aurantio-obtusin were $0.03{\pm}0.01%$ in 50 samples collected throughout the various regions of Korea.

• Journal of Microbiology and Biotechnology
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• v.17 no.11
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• pp.1894-1897
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• 2007

Cassiae Semen (seeds of Cassia tora) showed a remarkably different HPLC chromatogram after being treated with a crude enzyme extract from Aspergillus usamii. Increased and decreased compounds were identified as aurantio-obtusin and glucoaurantio-obtusin, respectively. The aurantio-obtusin content reached its maximum level ($133.58{\pm}0.39\;{\mu}g/mg$ extract) after being incubated for 50 min at $37^{\circ}C$, whereas the inactivated crude enzyme-treated control remained unchanged ($54.13{\pm}1.33\;{\mu}g/mg$). On the other hand, the glucoaurantio-obtusin content decreased by less than one-third ($51.09{\pm}1.63\;{\mu}g/mg$) ofthe untreated control ($143.19{\pm}2.12\;{\mu}g/mg$), suggesting that an increase in aurantio-obtusin content originated from the enzymatic cleavage of its glucoside glucoaurantio-obtusin.

• Korean Journal of Pharmacognosy
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• v.18 no.4
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• pp.203-206
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• 1987

An activity guided fractionation of the methanol extract of Cassiae Semen yielded three platelet anti-aggregatory components, aurantio-obtusin, chryso-obtusin and emodin.

• Korean Journal of Pharmacognosy
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• v.45 no.3
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• pp.200-208
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• 2014

In this study, we performed quantification determination of four major components including aurantio-obtusin, emodin, chrysophanol, and physcion in the 70% ethanol extracts of non-processed Cassiae Semen and processed Cassiae Semen using a high-performance liquid chromatography coupled with photodiode array detector. The analytical column for separation of the 4 constituents used a Gemini $C_{18}$ column kept at $40^{\circ}C$ by the gradient elution with 1.0% (v/v) acetic acid in water and 1.0% (v/v) acetic acid in acetonitrile as mobile phase. The flow rate was 1.0 mL/min and the injection volume was $10{\mu}L$. The amount of aurantio-obtusin, emodin, chrysophanol, and physcion in non-processed Cassiae Semen were 0.07%, 0.02%, 0.25%, and 0.10%, respectively. The amount of aurantio-obtusin, emodin, chrysophanol, and physcion in processed Cassiae Semen were 0.04-0.14%, 0.01-0.03%, 0.02-0.42%, and 0.01-0.24%, respectively. Consequently, the optimal processing condition of Cassiae Semen for the improvements of amounts of four anthraquinone compounds was obtained by roasting at $240^{\circ}C$ for 15 min.

• Archives of Pharmacal Research
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• v.19 no.4
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• pp.302-306
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• 1996

The $^1H- and^{13}C-NMR$ spectra of alaternin, aurantio-obtusin, chryso-obtusin, obtusin and 2-glucosyl obtusifolin isolated from the seeds of Cassia tora have been assigned based on HMBC, long-range HETCOR, fully $^1H-coupled {13}^C-NMR$, deuterium isotope experiment, and by comparison with the model compounds.

• The Korean Journal of Physiology and Pharmacology
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• v.28 no.1
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• pp.11-19
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• 2024

Acute kidney injury (AKI) is one of the major complications of sepsis. Aurantio-obtusin (AO) is an anthraquinone compound with antioxidant and anti-inflammatory activities. This study was developed to concentrate on the role and mechanism of AO in sepsis-induced AKI. Lipopolysaccharide (LPS)-stimulated human renal proximal tubular epithelial cells (HK-2) and BALB/c mice receiving cecal ligation and puncture (CLP) surgery were used to establish in vitro cell model and in vivo mouse model. HK-2 cell viability was measured using MTT assays. Histological alterations of mouse renal tissues were analyzed via hematoxylin and eosin staining. Renal function of mice was assessed by measuring the levels of serum creatinine (SCr) and blood urea nitrogen (BUN). The concentrations of pro-inflammatory cytokines in HK-2 cells and serum samples of mice were detected using corresponding ELISA kits. Protein levels of factors associated with nuclear factor kappa-B (NF-κB) pathway were measured in HK-2 cells and renal tissues by Western blotting. AO exerted no cytotoxic effect on HK-2 cells and AO dose-dependently rescued LPS-induced decrease in HK-2 cell viability. The concentrations of pro-inflammatory cytokines were increased in response to LPS or CLP treatment, and the alterations were reversed by AO treatment. For in vivo experiments, AO markedly ameliorated renal injury and reduced high levels of SCr and BUN in mice underwent CLP operation. In addition, AO administration inhibited the activation of NF-κB signaling pathway in vitro and in vivo. In conclusion, AO alleviates septic AKI by suppressing inflammatory responses through inhibiting the NF-κB pathway.

• Korean Journal of Pharmacognosy
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• v.38 no.4
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• pp.400-402
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• 2007

Tacrine is an acetylcholinesterase inhibitor that is approved for the treatment of Alzheimer's disease. However, tacrine treatment for Alzheimer's disease results in reversible hepatotoxicity in 30-50% of patients, which seriously limits its clinical use. Accordingly, the identification of constituents in natural products that have protective effects on tacrine-induced hepatotoxicity would be valuable. In the present study, an immortalized human hepatoma cell line, HepG2 was employed to screen for agents that protect against tacrine-induced hepatotoxicity. The bioassay-guided fractionation of water extract of Cassiae Semen furnished two anthraquinones, aurantio-obtusin (1) and obtusifolin (2). Compounds 1 and 2 showed hepatoprotective effects with the protection ratio values of 55.3 +/- 0.5% and 41.2 +/- 0.8% at $160{\mu}M$, respectively.

• Journal of Applied Biological Chemistry
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• v.63 no.4
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• pp.365-373
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• 2020

We previously reported the potential of Senna tora L. seeds fermented by Lactobacillus casei (FSL) as a laxative agent in a loperamide-induced constipation rat model. Here, we examine the mechanism of action of FSL and its bioactive compound, revealed herein, on loperamide-induced constipation Sprague Dawley rat model. We identified the compound aurantio-obtusin (AO) using HPLC quantitative analysis. Rats were randomly assigned to six experimental groups (eight rats each)-normal and constipated groups (loperamide, FSL [100, 300, 500 mg/kg], and AO [1 mg/kg]). The FSL and AO-treated group showed an increase in the frequency, amount, and water content of feces in the constipated rat. Moreover, FSL and AO increased the intestinal transit speed in the constipated rat. Histological analysis revealed that FSL and AO recovered the intestinal mucus, the number of goblet cells, as well as thickness of the mucosa layer and muscle. Furthermore, the protein levels of the muscarinic acetylcholine receptor M3, which is involved in intestine contraction, were recovered in the FSL and AO-treated group. Its downstream signaling pathway (p-protein kinase C) was recovered by FSL and AO treatment. In conclusion, fermentation of S. tora L. seeds increases AO, which improves intestinal function, indicating that FSL is effective for treating constipation.