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- 저자 : Chittiboyina (검색결과 2 건)
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Hwang, In Hyun,Oh, Joonseok,Zhou, Wei,Park, Seoyoung,Kim, Joo-Hyun,Chittiboyina, Amar G.,Ferreira, Daneel,Song, Gyu Yong,Oh, Sangtaek,Na, MinKyun,Hamann, Mark T. American Chemical Society and American Society of 2015 Journal of natural products Vol.78 No.3
<P/><P>Colorectal cancer has emerged as a major cause of death in Western countries. Down-regulation of β-catenin expression has been considered a promising approach for cytotoxic drug formulation. Eight 4,9-friedodrimane-type sesquiterpenoids (<B>1</B>–<B>8</B>) were acquired using the oxidative potential of <I>Verongula rigida</I> on bioactive metabolites from two <I>Smenospongia</I> sponges. Compounds <B>3</B> and <B>4</B> contain a 2,2-dimethylbenzo[<I>d</I>]oxazol-6(2<I>H</I>)-one moiety as their substituted heterocyclic residues, which is unprecedented in such types of meroterpenoids. Gauge-invariant atomic orbital NMR chemical shift calculations were employed to investigate stereochemical details with support of the application of advanced statistics such as CP3 and DP4. Compounds <B>2</B> and <B>8</B> and the mixture of <B>3</B> and <B>4</B> suppressed β-catenin response transcription (CRT) via degrading β-catenin and exhibited cytotoxic activity on colon cancer cells, implying that their anti-CRT potential is, at least in part, one of their underlying antineoplastic mechanisms.</P>
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Bonnie A. Avery,Deepthi Pabbisetty,Lie Li,Abhisheak Sharma,Mahesh K. Gundluru,Amar G. Chittiboyina,John S. Williamson,Mitchell A. Avery 한국약제학회 2018 Journal of Pharmaceutical Investigation Vol.48 No.5
The ultimate goal of this study was to identify an orally active, affordable, potent and safe antimalarial drug based on the natural product artemisinin. During these efforts, a series of novel 7β-hydroxyartemisinin analogs were synthesized and characterized in vitro for their antimalarial activity against Plasmodium falciparum. Heterodimerization of 7β-hydroxyartemisinin provided the asymmetrical carbamate (ARB-89) while homodimerization provided the carbonate (ARB-92). These dimers were found to be highly active in vitro with an IC50 ≤ 0.50 nM against P. falciparum infected human red blood cells (RBC). For further development as potential antimalarial agents, a battery of in vitro and in vivo pharmacokinetic experiments was performed to distinguish the fate of the discovery compounds ARB-89 and ARB-92. Two UPLC-MS methods were developed and validated for the analysis of the compounds. Both ARB- 89 and ARB-92 exhibited moderate affinity (51 and 56%, respectively) to parasitized RBC, which is a perquisite for antimalarial activity. Following a single dose oral and intravenous pharmacokinetic study in rats, ARB-89 displayed a high clearance (92.8 ± 5.6 L/h kg), short elimination half-life ( t1/2, 1.2 ± 0.2 h) and moderate oral bioavailability (23.4%). ARB-89 was found to be excreted unchanged in feces, which may be due to its high lipophilicity, molecular weight and low oral exposure. In an attempt to identify a better lead antimalarial compound, ARB-92 was designed to be more water soluble than ARB-89 by incorporating a protonatable tertiary amine as part of the dimerizing ligand for 7β-hydroxyartemisinin. As anticipated, ARB-92 displayed a lower clearance (2.9 ± 0.7 L/h kg) and subsequently a longer t1/ 2 (2.3 ± 0.2 h) compared to ARB-89. The oral bioavailability of ARB-92 was found to be 34% in rats, a value somewhat better than the marketed artemisinin derivatives artenimol (19.3%), artemether (19.7%) or artesunate (29.5%).
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