• The Korean Journal of Pharmacology
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• v.19 no.2
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• pp.17-24
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• 1983

Buxus leaves(Buxus microphylla var. koreana Nakai) have been used as a folk medicine in treating woman's disease. The chemical constituents, which have teen identified from Buxus sempervirens L. in Europe, are so far known in isolation of buxus alkaloids, cyclobuxine, buxamine, norbuxamine and buxaminol. But But any study on the pharmacological action of Buxus microphylla var. koreana Nakai has not yet teen rallied out, however, active substances have not been identified. As an attempt to isolate the biologically active substances from this plant, the examination of chemical constituents was undertaken. In the experiment, the crystalline component$(C_{10}H_8O_4)$ obtained from Buxus microphylla var. koreana Nakai was identified as a 6-methoxy, 7-hydroxy coumarin by chemical and physical methods. We named this crystal buxuletin. Therefore, we intended to screen the pharmacological action of buxuletin, especially, its diuretic effects in rabbits. Buxuletin was intraveneously injected to the rabbit in the dose of 20 mg/kg, 10 mg/kg and 5 mg/kg. The variations of urine volume and minerals $(Na^+,\;K^+\;and\;Cl^-)$ in urine were measured at an interval of 15 minutes for 4 hours after the treatment of buxuletin. The observed results are as follows: 1) With the administration of buxuletin (20 mg/kg, 10 mg/kg), the remarkable increment of the excreted urine volume was observed during the relatively long period. Excretion rates of urinary minerals $(Na^+,\;K^+\;and\;Cl^-)$ were also increased. 2) In a dose of 5 mg/kg, the slight increment on the diuretic actions of rabbits was observed. From the above results, authors name this crystal buxuletin and buxuletin shows the diuretic action.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.21
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• pp.9049-9058
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• 2014

Casticin (3', 5-dihydroxy-3, 4', 6, 7-tetramethoxyflavone) is an active compound isolated from roots, stems, leaves, fruits and seeds of a variety of plants. It is well known for its pharmacological properties and has been utilized as an anti-hyperprolactinemia, anti-tumor, anti-inflammatory, neuroprotetective, analgesic and immunomodulatory agent. Recently, the anticancer activity of casticin has been extensively investigated. The resulkts showed that it exerts protective potential by targeting apoptosis, considered important for cancer therapies. In this article, our aim was to review the pharmacological and therapeutic applications of casticin with specific emphasis on its anticancer functions and related molecular mechanisms. Chemotherapeutic effects are dependent on multiple molecular pathways, which may provide a new perspective of casticin as a candidate anti-neoplastic drug. This review suggests that additional studies and preclinical trials are required to determine specific intracellular sites of action and derivative targets in order to fully understand the mechanisms of its antitumor activity and validate this compound as a medicinal agent for the prevention and treatment of various cancers.

• Biomolecules & Therapeutics
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• v.24 no.5
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• pp.536-542
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• 2016

Shuangdan oral liquid (SDO) containing radix Salviae miltiorrhizae (Chinese name Danshen) and cortex moutan (Chinese name Mudanpi) is a traditional Chinese medicine using for treating vascular diseases. Danshensu (DSS) is a main effective monomer composition derived from radix Salviae miltiorrhizae and paeonol (Pae) from cortex moutan. Although the two herbs are widely used in traditional Chinese medicine, the pharmacological functions of their active compositions were not reported. Therefore, the research of DSS and Pae in mechanisms and pharmacodynamics interaction can provide scientific evidence to support clinical application. The diabetic nephropathy (DN) rats which were induced by streptozotocin (STZ) were treated with SDO, DSS, Pae, and DSS+Pae for eight weeks. The positive effects on DN animal models were investigated by detection of physiological and biochemical indexes and oxidative stress markers, within five treatments: SDO, DSS, Pae, DSS+Pae and insulin group. Compared with the model group, the DSS+Pae group improved the renal function, blood lipid metabolism and blood viscosity, increased the vitality of T-SOD or T-AOC and decreased the level of MDA or NO after the treatment. The study was successfully showed that the DSS+Pae group could delay the process of DN, especially in the renal injury part of histopathology changes. Our results suggest that the co-administration of DSS and Pae significantly may play a protective role in DN rats through decreasing the oxidative stress and improving the blood lipid metabolism mechanisms.

• The Research Journal of the Costume Culture
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• v.14 no.2
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• pp.260-270
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• 2006

In this research, the curly dock was used in the process of dyeing for fabrics of the inner wear & the patient wear. Since the curly dock has a pharmacological effect on dermatosis, this study focused on the variety of color and functions of the inner wear fabrics & patient wear fabrics to make the best use of the pharmacological effect of curly dock. With regards to giving a variety of colors and functions in the inner wear, patient wear fabrics, the curly dock dye was used in each treatment conditions on the cotton & silk fabrics. After dyeing, the dyeability, color change, light fastness, washing fastness, perspiration fastness, antibiosis, far infrared emissivity and emission power were evaluated. The evaluation results are as follows; The dyeablity increased from repeated dyeing and, by using the mordant, variety of colors such as skin, mustard, greyish-brown and dark earth colors were conformed to the naked eye. Fe mordant was better than Al on the lightfastness and the washing fastness. The repeated dyeing was found out to have less effect on neither lightfastness nor washing fastness. Both silk and cotton fabrics were graded $3{\sim}4$, since their degree of degradation appeared to be the same in alkali perspiration and acidic perspiration. In the case of silk fabrics mordanted by Al, the rate of declining in both Staphylococcus aureus ATCC 6538 and Klebsiella pneumonia ATCC 4352 were 99.9%. In addition, the antibiosis was enhanced when the mordant was used. The far infrared was 86.6% of emissivity, $3.34{\times}10^2\;W/m^2{\cdot}{\mu}m$ emission power.

• KSBB Journal
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• v.27 no.6
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• pp.367-374
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• 2012

Cigarette smoking (SM) is considered to be well known environmental toxin which contributes to the onset of various diseases. SM cause direct lungs damage, activate lungs inflammatory responses, and in some cases leads to the development of lung cancer. Cytokines in injured starfish (Asterina pectinifera) is the potential changes in its expression during the regeneration process. Especially, expression of TGF-${\beta}1$ has increased in arm cut starfish extract after eight days. Also, starfish including saponin like the ginseng. Saponin is widely used in the world because of some effective pharmacological activities. Therefore, the current study was designed to elucidate the pharmacological activities of starfish extract against cigarette smoking induced damage in cell line and pulmonary tissue. We investigate that the effect of eight days starfish extract after arm cut (8d) and intact starfish extract on cell line and mouse lung injury by SM. In cell proliferation analysis, although cigarette smoking extract (CSE) was co-treated, the higher proliferation ability is shown in 8d treatment than intact starfish extract. 8d and intact starfish extract was directly transported to pulmonary cells through respiratory organ by nebulizer inhalation. In this case of cigarette smoking, the pulmonary structure was damaged and functions become abnormal. However, 8d treated groups showed similar with the control group compared with SM group. Among them, 8d was proved to be more effective than intact starfish extract. These results demonstrate that 8d could more protect pulmonary structure and function than intact starfish extract against cigarette smoking by ginseng like saponin and regulation of inflammatory cytokines.

• Korean Journal of Psychosomatic Medicine
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• v.21 no.2
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• pp.81-92
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• 2013

Newer antidepressants are commonly used in clinical practice to treat psychiatric disorder and psychosomatic disorder including chronic pain syndrome, fibromyalgia, headache. However there are many unexpected adverse effects of these drugs such as nausea and vomiting, weight gain, sexual dysfunction. These are 3 most well-recognized common adverse effects of newer antidepressant and are most common causes of treatment failure. I reviewed mechanisms, epidemiology, and pharmacological management of these adverse effects of newer antidepressants. In this paper, newer antidepressants include selective serotonin reuptake inhibitor(fluoxetine, fluvoxamine, citalopram, escitalopram, sertraline, paroxetine), serotonin norepinephrine reuptake inhibitor(venlafaxine, duloxetine), norepinephrine and dopamine reuptake inhibitor(bupropion), noradrenergic and specific serotonergic antidepressant(mirtazapine), and reversible inhibitor of MAO-A(moclobemide). I suggest that psychiatrists and clinicians in the psychosomatic field should know mechanisms, epidemiology, and management of these common and well-recognized adverse effects of newer antidepressants. Therefore it will be helpful to recognize easily and treat well for patients with psychiatric disorder and psychosomatic disorder using newer antidepressants.

• Journal of Society of Preventive Korean Medicine
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• v.22 no.2
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• pp.77-107
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• 2018

Objectives : In present study, therefore, possible beneficial pharmacological activities of standard potato protein extracts (SPE) were observed on the mild diabetic obese mice. Methods : After end of 12 weeks of continuous oral administrations of three different dosages of SPE 400, 200 and 100 mg/kg, or metformin 250 mg/kg, analyzed the hepatoprotective, hypolipidemic, hypoglycemic, nephroprotective and anti-obesity effects, separately. In addition, liver antioxidant defense systems were additionally measured with lipid metabolism-related genes expressions and hepatic glucose-regulating enzyme activities for action mechanism. Results : All of diabetes and related complications including obesity were significantly inhibited by treatment of SPE 400, 200 and 100 mg/kg, dose-dependently, and they also dramatically normalized the hepatic lipid peroxidation and depletion of liver endogenous antioxidant defense system, the changes of the hepatic glucose-regulating enzyme activities, also changes of the lipid metabolism-related genes expressions including hepatic $AMPK{\alpha}1$ and $AMPK{\alpha}2$ mRNA expressions, dose-dependently. Especially, SPE 200 mg/kg constantly showed favorable inhibitory activities against type II diabetes and related complications as comparable to those of metformin 250 mg/kg in HFD mice, respectively. Conclusions : The present work demonstrated that SPE 400, 200 and 100 mg/kg showed favorable anti-diabetic and related complications including obesity refinement activities in HFD mice, through AMPK upregulation mediated hepatic glucose enzyme activity and lipid metabolism-related genes expression, antioxidant defense system and pancreatic lipid digestion enzyme modulatory activities.

• Toxicological Research
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• v.22 no.4
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• pp.431-438
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• 2006

The object of this study was to obtain acute toxicity information (single oral dose toxicity) of lyophilized water extract of Puerariae Radix (PR) in both male and female mice. In order to investigate the 50% lethal dose $(LD_{50})$, approximate lethal dosage (ALD), test substances were once orally administered to female and male ICR mice at dose levels of 2000 and 0 (control) mg/kg (body wt.) according to the recommendation of KFDA Guidelines [2005-60, 2005]. The mortality and body weight changes, clinical signs and gross observation were monitored during 14 days after dosing. Organ weight and histopathology of 12 principal organs were measured. As the results, we could not find any mortality, clinical signs, body weight changes and gross findings except for PR extracts unrelated sporadic findings. In addition, no abnormal changes related PR extracts treatment on the organ weight and histopathology of principal organs were detected except for some sporadic findings including hyperplasia of lymphoid follicles in the popliteal lymph nodes and spleen as pharmacological effects of PR extracts. The results obtained in this study suggest that the PR extracts does not cause any toxicological signs except for pharmacological effects of enhancement of Immune system. The $LD_{50}$ and ALD of PR extracts in both female and male mice were considered as over 2000 mg/kg because no mortalities were detected up to 2000mg/kg that was the highest dose recommended by KFDA and Organization for Economic Co-Operation and Development.

• Molecules and Cells
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• v.37 no.8
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• pp.585-591
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• 2014

The ${\beta}_2$ adrenergic receptor (ADRB2) is a G protein-coupled transmembrane receptor expressed in the human respiratory tract and widely recognized as a pharmacological target for treatments of asthma and chronic obstructive pulmonary disorder (COPD). Although a number of ADRB2 agonists have been developed for use in asthma therapy, indacaterol is the only ultra-long-acting inhaled ${\beta}_2$-agonist (LABA) approved by the FDA for relieving the symptoms in COPD patients. The precise molecular mechanism underlying the pharmacological effect of indacaterol, however, remains unclear. Here, we show that ${\beta}$-arrestin-2 mediates the internalization of ADRB2 following indacaterol treatment. Moreover, we demonstrate that indacaterol significantly inhibits tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$)-induced NF-${\kappa}B$ activity by reducing levels of both phosphorylated-IKK and -$I{\kappa}B{\alpha}$, thereby decreasing NF-${\kappa}B$ nuclear translocation and the expression of MMP-9, an NF-${\kappa}B$ target gene. Subsequently, we show that indacaterol significantly inhibits TNF-${\alpha}$/NF-${\kappa}B$-induced cell invasiveness and migration in a human cancer cell line. In conclusion, we propose that indacaterol may inhibit NF-${\kappa}B$ activity in a ${\beta}$-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD patients.

• Journal of Pharmaceutical Investigation
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• v.25 no.3
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• pp.177-184
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• 1995

In order to formulate an aqueous topical preparation of epidermal growth factor(EGF) for the treatment of open wound and bum, the stability of EGF in aqueous vehicles containing various stabilizers was evaluated and the pharmacological activity of gel preparations formulated with poloxamer 407 was determined with wound model. Various additives, which are known as potent stabilizers for proteins and polypeptides so far, were used to increase the stability of EGF in aqueous vehicles. The contents of EGF in the vehicles containing stabilizers were determined with an HPLC method after the storage at $37^{\circ}C$. EGF was more stable in ultrapure water than RO water or saline. All the additives studied resulted in deleterious effects on EGF stability. Therefore, it was speculated that any additives or impurities in the vehicle made EGF unstable. However, nitrogen purge of solution increased the stability of EGF in aqueous vehicles. The aqueous topical preparations of EGF were formulated with poloxamer 407 as a gel base in saline. Gelatin or amastatin was employed as a protease inhibitor. The pharmacological effect of EGF gel was studied with open wound model in mice. EGF preparations, made of oleaginous base or poloxamer gel base, showed significant healing effect compared to the control group(p<0.05). The addition of protease inhibitor in poloxamer 407 gel resulted in significant healing effect compared to the gel without it(p<0.05). Body weights of mice treated with EGF preparation were increased at the first day after the formation of open wound, while those of the control group were decreased. The EGF gel made of poloxamer 407 containing a pretense inhibitor would be a promising aqueous topical preparation for EGF.