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Sharma, Vinay K.,Lee, Ki-Cheul,Joo, Cheon-Ik,Sharma, Niti,Jung, Sang-Hun Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.suppl8
To investigate the possible isosteric replacement of imidazolidinone moiety in 4-phenyl-N-arylsulfonylimidazolidinone for broad and potent anticancer agents, a series of 4-phenyl-l(N)-arylsulfonylimidazolidinones 6a-k, imidazolidinethione analogs 7a-i, and imidazolidine oxime analogs 8a-c were prepared and evaluated for their in vitro anticancer activity against four human cancer cell lines (human lung A549, human colon COLO205, human leukemia K562, human ovary SK-OV-3). Among all the derivatives of N-arylsulfonylimidazolidinone 6a-k, compounds 6f and 6g showed the best inhibition comparable to doxorubicin against all cancer cell lines. Increasing the carbon chain on alkyl moieties of carbamates as shown in 6c-g did not alter the activity. The imidazolidinethione analogs 7a-i and imidazolidin-2-one oxime derivatives 8a-c did not possess any good activity. Therefore, imidazolidinone moiety is the best pharmacophore among the 4-phenyl-Narylsulfonylimidazolidinone derivatives.
Sharma Niti,Park Seung Moon,Kwon Tae Ho,Kim Dae Hyuk,Yang Moon Sik The Korean Society for Biotechnology and Bioengine 2004 Biotechnology and Bioprocess Engineering Vol.9 No.6
A simple purification procedure of bioactive human granulocyte macrophage colony stimulating factor (hGM-CSF) secreted in rice cell suspension culture has previously been described. In this study the protein was purified to apparent homogeneity with an overall yield of $80.1\%$ by ammonium sulfate precipitation and a single chromatographic step involving FPLCanion exchange chromatography. The purified hGM-CSF revealed at least five glycosylated forms ranging from $21.5{\~}29$ kDa, and its biological activity was independent of the glycosylation pattern. This is the first purification report of recombinant hGM-CSF to apparent homogeneity from rice cell suspension cultures.
Production and Secretion of Human Interleukin-18 in Transgenic Tobacco Cell Suspension Culture
Sharma, Niti,Kim, Tae-Geum,Yang, Moon-Sik The Korean Society for Biotechnology and Bioengine 2006 Biotechnology and Bioprocess Engineering Vol.11 No.2
Interleukin-18 (IL-18), otherwise known as interferon-gamma-inducing factor (IGIF), is one of several well characterized and important cytokines that contribute to host defenses. The complementary DNA (cDNA) of mature human interleukin-18 gene (hIL-18) was fused with the signal peptide of the rice amylase 1A gene (Ramy1A) and introduced into the plant expression vector under the control of a duplicated CaMV 35S promoter. The recombinant plasmid was transformed into tobacco (Nicotiana tabacum L. cv Havana) using the Agrobacterium-mediated transformation method. The integration of the hlL-18 gene into the genome of transgenic tobacco plants was confirmed by polymerase chain reaction (PCR) amplification and its expression was observed in the suspension cells that were derived from the transgenic plant callus by using Northern blot analysis. The hlL-18 protein was detected in the extracts of the transgenic callus and in the medium of the transgenic tobacco suspension culture by using immunoblot analysis. Based upon enzyme-linked immunosorbant assay (ELISA) results, the expression level of the hlL-18 protein approximated $166{\mu}g/L$ in the suspension culture medium. Bioassay results from the induction of $interferon-{\gamma}$ from a KG-1 cell line indicated that the hlL-18 secreted into the suspension culture medium was bioactive.
Vinay K. Sharma,이기철,Cheonik Joo,Niti Sharma,정상헌 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.8
To investigate the possible isosteric replacement of imidazolidinone moiety in 4-phenyl-N-arylsulfonylimidazolidinone for broad and potent anticancer agents, a series of 4-phenyl-l(N)-arylsulfonylimidazolidinones 6ak,imidazolidinethione analogs 7a-i, and imidazolidine oxime analogs 8a-c were prepared and evaluated for their in vitro anticancer activity against four human cancer cell lines (human lung A549, human colon COLO205, human leukemia K562, human ovary SK-OV-3). Among all the derivatives of N-arylsulfonylimidazolidinone 6a-k, compounds 6f and 6g showed the best inhibition comparable to doxorubicin against all cancer cell lines. Increasing the carbon chain on alkyl moieties of carbamates as shown in 6c-g did not alter the activity. The imidazolidinethione analogs 7a-i and imidazolidin-2-one oxime derivatives 8a-c did not possess any good activity. Therefore, imidazolidinone moiety is the best pharmacophore among the 4-phenyl-Narylsulfonylimidazolidinone derivatives.
Production and Secretion of Human Interleukin-18 in Transgenic Tobacco Cell Suspension culture
양문식,김태금,Niti Sharma 한국생물공학회 2006 Biotechnology and Bioprocess Engineering Vol.11 No.2
Interleukin-18 (IL-18), otherwise known as interferon-gamma-inducing factor (IGIF), is one of several well characterized and important cytokines that contribute to host defenses. The complementary DNA (cDNA) of mature human interleukin-18 gene (hIL-18) was fused with the signal peptide of the rice amylase 1A gene (Ramy1A) and introduced into the plant expression vector under the control of a duplicated CaMV 35S promoter. The recombinant plasmid was transformed into tobacco (Nicotiana ta-bacum L. cv Havana) using the Agrobacterium-mediated transformation method. The integration of the hIL-18 gene into the genome of transgenic tobacco plants was confirmed by polymerase chain reaction (PCR) amplification and its expression was observed in the suspension cells that were derived from the transgenic plant callus by using Northern blot analysis. The hIL-18 protein was detected in the extracts of the transgenic callus and in the medium of the transgenic tobacco suspension culture by using im-munoblot analysis. Based upon enzyme-linked immunosorbant assay (ELISA) results, the expression level of the hIL-18 protein approximated 166 µg/L in the suspension culture medium. Bioassay results from the induction of interferon-g from a KG-1 cell line indicated that the hIL-18 secreted into the sus-pension culture medium was bioactive.
Synthesis of Water Soluble Analogs of Arylsulfonylimidazolidinone (JSH-2282)
방성철,이기철,Vinay K. Sharma,Niti Sharma,Hyun-Sun Yang,정상헌 대한화학회 2013 Bulletin of the Korean Chemical Society Vol.34 No.7
To improve the water solubility of arylsulfonylimidazolidinone (JSH-2282), a potent anti-cancer agent, two urea derivatives, sodium (S)-2-(3-(4-(5-((S)-2-oxo-4-phenylimidazolidin-1-ylsulfonyl)indoline-1-carbonyl)- phenyl)ureido)succinate (2a) and sodium (S)-2-(3-(4-(5-((S)-2-oxo-4-phenylimidazolidin-1-ylsulfonyl)indoline- 1-carbonyl)phenyl)ureido)pentanedioate (2b), were synthesized and studied for solubility and anti-cancer activity.
양문식,박승문,김대혁,Tae-Ho Kwon,Niti Sharma 한국생물공학회 2004 Biotechnology and Bioprocess Engineering Vol.9 No.6
A simple purification procedure of bioactive human granulocyte macrophage colony stimulating factor (hGM-CSF) secreted in rice cell suspension culture has previously been described. In this study the protein was purified to apparent homogeneity with an overall yield of 80.1% by ammonium sulfate precipitation and a single chromatographic step involving FPLC-anion exchange chromatography. The purified hGM-CSF revealed at least five glycosylated forms ranging from 21.529 kDa, and its biological activity was independent of the glycosylation pattern. This is the first purification report of recombinant hGM-CSF to apparent homogeneity from rice cell suspension cultures.
Eeda Venkateswara Rao,Vinay Kumar Sharma,Niti Sharma,Young-Soo Kim,Sang-Hun Jung 충남대학교 약학대학 의약품개발연구소 2014 藥學論文集 Vol.29 No.-
To define the role of substituents of chalcones as potent MD-2 inhibitors, we designed and synthesized analogs of 1-(2-hydroxy-6-(isopentyloxy)phenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one (1) for their in vitro activities against RAW 264.7 cell using the SEAP assay as well as for LPS displacement assay. Among all the derivatives, compound 5 (IC50=27.3 μM), showed good inhibition of NF-κB activation by blocking the TLR4-mediated NF-κB activation signalling in RAW 264.7 as well as the rhMD-2 binding to immobilized LPS with 53% inhibition at 30 μM. The SAR studies indicated that small alkyl group like 3-methylbutoxy at 6-position of ring A and substituent with hydrogen bonding capability at 4-position of ring B of chalcone should be very important for inhibition of LPS induced NF-κB activation and LPS displacement of MD-2.
Ki-Cheul Lee,Vinay K. Sharma,Niti Sharma,Sang-Hun Jung 충남대학교 약학대학 의약품개발연구소 2012 藥學論文集 Vol.27 No.-
To investigate the anti-proliferate effect of chromenone through inactivation of NF-κB, a series of novel chromenone derivatives 5a-g were prepared and evaluated for their NF-κB inhibition as well as cytotoxicity against three human cancer cell lines namely, NCI-H23 (lung), NUGC-3 (stomach) and PC-3 (prostate). Among all the derivatives, compound 5d showed potent NF-κB inhibition as well as cytotoxicity against all cell lines. The SAR studies revealed that the hydrophobic group such as cyclohexylmethoxy at 5th position of ring A and small size of hydrogen bonding group with electron donating property such as phenolic hydroxyl group at 4th position of ring B are important for NF-κB inhibitory activity and cytotoxicity.
Synthesis of Water Soluble Analogs of Arylsulfonylimidazolidinone (JSH-2282)
Bang, Seong-Cheol,Lee, Ki-Cheul,Sharma, Vinay K.,Sharma, Niti,Yang, Hyun-Sun,Jung, Sang-Hun Korean Chemical Society 2013 Bulletin of the Korean Chemical Society Vol.34 No.7
To improve the water solubility of arylsulfonylimidazolidinone (JSH-2282), a potent anti-cancer agent, two urea derivatives, sodium (S)-2-(3-(4-(5-((S)-2-oxo-4-phenylimidazolidin-1-ylsulfonyl)indoline-1-carbonyl)-phenyl)ureido)succinate (2a) and sodium (S)-2-(3-(4-(5-((S)-2-oxo-4-phenylimidazolidin-1-ylsulfonyl)indoline-1-carbonyl)phenyl)ureido)pentanedioate (2b), were synthesized and studied for solubility and anti-cancer activity.