• 약학회지
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• 제49권5호
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• pp.392-398
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• 2005

In this study, we evaluated the stability of amoxicillin (AMX) and clavulanic acid (CLA) in aqueous solution, and compared the stability of AMX and CLA in commercial combination products. In aqueous solutions, the degradation of AMX ($t_{90}=8.88\;day\;at\;10^{circ}C$) and CLA ($t_{90}=3.53\;day\;at\;10^{circ}C$) occurred rapidly. From the pH-rate profile, AMX and CLA were the most stable at the range of pH 5.5 and 6.0. After reconstitution of commercial dry syrups, the contents of AMX and CLA in suspensions were gradually decreased for 7 days. However, AMX and CLA in dispersible tablet were not changed at all. The contents of CLA in the dispersible tablet ($87.92\%$) and dry syrups (2.16 and $3.91\%$) were remained in the accel­erated stability test ($75\%\;RH,\;at\;40^{circ}C$) after 10 hours. And the colors of the dry syrups were rapidly changed from white to yellow. From these results, we concluded that the dispersible tablet could overcome the stability problems of dry syrups.

• Natural Product Sciences
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• 제26권1호
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• pp.90-96
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• 2020

Artemisia capillaris Thunb. (Compositae) is a traditional medicinal plant with various pharmacological activities. To elucidate new anti-allergic and anti-inflammatory constituents, the aerial parts of A. capillaries were investigated to afford a new compound, (6E,8E)-6-methylundeca-6,8-diene-2,5,10-trione (17) together with 19 known compounds (1 - 16, 18 - 20). The structures of these compounds were determined by extensive spectroscopic analyses including 1D, 2D NMR, HREIMS, and optical rotation [α]_D. The absolute configuration of compound 2 was determined to be S form for the first time. All isolates (1 - 20) were tested their inhibitory effects on interleukin 2 (IL-2) expression in T cells and NO production in lipopolysaccharide (LPS)-stimulated RAW246.7. Among them, compounds 10, 11, 19, and 20 reduced IL-2 expression in a dose-dependent manner. In addition, compound 10 also inhibited NO production with an IC₅₀ value of 37.3 ± 0.4 μM.

• Toxicological Research
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• 제12권1호
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• pp.93-99
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• 1996

The effect of KTC-1, a new semisynthetic rifamycin antituberculous drug, on general toxicity, reproductive capability and fetal development was investigated in Sprague-Dawley rats. Male rats were administered KTC-1 with mashed feed from 63 days before mating to the end of mating period, and female rats were given from 14 days before mating to day 7 of gestation at dose levels of 0, 375, 750, and 1,500 ppm. The females were sacrificed on day 21 of gestation for examination of their fetuses. At 1,500 ppm, a reduction in body weight gain and testis atrophy were observed in male rats. Histological examination revealed testicular atrophy, absence or decrease of germinal cells, and vacuolization of Sertoli cells in testis. A reduction in body weight gain, a decrease in food consumption were found in female rats. In addition, decreases in the number of corpora lutea, iraplantations, and the litter size of live fetuses were seen. Mating, fertility, and pregnancy performances were also affected. There were no external abnormalities observed by examination of fetuses. At 750 ppm, a reduction in the body weight gain of male and female rats and decreases in the number of implantations and litter size were found. At 375 ppm, no treatment-related effects were observed. The results suggest that the no-effect dose levels (NOELs) of KTC-1 are 375 ppm for males and females on general toxicity, 750 ppm for males and females on reproductive capability, and 375 ppm for fetuses on embryonic development.

• Biomolecules & Therapeutics
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• 제27권1호
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• pp.78-84
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• 2019

Cell therapeutic agents for treating degenerative brain diseases using neural stem cells are actively being developed. However, few systems have been developed to monitor in real time whether the transplanted neural stem cells are actually differentiated into neurons. Therefore, it is necessary to develop a technology capable of specifically monitoring neuronal differentiation in vivo. In this study, we established a system that expresses cell membrane-targeting red fluorescent protein under control of the Synapsin promoter in order to specifically monitor differentiation from neural stem cells into neurons. In order to overcome the weak expression level of the tissue-specific promoter system, the partial 5' UTR sequence of Creb was added for efficient expression of the cell surface-specific antigen. This system was able to track functional neuronal differentiation of neural stem cells transplanted in vivo, which will help improve stem cell therapies.

• 대한한의학회지
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• 제40권2호
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• pp.94-105
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• 2019

Objectives: The correlation between medicinal herbal formulas and a risk of cardiotoxicity has been controversial. Thus, this study investigated cardiac safety assessment of 52 most commonly used medicinal herbal formulas. Methods: We evaluated the in vitro effects of medicinal herbal formulas on recombinant human embryonic kidney 293 (HEK 293) cell line expressing human ether-a-go-go-related gene (hERG) potassium channel. Results and Conclusion: Our results demonstrated that all of 52 medicinal herbal formulas did not show inhibition of hERG current in hERG-HEK 293 recombinant cells. In conclusion, these safety data suggest that 52 medicinal herbal formulas were not associated with an increased risk of cardiotoxicity in hERG-HEK 293 recombinant cells.

• BMB Reports
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• 제56권11호
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• pp.612-617
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• 2023

Pleiotropic regulator 1 (PLRG1), a highly conserved element in the spliceosome, can form a NineTeen Complex (NTC) with Prp19, SPF27, and CDC5L. This complex plays crucial roles in both pre-mRNA splicing and DNA repair processes. Here, we provide evidence that PLRG1 has a multifaceted impact on cancer cell proliferation. Comparing its expression levels in cancer and normal cells, we observed that PLRG1 was upregulated in various tumor tissues and cell lines. Knockdown of PLRG1 resulted in tumor-specific cell death. Depletion of PLRG1 had notable effects, including mitotic arrest, microtubule instability, endoplasmic reticulum (ER) stress, and accumulation of autophagy, ultimately culminating in apoptosis. Our results also demonstrated that PLRG1 downregulation contributed to DNA damage in cancer cells, which we confirmed through experimental validation as DNA repair impairment. Interestingly, when PLRG1 was decreased in normal cells, it induced G1 arrest as a self-protective mechanism, distinguishing it from effects observed in cancer cells. These results highlight multifaceted impacts of PLRG1 in cancer and underscore its potential as a novel anti-cancer strategy by selectively targeting cancer cells.

• 한국임상약학회지
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• 제23권2호
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• pp.89-96
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• 2013

This article aimed to introduce 'risk sharing' schemes for pharmaceuticals between drug manufacturers and healthcare payer. Published literature review was undertaken to summarize risk sharing concepts and collect information on existing scheme examples in other countries focusing on new anticancer drugs. Risk sharing schemes could be categorized into health outcomes-based and non-outcomes (financial) based ones. Outcome-based schemes could be broken down into performance-linked reimbursement and conditional coverage. Performance-linked reimbursement can be further broken into outcomes guarantee and pattern or process of care and conditional coverage included coverage with evidence development and conditional treatment continuation schemes. Non-outcome based schemes included market share and price volume at population level, and utilization caps and manufacturer funded treatment initiation at patient level. We reviewed the fifteen examples for anticancer drugs that risk sharing agreements in response to the inherent uncertainties and increased costs of eleven anticancer drugs. Of them, eight cases were coverage with evidence development schemes. The anticancer drugs except bevacizumab and cetuximab were all listed on the national health insurance formulary in Korea, with reimbursement criteria defined on the basis of approved indications and administrations. Risk sharing approach may be a useful tool to ensure values for drug expenditure, but there are a number of concerns such as high administration costs, lack of transparency and conflicts of interest, especially for performance-based health outcomes reimbursement schemes.

• Near Infrared Analysis
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• 제1권2호
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• pp.29-33
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• 2000

The identification step of raw drug materials is an indispensible procedure in the GMP manufacturing process within the pharmaceutical industry. However, wet chemistry methods for identification of drug materials, used by the various Pharmacopeia are time-consuming and expensive steps. In this paper, near-infrared spectroscopy (NIRS) has been developed for identifying eleven drug substances including calcium pantothenate, cefaclor, cefoperazone, cephradine, dextromethorphan, ehtambutol, nicotinamide, pyrozinamide, tramadol, vitamin C, and vitamin E. Also the aim of ths work is to consturct a new algorithm for calibration model using soft independence modeling of class analogy (SIMCA) with Malinowskis Indicator Function (IND), which is used for finding the number of principal components of each class of the SIMACA model. The use of NIR technique with pattern recognition to qualify raw materials can make it possible to monitor process in real time as well as to control all procedures in the pharmaceutical industry. As the result, the samples identified of 183 different batches from 11 different compounds were separated clearly by SIMCA with 2nd derivative spectra in the NIR region of 1100∼2400 nm.

• Nuclear Medicine and Molecular Imaging
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• 제42권5호
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• pp.337-346
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• 2008

Applications of nanotechnology in the medical field have provided the fundamentals of tremendous improvement in precise diagnosis and customized therapy. Recent advances in nanomedicine have led to establish a new concept of theragnosis, which utilizes nanomedicines as a therapeutic and diagnostic tool at the same time. The development of high affinity nanoparticles with large surface area and functional groups multiplies diagnostic and therapeutic capacities. Considering the specific conditions related to the disease of individual patient, customized therapy requires the identification of disease target at the cellular and molecular level for reducing side effects and enhancing therapeutic efficiency. Well-designed nanoparticles can minimize unnecessary exposure of cytotoxic drugs and maximize targeted localization of administrated drugs. This review will focus on major pharmaceutical nanomaterials and nanoparticles as key components of designing and surface engineering for targeted theragnostic drug development.

• 한국해양바이오학회지
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• 제2권4호
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• pp.209-223
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• 2007

Nature is one of the most important sources of pharmacologically active compounds in the search for drugs against life threatening diseases. Even though plants and terrestrial microorganisms have played as an important source for the new drug candidates from nature, marine organisms such as tunicates, sponges, soft corals, sea horses, sea snakes, marine mollusks, seaweeds, nudibranches, sea slugs and marine microorganisms are increasingly attracting attention in recent years. Marine organisms also have the potential to develop into future drugs against important diseases, such as cancer, a range of bacterial and viral diseases, malaria, and inflammations. Even though the mechanism of action in the molecular level of most metabolites is still unclear, the mechanisms by which they interfere with the pathogenesis of a wide range of diseases have been reported. The knowledge of this is one of the key factors necessary to develop bioactive compounds into medicines. This is due to their structurally unique and pharmacologically active compounds. The potential pharmaceutical, medicinal and research applications of some of these compounds are discussed in hundreds of scientific papers, and are reviewed here.