• Title/Summary/Keyword: Bio-Pharmaceutical

Search Result 376, Processing Time 0.025 seconds

Graphiumins I and J, New Thiodiketopiperazines from the Marine-derived Fungus Graphium sp. OPMF00224

  • Fukuda, Takashi;Nagai, Kenichiro;Kurihara, Yuko;Kanamoto, Akihiko;Tomoda, Hiroshi
    • Natural Product Sciences
    • /
    • v.21 no.4
    • /
    • pp.255-260
    • /
    • 2015
  • Two new thiodiketopiperazines (TDKPs), designated graphiumins I (1) and J (2), were isolated from the culture broth of the marine-derived fungus Graphium sp. OPMF00224 by solvent extraction, silica gel column chromatography, and HPLC. Their absolute structures were elucidated by spectroscopic analyses (1D and 2D NMR data, ROESY correlations, and CD data) and chemical methods. They were found to be structurally rare TDKPs with a phenylalanine-derived indolin substructure. Compounds 1 and 2 inhibited yellow pigment production by methicillin-resistant Staphylococcus aureus (MRSA) with $IC_{50}$ values of 63.5 and $76.5{\mu}g/ml$, respectively, without inhibiting its growth, even at $250{\mu}g/ml$.

A novel HDAC6 inhibitor, CKD-504, is effective in treating preclinical models of huntington's disease

  • Endan Li;Jiwoo Choi;Hye-Ri Sim;Jiyeon Kim;Jae Hyun Jun;Jangbeen Kyung;Nina Ha;Semi Kim;Keun Ho Ryu;Seung Soo Chung;Hyun Sook Kim;Sungsu Lee;Wongi Seol;Jihwan Song
    • BMB Reports
    • /
    • v.56 no.3
    • /
    • pp.178-183
    • /
    • 2023
  • Huntington's disease (HD) is a neurodegenerative disorder, of which pathogenesis is caused by a polyglutamine expansion in the amino-terminus of huntingtin gene that resulted in the aggregation of mutant HTT proteins. HD is characterized by progressive motor dysfunction, cognitive impairment and neuropsychiatric disturbances. Histone deacetylase 6 (HDAC6), a microtubule-associated deacetylase, has been shown to induce transport- and release-defect phenotypes in HD models, whilst treatment with HDAC6 inhibitors ameliorates the phenotypic effects of HD by increasing the levels of α-tubulin acetylation, as well as decreasing the accumulation of mutant huntingtin (mHTT) aggregates, suggesting HDAC6 inhibitor as a HD therapeutics. In this study, we employed in vitro neural stem cell (NSC) model and in vivo YAC128 transgenic (TG) mouse model of HD to test the effect of a novel HDAC6 selective inhibitor, CKD-504, developed by Chong Kun Dang (CKD Pharmaceutical Corp., Korea). We found that treatment of CKD-504 increased tubulin acetylation, microtubule stabilization, axonal transport, and the decrease of mutant huntingtin protein in vitro. From in vivo study, we observed CKD-504 improved the pathology of Huntington's disease: alleviated behavioral deficits, increased axonal transport and number of neurons, restored synaptic function in corticostriatal (CS) circuit, reduced mHTT accumulation, inflammation and tau hyperphosphorylation in YAC128 TG mouse model. These novel results highlight CKD-504 as a potential therapeutic strategy in HD.

Sensitive Determination of Felodipine in Human Plasma by LC-MS/MS

  • Kim, Ho-Hyun;Roh, Hyeon-Jin;Lee, He-Joo;Han, Sang-Beom
    • Proceedings of the PSK Conference
    • /
    • 2003.04a
    • /
    • pp.283.2-283.2
    • /
    • 2003
  • This study established a highly sensitive novel quantification method for detecting felodipine in human plasma using LC-MS/MS. The mobile phase used after degassing was composed of 1 mM ammonium acetate and acetonitrile (20:80, pH 6.0), with flow rate of 200 uL/min. One mL plasma were pipetted into glass tubes and spiked with 0.1 mL of internal standard solution. (omitted)

  • PDF

Determination of Glimepiride in Human Plasma by LC-MS/MS

  • Kim, Ho-Hyun;Roh, Hyeong-Jin;Lee, Hee-Joo;Han, Sang-Beom
    • Proceedings of the PSK Conference
    • /
    • 2003.04a
    • /
    • pp.282.1-282.1
    • /
    • 2003
  • This study established a sensitive novel Quantification method for detecting glimepiride in human plasma using LC-MS/MS for pharmacokinetic studies. The mobile phase used after degassing was composed of 10 mM ammonium acetate and acetonitrile (20:80, pH 3.0), with flow rate of 200uL/min. One mL plasma were pipetted into glass tubes and spiked with 0.1 mL of internal standard solution. (omitted)

  • PDF

Gadolinium-Chlorin is Potentially a New Tumor Specific MRI Contrast Agent

  • Kim Jong-Ki;Kim Dong-Myung;Kang Min-Suk;Kim Hae-Kyung;Kim Jeong-Sook;Yu Eun-Kyung;Jeong Jin-Hyun
    • Archives of Pharmacal Research
    • /
    • v.29 no.3
    • /
    • pp.188-190
    • /
    • 2006
  • In this study, a newly-synthesized metalloporphyrin, Gd-chlorin (PB Chlorin), was investigated by using a simple tissue phantom to test its efficacy as an MRI contrast agent. This study demonstrated the potential activity of Gd-chlorin as not only a MRI contrast agent, but also as a PDT photosensitizer by using a simple tissue phantom and conducting a very brief MRI experiment.

Antibacterial and Antioxidant activities of Bio-fermented Sanguisorbae Radix Extract (지유 발효추출물의 항세균 및 항산화 활성)

  • Kil, Ki-Jung;Doh, Eun-Soo;Chang, Jun-Pok;Lee, Seung-Hyun;Yoo, Ji-Hyun
    • The Korea Journal of Herbology
    • /
    • v.30 no.4
    • /
    • pp.29-35
    • /
    • 2015
  • Objectives : The objective of this research was to investigate the antibacterial and antioxidant activities of bio-fermented Sanguisorbae Radix extract.Methods : The Sanguisorbae Radix extract was fermented byStreptococcus thermophilus,and their products was tested for antibacterial activity against pathogenic microorganisms namely,Bacillus cereus,Bacillus subtilis,Staphylococcus aureus,Escherichia coli,Vibrio parahaemolyticusandSalmonella typhimuriumby paper disc diffusion method and the antioxidant activities of extract was evaluated by five different assays as electron donating ability(EDA), superoxide dismutase(SOD)-like activity, polyphenol, flavonoid contents and nitrite scavenging ability.Results : The bio-fermented Sanguisorbae Radix extract was safe from heat. Antibacterial activity of fermented Sanguisorbae Radix extract appeared relatively highly againstBacillus cereusandStaphylococcus aureusand didn't show any difference. EDA in comparison to Vitamin C showed over 90% activity at about the same time of Sanguisorbae Radix extract expressed highly. SOD activity showed 15% in fermentation before and after. The nitrite scavenging ability of Sanguisorbae Radix extract before and after fermentation showed higher numerical value over 70% in pH 2.5 than that of butylated hydroxytoluene(BHT). But SOD activity, EDA and nitrite scavenging ability were not different between the Sanguisorbae Radix extract before and after fermentation. Total polyphenol content expressed over about 20 mg/g, and that of the Sanguisorbae Radix extracts was increased than that of the fermented Sanguisorbae Radix extracts.Conclusions : The results suggest the usefulness of developing functional materials using antioxidant active Sanguisorbae Radix extract was fermented bySalmonella typhimuriumwith high polyphenol contents and nitrite scavenging ability.

Bioequivalence of GomcillinTM Capsule to FamoxinTM Capsule (Amoxicillin 500 mg) (파목신 캅셀(아목시실린 500 mg)에 대한 곰실린 캅셀의 생물학적동등성)

  • Lee, Yun-Young;Choi, Mee-Hee;Lee, Kyung-Ryul;Lee, Hee-Joo
    • Journal of Pharmaceutical Investigation
    • /
    • v.34 no.4
    • /
    • pp.311-317
    • /
    • 2004
  • A bioequivalence study of $Gomcillin^{TM}$ capsules (DAEWOONG Pharmaceutical Co., Korea) to $Famoxin^{TM}$ capsules (Dong Wha Pharm. Ind. Co., Korea) was conducted according to the guideline of Korea Food and Drug Administration (KFDA). Twenty four healthy male Korean volunteers received each medicine at the amoxicillin dose of 500 mg in a $2{\times}2$ crossover study. There was a one-week wash out period between the doses. Plasma concentrations of amoxicillin were monitored by a high-performance liquid chromatography for over a period of 8 hours after the administration. $AUC_t$ (the area under the plasma concentration-time curve from time zero to 8 hr) was calculated by the linear trapezoidal rule method. $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{max}$) were compiled from the plasma concentration-time data. Analysis of variance was carried out using logarithmically transformed $AUC_t$ and $C_{max}$. No significant sequence effect was found for all of the bioavailability parameters indicating that the crossover design was properly performed. The 90% confidence intervals of the $AUC_t$ ratio and the $C_{max}$ ratio for $Gomcillin^{TM}/Famoxin^{TM}$ were $log0.91\;{\sim}\;log1.03$ and $;log0.93\;{\sim}\;log1.10$, respectively. These values were within the acceptable bioequivalence intervals of $log0.80\;{\sim}\;log1.25$. Thus, our study demonstrated the bioequivalence of $Gomcillin^{TM}$ and $Famoxin^{TM}$ with respect to the rate and extent of absorption.