• Title/Summary/Keyword: Pharmaceutical compound

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HPLC Analysis and Screening of Standard Compound on Saposhnikoviae Radix for Standardization of GCSB-5 Preparation (생약복합제 GCSB-5의 품질 표준화를 위한 방풍의 지표성분 탐색 및 HPLC 분석)

  • Cha, Bae-Cheon;Lee, Eun-Hee
    • Korean Journal of Pharmacognosy
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    • v.40 no.2
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    • pp.103-108
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    • 2009
  • GCSB-5 preparation is a purified extract from a mixture of 6 medicinal plants(Acanthopanacis Cortex, Achyranthis Radix, Saposhnikoviae Radix, Cibotii Rhizoma, Glycine Semen Nigra, Eucommiae Cortex) that have been widely used for the treatment of various bone disorders. The aim of this study was to investigate HPLC analysis method and screening of standard compound on Saposhnikoviae Radix for quality standardization of a medicinal crude drug GCSB-5. Standard compound of Saposhnikoviae Radix was decided with cimifugin by isolation and instrumental analysis such as NMR. HPLC analysis method for the simultaneous determination of cimifugin was established for the quality control of the medicinal plants of Saposhnikoviae Radix species, GCSB-5 raw material and preparation. And validation of HPLC analysis methods were conformed for verification of HPLC methods by check to specificity, linearity, intra-day precision, inter-day precision and accuracy following ICH guideline.

Phytochemical Studies of Phyllanthus debilis

  • Chandrashekar, K.S.;Satyanarayana, D.;Joshi, A.B.;Subrahmanyam, E.V.S.
    • Natural Product Sciences
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    • v.10 no.3
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    • pp.101-103
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    • 2004
  • Two Lignans Phyllanthin and Hypophyllanthin, and a steroid ${\beta}-sitosterol$ has been isolated from the leaves of Phyllanthus debilis and their structures were established by spectral analysis and direct comparison with authentic samples. This is the first report of occurrence of these compound from P.debilis.

Ethyl Haematommate from Stereocaulon graminosum Schaer.: Isolation and Crystal Structure

  • Ismed, Friardi;Arifa, Nurwahidatul;Zaini, Erizal;Bakhtiar, Amri;Umeda, Daiki;Putra, Okky Dwichandra;Yonemochi, Etsuo
    • Natural Product Sciences
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    • v.24 no.2
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    • pp.115-118
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    • 2018
  • Herein, we reported the phytochemical investigation of whole thallus Sumatran lichen, Stereocaulon graminosum Schaer, and isolated a mono aromatic compound, ethyl haematommate (1). The structure of compound 1 have been established based on spectroscopic data and confirmed by single crystal X-ray structure analysis.

Synthesis and Inhibition Effects on 5-HT6 Receptor of Benzothiazole Derivatives

  • Hayat, Faisal;Yoo, Euna;Rhim, Hyewhon;ParkChoo, Hea-Young
    • Bulletin of the Korean Chemical Society
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    • v.34 no.2
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    • pp.495-499
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    • 2013
  • A novel series of aryl sulfonylpiperazine derivatives (5-15) were synthesized as 5-$HT_6$ ligands. In vitro assay was evaluated by measuring the 5-HT-induced $Ca^{2+}$ increases using HeLa cell line expressing the cloned human 5-$HT_6$ receptor, and the compound 13 showed potent 5-$HT_6$ receptor antagonistic effect with $IC_{50}$ value of 3.9 ${\mu}M$. Compound 13 also showed good selectivity on the 5-$HT_6$ over 5-$HT_4$ and 5-$HT_7$ receptors.

3-Phenethyl-2-phenylquinazolin-4(3H)-one isolated from marine-derived Acremonium sp. CNQ-049 as a dual- functional inhibitor of monoamine oxidases-B and butyrylcholinesterase

  • Jong Min Oh;Prima F. Hillman;Sang-Jip Nam;Hoon Kim
    • Journal of Applied Biological Chemistry
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    • v.66
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    • pp.165-170
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    • 2023
  • Isolation of the culture broth of a marine-derived Acremonium sp. CNQ-049 guided by HPLC-UV yielded compound 1 (3-phenethyl-2-phenylquinazolin-4(3H)-one), and its inhibitory activities against monoamine oxidases (MAOs), cholinesterases (ChEs), and β-secretase 1 (BACE1) were evaluated. Compound 1 was an effective selective MAO-B inhibitor with an IC50 value of 9.39 µM and a selectivity index (SI) value of 4.26 versus MAO-A. In addition, compound 1 showed a potent selective butyrylcholinesterase (BChE) inhibition with an IC50 value of 7.99 µM and an SI value of 5.01 versus acetylcholinesterase (AChE). However, compound 1 showed weak inhibitions against MAO-A, AChE, and BACE1. The Ki value of compound 1 for MAO-B was 5.22±1.73 µM with competitive inhibition, and the Ki value of compound 1 for BChE was 3.00±1.81 µM with mixed-type inhibition. Inhibitions of MAO-B and BChE by compound 1 were recovered by dialysis experiments. These results suggest that compound 1 is a dual-functional reversible inhibitor of MAO-B and BChE, that can be used as a treatment agent for neurological disorders.

Synthesis of 3-mercapto-4H-pyrrolopyridine (3-멀?토-4H-피롤로피리딘의 합성)

  • 마은숙
    • YAKHAK HOEJI
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    • v.46 no.6
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    • pp.369-374
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    • 2002
  • Dilithiation of 4-(pivaloylamino)pyridine (5) followed by reaction with tetraisopropylthiuram disulfide(TITD) gave rise to 3-(diisopropyldithiocarbamato)-4-(pivaloylamino)pyridine (6). 3-Mercapto-4H-pyrrolopyridine(2) was synthesized from compound 6 by two methods. The first method was that compound 6 was treated with 5M-HCl to form 2-t-butylthiazolo[5,4-c]pyridine (7) and hydrolysed in refluxing 10% NaOH and solid NaOH to prepare bis(4-amino-3-pyridyl)disulfide (8). And compound 8 was reacted with 2,5-dimethoxytetrahydrofuran and NaBH$_4$ to afford compound 2. The second method was that compound 6 was hydrolysed with 10% NaOH and followed to react with 2,5-dimethoxytetrahydrofuran to form compound 11. And then compound 11 was treated with 20% ethanolic KOH solution to synthesize compound 2.

Anthraquinone and Stibene Derivatives from the Cultivated Korean Rubbarb Rhizomes

  • Ko, Sung-Kwon;Whang, Wan-Kyunn;Kim, Il-Hyuk
    • Archives of Pharmacal Research
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    • v.18 no.4
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    • pp.282-288
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    • 1995
  • The sutdies were carried out to evaluate the consituents in the rihzomes of the cultivated Korean Rhubarb (Polygonaceae). From the acetone fraction ofl methanol extract Compound I (1, 8-dihydroxy-3-methyl anthraquinone, chrysophanic acid), Compound II($chrysophanol-8-O-{\beta}-D-glucopyranoside$), Compound III ($emodin-8-O-{\beta}-D-glucopyranoside$) and Compound IV ($aloe-emodin-8-O-{\beta}-D-glucopyranoside$), and from the ether fraction Compound V(1, 8-dihydorxy-3-emthyl-6-methoxy anthraquinone, physcion) and Compound VI (1, 6, 8-thitydroxy-3-emthyl anthrauinone, emodin), and also from the n-buthanol fraction Compound VII ($rhapontigenin-3-O-{\beta}-D-glucopyranoside, rhaponticin$) and Compound VIII ($piceatannol-3'-O-{\beta}-D-glucopyranoside$), were isolated and identified on the basis of their physico-chemical and spectroscopic evidences (UV, IR, H-NMR, C-NMR, EI-MS), respectively.

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Synthesis of Several heterocyclic Steroides. (이환성 Steroid의 합성)

  • 이성규
    • YAKHAK HOEJI
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    • v.7 no.4
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    • pp.98-99
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    • 1963
  • Compound III and IV were formed from I and II with $NH_{2}(CH_{2})_{3}NH_{2}$ respectively. Reduction of I with $LiAlH_{4}$ bollowed by $PoCl_{3}$ treatment affored VIII. Compound VI which was asumed by IR-data were obtained by treatment of $NH_{2}NH_{2}$ upon I or V.

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Cytotoxic Constituents form the Roots of Anthriscus sylvestris

  • Lim, Young-Hee;Leem, Moon-Jeong;Shin, Dong-Hyuk;Chang, Hwan-Bong;Hong, Seung-Woo;Moon, Eun-Yi;Lee, Dug-Keun;Yoon, Sung-June;Woo, Won-Sick
    • Archives of Pharmacal Research
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    • v.22 no.2
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    • pp.208-212
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    • 1999
  • Activity-guided fractionation of the roots of Anthriscus sylvestris resulted in the isolated and characterization of five cytotoxic compounds, deoxypodophyllotoxin (1), falcarindiol (2), and angeloyl podophyllotoxin (5) from the hexane soluble fraction and morelensin (3), bursehernin (4) from the choloroform soluble fraction. It is the first report of the occurrence of compound 5 in nature.

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Assessment of Occupational Exposure to Antineoplastic Agents in a Healthcare Setting (무균조제 항암제 취급의 안전관리)

  • Lee, Su-Mi;Chung, Seon-Young;Im, Hyun-Jeong;Park, Hyo-Jung;Lee, Su-Yun;Jeon, Eun-Yong;Sohn, Kie-Ho
    • YAKHAK HOEJI
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    • v.55 no.2
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    • pp.81-90
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    • 2011
  • Most antineoplastic agents are nonselective in their mechanism of action, affecting noncancerous as well as cancerous cells, and resulting in acute effects such as irritation of mucous membranes and chronic effects such as genotoxicity, teratogenicity, and carcinogenicity. Healthcare workers occupationally exposed to antineoplastic agents are at risk. The present study aimed to develop and apply methods to monitor occupational exposure to antineoplastic agents, using cyclophosphamide (CP) as the model compound. To monitor environmental and biological exposure, potentially contaminated surfaces were wiped and 24 hour urine samples were collected from workers. Liquid chromatography combined with tandem mass spectrometry was performed, with a limit of detection of 0.05 ng/ml. Measurable amounts of CP were detected on 92% of the sampled surfaces, with a geometric mean of 175.22 $ng/m^2$. Despite the environmental contamination of the model compound, CP was below the detection limit in all urine samples. If workplace contamination cannot be completely avoided, it is importance to reduce exposure to the lowest possible levels. To this aim, efforts to minimize occupational exposure along with biological and environmental monitoring are required. The standardized sampling techniques, and specific and sensitive analytical methods reported in this study may be helpful in assessing occupational exposure and devising strategies to reduce exposure.