• Title/Summary/Keyword: new drugs

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A Study for New Hepatotropic Agents from Natural Resources -The Effect of Azalea Pollen on Aromatic Toxicants Induced Hepatotoxicity- (천연자원을 이용한 간기능 증진제 개발 연구-Aromatic toxicants 에 의해 유도된 간기능 장해에 미치는 진달래 화분립의 영향)

  • 윤수홍;박은주
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.21 no.4
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    • pp.341-347
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    • 1992
  • In search for new drugs and methods of pharmacotherapy of liver damage , the pollen extracts was administrated to the experimental animals and ivnestigated its biochemical effects in the serum and liver when aromatic hepatotoxicants-phenybutazone, aniline and benzo(a) pyrene-was administered. As the results are the pretretment of azalea pollen was prevented the leakage of asartate aminotransaminase (AST), alanine aminotransfease(ALT), alkaline phosphatase (ALP) activity and bilirubin level to serum and liver, except serum lactate dehydrogenase (LDH) activity.

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Synthesis of 5-Aslkylthio (or sulfonyl) methyl-5-m-methoxy-phenylhydantion-3-acetic Acid Derivatives

  • Kwon, Soon-Kyoung;Park, Muoung-Suk;Nam, Young-Ju
    • Archives of Pharmacal Research
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    • v.16 no.4
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    • pp.322-326
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    • 1993
  • For the development of new antinflammatory and analgesic drugs, new 5-alkylthio (or sulfonyl) methyl-5-m-methoxyphenylhydantoin-3-acetic acid derivatives(alkyl; ethyl, propyl, butyl) were prepared. The 5,5 -disubstituted hydantoins which were used as starting materials, were prepared acording to Bucherer-Berg method. The reaction of ethyl chloroacelate with these compounds gave 3-acetate and the subsequent hydrolysis with dilute sodium hydroxide resulted in hydantoin 3-acetate and the subsequent hydrolysis with dilute sodium hydroxide resulted in hydantoin 3-acetic acid derivatives. Through the same procedure of equivalent hydroxide resulted in hydantoin 3-acetic acid derivatives. Through the same procedure of equivelent hydantions or the oxidation of 5-alkylthiohydantoin ocmpounds described above, 5-alkylsulfonylme-thyl-5-m-methoxyphenylhydantoin-30acetic acid derivatives were also synthesized.

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Molecular mechanisms and therapeutic interventions in sarcopenia

  • Park, Sung Sup;Kwon, Eun-Soo;Kwon, Ki-Sun
    • Osteoporosis and Sarcopenia
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    • v.3 no.3
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    • pp.117-122
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    • 2017
  • Sarcopenia is the degenerative loss of muscle mass and function with aging. Recently sarcopenia was recognized as a clinical disease by the International Classification of Disease, 10th revision, Clinical Modification. An imbalance between protein synthesis and degradation causes a gradual loss of muscle mass, resulting in a decline of muscle function as a progress of sarcopenia. Many mechanisms involved in the onset of sarcopenia include age-related factors as well as activity-, disease-, and nutrition-related factors. The stage of sarcopenia reflecting the severity of conditions assists clinical management of sarcopenia. It is important that systemic descriptions of the disease conditions include age, sex, and other environmental risk factors as well as levels of physical function. To develop a new therapeutic intervention needed is the detailed understanding of molecular and cellular mechanisms by which apoptosis, autophagy, atrophy, and hypertrophy occur in the muscle stem cells, myotubes, and/or neuromuscular junction. The new strategy to managing sarcopenia will be signal-modulating small molecules, natural compounds, repurposing of old drugs, and muscle-specific microRNAs.

A New Synthesis of Hydantoin derivatives by the Reaction of Unnatural Amino acids with Potassium Isocyanate

  • Park, Hae-Sun;Choi, Hee-Jeon;Kwon, Soon-Kyoung;Park, Myoung-Sook
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.339.1-339.1
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    • 2002
  • Since two selective COX-2 inhibitors. celecoxib and rofecoxib, showed good biological activity as antiinflammatory agents. many medicinal chemists are interested in specific COX-2 inhibitors. The distinguished feature of these drugs is that the 5-membered heterocycle ring is substituted with two aryl groups. Therefore, in this study, we designed a new hydantoin derivatives via the reaction of unnatural amino acids as selective COX-2 inhibitors, In systematically steps. 5-phenyl-1 (or substituted) hydantoin derivatives were prepared through esterification. bromination, C-N bond formation, cyclization from phenyl acetic acid. Particularly. a novel hydantoin ring was converted from unnatural amino acids with potassium isoyanate. In last step. the final analogs were synthesized the substitution at 3-position with alkyl reagents.

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Constructing Reference Transcriptome Sets of Codonopsis lanceolate(Deodeok) and Ixeridium dentatum

  • Tae-Ho Lee;Yun-Ho Oh
    • Proceedings of the Korean Society of Crop Science Conference
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    • 2022.10a
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    • pp.242-242
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    • 2022
  • As the aging population increases and interest in well-being increases, the importance of developing special crops increases. Natural medicine based on the special crops has been mainly used as an adjunct therapy for many diseases and symptoms based on culture, traditional medicine, and experience. In particular, it is attracting attention as a new resource to develop new drugs such as Artemisinin, a treatment for malaria. In order to efficiently use crops, it is essential to establish omics data such as genomes, transcriptomes, and metabolites of special-purpose crops. However, many special-purpose crops have large, heterogeneous and polyploid genomes that require high cost and long time to reference genome sequencing. Therefore, we built an inexpensive, fast, but very usefill reference transcriptome as the first step. We constructed high-quality reference transcriptom sets of Codonopsis lanceolata and Ixeridium dentatum with PacBio data. Our team will continue to construct reference transcriptoms of more special-purpose crops, and the data will be released by the National Agricultural Biotechnology Information Center (NABIC) in order to be widely used in agricultural as well as medical R&D.

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Evaluation of the Abuse Potential of Novel Amphetamine Derivatives with Modifications on the Amine (NBNA) and Phenyl (EDA, PMEA, 2-APN) Sites

  • Custodio, Raly James Perez;Botanas, Chrislean Jun;Yoon, Seong Shoon;de la Pena, June Bryan;dela Pena, Irene Joy;Kim, Mikyung;Woo, Taeseon;Seo, Joung-Wook;Jang, Choon-Gon;Kwon, Yong Ho;Kim, Nam Yong;Lee, Yong Sup;Kim, Hee Jin;Cheong, Jae Hoon
    • Biomolecules & Therapeutics
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    • v.25 no.6
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    • pp.578-585
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    • 2017
  • Recently, there has been a rise in the number of amphetamine derivatives that serve as substitutes for controlled substances (e.g. amphetamine and methamphetamine) on the global illegal drug market. These substances are capable of producing rewarding effects similar to their parent drug. In anticipation of the future rise of new and similar psychoactive substances, we designed and synthesized four novel amphetamine derivatives with N-benzyl, N-benzylamphetamine HCl (NBNA) substituent on the amine region, 1,4-dioxane ring, ethylenedioxy-amphetamine HCl (EDA), methyl, para-methylamphetamine HCl (PMEA), and naphthalene, 2-(aminopropyl) naphthalene HCl (2-APN) substituents on the phenyl site. Then, we evaluated their abuse potential in the conditioned place preference (CPP) test in mice and self-administration (SA) test in rats. We also investigated the psychostimulant properties of the novel drugs using the locomotor sensitization test in mice. Moreover, we performed qRT-PCR analyses to explore the effects of the novel drugs on the expression of D1 and D2 dopamine receptor genes in the striatum. NBNA, but not EDA, PMEA, and 2-APN, induced CPP and SA in rodents. None of the test drugs have produced locomotor sensitization. qRT-PCR analyses demonstrated that NBNA increased the expression of striatal D1 dopamine receptor genes. These data indicate that NBNA yields rewarding effects, suggesting potential for abuse. Continual observation for the rise of related substances is thus strongly encouraged.

A Comparative Analysis of the Systems Related to the Production, Authorization, and Listing for Insurance of Herbal Medicine Products in South Korea and Taiwan (국내와 대만의 전통약제제 생산.허가.보험등재 관련 제도)

  • Son, Chi-Hyoung;Lim, Sabina;Lee, Eun-Kyoung;Kim, Dong-Su;Kim, Yun-Gi;Cheng, Huan-Chiang;Kim, Yong-Ho
    • The Journal of Korean Medicine
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    • v.33 no.3
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    • pp.147-159
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    • 2012
  • Objectives: Systems related to the production, authorization, and listing for insurance of herbal medicine products were compared between South Korea and Taiwan to illuminate herbal medicine products system issues in South Korea. Methods: Papers, and laws and policies related to the production, authorization, and listing for insurance of herbal medicine products in South Korea and Taiwan are analyzed to create the primary documents. The documents from South Korea were screened with the advice of a specialist, while those from Taiwan have been verified through local investigation and with the help of a related specialist. The screened documents were then compared and analyzed in the order of the systems related to the production, authorization, and listing for insurance of herbal medicine products. Results: The systems related to the production of herbal medicine products satisfy GMP requirements in both countries, while Taiwan has more specialized systems related to the production of herbal medicine products and a more strict authorization program as compared to South Korea. While South Korea has most of the herbal medicine products classified as non-prescription drugs, Taiwan has them as prescription drugs. And while South Korea does not allow new herbal medicine products to be listed for insurance, Taiwan allows for once-a-year application toward listing for insurance. Conclusions: In order to ensure the safe and effective use of herbal medicine products, systems related to the production, authorization, and listing for insurance of herbal medicine products are to be established, while the categorization of medicine products principally used by Korean medicine doctors should be prepared. Furthermore, prescription by a Korean medicine doctor for new drugs made with natural products and their listing for insurance need to be encouraged.

Establishment of Quantitative Method for Generic Drugs in Korea Pharmaceutical Codex Monograph (공정서 수재 의약품의 정량법 개선에 관한 연구)

  • Song, JaeYong;Jang, JinSeob;Jang, SeungEun;Kim, SunHoi;Kim, InKyu;Lee, GilBong;Lee, JeaMan;Kim, YongHee
    • YAKHAK HOEJI
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    • v.56 no.5
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    • pp.288-292
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    • 2012
  • The aim of the paper is to ameliorate old research methods of Korean Pharmaceutical Codex to adjust the newest scientistic level which is necessary to maintain quality of medical supplies effectively. After reviewing result of Establishment of Dissolution Specifications for Generic Drugs in Korea Pharmaceutical Codex Monograph, there are two items chosen for the methods - Establishment of Dissolution Specifications for Generic Drugs in Korea Pharmaceutical Codex Monograph which KFDA researched in 2010, arranged new measuring standard by having an experiment to set measuring method after obtaining each item. According to the result, The experiment includes a measuring method of two items; Nafronyl Oxalate Capsules, and Ticlopidine Hydrochloride Tablets. The research is ameliorated by research methods through several experiments such as High Performance Liquid Chromatography validation, preparing items, implement of trial-experiment and authentic experiment, and experiment on measuring method of regulations of Korea Pharmaceutical Codex. The experiments are taken opinions of experts in KFDA into consideration and wrote out a report of the new measuring method on each last item. The report is combined as each two experiment sections of analyzing method to maintain the quality on the basis of the research in 2010 on setting of dissolution specifications for oral solid dosage forms. The result of measuring method of medical supplies through modernizing trial method of oral solid dosage forms is available to be accurate. In conclusion, this study could contribute to promotion of public health by organizing a basis for safe and high quality of medical supplies in domestic market.

Molecular Nuclear imaging of Angiogenesis (혈관신생 분자핵의학 영상)

  • Lee, Kyung-Han
    • The Korean Journal of Nuclear Medicine
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    • v.38 no.2
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    • pp.171-174
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    • 2004
  • Angiogenesis, the formation of new capillaries from existing vessels, increases oxygenation and nutrient supply to ischemic tissue and allows tumor growth and metastasis. As such, angiogenesis targeting provides a novel approach for cancer treatment with easier drug delivery and less drug resistance. Therapeutic anti-angiogenesis has shown impressive effects in animal tumor models and are now entering clinical trials. However, the successful clinical introduction of this new therapeutic approach requires diagnostic tools that can reliably measure angiogenesis in a noninvasive and repetitive manner. Molecular imaging is emerging as an exciting new discipline that deals with imaging of disease on a cellular or genetic level. Angiogenesis imaging is an important area for molecular imaging research, and the use of radiotracers offers a particularly promising technique for its development. While current perfusion and metabolism radiotracers can provide useful information related to tissue vascularity, recent endeavors are focused on the development of novel radioprobes that specifically and directly target angiogenic vessels. Presently available proges include RGD sequence containing peptides that target ${\alpha}_v\;{\beta}_3$ integrin, endothelial growth factors such as VEGF or FGF, metalloptoteinase inhibitors, and specific antiangiogenic drugs. It is now clear that nuclear medicine techniques have a remarkable potential for angiogenesis imaging, and efforts are currently continuing to develop new radioprobes with superior imaging properties. With future identification of novel targets, design of better probes, and improvements in instrumentation, radiotracer angiogenesis imaging promises to play an increasingly important role in the diagnostic evaluation and treatment of cancer and other angiogenesis related diseases.

Recent Progress in Drug Delivery Systems for Anticancer Agents

  • Kim, Chong-Kook;Lim, Soo-Jeong
    • Archives of Pharmacal Research
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    • v.25 no.3
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    • pp.229-239
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    • 2002
  • Recent progress in understanding the molecular basis of cancer brought out new materials such as oligonucleotides, genes, peptides and proteins as a source of new anticancer agents. Due to their macromolecular properties, however, new strategies of delivery for them are required to achieve their full therapeutic efficacy in clinical setting. Development of improved dosage forms of currently marketed anticancer drugs can also enhance their therapeutic values. Currently developed delivery systems for anticancer agents include colloidal systems (liposomes, emulsions, nanoparticles and micelles), polymer implants and polymer conjugates. These delivery systems have been able to provide enhanced therapeutic activity and reduced toxicity of anticancer agents mainly by altering their pharmacokinetics and biodistribution. Furthermore, the identification of cell-specific receptor/antigens on cancer cells have brought the development of ligand- or antibody-bearing delivery systems which can be targeted to cancer cells by specific binding to receptors or antigens. They have exhibited specific and selective delivery of anticancer agents to cancer. As a consequence of extensive research, clinical development of anticancer agents utilizing various delivery systems is undergoing worldwide. New technologies and multidisciplinary expertise to develop advanced drug delivery systems, applicable to a wide range of anticancer agents, may eventually lead to an effective cancer therapy in the future.