• 제목/요약/키워드: Acidic drug

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Histochemical effects on the mucin of the Trachea Epithelium in cis-Diamminedichloroplatinum(Ⅱ)Treated rats (cis-Diamminedichloroplatinum(Ⅱ)이 흰쥐의 기관섬모상피내 점액질 조성에 미치는 영향)

  • Kim, Bo-Hyung;Kang, Sung-Ho;Kim, Dong-Wook
    • Korean Journal of Bronchoesophagology
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    • v.5 no.2
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    • pp.164-173
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    • 1999
  • Background : cis-Diamminedichloroplatinum(Ⅱ)(cis-platin) has been exhibited similar to bifunctional alkylating agents in the cell and known as an effective anticancer drug. Although this agent is very beneficial to the cancer patients, it may also damage to the normal cell. Many side effects were developed. Objectives : This experiments was undertaken to pursue the effect of cis-Platin on the mucous variation of the trachea. Materials and Methods : The male of Sprague-Dawley strain were used as and experimental animals. The experimental animals were killed at 1, 3 days and 1, 2 and 3 weeks after the third injection of cis-Platin was administered 1.5mg/kg to intraperitoneal injection at once a week for three weeks. The trachea was fixed to neutral formaline and stained with alcian blue(pH 1.0)-PAS, alcian blue(pH 2.5)-PAS double stains and these preparation observed with light microscope. Results : 1. In the trachea stained with alcian blue(pH 2.5)-PAS double stain, the epithelial cells were constricted in the 1 week, In the 1st day, 3rd day and 1st week, acidic mucopolysaccharide was increased but in the 2nd week, neutral mucopolysaccharide was increase. 2. In the trachea stained with alcian blue(pH 1.0)-PAS double stain, the 1st and 3rd day exhibited sulfa mucopolysaccharide with moderately or weakly positive reaction. In the 1st week the sulfa mucopolysaccharide with strongly positive reaction was increased. In the 2nd and 3rd week, the sulfa mucopolysaccharide with weakly positive and non-sulfa or neutral mucopolsaccharide with negative reaction were modified. Conclusion : It is consequently suggested that cis-Platin induces reversible toxic damage to tracheal cells including goblet cell.

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Analytical trend of perfluorinated compounds in environmental and biota samples (환경 및 생체시료 중 과불화 화합물의 분석 동향)

  • Lee, Won-Woong;Chang, Won-Hee;Pyo, Hee-Soo;Kang, Tae-Seok;Hong, Jong-Ki
    • Analytical Science and Technology
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    • v.23 no.4
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    • pp.331-346
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    • 2010
  • Perfluorinated compounds have characteristics of resistance to heat, acidic, basic conditions and also resist water, oil, grease, pollutant. Futhermore they are used by various industrial material, nowadays, they produced in large scale for indutrial and commercial areas. However, they also resist metabolizing and degrading in environmental system (plant, animal, even human body). Moreover, in animal's bodies, PFCs can be accumulated in organ (eg; liver) and lead to liver cell necrosis even oncogenesis. Perfluorinated compounds are newly registered as new persistent organic pollutants (POPs) on Stockholm convention in 2009. Therefore necessity for analytical methodology for determination of PFCs in various environmental samples is even more increased. This study discussed sample preparation and instrumental conditions for the analysis of PFCs in environmental and biota samples.

Solubility and Physicochemical Stability of Caroverine Hydrochloride in Aqueous Solution (수용액중 염산카로베린의 용해성 및 안정성)

  • Gwak, Hye-Sun;Lee, Dong-Soo;Chun, In-Koo
    • Journal of Pharmaceutical Investigation
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    • v.28 no.2
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    • pp.121-126
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    • 1998
  • The solubility and physicochemical stability of caroverine hydrochloride (CRV), an antispasmodic, in buffered aqueous solutions were studied using a reverse phase high performance liquid chromatography. The solubilty of the drug at pH 2.76-5.40 was similar at the range 31.9-36.2 mg/ml $(34^{circ}C)$, but, at the pH higher than 6.0, markedly decreased. The use of polyethylene glycol 400 as a cosolvent did not increase the solubility at any compositions examined. Moreover. increasing molar concentration of aqueous phosphate buffer from 0 to 0.5 M remarkably decreased the solubility. The degradation of CRY followed the apparent first-order kinetics. The degradation was accelerated with decreasing pH and increasing storage temperature. The half-lives for the degradation of CRY (1.0 mg/ml) at pH 1.28. 4.01 and 5.93 $(45^{\circ}C)$ were 2.8, 31.4 and 124 hr. respectively. The pHs of incubated solutions were to some extent lowered perhaps due to the formation of acidic degradation products. The addition of disodium edetate (0.01%) to the CRY solution (pH 4.95) retarded 2.5 times the degradation rate at $45^{\circ}C$, but the use of sodium bisulfite (0.1%) accelerated 2.9 times the rate. The activation energy for the CRY solution (20 mg/ml. pH 5.4) containing 0.01% EDTA was calculated to be 5.98 kcal/mole. When the solution was stored under nitrogen displacement in ampoule, there was no significant degradation even after 3 months at $40^{\circ}C$, indicating that protection from oxidation by air (oxygen) is essential for the complete stabilization of CRY solution.

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Evaluation of the Anti-Tumor Effects of Paclitaxel-Encapsulated pH-Sensitive Micelles

  • Han, Jong-Kwon;Kim, Min-Sang;Lee, Doo-Sung;Kim, Yoo-Shin;Park, Rang-Woon;Kim, Kwang-Meyung;Kwon, Ick-Chan
    • Macromolecular Research
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    • v.17 no.2
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    • pp.99-103
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    • 2009
  • We evaluated the efficacy of pH-sensitive micelles, formed by methoxy poly(ethylene glycol)-b-poly($\beta$)-amino ester) (PEG-PAE), as carriers for paclitaxel (PIX), a drug currently used to treat various cancers. PTX was successful encapsulated by a film hydration method. Micelles encapsulated more than 70% of the PTX and the size of the PTX-encapsulated micelles (PTX-PM) was less than 150 nm. In vitro experiments indicated that the micelles were unstable below pH 6.5. After encapsulation of PTX within the micelles, dynamic light scattering (DLS) studies indicated that low pH had a similar demicellization effect. An in vitro release study indicated that PTX was slowly released at pH 7.4 (normal body conditions) but rapidly released under weakly acidic conditions (pH 6.0). We demonstrated the safety of micelles from in vitro cytotoxicity tests on HeLa cells and the in vivo anti-tumor activity of PTX-PM in B16F 10 tumor-bearing mice. We concluded that these pH-sensitive micelles have potential as carriers for anti-cancer drugs.

Effects of aloe-emodin on alveolar bone in Porphyromonas gingivalis-induced periodontitis rat model: a pilot study

  • Yang, Ming;Shrestha, Saroj K;Soh, Yunjo;Heo, Seok-Mo
    • Journal of Periodontal and Implant Science
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    • v.52 no.5
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    • pp.383-393
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    • 2022
  • Purpose: Aloe-emodin (AE), a natural anthraquinone abundant in aloe plants and rhubarb (Rheum rhabarbarum), has long been used to treat chronic inflammatory diseases. However, AE's underlying mechanisms in periodontal inflammation have not been fully elucidated. Acidic mammalian chitinase (AMCase) is a potential biomarker involved in bone remodeling. This study aimed to evaluate AE's effect on periodontitis in rats and investigate AMCase expression. Methods: Eighteen Sprague-Dawley rats were separated into the following groups: healthy (group 1), disease (group 2), vehicle (group 3), AE high-dose (group 4), and AE low-dose (group 5). Porphyromonas gingivalis ligatures were placed in rats (groups 2-5) for 7 days. Groups 4 and 5 were then treated with AE for an additional 14 days. Saliva was collected from all groups, and probing pocket depth was measured in succession. Periodontal pocket tissues were subjected to histomorphometric analysis after the rats were sacrificed. Bone marrow-derived macrophages and murine macrophages were stimulated with receptor activator of nuclear factor-κB ligand (RANKL) and treated with different concentrations of AE. AMCase expression was detected from the analysis of saliva, periodontal pocket tissues, and differentiated osteoclasts. Results: Among rats with P. gingivalis-induced periodontitis, the alveolar bone resorption levels and periodontal pocket depth were significantly reduced after treatment with AE. AMCase protein expression was significantly higher in the disease group than in the healthy control (P<0.05). However, AE inhibited periodontal inflammation by downregulating AMCase expression in saliva and periodontal pocket tissue. AE significantly reduced RANKL-stimulated osteoclastogenesis by modulating AMCase (P<0.05). Conclusions: AE decreases alveolar bone loss and periodontal inflammation, suggesting that this natural anthraquinone has potential value as a novel therapeutic agent against periodontal disease.

Panaxcerol D from Panax ginseng ameliorates the memory impairment induced by cholinergic blockade or Aβ25-35 peptide in mice

  • Keontae Park;Ranhee Kim;Kyungnam Cho;Chang Hyeon Kong;Mijin Jeon;Woo Chang Kang;Seo Yun Jung;Dae Sik Jang ;Jong Hoon Ryu
    • Journal of Ginseng Research
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    • v.48 no.1
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    • pp.59-67
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    • 2024
  • Background: Alzheimer's disease (AD) has memory impairment associated with aggregation of amyloid plaques and neurofibrillary tangles in the brain. Although anti-amyloid β (Aβ) protein antibody and chemical drugs can be prescribed in the clinic, they show adverse effects or low effectiveness. Therefore, the development of a new drug is necessarily needed. We focused on the cognitive function of Panax ginseng and tried to find active ingredient(s). We isolated panaxcerol D, a kind of glycosyl glyceride, from the non-saponin fraction of P. ginseng extract. Methods: We explored effects of acute or sub-chronic administration of panaxcerol D on cognitive function in scopolamine- or Aβ25-35 peptide-treated mice measured by several behavioral tests. After behavioral tests, we tried to unveil the underlying mechanism of panaxcerol D on its cognitive function by Western blotting. Results: We found that pananxcerol D reversed short-term, long-term and object recognition memory impairments. The decreased extracellular signal-regulated kinases (ERK) or Ca2+/calmodulin-dependent protein kinase II (CaMKII) in scopolamine-treated mice was normalized by acute administration of panaxcerol D. Glial fibrillary acidic protein (GFAP), caspase 3, NF-kB p65, synaptophysin and brainderived neurotrophic factor (BDNF) expression levels in Aβ25-35 peptide-treated mice were modulated by sub-chronic administration of panaxcerol D. Conclusion: Pananxcerol D could improve memory impairments caused by cholinergic blockade or Aβ accumulation through increased phosphorylation level of ERK or its anti-inflammatory effect. Thus, panaxcerol D as one of non-saponin compounds could be used as an active ingredient of P. ginseng for improving cognitive function.

Food Functionality and Bioactivity of Vacuum Freeze-dried Fish Roe Concentrates (동결건조 어류 알 농축물의 식품기능성 및 생리활성)

  • Yoon, In Seong;Kim, Hyeung Jun;Kang, Sang In;Kim, Do Youb;Lee, Chang Young;Jeong, U-Cheol;Kim, Jin-Soo;Heu, Min Soo
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.53 no.3
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    • pp.403-416
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    • 2020
  • The purpose of this study was to evaluate the food functional properties and in vitro bioactivity of vacuum freeze-dried fish roe concentrates (FRCs) prepared from Alaska pollock Theragra chalcogramma (AP), bastard halibut Paralichthys olivaceus (BH) and skipjack tuna Katsuwonus pelamis (ST). All three species showed better buffering capacity on the alkaline side (pH 10-12) than on the acidic side. The water-holding capacities of the FRCs were 3.5, 8.5 and 4.2 g/g protein for AP, BH and ST, respectively, and were significantly higher than that of commercial egg white. The protein solubilities of the FRCs were 42.5% (AP), 50.0% (BH) and 13.9% (ST). The foaming capacities of the FRCs were not significantly different among the species (128.0% for AP, 128.3% for BH, and 143.3% for ST; P>0.05), and their foam stability was maintained at 53.0-74.2% for 60 minutes. The oil-in-water emulsifying activity indexes of AP and BH (19.5 and 20.2 ㎡/g protein, respectively) were significantly superior to that of ST (P<0.05). The 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis-3-ethylbenzothia-zoline-6-sulfonic acid radical-scavenging activities (IC50, mg/mL) of the FRCs were in the ranges of 1.05-3.26 and 0.13-0.18 mg/mL, respectively, and the angiotensin I converting enzyme inhibitory activity was in the range of 0.97-1.89 mg/mL.

Characteristics of Whey Protein (WPC-30) Hydrolysate from Cheese Whey (치즈유청으로부터 제조한 유청단백질 가수분해물의 특성에 관한 연구)

  • Yoon, Yoh-Chang;An, Sung-Il;Jeong, A-Ram;Han, Song-Ee;Kim, Myeong-Hee;Lee, Chang-Kwon
    • Journal of Animal Science and Technology
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    • v.52 no.5
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    • pp.435-440
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    • 2010
  • Whey protein concentrate (WPC) is widely used to increase the nutritional and functional properties of food. In this study, the physiochemical and functionality of WPC-30 hydrolysates were examined to evaluate the possibility of application in the food industry. The WPC-30 was manufactured using ultrafiltration and spray-drying, and then hydrolyzed with proteolytic enzyme including alcalase, flavourzyme, nuetrase and protamex. Enzymatic hydrolysis had a significant influence on the physicochemical properties as evident from the increased foaming capacity, solubility. Alcalase caused highest protein hydrolysis (3.26%) and the bitterness. Foaming capacity was largest in WPC-30 hydrolysate treated with flavourzyme. Protein solubility at various levels of pH was highest in protamex-treated WPC-30 hydrolysate. However, the solubility of WPC-30 hydrolysates was significantly improved in alkaline condition than in acidic and neutral conditions. The study revealed that spray dried enzyme modified WPC can be used in various functional food.

The Anti-tumor Effect of Polysaccharide from the Leaves of Panax Ginseng C.A. Meyer(MB40) in a Murine Squamous Cell Carcinoma Model (편평세포암 동물 모델에서 고려인삼잎-다당체(MB40)의 항암치료효과)

  • Joo, Eun-Jung;Choi, Jun;Chung, Eun-Jae;Hong, Seok-Jin;Cho, Jae-Gu;Baek, Seung-Kuk;Woo, Jeong-Soo;Jung, Kwang-Yoon;Kwon, Soon-Young
    • Korean Journal of Head & Neck Oncology
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    • v.25 no.1
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    • pp.3-7
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    • 2009
  • Background and Objectives : Panax ginseng C.A. Meyer is a medical plant that has been widely utilized as a tonic and nutritional agent since ancient times in Korea. Ginseng has anti-metastatic property of cancer and immunomodulating activity. The novel acidic polysaccharide compound(MB40) was isolated from the leaves of Panax ginseng C.A. Meyer. To determine immunomodulating activities of MB40, we evaluate anti-cancer and anti-metastatic effects of MB40 in tumor bearing immune competent mice. Material and Methods : C3H mice were divided into three equal groups(Cisplatin treatment group, MB40 treat-ment group, Cisplatin and MB40 treatment group) and were transplanted SCC(Squamous Cell Carcinoma) cells(2${\times}$106) to the lateral side of abdomen. From day 4 after transplantation, MB40 was administrated at dose of 10mg/kg, respectively, every other day by intratumoral injection. Cisplatin was systemically administrated at doses of 1mg/kg, respectively, every week by intraperitoneal injection. Results : 5 days after administration, tumors can be palpated in every mice group. After 13 days of administration, the mice group to which MB40 were administrated exhibited reduction in tumor size respectively, compared to cisplatin group. Overall status of mice such as body weight and activity were superior in MB40 group than cisplatin group. Conclusion : The result of this study indicates MB40 may have significant therapeutic effect and decreases complications induced by systemic chemotheraphy. MB40 may be developed as a novel and potent immunotropics to improve the cell immune system and anti-cancer drug for the treatment of cancer patients in head and neck squamous cell carcinoma.

Studies on the Acid Tolerance of Acetobacter sp. Isolated from Persimmon Vinegar (감식초로부터 분리한 Acetobacter sp.의 내산성에 관한 연구)

  • Sim, Kyu-Chang;Lee, Kap-Sang;Kim, Dong-Han;Ryu, Il-Hwan;Lee, Jung-Sung
    • Korean Journal of Food Science and Technology
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    • v.33 no.5
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    • pp.574-581
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    • 2001
  • The microbial properties and acid tolerance of the three kinds of Acetobacter sp. isolated from persimmon vinegar were investigated. Acid tolerance was also evaluated. Acetobacter sp. were gram negative, short rod, nonspore forming and motile. They reacted positively catalase, methyl red, oxidation fermentation, Voges-Proskauer and nitrate reduction tests and negative to hydrogen sulfide test and ONPG. Acetobacter sp. showed normal growth curve in Carr broth and there was no significant difference between isolates and (standard on) typical strains such as Acetobacter aceti (KCTC1010), Acetobacter liquefaciens (KCTC2804), Acetobacter diazotrophicus (KCTC 2859). Optimum temperature and initial ethanol concentration in incubation were $30^{\circ}C$ and 6%, respectively. Growth and acid production of Acetobacter sp. were suppressed by the concentration of above 4% acetic acid. The amount of $Mg^{++}$ release from Acetobacter sp. cells in medium was increased by acetic acid, and almost in the concentration of 6% acetic acid. Glycolysis by Acetobacter sp. had optimal pH about 6.0 to 7.0 and more stable in acidic condition than in alkalic. The $H^+-ATPase$ of Acetobacter sp. S-1 and S-3 showed a maximal activity between pH values of approximately 5.5 to 7.5 and 6.0 to 7.5, respectively.

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