• Title/Summary/Keyword: R&D of new drug

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Effect of Ssanghwa-tang Extract on Antioxidant and Anti-aging Enzyme Activities (쌍화탕 추출물이 항산화효소 및 항노화관련 효소 활성에 미치는 영향)

  • Park, Ji-Young;Hwang, Jae-Gyu;Yun, Jong-Kuk;Han, Kil-Hwan;Do, Eun-Ju;Kim, Sung-Ok;Kim, Mi-Ryeo
    • The Korea Journal of Herbology
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    • v.27 no.3
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    • pp.67-74
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    • 2012
  • Objectives : The present study was designed to investigate effects of Ssanghwa-tang (Shu$\bar{a}$nghu$\bar{a}$-g$\bar{e}$ng) on oxidation/reduction reaction-related and aging-related enzymes $in$ $vitro$. Methods : We performed MTT assay, collagenase inhibition assay, elastase inhibition assay, tyrosinase inhibition assay, DPPH free radical scavenging assay, SOD-like activity and xanthine oxidase (XO) inhibition assay. Results : The 50% ethanol (EtOH) extract of Ssanghwa-tang (SHT) showed 55% inhibition of collagenase activity, and 42% inhibition of elastase activity at 1 mg/ml concentration. Also it's treatment showed 18% inhibition of tyrosinase activity, to relate whitening effect, at the same dose of 50% ethanol extract of SHT. Antioxidant activities were determined by DPPH radical scavenging, XO inhibiting activity and SOD-like activity. These scavenging, XO-inhibiting and SOD-like activities were measured in 80%, 75%, and 28% inhibitions, respectively, at a 1 mg/ml treated dose, compared to those of control. The inhibitory effects of 50% EtOH extract on aging and oxidation-related enzyme activities were higher than those of water extract and 95% EtOH extract. Conclusions : Taken together, our findings suggest that the SHT has potential and applicable benefits for development of cosmetics to have anti-aging (anti-wrinkle and whitening) and anti-oxidation functions.

New platinum-complex compounds with reduced nephrotoxicity discovered in long term histoculture of human renal cortex

  • Chang, S-G.;Jung, J.C.;Rho, Y.S.;Kwon, D.U.;Hoffman, R.M.
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1995.04a
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    • pp.124-124
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    • 1995
  • Cisplatinum is often effective in cancer treatment, but potent nephrotoxicity limits its clinical use. We have, therefore, developed new anticancer drugs that contain platinum. We have synthesized six new platinum compounds based on Figure 1. Drugs were initially administrated at 5${\times}$10$\^$-4/M with 48 hours exposure in monolayer cultures of primary rabbit proximal tubular cells and human renal cortical cells with the M.T.T. endpoint to measure toxicity. Drug concentrations of 10$\^$-3/M, 10$\^$-4/M, and 10$\^$-5/M with 72 hours exposure were used for human renal cortical tissues in 7 weeks histoculture with toxicity measured by the glucose-consumption endpoint. From these studies, we determined that the new platinum drugs have lower nephrotoxicity than cisplatinum. Drugs D, E, and H. have lower nephrotoxicity than the other new drugs. We are currently measuring the anticancer efficacy of drugs D, E, and H.

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A Study on Amendment of Approval Specifications for Traditional Korean Medicines (한약제제 허가기준 개선방안 연구(I))

  • Han Byong-Hyon;Hwang Gwi-Seo
    • Journal of Society of Preventive Korean Medicine
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    • v.5 no.1
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    • pp.57-75
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    • 2001
  • This study was conducted to improve the current regulation guidelines for developing traditional Korean medicines with effectiveness and productivity, in order to cope with the upcoming ICH on specifications on oriental herbal drugs. Also, major purposes of this study are to motivate R&D and to pioneer foreign markets for domestic herbal drug companies. First, after examining concepts of traditional Korean medicines and comparing the numbers and differentiation of herbal drugs registered on Pharmacopeia among Korea, China, and Japan, the current new drug development requirements for traditional Korean medicines were reviewed in detail, followed by comparison of foreign regulation systems including USA, EU, China, and Japan. Second, empirical cases on failure of development for new traditional Korean medicines under the current regulation system in the domestic companies including Dong-A, Kwangdong, and Samchondang, were collected and analyzed. As a result, hanbangsaengyak, the new category for traditional Korean medicines was newly developed on the basis of scientification of data between saengyak and hanyak, from the perspectives of harmonization between oriental medicine and western medicine and of balance between food and drug, in terms of industrialization, publicity, modernization, and effectiveness of administration. In addition, the new regulation requirements for the new hanbangsaengyak preparations were discussed by establishing principles of reinforcing preclinical test and of simplifying clinical trials in Korea. Finally, the further researches to articulate the complete specifications for pre-clinical and clinical requirements for traditional Korean medicines were strongly suggested.

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In vitro and In vivo Anti-Helicobacter pylori Activities of Centella asiatica Leaf Extract

  • Zheng, Hong-Mei;Choi, Myung-Joo;Kim, Jae Min;Lee, Kye Wan;Park, Yu Hwa;Lee, Don Haeng
    • Preventive Nutrition and Food Science
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    • v.21 no.3
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    • pp.197-201
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    • 2016
  • Helicobacter pylori infection is associated with an increased risk of developing upper gastrointestinal tract diseases. However, treatment failure is a major cause of concern mainly due to possible recurrence of infection, the side effects, and resistance to antibiotics. The aim of this study was to investigate the activities of Centella asiatica leaf extract (CAE) against H. pylori both in vitro and in vivo. The minimum inhibitory concentrations (MICs) against 55 clinically isolated strains of H. pylori were tested using an agar dilution method. The MICs of CAE ranged from 0.125 mg/mL to 8 mg/mL, effectiveness in inhibiting H. pylori growth was 2 mg/mL. The anti-H. pylori effects of CAE in vivo were also examined in H. pylori-infected C57BL/6 mice. CAE was orally administrated once daily for 3 weeks at doses of 50 mg/kg and 250 mg/kg. CAE at the 50 mg/kg dose significantly reduced H. pylori colonization in mice gastric mucosa. Our study provides novel insights into the therapeutic effects of CAE against H. pylori infection, and it suggests that CAE may be useful as an alternative therapy.

Absorption Enhancer and Polymer (Vitamin E TPGS and PVP K29) by Solid Dispersion Improve Dissolution and Bioavailability of Eprosartan Mesylate

  • Ahn, Jae-Soon;Kim, Kang-Min;Ko, Chan-Young;Kang, Jae-Seon
    • Bulletin of the Korean Chemical Society
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    • v.32 no.5
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    • pp.1587-1592
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    • 2011
  • The aim of the present study was to improve the solubility and bioavailability of a poorly water-soluble drug in human body, using a solid dispersion technique (hot melt extrusion). The solid dispersion was prepared by cooling the hot melt of the drug in the carrier (Vitamin E TPGS and PVP). The dissolution rate of formulation 1 from a novel formulation prepared by solid dispersion technique was equal to release of formulation 6 (40% of eprosartan mesylate is in contrast to teveten$^{(R)}$) within 60 min (Table 1). The oral bioavailability of new eprosartan mesylate tablet having vitamin E TPGS and PVP K29 was tested on rats and dogs. Of the absorption enhancer and polymer tested, vitamin E TPGS and PVP K29, resulted in the greatest increases of AUC in animals (about 2.5-fold increase in rat and dog). When eprosartan mesylate was mixed with the absorption enhancer and polymer in a ratio of 2.94:2:1, vitamin E TPGS and PVP K29 improved eprosartan mesylate bioavailability significantly compared with the conventional immediate release (IR) tablet Teveten$^{(R)}$ (formulation 7). These results show that solid dispersion using vitamin E TPGS and PVP K29 is a promising approach for developing eprosartan mesylate drug products.

Isolation and Structure Elucidation of a New Glycolipid from the Soft Coral Lobophytum microlobulatum Collected from Havellock Island of Andaman and Nicobar Group of Islands

  • Anjaneyulu, Ammanamanchi S.R.;Rao, Nidasanametla S. Kameswara;Garg, H.S.
    • Natural Product Sciences
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    • v.2 no.2
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    • pp.102-105
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    • 1996
  • A new glycolipid, 2-hydroxy-3 $(octadecyloxy)-propyl-{\alpha}-D-arabinopyranoside$ (1) has been isolated from Lobophytum microlobulatum and its structure has been elucidated by physical and spectral $(UV,\;IR,\;^1H,\;^{13}C\;NMR,\;FABMS)$ data.

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Hepatic Drug Metabolism Modifier from Arils of Myristica fragrans

  • Shin, Kuk-Hyun;Woo, Won-Sick
    • Korean Journal of Pharmacognosy
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    • v.17 no.1
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    • pp.91-99
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    • 1986
  • The single treatment of mice with steam distillate, non-volatile ether extract and methanol extract from mace (Arils of Myristica fragrans) caused a significant prolongation of hexobarbital-induced narcosis and increase in strychnine toxicity as well as a significant decrease in hepatic microsomal drug metabolizing enzyme activities. On 7 consecutive daily administrations, however, the duration of hypnosis was markedly shortened and significant increases in the hepatic enzyme activities were shown. With systematic fractionation by $SiO_2$ column chromatography of non-volatile ether fraction monitoring by animal tests a new lignan (mp $70{\sim}72^{\circ}$, MW 328, $[{\alpha}]^{20}_D+5.28$) was isolated as an active principle and its structure was elucidated as (2R, 3S)-1-(3,4-methylendioxyphenyl)-2,3 dimethyl-4-(4-hydroxy-3-methoxyphenyl) butane.

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Analytical comparison of structural changes of plastic cell-based therapeutic drug storage containers when exposed to cryogenic environments (플라스틱 세포치료제 보관용기의 극저온 환경 노출 시 구조적 변화에 대한 해석적 비교)

  • Park, Jeong-Yeon;Lee, Dong-Mok;Lee, Jienny;Lee, Sun-ray;Yoon, Gil-Sang
    • Design & Manufacturing
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    • v.14 no.2
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    • pp.1-6
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    • 2020
  • Recently, research and commercialization related to the field of cell-based therapeutic drug development has been actively conducted. In order to maintain cell viability and prevent contamination, refrigeration preservation devices, such as CRF (controlled rate freezer) or vapor type LN2 tanks have been developed. On the other hand, the storage container for liquid nitrogen tanks currently on sale minimizes the flow structure to prevent structural defects when stored in a liquid nitrogen tank having a high thermal conductivity than vapor nitrogen. If the cell-based treatment drug is stored in the gaseous LN2 tank as it is, the cell survival after thawing is greatly reduced. It was estimated that the existing storage container structure was a factor that prevented the rapid entry and circulation of gaseous nitrogen into the container. Therefore, this study intends to propose a new supercellular storage container model that can maintain the mechanical strength while maximizing the fluid flow structure. To this end, we estimated that the structural change of the storage container effects on the equivalent stress formed around the through-holes of them when exposed to a cryogenic environment using thermal-structural coupled field analysis. As a result of storage experiments in the gas phase tank of the cell-based therapeutic agent using the developed storage container, it was confirmed that the cell growth rate was improved from 66% to 77%, which satisfied the transportation standards of the FDA(Food and Drug Administration) cell-based therapeutic agent.

A Comparative Study on the Real Options Valuation of Biotechnology R&D (인간유전체 기능연구사업의 실물옵션 가치평가 비교)

  • Park Jung-Min;Seol Sung-Soo
    • Journal of Korea Technology Innovation Society
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    • v.9 no.1
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    • pp.84-102
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    • 2006
  • This paper compares four models to value a biotechnology R&D project; option tree model, dynamic discounted cash flow(DCF) model, and option thinking DCF model with general DCF model. Real Options, especially 6-folded option tree model yields boner estimate of value than values using other methods. According to sensitivity analysis, sales of final products, number of investigational new drug developments(INDs) and success rates of each stage are key factors for the value of biotechnology R&D investment.

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Effects of Mixed Medicinal Herbs on Adipogenesis and Apoptosis in 3T3-L1 Adipocytes (배합된 한약재의 추출물이 3T3-L1 지방세포의 지방생성과 세포사멸에 미치는 영향)

  • Hwang, Su-Jung;Shin, In-Soon;Kim, Mi-Ryeo
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.24 no.4
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    • pp.661-667
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    • 2010
  • Astragali Radix (AR) has been used in traditional medicinal herb, which is known to tonify the qi and blood. It has been asserted to be a tonic that can improve the function of the lungs, adrenal glands and the gastrointestinal tract, increase metabolism, promote healing and reduce fatigue. Also, Plantago asiatica (PA) has the anti-inflammatory, antiseptic, antitussive, cardiac, diuretic, expectorant, haemostatic effects, though it is considered to be less powerful than the seed. Recent research is showing that it is promising in lowering cholesterol and controlling diabetes. Obesity is characterized at the cellular level by an increase in the number and size of adipocytes differentiated from fibroblastic preadipocytes in adipose tissue. In the present study, we investigated the effects of 3 to 7 extracts of mixed medicinal herbs (water and ethanol extract of Astragali Radix; ARW and ARE, water and ethanol extract of Plantago asitica; PAW and PAE, and those mixed extracts; ARW+PAE, ARW+PAW and ARE+PAE) on adipogenesis and apoptosis in 3T3-L1 adipocytes by MTT assay, Oil-Red-O staining and TUNEL assay. And then, we determined total contents of phenolic compounds and flavonoid compounds in mixed herbal extracts. These result showed that herbal extracts (ARW, PAE and ARW+PAE) affected on adipogenesis and apoptosis in 3T3-L1 adipocytes among 3 to 7 extracts tested. Especially herbal mixed extracts (ARW+PAE) had the highest inhibition on differentiation of preadipocytes and lipoid accumulation of maturing adipocytes. And it did not affect cell viability of mature adipocytes, but herbal mixed extracts (ARW+PAE) increased apoptosis in mature adipocytes, as proved by highest concentration $200\;{\mu}g/m{\ell}$ using TUNEL assay. In addition, contents of total phenoilc compounds and flavonoids showed the highest level in ARE+PAE and PAE than ARW. These results suggest that this main target for adipocyte functions could be effective in improving the metabolic syndrome including obesity.