• Title/Summary/Keyword: New drug development

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Studies on the Method of Decoction Preparation in the Prescription of Crude Drugs. -on the prevention to the loss of volatile oil- (생약처방(生藥處方)의 탕(湯)(전(煎))제(劑) 제조(製造)에 관(關)한 연구(硏究) -유효휘발성분(有效揮發成分)의 손실방지(損失防止)에 관(關)하여-)

  • Chung, Myung-Hyun;Lee, Choon-Heung
    • Korean Journal of Pharmacognosy
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    • v.8 no.2
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    • pp.69-72
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    • 1977
  • The investigation is involved with the development of the new method of decoction preparation in order to prevent the loss of volatile oil from crude drugs. Volatile oil in crude drug containig volatile oil ranged from 1 to 2.2% in content. Volatile oil content in crude drung prescription which main component is a crude drug containing volatile oil was $0.11{\sim}0.39\;ml$. It was found that traditional method of decoction preparation has caused to lose almost all of the volatile oil. Application of method of Pharmacopoea (Kp II) for the preparation of decoction prevented the loss of volatile oil from one half to two-third of its content. The method of Pharmacopoea to which air condenser was attached could completely prevented the loss of volatile oil from the preparation.

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Metabolism-based Anticancer Drug Design

  • Kwon, Chul-Hoon
    • Archives of Pharmacal Research
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    • v.22 no.6
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    • pp.533-541
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    • 1999
  • Many conventional anticancer drugs display relatively poor selectivity for neoplastic cells, in particular for solid tumors. Furthermore, expression or development of drug resistance, increased glutathione transferases as well as enhanced DNA repair decrease the efficacy of these drugs. Research efforts continue to overcome these problems by understanding these mechanisms and by developing more effective anticancer drugs. Cyclophosphamide is one of the most widely used alkylating anticancer agents. Because of its unique activation mechanism, numerous bioreversible prodrugs of phosphramide mustard, the active species of cyclophosphamide, have been investigated in an attempt to improve the therapeutic index. Solid tumors are particularly resistant to radiation and chemotherapy. There has been considerable interest in designing drugs selective for hypoxic environments prevalent in solid tumors. Much of the work had been centered on nitroheterocyclics that utilize nitroreductase enzyme systems for their activation. In this article, recent developments of anticancer prodrug design are described with a particular emphasis on exploitation of selective metabolic processes for their activation.

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Effects of Ascaris suum Extract and Sulfamethoxazole on Allergic Airway Inflammation

  • Cho, Eun-Sang;Park, Bae-Keun;Son, Hwa-Young
    • Biomolecules & Therapeutics
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    • v.19 no.4
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    • pp.466-471
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    • 2011
  • Allergic asthma is complex inflammatory airway disorder caused by genetic and environmental factors. Sulfamethoxazole, a sulfonamide, is the cause of drug rash with eosinophilia and systemic symptoms syndrome. Parasites infection also related with eosinophilia and allergic diseases. In the present study, we investigated the modulating effects of parasitic derivative and sulfamethoxazole (SMX) on allergic airway inflammation in the ovalbumin (OVA)-induced murine asthma model. Histopathological changes, cytokine secretion, and total and allergen-specific IgE were investigated. BALB/c mice were treated with Ascaris suum extract or SMX for 4 weeks before sensitized and challenged to ovalbumin. Pre-treatment of Ascaris suum extract decreased allergic inflammation in lung tissue and IL-4, total IgE, and OVA-specific IgE levels in bronchoalveolar lavage fluid. However, pre-treatment of SMX did not show any effects on allergic airway inflammation. These results indicate that parasitic infection has protective effects on allergic asthma, but the sulfamamides may not relate with allergic asthma.

Recent Trends in Cyclic Peptides as Therapeutic Agents and Biochemical Tools

  • Choi, Joon-Seok;Joo, Sang Hoon
    • Biomolecules & Therapeutics
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    • v.28 no.1
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    • pp.18-24
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    • 2020
  • Notable progress has been made in the therapeutic and research applications of cyclic peptides since our previous review. New drugs based on cyclic peptides are entering the market, such as plecanatide, a cyclic peptide approved by the United States Food and Drug Administration in 2017 for the treatment of chronic idiopathic constipation. In this review, we discuss recent developments in stapled peptides, prepared with the use of chemical linkers, and bicyclic/tricyclic peptides with more than two rings. These have widespread applications for clinical and research purposes: imaging, diagnostics, improvement of oral absorption, enzyme inhibition, development of receptor agonist/antagonist, and the modulation of protein-protein interaction or protein-RNA interaction. Many cyclic peptides are expected to emerge as therapeutics and biochemical tools.

Deciphering the underlying mechanism of liver diseases through utilization of multicellular hepatic spheroid models

  • Sanghwa Kim;Su-Yeon Lee;Haeng Ran Seo
    • BMB Reports
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    • v.56 no.4
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    • pp.225-233
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    • 2023
  • Hepatocellular carcinoma (HCC) is a very common form of cancer worldwide and is often fatal. Although the histopathology of HCC is characterized by metabolic pathophysiology, fibrosis, and cirrhosis, the focus of treatment has been on eliminating HCC. Recently, three-dimensional (3D) multicellular hepatic spheroid (MCHS) models have provided a) new therapeutic strategies for progressive fibrotic liver diseases, such as antifibrotic and anti-inflammatory drugs, b) molecular targets, and c) treatments for metabolic dysregulation. MCHS models provide a potent anti-cancer tool because they can mimic a) tumor complexity and heterogeneity, b) the 3D context of tumor cells, and c) the gradients of physiological parameters that are characteristic of tumors in vivo. However, the information provided by an multicelluar tumor spheroid (MCTS) model must always be considered in the context of tumors in vivo. This mini-review summarizes what is known about tumor HCC heterogeneity and complexity and the advances provided by MCHS models for innovations in drug development to combat liver diseases.

Synthesis of unnatural compounds by enzyme engineering

  • Morita, Hiroyuki
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2019.04a
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    • pp.34-34
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    • 2019
  • About 60% of the present drugs were developed from natural products with unique chemical diversity and biological activities. Hence, discovery of new bioactive compounds from natural products is still important for the drug development. On the other hand, breakthrough made in synthetic biology has also begun to supply us with many useful compounds through manipulation of biosynthetic gene for secondary metabolites. Theoretically, this approach can also be exploited to generate new unnatural compounds by intermixing genes from different biosynthetic pathway. Considering the potential, we are studying about bioactive compounds in natural sources, as well as the biosynthesis of natural products including engineering of the secondary metabolite enzymes to make new compounds in order to construct the methodological basis of the synthetic biology. In this symposium, engineering of secondary metabolite enzymes that are involved in the biosynthesis of plant polyketides to generate new compounds in our laboratory will be mainly introduced.

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Perinatal and Postnatal Study of KTC-1, a New Semisynthetic Rifamycin Derivative, in Rats (새로운 반합성 Rifamycin 유도체 KTC-1의 랫트 주산기 및 수유기 시험)

  • 김종춘;정문구;한상섭;노정구
    • Toxicological Research
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    • v.11 no.1
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    • pp.91-101
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    • 1995
  • A perinatal and postnatal study of KTC-1, a new semisyntheitic rifamycin antituberculous drug, was conducted in Sprague-Dawley rats. Dosages of KTC-1 0, 12, 27.6, and 63.5 mg/kg/day were administered to dams orally by gavage from day 17 of gestation to day 21 of lactation. All pregnant rats were allowed to deliver naturally for postnatal examination of their offspring. At 63.5 mg/kg/day, weakness, dark-red discharge around eyes, a loss in body weight, and a decrease in food and water consumption were observed in dams. An increase in the weight of adrenal gland and spleen, and a decrease in the weight of kidney and heart were also found. An increase in neonatal deaths during the lactation period, a loss in body weight, a delay in physical development, a decrease in traction ability, an increase in the number of errors and the time required for the multiple T-maze trial were found in F1 offspring. In addition, an increase in the incidence of visceral variations and retarded ossification were observed in F1 4 day old rats. An increase in the incience of skeletal anomalies was seen in F2 fetuses. There were no sings of maternal toxicity or embryotoxicity at 12 and 27.6 mg/kg/day. From the results mentioned above, it can be concluded that the no-effect dose levels(NOELs)for dams, F1 offspring, and F2 fetuses are 27.6 mg/kg/day.

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A New Cell Counting Method to Evaluate Anti-tumor Compound Activity

  • Wang, Xue-Jian;Zhang, Xiu-Rong;Zhang, Lei;Li, Qing-Hua;Wang, Lin;Shi, Li-Hong;Fang, Chun-Yan
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.8
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    • pp.3397-3401
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    • 2014
  • Determining cell quantity is a common problem in cytology research and anti-tumor drug development. A simple and low-cost method was developed to determine monolayer and adherent-growth cell quantities. The cell nucleus is located in the cytoplasm, and is independent. Thus, the nucleus cannot make contact even if the cell density is heavy. This phenomenon is the foundation of accurate cell-nucleus recognition. The cell nucleus is easily recognizable in images after fluorescent staining because it is independent. A one-to-one relationship exists between the nucleus and the cell; therefore, this method can be used to determine the quantity of proliferating cells. Results indicated that the activity of the histone deacetylase inhibitor Z1 was effective after this method was used. The nude-mouse xenograft model also revealed the potent anti-tumor activity of Z1. This research presents a new anti-tumor-drug evaluation method.

Effect of Ijintang - hot water & methanol extracts - on the regional cerebral blood flow and cerebral edema in MCA occlusioned rats (뇌경색유발(腦梗塞誘發) 흰쥐의 국소뇌혈류량(局所腦血流量)과 뇌부종(腦浮腫)에 대한 이진탕(二陳湯)의 수(水) 및 메탄올추출엑스의 효과(效果))

  • Yun, Sang-Hyeop;Min, Byeong-Il;Ryu, Jae-Hwan
    • The Journal of Korean Medicine
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    • v.17 no.2 s.32
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    • pp.161-167
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    • 1996
  • For the purpose of developing a new drug against cerebral infarction, we chose Ijintang which is frequently applied in the field of Jung Pung of traditional medicine. From this formula, water extract and methanol extract were prepared respectively. Animals were divided into three groups; control group, water extract medicated group, methanol extract treated group. water extract was given 195mg/kg orally and methanol extract, 165mg/kg for 2 weeks in case of cerebral edema and 1 month in regional cerebral blood flow. On the regional cerebral blood flow, the drug medicated groups showed no significant changes as compared gith control group. There was no significant difference on the cerebral edema among the groups. According to the results above, it is suggested that oral medication of water extract and methanol extract from Ijintang have no effect on the change of rCBF and edema after acutely induced cerebral infarction. However, it is thought that modification of administration method and development of new animal model for traditional medicine are needed.

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Parametric Sequential Test Procedure to Find the Minimum Effective Dose (최소 효과 용량을 정하는 축차 검정법)

  • Park, Su-Jin;Kim, Dong-Jae
    • The Korean Journal of Applied Statistics
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    • v.22 no.5
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    • pp.1033-1046
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    • 2009
  • In new drug development studies or clinical trials, zero-dose control is needed in general to determine the lowest dose level for a new drug which can act with our bodies. When the lowest dose level compared with zero-dose control has significant difference in effect, it is referred as minimum effective dose(MED). We propose, in this paper, parametric sequential test using updated control to identify the minimum effective dose(MED) level. Monte Carlo Simulation is adapted to examine the power and experimental significance levels of the proposed method with other methods.