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Peng Liao,Shi-Qin Hu,Hong Zhang,Liang-Bi Xu,Jing-Zi Liu,Bin He,Shang-Gao Liao,Yong-Jun Li 대한화학회 2018 Bulletin of the Korean Chemical Society Vol.39 No.3
In our previous studies, we have shown that thiourea compounds containing phosphate esters have potent antitumor activity and can be used as a novel strategy for the development of antitumor agents. Herein, a series of novel phosphonate thioureas 5–38 have been synthesized, which were fully characterized by 1H NMR, 13C NMR spectrum, elemental analysis. Three human cancer cell lines (Bcap-37, BGC-823, and PC-3) have been used to investigate these compounds’ antitumor activities. After the summarization of the structure–activity relationships, we found that the variation of R, R1, and R2 in these novel phosphonate thioureas contribute to the antitumor activities. All these SAR-guided efforts may lead to novel antitumor drugs in the market in the near future.
Liu, Ai Ling,Liao, Hong Qing,Li, Zhi Liang,Liu, Jun,Zhou, Cui Lan,Guo, Zi Fen,Xie, Hong Yan,Peng, Cui Ying Asian Pacific Journal of Cancer Prevention 2016 Asian Pacific journal of cancer prevention Vol.17 No.12
mTOR, the mammalian target of rapamycin, is a conserved serine/threonine kinase which belongs to the phosphatidyl-linositol kinase-related kinase (PIKK) family. It has two complexes called mTORC1 and mTORC2. It is well established that mTOR plays important roles in cell growth, proliferation and differentiation. Over-activation of the mTOR pathway is considered to have a relationship with the development of many types of diseases, including polycystic ovary syndrome (PCOS) and ovarian cancer (OC). mTOR pathway inhibitors, such as rapamycin and its derivatives, can directly or indirectly treat or relieve the symptoms of patients suffering from PCOS or OC. Moreover, mTOR inhibitors in combination with other chemical-molecular agents may have extraordinary efficacy. This paper will discuss links between mTOR signaling and PCOS and OC, and explore the mechanisms of mTOR inhibitors in treating these two diseases, with conclusions regarding the most effective therapeutic approaches.
Zhong-Liu Zhou,Wen-Qing Yin,Xiao-Peng Zou,Dan-Ying Huang,Cui-Liu Zhou,Lian-Mei Li,Ke-Cheng Chen,Zi-Ying Guo,San-Qing Lin 한국응용생명화학회 2014 Applied Biological Chemistry (Appl Biol Chem) Vol.57 No.6
The extraction and solvent partition of the leaves ofEucalyptus citriodora, and repeated column chromatography for n-BuOH fraction yielded a new flavonoid glycoside, citrioside C (1),along with three known flavonoid glycosides (2-4). The latter wereidentified with kaempferol-3-O-β-D-glucopyranosyl (12)-α-L-rhamnoside(2), kaempferol-3-O-α-L-rhamnoside (3), and quercetin-3-O-α-Lrhamnoside(4). Their chemical structures were identified on thebasis of spectroscopic data analyses including NMR, MS, UV, andIR. All constitutents were isolated for the first time from the leavesof Eucalyptus citriodora. The potential antivirus activity of all theisolated compounds was evaluated. Compound 4 showed potentantiviral activity against respiratory syncytial virus with 50%inhibition concentration (IC50) value of 1.9 μg/mL and selectiveindex value of 9.8.
A Novel Method to Estimate the System Damping After Generator Tripping
Bin Zi-Jun,Liu Yun,Hao Si-Peng,Zhu Xin-Yao,Kong Xiang-Ping,Wang Ming-Shen 대한전기학회 2023 Journal of Electrical Engineering & Technology Vol.18 No.2
Generator tripping strategies are generally decided by offline transient stability analysis. However, traditional methods can hardly ensure dynamic stability after GT. Simulation tests show that GT strategies change the topology and the state variables of a power system, which may weaken the system damping after GT. In order to estimate the system damping, this paper proposes a time-varying linearized model under unsteady states based on the virtual equilibrium point (VEP) theory. Then, the changes in dynamic characteristics caused by GT can be represented by the eigenvalues at VEPs before and after GT. An inertia equivalence system is mathematically formulated to analyze the effects of generator inertia, damping ratio, and controllers. Two indices are designed to estimate the system damping changes. Based on the indices, a framework is proposed to improve the current GT strategy decision-making system. The sensitivity analysis and the fault scanning verify the effectiveness and robustness of the proposed method and indices.
Zhou, Zhong-Liu,Yin, Wen-Qing,Zou, Xiao-Peng,Huang, Dan-Ying,Zhou, Cui-Liu,Li, Lian-Mei,Chen, Ke-Cheng,Guo, Zi-Ying,Lin, San-Qing 한국응용생명화학회 2014 Applied Biological Chemistry (Appl Biol Chem) Vol.57 No.6
The extraction and solvent partition of the leaves of Eucalyptus citriodora, and repeated column chromatography for n-BuOH fraction yielded a new flavonoid glycoside, citrioside C (1), along with three known flavonoid glycosides (2-4). The latter were identified with kaempferol-3-O-${\beta}$-$\small{D}$-glucopyranosyl (12)-${\alpha}$-$\small{L}$-rhamnoside (2), kaempferol-3-O-${\alpha}$-$\small{L}$-rhamnoside (3), and quercetin-3-O-${\alpha}$-$\small{L}$-rhamnoside (4). Their chemical structures were identified on the basis of spectroscopic data analyses including NMR, MS, UV, and IR. All constitutents were isolated for the first time from the leaves of Eucalyptus citriodora. The potential antivirus activity of all the isolated compounds was evaluated. Compound 4 showed potent antiviral activity against respiratory syncytial virus with 50% inhibition concentration ($IC_{50}$) value of $1.9{\mu}g/mL$ and selective index value of 9.8.
Ma Chen,Liu Hui,Liu Bo,Zhao Ju-Peng,Zhao Qing-Ying,Song Zi-Jiao,Han Xin,Zhan Guo-Ping 한국응용곤충학회 2022 Journal of Asia-Pacific Entomology Vol.25 No.4
The cacao mealybug, Planococcus lilacinus Cock, is an important quarantine pest. Infested commodity should be subject to appropriate phytosanitary treatment, while irradiation is recommended for the cacao mealybug. Radio-tolerance comparison tests were conducted on the crawler, nymphs, and adult females of P. lilacinus at the X-ray radiation doses of 40, 80, and 120 Gy, respectively. The results showed that irradiation had a strong effect on preventing of development and reproduction; the adult female stage was identified as the most tolerant. During the following dose–response tests, among young and late females X-ray-irradiation (20–100 Gy), the late females were most tolerant when preventing F 1 generation 2nd instars emergence was used as the evaluation criterion. Minimum absorbed dose and its 95 % fiducial limits to provide probit 9 efficacy at 95 % confidence level (100 % mortality/inhibition in an estimated population of 93,616 individuals) were 131.5 Gy (122.5, 142.6 Gy) and 144.4 Gy (132.7, 159.4 Gy), estimating from the probit analysis on dose-mortality data of 1–30 and 1–10-day-old neonates laid by late females, respectively. In the large-scale confirmatory tests, a total of estimating 97,384 late females of P. lilacinus rearing on the pumpkins fruits were irradiated with gamma-ray at the target dose of 135 or 145 Gy (measured doses 126.1–163.0 Gy), which resulted in no F 1 generation 2nd nymphs developing during a 6-week post-treatment period. The treatment efficacy calculated is 99.9969 % at the 95 % confidence level. Therefore, a minimum absorbed dose of 163.0 Gy is recommended for phytosanitary treatment of P. lilacinus in infested commodity.
p13 from group II baculoviruses is a killing-associated gene
( Nan Lu ),( En Qi Du ),( Yang Kun Liu ),( Hong Qiao ),( Lun Guang Yao ),( Zi Shu Pan ),( Song Ya Lu ),( Yi Peng Qi ) 생화학분자생물학회(구 한국생화학분자생물학회) 2012 BMB Reports Vol.45 No.12
p13 gene was first described in Leucania separata multinuclear polyhedrosis virus (Ls-p13) several years ago, but the function of P13 protein has not been experimentally investigated to date. In this article, we indicated that the expression of p13 from Heliothis armigera single nucleocapsid nucleopolyhedrovirus (Ha-p13) was regulated by both early and late promoter. Luciferase assay demonstrated that the activity of Ha-p13 promoter with hr4 enhancer was more than 100 times in heterologous Sf9 cells than that in nature host Hz-AM1 cells. Both Ls-P13 and Ha-P13 are transmembrane proteins. Confocal microscopic analysis showed that both mainly located in the cytoplasm membrane at 48 h. Results of RNA interference indicated that Ha-p13 was a killing-associated gene for host insects H. armigera. The AcMNPV acquired the mentioned killing activity and markedly accelerate the killing rate when expressing Ls-p13. In conclusion, p13 is a killing associated gene in both homologous and heterologous nucleopolyhedrovirus. [BMB Reports 2012; 45(12): 730-735]
Lin, Xiao-Li,Niu, De,Hu, Zi-Liang,Kim, Dae Heon,Jin, Yin Hua,Cai, Bin,Liu, Peng,Miura, Kenji,Yun, Dae-Jin,Kim, Woe-Yeon,Lin, Rongcheng,Jin, Jing Bo Public Library of Science 2016 PLoS genetics Vol.12 No.4
<P>COP1 (CONSTITUTIVE PHOTOMORPHOGENIC 1), a ubiquitin E3 ligase, is a central negative regulator of photomorphogenesis. However, how COP1 activity is regulated by post-translational modifications remains largely unknown. Here we show that SUMO (small ubiquitin-like modifier) modification enhances COP1 activity. Loss-of-function siz1 mutant seedlings exhibit a weak constitutive photomorphogenic phenotype. SIZ1 physically interacts with COP1 and mediates the sumoylation of COP1. A K193R substitution in COP1 blocks its SUMO modification and reduces COP1 activity in vitro and in planta. Consistently, COP1 activity is reduced in siz1 and the level of HY5, a COP1 target protein, is increased in siz1. Sumoylated COP1 may exhibits higher transubiquitination activity than does non-sumoylated COP1, but SIZ1-mediated SUMO modification does not affect COP1 dimerization, COP1-HY5 interaction, and nuclear accumulation of COP1. Interestingly, prolonged light exposure reduces the sumoylation level of COP1, and COP1 mediates the ubiquitination and degradation of SIZ1. These regulatory mechanisms may maintain the homeostasis of COP1 activity, ensuing proper photomorphogenic development in changing light environment. Our genetic and biochemical studies identify a function for SIZ1 in photomorphogenesis and reveal a novel SUMO-regulated ubiquitin ligase, COP1, in plants.</P>
Perforation optimization of hydraulic fracturing of oil and gas well
Zhu, Hai Yan,Deng, Jin Gen,Chen, Zi Jian,An, Feng Chen,Liu, Shu Jie,Peng, Cheng Yong,Wen, Min,Dong, Guang Techno-Press 2013 Geomechanics & engineering Vol.5 No.5
Considering the influences of fluid penetration, casing, excavation processes of wellbore and perforation tunnels, the seepage-deformation finite element model of oil and gas well coupled with perforating technique is established using the tensile strength failure criterion, in which the user-defined subroutine is developed to investigate the dynamic evolvement of the reservoir porosity and permeability. The results show that the increases of perforation angle and decreases of perforation density lead to a higher fracture initiation pressure, while the changes of the perforation diameter and length have no evident influences on the fracture initiation pressure. As for initiation location for the fracture in wellbore, it is on the wellbore face while considering the presence of the casing. By contrast, the fractures firstly initiate on the root of the tunnels without considering casing. Besides, the initial fracture position is also related with the perforation angle. The fracture initiation position is located in the point far away from the wellbore face, when the perforation angle is around $30^{\circ}$; however, when the perforation angle is increased to $45^{\circ}$, a plane fracture is initiated from the wellbore face in the maximum horizontal stress direction; no fractures was found around perforation tunnels, when the angel is close to $90^{\circ}$. The results have been successfully applied in an oilfield, with the error of only 1.1% comparing the fracture initiation pressure simulated with the one from on-site experiment.