• Title/Summary/Keyword: Synthetic drugs

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Residue of Synthetic Antimicrobial Agent in Eggs by High Performance Liquid Chromatography (고속액체크로마토그라피에 의한 계란중의 합성항균제 잔류량)

  • Kim, Jong-Bea;Lee, Sung-Kuk;Kim, Doo-Hie
    • Journal of agricultural medicine and community health
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    • v.18 no.1
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    • pp.55-63
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    • 1993
  • A simultaneous determination method by HPLC for egg-residues sulfamerazine, sulfamethazine, sulfadimethoxine, furazolidone and zoalene was assesed. The drugs were extracted by dechloromethane, The extract after solvent evaporation, is partitioning in hex ane/water and back-partitioning in dechloromethane and analysis by HPLC. The average recovery rates of the above microbials from the egg spiked standard solution were approximately 81.2%, 87.6%, 92.5%. 86.1% and 79.3% respectively. The limit of detection of sulfamerazine. sulfamethazine and sulfamethoxine were in the levels of 0.2ppb, furazolidone and zoalene 0.5ppb respectively. According to this method 84 commercial eggs were examined. Sulfamethanzine was detected at levels of 0.005-0.008ppm in 3 eggs. Sulfadimethoxine was detected at levels of 0.012-0.019ppm in 4 eggs. No sulfamerazine, furazolidone and zoalene was detected in every samples. The residues of antimicrobial agent were safety level as food generally.

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Development of HPTLC Fingerprinting and Phytochemical Study of a Polyherbal Unani Formulation

  • Alam, Abrar;Siddiqui, Javed Inam;Naikodi, Mohammed Abdul Rasheed;Kazmi, Munawwar Husain
    • CELLMED
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    • v.10 no.1
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    • pp.7.1-7.6
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    • 2020
  • Plants produce a wide range of active principles, making them a rich source of different types of medicines. Without any knowledge of the phytoconstituents or active principles the medicinal plants itself or in the form of polyherbal formulations, were used by all society of human being from ancient times for prevention and cure of disease, but most of the traditional formulations including the formulation of Ayurveda and Unani have not been scientifically validated in order to establish the pharmacopoeial standards to improve the efficacy. Globally, the people become conscious that uses of synthetic drugs for a long period is not safe; the trend of medical society at large is looking at alternatives from natural, safe sources to combat diseases. Due to this comprehension, it has been increased the demand for plant-derived medicine, and on the other side, it is extremely important to standardize the polyherbal formulations and validate them scientifically to improve their safety and efficacy. The polyherbal Unani formulation Safuf-e-Muallif is widely used and recommended in Unani system of medicine (USM) as a spermatogenic agent, semen thickening agent, etc. to treat sexual disorders viz. premature ejaculation, nocturnal emission, etc. The study mainly deals with phytochemical screening for the detection of nature of phytoconstituents and analytical technique like High-performance thin-layer chromatography (HPTLC) for developing fingerprint of Safuf-e-Muallif revealing specific identities of the drug. The phytochemical screening and HPTLC fingerprint profile for SM reported here may be used as a reference standard for quality control purpose in future.

Synthesis and Anticonvulsant Evaluations of N-Cbz-$\alpha$-amino-N- alkoxyglutarimides

  • Kim, Min-Jeong;Byun, Ae-Sun;Choi, Jong-Won;Moon, Kyung-Ho;Lee, Chung-Kyu;Park, Min-Soo
    • Archives of Pharmacal Research
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    • v.27 no.2
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    • pp.151-155
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    • 2004
  • In our previous studies for the development of new anticonvulsant of broad spectrum, we found that N-cbz-$\alpha$-aminoglutarimides showed significant anticonvulsant activities of broad spectrum enough to be recommended for the new anticonvulsants and their anticonvulsant activities were dependent on their imide substituent groups. Based on these results, various N-cbz--$\alpha$-amino-N-alkoxyglutarimides, where the imide N-H was substituted with the hydroxy and alkoxy group, were prepared and evaluated for their anticonvulsant activities using the Maximal electroshock seizure (MES) and Pentylenetetrazole induced seizure (PTZ) tests and also the rotorod test. A series of (R) or (S)-N-cbz--$\alpha$-amino-N-alkoxyglutarimides could be prepared from the corresponding (R) or (S)-N-cbz-glutamic acid following the usual synthetic procedure. Among them, (R)-N-cbz--$\alpha$-amino-N-hydroxyglutarimide ($ED_{50}$=86.25 mg/kg) was most active in the MES test. In the case of the PTZ test, (R)-N-cbz--$\alpha$-amino-N-benzyloxyglutarimide ($ED_{50}$= 62.5 mg/kg) was most active. Among the tested compounds, 2a-c, 3a, and 3b showed anticonvulsant activities in the MES and PTZ test. All of the tested compounds, except 2f and 3f, showed significant anticonvulsant activities in the MES or PTZ test. In addition, the neurotoxicities of these compounds were comparable to other anticonvulsant drugs.

Cellular-uptake Behavior of Polymer Nanoparticles into Consideration of Biosafety

  • Do, Jeong-Hoe;An, Jeong-Ho;Joun, Yong-Seung;Chung, Dong-June;Kim, Ji-Heung
    • Macromolecular Research
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    • v.16 no.8
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    • pp.695-703
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    • 2008
  • Nanoparticles have tremendous potential in cancer prevention, detection and augmenting existing treatments. They can target tumors, carry imaging capability to document the presence of tumors, sense pathophysiological defects in tumor cells, deliver therapeutic genes or drugs based on the tumor characteristics, respond to external triggers to release an appropriate agent, document the tumor response, and identify the residual tumor cells. Nanoparticles < 30 nanometers in diameter show unexpected and unique properties. Furthermore, particles < 5 nanometers in size can easily penetrate cells as well as living tissues and organs. This study evaluated the safety of nano materials in a living body and the relationship between the living tissue and synthetic nano materials by examining the in-vitro cytotoxicity of poly(lactic-co-glycolic) acid (PLGA) nano-spheres and fluorescein isothiocynate(FITC)-labeled dendrimers as polymer nanoparticles. PLGA was chosen because it has been used extensively for biodegradable nanoparticles on account of its outstanding bio-compatibility and its acceptance as an FDA approved material. The dendrimer was chosen because it can carry a molecule that recognizes cancer cells, a therapeutic agent that can kill those cells, and a molecule that recognizes the signals of cell death. Cytotoxicity in L929 mouse fibroblasts was monitored using MTT assay. Microscopic observations were also carried out to observe cell growth. All assays yielded meaningful results and the PLGA nanoparticles showed less cytotoxicity than the dendrimer. These nano-particles ranged in size from 10 to 100 nm according to microscopy and spectroscopic methods.

Differential Expression of Ubiquitin-Specific Protease 16 Gene by Methylprednisolone in Neuronal Cells

  • Choi, Seung-Won;Kwon, Hyon-Jo;Koh, Hyeon-Song;Song, Shi-Hun;Kwon, O-Yu;Kim, Seon-Hwan
    • Biomedical Science Letters
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    • v.16 no.2
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    • pp.105-112
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    • 2010
  • Methylprednisolone (MPD) is a synthetic glucocorticoid drug used in treatment of many neurological diseases and neurotraumas, including spinal cord injuries. Little is known of the mechanism of MPD in neuronal cells, particularly the genetic expression aspect. DD-PCR was used in identification of genes expressed during MPD treatment of PC12 cells. We have isolated 3 predicted up- or down-regulated genes, which are differentially expressed in neurons by MPD. One of these genes, USP16 (ubiquitin specific protease 16), is the deubiquitinating enzyme that is up-regulated by MPD in neurons. In order to observe the effect of MPD on USP16 gene expression, PC12 cells were treated under several experimental conditions, including endoplasmic reticulum stress drugs. We have isolated the total RNAs in PC12 cells and detected USP16 and ER related genes by RT-PCR. Because its expression pattern is similar to expression of ER chaperons, USP16 gene expression is strongly associated with unfolded protein response. A meaningful negative effect on each tissue treated by methylprednisolone is not shown in vivo. USP16 gene expression is suppressed by LY294002 (phosphatidylinositol 3-kinase inhibitor), which suggests that USP16 gene expression is regulated by the phosphatidylinositol 3-kinase pathway.

Green Synthesis to Develop Iron-Nano Formulations and Its Toxicity Assays

  • Kulkarni, Smital;Mohanty, Nimain;Kadam, Nitin N.;Swain, Niharika;Thakur, Mansee
    • Journal of Pharmacopuncture
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    • v.23 no.3
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    • pp.165-172
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    • 2020
  • Objectives: In the past few years, herbal medicines have gained popularity over synthetic drugs because of their natural source and minimal side effects which has led to a tremendous growth of phytopharmaceuticals usage. With the development of nanotechnology, it provides alternative approaches to overcome several limitations using nano-formulations. In spite of considerable quantity of antianemic preparations with different iron forms available, currently additives are used and represented in modern pharmaceutical market. Iron deficiency anemia is a major global public health problem which particularly affects pregnant women, children and elderly persons. The situation is complicated because of disadvantages and drug side effects from existing antianemic medicines. There is a great demand for the development of new antianemic preparations. Green synthesis of iron oxide nanoparticles, possess high potential in this field. Methods: Our study focuses on developing green synthesis of iron oxide nanoparticles (IONPs) of 10-50 nm with spherical shape where different dosages were used -1 mg/kg, 10 mg/kg and 100 mg/kg for exposure in Wistar albino female rats for 28 days. The toxicity was assessed using various parameters such as measurements of the rat body and organ mass, hematology, biochemical evaluation and histopathological examinations. Results: No significant differences were observed in body and organ weights. Hematological indices also indicated no significant differences whereas biochemical factors showed increase in levels of direct bilirubin and globulin of medium as well as high dose and SGPT levels were increased only in high dose. The major organs (heart, kidney and liver) showed histopathological alterations in 10 and 100 mg/kg whereas brain showed only in 100 mg/kg. Conclusion: The toxicity of IONPs was found to be more significant when the concentration was increased; however, low doses can be used for further investigation as an antianemic preparation.

Development of a Label-Free LC-MS/MS-Based Glucosylceramide Synthase Assay and Its Application to Inhibitors Screening for Ceramide-Related Diseases

  • Fu, Zhicheng;Yun, So Yoon;Won, Jong Hoon;Back, Moon Jung;Jang, Ji Min;Ha, Hae Chan;Lee, Hae Kyung;Shin, In Chul;Kim, Ju Yeun;Kim, Hee Soo;Kim, Dae Kyong
    • Biomolecules & Therapeutics
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    • v.27 no.2
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    • pp.193-200
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    • 2019
  • Ceramide metabolism is known to be an essential etiology for various diseases, such as atopic dermatitis and Gaucher disease. Glucosylceramide synthase (GCS) is a key enzyme for the synthesis of glucosylceramide (GlcCer), which is a main ceramide metabolism pathway in mammalian cells. In this article, we developed a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method to determine GCS activity using synthetic non-natural sphingolipid C8-ceramide as a substrate. The reaction products, C8-GlcCer for GCS, could be separated on a C18 column by reverse-phase high-performance liquid chromatography (HPLC). Quantification was conducted using the multiple reaction monitoring (MRM) mode to monitor the precursor-to-product ion transitions of m/z $588.6{\rightarrow}264.4$ for C8-GlcCer at positive ionization mode. The calibration curve was established over the range of 0.625-160 ng/mL, and the correlation coefficient was larger than 0.999. This method was successfully applied to detect GCS in the human hepatocellular carcinoma cell line (HepG2 cells) and mouse peripheral blood mononuclear cells. We also evaluated the inhibition degree of a known GCS inhibitor 1-phenyl-2-decanoylamino-3-morpholino-1-propanol (PDMP) on GCS enzymatic activity and proved that this method could be successfully applied to GCS inhibitor screening of preventive and therapeutic drugs for ceramide metabolism diseases, such as atopic dermatitis and Gaucher disease.

Rapid determination and quantification of hair-growth compounds in adulterated products by ultra HPLC coupled to quadrupole-orbitrap MS

  • Lee, Ji Hyun;Park, Han Na;Kang, Gihaeng;Kim, Nam Sook;Park, Seongsoo;Lee, Jongkook;Kang, Hoil
    • Analytical Science and Technology
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    • v.32 no.2
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    • pp.56-64
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    • 2019
  • Recently, a number of adulterated products, which are advertised as hair-growth enhancer have been emerged among those who suffer hair loss disease. For continuous control of illegal products, in this study, a rapid and sensitive method for simultaneous screening of 12 compounds that enhance hair-growth was established to protect public health by ultrahigh-performance liquid chromatography coupled to quadrupole-orbitrap mass spectrometry (UHPLC-Q-Orbitrap-MS). Fragmentation pathways of them were proposed based on $MS^2$ spectral data obtained using the established method. In this analysis, the LODs and LOQs ranged from 0.05 to 50 ng/mL and from 0.17 to 167 ng/mL, respectively. The square of the linear correlation coefficient ($R^2$) was determined as more than 0.995. The intra- and inter-assay accuracies were respective 88-112 % and 88-115 %. Their precision values were measured within 5 % (intra-day) and 10 % (inter-day). Mean recoveries of target compounds in adulterated products ranged from 84 to 115%. The relative standard deviation of stability was less than 12 % at $4^{\circ}C$ for 48 h. The method was employed to screen 14 dietary supplements advertised to be effective for the treatment of hair loss. Some of the products (~21 %) were proven to contain synthetic drugs that promote hair growth such as triaminodil, minoxidil, and finasteride.

Novel GPR43 Agonists Exert an Anti-Inflammatory Effect in a Colitis Model

  • Park, Bi-Oh;Kang, Jong Soon;Paudel, Suresh;Park, Sung Goo;Park, Byoung Chul;Han, Sang-Bae;Kwak, Young-Shin;Kim, Jeong-Hoon;Kim, Sunhong
    • Biomolecules & Therapeutics
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    • v.30 no.1
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    • pp.48-54
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    • 2022
  • GPR43 (also known as FFAR2), a metabolite-sensing G-protein-coupled receptor stimulated by short-chain fatty acid (SCFA) ligands is involved in innate immunity and metabolism. GPR43 couples with Gαi/o and Gαq/11 heterotrimeric proteins and is capable of decreasing cyclic AMP and inducing Ca2+ flux. The GPR43 receptor has additionally been shown to bind β-arrestin 2 and inhibit inflammatory pathways, such as NF-κB. However, GPR43 shares the same ligands as GPR41, including acetate, propionate, and butyrate, and determination of its precise functions in association with endogenous ligands, such as SCFAs alone, therefore remains a considerable challenge. In this study, we generated novel synthetic agonists that display allosteric modulatory effects on GPR43 and downregulate NF-κB activity. In particular, the potency of compound 187 was significantly superior to that of pre-existing compounds in vitro. However, in the colitis model in vivo, compound 110 induced more potent attenuation of inflammation. These novel allosteric agonists of GPR43 clearly display anti-inflammatory potential, supporting their clinical utility as therapeutic drugs.

Polyphenol-rich Sargassum horneri alleviates atopic dermatitis-like skin lesions in NC/Nga mice by suppressing Th2-mediated cytokine IL-13

  • Suyama Prasansali, Mihindukulasooriya;Hyo Jin, Kim;Jinhee, Cho;Kalahe Hewage Iresha Nadeeka Madushani, Herath;Jiwon, Yang;Duong Thi Thuy, Dinh;Mi-Ok, Ko;You-Jin, Jeon;Ginnae, Ahn;Youngheun, Jee
    • ALGAE
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    • v.37 no.4
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    • pp.331-347
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    • 2022
  • Atopic dermatitis (AD) is one of major skin inflammatory diseases characterized by excessive Th2-mediated immune responses. Recent evidence provides that interlukin-13 (IL-13) plays the role of a key Th2 cytokine that drives the inflammation underlining AD. Due to adverse effects of commercially available synthetic drugs, the need for treatments based on natural products is gaining much attention. Sargassum horneri is an edible brown algae known for beneficial bioactivities including anti-inflammation. We investigated if polyphenol-rich S. horneri extracts (SHE) could suppress AD-like skin lesions in NC/Nga mice and if that involved inhibition of the infiltration of Th2-mediated cytokine IL-13. We observed markedly increased infiltration of IL-13 positive cells in AD-like skin lesions of mice but SHE treatments decreased it. Also, the dermal expression of IL-13 was sufficient to cause inflammatory responses in mice skin resembling human AD. SHE suppressed the dermal infiltration of inflammatory cells where IL-13 plays a crucial role in skin tissues and in the recruitment of inflammatory cells. Furthermore, it was confirmed that SHE reduced T cell, dendritic cell, and macrophage populations in spleen. Moreover, SHE decreased the collagen deposition in skin and ear dermis resulting in reduced fibrosis that occurs in AD due to excessive collagen. Taken together, our results reveal that SHE suppressed the infiltration of inflammatory cells into skin dermis by decreasing the infiltration of IL-13 positive cells. Therefore, SHE could be taken as a useful therapeutic agent to alleviate AD.