• Korean Journal of Medicinal Crop Science
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• v.11 no.5
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• pp.358-363
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• 2003

ScopoIamine and hyoscyamine which belong to tropane alkaloids are the pharmaceutically valuable anticholinergic drugs. In order to increase the productivities, the effects of elicitation were investigated during hairy root cultures of Scopolia. parviflora. Biotic elicitors originated from 3 fungi and 1 yeast were prepared as homogenate and supernatant and added to 3-week-old cultures. Both of homogenate and supernatant of Candida albicans elicitors increased the scopolamine production. The production of hyoscyamine was enhanced by homogenate of Fusarium solani and supernatant of C. albicans. Most of the other fungal elicitors were also improved on the tropane alkaloid production compared to non-treatment. Among the elicitors tested, C. albicans was proved the optimal biotic elicitor on tropane alkaloids production. These results will be served mass production of tropane alkaloids by large-scale production.

• Journal of Haehwa Medicine
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• v.20 no.1
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• pp.91-104
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• 2011

Background : Although chronic non-bacterial prostatitis is increasing, it is hard to treat effectively. In western medicine, antimicrobials drug, ${\alpha}$-adreno-ceptor antagonists, anti-inflammatory drugs, tricyclic antidepressants and anticholinergic agents are used commonly, but chronic prostatitis/chronic pelvic pain syndromes is confusing and frustrating for urologist. IDS(Indongsoyeom-bang) is used in treatment of chronic prostatitis/chronic pelvic pain syndromes. And it is reported that GLS(Gleditsiae spina) and TOF(Toosendan fructus) components of IDS have significant effect on protection of the glandular epithelial cells. Objective : In this study was conducted to investigate the therapeutic effects and action machanism of IDS in the rat model of non-bacterial prostatitis induced by castration and testosterone treatment. Methods : We observed six experimental objects of normal group, control group, testosterone group, and IDS 50 mg/kg, 200mg/kg, 400mg/kg group. Rats were treated with 17 ${\beta}$-estradiol after castration for induction of experimental non-bacterial prostatitis, which is similar to human chronic prostatitis in histophatological profiles. IDS and testosterone were administered as an experimental specimen and a positive control, respectively. The prostates were evaluated by histological parameters including the epithelial score and epithelio-stromal ratio for glandular damage. Also, the prostates were observed by Hematological alterations of WBC, RBC, hemoglobin and platelet. Results : While prostates of control rats revealed severe acinar gland atrophy and stromal proliferation, the rats treated with IDS-50 showed a diminished range of the tissue damage. Epithelial score was improved in IDS than that of the control. The epithelio-stromal ratio was lower in IDS when compared to that of the control. Also, the examination of bloods were not observed hematological change. Conclusion : These finding suggests that IDS may protects the glandular epithelial cells. We concluded that IDS could be a useful remedy agent for treating chronic non-bacterial prostatitis.

• Journal of Haehwa Medicine
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• v.19 no.2
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• pp.57-64
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• 2011

Parkinson's disease is a degenerative disease of a cranial nerve and has a main symptoms of irregular movement of muscle, stiffening, trembling which occurred by about 1% of population in the age of over 65. Moreover, the and prevalence rate and attack rate are soaring according to increase of elderly population. However, allopathy and surgery were done through dopamine and anticholinergic medicine for treatment but it developed a lot of complications due to medicine and progress since it makes slow progress or can't stop the treatment. Hereupon, I report that there is a case on one of the patients Young Jin Oriental Medical Clinic. The patient who is in state of treatment termination who doesn't need any further remedy and no worsening of symptoms after conduction of therapies of dialectic and 5 upright life cure regulations. 5 upright life cure regulations means five practive way for improvement of nature healing power. Upon undertaking the 5 upright life cure regulations, there were found significant results in such tests as Unified Parkinson Disease Rating Scale (UPDRS), Hoehn & Yahr Staging Scale, and Activity of Daily Living (ADL), and the ingestion of Benztropine 1mg and Requip 0.25mg was decreased from 3 times to 0 times. The study offers objective clinical data on Oriental Medicine treatment for Parkinson's disease which is one of representative neuro-degenerative diseases and thus broadens the application range of Oriental Medical treatment and presents the fundamental data on the clinical research on Parkinson's disease by adopting evidence-based medicine (EBM).

• Korean Journal of Biological Psychiatry
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• v.21 no.2
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• pp.49-56
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• 2014

Objectives Previous literature on the prescription change among patients with schizophrenia mainly focused on antipsychotics. This study investigated chronological change in the patterns of discharge medication among inpatients with schizophrenia at a psychiatric inpatient unit of a university-affiliated hospital. Methods All admission records at a psychiatric unit of Hanyang University Guri Hospital with discharge diagnosis of schizophrenia during two different five-year time frames (1996-2000 and 2006-2010) were reviewed including the demographic and clinical data and discharge medications. The data were gathered from a total of 207 patients (95 in 1990s and 112 in 2000s). Results The frequency in use of atypical antipsychotics (p < 0.01), antidepressants (p < 0.05), beta-blockers (p < 0.01), and benzodiazepine (p < 0.01) was significantly higher in 2000s. Anticholinergic drugs were less likely used in 2000s (p < 0.01). We did not find significant differences in the equivalent dose of antipsychotic drugs, the use of mood stabilizers and cholinergic drugs between two time frames. Conclusions Increased proportion of atypical antipsychotics and decreased use of anti-parkinsonian drugs are in line with literature. Our results show that more diverse classes of psychotic medications are used for schizophrenia in recent years. It is likely that psychiatrists are becoming more conscious of negative symptoms, anxiety, and depression in the pharmacotherapy of schizophrenia as well as positive symptoms of the illness.

• Analytical Science and Technology
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• v.8 no.1
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• pp.79-84
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• 1995

Ion-selective poly(vinyl chloride) membrane electrodes for the determination of the anticholinergic drug alverine in pure substances is described. Ion-pair complex of alverine with anionic counter ion acid red 97 is investigated as electroactive compound for the electrode membrane. On the optimal composition of membrane, its slope was 55.35mV/decade, relative standard deviation was 0.61 and lower limit of linear range was $1.0{\times}10^{-5}M$. The observed potentiometric selectivity coefficient was -2.625 toward methylephedrine and -2.216 toward histidine. We can got the stable potential at pH 7.0~4.0. Response time was 20~30 seconds for solutions${\leq}10^{-4}M$, about 10 seconds for solutions ${\geq}10^{-4}M$ of these compounds.

• Clinical and Experimental Pediatrics
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• v.51 no.11
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• pp.1140-1146
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• 2008

Nocturnal enuresis is a heterogeneous disorder with various underlying pathophysiological mechanisms and causes a mismatch between the nocturnal bladder capacity and the amount of urine produced during sleep at night. It is associated with a simultaneous failure of conscious arousal in response to the sensation of bladder fullness. Generally, a complete history and physical examination, with a specific focus on the genitourinary, gastrointestinal, and neurologic systems, is sufficient to evaluate a patient with enuresis. The therapeutic focus is directed toward a differential approach based on the underlying mechanism and toward combination therapies such as alarm devices and desmopressin as well as anticholinergic agents and desmopressin. Children with increased nocturnal urine production usually have a good response to desmopressin therapy. Patients with a small bladder generally show a poor response to desmopressin treatment, but they would benefit more from combination therapy with enuretic alarm, urotherapy, and antimuscarinic agents in addition to desmopressin. Different types of bladder dysfunction, which result in a small nocturnal bladder capacity, probably contribute significantly to the pathogenesis of nocturnal enuresis, particularly in those with treatment failure and refractory symptoms. Because different clinical subgroups may show different responses to treatment, it is necessary to distinguish these subgroups before a decision on the specific treatment protocol can be made.

• The Korean Journal of Pain
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• v.10 no.2
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• pp.166-169
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• 1997

Background: We have noted a high incidence of vasovagal episodes associated with use of interscalene block(ISB) for shoulder arthroscopy in the sitting position. The purpose of this retrospective study is to alert the possibility of potentially dangerous vasovagal events, describe the characteristics of this problem, and propose therapeutic devices. Methods: Results 62 patients who underwent shoulder arthroscopy in the sitting position with ISB were retrospectively analyzed. Group 1, 10 patients experienced vasovagal events characterized by sudden hypotension and bradycardia. Remaining 52 patients, Group 2, did not experience these symptoms. All patient charts were reviewed for age, sex, side of surgery, premedication, preoperative fluid and intraoperative medications. Perioperative hemodynamic changes were also compared between the two groups. Results: Vasovagal events experienced in 16% of patients(10/62) and occurred $39{\pm}18$ min after sitting position and $22{\pm}18$ min after start of operation. Number of patients who receiving anticholinergics for premedication were significantly lower in Group 1 than Group 2(2/10 vs. 28/52, p<0.05). Conclusions: Bezold-parish reflex is a potential mechanism for sudden hypotension and bradycardia which can occur during shoulder arthroscopy in sitting position. Therefore anticholinergic pretreatment and meticulous monitoring during operation are recommended to prevent B-J reflex.

• YAKHAK HOEJI
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• v.32 no.2
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• pp.101-111
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• 1988

$[^3H]$ Quinuclidinyl benzilate(QNB) binding assays were performed in the dog ventricular sarcolemma fraction enriched approx. 32-fold in sarcolemma compared to the starting homogenate to elucidate the effect of antihistaminics on cardiac muscarinic receptor. Chlorpheniramine(CHP) inhibited specific binding of $[^3H]$QNB and delayed the equilibrium binding. The rate constants at $37^{\circ}C$ for formation and dissociation of the QNB receptor complex were $0.38{\times}10^9\;M^{-1}$ and $1.6{\times}10^{-2}\;min^{-1}$, respectively. The mean value for the dissociation constant from the pairs of the rate constants was 43. 2 pM and this value was similar to the value(44.8pM) determined from Scatchard analysis. CHP decreased association rate constant, indicating increase in $K_D$ value. Decrease in affinity without affecting the binding site concentration$(B_{max})$ for $[^3H]$QNB binding by CHP was also demonstrated by Scatchard analysis. $K_i$ values for $H_i$-blockers that inhibited specific $[^3H]$QNB binding were $0.02{\sim}4.8{\mu}M$. Cimetidine with $K_i$ value of $230{\mu}M$, however, was ineffective in displacing $[^3H]$QNB binding at concentration of $50{\mu}M$. The Hill coefficient for $H_1$-blockers were about one. The results indicate that $H_1$-antihistaminics inhibit $[^3H]$ QNB binding by interaction with myocardiac muscarinic cholinergic receptor and anticholinergic side effects of these drugs are mainly due to this receptor blocking mechanism.

• Archives of Pharmacal Research
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• v.24 no.3
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• pp.219-223
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• 2001

Nasal absorption of procyclidine, a synthetic anticholinergic compound, was investigated in Wistar rats and Beagle dogs. The dosing solution was prepared by dissolving$^{14}C$-procyclidme in 50% ethanolic saline. The dosing solution was administered intravenously and intranasally to rats at a dose of 0.6 mg/kg (i.e., $60{\mu}$l/kg in the form of a 1% w/v solution), and intravenously, orally and intranasally to doss at a dose of 0.3 mg/kg(i.e., $6{mu}$l/kg in the form of a 5% w/v solution). Blood samples were taken from an artery of the animals through the catheter for periods of 1200 (for rats) and 1440 min (for dogs), and the radioactivity in the samples was determined by liquid scintillation counting. The nasal bioavailability of Procyclidine in rats and dogs, based on the radioactivity was calculated to be 81.1 and 98.6% respectively. In both rats and dogs, the plasma profiles of procyclidine following nasal administration were very close to those following intravenous administration, leading to nearly superimposable profiles between the two protocols. In dogs, nasal administration resulted in significantly higher plasma concentrations during the first 30 min period compared to oral administration, suggesting the superiority of the nasal route over the oral route in terms of a prompt expression of the pharmacological effect of the drug. The results obtained in this study indicate that procyclidine is rapidly and nearly completely absorbed via the nasal route. In conclusion, nasal administration represents a viable alternative to intravenous administration in the case of procyclidine.

• Mass Spectrometry Letters
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• v.12 no.4
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• pp.200-205
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• 2021

Polynemoraline C, a pyridocoumarin alkaloid, exhibits anticholinergic, anti-inflammatory, antitumor, and antimicrobial activities. A sensitive analytical method of polynemoraline C in mouse plasma was developed and validated using liquid chromatography-tandem mass spectrometry (LC-MS/MS). Polynemoraline C and ¹³C-caffeine (internal standard) in mouse plasma were extracted using a liquid-liquid extraction method coupled with ethyl acetate. This extraction method resulted in high and reproducible extraction recovery in the range of 73.49%-77.31% with no interfering peaks around the peak retention time of polynemoraline C and ¹³C-caffeine. The standard calibration curves for polynemoraline C were linear over the range of 0.5-200 ng/mL with r² > 0.985. The accuracy, precision, and the stability of the data were within acceptable limits on the FDA guideline. After intravenous and oral administration of polynemoraline C at doses of 5 and 30 mg/kg, respectively, the present method was successfully applied to the pharmacokinetic study of polynemoraline C. Polynemoraline C in mouse plasma showed a multi-exponential elimination pattern with a high volume of distribution values. This compound's absolute oral bioavailability was found to be 17.0%. Polynemoraline C's newly developed LC-MS/MS method can be used for further studies on the efficacy, toxicity, and biopharmaceutics of polynemoraline C, as well as its pharmacokinetic studies.