• 제목/요약/키워드: Phosphatase inhibition

검색결과 192건 처리시간 0.03초

Monocrotophos induced inhibition of the activities of testis and accessory reproductive organs in male mice

  • Patill, Saraswati B;Malashetty, Vijaykumar B
    • Advances in Traditional Medicine
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    • 제7권3호
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    • pp.304-310
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    • 2007
  • Monocrotophos was administered orally to adult male albino mice at dose level of 3.0 mg/kg body weight/day/mice for 50 days. The treatment has found to affect spermatogenesis as well as the endocrine functions of the testis as indicated by gravimetric, histopathological and biochemical changes. The treatment has caused degenerative changes in the seminiferous tubules and Leydig cells of the testis and regression of the epididymis, seminal vesicle, vas deferens, prostate, Cowper's gland and levator ani. Similarly, cauda epididymal sperm count and sperm motility have shown significant reduction. There was a significant reduction in the protein, glycogen, sialic acid, acid and alkaline phosphatase and increase in cholesterol in the testis of monocrotophos treated mice compared with the control. The causative factors for these changes due to monocrotophos administration were discussed.

Sulforaphane Inhibits Osteoclastogenesis by Inhibiting Nuclear Factor-κB

  • Kim, Soo-Jin;Kang, So-Young;Shin, Hyun-Hee;Choi, Hye-Seon
    • Molecules and Cells
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    • 제20권3호
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    • pp.364-370
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    • 2005
  • We show that sulforaphane inhibits osteoclastogenesis in the presence of macrophage colony-stimulating factor (M-CSF) and receptor for activation of nuclear factor-${\kappa}B$ ligand (RANKL) in osteoclast (OC) precursors. Sulforaphane, an aliphatic isothiocyanate, is a known cancer chemo-preventative agent with anti-oxidative properties. Nuclear factor-${\kappa}B$ (NF-${\kappa}B$) is a critical transcription factor in RANKL-induced osteoclastogenesis, and electrophoretic mobility shift assays (EMSAs) and assay of NF-${\kappa}B$-mediated secreted alkaline phosphatase (SEAP) revealed that sulforaphane selectively inhibited NF-${\kappa}B$ activation induced by RANKL. Inhibition may involve interaction of sulforaphane with thiol groups, since it was prevented by reducing agents.

Chlorophenol류의 세포화학적 독성에 관한 연구 (Studies on Cytochemical Toxicities of Chlorophenols to the Rat)

  • 정용
    • 약학회지
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    • 제22권4호
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    • pp.175-192
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    • 1978
  • Chlorination of the polluted water may produce odoriferous and objectionable-tasting chlorophenols which are hazardous to health. These studies were undertaken to investigate the hazardous effects of chlorophenols to the rat. 1. The chlorophenols such as o-chlorophenol and 2,6-dichlorophenol inhibited rat growth and caused increment of the ratio between liver weight and body weight. 2. The hemoglobin content, hamatocrit ratio and A/G of rat blood were decreased by chlorophenols administration. The activities of alkaline phosphatase, lactic dehydrogenase (LDH) and glutamate oxaloacetate transaminase (GOT) in serum as well as in liver were increased provisonally and decreased after one or two weeks adminstration. 3. The liver mitochondrial respiration ($QO_{2}$) was inhibited by chlorophenols treatment in in-vivo and in-vitro test. 4. The liver microsomal cytochrome P-450 was decreased by chlorophenols administration 5. Liver tissue was degenerated with congestion, atrophy, swelling, vacuolation, dilation of rough endoplasmic reticulum and denature of mitochondrial particle with swelling, and cristal destruction by chlorophenols adminstration. 6. After one and two weeks of adminstration of chlorophenols to rat, the aberrations of bone marrow chromosome and inhibition of its mitosis were observed respectively.

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자혈양근탕(滋血養筋湯)이 부신피질호르몬에 의해 억제된 조골세포 기능에 미치는 영향 (Effects of JY on Osteoblastic Cell from Rat Calvariae in the Presence of Glucocorticoid)

  • 최정신;황귀서
    • 대한예방한의학회지
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    • 제12권2호
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    • pp.197-206
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    • 2008
  • The inhibition of osteoblast by glucocorticoid is recognized as its action mechanism of decreased bone formation. In this study, the effect of JY, Jahyulyangkeuntang, on the differentiation and mineralization of osteoblastic cells was investigated in the presence of dexamethasone. The cell counting, enzyme activity assay, MTT assay, collagen content assay were done to determine the cell proliferation, alkaline phosphatase(ALP) activity, bone martrix production, and cell apoptosis. JY enhanced the cell proliferation after the culture for 10 days. ALP activity and total protein synthesis, and intracellular collagen synthesis were increased when the cells were treated with JY. And JY restored calvarial cell function decreased by dexamethasone.

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Acid sphingomyelinase-mediated blood-brain barrier disruption in aging

  • Park, Min Hee;Jin, Hee Kyung;Bae, Jae-sung
    • BMB Reports
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    • 제52권2호
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    • pp.111-112
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    • 2019
  • Although many studies have reported that the breakdown of the blood-brain barrier (BBB) represents one of the major pathological changes in aging, the mechanism underlying this process remains relatively unexplored. In this study, we described that acid sphingomyelinase (ASM) derived from endothelial cells plays a critical role in BBB disruption in aging. ASM levels were elevated in the brain endothelium and plasma of aged humans and mice, resulting in BBB leakage through an increase in caveolae-mediated transcytosis. Moreover, ASM caused damage to the caveolae-cytoskeleton via protein phosphatase 1-mediated ezrin/radixin/moesin dephosphorylation in primary mouse brain endothelial cells. Mice overexpressing brain endothelial cell-specific ASM exhibited acceleration of BBB impairment and neuronal dysfunction. However, genetic inhibition and endothelial specific knock-down of ASM in mice improved BBB disruption and neurocognitive impairment during aging. Results of this study revealed a novel role of ASM in the regulation of BBB integrity and neuronal function in aging, thus highlighting the potential of ASM as a new therapeutic target for anti-aging.

Inhibition of tyrosine phosphatases blocks plasma membrane blebbing during Fas- induced apoptosis of Jurkat T cells without affecting the cytotoxicity of Fas-ligation

  • Cho, Jun-Young;Kim, Kwang-Dong;Kho, Chang-Won;Park, Sung-Goo;Chung, Kyeong-Soo;Lim, Jong-Seok
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.135.2-135.2
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    • 2003
  • Plasma membrane blebs are observed in many types of apoptotic cells, but their processes of formation remain to be clarified. In the present study, we investigated whether there is a relationship between change of intracellular phosphotyrosine levels and biochemical apoptotic events in Jurkat T cells undergoing apoptosis by agonistic anti-Fas antibody. When Jurkat cells were treated with Fas-antibody in the presence or absence of pretreatment with sodium orthovanadate ($Na_3${VO}_4$), a phosphotyrosine phosphatase (PTPase) inhibitor, membrane blebs disappeared in orthovanadate-treated cells. (omitted)

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Sopungsungi-won (SP) Prevents the Onset of Hyperglycemia and Hyperlipidemia in Zucker Diabetic Fatty Rats

  • Kim, Youn-Young;Kang, Hyo-Joo;Ko, Sung-Kwon;Chung, Sung-Hyun
    • Archives of Pharmacal Research
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    • 제25권6호
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    • pp.923-931
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    • 2002
  • Sopungsungi-won (SP) is a known for\mula for senile constipation and diabetes mellitus, based on traditional Korean medicine. The preventive effect of SP on the development of overt diabetes in Zucker diabetic fatty (ZDF) rats was evaluated. When administered orally through a diet for 8 weeks, diabetic conditions such as hyperglycemia, polydipsia and hypertriglyceridemia were all ameliorated in SP-treated rats. In parallel with the onset and progression of hyperglycemia in the ZDF control rats; there was a marked decline in plasma insulin concentrations from 26.1 $\mu$U/ml, at age 7 weeks, to 14.8 $\mu$U/ml at age 15 weeks. In the SP-treated rats, however, the plasma insulin concentrations did not decline, and SP at a dose of 5 g/kg significantly increased the insulin levels to 31.9 $\mu$U/ml. Early normalization of plasma insulin and a retained ability to subsequently increase plasma insulin were indicative of a pancreatic $\beta$ cell protective action by the SP for\mula. In addition, expressions of an insulin-responsive gene and corresponding protein, glucose transporter 4 (GLUT4), in skeletal \muscle, were also determined in SP- and rosiglitazone-treated ZDF rats. mRNA and protein levels of GLUT4 in SP-treated rats were upregulated in a dose dependent manner. Furthermore, when ZDF rats were treated with 2 g/kg of the SP for\mula, the activity of glucose-6-phosphatase was decreased by 49%, whereas the activity of glucokinase was increased by 196%, compared to the ZDF control rats. Taken together, these data provide evidence that the SP for\mula markedly lowered the plasma glucose levels, probably through an effect not only on improvement of insulin action, but through a combined sti\mulation of glycolysis and an inhibition of gluconeogenesis in the liver, and also suggest the validity of SP's clinical use in the treatment of type 2 diabetes mellitus following further toxicological investigation.

제초제(除草劑)가 토양환경중(土壤環境中) 효소활성(酵素活性)에 미치는 영향(影響) (Effects of Herbicides on Enzyme Activities in Soil Environment)

  • 김장억;홍종욱
    • Applied Biological Chemistry
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    • 제31권1호
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    • pp.79-85
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    • 1988
  • 제초제(除草劑)가 토양환경내(土壤環境內)의 생화학적(生化學的) 전환과정(轉換過程)에 미치는 영향(影響)을 규명(糾明)하기 위해서 화학구조(化學構造)가 다른 여러 종류의 제초제(除草劑)를 질소질비료(室素質肥料)인 요소(尿素)와 함께 토양(土壤)에 처리(處理)하였을때 토양효소(土壞酵素)의 활성(活性)에 미치는 영향(影響)과 농약(農藥)의 잔류량(殘留量)의 변화(變化)를 조사(調査)한 결과(結果)는 다음과 같았다. 제초제(除草劑)의 처리(處理)로 Urease의 활성(活性)에는 Urea계(系), dinoseb, propanil, diphenylether계(系), 산amide계(系)의 순(順)으로 저해율(沮害率)이 높았다. L-Glutaminase 및 protease의 활성(活性)에는 dinoseb, urea계(系), diphenylether계(系), 산amide계(系)의 순(順)으로 저해율(沮害率)이 높았으며 phosphatase는 dinoseb, diphenylether계(系), urea계(系), 산amide계(系)의 순(順)으로 저해율(沮書率)이 높았다. 대체적으로 제초제(除草劑)의 처리(處理)로 처리초기(處理初期)에는 저해(沮害)를 보이다가 28일(日) 이후(以後)에는 거의 영향(影響)이 없거나 활성(活性)을 약간 증가(增加)시켰다. 요소(尿素)의 시용(施用)으로 인(因)해 제초제(除草劑)의 분해(分解)는 무시용구(無施用區)에 비해서 약간 촉진(促進)되었다.

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Ceramide is Involved in $MPP^+-induced$ Cytotoxicity in Human Neuroblastoma Cells

  • Nam, Eun-Joo;Lee, Hye-Sook;Lee, Young-Jae;Joo, Wan-Seok;Maeng, Sung-Ho;Im, Hye-In;Park, Chan-Woong;Kim, Yong-Sik
    • The Korean Journal of Physiology and Pharmacology
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    • 제6권6호
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    • pp.281-286
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    • 2002
  • To understand the cytotoxic mechanism of $MPP^+,$ we examined the involvement of ceramide in $MPP^+-induced$ cytotoxicity to human neuroblastoma SH-SY5Y cells. When SH-SY5Y cells were exposed to $MPP^+,\;MPP^+$ induced dose-dependent cytotoxicity accompanied by 2-fold elevation of intracellular ceramide levels in SH-SY5Y cells. Three methods were used to test the hypothesis that the elevated intracellular ceramide is related to $MPP^+-induced$ cytotoxicity: $C_2-ceramide$ was directly applied to cells, sphingomyelinase (SMase) was exogenously added, and oleoylethanolamine (OE) was used to inhibit degradation of ceramide. Furthermore, inhibition of ceramide-activated protein phosphatase (CAPP), the effector of ceramide, using okadaic acid (OA) attenuated cell death but treatment of fumonisin $B_1,$ the ceramide synthase inhibitor, did not alter the cytotoxic effect of $MPP^+.$ Based on these, we suggest that the elevation of intracellular ceramide is one of the important mediators in $MPP^+-induced$ cell death.

A Cell-Based Assay System for Monitoring NF-$\kappa$B Activity in Human Epidermal Keratinocytes: A Screening Tool of the Antioxidants and Anti-inflammatories for Dermatological Purpose

  • Moon, Ki-Young;Hahn, Bum-Soo;Lee, Jinseon;Kim, Yeong-Shik
    • 대한화장품학회지
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    • 제27권1호
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    • pp.17-27
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    • 2001
  • A cell-based assay system for monitoring NF-$textsc{k}$B activity was developed to determine the influence of activated NF-$textsc{k}$B in human HaCaT cells. The pNF-$textsc{k}$B-SEAP-NPT plasmid that permits expression of the secreted alkaline phosphatase (SEAP) reported gene in response to the NF-$textsc{k}$B activity and contains neomycin phosphotransferase (NPT) gene for the geneticin resistance in host cells was constructed and transfected into human keratinocyte cell line HaCaT. Human HaCaT transfectant cells secreted the SEAP enzyme into the culture medium in a time-dependent manner until 72h. NF-$textsc{k}$B activities were measured in the SEAP reporter gene assay using a fluorescent detection method. The treatment of HaCaT cell transfectants with known antioxidants [e.g., N-acetyl-L-cysteine and vitamin C] showed inhibition of NF-$textsc{k}$B activity in a time-and concentration-dependent manner. The phorbol 12-myristate 13-acetate (PMA) known as a stimulator of NF-$textsc{k}$B expression demonstrated that it increased NF-$textsc{k}$B activity in a time- and concentration-dependent manner. This assay system could be used to determine the quantitative measurement of NF-$textsc{k}$B activity in the human skin and allow the screening of anti-inflammatory agents from various synthetic chemicals and natural products for dermatological purpose. Abbrevitions used: NF-$textsc{k}$B, nuclear factor kappa B; I-$textsc{k}$B, Inhibitory kappa B; SEAP, secreted alkaline phosphatase; NPT, neomycin phosphotransferease; PCR, polymerase chain reaction: dNTP, deoxynucleoside triphosphates; DMEM, dulbecco’s modified eagle medium; FBS, fetal bovine serum; PBs, phosphate-buffered saline; MUP, 4-methylumbellifery phosphate; NAC, N-acetyl-L-cysteine; DMSO, dimethyl sulfoxide; PMA, phorbol 12-myristate 13-acetate.

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