• Title/Summary/Keyword: aPPT

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Effect of Salinity Change on Physiological Response and Growth of yearling Sea Bass, Lateolabrax japonicus (염분 변화에 따른 농어, Lateolabrax japonicus 유어의 생리 반응과 성장 차이)

  • 한형균;강덕영;전창영;장영진
    • Journal of Aquaculture
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    • v.16 no.1
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    • pp.31-36
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    • 2003
  • Two experiments were conducted for the physiological and growth responses of yearling sea bass, Lateolabrax japonicus (total length 24.4$\pm$1.5 cm, body weight 125.4$\pm$25.4 g) by the manipulation of salinity. To study the physiological responses of the sea bass by acute salinity change, we changed water salinity from 30 ppt into 2 ppt in rearing tank through 1 hour or 6 hour. To access the effect of salinity in the growth of sea bass, we also examined the growth of the sea bass in 2, 10, 20 and 30 ppt for 180 days. After salinity change, all yearlings appeared some stress response and ions changes in blood. The yearlings showed a slow recovery by an acute salinity exchange, but a fast recovery by slow salinity exchange. In the study about the influence of salinity in growth, although the food intake of yearlings in 20 ppt was significantly higher than the yearling in the other salinities, feed efficiency was higher in 10 ppt than the other salinities. However, the food intake and the feed efficiency in 2 ppt were significantly lower than in other groups. The growth of yearlings was significantly faster in 20 ppt than in the other salinities, but the growth showed significantly slower in 2 ppt than in the other salinities.

Effect of Podophyllotoxin Conjugated Stearic Acid Grafted Chitosan Oligosaccharide Micelle on Human Glioma Cells

  • Wang, Geng Huan;Shen, He Ping;Huang, Xuan;Jiang, Xiao Hong;Jin, Cheng Sheng;Chu, Zheng Min
    • Journal of Korean Neurosurgical Society
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    • v.63 no.6
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    • pp.698-706
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    • 2020
  • Objective : To study the physiochemical characteristics of podophyllotoxin (PPT) conjugated stearic acid grafted chitosan oligosaccharide micelle (PPT-CSO-SA), and evaluate the ability of the potential antineoplastic effects against glioma cells. Methods : PPT-CSO-SA was prepared by a dialysis method. The quality of PPT-CSO-SA including micellar size, zeta potential, drug encapsulation efficiency and drug release profiles was evaluated. Glioma cells were cultured and treated with PPT and PPT-CSO-SA. The ability of glioma cells to uptake PPT-CSO-SA was observed. The proliferation of glioma cells was determined by 3-[4, 5-dimethyl-2-thiazolyl]-2, 5-diphenyl-2H-tetrazolium bromide (MTT) assay. The apoptosis and morphology of U251 cells were observed by 4',6-Diamidino-2-phenylindole dihydrochloride (DAPI) dye staining. Cell cycle analysis was performed by flow cytometry. The migration ability of U251 cells was determined by wound healing test. Results : PPT-CSO-SA had nano-level particle size and sustained release property. The encapsulation efficiency of drug reached a high level. The cellular uptake percentage of PPT in glioma cells was lower than that of PPT-CSO-SA (p<0.05). The inhibitory effect of PPT-CSO-SA on glioma cells proliferation was significantly stronger than that of PPT (p<0.05). The morphologic change of apoptosis cell such as shrinkage, karyorrhexis and karyopyknosis were observed. The percentage of U251 cells in G2/M phase increased significantly in the PPT-CSO-SA group compared with PPT group (p<0.05). Compared with the PPT group, the cell migration ability of the PPT-CSO-SA group was significantly inhibited after 12 and 24 hours (p<0.05). Conclusion : PPT-CSO-SA can effectively enhance the glioma cellular uptake of drugs, inhibit glioma cells proliferation and migration, induce G2/M phase arrest of them, and promote their apoptosis. It may be a promising anti-glioma nano-drug.

Histological Changes in the Accessory Reproductive Organs and Liver of Male Mice in Response to Short-term Treatment with an Estrogen Receptor Agonist (에스트로겐 수용체 촉진제의 단기 처리에 따른 수컷 생쥐 부속 생식기관 및 간의 조직학적인 변화)

  • Mo, Yun Jeong;Cho, Young Kuk;Cho, Hyun Wook
    • Journal of Life Science
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    • v.24 no.10
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    • pp.1070-1077
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    • 2014
  • In this study, the estrogen receptor agonist propyl pyrazole triol (PPT), which has high-affinity with the estrogen receptor alpha, was subcutaneously injected into adult male mice every 2 days for 8, 16 and 24 days, after which histological changes in accessory genital glands, including the prostate and seminal vesicle, and the liver were observed. The body and genital gland weights decreased in the PPT group relative to those of the control group. However, the liver weight was two times greater in the PPT group. The luminal area of the prostate and seminal vesicle organs was lower in the PPT group, and the epithelial cell height of the prostate was increased relative to that of the control. There were many secretory vacuoles in the supranuclear cytoplasm of epithelial cells in the seminal vesicles of the control group, but these were not observed in the PPT group. The short sinusoidal diameter of the liver was 147.0%, 198.7%, and 223.3% greater in the PPT group than in the control group after 8, 16, and 24 days of treatment, respectively. These results suggest that PPT administration affected the reproductive organs and the liver and that the histological changes increased in accordance with a rise in the concentration of PPT. Overall, the PPT treatment caused changes in the epithelial cell height and resulted in atrophy of the luminal area of the prostate, leading to altered fertility. The sinusoidal diameter of the liver dramatically increased in response to the administration of PPT, increasing the liver weight.

Effects of Estrogen Receptor Agonist on Morphology in the Female Mouse Reproductive Organs (암컷 마우스 생식기관의 형태에 미치는 에스트로겐 수용체 촉진제의 영향)

  • Lee, Eun-Jung;Han, Ji-Yeon;Cho, Hyun-Wook
    • Applied Microscopy
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    • v.39 no.4
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    • pp.301-309
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    • 2009
  • Estrogens induce pronounced structural and functional changes in male and female reproductive system, but the exact mechanisms of estrogen are not fully understood. In relation to estrogen's function, the present study was designed to identify effects of estrogen receptor agonist, 4,4',4"- (4-propyl-[1H]-pyrazole-1,3,5-triyl)tris phenol (PPT) in the reproductive organ of the female mouse. The PPT was subcutaneously given to adult female mice at a weekly dosage of 3 mg in a volume 0.06 mL of vehicle for 3, 5 or 8 weeks whereas controls received weekly injections of the castor oil vehicle. Effects of PPT on reproductive organs were analyzed using a light microscope. PPT induced decreases of body, ovary and adipose tissue weights with experimental time. Ovary diameter of PPT treatment group was reduced as compared with control group. The number of Graffian follicle and corpus luteum was reduced in PPT treatment group. The luminal diameter of uterus was increased in relation with decrease of myometrium and endometrium height by PPT administration. The number of uterine glands was decreased by PPT treatment. These data indicate that PPT treatment induced morphological change of female reproductive organs resulting in alteration of fertility.

Picropodophyllotoxin Inhibits Cell Growth and Induces Apoptosis in Gefitinib-Resistant Non-Small Lung Cancer Cells by Dual-Targeting EGFR and MET

  • Jin-Young, Lee;Bok Yun, Kang;Sang-Jin, Jung;Ah-Won, Kwak;Seung-On, Lee;Jin Woo, Park;Sang Hoon, Joo;Goo, Yoon;Mee-Hyun, Lee;Jung-Hyun, Shim
    • Biomolecules & Therapeutics
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    • v.31 no.2
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    • pp.200-209
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    • 2023
  • Patients with non-small-cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) amplification or sensitive mutations initially respond to the tyrosine kinase inhibitor gefitinib, however, the treatment becomes less effective over time by resistance mechanism including mesenchymal-epithelial transition (MET) overexpression. A therapeutic strategy targeting MET and EGFR may be a means to overcoming resistance to gefitinib. In the present study, we found that picropodophyllotoxin (PPT), derived from the roots of Podophyllum hexandrum, inhibited both EGFR and MET in NSCLC cells. The antitumor efficacy of PPT in gefitinib-resistant NSCLC cells (HCC827GR), was confirmed by suppression of cell proliferation and anchorage-independent colony growth. In the targeting of EGFR and MET, PPT bound with EGFR and MET, ex vivo, and blocked both kinases activity. The binding sites between PPT and EGFR or MET in the computational docking model were predicted at Gly772/Met769 and Arg1086/Tyr1230 of each ATP-binding pocket, respectively. PPT treatment of HCC827GR cells increased the number of annexin V-positive and subG1 cells. PPT also caused G2/M cell-cycle arrest together with related protein regulation. The inhibition of EGFR and MET by PPT treatment led to decreases in the phosphorylation of the downstream-proteins, AKT and ERK. In addition, PPT induced reactive oxygen species (ROS) production and GRP78, CHOP, DR5, and DR4 expression, mitochondrial dysfunction, and regulated involving signal-proteins. Taken together, PPT alleviated gefitinib-resistant NSCLC cell growth and induced apoptosis by reducing EGFR and MET activity. Therefore, our results suggest that PPT can be a promising therapeutic agent for gefitinib-resistant NSCLC.

Effects of mechanical intervention on cutaneous sensory change and pressure pain threshold in the same spinal segment of myofascial pain

  • Kim, Do Hyung;Lee, Su-Hyun;Lee, Byoung Hee
    • Physical Therapy Rehabilitation Science
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    • v.8 no.1
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    • pp.15-21
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    • 2019
  • Objective: The purpose of this study was to identify whether cutaneous sensory (CS) changes induced by mechanical intervention (MI) increases the trigger point threshold of the same spinal segment as well as to investigate the relationship between the amounts of change in CS pressure pain thresholds (PPT). Design: Randomized controlled trial. Methods: Thirty-nine persons with myofacial pain (MFP) were recruited in this experiment. The subjects consisted of 20 men and 19 women (age 20-39). MI was applied on the subjects using the Graston technique for 5 minutes to induce CS changes. The CS changes were measured with sensory tests by using the Von Frey Filament, and PPT changes were estimated by using the pressure threshold meter. For the observation of sensory and PPT changes with time, the test was conducted for 15 minutes including a pre, post, and after intervention session. Results: CS threshold increased significantly when MI was applied (p<0.001). On the same spinal segment, changes in the right infraspinatus PPT was observed (p<0.001) but the PPT changes in other muscles were not significantly different. Furthermore, the control group CS and PPT were not significantly different. In addition, regression analysis showed that the CS changes have a larger impact on PPT in the same spinal segment (p<0.001). Conclusions: CS changes induced by MI make to change PPT on the same spinal segment. In other words, it is possible to identify PPT changes following CS changes except for the muscle which belongs to a different spinal segment. Therefore, application of MI is necessary for the CS changes in the same spinal segment. Furthermore, it can be useful in the clinical fields as a method of providing pain control and increasing the PPT.

Ginsenosides Inhibit Endothelium - dependent Contraction in the Spontaneously Hypertensive Rat Aorta isn vitro (선천성 고혈압 랫드에서 ginsenosides에 의한 내피의존성수축의 억제작용)

  • 김낙두;최원선
    • Journal of Ginseng Research
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    • v.21 no.2
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    • pp.125-132
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    • 1997
  • Our previous study showed that in vivo treatment of spontaneously hypertensive rats (SHR) with protopanaxatriol ginsenosides (PPT) reduces the blood pressure and inhibits the con- tractions induced by endothelium-derived contracting factor (prostaglandin endoperoxide ($PGH_2$) and superoxide anion) in aorta isolated from SHR. The aim of the present study is to examine whether PPT improves endothelial functions in the isolated thoracic aorta of SHR in vitro. Treatments of aortic rings with PPT, purified ginsenoside $Rg_1$ ($Rg_1$) or indomethacin normalized endotheliuln-dependent relaxation to acetylcholine, but not with protopanaxadiol ginsenosides (PPD) and purified ginsenoside Rb1 (Rb1). The effects of PPT were dose-dependent. PGH,- and oxygen free radical-inducted contractions in rat aorta without endothelium were inhibited by PPT or $Rg_1$, but not by PPD or $Rb_1$. Contractions induced by PGF2$\alpha$, U-46619, a stable thromboxane A2 agonist or KCI (60 mM) were not inhibited by PPT, $Rg_1$ or $Rb_1$. These findings demonstrate that PPT but not PPD scavenges the oxygen-derived free radicals and/or antagonize the effects of $PGH_2$ in the vascular smooth muscle and may explain the hypotensive effect of ginseng in the SHR.

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Enhancement of skin barrier and hydration-related molecules by protopanaxatriol in human keratinocytes

  • Lee, Jeong-Oog;Hwang, So-Hyeon;Shen, Ting;Kim, Ji Hye;You, Long;Hu, Weicheng;Cho, Jae Youl
    • Journal of Ginseng Research
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    • v.45 no.2
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    • pp.354-360
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    • 2021
  • Background: Protopanaxatriol (PPT) is a secondary intestinal metabolite of ginsenoside in ginseng. Although the effects of PPT have been reported in various diseases including cancer, diabetes and inflammatory diseases, the skin protective effects of PPT are poorly understood. Methods: HaCaT cells were treated with PPT in a dose-dependent manner. mRNA and protein levels which related to skin barrier and hydration were detected compared with retinol. Luciferase assay was performed to explore the relative signaling pathway. Western blot was conducted to confirm these pathways and excavated further signals. Results: PPT enhanced the expression of filaggrin (FLG), transglutaminase (TGM)-1, claudin, occludin and hyaluronic acid synthase (HAS) -1, -2 and -3. The mRNA expression levels of FLG, TGM-1, HAS-1 and HAS-2 were suppressed under NF-κB inhibition. PPT significantly augmented NF-κB-luc activity and upregulated Src/AKT/NF-κB signaling. In addition, PPT also increased phosphorylation of the mitogen-activated protein kinases (MAPKs) ERK, JNK and p38 and upstream MAPK activators (MEK and MKK). Furthermore, transcriptional activity of AP-1 and CREB, which are downstream signaling targets of MAPK, was enhanced by PPT. Conclusion: PPT improves skin barrier function and hydration through Src/AKT/NF-κB and MAPK signaling. Therefore, PPT may be a valuable component for cosmetics or treating skin disorders.

Concentration Effect of Estrogen Receptor-${\alpha}$ Selective Agonist on the Morphology of Reproductive Organs of the Male Mice (수컷 생쥐 생식기관의 형태에 미치는 에스트로겐 수용체 알파의 선택적 촉진제의 농도별 영향)

  • Han, Ji-Yeon;Cho, Young-Kuk;Cho, Hyun-Wook
    • Applied Microscopy
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    • v.41 no.1
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    • pp.37-45
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    • 2011
  • Known as a female hormone, estrogen, has an effect on the male reproductive organs. The estrogen has to combine with the estrogen receptor to communicate a signal. Propyl pyrazole triol (PPT) is an estrogen receptor alpha selective agonist with a 410-, or 1,000-fold relative binding affinity for estrogen receptor alpha versus estrogen receptor beta. In this study, adult male mice were treated weekly with subcutaneously injections of PPT (0.01 mg, 0.1 mg, 1mg and 4 mg) suspended in castor oil (as control) for 8 weeks and observed histologically changes in testis, efferent ductule and epididymis. In the high concentrations of PPT 4 mg treatment group, a remarkable reduction was observed in the weight of the body, testis and epididymis. Microscopic examination revealed a reduction in seminiferous tubular diameter of the testis, and epithelial cell height of the epididymis in treated group during the experiment. In addition, as the diameter of the efferent ductule increased gradually, the height of epithelial cells was decreased. PPT 4 mg treatment group caused inhibition of spermatogenesis due to atrophied germinal epithelium in the testis, and decrease of adipocyte size attached to the epididymis. Sperm was not observed in the caudal epididymis of PPT 4 mg treated group. In conclusion, the injection of high concentrations of PPT into adult male mice induced physiological changes, such as an inhibition of spermatogenesis, and also histological changes within the reproductive organs.

Morphological Changes of Accessory Genital Organs Induced by Treatment with Different Concentration of Estrogen Receptor Agonist in the Male Mouse (수컷 생쥐에서 에스트로겐 수용체 촉진제의 농도별 투여에 의한 부속 생식샘의 형태학적 변화)

  • Cho, Young-Kuk;Han, Ji-Yeon;Cho, Hyun-Wook
    • Applied Microscopy
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    • v.41 no.4
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    • pp.265-276
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    • 2011
  • The aim of the present study is to validate the effects of treatment with different concentration of estrogen receptor alpha agonist, propyl pyrazole triol (PPT) on the weight and histological structure in the accessory reproductive organs (ventral prostate, seminal vesicle and preputial gland) of male mouse. Treated groups received different doses of PPT 0.01 mg, 0.1 mg and 1.0 mg per week respectively, for 3, 5, and 8 weeks. In general, the weight of reproductive organs was increased in PPT 0.01 mg and 0.1 mg treatment, however decreased in PPT 1.0 mg treatment. Epithelial tissues in the ventral prostate were changed from simple columnar epithelium to squamous or cuboidal epithelium in the treated groups. On week 3, PPT groups caused decrease of epithelial cell height in the ventral prostate. Lumen of the seminal vesicle was narrowed in the treated group. Epithelial cell height of seminal vesicle was reduced in the PPT treatment. Acinus tissue of preputial gland in PPT 1.0 mg treatment was dramatically atrophied than that of control group. These results are useful as a reference to determine the administration concentration of PPT in experiments for understanding the physiological functions of estrogen in the male.