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Byun, Hee Sun,Zhou, Wei,Park, InWha,Kang, Kidong,Lee, So-Ra,Piao, Xuezhe,Park, Jin Bong,Kwon, Taeg Kyu,Na, MinKyun,Hur, Gang Min Elsevier 2018 Biochemical pharmacology Vol.158 No.-
<P><B>Abstract</B></P> <P>Despite recent tremendous progress, targeting of TNF-related apoptosis-inducing ligand (TRAIL) as a cancer therapy has limited success in many clinical trials, in part due to inactivation of death inducing signaling complex (DISC)-mediated caspase-8 signaling cascade in highly malignant tumors such as glioblastoma. In this study, screening of constituents derived from <I>Astilbe rivularis</I> for TRAIL-sensitizing activity identified C-27-carboxylated oleanolic acid derivatives (C27OAs) including 3β-hydroxyolean-12-en-27-oic acid (C27OA-1), 3β,6β,7α-trihydroxyolean-12-en-27-oic acid (C27OA-2), and 3β-<I>trans</I>-<I>p</I>-coumaroyloxy-olean-12-en-27-oic acid (C27OA-3) as novel TRAIL sensitizers. Interestingly, these C27OAs did not affect apoptotic cell death induced by either ligation of other death receptor (DR) types, such as TNF and Fas or DNA damaging agents, which suggests that C27OAs effectively and selectively sensitize TRAIL-mediated caspase-8 activation. Mechanistically, C27OAs upregulate the expression of cell surface DR5 and DISC formation without affecting downstream intracellular apoptosis-related proteins. The upregulation of DR5 expression by C27OAs strictly depends on transactivation of C/EBP homology protein, which is regulated through the p38 MAPK pathway, rather than p53 and intracellular reactive oxygen species status. Taken together, our results identify the novel C27OAs as TRAIL sensitizers targeting the upstream DISC assembly of DR5, and provide a rationale for further development of C27OAs for facilitating TRAIL-based chemotherapy in glioblastoma patients.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
A unique cytoplasmic localization of retinoic acid receptor-gamma and its regulations.
Han, Young-Hoon,Zhou, Hu,Kim, Jin-Hee,Yan, Ting-dong,Lee, Kee-Ho,Wu, Hua,Lin, Feng,Lu, Na,Liu, Jie,Zeng, Jin-zhang,Zhang, Xiao-kun American Society for Biochemistry and Molecular Bi 2009 The Journal of biological chemistry Vol.284 No.27
<P>Recent evidence suggests that extranuclear action of retinoid receptors is involved in mediating the pleiotropic effects of retinoids. However, whether they reside in the cytoplasm remains elusive. Here, we showed that retinoic acid receptor-gamma (RARgamma) was cytoplasmic in confluent cells, or when cells were released from serum depletion or treated with growth factors. In studying the regulation of RARgamma subcellular localization, we observed that ectopically overexpressed RARgamma was mainly cytoplasmic irrespective of serum concentration and cell density. The cytoplasmic retention of RARgamma was inhibited by ligand retinoic acid (RA). In addition, coexpression of retinoid X receptor-alpha (RXRalpha) resulted in nuclear localization of RARgamma through their heterodimerization. Mutagenesis studies revealed that a C-terminal fragment of RXRalpha potently prevents RA-induced RARgamma nuclear localization and transcriptional function. Furthermore, our results showed that the cytoplasmic retention of RARgamma was due to the presence of its unique N-terminal A/B domain, which was subject to regulation by p38 MAPK-mediated phosphorylation. Deletion or mutation of the N-terminal A/B domain largely impaired its cytoplasmic localization. Together, our data demonstrate that the subcellular localization of RARgamma is regulated by complex interactions among ligand binding, receptor phosphorylation, and receptor dimerizations.</P>
Sangwoo Nam,Hyo Gyeong Na,Eun Hye Oh,Eunhye Jung,Yeon Hee Lee,Eun Ju Jeong,Yu-Da Ou,Bin Zhou,Sunjoo Ahn,Jin Soo Shin,Soo Bong Han,Yun Young Go 대한약학회 2022 Archives of Pharmacal Research Vol.45 No.4
Zika virus (ZIKV), an arbovirus of the Flaviviridaefamily, has emerged as a signifi cant public healthconcern owing to its association with congenital abnormalitiesand severe neurological sequelae. Thus, there is anurgent need to develop eff ective therapeutic approaches toeffi ciently treat ZIKV infections. This study used phenotypicscreening to identify a series of 1,2,4-oxadiazole derivativesthat possess antiviral activity against ZIKV infection. Subsequently,28 new derivatives were designed, synthesized,and evaluated for this purpose. Among these compounds,4-(5-phenyl-1,2,4-oxadiazol-3-yl)-N-(pyridin-3-ylmethyl)aniline ( 5d ) had potent antiviral activity against ZIKV infections. Furthermore, a structure–activity relationship analysisindicated that a benzyl substitution on the aniline nitrogen ofthis compound improved potency while augmenting its druglikeproperties. In addition, 5d exhibited antiviral activity against various viruses of Flaviviridae family of worldwidepublic health importance, such as dengue, Japanese encephalitisand classical swine fever viruses, indicating its potentialas a lead compound for generating 1,2,4-oxadiazole derivativeswith broad-spectrum anti-fl aviviral properties.
Khan Tahir,Hou Dong-Hai,Zhou Jin-Na,Yang Yin-Long,Yu Hong 한국균학회 2023 Mycobiology Vol.51 No.3
Cordyceps fumosorosea is an important species in the genus of Cordyceps, containing a variety of bioactive compounds, including fumosorinone (FU). This study was a ground-breaking assessment of FU levels in liquid and solid cultures. The present study focused on the impacts of solid-state fermentation (SSF) using solid substrates (wheat, oat, and rice), as well as the effects of fermentation parameters (pH, temperature, and incubation period), on the generation of FU. All the fermentation parameters had significant effects on the synthesis of FU. In a study of 25 C, 5.5 pH, and 21 days of incubation period combinations calculated -to give maximal FU production, it was found that the optimal values were 25 C, 5.5 pH, and 21 days, respectively. In a solid substrate medium culture, FU could be produced from SSF. At 30 days, a medium composed of rice yielded the most FU (798.50mg/L), followed by a medium composed of wheat and oats (640.50 and 450.50mg/L), respectively. An efficient method for increasing FU production on a large scale could be found in this approach. The results of this study might have multiple applications in different industrial fermentation processes.
( In Hyun Hwang ),( Roshan Kulkarni ),( Min Hye Yang ),( Soo Jin Choo ),( Wei Zhou ),( Sang Myung Lee ),( Tae Su Jang ),( Gil Saeng Jeong ),( Hyeun Wook Chang ),( Min Kyun Na ) 영남대학교 약품개발연구소 2015 영남대학교 약품개발연구소 연구업적집 Vol.25 No.-
Four asterosaponins, thornasteroside A (1), versicoside A (2), anasteroside B (3), and asteronylpentaglycoside sulfate (4), were isolated from the predatory starfish Asterias amurensis Lu¨tken. Unlike previous studies focusing on structure elucidation by degradation of the complex saponin molecules, complete nuclear magnetic resonance (NMR) assignment for the intact molecules was accomplished using 600 MHz high magnetic field NMR. The complete set of NMR assignments can help in the structure elucidation of asterosaponins isolated in low yields without resorting to chemical degradation. Furthermore, this approach can be extended to other complex steroidal saponins, which may accelerate the discovery of bioactive secondary metabolites from this invasive starfish species.