• Biomolecules & Therapeutics
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• v.14 no.3
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• pp.171-177
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• 2006

Gastritis and gastric ulcer were known to be induced by gastic acid, stress, ethanol, Helicobacter pylori and free radical, etc. This study was performed for the development of a new drug or nutraceutical from medicinal plants or natural products with anti-gastritis, anti-ulcerative and gastroprotective activities. The water extract of Scutellaria baicalensis was exhibited potent inhibition in HCl ethanol-induced gastric lesion, acetic acid-induced and Shay ulcers, indicating the effects on gastric lesion and ulcer in rats. The water extract of Scutellaria baicalensis significantly inhibited HCl ethanol-induced gastric lesions at the oral dose of 300, 500 mg/kg. In pylorus ligated rats, the treatments of the water extract from Scutellaria baicalensis showed decrease in the volume of gastric secretion and acid output and increase pH at oral dose of 300, 500 mg/kg. And significantly reduced acetic acid-induced ulcer at the oral dose of 500 mg/kg for 12 days. In this study, we have found that the water extract from Scutellaria baicalensis had significant improvement in acute gastritis and ulcer at the dose of 300, 500 mg/kg and in chronic gastritis and ulcer at the dose of 500 mg/kg. Also we evaluated the antibacterial activity against Helicobacter pylori treated with Scutellaria baicalensis. Scutellaria baicalensis had a equivalent antibacterial activity with ampicilin against H. pylori at the dose of $100\;{\mu}/ml$. In histological examination, the water extract of Scutellaria baicalensis drastically restored gastric damages induced by HCl ethanol solution, pylorus- ligature and acetic acid. Therefore, we may use the water extract from Scutellaria baicalensis as antigastritic and antiulcerative agent for the purpose of the improvement or treatment of gastritis and gastric ulcer.

• Journal of the Korean Applied Science and Technology
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• v.30 no.2
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• pp.215-224
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• 2013

Recently, many cosmetic researchers have been focused on the development of high functional cosmetics including anti-wrinkle and whitening. In these studies, they couldn't afford to pay a deep attention to stable encapsulations for unstable materials and efficient drug deliveries for them. Particularly, in order to show a degree of instant effects as cosmetics, they can't also ignore moisturizing effect enough to satisfy customers just after applying and its maintenance by improving the function of skin barrier as well as above two effects. Therefore, skin analogue systems have attracted considerable attention in the view of structural and compositional similarity to intercellular membrane in stratum corneum. And, some models for skin analogue composition were developed to improve the function of skin barrier, stably encapsulate unstable materials such as retinol, vitamin B, C, E, etc., and control their skin penetration in order to show good effects as cosmetics. In this study, we suggest the new skin analogue model having the compositional similarity as well as conventional structural ones. Our skin analogue membrane(SAM) is mainly composed of ceramide/ cholesterol/phosphatidylcholin/fatty acids and its structural defects are compensated by including cholesterol amphiphile and controlling the ratio of ceramide/cholesterol. It was possible to confirm the formation of skin analogue membrane having highly-densed multilamella structure and compare them according to the change of each ratio with a polarized microscope, X-ray diffraction. More detaily, we observed their structures with a electron microscope(TEM). Finally, we dispersed them in excess of continuous water phase, observed the formation of maltese-cross liquid crystalline and measured the efficiency of drug deliveries and moisturizing effects.

• Biomolecules & Therapeutics
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• v.21 no.3
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• pp.234-240
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• 2013

Monoamine oxidase inhibitors (MAOI) have been widely used as antidepressants. Recently, there has been renewed interest in MAO inhibitors. The activity-guided fractionation of extracts from Angelica keiskei Koidzumi (A. keiskei K.) led to the isolation of two prenylated chalcones, xanthoangelol and 4-hydroxyderricin and a flavonoid, cynaroside. These three isolated compounds are the major active ingredients of A. keiskei K. to inhibit the MAOs and DBH activities. Xanthoangelol is a nonselective MAO inhibitor, and a potent dopamine ${\beta}$-hydroxylase (DBH) inhibitor. $IC_{50}$ values of xanthoangelol to MAO-A and MAO-B were calculated to be 43.4 ${\mu}M$, and 43.9 ${\mu}M$. These values were very similar to iproniazid, which is a nonselective MAO inhibitor used as a drug against depression. The $IC_{50}$ values of iproniazid were 37 ${\mu}M$, and 42.5 ${\mu}M$ in our parallel examination. Moreover, $IC_{50}$ value of xanthoangelol to DBH was calculated 0.52 ${\mu}M$. 4-Hydroxyderricin is a potent selective MAO-B inhibitor and also mildly inhibits DBH activity. The $IC_{50}$ value of 4-hydroxyderricin to MAO-B was calculated to be 3.43 ${\mu}M$ and this value was higher than that of deprenyl (0.046 ${\mu}M$) used as a positive control for selective MAO-B inhibitor in our test. Cynaroside is a most potent DBH inhibitor. The $IC_{50}$ value of cynaroside to DBH was calculated at 0.0410 ${\mu}M$. Results of this study suggest that the two prenylated chalcones, xanthoangelol and 4-hydroxyderricin isolated from A. keiskei K., are expected for potent candidates for development of combined antidepressant drug. A. keiskei K. will be an excellent new bio-functional food material that has the combined antidepressant effect.

• Biomolecules & Therapeutics
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• v.29 no.5
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• pp.498-505
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• 2021

Amyotrophic lateral sclerosis (ALS) is a lethal neurological disorder characterized by the deterioration of motor neurons. The aim of this study was to investigate alteration of cationic amino acid transporter (CAT-1) activity in the transport of lysine and the pretreatment effect of lysine on pro-inflammatory states in an amyotrophic lateral sclerosis cell line. The mRNA expression of cationic amino acid transporter 1 was lower in NSC-34/hSOD1^G93A (MT) than the control cell line (WT), lysine transport is mediated by CAT-1 in NSC-34 cell lines. The uptake of [³H]L-lysine was Na⁺-independent, voltage-sensitive, and strongly inhibited by inhibitors and substrates of cationic amino acid transporter 1 (system y⁺). The transport process involved two saturable processes in both cell lines. In the MT cell line, at a high-affinity site, the affinity was 9.4-fold higher and capacity 24-fold lower than that in the WT; at a low-affinity site, the capacity was 2.3-fold lower than that in the WT cell line. Donepezil and verapamil competitively inhibited [³H]L-lysine uptake in the NSC-34 cell lines. Pretreatment with pro-inflammatory cytokines decreased the uptake of [³H]L-lysine and mRNA expression levels in both cell lines; however, the addition of L-lysine restored the transport activity in the MT cell lines. L-Lysine exhibited neuroprotective effects against pro-inflammatory states in the ALS disease model cell lines. In conclusion, studying the alteration in the expression of transporters and characteristics of lysine transport in ALS can lead to the development of new therapies for neurodegenerative diseases.

• Communications for Statistical Applications and Methods
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• v.29 no.4
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• pp.421-439
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• 2022

Phase I dose-finding trials are essential in drug development. By finding the maximum tolerated dose (MTD) of a new drug or treatment, a Phase I trial establishes the recommended doses for later-phase testing. The primary toxicity endpoint of interest is often a binary variable, which describes an event of a patient who experiences dose-limiting toxicity. However, there is a growing interest in dose-finding studies regarding non-binary outcomes, defined by either the weighted sum of rates of various toxicity grades or a continuous outcome. Although several novel methods have been proposed in the literature, accessible software is still lacking to implement these methods. This study introduces a newly developed R package, UnifiedDoseFinding, which implements three phase I dose-finding methods with non-binary outcomes (Quasi- and Robust Quasi-CRM designs by Yuan et al. (2007) and Pan et al. (2014), gBOIN design by Mu et al. (2019), and by a method by Ivanova and Kim (2009)). For each of the methods, UnifiedDoseFinding provides corresponding functions that begin with next that determines the dose for the next cohort of patients, select, which selects the MTD defined by the non-binary toxicity endpoint when the trial is completed, and get oc, which obtains the operating characteristics. Three real examples are provided to help practitioners use these methods. The R package UnifiedDoseFinding, which is accessible in R CRAN, provides a user-friendly tool to facilitate the implementation of innovative dose-finding studies with nonbinary outcomes.

• Korean Journal of Clinical Pharmacy
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• v.32 no.3
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• pp.260-269
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• 2022

Background: Comprehensive medication management is essential to achieve safe and optimal drug use for the elderly in long-term care facilities (LTCF). This study aimed to develop eligibility criteria for "Comprehensive medication management program in LTCF" using the RAND/UCLA Appropriateness Method (RAM). Furthermore, we attempted to estimate the number of beneficiaries who met the criteria by analyzing the National Health Insurance claims data. Methods: Twelve criteria were selected initially. We composed a panel of 14 experts with expertise in long-term care. We conducted two survey rounds to reach a consensus. Rating for appropriateness and decision regarding agreement were applied per RAM. We analyzed the National Health Insurance data to estimate the number of LTCF residents who met each eligibility criterion. Results: Of the 11 items agreed upon, ten items were determined to be appropriate. In 2018, 83.6% of 165,994 residents of LTCF met one or more eligibility criteria. The largest number of subjects met the "New residents of LTCF" criterion, followed by "Take high-alert drugs" and "Chronic excessive polypharmacy." Since the items evaluated as most appropriate by the expert panel and those with a large number of subjects were similar, we confirmed the external validity of our criteria. Conclusion: It is worth noting that this is the first attempt to establish the eligibility criteria for medication management in LTCF. Further preliminary research is needed to identify the selected subjects' drug-related problems and revise the criteria according to the results.

• Microbiology and Biotechnology Letters
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• v.51 no.4
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• pp.432-440
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• 2023

Irrational and injudicious use of antibiotics, easy availability of them as over-the-counter drugs in economically developing countries, and unavailability of regulatory policies governing antimicrobial use in agriculture, animals, and humans, has led to the development of multi-drug resistance (MDR) bacteria. The use of medicinal plants can be considered as an alternative, with a consequent impact on microbial resistance. We tested extracts of Piper longum fruits as new natural products as agents for reversing the resistance to antibiotics. Six crude extracts of P. longum fruits were utilized against a clinical isolate of multidrug-resistant Staphylococcus aureus.The antibiotic susceptibility testing disc method was used in the antibiotic resistance reversal analysis. Apart from cefoxitin and erythromycin, all other antibiotics used (lincosamides [clindamycin], quinolones [levofloxacin and ciprofloxacin], and aminoglycosides [amikacin and gentamicin]) were enhanced by P. longum extracts. The extracts that showed the greatest synergy with the antibiotics were EAPL (ethyl acetate [extract of] P. longum), n-BPL (n-butanol [extract of] P. longum), and MPL (methanolic [extract of] P. longum The results of this study suggest that P. longum extracts have the ability to increase the effectiveness of different classes of antibiotics and reverse their resistance. However, future studies are needed to elucidate the molecular mechanisms behind the synergy between antibiotic and phytocompound(s) and identify the active biomolecules of P. longum responsible for the synergy in S. aureus.

• Preventive Nutrition and Food Science
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• v.18 no.2
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• pp.104-110
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• 2013

Presence of Helicobacter pylori is associated with an increased risk of developing upper gastrointestinal tract diseases. Antibiotic therapy and a combination of two or three drugs have been widely used to eradicate H. pylori infections. Due to antibiotic resistant drugs, new drug resources are needed such as plants which contain antibacterial compounds. The aim of this study was to investigate the ability of GutGard$^{TM}$ to inhibit H. pylori growth both in Mongolian gerbils and C57BL/6 mouse models. Male Mongolian gerbils were infected with the bacteria by intragastric inoculation ($2{\times}10^9$ CFU/gerbil) 3 times over 5 days and then orally treated once daily 6 times/week for 8 weeks with 15, 30 and 60 mg/kg GutGard$^{TM}$. After the final administration, biopsy samples of the gastric mucosa were assayed for bacterial identification via urease, catalase and ELISA assays as well as immunohistochemistry (IHC). In the Mongolian gerbil model, IHC and ELISA assays revealed that GutGard$^{TM}$ inhibited H. pylori colonization in gastric mucosa in a dose dependent manner. The anti-H. pylori effects of GutGard$^{TM}$ in H. pylori-infected C57BL/6 mice were also examined. We found that treatment with 25 mg/kg GutGard$^{TM}$ significantly reduced H. pylori colonization in mice gastric mucosa. Our results suggest that GutGard$^{TM}$ may be useful as an agent to prevent H. pylori infection.

• KSBB Journal
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• v.29 no.1
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• pp.36-41
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• 2014

Skin disease is one of the most common diseases and its incidence is increasing dramatically in modern society. Specially, many attempts have been made to treat chronic skin inflammation diseases, such as psoriasis and atopic dermatitis, but effective therapies for the immune cell-mediated skin diseases, including psoriasis and atopic dermatitis have not been developed. Until recently, several drug candidates which were claimed to be effective for skin diseases have been reported, but most of them are not used to treat chronic skin disease. Especially, Psoriasis is characterized by excessive growth and aberrant differentiation of keratinocytes, but is fully reversible with appropriate therapy. The trigger of the keratinocyte response is thought to be activation of the cellular immune system, with T cells and various immune-related cytokines. Formation of new blood vessels starts with early psoriatic changes and disappears with disease clearance. Several angiogenic mediators are up-regulated in psoriasis development. Contact- and mediator-dependent factors derived from keratinocytes, mast cells and immune cells may contribute to the strong blood vessel formation of psoriasis. New technologies and experimental models provide new insights into the role of angiogenesis in psoriasis pathogenesis. TMP and its derivatives themselves effectively inhibited in vitro cell migration, tube formation, and the expression of angiogenic factors. However, TMP and its derivatives induced side effects including hemolysis and local side effects. Therefore, in an attempt to reduce the toxicity and the undesirable side effects of TMP and derivatives, a liposomal formulation was prepared and tested for its effectiveness. TMP and derivatives liposomes retained the effectiveness of TMP in vitro while side effects were reduced. These results support the conclusion that TMP effectively inhibits in vitro angiogenesis, with the possibility that use as a psoriasis relief agent.

• The Journal of Korean Medicine
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• v.20 no.3 s.39
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• pp.9-17
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• 1999

Objectives: Recently a renovation of the medical-welfare system to reflect the changes of disease spectrum with the demographic changes of society, the increase in income level, and marked concerns for health promotion has been demanded. In accordance with this, attempts have been made to actively integrate traditional medicine based on symptom-differentiated treatment and Western medicine based on disease treatment so that they can complement each other. China has already tried a complementary medical treatment system integrating traditional Chinese and Western medicine. So, this article reviewed major advances in research on integrated traditional Chinese medicine and Western medicine in China. Methods: The authors analyzed data from clinical articles and experimental works in the ' Chinese Journal of Integrated Traditional and Western Medicine' Results and conclusions: Each department attempted to integrate Traditional Chinese Medicine(TCM) and Western Medicine in treatment of various diseases such as malaria, AIDS, and intoxication (rarely found in Korea clinically). Especially in the departments of surgery, dentistry, radiology, and anesthesiology we could see the frequent use of combined treatment. TCM and Western medicine complemented each other very successfully, and the effect of the combined therapy was superior to that of traditional therapy alone. There were diverse methods for therapy in integrated TCM and Western medicine; bath-Tx, physical-Tx, manipulative-Tx, drug -acupuncture, Tibetan medicine, etc. were available in therapy as well as traditional methods such as acupuncture, moxibustion, and negative- Tx. The way of producing Chinese medications were diversified and formulated; making new prescriptions, compounding various kinds of new medicine called' Zhong Cheng Yao' (中成藥) which were easily made, stored, and taken. 'Diagnosis Criteria', 'The effect of TCM Treatment Criteria' were made by committee and broadly used for objectifying diagnosis, discriminating effects of treatments and treatment development, and developing new medical products.