• Title/Summary/Keyword: pharmaceutical effects

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Nelumbinis Semen Reverses a Decrease in $5-HT_{1A}$Receptor Binding Induced by Chronic Mild Stress, a Depression-like Symptom

  • Jang, Choon-Gon;Kang, Moon-Kyu;Cho, Jae-Han;Lee, Sun-Bok;Kim, Hyun-Taek;Park, Soon-Kwon;Lee, Jin-Woo;Park, Seong-Kyu;Hong, Moo-Chang;Shin, Min-Kyu;Shim, In-Sup;Bae , Hyun-Su
    • Archives of Pharmacal Research
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    • v.27 no.10
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    • pp.1065-1072
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    • 2004
  • Depression is associated with a dysfunctional serotonin (5-hydroxytryptamine; 5-HT) system. More recently, several lines of evidence suggest that an important factor in the development of depression may be a deficit in the function and expression of $5-HT_{1A}$ receptors. The present study assessed if Nelumbinis Semen (N. s.) had an anti-depression effect through reversing a decrease in $5-HT_{1A}$receptor binding in rats with depression-like symptoms induced by chronic mild stress. Using a $5-HT_{1A}$ receptor binding assay, with a specific $5-HT_{1A}$receptor agonist, 8- OH-DPAT (8-hydroxy-2-(di-n-propylamino) tetralin), the mechanism of the anti-depression effect of N. s. on rats was investigated, and the effects compared with two well-known antidepressants, Hyperium Perforatum (St. Johns Wort) and fluoxetine (Prozac). Animals were divided into five groups: the normal (N) group without chronic mild stress (CMS), the control (C) group under CMS for 8 weeks, the Nelumbinis Semen (N. s.) treatment group under CMS for 8 weeks, the Hyperium Perforatum (H. p.) treatment group under CMS for 8 weeks and finally, the fluoxetine (F) treatment group under CMS for 8 weeks. Each treatment was administered to rats during the last 4 weeks of the 8-week CMS. A sucrose intake test was performed to test the anti-depression effect of N. s. The N. s. treatment significantly reversed the decreased sucrose intake under CMS (P<0.05 compared to control group under CMS). In the CA2 and CA3 regions of the hippocampus, both N. s. and H. p. reversed the CMS-induced decrease in $5-HT_{1A}$receptor binding. In the I to II regions of the frontal cortex, N. s. and H. p. also reversed the CMS-induced decrease in$5-HT_{1A}$receptor binding, and even showed a significant increase in $5-HT_{1A}$receptor binding compared to the F treatment group (N. s. vs. P, p<0.05, H. p. vs. P, p<0.05). However, in the hypothalamus, all treatments reversed the CMSinduced decrease in $5-HT_{1A}$receptor binding. This reversal effect of N. s. on the decrease in $5-HT_{1A}$receptor binding in the frontal cortex, hippocampus and hypothalamus of rat brains was very similar to that of H. p, but different from that of F. It is concluded that N. s. presents an anti-depression effect through enhancing $5-HT_{1A}$receptor binding.

Antioxidative Activity of Rumex crispus L. Extract (소리쟁이 추출물의 항산화 효능)

  • Rhim, Tae-Jin;Choi, Moo-Young;Park, Hee-Juhn
    • Korean Journal of Plant Resources
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    • v.25 no.5
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    • pp.568-577
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    • 2012
  • The objective of this study was to investigate the antioxidative capacity of ethanol extracts from Rumex crispus L. The concentration of R. crispus L. extract at which DPPH radical scavenging activity was inhibited by 50% was 2.15 mg/mL, which was lower than that of ${\alpha}$-tocopherol (0.43 mg/mL), as compared to 100% by pyrogallol as a reference. Total antioxidant status was examined by total antioxidant capacity against ABTS radical reactions. Total antioxidant capacities of R. crispus L. extract at concentrations of 0.1 and 1 mg/mL were 0.47 and 2.33 mM Trolox equivalents, respectively, which were higher than those of ${\alpha}$-tocopherol. Superoxide scavenging activities of R. crispus L. extract at concentrations of 0.1 and 1 mg/mL were 21.5 and 78.9%, respectively, which were not significantly (p>0.05) different from those of catechin. Oxygen radical absorbance capacities of R. crispus L. extract at concentrations of 20 and 100 ${\mu}g/mL$ were 62.5 and 156.4 ${\mu}M$ Trolox equivalents, respectively, which were lower than those of ascorbic acid. Cupric reducing antioxidant capacities of R. crispus L. extract at concentrations of 0.1 and 1 mg/mL were 0.28 and 1.88 mM Trolox equivalents, which were similar or significantly (p<0.05) higher than those of ${\alpha}$-tocopherol, respectively. R. crispus L. extract prevented supercoiled DNA strand breakage induced by hydroxyl radical and peroxyl radical. Total phenolic contents of R. crispus L. extract at concentrations of 0.5 and 5 mg/mL were 0.58 and 3.85 mM gallic acid equivalents, respectively. R. crispus L. extract at concentration of 0.1 and 0.5 mg/mL inhibited 0.2 mM tert-butyl hydroperoxide-induced cytotoxicity by 38.5 and 63.5%, respectively, in HepG2 cell culture system. Thus, strong antioxidant and cytotoxicity-inhibiting effects of R. crispus L. extract seem to be due to, at least in part, the prevention from free radicals-induced oxidation as well as high levels in total phenolic contents.

Antioxidative Activities and Whitening Effects of Solvent Fraction from Prunus davidiana (Carriere) Franch. Fruit (산복사나무(Prunus davidiana (Carriere) Franch.) 열매 분획 추출물의 항산화 및 미백 효능)

  • Kim, Won Baek;Park, So Hae;Hwang, Hye Sun;Woo, Jung Yoon;Lee, Hye Ryun;Hwang, Dae Youn;Choi, Ji Hye;Lee, Heeseob
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.10
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    • pp.1363-1370
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    • 2012
  • In this study, methanol extract and its organic solvent fractions were prepared from Prunus davidiana (Carriere) Franch. fruit. Antioxidative activities, polyphenolic and flavonoid contents, and tyrosinase inhibitory activities were evaluated. Among the fractions, ethyl acetate fraction showed the highest antioxidative activity with $IC_{50}$ values of 5.8 ${\mu}g/mL$ and 88.1 ${\mu}g/mL$ for DPPH radical and nitrite scavenging, respectively, which were comparable to those of ascorbic acid. Further, total flavonoid and polyphenolic contents were highest in the ethyl acetate fraction with $IC_{50}$ values of 244.5 mg/g and 210.2 mg/g, respectively. $IC_{50}$ values for tyrosinase inhibitory activity were 0.310 mg/mL and 0.329 mg/mL for the ethyl acetate and n-butanol fractions, respectively. Based on these results, it is suggested that the ethyl acetate fraction of Prunus davidiana (Carriere) Franch. fruit could be used as a functional material in the food and pharmaceutical industries.

Effects of Makgeolli and Makgeolli precipitate on Hepatotoxicity and Serum Lipid Content in Rats (막걸리와 막걸리 침전물이 간 독성 및 혈청 지질함량에 미치는 영향)

  • Kim, Bo Kyung;Kang, Min Sook;Jeon, Myeong-Jeong;Lee, Sang-Hyeon;Kim, Mihyang
    • Journal of Life Science
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    • v.23 no.2
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    • pp.282-289
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    • 2013
  • This study was conducted to investigate the effect of Makgeolli and Makgeolli precipitate on hepatotoxity and the serum lipid content in rats. First, we investigated the effect of Makgeolli and ethanol on the progress of alcoholic fatty liver. The effect of Makgeolli precipitate on carbon tetrachloride ($CCl_4$)-induced hepatotoxicity in the rats was then studied. Indicators of the health status of the experimental period, the body weight gain in ethanol-treated group tended to be lower than those in the control and the Makgeolli-treated groups. The weight of the liver tissue decreased significantly following the administration of ethanol. However, this was not seen following the administration of Makgeolli. The activities of serum aspartate transaminase (AST) and alanine transaminase (ALT) were decreased in the Makgeolli group compared to the ethanol group. Serum cholesterol concentrations increased in the ethanol group, but decreased in the Makgeolli-treated group to an equal volume of the ethanol-treated group. The serum HDL-cholesterol content was significantly higher in the Makgeolli group than in the ethanol group. Analysis of the impact of the Makgeolli precipitate on toxicity induced by $CCl_4$ in the liver showed that the $CCl_4$ treatment significantly increased the activities of serum ALT and AST. However, the levels of cholesterol and triglyceride in serum were decreased. The $CCl_4$ treatment increased the activities of AST and ALT. However, the raw Makgeolli precipitate decreased their activities. Moreover, raw Makgeolli precipitate significantly reduced the $CCl_4$-induced elevation of serum lipids more than heated Makgeolli precipitate. These results suggest that raw Makgeolli precipitate may exert a protective effect against $CCl_4$-induced liver injury by preventing lipid peroxidation.

Variation in bioactive principles and bioactive compounds of Rosa rugosa fruit during ripening (해당화 열매 성숙단계에 따른 생리활성 및 기능성 물질 변화 분석)

  • Kwak, Minjeong;Eom, Seung Hee;Gil, Jinsu;Kim, Ju-Sung;Hyun, Tae Kyung
    • Journal of Plant Biotechnology
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    • v.46 no.3
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    • pp.236-245
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    • 2019
  • Fruit ripening is a genetically programmed process involving a number of biochemical and physiological processes assisted by variations in gene expression and enzyme activities. This process generally affects the phytochemical profile and the bioactive principles in fruits and vegetables. To appraise the variation in bioactive principles of fruits from Rosa rugosa during its ripening process, we analyzed the changes in antioxidant and anti-elastase activities and polyphenolic compounds during the four ripening stages of fruits. Overall, an extract of unripe fruits contained the highest levels of total phenolic and flavonoid contents, radical scavenging activity, reducing power, oxygen radical antioxidant capacity, and elastase inhibitory activity, compared with the extracts of fruits at other stages of ripening. Additionally, we found that the reduction of flavonoid content occurs because of decreased transcriptional levels of genes involved in flavonoid biosynthesis pathway during the ripening process. Based on HPLC analysis, we found that the extract of unripe fruits contained the highest amount of myricetin, caffeic acid, chlorogenic acid, syringic acid, and p-coumaric acid and suggested that the antioxidant and anti-elastase activities of the extract obtained from stage 1, should be mediated by the presence of these compounds. Additionally, we analyzed the interaction sites and patterns between these compounds and elastase using the structure-based molecular docking approach, and suggested that chlorogenic acid strongly interacted with elastase. Together, these findings suggest that the maturity of fruits has profound effects on the pharmaceutical value of R. rugosa.

Enhancement of Anti-inflammatory Activity of Lactobacillus plantarum Fermented by Achyranthes japonica on Extraction Solvents (추출 용매에 따른 Lactobacillus plantarum 발효 우슬의 항염증 효과 증진)

  • Jo, Eun Sol;Woo, Young Min;Kim, Ok Ju;Jo, Min Young;Ahn, Mee Young;Lee, Jae-Hwa;Ha, Jong-Myung;Kim, Andre
    • Applied Chemistry for Engineering
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    • v.30 no.2
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    • pp.145-150
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    • 2019
  • In this study, we used extracts obtained from five different solvents (water, ethanol, hexane, ethyl acetate, butanol) of Achyranthes japonica (AJ) and also AJ fermented with Lactobacillus plantarum (LP) to confirm effects on the anti-inflammatory activity in RAW264.7 cells. Experiments of measuring nitric oxide (NO) and cytokine production were performed in lipopolysaccharide (LPS)-induced RAW264.7 cells, and the expression of both cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) was observed by a western blot method. The cytotoxicity of RAW264.7 was confirmed by the cell counting kit (CCK) assay at a concentration of $100{\mu}g/mL$, which has no toxicity. As a result of the inhibition of NO production, the inhibition rate of AJ-LP extracted with ethanol samples was about 74% higher than that of using the control group. Interleukin-6 (IL-6), tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), and Interleukin-$1{\beta}$ (IL-$1{\beta}$), which are inflammatory cytokines, also showed an excellent efficacy with inhibition rates of about 57, 70, and 74%, respectively. Comparing to the results of COX-2 and iNOS expression in the AJ group, the inhibition rate of 20-hydroxyecdysone was the highest than others. On the other hand, the COX-2 expression level of AJ-LP group decreased about 16% compared to that of the control group, and the iNOS expression level was also decreased about 7%. These results suggest that the extract of AJ fermented from L. plantarum can be used as an anti-inflammatory natural material.

Continuous Control of Acetaminophen Poisoning after Implementation of Regulation for Ease Access of Acetaminophen: Cohort Study from Emergency Department Based in-depth Injury Surveillance (아세트아미노펜 사용 편의성 증가 후 중독발생 위험의 지속적 관리 필요성)

  • Jo, Seung Jik;Gang, Hyun Young;Lee, Si Jin;Bae, Gyu Hyun;Lee, Eui Jung;Han, Kap Su;Kim, Su Jin;Lee, Sung Woo
    • Journal of The Korean Society of Clinical Toxicology
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    • v.18 no.2
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    • pp.57-65
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    • 2020
  • Purpose: Since 2012, acetaminophen can be accessed easily not only at pharmacies but also at convenience stores. The relationship between the easy access of acetaminophen and the risk of poisoning has been controversial. Several studies also reported different results regarding the risk of acetaminophen poisoning after access to acetaminophen was relaxed. This study examined the long-term effects on the risk of acetaminophen poisoning after easy access to acetaminophen was implemented. Methods: This was a retrospective analysis of an emergency department (ED)-based in-depth Injury Surveillance Cohort by the Korea Center for Disease Control and prevention from 2011 to 2018. Poisoning cases were selected from the Cohort, and the incidence of acetaminophen poisoning and the characteristics of the cases of acetaminophen poisoning were analyzed. The purchase path and the amount of ingestion in acetaminophen poisoning were sub-analyzed from data of six EDs. Results: Of 57,326 poisoning cases, 4.0% (2,272 cases) were acetaminophen poisoning. Of 2,272 cases of acetaminophen poisoning, 42.8% (974 cases) required in-patient care after ED management. Two hundred and sixty-four of these 964 cases required intensive care. The rates of cases that required in-patient treatment and the rates of cases that required intensive care increased from 29.4% in 2011 to 48.1% in 2018, and from 3.1% in 2011 to 15.2% in 2018, respectively (p<0.001, p<0.001). In the poisoning group with in-depth toxic surveillance (n=15,908), the incidence and proportion of acetaminophen (AAP) poisoning increased from 55 cases per year to 187 cases per year and 4.9% to 6.1%, respectively (p=0.009, p<0.001, respectively). The most common age group of acetaminophen poisoning was teenagers, which is different from the most common age group of other pharmaceutical agents: the middle age group of 40-49 years (p<0.001). Of 15,908 in-depth toxic surveillance patients, 693 patients had AAP poisoning, of whom 377 cases (54.2%) purchased acetaminophen from a non-pharmacy. The proportions of the purchase path from non-pharmacy were 41.4% at 2011-12 and 56.4% (2013-18) (p=0.004). The amount of acetaminophen ingestion was 13.5±14.3 g at 2011-12 and 13.9±15.1 g at 2013-18 (p=0.794). Conclusion: Although the incidence of acetaminophen poisoning did not increase remarkably in the short term after the implementation of the new regulation, the incidence of acetaminophen poisoning has increased slightly during the study period of 2017-18. In addition, the proportion of the purchase path from non-pharmacies has increased since the emergence of new regulations for the easy access of acetaminophen in 2012. The incidence of acetaminophen poisoning might have been affected after the increasing accessibility of acetaminophen in convenience stores. Continuous control of acetaminophen poisoning is required. Furthermore, the prevention of acetaminophen poisoning should be focused on teenagers with specialized school education programs.

Effects of Supplementation of Spent Mushroom(Flammulina velutipes) Substrates on the in vitro Ruminal Fermentation Characteristics and Dry Matter Digestibility of Rye Silage (호밀 사일리지 제조 시 팽이버섯 수확 후 배지 첨가수준이 in vitro 반추위 발효특성 및 건물소화율에 미치는 영향)

  • Kang, Han-Byeol;Cho, Woong-Ki;Cho, Soo-Jeong;Lee, Shin-Ja;Lee, Sung-Sill;Moon, Yea-Hwang
    • Journal of agriculture & life science
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    • v.51 no.5
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    • pp.91-101
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    • 2017
  • The in vitro experiment was conducted to ensure the supplemental level of spent Flammulina velutipes mushroom substrates(SMS) as an energy source in manufacturing of rye silage. Rye harvested at heading stage was ensiled with spent mushroom substrates of 0%(Control), 20%(R-20), 40%(R-40) and 60%(R-60) as fresh matter basis for 6week. The rumen fluid for preparation of in vitro solution was collected from two cannulated Holstein bulls fed a 40:60 concentrate:timothy diet. The experiment was conducted by 3, 6, 9, 12, 24, and 48 hrs of ncubation time with 3 replications. The silages were evaluated fermentation characteristics and dry matter digestibility(DMD) in vitro. The pH of in vitro solution was inclined to decrease with elapsing the incubation time, and that of the R-60 was significantly(p<0.05) lower than the other treatment at 48 hr of incubation. The microbial growth in vitro was inclined to increase with elapsing the incubation time, and that of the R-20 was significantly(p<0.05) greater than the Control at 48 hr of incubation. Gas production was greater(p<0.05) in the Control than the other treatments at 48 hr of incubation. In vitro dry matter digestibility(IVDMD) was higher with increasing the supplemental level of SMS, and was significantly(p<0.05) lower in the Control compared with other treatments throughout whole incubation time. The IVDMD for R-60 was the highest(p<0.05) among treatments at 24 hr and 48 hr of incubation. Considering of above results and the availability of SMS, SMS could be supplemented by 60% in fresh matter basis for rye silage fermentation.

Critical Essay on the Notice of the Price Adjustment of Generic Drugs (제네릭 의약품 약가 조정 고시에 대한 비판적 고찰)

  • Park, Jeong Yeon
    • The Korean Society of Law and Medicine
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    • v.22 no.1
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    • pp.91-124
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    • 2021
  • In May 2019, the Ministry of Food and Drug Safety revised the "Pharmaceutical Determination and Adjustment Criteria" with the content of differentially calculating the price of generic drugs according to the registration of the drug substance and meeting the requirements for their own bioequivalence test. According to this revised rule, if their own bioequivalence test is not conducted, even the generic drugs that have already been approved would be lowered in price. I wondered whether this system was introduced with sufficient public legal considerations regarding its legislative purposes and means. Therefore, I reviewed the contents of the revised notice based on whether or not it is valid to determine and adjust the price of generic drugs in terms of the legitimacy of legislative purposes and the proportionality principle after introducing the history and background of the rule. First, I raised a question as to whether the purpose of preventing the overrun of generic drugs is indeed legitimate in terms of the legitimacy of the purpose. In order for the revised notice of "reduction of drug prices when the test requirements are not met," to meet the conformity principle, the premise that it is difficult to recognize safety and effectiveness through consignment (joint) bioequivalence test or that these tests are insufficient in safety and efficacy verification than their own test must be established. Nevertheless, it seems that suffficient review has not been carried out. In order to achieve the purpose of securing safety and effectiveness, the focus should be on 'reinforcement of the standards for bioequivalence test and the management of the bioequivalence test itself' rather than whether it is a their own test or a consignment (joint) test. Third, it is contrary to the necessity and substantiality principle that strict standards are uniformly applied to the products that can be considered to have been sufficiently verified for safety and effectiveness after a considerable period of time has passed after the product approval. In many cases, revised administrative legislations quickly enacted and amended in the state of lack of legal review or consensus, while the regulatory effects resulting from it are quite direct and specific to the regulated person. In this respect, I emphasized that the administrative legislative process also requires substantial review and prior control of the regulatory purposes and means, and that the participation of stakeholders in the legislative procedure is to be strengthened.

Anti-tumor Effect of a Combination of Hongyoung Ethanol Extract and Cisplatinin YD-10B Oral Cancer Cells (YD-10B 구강암세포에서 홍영 에탄올 추출물과 시스플라틴 병용에 의한 항암 효과)

  • Eun-Jung Kim;Sung-Hee Hwang;Sangwook Park
    • Journal of Life Science
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    • v.33 no.6
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    • pp.498-505
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    • 2023
  • Solanum tuberosum Linnaeus cv Hongyoung, which represents red potato, was developed in Korea. Hongyoung is known to have anti-oxidant, anti-inflammatory, anti-viral, and anti-tumor properties, but no research has been conducted on the growth inhibition and apoptosis effects of hongyoung in YD-10B oral cancer cells. In this study, the combined treatment of hongyoung ethanol extract (HEE) and cisplatin were examined to determine its ability to inhibit cancer cell growth, induce apoptosis, and inhibit matrix metalloproteinases (MMP)-2 and MMP-9 cancer metastasis. The cell viability was investigated using a 2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H- tetrazolium monosodium salt (MTS) assay, and the ability to induce apoptosis was analyzed using an FACS analyzer. The mRNA expression and protein activity of MMP-2 and MMP-9 were measured via RT-PCR and zymography. The YD-10B oral cancer cells showed an increase in growth inhibition as the concentration of HEE increased. The combination of 200 µM cisplatin and 500 ㎍/ml HEE reduced the growth of the YD-10B oral cancer cells by more than 50% compared to cisplatin alone. When phorbol 12-myristate 13-acetate (PMA)-treated YD-10B oral cancer cells were co-treated with 200 µM cisplatin and 500 ㎍/ml HEE, both the mRNA expression and protein activity of the MMP-2 and MMP-9 decreased. In addition, the percentage of the sub-G1 phase, which indicates apoptosis ability, more than doubled when treated in combination with 200 µM cisplatin and 500 ㎍/ml HEE than when cisplatin alone was used. The results of this study therefore suggest the possibility of using a combination of HEE and cisplatin in the development of effective drugs to treat oral cancer.