• Title/Summary/Keyword: Inhibition dose

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Inhibition of Mouse Ear Edema by Steroidal and Triterpenoid Saponins

  • Kim, Sung-Yong;Son, Kun-Ho;Chang, Hyeun-Wook;Kang, Sam-Sik;Kim, Hyun-Pyo
    • Archives of Pharmacal Research
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    • v.22 no.3
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    • pp.313-316
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    • 1999
  • Certain steroids and triterpenoids isolated from diverse plant families were known to posses anti-inflammatory activity. In the course of finding new anti-inflammatory natural products, some steroidal and triterpenoid saponins were isolated and evaluated for their anti-inflammatory activity using in vivo mouse ear edema test. At the oral dose of 100 mg/kg, several steroidal saponins and triterpenoid saponins such as hederagenin glycosides showed significant inhibition of ear edema (20∼37% inhibition), though less potent than indomethacin and hydrocortisone.

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Effects of Low Dose ${\gamma}$ Radiation on the Radiosensitivity of Soybean(Glycine max L.) Plant (저선량 ${\gamma}$선 조사가 대두 식물체의 방사선 감수성에 미치는 영향)

  • Kim, Jae-Sung;Chae, Sung-Ki;Back, Myung-Hwa;Kim, Dong-Hee
    • Korean Journal of Environmental Agriculture
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    • v.19 no.4
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    • pp.324-327
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    • 2000
  • Soybean (Glycine max L. cv. Hwangkeum) seeds were irradiated with the dose of $0{\sim}20$ Gy to investigate the effect of the low dose ${\gamma}-ray$ radiation on the early growth and resistance to subsequent high dose of radiation. Germination rate was not enhanced in the seeds irradiated with low dos ${\gamma}-ray$ but plant height and fresh weight increased in the low dose irradiation group. The optimal radiation dose for the growth increasing was 8 Gy in soybean plant. Growth inhibition of soybean plants by high dose radiation was noticeably reduced by pre-irradiation of low dose radiation, Resistance to subsequent high dose of radiation was effective in 8 Gy and 20 Gy irradiation group.

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Intraventricular guanethidine on rabbit blood pressure (가토측뇌실내(家兎側腦室內) Guanethidine의 혈압작용(血壓作用))

  • Chung, In-Sung
    • The Korean Journal of Pharmacology
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    • v.1 no.1 s.1
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    • pp.63-65
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    • 1965
  • Rabbit blood pressure showed gradual fall by intraventricular guanethidine (5mg). The pressure rise by carotid occlusion was markedly inhibited or abolished by the guanethidine, while it was enhanced by small dose (2mg). The intraventricular guanethidine did not affect norepinephrine pressor effect, but caused marked inhibition or abolishment of depressor action of serotonin.

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Evaluation of Anticancer Activity of Curcumin Analogues Bearing a Heterocyclic Nucleus

  • Ahsan, Mohamed Jawed
    • Asian Pacific Journal of Cancer Prevention
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    • v.17 no.4
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    • pp.1739-1744
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    • 2016
  • We report herein an in vitro anticancer evaluation of a series of seven curcumin analogues (3a-g). The National Cancer Institute (NCI US) Protocol was followed and all the compounds were evaluated for their anticancer activity on nine different panels (leukemia, non small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer) represented by 60 NCI human cancer cell lines. All the compounds showed significant anticancer activity in one dose assay (drug concentration $10{\mu}M$) and hence were evaluated further in five dose assays (0.01, 0.1, 1, 10 and $100{\mu}M$) and three dose related parameters $GI_{50}$, TGI and $LC_{50}$ were calculated for each (3a-g) in micro molar drug concentrations (${\mu}M$). The compound 3d (NSC 757927) showed maximum mean percent growth inhibition (PGI) of 112.2%, while compound 3g (NSC 763374) showed less mean PGI of 40.1% in the one dose assay. The maximum anticancer activity was observed with the SR (leukemia) cell line with a $GI_{50}$ of $0.03{\mu}M$. The calculated average sensitivity of all cell lines of a particular subpanel toward the test agent showed that all the curcumin analogues showed maximum activity on leukemia cell lines with $GI_{50}$ values between 0.23 and $2.67{\mu}M$.

Prediction of drug-Drug Interaction During Oral Absorption of Carrier-Mediated Compounds in Humans

  • Oh, Doo-Man;Gordon L. Amidon
    • Archives of Pharmacal Research
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    • v.17 no.5
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    • pp.364-370
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    • 1994
  • A microscopic mass balance approach has been developed to estimate the extent and rate of absorption for camier-mediated comounds. For the case competitive inhibition in the presence of an inhibitor which shares the same camier, the fraction dose absorbed (F) and absorption rate constant ($K_a$) of a drug can be calculated from its concentration profile in the intestinal lumen. Absorption parameters obtained by single-pass perfusion experiments were used in the simultaion of the absorption of some aminopenicilins. Predicted fractions dose absorbed and absorption rate constants of ampicilin and amoxicilin were significantly reduced in the presence of a 6-times higher molar dose of cyclacilin. The drug-drug interactions on the competitive absroption of camier-mediated compounds were determined with regard to F and $K_a$. Predicted decreases in F for some aminopenicilins corrlated well with decrease in the urinary recovery in humans reported in the literature. Predicted decrease in the mean absorption rate constant ($\barK_a$) explain the delays in the time of peak plasma concentration ($T_{max}$) reported in humans.

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Anti-metastatic Effect of Samguikoeui-Tang Via Inhibition of Matrix Metalloproteinases Activities (금속단백분해효소의 활성 저해를 통한 삼귀고의탕의 전이억제 효과)

  • Kim, Sung-Moo;Rhee, Yun-Hee;Lee, Joo-Ho;Kim, Sung-Hoon;Lee, Eun-Ok
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.22 no.6
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    • pp.1470-1474
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    • 2008
  • This study was performed to examine the anti-metastatic effect of ethanol extract of Samguikoeui-Tang (SGKE), a formula consisting of four oriental herbs, in highly-metastatic HT1080 human fibrosarcoma cells. SGKE significantly inhibited the adhesion of HT1080 cells to matrigel at nontoxic concentrations in a dose-dependent manner, while it did not exert cytotoxicity against HT1080 cells up to the concentration of 100 ${\mu}g$/ml. Also, SGKE depressed the activity of matrix metalloproteinase-2 (MMP-2) and matrix metalloproteinase-9 (MMP-9) by gelatin zymography. However, SGKE did not affect the mRNA expression of MMP-2 and TIMP-2, an inhibitor of MMP-2, by RT-PCR analysis. In addition, the effect of SGKE on HT1080 cell invasion was determined using Boyden chamber assay. SGKE suppressed the invasion of HT1080 cells in a dose-dependent manner. Taken together, these results suggest that SGKE has an anti-metastatic effect via inhibition of MMP-2 and -9 activities.

Anti-nociceptive Effect of Curcuma longa Extract on Acetic Acid induced Pain Model (강황 에탄올 추출물 및 그 분획물의 초산 유발에 의한 통증억제 효과)

  • Yoon, Won Ho;Lee, Keyong Ho
    • Korean Journal of Pharmacognosy
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    • v.46 no.3
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    • pp.229-233
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    • 2015
  • The anti-nociceptive effect of an ethanol extract and its various solvent fractions from Curcuma longa Linne ethanol extract was studied using the writhing test in mice. Different fractions by various solvent extraction from Curcuma longa Linne ethanol extract were administered orally 1 hr or time-course (0.5, 1, 2 and 5 hr) before intraperitoneal injection of acetic acid. After treatment with 30% ethanol extract and n-butanol fraction, CB-1, at a dose of 250 mg/kg, the significant writhing responses were 87.5 ± 13.4 (inhibition rate 31%, p<0.01) and 75.1 ± 11.1 (inhibition rate 41%, p<0.01) lower than the control group. At the dose of CB-1 50 mg/kg and 250 mg/kg, CB-1 showed a similar activity comparing to diclofenac of 10 mg/kg. A time-course experiment was performed, which involved oral administration of CB-1 (250 mg/kg) at 0, 0.5, 1, 2, and 5 hr before acetic acid intraperitoneal injection. The most effective time of CB-1 was 30 min before treatment and persisting until 2 hr. This study showed that Curcuma longa Linne has anti-nociceptive properties comparable with those of diclofenac, which suggests promise for the treatment of intractable visceral pain in humans. Major components of the active fraction are identified as curcumin, cyclocurcumin and demethoxycurcumin.

Anti-tumor Substance from Panax Kin.ienk Roots (고려인삼 뿌리에 있는 항종량 물질)

  • Hiroshi Yamamoto;Mitsuo Katario;Hisashi Matsunaga
    • Journal of Ginseng Research
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    • v.14 no.2
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    • pp.244-252
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    • 1990
  • Antitumor polyacetylenic alcohol, panaxytriol (Cl7 H26O3), was isolated and purified from a powder of the root of Pnnnx tin.1.encl C.A. Meyer. Panaxytriol possesses unusual property of being soluble in both water and organic solvents. Panaxytriol inhibited the growth of various kinds of human cultured cell lines in dose-dependent fashion in vitro. The in vivo effects of panaxytriol were tested against C57BL/6 mice transplanted with Bl6 melanomas. Panaxytriol (8 and 40 mg/kg) administered intra-muscularly(im) produced significant tumor growth delays in mice. Although a detailed mechanism of growth inhibition by panaxytriol is unknown, preliminary results appear to implicates a surface membrane site of action. And its action seems to be more dose-dependent than time-dependent. Finally, panaxytriol pharmacokinetics was evaluated in mice given single 8 mg/kg doses intraperitoneally (ip) or im. Serum panaxytriol content was measured using both tumor growth inhibitory assay and a gas chromatographic method. The maximum serum panaxytriol content after ip and im administration was 35.0 and 1.6 $\mu$g/ml respectively. These results indicate that the compound may act as cytotoxic substance even in patients.

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In vitro and in vivo Evaluation of the Antitumor Efficiency of Resveratrol Against Lung Cancer

  • Yin, Hai-Tao;Tian, Qing-Zhong;Guan, Luan;Zhou, Yun;Huang, Xin-En;Zhang, Hui
    • Asian Pacific Journal of Cancer Prevention
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    • v.14 no.3
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    • pp.1703-1706
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    • 2013
  • Lung cancer remains a deadly disease with unsatisfactory overall survival. Resveratrol (Res) has the potential to inhibit growth of several types of cancer such as prostate and colorectal examples. In the current study, we evaluated in vitro and in vivo anticancer efficiency of Res in a xenograft model with A549 cells. Cell inhibition effects of Res were measured by MTT assay. Apoptotis of A549 cells was assessed with reference to caspase-3 activity and growth curves of tumor volume and bodyweight of the mice were measured every two days. In vitro cytotoxicity evaluation indicated Res to exert dose-dependent cell inhibition effects against A549 cells with activation of caspase-3. In vivo evaluation showed Res to effectively inhibit the growth of lung cancer in a dose-dependent manner in nude mice. Therefore, we believe that Res might be a promising phytomedicine for cancer therapy and further efforts are needed to explore this potential therapeutic strategy.

CYTOTOXICITY OF D-GALACTOSAMINE ON PRIMARY CULTURES OF ADULT RAT HEPATOCYTES

  • Yang, K.H.;Park, Kwan-Ha;Kim, Byung-Sam
    • Toxicological Research
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    • v.3 no.2
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    • pp.73-80
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    • 1987
  • Primary cultures of adult rat hepatocytes were used to study the cytotoxicity of D-galactosamine. Hepatocytes were isolated by a collagenase perfusion technique and maintained as monolayers in serum-free medium on collagen-coated culture dishes. Treatment of galactosamine to the culture markedly inhibited the uptake of ${\alpha}$-aminoisobutyric acid (AIB) inducible with glucagon and dexamethasone. At0.1 mM of galactosamine, AIB uptake was inhibited significantly when treated for 12 hr. At higher doses (0.25, 0.5 and 1.0mM), a significant inhibition was noticed after 1 hr exposure. Generally the magnitude of the inhibition was related to the dose and treatment time of galactosamine. Treatment of galactosamine also produced a dose- and treatment time-related suppression of the tyrosine aminotransferase (TAT) induction caused by dexamethasone. Meanwhile, uptake of ouabain was not affected by the treatment of galactosamine. The viability of the hepatocytes was decreased only slightly by the treatment of galactosamine; more than 87% of the cells excluded tryphane blue when treated 1 mM galactosamine for 12 hr. Galactosamine induced depressions of AIB uptake and TAT activity were prevented by the simultaneous addition of uridine to the culture. D-Galactosamine, cytotoxicity, hepatocytes culture, ${\alpha}$-aminoisobutyric acid uptake, tyrosine aminotransferase.

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