http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
Xanthones from Garcinia paucinervis with in vitro anti-proliferative activity against HL-60 cells
Da-Hong Li,Chen-Xi Li,Cui-Cui Jia,Ya-Ting Sun,Chun-Mei Xue,Jiao Bai,Hui-Ming Hua,Xiao-Qiu Liu,Zhan-Lin Li 대한약학회 2016 Archives of Pharmacal Research Vol.39 No.2
Three new xanthones, paucinervins H–J (1–3), as well as eleven known compounds (4–14), were isolated from the leaves of Garcinia paucinervis. The structures of the new compounds (1–3) were elucidated by 1D, 2D NMR spectra and HR ESIMS. In vitro antiproliferative activity against human promyelocytic leukemia HL-60 cells was tested, among which, compounds 2, 5, 6 and 7 exhibited strong growth inhibitory effects with GI50 values ranging from 1.30 to 9.08 lM, respectively. Preliminary SARs were also discussed.
Da-Hong Li,Jia Guo,Wen Bin,Nan Zhao,Kai-bo Wang,Jian-yong Li,Zhan-Lin Li,Hui-Ming Hua 대한약학회 2016 Archives of Pharmacal Research Vol.39 No.7
Two novel rare chloro-containing benzylisoquinolinealkaloids, thalfoliolosumines A (1) and B (2),along with eight known isoquinoline alkaloids (3–10) wereisolated from the whole plant of Thalictrum foliolosum. The structures of these compounds were elucidated byspectral analyses, including 1D and 2D NMR (COSY,HSQC, HMBC and NOESY) experiments. The antiproliferativeeffects of all the isolated compounds were evaluatedby MTT method against MCF-7, PC-3, and U937cells, and trypan blue method against HL-60 cells. Newcompounds 1 and 2 exhibited moderate in vitro antiproliferativeactivity against MCF-7, PC-3, and HL-60 cells,and good inhibitory effects against U937 cells with IC50values of 7.50 and 6.97 μM, respectively. Compounds 7and 10 showed the strongest in vitro antiproliferative withIC50 values of 0.93 and 1.69 lM against HL-60 cell line. The antioxidant properties were also measured, bisbenzyltetrahydroisoquinolinealkaloids 3–6 showed the strongestantioxidant activities in ABTS assay.
Da-Hua Shi,Jun-Hua Wu,Zhi-Qiang Yan,Li-Na Zhang,Yu-Rong Wang,Chun-Ping Jiang 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.9
To find the multi-target-directed compounds for the treatment of Alzheimer’s disease (AD), we synthesized 7-(4-(diethylamino)butoxy)-5-hydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one, a novel 7-O-modified genistein derivative (GS-14), and investigated its acetylcholinesterase (AChE) inhibitory effect, estrogenic activity and neuroprotective effect. GS-14 acted as a selective AChE inhibitor in vitro, with an IC50 value of 0.17 μM and showed no inhibition activity against butyrylcholinesterase (BuChE). The Lineweaver–Burk plot revealed that GS-14 was a non-competitive AChE inhibitor with a Ki value of 0.23 μM and the molecular docking model indicated that GS-14 interacted with the peripheral anionic site (PAS) of AChE. The MCF-7 proliferation assay demonstrated that GS-14 possessed estrogenic activity and GS-14 exhibited a high specificity for estrogen receptor β (ERβ) with a dissociation constant (Ki) of 2.86 nM compared with that of 1.01 μM for estrogen receptor α (ERα) in the molecular docking study. GS-14 also possessed a neuroprotective effect and showed the best protective effect against the β-amyloid protein-induced injury on SH-SY5Y cells at a concentration of 1 nM. Considering its AChEinhibition activity, estrogenic activity and neuroprotective effect, GS-14 may be a potential multi-target agent for the treatment of AD.
Li, Jun-Qin,Xue, Hui,Zhou, Lan,Dong, Li-Hua,Wei, Da-Peng,Li, Hua Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.18
Objective: The mechanism of action of fatty acid synthase (FASN) in drug tolerance of breast cancer cells with epithelial-mesenchymal transition (EMT) features was investigated. Methods: The breast cancer cell line MCF-7-MEK5 with stably occurring EMT and tumour necrosis factor-${\alpha}$ (TNF-${\alpha}$) tolerance was used as the experimental model, whereas MCF-7 acted as the control. Tumour cells were implanted into nude mice for in vivo analysis, and cerulenin was used as a FASN inhibitor. RT-PCR, real-time quantitative PCR and Western blot were employed to detect the expression of FASN, TNFR-1, TNFR-2, Wnt-1, ${\beta}$-catenin and cytC at the RNA and protein levels. Results: Compared with MCF-7, TNFR-1 expression in MCF-7-MEK5 was slightly changed, TNFR-2 was decreased, and FASN, Wnt-1, ${\beta}$-catenin and cytC were increased. The expression of Wnt-1 and ${\beta}$-catenin in MCF-7-MEK5 decreased after cerulenin treatment, whereas cytC expression increased. Conclusions: The important function of FASN in the drug tolerance of breast cancer may be due to the following mechanisms: FASN downregulated TNFR-2 expression through lipid rafts to make the cells less sensitive to TNF-${\alpha}$, and simultaneously activated the Wnt-$1/{\beta}$-catenin signalling pathway. Thus, cytC expression increased, which provided cells with anti-apoptotic capacity and induced drug tolerance.
Si-ping Deng,Chun-hua Zhu,Jing Sun,Wen-da Wang,Tian-li Wu,Hua-pu Chen,Shang-li Shi,Guang-li Li 한국유전학회 2015 Genes & Genomics Vol.37 No.8
Winged helix/forkhead transcription factor gene 2 (Foxl2) plays a crucial role during early ovarian development in fish. Sex steroids and aromatase inhibitors can regulate gonadal differentiation in teleosts. To address the role of Foxl2 in gonadal differentiation, foxl2 was isolated and characterized from the Hong Kong catfish, Clarias fuscus. Tissue distribution analysis by quantitative real-time PCR (qPCR) showed that the foxl2 mRNA was highest in the ovaries; moderate in the female pituitary and hypothalamus; but weak in the forebrain, liver, testis and male pituitary, with a sexually dimorphic pattern in which there was higher expression overall in females versus males. Treatment of the fries during the period of gonadal differentiation [2–30 days post hatching (dph)] with 17amethyltestosterone (MT), an aromatase inhibitor (letrozole) and 17b-estradiol (E2) affected the expression of foxl2. The expression of foxl2 was highest before gonadal differentiation (12 dph), but decreased significantly after gonadal differentiation (18-30 dph). In addition, MT and letrozole were able to down-regulate foxl2, but E2 up-regulated foxl2 during gonadal morphological differentiation. These results indicate the significant roles of Foxl2 in the gonadal differentiation of C. fuscus.
High-j Proton h11/2 and g7/2 Intruder Bands in 113In
Ma Ke Yan,Lu Jing Bin,Ma Ying Jun,Li Jian,Yang Dong,Sun Wu Ji,Wang Hao,Pan Hao Nan,Wang Jia Qi,Yang Qing Yu,Zhang Da Ming,Zhu Li Hua,Wu Xiao Guang,Zheng Yun,Li Cong Bo 한국물리학회 2020 THE JOURNAL OF THE KOREAN PHYSICAL SOCIETY Vol.76 No.12
Excited states of 113In have been populated through the heavy-ion fusion evaporation reaction 110Pd(7Li, 4n)113In. A new band with the configuration of a proton d5/2 orbital is identified. Two ΔI = 2 intruder bands, built on the πh11/2 and the πg7/2 orbitals, have been extended to spins (63/2-)ħ and (55/2+)ħ, respectively. The negative-parity πh11/2 intruder band shows a smooth increase in aligned spin, which is attributed to a strong proton-neutron interaction. The properties of the positive-parity πg7/2 band are discussed based on tilted axis cranking model calculations, and the features of the antimagnetic rotation for this band are shown after backbend. Furthermore, the contributions of the two-shears-like mechanism, the neutron (gd)ν shell and the core rotation are investigated for the positive-parity πg7/2 band.
Anti-Inflammatory Activity of Sulfur-Containing Compounds from Garlic
Da Yeon Lee,Hua Li,Hyo Jin Lim,이화진,전라옥,류재하 한국식품영양과학회 2012 Journal of medicinal food Vol.15 No.11
We identified four anti-inflammatory sulfur-containing compounds from garlic, and their chemical structures were identified as Z- and E-ajoene and oxidized sulfonyl derivatives of ajoene. The sulfur compounds inhibited the production of nitric oxide (NO) and prostaglandin E2 (PGE2) and the expression of the pro-inflammatory cytokines tumor necrosis factor-α, interleukin-1β, and interleukin-6 in lipopolysaccharide (LPS)-activated macrophages. Western blotting and reverse transcription–polymerase chain reaction analysis demonstrated that these sulfur compounds attenuated the LPS-induced expression of the inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) proteins and mRNA. Moreover, these sulfur-containing compounds suppressed the nuclear factor-κB (NF-κB) transcriptional activity and the degradation of inhibitory-κBα in LPS-activated macrophages. Furthermore, we observed that they markedly inhibited the LPS-induced phosphorylations of p38 mitogen-activated protein kinases and extracellular signal-regulated kinases (ERK) at 20 μM. These data demonstrate that the sulfur compounds from garlic, (Z, E)-ajoene and their sulfonyl analogs, can suppress the LPS-induced production of NO/PGE2 and the expression of iNOS/COX-2 genes by inhibiting the NF-κB activation and the phosphorylations of p38 and ERK. Taken together, these data show that Z- and E-ajoene and their sulfonyl analogs from garlic might have anti-inflammatory therapeutic potential.
Application of Energy Dissipation Technology in High-Rise Buildings
Hu, Da-Zhu,Zhang, Xiao-Xuan,Li, Guo-Qiang,Sun, Fei-Fei,Jin, Hua-Jian Council on Tall Building and Urban Habitat Korea 2021 International journal of high-rise buildings Vol.10 No.2
The principle of energy dissipation technology is to dissipate or absorb the seismic energy input through the deformation or velocity change of dampers installed in the main structure of high-rise buildings, so as to reduce the seismic response of the buildings. With the development of energy dissipation technology, recognized as an effective and new measurement for reducing seismic effects, its application in high-rise buildings has become more and more popular. The appropriate energy dissipation devices suitable for high-rise buildings are introduced in this paper. The effectiveness of energy-dissipation technology for reducing the seismic response of high-rise buildings with various structural forms is demonstrated with a number of actual examples of high-rise buildings equipped with various energy dissipation devices.
Haonan Li,Baojia Sun,Mingying Wang,Xu Hu,Xiang Gao,Sheng-tao Xu,Yongnan Xu,Jin-yi Xu,Hui-Ming Hua,Da-Hong Li 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.11
Diterpenoids are important and widely distributed natural compounds with various biological effects, including antitumor, anti-inflammatory and so on. Great efforts have been put in phytochemistry research on diterpenoids. A number of structural modified derivatives and pharmacophore incorporated hybrids were also designed and synthesized with promising therapeutic effects. Among the hopefuls, enmein-type 6,7-seco-ent-kaurane diterpenoids with unique ring system and stereogenic centers exhibit attractive activities. Based on their lead-like properties, enmein-type diterpenoids are suitable for further medicinal study. The derivatives were biologically evaluated and showed promising activities, which warranted in-depth research for further understanding. In this review, the natural bioactive enmein-type diterpenoids and the synthetic derivatives were comprehensively summarized.
Ze-Hua Zhao,Feng-Zhi Xin,Yaqian Xue,Zhimin Hu,Yamei Han,Fengguang Ma,Da Zhou,Xiao-Lin Liu,Aoyuan Cui,Zhengshuai Liu,Yuxiao Liu,Jing Gao,Qin Pan,Yu Li,Jian-Gao Fan 생화학분자생물학회 2019 Experimental and molecular medicine Vol.51 No.-
Microbial metabolites have emerged as critical components that mediate the metabolic effects of the gut microbiota. Here, we show that indole-3-propionic acid (IPA), a tryptophan metabolite produced by gut bacteria, is a potent anti-non-alcoholic steatohepatitis (NASH) microbial metabolite. Here, we demonstrate that administration of IPA modulates the microbiota composition in the gut and inhibits microbial dysbiosis in rats fed a high-fat diet. IPA induces the expression of tight junction proteins, such as ZO-1 and Occludin, and maintains intestinal epithelium homeostasis, leading to a reduction in plasma endotoxin levels. Interestingly, IPA inhibits NF-κB signaling and reduces the levels of proinflammatory cytokines, such as TNFα, IL-1β, and IL-6, in response to endotoxin in macrophages to repress hepatic inflammation and liver injury. Moreover, IPA is sufficient to inhibit the expression of fibrogenic and collagen genes and attenuate diet-induced NASH phenotypes. The beneficial effects of IPA on the liver are likely mediated through inhibiting the production of endotoxin in the gut. These findings suggest a protective role of IPA in the control of metabolism and uncover the gut microbiome and liver cross-talk in regulating the intestinal microenvironment and liver pathology via a novel dietary nutrient metabolite. IPA may provide a new therapeutic strategy for treating NASH.