• YAKHAK HOEJI
• /
• v.51 no.2
• /
• pp.145-149
• /
• 2007

Saussurea Radix, the dried roots of Saussurea lappa Clark (Compositae), has been used in oriental traditional medicine for aromatic stomachic. Present study was carried out for the anticancer effect of Saussurea Radix. Bioassay-directed fractionation of Saussurea Radix led to the isolation of two sesquiterpenes, dehydrocostuslactone (1) and costunolide (2). The structures of 1 and 2 were elucidated by spectral methods (MS, IR, $^1$H and $^{13}$C NMR). These compounds showed a potent cell proliferation activity against human breast cancer cell MCF-7 and MDA-MB-453.

• THE JOURNAL OF KOREAN ORIENTAL ONCOLOGY
• /
• v.7 no.1
• /
• pp.1-18
• /
• 2001

Objective: This experimental study was carried out to evaluate the effects of Saussurea Radix and Plantaginis Herba on cellular viability, proliferation, apoptosis and expression of the cell cycle-related genes in cultured gastric cancer cells. Method :MTT assay for analysis of cellular toxicity and the effect on suppression of cellular viability, $[^{3}H]$ thymidine incorporation assay for evaluation of the effect on suppression of DNA replication, tryphan blue exclusion assay for measurement of induction of apoptosis and Quantitative RT-PCR for analysis of the effects on expression of cell cycle or apoptosis-related genes were performed. Results: Antitumor activity of Saussurea Radix associated with inhibition of cell cycle progression and promotion of apoptosis caused by transcriptional regulation of p53, p21/Wafl and the other related genes was observed.

• Korean Journal of Pharmacognosy
• /
• v.36 no.2 s.141
• /
• pp.97-101
• /
• 2005

Saussureae Radix, the dried root of Saussurea lappa Clarke, has traditionally used for alleviating pain in abdominal distention and tenesmus, indigestion with anorexia, dysentery, nausea, and vomiting. Here we observed that methanol extracts of Saussurea Radix inhibited CDK2 activities in vitro. This inhibitory compound was isolated and identified as dehydrocostuslactone, one of the major constituents of Saussurea Radix. It is well known that dehydrocostuslactone induces apoptotic cell death. In this study, we also showed that dehydrocosruslactone inhibited cellular Rb phosphorylation and blocked cell growth at the concentration below $12\;{\mu}g/ml$ at which apoptotic cell death was not observed. Taken together, these results indicated that dehydrocostuslactone showed its anti-proliferative effects through the inhibition of CDK2 activity as well as the induction of apoptotic cell death.

• Korean Journal of Pharmacognosy
• /
• v.30 no.1
• /
• pp.48-53
• /
• 1999

Isolation and quantitative determination of costunolide from Saussurea lappa Clarke (Compositae) has been conducted by using HPLC method. Costunolide in an acetone extract from the crude drug was separated on a RP-18 column using a $MeOH-H_20$ mixture (65:35) as an eluent and the average content is about $1.32{\sim1.42%.$ The content of costunolide in dried extract was decreased by about 24% in seven days. However it showed a slight decrease in solution. It is highly recommended that quantitative determination of costunolide from Saussureae Radix should be conducted as early as possible after solvent extraction.

• Korean Journal of Oriental Medicine
• /
• v.12 no.3 s.18
• /
• pp.117-130
• /
• 2006

The purpose of this study was to introduce the differential standard of Mok-Hyaeng Radix species. We established the classificatory standard according to the external and internal morphology and the pattern in 4 kinds of Mok-Hyaeng Radix. The results follow: 1. On the external morphology, Radix of Vladimiria souliei had a sticky material in the head of roots and it was yellowish white in the cut surface. It attached to teeth during chewing. Radix of Aucklandia lappa (=Saussurea lappa) was dark grayish brown and was grayish brown in the cut surface. It had special odor and was not attache to teeth chewing it. On the other hand, Radix of Inula helenium was dark brown. In the cut surface, cortical layer was different from wood layer. Radix of Aristolochia contorta was yellowish brown. In the cut surface, it was not smooth and cortical layer was different from wood layer. 2. On the internal morphology, Radix of Vladimiria souliei had many fascicular fibers and scattered large oil chambers in the bast ray, xylem ray, and parenchyma. On Radix of Aucklandia lappa (=Saussurea lappa), it was difficult to find out the trace when the cork layer was exfoliated. The cambium formed circle and the large oil chambers were scattered in the phloem and xylem. On the other hand, external cortical layer of Radix of Inula helenium was detached and cambium was formed to indistinct circle and large oil chambers were scattered in the phloem and xylem. On Radix of Arustolochia contorta, the large oil chambers were scattered in the surface later, bast part was relatively broad and cambium formed circle. 3. On the TLC pattern, Radix of Aristolochia contorta, Inula helenium, Aucklandia lappa, and Vladimiria souliei were chromogenic to violet and purple according to sulfuric acid colour pattern, especially faint on Aristolochia contorta. 4. On the pattern analysis of HPLC, we compared the content and the pattern of constunolide and dehydrocostus lactone, Radix of Aucklandia lappa was similar to Radix of Vladimiria souliei and Radix of Aristolochia contorta was similar to Radix of Inula helenium. On the total HPLC component pattern, constunolide and dehydrocostus lactone were similar in all four types, but it showed the Rf 5-6 peak was only in Radix of Aristolochia contorta, not in Radix of Inula helenium, Aucklandia lappa, and Vladimiria souliei. It is considered the results of this study will be furnished the basis to succeeding studies and it is needed to extensive comparative study for the same genus-degree of relatedness.

• Journal of Society of Preventive Korean Medicine
• /
• v.17 no.2
• /
• pp.169-178
• /
• 2013

Objectives : Many cancers acquired resistance to chemotherapy, thus limiting its anticancer efficacy. It is known that Glutathione (GSH) is related to the development of drug resistance. The expression of GSH synthesizing glutamylcysteine ligase (GCL) was controlled by nuclear factor-E2-related factor(Nrf2). Previous studies showed that pharmacological depletion of GSH results in ROS increase, apoptotic response, and sensitization to oxidizing stimuli. In the current study, we examined Saussurea Lappa (SL) have the inhibitory effect on Nrf2 activity using human lung cancer A549 cells overexpressing Nrf2. Methods : Cell viability of A549 cells on SL treatment was determined by MTT assay. To detect the apeptosis in SL-treated A549 cells, sub-G1 population was measured by flow cytometry analysis (FACS). The level ROS was determined by FACS and fluorescence microscopy. To investigate whether SL have effect the suppression on Nrf2, we performed western blotting analysis. The GSH content was measured since GSH plays an important role in response to oxidative stress and was regulated by Nrf2. Results : A549 cells treated with an SL extract showed a substantial decrease in cell viability, along with a concomitant increase in apoptosis compared to untreated cells. Treatment of the SL extract led to increased Reactive oxygen species (ROS) production and a suppression of Nrf2. In addition, the antioxidant NAC attenuated SL-induced ROS generation, Nrf2 inhibition, and apoptosis. Taken together, these data show that the SL extract induced the production of ROS, and the inhibition of Nrf2, consequently resulting in A549 cell death. Conclusions : These results suggest that SL might be an effective agent to enhance anticancer drug sensitivity via Nrf2 inhibition.

• The Journal of Internal Korean Medicine
• /
• v.16 no.1
• /
• pp.40-61
• /
• 1995

This study was performed to investigate concept, systoms, causes of disease, pathogenic mechanisms, therapies and precriptions about senile constipation through the successive medical literature, recent chinese medical literature and chinese medical joumals. Senile constipation seems to be applicable to dryness syndrom and constipation of insufficiency type, have something to do with kidney(the most), lung, spleen and large intestine. The most principal cause of disease is yin-fluid, the rest deficiency of qi, insufficiency of yang, stagnation of qi and retention of fever etc. There are enriching the blood and moistening dryness in principal therapy, the rest are invigorating qi and loosing the bowel, warming and invigorating the spleen and kidney, regulating the flow of qi and promoting the stagnancy of qi and expelling the pathogenic heat etc. In prescriptions there are Yunjangtang, Jengaektang, Hwanggitang, Jechunjeon, Yukmatang and Majainhwan as the causes of disease, meanwhile are Yungjang-tang, Jechunjeon and Majainhwan in the vulgaris prescriptions. And in medical herbs there are nourishing yin medicines as Rhizoma rehmanniac, Radix ophiopogonis and Radix scrophulariae etc., invigorating qi medicines as Radix astragali, Radix codonopsitis and Radix polygoni multiflori etc, invigorating yang medicines as Caulis cistanchis and Semen psoraleae etc., promoting qi circulating medicines as Radix saussurea, Lignum aquilariae and Radix linderae etc., and reducing fever and therapeutic method to keep the adverse qi flowing downward medicines as Semen cannabis, Rhizoma rhei, Fructus immaturus ponciri, and Cortex magnoliae etc.. Meantime Rhizoma rehmanniae, Radix ophiopogonis, Caulis cistanchis, Radix angelicae gigantis, Semen cannabis, Semen biotae, Semen pruni japonicae and Semen persicae in principal herb-medicines. In clinical reports the process of disease was between 10 to 20 years, the evacuation cycle between 4 to 7 days, generally possessed chronic diseases as hypertension, diabetes, arteriosclerosis and cerebro- vascular disorders etc. and the efficiency rate was more than 90%. The senile constipation is occured in succession or promoted by chronic diseases as obesity, hypertension, diabetes, arteriosclerosis. hrperlipemia, cerebro- vascular disorders etc., so diet-regulating, adequate exercise, proper evacuation-habit and psychologic rest etc. are important more than medicine-treatments.

• Herbal Formula Science
• /
• v.16 no.2
• /
• pp.193-204
• /
• 2008

Dehydrocostus lactone (DHL) and Mokko lactone (ML) were isolated from Saussureae Radix, and their effects on heme oxygenase-1 (HO-1) expression and hepatoprotection in the liver cell line HepG2 were investigated. DHL induced HO-1 expression and HO activity in a dose-dependent manner, whereas ML lacking one double bond property at 11 and 13 carbons on its own chemical structure had no apparent effects. DHL also induced Nrf2 nuclear translocation and enhanced antioxidant response element (ARE) activation which mediated HO-1 gene transcription. Pretreatment with DHL protected HepG2 cells against oxidative damages caused by H2O2. Interestingly, the hepatoprotective effects of DHL appeared to be associated with HO enzymatic activation, HO-1 expression and Nrf2 activation, because blockage of HO activity by a HO inhibitor and inhibition of HO-1 and Nrf2 cellular synthesis by small interfering RNA abolished heptoprotection afforded by DHL. Taken together, this investigation provides evidence supporting that Saussureae Radix is hepatoprotective against oxidative stress that causes abnormal liver damages.

• The Korea Journal of Herbology
• /
• v.26 no.2
• /
• pp.31-37
• /
• 2011

Objectives : This study was focused to investigate the toxicity of Saussurea lappa (SL) extracts in HL-60 cells and human lymphocytes. We also examined the differentiation effect of SL against leukemia cells. Methods : For examining the toxicity of SL, cytokinesis-block micronucleus (CBMN) assay and single cell gel eletrophoresis (SCGE) assay were used in present study. The cell differentiation effect of SL was evaluated by nitroblue tetrazolium (NBT) reduction assay. Results : The inhibition of cell growth in HL-60 cells was observed in a dose-dependant manner after SL treatment for 24 h. According to SCGE assay, HL-60 cells treated with SL increased DNA damage at $10{\mu}g/m{\ell}$, while DNA damage was induced by 0.1, 1, $10{\mu}g/m{\ell}$ concentration of SL in human lymphocytes. Our results indicated that SL have no genotoxic effect in HL-60 cells and human lymphocytes. Additionally, the differentiation effect was induced in $1{\mu}g/m{\ell}$ SL-treated HL-60 cells. Conclusions : From above results it is suggested that SL could be beneficial for the preparation of the useful agent for treating leukemia.

• Biomolecules & Therapeutics
• /
• v.7 no.1
• /
• pp.29-34
• /
• 1999

The cellular growth inhibition of 20 natural products was screened using SRB (sulforhodamine B) assay against 4 human cancer cell lines(SNU-1, SNU-C$_{4}$, Hep3B, Kato III). Ethanol extracts of Salvia miltiorrhiza, Saussurea lappa and Chelidonium majus showed potent anticancer activity among them, and further, it was fractionated into methylene chloride, hexane and methanol. Methylene chloride and methanol fraction of Salvia radix showed significant inhibitory activity against 4 human cancer cell lines. The effect of Salvia miltiorrhiza on anticancer activity in vitro models was evaluated with methylene chloride fraction of Salvia miltiorrhiza. Life span of ICR mice implanted with sarcoma-180 was increased by 40-61% and BDF$^{1}$ mice implanted with L1210 was increased by 66-89% upon intraperitoneal administration with methylene chloride fraction of Salvia miltiorrhiza. Based on these result, we suggested that Salvia miltiorrhiza showed anticancer activity on the in vivo and in vitro models