• Title/Summary/Keyword: Scopolamine

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Optimal Culture Conditions and XAD Resin on Tropane Alkaloid production in Scopolia parviflora Hairy Root Cultures (미치광이풀 모상근의 배양조건 구명 및 XAD Resin 처리에 의한 Tropane Alkaloid 생산)

  • 정희영;강민정;강영민;윤대진;박정동;정영관;최명석
    • KSBB Journal
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    • v.17 no.6
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    • pp.525-530
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    • 2002
  • The optimum culture conditions for tropane alkaloid production in hairy root cultures of Korea native Scopolia paviflora Nak. were investigated. Hairy root was induced from the rhizome of the mother plant on B5 medium containing 1.0 mg/L IBA. Among the culture media examined, 1/2 B5 medium was the best for tropane alkaloid production, whereas the growth of hairy root increased in SH medium. The best result on the growth of hairy root was obtained in 1.0 mg/L NAA, and tropane alkaloid production was obtained in plant growth regulator-free medium. Of the carbone sources tested, 3% sucrose promoted the growth of hairy root, whereas 5% sucrose increased tropane alkaloid production. Optimum inoculum densities for root growth and tropane alkaloid production were 0.5 g and 1 g, respectively. The addition of XAD resins (1 % w/v) to hairy root cultures led to increases in tropans alkaloid production, and the release of alkaloid into the medium and its adsorption by the resin accounted for about 50 to 80% of total production. It is concluded that optimized culture conditions and the addition of XAD resins could be used in the development of a bioprocess for tropane alkaloid production in hairy root cultures of S. paviflora Nak.

Black ginseng-enriched Chong-Myung-Tang extracts improve spatial learning behavior in rats and elicit anti-inflammatory effects in vitro

  • Saba, Evelyn;Jeong, Da-Hye;Roh, Seong-Soo;Kim, Seung-Hyung;Kim, Sung-Dae;Kim, Hyun-Kyoung;Rhee, Man-Hee
    • Journal of Ginseng Research
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    • v.41 no.2
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    • pp.151-158
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    • 2017
  • Background: Chong-Myung-Tang (CMT) extract is widely used in Korea as a traditional herbal tonic for increasing memory capacity in high-school students and also for numerous body ailments since centuries. The use of CMT to improve the learning capacity has been attributed to various plant constituents, especially black ginseng, in it. Therefore, in this study, we have first investigated whether black ginseng-enriched CMT extracts affected spatial learning using the Morris water maze (MWM) test. Their molecular mechanism of action underlying improvement of learning and memory was examined in vitro. Methods: We used two types of black ginseng-enriched CMT extracts, designated as CM-1 and CM-2, and evaluated their efficacy in the MWM test for spatial learning behavior and their anti-inflammatory effects in BV2 microglial cells. Results: Our results show that both black ginseng-enriched CMT extracts improved the learning behavior in scopolamine-induced impairment in the water maze test. Moreover, these extracts also inhibited nitric oxide production in BV2 cells, with significant suppression of expression of proinflammatory cytokines, especially inducible nitric oxide synthase, cyclooxygenase-2, and $interleukin-1{\beta}$. The protein expression of mitogen-activated protein kinase and nuclear $factor-{\kappa}B$ pathway factors was also diminished by black ginseng-enriched CMT extracts, indicating that it not only improves the memory impairment, but also acts a potent anti-inflammatory agent for neuroinflammatory diseases. Conclusion: Our research for the first time provides the scientific evidence that consumption of black ginseng-enriched CMT extract as a brain tonic improves memory impairment. Thus, our study results can be taken as a reference for future neurobehavioral studies.

Bioequivalence of Alpit Tablet to Algiron Tablet (Cimetropium Bromide 50 mg) (알기론 정(브롬화 시메트로피움 50 mg)에 대한 알피트 정의 생물학적 동등성)

  • Cho, Hea-Young;Moon, Jai-Dong;Lee, Yong-Bok
    • Journal of Pharmaceutical Investigation
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    • v.32 no.1
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    • pp.47-54
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    • 2002
  • Cimetropium bromide, a quaternary ammonium compound which is chemically related to scopolamine, exhibits its antispasmodic activity by competing with acetylcholine for the muscarinic receptors of the smooth muscle of gastrointestinal tract. The drug has been used for the treatment of various disorders involving spasms of the musculature of the gastrointestinal, biliary and genitourinary tracts. The purpose of the present study was to evaluate the bioequivalence of two cimetropium bromide tablets, $Algiron^{TM}$ (Boehringer Ingelheim Korea Ltd.) and $Alpit^{TM}$ (Hana Pharmaceutical Co., Ltd.), according to the prior and revised guidelines of Korea Food and Drug Administration (KFDA). The cimetropium bromide release from the two cimetropium bromide tablets in vitro was tested using KP VII Apparatus II method with various different kinds of dissolution media (pH 1.2, 4.0, 6.8 buffer solution and water). Twenty normal male volunteers, $25.25{\pm}2.10$ years in age and $65.76{\pm}6.39$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After three tablets containing 50 mg of cimetropium bromide per tablet were orally administered, blood was taken at predetermined time intervals and the concentrations of cimetropium bromide in serum were determined using HPLC method with UV detector. The dissolution profiles of two cimetropium bromide tablets were very similar at all dissolution media. Besides, the pharmacokinetic parameters such as $AUC_t,\;C_{max}\;and\;T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using non-transformed and logarithmically transformed $AUC_t\;and\;C_{max}$. The results showed that the differences in $AUC_t,\;C_{max}\;and\;T_{max}$ between two tablets based on the $Algiron^{TM}$ were 2.19%, -5.97% and 3.49%, respectively. Minimum detectable differences $({\Delta})\;at \;{\alpha}=0.05\;and\;1-{\beta}=0.8$ were less than 20% (e.g., 13.71 %, 19.05% and 15.11% for $AUC_t,\;C_{max}\;and\;T_{max}$, respectively). The powers $(1-{\beta})\;at\;{\alpha}=0.05,\;{\Delta}=0.2\;for\;AUC_t$, $C_{max}\;and\;T_{max}$ were 97.79%, 83.22% and 95.60%, respectively. The 90% confidence intervals were within ${\pm}20%$ (e.g., $-5.84{\sim}10.21,\;-17.11{\sim}5.18\;and\;-5.35{\sim}12.33\;for\;AUC_t,\;C_{max}\;and\;T_{max}$, respectively). There were no sequence effect between two tablets in logarithmically transformed $AUC_t\;and\;C_{max}$. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log(0.8) to log(1.25) (e.g., $0.94{\sim}1.10\;and\;0.85{\sim}1.05\;for\;AUC_t\;and\;C_{max}$, respectively). Two parameters met the criteria of prior and revised KFDA guideline for bioequivalence, indicating that $Alpit^{TM}$ tablet is bioequivalent to $Algiron^{TM}$ tablet.

Drug Delivery into the Blood-Brain Barrier by Endogenous Substances-A Role of Amine and Monocarboxylic Acid Carrier Systems for the Drug Transport- (내인성물질의 수송계를 이용한 혈액-뇌관문에의 약물송달V-약물의 혈액-뇌관문 투과성에 대한 염기성 아민 및 모노카르본산 수송계의 역할-)

  • Kang, Young-Sook
    • Journal of Pharmaceutical Investigation
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    • v.20 no.4
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    • pp.223-228
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    • 1990
  • The contribution of endogenous transport systems to the blood-brain barrier (BBB) transport of basic and acidic drugs was studied by using a carotid injection technique in rats and an isolated bovine cerebrovascular disease state were compared between the normotensive rats (WKY) and stroke-prone spontaneously hypertensive rats (SHRSP) which have been well established as an animal model with pathogenic similarities to humans. Basic drugs such as eperisone, thiamine and scopolamine inhibited, in a concentration dependent manner the in vivo uptake of $[{^3}H]choline$ through BBB, whereas amino acids and acidic drugs such as salicylic acid and valproic acid did not inhibit the uptake. The uptake of $[^3H]choline$ by B-CAP increased with time and showed a remarkable temperature dependency. The uptake of $[^3H]choline$ by B-CAP showed the very similar inhibitory effects as observed in the in vivo brain uptake, and was competitively inhibited by a basic drug, eperisone. The in vivo BBB uptakes of $[^3H]acetic$ acid and $[^{14}C]salicylic$ acid were dependent on pH of the injectate and the concentration of drugs. Several acidic drugs such such as salicylic acid, benzoic acid and valproic acid inhibited the in vivo uptake of $[^3H]acetic$ acid, whereas amino acid, choline and a basic drug such as eperisone did not inhibit the uptake. The uptake of acetic acid by B-CAP was competitively inhibited by salicylic acid. The permeability surface area product (PS) through BBB for $[^3H]choline$ in SHRSP was significantly lower than that in WKY. The concentration of choline in the brain dialysate in SHRSP was about half of that in WKY, while no significant difference was observed in the plasma concentration of choline between SHRSP and WKY. No significant difference was observed in the transport of monocarboxylic acids, glucose and neutral amino acid through BBB between SHRSP and WKY. From these results, it was concluded that BBB transport system of choline contributes to the transport of basic drugs through BBB, that acidic drugs can be transported via a moncarboxylic acid BBB transport system and that the specific dysfuntion of the BBB choline transport in SHRSP was ascribed to the reduction of the maximum velocity of choline concentration in the brain interstitial fluids.

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Technical Feasibility of Quantitative Measurement of Various Degrees of Small Bowel Motility Using Cine Magnetic Resonance Imaging

  • Ji Young Choi;Jihye Yun;Subin Heo;Dong Wook Kim;Sang Hyun Choi;Jiyoung Yoon;Kyuwon Kim;Kee Wook Jung;Seung-Jae Myung
    • Korean Journal of Radiology
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    • v.24 no.11
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    • pp.1093-1101
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    • 2023
  • Objective: Cine magnetic resonance imaging (MRI) has emerged as a noninvasive method to quantitatively assess bowel motility. However, its accuracy in measuring various degrees of small bowel motility has not been extensively evaluated. We aimed to draw a quantitative small bowel motility score from cine MRI and evaluate its performance in a population with varying degrees of small bowel motility. Materials and Methods: A total of 174 participants (28.5 ± 7.6 years; 135 males) underwent a 22-second-long cine MRI sequence (2-dimensional balanced turbo-field echo; 0.5 seconds per image) approximately 5 minutes after being intravenously administered 10 mg of scopolamine-N-butyl bromide to deliberately create diverse degrees of small bowel motility. In a manually segmented area of the small bowel, motility was automatically quantified using a nonrigid registration and calculated as a quantitative motility score. The mean value (MV) of motility grades visually assessed by two radiologists was used as a reference standard. The quantitative motility score's correlation (Spearman's ρ) with the reference standard and performance (area under the receiver operating characteristics curve [AUROC], sensitivity, and specificity) for diagnosing adynamic small bowel (MV of 1) were evaluated. Results: For the MV of the quantitative motility scores at grades 1, 1.5, 2, 2.5, and 3, the mean ± standard deviation values were 0.019 ± 0.003, 0.027 ± 0.010, 0.033 ± 0.008, 0.032 ± 0.009, and 0.043 ± 0.013, respectively. There was a significant positive correlation between the quantitative motility score and the MV (ρ = 0.531, P < 0.001). The AUROC value for diagnosing a MV of 1 (i.e., adynamic small bowel) was 0.953 (95% confidence interval, 0.923-0.984). Moreover, the optimal cutoff for the quantitative motility score was 0.024, with a sensitivity of 100% (15/15) and specificity of 89.9% (143/159). Conclusion: The quantitative motility score calculated from a cine MRI enables diagnosis of an adynamic small bowel, and potentially discerns various degrees of bowel motility.