• Korean Journal of Pharmacognosy
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• v.37 no.4 s.147
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• pp.294-301
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• 2006

The aim of this study was to investigate the protective activity of gomisin A and gomisin N, bioactive lignan components isolated from Schizandae Fructus, on hepatocyte injury induced by carbon tetrachloride($CCl_4$, 10 mM), t-butyl hydroperoxide(TBH, 0.5 mM), and D-galactosamine(GalN, 30 mM). Primary cultures of rat hepatocyte(18 h culture) were treated with $CCl_4$, TBH or GalN and various concentrations(0.1, 1, 10, $100{\mu}M$) of gomisin A or gomisin N. $CCl_4$ significantly increased the levels of lactate dehydrogenase(LDH), alanine aminotransferase(ALT), and aspartate aminotransferase(AST). These increases were inhibited by gomisin N. TBH significantly increased the level of AST; an increase that was inhibited by gomisin N. GalN markedly increased the levels of LDH and ALT, and these increases was significantly inhibited by both gomisin A and gomisin N. These results suggest that gomisin A and gomisin N have the hepatoprotective activity.

• Journal of Life Science
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• v.20 no.7
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• pp.977-982
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• 2010

We investigated the anti-cancer effects of two dibenzocyclooctadiene lignans, gomisin A and gomisin N, isolated from Schizandra chinensis Baill, in human promyelocytic U937 cells. Gomisin N, but not gomisin A, inhibited cell growth in a concentration-dependent manner, which was associated with the induction of G1 arrest of the cell cycle. G1 arrest induced by gomisin N was correlated with down-regulation of cyclin E, cyclin-dependent kinase (Cdk) 2 and Cdk4, and a concomitant up-regulation of Cdk inhibitors such as p16 (INK4A) and p21 (WAF1/CIP1). Furthermore, gomisin N inhibited phosphorylation of retinoblastoma protein (pRB) and p130, and expression of transcription factor E2Fs. The results indicated that growth inhibition by gomisin N is related to cell cycle arrest at G1 in U937 cells and these findings suggest that gomisin N may be a useful chemotherapeutic agent.

• Korean Journal of Pharmacognosy
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• v.50 no.2
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• pp.148-153
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• 2019

The lignan compound of Schisandra chinensis Baill. (Schizandraceae) has been reported to have a variety of biological activities such as liver protection, neuroprotection, anti-oxidant and anti-diabetes. In this study, we investigated a quantitative analytical method for schisandrin, gomisin A and gomisin $M_2$ isolated from S. chinensis by high-performance liquid chromatography-ultraviolet spectroscopy (HPLC-UV). The isolated compounds were identified by the analysis of 1H- and 13C-NMR spectroscopic data. The results showed that calibration curves of three compounds indicated great linearity with a correlation coefficient ($R^2$) of schisandrin 0.9983, gomisin A 0.9982 and gomisin $M_2$ 0.9986. The limits of detection (LOD) of schisandrin, gomisin A and gomisin $M_2$ were 0.14, 0.07 and $0.05{\mu}g/ml$ and the limits of quantification (LOQ) were 0.42, 0.22 and $0.14{\mu}g/ml$. Intra-day and inter-day precisions of schisandrin were 0.40~1.44%, 0.07~1.02% gomsin A were 0.22~0.52%, 0.10~0.63%, gomisin $M_2$ were 0.40~0.99%, 0.81~2.88%. In result, contents of schisandrin, gomisin A and gomisin $M_2$ in ethanol extract of S. chinensis were $25.95{\pm}0.15$, $2.51{\pm}0.02$ and $2.17{\pm}0.07mg/g$.

• Journal of Life Science
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• v.27 no.2
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• pp.233-240
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• 2017

Previously, we have shown that Schisandra chinensis (Turcz.) Baill. (S. chinensis) has a protective effect against endoplasmic reticulum (ER) stress-induced hepatic steatosis. Gomisin A is a bioactive phytoestrogen derived from S. chinensis. In the present study, the in vitro and in vivo effects of gomisin A on ER stress and hepatic steatosis were investigated. We quantified the expression of markers of ER stress, including glucose regulated protein 78 (GRP78), C/EBP homolog protein (CHOP), and X-box-binding protein-1 (XBP-1), in HepG2 cells treated with tunicamycin or palmitate. Tunicamycin treatment in HepG2 cells induced the expression of markers of ER stress, including GRP78, CHOP, and XBP-1c. However, treatment with gomisin A reduced the expression of markers of ER stress. These inhibitory effects were also observed in palmitate-incubated HepG2 cells. The in vivo inhibitory effects of gomisin A were assessed in mice injected with tunicamycin or fed with a high fat diet (HFD). Gomisin A reduced the expression of markers of ER stress and decreased triglyceride levels in the livers of mice after tunicamycin injection or HFD feeding. Furthermore, gomisin A decreased the expression of inflammatory genes in palmitate-incubated HepG2 cells and the liver of HFD-fed obese mice. These results suggest that gomisin A inhibits ER stress and ameliorates hepatic steatosis induced by ER stress.

• Korean Journal of Pharmacognosy
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• v.33 no.4 s.131
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• pp.272-276
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• 2002

This study was carried out to establish the quantitative analysis of lignans for the quality evaluation of fruit from Schizandra chinensis. Five lignans, gomisin N, schizandrin, gomisin C, schisantherin C, and gomisin A were isolated from the fruits of S. chinensis and identified by the spectroscopic methods. Quantitative determination of three lignans, schizandrin, gomisin A, gomisin N, was conducted using HPLC. Average contents of three lignans in collected lines were 0.70% of schizandrin, 0.20% of gomisin A, 0.57% of gomisin N, and 1.47% of total lignans.

• Journal of Food Hygiene and Safety
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• v.30 no.1
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• pp.59-64
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• 2015

This study compared the content change of physiological active substances according to the extraction condition when we generally drink the extractive of Schisandra fruit with using water. Physiological active substances of the Schisandra fruit, schizandrin, gomisin A and gomisin N were analysed with HPLC. The results of extracting 1 dose of the Schisandra fruit tea, which is some as 1 g of Schisandra fruit, in 100 mL of water by differing the extraction type, extraction temperature and extraction time were of the followings. The total content of schizandrin, gomisin A and gomisin N of powder type in $26^{\circ}C$ leaching was the highest (p < 0.05) as the leaching content of 24 hours (5.54 mg/g) showed difference with different times and the contents of raw type Schisandra fruit were less than 0.1 mg/g in all of extraction time. The contents of powder type Schisandra fruit in $60^{\circ}C$ heating extraction was over 4.50 mg/g except for the 5 minute (2.94 mg/g), and the contents of raw Schisandra fruit were less than 0.3 mg/g. In case of $100^{\circ}C$ heating extraction, the contents of powder type Schisandra fruit showed over 5.10 mg/g in every time zone, and the raw type Schisandra fruit was less than 1.0 mg/g.

• Biomolecules & Therapeutics
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• v.27 no.2
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• pp.210-215
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• 2019

Colorectal cancer is one of the leading causes of cancer related death due to a poor prognosis. In this study, we investigated the effect of Gomisin G on colon cancer growth and examined the underlying mechanism of action. We found that Gomisin G significantly suppressed the viability and colony formation of LoVo cells. Gomisin G reduced the phosphorylation level of AKT implying that Gomisin G suppressed the PI3K-AKT signaling pathway. Gomisin G also induced apoptosis shown by Annexin V staining and an increased level of cleaved poly-ADP ribose polymerase (PARP) and Caspase-3 proteins. Furthermore, Gomisin G remarkably triggered the accumulation of cells at the sub-G1 phase which represents apoptotic cells. In addition, the level of cyclin D1 and phosphorylated retinoblastoma tumor suppressor protein (Rb) was also reduced by the treatment with Gomisin G thus curtailing cell cycle progression. These findings show the suppressive effect of Gomisin G by inhibiting proliferation and inducing apoptosis in LoVo cells. Taken together, these results suggest Gomisin G could be developed as a potential therapeutic compound against colon cancer.

• Journal of Life Science
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• v.22 no.9
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• pp.1224-1230
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• 2012

Cancer chemotherapy drugs command a large share of the market, and the development of new therapeutics with high efficacy and specificity is an active area of study. Recently, the development of cancer therapeutics from natural products targeting angiogenesis has drawn attention due to conventional chemotherapeutics showing serious side effects and resistance in cancer cells. In this study, we investigated the pharmacological efficacy of Gomisin A, an active ingredient of Schizandra chinensis baillon, on tumor growth and metastasis. Administration of Gomisin A at 10 and 100 ${\mu}g/ml$ reduced tumor growth in vivo by $80.5{\pm}8.1%$ and $96.2{\pm}2%$, respectively, compared with positive tumor controls. Treatment of Gomisin A in normal and various tumor cell lines did not exert significant toxicity. Mice treated with Gomisin A at a concentration of 10 and 100 ${\mu}g$/head showed a significant reduction in tumor-induced angiogenesis of $151{\pm}16.9%$ and $98.5{\pm}29.5%$, respectively. Furthermore, tumor metastasis analysis revealed that the administration of Gomisin A at a concentration of 10 and 100 ${\mu}g$/head inhibited tumor metastasis by $13.5{\pm}8.56%$ and $58.3{\pm}9.12%$, respectively. In addition, Gomisin A significantly decreased cell adhesion of the B16BL6 cells to the extracellular matrix. These results demonstrate that Gomisin A inhibits tumor growth via suppression of angiogenesis and tumor metastasis inhibition, without cellular toxicity. The pharmacological efficacy of Gomisin A suggests that it may be a potential candidate for the development of cancer drugs.

• Biomolecules & Therapeutics
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• v.26 no.3
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• pp.322-327
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• 2018

A type of breast cancer with a defect in three molecular markers such as the estrogen receptor, progesterone receptor, and human epidermal growth factor receptor is called triple-negative breast cancer (TNBC). Many patients with TNBC have a lower survival rate than patients with other types due to a poor prognosis. In this study, we confirmed the anti-cancer effect of a natural compound, Gomisin G, in TNBC cancer cells. Treatment with Gomisin G suppressed the viability of two TNBC cell lines, MDA-MB-231 and MDA-MB-468 but not non-TNBC cell lines such as MCF-7, T47D, and ZR75-1. To investigate the molecular mechanism of this activity, we examined the signal transduction pathways after treatment with Gomisin G in MDA-MB-231 cells. Gomisin G did not induce apoptosis but drastically inhibited AKT phosphorylation and reduced the amount of retinoblastoma tumor suppressor protein (Rb) and phosphorylated Rb. Gomisin G induced in a proteasome-dependent manner a decrease in Cyclin D1. Consequently, Gomisin G causes cell cycle arrest in the G1 phase. In contrast, there was no significant change in T47D cells except for a mild decrease in AKT phosphorylation. These results show that Gomisin G has an anti-cancer activity by suppressing proliferation rather than inducing apoptosis in TNBC cells. Our study suggests that Gomisin G could be used as a therapeutic agent in the treatment of TNBC patients.

• Korean Journal of Medicinal Crop Science
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• v.12 no.6
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• pp.478-482
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• 2004

Suspension culture of Schisandra chinensis for production of gomisin J was perfomed in bioreactor. The inoculum size and initial sucrose concentration had significant effect on the cell growth and gomisin J accumulation. The maximum dry cell weight $(DCW;\;43.5\;g/{\ell})$ and gomisin J content $(0.71\;{\times}\;10^{-3}\;{\mu}g/g\;DCW)$ were obtained at inoculum size of 100 g fresh cell weight (FCW) per liter and MB5 medium containing 6% sucrose after 8 weeks of culture. The effect of oxygen supply on the cell growth and gomisin J accumulation was also investigated in an airlift-type bioreactor. The optimal cell growth and gomisin J content was obtained under 0.5 vvm. The productivity of gomisin J was 0.7 fold in bioreactor culture lower than that obtained in a flask cultivation.